Search results for: inhibitory neurotransmitters

Authors: Ramalingam Boobalan, Chinpiao Chen, Jui-I. Chiao

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A series of erlotinib analogues that have structural modification at 6,7-alkoxyl positions is efficiently synthesized. The key reactions that involved in synthesis are one-pot oxime formation-dehydration for the formation of nitrile, quinazoline ring formation reaction between aniline and o-cyanoaniline via formamidine intermediate, Fe/NH4Cl catalyzed reduction-hetereocyclization-reductive ring opening reaction for the formation of o-aminobenzamide, high yielding seal tube reactions for O-demethylation, sodium iodide substitution, ammonia substitution. The in vitro anti-tumor activity of synthesized compounds is studied in two non-small cell lung cancer (NSCLC) cell lines (A549 and H1975). Among the synthesized compounds, the iodo compound 6 (ETN-6) exhibits higher anti-cancer activity compared to erlotinib. An efficient method is developed for the conjugation of erlotinib analogue-4, alcohol compound, with protein, bovine serum albumin (BSA), via succinic acid linker. The in vitro anti-tumor activity of the protein attached erlotinib analogue, 8 (ETN-4-Suc-BSA), showed stronger inhibitory activity in both A549 and H1975 NSCLC cell lines.

Keywords: anti-cancer, BSA, EGFR, Erlotinib

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Authors: Shah Md. Asraful Islam, Shabina Yeasmin, Fatima Aktar Mousumi

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The experiment was conducted to evaluate the antagonistic potential of three commercially available Trichoderma strains viz., T. harzianum (armigera), T. harzianum (Ispahani), and T. viride against Colletotrichum musae isolates from three banana varieties viz., sagar, sobri, and katali. Mycelial growth rates of C. musae isolates were observed, the highest mycelial growth (11.62, 15.75, and 23.12 mm diameter) was observed by C. musae from sagor banana at 1, 2 and 3 days after inoculation, respectively. All the Trichoderma strains were capable of growth inhibition of C. musae isolates. After 4 days of duel culture, the highest mycelial growth reduction (10.33 mm diameter) was observed by the interaction between T. harzianum (armigera) with C. musae from sagor banana. Moreover, the highest growth inhibition (46.29%) was observed by the interaction between T. harzianum (armigera) with C. musae from the sobri banana. All the Trichoderma strains fully affected the viability of all the Colletotrichum isolates. Interestingly, both cultural filtrates and mycelial powders of all the Trichoderma strains showed a very nice inhibitory effect against C. musae isolates, where cultural filtrates were more potential than that of mycelial powders. So, all the tested Trichoderma strains may be used for the control of banana anthracnose disease.

Keywords: biological control, banana, anthracnose, Trichoderma, Colletotrichum

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Authors: Eleni Peristeri, Georgia Fotiadou, Ianthi-Maria Tsimpli

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The local-global dimension has been studied extensively in healthy controls and preference for globally processed stimuli has been validated in both the visual and auditory modalities. Critically, the local-global dimension has an inherent interference resolution component, a type of cognitive control, and left-prefrontal-cortex-damaged (LPFC) individuals have exhibited inability to override habitual response behaviors in item recognition tasks that involve representational interference. Eight patients with damage in the left PFC (age range: 32;5 to 69;0. Mean age: 54;6 yrs) and twenty age- and education-matched language-unimpaired adults (mean age: 56;7yrs) have participated in the study. Distinct performance patterns were found between the language-unimpaired and the LPFC-damaged group which have mainly stemmed from the latter’s difficulty with inhibiting global stimuli in incongruent trials. Overall, the local-global attentional dimension affects LPFC-damaged individuals with non-fluent aphasia in non-language domains implicating distinct types of inhibitory processes depending on the level of processing.

Keywords: left lateral prefrontal cortex damage (LPFC), local-global non-language attention, representational interference, non-fluent aphasia

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Authors: Archana Sharma, Vijayashree Nayak, Ashok Kumar

