Design, synthesis and antiplatelet aggregation activity of 3-acetyl-7-hydroxycoumarin derivatives / 中国药科大学学报

@#Abstract: In order to search for coumarin-based anti-platelet aggregation compounds with high efficacy and good druggability, twenty-five 3-acetyl-7-hydroxy-coumarin oxime derivatives (6a-6y) were synthesized via Vilsmeier-Haack reaction, Knoevenagel reaction, Williamson reaction, electrophilic substitution reaction and oximation reaction from resorcinol. Their structures were confirmed by HRMS and 1H NMR spectra. The anti-platelet aggregation activity of the target compounds was evaluated using Born’s turbidimetric method. The results revealed that most of them could significantly inhibit platelet aggregation induced by adenosine diphosphate (ADP), collagen, arachidonic acid (AA) and thrombin. Among them, the target compounds 6a and 6b not only had strong inhibitory activity on platelet aggregation induced by the four inducers, but also exhibited good water solubility (3.46 mg/mL and 3.85 mg/mL, respectively) and lipid-water partition coefficient (2.56 and 2.85, respectively) and were expected to become a preclinical candidate compound with multi-target action against platelet aggregation.

High on-treatment platelet reactivity in patients with ischemic stroke or transient ischemic attack / 国际脑血管病杂志

Antiplatelet drugs are the cornerstone of long-term treatment and secondary prevention for ischemic stroke/transient ischemic attack (TIA) recommended by guidelines, aimed at reducing the risk of recurrent stroke and other cardiovascular events. However, some patients with ischemic stroke/TIA may still experience ischemic events during antiplatelet therapy, known as high on-treatment platelet reactivity (HTPR), which typically occurs in patients taking aspirin or clopidogrel. This article elaborates the incidence, risk factors, and commonly used evaluation methods of HTPR in patients with ischemic stroke/TIA, and elucidates the clinical significance of HTPR in patients with ischemic stroke/TIA, and investigates the antiplatelet treatment protocol of patients with HTPR.

Novedades de las guías de la Sociedad Europea de Cardiología 2020 sobre manejo del síndrome coronario agudo sin elevación persistente del segmento ST / News from the European Society of Cardiology 2020 guidelines on the management of acute coronary syndrome without persistent ST-segment elevation / Novidades da Sociedade Europeia de Cardiologia 2020 diretrizes sobre o tratamento da síndrome coronariana aguda sem elevação persistente do segmento ST

Las enfermedades cardiovasculares representan la primera causa de muerte en el mundo. El manejo de los síndromes coronarios ha avanzado formidablemente en los últimos 50 años, reduciendo el riesgo isquémico, a expensas del consiguiente aumento del riesgo hemorrágico. La Sociedad Europea de Cardiología publicó en el año 2020 la guía sobre el manejo de síndrome coronario agudo sin elevación del segmento ST, donde se destacan cambios en los algoritmos de estratificación de riesgo y la terapia antiplaquetaria y anticoagulante como dos de los aspectos principales. En el presente editorial se resumen las principales novedades publicadas en este documento.

Cardiovascular disease is the leading cause of death worldwide. The management of coronary syndromes has advanced dramatically in the last 50 years, reducing ischemic risk, but observing an increase in bleeding risk. The European Society of Cardiology published in 2020 the guideline on the management of acute coronary syndrome without ST-segment elevation, where changes in risk stratification algorithms and antiplatelet and anticoagulant therapy are highlighted as two of the main aspects. This editorial summarizes the main developments published in this document.

A doença cardiovascular é a principal causa de morte em todo o mundo. O manejo das síndromes coronarianas avançou dramaticamente nos últimos 50 anos, reduzindo o risco isquêmico, mas observando um aumento no risco de sangramento. A Sociedade Europeia de Cardiologia publicou em 2020 a diretriz sobre o manejo da síndrome coronariana aguda sem supradesnivelamento do segmento ST, onde as alterações nos algoritmos de estratificação de risco e na terapia antiplaquetária e anticoagulante são destacadas como dois dos principais aspectos. Este editorial resume os principais desenvolvimentos publicados neste documento.

