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Bioactive Natural Products: Composition, Molecular Mechanisms and Beneficial Effects

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (30 September 2023) | Viewed by 7091

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Dr. Maria João Sousa

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Centro de Investigação de Montanha (CIMO), Instituto Politécnico de Bragança, Campus de Santa Apolónia, 5300-253 Bragança, Portugal
Interests: biology; chemistry of natural products; cosmetics; plant physiology and plant tissue culture
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Special Issue Information

Dear Colleagues,

Currently, the search for beneficial products is a constant, to the extent that in areas such as food science, pharmacology, medicine, or even agronomic or industrial science, the use of natural, less toxic and biodegradable products is increasingly important in terms of sustainability and socio-cultural requirements.

Different compounds from a variety of sources, such as microorganisms (virus, bacteria and fungi), animals (terrestrial and marines) and plants, can represent new and interesting, active, non-toxic and sustainable products for different applications in medicine, pharmacology, cosmetics, agriculture, food science and industry. These natural products must be studied, evaluated and tested for their ability in new applications in living organisms.

The classification of the chemical composition of these compounds is an essential tool for the understanding of their mechanisms of action, their metabolism and their interrelations with other products. The molecular mechanisms for their production and bioactivity will be clarified, investigated, and presented in this Special Issue.

The methods of extraction, manipulation and even modification (chemical and genetics) of these products, which are essential to the application of new knowledge in all of these areas of study, should also be suggested and discussed in this Special Issue.

Chemical compounds are the basis of this field, but the benefits of bioactive compounds and the methodologies used to study biochemicals and the biological pathways involved in their production, modification, or excretion are also important and interesting.

We invite authors with an expertise in this field to contribute to this Special Issue with either original research or review articles focusing on, but not limited to: 1) the chemical transformation of natural products towards the production of more stabilized structures; 2) the stabilization of compounds and formulations using original approaches; 3) mechanisms of action in improving health; 4) bioactivity (bioavailability, metabolites, enzyme inhibition, anti-proliferative and anti-bacterial activities); 5) new sustainable methods to extract bioactive compounds; 6) new sources of bioactive compounds; 7) the biological production of bioactive products; and 8) the development of new mixtures or formulations based on natural products.

Dr. Maria João Sousa
Guest Editor

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Keywords

natural products
bioactivity
chemical composition
metabolism and molecular structure
biological effects

Published Papers (4 papers)

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Research

14 pages, 5383 KiB

Open AccessArticle

Exploring the Effect of Deep-Sea Water on the Therapeutic Potential of the Anti-Inflammatory Response in an Indomethacin-Induced Gastric Ulcer Rat Model

by Soo-yeon Park, Jin A Im and Ji Yeon Kim

Int. J. Mol. Sci. 2023, 24(24), 17430; https://doi.org/10.3390/ijms242417430 - 13 Dec 2023

Viewed by 731

Abstract

Gastric ulcers are often exacerbated by factors such as nonsteroidal anti-inflammatory drugs (NSAIDs) and inflammation, and they have a substantial impact on a significant portion of the population. Notably, indomethacin is recognized as a prominent contributor to ulcers. This study investigated this potential method, with normalization to the anti-inflammatory and antiulcer properties of deep-sea water (DSW)-derived mineral water, using an indomethacin-induced gastric ulcer model in rats. The study involved four groups (n = 6 rats/group): normal control group (CON), indomethacin-only group (IND), indomethacin with trace mineral water group (TM), and indomethacin with high magnesium low sodium water group (HMLS). For three weeks, the CON and IND groups consumed tap water, while the TM and HMLS groups had access to mineral water. Gastric ulcers were induced on the final day using indomethacin, for all groups except the CON group. The results demonstrated that HMLS intake significantly improved gastric mucosal damage, preserved mucin stability, and increased gastric thickness, indicating its potential to prevent and alleviate indomethacin-induced gastric ulcers. Furthermore, HMLS consumption led to the upregulation of key genes associated with inflammation and a reduction in inflammatory cytokines. These findings suggest that DSW-derived mineral water, and particularly its high Mg²⁺ content, may offer promising health benefits including anti-inflammatory and anti-ulcer properties. Full article

