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Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (30 December 2021) | Viewed by 48688

Special Issue Editors

Prof. Dr. Marianna Lauricella

E-Mail Website
Guest Editor
Section of Biochemistry, Department of Biomedicine, Neurosciences and Advanced Diagnostics (BIND), University of Palermo, 90127 Palermo, Italy
Interests: mechanisms of oxidative stress induction and main antioxidant systems; biochemical pathways of cell death and survival (apoptosis, necrosis, autophagy) in tumor cells; effects of phytocompounds in obesity reduction
Special Issues, Collections and Topics in MDPI journals
Dr. Antonella D'Anneo

E-Mail Website
Guest Editor
Laboratory of Biochemistry, Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, 90127 Palermo, Italy
Interests: biochemical pathways in cancer cell death (apoptosis, necrosis, necroptosis, autophagy and anoikis); nutrition and human diseases; oxidative stress; signal transduction; targeted therapies; cancer stem-like cells; analysis of the behaviours of phytocompounds in obesity treatment
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Obesity is a serious worldwide health concern responsible for a high incidence of mortality and morbidity. Many drivers have been identified for its etiopathogenesis, such as an imbalance between energy intake and its expenditure, resulting from a combination of excessive food intake, sedentary lifestyle, reduced physical activity and genetic predisposition. In addition, environmental chemicals such as pesticides, organotins and phthalates have also shown a decisive role in promoting obesity. These obesogens represent risk factors during fetal development, predisposing or programming the offspring to gain weight.Adipose tissue exerts an active metabolic role in regulating energy storage and its utilization. In addition, it may be considered an endocrine organ since it produces and secretes multiple immune-modulatory proteins, known as adipokines. Through adipokines, the adipose tissue regulates several important physiological functions, including insulin sensitivity and secretion, glucose and lipid metabolism, blood pressure and the function of the immune system. Adipokines can be classified into molecules with a pro-inflammatory or anti-inflammatory profile. An unbalanced production of adipokines with a pro-inflammatory role in adipose tissue induces low-grade systemic inflammation in obese patients, which predisposes to insulin resistance, type II diabetes, non-alcoholic fatty liver disease and cardiovascular disorders and cancer. Therefore, the reduction of adipose tissue in the obese subjects represents an important goal for the prevention and treatment of these chronic diseases.Nowadays, there has been a growing interest in finding novel targeted compounds, both natural and synthetic, with potential action against obesity. Investigating the effects of these compounds in reducing obesity and preventing the associated diseases could provide novel insights.We are inviting investigators to contribute either original research or review articles focusing on the pathophysiology of obesity as well as on the identification of compounds capable of managing an obesity profile and disease-related conditions.

Dr. Marianna Lauricella
Dr. Antonella D'Anneo
Guest Editors

Manuscript Submission Information

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Keywords

  • Obesity
  • Adipokines
  • Obesogens
  • Genetic predisposition
  • Natural/synthetic compounds
  • Cardiovascular disorders
  • Type II diabetes
  • Non-alcoholic fatty liver disease
  • Cancer

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Published Papers (9 papers)

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Editorial

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5 pages, 209 KiB  
Editorial
Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity
by Antonella D’Anneo and Marianna Lauricella
Int. J. Mol. Sci. 2022, 23(5), 2890; https://doi.org/10.3390/ijms23052890 - 7 Mar 2022
Cited by 4 | Viewed by 2008
Abstract
For a long time, adipose tissue has been considered an inert tissue involved in fat accumulation [...] Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)

