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Evaluation of the anticancer activity of a newly synthetic combretastatine analogue against hepatocellular carcinoma.
Author(s) -
ElMoselhy Mohamed A.,
Aboubakr Esam Mohamed,
Aly Omar Mohamed,
Taye Ashraf
Publication year - 2018
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.2018.32.1_supplement.836.13
Subject(s) - combretastatin , in vivo , hepatocellular carcinoma , chemistry , liver cancer , in vitro , pathology , cytotoxic t cell , medicine , tubulin , endocrinology , biology , biochemistry , microtubule , microbiology and biotechnology
Combretastatin A‐4 has been emerged as a promising vascular disrupting agent, which displayed potent cytotoxic activities against a wide range of human cancer cell lines. Therefore, the present study was conducted to evaluate the anticancer activity of a newly synthesized combretastatin A‐4 analogue (1‐(3,4‐Dimethoxyphenyl)‐N‐(2‐methoxyphenyl)‐5‐(3,4,5‐trimethoxyphenyl)‐1H‐1,2,4‐triazole‐3‐carboxamide) against hepatocellular carcinoma (HCC) both in vitro and in vivo. In vitro study used HepG2 cell lines to evaluate the cytotoxic (antitumour) activity, tubulin protein inhibition and cell cycle analysis. While, in vivo study used DENA + CCl 4 as a well‐established model for HCC induction in rats. Animal groups were divided as following: Normal non‐treated group, DENA + CCl 4 group, CA4‐P treated group and CA4‐P analogue treated group. The following parameters were determined: hepatic relative weight, number of hepatic nodules, relative volume of hepatic nodules, hepatic tissue content of tubulin, histopathological examination of the hepatic tissue, hepatic tissue lipid peroxidation, hepatic tissue carbonyl content, serum ALT, serum AST, hepatic tissue TNF‐α and hepatic AFP concentrations. CA4‐P analogue significantly decreased liver relative weight, number of hepatic nodules and there relative volumes, tubulin content of the hepatic tissue, GSH and AFP which were more pronounced than CA4‐P group. Whereas a marked increase in MDA, carbonyl content and TNF‐a inside hepatic tissue were observed in the CA4‐P analogue treated group, which were higher than CA4‐P group. In conclusion CA4‐P analogue has a potential anti‐cancer activity against hepatocellular carcinoma and this effect was more noticeable than its parent drug (CA4‐P). This abstract is from the Experimental Biology 2018 Meeting. There is no full text article associated with this abstract published in The FASEB Journal .