Topic Editors

Department of Neuroscience, Biomedicine and Movement Sciences, Biochemistry Section, University of Verona, Strada Le Grazie 8, 37134 Verona, Italy
Department of Pharmacy, University of Salerno, Campus di Fisciano, Salerno, Italy

Natural Products and Drug Discovery

Abstract submission deadline
30 September 2024
Manuscript submission deadline
31 December 2024
Viewed by
66993

Topic Information

Dear Colleagues,

Natural products are the oldest medicaments which have evolved in human history; they have always represented promising lead compounds for new drugs. Indeed, more than 50% of drugs approved in the last four decades are of natural origins.

Natural products and their derivatives have historically given a high contribution to pharmacotherapy, especially for the treatment of cancer, inflammatory and infectious diseases. They are now used for their antibiotic and antimitotic, antidiabetic and anti-metabolite, anti-aging and neuroprotective properties, as well as in antitumor drugs.

Additionally, fruits and vegetables, along with their nutritional constituents, are rich in bioactive compounds, often cited as ‘phytochemicals’, with health-promoting properties. Bioactives occurring in food plants, in particular polyphenols, exert activities that are considered of great interest in the prevention and treatment of diseases largely present in an ageing society.

Thus, natural products as drug leads continue to be highly attractive; however, the strategy for disease-based drug discovery must be achieved in parallel with the investigation of the molecular mechanisms and the intracellular targets of each natural compound.

This General Topic is focused on, but not limited to:

  • Isolation of new active natural compounds and their structural identification;
  • Characterization, purification and stabilization of bioactive natural compounds as well as their derivatives;
  • Bioavailability, enzyme inhibition, neuro-protective, anti-inflammatory, anti-proliferative and anti-bacterial activities of natural products;
  • Biochemical and the signaling pathways involved in the activity of natural compounds;
  • Different therapeutic applications of well-known natural compounds to explore new directions for future research.

The General Topic “Natural Products and Drug Discovery” will include original articles and reviews on in vitro or animal studies together with human studies aimed at defining their efficacy as therapeutic agents.

Dr. Marta Menegazzi
Dr. Sonia Piacente
Topic Editors

Keywords

  • bioactive phytochemicals
  • functional food ingredients
  • chemical identification of natural compounds
  • structure–bioactivity relations
  • mechanism of action
  • inflammatory diseases
  • autoimmune diseases
  • neurodegenerative diseases
  • cardiovascular disease
  • metabolic diseases
  • cancer
  • skin diseases

Participating Journals

Journal Name Impact Factor CiteScore Launched Year First Decision (median) APC
Biomedicines
biomedicines
4.7 5.2 2013 15.4 Days CHF 2600 Submit
Biomolecules
biomolecules
5.5 9.4 2011 16.9 Days CHF 2700 Submit
International Journal of Molecular Sciences
ijms
5.6 8.1 2000 16.3 Days CHF 2900 Submit
Scientia Pharmaceutica
scipharm
2.5 4.6 1930 22.7 Days CHF 1000 Submit
Plants
plants
4.5 6.5 2012 15.3 Days CHF 2700 Submit
Foods
foods
5.2 7.4 2012 13.1 Days CHF 2900 Submit
Molecules
molecules
4.6 7.4 1996 14.6 Days CHF 2700 Submit

Preprints.org is a multidiscipline platform providing preprint service that is dedicated to sharing your research from the start and empowering your research journey.

MDPI Topics is cooperating with Preprints.org and has built a direct connection between MDPI journals and Preprints.org. Authors are encouraged to enjoy the benefits by posting a preprint at Preprints.org prior to publication:

  1. Immediately share your ideas ahead of publication and establish your research priority;
  2. Protect your idea from being stolen with this time-stamped preprint article;
  3. Enhance the exposure and impact of your research;
  4. Receive feedback from your peers in advance;
  5. Have it indexed in Web of Science (Preprint Citation Index), Google Scholar, Crossref, SHARE, PrePubMed, Scilit and Europe PMC.

Published Papers (30 papers)

Order results
Result details
Journals
Select all
Export citation of selected articles as:
14 pages, 1240 KiB  
Article
Uncovering the Chemical Composition and Biological Potentials of Bupleurum lancifolium Hornem. from Jordan
by Nezar Al-Bataineh, Sultan T. Abu-Orabi, Suhair B. Shannag, Hala I. Al-Jaber, Tareq T. Bataineh, Wael A. Al-Zereini and Mahmoud A. Al-Qudah
Molecules 2024, 29(12), 2730; https://doi.org/10.3390/molecules29122730 - 8 Jun 2024
Viewed by 326
Abstract
The current study was designed to uncover the chemistry and bioactivity potentials of Bupleurum lancifolium growing wild in Jordan. In this context, the fresh aerial parts obtained from the plant material were subjected to hydrodistillation followed by GC/MS analysis. The main components of [...] Read more.
The current study was designed to uncover the chemistry and bioactivity potentials of Bupleurum lancifolium growing wild in Jordan. In this context, the fresh aerial parts obtained from the plant material were subjected to hydrodistillation followed by GC/MS analysis. The main components of the HDEO were γ-patchoulene (23.79%), β-dihydro agarofuran (23.50%), α-guaiene (14.11%), and valencene (13.28%). Moreover, the crude thanolic extract was partitioned to afford two main major fractions, the aqueous methanol (BLM) and butanol (BLB). Phytochemical investigation of both fractions, using conventional chromatographic techniques followed by careful inspection of the spectral data for the isolated compounds (NMR, IR, and UV-Vis), resulted in the characterization of five known compounds, including α-spinasteryl (M1), ethyl arachidate (M2), ethyl myristate (M3), quercetin-3-O-β-d-glucopyranosyl-(1-4”)-α-L-rhamnopyranosyl (B1), and isorhamnetin-3-O-β-d-glucopyranosyl-(1-4”)-α-L-rhamnopyranosyl (B2). The TPC, TFC, and antioxidant activity testing of both fractions and HDEO revealed an interesting ABTS scavenging potential of the BLB fraction compared to the employed positive controls, which is in total agreement with its high TP and TF contents. Cytotoxic evaluation tests revealed that BLM had interesting cytotoxic effects on the normal breast cell line MDA-MB-231 (ATCC–HTB-26) and the normal dermal fibroblast (ATCC® PCS-201-012) and normal African green monkey kidney Vero (ATCC-CCL-81) cell lines. Despite both the BLB and BLM fractions showing interesting AChE inhibition activities (IC50 = 217.9 ± 5.3 µg/mL and 139.1 ± 5.6 µg/mL, respectively), the HDEO revealed an interestingly high AChE inhibition power (43.8 ± 2.7 µg/mL) that far exceeds the one observed for galanthamine (91.4 ± 5.2 µg/mL). The HDEO, BLM, and BLB exhbitied no interesting antimicrobial activity against Bacillus cereus, Bacillus subtilis, Staphylococcus aureus, Escherichia coli, or Pseudomonas aeruginosa. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

17 pages, 1324 KiB  
Review
Medicinal Use of Chicory (Cichorium intybus L.)
by Łukasz Duda, Karol Kamil Kłosiński, Grażyna Budryn, Andrzej Jaśkiewicz, Damian Kołat, Żaneta Kałuzińska-Kołat and Zbigniew Włodzimierz Pasieka
Sci. Pharm. 2024, 92(2), 31; https://doi.org/10.3390/scipharm92020031 - 5 Jun 2024
Viewed by 469
Abstract
The aim of this review is to discuss the numerous health-promoting properties of Cichorium intybus L. and bring together a range of publications to broaden knowledge and encourage further research and consideration of the plant use as treatment for a range of conditions. [...] Read more.
The aim of this review is to discuss the numerous health-promoting properties of Cichorium intybus L. and bring together a range of publications to broaden knowledge and encourage further research and consideration of the plant use as treatment for a range of conditions. A comprehensive search of articles in Polish and English from 1986–2022 years was carried out in PubMed, Google Scholar and ScienceDirect using the keywords chicory, Cichorium intybus L., sesquiterpene lactones and their synonyms. Articles were checked for titles, abstracts, and full-text reviews. The first part of the review article discusses chicory, the countries in which it is found, its life cycle or modern cultivation methods, as well as its many uses, which will be discussed in more detail later in the article. The increased interest in plants as medicines or supplements is also briefly mentioned, as well as some limits that are associated with the medical use of plants. In the Results and Discussion section, there is a discussion of the numerous health-promoting properties of Cichorium intybus L. as a whole plant, with its collection of all the components, and we then examine the structure and the individual constituents of Cichorium intybus L. Among these, this article discusses those that can be utilized for causal applications in medicine, including sesquiterpene lactones and polyphenols, mainly known for their anti-cancer properties, although, in this article, their other health-promoting properties are also discussed. The article also examines inulin, a major component of Cichorium intybus L. The Discussion and the Conclusions sections propose directions for more detailed research and the range of factors that may affect specific results, which may have safety implications when used as supplements or medications. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

