Continued innovation in screening methodologies remains important for the discovery of high-quality multiactive fungi,which have been of great significance to the development of new drugs.Mangrove-derived fungi,which ...Continued innovation in screening methodologies remains important for the discovery of high-quality multiactive fungi,which have been of great significance to the development of new drugs.Mangrove-derived fungi,which are well recognized as prolific sources of natural products,are worth sustained attention and further study.In this study,118 fungi,which mainly included Aspergillus spp.(34.62%)and Penicillium spp.(15.38%),were isolated from the mangrove ecosystem of the Maowei Sea,and 83.1%of the cultured fungi showed at least one bioactivity in four antibacterial and three antioxidant assays.To accurately evaluate the fungal bioactivities,the fungi with multiple bioactivities were successfully evaluated and screened by principal component analysis(PCA),and this analysis provided a dataset for comparing and selecting multibioactive fungi.Among the 118 mangrove-derived fungi tested in this study,Aspergillus spp.showed the best comprehensive activity.Fungi such as A.clavatonanicus,A.flavipes and A.citrinoterreus,which exhibited high comprehensive bioactivity as determined by the PCA,have great potential in the exploitation of natural products and the development of new drugs.This study demonstrated the first use of PCA as a time-saving,scientific method with a strong ability to evaluate and screen multiactive fungi,which indicated that this method can affect the discovery and development of new drugs.展开更多
We previously isolated a natural product, namely guaiazulene-2,9-dione showing strong antibacterial activity against Vibrio anguillarum, from a gorgonian Muriceides collaris collected in South China Sea. In this exper...We previously isolated a natural product, namely guaiazulene-2,9-dione showing strong antibacterial activity against Vibrio anguillarum, from a gorgonian Muriceides collaris collected in South China Sea. In this experiment, guaiazulene-2,9-dione was quantitatively synthesized with an optimized one-step bromine oxidation method using guaiazulene as the raw material. The key reaction condition including reaction time and temperature, drop rate of bromine, concentration of aqueous THF solution, respective molar ratio of guaiazulene to bromine and acetic acid, and concentration of guaiazulene in aqueous THF solution, were investigated individually at five levels each for optimization. Combined with the verification test to show the absolute yield of each optimization step, the final optimal condition was determined as: when a solution of 0.025 mmol m L-1 guaiazulene in 80% aqueous THF was treated with four volumes of bromine at a drop rate of 0.1 m L min-1 and four volumes of acetic acid at-5℃ for three hours, the yield of guaiazulene-2,9-dione was 23.72%. This was the first report concerning optimized one-step synthesis to provide a convenient method for the large preparation of guaiazulene-2,9-dione.展开更多
To exploit efficient adsorbents for removing middle molecular peptides containing DFLAE (DE5, a typical peptide sequence accumulated in uremic serum) sequence by hemoperfusion, we designed and synthesized three affini...To exploit efficient adsorbents for removing middle molecular peptides containing DFLAE (DE5, a typical peptide sequence accumulated in uremic serum) sequence by hemoperfusion, we designed and synthesized three affinity adsorbents (C1-Zn^2+, C2-Zn^2+ and C3-Zn^2+) that could have high affinity to DE5. Subsequently, we evaluated the corresponding adsorption ability of each adsorbent by static adsorption experiments and isothermal titration calorimetry (ITC). The results showed that C1-Zn^2+ bad the best adsorption ability to DE5-containing peptides and the adsorption capacity for DE5 was 8.52 mg/g. By changing the adsorption conditions, the adsorption mechanism was elucidated. The main driving force of the adsorption is metal-carboxyl coordination and the hydrophobic force affords the cooperative effect. It is expected that our present work can provide basic understanding for the design of adsorbents with high affinity and selectivity towards oligopeptides.展开更多
基金the Key R&D Program of Shandong Province(No.2020CXGC010703)the Key Project of the Natural Science Foundation of Shandong Province(No.ZR2020 KB021)。
文摘Continued innovation in screening methodologies remains important for the discovery of high-quality multiactive fungi,which have been of great significance to the development of new drugs.Mangrove-derived fungi,which are well recognized as prolific sources of natural products,are worth sustained attention and further study.In this study,118 fungi,which mainly included Aspergillus spp.(34.62%)and Penicillium spp.(15.38%),were isolated from the mangrove ecosystem of the Maowei Sea,and 83.1%of the cultured fungi showed at least one bioactivity in four antibacterial and three antioxidant assays.To accurately evaluate the fungal bioactivities,the fungi with multiple bioactivities were successfully evaluated and screened by principal component analysis(PCA),and this analysis provided a dataset for comparing and selecting multibioactive fungi.Among the 118 mangrove-derived fungi tested in this study,Aspergillus spp.showed the best comprehensive activity.Fungi such as A.clavatonanicus,A.flavipes and A.citrinoterreus,which exhibited high comprehensive bioactivity as determined by the PCA,have great potential in the exploitation of natural products and the development of new drugs.This study demonstrated the first use of PCA as a time-saving,scientific method with a strong ability to evaluate and screen multiactive fungi,which indicated that this method can affect the discovery and development of new drugs.
基金supported by National Natural Science Foundation of China (No. 21102136)Changjiang Scholars and Innovative Research Team in University (PCSIRT,No. IRT0944)
文摘We previously isolated a natural product, namely guaiazulene-2,9-dione showing strong antibacterial activity against Vibrio anguillarum, from a gorgonian Muriceides collaris collected in South China Sea. In this experiment, guaiazulene-2,9-dione was quantitatively synthesized with an optimized one-step bromine oxidation method using guaiazulene as the raw material. The key reaction condition including reaction time and temperature, drop rate of bromine, concentration of aqueous THF solution, respective molar ratio of guaiazulene to bromine and acetic acid, and concentration of guaiazulene in aqueous THF solution, were investigated individually at five levels each for optimization. Combined with the verification test to show the absolute yield of each optimization step, the final optimal condition was determined as: when a solution of 0.025 mmol m L-1 guaiazulene in 80% aqueous THF was treated with four volumes of bromine at a drop rate of 0.1 m L min-1 and four volumes of acetic acid at-5℃ for three hours, the yield of guaiazulene-2,9-dione was 23.72%. This was the first report concerning optimized one-step synthesis to provide a convenient method for the large preparation of guaiazulene-2,9-dione.
基金supported by the National Natural Science Foundation of China (20634030 & 51003048)the Specialized Research Fund for the Doctoral Program of Higher Education (20090031120020) the Fun-damental Research Funds for the Central Universities
文摘To exploit efficient adsorbents for removing middle molecular peptides containing DFLAE (DE5, a typical peptide sequence accumulated in uremic serum) sequence by hemoperfusion, we designed and synthesized three affinity adsorbents (C1-Zn^2+, C2-Zn^2+ and C3-Zn^2+) that could have high affinity to DE5. Subsequently, we evaluated the corresponding adsorption ability of each adsorbent by static adsorption experiments and isothermal titration calorimetry (ITC). The results showed that C1-Zn^2+ bad the best adsorption ability to DE5-containing peptides and the adsorption capacity for DE5 was 8.52 mg/g. By changing the adsorption conditions, the adsorption mechanism was elucidated. The main driving force of the adsorption is metal-carboxyl coordination and the hydrophobic force affords the cooperative effect. It is expected that our present work can provide basic understanding for the design of adsorbents with high affinity and selectivity towards oligopeptides.
