Drotaverine - a Concealed Cytostatic!

  • Arch Pharm (Weinheim). 2017 Jan;350(1). doi: 10.1002/ardp.201600289.
Ioana Z Pavel  1  2 ,  Lucie Heller  3 ,  Sven Sommerwerk  3 ,  Anne Loesche  3 ,  Ahmed Al-Harrasi  4 ,  René Csuk  3
Affiliations
  • 1. Department of Pathophysiology, Victor-Babes-University of Medicine and Pharmacy, Timisoara, Romania.
  • 2. Department of Pharmacognosy, Victor-Babes-University of Medicine and Pharmacy, Timisoara, Romania.
  • 3. Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Halle (Saale), Germany.
  • 4. Chair of Oman's Medicinal Plants and Marine Natural Products, University of Nizwa, Birkat Al-Mauz, Nizwa, Sultanate of Oman.
PMID: 27879007 DOI: 10.1002/ardp.201600289
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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