Research

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15 pages, 2220 KiB  
Article
Inhibitory Effects of Pinostilbene on Adipogenesis in 3T3-L1 Adipocytes: A Study of Possible Mechanisms
by You Chul Chung and Chang-Gu Hyun
Int. J. Mol. Sci. 2021, 22(24), 13446; https://doi.org/10.3390/ijms222413446 - 14 Dec 2021
Cited by 16 | Viewed by 4166
Abstract
Resveratrol is a phytoalexin with multiple bioactive properties, including antioxidative, neuroprotective, cardioprotective, and anticancer effects. However, resveratrol exhibits structural instability in response to UV irradiation, alkaline pH, and oxygen exposure. Thus, resveratrol derivatives have attracted considerable research interest. In this study, we aimed [...] Read more.
Resveratrol is a phytoalexin with multiple bioactive properties, including antioxidative, neuroprotective, cardioprotective, and anticancer effects. However, resveratrol exhibits structural instability in response to UV irradiation, alkaline pH, and oxygen exposure. Thus, resveratrol derivatives have attracted considerable research interest. In this study, we aimed to evaluate the anti-adipogenic effects of pinostilbene hydrate (PH), a methylated resveratrol derivative, in 3T3-L1 cells. We also evaluated the mechanisms underlying the effects of PH on adipogenesis in 3T3-L1 adipocytes. Oil Red O staining, lipid accumulation assay, and triglyceride (TG) content assay revealed that PH significantly inhibited lipid and TG accumulation without cytotoxicity. In addition, we determined that PH decreased the expression of adipogenesis-related transcription factors, such as PPARγ, C/EBPα, SREBP-1c, and FABP4, and the phosphorylation of MAPK and protein kinase B (AKT). Moreover, PH attenuated the expression of CREB and C/EBPβ, while increasing the phosphorylation of AMPK and ACC, and decreasing the expression of fatty acid synthase and FABP4. Based on these results, we suggest that PH suppresses adipogenesis in 3T3-L1 cells via the activation of the AMPK signaling pathway and the inhibition of the MAPK and AKT insulin-dependent signaling pathways. Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)
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11 pages, 2104 KiB  
Article
Metformin Attenuates Postinfarction Myocardial Fibrosis and Inflammation in Mice
by Halyna Loi, Solomiia Kramar, Charlotte Laborde, Dimitri Marsal, Nathalie Pizzinat, Daniel Cussac, Jerome Roncalli, Frederic Boal, Helene Tronchere, Oleksandra Oleshchuk, Mykhaylo Korda and Oksana Kunduzova
Int. J. Mol. Sci. 2021, 22(17), 9393; https://doi.org/10.3390/ijms22179393 - 30 Aug 2021
Cited by 19 | Viewed by 3627
Abstract
Diabetes is a major risk factor for the development of cardiovascular disease with a higher incidence of myocardial infarction. This study explores the role of metformin, a first-line antihyperglycemic agent, in postinfarction fibrotic and inflammatory remodeling in mice. Three-month-old C57BI/6J mice were submitted [...] Read more.
Diabetes is a major risk factor for the development of cardiovascular disease with a higher incidence of myocardial infarction. This study explores the role of metformin, a first-line antihyperglycemic agent, in postinfarction fibrotic and inflammatory remodeling in mice. Three-month-old C57BI/6J mice were submitted to 30 min cardiac ischemia followed by reperfusion for 14 days. Intraperitoneal treatment with metformin (5 mg/kg) was initiated 15 min after the onset of reperfusion and maintained for 14 days. Real-time PCR was used to determine the levels of COL3A1, αSMA, CD68, TNF-α and IL-6. Increased collagen deposition and infiltration of macrophages in heart tissues are associated with upregulation of the inflammation-associated genes in mice after 14 days of reperfusion. Metformin treatment markedly reduced postinfarction fibrotic remodeling and CD68-positive cell population in mice. Moreover, metformin resulted in reduced expression of COL3A1, αSMA and CD68 after 14 days of reperfusion. Taken together, these results open new perspectives for the use of metformin as a drug that counteracts adverse myocardial fibroticand inflammatory remodeling after MI. Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)
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12 pages, 1738 KiB  
Article
Metformin and Vitamin D Modulate Inflammation and Autophagy during Adipose-Derived Stem Cell Differentiation
by Sara Cruciani, Giuseppe Garroni, Renzo Pala, Maria Laura Cossu, Giorgio Carlo Ginesu, Carlo Ventura and Margherita Maioli
Int. J. Mol. Sci. 2021, 22(13), 6686; https://doi.org/10.3390/ijms22136686 - 22 Jun 2021
Cited by 15 | Viewed by 3178
Abstract
Adipose-derived stem cells (ADSCs) came out from the regenerative medicine landscape for their ability to differentiate into several phenotypes, contributing to tissue regeneration both in vitro and in vivo. Dysregulation in stem cell recruitment and differentiation during adipogenesis is linked to a chronic [...] Read more.
Adipose-derived stem cells (ADSCs) came out from the regenerative medicine landscape for their ability to differentiate into several phenotypes, contributing to tissue regeneration both in vitro and in vivo. Dysregulation in stem cell recruitment and differentiation during adipogenesis is linked to a chronic low-grade inflammation and macrophage infiltration inside the adipose tissue, insulin resistance, cardiovascular disease and obesity. In the present paper we aimed to evaluate the role of metformin and vitamin D, alone or in combination, in modulating inflammation and autophagy in ADSCs during adipogenic commitment. ADSCs were cultured for 21 days in the presence of a specific adipogenic differentiation medium, together with metformin, or vitamin D, or both. We then analyzed the expression of FoxO1 and Heat Shock Proteins (HSP) and the secretion of proinflammatory cytokines IL-6 and TNF-α by ELISA. Autophagy was also assessed by specific Western blot analysis of ATG12, LC3B I, and LC3B II expression. Our results showed the ability of the conditioned media to modulate adipogenic differentiation, finely tuning the inflammatory response and autophagy. We observed a modulation in HSP mRNA levels, and a significant downregulation in cytokine secretion. Taken together, our findings suggest the possible application of these molecules in clinical practice to counteract uncontrolled lipogenesis and prevent obesity and obesity-related metabolic disorders. Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)
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Review

