Crude decoction, aqueous and ethanolic extracts of two medicinal plants （Psidiura guajava and Diospyros raespiliformis）, widely used in the central plateau of Burkina Faso to treat many diseases were evaluated for t...Crude decoction, aqueous and ethanolic extracts of two medicinal plants （Psidiura guajava and Diospyros raespiliformis）, widely used in the central plateau of Burkina Faso to treat many diseases were evaluated for their antagonistic effects on caffeine induced calcium release from sarcoplasmic reticulum of rat skeletal muscle cells. These different extracts showed a decrease of caffeine induced calcium release in a dose dependent manner. Comparison of the results showed that Psidiura guajava leaf extracts are more active than extracts of Diospyros mespiliformis and that crude decoctions show better inhibitory activity. The observed results could explaine their use as antihypertensive and antidiarrhoeal agents in traditional medicine, by inhibiting intracellular calcium release.展开更多
Objective To investigate the effect of succinylcholine on the dose-response relationship of sub-sequently administered rocuronium in healthy patients. Methods Forty-eight ASA physical status I-II patients,aged 17-65 y...Objective To investigate the effect of succinylcholine on the dose-response relationship of sub-sequently administered rocuronium in healthy patients. Methods Forty-eight ASA physical status I-II patients,aged 17-65 years, scheduled for elective general surgery, were randomly assigned to either the rocuronium treat-ment group (R) or succinylcholine-rocuronium treatment group (SR). General anesthesia was induced with thio-pental 4 to 6mg/kg and fentanyl 2 to 5/μg/kg intravenously and maintained with 60% nitrous oxide in oxygen. Addi-tional doses of thiopental or fentanyl were administered as required. The dose-response relationship of rocuroniumwas determined by the single dose-response technique. In R group (n =24) , rocuronium was given after induction ofanesthesia. In SR group (n =24) , patients were intubated after 1. 5mg/kg of succinylcholine and rocuronium wasgiven after the complete recovery of neuromuscular blockade from succinylcholine. Patients were further randomlydivided into 4 subgroups receiving 150, 200, 250 or 300μg/kg of rocuronium respectively in both groups. Neuro-muscular function was assessed accelographically with train-of-four (TOF) stimulation at the wrist every 12s (usingthe TOF Guard? accelerometer). The relationship between probit-tranformed percentage depression of first twitchheight (Th) of train-of-four stimulation and logarithm dose of rocuronium was analyzed using linear regression.Results The dose-response curve of rocuronium after succinylcholine was shifted to the left in a parallel fashioncompared with that of rocuronium given alone. ED50 and ED95 of rocuronium were 193 ± 69 and 367 ± 73μg/kg re-spectively in R group, and 158 ±35 and 317 ±80μg/kg respectively in SR group (P <0.05). Conclusion Suc-cinylcholine shifts the dose-response curve of rocuronium to the left and potentiates the effects of the neuromuscularblockade by about 15% of subsequently administered rocuronium. Lower doses of rocuronium are required afterprior succinylcholine.展开更多
The present study was designed to establish a suitable assay to explore CCR2 b receptor antagonists from the natural products of Artemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as ...The present study was designed to establish a suitable assay to explore CCR2 b receptor antagonists from the natural products of Artemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as a cell-based assay suitable for 384-well microplate and used for screening CCR2 b receptor antagonists from natural products. Through establishing suitable conditions, the assay was shown to be suitable for screening of CCR2 b receptor antagonists. Seven compounds were identified in preliminary screening. Five of them showed evident dose-response relationship in secondary screening. The structure–activity relationship study suggested that 7-position hydroxyl group of flavonoids was necessary, a polar group should be introduced on the 3-position, and the substituents on 2-position benzene ring of flavonoids have little influence on the potentency of the inhibition activity on CCR2 b receptor. The ortho-position dihydroxyl structure in quinic acid compounds may be important. In conclusion, Compounds HR-1, 5, 7, and AR-20, 35 showed activity as antagonist of CCR2 b receptor, which shed lights on the development of novel drugs as CCR2 b receptor antagonists for preventing inflammation related diseases.展开更多
文摘Crude decoction, aqueous and ethanolic extracts of two medicinal plants （Psidiura guajava and Diospyros raespiliformis）, widely used in the central plateau of Burkina Faso to treat many diseases were evaluated for their antagonistic effects on caffeine induced calcium release from sarcoplasmic reticulum of rat skeletal muscle cells. These different extracts showed a decrease of caffeine induced calcium release in a dose dependent manner. Comparison of the results showed that Psidiura guajava leaf extracts are more active than extracts of Diospyros mespiliformis and that crude decoctions show better inhibitory activity. The observed results could explaine their use as antihypertensive and antidiarrhoeal agents in traditional medicine, by inhibiting intracellular calcium release.