Prevalence of CYP2C19 gene mutations in patients with coronary heart disease and its biological activation effect in clopidogrel antiplatelet response / 中华心血管病杂志

Objective: The purpose of this study was to investigate the effects of CYP2C19 gene mutations on clopidogrel antiplatelet activity in the patients with coronary heart disease treated by percutaneous coronary intervention. Methods: Patients with coronary heart disease, who hospitalized in the Second Affiliated Hospital of Nanchang University from March 2011 to June 2019, and healthy individuals with matching genetic background, gender, and age as controls were included in this study. Basic clinical data were analyzed and blood samples of all research subjects were obtained for extraction of DNA, and Sanger first-generation sequencing method was used to detect CYP2C19 gene mutation from full exon and exon and intron junction. CYP2C19 gene variations in patients with coronary heart disease were compared with the 1000 Genomes Browse database and the sequencing results of healthy controls to determine whether the gene variation was a genetic mutation or a genetic polymorphism. After that, PolyPhen-2 prediction software was used to analyze the harmfulness of gene mutations to predict the effect of mutations on protein function. The same dose of CYP2C19 wild-type plasmid and the CYP2C19 gene mutant plasmids were transfected into human normal liver cells HL-7702. After transfection of 24 h, the expression of CYP2C19 protease in each group was detected. The liver S9 protein was incubated with clopidogrel, acted on platelets to detect the platelet aggregation rate and the activity of human vasodilator-activated phosphoprotein (VASP). Results: A total of 1 493 patients with coronary heart disease (59.36%) were enrolled, the average age was (64.5±10.4) years old, of which 1 129 were male (75.62%). Meanwhile, 1 022 healthy physical examination volunteers (40.64%) were enrolled, and the average age was (64.1±11.0) years old, of which 778 were male (76.13%). A total of 5 gene mutations of CYP2C19 gene were identified in 12 patients (0.80%), namely, 4 known mutations T130K (1 case), M136K (6 cases), N277K (3 cases), V472I (1 case) and one new mutation G27V (1 case), no corresponding gene mutation was found in healthy controls. It was found that T130K and M136K were probably damaging, G27V was possibly damaging, and N277K and V472I were benign mutations. In vitro, we demonstrated that the platelet aggregation rate of the M136K gene mutation group was 24.83% lower than that of the wild type (59.58% vs. 34.75%; P<0.05), and the phosphorylated VASP level was 23.0% higher than that of the wild type (1.0 vs. 1.23; P<0.05). However, the platelet aggregation rate and phosphorylated VASP level were similar between of G27V, T130K, N277K, V472I gene mutation groups and wild type group (P>0.05). Conclusions: In this study, 5 gene mutations are defined in patients with coronary heart disease, namely G27V, T130K, M136K, N277K, V472I. In vitro functional studies show that CYP2C19 gene mutation M136K, as a gain-of-function gene mutation, can enhance the activation of CYP2C19 enzyme on clopidogrel, thereby inhibiting the platelet aggregation rate.

Analysis of the efficacy of tirofiban in the treatment of transient ischemic attack with high risk of recurrence / 中风与神经疾病杂志

@#Objective　To investigate the efficacy of tirofiban on transient ischemic attack with high risk of recurrence.Methods　156 patients with non-cardiogenic transient ischemic attack with ABCD2 score ≥ 4 points were hospitalized at the Department of Neurology,Sinopharm Tongmei General Hospital from Jan 2019 to Mar 2021.Eight patients were excluded due to incomplete data or drop-off from follow-up.The remaining 148 patients were randomly divided into two groups,78 in the observation group and 70 in the control group.The observation group was given tirofiban treatment (loading tirofiban via a micropump,and continuous intravenous pumping for 48 hours) and intensive lipid-lowering therapy.The control group was given intensive anti-platelet aggregation therapy with Aspirin enteric-coated tablets,hydroclopidogre and intensive lipid-lowering therapy.We made a comparative analysis between two groups about efficacy,safety and short-term stroke incidence.Results　In the observation group,57 cases were cured,14 cases were effective,and 7 cases were ineffective;6 cases (7.69%) had a stroke (cerebral infarction) within 7 days,7 cases (8.97%) had a stroke within 30 days,and 7 cases (8.97%) had a stroke within 90 days.In the control group,39 cases were markedly effective,15 cases were effective,and 16 cases were ineffective;in the control group,13 cases (18.57%) had a stroke (cerebral infarction) within 7 days,15 cases (21.43%) had a stroke within 30 days,16 cases (22.86%) had a stroke within 90 days.No intracerebral hemorrhage occurred in either group within 90 days.The two groups had statistical significance in terms of effective treatment rate (P<0.05).However,there was no significant difference in the number of stroke cases between the observation group and the control group in the short-term 7 days,30 days,and 90 days (P>0.05).There was no significant difference in coagulation,platelet,liver and kidney function between the two groups after 48 hours of treatment (P>0.05).Conclusion　For patients with transient ischemic attack at high risk of recurrence,tirofiban treatment can effectively control TIA attacks,but it cannot reduce the risk of stroke.

