The auxiliary effect of suramin application in acute angle closure glaucoma surgery patients / 中国医师杂志

Objective To investigate the effects of suramin application in acute angle closure glaucoma surgery patients.Methods A prospective study method was used.From February 2012 to January 2016,178 acute angle closure glaucoma surgeries in our hospital for treatment were selected,and were equally divided into observation and control groups (89 cases in each group) according to the order of admission,and two groups were given filtration surgery.The observation group was treated with suramin adjuvant therapy after surgery.The duration were 1 ～ 14 d after operation.The prognosis of two groups was observed.Results All patients were successfully completed surgery.The intraoperative and postoperative complications were no seriously occurred;the postoperative intraocular pressure in the observation group and the control group were (11.52 ± 3.24) mmHg and (16.98 ± 5.33) mmHg that compared preoperative [(31.98 ± 5.22) mmHg,(31.87 ± 5.11) mmHg] with significantly different (P ＜ 0.05),while the observation group was significantly lower than that of the control group (P ＜ 0.05).The postoperative peak systolic velocity (PSV) and end diastolic velocity (EDV) values of the central retinal artery of the observation group and the control group were significantly higher than that of preoperation (P ＜ 0.05),and the postoperative PSV and EDV values of the central retinal artery of the observation group were significantly higher than that in the control group (P ＜ 0.05).The postoperative ratios of functional filtering bleb in the observation group and control group were 80.9％ and 60.7％,respectively.The observation group was significantly higher than that of the control group (P ＜ 0.05).Conclusions The application of suramin in acute close angle glaucoma filtration surgery can promote the function of filtering bleb and intraocular pressure reduction,and improve the ocular blood flow speed that has good application effects.

Effect of suramin on trabeculectomy in rabbit / 国际眼科杂志(Guoji Yanke Zazhi)

AIM:To investigate the effect of suramin concentration changes on trabeculectomy in rabbit, and to provide treatment strategies for glaucoma on the basis of experiment. METHODS:Thirty-two albino rabbits were randomly divided into four groups, including standard control group, experimental group Ⅰ, experimental group II, and experimental group Ⅲ. Each eye was performed standard trabeculectomy. During surgery, standard control group was given a piece of cotton with 0. 3mg/mL mitomycin C ( MMC ) for 2min, and the other three groups were given a piece of cotton with 0. 3, 0. 4, and 0.5mg/mL suramin respectively for 2min. The filtering blebs and intraocular pressure ( IOP ) were observed at the 3, 7, 15, and 30d after surgery. Some conjunctiral specimen were observed with hitochemicall ( HE staining) and immunohistochemicall methods. RESULTS:At postoperative 7, 15, and 30d, the changes of the IOP, functional filtering blebs, and the number of positive cell nuclear in experimental group II and experimental group Ⅲ were significantly different compared with those in standard control group and experimental group Ⅰ (all P0. 05). The changes of the IOP and the number of positive cell nuclear in experimental group Ⅲ were significantly different compared with those in experimental group II (P0. 05). The status of filtering channel in experimental groupII and experimental group Ⅲ were better than those in experimental group Ⅰ and standard control group. CONCLUSION: The concentration of suramin has a significantly influence on its effect. When the concentration is 0. 3mg/mL, the antiproliferative effect of suramin is no more than that of MMC. The effect of 0. 4, 0.5mg/mL suramin is better than MMC. 0. 5mg/mL suramin has a better effect on controlling IOP and suppressing the growth of fibroblasts than 0. 4mg/mL suramin.

