AIM: The fruits of Lagenaria siceraria (Molina) Standl. (Cucurbitaceae), a commonly used vegetable, are reported to possess various medicinal properties. In previous studies, the fibrinolytic potential of an ethanolic extract of fruits of Lagenaria siceraria was investigated in comparison with kaempferol isolated from it. The aim of the present study was to explore its mechanistic antithrombotic potential and antiplatelet activity using a wide dose range in different in vitro and in vivo models, and to quantify the total phenolic, flavonoid, and kaempferol contents using a colorimetric method. METHOD: The antithrombotic potential was investigated using tail bleeding time in mice, a plasma recalcification assay, and pulmonary thromboembolism in mice. The antiplatelet activity was studied using an in vitro model to investigate IC50 value. RESULTS: A significant amount of total phenols, flavonoids, and kaempferol was quantified in L. siceraria ethanolic extract. An ethanolic extract of the fruits of L. siceraria showed a significant increase in tail bleeding time and plasma recalcification time, significant protection against ADP induced pulmonary thromboembolism in mice, and also inhibited the platelet aggregation induced by ADP in vitro. The study suggested that the fruits of L. siceraria exhibit significant antithrombotic potential due to inhibition of ADP-mediated platelet aggregation and the involvement of various non-cellular chemical mediators of blood. CONCLUSION This finding may be helpful in treating the serious consequences of the thrombus formed in blood vessels which include atherothrombotic diseases, such as myocardial or cerebral infarction. So, further investigation should be done for revealing exact mechanism of action behind these types of activities.
Adenosine Diphosphate ; Animals ; Calcium ; blood ; Cucurbitaceae ; chemistry ; Female ; Fibrinolytic Agents ; analysis ; pharmacology ; therapeutic use ; Fruit ; Goats ; Kaempferols ; analysis ; pharmacology ; therapeutic use ; Male ; Mice ; Phytotherapy ; Plant Extracts ; chemistry ; pharmacology ; therapeutic use ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; analysis ; pharmacology ; therapeutic use ; Polyphenols ; analysis ; pharmacology ; therapeutic use ; Pulmonary Embolism ; blood ; chemically induced ; drug therapy ; Rats, Wistar ; Thrombosis ; prevention & control

OBJECTIVE: To evaluate correlation between and agreement in light transmittance aggregation (LTA) and thromboelastography (TEG) in laboratory diagnosing aspirin resistance (AR), and to determine the prevalence of AR in old patients. METHODS: Patients in the Wanshoulu District of Beijing with ischemic atherothrombotic diseases were recruited. Inclusion criteria were age ≥ 65 years, and having received regular aspirin therapy (75-100 mg daily) for at least 4 weeks. On the basis of LTA assay, the definition of AR was taken as aggregation of ≥ 20% with AA (arachidonic acid), and of ≥ 70% with ADP (adenosine diphosphate). Aspirin-sensitivity was indicated by the absence of either of these criteria; aspirinsensitivity was indicated as both criteria being met. The definition of AR by TEG is ≥ 50% via AA-induced whole blood aggregation. RESULTS: There were 13.69% prevalence of aspirin resistance for LTA using AA as the agonist, 30.16% prevalence of aspirin resistance for LTA using ADP as the agonist, and 23.67% prevalence of aspirin resistance for TEG using AA as the agonist. Results from these tests showed poor agreement (Kappa<0.4). However, by the method of LTA using AA and ADP as the agonists, prevalence of AR was 8.35%. By methods of AA-induced LTA and AA-induced TEG, prevalence of AR was 8.82%. Results from these two latter methods showed good agreement (Kappa = 0.793). CONCLUSION Combined methods, as described here, have good correlation and agreement in the assays of AR, and the results with them represent a realistic measure of the prevalence of AR. Prevalence of AR of elderly patients from Wanshoulu district of Beijing is about 9%.
Aged ; Aspirin ; pharmacology ; therapeutic use ; Cerebrovascular Disorders ; blood ; drug therapy ; Coronary Disease ; blood ; drug therapy ; Drug Resistance ; Female ; Humans ; Male ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; pharmacology ; therapeutic use ; Prevalence ; Surveys and Questionnaires

