This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic propert...This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic properties.Hypericum sampsonii was investigated,leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2),eight phenolic derivatives(3-10),and four terpene derivatives(11-14).The structures of compounds 1 and 2,featuring an unprecedented octahydro-2H-chromen-2-one ring system,were fully characterized using extensive spectroscopic data and quantum chemistry calculations.Six compounds(1,5-7,9,and 14)exhibited potential inhibitory effects against α-glucosidase,with IC_(50) values ranging from 0.050±0.0016 to 366.70±11.08μg·mL^(-1).Notably,compound 5(0.050±0.0016μg·mL^(-1))was identified as the most potential α-glucosidase inhibitor,with an inhibitory effect about 6900 times stronger than the positive control,acarbose(IC_(50)=346.63±15.65μg·mL^(-1)).A docking study was conducted to predict molecular interactions between two compounds(1 and 5)and α-glucosidase,and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed.展开更多
The total flavonoid contents in cultural materials and natural plant of Hypericum sampsonii Hance were analysed and comparedwith that in cultural materials of H. perforatum Linn. The results showed that the total flav...The total flavonoid contents in cultural materials and natural plant of Hypericum sampsonii Hance were analysed and comparedwith that in cultural materials of H. perforatum Linn. The results showed that the total flavonoid contents reached 5.416%-5.868% in H.sampsonii calli cultured for 30 d, which werehigher than that ofnatural plantof thisspecies (4.325%-4.527%) and approached to cultural materials of H. perforatum .展开更多
基金supported by the National Natural Science Foundation of China(No.32270413,U1812403)the Science and Technology Department of Guizhou Province(No.QKH 2020-1Z076)+5 种基金the 13th batch of Outstanding Young Scientific and Technological Talents in Guizhou Province(No.QKHPTRC[2021]5633)Cultivation project of National Natural Science Foundation of Guizhou Medical University(No.19NSP003)the Education Department of Guizhou Province(No.QJH KY[2021]189)the Natural Science Foundation of Guizhou Province(No.QKHZYD[2022]4015)High-level Innovative Talents in Guizhou Province(Thousand Levels of Talent for Chunmao Yuan in 2018)“Light of the West”Talent Cultivation Program of Chinese Academy of Sciences for Chunmao Yuan(No.RZ[2020]82).
文摘This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic properties.Hypericum sampsonii was investigated,leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2),eight phenolic derivatives(3-10),and four terpene derivatives(11-14).The structures of compounds 1 and 2,featuring an unprecedented octahydro-2H-chromen-2-one ring system,were fully characterized using extensive spectroscopic data and quantum chemistry calculations.Six compounds(1,5-7,9,and 14)exhibited potential inhibitory effects against α-glucosidase,with IC_(50) values ranging from 0.050±0.0016 to 366.70±11.08μg·mL^(-1).Notably,compound 5(0.050±0.0016μg·mL^(-1))was identified as the most potential α-glucosidase inhibitor,with an inhibitory effect about 6900 times stronger than the positive control,acarbose(IC_(50)=346.63±15.65μg·mL^(-1)).A docking study was conducted to predict molecular interactions between two compounds(1 and 5)and α-glucosidase,and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed.
文摘The total flavonoid contents in cultural materials and natural plant of Hypericum sampsonii Hance were analysed and comparedwith that in cultural materials of H. perforatum Linn. The results showed that the total flavonoid contents reached 5.416%-5.868% in H.sampsonii calli cultured for 30 d, which werehigher than that ofnatural plantof thisspecies (4.325%-4.527%) and approached to cultural materials of H. perforatum .
