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Pharmacokinetics (0):
Recent article
Pharmacokinetics
Abstract
A key to understanding the biological function(s) of the aryl hydrocarbon receptor (AHR) - a xenobiotic-activated receptor - is to identify its endogenous ligand(s). The discovery of a tryptophan photoproduct 6-formylindolo[3,2-b]carbazole (FICZ) as an endogenous, high affinity agonist of AHR filled...
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PMID: 21883026
PDF is available here.
PDF is available here.
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Abstract
9-Substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles were discovered as highly selective and potent anaplastic lymphoma kinase (ALK) inhibitors by structure-based drug design. The high target selectivity was achieved by introducing a substituent close to the E(0) regi...
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PMID: 21823617
PDF is available here.
PDF is available here.
Biomacromolecules (12)9 2011
Abstract
We investigated the properties of micellar siRNA delivery vehicles prepared with poly(ethylene glycol)-block-poly(l-lysine) (PEG-b-PLL) comprising lysine amines modified to contain amidine and thiol functionality. Lysine modification was achieved using 2-iminothiolane (2-IT) [yielding PEG-b-PLL(N2IM...
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PMID: 21863796
PDF is available here.
PDF is available here.
Abstract
We characterized the pharmacokinetics of fentanyl in 15 patients (American Society of Anesthesiologists Physical Status Classification 2 or 3) undergoing living-donor liver transplantation (LDLT). Fentanyl was continuously infused at the rate of 200-400 µg/h throughout the operation. The time cour...
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PMID: 21814196
PDF is available here.
PDF is available here.
Abstract
We tested the hypothesis that a high-fat diet (HFD) modifies the liver mitochondrial proteome and alters proteins involved in NO metabolism, namely arginase 1 and endothelial NO synthase. Male C57BL/6 mice were fed a control or HFD and liver mitochondria were isolated for proteomics and reactive oxy...
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PMID: 20919931
PDF is available here.
PDF is available here.
Abstract
Although clinical drug trials are indispensable in providing an appropriate background for dosage recommendations, they can provide mechanistic pharmacokinetic information only indirectly with the help of certain biomarkers for pathological, physiological and pharmacological determinants. Thus, to pr...
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PMID: 21740072
PDF is available here.
PDF is available here.
Abstract
We detected no increased risk for perinatal events with fluoxetine therapy compared to the short half-life antidepressants.
clinicaltrials.gov Identifier: NCT00279370.
© Copyright 2011 Physicians Postgraduate Press, Inc....
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PMID: 21824458
PDF is available here.
PDF is available here.
Audio, Transactions of the IRE Professional Group on (204)6 Suppl 1 2011
Abstract
Abstract
We hypothesized that activating NRF2-dependent cytoprotective gene expression with sulforaphane (SFN) affords protection against CS-induced lung damage by inhibiting chemokine production. Results indicate that in the human BEAS-2B epithelial cell line, 5 μM SFN activated NRF2-dependent gene express...
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PMID: 21401388
PDF is available here.
PDF is available here.
Abstract
Dichlorodiphenyltrichloroethane (DDT) is still used in Africa for the indoor control of malaria and it may represent a potential hazard for wildlife. The littoral sediments of two alkaline-saline lakes, Natron (Tanzania) and Bogoria (Kenya), in the Eastern Rift Valley, supporting lar...
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PMID: 21809777
PDF is available here.
PDF is available here.
Abstract
Characterization of the exposure-response relationship has identified that a dose range of 8 to 12 mg provides clinical benefit for the improvement in UPDRS total motor score in patients with early PD. Similarly, pharmacokinetic-pharmacodynamic analysis showed that, in patients with advanced PD, the...
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PMID: 18978485
PDF is available here.
PDF is available here.
MMW Fortschritte der Medizin (153)19 2011
Abstract
Abstract
Cocoa, especially the water-insoluble cocoa fraction (WICF), is a rich source of polyphenols. In this study, sequential in vitro digestion of the WICF with gastrointestinal enzymes as well as its bacterial fermentation in a human colonic model system were carried out to investigate b...
