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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
Hussain Md Shahjalal et al.
Journal of molecular cell biology, 6(5), 394-408 (2014-06-28)
Human induced pluripotent stem (hiPS) cells are considered a potential source for the generation of insulin-producing pancreatic β-cells because of their differentiation capacity. In this study, we have developed a five-step xeno-free culture system to efficiently differentiate hiPS cells into
Pil H Lee et al.
Bioorganic & medicinal chemistry letters, 20(1), 69-73 (2009-12-08)
A multiple linear regression QSAR model was developed based on a set of 61 compounds with internally consistent permeability data measured across Franz cell. The data was normalized using a mean permeability value of a reference compound, 3-isobutyl-1-methylxanthine (IBMX). The
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
Shaojun Yang et al.
The Journal of pharmacology and experimental therapeutics, 352(3), 529-540 (2015-01-01)
Sepiapterin reductase (SPR) catalyzes the reduction of sepiapterin to dihydrobiopterin (BH2), the precursor for tetrahydrobiopterin (BH4), a cofactor critical for nitric oxide biosynthesis and alkylglycerol and aromatic amino acid metabolism. SPR also mediates chemical redox cycling, catalyzing one-electron reduction of
Xuejia Zhai et al.
Die Pharmazie, 68(1), 19-26 (2013-03-01)
Cytochrome P450 enzymes are responsible for the oxidative metabolism of most pharmaceutical compounds. A "cocktail" approach which employs simultaneous administration of a mixture of substrates of CYP enzymes was often used to assess the metabolic activity of multiple P450 forms
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
A Guerra et al.
European journal of medicinal chemistry, 45(3), 930-940 (2009-12-22)
A neural model based on a numerical molecular representation using CODES program to predict oral absorption of any structure is described. This model predicts both high and low-absorbed compounds with a global accuracy level of 74%. CODES/ANN methodology shows promising
Valentina L Kouznetsova et al.
Bioorganic & medicinal chemistry, 19(11), 3320-3340 (2011-05-17)
Organic anion transporter 1 (Oat1), first identified as NKT, is a multispecific transporter responsible for the handling of drugs and toxins in the kidney and choroid plexus, but its normal physiological role appears to be in small molecule metabolite regulation.
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
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
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
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
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
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
Kayo Yuminoki et al.
Journal of pharmaceutical sciences, 103(11), 3772-3781 (2014-09-12)
In this study, we reported the application of Povacoat®, a hydrophilic polyvinylalcohol copolymer, as a dispersion stabilizer of nanoparticles of poorly water-soluble compounds. In addition, the influence of aggregation of the nanoparticles on their solubility and oral absorption was studied.
Ren-ai Xu et al.
Pakistan journal of pharmaceutical sciences, 26(4), 813-817 (2013-07-03)
A "cocktail"of numerous probe drugs to assess the metabolic activity of the corresponding cytochrome P450 enzymes requires that there is no problem of interaction among them. Some interactions among probe drugs can appear and may affect the rate of biotransformation
John T Barr et al.
Drug metabolism and disposition: the biological fate of chemicals, 43(1), 34-41 (2014-10-19)
The mechanistic understanding of interactions between diet-derived substances and conventional medications in humans is nascent. Most investigations have examined cytochrome P450-mediated interactions. Interactions mediated by other phase I enzymes are understudied. Aldehyde oxidase (AO) is a phase I hydroxylase that
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
David Buttar et al.
Bioorganic & medicinal chemistry, 18(21), 7486-7496 (2010-09-28)
The displacement of probes that bind selectively to subdomains IIA or IIIA on human serum albumin (HSA) by competing compounds has been followed using fluorescence spectroscopy, and has therefore been used to assign a primary binding site for these compounds
Philip Reinoß et al.
Current biology : CB, 30(23), 4579-4593 (2020-09-26)
Locomotion requires energy, yet animals need to increase locomotion in order to find and consume food in energy-deprived states. While such energy homeostatic coordination suggests brain origin, whether the central melanocortin 4 receptor (Mc4r) system directly modulates locomotion through motor
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
Phedias Diamandis et al.
Nature chemical biology, 3(5), 268-273 (2007-04-10)
The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain cancer. However, the complete repertoire of signaling pathways that governs the
Wei Guo et al.
Environmental toxicology and pharmacology, 38(3), 901-912 (2014-12-03)
This study aimed to identify the specific cytochrome P450 (CYP450) enzymes involved in the metabolism of dipfluzine hydrochloride using the combination of a chemical inhibition study, a correlation analysis and a panel of recombinant rat CYP450 enzymes. The incubation of
Kim D Mooiman et al.
The Journal of pharmacy and pharmacology, 66(9), 1339-1346 (2014-04-16)
The aim of this study is to establish the inhibitory effects of 14 commonly used complementary and alternative medicines (CAM) on the metabolism of cytochrome P450 2C9 (CYP2C9) substrates 7-methoxy-4-trifluoromethyl coumarine (MFC) and tolbutamide. CYP2C9 is important for the metabolism
Xiwei Zheng et al.
Journal of chromatography. A, 1371, 82-89 (2014-12-03)
Ultrafast affinity extraction and a multi-dimensional affinity system were developed for measuring free drug fractions at therapeutic levels. This approach was used to compare the free fractions and global affinity constants of several sulfonylurea drugs in the presence of normal
Yi Huang et al.
Pharmaceutical biology, 52(6), 681-687 (2014-05-16)
Alismatis rhizome (RA) (Water Plantain Family, also called "Zexie" in Chinese), one of the commonly used components of traditional Chinese medicines, is derived from the dried rhizomes of Alisma orientalis (Sam.) Juzep. (Alismataceae). This study explores the RA influences on
Dipy M Vasa et al.
Journal of pharmaceutical sciences, 103(9), 2911-2923 (2014-05-16)
Fifteen model drugs were quenched from 3:1 (w/w) mixtures with polyethylene glycol 4000 (PEG4000). The resulting solids were characterized using powder X-ray diffraction (PXRD), analysis of pair distribution function-transformed PXRD data (where appropriate), hot-stage polarized light microscopy, and differential scanning
Y Abe et al.
Die Pharmazie, 70(1), 38-46 (2015-05-16)
Ritobegron, a selective β3-adrenoceptor agonist, is the prodrug of the active compound, KUC-7322. We investigated species differences in its metabolism in vitro and the potential for drug-drug interactions with ritobegron. In rat, dog, monkey, and human liver microsomes, ritobegron was
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 35(3), 493-500 (2006-12-30)
CYP51 fulfills an essential requirement for all cells, by catalyzing three sequential mono-oxidations within the cholesterol biosynthesis cascade. Inhibition of fungal CYP51 is used as a therapy for treating fungal infections, whereas inhibition of human CYP51 has been considered as
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