2. Academic Validation
  3. An investigation of in vitro cytotoxicity and apoptotic potential of aromatic diselenides

An investigation of in vitro cytotoxicity and apoptotic potential of aromatic diselenides

  • Bioorg Med Chem Lett. 2014 Aug 1;24(15):3440-6. doi: 10.1016/j.bmcl.2014.05.075.
Masood Ahmad Rizvi 1,  Santosh Guru 2,  Tahira Naqvi 3,  Manjeet Kumar 4,  Navanath Kumbhar 5,  Showkat Akhoon 3,  Shazia Banday 3,  Shashank K Singh 2,  Shashi Bhushan 2,  G Mustafa Peerzada 3,  Bhahwal Ali Shah 6
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Kashmir, Hazratbal, Srinagar 190006, J&K, India. Electronic address: masoodku2@gmail.com.
  • 2 Division of Cancer Pharmacology, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India.
  • 3 Department of Chemistry, University of Kashmir, Hazratbal, Srinagar 190006, J&K, India.
  • 4 Natural Product Chemistry Division, CSIR-Indian Institute of Integrative Medicine (IIIM), Canal Road, Jammu Tawi 180001, India.
  • 5 Institute of Bio-Informatics and Biotechnology, University of Pune, Ganeshkhind Road, Pune 411007, India.
  • 6 Natural Product Chemistry Division, CSIR-Indian Institute of Integrative Medicine (IIIM), Canal Road, Jammu Tawi 180001, India. Electronic address: bashah@iiim.res.in.
PMID: 24961641 DOI: 10.1016/j.bmcl.2014.05.075
Abstract

A target synthesis of a library of symmetric aromatic diselenides was attempted with the aim of generating Anticancer lead compounds. Out of thirteen screened molecules (1-13) against a panel of human Cancer cell lines, compound 8 exhibited highest cell growth inhibition in Human leukemia HL-60 cells with IC50 value of 8 μM. Compound 8 had a good pro-apoptotic potential as evidenced from several apoptotic protocols like DNA cell cycle analysis and monitoring of apoptotic bodies formation using phase contrast and nuclear microscopy with Hoechst 33,258. Also, 8 significantly inhibits S phase of the cell cycle and eventually trigger Apoptosis in HL-60 cells through mitochondrial dependent pathway substantiated by the loss of mitochondrial potential. A theoretical investigation of DNA binding ability of 8 showed that it selectively bind to minor groove of DNA, where it is stabilized by hydrogen bonding and hydrophobic interactions.

Keywords

Anti-cancer; Apoptosis; DNA-binding; Diselenides; In silico.

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