Excretion metabolism caco 2 cells. Medical search. Frequent questions

Experimental data on absorption, distribution, metabolism and excretion (ADME) are not available for these components of 1,4-CHDM DGE. (europa.eu)
Pharmacokinetic parameters estimatedincludedthe partition coefficient (logKow),volume of distribution (Vd), absorption rate (ka), permeability in human jejunum, Caco-2 cell permeability, percent bioavailability (F%), and dermal permeability constant (Kp). (europa.eu)
The corresponding predicted absorption half-lives (t 1/2 ) are about 11 minutes for all three major components. (europa.eu)
The most common in vitro model for absorption, distribution, metabolism, and excretion (ADME) purposes is currently the Caco-2 cell line. (bvsalud.org)
However, clear differences in gene and protein expression towards the small intestine and an, at best, fair prediction accuracy of intestinal drug absorption restrict the usefulness of a model for intestinal epithelial cells. (bvsalud.org)
To overcome these limitations, we evaluated a panel of low-passaged patient-derived colorectal cancer cell lines of the HROC collection concerning similarities to small intestinal epithelial cells and their potential to predict intestinal drug absorption. (bvsalud.org)
In this study, we investigated the metabolic stability, metabolite production, metabolic pathways and plasma protein binding (PPB) of FHND6081 along with its absorption, tissue distribution, excretion (ADME) and pharmacokinetics (PK) in animals. (scienceopen.com)
Here, we discuss some aspects of metabolism and absorption of phenolic compounds. (docksci.com)
ABSORPTION AND METABOLISM OF POLYPHENOLIC COMPOUNDS The concentrations of polyphenolic compounds in the bloodstream depend on their modiﬁcations during metabolism and absorption form the gastrointestinal tract. (docksci.com)
This suggests that at this stage the nanoparticles' absorption process is residual compared with the following steps in metabolism, distribution and/or excretion processes, indicated by the increase of iron accumulation proteins at both transcriptional and translational level. (uea.ac.uk)
Lönnerdal B, Georgieff MK, Hernell O. Developmental Physiology of Iron Absorption, Homeostasis, and Metabolism in the Healthy Term Infant. (ucdavis.edu)
High lipophilicity often leads to high rate of metabolism, poor solubility, high turn-over, and low absorption. (themama.ai)
P-glycoprotein (Pgp) is an ABC transporter protein involved in intestinal absorption, drug metabolism, and brain penetration, and its inhibition can seriously alter a drug's bioavailability and safety. (themama.ai)
This includes absorption, storage and excretion processes at the level of gastrointestinal tract, bone, and kidney, which are strictly controlled by a number of known and as yet unknown regulators, transporters and endocrine and paracrine signals. (biomedcentral.com)
Furthermore, absorption, distribution, metabolism and excretion (ADME) drug-likeness analysis was done using the Swiss online ADME web tool. (springeropen.com)
Soy protein peptic hydrolysate with bound phospholipids decreases micellar solubility and cholesterol absorption in rats and caco-2 cells. (cmdm.tw)

The Caco-2 cell permeability values of the three components (A-C) are estimated to be from 1.38 x 10 -4 to2.27 x 10 -4 ( Table 1, see attached table 1 ). (europa.eu)
In Caco-2 cell experiments, the compound displayed modest permeability suggesting that it may show limited bioavailability via oral routes. (scienceopen.com)
Furthermore, permeability was found to be highly temperature-dependent in Chinese hamster ovary (CHO) control cells and artificial membranes (parallel artificial membrane permeability assay). (aspetjournals.org)
Mechanisms of toxicity include inhibition of enzyme activity and protein synthesis, alterations in nucleic acid function, and changes in cell membrane permeability. (medscape.com)

