1.Research on PEG modification of uricase
Lei CAI ; Xiangdong GAO ; Shu ZHU ; Hua WANG ; Wenbing YAO
Journal of China Pharmaceutical University 2008;(6):557-562
To modify uricase with PEG reagent in order to decrease uricase immunogenieity and increase its stability.Methods:The branched PEG of 40 kD was chosen to modify native uricase.The properties of the mod-ified uricase including the stabilities to protease,pH and temperature,in vivo half-life time,as well as the immu-nogenicity were evaluated.The pharmacokinetic profiles of the midofied uricase were studied in mice.Results:It is demonstrated that the conjugation of PEG to lysine residues of Candida utilis uricase resulted in higher tryp-sin resistance.reduced immune response.and prolonged in vivo half-life.PEG modified uricase retained 80% of the enzymatic activity of native uricase.In addition,it was found that half-life in serum of the intravenously injec-ted PEGylated uriease of up to 696 min was longer that that of native uficase of 45 min.Higher plasma drug con-centrations were also reached with dosing of the PEGylated uricase to mice.Furthermore,the binding affinity Was shown to be reduced for the PEG-uricase using ELISA assay.and it was one-eishth that of native uricase.Final-ly,it Was indicated that the PEG uficase induced a delayed immunoresponse in mice following repeated adminis-trations.Conclusion:These findings demonstrate that this chemically modified form of uricase may serve as a potentially effective drug to treat gout patients.
2.Clinical study on primary osteoporosis treated with spreading moxibustion for warming yang and activating blood circulation.
Kun YANG ; Sheng-Chao CAI ; Cai-Feng ZHU ; Ai-Hua FEI ; Xiao-Feng QIN ; Jian-Guo XIA
Chinese Acupuncture & Moxibustion 2014;34(6):555-558
OBJECTIVETo observe the efficacy on primary osteoporosis treated with spreading moxibustion for warming yang and activating blood circulation so as to provide the effective clinical therapeutic methods for osteoporosis.
METHODSSixty cases of primary osteoporosis were randomized into a spreading moxibustion group (30 cases) and a calcium tablet group (30 cases). In the calcium tablet group, caltrate was prescribed for oral administration, 600 mg per day. In the spreading moxibustion group, on the basis of the treatment as the calcium tablet group, the spreading moxibustion was applied at Dazhui (GV 14) to Yaoshu (GV 2) for warming yang and activating blood circulation. The duration of treatment was 12 weeks. Visual analogue scale (VAS) score, TCM clinical symptom score and bone mineral density (BMD) were observed and compared before and after treatment in the patients between the two groups.
RESULTSVAS scores were reduced apparently after treatment in the two groups (both P < 0.01) and the results in the spreading moxibustion group were obviously superior to that in the calcium tablet group (2.36 +/- 0.43 vs 4.52 +/- 0.35, P < 0.01). BMD were all increased in the two groups (P < 0.05, P < 0.01) and the results in the spreading moxibustion group were superior to those in the calcium tablet group (both P < 0.05). The total clinical effective rate was 86.67% (26/30) in the spreading moxibustion group, apparently better than 63.33% (19/30) in the calcium tablet group (P < 0.05). TCM clinical symptom scores after treatment were all reduced apparently in the two groups (both P < 0.01), and the result in the spreading moxibustion group was obviously superior to that in the calcium tablet group (4.72 +/- 1.90 vs 6.82 +/- 2.30, P < 0.01). The total effective rate of TCM symptoms was 93.33% (28/30) in the spreading moxibustion group, apparently better than 70.00% (21/30) in the calcium tablet group (P < 0.05).
CONCLUSIONThe combined therapy of spreading moxibustion for warming yang and activating blood circulation and the oral administration of caltrate apparently relieves pain and TCM clinical symptoms, improves BMD in the patients of osteoporosis and achieves definite clinical efficacy in the patients of osteoporosis.
