6-ketoprostaglandin-f1-alpha and tetramethylpyrazine

To explore the protective effect and mechanism of ligustrazine (LGT) and propofol (PRO) on peri-operational liver ischemia-reperfusion injury (HIRI).. Thirty-six patients scheduled for hepatic surgery were randomly divided into the control group, the LGT group, the PRO group and the LGT + PRO group, 9 patients in each group. Changes of superoxide dismutase (SOD), lipid peroxide (LPO), ratio of thromboxane B2 (TXB2) and 6-keto-prostaglandin F1alpha (6-keto-PGF1alpha), alanine aminotransferase (ALT) activity, and the ultrastructure of liver tissue were dynamically observed.. Compared with the control group, SOD activity was significantly higher, LPO concentration, TXB2/6-keto-PGF1alpha ratio and ALT value were significantly lower (P < 0.05 and P < 0.01) in the LGT group, the PRO group and the LGT + PRO group during HIRI, with the abnormal changes of hepatic ultrastructure 25 min after reperfusion significantly alleviated in the three treated group.. Combination of ligustrazine and propofol shows protective effect on liver by decreasing oxygen free radical level, reducing lipid peroxidation and adjusting TXA2/PGI2 imbalance after hepatic ischemia-reperfusion in patients undergoing hepatic cancer surgery.

Topics: 6-Ketoprostaglandin F1 alpha; Adult; Drug Therapy, Combination; Female; Humans; Lipid Peroxides; Liver; Liver Neoplasms; Male; Middle Aged; Propofol; Pyrazines; Reperfusion Injury; Superoxide Dismutase

To study protective effects of tetramethylpyrazine (TMP) on the imbalance of TXA2/PGI2 during cardiopulmomary bypass (CPB) in congenital heart disease (CHD) with pulmonary hypertension (PH) patients.. Thirty patients suffered from non-cyanotic CHD-PH were randomly divided into control group (n = 15) and treatment group (n = 15). 3 mg/kg of TMP was dripped intravenously after anesthesia and 1 mg/kg of TMP was infused into oxygenator after CPB individually. Blood samples were collected and TXA2 as well as PGI2 were measured after anesthesia induction, 15 min during CPB, 5 min after release of the aortic cross-clamp, and 20 min, 6 hrs and 24 hrs after CPB.. There was significant difference between treatment group and control group except before operation and 24 hrs after CPB.. The imbalance of TXA2 and PGI2 in patients with CHD-PH during CPB could correct by TMP.

Topics: 6-Ketoprostaglandin F1 alpha; Adolescent; Adult; Cardiopulmonary Bypass; Child; Child, Preschool; Female; Heart Septal Defects, Atrial; Heart Septal Defects, Ventricular; Humans; Hypertension, Pulmonary; Male; Pyrazines; Thromboxane B2; Vasodilator Agents

To explore the role of hypercoagulation in the metastasis of carcinoma.. The effect of Tetramethylpyrazine (TTMP) on platelet functions among the 25 advanced cases of lung carcinoma, and 26 matched control subjects were investigated in the study. Their ages varied from 31-86 years (mean 58.2) in lung carcinoma group (13 male, 12 female) and 36 to 61 (mean 52.9) in the control group (16 male, 10 female). The pathologic types were as follows: 7 cases of squamous cell cancer, 12 adenocarcinoma, 2 small cell carcinoma and 4 undistinguished type. The TNM stage revealed 14 cases in stage IIIa, 3 in stage IIIb and 8 in stage IV. The site of metastasis included mediastinal lymph node, pleura, supraclavicular lymph node, brain, spine, costa, skin and pericardium. The levels of plasma TXB2, 6-keto-PGF1 alpha, VIII:C, vWF, AT-III:a, AT-III:Ag, Fg and blood PAdT, PAgT were measured before and after the intravenous infusion of 80 mg TTMP in patients with lung carcinoma.. The levels of TXB2, 6-keto-PGF1 alpha, VIII:C, vWF and Fg in lung carcinoma group were significantly elevated, while the levels of PAdT was greatly decreased, compared with the control group, no significant differences in levels of PAgT, AT-III:a and AT-III:Ag were found between the two groups. After the infusion of TTMP the levels of PAdT, PagT, VIII:C, dWF and Fg were decreased significantly, while TXB2, 6-keto-PGF1 alpha, AT-III:a and AT-III:Ag remained unchanged.. TTMP inhibits the adhesion and aggregatory functions of blood platelet and the activity of coagulation factors. It might be one of the mechanisms of TTMP's antimetastasis of lung carcinoma.

