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11.
Background
Given the high occurrence of prostate cancer worldwide and one of the major sources of the discovery of new lead molecules being medicinal plants, this research undertook to investigate the possible anti-cancer activity of two natural cycloartanes; cycloartane-3,24,25-diol (extracted in our lab from Tillandsia recurvata) and cycloartane-3,24,25-triol (purchased). The inhibition of MRCKα kinase has emerged as a potential solution to restoring the tight regulation of normal cellular growth, the loss of which leads to cancer cell formation.Methods
Kinase inhibition was investigated using competition binding (to the ATP sites) assays which have been previously established and authenticated and cell proliferation was measured using the WST-1 assay.Results
Cycloartane-3,24,25-triol demonstrated strong selectivity towards the MRCKα kinase with a Kd50 of 0.26 μM from a total of 451 kinases investigated. Cycloartane-3,24,25-triol reduced the viability of PC-3 and DU145 cell lines with IC50 values of 2.226?±?0.28 μM and 1.67?±?0.18 μM respectively.Conclusions
These results will prove useful in drug discovery as Cycloartane-3,24,25-triol has shown potential for development as an anti-cancer agent against prostate cancer. 相似文献12.
13.
Menchari Y Camilleri C Michel S Brunel D Dessaint F Le Corre V Délye C 《The New phytologist》2006,171(4):861-874
Effective herbicide resistance management requires an assessment of the range of spatial dispersion of resistance genes among weed populations and identification of the vectors of this dispersion. In the grass weed Alopecurus myosuroides (black-grass), seven alleles of the acetyl-CoA carboxylase (ACCase) gene are known to confer herbicide resistance. Here, we assessed their respective frequencies and spatial distribution on two nested geographical scales (the whole of France and the French administrative district of C?te d'Or) by genotyping 13 151 plants originating from 243 fields. Genetic variation in ACCase was structured in local populations at both geographical scales. No spatial structure in the distribution of resistant ACCase alleles and no isolation by distance were detected at either geographical scale investigated. These data, together with ACCase sequencing and data from the literature, suggest that evolution of A. myosuroides resistance to herbicides occurred at the level of the field or group of adjacent fields by multiple, independent appearances of mutant ACCase alleles that seem to have rather restricted spatial propagation. Seed transportation by farm machinery seems the most likely vector for resistance gene dispersal in A. myosuroides. 相似文献
14.
Cuttlefish powder (CFP) from Sepia officinalis by-products was prepared and tested as a fermentation substrate for microbial growth and protease production by several species of bacteria: Bacillus licheniformis, Bacillus subtilis, Pseudomonas aeruginosa, Bacillus cereus BG1, and Vibrio parahaemolyticus. All microorganisms studied grew well and produced protease activity when cultivated in medium containing only CFP indicating that the strains can obtain their carbon and nitrogen source requirements directly from whole by-product proteins. Moreover, it was found that the addition to the cuttlefish medium of diluted fishery wastewaters (FWW), generated by marine-products processing factories, enhanced the production of protease. Maximum activity was obtained when cells were grown in cuttlefish media containing 5-times or 10-times diluted FWW. Five-times diluted FWW enhanced protease production by B. cereus BG1 and B. subtilis by 467% and 75% more than control media, respectively. The enhancement could have been due to the high organic content or high salts in FWW.As a result, cuttlefish by-products powder enriched with diluted FWW was found to be a suitable growth media for protease-producing strains. This new process, which converts underutilized wastes (liquid and solid) into more marketable and acceptable forms, coupled with protease production, can be an alternative way to the biological treatment of solid and liquid wastes generated by the cuttlefish processing industry. 相似文献
15.
Sherbin Nahid Ahmed Anwar Fatani Abdulhamid Al-Otaibi Khalid Al-Jahdali Fares Ali Yosra Z. Al-Harbi Abdullah Khan Mohammad Baharoon Salim Al-Jahdali Hamdan 《Sleep and biological rhythms》2017,15(2):127-135
Sleep and Biological Rhythms - The aim of this cross-sectional study was to determine the prevalence, risk factors, other associated sleep disorders and commodities of Restless Legs Syndrome (RLS)... 相似文献
16.
Yosra Shaaban R. Elnaggar Magda A. El-Massik Ossama Y. Abdallah Abd Elazim R. Ebian 《AAPS PharmSciTech》2010,11(2):645-651
The recent challenge in orally disintegrating tablets (ODT) manufacturing encompasses the compromise between instantaneous
disintegration, sufficient hardness, and standard processing equipment. The current investigation constitutes one attempt
to fulfill this challenge. Maltodextrin, in the present work, was utilized as a novel excipient to prepare ODT of meclizine.
Tablets were prepared by both direct compression and wet granulation techniques. The effect of maltodextrin concentrations
on ODT characteristics—manifested as hardness and disintegration time—was studied. The effect of conditioning (40°C and 75%
relative humidity) as a post-compression treatment on ODT characteristics was also assessed. Furthermore, maltodextrin-pronounced
hardening effect was investigated using differential scanning calorimetry (DSC) and X-ray analysis. Results revealed that
in both techniques, rapid disintegration (30–40 s) would be achieved on the cost of tablet hardness (about 1 kg). Post-compression
conditioning of tablets resulted in an increase in hardness (3 kg), while keeping rapid disintegration (30–40 s) according
to guidance of the FDA for ODT. However, direct compression-conditioning technique exhibited drawbacks of long conditioning
time and appearance of the so-called patch effect. These problems were, yet, absent in wet granulation-conditioning technique.
