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Imatinib reduces cholesterol uptake and matrix metalloproteinase activity in human THP-1 macrophages.
CONCLUSION: Our results indicate that imatinib causes post-translational inhibition with respect to cholesterol uptake and regulation of MMP-2 and MMP-9. More research is needed to further evaluate the role of imatinib in the regulation of other genes and processes. PMID: 26721343 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Gacic J, Vorkapic E, Olsen RS, Söderberg D, Gustafsson T, Geffers R, Skoglund K, Matussek A, Wågsäter D Tags: Pharmacol Rep Source Type: research

β-Elemene induces apoptosis of human rheumatoid arthritis fibroblast-like synoviocytes via reactive oxygen species-dependent activation of p38 mitogen-activated protein kinase.
CONCLUSIONS: Taken together, β-elemene is effective in inducing mitochondrial apoptosis of RA-FLS, which is mediated through induction of ROS formation and p38 MAPK activation. β-Elemene may thus have therapeutic benefits for RA. PMID: 26721344 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Zou S, Wang C, Cui Z, Guo P, Meng Q, Shi X, Gao Y, Yang G, Han Z Tags: Pharmacol Rep Source Type: research

Enhanced pretreatment CD25 expression on peripheral blood CD4+ T cell predicts shortened survival in acute myeloid leukemia patients receiving induction chemotherapy.
CONCLUSIONS: Our data indicate that quantification of CD25 expression on peripheral blood CD4+ T cells could become a novel, easily accessible method of shortened survival prognostication of AML patients subjected to standard cytotoxic therapy. PMID: 26721345 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Bołkun Ł, Rusak M, Eljaszewicz A, Pilz L, Radzikowska U, Łapuć I, Łuksza E, Dąbrowska M, Bodzenta-Łukaszyk A, Kłoczko J, Moniuszko M Tags: Pharmacol Rep Source Type: research

TBBPA causes neurotoxic and the apoptotic responses in cultured mouse hippocampal neurons in vitro.
CONCLUSION: We suggest that the H2DCFDA assay cannot be used to measure TBBPA-stimulated cell-mediated ROS production. PMID: 26721346 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Szychowski KA, Wójtowicz AK Tags: Pharmacol Rep Source Type: research

β-Lapachone enhances Mre11-Rad50-Nbs1 complex expression in cisplatin-induced nephrotoxicity.
CONCLUSION: Although, it remains unclear how β-lapachone induces MRN complex expression, our findings suggest that β-lapachone might affect MRN complex expression and participate in DNA damage recovery in cisplatin-induced nephrotoxicity. PMID: 26721347 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kim TW, Kim YJ, Kim HT, Park SR, Jung JY Tags: Pharmacol Rep Source Type: research

Mixed MOP/DOP agonist biphalin elicits anti-transit effect in mouse models mimicking diarrhea-predominant irritable bowel syndrome symptoms.
CONCLUSION: Biphalin is an interesting template for novel opioid-based agents to be used in therapy of functional GI diseases. PMID: 26721348 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Zielińska M, Jarmuż A, Sałaga M, Lipkowski AW, Fichna J Tags: Pharmacol Rep Source Type: research

Hydrogen sulfide inhibits endothelial nitric oxide formation and receptor ligand-mediated Ca(2+) release in endothelial and smooth muscle cells.
CONCLUSIONS: H2S antagonized Ca(2+) mobilization by receptor agonists and store-operated Ca(2+) entry thereby limiting eNOS activation and NO formation. The effect of H2S on Ca(2+) stores was not restricted to endothelial cells but was also observed in vascular and tracheal smooth muscle cells. PMID: 26721349 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kloesch B, Steiner G, Mayer B, Schmidt K Tags: Pharmacol Rep Source Type: research

Oral treatment with enrofloxacin early in life promotes Th2-mediated immune response in mice.
CONCLUSION: Our results clearly indicate that the immune system is more vulnerable to decreased bacterial exposure early in life that may promote development of allergy. PMID: 26721350 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Strzępa A, Majewska-Szczepanik M, Kowalczyk P, Woźniak D, Motyl S, Szczepanik M Tags: Pharmacol Rep Source Type: research

