Read by QxMD icon Read


Fadzilah Adibah Abd Majid, Nur Syukriah Ab Rahman, Effendy Abd Wahid, Ain Nabihah Zainudin, Siti Nurazwa Zainol, Hassan Fahmi Ismail, Tet Soon Wong, K Vijaya Bhargava, Nirbhay Kumar Tiwari, Sanjeev Giri
Drug interaction of SynacinnTM polyherbal with known diabetic drugs is unknown. SynacinnTM contains standardized extracts of five herbal against gallic acid, curcumin, rosmarinic acid, catechin and andrographolide. SynacinnTM and its five standard markers were analysed for its possible interaction with CYP450 enzymes assay. This study was conducted using liquid chromatography-tandem mass spectroscopy (LC-MS/MS) using probe substrates using human liver microsomes against CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4(Midazolam) and CYP3A4 (Testosteron)...
March 13, 2018: Drug Metabolism Letters
Li Li, Bing Chen, Hongbin Yan, Yannan Zhao, Zhongzi Lou, Jianqiu Li, Baoquan Fu, Xingquan Zhu, Donald P McManus, Jianwu Dai, Wanzhong Jia
BACKGROUND: Hepatocyte-based metacestode culture is an attractive method to study alveolar echinococcosis (AE), but it is limited by the relatively short lifespan of cultured hepatocytes in maintaining their normal function. METHODOLOGY/PRINCIPAL FINDINGS: We describe a three-dimensional (3D) hepatic culture system developed from co-cultured hepatocytes and mesenchymal stem cells using a collagen scaffold to study the development of Echinococcus multilocularis larvae...
March 14, 2018: PLoS Neglected Tropical Diseases
Wasco Wruck, James Adjaye
Induced pluripotent stem cells (iPSCs) and human embryonic stem cells (hESCs) differentiated into hepatocyte-like cells (HLCs) provide a defined and renewable source of cells for drug screening, toxicology and regenerative medicine. We previously reprogrammed human fetal foreskin fibroblast cells (HFF1) into iPSCs employing an episomal plasmid-based integration-free approach, this iPSC-line and the hESC lines H1 and H9 were used to model hepatogenesis in vitro. Biochemical characterisation confirmed glycogen storage, ICG uptake and release, urea and bile acid production, as well as CYP3A4 activity...
March 13, 2018: Scientific Data
Molly M Lockart, Carlo A Rodriguez, William M Atkins, Michael K Bowman
Cytochrome P450 (CYP) monoxygenses utilize heme cofactors to catalyze oxidation reactions. They play a critical role in metabolism of many classes of drugs, are an attractive target for drug development, and mediate several prominent drug interactions. Many substrates and inhibitors alter the spin state of the ferric heme by displacing the heme's axial water ligand in the resting enzyme to yield a five-coordinate iron complex, or they replace the axial water to yield a nitrogen-ligated six-coordinate iron complex, which are traditionally assigned by UV-vis spectroscopy...
February 24, 2018: Journal of Inorganic Biochemistry
Jin-Jun Wu, Zhen-Zhen Guo, Yuan-Feng Zhu, Zhi-Jian Huang, Xia Gong, Yu-Huan Li, Wen-Jie Son, Xiao-Yan Li, Yan-Mei Lou, Li-Jun Zhu, Lin-Lin Lu, Zhong-Qiu Liu, Liang Liu
BACKGROUND: Fuzi, which is the processed lateral roots of Aconitum carmichaeli Debx. (Ranunculaceae), is a traditional herbal medicine that is well known for its excellent pharmacological effects and acute toxicity. Aconitum alkaloids are responsible for its pharmacological activity and toxicity. Although a large number of studies on Fuzi have been reported, no comprehensive review on its pharmacokinetics has yet been published. PURPOSE: This paper seeks to present a comprehensive review regarding the phytochemistry, pharmacokinetic features and toxicity of Fuzi...
March 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Jasmine L Gowarty, Jon D Herrington
A promising drug, palbociclib, received accelerated approval as a first line treatment when used with the aromatase inhibitor, letrozole, for postmenopausal women with hormone receptor positive advanced or metastatic breast cancer. We report a case of a patient who presented with febrile neutropenia, grade 3 stomatitis with lip swelling, periorbital edema, and transaminitis while on palbociclib and verapamil. Labs normalized upon discontinuation of verapamil and our patient was able to continue treatment with palbociclib and letrozole...
January 1, 2018: Journal of Oncology Pharmacy Practice
Sufeng Zhou, Mingxue Tao, Yuanyuan Wang, Lu Wang, Lijun Xie, Juan Chen, Yuqing Zhao, Yun Liu, Hongwen Zhang, Ning Ou, Guangji Wang, Feng Shao, Jiye Aa
1. The aim of this analysis was to explore the influence of CYP3A4*1G and CYP3A5*3 polymorphisms on the pharmacokinetics of tylerdipine in healthy Chinese subjects. 2. A total of 64 and 63 healthy Chinese subjects were included and identified as the genotypes of CYP3A4*1G and CYP3A5*3, respectively. Plasma samples were collected for up to 24 h post-dose to characterize the pharmacokinetic profile following single oral dose of the drug (5, 15, 20, 25, 30 mg). Plasma levels were measured by a high-performance liquid chromatography-mass spectrometry (LC-MS/MS)...
