Phytochemical and Cytotoxic Evaluation of Peganum Harmala: Structure Activity Relationship Studies of Harmine

摘要

Four alkaloid constituents: harmine, vasicine, vasicinone and harmaline were isolated and characterized from Peganum harmala roots. Harmine showed the best cytotoxicity with IC50 of 32, 106, 45, 33 and 61 mu M against breast (HBL-100), lung (A549), colon (HT-29 & HCT-116) and cervical (HELA) cells respectively. The harmine analogs, synthesized via click chemistry, revealed that few derivatives possess potent cytotoxic effects. m-Fluoro phenyl-1, 2,3-triazolyl harmine was found to be selectively cytotoxic against human breast cancer cell lines only displaying an IC50 of 16 mu M. p-Fluoro phenyl-1,2,3-triazolyl harmine and p-methoxy phenyl-1,2,3-triazolyl harmine displayed improved cytotoxicity. p-Fluorophenyl-1,2,3-triazolyl harmine displayed broad spectrum cytotoxic effects against all the tested cancer-cell lines with IC50 of 17, 19, 29 and 17 mu M against lung (A-549), Colon (HT-29), Cervic (HELA) and Colon (HCT-116) cell lines respectively while as p-methoxy phenyl1,2,3- triazolyl harmine showed selectivity towards lung and colon cancer cell lines with IC50 of 27, 18 and 17mM against A549, HT-29 and HCT-116 respectively.