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Hua Zhang, Suya Sun, Lili Wu, Ekaterina Pchitskaya, Olga Zakharova, Klementina Fon Tacer, Ilya Bezprozvanny
: Mushroom dendritic spine structures are essential for memory storage and the loss of mushroom spines may explain memory defects in aging and Alzheimer's disease (AD). The stability of mushroom spines depends on stromal interaction molecule 2 (STIM2)-mediated neuronal-store-operated Ca(2+) influx (nSOC) pathway, which is compromised in AD mouse models, in aging neurons, and in sporadic AD patients. Here, we demonstrate that the Transient Receptor Potential Canonical 6 (TRPC6) and Orai2 channels form a STIM2-regulated nSOC Ca(2+) channel complex in hippocampal mushroom spines...
November 23, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
Simona Negreş, Corina Scutari, Floriana Elvira Ionică, Veaceslav Gonciar, Bruno Ştefan Velescu, Oana Cristina Şeremet, Anca Zanfirescu, Cristina Elena Zbârcea, Emil Ştefănescu, Emilia Ciobotaru, Cornel ChiriŢă
BACKGROUND AND AIMS: Hyperforin (HY) is used to treat depression and skin irritation and has been shown a number of pharmacological activities. The literature does no cite data on changes that may occur in the body after HY intake (ethylene diammonium salt - EDS) in long-term administration. From this point of view, the present work is a key to determining the pharmacotoxicological profile of the HY-EDS, in long-term administration. MATERIALS AND METHODS: In present research, the influence of toxic doses of HY-EDS was investigated on the biochemical serum parameters and the histopathological changes in internal organs on the experimental mice model...
2016: Romanian Journal of Morphology and Embryology, Revue Roumaine de Morphologie et Embryologie
Andrea Kucharíková, Souvik Kusari, Selahaddin Sezgin, Michael Spiteller, Eva Čellárová
A plethora of plants belonging to the genus Hypericum have been investigated so far owing to the biological efficacies of pharmacologically important secondary metabolites produced by several Hypericum species. However, there is currently a dearth of information about the localization (accumulation) of these compounds in the plants in situ. In particular, the biosynthetic and ecological consequence of acclimatization of in vitro cultured Hypericum spp. to outdoor conditions is not fully known. Herein, we report an application of matrix-assisted laser desorption/ionization high-resolution mass spectrometry (MALDI-HRMS) to reveal the distribution of major naphthodianthrones hypericin, pseudohypericin, protohypericin, and their proposed precursor emodin as well as emodin anthrone, along with the phloroglucinol derivative hyperforin, the flavonoids quercetin, quercitrin, rutin and hyperoside (and/or isoquercitrin), and chlorogenic acid in Hypericum leaves...
2016: Frontiers in Plant Science
Michela Novelli, Marta Menegazzi, Pascale Beffy, Svetlana Porozov, Alex Gregorelli, Daniela Giacopelli, Vincenzo De Tata, Pellegrino Masiello
The extract of the herbaceous plant St. John's wort (SJW) and its phloroglucinol component hyperforin (HPF) were previously shown to inhibit cytokine-induced STAT-1 and NF-κB activation and prevent damage in pancreatic β cells. To further clarify the mechanisms underlying their protective effects, we evaluated the phosphorylation state of various factors of cytokine signaling pathways and the expression of target genes involved in β-cell function, inflammatory response and apoptosis induction. In the INS-1E β-cell line, exposed to a cytokine mixture with/without SJW extract (2-5μg/ml) or HPF (1-5μM), protein phosphorylation was assessed by western blotting and expression of target genes by real-time quantitative PCR...
October 22, 2016: International Journal of Biochemistry & Cell Biology
Kévin Cottet, Bin Xu, Pascale Coric, Serge Bouaziz, Sylvie Michel, Michel Vidal, Marie-Christine Lallemand, Sylvain Broussy
Natural products guttiferone A, hyperforin, and aristoforin were able to inhibit or increase SIRT1 catalytic activity, depending on protein concentration and presence of detergent. On the basis of NMR data for guttiferone A, we demonstrated that the aggregation state of the natural product played a crucial role for its interaction with the enzyme. These results are useful to interpret future in vitro structure-activity relationship studies on these natural products in the quest of their biological target(s)...
October 7, 2016: Journal of Medicinal Chemistry
Nikos Seferos, Loukas Petrokokkinos, Antonia Kotsiou, George Rallis, Christine Tesseromatis
: Stress, via corticosteroids release, influences bone mass density. Hypericum perforatum (Hp) a traditional remedy possess antidepressive activity (serotonin reuptake inhibitor) and wound healing properties. Hp preparation contains mainly hypericin, hyperforin, hyperoside and flavonoids exerting oestrogen-mimetic effect. Cold swimming represents an experimental model of stress associating mental strain and corporal exhaustion. OBJECTIVES: This study investigates the Hp effect on femur and mandible bone mass changes in rats under cold forced swimming procedure...
