目的:对有活性的茜草氯仿提取部位进行化学成分的分离筛选。方法:首次利用DPPH(1,1-d iphenyl-2-p icrylhydrazy)方法,对茜草提取部位进行抗氧化筛选。结果:从有活性的氯仿部位分离得到11个化合物,经波谱分析鉴定为Mollugin(1),Furomoll...目的:对有活性的茜草氯仿提取部位进行化学成分的分离筛选。方法:首次利用DPPH(1,1-d iphenyl-2-p icrylhydrazy)方法,对茜草提取部位进行抗氧化筛选。结果:从有活性的氯仿部位分离得到11个化合物,经波谱分析鉴定为Mollugin(1),Furomollugin(2),6-hydroxyrub iad in(3),A lizarin(4),6-m ethxylqu in izarin(5),1-hy-droxy-2-m ethylanthraqu inone(6),Xanthopurpurin(7),Anthragallol(8),Rub iad in(9),Ursolic ac id(10),β-sitos-terol(11)。结论:其中化合物3,4,8具有抗氧化活性,化合物10为首次从该属中分离得到。展开更多
建立以4种离子液体为萃取剂,结合超声辅助萃取,利用高效液相色谱法来测定茜草中茜草素与大叶茜草素素含量的方法。采用Purospher star RP-C18柱（4.6 mm×250 mm,5μm）,以B为甲醇、C为0.4%乙酸-水溶液为流动相,梯度洗脱,流速为0.85...建立以4种离子液体为萃取剂,结合超声辅助萃取,利用高效液相色谱法来测定茜草中茜草素与大叶茜草素素含量的方法。采用Purospher star RP-C18柱（4.6 mm×250 mm,5μm）,以B为甲醇、C为0.4%乙酸-水溶液为流动相,梯度洗脱,流速为0.85 m L·min-1,紫外检测波长为250 nm,柱温为室温。结果显示,茜草素和大叶茜草素的最佳萃取条件均为0.6 mo L·L-1的[HMIM]PF6甲醇溶液作为萃取剂,1∶80（g·m L-1）作为最佳固液比;茜草素进样量在0.01～0.04μg呈良好的线性关系（r=0.999 9）,平均回收率为97.12%;大叶茜草素进样量在0.41～1.35μg呈良好的线性关系（r=0.999 9）,平均回收率为98.10%。该实验采取环境友好型试剂作为萃取剂,提高了萃取效率,避免了有机溶剂对环境的污染,减少了对人体的伤害,操作简单,重复性好,对中药活性成分提取研究方法的创新有重要参考意义。展开更多
目的:运用网络药理学探讨茜草治疗溃疡性结肠炎的活性成分、作用靶点及信号通路等,解释其分子作用机制。方法:应用中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,...目的:运用网络药理学探讨茜草治疗溃疡性结肠炎的活性成分、作用靶点及信号通路等,解释其分子作用机制。方法:应用中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)筛选茜草的潜在活性成分及作用靶点。利用Cytoscape软件,通过TCMSP、GeneCards数据库构建“药物-成分-靶点-疾病”网络,并通过String平台及Cytoscape软件进行蛋白质-蛋白质相互作用(Protein-Protein Interaction,PPI)网络模型的构建,找出核心靶点。通过R语言对潜在靶点进行基因本体论(Gene Ontology,GO)和京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)富集分析。结果:分析结果表明,茜草中排名前3位的活性成分是β-谷甾醇、去氢-α-拉杷醌、异落叶松脂素。茜草治疗溃疡性结肠炎的潜在靶点共37个,关键靶点包括转录因子激活蛋白-1亚基JUN、半胱氨酰天冬氨酸特异性蛋白酶-3(Caspase-3,CASP3)、内皮型一氧化氮合酶(Nitric Oxide Synthase 3,NOS3)、热休克蛋白90α家族A类成员1(Heat Shock Protein HSP 90-alpha,HSP90AA1)等,主要通过影响核受体活性以及雌激素信号通路、白细胞介素17(Interleukin-17,IL-17)信号通路、糖尿病并发症晚期糖基化终末产物及其受体(AGE-RAGE)信号通路等来发挥治疗溃疡性结肠炎的作用。结论:从网络药理学的角度预测了茜草治疗溃疡性结肠炎的作用机制,证明其治疗溃疡性结肠炎具有多成分、多靶点和多途径的特点,为进一步研究提供了理论基础及方向。展开更多
Introduction: Resistance to antituberculosis drugs and adverse drug reactions remain the leading causes of tuberculosis therapeutic failure globally. Despite the increasing acceptance of medicinal plant use in combina...Introduction: Resistance to antituberculosis drugs and adverse drug reactions remain the leading causes of tuberculosis therapeutic failure globally. Despite the increasing acceptance of medicinal plant use in combination with conventional antituberculosis drugs in treatment of tuberculosis (TB) in Uganda, there is paucity of knowledge on their combination effect. Aim: This research aimed to determine combination activity of standard antituberculosis drugs with extracts of Zanthoxylum leprieurii Guill. & Perr. and Rubia cordifolia L., the two common antituberculosis medicinal plants in Uganda, against pansensitive (H37Rv) and multi-drug resistant (MDR) Mycobacterium tuberculosis strains. Materials and Methods: Two reference MTB strains (H37Rv and MDR strain) were inoculated on Middlebrook 7H11 medium containing a combination of standard antituberculosis drugs and methanol extracts of Z. leprieurii and R. cordifolia at varying concentrations. The number of colonies on the plates was observed and counted weekly for up to 8 weeks. In vitro combination activity was determined using proportion method. Mean percentage inhibition was calculated for the reduction of number of colonies on drug-extract combination medium in relation to drug-extract-free control medium. Results: Drug-extract combinations showed good combination activity against Mycobacterium tuberculosis strains when compared with individual standard anti-TB drugs. This was more exhibited against MDR strain. There was however a reduction in percentage inhibition when extracts were combined with ethambutol and streptomycin against H37Rv strain. Conclusions: Zanthoxylum leprieurii and Rubia cordifolia in combination with standard anti-TB drugs exhibited increased in vitro activity against Mycobacterium tuberculosis, especially MDR-TB strain. This justifies the local use of these plants in traditional treatment of tuberculosis especially in resistant cases in Uganda.展开更多
