Protolichesterinic acid enhances doxorubicin-induced apoptosis in HeLa cells in vitro.

Abstract:

AIM:The aim of this study was to investigate the effect of protolichesterinic acid, a lichen secondary metabolite, on anti-proliferative activity of doxorubicin in three human cancer cell lines, HeLa, SH-SY5Y and K562 cells. MAIN METHODS:The data obtained from MTT assays, performed on cells treated with protolichesterinic acid and doxorubicin alone and in combination, were analysed by the median-effect method as proposed by Chou and Talalay and the Bliss independence model. Apoptosis rate was evaluated by fluorescence microscopy, caspase-3, 8 and 9 activities were detected by spectrofluorimetric analysis and protein expression of Bim, Bid, Bax and Mcl-2 was analysed by Western blotting. The interaction of protolichesterinic acid with thioesterase domain of human fatty acid synthase (hFAS) was investigated by a molecular docking study. KEY FINDINGS:The in vitro activity of doxorubicin against HeLa cancer cell line, but not against SH-SY5Y and K562 cells, was synergically increased by protolichesterinic acid. The increased cytotoxicity caused by protolichesterinic acid in HeLa cells was due to a pro-apoptotic effect and was associated to caspase-3, 8 and 9 activation. The simultaneous treatment for 24h with protolichesterinic acid plus doxorubicin caused an increase of Bim protein expression and the appearance of cleaved form of Bid protein. The molecular modelling analysis showed that protolichesterinic acid seemed to behave as a competitive inhibitor of hFAS. SIGNIFICANCE:These results suggest that protolichesterinic acid could be envisaged as an useful tool against certain types of tumor cells in combination with anticancer drugs.

journal_name

Life Sci

journal_title

Life sciences

authors

Brisdelli F,Perilli M,Sellitri D,Bellio P,Bozzi A,Amicosante G,Nicoletti M,Piovano M,Celenza G

doi

10.1016/j.lfs.2016.06.023

subject

Has Abstract

pub_date

2016-08-01 00:00:00

pages

89-97

eissn

0024-3205

issn

1879-0631

pii

S0024-3205(16)30379-4

journal_volume

158

pub_type

杂志文章
  • Simple and rapid physico-chemical methods to examine action of antimalarial drugs with hemin: its application to Artemisia annua constituents.

    abstract::Malaria is a major health problem in many countries and according to an estimate of the WHO, more than 500 million infections occur per year. Artemisinin, a sesquiterpene from Artemisia annua L., has received considerable attention as a promising and potent antimalarial drug for its stage speciticity, its rather low t...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(01)01447-3

    authors: Bilia AR,Lazari D,Messori L,Taglioli V,Temperini C,Vincieri FF

    更新日期:2002-01-04 00:00:00

  • Norepinephrine-induced down regulation of alpha 1 adrenergic receptors in cultured rabbit aorta smooth muscle cells.

    abstract::Drug-induced refractoriness of alpha-adrenergic receptor-mediated vasoconstriction may be a clinically important phenomenon. We have investigated the possible molecular mechanisms underlying this phenomenon in cultured vascular smooth muscle cells derived from the rabbit aorta. alpha 1-Adrenergic receptors were identi...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(83)90824-x

    authors: Wikberg JE,Akers M,Caron MG,Hagen PO

    更新日期:1983-10-03 00:00:00

  • Sex differences in the uptake and retention of imipramine and desmethylimipramine in the rat lung.

    abstract::14C-Imipramine was administered to male and female Sprague-Dawley rats and animals were sacrificed at 4, 8, 12, and 20 hours later. At all time points, total radioactivity in female lung was several-fold higher than in males. In addition, female lungs had a higher concentration of desmethylimipramine (DMI) as compared...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(82)90610-5

    authors: Ginsburg E,Hirokata Y,Gram TE

    更新日期:1982-03-01 00:00:00

  • Properties of calcium channels coupled to endogenous glutamate release from the vascularly perfused rat stomach in vitro.

