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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 dose of lithocholic acid-piperidine derivative is enough to reduce the tumor burden by 75% in tumor xenograft model.

SUBMITTER: Singh M 

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

REPOSITORIES: biostudies-literature

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

Singh Manish M   Bansal Sandhya S   Kundu Somanath S   Bhargava Priyanshu P   Singh Ashima A   Motiani Rajender K RK   Shyam Radhey R   Sreekanth Vedagopuram V   Sengupta Sagar S   Bajaj Avinash A  

MedChemComm 20141015 1

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 (<b>LCA-PIP<sub>1</sub></b> ) is ~10 times more  ...[more]

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