Sophora alopecuroides L.,a perennial plant belonging to Leguminosae family,is used as medicinal materials to treat a variety of skin diseases.Its chemical components are complex and diverse,mainly including alkaloids ...Sophora alopecuroides L.,a perennial plant belonging to Leguminosae family,is used as medicinal materials to treat a variety of skin diseases.Its chemical components are complex and diverse,mainly including alkaloids and flavonoids.Modern pharmacological studies have found that the isolated compounds from S.alopecuroides have a variety of pharmacological activities.In particular,alkaloids represented by matrine,aloperine and oxymatrine have significant anti-inflammatory,anti-viral,anti-tumor,anti-bacterial and immunomodulatory activities.This paper summarized the chemical constituents and pharmacological activities of S.alopecuroides,aiming to provide the basis for further research.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
Objective： To evaluate the antimicrobial activity of total alkaloids extracted from Sophorea alopecuroides L. （TASA） against clinical isolated extended-spectrum beta-lactamases （ESBLs） producing Escherichia coil ...Objective： To evaluate the antimicrobial activity of total alkaloids extracted from Sophorea alopecuroides L. （TASA） against clinical isolated extended-spectrum beta-lactamases （ESBLs） producing Escherichia coil （E.. coil） strains. Methods： The antibacterial activity of TASA either itself or in combination with cefotaxime （CTX） or ceftazidime （CAZ） was investigated by using the microbroth dilution method and phenotypic confirmatory disk diffusion test against three clinical isolated ESBLs-producing E. coil strains; the interactions of TASA and C＇I＇X or CAZ were ascertained by evaluating the fractional inhibitory concentration index （FICI）. Results： The antibacterial activity of either TASA itself or in combination with C＇IX or CAZ was found. The minimum inhibitory concentration （MICs） of TASA against the ESBLs producing isolates was 12.5 mg/mL. In the combinations with a sub-inhibitory concentration of TASA, a synergistic effect on CTX and CAZ against the ESBLs producing isolates was observed. Similarly, the isolates exposed to lower dose of TASA yielded an increased susceptibility to CTX and CAZ by 8-16 folds determined by microdilution assay. Moreover, enzymatic detection of ESBLs demonstrated that TASA induced reversal resistance to CTX and CAZ partially by a mechanism of inhibition of ESBLs activity in these isolates. Additionally, in the tested isolates following the exposure of TASA, molecular analysis verified the SHV-type beta-lactamase encoding ESBL gene in these isolates, and no mutation was introduced into the ESBL gene. Conclusions： These results suggest that TASA could be used as a source of natural compound with pharmacological activity of reversal resistance to antimicrobial agent. These findings also indicated that the application of the TASA in combination with antibiotics might prove useful in the control and treatment of infectious diseases caused by the ESBLs producing enterobacteriaceae.展开更多
Sophaloseedlines A-G(1-7),seven new matrine-based alkaloids along with two known analogues,were isolated from the seeds of Sophora alopecuroides.The new structures were determined based on extensive spectroscopic data...Sophaloseedlines A-G(1-7),seven new matrine-based alkaloids along with two known analogues,were isolated from the seeds of Sophora alopecuroides.The new structures were determined based on extensive spectroscopic data,electronic circular dichroism calculations,and X-ray crystallography.Notably,sophaloseedline A(1)represents a novel rearranged 6(5→17)-abeo-matrine alkaloid featuring unprecedented highly constructed 7/6/5/6 tetracyclic fused ring skeleton.The hypothetical biosynthetic pathways for sophaloseedli nes A-F were proposed based on co-existing precursors.Additionally,all the isolated alkaloids were screened for their antiviral activities against hepatitis B virus,and new alkaloids 1 and 2 displayed more potent activities than those of matrine(a parent alkaloid of title plant)and positive control(lamivudine).展开更多
