Acute respiratory infection caused by severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)had caused a global pandemic since 2019,and posed a serious threat to global health security.Traditional Chinese medicin...Acute respiratory infection caused by severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)had caused a global pandemic since 2019,and posed a serious threat to global health security.Traditional Chinese medicine(TCM)has played an indispensable role in the battle against the epidemic.Many components originated from TCMs were found to inhibit the production of SARS-CoV-23C-like protease(3CLpro)and papain-like protease(PLpro),which are two promising therapeutic targets to inhibit SARS-CoV-2.This study describes a systematic investigation of the roots and rhizomes of Sophora tonkinensis,which results in the characterization of 12 new flavonoids,including seven prenylated flavanones(1−7),one prenylated flavonol(8),two prenylated chalcones(9−10),one isoflavanone(11),and one isoflavan dimer(12),together with 43 known compounds(13−55).Their structures including the absolute configurations were elucidated by comprehensive analysis of MS,1D and 2D NMR data,and time-dependent density functional theory electronic circular dichroism(TDDFT ECD)calculations.Compounds 12 and 51 exhibited inhibitory effects against SARS-CoV-23CLpro with IC_(50) values of 34.89 and 19.88μmol·L^(−1),repectively while compounds 9,43 and 47 exhibited inhibitory effects against PLpro with IC_(50) values of 32.67,79.38,and 16.74μmol·L^(−1),respectively.展开更多
AIM： To search for new antiviral agents from traditional Chinese medicine, specifically anti-enterovirosuses agents. METHODS： The aqueous extracts （AE） of more than 100 traditionally used medicinal plants in China...AIM： To search for new antiviral agents from traditional Chinese medicine, specifically anti-enterovirosuses agents. METHODS： The aqueous extracts （AE） of more than 100 traditionally used medicinal plants in China were evaluated for their in vitro anti-Coxsackie virus B3 activities with a MTT-based colorimetric assay. RESULTS： The test for AE of 16 plants exhibited anti- Coxsackie virus B3 activities at different magnitudes of potency. They can inhibit three steps （inactivation, adsorption and replication） during the infection. Among the 16 plants, Sargentodoxa cuneata （Oliv.） Rehd. et Wils., Sophora tonkinensis Gapnep., Paeonia veitchii Lynch, Spatholobus suberectus Dunn. and Cyrtorniurn fortunei J, sm. also have activity against other enterovirus, including Coxsackie virus 135, Polio virus I, Echo virus 9 and Echo virus 29. Cell cytotoxic assay demonstrated that all tested AE had CC50 values higher than their EC50 values. CONCLUSION： The sixteen traditionally used medicinal plants in China possessed antMral activity, and some of them merit further investigations.展开更多
Three novel matrine-type alkaloids(1-3)and two unprecedented aloperine-type alkaloids(4 and 5)were isolated from the root of Sophora tonkinensis and the seeds of Sophora alopecuroides respectively.Notably,compound 1 p...Three novel matrine-type alkaloids(1-3)and two unprecedented aloperine-type alkaloids(4 and 5)were isolated from the root of Sophora tonkinensis and the seeds of Sophora alopecuroides respectively.Notably,compound 1 possessed an unprecedented 6/5/6 tricyclic skeleton,while compounds 2 and 3 characterized by rare 6/6/5/6 tetracyclic system and 6/6/6/6/6 pentacyclic system respectively.Moreover,compound 4 possessed an unprecedented 6/7/6/6 tetracyclic core,and compound 5 characterized by rare 6/6/6/6tetracyclic skeleton.Their structures were elucidated by comprehensive spectroscopic data analysis and electronic circular dichroism(ECD)calculations.Biological tests indicated that compound 5 displayed significant anti-tobacco mosaic virus(TMV)activity compared with the positive control ningnanmycin.展开更多
Radix Sophorae tonkinensis(RST) is a widely used herb in Traditional Chinese Medicine(TCM) for treating infectious and inflammatory diseases. However, the toxicity data for RST are limited. The aim of this work is to ...Radix Sophorae tonkinensis(RST) is a widely used herb in Traditional Chinese Medicine(TCM) for treating infectious and inflammatory diseases. However, the toxicity data for RST are limited. The aim of this work is to assess and compare the toxicity of the whole RST extract and its five active fractions using the zebrafish model. Five active fractions of RST were prepared using five different types of solvents, which included dealkalized water, ethanol, n-butyl ethanol, dichloromethane, and diethyl ether. The chemical profiles of the active fractions were determined by high-performance liquid chromatography(HPLC), and the toxicity observed in the zebrafish model was confirmed using mouse models. In the zebrafish model, cardiovascular toxicity was observed for the fraction extracted using diethyl ether, and hepatotoxicity was observed for the whole RST extract and the fractions extracted using water and ethanol, whereas both cardiovascular and hepatic toxicities were observed for the fractions extracted using n-butyl ethanol and dichloromethane. The hepatotoxicity of the fractions extracted using n-butyl ethanol and dichloromethane was also observed in mice. Our findings provide the toxicity data for RST and its five active fractions through modeling in a zebrafish, and indicate that the different fractions may each have a different toxicity, which is helpful for the optimal use of RST in clinical practice.展开更多
基金This work was supported from the National Natural Science Foundation of China(Nos.82173696 and 21920102003)the Science and Technology Commission of Shanghai Municipality(Nos.20431900200 and 20430780300)+1 种基金the Strategic Priority Research Program of Chinese Academy of Sciences(Nos.SIMM010110 and SIMM040302)the Sustainable Development of Precious Traditional Chinese Medicine Resources(No.2060302-2001-01).