Preventive and therapeutic effects of suramin on lipopolysaccharide-induced mouse model of acute lung injury and its molecular mechanism / 中华急诊医学杂志

Objective The purpose of this research is to study the preventive and therapeutic effects of suramin on lipopolysaccharide (LPS)-induced mouse model of acute lung injury and its molecular mechanism.Methods A total of 24 healthy male C57BL/6 mice were randomly divided into two groups: Control group and suramin group.LPS (5 mg/kg, iv) induced acute lung injury model was used in this study.The severity of lung injury was evaluated using haematoxylin-eosin (HE) staining after the injection of LPS for 0, 24 and 72 hours.The expression of TNF-α and IL-6 mRNA levels were also detected by RT-PCR.In vitro, THP-1 cells were stimulated by LPS (100 ng/mL) with saline or suramin pre-treatment.The expressions of p-ERK1/2, p-JNK and p-P38 were analyzed by Western blot at 10 min, 20 min and 30 min after LPS insult.A 2-tailed Student's t test was used to compare difference between two independent groups.Results Compared with the saline group, the lung tissues injury were significantly decreased in the suramin group of 72 hours after the injection of LPS (saline 3.90 ±0.35;suramin 2.50 ±0.12) (t =7.668, P ＜ 0.01).The expressions of TNF-α (saline 8.35 ± 1.63;suramin 4.62 ± 0.70) (t =4.187, P＜0.01) andIL-6 (saline10.53 ± 2.10;suramin5.53±1.10) (t=4.224, P＜0.01) mRNA were also obviously reduced in suramin group after the injection of LPS for 24 hours.The expression levels of pERK1/2, p-JNK and p-P38 were obviously down-regulated by suramin at 10 min, 20 min and 30 min after LPS stimulation.Conclusion Suramin protected LPS-induced acute lung injury through down-regulating the expression of pro-inflammatory factors, which was closely relative to the inhibition of the MAPK pathway.

Inhibitory Effects of Suramin in Combination with PG-Rg3 on the Growth of Lung Adencarcinoma in Mice / 天津医药

Objective To observe the effect of suramin combinated with PG-Rg3 on xenograft growth of lung adeno-carcinoma in mice, and the related mechanism thereof. Methods Forty C57BL/6J mice bearing Lewis cells were random-ized into five groups:control group, cisplatin (DDP) group, suramin group, PG-Rg3 group and combination group. Appropri-ate interventions were given in five groups of mice. Mice were sacrificed at day 24 after tumor inoculation. The subcutaneous tumors were stripped for histological examination. The tumor inhibitory rate was measured. The expressions of erythropoietin-producing hepatoma amplified sequences (Eph) B4 protein, Bcl-2 and tumors microvessel density (MVD) were determined by immunohistochemistry method with image analyze system. The apoptosis of tumor cells was measured by biotinyated dUTP nick and labeling (TUNEL) method. Results There were significantly lower values in subcutaneous tumor volume and weight in drug-treated groups than those in control group (P<0.05). The inhibitory rates were 39.20%, 49.11%, 54.86%and 62.49%in cisplatin group, suramin group, PG-Rg3 group and combined group (P<0.05). The values of EphB4, MVD and Bcl-2 grey values were significantly decreased, the apoptotic index was significantly increased, in suramin group, PG-Rg3 group and combined group than those of control group and DDP group (P<0.05). The values of EphB4, MVD and Bcl-2 grey values were significantly increased, the apoptotic index was significantly decreased, in suramin group and PG-Rg 3 group than those of combined group (P<0.05). Conclusion Suramin combinated with PG-Rg3 can produce a synergetic inhibitory activity against tumor growth of lung adenocarcinoma, which may be associated with the effect of suppressing the expression of EphB4 and angiogenesis, and the promotion of tumor cell apoptosis.

