Chemical Group Profiling, In Vitro and In Silico Evaluation of Aristolochia ringens on α-Amylase and α-Glucosidase Activity

马兜铃的化学基团分析、体外和计算机模拟评估对 α-淀粉酶和 α-葡萄糖苷酶活性的影响

阅读:5
作者:J B Ahmad, E O Ajani, S Sabiu

Abstract

Diabetes mellitus (DM) has become a global scourge, and there is a continuous search for novel compounds as viable alternatives to synthetic drugs which are often accompanied by severe adverse effects. Aristolochia ringens is among the scientifically implicated botanicals effective in the management of several degenerative diseases including DM. The current study evaluated the inhibitory mechanism(s) of root extract of A. ringens on α-amylase and α-glucosidase in vitro and in silico, while its constituents were characterized using liquid chromatography-mass spectrometric technique. The extract had concentration-dependent inhibitory effect on the study enzymes, and the inhibition compared well with that of standard drug (acarbose) with respective IC50 values of 0.67 mg/mL (α-amylase) and 0.57 mg/mL (α-glucosidase) compared with that of the extract (0.63 and 0.54 mg/mL). The extract competitively and uncompetitively inhibited α-amylase and α-glucosidase, respectively. Of the identified compounds, dianoside G (-12.4, -12.5 kcal/mol) and trilobine (-10.0, -10.0 kcal/mol) had significant interactions with α-amylase and α-glucosidase, respectively, while magnoflorine and asiatic acid also interacted keenly with both enzymes, with quercetin 3-O-glucuronide and strictosidine showing better affinity towards α-glucosidase. These observations are suggestive of involvement of these compounds as probable ligands contributing to antidiabetic potential of the extract. While studies are underway to demystify the yet to be identified compounds in the extract, the data presented have lent scientific credence to the acclaimed in vivo antidiabetic potential of the extract and suggested it as a viable source of oral hypoglycaemic agent.

特别声明

1、本页面内容包含部分的内容是基于公开信息的合理引用;引用内容仅为补充信息,不代表本站立场。

2、若认为本页面引用内容涉及侵权,请及时与本站联系,我们将第一时间处理。

3、其他媒体/个人如需使用本页面原创内容,需注明“来源:[生知库]”并获得授权;使用引用内容的,需自行联系原作者获得许可。

4、投稿及合作请联系:info@biocloudy.com。