Thiolated pectin–doxorubicin conjugates: Synthesis, characterization and anticancer activity studies
MetadataShow full item record
© 2017 Elsevier Ltd In this paper, pectin was cross-linked by a coupling reaction with either thioglycolic acid or cystamine dihydrochloride to form thiolated pectins. The thiolated pectins were then coupled with doxorubicin (DOX) derivative to obtain thiolated pectin–DOX conjugates by two different methods, disulfide bond formation and disulfide bond exchange. The disulfide bond exchange method provided a simple, fast, and efficient approach for synthesis of thiolated pectin–DOX conjugates, compared to the disulfide bond formation. Characteristics, physicochemical properties, and morphology of thiolated pectins and thiolated pectin–DOX conjugates were determined. DOX content in thiolated pectin–DOX conjugates using low methoxy pectin was found to be higher than that using high methoxy pectin. The in vitro anticancer activity of thiolated pectin–DOX conjugates was significantly higher than that of free DOX, in mouse colon carcinoma and human bone osteosarcoma cells, but insignificantly different from that of free DOX, in human prostate cancer cells. Due to their promising anticancer activity in mouse colon carcinoma cells, the thiolated pectin–DOX conjugates might be suitable for building drug platform for colorectal cancer-targeted delivery of DOX.
Showing items related by title, author, creator and subject.
Characterization and in vitro release studies of oral microbeads containing thiolated pectin-doxorubicin conjugates for colorectal cancer treatmentCheewatanakornkool, K.; Niratisai, S.; Manchun, S.; Dass, Crispin; Sriamornsak, P. (2017)© 2017 Shenyang Pharmaceutical University. Novel oral microbeads were developed based on a biopolymer-drug conjugate of doxorubicin (DOX) conjugated with thiolated pectin via reducible disulfide bonds. The microbeads were ...
Redox-responsive microbeads containing thiolated pectin-doxorubicin conjugate inhibit tumor growth and metastasis: An in vitro and in vivo studyCheewatanakornkool, K.; Niratisai, S.; Dass, Crispin; Sriamornsak, P. (2018)© 2018 The objective of this study was to investigate the in vitro cytotoxicity and in vivo anticancer efficacy of redox-responsive microbeads containing thiolated pectin–doxorubicin (DOX) conjugate. Oral microbeads were ...
Ho, D.; Kretzmann, J.; Norret, M.; Toshniwal, P.; Veder, Jean-Pierre; Jiang, H.; Guagliardo, P.; Munshi, A.; Chawla, R.; Evans, C.; Clemons, T.; Nguyen, M.; Kretzmann, A.; Blythe, A.; Saunders, M.; Archer, M.; Fitzgerald, Melinda; Keelan, J.; Bond, C.; Kilburn, M.; Hurley, L.; Smith, N.; Iyer, K. (2018)© 2018, The Author(s), under exclusive licence to Springer Nature Limited. Gold nanorods are one of the most widely explored inorganic materials in nanomedicine for diagnostics, therapeutics and sensing1. It has been shown ...