当前位置： SCI文献检索 > PHARMACEUTICAL RESEARCH期刊下所有文献 > Influence of gallate esterification on the activity of procyanidin B2 in androgen-dependent human prostate carcinoma LNCaP cells.

Influence of gallate esterification on the activity of procyanidin B2 in androgen-dependent human prostate carcinoma LNCaP cells.

Abstract：

PURPOSE:Present study assessed the influence of gallate esterification on the anti-cancer activity of procyanidin B2 (B2) in androgen-dependent human prostate carcinoma LNCaP cells employing B2-3,3'-di-O-gallate (B2-G(2)), two mono-gallate esters B2-3-O-gallate (B2-3G) and B2-3'-O-gallate (B2-3'G) and the parent compound B2, all isolated from grape seed extract (GSE). MATERIALS AND METHODS:Study compounds were isolated from GSE by several chromatographic steps and structures determined by a combination of enzymatic hydrolysis, mass spectrometry and comparisons with standards. Cells, treated with these compounds, were assessed for viability and apoptosis and examined by western blotting. RESULTS:Gallate esters B2-G(2), B2-3G and B2-3'G significantly decreased LNCaP cell viability; however, B2 and gallic acid were ineffective. Furthermore, only B2-G(2) also significantly decreased cell growth. Decreases in cell viability were largely due to apoptosis induction with B2-G(2) and B2-3'G exhibiting comparable effects, whereas B2-3G was less effective. In mechanistic studies, B2-G(2) and B2-3'G treatments caused caspases-9 and -3 and PARP cleavage, and down-regulated Bcl-2, Bcl-Xl and androgen receptor levels. CONCLUSION:Together, our findings demonstrate anti-PCA efficacy of B2-G(2) and suggest that a gallate ester moiety at 3' position of procyanidin B2 contributes more extensively toward the biological activity of the di-gallate ester than esterification of position 3.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Chou SC,Kaur M,Thompson JA,Agarwal R,Agarwal C

doi

10.1007/s11095-009-0037-6

subject

Has Abstract

pub_date

2010-04-01 00:00:00

pages

619-27

issue

4

eissn

0724-8741

issn

1573-904X

journal_volume

27

pub_type

杂志文章

相关文献

PHARMACEUTICAL RESEARCH文献大全
  • Magnetized aerosols comprising superparamagnetic iron oxide nanoparticles improve targeted drug and gene delivery to the lung.

    abstract：PURPOSE:Targeted delivery of aerosols could not only improve efficacy of inhaled drugs but also reduce side effects resulting from their accumulation in healthy tissue. Here we investigated the impact of magnetized aerosols on model drug accumulation and transgene expression in magnetically targeted lung regions of una...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-012-0682-z

    authors： Hasenpusch G,Geiger J,Wagner K,Mykhaylyk O,Wiekhorst F,Trahms L,Heidsieck A,Gleich B,Bergemann C,Aneja MK,Rudolph C

    更新日期：2012-05-01 00:00:00

  • On the Nature of Physiologically-Based Pharmacokinetic Models -A Priori or A Posteriori? Mechanistic or Empirical?

    abstract：:Physiologically-based pharmacokinetic (PBPK) models explicitly incorporate tissue-specific blood flows, partition coefficients, and metabolic processes. Since PBPK models are derived using physiologic parameters and interactions of the compound with tissue components, these models are considered to be "bottom up" as o...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章,评审

    doi：10.1007/s11095-016-2089-8

    authors： Korzekwa K,Nagar S

    更新日期：2017-03-01 00:00:00

  • The relationship of pKa and acute skin irritation in man.

    abstract：:The relationship between pKa and skin irritation in man is studied for a homologous series of benzoic acid derivatives, which permeate through human skin at comparable rates (15-88 micrograms/cm2/hr). Skin irritation and pKa are correlated for pKa less than or equal to 4. Laser Doppler velocimetric assessment of skin ...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1015931105660

    authors： Berner B,Wilson DR,Guy RH,Mazzenga GC,Clarke FH,Maibach HI

    更新日期：1988-10-01 00:00:00

  • Cyclodextrins as mucosal absorption promoters of insulin. II. Effects of beta-cyclodextrin derivatives on alpha-chymotryptic degradation and enteral absorption of insulin in rats.

    abstract：:The relative effectiveness of two beta-cyclodextrin derivatives, i.e., dimethyl-beta-cyclodextrin (DM beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD), in enhancing enteral absorption of insulin was evaluated in the lower jejunal/upper ileal segments of the rat by means of an in situ closed loop method. The i...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1018997101542

    authors： Shao Z,Li Y,Chermak T,Mitra AK

    更新日期：1994-08-01 00:00:00

  • Cell-penetrating antimicrobial peptides - prospectives for targeting intracellular infections.

