115,808 results match your criteria rats compounds

Novel strategy of cartilage repairing via application of P. atlantica with stem cells and collagen.

Artif Organs 2021 Jun 21. Epub 2021 Jun 21.

Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

Background: Osteoarthritis (OA) is an inflammatory joint condition, still lacking effective treatments. Some factors consider as the main causes of OA, including biochemical, mechanical, and genetic factors. The growth of studies confirmed that modern medicine in combination with folk medicine regarding the arrival of reliable, efficient, and safe therapeutic products against OA. Read More

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Xanthine oxidase inhibitory activity of Euphorbia peplus L. phenolics.

Comb Chem High Throughput Screen 2021 Jun 8. Epub 2021 Jun 8.

Department of Pharmacology and Toxicology, College of Pharmacy, Taif University, Taif, Saudi Arabia.

Background: Various phenolics show inhibitory activity towards xanthine oxidase (XO), an enzyme that generates reactive oxygen species which cause oxidative damage.

Objective: This study investigated the XO inhibitory activity of Euphorbia peplus phenolics.

Methods: The dried powdered aerial parts of E. Read More

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Evaluation of antidiabetic activity of dietary phenolic compound chlorogenic acid in streptozotocin induced diabetic rats: Molecular docking, molecular dynamics, in silico toxicity, in vitro and in vivo studies.

Comput Biol Med 2021 May 2;134:104462. Epub 2021 May 2.

Department of Biochemistry, University of Allahabad, Prayagraj, 211002, India. Electronic address:

Background: Chlorogenic acid is amongst the well-known polyphenolic compounds being used in human food and beverages. Its presence has been reported in tea leaves, roasted green beans, coffee, cocoa, berry fruits, apples, citrus fruits, and pears.

Objective: The present study aims to elucidate the effectiveness of chlorogenic acid on in silico and in vitro inhibition of glucose metabolising enzymes (α-amylase and α-glucosidase) and on blood-based markers associated with diabetic complications in vivo. Read More

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Metabolite profiling of Shuganzhi tablets in rats and pharmacokinetics study of four bioactive compounds with liquid chromatography combined with electrospray ionization tandem mass spectrometry.

J Chromatogr B Analyt Technol Biomed Life Sci 2021 Jun 12;1179:122827. Epub 2021 Jun 12.

Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.

Shuganzhi Tablets (SGZT) is developed on the basis of a clinical empirical formula as a hospital preparation for the treatment of fatty liver. In this study, a rapid and highly sensitive LC-MS/MS method was established and validated for simultaneous determination of ginsenoside Re, ginsenoside Rg1, notoginsenoside R1, naringin, specnuezhenide, emodin, polydatin, hesperidin and saikosaponin A in rat plasma. Multiple reaction monitoring mode played an important role in simultaneous quantitative analysis of multiple components. Read More

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Synthesis and Characterization of a Series of Temozolomide Esters and Its Anti-glioma Study.

J Pharm Sci 2021 Jun 17. Epub 2021 Jun 17.

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, P.R. China.

Temozolomide is a first-line therapeutic drug for glioblastoma (GBM), and it has a low solubility, short biological half-life, and resistance to drug limits in clinical applications. Therefore, it is necessary to find more effective anti-tumor drugs to overcome drug resistance and enhance its anti-glioma activity. We therefore used n-butanol, n-hexanol, n-octanol, 1-dodecanol and 1-hexadecanol to synthesize a series of temozolomide ester compounds (TMZEs) and then investigated their physicochemical properties and anti-glioma efficacy. Read More

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Ameliorative effect of Annona reticulata L. leaf extract on antihyperglycemic activity and its hepato-renal protective potential in streptozotocin induced diabetic rats.

J Ayurveda Integr Med 2021 Jun 16. Epub 2021 Jun 16.

