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Showing 1-30 of 119 results for "T0891" within Papers
Francisco J Prado-Prado et al.
Bioorganic & medicinal chemistry, 18(6), 2225-2231 (2010-02-27)
There are many of pathogen parasite species with different susceptibility profile to antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one parasite species. Consequently, predicting the probability with which a drug is active against
Aurelie Vivares et al.
Xenobiotica; the fate of foreign compounds in biological systems, 45(1), 29-44 (2014-07-30)
1. The quantitative prediction of the pharmacokinetic parameters of a drug from data obtained using human in vitro systems remains a significant challenge i.e. prediction of metabolic clearance in humans and estimation of the relative contribution of enzymes involved in
T Marras-Marquez et al.
International journal of pharmaceutics, 479(2), 265-276 (2014-12-30)
Pectin-based resistant, interactive and versatile hydrogel vehicles for oral administration have been prepared. These systems are thought to be versatile enough to allow the inclusion of substances (such as the surfactants tested: Pluronic, Tween, Na Lauryl sulphate) that may contribute
Izumi Yamasaki et al.
Biomedical research (Tokyo, Japan), 33(4), 235-242 (2012-09-15)
Kale (Brassica oleracea L. var acephala DC) is a leafy green vegetable belonging to the cabbage family (Brassicaceae) that contains a large amount of health-promoting phytochemicals. There are any reports about the effects of kale ingestion on the chemoprevention function
Nigel Greene et al.
Chemical research in toxicology, 23(7), 1215-1222 (2010-06-18)
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential
Jingwen Gao et al.
Journal of ethnopharmacology, 145(2), 566-572 (2012-12-05)
Cooked rhubarb and wine processed rhubarb are the processed rhubarbs of raw rhizomes from Rheum palmatum L., Rheum tanguticum Maxim. ex Balf. or Rheum officinale Baill. They are clinically used in traditional Chinese medicine to compose anti-diabetic formulas and remove
Jeffrey C Davis et al.
Cell reports, 31(6), 107623-107623 (2020-05-14)
Stem cell-derived β (SC-β) cells could provide unlimited human β cells toward a curative diabetes treatment. Differentiation of SC-β cells yields transplantable islets that secrete insulin in response to glucose challenges. Following transplantation into mice, SC-β cell function is comparable
Yu-Jin Guo et al.
Die Pharmazie, 69(4), 306-310 (2014-05-06)
Myricetin is one of the main ingredients of Chinese bayberry, which is used as a traditional medicine. The purpose of this study was to find out whether myricetin influences the rat cytochrome P450 (CYP) enzymes (CYP1A2, CYP2C9 and CYP3A4) by
Renli Teng et al.
International journal of clinical pharmacology and therapeutics, 51(4), 305-312 (2013-02-06)
To assess the effect of ticagrelor on the pharmacokinetics of tolbutamide (a CYP2C9 substrate), and the effect of tolbutamide on ticagrelor pharmacokinetics. In this randomized, double-blind, two-period, crossover study, 23 healthy volunteers received either placebo or ticagrelor 180 mg twice
Anne-Charlotte Dubbelman et al.
Journal of chromatography. A, 1374, 122-133 (2014-12-02)
The present study investigated the practical use of modern ultra-high performance liquid chromatography (UHPLC) separation techniques for drug metabolite profiling, aiming to develop a widely applicable, high-throughput, easy-to-use chromatographic method, with a high chromatographic resolution to accommodate simultaneous qualitative and
Ru Feng et al.
Phytomedicine : international journal of phytotherapy and phytopharmacology, 19(12), 1125-1133 (2012-07-24)
Halenia elliptica D. Don is a Tibetan herb and medicinal preparations containing Halenia elliptica have been commonly used for the treatment of hepatitis B virus infection in China. The metabolism of 1-hydroxy-2,3,5-trimethoxy-xanthone (HM-1) to its metabolites is mediated through cytochrome
Xi Huang et al.
PloS one, 9(11), e113819-e113819 (2014-11-27)
Meranzin hydrate (MH), an absorbed bioactive compound from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS), was first isolated in our laboratory and was found to possess anti-depression activity. However, the role of cytochrome P450s (CYPs) in the metabolism of MH
Mi Ran Choi et al.
Biopharmaceutics & drug disposition, 35(5), 264-274 (2014-03-05)
Under hyperlipidemic conditions, there are likely to be alterations in the pharmacokinetics of CYP2C11 substrates following decreased expression of CYP2C11, which is homologous to human CYP2C9. The pharmacokinetics of tolbutamide (TB) and its metabolite 4-hydroxy tolbutamide (4-OHTB) were evaluated as
Dong-Lou Liang et al.
Die Pharmazie, 69(4), 301-305 (2014-05-06)
The purpose of this study was to find out whether icaritin influences the effect on rat cytochrome P450 (CYP) enzymes (CYP1A2, CYP2C9, CYP2E1 and CYP3A4) using cocktail probe drugs in vivo. A cocktail solution at a dose of 5 mL/kg
Rajesh H Bahekar et al.
Bioorganic & medicinal chemistry, 15(21), 6782-6795 (2007-08-29)
In the present investigation, two series of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines (2a-l) and thieno[2,3-b]pyridines (3a-l) were designed as analogs of BL 11282 (1). The in vitro glucose dependent insulinotropic activity of all the test compounds was evaluated using RIN5F cell based assay and
Simona Bo et al.
