Stability of Caffeic Acid Phenethyl Amide (CAPA) in Rat Plasma

2011 ◽  
Vol 26 (5) ◽  
pp. 594-598 ◽  
Author(s):  
John Yang ◽  
Sean M. Kerwin ◽  
Phillip D. Bowman ◽  
Salomon Stavchansky
Keyword(s):  
Caffeic Acid ◽  
Rat Plasma ◽  
Caffeic Acid Phenethyl Amide

scholarly journals Cinnamides Target Leishmania amazonensis Arginase Selectively

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5271
Author(s):  
Edson Roberto da Silva ◽  
Júlio Abel Alfredo dos Santos Simone Come ◽  
Simone Brogi ◽  
Vincenzo Calderone ◽  
Giulia Chemi ◽  
...  
Keyword(s):  
Caffeic Acid ◽  
Selective Inhibition ◽  
Leishmania Amazonensis ◽  
The Other ◽  
Computational Investigation ◽  
Weak Inhibitor ◽  
Starting Point ◽  
Insight Into ◽  
Caffeic Acid Phenethyl Amide

Caffeic acid and related natural compounds were previously described as Leishmania amazonensis arginase (L-ARG) inhibitors, and against the whole parasite in vitro. In this study, we tested cinnamides that were previously synthesized to target human arginase. The compound caffeic acid phenethyl amide (CAPA), a weak inhibitor of human arginase (IC50 = 60.3 ± 7.8 μM) was found to have 9-fold more potency against L-ARG (IC50 = 6.9 ± 0.7 μM). The other compounds that did not inhibit human arginase were characterized as L-ARG, showing an IC50 between 1.3–17.8 μM, and where the most active was compound 15 (IC50 = 1.3 ± 0.1 μM). All compounds were also tested against L. amazonensis promastigotes, and only the compound CAPA showed an inhibitory activity (IC50 = 80 μM). In addition, in an attempt to gain an insight into the mechanism of competitive L-ARG inhibitors, and their selectivity over mammalian enzymes, we performed an extensive computational investigation, to provide the basis for the selective inhibition of L-ARG for this series of compounds. In conclusion, our results indicated that the compounds based on cinnamoyl or 3,4-hydroxy cinnamoyl moiety could be a promising starting point for the design of potential antileishmanial drugs based on selective L-ARG inhibitors.

Simultaneous Determination of Kirenol, Rosmarinic Acid and Caffeic Acid in Rat Plasma and Pharmacokinetic Study After Oral Administration of the Extract of Manxingshizhen Preparation by UPLC-MS/MS

2018 ◽  
Vol 15 (1) ◽  
pp. 74-81 ◽  
Author(s):  
Shuo Sun ◽  
Xue Zhang ◽  
Linda Luo ◽  
Ping Wang ◽  
Mengxuan Bai ◽  
...  
Keyword(s):  
Oral Administration ◽  
Electrospray Ionization ◽  
Simultaneous Determination ◽  
Caffeic Acid ◽  
Pharmacokinetic Study ◽  
Rosmarinic Acid ◽  
Rat Plasma ◽  
Pharmacokinetic Parameters ◽  
Tandem Mass Spectrometric

Introduction: A rapid, sensitive and convenient ultra-performance liquid chromatography with tandem mass spectrometric detection (UPLC-MS/MS) method has been validated and applied to the simultaneous determination of kirenol, rosmarinic acid and caffeic acid after oral administration of the extract of Manxingshizhen preparation in rat plasma. Materials and Methods: Puerarin was selected as the internal standard (IS). The plasma sample preparation was pretreated by liquid-liquid extraction of the mixture with ethyl acetate. All analytes were simultaneously detected in multiple reaction monitoring (MRM) mode via both the positive electrospray ionization (ESI+) and negative electrospray ionization (ESI). In the experiment, all calibration curves revealed good linearity (r > 0.999). The LLOQ were between 0.80-2.00 ng/mL, respectively. Besides, the intra-day and inter-day precision ranged from 6.4 to 13.8%, respectively. Moreover, the accuracy was within - 11.4% and 12.8% for all the QC levels of all analytes. The extraction recoveries of the analytes and IS in plasma at three concentration levels ranged from 88.5 to 103.2%, moreover, the matrix effects of all the analytes and the IS were found to be satisfied with the acceptable range of 89.8%-101.7%. Meanwhile, the RSD values of stability met the requirement of not more than 15%. Furthermore, the pharmacokinetic parameters of three compounds were analyzed using concentrationtime profiles. Conclusion and Results: Plasma concentrations of the three compounds were determined up to 24 h after oral administration, and their pharmacokinetic parameters were in agreement with previous studies. The validated method was successfully applied in a pharmacokinetic study in rat plasma after oral administration of Manxingshizhen preparation.

scholarly journals Caffeic acid phenethyl amide improves glucose homeostasis and attenuates the progression of vascular dysfunction in Streptozotocin-induced diabetic rats

2013 ◽  
Vol 12 (1) ◽  
pp. 99 ◽  
Author(s):  
Yi-Jin Ho ◽  
Wen-Pin Chen ◽  
Tzong-Cherng Chi ◽  
Ching-Chia Chang Chien ◽  
An-Sheng Lee ◽  
...  
Keyword(s):  
Caffeic Acid ◽  
Glucose Homeostasis ◽  
Vascular Dysfunction ◽  
Diabetic Rats ◽  
Caffeic Acid Phenethyl Amide

Microencapsulation of caffeic acid phenethyl ester and caffeic acid phenethyl amide by inclusion in hydroxypropyl-β-cyclodextrin

2018 ◽  
Vol 254 ◽  
pp. 260-265 ◽  
Author(s):  
E. Manuela P.J. Garrido ◽  
Ana S. Cerqueira ◽  
Daniel Chavarria ◽  
Tiago Silva ◽  
Fernanda Borges ◽  
...  
Keyword(s):  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Caffeic Acid Phenethyl Amide
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