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Objective: To study the different pharmacokinetics effect of acteoside extracted from Rehmanniae Radix Preparata in normal and blood deficiency rats. Methods: Injected acetyl phenylhydrazine and cyclophosphamide to make blood deficiency rats models subcutaneously,and gave mice the ethand extracts of Rehmanniae Radix preparata by oral administration,the concentration of acteoside in rats at different time points were detected by HPLC method, pharmacokinetic parameters were calculated by 3p87 software. Results: The determination of acteoside in the linear range were 0. 2 ~ 80 µg / m L, the limit of detection and quantification was 0. 03 and 0. 12µg/m L,respectively. Compared with the normal group,the content of AUC0-tand AUC0-∞of corresponding dose in model group rats increased significantly, and the average dwell time and the elimination half-life prolong significantly. Conclusion: This method has high specificity,high sensitivity and simple operation, which can be used for the determination to pharmacokinetic process of acteoside in blood deficiency model.
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Cromatografía Líquida de Alta Presión , Glucósidos/farmacología , Fenoles/farmacología , Administración Oral , Animales , Fenilhidrazinas , Ratas , Ratas Sprague-DawleyRESUMEN
Objective: To study the differences of anti-inflammatory and analgesic effects between oil,sand and vinegar processing Strychnos nux-vomica seeds. Methods: Mouse auricular swelling and writhing test and mice hot water tail flick latency effect method were used to study and compare the anti-inflammatory and analgesic effects of different processing products of Strychnos nux-vomica seeds. Results: The anti-inflammatory and analgesic effects of vinegar processing Strychnos nux-vomica seeds was better than that of oil and sand processing products. Conclusion: This study can provide theoretical basis for the optimization of processing technology of reducing toxicity and enhancing effects of processed Strychnos nux-vomica seeds.
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Strychnos nux-vomica , Ácido Acético , Analgésicos , Animales , Antiinflamatorios , Edema , Ratones , Extractos Vegetales , Semillas , EstricninaRESUMEN
OBJECTIVE: To compare the pharmacokinetic differences of brucine in rats after different administration methods of brucine liposome. METHODS: To determine brucine in rat plasma at different points in time by HPLC after oral administration, intramuscular injection, subcutaneous injection and intravenous injection of brucine liposome, respectively. The pharmacokinetic parameters were calculated and analyzed by DAS 3.0. RESULTS: Compared with other groups, AUC(0 --> t) of subcutaneous injection were higher, C(max) were lower and MRT(0 --> 1), were significantly improved. The pharmacokinetics parameters and absolute bioavailability of brucine show that bioavailability in rats after different administration methods of brucine liposome is subcutaneous injection > intramuscular injection > oral administration.
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Liposomas/administración & dosificación , Estricnina/análogos & derivados , Administración Oral , Animales , Disponibilidad Biológica , Cromatografía Líquida de Alta Presión , Inyecciones Intramusculares , Inyecciones Intravenosas , Inyecciones Subcutáneas , Liposomas/farmacocinética , Ratas , Ratas Sprague-Dawley , Estricnina/administración & dosificación , Estricnina/farmacocinéticaRESUMEN
OBJECTIVE: To establish an HPLC-UV method for determining pharmacokinetic difference of notoginsenoside R1 between normal rats and ischemic rats. METHODS: 48 male SD rats were randomly divided into normal group and acute myocardial ischemia( AMI) model group induced by pituitrin and each group was classified into high,middle and low-dose of groups with notoginsenoside R1 (200, 100 and 50 mg/kg) respectively. Blood samples were collected at different points in time after they were administered once by gavage and separated by Waters symmetry C18 column (250 mm x 4.6 mm, 5 µm) under the detective wavelength 203 nm, the mobile phase was acetonitrile-water with icariin as the internal standard and the pharmacokinetic parameters were calculated by DAS 2. 0. RESULTS: Notoginsenoside R1 had good linearity in the ranges of 0.2~125 µg/mL (R2 = 0.9997) with SNR 1:3 and the lowest detection limit was 0.053 µg/mL, the extraction rate, RSDs of within-day and between-day, specificity, accuracy and precision accorded with the require-ment of bio-sample pretreatment. Compared to the normal group, AUC0-t, and AUC0-∞ was significantly increased (P < 0.01) and the terminal half-life was prolonged markedly (P < 0.01) in AMI group. CONCLUSIONS: The method is simple, accurate and had high specificity and sensitivity, that could be applied in quantitative determination of notoginsenoside R1 and research of pharmacokinetics; the relative bioavailability of notoginsenoside R1 is increased significantly in AMI group,which indicates that notoginsenoside R1 has better effect in model rat.
