AIM: To investigate the pharmacological effects of rice flavone (5,4'-dihydroxy-3',5'-dimethoxy-7-0-β-D-glucopyranosyloxy-flavone, RF) separated from panicle-differentiating to flowing rice on rat experim...AIM: To investigate the pharmacological effects of rice flavone (5,4'-dihydroxy-3',5'-dimethoxy-7-0-β-D-glucopyranosyloxy-flavone, RF) separated from panicle-differentiating to flowing rice on rat experimental hepatic injury. METHODS: Models of rat acute hepatic injury induced by carbon tetrachloride (CCl4) administration, rat hepatic fibrosis induced by thioacetamide, injury of primary cultured rat hepatocytes induced by CCl4, respectively, were established. After treated with RF, content of serum alanine transaminase (ALT), aspartate aminotransferase (AST) and albumin (Alb), hyaluronic acid (HA), the activity of glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), and hydroxyproline (Hyp) were measured and liver tissue was observed pathologically by hematoxylin-eosin (HE) staining. Effects of RF on pathological changes, function index, enzyme of scavenging free radicals and blood rheology were evaluated. RESULTS: In model of rat acute hepatic injury induced by CCI4, RF can significantly decrease the contents of serum ALT, AST, increase the content of Alb, improve the dropsy and fat denaturalization of hepatocytes. In model of rat hepatic fibrosis induced by thioacetamide, RF can inhibit the increase of HA, Hyp and whole blood viscosity, and improve the activities of GSH-Px and SOD, and inauricular microcirculation. CONCLUSION: RF has apparent protective effects on hepatic injury by increasing activity of GSH-Px and SOD, scavenging free radicals produced by CCI4, reducing blood viscosity, and improving microcirculation and blood supply.展开更多
The purpose of this study is to use the newly synthesized molecule Sodium 8-(((carboxymethyl)amino)methyl)-4',7-bishydroxy-isoflavone-3'-sulfonate(M)as a research object,the pharmacological mechanism of the mo...The purpose of this study is to use the newly synthesized molecule Sodium 8-(((carboxymethyl)amino)methyl)-4',7-bishydroxy-isoflavone-3'-sulfonate(M)as a research object,the pharmacological mechanism of the molecule was analyzed by using a series of Systematic pharmacology methods.The results show that the M molecule has a higher drug-like DL value of 0.59 and better molecular property parameters,namely Hdon=4,Hacc=10 and AlogP=0.94;A total of 11 M molecules related targets,namely F2,ESR1,AR,F10,CA2,DPP4,CCNA2,PRSS1,CDK2,GSK3B and PTPN1;A total of 140 diseases are associated with M molecule targets,and these diseases are mainly related to cancer and cardiovascular diseases;A total of 52 pathways involve the pharmacological mechanisms of M molecules,which are mainly related to cancer and other related diseases;GO-enriched analysis showed that these targets are closely related to the regulation of peptidase activity and biological processes such as blood coagulation and hemostasis.This article clearly demonstrated the pharmacological mechanism of M molecule,which provides references for exploring the pharmacological mechanism of new compounds.展开更多
A hydrolyte of magnesium 7 methoxyl 4′ hydroxylisoflavone 3′ sulfonate ([Mg(H 2O) 6](C 16 H 11 O 4SO 3) 2·10H 2O) was synthesized and its crystal structure was determined by X ray diffractio...A hydrolyte of magnesium 7 methoxyl 4′ hydroxylisoflavone 3′ sulfonate ([Mg(H 2O) 6](C 16 H 11 O 4SO 3) 2·10H 2O) was synthesized and its crystal structure was determined by X ray diffraction analyses. The crystal belongs to triclinic crystal system, space group P ī with cell constants a =0 7359(1) nm, b =0 9935(1) nm, c = 1 6335(2) nm, α =91 16(1)°, β =92 07(1)°, γ =106 53(1)°, V =1 1436(2) nm 3 and Z =1. The results show that the title compound consists of [Mg(H 2O) 6] 2+ , C 16 H 11 O 4SO - 3 and H 2O. Mg(II) is located at the symmetry center of the title compound. [Mg(H 2O) 6] 2+ , C 16 H 11 O 4SO - 3 and H 2O form fourteen kinds of hydrogen bonds. The distance of 0 351 nm between parallel isoflavone rings shows a π π stacking interaction. The hydrogen bonds and π π stacking interaction lead to supramolecular formation with three dimensional network structure. The title compound was also characterized by IR and 1H NMR spectra.展开更多
