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Trends in Biologically Active Compounds for Biomedicines and Natural Products
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Trends in Biologically Active Compounds for Biomedicines and Natural Products

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

Deadline for manuscript submissions: closed (31 January 2023) | Viewed by 17130

Special Issue Editor

Dr. Weijun Kong

E-Mail Website
Guest Editor
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100193, China
Interests: natural products; analytical chemistry; isolation; identification; active compounds detection; molecules; materials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Researches on the extraction, isolation, identification, and detection of multiple compounds in food/plant-original natural products, as well as their bioactivity evaluation are all contained. Effective extraction and isolation methods for active compounds with new structures and activities, chemical and molecular identification of natural products and multiple components, new improved techniques for accurate quantitation, in vitro and in vivo activity assessment on cell, microorganism and animal, and other outstanding studies on active compounds in natural products are especially involved.

Research articles, reviews and comments are all welcome. 

Dr. Weijun Kong
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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

  • natural products
  • biomedicines
  • biologically active compounds
  • phytochemistry
  • extraction
  • isolation
  • molecular identification
  • detection
  • activity assessment

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Published Papers (6 papers)

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Research

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13 pages, 1686 KiB  
Article
A Novel Drug Delivery System: Hyodeoxycholic Acid-Modified Metformin Liposomes for Type 2 Diabetes Treatment
by Minghao Hu, Tingting Gou, Yuchen Chen, Min Xu, Rong Chen, Tao Zhou, Junjing Liu, Cheng Peng and Qiang Ye
Molecules 2023, 28(6), 2471; https://doi.org/10.3390/molecules28062471 - 8 Mar 2023
Cited by 5 | Viewed by 2746
Abstract
Metformin is a first-line drug for the clinical treatment of type 2 diabetes; however, it always leads to gastrointestinal tolerance, low bioavailability, short half-life, etc. Liposome acts as an excellent delivery system that could reduce drug side effects and promote bioavailability. Hyodeoxycholic acid, [...] Read more.
Metformin is a first-line drug for the clinical treatment of type 2 diabetes; however, it always leads to gastrointestinal tolerance, low bioavailability, short half-life, etc. Liposome acts as an excellent delivery system that could reduce drug side effects and promote bioavailability. Hyodeoxycholic acid, a cholesterol-like structure, can regulate glucose homeostasis and reduce the blood glucose levels. As an anti-diabetic active ingredient, hyodeoxycholic acid modifies liposomes to make it overcome the disadvantages of metformin as well as enhance the hypoglycemic effect. By adapting the thin-film dispersion method, three types of liposomes with different proportions of hyodeoxycholic acid and metformin were prepared (HDCA:ME-(0.5:1)-Lips, HDCA:ME-(1:1)-Lips, and HDCA:ME-(2:1)-Lips). Further, the liposomes were characterized, and the anti-type 2 diabetes activity of liposomes was evaluated. The results from this study indicated that three types of liposomes exhibited different characteristics—Excessive hyodeoxycholic acid decreased encapsulation efficiency and drug loading. In the in vivo experiments, liposomes could reduce the fasting blood glucose levels, improve glucose tolerance, regulate oxidative stress markers and protect liver tissue in type 2 diabetic mice. These results indicated that HDCA:ME-(1:1)-Lips was the most effective among the three types of liposomes prepared and showed better effects than metformin. Hyodeoxycholic acid can enhance the hypoglycemic effect of metformin and play a suitable role as an excipient in the liposome. Full article
(This article belongs to the Special Issue Trends in Biologically Active Compounds for Biomedicines and Natural Products)
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21 pages, 10911 KiB  
Article
Paeoniflorin Protects against Acetaminophen-Induced Liver Injury in Mice via JNK Signaling Pathway
by Xinyu Deng, Yubing Li, Xing Li, Zhenpeng Zhang, Shu Dai, Hefei Wu, Fangling Zhang, Qichao Hu, Yuan Chen, Jinhao Zeng and Xiao Ma
Molecules 2022, 27(23), 8534; https://doi.org/10.3390/molecules27238534 - 4 Dec 2022
Cited by 14 | Viewed by 2943
Abstract
