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连翘果实中的抗炎和抗病毒拉伯烷二萜。

Anti-inflammatory and anti-viral labdane diterpenoids from the fruits of Forsythia suspensa.

机构信息

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

School of Pharmaceutical Science, Binzhou Medical University, Yantai 264003, People's Republic of China.

出版信息

Bioorg Chem. 2020 Mar;96:103651. doi: 10.1016/j.bioorg.2020.103651. Epub 2020 Feb 4.

DOI:10.1016/j.bioorg.2020.103651
PMID:32050134
Abstract

Eight labdane diterpenoids, including two new labdane diterpenoids, named forsyshiyanins A-B (2-3), along with six known ones (1, 4-8), were isolated from the fruits of Forsythia suspensa. The new structures including their absolute configurations were elucidated by extensive spectroscopic analyses, X-ray diffraction and computational calculation. In vitro, eight labdane diterpenoids showed anti-inflammatory activities, with the inhibition rates of release of β-glucuronidase from polymorphonuclear leukocytes of rats being in the range 46.8-51.0% at concentrations of 10 µM, as well as anti-viral activities against influenza A (H1N1) virus and respiratory syncytial virus (RSV), with the IC values in the range 18.4-26.2 μM and EC values in the range 10.5-14.4 μM, respectively.

摘要

从连翘果实中分离得到了 8 个拉伯烷二萜类化合物,包括 2 个新的拉伯烷二萜类化合物,命名为forsyshiyanin A-B(2-3),以及 6 个已知化合物(1、4-8)。通过广泛的光谱分析、X 射线衍射和计算计算,阐明了新结构及其绝对构型。在体外,8 个拉伯烷二萜类化合物表现出抗炎活性,在 10 μM 浓度下,对大鼠多形核白细胞β-葡糖苷酸酶释放的抑制率在 46.8-51.0%范围内,并且对甲型流感(H1N1)病毒和呼吸道合胞病毒(RSV)具有抗病毒活性,IC 值范围为 18.4-26.2 μM,EC 值范围为 10.5-14.4 μM。

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