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Natural Products: Chemical Composition and Pharmacological Activity

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (29 February 2024) | Viewed by 15734

Special Issue Editor


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Guest Editor
College of Chinese Medicinal Materials, Jilin Agricultural University, Changchun, China
Interests: natural medicinal resources; molecular pharmacology; the minor ginsenosides and physiological function of terpenoid natural products from Chinese herbal medicine
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Human life cannot live without natural products, such as plant ingredients, including food, drugs, health products, and even cosmetics. Currently, about 40% of drugs are directly or indirectly derived from natural products, which provides many structurally novel active molecules for new drug development. For example, natural products, such as paclitaxel and vincristine, have exerted their pharmacological activities through different mechanisms of action and have taken their place.

In this Special Issue, we address both the chemical composition and pharmacological activity of natural products. We focus on the chemical identification and extraction and separation of natural products, based on which we can improve the extraction process and even explore technical formulations to achieve industrial production, exploring classical and innovative methods. In addition, research on the potential pharmacological activity of these natural products will also be focused on.

Natural products produce far fewer side effects in humans than synthetic drugs, and these studies promote their application in the future. We look forward to receiving contributions to this Special Issue from scholars and experts, and welcome your participation in the exchange and discussion of this topic.

Prof. Dr. Wei Li
Guest Editor

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Keywords

  • chemical composition
  • extraction and separation
  • industrial production
  • pharmacological activity

Published Papers (10 papers)