Background: Drug-induced liver injury (DILI), represented by acetaminophen (APAP), is a common cause of acute liver failure in clinics. Paeoniflorin (PF) has been proven to demonstrate a significant hepatoprotective effect. However, it is still unclear whether it can be a potential agent against [...] Read more.
Background: Drug-induced liver injury (DILI), represented by acetaminophen (APAP), is a common cause of acute liver failure in clinics. Paeoniflorin (PF) has been proven to demonstrate a significant hepatoprotective effect. However, it is still unclear whether it can be a potential agent against hepatotoxicity induced by APAP. This study aimed to explore the preventive and therapeutic effects and mechanisms of PF on APAP-induced liver injury. Methods: Different doses of PF (50, 100, and 200 mg/kg) were given to C57BL/6 male mice for five consecutive days. After 12 h of APAP (250 mg/kg i.p.) treatment, blood and liver tissues were collected and isolated for detection. Results: The results showed that the therapeutic effects of PF on APAP mice were presented in the downregulation of the content of serum indices and significantly improved hepatic tissue edema and inflammatory infiltration. Meanwhile, PF reduces the level of the mitochondrial metabolic enzyme. Ulteriorly, it was found that PF has a downregulating effect on the apoptotic reaction and could inhibit the protein expression of CYP2E1/JNK signaling, which in turn reduces the damage of APAP. Conclusion: Our findings showed that PF acted as a protective agent against APAP-induced hepatotoxicity by inhibiting JNK-related signals, suggesting a novel insight into treating APAP-induced liver injury. Full article
(This article belongs to the Special Issue Trends in Biologically Active Compounds for Biomedicines and Natural Products)
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9 pages, 895 KiB  
Article
Daphnane-Type Diterpenes from Stelleropsis tianschanica and Their Antitumor Activity
by Xiaoyan He, Xiatiguli Abulizi, Xiaowan Li, Guoxu Ma, Zhaocui Sun, Hongyan Wei, Xudong Xu, Leiling Shi and Jing Zhang
Molecules 2022, 27(17), 5701; https://doi.org/10.3390/molecules27175701 - 4 Sep 2022
Cited by 1 | Viewed by 1643
Abstract
Four new daphnane-type diterpenes named tianchaterpenes C-F (1–4) and six known ones were isolated from Stelleropsis tianschanica. Their structures were elucidated based on chemical and spectral analyses. The comparisons of calculated and experimental electronic circular dichroism (ECD) methods [...] Read more.
Four new daphnane-type diterpenes named tianchaterpenes C-F (1–4) and six known ones were isolated from Stelleropsis tianschanica. Their structures were elucidated based on chemical and spectral analyses. The comparisons of calculated and experimental electronic circular dichroism (ECD) methods were used to determine the absolute configurations of new compounds. Additionally, compounds 1–10 were evaluated for their cytotoxic activities against HGC-27 cell lines; the results demonstrate that compound 2 had strong cytotoxic activities with IC50 values of 8.8 µM, for which activity was better than that of cisplatin (13.2 ± 0.67 µM). Full article
(This article belongs to the Special Issue Trends in Biologically Active Compounds for Biomedicines and Natural Products)
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9 pages, 1046 KiB  
Article
Five New Polyoxypregnane Glycosides from the Vines of Aspidopterysobcordata and Their Antinephrolithiasis Activity
by Zhaocui Sun, Meiying Chen, Qinglong Li, Guoxu Ma, Haifeng Wu, Junshan Yang, Yihang Li and Xudong Xu
Molecules 2022, 27(14), 4596; https://doi.org/10.3390/molecules27144596 - 19 Jul 2022
Viewed by 1453
Abstract
From the dried vines of Aspidopterys obcordata Hemsl, five new polyoxypregnane glycosides, named obcordatas J–N (1–5), were obtained. Their structures were fully elucidated and characterized by HRESIMS and extensive spectroscopic data. In addition, all of the new compounds were [...] Read more.
From the dried vines of Aspidopterys obcordata Hemsl, five new polyoxypregnane glycosides, named obcordatas J–N (1–5), were obtained. Their structures were fully elucidated and characterized by HRESIMS and extensive spectroscopic data. In addition, all of the new compounds were screened for their antinephrolithiasis activity in vitro. The results showed that compounds 1–3 have prominent protective effects on calcium oxalate crystal-induced human kidney 2 (HK-2) cells, with EC50 values ranging from 6.72 to 14.00 μM, which is consistent with the application value of A. obcordata in folk medicine for kidney stones. Full article
(This article belongs to the Special Issue Trends in Biologically Active Compounds for Biomedicines and Natural Products)
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Review

