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Search Results (1,514)

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16 pages, 3158 KiB  
Article
Comparative Metabolomics Analysis of Four Pineapple (Ananas comosus L. Merr) Varieties with Different Fruit Quality
by Ping Zheng, Jiahao Wu, Denglin Li, Shiyu Xie, Xinkai Cai, Qiang Xiao, Jing Wang, Qinglong Yao, Shengzhen Chen, Ruoyu Liu, Yuqin Liang, Yangmei Zhang, Biao Deng, Yuan Qin and Xiaomei Wang
Plants 2025, 14(15), 2400; https://doi.org/10.3390/plants14152400 - 3 Aug 2025
Abstract
Understanding the metabolic characteristics of pineapple varieties is crucial for market expansion and diversity. This study performed comparative metabolomic analysis on the “Comte de Paris” (BL) and three Taiwan-introduced varieties: “Tainong No. 11” (XS), “Tainong No. 23” (MG), and “Tainong No. 13” (DM). [...] Read more.
Understanding the metabolic characteristics of pineapple varieties is crucial for market expansion and diversity. This study performed comparative metabolomic analysis on the “Comte de Paris” (BL) and three Taiwan-introduced varieties: “Tainong No. 11” (XS), “Tainong No. 23” (MG), and “Tainong No. 13” (DM). A total of 551 metabolites were identified across the four varieties, with 231 metabolites exhibiting no significant differences between all varieties. This included major sugars such as sucrose, glucose, and fructose, as well as key acids like citric, malic, and quinic acids, indicating that the in-season maturing fruits of different pineapple varieties can all achieve good sugar–acid accumulation under suitable conditions. The differentially accumulated metabolites (DAMs) that were identified among the four varieties all primarily belonged to several major subclasses, including phenolic acids, flavonoids, amino acids and derivatives, and alkaloids, but the preferentially accumulated metabolites in each variety varied greatly. Specifically, branched-chain amino acids (L-leucine, L-isoleucine, and L-valine) and many DAMs in the flavonoid, phenolic acid, lignan, and coumarin categories were most abundant in MG, which might contribute to its distinct and enriched flavor and nutritional value. XS, meanwhile, exhibited a notable accumulation of aromatic amino acids (L-phenylalanine, L-tryptophan), various phenolic acids, and many lignans and coumarins, which may be related to its unique flavor profile. In DM, the dominant accumulation of jasmonic acid might contribute to its greater adaptability to low temperatures during autumn and winter, allowing off-season fruits to maintain good quality. The main cultivar BL exhibited the highest accumulation of L-ascorbic acid and many relatively abundant flavonoids, making it a good choice for antioxidant benefits. These findings offer valuable insights for promoting different varieties and advancing metabolome-based pineapple improvement programs. Full article
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12 pages, 1435 KiB  
Article
Amino Acid Analysis and Cytotoxicity Study of Iraqi Ocimum basilicum Plant
by Omar Hussein Ahmed
Molecules 2025, 30(15), 3232; https://doi.org/10.3390/molecules30153232 - 1 Aug 2025
Viewed by 133
Abstract
Background: This paper deals with the detection of amino acid composition of Iraqi Ocimum basilicum (basil) leaves and evaluation of the cytotoxic effects of the plant leaf extract on human colorectal cancer cells. Methods: Leaves of Ocimum basilicum were collected from Iraq in [...] Read more.
Background: This paper deals with the detection of amino acid composition of Iraqi Ocimum basilicum (basil) leaves and evaluation of the cytotoxic effects of the plant leaf extract on human colorectal cancer cells. Methods: Leaves of Ocimum basilicum were collected from Iraq in November 2024. After drying and powdering, the plant material went through cold methanol extraction. Initial phytochemical screening was conducted to identify the presence of alkaloids, flavonoids, coumarins, and terpenoids. Amino acid analysis was completed by an amino acid analyzer with fluorescence detection. The cytotoxic effect was evaluated via the MTT assay on HRT-18 cell lines. Morphological changes were further tested using dual Propidium Iodide/Acridine Orange assay fluorescent staining. Results: Seventeen amino acids were detected in the plant extract. The extract showed dose-dependent cytotoxic effects on HRT-18 cells, with significant reduction in cell viability at concentrations of more than 25 µg/mL. Morphological alterations of membrane blebbing and cell shrinkage were observed, suggesting apoptotic activity. The IC50 value confirmed strong cytotoxic potential. Conclusions: The extract of Ocimum basilicum leaf cultivated in Iraq shows a rich amino acid profile and significant cytotoxic activity against colorectal cancer cells that highlights its potential effect as a natural source of anticancer compounds. Full article
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28 pages, 2898 KiB  
Review
Chemical Composition and Biological Activities of Pelargonium sp.: A Review with In Silico Insights into Potential Anti-Inflammatory Mechanism
by Diana Celi, Karina Jimenes-Vargas, António Machado, José Miguel Álvarez-Suárez and Eduardo Tejera
Molecules 2025, 30(15), 3198; https://doi.org/10.3390/molecules30153198 - 30 Jul 2025
Viewed by 187
Abstract
The Pelargonium genus, encompassing over 280 species, remains markedly underexplored despite extensive traditional use for respiratory, gastrointestinal, and dermatological disorders. This review of aqueous, alcoholic, and hydroalcoholic extracts reveals critical research gaps: only 10 species have undergone chemical characterization, while 17 have been [...] Read more.
