桦木酸与 γ-环糊精衍生物的复合物可降低非转移性和转移性 B164A5 细胞的增殖和体内肿瘤发展。

Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania.

Institute of Pharmaceutical Technology, University of Szeged, 6 Eotvos Ut., H-6720 Szeged, Hungary.

Int J Mol Sci. 2014 May 9;15(5):8235-55. doi: 10.3390/ijms15058235.

Betulinic acid, a very promising anti-melanoma agent, has very low water solubility that causes low bioavailability. To overcome this inconvenience, a highly water-soluble cyclodextrin was used (octakis-[6-deoxy-6-(2-sulfanyl ethanesulfonic acid)]-γ-cyclodextrin). The complex was physico-chemically analyzed using differential scanning calorimetry (DSC), X-ray and scanning electron microscopy (SEM) methods and then in vitro tested for its antiproliferative activity by the MTT assay and by cell cycle analysis. Finally, the complex was tested in vivo using an animal model of murine melanoma developed in C57BL/6J mice, where it caused a reduction in tumor volume and weight. The study revealed the beneficial influence of betulinic acid inclusion into the cyclodextrin in terms of antiproliferative activity and in vivo tumor development.

白桦脂酸是一种很有前途的抗黑色素瘤药物，但水溶性很低，生物利用度低。为了克服这一不便，使用了一种高水溶性的环糊精（八[6-脱氧-6-（2-巯基乙磺酸）]-γ-环糊精）。该配合物通过差示扫描量热法（DSC）、X 射线和扫描电子显微镜（SEM）等方法进行了物理化学分析，然后通过 MTT 测定法和细胞周期分析体外测试其增殖活性。最后，该配合物在 C57BL/6J 小鼠建立的小鼠黑色素瘤动物模型中进行了体内测试，结果表明其能降低肿瘤体积和重量。该研究表明，白桦脂酸包入环糊精中对增殖活性和体内肿瘤发展具有有益的影响。