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
The nuclear factor-KB （NF-KB） transcription factors control many physiological processes including in- flammation, immunity, apoptosis, and angiogenesis. In our search for NF-KB inhibitors from natural resources, we...The nuclear factor-KB （NF-KB） transcription factors control many physiological processes including in- flammation, immunity, apoptosis, and angiogenesis. In our search for NF-KB inhibitors from natural resources, we identified 4＇,6-dihydroxy-4-methoxyisoaurone （ISOA） as an inhibitor of NF-KB activation from the seeds of Tricho- santhes kirilowii. However, the mechanism by which ISOA inhibits NF-KB activation is not fully understood. In the present study, we demonstrated the effect of ISOA on NF-KB activation in TNF-α-stimulated HeLa cells. This com- pound suppressed NF-KB activation through the inhibition of IKB kinase （IKK） activation. ISOA also has an influ- ence on upstream signaling of IKK through the inhibition of expression of adaptor proteins, TNF receptor-associated factor 2 （TRAF2） and receptor interacting protein 1 （RIP1）. Consequently, ISOA blocked the phosphorylation and degradation of the inhibitor of NF-KB alpha （IKBα） , and subsequent phosphorylation and nuclear translocation of p65. The suppression of NF-KB activation by ISOA led to the down-regulation of target genes involved in inflam- mation, proliferation, angiogenesis and invasion, as well as potentiation of TNF-α-induced apoptosis at least in part through activation of caspase-8. Taken together, this study extends our understanding on the mechanisms underly- ing the anti-inflammatory and anti-cancer activities of ISOA. Our findings provide new insight into the molecular mechanisms and a potential application of ISOA for inflammatory diseases as well as certain cancers associated with abnormal NF-KB activation.展开更多
A new flavone glycoside, 5,8-dihydroxy-4',6,7-trimethoxyflavone 8-O-(-D-glucopyranoside 1, together with three known flavonoids, pedalitin 2, cirsimartin 3 and genkwanin 4, were isolated from the aerial parts of I...A new flavone glycoside, 5,8-dihydroxy-4',6,7-trimethoxyflavone 8-O-(-D-glucopyranoside 1, together with three known flavonoids, pedalitin 2, cirsimartin 3 and genkwanin 4, were isolated from the aerial parts of Isodon enanderianus. Their structures were determined on the basis of spectral data.展开更多
A new flavonoid glycoside, 5, 7-dihydroxy-4'-methoxyflavonoid 7-Q-[6-O-(4-O-acetyl-alpha-L-rhamnosyl)-3-O-beta-D-glucosyl]-6-O-acetyl-beta-D-glucoside was isolated from Thalictrum przewalskii. Its structure was de...A new flavonoid glycoside, 5, 7-dihydroxy-4'-methoxyflavonoid 7-Q-[6-O-(4-O-acetyl-alpha-L-rhamnosyl)-3-O-beta-D-glucosyl]-6-O-acetyl-beta-D-glucoside was isolated from Thalictrum przewalskii. Its structure was determined on basis of spectroscopic evidences.展开更多
Two hydrates of sodium 5,7-dihydroxy-6,4'-dimethoxyisoflavone-3'-sulfonate ([Na(H2O)](C17H13O6SO3)2H2O, 1) and nickel 5,7-dihydroxy-6,4'-dimethoxyisoflavone-3'-sulfonate ([Ni(H2O)6](C17H13O6SO3)24H2O, ...Two hydrates of sodium 5,7-dihydroxy-6,4'-dimethoxyisoflavone-3'-sulfonate ([Na(H2O)](C17H13O6SO3)2H2O, 1) and nickel 5,7-dihydroxy-6,4'-dimethoxyisoflavone-3'-sulfonate ([Ni(H2O)6](C17H13O6SO3)24H2O, 2) were syn-thesized and characterized by IR, 1H NMR and X-ray diffraction analyses. The hydrate 1 crystallizes in the mono-clinic system, space group P2(1) with a=0.8201(9) nm, b=0.8030(8) nm, c=1.5361(16) nm, =102.052(12), V=0.9893(18) nm3, Dc=1.579 g/cm3, Z=2, =0.252 nm-1, F(000)=488, R=0.0353, wR=0.0873. The hydrate 2 belongs to triclinic system, space group P-1 with a=0.7411(3) nm, b=0.8333(3) nm, c=1.7448(7) nm, a=86.361(6), 撸?6.389(5), ?=88.999(3), V=1.0731(7) nm3, Dc=1.587 g/cm3, Z=1, =0.649 mm-1, F(000)=534. In the structure of 1, the sodium cation is coordinated by six oxygen atoms and two adjacent ones are bridged by three oxygen atoms to form an octahedron chain. The C—H…p hydrogen bonds exist between two isoflavone molecules in the structure of 2. Meanwhile, hydrogen bonds in two compounds, link themselves to assemble two three-dimensional network structures, respectively.展开更多
A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots o...A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots of Stellera chamaejasme L. together with known chamaechromone. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.展开更多
Two new compounds 7-hydroxy-5-O-（β-D-glucopyranoside） flavan （1） and （Z）-4＇,6＇-dihydroxy-2＇-O-（β-D-glucopyranoside） chalcone （2）, along with eight known compounds, were isolated from the stem bark of Dr...Two new compounds 7-hydroxy-5-O-（β-D-glucopyranoside） flavan （1） and （Z）-4＇,6＇-dihydroxy-2＇-O-（β-D-glucopyranoside） chalcone （2）, along with eight known compounds, were isolated from the stem bark of Drypetes parvifolia （Euphorbiaceae）. Their structures were established on the basis of spectroscopic analysis and chemical evidence.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.
