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Medicines for the Treatment of Obesity
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Medicines for the Treatment of Obesity

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pathology, Diagnostics, and Therapeutics".

Deadline for manuscript submissions: closed (31 January 2021) | Viewed by 35262

Special Issue Editor

Prof. Dr. Michung Yoon

E-Mail Website
Guest Editor
Department of Biomedical Engineering, Mokwon University, Daejeon 35349, Republic of Korea
Interests: obesity; herbal medicine; peroxisome proliferator-activated receptor α; angiogenesis; nonalcoholic fatty liver disease; ginseng

Special Issue Information

Dear Colleagues,

Obesity is the result of an energy imbalance caused by an increased ratio of caloric intake to energy expenditure. In conjunction with obesity, such related metabolic disorders as type 2 diabetes, dyslipidemia, atherosclerosis, and nonalcoholic fatty liver disease have become global health problems. The number of obese patients is increasing in many countries all over the world. Reducing body weight by lifestyle modification is recommended, but drug intervention is necessary for morbidly obese individuals. Antiobesity drugs can be divided into several categories: central appetite suppressants, digestion and absorption blockers, metabolic promoters, obesity gene product inhibitors, and other drugs for the treatment of obesity. Five drug therapies, including orlistat, locarserin, phentermine/topiramate, and bupropion/naltrexone, approved by the FDA, are currently being used for the treatment of obesity. Additionally, there has been a great increase in the use of alternative treatments, such as herbal remedies, for the treatment of obesity since there remains a need for safer and more effective alternative therapies to the long-term use of synthetic chemical drugs. Furthermore, it is also reported that imbalanced intestinal microbiota can contribute to obesity, suggesting the antiobesity potential of probiotics.

This Special Issue, "Medicines for the Treatment of Obesity”, of the International Journal of Molecular Sciences will comprise a selection of research papers and reviews that will contribute to understanding the efficacy, safety, and mechanisms of medicines used in the treatment of obesity. Potential topics include but are not limited to the following approaches:

  1. Synthetic chemical drugs as antiobesity strategies;
  2. Herbal medicines and their products as antiobesity approaches;
  3. Probiotics as potential antiobesity strategies.

Prof. Dr. Michung Yoon
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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
  • Antiobesity drug
  • Synthetic chemical drug
  • Herbal medicine
  • Complementary and alternative medicine
  • Probiotics
  • Gut microbiota
  • Pharmacotherapy
  • Efficacy
  • Safety
  • Mechanism

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Published Papers (6 papers)

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Editorial

Jump to: Research, Review

2 pages, 171 KiB  
Editorial
Medicines for the Treatment of Obesity
by Soonshik Shin and Michung Yoon
Int. J. Mol. Sci. 2021, 22(8), 3866; https://doi.org/10.3390/ijms22083866 - 8 Apr 2021
Cited by 3 | Viewed by 2278
Abstract
Obesity is the result of an energy imbalance caused by an increased ratio of caloric intake to energy expenditure [...] Full article
(This article belongs to the Special Issue Medicines for the Treatment of Obesity)

