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Literature DB >> 25685308

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

Manish Singh¹, Sandhya Bansal¹, Somanath Kundu^1,2, Priyanshu Bhargava¹, Ashima Singh¹, Rajender K Motiani¹, Radhey Shyam³, Vedagopuram Sreekanth^1,2, Sagar Sengupta³, Avinash Bajaj¹.

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.

Entities: CellLine Chemical Disease Gene Species

Keywords: Amphiphiles; Anticancer activities; Bile acids; Cancer; Colon Cancer

Year: 2014 PMID： 25685308 PMCID： PMC4322782 DOI： 10.1039/C4MD00223G

Source DB: PubMed Journal: Medchemcomm ISSN： 2040-2503 Impact factor: 3.597

22 in total

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Review 9. Bile acids: regulation of synthesis.

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2. Lithocholic Acid Hydroxyamide Destabilizes Cyclin D1 and Induces G₀/G₁ Arrest by Inhibiting Deubiquitinase USP2a.

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