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玉竹甾体皂苷作为α-淀粉酶、α-葡萄糖苷酶和二肽基肽酶 IV 抑制剂。

Steroidal saponins from Trillium govanianum as α-amylase, α-glucosidase, and dipeptidyl peptidase IV inhibitory agents.

机构信息

Chemical Technology Division, CSIR-IHBT, Palampur, India.

Food and Nutraceuticals Division, CSIR-IHBT, Palampur, India.

出版信息

J Pharm Pharmacol. 2021 Mar 8;73(4):487-495. doi: 10.1093/jpp/rgaa038.

DOI:10.1093/jpp/rgaa038
PMID:33793831
Abstract

OBJECTIVE

To provide the scientific basis for the utility of rhizome of Trillium govanianum as nutraceutical supplements in managing physiological glycemic levels.

METHODS

The in vitro enzyme inhibitory activity of the extract, fractions, and the isolated steroidal saponins from the rhizome part of T. govanianum was carried out against α-amylase, α-glucosidase, and dipeptidyl peptidase IV. The molecular interactions, binding score, and pharmacokinetic parameters (absorption, distribution metabolism, and excretion) of steroidal saponins were analyzed by the Schrodinger molecular docking software.

KEY FINDINGS

Current study explained that the extract, fractions, and isolated steroidal saponins from T. govanianum possess good α-amylase and α-glucosidase inhibitory activity while moderate dipeptidyl peptidase IV inhibitory activity. Moreover, in vitro results revealed that borassoside E (IC50 7.15 ± 1.78 μM), protodioscin (IC50 6.72 ± 0.04 μM), and diosgenin (IC50 12.75 ± 2.70 μM) are most effective in inhibiting the activity of α-amylase, α-glucosidase, and dipeptidyl peptidase IV, respectively. Current in silico and in vitro studies established an association between the steroidal saponins from T. govanianum and their molecular interactions with α-amylase, α-glucosidase, and dipeptidyl peptidase IV.

CONCLUSION

The results of this investigation suggest that fractions and steroidal saponins from T. govanianum exhibit good antidiabetic activity which could be used as nutraceutical supplements for the management of systemic glucose level.

摘要

目的

为将延龄草根茎用作管理生理血糖水平的营养补充剂提供科学依据。

方法

采用体外实验方法,对延龄草根茎部分的提取物、馏分和分离得到的甾体皂苷对α-淀粉酶、α-葡萄糖苷酶和二肽基肽酶 IV 的抑制活性进行了研究。采用 Schrodinger 分子对接软件对甾体皂苷的分子相互作用、结合评分和药代动力学参数(吸收、分布、代谢和排泄)进行了分析。

主要发现

本研究表明,延龄草根茎的提取物、馏分和分离得到的甾体皂苷对α-淀粉酶和α-葡萄糖苷酶具有良好的抑制活性,对二肽基肽酶 IV 具有中等抑制活性。此外,体外实验结果表明,婆罗双苷 E(IC50 7.15 ± 1.78 μM)、原薯蓣皂苷(IC50 6.72 ± 0.04 μM)和薯蓣皂苷(IC50 12.75 ± 2.70 μM)对α-淀粉酶、α-葡萄糖苷酶和二肽基肽酶 IV 的抑制活性最强。目前的体内外研究建立了延龄草甾体皂苷与其与α-淀粉酶、α-葡萄糖苷酶和二肽基肽酶 IV 的分子相互作用之间的关系。

结论

本研究结果表明,延龄草的馏分和甾体皂苷具有良好的抗糖尿病活性,可作为营养补充剂用于管理全身血糖水平。

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