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Appearance and distribution of dendritic cells and macrophages in dental pulp during early postnatal morphogenesis of mouse mandibular first molars.

Dendritic cells and macrophages were examined in dental pulp during the postnatal development of mouse mandibular first molars, by immuno- and enzyme histochemistry. F4/80 antibody against dendritic cells and macrophages demonstrated labeled cells predominantly in and around the odontoblastic layer during tooth development from postnatal day 0 (PN0) to PN5. Labeling with Mac-1, Mac-2, and MOMA-2 antibodies against macrophages showed varied distribution patterns. Mac-1-positive cells were not detected in the dental pulp. Mac-2-positive cells appeared in the dental pulp at PN0, but not in or aro

Metabolic resistance to pyrethroids with possible involvement of non-coding ribonucleic acids in Anopheles funestus, the major malaria vector in western Kenya.

BACKGROUND: The resurgence of Anopheles funestus, a dominant vector of human malaria in western Kenya was partly attributed to insecticide r … 4%), glutathione S-transferases (3%), UDP-glycosyltransferases (2%), ATP-binding cassettes (2%) and carboxylesterases (1%). CONCLUSION: This study unveils the molecular basis of insecticide resistance in An. funestus in western Kenya, highlighting for the first time the potential role of non-coding RNAs alongside metabolic detoxification in pyrethroid resistance. …

Lysophospholipase from the human blood fluke, Schistosoma japonicum.

BACKGROUND: Given the unusual nature of the schistosome surface (a highly unusual lipid bi-layer) and the central role of the schistosome te … A of Pseudomonas fluorescens, appeared to belong to the abhydrolase_2 family of phospholipases and carboxylesterases, and was structurally related to the alpha/beta-hydrolases (pfam00561). The S. japonicum enzyme exhibited the GXSXG consensus active site characteristic of serine proteases, esterases, and lipases, and included the catalytic triad motif of Ser-Asp- …

Biotransformation enzyme activities and phase I metabolites analysis in Litopenaeus vannamei following intramuscular administration of T-2 toxin.

T-2 toxin (T-2) is a type-A trichothecene produced by Fusarium that causes toxicity to animals. T-2 contamination of grain-based aquatic feed is a concern for the industries related to edible aquatic crustacean species such as the shrimp industry because it can lead to serious food safety issues. T-2, its metabolites, and selected phase I (EROD, CarE) and phase II (GST, UGT, SULT) detoxification enzymes in hemolymph and tissues were monitored at 0, 5, 10 15, 30, 45, and 60 min following T-2 intramuscular administration (3 mg/kg bw) in shrimp (Litopenaeus vannamei). Marked increases of EROD act

In Vitro Degradation of Chlorpyrifos by the Ruminal Microbes: Insights from the Rumen Metagenome.

In vitro studies were conducted in a series to investigate if the ruminal microbes are capable of degrading chlorpyrifos. This in vitro stud … ified, which demonstrated that degradation of chlorpyrifos was carried out by the affiliated enzyme carboxylesterase. The presence of GO:0004035, GO:0004364, GO:0019637, GO:0016791, and GO:0042178 in the metagenome strengthens that the chlorpyrifos degradation in the present study was primarily assigned to the rumen microbiota. This in vitro study provided insight …

Effect of hyperlipidemic diets, proinflammatory agents and plasma expanders on leukocyte adhesion to the endothelium of aorta and carotid artery of rats.

A comparative study of leukocyte adhesion to the endothelium of the thoracic aorta and left carotid artery in rats has been performed after administration of two hyperlipidemic diets for 15 days, proinflammatory agents (thrombin, lipopolysaccharide and zymosan activated serum) and plasma expanders [dextran, polyvinylpyrrolidone (PVP), rat albumin and several bovine albumins from different sources]. Leukocytes adhered to the endothelium were demonstrated in surface preparations by esterase activity. Activation of circulating leukocytes was measured by nitroblue tetrazolium reduction and luminol

Carboxyl ester lipase is highly conserved in utilizing maternal supplied lipids during early development of zebrafish and human.

Carboxyl ester lipase (Cel), is a lipolytic enzyme secreted by the pancreas, which hydrolyzes various species of lipids in the gut. Cel is also secreted by mammary gland during lactation and exists in breast milk. It facilitates dietary fat digestion and absorption, thus contributing to normal infant development. This study aimed to examine whether the Cel in zebrafish embryos has a similar role of maternal lipid utilization as in human infants, and how Cel contributes to the utilization of yolk lipids in zebrafish. The cel1 and cel2 genes were expressed ubiquitously in the blastodisc and yolk

The effect of sodium fluoride preservative and storage temperature on the stability of cocaine in horse blood, sheep vitreous and deer muscle.

The in vitro stability of cocaine in horse blood, sheep vitreous humour (VH) and homogenised deer muscle is described. The stability of coca … od appeared to be less than that reported for human blood, probably attributable to the presence of carboxylesterase in horse plasma. Cocaine stored in VH at -18°C was essentially stable for the study period whereas at 4°C concentrations decreased by >50% in preserved and unpreserved VH stored for longer than 14 days. Fluoride did not significantly affect cocaine …

Drug interactions involving aspirin (acetylsalicylic acid) and salicylic acid.

