Singh, Manish and Bansal, Sandhya and Kundu, Somanath and Bhargava, Priyanshu and Singh, Ashima and Motiani, Rajender K. and Shyam, Radhey and Sreekanth, Vedagopuram and Sengupta, Sagar and Bajaj, Avinash (2015) Synthesis, structure–activity relationship, and mechanistic investigation of lithocholic acidamphiphiles for colon cancer therapy. Med. Chem. Commun., 6 (1). pp. 192-201. ISSN 2040-2503

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Abstract

We report a structure–activity relationship of lithocholic acid amphiphiles for their anticancer activities against colon cancer. We synthesized ten cationic amphiphiles, differing in nature of their cationic charged head groups, using lithocholic acid. We observed that anticancer activities of these amphiphiles against colon cancer cell lines are contingent on nature of the charged head group. The lithocholic acid-based amphiphile possessing a piperidine head group (LCA-PIP1) is ∼10 times more cytotoxic than its precursor. Biochemical studies revealed that enhanced activity of LCA-PIP1 compared to lithocholic acid is due to a greater activation of apoptosis. LCA-PIP1 induces sub G0 arrest and causes cleavage of caspases. A single dose of lithocholic acid–piperidine (LCA-PIP1) derivative is enough to reduce the tumor burden by 75% in a tumor xenograft model.

Item Type:	Article
Subjects:	Biochemical and Biophysical Sciences
Depositing User:	RCB Library
Date Deposited:	15 Nov 2017 12:02
Last Modified:	15 Nov 2017 12:02
URI:	http://rcb.sciencecentral.in/id/eprint/139

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