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. 2017 Jan;350(1).
doi: 10.1002/ardp.201600289. Epub 2016 Nov 23.

Drotaverine - a Concealed Cytostatic!

Ioana Z Pavel  1   2 , Lucie Heller  3 , Sven Sommerwerk  3 , Anne Loesche  3 , Ahmed Al-Harrasi  4 , René Csuk  3
Affiliations

Drotaverine - a Concealed Cytostatic!

Ioana Z Pavel et al. Arch Pharm (Weinheim). 2017 Jan.

Abstract

Drotaverine (also known as dihydroperparine or No-Spa® ) is an antispasmodic drug closely related to papaverin. Drotaverin also acts as a cytostatic compound for several human tumor cell lines and nonmalignant mouse fibroblasts, and EC50 values as low as 3.0 μM were observed in SRB assays for HT-29 human colorectal carcinoma cells. Small structural changes (e.g., aromatization, benzylic oxidation) led to a reduced activity or a complete loss of cytotoxicity. Staining of the cells with acridine orange showed the cell membrane of the dead cells to be still intact, and a slight G1/G0 arrest in the treated cells was observed after 24 h. Extra annexin V-FITC/PI assays and flow cytometry revealed drotaverine mainly to act as a cytostatic and only to a minor extent as cytotoxic agent.

Keywords: Cytostatic activity; Drotaverine; No-Spa®.

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