The purpose of this study was to isolate and characterize endophytic fungi from the stem tissue which can produce fragrant ingredients in Aquilaria sinensis(also called agarwood) to determine their antitumor and antim...The purpose of this study was to isolate and characterize endophytic fungi from the stem tissue which can produce fragrant ingredients in Aquilaria sinensis(also called agarwood) to determine their antitumor and antimicrobial activities.Twenty-eight fungal endophytes were isolated from agarwood by strict sterile sample preparation and were classified into 14 genera and 4 taxonomic classes(Sordariomycetes,Dothideomycetes,Saccharomycetes,and Zy-gomycetes) based on molecular identification.Of the 28 isolates,13(46.4%) showed antimicrobial activity against at least one of the test strains by the agar well diffusion method,and 23 isolates(82.1%) displayed antitumor activity against at least one of five cancer cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay.The diameters of inhibition zones of YNAS07,YNAS14,HNAS04,HNAS05,HNAS08,and HNAS11 were equal to or higher than 14.0 mm against Staphylococcus aureus,Escherichia coli,Bacillus subtilis,B.subtilis,Aspergillus fumigatus,and B.subtilis,respectively.The inhibition rates of YNAS06,YNAS08,and HNAS06 were not less than 60% to 293-T,293-T,and SKVO3 cells,respectively.These results suggest that the endophytic fungi associated with agarwood will provide us with not only useful micro-ecological information,but also potential antimicrobial and anti-tumor agents.展开更多
In this study,we designed and synthesized a series of phthalazinone acridine derivatives as dual PARP and Topo inhibitors.MTT assays indicated that most of the compounds significantly inhibited multiple cancer cells p...In this study,we designed and synthesized a series of phthalazinone acridine derivatives as dual PARP and Topo inhibitors.MTT assays indicated that most of the compounds significantly inhibited multiple cancer cells proliferation.In addition,all the compounds displayed Topo Ⅱ inhibition activity at 10 mol/L,and also possessed good PARP-1 inhibitory activities.Subsequent mechanistic studies showed that compound 9 a induced remarkable apoptosis and caused prominent S cell cycle arrest in HCT116 cells.Our study suggested that 9 a inhibiting Topo and PARP concurrently can be a potential lead compound for cancer therapy.展开更多
基金Project supported by the National High-Tech R & D Program (863) of China (No.2008AA09Z405)the International Science and Tech-nology Cooperation Projects of China (No.2009DFA32250)
文摘The purpose of this study was to isolate and characterize endophytic fungi from the stem tissue which can produce fragrant ingredients in Aquilaria sinensis(also called agarwood) to determine their antitumor and antimicrobial activities.Twenty-eight fungal endophytes were isolated from agarwood by strict sterile sample preparation and were classified into 14 genera and 4 taxonomic classes(Sordariomycetes,Dothideomycetes,Saccharomycetes,and Zy-gomycetes) based on molecular identification.Of the 28 isolates,13(46.4%) showed antimicrobial activity against at least one of the test strains by the agar well diffusion method,and 23 isolates(82.1%) displayed antitumor activity against at least one of five cancer cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay.The diameters of inhibition zones of YNAS07,YNAS14,HNAS04,HNAS05,HNAS08,and HNAS11 were equal to or higher than 14.0 mm against Staphylococcus aureus,Escherichia coli,Bacillus subtilis,B.subtilis,Aspergillus fumigatus,and B.subtilis,respectively.The inhibition rates of YNAS06,YNAS08,and HNAS06 were not less than 60% to 293-T,293-T,and SKVO3 cells,respectively.These results suggest that the endophytic fungi associated with agarwood will provide us with not only useful micro-ecological information,but also potential antimicrobial and anti-tumor agents.
基金financial supports from the Shenzhen Development and Reform Committee(Nos.20151961 and 2019156)Department of Science and Technology of Guangdong Province(No.2017B030314083)。
文摘In this study,we designed and synthesized a series of phthalazinone acridine derivatives as dual PARP and Topo inhibitors.MTT assays indicated that most of the compounds significantly inhibited multiple cancer cells proliferation.In addition,all the compounds displayed Topo Ⅱ inhibition activity at 10 mol/L,and also possessed good PARP-1 inhibitory activities.Subsequent mechanistic studies showed that compound 9 a induced remarkable apoptosis and caused prominent S cell cycle arrest in HCT116 cells.Our study suggested that 9 a inhibiting Topo and PARP concurrently can be a potential lead compound for cancer therapy.