    abstract：PURPOSE:To investigate the suitability of three antimicrobial peptides (AMPs) as cell-penetrating antimicrobial peptides. METHODS:Cellular uptake of three AMPs (PK-12-KKP, SA-3 and TPk) and a cell-penetrating peptide (penetratin), all 5(6)-carboxytetramethylrhodamine-labeled, were tested in HeLa WT cells and analyzed ...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-014-1550-9

    authors： Bahnsen JS,Franzyk H,Sayers EJ,Jones AT,Nielsen HM

    更新日期：2015-05-01 00:00:00

  • Identification of Factors of Importance for Spray Drying of Small Interfering RNA-Loaded Lipidoid-Polymer Hybrid Nanoparticles for Inhalation.

    abstract：BACKGROUND:With the recent approval of the first small interfering RNA (siRNA) therapeutic formulated as nanoparticles, there is increased incentive for establishing the factors of importance for the design of stable solid dosage forms of such complex nanomedicines. METHODS:The aims of this study were: (i) to identify...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-019-2663-y

    authors： Dormenval C,Lokras A,Cano-Garcia G,Wadhwa A,Thanki K,Rose F,Thakur A,Franzyk H,Foged C

    更新日期：2019-08-02 00:00:00

  • Characterization of oil-in-water emulsions prepared from solid-state emulsions: effect of matrix and oil phase.

    abstract：:Emulsions (o/w) were prepared from solid-state emulsions comprised of various matrix materials and oils and the resultant particle size properties determined. Results suggest that for those matrices that can form solid-state emulsions, the droplet size decreased as a function of time, as previously observed. The final...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1018912100826

    authors： Shively ML

    更新日期：1993-08-01 00:00:00

  • Dynamic analysis of GI absorption and hepatic distribution processes of telmisartan in rats using positron emission tomography.

    abstract：PURPOSE:To dynamically analyze the processes of oral absorption and hepatobiliary distribution of telmisartan using positron emission tomography (PET). METHODS:(11)C-labeled telmisartan ([(11)C]TEL) was orally administered to rats with or without non-radiolabeled telmisartan (0.5, and 10 mg/kg). PET scanning of abdomi...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-012-0768-7

    authors： Kataoka M,Takashima T,Shingaki T,Hashidzume Y,Katayama Y,Wada Y,Oh H,Masaoka Y,Sakuma S,Sugiyama Y,Yamashita S,Watanabe Y

    更新日期：2012-09-01 00:00:00

  • Development of a Virosomal RSV Vaccine Containing 3D-PHAD® Adjuvant: Formulation, Composition, and Long-Term Stability.

    abstract：PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-018-2453-y

    authors： Lederhofer J,van Lent J,Bhoelan F,Karneva Z,de Haan A,Wilschut JC,Stegmann T

    更新日期：2018-07-03 00:00:00

  • Synthesis and in vitro evaluation of a novel chitosan-glutathione conjugate.

    abstract：PURPOSE:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-005-6248-6

    authors： Kafedjiiski K,Föger F,Werle M,Bernkop-Schnürch A

    更新日期：2005-09-01 00:00:00

  • N-terminal site-specific mono-PEGylation of epidermal growth factor.

    abstract：PURPOSE:N-terminal site-specific mono-PEGylation of recombinant human epidermal growth factor (EGF) was accomplished using polyethyleneglycol (PEG) derivatives (Mw = 2000 and 5000) through a reactive terminal aldehyde group. METHODS:The site-specific PEG conjugation was conducted ata slightly acidic pH condition (pH 5...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1023402123119

    authors： Lee H,Jang IH,Ryu SH,Park TG

    更新日期：2003-05-01 00:00:00

  • Nanotechnology-based cancer therapeutics--promise and challenge--lessons learned through the NCI Alliance for Nanotechnology in Cancer.

    abstract：:The new generation of nanotechnology-based drug formulations is challenging the accepted ways of cancer treatment. Multi-functional nanomaterial constructs have the capability to be delivered directly to the tumor site and eradicate cancer cells selectively, while sparing healthy cells. Tailoring of the nano-construct...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-010-0214-7

    authors： Farrell D,Ptak K,Panaro NJ,Grodzinski P

    更新日期：2011-02-01 00:00:00

  • Evaluation of Predictors of Protein Relative Stability Obtained by Solid-State Hydrogen/Deuterium Exchange Monitored by FTIR.