文摘目的:对有活性的茜草氯仿提取部位进行化学成分的分离筛选。方法:首次利用DPPH(1,1-d iphenyl-2-p icrylhydrazy)方法,对茜草提取部位进行抗氧化筛选。结果:从有活性的氯仿部位分离得到11个化合物,经波谱分析鉴定为Mollugin(1),Furomollugin(2),6-hydroxyrub iad in(3),A lizarin(4),6-m ethxylqu in izarin(5),1-hy-droxy-2-m ethylanthraqu inone(6),Xanthopurpurin(7),Anthragallol(8),Rub iad in(9),Ursolic ac id(10),β-sitos-terol(11)。结论:其中化合物3,4,8具有抗氧化活性,化合物10为首次从该属中分离得到。
文摘建立以4种离子液体为萃取剂,结合超声辅助萃取,利用高效液相色谱法来测定茜草中茜草素与大叶茜草素素含量的方法。采用Purospher star RP-C18柱（4.6 mm×250 mm,5μm）,以B为甲醇、C为0.4%乙酸-水溶液为流动相,梯度洗脱,流速为0.85 m L·min-1,紫外检测波长为250 nm,柱温为室温。结果显示,茜草素和大叶茜草素的最佳萃取条件均为0.6 mo L·L-1的[HMIM]PF6甲醇溶液作为萃取剂,1∶80（g·m L-1）作为最佳固液比;茜草素进样量在0.01～0.04μg呈良好的线性关系（r=0.999 9）,平均回收率为97.12%;大叶茜草素进样量在0.41～1.35μg呈良好的线性关系（r=0.999 9）,平均回收率为98.10%。该实验采取环境友好型试剂作为萃取剂,提高了萃取效率,避免了有机溶剂对环境的污染,减少了对人体的伤害,操作简单,重复性好,对中药活性成分提取研究方法的创新有重要参考意义。
文摘目的:运用网络药理学探讨茜草治疗溃疡性结肠炎的活性成分、作用靶点及信号通路等,解释其分子作用机制。方法:应用中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)筛选茜草的潜在活性成分及作用靶点。利用Cytoscape软件,通过TCMSP、GeneCards数据库构建“药物-成分-靶点-疾病”网络,并通过String平台及Cytoscape软件进行蛋白质-蛋白质相互作用(Protein-Protein Interaction,PPI)网络模型的构建,找出核心靶点。通过R语言对潜在靶点进行基因本体论(Gene Ontology,GO)和京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)富集分析。结果:分析结果表明,茜草中排名前3位的活性成分是β-谷甾醇、去氢-α-拉杷醌、异落叶松脂素。茜草治疗溃疡性结肠炎的潜在靶点共37个,关键靶点包括转录因子激活蛋白-1亚基JUN、半胱氨酰天冬氨酸特异性蛋白酶-3(Caspase-3,CASP3)、内皮型一氧化氮合酶(Nitric Oxide Synthase 3,NOS3)、热休克蛋白90α家族A类成员1(Heat Shock Protein HSP 90-alpha,HSP90AA1)等,主要通过影响核受体活性以及雌激素信号通路、白细胞介素17(Interleukin-17,IL-17)信号通路、糖尿病并发症晚期糖基化终末产物及其受体(AGE-RAGE)信号通路等来发挥治疗溃疡性结肠炎的作用。结论:从网络药理学的角度预测了茜草治疗溃疡性结肠炎的作用机制,证明其治疗溃疡性结肠炎具有多成分、多靶点和多途径的特点,为进一步研究提供了理论基础及方向。
文摘Introduction: Resistance to antituberculosis drugs and adverse drug reactions remain the leading causes of tuberculosis therapeutic failure globally. Despite the increasing acceptance of medicinal plant use in combination with conventional antituberculosis drugs in treatment of tuberculosis (TB) in Uganda, there is paucity of knowledge on their combination effect. Aim: This research aimed to determine combination activity of standard antituberculosis drugs with extracts of Zanthoxylum leprieurii Guill. & Perr. and Rubia cordifolia L., the two common antituberculosis medicinal plants in Uganda, against pansensitive (H37Rv) and multi-drug resistant (MDR) Mycobacterium tuberculosis strains. Materials and Methods: Two reference MTB strains (H37Rv and MDR strain) were inoculated on Middlebrook 7H11 medium containing a combination of standard antituberculosis drugs and methanol extracts of Z. leprieurii and R. cordifolia at varying concentrations. The number of colonies on the plates was observed and counted weekly for up to 8 weeks. In vitro combination activity was determined using proportion method. Mean percentage inhibition was calculated for the reduction of number of colonies on drug-extract combination medium in relation to drug-extract-free control medium. Results: Drug-extract combinations showed good combination activity against Mycobacterium tuberculosis strains when compared with individual standard anti-TB drugs. This was more exhibited against MDR strain. There was however a reduction in percentage inhibition when extracts were combined with ethambutol and streptomycin against H37Rv strain. Conclusions: Zanthoxylum leprieurii and Rubia cordifolia in combination with standard anti-TB drugs exhibited increased in vitro activity against Mycobacterium tuberculosis, especially MDR-TB strain. This justifies the local use of these plants in traditional treatment of tuberculosis especially in resistant cases in Uganda.
