Abstract：
:Aim of this study was to extend the knowledge on the antineoplastic effect of aloe-emodin (AE), a natural hydroxyanthraquinone compound, both in metastatic human melanoma cell lines and in primary stem-like cells (melanospheres). Treatment with AE caused reduction of cell proliferation and induction of SK-MEL-28 and A375 cells differentiation, characterized by a marked increase of transamidating activity of transglutaminase whose expression remained unmodified. In vitro antimetastatic property of AE was evaluated by adhesion and Boyden chamber invasion assays. The effect of AE on melanoma cytokines/chemokines production was determined by a multiplex assay: interestingly AE showed an immunomodulatory activity through GM-CSF and IFN-γ production. We report also that AE significantly reduced the proliferation, stemness and invasive potential of melanospheres. Moreover, AE treatment significantly enhanced dabrafenib (a BRAF inhibitor) antiproliferative activity in BRAF mutant cell lines. Our results confirm that AE possesses remarkable antineoplastic properties against melanoma cells, indicating this anthraquinone as a promising agent for differentiation therapy of cancer, or as adjuvant in chemotherapy and targeted therapy. Further, its mechanisms of action support a potential efficacy of AE treatment to counteract resistance of BRAF-mutated melanoma cells to target therapy.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Tabolacci C,Cordella M,Turcano L,Rossi S,Lentini A,Mariotti S,Nisini R,Sette G,Eramo A,Piredda L,De Maria R,Facchiano F,Beninati Sdoi
10.1016/j.ejphar.2015.05.057subject
Has Abstractpub_date
2015-09-05 00:00:00pages
283-92eissn
0014-2999issn
1879-0712pii
S0014-2999(15)30060-1journal_volume
762pub_type
杂志文章abstract：:This study compares the membrane activity of ibutilide, d-sotalol, sematilide, E-4031 and dofetilide on single ventricular cells under identical experimental conditions. We found that ibutilide and dofetilide produced a 'bell-shaped' concentration-dependent effect on action potential duration. Ionic current measuremen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90704-l
更新日期：1993-03-30 00:00:00
abstract：:The effects of three vinca derivatives on [3H]batrachotoxin binding in rat cortical synaptosomes, on the inhibition of whole-cell Na+ currents evoked in voltage-clamped cortical neurones of the rat, on the protection against veratridine-induced cell death in cortical cultures and on the maximal electroshock-induced se...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00542-0
更新日期：1996-10-24 00:00:00
abstract：:The qualitative and quantitative effects of the (+)-S and (-)-R enantiomers and of the racemic mixture of the Ca2+ channel antagonist, nicardipine, were compared on the isolated porcine coronary artery with intact and removed endothelium. All three forms of nicardipine inhibited the contractions induced by KCl (5-90 m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00049-7
更新日期：1999-03-12 00:00:00
abstract：:Cd2+ competitively antagonizes Ca2+ in the evoked release of acetylcholine from nerve terminals in the frog sciatic-sartorius neuromuscular junction. The dissociation constant between Cd2+ and its receptor sites was calculated to be 1.7 microM. In agreement with previous work we found that brief exposures to 100-500 m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90131-6
更新日期：1984-04-06 00:00:00
abstract：:Posttraumatic nerve recovery remains a challenge in regenerative medicine. As such, there is a need for agents that limit nerve damage and enhance nerve regeneration. Here we investigate rosuvastatin, a 3-hydroxy-3-methylglutaryl coenzyme (HMG-CoA) reductase inhibitor, with anti-inflammatory and antioxidant properties...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173260
更新日期：2020-09-05 00:00:00
abstract：:The effects of (-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'- trifluoromethylpropiophenone monohydrochloride (NK433), a novel centrally acting muscle relaxant, on masticatory muscle reflexes were investigated in rats. NK433 inhibited the monosynaptic tonic vibration reflex of the masseter muscle and the polysynaptic tonic pe...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00783-0
更新日期：1996-02-29 00:00:00
abstract：:Malfunction of the serotonergic system and dysregulation of the hypothalamo-pituitary-adrenocortical axis have been implicated in the pathophysiology of depression. Several studies provide evidence for reciprocal influences between glucocorticoids and 5-HT receptors. The effect of repeated treatment with a high dose o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00286-5
更新日期：1996-07-18 00:00:00
