12,165 results match your criteria 2-[4-1-hydroxy-2-methylpropylphenyl]propanoic acid


Biostability study, quantitation method and preliminary pharmacokinetics of a new antifilovirus agent based on borneol and 3-(piperidin-1-yl)propanoic acid.

J Pharm Biomed Anal 2021 Apr 3;199:114062. Epub 2021 Apr 3.

N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, acad. Lavrentiev ave., 9, Novosibirsk, 630090, Russia; Novosibirsk State University, Pirogov str., 2, Novosibirsk, 630090, Russia.

The stability of the new antifiloviral agent AS-358, which is a derivative of borneol and 3-(piperidin-1-yl)propanoic acid, was studied in the blood and blood plasma of rats in vitro. It was found that both in the blood and in the plasma stabilized by EDTA or heparin, the compound is rapidly hydrolyzed at the ester bond. When sodium fluoride was added to the whole blood, the decomposition of the compound was significantly slowed down, which made it possible to develop and validate a method for the quantitative determination of the agent in this matrix. Read More

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Insight on the fractionations and structural characterizations of innovative antidiarrheal compounds screened from leaves of Psidium guajava of local origin in Pakistan.

Pak J Pharm Sci 2020 Sep;33(5(Supplementary)):2323-2329

Imran Adrees College of Pharmacy, 3Km Daska Road, Sialkot, Pakistan.

Numerous ailments have been effectively treated with natural plants for long time all over the world. Plants provided a back bone for the exploration of novel medicinal compounds. Therefore, chief focus of our study was to isolate the biologically active compounds from the plant source and evaluate their antidiarrheal potentials, as diarrhea is still the most dominant disease in developing countries. Read More

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September 2020

Xanthenylacetic Acid Derivatives Effectively Target Lysophosphatidic Acid Receptor 6 to Inhibit Hepatocellular Carcinoma Cell Growth.

ChemMedChem 2021 Apr 8. Epub 2021 Apr 8.

University of Bari School of Medicine, Interdisciplinary of Medicine, Piazza G. Cesare, 11, 76124, Bari, ITALY.

Despite the increasing incidence of Hepatocellular carcinoma (HCC) worldwide, current pharmacological treatments are still unsatisfactory. We have previously shown that lysophosphatidic acid receptor 6 (LPAR6) supports HCC growth and that 9-xanthenylacetic acid (XAA) acts as an LPAR6 antagonist inhibiting HCC growth without toxicity. Here, we synthesized four novel XAA derivatives, (±)-2-(9H-xanthen-9-yl)propanoic acid (compound 4 - MC9), (±)-2-(9H-xanthen-9-yl)butanoic acid (compound 5 - MC6), (±)-2-(9H-xanthen-9-yl)hexanoic acid (compound 7 - MC11), and (±)-2-(9H-xanthen-9-yl)octanoic acid (compound 8 - MC12, sodium salt) by introducing alkyl groups of increasing length at the acetic α-carbon atom. Read More

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Sulfur amino acids status controls selenium methylation in : Identification of a novel metabolite from promiscuous enzyme reactions.

Appl Environ Microbiol 2021 Apr 2. Epub 2021 Apr 2.

Institute for Ecopreneurship, School of Life Sciences, University of Applied Sciences and Arts Northwestern Switzerland, Hofackerstrasse 30, 4132 Muttenz, Switzerland.

Selenium (Se) deficiency affects many millions of people worldwide, and the volatilization of methylated Se species to the atmosphere may prevent Se from entering the food chain. Despite the extent of Se deficiency, little is known about fluxes in volatile Se species and their temporal and spatial variation in the environment, giving rise to uncertainty in atmospheric transport models. To systematically determine fluxes, one can rely on laboratory microcosm experiments to quantify Se volatilization in different conditions. Read More

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Per- and Polyfluoroalkyl Substance (PFAS) Transport from Groundwater to Streams near a PFAS Manufacturing Facility in North Carolina, USA.

Environ Sci Technol 2021 Apr 2. Epub 2021 Apr 2.

Department of Civil, Construction, and Environmental Engineering, North Carolina State University, Raleigh 27695-8201, North Carolina, United States.

