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Polyunsaturated Alkamides (1):
Recent article
Polyunsaturated Alkamides
Abstract
We propose a reconsideration of the dogma that endocannabinoids are exclusively synthesized and released 'on demand', and suggest that their metabolic control is complemented by intracellular trafficking and storage in specific reservoirs.
Copyright © 2010 Elsevier Ltd. All rights reserved....
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PMID: 20570522
PDF is available here.
PDF is available here.
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Abstract
We discuss recent progress in the studies on the enzymes involved in the biosynthesis and degradation of NAEs with special reference to NAAA.
Copyright © 2010 Elsevier Ltd. All rights reserved....
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PMID: 20152858
PDF is available here.
PDF is available here.
Abstract
We measured circulating OEA, AEA and 2-AG in patients with sleep apnea (n = 20) and healthy control subjects (n = 57). Respiratory distress index (RDI) as measured by polysomnography was used as a quantitative index of sleep apnea.
In patients with sleep apnea OEA serum concentrations were significa...
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PMID: 20429051
PDF is available here.
PDF is available here.
Abstract
We explored the potential role of transient receptor potential (TRP) channels in this process. Previously, we observed that after metabolism AEA and arachidonic acid (ArA) can be recycled into new endocannabinoid molecules. Consistent with these previous findings, we found that Cath.a differentiated...
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PMID: 20466028
PDF is available here.
PDF is available here.
Abstract
The intestinal hormone cholecystokinin (CCK) inhibits food intake via stimulation of vagal afferent neurons (VAN). Recent studies suggest that CCK also regulates the expression of some G protein-coupled receptors and neuropeptide transmitters in these neurons. The aim of the present study was to cha...
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PMID: 20430875
PDF is available here.
PDF is available here.
Abstract
We studied whether activation of the CB1 receptor resulted in reduced TRPV1-mediated responses in cultured rat primary sensory neurons. We found that TRPV1-mediated whole-cell currents were significantly reduced respectively, by 50% and 25% by 10 nM and 30 nM of the endogenous CB1 receptor agonist,...
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PMID: 20511124
PDF is available here.
PDF is available here.
YAKUGAKU ZASSHI (130)6 2010
Abstract
Eighty percent (80%) aqueous acetone extract from fruit of Piper chaba (Piperaceae) was found to have a hepatoprotective effect on D-galactosamine (D-GalN)/lipopolysaccharide (LPS)-induced liver injury in mice. Among the isolates, several amide constituents inhibited D-GalN/tumor necrosis factor-alp...
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PMID: 20519856
PDF is available here.
PDF is available here.
Abstract
We investigated a series of isoflavones with respect to their abilities to inhibit FAAH.
In vitro assays of FAAH activity and affinity for CB receptors were used to characterize key compounds. In vivo assays used were biochemical responses to formalin in anaesthetized mice and the 'tetrad' test for...
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PMID: 20590565
PDF is available here.
PDF is available here.
Abstract
We demonstrate a divergent regulation of the two endocannabinoid ligands, N-arachidonylethanolamine (anandamide; AEA) and 2-arachidonoylglycerol (2-AG), following repeated stress such that AEA content is persistently decreased throughout the corticolimbic stress circuit, whereas 2-AG is exclusively...
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PMID: 20439721
PDF is available here.
PDF is available here.
Psychopharmacology (209)2 2010
Abstract
Dopamine does not play a major role in THC discrimination. However, activation of the dopaminergic system positively modulates the discriminative effects of THC, possibly through D(2)-induced elevations in brain levels of anandamide....
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PMID: 20179908
PDF is available here.
PDF is available here.
Abstract
Pellitorine (1), which was isolated from the roots of Piper nigrum, showed strong cytotoxic activities against HL60 and MCT-7 cell lines. Microbial transformation of piperine (2) gave a new compound 5-[3,4-(methylenedioxy)phenyl]-pent-2-ene piperidine (3). Two other alkaloids were also found from Pi...
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PMID: 20428051
PDF is available here.
PDF is available here.
Abstract
We explored the pharmacology of TRPV1-induced cytotoxicity in a homogeneous, neurone-like cellular environment.
Cell death was examined in a human neurone-like cell line, stably expressing recombinant human TRPV1. Cytotoxicity was quantified in terms of nuclear morphology and mitocho...
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PMID: 20354008
PDF is available here.
PDF is available here.