(This article belongs to the Special Issue Bioactive Natural Products: Composition, Molecular Mechanisms and Beneficial Effects)

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17 pages, 2263 KiB

Open AccessArticle

From Fruit Waste to Medical Insight: The Comprehensive Role of Watermelon Rind Extract on Renal Adenocarcinoma Cellular and Transcriptomic Dynamics

by Chinreddy Subramanaym Reddy, Purushothaman Natarajan, Padma Nimmakayala, Gerald R. Hankins and Umesh K. Reddy

Int. J. Mol. Sci. 2023, 24(21), 15615; https://doi.org/10.3390/ijms242115615 - 26 Oct 2023

Viewed by 1943

Abstract

Cancer researchers are fascinated by the chemistry of diverse natural products that show exciting potential as anticancer agents. In this study, we aimed to investigate the anticancer properties of watermelon rind extract (WRE) by examining its effects on cell proliferation, apoptosis, senescence, and global gene expression in human renal cell adenocarcinoma cells (HRAC-769-P) in vitro. Our metabolome data analysis of WRE exhibited untargeted phyto-constituents and targeted citrulline (22.29 µg/mg). HRAC-769-P cells were cultured in RPMI-1640 media and treated with 22.4, 44.8, 67.2, 88.6, 112, 134.4, and 156.8 mg·mL⁻¹ for 24, 48, and 72 h. At 24 h after treatment, (88.6 mg·mL⁻¹ of WRE) cell proliferation significantly reduced, more than 34% compared with the control. Cell viability decreased 48 and 72 h after treatment to 45% and 37%, respectively. We also examined poly caspase, SA-beta-galactosidase (SA-beta-gal), and wound healing activities using WRE. All treatments induced an early poly caspase response and a significant reduction in cell migration. Further, we analyzed the transcript profile of the cells grown at 44.8 mg·mL⁻¹ of WRE after 6 h using RNA sequencing (RNAseq) analysis. We identified 186 differentially expressed genes (DEGs), including 149 upregulated genes and 37 downregulated genes, in cells treated with WRE compared with the control. The differentially expressed genes were associated with NF-Kappa B signaling and TNF pathways. Crucial apoptosis-related genes such as BMF, NPTX1, NFKBIA, NFKBIE, and NFKBID might induce intrinsic and extrinsic apoptosis. Another possible mechanism is a high quantity of citrulline may lead to induction of apoptosis by the production of increased nitric oxide. Hence, our study suggests the potential anticancer properties of WRE and provides insights into its effects on cellular processes and gene expression in HRAC-769-P cells. Full article

(This article belongs to the Special Issue Bioactive Natural Products: Composition, Molecular Mechanisms and Beneficial Effects)

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22 pages, 3219 KiB

Open AccessArticle

Antifungal Activities of Fluorinated Pyrazole Aldehydes on Phytopathogenic Fungi, and Their Effect on Entomopathogenic Nematodes, and Soil-Beneficial Bacteria

by Vesna Rastija, Karolina Vrandečić, Jasenka Ćosić, Gabriella Kanižai Šarić, Ivana Majić, Dejan Agić, Domagoj Šubarić, Maja Karnaš, Drago Bešlo, Harshad Brahmbhatt and Mario Komar

Int. J. Mol. Sci. 2023, 24(11), 9335; https://doi.org/10.3390/ijms24119335 - 26 May 2023

