1.Preparation and bioevaluation of 111 In-DTPA-avastin for non-invasive tumor targeted imaging
Hua ZHU ; Jinming ZHANG ; Fei LIU ; Xuedi HAN ; Zhi YANG
Chinese Journal of Nuclear Medicine and Molecular Imaging 2017;37(1):5-9
Objective To label human VEGF targeted bevacizumab (avastin) with 111In and to evaluate the application of 111 In?DTPA?avastin SPECT imaging for tumor diagnosis. Methods DTPA?avastin was prepared by coupling with a bifunctional chelating agent, and then labeled with 111 In to obtain 111 In?DTPA?avastin. The stability and molecular integrity of the labeled radiotracer were studied. Human hepatoma cell ( BEL7404) bearing nude mice tumor model was employed for tumor targeting evaluation. Gamma imaging was acquired after intravenous injection of 18.5 MBq probe. At the end of the observation, animals were sac?rificed for bio?distribution study. Results 111 In?DTPA?avastin tracer was synthesized and purified to a?chieve a radiochemical purity yield above 98% and specific activity up to 185 GBq/nmol. Its stability in 5%BSA was optimal, and the radiochemical purity after incubation for 96 h was over 90%. Gamma imaging re?sults showed that the tracer possessed definite tumor targeting property. Its biodistribution was consistent with that of normal in vivo antibody metabolism while possessing a good tumor?targeting property with a relatively high uptake of (3.8±0.8) %ID/g in tumor tissues 96 h after injection. Conclusions 111 In?DTPA?avastin tracer has good physicochemical properties, in vivo stability and good VEGF targeted binding. 111 In?DTPA?avastin has potential to be a new molecular probe for SPECT imaging.
2.Literature review on premarketing and postmarketing evidence of xiyanping injection.
Zhi-Fei WANG ; Xiao CHEN ; Wen ZHANG ; Yan-Ming XIE
China Journal of Chinese Materia Medica 2014;39(18):3637-3640
This article systematically summarizes the non-clinical safety studies, pharmacological studies and postmarketing safety studies of Xiyanping injection based on literature. These studies include acute toxicity test, long-term toxicity test, reproductive toxicity test, active and passive anaphylaxis test, curative mechanism study, clinical trials of effectiveness, active surveillance, security analysis of passive monitoring data, the real world analysis of hospital information system (HIS) data, literature analysis, etcetera This article also analysis the relationship of the different evidence, summarizes the strategy of the researches, in order to make it to be a reference for making a systemic research program of traditional Chinese medicine injection.
Drugs, Chinese Herbal
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administration & dosage
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adverse effects
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Injections
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Medicine, Chinese Traditional
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methods
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Product Surveillance, Postmarketing
3.Analysis of influencing factors on adverse reaction of Shengfu injection based on prospective active safety monitoring.
Zhi-fei WANG ; Wei ZHAO ; Yin ZHANG ; Yan-ming XIE
China Journal of Chinese Materia Medica 2015;40(24):4746-4751
This study collected demographic data, past history, personal history, family history, dosage, solvent, combined medication information of adverse reaction cases from a prospective, multi center, large sample intensive hospital monitoring, and found the influencing factors with cross-tab analysis. The results showed that in the medication group of 19-45, patients with allergic histories had a higher proportion in ADR; in the medication group of 46-65, male patients with allergic histories had a higher proportion in ADR; indication and non-indication group, patients of 19-45 years old, with combined medications and allergy histories had a higher proportion in ADR; Non-indication medication group, patients with combined medication, higher concentration, out-instruction solvent and dosage, had a higher proportion in ADR. So, the ADRs of Shenfu injection were related to the history of drug allergy, and also related to the indication, dosage, solvent, concentration when it was used.
