Twelve new grayanoids(1-12)along with five known compounds were isolated from flowers of Rhododendron molle.Their structures were fully characterized using a combination of spectroscopic analyses,computational calcula...Twelve new grayanoids(1-12)along with five known compounds were isolated from flowers of Rhododendron molle.Their structures were fully characterized using a combination of spectroscopic analyses,computational calculations,and single crystal X-ray diffraction.Rhomollone A(1)possesses an unprecedented 5/6/6/5 tetra-cyclic ring system(B-nor grayanane)incorporating a cyclopentene-1,3-dione scaffold.Rhodomollein XLIII(2)is a dimeric grayanoid,containing a novel 14-membered heterocyclic ring with a C2 symmetry axis.The antinociceptive activities of compounds 3,4,6,7,and 12-17 were evaluated by an acetic acid-induced writhing test.Among them,compounds 3,7,12,15 and 16 displayed significant antinociceptive activities at a dose of 20 mg/kg with inhibition rates ranging from41.9%to 91.6%.Compounds 6 and 13 inhibited 46.0%and 39.4%of the acetic acid-induced writhes at a dose of 2 mg/kg,while compound 17 inhibited 34.3%of the writhes at a dose of 0.4 mg/kg.展开更多
基金supported by grants from the National Natural Science Foundation of China(Nos.21572274 and 21732008)the CAMS Innovation Fund for Medical Sciences(No.2016-I2M1-010,China)
文摘Twelve new grayanoids(1-12)along with five known compounds were isolated from flowers of Rhododendron molle.Their structures were fully characterized using a combination of spectroscopic analyses,computational calculations,and single crystal X-ray diffraction.Rhomollone A(1)possesses an unprecedented 5/6/6/5 tetra-cyclic ring system(B-nor grayanane)incorporating a cyclopentene-1,3-dione scaffold.Rhodomollein XLIII(2)is a dimeric grayanoid,containing a novel 14-membered heterocyclic ring with a C2 symmetry axis.The antinociceptive activities of compounds 3,4,6,7,and 12-17 were evaluated by an acetic acid-induced writhing test.Among them,compounds 3,7,12,15 and 16 displayed significant antinociceptive activities at a dose of 20 mg/kg with inhibition rates ranging from41.9%to 91.6%.Compounds 6 and 13 inhibited 46.0%and 39.4%of the acetic acid-induced writhes at a dose of 2 mg/kg,while compound 17 inhibited 34.3%of the writhes at a dose of 0.4 mg/kg.
