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五环三萜:对抗代谢综合征的新工具。

Pentacyclic triterpenes: New tools to fight metabolic syndrome.

机构信息

Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, 136 119 Haryana, India.

School of Pharmacy, Lake Erie College of Osteopathic Medicine, Bradenton, FL 34211, USA.

出版信息

Phytomedicine. 2018 Nov 15;50:166-177. doi: 10.1016/j.phymed.2018.09.011. Epub 2018 Sep 5.

DOI:10.1016/j.phymed.2018.09.011
PMID:30466975
Abstract

BACKGROUND

Metabolic syndrome is a combination of dysregulated cardiometabolic risk factors characterized by dyslipidemia, impaired glucose tolerance, insulin resistance, inflammation, obesity as well as hypertension. These factors are tied to the increased risk for type-II diabetes and cardiovascular diseases including myocardial infarction in patients with metabolic syndrome.

PURPOSE

To review the proposed molecular mechanisms of pentacyclic triterpenes for their potential use in the metabolic syndrome.

METHODS

PubMed, Science Direct, and Google Scholar database were searched from commencement to April 2018. Following keywords were searched in the databases with varying combinations: "metabolic syndrome", "pentacyclic triterpenes", "transcription factors", "protein kinase", "lipogenesis", "adipogenesis", "lipolysis", "fatty acids", "gluconeogenesis", "cardiovascular", "mitochondria", "oxidative stress", "pancreas", "hepatic cells", "skeletal muscle", "3T3-L1", "C2C12", "obesity", "inflammation", "insulin resistance", "glucose uptake", "clinical studies" and "bioavailability".

RESULTS

Pentacyclic triterpenes, such as asiatic acid, ursolic acid, oleanolic acid, 18β-glycyrrhetinic acid, α,β-amyrin, celastrol, carbenoxolone, corosolic acid, maslinic acid, bardoxolone methyl and lupeol downregulate several metabolic syndrome components by regulating transcription factors, protein kinases and enzyme involved in the adipogenesis, lipolysis, fatty acid oxidation, insulin resistance, mitochondria biogenesis, gluconeogenesis, oxidative stress and inflammation.

CONCLUSION

In vitro and in vivo studies suggests that pentacyclic triterpenes effectively downregulate various factors related to metabolic syndrome. These phytochemicals may serve as promising candidates for clinical trials for the management of metabolic syndrome.

摘要

背景

代谢综合征是一组心血管代谢危险因素失调的病症,其特征为血脂异常、葡萄糖耐量受损、胰岛素抵抗、炎症、肥胖以及高血压。这些因素与代谢综合征患者的 II 型糖尿病和心血管疾病(包括心肌梗死)风险增加有关。

目的

综述五环三萜类化合物在代谢综合征中的潜在作用的提出的分子机制。

方法

检索了 PubMed、Science Direct 和 Google Scholar 数据库,检索时间从建库开始至 2018 年 4 月。在数据库中以不同的组合搜索了以下关键词:“代谢综合征”、“五环三萜”、“转录因子”、“蛋白激酶”、“脂肪生成”、“脂肪形成”、“脂肪分解”、“脂肪酸”、“糖异生”、“心血管”、“线粒体”、“氧化应激”、“胰腺”、“肝细胞”、“骨骼肌”、“3T3-L1”、“C2C12”、“肥胖”、“炎症”、“胰岛素抵抗”、“葡萄糖摄取”、“临床研究”和“生物利用度”。

结果

五环三萜类化合物,如齐墩果酸、熊果酸、齐墩果酸、18β-甘草次酸、α、β-桉叶醇、雷公藤红素、卡波醇、柯诺辛酸、马粟树皮酸、巴德酮酸、波多醇和羽扇豆醇,通过调节参与脂肪生成、脂肪分解、脂肪酸氧化、胰岛素抵抗、线粒体生物发生、糖异生、氧化应激和炎症的转录因子、蛋白激酶和酶,下调几种代谢综合征成分。

结论

体外和体内研究表明,五环三萜类化合物有效地下调与代谢综合征相关的各种因素。这些植物化学物质可能成为治疗代谢综合征的临床试验的有希望的候选药物。

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