ResearchPad - Toxicology https://www.researchpad.co Default RSS Feed en-us © 2020 Newgen KnowledgeWorks <![CDATA[Small molecules that target the ubiquitin system]]> https://www.researchpad.co/product?articleinfo=N31a5939f-3624-42e8-a80d-c62cc785b62a

Eukaryotic life depends upon the interplay between vast networks of signaling pathways composed of upwards of 109–1010 proteins per cell. The integrity and normal operation of the cell requires that these proteins act in a precise spatial and temporal manner. The ubiquitin system is absolutely central to this process and perturbation of its function contributes directly to the onset and progression of a wide variety of diseases, including cancer, metabolic syndromes, neurodegenerative diseases, autoimmunity, inflammatory disorders, infectious diseases, and muscle dystrophies. Whilst the individual components and the overall architecture of the ubiquitin system have been delineated in some detail, how ubiquitination might be successfully targeted, or harnessed, to develop novel therapeutic approaches to the treatment of disease, currently remains relatively poorly understood. In this review, we will provide an overview of the current status of selected small molecule ubiquitin system inhibitors. We will further discuss the unique challenges of targeting this ubiquitous and highly complex machinery, and explore and highlight potential ways in which these challenges might be met.

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<![CDATA[Cytotoxicity of snake venom enzymatic toxins: phospholipase A2 and l-amino acid oxidase]]> https://www.researchpad.co/product?articleinfo=N1086ae34-0b6d-4362-83cd-31ea9ffc11ad

The phospholipase A2 (PLA2) and l-amino acid oxidase (LAAO) are two major enzymes found in the venoms from most snake species. These enzymes have been structurally and functionally characterised for their pharmacological activities. Both PLA2 and LAAO from different venoms demonstrate considerable cytotoxic effects on cancer cells via induction of apoptosis, cell cycle arrest and suppression of proliferation. These enzymes produce more pronounced cytotoxic effects in cancer cells than normal cells, thus they can be potential sources as chemotherapeutic agents. It is proposed that PLA2 and LAAO contribute to an elevated oxidative stress due to their catalytic actions, for instance, the ability of PLA2 to produce reactive oxygen species during lipolysis and formation of H2O2 from LAAO catalytic activity which consequently lead to cell death. Nonetheless, the cell-death signalling pathways associated with exposure to these enzymatic toxins are not fully elucidated yet. Here in this review, we will discuss the cytotoxic effects of PLA2 and LAAO in relationship to their catalytic mechanisms and the underlying mechanisms of cytotoxic actions.

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<![CDATA[Data of ureagenesis from ammonia, glutamine and alanine, and mitochondrial aquaporin-8 expression in thioacetamide-treated hepatocytes]]> https://www.researchpad.co/product?articleinfo=N31bbd1ba-207b-4380-9fa0-013b26ff2dd3

We present data about the synthesis of urea from different substrates, i.e., free ammonia, glutamine and alanine in primary cultured rat hepatocytes treated or untreated with the model hepatotoxic agent thioacetamide (TAA). We also provide data about the expression of mitochondrial aquaporin-8 (mtAQP8), a hepatocyte channel protein which facilitates ammonia diffusion into mitochondria to supply the urea cycle. Ammonia-derived ureagenesis was significantly inhibited by about 30% while that from the both amino acids resulted unaffected in TAA-treated hepatocytes. Protein expression of mtAQP8 was decreased by about 80% after TAA treatment. These data can be useful for the understanding of the mechanisms of drug-induced hepatic dysfunction.

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<![CDATA[Pipeline for the removal of hardware related artifacts and background noise for Raman spectroscopy]]> https://www.researchpad.co/product?articleinfo=N62784fe2-635a-4b82-912b-cad3436d7cd3

Raman spectroscopy is a real-time, non-contact, and non-destructive technique able to obtain information about the composition of materials, chemicals, and mixtures. It uses the energy transfer properties of molecules to detect the composition of matter. Raman spectroscopy is mainly used in the chemical field because background fluorescence and instrumental noise affect biological (in vitro and in vivo) measurements. In this method, we describe how hardware related artifacts and fluorescence background can be corrected without affecting signal of the measurement. First, we applied manual correction for cosmic ray spikes, followed by automated correction to reduce fluorescence and hardware related artifacts based on a partial 5th degree polynomial fitting and Tophat correction. Along with this manuscript we provide a MatLab script for the automated correction of Raman spectra.