22 pages, 11727 KiB  
Article
Polyphenol Compound 18a Modulates UCP1-Dependent Thermogenesis to Counteract Obesity
by Xueping Wen, Yufei Song, Mei Zhang, Yiping Kang, Dandan Chen, Hui Ma, Fajun Nan, Yanan Duan and Jingya Li
Biomolecules 2024, 14(6), 618; https://doi.org/10.3390/biom14060618 - 23 May 2024
Viewed by 424
Abstract
Recent studies increasingly suggest that targeting brown/beige adipose tissues to enhance energy expenditure offers a novel therapeutic approach for treating metabolic diseases. Brown/beige adipocytes exhibit elevated expression of uncoupling protein 1 (UCP1), which is a thermogenic protein that efficiently converts energy into heat, [...] Read more.
Recent studies increasingly suggest that targeting brown/beige adipose tissues to enhance energy expenditure offers a novel therapeutic approach for treating metabolic diseases. Brown/beige adipocytes exhibit elevated expression of uncoupling protein 1 (UCP1), which is a thermogenic protein that efficiently converts energy into heat, particularly in response to cold stimulation. Polyphenols possess potential anti-obesity properties, but their pharmacological effects are limited by their bioavailability and distribution within tissue. This study discovered 18a, a polyphenol compound with a favorable distribution within adipose tissues, which transcriptionally activates UCP1, thereby promoting thermogenesis and enhancing mitochondrial respiration in brown adipocytes. Furthermore, in vivo studies demonstrated that 18a prevents high-fat-diet-induced weight gain and improves insulin sensitivity. Our research provides strong mechanistic evidence that UCP1 is a complex mediator of 18a-induced thermogenesis, which is a critical process in obesity mitigation. Brown adipose thermogenesis is triggered by 18a via the AMPK-PGC-1α pathway. As a result, our research highlights a thermogenic controlled polyphenol compound 18a and clarifies its underlying mechanisms, thus offering a potential strategy for the thermogenic targeting of adipose tissue to reduce the incidence of obesity and its related metabolic problems. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

23 pages, 5076 KiB  
Article
Natural Compounds for Bone Remodeling: A Computational and Experimental Approach Targeting Bone Metabolism-Related Proteins
by Alexandros-Timotheos Loukas, Michail Papadourakis, Vasilis Panagiotopoulos, Apostolia Zarmpala, Eleni Chontzopoulou, Stephanos Christodoulou, Theodora Katsila, Panagiotis Zoumpoulakis and Minos-Timotheos Matsoukas
Int. J. Mol. Sci. 2024, 25(9), 5047; https://doi.org/10.3390/ijms25095047 - 6 May 2024
Viewed by 956
Abstract
Osteoporosis, characterized by reduced bone density and increased fracture risk, affects over 200 million people worldwide, predominantly older adults and postmenopausal women. The disruption of the balance between bone-forming osteoblasts and bone-resorbing osteoclasts underlies osteoporosis pathophysiology. Standard treatment includes lifestyle modifications, calcium and [...] Read more.
Osteoporosis, characterized by reduced bone density and increased fracture risk, affects over 200 million people worldwide, predominantly older adults and postmenopausal women. The disruption of the balance between bone-forming osteoblasts and bone-resorbing osteoclasts underlies osteoporosis pathophysiology. Standard treatment includes lifestyle modifications, calcium and vitamin D supplementation and specific drugs that either inhibit osteoclasts or stimulate osteoblasts. However, these treatments have limitations, including side effects and compliance issues. Natural products have emerged as potential osteoporosis therapeutics, but their mechanisms of action remain poorly understood. In this study, we investigate the efficacy of natural compounds in modulating molecular targets relevant to osteoporosis, focusing on the Mitogen-Activated Protein Kinase (MAPK) pathway and the gut microbiome’s influence on bone homeostasis. Using an in silico and in vitro methodology, we have identified quercetin as a promising candidate in modulating MAPK activity, offering a potential therapeutic perspective for osteoporosis treatment. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

13 pages, 1643 KiB  
Article
Quantitative 1H NMR Spectroscopy Method for Determination of Anthraquinone Derivatives in Extracts from Rubia tinctorum L. Roots and Rhizomes
by Vasilii Vasil’ev, Anzhelika Sheremeta, Vasilii Ivlev, Sergey Goriainov, Fadi Hajjar, Cesar Esparza, Evgeniy Platonov, Arkadiy Khromov, Alexandr Kolesnov, Victoria Romashchenko and Gennady Kalabin
Sci. Pharm. 2024, 92(2), 24; https://doi.org/10.3390/scipharm92020024 - 4 May 2024
Viewed by 786
Abstract
The roots and rhizomes of Rubia tinctorum L. have been widely used both for industrial and medicinal purposes for centuries. The primary biologically active substances from Rubia tinctorum L. roots and rhizomes are anthraquinone derivatives such as ruberythric acid and lucidin-3-primeveroside. Their identification [...] Read more.
The roots and rhizomes of Rubia tinctorum L. have been widely used both for industrial and medicinal purposes for centuries. The primary biologically active substances from Rubia tinctorum L. roots and rhizomes are anthraquinone derivatives such as ruberythric acid and lucidin-3-primeveroside. Their identification and quantification are carried out by various analytical methods, requiring a complicated sample preparation as well as special reagents and reference samples. However, NMR spectroscopy has no limitations of this kind. In this work, we have developed and validated a new express and standard-free method for the qualitative and quantitative analysis of ruberythric acid and lucidin-3-primeveroside by 1H NMR spectroscopy in the extracts from the roots and rhizomes of Rubia tinctorum L. In this work, we have optimized the conditions of the sample preparation and registration of 1H NMR spectra, determined the optimal solvent and reference compound and confirmed the obtained results by HPLC-UV-MS. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

35 pages, 705 KiB  
Review
The Analgesic Potential of Litsea Species: A Systematic Review
by May Poh Yik Goh, Raudhatun Na’emah Samsul, Amal Widaad Mohaimin, Hui Poh Goh, Nurul Hazlina Zaini, Nurolaini Kifli and Norhayati Ahmad
Molecules 2024, 29(9), 2079; https://doi.org/10.3390/molecules29092079 - 30 Apr 2024
Viewed by 889
Abstract
Various plant species from the Litsea genus have been claimed to be beneficial for pain relief. The PRISMA approach was adopted to identify studies that reported analgesic properties of plants from the Litsea genus. Out of 450 records returned, 19 primary studies revealed [...] Read more.
Various plant species from the Litsea genus have been claimed to be beneficial for pain relief. The PRISMA approach was adopted to identify studies that reported analgesic properties of plants from the Litsea genus. Out of 450 records returned, 19 primary studies revealed the analgesic potential of nine Litsea species including (1) Litsea cubeba, (2) Litsea elliptibacea, (3) Litsea japonica, (4) Litsea glutinosa, (5) Litsea glaucescens, (6) Litsea guatemalensis, (7) Litsea lancifolia, (8) Litsea liyuyingi and (9) Litsea monopetala. Six of the species, 1, 3, 4, 7, 8 and 9, demonstrated peripheral antinociceptive properties as they inhibited acetic-acid-induced writhing in animal models. Species 1, 3, 4, 8 and 9 further showed effects via the central analgesic route at the spinal level by increasing the latencies of heat stimulated-nocifensive responses in the tail flick assay. The hot plate assay also revealed the efficacies of 4 and 9 at the supraspinal level. Species 6 was reported to ameliorate hyperalgesia induced via partial sciatic nerve ligation (PSNL). The antinociceptive effects of 1 and 3 were attributed to the regulatory effects of their bioactive compounds on inflammatory mediators. As for 2 and 5, their analgesic effect may be a result of their activity with the 5-hydroxytryptamine 1A receptor (5-HT1AR) which disrupted the pain-stimulating actions of 5-HT. Antinociceptive activities were documented for various major compounds of the Litsea plants. Overall, the findings suggested Litsea species as good sources of antinociceptive compounds that can be further developed to complement or substitute prescription drugs for pain management. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