We quantified per- and polyfluoroalkyl substance (PFAS) transport from groundwater to five tributaries of the Cape Fear River near a PFAS manufacturing facility in North Carolina (USA). Hydrologic and PFAS data were coupled to quantify PFAS fluxes from groundwater to the tributaries. Up to 29 PFAS were analyzed, including perfluoroalkyl acids and recently identified fluoroethers. Read More

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Effects of smoking on the optimal effect-site concentration of remifentanil required for preventing cough during anesthetic emergence in male patients undergoing laparoscopic or robotic cholecystectomy.

Medicine (Baltimore) 2021 Apr;100(13):e25288

Department of Anesthesiology and Pain Medicine.

Abstract: Target-controlled infusion of remifentanil is known to reduce cough effectively during emergence from general anesthesia. The effect of smoking on emergence cough remains controversial. Therefore, we aimed to investigate the effect-site concentration (Ce) of remifentanil in the male patients undergoing laparoscopic or robotic cholecystectomy for suppressing emergence cough in smokers and non-smokers. Read More

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Structure-Activity Relationship Study and Biological Evaluation of 2-(Disubstituted phenyl)-indole-5-propanoic Acid Derivatives as GPR40 Full Agonists.

J Med Chem 2021 Apr 26;64(7):4130-4149. Epub 2021 Mar 26.

School of Pharmacy, Sungkyunkwan University, Suwon 16419, South Korea.

G-protein-coupled receptor 40 (GPR40) is considered as an attractive drug target for treating type 2 diabetes, owing to its role in the free fatty acid-mediated increase in glucose-stimulated insulin secretion (GSIS) from pancreatic β-cells. To identify a new chemotype of GPR40 agonist, a series of 2-aryl-substituted indole-5-propanoic acid derivatives were designed and synthesized. We identified two GPR40 agonist lead compounds- (3-[2-(4-fluoro-2-methylphenyl)-1-indol-5-yl]propanoic acid) and (3-[2-(2,5-dimethylphenyl)-1-indol-5-yl]propanoic acid), having GSIS and glucagon-like peptide 1 secretory effects. Read More

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The efficacy of novel metabolic targeted agents and natural plant drugs for nonalcoholic fatty liver disease treatment: A PRISMA-compliant network meta-analysis of randomized controlled trials.

Medicine (Baltimore) 2021 Mar;100(12):e24884

The First Clinical Medical College of Nanjing University of Chinese Medicine, Nanjing.

Background: Nonalcoholic fatty liver disease (NAFLD) is a highly prevalent chronic liver disease characterized by excess accumulation of fat in hepatocytes. Because no drug has been approved for NAFLD treatment, this work analyzed the effects of agents resulting from 2 research hotspots, metabolic target agents, and natural plant drugs, on NAFLD with network meta-analysis.

Methods: Public databases were searched through August 14, 2020. Read More

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Strawberry Consumption, Cardiometabolic Risk Factors, and Vascular Function: A Randomized Controlled Trial in Adults with Moderate Hypercholesterolemia.

J Nutr 2021 Mar 23. Epub 2021 Mar 23.

Department of Food Science and Nutrition, Center for Nutrition Research, Institute for Food Safety and Health, Illinois Institute of Technology, Chicago, IL, USA.

Background: Certain fruits, such as strawberries, may impart cardiometabolic benefits due to their phytochemical content.

Objectives: Study aims were to assess the effects of strawberry intake on cardiometabolic risk factors and vascular endothelial function in adults with moderate hypercholesterolemia.

Methods: This study was a randomized, controlled, double-blinded, 2-arm, 2-period (4-wk/period) crossover trial. Read More

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Efficacy of target controlled infusion of remifentanil with spontaneous ventilation for procedural sedation and analgesia (Remi TCI PSA): A double center prospective observational study.

J Opioid Manag 2021 Jan-Feb;17(1):69-78

Department of Anaesthesia, Gustave Roussy Cancer Centre, Villejuif, France.

Objective: Remifentanil, a rapid onset rapid offset synthetic opioid and potent analgesic, is often used for procedural conscious sedation in spontaneous ventilation, especially when delivered in target controlled infusion (TCI), which allows precise titration. We assessed efficacy, tolerance, and adverse events related with the use of remifentanil TCI during various procedures.

