使用超高效液相色谱⁃串联质谱仪,采用同位素内标法定量,建立枸杞中苦参碱和氧化苦参碱的测定方法。样品经1.0%磷酸水溶液超声提取,强阳离子固相萃取柱净化,10 mL 5%氨水甲醇溶液洗脱,采用0.1%甲酸水溶液和甲醇为流动相,梯度洗脱,通过T3...使用超高效液相色谱⁃串联质谱仪,采用同位素内标法定量,建立枸杞中苦参碱和氧化苦参碱的测定方法。样品经1.0%磷酸水溶液超声提取,强阳离子固相萃取柱净化,10 mL 5%氨水甲醇溶液洗脱,采用0.1%甲酸水溶液和甲醇为流动相,梯度洗脱,通过T3色谱柱分离,电喷雾离子源正离子扫描模式、多反应监测模式检测。通过考察不同种类提取溶剂、超声时间、固相萃取条件下目标化合物峰面积,确定最优前处理方式。结果表明:苦参碱和氧化苦参碱在0.5~50.0μg/kg范围内呈现良好线性关系,相关系数(R2)均大于0.999。方法检出限0.05μg/kg,定量限0.2μg/kg。低、中、高3个浓度加标回收试验,苦参碱回收率范围在76.3%~90.7%,相对标准偏差(relative standard deviation,RSD)在2.2%~7.4%,氧化苦参碱回收率范围在79.2%~89.0%,RSD在3.1%~6.6%。该方法适用于枸杞中苦参碱和氧化苦参碱检测。展开更多
AIM:To determine the antiviral mechanism or target of oxymatrine against hepatitis B virus(HBV).METHODS:HepG2.2.15 cells were incubated with culture medium containing 500 μg/mL of oxymatrine for 2 and 5 d.The surface...AIM:To determine the antiviral mechanism or target of oxymatrine against hepatitis B virus(HBV).METHODS:HepG2.2.15 cells were incubated with culture medium containing 500 μg/mL of oxymatrine for 2 and 5 d.The surface antigen of HBV(HBsAg) and e antigen of HBV(HBeAg) in supernatant were determined by ELISA.HBV DNA in supernatant,and intracellular covalently closed circular DNA(cccDNA),relaxed circular DNA(rcDNA) and pregenomic RNA(pgRNA) were quantif ied by specif ic real-time polymerase chain reaction(PCR) or reverse transcription(RT)-PCR.RESULTS:Treatment with oxymatrine for 2 d and 5 d reduced the production of HBV by the cell line,as indicated by the decline of HBsAg(22.67%,t = 5.439,P = 0.0322 and 22.39%,t = 5.376,P = 0.0329,respectively),HBeAg(55.34%,t = 9.859,P = 0.0101 and 43.97%,t = 14.080,P = 0.0050) and HBV DNA(40.75%,t = 4.570,P = 0.0447 and 75.32%,t = 14.460,P = 0.0047) in the supernatant.Intracellular cccDNA was also markedly reduced by 63.98%(t = 6.152,P = 0.0254) and 80.83%(t = 10.270,P = 0.0093),and intracellular rcDNA by 34.35%(t = 4.776,P = 0.0413) and 39.24%(t = 10.050,P = 0.0097).In contrast,intracellular pgRNA increased by 6.90-fold(t = 8.941,P = 0.0123) and 3.18-fold(t = 7.432,P = 0.0176) after 500 μg/mL of oxymatrine treatment for 2 d and 5 d,respectively.CONCLUSION:Oxymatrine may inhibit the replication of HBV by interfering with the process of packaging pgRNA into the nucleocapsid,or inhibiting the activity of the viral DNA polymerase.展开更多
This study was aimed to investigate the role of the delta-opioid receptor (DOR)-β-arrestinl-Bcl-2 signal transduction pathway in the pathogenesis of ulcerative colitis (UC) and the intervention effects of oxymatr...This study was aimed to investigate the role of the delta-opioid receptor (DOR)-β-arrestinl-Bcl-2 signal transduction pathway in the pathogenesis of ulcerative colitis (UC) and the intervention effects of oxymatrine on UC. Forty Sprague-Dawley rats were divided into nor- mal group, model group, oxymatrine-treated group and mesalazine-treated group (n=10 each) at ran- dom. The rat UC model was established by intra-colonic injection of trinitrobenzene sulfonic acid in the model group and two treatment groups. The rats in oxymatrine-treated group were subjected to intramuscular injection of oxymatrine [63 mg/(kg·day)] for 15 days, and those in mesalazine-treated group given mesalazine solution [0.5 g/(kg·day)] by gastric lavage for the same days. Animals in normal group and model group were administered 3 mL water by gastric lavage for 15 days. On the 16th day, after fasting for 24 h, the rats were