Effect of suramin on the epithelial-mesenchymal transition in peritoneal mesothelial cells induced by high concentration glucose / 中华肾脏病杂志

Objective To explore the effect of suramin on the epithelial-mesenchymal transition (EMT) and the excretion of transforming growth factor-β1 (TGF-β1) in peritoneal mesothelial cells (PMCs) induced by high concentrations of glucose solution (GS).Methods Cultured PMCs were divided into three groups:(1) normal control group; (2) GS-treated group:cells were treated with 1.5％,2.5％,4.25％ GS for 12 h,24 h,48 h,respectively; (3) Suramin-treated group:PMCs cultured with 4.25％ GS were exposed to different doses of suramin (25,50,100 μmol/L) for 48 h.Expression levels of α-smooth muscle actin (α-SMA) and E-cadherin were detected by Western blotting and the concentration of TGF-β1 in the culture supernatant was determined by ELISA.Results Compared with normal control group,GS-treated PMCs exhibited a time-dependent increase in the expression of α-SMA,and decrease in the expression of E-cadherin.GS also stimulated PMCs to secrete TGF-β1.In the presence of suramin,GS-induced α-SMA expression and TGF-β1 production were reduced,E-cadherin expression was increased.Conclusions Suramin can inhibit high glucose-induced EMT of PMCs by down-regulating the expression of TGF-β1.Suramin may be a novel therapeutic agent for the treatment of peritoneal fibrosis.

Evaluation of anti-allergic activity of gossypin and suramin in mast cell-mediated allergy model.

The mast cell-mediated allergic reactions are involved in many allergic diseases, such as asthma, allergic rhinitis and sinusitis. Stimulation of mast cells initiates the process of degranulation, resulting in the release of mediators such as histamine and an array of inflammatory cytokines. In this report, we investigated the effect of gossypin (a biflavonoid) and suramin (a synthetic polysulphonated naphtylurea) on the mast cell-mediated allergy model, and studied the possible mechanism of their action. Both gossypin and suramin inhibited (P<0.001) compound 48/80-induced systemic anaphylaxis reactions, antiprurities (P<0.001) and reduced the histamine release in rats. Further, both showed significant (P<0.001) protection against rat peritoneal mast cells activated by compound 48/80. Thus, our findings provide evidence that gossypin and suramin inhibit mast cell-derived allergic reactions.

Effects of ATP and LTC4 on hypoxic pulmonary vasoconstriction in isolated rat lungs / 대한마취과학회지

BACKGROUND: Hypoxic pulmonary vasoconstriction (HPV) is unique to pulmonary circulation but the mechanism remains elusive. Red blood cells (RBCs) are known to augment HPV and to release more ATP as oxygen content falls. Leukotrienes constrict smooth muscle and could be important for the regulation of the pulmonary circulation. Hence we hypothesized that ATP and leukotrienes are mediators of HPV produced during acute alveolar hypoxia. METHODS: In forty Sprague-Dawley rats, lungs were isolated and perfused. We administered ATP (10 micrometer) to the ATP group (n = 8), the ATP antagonist, suramin (100 micrometer) to the suramin group (n = 8), leukotriene C4 (LTC4, 5 microgram) to the LTC4 group (n = 8), the LTC4 antagonist, LY171883 (20 micrometer) to the LY171883 group (n = 8), and LTC4 (5 microgram) + ATP (10 micrometer) to the LTC4 + ATP group (n = 8) during normoxic ventilation. HPV responses were induced by three hypoxic challenges for 5 minutes separated by 5 minutes of ventilation with a normoxic gas mixture. Baseline pulmonary artery pressure change after exposure to each drug and hypoxic pressor response between a period 21% normoxic gas ventilation and that of 3% hypoxic gas ventilation were measured. RESULTS: ATP and LTC4 + ATP increased baseline pulmonary artery pressures but LTC4 did not alter it. ATP did not affect hypoxic pressor response. Suramin, LY171883 and LTC4 + ATP inhibited the pressor response to hypoxia. LTC4 increased hypoxic pressor response. CONCLUSIONS: In isolated rat lungs, HPV may be mediated by ATP and LTC4 appears more likely to be a modulator than a mediator of HPV.

