scholarly journals Towards a Comprehensive Understanding of Anesthetic Mechanisms of Action: A Decade of Discovery

2019 ◽  
Vol 40 (7) ◽  
pp. 464-481 ◽  
Author(s):  
Hugh C. Hemmings ◽  
Paul M. Riegelhaupt ◽  
Max B. Kelz ◽  
Ken Solt ◽  
Roderic G. Eckenhoff ◽  
...  
Keyword(s):  
Mechanisms Of Action ◽  
Comprehensive Understanding ◽  
Anesthetic Mechanisms

scholarly journals Aberrance of Zinc Metalloenzymes-Induced Human Diseases and Its Potential Mechanisms

Nutrients ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 4456
Author(s):  
Yunqi Cheng ◽  
Hongping Chen
Keyword(s):  
Enzyme Activity ◽  
Immune Responses ◽  
Enzymatic Activity ◽  
Mechanisms Of Action ◽  
Zinc Homeostasis ◽  
Human Diseases ◽  
Comprehensive Understanding ◽  
Physiological Processes ◽  
Zinc Metalloenzymes ◽  
Regulatory Functions

Zinc, an essential micronutrient in the human body, is a component in over 300 enzymes and participates in regulating enzymatic activity. Zinc metalloenzymes play a crucial role in physiological processes including antioxidant, anti-inflammatory, and immune responses, as well as apoptosis. Aberrant enzyme activity can lead to various human diseases. In this review, we summarize zinc homeostasis, the roles of zinc in zinc metalloenzymes, the physiological processes of zinc metalloenzymes, and aberrant zinc metalloenzymes in human diseases. In addition, potential mechanisms of action are also discussed. This comprehensive understanding of the mechanisms of action of the regulatory functions of zinc in enzyme activity could inform novel zinc-micronutrient-supply strategies for the treatment of diseases.

New insights into the mechanism of action of the cyclopalladated complex - CP2 in Leishmania : Calcium Dysregulation, Mitochondrial Dysfunction and Cell Death

2021 ◽  
Author(s):  
Angela M. A. Velásquez ◽  
Paula J. Bartlett ◽  
Irwin A. P. Linares ◽  
Thais G. Passalacqua ◽  
Daphne D. L. Teodoro ◽  
...  
Keyword(s):  
Cell Death ◽  
Mechanism Of Action ◽  
Molecular Mechanisms ◽  
Parasite Load ◽  
Current Treatment ◽  
Mechanisms Of Action ◽  
S Phase ◽  
Comprehensive Understanding ◽  
Calcium Dysregulation ◽  
Cycle Arrest

The current treatment of leishmaniasis is based on few drugs that present several drawbacks such as high toxicity, difficult administration route, and low efficacy. These disadvantages raise the necessity to develop novel antileishmanial compounds allied to a comprehensive understanding of their mechanisms of action. Here, we elucidate the probably mechanism of action of the antileishmanial binuclear cyclopalladated complex [Pd(dmba)(μ-N 3 )] 2 ( CP2 ) in Leishmania amazonensis . CP2 causes oxidative stress in the parasite resulting in disruption of mitochondrial Ca 2+ homeostasis, cell cycle arrest at S-phase, increasing the ROS production and overexpression of stress-related and cell detoxification proteins, collapsing the Leishmania mitochondrial membrane potential and promotes apoptotic-like features in promastigotes leading to necrosis or directs programmed cell death (PCD)-committed cells toward necrotic-like destruction. Moreover, CP2 is able to reduce the parasite load in both liver and spleen in Leishmania infantum -infected hamsters when treated for 15 days with 1.5 mg/Kg/day CP2 , expanding its potential application in addition to the already known effectiveness on cutaneous leishmaniasis for the treatment of visceral leishmaniasis, showing the broad spectrum of action of this cyclopalladated complex. The data herein presented bring new insights into the CP2 molecular mechanisms of action, assisting to promote its rational modification to improve both safety and efficacy.

scholarly journals Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity

2021 ◽  
Vol 11 ◽  
Author(s):  
Lee Han Jie ◽  
Ibrahim Jantan ◽  
Syaratul Dalina Yusoff ◽  
Juriyati Jalil ◽  
Khairana Husain
Keyword(s):  
Drug Discovery ◽  
Scientific Information ◽  
Mechanisms Of Action ◽  
Comprehensive Understanding ◽  
Anticancer Activities ◽  
Pharmacological Activities ◽  
Disease States ◽  
Wide Range

Sinensetin, a plant-derived polymethoxylated flavonoid found in Orthosiphon aristatus var. aristatus and several citrus fruits, has been found to possess strong anticancer activities and a variety of other pharmacological benefits and promising potency in intended activities with minimal toxicity. This review aims to compile an up-to-date reports of published scientific information on sinensetin pharmacological activities, mechanisms of action and toxicity. The present findings about the compound are critically analyzed and its prospect as a lead molecule for drug discovery is highlighted. The databases employed for data collection are mainly through Google Scholar, PubMed, Scopus and Science Direct. In-vitro and in-vivo studies showed that sinensetin possessed strong anticancer activities and a wide range of pharmacological activities such as anti-inflammatory, antioxidant, antimicrobial, anti-obesity, anti-dementia and vasorelaxant activities. The studies provided some insights on its several mechanisms of action in cancer and other disease states. However, more detail mechanistic studies are needed to understand its pharmacological effects. More in vivo studies in various animal models including toxicity, pharmacokinetic, pharmacodynamic and bioavailability studies are required to assess its efficacy and safety before submission to clinical studies. In this review, an insight on sinensetin pharmacological activities and mechanisms of action serves as a useful resource for a more thorough and comprehensive understanding of sinensetin as a potential lead candidate for drug discovery.