sacrificed for the removal of colon tissues. The expres- sion levels of DOR, β-arrestinl and Bcl-2 were determined in colon tissues by immunohistochemistry and real-time quantitative polymerase chain reaction (RT-PCR), respectively. It was found that the expression levels of DOR, [3-arrestinl and Bcl-2 protein and mRNA were significantly increased in the model group as compared with the other groups (P〈0.05). They were conspicuously decreased in both mesalazine-treated and oxymatrine-treated groups in contrast to the model group (P〈0.05). No statistically significant difference was noted in these indices between mesalazine- and oxyma- trine-treated groups (P〉0.05). This study indicated that the DOR-β-arrestinl-Bcl-2 signal transduc- tion pathway may participate in the pathogenesis of UC. Moreover, oxymatrine can attenuate the de- velopment of UC by regulating the DOR-β-arrestin 1-Bcl-2 signal transduction pathway.展开更多
AIM To evaluate the effect of oxymatrine(OMT) on hepatocyte apoptosis in rats with lipopolysaccharide(LPS)/D-galactosamine(D-Gal N)-induced acute liver failure(ALF). METHODS LPS/D-Gal N was used to establish a model o...AIM To evaluate the effect of oxymatrine(OMT) on hepatocyte apoptosis in rats with lipopolysaccharide(LPS)/D-galactosamine(D-Gal N)-induced acute liver failure(ALF). METHODS LPS/D-Gal N was used to establish a model of ALF in rats. To evaluate the effect of OMT, we assessed apoptosis by transmission electron microscopy, and the pathological changes in the liver by light microscopy with hematoxylin and eosin staining. An automated biochemical analyzer was used to measure serum alanine aminotransferase(ALT) and aspartate aminotransferase(AST). Enzyme-linked immunosorbent assay was used to determine the levels of tumor necrosis factor(TNF)-α and interleukin(IL)-1β. Western blotting was used to detect protein levels in liver tissues. Streptavidin peroxidase immunohistochemistry was used to observe expression of Toll-like receptor(TLR)4, active caspase-3, Bax and Bcl-2. RESULTS All rats in the normal control and OMT-pretreated groups survived. The mortality rate in the model group was 30%. OMT preconditioning down-regulated apoptosis of hepatocytes and ameliorated pathological changes in liver tissue. The levels of AST, ALT, TNF-α and IL-1β in the model group increased significantly, and were significantly reduced by OMT pretreatment. OMT pretreatment down-regulated expression of TLR4 and active caspase-3 and the Bax/Bcl-2 ratio, and upregulated expression of P-AktSer473(Akt phosphorylated at serine 473) and P-GSK3βSer9(glycogen synthase kinase 3β phosphorylated at serine 9) induced by LPS/D-Gal N. CONCLUSION OMT inhibits hepatocyte apoptosis by suppressing the TLR4/PI3K/Akt/GSK-3β signaling pathway, which suggests that OMT is an effective candidate for ameliorating acute liver failure.展开更多
The effects of Oxymatrine (Oxy) on the proliferation and apoptosis of human esophageal carcinoma Ecal09 cell line and the mechanism were investigated. The human esophageal carcinoma Eca 109 celis were cultured in vi...The effects of Oxymatrine (Oxy) on the proliferation and apoptosis of human esophageal carcinoma Ecal09 cell line and the mechanism were investigated. The human esophageal carcinoma Eca 109 celis were cultured in vitro. The Oxy-induced apoptosis of Eca 109 cells was assayed by using flow cytometry. The