    abstract::We have demonstrated that both high-K+ and electrical stimulation of the vagus nerves release endogenous glutamate from the vascularly-perfused rat stomach in a calcium-dependent manner. In the present study, we examined properties of calcium channel subtypes mediating endogenous glutamate release from the stomach. Ap...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(98)00121-0

    authors: Okuma Y,Yokotani K,Murakami Y,Osumi Y

    更新日期:1998-01-01 00:00:00

  • Uncoupling of receptors is essential for opiate-induced desensitization (tolerance) in neuroblastoma x glioma hybrid cells NG 108-15.

    abstract::Neuroblastoma x glioma hybrid cells NG 108-15 were chronically treated with opioid agonists and tested for their development of "tolerance" as evaluated by the loss of inhibitory activity of opioids upon cAMP-accumulation. Desensitization was dose-dependent and non-competitive and highly selective, since the activity ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(83)90512-x

    authors: Wüster M,Costa T,Gramsch C

    更新日期:1983-01-01 00:00:00

  • Molecular mechanisms of curcumin and its analogs in colon cancer prevention and treatment.

    abstract::Colorectal cancer remains to be the most prevalent malignancy in humans and 1.5 million men and women living in the United States are diagnosed with colorectal cancer, with a predicted 145,600 new cases to be diagnosed in 2019. Curcuminoids and its synthetic analogs are now of interest due to their bioactive attribute...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2019.117032

    authors: Selvam C,Prabu SL,Jordan BC,Purushothaman Y,Umamaheswari A,Hosseini Zare MS,Thilagavathi R

    更新日期:2019-12-15 00:00:00

  • Effect of some acute and prophylactic antimigraine drugs on the vasodepressor sensory CGRPergic outflow in pithed rats.

    abstract:AIMS:This study analyzed in pithed rats the effect of several acute and prophylactic antimigraine drugs on the CGRPergic vasodepressor sensory outflow, in an attempt to investigate systemic cardiovascular effects in a model unrelated to migraine. MAIN METHODS:Male Wistar pithed rats were pretreated with continuous i.v...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2008.11.008

    authors: Lozano-Cuenca J,González-Hernández A,Muñoz-Islas E,Sánchez-López A,Centurión D,Cobos-Puc LE,Villalón CM

    更新日期:2009-01-30 00:00:00

  • The role of circulating ghrelin in growth hormone (GH) secretion in freely moving male rats.

    abstract::To examine the physiological significance of plasma ghrelin in generating pulsatile growth hormone (GH) secretion in rats, plasma GH and ghrelin levels were determined in freely moving male rats. Plasma GH was pulsatilely secreted as reported previously. Plasma ghrelin levels were measured by both N-RIA recognizing th...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(03)00147-4

    authors: Okimura Y,Ukai K,Hosoda H,Murata M,Iguchi G,Iida K,Kaji H,Kojima M,Kangawa K,Chihara K

    更新日期:2003-04-18 00:00:00

  • The silencing of replication protein A1 induced cell apoptosis via regulating Caspase 3.

    abstract:AIMS:Gastrointestinal cancers are a kind of deadly malignancy afflicting close to a million peoples worldwide. 5-Fluorouracil (5-Fu) is a main chemotherapeutic agent for cancer treatment. However, prolonged exposure of 5-Fu to cancer cells may cause chemoresistance and decrease the therapeutic potential of 5-Fu. MAIN ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2018.03.054

    authors: Zhu Y,Yi Y,Bai B,Li L,You T,Sun W,Yu Y

    更新日期:2018-05-15 00:00:00

  • New diaryl ω-(isothiocyanato)alkylphosphonates and their mercapturic acids as potential antibacterial agents.

    abstract::Thirty-four novel, diaryl ω-(isothiocyanato)alkylphosphonates with chlorine atom and methoxy, dimethoxy, methylsulfanyl, or methoxycarbonyl groups at ortho, meta, or para positions of the phenyl ring, and with an unbranched alkyl chain (n = 2-6) were designed and synthesized in a one-pot reaction in 11-76% yields. All...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2019.01.020

    authors: Janczewski Ł,Burchacka E,Psurski M,Ciekot J,Gajda A,Gajda T

    更新日期:2019-02-15 00:00:00

  • Central interaction of dexamethasone and RU-38486 on morphine antinociception in mice.

