羟丙基-β-环糊精包合厚朴酚的抗癌活性评价。
Evaluation of anticancer activity of honokiol by complexation with hydroxypropyl-β-cyclodextrin.
机构信息
Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, Department of Biomedical Engineering, Jinan University, Guangzhou, 510632, China.
Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, Department of Biomedical Engineering, Jinan University, Guangzhou, 510632, China; Institute of Life and Health Engineering, Key Laboratory of Functional Protein Research of Guangdong Higher Education Institutes, Jinan University, Guangzhou, 510632, China; The First Affiliated Hospital of Jinan University, Guangzhou, 510632, China.
出版信息
Colloids Surf B Biointerfaces. 2020 Dec;196:111298. doi: 10.1016/j.colsurfb.2020.111298. Epub 2020 Jul 31.
Honokiol (HK), an active compound derived from Magnolia officinalis Rehd. et Wils, possesses many beneficial biological activities for human beings. However, its poor solubility and low bioavailability severely limits its application. In this way, to improve the pharmaceutical properties, the HK was complexed in hydroxypropyl-β-cyclodextrin (HP-β-CD) and its oral bioavailability and antitumor effects were evaluated. The HK/HP-β-CD inclusion complex (1:1) was prepared by saturated aqueous solution method. The inclusion complex (HK-HP-β-CD) obtained had a higher solubility, about 1497 times that of the free HK. The dissolution rate and the oral bioavailability of HK was also significantly higher from inclusion complex than from free HK. Furthermore, the HK-HP-β-CD exhibited higher antitumor activity against Human Hepatoma Cell Line (HepG2) than free HK. More cells were arrested in the sub-G1 phase of the cell cycle and were induced to undergo late apoptosis when treated with the HK-HP-β-CD than when treated with free HK.
厚朴酚（HK）是从厚朴中提取的一种活性化合物，对人类具有许多有益的生物学活性。然而，其较差的溶解度和低生物利用度严重限制了它的应用。为了改善药物性质，将 HK 与羟丙基-β-环糊精（HP-β-CD）复合，并对其口服生物利用度和抗肿瘤作用进行了评价。采用饱和水溶液法制备 HK/HP-β-CD 包合物（1:1）。所得包合物（HK-HP-β-CD）的溶解度更高，约为游离 HK 的 1497 倍。与游离 HK 相比，包合物的溶解速率和口服生物利用度也显著提高。此外，与游离 HK 相比，HK-HP-β-CD 对人肝癌细胞系（HepG2）的抗肿瘤活性更高。用 HK-HP-β-CD 处理后，细胞周期的 sub-G1 期有更多的细胞被阻滞，并诱导晚期凋亡。
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