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

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

Abstract 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 PaC...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autores principales: Srinuvasarao Rayavarapu, Nagendra Sastry Yarla, Sunanda Kumari Kadiri, Anupam Bishayee, Siddaiah Vidavalur, Ramu Tadikonda, Mahaboob Basha, Vijaya Rao Pidugu, Kaladhar S. V. G. K. Dowluru, Dhananjaya Bhadrapura Lakappa, Mohammad A. Kamal, Ghulam Md Ashraf, Vadim V. Tarasov, Vladimir N. Chubarev, Sergey G. Klochkov, George E. Barreto, Sergey O. Bachurin, Gjumrakch Aliev
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2017
Materias:
Medicine
R
Science
Q
Acceso en línea:https://doaj.org/article/72d39702eeff4e1ea38b4f19a7576149
Etiquetas: Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
Descripción
Sumario:Abstract 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.

Ejemplares similares