Abstract
The present study aimed to investigate standardized ethanol extracts of fruit and leaves of Piper sarmentosum for their in vivo antioxidant activity in rats using a CCl (4)-induced oxidative stress model. The standardization was based on the quantification of the markers pellitorine, sarmentine and...
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PMID: 19862670
PDF is available here.
PDF is available here.
Zhonghua gan zang bing za zhi = Zhonghua ganzangbing zazhi = Chinese journal of hepatology (18)3 2010
Abstract
The FAAH, CB1 and CB2 receptor proteins were observed both in cytoplasm and on membrane in L02 and HepG2 cells. The expression level of FAAH protein was higher in HepG2 than in L02 cells. The expression level of CB1 receptor protein was very low in both L02 and HepG2 cells. The expression level of C...
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PMID: 20380798
PDF is available here.
PDF is available here.
Abstract
Recently, numerous medicinal plants possessing profound central nervous system effects and antioxidant activity have received much attention as food supplement to improve cognitive function against cognitive deficit condition including in Alzheimer's disease condition. Based on this information, the...
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PMID: 20034530
PDF is available here.
PDF is available here.
Pharmaceutical Biology (48)2 2010
Abstract
Heliopsis longipes S.F. Blake (Asteraceae: Heliantheae) (chilcuague) is used in Mexican traditional medicine against parasites and to alleviate tooth and muscle pains. Its biocide effect has already been experimentally demonstrated; however, its analgesic action and its action on the nervous system...
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PMID: 20645840
PDF is available here.
PDF is available here.
Abstract
We have made an attempt to clarify the extent to which, these channels are involved in such mechanisms using in vitro model of isolated rabbit carotid body. Selective TASK-1 channel blocker, anandamide (3 microM) induced stimulation of the carotid sinus nerve (CSN) activity, in a very similar patter...
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PMID: 20217348
PDF is available here.
PDF is available here.
Abstract
Synthetic metalloporphyrins, in the presence of monooxygen donors, are known to mimetize various reactions of cytochrome P450 enzymes systems in the oxidation of drugs and natural products. The oxidation of piperine and piplartine by iodosylbenzene using iron(III) and manganese(III) porphyrins yield...
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PMID: 20460777
PDF is available here.
PDF is available here.
Current Medicinal Chemistry (17)14 2010
Abstract
In the late 1990's, a series of experiments carried out independently in two laboratories led to establish an important connection between the function of the endocannabinoids, which, as exemplified in this special issue, is per se very complex and ubiquitous in animals, and that of the transient re...
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PMID: 20166923
PDF is available here.
PDF is available here.
Current Medicinal Chemistry (17)14 2010
Abstract
The cannabinoid CB1 and CB2 receptors are Class A G protein-coupled receptors (GPCRs). While many Class A GPCRs have endogenous ligands that are hydrophilic cations (e.g., the serotonin and dopamine receptors), the cannabinoid receptors have neutral, highly lipophilic ligands derived from the fatty...
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PMID: 20166921
PDF is available here.
PDF is available here.
Bratislavske lekarske listy (111)8 2010
Abstract
The presented study is aimed on exploring the effects of black pepper on blood pressure in the rat model of experimental hypertension induced by chronic NO synthesis inhibition.
Piperine, the compound of black pepper, can cause a significant decrease of blood pressure in normotensive rats possibly v...
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PMID: 21033621
PDF is available here.
PDF is available here.
Abstract
The therapeutic potential of cannabinoids has been the topic of extensive investigation following the discovery of cannabinoid receptors and their endogenous ligands. Cannabinoid receptors and their endogenous ligands are present at supraspinal, spinal and peripheral levels. Cannabinoids suppress be...
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PMID: 19839937
PDF is available here.
PDF is available here.
Abstract
Abstract
In cardiac papillary muscles, anandamide (1, 10, 100 nM) decreased AP duration in a concentration-dependent manner. Furthermore, 100 nM anandamide decreased AP amplitude, overshoot and Vmax in partially depolarized papillary muscles. These effects were abolished by AM251 (100 nM), a selective antago...
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PMID: 20050190
PDF is available here.
PDF is available here.
Abstract
We demonstrate antineoplastic activity of asukamycin. It inhibited cell growth at concentrations similar to other members of the manumycin family (IC50 1-5 microM). Cytotoxicity of asukamycin was accompanied by activation of caspases 8 and 3 and was diminished by SB 202190, a specific p38 mitogen-ac...
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PMID: 19787206
PDF is available here.
PDF is available here.
