亮叶杨桐黄酮提取物抗瘤活性及其对小鼠p53基因表达活性的影响

ANTITUMOR ACTIVITIES OF FLAVONOIDS EXTRACTED FROM ADINANDRA NITIDA AND THEIR EFFECTS ON THE EXPRESSION OF p53 GENE IN MICE SARCOMA-180

本文从亮叶杨桐中分离提取出黄酮类生物活性物质,对进行小鼠体内抗肿瘤试验和小鼠S-180肿瘤细胞中p53基因表达抑制实验。研究结果表明,亮叶杨桐中总黄酮含量达28.4％,黄酮提取物在剂量50mg·kg^(-1)时对小鼠肉瘤S-180的抑瘤率为64.0％,对艾氏腹水癌(EAC)Ⅰ小鼠的生命延长率为51.2％,有显著的抗肿瘤作用,并且药效与用药量有关。同时发现,黄酮类提取物的抗肿瘤活性优于化疗药物呋喃氟尿嘧啶(Ftorafur)。RT-PCR实验结果表明,在剂量500mg·kg^(-1)时,黄酮类提取物可以明显抑制小鼠S-180肿瘤细胞中突变型p53基因的转录活性,其抑制程度和呋喃氟尿嘧啶相同。

Adinadra mtida Merr ex H. L. Li mainly distributes in southwestern China,is a valuable pharmaceutical wild plant. In this study, the biological active sustances flavonoids were extracted and isolated from this plant. The inhibition of tumor growth and inhibition of tumor oncosuppressor gene p53 at the transcriptional level in mice Sarcoma-180 cells were evaluated by antitumor assays and RT PCR respectively. The results indicated that the extracted substances not only significantly inhibit the growth of Sarcoma-180 cells implanted subcutaneously in mice but also incresse the life span in Ehrlich ascite carcinoma mice at the dose of 500mg/kg per day × 1 0 with no sign of toxicity. The ratio of tumor inhibition is 64. 0% in S-180 mice and the increase in life span(ILS) is about 51. 2% in Ehrlich ascite carcinoma mice. The effects appear to be dose-related. The antitumor activities of the extracted flavonoids are higher than the anticancer drug Ftorafur under the same condition. RT-FCR results showed that the extracted flavonoids can significantly inhibit the expression of the mutant p53 gene in mice Sarcomar-180 cells at the transcriptional level at the dose of 500mg/kg per day ×1 0. These re-suits suggest that the antitumor activities of extracted flavonoids may attributed to the interaction on certain oncogenes.