Cytotoxicity of constituents from Mexican propolis against a panel of six different cancer cell lines.
The cytotoxicity of 39 compounds, including eighteen flavonoids (flavanones, 1-10; flavones, 11-17; flavanol, 18), sixteen phenolic acid derivatives (aromatic acids, 19-24; aldehyde, 25; esters, 26-34) and five glycerides (35-39), isolated from Mexican propolis, were evaluated against a panel of six different cancer cell lines; murine colon 26-L5 carcinoma, murine B16-BL6 melanoma, murine Lewis lung carcinoma, human lung A549 adenocarcinoma, human cervix HeLa adenocarcinoma and human HT-1080 fibrosarcoma. A phenylpropanoid-substituted flavanol, (2R,3S)-8-[4-phenylprop-2-en-1-one]-4',7-dihydroxy-3',5-dimethoxyflavan-3-ol (18), showed the most potent cytotoxicity against A549 cells (IC50, 6.2 microM) and HT-1080 cells (IC50, 3.9 microM), stronger than those of the clinically used anticancer drug, 5-fluorouracil (IC50, 7.5 microM and 5.4 microM, respectively). Based on the observed results, the structure-activity relationships are discussed.
Institute of Natural Medicine, University of Toyama, 2630-Sugitani, Toyama 930-0194, Japan.
Feng
F
Li
Suresh
S
Awale
Yasuhiro
Y
Tezuka
Shigetoshi
S
Kadota
D000818:Animals; D000970:Antineoplastic Agents / Q000302:isolation & purification*; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D011429:Propolis / Q000737:chemistry*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D011429:Propolis