Objective To analyze patent application status of Scutellaria Barbata industrial chain and provide some suggestions for its patent application and product development.Methods Patent data were collected through IncoPat...Objective To analyze patent application status of Scutellaria Barbata industrial chain and provide some suggestions for its patent application and product development.Methods Patent data were collected through IncoPat patent analysis system.Meanwhile,the patent analysis method combined with text mining method was adopted to analyze the situation and development trend of patent application in China’s Scutellaria Barbata industrial chain by using pie chart,bubble chart,trend chart and other visual charts to display the results.Results and Conclusion The patent application of Scutellaria Barbata in China mainly experienced three stages:Slow development,rapid development,and recession period.The number of patents is large,but the authorization rate is low.Individuals and enterprises are the main applicants for patent applications.Product development is involved in the whole industrial chain,but it basically focuses on its efficacy in downstream drugs,health food and other aspects.Therefore,government should enhance the awareness of patent protection,encourage collaborative innovation in industry-university-research to promote the combination of basic research and market application.Besides,it should provide theoretical support to tackle the problem of short board products,which can promote the transformation of scientific and technological achievements and contribute to the upgrading of Scutellaria Barbata industrial chain.展开更多
OBJECTIVE To investigate the effect of SBF on cortical cytoplasm apoptotic factors disturbances induced by complex Aβ25-35in rats.METHODS The cerebral injuries model was established by rats received intracere-brovent...OBJECTIVE To investigate the effect of SBF on cortical cytoplasm apoptotic factors disturbances induced by complex Aβ25-35in rats.METHODS The cerebral injuries model was established by rats received intracere-broventricular injection of RHTGF-β1,Aβ25-35and Al Cl3and then accepted SBF treatment.All the rats were sacrificed by decapitation for indicators detection at last the drug treatment.Western blotting method was for caspase-3 protein expression and RT-PCR method detected cytochrome c,apoptotic protease activating factor-1(Apaf-1),caspase-9 m RNA expression in cortical cytoplasm.RESULTS The protein expression of caspase-3in cortical cytoplasm of rats was assayed by Western blotting.The results indicated that compared with the sham group,the caspase-3 protein expression of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,the increased expression can be obviously reversed by SBF at doses of 35,70 and 140mg·kg-1,as compared with model group(P<0.01).The Cyt-C,Apaf-1 and caspase-9 m RNA expressions in cortical cytoplasm of rats were determined by RT-PCR.The results indicated that compared with the sham group,the Cyt-C Apaf-1 and caspase-9 m RNA relative expressions of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,these increased expressions can be differently reversed by SBF at doses of 35,70 and 140 mg·kg-1,as compared with model group(P<0.01).CONCLUSION SBF can definitely improve rats′cortical cytoplasm apoptotic factors disorders induced by complex Aβ25-35,which maybe benefit for treatment of degenerative disease.展开更多
