In vitro cytotoxic and toxicological activities of ethanolic extract of Kaempferia galanga Linn. and its active component,ethyl-p-methoxycinnamate, against cholangiocarcinoma  

作　　者：Porwornwisit Tritripmongkol Tullayakorn Plengsuriyakarn Mayuri Tarasuk Kesara Na-Bangchang 

机构地区：[1]Graduate Program in Bioclinical Sciences,Chulabhorn International College of Medicine,Thammasat University,Pathum Thani 12120,Thailand [2]Center of Excellence in Molecular Biology and Pharmacology of Malaria and Cholangiocarcinoma,Chulabhorn International College of Medicine,Thammasat University,Pathum Thani 12120,Thailand [3]Drug Discovery and Development Center,Office of Advanced Science and Technology,Thammasat University,Pathum Thani 12120,Thailand

出　　处：《Journal of Integrative Medicine》2020年第4期326-333,共8页结合医学学报（英文版）

基　　金：funded by Center of Excellence in Pharmacology and Molecular Biology of Malaria and Cholangiocarcinoma of Thammasat University;Thammasat University Research fund under the TU Research Scholar(Contract No.03/2561)。

摘　　要：Objective:To evaluate the cytotoxic,apoptotic,mutagenic and immunomodulatory activities of Kaempferia galanga Linn.(KG)extract and ethyl-p-methoxycinnamate(EPMC)in vitro.Methods:The present study investigated the cytotoxic[using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphe nyl-2-H-tetrazolium bromide test],apoptotic(using a mitochondrial membrane potential assay),mutagenic(using a micronucleus test)and immunomodulatory(using flow cytometry)activities of the ethanolic extract of KG and its bioactive component,EPMC,against two cholangiocarcinoma(CCA)cell lines,CL-6 and HuCCT1,and one normal human cell line,OUMS-36 T-1 F.Results:Both KG extract and EPMC exhibited moderate cytotoxic activity against both CCA cells.The cytotoxic activity was supported by their concentration-dependent induction of apoptosis.CL-6 was most sensitive(3–4 fold)and selective to 5-fluorouracil(5-FU),compared with KG extract and EPMC[median half inhibiting concentration(IC50)and selectivity index(SI)were 23.01 lg/mL and 17.32;78.41 lg/mL and 4.44;100.76 lg/mL and 2.20,respectively for 5-FU vs.KG extract vs.EPMC].HuCCT1 was relatively more sensitive and selective to 5-FU and EPMC than KG extract[median IC50 and SI were 66.03 lg/mL and6.04;60.90 lg/mL and 3.65;156.60 lg/mL and 2.23,respectively for 5-FU vs.EPMC vs.KG extract].EPMC produced relatively potent cytotoxic activity against polymorphonuclear cells(IC50=92.20 lg/mL).KG extract and EPMC exhibited concentration-dependent mutagenic activity,as well as inhibition of tumor necrosis factor-a and interleukin-6.Conclusion:Considering cytotoxic,apoptotic,immunomodulatory and mutagenic activities,further development of KG as a drug candidate is likely to focus on the oral pharmaceutical formulation of a standardized KG extract rather than isolated compounds.

关 键 词：Kaempferia galanga Linn. Cytotoxicity CHOLANGIOCARCINOMA MUTAGENICITY Apoptosis Immunomodulatory activity 

分 类 号：R285.5[医药卫生—中药学]