Review of studies on Bulbine natalensis Baker (Asphodelaceae): Ethnobotanical uses, biological and chemical properties

Bulbine natalensis Baker is a native succulent herb that belongs to the family Asphodelaceae, and is regarded asprecious, highly valued, and extensively used throughout the continent for medicinal purposes and in treating maleimpotency due to the aphrodisiac and invigorating effect. This study reviews the status of B. natalensis ethnobotanicaluses, biological and chemical properties. This review was conducted from April 2019 to February 2020 by applyingthe mixed-method review approach, and in the framework of a complete description of B. natalensis species, dataon morphology, distribution, and economic importance were discussed. Pharmacological screening reported thatB. natalensis possesses anti-inflammatory and broad-spectrum antimicrobial properties. The bulbous plant vapourcontains substances such as tannins, anthraquinones, cardiac glycosides, saponins, and alkaloids. Scientific evaluationsfrom various researchers have substantiated the use of B. natalensis in the enhancement of male sexual disorders, cureof wounds, rashes, itches, ringworm, diabetes, rheumatism, cracked lips and herpes, diarrhea, and paroxysms amongother diseases.

Advances in pharmacological effects of higenamine on cardiovascular system / 药学学报

Higenamine (HG) is an active cardiotonic component isolated from Aconite. Chinese and foreign scholars have done a lot of research on the metabolism and pharmacological effects of HG, which confirmed that it has cardiovascular pharmacological effects of cardiactonic action and vasodilation for the treatment of heart failure and bradycardia, anti-oxidative and anti-apoptotic effects which can be used to protect the heart and reduce heart ischemia and reperfusion injury. In addition, HG inhibits the expression of iNOS mRNA by inhibiting the activity of the transcription factor NF-κB, inhibits the lipopolysaccharide (LPS)-induced NO product, and inhibits platelet aggregation and thrombus formation, thereby improving the experimental septic shock in animals. This article reviews the recent progress in cardiovasular pharmacology of HG, which will contribute to the further development and clinical application of it in the future.

Design, synthesis, and neuroprotective and anti-platelet aggregation research of 3-n-butylphthalide derivatives / 药学学报

Butylphthalide and ferulic acid exhibit excellent therapeutic effects in ischemic stroke. In this research, twelve 3-n-butylphthalide derivatives were designed by molecular hybridization strategy. The target compounds were obtained by nucleophilic substitution, reduction reaction, esterification reaction and elimination reaction, and the structure was confirmed by 1H NMR, 13C NMR and ESI-MS. All compounds were evaluated for neuroprotective activity against OGD/R-induced neurotoxicity in rat cortical neurons by MTT assay. The compounds with the best neuroprotective activity were biologically evaluated for their ability to inhibit platelet aggregation induced by arachidonic acid (AA) and adenosine diphosphate (ADP) via the Bron method．The results indicate that 7b exhibited potent neurocyte protective activity as well as prominent anti-platelet aggregation activity. Compound 7b has potential to be developed as a drug for ischemic stroke.

