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Lovastatin

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https://www.readbyqxmd.com/read/29770527/assay-of-lovastatin-containing-dietary-supplement-by-lc-ms-ms-under-mrm-condition
#1
Leonardo Di Donna, Lucia Bartella, Anna Napoli, Giovanni Sindona, Fabio Mazzotti
Monacolin K, the active ingredient present in dietary supplement, is a nutraceutical whose health benefits have been widely documented. A fast approach for the assay of lovastatin in both form, lactone and acid, by mass spectrometry is presented. The quantitative assay is carried out by HPLC-MS/MS using the multiple reaction monitoring (MRM) mode and simvastatin and pravastatin as internal standards. The accuracy values ranged from 97 to 101%; the analytical parameters values of LOQ, LOD, recovery and reproducibility, were calculated analyzing fortified samples, confirming the reliability of the proposed approach...
May 16, 2018: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/29768081/unremarkable-impact-of-oatp-inhibition-on-the-liver-concentration-of-fluvastatin-lovastatin-and-pitavastatin-in-wild-type-and-oatp1a-1b-knockout-mouse
#2
Jae H Chang, Xiaolin Zhang, Kirsten Messick, Yi-Chen Chen, Eugene Chen, Jonathan Cheong, Justin Ly
1. OATP inhibitors have been shown to significantly increase the plasma exposure of statins. However, understanding alterations of liver concentration is also important. While modeling has simulated liver concentration changes, availability of experimental data is limited, especially when concerning drug-drug interactions (DDI). The objective of this work was to determine blood and liver concentrations of fluvastatin, lovastatin and pitavastatin, when blocking uptake transporters. 2. In wild-type mouse, rifampin pre-treatment decreased the unbound liver-to-plasma ratio (Kp,uu ) of fluvastatin by 4...
May 16, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29766796/biological-and-in-silico-studies-on-synthetic-analogues-of-tyrosine-betaine-as-inhibitors-of-neprilysin-a-drug-target-for-the-treatment-of-heart-failure
#3
Daniel Fabio Kawano, Marcelo Rodrigues de Carvalho, Mauricio Ferreira Marcondes Machado, Adriana Karaoglanovic Carmona, Gilberto Ubida Leite Braga, Ivone Carvalho
BACKGROUND: Fungal secondary metabolites are important sources for the discovery of new pharmaceuticals, as exemplified by penicillin, lovastatin and cyclosporine. Searching for secondary metabolites of the fungi Metarhizium ssp., we previously identified tyrosine betaine as a major constituent. METHODS: Because of the structural similarity with other inhibitors of neprilysin (NEP), an enzyme explored for the treatment of heart failure, we devised the synthesis of tyrosine betaine and three analogues to be subjected to in vitro NEP inhibition assays and to molecular modeling studies...
May 14, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29736804/influence-of-fatty-acid-modification-on-uptake-of-lovastatin-loaded-reconstituted-high-density-lipoprotein-by-foam-cells
#4
Yun Yang, Ji Wang, Hongliang He, Wenli Zhang, Yuansheng Zhang, Jianping Liu
PURPOSE: Spherical reconstituted high density lipoprotein (rHDL) can target atherosclerotic lesions by the very low density lipoprotein (VLDL) receptor, which is seldom expressed in liver. By promoting this pathway, the targeting efficiency was hyphothesized to be improved due to avoiding undesired uptake in liver mediated by the scavenger receptor class B type I (SR-BI). In this study, how fatty acid modification in spherical rHDL influenced the VLDL receptor-mediated endocytosis pathway was investigated...
May 7, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29727712/overexpression-of-acetyl-coa-carboxylase-in-aspergillus-terreus-to-increase-lovastatin-production
#5
Hanan Hasan, Muhammad Hafiz Abd Rahim, Leona Campbell, Dee Carter, Ali Abbas, Alejandro Montoya
The present work describes the application of homologous recombination techniques in a wild-type Aspergillus terreus (ATCC 20542) strain to increase the flow of precursors towards the lovastatin biosynthesis pathway. A new strain was generated to overexpress acetyl-CoA carboxylase (ACCase) by replacing the native ACCase promoter with a strong constitutive PadhA promoter from Aspergillus nidulans. Glycerol and a mixture of lactose and glycerol were used independently as the carbon feedstock to determine the degree of response by the A...