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PMID: 21294250
PDF is available here.
PDF is available here.
Abstract
Over the past decade, the use of the monoclonal antibody alemtuzumab in chronic lymphocytic leukemia has expanded from administration as a single-agent therapy, into use in combination with fludarabine or rituximab, and further to use as a consolidation agent with the goal of eradica...
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PMID: 21685865
PDF is available here.
PDF is available here.
Abstract
PURPOSE. Topical biphasic vesicle delivery system encapsulating interferon alpha (IFN α) was developed as an alternative to injections used to treat human papillomavirus (HPV) infections. METHODS. Biphasic lipid vesicles encapsulating increasing doses of IFN α (biphasic IFN α) wer...
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PMID: 21291377
PDF is available here.
PDF is available here.
Abstract
Burned patients have altered vancomycin pharmacokinetics necessitating adjusted dosing. Published initial dosing recommendations to target troughs of 15-20mg/L for this population are lacking.
This study was conducted to develop initial vancomycin dosing recommendatio...
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PMID: 21095062
PDF is available here.
PDF is available here.
Xenobiotica (41)5 2011
Abstract
We have created an ophthalmic time-release prodrug form combined with a muco-adhesive lubricant compound carboxymethylcellulose and other essential corneal absorption promoter excipients tailoring the increased intraocular absorption of L-carnosine in the aqueous humor and optimizing its specific ef...
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PMID: 20408504
PDF is available here.
PDF is available here.
Xenobiotica (41)5 2011
Abstract
Drug delivery by inhalation is routine for the treatment of local pulmonary conditions like asthma, cystic fibrosis, and chronic obstructive pulmonary disease. Only recently, though, has the inhalation route been considered for administering drugs for systemic diseases. The pulmonary route is attrac...
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PMID: 19085124
PDF is available here.
PDF is available here.
Abstract
The main objective of present research study was to evaluate the potential of lipid nanoparticles for active delivery of an antiretroviral drug to lymphatic tissues. Stavudine entrapped drug loaded solid lipid nanoparticles (SLNs) were prepared and characterized for a variety of phys...
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PMID: 21612153
PDF is available here.
PDF is available here.
Abstract
Sanguinarine liposomes were prepared by a remote loading method using three different ammonium salts. A series of studies, including in vitro release, in vitro and in vivo anti-tumor effects and pharmacokinetics in rats, were conducted. The three liposomes showed pH-sensitive release...
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PMID: 21612152
PDF is available here.
PDF is available here.
Abstract
The use of artemisinin combination therapies to treat uncomplicated malaria is growing and, therefore, so is the number of children exposed to these agents. As a result, there is a huge drive to develop paediatric formulations. However, relatively limited data exist regarding the pharmacokinetic pro...
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PMID: 21320023
PDF is available here.
PDF is available here.
Integrative Biology (3)4 2011
Abstract
We describe the design, production and characterization of a novel immunocytokine, in which murine interferon-alpha2 was sequentially fused with the tumor-targeting antibody fragment scFv(F8), specific to the alternatively-spliced EDA domain of fibronectin. The resulting fusion protein (F8-IFNa) cou...
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PMID: 21225052
PDF is available here.
PDF is available here.
Molecular Oncology (5)2 2011
Abstract
Activating mutations in BRAF, a constituent of the map kinase pathway, were first discovered as being most prevalent in melanoma in 2002. Only recently have potent and selective, orally available inhibitors of BRAF emerged for clinical testing and demonstrated clear evidence of tumor...
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PMID: 21393075
PDF is available here.
PDF is available here.
Abstract
We demonstrate the technique in dye infusion experiments that provide cylindrical and spherical distributions when infusing with porous membrane and conventional single-port catheters, respectively. This optical method incorporates important parameters, such as optimum camera exposure, captured came...
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PMID: 21342811
PDF is available here.
PDF is available here.