An antihypertensive opioid: Biphalin, a synthetic non-addictive enkephalin analog decreases blood pressure in spontaneously hypertensive rats.
CONCLUSION: Since biphalin, a non-addictive synthetic opioid, lowers MAP in SHR, a model of hypertension with pronounced neurogenic component, such analogs might find therapeutic application in human stress-induced hypertensive states. Biphalin's advantage is no associated reduction of renal perfusion. PMID: 26721351 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Bądzyńska B, Lipkowski AW, Sadowski J Tags: Pharmacol Rep Source Type: research

Caffeine augments the antidepressant-like activity of mianserin and agomelatine in forced swim and tail suspension tests in mice.
CONCLUSION: The synergistic effect of caffeine and the tested drugs may be associated with their summative actions on monoaminergic neurotransmission. Caffeine-mianserin and caffeine-agomelatine interactions might have been of pharmacodynamic origin. PMID: 26721352 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Poleszak E, Szopa A, Wyska E, Kukuła-Koch W, Serefko A, Wośko S, Bogatko K, Wróbel A, Wlaź P Tags: Pharmacol Rep Source Type: research

The anxiolytic-like activity of a novel N-cycloalkyl-N-benzoylpiperazine derivative.
CONCLUSIONS: The anxiolytic-like properties of N-bicyclo-[3.1.0]hexyl derivative (9) in the four plate test are mediated by the opioid system. The results obtained make this compound a promising lead structure for further development of anxiolytic drugs. PMID: 26721353 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Strub DJ, Sałat K, Librowski T, Lochyński S, Gaweł M, Podkowa A Tags: Pharmacol Rep Source Type: research

Epileptogenic effects of G protein-coupled estrogen receptor 1 in the rat pentylenetetrazole kindling model of epilepsy.
CONCLUSIONS: This is the first study that explores that GPER-1 receptors have epileptogenic effect on PTZ-induced kindling rat. GPER1 may mediate the epileptogenic effect of estrogens by changing the oxidative or anti-oxidative parameters in the brain. PMID: 26721354 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kurt AH, Bosnak M, Inan SY, Celik A, Uremis MM Tags: Pharmacol Rep Source Type: research

Renal vasculature reactivity to agonist of P2X7 receptor is increased in streptozotocin-induced diabetes.
CONCLUSIONS: It is possible that increased P2X7 receptor reactivity may be involved in the pathogenesis of diabetic nephropathy. PMID: 26721355 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kreft E, Kowalski R, Jankowski M, Szczepańska-Konkel M Tags: Pharmacol Rep Source Type: research

The effect of testosterone on cardiovascular risk factors in men with type 2 diabetes and late-onset hypogonadism treated with metformin or glimepiride.
CONCLUSIONS: Our results suggest that testosterone may bring more clinical benefits to metformin- than sulfonylurea-treated men with diabetes and LOH. PMID: 26721356 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Krysiak R, Gilowski W, Okopień B Tags: Pharmacol Rep Source Type: research

Stimulation of the metabotropic glutamate (mGlu) 2 receptor attenuates the MK-801-induced increase in the immobility time in the forced swimming test in rats.
CONCLUSIONS: The present results suggest that stimulation of the mGlu2 receptor attenuates the increase in the immobility time in the forced swimming test elicited by subchronic administration of MK-801, and may be potentially useful for treatment of the negative symptoms of schizophrenia. PMID: 26721357 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kawaura K, Karasawa J, Hikichi H Tags: Pharmacol Rep Source Type: research

Ameliorative potential of pioglitazone and ceftriaxone alone and in combination in rat model of neuropathic pain: Targeting PPARγ and GLT-1 pathways.
CONCLUSION: Based on these results we propose that possible interplay between the neuroprotective effects of pioglitazone and ceftriaxone exists in suppressing the behavioral, biochemical, mitochondrial, neuroinflammatory and apoptotic cascades in spinal nerve ligation induced neuropathic pain in rats. PMID: 26721358 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Pottabathini R, Kumar A, Bhatnagar A, Garg S, Ekavali E Tags: Pharmacol Rep Source Type: research