Department of Biotechnology, Dravidian University, Kuppam, 517 426, A.P, India. Electronic address:

Background: Annona reticulata L. is a traditionally important plant due to its versatile source of medicine and industrial products. It is used to treat cardiac problems, wound healing, diabetes, ulcers and bacterial infections. Read More

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Herbal Formulation Comprised of Methanol Extracts of Tribulus terristris L. and Zingiber officinale Roscoe Has Antihypertensive Effects.

Altern Ther Health Med 2021 Jun 18. Epub 2021 Jun 18.

People prefer to use medicinal plants rather than chemical compounds because they are low cost and have fewer adverse events. Zingiber officinale Roscoe is a natural dietary rhizome with anti-oxidative, anti-inflammatory and anti-carcinogenic properties. Tribulus terrestris L. Read More

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Preclinical safety assessment of the crude extract from Sida rhombifolia L. aerial parts in experimental models of acute and repeated-dose 28 days toxicity in rats.

Regul Toxicol Pharmacol 2021 Jun 14:104974. Epub 2021 Jun 14.

Universidade Federal de Santa Maria, Santa Maria, RS, Brazil.

Sida rhombifolia (Malvaceae) is popularly used as a treatment for several pathological conditions; however, there is a lack of studies that identify its compounds and that evaluate comprehensively the safety of its consumption. Therefore, the aim of this study was to determinate the phytochemical constitution of the crude extract of Sida rhombifolia (CESR), and its safety in models of acute and repeated doses (28 days) toxicity. The tested dose for the model of acute toxicity was 2000 mg/kg doses for the repeated dose model were 150, 300 e 600 mg/kg. Read More

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Differences in hydrolase activities in the liver and small intestine between marmosets and humans.

Drug Metab Dispos 2021 Jun 16. Epub 2021 Jun 16.

Faculty of Pharmaceutical Sciences, Kanazawa University, Japan.

For drug development, species differences in drug-metabolism reactions present obstacles for predicting pharmacokinetics in humans. We characterized the species differences in hydrolases among humans and mice, rats, dogs, and cynomolgusmonkeys. In this study, to expand the series of such studies, we attempted to characterize marmoset hydrolases. Read More

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Generation of High-Quality Pharmacokinetic Data from Parallel Tail Vein Dosing and Bleeding in Non-cannulated Rats.

J Pharm Sci 2021 Jun 11. Epub 2021 Jun 11.

DMPK, Research and Early Development, Oncology R&D, AstraZeneca, Boston, US. Electronic address:

It is common practice to use cannulated rats for pharmacokinetic (PK) in-life studies as it yields high quality PK parameter estimation. While offering many benefits, cannulation requires surgery, post-surgical care, and cannula maintenance. As an alternative approach, the strategy of dosing and bleeding rats via the tail vein in a single experiment is technically feasible and theoretically offers many benefits. Read More

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Metabolism and Tissue Distribution of Chelerythrine and Effects of Extracts on Liver NAD(P)H Quinone Oxidoreductase.

Front Vet Sci 2021 26;8:659771. Epub 2021 May 26.

College of Veterinary Medicine, Hunan Agricultural University, Changsha, China.

is listed as a feed additive in animal production by the European Food Authority. The metabolites of chelerythrine in rats were measured by rapid and accurate high-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry (HPLC/QqTOF-MS). The structures of CHE metabolites were elucidated by comparing their changes in accurate molecular masses and fragment ions with those of parent ion or metabolite. Read More

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A Study of the Identification, Fragmentation Mode and Metabolic Pathways of Imatinib in Rats Using UHPLC-Q-TOF-MS/MS.

J Anal Methods Chem 2021 24;2021:8434204. Epub 2021 May 24.

Department of Pharmacology, School of Pharmacy, China Medical University, Shenyang 110122, China.