2016: Stomatologija
Xiaodong Yan, Juanfang Liu, Zhengxu Ye, Jinghui Huang, Fei He, Wei Xiao, Xueyu Hu, Zhuojing Luo
Electrical stimulation (ES)-triggered up-regulation of brain-derived neurotrophic factor (BDNF) and neurite outgrowth in cultured rat postnatal dorsal root ganglion neurons (DRGNs) is calcium (Ca2+)-dependent. The effects of increased Ca2+ on BDNF up-regulation and neurite outgrowth remain unclear. We showed here that ES increased phosphorylation of the cAMP-response element binding protein (CREB). Blockade of Ca2+ suppressed CREB phosphorylation and neurite outgrowth. Down-regulation of phosphorylated (p)-CREB reduced BDNF transcription and neurite outgrowth triggered by ES...
2016: PloS One
Eric A Apaydin, Alicia R Maher, Roberta Shanman, Marika S Booth, Jeremy N V Miles, Melony E Sorbero, Susanne Hempel
BACKGROUND: This systematic review evaluated St. John's wort (SJW) for the treatment of Major Depressive Disorder (MDD). The objectives of this review are to (1) evaluate the efficacy and safety of SJW in adults with MDD compared to placebo and active comparator and (2) evaluate whether the effects vary by severity of MDD. METHODS: We searched PubMed, CINAHL, PsycINFO, CENTRAL, Embase, AMED, MANTIS, Web of Science, and ICTRP and existing reviews to November 2014...
September 2, 2016: Systematic Reviews
Joseph Kwon, Kyung Seo Oh, Se-Young Cho, Mi Ae Bang, Hwan Seon Kim, Bipin Vaidya, Duwoon Kim
Hyperforin, a major active compound of St. John's wort extract, affects estrogenic activity. In this study, the compound evoked estrogen response element-dependent luciferase activity and cell proliferation in MCF-7 cells. Hyperforin-induced cell proliferation was significantly inhibited by the estrogen receptor antagonist ICI 182,780. These results suggested that hyperforin had estrogenic and cell proliferation activities, which were stimulated via the estrogen receptor. Compared to 17β-estradiol, hyperforin showed significantly lower estrogenic activity and cell proliferation...
July 25, 2016: Planta Medica
Anna Misianiková, Daniela Zubrická, Linda Petijová, Katarina Brunákova, Eva Cellárová
BACKGROUND: The increasing demand for hypericins and hyperforins, the unique pharmaceuticals found in the Hypericum genus, requires the development of effective tools for long-term storage of cells and tissues with unique biochemical profiles. OBJECTIVE: To determine the temperature of crystallization (T(C)) and of ice formation of 14 cryoprotectant mixtures (CMs) for their use in cryoprotection of H. perforatum L. cell suspensions and to evaluate the impact of the lowest Tc on post-cryogenic recovery...
May 2016: Cryo Letters
Hitesh Soni, Adebowale Adebiyi
Glomerular mesangial cell (GMC) proliferation and death are involved in the pathogenesis of glomerular disorders. The mechanisms that control GMC survival are poorly understood, but may include signal transduction pathways that are modulated by changes in intracellular Ca(2+) ([Ca(2+)]i) concentration. In this study, we investigated whether activation of the canonical transient receptor potential (TRPC) 6 channels and successive [Ca(2+)]i elevation alter neonatal GMC survival. Hyperforin (HF)-induced TRPC6 channel activation increased [Ca(2+)]i concentration, inhibited proliferation, and triggered apoptotic cell death in primary neonatal pig GMCs...
2016: Scientific Reports
Jiancheng Zhang, Chengye Yao, Jiayi Chen, Yujing Zhang, Shiying Yuan, Yun Lin
Hyperforin, the main active ingredient of the medicinal plant Hypericum perforatum, has been shown to be neuroprotective against acute ischemic stroke. However, the long-term actions of hyperforin on the post-stroke functional recovery and underlying mechanisms have not been investigated. C57BL/6 wild-type mice or interleukin (IL)-17A knock-out mice underwent middle cerebral artery occlusion (60min) followed by reperfusion for 28 days. Here, we found that delayed treatment with hyperforin significantly promoted functional recovery and increased IL-17A expression in the ischemic hemisphere at 28 days post-ischemia (dpi)...
September 1, 2016: Brain Research
M Šemeláková, R Jendželovský, P Fedoročko
Our previous results have shown that the combination of hypericin-mediated photodynamic therapy (HY-PDT) at sub-optimal dose with hyperforin (HP) (compounds of Hypericum sp.), or its stable derivative aristoforin (AR) stimulates generation of reactive oxygen species (ROS) leading to antitumour activity. This enhanced oxidative stress evoked the need for an explanation for HY accumulation in colon cancer cells pretreated with HP or AR. Generally, the therapeutic efficacy of chemotherapeutics is limited by drug resistance related to the overexpression of drug efflux transporters in tumour cells...