文摘Acute respiratory infection caused by severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)had caused a global pandemic since 2019,and posed a serious threat to global health security.Traditional Chinese medicine(TCM)has played an indispensable role in the battle against the epidemic.Many components originated from TCMs were found to inhibit the production of SARS-CoV-23C-like protease(3CLpro)and papain-like protease(PLpro),which are two promising therapeutic targets to inhibit SARS-CoV-2.This study describes a systematic investigation of the roots and rhizomes of Sophora tonkinensis,which results in the characterization of 12 new flavonoids,including seven prenylated flavanones(1−7),one prenylated flavonol(8),two prenylated chalcones(9−10),one isoflavanone(11),and one isoflavan dimer(12),together with 43 known compounds(13−55).Their structures including the absolute configurations were elucidated by comprehensive analysis of MS,1D and 2D NMR data,and time-dependent density functional theory electronic circular dichroism(TDDFT ECD)calculations.Compounds 12 and 51 exhibited inhibitory effects against SARS-CoV-23CLpro with IC_(50) values of 34.89 and 19.88μmol·L^(−1),repectively while compounds 9,43 and 47 exhibited inhibitory effects against PLpro with IC_(50) values of 32.67,79.38,and 16.74μmol·L^(−1),respectively.
文摘AIM： To search for new antiviral agents from traditional Chinese medicine, specifically anti-enterovirosuses agents. METHODS： The aqueous extracts （AE） of more than 100 traditionally used medicinal plants in China were evaluated for their in vitro anti-Coxsackie virus B3 activities with a MTT-based colorimetric assay. RESULTS： The test for AE of 16 plants exhibited anti- Coxsackie virus B3 activities at different magnitudes of potency. They can inhibit three steps （inactivation, adsorption and replication） during the infection. Among the 16 plants, Sargentodoxa cuneata （Oliv.） Rehd. et Wils., Sophora tonkinensis Gapnep., Paeonia veitchii Lynch, Spatholobus suberectus Dunn. and Cyrtorniurn fortunei J, sm. also have activity against other enterovirus, including Coxsackie virus 135, Polio virus I, Echo virus 9 and Echo virus 29. Cell cytotoxic assay demonstrated that all tested AE had CC50 values higher than their EC50 values. CONCLUSION： The sixteen traditionally used medicinal plants in China possessed antMral activity, and some of them merit further investigations.
基金financially supported by the National Natural Science Foundation of China(Nos.32160103 and U1812403)the Science and Technology Department of Guizhou Province(Nos.QKH ZC-[2021]-YB181,QKH CXTD-[2022]-007 and QKH ZYD-[2022]-4015)Guizhou Provincial Engineering Research Center for Natural Drugs。
文摘Three novel matrine-type alkaloids(1-3)and two unprecedented aloperine-type alkaloids(4 and 5)were isolated from the root of Sophora tonkinensis and the seeds of Sophora alopecuroides respectively.Notably,compound 1 possessed an unprecedented 6/5/6 tricyclic skeleton,while compounds 2 and 3 characterized by rare 6/6/5/6 tetracyclic system and 6/6/6/6/6 pentacyclic system respectively.Moreover,compound 4 possessed an unprecedented 6/7/6/6 tetracyclic core,and compound 5 characterized by rare 6/6/6/6tetracyclic skeleton.Their structures were elucidated by comprehensive spectroscopic data analysis and electronic circular dichroism(ECD)calculations.Biological tests indicated that compound 5 displayed significant anti-tobacco mosaic virus(TMV)activity compared with the positive control ningnanmycin.
基金Project supported by the National Science and Technology Major Project of China(Nos.2012ZX09505001-002 and 2015ZX09501004-002-002)the Zhejiang Provincial Science and Technology Planning Project of China(No.2014C03009)
文摘Radix Sophorae tonkinensis(RST) is a widely used herb in Traditional Chinese Medicine(TCM) for treating infectious and inflammatory diseases. However, the toxicity data for RST are limited. The aim of this work is to assess and compare the toxicity of the whole RST extract and its five active fractions using the zebrafish model. Five active fractions of RST were prepared using five different types of solvents, which included dealkalized water, ethanol, n-butyl ethanol, dichloromethane, and diethyl ether. The chemical profiles of the active fractions were determined by high-performance liquid chromatography(HPLC), and the toxicity observed in the zebrafish model was confirmed using mouse models. In the zebrafish model, cardiovascular toxicity was observed for the fraction extracted using diethyl ether, and hepatotoxicity was observed for the whole RST extract and the fractions extracted using water and ethanol, whereas both cardiovascular and hepatic toxicities were observed for the fractions extracted using n-butyl ethanol and dichloromethane. The hepatotoxicity of the fractions extracted using n-butyl ethanol and dichloromethane was also observed in mice. Our findings provide the toxicity data for RST and its five active fractions through modeling in a zebrafish, and indicate that the different fractions may each have a different toxicity, which is helpful for the optimal use of RST in clinical practice.
