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从麻风树(Combretum leprosum)叶中分离得到的 3β-6β-16β-三羟基羽扇豆-20(29)-烯三萜对成年斑马鱼(Danio rerio)的降血糖作用:体内和计算方法。

Hypoglycemic effect on adult zebrafish (Danio rerio) of the 3β-6β-16β-trihydroxylup-20(29)-ene triterpene isolated from Combretum leprosum leaves in vivo and in silico approach.

机构信息

Postgraduate Program in Biotechnology - PPGB-Renorbio, State University of Ceara, Fortaleza, Brazil.

Graduate Program in Natural Sciences, State University of Ceara, Fortaleza, Brazil.

出版信息

Fundam Clin Pharmacol. 2022 Oct;36(5):818-826. doi: 10.1111/fcp.12776. Epub 2022 Mar 14.

Abstract

Drugs used to manage type 2 diabetes mellitus cause adverse effects. Therefore, the search for new drugs as an alternative for the treatment of diabetes increases. The effect of triterpene 3β-6β-16β-trihydroxylup-20(29)-ene isolated from the leaves of C. leprosum (CLF-1) on sucrose-induced hyperglycemia in adult zebrafish (Danio rerio) was evaluated. Initially, adult zebrafish (n = 6/group) underwent hyperglycemia induction by sucrose at 83.25 mM/L for 7 days by immersion. The hyperglycemic groups were treated with CLF-1 (4, 20, and 40 mg/kg), metformin (200 mg/kg), and acarbose (300 mg/kg) for 4 days. The in silico interaction of CLF-1, metformin, and acarbose with the enzyme maltase-glucoamylase (CtMGAM) was investigated. CLF-1 reduced sucrose-induced hyperglycemia after 4 days of treatment, in addition to having better affinity energy with CtMGAM than metformin and acarbose. Thus, CLF-1 may be a new pharmacological alternative as a hypoglycemic agent for the treatment of diabetes.

摘要

用于治疗 2 型糖尿病的药物会引起不良反应。因此,寻找新的药物作为治疗糖尿病的替代方法的需求增加了。从 Leprosy Tree(C. leprosum)的叶子中分离得到的三萜 3β-6β-16β-三羟基齐墩果酸(CLF-1)对成年斑马鱼(Danio rerio)蔗糖诱导的高血糖的影响进行了评估。最初,成年斑马鱼(每组 6 条)通过浸泡在 83.25mM/L 的蔗糖中 7 天来诱导高血糖。高血糖组用 CLF-1(4、20 和 40mg/kg)、二甲双胍(200mg/kg)和阿卡波糖(300mg/kg)治疗 4 天。还研究了 CLF-1、二甲双胍和阿卡波糖与酶麦芽糖酶-葡糖苷酶(CtMGAM)的相互作用。CLF-1 可降低 4 天治疗后的蔗糖诱导的高血糖,其与 CtMGAM 的亲和力能量优于二甲双胍和阿卡波糖。因此,CLF-1 可能是一种新的药理学替代物,可作为治疗糖尿病的降血糖药物。

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