Since the late 1980s, low dose aspirin has been used to prevent stroke and ischemic heart disease. However, prophylactic effect of antiplatelets against venous thromboembolism (VTE), in patients who undergo hip fracture surgery (HFS) is controversial. Our purpose was to determine the incidence of symptomatic VTE after HFS and to evaluate whether antiplatelets reduce the development of symptomatic VTE following HFS. We retrospectively reviewed 858 HFS in 824 consecutive patients which were performed from May 2003 to April 2010 at an East Asian institute. We compared the incidence of symptomatic VTE in antiplatelet users and non-users using multivariate logistic regression analyses. Overall incidences of symptomatic pulmonary embolism including fatal pulmonary embolism, and symptomatic deep vein thrombosis in this study were 2.4% (21/858), and 3.5% (30/858), respectively. The incidence of symptomatic VTE was 4.8% (12/250) in antiplatelet users and 4.3% (26/608) in non-users (P = 0.718). It is suggested that antiplatelet agents are not effective in prevention of symptomatic VTE after HFS.
Adolescent ; Adult ; Aged ; Aged, 80 and over ; Anticoagulants/therapeutic use ; Aspirin/administration & dosage/pharmacology/*therapeutic use ; Female ; Hip Fractures/complications/*surgery ; Humans ; Male ; Middle Aged ; Multivariate Analysis ; Platelet Aggregation Inhibitors/*therapeutic use ; Postoperative Complications/drug therapy/*epidemiology/*prevention & control ; Regression Analysis ; Venous Thromboembolism/complications/*epidemiology/*prevention & control

OBJECTIVETo evaluate the effificacy of dual antiplatelet therapy combined with Naoxintong Capsule ([see text], NXTC) in a rat model of coronary microembolization (CME).

METHODSA total of 95 rats were randomly divided into 6 groups: control, sham-operation, CME model, NXTC, dual antiplatelet (clopidogrel and aspirin) intervention (DA), and NXTC combined with DA (NDA) groups. The complete data in 69 rats were obtained. The number of CME, myocardial apoptosis rate, bleeding time, clotting time, and adensosine diphosphate (ADP)-induced platelet aggregation were assessed.

RESULTSCompared with the CME group, the number of CME and myocardial apoptosis rates were signifificantly decreased in the NXTC, DA, and NDA groups (P <0.01). Compared with other intervention groups, the number of CME and myocardial apoptosis rates were the least in the NDA group (P <0.01), and the incidence of surgical bleeding was the highest in the DA group (P <0.01). Compared with the CME group, ADP-induced maximum platelet aggregation rate was significantly inhibited in the NXTC, DA, and NDA groups (P <0.01), both bleeding time and clotting time were signifificantly increased in the NXTC, DA, and NDA groups (P <0.01), while the above parameters were the highest in the DA group (P <0.05).

CONCLUSIONThe combination therapy of NXTC and DA enhanced the anti-CME effect of either therapy alone and reduced the risk of the DA therapy-associated bleeding, demonstrating an improved benefifit/ risk ratio in the rat model of CME.

Animals ; Apoptosis ; drug effects ; Blood Coagulation ; drug effects ; Blood Loss, Surgical ; physiopathology ; Capsules ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Embolism ; complications ; drug therapy ; pathology ; physiopathology ; Male ; Myocardium ; pathology ; Platelet Aggregation Inhibitors ; pharmacology ; therapeutic use ; Rats ; Rats, Sprague-Dawley ; Survival Analysis ; Thrombosis ; complications ; drug therapy ; pathology ; physiopathology

BACKGROUNDAspirin is widely used in the secondary prevention of coronary artery diseases, including myocardial infarction, stroke, and vascular related deaths. However, the antiplatelet effect of aspirin appears to be variable and aspirin resistance (AR) is currently still controversial for Chinese patients. The aim of this study was to describe the prevalence of AR, and identify possible risk factors associated with a lack of response to aspirin treatments in patients with unstable coronary artery disease.

METHODSPlatelet function tests with arachidonic acid (ARA) and urinary 11-dehydro-thromboxane B2 (11-DH-TXB2) concentrations were performed in 262 patients with unstable coronary artery disease who had not been taking aspirin before admission. ARA induced platelet aggregation and 11-DH-TXB2 were detected to evaluate the functional and biochemical responses to aspirin before and on days 1, 4, and 10 after aspirin administration. Six-month follow-up was completed in patients who developed AR to evaluate the effect of aspirin in a long-term treatment. GP1Bα (C1018T), Pl (A1/A2), P2Y1 (A1622G), TBXA2R (T924C) were also detected to evaluate the influence of genetic variant on aspirin responsiveness.

