Abstract：
:Evaluation of possible interactions with enzymes of drug metabolism is an important part of studies on safety and, in general, on the properties of any drug or biologically active compound. Here, focus is given on interactions of three sesquiterpenes (beta-caryophyllene oxide (CAO), trans-nerolidol (tNER) and farnesol (FAR)) with CYP3A4. To determine the CYP3A4 activity, specific substrates testosterone (TES) and midazolam (MDZ) were used. In human liver microsomes, the CAO inhibited the MDZ 1´-hydroxylation by mixed type inhibition and K(i) 46.6 microM; TES 6beta-hydroxylation was inhibited more strongly by tNER by the same mechanism and with K(i) of 32.5 microM. Results indicated a possibility of different mode of interaction of both compounds within the active site of CYP3A4 and this was why the molecular docking study was done. The docking experiments showed that the studied sesquiterpenes (CAO and tNER) bound to the CYP3A4 active site cause a significant decrease of binding affinity of substrates tested which corresponded well to the inhibition studies. The inhibition observed, however, most probably does not pose a real harm to microsomal drug metabolism as the levels of sesquiterpenes in plasma (assuming the use of these compounds as spices or flavoring additives) does not usually exceed micromolar range. Hence, the interaction of drugs metabolized by CYP3A4 with sesquiterpenes is less probable.
journal_name
Physiol Resjournal_title
Physiological researchauthors
Špičáková A,Bazgier V,Skálová L,Otyepka M,Anzenbacher Pdoi
10.33549/physiolres.934323subject
Has Abstractpub_date
2019-11-22 00:00:00pages
S51-S58issue
Suppl 1eissn
0862-8408issn
1802-9973pii
934323journal_volume
68pub_type
杂志文章abstract：:Dihydrotestosterone (DHT) originates via irreversible reduction of testosterone by catalytic activity of 5alpha-reductase enzyme and it is demonstratively the most effective androgen. Androgens influence adipose tissue in men either directly by stimulation of the androgen receptor or indirectly, after aromatization, b...
journal_title：Physiological research
pub_type： 杂志文章,评审
doi：10.33549/physiolres.932080
更新日期：2011-01-01 00:00:00
abstract：:Research and clinical implications on novel cardiac biomarkers has intensified significantly in the past few years. The high-sensitive troponin T (hscTnT) assay plays a dominant role in diagnostic algorithm regarding myocardial injury in adults. Despite generally accepted use of hscTnT there are no data about physiolo...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.933704
更新日期：2018-05-04 00:00:00
abstract：:Graves' disease affects approximately 3 % of women and 0.5 % of men. The first-choice therapy is based on the administration of thyrostatic drugs. However, approximately half of patients relapse within two years of discontinuation. These patients must then decide whether to re-initiate thyrostatics, which may have ser...
journal_title：Physiological research
pub_type： 杂志文章,评审
doi：10.33549/physiolres.934018
更新日期：2018-11-28 00:00:00
abstract：:Sexually mature female Wistar rats were given daily intragastric doses of ethinylestradiol (EE) and levonorgestrel (LE) used normally in women: (1) 0.03 mg EE and 0.05 mg LE; (2) 0.04 mg EE and 0.075 mg LE; (3) 0.03 mg EE and 0.125 mg LE. All groups were treated for 6 months in 5-day cycles (four-day treatment with a ...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：1998-01-01 00:00:00
abstract：:Impressive advances in molecular genetic techniques allow to analyze the effects of natural selection on the development of human genome. For example, the trend towards blonde hair and blue eyes was documented. The approach to analyze possible effects of natural selection on the evolution of recent phenotypes with hig...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.933885
更新日期：2018-05-04 00:00:00
abstract：:Endothelin-1 (ET-1) acts on ET(A) and ET(B) receptors and has been implicated in hemorrhagic shock (shock). We determined effect of shock and resuscitation by hypertonic saline (saline) or centhaquin on ET(A) and ET(B) receptor expression. Rats were anesthetized, a pressure catheter was placed in the left femoral arte...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.933856
更新日期：2018-06-27 00:00:00
abstract：:Vascular endothelial growth factor (VEGF) has an important role in the pathogenesis of retinopathy of prematurity (ROP) and inhibition of VEGF expression in the neovascular phase might prevent destructive neovascularization in ROP. It is suggested that retinoids exert a highly potent antiangiogenic activity by inhibit...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：2006-01-01 00:00:00
abstract：:Experiments were conducted to study the effect of goldthioglucose (GTG) upon the processes associated with lipid peroxidation. The glucose-6-phosphate dehydrogenase activity (G6PD; E.C. 1. 1.1.49) in red blood cells (RBC) and the amount of malonaldehyde precursors (MDA) per gram of brain, liver and kidney were determi...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：1999-01-01 00:00:00
abstract：:Activation of calmodulin dependent protein kinase (CaMK)II by exercise is beneficial in controlling membrane lipids associated with type 2 diabetes and obesity. Regulation of lipid metabolism is crucial in the improvement of type 2 diabetes and obesity associated symptoms. The role of CaMKII in membrane associated lip...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.933509
更新日期：2017-12-20 00:00:00
abstract：:In this experiment we studied the effect of different pedalling rates during cycling at a constant power output (PO) 132+/-31 W (mean+/-S.D.), corresponding to 50% VO2 max, on the oxygen uptake and the magnitude of the slow component of VO2 kinetics in humans. The PO corresponded to 50% of VO2 max, established during ...