In this study, The metabolites, metabolic pathways, and metabolic fragmentation mode of a tyrosine kinase inhibitor- (TKI-) imatinib in rats were investigated. The samples for analysis were pretreated via solid-phase extraction, and the metabolism of imatinib in rats was studied using ultra-high-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS). Eighteen imatinib metabolites were identified in rat plasma, 21 in bile, 18 in urine, and 12 in feces. Read More

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Triazine Derivative as Putative Candidate for the Reduction of Hormone-Positive Breast Tumor: , Pharmacological, and Toxicological Approach.

Front Pharmacol 2021 28;12:686614. Epub 2021 May 28.

Department of Pharmacy, COMSAT University, Abbottabad, Pakistan.

Breast cancer is a heterogeneous disease that poses the highest incidence of morbidity among women and presents many treatment challenges. In search of novel breast cancer therapies, several triazine derivatives have been developed for their potential chemotherapeutic activity. This study aims to evaluate the N-nitroso-N-methyl urea (NMU)-induced anti-mammary gland tumor activity of 2,4,6 (O-nitrophenyl amino) 1,3,5-triazine (O-NPAT). Read More

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Neuroprotective effect of aspirin combined with ginkgolide injection on cerebral ischemic stroke rats and its effect on ERK12 signal pathway.

Saudi J Biol Sci 2021 Jun 15;28(6):3193-3197. Epub 2021 Apr 15.

Department of Emergency, Yantaishan Hospital, Yantai 264000, China.

The main aim of this study was to evaluate the neuroprotective effect of aspirin combined with ginkgolide injection on cerebral ischemic stroke model rats and its effect on extracellular regulated protein kinase 1/2 (REK1/2) signaling pathway, and to clarify the possible mechanism of aspirin combined with ginkgolide injection on neuroprotective mechanism. Experimental rats were randomly divided into sham group, model group, aspirin group, ginkgolide group and combination group (aspirin + ginkgolide injection) (n = 20). The results revealed scores of neurological dysfunction and infarct volume in aspirin group, ginkgolide group and combination group rats were lower than those in model group ( < 0. Read More

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Cardioprotective properties of natural medicine in isoproterenol induced myocardial damage in the male Albino rats.

Saudi J Biol Sci 2021 Jun 20;28(6):3169-3175. Epub 2021 Apr 20.

Department of Pharmacology and Toxicology, College of Pharmacy, Prince Sattam bin Abdul Aziz University, Al Kharj, Saudi Arabia.

The main aim of this study is to investigate cardioprotective properties of natural medicine inmyocardial damage induced male Albino rats. The aqueous extractof was used for the determination of phenolic compounds and flavonoids. The amount of phenol (1. Read More

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Design, synthesis and biological evaluation of selective hybrid coumarin-thiazolidinedione aldose reductase-II inhibitors as potential antidiabetics.

Bioorg Chem 2021 Jun 4;114:104970. Epub 2021 Jun 4.

Department of Chemistry, Osmania University, Hyderabad (T.S) 500 007, India.

Thiazolidinediones (TZD), benzopyrans are the proven scaffolds for inhibiting Aldose reductase (ALR2) activity and their structural confluence with the retention of necessary fragments helped in designing a series of hybrid compounds 2-(5-cycloalkylidene-2,4-dioxothiazolidin-3-yl)-N-(2-oxo-2H-chromen-3-yl)acetamide (10a-n) for better ALR2 inhibition. The compounds were synthesized by treating substituted 3-(N-bromoacetyl amino)coumarins (9a-d) with potassium salt of 5-cyclo alkylidene-1,3-thiazolidine-2,4-diones (4a-d). The inhibition activity against ALR2 with IC values range from 0. Read More

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Evaluation of carbon-11 labeled 5-(1-methyl-1H-pyrazol-4-yl)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)nicotinamide as PET tracer for imaging of CSF-1R expression in the brain.

Bioorg Med Chem 2021 May 30;42:116245. Epub 2021 May 30.

