Four extracts of the marine-derived fungus Penicillium velutinum J.F.H.Beyma were obtained via metal ions stress conditions based on the OSMAC(One Strain Many Compounds)strategy.Using a combination of modern approache...Four extracts of the marine-derived fungus Penicillium velutinum J.F.H.Beyma were obtained via metal ions stress conditions based on the OSMAC(One Strain Many Compounds)strategy.Using a combination of modern approaches such as LC/UV,LC/MS and bioactivity data analysis,as well as in silico calculations,influence metal stress factors to change metabolite profiles Penicillium velutinum were analyzed.From the ethyl acetate extract of the P.velutinum were isolated two new piperazine derivatives helvamides B(1)and C(2)together with known saroclazin A(3)(4S,5R,7S)-4,11-dihydroxy-guaia-1(2),9(10)-dien(4).Their structures were established based on spectroscopic methods.The absolute configuration of helvamide B(1)as 2R,5R was determined by a combination of the X-ray analysis and by time-dependent density functional theory(TD-DFT)calculations of electronic circular dichroism(ECD)spectra.The cytotoxic activity of the isolated compounds against human prostate cancer PC-3 and human embryonic kidney HEK-293 cells and growth inhibition activity against yeast-like fungi Candida albicans were assayed.展开更多
The fungus Xylaria sp.KYJ-15 was isolated from Illigera celebica.Based on the one strain many compounds(OSMAC)strategy,the strain was fermented on potato and rice solid media,respectively.As a result,two novel steroid...The fungus Xylaria sp.KYJ-15 was isolated from Illigera celebica.Based on the one strain many compounds(OSMAC)strategy,the strain was fermented on potato and rice solid media,respectively.As a result,two novel steroids,xylarsteroids A(1)and B(2),which are the first examples of C28-steroid with an unusualβ-andγ-lactone ring,respectively,along with two new dihydroisocoumarin glycosides,xylarglycosides A(3)and B(4),were identified.Their structures were elucidated by spectroscopic methods,X-ray diffraction and electronic circular dichroism(ECD)experiments.All isolated compounds were evaluated for cytotoxicity,DPPH radical scavenging activity,acetylcholinesterase inhibitory and antimicrobial effect.Compound 1 exhibited potent AChE inhibitory activity with an IC50 value of 2.61±0.05μmol·L^(−1).Theβ-lactone ring unit of 1 is critical for its AChE inhibitory activity.The finding was further confirmed through exploring the interaction of 1 with AChE by molecular docking.In addition,both compounds 1 and 2 exhibited obvious antibacterial activity against Bacillus subtilis with a minimum inhibitory concentration(MIC)of 2μg·mL^(−1).Compounds 3 and 4 exhibited antibacterial activities against Staphylococcus aureus with MICs of 4 and 2μg·mL^(−1),respectively,which also exhibited DPPH radical scavenging activity comparable to the positive control with IC50 values of 9.2±0.03 and 13.3±0.01μmol·L^(−1),respectively.展开更多
基金funded by Russian Science Foundation,grant number№22-73-00190,https://rscf.ru/en/project/22-73-00190/.
文摘Four extracts of the marine-derived fungus Penicillium velutinum J.F.H.Beyma were obtained via metal ions stress conditions based on the OSMAC(One Strain Many Compounds)strategy.Using a combination of modern approaches such as LC/UV,LC/MS and bioactivity data analysis,as well as in silico calculations,influence metal stress factors to change metabolite profiles Penicillium velutinum were analyzed.From the ethyl acetate extract of the P.velutinum were isolated two new piperazine derivatives helvamides B(1)and C(2)together with known saroclazin A(3)(4S,5R,7S)-4,11-dihydroxy-guaia-1(2),9(10)-dien(4).Their structures were established based on spectroscopic methods.The absolute configuration of helvamide B(1)as 2R,5R was determined by a combination of the X-ray analysis and by time-dependent density functional theory(TD-DFT)calculations of electronic circular dichroism(ECD)spectra.The cytotoxic activity of the isolated compounds against human prostate cancer PC-3 and human embryonic kidney HEK-293 cells and growth inhibition activity against yeast-like fungi Candida albicans were assayed.
文摘The fungus Xylaria sp.KYJ-15 was isolated from Illigera celebica.Based on the one strain many compounds(OSMAC)strategy,the strain was fermented on potato and rice solid media,respectively.As a result,two novel steroids,xylarsteroids A(1)and B(2),which are the first examples of C28-steroid with an unusualβ-andγ-lactone ring,respectively,along with two new dihydroisocoumarin glycosides,xylarglycosides A(3)and B(4),were identified.Their structures were elucidated by spectroscopic methods,X-ray diffraction and electronic circular dichroism(ECD)experiments.All isolated compounds were evaluated for cytotoxicity,DPPH radical scavenging activity,acetylcholinesterase inhibitory and antimicrobial effect.Compound 1 exhibited potent AChE inhibitory activity with an IC50 value of 2.61±0.05μmol·L^(−1).Theβ-lactone ring unit of 1 is critical for its AChE inhibitory activity.The finding was further confirmed through exploring the interaction of 1 with AChE by molecular docking.In addition,both compounds 1 and 2 exhibited obvious antibacterial activity against Bacillus subtilis with a minimum inhibitory concentration(MIC)of 2μg·mL^(−1).Compounds 3 and 4 exhibited antibacterial activities against Staphylococcus aureus with MICs of 4 and 2μg·mL^(−1),respectively,which also exhibited DPPH radical scavenging activity comparable to the positive control with IC50 values of 9.2±0.03 and 13.3±0.01μmol·L^(−1),respectively.