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Three-dimensional matrices were fabricated from blend of natural-natural polymers like carrageenan-gelatin and synthetic -natural polymers such as PEG- gelatin (PEG of different molecular weights (2,000 and 6,000) using two different crosslinkers; glutaraldehyde and EDC-NHS by cryogelation technique. Blends represented a feasible approach to design 3-D scaffolds with controllable mechanical, physical and biochemical properties without compromising biocompatibility and biodegradability. These matrices possessed interconnected porous structure, good mechanical strength, biodegradable nature, constant swelling kinetics, ability to withstand high temperature and visco-elastic behavior. Hemocompatibility of cryogel matrices was determined by coagulation assays and hemolytic activity assay which demonstrated that these cryogels have negligible effects on coagulation time and have excellent blood compatibility. In vitro biocompatibility (cell-matrix interaction) inferred good cell adhesion, proliferation, and secretion of ECM on matrices. These matrices provide a microenvironment for the growth, proliferation, differentiation and secretion of ECM of different cell types such as IMR-32, C2C12, Cos-7, rat bone marrow derived MSCs and human bone marrow MSCs. Hoechst 33342 and PI staining also confirmed that the cells were uniformly distributed, adhered and proliferated properly on the cryogel matrix. An ideal scaffold used for tissue engineering application should allow the cells to adhere, proliferate and maintain their functionality. Neurotransmitter analysis has been done which indicated that IMR-32 cells adhered, proliferated and secreted neurotransmitters when they interacted with these matrices which showed restoration of their functionality. The cell-matrix interaction up to molecular level was also evaluated so to check genotoxicity and protein expression profile which indicated that these cryogel matrices are non-genotoxic and maintained biofunctionality of cells growing on these matrices. All these cryogels, when implanted subcutaneously in balb/c mice, showed no adverse systemic or local toxicity effects at implantation site. There was no significant increase in inflammatory cell count has otherwise been observed after scaffold implantation. These cryogels are supermacroporous and this porous structure allows cell infiltration and proliferation of host cells. This showed the integration and presence of infiltrated cells into the cryogel implants. Histological analysis confirmed that the implanted cryogels do not have any adverse effect in spite of host immune system recognition at the site of implantation, on its surrounding tissues and other vital host organs. In vivo biocompatibility study after in vitro biocompatibility analysis has also concluded that these synthesized cryogels act as important biological substitutes, more adaptable and appropriate for transplantation. Thus, these cryogels showed their potential for soft tissue engineering applications.

Keywords: cryogelation, hemocompatibility, in vitro biocompatibility, in vivo biocompatibility, soft tissue engineering applications

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Authors: Bingjie Wang, Su-Yeon Kwon, Ik-Joong Kang

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A Surface-enhanced Raman Scattering (SERS) as the principle for enhancing Raman scattering by molecules adsorbed on rough metal surfaces or by nanostructures is used to detect the concentration change of γ-Aminobutyric Acid (GABA). As for the gold-chitosan nanoshell, it is made by using chitosan nanoparticles crosslinking with sodium tripolyphosphate(TPP) for the first step to form the chitosan nanoparticles, which would be covered with the gold sequentially. The size of the fabricated product was around 100nm. Based on the method that the sulfur end of the MPA linked to gold can form the very strong S–Au bond, and the carboxyl group, the other end of the MPA, can easily absorb the GABA. GABA is the mainly inhibitory neurotransmitter in the mammalian central nervous system in the human body. It plays such significant role in reducing neuronal excitability throughout the nervous system. When the system formed, it generated SERS, which made a clear difference in the intensity of Raman scattering within the range of GABA concentration. So it is obtained from the experiment that the calibration curve according to the GABA concentration relevant with the SERS scattering. In this study, DLS, SEM, FT-IR, UV, SERS were used to analyze the products to obtain the conclusion.

Keywords: chitosan-gold nanoshell, mercaptopropionic acid, γ-aminobutyric acid, surface-enhanced Raman scattering

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Authors: Hen Friman, Alex Schechter, Yeshayahu Nitzan, Rivka Cahan

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The treatment of aromatic hydrocarbons in wastewater resulting from oil spills and chemical manufactories is becoming a key concern in many modern countries. Benzene, ethylbenzene, toluene and xylene (BETX) contaminate groundwater as well as soil. These compounds have an acute effect on human health and are known to be carcinogenic. Conventional removal of these toxic materials involves separation and burning of the wastes, however, the cost of chemical treatment is very high and energy consuming. Bioremediation methods for removal of toxic organic compounds constitute an attractive alternative to the conventional chemical or physical techniques. Bioremediation methods use microorganisms to reduce the concentration and toxicity of various chemical pollutants Toluene is biodegradable both aerobically and anaerobically, it can be growth inhibitory to microorganisms at elevated concentrations, even to those species that can use it as a substrate. In this research culture of Pseudomonas putida was grown in bath bio-reactor (BBR) with toluene 100 mg/l as a single carbon source under constant voltage of 125 mV, 250 mV and 500 mV. The culture grown in BBR reached to 0.8 OD660nm while the control culture that grown without external voltage reached only to 0.6 OD660nm. The residual toluene concentration after 147 h, in the BBR operated under external voltage (125 mV) was 22 % on average, while in the control BBR it was 81 % on average.

