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瑞香科狼毒属二萜及其体外抗 NLRP3 炎性小体活性。

Diterpenoids from Callicarpa rubella and their in vitro anti-NLRP3 inflammasome activity.

机构信息

Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, Yunnan Research & Development Center for Natural Products, School of Chemical Science and Technology, Yunnan University, Kunming 650091, People's Republic of China.

Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, Yunnan Research & Development Center for Natural Products, School of Chemical Science and Technology, Yunnan University, Kunming 650091, People's Republic of China.

出版信息

Fitoterapia. 2020 Nov;147:104774. doi: 10.1016/j.fitote.2020.104774. Epub 2020 Nov 3.

Abstract

Nine new diterpenoids, Rubellacrns A - I (1-9), including five isopimaranes (1-4, 9), four pimaranes (5-8), together with five known isopimarane analogues (10-14), were isolated from Callicarpa rubella. The structures of these compounds were unambiguously established by HR-ESIMS and NMR spectroscopic data, the absolute configurations of compounds 5 and 9 were determined by ECD. All the isolated compounds were tested for their anti-inflammatory effects and compounds 2 and 11-14 showed NLRP3-inflammasome inhibitory activity with IC values ranging from 7.02 to 14.38 μM.

摘要

从紫珠属植物 Rubella 中分离得到了 9 个新的二萜类化合物,Rubellacrns A-I(1-9),包括 5 个异扁柏烷(1-4,9),4 个扁柏烷(5-8),以及 5 个已知的异扁柏烷类似物(10-14)。通过高分辨电喷雾质谱(HR-ESIMS)和核磁共振波谱数据确定了这些化合物的结构,通过圆二色谱(ECD)确定了化合物 5 和 9 的绝对构型。所有分离得到的化合物均进行了抗炎活性测试,化合物 2 和 11-14 对 NLRP3 炎症小体具有抑制活性,IC 值范围为 7.02-14.38μM。

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