Objective To investigate the biodistribution,excretion and other pharmacokinetics,of 188Re-1-hydroxy-1,1-ethylidene disodium phosphonate (HEDP) in cancer patients with osseous metastases who were suffering form bone pain. Methods A single dose (20,30,40,and 50 MBq/kg,10 patients in every group) of 188Re-HEDP was administered as a bolus injection,meanwhile dynamic images on patient's chest were collected for 30 min. Anterior and posterior whole-body images were obtained at 1,2,4,5,12,24,36,48,60 and 72 h after injection of 188Re-HEDP. By region of interest (ROI) technology,the curve of time-background corrected counts of left cardiac ventricle could be generated,and the background-corrected counts of various organs and total whole body could be calculated as a geometric mean using the anterior and posterior scans,and transformed to the percentage injected dose ( % ID). Urine was collected after injection of 188Re-HEDP. Counts of urine were measured by γ counter. Analysis of variance and t-test were used. Results Linear relationship of metabolism of 188Re-HEDP was observed in the doses from 20 to 50 MBq/kg,with correlation coefficient r2 = 0. 9376. A two-compartment model was the best fit for metabolism of 188Re-HEDP with the parameters median area under curve (AUC) 3.32 × 105,3.97 × 105,7.83 × 105,8.58 ×105,respectively; median α 0.06,0.05,0.04,0.06 respectively; median β 1.16 ×10-3,1.16 × 10-3,1.03 × 10-3,1.15 × 10 -3 respectively; median A 3591.21,4858.23,5642. 48,4167.05 respectively; median B 293.97,352.95,614.41,1063.82 respectively; median T1/2(α) 12.51,12.83,15.41,12.02 min respectively; median T1/2(β) 595.47,596.50,673.09,600.93 min respectively in the doses of 20,30,40and 50 MBq/kg. 188Re-HEDP was taken up mainly by bone up to 40% ID at 4 h. Urine profile showed that 66.79 % ID was eliminated within 24 h,being its 74% collected along the first 5 h after-administration.Conclusions In the doses of 20,30,40 and 50 MBq/kg,metabolism of 188Re-HEDP presented linear model. Pharmacokinetics of 188 Re-HEDP followed a two-compartment model administrated by blood vessel.Following injection,188 Re-HEDP was taken up mainly by bone and excreted by uropoietic system.

Adult ; Female ; Humans ; Middle Aged ; Thyroid Diseases ; microbiology ; Tuberculosis, Endocrine

Objective To evaluate the safety and feasibility of totally thoracoscopic anatomic pulmonary segmentectomy (TTAS) for the treatment of the peripheral stage ⅠA non small cell lung cancer(NSCLC).Methods The study involved 50 consecutive patients undergoing totally thoracoscopic anatomic segmentectomy (TTAS) from September 2010 to November 2012 in the First People's Hospital affiliatied to Nanjing Medical University.The diameter of the tumors were less than 2 cm [(mean diameter(1.35 ±0.48) cm].All lymph node sampling of N1 and N2 were neglive,All patients received symtematic lymph node dissection.The pulmonary vessels were individually ligated,and the bronchi were closed using an endoscopic stapler.The intersegmental plane was identified using the demarcation between the resected(inflated) and preserved(collapsed) lungs.Staplers were used for intersegmental dissection.Results The mean operative time and intraoperative bleeding were (191.5 ± 50.4) min and (49.2 ± 54.6) ml respectively.The chest tube drainage duration was (3 ± 1) days.The number of stapler cartridges used for intersegmental division was 3.9 ±0.8.The mean number of lymph nodes and nodal stations dissected were 12.6 ± 2.8 and 6.0 ± 1.5 respectively.No mortality and complications were observed 30 days after the surgery.Further,no local recurrence or metastases were observed during follow-up.Conclusion Totally thoracoscopic anatomic segmentectomy(TTAS) is a feasible and safe technique.With systematic lymph node dissection,TTAS can be a reasonable therapeutic option for stage ⅠA NSCLC.

