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Pharmaceuticals
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Drug Candidates for the Treatment of Obesity, 2nd Edition
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Drug Candidates for the Treatment of Obesity, 2nd Edition

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

Deadline for manuscript submissions: 25 August 2025 | Viewed by 5893

Special Issue Editors

Dr. Maria Isabel Cardoso Alonso-Vale

E-Mail Website
Guest Editor
Department of Biological Sciences, Institute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of Sao Paulo (UNIFESP), Sao Paulo, Brazil
Interests: adipose tissue; obesity; inflammation; fatty acids; mesenchymal stromal cells
Special Issues, Collections and Topics in MDPI journals
Dr. Monica Marques Telles

E-Mail Website
Guest Editor
Department of Physiology/Nutrition Physiology Division, Federal University of Sao Paulo (UNIFESP), Sao Paulo, Brazil
Interests: nutraceuticals; obesity; adipose tissue; metabolism; central control of food intake
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

According to the WHO, overweight and obesity have reached an epidemic proportion. It is estimated that one billion people globally will be living with obesity by 2030. This is particularly worrying when considering obesity-related metabolic risks, predisposing people to type 2 diabetes mellitus, cardiovascular diseases, and some types of cancer, among other pathological conditions. Furthermore, overweight and obesity might impair psychological health and self-esteem, occasionally resulting in anxiety and/or depression. On one hand, it is well recognized that dietary control and physical activity programs are the most effective interventions in order to manage obesity and its related disorders. On the other hand, it is also well known that adherence to the recommended lifestyle modifications is poor. In addition, the pharmacological management of obesity has often been ineffective or associated with important side effects, thus representing an enormous challenge to healthcare professionals. Despite all of the harmful health impacts for individuals with obesity, the high costs to treat obesity and its related disorders are also a matter of concern, and, thus, the development of new pharmacological therapies for overweight and obesity control has been addressed. Therefore, this Special Issue is focused on new drug candidates for the prevention and treatment of obesity.

Dr. Maria Isabel Cardoso Alonso-Vale
Dr. Monica Marques Telles
Guest Editors

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. 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

  • obesity
  • appetite supressors
  • nutraceuticals
  • plant extracts
  • lipid metabolism
  • high-fat diet
  • adipogenesis

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Published Papers (3 papers)

