华泽兰内生真菌Septoriella phragrnitis次级代谢产物及其生物活性研究OA北大核心CSTPCD

To study the chemical constituents and biological activities of the endophytic fungus Septoriella phragmitis,Silica gel column chromatography,semi-preparative high performance liquid chromatography and other methods were used to isolated and purified compounds.Modern spectrum technologies were applied to identify the structures of thoese isolated compunds.As a result,ten compounds were isolated from the extract of Septoriella phragmitis for the first time,named β-adenosine(1),cy-clo-(S-Pro-S-Ile)(2),5-hydroxy-2-methylol-4H-pyrane-4-ketone(3),3α-hydroxyartemisinic acid(4),leptosphaerone C(5),5,6,7,8-tetrahydronaphthalen-1-amine(6),euparin(7),tryptophan(8),cyclo-(Ala-Tyr)(9),β-D-fructopyranocy-(2→6)-D-glucopyranose(10).The α-glucosidase inhibitory activity of the obtained compounds was determined by p-nitro-phenyl-β-galactopyranoside method,the PTP1B inhibitory activity was determined by p-nitrophenyl phosphate method,the in-hibitory activity of gastric cancer cell HGC-27 was determined by MTT method,and the molecular docking was performed by standard precision docking method.Compounds 6 and 7 showed α-glucosidase inhibitory activity with IC50values of 8.1 and 8.6 μg/mL,respectively.Compounds 6,7 and 9 showed PTP1B inhibitory activity with IC50 values of 6.5,8.2 and 0.5μg/mL,respectively.Compounds 5 and 6 showed inhibitory activity against gastric cancer cell HGC-27 with IC50 values of 12.2 and 16.8 μg/mL,respectively.Molecular docking showed that compounds 6 and 7 had a strong correlation with α-gluco-sidase and PTP1B protein,which could be used as anti-diabetic lead compounds for subsequent research.