OBJECTIVE: To study the effect of various polarity fractions extracted from Sancaofang (SCF) and its combination on proliferation of human lung adenocarciaoma SPC-A-1 cells for bolting the most effective position of anti-tumor and suitable compatibility regimes.METHODS: Ethanol extraction and water extraction were adopted to prepare 95%,60% and 30% ethanol extract portion,water extract portion of SCF and compound decoction.The MTT assay was used to determine the effect of various polarity fractions of SCF,decoction and its combination on SPC-A-1 cells proliferation.RESULTS: IC50 of 60% ethanol extract was the smallest for SPC-A-1 cells.60% ethanol extract combined with 95% ethanol extract acts as a stimulus to anti-tumor activity significantly.CONCLUSION: The best suitable compatibility regimes were 95% ethanol extract combined with 60% ethanol extract.The liposolubility extract of SCF can be applied for anti-tumor.

Objective To explore the effects of bilirubin on myeloid differentiation factor 88 (MyD88)and interleukin-1 receptor associated kinase-4(IRAK-4).Methods Seven-day-old Sprague Daw-ley rats (clean grade),male or female,weighing 12.0 to 15.0 g,were randomly assigned to 6 groups.There were normal saline group(Ⅰ),lipopolysaccharide(LPS)control group (LPS,Ⅱ),15 mg /kg bilirubin con-trol (free-LPS)group (Ⅲ),15 mg /kg group (Ⅳa),30 mg /kg group (Ⅳb)and 50 mg /kg group (Ⅳc), and then subsequently divided into 2 h,5 h and 24 h subgroups in each groups.Some of the 200 newborn rats died amid the experiment.Finally a total of 144 were involved in the analysis of results,and 8 rats in each subgroups.Newborn Sprague Dawley rats were administered at various doses of bilirubin (15 mg /kg, 30 mg /kg and 50 mg /kg respectively)intravenously;1 h after injection,the rats were administered LPS intrap-eritoneally at a dose of 1 mg /kg;MyD88 and IRAK-4 were detected by immunohistochemistry at 2 h,5 h and 24 h after the injection of bilirubin.Results (1 )LPS could stimulate the expression of MyD88 and IRAK-4 in spleen cells (qMyD88 2 h =49.89,qMyD88 5 h =139.54,qIRAK-4 2 h =7.93,qIRAK-4 5 h =24.30,qIRAK-4 24 h =6.97 ,P <0.01 ).(2)Low concentration of bilirubin could promote the expression of MyD88 and inhibit the ex-pression of IRAK-4 (qMyD88 2 h =0.76,qMyD88 5 h =5.05,qIRAK-4 2 h =6.43,qIRAK-4 5 h =22.37,qIRAK-4 24 h =1.50, P <0.01 ).(3)LPS stimulation MyD88 affected by low concentration of bilirubin was not obvious (q2 h =1.48,q5 h =1.45,q24 h =0.10,P >0.05).Effects of medium and high concentration of bilirubin on LPS stim-ulation MyD88 were inhibitory(qⅣb 2 h =42.87,qⅣc 2 h =51.38,qⅣb 5 h =103.61 ,qⅣc 5 h =1 15.44,qⅣb 24 h =1.18,qⅣc 24 h =1 1.66,P <0.01 ).(4)Effects of low,medium and high concentration of bilirubin on LPS stimulation IRAK-4 were inhibitory(qⅣa 2 h =9.52,qⅣb 2 h =14.39,qⅣc 2 h =25.55,qⅣa 5 h =38.83,qⅣb 5 h =54.62,qⅣc 5 h =60.51 ,qⅣa 24 h =2.41 ,qⅣb 24 h =1.47,qⅣc 24 h =7.61 ,P <0.01 ).(5)The inhibition of biliru-bin to MyD88 and IRAK-4 was observed at 2 h,strengthened at 5 h,disappeared at 24 h in low-mid concen-trations of bilirubin(P <0.01 )while still visible at 24 h in high concentration of bilirubin.(6)There was neg-atively correlation between the expression level of MyD88,IRAK-4 and bilirubin concentration(rsMyD88 2 h =-0.86, rsMyD88 5 h =-0.92,rsMyD88 24 h =-0.53,rsIRAK-4 2 h =-0.82,rsIRAK-4 5 h =-0.86,rsIRAK-4 24 h =-0.57,P <0.01).(7) Under the effect of bilirubin and LPS,there were positively correlation between the expression levels of MyD88 and IRAK-4 of spleen cells(r2 h =0.77,r5 h =0.9,r24 h =0.67,P <0.01).Conclusion Bilirubin could inhibit the expression of MyD88 and IRAK-4.As the concentration of bilirubin increasing,its inhibition is more obvious and prolonged.The mechanism that bilirubin affects immune function of newborn rat may be related to regulation of expression of MyD88 and IRAK-4 at toll-like receptor 4 signal pathway.

