Synthesis and in vitro antitumor activity of phthalimide polymers containing podophyllotoxin |
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Authors: | Neung-Ju Lee In-Cheol Jeong Chang-Wan Jeon Young-Ok Kim Ildoo Chung |
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Affiliation: | a Department of Premedical Sciences, College of Medicine, Kosin University, Busan 602-703, Republic of Korea b Department of Biochemistry, College of Medicine, Kosin University, Busan 602-703, Republic of Korea c Department of Surgery, College of Medicine, Kosin University, Busan 602-703, Republic of Korea d Department of Internal Medicine, College of Medicine, Kosin University, Busan 602-703, Republic of Korea e Department of Pathology , College of Medicine, Kosin University, Busan 602-703, Republic of Korea f Department of Biochemistry, College of Medicine, Pusan National University, Busan 609-735, Republic of Korea g Department of Polymer Science and Engineering, Pusan National University, Busan 609-735, Republic of Korea |
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Abstract: | Polymer-linked PT (podophyllotoxin) conjugates have been designed to improve the therapeutic efficacy of PT. A new PT-conjugate, 3,6-endo-methylene-1,2,3,6-tetrahydrophthalimido-acetamidoglycinylglycine podophyllotoxin ester (ETPA-gly-gly-PT), was synthesized by covalently coupling its hydroxyl group onto the phthalimido monomer through a glycine-glycine-glycine spacer. Its homo- and copolymer with acrylic acid (AA) were prepared by photopolymerization using 2,2-dimethoxy-2-phenylacetophenone (DMP) as a photoinitiator. ETPA-gly-gly-PT and its polymers were characterized by IR and proton NMR spectra. The ETPA-gly-gly-PT content in the copolymer obtained by elemental analysis was 44 wt%. The number-average molecular weights of the polymers determined by gel permeation chromatography were as follows: Mn = 13,500 for poly(ETPA-gly-gly-PT), Mn = 17,000 for poly(ETPA-gly-gly-PT-co-AA). The in vitro antitumor activity of these conjugates and polymers were determined and used to evaluate the potential applications in antitumor drugs. The IC50 values indicated that the synthesized ETPA-gly-gly-PT and its polymers against cancer cells were much better inhibitors than PT. |
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Keywords: | 3,6-Endo-methylene-1,2,3,6-tetrahydrophthalimidoacetamidoglycinylglycine podophyllotoxin ester (ETPA-gly-gly-PT) Podophyllotoxin In vitro cytotoxicity Antitumor activity |
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