目的对比研究顺式和反式二苯乙烯苷的降血脂作用。方法分别考察顺式、反式二苯乙烯苷对正常小鼠、慢性高血脂小鼠和急性高血脂小鼠血清中总胆固醇(total cholesterol,TC)、甘油三酯(triglyceride,TG)、高密度脂蛋白胆固醇(high density ...目的对比研究顺式和反式二苯乙烯苷的降血脂作用。方法分别考察顺式、反式二苯乙烯苷对正常小鼠、慢性高血脂小鼠和急性高血脂小鼠血清中总胆固醇(total cholesterol,TC)、甘油三酯(triglyceride,TG)、高密度脂蛋白胆固醇(high density lipoprotein cholesterol,HDL-C)和低密度脂蛋白胆固醇(low density lipoprotein cholesterol,LDL-C)含量的影响。结果顺式二苯乙烯苷能显著性降低高血脂小鼠血清中TC、TG及LDL-C的水平,也能显著性降低正常血脂小鼠血清中LDL-C的含量,高剂量顺式二苯乙烯苷还能显著性升高正常血脂小鼠和高血脂小鼠血清中HDL-C的水平。顺式二苯乙烯苷对正常小鼠和急性高血脂小鼠的降血脂作用与反式基本相同,但对慢性高血脂小鼠血浆中TC和TG的降低作用明显强于反式二苯乙烯苷。结论顺式二苯乙烯苷具有比反式二苯乙烯苷更好的降血脂作用。展开更多
目的采用半定量分析方法对制首乌与9个补虚药配伍后成分含量及DPPH自由基清除能力变化进行研究。方法以UPLC-DAD建立制首乌多成分半定量分析方法,对制首乌与9味常用补虚药(当归、熟地黄、白芍、党参、黄芪、甘草、麦冬、枸杞子、墨旱莲...目的采用半定量分析方法对制首乌与9个补虚药配伍后成分含量及DPPH自由基清除能力变化进行研究。方法以UPLC-DAD建立制首乌多成分半定量分析方法,对制首乌与9味常用补虚药(当归、熟地黄、白芍、党参、黄芪、甘草、麦冬、枸杞子、墨旱莲)配伍后成分含量变化进行分析。采用DPPH法分别测定单味药以及配伍药对的自由基清除能力,绘制量-效曲线并计算半数清除浓度(EC50)。采用多元统计分析方法建立制首乌中多成分含量与DPPH自由基清除能力间的量-效回归模型,筛选量-效关系中影响显著的化学标志物,并通过质谱进行定性分析。结果线性范围、准确度、精密度、重复性及稳定性5项方法学验证结果表明,半定量分析方法可用于制首乌中12个成分在配伍前后的含量对比分析。含量对比分析结果表明,制首乌与不同药物配伍后,12个成分的含量均发生了不同程度的变化,且与墨旱莲配伍后制首乌中有33%的成分含量显著降低(P<0.05)、42%的成分含量显著升高外(P<0.05),与另8味药配伍后制首乌中至少50%的成分含量显著降低(P<0.05)。DPPH自由基清除能力实验结果显示,制首乌DPPH自由基清除能力高于其他9味中药,配伍后9个制首乌药对的DPPH自由基清除能力低于制首乌,但高于相应的配伍药物。量-效回归正交偏最小二乘法(orthogonal projections to latentstructures,OPLS)模型中R2X、R2Y及Q2值分别为0.841、0.981及0.962,筛选出4个量-效关系化学标志物,分别为反式-2,3,5,4′-四羟基二苯乙烯-2-O-β-D-吡喃葡萄糖苷(trans-THSG)、大黄素甲醚、顺式-2,3,5,4′-四羟基二苯乙烯-2-O-β-D-吡喃葡萄糖苷(cis-THSG)、大黄素-8-O-β-D-吡喃葡萄糖苷(EG)。结论建立的多成分半定量分析方法可用于何首乌在药对配伍过程中多成分含量变化的对比分析,trans-THSG、大黄素甲醚、cis-THSG、EG是影响制首乌在上述药对中发挥DPPH�展开更多
The novel well-defined chiral bicyclic thioureas based on enantiopure unsymmetric cis-2,5-disustituted pyrrolidine skeleton were firstly synthesized and fully characterized by their 1H NMR, 13C NMR and HRMS. Their abs...The novel well-defined chiral bicyclic thioureas based on enantiopure unsymmetric cis-2,5-disustituted pyrrolidine skeleton were firstly synthesized and fully characterized by their 1H NMR, 13C NMR and HRMS. Their absolute configurations were also determined by single-crystal X-ray analysis.展开更多
