Synthesis of Saccharumoside-B analogue with potential of antiproliferative and pro-apoptotic activities
| Autor: | Vijaya Rao Pidugu, Siddaiah Vidavalur, Sergey G. Klochkov, Anupam Bishayee, Kaladhar S. V. G. K. Dowluru, George E. Barreto, Dhananjaya Bhadrapura Lakappa, Sergey O. Bachurin, Gjumrakch Aliev, Mohammad Amjad Kamal, Ghulam Md Ashraf, Vadim V. Tarasov, Srinuvasarao Rayavarapu, Vladimir N. Chubarev, Mahaboob Basha, Nagendra Sastry Yarla, Sunanda Kumari Kadiri, Ramu Tadikonda |
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| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Science Antineoplastic Agents Apoptosis Article HeLa 03 medical and health sciences 0302 clinical medicine DU145 Cell Line Tumor Humans Cytotoxic T cell Medicine MTT assay Glycosides Cell Proliferation Multidisciplinary Molecular Structure Phenol biology business.industry Esters Cell cycle biology.organism_classification Publisher Correction Molecular biology 030104 developmental biology Biochemistry Cell culture 030220 oncology & carcinogenesis Cancer cell MCF-7 Cells business |
| Zdroj: | Scientific Reports Scientific Reports, Vol 7, Iss 1, Pp 1-14 (2017) |
| ISSN: | 2045-2322 |
| Popis: | A new series of phenolic glycoside esters, saccharumoside-B and its analogs (9b-9n, 10) have been synthesized by the Koenigs-Knorr reaction. Antiproliferative activities of the compounds (9b-9n, 10) were evaluated on various cancer cell lines including, MCF-7 breast, HL-60 leukemia, MIA PaCa-2 pancreatic, DU145 prostate, HeLa cervical and CaCo-2 colon, as well as normal human MCF10A mammary epithelial and human peripheral blood mononuclear cells (PBMC) by MTT assay. Compounds (9b-9n, 10) exhibited considerable antiproliferative effects against cancer cells with IC50 range of 4.43 ± 0.35 to 49.63 ± 3.59 µM, but they are less cytotoxic on normal cells (IC50 > 100 µM). Among all the compounds, 9f showed substantial antiproliferative activity against MCF-7 and HL-60 cells with IC50 of 6.13 ± 0.64 and 4.43 ± 0.35, respectively. Further mechanistic studies of 9f were carried out on MCF-7 and HL-60 cell lines. 9f caused arrest of cell cycle of MCF-7 and HL-60 cells at G0/G1 phase. Apoptotic population elevation, mitochondrial membrane potential loss, increase of cytosolic cytochrome c and Bax levels, decrease of Bcl-2 levels and enhanced caspases-9 and -3 activities were observed in 9f-treated MCF-7 and HL-60 cells. These results demonstrate anticancer and apoptosis-inducing potentials of 9f in MCF-7 and HL-60 cells via intrinsic pathway. |
| Databáze: | OpenAIRE |
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