Assessment of the Antitumor Potentiality of Newly Designed Steroid Derivatives: Pre-Clinical Study

Document Type: Research Articles

Authors

1 Department of Hormones, Medical Research Division, National Research Centre, Dokki, Giza, Egypt.

2 Department of Applied Medical Sciences, Community College in Al-Qurayyat, Al-Jouf University, KSA.

Abstract

Cancer is recognized as one of the most prevalent contributors to mortality in several nations and it remains one of
the common health issues globally. In particular, hepatocellular carcinoma (HCC) has become a public health problem
along with the increase of hepatitis B (HBV) and hepatitis C (HCV) virus infections. Based on this fact, our study
goaled to synthesize newly hybrid drugs containing heterocyclic rings incorporated to steroid moiety and to examine
the potential antitumor activity of the newly designed heterosteroid derivatives against HCC induced in animal model.
Several heterocyclic steroids were synthesized 2-7 and confirmed via the analytical and spectral data (IR, 1H NMR13C
NMR and Mass spectroscopy). Compounds 3, 4, and 5 were chosen to be investigated as anticancer agents in HCC rat
model by means of validated biomarkers (alfa –fetoprotein, endoglin, lipocali-2 and heat shock protein-70). Following
administration of compounds 3, 4 or 5, availability of the active tumor marker molecules was significantly dropped and
a substantial decrease of the angiogenic and inflammatory mediators was also evident. These findings were supported
by the histological examination of liver tissue. Taken together, this study indicates the potential anticancer activity
of the newly synthesized heterosteroid derivatives against HCC in vivo. The antitumor activity of these compounds
was likely attributable to modulating some signal transduction pathways involved in tumorigenesis, angiogenesis and
inflammation.

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