15 pages, 3098 KiB  
Article
β-Sitosterol Mediates Gastrointestinal Smooth Muscle Relaxation Induced by Coccoloba uvifera via Muscarinic Acetylcholine Receptor Subtype 3
by Francisco J. Aguirre-Crespo, José L. Aragón-Gastélum, Eduardo J. Gutiérrez-Alcántara, Pedro Zamora-Crescencio, Diana L. Gómez-Galicia, Diego R. Alatriste-Kurzel, Guzman Alvarez and Emanuel Hernández-Núñez
Sci. Pharm. 2024, 92(2), 19; https://doi.org/10.3390/scipharm92020019 - 5 Apr 2024
Viewed by 1368
Abstract
Coccoloba uvifera is a Mayan medicinal plant, and these leaves are used as antidiarrheal and diuretic agents. In the present work, we develop in-vitro, ex-vivo, in-vivo, and in-silico strategies to evaluate several aqueous extracts of C. uvifera leaves. In vitro tests showed that [...] Read more.
Coccoloba uvifera is a Mayan medicinal plant, and these leaves are used as antidiarrheal and diuretic agents. In the present work, we develop in-vitro, ex-vivo, in-vivo, and in-silico strategies to evaluate several aqueous extracts of C. uvifera leaves. In vitro tests showed that decoction extract (CuDe) presented the best yield and chlorophyll, phenol, and flavonoid content; however, CuDe showed low antioxidant activity (DPPH model). All aqueous extracts exert spasmolytic and vasorelaxant activity in a concentration-dependent manner (ex vivo), and in vivo tests showed that CuDe exerts the best antiperistaltic and diuretic effects. The in-silico analysis suggests that C. uvifera triterpenes act as a ligand of GPCR, and β-sitosterol could act as an antagonist of muscarinic acetylcholine receptor subtype 3 (m3AChR). In the context of aqueous extracts of C. uvifera, β-sitosterol and their heterosides were identified by FTIR and 1H-NMR spectroscopy. The concerted binding of β-sitosterol and other triterpenes within the m3AChR binding site may be relevant for the induction of relaxant effects at the gastrointestinal smooth muscle level. In this context, C. uvifera is a high-value plant species that requires analytical and pharmacological studies to confirm traditional medicinal use. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

14 pages, 3928 KiB  
Article
Protective Effect of Panicum dichotomiflorum in a Rodent Model of Testosterone-Induced Benign Prostatic Hyperplasia
by Eun Bok Baek, Eun-Ju Hong, Jung-Hee Kim, Min Kim, Jongmin Ahn and Hyo-Jung Kwun
Sci. Pharm. 2024, 92(1), 13; https://doi.org/10.3390/scipharm92010013 - 19 Feb 2024
Viewed by 1684
Abstract
Benign prostatic hyperplasia (BPH) is a common disease in aging men. Panicum dichotomiflorum (PD) is an annual grass species of Poaceae that is distributed worldwide. The present study examined whether PD has a protective effect against BPH. BPH was generated in rats by [...] Read more.
Benign prostatic hyperplasia (BPH) is a common disease in aging men. Panicum dichotomiflorum (PD) is an annual grass species of Poaceae that is distributed worldwide. The present study examined whether PD has a protective effect against BPH. BPH was generated in rats by daily subcutaneous administration of testosterone for four weeks. During this period, the rats were also given daily oral gavages of an extract of PD (150 mg/kg). After the final treatment, all animals were euthanized and their prostates were collected and weighed. In BPH model rats, the prostate weight and levels of dihydrotestosterone (DHT) and 5α-reductase expression were inhibited following treatment with PD extract. Testosterone-induced increases in prostate gland epithelial thickness and expression of cyclin D1 and proliferating cell nuclear antigen (PCNA) were markedly suppressed in PD-treated rats, whereas cleaved caspase-3 levels were increased. PD administration also decreased the expression of transforming growth factor (TGF)-β and vascular endothelial growth factor (VEGF), the phosphorylation of Akt, and inflammatory cytokines levels. Taken together, these results show that PD extract protects against testosterone-induced BPH progression by alleviating prostate cell growth and reducing levels of growth factors and inflammatory cytokines, indicating that PD extract may have potential in protecting against BPH. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

14 pages, 2018 KiB  
Article
Effect of Zoapatle (Montanoa tomentosa) on Inflammatory Markers in a Murine Model of Ventricular Hypertrophy
by Carlos Enrique López-Luna, Cruz Vargas-De-León, Rocio Alejandra Gutiérrez-Rojas, Karla Aidee Aguayo-Cerón, Claudia Camelia Calzada-Mendoza, Fengyang Huang, Rodrigo Romero-Nava and Maria Esther Ocharan-Hernandez
Sci. Pharm. 2024, 92(1), 9; https://doi.org/10.3390/scipharm92010009 - 24 Jan 2024
Viewed by 1757
Abstract
Zoapatle, a native plant utilized for centuries in traditional Mexican medicine, is abundantly found in Mesoamerica and northern South America. Pleiotropic effects of this genus have been recognized, primarily inducing alterations in smooth muscle contractility in animal models. The aim of this study [...] Read more.
Zoapatle, a native plant utilized for centuries in traditional Mexican medicine, is abundantly found in Mesoamerica and northern South America. Pleiotropic effects of this genus have been recognized, primarily inducing alterations in smooth muscle contractility in animal models. The aim of this study was to evaluate the effect of Zoapatle on the hypertrophy index and the gene expression of TNF-α, IL-1β, NF-κB, STAT5, and the PRLR in the brain, left ventricle, and renal cortex of rats with isoproterenol-induced cardiac hypertrophy. Three groups were studied, the control group (n = 4), hypertrophy group (n = 4) and hypertrophy group treated with Zoapatle (n = 4). A ventricular hypertrophy model was developed with 150 mg/kg/day of isoproterenol intraperitoneally administered over two days with a 24 h interval between applications. Zoapatle was administered for 28 consecutive days (25 mg/kg). Gene expression was determined with RT-qPCR. Subsequently, a principal component analysis (PCA) was performed using the RNA expression variables. A notably reduced left ventricle mass index was observed in the Zoapatle group. Additionally, Zoapatle administration in cardiac hypertrophy demonstrated a significant decrease in the gene expression of TNF-α, IL-1B, STAT 5, and the PRLR. TNF-α and the transcription factor STAT5 exhibited a similar trend in both the left ventricle and renal cortex, suggesting a correlation with the inflammatory state in these tissues due to ventricular hypertrophy. The findings suggest that Zoapatle reverses the hypertrophy index in a hypertrophy model, concurrently reducing several proinflammatory mediators associated with the hypertrophy index. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