Abstract
We demonstrate that undeca-2E-ene-8,10-diynoic acid, an Echinacea angustifolia-derived alkylamide lacking affinity for the CB2 receptor, inhibits IL-2 secretion in Jurkat T cells through PPARgamma activity at low micromolar concentrations (330 ng/mL). The IL-2 inhibition is reversed by the addition...
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PMID: 19712756
PDF is available here.
PDF is available here.
Abstract
In the field of phytopharmaceuticals efficient and eco-friendly extraction processes are still a goal to be achieved. Extraction with Gelucire 44/14 could be a potential method of extraction for phytopharmaceuticals. Compared with conventional methods of extraction it is more efficient, easier to pr...
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PMID: 19703367
PDF is available here.
PDF is available here.
Abstract
We synthesized 18 aryl analogues of anandamide, FAAH's endogenous substrate, and in vitro evaluated their potential as metabolic trapping tracers. Interaction studies with recombinant FAAH revealed good to very good interaction of the methoxy substituted aryl anandamide analogues 17, 18, 19, and 20...
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PMID: 19719235
PDF is available here.
PDF is available here.
European Journal of Pharmacology (615)1-3 2009
Abstract
Primarily, rats have served as subjects in Delta(9)-tetrahydrocannabinol's (THC) discrimination studies although other species such as monkeys and pigeons have been used. While the introduction of the knockout and transgenic mice has vastly stimulated the study of the discriminative stimulus effects...
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PMID: 19470387
PDF is available here.
PDF is available here.
Abstract
We show that ethanolic E. purpurea radix and herba extracts produce synergistic pharmacological effects on the endocannabinoid system in vitro. Superadditive action of N-alkylamide combinations was seen at the level of intracellular calcium release as a function of CB2 receptor activation. Likewise,...
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PMID: 19303464
PDF is available here.
PDF is available here.
Abstract
We demonstrated that the antidepressant-like effects of piperine and its mechanisms might be involved by up-regulation of the progenitor cell proliferation of hippocampus and cytoprotective activity....
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PMID: 19777847
PDF is available here.
PDF is available here.
Abstract
I antagonist could block the effect of LPS (P < 0.001). This endotoxin inhibited anandamide uterine degradation (P < 0.05) and increased the expression of one of its synthesizing enzymes (P < 0.05). Contrary to the known anti-inflammatory and protective effects, in this model anandamide seems to act...
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PMID: 19490788
PDF is available here.
PDF is available here.
Journal of Hypertension (27)6 2009
Abstract
Plasma levels of AEA, CGRP, asymmetric dimethylarginine (ADMA) and nitric oxide in patients with essential hypertension, spontaneously hypertensive rats (SHRs) and 2 kidney 1 clip hypertensive rats and the CGRP mRNA expression in dorsal root ganglion of rats were measured. Peripheral blood lymphocyt...
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PMID: 19462497
PDF is available here.
PDF is available here.
Psychopharmacology (203)2 2009
Abstract
Dose-generalization curves of AM1346, Delta(9)-THC, and mAEA suggested the following order of potency: Delta(9)-THC > AM1346 > mAEA both for rats discriminating between 3 and 5.6 mg/kg AM1346 from vehicle. In group 3 mg/kg, challenge by 1 mg/kg rimonabant resulted in parallel shifts to the right of...
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PMID: 18521574
PDF is available here.
PDF is available here.
Psychopharmacology (203)2 2009
Abstract
Rimonabant can produce surmountable antagonism of the behavioral effects of not only Delta(9)-THC but also anandamide, methanandamide, and ACPA, and the interactions appear simple, competitive, and reversible. These cannabinoid agonists act at the same receptors to produce discriminative stimulus ef...
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PMID: 18592221
PDF is available here.
PDF is available here.
Abstract
Endocannabinoids, such as anandamide and 2-arachidonoylglycerol, are synthesized from membrane phospholipids in the heart and other cardiovascular tissues. They activate cannabinoid CB1 and CB2 receptors, transient receptor potential V1 (TRPV1), peroxisome proliferator-activated receptors, and perha...
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PMID: 19276990
PDF is available here.
PDF is available here.
Diabetologia (52)4 2009
Abstract
We revealed an increase of CB1R protein in SkM during differentiation. Twenty-four hour incubation of SkM with CM or AEA impaired insulin-stimulated Akt(Ser473) phosphorylation by 60% and up to 40%, respectively. Pretreatment of cells with Rim or AM251 reduced the effect of CM by about one-half, whi...