    abstract::The central interference induced by dexamethasone and RU-38486, (a glucocorticoid receptor antagonist) on morphine antinociception were studied by using the tail flick test in mice. Dexamethasone, injected intracerebrally (i.c.v.) 10 minutes before morphine, dose-dependently reduced morphine antinociception, whereas R...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(92)90521-p

    authors: Capasso A,Di Giannuario A,Loizzo A,Pieretti S,Sorrentino L

    更新日期:1992-01-01 00:00:00

  • Serum gastrin level and gastric somatostatin content and binding in long-term pyloromyotomized children.

    abstract::Since somatostatin inhibits basal and stimulated gastric acid secretion and gastrin release, it is conceivable that decreased gastric somatostatin concentration may be one of the factors responsible for gastric hypersecretion found in patients who have undergone long-term pylorotomy for hypertrophic pyloric stenosis. ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(94)00734-9

    authors: Barrios V,Urrutia MJ,Hernández M,Lama R,García-Novo MD,Hernanz A,Arilla E

    更新日期:1994-01-01 00:00:00

  • Firing properties of substantia nigra dopaminergic neurons in freely moving rats.

    abstract::Single unit recordings were obtained from putative dopaminergic neurons in the substantia nigra of awake, freely moving rats. The cells exhibited waveforms, range of firing rates and types of firing patterns identical to those of identified DA neurons of anesthetized or paralyzed rats. Two firing patterns were observe...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(85)90448-5

    authors: Freeman AS,Meltzer LT,Bunney BS

    更新日期:1985-05-20 00:00:00

  • Alpha(1)-adrenergic receptor subtypes: non-identical triplets with different dancing partners?

    abstract::Alpha(1)-adrenergic receptors are one of the three subfamilies of G protein coupled receptors activated by epinephrine and norepinephrine to control important functions in many target organs. Three human subtypes (alpha(1A), alpha(1B), alpha(1D)) are derived from separate genes and are highly homologous in their trans...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2003.07.008

    authors: Hague C,Chen Z,Uberti M,Minneman KP

    更新日期:2003-12-12 00:00:00

  • Inhibiting Rab27a in renal tubular epithelial cells attenuates the inflammation of diabetic kidney disease through the miR-26a-5p/CHAC1/NF-kB pathway.

    abstract::The effect of exosomes on receptor cells participating in intercellular communication has been extensively studied, but the effect of exosomes on donor cells remains unclear. It has been reported that exosomes secreted by renal proximal tubular epithelial cells (PTECs) under different stimuli accelerate acute and chro...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.118347

    authors: Li S,Jia Y,Xue M,Hu F,Zheng Z,Zhang S,Ren S,Yang Y,Si Z,Wang L,Guan M,Xue Y

    更新日期:2020-11-15 00:00:00

  • Effect of Y-24180 on Ca2+ movement and proliferation in renal tubular cells.

    abstract::In canine renal tubular cells, the effect of Y-24180, a presumed specific platelet activating factor (PAF) receptor antagonist, on intracellular Ca(2+) concentration ([Ca(2+)](i)) was measured by using fura-2 as a Ca(2+)-sensitive fluorescent probe. Y-24180 (0.1-10 microM) caused a rapid and sustained [Ca(2+)](i) rise...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2003.09.033

    authors: Chao YY,Jan CR

    更新日期:2004-01-02 00:00:00

  • Citrate diminishes hypothalamic acetyl-CoA carboxylase phosphorylation and modulates satiety signals and hepatic mechanisms involved in glucose homeostasis in rats.

