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Discovery, Metabolism and Potential Bio-Activities of Natural Products in Traditional...
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Discovery, Metabolism and Potential Bio-Activities of Natural Products in Traditional Medicine 2024

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (25 July 2024) | Viewed by 5009

Special Issue Editors

Prof. Dr. Shengbao Cai

E-Mail Website
Guest Editor
Faculty of Food Science and Engineering, University of Science and Technology, Kunming 650500, China
Interests: bioactive compounds; bioaccessibility and bioavailability; bioactivity exploration; metabolism
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Jiangbo He

E-Mail Website
Guest Editor
School of Medicine, Kunming University, Kunming, 650208, China
Interests: isolation and identification of plant and microbial natural products
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Traditional medicine is a precious commodity accumulated by the struggle between human beings and nature. A large number of studies have found that natural products in traditional medicines contain active substances that treat diseases. Many of those natural products are being developed into clinical drugs or used as lead compounds for drug design and synthesis. With the development of modern separation technology, more and more trace natural products or metabolites have been discovered and identified. Moreover, it is well-known that the bioavailability and metabolic characteristics of natural products in vivo are an important basis for their biological activities. In addition, the exploration of the potential biological activities of those natural products is conducive to their further drug development and application. Therefore, this Special Issue is expected to collect original works or reviews on the latest advances and prospects of discovery, metabolism and potential bio-activities of natural products in traditional medicine. With this Special Issue, we hope to publish research results that will further promote people's understanding of the properties of the natural products isolated from traditional medicine and to contribute to the development of drugs based on those natural products.

Prof. Dr. Shengbao Cai
Prof. Dr. Jiangbo He
Guest Editors

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • traditional medicine
  • natural product
  • bioaccessibility and bioavailability
  • bioactivity evaluation
  • metabolism

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Published Papers (5 papers)