Adult
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Aged
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Drug Hypersensitivity
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etiology
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Drugs, Chinese Herbal
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adverse effects
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Female
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Humans
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Injections
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Male
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Middle Aged
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Prospective Studies
4.Expression of osteopontin in different metastatic potential uveal melanoma and its significance
Xu, ZHANG ; Xiao-lin, XU ; Bin, LI ; Fei, GAO ; Zhi-bao, ZHANG ; Liang, LI
Chinese Journal of Experimental Ophthalmology 2012;30(3):199-203
BackgroundOsteopontin is highly expressed in many metastatic tumors,but its expression in uveal melanoma and the relationship of osteopontin with metastasis is still under investigation.Objective This study was to investigate the relationship between osteopontin expression and uveal melanoma metastatic potential.Methods Fifty samples of uveal melanoma were collected in Beijing Tongren Hospital.The expressions of osteopontin in the samples were detected using immunohistochemistry,and expressions of osteopontin mRNA in different metastatic potential uveal melanoma cell lines (MU M-2B,C918,OCM-1A) were analyzed using quantitative polymerase chain reaction (Q-PCR).ResultsOsteopontin was positively expressed in 10 samples of 13 patients with metastasis and 14 samples of 37 patients without metastasis,showing a significant difference between them (x2=5.888,P=0.000).There were 11 samples and 13 samples exhibiting the positive expression of osteopontin in 15 epithelial type and 35 non-epithelial type of uveal melanoma respectively with the significant difference (x2=5.510,P =0.000).The positive expressing numbers of osteopontin were 20 tumors of 30 affected tumors and 4 tumors of 20unaffected ciliary tumors with the significant difference (x2 =10.470,P =0.000 ).No significant differences in the expression of osteopontige were found between different gender,age,eyes,largest basal diameters and invasion of scleral canal( P =0.536,0.256,0.802,0.848,0.555 ).The relative expression value of osteopontin mRNA was in turn 1.00±0.04,0.91 ±0.03,0.08±0.01 in MUM-2B,C918,OCM-1A with the significant difference among three cell lines( F=33.135,P<0.05).The osteopontige mRNA expression was significant enhanced in high metastatic potentialcell lines( MUM-2B,C918 ) compared with low metastatic potential cell lines( OCM-1 A) (P<0.05 ),but no significant difference was seen between two high metastatic potential cell lines(MUM-2B,C918) (P=0.804).Conclusions Osteopontige expression is associated with the uveal melanoma cell line invasion and metastasis potential.These results imply that osteopontige expression maybe an indicator of uveal melanoma invasion and metastasis ability.
5.Chemical constituents from a Tibetan medicine Meconopsis horridula.
Zhi-Qin GUO ; Qiang GUO ; Zhi-Xiang ZHU ; Shui-Ying ZHANG ; Chun LI ; Xing-Yun CHAI ; Peng-Fei TU
China Journal of Chinese Materia Medica 2014;39(7):1152-1156
A phytochemical investigation on the aerial parts of a Tibetan medicine Meconopsis horridula, by solvent extraction, repeated chromatographies on silica gel, Sephadex LH-20, and preparative TLC techniques, led to the isolation of 9 compounds. By spectroscopic analysis and comparison of its 1H and 13C-NMR data with those in literatures, their structures were identified as oleracein E(1), N-( trans-p-coumaroyl) tyramine (2), chrysoeriol (3), apigenin (4), hydnocarpin (5), p-coumaric acid glucosyl ester (6), stigmast-5-ene-3beta-ylformate (7), 3beta-hydroxy-7alpha-ethoxy-24beta-ethylcholest-5-ene (8), and beta-sitosterol (9), respectively, among which compounds 6-8 were isolated from the genus for the first time,and 1,3 were isolated from the species for the first time. A MTT method was applied to evaluate the cytotoxic activity of compounds 14 against the human hepatocellular liver carcinoma cell line (HepG2), and compound 1 showed significant cytotoxicity against HepG2,with its inhibitory rate of 52.2% at 10 micromol x L(-1).
Medicine, Tibetan Traditional
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Molecular Structure
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Papaveraceae
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chemistry
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Plant Extracts
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chemistry
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Spectrometry, Mass, Electrospray Ionization
6.Seroepidemiological survey of F1 antibody of indicator animals in wild rodents loci of plague in YunnanProvince
Yun, LIANG ; Zhi-zhong, SONG ; Ying, GUO ; Zhi-ming, YANG ; WUAIGUO ; Fu-xin, ZHANG ; Zheng-fei, ZHANG ; Ying-tian, HE ; Wei, HE ; Zhi-jun, CHENG
Chinese Journal of Endemiology 2008;27(6):644-646
Objective To study on the effect of indicator animals in plague surveillance throngh detecting F1 antibody against Yersiniapestis(Y.pestis)in indicator animals in wild rat plague foci,provide scientific evidence for plague control and determining the range of epidemic area.Methods According to investigation scheme of wild rodents plagne foci in Yunnan Province,indicator animals Canis familiarils and Felis catu(C.familiarils and F.catus)related to the plague were investigated in 75 villages,14 township and 10 counties around Yulong County,and living rodents were captured by cage,sera of indicator animals and rodents relevant to plague were simultaneously collected and detected for F1 antibody against Y.pestis using indirect hemagglutination(IHA).Results Seropositivity rate of indicator animals were 6.76%(202/2987),being 24.69% in C.familiaris and 24.69% in F.catus,there were statistical significance(X2=87.32,P<0.01)between C familiaris and F catus,the latter beingmore than the former.But F1 antibody of rodents sera were not detected,its seropositivity rate was zero.there was a statistical significance(P<0.01)between indicator animals and rodents.Conclusions Through serocpidemiological survey of indicator animals,new wild rat plague natural focus has been confirmed in YuLong County and Gucheng District in LiJiang City,therefore,serocpidemiological surveillance of indicator animals is very important for plague control and prevention.