Aged ; Blood Circulation ; Bone Density ; Female ; Humans ; Male ; Middle Aged ; Moxibustion ; Osteoporosis ; physiopathology ; therapy ; Yang Deficiency ; physiopathology ; therapy
3.Residual Hearing after Cochlear Implantation in Children
Lei CAI ; Qingquan HUA ; Yongmao CAO ; Kun YANG ; Suqin ZHU ; Wei CHANG ; Jun LI
Journal of Audiology and Speech Pathology 2014;(5):510-513
Objective To study the influence of cochlear implantation on residual hearing in children .Methods Behavioral audiometry were performed pre -implant and 3~21 months post -implant on thirty -four cochlear implant recipients with severe to profound hearing loss .According to follow -up time ,they were divided into 2 groups which were Group A(3~12 months ,21 cases) and Group B(≥13 months ,13 cases) .The thresholds at 250 Hz ,500 Hz ,1 000 Hz and 2 000 Hz were analyzed .Results There were 25 out of 34 patients (73 .53% ) had partial residual hearing after cochlear implantation .Comparing to the hearing loss pre -operation and post -operation , which were most obvious at 500 Hz ,followed by 250 Hz ,1 000 Hz ,2 000 Hz (P<0 .05) ,and there were significant different among different frequencies .There was significant difference at different frequencies at hearing loss thresh-olds only in Group A .But there was no significant difference in Group B .With the prolonged time after the cochlear implantation ,residual hearing at all frequencies showed a trend of recovery .Conclusion The residual hearing could be partial preserved after cochlear implant in pediatric patients with severe to profound hearing impaired ,the residu-al hearing at lower frequencies (250 Hz ,500 Hz) were less affected than those at higher frequencies .With the pro-longed time after the cochlear implantation ,the residual hearing showed a certain degree of recovery .
5.The effects of insulin and gliclazide therapy on endoplasmic reticulum stress and insulin sensitivity in liver of type 2 diabetic rats
Weiping SUN ; Yan BI ; Hua LIANG ; Mengyin CAI ; Xiang CHEN ; Yanhua ZHU ; Lizhen LIAO ; Jianping WENG
Chinese Journal of Internal Medicine 2012;51(8):638-641
Objective To investigate the effect of insulin and gliclazide therapy on endoplasmic reticulum (ER) stress and insulin sensitivity in the liver of type 2 diabetic rats.Methods A high fat diet plus a low-dose of streptozotocin was implemented to create a type 2 diabetic rats which were randomly divided into diabetes mellitus (DM) group,insulin treatment (INS) group and gliclazide treatment (GT)group; and healthy rats were as normal control group.Diabetic rats in INS and GT groups were given neutral protamine hagedorn (NPH) insulin and gliclazide respectively for 3 weeks.Protein expression levels of immunoglobulin binding protein (Bip),spliced X-box binding protein 1 (XBP-ls),phosphorylated c-Jun on serine 73 (p-c-Jun),phosphorylated insulin receptor substrate 1 on serine 307 (p-IRS-1),and glucose-6-phosphatase (G6Pase) in liver homogenate were detected by Western blotting.Results Compared with the normal rats,Bip and XBP-Is in the DM group were up-regulated (0.28 ±0.07 vs 0.90 ±0.10 for Bip;0.41 ± 0.07 vs 0.95 ±0.07 for XBP-1 s; both P < 0.01 ) ; p-c-Jun (0.59 ± 0.18 vs 1.94 ± 0.03 ),p-IRS-1( 1.73 ± 0.18 vs 5.32 ± 0.22) and G6Pase (0.11 ± 0.01 vs 0.45 ± 0.01 ) were increased ( all P values <0.01 ).In the INS group,all of aforementioned changes were reversed (0.90 ± 0.10 vs 0.25 ± 0.04 for Bip; 0.95 ±0.07 vs 0.47 ±0.01 for XBP-1s; 1.94 ± 0.03 vs 0.50 ±0.10 for p-c-Jun; 5.32 ± 0.22 vs 1.59 ±0.32 for p-IRS-1 ; 0.45 ±0.01 vs 0.15 ±0.02 for G6Pase,all P values <0.01 ).In the GT group,all of aforementioned changes were also attenuated ( 0.90 ± 0.10 vs 0.53 ± 00.02 for Bip ; 0.95 ± 0.07 vs 0.78±0.02 for XBP-1s; 1.94 ±0.03 vs 1.33 ±0.11 for p-c-Jun; 5.32 ±0.22 vs 3.13 ±0.02 for p-IRS-1; 0.45 ± 0.01 vs 0.25 ± 0.01 for G6Pase,all P values < 0.05).Furthermore,all of aforementioned protein levels were down-regulated more obviously in the INS group comparing to the GT group ( all P values < 0.01 ).Conclusions Both insulin and gliclazide therapy could relieve ER stress and e-Jun N-terminal kinase activity and improved insulin sensitivity.The effect of insulin on Bip,XBP-1s,p-c-Jun,p-IRS-1 and G6Pase protein expressions is more obvious than that of glilcazide,which indicates besides lowering glucose,insulin might have protective effects of anti-inflammation,anti-oxidative stress or stimulation of lipid redistribution.
