1.Chemical constituents from Callicarpa nudiflora and their hemostatic activity.
Jie ZHANG ; Baoquan LI ; Feng FENG ; Yuping TANG ; Wenyuan LIU
China Journal of Chinese Materia Medica 2010;35(24):3297-3301
OBJECTIVETo study the hemostatic effect of chemical constituents from Callicarpa nudiflora.
METHODThe chemical constituents were isolated and purified via silica gel and Sephadex LH-20 column chromatography. Their structures were determined on the basis of spectral analysis. prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT) and fibrinogen (FIB) of the constituents rabbit blood samples were tested with rabbit blood in vitro.
RESULTEleven compounds were isolated and identified as two diterpenens: 7alpha-hydroxy sandaracopimaric acid (1), 16, 17-dihydroxy-3-oxophyllocladane (2). Two phenoic glycosides: acteoside (3), samioside(4). Three triterpenes: 2alpha, 3alpha, 24-trihydroxy-ursa-12-en-28-oic acid (5), 2alpha, 3alpha, 19alpha-trihydroxyursa-12-en-28-oic acid-28-0-beta-D-glucopyranosyl ester (6), and 2alpha, 3alpha, 19alpha, 23-tetrahydroxy-ursa-12-en-28-oic acid-28-0-beta-D-glucopyranosyl ester (7). Four flavones: rhamnazin (8), 5-Hydroxy-3, 7, 4'-trimethoxy-flavone (9) , 5-Hydroxy-3, 7, 3', 4'-tetramethoxyflavone (10), and luteoloside (11). All Compounds cannot significantly shorten the PT (P < 0.01), compounds 3, 4, 7, 10 can remarkedly increase APTT (P < 0.01), compound 5 can prolong the T( P < 0.01) obviously, and compound 8 can significantly increase the contents of FIB (P < 0.01).
CONCLUSIONCompounds 2, 4 and 10 were isolated from this genus for the first time, and compounds 1, 3, 5, 6, 7 and 9 had been isolated from this plant for the first time. The hemostatic effect of C. nudiflora may be related to the activation of the intrinsic blood coagulation system.
Animals ; Blood Coagulation Factors ; metabolism ; Callicarpa ; chemistry ; Hemostasis ; drug effects ; Male ; Organic Chemicals ; analysis ; pharmacology ; Rabbits
3.Study on evaluation system for gynecological disease model characterized by Qi stagnation and blood stasis syndrome with female SD rats.
Wei LI ; Jin-Ao DUAN ; Pei LIU ; Xu-Qin SHI ; Zhen-Hao LI ; Xin-Sheng FAN ; Yong-Qing HUA ; Jian-Ming GUO
China Journal of Chinese Materia Medica 2013;38(8):1211-1218
OBJECTIVETo establish an evaluation system for animal model with gynecological disease characterized by Qi stagnation and blood stasis syndrome, in order to disprove syndrome characteristics of the model by classic clinical prescriptions, and evaluate the specificity and reliability of the model with macroscopic biological signs and symptoms.
METHODThe model characterized by Qi stagnation and blood stasis syndrome was established by injecting adrenaline into female SD rats and conducting unpredictable chronic stimulus such as reversal of day and night, swimming in cold water, thermal stimulation in oven, noise and tail suspension for two weeks. They were also orally administered with Xiangfu Siwu Tang, Shaofu Zhuyu Tang and positive control drug aspirin in groups. A comprehensive evaluation was conducted for the model on the basis of haemorheology, four blood coagulation indexes, four diagnostic information (digital imaging of tongue, paw and tail, temperature, weight, ingestion, electrocardiograph, and open filed test), and syndrome rating.
RESULTCompared with the normal group, the model group showed obvious changes in haemorheology, four blood coagulation indexes, animal behavior, weight, ingestion, syndrome rating and heart rate. Their tongue and paw pictures were analyzed with Photoshop 7.0, showing significant difference in red, green and blue percentage composition from the normal group. Groups given aspirin and Xiangfu Siwu Tang showed notable changes in haemorheology, four blood coagulation indexes, animal behavior, weight, ingestion, heart rate, syndrome rating, and red, green and blue percentage composition in tongue and paw pictures, whereas the group given Shaofu Zhuyu Tang showed no remarkable improvement.
CONCLUSIONThe evaluation system for the animal model with gynecological disease characterized by Qi stagnation and blood stasis syndrome is established to provide reference for studies on the evaluation system for qi stagnation and blood stasis syndrome models.
