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anti-obesity drugs

Xufeng Tao, Lianhong Yin, Lina Xu, Jinyong Peng
Currently, the numbers of patients with cancer, fibrosis, diabetes, chronic kidney disease, stroke and osteoporosis are increasing fast and fast. It's critical necessary to discovery lead compounds for new drug development. Dioscin, one active compound in some medicinal plants, has anti-inflammation, immunoregulation, hypolipidemic, anti-viral, anti-fungal and anti-allergic effects. In recent years, dioscin has reached more and more attention with its potent effects to treat liver, kidney, brain, stomach and intestine damages, and metabolic diseases including diabetes, osteoporosis, obesity, hyperuricemia as well as its anti-cancer activities through adjusting multiple targets and multiple signals...
October 10, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Misato Nakamura, Ayumi Eguchi, Mari Inohana, Rei Nagahara, Hirotada Murayama, Masashi Kawashima, Sayaka Mizukami, Mihoko Koyanagi, Shim-Mo Hayashi, Robert R Maronpot, Makoto Shibutani, Toshinori Yoshida
Mineralocorticoid receptor (MR)/NADPH oxidase (NOX) signaling is involved in the development of obesity, insulin resistance, and renal diseases; however, the role of this signaling on steatotic preneoplastic liver lesions is not fully elucidated. We determined the effects of the MR antagonist potassium canrenoate (PC) on MR/NOX signaling in hepatic steatosis and preneoplastic glutathione S-transferase placental form (GST-P)-positive liver foci. Rats were subjected to a two-stage hepatocarcinogenesis model and fed with basal diet or high fat diet (HFD) that was co-administered with PC alone or in combination with the antioxidant alpha-glycosyl isoquercitrin (AGIQ)...
2018: Journal of Toxicological Sciences
Liping Li, Hongmei Lei, Wei Wang, Weijuan Du, Jingqun Yuan, Meijuan Tu, Hui Zhou, Su Zeng, Huidi Jiang
Nuciferine (NF), one of the main and effective components in Nelumbo nucifera Gaertn. leaf extracts, is a promising drug candidate for treatment of obesity-related diseases, while metformin is a first line therapeutic drug for type 2 diabetesmellitus (T2DM). Since NF and metformin is likely to be co-administered, the aim of the present study was to evaluate whether co-administrationof NF would influence the liver (target tissue) distribution and the anti-diabetic effect of metformin via inhibiting hepatic organic cation transporter 1 (OCT1) and multidrug and toxin extrusion 1 (MATE1)...
October 7, 2018: Biopharmaceutics & Drug Disposition
Lori M Zeltser
Pro-opiomelanocortin (POMC)-expressing neurons regulate energy balance and mediate the effects of some classes of anti-obesity therapeutics. In this issue of Cell Metabolism, D'Agostino et al. (2018) demonstrate that a small and often overlooked population of POMC neurons in the brainstem contributes to satiation induced by the FDA-approved drug lorcaserin.
October 2, 2018: Cell Metabolism
Yi-Fan Dang, Xiao-Ning Jiang, Fu-Lian Gong, Xiu-Li Guo
Rosiglitazone (ROSI), a member of thiazolidinediones (TZDs) which act as high-affinity agonists of the nuclear receptor peroxisome-proliferator-activated receptor-γ (PPARγ), is clinically used as an antidiabetic drug which could attenuate the insulin resistance associated with obesity, hypertension, and impaired glucose tolerance in humans. However, recent studies reported that ROSI had significant anticancer effects on various human malignant tumor cells. Mounting evidence indicated that ROSI could exert anticancer effects through PPARγ-dependent or PPARγ-independent ways...
September 29, 2018: Chemico-biological Interactions
John C Mathers
The purpose of this review article is to examine the evidence of the mechanisms linking obesity with bowel cancer risk and to comment on the development of interventions that may lower risk of this common age-related disease. The choice of topics for inclusion reflects my personal research on the etiology and prevention of bowel cancer over the past 3 decades. I have cited literature which addresses each of these topics, but because of the breadth of the review article, I have not attempted to do this systematically...
September 1, 2018: Nutrition Research
Rosa E Pérez-Morales, María Dolores Del Pino, José Manuel Valdivielso, Alberto Ortiz, Carmen Mora-Fernández, Juan F Navarro-González
BACKGROUND: Diabetes is a growing public health problem. Diabetic kidney disease (DKD) is the most prevalent chronic renal disease and the major cause of end-stage renal failure worldwide, predominantly due to the increase of Type 2 diabetes associated with obesity. The intimate mechanisms leading to the development and progression of renal injury in DKD are not well understood, but current knowledge indicates that its pathogenesis is multifactorial, where the immune response and inflammation appear to be relevant factors...