Abstract
A simple validated LC-UV method for the phytochemical analysis of four bioactive quassinoids, 13alpha(21)-epoxyeurycomanone (EP), eurycomanone (EN), 13alpha,21-dihydroeurycomanone (ED) and eurycomanol (EL) in rat plasma following oral (200 mg/kg) and intravenous administration (10 mg...
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PMID: 21485270
PDF is available here.
PDF is available here.
Abstract
To highlight the significant impact breakthrough cancer pain (BTcP) can have on patients' quality of life and to discuss potential management strategies that could improve pain control in clinical practice as well as effective strategies to manage risk.
BTcP can place...
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PMID: 21325998
PDF is available here.
PDF is available here.
Abstract
Obesity is a worldwide epidemic with increasing importance in both industrialised and developing countries. Anaesthesiologists will be increasingly challenged by the care for morbidly and super-obese patients. Prerequisites for an optimal perioperative care are a suitable and adapted environment both...
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PMID: 21516912
PDF is available here.
PDF is available here.
British Journal of Cancer (104)5 2011
Abstract
I study was carried out to determine the safety, dose-limiting toxicity, recommended phase II dose (RPTD), as well as pharmacokinetic (PK) and pharmacodynamic (PD) profiles of SB939 in a daily × 5 schedule in advanced solid tumours.
Sequential dose-escalating cohorts of patients wer...
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PMID: 21285985
PDF is available here.
PDF is available here.
Abstract
We randomly assigned patients to receive fidaxomicin (200 mg twice daily) or vancomycin (125 mg four times daily) orally for 10 days. The primary end point was clinical cure (resolution of symptoms and no need for further therapy for C. difficile infection as of the second day after the end of the c...
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PMID: 21288078
PDF is available here.
PDF is available here.
Biomedical Materials (6)1 2011
Abstract
We report on the development of a CpG ODN-loaded suture that can close up the wound following tumor excision and provide sustained localized delivery of CpG ODN to treat local disease recurrence. The suture was prepared by melt extruding a mixture of polylactic acid-co-glycolic acid (PLGA 75:25 0.47...
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PMID: 21206000
PDF is available here.
PDF is available here.
Anti-Cancer Drugs (22)2 2011
Abstract
We showed that arginine deprivation in vitro profoundly and selectively sensitized human cancer cells of different organ origin to low doses of canavanine, an arginine analogue of plant origin. In sensitive cancer cells arginine starvation led to the activation of caspase-9, caspase-3 and caspase-7,...
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PMID: 20717004
PDF is available here.
PDF is available here.
Anti-Cancer Drugs (22)2 2011
Abstract
These results suggest that the Gal-PHEA-DOX conjugate has great potential for use in hepatocellular carcinoma chemotherapy because of its enhanced antitumor effect with reduced systemic toxicity including hepatotoxicity....
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PMID: 20966743
PDF is available here.
PDF is available here.
Abstract
Increasingly, early phase clinical trials involve pharmacodynamic (PD) and pharmacokinetic (PK) assays as well as frequent imaging studies. The authors conducted a prospective study examining patients' willingness to undergo such tests and the number of tests the patients would tolerate.
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PMID: 21246533
PDF is available here.
PDF is available here.
Abstract
These results support hypotheses as to why certain Cu(i) binding amino acids are preferred over others in proteins expressed at different pH and exposed to oxidative environments. The results also have implications for interpreting site-directed mutagenesis studies aimed at identifying copper bindin...
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PMID: 21553704
PDF is available here.
PDF is available here.
Abstract
Abstract
Risks to health from large-scale atmospheric nuclear weapons testing are still relatively unknown. A sample of 85,000 deciduous teeth collected from Americans born during the bomb-testing years assessed risk by in vivo measurement of residual strontium-90 (Sr-90) concentrations, usin...
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PMID: 21319726
PDF is available here.
PDF is available here.
Abstract
This article explores the issue of polypharmacy in older adults. The physiological changes in organ function in older people and the effect of this on pharmacokinetics and pharmacodynamics are discussed. The risks of adverse drug reactions and adverse drug interactions linked to polypharmacy are expl...
