Search results for "cb"
showing 10 items of 647 documents
Strategies to gain novel Alzheimer’s disease diagnostics and therapeutics using modulators of ABCA transporters
2021
Adenosine-triphosphate-(ATP)-binding cassette (ABC) transport proteins are ubiquitously present membrane-bound efflux pumps that distribute endo- and xenobiotics across intra- and intercellular barriers. Discovered over 40 years ago, ABC transporters have been identified as key players in various human diseases, such as multidrug-resistant cancer and atherosclerosis, but also neurodegenerative diseases, such as Alzheimer���s disease (AD). Most prominent and well-studied are ABCB1, ABCC1, and ABCG2, not only due to their contribution to the multidrug resistance (MDR) phenotype in cancer, but also due to their contribution to AD. However, our understanding of other ABC transporters is limited…
Central functional response to the novel peptide cannabinoid, hemopressin.
2013
Hemopressin is the first peptide ligand to be described for the CB₁ cannabinoid receptor. Hemopressin acts as an inverse agonist in vivo and can cross the blood-brain barrier to both inhibit appetite and induce antinociception. Despite being highly effective, synthetic CB₁ inverse agonists are limited therapeutically due to unwanted, over dampening of central reward pathways. However, hemopressin appears to have its effect on appetite by affecting satiety rather than reward, suggesting an alternative mode of action which might avoid adverse side effects. Here, to resolve the neuronal circuitry mediating hemopressin's actions, we have combined blood-oxygen-level-dependent, pharmacological-ch…
Cannabinoid type 1 receptor modulates intestinal propulsion by an attenuation of intestinal motor responses within the myenteric part of the peristal…
2007
Cannabinoid-1 (CB1) receptor activation affects gastrointestinal propulsion in vivo. It was our aim to further characterize the involved myenteric mechanisms in vivo and in vitro. In CB1(-/-) mice and wild-type littermates we performed in vivo transit experiments by charcoal feeding and in vitro electrophysiological recordings in mouse small intestinal smooth muscle. Ascending neuronal contraction (ANC) following electrical field stimulation was studied in rat ileum in a partitioned organ bath separating the aboral stimulation site from the oral recording site. The knockout animals displayed an accelerated upper gastrointestinal transit compared to control animals. The CB1 receptor antagoni…
The lignan, (-)-sesamin reveals cytotoxicity toward cancer cells: pharmacogenomic determination of genes associated with sensitivity or resistance.
2013
(-)-Sesamin is a lignan present in sesam oil and a number of medicinal plants. It exerts various pharmacological effects, such as prevention of hyperlipidemia, hypertension, and carcinogenesis. Moreover, (-)-sesamin has chemopreventive and anticancer activity in vitro and in vivo. Multidrug resistance (MDR) of tumors leads to fatal treatment outcome in many patients and novel drugs able to kill multidrug-resistant cells are urgently needed. P-glycoprotein (MDR1/ABCB1) is the best known ATP-binding cassette (ABC) drug transporter mediating MDR. ABCB5 is a close relative to ABCB1, which also mediates MDR. We found that the mRNA expressions of ABCB1 and ABCB5 were not related to the 50% inhibi…
Putative molecular determinants mediating sensitivity or resistance towards carnosic acid tumor cell responses.
2020
Abstract Background Carnosic acid (CA) is one of the main constituents in rosemary extract. It possesses valuable pharmacological properties, including anti-oxidant, anti-inflammatory, anti-microbial and anti-cancer activities. Numerous in vitro and in vivo studies investigated the anticancer profile of CA and emphasized its potentiality for cancer treatment. Nevertheless, the role of multidrug-resistance (MDR) related mechanisms for CA's anticancer effect is not yet known. Purpose We investigated the cytotoxicity of CA against known mechanisms of anticancer drug resistance (P-gp, ABCB5, BCRP, EGFR and p53) and determined novel putative molecular factors associated with cellular response to…
Cytotoxicity of cucurbitacin E from Citrullus colocynthis against multidrug-resistant cancer cells
2019
Abstract Background Cucurbitacin E (CuE) is an oxygenated tetracyclic triterpenoid isolated from the fruits of Citrullus colocynthis (L.) Schrad. Purpose This study outlines CuE's cytotoxic activity against drug-resistant tumor cell lines. Three members of ABC transporters superfamily, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and ABCB5 were investigated, whose overexpression in tumors is tightly linked to multidrug resistance. Further factors of drug resistance studied were the tumor suppressor TP53 and the epidermal growth factor receptor (EGFR). Methods Cytotoxicity assays (resazurin assays) were used to investigate the activity of Citrullus colocynthis and CuE towar…
Activity of orally self-administered acetaldehyde in an operant/conflict paradigm in rats; involvement of cannabinoid cb1 receptors
2012
Acetaldehyde (ACD), ethanol first metabolite, interacts with the dopaminergic reward system, and with the neuropeptidergic transmission in the hypothalamus. Self-administration within operant conditioning is a valid model to investigate drug-seeking and drug-taking behaviour in rats. Cannabinoid CB1 receptors are involved in reinstatement of alcohol-seeking behaviour and of many other drugs of abuse (3). Accordingly, this study was aimed at the evaluation of: 1) the motivational properties of oral ACD in the induction and maintenance of an operant-drinking behaviour; 2) the onset of a relapse drinking behaviour, following ACD deprivation; 3) ACD effect in a conflict situation employing the …
Innovative ready to use carrier-bacteria devices for bioremediation of oil contaminated water
2018
Bioremediation, that uses microorganisms to remove environmental pollutants, is the best way of restoring the environment due to its low cost and sustainability. Immobilization of microorganisms capable of degrading specific contaminants significantly promotes bioremediation processes. An innovative ready to use bioremediation system to clean up oil-contaminated water was developed immobilizing highly performant marine and soil HC degrading bacteria, on biodegradable oil-absorbing carriers. Two soil Actinobacteria (Gordonia sp. SoCg, Nocardia sp. SoB) and two marine Gammaproteobacteria (Alcanivorax sp. SK2, Oleibacter sp.5), were immobilized on biopolymeric membranes prepared by electrospin…
Transpiration and Water Use of an Irrigated Traditional Olive Grove with Sap-Flow Observations and the FAO56 Dual Crop Coefficient Approach
2021
The SIMDualKc model was applied to evaluate the crop water use and the crop coefficient (Kc) of an irrigated olive grove (Olea europaea L.) located in Sicily, Italy, using experimental data collected from two crop seasons. The model applies the FAO56 dual Kc approach to compute the actual crop evapotranspiration (ETc act) and its components, i.e., the actual tree transpiration (Tc act), obtained through the basal crop coefficient (Kcb), and soil evaporation according to an evaporation coefficient (Ke). Model calibration was performed by minimizing the difference between the predicted Tc act and the observed daily tree transpiration measured with sap flow instrumentation (TSF field) acquired…
Congenital undifferentiated sarcoma associated to BCOR-CCNB3 gene fusion
2017
Small round cell sarcomas are aggressive bone and soft tissue tumors that predominantly affect children and young adults. A new group of sarcomas with a recurrent BCOR-CCNB3 gene fusion has been recently identified in previously unclassifiable small round cell sarcomas. BCOR-CCNB3 sarcomas share clinical and pathologic similarities with Ewing sarcoma, but show a stronger male predilection and less aggressiveness, as well as distinct gene expression profiling and pangenomic SNP array analyses. We report the unusual case of a congenital BCOR-CCNB3 retroperitoneal sarcoma in a female born at 34th gestational week, which was diagnosed in necropsy after 21hours of life. Immunohistochemical analy…