abstract：:We studied the relationships between arachidonic acid (AA) metabolism and contractile responses to Na arachidonate (NaA) and the prostaglandins (PGs) in mesenteric arteries isolated from sham-operated and totally pancreatectomized dogs. PGE2 and PGF2 alpha produced a similar dose-dependent relaxation of mesenteric art...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90480-1
更新日期：1984-08-17 00:00:00
abstract：:Nitric oxide can exert either protective or damaging effects on the gastric mucosa. To further explore the role of nitric oxide in the modulation of gastric mucosal defense, the effects of intra-arterial administration of the precursor, L-arginine, on susceptibility of the gastric mucosa to damage induced by topically...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90018-3
更新日期：1994-07-21 00:00:00
abstract：:Salvianolate is a compound from traditional Chinese medicine widely used in the treatment of various cardiovascular diseases. This study explored the effects of salvianolate on myocardial infarction and used tandem mass tags (TMT) to discover differentially expressed proteins. Male Sprague Dawley rats were randomly di...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173610
更新日期：2020-12-15 00:00:00
abstract：:Antiepileptic and antidepressant drugs are the primary treatments for pain relief in diabetic neuropathy. Combination therapy is a valid approach in pain treatment, where a reduction of doses could reduce side effects and still achieve optimal analgesia. We examined the effects of two-drug combinations of gabapentin, ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.11.016
更新日期：2010-02-25 00:00:00
abstract：:Acetazolamide, a carbonic anhydrase inhibitor, was administered orally and subcutaneously to rats. Acetazolamide increased the gastric ulcerogenicity of indomethacin, but inhibited gastric ulcers produced by acidified aspirin. When administered alone to fasted rats, it did not produce gastric ulcers. Acetazolamide was...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90129-3
更新日期：1985-12-03 00:00:00
abstract：:Peripheral nerve injury, which gives rise to persistent chronic pain, has become an area of intense research activity, largely because it represents a disorder with a high unmet medical need. In this study, serum biomarkers of the spinal nerve ligation model were successfully investigated with the metabolomic method. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.03.079
更新日期：2009-08-01 00:00:00
abstract：:Beta2-adrenoceptor agonists are the first-line treatment of asthma and chronic obstructive pulmonary disease (COPD), in which a short-acting beta2-adrenoceptor agonist is used as required for relief of bronchoconstriction. A long-acting beta2-adrenoceptor agonist may be added to an inhaled corticosteroid as step 3 in ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2005.12.060
更新日期：2006-03-08 00:00:00
abstract：:Cats were treated for 35 days with flurazepam, 5 mg/kg per day. The drug was administered through a gastric fistula. Ro15-1788, a benzodiazepine antagonist, caused an abstinence syndrome when administered through the gastric fistula 24 h after the last dose of chronic treatment. Abstinence signs included increased mus...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90616-1
更新日期：1982-06-16 00:00:00
abstract：:CysLT1 receptors are known to be involved in the pathogenesis of asthma. However, the functional roles of CysLT2 receptors in this condition have not been determined. The purpose of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs and use this mod...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.11.036
更新日期：2017-01-05 00:00:00
abstract：:Vasoactive substances released from aggregating platelets inhibit beta-adrenergic neurotransmission in coronary arteries. Studies were carried out on the effects of two such vasoactive substances on canine coronary arteries, at concentrations equivalent to that released by platelets under physiological conditions. 5-H...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90030-6
更新日期：1987-01-20 00:00:00
abstract：:Glycine displaces [3H]CGP-39653 ([3H]D,L-(E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid) binding to the glutamate recognition site with both high and low affinity. We reported previously that chronic treatment with antidepressants reduced the proportion of high to low affinity sites, or, even eliminated the high af...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01589-6
更新日期：1998-01-26 00:00:00
abstract：:The effect and role of nitric oxide (NO) in the regulation of ion transport in the mouse cecum were investigated. L-arginine, used to increase NO production, increased short-circuit current (Isc), a measure of ion transport, in a concentration-dependent manner with a maximal increase of 193.8+/-65.5 microA/cm2. This i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00221-0