14 pages, 4965 KiB  
Article
Diastereomers of Spheroidal Form and Commercially Available Taxifolin Samples
by Roman P. Terekhov, Evgeny S. Melnikov, Ilya D. Nikitin, Margarita A. Tokareva, Tatyana A. Rodina, Anastasiya D. Savina, Denis I. Pankov, Anastasiya K. Zhevlakova, Vladimir L. Beloborodov and Irina A. Selivanova
Sci. Pharm. 2024, 92(1), 5; https://doi.org/10.3390/scipharm92010005 - 3 Jan 2024
Cited by 1 | Viewed by 2197
Abstract
Taxifolin is a natural polyphenol belonging to the class of flavonoids. The structure of this compound is characterized by the presence of two chiral centers. The spheroidal form of taxifolin (TAXs) has emerged as a promising modification due to enhanced solubility, higher safety [...] Read more.
Taxifolin is a natural polyphenol belonging to the class of flavonoids. The structure of this compound is characterized by the presence of two chiral centers. The spheroidal form of taxifolin (TAXs) has emerged as a promising modification due to enhanced solubility, higher safety profile, and long-term release from solid dosage forms. The study’s objective was to assess the diastereomeric content in TAXs and industrially produced samples of taxifolin. Considering the difference in the physico-chemical properties of diastereomers and based on the literature data, we developed a qualitative HPLC method. The chromatograms were recorded using a diode array detector at 290 nm and a mass spectrometer operated in negative ionization mode. Our data suggest that a biphenyl column and gradient elution using 0.1% formic acid in water and 0.2% formic acid in methanol, with the organic phase gradient from 7% to 21% and a flow rate of 0.65 mL/min for 15 min at 60 °C, provides the best conditions for the separation of taxifolin diastereomers. This method was validated for quantitative analysis. We discovered that the cis-isomer was present in all the analyzed samples, with its quantity ranging from 0.8% to 9.5%. TAXs can be considered a sample enriched with diastereomers. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

13 pages, 4016 KiB  
Article
Inhibitory Effect of Mistletoe Ointment on DNCB-Induced Atopic Dermatitis in BALB/c Mice
by Chang-Eui Hong and Su-Yun Lyu
Sci. Pharm. 2024, 92(1), 3; https://doi.org/10.3390/scipharm92010003 - 29 Dec 2023
Viewed by 1768
Abstract
Atopic dermatitis (AD) is increasingly prevalent globally. However, the frequent and prolonged use of corticosteroids, which are commonly employed for AD treatment, carries potential side effects. Korean mistletoe (Viscum album L. var. coloratum), a perennial parasitic plant, has demonstrated various biological [...] Read more.
Atopic dermatitis (AD) is increasingly prevalent globally. However, the frequent and prolonged use of corticosteroids, which are commonly employed for AD treatment, carries potential side effects. Korean mistletoe (Viscum album L. var. coloratum), a perennial parasitic plant, has demonstrated various biological effects. In this study, we conducted in vivo investigations to determine whether Korean mistletoe possesses anti-inflammatory effects that play pivotal roles in regulating the pathological mechanisms of AD. BALB/c mice with AD-like skin lesions induced by 2,4-dinitrochlorobenzene (DNCB) were utilized to explore the therapeutic effects of 1% and 2% Korean mistletoe extract (KME) ointments. The KME ointment was topically applied to the dorsal surface of the BALB/c mice, and they were categorized into four distinct groups: normal, DNCB-induced, DNCB-induced with 1% KME ointment, and DNCB-induced with 2% KME ointment. Each assessment parameter employed to evaluate the curative impact of the KME ointment displayed improvement with the application of the 1% KME ointment. While the effects observed were less pronounced than those of the 1% KME ointment, the overall therapeutic outcomes were also evident with the utilization of the 2% KME ointment. The results suggest the potential of Korean mistletoe as a viable therapeutic agent for AD. Further investigations are warranted to elucidate the underlying mechanisms of action. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

28 pages, 7007 KiB  
Article
Extreme Gradient Boosting Combined with Conformal Predictors for Informative Solubility Estimation
by Ozren Jovic and Rabah Mouras
Molecules 2024, 29(1), 19; https://doi.org/10.3390/molecules29010019 - 19 Dec 2023
Viewed by 941
Abstract
We used the extreme gradient boosting (XGB) algorithm to predict the experimental solubility of chemical compounds in water and organic solvents and to select significant molecular descriptors. The accuracy of prediction of our forward stepwise top-importance XGB (FSTI-XGB) on curated solubility data sets [...] Read more.
We used the extreme gradient boosting (XGB) algorithm to predict the experimental solubility of chemical compounds in water and organic solvents and to select significant molecular descriptors. The accuracy of prediction of our forward stepwise top-importance XGB (FSTI-XGB) on curated solubility data sets in terms of RMSE was found to be 0.59–0.76 Log(S) for two water data sets, while for organic solvent data sets it was 0.69–0.79 Log(S) for the Methanol data set, 0.65–0.79 for the Ethanol data set, and 0.62–0.70 Log(S) for the Acetone data set. That was the first step. In the second step, we used uncurated and curated AquaSolDB data sets for applicability domain (AD) tests of Drugbank, PubChem, and COCONUT databases and determined that more than 95% of studied ca. 500,000 compounds were within the AD. In the third step, we applied conformal prediction to obtain narrow prediction intervals and we successfully validated them using test sets’ true solubility values. With prediction intervals obtained in the last fourth step, we were able to estimate individual error margins and the accuracy class of the solubility prediction for molecules within the AD of three public databases. All that was possible without the knowledge of experimental database solubilities. We find these four steps novel because usually, solubility-related works only study the first step or the first two steps. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

15 pages, 6479 KiB  
Article
Peony Pollen Protects against Primary Dysmenorrhea in Mice by Inhibiting Inflammatory Response and Regulating the COX2/PGE2 Pathway
by Xu Yang, Yunyuan Tian, Jincai Liu, Yaoyao Kou, Yanhua Xie, Siwang Wang and Ye Zhao
Int. J. Mol. Sci. 2023, 24(24), 17245; https://doi.org/10.3390/ijms242417245 - 8 Dec 2023
Cited by 1 | Viewed by 1155
Abstract
Peony pollen contains multiple nutrients and components and has been used as a traditional Chinese medicine with a long history, but the effect of the treatment of primary dysmenorrhea remains to be clarified. The aim of this study is to investigate the therapeutic [...] Read more.
Peony pollen contains multiple nutrients and components and has been used as a traditional Chinese medicine with a long history, but the effect of the treatment of primary dysmenorrhea remains to be clarified. The aim of this study is to investigate the therapeutic effect of peony pollen on primary dysmenorrhea mice and the potential mechanism. A uterus contraction model in vitro and primary dysmenorrhea mice were used to evaluate the treatment effect of peony pollen on primary dysmenorrhea. The primary dysmenorrhea mice were treated with 62.5 mg/kg, 125 mg/kg, or 250 mg/kg of peony pollen, and the writhing response, latency period, histopathological changes in the uterus, prostaglandin E2 (PGE2) and prostaglandin F2α (PGF2α) levels, and infiltration of neutrophils and macrophages were investigated. Protein expression of interleukin 1 β (IL-1β), interleukin 6 (IL-6), NOD-like receptor thermal protein domain associated protein 3 (NLRP3), cyclooxygenase-2 (COX-2), microsomal prostaglandin-E synthase 1 (mPGEs-1), BCL2-Associated X (Bax), B-cell lymphoma-2 (BCL-2), caspase-3, and cleaved caspase-3 were detected by Western blot, and the oxidative stress related marker malondialdehyde (MDA), superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), and reactive oxygen species (ROS) were evaluated. Peony pollen could attenuate spontaneous or oxytocin-induced uterus contractions in vitro. Moreover, peony pollen decreased the writhing times, prolonged the writhing latency, and reduced the pathological damage of uterine tissues. Furthermore, the inflammatory cell infiltration and the protein expression of IL-1β, IL-6, and NLRP3 were decreased. The COX-2/PGE2 pathway was inhibited; oxidative stress and apoptosis in the uterus also improved in the uterus of primary dysmenorrhea mice. Peony pollen exerts a positive effect on primary dysmenorrhea by inhibiting the inflammatory response and modulating oxidative stress and apoptosis by regulating the COX-2/PGE2 pathway. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

