叶提取物中富含酚的部分可改善链脲佐菌素-烟酰胺诱导的糖尿病大鼠的高血糖和氧化应激症状

IF 1.7 Q3 INTEGRATIVE & COMPLEMENTARY MEDICINE Journal of Ayurveda and Integrative Medicine Pub Date : 2024-05-01 DOI:10.1016/j.jaim.2024.100906

Puspanjali Khound , Prashanta Kumar Deb , Swarnali Bhattacharjee , Karla Damián Medina , Partha Pratim Sarma , Biswatrish Sarkar , Rajlakshmi Devi

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引用次数: 0

摘要

背景Clerodendrum glandulosum Lindl.是印度东北部一种重要的民族药用灌木，被传统医学家用于控制糖尿病、高血压、关节炎等各种疾病。此外，还进行了室内分子对接研究，以了解已确定的主要化合物与一些与糖尿病并发症相关的靶蛋白之间的分子相互作用。材料和方法从叶的水乙醇（80% MeOH）提取物中纯化出富含多酚的馏分（PRF），并对其进行体外抗氧化和抗糖尿病特性评估。此外，还对链脲佐菌素-烟酰胺诱导的 Wistar 白化大鼠高血糖症的改善效果进行了评估。结果PRF的化学分析显示其含有咖啡酸、马鞭草苷、异马鞭草苷和芹菜素等酚类化合物，其中马鞭草苷（598.14 ± 1.24 mg/g）是主要化合物。体外研究显示，PRF 具有很强的抗氧化性（DPPH 的 IC50：32.45 ± 2.16 μg/mL；ABTS：39.08 ± 0.53 μg/mL）和出色的醛糖还原酶抑制潜力（IC50 2.18 ± 0.10 μg/mL）。使用 PRF 治疗后，血糖水平降低，血浆胰岛素水平升高。结果还表明，内源性抗氧化剂和炎症细胞因子（IL-6 和 TNF-α）的抑制作用与标准相当。分子对接研究预测了已鉴定分子与参与高血糖发生的酶的关键氨基酸残基之间的相互作用。

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Phenolic enriched fraction of Clerodendrum glandulosum Lindl. leaf extract ameliorates hyperglycemia and oxidative stress in streptozotocin-nicotinamide induced diabetic rats

Background

Clerodendrum glandulosum Lindl. is an important ethnomedicinal shrub of Northeast India, used by traditional healers to control various ailments like diabetes, hypertension, arthritis, etc.

Objectives

The present study was conducted to explore the anti-hyperglycemic and antioxidative effects of the polyphenol-rich fraction (PRF) of C. glandulosum leaf extract and identification of its major bioactive compounds. Further, an in-silico molecular docking study was also performed to understand the molecular interactions of the identified major compounds with some target proteins associated with diabetic complications.

Materials and methods

PRF was purified from the hydromethanolic (80% MeOH) extract of leaves and subjected to assessment of in-vitro antioxidant and anti-diabetic properties. It was also subjected to evaluate the ameliorative effect during streptozotocin-nicotinamide-induced hyperglycemia in Wistar albino rats. An in-silico molecular docking study was also performed to complement the in-vitro/in-vivo studies.

Results

Chemical analysis of PRF showed the presence of phenolics like caffeic acid, verbascoside, isoverbascoside, and apigenin, of which verbascoside (598.14 ± 1.24 mg/g) was found to be the principal compound. In-vitro studies showed potent antioxidant (IC₅₀ of DPPH:32.45 ± 2.16 μg/mL; ABTS:39.08 ± 0.53 μg/mL) properties and excellent aldose reductase inhibition potential (IC₅₀ 2.18 ± 0.10 μg/mL). Treatment with PRF showed reduced blood glucose levels and increased plasma insulin levels. The results also indicate an improvement of endogenous antioxidants and suppression of inflammatory cytokines (IL-6 and TNF-α) comparable to the standard. Molecular docking studies predicted promising interactions between the identified molecules and the crucial amino acid residues of the enzymes involved in the development of hyperglycemia.