RESULTSA total of 8.8% of patients were indentified as AR at the first day after aspirin treatment. The level of urine 11-DH-TXB2 in the AR group was higher compared to non-AR group (P < 0.05). There was no relationship between ARA induced platelet aggregation and urinary 11-DH-TXB2 levels (r = 0.038, P = 0.412). The results of DNA sequencing showed that TBXA2R-924TT homozygotes had a significantly high rate of AR. Logistic regression demonstrated that diabetes was an independent risk factor of AR.

CONCLUSIONSIn the beginning period of administration, aspirin was not a sufficient factor that inhibits platelet aggregation. TBXA2R-924T allele was involved in AR. Diabetes was an independent risk factor of AR.

Aged ; Aged, 80 and over ; Arachidonic Acid ; pharmacology ; Aspirin ; therapeutic use ; Coronary Artery Disease ; drug therapy ; genetics ; Diabetes Mellitus, Type 2 ; Female ; Genotype ; Humans ; Male ; Membrane Glycoproteins ; genetics ; Middle Aged ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; therapeutic use ; Platelet Function Tests ; Platelet Glycoprotein GPIb-IX Complex ; Polymerase Chain Reaction ; Polymorphism, Genetic ; genetics ; Receptors, Purinergic P2Y1 ; genetics ; Receptors, Thromboxane A2, Prostaglandin H2 ; genetics ; Thromboxane B2 ; analogs & derivatives ; urine

OBJECTIVETo evaluate the impact of different proton pump inhibitors on the antiplatelet activity of clopidogrel.

METHODSA total of 60 hospitalized patients undergoing percutaneous coronary intervention were randomly assigned to receive omeprazole group 40 mg/d (20 patients), pantoprazole group 40 mg/d (20 patients) and control group (20 patients). All patients also received standard clopidogrel therapy, continuing 30 days treatments. The percentage clotting inhibition was measured by the use of thrombelastogram and the maximal platelet aggregation rate (MPAR) was measured by turbidity method at the first day before admission and 15 or 30 days after treatment. Major adverse cardiac and cerebral events (MACCE) and hemorrhagic events within 30 days were recorded.

RESULTSThe baseline clinical characteristics, angiography and PCI result were compared among the three groups. At the first day before admission and 15 or 30 days after treatment, no significant difference was shown in the percentage clotting inhibition measured by thrombelastogram and the maximal platelet aggregation rate (MPAR) measured by turbidity method among the three groups. Though the platelet agglutination inhibition rate measured at 15 and 30 days increased and MPAR measured at 15 and 30 days declined compared with the baseline data (P < 0.05), no significant difference was found between levels measured at 15 and 30 days (P > 0.05). The rates of MACCE had no significant difference among the three groups. Compared with control group, the rates of hemorrhagic event were significantly decreased in omeprazole or pantoprazole group (P < 0.05), but no significant difference was shown between the omeprazole and pantoprazole group.

CONCLUSIONNo significant impact of different proton pump inhibitors on the antiplatelet activity of clopidogrel has been found in patients undergoing coronary stent implantation and short-time combined administration is safe.

2-Pyridinylmethylsulfinylbenzimidazoles ; pharmacology ; therapeutic use ; Adult ; Aged ; Angioplasty, Balloon ; Aspirin ; pharmacology ; therapeutic use ; Coronary Disease ; therapy ; Drug Therapy, Combination ; Female ; Humans ; Male ; Middle Aged ; Omeprazole ; pharmacology ; therapeutic use ; Platelet Aggregation ; drug effects ; Postoperative Period ; Proton Pump Inhibitors ; pharmacology ; therapeutic use ; Stents ; Ticlopidine ; analogs & derivatives ; pharmacology ; therapeutic use

OBJECTIVETo study the relationships of blood stasis syndrome (BSS), CYP2C19 gene polymorphism with clopidogrel resistance (CR) and post-PCI prognosis.

METHODSMaterials of 415 patients (Han nationality) with coronary atherosclerotic heart disease (CAHD) hospitalized between January 2008 and July 2009 were collected. The CYP2C19*2 gene distribution in patients with different degrees of BBS was observed, and the relationships of BSS, CYP2C19*2 with the laboratory CR [LCR, percentage of patients with ADP-induced maximal platelet aggregation (MPA) rate reduced for < or = 10% after a 10-day clopidogrel treatment] were analyzed. Besides, an assay on the relations of maximal platelet aggregation suppressive rate (MPAS), LCR, recurrent cardiovascular events (RCEs) with BSS and CYP2C19*2 gene mutation was performed in a 7-month (in median) follow-up study on 180 post-PCI patients who received conventional treatment by clopidogrel and aspirin.

