In vitro anti-tumor activity of 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone against six established human cancer cell lines.
2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC), isolated from the buds of Cleistocalyx operculatus, was investigated in its cytotoxicity and its influence on six human cancer cell lines. Among SMMC-7721, 8898, HeLa, SPC-A-1, 95-D and GBC-SD cell lines, SMMC-7721 cells was the most sensitive one in these tested cell lines, with IC50 equal to 32.3 +/- 1.13 microM, EC50 equal to 9.00 +/- 0.36 microM and the therapeutic index equal to 3.59. Staining with Hoechst 33258 showed fragmentation and condensation of chromatin in the cells treated with 9 microM DMC for 48 h. Flow cytometric analysis was performed to determine hypodiploid cells. The results of flow cytometry assay indicated that the percentage of hypodiploid SMMC-7721 cells were 49.44 +/- 1.06% after 48 h treatment with 18.0 microM DMC. The treatment resulted in the appearance of a hypodiploid peak (A0 region), probably due to the presence of apoptosing cells and/or apoptotic bodies with DNA content less than 2n. To our knowledge, this is the first report on anti-tumor activity by DMC.
State Key Laboratory of Bioreactor Engineering, Institute of Biochemistry, East China University of Science and Technology, Shanghai 200237, PR China.
Chun-Lin
CL
Ye
Jian-Wen
JW
Liu
Dong-Zhi
DZ
Wei
Yan-Hua
YH
Lu
Feng
F
Qian
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002599:Chalcone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D047188:Chalcones; D004305:Dose-Response Relationship, Drug; D006801:Humans; D027822:Myrtaceae; D014410:Tumor Stem Cell Assay / Q000706:statistics & numerical data
C118962:2',6'-dihydroxy-4'-methoxychalcone; D000972:Antineoplastic Agents, Phytogenic; D047188:Chalcones; D002599:Chalcone