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目的:观察活性炭纳米粒子(activated carbonna noparticles,ACNP)吸附5-Fu在体内外对5-Fu肿瘤作用的影响,探讨ACNP的作用机制。方法:用紫外分光光度法检测ACNP对5-Fu的吸附性能;分别采用MTT实验和S180小鼠、H22小鼠动物肿瘤模型观察了ACNP在体外和体内对5-Fu抗肿瘤作用的影响;采用流式细胞术测定ACNP对细胞周期的影响;采用甲基绿-派洛宁染色法观察ACNP对细胞凋亡的影响。结果:ACNP在常温下对5-Fu有良好的吸附性能,符合经验公式M=0.295C1.919;ACNP吸附5-Fu后对BGC-823的抑制生长作用显著高于相等浓度的5-Fu组,有良好的量效及时效关系;ACNP吸附5-Fu后对S180小鼠的抑瘤率及对H22小鼠的生命延长率均显著高于含药量相等的5-Fu组;ACNP可以将BGC-823细胞阻滞在S期、与5-Fu合用可以诱导BGC-823的早期凋亡。结论:ACNP吸附5-Fu具有显著的体内外抗肿瘤活性,与5-Fu合用诱导细胞早期凋亡,将细胞周期阻滞在S期,ACNP的载体效应可能是增强5-Fu药理学作用的机制之一。
Objective: To investigate the effect of activated carbon nano-particles (ACNP) adsorbing 5-Fu on 5-Fu tumor in vitro and in vivo, and to explore the mechanism of action of ACNP. Methods: The adsorption of 5-Fu by ACNP was detected by ultraviolet spectrophotometry. The antitumor effects of ACNP on 5-Fu were observed by MTT assay, S180 mouse and H22 mouse model respectively. The effect of ACNP on cell cycle was analyzed by flow cytometry. The effect of ACNP on cell apoptosis was observed by Methyl Green-Peyerine staining. Results: ACNP possessed good adsorption properties to 5-Fu at room temperature, which accorded with empirical formula M = 0.295C1.919. The inhibitory effect of ACNP on 5-Fu after adsorbing 5-Fu was significantly higher than that of 5-Fu , With good dose-effect and time-dependent relationship. The antitumor rate of S180 mice after 5-Fu adsorption of ACNP and the life extension rate of H22 mice were significantly higher than that of 5-Fu group with the same dosage of ACNP. BGC-823 cells arrested in the S phase, combined with 5-Fu can induce early apoptosis of BGC-823. CONCLUSION: ACNP adsorbed 5-Fu has significant antitumor activity in vitro and in vivo. Combined with 5-Fu, it induces early apoptosis of cells and blocks the cell cycle in S phase. The carrier effect of ACNP may be to enhance the pharmacological effects of 5-Fu One of the mechanisms.