Antitumor effect of a liposome-encapsulated beta1,4-galactosyltransferase inhibitor.
Antitumor effect of a liposome-encapsulated beta1,4-galactosyltransferase inhibitor.
复制标题
脂质体封装的 β1,4-半乳糖基转移酶抑制剂的抗肿瘤作用。
DOI：
10.1016/j.ijpharm.2018.10.010
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发表时间：
2018
影响因子：
5.8
通讯作者：
Gao Yin
中科院分区：
文献类型：
--
作者：
Cai Guangsheng;Wang Kun;Qu Na;Qiu Pengyu;Vlahakis Jason Z;Szarek Walter A;Lee Robert J;Gao Yin
Galactosyltransferases are a family of enzymes responsible for the synthesis of glycan chains which are involved in cell proliferation, adhesion and apoptosis. A recently synthesized galactosyltransferase inhibitor, 2-naphthyl 2-butanamido-2-deoxy-1-thio-β-D-glucopyranoside (612), has been found to selectively inhibit β1,4-galactosyltransferase over β1,3-galactosyltransferase and, therefore, has potential to suppress the synthesis of cancer associated epitopes. However, the application of this inhibitory activity in biological systems remains unknown. In this study,612was introduced into a cationic liposome (LP) delivery system, and the anti-proliferative effects of both free and the LP-incorporated612(612-LP) were investigated in A549 lung cancer cells, which actively express anionic sialic acid moieties on the surfaces of cells. The anti-proliferative effects were evaluated via MTT assays. The results revealed that free612and empty LP impose neither anti-proliferative nor apoptotic effects on cancer cells at low doses, whereas the 612-LP system inhibited cancer cell growth at a concentration as low as 0.1 μg/mL after 3 days of incubation, suggesting that this formulation enabled efficient delivery of612into cells and promoted the anti-proliferative activity of612against cancer cells. Therefore, this highly specific inhibitor612has the potential for development as an effective anti-cancer agent and merits further investigation.
