title: 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 ofLCA-PIP1as compared to lithocholic acid is due to greater activation of apoptosis.LCA-PIP1induces sub G0arrest 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.
authors: The Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 180 Udyog Vihar, Phase 1, Gurgaon-122016, Haryana, India.
authors: Manish
authors: M
authors: Singh
authors: The Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 180 Udyog Vihar, Phase 1, Gurgaon-122016, Haryana, India.
authors: Sandhya
authors: S
authors: Bansal
authors: The Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 180 Udyog Vihar, Phase 1, Gurgaon-122016, Haryana, India.|Manipal University, Manipal, Karnatka, India.
authors: Somanath
authors: S
authors: Kundu
authors: The Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 180 Udyog Vihar, Phase 1, Gurgaon-122016, Haryana, India.
authors: Priyanshu
authors: P
authors: Bhargava
authors: The Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 180 Udyog Vihar, Phase 1, Gurgaon-122016, Haryana, India.
authors: Ashima
authors: A
authors: Singh
authors: The Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 180 Udyog Vihar, Phase 1, Gurgaon-122016, Haryana, India.
authors: Rajender K
authors: RK
authors: Motiani
authors: National Institute of Immunology, Aruna Asif Ali Marg, New Delhi 110067, India.
authors: Radhey
authors: R
authors: Shyam
authors: The Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 180 Udyog Vihar, Phase 1, Gurgaon-122016, Haryana, India.|Manipal University, Manipal, Karnatka, India.
authors: Vedagopuram
authors: V
authors: Sreekanth
authors: National Institute of Immunology, Aruna Asif Ali Marg, New Delhi 110067, India.
authors: Sagar
authors: S
authors: Sengupta
authors: The Laboratory of Nanotechnology and Chemical Biology, Regional Centre for Biotechnology, 180 Udyog Vihar, Phase 1, Gurgaon-122016, Haryana, India.
authors: Avinash
authors: A
authors: Bajaj
keywords: Amphiphiles; Anticancer activities; Bile acids; Cancer; Colon Cancer