The Pelargonium genus, encompassing over 280 species, remains markedly underexplored despite extensive traditional use for respiratory, gastrointestinal, and dermatological disorders. This review of aqueous, alcoholic, and hydroalcoholic extracts reveals critical research gaps: only 10 species have undergone chemical characterization, while 17 have been evaluated for biological activities. Phytochemical analysis identified 252 unique molecules across all studies, with flavonoids emerging as the predominant class (n = 108). Glycosylated derivatives demonstrated superior bioactivity profiles compared to non-glycosylated analogs. Phenolic acids (n = 43) and coumarins (n = 31) represented additional major classes. Experimental studies primarily documented antioxidant, antibacterial, and anti-inflammatory effects, with emerging evidence for antidiabetic, anticancer, and hepatoprotective activities. However, methodological heterogeneity across studies limits comparative analysis and comprehensive understanding. In silico target prediction analysis was performed on 197 high-confidence molecular structures. Glycosylated flavonols, anthocyanidins, flavones, and coumarins showed strong predicted interactions with key inflammatory targets (ALOX15, ALOX5, PTGER4, and NOS2) and metabolic regulators (GSK3A and PI4KB), providing mechanistic support for observed therapeutic effects and suggesting potential applications in chronic inflammatory and metabolic diseases. These findings underscore the substantial therapeutic potential of underexplored Pelargonium species and advocate for systematic research employing untargeted metabolomics, standardized bioassays, and compound-specific mechanistic validation to fully unlock the pharmacological potential of this diverse genus. Full article
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29 pages, 4148 KiB  
Article
Metabolomic and Pharmacological Approaches for Exploring the Potential of Tanacetum parthenium L. Root Culture as a Source of Bioactive Phytochemicals
by Aurelio Nieto-Trujillo, Rosendo Luria-Pérez, Francisco Cruz-Sosa, Carmen Zepeda-Gómez, María G. González-Pedroza, Cristina Burrola-Aguilar, Armando Sunny, José Correa-Basurto, José A. Guerrero-Analco, Juan L. Monribot-Villanueva and María Elena Estrada-Zúñiga
Int. J. Mol. Sci. 2025, 26(15), 7209; https://doi.org/10.3390/ijms26157209 - 25 Jul 2025
Viewed by 549
Abstract
Tanacetum parthenium (Asteraceae) has been traditionally used worldwide for medicinal purposes, and some of its therapeutic uses have been attributed to the pharmacological effects of its secondary metabolites. The root culture of this species might represent a sustainable source of several pharmacologically active [...] Read more.
