RESUMEN
To reveal the rationality of compatibility of Salviae Miltiorrhizae Radix et Rhizoma(SMRR) and Puerariae Lobatae Radix(PLR) from the perspective of pharmacokinetics, this study established a UPLC-MS/MS method for quantitative determination of PLR flavonoids(3'-hydroxy puerarin, puerarin, puerarin 6â³-O-xyloside, 3'-methoxy puerarin, puerarin apioside) and salvianolic acids and tanshinones(salvianolic acid B, cryptotanshinone, and tanshinone â ¡_A) in plasma of rats. Rats were given SMRR extract, PLR extract, and SMRR-PLR extract by gavage and then plasma was collected at different time. UPLC separation was performed under the following conditions: Eclipse C_(18) column(2.1 mm×50 mm, 1.8 µm), 0.1% formic acid in water(A)-0.1% formic acid in acetonitrile(B) as mobile phase for gradient elution. Conditions for MS are as below: multiple reaction monitoring(MRM), ESI~(+/-). Comprehensive validation of the UPLC-MS/MS method(specifically, from the aspects of calibration curve, precision, accuracy, repeatability, stability, matrix effect, extract recovery) was performed and the result demonstrated that it complied with quantitative analysis requirements for biological samples. Compared with SMRR extract alone or PLR extract alone, SMRR-PLR extract significantly increased the AUC and C_(max) of PLR flavonoids and tanshinones in rat plasma, suggesting that the combination of SMRR and PLR promoted the absorption of the above components. The underlying mechanism needs to be further studied.
Asunto(s)
Medicamentos Herbarios Chinos , Pueraria , Salvia miltiorrhiza , Animales , Cromatografía Líquida de Alta Presión , Medicamentos Herbarios Chinos/farmacocinética , Raíces de Plantas/química , Pueraria/química , Ratas , Rizoma/química , Salvia miltiorrhiza/química , Espectrometría de Masas en TándemRESUMEN
OBJECTIVE: To study the effect of the ethanol extract of stir-bake to yellowish Meliae Toosendan Fructus on nerve system and its mechanism. METHODS: The effect of the ethanol extract on sensory nerve was carried out through ache models induced by hot board method and radiant heat stimulation method in mice. The thermalgesia liminal value was investigated. The effect of the ethanol extract on the A-delta fiber and C fiber was measured by electrical stimulation procedure. Motor nerve conduction velocity (NCV) was measured by indirect detection method in vivo. The pathology changes of the motor nerve were observed by transmission electron microscope and the silver stain test. RESULTS: The ethanol extract of Meliae Toosendan Fructus could increase the thermalgesia liminal value of mice and reduce the conduction velocity of motor nerves. Meanwhile, pathology results showed the changes of the fiber of motor nerve, including demyelination and the number of Schwann cells dropping. CONCLUSION: The ethanol extract of stir-bake to yellowish Meliae Toosendan Fructus can reduce the pain sensitivity of mice and slow down NCV, which may be related to decreasing of the number of Schwann cells.
Asunto(s)
Meliaceae/química , Conducción Nerviosa/efectos de los fármacos , Umbral del Dolor/efectos de los fármacos , Dolor/fisiopatología , Extractos Vegetales/farmacología , Nervio Ciático/fisiopatología , Animales , Recuento de Células , Femenino , Frutas/química , Masculino , Ratones , Neuronas Motoras/fisiología , Fibras Nerviosas Amielínicas/fisiología , Conducción Nerviosa/fisiología , Dimensión del Dolor , Extractos Vegetales/administración & dosificación , Extractos Vegetales/aislamiento & purificación , Ratas , Ratas Sprague-Dawley , Células de Schwann/fisiología , Nervio Ciático/efectos de los fármacosRESUMEN
Erigeron multiradiatus (Lindl.) Benth is a traditional Tibetan medicine herb long used to treat various diseases related to inflammation. Our previous phytochemical studies on E. multiradiatus resulted in the isolation of scutellarin, which is a known flavone glucuronide with comprehensive pharmacological actions. In present study, we investigated the inhibition action of scutellarin on high glucose-induced vascular inflammation in human endothelial cells (ECV304 cells). Consistent with previous reports, exposure of ECV304 cells to high glucose for 24 h caused an increase of intercellular adhesion molecule-1 (ICAM-1) and monocyte chemoattractant protein 1 (MCP-1), and promoted cell adhesion between monocyte and ECV304 cells. However, pretreatment with scutellarin (0.1 and 1 microM) reversed these effects in a concentration-dependent manner. Scutellarin was able to inhibit the activation of NF-kappaB induced by high glucose in ECV304 cells. Furthermore, although oral administration of scutellarin (10 and 50 mg/kg) did not produce significant antihyperglycemic action, it lowered the serum MCP-1 levels significantly in alloxan-induced diabetic mice. Therefore, our results suggest that scutellarin has anti-inflammation effect that may afford some protection against hyperglycemia-induced vascular inflammatory both in vitro and in vivo.
Asunto(s)
Apigenina/aislamiento & purificación , Apigenina/farmacología , Arteritis/etiología , Arteritis/prevención & control , Erigeron/química , Glucosa/efectos adversos , Glucuronatos/aislamiento & purificación , Glucuronatos/farmacología , Animales , Apigenina/uso terapéutico , Adhesión Celular/efectos de los fármacos , Células Cultivadas , Quimiocina CCL2/metabolismo , Diabetes Mellitus Experimental/complicaciones , Endotelio Vascular/metabolismo , Glucuronatos/uso terapéutico , Humanos , Hiperglucemia/complicaciones , Molécula 1 de Adhesión Intercelular/metabolismo , Ratones , FN-kappa B/metabolismo , FitoterapiaRESUMEN
OBJECTIVE: To evaluate the effect and acute toxicity of different extraction of Fructus Meliae Toosendan. METHODS: Samples were extracted from Fructus Meliae Toosendan using petroleum ether (I), ethyl acetate (II), 80% alcohol (III) or water (IV). Mices writhing response were induce by ip 0.9% acetic acid and foot ache were induced by sc formaldehyde. Mices feet or ears were smeated by sccarrageenin or dimethylbenzene. And the effects of these samples were evaluated on these models. RESULTS: The sample II 40 g/kg significantly decreased the writhing response induced by acetic acid and relieved mice foot pain induced by formaldehyde, inhibited the swelling of mice ear induced by dimethylbenzene. It markedly decreased the body weight and increased the index of testes in mice. The sample III 20 g/kg inhibited foot swelling induced by carrageenin and ear swelling induced by dimethylbenzene in mice. The sample I significantly relieved the foot pain induced by formaldehyde, increased the indexes of testis and adrenal gland in mice. The sample IV had no action on pain or inflammatory in mice. The LD50 of the sample II was 82.85 g/kg. And ig the sample I 133.2 g/kg, sample III 122.0 g/kg or sample IV 52.0 g/kg could not induce mice to death. CONCLUSION: The sample II has anti-inflammatory and antalgic action. But it also has serious acute toxicity. These results show that the efficacious component of Fructus Meilae Toosendan may exist in the ethyl acetate extraction, The toxicity and efficacious component may be the same material.