title: Drotaverine - a Concealed Cytostatic!
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 EC50values 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.
authors.affiliation: Department of Pathophysiology, Victor-Babes-University of Medicine and Pharmacy, Timisoara, Romania.|Department of Pharmacognosy, Victor-Babes-University of Medicine and Pharmacy, Timisoara, Romania.
authors.forename: Ioana Z
authors.initials: IZ
authors.lastname: Pavel
authors.affiliation: Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Halle (Saale), Germany.
authors.forename: Lucie
authors.initials: L
authors.lastname: Heller
authors.affiliation: Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Halle (Saale), Germany.
authors.forename: Sven
authors.initials: S
authors.lastname: Sommerwerk
authors.affiliation: Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Halle (Saale), Germany.
authors.forename: Anne
authors.initials: A
authors.lastname: Loesche
authors.affiliation: Chair of Oman's Medicinal Plants and Marine Natural Products, University of Nizwa, Birkat Al-Mauz, Nizwa, Sultanate of Oman.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Al-Harrasi
authors.affiliation: Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Halle (Saale), Germany.
authors.forename: René
authors.initials: R
authors.lastname: Csuk
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D002462:Cell Membrane / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D005347:Fibroblasts / Q000187:drug effects; D006801:Humans; D051379:Mice; D010208:Papaverine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D044005:Tetrahydroisoquinolines; C005317:drotaverin; D010208:Papaverine
keywords: Cytostatic activity; Drotaverine; No-Spa®