Design, synthesis, and biological evaluation of ligustrazine/resveratrol hybrids as potential anti-ischemic stroke agents / 中国天然药物

To search for potent anti-ischemic stroke agents, a series of tetramethylpyrazine (TMP)/resveratrol (RES) hybrids 6a-t were designed and synthesized. These hybrids inhibited adenosine diphosphate (ADP)- or arachidonic acid (AA)-induced platelet aggregation, among them, 6d, 6g-i, 6o and 6q were more active than TMP. The most active compound 6h exhibited more potent anti-platelet aggregation activity than TMP, RES, as well as positive control ticlopidine (Ticlid) and aspirin (ASP). Furthermore, 6h exerted strong antioxidative activity in a dose-dependent manner in rat pheochromocytoma PC12 cells which were treated with hydrogen peroxide (HO) or hydroxyl radical (·OH). Importantly, 6h significantly protected primary neuronal cells suffered from oxygen-glucose deprivation/reoxygenation (OGD/R) injury, comparable to an anti-ischemic drug edaravone (Eda). Together, our findings suggest that 6h may be a promising candidate warranting further investigation for the intervention of ischemic stroke.

Anti-platelet aggregation mechanism of Xixian Tongshuan Preparation based on molecular simulation methods / 中国中药杂志

The thrombus is a deposit that is formed on the surface of the endovascular or at the site of repair,and known as the main complication of cardiovascular disease and the cause of death. At the same time,thrombus is mainly treated by the following three ways: anticoagulation,anti-platelet aggregation and thrombolysis. In this study,the chemical constituents of seven traditional Chinese medicines in the Xixian Tongshuan Preparation were collected to construct a component database. Subsequently,the pharmacophore were used to screen out the component database,and molecular docking was used to screen out the results of pharmacophore for explaining the material basis and mechanism that Xixian Tongshuan Preparation exerts anti-thrombotic activity by inhibiting platelet aggregation. First of all,P2 Y12,GPⅡb/Ⅲa and PAR1 were selected as study vectors,the optimal models of inhibitors were obtained respectively through verification and evaluation of the pharmacophore models. Afterwards,the component database was screened out by the optimal pharmacophore models of PAR1,P2 Y12 and GP Ⅱ b/Ⅲ a,and the molecular docking method was used to further refine the screening results. The screening results indicated that the anti-platelet aggregation effect of Xixian Tongshuan Preparation was correlated with the inhibition of P2 Y12,PAR1 and GPⅡb/Ⅲa expressions with saffower yellower,hirudin and candidin and notoginseng triterpenes,folinic acid,respectively. The material basis and mechanism of anti-platelet aggregation of Xixian Tongshuan Preparation provided a theoretical basis for the clinical use of the preparation and the lead compounds for the development of anti-platelet aggregation drugs.

Measurement of antiplatelet aggregation and potency of hirudo / 药学学报

The objective of this work was to develop a bioassay to quantify the antiplatelet aggregation activity of hirudo for quality evaluation and control. Antithrombin activity of hirudo extracted by high temperature decoction was determined by thrombin titration. Antiplatelet aggregation activity of hirudo was determined through pharmacodynamic experiments in vitro and in vivo using a bioassay we developed for quantifying inhibition of platelet aggregation. Methodological investigation was carried out and the titers of 12 batches of hirudo samples were determined. During the experiment, the disposal of animals is in accordance with the ethical standards of animal experiments. The results showed that the antithrombin activity of hirudo decocted at high temperature decreased significantly and almost lost its activity. Hirudo inhibited platelet aggregation and results in vivo and in vitro were consistent. These assays were employed to test 12 batches of hirudo. The results demonstrated that the biopotency of 12 batches was 113.49, 96.13, 121.22, 127.33, 83.48, 108.72, 131.41, 127.95, 76.90, 126.27, 132.89 and 573.53 U·mg-1. The method was reliable and reproducible and can be used to assess the quality of hirudo.