Design: Prospective, observational. Read More

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2-[Bis(carboxymethyl)amino] propanoic acid-Chelated Copper Chelate Enhances Bacterial Elimination by Sodium Percarbonate.

Biocontrol Sci 2021 ;26(1):9-15

Department of Applied Molecular Chemistry, Graduate School of Industrial Technology, Nihon University.

Sodium percarbonate (SP) is a relatively low-cost and stable solid oxidizer with a small environmental burden. It is often included in cleansers for sanitizing circulating water pipes and as bleaching reagents in laundry, although the bactericidal effect of SP is lower than that of chlorine-based agents. 2-[Bis(carboxymethyl)amino] propanoic acid-chelated copper (MGDA-Cu) was added to increase the effect of SP. Read More

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January 2021

Effects of dietary chromium propionate on laying performance, egg quality, serum biochemical parameters and antioxidant status of laying ducks under heat stress.

Animal 2021 Feb 10;15(2):100081. Epub 2020 Dec 10.

Institute of Animal Husbandry and Veterinary Science, Jiangxi Academy of Agricultural Sciences, Nanchang 330200, China.

Recent studies have shown that chromium (Cr) could alleviate the negative effects of heat stress on livestock and poultry, but there is little information available to laying ducks. This study aimed to investigate the effects of dietary addition of chromium propionate on laying performance, egg quality, serum biochemical parameters and antioxidant status of laying ducks under hot (average 32 °C) and humid (average 75% relative humidity) summer conditions. A total of 900 66-week-old weight- and laying-matched Shanma laying ducks were randomly divided into five treatments, each with 6 replicates of 30 individually caged birds. Read More

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February 2021

Identification of Chemical Composition and Metal Determination of (Forssk) Stem Constituents Using ICP-MS, GC-MS-MS, and DART-MS.

J Anal Methods Chem 2021 24;2021:6667238. Epub 2021 Feb 24.

Department of Chemistry, College of Science, King Saud University, Riyadh 11451, Saudi Arabia.

This study aims to investigate the chemical constituents of the stem of growing in Saudi Arabia. The organic and inorganic composition of ethanol extract of stem has been explored using direct analysis in real time-mass spectrometry (DART-MS), gas chromatography-mass spectrometry (GC-MS), and inductively coupled plasma-mass spectrometry (ICP-MS). Analysis conducted by DART-MS and GC-MS reveals the presence of several interesting organic constituents identified as 2,4-di-tert-butylphenol, sparteine, benzenepropanoic acid, 3,5-bis(1,1-dimethylethyl)-4-hydroxy-, methyl ester, phthalic acid, 1-octadecanol, squalene, argentamin, 2,4-di-tert-butylphenol, sparteine, benzene propanoic acid, 3,5-bis(1,1-dimethylethyl)-4-hydroxy-, methyl ester, phthalic acid, 1-octadecanol, squalene, argentamin, and hentriacontane in the ethanol extract of the stem. Read More

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February 2021

Innovative 2'--Imino-2-propanoate-Protecting Group for Effective Solid-Phase Synthesis and 2'--Deprotection of RNA Sequences.

J Org Chem 2021 Apr 11;86(7):4944-4956. Epub 2021 Mar 11.

Laboratory of Biological Chemistry, Division of Biotechnology Review and Research IV, Center for Drug Evaluation and Research, Food and Drug Administration, 10903 New Hampshire Avenue, Silver Spring, Maryland 20993, United States.

The implementation of protecting groups for the 2'-hydroxyl function of ribonucleosides is still challenging, particularly when RNA sequences must be of the highest purity for therapeutic applications as nucleic acid-based drugs. A 2'-hydroxyl-protecting group should optimally (i) be easy to install; (ii) allow rapid and efficient incorporation of the 2'--protected ribonucleosides into RNA sequences to minimize, to the greatest extent possible, the formation of process-related impurities (, shorter than full-length sequences) during solid-phase synthesis; and (iii) be completely cleaved from RNA sequences without the production of alkylating side products and/or formation of mutagenic nucleobase adducts. The reaction of 2'--aminoribonucleosides with ethyl pyruvate results in the formation of stable 2'--imino-2-methyl propanoic acid ethyl esters and, subsequently, of the fully protected ribonucleoside phosphoramidite monomers, which are required for the solid-phase synthesis of two chimeric RNA sequences (20-mers) containing the four canonical ribonucleosides. Read More

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Probiotic potential of γ-aminobutyric acid (GABA)-producing yeast and its influence on the quality of cheese.

