Hu Rui-Dan, Lin Wei-Yao, Feng Qian, Liu Jinru, Chen Yidi, Ji Aijia, Wang Caiyan, Cao Liping, Zhang Rong, Liu Zhongqiu, Cui Hui, Liang Qi, Zhang Rong-Rong
Guangdong Provincial Key Laboratory of Translational Cancer Research of Chinese Medicines, Joint International Research Laboratory of Translational Cancer Research of Chinese Medicines, International Institute for Translational Chinese Medicine, School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, People's Republic of China.
Shenzhen Bao'an Traditional Chinese Medicine Hospital, Guangzhou University of Chinese Medicine, Shenzhen 518100, People's Republic of China.
J Agric Food Chem. 2024 May 22;72(20):11452-11464. doi: 10.1021/acs.jafc.4c00500. Epub 2024 May 12.
In this work, a new rapid and targeted method for screening α-glucosidase inhibitors from was developed and verified. Ten new polycyclic polyprenylated acylphloroglucinols (PPAPs), hyperlagarol A-J (-), and nine known PPAPs (-) were obtained from . Their structures were identified by using comprehensive analyses involving mass spectrometry, ultraviolet spectroscopy, infrared spectroscopy, nuclear magnetic resonance spectroscopy, and electron capture dissociation calculations. and are two new rare 2,3--spirocyclic PPAPs, and are two novel 12,13--spirocyclic PPAPs, and are two novel spirocyclic PPAPs, and are two new unusual spirocyclic PPAPs with complex bridged ring systems, and and are two novel nonspirocyclic PPAPs. α-GC inhibitory activities of all isolated compounds were tested. Most of them displayed inhibitory activities against α-glucosidase, with the IC values ranging from 6.85 ± 0.65 to 112.5 ± 9.03 μM. Moreover, the inhibitory type and mechanism of the active compounds were further analyzed using kinetic studies and molecular docking.
在这项工作中，开发并验证了一种从[具体来源未给出]中筛选α-葡萄糖苷酶抑制剂的新的快速靶向方法。从[具体来源未给出]中获得了10种新的多环多异戊烯基酰基间苯三酚（PPAPs），hyperlagarol A-J（-），以及9种已知的PPAPs（-）。通过质谱、紫外光谱、红外光谱、核磁共振光谱和电子捕获解离计算等综合分析确定了它们的结构。[化合物名称未给出]和[化合物名称未给出]是两种新的罕见的2,3-螺环PPAPs，[化合物名称未给出]和[化合物名称未给出]是两种新型的12,13-螺环PPAPs，[化合物名称未给出]和[化合物名称未给出]是两种新型螺环PPAPs，[化合物名称未给出]和[化合物名称未给出]是两种具有复杂桥环系统的新的不寻常螺环PPAPs，[化合物名称未给出]和[化合物名称未给出]是两种新型非螺环PPAPs。测试了所有分离化合物的α-GC抑制活性。它们中的大多数对α-葡萄糖苷酶表现出抑制活性，IC值范围为6.85±0.65至112.5±9.03μM。此外，使用动力学研究和分子对接进一步分析了活性化合物的抑制类型和机制。