May 1, 2018: New Biotechnology
https://www.readbyqxmd.com/read/29723430/relationships-of-changes-in-pharmacokinetic-parameters-of-substrate-drugs-in-drug-drug-interactions-on-metabolizing-enzymes-and-transporters
#6
Shinji Yamazaki
A general objective of drug-drug interaction (DDI) studies is to determine whether potential interactions of new molecular entities with concomitantly administered other drugs exist and, if DDIs occur, whether dosage adjustments are required. A typical end point for DDI evaluations is the ratio of area under the plasma concentration-time curve (AUC) of substrate drugs (AUCR), whereas the ratios of maximal plasma concentration (Cmax ) and terminal half-life (t1/2 ) are also important to understand DDI mechanisms (Cmax R and t1/2 R, respectively)...
May 3, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29717011/statins-suppress-ebola-virus-infectivity-by-interfering-with-glycoprotein-processing
#7
Punya Shrivastava-Ranjan, Mike Flint, Éric Bergeron, Anita K McElroy, Payel Chatterjee, César G Albariño, Stuart T Nichol, Christina F Spiropoulou
Ebola virus (EBOV) infection is a major public health concern due to high fatality rates and limited effective treatments. Statins, widely used cholesterol-lowering drugs, have pleiotropic mechanisms of action and were suggested as potential adjunct therapy for Ebola virus disease (EVD) during the 2013-2016 outbreak in West Africa. Here, we evaluated the antiviral effects of statin (lovastatin) on EBOV infection in vitro Statin treatment decreased infectious EBOV production in primary human monocyte-derived macrophages and in the hepatic cell line Huh7...
May 1, 2018: MBio
https://www.readbyqxmd.com/read/29691631/lovastatin-synergizes-with-itraconazole-against-planktonic-cells-and-biofilms-of-candida-albicans-through-the-regulation-on-ergosterol-biosynthesis-pathway
#8
Yujie Zhou, Hong Yang, Xuedong Zhou, Hongke Luo, Fan Tang, Jin Yang, Gil Alterovitz, Lei Cheng, Biao Ren
The increase of fungal infectious diseases and lack of safe and efficacious antifungal drugs result in the urgent need of new therapeutic strategies. Here, we repurposed the lovastatin (LOV) as a synergistic antifungal potentiator to itraconazole (ITZ) against Candida albicans planktonic cells and biofilms in vitro for the first time. Mutants from ergosterol biosynthesis pathway were employed and key gene expression profiles of ergosterol pathway were also measured. LOV single treatment was unable to inhibit C...
April 25, 2018: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/29685507/the-effect-of-statin-use-and-intensity-on-stroke-and-myocardial-infarction-after-carotid-endarterectomy
#9
Nkiruka Arinze, Alik Farber, Teviah Sachs, Gregory Patts, Jeffrey Kalish, Angela Kuhnen, George Kasotakis, Jeffrey J Siracuse
OBJECTIVE: Statin use in patients with cerebrovascular disease undergoing carotid endarterectomy (CEA) has been advocated for prevention of stroke and cardiovascular events. However, the effect of statin therapy on long-term outcomes after CEA still needs to be delineated. METHODS: OptumLabs Data Warehouse, a comprehensive, longitudinal, real-world dataset with deidentified lives across claims and clinical information, was used to analyze the rates of stroke, myocardial infarction (MI), and statin use after CEA...
April 20, 2018: Journal of Vascular Surgery
https://www.readbyqxmd.com/read/29673993/dynamics-of-bacterial-composition-and-the-fate-of-antibiotic-resistance-genes-and-mobile-genetic-elements-during-the-co-composting-with-gentamicin-fermentation-residue-and-lovastatin-fermentation-residue
#10
Yuanwang Liu, Yao Feng, Dengmiao Cheng, Jianming Xue, Steven Wakelin, Zhaojun Li
Dynamics in bacterial community composition, along with 13 antibiotic resistance genes (ARGs) and eight mobile genetic elements (MGEs), were assessed during co-composting with gentamicin and lovastatin fermentation residue (GFR and LFR, respectively). Using next generation sequencing, the key bacterial taxa associated with the different stages of composting were identified. Most importantly, Bacillus, belonging to Phylum Firmicutes, was associated with enhanced degradation of gentamicin, decomposition of organic matter (OM) and dissolved organic carbon (DOC), and also extension of the thermophilic phase of the composting cycle...
