Results 41 to 50 of about 23,100 (164)

Selection of Suitable Prodrug Candidates for in vivo Studies via in vitro Studies; The Correlation of Prodrug Stability in Between Cell Culture Homogenates and Human Tissue Homogenates

Journal of Pharmacy & Pharmaceutical Sciences, 2012
Purpose. To determine the correlations/discrepancies of drug stabilities between in the homogenates of human culture cells and of human tissues. Methods. Amino acid/dipeptide monoester prodrugs of floxuridine were chosen as the model drugs.
Yasuhiro Tsume, Gordon L Amidon
doaj   +1 more source

Biotransformation of 2,4,6-tris(2,4,6-tribromophenoxy)-1,3,5-triazine (TTBP-TAZ) can contribute to high levels of 2,4,6-tribromophenol (2,4,6-TBP) in humans

Environment International, 2022
2,4,6-Tribromophenol (2,4,6-TBP) is a brominated flame retardant that accumulates in human tissues and is a potential toxicant. Previous studies found 2,4,6-TBP levels in human tissues were significantly higher than those of brominated flame retardants ...
Guomao Zheng, Luma Melo, Rishika Chakraborty, James E. Klaunig, Amina Salamova   +4 more
doaj   +1 more source

Isoflavones modulate the glucuronidation of estradiol in human liver microsomes [PDF]

Carcinogenesis, 2005
Soy food has been associated with a reduced incidence of hormonal cancer in Asian countries, and the soy isoflavones daidzein and genistein are believed to protect against tumors induced by the endogenous hormone 17beta-estradiol (E2). In the present study, we have examined if daidzein and genistein as well as several structurally related isoflavones ...
Pfeiffer, E., Treilling, C., Hoehle, S., Metzler, M.   +3 more
openaire   +2 more sources

Identification of the metabolites of ivermectin in humans

Pharmacology Research & Perspectives, 2021
Mass drug administration of ivermectin has been proposed as a possible malaria elimination tool. Ivermectin exhibits a mosquito‐lethal effect well beyond its biological half‐life, suggesting the presence of active slowly eliminated metabolites.
Phornpimon Tipthara, Kevin C. Kobylinski, Markus Godejohann, Borimas Hanboonkunupakarn, Alison Roth, John H. Adams, Nicholas J. White, Podjanee Jittamala, Nicholas P. J. Day, Joel Tarning   +9 more
doaj   +1 more source

Studies on acyl-coenzyme A: cholesterol acyltransferase activity in human liver microsomes.

Journal of Lipid Research, 1989
The aim of the present study was to characterize the acyl-coenzyme A: cholesterol acyltransferase (ACAT) activity in human liver microsomes. Liver biopsies were obtained from patients undergoing elective cholecystectomy under highly standardized ...
K Einarsson, L Benthin, S Ewerth, G Hellers, D Ståhlberg, B Angelin   +5 more
doaj   +1 more source

Metabolic Profiling of the Uncaria Hook Alkaloid Geissoschizine Methyl Ether in Rat and Human Liver Microsomes Using High-Performance Liquid Chromatography with Tandem Mass Spectrometry

Molecules, 2015
Geissoschizine methyl ether (GM) is an indole alkaloid found in Uncaria hook, which is a galenical constituent of yokukansan, a traditional Japanese medicine. GM has been identified as the active component responsible for anti-aggressive effects. In this
Hirotaka Kushida, Takashi Matsumoto, Yasushi Igarashi, Hiroaki Nishimura, Junko Watanabe, Kazuya Maemura, Yoshio Kase   +6 more
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Preclinical metabolism and metabolic drug–drug interaction profile of pedunculoside and rotundic acid

Clinical and Translational Science
Pedunculoside and rotundic acid, the most abundant components in plants of the genus Ilex L. (Aquifoliaceae), exhibit biological and pharmacological significance in the treatment of cardiovascular diseases.
Liang Wu, Linling Dong, Zhu Zhou, Xin Wang, Yujie Lin, Xuesong Shi, Peijing Wang, Suocheng Xu, Zhiyi Fang   +8 more
doaj   +1 more source

In Vitro Inhibitory Effects of Scutellarin on Six Human/Rat Cytochrome P450 Enzymes and P-glycoprotein

Molecules, 2014
Inhibition of cytochrome P450 (CYP) and P-glycoprotein (P-gp) are regarded as the most frequent and clinically important pharmacokinetic causes among the various possible factors for drug-drug interactions. Scutellarin is a flavonoid which is widely used
Yong-Long Han, Dan Li, Quan-Jun Yang, Zhi-Yong Zhou, Li-Ya Liu, Bin Li, Jin Lu, Cheng Guo   +7 more
doaj   +1 more source

Metabolism and Metabolic Inhibition of Xanthotoxol in Human Liver Microsomes [PDF]

Evidence-Based Complementary and Alternative Medicine, 2016
Cytochrome p450 (CYP450) enzymes are predominantly involved in Phase I metabolism of xenobiotics. In this study, the CYP450 isoforms involved in xanthotoxol metabolism were identified using recombinant CYP450s. In addition, the inhibitory effects of xanthotoxol on eight CYP450 isoforms and its pharmacokinetic parameters were determined using human ...
Zhongnv Ma, Xianbao Shi, Gang Zhang, Feng Guo, Lina Shan, Jiqun Cai   +5 more
openaire   +3 more sources

Metabolism of (+)-Fenchone by CYP2A6 and CYP2B6 in Human Liver Microsomes

Biological and Pharmaceutical Bulletin, 2006
The in vitro metabolism of (+)-fenchone was examined in human liver microsomes and recombinant enzymes. Biotransformation of (+)-fenchone was investigated by gas chromatography-mass spectrometry. (+)-Fenchone was found to be oxidized to 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone and 10-hydroxyfenchone by human liver microsomal P450 enzymes.
Miyazawa, Mitsuo, Gyoubu, Kunihiko
openaire   +4 more sources