Marine microorganisms are the important resources for natural drug discovery. However, most of genes are usually in silent and could not express under the condition of traditional culture, which limits the discovery of lead compounds. In the present research, marine fungus <i>Schizophyllum</i> sp. YS-08 was selected as the research object, which was from Yellow Sea of China, to activate its silent genes by changing the medium of nutrients and environmental conditions. The crude extracts from metabolites of marine fungi were analyzed by HPLC, and their antioxidant activity and acetylcholinesterase (AChE) inhibitory activity were studied by DPPH radical-scavenging and Ellman's method, respectively. The results indicated that metabolic pathway of fungus was regulated effectively in different culture conditions, especially in the normal sea water medium with peptone. The antioxidant activity and AChE inhibitory activity increased significantly in comparison with wild strain and increase of the quantity of chemical constituents were even more. It is also observed that the strains showed relatively slow growth in the high salinity situation, while this adversely environmental condition could promote and produce more active metabolites. Furthermore, 6 mutant strains were obtained under salt stress and were identified. Interestingly, we found that all mutant strains had potency toward antioxidant and AChE inhibitory activity. Among them, YS-08-2 was the most potent, scavenging more than 56.02% towards DPPH free radicals, and YS-08-1, YS-08-4 and YS-08-5 exhibited more than 40% inhibition against AChE. HPLC analysis of extracts showed the metabolites of most fungi were more abundant after regulation of culture conditions.