- Hapten synthesis, monoclonal antibody production and immunoassay development for direct detection of 4-hydroxybenzehydrazide in chicken, the metabolite of nifuroxazide
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Derivatization is usually employed in immunoassay for detection of metabolites of nitrofurans and avoiding derivatization could be preferable to achieve an efficient screening. In the study, we designed four haptens of 4-hydroxybenhydrazide (HBH), the nifuroxazide metabolite. The effect of hapten structures on antibody affinity were evaluated and one monoclonal antibody was produced by using the Hapten C with a linear alkalane spacer arm. After optimization, an enzyme linked-immunosorbent assay (ELISA) was established with an 50% inhibition concentration of 0.25 ng mL?1 for HBH, which could ensure the direct detection of HBH without derivatization. The limit of detection of the ELISA for HBH was 0.12 μg kg?1 with the recoveries of 90.1–96.2% and coefficient of variation (CV) values lower than 9.1%. In conclusion, we produced several high affinity antibodies to HBH with new designed hapten and developed an icELISA for the direct detection of HBH without derivatization in chicken.
- Mari, Ghulam Mujtaba,Li, Hongfang,Dong, Baolei,Yang, Huijuan,Talpur, Aisha,Mi, Jiafei,Guo, Liuchuan,Yu, Xuezhi,Ke, Yuebin,Han, Diangang,Wang, Zhanhui
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- Nifursol hapten, artificial antigen, and preparation method and application thereof
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The invention relates to the field of biochemical engineering, and specifically relates to a nifursol hapten, an artificial antigen, and a preparation method and application thereof. The structure of the nifursol hapten is shown as a formula (I), the artificial antigen is obtained after the nifursol hapten is coupled with carrier protein, the artificial antigen is used as an immunogen to prepare a corresponding hybridoma cell 3H10, and a monoclonal antibody secreted by the hybridoma cell 3H10 can be used for detecting nifursol. A monoclonal antibody prepared by immunizing a mouse with an artificial antigen prepared from the nifursol hapten provided by the invention has relatively high sensitivity in detection of nifursol and derivatives thereof, and a new material basis is provided for establishing a rapid, simple, cheap, sensitive and specific nifursol detection method.
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Paragraph 0058-0060; 0062; 0066-0067
(2021/08/07)
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- Nifuraldezone hapten and artificial antigen as well as preparation method and application thereof
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The invention relates to nifuraldezone hapten and artificial antigen as well as a preparation method and application thereof. The nifuraldezone hapten has a structural formula (I) or (II) shown in thedescription. The nifuraldezone artificial antigen is prepared by coupling the hapten of the formula (I) or (II) with a carrier protein. When the nifuraldezone artificial antigen is adopted to immunize animals, specific antibodies with high valences and high sensitivity can be obtained. By adopting the nifuraldezone hapten and antibodies prepared from same, novel means for establishing rapid, simple, cheap, sensitive and specific nifuraldezone detection methods can be provided.
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- Preparation method and application of derived hapten and artificial antigen of furazolidone metabolite AOZ
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The invention discloses a preparation method and application of a derived hapten and an artificial antigen of a furazolidone metabolite AOZ. An active arm introduced into the hapten completely retains a feature structure of an AOZ derivative and has no in
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Paragraph 0048; 0049; 0050; 0051; 0052
(2017/07/20)
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- Preparation methods and application of semicarbazide SEM derived hapten and artificial antigen
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The invention discloses preparation methods and application of semicarbazide SEM derived hapten and artificial antigen. An active arm introduced by the hapten integrally keeps a characteristic structure of an SEM derivative and has no influences on electr
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Paragraph 0048; 0049; 0050; 0051; 0052
(2017/07/19)
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- Macrodantin metabolite AHD derivatization semiantigen, and preparation method and application of artificial antigen
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The invention discloses a macrodantin metabolite AHD derivatization semiantigen, and a preparation method and application of an artificial antigen. An active arm introduced by the semiantigen completely retains a characteristic structure of an AHD derivat
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Paragraph 0051
(2017/09/13)
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- Photodegradable macromers and hydrogels for live cell encapsulation and release
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Hydrogel scaffolds are commonly used as 3D carriers for cells because their properties can be tailored to match natural extracellular matrix. Hydrogels may be used in tissue engineering and regenerative medicine to deliver therapeutic cells to injured or diseased tissue through controlled degradation. Hydrolysis and enzymolysis are the two most common mechanisms employed for hydrogel degradation, but neither allows sequential or staged release of cells. In contrast, photodegradation allows external real-time spatial and temporal control over hydrogel degradation, and allows for staged and sequential release of cells. We synthesized and characterized a series of macromers incorporating photodegradbale ortho-nitrobenzyl (o-NB) groups in the macromer backbone. We formed hydrogels from these macromers via redox polymerization and quantified the apparent rate constants of degradation (kapp) of each via photorheology at 370 nm, 10 mW/cm2. Decreasing the number of aryl ethers on the o-NB group increases kapp, and changing the functionality from primary to seconday at the benzylic site dramatically increases kapp. Human mesenchymal stem cells (hMSCs) survive encapsulation in the hydrogels (90% viability postencapsulation). By exploiting the differences in reactivity of two different o-NB linkers, we quantitatively demonstrate the biased release of one stem cell population (green-fluoroescent protein expressing hMSCs) over another (red-fluorescent protein expressing hMSCs).
