Enhancing Anticancer Potency of a 13-Substituted Berberine Derivative with Cationic Liposomes
| Autor: | Nuttapon Apiratikul, Kanlayanee Sriklung, Kulvadee Dolsophon, Pattamaporn Thamvapee, Ramida Watanapokasin, Boon-ek Yingyongnarongkul, Nattisa Niyomtham, John B. Bremner, Petcharat Watanavetch, Siritron Samosorn |
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| Rok vydání: | 2022 |
| Předmět: | |
| Zdroj: | Chemical and Pharmaceutical Bulletin. 70:420-426 |
| ISSN: | 1347-5223 0009-2363 |
| DOI: | 10.1248/cpb.c21-01049 |
| Popis: | 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 60 min 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. |
| Databáze: | OpenAIRE |
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