Topics: 6-Ketoprostaglandin F1 alpha; Adenocarcinoma; Adult; Aged; Aged, 80 and over; Carcinoma, Squamous Cell; Female; Humans; Lung Neoplasms; Male; Middle Aged; Platelet Aggregation; Platelet Aggregation Inhibitors; Pyrazines; Thromboxane B2

To explore the effects of ligustrazine on proteinuria, urinary TxB2 (metabolism of thromboxane A2, TxA2) and 6-keto-PGF1alpha (metabolism of prostacyclines I2, PG I2), glomerular inducible nitric oxide(NO) synthase (iNOS) mRNA, urinary NO3-/NO2- (decomposing products of NO) and pathological changes in rats with passive Heymann nephritis (PHN).. A rat PHN model was induced by intravenous injection of rabbit anti-rat renal tubular antigen (Tub-Ag) antiserum, and ligustrazine was given intraperitoneally into PHN rats every 2 days for 1-5 weeks. Then, proteinuria, urinary TxB2 and 6-keto-PGF1alpha, glomerular iNOS mRNA, and urinary NO3-/NO2- were measured by sulfosalicylic acid, radioimmunoassay (RIA), Northern blot and nitric acid reductase methods, respectively. Moreover, the damage to the renal tissue of the rats was observed under light and electron microscopy and immunofluorescence (IF).. The urinary TxB2 in PHN rats was significantly higher than that in control rats, but the PHN rats treated with ligustrazine had significantly less proteinuria, urinary TxB2 and tissue lesions, and more urinary 6-keto-PGF(1alpha), glomerular iNOS mRNA and urinary NO2-/NO3- than the PHN rats without the administration of ligustrazine.. These data indicate that ligustrazine has inhibitory roles on the glomerular injury of PHN rats, which may associate with modulating the balance of TxA2-PGI2 and elevating synthesis of NO to a certain extent.

Topics: 6-Ketoprostaglandin F1 alpha; Animals; Epoprostenol; Female; Fluorescent Antibody Technique, Direct; Glomerular Basement Membrane; Glomerulonephritis; Immunoglobulin G; Kidney Glomerulus; Nitrates; Nitric Oxide; Nitric Oxide Synthase Type II; Nitrites; Proteinuria; Pyrazines; Rats; RNA, Messenger; Thromboxane A2

To study the effect on large dose of Ligustrazine on the function of platelet and endothelial cells of patients with acute onset of cor pulmonale.. Platelet aggregation rate (PAR), thromboxane B2 (TXB2), 6-keto-prostaglandin F1 alpha (6-keto-PGF1 alpha), von Willebrand's factor (vWF), PaO2 and PaCO2 were assayed in 30 patients with acute onset of cor pulmonale and 26 cases of control before and after treatment of large dose of Ligustrazine.. PAR, vWF, TXB2, TXB2/6-keto-PGF1 alpha and PaCO2 decreased (P < 0.05, P < 0.01), and 6-keto-PGF1 alpha, PaO2, SaO2 increased (P < 0.01) after treatment of Ligustrazine, and only PaCO2 decreased in control.. Ligustrazine had the function of antiplatelet and protecting the endothelial cells. Large dose (800 mg/d) had no side-effects.

Topics: 6-Ketoprostaglandin F1 alpha; Aged; Female; Humans; Male; Middle Aged; Platelet Aggregation; Platelet Aggregation Inhibitors; Pulmonary Heart Disease; Pyrazines; Qi; Thromboxane B2; von Willebrand Factor

The purpose of this study was to investigate effects of tetramethylpyrazine (TMP), a Chinese plant-derived medicine, on coronary vasoconstriction and related electrocardiographic and histologic changes caused by endothelin-1 (ET-1), and on plasma ET-1 levels. ET-1 (75 pmol) was administered into the left coronary artery (LCA) in anesthetized closed-chest dogs with and without prior infusion of TMP (80 mg/kg). Coronary arterial diameter (CAD) was determined by coronary arteriography (CAG). Blood pressure and electrocardiogram (ECG) were monitored continuously. Histologic damage in tissues was ascertained microscopically. Plasma ET-1 and 6-keto-PGF1 levels were determined by RIA 90 min after i.v. injection of TMP (25 mg/kg; n = 5) in rabbits. Intracoronary injection of ET-1 resulted in a significant vasoconstriction of the entire vascular bed of the LCA, with a decrease in CAD of 35.9 +/- 5.7% (n = 5; p < 0.01) and ischemic changes on ECG and in tissues of endocardium, myocardium, coronary endothelial cells, and capillary vessels. Pretreatment with TMP produced a significant increase in CAD by 38.5 +/- 7.8% (n = 5; p < 0.01) and greatly suppressed the vasoconstriction produced by ET-1. The myocardial tissue damage estimated from the ratio of ischemic area for the entire area after ET-1 injection (35.6%) was completely abolished by TMP (0.6%). In addition, TMP injection induced a significant decrease in plasma ET-1 levels and an increase in 6-keto-PGF1 levels in rabbits. The Chinese medicine TMP could be a useful therapeutic agent in ischemic heart disease by suppressing coronary vasoconstriction and ischemic changes in the tissues produced by ET-1.