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PMID: 21706978
PDF is available here.
PDF is available here.
Abstract
Our goal was to identify candidate polymorphisms that could influence overall survival (OS) in advanced non-small cell lung cancer (NSCLC) patients treated with carboplatin (CBDCA) and paclitaxel (PTX).
Chemotherapy-naïve stage IIIB or IV NSCLC patients treated with CBDCA (area unde...
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PMID: 21079520
PDF is available here.
PDF is available here.
Abstract
We generated a cell line that was resistant to the IGF-1R/InsR benzimidazole inhibitors, BMS-554417 and BMS-536924, and compared expression profiles of the parental and resistant cells lines using Affymetrix GeneChip Human Genome U133 arrays. Compared with MCF-7 cells, breast cancer resistance prote...
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PMID: 21220496
PDF is available here.
PDF is available here.
Abstract
We aimed to study the effects of gliadin and various intestinal bacterial strains on mucosal barrier integrity, gliadin translocation, and cytokine production.
Changes in gut mucosa were assessed in the intestinal loops of inbred Wistar-AVN rats that were reared under germ-free condi...
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PMID: 21249146
PDF is available here.
PDF is available here.
Abstract
We describe an improved fluorescent imaging approach to detect potential islet dysfunction. Using Cell Tracker Red (CTR, a mildly thiol-reactive fluorescent probe) to positively label particular islets, we measured intracellular free calcium with fura-2 AM in both CTR-labeled and unlabeled sets of p...
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PMID: 21266850
PDF is available here.
PDF is available here.
Abstract
Our results implicate that, when equipped with targeting ligands, liposomes are most suitable for the imaging of plaque-associated endothelial markers due to low background enhancement, whereas micelles, which accumulate extravascularly on a long timescale, are suited for imaging of less abundant ma...
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PMID: 20882509
PDF is available here.
PDF is available here.
Abstract
This pharmacokinetic (PK) study was designed to investigate the maximum intranasal insulin dose that could be achieved by repeated doses in a single nostril of a nasal spray of recombinant regular human insulin 1% in combination with cyclopentadecalactone (CPE-215) 2%, a compound tha...
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PMID: 21303633
PDF is available here.
PDF is available here.
Abstract
We outline key PK concepts relevant to PD, and then consider real-life experiments to illustrate the importance to the medicinal chemist of data obtained by PKPD. Useful assumptions and potential pitfalls are described, providing a holistic view of the plethora of determinants behind in vitro-in viv...
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PMID: 21320067
PDF is available here.
PDF is available here.
Abstract
The objective of this study was to develop an estimate of the percent dermal absorption of permethrin in humans to provide more accurate estimates of potential systemically absorbed dose associated with dermal exposure scenarios. Piperonyl butoxide (PBO) was used as a reference compo...
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PMID: 21271436
PDF is available here.
PDF is available here.
Abstract
To compare the subjective effects of oxymorphone extended release (OM-ER) versus oxycodone controlled release (OC-CR).
Randomized, double-blind, crossover study.
Inpatient unit.
Healthy, nondependent recreational opioid users....
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PMID: 21823549
PDF is available here.
PDF is available here.
Abstract
We have developed a statistical text-mining approach (BInary Characteristics Extractor and biomedical Properties Predictor: BICEPP) to help experts screen drugs that may have important clinical characteristics of interest....
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PMID: 21510898
PDF is available here.
PDF is available here.
Abstract
Nilotinib (Tasigna®), a highly selective and potent BCR-ABL tyrosine kinase inhibitor, is approved for the treatment of chronic myeloid leukaemia in the chronic phase (CML-CP) and the accelerated phase (CML-AP) in patients resistant or intolerant to prior therapy, including imatinib...
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PMID: 21184622
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)4 2011
Abstract
Prasugrel (CAS 150322-43-3), an inhibitor of platelet activation and aggregation, is indicated to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome. If a proton pump inhibitor is co-administered with prasugrel, a pH dependent salt-to-base conversion rate of...
