Inhibitors from the rhizomes of Alpinia officinarum on production of nitric oxide in lipopolysaccharide-activated macrophages and the structural requirements of diarylheptanoids for the activity

Inhibitors from the rhizomes of Alpinia officinarum on production of nitric oxide in lipopolysaccharide-activated macrophages and the structural requirements of diarylheptanoids for the activity
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DOI:
10.1016/j.bmc.2005.08.003
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发表时间:
2006-01-01
影响因子:
3.5
通讯作者:
Yoshikawa, M
Yoshikawa, M
中科院分区:
医学3区
文献类型:
--
作者:
Matsuda, H;Ando, S;Yoshikawa, M

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用80%丙酮水提物对脂多糖(LPS)激活小鼠腹腔巨噬细胞产生一氧化氮(NO)有抑制作用。通过生物测定指导分离,两种二芳基庚烷[7-(4”-羟基-3”-甲氧基苯基-l-苯基庚烷-4-en-3- 1和3,5-二羟基-1,7-二苯庚烷]和一种黄酮醇成分(高良姜素)显著抑制lps诱导的NO生成,IC50值为33-62 μ M.为了阐明二芳基庚烷的构效关系,研究莪术中相关二芳基庚烷。结果表明,1-7位的双键或烯酮部分对活性有重要影响。(c) 2005 Elsevier Ltd版权所有。
The 80% aqueous acetone extract from the rhizomes of Alpinia officinarum, a Chinese medicinal herb, were found to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-activated mouse peritoneal macrophages. Through bioassay-guided separation, two diarylheptanoids [7-(4"-hydroxy-3"-methoxyphenyl-l-phenylhept-4-en-3-one and 3,5-dihydroxy-1,7-diphenylheptane] and a flavonol constituent (galangin) Substantially inhibited LPS-induced NO production with IC50 values of 33-62 mu M. To clarify structure-activity relationships of diarylheptanoids, related diarylheptanoids from Curcuma Zedoaria were examined. Results indicate that the double bond or enone moiety at the 1-7 positions is important for the activity. (c) 2005 Elsevier Ltd. All rights reserved.