Response of P2X receptors in CA1 region of rat hippocampus to ATP and suramin / 第三军医大学学报

Objective To investigate the effects of ATP, suramin, ivermectin (IVM) and low pH value on pyramidal cells of rat hippocampus. Methods Pyramidal cells were rapidly dissociated from the hippocampus of 7-day postnatal rats by mechanical and enzymatic methods. Effects of ATP, suramin, IVM and low pH value on P2X receptor of neurons were studied by the technique of whole cell patch clamp. Results The transmembrane current was affected by ATP and suramin. There were different effects of IVM and low pH value on ATP induced current on different neurons. Conclusion There is extensive expression of P2X receptor on hippocampus pyramidal cells of rats. The expression of P2X receptors subunits are different among neurons.

Long-term effect of suramin on the inhibition of proliferation of cultured human retinal pigment epithelial cells / 中华眼底病杂志

Objective To observe the long-term effect of suramin on the inhibition of proliferation of human retinal pigment epithelial (RPE) cells in vitro. Methods RPE cells grown in 9 pieces of 96-well plate (12 wells each plate) were divided into experimental and control group, with 6 wells in each group. The concentration of 0.1 ml RPE cells in each well is 5?104 cells/ml. After the change of the medium, RPE cells were treated with suramin (250 ?g/ml) in experimental group while treated with nothing in the control group. The medium of the 2 groups were changed to the normal medium after 4 days. At the 1~st , 2~nd , and 4~th day after the addition of suramin and at the 1~st , 2~nd , 3~rd , 5~th , 6~th , 7~th , 9~th , 11~th and 13~th day after removing suramin, 1 plate was randomly selected to stop culturing, and the proliferation of RPE cells were detected by methyl thiazolyl tetrazolium (MTT) assay. Results Under reversed microscope, RPE cells in control group were fused completely at the 7~th day after inoculation. The extracellular space of RPE cells in experimental groups was larger than that in the control group, and remained unfused at the 13~th day after inoculation. The inhibitory rate of proliferation of RPE cells at the first day after treated with suramin was 14.85% and increased to the highest 25.79% at the 4~th day. The first day after the suramin-containing media was removed, the inhibitory rate decreased to 12.35%, and then raised gradually to over 20% at the 3~rd to 5~th day. Finally, the rate drop to 14.71%. Conclusion Suramin has the long-term effect on the inhibition of RPE cells induced by serum, especially the inhibitive effect after the remove of suramin, which indicates the specific double-peak inhibition during the whole process.

The experimental study of antiproliferative effect of suramin on trabeculectomy in rabit / 眼科

Objective To investigate the antiproliferative effect of suramin on trabeculectomy in rabit.Design Experimental study. Participants 32 New Zealand albino rabbits.Methods 32 albino rabbits were randomly divided into four groups.Both eyes of rabbits were performed trabaculectomy and placed a piece of cotton with 0.3 mg/ml mitomycin C(MMC)for 2 minutes in standard control group,220 mg/ml suramin for 2 minutes in experimental groupⅠ,250 mg/ml suramin for 2 minutes in experimental groupⅡ.The examination of intraocular pressure was performed before surgery.The filtration bleb and intraocular pressure were observed at 3,7,15, 30 days after surgery.Some conjunctiral specimen was observed with histochemicall(HE staining)and immunohistochemicall(PCNA staining)methods.Main Outcome Measures Intraocular pressure(IOP),filtering bleb appearance,histopathological staining.Results The percentage of the functional blebs in empty control group and experimental groupⅠwas lower than in standard control group,and experimental groupⅡwas higher than in the other 3 groups at 30 days after surgery.Immunohistochemical staining showed the number difference of PCNA positive cell nuclear was no significant between experiment groupⅠand standard control group,but less than empty control group,and experiment groupⅡwas the least(P

Effects suramin, tumor necrosis factor-alpha(TNF-alpha, interferon-alpha(IFN-alpha on human renal carcinoma cell line growth / 대한비뇨기과학회지

