Y E Bi1, Yulin Zhou1, Mengqiao Wang1, Lianlian Li1, Robert J Lee2,3,4, Jing Xie1, Lesheng Teng2,4. 1. Jilin University, College of Life Science, P. R. China. 2. Jilin University, College of Life Science, P. R. China lee.1339@osu.edu tenglesheng@jlu.edu.cn. 3. Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH, U.S.A. 4. Department of Chemistry, Zhuhai College of Jilin University, Zhuhai, P.R. China.
Abstract
BACKGROUND/AIM: Cordycepin is an endogenous nucleoside with significant anticancer biological activity. The objective of this study was to develop targeted liposomes to improve solubility and biological activity of cordycepin. MATERIALS AND METHODS: We established transferrin-conjugated liposomes to deliver cordycepin to liver cancer cells and evaluated the uptake and effect. RESULTS: The liposomes were loaded with cordycepin. Their average size was 125.3 nm, with drug encapsulation efficiency of 65.3%. The liposomes had good colloidal stability and released cordycepin slowly. Liposomal cordycepin was shown to increase reactive oxygen species production and cause depolarization of the mitochondrial transmembrane in liver cancer cells. Cellular uptake of liposomal cordycepin was enhanced by conjugation to transferrin, that facilitated receptor-mediated endocytosis. CONCLUSION: Transferrin-conjugated liposomes are effective as nanocarriers for cordycepin delivery to liver cancer cells. Copyright
BACKGROUND/AIM: Cordycepin is an endogenous nucleoside with significant anticancer biological activity. The objective of this study was to develop targeted liposomes to improve solubility and biological activity of cordycepin. MATERIALS AND METHODS: We established transferrin-conjugated liposomes to deliver cordycepin to liver cancer cells and evaluated the uptake and effect. RESULTS: The liposomes were loaded with cordycepin. Their average size was 125.3 nm, with drug encapsulation efficiency of 65.3%. The liposomes had good colloidal stability and released cordycepin slowly. Liposomal cordycepin was shown to increase reactive oxygen species production and cause depolarization of the mitochondrial transmembrane in liver cancer cells. Cellular uptake of liposomal cordycepin was enhanced by conjugation to transferrin, that facilitated receptor-mediated endocytosis. CONCLUSION:Transferrin-conjugated liposomes are effective as nanocarriers for cordycepin delivery to liver cancer cells. Copyright
Authors: Masar Radhi; Sadaf Ashraf; Steven Lawrence; Asta Arendt Tranholm; Peter Arthur David Wellham; Abdul Hafeez; Ammar Sabah Khamis; Robert Thomas; Daniel McWilliams; Cornelia Huiberdina de Moor Journal: Molecules Date: 2021-09-28 Impact factor: 4.411