Keywords: bioremediation, aromatic hydrocarbons, BETX, toluene, pseudomonas putida

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Authors: I. L. Ibrahim, A. Mann, A. Ndanaimi

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The research involved phytochemical screening, antibacterial activities and mineral determination by flame photometry of the crude extract of Brysocarpus coccineus schum indeed were carried out. The result of Phytochemical screening reveal tha saponins, alkaloids, cardiac glycosides, and anthraquinones were present. This suggests that the plant extract could be used as anti-inflammatory and anti-bleeding agents. Estimation of mineral content shows that the crude extract of B. coccineus contains 0.73 (Na+), 1.06 (K+) and 1.98 (Ca+) which justifies its use to be safe for hypertensive patients and could be used to lower blood pressure. The antibacterial properties of aqueous and ethanol extract were studied against some bacteria; pseudomonas aeruginosa, Escherichia coli, Bacilus subtilis, Klebsilla penmuoniae by disc diffusion method. The aqueous extract showed significant activity against the organisms while the ethanol at concentrations 5-10mg/ml ethanol extract showed significant zone of inhibition against the organisms, E. coli, (19 mm), B. cereus (12 mm), P. aeruginosa (11 mm), K. pnemuoniae (11 mm). Minimum inhibitory concentration (MIC) was carried with considerable effect of inhibition on the organisms. The MIC values observed were 1, 24, 16 and 19 mm against E. coli, B. cereus, P. aeruginosa and K. pnemuoniae respectively. Therefore, the plant could be a potential source of antibacterial agent although more pharmacological and clinical study may be recommended.

Keywords: phytochemicals, microorganisms, screenings, mineral ions

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Authors: Azhar Jabareen, Mahmoud Huleihel

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BRCA-1 is a multifunctional tumor suppressor, whose expression is activated by the estrogen (E2)-liganded ERα receptor. The activated ERα is a transcriptional factor which activates various genes either by direct binding to the DNA at E2-responsive elements (EREs) and indirectly associated with a range of alternative non-ERE elements. Interference with BRCA-1 expression and/or functions leads to high risk of breast or/and ovarian cancer. Our lab investigated the involvement of Human T-cell leukemia Virus Type 1 (HTLV-1) in breast cancer, since HTLV-1 Tax was found to strongly inhibit BRCA-1 expression. In addition, long exposure of 12-O-tetradecanoylphorbol-13-acetate (TPA), which is one of the stress-inducing agents activated the HTLV-1 promoter. So here the involvement of TPA in breast cancer had been examined by testing the effect of TPA on BRCA-1 and ERE expression. The results showed that TPA activated both BRCA-1 and ERE expression. In the 12 hours TPA activated the tow promoters more than others time, and after 24 hours the level of the tow promoters was decreased. Tax inhibited BRCA-1 expression but did not succeed to inhibit the effect of TPA. Then the activation of the two promoters was not through ERα pathway because TPA had no effect on ERα binding to the two promoters of the BRCA-1 and ERE. Also, the activation was not via nuclear factor kappa B (NF-κB) pathway because when the inhibitory of NF-κB had been added to the TPA, it still activated the tow promoters. However, it seems that 53BP1 may be involved in TPA activation of these promoters because ectopic high expression of 53BP1 significantly reduced the TPA activity. In addition, in the presence of Bisindolylmaleimide-I (BI)- the inhibitor of Protein Kinase C (PKC)- there was no activation for the two promoters, so the PKC is agonized BRCA-1 and ERE activation.

Keywords: BRCA-1, ERE, HTLV-1, TPA

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Authors: Sihem Benmimoune, Abdelbaki Lemgharbi, Ahmed Ait Yahia, Abdelkrim Kameli

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Our study is based on chemical and phytochemical characterization of Artemisia absinthium L and in vitro tests to demonstrate the biological activities of essential oil and natural extract. A qualitative and quantitative comparison of the essential oil extracted by two extraction procedures was performed by analysis of CG/SM and the yield calculation. The method of hydrodistillation has a chemical composition and provides oil content than the best training water vapor. These oils are composed mainly of thujone followed chamazulene and ρ-cymene. The antimicrobial activity of wormwood oil was tested in vitro by two methods (agar diffusion and microdilution) on four plant pathogenic fungi (Aspergillus sp, Botrytis cinerea, Fusarium culmorum and Helminthosporium sp). The study of the antifungal effect showed that this oil has an inhibitory effect counterpart the microorganisms tested in particular the strain Botrytis cinerea. Otherwise, this activity depends on the nature of the oil and the germ itself. The antioxidant activity in vitro was studied with the DPPH method. The activity test shows that the oil and extract of Artemisia absinthium have a very low antioxidant capacity compared to the antioxidants used as a reference. The extract has a potentially high antiradical power not from its oil. The quantitative determinations of phenolic compounds by the Folin-Ciocalteu revealed that absinthe is low in total polyphenols and tannins.