March 9, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Christopher MacLauchlin, Stephen E Schneider, Kara Keedy, Prabhavathi Fernandes, Brian D Jamieson
Solithromycin, a novel macrolide and the first fluoroketolide, is being developed as a therapy for community-acquired bacterial pneumonia, with a distinct mechanism that provides activity against macrolide-resistant bacteria. The pharmacokinetics, metabolism, and excretion of solithromycin, were studied in healthy male subjects after oral administration of a single 800 mg (∼100 μCi) dose of [14 C]solithromycin. Solithromycin was well tolerated and absorption from the solution occurred with a median time to peak concentration of 4...
March 5, 2018: Antimicrobial Agents and Chemotherapy
David E Moody, Yueqiao Fu, Wenfang B Fang
The purpose of this study was to test the hypothesis that skeletal muscle relaxants could inhibit the in vitro metabolism of common co-medications opioids buprenorphine, methadone and oxycodone. The compounds (solubility-limited concentration (μM) studied) were: baclofen (1000), carisoprodol (200), its metabolite meprobamate (1000), chlorzoxazone (200), cyclobenzaprine (1000), metaxalone (50), methocarbamol (1000), orphenadrine (1000) and tizanidine (1000). Compounds were first incubated with human liver microsomes (HLM) ± pre-incubation, screened with pathway-specific cDNA-expressed cytochrome P450s (rCYP), and then IC50 values determined using either 8-concentration tests for those where the rCYP screen suggested an IC50 was achievable, or a 3-concentration test with downward extrapolation if screen suggested 50% inhibition was not achievable...
March 5, 2018: Basic & Clinical Pharmacology & Toxicology
P Riera, J Salazar, A Virgili, M Tobeña, A Sebio, P Gallano, A Barnadas, D Páez
AIM: Severe irinotecan-induced toxicity is associated with UGT1A1 polymorphisms. However, some patients develop side-effects despite harbouring a normal UGT1A1 genotype. As CYP3A4 is also an irinotecan-metabolizing enzyme, our study aimed to elucidate the influence of the CYP3A4*20 loss-of-function allele in the toxicity profile of these patients. METHODS: Three-hundred and eight metastatic colorectal cancer patients treated with an irinotecan-containing chemotherapy were studied...
March 5, 2018: British Journal of Clinical Pharmacology
Nikhat Saba, Alpana Seal
Vinca alkaloids are chemotherapeutic agents used in the treatment of both pediatric and adult cancer patients. Cytochrome P450 3A5 (CYP3A5) is 9- to 14-fold more efficient at clearing vincristine than cytochrome P450 3A4 (CYP3A4) is. However, patients who express an inactive form of the polymorphic CYP3A5 enzyme suffer from severe neurotoxicity during vincristine treatment, resulting in chemotherapy failure. Previous studies have found that the addition of new features to the parent drug can enhance its binding affinity to tubulin manyfold and could therefore yield novel anticancer drugs...
March 4, 2018: Journal of Molecular Modeling
Jingwen Li, Peng Peng, Qi Mei, Shu Xia, Yijun Tian, Liya Hu, Yuan Chen
BACKGROUND: Single nucleotide polymorphisms (SNPs) in UGT2B7 C802T and CYP3A4*1G impact drug metabolism. This study aimed to investigate the impact of these SNPs on the efficacy of oxycontin for pain relief in cancer patients. METHODS: A total of 57 Han Chinese cancer patients (age range 20-70 years) who received oxycontin to ease pain for the first time were enrolled and divided into two groups (refractory group and remission group) according to pain relief. Peripheral blood samples were collected from each patient for sequencing analysis...
March 3, 2018: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
Chen Peng, Ying Ding, Xin Yi, Yupei Shen, Zhiqiang Dong, Limei Cao, Qiang Li, Haiyan Ren, Lin He, Daizhan Zhou, Xu Chen
PURPOSE: Ischemic stroke (IS) is one of the most common neurologic diseases and is the main cause of death and disability in the Chinese population. This retrospective cohort study was performed to elucidate the relationship between single nucleotide polymorphisms (SNPs) in cytochrome P450 genes and the therapeutic effect of atorvastatin. METHODS: A total of 192 cases of IS were enrolled in the study. All patients were treated with atorvastatin, and their lipid levels and proportions were measured...
