Drotaverine - a Concealed Cytostatic!

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Pavel IZ, Heller L, Sommerwerk S, Loesche A, Al-Harrasi A, Csuk R

Drotaverine - a Concealed Cytostatic!

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

PubMed ID
27879007 [ View in PubMed
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Abstract

Drotaverine (also known as dihydroperparine or No-Spa((R)) ) 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 muM 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.

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