Background Helicobacterpylori （H.pylori） infection could lead to most gastroduodenal diseases and is even identified as a carcinogen of gastric cancer.Total alkaloids of sophora alopecuroides （TASA） is widely used...Background Helicobacterpylori （H.pylori） infection could lead to most gastroduodenal diseases and is even identified as a carcinogen of gastric cancer.Total alkaloids of sophora alopecuroides （TASA） is widely used in herbal remedies to treat various infectious diseases,including stomach-associated diseases.This study is aimed at evaluating the antimicrobial activity of TASA on H.pylori-infected BALB/c mice mouse gastritis.Methods Totally 120 BALB/c mice were orally inoculated with H.pylori Bacterial liquid to construct BALB/c mice H.pylori infection gastritis animal model,after the model was successfully created.We randomly assigned 100 infected mice into 10 treatment groups,the first group （normal saline）; the second group （bismuth pectin）; the third group （omeprazole）; the fourth group （TASA 2 mg/d）; the fifth group （TASA 4 mg/d）; the sixth group （TASA 5 mg/d）; the seventh group （TASA ＋ bismuth pectin）; the eighth group （TASA ＋ omeprazole）; the ninth group （bismuth pectin ＋ clarithromycin ＋ metronidazole）;the tenth group （omeprazole ＋ clarithromycin ＋ metronidazole）,5 other non-infected mice as negative control.Mice were orally inoculated twice a day and 7 days continuously.Then the mice were killed 4 weeks after treatment,we used realtime PCR to detect 16sDNA of H.pylori to test both the colonization and the clearance mice of bacteria of each treatment.We applied hematoxylin and eosin （HE） staining and immunostaining of mice gastric mucosa to observe the general inflammation and related factors interleukin 8 （IL-8）,cyclooxygenase 2 （COX-2）,and nuclear factor-kappa B （NF-KB） expression change after treatments.Results Firstly,we ensured that after 6-week intragastric administration,the bacteria colonization reached an exceed peak which is far higher than positive threshold （P ＜0.001）; secondly,after treatments,it is revealed that TASA combined with omeprazole or bismuth pectin showed promising antimicrobial activity against H.pylori as well as conventional triple therapy （P ＜0.001）; thirdly,HE staining showed that the inflammation on mice gastric mucosal membrane were also relieved obviously in TASA combined treatments and conventional triple therapy compared with normal saline treated mice,moreover,from immunohistochemistry results,H.pylori-induced IL-8,COX-2,and NF-KB were consistently suppressed in seventh,eighth,ninth,and tenth group to a certain extent.Conclusion These results open the possibility of taking TASA as an anti-inflammatory agent for H.pylori gastritis.展开更多
Objective：To investigate the effect of total alkaloids of Sophora alopecuroides（TASA） on dextran sulfate sodium（DSS）-induced colitis in mice.Methods：Chronic experimental colitis was induced by administration of ...Objective：To investigate the effect of total alkaloids of Sophora alopecuroides（TASA） on dextran sulfate sodium（DSS）-induced colitis in mice.Methods：Chronic experimental colitis was induced by administration of 4 cycles of 4%DSS.Fifty mice were randomly distributed into 4 groups（normal,DSS,DSS/high-dose TASA, and DSS/low-dose TASA groups） by a random number table with body weight stratification.Mice in the normal group（n=11） and DSS-induced colitis control group（n=15） received control treatment of 20 mL/kg distilled water; DSS plus TASA high- and low-dose groups（n=12 each） were treated with TASA solution（20 mL/kg） at the doses of 60 mg/kg and 30 mg/kg,respectively.The severity of colitis was assessed on the basis of clinical signs, colon length,and histology scores.Moreover,secretory immunoglobulin A（slgA） and haptoglobin（HP） were analyzed by enzyme linked immunosorbent assay;intercellular adhesion molecule 1（ICAM-1） and macrophage-migration inhibitory factor（MIF） gene expressions were analyzed by quantitative reverse transcriptase realtime polymerase chain reaction（qRT-PCR） using SYBA greenⅠ;and nuclear factorκB（NF-κB） expression and activation and p65 interaction with the promoter of ICAM-1 gene were assessed by Western blotting and chromatin immunoprecipitation assay.Results：TASA administration significantly attenuated the damage and substantially reduced HP elevation and maintained the level of cecum slgA.TASA inhibited the ICAM-1 gene expression and had no effect on MIF gene expression.Also,TASA was able to reduce phospho-lκBα（p-lκBα） protein expression;however,it had no effect on the activation of IκB kinaseα（IKKα） and inhibitor of NF-κBα（IκBα）.Moreover,TASA inhibited the p65 recruitment to the ICAM-1 gene promoter.Conclusions：TASA had a protective effect on DSS-induced colitis.Such effect may be associated with its inhibition of NF-κB activation and blockade of NF-κB-regulated transcription activation of proinflammatory mediator gene.展开更多
