2. Academic Validation
  3. β-Ionone derived apoptosis inducing endoperoxides; Discovery of potent leads for anticancer agents

β-Ionone derived apoptosis inducing endoperoxides; Discovery of potent leads for anticancer agents

  • Eur J Med Chem. 2014 Nov 24:87:228-36. doi: 10.1016/j.ejmech.2014.09.049.
Vishal Sharma 1,  Ashun Chaudhry 2,  Gousia Chashoo 3,  Rohit Arora 2,  Saroj Arora 2,  Ajit K Saxena 3,  Mohan Paul S Ishar 4
Affiliations

Affiliations

  • 1 Bio-Organic and Photochemistry Laboratory, Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143 005, Punjab, India.
  • 2 Department of Botanical and Environment Sciences, Guru Nanak Dev University, Amritsar 143 005, Punjab, India.
  • 3 Indian Institute of Integrative Medicine, Cancer Pharmacology Division, Jammu 180 001, J & K, India.
  • 4 Bio-Organic and Photochemistry Laboratory, Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143 005, Punjab, India. Electronic address: mpsishar@yahoo.com.
PMID: 25259515 DOI: 10.1016/j.ejmech.2014.09.049
Abstract

A series of endoperoxides (3a-j) were synthesized and evaluated for cytotoxic activity against four human Cancer cell lines by using SRB dye assay. All the compounds displayed moderate to high cytotoxic effect against almost all investigational Cancer cells. Particularly, compounds bearing electron withdrawing groups such as nitro substituted compound 3j (IC50 = 0.001 μM) and fluoro substituted compound 3i (IC50 = 0.003 μM) showed comparatively more cytotoxic potential than standard drugs against lung Cancer cell line (A549). All synthesized endoperoxides (3a-j) were further evaluated for their apoptotic potential through various parameters such as flow-cytometric analysis of nuclear DNA, flow-cytometric determination of mitochondrial membrane potential (ΔΨm), spectrofluorimetric estimation of intracellular ROS level and Caspase-3 & 9 assays in treated lung Cancer cells (A549); results reveal that endoperoxides induce Apoptosis in Cancer cells via mitochondrial pathway.

Keywords

Anticancer activity; Apoptosis; Cytotoxic activity; Endoperoxides.

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