文摘Objective To investigate the effect of succinylcholine on the dose-response relationship of sub-sequently administered rocuronium in healthy patients. Methods Forty-eight ASA physical status I-II patients,aged 17-65 years, scheduled for elective general surgery, were randomly assigned to either the rocuronium treat-ment group (R) or succinylcholine-rocuronium treatment group (SR). General anesthesia was induced with thio-pental 4 to 6mg/kg and fentanyl 2 to 5/μg/kg intravenously and maintained with 60% nitrous oxide in oxygen. Addi-tional doses of thiopental or fentanyl were administered as required. The dose-response relationship of rocuroniumwas determined by the single dose-response technique. In R group (n =24) , rocuronium was given after induction ofanesthesia. In SR group (n =24) , patients were intubated after 1. 5mg/kg of succinylcholine and rocuronium wasgiven after the complete recovery of neuromuscular blockade from succinylcholine. Patients were further randomlydivided into 4 subgroups receiving 150, 200, 250 or 300μg/kg of rocuronium respectively in both groups. Neuro-muscular function was assessed accelographically with train-of-four (TOF) stimulation at the wrist every 12s (usingthe TOF Guard? accelerometer). The relationship between probit-tranformed percentage depression of first twitchheight (Th) of train-of-four stimulation and logarithm dose of rocuronium was analyzed using linear regression.Results The dose-response curve of rocuronium after succinylcholine was shifted to the left in a parallel fashioncompared with that of rocuronium given alone. ED50 and ED95 of rocuronium were 193 ± 69 and 367 ± 73μg/kg re-spectively in R group, and 158 ±35 and 317 ±80μg/kg respectively in SR group (P <0.05). Conclusion Suc-cinylcholine shifts the dose-response curve of rocuronium to the left and potentiates the effects of the neuromuscularblockade by about 15% of subsequently administered rocuronium. Lower doses of rocuronium are required afterprior succinylcholine.
基金supported by the Major Scientific and Technological Special Project for Significant New Drugs Creation(No.2012ZX09504001-001)National Natural Science Foundation of China(No.81102876+2 种基金81430082)the Fundamental Research Funds for the Central Universities(No.2015ZD005)333 high level project of Jiangsu Province(NO.BRA2014245)
文摘The present study was designed to establish a suitable assay to explore CCR2 b receptor antagonists from the natural products of Artemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as a cell-based assay suitable for 384-well microplate and used for screening CCR2 b receptor antagonists from natural products. Through establishing suitable conditions, the assay was shown to be suitable for screening of CCR2 b receptor antagonists. Seven compounds were identified in preliminary screening. Five of them showed evident dose-response relationship in secondary screening. The structure–activity relationship study suggested that 7-position hydroxyl group of flavonoids was necessary, a polar group should be introduced on the 3-position, and the substituents on 2-position benzene ring of flavonoids have little influence on the potentency of the inhibition activity on CCR2 b receptor. The ortho-position dihydroxyl structure in quinic acid compounds may be important. In conclusion, Compounds HR-1, 5, 7, and AR-20, 35 showed activity as antagonist of CCR2 b receptor, which shed lights on the development of novel drugs as CCR2 b receptor antagonists for preventing inflammation related diseases.