April 5, 2018: Bioresource Technology
https://www.readbyqxmd.com/read/29623039/simvastatin-therapy-for-drug-repositioning-to-reduce-the-risk-of-prostate-cancer-mortality-in-patients-with-hyperlipidemia
#11
Yu-An Chen, Ying-Ju Lin, Cheng-Li Lin, Hwai-Jeng Lin, Hua-Shan Wu, Hui-Ying Hsu, Yu-Chen Sun, Hui-Yu Wu, Chih-Ho Lai, Chia-Hung Kao
Prostate cancer (PCa) is one of the most commonly diagnosed cancers in the western world, and the mortality rate from PCa in Asia has been increasing recently. Statins are potent inhibitors of 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase and are commonly used for treating hyperlipidemia, with beneficial effects for cardiovascular disease and they also exhibit anti-cancer activity. However, the protective effects of statins against PCa are controversial. In this study, we investigated the effect of two types of statins (simvastatin and lovastatin) and the mortality rate of PCa patients by using the Taiwan National Health Insurance Research Database (NHIRD)...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29609611/association-between-industry-payments-and-prescribing-costly-medications-an-observational-study-using-open-payments-and-medicare-part-d-data
#12
Manvi Sharma, Aisha Vadhariya, Michael L Johnson, Zachary A Marcum, Holly M Holmes
BACKGROUND: While many new medications may offer advantages over existing drugs, some newer drugs are reformulations of existing products that provide little innovation or incremental benefit while driving up drug costs. Despite the lack of benefit of these medications, prescribers may be motivated by payments made by the pharmaceutical industry. The objective of the study was to determine the association between payments made to physicians by the pharmaceutical industry and prescriptions for certain selected costly brand name drugs...
April 2, 2018: BMC Health Services Research
https://www.readbyqxmd.com/read/29607441/in-hospital-mortality-following-traumatic-brain-injury-among-older-medicare-beneficiaries-comparing-statin-users-with-nonusers
#13
Bilal Khokhar, Linda Simoni-Wastila, Julia F Slejko, Eleanor Perfetto, Min Zhan, Gordon S Smith
Background: Traumatic brain injury (TBI) is a significant public health concern for older adults. Small-scale human studies have suggested pre-TBI statin use is associated with decreased in-hospital mortality following TBI, highlighting the need for large-scale translational research. Objective: To investigate the relationship between pre-TBI statin use and in-hospital mortality following TBI. Methods: A retrospective study of Medicare beneficiaries 65 and older hospitalized with a TBI during 2006 to 2010 was conducted to assess the impact of pre-TBI statin use on in-hospital mortality following TBI...
December 2017: Journal of Pharmacy Technology: JPT: Official Publication of the Association of Pharmacy Technicians
https://www.readbyqxmd.com/read/29580713/effect-of-statin-therapy-on-plasma-apolipoprotein-ciii-concentrations-a-systematic-review-and-meta-analysis-of-randomized-controlled-trials
#14
Amirhossein Sahebkar, Luis E Simental-Mendía, Dimitri P Mikhailidis, Matteo Pirro, Maciej Banach, Cesare R Sirtori, Massimiliano Ruscica, Željko Reiner
BACKGROUND: Statins are well-established low-density lipoprotein cholesterol-lowering drugs. Elevated apolipoprotein CIII (Apo CIII) levels are associated with elevated triglyceride-rich particles, which are also considered to be a possible risk factor for cardiovascular disease. OBJECTIVE: The aim of this meta-analysis of randomized placebo-controlled clinical trials was to assess the effect of statins on Apo CIII concentrations. METHODS: Randomized placebo-controlled trials investigating the impact of statin treatment on cholesterol lowering that include lipoprotein measurement were searched in PubMed, MEDLINE, Scopus, Web of Science, and Google Scholar databases (up to July 31, 2017)...
February 1, 2018: Journal of Clinical Lipidology
https://www.readbyqxmd.com/read/29521223/effects-of-a-series-of-acidic-drugs-on-l-lactic-acid-transport-by-the-monocarboxylate-transporters-mct1-and-mct4
#15
Yat H Leung, Francois Belanger, Jennifer Lu, Jacques Turgeon, Veronique Michaud
BACKGROUND: Drug-induced myopathy is a serious side effect that often requires removal of a medication from a drug regimen. For most drugs, the underlying mechanism of drug-induced myopathy remains unclear. Monocarboxylate transporters (MCTs) mediate L-lactic acid transport, and inhibition of MCTs may potentially lead to perturbation of L-lactic acid accumulation and muscular disorders. Therefore, we hypothesized that L-lactic acid transport may be involved in the development of drug-induced myopathy...
