Department of Biochemistry, Faculty of Science, University of Dschang, P.O. Box 67, Dschang, Cameroon.
Department of Pharmaceutics and Biopharmaceutics, University of Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany.
Mediators Inflamm. 2022 Aug 30;2022:8886087. doi: 10.1155/2022/8886087. eCollection 2022.
Guttiferone E is a naturally occurring polyisoprenylated benzophenone exhibiting a wide range of remarkable biological activities. But its therapeutic application is still limited due to its poor water solubility. This study is aimed at preparing guttiferone E-loaded liposomes and assessing their cytotoxicity and anti-inflammatory effect.
Liposomes containing guttiferone E were prepared by the thin film hydration method, and the physicochemical characteristics were determined using dynamic light scattering, laser Doppler velocimetry, and atomic force microscopy. The cytotoxicity was assessed by the MTT assay. The fluorometric cyclooxygenase (COX) activity assay kit was used to assess the COX activity while the nitric oxide production was evaluated by the Griess reagent method.
The liposomes with a mean size of 183.33 ± 17.28 nm were obtained with an entrapment efficiency of 63.86%. Guttiferone E-loaded liposomes successfully decreased the viability of cancer cells. The overall IC values varied between 5.46 g/mL and 22.25 g/mL. Compared to the untreated control, guttiferone E-loaded liposomes significantly reduced the nitric oxide production and the activity of COX in a concentration-dependent manner.
This study indicates that liposomes can be an alternative to overcome the water insolubility issue of the bioactive guttiferone E.
吉非替尼 E 是一种天然存在的多异戊二烯基二苯甲酮，具有广泛的显著的生物学活性。但其治疗应用仍受到其水溶性差的限制。本研究旨在制备吉非替尼 E 载脂蛋白体，并评估其细胞毒性和抗炎作用。
采用薄膜水化法制备吉非替尼 E 载脂蛋白体，采用动态光散射、激光多普勒 velocimetry 和原子力显微镜测定其理化特性。采用 MTT 法评估细胞毒性。采用荧光环加氧酶（COX）活性测定试剂盒评估 COX 活性，采用格里试剂法评估一氧化氮产生。
得到平均粒径为 183.33±17.28nm 的载脂蛋白体，包封率为 63.86%。吉非替尼 E 载脂蛋白体成功降低了癌细胞的活力。总体 IC 值在 5.46g/ml 至 22.25g/ml 之间。与未处理的对照组相比，吉非替尼 E 载脂蛋白体以浓度依赖的方式显著降低了一氧化氮的产生和 COX 的活性。
本研究表明，载脂蛋白体可以作为克服生物活性吉非替尼 E 水溶性差的一种替代方法。
