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本文用消旋棉酚及其旋光异构体比较研究了对纯化小鼠肝脏LDH-A_4,心脏LDH-B_4和睾丸LDH-C_4的抑制作用。其抑制程度与实验温度和棉酚剂量有关。37℃时的抑制作用比25℃时强得多。棉酚低浓度(1～4μM)时三种酶对同一种棉酚的反应有明显的不同,而在较高棉酚浓度(20～100μM)时棉酚对三种酶的抑制作用大体相同。对同一种酶来说,消旋棉酚,右旋棉酚和左旋棉酚对LDH的抑制作用并无差异。结论是,棉酚及其旋光异构体并不特异地抑制LDH-C_4,而在离体试验中,不能反映棉酚在体内试验中所表现的光学立体结构特异性。
In this paper, the inhibitory effects of purified racemic gossypol and its optical isomers on the purified mouse liver LDH-A_4, cardiac LDH-B_4 and testis LDH-C_4. The degree of inhibition is related to the experimental temperature and the dose of gossypol. The inhibition at 37°C is much stronger than at 25°C. At low concentrations of gossypol (1 to 4 μM), the reactions of the three enzymes to the same gossypol were significantly different, whereas at higher concentrations of gossypol (20 to 100 μM), the inhibitory effects of gossypol on the three enzymes were approximately the same. For the same enzyme, there was no difference in the inhibitory effect of racemic gossypol, d-gossypol, and l- gossypol on LDH. In conclusion, gossypol and its optical isomers do not specifically inhibit LDH-C4, but in vitro experiments do not reflect the optical stereostructure specificity of gossypol in vivo tests.