Main constituents of a commercial Drosera fluid extract and their antagonist activity at muscarinic M3 receptors in guinea-pig ileum.
The range of known constituents of Drosera species is extended by identification of myricetin 3-O-galactoside, from D. madagascariensis, and (+)-cis-isoshinanolone, obtained from a commercial fluid extract. They are accompanied by the naphthoquinones droserone and plumbagin, typical of this taxon, and a series of ubiquitous flavonols, including the rarely found gossypitrin present in the latter source. Conspicuously, the commercial form of D. peltata, non-accepted by the commission E, was found to be devoid of flavonoids. In addition, the fortuitous availability of the authentic enigmatic sample 'CON', previously isolated from D. rotundifolia, led to its characterization as common quercetin. Experiments performed on isolated guinea-pig ileum demonstrated that quercetin respectively 'CON' moderately inhibited carbachol-induced contractions at 10 microM (pD'2 5.09 +/- 0.02), while (+)-cis-isoshinanolone (100 microM) was inactive. This result indicates that quercetin derivatives may well contribute to the therapeutic use of Drosera preparations.
Kolodziej
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H
Institut für Pharmazie, Pharmazeutische Biologie, Freie Universität Berlin, Berlin, Germany. kolpharm@zedat.fu-berlin.de
Pertz
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HH
Humke
A
A
D000465:Algorithms; D000818:Animals; D002217:Carbachol / Q000494:pharmacology; D029787:Drosera / Q000737:chemistry*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D018721:Muscarinic Agonists / Q000494:pharmacology; D018727:Muscarinic Antagonists / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D009130:Muscle, Smooth / Q000187:drug effects*; D010936:Plant Extracts / Q000032:analysis / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry*; D043587:Receptor, Muscarinic M3; D011976:Receptors, Muscarinic / Q000187:drug effects*
D018721:Muscarinic Agonists; D018727:Muscarinic Antagonists; D010936:Plant Extracts; D043587:Receptor, Muscarinic M3; D011976:Receptors, Muscarinic; D002217:Carbachol