DSC and X-ray analysis suggested involvement of glass-elastic deformation in maltodextrin hardening effect. High-performance
liquid chromatography analysis of meclizine ODT suggested no degradation of the drug by the applied conditions of temperature
and humidity. Overall results proposed that maltodextrin is a promising saccharide for production of ODT with accepted hardness-disintegration
time compromise, utilizing standard processing equipment and phenomena of phase transition. 相似文献
17.
Yosra Bouyacoub Hela Zribi Hatem Azzouz Fehmi Nasrallah Rim Ben Abdelaziz Monia Kacem Ben Rekaya Olfa Messaoud Lilia Romdhane Cherine Charfeddine Mustapha Bouziri Sonia Bouziri Neji Tebib Mourad Mokni Naziha Kaabachi Samir Boubaker Sonia Abdelhak 《Gene》2013
Tyrosinemia type II, also designated as oculocutaneous tyrosinemia or Richner–Hanhart syndrome (RHS), is a very rare autosomal recessive disorder. In the present study, we report clinical features and molecular genetic investigation of the tyrosine aminotransferase (TAT) gene in two young patients, both born to consanguineous unions between first-degree cousins. These two unrelated families originated from Northern and Southern Tunisia. The clinical diagnosis was based on the observation of several complications related to Richner–Hanhart syndrome: recurrent eye redness, tearing and burning pain, photophobia, bilateral pseudodendritic keratitis, an erythematous and painful focal palmo-plantar hyperkeratosis and a mild delay of mental development. The diagnosis was confirmed by biochemical analysis. Sequencing of the TAT gene revealed the presence of a previously reported missense mutation (c.452G > A, p.Cys151Tyr) in a Tunisian family, and a novel G duplication (c.869dupG, p.Trp291Leufs*6). Early diagnosis of RHS and protein-restricted diet are crucial to reduce the risk and the severity of long-term complications of hypertyrosinemia such as intellectual disability. 相似文献
18.
Hamdi Y Masmoudi-Kouki O Kaddour H Belhadj F Gandolfo P Vaudry D Mokni M Leprince J Hachem R Vaudry H Tonon MC Amri M 《Journal of neurochemistry》2011,118(3):416-428
Oxidative stress, resulting from accumulation of reactive oxygen species (ROS), plays a critical role on astrocyte death associated with neurodegenerative diseases. Astroglial cells produce endozepines, a family of biologically active peptides that have been implicated in cell protection. Thus, the purpose of the present study was to investigate the potential protective effect of one of the endozepines, the octadecaneuropeptide ODN, on hydrogen peroxide (H(2) O(2) )-induced oxidative stress and cell death in rat astrocytes. Incubation of cultured astrocytes with graded concentrations of H(2) O(2) for 1 h provoked a dose-dependent reduction of the number of living cells as evaluated by lactate dehydrogenase assay. The cytotoxic effect of H(2) O(2) was associated with morphological modifications that were characteristic of apoptotic cell death. H(2) O(2) -treated cells exhibited high level of ROS associated with a reduction of both superoxide dismutases (SOD) and catalase activities. Pre-treatment of astrocytes with low concentrations of ODN dose-dependently prevented cell death induced by H(2) O(2) . This effect was accompanied by a marked attenuation of ROS accumulation, reduction of mitochondrial membrane potential and activation of caspase 3 activity. ODN stimulated SOD and catalase activities in a concentration-dependent manner, and blocked H(2) O(2) -evoked inhibition of SOD and catalase activities. Blockers of SOD and catalase suppressed the effect of ODN on cell survival. Taken together, these data demonstrate for the first time that ODN is a potent protective agent that prevents oxidative stress-induced apoptotic cell death. 相似文献
19.
Y Hamdi H Kaddour D Vaudry S Bahdoudi S Douiri J Leprince H Castel H Vaudry MC Tonon M Amri O Masmoudi-Kouki 《PloS one》2012,7(8):e42498
Astrocytes synthesize and release endozepines, a family of regulatory peptides, including the octadecaneuropeptide (ODN) an endogenous ligand of both central-type benzodiazepine (CBR) and metabotropic receptors. We have recently shown that ODN exerts a protective effect against hydrogen peroxide (H(2)O(2))-induced oxidative stress in astrocytes. The purpose of the present study was to determine the type of receptor and the transduction pathways involved in the protective effect of ODN in cultured rat astrocytes. We have first observed a protective activity of ODN at very low concentrations that was abrogated by the metabotropic ODN receptor antagonist cyclo(1-8)[DLeu(5)]OP, but not by the CBR antagonist flumazenil. We have also found that the metabotropic ODN receptor is positively coupled to adenylyl cyclase in astrocytes and that the glioprotective action of ODN upon H(2)O(2)-induced astrocyte death is PKA- and MEK-dependent, but PLC/PKC-independent. Downstream of PKA, ODN induced ERK phosphorylation, which in turn activated the expression of the anti-apoptotic gene Bcl-2 and blocked the stimulation by H(2)O(2) of the pro-apoptotic gene Bax. The effect of ODN on the Bax/Bcl-2 balance contributed to abolish the deleterious action of H(2)O(2) on mitochondrial membrane integrity and caspase-3 activation. Finally, the inhibitory effect of ODN on caspase-3 activity was shown to be PKA and MEK-dependent. In conclusion, the present results demonstrate that the potent glioprotective action of ODN against oxidative stress involves the metabotropic ODN receptor coupled to the PKA/ERK-kinase pathway to inhibit caspase-3 activation. 相似文献
20.
Yosra Ben Halima Rym Kefi Marco Sazzini Cristina Giuliani Sara De Fanti Chokri Nouali Majdi Nagara Giacomo Mengozzi Sahar Elouej Abdelmajid Abid Henda Jamoussi Lotfi Chouchane Giovanni Romeo Sonia Abdelhak Donata Luiselli 《Genes & nutrition》2017,12(1):20