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为解决虫草素在体内被腺苷脱氢酶(ADA)快速降解的问题,制备虫草素/LDH复合物,研究其在体内外对虫草素的缓释以及对HeLa细胞的生长抑制作用.结果表明:当虫草素/LDH复合物中虫草素质量浓度为30,60,90μg·mL-1时,复合物对HeLa细胞的生长抑制率分别为52.4%、61.3%、79.6%,与虫草素对照组比较,P<0.01.显微镜观察发现,当虫草素质量浓度60μg·mL-1时,虫草素/LDH复合物使大部分HeLa细胞死亡;虫草素的对照组HeLa细胞死亡较少,但细胞内部明显出现空泡.虫草素/LDH复合物体外释放表明,虫草素插入LDH双层结构之后,使虫草素释放速度明显被降低.对SD大鼠腹腔给药后,虫草素/LDH复合物血药最高质量浓度为82.1μg·mL-1,在药后1.5h出现,虫草素对照组的血药最高质量浓度为75.3μg·mL-1,在给药后1h出现.
In order to solve the problem that cordycepin is rapidly degraded by adenosine dehydrogenase (ADA) in vivo, the cordycepin / LDH complex was prepared and its sustained release in vitro and in vivo as well as its inhibitory effect on the growth of HeLa cells were studied. : When the concentration of cordycepin in cordycepin / LDH complex was 30, 60 and 90μg · mL-1, the inhibitory rates of complex on HeLa cells were 52.4%, 61.3% and 79.6%, respectively, Compared with the control group, P <0.01.Microscope observation showed that cordycepin / LDH complex caused most of the HeLa cells to die when the concentration of cordycepin was 60 μg · mL-1, while that of the control group of cordycepin was less, The vacuolization of the cordycepin / LDH complex in vitro showed that the release of cordycepin was significantly reduced after the insertion of cordycepin into the double-layered structure of LDH.After intraperitoneal administration of cordycepin / LDH complex, the highest plasma level of cordycepin / LDH complex The highest concentration of blood was 75.3μg · mL-1 in the control group of cordycepin, which appeared at 1h after administration.