Natural Products for the Treatment of Obesity

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

Deadline for manuscript submissions: closed (20 February 2024) | Viewed by 10484

Special Issue Editors


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Guest Editor
1. Institute for Obesity Research, Tecnologico de Monterrey, Monterrey 64849, Mexico
2. Department of Bioengineering, School of Engineering & Sciences, Tecnologico de Monterrey, Puebla 72453, Mexico
Interests: plant based proteins; bioactive peptides; natural pigments; anthocyanins; obesity photo
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Guest Editor
Tecnología Alimentaria, Centro de Investigación y Asistencia en Tecnología y Diseño del Estado de Jalisco, A. C., CIATEJ, Unidad Zapopan, Camino Arenero 1227, El Bajío, Zapopan 45019, Mexico
Interests: obesity; polyphenols; novel food ingredients; alternative proteins

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Guest Editor
The Institute for Obesity Research, Tecnológico de Monterrey, Av. Eugenio Garza Sada 2501 Sur, Monterrey 64849, Mexico
Interests: obesity; dyslipidemia; bioactive compounds; polyphenols

Special Issue Information

Dear Colleagues,

Changes in dietary habits, especially in the consumption of high-fat, high-sugar and high-salt foods, have increased the prevalence of several health conditions, including obesity. According to the World Health Organization, obesity has nearly tripled since 1975; in 2016, more than 1.9 billion adults were overweight, and over 650 million of this number were obese. Additionally, 39 million children under the age of 5 were overweight or obese in 2020. Physiologically, obesity is defined as an abnormal accumulation of adipose tissue within the body that carries out a subclinical chronic state of inflammation. This condition is known to be closely related to the onset of comorbidities, including insulin resistance, diabetes, hypertension, dyslipidemia, etc. The growing association between plant-derived food and its effect in reducing the risk of noncommunicable diseases has opened doors for wide range of research focused on the chemical characterization of natural compounds and their potential health benefits. Anti-obesity natural compounds have been reported, including those extracted from plants (polyphenols, alkaloids, nortriterpen quinones, carotenoids, bioactive peptides, etc.), products from microbial sources (lipstatin, gut microbiota, probiotic bacteria), and compounds from marine organisms (polyacetylenic acids, sesquiterpene quinones, dihydroxyanthraquinones, etc). However, there is still a need to address important aspects of the use of natural compounds in obesity, for instance, chemical characterization and stabilization, effective dosing, mechanisms of action, etc.

This Special Issue invites both reviews and original articles that elucidate recent research progress in natural products that serve as drug candidates or adjuvants in the treatment of obesity. Topics include but are not limited to natural products and obesity-related comorbidities, chemical characterization, anti-obesity mechanisms of action in natural products, chemical characterizations, the pre-clinical and clinical evaluation of natural compounds in obesity, and functional food development incorporating anti-obesity natural compounds. A collection of high-quality manuscripts on these topics will be published in this Special Issue of Pharmaceuticals.

Dr. Diego A. Luna-Vital
Dr. Luis Mojica
Dr. Astrid Domínguez-Uscanga
Guest Editors

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Keywords

  • natural compounds
  • obesity
  • polyphenols
  • molecular nutrition
  • metabolic diseases
  • inflammation

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Published Papers (5 papers)