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Ginsenósidos/farmacocinética , Infarto del Miocardio/tratamiento farmacológico , Animales , Modelos Animales de Enfermedad , Masculino , Ratas , Ratas Sprague-DawleyRESUMEN
OBJECTIVE: To analyse the volatile compositions of different specification of Panax notoginseng. METHODS: Volatile compositions from different specification of Panax notoginseng were detected by Headspace Solid-Phase Micro-Extraction with GC/MS. RESULTS: Terpenoids were the main compositions in different specification of Panax Notoginseng, and a-guaiene was the fundamental ingredient. The type, content and quantity of the compounds were different in different type of Panax notoginseng. CONCLUSION: Terpenoids were the main pharmacodynamics of the volatile compositions of Panax notoginseng and worthy of further study.
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Panax notoginseng/química , Microextracción en Fase Sólida/métodos , Terpenos/análisis , Compuestos Orgánicos Volátiles/análisis , Cromatografía de Gases y Espectrometría de Masas , Raíces de Plantas/química , Control de Calidad , Rizoma/química , Sesquiterpenos de Guayano/análisis , VolatilizaciónRESUMEN
OBJECTIVE: To research the effects of Panax notoginseng saponins (PNS) on angiotensin-converting enzymes 2 ( ACE2) and tumor necrosis factor-alpha (TNF-alpha) in rats with post-myocardial infarction ventricular remodeling. METHODS: Models of acute myocardial infarction (AMI) were produced by ligation of left anterior descending coronary artery, 24 hours after operation the rats were randomly divided into control and experiment groups, then respectively administrated with NS, fosinopril and low, middle and high dosage of PNS for four consecutive weeks. To observe effects of PNS on malondialdehyde (MDA), nitric oxide (NO), glutathione peroxidase (GSH-Px), ACE2 and TNF-alpha in rats with post-myocardial infarction ventricular remodeling. RESULTS: Compared with NS group, MDA significantly decreased, the activity of GSH-Px significantly increased (P < 0.05 or P < 0.01), NO of the high-dose PNS group decreased (P < 0.05), Compared with the NS group, ACE2 increased and TNF-a significantly decreased in low-dose PNS group, middle and high-dose groups (P < 0.05). CONCLUSION: PNS can stimulate ACE2 to inhibit the expression of TNF-alpha and enhance the antioxidance. PNS can reduce pathological injury of cardiac myocytes in myocardial ischemia and cardiac muscle, which can improve ventricular remodeling.
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Antioxidantes/farmacología , Infarto del Miocardio/tratamiento farmacológico , Peptidil-Dipeptidasa A/sangre , Saponinas/farmacología , Factor de Necrosis Tumoral alfa/sangre , Remodelación Ventricular/efectos de los fármacos , Enzima Convertidora de Angiotensina 2 , Animales , Modelos Animales de Enfermedad , Femenino , Fosinopril/farmacología , Glutatión Peroxidasa/sangre , Glutatión Peroxidasa/metabolismo , Masculino , Malondialdehído/sangre , Malondialdehído/metabolismo , Infarto del Miocardio/patología , Infarto del Miocardio/fisiopatología , Miocardio/metabolismo , Miocardio/patología , Óxido Nítrico/sangre , Óxido Nítrico/metabolismo , Panax notoginseng/química , Peptidil-Dipeptidasa A/metabolismo , Distribución Aleatoria , Ratas , Ratas Sprague-Dawley , Factor de Necrosis Tumoral alfa/metabolismoRESUMEN
Although the concept of inflammatory obesity remains to be widely accepted, a plethora of antibiotics, anti-inflammatory agents, mitochondrial uncouplers, and other structurally distinct compounds with unknown mechanisms have been demonstrated to exert functionally identical effects on weight reduction. Here we summarize a universal mechanism in which weight loss is modulated by mitochondrial biogenesis, which is correlated with conversion from the mitochondria-insufficient white adipose tissue to the mitochondria-abundant brown adipose tissue. This mechanistic description of inflammatory obesity may prove useful in the future for guiding pathology-based drug discovery for weight reduction.