    abstract::The hypothalamic AMP-activated protein kinase (AMPK)/acetyl-CoA carboxylase (ACC) pathway is known to play an important role in the control of food intake and energy expenditure. Here, we hypothesize that citrate, an intermediate metabolite, activates hypothalamic ACC and is involved in the control of energy mobilizat...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2008.04.015

    authors: Cesquini M,Stoppa GR,Prada PO,Torsoni AS,Romanatto T,Souza A,Saad MJ,Velloso LA,Torsoni MA

    更新日期:2008-06-20 00:00:00

  • Fenofibrate reduces cardiac remodeling and improves cardiac function in a rat model of severe left ventricle volume overload.

    abstract:AIMS:Fenofibrate is a peroxisome proliferator-associated receptor alpha agonist (PPARα) used clinically for the management of dyslipidemia and is a myocardial fatty acid oxidation stimulator. It has also been shown to have cardiac anti-hypertrophic properties but the effects of fenofibrate on the development of eccentr...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2012.10.022

    authors: Dhahri W,Couet J,Roussel É,Drolet MC,Arsenault M

    更新日期:2013-01-17 00:00:00

  • Effect of Rp diastereoisomer of adenosine 3',5' cyclic-monophosphothioate on the cAMP-dependent relaxation of smooth muscle.

    abstract::The effect of Rp diastereoisomer of adenosine 3',5'-cyclic monophosphothioate (Rp-cAMPS) on relaxation elicited by histamine (1-100 microM), forskolin (1-60 microM), papaverine (1-100 microM), vinpocetine (1-100 microM), rolipram (0.1-1 mM), Sp-cAMPS (10-300 microM), 8-BrcAMP (10 microM - 1 mM) and 8-BrcGMP (3 microM ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(97)00589-4

    authors: Perez-Vallina JR,Revuelta MP,Cantabrana B,Hidalgo A

    更新日期:1997-01-01 00:00:00

  • Specific binding of atrial natriuretic factor to renal glomeruli during day or night antiorthostatic suspension in the rat.

    abstract::We observed a significant increase in plasma atrial natriuretic factor (ANF) in antiorthostatic hypokinetic suspension (AOH) rats after 2 h of suspension when the experiment was made during day. Plasma ANF was investigated in relation to renal glomerular ANF receptors during AOH at night. The aim of this study was 1) ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(88)80008-0

    authors: Gauquelin G,Schiffrin EL,Garcia R,Entresangles M,Cantin M,Gharib C

    更新日期:1988-01-01 00:00:00

  • Ginsenoside Rd promotes non-amyloidogenic pathway of amyloid precursor protein processing by regulating phosphorylation of estrogen receptor alpha.

    abstract:AIMS:Previous study demonstrated that Ginsenoside Rd. (GS-Rd) could improve cognitive and memory function in animal model of Alzheimer's disease. This study was aimed to investigate whether GS-Rd could improve non-amyloidogenic pathway by activating estrogen receptor (ER). MAIN METHODS:10mg/kg GS-Rd in ovariectomy (OV...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2016.11.002

    authors: Yan X,Hu G,Yan W,Chen T,Yang F,Zhang X,Zhao G,Liu J

    更新日期:2017-01-01 00:00:00

  • Activation of the NADPH oxidase in a cell-free system from human neutrophils stimulated by phorbol myristate acetate.

    abstract::Kinetics of activation of the NADPH oxidase in a fully soluble cell-free system from phorbol myristate acetate (PMA)-stimulated human neutrophils were investigated. In a cell-free system in which Mg2+ and sodium dodecyl sulfate, an anionic detergent required for the activation of NADPH oxidase are contained, cytosol p...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(90)90447-y

    authors: Umeki S

    更新日期:1990-01-01 00:00:00

  • A potent nonpeptide neuropeptide Y Y1 receptor antagonist, a benzodiazepine derivative.

    abstract::We describe here a nonpeptide neuropeptide Y Y1 receptor antagonist, 2,4-dioxo-1,5-bis(2-oxo-2-orthotolyl-ethyl)-3-[3-[3-([3-[3-(3-p iperidin-1-ylmethyl-phenoxy)-propylcarbamoyl]-propyl]-car bamoyloxymethyl)-phenyl]-ureido]-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diaz epine (Compound 1), which was previously synthesized as...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(98)00357-9

    authors: Shigeri Y,Ishikawa M,Ishihara Y,Fujimoto M

    更新日期:1998-01-01 00:00:00

  • 3-Nitroacridine derivatives arrest cell cycle at G0/G1 phase and induce apoptosis in human breast cancer cells may act as DNA-target anticancer agents.