Animals ; Diagnosis, Differential ; Disease Models, Animal ; Female ; Gynecology ; Hemostasis ; drug effects ; Medicine, Chinese Traditional ; Qi ; Rats ; Syndrome
4.Efficacy, Safety, and Pharmacokinetics of Beroctocog Alfa in Patients Previously Treated for Hemophilia A.
Shin Young HYUN ; Seon Yang PARK ; Soon Yong LEE ; Hoon KOOK ; Sang Hoon PAIK ; In Jin JANG ; Kun Soo LEE
Yonsei Medical Journal 2015;56(4):935-943
PURPOSE: Beroctocog alfa is a second generation recombinant factor VIII manufactured by removing the B-domain from factor VIII. This prospective clinical trial was conducted to evaluate the efficacy, safety, and pharmacokinetics of beroctocog alfa in patients of ages > or =12 years previously treated for severe hemophilia A. MATERIALS AND METHODS: Seventy subjects received beroctocog alfa as an on-demand treatment for acute hemorrhage. RESULTS: The final hemostatic effect was excellent in 35 subjects (50%) and good in 26 subjects (37.1%). The drug showed an overall efficacy rate of 87.1%. The majority of acute hemorrhages was treated by administering the study drug once (86.2%) or twice (10.0%), and the mean dose administered per single infusion was 28.55+/-6.53 IU/kg. Ten subjects underwent 12 surgical procedures, and hemostatic efficacy was excellent in seven cases (58.3%) and good in five cases (41.7%), showing a 100% efficacy rate. A total of 52 of 88 subjects (59.0%) experienced 168 adverse events. There were 18 serious adverse events (10.7%) in 11 subjects, and two (mild dyspnea and facial edema) in one subject were related to the study drug. Only one subject formed a de novo factor VIII inhibitor, for an occurrence rate of 1.4% (one-sided 95% upper confidence limit: 3.85%). The final elimination half-life was 13.3 h and 12.6 h at baseline and 6 months after administration, respectively. CONCLUSION: Our results suggest that beroctocog alfa is safe and efficacious as either an on-demand treatment for acute hemorrhage or a surgical prophylaxis in patients with hemophilia A.
Adult
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Consumer Product Safety
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Dyspnea
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Factor VIII/adverse effects/*pharmacokinetics/therapeutic use
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Female
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Hemophilia A/*drug therapy
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Hemorrhage/prevention & control
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Hemostasis
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Hemostasis, Surgical/methods
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Humans
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Male
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Middle Aged
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Prospective Studies
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Recombinant Proteins/adverse effects/*pharmacokinetics/*therapeutic use
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Treatment Outcome
5.Effects of L.F04, the active fraction of Lycopus lucidus, on erythrocytes rheological property.
Hong-zhi SHI ; Nan-nan GAO ; Yong-zhi LI ; Jing-guang YU ; Quan-chun FAN ; Gui-e BAI ; Bing-mu XIN
Chinese journal of integrative medicine 2005;11(2):132-135
OBJECTIVETo study the effects of L.F04, the active fraction of Lycopus lucidus, on erythrocytes rheological property so as to investigate its mechanism in promoting blood circulation and removing blood stasis.
METHODThe effects of L.F04 (used for treatment for 10 days in different dosages) on deformability, aggregation and membrane liquidity of erythrocytes (MLE) as well as whole blood apparent viscosity (eta(b)) were examined on the basis of rat model of blood-stasis syndrome induced by venous injection of high molecular weight dextran.
RESULTAs compared with the normal control group, the model group's RBC deformability and MLE were lower, and the aggregation of erythrocytes and eta(b) were higher. Compared with the model group, both L.F04 0.612 g/kg and 0.306 g/kg showed significant effect in improving deformability and inhibiting aggregation of red blood cells (RBC) and reducing blood viscosity. The trend of improving MLE was also shown.
CONCLUSIONL.F04 could significantly improve the abnormal rheological property of erythrocytes.
Animals ; Blood Viscosity ; drug effects ; Dextrans ; pharmacology ; Drugs, Chinese Herbal ; administration & dosage ; Erythrocyte Aggregation ; drug effects ; Erythrocyte Deformability ; drug effects ; Hemorheology ; Hemostasis ; drug effects ; Lycopus ; Male ; Rats ; Rats, Wistar ; Space Flight
6.Evaluate activating blood circulation and dissipating blood stasis effect mechanism of foshousan on acute blood stasis rats on basis of metabolomic approach.