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To investigate the effect of moisture change on nitrification and denitrification and their corresponding functional microbes, an acidic paddy soil from Taoyuan, Hunan Province was selected as the study object, and soil microcosm experiment containing 4 different water holding capacity (WHC) levels (30% WHC, 60% WHC, 90% WHC, and waterlog) was set up in this study. Results showed that no active nitrification and denitrification occurred in 30% WHC treatment as there were no obvious ammonia consumption and nitrate accumulation, while nitrification was active in 60% WHC and 90% WHC treatments as indicated by the obvious accumulation of nitrate in those two treatments. Meanwhile, significant ammonia consumption and N2O emission were only observed in 90% WHC treatment, implying that a much stronger nitrification in 90% WHC treatment than in 60% WHC treatment and the co-occurrence of nitrification and denitrification in 90% WHC treatment. In waterlog treatment, relatively lower N2O emission was detected and no obvious nitrification was detected, corresponding to a significant lower soil Eh in this treatment than in the other three non-waterlog treatments. Except the early stage of incubation (7 d), the abundance of nirS, nirK and ammonia-oxidizing bacteria (AOB) amoA genes showed similar responses to soil moisture change over time. Except the slight decrease in waterlog treatment, the abundances of the three genes increased significantly as the soil moisture increased, and the highest abundances of nirS, nirK, and amoA gene were observed in 90% WHC treatment in which the highest nitrification and denitrification activity was detected. T-RFLP analysis showed that the community composition of nirS gene-containing denitrifiers changed significantly in response to soil moisture change after two weeks, and soil Eh and C(w) were the main factors affecting the community composition of denitrifiers.
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Desnitrificación , Nitrificación , Microbiología del Suelo , Agua , Amoníaco/química , Bacterias/crecimiento & desarrollo , Genes Bacterianos , Nitratos/química , Óxido Nitroso/química , Oryza , Suelo/químicaRESUMEN
OBJECTIVE: To observe the effects of Panax notoginsenoside (PNS) on tumor necrosis factor-alpha (TNF-alpha) and matrix metalloproteinases-2 (MMP-2) expressions in rats with post-myocardial infarction ventricular remodeling and explore the mechanism. METHODS: Rat models of acute infarction ventricular (AMI) were established by ligation of the left anterior descending coronary artery. Twenty-four hours after the operation, the rats were randomized into control and experimental groups for intragastric administration of normal saline (control), fosinopril and PNS at the low, medium and high doses for 4 consecutive weeks. The effects of PNS on the cardiac function index including the left ventricular end-diastolic dimension (LVIDd), left ventricular end-systolic diameter (LVIDs), ejection fraction (EF), percentage of left ventricular systole (FS), mitral early diastolic flow velocity mouth (MV), and heart rate (HR) were observed, and the changes in TNF-alpha and MMP-2 expression were detected after post-myocardial infarction ventricular remodeling. RESULTS: Compared with the control group, PNS at the medium and high doses produced significant improvements in the EF, FS and MV of the rats (P<0.01 or 0.05). TNF-alpha and MMP-2 expressions were significantly decreased by PNS treatment at low, medium and high doses (P<0.01). CONCLUSION: PNS can inhibit or reduce the expression of TNF-alpha and MMP-2, thereby enhancing left ventricular systolic and diastolic functions, decreasing peripheral resistance, and improving the cardiac function of rats with post-myocardial infarction left ventricular remodeling.