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Research

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18 pages, 2630 KiB  
Article
Study on the Compositional Analysis, Extraction Process, and Hemostatic and Anti-Inflammatory Activities of Cirsium japonicum Fisch. ex DC.Cirsium setosum (Willd.) MB Extracts
by Fanyu Kong, Zhongxue Fang, Biyue Cui, Jinshuang Gao, Changhai Sun and Shuting Zhang
Molecules 2024, 29(9), 1918; https://doi.org/10.3390/molecules29091918 - 23 Apr 2024
Viewed by 198
Abstract
Cirsium japonicum Fisch. ex DC. (CF) and Cirsium setosum (Willd.) MB (CS) are commonly used clinically to stop bleeding and eliminate carbuncles. Still, CF is mainly used for treating inflammation, while CS favors hemostasis. Therefore, the present study used UHPLC-MS to analyze the [...] Read more.
Cirsium japonicum Fisch. ex DC. (CF) and Cirsium setosum (Willd.) MB (CS) are commonly used clinically to stop bleeding and eliminate carbuncles. Still, CF is mainly used for treating inflammation, while CS favors hemostasis. Therefore, the present study used UHPLC-MS to analyze the main chemical constituents in CF-CS extract. We optimized the extraction process using single-factor experiments and response surface methodology. Afterward, the hemostatic and anti-inflammatory effects of CF-CS extract were investigated by determining the clotting time in vitro, the bleeding time of rabbit trauma, and the induction of rabbit inflammation using xylene and lipopolysaccharide. The study of hemostatic and anti-inflammatory effects showed that the CF-CS, CF, and CS extract groups could significantly shorten the coagulation time and bleeding time of rabbits compared with the blank group (p < 0.01); compared with the model group, it could dramatically inhibit xylene-induced ear swelling in rabbits and the content of TNF-α, IL-6, and IL-1β in the serum of rabbits (p < 0.01). The results showed that combined CF and CS synergistically increased efficacy. CF-CS solved the problem of the single hemostatic and anti-inflammatory efficacy of a single drug, which provided a new idea for the research and development of natural hemostatic and anti-inflammatory medicines. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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14 pages, 8500 KiB  
Article
Cynaroside Induces G1 Cell Cycle Arrest by Downregulating Cell Division Cycle 25A in Colorectal Cancer
by Shan Lei, Wenpeng Cao, Zhirui Zeng, Lu Wang, Jinzhi Lan and Tengxiang Chen
Molecules 2024, 29(7), 1508; https://doi.org/10.3390/molecules29071508 - 28 Mar 2024
Viewed by 622
Abstract
Natural chemicals derived from herbal plants have recently been recognized as potentially useful treatment alternatives owing to their ability to target a wide range of important biological molecules. Cynaroside is one of these natural compounds with promising anticancer activity for numerous tumor types. [...] Read more.
Natural chemicals derived from herbal plants have recently been recognized as potentially useful treatment alternatives owing to their ability to target a wide range of important biological molecules. Cynaroside is one of these natural compounds with promising anticancer activity for numerous tumor types. Nevertheless, the anticancer effects and molecular mechanisms of action of cynaroside on colorectal cancer (CRC) remain unclear. In this study, cynaroside was found to markedly inhibit CRC cell proliferation and colony formation in vitro. Cynaroside also inhibited cell proliferation in vivo and decreased the expression of KI67, a cell nuclear antigen. RNA sequencing revealed 144 differentially expressed genes (DEGs) in HCT116 cells and 493 DEGs in RKO cells that were enriched in the cell cycle signaling pathway. Cell division cycle 25A (CDC25A), a DEG widely enriched in the cell cycle signaling pathway, is considered a key target of cynaroside in CRC cells. Cynaroside also inhibited DNA replication and arrested cells in the G1/S phase in vitro. The expression levels of CDC25A and related G1-phase proteins were significantly elevated after CDC25A overexpression in CRC cells, which partially reversed the inhibitory effect of cynaroside on CRC cell proliferation and G1/S-phase arrest. In summary, cynaroside may be used to treat CRC as it inhibits CDC25A expression. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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20 pages, 5733 KiB  
Article
The Extracts Derived from Artemisia japonica Thunb. Leaves Mitigate Oxidative Stress and Inflammatory Response Induced by LPS in RAW264.7 Cells through Modulation of the Nrf2/HO-1 Signaling Pathway
by Yueyu Ye, Xiaomei Li, Man Chen, Xia Wang, Meiya Li, Fusheng Jiang, Xiaobo Zhang, Chunchun Zhang and Shiqing Li
Molecules 2024, 29(6), 1375; https://doi.org/10.3390/molecules29061375 - 20 Mar 2024
Viewed by 524
Abstract
Artemisia japonica Thunb. has been used as a traditional Chinese medicine and a vegetable for thousands of years in China. However, there are few reports on the chemical composition and biological activity of its leaves. Thus, this study aimed to evaluate the chemical [...] Read more.