  • Polynomial_Tophat_background_subtraction _methods.m” offers an automated method for the removal of hardware related artifacts and fluorescence signals in Raman spectra.

  • Polynomial_Tophat_background_subtraction _methods.m” provides a modifiable MatLab file adjustable for multipurpose spectroscopy analysis.

  • We offer a standardized method for Raman spectra processing suitable for biological and chemical applications for modular confocal Raman spectroscopes.

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<![CDATA[Data on the characterization of a platelet lysate and of the system in which it is included (nanoparticles/hydrogel), intended for the treatment of wounds]]> https://www.researchpad.co/product?articleinfo=N504cd2b6-9397-45c1-ae32-998fb84e4713

Platelet lysate has attracted attention for different biomedical applications, including biological processes where cellular proliferation and migration have been altered. Spectroscopic properties of a platelet lysate obtained from human platelets were performed in order to be incorporated in polymeric nanoparticles and then into a Pluronic F127 hydrogel, intended for wound healing (more details can be found at https://doi.org/10.1016/j.ejps.2020.105231 [1]). The platelet lysate (PL) was assessed by ultraviolet, infrared and circular dichroism spectroscopy. The developed hydrogel was also analyzed by infrared spectroscopy to evaluate if the Pluronic F127 structure was maintained when the nanoparticles or platelet lysate-loaded nanoparticles were included. The sol-gel transition temperature of the hydrogel was determined through its thermal behavior and by dynamic light scattering.

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<![CDATA[A novel method for the collection of highly developmental murine immature oocytes]]> https://www.researchpad.co/product?articleinfo=N2cfb2892-63b5-43ce-982e-b341a580758c

Isolation of germinal vesicle (GV) or metaphase I (MI) oocytes from large antral follicles, using a 30 gauge needle, in mice is a common method for the retrieval of immature oocytes from ovaries. However, this method depends entirely on the experience and judgment of the investigator. It is possible that not all of the isolated immature oocytes are from large antral follicles nor necessarily represent the cohort of oocytes that would be perfectly developed and consequently ovulated upon hormonal stimulation. Here, we administered an FDA approved phosphodiesterase 3A inhibitor, named cilostazol, in superovulated mice to result in the ovulation of GV or MI oocytes, depending on time and frequency of administration. The presented method results in mice ovulating GV or MI oocytes, which can be recovered from the oviduct without the investigator's judgment mentioned above. This method does not only result in immature oocytes with high yield, health, synchronized maturation, and competence levels but also is time and labor efficient. It also permits for physiological selections of a cohort of immature oocytes that would be entirely developed and eventually ovulated, as opposed to the conventional method.

  • Complete superovulation

  • Administration of cilostazol at different times

  • Recovery of ovulated immature oocytes from oviducts

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<![CDATA[Investigating the potential use of an ionic liquid (1-Butyl-1-methylpyrrolidinium bis(trifluoromethylsulfonyl)imide) as an anti-fungal treatment against the amphibian chytrid fungus, Batrachochytrium dendrobatidis]]> https://www.researchpad.co/product?articleinfo=N5c2fa054-4262-4dfe-83a3-c606a06f5241