Tanacetum parthenium (Asteraceae) has been traditionally used worldwide for medicinal purposes, and some of its therapeutic uses have been attributed to the pharmacological effects of its secondary metabolites. The root culture of this species might represent a sustainable source of several pharmacologically active compounds. The biomass of a root T. parthenium culture was extracted with methanol and fractionated using column chromatography. Three selected fractions (4TP, 5TP, and 8TP) were analyzed via spectrophotometric, chromatographic, and mass spectrometry techniques and in vitro pharmacological assays. The greatest values for total phenolic and phenolic acid contents and antibacterial activity against Escherichia coli were determined for 4TP. The highest values for total flavonoid and sesquiterpene lactone contents, antioxidant potential, and α-amylase inhibitory effect were determined for 8TP. The antibacterial effect against Staphylococcus aureus was not significantly different among the three fractions. The root culture of T. parthenium is a potential source of several metabolites, such as phenolic acids, fatty acids, coumarins, sesquiterpenoids, and triterpenoids, which are capable of exerting α-amylase inhibition and antioxidant, antibacterial, and cytotoxic effects. Among eight phenolic compounds detected and quantified in the fractions, chlorogenic acid was the most abundant. Full article
(This article belongs to the Special Issue Plant Phenolic Accumulation and Application in Human Diseases)
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22 pages, 3896 KiB  
Article
Anti-Inflammatory Pharmacological Mechanism Mediated by the Conversion of Glycosides to Aglycones in Fangfeng (Saposhnikoviae Radix) in Rheumatoid Arthritis Models Based on Serum Metabolomics, Network Pharmacology, and Molecular Docking
by Wenguang Jing, Xiaoyu Lin, Wenmin Pi, Fangliang He, Haonan Wu, Xianrui Wang, Jia Chen, Xianlong Cheng, Penglong Wang and Feng Wei
Int. J. Mol. Sci. 2025, 26(15), 7088; https://doi.org/10.3390/ijms26157088 - 23 Jul 2025
Viewed by 160
Abstract
This study aims to explore the anti-inflammatory pharmacological components and anti-inflammatory mechanisms of the alcohol extract of Saposhnikoviae Radix (SR). The components of the alcohol extract of SR were analyzed using the UPLC-MS/MS system. The anti-inflammatory efficacy of the alcohol extract and core [...] Read more.
This study aims to explore the anti-inflammatory pharmacological components and anti-inflammatory mechanisms of the alcohol extract of Saposhnikoviae Radix (SR). The components of the alcohol extract of SR were analyzed using the UPLC-MS/MS system. The anti-inflammatory efficacy of the alcohol extract and core components of SR was evaluated using the LPS-induced inflammation model of RAW264.7 cells. The anti-inflammatory mechanism of SR in a mouse model of rheumatoid arthritis was expounded by means of serum metabolomics, network pharmacology, and molecular docking. A total of 12 chromones and 13 coumarins were identified in the alcohol extract of SR. The alcohol extract of SR and its components all had good anti-inflammatory activities. In the mouse model of rheumatoid arthritis, the glycoside compounds of SR were transformed into aglycones, thereby exerting anti-inflammatory effects. Moreover, the alcohol extract of SR alleviated the inflammatory response by up-regulating the expression levels of metabolites such as phenylalanine and tyrosine. Network pharmacology and molecular docking results show that SR could exert an anti-inflammatory effect by regulating AGE-RAGE, PI3K-Akt, TNF, MAPK, and Toll-like signaling pathways. In this study, the anti-inflammatory efficacy and mechanisms of the alcohol extract of SR are explored, with the aim of providing a reference for subsequent research. Full article
(This article belongs to the Section Molecular Pharmacology)
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48 pages, 2454 KiB  
Review
How Can Plant-Derived Natural Products and Plant Biotechnology Help Against Emerging Viruses?
by Gergana Zahmanova, Katerina Takova, Valeria Tonova, Ivan Minkov, Momchil Barbolov, Neda Nedeva, Deyana Vankova, Diana Ivanova, Yoana Kiselova-Kaneva and Georgi L. Lukov
Int. J. Mol. Sci. 2025, 26(15), 7046; https://doi.org/10.3390/ijms26157046 - 22 Jul 2025
Viewed by 1534
Abstract
Infectious diseases have been treated using plants and their compounds for thousands of years. This knowledge has enabled modern techniques to identify specific antiviral remedies and to understand their molecular mechanism of action. Numerous active phytochemicals, such as alkaloids, terpenoids, polyphenols (phenolic acids, [...] Read more.