Mei-Yan HUANG ; Yu-Ping TANG ; Wei-Xia LI ; Er-Xin SHANG ; Jian-Ming GUO ; Da-Wei QIAN ; Jin-Ao DUAN
China Journal of Chinese Materia Medica 2013;38(20):3576-3582
Ice water bath and subcutaneous injection of adrenaline were used to establish the acute blood stasis model of rats. Ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) was used to study the urine metabolic changes of acute blood stasis rats. Potential biomarkers were selected by variable importance projection, and identified on basis of MS information and databases. The metabolic pathways were predicted via MetPA database. To study the effect of Foshousan on endogenous metabolites of acute blood stasis model rats, find potential biomarkers, and explore the effect mechanism of Foshousan on activating blood circulation and dissipating blood stasis. Eleven potential biomarkers were identified with multivariate statistical analysis of urine metabolite profiles, and which also were used to explain the phenylalanine metabolism, tryptophan metabolism and sphingolipid metabolism. Those disturbed metabolic pathways in acute blood stasis rats could be regulated closely to normal state after Foshousan administration. Metabolomics has a bright prospect in the efficacy evaluation and effect mechanism elucidation of the traditional Chinese medicines.
Animals
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Biomarkers
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urine
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Blood Circulation
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drug effects
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Blood Coagulation Disorders
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blood
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drug therapy
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metabolism
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physiopathology
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Drugs, Chinese Herbal
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administration & dosage
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Female
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Hemostasis
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drug effects
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Humans
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Metabolic Networks and Pathways
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drug effects
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Metabolomics
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Rats
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Rats, Sprague-Dawley
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Urine
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chemistry
7.Advances in study of the pharmacological effects of danshen on hemorheology.
China Journal of Chinese Materia Medica 2005;30(8):630-640
The article reviewed the research on the pharmacological effects of Danshen on hemorheology. We discussed the action mechanism of Danshen and its preparations from the points of hemorheology, blood and vessel endothelium cell. Danshen and its preparations can obviously improve the hemorheological characteristic by various ways.
Animals
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Benzofurans
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isolation & purification
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pharmacology
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Diterpenes, Abietane
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Drugs, Chinese Herbal
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isolation & purification
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pharmacology
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Hemorheology
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drug effects
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Hemostasis
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drug effects
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Lactates
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isolation & purification
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pharmacology
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Phenanthrenes
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isolation & purification
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pharmacology
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Plant Roots
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chemistry
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Plants, Medicinal
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chemistry
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Platelet Aggregation
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drug effects
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Salvia miltiorrhiza
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chemistry
8.Effects of multiwall carbon nano-onions on platelet aggregation and hemostatic function.
Gui-li YANG ; Jie YANG ; Jun ZHANG ; Yu-ying XU ; Qiao-hui WEI ; Xiang-yu SUN ; Xiao-min GU ; Yin ZHANG ; Qiu-ping DING ; Yi-fan ZHENG ; Jun YANG ; Xin-qiang ZHU
Chinese Journal of Industrial Hygiene and Occupational Diseases 2011;29(5):321-323
OBJECTIVETo observe the effects of multiwall carbon nano-onions (MWCNOs) on platelet aggregation and hemostatic function.
METHODSThe platelet aggregation was determined with Born's method at different concentration of MWCNOs (0, 0.2, 2.0, 20.0 microg/ml) in vitro. Twenty male SD rats were randomly divided into 4 groups which were exposed to 0, 2, 4 and 8 mg/kg MWCNOs, respectively. Then platelet count, platelet aggregation, activated partial thromboplastin time (APTT), prothrombin time (PT), thrombin time (TT), bleeding time (BT) and platelet count (PC) were measured at 12 h after receiving tail intravenous injection of MWCNOs. The effects of MWCNOs (4 mg/kg) on platelet aggregation and platelet count at different time points were observed.
RESULTSIn vitro, MWCNOs exhibited the potent inhibitory effects on rat platelet aggregation caused by ADP in a concentration-dependent manner. The platelet aggregation in the highest dosage of 20.0 microg/ml group was 50.0% +/- 6.9% which was significantly lower than that (73.2% +/- 4.3%) in control group (P<0.01). In vivo, the highest inhibitory was up to 20.4%, but there was no significant difference, as compared with control group. MWCNOs did not affect the APTT, PT, TT, BT and PC.
CONCLUSIONUnder this experimental condition, MWCNOs might inhibit platelet aggregation but not affect hemostatic function.