expressions of p-ERKII2, Cyclin D1, p21^waf/cipl, Bax and Bcl-2 were detected by Western blot. Flow cytometry revealed that Oxy could induce the apoptosis of Eca l09 cells. Western blot showed that Oxy of different concentrations suppressed the expressions of p-ERK1/2, Cyclin D1 and Bcl-2, but up-regulated the expression of p21waf/cip1 and Bax, and the ratio of Bax/Bcl-2 was increased. It was suggested the Oxy could induce the apoptosis of Eca l09 cells, which might be related to the upregulation of p21waf/cip1 and the downregulation of p-ERK1/2, Cyclin D1 and p21^waf/cip1. The possible pathway may be related to Bcl-2/Bax.展开更多
Cerebral neuroinflammation models were established by injecting 10μg lipopolysaccharide into the hippocampus of male Sprague-Dawley rats. The rats were treated with an intraperitoneal injection of 120, 90, or 60 mg/k...Cerebral neuroinflammation models were established by injecting 10μg lipopolysaccharide into the hippocampus of male Sprague-Dawley rats. The rats were treated with an intraperitoneal injection of 120, 90, or 60 mg/kg oxymatrine daily for three days prior to the lipopolysaccharide injection. Twenty-four hours after model induction, the hippocampus was analyzed by real-time quantitative PCR, and the cerebral cortex was analyzed by enzyme-linked immunosorbent assay and western blot assay. The results of the enzyme-linked immunosorbent assay and the real-time quantitative PCR showed that the secretion and mRNA expression of the pro-inflammatory cytokines interleukin-113 and tumor necrosis factor-a were significantly decreased in the hippocampus and cerebral cortex of model rats treated with oxymatrine. Western blot assay and real-time quantitative PCR analysis indicated that toll-like receptor 4 mRNA and protein expression were significantly decreased in the groups receiving different doses of oxymatrine. Additionally, 120 and 90 mg/kg oxymatrine were shown to reduce protein levels of nuclear factor-KB p65 in the nucleus and of phosphorylated IKBa in the cytoplasm of brain cells, as detected by western blot assay. Experimental findings indicate that oxymatrine may inhibit neuroinflammation in rat brain via downregulating the expression of molecules in the toll-like receptor 4/nuclear factor-KB signaling Dathwav.展开更多
Oxymatrine (OM)/N-succinyl-chitosan (Suc-Chi, with a degree of substitution being 0. 32) was synthesized via the ring-opening reaction of succinic anhydride with chitosan in dimethyl sulfoxide. OM-loaded Suc-Chi n...Oxymatrine (OM)/N-succinyl-chitosan (Suc-Chi, with a degree of substitution being 0. 32) was synthesized via the ring-opening reaction of succinic anhydride with chitosan in dimethyl sulfoxide. OM-loaded Suc-Chi nanoparticles were prepared by an ionotropic gelation process and OM was quantified via the HPLC method: The influences of the initial OM concentration on the nanoparticle characteristics and OM release behavior were evaluated. The nanoparticles were found to have a mean diameter within a range of 267-392 nm, a positive surface charge, and a zeta potential in the range of 19-27 inV. The formulation with an initial OM concentration of 100μg/mL provided the highest loaded capacity(0. 77% ) and the highest extent of the released OM (68% at 24 h), suggesting the possibility to achieve a therapeutic dose. According to the data obtained, this Suc-Chi-based nanotechnology will open up new and interesting prospects for the development of new anticancer drugs.展开更多