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PMID: 19089403
PDF is available here.
PDF is available here.
Journal of Neurochemistry (109)2 2009
Abstract
We examined the role of two endocannabinoids, anandamide (AEA) and N-arachidonoyldopamine (NADA) in the regulation of prostaglandin E(2) (PGE(2)) synthesis in primary glial cells. We show that NADA is a potent inhibitor of PGE(2) synthesis in lipopolysaccharide (LPS) stimulated cells, without modify...
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PMID: 19200337
PDF is available here.
PDF is available here.
Abstract
The results suggest that the therapeutic mechanism by which piperine effectively treats asthma is based on a reduction of Th2 cytokines (interleukin-4, interleukin-5), eosinophil infiltration, and by marked reduction of thymus and activation regulated chemokine, eotaxin-2 and interleukin-13 mRNA exp...
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PMID: 19222908
PDF is available here.
PDF is available here.
Abstract
We used the rat hippocampal slice preparation to study and compare the effect of various synthetic and endogenous CB1 ligands on excitatory synaptic transmission. The full CB1 agonist WIN55212-2 (WIN2) greatly decreased excitatory synaptic transmission by 62%. The effect of WIN-2 was concentration d...
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PMID: 18816788
PDF is available here.
PDF is available here.
Abstract
We observed 100 percent tumour formation in DMBA-alone painted hamsters. Disturbances in the status of lipid peroxidation, antioxidants and phase II detoxification agents were noticed in DMBA-alone painted hamsters. Oral administration of curcumin (80 mg/kg body weight) and piperine (50 mg/kg body w...
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PMID: 19296028
PDF is available here.
PDF is available here.
Abstract
Chemical characterization and acute and sub-acute toxicity study of Trikatu, a generic herbal formulation of Indian system of medicine, was carried out in Charles Foster (CF) rats for safety profiling. In acute toxicity experiment, Trikatu at 2,000 mg/kg body weight once orally was well tolerated by...
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PMID: 19182439
PDF is available here.
PDF is available here.
Abstract
Nitrergic myenteric neurons co-innervating motor endplates were previously shown to inhibit vagally induced contractions of striated muscle in the rodent oesophagus. Immunohistochemical demonstration of putative co-transmitters, e.g. galanin, in enteric neurons prompted us to study a possible role o...
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PMID: 19077146
PDF is available here.
PDF is available here.
Abstract
Anandamide is an endocannabinoid known to participate in reproductive processes. This study observed that 17beta-oestradiol and progesterone modulated the production of anandamide and its metabolizing enzymes in the rat uterus. Anandamide production was highest at the oestrous stage and 17beta-oestr...
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PMID: 19192341
PDF is available here.
PDF is available here.
Vitamins & Hormones (81) 2009
Changes in the endocannabinoid system may give insight into new and effective treatments for cancer.
Abstract
The endocannabinoid system comprises specific cannabinoid receptors such as Cb1 and Cb2, the endogenous ligands (anandamide and 2-arachidonyl glycerol among others) and the proteins responsible for their synthesis and degradation. This system has become the focus of research in recent years because...
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PMID: 19647123
PDF is available here.
PDF is available here.
Abstract
We investigated the role of TRPV1 channels in the control of both excitatory and inhibitory transmission in the striatum. Pharmacological stimulation of TRPV1 channels with capsaicin (10 nM) selectively enhanced the frequency of glutamate-mediated spontaneous (sEPSCs) and miniature excitatory postsy...
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PMID: 18930149
PDF is available here.
PDF is available here.
Abstract
Simple and rapid stability-indicating HPLC methods were developed for the individual analysis of aconitine (ACN) and piperine (PIN) in Mahamrutynjaya rasa, an herbal dosage form containing Aconitum ferox, Piper nigrum, and Piper longum in combination. Separation of the ACN from its major and minor d...
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PMID: 19714970
PDF is available here.
PDF is available here.
Cancer Science (100)1 2009
Abstract
We report that phthoxazolin A and its analog inthomycin B inhibit the growth of human prostate cancer DU-145 cells by modulating tumor-stromal cell interactions. Using an in vitro coculture system, in which prostate cancer cell growth is upregulated by prostate stromal cells (PrSC), we found that ph...
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PMID: 19018764
PDF is available here.
PDF is available here.
