화학공학소재연구정보센터
학회 한국고분자학회
학술대회 2005년 가을 (10/13 ~ 10/14, 제주 ICC)
권호 30권 2호
발표분야 의료용 고분자 부문위원회
제목 Pegylation of all trans-retinoic acid
초록 Conjugation of biomolecules with polyethylene glycol (PEG), a process known as pegylation, is a technique of growing interest for enhancing the therapeutic and biotechnological potential of anti-drugs, peptides and proteins. The PEGs as nontoxic water-soluble polymers owing to their large hydrodynamic volume, create a shield around the pegylated drug, thus protecting it from renal clearance, enzymatic degradation, and recognition by cells of the immune system. Agent-specific pegylation methods have been used in recent years to produce pegylated drugs that have biologic activity that is the same as, or greater than, that of the parent drug.
All trans-retinoic acid (atRA), the metabolite of vitamin A, regulates all important biological programs, such as growth, development, differentiation, reproduction, morphogenesis, metabolism and homeostasis. And it has been shown to have chemo-preventive and therapeutic activity for certain cancers, and it can induce differentiation and/or growth arrest.
But, there are some shortcomings with atRA, such as cytotoxity, light sensitive, low solubility in water, etc. So in this study, all trans-retinoic acid was conjugated with PEG to overcome these shortcomings, and extend blood circulation time and improve the biocompatibility.
In the measurement of cell viability, average cell viability over 100 % for pegylated atRA was obtained at any concentrations whereas cell viability for atRA was rapidly decreased. The cell viability was not changed with an increase of concentration of pegylated atRA whereas it was rapidly decreased with an increase of atRA concentration owing to the cell toxicity of atRA. And the pegylated atRA can induce or change some genes expression that similar to atRA. Pegylated atRA can induce P450RAI gene expression in hepatocytes, and the expression levels was gradually increased by increasing the atRA exposure time, like atRA. And anti-cancer property of the pegylated atRA in vitro will be reported.
저자 곽정정, 서석진, 문현석, 조종수
소속 서울대
키워드 all trans-retinoic acid; pegylation; anti-cancer
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