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PMID: 21650084
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)4 2011
Abstract
The market of generic drugs has been greatly developing during the last 15 years in various European Union (EU) member states, mainly in the Mediterranean area, including non-EU countries, i.e., in the Middle East. This has required a more detailed support from EMA (European Medicines Agency) as guid...
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PMID: 21650079
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)4 2011
Abstract
The present study was performed to compare the bioavailability of two perindopril erbumine (CAS 107133-36-8) 4 mg tablet formulations (test formulation and reference formulation). This study was a randomized, single-blind, two-period, two-sequence cross-over study which included 20 healthy adult male...
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PMID: 21650082
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)6 2011
Abstract
The aim of the present study was to determine the prescribing practice for clozapine (CAS 5786-21-0) as well as the plasma levels of clozapine and its main metabolite norclozapine (CAS 6104-71-8) in Mexican patients. A prospective study was performed in 69 in and out psychotic patien...
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PMID: 21827043
PDF is available here.
PDF is available here.
Arzneimittel-Forschung (61)6 2011
Abstract
I was compared with that of clopidogrel bisulfate form II in 12 male Sprague-Dawley rats. The rats, randomly divided into two groups, received a single oral dose of 8 mg/kg clopidogrel (CP) bisulfate form I and form II, respectively, under fasting condition. The plasma concentrations of CP and its i...
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PMID: 21827046
PDF is available here.
PDF is available here.
British Journal of Nutrition (105)2 2011
Abstract
β-Carotene (BC), β-cryptoxanthin (CX) and α-carotene (AC) are common carotenoids that form retinol. The amount of retinol (vitamin A) formed from carotenoid-rich foods should depend chiefly on the bioavailability (absorption and circulation time in the body) of carotenoids from their major food s...
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PMID: 20807466
PDF is available here.
PDF is available here.
British Journal of Nutrition (105)2 2011
Abstract
Astaxanthin is a carotenoid with antioxidant, anti-cancer and anti-inflammatory properties. The pharmacokinetics of astaxanthin after its intravenous (5, 10, and 20 mg/kg) and oral (100 and 200 mg/kg) administration and its first-pass extraction ratios after its intravenous, intraportal or intragast...
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PMID: 20819240
PDF is available here.
PDF is available here.
British Journal of Nutrition (105)2 2011
Abstract
Ageing women may choose to drink soya milk to reduce menopausal symptoms. As fermentation enriches soya milk with isoflavone aglycones, its beneficial qualities may improve. To reduce osteoporotic risk, however, soya milk must be Ca enriched, and it is not known how fermentation affects Ca bioavaila...
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PMID: 20854699
PDF is available here.
PDF is available here.
British Journal of Nutrition (105)2 2011
Abstract
We tested curcumin for its ability to induce PON1 in Huh7 hepatocytes in culture. Curcumin ( ≥ 10 μmol/l) dose-dependently induced PON1 transactivation in Huh7 cells. However, dietary supplementation of female B6C3F1 mice with curcumin (500 mg/kg diet) for 2 weeks did not increase the hepatic PON...
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PMID: 21078213
PDF is available here.
PDF is available here.
British Journal of Nutrition (105)1 2011
Abstract
We evaluated the absorption and metabolism of palatinose in rats by the carbohydrate load test and the 13C- and H2-breath tests. We compared the results of these tests with those of sucrose, since sucrose is an isomer of palatinose and generally known to be degraded and absorbed from the small intes...
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PMID: 20807468
PDF is available here.
PDF is available here.
British Journal of Nutrition (105)2 2011
Abstract
We showed that enteric-coated bovine LF tablets can decrease visceral fat accumulation, hypothesising that the enteric coating is critical to the functional peptides reaching the visceral fat tissue and exerting their anti-adipogenic activity. The aim of the present study was to assess whether inges...
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PMID: 20854698
PDF is available here.
PDF is available here.
Abstract