Ishii R, Saito K, Horie M, Shibano T, Kitanaka S, Amano F
Saitama Institute of Public Health, Urawa, Japan.
Biol Pharm Bull. 1999 Jun;22(6):647-53. doi: 10.1248/bpb.22.647.
An extract of Melastoma dodecandrum LOUR. with 80% aqueous acetone (MDL) inhibited nitric oxide (NO) production by a murine macrophage-like cell line, RAW264.7, activated with lipopolysaccharide (LPS) and recombinant mouse interferon-gamma (IFN-gamma). On further fractionation of the extract, the majority of the inhibitory activity was recovered in the 50% methanol extracts, which contained hydrolyzable tannins. Among the latter, casuarinin, casuarictin, pedunclagin and nobotannin B exhibited strong inhibitory activities toward NO production, with ID50 values between 2.0 and 5.1 microM. Both MDL and the purified tannins significantly reduced the induction of the inducible nitric oxide synthase (iNOS) protein in the course of macrophage activation with LPS and IFN-gamma. In addition, the NO production by macrophages preactivated with LPS and IFN-gamma for 16 h was also inhibited by these tannins, with IC50 values around 30-130 microM, but not by MDL. These results suggest that MDL has the pharmacological ability to suppress NO production by activated macrophages and that the hydrolyzable tannins have major inhibitory activities.
用80%的丙酮水溶液提取的地稔提取物(MDL)可抑制脂多糖(LPS)和重组小鼠干扰素-γ(IFN-γ)激活的小鼠巨噬细胞样细胞系RAW264.7产生一氧化氮(NO)。对该提取物进一步分级分离后,大部分抑制活性存在于50%的甲醇提取物中,该提取物含有可水解单宁。在这些可水解单宁中,木麻黄亭、木麻黄鞣质、没食子鞣质和新鞣质B对NO的产生表现出较强的抑制活性,半数抑制浓度(ID50)值在2.0至5.1微摩尔之间。MDL和纯化的单宁均能显著降低LPS和IFN-γ激活巨噬细胞过程中诱导型一氧化氮合酶(iNOS)蛋白的表达。此外,这些单宁还能抑制经LPS和IFN-γ预激活16小时的巨噬细胞产生NO,半数抑制浓度(IC50)值约为30 - 130微摩尔,但MDL无此作用。这些结果表明,MDL具有抑制活化巨噬细胞产生NO的药理能力,且可水解单宁具有主要的抑制活性。