AIM: To observe the attenuation of ethanol extract of Herba Scutellaria barbata(SE) against diabetic retinopathy(DR) and its engaged mechanism.METHODS: C57BL/6J mice were intraperitoneally injected with streptozotocin...AIM: To observe the attenuation of ethanol extract of Herba Scutellaria barbata(SE) against diabetic retinopathy(DR) and its engaged mechanism.METHODS: C57BL/6J mice were intraperitoneally injected with streptozotocin(STZ, 55 mg/kg) for 5 consecutive days to induce diabetes. The diabetic mice were orally given with SE(100, 200 mg/kg) for 1mo at 1mo after STZ injection. Blood-retinal barrier(BRB) breakdown was detected by using Evans blue permeation assay. Real-time polymerase chain reaction(RT-PCR), Western blot and immunofluorescence staining were used to detect m RNA and protein expression. Enzyme-linked immunosorbent assay(ELISA) was used to detect serum contents of tumor necrosis factor-α(TNF-α) and interleukin(IL)-1β.RESULTS: SE(100, 200 mg/kg) reversed the breakdown of BRB in STZ-induced diabetic mice. The decreased expression of retinal claudin-1 and claudin-19, which are both tight junction(TJ) proteins, was reversed by SE. SE decreased the increased serum contents and retinal m RNA expression of TNF-α and IL-1β. SE also decreased the increased retinal expression of intercellular cell adhesion molecule-1(ICAM-1). SE reduced the increased phosphorylation of nuclear factor kappa B(NFκB) p65 and its subsequent nuclear translocation in retinas from STZinduced diabetic mice. Results of Western blot and retinal immunofluorescence staining of ionized calcium-binding adapter molecule 1(Iba1) demonstrated that SE abrogated the activation of microglia cells in STZ-induced diabetic mice.CONCLUSION: SE attenuates the development of DR by inhibiting retinal inflammation and restoring the decreased expression of TJ proteins including claudin-1 and claudin-19.展开更多
Objective: To investigate the effect of the ethanol extract of Scutellaria barbata D. Don(EESB) on colorectal cancer(CRC) growth and Wnt/β-catenin signaling pathway in vivo and in vitro. Methods: In vivoexperiment, C...Objective: To investigate the effect of the ethanol extract of Scutellaria barbata D. Don(EESB) on colorectal cancer(CRC) growth and Wnt/β-catenin signaling pathway in vivo and in vitro. Methods: In vivoexperiment, CRC xenograft mouse model was constructed with injection of HT-29 cells. Following xenograft implantation, twenty mice were randomly divided into EESB-treated group(n=10) and control group(n=10) by a random number table, and were given with intra-gastric administration of 2 g/kg EESB or saline, 5 days a week for 16 days, respectively. At the end of experiment, tumors were removed and weighed by electronic scales. The proliferation biomarker Ki-67 of tumor was evaluated by immunohistochemistry(IHC) assay. In vitro study, HT-29 cells were treated with 0, 0.5, 1.5, 2.5 mg/m L EESB for 24 h. At the end of the treatment, the viability and survival of HT-29 cells were determined by methylthiazolyldiphenyl-tetrazolium bromide(MTT) assay and colony formation assay, respectively. The m RNA expression of c-Myc, Survivin and adenomatous polyposis coli(APC) was examined by reverse transcription-polymerase chain reaction(RT-PCR) both in tumor tissues of CRC xenograft mice and HT-29 cells. Protein expression of c-Myc, Survivin, APC, and β-catenin as well as β-catenin phosphorylation level were evaluated by IHC assay or Western blotting. Results: EESB significantly reduced tumor weight in CRC xenografts mice, compared with the control group(P<0.05). IHC assay showed that EESB significantly inhibited protein expression of Ki-67 in tumor tissues(P<0.05). MTT assay showed that EESB significantly reduced HT-29 cell viability in a dose-dependent manner(P<0.05). Colony formation assay showed that EESB dose-dependently decreased the survival of HT-29 cells(P<0.05). In addition, RT-PCR assay showed that EESB decreased the m RNA expression of c-Myc and Survivin and