Recently much interest has been expressed for the use of biological response modifiers and growth factor antagonists in the treatment or radiation and chemotherapeutic drug-refractory renal cell carcinoma. Herein antiproliferative effects of Suramin, human recombinanl tumor necrosis factor alpha (TNF-alpha) and human recombinant interferon alpha (IFN-alpha) as a single and in combination were studied in vito on human renal carcinoma cell line (Caki-1). Antiproliferative effect was evaluated by trypan blue dye exclusion assay after 3 days exposure to Suramin at 10, 30, 100, 300, 1,000 mcg/ ml. TNF-alpha at 1, 10, 50, 100, 500, 1,000 units/ml and IFN-alpha at 10, 100, 1,000. 10,000 units/ml concentration, respectively. In addition, effects of combined administration in tolerable peak plasma level or suramin (300 mcg/ml). TNF-alpha (500 units/ml) and IFN-alpha (1000 units/ml) were comparatively analyzed to those of single drug administration. The results were as follows: 1. Significant dose dependent antiproliferative effects were shown by Suramin at above 100 mcg/ml. TNF-alpha at above 500 units/ml and IFN-alpha at above 10 units/ml, respectively (p<0.05). 2. At peak plasma level, suramin, TNF-alpha and IFN-alpha showed less than 50% inhibition of proliferation. 3. On combined administration, suramin plus TNF-alpha (61.0%), Suramin plus IFN-alpha(71.7%) and TNF-alpha plus IFN-alpha (57.2%) induced significantly greater inhibition of proliferation (p<0.005). These results suggest that further in vivo study using combination of Suramin plus TNF-alpha Suramin plus IFN-alpha and TNF-alpha plus IFN-alpha is necessary and that these combination trials may become one of the treatment options for renal cell carcinoma.

Experimental study on the effect of surmin on penile squamous carcinoma cell line(CUPE-1) / 대한비뇨기과학회지

Experimental study was done to investigate the effect of suramin on the in vitro and in vivo proliferation and metastasis of penile squamous carcinoma cell line(CUPE-1), morphological changes of CUPE-1 cells induced by suramin and mechanism of action of suramin. Suramin inhibited in vitro proliferation of CUPE-1 significantly with 1C50 of 100 microgram/ml media. In vitro antiproliferative effect of suramin on CUPE-1 was reversible after stopping administration of the drug. Weekly intraperitoneal administration of 200 mg/kg of suramin to nude mouse inhibited the proliferation and metastasis of intraperitoneally implanted CUPE-1 cells significantly. but did not show significant effect on the proliferation of subcutaneously implanted CUPE-1 cells. Suramin induced senile changes on ultrastructure of CUPE-1 cells. Suramin of 300 microgram/ml inhibited the prolireration-stimulating effect of EGF significantly, whereas, suramin of 100 microgram/ml did not inhibit the effect of EGF significantly. Suramin did not show significant cytotoxicity on 3H-thymidine release assay. These results suggest that suramin is a promising drug for the treatment of advanced penile squamous cell carcinoma and blood level of suramin in clinical trial should be continuously maintained in about 300 microgram/ml, and that the main machanism of suramin against CUPE-1 is cytostatic. by antagonizing the action of EGF and inducing growth arrest and senile change.

Effects of suramin on vascular endothelial growth factor of chronic hypoxia and hypercapnia rats / 中国药理学通报

AIM To explore the roles of vascular endothelial growth factor (VEGF) in hypoxia pulmonary hypertension and effects of suramin. METHODS Thirty SD rats were randomly divided into normal control group (N), hypoxia hypercapnia group(F), hypoxia hypercapnia +suramin group (S). The levels of VEGF in serum and in lung tissue were measured by ELISA, the ultrastructure of pulmonary arterioles was observed by electron microscopy, the expression of VEGF was observed by immunohistochemistry, the expression of VEGFmRNA was observed by in situ hybirdization. RESULTS ①Mean pulmonary arterial pressure(mPAP), weight ratio of RV to LV+S, the leves of VEGF in serum and in lung tissue of group F were significantly higher than that of group N and group S (P