目的探讨Embelin对甲状腺癌细胞增殖的影响并探讨相关机制。方法体外培养甲状腺癌细胞,经Embelin处理后,RT-PCR和Western印迹检测XIAP m RNA和蛋白的表达水平;MTT法测定细胞生长抑制率;流式细胞仪测定细胞凋亡率和细胞周期;免疫印迹检测...目的探讨Embelin对甲状腺癌细胞增殖的影响并探讨相关机制。方法体外培养甲状腺癌细胞,经Embelin处理后,RT-PCR和Western印迹检测XIAP m RNA和蛋白的表达水平;MTT法测定细胞生长抑制率;流式细胞仪测定细胞凋亡率和细胞周期;免疫印迹检测PI3K、Akt蛋白表达水平。结果 Embelin处理甲状腺癌细胞48 h后,XIAP m RNA和蛋白表达水平明显降低。在高剂量组中,MTT法检测其细胞生长抑制率为42.78%±4.29%,明显高于对照组(t=20.14,P<0.01);流式细胞仪检测高剂量组细胞凋亡率为37.94%±2.29%,明显高于对照组(t=42.09,P<0.01);流式细胞仪检测高剂量组细胞周期,发现其处于G1期细胞的百分比为68.23%±2.13%,明显高于对照组(t高剂量组=5.70,P<0.01);检测PI3K、Akt蛋白在高剂量组中的表达水平,发现p Akt蛋白表达水平明显低于对照组(t高剂量组=6.47,P<0.05)。结论 Embelin下调XIAP表达可抑制甲状腺癌细胞增殖,其作用机制可能与PI3K/Akt信号途径相关。展开更多
CThe objective of the present study was to prepare solid self-nanoemulsifying drug delivery system(S-SNEDDS)containing Capryol-90 as oil phase for the delivery of Embelin,a poorly water soluble herbal active ingredien...CThe objective of the present study was to prepare solid self-nanoemulsifying drug delivery system(S-SNEDDS)containing Capryol-90 as oil phase for the delivery of Embelin,a poorly water soluble herbal active ingredient.Box-Behnken experimental design was employed to optimise the formulation variables,X1(amount of oil;Capryol 90),X2(amount of surfactant;Acrysol EL 135)and X3(amount of co-surfactant;PEG 400).Systems were appraised for visual characteristics for self emulsifying time,globule size and drug release.Optimised liquid formulations were formulated into free flowing granules(S-SNEDDS)by adsorption on the porous materials like Aerosil 200 and Neusilin and thereby compressed into tablet.In vitro dissolution studies of SNEDDS revealed increased in the dissolution rate of the drug.FT-IR data revealed no physicochemical interaction between drug and excipients.Solid state characterization of S-SNEDDS by DSC and Powder XRD confirmed reduction in drug crystallinity which further supports the results of dissolution studies.TEM analysis exhibited spherical globules.Further,the accelerated stability studies for 6 months revealed that S-SNEDDS of Embelin are found to be stable without any significant change in physicochemical properties.Thus,the present studies demonstrated dissolution enhancement potential of porous carrier based S-SNEDDS for poorly water soluble herbal active ingredient,Embelin.展开更多
文摘目的探讨Embelin对甲状腺癌细胞增殖的影响并探讨相关机制。方法体外培养甲状腺癌细胞,经Embelin处理后,RT-PCR和Western印迹检测XIAP m RNA和蛋白的表达水平;MTT法测定细胞生长抑制率;流式细胞仪测定细胞凋亡率和细胞周期;免疫印迹检测PI3K、Akt蛋白表达水平。结果 Embelin处理甲状腺癌细胞48 h后,XIAP m RNA和蛋白表达水平明显降低。在高剂量组中,MTT法检测其细胞生长抑制率为42.78%±4.29%,明显高于对照组(t=20.14,P<0.01);流式细胞仪检测高剂量组细胞凋亡率为37.94%±2.29%,明显高于对照组(t=42.09,P<0.01);流式细胞仪检测高剂量组细胞周期,发现其处于G1期细胞的百分比为68.23%±2.13%,明显高于对照组(t高剂量组=5.70,P<0.01);检测PI3K、Akt蛋白在高剂量组中的表达水平,发现p Akt蛋白表达水平明显低于对照组(t高剂量组=6.47,P<0.05)。结论 Embelin下调XIAP表达可抑制甲状腺癌细胞增殖,其作用机制可能与PI3K/Akt信号途径相关。
文摘CThe objective of the present study was to prepare solid self-nanoemulsifying drug delivery system(S-SNEDDS)containing Capryol-90 as oil phase for the delivery of Embelin,a poorly water soluble herbal active ingredient.Box-Behnken experimental design was employed to optimise the formulation variables,X1(amount of oil;Capryol 90),X2(amount of surfactant;Acrysol EL 135)and X3(amount of co-surfactant;PEG 400).Systems were appraised for visual characteristics for self emulsifying time,globule size and drug release.Optimised liquid formulations were formulated into free flowing granules(S-SNEDDS)by adsorption on the porous materials like Aerosil 200 and Neusilin and thereby compressed into tablet.In vitro dissolution studies of SNEDDS revealed increased in the dissolution rate of the drug.FT-IR data revealed no physicochemical interaction between drug and excipients.Solid state characterization of S-SNEDDS by DSC and Powder XRD confirmed reduction in drug crystallinity which further supports the results of dissolution studies.TEM analysis exhibited spherical globules.Further,the accelerated stability studies for 6 months revealed that S-SNEDDS of Embelin are found to be stable without any significant change in physicochemical properties.Thus,the present studies demonstrated dissolution enhancement potential of porous carrier based S-SNEDDS for poorly water soluble herbal active ingredient,Embelin.