Stanford University, School of Medicine, Department of Radiology, Molecular Imaging Program at Stanford (MIPS), 1201 Welch Road, PS049, Stanford, CA 94305-5484, USA. Electronic address:

Pharmacological targeting of tumor associated macrophages and microglia in the tumor microenvironment is a novel therapeutic strategy in the treatment of glioblastoma multiforme. As such, the colony stimulating factor-1 receptor (CSF-1R) has been identified as a druggable target. However, no validated companion diagnostic marker for these therapies exists to date. Read More

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Calcitriol attenuates the cytotoxicity induced by aluminium phosphide via inhibiting mitochondrial dysfunction and oxidative stress in rat isolated cardiomyocytes.

Pestic Biochem Physiol 2021 Jul 24;176:104883. Epub 2021 May 24.

School of paramedical, Kermanshah University of Medical Sciences, Kermanshah, Iran.

These days, poisoning with aluminium phosphide (AlP), is one of the main health threats in human societies. Previous studies have been reported that cardiotoxicity induced by AlP, via mitochondrial dysfunction and oxidative stress is the main cause of death in victims. On the other, collectively, multiple lines of evidence strongly suggest that calcitriol has mitochondrial protective and antioxidant effects. Read More

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Beneficial effect of the methanolic leaf extract of Allium hookeri on stimulating glutathione biosynthesis and preventing impaired glucose metabolism in type 2 diabetes.

Arch Biochem Biophys 2021 Sep 10;708:108961. Epub 2021 Jun 10.

Chemical Biology Lab 1, Institute of Advanced Study in Science and Technology (IASST) Paschim Boragaon, Guwahati, 35, India; Assam Down Town University, Panikhaiti, Assam, 781068, India. Electronic address:

Oxidative stress resulting from the depletion of glutathione (GSH) level plays a vital role in generating various degenerative diseases, including type 2 diabetes (T2D). We tested the hypothesis that depleted glutathione levels can be enhanced and the impaired glucose metabolism can be prevented by supplementing Allium hookeri, a herb rich in organosulfur compounds, in a High Fat (HF) diet-induced T2D Male Sprague Dawley rat model. The experimental rats were divided into three groups (n = 6), namely normal diet, high-fat diet, and high-fat diet treated with A. Read More

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September 2021

Species-Specific Urothelial Toxicity with an anti-HIV Non-Catalytic Site Integrase Inhibitor (NCINI) is Related to Unusual pH-Dependent Physicochemical Changes.

Toxicol Sci 2021 Jun 12. Epub 2021 Jun 12.

Nonclinical Safety & Pathobiology, Gilead Sciences, Inc, Foster City, USA.

GS-9695 and GS-9822 are next generation Non-Catalytic Site Integrase Inhibitors (NCINIs) with significantly improved potency against HIV compared with previous drugs such as BI-224436. Development stopped due to vacuolation of the bladder urothelium seen in cynomolgus monkey but not in rat; this lesion was absent in equivalent preclinical studies with BI-224436 (tested in dog and rat). Lesions were unlikely to be attributable to target since NCINIs specifically target viral integrase protein and no mammalian homologue is known. Read More

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Biosynthesis of gold nanoparticles for the treatment of osteoarthritis alone or in combination with Diacerein in a rat model.

Inflammopharmacology 2021 Jun 11. Epub 2021 Jun 11.

Department of Food Toxicology and Contaminants, National Research Center, Dokki, Cairo, Egypt.

Gold (Au) compounds were used as an effective therapeutic agent for various inflammatory diseases; however, the use of Au compounds becomes limited because of its association with several side effects. Hence, gold nanoparticles (AuNPs) were developed as a new option for the medical proposes. However, the safety evaluation of gold nanoparticles (AuNPs) in osteoarthritis (OA) treatment remains vague. Read More

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Exploring the systemic delivery of a poorly water-soluble model drug to the retina using PLGA nanoparticles.

Eur J Pharm Sci 2021 Jun 8:105905. Epub 2021 Jun 8.