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21 pages, 1603 KiB  
Review
Interactions between Gut Microbiota and Polyphenols: New Insights into the Treatment of Fatigue
by Chuanhong Luo, Xichuan Wei, Jiao Song, Xiaorong Xu, Haozhou Huang, Sanhu Fan, Dingkun Zhang, Li Han and Junzhi Lin
Molecules 2022, 27(21), 7377; https://doi.org/10.3390/molecules27217377 - 30 Oct 2022
Cited by 19 | Viewed by 4351
Abstract
Fatigue seriously affects people’s work efficiency and quality of life and has become a common health problem in modern societies around the world. The pathophysiology of fatigue is complex and not fully clear. To some degree, interactions between gut microbiota and host may [...] Read more.
Fatigue seriously affects people’s work efficiency and quality of life and has become a common health problem in modern societies around the world. The pathophysiology of fatigue is complex and not fully clear. To some degree, interactions between gut microbiota and host may be the cause of fatigue progression. Polyphenols such as tannin, tea polyphenols, curcumin, and soybean isoflavones relieve fatigue significantly. Studies have shown that the gut microbiota is able to convert these active compounds into more active metabolites through intestinal fermentation. However, the mechanism of anti-fatigue polyphenols is currently mainly analyzed from the perspective of antioxidant and anti-inflammatory effects, and changes in gut microbiota are rarely considered. This review focuses on gut microecology and systematically summarizes the latest theoretical and research findings on the interaction of gut microbiota, fatigue, and polyphenols. First, we outline the relationship between gut microbiota and fatigue, including changes in the gut microbiota during fatigue and how they interact with the host. Next, we describe the interactions between the gut microbiota and polyphenols in fatigue treatment (regulation of the gut microbiota by polyphenols and metabolism of polyphenols by the gut microbiota), and how the importance of potential active metabolites (such as urolithin) produced by the decomposition of polyphenols by gut microbiota is emerging. Based on the new perspective of gut microbiota, this review provides interesting insights into the mechanism of polyphenols in fatigue treatment and clarifies the potential of polyphenols as targets for anti-fatigue product development, aiming to provide a useful basis for further research and design. Full article
(This article belongs to the Special Issue Trends in Biologically Active Compounds for Biomedicines and Natural Products)
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37 pages, 8748 KiB  
Review
The Biosynthesis Related Enzyme, Structure Diversity and Bioactivity Abundance of Indole-Diterpenes: A Review
by Yong Hou, Meiying Chen, Zhaocui Sun, Guoxu Ma, Deli Chen, Haifeng Wu, Junshan Yang, Yihang Li and Xudong Xu
Molecules 2022, 27(20), 6870; https://doi.org/10.3390/molecules27206870 - 13 Oct 2022
Cited by 6 | Viewed by 3032
Abstract
Indole diterpenes are a large class of secondary metabolites produced by fungi, possessing a cyclic diterpenoid backbone and an indole moiety. Novel structures and important biological activity have made indole diterpenes one of the focuses of synthetic chemists. Although the discovery, identification, structural [...] Read more.
Indole diterpenes are a large class of secondary metabolites produced by fungi, possessing a cyclic diterpenoid backbone and an indole moiety. Novel structures and important biological activity have made indole diterpenes one of the focuses of synthetic chemists. Although the discovery, identification, structural diversity, biological activity and especially structure–activity relationship of indole diterpenes have been reported in some papers in recent years, they are absent of a systematic and comprehensive analysis, and there is no elucidation of enzymes related to this kind of natural product. Therefore, it is necessary to summarize the relevant reports to provide new perspectives for the following research. In this review, for the first time, the function of related synthases and the structure–activity relationship of indole diterpenes are expounded, and the recent research advances of them are emphasized. Full article
(This article belongs to the Special Issue Trends in Biologically Active Compounds for Biomedicines and Natural Products)
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