6.Relativity among starch quantity, polysaccharides content and total alkaloid content of Dendrobium loddigesii.
Hua ZHU ; Jianbei TENG ; Yi CAI ; Jie LIANG ; Yilin ZHU ; Tao WEI
China Journal of Chinese Materia Medica 2011;36(23):3262-3264
OBJECTIVETo find out the relativity among starch quantity, polysaccharides content and total alkaloid content of Dendrobium loddigesii.
METHODMicroscopy-counting process was applied to starch quantity statistics, sulfuric acid-anthrone colorimetry was used to assay polysaccharides content and bromocresol green colorimetry was used to assay alkaloid content. Pearson product moment correlation analysis, Kendall's rank correlation analysis and Spearman's concordance coefficient analysis were applied to study their relativity.
RESULT AND CONCLUSIONExtremely significant positive correlation was found between starch quantity and polysaccharides content, and significant negative correlation between alkaloid content and starch quantity was discovered, as well was between alkaloid content and polysaccharides content.
Alkaloids ; analysis ; Dendrobium ; chemistry ; Polysaccharides ; analysis ; Starch ; analysis
7.Discussion on twenty four moxibustion styles of Meihua acupuncture-moxibustion school.
Cheng-Gong HE ; Sheng-Chao CAI ; Hong-Hui LONG ; Wei-Hua YUAN ; Cai-Feng ZHU
Chinese Acupuncture & Moxibustion 2013;33(7):622-626
Nomination, apparatus, manipulating techniques, indications and theoretical basis of 14 single moxibustion styles including Chuijiu (insufflating moxibustion), Dianjiubi Jiu (pecking moxibustion with a pen-like stool), Jiujia Xunjiu (moxibustion with frame), Tongmai Wenyang Jiu (moxibustion for removing meridian obstructions and warming up yang), QifuJiu (moxibustion on umbilicus and abdomen), Xiongyang Jiu (moxibustion on the chest for reinforcing yang qi), Toujing Jiu (moxibustion on head and neck), Anmo Jiu (moxibustion with massage), Zhiti Jiu (moxibustion on extremities), Guan Jiu (moxibustion with a tube), Zu Jiu (moxibustion on foot), Wenzhenjiu (warm needling), Huanong Jiu (festering moxibustion) and Gewu Jiu (indirect moxibustion) are expounded in this article. And 10 compound moxibustion with the combination of 2 or more than 2 above mentioned single moxibustion style under the instruction of combination of local and distal points, combination of upper and lower points as well as combination of frontal and back points are also stated. It suggests to classify moxibustion into categories of festering moxibustion and mild moxibustion, indirect moxibustion and direct moxibustion, and to classify moxibustion apparatus into the categories of treating tools and assisting tools.
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9.Inhibition of curcumin on histone deacetylase and expression promotion of P21 (WAF1/CIP1) in HepG2 cells.
Bi-Hua LV ; Ling ZHANG ; Chang-Cai ZHU ; Jing LIU
China Journal of Chinese Materia Medica 2007;32(19):2051-2055
OBJECTIVETo investigate the effect of curcumin (Cur) on histone deacetylase (HDAC1) and P21(WAF1/CIP1), a cyclin dependent kinase inhibitor, in HepG2 cells for exploring the mechanism of Cur in anti-cancer.