Institute of Medical Psychology, Medical Faculty, Otto-von-Guericke University Magdeburg, Leipziger Str. 44, 39120 Magdeburg, Germany; Clinic of Neurology with Institute of Translational Neurology, University Clinic Muenster, Mendel Str. 7, 48149 Muenster, Germany.

During the drug development process, many pharmacologically active compounds are discarded because of poor water solubility, but nanoparticle-based formulations are increasingly proposed as a solution for this problem. We therefore studied the distribution of nanoparticulate carriers and the delivery of their poorly water-soluble cargo to a structure of the central nervous system, the retina, under naive and pathological conditions. The lipophilic fluorescent dye coumarin 6 (Cou6) was encapsulated into poly(lactic-co-glycolic acid) PLGA nanoparticles (NPs). Read More

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Olive Leaf Powder Modulate Insulin Production and Circulating Adipokines in Streptozotocin Induced Diabetic Rats.

J Diet Suppl 2021 Jun 11:1-16. Epub 2021 Jun 11.

National Research Center, Cairo, Egypt.

Olives () have natural phytochemical compounds that are of great importance for their potential beneficially health effects. This study aimed to evaluate the effects of olive leaf powder (OLP) on insulin production and circulating adipokines in streptozotocin-induced diabetic rats. Forty Wistar-albino male rats, weighing 200-225 g were divided into four groups ( = 10); group I: Normal healthy rats received balanced diet; group II: Diabetic control rats receiving balanced diet; group III: Diabetic rats receiving balanced diet + standard antidiabetic drugs (metformin, 600 mg/bw) and group four: Diabetic rats received diet supplemented with 2. Read More

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Relevant essential oil components: a minireview on increasing applications and potential toxicity.

Toxicol Mech Methods 2021 Jun 10:1-27. Epub 2021 Jun 10.

Laboratory of Toxicology, Faculty of Pharmacy, Universitat de València. Av. Vicent Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain.

Phenolic compounds carvacrol, thymol, eugenol and vanillin are four of the most thoroughly investigated essential oil components given their relevant biological properties. These compounds are generally considered safe for consumption and have been used in a wide range of food and non-food applications. Significant biological properties, including antimicrobial, antioxidant, analgesic, anti-inflammatory, anti-mutagenic or anti-carcinogenic activity, have been described for these components. Read More

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HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor.

Eur J Med Chem 2021 May 29;222:113560. Epub 2021 May 29.

Pharmacological and Drug Safety Research, Gedeon Richter Plc., Budapest, Hungary.

HTS campaign of the corporate compound collection resulted in a novel, oxalic acid diamide scaffold of α7 nACh receptor positive allosteric modulators. During the hit expansion, several derivatives, such as 4, 11, 17 demonstrated not only high in vitro potency, but also in vivo efficacy in the mouse place recognition test. The advanced hit molecule 11 was further optimized by the elimination of the putatively mutagenic aromatic-amine building block that resulted in a novel, aminomethylindole compound family. Read More

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Pharmacokinetics, Tissue distribution and excretion of five rhubarb anthraquinones in rats after oral administration of effective fraction of anthraquinones from rheum officinale.

Xenobiotica 2021 Jun 10:1-32. Epub 2021 Jun 10.

Academy of Chinese Medical Sciences, Henan University of Chinese Medicine, Zhengzhou, 450046, China.

Rhubarb, a famous traditional Chinese medicine, shows a wide range of physiological activities and pharmacological benefits. Rhubarb anthraquinones are perceived as the pharmacologically active compounds of Rhubarb, and understanding metabolism of them is crucial to assure safety and effectiveness of clinical application. In this study, the pharmacokinetics, tissue distribution and excretion of five rhubarb anthraquinones (aloe-emodin, rhein, emodin, chrysophanol, physcion) were systematically investigated after oral administration of rhubarb extract to rats. Read More

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[The Comparison of Iron Deficiency Anemia Rat Treated with Hydroxypropyl Chitosan Ferrous Ion Complex and Ferrous Sulfate].