In vivo protective effect of betulinic acid on dexamethasone induced thymocyte apoptosis by reducing oxidative stress.
CONCLUSIONS: These findings reveal a protective capability of BA against Dex-induced cell death by reducing oxidative stress via mitochondrial mediated signal pathway which could be the potential mechanism underlying BA-elicited immunomodulation. PMID: 26721359 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Yi J, Zhu R, Wu J, Wu J, Xia W, Zhu L, Jiang W, Xiang S, Tan Z Tags: Pharmacol Rep Source Type: research

Nuclear factor E2-related factor-2 (Nrf2) expression and regulation in male reproductive tract.
CONCLUSIONS: Components of the Nrf2/NRF2 system along with coordinated genes are expressed in testis and epididymis. Moreover, some interspecies differences between rat and human were observed, which may impact extrapolation of experimental data into clinical findings. Studies on animal model showed that corpus of epididymis is the most responsive part of the male reproductive tract to oltipraz exposure at the gene expression level. PMID: 26721360 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Wajda A, Łapczuk J, Grabowska M, Słojewski M, Laszczyńska M, Urasińska E, Droździk M Tags: Pharmacol Rep Source Type: research

Hypoestrogenism alters mood: Ketamine reverses depressive-like behavior induced by ovariectomy in rats.
CONCLUSION: Similar to the literature, we showed the antidepressant effect of ketamine in depressive female rats which was induced by ovariectomy; including in female rats submitted to sham surgery that interestingly presented a premature menopausal. PMID: 26721361 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: da Silva Moreira SF, Nunes EA, Kuo J, de Macedo IC, Muchale A, de Oliveira C, Scarabelot VL, Marques Filho PR, Medeiros LF, Caumo W, Torres IL Tags: Pharmacol Rep Source Type: research

The effect of combined treatment with escitalopram and risperidone on the MK-801-induced changes in the object recognition test in mice.
CONCLUSIONS: The obtained results suggest that escitalopram may enhance the antipsychotic-like effect of risperidone in the animal tests used for evaluation of some cognitive symptoms of schizophrenia. PMID: 26721362 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Rogóż Z, Kamińska K Tags: Pharmacol Rep Source Type: research

ET-1 mediates the release of reactive oxygen species and TNF-α in lung tissue by protein kinase C α and β1.
CONCLUSION: Endothelin-1 induces ROS generation, increases TNF-α level and lung edema via activation of PKC αβ1. PMID: 26721363 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Gorąca A, Kleniewska P, Skibska B Tags: Pharmacol Rep Source Type: research

Therapeutic strategies for Alzheimer's disease in clinical trials.
This article presents current directions in the search for novel, potentially effective agents for the treatment of AD, as well as selected promising treatment strategies. These include agents acting upon the beta-amyloid, such as vaccines, antibodies and inhibitors or modulators of γ- and β-secretase; agents directed against the tau protein as well as compounds acting as antagonists of neurotransmitter systems (serotoninergic 5-HT6 and histaminergic H3). Ongoing clinical trials with Aβ antibodies (solanezumab, gantenerumab, crenezumab) seem to be promising, while vaccines against the tau protein (AADvac1 and ACI-35) ar...
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Godyń J, Jończyk J, Panek D, Malawska B Tags: Pharmacol Rep Source Type: research

A neutral effect of testosterone therapy on macroprolactin content in men with macroprolactinemia and late-onset hypogonadism.
CONCLUSIONS: Our results suggest a negligible effect of testosterone replacement on macroprolactin levels in macroprolactinemic men with late-onset hypogonadism. PMID: 26721365 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Krysiak R, Kowalska B, Szkróbka W, Okopień B Tags: Pharmacol Rep Source Type: research

