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从穿心莲中分离得到的新穿心莲内酯对体外和体内活化巨噬细胞中一氧化氮产生的抑制作用。

Suppression of NO production in activated macrophages in vitro and ex vivo by neoandrographolide isolated from Andrographis paniculata.

作者信息

Batkhuu Javzan, Hattori Koichi, Takano Fumihide, Fushiya Shinji, Oshiman Ko-ichi, Fujimiya Yoshiaki

机构信息

Experimental Station for Medicinal Plant Studies, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.

出版信息

Biol Pharm Bull. 2002 Sep;25(9):1169-74. doi: 10.1248/bpb.25.1169.

Abstract

In this study, we investigated the in vitro and ex vivo suppressive effects of Andrographis paniculata on nitric oxide (NO) production in mouse peritoneal macrophages elicited by bacillus Calmette-Guéin (BCG) and stimulated by lipopolysaccharide (LPS). Incubation of BCG-induced macrophages with the methanol extract of A. paniculata reduced LPS stimulated NO production. The diterpene lactones andrographolide and neoandrographolide were isolated as active components from the extract. These compounds suppressed NO production in a concentration-dependent manner in the concentration range from 0.1 to 100 microM and their IC50 values were 7.9 and 35.5 microM. Neoandrographolide also suppressed NO production by 35 and 40% when the macrophages were collected after oral administration of neoandrographolide at doses of 5 and 25 mg/kg/d and LPS stimulated NO production was examined. However, andrographolide did not reduce NO production on oral administration at the same doses. These results indicate that neoandrographolide, which inhibited NO production both in vitro and ex vivo may play an important role in the use of A. paniculata as an anti-inflammatory crude drug.

摘要

在本研究中,我们调查了穿心莲对卡介苗(BCG)诱导并经脂多糖(LPS)刺激的小鼠腹腔巨噬细胞中一氧化氮(NO)生成的体外和离体抑制作用。用穿心莲甲醇提取物孵育卡介苗诱导的巨噬细胞可降低LPS刺激的NO生成。从提取物中分离出二萜内酯穿心莲内酯和新穿心莲内酯作为活性成分。这些化合物在0.1至100 microM的浓度范围内以浓度依赖性方式抑制NO生成,其IC50值分别为7.9和35.5 microM。当以5和25 mg/kg/d的剂量口服新穿心莲内酯后收集巨噬细胞并检测LPS刺激的NO生成时,新穿心莲内酯也可使NO生成分别抑制35%和40%。然而,相同剂量口服穿心莲内酯并没有降低NO生成。这些结果表明,在体外和离体均能抑制NO生成的新穿心莲内酯可能在穿心莲作为抗炎生药的应用中发挥重要作用。

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