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Instead, the depression of biliary excretion of ibuprofen and ibuprofen metabolites turned out to be the indicative marker of hyperglycemia. The observed changes impact the pharmacokinetics of drugs administered in hyperglycemic individuals.Renal cell carcinoma is the most lethal cancer of the urological system due to late diagnosis and treatment resistance. Propolis, a beehive product, is a valuable natural source of compounds with bioactivities and may be a beneficial addition to current anticancer treatments. A Portuguese propolis sample, its fractions (n-hexane, ethyl acetate, n-butanol and water) and three subfractions (P1-P3), were tested for their toxicity on A498, 786-O and Caki-2 renal cell carcinoma cell lines and the non-neoplastic HK2 kidney cells. The ethyl acetate fraction showed the strongest toxicity against A498 (IC50 = 0.162 µg mL-1) and 786-O (IC50 = 0.271 µg mL-1) cells. With similar toxicity against 786-O, P1 (IC50 = 3.8 µg mL-1) and P3 (IC50 = 3.1 µg mL-1) exhibited greater effect when combined (IC50 = 2.5 µg mL-1). Results support the potential of propolis and its constituents as promising coadjuvants in renal cell carcinoma treatment.Modeling the dynamics of non-bound states in molecules requires an accurate description of how electronic motion affects nuclear motion and vice-versa. The exact factorization (XF) approach offers a unique perspective, in that it provides potentials that act on the nuclear subsystem or electronic subsystem, which contain the effects of the coupling to the other subsystem in an exact way. We briefly review the various applications of the XF idea in different realms, and how features of these potentials aid in the interpretation of two different laser-driven dissociation mechanisms. We present a detailed study of the different ways the coupling terms in recently-developed XF-based mixed quantum-classical approximations are evaluated, where either truly coupled trajectories, or auxiliary trajectories that mimic the coupling are used, and discuss their effect in both a surface-hopping framework as well as the rigorously-derived coupled-trajectory mixed quantum-classical approach.The polyphenolic extract of Ilex latifolia (PEIL) exhibits a variety of biological activities. An evaluation of the parameters influencing the ultrasonic extraction process and the assessment of PEIL antioxidant activity are presented herein. Response surface methodology (RSM) was used to optimize the experimental conditions for the polyphenols ultrasonic-assisted extraction (UAE) from the leaves of Ilex latifolia. We identified the following optimal conditions of PEIL ethanol concentration of 53%, extraction temperature of 60 °C, extraction time of 26 min and liquid-solid ratio of 60 mL/g. Using these parameters, the UAE had a yield of 35.77 ± 0.26 mg GAE/g, similar to the value we predicted using RSM (35.864 mg GAE/g). The antioxidant activity of PEIL was assessed in vitro, using various assays, as well as in vivo. We tested the effects of various doses of PEIL on D-galactose induced aging. Vitamin C (Vc) was used as positive control. After 21 days of administration, we measured superoxide dismutase (SOD) aated.
Health care-associated infections (HAIs) are a significant public health problem worldwide, favoring multidrug-resistant (MDR) microorganisms. The SARS-CoV-2 infection was negatively associated with the increase in antimicrobial resistance, and the ESKAPE group had the most significant impact on HAIs. The study evaluated the bactericidal effect of a high concentration of O
gas on some reference and ESKAPE bacteria.
Four standard strains and four clinical or environmental MDR strains were exposed to elevated ozone doses at different concentrations and times. NSC 737664 Bacterial inactivation (growth and cultivability) was investigated using colony counts and resazurin as metabolic indicators. Scanning electron microscopy (SEM) was performed.
The culture exposure to a high level of O
inhibited the growth of all bacterial strains tested with a statistically significant reduction in colony count compared to the control group. The cell viability of
(MRSA) (99.6%) and
(XDR) (29.2%) was reduced considerably, an high doses of ozone were able to interfere with the growth of all strains studied, evidencing that ozone-based decontamination approaches may represent the future of hospital cleaning methods.Technetium-99m macroaggregated albumin ([99mTc]Tc-MAA) is an injectable radiopharmaceutical used in nuclear medicine for lung perfusion scintigraphy. After changing to a new batch of macroaggregated albumin (MAA), we saw unwanted uptake in the liver and spleen. The batch was therefore tested by both the supplier and us and we found it to comply with the requirements of the European Pharmacopoeia (Ph. Eur.). However, a simple comparison between the problematic batch and a batch supplied by another manufacturer showed that there was a significant difference. The quality testing showed a higher number of small particles in the problem encumbered MAA batch with unwanted in vivo uptake. In this article we present a simple method of testing for particle size of [99mTc]Tc-MAA, which gives a good indication of how the radioactive drug performs in vivo. We argue that the quality control method described in the Ph. Eur. should be changed. The changes will improve concordance between the laboratory analyzes and what is seen in vivo in human lung perfusion scintigraphy. Furthermore, we hope that the MAA suppliers without delay will replace their release procedure to be in accordance with the method described in this article.Genista monspessulana (L.) L.A.S. Johnson (Fabaceae) is a Mediterranean plant introduced to South America and other regions for ornamental purposes. However, it is considered an invasive shrub due to its reproductive vigor in many areas. Unlike other Genista plants, G. monspessulana has few studies disclosing its biologically active components, particularly cytotoxic agents against cancer cells. Thus, as part of our research on anti-proliferative bioactives, a