Objective To study the tolerance to 188Re-1-hydroxy-1 ,1-ethylidene disodium phosphonate(HEDP) in patients with bone pain caused by osseous metastases. Methods Thirty-one patients(10with prostate cancer, 9 with breast cancer, 3 with lung cancer, 5 with liver cancer, 2 with rectal cancer, 1with esophageal cancer and 1 with renal cancer) received a single injection dose of 188Re-HEDP. The patients were divided into four groups according to the injection dose: 20 MBq/kg (6 patients), 30 MBq/kg(6 patients), 40 MBq/kg (9 patients), and 50 MBq/kg (10 patients). Haematological toxicity (WHO grading) of grade Ⅲ- Ⅳ was considered unacceptable. Vital signs and adverse effects after injection were recorded for 8 weeks. Blood counts were measured weekly during a period of 8 weeks. Biochemical parameters and electrocardiogram were assayed at week 4 and 8. Statistical analysis was performed for per-protocol (pp) population (t-test). Results Twenty-seven patients belonged to PP population with 5 in the group of 20 MBq/kg, 5 in the group of 30 MBq/kg, 8 in the group of 40 MBq/kg and 9 in the group of 50 MBq/kg.No obvious adverse effects and no significant change of vital signs, electrocardiogram, liver and renal function were found after injection. Alkaline phosphatase was slightly higher than baseline at week 4 and 8 after therapy, but the difference was not statistically significant. In the 20 MBq/kg group, reversible grade Ⅰ leucopenia was noted in 1 patient. In the 30 MBq/kg group, 2 patients showed reversible grade Ⅰ leucopenia including 1 alone with reversible grade Ⅲ thrombopenia. In the 40 MBq/kg group, reversible grade Ⅰ leucopenia and thrombopenia was observed in 1 patient and reversible grade Ⅱ leucopenia and thrombopenia in another patient. In the .50 MBq/kg group, 3 patients showed reversible grade Ⅱ leucopenia. The lowest level of thrombopenia was at week 4(143.5 × 109/L), leucopenia at week 6 (5.4 × 109/L) and anaemia at week 8(t = 3.1325, 3.3156, 3.4917, all P ＜ 0. 05 compared with baseline). At week 8, the mean level of platelet and leucocyte recovered to baseline. "Bounce pain" was found in 2 of 27 patients (7.41%).Conclusions The dose of 20 MBq/kg, 30 MBq/kg, 40 MBq/kg or 50 MBq/kg of 188Re-HEDP do not cause significant side effects on cancer patients with bone metastases, though there is a tendency that the haematological toxicity may increase as the dose of 188Re-HEDP increases.

Objective To probe into the clinical curative effect of laparoscopic high ligation of spermatic vein in the treatment of critical varicocele.Methods The clinical data of the 26 eases of laparoscopic high ligation of apermatic vein in the treatment of critical varicocde were reviewed and analyzed in the last two years in this hospi- tal.Results All the 26 cases had been conducted smoothly with the operation time 25～50min,an average of(28?3)min.After 3～24 months being followed-up,all the symptoms and signs disappeared with no relapse and testicle a- trophy.Eight wives of the patients who had been operated on got pregnant.Conclusion With soon recovery and small wound,it was safe to adopt laparoscopic high ligation of spermatic vein in the treatment of critical varicocele, especially for critical two-sided varicocde.

OBJECTIVETo study the efficacy of Xiaoyao Powder (XYP) combined with interferon alpha (IFN-alpha) in treating HBeAg positive chronic hepatitis B (CHB) patients and the effect on their quality of life (QOL).

