中国药师
中國藥師
중국약사
CHINA PHARMACIST
2015年
2期
197-200
,共4页
李喜平%徐艳娇%张程亮%向道春%冯承阳%刘东
李喜平%徐豔嬌%張程亮%嚮道春%馮承暘%劉東
리희평%서염교%장정량%향도춘%풍승양%류동
中药单体%羧酸酯酶%咪达普利%伊立替康
中藥單體%羧痠酯酶%咪達普利%伊立替康
중약단체%최산지매%미체보리%이립체강
Chinese medicine monomer%Carboxylesterases%Imidapril%Irinotecan
目的::初步考察5种中药成分黄芩苷、穿心莲内酯、橙皮苷、茶多酚及黄豆苷元在体外对羧酸酯酶1(CES1)和羧酸酯酶2(CES2)活性的影响。方法:采用CES1、CES2特异性探针咪达普利和伊立替康(CPT-11)及其代谢产物咪达普利拉和SN-38,在大鼠肝微粒体孵育体系中初步考察上述5种中药成分抑制两种CESs活性强度。结果:上述5种中药成分在100μmol ·L-1浓度下对CES1、CES2活性均无显著抑制作用(P<0.05)。结论:黄芩苷、穿心莲内酯、橙皮苷、茶多酚及黄豆苷元在体外不影响CESs活性,体内实验有待进一步开展。
目的::初步攷察5種中藥成分黃芩苷、穿心蓮內酯、橙皮苷、茶多酚及黃豆苷元在體外對羧痠酯酶1(CES1)和羧痠酯酶2(CES2)活性的影響。方法:採用CES1、CES2特異性探針咪達普利和伊立替康(CPT-11)及其代謝產物咪達普利拉和SN-38,在大鼠肝微粒體孵育體繫中初步攷察上述5種中藥成分抑製兩種CESs活性彊度。結果:上述5種中藥成分在100μmol ·L-1濃度下對CES1、CES2活性均無顯著抑製作用(P<0.05)。結論:黃芩苷、穿心蓮內酯、橙皮苷、茶多酚及黃豆苷元在體外不影響CESs活性,體內實驗有待進一步開展。
목적::초보고찰5충중약성분황금감、천심련내지、등피감、다다분급황두감원재체외대최산지매1(CES1)화최산지매2(CES2)활성적영향。방법:채용CES1、CES2특이성탐침미체보리화이립체강(CPT-11)급기대사산물미체보리랍화SN-38,재대서간미립체부육체계중초보고찰상술5충중약성분억제량충CESs활성강도。결과:상술5충중약성분재100μmol ·L-1농도하대CES1、CES2활성균무현저억제작용(P<0.05)。결론:황금감、천심련내지、등피감、다다분급황두감원재체외불영향CESs활성,체내실험유대진일보개전。
Objective:To evaluate the inhibitory effect of 5 Chinese herbal medicinal ingredients baicalin, andrographolide, hes-peridin, polyphenols and daidzein on the activity of carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2). Methods: The spe-cial probes respectively for CES1 and CES2, namely imidapril and CPT-11, imidaprilat and SN-38, were used to investigate the poten-tial effect of the above drugs on CES1 and CES2 in rat liver microsomes incubation system. Results:Compared with that in the control group, the activity of CES1 and CES2 was not significantly influenced by the above 5 Chinese herbal medicinal ingredients ( P <0. 05). Conclusion:Baicalin, andrographolide, hesperidin, polyphenols and daidzein exhibit no inhibitory effect against CES1 and CES2, and further studies should be conducted to confirm the effect in vivo.