1.The key to fine manufacturing of liquid polyphenol preparations: the principle of multi-precipitation with steady-state reconstruction
Hao-zhou HUANG ; Fei RAN ; Jun-zhi LIN ; Meng-qi LI ; Wen-quan ZOU ; San-hu FAN ; Ming YANG ; Run-chun XU ; Li HAN ; Ding-kun ZHANG
Acta Pharmaceutica Sinica 2020;55(1):45-53
Plant polyphenols have a wide range of pharmacological activities and application prospects. Liquid polyphenol preparations have special physical phases and complex chemical compositions, with problems such as poor stability and easy precipitation during production and marketing. Taking the multi-precipitation mechanism of plant polyphenol liquid preparations as an example,we discuss the chemistry and composition of the precipitation, how it forms, whether precipitationcan be controlled, and the interaction law of three precipitation approaches. An unstable mechanism model is proposed where hydrolyzed tannin hydrolysis and catechin non-enzymatic oxidative polymerization repeatedly induces associative colloid aggregation and precipitation. This study explains the complex physicochemical changes in polyphenol solutions and the microcosmic mechanism of instability in the induced system and proposes a steady state reconstruction of liquid polyphenol preparation consistent with the common law of precipitation and control. It has scientific significance for promoting the development and manufacture of high quality liquid polyphenol preparations.
2.Research,evaluation,industry status and development strategy of traditional Chinese medicine functional food.
Rong SUN ; Xiao-Tian QI ; Guang-Yao CHEN ; Gui-Min ZHANG ; Er-Ping XU ; Ming-San MIAO ; Na-Na HUANG ; Jin-Bo WANG
China Journal of Chinese Materia Medica 2019;44(5):861-864
With the development of social economy,people's demand for health services is growing rapidly. As health resource with Chinese characteristics,health food containing Chinese materia medica have broad prospect and great market space for development.However,at present,there are still many problems of health food containing Chinese materia media in the research,development,evaluation and market application. In addition,due to lack of theoretical support of traditional Chinese medicine(TCM) in the research and development of health food containing Chinese materia media,blurred boundaries between health food containing Chinese materia media and other health products as well as TCM are present,lacking of TCM characteristics. In the evaluation process of health food containing Chinese materia media,the construction of functional food laws,regulations and evaluation norms is relatively lagging behind,which can't meet the needs of health food containing Chinese materia media research and development,severely restricting the development of health food containing Chinese materia media. Based on the research and evaluation of health food containing Chinese materia media,the existing problems were reviewed and the reasons for the deficiencies were analyzed in this paper. Guided by the theory of TCM,based on the constitution identification in TCM,and combined with modern scientific and technological means,a new research and development mode of functional food was put forward in this paper to distinguish health food containing Chinese materia media from TCM as well as general health products. Nevertheless,we should ensure the vitality of Chinese medicine health products with original thinking and scientific and technological connotations,and accelerate the harmonious,rapid and sustainable development of Chinese medicine health industry.
Functional Food
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Industry
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Materia Medica
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Medicine, Chinese Traditional
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Research
3.Effect of electrical stimulation at auricular points combined with sound masking on the expression of CREB, BDNF and TrkB in the auditory cortex of tinnitus rats.
Song-Bai YANG ; Li-Yan PENG ; Zhi-Gang MEI ; Ling-Jing TAN ; Ya-Guang HUANG ; Zhi-Tao FENG ; San-Jin CAI ; Wen-Han MA ; Ding-Qi ZHANG
Chinese Acupuncture & Moxibustion 2019;39(6):637-642
OBJECTIVE:
To explore the effect of electrical stimulation at auricular points (EAS) combined with sound masking on the expression of cAMP-response element binding protein (CREB), brain-derived neurotrophic factor (BDNF) and tyrosine receptor kinase B (TrkB) in the auditory cortex of tinnitus rats.
METHODS:
A total of 27 adult male SD rats were randomly divided into a control group, a model group and an EAS group. The rats in the model group and the EAS group were intervened with intraperitoneal injection of sodium salicylate to induce tinnitus model, while the rats in the control group were intervened with injection of 0.9% NaCl solution. After the model was successfully established, the rats in the EAS group were treated with electrical stimulation at "Shenmen" (TF) and "Yidan" (CO), combined with sound masking; the treatment was given once a day for 15 days. The gap prepulse inhibition of acoustic startle (GPIAS) and prepulse inhibition (PPI) testing were performed using the acoustic startle reflex starter package for rats. The expression of BDNF, TrkB, CREB and p-CREB in the auditory cortex of each group were measured with Western Blot analysis.
