细胞学方法评价苯甲醛类化合物寒热药性的构效关系
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摘要
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 0.1-50 g/mL. With the increase of concentration, the inhibition rate gradually increased and was judged to be cold; in the concentration range of 0.1-50 g/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.
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 0.1-50 g/mL. With the increase of concentration, the inhibition rate gradually increased and was judged to be cold; in the concentration range of 0.1-50 g/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.
引文
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[13]王征,张宁,王翠玲,等.热者寒之细胞中药学初探.吉林中医药,2015,35(12):1255-1259
[14]张宁,王征,王征帆,等.细胞中药学初探之寒者热之.西北大学学报(自然科学版),2016,46(1):7-11
[15]王征,刘建利,王翠玲,等.用两种细胞评价中药白薇寒热药性.中华中医药杂志,2016,31(4):1383-1385
[16]王征,刘建利,王翠玲,等.丹参寒热药性的实验评价.长春中医药大学学报,2016,32(1):37-39
[17]王征,刘建利,唐志书,等.千年健寒热药性的实验评价.长春中医药大学学报,2016,32(2):266-268
[18]张宁,成程,李红民,等.用细胞学方法评价5种中药复方的寒热药性.中华中医药杂志,2016,31(3):79-82
[19]王征,武雪,刘建利,等.川乌和附子的毒性与热性的细胞实验研究.长春中医药大学学报,2016,32(3):582-584
[2]王厚伟,窦彦玲.基于系统分离的中药及其组分寒热药性矩阵判别与应用研究.山东中医药大学学报,2012,36(3):179-180
[3]梁月华.寒热本质研究进展.中医杂志,1996,37(12):747-750
[4]余惠曼,周红祖,肖小河,等.中药四性的研究进展与展望.中国中医基础医学杂志,2001,7(8):621-624
[5]袁永明,陈晓,潘志强,等.寒证热证大鼠模型的红外热图研究.辽宁中医杂志,2008,35(5):85-78
[6]程薇薇,刘建利,张宁,等.评价中药寒热药性的实验方法研究.中草药,2010,41(7):1122-1126
[7]王征,张宁,成程,等.采用两种细胞模型评价野菊花的寒热属性.中草药,2012,43(8):1586-1589
[8]王征,张宁,孙艳妮,等.白头翁寒热药性的试验评价.药物评价研究,2013,36(5):359-362
[9]王思文,张宁,于涛,等.细胞学方法评价9种抗溃疡药的寒热药性.西北大学学报(自然科学版),2014,44(3):444-450
[10]杨花,张宁,王征,等.用细胞学方法评价12种降压药的寒热药性.药物评价研究,2014,37(3):222-237
[11]王思文,刘建利.用细胞学方法评价10种抗生素的寒热药性.西安交通大学学报(医学版),2015,36(3):408-413
[12]王思文,刘建利.用细胞学方法评价7种抗心律失常西药的寒热药性.中华中医药杂志,2015,30(4):1053-1057
[13]王征,张宁,王翠玲,等.热者寒之细胞中药学初探.吉林中医药,2015,35(12):1255-1259
[14]张宁,王征,王征帆,等.细胞中药学初探之寒者热之.西北大学学报(自然科学版),2016,46(1):7-11
[15]王征,刘建利,王翠玲,等.用两种细胞评价中药白薇寒热药性.中华中医药杂志,2016,31(4):1383-1385
[16]王征,刘建利,王翠玲,等.丹参寒热药性的实验评价.长春中医药大学学报,2016,32(1):37-39
[17]王征,刘建利,唐志书,等.千年健寒热药性的实验评价.长春中医药大学学报,2016,32(2):266-268
[18]张宁,成程,李红民,等.用细胞学方法评价5种中药复方的寒热药性.中华中医药杂志,2016,31(3):79-82
[19]王征,武雪,刘建利,等.川乌和附子的毒性与热性的细胞实验研究.长春中医药大学学报,2016,32(3):582-584