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Bioactive Natural Compounds: Therapeutic Insights and Applications

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A special issue of Life (ISSN 2075-1729). This special issue belongs to the section "Pharmaceutical Science".

Deadline for manuscript submissions: 30 May 2025 | Viewed by 11343

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Special Issue Editor

Dr. Vaidotas Žvikas

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Institute of Pharmaceutical Technologies, Lithuanian University of Health Sciences, 44307 Kaunas, Lithuania
Interests: natural products; bioactive compounds; phytochemistry; metabolomics; mass spectrometry

Special Issue Information

Dear Colleagues,

Life will soon publish a Special Issue on “Bioactive Natural Compounds: Therapeutic Insights and Applications”. Plant extracts and other natural products are complex mixtures of natural compounds and they and their metabolites are suitable for a various applications in the fields of pharmaceutics and nutrition. Natural products enriched with bioactive compounds provide the scientific and industrial communities with opportunities to develop new drugs, cosmetics and functional foods.

The natural compounds analysed in this Special Issue should include plant phytochemicals and animal products with proven effects. The bioactivity of phytochemicals of plant extracts is essential for their functionality and this bioactivity should be determined through novel and appropriate techniques and assays. Extraction is one of the most important steps in determining the functionality of chemicals of natural origin and different extraction methods and techniques could change composition and bioactive effects of plant extracts, which may also be covered by this Special Issue. Since bioactive compounds extracted from plant material are complex mixtures, their separation and quantitative and qualitative analysis are crucial steps in the structural composition of extracts. Appropriate and novel analytical methods or their validation procedures should be used for publications in this Special Issue., and extensive literature reviews of novel topics will be published in tandem.

Therefore, considering the great and growing interest in natural compounds, this Special Issue will cover the diverse perspectives of their qualitative and quantitative analysis. In striving to achieve this, we will compare extraction methods with the phytochemical profiles of extracts and their bioactivity to generate structure-focused views of natural compounds that can be employed as bioactive elements in various fields.

Dr. Vaidotas Žvikas
Guest Editor

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Keywords

medicinal plants
bioactive compounds
plant extracts
phytochemicals
analytical method validation

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Published Papers (8 papers)

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Research

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19 pages, 3390 KiB

Open AccessArticle

Comparison of Major Compounds in Essential Oils Steam Distilled from Fresh Plant Material of South African Hop Varieties

by Olga de Smidt, Wanda du Plessis, Puleng Rose Zacharia and Idah Tichaidza Manduna

Life 2025, 15(2), 282; https://doi.org/10.3390/life15020282 - 12 Feb 2025

Viewed by 882

Abstract

Apart from the importance of bittering acids in the brewing sector, hops also produce terpene-rich essential oils, recognised for their therapeutic benefits. Agri-processing practices of this crop in South Africa produce tonnes of discarded (waste) plant material that could still contain sufficient bioactive compounds to justify upcycling. This research aimed to determine the chemical composition of steam distilled essential oils from fresh hop plant material destined for disposal. Essential oils from eight hop varieties unique to South Africa were produced on industrial scale using steam distillation. Chemical profiling was performed using GC-FID and MS. A total of 208 compounds were identified and oil consisted largely of terpenes (89.04 ± 1.89%) as well as aliphatic esters and -ketones (6.1 ± 1.15%). Myrcene (27.8–48.15%) was the most abundant monoterpene and α-humulene (19.52–24.98%), β-caryophyllene (8.47–13.73%) and β-farnesene (2.08–7.57%) constituted the majority of the sesquiterpenes fraction. Experimental variety XJA2/436 had the highest myrcene fraction (48.15%) and its chemical composition was markedly different from the other varieties. The major compounds in African Queen hop oil were methyl (4Z) decanoate (0.74%), 2-tridecanone (0.77%) and β-farnesene (7.57%). Southern Dawn hop oil contained the highest fractions of 2-undecanone (1.21%) and α-humulene (24.89%) and Southern Passion hop oil contained the highest β-caryophyllene fraction (13.73%). These findings established that fresh hop vegetative biomass shows promise to be transformed into a valuable resource. Full article

(This article belongs to the Special Issue Bioactive Natural Compounds: Therapeutic Insights and Applications)

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11 pages, 7476 KiB

Open AccessArticle

Two Small Peptides from Buthus martensii Hydrolysates Exhibit Antitumor Activity Through Inhibition of TNF-α-Mediated Signal Transduction Pathways

by Mengshuang Zhu, Shanshan Zhang, Jiyang Tang, Hairong Hou, Lizhen Wang, Houwen Lin, Xuanming Zhang and Meng Jin