7.A Study in Construction of Short Hairpin Small Interfering RNA Expression Vector Target Lectin Like Oxidized Low Density Lipoprotein Receptor-1 Gene and Its Effect on Foam Cells
Hui-Yu YANG ; Yun-Fei BIAN ; Zhi-Ming YANG ; Na-Na ZHANG ; Chuan-Shi XIAO ;
China Biotechnology 2006;0(10):-
Aim:To construct the short hairpin small interfering RNA(shRNA) eukaryotic expression vector specific to mouse lectin like oxidized low density lipoprotein receptor 1(LOX-1) gene and to observe its silencing effect on LOX-1 in RAW264.7 cells.Methods:(1)The pLOX-1-shRNA expression vector was constructed by gene recombination,Then transfected into the cultured RAW264.7 cells.At 48 h after Transfection,the expression of LOX-1 mRNA in RAW264.7 cells were determined by semi-quantitative RT-PCR,the expression of LOX-1 proteins examined by Western blot.(2) Oil Red O Dyeing experiment was used to show the cellular lipid droplets in lipid-loaded cells.The method of cholesterol oxidase analysis was performed to determine the content of cellular cholesterol.The ability of uptake Dil-ox-LDL in RAW264.7 cells was assayed by fluorescence microscopy.Results: pLOX-1-shRNA expression vector was successfully constructed.Transfection of pLOX-1-shRNA expression vector into RAW264.7 cells down regulaled the expression level of LOX-1 gene,as compared with the control group,transfection of the RAW264.7 cells with LOX 1-shRNA led to a remarkable reduction of the number macrophages transformed into foam cell,and could suppress the uptake of ox-LDL.Conclusion:The pLOX-1-shRNA expression vector can inhibit the expression of LOX 1 in RAW264.7 cells and the transformation of the macrophages into foam,which may he beneficial in searching new gene therapy of atherosclerosis.
8.The clinical observation of oxaliplatin combined with capecitabin for patients with advanced colorectal cancer
Xin-Jian RUAN ; Jian-Fei WANG ; Zhi GUO ; Zhao-Liang CHEN ; Xia ZHANG ;
Cancer Research and Clinic 2000;0(06):-
Objective To observe the therapeutic effect and toxicity reaction of Oxaliplatin com- bined with XeLoda in the treatment of 42 patients with advanced colorectal cancer.Methods All the pa- tients were treated with Oxaliplatin(130 mg/m~2,ivgtt for 2 h,d1)combined with XeLoda(2000 mg?m~(-2)?d~(-1), po,bid,d1 to d14).The regime was repeated every 21 days for at least 3 consecutive cycles.Results The to- tal response rate was 40.5%(17/42)in which 2 got CR and 15 PR.24 patients got Kamofsky score increased. The major toxic effects were alopecia,peripheral neuritis,gastrointestinal tract reactions and myelosuppression. Conclusion Oxaliplatin combined with XeLoda regimen is effective in the treatment of advanced colorectal cancer,and its toxicity is tolerable.It is worth studying in the future.