METHODSTotally 193 patients with HBeAg-positive CHB confirmed by liver biopsy were randomly assigned to 2 groups, Group A (94 cases) and Group B (99 cases). IFN-alpha1b was subcutaneously injected to patients in Group A at the dose of 50 microg, thrice per week. Those in Group B additionally took XYP. The therapeutic course for all was 24 weeks. Clinical efficacy was observed by assessing ALT restoration rate, HBeAg negative rate, HBeAg conversion rate, HBV DNA negative rate, complete response rate, partial response rate, and symptoms integral. The evaluation of QOL was performed by using chronic liver disease questionnaire (CLDQ) score. Adverse reaction occurrence rate was observed in the two groups.

RESULTSBetter effects were obtained in Group A on ALT restoration rate, HBeAg negative rate, HBV DNA negative rate, complete response rate, partial response rate, TCM symptoms integral, the total effective rate of TCM sysmptoms, CLDQ score, and adverse reaction rates, showing statistical difference when compared with Group B (P < 0.05, P < 0.01).

CONCLUSIONXYP could elevate the efficacy of TCM symptoms of HBeAg-positive CHB patients and anti-viral effect, improve their QOL, and reduce adverse reaction of IFN-alpha.

Adult ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Hepatitis B e Antigens ; Hepatitis B, Chronic ; drug therapy ; Humans ; Interferon-alpha ; therapeutic use ; Male ; Quality of Life ; Treatment Outcome

Animals ; Humans ; Liver ; diagnostic imaging ; Liver Diseases ; diagnostic imaging ; Radiographic Image Interpretation, Computer-Assisted ; methods ; Rats ; X-Ray Diffraction ; methods

To investigate me material basis of Mahuang Fuzi Xixin decoction (MFXD) for anti-inflammation and immune-suppression based on the combined method of serum chemical and serum pharmacological. The LC-MS/MS fingerprints of MFXD, drug-containing serum and blank serum were compared to define the components in plasma. Histamine, β-hexosaminidase released from RBL-2H3 cell infulenced by drug-containing serum at different time points were measured by ELISA. The effect of drug-containing serum on lipopolysaccharide-induced splenocyte proliferation at different time points were determined by MTT. A correlation analysis was made on components of MFXD and pharmacological indexes based the stepwise regression method. After the intragastrical administration with MFXD, 32 components were discovered in rat serum, including 27 prototype components (10 from Mahuang, 13 from Fuzi and four from Xixin) and five unknown components. Compared with blank serum, drug-containing serum could reduce the release of histamine from RBL-2H3 induced by antigen at different time points (P < 0.05); except the 4-hour drug-containing serum, all of the remaining drug-containing serums could inhibit the RBL-2H3 mastocyte degranulation induced by antigen at different time points (P < 0.05). Drug-containing serum could significantly lipopolysaccharide-induced mouse splenocyte proliferation at 15 and 30 min (P < 0.05). A regression analysis was made on the chemical data of components absorbed into blood and pharmacological indexes, i. e. release rate of histamine, release rate of β-hexosaminidase and inhibition rate of splenocyte. This suggested the close correlations among methyl pseudo-ephedrine, pseudoephedrine and histamine released from RBL-2H3 induced by antigen; pseudoephedrine, hypaconine, methyl pseudoephedrine and β-hexosaminidase released from RBL-2H3 induced by antigen; as well as benzoyl hypaconine, benzoylaconine, 14-benzoyl-10-OH-mesaconine, mesaconine and lipopolysaccharide-induced mouse splenocyte proliferation. Methylpseudoephedrine, pseudoephedrine, benzoyl hypaconine, benzoylaconine and mesaconine may be part of material basis of MFXD on anti-inflammation and immune suppression.
Animals ; Anti-Inflammatory Agents ; chemistry ; pharmacology ; Cell Degranulation ; drug effects ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Female ; Histamine ; immunology ; Immunosuppressive Agents ; chemistry ; pharmacology ; Male ; Mass Spectrometry ; Mast Cells ; drug effects ; immunology ; Mice ; Rats ; Rats, Wistar ; Serum ; chemistry