Pioglitazone, an anti-diabetic drug requires sustained MAPK activation for its anti-tumor activity in MCF7 breast cancer cells, independent of PPAR-γ pathway.
CONCLUSIONS: Pio suppresses the proliferation of MCF7 cells, at least partly by a PPAR-γ-independent mechanism involving the induction of p21 which in turn requires sustained activation of MAPK. These findings implicate the utility of Pio in the treatment of PPAR positive or negative human cancers and the development of a new class of compounds to enhance the effectiveness of Pio. PMID: 26721366 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Kole L, Sarkar M, Deb A, Giri B Tags: Pharmacol Rep Source Type: research

Alzheimer-associated presenilin 2 gene is dysregulated in rat medial temporal lobe cortex after complete brain ischemia due to cardiac arrest.
CONCLUSIONS: Thus, presented changes suggest that the significant dysregulation of presenilin 2 gene may be connected with a response of neuronal cells to transient global brain ischemia due to cardiac arrest. Finally, the ischemia-induced gene dysregulation may play a key role in the late onset of Alzheimer's-type dementia. PMID: 26721367 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Pluta R, Kocki J, Ułamek-Kozioł M, Bogucka-Kocka A, Gil-Kulik P, Januszewski S, Jabłoński M, Petniak A, Brzozowska J, Bogucki J, Furmaga-Jabłońska W, Czuczwar SJ Tags: Pharmacol Rep Source Type: research

Ethylene glycol ethers induce apoptosis and disturb glucose metabolism in the rat brain.
CONCLUSIONS: It can be concluded that chronic treatment with BE and PHE induced mitochondrial pathway of apoptosis, and disturbed glucose metabolism in the rat brain. PMID: 26721368 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Pomierny B, Krzyżanowska W, Niedzielska E, Broniowska Ż, Budziszewska B Tags: Pharmacol Rep Source Type: research

Estimation of oxidative stress parameters in rats after simultaneous administration of rosuvastatin with antidepressants.
CONCLUSIONS: The observed changes may indicate an increased activity of the enzyme system preventing oxidation, which appears to be the effect of the reaction on the severity of oxidative stress during the combined treatment with rosuvastatin and antidepressants. PMID: 26721369 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Herbet M, Izdebska M, Piątkowska-Chmiel I, Poleszak E, Jagiełło-Wójtowicz E Tags: Pharmacol Rep Source Type: research

Effects of ketamine administration on the phosphorylation levels of CREB and TrKB and on oxidative damage after infusion of MEK inhibitor.
CONCLUSION: Ketamine's effects on pCREB, pTrKB, and oxidative stress are mediated, at least in part, by a mechanism dependent of MAPK signaling inhibition. PMID: 26721370 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Réus GZ, Abaleira HM, Titus SE, Arent CO, Michels M, da Luz JR, Dos Santos MA, Carlessi AS, Matias BI, Bruchchen L, Steckert AV, Ceretta LB, Dal-Pizzol F, Quevedo J Tags: Pharmacol Rep Source Type: research

The effect of fenofibrate on cardiometabolic risk factors in bromocriptine-treated women with mixed dyslipidemia: A pilot study.
CONCLUSIONS: Our study shows that the effect of fenofibrate on plasma lipids and circulating levels of cardiometabolic risk factors may be potentiated by bromocriptine treatment. They also suggest that hyperprolactinemic women with mixed dyslipidemia and early glucose metabolism abnormalities may receive the greatest benefits from concomitant treatment with a fibrate and bromocriptine. PMID: 26721371 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Krysiak R, Okrzesik J, Szkrobka W, Okopień B Tags: Pharmacol Rep Source Type: research

Pre- and post-exposure talampanel (GYKI 53773) against kainic acid seizures in neonatal rats.
CONCLUSION: The present results suggested that talampanel is protective in kainic acid-induced neonatal status epilepticus model; however, the time of administration is a crucial factor in determining its effectiveness. PMID: 26721372 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Dhir A, Chavda V Tags: Pharmacol Rep Source Type: research

The effect of testosterone on cardiometabolic risk factors in atorvastatin-treated men with late-onset hypogonadism.
CONCLUSIONS: Our study may suggest the clinical benefits associated with combination therapy with a statin and testosterone in elderly men with LOH. PMID: 26721373 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Krysiak R, Gilowski W, Okopień B Tags: Pharmacol Rep Source Type: research