J Dairy Sci 2021 Mar 5. Epub 2021 Mar 5.

School of Food Science and Technology and Key Laboratory of Xinjiang Phytomedicine Resource and Utilization of the Ministry of Education, Shihezi University, Shihezi, Xinjiang 832000, P. R. China. Electronic address:

Kazakh cheese is a traditional dairy product in Xinjiang, China. To study the function and potential probiotic characteristics of yeast in Kazakh cheese and its contribution to cheese fermentation, we screened the γ-aminobutyric acid (GABA)-producing yeasts Pichia kudriavzevii 1-21, Kluyveromyces marxianus B13-5, Saccharomyces cerevisiae DL6-20, and Kluyveromyces lactis DY1-10. We investigated the potential probiotic properties of these strains and their use in cheese fermentation (cheeses designated CSP, CSM, CSS, and CSI, respectively); a control with no added yeast was designated CS. Read More

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Dynamics of the Degradation of Acetyl-CoA Carboxylase Herbicides in Vegetables.

Foods 2021 Feb 12;10(2). Epub 2021 Feb 12.

Department of Food Analysis and Nutrition, University of Chemistry and Technology Prague, 166 28 Prague, Czech Republic.

(1) Background: Aryloxyphenoxy-propionates and cyclohexanediones are herbicides most widely used in dicot crops worldwide. The main objective of the study was to determine the dynamics of herbicide residues in carrot, lettuce, cauliflower, and onion in order to suggest a low level of residues in harvested vegetables. (2) Methods: Small plot field trials were carried out in four vegetables in the Czech Republic. Read More

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February 2021

Antioxidant Activity and Bio-Accessibility of Polyphenols in Black Carrot ( L. ssp. var. Alef.) and Two Derived Products during Simulated Gastrointestinal Digestion and Colonic Fermentation.

Foods 2021 Feb 19;10(2). Epub 2021 Feb 19.

Department of Food Science and Health, Andalusian Institute of Agricultural and Fisheries Research and 7 Training (IFAPA), Alameda del Obispo, Avda. Menéndez-Pidal, s/n, 14004 Córdoba, Spain.

Black carrot has been attracting increasing thanks to its high bioactive compound content. This study presents the polyphenol bio-accessibility of black carrot and two derived products (black carrot snack (BC snack) and black carrot seasoning (BC seasoning)) after in vitro gastrointestinal digestion and colonic fermentation. Additionally, antioxidant activity was measured by 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS), 1,1-diphenyl-2-picryl-hydrazyl (DPPH) and oxygen radical absorbance capacity (ORAC) assays. Read More

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February 2021

Volatile aroma compounds and bioactive compounds of hawthorn vinegar produced from hawthorn fruit (Crataegus tanacetifolia (lam.) pers.).

J Food Biochem 2021 Mar 2:e13676. Epub 2021 Mar 2.

Department of Food Processing, Egirdir Vocational School, Isparta University of Applied Science, Isparta, Turkey.

This study was aimed to produce of hawthorn vinegar to increase the usage area and consumability of the hawthorn fruit and benefit from its functional properties, and to reveal some bioactive compounds, occurred during vinegar production, the functional properties and the volatile compounds (VC). The results showed that the gallic acid was a prominent phenolic substance in both wine and vinegar, followed by the chlorogenic acid. The prominent VACs of the hawthorn vinegar were acetic acid, phenylacetic acid, acetoin, then, respectively, pentanoic acid, benzoic acid, (E)-isoeugenol, 2-cyclohexenone, propanoic acid, chavicol, and diethyl succinate. Read More

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Mechanisms for tissue-specific accumulation and phase I/II transformation of 6:2 fluorotelomer phosphate diester in earthworm (M. guillelmi).