The disease chytridiomycosis, caused by the pathogenic chytrid fungus, Batrachochytrium dendrobatidis (Bd), has contributed to global amphibian declines. Bd infects the keratinized epidermal tissue in amphibians and causes hyperkeratosis and excessive skin shedding. In individuals of susceptible species, the regulatory function of the amphibian’s skin is disrupted resulting in an electrolyte depletion, osmotic imbalance, and eventually death. Safe and effective treatments for chytridiomycosis are urgently needed to control chytrid fungal infections and stabilize populations of endangered amphibian species in captivity and in the wild. Currently, the most widely used anti-Bd treatment is itraconazole. Preparations of itraconazole formulated for amphibian use has proved effective, but treatment involves short baths over seven to ten days, a process which is logistically challenging, stressful, and causes long-term health effects. Here, we explore a novel anti-fungal therapeutic using a single application of the ionic liquid, 1-Butyl-1-methylpyrrolidinium bis(trifluoromethylsulfonyl)imide (BMP-NTf2), for the treatment of chytridiomycosis. BMP-NTf2 was found be effective at killing Bd in vitro at low concentrations (1:1000 dilution). We tested BMP-NTf2 in vivo on two amphibian species, one that is relatively tolerant of chytridiomycosis (Pseudacris regilla) and one that is highly susceptible (Dendrobates tinctorius). A toxicity trial revealed a surprising interaction between Bd infection status and the impact of BMP-NTf2 on D. tinctorius survival. Uninfected D. tinctorius tolerated BMP-NTf2 (mean ± SE; 96.01 ± 9.00 μl/g), such that only 1 out of 30 frogs died following treatment (at a dose of 156.95 μL/g), whereas, a lower dose (mean ± SE; 97.45 ± 3.52 μL/g) was not tolerated by Bd-infected D. tinctorius, where 15 of 23 frogs died shortly upon BMP-NTf2 application. Those that tolerated the BMP-NTf2 application did not exhibit Bd clearance. Thus, BMP-NTf2 application, under the conditions tested here, is not a suitable option for clearing Bd infection in D. tinctorius. However, different results were obtained for P. regilla. Two topical applications of BMP-NTf2 on Bd-infected P. regilla (using a lower BMP-NTf2 dose than on D. tinctorius, mean ± SE; 9.42 ± 1.43 μL/g) reduced Bd growth, although the effect was lower than that obtained by daily doses of itracanozole (50% frogs exhibited complete clearance on day 16 vs. 100% for itracanozole). Our findings suggest that BMP-NTf2 has the potential to treat Bd infection, however the effect depends on several parameters. Further optimization of dose and schedule are needed before BMP-NTf2 can be considered as a safe and effective alternative to more conventional antifungal agents, such as itraconazole.

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<![CDATA[Lateral flow immunoassay (LFIA) for the detection of lethal amatoxins from mushrooms]]> https://www.researchpad.co/product?articleinfo=N089b971a-62b1-4256-a74f-acfba8aef66c

The mushroom poison that causes the most deaths is the class of toxins known as amatoxins. Current methods to sensitively and selectively detect these toxins are limited by the need for expensive equipment, or they lack accuracy due to cross-reactivity with other chemicals found in mushrooms. In this work, we report the development of a competition-based lateral flow immunoassay (LFIA) for the rapid, portable, selective, and sensitive detection of amatoxins. Our assay clearly indicates the presence of 10 ng/mL of α-AMA or γ-AMA and the method including extraction and detection can be completed in approximately 10 minutes. The test can be easily read by eye and has a presumed shelf-life of at least 1 year. From testing 110 wild mushrooms, the LFIA identified 6 out of 6 species that were known to contain amatoxins. Other poisonous mushrooms known not to contain amatoxins tested negative by LFIA. This LFIA can be used to quickly identify amatoxin-containing mushrooms.

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<![CDATA[Effects of sea-level rise on physiological ecology of populations of a ground-dwelling ant]]> https://www.researchpad.co/product?articleinfo=N7f89605c-5421-4b76-a019-ba0e7ddd5b34

Introduction

Sea-level rise is a consequence of climate change that can impact the ecological and physiological changes of coastal, ground-dwelling species. Sea-level rise has a potential to inundate birds, rodents, spiders, and insects that live on the ground in coastal areas. Yet, there is still much to be learned concerning the specifics of these impacts. The red imported fire ant Solenopsis invicta (Buren) excavates soil for its home and is capable of surviving flooding. Because of their ground-dwelling life history and rapid reproduction, fire ants make an ideal model for discovery and prediction of changes that may be due to sea-level rise. There are up to 500,000 individuals in a colony, and these invasive ants naturally have a painful sting. However, observations suggest that colonies of fire ants that dwell in tidally-influenced areas are more aggressive with more frequent stings and more venom injected per sting (behavioral and physiological changes) than those located inland. This may be an adaption to sea-level rise. Therefore, the objective of this study is to elucidate differences in inland and coastal defensiveness via micro-dissection and comparison of head width, head length, stinger length, and venom sac volume. But first because fire ants’ ability to raft on brackish tidal water is unknown, it had to be determined if fire ants could indeed raft in brackish water and examine the behavior differences between those flooded with freshwater vs. saltwater.

Methods

To test the coastal-aggression hypothesis, inland colonies and coastal colonies, which experience relatively greater amounts of flooding, specifically regular tidal and windblown water and oscillations (i.e. El Nińo Southern Oscillation) from the Gulf of Mexico, were collected. To mimic sea-level rise, the colonies were flooded in salinities that correspond to both their collection site and conditions found in a variety of locales and situations (such as storm surge from a tropical storm). Individual ants were immediately taken from each colony for dissection before flooding, 1-hour into flooding, and 24-hours into flooding.

