scholarly journals Preparation and Characterization of Colon-Targeted pH/Time-Dependent Nanoparticles Using Anionic and Cationic Polymethacrylate Polymers

Author(s):  
Yasin Turanlı ◽  
Füsun Acartürk
Keyword(s):  
2021 ◽  
Vol 22 ◽  
Author(s):  
Kehan Zhang ◽  
Yilin Li ◽  
Yao Fu ◽  
Tiantian Cui ◽  
Qian Wang ◽  
...  

Background: Herbal medicine Angelica dahurica is widely employed for the treatment of rheumatism and pain relief in China. Oxypeucedanin is a major component of the herb. Objectives : The objectives of this study are aimed at the investigation of mechanism-based inactivation of CYP2B6 and CYP2D6 by oxypeucedanin, characterization of the reactive metabolites associated with the enzyme inactivation, and identification of the P450s participating in the bioactivation of oxypeucedanin. Methods : Oxypeucedanin was incubated with liver microsomes or recombinant CYPs2B6 and 2D6 under designed conditions, and the enzyme activities were measured by monitoring the generation of the corresponding products. The resulting reactive intermediates were trapped with GSH and analyzed by LC-MS/MS. Results : Microsomal incubation with oxypeucedanin induced a time-, concentration-, and NADPH-dependent inhibition of CYPs2B6 and 2D6 with kinetic values of KI/kinact 1.82 µM/0.07 min-1 (CYP2B6) and 8.47 µM/0.044 min-1 (CYP2D6), respectively. Ticlopidine and quinidine attenuated the observed time-dependent enzyme inhibitions. An epoxide and/or γ-ketoenal intermediate(s) derived from oxypeucedanin was/were trapped in microsomal incubations. CYP3A4 was the primary enzyme involved in the bioactivation of oxypeucedanin. Conclusion : Oxypeucedanin was a mechanism-based inactivator of CYP2B6 and CYP2D6. An epoxide and/or γ-ketoenal intermediate(s) may be responsible for the inactivation of the two enzymes.


Parasitology ◽  
1994 ◽  
Vol 109 (5) ◽  
pp. 623-630 ◽  
Author(s):  
L. J. Drake ◽  
A. E. Bianco ◽  
D. A. P. Bundy ◽  
F. Ashall

Excretory/secretory (E/S) material of Trichuris muris was found to contain 2 major peptidases, Mr 85 and 105 kDa, which degrade gelatin optimally at pH 6·0 in sodium dodecyl sulphate–polyacrylamide gels. The peptidases were inactivated diisopropylfluorophosphate, leupeptin and soybean trypsin inhibitor, but were unaffected by inhibitors of aspartic-, cysteine- and metallo-peptidases, indicating that they are serine peptidases. Both enzymes were detectable within 5 h after incubation of worms in culture medium and showed a time-dependent increase in levels. Neither peptidase was detected in worm extracts, suggesting that they are activated during or following secretion from worms. Live worms degraded radio-isotope labelled extracellular matrix protein substratum derived from mammalian cells. Aminopeptidase activities capable of catalysing hydrolysis of amino acyl aminomethylcoumarin (MCA) substrates and a Z-Phe-Arg-MCA-hydrolysing cysteine peptidase activity, were detected in extracts of adult worms but not in E/S material.


1997 ◽  
Vol 101 (20) ◽  
pp. 4085-4089 ◽  
Author(s):  
A. Kadyshevitch ◽  
R. Naaman ◽  
R. Cohen ◽  
D. Cahen ◽  
J. Libman ◽  
...  

2005 ◽  
Vol 127 (4) ◽  
pp. 370-374 ◽  
Author(s):  
X. B. Chen

In electronics packaging, one of the key processes is dispensing fluid materials, such as adhesive, epoxy, encapsulant, onto substrates or printed circuit boards for the purpose of surface mounting or encapsulation. In order to precisely control the dispensing process, the understanding and characterization of the flow behavior of the fluid being dispensed is very important, as the behavior can have a significant influence on the dispensing process. However, this task has proven to be very challenging due to the fact that the fluids for electronics packaging usually exhibit the time-dependent rheological behavior, which has not been well defined in literature. In the paper a study on the characterization of the time-dependent rheological behavior of the fluids for electronics packaging is presented. In particular, a model is developed based on structural theory and then applied to the characterization of the decay and recovery of fluid behavior, which happen in the dispensing process due to the interruption of process. Experiments are carried out to verify the effectiveness of the model developed.


2006 ◽  
Vol 975 ◽  
Author(s):  
Michelle L. Oyen ◽  
Amanpreet K. Bembey ◽  
Andrew J. Bushby

ABSTRACTIndentation techniques are employed for the measurement of mechanical properties of a wide range of materials. In particular, techniques focused at small length-scales, such as nanoindentation and AFM indentation, allow for local characterization of material properties in heterogeneous materials including natural tissues and biomimetic materials. Typical elastic analysis for spherical indentation is applicable in the absence of time-dependent deformation, but is inappropriate for materials with time-dependent responses. Recent analyses for the viscoelastic indentation problem, based on elastic-viscoelastic correspondence, have begun to address the issue of time-dependent deformation during an indentation test. The viscoelastic analysis has been shown to fit experimental indentation data well, and has been demonstrated as useful for characterization of viscoelasticity in polymeric materials and in hydrated mineralized tissues. However, a viscoelastic analysis is not necessarily sufficient for multi-phase materials with fluid flow. In the current work, a poroelastic analysis—based on fluid motion through a porous elastic network—is used to examine spherical indentation creep responses of hydrated biological materials. Both analytical and finite element approaches are considered for the poroelastic Hertzian indentation problem. Modeling results are compared with experimental data from nanoindentation of hydrated bone immersed in water and polar solvents (ethanol, methanol, acetone). Baseline (water-immersed) bone responses are characterized using the poroelastic model and numerical results are compared with altered hydration states due to polar solvents.


2003 ◽  
Author(s):  
X. B. Chen ◽  
W. J. Zhang ◽  
G. Schoenau ◽  
B. W. Surgenor

To effectively control the dispensing process by which fluids are delivered onto substrates in electronics packaging, one of the key issues is to understand and characterize the flow behavior of the fluids being dispensed. However, this task has proven to be a demanding one as the fluids used for electronics packaging usually exhibit the time-dependent rheological behavior, which has not been well documented in the literature. In this paper, the characterization of time-dependent rheological behavior of fluids is studied. In particular, a model using the structural theory is proposed and applied to the characterization of the decay and recovery of fluid behavior, which are typically encountered in a dispensing process. Experiments are conducted to validate the proposed model.


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