更新日期：1998-05-29 00:00:00
abstract：:The antiarrhythmic potency of procainamide (PA) and N-acetylprocainamide (NAPA) has been investigated in rabbits using isolated atrial preparations and ouabain-induced ventricular fibrillation in vivo. At concentrations in the range 3 x 10(-5) to 1 x 10(-3) M, both PA and NAPA decreased the maximum following frequency...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90373-4
更新日期：1978-01-01 00:00:00
abstract：:A specific protein kinase C inhibitor, calphostin C, which injected alone had no effect on the antinociception induced by intrathecal (i.t.) administration of a selective mu-opioid receptor agonist, [D-Ala2,NMePhe4,Gly(ol)5]enkephalin (DAMGO), dose-dependently attenuated the development of acute tolerance to the i.t. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00322-c
更新日期：1995-07-04 00:00:00
abstract：:Attempts were made to find whether [3H]batrachotoxinin A 20-alpha-benzoate provides a specific probe for measuring interactions of local anesthetics with the sodium channel complex. [3H]Batrachotoxinin A 20-alpha-benzoate binding, [14C]guanidine and 22Na uptake were investigated in rat brain crude synaptosomal prepara...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90230-x
更新日期：1986-05-27 00:00:00
abstract：:MMPT, (5-[(4-methylphenyl)methylene]-2-(phenylamino)-4(5H)-thiazolone), a thiazolidin compound, was identified in our laboratory as a novel antineoplastic agent with a broad spectrum of antitumor activity against many human cancer cells. A previous study showed that MMPT inhibited cell growth, and induced apoptosis in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.05.003
更新日期：2012-08-05 00:00:00
abstract：:Although the vasorelaxant effects of taurine have been studied in rabbit ear artery, rat isolated aorta and mesenteric artery, its pharmacological properties in other vascular beds and underlying mechanism(s) are still not well clarified. The present study was designed to observe the effects of taurine on the contract...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.10.039
更新日期：2008-02-02 00:00:00
abstract：:Receptor autoradiography was used to examine the distribution of muscarinic cholinoceptors ([3H]QNB), alpha 2-adrenoceptors ([3H]rauwolscine), beta-adrenoceptors ([125I]CYP) and substance P receptors ([125I]BHSP) in rabbit aorta, pulmonary artery, rat aorta, dog aorta, splenic, renal and coronary arteries, bovine aort...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90128-2
更新日期：1987-01-28 00:00:00
abstract：:Because of their importance in pathophysiology, the dopamine receptors have been the subjects of intense pharmacological and physiological research. Their structures have remained mostly unknown until recently with the application of molecular biological approaches. The cloning of the first dopamine receptor, the D2 r...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/0922-4106(91)90001-x
更新日期：1991-08-14 00:00:00
abstract：:The mechanisms of ryanodine-induced contractions were studied in strips of femoral arteries from spontaneously hypertensive rats (SHR) and normotensive Wistar-Kyoto rats (WKY). Ryanodine (30 nM to 30 microM) alone contracted arterial strips in a dose-dependent manner. The maximum contraction in SHR was about 5 times g...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90383-2
更新日期：1994-03-11 00:00:00
abstract：:Two highly selective mu-opioid receptor agonists, endomorphin-1 and endomorphin-2, have been identified and postulated to be endogenous ligands for mu-opioid receptors. Intrathecal (i.t.) administration of endomorphin-1 and endomorphin-2 at doses from 0.039 to 5 nmol dose-dependently produced antinociception with the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01238-9
更新日期：2001-09-21 00:00:00
abstract：:GABAA receptors are pentameric chloride ion channels that are opened by GABA. We have screened a cell line derived from human glioblastoma, U3047MG, for expression of GABAA receptor subunit isoforms and formation of functional ion channels. We identified GABAA receptors subunit α2, α3, α5, β1, β2, β3, δ, γ3, π, and θ ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.12.001
更新日期：2015-02-05 00:00:00
abstract：:Structurally diverse compounds have been shown to possess high affinities for benzodiazepine receptors in their 'diazepam-sensitive' (DS) conformations. In contrast, only the imidazobenzodiazepinone Ro 15-4513 has been shown to exhibit a high affinity for the 'diazepam-insensitive' (DI) conformation of benzodiazepine ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(92)90040-3
更新日期：1992-01-14 00:00:00