Results and discussion

Fire ants use their venom to defend themselves and to communicate alarm or aggression. Dissections and measurement of heads, venom sacs, and stingers revealed both coastal and inland colonies experience an increase in venom sac volume after 24 hours; in fact coastal colonies increased their venom volume by 75% after 24 h of flooding Whether this venom sac enlargement is due to diffusion of water or venom sac production is unknown. These ground-dwelling ants exhibit physiological and behavioral adaptations to ongoing sea-level rise possibly indicating that they are responding to increased flooding. Fire ants will raft on high-salinity water; and sea-level rise may cause stings by flooded ants to be more severe because of increased venom volume.

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<![CDATA[Data on the stability of darunavir/cobicistat suspension after tablet manipulation]]> https://www.researchpad.co/product?articleinfo=Nb07c557b-e791-4fd2-8ef9-697b722fc19b

The COVID-19 outbreak is now one of the most critical crises to manage for most of the national healthcare systems in the world. In the absence of authorised pharmacological treatments, many antiretrovirals, including darunavir/cobicistat fixed combination, are used off-label in the hospital wards as life-treating medicines for COVID-19 patients. Unfortunately, for most of them, the drug products available on the market are not designed to be administered by a nasogastric tube to inpatients of intensive care units. Therefore, their manipulation, even if it can strongly affect the product quality, is necessary for the preparation of suspension to meet patients’ need. In this situation, it is urgent to provide data and guidance to support hospital pharmacists and clinicians in their activity. The data in this article indicate that darunavir/cobicistat suspensions compounded by pharmacists using as active ingredient a commercially available tablet can be stable at least for one week.

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<![CDATA[Secondary prevention of acute coronary syndrome with antiplatelet agents in real life: A high-dimensional propensity score matched cohort study in the French National claims database]]> https://www.researchpad.co/product?articleinfo=N40eff8b8-f258-43ec-82a3-f4c81c576861

Graphical abstract

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<![CDATA[Identification of NUDT15 gene variants in Amazonian Amerindians and admixed individuals from northern Brazil]]> https://www.researchpad.co/product?articleinfo=N0a09703b-e69a-40d3-8ae4-dfe23e56b45d

Introduction

The nudix hydrolase 15 (NUDT15) gene acts in the metabolism of thiopurine, by catabolizing its active metabolite thioguanosine triphosphate into its inactivated form, thioguanosine monophosphate. The frequency of alternative NUDT15 alleles, in particular those that cause a drastic loss of gene function, varies widely among geographically distinct populations. In the general population of northern Brazilian, high toxicity rates (65%) have been recorded in patients treated with the standard protocol for acute lymphoblastic leukemia, which involves thiopurine-based drugs. The present study characterized the molecular profile of the coding region of the NUDT15 gene in two groups, non-admixed Amerindians and admixed individuals from the Amazon region of northern Brazil.

Methods

The entire NUDT15 gene was sequenced in 64 Amerindians from 12 Amazonian groups and 82 admixed individuals from northern Brazil. The DNA was extracted using phenol-chloroform. The exome libraries were prepared using the Nextera Rapid Capture Exome (Illumina) and SureSelect Human All Exon V6 (Agilent) kits. The allelic variants were annotated in the ViVa® (Viewer of Variants) software.

Results

Four NUDT15 variants were identified: rs374594155, rs1272632214, rs147390019, andrs116855232. The variants rs1272632214 and rs116855232 were in complete linkage disequilibrium, and were assigned to the NUDT15*2 genotype. These variants had high frequencies in both our study populations in comparison with other populations catalogued in the 1000 Genomes database. We also identified the NUDT15*4 haplotype in our study populations, at frequencies similar to those reported in other populations from around the world.

Conclusion

Our findings indicate that Amerindian and admixed populations from northern Brazil have high frequencies of the NUDT15 haplotypes that alter the metabolism profile of thiopurines.

