期刊
BIOCONJUGATE CHEMISTRY
卷 12, 期 1, 页码 129-133出版社
AMER CHEMICAL SOC
DOI: 10.1021/bc000080w
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- NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES [R01DK039544] Funding Source: NIH RePORTER
- NIDDK NIH HHS [DK39544] Funding Source: Medline
Cyclosporin A (CsA) was epoxidized with m-chloroperoxybenzoic acid in the presence of sodium carbonate or with tert-butyl hydroperoxide in the presence of dioxomolybdenum iminodiethanoxide. The CsA epoxide was not stable and rearranged into a compound with a more stable five-member ring structure. An amino group containing cyclosporin A derivative (CsA amine) was obtained by the reaction of CsA epoxide with excess ethylenediamine. The yield of the CsA amine was 30-40% based on the CsA. An HPMA copolymer-CsA conjugate was prepared by the reaction of the CsA amine with an HPMA and MA-Gly-Phe-Leu-Gly-ONp copolymer. The content of CsA amine in the conjugate was 8.7 wt%. The CsA amine was released from the copolymer by enzymatic hydrolysis with papain.
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