Infectious diseases have been treated using plants and their compounds for thousands of years. This knowledge has enabled modern techniques to identify specific antiviral remedies and to understand their molecular mechanism of action. Numerous active phytochemicals, such as alkaloids, terpenoids, polyphenols (phenolic acids, flavonoids, stilbenes, and lignans), coumarins, thiophenes, saponins, furyl compounds, small proteins, and peptides, are promising options for treating and preventing viral infections. It has been shown that plant-derived products can prevent or inhibit viral entry into and replication by host cells. Biotechnological advances have made it possible to engineer plants with an increased capacity for the production and accumulation of natural antiviral compounds. Plants can also be engineered to produce various types of antivirals (cytokines, antibodies, vaccines, and lectins). This study summarizes the current understanding of the antiviral activity of specific plant-derived metabolites, emphasizing their mechanisms of action and exploring the enormous potential of plants as biological factories. Full article
(This article belongs to the Special Issue Molecular Insights in Antivirals and Vaccines)
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21 pages, 3372 KiB  
Article
Advanced Research on Biological Properties—A Study on the Activity of the Apis mellifera Antioxidant System and the Crystallographic and Spectroscopic Properties of 7-Diethylamino-4-hydroxycoumarin
by Klaudia Rząd, Iwona Budziak-Wieczorek, Aneta Strachecka, Patrycja Staniszewska, Adam Staniszewski, Anna Gryboś, Alicja Matwijczuk, Bożena Gładyszewska, Karolina Starzak, Anna A. Hoser, Maurycy E. Nowak, Małgorzata Figiel, Sylwia Okoń and Arkadiusz Paweł Matwijczuk
Int. J. Mol. Sci. 2025, 26(14), 7015; https://doi.org/10.3390/ijms26147015 - 21 Jul 2025
Viewed by 428
Abstract
The search for substances that increase the immunity of bees is becoming a necessity in the era of various environmental threats and the declining immunocompetence of these insects. Therefore, we tested the biological and physicochemical properties of 7-diethylamino-4-hydroxycoumarin (7DOC). In a cage test, [...] Read more.
The search for substances that increase the immunity of bees is becoming a necessity in the era of various environmental threats and the declining immunocompetence of these insects. Therefore, we tested the biological and physicochemical properties of 7-diethylamino-4-hydroxycoumarin (7DOC). In a cage test, two groups of bees were created: a control group fed with sugar syrup and an experimental group fed with sugar syrup with the addition of 7DOC. In each group, the longevity of the bees was determined and the protein concentrations and antioxidant activities in the bees’ hemolymph were determined. The bees fed with 7DOC lived 2.7 times longer than those in the control group. The protein concentrations and activities of SOD, CAT, GPx and GST, as well as the TAC levels, were significantly higher in the hemolymph of the supplemented workers. To confirm these potent biological properties of 7DOC, the UV-Vis spectra, emission and excitation of fluorescence, synchronous spectra and finally the fluorescence lifetimes of this compound were measured using the time-correlated single photon counting method, in various environments differing in polarity and in the environment applied in bee research. This compound was shown to be sensitive to changes in solvent polarity. The spectroscopic assays were complemented with crystallographic tests of the obtained monocrystals of the aforementioned compounds, which attested to the aggregation effects observed in the spectra measurements for the selected coumarin. The research results confirm that this compound has the potential to be implemented in apiary management, which will be our application goal, but further research into apiary conditions is required. Full article
(This article belongs to the Section Bioactives and Nutraceuticals)
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16 pages, 3376 KiB  
Article
Evidence of the Differences Between Human and Bovine Serum Albumin Through the Interaction with Coumarin-343: Experimental (ICD) and Theoretical Studies (DFT and Molecular Docking)
by Carmen Regina de Souza, Maurício Ikeda Yoguim, Nathalia Mariana Pavan, Nelson Henrique Morgon, Valdecir Farias Ximenes and Aguinaldo Robinson de Souza
Biophysica 2025, 5(3), 27; https://doi.org/10.3390/biophysica5030027 - 15 Jul 2025
Viewed by 242
Abstract
Coumarins are known for interacting with proteins and exhibiting diverse biological activities. This study investigates the interaction between coumarin-343 (C343) and human (HSA) and bovine (BSA) serum albumins. Fluorescence spectroscopy and theoretical simulations, including density functional theory (DFT) and molecular docking, were used [...] Read more.
Coumarins are known for interacting with proteins and exhibiting diverse biological activities. This study investigates the interaction between coumarin-343 (C343) and human (HSA) and bovine (BSA) serum albumins. Fluorescence spectroscopy and theoretical simulations, including density functional theory (DFT) and molecular docking, were used to analyze the ligand–protein complex formation. The fluorescence quenching data revealed that C343 binds to both proteins, with binding constants of 2.1 × 105 mol·L−1 (HSA) and 6.5 × 105 mol·L−1 (BSA), following a 1:1 stoichiometry. Binding site markers identified drug site I (DS1), located in subdomain IIA, as the preferential binding region for both proteins. Computational results supported these findings, showing high affinity for DS1, with binding energies of −69.02 kcal·mol−1 (HSA) and −67.22 kcal·mol−1 (BSA). While complex formation was confirmed for both proteins, differences emerged in the induced circular dichroism (ICD) signals. HSA displayed a distinct ICD profile compared to BSA in both intensity and absorption maximum. Molecular Docking revealed that the C343 conformation differed between HSA and BSA, explaining the variation in ICD signals. These results highlight the importance of protein structure in modulating ligand interactions and spectral responses. Full article
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41 pages, 5101 KiB  
Review
Dual Inhibitors of Acetylcholinesterase and Monoamine Oxidase-B for the Treatment of Alzheimer’s Disease
by Ayesha Asim, Michał K. Jastrzębski and Agnieszka A. Kaczor
Molecules 2025, 30(14), 2975; https://doi.org/10.3390/molecules30142975 - 15 Jul 2025
Viewed by 545
Abstract
Alzheimer’s disease (AD) is a multi-factorial neurodegenerative disease with a complex pathomechanism that can be best treated with multi-target medications. Among the possible molecular targets involved in AD, acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) are well recognized because they control the neurotransmitters [...] Read more.