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<![CDATA[Toxin-neutralizing antibodies elicited by naturally acquired cutaneous anthrax are elevated following severe disease and appear to target conformational epitopes]]> https://www.researchpad.co/product?articleinfo=N0733fdcc-4c39-44e4-82cd-032e69d54dbc

Understanding immune responses to native antigens in response to natural infections can lead to improved approaches to vaccination. This study sought to characterize the humoral immune response to anthrax toxin components, capsule and spore antigens in individuals (n = 46) from the Kayseri and Malatya regions of Turkey who had recovered from mild or severe forms of cutaneous anthrax infection, compared to regional healthy controls (n = 20). IgG antibodies to each toxin component, the poly-γ-D-glutamic acid capsule, the Bacillus collagen-like protein of anthracis (BclA) spore antigen, and the spore carbohydrate anthrose, were detected in the cases, with anthrax toxin neutralization and responses to Protective Antigen (PA) and Lethal Factor (LF) being higher following severe forms of the disease. Significant correlative relationships among responses to PA, LF, Edema Factor (EF) and capsule were observed among the cases. Though some regional control sera exhibited binding to a subset of the tested antigens, these samples did not neutralize anthrax toxins and lacked correlative relationships among antigen binding specificities observed in the cases. Comparison of serum binding to overlapping decapeptides covering the entire length of PA, LF and EF proteins in 26 cases compared to 8 regional controls revealed that anthrax toxin-neutralizing antibody responses elicited following natural cutaneous anthrax infection are directed to conformational epitopes. These studies support the concept of vaccination approaches that preserve conformational epitopes.

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<![CDATA[A compound attributes-based predictive model for drug induced liver injury in humans]]> https://www.researchpad.co/product?articleinfo=Ndeb57c49-a1cc-41d4-9618-08dc56c45dac

Drug induced liver injury (DILI) is one of the key safety concerns in drug development. To assess the likelihood of drug candidates with potential adverse reactions of liver, we propose a compound attributes-based approach to predicting hepatobiliary disorders that are routinely reported to US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS). Specifically, we developed a support vector machine (SVM) model with recursive feature extraction, based on physicochemical and structural properties of compounds as model input. Cross validation demonstrates that the predictive model has a robust performance with averaged 70% of both sensitivity and specificity over 500 trials. An independent validation was performed on public benchmark drugs and the results suggest potential utility of our model for identifying safety alerts. This in silico approach, upon further validation, would ultimately be implemented, together with other in vitro safety assays, for screening compounds early in drug development.

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<![CDATA[Extracellular DNA in blood products and its potential effects on transfusion]]> https://www.researchpad.co/product?articleinfo=N2c43a6d9-b325-4827-8d79-69a6ffb5c163

Abstract

Blood transfusions are sometimes necessary after a high loss of blood due to injury or surgery. Some people need regular transfusions due to medical conditions such as haemophilia or cancer. Studies have suggested that extracellular DNA including mitochondrial DNA present in the extracellular milieu of transfused blood products has biological actions that are capable of activating the innate immune systems and potentially contribute to some adverse reactions in transfusion. From the present work, it becomes increasingly clear that extracellular DNA encompassed mitochondrial DNA is far from being biologically inert in blood products. It has been demonstrated to be present in eligible blood products and thus can be transfused to blood recipients. Although the presence of extracellular DNA in human plasma was initially detected in 1948, some aspects have not been fully elucidated. In this review, we summarize the potential origins, clearance mechanisms, relevant structures, and potential role of extracellular DNA in the innate immune responses and its relationship with individual adverse reactions in transfusion.

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<![CDATA[Assessment of carcinogenic and toxic substances in ‘Insunko’ herb]]> https://www.researchpad.co/product?articleinfo=N89696eec-d4c5-4fdd-a866-12b7dbd9dccf

Highlights

  • Both males and females sniff ‘insunko’ herb, 3 g per day.

  • Females also insert ‘insunko’ herb vaginally, 6 g prior for sexual intercourse.

  • High concentration of toxic heavy metals have been detected in ‘insunko’ herb.

  • Hazard Indexes for arsenic, cadmium, chromium, manganese, and copper were greater than one.

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<![CDATA[Effect of Crop Volume on Contraction Rate in Adult House Fly]]> https://www.researchpad.co/product?articleinfo=N338ab037-04b4-4636-abfe-cf4da4af0e94

Abstract

The functional aspects of the adult house fly crop have not been studied even though various human and domestic animal pathogens have been discovered within the crop lumen. The average volume consumed (midgut and crop) by flies starved for 24 h was 3.88 μl by feeding both sexes on a sucrose phosphate glutamate buffer. In addition, various volumes of a solution (0.125 M sucrose plus Amaranth dye) were fed to 3-d-old adult female house flies to quantify the crop contraction rate as affected by crop volume. As crop volume increased, the contraction rate increased until it reached a peak at 2 μl, after which it declined. It is hypothesized that the high contraction rate of the crop, which in house fly is almost twice the rate of three other fly species, is one of the factors that makes house fly an excellent vector. The mechanism for such a high contraction rate needs to be investigated.