increased APC expression, both in tumor tissues of CRC xenograft mice and HT-29 cells(P<0.05). IHC assay or Western blotting showed that EESB decreased protein expression of β-catenin, c-Myc and Survivin, as well as increased APC expression and β-catenin phosphorylation in tumor tissues or HT-29 cells(P<0.05). Conclusions: EESB significantly reduced tumor growth in CRC xenografts mice, and inhibited the viability and survival of HT-29 cells. EESB could suppress the activation of the Wnt/β-catenin pathway, which might be one of the mechanisms whereby Scutellaria barbata D. Don exerts its anticancer activity.展开更多
Two new neo-clerodane diterpenoids, 6,7-dibenzoyloxybarbatin C (1, named barbatin D) and 6-(2-acetoxy-3- methylbutanoloxy)-7-(2-carbonyl-3-methylbutanoyloxy) barbatin C (2, named barbatin E) were isolated from the who...Two new neo-clerodane diterpenoids, 6,7-dibenzoyloxybarbatin C (1, named barbatin D) and 6-(2-acetoxy-3- methylbutanoloxy)-7-(2-carbonyl-3-methylbutanoyloxy) barbatin C (2, named barbatin E) were isolated from the whole plant of Scutellaria barbata D. Don. Their structures were elucidated by spectroscopic methods including extensive 1D and 2D NMR analyses. In vitro, compounds 1–2 showed cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with IC50 values in the range of 3.5–6.7 μM.展开更多
目的 基于网络药理学及分子对接技术,探究白花蛇舌草和半枝莲药治疗卵巢癌的作用机制。并对药对活性成分槲皮素进行体外细胞实验,验证其对卵巢癌的作用。方法 从中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems P...目的 基于网络药理学及分子对接技术,探究白花蛇舌草和半枝莲药治疗卵巢癌的作用机制。并对药对活性成分槲皮素进行体外细胞实验,验证其对卵巢癌的作用。方法 从中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology,TCMSP)数据库筛选白花蛇舌草和半枝莲的活性成分并找出对应的靶点;在GeneCards数据库中检索出卵巢癌相关靶点;用jvenn在线作图工具得到药对和疾病相同的靶点交集;将交集靶点导入STRING平台,构建蛋白质-蛋白质相互作用(protein-protein interaction network,PPI)关系,用Cytoscape做出白花蛇舌草和半枝莲药对治疗卵巢癌的主要靶点图,用Metascape数据库对主要靶点进行基因本体(GO)富集分析和京都基因与基因组百科全书(KEGG)通路富集分析。用分子对接对结果进行验证。并对白花蛇舌草-半枝莲活性成分槲皮素进行CCK-8细胞增殖实验和流式细胞术检测细胞凋亡实验。结果 与卵巢癌相关的白花蛇舌草-半枝莲药对成分-靶点网络中包含30种成分、109个靶点。其相关性位于前3位的候选化合物分子为槲皮素、木犀草素、β-谷甾醇。这些成分通过AKT1、BCL2L1、CASP3、CASP7等信号蛋白来抑制卵巢癌细胞的生长和转移,涉及信号通路有癌症的途径、乙型肝炎、脂质和动脉粥样硬化、AGE-RAGE信号通路在糖尿病并发症中的应用、PI3K-AKT信号通路等。分子对接结果显示核心成分与核心靶点均有较好的结合能力。不同浓度槲皮素可明显抑制卵巢癌细胞增殖,且浓度越高细胞抑制率越高,细胞凋亡率也随浓度增高,数据结果差异有统计学意义(P<0.01)。结论 从网络药理学和分子对接技术得出白花蛇舌草和半枝莲药对可通过多成分、多靶点、多通路治疗卵巢癌的作用机制。槲皮素能有效抑制卵巢癌细胞并促进其凋亡。展开更多
文摘Objective To analyze patent application status of Scutellaria Barbata industrial chain and provide some suggestions for its patent application and product development.Methods Patent data were collected through IncoPat patent analysis system.Meanwhile,the patent analysis method combined with text mining method was adopted to analyze the situation and development trend of patent application in China’s Scutellaria Barbata industrial chain by using pie chart,bubble chart,trend chart and other visual charts to display the results.Results and Conclusion The patent application of Scutellaria Barbata in China mainly experienced three stages:Slow development,rapid development,and recession period.The number of patents is large,but the authorization rate is low.Individuals and enterprises are the main applicants for patent applications.Product development is involved in the whole industrial chain,but it basically focuses on its efficacy in downstream drugs,health food and other aspects.Therefore,government should enhance the awareness of patent protection,encourage collaborative innovation in industry-university-research to promote the combination of basic research and market application.Besides,it should provide theoretical support to tackle the problem of short board products,which can promote the transformation of scientific and technological achievements and contribute to the upgrading of Scutellaria Barbata industrial chain.