set of ethanolic seed extracts from ten accessions of G. monspessulana, collected in the Bogotá plateau, were evaluated against four cell lines PC-3 (prostate adenocarcinoma), SiHa (cervical carcinoma), A549 (lung carcinoma), and L929 (normal mouse fibroblasts). Extracts were also analyzed through liquid chromatography coupled with mass spectrometry (LC/MS) to record chemical fingerprints and determine the composition and metabolite variability between accessions. Using multiple covariate statistics, chemical and bioactivity datasets were integrated to used on the targeted isolation of anti-proliferative compounds from Genista plants and accessions.Propolis contains a wide range of pharmacological activities because of their various bioactive compounds. The beneficial effect of propolis is interesting for treating type-2 diabetes mellitus (T2DM) owing to dysregulation of multiple metabolic processes. In this study, 275 of 658 Asian propolis compounds were evaluated as potential anti-T2DM agents using the DIA-DB web server towards 18 known anti-diabetes protein targets. More than 20% of all compounds could bind to more than five diabetes targets with high binding affinity (<-9.0 kcal/mol). Filtering with physicochemical and pharmacokinetic properties, including ADMET parameters, 12 compounds were identified as potential anti-T2DM with favorable ADMET properties. Six of those compounds, (2R)-7,4'-dihydroxy-5-methoxy-8-methylflavone; (RR)-(+)-3'-senecioylkhellactone; 2',4',6'-trihydroxy chalcone; alpinetin; pinobanksin-3-O-butyrate; and pinocembrin-5-methyl ether were first reported as anti-T2DM agents. We identified the significant T2DM targets of Asian propolis, namely retinol-binding protein-4 (RBP4) and aldose reductase (AKR1B1) that have important roles in insulin sensitivity and diabetes complication, respectively. Molecular dynamic simulations showed stable interaction of selected propolis compounds in the active site of RBP4 and AKR1B1. These findings suggest that Asian propolis compound may be effective for treatment of T2DM by targeting RBP4 and AKR1B1.Ethnobotanical studies have reported the traditional medicinal uses of Acacia senegal (L.) Willd. and Argania spinosa (L.) Skeels against kidney stone formation and other chronic kidney diseases. The present work is undertaken to study the litholytic activity and the inhibiting activity of calcium oxalate crystallization by bioactive compounds identified in Argania spinosa (L.) Skeels press-cake (residue of Argan oil) and in Acacia senegal (L.) Willd. The litholytic activity was studied in vitro on cystine and uric acid stones using a porous bag and an Erlenmeyer glass. The study of the inhibiting activity of calcium oxalate crystallization, was based on temporal measurements of the optical density, registered at a 620 nm wavelength for 30 min using an ultraviolet-visible spectrophotometer. The silylation method was performed to identify phytochemicals, followed by gas chromatography coupled with mass spectrophotometry (GC/MS) analysis. The results show significant litholytic activity of Argania Spinosa press-cake hydro-ethanolic extract on uric acid and cystine stones, respectively, with dissolution rates (DR) of 86.38% and 60.42% versus 3.23% and 9.48% for the hydro-ethanolic extract of Acacia senegal exudate. Furthermore, the percentages of nucleation inhibition are 83.78% and 43.77% (p ˂ 0.05) for Argania spinosa and Acacia senegal, respectively. The results point to the detection of 17 phytochemicals in Argania spinosa press-cake extract, the majority of which are phenolic acids and have potent anti-urolithiatic action.Three organic blue-light-emitting tetraphenylethylene (TPE) derivatives that exhibit aggregation-induced emission (AIE) were used as additives in the preparation of inorganic perovskite-structured green-light-emitting materials for three-color white-light emission. For these organic-inorganic light-emitting materials, two-color (blue and green) light-emitting films based on the CsPbBr3 perovskite-structured green-light-emitting inorganic material were prepared. The three TPE derivatives were prepared by varying the number of bromide groups, and a distinct AIE effect was confirmed when the derivatives were dissolved in a water-tetrahydrofuran mixed solvent containing 90 vol% water. When 0.2 molar ratio of the 1,1,2,2-tetrakis(4-bromophenyl)ethylene (TeBrTPE) additive was mixed with nanocrystal-pinning toluene solvent, the green-light-emission photoluminescence quantum efficiency (PLQY) value at 535 nm was 47 times greater than that of the pure bulk CsPbBr3 without additives and a blue emission at 475 nm was observed from the TeBrTPE itself. When a CBPIr(piq)3 film was prepared on top of this layer, three PL peaks with maximum wavelength values of 470, 535, and 613 nm were confirmed. The film exhibited white-light emission with CIE color coordinates of (0.25, 0.36).The antitumor effects of Coix lacryma-jobi L. var. ma-yuen Stapf. (adlay seed) ethanolic extract have been increasingly shown. This study aimed to investigate the beneficial effects of both the fractions and subfractions of adlay seed ethanolic extract on the human breast (MCF-7) and cervical (HeLa) cancer cell lines, as well as exploring their possible mechanisms of action. The ethanolic extracts were obtained from different parts of adlay seed, including AHE (adlay hull extract), ATE (adlay testa extract), ABE (adlay bran extract) and PAE (polished adlay extract). The results of a 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl- tetrazolium bromide (MTT) assay showed that AHE-Ea and ATE-Ea showed significant growth inhibitory effects in a dose-dependent manner. The results also showed that the AHE-Ea-K, AHE-Ea-L, ATE-Ea-E and ATE-Ea-F subfractions inhibited cell proliferation, induced cell cycle arrest in the G0/G1 phase and decreased CDK4/Cyclin D1 protein expression. Finally, the extract activated caspase-3 activity and PARP protein expression, which induced MCF-7 and HeLa cell apoptosis.
Website: https://www.selleckchem.com/products/ABT-888.html
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