Publication: Enhancing Anticancer Potency of a 13-Substituted Berberine Derivative with Cationic Liposomes
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Issued Date
2022
Resource Type
Language
eng
File Type
application/pdf
ISSN
92363
Rights Holder(s)
Scopus
Bibliographic Citation
Bioresource Technology Reports. Vol 18, No. (2022)
Suggested Citation
Apiratikul N., Sriklung K., Dolsophon K., Thamvapee P., Watanapokasin R., Yingyongnarongkul B.-E., Niyomtham N., Bremner J.B., Watanavetch P., Samosorn S. Enhancing Anticancer Potency of a 13-Substituted Berberine Derivative with Cationic Liposomes. Bioresource Technology Reports. Vol 18, No. (2022). doi:10.1248/cpb.c21-01049 Retrieved from: https://hdl.handle.net/20.500.14740/9237
Abstract
Cationic liposomal formulations of the telomeric G-quadruplex stabilizing ligand, 13-(2-naphthylmethoxy)-berberine bromide (1), have been developed with the purpose of delivering 1 into the nucleus of cancer cells for potential telomere targeting. Berberine derivative 1 was encapsulated in various cationic lipids 2–4 by the thin film evaporation method; these lipids are cationic after amine protonation. The most appropriate liposomal berberine formulation was that of 1 and the cholesterol derived cationic lipid 4 in a weight ratio of 1:20 with 76.5% encapsulation efficiency of 1. Cellular uptake studies in the HeLa and HT-29 cancer cells lines showed that the liposomal berberine derivative uptake in the cells was higher and more stable than for berberine derivative 1 alone while free 1 was completely decomposed in the cells within 60min exposure to the cells. Anticancer activity of the liposomal berberine derivative 1 based on 4 was greater than that for the free berberine derivative 1 in the MCF-7, HeLa and HT-29 cell line by 2.3-, 4.9- and 5.3-fold, respectively, and also, interestingly, superior to the anticancer drug doxorubicin against the HT29 cancer cell line. © 2022 The Pharmaceutical Society of Japan