Herein we investigated whether lupin proteins compared to casein modulate sterol excretion and mRNA expression of intestinal sterol transporters by use of pigs as an animal model with similar lipid metabolism as humans, and cellular cholesterol-uptake by Caco-2 cells. (biomedcentral.com)
Cholesterol-uptake studies were performed with Caco-2 cells that were incubated with lupin conglutin γ, phytate, ezetimibe or albumin in the presence of labelled [4- 14 C]-cholesterol. (biomedcentral.com)
The NBD cholesterol uptake in Caco-2 cells was determined using fluorometric assay. (biomedcentral.com)
Another study suggests C3R could inhibit the glucose uptake in Caco-2 cells [ 19 ]. (biomedcentral.com)
The uptake of [ 3 H]vinblastine, a substrate of P-gp, by Caco-2 cells was measured. (aspetjournals.org)
No significant effect on the uptake of 3- O -[ 3 H]methylglucose or [ 14 C]phenylalanine by Caco-2 cells was found, compared with the control. (aspetjournals.org)
The ethyl acetate extract of orange juice and these methoxyflavones also increased steady-state [ 3 H]vinblastine uptake by LLC-GA5-COL300 cells (a cell line transfected with human MDR1 cDNA). (aspetjournals.org)
This two-compartmental model was parameterized to account for nonspecific binding, bidirectional passive diffusion, and active uptake processes based on the physiology of the cells. (aspetjournals.org)
In the liver, the interplay between uptake and export processes influences the drug intracellular concentration and thereby the amount of drug available for metabolic elimination and/or biliary excretion. (aspetjournals.org)
The effects of hepatic uptake and efflux transporters on metabolism of digoxin were examined in isolated rat hepatocytes versus microsomes. (aspetjournals.org)
Rifampin (an organic anion-transporting peptide 2 inhibitor) or GG918 [GF120918 ( N -(4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]-phenyl)-9,10-dihydro-5-methoxy-9-oxo-4-acridine carboxamide)] (a potent P-glycoprotein inhibitor) were used to estimate effects of uptake or efflux transporters on digoxin metabolism. (aspetjournals.org)
These results strongly suggest that the hepatic uptake and efflux transporters that are found in hepatocytes, but not in microsomes, modulate intracellular concentration of digoxin and thus affect metabolism. (aspetjournals.org)
12 This reaction both increases cellular retention of pralatrexate for extended drug action and impedes the uptake of folate, also a substrate of FPGS, to further inhibit folate metabolism in cancer cells. (drugbank.com)

The use of an increased MRT to explain increased extents of metabolism upon increased apical excretion is not tenable in these organs or "open systems" since the MRT of drug in the cell is reduced with irreversible loss from biliary excretion or hastened gastrointestinal transit of the secreted drug in the lumen. (nih.gov)

Additional processes, such as nonspecific binding and bidirectional passive diffusion between medium and cells need to be assessed separately from active transport to enable proper mechanistic scaling. (aspetjournals.org)
We applied a recently developed in vitro-in vivo extrapolation method, including hepatic metabolism and transport processes, herein referred to as the Extended Clearance Concept Classification System (ECCCS). (degruyter.com)
Sufficient dietary supply of calcium (Ca) and phosphorus (P) is essential for all vertebrates to ensure various biological processes including bone formation, blood clotting, cell proliferation and energy metabolism. (biomedcentral.com)
The various processes that occur during the cycling of water are illustrated in Figure 2 below. (uwf.edu)

The human colon epithelial cancer cell line, Caco-2, is used as an in vitro model to simulate the human intestinal tissue. (themama.ai)

Conversely, drugs, or compounds that inhibit this enzyme can reduce the normal metabolism of another drug, causing elevated levels and potential toxic side effects The inhibitory effect on CYP3A4 is generally measured by the biotransformation and hydroxylation of the drug Midazolam. (iwerliewen.org)
13 As well, the study dose far exceeded the target dose for patients with peripheral T-cell lymphoma and pralatrexate does not inhibit the human ether-a-go-go-related gene (hERG) K + channel 13 . (drugbank.com)

