Identification of gallic acid based glycoconjugates as a novel tubulin polymerization inhibitors

Abstract

A novel class of gallic acid based glycoconjugates were designed and synthesized as potential anticancer agents. Among all the compounds screened, compound 2a showed potent anticancer activity against breast cancer cells. The latter resulted in tubulin polymerization inhibition and induced G2/M cell cycle arrest, generation of reactive oxygen species, mitochondrial depolarization and subsequent apoptosis in breast cancer cells. In addition, ultraviolet-visible spectroscopy and fluorescence quenching studies of the compound with tubulin confirmed direct interaction of compounds with tubulin. Molecular modeling studies revealed that it binds at the colchicine binding site in tubulin. Further, 2a also exhibited potent in vivo anticancer activity in LA-7 syngeneic rat mammary tumor model. Current data projects its strong candidature to be developed as anticancer agent.

Antifibrotic effects of gallic acid on hepatic stellate cells: In vitro and in vivo mechanistic study

“…In addition, 13 CNMR spectrum revealed five quaternary carbons at δ 121.4 (C-1), 109.8 (C-2, 6), 146.0 (C-3, 5), 140.3(C-4) and 167.3 (C = O). Based on the spectroscopic data and by comparing to the published literature, 38 this compound was identified as GA.…”

Discovery of 3,4,6-Triaryl-2-pyridones as Potential Anticancer Agents that Promote ROS-Independent Mitochondrial-Mediated Apoptosis in Human Breast Carcinoma Cells

“…Mitochondria are critical for regulation of cell death and the intrinsic apoptotic pathway is dependent on disruption of mitochondria . Treatment of MDA‐MB‐231 cells with compound 35 and analysis with Jc‐1 dye showed that compound 35 induced significant loss of mitochondrial membrane potential (Figure ) suggesting that compound 35 induced apoptosis involves mitochondrial dysfunction.…”

New piperidine derivative DTPEP acts as dual‐acting anti‐breast cancer agent by targeting ERα and downregulating PI3K/Akt‐PKCα leading to caspase‐dependent apoptosis

“…Tumour size and body weight were measured on every fifth day. Tumour volume was calculated using formula, V = [(Length) × (Width)2]/2 . Finally, tumours and other organs were collected in RNA later as well as 10% neutral‐buffered formalin while lungs were collected in Bouin's solution .…”