Synthesis, Structure-Activity Relationship, and Mechanistic Investigation of Lithocholic Acid Amphiphiles for Colon Cancer Therapy.

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 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 charged head group. Lithocholic acid based amphiphile possessing piperidine head group (LCA-PIP₁ ) is ~10 times more cytotoxic as compared to its precursor. Biochemical studies revealed that enhanced activity of LCA-PIP₁ as compared to lithocholic acid is due to greater activation of apoptosis.LCA-PIP₁ induces sub G₀ arrest and causes cleavage of caspases. A single d

SUBMITTER: Singh M 

PROVIDER: S-EPMC4322782 | biostudies-literature | 2015 Jan

REPOSITORIES: biostudies-literature