Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Michelle Prudhomme  
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France

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Antineoplastic Activity of Monocrotaline Against Hepatocellular Carcinoma

Author(s): Sandeep Solmon Kusuma, Karunakar Tanneeru, Swroopa Didla, Bellary Nagaraju Devendra, Patnala Kiranmayi.

Graphical Abstract:


Abstract:

Plants are fantastic sources for present day life saving drugs. Monocrotaline a natural ligand exhibits dose-dependent cytotoxicity with potent antineoplastic activity. This study was intended to disclose the therapeutic potential of monocrotaline against hepatocellular carcinoma. The in silico predictions have highlighted the antineoplastic potential, druglikeness and biodegradability of monocrotaline. The in silico docking study has provided an insight and evidence for the antineoplastic activity of monocrotaline against p53, HGF and TREM1 proteins which play a threatening role in causing hepatocellular carcinoma. The mode of action of monocrotaline was determined experimentally by in vitro techniques such as XTT assay, NRU assay and whole cell brine shrimp assay have further supported our in silico studies. The in vitro cytotoxicity of monocrotaline was proved at IC50 24.966 µg/mL and genotoxicity at 2 X IC50 against HepG2 cells. Further, the credible druglike properties with non-mutagenicity, non-toxic on mammalian fibroblast and the potential antineoplastic activity through in vitro experimental validations established monocrotaline as a novel scaffold for liver cancer with superior efficacy and lesser side effects.

Keywords: DNA laddering, docking, monocrotaline, NRU assay and brine shrimp assay, PASS, XTT assay.

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Article Details

VOLUME: 14
ISSUE: 9
Year: 2014
Page: [1237 - 1248]
Pages: 12
DOI: 10.2174/1871520614666140715085907
Price: $58