Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil.
Division of Biomaterials and Biomechanics, Department of Restorative Dentistry, School of Dentistry, Oregon Health and Science University, Portland, OR, United States.
Food Chem Toxicol. 2019 Mar;125:198-209. doi: 10.1016/j.fct.2019.01.003. Epub 2019 Jan 4.
Carvacrol, a phenolic monoterpene derived from thyme oil has gained wide interest recently because of its anticancer activities. To improve the solubility of carvacrol, the formation of inclusion complexes with β-cyclodextrin was performed by ultrasound and freeze-drying methods and characterized using thermal analysis, FTIR, XRD, SEM, NMR and HPLC analysis. From these results, carvacrol was successfully complexed within β-cyclodextrin cavity. Moreover, HPLC analysis demonstrated a higher entrapment efficiency for freeze-drying method (81.20 ± 0.52%) in contrast to ultrasound method (34.02 ± 0.67%). Hence, freeze-drying inclusion complex was evaluated for its antiproliferative effect and cytotoxicity against prostate cancer cell line (PC3) in vitro. Further, freeze-drying complex led to a dose-dependent inhibition in tumor cell growth in 2D and 3D cell culture systems. Altogether, the inclusion of carvacrol in β-cyclodextrin led to the formation of stable complexes with potent antiproliferative effects against PC3 cells, in vitro. Such an improved cytotoxic effect can be attributed to the enhanced the aqueous solubility and bioavailability of carvacrol by effective complexation in β-cyclodextrin.
香芹酚是一种从百里香油中提取的酚类单萜,由于其抗癌活性而受到广泛关注。为了提高香芹酚的溶解度,采用超声和冷冻干燥法将其与β-环糊精形成包合物,并通过热分析、FTIR、XRD、SEM、NMR 和 HPLC 分析进行了表征。结果表明,香芹酚成功地被包合在β-环糊精空腔内。此外,HPLC 分析表明,与超声法(34.02 ± 0.67%)相比,冷冻干燥法的包封效率更高(81.20 ± 0.52%)。因此,对其进行了体外抗前列腺癌细胞系(PC3)增殖作用和细胞毒性评价。进一步的研究表明,在 2D 和 3D 细胞培养系统中,冷冻干燥复合物可导致肿瘤细胞生长呈剂量依赖性抑制。总之,香芹酚在β-环糊精中的包合作用形成了对 PC3 细胞具有强大增殖抑制作用的稳定复合物,体外实验。这种增强的细胞毒性作用可以归因于通过β-环糊精的有效包合作用提高了香芹酚的水溶解度和生物利用度。