Research

Jump to: Editorial, Review

17 pages, 5165 KiB  
Article
Lemon Balm Extract ALS-L1023 Regulates Obesity and Improves Insulin Sensitivity via Activation of Hepatic PPARα in High-Fat Diet-Fed Obese C57BL/6J Mice
by Dongju Lee, Yujin Shin, Jong Seong Roh, Jiwon Ahn, Sunhyo Jeoong, Soon Shik Shin and Michung Yoon
Int. J. Mol. Sci. 2020, 21(12), 4256; https://doi.org/10.3390/ijms21124256 - 15 Jun 2020
Cited by 11 | Viewed by 5653
Abstract
Our previous studies demonstrated that peroxisome proliferator-activated receptor α (PPARα) activation reduces weight gain and improves insulin sensitivity in obese mice. Since excess lipid accumulation in non-adipose tissues is suggested to be responsible for the development of insulin resistance, this study was undertaken [...] Read more.
Our previous studies demonstrated that peroxisome proliferator-activated receptor α (PPARα) activation reduces weight gain and improves insulin sensitivity in obese mice. Since excess lipid accumulation in non-adipose tissues is suggested to be responsible for the development of insulin resistance, this study was undertaken to examine whether the lemon balm extract ALS-L1023 regulates hepatic lipid accumulation, obesity, and insulin resistance and to determine whether its mechanism of action involves PPARα. Administration of ALS-L1023 to high-fat-diet-induced obese mice caused reductions in body weight gain, visceral fat mass, and visceral adipocyte size without changes of food consumption profiles. ALS-L1023 improved hyperglycemia, hyperinsulinemia, glucose and insulin tolerance, and normalized insulin-positive β-cell area in obese mice. ALS-L1023 decreased hepatic lipid accumulation and concomitantly increased the expression of PPARα target genes responsible for fatty acid β-oxidation in livers. In accordance with the in vivo data, ALS-L1023 reduced lipid accumulation and stimulated PPARα reporter gene expression in HepG2 cells. These effects of ALS-L1023 were comparable to those of the PPARα ligand fenofibrate, while the PPARα antagonist GW6471 inhibited the actions of ALS-L1023 on lipid accumulation and PPARα luciferase activity in HepG2 cells. Higher phosphorylated protein kinase B (pAkt)/Akt ratios and lower expression of gluconeogenesis genes were observed in the livers of ALS-L1023-treated mice. These results indicate that ALS-L1023 may inhibit obesity and improve insulin sensitivity in part through inhibition of hepatic lipid accumulation via hepatic PPARα activation. Full article
(This article belongs to the Special Issue Medicines for the Treatment of Obesity)
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15 pages, 1518 KiB  
Article
Relationship between IL-8 Circulating Levels and TLR2 Hepatic Expression in Women with Morbid Obesity and Nonalcoholic Steatohepatitis
by Teresa Auguet, Laia Bertran, Jessica Binetti, Carmen Aguilar, Salomé Martínez, Fàtima Sabench, Jesús Miguel Lopez-Dupla, José Antonio Porras, David Riesco, Daniel Del Castillo and Cristóbal Richart
Int. J. Mol. Sci. 2020, 21(11), 4189; https://doi.org/10.3390/ijms21114189 - 11 Jun 2020
Cited by 34 | Viewed by 4104
Abstract
The progression of nonalcoholic fatty liver disease (NAFLD) to nonalcoholic steatohepatitis (NASH) is linked to systemic inflammation. Currently, two of the aspects that need further investigation are diagnosis and treatment of NASH. In this sense, the aim of this study was to assess [...] Read more.
The progression of nonalcoholic fatty liver disease (NAFLD) to nonalcoholic steatohepatitis (NASH) is linked to systemic inflammation. Currently, two of the aspects that need further investigation are diagnosis and treatment of NASH. In this sense, the aim of this study was to assess the relationship between circulating levels of cytokines, hepatic expression of toll-like receptors (TLRs), and degrees of NAFLD, and to investigate whether these levels could serve as noninvasive biomarkers of NASH. The present study assessed plasma levels of cytokines in 29 normal-weight women and 82 women with morbid obesity (MO) (subclassified: normal liver (n = 29), simple steatosis (n = 32), and NASH (n = 21)). We used enzyme-linked immunosorbent assays (ELISAs) to quantify cytokine and TLR4 levels and RTqPCR to assess TLRs hepatic expression. IL-1β, IL-8, IL-10, TNF-α, tPAI-1, and MCP-1 levels were increased, and adiponectin levels were decreased in women with MO. IL-8 was significantly higher in MO with NASH than in NL. To sum up, high levels of IL-8 were associated with the diagnosis of NASH in a cohort of women with morbid obesity. Moreover, a positive correlation between TLR2 hepatic expression and IL-8 circulating levels was found. Full article
(This article belongs to the Special Issue Medicines for the Treatment of Obesity)
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14 pages, 2544 KiB  
Article
Gomisin N from Schisandra chinensis Ameliorates Lipid Accumulation and Induces a Brown Fat-Like Phenotype through AMP-Activated Protein Kinase in 3T3-L1 Adipocytes
by Kippeum Lee, Yeon-Joo Lee, Kui-Jin Kim, Sungwoo Chei, Heegu Jin, Hyun-Ji Oh and Boo-Yong Lee
Int. J. Mol. Sci. 2020, 21(6), 2153; https://doi.org/10.3390/ijms21062153 - 20 Mar 2020
Cited by 18 | Viewed by 5165
Abstract
Obesity results from an imbalance between energy intake and energy expenditure, in which excess fat is stored as triglycerides (TGs) in white adipocytes. Recent studies have explored the anti-obesity effects of certain edible phytochemicals, which suppress TG accumulation and stimulate a brown adipocyte-like [...] Read more.
Obesity results from an imbalance between energy intake and energy expenditure, in which excess fat is stored as triglycerides (TGs) in white adipocytes. Recent studies have explored the anti-obesity effects of certain edible phytochemicals, which suppress TG accumulation and stimulate a brown adipocyte-like phenotype in white adipocytes. Gomisin N (GN) is an important bioactive component of Schisandra chinensis, a woody plant endemic to Asia. GN has antioxidant, anti-inflammatory and hepatoprotective effects in vivo and in vitro. However, the anti-obesity effects of GN in lipid metabolism and adipocyte browning have not yet been investigated. In the present study, we aimed to determine whether GN suppresses lipid accumulation and regulates energy metabolism, potentially via AMP-activated protein kinase (AMPK), in 3T3-L1 adipocytes. Our findings demonstrate that GN inhibited adipogenesis and lipogenesis in adipocyte differentiation. Also, GN not only increased the expression of thermogenic factors, including uncoupling protein 1 (UCP1), but also enhanced fatty acid oxidation (FAO) in 3T3-L1 cells. Therefore, GN may have a therapeutic benefit as a promising natural agent to combat obesity. Full article
(This article belongs to the Special Issue Medicines for the Treatment of Obesity)
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13 pages, 2356 KiB  
Article
Ergosterol Peroxide from the Medicinal Mushroom Ganoderma lucidum Inhibits Differentiation and Lipid Accumulation of 3T3-L1 Adipocytes
by Yong-Un Jeong and Young-Jin Park
Int. J. Mol. Sci. 2020, 21(2), 460; https://doi.org/10.3390/ijms21020460 - 10 Jan 2020
Cited by 51 | Viewed by 6517
Abstract
Ergosterol peroxide is a natural compound of the steroid family found in many fungi, and it possesses antioxidant, anti-inflammatory, anticancer and antiviral activities. The anti-obesity activity of several edible and medicinal mushrooms has been reported, but the effect of mushroom-derived ergosterol peroxide on [...] Read more.
Ergosterol peroxide is a natural compound of the steroid family found in many fungi, and it possesses antioxidant, anti-inflammatory, anticancer and antiviral activities. The anti-obesity activity of several edible and medicinal mushrooms has been reported, but the effect of mushroom-derived ergosterol peroxide on obesity has not been studied. Therefore, we analyzed the effect of ergosterol peroxide on the inhibition of triglyceride synthesis at protein and mRNA levels and differentiation of 3T3-L1 adipocytes. Ergosterol peroxide inhibited lipid droplet synthesis of differentiated 3T3-L1 cells, expression of peroxisome proliferator-activated receptor gamma (PPARγ) and CCAT/enhancer-binding protein alpha (C/EBPα), the major transcription factors of differentiation, and also the expression of sterol regulatory element-binding protein-1c (SREBP-1c), which promotes the activity of PPARγ, resulting in inhibition of differentiation. It further inhibited the expression of fatty acid synthase (FAS), fatty acid translocase (FAT), and acetyl-coenzyme A carboxylase (ACC), which are lipogenic factors. In addition, it inhibited the phosphorylation of mitogen-activated protein kinases (MAPKs) involved in cell proliferation and activation of early differentiation transcription factors in the mitotic clonal expansion (MCE) stage. As a result, ergosterol peroxide significantly inhibited the synthesis of triglycerides and differentiation of 3T3-L1 cells, and is, therefore, a possibile prophylactic and therapeutic agent for obesity and related metabolic diseases. Full article
(This article belongs to the Special Issue Medicines for the Treatment of Obesity)
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Review