13 pages, 3005 KiB  
Article
Analysis of Beneficial Effects of Flavonoids in Patients with Atherosclerosis Risk on Blood Pressure or Cholesterol during Random Controlled Trials: A Systematic Review and Meta-Analysis
by Rosa Edith Grijalva-Guiza, Thais Lucía Grijalva-Montano, Mariana Cuautle, Enrique Quiroga-González, Luis Ricardo Hernández, Alicia Ortega Aguilar and Aura Matilde Jiménez-Garduño
Sci. Pharm. 2023, 91(4), 55; https://doi.org/10.3390/scipharm91040055 - 22 Nov 2023
Cited by 1 | Viewed by 1884
Abstract
Flavonoids are plant-secondary metabolites with cardiovascular protective properties. Few studies have examined specific flavonoid classes or pure flavonoids concerning some common cardiovascular risks. To obtain information in a systematic review to analyze in a meta-analysis, data were recovered regarding flavonoid intake in random [...] Read more.
Flavonoids are plant-secondary metabolites with cardiovascular protective properties. Few studies have examined specific flavonoid classes or pure flavonoids concerning some common cardiovascular risks. To obtain information in a systematic review to analyze in a meta-analysis, data were recovered regarding flavonoid intake in random controlled trials and atherosclerosis disease, related to risk factors such as blood pressure, total cholesterol (TC), and low-density lipoprotein cholesterol (LDLc). Our aim was to conduct a meta-analysis using the Scopus and PubMed databases without restrictions on the year of publication, extracting articles over the period 1–15 April 2023, searching for randomized controlled trials (RCTs) that investigated different types of flavonoids, measuring blood pressure and low-density cholesterol plasmatic concentration. This paper’s Prospero registration is CRD 42023414153. There were 19 RCTs: twelve RCTs were considered for blood pressure data analysis and fifteen RCTs for total cholesterol and LDL cholesterol data analysis. The meta-analysis showed no significant differences between placebo treatments and treatments with different flavonoids on blood pressure. However, there was a significant difference found in quantitative analysis for TC and LDLc. In conclusion, flavonoid consumption can be associated with a lower risk of LDLc and TC, and more RCTs are needed to specify the effect of more types of pure flavonoids in atherosclerotic patients. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

39 pages, 1357 KiB  
Review
Natural Products for the Treatment of Non-Alcoholic Fatty Liver Disease: A Comprehensive Review
by Saverio Nucera, Rosa Maria Bulotta, Stefano Ruga, Rosamaria Caminiti, Maria Serra, Roberto Bava, Fabio Castagna, Carmine Lupia, Mariangela Marrelli, Filomena Conforti, Giancarlo Statti, Vincenzo Mollace and Ernesto Palma
Sci. Pharm. 2023, 91(4), 53; https://doi.org/10.3390/scipharm91040053 - 8 Nov 2023
Cited by 1 | Viewed by 3592
Abstract
Plants are an untapped natural resource; their secondary metabolites take part in a variety of pharmacological activities, making them an essential ingredient in the synthesis of novel medications and the source of reserve resources in this process. Hepatitis and liver cancer are two [...] Read more.
Plants are an untapped natural resource; their secondary metabolites take part in a variety of pharmacological activities, making them an essential ingredient in the synthesis of novel medications and the source of reserve resources in this process. Hepatitis and liver cancer are two conditions that can result from non-alcoholic fatty liver disease (NAFLD). NAFLD is a condition that now affects a significant section of the global population. There is a need for preventative action on predisposing factors. Due to their effectiveness and few side effects, herbal medications are frequently utilized for the prevention and treatment of NAFLD. This review discusses the pathogenetic processes of NAFLD and the evidence brought to support the potential of botanical species and their derivatives in limiting the causes that predispose to the onset of NAFLD. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

15 pages, 1038 KiB  
Article
Bioactive Compounds from an Endophytic Pezicula sp. Showing Antagonistic Effects against the Ash Dieback Pathogen
by Özge Demir, Haoxuan Zeng, Barbara Schulz, Hedda Schrey, Michael Steinert, Marc Stadler and Frank Surup
Biomolecules 2023, 13(11), 1632; https://doi.org/10.3390/biom13111632 - 8 Nov 2023
Cited by 2 | Viewed by 1344
Abstract
A fungal endophyte originating from the Canary Islands was identified as a potent antagonist against the fungal phytopathogen Hymenoscyphus fraxineus, which causes the devastating ash dieback disease. This endophyte was tentatively identified as Pezicula cf. ericae, using molecular barcoding. Isolation of [...] Read more.
A fungal endophyte originating from the Canary Islands was identified as a potent antagonist against the fungal phytopathogen Hymenoscyphus fraxineus, which causes the devastating ash dieback disease. This endophyte was tentatively identified as Pezicula cf. ericae, using molecular barcoding. Isolation of secondary metabolites by preparative high-performance liquid chromatography (HPLC) yielded the known compounds CJ-17,572 (1), mycorrhizin A (3) and cryptosporioptides A–C (46), besides a new N-acetylated dihydroxyphenylalanin derivative 2, named peziculastatin. Planar structures were elucidated by NMR and HRMS data, while the relative stereochemistry of 2 was assigned by H,H and C,H coupling constants. The assignment of the unknown stereochemistry of CJ-17,572 (1) was hampered by the broadening of NMR signals. Nevertheless, after semisynthetic conversion of 1 into its methyl derivatives 7 and 8, presumably preventing tautomeric effects, the relative configuration could be assigned, whereas comparison of ECD data to those of related compounds determined the absolute configuration. Metabolites 1 and 3 showed significant antifungal effects in vitro against H. fraxineus. Furthermore, 46 exhibited significant dispersive effects on preformed biofilms of S. aureus at concentrations up to 2 µg/mL, while the biofilm formation of C. albicans was also inhibited. Thus, cryptosporioptides might constitute a potential source for the development of novel antibiofilm agents. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

37 pages, 8523 KiB  
Review
Natural Polyketides Act as Promising Antifungal Agents
by Li Wang, Hui Lu and Yuanying Jiang
Biomolecules 2023, 13(11), 1572; https://doi.org/10.3390/biom13111572 - 24 Oct 2023
Cited by 2 | Viewed by 1687
Abstract
Invasive fungal infections present a significant risk to human health. The current arsenal of antifungal drugs is hindered by drug resistance, limited antifungal range, inadequate safety profiles, and low oral bioavailability. Consequently, there is an urgent imperative to develop novel antifungal medications for [...] Read more.
Invasive fungal infections present a significant risk to human health. The current arsenal of antifungal drugs is hindered by drug resistance, limited antifungal range, inadequate safety profiles, and low oral bioavailability. Consequently, there is an urgent imperative to develop novel antifungal medications for clinical application. This comprehensive review provides a summary of the antifungal properties and mechanisms exhibited by natural polyketides, encompassing macrolide polyethers, polyether polyketides, xanthone polyketides, linear polyketides, hybrid polyketide non-ribosomal peptides, and pyridine derivatives. Investigating natural polyketide compounds and their derivatives has demonstrated their remarkable efficacy and promising clinical application as antifungal agents. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

17 pages, 1975 KiB  
Article
In Vitro Inhibitory Activities against α-Glucosidase, α-Amylase, and Pancreatic Lipase of Medicinal Plants Commonly Used in Chocó (Colombia) for Type 2 Diabetes and Obesity Treatment
by Kevin P. Lévuok-Mena, Oscar J. Patiño-Ladino and Juliet A. Prieto-Rodríguez
Sci. Pharm. 2023, 91(4), 49; https://doi.org/10.3390/scipharm91040049 - 18 Oct 2023
Cited by 1 | Viewed by 2077
Abstract
Plant-based therapies are widely utilized for treating diseases in approximately 80% of the global population, including Colombia’s Chocó Department. This study aimed to identify and evaluate plants with significant therapeutic value for obesity and diabetes in Chocó. The inhibitory effects of these plants [...] Read more.
Plant-based therapies are widely utilized for treating diseases in approximately 80% of the global population, including Colombia’s Chocó Department. This study aimed to identify and evaluate plants with significant therapeutic value for obesity and diabetes in Chocó. The inhibitory effects of these plants on pancreatic lipase (PL), α-glucosidase (AG), and α-amylase (AA) were assessed, and the most promising species were selected to isolate and identify bioactive components. Artocarpus altilis, Momordica balsamina, Bauhinia picta, Neurolaena lobata, and Vismia macrophylla emerged as key species based on their traditional usage among the Chocó population. Notably, the extract derived from Vismia macrophylla demonstrated the most encouraging outcomes as a digestive enzyme inhibitor, exhibiting IC50 values of 0.99 ± 0.21 μg/mL, 5.61 ± 0.82 mg/mL, and 28.91 ± 2.10 μg/mL for AG, AA, and PL, respectively. Further chemical analysis led to the isolation of three bioactive compounds: 5′-demethoxycadensin G 1, para-hydroxybenzoic acid methyl ester 2, and para-hydroxybenzoic acid butyl ester 3. Compound 1 displayed the highest activity against AG (IC50 = 164.30 ± 0.11 μM), while compounds 2 (IC50 = 28.50 ± 4.07 μM) and 3 (IC50 = 10.15 ± 3.42 μM) exhibited potent inhibitory effects on PL. Molecular docking and enzymatic kinetics studies indicate that these bioactive compounds primarily act as mixed inhibitors of AG and non-competitive inhibitors of PL. These findings underscore the potential of V. macrophylla and its compounds as effective inhibitors of digestive enzymes associated with obesity and type 2 diabetes. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