Keywords: artemisia absinthium, biological activities, essential oil, extraction processes

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Authors: Anjana Goel, Ashok Kumar Bhatia

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Ocimum sanctum, a well known medicinal plant is used for various alignments in Ayurvedic medicines. It was found to be effective in treating the humans suffering from different viral infections like chicken pox, small pox, measles and influenza. In addition, curative effect of the plant in malignant patients was also reported. In the present study, leaves of this plant were screened against animal viruses i.e. Bovine Herpes Virus-type-1 (BHV-1), Foot and Mouth disease virus (FMDV) and Newcastle Disease Virus (NDV). BHV-1 and FMDV were screened in MDBK and BHK cell lines respectively using cytopathic inhibition test. While NDV was propagated in chick embryo fibroblast culture and tested by haemagglutination inhibition test. Maximum non toxic dose of aqueous extract of Ocimum sanctum leaves was calculated by MTT assay in all the cell cultures and nontoxic doses were used for antiviral activity against viruses. 98.4% and 85.3% protection were recorded against NDV and BHV-1 respectively. However, Ocimum sanctum extract failed to show any inhibitory effect on the cytopathic effect caused by FMD virus. It can be concluded that Ocimum sanctum is a very effective remedy for curing viral infections in animals also.

Keywords: bovine herpes virus-type-1, foot and mouth disease virus, newcastle disease virus, Ocimum sanctum

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Authors: I. L. Ibrahim, A. Mann, B. A. Adam

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This project involved screening for antibacterial activity, phytochemical and mineral properties of Leptadenia hastata by flame photometry. The result of phytochemical screening reveals that the presence of flavonoids, tannins, saponins, alkaloids, steroidal, and anthraquinones while the cardiac glycoside was absent. This justifies the plant been used as anti-bleeding and anti-inflammatory agents. The result of flame photometry revealed that 1.85 % (Na), 0.65% (K) and 1.85 % (Ca) which indicates the safe nature of the plant extract as such could be used to lower high blood pressure. The antibacterial properties of both the aqueous and ethanolic extract were studied against some bacteria, Escherichia coli, Bacillus Cercus, Pseudomonas aeruginas, and Enterobacter aerogegens, by disc diffusion method and the result reveals that there are very good activities against the organism while the ethanolic extract at concentration 1.0 – 1.2 mg/ml. the ethanolic extract showed in considerable zone inhibition against bacteria’s; Escherichia coli, Bacillus Cercus, pseudomonas aeruginosa andklebsellapnemuoniae. Minimum inhibitory concentration (MIC) and minimum Bacterial concentration (MBC) were conducted with fairly good significant effect of inhibition on the organism, therefore, plant extract could be a potential source of antibacterial agent.

Keywords: antibacterial activity, Leptadenia hastata, infectious diseases, phytochemical screening

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Authors: Oluwafemi Ojo, Omotade Oloyede

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This study seeks to investigate the antioxidative properties and the ability of aqueous, ethanolic and ethyl acetate extracts from Ocimum gratissimum (OG) leaves to inhibit some pro-oxidants (Fe2+ and sodium nitroprusside) induced lipid peroxidation in rat’s liver homogenates in vitro. The ability of the extracts to inhibit 25 µM FeSO4 and 7.0 µM sodium nitroprusside induced lipid peroxidation in isolated rat’s liver was determined. The results of the study revealed that both pro-oxidants caused a significantly decrease in (p < 0.05) accumulation of lipid peroxides. However, aqueous extract of OG shows a high ability to inhibit lipid production in the liver induced with SNP than Fe2+. Ethanolic and ethyl acetate extract of OG which shows a high ability to inhibit lipid production more when induced with Fe2+ than SNP. However, ethyl acetate fraction of OG shows a higher inhibitory effect on both Fe2+ and SNP induced lipid peroxidation in rat’s liver. This applies to its significantly higher extractable phytochemicals. Therefore, Fe II and sodium nitroprusside induced oxidative stress could be managed by dietary intake of Ocimum gratissimum leaves.