Cited by 3 | Viewed by 1441

Abstract

Fluoro-substituted pyrazoles have a wide range of biological activities, such as antibacterial, antiviral, and antifungal activities. The aim of this study was to evaluate the antifungal activities of fluorinated 4,5-dihydro-1H-pyrazole derivatives on four phytopathogenic fungi: Sclerotinia sclerotiorum, Macrophomina phaseolina, Fusarium oxysporum f. sp. lycopersici, and F. culmorum. Moreover, they were tested on two soil beneficial bacteria—Bacillus mycoides and Bradyrhizobium japonicum—as well as two entomopathogenic nematodes (EPNs)—Heterorhabditis bacteriophora and Steinernema feltiae. The molecular docking was performed on the three enzymes responsible for fungal growth, the three plant cell wall-degrading enzymes, and acetylcholinesterase (AChE). The most active compounds against fungi S. sclerotiorum were 2-chlorophenyl derivative (H9) (43.07% of inhibition) and 2,5-dimethoxyphenyl derivative (H7) (42.23% of inhibition), as well as H9 against F. culmorum (46.75% of inhibition). Compounds were shown to be safe for beneficial soil bacteria and nematodes, except for compound H9 on EPN H. bacteriophora (18.75% mortality), which also showed the strongest inhibition against AChE (79.50% of inhibition). The molecular docking study revealed that antifungal activity is possible through the inhibition of proteinase K, and nematicidal activity is possible through the inhibition of AChE. The fluorinated pyrazole aldehydes are promising components of future plant protection products that could be environmentally and toxicologically acceptable. Full article

(This article belongs to the Special Issue Bioactive Natural Products: Composition, Molecular Mechanisms and Beneficial Effects)

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31 pages, 11742 KiB

Open AccessArticle

Vachellia farnesiana Pods or a Polyphenolic Extract Derived from Them Exert Immunomodulatory, Metabolic, Renoprotective, and Prebiotic Effects in Mice Fed a High-Fat Diet

by Claudia Delgadillo-Puga, Dulce R. Sánchez-Castillo, Yonatan Y. Cariño-Cervantes, Ivan Torre-Villalvazo, Claudia Tovar-Palacio, Sarai Vásquez-Reyes, Janette Furuzawa-Carballeda, Joshua Ayork Acevedo-Carabantes, María del Rayo Camacho-Corona, Jorge Luis Guzmán-Mar, Luis Cisneros-Zevallos, Armando R. Tovar, Rosa Rebollar-Vega, Georgina Hernández-Montes, Alfredo Ulloa-Aguirre, Berenice Palacios-Gonzalez and Lilia G. Noriega

Int. J. Mol. Sci. 2023, 24(9), 7984; https://doi.org/10.3390/ijms24097984 - 28 Apr 2023

Cited by 4 | Viewed by 2430

Abstract

Obesity causes systemic inflammation, hepatic and renal damage, as well as gut microbiota dysbiosis. Alternative vegetable sources rich in polyphenols are known to prevent or delay the progression of metabolic abnormalities during obesity. Vachellia farnesiana (VF) is a potent source of polyphenols with antioxidant and anti-inflammatory activities with potential anti-obesity effects. We performed an in vivo preventive or an interventional experimental study in mice and in vitro experiments with different cell types. In the preventive study, male C57BL/6 mice were fed with a Control diet, a high-fat diet, or a high-fat diet containing either 0.1% methyl gallate, 10% powdered VFP, or 0.5%, 1%, or 2% of a polyphenolic extract (PE) derived from VFP (Vachellia farnesiana pods) for 14 weeks. In the intervention study, two groups of mice were fed for 14 weeks with a high-fat diet and then one switched to a high-fat diet with 10% powdered VFP for ten additional weeks. In the in vitro studies, we evaluated the effect of a VFPE (Vachellia farnesiana polyphenolic extract) on glucose-stimulated insulin secretion in INS-1E cells or of naringenin or methyl gallate on mitochondrial activity in primary hepatocytes and C2C12 myotubes. VFP or a VFPE increased whole-body energy expenditure and mitochondrial activity in skeletal muscle; prevented insulin resistance, hepatic steatosis, and kidney damage; exerted immunomodulatory effects; and reshaped fecal gut microbiota composition in mice fed a high-fat diet. VFPE decreased insulin secretion in INS-1E cells, and its isolated compounds naringenin and methyl gallate increased mitochondrial activity in primary hepatocytes and C2C12 myotubes. In conclusion VFP or a VFPE prevented systemic inflammation, insulin resistance, and hepatic and renal damage in mice fed a high-fat diet associated with increased energy expenditure, improved mitochondrial function, and reduction in insulin secretion. Full article

(This article belongs to the Special Issue Bioactive Natural Products: Composition, Molecular Mechanisms and Beneficial Effects)

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