Topics: 6-Ketoprostaglandin F1 alpha; Angiography; Animals; Coronary Vessels; Dogs; Drugs, Chinese Herbal; Electrocardiography; Endothelin-1; Male; Pyrazines; Rabbits; Vasoconstriction; Vasodilator Agents

To study the pathophysiological changes and effective treatment of intrauterine growth retardation (IUGR).. Eighty-five cases with normal pregnancy and 58 IUGR women maternal red blood cell superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), serum lipid peroxide (LPO) and thromboxane B2 (TXB2), 6-keto-PGF1 alpha(6KP) were examined. IUGR group was divided into Ligustrazine group (LIG, 47 cases) and amino acid group (AAG, 11 cases) and treated accordingly.. In IUGR group, LPO increased and SOD, GSH-Px activity, 6KP value decreased abnormally, TXB2/6KP ratio significantly increased, which was negative correlated with SOD, GSH-Px activity and positive correlated with LPO level markedly. After treatment, all the changes were improved and almost reached normal range. The fetal outcome showed that the total effective rate was 95.7% in LIG, markedly higher than that in AAG (81.8%, P < 0.05), there was significant difference between LIG and AAG.. The balance of body oxidate/antioxidate system was disturbed and the uteroplacental-fetal circulation was obstracted in IUGR. Ligustrazine could inhibit oxygen free radical, rise SOD, GSH-Px activity, regulate TXA2/PGI2 balance, promote fetal growth.

Topics: 6-Ketoprostaglandin F1 alpha; Adult; Female; Fetal Growth Retardation; Free Radical Scavengers; Humans; Pregnancy; Pyrazines; Superoxide Dismutase; Thromboxane B2

We examined the effect on 6-Keto-PGF1a and TXB2 (the stable metabolites of PGI2 and TXA2) outflow of pretreatment with tetramethylpyrazine in the hypoxic isolated rat heart. In control hearts, 6-Keto-PGF1a was increased from 185 +/- 46 pg/ml of baseline value to 335 +/- 76 pg/ml after 2 min of hypoxia and TXB2 increased from 136 +/- 28 pg/ml of baseline value to 230 +/- 43 pg/ml at 20 min of hypoxia and 252 +/- 32 pg/ml after 5 min of reoxygenation. Pretreatment with tetramethylpyrazine increased the 6-Keto-PGF1a concentration to 266 +/- 51 pg/ml (143% of control heart), 471 +/- 89 pg/ml (150% of control heart) and 332 +/- 47 pg/ml (195% of control heart) at 15 min of normoxia, 2 min of hypoxia and 5 min of reoxygenation, respectively (p < 0.05 vs control). On the other hand, tetramethylpyrazine diminished the release of TXB2 to 78 +/- 21 pg/ml (174% of control heart), 160 +/- 30 pg/ml (144% of control heart), and 196 +/- 23 pg/ml (128% of control heart) at 15 min of normoxia, 20 min of hypoxia and 5 min of reoxygenation, respectively (p < 0.05 vs control). These data show that pretreatment with tetramethylpyrazine enhances PGI2 outflow and attenuates release of TXA2 in the rat heart during normoxia, hypoxia and reoxygenation.

Topics: 6-Ketoprostaglandin F1 alpha; Animals; Blood Pressure; Coronary Circulation; Epoprostenol; Heart; Hypoxia; In Vitro Techniques; Male; Myocardium; Perfusion; Platelet Aggregation Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Thromboxane A2; Thromboxane B2; Time Factors; Vasodilator Agents

We investigated the release of PGI2 and TXA2 by measuring their stable metabolites of 6-keto-PGF1a and TXB2 in the perfusate in the isolated rat heart after pretreatment with tetramethylpyrazine (TMP). Pretreatment with TMP (12 mg/kg, i.p.) 7 days before preparation produced a significant elevation of 6-keto-PGF1a from 2.30 +/- 0.65 ng/min/g of untreated controls to 3.8 +/- 0.77 ng/mir/g (p < 0.05). Pretreatment with TMP also decreased TXB2 release (p < 0.05 versus control).

