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1.
J Med Chem ; 59(11): 5356-67, 2016 06 09.
Artículo en Inglés | MEDLINE | ID: mdl-27167608

RESUMEN

Elevated levels of human lipoprotein-associated phospholipase A2 (Lp-PLA2) are associated with cardiovascular disease and dementia. A fragment screen was conducted against Lp-PLA2 in order to identify novel inhibitors. Multiple fragment hits were observed in different regions of the active site, including some hits that bound in a pocket created by movement of a protein side chain (approximately 13 Å from the catalytic residue Ser273). Using structure guided design, we optimized a fragment that bound in this pocket to generate a novel low nanomolar chemotype, which did not interact with the catalytic residues.


Asunto(s)
1-Alquil-2-acetilglicerofosfocolina Esterasa/antagonistas & inhibidores , Descubrimiento de Drogas , Inhibidores Enzimáticos/farmacología , Pirazoles/farmacología , Tiazoles/farmacología , 1-Alquil-2-acetilglicerofosfocolina Esterasa/metabolismo , Sitios de Unión/efectos de los fármacos , Cristalografía por Rayos X , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Humanos , Modelos Moleculares , Estructura Molecular , Pirazoles/síntesis química , Pirazoles/química , Relación Estructura-Actividad , Tiazoles/síntesis química , Tiazoles/química
2.
J Ethnopharmacol ; 173: 266-72, 2015 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-26216512

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Reduction of Sheng-Nao-Kang decoction (RSNK), composed of Salvia miltiorrhiza Bge., Ligusticum chuanxiong Hort., Astragalus membranaceus (Fisch.) Bunge., Pueraria lobata (Willd.) Ohwi., Paeonia lactiflora Pall. and Panax notoginseng (Burk.) F. H. Chen., is a modified traditional Chinese medicinal formula of Sheng-Nao-Kang pill preparation, which has been investigated its protective effect on focal cerebral ischemia-reperfusion injury in rat in our previous report. AIM OF THE STUDY: To evaluate the antithrombotic effect of RSNK in blood stasis model rats and explore the potential mechanisms. MATERIALS AND METHODS: Subcutaneous injection of norepinephrine and bovine serum albumin combined with ice water bath was used to establish the acute blood stasis rat model. The anticoagulant activities were investigated by measuring activated partial thromboplastin time (APTT), thrombin time (TT), prothrombin time (PT), and the content of fibrinogen (FIB). Meanwhile, the levels of thromboxane A2 (TXA2), prostaglandins I2 (PGI2), endothelial nitric oxide synthase (eNOS) and endothelin (ET) were detected. RESULTS: The treatment of RSNK was able to prolong APTT, TT and PT, and decrease FIB content obviously. Furthermore, it markedly suppressed TXB2 level and up-regulated 6-keto-PGF1α level of the blood-stasis model rats, accompanied with the decrease of T/K. The level of ET and TXA2 in plasma was down-regulated and the levels of eNOS in plasma and PGI2 in serum was up-regulated in RSNK-treated rats compared with model rats (P<0.05). CONCLUSION: The present study suggested that RSNK possessed remarkable antithrombotic property in blood stasis model rats induced by ice water bath and subcutaneous injection of norepinephrine and bovine serum albumin. This property could be associated with its anticoagulation activity, the regulation of active substances in vascular endothelium and maintaining the balance of TXA2 and PGI2.


Asunto(s)
Abietanos/uso terapéutico , Anticoagulantes/uso terapéutico , Ácidos Cafeicos/uso terapéutico , Catecoles/uso terapéutico , Medicamentos Herbarios Chinos/uso terapéutico , Trombosis/tratamiento farmacológico , 6-Cetoprostaglandina F1 alfa/sangre , Abietanos/farmacología , Animales , Anticoagulantes/farmacología , Coagulación Sanguínea/efectos de los fármacos , Pruebas de Coagulación Sanguínea , Ácidos Cafeicos/farmacología , Arterias Carótidas/efectos de los fármacos , Arterias Carótidas/patología , Catecoles/farmacología , Frío , Modelos Animales de Enfermedad , Medicamentos Herbarios Chinos/farmacología , Endotelinas/sangre , Masculino , Óxido Nítrico Sintasa de Tipo III/sangre , Norepinefrina , Fitoterapia , Ratas Sprague-Dawley , Albúmina Sérica Bovina , Trombosis/sangre , Trombosis/patología , Tromboxano A2/sangre
3.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 32(2): 160-3, 2012 Feb.
Artículo en Chino | MEDLINE | ID: mdl-22574583

