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<p><b>BACKGROUND</b>Recent studies have shown the LyP-1 peptide can home to either tumor lymphatics or the tumor cells and be internalized by targeted cells. This study aimed to investigate the possibility of using Na(131)I labeled LyP-1 peptide as an imaging agent or a therapeutic radiopharmaceutical in breast carcinoma and its metastasis.</p><p><b>METHODS</b>The 10-mer cyclic peptide contained the LyP-1 sequence (YCGNKRTRGC) was synthesized by the solid phase method. Disulfide bonds between the cysteines maintain the cyclic structure. The LyP-1 peptide was labeled with Na(131)I using the chloramine-T method. The [(131)I] LyP-1 peptide and a [(131)I] control peptide were injected via tail vein into nude mice bearing MDA-MB-435 tumor xenografts. Biodistribution and imaging results in vivo were obtained.</p><p><b>RESULTS</b>The labeling efficiencies of LyP-1 peptide reached 80% ± 5% (n = 5). The radiochemical purity was about 96%. The radiochemical purity of the labeled compound remains 92% at 24 hours in human serum at 37°C. In the biodistribution studies, the [(131)I] LyP-1 peptide accumulated in the tumor to a higher level than in other organs. The [(131)I] LyP-1 peptide can successfully image the tumor in nude mice bearing MDA-MB-435 tumor xenografts.</p><p><b>CONCLUSIONS</b>The LyP-1 peptide could be effectively labeled with Na(131)I and the labeled compound is stable in human serum at 37°C for 24 hours. The high specificity of [(131)I] LyP-1 peptide suggests it may be a promising new radiotracer for identifying tumors.</p>
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Animals , Female , Humans , Mice , Breast Neoplasms , Diagnosis , Cell Line, Tumor , Heterografts , Mice, Nude , Peptides, Cyclic , Chemistry , Tomography, Emission-Computed, Single-PhotonABSTRACT
Objective To evaluate the efficacy and safety of diacerhein in the treatment of patients with knee osteoarthritis.Methods The efficacy and safety of diacerhein was randomly investigated in 42 pa- tients with knee osteoarthritis using parallel group methodology and a double-dummy technique to ensure dou- ble blind status with respect to diacerhein and control drugs diclofenac.Results Significant changes were ob- served in 20 meters walk pain,knee joint tenderness scale,WOMAC index scale,5F-36 health survey,knee joint swelling scale,compared with baseline(P＞0.05)in both diacerhein and diclofenac group respectively.No difference was found between diacerhein group and diclofenae group.The patient global assessment and physi- cian's global assessment were similar in diacerhein group and diclofenac group(P＞0.05).The side effect was similar in two groups.All of these side effects in gastrointestinal tract appeared to be transient.Conclusion Diacerhein can effectively relieve pain and swelling of knee osteoarthritis,and provides us a new effective and safe approach for treating knee osteoarthritis.
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Objective To study the risk of tuberculosis (TB) infection in rheumatoid arthritis (RA) and ankylosing spondylitis (AS) patients before and after treated with tumor necrosis factor (TNF) antago- nists.Methods RA and AS patients treated with TNF antagonists infliximab and etanercept between 2003 and 2006 were followed up for the risk of TB infection.The protein purified derivative (PPD) test and chest anteroposterior and lateral view X-ray were done at screening for all these patients.Results Among 67 RA patients screened,1 was PPD positive.One patient developed right supraclavicular lymph node TB 4 months after study completion.Among 203 AS patients screened,27 patients were PPD positive,2 had calcified pul- monary TB foci and 2 had pulmonary TB.PPD positive rates and calcified TB foci or active TB found in RA and AS patients screened were significantly lower than national TB infection rates and prevalence (P＜0.01). Conclusion In this short-term clinical observation,increased risk of TB infection was not found after TNF antagonists treatment in RA and AS patients.However,it is necessary to screen patients for signs of TB infec- tion before TNF antagonists treatment.
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Objective To analysis the quality of life of patients with active ankylosing spondylitis (AS).Methods The quality of life was assessed in 52 patients with active AS using SF-36 and was compared with the general population.The correlation between the quality of life and the clinical measures of disease,in- cluding the Bath AS disease activity index(BASDAI),Bath AS functional index(BASFI),Bath AS metrology index(BASMI),patient's global assessment(PGA),spinal inflammation,total back pain,nocturnal back pain, and enthesis index(EI),were determined.Results The patients with active AS reported significant decreased scores on all dimensions of SF-36.The score of physical health components was poorer than that of mental health components.BASFI was the strongest factor correlated with the score of SF-36,followed by BASDAI and PGA.BASMI and total back pain were correlated with three dimensions only.In multivariate regression analysis,BASFI showed relative closer relationship to the qulity of life with active AS than other clinical mea- sures of disease and it accounted for 50.3%,35.2% and 47.9% of the variance in the physical health compo- nents,the mental health components and the overall score of SF-36,respectively.Conclusion The quality of life in patients with active AS is significantly declined compared with general population.The physical aspects seem to be more severely affected.Functional status of the patients with active AS are correlated with the quality of life closely.
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0.05).In addition,in different medication intervals and the same total dosage(200 mg),there was no difference in the number of patients who reached ASAS20,ASAS50 anti BASDAI50 in both groups.The changes of other parameters were not observed.Conclusion Two dosages and different medication interval of rhTNFR-Fc have similiar efficacy onset time and maintenee period.Mean- while,at the same total dosage,there is no signifieant difference in therapeutic effect in the two dosage groups. However,50 mg(1/7 d)regimen has better compliance than 25 mg(1/3 d).
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Objective To investigate the role of CD4~+CD25~+ Treg cells on the pathogenesis of ankylos- ing spondylitis(AS), and to study the machanism of tumor necrosis factor(TNF)-?blocker on the treatment of AS by detecting the number of CD4~+D25~+ Treg cells before and after the treatment. Methods The diagno- sis of 10 AS patients was made based on the 1984 modified New York criteria. The patients received subcuta- neou injection of recombinant human tumor necrosis factor receptor-Fc fusion protein(rhTNFR-Fc)(etaner- cept)50 mg weekly for 8 weeks and 10 heathy subjects were enrolled for control. The mononuclear cells were isolated from peripheral blood in beth patients and controls. The number of CD4~+CD25~+ T cells and CD4~+ CD25~(high)T cells and the expression of CTLA-4. were detected by flow cytometry. Results The proportion of CD4~+CD25~+ T cells(24?19)% in total CD4~+ T lymphocytes of peripheral blood and CD4~+CD25~(high)T/CD4~+ T (6?6)% from AS patients before treated with rhTNFR-Fc was higher than that in healthy volunteers and AS patients after treatment(P