October 1, 2018: Nephron
Vandana Panda, Priyanka Shinde, Payal Dande
CONTEXT: Spinaciaoleracea (spinach) is abundant in antioxidant phytoconstituents, termed as the natural antioxidant mixture (NAO). OBJECTIVE: This study evaluates the anti-hyperlipidemicand anti-obesity effects of an antioxidant-rich extract of Spinaciaoleracea (NAOE) and aerobic exercise (AE) in rats fed with high fat diet (HFD). METHODS: Rats received NAOE (200 and 400 mg/kg), the standard drug orlistat (10 mg/kg), AE and NAOEAE (NAOE 400 mg/kg + AE) daily with HFD for 21 d...
September 29, 2018: Archives of Physiology and Biochemistry
Fei Li, Xiongzhong Ruan, Le Min
Obesity is a chronic, complex disease, which is associated with several comorbidities, including diabetes mellitus, hypertension, and cardiovascular diseases. It is estimated that the prevalence of obesity among both adults and children nearly tripled between 1975 and 2016, highlighting a huge unmet treatment need. However, the currently available anti-obesity drugs have serious side effects, which limit their long-term use. The finding that the newly-identified brain GDF15-GFRAL-RET receptor signaling complex is involved in stress/disease-induced anorexia will certainly impact our knowledge of body weight homeostasis under healthy and disease conditions...
December 2017: Genes & Diseases
Yi-Ju Chen, Hsiu J Ho, Ching-Hung Tseng, Zi-Lun Lai, Jeng-Jer Shieh, Chun-Ying Wu
OBJECTIVES: The intestinal microbiota has been known to involve in obesity and host immune response. We aimed to investigate the intestinal microbiota and potential genetic function in relation to clinical presentation in psoriasis patients. METHODS: Fecal microbiota and predicted genetic function inferred from high-throughput 16S ribosomal RNA sequencing were analyzed between psoriasis (n=32) and age-, gender- and body mass index (BMI)-matched non-psoriasis subjects (n=64), from a referral medical center...
September 20, 2018: Experimental Dermatology
Sara J Brandt, Timo D Müller, Richard D DiMarchi, Matthias H Tschöp, Kerstin Stemmer
Obesity and its comorbidities, such as type 2 diabetes, are pressing worldwide health concerns. Available anti-obesity treatments include weight loss pharmacotherapies and bariatric surgery. While surgical interventions typically result in significant and sustained weight loss, available pharmacotherapies are far less effective, typically decreasing body weight by no more than 5 - 10%. An emerging class of multiagonist drugs may eventually bridge this gap. This new class of specially-tailored drugs hybridizes the amino acid sequences of key metabolic hormones into one single entity with enhanced potency and sustained action...
September 19, 2018: Journal of Internal Medicine
Hu Huang, Seung-Hwan Lee, Inês Sousa-Lima, Sang Soo Kim, Won Min Hwang, Yossi Dagon, Won-Mo Yang, Sungman Cho, Min-Cheol Kang, Ji A Seo, Munehiko Shibata, Hyunsoo Cho, Getachew Debas Belew, Jinhyuk Bhin, Bhavna N Desai, Min Jeong Ryu, Minho Shong, Peixin Li, Hua Meng, Byung-Hong Chung, Daehee Hwang, Min Seon Kim, Kyong Soo Park, Paula Macedo, Morris White, John Jones, Young-Bum Kim
Obesity is a major risk factor for developing nonalcoholic fatty-liver disease (NAFLD). NAFLD is the most common form of chronic liver disease and closely associated with insulin resistance, ultimately leading to cirrhosis and hepatocellular carcinoma. However, knowledge of the intracellular regulators of obesity-linked fatty-liver disease remains incomplete. Here we showed that hepatic Rho-kinase 1 (ROCK1) drives obesity-induced steatosis in mice through stimulation of de novo lipogenesis. Mice lacking ROCK1 in the liver were resistant to diet-induced obesity due to increased energy expenditure and thermogenic gene expression...
September 18, 2018: Journal of Clinical Investigation
Soumya Ranjan Panda, Madhu Jain, Shuchi Jain, Riden Saxena, Smrutismita Hota
Background: Polycystic ovarian syndrome (PCOS), a commonly prevalent endocrinopathy among reproductive age group women, is most often associated with obesity. Increased insulin resistance appears to be the central pathophysiologic mechanism responsible for various complications of PCOS. This makes 'weight loss' as the first-line treatment approach in PCOS. So various trials have tried to compare metformin (an insulin-sensitizing agent) and orlistat (an anti-obesity drug) aiming to achieve weight loss and hence higher ovulation rate for the group of obese PCOS patients...