RESUMEN

OBJECTIVE: To observe the effects of qi-supplementing dominated Chinese materia medica (QSDCMM) combined with rehabilitation training on the quality of life (QOL) of ischemic post-stroke fatigue (PSF) patients of qi deficiency syndrome. METHODS: Ninety ischemic stroke patients of qi deficiency were randomly assigned to 3 groups, 30 in each. Patients in the Chinese medicine treatment group were treated with oral administration of QSDCMM decoction and rehabilitation. Those in the Western medicine treatment group were treated with Chinese medicine placebo, Western medicine, and rehabilitation. Those in the control group were treated with Chinese medicine placebo and rehabilitation. The therapeutic course for all was 4 weeks. All patients were assessed using Stroke Specific Quality of Life Scale (SS-QOL) and Fatigue Severity Scale (FSS) before treatment and 4 weeks after treatment. RESULTS: After treatment the scores of SS-QOL and FSS increased in the 3 groups, especially in the CM treatment group, showing significant difference (P < 0.05). After treatment significant difference existed between the CM treatment group and the Western medicine treatment group, between the CM treatment group and the control group, showing significant difference (P < 0.05). There was no statistical difference between the Western medicine treatment group and the control group (P > 0.05). CONCLUSION: QSDCMM combined with rehabilitation training could improve the QOL of ischemic PSF patients of qi deficiency syndrome.


Asunto(s)
Medicamentos Herbarios Chinos/uso terapéutico , Fatiga/rehabilitación , Fitoterapia , Accidente Cerebrovascular/complicaciones , Anciano , Isquemia Encefálica/rehabilitación , Fatiga/etiología , Fatiga/terapia , Femenino , Humanos , Masculino , Medicina Tradicional China , Persona de Mediana Edad , Qi , Calidad de Vida , Rehabilitación , Rehabilitación de Accidente Cerebrovascular
4.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 31(9): 1175-80, 2011 Sep.
Artículo en Chino | MEDLINE | ID: mdl-22013790

RESUMEN

OBJECTIVE: To study the effects of integrative medicine protocols on the neural function deficit and short-term disability outcomes in patients with acute ischemic cerebral stroke. METHODS: 99 patients were randomly assigned to three groups, i.e., the Dengzhan Xixin (fleabane) group (Group A), the Kudiezi (sowthistle-leaf ixeris seedling) group (Group B), and the Western medicine control group (Group C). Dengzhan Xixin Injection was intravenously dripped to patients in Group A for 14 days. Chinese decoction was administered to them by pattern typing as well. Meanwhile, they took Dengzhan Shengmai Capsule for two months. Kudiezi Injection was intravenously dripped to patients in Group B for 14 days. Chinese decoction was administered to them by pattern typing as well. Meanwhile, they took Naoshuantong Capsule for two months. In addition to internal therapies, patients in Group A and B received acupuncture, massage, and external washing with Chinese medicine for 21 days. Patients in Group C also received modem rehabilitation therapy for 21 days, including rehabilitation training and electronic stimulus in addition to the internal medicine. The National Institute of Health Stroke Scale (NIHSS) and disability outcome (modified Rank Scale, mRS) were taken as main effect indices. RESULTS: The NIHSS scores at each time point obviously decreased more than before treatment in all the three groups (P<0.01), but with no difference at each time point (P>0.05). The disability outcomes of all the three groups postponed as time went by. Significant difference existed among the three groups by log-lineal model (CATMOD) (P<0.05). The best effect was shown in Group B, with the markedly effective rate of 19. 35% and the total effective rate 54.84%. CONCLUSIONS: The integrative medicine protocols could improve the nerve functions of ischemic stroke patients. Therefore, it could improve the disability outcomes. The comprehensive protocol (Kudiezi Injection + Naoshuantong Capsule + Chinese decoction according to pattern typing + acupuncture + massage + external washing with Chinese medicine) was better.


Asunto(s)
Isquemia Encefálica/terapia , Medicina Integrativa , Accidente Cerebrovascular/terapia , Anciano , Anciano de 80 o más Años , Medicamentos Herbarios Chinos/uso terapéutico , Femenino , Humanos , Masculino , Persona de Mediana Edad , Fitoterapia , Resultado del Tratamiento
5.
Phytother Res ; 25(12): 1895-7, 2011 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-21674630

