目的观察扶正解毒化瘀方总苷提取物对呼吸道合胞病毒(RSV)感染HEp-2细胞Toll样受体(TLRs)相关细胞炎性因子的影响,探讨其可能的作用机制。方法建立RSV感染HEp-2细胞模型,随机分为病毒对照组、总苷提取物组及利巴韦林组,各给药组给予相...目的观察扶正解毒化瘀方总苷提取物对呼吸道合胞病毒(RSV)感染HEp-2细胞Toll样受体(TLRs)相关细胞炎性因子的影响,探讨其可能的作用机制。方法建立RSV感染HEp-2细胞模型,随机分为病毒对照组、总苷提取物组及利巴韦林组,各给药组给予相应药物,同时以未感染RSV的HEp-2细胞作为空白对照。应用液相色谱-质谱分析扶正解毒化瘀方全方、总苷提取物及其药物血清的主要成分。采用ELISA检测细胞上清液白细胞介素(IL)-1β、IL-8、干扰素-α(IFN-α)、TLR3、TLR7水平。结果扶正解毒化瘀方全方提取物共鉴别出10个化学成分,以苷类为主。扶正解毒化瘀方总苷提取物共鉴别出9个化学成分,其中入血成分共鉴别出8个化学成分,包括芍药苷、木犀草素、野黄芩苷、连翘酯苷H、异荭草苷、连翘苷、人参皂苷Rb1、人参皂苷Re。与HEp-2细胞组比较,病毒对照组感染后24、48、72 h IFN-α、IL-1β、IL-8、TLR3和TLR7水平均升高;与病毒对照组比较,总苷提取物组感染后24、48、72 h IFN-α、IL-1β、IL-8、TLR3和TLR7水平均降低。结论扶正解毒化瘀方总苷提取物可能通过调节TLRs相关细胞炎性因子,抑制细胞炎性反应起到治疗RSV肺炎的作用。展开更多
As the carrier of water-insoluble drugs, microspheres can play a role in increasing solubility and delaying releasing essence. The objective of this study was to improve the solubility and to delay the release of a ne...As the carrier of water-insoluble drugs, microspheres can play a role in increasing solubility and delaying releasing essence. The objective of this study was to improve the solubility and to delay the release of a newly discovered antitumor compound 3β-hydroxyolea-12-en-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester(T-OA). Early-stage preparation discovery concept(EPDC) was employed in the present study. The preparation, physicochemical characterization, and drug release properties of PLGA microspheres were evaluated. T-OA-loaded PLGA microspheres were prepared by an oil-in-water(O/W) emulsification solvent evaporation method. Characterization and release behaviors of the T-OA PLGA microspheres were evaluated by X-ray diffract(XRD), differential scanning calorimetry(DSC), Fourier transform infrared spectroscopy(FTIR), scanning electron microscopy(SEM), and high performance liquid chromatography(HPLC). The results demonstrated that T-OA-loaded PLGA microspheres could be successfully obtained through solvent evaporation method with appropriate morphologic characteristics and high encapsulation efficiency. The XRD analysis showed that T-OA would be either molecularly dispersed in the polymer or distributed in an amorphous form. The DSC and FTIR analysis proved that there were interactions between T-OA and PLGA polymer. SEM observations displayed the morphology of the microspheres was homogeneous and the majority of the spheres ranged between 50 and 150 μm. The drug release behavior of the microspheres in the phosphate buffered saline medium exhibited a sustained release and the duration of the release lasted for more than 23 days, which was fit with zero-order release pattern with r^2 = 0.994 7. In conclusion, TOA-loaded PLGA microspheres might hold great promise for using as a drug-delivery system in biomedical applications.展开更多
文摘目的观察扶正解毒化瘀方总苷提取物对呼吸道合胞病毒(RSV)感染HEp-2细胞Toll样受体(TLRs)相关细胞炎性因子的影响,探讨其可能的作用机制。方法建立RSV感染HEp-2细胞模型,随机分为病毒对照组、总苷提取物组及利巴韦林组,各给药组给予相应药物,同时以未感染RSV的HEp-2细胞作为空白对照。应用液相色谱-质谱分析扶正解毒化瘀方全方、总苷提取物及其药物血清的主要成分。采用ELISA检测细胞上清液白细胞介素(IL)-1β、IL-8、干扰素-α(IFN-α)、TLR3、TLR7水平。结果扶正解毒化瘀方全方提取物共鉴别出10个化学成分,以苷类为主。扶正解毒化瘀方总苷提取物共鉴别出9个化学成分,其中入血成分共鉴别出8个化学成分,包括芍药苷、木犀草素、野黄芩苷、连翘酯苷H、异荭草苷、连翘苷、人参皂苷Rb1、人参皂苷Re。与HEp-2细胞组比较,病毒对照组感染后24、48、72 h IFN-α、IL-1β、IL-8、TLR3和TLR7水平均升高;与病毒对照组比较,总苷提取物组感染后24、48、72 h IFN-α、IL-1β、IL-8、TLR3和TLR7水平均降低。结论扶正解毒化瘀方总苷提取物可能通过调节TLRs相关细胞炎性因子,抑制细胞炎性反应起到治疗RSV肺炎的作用。
基金supported by the Innovation Team of Beijing University of Chinese Medicine(No.2011-CXTD-13)the Collaborative Innovation Construction Plan of Beijing University of Chinese Medicine(No.2013-XTCX-03)
文摘As the carrier of water-insoluble drugs, microspheres can play a role in increasing solubility and delaying releasing essence. The objective of this study was to improve the solubility and to delay the release of a newly discovered antitumor compound 3β-hydroxyolea-12-en-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester(T-OA). Early-stage preparation discovery concept(EPDC) was employed in the present study. The preparation, physicochemical characterization, and drug release properties of PLGA microspheres were evaluated. T-OA-loaded PLGA microspheres were prepared by an oil-in-water(O/W) emulsification solvent evaporation method. Characterization and release behaviors of the T-OA PLGA microspheres were evaluated by X-ray diffract(XRD), differential scanning calorimetry(DSC), Fourier transform infrared spectroscopy(FTIR), scanning electron microscopy(SEM), and high performance liquid chromatography(HPLC). The results demonstrated that T-OA-loaded PLGA microspheres could be successfully obtained through solvent evaporation method with appropriate morphologic characteristics and high encapsulation efficiency. The XRD analysis showed that T-OA would be either molecularly dispersed in the polymer or distributed in an amorphous form. The DSC and FTIR analysis proved that there were interactions between T-OA and PLGA polymer. SEM observations displayed the morphology of the microspheres was homogeneous and the majority of the spheres ranged between 50 and 150 μm. The drug release behavior of the microspheres in the phosphate buffered saline medium exhibited a sustained release and the duration of the release lasted for more than 23 days, which was fit with zero-order release pattern with r^2 = 0.994 7. In conclusion, TOA-loaded PLGA microspheres might hold great promise for using as a drug-delivery system in biomedical applications.