Zhongguo Shi Yan Xue Ye Xue Za Zhi 2021 Jun;29(3):853-859

Medical Center of Children, Affiliated Hospital of Guangdong Medical University, Zhanjiang 524000, Guangdong Province,

Objective: To observe and compare the therapeutic effects of hydroxypropyl chitosan ferrous ion complex solution and ferrous sulfate solution in iron deficiency anemia rats and their effects on gastric mucosa.

Methods: Seven rats were randomly selected from thirty five SPF grade SD rats as control group, and were fed with normal diet, distilled water (E). The rest of SD rats were fed with low iron feed and distilled water plus continuous tail vein bloodletting to establish the iron deficiency anemia model. Read More

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An integrated approach to uncover quality markers of stir-baking Semen Cuscuta with salt solution preventing recurrent spontaneous abortion based on chemical and metabolomic profiling.

J Chromatogr B Analyt Technol Biomed Life Sci 2021 Jul 11;1177:122727. Epub 2021 May 11.

Key Laboratory of Chinese Medicinal Formula of Anhui Province, Anhui University of Chinese Medicine, Hefei 230031, PR China; Anhui Province Key Laboratory of Traditional Chinese Medicine Decoction Pieces of New Manufacturing Technology, Bozhou 236800, PR China; Anhui Province Key Laboratory of Research & Development of Chinese Medicine, Hefei 230012, PR China. Electronic address:

The previous research of clinical big data mining showed that stir-baking Semen Cuscuta with salt solution (YP) ranked the first in the usage rate of treating abortion caused by kidney deficiency. At the same time, pharmacodynamic studies also showed that YP has better effect on improving recurrent spontaneous abortion (RSA) compared to raw products of Semen Cuscuta (SP). However, there were few studies on the biomarkers of YP improving RSA. Read More

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Feasibility of deuterium magnetic resonance spectroscopy of 3-O-Methylglucose at 7 Tesla.

PLoS One 2021 7;16(6):e0252935. Epub 2021 Jun 7.

Institute of Radiology, University Hospital Erlangen, Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU), Erlangen, Germany.

Deuterium Magnetic Resonance Spectroscopy (DMRS) is a non-invasive technique that allows the detection of deuterated compounds in vivo. DMRS has a large potential to analyze uptake, perfusion, washout or metabolism, since deuterium is a stable isotope and therefore does not decay during biologic processing of a deuterium labelled substance. Moreover, DMRS allows the distinction between different deuterated substances. Read More

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Prevention of tubulin/aldose reductase association delays the development of pathological complications in diabetic rats.

J Physiol Biochem 2021 Jun 7. Epub 2021 Jun 7.

Departamento de Biología Molecular, Facultad de Ciencias Exactas, Físico-Químicas y Naturales, Universidad Nacional de Río Cuarto, Río Cuarto, 5800, Córdoba, CP, Argentina.

In recent studies, we found that compounds derived from phenolic acids (CAFs) prevent the formation of the tubulin/aldose reductase complex and, consequently, may decrease the occurrence or delay the development of secondary pathologies associated with aldose reductase activation in diabetes mellitus. To verify this hypothesis, we determined the effect of CAFs on Na,K-ATPase tubulin-dependent activity in COS cells, ex vivo cataract formation in rat lenses and finally, to evaluate the antidiabetic effect of CAFs, diabetes mellitus was induced in Wistar rats, they were treated with different CAFs and four parameters were determinates: cataract formation, erythrocyte deformability, nephropathy and blood pressure. After confirming that CAFs are able to prevent the association between aldose reductase and tubulin, we found that treatment of diabetic rats with these compounds decreased membrane-associated acetylated tubulin, increased NKA activity, and thus reversed the development of four AR-activated complications of diabetes mellitus determined in this work. Read More

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