October 2018: Journal of Obstetrics and Gynaecology of India
Luyao Ma, Zhenghai Sun, Yawen Zeng, Mingcan Luo, Jiazhen Yang
Functional ingredients in blueberry have the best health benefits. To obtain a better understanding of the health role of blueberry in chronic disease, we conducted systematic preventive strategies for functional ingredients in blueberry, based on comprehensive databases, especially PubMed, ISI Web of Science, and CNKI for the period 2008⁻2018. Blueberry is rich in flavonoids (mainly anthocyanidins), polyphenols (procyanidin), phenolic acids, pyruvic acid, chlorogenic acid, and others, which have anticancer, anti-obesity, prevent degenerative diseases, anti-inflammation, protective properties for vision and liver, prevent heart diseases, antidiabetes, improve brain function, protective lung properties, strong bones, enhance immunity, prevent cardiovascular diseases, and improve cognitive decline...
September 16, 2018: International Journal of Molecular Sciences
F García-Rio, M J Alvarez-Puebla, I De Esteban, P Barranco, J M Olaguibel
Obesity is an asthma common comorbidity and is associated not only with its development, but also with a poorer control and higher severity of it. Recent prospective evidence supports the idea that body weight gain precedes the development of asthma, but the debate is far from over. The objective of this document is to conduct a systematic review of 3 clinical questions related to asthma and obesity: 1. Obesity and asthma: the chicken or the egg? Clinical insights from epidemiological and phenotypes studies...
September 17, 2018: Journal of Investigational Allergology & Clinical Immunology
J Barbarroja-Escudero, A Asúnsolo-Del-Barco, M J Sánchez-González, M Rodríguez-Rodríguez, M Alvarez-Mon
BACKGROUND AND OBJECTIVE: Edema of the uvula (EU) may appear in isolation or in association with other associated clinical manifestations such as urticaria, angioedema or anaphylaxis. EU may lead to upper airway obstruction, provoking obstructive respiratory distress and asphyxia. Objective: We sought to investigate the etiology of, and predisposing factors for, EU in a large population of patients referred to an outpatient clinic. METHODS: In this 3-year-follow-up cohort study, 171 patients presenting with EU were identified and classified as having isolated EU or non-isolated EU...
September 17, 2018: Journal of Investigational Allergology & Clinical Immunology
Joo Wan Kim, You-Suk Lee, Du Jin Seol, Il Je Cho, Sae Kwang Ku, Jae-Suk Choi, Hae-Jeung Lee
Blue honeysuckle (BH, Lonicera caerulea) is used as a traditional medicine in Russia, Japan and China, but is not commonly considered as an edible berry in Europe, USA or Korea. BH has been revealed to decrease serum cholesterol and triacylglycerol (triglyceride or TG) levels through the activation of AMP‑activated protein kinase (AMPK), thus it is expected to be a health functional food and pharmaceutical agent for the prevention of non‑alcoholic liver damage, in addition to effects as a suppressor of hyperlipidemia and as an anti‑obesity agent...
September 14, 2018: International Journal of Molecular Medicine
Benarous Khedidja, Benguechoua Madjeda, Ghibeche Abderrahmane
BACKGROUND: Inhibition activity of 8 synthetic molecules known as anti-allergy drugs on lipases have been investigated. The enzymatic inhibition produced by these molecules is described here for the first time. OBJECTIVE: The used anti-allergy drugs are: loratidine, primalan, zyrtec, histagan, periactin, ketotifene, rifex and bilastine. METHODS: lipase inhibition is studied using spectrophotometric method. Molecular docking has been achieved for the first time for these drugs using AutoDock Vina program to discuss the nature of interactions, structure activity relationship and the mechanism of inhibition...
September 10, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Amir Reza Ariamoghaddam, Bahman Ebrahimi-Hosseinzadeh, Ashrafalsadat Hatamian-Zarmi, Razi Sahraeian
Obesity as a dominant problem in developed countries which is known to be basic step of so many diseases is subjected to find a solution for in this work. Curcumin containing polyvinyl alcohol-gelatin nanofibers which ranging from 200 to 250 nm in diameter as a transdermal drug delivery system for declining volume of subcutaneous adipose tissue is investigated here. Morphology and synthesis method of nanofibers is designed and optimized by statistical software and a totally uniform and reproducible method of synthesis is used for preparation of a transdermal patch...
November 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Xiaopeng Li, Shuyi Li, Mo Chen, Jingyi Wang, Bijun Xie, Zhida Sun
As a major component of green tea, (-)-epigallocatechin-3-gallate (EGCG) has attracted interest from scientists owing to its potential to combat a variety of human diseases including abnormal glucose metabolism in obesity and diabetes. This study aims to (1) evaluate the molecular mechanism of EGCG in starch digestion before EGCG absorption; (2) investigate the link between PXR/CAR-mediated phase II metabolism and glucose homeostasis after EGCG is transported to small intestine and liver. EGCG suppressed starch hydrolysis both in vitro and in vivo...
September 19, 2018: Food & Function
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