The EC50 values of matrine and oxymatrine against five forest pathogenic fungi (Fusarium oxysporum, Valsa pini, Cladosporium oxysporum, Sphaeropsis sapinea, Marssonina brunnea) were examined by bioassay methods. The...The EC50 values of matrine and oxymatrine against five forest pathogenic fungi (Fusarium oxysporum, Valsa pini, Cladosporium oxysporum, Sphaeropsis sapinea, Marssonina brunnea) were examined by bioassay methods. The results demonstrated that matrine and oxymatrine had strong inhibitory activities to the conidium germination of the tested fungi. The ECso values of matrine for inhibiting the conidium germination of Marssonina brunnea, Cladosporium oxysporum, Sphaeropsis sapinea were 123μg·mL^-1, 272 μg·mL^-1, 1133 μg·mL^-1, respectively, and the EC50 values of oxymatrine for inhibiting the conidium germination of Fusarium oxysporum, Sphaeropsis sapinea were 532μg·mL^-1, 601μg·mL^-1, respectively. The hyphal growth of the fungi was also significantly inhibited by matrine and oxymatrine. The ECs0 values of matrine inhibiting the conidium germination of Sphaeropsis sapinea, Valsa pini, Fusarium oxysporum were 428μg·mL^-1, 535 μg·mL^-1, 592 μg·mL^-1, respectively. The EC50 values of oxymatrine inhibiting the conidium germination of Valsa pini, Fusarium oxysporum were 323, 618μg·mL^-1, respectively. In the synergetic tests the ECs0 values of the mixtures of thiophanate methyl (or chlorthalonil) and matrine (or oxymatrine) were lower than 34 μg·mL^-1 while their co-toxicity coefficients were significantly higher than 1130 It indicated that the mixture of the alkaloids and the chemical had potential practical utilization in controlling certain forest fungal diseases.展开更多
Inflammatory bowel disease is thought to be regulated by the balance between Th1 and Th2 cytokines secreted by T cells, and NF-κB p65 also plays a predominant role in the intestinal inflammation. We evaluated the pot...Inflammatory bowel disease is thought to be regulated by the balance between Th1 and Th2 cytokines secreted by T cells, and NF-κB p65 also plays a predominant role in the intestinal inflammation. We evaluated the potency of oxymatrine, one of active components of Sophora Root, in inhibiting the immune responses and inflammation in 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis. The inflammation was markedly ameliorated in the oxymatrine-treated rats. The level of IL-2 was increased and that of IL-10 was decreased in colon tissue in the rat model, which was reversed by the treatment of oxymatrine. Moreover, the elevated expression of NF-κB p65 in colon tissue in the model was also improved by oxymatrine treatment. Our results suggest that oxymatrine might be beneficial for the abnormal immune responses and inflammation by regulating the unbalance of Th1 and Th2 cytokines secretion and inhibiting the expression of NF-κB p65 in colon tissue.展开更多