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27 pages, 3282 KiB  
Review
The Potential to Fight Obesity with Adipogenesis Modulating Compounds
by Jiaqi Zhao, Ailin Zhou and Wei Qi
Int. J. Mol. Sci. 2022, 23(4), 2299; https://doi.org/10.3390/ijms23042299 - 19 Feb 2022
Cited by 26 | Viewed by 8733
Abstract
Obesity is an increasingly severe public health problem, which brings huge social and economic burdens. Increased body adiposity in obesity is not only tightly associated with type 2 diabetes, but also significantly increases the risks of other chronic diseases including cardiovascular diseases, fatty [...] Read more.
Obesity is an increasingly severe public health problem, which brings huge social and economic burdens. Increased body adiposity in obesity is not only tightly associated with type 2 diabetes, but also significantly increases the risks of other chronic diseases including cardiovascular diseases, fatty liver diseases and cancers. Adipogenesis describes the process of the differentiation and maturation of adipocytes, which accumulate in distributed adipose tissue at various sites in the body. The major functions of white adipocytes are to store energy as fat during periods when energy intake exceeds expenditure and to mobilize this stored fuel when energy expenditure exceeds intake. Brown/beige adipocytes contribute to non-shivering thermogenesis upon cold exposure and adrenergic stimulation, and thereby promote energy consumption. The imbalance of energy intake and expenditure causes obesity. Recent interest in epigenetics and signaling pathways has utilized small molecule tools aimed at modifying obesity-specific gene expression. In this review, we discuss compounds with adipogenesis-related signaling pathways and epigenetic modulating properties that have been identified as potential therapeutic agents which cast some light on the future treatment of obesity. Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)
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22 pages, 837 KiB  
Review
Skeletal Muscle Microvascular Dysfunction in Obesity-Related Insulin Resistance: Pathophysiological Mechanisms and Therapeutic Perspectives
by Chiedozie Kenneth Ugwoke, Erika Cvetko and Nejc Umek
Int. J. Mol. Sci. 2022, 23(2), 847; https://doi.org/10.3390/ijms23020847 - 13 Jan 2022
Cited by 16 | Viewed by 4151
Abstract
Obesity is a worrisomely escalating public health problem globally and one of the leading causes of morbidity and mortality from noncommunicable disease. The epidemiological link between obesity and a broad spectrum of cardiometabolic disorders has been well documented; however, the underlying pathophysiological mechanisms [...] Read more.
Obesity is a worrisomely escalating public health problem globally and one of the leading causes of morbidity and mortality from noncommunicable disease. The epidemiological link between obesity and a broad spectrum of cardiometabolic disorders has been well documented; however, the underlying pathophysiological mechanisms are only partially understood, and effective treatment options remain scarce. Given its critical role in glucose metabolism, skeletal muscle has increasingly become a focus of attention in understanding the mechanisms of impaired insulin function in obesity and the associated metabolic sequelae. We examined the current evidence on the relationship between microvascular dysfunction and insulin resistance in obesity. A growing body of evidence suggest an intimate and reciprocal relationship between skeletal muscle microvascular and glucometabolic physiology. The obesity phenotype is characterized by structural and functional changes in the skeletal muscle microcirculation which contribute to insulin dysfunction and disturbed glucose homeostasis. Several interconnected etiologic molecular mechanisms have been suggested, including endothelial dysfunction by several factors, extracellular matrix remodelling, and induction of oxidative stress and the immunoinflammatory phenotype. We further correlated currently available pharmacological agents that have deductive therapeutic relevance to the explored pathophysiological mechanisms, highlighting a potential clinical perspective in obesity treatment. Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)
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23 pages, 1444 KiB  
Review
Curcumin and Weight Loss: Does It Work?
by Kamila Kasprzak-Drozd, Tomasz Oniszczuk, Marek Gancarz, Adrianna Kondracka, Robert Rusinek and Anna Oniszczuk
Int. J. Mol. Sci. 2022, 23(2), 639; https://doi.org/10.3390/ijms23020639 - 7 Jan 2022
Cited by 40 | Viewed by 10123
Abstract
Obesity is a global health problem needing urgent research. Synthetic anti-obesity drugs show side effects and variable effectiveness. Thus, there is a tendency to use natural compounds for the management of obesity. There is a considerable body of knowledge, supported by rigorous experimental [...] Read more.