Life 2025, 15(1), 105; https://doi.org/10.3390/life15010105 - 15 Jan 2025

Viewed by 975

Abstract

The scorpion Buthus martensii Karsch is edible and has been an essential resource in traditional Chinese medicine for treating numerous diseases. In this study, two small peptides from B. martensii hydrolysates were examined to elucidate their potential against gastric cancer. The small peptides (AK and GK) were identified using the LC-QTOF-MS-based approach. In silico prediction of therapeutic targets, MGC-803 cells and transgenic zebrafish models, and immunoblotting experiments were used to reveal the molecular mechanism of action of the peptides. The peptides AK and GK competitively bound to the receptor to modulate the TNF/TNFR-signaling cascade and alter the tumor microenvironment. EGFR, TP53, MYC, PTEN, and STAT3 were also identified as major functional targets of the peptides. Mechanistically, AK and GK inactivated the TNF-α/EGFR/STAT3-signaling pathway, decreased c-myc protein expression levels, and upregulated p53 and PTEN expression, thereby preventing TNF-α-induced tumor growth. Our findings indicated that AK and GK played a pivotal role in offsetting the inflammatory stimuli that caused gastric cancer cell invasion and highlighted the use of B. martensii resources as functional products with health benefits. Full article

(This article belongs to the Special Issue Bioactive Natural Compounds: Therapeutic Insights and Applications)

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19 pages, 6403 KiB

Open AccessArticle

Is Punica granatum Efficient Against Sepsis? A Comparative Study of Amifostine Versus Pomegranate

by Kazim Sahin, Sena Sahin Aktura, Ilkay Bahceci, Tolga Mercantepe, Levent Tumkaya, Atilla Topcu, Filiz Mercantepe, Omer Faruk Duran, Huseyin Avni Uydu and Zihni Acar Yazici

Life 2025, 15(1), 78; https://doi.org/10.3390/life15010078 - 10 Jan 2025

Cited by 1 | Viewed by 837

Abstract

Sepsis is a clinical condition causing tissue damage as a result of infection and an exaggerated immune response. Sepsis causes 11 million deaths annually, a third of which are associated with acute lung injury (ALI). Rapid and effective treatment is crucial to improve survival rates. Punica granatum (pomegranate) is rich in polyphenols and demonstrates strong antioxidant activity, while amifostine acts as a free radical scavenger. This study aimed to investigate the antioxidant and anti-inflammatory effects of P. granatum peel extract (PGPE) and amifostine in sepsis-related ALI. Experimental groups included Control, CLP (cecal ligation and puncture-induced sepsis), Amf (200 mg/kg amifostine, intraperitoneally), and PGPE250, and PGPE500 (250 and 500 mg/kg PGPE via oral gavage, respectively). Thiobarbituric acid reactive substances (TBARS), total thiol (TT), tumor necrosis factor-alpha (TNF-α) levels, and metalloproteinases 2 and 9 (MMP-2 and MMP-9) were assessed in the lung tissue. Biochemical analysis demonstrated that TBARS and TNF-α levels significantly decreased in both the PGPE and amifostine treatment groups compared to the CLP group, while TT levels showed notable improvement. Histopathological evaluation revealed reduced MMP-2 and MMP-9 immunopositivity in the PGPE250 and PGPE500 groups. These findings highlight the lung-protective properties of PGPE, underscoring its potential as a therapeutic agent for sepsis-induced acute lung injury. Full article

(This article belongs to the Special Issue Bioactive Natural Compounds: Therapeutic Insights and Applications)

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20 pages, 3302 KiB

Open AccessArticle

Genotypes of Sechium spp. as a Source of Natural Products with Biological Activity

by Jorge Cadena-Iñiguez, Ma. de Lourdes Arévalo-Galarza, Edelmiro Santiago-Osorio, Itzen Aguiñiga-Sánchez, Jorge David Cadena-Zamudio, Marcos Soto-Hernández, Yeimy C. Ramírez-Rodas, Lucero del Mar Ruiz-Posadas, Sandra Salazar-Aguilar and Víctor Manuel Cisneros-Solano

Life 2025, 15(1), 15; https://doi.org/10.3390/life15010015 - 27 Dec 2024

Viewed by 806

Abstract

The genus Sechium P. Br. (Cucurbitaceae) includes ten species, two of which are edible. The inedible genotypes are in a fragile ecological niche, since they are not used by rural inhabitants. A rescue and genetic crossing program was designed to identify uses that favor their conservation due to their content of bioactive secondary metabolites (Sm) for health. Fruits of S. compositum (wild type), hybrid H-D Victor (inedible), and S. edule var. nigrum spinosum (edible) were evaluated by extraction methods such as juice and oven drying to determine the yields of Sm, with in vivo evaluations of liver damage. The dried biomass (40 °C) extracted with ethanolic and methanolic procedures showed lower Sm content than the juice (fresh biomass). More than 90% of phenolic acids and cucurbitacins in the extracts were degraded, possibly due to the drying time (oven). Biological activity showed that nigrum spinosum and HD-Victor have fewer toxic metabolites than S. compositum. The hybrid H-D Victor is of reduced cytotoxicity, showing the advantages of hybridization with wild types. Phytochemical and biological activity characterization may contribute to the conservation of genotypes and become a source of bioactive natural products. Full article