Artemisia japonica Thunb. has been used as a traditional Chinese medicine and a vegetable for thousands of years in China. However, there are few reports on the chemical composition and biological activity of its leaves. Thus, this study aimed to evaluate the chemical composition, antioxidant and anti-inflammatory effects of water extracts of A. japonica leaves and their underlying mechanisms. A total of 48 compounds were identified in the water extract using UPLC-QTOF-MS2 analysis, with phenolic acids, particularly chlorogenic acid compounds, being the predominant components. The ethyl acetate fraction (EAF) contained most of the total phenolic content (385.4217 mg GAE/g) and displayed superior antioxidant capacity with the IC50DPPH•, IC50ABTS•+, and OD0.5reducing power at 10.987 μg/mL, 43.630 μg/mL and 26.883 μg/mL, respectively. Furthermore, EAF demonstrated potent antioxidant and anti-inflammatory effects in LPS-induced RAW264.7 cells by upregulating the Nrf2/HO-1 signal pathway. These findings highlight that A. japonica leaves possess remarkable abilities to mitigate inflammation and oxidative stress, suggesting their potential utilization as medicinal agents and food additives for promoting human health. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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16 pages, 5062 KiB  
Article
Nodakenin Ameliorates Ovariectomy-Induced Bone Loss by Regulating Gut Microbiota
by Chunxiao Liu, Jingyue Chen, Zijiao Wang, Yueyao Li, Yuanyuan Zhang and Guangyu Li
Molecules 2024, 29(6), 1240; https://doi.org/10.3390/molecules29061240 - 11 Mar 2024
Viewed by 768
Abstract
Disordered gut microbiota (GM) structure and function may contribute to osteoporosis (OP). Nodakenin has been shown to ameliorate osteoporosis; however, its anti-osteoporotic mechanism is unknown. This study aimed to further reveal the mechanism of the anti-osteoporotic action of nodakenin from the perspective of [...] Read more.
Disordered gut microbiota (GM) structure and function may contribute to osteoporosis (OP). Nodakenin has been shown to ameliorate osteoporosis; however, its anti-osteoporotic mechanism is unknown. This study aimed to further reveal the mechanism of the anti-osteoporotic action of nodakenin from the perspective of the microbiome and metabolome. An osteoporosis model was induced in mice through ovariectomy (OVX), with bone mass and microstructure assessed using μCT. Subsequently, ELISA and histologic examination were used to detect biochemical indicators of bone conversion and intestinal morphology. Using metabolomics and 16S rRNA sequencing, it was possible to determine the composition and abundance of the gut microbiota in feces. The results revealed that nodakenin treatment improved the bone microstructure and serum levels of bone turnover markers, and increased the intestinal mucosal integrity. 16S rRNA sequencing analysis revealed that nodakenin treatment decreased the relative abundance of Firmicutes and Patescibacteria, as well as the F/B ratio, and elevated the relative abundance of Bacteroidetes in OVX mice. In addition, nodakenin enhanced the relative abundance of Muribaculaceae and Allobaculum, among others, at the genus level. Moreover, metabolomics analysis revealed that nodakenin treatment significantly altered the changes in 113 metabolites, including calcitriol. A correlation analysis revealed substantial associations between various gut microbiota taxa and both the osteoporosis phenotype and metabolites. In summary, nodakenin treatment alleviated OVX-induced osteoporosis by modulating the gut microbiota and intestinal barrier. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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17 pages, 4805 KiB  
Article
Microanalysis Characterization and Immunomodulatory Effect for Selenium-Enriched Polysaccharide from Morchella esculenta (L.) Pers.
by Lijuan Qian, Mengxiang Du, Xiaoyan Yang, Qian Wang, Shengwei Huang, Yuhan Ma and Yujun Sun
Molecules 2023, 28(7), 2885; https://doi.org/10.3390/molecules28072885 - 23 Mar 2023
Cited by 4 | Viewed by 1684
Abstract
Morchella esculenta (L.) Pers., referred to as Morel, is a medicinal and edible homologous fungus, which contains many bioactive substances. In Morel, polysaccharides are the most abundant and have various bioactivities. In the present work, two novel polysaccharides, Se-MPS and MPS, [...] Read more.
Morchella esculenta (L.) Pers., referred to as Morel, is a medicinal and edible homologous fungus, which contains many bioactive substances. In Morel, polysaccharides are the most abundant and have various bioactivities. In the present work, two novel polysaccharides, Se-MPS and MPS, were prepared and purified from selenium-enriched (Se-enriched) and common Morel mycelia, respectively, and their structural and immunomodulatory properties were evaluated. The results show that Se-enriched treatment significantly changed the polysaccharides’ chemical composition, molecular weight, and sugar chain configuration. In addition, the Se-enriched treatment also improved the polysaccharides’ fragmentation and thermal stability. Importantly, Se-enriched Morel polysaccharide (Se-MPS) could significantly enhance phagocytosis of RAW 264.7 macrophage cells and, remarkably, activate their immune response via activating the TLR4-TRAF6-MAPKs-NF-κB cascade signaling pathway, finally exerting an immunomodulatory function. Based on these findings, selenium-enriched Morel polysaccharide appears to have more potential for development and utilization in functional foods or medicines than ordinary Morel polysaccharide. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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18 pages, 3849 KiB  