RESUMEN

Du-Zhong is one of the most important tonic herbs in traditional Chinese medicine for the treatment of bone fractures and other bone diseases. The present study examined whether Du-Zhong seed extract named total glycosides from Eucommia ulmoides seed (TGEUS) could display an increased effect on bone density and bone strength of the femur in rats. Sprague-Dawley rats were used and randomly assigned to the normal group and the TGEUS group (400 mg/kg body weight/day). Daily oral administration of TGEUS was found to increase significantly the biomechanical quality of the femur. The mechanical changes were associated with a bone mineral density (BMD) increase or even with some improvements in microarchitecture. Micro-CT analysis of the distal femur showed that TGEUS significantly increased the bone volume/tissue volume (BV/TV), connectivity density (Conn.D), trabecular number (Tb.N) and trabecular thickness (Tb.Th), and decreased trabecular separation (Tb.Sp) and the structure model index (SMI) in normal rats. To conclude, TGEUS taken orally increased bone density and altered bone histomorphology, suggesting that TGEUS might be a potential alternative medicine for the treatment of postmenopausal osteoporosis.


Asunto(s)
Densidad Ósea/efectos de los fármacos , Eucommiaceae/química , Fémur/efectos de los fármacos , Glicósidos/farmacología , Extractos Vegetales/farmacología , Animales , Femenino , Ratas , Ratas Sprague-Dawley , Semillas/química
6.
Zhongguo Zhen Jiu ; 31(5): 451-4, 2011 May.
Artículo en Chino | MEDLINE | ID: mdl-21692300

RESUMEN

Suggestions such as how to enhance the rationality of designation of clinical trails, regulate the evaluation system on therapeutic effects, control the quality strictly and unify the standard of report on key points of acupuncture clinical trials from the aspects of designation, therapeutic evaluation, quality control and report standard were expounded in this paper. Highlights such as perspective of acupuncture in qualitative investigation and practical clinical trails were explored as well in this paper. And some international and domestic disputes in the related fields such as placebo acupuncture and selection of acupoints were discussed and analyzed so as to provide methodological instruction for acupuncture clinical trails and promote its normalization process.


Asunto(s)
Terapia por Acupuntura , Ensayos Clínicos como Asunto , Humanos , Proyectos de Investigación
7.
J Ethnopharmacol ; 126(1): 184-7, 2009 Oct 29.
Artículo en Inglés | MEDLINE | ID: mdl-19665537

RESUMEN

AIM OF THE STUDY: Polyporus umbellatus is a fungus used as a diuretic medicine. The objective of this study was to isolate and elucidate the diuretic constituents of n-hexane, ethyl acetate, n-butanol and water extracts of Polyporus umbellatus and to evaluate their diuretic activity. MATERIALS AND METHODS: The n-hexane, ethyl acetate, n-butanol and water extracts of Polyporus umbellatus were tested by diuretic experiment of normal rats in metabolic cage. The n-hexane extract and n-butanol extract were prepared separately by the bioassay-guided approach. Three isolated compounds doses (5, 10 and 20 mg/kg BW) were orally administered to normal rats. Water excretion rate, pH and content of Na(+), K(+) and Cl(-) were measured in the urine of saline-loaded rats. RESULTS: n-Hexane extract (P<0.05), n-butanol extract (P<0.05) and three isolated compounds (ergosta-4,6,8(14),22-tetraen-3-one, ergosterol and d-mannitol) displayed diuretic activity. CONCLUSIONS: The ergosta-4,6,8(14),22-tetraen-3-one was the strongest diuretic constituent in the three compounds. Ergosterol and D-mannitol were found to be also responsible for duiretic effects in Polyporus umbellatus for the first time. Data show that 20 mg/kg dose of the ergosterol for urine out put became significantly higher than in the control rats, but the ratio of Na(+)/K(+) almost unaltered in the three doses. The highest dose of the D-mannitol was significant and increased the cumulative urine output. Regarding the electrolyte excretion, data show that the doses 10 and 20 mg/kg produce significant increase for excretion of Na(+) and Cl(-). The present results provide a quantitative basis explaining application of Polyporus umbellatus as a diuretic medicine. The result proved that its diuretic effects were also due to the contribution of multi-components in clinical application.