基金The project supported by Hebei Provincial Natural Science Foundation(C2009001007,H2014406048)Hebei Provincial Administration of Traditional Chinese Medicine of China(05027,2014062)the Key Discipline Construction in Institution of High Education in Hebei Province
文摘OBJECTIVE To investigate the effect of SBF on cortical cytoplasm apoptotic factors disturbances induced by complex Aβ25-35in rats.METHODS The cerebral injuries model was established by rats received intracere-broventricular injection of RHTGF-β1,Aβ25-35and Al Cl3and then accepted SBF treatment.All the rats were sacrificed by decapitation for indicators detection at last the drug treatment.Western blotting method was for caspase-3 protein expression and RT-PCR method detected cytochrome c,apoptotic protease activating factor-1(Apaf-1),caspase-9 m RNA expression in cortical cytoplasm.RESULTS The protein expression of caspase-3in cortical cytoplasm of rats was assayed by Western blotting.The results indicated that compared with the sham group,the caspase-3 protein expression of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,the increased expression can be obviously reversed by SBF at doses of 35,70 and 140mg·kg-1,as compared with model group(P<0.01).The Cyt-C,Apaf-1 and caspase-9 m RNA expressions in cortical cytoplasm of rats were determined by RT-PCR.The results indicated that compared with the sham group,the Cyt-C Apaf-1 and caspase-9 m RNA relative expressions of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,these increased expressions can be differently reversed by SBF at doses of 35,70 and 140 mg·kg-1,as compared with model group(P<0.01).CONCLUSION SBF can definitely improve rats′cortical cytoplasm apoptotic factors disorders induced by complex Aβ25-35,which maybe benefit for treatment of degenerative disease.
基金Supported by the National Natural Science Foundation of China(No.81173517No.81322053)
文摘AIM: To observe the attenuation of ethanol extract of Herba Scutellaria barbata(SE) against diabetic retinopathy(DR) and its engaged mechanism.METHODS: C57BL/6J mice were intraperitoneally injected with streptozotocin(STZ, 55 mg/kg) for 5 consecutive days to induce diabetes. The diabetic mice were orally given with SE(100, 200 mg/kg) for 1mo at 1mo after STZ injection. Blood-retinal barrier(BRB) breakdown was detected by using Evans blue permeation assay. Real-time polymerase chain reaction(RT-PCR), Western blot and immunofluorescence staining were used to detect m RNA and protein expression. Enzyme-linked immunosorbent assay(ELISA) was used to detect serum contents of tumor necrosis factor-α(TNF-α) and interleukin(IL)-1β.RESULTS: SE(100, 200 mg/kg) reversed the breakdown of BRB in STZ-induced diabetic mice. The decreased expression of retinal claudin-1 and claudin-19, which are both tight junction(TJ) proteins, was reversed by SE. SE decreased the increased serum contents and retinal m RNA expression of TNF-α and IL-1β. SE also decreased the increased retinal expression of intercellular cell adhesion molecule-1(ICAM-1). SE reduced the increased phosphorylation of nuclear factor kappa B(NFκB) p65 and its subsequent nuclear translocation in retinas from STZinduced diabetic mice. Results of Western blot and retinal immunofluorescence staining of ionized calcium-binding adapter molecule 1(Iba1) demonstrated that SE abrogated the activation of microglia cells in STZ-induced diabetic mice.CONCLUSION: SE attenuates the development of DR by inhibiting retinal inflammation and restoring the decreased expression of TJ proteins including claudin-1 and claudin-19.
基金Supported by the Natural Science Foundation of Fujian Province of China(No.2013J01333)the Youth Science Foundation of the Health Department of Fujian Province(2012-2-60)the Developmental Fund of Chen Keji Integrative Medicine(No.CKJ2015008)
