Suppr超能文献

来自巴生良姜(Alpinia pahangensis Ridl.)的巴生良姜素A对α-葡萄糖苷酶和α-淀粉酶的分子洞察及抑制模式

Molecular Insight and Mode of Inhibition of α-Glucosidase and α-Amylase by Pahangensin A from Alpinia pahangensis Ridl.

作者信息

Loo Kong Yong, Leong Kok Hoong, Sivasothy Yasodha, Ibrahim Halijah, Awang Khalijah

机构信息

Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia.

Center for Natural Product and Drug Discovery (CENAR), Department of Chemistry, Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia.

出版信息

Chem Biodivers. 2019 Jun;16(6):e1900032. doi: 10.1002/cbdv.201900032. Epub 2019 May 9.

Abstract

The inhibition of carbohydrate-hydrolyzing enzymes in human digestive organs is crucial in controlling blood sugar levels, which is important in treating type 2 diabetes. In the current study, pahangensin A (1), a bis-labdanic diterpene characterized previously in the rhizomes of Alpinia pahangensis Ridl., was identified as an active dual inhibitor for α-amylase (IC =114.80 μm) and α-glucosidase (IC =153.87 μm). This is the first report on the dual α-amylase and α-glucosidase inhibitory activities of a bis-labdanic diterpene. The Lineweaver-Burk plots of compound 1 indicate that it is a mixed-type inhibitor with regard to both enzymes. Based on molecular docking studies, compound 1 docked in a non-active site of both enzymes. The dual inhibitory activity of compound 1 makes it a suitable natural alternative in the treatment of type 2 diabetes.

摘要

抑制人体消化器官中的碳水化合物水解酶对于控制血糖水平至关重要,这在治疗2型糖尿病中具有重要意义。在当前的研究中,曾在彭亨月桂(Alpinia pahangensis Ridl.)根茎中鉴定出的双-labdanic二萜类化合物彭亨月桂素A(1),被确定为α-淀粉酶(IC =114.80 μm)和α-葡萄糖苷酶(IC =153.87 μm)的活性双重抑制剂。这是关于双-labdanic二萜类化合物具有双重α-淀粉酶和α-葡萄糖苷酶抑制活性的首次报道。化合物1的Lineweaver-Burk图表明,它对于这两种酶而言都是混合型抑制剂。基于分子对接研究,化合物1对接在这两种酶的非活性位点。化合物1的双重抑制活性使其成为治疗2型糖尿病的合适天然替代品。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验