Alzheimer’s disease (AD) is a multi-factorial neurodegenerative disease with a complex pathomechanism that can be best treated with multi-target medications. Among the possible molecular targets involved in AD, acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) are well recognized because they control the neurotransmitters responsible for memory processes. This review discusses the current understanding of AD pathology, recent advances in AD treatment, and recent reports in the field of dual AChE/MAO-B inhibitors for treating AD. We provide a classification of dual inhibitors based on their chemical structure and describe active compounds belonging to, i.a., chalcones, coumarins, chromones, imines, and hydrazones. Special emphasis is given to the computer-aided strategies of dual inhibitors design, their structure–activity relationships, and their interactions with the molecular targets at the molecular level. Full article
(This article belongs to the Section Medicinal Chemistry)
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13 pages, 3561 KiB  
Article
Preparing Surface-Functionalized Polymer Films with Hierarchically Ordered Structure by a Combination of Nanoimprinting and Controlled Graft Polymerization
by Masahiko Minoda, Daichi Shimizu, Tatsuya Nohara and Jin Motoyanagi
Surfaces 2025, 8(3), 48; https://doi.org/10.3390/surfaces8030048 - 11 Jul 2025
Viewed by 279
Abstract
It is widely recognized that fine surface structures found in nature contribute to surface functionality, and studies on the design of functional materials based on biomimetics have been actively conducted. In this study, polymer thin films with hierarchically ordered surface structure were prepared [...] Read more.
It is widely recognized that fine surface structures found in nature contribute to surface functionality, and studies on the design of functional materials based on biomimetics have been actively conducted. In this study, polymer thin films with hierarchically ordered surface structure were prepared by combining both nanoimprinting using anodically oxidized porous alumina (AAO) as a template and surface-initiated atom transfer radical polymerization (SI-ATRP). To prepare such polymer films, we designed a new copolymer (poly{[2-(4-methyl-2-oxo-2H-chromen-7-yloxy)ethyl methacrylate]-co-[2-(2-bromo-2-methylpropionyloxy)ethyl methacrylate]}; poly(MCMA-co-HEMABr)) with coumarin moieties and α-haloester moieties in the pendants. The MCMA repeating units function to fix the pillar structure by photodimerization, and the HEMABr ones act as the polymerization initiation sites for SI-ATRP on the pillar surfaces. Surface structures consisting of vertically oriented multiple pillars were fabricated on the spin-coated poly(MCMA-co-HEMABr) thin films by nanoimprinting using an AAO template. Then, the coumarin moieties inside each pillar were crosslinked by UV light irradiation to fix the pillar structure. SEM observation confirmed that the internally crosslinked pillar structures were maintained even when immersed in organic solvents such as 1,2-dichloroethane and anisole, which are employed as solvents under SI-ATRP conditions. Finally, poly(2,2,2-trifluoroethyl methacrylate) and poly(N-isopropylacrylamide) chains were grafted onto the thin film by SI-ATRP, respectively, to prepare the hierarchically ordered surface structure. Furthermore, in this study, the surface properties as well as the thermoresponsive hydrophilic/hydrophobic switching of the obtained polymer films were investigated. The surface morphology and chemistry of the films with and without pillar structures were compared, especially the interfacial properties expressed as wettability. Grafting poly(TFEMA) increased the static contact angle for both flat and pillar films, and the con-tact angle of the pillar film surface increased from 104° for the flat film sample to 112°, suggesting the contribution of the pillar structure. Meanwhile, the pillar film surface grafted with poly(NIPAM) brought about a significant change in wettability when changing the temperature between 22 °C and 38 °C. Full article
(This article belongs to the Special Issue Surface Science: Polymer Thin Films, Coatings and Adhesives)
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27 pages, 2356 KiB  
Article
Exploring the Anticancer Activity of Artocarpus heterophyllus Leaves: Selective Effects on Triple-Negative Breast Cancer and HPV16-Positive Tumorigenic Cells
by Ariana Cabrera-Licona, Gustavo A. Hernández-Fuentes, Oscar F. Beas-Guzmán, Alejandra E. Hernández-Rangel, Janet Diaz-Martinez, Osval A. Montesinos-López, José Guzmán-Esquivel, Víctor H. Cervantes-Kardasch, Mario Ramírez-Flores, Alejandrina Rodriguez-Hernandez, Erika R. González-Espinosa, Ana B. Castellanos-Gutiérrez, Francisco Orozco-Ramos, Valery Melnikov and Iván Delgado-Enciso
Life 2025, 15(7), 1090; https://doi.org/10.3390/life15071090 - 11 Jul 2025
Viewed by 448
Abstract
Artocarpus heterophyllus (jackfruit) is widely distributed in subtropical and tropical regions, and some phytochemicals isolated from this species have demonstrated anti-proliferative effects. However, its impact on triple-negative breast cancer (TNBC) and HPV-related cervical cancer models remains unclear. This study evaluated the phytochemical profile [...] Read more.