(This article belongs to the Special Issue Bioactive Natural Compounds: Therapeutic Insights and Applications)

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25 pages, 2124 KiB

Open AccessArticle

Seaweed Nutritional Value and Bioactive Properties: Insights from Ascophyllum nodosum, Palmaria palmata, and Chondrus crispus

by Natália Čmiková, Przemysław Łukasz Kowalczewski, Dominik Kmiecik, Aneta Tomczak, Agnieszka Drożdżyńska, Mariusz Ślachciński, Łukasz Szala, Sanja Matić, Tijana Marković, Suzana Popović, Dejan Baskic and Miroslava Kačániová

Life 2024, 14(11), 1522; https://doi.org/10.3390/life14111522 - 20 Nov 2024

Cited by 1 | Viewed by 2957

Abstract

This study investigates the nutritional composition and bioactive properties of Palmaria palmata (dulse), Ascophyllum nodosum (knotted wrack), and Chondrus crispus (Irish moss). Understanding the nutritional values of these seaweeds is very important due to their potential health benefits, especially their antioxidant properties and cytotoxic activities, which point to their ability to inhibit cancer cell proliferation. Comprehensive analyses were conducted to assess protein content, amino acid composition, mineral profile, fatty acids, polyphenols, total carotenoids, antioxidant activity, and cytotoxicity against cervical (HeLa), and colon (HCT-116) cell lines. P. palmata exhibited the highest protein content, while C. crispus was richest in calcium, iron, manganese, and zinc. Amino acid analysis revealed C. crispus as being particularly high in essential and non-essential amino acids, including alanine, glutamic acid, and glycine. A. nodosum and C. crispus were rich in polyunsaturated fatty acids (PUFAs), notably eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA). A. nodosum showed the highest total carotenoid content. Polyphenol analysis highlighted the presence of compounds such as p-coumaric acid, gallic acid, and p-hydroxybenzoic acid across the species. Both the ethanolic and hexane A. nodosum extracts demonstrated the strongest antioxidant potential in DPPH^• and ABTS⁺ assays. The cytotoxicity evaluation revealed high anticancer activity of A. nodosum and C. crispus hexane extract against HeLa and HCT-116, though it employed cell cycle arrest and apoptosis. A. nodosum hexane extract exhibited moderate selective anticancer activity against HCT-116. These findings underscore the nutritional diversity and potential health benefits of these macroalgae (seaweed) species, suggesting their suitability as functional foods or supplements, offering diverse nutritional and therapeutic benefits. Full article

(This article belongs to the Special Issue Bioactive Natural Compounds: Therapeutic Insights and Applications)

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17 pages, 5472 KiB

Open AccessArticle

The Nephroprotective Effect of Punica granatum Peel Extract on LPS-Induced Acute Kidney Injury

by Sena Sahin Aktura, Kazim Sahin, Levent Tumkaya, Tolga Mercantepe, Atilla Topcu, Esra Pinarbas and Zihni Acar Yazici

Life 2024, 14(10), 1316; https://doi.org/10.3390/life14101316 - 16 Oct 2024

Cited by 2 | Viewed by 1818

Abstract

Sepsis is an exaggerated immune response resulting from systemic inflammation, which can damage tissues and organs. Acute kidney injury has been detected in at least one-third of patients with sepsis. Sepsis-associated acute kidney injury increases the risk of a secondary infection. Rapid diagnosis and appropriate initiation of antibiotics can significantly reduce mortality and morbidity. However, microorganisms are known to develop resistance to antibiotics. Estimations indicate that the annual casualties caused by microbial resistance will surpass cancer fatalities by 2050. The prevalence of bacterial infections and their growing antibiotic resistance has brought immediate attention to the search for novel treatments. Plant-derived supplements contain numerous bioactive components with therapeutic potential against a variety of conditions, including infections. Punica granatum peel is rich in phenolic compounds. The purpose of this study was to determine the anti-inflammatory and anti-bacterial properties of P. granatum peel extract (PGPE) on lipopolysaccharide (LPS)-induced acute kidney injury. Experimental groups were Control, LPS (10 mg/kg LPS, intraperitoneally), PGPE100, and PGPE300 (100 and 300 mg/mL PGPE via oral gavage, respectively, for 7 days). According to biochemical results, serum blood urea nitrogen (BUN), creatinine (Cr) and C-reactive protein (CRP), kidney tissue thiobarbituric acid reactive substances (TBARS), and reduced glutathione (GSH) levels significantly decreased in the PGPE groups compared to the LPS group. Histopathological and immunohistochemical findings revealed that toll-like receptor 4 (TLR4) level and nuclear factor kappa B (NF-κB) expression increased in the LPS group compared to the Control group. In addition, the anti-Gram-negative activity showed a dose-dependent effect on Acinetobacter baumannii, Escherichia coli, and Pseudomonas aeruginosa with the agar well diffusion method and the minimal inhibitory concentration (MIC). The MIC value was remarkable, especially on A. baumannii. We conclude that PGPE has the potential to generate desirable anti-bacterial and anti-inflammatory effects on LPS-induced acute kidney injury in rats. Full article

