探讨SIOC-AA-005抗肿瘤的作用机制.采用测定HT-29 细胞线粒体膜流动性、线粒体ATP含量、线粒体ATP酶活性及NADH-CoQ氧化还原酶活性、细胞质膜NADH氧化酶活性的方法,对其作用机制进行了深入探讨;SIOC-AA-005在10 nmol/L剂量下可明显降低线粒体膜的流动性,并使线粒体膜电位显著升高;在此浓度下,SIOC-AA-005还可使HT-29细胞内的ATP耗竭,ATP酶活性受到抑制,线粒体中能量产生过程受阻.在胞外反应体系中,SIOC-AA-005对NADH-CoQ氧化还原酶有强烈的抑制作用,对细胞质膜NADH氧化酶也具有较强的抑制作用.SIOC-AA-005可能是通过抑制线粒体NADH-CoQ氧化还原酶、抑制细胞质膜NADH氧化酶以及线粒体ATP酶活性,从而使线粒体膜流动性下降,膜电位升高,细胞内ATP耗竭,最终使肿瘤细胞死亡.

Bio-activities of 21 kinds of compounds of spiro enol ether derivatives against the2nd instar larvae of Plutella xylostella were tested for antifeedant activity.Antifeedant activity ofcompound No.8,No.12 and No.20 against 4th larvae of P.xylostella,effects of compoundNo.20 on cuticle and blood cell of 4th instar larvae of Pieris rapae,and control effect of com-pound No.20 against larvae of P.rapae were studied.Antifeedant activity of compound No.8,No.12,No.16 and No.20 against larvae of P.xylosteUa were better than those of others.AFC_(50) of compound No.8,No.12 and No.20 in non-selective test against 4th instar larvae ofP.xylostella were 549.03μg/mL,405.97μg/mL and 205.06μg/mL after 24h treatment,andAFC_(50) in selective test were 432.57μg/mL,114.34μg/mL and 72.32μg/mL.AFC_(50) of com-pound No.12,No.20 in selective test against 4th instar larvae of P.rapae were 398.88μg/mLand 280.54μg/mL,respectively,and AFC_(50) of compound No.20 in non-selective test was112.76μg/mL after 24h treatment.Compound No.20 could reduce the content of cuticle andamount of blood cell of 4th instar larvae of P.rapae.Field trial showed that control efficacy ofcompound No.20 at concentration of 800μg/mL against larvae of P.rapae were 28.60%,54.93% and 58.21% 3d,5d and 7d after treatment.

A study of the bioactivity of2 kinds of spiro enol ether analogues against Pieris rapae slowed that AFC5o in choice test of compounds No. 12 and No.20 against the 4th instar larvae of P. rapae within 24 h was 398.88 mg/L and 280.54mg/L, respectively. The two compounds significantly reduced the weight of the larvae and the pupae of the pest and decreased the eclosion rate of its adults.