红缘拟层孔菌子实体中抗肿瘤活性成分研究

目的对红缘拟层孔菌Fomitopsis pinicola子实体的石油醚提取物、氯仿提取物、水层提取物和氯仿提取物中获得的化合物A(3-乙酰氧基-8,24-羊毛甾二烯-21-酸)进行了体内外抗肿瘤活性和细胞凋亡实验研究。方法通过测定脾脏指数、胸腺指数以及血清中白介素-2(IL-2)的含量,检测了各提取物对荷瘤小鼠免疫功能的影响。结果氯仿提取物和化合物A对H22荷瘤小鼠具有较高的抑瘤率,当氯仿提取物剂量为200 mg.kg-1.d-1时,抑瘤率为52.97%,胸腺指数明显高于对照组和环磷酰胺(CTX)组(P<0.05),而接近于正常组(P>0.05);脾脏指数接近于对照组和CTX组而明显高于正常组(P<0.01);IL-2的含量明显升高;化合物A具有较好的抗肿瘤作用,各剂量组之间存在良好的剂量关系;且同对照组相比存在显著性差异(P<0.01);在剂量为10mg.kg-1.d-1时,抑瘤率最高可达到52.31%。体外实验研究结果表明化合物A对人肝癌细胞SMMC-7721和人乳腺癌细胞MCF-7均具有良好的抑制作用,其抑制率最大分别为77.63%和90.29%,IC50分别为213.80μg/ml和123.03μg/ml。化合物A作用后的细胞凋亡率仅为23.2%,接近阴性对照组的20.9%,促进细胞凋亡效果不明显。结论结合体内外实验可推断化合物A(3-乙酰氧基-8,24-羊毛甾二烯-21-酸)为红缘拟层孔菌抗肿瘤活性成分之一,提高机体免疫活性可能是其抗肿瘤作用的机理之一。

Antitumor Active Constituent in Fruiting Body of Fomitopsis pinicola

Objective In this paper,the antitumor activities of extracts of petroleum,chloroform,water and compound A(3-acetoxylanosta-8,24-dien-21-oic acid) which were isolated from chloroform extract were studied,the anti-tumor activities of the three extracts and the monomer compound were studied in vivo and vitro. Methods Effects of extracts on immune organ in H22 mice were detected with measuring the thymus index,spleen index and IL-2 levels. Results The results showed that the chloroform extract and compound A had a higher inhibition rate.The inhibition rate was 52.97% on the dose of 200mg/kg/d.The thymus index of chloroform was significantly higher than those of the control and CTX groups(P>0.05),closing to the normal group(P>0.05).The spleen index was significantly higher than the normal group(P<0.01),closing to the control and CTX groups(P<0.01).The contents of IL-2 increased significantly.Compound A had better antitumor effect in vivo,showing a good dose relationship.Compared with the control group,there were significant differences(P<0.01).The inhibitory rate was 52.31% on the dose of 10mg/kg/d.Compound A could improve the immunity and increase the content of IL-2.And more,the results indicated that Compound A had good effect on human liver cancer cell SMMC-7721 and human breast cancer cells MCF-7 in vitro.The max inhibition rate were 77.63% and 90.29%,the median effective dose was 213.80 μg/ml and 123.03μg/ml.The apoptosis rate of cancer cell of compound A was only 23.2%,close to 20.9% of the negative control group,promote cell apoptosis effect was not obvious. Conclusion Based on the experimental results in vivo and in vitro,compound A is determined as one of the compositions of antitumor of Fomtopsis pinicola.The antitumor effect may realize by increasing the body’s immune activity.