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Synthesis of Saccharumoside-B analogue with potential of antiproliferative and pro-apoptotic activities

dc.contributor.authorRayavarapu S.
dc.contributor.authorYarla N.S.
dc.contributor.authorKadiri S.K.
dc.contributor.authorBishayee A.
dc.contributor.authorVidavalur S.
dc.contributor.authorTadikonda R.
dc.contributor.authorBasha M.
dc.contributor.authorPidugu V.R.
dc.contributor.authorDowluru K.S.V.G.K.
dc.contributor.authorLakappa D.B.
dc.contributor.authorKamal M.A.
dc.contributor.authorMd Ashraf G.
dc.contributor.authorTarasov V.V.
dc.contributor.authorChubarev V.N.
dc.contributor.authorKlochkov S.G.
dc.contributor.authorBarreto G.E.
dc.contributor.authorBachurin S.O.
dc.contributor.authorAliev G.
dc.date.accessioned2020-09-02T22:26:35Z
dc.date.available2020-09-02T22:26:35Z
dc.date.issued2017
dc.identifier10.1038/s41598-017-05832-w
dc.identifier.citation7, 1, -
dc.identifier.issn20452322
dc.identifier.urihttps://hdl.handle.net/20.500.12728/5968
dc.descriptionA 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. © 2017 The Author(s).
dc.language.isoen
dc.publisherNature Publishing Group
dc.titleSynthesis of Saccharumoside-B analogue with potential of antiproliferative and pro-apoptotic activities
dc.typeArticle


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