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Molecules
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Anti-Obesity Drug Discovery: Recent Advances and Future Perspectives
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Anti-Obesity Drug Discovery: Recent Advances and Future Perspectives

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

Deadline for manuscript submissions: 30 June 2024 | Viewed by 4135

Special Issue Editor

Dr. Liqing Zang

E-Mail Website
Guest Editor
Graduate School of Regional Innovation Studies, Mie University, Tsu, Mie 514-8507, Japan
Interests: obesity; diabetes; metabolic syndrome; natural product; zebrafish; molecular biology; pharmacology; drug screening
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Obesity is now an increasingly public global health issue. Overweight and obesity are defined as abnormal or excessive fat accumulation due to an energy imbalance between calorie intake and expenditure. Progressed obesity increases the heath threats, including hypertension, non-alcoholic fatty liver, cardiovascular diseases, diabetes, musculoskeletal disorders, and cancers. Lifestyle management (such as physical activity and calorie intake) and pharmaceutical medicines are primary treatments for obesity. However, lifestyle modification alone is frequently limited and challenging to maintain, and unfavorable side effects plague the current pharmacotherapy for obesity. For this reason, the continuous discovery of new anti-obesity drugs is needed. In addition, bioactive natural products and derived components have attracted attention to counteract obesity with minimal side effects.

Therefore, this Special Issue aims to focus on anti-obesity drug discovery, including but not limited to the following:

  • Anti-obesity drug discovery using culture cells, model animals, or clinical trials.
  • New bioactive compounds discovery and the related molecular mechanism research on obesity and related disease, including diabetes, diabetic complications, cardiovascular diseases, cancers, etc.
  • Bioactive chemicals work on inflammation, carcinogenesis, gut microbiota, body–brain crosstalk focusing on obesity and brain function, etc.
  • Methodology for optimizing anti-obesity drug discovery.

We encourage researchers to share their findings in this field, both in the form of original research or review articles.

Dr. Liqing Zang
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

  • obesity
  • metabolic syndrome
  • natural products
  • bioactive components
  • diabetes
  • cardiovascular disease
  • model animals
  • drug screening

Published Papers (3 papers)

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Research

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19 pages, 6422 KiB  
Article
The Hexane Extract of Citrus sphaerocarpa Ameliorates Visceral Adiposity by Regulating the PI3K/AKT/FoxO1 and AMPK/ACC Signaling Pathways in High-Fat-Diet-Induced Obese Mice
by Liqing Zang, Kazuhiro Kagotani, Takuya Hayakawa, Takehiko Tsuji, Katsuzumi Okumura, Yasuhito Shimada and Norihiro Nishimura
Molecules 2023, 28(24), 8026; https://doi.org/10.3390/molecules28248026 - 09 Dec 2023
Viewed by 1203
Abstract
Obesity is an emerging global health issue with an increasing risk of disease linked to lifestyle choices. Previously, we reported that the hexane extract of Citrus sphaerocarpa (CSHE) suppressed lipid accumulation in differentiated 3T3-L1 adipocytes. In this study, we conducted in vivo experiments [...] Read more.
Obesity is an emerging global health issue with an increasing risk of disease linked to lifestyle choices. Previously, we reported that the hexane extract of Citrus sphaerocarpa (CSHE) suppressed lipid accumulation in differentiated 3T3-L1 adipocytes. In this study, we conducted in vivo experiments to assess whether CSHE suppressed obesity in zebrafish and mouse models. We administered 10 and 20 μg/mL CSHE to obese zebrafish juveniles. CSHE significantly inhibited visceral fat accumulation compared to untreated obese fish. Moreover, the oral administration (100 μg/g body weight/day) of CSHE to high-fat-diet-induced obese mice significantly reduced their body weight, visceral fat volume, and hepatic lipid accumulation. The expression analyses of key regulatory genes involved in lipid metabolism revealed that CSHE upregulated the mRNA expression of lipolysis-related genes in the mouse liver (Pparα and Acox1) and downregulated lipogenesis-related gene (Fasn) expression in epididymal white adipose tissue (eWAT). Fluorescence immunostaining demonstrated the CSHE-mediated enhanced phosphorylation of AKT, AMPK, ACC, and FoxO1, which are crucial factors regulating adipogenesis. CSHE-treated differentiated 3T3L1 adipocytes also exhibited an increased phosphorylation of ACC. Therefore, we propose that CSHE suppresses adipogenesis and enhances lipolysis by regulating the PI3K/AKT/FoxO1 and AMPK/ACC signaling pathways. These findings suggested that CSHE is a promising novel preventive and therapeutic agent for managing obesity. Full article
(This article belongs to the Special Issue Anti-Obesity Drug Discovery: Recent Advances and Future Perspectives)
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Review