Aspirin (acetylsalicylic acid) is metabolically converted to salicyclic acid by the action of carboxylesterases. Although metabolic drug interactions involving aspirin are theoretically possible, there appear to have been no studies to date which have shown conclusively that aspirin hydrolysis is altered by coadministered drugs. However, a number of treatments are known to affect the rate or extent of aspirin absorption, including activated charcoal, antacids, cholestyramine and metoclopramide. Caffeine and metoprolol have been reported to increase peak salicylic acid concentration following a…

A symbiotic gut bacterium enhances Aedes albopictus resistance to insecticide.

BACKGROUND: The increasing insecticide resistance of Aedes albopictus puts many countries in Asia and Africa, including China, at great risk … rees. Meanwhile, the activity of extracellular enzymes released by S. oryzae was measured, but only carboxylesterase activity was detected. HPLC and UHPLC were respectively used to measure deltamethrin residue concentration and metabolite qualitative analysis, showing that the deltamethrin degradation efficiency of S. oryzae was positively correlated with time and …

Influence of CYP450 Enzymes, CES1, PON1, ABCB1, and P2RY12 Polymorphisms on Clopidogrel Response in Patients Subjected to a Percutaneous Neurointervention.

PURPOSE: Clopidogrel is a thienopyridine prodrug that inhibits platelet aggregation. It is prescribed to prevent atherothrombotic and thromb … ding the clopidogrel-metabolizing enzymes (CYP2C19, CYP1A2, CYP2B6, CYP2C9, CYP2C9, CYP3A4, CYP3A5, carboxylesterase-1 [CES1], and paraoxonase-1 [PON1]), P-glycoprotein transporter (ABCB1), and platelet receptor P2Y12. Polymorphisms were analyzed by quantitative real-time polymerase chain reaction and matrix-assisted laser desorption/ionization-time-of-flight mass …

Macrophage-like cell line (HS-P) from a rat histiocytic sarcoma.

With future exploration of macrophage properties in mind, we established a novel cell line (HS-P) from a transplantable histiocytic sarcoma, derived originally from a tumour in an aged F344 rat. HS-P was subjected to 70 serial passages, in which the mean doubling time was 15.7 h. The cells, which were round, oval or polygonal in shape, were arranged in a compact sheet. They reacted to varying degrees for lysosomal enzymes (acid phosphatase and non-specific esterase) and with the following antibodies: ED1/ED2 (rat macrophage/histiocyte-specific), OX6 (rat MHC class II-specific), lysozyme antibo

Monitoring Aedes populations for arboviruses, Wolbachia, insecticide resistance and its mechanisms in various agroecosystems in Benin.

Aedes mosquitoes are the main vectors of arboviruses in Benin. Cases of dengue have been reported in Benin with all four serotypes of the vi … 9P) and the expression levels of eight detoxification genes (P450s from the CYP9 and CYP6 families, carboxylesterases and glutathione-S-transferases). Aedes aegypti (Ae. aegypti) mosquitoes were the most abundant (93.9%) in the three agroecosystems studied, followed by Aedes albopictus (Ae. albopictus) mosquitoes (6.1%). No arboviruses were detected in the study's …

The hepatic expression status of hepatocyte nuclear factor 4α in subclinical and clinical ketotic dairy cows and its impact on lipid metabolism in hepatocytes.

Due to sustained lipolysis, excessive nonesterified fatty acid (NEFA) concentrations are a common pathological factor of ketosis in peripart … hepatic steatosis and liver dysfunction. The protein abundance of HNF4α and its downstream targets carboxylesterase 1 (CES1) and CES2 as well as the mRNA abundance of CES1 and CES2 were upregulated in the liver of cows with SCK, but downregulated in CK cows. A dose of 1.2 mM NEFA decreased protein abundance of HNF4α, CES1, and CES2, and induced lipid accumulation …

Assessment of monocytic component in acute myelomonocytic and monocytic/monoblastic leukemias by a chemiluminescent assay.

INTRODUCTION: Classically, the monocytic component of acute myelomonocytic (FAB-M4) and acute monocytic/monoblastic (FAB-M5) leukemias is demonstrated by nonspecific esterase positivity in cytochemical stainings. We have previously demonstrated that non-specific esterases from normal monocytes can be determined by a chemiluminescent method. In the present study, we investigated whether this assay can also determine the monocytic component of FAB-M4 and FAB-M5 and distinguish these acute myeloid leukemia (AML) categories. MATERIALS AND METHODS: Bone marrow samples were obtained from 66 patient

Organophosphates and their impact on the global environment.