A phytochemical investigation on the seeds of Sophora alopecuroides led to obtaining fourteen structurally diverse matrine-based alkaloids(1-14),including eight new ones(1,6,8-12,14).Notably,alopecuroide F(1)represent...A phytochemical investigation on the seeds of Sophora alopecuroides led to obtaining fourteen structurally diverse matrine-based alkaloids(1-14),including eight new ones(1,6,8-12,14).Notably,alopecuroide F(1)represents the first dimeric matrine-type skeleton assembled via unprecedent C-13-C-12'connection.The new structures were determined through extensive spectroscopic data(UV,OR,HRESIMS,1D,and 2D NMR),ECD calculations,and three instances,verified by X-ray crystallography.Biologically,all alkaloids were evaluated for cytotoxicity against four human cancer cell lines(HepG2,A549,THP-1,and MCF-7)and anti-inflammatory activities for two pro-inflammatory cytokines(TNF-αand IL-6).Alopecuroide F(1)can inhibit TNF-αand IL-6 productions in a dose-dependent manner with IC50 values of 35.6±0.5 and 41.7±0.8μmol/L,respectively.展开更多
基金the College Student Innovation and Entrepreneurship Training Program(X202010163166).
文摘Sophora alopecuroides L.,a perennial plant belonging to Leguminosae family,is used as medicinal materials to treat a variety of skin diseases.Its chemical components are complex and diverse,mainly including alkaloids and flavonoids.Modern pharmacological studies have found that the isolated compounds from S.alopecuroides have a variety of pharmacological activities.In particular,alkaloids represented by matrine,aloperine and oxymatrine have significant anti-inflammatory,anti-viral,anti-tumor,anti-bacterial and immunomodulatory activities.This paper summarized the chemical constituents and pharmacological activities of S.alopecuroides,aiming to provide the basis for further research.
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Supported by a Sub-project of National Basic Research Program of China(No.2006CB504401)the National Natural Science Foundation of China(No.31060348,No.30860207)Grants of Science and Technology Program of Ningxia to Yujiong Wang(No.Z2006-1-75001,KGZ-12-10-02)
文摘Objective： To evaluate the antimicrobial activity of total alkaloids extracted from Sophorea alopecuroides L. （TASA） against clinical isolated extended-spectrum beta-lactamases （ESBLs） producing Escherichia coil （E.. coil） strains. Methods： The antibacterial activity of TASA either itself or in combination with cefotaxime （CTX） or ceftazidime （CAZ） was investigated by using the microbroth dilution method and phenotypic confirmatory disk diffusion test against three clinical isolated ESBLs-producing E. coil strains; the interactions of TASA and C＇I＇X or CAZ were ascertained by evaluating the fractional inhibitory concentration index （FICI）. Results： The antibacterial activity of either TASA itself or in combination with C＇IX or CAZ was found. The minimum inhibitory concentration （MICs） of TASA against the ESBLs producing isolates was 12.5 mg/mL. In the combinations with a sub-inhibitory concentration of TASA, a synergistic effect on CTX and CAZ against the ESBLs producing isolates was observed. Similarly, the isolates exposed to lower dose of TASA yielded an increased susceptibility to CTX and CAZ by 8-16 folds determined by microdilution assay. Moreover, enzymatic detection of ESBLs demonstrated that TASA induced reversal resistance to CTX and CAZ partially by a mechanism of inhibition of ESBLs activity in these isolates. Additionally, in the tested isolates following the exposure of TASA, molecular analysis verified the SHV-type beta-lactamase encoding ESBL gene in these isolates, and no mutation was introduced into the ESBL gene. Conclusions： These results suggest that TASA could be used as a source of natural compound with pharmacological activity of reversal resistance to antimicrobial agent. These findings also indicated that the application of the TASA in combination with antibiotics might prove useful in the control and treatment of infectious diseases caused by the ESBLs producing enterobacteriaceae.