Keywords: antioxidative, pro-oxidants, lipid peroxidation, Ocimum gratissimum

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Authors: Etienne Sugewe

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Purpose: The establishment of a positive HIV serologic status of an individual could have been an inhibitory factor to prevent risk behaviours in people living with HIV/AIDS. We conducted a cross-sectional study in order to assess the prevalence and predictors of risk behaviors among HIV-positive people in Douala-Cameroon. Methods: We used pre-checked questionnaires to systematically collect data from four HIV treatment centers in Douala. This was done to some of them during the distribution of drugs and to others during their classical rendezvous between the months of May and July 2012. The Chi-Square and Student t-test were used for cross tabulation of variables; multiple regression analysis was performed to identify predictors of risky sexual behaviours. Results: Of the 330 persons interviewed, sixty percent were reported to have had sexual intercourse after the diagnosis of HIV. We obtained 37% HIV-positive partners, and 63% had HIV- negative partners or partners with unknown status. Among our patients, 45% of the subjects with regular partners reported to have had anal or vaginal sex. Those whose score on the knowledge about HIV/AIDS was < 50% and where 90% of them were less susceptible to the condom during intercourse (p: 0.01). About 74% of patients on ARV were less susceptible to the use of condoms during sexual intercourse (p: 0.03). Conclusion: Risk sexual behaviours among people living with HIV/AIDS are common and potentially expose their partners. For HIV-positive partners, these habits pose a real risk of suprainfection by other strains of HIV. The need to increase awareness and education among people living with HIV is therefore highly recommended.

Keywords: HIV/AIDS, behaviours, HIV positive, Douala, 2012

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Authors: Pun Jankrajangjaeng

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Senna garrettiana is a climatic tropical plant in Southeast Asia. Senna garrettiana (Craib) is used as a medicinal plant in Thailand, in which the experiment reported that the plant contains triterpenoids, ligans, phenolics, and fungal metabolites. Thus, it is also reported that the plant possesses interesting biological activity such as antioxidant activity. Therefore, Senna garrettiana is selected to examine the antimicrobial activity. The purpose of this study is to examine the antimicrobial activity of Senna garrettiana (crab) extract against Gram-positive Staphylococcus aureus and Gram-negative Salmonella typhi, and the fungus Candida albicans. This study performed the agar disk-diffusion method and broth microdilution by using five concentrations of plant extract to determine the minimum inhibitory concentration (MIC) of S. garrettiana extract. The result showed that S. garrettiana extract gave the maximum zone inhibition of 11.7 mm, 13.7 mm, and 14.0 mm against S. aureus, S. typhi, and C. albicans, respectively. The MIC value of S. garrettiana against S. aureus was 125 µg/mL while the MIC in S. typhi and C. albicans greater than 2000 µg/mL. To conclude, S. garrettiana extract showed higher sensitivity of antibacterial activity against gram-positive bacteria than gram-negative bacteria. In addition, the plant extracts also possessed antifungal activity. Therefore, further investigation to confirm the mechanism of action of antimicrobial activity in S. garrettiana extract should be performed to identify the target of the antimicrobial action.

Keywords: antimicrobial activity, Candida albicans, Salmonella typhi, Senna garrettiana, Staphylococcus aureus

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Authors: P. Christodoulou, M. Gerasimou, S. Mantzoukis, N. Varsamis, G. Kolliopoulou, N. Zotos

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Abstract— Purpose: The Intensive Care Unit (ICU) environment is conducive to the growth of microorganisms. A variety of microorganisms gain access to the intravascular area and are transported throughout the circulatory system. Therefore, examination of the catheters used in ICU patients is of paramount importance. Material and Method: The culture medium is a catheter tip, which is enriched with Tryptic soy broth (TSB). After one day of incubation, the broth is passaged in the following selective media: Blood, Mac conkey No. 2, chocolate, Mueller Hinton, Chapman, and Saboureaud agar. The above selective media is incubated for 2 days. After this period, if any number of microbial colonies is detected, gram staining is performed and then the microorganisms are identified by biochemical techniques in the automated Microscan (Siemens) system followed by a sensitivity test in the same system using the minimum inhibitory concentration (MIC) technique. The sensitivity test is verified by a Kirby Bauer test. Results: In 2017, the Microbiology Laboratory received 84 catheters from the ICU. 42 were found positive. Of these, S. epidermidis was identified at 8, A. baumannii in 10, K. pneumoniae in 6, P. aeruginosa in 6, P. mirabilis in 3, S. simulans in 1, S. haemolyticus in 4, S. aureus in 3 and S. hominis in 1. Conclusions: The results show that the placement and maintenance of the catheters in ICU patients are relatively successful, despite the unfavorable environment of the unit.