Article
Saikosaponin A and Its Epimers Alleviate LPS-Induced Acute Lung Injury in Mice
by Donghui Peng, Yuchan Chen, Yanping Sun, Zhihong Zhang, Na Cui, Wensen Zhang, Ying Qi, Yuanning Zeng, Bin Hu, Bingyou Yang, Qiuhong Wang and Haixue Kuang
Molecules 2023, 28(3), 967; https://doi.org/10.3390/molecules28030967 - 18 Jan 2023
Cited by 6 | Viewed by 1494
Abstract
The purpose of this work was to illustrate the effect of processing with vinegar on saikosaponins of Bupleurum chinense DC. (BC) and the protective effects of saikosaponin A (SSA), saikosaponin b1 (SSb1), saikosaponin b2 (SSb2), and saikosaponin D (SSD) in lipopolysaccharide (LPS)-induced acute [...] Read more.
The purpose of this work was to illustrate the effect of processing with vinegar on saikosaponins of Bupleurum chinense DC. (BC) and the protective effects of saikosaponin A (SSA), saikosaponin b1 (SSb1), saikosaponin b2 (SSb2), and saikosaponin D (SSD) in lipopolysaccharide (LPS)-induced acute lung injury (ALI) mice. We comprehensively evaluated the anti-inflammatory effects and potential mechanisms of SSA, SSb1, SSb2, and SSD through an LPS-induced ALI model using intratracheal injection. The results showed that SSA, SSb1, SSb2, and SSD significantly decreased pulmonary edema; reduced the levels of IL-6, TNF-α, and IL-1β in serum and lung tissues; alleviated pulmonary pathological damage; and decreased the levels of the IL-6, TNF-α, and IL-1β genes and the expression of NF-κB/TLR4-related proteins. Interestingly, they were similar in structure, but SSb2 had a better anti-inflammatory effect at the same dose, according to a principal component analysis. These findings indicated that it may not have been comprehensive to only use SSA and SSD as indicators to evaluate the quality of BC, especially as the contents of SSb1 and SSb2 in vinegar-processed BC were significantly increased. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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13 pages, 4070 KiB  
Article
Effects of Drying Temperature and Solvents on In Vitro Diabetic Wound Healing Potential of Moringa oleifera Leaf Extracts
by Saima Muzammil, Jorddy Neves Cruz, Rabia Mumtaz, Ijaz Rasul, Sumreen Hayat, Muhammad Asaf Khan, Arif Muhammad Khan, Muhammad Umar Ijaz, Rafael Rodrigues Lima and Muhammad Zubair
Molecules 2023, 28(2), 710; https://doi.org/10.3390/molecules28020710 - 11 Jan 2023
Cited by 14 | Viewed by 2987
Abstract
The delayed healing of wounds among people with diabetes is a severe problem worldwide. Hyperglycemia and increased levels of free radicals are the major inhibiting factors of wound healing in diabetic patients. Plant extracts are a rich source of polyphenols, allowing them to [...] Read more.
The delayed healing of wounds among people with diabetes is a severe problem worldwide. Hyperglycemia and increased levels of free radicals are the major inhibiting factors of wound healing in diabetic patients. Plant extracts are a rich source of polyphenols, allowing them to be an effective agent for wound healing. Drying temperature and extraction solvent highly affect the stability of polyphenols in plant materials. However, there is a need to optimize the extraction protocol to ensure the efficacy of the final product. For this purpose, the effects of drying temperature and solvents on the polyphenolic composition and diabetic wound healing activity of Moringa oleifera leaves were examined in the present research. Fresh leaves were oven dried at different temperatures (10 °C, 30 °C, 50 °C, and 100 °C) and extracted in three solvents (acetone, ethanol, and methanol) to obtain twelve extracts in total. The extracts were assessed for free radical scavenging and antihyperglycemic effects using DPPH (2,2-diphenylpicrylhydrazyl) and α- glucosidase inhibition assays. Alongside this, a scratch assay was performed to evaluate the cell migration activity of M. oleifera on the human retinal pigment epithelial cell line. The cytotoxicity of the plant extracts was assessed on human retinal pigment epithelial (RPE) and hepatocellular carcinoma (Huh-7) cell lines. Using high-performance liquid chromatography, phenolic compounds in extracts of M. oleifera were identified. We found that an ethanol-based extract prepared by drying the leaves at 10 °C contained the highest amounts of identified polyphenols. Moringa oleifera extracts showed remarkable antioxidant, antidiabetic, and cell migration properties. The best results were obtained with leaves dried at 10 °C and 30 °C. Decreased activities were observed with drying temperatures of 50 °C and above. Moreover, M. oleifera extracts exhibited no toxicity on RPE cells, and the same extracts were cytotoxic for Huh-7 cells. This study revealed that M. oleifera leaves extracts can enhance wound healing in diabetic conditions due to their antihyperglycemic, antioxidant, and cell migration effects. The leaves of this plant can be an excellent therapeutic option when extracted at optimum conditions. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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Review