February 27, 2018: Clinical Therapeutics
Dennis M Fisher, Peter Chang, D Russell Wada, Albert Dahan, Pamela P Palmer
BACKGROUND: Desirable product attributes for treatment of moderate-to-severe acute pain in many medically supervised settings are rapid onset and a route of administration not requiring intravenous access. The pharmacokinetic characteristics of sublingually administered tablets containing 15 or 30 µg of sufentanil are described. METHODS: Blood was sampled from healthy subjects (four studies, 122 subjects) and patients (seven studies, 944 patients). Studies in healthy subjects determined bioavailability, effect of inhibition of cytochrome P450 3A4, and the plasma concentration profile with single and hourly sublingual doses...
March 2, 2018: Anesthesiology
Isha Ranadive, Sonam Patel, Abhilasha Mhaske, Gowri Kumari Uggini, Isha Desai, Suresh Balakrishnan
Currently, scientists show keen interest in the drugs that inhibit multiple kinases, LDN193189, being an example. It combats certain cancers in vitro as well as in vivo, making it a prerequisite for researchers to study the toxic potential of this drug in animal models. As most of the drugs metabolized by liver cause hepatic injury, LDN193189-induced hepatotoxicity was examined using a teleost fish, Poecilia latipinna. As a prelude, calculation of LD50 showed a value of 95.22 mg/kg body weight and three doses were decided based on it for further evaluations...
March 2, 2018: Drug and Chemical Toxicology
Chun-Hua Zhou, Meng Xu, Hai-Bing Yu, Xiao-Ting Zheng, Zhang-Feng Zhong, Lan-Tong Zhang
Nowadays, the Herb-drug combination is becoming increasingly popular in China. However, the possible interaction induced by their combination was examined rarely. The aim of this study was to investigate the effect of multi-dose administration of Danshen capsules on clopidogrel pharmacokinetics and pharmacodynamics in healthy volunteers. A sequential, open-label, and two-period pharmacokinetic drug interaction study was designed to compare clopidogrel pharmacokinetic parameters before and after 7 days of administration of Danshen capsules in twenty healthy male volunteers...
February 26, 2018: Food and Chemical Toxicology
Zhao-Yan Zhang, Liang Yang, Xiao-Yan Huang, Mei-Xi Wang, Zeng-Chun Ma, Xiang-Lin Tang, Yu-Guang Wang, Yue Gao
The rapid screening technology was used to investigate the transcriptional regulation effect of main chemical constituents in tubers of Polygonum multiflorum, including 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucopyranoside(THSG) and anthraquinones (such as rhein, chrysophanol, aloe-emodin, emodin) on CYP3A4 drug inducers induced by human pregnancy X receptor (PXR).The effect of chemical composition on the cell activity was detected by MTS cell viability assay. IC₅₀ was calculated. The expression vector and the reporter vector were co-transfected into HepG2 cells, with 10 μmol•L⁻¹ rifampicin (RIF) as a positive control, and 10 μmol•L⁻¹ ketoconazole (TKZ) as a negative control...
December 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Fawzy Elbarbry, Aimy Ung, Khaled Abdelkawy
Background: Quercetin (QR) and thymoquinone (TQ) are herbal remedies that are currently extensively used by the general population to prevent and treat various chronic conditions. Therefore, investigating the potential of pharmacokinetic interactions caused by the concomitant use of these herbal remedies and conventional medicine is warranted to ensure patient safety. Purpose of the Study: This study was conducted to determine the inhibitory effect of QR and TQ, two commonly used remedies, on the activities of selected cytochrome P450 (CYP) enzymes that play an important role in drug metabolism and/or toxicology...
January 2018: Pharmacognosy Magazine
Łucja Fiszer-Maliszewska, Łukasz Łaczmański, Aneta Dolińska, Maria Jagas, Ewelina Kołodziejska, Magdalena Jankowska, Piotr Kuśnierczyk
BACKGROUND/AIM: Ovarian cancer is a lethal gynecological malignancy, with 5-year survival of only about one third of patients. The ABCB1 gene encodes the P-glycoprotein which is one of the multidrug efflux pumps. Its decreased activity may result in multidrug resistance of cancer cells. Drug-metabolizing enzymes Cyp3A4 and Cyp3A5 may affect success of chemotherapy. In this study we attempted to examine the effects of 12 single nucleotide polymorphisms (SNPs) of the ABCB1 gene and one SNP in each of CYP3A4 and CYP3A5 genes on the incidence of ovarian cancer in Polish women and their response to treatment...
March 2018: Anticancer Research
Caroline A Lee, Chun Yang, Vishal Shah, Zancong Shen, David M Wilson, Traci M Ostertag, Jesse Hall, Jean-Luc Girardet, Michael Gillen
Following a single oral solution of 10 mg dose of [14C]verinurad (500 μCi), verinurad was rapidly absorbed with a median Tmax of 0.5 hour and terminal half-life of 15 hours. In human plasma, verinurad constituted 21% of total radioactivity. The majority of circulating radioactivity is associated with plasma with no preferential distribution of the drug to red blood cells. Recovery of radioactivity in urine and feces was 97.1%. Unchanged verinurad was the predominant component in the feces (29.9%) while levels were low in the urine (1...
February 28, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"