The Constituents And Bioactivity Evaluation Of The Secondary Metabolites By Aspergillus Terreus 3.05358 And Neosartorya Spinosa

Microbial secondary metabolites have been proved to be an important source of lead compounds by its various structures, diverse biological activities and unique mechanism. In this thesis, two strains of fungi, Aspergillus terreus 3.05358 and Neosartorya spinosa, were chosen to study their secondary metabolites and biological activities.The thesis was devided into four chapters. In the first chapter, the progress on the study of Aspergillus sp. and macrocyclic trichothecene was reviewed. The significance of this research was then proposed.The second chapter concerned the extraction, purification and structural identification of secondary metabolites from these two strains. Six compounds were isolated from the wheat cultured Aspergillus terreus 3.05358. They were elucidated as amauromine B(1), a new diketopiperazine, and five known compounds(2?6). Their structures were elucidated by extensive spectroscopic techniques, including 2D-NMR and MS analysis, the absolute configuration of compound 1 was unambiguously established by single crystal X-ray diffraction analysis. Nine macrocyclic trichothecene compounds were isolated from the wheat cultured Neosartorya spinosa.The inhibitory effects on ?-glucosidase for compounds 1?6 were evaluated in the third chapter. The results showed that Amauromine B(1) and austalide N(3) exhibited more potent α-glucosidase inhibitory activities than positive control acarbose. In the fourth chapter, cytotoxicity evaluation of compounds 7?15 was reported. The cytotoxic activity for 7?15 was evaluated by the MTT method against human breast tumor cells(MDA-MB-231 cells), human hepatoma tumor cells(HepG 2), human lung tumor cells(A549), paclitaxel as positive control. The results showed that the macrocyclic trichothecene compounds were potent anti-tumor active, some of which are stronger than paclitaxel by 2 to 3 orders of magnitude.