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47 pages, 2990 KiB  
Review
Sesquiterpenoids from Meliaceae Family and Their Biological Activities
by Sandra Amalia Riyadi, Al Arofatus Naini and Unang Supratman
Molecules 2023, 28(12), 4874; https://doi.org/10.3390/molecules28124874 - 20 Jun 2023
Cited by 4 | Viewed by 1910
Abstract
Sesquiterpenoids, an important class of natural products possessing three isoprene-derived units, are widely distributed across plants and have a variety of biological activities. All sesquiterpenoids are derived from farnesyl pyrophosphate (FPP), a biosynthesis precursor that can form various carbon skeletons. In order to [...] Read more.
Sesquiterpenoids, an important class of natural products possessing three isoprene-derived units, are widely distributed across plants and have a variety of biological activities. All sesquiterpenoids are derived from farnesyl pyrophosphate (FPP), a biosynthesis precursor that can form various carbon skeletons. In order to provide a reference for further research and development of these compounds, this review focused on the increasing number of isolated and volatile sesquiterpenoids found to be produced by plants of the Meliaceae family between 1968 and 2023. The related articles were collected from SciFinder, Google Scholar, and PubMed. According to a literature review, several studies were started for more than 55 years on the plant’s stem barks, twigs, leaves, flowers, seeds, and pericarps, where approximately 413 sesquiterpenoid compounds from several groups such as eudesmane, aromadendrane, cadinane, guaiane, bisabolane, furanoeremophilane, humulene, germacrane, and oppositane-type were isolated and identified with some minor products. Additionally, the hypothetical route of sesquiterpenoids biosynthesis from this family was identified, and eudesmane-type was reported to be 27% of the total compounds. The antimicrobial, antidiabetic, antioxidant, antiplasmodial, antiviral, and cytotoxic activities of the isolated compounds and major volatile sesquiterpenoids constituent on essential oil were also evaluated. The result showed the fundamental of using the sesquiterpenoid compounds from the Meliaceae family in traditional medicine and the discovery of new drugs. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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14 pages, 1085 KiB  
Review
Review on Extraction, Modification, and Synthesis of Natural Peptides and Their Beneficial Effects on Skin
by Jiabing An, Ivan Stève Nguepi Tsopmejio, Zi Wang and Wei Li
Molecules 2023, 28(2), 908; https://doi.org/10.3390/molecules28020908 - 16 Jan 2023
Cited by 2 | Viewed by 2158
Abstract
Peptides, functional nutrients with a size between those of large proteins and small amino acids, are easily absorbed by the human body. Therefore, they are seeing increasing use in clinical medicine and have revealed immunomodulatory and anti-inflammatory properties which could make them effective [...] Read more.
Peptides, functional nutrients with a size between those of large proteins and small amino acids, are easily absorbed by the human body. Therefore, they are seeing increasing use in clinical medicine and have revealed immunomodulatory and anti-inflammatory properties which could make them effective in healing skin wounds. This review sorted and summarized the relevant literature about peptides during the past decade. Recent works on the extraction, modification and synthesis of peptides were reviewed. Importantly, the unique beneficial effects of peptides on the skin were extensively explored, providing ideas for the development and innovation of peptides and laying a knowledge foundation for the clinical application of peptides. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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19 pages, 1996 KiB  
Review
Current Research of Phytochemical, Medicinal and Non-Medicinal Uses of Uncaria gambir Roxb.: A Review
by Indah Putri Munggari, Dikdik Kurnia, Yusi Deawati and Euis Julaeha
Molecules 2022, 27(19), 6551; https://doi.org/10.3390/molecules27196551 - 03 Oct 2022
Cited by 4 | Viewed by 2493
Abstract
Uncaria gambir Roxb. is a plant from Southeast Asia and is widely used as an alternative medicine with various applications. This plant has been widely used in traditional medicine. This paper aims to provide information on U. gambir, a summary of data [...] Read more.
Uncaria gambir Roxb. is a plant from Southeast Asia and is widely used as an alternative medicine with various applications. This plant has been widely used in traditional medicine. This paper aims to provide information on U. gambir, a summary of data on phytochemicals and on medical and nonmedical activities. Phytochemical studies reveal biologically active constituents such as flavonoids, phenolics, and alkaloids. Various studies have shown that extracts and compounds obtained from U. gambir have medical uses for their antioxidant, antibacterial, anti-helminthic, anticancer, antifungal, anti-inflammatory, anti-hyperglycemic, anti-hyperuricemic, anti-lipid peroxidation, antihyperlipidemic and other properties. In addition, this extract has other uses, such as adsorbent for dyes and metal ions, as well as corrosion inhibition. Thus, U. gambir, which is commonly used in traditional medicine, is a potential plant for many therapeutic applications and prospects for drug development as well as other applications such as adsorbent and corrosion inhibition. Full article
(This article belongs to the Special Issue Natural Products: Chemical Composition and Pharmacological Activity)
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