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目的:探讨三种生物黄酮类化合物在棉酚诱发低血钾中的作用.方法:从豚鼠肾脏制备11β-羟甾脱氢酶,NAD为辅酶,加入待测化合物,37℃反应一小时后提取甾体,反相高压液相测定酶活性,热辐射图像法分析药物相互作用.结果:所试生物黄酮类化合物均能抑制11β-羟甾脱氢酶,其IC_(50)(95％可信限)分别为:槲皮素164(7-341)μmol/L,桑色素 913(385-2173)μmol/L,柑桔素2193 (1114-4315)μmol/L.当11β-羟甾脱氢酶分别用槲皮素,红桔素,桑色素,柑桔素加上棉酚处理时,其C1值分别为:0.92、0.85、0.98和1.01,结论:三种生物黄酮类化合物与棉酚在抑制11β-羟甾脱氢酶中具有协同或相加作用.
OBJECTIVE: To investigate the effects of three flavonoids in gossypol-induced hypokalemia.Methods: 11β-hydroxysteroid dehydrogenase (NAD) was prepared from the guinea pig kidney and NAD was added as the coenzyme. The reaction mixture was incubated at 37 ℃ for one hour. Steroids, reverse-phase high-pressure liquid phase determination of enzyme activity, thermal radiation image analysis of drug interactions.Results: All the tested bioflavonoids can inhibit 11β-hydroxy steroid dehydrogenase, IC 50 (95% confidence Respectively, quercetin 164 (7-341) μmol / L, morin 913 (385-2173) μmol / L, citrus fruit 2193 (1114-4315) μmol / L. When 11β-hydroxysteroid dehydrogenation When the enzyme was treated with quercetin, mandarin, morin, citrus and gossypol respectively, the C1 values were 0.92, 0.85, 0.98 and 1.01, respectively. Conclusion: The results of three bio-flavonoids and gossypol Inhibition of 11β-hydroxysteroid dehydrogenase has a synergistic or additive effect.