Carbazoles and imidazole represent two important classes of heterocycles which exhibit diverse biological activities such as antitumor properties. In this study, imidazole (C1-C3) and carbazole (C4 and C5) derivatives were evaluated for their cytotoxic activity against three human cancer cell lines namely, MCF7 (human breast cancer), HT29 (human colon cancer), and HeLa (human cervical cancer). Carbazole derivatives (C4 and C5) with IC50 < 10 µM showed greater cytotoxic effect than imidazole derivatives (C1-C3). Furthermore, all compounds exhibited better anticancer activity against MCF-7 than other two cell lines (HT-29, HeLa) and compound C4 was the most potent compound with the IC50 values of 2.5, 5.4 and 4.0 µM, against MCF-7, Hela and HT-29 cell lines, respectively. Physicochemical properties of compounds were calculated and their correlation with the IC50 values on MCF-7 cell line investigated. Surface area and polarizability of compounds showed good correlation by R2 = 0.8396 and R2 = 0.834, respectively. Docking studies of these compounds were also performed on the DNA as proposed target to comprehend their binding interactions and binding energies. The docking energy of compounds ranged from - 11.32 to -13.48 kcal/mol. Compound C3 with energy of -13.48 kcal/mol had the highest docking energy. Docking results indicated that these compounds (C1-C5) had strong affinity in binding to the DNA. KEY WORDS: Imidazole, Carbazole, Molecular docking, Cancer, MTT assay Bull. Chem. Soc. Ethiop. 2020, 34(2), 377-384 DOI: https://dx.doi.org/10.4314/bcse.v34i2.14
Honey has long been used in medicine for different purposes. Only recently, however, its antioxidant property and preventive effects against different diseases, such as cancer, have been highlighted. In this study, we investigated the potential of honey to induce cytotoxic and apoptosis effects in cultured carcinomic human prostate cells (PC-3), a commonly used cell culture system for in vitro studies on prostate cancer. The cells were cultured in Roswell Park Memorial Institute (RPMI) medium and treated with different concentrations of honey for three consecutive days. Cell viability was quantitated by MTT assay. Apoptotic cells were determined using Annexin-V-FITC by flow cytometry. Honey could decrease cell viability in malignant cells in a concentration and time-dependent manner. The IC 50 values against PC-3 were determined at 14.3, 9.2 and 4.3% after 24, 48 and 72 h, respectively. Honey induced apoptosis of PC-3 cells, as determined by flow cytometry histogram of treated cells which inducing apoptotic cell death is involved in honey toxicity. It might be concluded that honey could cause cell death in PC-3 cells, in which apoptosis plays an important role. Honey could also be considered as a promising chemotherapeutic agent in prostate cancer treatment in future.
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