Chemical constituents from a Tibetan herbal medicine Corydalis hendersonii / 中国中药杂志

Nine alkaloids and two phenolic glycosides were isolated from EtOH extract of the whole plants of Corydalis hendersonii by various chromatographic techniques including silica gel, ODS, Sephadex LH-20, and semi-preparative HPLC. Their structures were identified as groenlandicine (1), berberine (2), protopine (3), cryptopine (4), N-trans-feruloyloctopamine(5), 3-(4-hydroxy-3-methoxyphenyl)-N-[2-(4-hydroxyphenyl)-2-methoxyethyl] acrylamide (6), N-cis-p-coumaroyloctopamine (7), N-trans-p-coumaroylnoradrenline (8),N-cis-feruloyloctopamine (9), apocynin (10), and glucoacetosyringone (11) by the spectroscopic data analysis and comparison with those in the literature. Among them, compounds 10 and 11 were isolated from this genus for the first time, and 1, 2, and 5-9 were isolated from the species for the first time. All isolates were tested for their protection for in vitro PC12 cell line and antiplatelet aggregation activity. The results showed that compounds 5 and 7 displayed protective effects at a concentration of 10 μmol·L⁻¹, and compound 2 showed antiplatelet aggregation activity induced by THR, ADP, and AA, and compound 3 exhibted inhibitory effect induced by THR.

Anti-platelet Aggregation Activity of Ergosterol in Vitro / 医药导报

Objective To evaluate the anti-platelet aggregation effect of ergosterol in vitro and explore the preliminary mechanism. Methods The anti-platelet aggregation activity of ergosterol was assessed in vitro on rabbit platelet aggregation. Different inducers, ADP ( 4 μmol?L-1 ) , collagen ( 4 μg?mL-1 ) , arachidonic acid ( AA, 1 mmol?L-1 ) and thrombin (0.5 U?mL-1), and blockers (ozagrel, dipyridamole, clopidogrel and aspirin) were applied to observe the potential targets of ergosterol, platelet aggregation induced by ADP (0, 1, 2, 4, 6μmol?L-1) or fibrinogen (0, 1, 2, 4, 6, 10 mg?mL-1). Results Ergosterol exhibited an obvious anti-platelet aggregation effect in vitro with IC50 values on different inducers ( ADP, collagen, AA and thrombin) of (19.3±0.8), (23.4±1.2), (26.7±0.7), (32.9±1.5) μmol?L-1, respectively. Conclusion Ergosterol can significantly inhibit aggregation and activation of platelet. It provides experimental basis for full exploration of ergosterol and development of novel anti-platelet aggregation drugs.

Antiplatelet aggregation bioactivity of Polygoni Multiflori Radix with chemical fingerprints and spectrum-effect correlation analysis / 中国中药杂志

To explore the active substance of antiplatelet aggregation of Polygoni Multiflori Radix by using chemical fingerprints and antiplatelet aggregation bioactivity test for spectrum-effect correlation analysis. The Polygoni Multiflori Radix was tested by antiplatelet aggregation in vitro, and the results showed that 50% aqueous ethanol extract of Polygoni Multiflori Radix had more potent antiplatelet aggregation effect than 10% or 90% aqueous ethanol extract, and ultrasonic extraction was superior to refluxing extraction in the aspect of antiplatelet aggregation. The antiplatelet aggregation bioactivity of the different Polygoni Multiflori Radix extracts was evaluated and the results showed that the inhibition rate was 32.03%-74.56%. Spectrum-effect correlation analysis indicated that trans-stilbene glucoside, cis-stilbene glucoside and catechinic acid had higher correlation coefficient and they were 0.963 (P<0.01), 0.902 (P<0.01) and 0.656 (P<0.05) respectively; furthermore, all of the above three compounds demonstrated significant antiplatelet aggregation bioactivities. Considering their content difference in Polygoni Multiflori Radix, we calculated the relative active contributions, and the results suggested that trans-stilbene glucoside was the main active substance of Polygoni Multiflori Radix in the aspect of antiplatelet aggregation in vitro.

Anti-platelet Aggregation Activity of Ergosterol in Vitro / 医药导报

Objective To evaluate the anti-platelet aggregation effect of ergosterol in vitro and explore the preliminary mechanism. Methods The anti-platelet aggregation activity of ergosterol was assessed in vitro on rabbit platelet aggregation. Different inducers, ADP ( 4 μmol?L-1 ) , collagen ( 4 μg?mL-1 ) , arachidonic acid ( AA, 1 mmol?L-1 ) and thrombin (0.5 U?mL-1), and blockers (ozagrel, dipyridamole, clopidogrel and aspirin) were applied to observe the potential targets of ergosterol, platelet aggregation induced by ADP (0, 1, 2, 4, 6μmol?L-1) or fibrinogen (0, 1, 2, 4, 6, 10 mg?mL-1). Results Ergosterol exhibited an obvious anti-platelet aggregation effect in vitro with IC50 values on different inducers ( ADP, collagen, AA and thrombin) of (19.3±0.8), (23.4±1.2), (26.7±0.7), (32.9±1.5) μmol?L-1, respectively. Conclusion Ergosterol can significantly inhibit aggregation and activation of platelet. It provides experimental basis for full exploration of ergosterol and development of novel anti-platelet aggregation drugs.