RESULTS:
① Compared with the control group, the GPIAS values in 12 kHz, 16 kHz, 20 kHz and 28 kHz were significantly decreased in the model group (all <0.05); compared with the model group, GPIAS values in 12 kHz, 16 kHz, 20 kHz and 28 kHz were significantly increased in the EAS group (all <0.05). ② Compared with the control group, the expression of BDNF and p-CREB in the model group was significantly increased (<0.01), and the expression of TrkB in the model group was significantly increased (<0.05); the differences of expression of BDNF, TrkB, CREB and p-CREB between the model group and the EAS group had no statistics significance (all >0.05).
CONCLUSION
EAS could improve the GPIAS values of high-frequency background sound in tinnitus rats, which may be related with the upregulation of the BDNF/TrkB/CREB signaling pathway in the auditory cortex, leading to the reversion of the maladaptive plasticity.
Acupuncture Points
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Animals
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Auditory Cortex
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Brain-Derived Neurotrophic Factor
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metabolism
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Cyclic AMP Response Element-Binding Protein
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metabolism
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Electric Stimulation
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Male
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Rats
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Rats, Sprague-Dawley
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Receptor, trkB
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metabolism
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Tinnitus
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metabolism
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therapy
4.Cryptosporidium spp., Giardia intestinalis, and Enterocytozoon bieneusi in Captive Non-Human Primates in Qinling Mountains.
Shuai Zhi DU ; Guang Hui ZHAO ; Jun Feng SHAO ; Yan Qin FANG ; Ge Ru TIAN ; Long Xian ZHANG ; Rong Jun WANG ; Hai Yan WANG ; Meng QI ; San Ke YU
The Korean Journal of Parasitology 2015;53(4):395-402
Non-human primates (NHPs) are confirmed as reservoirs of Cryptosporidium spp., Giardia intestinalis, and Enterocytozoon bieneusi. In this study, 197 fresh fecal samples from 8 NHP species in Qinling Mountains, northwestern China, were collected and examined using multilocus sequence typing (MLST) method. The results showed that 35 (17.8%) samples were positive for tested parasites, including Cryptosporidium spp. (3.0%), G. intestinalis (2.0%), and E. bieneusi (12.7%). Cryptosporidium spp. were detected in 6 fecal samples of Macaca mulatta, and were identified as C. parvum (n=1) and C. andersoni (n=5). Subtyping analysis showed Cryptosporidium spp. belonged to the C. andersoni MLST subtype (A4, A4, A4, and A1) and C. parvum 60 kDa glycoprotein (gp60) subtype IId A15G2R1. G. intestinalis assemblage E was detected in 3 M. mulatta and 1 Saimiri sciureus. Intra-variations were observed at the triose phosphate isomerase (tpi), beta giardin (bg), and glutamate dehydrogenase (gdh) loci, with 3, 1, and 2 new subtypes found in respective locus. E. bieneusi was found in Cercopithecus neglectus (25.0%), Papio hamadrayas (16.7%), M. mulatta (16.3%), S. sciureus (10%), and Rhinopithecus roxellana (9.5%), with 5 ribosomal internal transcribed spacer (ITS) genotypes: 2 known genotypes (D and BEB6) and 3 novel genotypes (MH, XH, and BSH). These findings indicated the presence of zoonotic potential of Cryptosporidium spp. and E. bieneusi in NHPs in Qinling Mountains. This is the first report of C. andersoni in NHPs. The present study provided basic information for control of cryptosporidiosis, giardiasis, and microsporidiosis in human and animals in this area.
Animals
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China
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Cryptosporidiosis/*parasitology
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Cryptosporidium/classification/genetics/*isolation & purification
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Enterocytozoon/classification/genetics/*isolation & purification
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Feces/parasitology
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Female
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Genotype
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Giardia lamblia/classification/genetics/*isolation & purification
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Giardiasis/parasitology/*veterinary
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Male
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Microsporidiosis/parasitology/*veterinary
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Molecular Sequence Data
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Phylogeny
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Primate Diseases/*parasitology
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Primates/classification/parasitology
5.MAGI3 Suppresses Glioma Cell Proliferation via Upregulation of PTEN Expression.