Artocarpus heterophyllus (jackfruit) is widely distributed in subtropical and tropical regions, and some phytochemicals isolated from this species have demonstrated anti-proliferative effects. However, its impact on triple-negative breast cancer (TNBC) and HPV-related cervical cancer models remains unclear. This study evaluated the phytochemical profile and anticancer activity of an ethanolic extract from A. heterophyllus leaves (AHEE) in the TNBC cell line MDA-MB-231 and in the HPV-16+ murine cancer cell line TC-1. Phytochemical screening and spectroscopic analyses (UV-Vis, IR, 1H, and 13C NMR) revealed the presence of tannins, alkaloids, steroids, coumarins, and flavone-type flavonoids, with a total phenolic content of 3.34 µg GAE/mg and flavonoid content of 0.44 mg QE/g extract. In 2D cultures, AHEE reduced cell viability by 49% in TC-1 and 24% in MDA-MB-231 at 300 µg/mL, inhibited colony formation and migration in TC-1, and impaired survival but not migration in MDA-MB-231. In 3D cultures, 250 µg/mL inhibited proliferation, migration, and anchorage-independent growth in both cell lines. Furthermore, the combination of AHEE with one-fifth of the IC50 of doxorubicin or cisplatin produces an effect comparable to that observed with the full IC50 of these drugs. These findings suggest that AHEE possesses anticancer activity with cell-type-specific effects and highlight its potential as an adjuvant therapy. Further studies are warranted to elucidate its mechanisms of action. Full article
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40 pages, 12228 KiB  
Article
Design and Synthesis of Arylboronic Acid Chemosensors for the Fluorescent-Thin Layer Chromatography (f-TLC) Detection of Mycolactone
by Gideon Atinga Akolgo, Benjamin M. Partridge, Timothy D. Craggs, Kingsley Bampoe Asiedu and Richard Kwamla Amewu
Chemosensors 2025, 13(7), 244; https://doi.org/10.3390/chemosensors13070244 - 9 Jul 2025
Viewed by 800
Abstract
Fluorescent chemosensors are increasingly becoming relevant in recognition chemistry due to their sensitivity, selectivity, fast response time, real-time detection capability, and low cost. Boronic acids have been reported for the recognition of mycolactone, the cytotoxin responsible for tissue damage in Buruli ulcer disease. [...] Read more.