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Research

17 pages, 2750 KiB  
Article
Efficacy of Probiotic Strains Lactobacillus sakei Probio65 and Lactobacillus plantarum Probio-093 in Management of Obesity: An In Vitro and In Vivo Analysis
by Aneela Gulnaz, Lee-Ching Lew, Yong-Ha Park, Jamal S. M. Sabir, Raed Albiheyri, Irfan A. Rather and Yan-Yan Hor
Pharmaceuticals 2024, 17(6), 676; https://doi.org/10.3390/ph17060676 - 24 May 2024
Viewed by 1584
Abstract
The prevalence of obesity, characterized by an excessive accumulation of adipose tissue and adipocyte hypertrophy, presents a major public health challenge. This study investigates the therapeutic potential of two probiotic strains, Lactobacillus sakei Probio65 and Lactobacillus plantarum Probio-093, in the context of obesity. [...] Read more.
The prevalence of obesity, characterized by an excessive accumulation of adipose tissue and adipocyte hypertrophy, presents a major public health challenge. This study investigates the therapeutic potential of two probiotic strains, Lactobacillus sakei Probio65 and Lactobacillus plantarum Probio-093, in the context of obesity. Utilizing 3T3-L1 cell-derived human adipocytes, we assessed Probio65’s and Probio-093’s capacity to mitigate triglyceride accumulation and influence adipocytokine production in vitro. Subsequently, an in vivo trial with male C57BL/6J mice examined the effects of both probiotic strains on adipose tissue characteristics, body weight, fat mass, and obesity-related gene expression. This study employed both live and ethanol-extracted bacterial cells. The results demonstrated significant reductions in the triglyceride deposition, body weight, and adipose tissue mass in the treated groups (p < 0.05). Furthermore, both strains modulated adipokine profiles by downregulating proinflammatory markers such as PAI-1, leptin, TNF-α, STAMP2, F4/80, resistin, and MCP-1, and upregulating the insulin-sensitive transporter GLUT4 and the anti-inflammatory adiponectin (p < 0.05). Our findings suggest that Lactobacillus sakei Probio65 and Lactobacillus plantarum Probio-093 are promising agents for microbiome-targeted anti-obesity therapies, offering the effective mitigation of obesity and improvement in adipocyte function in a murine model. Full article
(This article belongs to the Special Issue Natural Products for the Treatment of Obesity)
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18 pages, 4249 KiB  
Article
Evaluation of Anti-Obesity and Antidiabetic Activities of Orostachys japonicus in Cell and Animal Models
by Ramakanta Lamichhane, Prakash Raj Pandeya, Kyung-Hee Lee, Gopal Lamichhane, Jae-Young Cheon, Hyo Shin Park, Nguyen Quoc Tuan and Hyun-Ju Jung
Pharmaceuticals 2024, 17(3), 357; https://doi.org/10.3390/ph17030357 - 10 Mar 2024
Cited by 1 | Viewed by 1749
Abstract
Orostachys japonicus is a popular traditional medicinal herb used in Asian countries. This study is focused on evaluating its role in lipid and glucose metabolism in cell and animal models to establish the plant as an anti-obesity and antidiabetic herb. A butanol fraction [...] Read more.
Orostachys japonicus is a popular traditional medicinal herb used in Asian countries. This study is focused on evaluating its role in lipid and glucose metabolism in cell and animal models to establish the plant as an anti-obesity and antidiabetic herb. A butanol fraction of O. japonicus was used in the study. The lipid production was evaluated by the Oil Red O technique while the expression of adipogenic markers by Western blotting and RT-PCR using 3T3-L1 preadipocyte. The effect on glucose uptake activity was evaluated in C2C12 myoblast cells. The animal study was carried out in C57BL mice to evaluate anti-obesity activity using the high-fat diet model. The evaluation of serum lipid, blood glucose, adipogenic and fibrosis markers in the liver, and fat deposition in the liver and adipose tissue (by histology) of mice was conducted. Butanol fraction of O. japonicus significantly inhibited the lipid production in the 3T3-L1 cells and reduced the expression of PPARγ, C/EBPα, SREBP-1c and aP2. It enhanced glucose uptake in insulin-resistant C2C12 myoblast cells. It reduced body weight, triglycerides, and blood glucose in the obese mice. It significantly inhibited lipid accumulation in the liver and adipose tissue of obese mice along with suppression of expression of adipogenic and fibrosis markers in the liver. In summary, supporting the previous results, this study helped to establish the potent anti-obesity, antidiabetic, and liver-protecting effect of the butanol fraction of O. japonicus. Full article
(This article belongs to the Special Issue Natural Products for the Treatment of Obesity)
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13 pages, 3642 KiB  
Article
Betanin from Beetroot (Beta vulgaris L.) Regulates Lipid Metabolism and Promotes Fat Browning in 3T3-L1 Adipocytes
by Ho Seon Lee, Seung Min Choi, Sung Ho Lim and Chang-Ik Choi
Pharmaceuticals 2023, 16(12), 1727; https://doi.org/10.3390/ph16121727 - 14 Dec 2023
Cited by 2 | Viewed by 1844
Abstract
Fat browning, which converts white adipose tissue to brown, has attracted attention as a promising strategy for the treatment of obesity. Betanin (BT) has been reported to have potential anti-obesity activity. 3T3-L1 cells were differentiated for 7 days during BT treatment. The BT [...] Read more.