(This article belongs to the Special Issue Bioactive Natural Compounds: Therapeutic Insights and Applications)

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24 pages, 2986 KiB

Open AccessArticle

Effect of the Phenological Stage on the Phenolic Composition, and Antioxidant and Antimicrobial Properties of Cirsium vulgare (Savi) Ten. Extracts

by Urte Griskeviciene, Justina Dambrauskiene, Mindaugas Marksa, Zaneta Mazeliene, Rimanta Vainoriene and Liudas Ivanauskas

Life 2024, 14(9), 1191; https://doi.org/10.3390/life14091191 - 20 Sep 2024

Cited by 2 | Viewed by 1265

Abstract

Cirsium vulgare (Savi) Ten. is a plant from the Asteraceae family that is commonly used in traditional medicine. The purpose of this work was to investigate the antioxidant and antimicrobial characteristics of phenolic compounds found in ethanol and dry extracts of C. vulgare leaves, inflorescence, and roots during various phenological stages. Apigenin-7-O-glucoside and chlorogenic acid were identified in practically all C. vulgare extracts. Extracts from leaves collected at the end of the phenological dormancy period and in the first growing year had the highest antioxidant (cupric ion-reducing antioxidant capacity of 12,938 Trolox equivalents/g dry weight) and antimicrobial activity (against Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, Proteus vulgaris, and Candida albicans) with MIC values of ethanol extract from 16.7 mg/mL to 8.35 mg/mL. These extracts included a high concentration of chlorogenic acid and apigenin-7-O-glucoside. Also, dry extracts from C. vulgare roots and inflorescences showed a higher antimicrobial effect compared to ethanolic extracts with MIC values from 5.57 mg/mL to 3 mg/mL. The study emphasizes the critical role of phenological stages and raw material composition in the accumulation of phenolic compounds and their biological activity in C. vulgare. The findings suggest that extracts from C. vulgare leaves, especially those collected at the end of the phonological dormancy period, are promising candidates for further research into bioactive compounds with potential medicinal applications. The strong antioxidant and antibacterial properties of these extracts highlight their potential for development into natural pharmaceutical products. Full article

(This article belongs to the Special Issue Bioactive Natural Compounds: Therapeutic Insights and Applications)

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38 pages, 2898 KiB

Open AccessReview

Moringa oleifera Lam.: A Nutritional Powerhouse with Multifaceted Pharmacological and Functional Applications

by Natalina Panova, Anelia Gerasimova, Galia Gentscheva, Stoyanka Nikolova, Lubomir Makedonski, Margarita Velikova, Abdessamad Beraich, Abdelmonaem Talhaoui, Nadezhda Petkova, Daniela Batovska and Krastena Nikolova

Life 2025, 15(6), 881; https://doi.org/10.3390/life15060881 (registering DOI) - 29 May 2025

Abstract

Moringa oleifera, often referred to as the “miracle tree”, has gained widespread recognition for its exceptional nutritional profile and broad pharmacological potential. This review provides a comprehensive synthesis of the plant’s botanical characteristics, taxonomy, cultivation practices, and biochemical composition. Special emphasis is placed on its rich content of bioactive secondary metabolites-such as flavonoids, alkaloids, phenolic acids, saponins, isothiocyanates, and glucosinolates-which underlie its diverse therapeutic effects. The paper compiles and analyzes evidence from over 200 peer-reviewed studies, documenting antioxidant, anti-inflammatory, antimicrobial, antidiabetic, anticancer, hepatoprotective, neuroprotective, and anti-obesity effects, among others. For instance, leaf extracts have demonstrated potent antioxidant and antidiabetic effects in both animal models and clinical trials, while seed-derived isothiocyanates have shown significant antibacterial and anticancer activity. In addition, clinical and in vivo data support M. oleifera’s role in fertility regulation, cardiovascular protection, and neurodegenerative disease mitigation. Beyond its medicinal applications, the review highlights its growing use in functional foods, dietary supplements, and cosmeceutical products, reflecting its commercial and industrial relevance. By consolidating findings across disciplines, this review underscores the multifaceted value of M. oleifera as a nutraceutical and therapeutic resource. Full article

(This article belongs to the Special Issue Bioactive Natural Compounds: Therapeutic Insights and Applications)

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