2017: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/29515531/-nsg2-orf19-273-encoding-protein-controls-sensitivity-of-candida-albicans-to-azoles-through-regulating-the-synthesis-of-c14-methylated-sterols
#16
Quan-Zhen Lv, Yu-Lin Qin, Lan Yan, Liang Wang, Chuyue Zhang, Yuan-Ying Jiang
Antifungal azole drugs inhibit the synthesis of ergosterol and cause the accumulation of sterols containing a 14α-methyl group, which is related to the properties of cell membrane. Due to the frequent recurrence of fungal infections and clinical long-term prophylaxis, azole resistance is increasing rapidly. In our research, Nsg2p, encoded by the ORF19.273 in Candida albicans , is found to be involved in the inhibition of 14α-methylated sterols and resistance to azoles. Under the action of fluconazole, nsg2 Δ/Δ mutants are seriously damaged in the integrity and functions of cell membranes with a decrease of ergosterol ratio and an increase of both obtusifoliol and 14α-methylfecosterol ratio...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29502067/dual-effects-for-lovastatin-in-anaplastic-thyroid-cancer-the-pivotal-effect-of-transketolase-tkt-on-lovastatin-and-tumor-proliferation
#17
Chih-Yuan Wang, Hao-Ai Shui, Tien-Chun Chang
This study tested the hypothesis that the effects of lovastatin on anaplastic thyroid cancer cell growth are mediated by upregulation of transketolase (TKT) expression. The effects of lovastatin on TKT protein levels in ARO cells were determined using western blot and proteomic analyses. After treatment with lovastatin and oxythiamine, the in vitro and in vivo growth of ARO cells was determined using 3-(4,5-Dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assays and tumor xenografts in nude mice...
March 2, 2018: Journal of Investigative Medicine: the Official Publication of the American Federation for Clinical Research
https://www.readbyqxmd.com/read/29471671/cholesterol-enriched-membrane-microdomains-are-needed-for-insulin-signaling-and-proliferation-in-hepatic-cells
#18
Matheus de Castro Fonseca, Andressa França, Rodrigo Machado Florentino, Roberta Cristelli Fonseca, Antônio Carlos Melo, Paula Teixeira Vieira Vidigal, André G Oliveira, Laurent Dubuquoy, Michael H Nathanson, M Fátima Leite
Hepatocyte proliferation during liver regeneration is a well-coordinated process regulated by the activation of several growth factor receptors, including the insulin receptor (IR). The IR can be localized in part to cholesterol-enriched membrane microdomains, but the role of such domains in insulin-mediated events in hepatocytes is not known. We investigated whether partitioning of IRs into cholesterol-enriched membrane rafts is important for the mitogenic effects of insulin in the hepatic cells. IR and lipid rafts were labeled in HepG2 cells and primary rat hepatocytes...
February 22, 2018: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/29427912/adjunctive-therapy-with-statins-in-schizophrenia-patients-a-meta-analysis-and-implications
#19
Hong Shen, Rui Li, Rong Yan, Xia Zhou, Xia Feng, Mengjie Zhao, Hong Xiao
There are some conflicting results regarding the benefit of adjunctive therapy with statins for severity of negative symptoms in schizophrenia. This study aimed to verify whether statins use for adjunctive therapy was indeed beneficial to improve psychiatric symptoms in schizophrenia. The data were from CENTRAL, PubMed, Embase and MEDLINE. The Boolean search term used for the electronic database search was (statin OR simvastatin OR atorvastatin OR fluvastatin OR lovastatin OR mevastatin OR pitavastatin OR pravastatin OR rosuvastatin OR cerivastatin) and (schizophrenia OR schizoaffective disorder OR psychosis)...
April 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29427042/amyotrophic-lateral-sclerosis-associated-with-statin-use-a-disproportionality-analysis-of-the-fda-s-adverse-event-reporting-system
#20
Beatrice A Golomb, Abril Verden, Alexis K Messner, Hayley J Koslik, Keith B Hoffman
INTRODUCTION: Apparent elevations in reporting of amyotrophic lateral sclerosis (ALS)-like conditions associated with statin use have been previously described from data obtained via US and European databases. OBJECTIVE: The aim of this study was to examine US FDA Adverse Event Reporting System (FAERS) data to compare reporting odds ratios (RORs) of ALS and ALS-like conditions between statins and other drugs, for each statin agent. METHODS: We assessed for disproportional rates of reported ALS and ALS-related conditions for each statin agent separately by using the ROR formula...
April 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
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