European journal of endocrinology, 169(1), 117-126 (2013-05-11)
Available data about mortality of type 2 diabetic patients treated with different sulphonylureas are scarce and contradictory. We evaluated the associations between all-cause and cause-specific mortality and treatments with different sulphonylureas in a retrospective cohort of type 2 diabetic patients
Sang Yoon Lee et al.
Toxicology letters, 229(1), 33-40 (2014-06-10)
Although cytochrome P450 inhibition is the major drug-drug interaction (DDI) mechanism in clinical pharmacotherapy, DDI of a number of well-established drugs have not been investigated. Rifampicin, isoniazid, pyrazinamide and ethambutol combination therapy inhibits clearance of theophylline in patients with tuberculosis.
Xuelin Zhou et al.
Phytomedicine : international journal of phytotherapy and phytopharmacology, 20(3-4), 367-374 (2012-10-30)
Previous studies have shown that major tanshinones isolated from Danshen (Salvia miltiorrhiza) inhibited human and rat CYP450 enzymes-mediated metabolism of model probe substrates, with potential in causing herb-drug interactions. Miltirone, another abietane type-diterpene quinone isolated from Danshen, has been reported
Yuan Zhang et al.
Die Pharmazie, 70(1), 47-54 (2015-05-16)
Polygonum multiflorum is a traditional Chinese medicinal herb used in clinical medicine to nourish the liver and kidney. However, in recent years, there have been increased reports of clinical adverse reactions associated with Polygonum multiflorum preparations, especially due to liver
Rafael Gozalbes et al.
Bioorganic & medicinal chemistry, 18(19), 7078-7084 (2010-09-03)
Solubility plays a very important role in the selection of compounds for drug screening. In this context, a QSAR model was developed for predicting water solubility of drug-like compounds. First, a set of relevant parameters for establishing a drug-like chemical
Aysun Özdemİr et al.
Turkish journal of biology = Turk biyoloji dergisi, 45(1), 35-45 (2021-02-19)
In drug discovery, most small molecules cannot cross many stages, only a few can become drug candidates. Once the drug molecule is approved and marketed, nontarget effects that are not easily distinguishable from the actual target of the drugs might
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this
Manthena V S Varma et al.
Journal of medicinal chemistry, 52(15), 4844-4852 (2009-05-19)
Kidney plays an important role in the elimination of drugs, especially with low or negligible hepatic clearance. An analysis of the interrelation of physicochemical properties and the human renal clearance for a data set of 391 drugs or compounds tested
Therese Ericsson et al.
Xenobiotica; the fate of foreign compounds in biological systems, 44(7), 615-626 (2014-01-10)
1. Cytochrome P450 enzyme system is the most important contributor to oxidative metabolism of drugs. Modification, and more specifically inhibition, of this system is an important determinant of several drug-drug interactions (DDIs). 2. Effects of the antimalarial agent artemisinin and
Yan Liu et al.
Journal of chromatographic science, 51(1), 26-32 (2012-06-15)
A specific ultra-performance liquid chromatography tandem mass spectrometry method has been described for the simultaneous determination of caffeine, tolbutamide, metoprolol and dapsone in rat plasma, which are the four probe drugs of the four cytochrome P450 (CYP450) isoforms CYP1A2, CYP2C9
Zhiping Lin et al.
Die Pharmazie, 69(7), 537-541 (2014-07-31)
To investigate the influence of scutellarin on the activities of CYP1A2, CYP2C11, CYP2D1, and CYP3A1/2 in rats in vivo. Scutellarin and saline were intravenously administered to male Wistar rats via the caudal vein for 7 days consecutively. On the 8th
Meiling Ye et al.
Nanoscale research letters, 9(1), 642-642 (2014-12-19)
Nano-sized particles are known to interfere with drug-metabolizing cytochrome P450 (CYP) enzymes, which can be anticipated to be a potential source of unintended adverse reactions, but the mechanisms underlying the inhibition are still not well understood. Herein we report a
Xin-shuai Wang et al.
Phytotherapy research : PTR, 29(3), 366-372 (2014-12-03)
In traditional therapy with Chinese medicine, vitexin has several pharmacological properties, including antinociceptive, antispasmodic, antioxidant, antimyeloperoxidase, and α-glucosidase inhibitory activities. Recently, vitexin was shown to protect the heart against ischemia/reperfusion injury in an in vitro model by inhibiting apoptosis. The
Kazuo Takayama et al.
Journal of hepatology, 57(3), 628-636 (2012-06-05)
Hepatocyte-like cells differentiated from human embryonic stem cells (hESCs) and induced pluripotent stem cells (hiPSCs) can be utilized as a tool for screening for hepatotoxicity in the early phase of pharmaceutical development. We have recently reported that hepatic differentiation is
Haiyan Li et al.
European journal of medicinal chemistry, 44(4), 1600-1606 (2008-09-05)
The first-principle, quantitative structure-hepatic clearance relationship for 50 drugs was constructed based on selected molecular descriptors calculated by TSAR software. The R(2) of the predicted and observed hepatic clearance for the training set (n=36) and test set (n=13) were 0.85
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