RESULTS(1) The frequency of 681G>A mutation in patients with severe BSS and in those who received PCI was higher than that in those with mild BSS (P<0.01); (2) After clopidogrel treatment, LCR was 45.06% (187/415) in total patients, 61.63% (143/232) in patients with severe BSS, 53.24% (115/216) in patients carrying 681A allele; (3) The MPA was less decreased and the LCR was higher in patients with severe BSS than in those with mild BSS (P<0.01); (4) After clopidogrel treatment, the MPA was less decreased and the LCR was higher in carrying CYP2C19 681A allele than in those carrying 681 GG type gene (P<0.01); (5) Follow-up study showed that not only the MPA suppressive rate was lower, LCR was higher in patients with severe BSS or those carrying CYP2C19 681A allele, but a higher RCEs was also shown in them (P<0.01). Moreover, after the various risk factors had been adjusted, the RCEs in patients with severe BSS or carrying CYP2C19 681A allele was higher than in those with mild BSS (OR: 4.01; 95% CI: 1.79-8.99) or carrying GG type gene (OR: 6.89; 95% CI: 2.97-15.97).

CONCLUSIONSevere BSS and CYP2C19*2 gene mutation are associated with LCR, and could increase the risk of post-PCI cardiovascular events recurrence in patients with CAHD.

Aged ; Aryl Hydrocarbon Hydroxylases ; genetics ; Coronary Artery Disease ; therapy ; Cytochrome P-450 CYP2C19 ; Diagnosis, Differential ; Drug Resistance ; Female ; Humans ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Percutaneous Coronary Intervention ; Platelet Aggregation Inhibitors ; pharmacology ; therapeutic use ; Polymorphism, Genetic ; Prognosis ; Ticlopidine ; analogs & derivatives ; pharmacology ; therapeutic use

Ginkgo biloba extract (GBE) is one of the hot spots of drugs extracted from plants recently; it protects brain from ischemia/reperfusion injuries. The mechanism of protective effects includes antioxidation, free radicals clearance, inhibiting the release of excitatory amino acid, anti-inflammation, inhibiting neural apoptosis and other biological effects.
Animals ; Antioxidants ; pharmacology ; therapeutic use ; Brain Ischemia ; complications ; drug therapy ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Ginkgo biloba ; chemistry ; Humans ; Phytotherapy ; Plant Leaves ; chemistry ; Platelet Aggregation Inhibitors ; pharmacology ; therapeutic use ; Reperfusion Injury ; prevention & control

Angioplasty, Balloon, Coronary ; adverse effects ; Aspirin ; pharmacology ; therapeutic use ; Coronary Angiography ; Drug-Eluting Stents ; adverse effects ; Humans ; Male ; Middle Aged ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; pharmacology ; therapeutic use ; Sirolimus ; pharmacology ; therapeutic use ; Ticlopidine ; analogs & derivatives ; pharmacology ; therapeutic use ; Treatment Outcome ; Tyrosine ; analogs & derivatives ; pharmacology ; therapeutic use

Inonotus obliquus has high nutritional and medicinal value, especially in treating malignant tumors, diabetes, cardiovascular disease and AIDS, attracting significant attention from scholars in recent years. In this paper, the biological characteristics, chemical composition and pharmacologic effects of Inonotus obliquus were summarized. And the applications in medicine and food were introduced. Future research on Inonotus obliquus was also discussed in order to make Inonotus obliquus obtain effective exploitation and satisfy people's demands.
Anti-Inflammatory Agents ; chemistry ; pharmacology ; therapeutic use ; Antineoplastic Agents ; chemistry ; pharmacology ; therapeutic use ; Antioxidants ; chemistry ; pharmacology ; therapeutic use ; Antiviral Agents ; chemistry ; pharmacology ; therapeutic use ; Basidiomycota ; chemistry ; Biomedical Research ; trends ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; therapeutic use ; Humans ; Hypoglycemic Agents ; chemistry ; pharmacology ; therapeutic use ; Platelet Aggregation Inhibitors ; chemistry ; pharmacology ; therapeutic use ; Triterpenes ; chemistry ; isolation & purification