    abstract::DNA is considered to be one of the most promising targets for anticancer agents. Acridine analogues have anticancer activity based on DNA binding and topoisomerases inhibition. However, due to the side effects, resistance and low bioavailability, a few have entered into clinical usage and the mechanisms of action are ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2018.05.010

    authors: Zhou Q,You C,Zheng C,Gu Y,Gu H,Zhang R,Wu H,Sun B

    更新日期:2018-08-01 00:00:00

  • Prolonged beta-adrenoceptor stimulation increases the amount of GDP-binding protein in brown adipose tissue mitochondria.

    abstract::Cold acclimation increases the thermogenic capacity of brown adipose tissue (BAT) and this is associated with both a general hypertrophy of the tissue and a selective increase in the proportion of a specific 32,000 molecular weight, GDP-binding protein in the mitochondrial membrane. This protein regulates the activity...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(84)90081-x

    authors: Young P,Wilson S,Arch JR

    更新日期:1984-03-19 00:00:00

  • Endurance exercise causes mitochondrial and oxidative stress in rat liver: effects of a combination of mitochondrial targeting nutrients.

    abstract:AIMS:Endurance exercise causes fatigue due to mitochondrial dysfunction and oxidative stress. In order to find an effective strategy to prevent fatigue or enhance recovery, the effects of a combination of mitochondrial targeting nutrients on physical activity, mitochondrial function and oxidative stress in exercised ra...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2009.11.003

    authors: Sun L,Shen W,Liu Z,Guan S,Liu J,Ding S

    更新日期:2010-01-02 00:00:00

  • Association between the behavioral and neurochemical effects of amphetamine: hemispheric asymmetry study.

    abstract::Effects of amphetamine on concentrations of dopamine, norepinephrine and serotonin in several monoamine-containing cell body and terminal regions were examined left and right separately in rats. Results suggest that amphetamine reduced the L-R asymmetry of most of these measures, and this effect is more significant in...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(87)90334-1

    authors: Lee EH,Huang SL,Chai CY

    更新日期:1987-04-06 00:00:00

  • Evidence that nitric oxide modulates food intake in mice.

    abstract::Nitric oxide (NO) may be an intercellular modulator within the central nervous system. L-arginine, which results in NO synthesis, increased food intake in mice while the inhibitor of NO synthesis, L-NG-nitro arginine (L-NO Arg) inhibited food intake in food deprived mice. L-arginine, but not D-arginine, partially reve...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(91)90102-h

    authors: Morley JE,Flood JF

    更新日期:1991-01-01 00:00:00

  • Effects of bilateral striatal 6-OHDA lesions on circadian rhythms in the rat: a radiotelemetric study.

    abstract::The present work aims to document, in a previously described animal model of Parkinson (double bilateral striatal injection of 6-OHDA), the possible modifications of circadian markers rhythms i.e. temperature (T), heart rate (H) and locomotor activity (A) registered continuously by telemetry, in order to evaluate a po...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(00)00751-7

    authors: Ben V,Bruguerolle B

    更新日期:2000-08-18 00:00:00

  • Isolation of anti-leukemia compounds from Citrus reticulata.

    abstract::In vitro effects of medicinal plant extracts from the pericarpium of Citrus reticulata (cv Jiao Gan) (PCRJ) on the growth and differentiation of a recently characterized murine myeloid leukemic cell clone WEHI 3B (JCS) were investigated. Extracts of PCRJ not only inhibited the proliferation of JCS cells in a dose depe...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(96)00088-4

    authors: Mak NK,Wong-Leung YL,Chan SC,Wen J,Leung KN,Fung MC

    更新日期:1996-01-01 00:00:00