Topics: 6-Ketoprostaglandin F1 alpha; Animals; Epoprostenol; Heart; In Vitro Techniques; Male; Myocardium; Pyrazines; Rats; Rats, Sprague-Dawley; Reference Values; Thromboxane A2; Vasodilator Agents

The toxic effect of cyclosporine A (CsA) on pancreatic islet beta-cells and the preventive effect of ligustrazine (LIG) on CsA-associated beta-cell toxicity in SD rats were investigated. The oral administration of CsA 50 mg/kg/day for ten days caused hyperglycaemia and lowering of plasma and pancreatic insulin levels that were prevented and/or minimized by the combined intra-peritoneal administration of LIG 50 mg/kg/day. An increase of urinary thromboxane B2 (TXB2) and urinary TXB2/6-keto-prostaglandin F1 alpha (6-k-PGF1 alpha) ratio in CsA-treated rats could also be prevented and/or minimized by the administration of LIG. The results suggested that the preventive effect of LIG on CsA-associated islet beta-cell toxicity was relevant to the improvement of prostacyclin-thromboxane A2 imbalance.

Topics: 6-Ketoprostaglandin F1 alpha; Animals; Cyclosporine; Fibrinolytic Agents; Islets of Langerhans; Male; Pyrazines; Rats; Rats, Sprague-Dawley; Thromboxane B2

To evaluate the therapeutic effects and mechanisms of tetramethylpyrazine (TMP), a Chinese herbal medicine, on the lung injury in bile-induced acute haemorrhagic necrotizing pancreatitis (AHNP) in the SD rats, the rats were randomly divided into three groups: sham-operative, untreated and TMP treated. AHNP model were induced by ligation with 5% taurocholate. The changes of lung index, serum lipid peroxide (LPO), TXB2, 6-keto-PGF1 alpha, and lung pathology at light and electron microscope were all investigated at 1, 6, 12 hours after induction of AHNP model. Survival rate of AHNP in rats were recorded also. Results of the study showed that in untreated group, the time-related progressive pancreatic haemorrhage and necrosis, accompanied by pancreatitis-associated lung injury, such as pronounced pulmonary congestion, alveolar and interstitial edema, polymorphonuclear granulocytes infiltration, transparent membrane formation, the density of layer body in type II endothelial cells decreasing, with some vacuole formation, mitochondria, endoplasmic reticulum swollen, basal membrane of endothelial cells rupture were observed. The level of LPO elevated at 1 hour after induction of AHNP and peaked at 12 hours. TXB2 and 6-keto-PGF1 alpha was increased. Using TMP treatment, survival rate increased, and lung at light and electron microscope were much improved and lung index, value of LPO, TXB2 decreased significantly, 6-keto-PGF1 alpha increased slightly, the ratio of TXB2/6-keto-PGF1 alpha was stabilized. It was suggested that TMP has definite therapeutic effects on AHNP-related lung injury in rats, and exerted by scavenging oxygen free radical, inhibiting synthesis of TXA2, augmenting production of PGI2 and maintaining balance between TXA2 and PGI2.

Topics: 6-Ketoprostaglandin F1 alpha; Animals; Free Radical Scavengers; Lipid Peroxides; Lung; Necrosis; Pancreatitis; Pyrazines; Random Allocation; Rats; Rats, Sprague-Dawley; Thromboxane B2

The effect of 18 kinds of Chinese herbal medicine for the synthesis of TXA2 and PGI2 was studied. The porcine lung microsoma was used as donor of enzymes such as cyclo-oxygenase, thromboxane A2 synthetase and prostacyclin synthetase, etc. It was found that Glehnia littoralis could inhibit the synthesis of TXA2 and increase the formation of PGI2. Rheum palmatum (300 mg group) and Erigeron breviscapus significantly inhibited the synthesis of TXA2, but no apparent effection on the synthesis of PGI2. When Codonopsis pilosulae, Astragalus membracaceus, Angelica sinensis, Ginsenosides and Baicalin, etc. markedly inhibited the formation of TXA2 and mildly affected the formation of PGI2. Some Chinese herbs for promoting blood circulation play an important role on the inhibition of TXA2 synthesis. Some tonic herbs could either inhibit the synthesis of TXA2 and increase the synthesis of PGI2 or inhibit the formation of PGI2. Therefore these tonic herbs had the characteristics of both strengthening the body resistance and eliminating pathogenic factors. In this aspect they are better than the control drug (Aspirin) and other herbs of promoting blood circulation.