July 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Alexandre Bouron, Sylvain Chauvet, Stuart Dryer, Juan A Rosado
Canonical transient receptor potential 6 (TRPC6) proteins assemble into heteromultimeric structures forming non-selective cation channels. In addition, many TRPC6-interacting proteins have been identified like some enzymes, channels, pumps, cytoskeleton-associated proteins, immunophilins, or cholesterol-binding proteins, indicating that TRPC6 are engaged into macromolecular complexes. Depending on the cell type and the experimental conditions used, TRPC6 activity has been reported to be controlled by diverse modalities...
2016: Advances in Experimental Medicine and Biology
Reza Nosratabadi, Maryam Rastin, Mojtaba Sankian, Dariush Haghmorad, Mahmoud Mahmoudi
Hyperforin an herbal compound, is commonly used in traditional medicine due to its anti-inflammatory activities. The aim of this study was to use a hyperforin loaded gold nanoparticle (Hyp-GNP) to treatment of experimental autoimmune encephalomyelitis (EAE) an animal model of multiple sclerosis (MS). Hyp-GNP and hyperforin significantly reduced clinical severity of EAE, which was accompanied by a decrease in the number of inflammatory cell infiltration in the spinal cord. Additionally, treatment with Hyp-GNP significantly inhibited disease-associated cytokines as well as an increase in the anti-inflammatory cytokines in comparison to all groups including free-hyp group...
April 20, 2016: Nanomedicine: Nanotechnology, Biology, and Medicine
M K Sarath Josh, S Pradeep, Aparna K Balan, M N Sreejith, Sailas Benjamin
Phthalates are known to cause endocrine disruption in humans and animals. Being lipophilic xenobiotic chemicals, phthalates from the surrounding environments can easily be absorbed into the biological system, thereby causing various health dysfunctions. This molecular docking study evaluates a variety of molecular interactions of 12 commonly used diphthalates and respective monophthalates onto the ligand binding domain (LBD) of the human pregnane X receptor (hPXR), a xenosensor, which would be beneficial for further in vitro and in vivo studies on hazardous phthalates...
April 12, 2016: Journal of Applied Toxicology: JAT
Cuneyt Cirak, Jolita Radusiene, Valdas Jakstas, Liudas Ivanauskas, Fatih Seyis, Fatih Yayla
Context The genus Hypericum (Hypericaceae) has attracted remarkable scientific interest as its members have yielded many bioactive compounds. Objective The current study presents investigations on the accumulation of hypericin, pseudohypericin, hyperforin, adhyperforin, chlorogenic acid, neochlorogenic acid, caffeic acid, 2,4-dihydroxybenzoic acid, 13,118-biapigenin, hyperoside, isoquercitrin, quercitrin, quercetin, avicularin, rutin, (+)-catechin and (-)-epicatechin in seven Hypericum (Hypericaceae) species growing wild in Turkey, namely, H...
October 2016: Pharmaceutical Biology
Serge A T Fobofou, Katrin Franke, Andrea Porzel, Wolfgang Brandt, Ludger A Wessjohann
The chemical investigation of the chloroform extract of Hypericum lanceolatum guided by (1)H NMR, ESIMS, and TLC profiles led to the isolation of 11 new tricyclic acylphloroglucinol derivatives, named selancins A-I (1-9) and hyperselancins A and B (10 and 11), along with the known compound 3-O-geranylemodin (12), which is described for a Hypericum species for the first time. Compounds 8 and 9 are the first examples of natural products with a 6-acyl-2,2-dimethylchroman-4-one core fused with a dimethylpyran unit...
April 22, 2016: Journal of Natural Products
Lucie Hyrsova, Tomas Smutny, Alejandro Carazo, Stefan Moravcik, Jana Mandikova, Frantisek Trejtnar, Sabine Gerbal-Chaloin, Petr Pavek
BACKGROUND AND PURPOSE: The organic cation transporter 1 (OCT1) transports cationic drugs into hepatocytes. The high hepatic expression of OCT1 is controlled by the HNF4α and USF transcription factors. Pregnane X receptor (PXR) mediates induction of the principal xenobiotic metabolizing enzymes and transporters in the liver. Here, we have assessed the down-regulation of OCT1 expression by PXR activation. EXPERIMENTAL APPROACH: We used primary human hepatocytes and related cell lines to measure OCT1 expression and activity, by assaying MPP(+) accumulation...
May 2016: British Journal of Pharmacology
Mariam Gaid, Paul Haas, Till Beuerle, Stephan Scholl, Ludger Beerhues
Extracts of the medicinal plant Hypericum perforatum are used to treat depression and skin irritation. A major API is hyperforin, characterized by sensitivity to light, oxygen and temperature. Total synthesis of hyperforin is challenging and its content in field-grown plants is variable. We have established in vitro cultures of auxin-induced roots, which are capable of producing hyperforin, as indicated by HPLC-DAD and ESI-MS analyses. The extraction yield and the productivity upon use of petroleum ether after solvent screening were ∼5 mg/g DW and ∼50 mg/L culture after six weeks of cultivation...
March 20, 2016: Journal of Biotechnology
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