Environ Int 2021 Jun 26;151:106451. Epub 2021 Feb 26.

Key Laboratory of Pollution Processes and Environmental Criteria, Ministry of Education, Tianjin Key Laboratory of Environmental Remediation and Pollution Control, College of Environmental Science and Engineering, Nankai University, Tianjin 300350, PR China. Electronic address:

Polyfluoroalkyl phosphate esters (PAPs) are high production volume surfactants used in the food contact paper and packaging industries. They are prone to partition to soil due to their strong hydrophobicity and may biotransform into recalcitrant perfluoroalkyl carboxylic acids (PFCAs); little is known about their fate and behaviors in terrestrial organisms. Here, geophagous earthworms (M. Read More

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In Vitro Antioxidation, Antihepatic Steatosis, and Anti-Inflammatory Effects of Ethyl Acetate Fraction from Auricularia nigricans (Agaricomycetes).

Int J Med Mushrooms 2021 ;23(2):43-56

Mushroom Research Centre, Institute of Biological Sciences, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia.

Nonalcoholic fatty liver disease (NAFLD) is currently one of the most common liver diseases worldwide. Lifestyle modifications through the diet are the mainstay of treatment. Auricularia nigricans is a popular edible mushroom known to possess medicinal properties. Read More

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January 2021

Metabolomic Markers of Southern Dietary Patterns in the Jackson Heart Study.

Mol Nutr Food Res 2021 Feb 25:e2000796. Epub 2021 Feb 25.

Division of Cardiology, Department of Medicine, Beth Israel Deaconess Medical Center, Boston, Massachusetts, USA.

Scope: New biomarkers are needed that are representative of dietary intake.

Methods And Results: We assess metabolites associated with Southern dietary patterns in 1401 Jackson Heart Study participants. Three dietary patterns are empirically derived using principal component analysis: meat and fast food, fish and vegetables, and starchy foods. Read More

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February 2021

The fate of anaerobic syntrophy in anaerobic digestion facing propionate and acetate accumulation.

Waste Manag 2021 Apr 19;124:128-135. Epub 2021 Feb 19.

School of Life, Jiangsu Normal University, Shanghai Road 101, 221116 Xuzhou, China. Electronic address:

How the acetate and propionate accumulation impact anaerobic syntrophy during methane formation is not well understood. To investigate such effect, continuous acetate (35 g/L), propionate (11.25 g/L) and bicarbonate (30 g/L) supplementation were used during mesophilic anaerobic digestion. Read More

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Urate Lowering With Combination Therapy in CKD: Reason for Optimism or Einstein's Definition of Insanity?

Am J Kidney Dis 2021 04 7;77(4):478-480. Epub 2021 Feb 7.

Division of Nephrology, Departments of Medicine and Epidemiology and Population Health, Stanford University School of Medicine, Stanford, California.

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Enantioselective effects of cyflumetofen on microbial community and related nitrogen cycle gene function in acid-soil.

Sci Total Environ 2021 Jun 27;771:144831. Epub 2021 Jan 27.

Key Laboratory of Entomology and Pest Control Engineering, College of Plant Protection, Southwest University, Chongqing, China; Academy of Agricultural Sciences, Southwest University, Chongqing, China; State Cultivation Base of Crop Stress Biology for Southern Mountainous Land of Southwest University, Southwest University, Chongqing, China. Electronic address:

Cyflumetofen (CYF) is a novel chiral acaricide widely used in commercial crops to control mites. The environmental risks exposed by CYF in the soil, especially at the enantiomer level, remain unclear. We found that the (+)-CYF enantiomer was preferentially degraded in acid-soil, resulting in (-)-CYF enrichment. Read More

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Synthesis, Molecular Docking and Biological Properties of Novel Thiazolo[4,5-b]pyridine Derivatives.

Acta Chim Slov 2020 Dec;67(4):1035-1043

The synthesis, anti-inflammatory and antioxidant properties of novel 5-hydroxy-7-methyl-3H-thiazolo[4,5-b]pyridin-2-one derivatives were discussed. Fused thiazolo[4,5-b]pyridin-2-ones were synthesized and modified at the N3, C5 and C6 positions of the main core in order to obtain the compounds with a satisfactory pharmacological profile. The synthesized compounds were preselected via molecular docking for further testing of their anti-inflammatory activity in vitro. Read More

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December 2020

The Protective Role of Butyrate against Obesity and Obesity-Related Diseases.

