Abstract:
:We have recently shown that covalent attachment of the nitric oxide (NO) moiety to the HIV protease inhibitor Saquinavir (Saq) produced a qualitatively new chemical entity, named Saquinavir-NO (Saq-NO), with enhanced anticancer properties and reduced toxicity both in vitro and in vivo. The aim of this study was to address several unanswered questions both on the pharmacological profile of Saq-NO as well as on the in vivo role of NO in the oncogenesis of A375 human melanoma cells. To this end, we have evaluated here the impact of single and combined effects of Saq-NO, Saq, the NO-donor DETA NONOate and the iNOS inhibitor L-NAME on the in vitro as well as in vivo growth of the iNOS positive A375 cells. Our data confirm clear-cut evidence for a strong and powerful anti-melanoma action of Saq-NO that is not duplicable by the combined use of Saq and DETA NONOate. Surprisingly, but also in agreement with the complex and multifaceted role of endogenous NO in A375 cells, both DETA NONOate and L-NAME significantly suppressed the in vivo growth of xenotransplants.
journal_name
Oncol Repjournal_title
Oncology reportsauthors
Donia M,Mangano K,Fagone P,De Pasquale R,Dinotta F,Coco M,Padron J,Al-Abed Y,Giovanni Lombardo GA,Maksimovic-Ivanic D,Mijatovic S,Zocca MB,Perciavalle V,Stosic-Grujicic S,Nicoletti Fdoi
10.3892/or.2012.1840subject
Has Abstractpub_date
2012-08-01 00:00:00pages
682-8issue
2eissn
1021-335Xissn
1791-2431journal_volume
28pub_type
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