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Objective To observe the antitumor effect of 153Sm-DTPA-c (CGRRAGGSC) on MHCC97-H human liver cancer using a nude mice model.Methods 153Sm-DTPA-c(CGRRAGGSC) was indirectly synthesized by the reaction of 153SmC13 with DTPA-c(CGRRAGGSC).Western blot was used to detect the expression changes of IL-11 receptor of eight different cell lines.20 MHCC97-H tumor-bearing nude mice were randomly divided into four groups by random number table method with five mice in each group,administered with different activities of 153 Sm-DTPA-c (CGRRAGGSC) by tail vein injection (5.5,11.0,22.0 MBq/0.2 ml and physiological saline/0.2 ml in turn).All nude mice were terminated after 16 d then the tumor tissue was observed and analyzed with microscopy,electron microscopy and immunohistochemistry for Ki-67,Bc1-2 and IL-11 receptor.Western blot was used to evaluate the expression changes on IL-11 receptor of tumor tissue at different doses.Results After administration with 153 Sm-DTPA-c(CGRRAGGSC),the central region in the early stage of tumor became dry,necrosis,and crusting.In the late stage,tumor continually grew surrounding necrosis tissue.The inhibition rates in the low,middle and higher dose group were (22.72 ±2.76)％,(34.65 ±2.36)％ and (85.13 ±5.78)％,respectively(F =89.32,P ＜ 0.05).The morphologic results showed that tumor structures were severely damaged along with radiation dose.The results of immunohistochemistry showed that the IL-11 receptor-positive cells in the control group and 5.5 MBq group was (84.13 ± 5.71) ％ and (61.57 ± 5.98) ％ (t =13.62,P ＜0.05),respectively.The Ki-67 and Bcl-2 positive cells were decreased in the injection group (t =20.91,6.68,P ＜0.05).Western blot analysis showed that the expression of IL-11 receptor protein decreased with antitumor-effect of radiation.Conclusions 153Sm-DTPA-c (CGRRAGGSC) effectively depresses the growth of MHCC97-H human liver cancer and suppresses the expression of IL-11 receptor,and hence could be a promoting agent for the treatment of MHCC97-H human liver cancer.
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Objective To explore the effect of 153Sm-EDTMP combined ibandranate in treatment of osseous metastasis of lung cancer.Methods 100 patients with osseous metastasis of lung cancer were randomly divided into two groups.The patients received intervenous drop infusion of 153Sm-EDTMP and ibandranate in treatment group( n =52).The patients received therapy with 153Sm-EDTMP in control group( n =48).The differentces of effect of odynolysis,locomotor activity,improvement of quality of life,recovery of osteolysis,toxical and adverse reaction between two groups were compared.Results The overall response rate 94.2％ in treatment group was significantly higher than that 64.5 ％ in control group( x2 =4.78,P ＜ 0.0.5 ) ;The activity to improve situation 82.6％ in treatment group was significantly higher than that 64.5％ in control group( x2 =4.13,P ＜ 0.05 ) ;The total effective rate of quality of life improve the situation 84.6％ in treatment group was significantly higher than that 62.5％ in control group( x2 =4.58,P ＜0.05 ) ;The side effects had no significant difference between two groups ( x2 =0.345,P ＞ 0.05).Conclusion The treatment of 153Sm-EDTMP combined with ibandranate in the treatment of osseous-metastasis of lung cancer was effective for relieving pain,improvement locomotor activity,improvement of quality of life,recovery of osteolysis.
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Objective To evaluate the clinical curative effect of using 153Sm-EDTMP in painful bone metastasis of malignant tumor. Methods Eighty patients with bone metastasis of malignant rumor underwent radionuclide bone palliation therapy were analysed.The treatment efficacy was evaluated by visual analogue scale (VAS) and Kamofsky performance scale.Results 68.75% of patients had a positive response.A better analgesic effect was found in cases of lung,prostate and breast carcinoma metastasm compared to metastasis from other malignant lesions.Improvement of performance in Karnofsky scale was found in cases of midrange and heavy range patients.Conclusion The analgesic effects of 153Sm-EDTMP is obvious in painful bone metastasis of malignant tumor.Improvement of life quality is significant in cases of midrange and heavy range patients.The therapeusis is a beneficial supplement of radiotherapy and odynolysis therapy.
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PURPOSE: Ethylenediamine-tetramethylenephosphonic acid (EDTMP) has widely used chelator for the labeling of bone seeking radiopharmaceuticals complexed with radiometals. 153Sm can be produced by the HANARO reactor at the Korea Atomic Energy Research Institute, Taejon, Korea. 153Sm has favourable radiation characteristics T1/2=46.7 h, beta max=0.81 MeV (20%), 0.71 MeV (49%), 0.64 MeV (30%) and gamma=103 keV (30%) emission which is suitable for imaging purposes during therapy. We investigated the labeling condition of 153Sm-EDTMP and imaging of 153Sm-EDTMP in normal rats. MATERIALS AND METHODS: EDTMP 20 mg was solved in 0.1 mL 2 M NaOH. 153SmCl3 was added to EDTMP solution and pH of the reaction mixtures was adjusted to 8 and 12, respectively. Radiochemical purity was determined with paper chromatography. After 30 min. reaction, reaction mixtures were neutralized to pH 7.4, and the stability was estimated upto 120 hrs. Imaging studies of each reaction were perfomed in normal rats (37 MBq/0.1 mL). RESULTS: The labeling yield of 153Sm-EDTMP was 99%. The stability of pH 8 reaction at 60, 96 and 120 hr was 99%, 95%, 89% and that of pH 12 at 36, 60, 96 and 120 hr was 99%, 95%, 88%, 66%, respectively. The 153Sm-EDTMP showed constantly higher bone uptake from 2 to 48 hr after injection. CONCLUSION: 153Sm-EDTMP, labeled at pH 8 reaction condition, has been stably maintained. Image of 153Sm-EDTMP at 2, 24, 48 hr after injection, demonstrate that 153Sm-EDTMP is a good bone seeking radiopharmaceuticals.
