中国生化药物杂志
中國生化藥物雜誌
중국생화약물잡지
CHINESE JOURNAL OF BIOCHEMICAL PHARMACEUTICS
2014年
4期
12-14,18
,共4页
多肽修饰%紫杉醇%脂质体%CD133%肿瘤干细胞
多肽脩飾%紫杉醇%脂質體%CD133%腫瘤榦細胞
다태수식%자삼순%지질체%CD133%종류간세포
peptide modified%paclitaxel%liposomes%CD133%neoplastic stem cells
目的：制备与肺癌干细胞标志物CD133具有高度亲和力的多肽修饰载紫杉醇脂质体（CD133 specific-binding peptide conjugated paclitaxel loaded liposome，TLP-PTX），考察TLP-PTX与A549肺癌干细胞的结合能力及其对A549肺癌干细胞和肺癌干细胞移植瘤的抑制作用。方法采用薄膜分散法制备TLP-PTX，观察其粒径，电位及紫杉醇的包封率等理化性质。采用细胞摄取实验和肿瘤球穿透实验考察TLP-PTX与A549肺癌干细胞的亲和力。通过MTT实验和肺癌干细胞肿瘤球抑制实验观察TLP-PTX对肺癌干细胞的抑制效果。结果制备得到的TLP-PTX粒径为（115.8±8.3）nm，紫杉醇的包封率为88.5％。经过CD133特异性多肽修饰后能够明显增强肺癌干细胞和肿瘤球对脂质体的摄取能力，A549肺癌干细胞对TLP的摄取效率是LP的2.6倍，差异有统计学意义（P＜0.05）。MTT实验结果表明TLP-PTX对A549肺癌干细胞的毒性显著强于LP-PTX和紫杉醇溶液（P＜0.05）；A549肺癌干细胞肿瘤球抑制实验表明TLP-PTX具有良好的抗肿瘤效果。结论 TLP-PTX能够特异识别A549肺癌干细胞表面的CD133，介导脂质体进入细胞，抑制肺癌干细胞增殖。TLP-PTX是一种有效的A549肺癌干细胞靶向给药系统。
目的：製備與肺癌榦細胞標誌物CD133具有高度親和力的多肽脩飾載紫杉醇脂質體（CD133 specific-binding peptide conjugated paclitaxel loaded liposome，TLP-PTX），攷察TLP-PTX與A549肺癌榦細胞的結閤能力及其對A549肺癌榦細胞和肺癌榦細胞移植瘤的抑製作用。方法採用薄膜分散法製備TLP-PTX，觀察其粒徑，電位及紫杉醇的包封率等理化性質。採用細胞攝取實驗和腫瘤毬穿透實驗攷察TLP-PTX與A549肺癌榦細胞的親和力。通過MTT實驗和肺癌榦細胞腫瘤毬抑製實驗觀察TLP-PTX對肺癌榦細胞的抑製效果。結果製備得到的TLP-PTX粒徑為（115.8±8.3）nm，紫杉醇的包封率為88.5％。經過CD133特異性多肽脩飾後能夠明顯增彊肺癌榦細胞和腫瘤毬對脂質體的攝取能力，A549肺癌榦細胞對TLP的攝取效率是LP的2.6倍，差異有統計學意義（P＜0.05）。MTT實驗結果錶明TLP-PTX對A549肺癌榦細胞的毒性顯著彊于LP-PTX和紫杉醇溶液（P＜0.05）；A549肺癌榦細胞腫瘤毬抑製實驗錶明TLP-PTX具有良好的抗腫瘤效果。結論 TLP-PTX能夠特異識彆A549肺癌榦細胞錶麵的CD133，介導脂質體進入細胞，抑製肺癌榦細胞增殖。TLP-PTX是一種有效的A549肺癌榦細胞靶嚮給藥繫統。
목적：제비여폐암간세포표지물CD133구유고도친화력적다태수식재자삼순지질체（CD133 specific-binding peptide conjugated paclitaxel loaded liposome，TLP-PTX），고찰TLP-PTX여A549폐암간세포적결합능력급기대A549폐암간세포화폐암간세포이식류적억제작용。방법채용박막분산법제비TLP-PTX，관찰기립경，전위급자삼순적포봉솔등이화성질。채용세포섭취실험화종류구천투실험고찰TLP-PTX여A549폐암간세포적친화력。통과MTT실험화폐암간세포종류구억제실험관찰TLP-PTX대폐암간세포적억제효과。결과제비득도적TLP-PTX립경위（115.8±8.3）nm，자삼순적포봉솔위88.5％。경과CD133특이성다태수식후능구명현증강폐암간세포화종류구대지질체적섭취능력，A549폐암간세포대TLP적섭취효솔시LP적2.6배，차이유통계학의의（P＜0.05）。MTT실험결과표명TLP-PTX대A549폐암간세포적독성현저강우LP-PTX화자삼순용액（P＜0.05）；A549폐암간세포종류구억제실험표명TLP-PTX구유량호적항종류효과。결론 TLP-PTX능구특이식별A549폐암간세포표면적CD133，개도지질체진입세포，억제폐암간세포증식。TLP-PTX시일충유효적A549폐암간세포파향급약계통。
Objective To prepare CD133 specific-binding peptide conjugated liposome loaded paclitaxel and evaluate the efficiency of cellular uptake and the ability of inhibiting A549 lung cancer stem cell.Methods Liposomes were prepared by film-ultrasonic method.The partical size,zeta-potential and entrapment efficiency of liposomes were evaluated.Cellular uptake effciency of A549 lung cancer stem cell for liposomes were explored.The anti-proliferation efficiency of TLP-PTX to A549 lung cancer stem cell was evaluated by MTT assay.Tumor spheroids were used to evaluate anti-tumor ability of TLP-PTX to A549 lung cancer stem cell. Results The particle diameter of TLP-PTX was (115.8 ±8.3)nm and the entrapment efficiency of PTX was 88.5%.CD133 specific-binding peptide could enhance the efficiency of cellar uptake.The uptaken efficiency of TLP by A549 lung cancer stem cell were 2.6 times higher than that of LP(P<0.05 ).The MTT Results showed that the toxicity of TLP-PTX on A549 lung cancer stem cell was significantly stronger than LP-PTX and paclitaxel solution(P<0.05 ).The tumor inhibition test results showed that TLP-PTX has good anti-tumor effect. Conclusion TLP-PTX can specifically recognize the surface marker CD133 of A549 lung cancer stem cell,facilitate liposomes into cells and inhibit A549 lung cancer stem cell proliferation.TLP-PTX is an effective drug delivery system targeting to A549 lung cancer stem cell.