METHODThe HDAC1, P21(WAF1/CIP1) proteins and P21(WAF1/CIP1) mRNA were extracted from human hepatoma cells treated with or without Cur of different concentrations at different time points. Western blot analysis was performed to determine the levels of HDAC1 and P21(WAF1/CIP1) proteins, respectively. RT-PCR was performed to detect the level of P21(WAF1/CIP1) mRNA.
RESULTThe IC50 of concentration treated by Cur was 25 micromol x L(1) on HepG2 cell. The level of HDAC1 was obviously inhibited by Cur, and decreased at 4 hours at IC, and lasted for 48 h in a time-dependent manner. The inhibition of HDAC1 was significant at the Cur concentration of 12.5 micromol x L(-1) but there was no difference between 50 and 100 micromol x L(-1). The levels of P21(WAF1/CIP1) mRNA and protein were up-regulated by Cur in dose and time-dependent manner, and the change of mRNA and protein was detected at 8 hours and lasted for 48 hours.
CONCLUSIONCur can inhibit the level of HDAC1 and enhance the expression of P21(WAF1/CIP1) protein and mRNA, and the results suggest that inhibiting HDAC1 and increasing P21(WAF1/CIP1) may be one of the possible mechanisms of anti-cancer by Cur.
Blotting, Western ; Carcinoma, Hepatocellular ; genetics ; metabolism ; pathology ; Cell Line, Tumor ; Curcuma ; chemistry ; Curcumin ; administration & dosage ; isolation & purification ; pharmacology ; Cyclin-Dependent Kinase Inhibitor p21 ; genetics ; metabolism ; Dose-Response Relationship, Drug ; Gene Expression Regulation, Neoplastic ; drug effects ; Histone Deacetylase Inhibitors ; Histone Deacetylases ; metabolism ; Humans ; Liver Neoplasms ; genetics ; metabolism ; pathology ; Plants, Medicinal ; chemistry ; RNA, Messenger ; biosynthesis ; genetics ; Reverse Transcriptase Polymerase Chain Reaction ; Time Factors
10.Residue and Degradation of Cyantraniliprole and Its Main Metabolite in Pepper and Soil
Hongmei HE ; Chunrong ZHANG ; Yahong ZHU ; Changpeng ZHANG ; Lifeng PING ; Hua ZHAO ; Min WU ; Tao TANG ; Xiaoming CAI ; Zhen LI
Chinese Journal of Analytical Chemistry 2014;(8):1178-1183
An analytical method based on ultra performance liquid chromatography-tandem mass spectrometry was developed for the determination of cyantraniliprole and its main metabolite J9 Z38 residues in pepper and soil. The fate of cyantraniliprole and J9Z38 in pepper and soil was also evaluated. The target compounds were extracted with acetonitrile, cleaned up by C18 cartridge, and further analyzed by gradient ultra performance liquid chromatography-tandem mass spectrometry with electrospray ionization in positive mode ( ESI﹢) using a UPLC BEH C18 Column. The method was validated using fortified pepper and soil. Intra-day mean recoveries of cyantraniliprole and J9Z38 at three spiked levels (0. 01, 0. 10 and 1. 00 mg/kg) ranged from 88. 6% to 105 . 7% with relative standard deviations of 3 . 8%-15 . 1%. Inter-day mean recoveries of cyantraniliprole and J9 Z38 were found between 91 . 4% and 105 . 3% with relative standard deviations of 4 . 9%-12 . 3% at three spiked levels. Limits of quantification ( LOQs) of cyantraniliprole and J9Z38 were 0. 1 and 0. 2 μg/kg, respectively. Linear calibration functions with correlation coefficients of r>0. 9992 were obtained in the concentration range of 2. 0-128. 0 μg/L. This method was applied to the analysis of cyantraniliprole and J9Z38 residues in real pepper and soil samples selected from field. The results of the residue dynamic experiment showed that the half-life of cyantraniliprole ranged from 9 . 2 to 11 . 2 days in pepper and from 9 . 2 to 20. 8 days in soil. While, the residues of J9Z38 in pepper were below LOQ, and the half-life of J9Z38 in soil was 9. 4 days. The degradation speed of cyantraniliprole increased with the increase of the precipitation.