Suspension or plated cultures of primary hepatocytes or hepatocyte-like cell lines (HepG2, HepaRG) can be used to study and quantify metabolism of chemicals. (wikipedia.org)
In this work, the in vitro toxicity of the nanoparticles was evaluated in five cellular models (Caco-2, HepG2, MDCK, Calu-3 and Raw 264.7) representing different target organs/systems (gastrointestinal system, liver, kidney, respiratory system and immune system). (uea.ac.uk)

Finally, C3R (100 μM) was able to suppress mRNA expression of NPC1L1 in Caco-2 cells after 24 h incubation. (biomedcentral.com)
Expression of sterol regulatory element-binding protein 1c (SREBP-1c) mRNA in rat hepatoma cells requires endogenous LXR ligands. (cmdm.tw)

All lines expressed multiple transporter molecules, with the expression levels in three lines being close to those of small intestinal epithelial cells. (bvsalud.org)
Compared with the Caco-2 model, three HROC lines demonstrated both higher similarity to jejunal epithelial tissue cells and higher regulatory potential of relevant drug transporters. (bvsalud.org)
Jiang R, Lonnerdal B. Transcriptomic profiling of intestinal epithelial cells in response to human, bovine and commercial bovine lactoferrins. (ucdavis.edu)

Controversy existed on the explanation underlying the interplay between transporters and enzymes in the Caco-2 cell monolayer or cell culture systems, but less so on eliminating organs such as the intestine and liver. (nih.gov)
The general conclusion is that a reciprocal relationship exists between the clearances related to enzymes and apical transporters due to their competition for the substrate within the cell, and is a relationship independent of the MRT of drug in the system. (nih.gov)

It may be argued whether the observed alterations in liver lipid metabolism can be attributed to intact lupin polypeptides that enter the organism. (biomedcentral.com)
Reduction of total cholesterols (TC) and LDL-C by dietary alterations and medications that affect lipid metabolism [ 14 ] is found to reduce the occurrence of atherosclerosis in animals and clinical cardiovascular events in human [ 15 ]. (hindawi.com)

Overview of metabolism and bioavailability enhancement of polyphenols. (docksci.com)

We found that memory CD8+ T cells deployed a range of adaptations to tissue residency, including reliance on non-steroidal products of the mevalonate-cholesterol pathway, such as coenzyme Q, driven by increased activity of the transcription factor SREBP2. (bvsalud.org)
Whether isolated lupin proteins themselves could contribute to the increased cholesterol excretion has not been demonstrated yet, though there is evidence suggesting that proteins cause these kind of effects. (biomedcentral.com)
In that study soybean proteins revealed a specific impact on cholesterol output, whilst the excretion of bile acids was not influenced in response to soybean proteins. (biomedcentral.com)
des 1 and 8 upregulate cholesterol excretion through LXR-mediated ABCG5 and ABCG8 levels.Figure three. (namptinhibitor.com)
A) The relative TICE IKK-β Inhibitor site amount in peptide 1 or 8-treated Caco-2 cells by means of cholesterol assay. (namptinhibitor.com)
B) The protein expression TICE amount in peptide 1 or 8-treated Caco-2 cells by way of cholesterol assay. (namptinhibitor.com)
E) Utilizing cholesterol assay, the relative TICE amount in GSK2033 (1 ) and peptide 1 or 8-treated Caco-2 cells. (namptinhibitor.com)
hepatobiliary cholesterol transport can also be essential for cholesterol excretion to feces and hypolipidemic technique [35]. (namptinhibitor.com)
Cholesterol is associated with abnormalities such as Trypanosomiasis, Chagas Disease, Cleft Palate, Chondrodysplasia punctata 2, X-linked dominant and Child syndrome. (cmdm.tw)
Stimulation of fecal steroid excretion after infusion of recombinant proapolipoprotein A-I. Potential reverse cholesterol transport in humans. (cmdm.tw)
Although the clinical manifestations are unclear, vitamin C is a cofactor in the metabolism of tyrosine and cholesterol and the synthesis of carnitine, neurotransmitters (eg, norepinephrine), peptide hormones, corticosteroids, and aldosterone. (medscape.com)