Qian MA ; Yan ZHANG ; Ran MENG ; Kun Ming XIE ; Ying XIONG ; Song LIN ; Zong Lin K HE ; Tao TAO ; Ying YANG ; Ji Zong ZHAO ; Jun Qi HE
Biomedical and Environmental Sciences 2015;28(7):502-509
OBJECTIVETo investigate the role and molecular mechanism of membrane-associated guanylate kinase inverted 3 (MAGI3) in glioma cell proliferation.
METHODSThe expression levels of MAGI3 and PTEN were assessed in glioma samples by Western blotting. MAGI3 was stably transfected into C6 glioma cells to obtain C6-MAGI3 cells. Then, the proliferation, the expression levels of MAGI3 and PTEN, and Akt phosphorylation were evaluated in C6 and C6-MAGI3 cells. Xenograft tumor models were established by subcutaneous injection of C6 and C6-MAGI3 cells into nude mice, and the growth rates of xenografts in the mice were compared. The potential role of MAGI3 expression in PI3K/Akt signaling activation was further investigated by examining the correlation between MAGI3 expression and the expression of PI3K/Akt signaling downstream target genes in a glioma dataset using gene set enrichment analysis (GSEA).
RESULTSExpression levels of MAGI3 and PTEN were significantly downregulated in gliomas. Overexpression of MAGI3 in the glioma C6 cell line upregulated PTEN protein expression, inhibited the phosphorylation of Akt, and suppressed cell proliferation. MAGI3 overexpression also inhibited the growth of C6 glioma tumor xenografts in nude mice. Analysis based on the GEO database confirmed the negative correlation between activation of PI3K/Akt pathway and MAGI3 mRNA levels in human glioma samples.
CONCLUSIONThe loss of MAGI3 expression in glioma may enhance the proliferation of glioma cells via downregulation of PTEN expression, leading to the activation of the PI3K/Akt pathway. MAGI3 is a potential glioma suppressor.
Animals ; Brain Neoplasms ; genetics ; metabolism ; pathology ; Cell Line, Tumor ; Cell Proliferation ; genetics ; Down-Regulation ; Glioma ; genetics ; metabolism ; pathology ; Humans ; Membrane Proteins ; genetics ; metabolism ; Mice, Nude ; PTEN Phosphohydrolase ; genetics ; metabolism ; Phosphatidylinositol 3-Kinases ; metabolism ; Phosphorylation ; Proto-Oncogene Proteins c-akt ; metabolism ; Rats ; Signal Transduction ; Transfection ; Up-Regulation ; Xenograft Model Antitumor Assays
6.The preparation and kinetic study on enzymatically-controlled drug release of isotretinoin/amylose inclusion complex.
Qi-Fang WANG ; San-Ming LI ; Tian-Hong ZHANG ; Jing YU ; Zhong-Sheng HU ; Yue LI
Acta Pharmaceutica Sinica 2012;47(9):1227-1230
The inclusion complex of isotretinoin was prepared by sealed-control temperature method and amylose was used as carrier. The formation of inclusion complex was confirmed by powder X-ray diffraction and DSC. The equation of enzymatically-controlled drug release was established by kinetic theory, and the release characteristic of drug was confirmed by using the kinetic equation. The results show that the drug release was attributed to first order reaction without alpha-amylase. However, with alpha-amylase, the drug release was an acceleration process by the effect of both dissociation and enzymatic hydrolysis simultaneously. The research indicates that drug release from the inclusion complex was modulated by the addition of alpha-amylase.
Amylose
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chemistry
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Calorimetry, Differential Scanning
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Dermatologic Agents
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chemistry
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Drug Carriers
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chemistry
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Hydrolysis
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Isotretinoin
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chemistry
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Kinetics
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Temperature
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X-Ray Diffraction
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alpha-Amylases
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chemistry
7.Modulating drug loading and release profile of beta-cyclodextrin polymers by means of cross-linked degree.
