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补骨脂种子中二酰甘油酰基转移酶抑制新型倍半萜类化合物及其构效关系研究。

Diacylglycerol acyltransferase inhibitory new meroterpenes from the seeds of Psoralea corylifolia, and their structure-activity relationship study.

机构信息

College of Pharmacy, Beihua University, Jilin 132013, China.

Molecular Cancer Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), 685-1 Yangcheongri, Ochangeup, Cheongwongun, Chungbuk 363-883, Republic of Korea.

出版信息

Fitoterapia. 2021 Jun;151:104881. doi: 10.1016/j.fitote.2021.104881. Epub 2021 Mar 10.

DOI:10.1016/j.fitote.2021.104881
PMID:33713740
Abstract

Five new meroterpenes, 12α-Psoracorylifol F (1), 7β,8α-hydroxy-12β-Psoracorylifol F (2), 8-ketone-Cyclobakuchiol C (3), 7α,8β-hydroxy-12β-Cyclobakuchiol C (4) and 8α-hydroxy-Cyclobakuchiol C (5) together with six known compounds (6-11) were isolated from seeds of Psoralea corylifolia, and their structures were elucidated on the basis of spectroscopic and physicochemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1/2. Among them, compounds 1-6 were found to exhibit selective inhibitory activity on DGAT1 with IC values ranging from 61.5 ± 1.1 to 89.1 ± 1.2 μM.

摘要

从补骨脂种子中分离得到了 5 个新的倍半萜类化合物,12α-补骨脂酚 F(1)、7β,8α-羟基-12β-补骨脂酚 F(2)、8-酮环巴考醇 C(3)、7α,8β-羟基-12β-环巴考醇 C(4)和 8α-羟基环巴考醇 C(5),以及 6 个已知化合物(6-11)。基于光谱和物理化学分析确定了它们的结构。所有分离物均评估了对 DGAT1/2 的体外抑制活性。其中,化合物 1-6 对 DGAT1 表现出选择性抑制活性,IC 值范围为 61.5±1.1 至 89.1±1.2 μM。

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