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具有罕见骨架的连翘生物碱在体外具有抗炎和抗病毒活性。

Alkaloids bearing rare skeletons from Forsythia suspensa with anti-inflammatory and anti-viral activities in vitro.

作者信息

Zhao Lin, Li Wei, Dai Sheng-Jun, Liu Rong-Xia, Xie Ze-Ping, Zhang Shu-Min, Yue Xi-Dian

机构信息

School of Pharmaceutical Science, Yantai University, Yantai, 264005, People's Republic of China.

School of Pharmaceutical Science, Yantai University, Yantai, 264005, People's Republic of China.

出版信息

Phytochemistry. 2021 Jun;186:112739. doi: 10.1016/j.phytochem.2021.112739. Epub 2021 Mar 25.

DOI:10.1016/j.phytochem.2021.112739
PMID:33773412
Abstract

Five alkaloids, including two previously undescribed alkaloids, named forsyshiyanines A and B, attributable to the rare skeletons 4b,5,6,7,8,8a,9,10-octahydrobenzo[f]quinoline and (6,7-dihydro-5H-cyclopenta[c]pyridin-7-yl)methyl, respectively, along with three known ones (3-5), were isolated from the ripe fruits of Forsythia suspensa. The chemical structures including absolute configurations of two undescribed compounds were established using integrated spectroscopic techniques, electronic circular dichroism calculations, and single-crystal x-ray diffraction analysis. In vitro, five alkaloids showed anti-inflammatory activities, with the inhibition rates of the release of β-glucuronidase from polymorphonuclear leukocytes of rats being in the range 47.9%-56.0% at a concentration of 10 μM. Moreover, five compounds exhibited anti-viral activities against influenza A virus and respiratory syncytial virus, with IC values in the range of 7.3-32.5 μM and EC values in the range 3.7-14.1 μM.

摘要

从连翘的成熟果实中分离出了5种生物碱,其中包括两种以前未描述过的生物碱,分别命名为连翘碱A和连翘碱B,它们具有罕见的骨架结构,分别为4b,5,6,7,8,8a,9,10-八氢苯并[f]喹啉和(6,7-二氢-5H-环戊[c]吡啶-7-基)甲基,还有三种已知的生物碱(3-5)。利用综合光谱技术、电子圆二色性计算和单晶X射线衍射分析确定了两种未描述化合物的化学结构,包括绝对构型。在体外,这5种生物碱表现出抗炎活性,在浓度为10 μM时,大鼠多形核白细胞中β-葡萄糖醛酸酶释放的抑制率在47.9%-56.0%之间。此外,这5种化合物对甲型流感病毒和呼吸道合胞病毒具有抗病毒活性,IC值在7.3-32.5 μM范围内,EC值在3.7-14.1 μM范围内。

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Alkaloids bearing rare skeletons from Forsythia suspensa with anti-inflammatory and anti-viral activities in vitro.具有罕见骨架的连翘生物碱在体外具有抗炎和抗病毒活性。
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