Cyclosporine-A, but not tacrolimus significantly increases reactivity of vascular smooth muscle cells.
CONCLUSION: Our results strongly support the idea that main difference between effects on smooth muscle contractility of calcineurin-dependent immunosuppressants: CsA and tacrolimus is related to the different level of extracellular calcium influx to the cytoplasm. The elucidation of these mechanisms may permit the identification of new therapeutic strategies against CsA-induced hypertension. PMID: 26721374 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Grześk E, Malinowski B, Wiciński M, Szadujkis-Szadurska K, Sinjab TA, Manysiak S, Tejza B, Słupski M, Odrowąż-Sypniewska G, Grześk G Tags: Pharmacol Rep Source Type: research

Treatment with a carbon monoxide-releasing molecule (CORM-2) inhibits neuropathic pain and enhances opioid effectiveness in rats.
CONCLUSIONS: Our data suggest that P2X4 receptors play a significant role in neuropathic pain development, suggesting that their blockade may have potential therapeutic utility. PMID: 26721375 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - January 13, 2016 Category: Drugs & Pharmacology Authors: Jurga AM, Piotrowska A, Starnowska J, Rojewska E, Makuch W, Mika J Tags: Pharmacol Rep Source Type: research

Cancer Chemoprevention with Korean Angelica: Active Compounds, Pharmacokinetics, and Human Translational Considerations.
Abstract Angelica gigas Nakai (AGN) is a major medicinal herb used in Korea and several other Asian countries. Traditionally, its dried root has been used to treat anemia, pain, infection and articular rheumatism, most often through boiling in water to prepare the dosage forms. AGN extract or AGN-containing herbal mixtures are sold in the US and globally as dietary supplements for pain killing, memory enhancement and post-menopausal symptom relief. Decursin (D) and its isomer decursinol angelate (DA) are the major chemicals in the alcoholic extracts of the root of AGN. The anti-cancer activity of AGN alcoholic extr...
Source: Pharmacological Reports - December 1, 2015 Category: Drugs & Pharmacology Authors: Lü J, Zhang J, Li L, Jiang C, Xing C Tags: Curr Pharmacol Rep Source Type: research

Extracting the Benefit of Nexrutine(®) for Cancer Prevention.
Abstract The current standard of care for prostate cancer includes hormone therapy, radiation therapy and radical prostatectomy, each with its own set of undesirable side effects. In this regard there is an unmet need to develop strategies that can prevent or delay the development of clinical prostate cancer. One potential area involves the use of natural compounds involving botanicals. Along these lines we have found that Nexrutine(®), a dietary supplement derived from Phellodendron amurense bark extract, has prostate cancer prevention activity. The "extract" nature of this botanical, which constitutes a blend of...
Source: Pharmacological Reports - November 7, 2015 Category: Drugs & Pharmacology Authors: Hussain SS, Patel D, Ghosh R, Kumar AP Tags: Curr Pharmacol Rep Source Type: research

Retinoid Chemoprevention: Who Can Benefit?
Abstract Acute promyelocytic leukemia (APL) is a treatment success story. From a highly deadly disease it was turned into a highly curable disease by the introduction of differentiation-induction therapy with all-trans retinoic acid (ATRA) in the 1990's. During the last quarter of century, ATRA and other retinoids were used for the treatment and prevention of other cancers and even other diseases. The results were less spectacular, but nevertheless important. Progress has been made toward understanding the mechanism of action of retinoids in different physiological and pathological contexts. For some diseases, spec...
Source: Pharmacological Reports - November 7, 2015 Category: Drugs & Pharmacology Authors: Bunaciu RP, Yen A Tags: Curr Pharmacol Rep Source Type: research