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25 pages, 2901 KiB  
Review
Could Natural Products Help in the Control of Obesity? Current Insights and Future Perspectives
by Jiwon Park, Fahrul Nurkolis, Hyunji Won, Jiye Yang, Dayeon Oh, Hyunkyung Jo, Jinwon Choi, Sanghyun Chung, Rudy Kurniawan and Bonglee Kim
Molecules 2023, 28(18), 6604; https://doi.org/10.3390/molecules28186604 - 13 Sep 2023
Cited by 3 | Viewed by 1810
Abstract
Obesity is a global issue faced by many individuals worldwide. However, no drug has a pronounced effect with few side effects. Green tea, a well-known natural product, shows preventive effects against obesity by decreasing lipogenesis and increasing fat oxidation and antioxidant capacity. In [...] Read more.
Obesity is a global issue faced by many individuals worldwide. However, no drug has a pronounced effect with few side effects. Green tea, a well-known natural product, shows preventive effects against obesity by decreasing lipogenesis and increasing fat oxidation and antioxidant capacity. In contrast, other natural products are known to contribute to obesity. Relevant articles published on the therapeutic effect of natural products on obesity were retrieved from PubMed, Web of Science, and Scopus. The search was conducted by entering keywords such as “obesity”, “natural product”, and “clinical trial”. The natural products were classified as single compounds, foods, teas, fruits, herbal medicines—single extract, herbal medicines—decoction, and herbal medicines—external preparation. Then, the mechanisms of these medicines were organized into lipid metabolism, anti-inflammation, antioxidation, appetite loss, and thermogenesis. This review aimed to assess the efficacy and mechanisms of effective natural products in managing obesity. Several clinical studies reported that natural products showed antiobesity effects, including Coffea arabica (coffee), Camellia sinensis (green tea), Caulerpa racemosa (green algae), Allium sativum (garlic), combined Ephedra intermedia Schrenk, Thea sinensis L., and Atractylodes lancea DC extract (known as Gambisan), Ephedra sinica Stapf, Angelica Gigantis Radix, Atractylodis Rhizoma Alba, Coicis semen, Cinnamomi cortex, Paeoniae radix alba, and Glycyrrhiza uralensis (known as Euiiyin-tang formula). Further studies are expected to refine the pharmacological effects of natural products for clinical use. Full article
(This article belongs to the Special Issue Anti-Obesity Drug Discovery: Recent Advances and Future Perspectives)
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Other

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16 pages, 2972 KiB  
Perspective
Unraveling Light-Activated Insulin Action in Regulating Blood Glucose: New Photoactivatable Insight as a Novel Modality in Diabetes Management
by Fahrul Nurkolis, Rudy Kurniawan, Elvan Wiyarta, Rony Abdi Syahputra, Reggie Surya, Nurpudji Astuti Taslim, Trina Ekawati Tallei, Raymond Rubianto Tjandrawinata, Eli Y. Adashi and Bonglee Kim
Molecules 2024, 29(6), 1294; https://doi.org/10.3390/molecules29061294 - 14 Mar 2024
Viewed by 739
Abstract
Diabetes, particularly type 2 diabetes (T2D), is the main component of metabolic syndrome. It is highly prevalent and has drastically increased with sedentary lifestyles, notably behaviors linked to ease of access and minimal physical activity. Central to this condition is insulin, which plays [...] Read more.
Diabetes, particularly type 2 diabetes (T2D), is the main component of metabolic syndrome. It is highly prevalent and has drastically increased with sedentary lifestyles, notably behaviors linked to ease of access and minimal physical activity. Central to this condition is insulin, which plays a pivotal role in regulating glucose levels in the body by aiding glucose uptake and storage in cells, and what happens to diabetes? In diabetes, there is a disruption and malfunction in insulin regulation. Despite numerous efforts, effectively addressing diabetes remains a challenge. This article explores the potential of photoactivatable drugs in diabetes treatment, with a focus on light-activated insulin. We discuss its advantages and significant implications. This article is expected to enrich the existing literature substantially, offering a comprehensive analysis of potential strategies for improving diabetes management. With its minimal physical intrusion, light-activated insulin promises to improve patient comfort and treatment adherence. It offers precise regulation and localized impact, potentially mitigating the risks associated with conventional diabetes treatments. Additionally, light-activated insulin is capable of explicitly targeting RNA and epigenetic factors. This innovative approach may pave the way for more personalized and effective diabetes treatments, addressing not only the symptoms but also the underlying biological causes of the disease. The advancement of light-activated insulin could revolutionize diabetes management. This study represents a pioneering introduction to this novel modality for diabetes management. Full article
(This article belongs to the Special Issue Anti-Obesity Drug Discovery: Recent Advances and Future Perspectives)
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