Keywords: culture, intensive care unit, microorganisms, vascular catheters

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Authors: Samy Selim

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Natural products are still major sources of innovative therapeutic agents for various conditions, including infectious diseases. Peganum harmala L. oil had wide range uses as traditional medicinal plants. The current study was designed to evaluate the antibacterial activity of P. harmala essential oil. The chemical constitutes and toxicity of these oils was also determined to obtain further information on the correlation between the chemical contents and antibacterial activity. The antibacterial effect of the essential oils of P. harmala oil was studied against some foodborne pathogenic bacteria species. The oil of plant was subjected to gas chromatography-mass spectrometry (GC/MS). The impact of oils administration on the change in rate of weight gain and complete blood picture in hamsters were investigated. P. harmala oil had strong antibacterial effect against bacterial species especially at minimum inhibitory concentration (MIC) less than 75.0 μg/ml. From the oil of P. harmala, forty one compounds were identified, and the major constituent was 1-hexyl-2-nitrocyclohexane (9.07%). Acute toxicity test was performed on hamsters and showed complete survival after 14 days, and there were no toxicity symptoms occurred. This study demonstrated that these essential oils seemed to be destitute of toxic effect which could compromise the medicinal use of these plants in folk medicine.

Keywords: analysis mass spectrometry, antibacterial activities, acute toxicity, chemical constitutes, gas chromatography, weight gain, Peganum harmala

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Authors: Bingjie Wang, Su-Yeon Kwon, Ik-Joong Kang

Abstract:

The goal of this experiment is to develop a sensor that can quickly check the concentration by using the nanoparticles made by chitosan and gold. Using chitosan nanoparticles crosslinking with sodium tripolyphosphate(TPP) is the first step to form the chitosan nanoparticles, which would be covered with the gold sequentially. The size of the fabricated product was around 100nm. Based on the method that the sulfur end of the MPA linked to gold can form the very strong S–Au bond, and the carboxyl group, the other end of the MPA, can easily absorb the GABA. As for the GABA, what is the primary inhibitory neurotransmitter in the mammalian central nervous system in the human body. It plays such significant role in reducing neuronal excitability pass through the nervous system. A Surface-enhanced Raman Scattering (SERS) as the principle for enhancing Raman scattering by molecules adsorbed on rough metal surfaces or by nanostructures is used to detect the concentration change of γ-Aminobutyric Acid (GABA). When the system is formed, it generated SERS, which made a clear difference in the intensity of Raman scattering within the range of GABA concentration. So it is obtained from the experiment that the calibration curve according to the GABA concentration relevant with the SERS scattering. In this study, DLS, SEM, FT-IR, UV, SERS were used to analyze the products to obtain the conclusion.

Keywords: mercaptopropionic acid, chitosan-gold nanoshell, γ-aminobutyric acid, surface-enhanced raman scattering

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Authors: Uzma Saqib, Mirza S. Baig

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Myeloid differentiation primary response protein 88 (MYD88) has long been considered a central player in the inflammatory pathway. Recent studies clearly suggest that it is an important therapeutic target in inflammation. On the other hand, a recent study on the interaction between the orphan nuclear receptor (Nur77) and p38α, leading to increased lipopolysaccharide-induced hyperinflammatory response, suggests this binary complex as a therapeutic target. In this study, we have designed inhibitors that can inhibit both MYD88 and Nur77 at the same time. Since both MYD88 and Nur77 are an integral part of the pathways involving lipopolysaccharide-induced activation of NF-κB-mediated inflammation, we tried to target both proteins with the same library in order to retrieve compounds having dual inhibitory properties. To perform this, we developed a homodimeric model of MYD88 and, along with the crystal structure of Nur77, screened a virtual library of compounds from the traditional Chinese medicine database containing ~61,000 compounds. We analyzed the resulting hits for their efficacy for dual binding and probed them for developing a common pharmacophore model that could be used as a prototype to screen compound libraries as well as to guide combinatorial library design to search for ideal dual-target inhibitors. Thus, our study explores the identification of novel leads having dual inhibiting effects due to binding to both MYD88 and Nur77 targets.

