细胞学方法评价苯甲醛类化合物寒热药性的构效关系

Evaluation of structure-activity relationship of benzaldehyde in cold and hot properties by cytological methods

目的:用细胞学方法评价苯甲醛类化合物的寒热药性,探讨化合物结构与其寒热药性之间的关系。方法:用噻唑蓝(MTT)比色法考察12种苯甲醛类化合物对HepG2细胞和MCF-7细胞体外增殖的影响,以确定它们的寒热药性。结果:苯甲醛、对氯苯甲醛、2-硝基苯甲醛、间硝基苯甲醛在0.1～50μg/mL浓度范围内对HepG2细胞和MCF-7细胞的生长增殖表现出抑制作用,随着浓度的增大,抑制率逐渐增大,判定为寒性;对羟基苯甲醛、2,4-二羟基苯甲醛、3,4-二羟基苯甲醛、3,4,5-三甲氧基苯甲醛、2,4,6-三甲氧基苯甲醛、香草醛、邻香草醛、异香草醛在0.1～50μg/mL浓度范围内对HepG2细胞和MCF-7细胞的生长增殖表现出低浓度促进,高浓度抑制,判定为热性。结论:化合物的寒热药性是由其结构决定的。苯甲醛为基本结构显寒性,吸电子基取代使其寒性增强,给电子基取代使其显热性。

Objective： To evaluate the cold-heat pharmacodynamics of benzaldehydes by cytological method, and to explore the relationship between the structure of benzaldehydes and their cold-heat pharmacodynamics. Methods： The effects of 12 benzaldehydes on the proliferation of HepG2 cells and MCF-7 cells in vitro were investigated by MTT colorimetry to determine their cold-heat properties. Results： Benzaldehyde, p-chlorobenzaldehyde, 2-nitrobenzaldehyde and m-nitrobenzaldehyde inhibited the growth and proliferation of HepG2 cells and MCF-7 cells in the concentration range of 0.1-50g/mL. With the increase of concentration, the inhibition rate gradually increased and was judged to be cold; in the concentration range of 0.1- 50g/mL, p-hydroxybenzaldehyde, 2,4-dihydroxybenzaldehyde, 3,4-dihydroxybenzaldehyde, 3,4,5-trimethoxybenzaldehyde, 2,4,6-trimethoxybenzaldehyde, vanillin, o-vanillin and isovanillin promoted the growth and proliferation of HepG2 cells and MCF-7 cells at low concentration, and inhibited the growth and proliferation at high concentration. Conclusion： The hot and cold characteristics of compounds depending on their chemical structures. Benzaldehyde as the basic structure shows cold characteristics. The substituent of electron with drawing groups on the benzaldehyde enhance its cold characteristics. However, the substituent of electron donating groups on the benzaldehyde shows hot characteristics.