Obesity is a global health problem needing urgent research. Synthetic anti-obesity drugs show side effects and variable effectiveness. Thus, there is a tendency to use natural compounds for the management of obesity. There is a considerable body of knowledge, supported by rigorous experimental data, that natural polyphenols, including curcumin, can be an effective and safer alternative for managing obesity. Curcumin is a is an important compound present in Curcuma longa L. rhizome. It is a lipophilic molecule that rapidly permeates cell membrane. Curcumin has been used as a pharmacological traditional medicinal agent in Ayurvedic medicine for ∼6000 years. This plant metabolite doubtless effectiveness has been reported through increasingly detailed in vitro, in vivo and clinical trials. Regarding its biological effects, multiple health-promoting, disease-preventing and even treatment attributes have been remarkably highlighted. This review documents the status of research on anti-obesity mechanisms and evaluates the effectiveness of curcumin for management of obesity. It summarizes different mechanisms of anti-obesity action, associated with the enzymes, energy expenditure, adipocyte differentiation, lipid metabolism, gut microbiota and anti-inflammatory potential of curcumin. However, there is still a need for systematic and targeted clinical studies before curcumin can be used as the mainstream therapy for managing obesity. Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)
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21 pages, 881 KiB  
Review
The Beneficial Effects of Essential Oils in Anti-Obesity Treatment
by Anna De Blasio, Antonella D’Anneo, Marianna Lauricella, Sonia Emanuele, Michela Giuliano, Giovanni Pratelli, Giuseppe Calvaruso and Daniela Carlisi
Int. J. Mol. Sci. 2021, 22(21), 11832; https://doi.org/10.3390/ijms222111832 - 31 Oct 2021
Cited by 24 | Viewed by 8171
Abstract
Obesity is a complex disease caused by an excessive amount of body fat. Obesity is a medical problem and represents an important risk factor for the development of serious diseases such as insulin resistance, type 2 diabetes, cardiovascular disease, and some types of [...] Read more.
Obesity is a complex disease caused by an excessive amount of body fat. Obesity is a medical problem and represents an important risk factor for the development of serious diseases such as insulin resistance, type 2 diabetes, cardiovascular disease, and some types of cancer. Not to be overlooked are the psychological issues that, in obese subjects, turn into very serious pathologies, such as depression, phobias, anxiety, and lack of self-esteem. In addition to modifying one’s lifestyle, the reduction of body mass can be promoted by different natural compounds such as essential oils (EOs). EOs are mixtures of aromatic substances produced by many plants, particularly in medicinal and aromatic ones. They are odorous and volatile and contain a mixture of terpenes, alcohols, aldehydes, ketones, and esters. Thanks to the characteristics of the various chemical components present in them, EOs are used in the food, cosmetic, and pharmaceutical fields. Indeed, it has been shown that EOs possess great antibiotic, anti-inflammatory, and antitumor powers. Emerging results also demonstrate the anti-obesity effects of EOs. We have examined the main data obtained in experimental studies and, in this review, we summarize the effect of EOs in obesity and obesity-related metabolic diseases. Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)
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14 pages, 654 KiB  
Review
Salivary Adipokine and Cytokine Levels as Potential Markers for the Development of Obesity and Metabolic Disorders
by Beata Zyśk, Lucyna Ostrowska and Joanna Smarkusz-Zarzecka
Int. J. Mol. Sci. 2021, 22(21), 11703; https://doi.org/10.3390/ijms222111703 - 28 Oct 2021
Cited by 11 | Viewed by 2911
Abstract
Currently, the number of people suffering from obesity is increasing worldwide. In addition, the disease is affecting younger individuals. Therefore, it is essential to search for new diagnostic methods and markers for early assessment of the risk of obesity, metabolic disorders, and other [...] Read more.
Currently, the number of people suffering from obesity is increasing worldwide. In addition, the disease is affecting younger individuals. Therefore, it is essential to search for new diagnostic methods and markers for early assessment of the risk of obesity, metabolic disorders, and other comorbidities. The discovery of the secretory function of adipose tissue and coexistence of low-grade chronic inflammation with obesity set a new direction in this disease diagnosis using the assessment of the concentration of inflammatory markers secreted by adipose tissue. The aim of this review was to determine, based on previous findings, whether saliva can be useful in the diagnosis of obesity and its early metabolic complications and whether it can be an alternative diagnostic material to serum. Full article
(This article belongs to the Special Issue Natural and Synthetic Compounds for Management, Prevention and Treatment of Obesity)
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