木芙蓉花萼甲醇提取物的口服葡萄糖耐量试验及花萼植物化学物质对硅-淀粉酶的抑制作用研究

Nasrin Akter Shova, M. A. S. Azad, M.M. Islam, R. Jahan, M. Rahmatullah
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摘要

背景:糖尿病(DM)是一种以血糖升高为特征的内分泌系统疾病,血糖升高导致氧化应激增加和其他复杂疾病的发展。这种疾病是由胰腺细胞不产生胰岛素或胰岛素抵抗引起的。近年来,糖尿病呈快速增长趋势。虽然高血糖(高血糖)可以通过抗糖尿病药物和/或注射胰岛素来控制,但孟加拉国的农村居民更喜欢由传统医生配发的植物性传统药物。方法和结果:采用木芙蓉花萼(MEHS)甲醇提取物对小鼠进行口服葡萄糖耐量试验;花萼在孟加拉国被广泛用于控制高血糖。在每公斤体重100、200和400毫克的剂量下,与未治疗的对照组小鼠相比,MEHS的血糖水平分别降低了55.8、62.0和62.77%。相比之下,格列本脲每公斤体重10毫克的剂量可使血糖水平降低61%。此外,硅分子对接研究表明,木芙花花萼中存在的一些植物化学物质预测了人类-淀粉酶(PDB编号:2QV4)的低结合能,具有抑制高血糖的潜力。结论:MEHS在400 mg/kg剂量下降低血糖近63%,与格列本脲10 mg/kg剂量相当。计算机实验进一步表明,木槿花萼中的一些植物化学物质值得进一步评价,以开发新的抗糖尿病药物。
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Oral glucose tolerance test with methanol extract of Hibiscus sabdariffa L. calyces and in silico alpha-amylase inhibition studies with selected calyce phytochemicals
Background: Diabetes mellitus (DM) is an endocrinological disorder characterized by increased blood glucose, which in turn leads to increased oxidative stress and development of other complicated disorders. The disorder is caused either by non-production of insulin by pancreatic  -cells or development of insulin resistance. In recent years, diabetes is increasing rapidly. Although high blood glucose (hyperglycemia) is controllable through anti-diabetic drugs and/or insulin injection, rural people in Bangladesh prefer plant-based traditional medicines dispensed by traditional medicinal practitioners. Methods and findings: The present study objective was to conduct oral glucose tolerance test (OGTT) in glucose-challenged mice with methanol extract of Hibiscus sabdariffa calyces (MEHS); the calyces are widely used in Bangladesh for controlling hyperglycemia. At doses of 100, 200 and 400 mg per kg body weight, MEHS reduced blood glucose level by 55.8, 62.0 and 62.77%, respectively compared to control mice, which were untreated. Glibenclamide, by comparison, reduced blood glucose level by 61% at a dose of 10 mg per kg body weight. Furthermore, in silico molecular docking studies showed that a number of phytochemicals present in Hibiscus sabdariffa calyces have predicted low binding energies for human  -amylase (PDB number: 2QV4) with the potential for inhibiting hyperglycemia. Conclusions: (MEHS) reduced blood glucose by nearly 63% at a dose of 400 mg/kg, which was comparable to that of glibenclamide at a dose of 10 mg/kg. In silico studies further indicated that a number of phytochemicals of the calyces of Hibiscus sabdariffa merits further evaluation towards new anti-diabetic drug discovery.
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