基金supported by grants from the National Natural Science Foundation of China(Nos.81803376,82074116,81973190)the Guangdong Basic and Applied Basic Research Foundation(No.2020B1515020033)+3 种基金the Natural Science Foundation of Guangdong Province(No.2018B030311020)the Local Innovative and Research Teams Project of Guangdong Pearl River Talents Program(No.2017BT01Y036)the Guangdong Basic and Applied Basic Research Foundation-Regional Joint Fund(Youth Fund Project,No.2020A1515110415)the high performance public computing service platform of Ji nan Un iversity.
文摘Sophaloseedlines A-G(1-7),seven new matrine-based alkaloids along with two known analogues,were isolated from the seeds of Sophora alopecuroides.The new structures were determined based on extensive spectroscopic data,electronic circular dichroism calculations,and X-ray crystallography.Notably,sophaloseedline A(1)represents a novel rearranged 6(5→17)-abeo-matrine alkaloid featuring unprecedented highly constructed 7/6/5/6 tetracyclic fused ring skeleton.The hypothetical biosynthetic pathways for sophaloseedli nes A-F were proposed based on co-existing precursors.Additionally,all the isolated alkaloids were screened for their antiviral activities against hepatitis B virus,and new alkaloids 1 and 2 displayed more potent activities than those of matrine(a parent alkaloid of title plant)and positive control(lamivudine).
文摘Background Helicobacterpylori （H.pylori） infection could lead to most gastroduodenal diseases and is even identified as a carcinogen of gastric cancer.Total alkaloids of sophora alopecuroides （TASA） is widely used in herbal remedies to treat various infectious diseases,including stomach-associated diseases.This study is aimed at evaluating the antimicrobial activity of TASA on H.pylori-infected BALB/c mice mouse gastritis.Methods Totally 120 BALB/c mice were orally inoculated with H.pylori Bacterial liquid to construct BALB/c mice H.pylori infection gastritis animal model,after the model was successfully created.We randomly assigned 100 infected mice into 10 treatment groups,the first group （normal saline）; the second group （bismuth pectin）; the third group （omeprazole）; the fourth group （TASA 2 mg/d）; the fifth group （TASA 4 mg/d）; the sixth group （TASA 5 mg/d）; the seventh group （TASA ＋ bismuth pectin）; the eighth group （TASA ＋ omeprazole）; the ninth group （bismuth pectin ＋ clarithromycin ＋ metronidazole）;the tenth group （omeprazole ＋ clarithromycin ＋ metronidazole）,5 other non-infected mice as negative control.Mice were orally inoculated twice a day and 7 days continuously.Then the mice were killed 4 weeks after treatment,we used realtime PCR to detect 16sDNA of H.pylori to test both the colonization and the clearance mice of bacteria of each treatment.We applied hematoxylin and eosin （HE） staining and immunostaining of mice gastric mucosa to observe the general inflammation and related factors interleukin 8 （IL-8）,cyclooxygenase 2 （COX-2）,and nuclear factor-kappa B （NF-KB） expression change after treatments.Results Firstly,we ensured that after 6-week intragastric administration,the bacteria colonization reached an exceed peak which is far higher than positive threshold （P ＜0.001）; secondly,after treatments,it is revealed that TASA combined with omeprazole or bismuth pectin showed promising antimicrobial activity against H.pylori as well as conventional triple therapy （P ＜0.001）; thirdly,HE staining showed that the inflammation on mice gastric mucosal membrane were also relieved obviously in TASA combined treatments and conventional triple therapy compared with normal saline treated mice,moreover,from immunohistochemistry results,H.pylori-induced IL-8,COX-2,and NF-KB were consistently suppressed in seventh,eighth,ninth,and tenth group to a certain extent.Conclusion These results open the possibility of taking TASA as an anti-inflammatory agent for H.pylori gastritis.