AIM To investigate the anti-HBV effect ofoxymatrine (oxy) in vivo.METHODS HBV transgenic mice were producedby micro-injection of a 4.2kb fragmentcontaining the complete HBV genomes.Expression level of HBsAg and HBcAg ...AIM To investigate the anti-HBV effect ofoxymatrine (oxy) in vivo.METHODS HBV transgenic mice were producedby micro-injection of a 4.2kb fragmentcontaining the complete HBV genomes.Expression level of HBsAg and HBcAg in thetransgenic mice liver was determined byimmunohistochemical assay.RESULTS Four groups (6 mice in each group)were injected intraperitoneally with oxy at thedosage of 100,200, and 300 mg/kg or with salineonce a day for 30 days. Both HBsAg and HBcAgwere positive in livers of all the six mice in thecontrol group (injected with saline), and werepositive in livers of two mice in 100 mg/kg groupand 300mg/kg group. In 200mg/kg group,HBsAg and HBcAg were negative in livers of allthe six mice. Based on the results, 200 mg/kg isthe ideal dosage to explore the effect of oxy atdifferent time points. According to the oxytreatment time, mice were divided into fourgroups: 10 d, 20 d, 30 d and 60 d (4 mice in eachgroup). Each mouse underwent liver biopsy twoweeks before the treatment of oxy. Down-regulation of HBsAg and HBcAg appeared aftertreatment of oxymatrine for 10 d and 20 d, Dane-like particles disappeared after the treatment ofoxy for 20d under electron microscopy,however, the expression level of HBsAg andHBcAg returned to normal 60 d later after oxytreatment.CONCLUSION oxymatrine can reduce thecontents of HBsAg and HBcAg in transgenic miceliver, longer treatment time and larger dosagedo not yield better effects.展开更多
文摘使用超高效液相色谱⁃串联质谱仪,采用同位素内标法定量,建立枸杞中苦参碱和氧化苦参碱的测定方法。样品经1.0%磷酸水溶液超声提取,强阳离子固相萃取柱净化,10 mL 5%氨水甲醇溶液洗脱,采用0.1%甲酸水溶液和甲醇为流动相,梯度洗脱,通过T3色谱柱分离,电喷雾离子源正离子扫描模式、多反应监测模式检测。通过考察不同种类提取溶剂、超声时间、固相萃取条件下目标化合物峰面积,确定最优前处理方式。结果表明:苦参碱和氧化苦参碱在0.5~50.0μg/kg范围内呈现良好线性关系,相关系数(R2)均大于0.999。方法检出限0.05μg/kg,定量限0.2μg/kg。低、中、高3个浓度加标回收试验,苦参碱回收率范围在76.3%~90.7%,相对标准偏差(relative standard deviation,RSD)在2.2%~7.4%,氧化苦参碱回收率范围在79.2%~89.0%,RSD在3.1%~6.6%。该方法适用于枸杞中苦参碱和氧化苦参碱检测。
基金Supported by The National Natural Scientifi c Foundation of China,No. 30070958The National Key Technologies Research and Development Program of China during the 11th Five-year Plan Period,No. 2008zx1002-006
文摘AIM:To determine the antiviral mechanism or target of oxymatrine against hepatitis B virus(HBV).METHODS:HepG2.2.15 cells were incubated with culture medium containing 500 μg/mL of oxymatrine for 2 and 5 d.The surface antigen of HBV(HBsAg) and e antigen of HBV(HBeAg) in supernatant were determined by ELISA.HBV DNA in supernatant,and intracellular covalently closed circular DNA(cccDNA),relaxed circular DNA(rcDNA) and pregenomic RNA(pgRNA) were quantif ied by specif ic real-time polymerase chain reaction(PCR) or reverse transcription(RT)-PCR.RESULTS:Treatment with oxymatrine for 2 d and 5 d reduced the production of HBV by the cell line,as indicated by the decline of HBsAg(22.67%,t = 5.439,P = 0.0322 and 22.39%,t = 5.376,P = 0.0329,respectively),HBeAg(55.34%,t = 9.859,P = 0.0101 and 43.97%,t = 14.080,P = 0.0050) and HBV DNA(40.75%,t = 4.570,P = 0.0447 and 75.32%,t = 14.460,P = 0.0047) in the supernatant.Intracellular cccDNA was also markedly reduced by 63.98%(t = 6.152,P = 0.0254) and 80.83%(t = 10.270,P = 0.0093),and intracellular rcDNA by 34.35%(t = 4.776,P = 0.0413) and 39.24%(t = 10.050,P = 0.0097).In contrast,intracellular pgRNA increased by 6.90-fold(t = 8.941,P = 0.0123) and 3.18-fold(t = 7.432,P = 0.0176) after 500 μg/mL of oxymatrine treatment for 2 d and 5 d,respectively.CONCLUSION:Oxymatrine may inhibit the replication of HBV by interfering with the process of packaging pgRNA into the nucleocapsid,or inhibiting the activity of the viral DNA polymerase.