Fluorescent chemosensors are increasingly becoming relevant in recognition chemistry due to their sensitivity, selectivity, fast response time, real-time detection capability, and low cost. Boronic acids have been reported for the recognition of mycolactone, the cytotoxin responsible for tissue damage in Buruli ulcer disease. A library of fluorescent arylboronic acid chemosensors with various signaling moieties with certain beneficial photophysical characteristics (i.e., aminoacridine, aminoquinoline, azo, BODIPY, coumarin, fluorescein, and rhodamine variants) and a recognition moiety (i.e., boronic acid unit) were rationally designed and synthesised using combinatorial approaches, purified, and fully characterised using a set of complementary spectrometric and spectroscopic techniques such as NMR, LC-MS, FT-IR, and X-ray crystallography. In addition, a complete set of basic photophysical quantities such as absorption maxima (λabsmax), emission maxima (λemmax), Stokes shift (∆λ), molar extinction coefficient (ε), fluorescence quantum yield (ΦF), and brightness were determined using UV-vis absorption and fluorescence emission spectroscopy techniques. The synthesised arylboronic acid chemosensors were investigated as chemosensors for mycolactone detection using the fluorescent-thin layer chromatography (f-TLC) method. Compound 7 (with a coumarin core) emerged the best (λabsmax = 456 nm, λemmax = 590 nm, ∆λ = 134 nm, ε = 52816 M−1cm−1, ΦF = 0.78, and brightness = 41,197 M−1cm−1). Full article
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25 pages, 1560 KiB  
Article
Phytochemical Screening and Biological Activities of Lippia multiflora Moldenke
by Dorcas Tlhapi, Ntsoaki Malebo, Idah Tichaidza Manduna, Monizi Mawunu and Ramakwala Christinah Chokwe
Molecules 2025, 30(13), 2882; https://doi.org/10.3390/molecules30132882 - 7 Jul 2025
Viewed by 411
Abstract
Lippia multiflora Moldenke is widely used in Angola, on the African continent, and beyond for the treatment of many health conditions such as hypertension, enteritis, colds, gastrointestinal disturbances, stomachaches, jaundice, coughs, fevers, nausea, bronchial inflammation, conjunctivitis, malaria, and venereal diseases. However, there is [...] Read more.
Lippia multiflora Moldenke is widely used in Angola, on the African continent, and beyond for the treatment of many health conditions such as hypertension, enteritis, colds, gastrointestinal disturbances, stomachaches, jaundice, coughs, fevers, nausea, bronchial inflammation, conjunctivitis, malaria, and venereal diseases. However, there is limited literature about the active compounds linked with the reported biological activities. This study aims to assess the chemical profiles, antioxidant properties, and the cytotoxicity effects of the roots, stem bark, and leaves of L. multiflora. Chemical characterization of the crude extracts was assessed through quantification of total phenolic and flavonoid contents followed by Q exactive plus orbitrap™ ultra-high-performance liquid chromatography-mass spectrometer (UHPLC-MS) screening. The correlation between the extracts and the correlation between the compounds were studied using the multivariate analysis. Principal component analysis (PCA) loading scores and principal component analysis (PCA) biplots and correlation plots were used to connect specific compounds with observed biological activities. The antioxidant activities of the crude extracts were carried out in vitro using DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging and reducing power assays, while the in vitro toxicology of the crude extracts was evaluated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. A total of twenty constituents were characterized and identified using the UHPLC–Q/Orbitrap/MS. The methanol leaf extract showed the highest antioxidant activity in the DPPH free radical scavenging activity (IC50 = 0.559 ± 0.269 μg/mL); however, the stem bark extract had the highest reducing power (IC0.5 = 0.029 ± 0.026 μg/mL). High phenolic and flavonoid content was found in the dichloromethane leaf extract (32.100 ± 1.780 mg GAE/g) and stem bark extract (624.153 ± 29.442 mg QE/g), respectively. The results show the stem bark, methanol leaf, and dichloromethane leaf extracts were well-tolerated by the Vero cell line at concentrations up to 50 µg/mL. However, at 100 µg/mL onward, some toxicity was observed in the root, methanol leaf, and dichloromethane leaf extracts. The UHPLC–Q/Orbitrap/MS profiles showed the presence of terpenoids (n = 5), flavonoids (n = 5), phenols (n = 4), alkaloids (n = 3), coumarins (n = 1), fatty acids (n = 1), and organic acids (n = 1). According to several studies, these secondary metabolites have been reported and proven to be the most abundant for antioxidant potential. The identified flavonoids (catechin, quercitrin, and (−)-epigallocatechin) and phenolic compound (6-gingerol) can significantly contribute to the antioxidant properties of different plant parts of L. multiflora. The research findings obtained in this study provide a complete phytochemical profile of various parts of L. multiflora that are responsible for the antioxidant activity using UHPLC–Q/Orbitrap/MS analysis. Furthermore, the results obtained in this study contribute to the scientific information or data on the therapeutic properties of Lippia multiflora and provide a basis for further assessment of its potential as a natural remedy. Full article
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16 pages, 2795 KiB  
Article
Therapeutic Potential of 7,8-Dimethoxycoumarin in Tumor Necrosis Factor-Alpha-Induced Trigeminal Neuralgia in a Rat Model
by Nallupillai Paramakrishnan, Kanthiraj Raadhika, Sumitha Elayaperumal, Yuvaraj Sivamani, Yamunna Paramaswaran, Lim Joe Siang, Thiagharajan Venkata Rathina Kumar, Khian Giap Lim, Muthusamy Ramesh and Arunachalam Muthuraman
Curr. Issues Mol. Biol. 2025, 47(7), 518; https://doi.org/10.3390/cimb47070518 - 4 Jul 2025
Viewed by 353
Abstract
Trigeminal neuralgia is a chronic pain disorder due to neuronal damage. The present study was designed to investigate the effect of 7,8-dimethoxy coumarin (DMC) in a rat model of trigeminal neuralgia. The neuropathic pain was induced by the single endoneural injection of tumor [...] Read more.