Comparison of Preventive Effects and Safety of Aspirin and Clopidogrel Respectively Used for Vascular Re-stenosis after Coronary Intimal Stripping with Coronary Artery Bypass Grafting / 中国药房

OBJECTIVE:To compare the preventive effects and safety of aspirin and clopodogrel respectively used for vascular restenosis after coronary intimal striping with coronary artery bypass grafting. METHODS:110 patients with coronary atherosclerot-ic heart disease were divided into aspirin group (55 cases) and clopodogrel group (55 cases). All patients intravenously mi-cro-pumped Nitroglycerin injection 10 mg+5% Glucose injection totally 20 mL for maintaining 48-72 h after coronary intimal strip-ing with coronary artery bypass grafting,intravenously pumped Dopamine hydrochloride injection 1-5 μg/kg if necessary. Unplug the endotracheal tube after surgery,patients received Cefuroxime sodium for injection 1.5 g adding into Sterile water for injection 50 mL,intravenous injection,3 times a day,for 2-3 d. Meanwhile,patients were orally given Rosuvastatin calcium tablet 10 mg 30 min after daily dinner,8-week was a course,for 3 courses. Based on it,aspirin group received Aspirin enteric-coated tablet with initial dose of 300 mg,once a day,orally taking 100 mg from the second day,once a day,for 6 months;clopodogrel group received Clopidogrel hydrogen sulfate tablet with initial dose of 300 mg,once a day,orally taking 75 mg from the second day, once a day,for 6 months. Graft patency rate,and platelet aggregation rate,platelet aggregation compliance rate,fibrinogen(Fg), D-dimer (D-D),platelet count (PLT),tissue-type plasminogen activator (t-PA) before and after treatment,and the incidence of adverse reactions in 2 groups were observed. RESULTS:There were no significant differences in the graft patency rate and inci-dence of adverse reactions in 2 groups (P>0.05). Before treatment,there were no significant differences in platelet aggregation rate,platelet aggregation compliance rate,Fg,D-D,PLT and t-PA in 2 groups (P>0.05). After treatment,platelet aggregation rate,Fg and D-D level in 2 groups were significantly lower than before,platelet aggregation compliance rate,PLT and t-PA level were significantly higher than before,with statistical significance(P0.05). CONCLUSIONS:Based on conventional treatment,both aspirin and clopidogrel used for coronary intimal strip-ing with coronary artery bypass grafting can inhibit platelet aggregation,reduce thrombosis,maintain vascular patency and prevent vascular restenosis,with good safety.

Inhibition of piperlongumine on platelet aggregation and blood coagulation for children in vitro study / 国际检验医学杂志

