Three new isocoumarin derivatives,(S)-6,8-dihydroxy-5-(methoxymethyl)-3,7-dimethylisochroman-1-one(1),(S)-6,8-dihydroxy-3,5,7-trimethyl-isochroman-1-one(2) and(R)-2-chloro-3-(8-hydroxy-6-methoxy-1-oxo-1 H-isochromen-3...Three new isocoumarin derivatives,(S)-6,8-dihydroxy-5-(methoxymethyl)-3,7-dimethylisochroman-1-one(1),(S)-6,8-dihydroxy-3,5,7-trimethyl-isochroman-1-one(2) and(R)-2-chloro-3-(8-hydroxy-6-methoxy-1-oxo-1 H-isochromen-3-yl) propyl acetate(3), along with four known compounds(4–7) were isolated from a mangrove endophytic fungus Penicillium sp. YYSJ-3. Their structures were established on the basis of the extensive spectroscopic data and HR-ESI-MS analysis. The absolute configurations of1–3 were further determined by X-ray diffraction analysis and optical rotations. Compounds 3, 6 and 7 showed promising inhibitory activity against α-glucosidase, which were stronger than that of the positive control 1-deoxynojirimycin(IC50 141.2 μmol·L-1).展开更多
Xylariaceae sp.QGS 01,an endophytic fungus isolated from the stem of Quercus gilva Blume showed high-glucosidase inhibitory activity.α-Glucosidase inhibitor have the role as one of carbohydrate-hydrolyzing enzymes to...Xylariaceae sp.QGS 01,an endophytic fungus isolated from the stem of Quercus gilva Blume showed high-glucosidase inhibitory activity.α-Glucosidase inhibitor have the role as one of carbohydrate-hydrolyzing enzymes to postpone absorption of glucose in the digestive organs.The α-glucosidase inhibitor constituents were isolated from the ethyl acetate extract of the mycellium of endophytic fungi Xylariaceae sp.QGS 01 using a bioassay-guided fractionation technique.Further separation and purification of the active fraction led to the isolation of constituents with strong inhibitory activities against-glucosidase:8-hydroxy-6,7-dimethoxy-3-methylisocoumarine(1)with inhibitory concentration(IC50)values against-glucosidase from Saccharomyces cerevisiae of 41.75μg/mL,while quercetin as the standard had an IC50 value of 4.80g/mL.The results of the present study showed that the endophytic fungus Xylariaceae sp.QGS 01 is potentially a rich source of antidiabetic medicine.展开更多
基金the National Natural Science Foundation of China (No. 21877133)Guangdong MEPP Fund (No. GDOE-2019A21)the Key Project of Natural Science Foundation of Guangdong Province (No. 2016A040403091) for generous support。
文摘Three new isocoumarin derivatives,(S)-6,8-dihydroxy-5-(methoxymethyl)-3,7-dimethylisochroman-1-one(1),(S)-6,8-dihydroxy-3,5,7-trimethyl-isochroman-1-one(2) and(R)-2-chloro-3-(8-hydroxy-6-methoxy-1-oxo-1 H-isochromen-3-yl) propyl acetate(3), along with four known compounds(4–7) were isolated from a mangrove endophytic fungus Penicillium sp. YYSJ-3. Their structures were established on the basis of the extensive spectroscopic data and HR-ESI-MS analysis. The absolute configurations of1–3 were further determined by X-ray diffraction analysis and optical rotations. Compounds 3, 6 and 7 showed promising inhibitory activity against α-glucosidase, which were stronger than that of the positive control 1-deoxynojirimycin(IC50 141.2 μmol·L-1).
文摘Xylariaceae sp.QGS 01,an endophytic fungus isolated from the stem of Quercus gilva Blume showed high-glucosidase inhibitory activity.α-Glucosidase inhibitor have the role as one of carbohydrate-hydrolyzing enzymes to postpone absorption of glucose in the digestive organs.The α-glucosidase inhibitor constituents were isolated from the ethyl acetate extract of the mycellium of endophytic fungi Xylariaceae sp.QGS 01 using a bioassay-guided fractionation technique.Further separation and purification of the active fraction led to the isolation of constituents with strong inhibitory activities against-glucosidase:8-hydroxy-6,7-dimethoxy-3-methylisocoumarine(1)with inhibitory concentration(IC50)values against-glucosidase from Saccharomyces cerevisiae of 41.75μg/mL,while quercetin as the standard had an IC50 value of 4.80g/mL.The results of the present study showed that the endophytic fungus Xylariaceae sp.QGS 01 is potentially a rich source of antidiabetic medicine.
