ResearchPad - pharmacology-toxicology-and-pharmaceutical-science https://www.researchpad.co Default RSS Feed en-us © 2020 Newgen KnowledgeWorks <![CDATA[Avidin-biotin technology to synthesize multi-arm nano-construct for drug delivery]]> https://www.researchpad.co/article/elastic_article_5891 Image, graphical abstract

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<![CDATA[Pipeline for the removal of hardware related artifacts and background noise for Raman spectroscopy]]> https://www.researchpad.co/article/N62784fe2-635a-4b82-912b-cad3436d7cd3 Image, graphical abstract

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<![CDATA[A novel method for the collection of highly developmental murine immature oocytes]]> https://www.researchpad.co/article/N2cfb2892-63b5-43ce-982e-b341a580758c Image, graphical abstract

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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/article/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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<![CDATA[Data of ureagenesis from ammonia, glutamine and alanine, and mitochondrial aquaporin-8 expression in thioacetamide-treated hepatocytes]]> https://www.researchpad.co/article/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[Data on the stability of darunavir/cobicistat suspension after tablet manipulation]]> https://www.researchpad.co/article/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/article/N40eff8b8-f258-43ec-82a3-f4c81c576861

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<![CDATA[The method simulating spontaneous pain in patients with nociplastic pain using rats with fibromyalgia-like condition]]> https://www.researchpad.co/article/N7b23d9d7-4da4-4ec5-a86b-1cd7d92bc21e

The method shown in this article simulates spontaneous pain in patients with nociplastic pain using rats; the measurement with this method could be related to better translation of analgesic efficacies of therapeutic compounds between rats and humans. Nociplastic pain occurs in various disorders including fibromyalgia. Because the pain in patients occurs without an external stimulus, we assessed spontaneous pain in rats. The grimace scale, a methodology for rating facial expression, has been used for measuring spontaneous pain in animals. However, the responses in animals have been rather short-lived, and the scale has never been applied to animals exhibiting nociplastic pain. Here, we apply the rat grimace scale (RGS) to the reserpine-induced fibromyalgia-like rat, which induces nociplastic pain. The ratings of the orbital tightening, nose/cheek flattening, and changes in characteristics of ears and whiskers by three raters, who were blinded to the treatment allocated to rats, demonstrated substantial, long-lasting change in facial expression of rats. In this article, reference images for raters, and sample images used for rater training are provided. All raters independently indicated that the RGS score is significantly elevated with this methodology in reserpine-induced fibromyalgia-like rats.

  • The grimace scale, a method for rating facial expression, is applied to the reserpine-induced fibromyalgia-like rat, which manifests nociplastic pain.

  • Facial expression change in the reserpine-induced fibromyalgia-like rat is substantial and long-lasting.

  • Elevation of the RGS score in the reserpine-induced fibromyalgia-like rat may simulate spontaneous pain in patients with nociplastic pain.

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<![CDATA[Data on GC-MS analysis, in vitro anti-oxidant and anti-microbial activity of the Catharanthus roseus and Moringa oleifera leaf extracts]]> https://www.researchpad.co/article/N6a38c90d-0037-4102-b25f-966a2cdd83eb

The article reports data on chemical profiling by gas chromatography-mass spectrometry (GC-MS) of aqueous and methanolic leaf extracts of Madagascar periwinkle (Catharanthus roseus) and drumstick tree (Moringa oleifera) and on their antioxidant and antibacterial effects against three clinical human pathogens. In total 105 compounds were tentatively identified; in which 65 in Catharanthus roseus and 40 in Moringa oleifera compounds. A large number of peaks with good area percentage was found in methanolic extract of Catharanthus roseus with core chemical constituents such as trans-squalene, n-hexadecanoic acid, Eicosyl acetate, stearin, 1H-Benz(G)indole-3-carboxylic acid. The corresponding constituents from Moringa oleifera include 9-Octadecenoic acid (z)-, Heptadecanoic acid and phytol acetate. The highest scavenging activity (87.7% at 200 μg/mL) was shown by DPPH aqueous leaf extract of C. roseus. Moreover, the methanolic scavenging of both plant extracts was in the order of FRAP>DPPH>NO> H2O2 with lowest antioxidant activity (51.4% at 200 μg/mL) exposed by Catharanthus roseus in comparison of all cases. Good antibacterial action was examined against three different organisms (E.coli, B. subtilis and S. aureus) of aqueous infusion of Catharanthus roseus.

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<![CDATA[A method to dissolve 3-MCPD mono- and di-esters in aqueous cell culture media]]> https://www.researchpad.co/article/N845aa6e8-ad45-4619-a30e-ca25563e4888

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<![CDATA[Protocol for evaluating the abilities of diverse nitroaromatic prodrug metabolites to exit a model Gram negative bacterial vector]]> https://www.researchpad.co/article/N3dad3f2d-00d1-4f45-af16-275f5285761b

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<![CDATA[Method for the synthesis of flavonoid nitrogen mustard derivatives]]> https://www.researchpad.co/article/Nf5a4d441-4c88-4a0e-902c-682cd90673d3 <![CDATA[Data demonstrating the challenges of determining the kinetic parameters of P-gp mediated transport of low-water soluble substrates]]> https://www.researchpad.co/article/5b4bdbb0463d7e7e0dcdb8a5

The presented data are related to the research article entitled “Characterization of the IPEC-J2 MDR1 (iP-gp) cell line as a tool for identification of P-gp substrates” by Ozgur et al. (2017) [1]. This data report describes the challenges of investigating the concentration-dependent transport of P-glycoprotein (P-gp) substrates with relatively low aqueous solubility. Thus, we provide solubility data on two prototypical P-gp substrates, digoxin and rhodamine 123, representing P-gp substrates with a relatively low- and high-aqueous solubility, respectively. We present a hypothetical Michaelis-Menten curve of the P-gp mediated transport of digoxin to demonstrate that the maximal donor concentration, which can be reached in the experimental transport buffer, is too low to yield transport data in the saturable range of the Michaelis-Menten relationship. Furthermore, we present data on the bidirectional transport of digoxin and rhodamine 123 across cell monolayers of the MDCK II MDR1 cell line and iP-pg cell line in the presence of the selective P-gp inhibitor, zosuquidar/LY335979.

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