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Research

14 pages, 6750 KiB  
Article
Lycopene and Garcinia cambogia Induce White-to-Brown Adipose Differentiation: An Innovative Strategy to Curb Obesity
by Federica Mannino, Vincenzo Arcoraci, Giovanna Vermiglio, Davide Labellarte, Igor Pirrotta, Domenico Antonio Giorgi, Alessandro Scarfone, Alessandra Bitto, Letteria Minutoli, Mario Vaccaro, Mariarosaria Galeano, Giovanni Pallio and Natasha Irrera
Pharmaceuticals 2024, 17(8), 986; https://doi.org/10.3390/ph17080986 - 25 Jul 2024
Cited by 1 | Viewed by 1576
Abstract
Obesity is considered one of the main risk factors for cardiovascular diseases. The browning process has been recently recognized as a promising anti-obesity therapy. Lycopene (LYC) and Garcinia cambogia fruit extract (GE) might be important resources for anti-obesity drugs; therefore, the aim of [...] Read more.
Obesity is considered one of the main risk factors for cardiovascular diseases. The browning process has been recently recognized as a promising anti-obesity therapy. Lycopene (LYC) and Garcinia cambogia fruit extract (GE) might be important resources for anti-obesity drugs; therefore, the aim of this study was to investigate the anti-obesity effects of LYC and GE on 3T3-L1 adipocytes and Zucker rats. Mouse 3T3-L1 pre-adipocytes were differentiated in mature adipocytes and then treated with LYC (0.5 μM), GE (30 mg/mL) or LYC + GE for 24 h. Moreover, male Zucker Crl:ZUC-Leprfa rats were randomly assigned to 5 groups of 10 animals to orally receive Vehicle (Ctrl), Orlistat (20 mg/kg), LYC (5 mg/kg), GE (1000 mg/kg) or LYC + GE for 28 days. LYC, GC extracts and even more LYC + GE stimulated the mRNA and protein expression of thermogenic genes UCP1, CIDEA and DIO2, significantly reduced lipid droplet size and increased lipid droplet number in adipocytes. UCP1 mRNA and protein expression was also increased in the visceral adipose tissue of the rats that received the dietary intake of LYC, GE and even more LYC + GE. Moreover, LYC + GE induced the reorganization of visceral fat depots that showed a great number of small adipocytes and a significant reduction in weight gain and food intake compared to the control group. The obtained results demonstrated that LYC + GE might be used as new approaches for obesity management in order to induce the browning process and achieve a metabolically active tissue instead of a tissue characterized by lipid depot accumulation. Full article
(This article belongs to the Special Issue Drug Candidates for the Treatment of Obesity, 2nd Edition)
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21 pages, 1605 KiB  
Article
Fish Oil Supplementation Mitigates High-Fat Diet-Induced Obesity: Exploring Epigenetic Modulation and Genes Associated with Adipose Tissue Dysfunction in Mice
by Jussara de Jesus Simão, Andressa França de Sousa Bispo, Victor Tadeu Gonçalves Plata, Lucia Maria Armelin-Correa and Maria Isabel Cardoso Alonso-Vale
Pharmaceuticals 2024, 17(7), 861; https://doi.org/10.3390/ph17070861 - 1 Jul 2024
Cited by 4 | Viewed by 1699
Abstract
This study investigated the effects of fish oil (FO) treatment, particularly enriched with eicosapentaenoic acid (EPA), on obesity induced by a high-fat diet (HFD) in mice. The investigation focused on elucidating the impact of FO on epigenetic modifications in white adipose tissue (WAT) [...] Read more.
This study investigated the effects of fish oil (FO) treatment, particularly enriched with eicosapentaenoic acid (EPA), on obesity induced by a high-fat diet (HFD) in mice. The investigation focused on elucidating the impact of FO on epigenetic modifications in white adipose tissue (WAT) and the involvement of adipose-derived stem cells (ASCs). C57BL/6j mice were divided into two groups: control diet and HFD for 16 weeks. In the last 8 weeks, the HFD group was subdivided into HFD and HFD + FO (treated with FO). WAT was removed for RNA and protein extraction, while ASCs were isolated, cultured, and treated with leptin. All samples were analyzed using functional genomics tools, including PCR-array, RT-PCR, and Western Blot assays. Mice receiving an HFD displayed increased body mass, fat accumulation, and altered gene expression associated with WAT inflammation and dysfunction. FO supplementation attenuated these effects, a potential protective role against HFD-induced obesity. Analysis of H3K27 revealed HFD-induced changes in histone, which were partially reversed by FO treatment. This study further explored leptin signaling in ASCs, suggesting a potential mechanism for ASC dysfunction in the obesity-rich leptin environment of WAT. Overall, FO supplementation demonstrated efficacy in mitigating HFD-induced obesity, influencing epigenetic and molecular pathways, and shedding light on the role of ASCs and leptin signaling in WAT dysfunction associated with obesity. Full article
(This article belongs to the Special Issue Drug Candidates for the Treatment of Obesity, 2nd Edition)
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14 pages, 1534 KiB  
Article
Dynamic Changes in Adiponectin and Resistin Drive Remission of Cardiometabolic Risk Biomarkers in Individuals with Obesity Following Bariatric Surgery
by Amanda Machado Fiorotti, Amanda Cristina Araújo Gomes, Amanda Motta Bortoli, Beatriz Bobbio de Brito, Karolini Zuqui Nunes, Fabiano Kenji Haraguchi and Andressa Bolsoni-Lopes
Pharmaceuticals 2024, 17(2), 215; https://doi.org/10.3390/ph17020215 - 7 Feb 2024
Cited by 2 | Viewed by 2037
Abstract
The remission of obesity-related diseases following bariatric surgery appears to result from the reorganization of metabolic and hormonal pathways involving adipokines. This study aimed to investigate the relationship between changes in body adiposity and serum adipokine levels, as well as the association between [...] Read more.
The remission of obesity-related diseases following bariatric surgery appears to result from the reorganization of metabolic and hormonal pathways involving adipokines. This study aimed to investigate the relationship between changes in body adiposity and serum adipokine levels, as well as the association between variations in adiponectin or resistin levels and cardiometabolic risk blood biomarkers before and after Roux-en-Y gastric bypass. A longitudinal and prospective study was conducted with bariatric surgery patients. Anthropometric, body composition and blood biochemical parameters were measured before and at 2 and 6 months post-surgery. The data were analyzed using ANOVA, Pearson or Spearman correlation, and simple linear regression with a significance level of p < 0.05. Among 36 mostly female patients aged 30 to 39 years, significant reductions in body weight (−26.8%), fat mass (−50%), waist circumference (−18%) and waist-to-height ratio (−22%) were observed post-surgery. Serum adiponectin levels increased (+107%), while resistin (−12.2%), TNF-α (−35%), and PAI-1 (−11.1%) decreased. Glucose, insulin, CRP, cholesterol, LDL-c, triglycerides, and vitamin D also decreased. Waist circumference variation showed a positive correlation with PAI-1 and TNF-α and a negative correlation with adiponectin. The total fat mass showed a positive correlation with PAI-1. Adiponectin variation correlated negatively with glucose, resistin, and CRP but positively with HDL-c. Resistin showed a positive correlation with insulin and CRP. In conclusion, 6 months post-bariatric surgery, reducing abdominal adiposity had a more significant impact on serum adipokine levels than total fat mass. Adiponectin increase and resistin decrease acted as endocrine mediators driving the remission of cardiometabolic risk biomarkers in individuals with obesity following Roux-en-Y gastric bypass. Full article
(This article belongs to the Special Issue Drug Candidates for the Treatment of Obesity, 2nd Edition)
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