文摘The nuclear factor-KB （NF-KB） transcription factors control many physiological processes including in- flammation, immunity, apoptosis, and angiogenesis. In our search for NF-KB inhibitors from natural resources, we identified 4＇,6-dihydroxy-4-methoxyisoaurone （ISOA） as an inhibitor of NF-KB activation from the seeds of Tricho- santhes kirilowii. However, the mechanism by which ISOA inhibits NF-KB activation is not fully understood. In the present study, we demonstrated the effect of ISOA on NF-KB activation in TNF-α-stimulated HeLa cells. This com- pound suppressed NF-KB activation through the inhibition of IKB kinase （IKK） activation. ISOA also has an influ- ence on upstream signaling of IKK through the inhibition of expression of adaptor proteins, TNF receptor-associated factor 2 （TRAF2） and receptor interacting protein 1 （RIP1）. Consequently, ISOA blocked the phosphorylation and degradation of the inhibitor of NF-KB alpha （IKBα） , and subsequent phosphorylation and nuclear translocation of p65. The suppression of NF-KB activation by ISOA led to the down-regulation of target genes involved in inflam- mation, proliferation, angiogenesis and invasion, as well as potentiation of TNF-α-induced apoptosis at least in part through activation of caspase-8. Taken together, this study extends our understanding on the mechanisms underly- ing the anti-inflammatory and anti-cancer activities of ISOA. Our findings provide new insight into the molecular mechanisms and a potential application of ISOA for inflammatory diseases as well as certain cancers associated with abnormal NF-KB activation.
文摘A new flavone glycoside, 5,8-dihydroxy-4',6,7-trimethoxyflavone 8-O-(-D-glucopyranoside 1, together with three known flavonoids, pedalitin 2, cirsimartin 3 and genkwanin 4, were isolated from the aerial parts of Isodon enanderianus. Their structures were determined on the basis of spectral data.
文摘A new flavonoid glycoside, 5, 7-dihydroxy-4'-methoxyflavonoid 7-Q-[6-O-(4-O-acetyl-alpha-L-rhamnosyl)-3-O-beta-D-glucosyl]-6-O-acetyl-beta-D-glucoside was isolated from Thalictrum przewalskii. Its structure was determined on basis of spectroscopic evidences.
基金the Natural Science Foundation of Shaanxi Province (No. 2001K11-G5).
文摘Two hydrates of sodium 5,7-dihydroxy-6,4'-dimethoxyisoflavone-3'-sulfonate ([Na(H2O)](C17H13O6SO3)2H2O, 1) and nickel 5,7-dihydroxy-6,4'-dimethoxyisoflavone-3'-sulfonate ([Ni(H2O)6](C17H13O6SO3)24H2O, 2) were syn-thesized and characterized by IR, 1H NMR and X-ray diffraction analyses. The hydrate 1 crystallizes in the mono-clinic system, space group P2(1) with a=0.8201(9) nm, b=0.8030(8) nm, c=1.5361(16) nm, =102.052(12), V=0.9893(18) nm3, Dc=1.579 g/cm3, Z=2, =0.252 nm-1, F(000)=488, R=0.0353, wR=0.0873. The hydrate 2 belongs to triclinic system, space group P-1 with a=0.7411(3) nm, b=0.8333(3) nm, c=1.7448(7) nm, a=86.361(6), 撸?6.389(5), ?=88.999(3), V=1.0731(7) nm3, Dc=1.587 g/cm3, Z=1, =0.649 mm-1, F(000)=534. In the structure of 1, the sodium cation is coordinated by six oxygen atoms and two adjacent ones are bridged by three oxygen atoms to form an octahedron chain. The C—H…p hydrogen bonds exist between two isoflavone molecules in the structure of 2. Meanwhile, hydrogen bonds in two compounds, link themselves to assemble two three-dimensional network structures, respectively.
文摘A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots of Stellera chamaejasme L. together with known chamaechromone. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.
基金One of the authors(J.Wandji)is grateful for grant(No.F/2624-3F)from the International Foundation for Science(Sweden)the sponsorship of the"UniversitéParis Descartes,France"during his multiple research visits in Paris.
文摘Two new compounds 7-hydroxy-5-O-（β-D-glucopyranoside） flavan （1） and （Z）-4＇,6＇-dihydroxy-2＇-O-（β-D-glucopyranoside） chalcone （2）, along with eight known compounds, were isolated from the stem bark of Drypetes parvifolia （Euphorbiaceae）. Their structures were established on the basis of spectroscopic analysis and chemical evidence.