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Research

23 pages, 7313 KiB  
Article
Knockdown and Overexpression Experiments to Investigate the Inhibitory Mechanism of Fuzheng Xiaozheng Prescription, an Effective Chinese Herbal Formula for the Clinical Treatment of Hepatocellular Carcinoma
by Xia Li, Xiaofeng Chen, Han Yu, Renwei Huang, Peijie Wu, Yanju Gong, Xiping Chen and Chao Liu
Pharmaceuticals 2024, 17(9), 1159; https://doi.org/10.3390/ph17091159 - 31 Aug 2024
Viewed by 481
Abstract
Fuzheng Xiaozheng prescription (FZXZP) is an effective formula for the treatment of different kinds of chronic liver diseases. However, its potential molecular mechanisms in treating hepatocellular carcinoma (HCC) have not been investigated thoroughly. The aim of this study is to elucidate the targets [...] Read more.
Fuzheng Xiaozheng prescription (FZXZP) is an effective formula for the treatment of different kinds of chronic liver diseases. However, its potential molecular mechanisms in treating hepatocellular carcinoma (HCC) have not been investigated thoroughly. The aim of this study is to elucidate the targets and intrinsic mechanisms of FZXZP and their active components for the treatment of HCC. The efficacy of FZXZP against HCC was clarified through a rat HCC model and HCC cell culture. Network pharmacology and molecular docking were utilized to predict the mechanism of action and effector components of FZXZP. The key mechanism and targets were verified by the construction of overexpression and knockout cell models. The results showed that FZXZP greatly delayed the development of HCC in vivo experiments, as evidenced by biochemical evaluations, H&E analyses and growth inhibition of HCC. FZXZP dramatically inhibited cell viability and proliferative capacity and induced the apoptosis of hepatoma cells in vitro. Moreover, network pharmacology analyses demonstrated that the EGFR family and apoptosis-related targets were found to be the most significant in bioinformatics analysis. Furthermore, the EGFR/STAT3 signal axis might be the most likely target of FZXZP in anti-HCC due to the fact that it could be down-regulated by FZXZP with an upward trend of Bax, Caspase-3, Caspase-8, Caspase-9 and an inverse trend of Bcl2. Importantly, the above targeted signal axis was finally validated by our knockdown and overexpression analyses. Meanwhile, flow cytometry and TUNEL staining also revealed that FZXZP significantly induced apoptosis in the EGFR-overexpressing HCC cell line. The molecular docking results revealed that the key effector components of FZXZP that exerted the above regulatory roles were wogonin and glycitein. All of these results suggest that FZXZP could significantly delay HCC development by inhibiting proliferation and promoting apoptosis of HCC cells, and the EGFR/STAT3 signal axis might be a critical signal axis of FZXZP in suppressing HCC progression. Full article
(This article belongs to the Special Issue Discovery, Metabolism and Potential Bio-Activities of Natural Products in Traditional Medicine 2024)
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14 pages, 776 KiB  
Article
A Compound Containing Aldehyde Dehydrogenase Relieves the Effects of Alcohol Consumption and Hangover Symptoms in Healthy Men: An Open-Labeled Comparative Study
by In-Kyung Jeong, Anna Han, Ji Eun Jun, You-Cheol Hwang, Kyu Jeung Ahn, Ho Yeon Chung, Bo Seung Kang and Se-Young Choung
Pharmaceuticals 2024, 17(8), 1087; https://doi.org/10.3390/ph17081087 - 20 Aug 2024
Viewed by 504
Abstract
This open-labeled and comparative study aimed to test the efficacy and safety of a fermented rice extract-based substance containing yeast-fermented powder having aldehyde dehydrogenase (KisLip®, Pico Entech, Republic of Korea) in healthy male individuals. Healthy male subjects (n = 20) consumed [...] Read more.
This open-labeled and comparative study aimed to test the efficacy and safety of a fermented rice extract-based substance containing yeast-fermented powder having aldehyde dehydrogenase (KisLip®, Pico Entech, Republic of Korea) in healthy male individuals. Healthy male subjects (n = 20) consumed 90 g of alcohol at their first visit. At the second visit, participants consumed 90 g of alcohol or alcohol with a low dose of KISLip® (2000 mg, KL-L) and then 90 g of alcohol or alcohol with a high dose of KISLip® (3000 mg, KL-H) at the third visit. The efficacy of KISLip® depends on the mutational status of important genes related to alcohol metabolism, including alcohol dehydrogenase (ADH1B), cytochrome P4502E1 (CYP2E1 (5B) and CYP2E1 (6)), and aldehyde dehydrogenase (ALDH2). KISLip® significantly reduced the highest level (Cmax) of alcohol and overall levels of acetaldehyde compared to the alcohol-only group in a dose-dependent manner. These significant effects of KISLip® on alcohol metabolism were observed independent of mutations in the four genes. In addition, hangover symptoms were significantly decreased in the KISLip® treated groups. During the study, the participants did not show any adverse events after KISLip® intake. This clinical study suggested that supplementation of KISLip® had beneficial effects on alcohol metabolism and might ameliorate the severity of hangovers without any adverse events. Full article
(This article belongs to the Special Issue Discovery, Metabolism and Potential Bio-Activities of Natural Products in Traditional Medicine 2024)
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18 pages, 4283 KiB  
Article
Siraitia grosvenorii Extract Protects Lipopolysaccharide-Induced Intestinal Inflammation in Mice via Promoting M2 Macrophage Polarization
by Huining Wu, Mengru Guo, Linlu Zhao, Jin Zhang, Jieyi He, Anning Xu, Zhichao Yu, Xingbin Ma, Yanhong Yong, Youquan Li, Xianghong Ju and Xiaoxi Liu
Pharmaceuticals 2024, 17(8), 1023; https://doi.org/10.3390/ph17081023 - 4 Aug 2024
Viewed by 593
Abstract
Siraitia grosvenorii has anti-inflammatory, antioxidant, and immune-regulating effects, while macrophages play an important role in reducing inflammation. However, it is still unclear whether Siraitia grosvenorii extract (SGE) is effective in reducing inflammation by regulating macrophages. This study investigated the regulatory effect of SGE [...] Read more.
