Drotaverine – a Concealed Cytostatic!. Issue 1 (23rd November 2016)

• Record Type: Journal Article
• Authors: Pavel, Ioana Z.; Heller, Lucie; Sommerwerk, Sven; Loesche, Anne; Al‐Harrasi, Ahmed; Csuk, René
• Is Part Of: Archiv der Pharmazie. Volume 350:Issue 1(2017)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2016-11-23
• Subjects: Cytostatic activity -- Drotaverine -- No‐Spa®; Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201600289
• Languages: English
• ISSNs: 0365-6233

Abstract

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. Abstract : Drotaverine, an antispasmodic drug related to papaverin, also acts as a cytostatic compound for several human tumor cell lines. Small structural changes led to reduced activity or complete loss of cytotoxicity. Drotaverine mainly acts as a cytostatic and only to a minor extent as a cytotoxic agent.