Asunto(s)
Bioensayo/métodos , Mezclas Complejas/farmacología , Diuresis/efectos de los fármacos , Diuréticos/química , Diuréticos/farmacología , Polyporus/química , Animales , Colestenonas , Mezclas Complejas/química , Evaluación Preclínica de Medicamentos/métodos , Ergosterol/análogos & derivados , Ergosterol/síntesis química , Ergosterol/farmacología , Masculino , Manitol/farmacología , Medicina Tradicional China , Ratas , Ratas Sprague-Dawley
8.
Chin J Integr Med ; 13(2): 148-51, 2007 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-17609917

RESUMEN

In the last several years, traditional Chinese medicine (TCM) has made much progress in the treatment of neurological diseases. The living space of TCM in neurological diseases lies in refractory diseases, aging and chronic diseases caused by multiple factors as well as sub-health state and chronic fatigue state. The effect model of TCM mainly consists of whole effect, self-organization, self-stable model, holographic effect and butterfly effect. The effective point of TCM in neurological diseases lies mainly in end-points and health-related events. Moreover, TCM has advantages in the evaluation of symptoms, syndrome and quality of life (QOL). Some key indexes should be included when evaluating the efficacy of TCM in neurological diseases. Meanwhile, the advantages of TCM such as end-points, health-related events and QOL should be highlighted. Multi-subject researching methods could be adopted to make a comprehensive evaluation of subjective and objective indexes. The clinical evidence on the TCM efficacy evaluation may come from RCTs, and other types of designs can also be considered.


Asunto(s)
Medicina Tradicional China , Enfermedades del Sistema Nervioso/tratamiento farmacológico , Envejecimiento , Humanos , Enfermedades del Sistema Nervioso/psicología , Calidad de Vida
9.
Zhong Xi Yi Jie He Xue Bao ; 5(3): 276-81, 2007 May.
Artículo en Chino | MEDLINE | ID: mdl-17498487

RESUMEN

OBJECTIVE: To explore the clinical evaluation system reflecting the superiority and characteristics of comprehensive traditional Chinese medicine (TCM) therapy for acute stroke. METHODS: A randomized controlled trial with single blind in various therapeutic centers was applied on the patients with the acute stage of hemorrhagic stroke due to hypertension, who were allocated to the trial group and the control group. The trial group accepted the general Western medicine therapy and differential treatment of traditional Chinese medicine based on stage classification. Patients in the control group were treated with the general Western medicine and the placebo of traditional Chinese herbal medicine. The treatment effect was assessed at the 7th day, 14th day, 21st day, and 28th day of post-treatment and after 3-month follow-up. The clinical evaluation system included the syndromes of TCM (ZH), Glasgow coma standard (GCS), nerve functional failure (NF), activity of daily living (ADL), Barther index (BI), quality of life index (QLI) and functional activities questionnaire (FAQ). RESULTS: Four hundred and four patients with acute stroke were included. There were 178 cases with yang-syndrome and 21 cases with yin-syndrome in the trial group (n=199), and there were 165 cases with yang-syndrome and 40 cases with yin-syndrome in the control group (n=205). The rates of recovery and obvious improvement after 3-month treatment in the trial group and the control group were 86.5% and 73.6% respectively. There was significant difference between the two groups (P<0.01). The response sensitivity of the effect items indicated that the sensitivity of GCS began to increase from the 7th day and was high at the 14th day and the 21st day for all patients. The response sensitivity of the NF scale was high for all patients at the 14th day, the 21st day and the 28th day. The BI scale and the QLI scale were sensitive to the patients with light and middle stage of stroke at the 21st day, and were sensitive to the patients with light stage of stroke after 3-month follow-up. The FAQ scale was sensitive to the light stroke at the 21st day and after 3-month follow-up. The ADL scale was sensitive to all patients at the 28th day and the patients with light stage of stroke after 3-month follow-up. The ZH scale was sensitive to all patients from 0 to 7d, the 14th day, and the 28th day. The principle components analysis indicated these 7 items could reflect the condition of stroke from 0-7d, the 21st day and after 3-month follow-up, and could be used to evaluate the therapeutic effect of hemorrhagic stroke. ZH scale and FAQ scale were more sensitive than other effect items at the 28th day. CONCLUSION: The seven items (GCSbNFbBIbQLIbFAQbADLbZH) have high sensibility to all patients in the acute stage of hemorrhage stroke especially at the 21st day. The ZH score will change in accord with the condition of stroke, and is appropriate to reflect the condition of stroke. It is believed that the seven items can form the system of effect evaluation in different stages of stroke, and the ZH scale is a very important item.


Asunto(s)
Quimioterapia/métodos , Medicina Tradicional China/métodos , Accidente Cerebrovascular/terapia , Enfermedad Aguda , Adulto , Anciano , Anciano de 80 o más Años , Hemorragia Cerebral/etiología , Hemorragia Cerebral/terapia , Diagnóstico Diferencial , Femenino , Estudios de Seguimiento , Humanos , Hipertensión/complicaciones , Masculino , Persona de Mediana Edad , Método Simple Ciego , Accidente Cerebrovascular/etiología , Deficiencia Yang/terapia
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