Inhibition of voltage-gated Na(+) channels by hinokiol in neuronal cells.
CONCLUSION: Our results therefore suggest hinokiol inhibited VGSC in a closed-channel block manner and such inhibition involved intensification of channel inactivation. PMID: 26481521 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Wang YW, Yang CT, Gong CL, Chen YH, Chen YW, Wu KC, Cheng TH, Kuo YH, Chen YF, Leung YM Tags: Pharmacol Rep Source Type: research

Molecular identification of P2X receptors in vascular smooth muscle cells from rat anterior, posterior, and basilar arteries.
CONCLUSIONS: Our work therefore identified that in major arteries of rat cerebral circulation VSMCs express only P2X1 and P2X4 receptors subunits. We can propose that these P2X receptor subunits participate in functional P2X receptor structures mediating ATP-evoked stimulatory responses in cerebral vascular myocytes in vivo. PMID: 26481522 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Harhun MI, Sukhanova K, Gordienko D, Dyskina Y Tags: Pharmacol Rep Source Type: research

Protective effect of gallic acid against bleomycin-induced pulmonary fibrosis in rats.
CONCLUSION: Results of the present study demonstrate that GA, by its antioxidant properties, attenuates oxidative damage and fibrosis induced by BLM. Thus, an effective supplement with GA as an adjuvant therapy may be a very promising compound in reducing the side effects of BLM. PMID: 26481523 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Nikbakht J, Hemmati AA, Arzi A, Mansouri MT, Rezaie A, Ghafourian M Tags: Pharmacol Rep Source Type: research

Targeting aberrant cancer metabolism - The role of sirtuins.
Abstract Cancer cells, as opposed to normal cells, generate energy by increasing aerobic glycolysis, which is a phenomenon called "the Warburg effect". An altered energy metabolism supporting continuous cell growth and proliferation was pointed to as the new "hallmark" of cancer cells. Several hypotheses have been proposed to explain the maintenance of this seemingly wasteful catabolic state. The epigenetic mechanisms which depend on the covalent modifications of both DNA and histones have recently emerged as important players in the regulation of glucose metabolism. The sirtuin family of histone deacetylases has e...
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Kleszcz R, Paluszczak J, Baer-Dubowska W Tags: Pharmacol Rep Source Type: research

In vitro studies of antifibrotic and cytoprotective effects elicited by proto-berberine alkaloids in human dermal fibroblasts.
CONCLUSIONS: Due to its irritant effects and the lack of desired properties, coptisine has low exploitation potentialities. The other proto-berberine alkaloids investigated resulted all endowed with activities for which they can be exploited as antifibrotic and cytoprotective agents. Stylopine globally proved to be the most promising compound, being endowed with revitalizing, anti-inflammatory, antifibrotic and wound-healing promoting activities, and showing no toxic effects. PMID: 26481525 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Pietra D, Borghini A, Bianucci AM Tags: Pharmacol Rep Source Type: research

Naringenin protects cardiac hypercholesterolemia-induced oxidative stress and subsequent necroptosis in rats.
CONCLUSIONS: Our results show that the co-administration of NGEN (50mg/kg/bw) in HCD rats improved all the altered parameters and provided insight into a possible molecular mechanism underlying NGEN suppression of necroptosis pathway in the heart. PMID: 26481526 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Chtourou Y, Slima AB, Makni M, Gdoura R, Fetoui H Tags: Pharmacol Rep Source Type: research

Current approach for detection of sub-clinical left ventricular dysfunction associated with chemotherapy.
Abstract The article describes the current knowledge concerning approaches for detection of sub-clinical left ventricular dysfunction associated with chemotherapy. The authors focused on the problem of defining cardiotoxicity as well as diagnostic methods, which may be useful in predicting the occurrence of such complications. Currently, cardiac biomarkers measurement (troponin, NT-proBNP), tissue Doppler-based strain imaging and peak systolic longitudinal strain rate are most useful for detection of early myocardial changes during therapy, whereas speckle tracking echocardiography (STE) and peak systolic global lo...
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Korzeniowska K, Jankowski J, Cieślewicz A, Jabłecka A Tags: Pharmacol Rep Source Type: research