Qi-fang WANG ; San-ming LI ; Yu-yang ZHANG ; Hong ZHANG
Acta Pharmaceutica Sinica 2011;46(2):221-226
The purpose of the present study is to use beta-cyclodextrin polymers (beta-CDP) with different cross-linked degree (CLD) to form inclusion complexes with ibuprofen and examine the effects of structural and compositional factors of beta-CDP on its drug loading and release behaviors. A series of beta-CDP with different CLD were synthesized and characterized by Fourier Transform Infrared Spectroscopy (FT-IR) and 13C NMR spectrum. The beta-CDP was systemically characterized for the relation between the CLD of beta-CDP and the drug loading and release as well. The results of FT-IR and 13C NMR showed that similar peak-shaped vibration of beta-CDP and beta-CD implies that the polymer keeps the original characteristic structure of beta-CD. The CLD of the beta-CDP played a critical role in the drug loading and release, increasing the CLD resulted in reduction of drug loading, but increase in drug release.
Carbon Isotopes
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Cross-Linking Reagents
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chemistry
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Delayed-Action Preparations
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Drug Carriers
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Drug Compounding
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Drug Delivery Systems
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Ibuprofen
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administration & dosage
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chemistry
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Magnetic Resonance Spectroscopy
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Pharmaceutical Preparations
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administration & dosage
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chemistry
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Polymers
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chemistry
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Solubility
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Spectroscopy, Fourier Transform Infrared
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beta-Cyclodextrins
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chemistry
8.Re-analysis of occupational hazards in foundry.
Min ZHANG ; Cheng QI ; Wei-Hong CHEN ; Yang LU ; Xie-Yi DU ; Wen-Jie LI ; Chuan-San MENG
Chinese Journal of Industrial Hygiene and Occupational Diseases 2010;28(4):280-285
OBJECTIVETo analyze systematically the characteristics of occupational hazards in the foundry, and provide precise data for epidemiology studies and control of occupational hazards in the foundry.
METHODSData of airborne dust, chemical occupational hazards and physical occupational agents in environment in the foundry from 1978 to 2008 were dynamically collected. Mean concentration and intensity (geometric mean) of occupational hazards were calculated by job in different years.
RESULTSMain occupational hazards in the foundry were silica, metal fume, noise and heat stress. Silica existed in all of main jobs. The mean concentration of silica before 1986 was an extremely high level of 8.6 mg/m(3), and then remarkably dropped after 1986, with the level of 2.4 mg/m(3) from 1986 to 1989, 2.7 mg/m(3) from 1990 to 2002 and 2.7 mg/m(3) from 2003 to 2008. The trend of silica concentrations by job was consistent with that in general. Silica concentrations among jobs were significantly different, with highest level in melting (4.4 mg/m(3)), followed by cast shakeout and finishing (3.4 mg/m(3)), pouring (3.4 mg/m(3)), sand preparation (2.4 mg/m(3)), moulding (2.1 mg/m(3)) and core-making (1.7 mg/m(3)). Concentration of respirable dust in pouring was highest (2.76 mg/m(3)), followed by cast shakeout and finishing (1.14 mg/m(3)). Mean concentration of asbestos dust in melting was a relative high level of 2.0 mg/m(3). In core-making and sand preparation, there existed emission production of adhesive, with mean concentrations as followed, ammonia (5.84 mg/m(3)), formaldehyde (0.60 mg/m(3)), phenol (1.73 mg/m(3)) and phenol formaldehyde resin (1.3 mg/m(3)) also existed. Benzene and its homologues existed in cast shakeout and finishing, and the level of benzene, toluene, xylene was 0.2 mg/m(3), 0.1 mg/m(3) and 1.3 mg/m(3), respectively. In pouring and melting, there existed chemical occupational hazards, including benzo(a) pyrene, metal fume (lead, cadmium, manganese, nickel, chromium) and gas(hydrogen sulfide, phosphine, sulfur dioxide, carbon monoxide). Mean concentration of benzo(a) pyrene was a low level of 1.80 x 10(-4) microg/m(3). Physical occupational agents in the foundry were noise, heat stress and vibration. Intensity of heat stress was high in melting, pouring and cast shakeout and finishing, with the level of 30 degrees C, 29 degrees C and 26 degrees C, respectively. Noise was high in cast shakeout and finishing and core-making, with the level of 93.1 dB(A) and 89.5 dB(A), respectively. Vibration existed in core-making and cast shakeout and finishing. Compulsory postures included long standing, seating and bowing.