基金supported by grants from the National Nature Science Foundation of China(No.81072944,and No.81273908)Nature Science Foundation of Hubei Province of China(No.2011CDB379)+1 种基金Postdoctoral Science Foundation of China(No.2012M510120)Doctor Fund Project of Higher Education of Ministry of Education of China(No.20110142120096)
文摘This study was aimed to investigate the role of the delta-opioid receptor (DOR)-β-arrestinl-Bcl-2 signal transduction pathway in the pathogenesis of ulcerative colitis (UC) and the intervention effects of oxymatrine on UC. Forty Sprague-Dawley rats were divided into nor- mal group, model group, oxymatrine-treated group and mesalazine-treated group (n=10 each) at ran- dom. The rat UC model was established by intra-colonic injection of trinitrobenzene sulfonic acid in the model group and two treatment groups. The rats in oxymatrine-treated group were subjected to intramuscular injection of oxymatrine [63 mg/(kg·day)] for 15 days, and those in mesalazine-treated group given mesalazine solution [0.5 g/(kg·day)] by gastric lavage for the same days. Animals in normal group and model group were administered 3 mL water by gastric lavage for 15 days. On the 16th day, after fasting for 24 h, the rats were sacrificed for the removal of colon tissues. The expres- sion levels of DOR, β-arrestinl and Bcl-2 were determined in colon tissues by immunohistochemistry and real-time quantitative polymerase chain reaction (RT-PCR), respectively. It was found that the expression levels of DOR, [3-arrestinl and Bcl-2 protein and mRNA were significantly increased in the model group as compared with the other groups (P〈0.05). They were conspicuously decreased in both mesalazine-treated and oxymatrine-treated groups in contrast to the model group (P〈0.05). No statistically significant difference was noted in these indices between mesalazine- and oxyma- trine-treated groups (P〉0.05). This study indicated that the DOR-β-arrestinl-Bcl-2 signal transduc- tion pathway may participate in the pathogenesis of UC. Moreover, oxymatrine can attenuate the de- velopment of UC by regulating the DOR-β-arrestin 1-Bcl-2 signal transduction pathway.
基金Supported by the Jiangsu Bureau of Traditional Chinese Medicine,No.YB2015177
文摘AIM To evaluate the effect of oxymatrine(OMT) on hepatocyte apoptosis in rats with lipopolysaccharide(LPS)/D-galactosamine(D-Gal N)-induced acute liver failure(ALF). METHODS LPS/D-Gal N was used to establish a model of ALF in rats. To evaluate the effect of OMT, we assessed apoptosis by transmission electron microscopy, and the pathological changes in the liver by light microscopy with hematoxylin and eosin staining. An automated biochemical analyzer was used to measure serum alanine aminotransferase(ALT) and aspartate aminotransferase(AST). Enzyme-linked immunosorbent assay was used to determine the levels of tumor necrosis factor(TNF)-α and interleukin(IL)-1β. Western blotting was used to detect protein levels in liver tissues. Streptavidin peroxidase immunohistochemistry was used to observe expression of Toll-like receptor(TLR)4, active caspase-3, Bax and Bcl-2. RESULTS All rats in the normal control and OMT-pretreated groups survived. The mortality rate in the model group was 30%. OMT preconditioning down-regulated apoptosis of hepatocytes and ameliorated pathological changes in liver tissue. The levels of AST, ALT, TNF-α and IL-1β in the model group increased significantly, and were significantly reduced by OMT pretreatment. OMT pretreatment down-regulated expression of TLR4 and active caspase-3 and the Bax/Bcl-2 ratio, and upregulated expression of P-AktSer473(Akt phosphorylated at serine 473) and P-GSK3βSer9(glycogen synthase kinase 3β phosphorylated at serine 9) induced by LPS/D-Gal N. CONCLUSION OMT inhibits hepatocyte apoptosis by suppressing the TLR4/PI3K/Akt/GSK-3β signaling pathway, which suggests that OMT is an effective candidate for ameliorating acute liver failure.