Keywords: drug design, Nur77, MYD88, inflammation

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Authors: Y. S. Mohamed, L. A. Ahmed, H. A. Salem, A. M. Agha

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Liver Fibrosis is one of the most serious conditions that affect the Egyptian society. In the present study, the effect of nicorandil was investigated in experimentally-induced liver fibrosis by bile duct ligation in rats. Nicorandil (3mg/kg/day) was given orally 24 h after bile duct ligation for 14 days till the end of the experiment. Nicorandil group showed a significant improvement in liver function tests (ALT and ALP) as well as a significant decrease in oxidative stress biomarkers (TBARS and GSH), area of fibrosis and activity of hepatic stellate cells as indicated by decreased expression of alpha smooth muscle actin.Moreover, nicorandil treatment decreased HSCs proliferation due to its inhibitory effects on protein kinase C(PKC) and Platelet derived growth factor (PDGF) . Oral administration of either glibenclamide (10 mg/kg/day)(a KATP channel blocker) or L-NAME (30 mg/kg/day) (an inhibitor of nitric oxide synthase) blocked the protective effects of nicorandil. However, nicorandil and L-NAME treated group showed more or less results similar to that of untreated bile duct ligated group. In conclusion, nicorandil was effective against the development of bile duct ligated-induced liver fibrosis in rats where activation of the NO pathway plays an important role in the protective effect nicorandil.

Keywords: hepatic stellate cells, nicorandil, nitric oxide donor, liver fibrosis

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Authors: Maria Borawska, Patryk Nowakowski, Sylwia K. Naliwajko, Renata Markiewicz-Zukowska, Anna Puscion-Jakubik, Krystyna Gromkowska-Kepka, Justyna Moskwa

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Coprinus comatus (O. F. Müll.) Pers.) should not be confused with the common Ink Cap, which contains coprine and can induce coprine poisoning. We study the possibility of applying coprinus mushroom (Coprinus comatus), available in Poland, as food product supporting the treatment of human glioblastoma cells. The U87MG and T98 glioblastoma cell lines were exposed to water (CW) or ethanol 95° (CE) Cantharellus extracts (50-500 μg/ml), with or without temozolomide (TMZ) during 24, 48 or 72 hours. The cell division was examined by the H³-thymidine incorporation. The statistical analysis was performed using Statistica v. 13.0 software. Significant differences were assumed for p < 0.05. We found that both, CW and CE, administrated alone, had inhibitory effect on cell lines growth, but the CE extract had a higher degree of growth inhibition. The anti-tumor effect of TMZ (50 μM) on U87MG was enhanced by mushroom extracts, and the effect was lower to the effect after using Coprinus comatus extracts (CW and CE) alone. A significant decrease (p < 0.05) in pro-MMP2 (82.61 ± 6.3% of control) secretion in U87MG cells was observed after treated with CE (250 μg/ml). We conclude that extracts of Coprinus comatus, edible mushroom, present cytotoxic properties on U87MG and T98 cell lines and may cooperate with TMZ synergistically enhancing its growth inhibiting activity against glioblastoma U87MG cell line.

Keywords: anticancer, glioma, mushroom, temozolomide

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Authors: Nattawit Thiapairat

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Multiple diseases have been linked to excessive levels of free radicals, which cause tissue or cell damage as a result of oxidative stress. Many plants are sources of high antioxidant activity. Derris scandens has a high amount of phenolic and flavonoid contents which demonstrated good biological activities. This study focused on the antioxidant activity of polyphenols extracted from D. scandens. This study performs total flavonoids content and various antioxidant assays, which were 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity assays. The total flavonoid content of D. scandens extract was determined and expressed as quercetin equivalents (QE)/g measured by the aluminum chloride colorimetric method. The antioxidant activity of D. scandens extract was also determined by DPPH and ABTS assays. In the DPPH assay, vitamin C was used as a positive control, whereas Trolox was used as a positive control in the ABTS assay. The half-maximal inhibitory concentration (IC50) values for D. scandens extract from DPPH and ABTS assays were 41.79 μg/mL ± 0.783 and 29.42 μg/mL ± 0.890, respectively, in the DPPH assay. To conclude, D. scandens extract consists of a high amount of total phenolic content, which exhibits a significant antioxidant activity. However, further investigation regarding antioxidant activity such as SOD, ROS, and RNS scavenging assays and in vivo experiments should be performed.