CONCLUSIONOccupational hazards in environment of the foundry are diversified and their concentrations exceed permissible exposure limits stipulated by the national occupational hygienic standards. High-concentrations of dust, metal fume, low-concentrations of variety of chemicals, high-intensity of noise and vibration, heat stress, and harmful compulsory posture, and so on all co-exist in the foundry. Control and protective measures should be strengthened.
Dust ; analysis ; Hazardous Substances ; analysis ; Metallurgy ; Occupational Exposure
9.Synthesis of 2-hydroxyl-5-butyramidobenzoic acid and its effect on acetic acid-induced colitis in rats.
Rui-cai SHI ; Jian-feng XING ; Zhao-guo LIU ; Zhi-zhao YUAN ; San-qi ZHANG ; Xiao-li BIAN ; Ai-guo ZENG
Journal of Southern Medical University 2009;29(9):1843-1845
OBJECTIVETo study the method for synthesis of 2-hydroxyl-5- butyramidobenzoic acid and test its effect on acetic acid-induced colitis in rats.
METHODS2-hydroxyl-5-butyramidobenzoic acid was synthesized from 5-aminosalicylic acid and butyric acid by amidation, esterification and hydrolization. The effect of 2-hydroxyl-5-butyramidobenzoic acid on acetic acid enema-induced colitis in rats was investigated.
RESULTSThe structure of 2-hydroxyl-5-butyramidobenzoic acid was identified by IR and 1H-NMR. After treatment with acetic acid, the colon mucosal damage index (CMDI), fecal occult blood (OB) test, and activity of myelperoxidase (MPO) increased significantly in the rats as compared to the control levels. 2-hydroxyl-5- butyramidobenzoic acid obviously reduced the CMDI and OB, and reduced the level of MPO in the rats with colitis.
CONCLUSIONThe synthesis of 2-hydroxyl-5-butyramidobenzoic acid requires only mild conditions with simple procedures, and the synthesized 2-hydroxyl-5-butyramidobenzoic acid shows obvious therapeutic effects on mucosal damage of in rats with acetic acid-induced colitis.
Acetic Acid ; Aminobenzoates ; chemical synthesis ; chemistry ; pharmacology ; therapeutic use ; Animals ; Colitis, Ulcerative ; chemically induced ; drug therapy ; Male ; Protective Agents ; chemical synthesis ; pharmacology ; therapeutic use ; Rats ; Rats, Sprague-Dawley ; Salicylates
10.Preparation and identification of a polyclonal antibody against novel cysteinyl leukotriene receptor GPR17.
Ling-ling QI ; Yun-bi LU ; Wen-zhen SHI ; Chun-zhen ZHAO ; Yong-mei ZHANG ; Li-ping CHEN ; Li-hui ZHANG ; San-hua FANG ; Jian-fang BAO ; Jian-gen SHEN ; Er-qing WEI
Journal of Zhejiang University. Medical sciences 2009;38(4):357-361
OBJECTIVETo prepare and identify a polyclonal antibody (pAb) against GPR17, a novel cysteinyl leukotriene receptor.
METHODSRabbits were immunized with KLH-coupled GPR17 peptide to prepare the pAb. The titer of the pAb in rabbit plasma was detected by indirect ELISA, and the specificity of the pAb was tested by antigen blockade. GPR17 tissue distribution was detected by Western blot with the pAb.
RESULTSThe pAb showed a titer as high as 1:16 364,and was not cross-reacted with the antigens of CysLT(1) and CysLT(2) receptors. A higher expression of GPR17 in the rat brain and heart was detected using the newly prepared pAb. The molecular weigh of GPR17 protein was about 43 kD.
CONCLUSIONThe prepared GPR17 pAb has high sensitivity and specificity,and can be used in Western blot for detecting GPR17.
Animals ; Antibodies, Monoclonal ; biosynthesis ; immunology ; Enzyme-Linked Immunosorbent Assay ; Humans ; Rabbits ; Rats ; Receptors, G-Protein-Coupled ; immunology ; Receptors, Leukotriene ; immunology

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