Topics: 6-Ketoprostaglandin F1 alpha; Animals; Drug Combinations; Drugs, Chinese Herbal; Ginsenosides; Lung; Microsomes; Phenanthrolines; Plant Extracts; Pyrazines; Salvia miltiorrhiza; Saponins; Swine; Thromboxane B2

In recent years, it is believed by some scholars that the injury of myocardial ischemic reperfusion is correlated to the thromboxane A2 (TXA2) released by platelets. In order to explore that whether the myocardial and hemangio-endothelial cells participate in the TXA2 production during the process of reperfusion, the modified Langendorff method was used to establish the model of reperfusing the isolated rat heart. On the other hand, this experiment was also intended to observe the effect of ligustrazine on the injury of myocardial ischemic reperfusion. The results revealed that the level of thromboxane B2 (metabolite of TXA2) and lactic dehydrogenase (LDH) in coronary sinus reflux fluid increased during the process of reperfusion, while the level of 6-keto-PGF1 alpha in the same fluid relatively decreased (P < 0.05). The ratio of TXB2/6-keto-PGF1 alpha was raised. The ligustrazine inhibited the release of TXB2 and LDH, but promoted the production of 6-keto-PGF1 alpha (P < 0.05). The results also proved that the myocardial and hemangio-endothelial cells could synthesize TXA2, and the amount of TXA2 released increased during the reperfusion of ischemic myocardium, which was likely to be the major factor of the injury of ischemic myocardial reperfusion. Ligustrazine plays an important role in protecting the myocardium.

Topics: 6-Ketoprostaglandin F1 alpha; Animals; Female; In Vitro Techniques; L-Lactate Dehydrogenase; Male; Myocardial Reperfusion Injury; Pyrazines; Rats; Rats, Sprague-Dawley; Thromboxane B2

Before and after oral administration of Ligustrazine controlled release capsule, changes of hemorrheology and TXA2/PGI2 were evaluated in 16 patients with advanced cor pulmonale. It was shown that the effects of decreasing whole blood and plasma viscosity and lowering hematocrit and fibrinogen level were noted after one course of treatment with this medication. It is suggests that anticoagulant, effect of Ligustrazine is probably related to its role of improving inbalance between TXA2 and PGI2 in patients with cor pulmonale.

Topics: 6-Ketoprostaglandin F1 alpha; Aged; Blood Viscosity; Delayed-Action Preparations; Female; Fibrinogen; Hematocrit; Humans; Male; Middle Aged; Pulmonary Heart Disease; Pyrazines; Thromboxane B2

Before and after oral administration of sustained Ligustrazine, changes of hemorrheology and TXA2/PGI2 were evaluated in 16 patients with advanced chronic pulmonary heart disease. A decrease in whole blood and plasma viscosity, and reductions in hematocrit and fibrinogen were found after one course of treatment with sustained Ligustrazine. The mechanism of these effects may be related to improved modulation of imbalance of TXA2/PGI2 in patients with advanced chronic pulmonary heart disease.

Topics: 6-Ketoprostaglandin F1 alpha; Aged; Aged, 80 and over; Blood Viscosity; Female; Fibrinolytic Agents; Heart Failure; Hematocrit; Humans; Male; Middle Aged; Pulmonary Heart Disease; Pyrazines; Thromboxane B2

Thirty two rabbits were equally divided at random into 4 groups: A. control; B. E.coli; C. E.coli + ibuprofen; D. E.coli + tetramethylpyrazine. The plasma concentration of 6-keto-PGF1 alpha and TXB2, arterial blood gas as well as platelet aggregability were measured and the pathological changes of lung tissue were observed. The results suggest that TXA2 and PGI2 do take part in the pathogenesis of acute lung injury; that PGI2 may serve as an indicator in the evaluation of the degree of injury in the pulmonary endothelial cells and may also contribute to septic shock; and that both tetramethylpyrazine and ibuprofen possess therapeutic effects on the amelioration of acute lung injury, and the former is rather stronger than the latter in the inhibitory effect on granulocytic sequestration within the lung.

Topics: 6-Ketoprostaglandin F1 alpha; Animals; Escherichia coli Infections; Lung; Lung Diseases; Male; Platelet Aggregation; Platelet Aggregation Inhibitors; Pyrazines; Rabbits; Thromboxane B2