A ground state of PPARγ activity and expression is required for appropriate neural differentiation of hESCs.
CONCLUSIONS: We conclude that a ground state of PPARγ activity is required for NP formation of hESCs during early neural differentiation. However, high expression and activity of PPARγ could not enhance the required neural differentiation, whereas the PPARγ inactivation could negatively influence NP formation from hESCs by antagonist. PMID: 26481528 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Taheri M, Salamian A, Ghaedi K, Peymani M, Izadi T, Nejati AS, Atefi A, Nematollahi M, Ahmadi Ghahrizjani F, Esmaeili M, Kiani Esfahani A, Irani S, Baharvand H, Nasr-Esfahani MH Tags: Pharmacol Rep Source Type: research

Knockdown of AKT3 and PI3KCA by RNA interference changes the expression of the genes that are related to apoptosis and autophagy in T98G glioblastoma multiforme cells.
CONCLUSIONS: Thus, there is a high probability that the knockdown of these genes induces apoptosis and autophagy in T98G cells, but further studies are necessary in order to clarify and check whether autophagy induction is a positive phenomenon for the treatment of GBM. PMID: 26481529 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Paul-Samojedny M, Pudełko A, Kowalczyk M, Fila-Daniłow A, Suchanek-Raif R, Borkowska P, Kowalski J Tags: Pharmacol Rep Source Type: research

Valproic acid (VPA) reduces sensorimotor gating deficits and HDAC2 overexpression in the MAM animal model of schizophrenia.
CONCLUSIONS: Prenatal MAM administration impaired histone acetylation in the mPFC, which might be involved in the development of some of the neurobehavioral deficits (i.e., sensorimotor gating deficits) associated with schizophrenia. Blockade of HDAC2 might prevent the disruption of sensorimotor gating in adulthood. PMID: 26481530 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Bator E, Latusz J, Radaszkiewicz A, Wędzony K, Maćkowiak M Tags: Pharmacol Rep Source Type: research

Decrease of interleukin (IL)17A gene expression in leucocytes and in the amount of IL-17A protein in CD4+ T cells in children with Down Syndrome.
CONCLUSIONS: Our data indicate that decreased IL-17A expression may play a significant role in the etiology of infections in Down Syndrome. Moreover, we demonstrated that in Down Syndrome the other gene located outside the extra chromosome 21 is also affected. PMID: 26481531 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Jakubiuk-Tomaszuk A, Sobaniec W, Rusak M, Poskrobko E, Nędzi A, Olchowik B, Galicka A Tags: Pharmacol Rep Source Type: research

Up-regulation of the GPR39 Zn(2+)-sensing receptor and CREB/BDNF/TrkB pathway after chronic but not acute antidepressant treatment in the frontal cortex of zinc-deficient mice.
CONCLUSIONS: The present study for the first time demonstrates the up-regulation of GPR39 (and CREB, BDNF, and TrkB) protein when induced by chronic treatment with antidepressants (with different pharmacological profiles) in a zinc-deficiency model in mice. These data further indicate that the GPR39 receptor may be an important target in the antidepressant response. PMID: 26481532 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Młyniec K, Nowak G Tags: Pharmacol Rep Source Type: research

Interactions between an antidepressant reboxetine and four classic antiepileptic drugs in the mouse model of myoclonic seizures.
CONCLUSION: If further research confirms the obtained results, reboxetine may be categorized as an antidepressant which can be safely administered to epileptic patients treated with valproate, phenobarbital, ethosuximide or clonazepam. PMID: 26481533 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Popławska M, Wróblewska D, Borowicz KK Tags: Pharmacol Rep Source Type: research

Icariin regulates PRMT/ADMA/DDAH pathway to improve endothelial function.
CONCLUSIONS: The present results suggest that icariin regulates PRMT/ADMA/DDAH pathway to improve endothelial function. PMID: 26481534 [PubMed - in process] (Source: Pharmacological Reports)
Source: Pharmacological Reports - October 24, 2015 Category: Drugs & Pharmacology Authors: Xiao HB, Liu ZK, Lu XY, Deng CN, Luo ZF Tags: Pharmacol Rep Source Type: research