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<![CDATA[Comparison of Fresh and Room-Aged Cigarette Sidestream Smoke in a Subchronic Inhalation Study on Rats]]> https://www.researchpad.co/product?articleinfo=Na555ad33-8288-4b78-bd49-87abee85207b

Abstract

Two experimental types of cigarette sidestream smoke (SS) were compared in a subchronic inhalation study on rats. Fresh SS (FSS) was generated continuously from the reference cigarette 2R1. Room-aged SS (RASS) was generated by aging FSS for 1.5 h in a room with noninert surfaces with materials typically found in residences or offices. Male Sprague-Dawley rats were head-only exposed to three dose levels of each SS type and to filtered, conditioned fresh air (sham-exposure) for 6 h/day, 7 days/week, for 90 days. Room-aging resulted in decreased concentrations of various SS components, e.g., total participate matter (TPM) and nicotine, while other components, such as carbon monoxide (CO), were not affected. The CO concentrations were 6, 13, and 28 ppm for both SS types. TPM concentrations were between 0.6 and 8.7 (μg/liter and thus up to 100-fold above the maximum of average concentrations of respiratory suspended particles reported for environmental tobacco smoke. Slight reserve cell hyperplasia in the anterior part of the nose as well as hyperplastic and metaplastic epithelial changes in the larynx were the only observed dose-dependent findings. The metabolism of benzo(a)-pyrene-as a proxy for polycyclic aromatic hydrocarbon metabolism-was induced in the nasal respiratory epithelium and in the lungs while no effect was seen in the nasal olfactory epithelium. The lowest-observed effect level was 6 ppm CO or 0.6 μg TPM/liter. Most of the effects seen were less expressed in RASS- than in FSS-exposed rats when compared on the basis of the CO concentrations. When compared on the basis of TPM, these effects were equally pronounced for both SS types, suggesting a major role of particulate matter-associated compounds. All findings reverted to sham control levels following a 42-day postinhalation period.

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<![CDATA[The biochemical and metabolic profiles of dairy cows with mycotoxins-contaminated diets]]> https://www.researchpad.co/product?articleinfo=N22e82420-dbfc-489c-86c7-6f9a6d57617d

Background

Previous studies on the effects of mycotoxins have solely focused on their biochemical profiles or products in dairy ruminants. Changes in metabolism that occur after exposure to mycotoxins, as well as biochemical changes, have not been explored.

Methods

We measured the biochemical and metabolic changes in dairy cows after exposure to mycotoxins using biochemical analyses and nuclear magnetic resonance. Twenty-four dairy cows were randomly assigned to three different treatment groups. Control cows received diets with 2 kg uncontaminated cottonseed. Cows in the 50% replacement group received the same diet as the control group, but with 1 kg of uncontaminated cottonseed and 1 kg of cottonseed contaminated with mycotoxins. Cows in the 100% replacement group received the same diet as the control, but with 2 kg contaminated cottonseed.

Results

The results showed that serum γ-glutamyl transpeptidase and total antioxidant capacities were significantly affected by cottonseed contaminated with mycotoxins. There were also significant differences in isovalerate and NH3-N levels, and significant differences in the eight plasma metabolites among the three groups. These metabolites are mainly involved in amino acid metabolism pathways. Therefore, the results suggest that amino acid metabolism pathways may be affected by mycotoxins exposure.

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<![CDATA[Data on metabolic stability, aqueous solubility and CYP inhibition of novel triazole-based nicotinamide phosphoribosyltransferase (NAMPT) inhibitors]]> https://www.researchpad.co/product?articleinfo=N60ba1e8b-af71-45b3-ab92-d5cb2dc5e5e0

In the related research article, entitled “Identification of novel triazole-based nicotinamide phosphoribosyltransferase (NAMPT) inhibitors endowed with antiproliferative and antiinflammatory activity” [1], we reported the in vitro hepatic metabolism data for compounds 30c, 48b, and 31b (here named as E5, A6, and T1), in comparison with the reference compounds GPP78 and FK866 [1–3]. In this article, we retrieved the available data about the hepatic microsomal stability and metabolites structural characterization of the entire library of triazole-based NAMPT inhibitors, also implementing the given information with data regarding aqueous solubility and CYP inhibition. Compounds are divided in subclasses based on the hydrolytic resistant groups replacing the amide function of GPP78 [1, 2].

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