journal_title：Physiological research
pub_type： 临床试验,杂志文章,随机对照试验
doi：
更新日期：1998-01-01 00:00:00
abstract：:Neutral trehalase 1 (Nth1) from Saccharomyces cerevisiae catalyzes disaccharide trehalose hydrolysis and helps yeast to survive adverse conditions, such as heat shock, starvation or oxidative stress. 14-3-3 proteins, master regulators of hundreds of partner proteins, participate in many key cellular processes. Nth1 is...
journal_title：Physiological research
pub_type： 杂志文章,评审
doi：10.33549/physiolres.933950
更新日期：2019-04-30 00:00:00
abstract：:We sought to examine the association between maternal erythrocyte omega-3, omega-6 and trans fatty acids and risk of preeclampsia. We conducted a case-control study of 170 women with proteinuric, pregnancy-induced hypertension and 185 normotensive pregnant women who delivered at Harare Maternity Hospital, Harare, Zimb...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：2007-01-01 00:00:00
abstract：:This study aimed to examine relationships between DHEA(S), anthropometric parameters, oral glucose tolerance test derived data and lipid spectra in a Czech non-diabetic population. 380 healthy volunteers both with and without a family history of diabetes type 2 (DM2) were enrolled into the study (women: n=235, age 28....
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：2008-01-01 00:00:00
abstract：:The effects of 8-days treatment with 17alpha-estradiol (33.3 microg/kg) and progesterone (1.7 mg/kg) on plasma lipids and fatty acid composition of plasma phospholipids were examined in intact (INT) and bilaterally common carotid arteries occluded (BCO) male Wistar rats. Significant decrease of triglyceride level was ...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.932590
更新日期：2014-01-01 00:00:00
abstract：:Parenteral nutrition-associated liver disease (PNALD) is a severe complication in patients completely dependent on parenteral nutrition (PN). The gold diagnostic standard, liver biopsy, is associated with significant health risk and therefore its use is limited. MicroRNAs (miRNAs) are small non-coding regulatory RNA m...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.934103
更新日期：2019-08-29 00:00:00
abstract：:Anthracyclines, e.g. doxorubicin, pirarubicin, are widely used as cytostatic agents in the polymer nanotherapeutics designed for the highly effective antitumor therapy with reduced side effects. However, their precise dosage scheme needs to be optimized, which requires an accurate method for their quantification on th...
