title: Cytotoxic and apoptotic effects of synthetic benzochromene derivatives on human cancer cell lines.
abstract: With the aim of discovering potential cytotoxic agents, a series of benzochromene derivatives were screened for their cytotoxic activity against seven human cancer cell lines by standard 3-(4, 5-dimethyl thiazol)-2,5-diphenyl tetrazolium bromide (MTT) assay. Apoptosis, as the mechanism of cell death, was investigated morphologically by acridine orange/ethidium bromide staining and cell surface expression assay of phosphatidylserine by Annexin V-PE/7-AAD technique. The effects of compounds on reactive oxygen species (ROS) and nitric oxide (NO) generations in three human breast cancer cell lines were also studied. All compounds showed significant cytotoxic activity with inhibitory concentration (IC50) values in the micromolar range (4.6-21.5 μM). The results of apoptosis evaluation suggested that the cytotoxic activity of these compounds in breast cancer cells occurs via apoptosis. MCF-7 cell line showed higher levels of ROS and NO production after treatment with compounds. The increase in ROS production after 4 and 24 h indicated that one of the ways that these compounds can induce apoptosis is by increasing ROS generation. Cytotoxic and apoptotic effects of these compounds in human cancer cells indicated that they can be a good candidate for further pharmacological studies to discover effective anticancer agents.
authors.affiliation: Department of Biochemistry, Institute of Biochemistry and Biophysics, University of Tehran, Tehran, Iran.
authors.forename: Asma
authors.initials: A
authors.lastname: Kheirollahi
authors.forename: Mahboobeh
authors.initials: M
authors.lastname: Pordeli
authors.forename: Maliheh
authors.initials: M
authors.lastname: Safavi
authors.forename: Sara
authors.initials: S
authors.lastname: Mashkouri
authors.forename: M Reza
authors.initials: MR
authors.lastname: Naimi-Jamal
authors.forename: Sussan Kabudanian
authors.initials: SK
authors.lastname: Ardestani
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001578:Benzopyrans / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D009569:Nitric Oxide / Q000378:metabolism; D017382:Reactive Oxygen Species / Q000378:metabolism; D013997:Time Factors
chemical_list: D000970:Antineoplastic Agents; D001578:Benzopyrans; D017382:Reactive Oxygen Species; D009569:Nitric Oxide