We hold the opposite view and assert that increased secretion should evoke a decrease in metabolism due to the competition between the enzyme and apical efflux transporter for the drug within the cell. (nih.gov)
Use of transporter knockdown Caco-2 cells to investigate the in vitro efflux of statin drugs. (degruyter.com)

Fecal steroid excretion is increased in rats by oral administration of gymnemic acids contained in Gymnema sylvestre leaves. (cmdm.tw)

Intestine-derived secretary factors regulate bile acid metabolism within the liver. (namptinhibitor.com)
To validate regulation of FGF19 through peptide for the metabolic pathway of bile acid in liver, conditioned media (CM) from the peptide-treated Caco-2 cells was added to MIHA cells. (namptinhibitor.com)

In addition, we monitored the bio-distribution and excretion pathway of GNS@CaCO 3 /ICG based on the NIR fluorescence from ICG and two-photon fluorescence and photoacoustic signal from GNSs, and the results proved that GNS@CaCO 3 /ICG had a great ability for tumor-specific and tumor-triggered drug release. (thno.org)
Toxic effects depend on the amount of metal ingested, entry rate, tissue distribution, concentration achieved, and excretion rate. (medscape.com)

Pralatrexate is a folate analog metabolic inhibitor that competitively inhibits dihydrofolate reductase (DHFR) selectively in cancer cells overexpressing the reduced folate carrier protein-1 (RFC-1). (drugbank.com)

The Hp 2-2 polymers are less efficient inhibitors of hemoglobin-driven oxidative stress, leading to ascorbic acid depletion. (medscape.com)

To validate the impact of FGF19 on CYP7A1 and CYP8B1 levels in the liver, CM from FGF19 siRNA-treated was added to Caco-2 cells (Figure 4E). (namptinhibitor.com)
The liver is a major site of metabolism of many endogenous compounds and xenobiotics since hepatocytes (which comprise 80% of the liver cells) contain large amounts of smooth endoplasmic reticulum, where many metabolizing enzymes reside. (aspetjournals.org)
Liver microsome incubations are routinely carried out to survey the metabolism of potential drugs by pharmaceutical companies. (aspetjournals.org)
It is responsible for the metabolism of more than half of ingested drugs, including artemisinin and its derivatives Svensson US, Mäki-Jouppila M, Hoffmann KJ, Ashton M. Characterisation of the human liver in vitro metabolic pattern of artemisinin and auto-induction in the rat by use of nonlinear mixed effects modelling. (iwerliewen.org)

Whereas both inhibitors exerted minimal effects on metabolism in microsomes, rifampin and GG918 significantly decreased and increased digoxin metabolism in hepatocytes, respectively. (aspetjournals.org)

The conclusion is that the f(met) is the more appropriate index to reflect the extent of metabolism in transporter-enzyme interplay, since the parameter captures drug metabolism in the cell when its contents in the apical, cell, and basolateral compartments or the entire dose is considered to be available for metabolism. (nih.gov)
This parameter for metabolism (f(met)) bears a reciprocal relationship to the secretory intrinsic clearance and is in concordance with the notion that both the enzyme and apical transporter compete for the cellular substrate within. (nih.gov)

As cancer cells are rapidly replicating, they require a lot of folates to accommodate an accelerated cell division and DNA and protein modification for cellular transformation. (drugbank.com)

8. Antony J. Debroy S. Manisha C. Thomas P. Jeyarani V. Choephel T. In-vitro cell line Models and Assay methods to study the Anti-diabetic Activity. (rjptonline.org)

Bailey SJ, Winyard P, Vanhatalo A, Blackwell JR, Dimenna FJ, Wilkerson DP, Tarr J, Benjamin N, Jones AM (2009) Dietary nitrate supplementation reduces the O 2 cost of low-intensity exercise and enhances tolerance to high-intensity exercise in humans. (springer.com)