文摘The effects of Oxymatrine (Oxy) on the proliferation and apoptosis of human esophageal carcinoma Ecal09 cell line and the mechanism were investigated. The human esophageal carcinoma Eca 109 celis were cultured in vitro. The Oxy-induced apoptosis of Eca 109 cells was assayed by using flow cytometry. The expressions of p-ERKII2, Cyclin D1, p21^waf/cipl, Bax and Bcl-2 were detected by Western blot. Flow cytometry revealed that Oxy could induce the apoptosis of Eca l09 cells. Western blot showed that Oxy of different concentrations suppressed the expressions of p-ERK1/2, Cyclin D1 and Bcl-2, but up-regulated the expression of p21waf/cip1 and Bax, and the ratio of Bax/Bcl-2 was increased. It was suggested the Oxy could induce the apoptosis of Eca l09 cells, which might be related to the upregulation of p21waf/cip1 and the downregulation of p-ERK1/2, Cyclin D1 and p21^waf/cip1. The possible pathway may be related to Bcl-2/Bax.
基金supported by a project of the Priority Academic Program Development of Jiangsu Higher Education InstitutionsApplied Research and Technology Plan of Nantong City, No. k2010036+2 种基金2011 Jiangsu Graduated Students' Research and Innovation Program, No. CX2211-0640Nantong University Graduated Students' Technological and Innovative Program, No. YKC11033Students' Practice Innovative Training Project of Nantong University
文摘Cerebral neuroinflammation models were established by injecting 10μg lipopolysaccharide into the hippocampus of male Sprague-Dawley rats. The rats were treated with an intraperitoneal injection of 120, 90, or 60 mg/kg oxymatrine daily for three days prior to the lipopolysaccharide injection. Twenty-four hours after model induction, the hippocampus was analyzed by real-time quantitative PCR, and the cerebral cortex was analyzed by enzyme-linked immunosorbent assay and western blot assay. The results of the enzyme-linked immunosorbent assay and the real-time quantitative PCR showed that the secretion and mRNA expression of the pro-inflammatory cytokines interleukin-113 and tumor necrosis factor-a were significantly decreased in the hippocampus and cerebral cortex of model rats treated with oxymatrine. Western blot assay and real-time quantitative PCR analysis indicated that toll-like receptor 4 mRNA and protein expression were significantly decreased in the groups receiving different doses of oxymatrine. Additionally, 120 and 90 mg/kg oxymatrine were shown to reduce protein levels of nuclear factor-KB p65 in the nucleus and of phosphorylated IKBa in the cytoplasm of brain cells, as detected by western blot assay. Experimental findings indicate that oxymatrine may inhibit neuroinflammation in rat brain via downregulating the expression of molecules in the toll-like receptor 4/nuclear factor-KB signaling Dathwav.
文摘Oxymatrine (OM)/N-succinyl-chitosan (Suc-Chi, with a degree of substitution being 0. 32) was synthesized via the ring-opening reaction of succinic anhydride with chitosan in dimethyl sulfoxide. OM-loaded Suc-Chi nanoparticles were prepared by an ionotropic gelation process and OM was quantified via the HPLC method: The influences of the initial OM concentration on the nanoparticle characteristics and OM release behavior were evaluated. The nanoparticles were found to have a mean diameter within a range of 267-392 nm, a positive surface charge, and a zeta potential in the range of 19-27 inV. The formulation with an initial OM concentration of 100μg/mL provided the highest loaded capacity(0. 77% ) and the highest extent of the released OM (68% at 24 h), suggesting the possibility to achieve a therapeutic dose. According to the data obtained, this Suc-Chi-based nanotechnology will open up new and interesting prospects for the development of new anticancer drugs.