- Griffin, Donald R.,Kasko, Andrea M.
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p. 13103 - 13107
(2012/10/07)
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- 1H-1,2,4-thiadiazolo(3,4-b)quinazolin-5-one-2,2-dioxides, and a method for increasing the cardiac output of a mammal with them
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1H-1,2,4-thiadiazolo[3,4-b]quinazolin-5-one-2,2-dioxides are disclosed. These compounds are useful as caridotonic agents. A preferred compound is 7-(n-cyclohexyl-N-methyl-4-amino-4-oxobutyloxy)-1H-1,2,4-thiadiazolo[3,4-b]quinazolin-5-one-2,2-dioxide.
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- Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide
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Evaluation of a series of lactam heterocyclic analogues of cilostamide as inhibitors of cyclic AMP phosphodiesterase derived from both human platelets and rat heart in comparison with their corresponding methoxy-substituted heterocycles has revealed that the N-cyclohexyl-N-methyl-4-oxybutyramide side chain of 2 is an important lipophilic and/or steric pharmacophore. Attachment of this side chain to the parent heterocycle of the potent cyclic AMP phosphodiesterase inhibitor anagrelide afforded the hybrid structure RS-82856, shown to be more potent than either of its progenitors as an inhibitor of cyclic AMP phosphodiesterase or of ADP-induced platelet aggregation. The available in vitro data suggest that 1 possesses potentially useful antithrombotic and cardiotonic properties.
- Jones,Venuti,Alvarez,Bruno,Berks,Prince
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p. 295 - 303
(2007/10/02)
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- (2-Oxo-1,2,3,5-tetrahydroimidazo-[2,1-B]quinazolinyl) oxyalkylamides properties having phosphodiosterase inhibiting
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Compounds according to the formula STR1 , its optical isomers, or a pharmaceutically acceptable salt thereof wherein: m and n are integers of 1 to 6; R1 is hydrogen or alkyl of 1 to 4 carbons; R2 is hydrogen or R1 and R2 are combined to form an oxo group; R3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or α-amino acid side chains; R4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl; R5 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR6, halo, --NH2, --N(R6)2, --NHCOR6, --COOH, or --COO(R6) group wherein R6 is lower alkyl; phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with 1 or more lower alkyl, halo or lower alkoxy groups or an --NH2, --N(R6)2, --NHCOR6, --COOH, or --COOR6 group wherein R6 is lower alkyl; Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy; and Z is --OR7 or --NR7 R8 wherein R7 and R8 are independently hydrogen or lower alkyl.
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- (2-oxo-3-methylene-1,2,3,5-tetrahydroimidazo[2,1-b]quinazolinyl)oxyalkylamides useful as cyclic AMP phosphodiesterase inhibitors
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This invention relates to compounds of the formula (I) and the pharmaceutically acceptable acid addition salts thereof wherein the various substituents are defined herein. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents in mammals
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- Method of treating heart failure using (2-oxo-1,2,3,5-tetrahydroimidazo-[2,1-b]quinazolinyl)oxyalkylamides
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Compounds according to the formula STR1 and the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer of 1 to 6; R1 is hydrogen or alkyl of 1 to 4 carbon; R2 is hydrogen or R1 and R2 combined are oxo; R3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its acylates, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or amino acid side chains; R4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl; Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy; A is an amide forming group wherein the nitrogen substituents are: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms; cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR5, halo, --NH2, --N(R5)2, --NHCOR5, --COOH, or --COO(R5) group wherein R5 is lower alkyl; phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with 1 or more lower alkyl, halo or lower alkoxy groups or an --NH2, --N(R5)2, --NHCOR5, --COOH, or --COOR5 group wherein R5 is lower alkyl; morpholinyl; piperidinyl; perhexylenyl; N-loweralkylpiperazinyl; pyrrolidinyl; tetrahydroquinolinyl; tetrahydroisoquinolinyl; (±)-decahydroquinolinyl or indolinyl. These compounds have inotropic activity.
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- N,N-Disubstituted-(2-oxo-1,2,3,5-tetrahydroimidazo-[2,1-B]quinazolinyl)oxyalkylamides
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Compounds according to the formula STR1 and the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer of 1 to 6; R1 is hydrogen or alkyl of 1 to 4 carbons; R2 is hydrogen or R1 and R2
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