Objective To observe the inhibition of piperlongumine in vitro on platelet aggregation and blood coagulation tests for children,to provide the experimental basis for clinical medication.Methods Venous blood samples from 30 children were randomly devided into 5 groups,and was centrifuge to separate platelet-rich plasma (PRP).After storing in 37 ℃ thermostat water bath for 5 minutes,the PRP which have been added DMSO as blank group,and added Aspirin (10 μmol/L)as control group,and added PL (20 μmol/L),PL(100 μmol/L),PL(200 μmol/L) as different concentrations of PL groups respectively,were induced by the addition of adenosine diphosphate (10 μmol/L),collagen(2.5 μg/mL) and the arachidonic acid(500 μg/mL).Then the platelet aggregation rate of the PRP from 5 groups could be measured by turbidimetry.Blood plasma isolated from venous blood was divided into 5 groups.In the PL groups,blood plasma were mixed up with PRP concentrations of which were 5,10,20 μmol/L.In the bland group,blood plasma were mixed up with DMSO (1％).In the control group,blood plasma were mixed up with heparin sodium(35 U/mL).After storing in 37 ℃ thermostat water bath for 5 minutes,fibrinogen(FIB),prothrombin time(PT),thrombin time(TT) and activated partial thromboplastin time of different groups were detected.Results Compared to the control group,the groups which were add PL with different concentrations (20,100,200 μmol/L) showed significant inhibition on platelet aggregation induced by AA and collagen(P<0.05).PL with concentrations of 100 μmol/L and 200 μmol/L showed significant inhibition on platelet aggregation induced by ADP(P<0.05).The PT,APTT,TT of blood plasma from children had been significantly prolonged by the intervention of PL 10 μmol/L and PL 20 μmol/L(P<0.05),however,no significant change of FIB was observed.Conclusion There are inhibitory effects of PL on platelet aggregation of blood plasma from children and anticoagulant activity in this study.

Design, synthesis, and biological evaluation of phenylpropenamides compounds as anti-platelet aggregation / 药学学报

Twenty phenylpropenamide analogs with structural novelty were designed and synthesized upon pharmacophore-combination strategy. The structures of target compounds were elucidated by IR, 1H NMR, 13C NMR and MS, and all the target compounds were biologically evaluated for the inhibitory activities of platelet aggregation induced by adenosine diphoshate (ADP) and (AA) arachidonic acid via Bron method. As a result, compounds 6b, 9b, 9d and 9h demonstrated potent inhibitory activity against platelet aggregation induced by AA. Meanwhile, compounds 6b, 6d, 6j, 9b and 9g exhibited significant suppression of platelet aggregation induced by ADP.

Analysis of clinical symptoms and influencing factors of anti-platelet aggregation drugs in patients with upper gastrointestinal bleeding / 中国生化药物杂志

Objective To analysis of clinical symptoms and influencing factors of anti-platelet aggregation drugs in patients with upper gastrointestinal bleeding.Methods Using the research methods of retrospective analysis, collected 110 cases of gastrointestinal bleeding patients from June 2012 to June 2015 into the first affiliated hospital of xiamen university,and divided into two groups,the control group,79 patients were treated without antiplatelet aggregation drugs,the experimental group,31 patients were treated with single antiplatelet aggregation drug.observed the degree of gastrointestinal bleeding,the mode of bleeding, and the characteristics of endoscopic findings between two groups,according to the age,INR, and the type of drug taken, the clinical symptoms and influencing factors of the patients were analyzed further.Results The rate of gastrointestinal bleeding was significantly higher in the experimental group than in the control group(P3 had a significantly higher rate of gastrointestinal bleeding than patients with INR<3.Conclusion Anti-platelet aggregation drugs can significantly increase the chance of serious bleeding in the digestive tract,the patient's age, INR value and the type of medication can affect the incidence of gastrointestinal bleeding;long-term use of these drugs lead the most serious impact on the duodenum, can lead to the site intestinal mucosa damage,with the increasing age of patients,adverse reactions of the digestive tract increased.

Synthesis and biological evaluation of novel chalcone aromatic oxygen alkyl acids compounds / 药学学报

Six novel ligustrazine chalcone aromatic oxygen alkyl acids compounds and two pyridine chalcone aromatic oxygen alkyl acids ester compounds were synthesized according to the traditional Chinese medicine theory removing blood stasis. The structures of target compounds were identified by IR, NMR and ESI-MS. The inhibitory activities of platelet aggregation induced by adenosine diphosphate (ADP) and arachidonic acid (AA) were measured by the liver microsomal incubation method in vitro. Hypolipidemic activities of compounds were tested in vivo for better inhibitory activities of platelet aggregation. Preliminary pharmacological results showed that compounds 7c, 8a and 11a had potent inhibitory activity against platelet aggregation induced by AA, compounds 7c, 7d, 8a and 11b showed significant inhibitory activity against platelet aggregation induced by ADP. Compounds 7c and 8a exhibited good hypolipidemic activities in high-fat-diet (HFD) induced hyperlipidemia C57/BL6 mice and worthy for further investigation.