Trigeminal neuralgia is a chronic pain disorder due to neuronal damage. The present study was designed to investigate the effect of 7,8-dimethoxy coumarin (DMC) in a rat model of trigeminal neuralgia. The neuropathic pain was induced by the single endoneural injection of tumor necrosis factor-alpha (TNF-α; 0.1 μL: stock 10 pg/mL) in the rat trigeminal nerve. The DMC (100 and 200 mg/kg) and carbamazepine (100 mg/kg) were administered orally for 10 consecutive days from the 5th day of TNF-α injection. The battery of behavioral tests, i.e., acetone drop and Von Frey filament test, was performed to assess the degree of thermal and mechanical allodynia on 0, 1st, 7th, and 14th days. In addition, the biochemical tests, i.e., total protein, thiobarbituric acid reactive substances (TBARS), reduced glutathione (GSH), and TNF-α, were also performed in trigeminal nerve tissue. Furthermore, TNF-α-induced neuronal histopathological changes were also evaluated by the eosin and hematoxylin staining method. The administration of DMC was shown to demonstrate the significant (p < 0.05) reversal of TNF-α-induced percentage reduction of thermal and mechanical sensitivity, along with a rise in TBARS and TNF-α and a decrease in GSH levels. Further, DMC also attenuates the histopathological changes. It may be concluded that DMC may be a potential therapeutic agent for the management of trigeminal neuralgia disorders. Full article
(This article belongs to the Section Molecular Pharmacology)
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Article
Unveiling the Pharmacognostic Potential of Peucedanum ostruthium (L.) W.D.J. Koch: A Comparative Study of Rhizome and Leaf Essential Oils
by Cristina Danna, Andrea Mainetti, Souda Belaid, Erminia La Camera, Domenico Trombetta, Laura Cornara and Antonella Smeriglio
Plants 2025, 14(13), 2047; https://doi.org/10.3390/plants14132047 - 3 Jul 2025
Viewed by 361
Abstract
Peucedanum ostruthium (L.) W.D.J. Koch (Apiaceae) is a perennial herb native to alpine regions that is renowned in traditional medicine. This study provided a pharmacognostic evaluation, comparing the EOs obtained from its rhizomes and leaves (REO and LEO, respectively). A micromorphological analysis, which [...] Read more.
Peucedanum ostruthium (L.) W.D.J. Koch (Apiaceae) is a perennial herb native to alpine regions that is renowned in traditional medicine. This study provided a pharmacognostic evaluation, comparing the EOs obtained from its rhizomes and leaves (REO and LEO, respectively). A micromorphological analysis, which was carried out using fluorescence and scanning electron microscopy, revealed terpenoid-rich secretory ducts in both organs. The EOs were extracted by hydrodistillation and characterized by gas chromatography, coupled with flame ionization detection and mass spectrometry (GC-FID and GC-MS), revealing distinct chemical profiles. REO was dominated by monoterpenes (80.08%), especially D-limonene (29.13%), sabinene (19.77%), and α-phellandrene (12.02%), while LEO was sesquiterpene-rich (81.15%), with β-caryophyllene (21.78%), β-selinene (14.09%), and germacrene D (10.43%) as the major compounds. The in vitro assays demonstrated that both EOs exhibit significant antioxidant and anti-inflammatory activities, with LEO consistently outperforming REO across all tests. However, neither EO showed antimicrobial effects against common bacterial or fungal strains. This may have been due to the absence of polar antimicrobial constituents, such as coumarins, which are poorly recovered by hydrodistillation. To fully exploit the therapeutic potential of P. ostruthium, especially its antimicrobial properties, future studies should aim to develop integrated formulations combining volatile and non-volatile fractions, preserving the complete plant complex and broadening bioactivity. Full article
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