9.Changes of P-glycoprotein and nuclear factor κB in the cerebral cortex of rat with chronic fluorosis
Kai-lin, ZHANG ; Di-dong, LOU ; Yan-fei, LIU ; Shuang-li, QIN ; Zhi-zhong, GUAN
Chinese Journal of Endemiology 2012;31(6):613-616
Objective The aim of the study was to investigate the expression of P-glycoprotein (P-gp)and nuclear factor κB (NF-κB) in the cerebral cortex of rat with chronic fluorosis,and to reveal the mechanisms of damaged nervous system resulted from the toxicity of fluoride.Methods Sixty SD rats were randomly divided into three groups.The rats in each group were given drinking water containing different levels of fluoride:control group less than 0.5 mg/L,small amount of fluoride exposure group 10.0 mg/L and large amount of fluoride exposure group 50.0 mg/L.The animals were examined at the sixth month after initiating the experiment.Protein levels of P-gp and NF-κB in brain tissues were detected by immunocytochemistry and Western blotting,and the P-gp protein and mRNA level by quantitative real time PCR method.Results As compared to the control group(28.21 ±6.13),the numbers of positive staining cells by P-gp antibody in the cortex of rat brains were significantly increased in both the small and the large amount of fluoride exposure groups[(48.46 ± 8.00),(53.72 ± 9.15),respectively,all P < 0.05] ; the protein levels in the control group(100.00 ± 3.86)% detected by Western blotting were significantly increased in the cortex of rat brains treated with fluoride in both the small and the large amount of fluoride exposure groups[(189.47 ± 3.14)%,(191.36 ± 11.09)%,respectively,all P < 0.05].The significantly increased expression of NF-κB at the protein level was observed in the cortex of rat brains of the small and the large amount of fluoride exposure groups[(365.97 ± 6.04)% and (417.15 ± 10.89)%,respectively] as compared with the control group[(100.00 ± 10.07)%,all P < 0.05].The mRMA level of P-gp in the cortex of rat brains of the small and the large amount of fluoride exposure groups(2396 ± 427,3479 ± 371,respectively) were higher than that of the control group(260 ± 106,all P < 0.05).Conclusion The increased expressions of P-gp and NF-κB in the cortex of rat brains are induced by chronic fluorosis,which might be connected with the mechanism of brain damages.
10.Changes of reactive oxygen species level and mitochondria fission-fusion hi cortical neurons of rats with chronic fluorosis
Di-dong, LOU ; Yan-fei, LIU ; Kai-lin, ZHANG ; Yan-ni, YU ; Zhi-zhong, GUAN
Chinese Journal of Endemiology 2011;30(3):256-260
Objective To investigate the changes of reactive oxygen species(ROS) level and mitochondria fission-fusion-balance in cortical neurons of rats with chronic fluorosis and reveal the correlation between these two factors. Methods One hundred and twenty rats were randomly divided into 3 groups(control group, low-dose fluorosis group, high-dose fluorosis group) and 40 rats were in each group according to body weight and the experiments were carried out for 3 months or 6 months. The rats were fed with different concentrations of fluoride (NaF) to establish fluorosis models. Controls were fed with tap water( < 0.5 mg/L), experimental animals in low- or high-dose group were fed with water containing NaF 10.0,50.0 mg/L, respectively. The level of ROS and the morphology in mitochondria fission-fusion balance in neurons of the cortex of rat brains prepared with cortical frozen sections were detected with ROS fluorescent probe and MitoTracker RED probe, respectively. Results Significant differences of the level of ROS and the numbers of abnormal mitochondria in morphology in the cortical neurons were found between 3 groups at the experiment period of 3 month and 6 month(F= 3.07,3.06,3.05,3.07, all P < 0.05). As compared with control group(10.43 ± 5.98,4.12 ± 3.86) at the experiment period of 3 month, the level of ROS and the numbers of abnormal mitochondria in morphology in the cortical neurons were obviously increased in high-dose fluorosis group(25.48 ± 6.09,20.47 ± 6.09, all P < 0.05), whereas no significant changes were found in low-dose fluorosis group(11.67 ± 3.49,6.68 ± 3.48, all P> 0.05). Furthermore, the increases in both ROS level and abnormal numbers of mitochondria were significant observed in the cortical neurons of low-dose fluorosis group (63.02 ± 8.15, 49.33 ± 8.61) and high-dose fluorosis group(65.60 ± 7.40,53.10 ± 6.95) as compared with the control group (25.26 ± 6.41,20.26 ± 6.41) at the experimental period of 6 month (all P < 0.05). The abnormal numbers of mitochondria correlated with ROS level(r = 0.93,0.81, all P < 0.05). Conclusions Taking excessive amount of fluoride results in high level of oxidative stress and impaired the balance of mitochondrial fission-fusion,which is dependent on the feeding times and doses of fluoride. The mechanism of the mitochondrial abnormalities might be associated with the high level of oxidative stress induced by chronic fluorosis.