Subject(s)
Animals , Rats , Academies and Institutes , Chromatography, Paper , Hydrogen-Ion Concentration , Korea , Nuclear Energy , RadiopharmaceuticalsABSTRACT
AIM: To comparatively analyze the pain related factors levels and therapeutic response in patients treated with ~(99)Tc-MDP and ~(153)Sm-EDTMP for painful skeletal metastases. METHODS: Plasma endothelin (ET), calcitonin gene-related peptide (CGRP), thromboxane B_2 (TXB_2) and 6-keto-prostaglandin F_ 1? (6-k-PGF_ 1? ) levels were analyzed in 93 patients with painful skeletal metastases prior and 3 months after treatment. 55 cases were just treated with 153 Sm-EDTMP (group A); 19 cases were treated only with 99 Tc-MDP (group B); and 19 cases were treated with both 153 Sm-EDTMP and 99 Tc -MDP (group C). RESULTS: 69.1 %, 73.7 % and 89.5 % of the patients were experienced pain relief 3 months after treatment in groups A, B and C, respectively. Comparative analysis shows that: ET and 6-k-PGF_ 1? levels increased significantly 3 months after treatment in all patients (P
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Objective To evaluate the feasibility of 153 Sm EDTMP for multiple bone metastasis.Methods 32 patients with multiple bone metastases were treated with 153 Sm EDTMP injected into the veins,0.4～1.0 mci/kg,of which 7 cases received therapy for 2～3 times.Results 53.1%(17/32)was relieved completely,25.0%(8/32)was relieved partially and 9.4%(3/32)was relieved slightly.No effects were found in 12.5%(4/32).The overall effective rate was 78.1%.Side effects that were the decreasing of WBC and PLT were found in 15.6%(5/32),which rose to the preoperative levels within 6～8 weeks.Conclusion Internal radiotherapy with 153 Sm EDTMP is safe and effective in the treatment of multiple bone metastases.
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Objective To investigate the clinical effect of 153 Sm-EDTMP treatment on pain palliation in the patients with bone metastasis of lung cancer, breast cancer or prostate cancer. Methods 166 patients with bone metastasis of cancers were intravenously injected 18.5～37 MBq/kg (0.5～1.0 mCi/kg ) body weight of 153 Sm-EDTMP, once a month or two months. Results The effective rate of pain palliation of 153 Sm-EDTMP treating bone metastasis of lung cancer, preast cancer and prostate cancer were 68.5%, 89.3% and 100%, respectively. The efficacious rate of pain palliation in breast and prostate cancers was significantly higher than that in lung cancer (P
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Objective Effects of intra articular injection of 153 Sm citrate HA on antigen induced arthritis were investigated to provide the theoretical fundation for its clinical application.Methods Rabbit arthritis was induced by subcutaneous injection of ovalbumin at weeks 2 and 4,and by intra articular injection of it at week 6.The dosage of 1 85?10 7 Bq or 3 7?10 7 Bq of 153 Sm citrate HA was injected separately into a side of knee joint.The severity of arthritis was determined by joint swelling,skin surface temperature,macroscopic and histologic changes in joints when the rabbits were killed at week 9 after establishment of model.Results Both dosages of 153 Sm have an initial pro inflammatory effects during one week after injection,and then resulted in reduction of joint diameter and skin surface temperature. 153 Sm (3 7?10 7 Bq) showed a more alleviation than 153 Sm (1 85?10 7 Bq) in respect of macroscopic and histologic changes.Conclusion Synovectomy with 153 Sm citrate HA is effective for treatment of chronic arthritis with dependence on the doses and deserves further study.
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Objective: To evaluate the effect of Samarium etramthylene phosphoric acid(153Sm-EDTMP) in the treatment of painful bony metastases from prostate cancer after hormone therapy.Methods: 18 patients after being treated with hormone therapy(excision of testes+flutamide) for 3~6 months and with painful bony metastases from prostate cancer were injected 153Sm-EDTMP(dosage:37MBq/kg),After the patients underwent 1~3 dose treatment.The palliation of pain and change of bone metastases on bone scans were evaluated.Results: A significant decrease of bone pain was achieved,making up 77.8%(14/18) and X ray and bone radionuclide imaging exam showed that 2 patients achieved complete focus disappearance,and 8 patients achieved partial focus disappearance.The response rate is 55.5%.Conclusion: 153Sm-EDTMP radiotherapy is efficacious to the refractory painful bone metastases in prostate cancer.