Natural Product Research (23)15 2009
Abstract
Detailed chemical studies on the roots of Piper sarmentosum and Piper nigrum have resulted in several alkaloids. The roots of P. sarmentosum gave a new aromatic compound, 1-nitrosoimino-2,4,5-trimethoxybenzene (1). Piper nigrum roots gave pellitorine (2), (E)-1-[3',4'-(methylenedioxy)cinnamoyl]piper...
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PMID: 19809914
PDF is available here.
PDF is available here.
Abstract
The fluorescence characteristics of the complex of piperine with cation in micellar system were studied. At the same time, the influence of experimental condition on the fluorescence intensity was also studied. The experiments indicated that piperine had very low fluorescence signal itself. But in p...
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PMID: 19385236
PDF is available here.
PDF is available here.
Abstract
We investigated whether human erythroleukemia (HEL) cells were able to bind, metabolise and transport the main endocannabinoids, anandamide (AEA) and 2-arachidonoylglycerol (2-AG). We also investigated whether AEA or 2-AG could modulate HEL differentiation. Although able to internalise both endocann...
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PMID: 18820887
PDF is available here.
PDF is available here.
Bratislavske lekarske listy (110)7 2009
Abstract
The results of the study demonstrated that mucosal injury in anandamide injected group was less expressed than in other groups suggesting that anandamide might have a protective effect on the mucosa. After L-NAME and indomethacin injection, the protective effect of anandamide seems to disappear due...
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PMID: 19711821
PDF is available here.
PDF is available here.
Biochemical Pharmacology (77)1 2009
Abstract
We investigated the effects of the endocannabinoid anandamide (AEA) on the inducible expression of the biologically active cytokines IL-12p70 and IL-23, and their forming subunits, in activated microglial cells. We also studied the signalling pathways involved in the regulation of IL-12p70/IL-23 exp...
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PMID: 18848818
PDF is available here.
PDF is available here.
Anesthesia & Analgesia (108)1 2009
Abstract
We describe the biochemical and biological properties of a potent and selective FAAH inhibitor, 4-(3-phenyl-[1,2,4]thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide (JNJ-1661010). The time-dependence of apparent IC(50) values at rat and human recombinant FAAH, dialysis and mass spectrometry...
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PMID: 19095868
PDF is available here.
PDF is available here.
Abstract
Anandamide dose-dependently decreased the mean arterial blood pressure of rats made hypertensive by AII-AVP infusion, but not normotensive rats. Interestingly, acute hypertension also revealed a hypotensive response to WIN55212-2, which caused hypertension in normotensive animals. The enhanced depre...
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PMID: 19133994
PDF is available here.
PDF is available here.
Effects of progesterone on total brain tissue adenosine deaminase activity in experimental epilepsy.
Abstract
Single seizure and epilepsy is one of the most commonly encountered neurologic disorders in elderly individuals, arising as a result of complex and often multiple acquired underlying pathologies. Adenosine, acting at A1 receptors, exhibits anticonvulsant effects in experimental epilepsy and inhibits...
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PMID: 19125374
PDF is available here.
PDF is available here.
Abstract
We have recently shown that interacting endocannabinoid, opioid, and dopamine systems modulate social play. In the present study, we tested the hypothesis that, in contrast to administration of exogenous cannabinoid agonists, increasing local endocannabinoid signaling through anandamide transporter...
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PMID: 18948500
PDF is available here.
PDF is available here.
Biochemistry (Washington) (47)51 2008
Abstract
We report the structures of HDAC8 complexes with trichostatin A and 3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide (APHA) in a new crystal form. The structure of the APHA complex reveals that the hydroxamate CO group accepts a hydrogen bond from Y306 but does not coordinate to Zn(...
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PMID: 19053282
PDF is available here.
PDF is available here.
European Journal of Pharmacology (600)1-3 2008
Abstract
Lack of involvement of the opioid system with the endocannabinoid, arachidonylethanolamide (anandamide) was possibly due to hydrolysis by fatty acid amide hydrolase (FAAH). Cyclohexylcarbamic acid 3'-carbamoyl-biphenyl-3-yl ester (URB597) is an inhibitor of FAAH, increases brain anandamide levels an...
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PMID: 18762181
PDF is available here.
PDF is available here.
Abstract
We studied effects of the endogenous cannabinoid anandamide (N-arachidonylethanolamine) in experimental colitis induced by TNBS (2,4,6-trinitrobenzene sulfonic acid) in AKR mice. A scoring system was used to describe clinical and macroscopic changes. Intraperitoneally administered anandamide signifi...
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PMID: 19212003
PDF is available here.
PDF is available here.