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基于活性导向从Benth.叶中发现α-葡萄糖苷酶和β-葡萄糖醛酸酶的双重抑制剂

Activity guided discovery of dual inhibitors of α-glucosidase and β-glucuronidase from the leaves of Benth.

作者信息

He Yanxi, Xu Huanran, Tan Shaoqian, Long Jing, Lei Hui, Xiao Ling, Qi Xiaoyi, Deng Mingming, Xiong Xia, You Jingcan, Zhu Liangliang, Lü Muhan, Liang Sicheng

机构信息

The Affiliated Hospital of Southwest Medical University, Luzhou, People's Republic of China.

Innovation Centre of Targeted Development of Medicinal Resources (iCTM), Anqing Normal University, Anqing, People's Republic of China.

出版信息

J Enzyme Inhib Med Chem. 2025 Dec;40(1):2501041. doi: 10.1080/14756366.2025.2501041. Epub 2025 May 15.

DOI:10.1080/14756366.2025.2501041
PMID:40371697
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12082738/
Abstract

Type 2 diabetes mellitus (T2DM) and cancers are two globally prevalent diseases which can increase the incidence of each other. Intestinal α-glucosidase and β-glucuronidase are key targets for glycaemic control and chemotherapy detoxification, respectively. This study first found that the leaf methanol extract of displayed dual inhibition to the two enzymes. The dually active constituents were then isolated and identified as two prenylated isoflavones of 6,8-diprenylorobol and 6,8-diprenylgenistein. Diprenylorobol exhibits competitive inhibition to both the two enzymes with values of 21.6 μM (α-glucosidase) and 1.41 μM (β-glucuronidase). Diprenylgenistein is an uncompetitive inhibitor of α-glucosidase ( = 11.4 μM) but a competitive inhibitor of β-glucuronidase ( = 1.69 μM). Molecular docking studies showed that both the two isoflavones tightly bind into the active pockets via various hydrogen bonds and hydrophobic interactions. In summary, the current study identifies two promising dual inhibitors of α-glucosidase and β-glucuronidase from the leaves of .

摘要

2型糖尿病（T2DM）和癌症是两种在全球普遍流行的疾病，它们会相互增加发病率。肠道α-葡萄糖苷酶和β-葡萄糖醛酸酶分别是血糖控制和化疗解毒的关键靶点。本研究首次发现[植物名称未给出]的叶片甲醇提取物对这两种酶具有双重抑制作用。随后分离并鉴定出具有双重活性的成分是两种异戊烯基化异黄酮，即6,8-二异戊烯基奥洛波尔和6,8-二异戊烯基染料木黄酮。二异戊烯基奥洛波尔对这两种酶均表现出竞争性抑制作用，对α-葡萄糖苷酶的Ki值为21.6 μM，对β-葡萄糖醛酸酶的Ki值为1.41 μM。二异戊烯基染料木黄酮是α-葡萄糖苷酶的非竞争性抑制剂（Ki = 11.4 μM），但却是β-葡萄糖醛酸酶的竞争性抑制剂（Ki = 1.69 μM）。分子对接研究表明，这两种异黄酮均通过各种氢键和疏水相互作用紧密结合到活性口袋中。总之，本研究从[植物名称未给出]的叶片中鉴定出两种有前景的α-葡萄糖苷酶和β-葡萄糖醛酸酶双重抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/4aae5f8cebb7/IENZ_A_2501041_F0009_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/03327ba20860/IENZ_A_2501041_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/e7fa0c611350/IENZ_A_2501041_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/1030fe56ce22/IENZ_A_2501041_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/af748f6d91ff/IENZ_A_2501041_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/73b5bd22b3cb/IENZ_A_2501041_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/77d15e3ea1b5/IENZ_A_2501041_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/17c84f9fe896/IENZ_A_2501041_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/f7017b923b9b/IENZ_A_2501041_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/be18d779ba1f/IENZ_A_2501041_F0008_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/4aae5f8cebb7/IENZ_A_2501041_F0009_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/03327ba20860/IENZ_A_2501041_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/e7fa0c611350/IENZ_A_2501041_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/1030fe56ce22/IENZ_A_2501041_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/af748f6d91ff/IENZ_A_2501041_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/73b5bd22b3cb/IENZ_A_2501041_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/77d15e3ea1b5/IENZ_A_2501041_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/17c84f9fe896/IENZ_A_2501041_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/f7017b923b9b/IENZ_A_2501041_F0007_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/be18d779ba1f/IENZ_A_2501041_F0008_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c68/12082738/4aae5f8cebb7/IENZ_A_2501041_F0009_C.jpg

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