    abstract：PURPOSE:Hydrogen/deuterium (H/D) exchange over a range of temperatures suggests a protein structural/mobility transition in the solid state below the system glass transition temperature (Tg). The purpose of this study was to determine whether solid-state protein stability correlates with the difference between storage ...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-020-02897-7

    authors： Fang R,Obeidat W,Pikal MJ,Bogner RH

    更新日期：2020-08-13 00:00:00

  • Column-switching high-performance liquid chromatography for on-line simultaneous determination and resolution of enantiomers of verapamil and its metabolites.

    abstract：:An on-line simultaneous assay for the enantiomers of verapamil (VA) and its three metabolites in plasma was developed with column-switching HPLC. This system consists of an ovomucoid protein chiral stationary phase coupled to an achiral reversed-phase column via a dilution tube and a trapping column. The reversed-phas...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1015848806240

    authors： Oda Y,Asakawa N,Kajima T,Yoshida Y,Sato T

    更新日期：1991-08-01 00:00:00

  • Inhibition of P-glycoprotein: rapid assessment of its implication in blood-brain barrier integrity and drug transport to the brain by an in vitro model of the blood-brain barrier.

    abstract：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1011913723928

    authors： Fenart L,Buée-Scherrer V,Descamps L,Duhem C,Poullain MG,Cecchelli R,Dehouck MP

    更新日期：1998-07-01 00:00:00

  • Long-circulating poly(ethylene glycol)-modified gelatin nanoparticles for intracellular delivery.

    abstract：PURPOSE:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1016486910719

    authors： Kaul G,Amiji M

    更新日期：2002-07-01 00:00:00

  • Fetal membrane transport enhancement using ultrasound for drug delivery and noninvasive detection.

    abstract：PURPOSE:The purpose of this research was to evaluate the effect of ultrasound on mass transport across fetal membrane for direct fetal drug delivery and sensing of the amniotic fluid in a noninvasive manner. METHODS:Post-delivery human fetal membranes (chorioamnion) were used for in vitro experiments, in which the eff...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-014-1470-8

    authors： Wolloch L,Azagury A,Goldbart R,Traitel T,Groisman G,Hallak M,Kost J

    更新日期：2015-02-01 00:00:00

  • In vivo effects of glycyl-glutamate and glycyl-sarcosine on gabapentin oral absorption in rat.

    abstract：PURPOSE:The objective of this study was to evaluate the in vivo consequences of glycyl-glutamate coadministration on gabapentin oral absorption. METHODS:Rats were administered gabapentin (10 mg/kg plus radiotracer) by gastric gavage, in the absence and presence of dipeptides, and by intravenous administration. Serial ...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-007-9272-x

    authors： Nguyen TV,Fleisher D,Smith DE

    更新日期：2007-08-01 00:00:00

  • Nonisothermal stability assessment of stable pharmaceuticals: testing of a clindamycin phosphate formulation.

    abstract：:The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1015840320410

    authors： Kipp JE,Hlavaty JJ

    更新日期：1991-05-01 00:00:00

  • Interaction of polysorbate 80 with erythropoietin: a case study in protein-surfactant interactions.

    abstract：PURPOSE:The cause of antibody positive pure red cell aplasia associated with the subcutaneous administration of EPREX to patients with chronic kidney failure has been determined to be due to the leaching of weakly adjuvant compounds from the uncoated rubber stoppers that were formerly used in prefilled syringes. Other ...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-005-5356-7

    authors： Villalobos AP,Gunturi SR,Heavner GA

    更新日期：2005-07-01 00:00:00

  • Effects of pluronic P85 on GLUT1 and MCT1 transporters in the blood-brain barrier.

    abstract：PURPOSE:The amphiphilic block copolymer Pluronic P85 (P85) increases the permeability of the blood-brain barrier (BBB) with respect to a broad spectrum of drugs by inhibiting the drug efflux transporter, P-glycoprotein (Pgp). In this regard, P85 serves as a promising component for CNS drug delivery systems. To assess t...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/b:pham.0000048189.79606.6e

    authors： Batrakova EV,Zhang Y,Li Y,Li S,Vinogradov SV,Persidsky Y,Alakhov VY,Miller DW,Kabanov AV

    更新日期：2004-11-01 00:00:00

  • Release of human serum albumin from poly(lactide-co-glycolide) microspheres.

    abstract：:Human serum albumin (HSA) was encapsulated in a 50:50 copolymer of DL-lactide/glycolide in the form of microspheres. These microspheres were used as a model formulation to study the feasibility of controlling the release of large proteins over a 20- to 30-day period. We show that HSA can be successfully incorporated i...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1015948829632

    authors： Hora MS,Rana RK,Nunberg JH,Tice TR,Gilley RM,Hudson ME

    更新日期：1990-11-01 00:00:00

  • Supramolecular Chitosan Micro-Platelets Synergistically Enhance Anti-Candida albicans Activity of Amphotericin B Using an Immunocompetent Murine Model.