Case Formulation and Design of Behavioral Treatment Programs

2003 ◽  
Vol 19 (3) ◽  
pp. 164-174 ◽  
Author(s):  
Stephen N. Haynes ◽  
Andrew E. Williams
Keyword(s):  
Functional Analysis ◽  
Behavior Problems ◽  
Behavioral Treatment ◽  
Clinical Case ◽  
Relative Magnitude ◽  
Mechanisms Of Action ◽  
Treatment Programs ◽  
Case Formulation ◽  
Functional Relations ◽  
Causal Variables

Summary: We review the rationale for behavioral clinical case formulations and emphasize the role of the functional analysis in the design of individualized treatments. Standardized treatments may not be optimally effective for clients who have multiple behavior problems. These problems can affect each other in complex ways and each behavior problem can be influenced by multiple, interacting causal variables. The mechanisms of action of standardized treatments may not always address the most important causal variables for a client's behavior problems. The functional analysis integrates judgments about the client's behavior problems, important causal variables, and functional relations among variables. The functional analysis aids treatment decisions by helping the clinician estimate the relative magnitude of effect of each causal variable on the client's behavior problems, so that the most effective treatments can be selected. The parameters of, and issues associated with, a functional analysis and Functional Analytic Clinical Case Models (FACCM) are illustrated with a clinical case. The task of selecting the best treatment for a client is complicated because treatments differ in their level of specificity and have unequally weighted mechanisms of action. Further, a treatment's mechanism of action is often unknown.

Enkephalin influences on behavioral and neural plasticity: Mechanisms of action.

1990 ◽  
Author(s):  
Joe L. Martinez ◽  
Patricia H. Janak ◽  
Susan B. Weinberger ◽  
Gery Schulteis
Keyword(s):  
Neural Plasticity ◽  
Mechanisms Of Action

The diabetic wound healing effect of a two-herb formula and its mechanisms of action

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
CBS Lau ◽  
VKM Lau ◽  
CL Liu ◽  
PKK Lai ◽  
JCW Tam ◽  
...  
Keyword(s):  
Wound Healing ◽  
Mechanisms Of Action ◽  
Diabetic Wound ◽  
Healing Effect ◽  
Diabetic Wound Healing ◽  
Wound Healing Effect

Mechanisms of action of antihyperglycemic mexicanolides isolated from Swietenia humillis: in vivo and in silico approaches

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381 ◽  
Author(s):  
B Ovalle-Magallanes ◽  
A Madariaga-Mazón ◽  
A Navarrete ◽  
R Mata
Keyword(s):  
In Silico ◽  
Mechanisms Of Action

Inhibition of the Activities of α2-Plasmin inhibitor (PI) and CI inhibitor (CI-Inh) by the Synthetic Fibrinolytic Agent, 3-Hydroxypropyl Flufenamide (Flu-HPA)

1979 ◽  
Author(s):  
L Miles ◽  
J Burnier ◽  
M Verlander ◽  
M Goodman ◽  
A Kleiss ◽  
...  
Keyword(s):  
Plasminogen Activators ◽  
Inhibitory Effect ◽  
Mechanisms Of Action ◽  
Flufenamic Acid ◽  
Clot Lysis ◽  
Factor Xiia ◽  
Dependent Inhibition ◽  
Normal Human ◽  
Plasmin Inhibitor

Flu-HPA is one of a series of flufenamic acid derivations that enhances plasminogen-dependent clot lysis in vitro. Studies of possible mechanisms of action of Flu-HPA were undertaken. The influence of Flu-HPA on the inhibition of purified plasmin by purified PI was studied. PI activity was assessed by its inhibition of the clevage of the tripeptide S-2251 (H-D-Val-Leu-Lys-pNA) by plasmin. Flu-HPA was dissolved in DMF or in methonol and preincubated with PI before addition of plasmin. At Flu-HPA concentrations greater than 1mM and up to 60mM, the inhibitory activity of PI was totally lost. The inhibitory effect of normal human plasma on plasmin was also completely abolished at concentrations of Flu-HPA between 2.5 and 40mM. The effect of Flu-HPA on the inhibition of purified plasma kallikrein by purified CI-Inh was also studied. CI-Inh activity was measured by its inhibition of cleavage of the tripeptide Bz-Pro-Phe-Arg-pNA by kallikrein. When Flu-HPA, dissolved in DMF or in methonol, was preincubated with CI-Inh, a concentration dependent inhibition of CI-Inh activity was observed. CI-Inh activity was abolished by concentrations of Flu-HPA greater than 1mM. Flu-HPA also inhibited the activity of CI-Inh on purified Factor XIIa. These observations suggest that this flufenamic acid derivative may enhance fibrinolysis not only by inhibiting PI activity but also by decreasing the inactivation of plasminogen activators by CI-Inh.

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