基金Supported by the National Natural Science Foundation of China, No. 30170105
文摘AIM: To investigate the pharmacological effects of rice flavone (5,4'-dihydroxy-3',5'-dimethoxy-7-0-β-D-glucopyranosyloxy-flavone, RF) separated from panicle-differentiating to flowing rice on rat experimental hepatic injury. METHODS: Models of rat acute hepatic injury induced by carbon tetrachloride (CCl4) administration, rat hepatic fibrosis induced by thioacetamide, injury of primary cultured rat hepatocytes induced by CCl4, respectively, were established. After treated with RF, content of serum alanine transaminase (ALT), aspartate aminotransferase (AST) and albumin (Alb), hyaluronic acid (HA), the activity of glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), and hydroxyproline (Hyp) were measured and liver tissue was observed pathologically by hematoxylin-eosin (HE) staining. Effects of RF on pathological changes, function index, enzyme of scavenging free radicals and blood rheology were evaluated. RESULTS: In model of rat acute hepatic injury induced by CCI4, RF can significantly decrease the contents of serum ALT, AST, increase the content of Alb, improve the dropsy and fat denaturalization of hepatocytes. In model of rat hepatic fibrosis induced by thioacetamide, RF can inhibit the increase of HA, Hyp and whole blood viscosity, and improve the activities of GSH-Px and SOD, and inauricular microcirculation. CONCLUSION: RF has apparent protective effects on hepatic injury by increasing activity of GSH-Px and SOD, scavenging free radicals produced by CCI4, reducing blood viscosity, and improving microcirculation and blood supply.
基金The study was funded by the Middle-Aged and Young Teachers in Colleges and Universities in Guangxi Basic Ability Promotion Project(No.2017KY0581)and Natural Science Foundation of Guangxi Province(No.2018GXNSFAA138140).
文摘The purpose of this study is to use the newly synthesized molecule Sodium 8-(((carboxymethyl)amino)methyl)-4',7-bishydroxy-isoflavone-3'-sulfonate(M)as a research object,the pharmacological mechanism of the molecule was analyzed by using a series of Systematic pharmacology methods.The results show that the M molecule has a higher drug-like DL value of 0.59 and better molecular property parameters,namely Hdon=4,Hacc=10 and AlogP=0.94;A total of 11 M molecules related targets,namely F2,ESR1,AR,F10,CA2,DPP4,CCNA2,PRSS1,CDK2,GSK3B and PTPN1;A total of 140 diseases are associated with M molecule targets,and these diseases are mainly related to cancer and cardiovascular diseases;A total of 52 pathways involve the pharmacological mechanisms of M molecules,which are mainly related to cancer and other related diseases;GO-enriched analysis showed that these targets are closely related to the regulation of peptidase activity and biological processes such as blood coagulation and hemostasis.This article clearly demonstrated the pharmacological mechanism of M molecule,which provides references for exploring the pharmacological mechanism of new compounds.
基金ProjectsupportedbytheNaturalScienceFoundationofShaanxiProvince (No .2 0 0 1K11 G5 )
文摘A hydrolyte of magnesium 7 methoxyl 4′ hydroxylisoflavone 3′ sulfonate ([Mg(H 2O) 6](C 16 H 11 O 4SO 3) 2·10H 2O) was synthesized and its crystal structure was determined by X ray diffraction analyses. The crystal belongs to triclinic crystal system, space group P ī with cell constants a =0 7359(1) nm, b =0 9935(1) nm, c = 1 6335(2) nm, α =91 16(1)°, β =92 07(1)°, γ =106 53(1)°, V =1 1436(2) nm 3 and Z =1. The results show that the title compound consists of [Mg(H 2O) 6] 2+ , C 16 H 11 O 4SO - 3 and H 2O. Mg(II) is located at the symmetry center of the title compound. [Mg(H 2O) 6] 2+ , C 16 H 11 O 4SO - 3 and H 2O form fourteen kinds of hydrogen bonds. The distance of 0 351 nm between parallel isoflavone rings shows a π π stacking interaction. The hydrogen bonds and π π stacking interaction lead to supramolecular formation with three dimensional network structure. The title compound was also characterized by IR and 1H NMR spectra.