文摘Objective: To investigate the effect of the ethanol extract of Scutellaria barbata D. Don(EESB) on colorectal cancer(CRC) growth and Wnt/β-catenin signaling pathway in vivo and in vitro. Methods: In vivoexperiment, CRC xenograft mouse model was constructed with injection of HT-29 cells. Following xenograft implantation, twenty mice were randomly divided into EESB-treated group(n=10) and control group(n=10) by a random number table, and were given with intra-gastric administration of 2 g/kg EESB or saline, 5 days a week for 16 days, respectively. At the end of experiment, tumors were removed and weighed by electronic scales. The proliferation biomarker Ki-67 of tumor was evaluated by immunohistochemistry(IHC) assay. In vitro study, HT-29 cells were treated with 0, 0.5, 1.5, 2.5 mg/m L EESB for 24 h. At the end of the treatment, the viability and survival of HT-29 cells were determined by methylthiazolyldiphenyl-tetrazolium bromide(MTT) assay and colony formation assay, respectively. The m RNA expression of c-Myc, Survivin and adenomatous polyposis coli(APC) was examined by reverse transcription-polymerase chain reaction(RT-PCR) both in tumor tissues of CRC xenograft mice and HT-29 cells. Protein expression of c-Myc, Survivin, APC, and β-catenin as well as β-catenin phosphorylation level were evaluated by IHC assay or Western blotting. Results: EESB significantly reduced tumor weight in CRC xenografts mice, compared with the control group(P<0.05). IHC assay showed that EESB significantly inhibited protein expression of Ki-67 in tumor tissues(P<0.05). MTT assay showed that EESB significantly reduced HT-29 cell viability in a dose-dependent manner(P<0.05). Colony formation assay showed that EESB dose-dependently decreased the survival of HT-29 cells(P<0.05). In addition, RT-PCR assay showed that EESB decreased the m RNA expression of c-Myc and Survivin and increased APC expression, both in tumor tissues of CRC xenograft mice and HT-29 cells(P<0.05). IHC assay or Western blotting showed that EESB decreased protein expression of β-catenin, c-Myc and Survivin, as well as increased APC expression and β-catenin phosphorylation in tumor tissues or HT-29 cells(P<0.05). Conclusions: EESB significantly reduced tumor growth in CRC xenografts mice, and inhibited the viability and survival of HT-29 cells. EESB could suppress the activation of the Wnt/β-catenin pathway, which might be one of the mechanisms whereby Scutellaria barbata D. Don exerts its anticancer activity.
基金the National Natural Science Foundation of China (20772104).
文摘Two new neo-clerodane diterpenoids, 6,7-dibenzoyloxybarbatin C (1, named barbatin D) and 6-(2-acetoxy-3- methylbutanoloxy)-7-(2-carbonyl-3-methylbutanoyloxy) barbatin C (2, named barbatin E) were isolated from the whole plant of Scutellaria barbata D. Don. Their structures were elucidated by spectroscopic methods including extensive 1D and 2D NMR analyses. In vitro, compounds 1–2 showed cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with IC50 values in the range of 3.5–6.7 μM.
文摘目的 基于网络药理学及分子对接技术,探究白花蛇舌草和半枝莲药治疗卵巢癌的作用机制。并对药对活性成分槲皮素进行体外细胞实验,验证其对卵巢癌的作用。方法 从中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology,TCMSP)数据库筛选白花蛇舌草和半枝莲的活性成分并找出对应的靶点;在GeneCards数据库中检索出卵巢癌相关靶点;用jvenn在线作图工具得到药对和疾病相同的靶点交集;将交集靶点导入STRING平台,构建蛋白质-蛋白质相互作用(protein-protein interaction network,PPI)关系,用Cytoscape做出白花蛇舌草和半枝莲药对治疗卵巢癌的主要靶点图,用Metascape数据库对主要靶点进行基因本体(GO)富集分析和京都基因与基因组百科全书(KEGG)通路富集分析。用分子对接对结果进行验证。并对白花蛇舌草-半枝莲活性成分槲皮素进行CCK-8细胞增殖实验和流式细胞术检测细胞凋亡实验。结果 与卵巢癌相关的白花蛇舌草-半枝莲药对成分-靶点网络中包含30种成分、109个靶点。其相关性位于前3位的候选化合物分子为槲皮素、木犀草素、β-谷甾醇。这些成分通过AKT1、BCL2L1、CASP3、CASP7等信号蛋白来抑制卵巢癌细胞的生长和转移,涉及信号通路有癌症的途径、乙型肝炎、脂质和动脉粥样硬化、AGE-RAGE信号通路在糖尿病并发症中的应用、PI3K-AKT信号通路等。分子对接结果显示核心成分与核心靶点均有较好的结合能力。不同浓度槲皮素可明显抑制卵巢癌细胞增殖,且浓度越高细胞抑制率越高,细胞凋亡率也随浓度增高,数据结果差异有统计学意义(P<0.01)。结论 从网络药理学和分子对接技术得出白花蛇舌草和半枝莲药对可通过多成分、多靶点、多通路治疗卵巢癌的作用机制。槲皮素能有效抑制卵巢癌细胞并促进其凋亡。