    abstract：PURPOSE:The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. METH...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-017-2117-3

    authors： Grisin T,Bories C,Bombardi M,Loiseau PM,Rouffiac V,Solgadi A,Mallet JM,Ponchel G,Bouchemal K

    更新日期：2017-05-01 00:00:00

  • Simultaneous in vivo visualization and localization of solid oral dosage forms in the rat gastrointestinal tract by magnetic resonance imaging (MRI).

    abstract：PURPOSE:Bioavailability of orally administered drugs is much influenced by the behavior, performance and fate of the dosage form within the gastrointestinal (GI) tract. Therefore, MRI in vivo methods that allow for the simultaneous visualization of solid oral dosage forms and anatomical structures of the GI tract have ...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1023/a:1012161630481

    authors： Christmann V,Rosenberg J,Seega J,Lehr CM

    更新日期：1997-08-01 00:00:00

  • Profiling the role of deacylation-reacylation in the lymphatic transport of a triglyceride-mimetic prodrug.

    abstract：PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-014-1579-9

    authors： Han S,Hu L,Quach T,Simpson JS,Trevaskis NL,Porter CJ

    更新日期：2015-05-01 00:00:00

  • Novel beads made of alpha-cyclodextrin and oil for topical delivery of a lipophilic drug.

    abstract：PURPOSE:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-007-9395-0

    authors： Trichard L,Delgado-Charro MB,Guy RH,Fattal E,Bochot A

    更新日期：2008-02-01 00:00:00

  • Characterization of Intestinal and Hepatic CYP3A-Mediated Metabolism of Midazolam in Children Using a Physiological Population Pharmacokinetic Modelling Approach.

    abstract：PURPOSE:Changes in drug absorption and first-pass metabolism have been reported throughout the pediatric age range. Our aim is to characterize both intestinal and hepatic CYP3A-mediated metabolism of midazolam in children in order to predict first-pass and systemic metabolism of CYP3A substrates. METHODS:Pharmacokinet...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-018-2458-6

    authors： Brussee JM,Yu H,Krekels EHJ,Palić S,Brill MJE,Barrett JS,Rostami-Hodjegan A,de Wildt SN,Knibbe CAJ

    更新日期：2018-07-30 00:00:00

  • A Novel Monocarboxylate Transporter Inhibitor as a Potential Treatment Strategy for γ-Hydroxybutyric Acid Overdose.

    abstract：PURPOSE:Monocarboxylate transporter (MCT) inhibition represents a potential treatment strategy for γ-hydroxybutyric acid (GHB) overdose by blocking its renal reabsorption in the kidney. This study further evaluated the effects of a novel, highly potent MCT inhibitor, AR-C155858, on GHB toxicokinetics/toxicodynamics (TK...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-014-1583-0

    authors： Vijay N,Morse BL,Morris ME

    更新日期：2015-06-01 00:00:00

  • Targeting 15d-prostaglandin J2 to hepatic stellate cells: two options evaluated.

    abstract：PURPOSE:Delivery of apoptosis-inducing compounds to hepatic stellate cells (HSC) may be an effective strategy to reverse liver fibrosis. The aim of this study was therefore to examine the selective targeting of the apoptosis-inducing drug 15-deoxy-delta12,14-prostaglandin J2 (15dPGJ2) with two different HSC-carriers: h...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-006-9175-2

    authors： Hagens WI,Mattos A,Greupink R,de Jager-Krikken A,Reker-Smit C,van Loenen-Weemaes A,Gouw IA,Poelstra K,Beljaars L

    更新日期：2007-03-01 00:00:00

  • Population Pharmacokinetics, Efficacy Exposure-response Analysis, and Model-based Meta-analysis of Fenebrutinib in Subjects with Rheumatoid Arthritis [corrected].

    abstract：PURPOSE:Fenebrutinib (GDC-0853), a Bruton's tyrosine kinase (BTK) inhibitor was investigated in a Phase 2 clinical trial in patients with rheumatoid arthritis (RA). Our aim was to apply a model-informed drug development (MIDD) approach to examine the totality of available clinical efficacy data. METHODS:Population pha...

    journal_title：Pharmaceutical research

    pub_type： 杂志文章

    doi：10.1007/s11095-019-2752-y

    authors： Chan P,Yu J,Chinn L,Prohn M,Huisman J,Matzuka B,Hanley W,Tuckwell K,Quartino A

    更新日期：2020-01-06 00:00:00