Animals ; Bleeding Time ; Blood Coagulation ; drug effects ; Carbon ; administration & dosage ; pharmacology ; Hemostasis ; drug effects ; Male ; Nanostructures ; Partial Thromboplastin Time ; Platelet Aggregation ; drug effects ; Platelet Count ; Prothrombin Time ; Rats ; Rats, Sprague-Dawley ; Thrombin Time
9.A multicenter, phase III trial of hemocoagulase Agkistrodon: hemostasis, coagulation, and safety in patients undergoing abdominal surgery.
Jun-min WEI ; Ming-wei ZHU ; Zhong-tao ZHANG ; Zhen-geng JIA ; Xiao-dong HE ; Yuan-lian WAN ; Shan WANG ; Dian-rong XIU ; Yun TANG ; Jie LI ; Jing-yong XU ; Qing-shan HENG
Chinese Medical Journal 2010;123(5):589-593
BACKGROUNDHemocoagulase Agkistrodon for injection is a single component thrombin which has passed phases I and II clinical trials. The purpose of this phase III clinical trial was to evaluate the effect of Hemocoagulase Agkistrodon on hemostasis and coagulation in abdominal skin and subcutaneous incisions and to assess the safety of this agent in surgical patients.
METHODSThis is a phase III, prospective, randomized, double-blind, and controlled multicenter clinical trial including 432 consecutive patients randomized into either a study group (injected with hemocoagulase Agkistrodon at 2 U, n = 324) or a control group (injected with hemocoagulase Atrox, n = 108). The hemostatic time, hemorrhagic volume, hemorrhagic volume per unit area, blood coagulation, and adverse events were measured and compared between the two groups.
RESULTSThe mean hemostatic time in the study group was (36.8 +/- 18.7) seconds; the hemorrhagic volume was (3.77 +/- 3.93) g; and the hemorrhagic volume per unit area was (0.091 +/- 0.125) g/cm(2). In the control group, the corresponding values were (38.1 +/- 19.7) seconds, (4.00 +/- 4.75) g, and (0.095 +/- 0.101) g/cm(2), respectively. No significant difference in values existed between the two groups (P > 0.05). Blood coagulation results and hepatic and renal function were also similar between the two groups. Adverse events were reported in two cases, but were deemed non-drug-related.
CONCLUSIONSHemocoagulase Agkistrodon has good hemostatic and coagulative function and is safe for the use of arresting capillary hemorrhage that occurs while incising the abdomen during surgery.
Abdomen ; surgery ; Adolescent ; Adult ; Aged ; Agkistrodon ; Animals ; Batroxobin ; adverse effects ; pharmacology ; Blood Coagulation ; drug effects ; Double-Blind Method ; Evidence-Based Medicine ; Female ; Hemostasis ; drug effects ; Hemostatics ; pharmacology ; Humans ; Male ; Middle Aged ; Prospective Studies
10.Effect of qilong capsule on hemoreology in acute stress blood stasis rats.
China Journal of Chinese Materia Medica 2004;29(4):362-365
OBJECTIVETo study the influence of Qilong capsule (QLC) on the hemoreology in acute stress blood stasis model rats.
METHODThe model of acute stress blood stasis rats were induced by putting the rats into ice-water between hyodermic epinephrine twice of 1 mg x kg(-1). With the models, the effect of QLC on hemoreology such as whole blood viscosity, whole blood reduction viscosity, plasma viscosity, haematocrit (Hct), erythrocyte deformation and erythrocyte aggregation were observed.
RESULTQLC 0.6, 0.3, 0.15 g x kg(-1) could significantly reduce the increase of whole blood viscosity at high-middle-low shear rate, reduce the whole blood reduction viscosity at middle-low shear rate, reduce Hct and erythrocyte aggregation, and increase the erythrocyte deformation in acute stress blood stasis rats (P < 0.05, P < 0.01, compared with vehicle). QLC 0.6, 0.3 g x kg(-1) could also reduce plasma viscosity (P < 0.05, P < 0.01, compared with vehicle).
CONCLUSIONQLC can significantly improve some indexes of hemoreology in acute stress blood stasis rats.
Animals ; Astragalus membranaceus ; chemistry ; Blood Viscosity ; drug effects ; Capsules ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; pharmacology ; Erythrocyte Aggregation ; drug effects ; Erythrocyte Deformability ; drug effects ; Hemorheology ; drug effects ; Hemostasis ; drug effects ; Male ; Materia Medica ; administration & dosage ; isolation & purification ; pharmacology ; Oligochaeta ; chemistry ; Plants, Medicinal ; chemistry ; Rats ; Rats, Wistar ; Salvia miltiorrhiza ; chemistry ; Stress, Physiological ; physiopathology