25 pages, 8291 KiB  
Article
Neuropharmacological Activity of the Acetonic Extract of Malpighia mexicana A. Juss. and Its Phytochemical Profile
by Dante Avilés-Montes, David Osvaldo Salinas-Sánchez, César Sotelo-Leyva, Alejandro Zamilpa, Franceli Itzel Batalla-Martinez, Rodolfo Abarca-Vargas, Juan Manuel Rivas-González, Óscar Dorado, Rodolfo Figueroa-Brito, Vera L. Petricevich, Dulce Lourdes Morales-Ferra and Manasés González-Cortazar
Sci. Pharm. 2023, 91(4), 47; https://doi.org/10.3390/scipharm91040047 - 10 Oct 2023
Viewed by 1791
Abstract
Mental and neurological disorders are conditions that affect thoughts, emotions, behavior, and relationships. Malpighia mexicana A. Juss. is a plant used in Mexican traditional medicine for the treatment of such disorders. This work aimed to investigate the antidepressant, anxiolytic, sedative, hypnotic, and anticonvulsant [...] Read more.
Mental and neurological disorders are conditions that affect thoughts, emotions, behavior, and relationships. Malpighia mexicana A. Juss. is a plant used in Mexican traditional medicine for the treatment of such disorders. This work aimed to investigate the antidepressant, anxiolytic, sedative, hypnotic, and anticonvulsant effects of the acetonic extract (MmAE) of M. mexicana and its fractions (F3, F4-10, F14) using the forced swimming test (FST), elevated plus maze (EPM), open field test (OFT), pentobarbital-induced sleep test (PBTt), and pentylenetetrazol-induced seizure test (PTZt). MmAE, F3, F4-10, F14, and vehicle were administrated orally 24, 18, and 1 h prior to the evaluations. Imipramine (15 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the FST, while diazepam (1 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the EPM, OFT, PBTt, and PTZt. MmAE had an anxiolytic effect; MmAE and F3, F4-10, and F14 showed an antidepressant effect, sedative effect, hypnotic effect, and anticonvulsant effect. Using HPLC, we identified the compounds quercetin 3-O-rutinoside (1), kaempferol 3-O-glucoside (2), luteolin 7-O-glucoside (3), quercetin (4), and kaempferol (5) in MmAE and compounds (1), (2), and (3) in F14. Using GC-MS, we identified α-tocopherol, phytol, and β-amyrin in F3; β-tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10; and α- tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10. The neuropharmacological effects found in this work may be due to the presence of vitamins, phytosterols, terpenes, and flavonoids. This research requires further study to clarify the mechanisms of action of the identified compounds. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

12 pages, 1141 KiB  
Article
Hypoglycemic and Antihyperglycemic Potential of Flavonoid Fraction from Citrus sinensis (L.) Osbeck in Normoglycemic and Diabetic Rats
by Jesús Alfredo Araujo-León, Maira Rubi Segura-Campos, Rolffy Ortiz-Andrade, Priscila Vazquez-Garcia, Daniela Carvajal-Sánchez, Ángel Cabañas-Wuan, Avel Adolfo González-Sánchez, Jonatan Uuh-Narvaez, Juan Carlos Sánchez-Salgado, Inés Fuentes-Noriega and Zhelmy Martín-Quintal
Sci. Pharm. 2023, 91(4), 46; https://doi.org/10.3390/scipharm91040046 - 27 Sep 2023
Cited by 1 | Viewed by 1814
Abstract
Diabetes is one of the most prevalent diseases worldwide, and the search for therapeutic alternatives in developing countries has been focused on natural products, primarily from plants. This study evaluated the antihyperglycemic and hypoglycemic activities of the albedo (FA) and flavedo (FF) flavonoid [...] Read more.
Diabetes is one of the most prevalent diseases worldwide, and the search for therapeutic alternatives in developing countries has been focused on natural products, primarily from plants. This study evaluated the antihyperglycemic and hypoglycemic activities of the albedo (FA) and flavedo (FF) flavonoid fractions obtained from orange peels (often discarded) in normoglycemic Wistar rats. The flavonoid fractions were identified and quantified using HPLC-UV-DAD and compared with glibenclamide, repaglinide, saxagliptin, and acarbose. Additionally, both fractions were tested in a streptozotocin (65 mg/kg)/nicotinamide (100 mg/kg)-induced diabetic model. In normoglycemic rats, the highest glucose variation (%VG) occurred during the first hour after FA (112.8%) and FF (105.30%) administration at 100 mg/kg, indicating a hypoglycemic effect. In diabetic rats, FF at 100 mg/kg showed the highest %VG (140.41%) during the first hour after administration. HPLC-UV-DAD analysis revealed the presence of hesperidin (HSP) and naringenin (NGN), with the highest concentrations found in FA (HSP: 41.41%; NGN: 10.75%). These findings suggest potential antihyperglycemic effects of FA and FF fractions, possibly attributed to the presence of HSP and NGN. The results obtained in this work lay the foundations to explore the therapeutic applications of orange peels for controlling hyperglycemia in diabetes. In conclusion, our results suggest a reevaluation and revalorization of orange peels, as they contain pharmaceutically relevant flavonoids. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

17 pages, 2506 KiB  
Article
Exposing Salmonella Senftenberg and Escherichia coli Strains Isolated from Poultry Farms to Formaldehyde and Lingonberry Extract at Low Concentrations
by Irena Choroszy-Król, Bożena Futoma-Kołoch, Klaudia Kuźnik, Dorota Wojnicz, Dorota Tichaczek-Goska, Magdalena Frej-Mądrzak, Agnieszka Jama-Kmiecik and Jolanta Sarowska
Int. J. Mol. Sci. 2023, 24(19), 14579; https://doi.org/10.3390/ijms241914579 - 26 Sep 2023
Viewed by 1092
Abstract
European Union (EU) countries strive to improve the quality and safety of food of animal origin. Food production depends on a good microbiological quality of fodder. However, feed can be a reservoir or vector of pathogenic microorganisms, including Salmonella or Escherichia coli bacteria. [...] Read more.
European Union (EU) countries strive to improve the quality and safety of food of animal origin. Food production depends on a good microbiological quality of fodder. However, feed can be a reservoir or vector of pathogenic microorganisms, including Salmonella or Escherichia coli bacteria. Salmonella spp. and E. coli are the two most important food-borne pathogens of public health concern. Contamination with these pathogens, mainly in the poultry sector, can lead to serious food-borne diseases. Both microorganisms can form biofilms on abiotic and biotic surfaces. The cells that form biofilms are less sensitive to disinfectants, which in turn makes it difficult to eliminate them from various surfaces. Because the usage of formaldehyde in animal feed is prohibited in European countries, the replacement of this antibacterial with natural plant products seems very promising. This study aimed to assess the inhibitory effectiveness of Vaccinium vitis-idaea extract against biofilm produced by model Salmonella enterica and E. coli strains. We found that formaldehyde could effectively kill both species of bacterial cells in biofilm, while the lingonberry extract showed some antibiofilm effect on S. enterica serovar Senftenberg. In conclusion, finding natural plant products that are effective against biofilms formed by Gram-negative bacteria is still challenging. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