Siraitia grosvenorii has anti-inflammatory, antioxidant, and immune-regulating effects, while macrophages play an important role in reducing inflammation. However, it is still unclear whether Siraitia grosvenorii extract (SGE) is effective in reducing inflammation by regulating macrophages. This study investigated the regulatory effect of SGE on macrophage polarization in a lipopolysaccharide (LPS)-induced intestinal inflammation model after establishing the model in vitro and in vivo. The results from the in vivo model showed that, compared with the LPS group, SGE significantly improved ileal morphology, restored the ileal mucosal barrier, and reduced intestinal and systemic inflammation by increasing CD206 and reducing iNOS proteins. In the in vitro model, compared with the LPS group, SGE significantly reduced the expression of iNOS protein and cytokines (TNF-α, IL-1β, and IFN-γ) while significantly increasing the protein expression of CD206 in RAW264.7 cells. In conclusion, SGE can alleviate intestinal inflammation, protect the mucus barrier, and block the systemic immunosuppressive response by increasing M2 macrophages. Full article
(This article belongs to the Special Issue Discovery, Metabolism and Potential Bio-Activities of Natural Products in Traditional Medicine 2024)
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19 pages, 946 KiB  
Article
Bioactivity Profiling of Daedaleopsis confragosa (Bolton) J. Schröt. 1888: Implications for Its Possible Application in Enhancing Women’s Reproductive Health
by Djordje Ilić, Maja Karaman, Mirjana Bogavac, Jovana Mišković and Milena Rašeta
Pharmaceuticals 2024, 17(5), 600; https://doi.org/10.3390/ph17050600 - 8 May 2024
Viewed by 841
Abstract
This study investigates the bioactivity profile of wood-rotting fungal species Daedaleopsis confragosa (Bolton) J. Schröt. 1888, focusing on its antioxidant, cytotoxic, and genotoxic activities and enzyme modulation properties with respect to its possible application in terms of enhancing women’s reproductive health. Two types [...] Read more.
This study investigates the bioactivity profile of wood-rotting fungal species Daedaleopsis confragosa (Bolton) J. Schröt. 1888, focusing on its antioxidant, cytotoxic, and genotoxic activities and enzyme modulation properties with respect to its possible application in terms of enhancing women’s reproductive health. Two types of extracts, including those based on EtOH extraction (DC) and hydrodistillation (DCHD), were investigated. The results indicate that the radical scavenging capacity against the DPPH radical and reduction potential were stronger in the DC extracts owing to the higher total phenolic content (TPC) and total flavonoid content (TFC) (25.30 ± 1.05 mg GAE/g d.w. and 2.84 ± 0.85 mg QE/g d.w., respectively). The same trend was observed in the protein phosphatase-1 (PP1) activity and in the genotoxic activity against the δ virus since only the DC extract exhibited DNA disintegration regarding a dilution of 1:100. Conversely, the DCHD extract exhibited increased hemolytic and cytotoxic effects (339.39% and IC50 = 27.76 ± 0.89 μg/mL—72 h incubation, respectively), along with greater inhibition of the AChE enzyme (IC50 = 3.11 ± 0.45 mg/mL) and hemolytic activity. These results suggest that terpenoids and steroids may be responsible for the observed activity in DCHD as these compounds could potentially be extracted following the HD procedure. This comprehensive bioactivity profiling offers valuable insights into the potential therapeutic applications of D. confragosa from Serbia and underscores the importance of further investigations for harnessing its pharmacological potential. Full article
(This article belongs to the Special Issue Discovery, Metabolism and Potential Bio-Activities of Natural Products in Traditional Medicine 2024)
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22 pages, 11173 KiB  
Article
Exploring the Mechanisms of Traditional Chinese Herbal Therapy in Gastric Cancer: A Comprehensive Network Pharmacology Study of the Tiao-Yuan-Tong-Wei decoction
by Juan Chen, Jingdong Kang, Shouli Yuan, Peter O’Connell, Zizhu Zhang, Lina Wang, Junying Liu and Rongfeng Chen
Pharmaceuticals 2024, 17(4), 414; https://doi.org/10.3390/ph17040414 - 25 Mar 2024
Cited by 1 | Viewed by 1877
Abstract
The use of herbal medicine as an adjuvant therapy in the management of gastric cancer has yielded encouraging outcomes, notably in enhancing overall survival rates and extending periods of disease remission. Additionally, herbal medicines have demonstrated potential anti-metastatic effects in gastric cancer. Despite [...] Read more.
The use of herbal medicine as an adjuvant therapy in the management of gastric cancer has yielded encouraging outcomes, notably in enhancing overall survival rates and extending periods of disease remission. Additionally, herbal medicines have demonstrated potential anti-metastatic effects in gastric cancer. Despite these promising findings, there remains a significant gap in our understanding regarding the precise pharmacological mechanisms, the identification of specific herbal compounds, and their safety and efficacy profiles in the context of gastric cancer therapy. In addressing this knowledge deficit, the present study proposes a comprehensive exploratory analysis of the Tiao-Yuan-Tong-Wei decoction (TYTW), utilizing an integrative approach combining system pharmacology and molecular docking techniques. This investigation aims to elucidate the pharmacological actions of TYTW in gastric pathologies. It is hypothesized that the therapeutic efficacy of TYTW in counteracting gastric diseases stems from its ability to modulate key signaling pathways, thereby influencing PIK3CA activity and exerting anti-inflammatory effects. This modulation is observed predominantly in pathways such as PI3K/AKT, MAPK, and those directly associated with gastric cancer. Furthermore, the study explores how TYTW’s metabolites (agrimoniin, baicalin, corosolic acid, and luteolin) interact with molecular targets like AKT1, CASP3, ESR1, IL6, PIK3CA, and PTGS2, and their subsequent impact on these critical pathways and biological processes. Therefore, this study represents preliminary research on the anticancer molecular mechanism of TYTW by performing network pharmacology and providing theoretical evidence for further experimental investigations. Full article
(This article belongs to the Special Issue Discovery, Metabolism and Potential Bio-Activities of Natural Products in Traditional Medicine 2024)
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