- Prednisolone artificial antigen and preparation method and application thereof
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The invention discloses a prednisolone artificial antigen and a preparation method and an application thereof. The prednisolone artificial antigen provided by the invention is an antigen obtained by coupling a prednisolone hapten represented by the formula I with a vector protein. The prednisolone artificial antigen provided by the invention has the advantages of simple synthetic method, high purity and high yield, and has significant value to preparation of a prednisolone antibody and detection of prednisolone drug residues.
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Paragraph 0040; 0041; 0042; 0043; 0044
(2017/01/02)
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- Prednisolone succinate-glucosamine conjugate: Synthesis, characterization and in vitro cellular uptake by kidney cell lines
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Prednisolone succinate-glucosamine (PSG) conjugate, a prodrug for prednisolone, was synthesized and confirmed by NMR and MS spectrum. The stabilities of the prodrug in PBS (pH 2.50, 5.00, 7.20, and 7.89) were studied. Cytotoxicity and uptake assay of the prodrug were perfomed on HK-2 and MDCK cell lines. The results showed that compared with prednisolone, the PSG not only did not increase the cytotoxicity but also improved the uptake to 2.2 times of prednisolone by the cells. Thus, it indicated that glucosamine might be a potential carrier for kidney-targeting delivery of prednisolone.
- Lin, Yan,Sun, Xun,Gong, Tao,Zhang, Zhi Rong
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scheme or table
p. 25 - 28
(2012/04/04)
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- Prednisolone-α-cyclodextrin-star PEG polypseudorotaxanes with controlled drug delivery properties
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The reaction of α-amino-ω-methoxypoly(ethylene glycol) [M = 5000] or star α-amino-poly(ethylene glycol) [M = 20000] with hemiesters of prednisolone dicarboxylic acids (succinic, glutaric, adipic, phthalic acid) has been used to prepare the corresponding conjugates. The rate of esterase catalyzed hydrolysis of the conjugates is controlled by the molecular mass of poly(ethylene glycol) and the length of the linker between prednisolone and poly(ethylene glycol) (τ1/2 ~ 5-0.5 h). The enzymatic hydrolysis proceeds most rapidly at conjugates with linkers derived from adipic and phthalic acids. The synthesized conjugates form polypseudorotaxanes with α-cyclodextrin which were characterized by 2D NOESY NMR spectra, powder X-ray diffraction patterns and in one case also by STM microscopy. In the case of the polypseudorotaxane having the linker derived from adipic acid, the enzymatic release proceeds ca. five times slower in comparison with the rate of prednisolone release from the corresponding conjugate. The rate of prednisolone release from the carrier can be controlled by three factors: character of the linker between the polymeric carrier and prednisolone, the molecular mass of poly(ethylene glycol) and complex formation with α-cyclodextrin. The synthesized polypseudorotaxanes represent new promising transport systems intended for targeted release of prednisolone in transplanted liver.
- Bilkova, Elika,Sedlak, Milo,Dvoak, Bohuslav,Ventura, Karel,Knotek, Petr,Benes, Ludvik
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experimental part
p. 5423 - 5430
(2011/01/11)
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- The synthesis and immunosuppressive activities of steroid-urotoxin linkers
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The urotoxins (Glu-Asp-Gly-OH, His-Gly-Glu-OH, His-Gly-Lys-OH, and His-Gly-Lys-NHNH2) were introduced into the convenient sites of hydrocortisone and prednisolone via the amidation or condensation reactions to form the corresponding linkers 7a-d, 8a-d, 9a,b, and 10a,b in acceptable yields. The bioassays such as prolongation of heterotopic transplanted cardiac tissue survival in vivo, inhibitory effects on phagocytosis of mouse peritoneal macrophages and concanavalin (ConA) or lipopolysaccharide (LPS) induced proliferation of mouse spleen lymphocytes in vitro show that at the comparable concentrations the immunosuppressive activities of the steroid-urotoxin linkers 7a-d, 8a-d, 9a,b, and 10a,b were higher than that of hydrocortisone, prednisolone, and the urotoxins alone, as well as significantly higher than that of the mixture of hydrocortisone and urotoxins or prednisolone and urotoxins. The so-called 'permissive action' may be responsible for the enhancement of the mentioned bioactivities of the steroid-urotoxin linkers 7a-d, 8a-d, 9a,b, and 10a,b.
- Wang, Chao,Zhao, Ming,Qiu, Xuecai,Peng, Shiqi
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p. 4403 - 4421
(2007/10/03)
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- Studies on the reductively triggered release of heterocyclic and steroid drugs from 5-nitrothien-2-ylmethyl prodrugs
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Hypoxia (inadequate concentrations of dioxygen in tissues) is present in several disease states, including cancer and rheumatoid arthritis. Prodrug systems, which after bioreduction, selectively release active drugs in these tissues may be important in therapy. The 5-nitrothien-2-ylmethyl ester of aspirin was synthesised by treatment of 5-nitrothiophene-2-methanol with 2-acetoxybenzoyl chloride, whereas that of prednisolone hemisuccinate was prepared by reaction of prednisolone with 5-nitrothien-2-ylmethyl pentafluorophenyl butanedioate. In chemical model systems, both of these ester-linked potential prodrugs suffered hydrolysis, rather than reductively triggered release of the corresponding drug. 1-(5-Nitrothien-2-ylmethoxy)isoquinolines released the corresponding isoquinolin-1-ones (potent inhibitors of poly(ADP-ribose)polymerase) rapidly upon reduction of the nitro group with sodium borohydride/palladium, showing that these may be useful as reductively triggered prodrugs. In approaches to N-linked potential prodrugs, isoquinolin-1-one and nifedipine (a 1,4-dihydropyridine Ca2+ channel antagonist) were alkylated at nitrogen by 2-chloromethylthiophene but the corresponding 5-nitrothien-2-ylmethyl derivatives were synthetically inaccessible.
- Ferrer, Sandra,Naughton, Declan P.,Threadgill, Michael D.
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p. 3437 - 3444
(2007/10/03)
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- STEROID COMPOUND COMBINED WITH POLYSACCHARIDE
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A compound which can maintain a blood steroid level unchanged for long after administration, obtained by combining a steroid derivative with a polysaccharide directly or via a spacer. Desirable examples of the steroid derivative include ones having carboxyl and/or hydroxyl groups, and those of the spacer include polybasic carboxylic acids, while those of the polysaccharide include water-soluble ones such as dextran. When administered, the compound releases the steroid in the blood and the steroid level is kept constant for long.
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