Astatine-211(^(211)At,t_(1/2)=7.21 h)emitting twoαparticles with energies of 5.87 and 7.45 MeV,can lead to a high linear energy transfer(LET=98.84 ke V/μm)and short tissue range(50~90μm).Since the 1950s,^(211)At ha...Astatine-211(^(211)At,t_(1/2)=7.21 h)emitting twoαparticles with energies of 5.87 and 7.45 MeV,can lead to a high linear energy transfer(LET=98.84 ke V/μm)and short tissue range(50~90μm).Since the 1950s,^(211)At had stepped into endoradiotherapy and has always been regarded as one of the most promisingα-emitters for targeted-alpha therapy(TAT)in various malignancies.In the past two decades,^(211)At related radiopharmaceuticals have achieved great progress in the studies of basic physicochemical properties of astatine,^(211)At labeling strategies,preclinical and clinical studies,producing profound effects in nuclear medicine.This work will give a panorama of^(211)At-related researches in the recent 20 years,which will cover both the fundamental insights of^(211)At radiochemistry and applied labeling compounds.It can provide some important hints for the studies of TAT and other radiopharmaceuticals applied in tumor radiotherapy.展开更多
study was conducted on the biologically active secondary metabolites produced by the marine fungus Cladosporium sp.MDW-211.Preparative high performance liquid chromatography(HPLC)and other techniques were used to isol...study was conducted on the biologically active secondary metabolites produced by the marine fungus Cladosporium sp.MDW-211.Preparative high performance liquid chromatography(HPLC)and other techniques were used to isolate and purify the compounds,the structures of the compounds 1 were determined by high-resolution electrospray ionization mass spectrometry(HR-ESI-MS),nuclear magnetic resonance(NMR)spectroscopy,X-ray and other methods,and the pro-angiogenic activity of the compounds was evaluated by zebrafish model.One new dihydroisocoumarin 1(4'S-hydroxyasperentin)and three known dihydroisocoumarins 2~4 were obtained and identified.Bioactivity assays revealed that compound 3 exhibited pro-angiogenic activity at concentrations of 20 and 40μmol/L,which is reported here for the first time.展开更多
基金the financial supports from the National Natural Science Foundation of China(No.22006105)the China Postdoctoral Science Foundation(No.2020M683309)the Fundamental Research Funds for the Central Universities。
文摘Astatine-211(^(211)At,t_(1/2)=7.21 h)emitting twoαparticles with energies of 5.87 and 7.45 MeV,can lead to a high linear energy transfer(LET=98.84 ke V/μm)and short tissue range(50~90μm).Since the 1950s,^(211)At had stepped into endoradiotherapy and has always been regarded as one of the most promisingα-emitters for targeted-alpha therapy(TAT)in various malignancies.In the past two decades,^(211)At related radiopharmaceuticals have achieved great progress in the studies of basic physicochemical properties of astatine,^(211)At labeling strategies,preclinical and clinical studies,producing profound effects in nuclear medicine.This work will give a panorama of^(211)At-related researches in the recent 20 years,which will cover both the fundamental insights of^(211)At radiochemistry and applied labeling compounds.It can provide some important hints for the studies of TAT and other radiopharmaceuticals applied in tumor radiotherapy.
基金Project supported by the National Natural Science Foundation of China(No.82204276)the Guangxi Natural Science Foundation(No.2025GXNSF-AA069557)+1 种基金the Guangxi Scholarship Fund of Guangxi Education Departmentthe Innovation Project of Guangxi Minzu University Graduate Education(No.gxmzu-chxs2024225)。
文摘study was conducted on the biologically active secondary metabolites produced by the marine fungus Cladosporium sp.MDW-211.Preparative high performance liquid chromatography(HPLC)and other techniques were used to isolate and purify the compounds,the structures of the compounds 1 were determined by high-resolution electrospray ionization mass spectrometry(HR-ESI-MS),nuclear magnetic resonance(NMR)spectroscopy,X-ray and other methods,and the pro-angiogenic activity of the compounds was evaluated by zebrafish model.One new dihydroisocoumarin 1(4'S-hydroxyasperentin)and three known dihydroisocoumarins 2~4 were obtained and identified.Bioactivity assays revealed that compound 3 exhibited pro-angiogenic activity at concentrations of 20 and 40μmol/L,which is reported here for the first time.