Antitumor Effects of Curcumin and Glycyrrhetinic Acid-Modified Curcumin-Loaded Cationic Liposome by Intratumoral Administration
Antitumor Effects of Curcumin and Glycyrrhetinic Acid-Modified Curcumin-Loaded Cationic Liposome by Intratumoral Administration
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DOI：
10.1155/2020/4504936
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发表时间：
2020-05-30
影响因子：
--
通讯作者：
Li, Hanmin
中科院分区：
文献类型：
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作者：
Chang, Mingxiang;Wu, Meimei;Li, Hanmin
姜黄素是从姜黄根茎中提取的一种疏水性多酚类化合物，具有一系列活性生物学功能，但由于其溶解度低、生物利用度低、代谢速度快，其应用一直受到限制和质疑。在抗肿瘤作用方面，这些缺点可以通过瘤内注射来克服。在这项研究中，我们提出了姜黄素和甘草次酸修饰的姜黄素阳离子脂质体(GAMCLCL)瘤内注射的H22荷瘤小鼠。实验结果表明，姜黄素在体外和体内均具有较强的抗肿瘤活性，但其抗肿瘤活性明显弱于GAMCLCL和阿霉素。与游离姜黄素相比，GAMCLCL在改善血液参数(WBC、RBC、PLT、ALT、CRE、LDH)，抑制肿瘤生长，降低肿瘤微血管密度，下调H22肿瘤组织中血管内皮生长因子-3蛋白和信使核糖核酸的表达，上调半胱氨酸天冬氨酸氨基转移酶-3的蛋白和信使核糖核酸的表达方面明显优于游离姜黄素。在本实验条件下，高剂量GAMCLCL的抗肿瘤作用与阿霉素相似。综上所述，实验结果表明，游离姜黄素具有一定的抗肿瘤作用，但其抗肿瘤活性较弱，应采取一些策略来克服其缺点，提高其临床疗效。
Curcumin is a hydrophobic polyphenolic compound extracted from the rhizome of Curcuma longa and shows a line of active biological functions, but its application has been limited and questioned because of its low solubility, low bioavailability, and rapid metabolism. In terms of antitumor effect, these disadvantages can be overcome by intratumoral injection. In this study, we present the intratumoral injection of curcumin and glycyrrhetinic acid-modified curcumin-loaded cationic liposome (GAMCLCL) in H22 tumor-bearing mice. The experimental results demonstrated that curcumin exhibited positive antitumor activities in vitro and in vivo by intratumoral injection, but its activities were much weaker than GAMCLCL and adriamycin. Compared with free curcumin, GAMCLCL showed much better effects in improving the blood parameters (WBC, RBC, PLT, ALT, CRE, and LDH), inhibiting tumor growth, reducing tumor microvascular density, downregulating the expression of VEGF-protein and mRNA, and upregulating the expression of caspase-3 protein and mRNA in H22 tumor tissues. Under the experimental conditions of this study, the antitumor effect of high-dose GAMCLCL was similar to adriamycin. In conclusion, the experimental results demonstrated that free curcumin possessed definite antitumor efficacy, but its antitumor activities were weaker, and some strategies should be adopted to overcome its disadvantages, improve, and ensure its clinical efficacy.