Objective To evaluate the synergy of the Burkholderia signaling molecule cis-2-dodecenoic acid(BDSF) and fluconazole(FLU) or itraconazole(ITRA) against two azole-resistant C. albicans clinical isolates in vitro and in...Objective To evaluate the synergy of the Burkholderia signaling molecule cis-2-dodecenoic acid(BDSF) and fluconazole(FLU) or itraconazole(ITRA) against two azole-resistant C. albicans clinical isolates in vitro and in vivo. Methods Minimum inhibitory concentrations(MICs) of antibiotics against two azole-resistant C. albicans were measured by the checkerboard technique, E-test, and time-kill assay. In vivo antifungal synergy testing was performed on mice. Analysis of the relative gene expression levels of the strains was conducted by quantitative reverse-transcription polymerase chain reaction(qR T-PCR). Results BDSF showed highly synergistic effects in combination with FLU or ITRA with a fractional inhibitory concentration index of ≤ 0.08. BDSF was not cytotoxic to normal human foreskin fibroblast cells at concentrations of up to 300 μg/mL. The qR T-PCR results showed that the combination of BDSF and FLU/ITRA significantly inhibits the expression of the efflux pump genes CDR1 and MDR1 via suppression of the transcription factors TAC1 and MRR1, respectively, when compared with FLU or ITRA alone. No dramatic difference in the mR NA expression levels of ERG1, ERG11, and UPC2 was found, which indicates that the drug combinations do not significantly interfere with UPC2-mediated ergosterol levels. In vivo experiments revealed that combination therapy can be an effective therapeutic approach to treat candidiasis. Conclusion The synergistic effects of BDSF and azoles may be useful as an alternative approach to control azole-resistant Candida infections.展开更多
文摘目的对比研究顺式和反式二苯乙烯苷的降血脂作用。方法分别考察顺式、反式二苯乙烯苷对正常小鼠、慢性高血脂小鼠和急性高血脂小鼠血清中总胆固醇(total cholesterol,TC)、甘油三酯(triglyceride,TG)、高密度脂蛋白胆固醇(high density lipoprotein cholesterol,HDL-C)和低密度脂蛋白胆固醇(low density lipoprotein cholesterol,LDL-C)含量的影响。结果顺式二苯乙烯苷能显著性降低高血脂小鼠血清中TC、TG及LDL-C的水平,也能显著性降低正常血脂小鼠血清中LDL-C的含量,高剂量顺式二苯乙烯苷还能显著性升高正常血脂小鼠和高血脂小鼠血清中HDL-C的水平。顺式二苯乙烯苷对正常小鼠和急性高血脂小鼠的降血脂作用与反式基本相同,但对慢性高血脂小鼠血浆中TC和TG的降低作用明显强于反式二苯乙烯苷。结论顺式二苯乙烯苷具有比反式二苯乙烯苷更好的降血脂作用。
文摘目的采用半定量分析方法对制首乌与9个补虚药配伍后成分含量及DPPH自由基清除能力变化进行研究。方法以UPLC-DAD建立制首乌多成分半定量分析方法,对制首乌与9味常用补虚药(当归、熟地黄、白芍、党参、黄芪、甘草、麦冬、枸杞子、墨旱莲)配伍后成分含量变化进行分析。采用DPPH法分别测定单味药以及配伍药对的自由基清除能力,绘制量-效曲线并计算半数清除浓度(EC50)。采用多元统计分析方法建立制首乌中多成分含量与DPPH自由基清除能力间的量-效回归模型,筛选量-效关系中影响显著的化学标志物,并通过质谱进行定性分析。结果线性范围、准确度、精密度、重复性及稳定性5项方法学验证结果表明,半定量分析方法可用于制首乌中12个成分在配伍前后的含量对比分析。含量对比分析结果表明,制首乌与不同药物配伍后,12个成分的含量均发生了不同程度的变化,且与墨旱莲配伍后制首乌中有33%的成分含量显著降低(P<0.05)、42%的成分含量显著升高外(P<0.05),与另8味药配伍后制首乌中至少50%的成分含量显著降低(P<0.05)。DPPH自由基清除能力实验结果显示,制首乌DPPH自由基清除能力高于其他9味中药,配伍后9个制首乌药对的DPPH自由基清除能力低于制首乌,但高于相应的配伍药物。量-效回归正交偏最小二乘法(orthogonal projections to latentstructures,OPLS)模型中R2X、R2Y及Q2值分别为0.841、0.981及0.962,筛选出4个量-效关系化学标志物,分别为反式-2,3,5,4′-四羟基二苯乙烯-2-O-β-D-吡喃葡萄糖苷(trans-THSG)、大黄素甲醚、顺式-2,3,5,4′-四羟基二苯乙烯-2-O-β-D-吡喃葡萄糖苷(cis-THSG)、大黄素-8-O-β-D-吡喃葡萄糖苷(EG)。结论建立的多成分半定量分析方法可用于何首乌在药对配伍过程中多成分含量变化的对比分析,trans-THSG、大黄素甲醚、cis-THSG、EG是影响制首乌在上述药对中发挥DPPH�
文摘The novel well-defined chiral bicyclic thioureas based on enantiopure unsymmetric cis-2,5-disustituted pyrrolidine skeleton were firstly synthesized and fully characterized by their 1H NMR, 13C NMR and HRMS. Their absolute configurations were also determined by single-crystal X-ray analysis.
基金financially supported by the National Natural Science Foundation of China [81273409]the Program for Changjiang Scholars and Innovative Research Team in University [IRT_15R37]the Ministry of Science and Technology of China [2017YFA0205301]
文摘Objective To evaluate the synergy of the Burkholderia signaling molecule cis-2-dodecenoic acid(BDSF) and fluconazole(FLU) or itraconazole(ITRA) against two azole-resistant C. albicans clinical isolates in vitro and in vivo. Methods Minimum inhibitory concentrations(MICs) of antibiotics against two azole-resistant C. albicans were measured by the checkerboard technique, E-test, and time-kill assay. In vivo antifungal synergy testing was performed on mice. Analysis of the relative gene expression levels of the strains was conducted by quantitative reverse-transcription polymerase chain reaction(qR T-PCR). Results BDSF showed highly synergistic effects in combination with FLU or ITRA with a fractional inhibitory concentration index of ≤ 0.08. BDSF was not cytotoxic to normal human foreskin fibroblast cells at concentrations of up to 300 μg/mL. The qR T-PCR results showed that the combination of BDSF and FLU/ITRA significantly inhibits the expression of the efflux pump genes CDR1 and MDR1 via suppression of the transcription factors TAC1 and MRR1, respectively, when compared with FLU or ITRA alone. No dramatic difference in the mR NA expression levels of ERG1, ERG11, and UPC2 was found, which indicates that the drug combinations do not significantly interfere with UPC2-mediated ergosterol levels. In vivo experiments revealed that combination therapy can be an effective therapeutic approach to treat candidiasis. Conclusion The synergistic effects of BDSF and azoles may be useful as an alternative approach to control azole-resistant Candida infections.
