本文对山西狭苞橐吾中倍半萜类化合物的生物学活性进行了筛选.用不同浓度的4种艾里莫芬烷型倍半萜干预携带有P53和SV40肿瘤病毒大T抗原基因的AH109菌液,采用酵母双杂交系统的β-半乳糖苷酶活力测定方法,分析了4种倍半萜对P53蛋白与SV40大T抗原之间相互作用力的影响.发现8β-methoxyeremophil-7(11) -ene-12,8α(4β,6α) -diolide(1)和8β-hydroxyl-6β-angloxyeremophil-7(11)-ene-12,8α-olide-15-oic acid (2)对P53蛋白及SV40 -大T抗原相互作用没有显著影响,但是中、高浓度的furanoeremophilan-4β,6α-oide(3)和低、中、高浓度的8β-hydroxyeremophil-7( 11) -ene-12,8α(4β,6α)-diolide (4)对P53蛋白与SV40大T抗原之间相互作用有抑制效应.说明从山西狭苞橐吾中提取出的化合物3和4对酵母双杂交系统中的P53和SV40-大T抗原的相互作用有生物学抑制活性.%To study the biological activity of sesquiterpene compounds from Ligularia intermedia Nakai of Shanxi. With different concentrations of four kinds of sesquiterpenes intervening AH109 bacteria solution which carries P53 and SV40 tumor virus large T-Antigen genes,we adopted yeast two-hybrid system method for determination of beta-galactose gluco-side enzyme activity to analyze the interaction effects on P53 protein and SV40 large T-antigen by the four compounds. The results indicated that 8β-methoxyeremophil-7 (11 )-ene-12,8α(4/3,6α)-diolide (1) and 8β-hydroxyl-6β-angloxyer-emophil-7(ll)-ene-12,8α-olide-15-oic acid (2) had no significant effects on the interaction between P53 protein and SV40-large T-antigen. However,medium and high concentrations of furanoeremophilan-4β,6α-olide (3 ), low, medium and high concentration of 8β-hydroxyeremophil-7 (11 )-ene-12,8α(4/3,6α)-diolide (4) had an inhibitory effects on the interaction between P53 protein and SV40 large T-antigen. It showed that compounds 3 and 4 which extracted from Ligularia intermedia Nakai of Shanxi had biological inhibitory activity effects on the interaction between P53 and SV40-large T-Antigen of the yeast two-hybrid system.
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