Inhibition of intestinal motility and secretion by flavonoids in mice and rats: structure-activity relationships.
Intraperitoneal administration of some flavonoids (apigenin, flavone, kaempferol, morin, myricetin, naringin and rutin; 12.5-50 mg kg-1) significantly (P < 0.05-0.01) reduced small (28-69%) and large (83-134%) intestinal transit in mice. Other flavonoids (naringenin, silibinin, silymarin and taxifolin, 100-200 mg kg-1) reduced (23-41%; P < 0.05-0.01) intestinal transit at doses of 100-200 mg kg-1 while hesperitin, catechin and phloridzin (up to 200 mg kg-1) had no effect. This effect was antagonized by yohimbine (87-96%) and phentolamine (87-91%) but not by prazosin, propranolol, atropine, hexamethonium, mepyramine, cyproheptadine and naloxone. Yohimbine (92-96%) also antagonized the inhibitory effect of flavonols (12.5-50 mg kg-1) (P < 0.05-0.01) on intraluminal accumulation of fluid and diarrhoea induced by castor oil. By contrast, verapamil potentiated the flavonol effect. It is suggested that these effects, influenced by the structure of the molecules, are mediated by alpha 2-adrenergic receptors and calcium.
Di Carlo
G
G
Department of Experimental Pharmacology, University of Naples Federico II, Italy.
Autore
G
G
Izzo
A A
AA
Maiolino
P
P
Mascolo
N
N
Viola
P
P
Diurno
M V
MV
Capasso
F
F
D000818:Animals; D001826:Body Fluids / Q000502:physiology; D003967:Diarrhea / Q000139:chemically induced / Q000188:drug therapy; D004573:Electrolytes / Q000378:metabolism; D005419:Flavonoids / Q000494:pharmacology*; D005769:Gastrointestinal Motility / Q000187:drug effects*; D007413:Intestinal Mucosa / Q000187:drug effects / Q000378:metabolism; D007419:Intestinal Secretions / Q000187:drug effects*; D007420:Intestine, Large / Q000187:drug effects / Q000502:physiology; D008297:Male; D051379:Mice; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects; D012964:Sodium / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship
D004573:Electrolytes; D005419:Flavonoids; D011956:Receptors, Cell Surface; D012964:Sodium