基金Supported by Guangdong Administration of Traditional Chinese Medicine(No.201 01 92)
文摘Objective：To investigate the effect of total alkaloids of Sophora alopecuroides（TASA） on dextran sulfate sodium（DSS）-induced colitis in mice.Methods：Chronic experimental colitis was induced by administration of 4 cycles of 4%DSS.Fifty mice were randomly distributed into 4 groups（normal,DSS,DSS/high-dose TASA, and DSS/low-dose TASA groups） by a random number table with body weight stratification.Mice in the normal group（n=11） and DSS-induced colitis control group（n=15） received control treatment of 20 mL/kg distilled water; DSS plus TASA high- and low-dose groups（n=12 each） were treated with TASA solution（20 mL/kg） at the doses of 60 mg/kg and 30 mg/kg,respectively.The severity of colitis was assessed on the basis of clinical signs, colon length,and histology scores.Moreover,secretory immunoglobulin A（slgA） and haptoglobin（HP） were analyzed by enzyme linked immunosorbent assay;intercellular adhesion molecule 1（ICAM-1） and macrophage-migration inhibitory factor（MIF） gene expressions were analyzed by quantitative reverse transcriptase realtime polymerase chain reaction（qRT-PCR） using SYBA greenⅠ;and nuclear factorκB（NF-κB） expression and activation and p65 interaction with the promoter of ICAM-1 gene were assessed by Western blotting and chromatin immunoprecipitation assay.Results：TASA administration significantly attenuated the damage and substantially reduced HP elevation and maintained the level of cecum slgA.TASA inhibited the ICAM-1 gene expression and had no effect on MIF gene expression.Also,TASA was able to reduce phospho-lκBα（p-lκBα） protein expression;however,it had no effect on the activation of IκB kinaseα（IKKα） and inhibitor of NF-κBα（IκBα）.Moreover,TASA inhibited the p65 recruitment to the ICAM-1 gene promoter.Conclusions：TASA had a protective effect on DSS-induced colitis.Such effect may be associated with its inhibition of NF-κB activation and blockade of NF-κB-regulated transcription activation of proinflammatory mediator gene.
基金This project was supported financially by grants from the National Natural Science Foundation of China(Nos.81803376,82074116,81973190)the Guangdong Basic and Applied Basic Research Foundation(No.2020B1515020033)+4 种基金the Natural Science Foundation of Guangdong Province(No.2018B030311020)the Local Innovative and Research Teams Project of Guangdong Pearl River Talents Program(No.2017BT01Y036)Guangdong Basic and Applied Basic Research Foundation-Regional Joint Fund(Youth Fund Project,No.2020A1515110415)Pearl River S&T Nova Program of Guangzhou(No.201906010069)We thank the High Performance Public Computing Service Platform of Jinan University for the help of theoretical ECD calculations.
文摘A phytochemical investigation on the seeds of Sophora alopecuroides led to obtaining fourteen structurally diverse matrine-based alkaloids(1-14),including eight new ones(1,6,8-12,14).Notably,alopecuroide F(1)represents the first dimeric matrine-type skeleton assembled via unprecedent C-13-C-12'connection.The new structures were determined through extensive spectroscopic data(UV,OR,HRESIMS,1D,and 2D NMR),ECD calculations,and three instances,verified by X-ray crystallography.Biologically,all alkaloids were evaluated for cytotoxicity against four human cancer cell lines(HepG2,A549,THP-1,and MCF-7)and anti-inflammatory activities for two pro-inflammatory cytokines(TNF-αand IL-6).Alopecuroide F(1)can inhibit TNF-αand IL-6 productions in a dose-dependent manner with IC50 values of 35.6±0.5 and 41.7±0.8μmol/L,respectively.