Molecules 2021 Jan 28;26(3). Epub 2021 Jan 28.

Department of Translational Medical Science, University of Naples Federico II, 80131 Naples, Italy.

Worldwide obesity is a public health concern that has reached pandemic levels. Obesity is the major predisposing factor to comorbidities, including type 2 diabetes, cardiovascular diseases, dyslipidemia, and non-alcoholic fatty liver disease. The common forms of obesity are multifactorial and derive from a complex interplay of environmental changes and the individual genetic predisposition. Read More

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January 2021

Rapid Structural Analysis of a Synthetic Non-canonical Amino Acid by Microcrystal Electron Diffraction.

Front Mol Biosci 2020 8;7:609999. Epub 2021 Jan 8.

School of Molecular Sciences, Arizona State University, Tempe, AZ, United States.

Structural characterization of small molecules is a crucial component of organic synthesis. In this work, we applied microcrystal electron diffraction (MicroED) to analyze the structure of the product of an enzymatic reaction that was intended to produce the unnatural amino acid 2,4-dihydroxyphenylalanine (24DHF). Characterization of our isolated product with nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry (MS) suggested that an isomer of 24DHF had been formed. Read More

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January 2021

Ex vivo fecal fermentation of human ileal fluid collected after raspberry consumption modifies (poly)phenolics and modulates genoprotective effects in colonic epithelial cells.

Redox Biol 2021 Apr 12;40:101862. Epub 2021 Jan 12.

Nutrition Innovation Centre for Food and Health, University of Ulster, Coleraine, Northern Ireland, UK. Electronic address:

Diets rich in fruit and vegetables are associated with a decreased incidence of colorectal cancer (CRC) due, in part, to the bioactive (poly)phenolic components and their microbiota-mediated metabolites. This study investigated how such compounds, derived from ingested raspberries in the gastrointestinal tract, may exert protective effects by reducing DNA damage. Ileal fluids collected pre- and post-consumption of 300 g of raspberries by ileostomists (n = 11) were subjected to 24 h ex vivo fermentation with fecal inoculum to simulate interaction with colonic microbiota. Read More

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Comparison of anesthesia effects between closedloop and openloop target controlled infusion of propofol using the bispectral index in abdominal surgery.

Zhong Nan Da Xue Xue Bao Yi Xue Ban 2020 Dec;45(12):1419-1424

Department of Anesthesiology, Beijing Hospital; National Center of Gerontology; Institute of Geriatric Medicine, Chinese Academy of Medical Sciences, Beijing 100730, China.

Objectives: Bispectral index (BIS) can reflect the depth of propofol sedation. This study aims to compare the anesthetic satisfaction, anesthetic dose, and hemodynamic changes between closed-loop target controlled infusion (CLTCI) and open-loop target controlled infusion (OLTCI) during abdominal surgery.

Methods: From December 2016 to December 2018, 70 patients undergoing abdominal surgery under general anesthesia were selected in Beijing Hospital, including 51 males and 19 females, at the age from 49 to 65 years old. Read More

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December 2020

Systematic Evaluations of Doxorubicin-Induced Toxicity in Rats Based on Metabolomics.

ACS Omega 2021 Jan 28;6(1):358-366. Epub 2020 Dec 28.

Department of Pharmacy, Jining No 1 People's Hospital, Jining Medical University, Jining 272000, China.

Doxorubicin (DOX) is widely used to treat solid tumors, but its use is limited by its severe cardiotoxicity, nephrotoxicity, hepatotoxicity, and neurotoxicity. Metabolomic studies on DOX-induced toxicity are mainly focused on alterations in the heart and kidney, but systematic research on multiple matrices (serum, heart, liver, brain, and kidney) is rare. Thus, in our study, gas chromatography-mass spectrometry analysis of main targeted tissues (serum, heart, liver, brain, and kidney) was used to systemically evaluate the toxicity of DOX. Read More

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January 2021