16 pages, 2042 KiB  
Article
Systematic Exploration of Functional Group Relevance for Anti-Leishmanial Activity of Anisomycin
by Anh Minh Thao Nguyen, Moran Shalev-Benami, Chloé Rosa-Teijeiro, Ana Victoria Ibarra-Meneses, Ada Yonath, Anat Bashan, Charles L. Jaffe, Martin Olivier, Christopher Fernandez-Prada and William D. Lubell
Biomedicines 2023, 11(9), 2541; https://doi.org/10.3390/biomedicines11092541 - 15 Sep 2023
Cited by 1 | Viewed by 1110
Abstract
Assessment of structure–activity relationships for anti-protozoan activity revealed a strategy for preparing potent anisomycin derivatives with reduced host toxicity. Thirteen anisomycin analogs were synthesized by modifying the alcohol, amine, and aromatic functional groups. Examination of anti-protozoal activity against various strains of Leishmania and [...] Read more.
Assessment of structure–activity relationships for anti-protozoan activity revealed a strategy for preparing potent anisomycin derivatives with reduced host toxicity. Thirteen anisomycin analogs were synthesized by modifying the alcohol, amine, and aromatic functional groups. Examination of anti-protozoal activity against various strains of Leishmania and cytotoxicity against leucocytes with comparison against the parent natural product demonstrated typical losses of activity with modifications of the alcohol, amine, and aromatic meta-positions. On the other hand, the para-phenol moiety of anisomycin proved an effective location for introducing substituents without significant loss of anti-protozoan potency. An entry point for differentiating activity against Leishmania versus host has been uncovered by this systematic study. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

56 pages, 25040 KiB  
Review
Saturated Cannabinoids: Update on Synthesis Strategies and Biological Studies of These Emerging Cannabinoid Analogs
by Maite L. Docampo-Palacios, Giovanni A. Ramirez, Tesfay T. Tesfatsion, Alex Okhovat, Monica Pittiglio, Kyle P. Ray and Westley Cruces
Molecules 2023, 28(17), 6434; https://doi.org/10.3390/molecules28176434 - 4 Sep 2023
Cited by 4 | Viewed by 2921
Abstract
Natural and non-natural hexahydrocannabinols (HHC) were first described in 1940 by Adam and in late 2021 arose on the drug market in the United States and in some European countries. A background on the discovery, synthesis, and pharmacology studies of hydrogenated and saturated [...] Read more.
Natural and non-natural hexahydrocannabinols (HHC) were first described in 1940 by Adam and in late 2021 arose on the drug market in the United States and in some European countries. A background on the discovery, synthesis, and pharmacology studies of hydrogenated and saturated cannabinoids is described. This is harmonized with a summary and comparison of the cannabinoid receptor affinities of various classical, hybrid, and non-classical saturated cannabinoids. A discussion of structure–activity relationships with the four different pharmacophores found in the cannabinoid scaffold is added to this review. According to laboratory studies in vitro, and in several animal species in vivo, HHC is reported to have broadly similar effects to Δ9-tetrahydrocannabinol (Δ9-THC), the main psychoactive substance in cannabis, as demonstrated both in vitro and in several animal species in vivo. However, the effects of HHC treatment have not been studied in humans, and thus a biological profile has not been established. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

14 pages, 1976 KiB  
Review
Ethnobotanical Review of Selected Medicinal Plants in Guam for the Treatment of Urinary Tract Ailments and Their Pharmacological Properties
by Sahena Ferdosh
Sci. Pharm. 2023, 91(3), 43; https://doi.org/10.3390/scipharm91030043 - 1 Sep 2023
Viewed by 5309
Abstract
The Chamorro healers of Guam have more than a thousand years of history of using herbs and medicinal plants for the treatment of common ailments. The objective of this study is to review the bioactive compounds and pharmacological properties of medicinal plants which [...] Read more.
The Chamorro healers of Guam have more than a thousand years of history of using herbs and medicinal plants for the treatment of common ailments. The objective of this study is to review the bioactive compounds and pharmacological properties of medicinal plants which are used for urinary tract health by local healers. Literature searches were performed using Google Scholar, ScienceDirect, PubMed, and SpringerLink, by using several keywords, including “medicinal plants in Guam”, “traditional uses”, “bioactive compounds”, “pharmacological properties”, and “urinary tract infections”. This review highlights the traditional uses, bioactive compounds, and pharmacological properties of five medicinal plant species, namely Euphorbia hirta, Phyllanthus amarus, Premna serratifolia, Psidium guajava, and Urena lobata. Phenolics, alkaloids, terpenoids, essential oils, and polypeptides are the leading secondary metabolites reported in different plant extracts, which have been found to have significant antimicrobial, antioxidant, anti-inflammatory, antidiabetic, and anticancer properties. The therapeutic claims made about medicinal plants in Guam are well supported by the literature, having similar applications and pharmacological properties in other regions of the world. These medicinal plants have a lot of unexplored potential that might be utilized to develop more potent drugs for the treatment of infectious diseases, as well as food and herbal supplements. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

29 pages, 2858 KiB  
Review
Essential Oils: Chemistry and Pharmacological Activities
by Damião P. de Sousa, Renan Oliveira S. Damasceno, Riccardo Amorati, Hatem A. Elshabrawy, Ricardo D. de Castro, Daniel P. Bezerra, Vitória Regina V. Nunes, Rebeca C. Gomes and Tamires C. Lima
Biomolecules 2023, 13(7), 1144; https://doi.org/10.3390/biom13071144 - 18 Jul 2023
Cited by 23 | Viewed by 11876
Abstract
In this review, we provide an overview of the current understanding of the main mechanisms of pharmacological action of essential oils and their components in various biological systems. A brief introduction on essential oil chemistry is presented to better understand the relationship of [...] Read more.
In this review, we provide an overview of the current understanding of the main mechanisms of pharmacological action of essential oils and their components in various biological systems. A brief introduction on essential oil chemistry is presented to better understand the relationship of chemical aspects with the bioactivity of these products. Next, the antioxidant, anti-inflammatory, antitumor, and antimicrobial activities are discussed. The mechanisms of action against various types of viruses are also addressed. The data show that the multiplicity of pharmacological properties of essential oils occurs due to the chemical diversity in their composition and their ability to interfere with biological processes at cellular and multicellular levels via interaction with various biological targets. Therefore, these natural products can be a promising source for the development of new drugs. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

20 pages, 861 KiB  
Review
Chromobacterium Violaceum: A Model for Evaluating the Anti-Quorum Sensing Activities of Plant Substances
by Petya D. Dimitrova, Tsvetozara Damyanova and Tsvetelina Paunova-Krasteva
Sci. Pharm. 2023, 91(3), 33; https://doi.org/10.3390/scipharm91030033 - 3 Jul 2023
Cited by 9 | Viewed by 4109
Abstract
In the new antibiotic era, the exponential increase in multiresistant bacterial strains has become the main global health problem. Many researchers have focused their efforts on exploring novel or combined strategies for combating bacterial resistance. Good knowledge of the molecular mechanisms of resistance [...] Read more.
In the new antibiotic era, the exponential increase in multiresistant bacterial strains has become the main global health problem. Many researchers have focused their efforts on exploring novel or combined strategies for combating bacterial resistance. Good knowledge of the molecular mechanisms of resistance and bacterial virulence factors as key targets provides us with a good basis for resolving the problem. One particularly attractive and promising strategy is to attack the main regulatory “network” of bacterial virulence determinants known as quorum sensing (QS). The inhibition of QS signals will be a novel means of screening more effective quorum-sensing inhibitors (QSIs) and will play a key role in the use of next-generation antimicrobials in the battle against resistance. This motivated the present review to provide a comprehensive clarification of the regulatory mechanisms of quorum-sensing signaling pathways in Chromobacterium violaceum and the discovery of potential plant quorum-sensing inhibitors. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

