title: The xanthones gentiacaulein and gentiakochianin are responsible for the vasodilator action of the roots of Gentiana kochiana.
abstract: Gentiana kochiana Perr. et Song. (Gentianaceae), a plant used in the traditional medicine of Tuscany (Italy) as antihypertensive remedy, exerts a vasodilator action on in vitro aortic rings that is probably linked to the blocking of the ryanodine-sensitive Ca++ channels. In the present study, three known xanthones were isolated from the crude methanolic extract of the roots: gentiacaulein, gentiakochianin, and swertiaperennin. The first two showed a vasorelaxing activity in rat aortic preparations, pre-contracted by 3 microM norepinephrine (pIC50 = 5.00 +/- 0.032 for gentiacaulein, pIC50 = 4.95 +/- 0.068 for gentiakochianin), 20 mM KCl (pIC50 = 4.90 +/- 0.15 for gentiacaulein; 4.59 +/- 0.069 for gentiakochianin), or 5 mM caffeine; on the contrary, in the same conditions, swertiaperennin did not show any vasodilator effect. In conclusion, gentiacaulein and gentiakochianin seem to be the compounds responsible for the vasorelaxing properties of the crude extract of Gentiana kochiana roots.
authors.affiliation: Dipartimento di Chimica Bioorganica, Università di Pisa, Pisa, Italy.
authors.forename: Silvio
authors.initials: S
authors.lastname: Chericoni
authors.forename: Lara
authors.initials: L
authors.lastname: Testai
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Calderone
authors.forename: Guido
authors.initials: G
authors.lastname: Flamini
authors.forename: Paola
authors.initials: P
authors.lastname: Nieri
authors.forename: Ivano
authors.initials: I
authors.lastname: Morelli
authors.forename: Enrica
authors.initials: E
authors.lastname: Martinotti
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D001011:Aorta / Q000187:drug effects*; D015220:Calcium Channels / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D030012:Gentiana; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D018517:Plant Roots; D051381:Rats; D017208:Rats, Wistar; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D044004:Xanthones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000959:Antihypertensive Agents; D015220:Calcium Channels; D010936:Plant Extracts; D014665:Vasodilator Agents; D044004:Xanthones; C479001:gentiacaulein; C479000:gentiakochianin; C009689:xanthone