Serious intoxications and incidences due to misuse of organophosphorus insecticides (OP) have been reported for over three decades. In this … d biomarker of OP-poisoning. Beta-glucuronidase (beta-G) is loosely bound to egasyn which is one of carboxylesterase isozymes in the liver microsomes. The oxon formed from OP in the liver microsomes is covalently bound to egasyn and causes the cleavage of the egasyn-glucuronidase complex, leading to the release of beta-G into the blood. In fact, plasma beta-G acti …

Polybasic nanogels for intracellular co-delivery of paclitaxel and carboplatin: a novel approach to ovarian cancer therapy.

Ovarian cancer is one of the leading causes of cancer-related deaths in women, with limited progress in treatments despite decades of research. Common treatment protocols rely on surgical removal of tumors and chemotherapy drugs, such as paclitaxel and carboplatin, which are capable of reaching cancer cells throughout the body. However, the effectiveness of these drugs is often limited due to toxic reactions in patients, nonspecific drug distribution affecting healthy cells, and the development of treatment resistance. In this study, we introduce a polybasic nanogel system composed of poly(die

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… Nanoparticle degradation and release by carboxylesterases Carboxylesterase-triggered hydrolysis of the nanoparticle crosslinking agent was explored as a function of three ester containing crosslinkers (PCL-DMA, PLA-PEG-DMA m = 2 and m = 5) ( Fig. 1 ). … Degradation occurred in the presence of either glutathione or human carboxylesterase 2 (CES2) at a relevant intracellular conditions. …

Prodrugs in Oncology: Bioactivation and Impact on Therapeutic Efficacy and Toxicity.

A prodrug is a molecule that lacks pharmacological activity, but upon enzymatic bioactivation, it can generate a therapeutically active molecule. The primary reason behind the design of a prodrug is to help circumvent challenges associated with the physicochemical properties of a drug molecule, such as solubility, absorption, distribution, and instability. Chemotherapy has been at the forefront of cancer treatment for over 70 years due to its ability to target rapidly proliferating tumor cells. However, a major concern with conventional chemotherapy is the lack of selectivity and its associate

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… phosphorylase, thymidine phosphorylase, and thymidine kinase | Angina, myocardial infarction, heart failure, encephalopathy, seizures, coma, and peripheral nerve damage [ 127 , 128 , 129 ] Irinotecan | Metastatic colorectal cancers, ovarian cancer, and small-cell lung cancer [ 130 , 131 , 132 , 133 ] | Carboxylesterases … As depicted in Figure 7 , irinotecan undergoes cleavage of the ester bond at the C10 position mediated by carboxylesterase (CE) to release the pharmacologically active SN-38 [ 174 , 175 ]. …

Examining the potentials of stem cell therapy in reducing the burden of selected non-communicable diseases in Africa.

Stem cell therapy (SCT) is a promising solution for addressing health challenges in Africa, particularly non-communicable diseases (NCDs). With their regenerative potential, stem cells have the inherent capacity to differentiate into numerous cell types for tissue repair. Despite infrastructural, ethical, and legal challenges, SCT holds immense promise for managing chronic illnesses and deep-seated tissue injuries. The rising prevalence of NCDs in Africa highlights the need for innovative strategies and treatment options. SCT offers hope in combating conditions like burns, osteoarthritis, diab

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… Allogeneic Neural Stem Cells and Irinotecan Hydrochloride in Treating Patients With Recurrent High-Grade Gliomas Active Biological: Carboxylesterase-expressing Allogeneic Neural Stem Cells Drug: Irinotecan Drug: Irinotecan Hydrochloride Other: Laboratory Biomarker Analysis Other: Pharmacological Study … Allogeneic Neural Stem Cells and Irinotecan Hydrochloride in Treating Patients With Recurrent High-Grade Gliomas | Active | Biological: Carboxylesterase-expressing Allogeneic Neural Stem Cells Drug: Irinotecan Drug: Irinotecan Hydrochloride Other: Laboratory Biomarker Analysis Other: Pharmacological …

Nanomedicine developments in the treatment of metastatic pancreatic cancer: focus on nanoliposomal irinotecan.

Nanoliposomal irinotecan (nal-IRI) was originally developed using an efficient and high-loading capacity system to encapsulate irinotecan within a liposomal carrier, producing a therapeutic agent with improved biodistribution and pharmacokinetic characteristics compared to free drug. Specifically, administration of nal-IRI results in prolonged exposure of SN-38, the active metabolite of irinotecan, within tumors, while at the same time offering the advantage of less systemic toxicity than traditional irinotecan. These favorable properties of nal-IRI, confirmed in a variety of tumor xenograft m

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… Specifically, the liposomal carrier system offers a way to protect irinotecan from premature conversion by nonspecific carboxylesterases into its active metabolite, SN-38, which is about 100- to 1,000-fold more potent. 31 This produces lower maximum plasma concentration ( C max ) and consequently reduced … Ultimately, using model sensitivity analyses, these investigators determined that tumor SN-38 duration – reflecting both drug deposition and local activation of irinotecan by carboxylesterases to its active metabolite – represents the key driver of in vivo sensitivity to irinotecan-based treatment. …