12 pages, 4118 KiB  
Article
Ex Vivo and In Silico Approaches of Tracheal Relaxation through Calcium Channel Blockade of 6-Aminoflavone and Its Toxicological Studies in Murine Models
by Angélica Flores-Flores, Samuel Estrada-Soto, César Millán-Pacheco, Blanca Bazán-Perkins, Rogelio Hernández-Pando, Maximiliano Ibarra-Barajas and Rafael Villalobos-Molina
Biomedicines 2023, 11(7), 1870; https://doi.org/10.3390/biomedicines11071870 - 30 Jun 2023
Viewed by 1268
Abstract
Asthma is a condition in which a person’s airways become inflamed, narrowed, and produce greater amounts of mucus than normal. It can cause shortness of breath, chest pain, coughing, or wheezing. In some cases, symptoms may be exacerbated. Thus, the current study was [...] Read more.
Asthma is a condition in which a person’s airways become inflamed, narrowed, and produce greater amounts of mucus than normal. It can cause shortness of breath, chest pain, coughing, or wheezing. In some cases, symptoms may be exacerbated. Thus, the current study was designed to determine the mechanism of action of 6-aminoflavone (6-NH2F) in ex vivo experiments, as well as to determine its toxicity in acute and sub-chronic murine models. Tissues were pre-incubated with 6-NH2F, and concentration–response curves to carbachol-induced contraction were constructed. Therefore, tracheal rings pre-treated with glibenclamide, 2-aminopyridine, or isoproterenol were contracted with carbachol (1 µM), then 6-NH2F relaxation curves were obtained. In other sets of experiments, to explore the calcium channel role in the 6-NH2F relaxant action, tissues were contracted with KCl (80 mM), and 6-NH2F was cumulatively added to induce relaxation. On the other hand, tissues were pre-incubated with the test sample, and after that, CaCl2 concentration–response curves were developed. In this context, 6-NH2F induced significant relaxation in ex vivo assays, and the effect showed a non-competitive antagonism pattern. In addition, 6-NH2F significantly relaxed the contraction induced by KCl and CaCl2, suggesting a potential calcium channel blockade, which was corroborated by in silico molecular docking that was used to approximate the mode of interaction with the L-type Ca2+ channel, where 6-NH2F showed lower affinity energy when compared with nifedipine. Finally, toxicological studies revealed that 6-NH2F possesses pharmacological safety, since it did not produce any toxic effect in both acute and sub-acute murine models. In conclusion, 6-aminoflavone exerted significant relaxation through calcium channel blockade, and the compound seems to be safe. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

26 pages, 6437 KiB  
Review
Structural Aspect of Hydroxyethyl-Starch–Anticancer-Drug-Conjugates as State-of-the-Art Drug Carriers
by Koushik Chandra, Sansa Dutta, Haradhan Kolya and Chun-Won Kang
Sci. Pharm. 2023, 91(3), 32; https://doi.org/10.3390/scipharm91030032 - 29 Jun 2023
Cited by 2 | Viewed by 2232
Abstract
Cancer is a genetic disorder and its treatment usually requires a long time and expensive diagnosis. While chemotherapy is the most conventional approach in treating most cancers, patients often suffer from undesired side effects due to various pharmacokinetic aspects. To address this issue, [...] Read more.
Cancer is a genetic disorder and its treatment usually requires a long time and expensive diagnosis. While chemotherapy is the most conventional approach in treating most cancers, patients often suffer from undesired side effects due to various pharmacokinetic aspects. To address this issue, target-oriented drug-delivery systems (DDS) or pulsatile drug-delivery systems (PDDS) have recently been developed as an alternative tool that takes care of the entire pharmacodynamic activities of drug action. Hydroxyethyl starch (HES) has emerged as an effective clinical tool for delivering anticancer agents into target cells. These systems have demonstrated significant potential as anticancer drug carrier conjugates through their innate pharmacokinetic properties with their safety profile. This review focuses primarily on the structural aspect during the use of HES or HES-based polymers as carriers for delivering well-known anticancer drugs. This review also indicates a perspective on the long-term research needed for the sake of improving modern drug-delivery systems based on HES polymers and in the form of nanocarriers. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

14 pages, 2512 KiB  
Article
Novel Peptides with Dual Properties for Treating Pseudomonas aeruginosa Keratitis: Antibacterial and Corneal Wound Healing
by Floriana Cappiello, Sudhir Verma, Xiao Lin, Isabel Y. Moreno, Bruno Casciaro, Debarun Dutta, Alison M. McDermott, Mark Willcox, Vivien J. Coulson-Thomas and Maria Luisa Mangoni
Biomolecules 2023, 13(7), 1028; https://doi.org/10.3390/biom13071028 - 23 Jun 2023
Cited by 3 | Viewed by 1881
Abstract
The corneal epithelium is a layer in the anterior part of eye that contributes to light refraction onto the retina and to the ocular immune defense. Although an intact corneal epithelium is an excellent barrier against microbial pathogens and injuries, corneal abrasions can [...] Read more.
The corneal epithelium is a layer in the anterior part of eye that contributes to light refraction onto the retina and to the ocular immune defense. Although an intact corneal epithelium is an excellent barrier against microbial pathogens and injuries, corneal abrasions can lead to devastating eye infections. Among them, Pseudomonas aeruginosa-associated keratitis often results in severe deterioration of the corneal tissue and even blindness. Hence, the discovery of new drugs able not only to eradicate ocular infections, which are often resistant to antibiotics, but also to elicit corneal wound repair is highly demanded. Recently, we demonstrated the potent antipseudomonal activity of two peptides, Esc(1-21) and its diastereomer Esc(1-21)-1c. In this study, by means of a mouse model of P. aeruginosa keratitis and an in vivo corneal debridement wound, we discovered the efficacy of these peptides, particularly Esc(1-21)-1c, to cure keratitis and to promote corneal wound healing. This latter property was also supported by in vitro cell scratch and ELISA assays. Overall, the current study highlights Esc peptides as novel ophthalmic agents for treating corneal infection and injury, being able to display a dual function, antimicrobial and wound healing, rarely identified in a single peptide at the same micromolar concentration range. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Graphical abstract

12 pages, 1922 KiB  
Review
Effectiveness of Zingiber montanum Herbal Compress Remedy for Pain Management: An Updated Systematic Review and Meta-Analysis
by Kanjana Worasing, Bunleu Sungthong and Wiraphol Phimarn
Sci. Pharm. 2023, 91(2), 24; https://doi.org/10.3390/scipharm91020024 - 3 May 2023
Cited by 1 | Viewed by 3072
Abstract
The Zingiber montanum herbal compress remedy is a type of herbal medicine that can be used as an alternative treatment for improving pain symptoms. This study aimed to evaluate the clinical efficacy of a Z. montanum herbal compress remedy for pain relief. PubMed, [...] Read more.
The Zingiber montanum herbal compress remedy is a type of herbal medicine that can be used as an alternative treatment for improving pain symptoms. This study aimed to evaluate the clinical efficacy of a Z. montanum herbal compress remedy for pain relief. PubMed, Scopus, ScienceDirect, and Thai databases were systematically searched for relevant articles published from inception to December 2022. Only randomized clinical trials (RCTs) wherein the efficacy of the Z. montanum remedy was compared to that of a placebo or non-steroidal anti-inflammatory drugs (NSAIDs) were included. Six RCTs with a total of 812 patients were included in the analysis. The efficacy of the Z. montanum remedy had a significantly decreased pain score compared to the placebo (SMD = −0.63; 95% CI = −1.20, −0.06; I2 = 90%), but there was no significant difference when compared to NSAIDs (SMD = −0.61; 95% CI = −1.41, 0.81; I2 = 73%). Moreover, the efficacy of the Z. montanum remedy in terms of the flexibility score (SMD = 0.59; 95% CI −0.56, 1.74; I2 = 86.0%) and quality of life (SMD = 0.34; 95% CI −0.38, 1.05; I2 = 81.0%) was similar to that of the placebo. This meta-analysis demonstrates that the use of the Z. montanum herbal compress remedy significantly reduces the pain scores reported by patients. Full article
(This article belongs to the Topic Natural Products and Drug Discovery)
Show Figures

Figure 1

Back to TopTop