巴西蘑菇菌丝体中抑瘤活性甾醇的分离和结构鉴定

SEPERATION AND IDENTIFICATION OF AN ANTITUMOR STEROL FROM THE MYCELIA OF AGARICUS BRASILIENSIS

筛选巴西蘑菇菌丝体醇提物中的抗肿瘤活性成分。巴西蘑菇深层发酵的菌丝体,在用热水提取出水溶性成分(主要是活性多糖)后,对其残渣用85%的乙醇提取,以S180荷瘤鼠为模型,对乙醇提取物进行抑瘤活性为导向的分级。先用丙酮、正己烷分步提取,再经硅胶柱层析进一步分级,并对分离出的高抑瘤活性组分,利用紫外、红外、质谱和NMR进行结构鉴定。根据抑瘤活性大小分步提取,最后经硅胶柱层析后,分离出6个组分,其中组分3抑瘤活性最强,腹腔注射(i.p.)50mg/kg/d,对S180荷瘤鼠的瘤重抑制率达78.30%。组分3在石油醚(60℃￣90℃)中反复结晶得淡黄色结晶体,经波谱解析,确定为麦角甾醇。巴西蘑菇菌丝体醇提物中的主要抗肿瘤活性成分是麦角甾醇。

To isolate and identify the antitumor constituents from the mycelia of Agaricus brasiliensis. After extraction with hot water, the residue of mycelia was further extracted with 85 % ethanol. The antitumor activity guided fractionation was carried out using the model of mice bearing Sarcoma 180. The ethanol extract was extracted with acetone and hexane consecutively, then fractionated by silica Gel column chromatography. The constituent with strongest antitumor activity was identified by means of UV, IR, MS and NMR respectively. Six fractions were isolated by silica Gel column chromatography. The fraction 3, having inhibition rate of 78.30 % against S180 tumor when intraperitoneally administered at the dose of 50 mg/ （kg·d）, is the strongest antitumor activity fraction. The fraction 3 was repeated recrystallized in petroleum ether （60℃-90 ℃） and the compound obtained was identified as ergosterol by spectral analysis. The main constituent with antitumor activity in ethanol extract of Agaricus brasiliensis mycelia is ergosterol.