基金This work was supported by a project of NationalNatural Science Foundation of China (No. 30170776)
文摘The EC50 values of matrine and oxymatrine against five forest pathogenic fungi (Fusarium oxysporum, Valsa pini, Cladosporium oxysporum, Sphaeropsis sapinea, Marssonina brunnea) were examined by bioassay methods. The results demonstrated that matrine and oxymatrine had strong inhibitory activities to the conidium germination of the tested fungi. The ECso values of matrine for inhibiting the conidium germination of Marssonina brunnea, Cladosporium oxysporum, Sphaeropsis sapinea were 123μg·mL^-1, 272 μg·mL^-1, 1133 μg·mL^-1, respectively, and the EC50 values of oxymatrine for inhibiting the conidium germination of Fusarium oxysporum, Sphaeropsis sapinea were 532μg·mL^-1, 601μg·mL^-1, respectively. The hyphal growth of the fungi was also significantly inhibited by matrine and oxymatrine. The ECs0 values of matrine inhibiting the conidium germination of Sphaeropsis sapinea, Valsa pini, Fusarium oxysporum were 428μg·mL^-1, 535 μg·mL^-1, 592 μg·mL^-1, respectively. The EC50 values of oxymatrine inhibiting the conidium germination of Valsa pini, Fusarium oxysporum were 323, 618μg·mL^-1, respectively. In the synergetic tests the ECs0 values of the mixtures of thiophanate methyl (or chlorthalonil) and matrine (or oxymatrine) were lower than 34 μg·mL^-1 while their co-toxicity coefficients were significantly higher than 1130 It indicated that the mixture of the alkaloids and the chemical had potential practical utilization in controlling certain forest fungal diseases.
基金a grant from Post-doctoral Sciences Foundation of China (No. 2005037679)a research grant from National Natural Sciences Foundation of China (No. 30772878)
文摘Inflammatory bowel disease is thought to be regulated by the balance between Th1 and Th2 cytokines secreted by T cells, and NF-κB p65 also plays a predominant role in the intestinal inflammation. We evaluated the potency of oxymatrine, one of active components of Sophora Root, in inhibiting the immune responses and inflammation in 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis. The inflammation was markedly ameliorated in the oxymatrine-treated rats. The level of IL-2 was increased and that of IL-10 was decreased in colon tissue in the rat model, which was reversed by the treatment of oxymatrine. Moreover, the elevated expression of NF-κB p65 in colon tissue in the model was also improved by oxymatrine treatment. Our results suggest that oxymatrine might be beneficial for the abnormal immune responses and inflammation by regulating the unbalance of Th1 and Th2 cytokines secretion and inhibiting the expression of NF-κB p65 in colon tissue.
基金Supported by Projects of the Science Development Foundation of Shanghai, No. 994919033Tackling Key Problems in Science+1 种基金 Technology from the State ScienceTechnology Ministry, TJ99-LA01
文摘AIM To investigate the anti-HBV effect ofoxymatrine (oxy) in vivo.METHODS HBV transgenic mice were producedby micro-injection of a 4.2kb fragmentcontaining the complete HBV genomes.Expression level of HBsAg and HBcAg in thetransgenic mice liver was determined byimmunohistochemical assay.RESULTS Four groups (6 mice in each group)were injected intraperitoneally with oxy at thedosage of 100,200, and 300 mg/kg or with salineonce a day for 30 days. Both HBsAg and HBcAgwere positive in livers of all the six mice in thecontrol group (injected with saline), and werepositive in livers of two mice in 100 mg/kg groupand 300mg/kg group. In 200mg/kg group,HBsAg and HBcAg were negative in livers of allthe six mice. Based on the results, 200 mg/kg isthe ideal dosage to explore the effect of oxy atdifferent time points. According to the oxytreatment time, mice were divided into fourgroups: 10 d, 20 d, 30 d and 60 d (4 mice in eachgroup). Each mouse underwent liver biopsy twoweeks before the treatment of oxy. Down-regulation of HBsAg and HBcAg appeared aftertreatment of oxymatrine for 10 d and 20 d, Dane-like particles disappeared after the treatment ofoxy for 20d under electron microscopy,however, the expression level of HBsAg andHBcAg returned to normal 60 d later after oxytreatment.CONCLUSION oxymatrine can reduce thecontents of HBsAg and HBcAg in transgenic miceliver, longer treatment time and larger dosagedo not yield better effects.