Fat browning, which converts white adipose tissue to brown, has attracted attention as a promising strategy for the treatment of obesity. Betanin (BT) has been reported to have potential anti-obesity activity. 3T3-L1 cells were differentiated for 7 days during BT treatment. The BT concentration range for the study was determined using an MTT assay, and lipid accumulation was evaluated by Oil-Red-O staining. The expression of protein level was analyzed by Western blot. Immunofluorescence images were performed with confocal microscopy to visually show the amount and location of thermogenesis factor uncoupling protein1 (UCP1) and mitochondria. qRT-PCR was performed to evaluate mRNA expression. BT inhibited lipid accumulation and increased the expression of UCP1, peroxisome-proliferator-activated receptor gamma (PPARγ), and PPARγ coactivator-1 alpha (PGC-1α). In addition, the increases in beige adipocyte-specific markers were observed, supporting BT-mediated browning of the fat tissue. The UCP1 was localized in the inner membrane of the mitochondria, and its expression was associated with mitochondrial activation. Consistent with this, the mRNA expression of mitochondrial biogenesis markers increased in 3T3-L1 cells after BT treatment. Immunofluorescence staining also indicated an increased number of mitochondria and UCP1, respectively. Moreover, BT inhibited lipogenesis and enhanced lipolysis and fatty acid oxidation. This mechanism has been suggested to be mediated by an adenosine monophosphate-activated protein kinase (AMPK) pathway. BT induces fat browning and regulates lipid metabolism via the AMPK-mediated pathway in 3T3-L1 cells, suggesting that BT can be a promising candidate for controlling obesity. Full article
(This article belongs to the Special Issue Natural Products for the Treatment of Obesity)
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11 pages, 1352 KiB  
Article
In Silico Identification of Peptides with PPARγ Antagonism in Protein Hydrolysate from Rice (Oryza sativa)
by Felipe de Jesús Ruiz-López, Bryan Alejandro Espinosa-Rodríguez, David Arturo Silva-Mares, Blanca Edelia González-Martínez, Manuel López-Cabanillas Lomelí, Luis Fernando Méndez-López and Jesús Alberto Vázquez-Rodríguez
Pharmaceuticals 2023, 16(3), 440; https://doi.org/10.3390/ph16030440 - 15 Mar 2023
Cited by 4 | Viewed by 2171
Abstract
At least half the population in industrialized countries suffers from obesity due to excessive accumulation of adipose tissue. Recently, rice (Oryza sativa) proteins have been considered valuable sources of bioactive peptides with antiadipogenic potential. In this study, the digestibility and bioaccessibility [...] Read more.
At least half the population in industrialized countries suffers from obesity due to excessive accumulation of adipose tissue. Recently, rice (Oryza sativa) proteins have been considered valuable sources of bioactive peptides with antiadipogenic potential. In this study, the digestibility and bioaccessibility in vitro of a novel protein concentrate (NPC) from rice were determined through INFOGEST protocols. Furthermore, the presence of prolamin and glutelin was evaluated via SDS-PAGE, and their potential digestibility and the bioactivity of ligands against peroxisome proliferator-activated receptor gamma (PPARγ) were explored by BIOPEP UWM and HPEPDOCK. For the top candidates, molecular simulations were conducted using Autodock Vina to evaluate their binding affinity against the antiadipogenic region of PPARγ and their pharmacokinetics and drug-likeness using SwissADME. Simulating gastrointestinal digestion showed a recovery of 43.07% and 35.92% bioaccessibility. The protein banding patterns showed the presence of prolamin (57 kDa) and glutelin (12 kDa) as the predominant proteins in the NPC. The in silico hydrolysis predicts the presence of three and two peptide ligands in glutelin and prolamin fraction, respectively, with high affinity for PPARγ (≤160). Finally, the docking studies suggest that the prolamin-derived peptides QSPVF and QPY (−6.38 & −5.61 kcal/mol, respectively) have expected affinity and pharmacokinetic properties to act as potential PPARγ antagonists. Hence, according to our results, bioactive peptides resulting from NPC rice consumption might have an antiadipogenic effect via PPARγ interactions, but further experimentation and validation in suitable biological model systems are necessary to gain more insight and to provide evidence to support our in silico findings. Full article
(This article belongs to the Special Issue Natural Products for the Treatment of Obesity)
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16 pages, 1475 KiB  
Article
West Mexico Berries Modulate α-Amylase, α-Glucosidase and Pancreatic Lipase Using In Vitro and In Silico Approaches
by Carmen Alejandrina Virgen-Carrillo, Elia Herminia Valdés Miramontes, David Fonseca Hernández, Diego A. Luna-Vital and Luis Mojica
Pharmaceuticals 2022, 15(9), 1081; https://doi.org/10.3390/ph15091081 - 30 Aug 2022
Cited by 6 | Viewed by 2219
Abstract
The objective was to evaluate the antioxidant and biological potential of eight freeze-dried berry varieties of southern Jalisco using in silico and in vitro approaches. Fourteen tentative phenolic compounds were identified in berries by ESI-QToF, including anthocyanins, phenolic acids, flavanols and flavonols. In [...] Read more.
The objective was to evaluate the antioxidant and biological potential of eight freeze-dried berry varieties of southern Jalisco using in silico and in vitro approaches. Fourteen tentative phenolic compounds were identified in berries by ESI-QToF, including anthocyanins, phenolic acids, flavanols and flavonols. In silico assays of phytochemicals in the berry inhibiting enzymes related to obesity and diabetes showed predicted binding energy interactions (ranging from −5.4 to −9.3 kcal/mol). Among the cultivars, antioxidant potential for DPPH IC50 ranged from 1.27 to 3.40 mg/mL, ABTS IC50 from 2.26 to 7.32 mg/mL and nitric oxide (NO) inhibition IC50 from 4.26 to 11.07 mg/mL. The potential to inhibit α-amylase IC50 ranged from 4.02 to 7.66 mg/mL, α-glucosidase IC50 from 0.27 to 4.09 mg/mL, lipase IC50 from 1.30 to 4.82 mg/mL and DPP-IV IC50 from 1.36 to 3.31 mg/mL. Blackberry cultivars from the southern Jalisco region showed outstanding biological potential compared to other evaluated berries and could be used in the formulation of functional foods in the prevention of noncommunicable diseases. Full article
(This article belongs to the Special Issue Natural Products for the Treatment of Obesity)
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