In vitro (meaning in glass, or in the glass) studies are performed with microorganisms, cells, or biological molecules outside their normal biological context. (wikipedia.org)
often not italicized in English usage) studies are conducted using components of an organism that have been isolated from their usual biological surroundings, such as microorganisms, cells, or biological molecules. (wikipedia.org)

We therefore conclude that the GNS@CaCO 3 /ICG holds great promise for clinical applications in anti-tumor therapy with tumor imaging or drug tracing. (thno.org)

Protein purification involves the isolation of a specific protein of interest from a complex mixture of proteins, often obtained from homogenized cells or tissues. (wikipedia.org)
B) The protein expression of ABCG5/8 in peptide 1 or 8-treated Caco-2 cells. (namptinhibitor.com)
These glycoproteins include the CD98 heavy chain protein of Mus musculus (gbU25708) and the orthologous 4F2 cell surface antigen heavy chain of Homo sapiens (spP08195). (tcdb.org)
10 Pralatrexate is designed to have a higher affinity for the reduced folate carrier, a protein that is overexpressed in malignant cells and is upregulated by oncogenes. (drugbank.com)
One study identified a genetic polymorphism of the human plasma protein haptoglobin, Hp 2, that may be an important non-nutritional modifying factor in the pathogenesis of vitamin C deficiency. (medscape.com)

The results of in vitro antidiabetic study against α-glucosidase indicated that compound 5o bearing 2-CH 3 -5-NO 2 substituent on phenyl ring was found to be the most active compound against both enzymes. (biomedcentral.com)
The electron donating (CH 3 ) group and electron withdrawing (NO 2 ) group on a phenyl ring highly favoured the inhibitory activity against these enzymes. (biomedcentral.com)

For example, microorganisms or cells can be studied in artificial culture media, and proteins can be examined in solutions. (wikipedia.org)
CONCLUSIONS: High levels of immune cells and immune checkpoint proteins have a significant impact on patient survival in SBA. (bvsalud.org)
Some animal proteins, for example, those in the LAT family (TC# 2.A.3.8) including ASUR4 (gbY12716) and SPRM1 (gbL25068) associate with a type 1 transmembrane glycoprotein that is essential for insertion or activity of the permease and forms a disulfide bridge with it. (tcdb.org)

In silico analysis, therefore, was performed to identify small drug-like molecules as potential inhibitors of transforming growth factor beta-2 receptor (TGFβRII). (brjnmims.org)
The CYP P450 genes are involved in the formation and breakdown (metabolism) of various molecules and chemicals within cells. (themama.ai)

1] The enzyme, L-gluconolactone oxidase, which would usually catalyze the conversion of L-gluconogammalactone to L-ascorbic acid, is defective due to a mutation or inborn error in carbohydrate metabolism. (medscape.com)

Pralatrexate is a folate analog that inhibits folate metabolism, thus impeding the synthesis of amino acids and nucleic acid. (drugbank.com)

Thus, an improved understanding of the metabolic strategies that enable tissue residency by T cells could inform new approaches to empower immune responses in tissues and solid tumours. (bvsalud.org)
Here, to systematically define the basis for the metabolic reprogramming supporting TRM cell differentiation, survival and function, we leveraged in vivo functional genomics, untargeted metabolomics and transcriptomics of virus-specific memory CD8+ T cell populations. (bvsalud.org)

Recombinant production of growth factors for application in cell culture. (au.dk)

Cumulative clinical evidence shows alterations in the ubiquitylation of cell-cycle regulators in the aetiology of many human malignancies. (scienceopen.com)

