Isolation of new rotenoids from Boerhaavia diffusa and evaluation of their effect on intestinal motility.
A bioassay-guided separation of a methanolic extract obtained from the roots of Boerhaavia diffusa L. (Nyctaginaceae) allowed us to isolate five compounds belonging to the class of rotenoids: the known boeravinone D ( 1), boeravinone E ( 2), compound 5 and two novel compounds that we have named boeravinone G ( 3) and boeravinone H ( 4). The structures of the new molecules have been determined on the basis of their HR-EI-MS, (1)H- and (13)C-NMR and 2D-NMR (HMQC, HMBC) data. All the isolated rotenoids have been evaluated for their effect on intestinal motility in vitro. Three of them (boeravinone G, boeravinone E and compound 5) exhibited spasmolytic activity. Preliminary structure-activity relationships have been established highlighting the effect of substitutions on rings B and D.
Borrelli
Francesca
F
Dipartimento di Farmacologia Sperimentale, Università di Napoli Federico II, Via D. Montesano 49, 80131 Naples, Italy. franborr@unina.it
Milic
Natasa
N
Ascione
Valeria
V
Capasso
Raffaele
R
Izzo
Angelo A
AA
Capasso
Francesco
F
Petrucci
Francesca
F
Valente
Roberta
R
Fattorusso
Ernesto
E
Taglialatela-Scafati
Orazio
O
D000818:Animals; D004305:Dose-Response Relationship, Drug; D005769:Gastrointestinal Motility / Q000187:drug effects*; D006168:Guinea Pigs; D008297:Male; D039281:Nyctaginaceae; D010276:Parasympatholytics / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018517:Plant Roots
D010276:Parasympatholytics; D010936:Plant Extracts