journal_title：Physiological research
pub_type： 杂志文章,评审
doi：10.33549/physiolres.933140
更新日期：2015-01-01 00:00:00
abstract：:The effect of ethanol on the structural development of the central nervous system was studied in offspring of Wistar rats, drinking 20 % ethanol during pregnancy and till the 28th day of their postnatal life. The structural changes in the hippocampus and dentate gyrus were analyzed at the age of 18, 35 and 90 days. A ...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：2008-01-01 00:00:00
abstract：:Nephrotoxicity of cisplatin (CP) involves renal oxidative stress and inflammation, and sesamin (a major liganin in many plants) has strong antioxidant and antiinflammatory actions. Therefore, we investigated here the possible mitigative action of sesamin on CP nephrotoxicity in rats. Sesamin was given orally (5 mg/kg/...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.934142
更新日期：2020-02-19 00:00:00
abstract：:Pulmonary hypertension (PH) unresponsive to pharmacological intervention is considered a contraindication for orthotopic heart transplantation (OHTX) due to risk of postoperative right-heart failure. In this prospective study, we describe our experience with a treatment strategy of improving severe PH in heart transpl...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.932158
更新日期：2011-01-01 00:00:00
abstract：:Gestational diabetes mellitus (GDM) and polycystic ovary syndrome (PCOS) are distinct pathologies with impaired insulin sensitivity as a common feature. The aim of this study was to evaluate the response of fat tissue adipokines and gastrointestinal incretins to glucose load in patients diagnosed with one of the two d...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.933366
更新日期：2017-05-04 00:00:00
abstract：:Chronic kidney disease adversely affects the structure and metabolism of bone tissue, which may be a result of disturbed biochemical processes in adipose tissue. Renal replacement therapy is a life-saving therapy but it does not restore all metabolic functions and sometimes even escalates some disturbances. The study ...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.934118
更新日期：2019-12-30 00:00:00
abstract：:It is believed that omentin is secreted by stromal cells of adipose tissue and modulates insulin sensitivity. Data from a few studies have shown lower serum omentin in obese children and higher in anorexia nervosa. However, to date, there is lack of research on serum omentin concentrations in adolescent patients in a ...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.932841
更新日期：2015-01-01 00:00:00
abstract：:As an autoimmune disease, type 1 diabetes mellitus (DM) can be associated with other autoimmune disorders. The aim of this study was to detect subclinically associated autoimmune thyroid disease, coeliac disease, and Addison's disease. The presence of autoantibodies was evaluated with special regard to the control of ...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：2005-01-01 00:00:00
abstract：:The objective of this study was to evaluate the effect of diet and 677 C-->T mutation of the methylenetetrahydrofolate reductase (MTHFR) gene on plasma homocyst(e)ine concentrations in an adolescent population (113 males, age: 14.2+/-2.4 years; 202 females, age: 14.9+/-2.1 years) from a region characterized by high ca...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：2000-01-01 00:00:00
abstract：:Metabolic acidosis could occur due to either endogenous acids accumulation or bicarbonate loss from the gastrointestinal tract or commonly from the kidney. This study aimed to investigate the possible underlying mechanism(s) of chronic acidosis-induced cardiac contractile and electrical changes in rats. Twenty four ad...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.933171
更新日期：2016-12-13 00:00:00
abstract：:The paper presents an example of a new type of a structured model containing time delays in parallel branches. This model was selected as optimal to describe mathematically the lymphocyte migration between the venous blood and prescapular lymph in Merino ewes under physiological conditions. The model allowed to identi...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：1999-01-01 00:00:00
abstract：:Glucose tolerance, insulin binding to erythrocytes, insulinaemia, plasma total cholesterol, plasma triglycerides, weight of fat pads, food consumption and body weight changes were studied in genetically hypertensive lean Koletsky rats. Long-term treatment with dopaminergic agonist terguride (0.2 mg/kg/day) normalized ...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：1997-01-01 00:00:00
abstract：:Pregnant rats were exposed to intermittent hypobaric hypoxia (at a simulated altitude of 7000 m or 5000 m) and the excitability of cortical neurons of their pups was tested. Stimulation of the sensorimotor cortex of rats prenatally exposed to hypoxia shortened the duration of cortical afterdischarges in 12-day-old rat...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：2001-01-01 00:00:00
abstract：:Transgenic mice overexpressing a transthyretin promoter-ANF structural fusion gene have a life-long reduction in arterial blood pressure compared to nontransgenic littermates. The present study was designed to test the hypothesis that the high plasma level of ANF in the transgenic mice inhibits the renin-angiotensin a...
journal_title：Physiological research
pub_type： 杂志文章
doi：
更新日期：1994-01-01 00:00:00
abstract：:The left and right ventricle originate from distinct parts of the cardiac tube, and several genes are known to be differentially expressed in these compartments. The aims of this study were to determine developmental differences in gene expression between the left and right ventricle, and to assess the effect of alter...
journal_title：Physiological research
pub_type： 杂志文章
doi：10.33549/physiolres.932379
更新日期：2012-01-01 00:00:00