6. Camenisch G, Umehara K. Predicting human hepatic clearance from in vitro drug metabolism and transport data: a scientific and pharmaceutical perspective for assessing drug-drug interactions. (degruyter.com)
In this model, human tumor cells (patient derived tumors (PDX) or tumor cell lines) are transplanted, either under the skin (xenograft) or directly into the organ (orthotopic) in which the tumor originated or associated, into immunocompromised (nude or SCID) mice that do not reject human cells. (atdrik.com)
[2] Tobacco, areca nut, alcohol, and high-risk oncogenic human papillomavirus 16/18 constitute major risk factors to oral cancer. (brjnmims.org)
The experimental result on the rate of drug passing through the Caco-2 cells can approximate the rate at which the drug permeates through the human intestinal tissue. (themama.ai)
In a pionneering study in 2010, the University of Louvain had studied the anti-inflammatory effect and modulation of cytochrome P450 activities by Artemisia annua tea infusions in human intestinal Caco-2 cells Melillo de Magalhães, Yves-Jacques Schneider. (iwerliewen.org)
Anti-inflammatory effect and modulation of cytochrome P450 activities by Artemisia annua tea infusions in human intestinal Caco-2 cell Food Chemistry 134(2):864-71 · September 2012 These assays were done on aqueous infusionsof Artemisia annua samples from 7 different origins. (iwerliewen.org)
The human body is about 60 percent water, and human cells are more than 70 percent water. (uwf.edu)

Meanwhile, the distinct pH-triggered drug release performance of GNS@CaCO 3 /ICG implemented the tumor-targeted NIR fluorescence imaging. (thno.org)

Disturbances in Ca and P homeostasis in chickens are associated with a decline in growth and egg laying performance and environmental burden due to excessive P excretion rates. (biomedcentral.com)
In vertebrates, mechanisms of P homeostasis are largely conserved and closely linked to Ca metabolism. (biomedcentral.com)

Viruses, which only replicate in living cells, are studied in the laboratory in cell or tissue culture, and many animal virologists refer to such work as being in vitro to distinguish it from in vivo work in whole animals. (wikipedia.org)
The application of GNS@CaCO 3 /ICG for in vitro and in vivo therapy achieved the combined antitumor effects upon the NIR irradiation, which was superior to the single PDT or PTT. (thno.org)

H 2 administration with different methods has been proved definitely potentials to prevent serious intestinal diseases. (biomedcentral.com)

PDT uses photosensitizers exposed to a laser tuned to a specific wavelength to produce highly reactive oxygen species, especially singlet oxygen ( 1 O 2 ), finally leading to the death of malignant cells [ 6 - 8 ], while photothermal therapy causes hyperthemia in tissues when absorbing energy from a laser [ 9 - 10 ]. (thno.org)

Abacavir may decrease the excretion rate of Procainamide which could result in a higher serum level. (drugbank.com)

The sulphonamide moiety (-SO 2 NH 2 ) is an effective pharmacophore revealing the clinical and medicinal importance of sulphonamide drugs in the field of drug discovery [ 11 ]. (biomedcentral.com)
The ECCCS represents a powerful tool to anticipate the DDI potential of victim drugs based on in vitro drug metabolism and transport data. (degruyter.com)
The authors wish to acknowledge the many Novartis Drug Metabolism and Pharmacokinetic scientists of Basel, Switzerland, who have supported this work. (degruyter.com)
2. Pandey S. Srivastava V. An Overview on Invasomes: Novel Vesicular Carrier for Transdermal Drug Delivery. (rjptonline.org)

Anatomy28

Organisms17

Diseases19

Chemicals and Drugs95

Analytical, Diagnostic and Therapeutic Techniques and Equipment32

Psychiatry and Psychology1

Phenomena and Processes70

Technology, Industry, Agriculture4

Information Science3

Health Care5

Geographicals2

Absorption16

Permeability4

Uptake13

Biliary excretion1

Processes4

Vitro model1

Inhibit2

HepG22

MRNA2

Epithelial3

Transporters2

Lipid metabolism2

Bioavailability1

Cholesterol11

Efflux2

Fecal1

Bile acid2

Distribution2

Inhibitor1

Oxidative1

Liver4

Hepatocytes1

Transporter2

Cellular1

Assay1

Humans1

Biological2

Conclude1

Protein5

Enzymes2

Proteins3

Molecules2

Enzyme1

Amino acids1

Metabolic2

Recombinant1

Alterations1

Human7

Tumor1

Homeostasis2

Vivo2

Methods1

Malignant cells1

Decrease1

Drug4