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28 pages, 748 KiB  
Review
Induction of Adipose Tissue Browning as a Strategy to Combat Obesity
by Alina Kuryłowicz and Monika Puzianowska-Kuźnicka
Int. J. Mol. Sci. 2020, 21(17), 6241; https://doi.org/10.3390/ijms21176241 - 28 Aug 2020
Cited by 138 | Viewed by 10988
Abstract
The ongoing obesity pandemic generates a constant need to develop new therapeutic strategies to restore the energy balance. Therefore, the concept of activating brown adipose tissue (BAT) in order to increase energy expenditure has been revived. In mammals, two developmentally distinct types of [...] Read more.
The ongoing obesity pandemic generates a constant need to develop new therapeutic strategies to restore the energy balance. Therefore, the concept of activating brown adipose tissue (BAT) in order to increase energy expenditure has been revived. In mammals, two developmentally distinct types of brown adipocytes exist; the classical or constitutive BAT that arises during embryogenesis, and the beige adipose tissue that is recruited postnatally within white adipose tissue (WAT) in the process called browning. Research of recent years has significantly increased our understanding of the mechanisms involved in BAT activation and WAT browning. They also allowed for the identification of critical molecules and critical steps of both processes and, therefore, many new therapeutic targets. Several non-pharmacological approaches, as well as chemical compounds aiming at the induction of WAT browning and BAT activation, have been tested in vitro as well as in animal models of genetically determined and/or diet-induced obesity. The therapeutic potential of some of these strategies has also been tested in humans. In this review, we summarize present concepts regarding potential therapeutic targets in the process of BAT activation and WAT browning and available strategies aiming at them. Full article
(This article belongs to the Special Issue Medicines for the Treatment of Obesity)
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