Keywords: ABTS assay, antioxidant activity, Derris scandens, DPPH assays, total flavonoid content

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Authors: Emad Heydarnia, Aref Sepasi, Nika Asefi, Sara Khakshournia, Javad Mohammadnejad

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Background: Despite breakthrough therapeutics in breast cancer, it is one of the main causes of mortality among women worldwide. Thus, drug therapies for treating breast cancer have recently been developed by scientists. Metformin and Sorafenib are well-known therapeutic in breast cancer. In the present study, we combined Sorafenib and PCL-sorafenib with metformin to improve drug absorption and promote therapeutic efficiency. Methods: The MCF-7 cells were treated with Metformin, Sorafenib, or PCL-sorafenib. The growth inhibitory effect of these drugs and cell viability were assessed using MTT and flow cytometry assays, respectively. The expression of targeted genes involved in cell proliferation, signaling, and the cell cycle was measured by Real-time PCR. Results: The results showed that MCF-7 cells treated with Metformin/Sorafenib and PCL-sorafenib/Metformin co-treatment contributed to 50% viability compared to untreated group. Moreover, PI and Annexin V staining tests showed that the cells viability for Metformin/Sorafenib and PCL-sorafenib/Metformin was 38% and 17%, respectively. Furthermore, Sorafenib/Metformin and PCL-sorafenib/Metformin leads to p53 gene expression increase by which they can increase ROS, thereby decreasing GPX4 gene expression. In addition, they affected the expression of BCL2, and BAX genes and altered the cell cycle. Conclusion: Together, the combination of PCL-sorafenib/Metformin and Sorafenib/Metformin increased Sorafenib absorption at lower doses and also leads to apoptosis and oxidative stress increases in MCF-7 cells.

Keywords: breast cancer, metformin, nanotechnology, sorafenib

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Authors: Nematollah Gheibi, Nader Divan Khosroshahi, Mahdi Mohammadi Ghanbarlou

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Introduction: Nowadays, the phenomenon of bacterial resistance is one of the most important challenge of the health community in the world. Propolis is most important production of bee colonies that collected from of various plants. So far, a lot of investigations carried out about its antibacterial effects. Material and methods: Thirty gram of propolis prepared as ethanolic extract and after different process of purification, 7.5 gr of its pure form were obtained. Propolis compounds identification was performed by TLC and VLC methods. The HPLC spectrum obtaining from propolis ethanolic extract was compared with some purified standard phenolic and flavonoid substances. Antibacterial effects of ethanol extract of purified propolis were evaluated on two strains of Staphylococcus aureus and Pseudomonas aeruginosa and their MIC was determined by the microdillution assay. Results: Ethanolic propolis extraction analyzed by TLC were resulted to confirm several phenolic and flavonoid compounds in this extract and some of the confirmed by HPLC technique. Minimum inhibitory concentration (MIC) for standard Staphylococcus aureus (ATCC25923) and Pseudomonas aeruginosa (ATCC27853) strains were obtained 2.5 mg/ml and 50 mg/ml respectively. Conclusion: Bee Propolis is a mix organic compound that has a lot of beneficial effects such as anti-bacterial that emphasized in this investigation. It is proposed as a rich source of natural phenolic and flavonoids compounds in designing of new biological resources for hygienic and medical applications.

Keywords: propolis, Staphylococcus aureus, Pseudomonas aeruginosa, antibacterial

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Authors: Anjali Verma, Mahesh Pal, Veena Pande, Dalip Kumar Upreti

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The present study is carried out to explore the anti-hyperglycemic activity of Leucas cephalotes plant parts. A fruit, leaves, stems, and roots part of the Leucas cephalotes has been extracted in ethanol and have been evaluated for anti-hyperglycemic activity. The present study indicated that, ethanolic extract of fruit and leaves have shown significant α- amylase inhibitory activity with IC50 value of 92.86 ± 0.89 μg/mL and 98.09 ± 0.69 μg/mL respectively. Two known compounds β-sitosterol and lupeol were isolated from ethanolic extract of L. cephalotes leaves and were subjected to anti-hyperglycemic activity. Lupeol shows the best activity with IC50 55.73 ± 0.47 μg/mL and the results were verified by docking study of these compounds with mammalian α-amylase was carried out on its active site. It was concluded from the study that β-sitosterol and lupeol form one H-bond interactions with the active site residues either Asp212 or Thr21. The estimated free energy binding of β-sitosterol was found to be -9.47 kcal mol-1 with an estimated inhibition constant (Ki) of 558.94 nmol whereas the estimated free energy binding of lupeol was -11.73 kcal mol-1 with an estimated inhibition constant (Ki) of 476.71pmmol. The present study clearly showed that lupeol is more potent in comparison to β-sitosterol. The study indicates that L. cephalotes have significant potential to inhibit α-amylase enzyme.

Keywords: alpha-amylase, beta-sitosterol, hyperglycemia, lupeol

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Authors: Chona Gelani, Mylene Uy, Keisuke Yasuda, Emi Ohta, Shinji Ohta

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The marine environment is undoubtedly a rich source of diverse organisms that possess bioactive secondary metabolites with important pharmacological activities. Marine sponges have since been contributing a wide array of compounds of biomedical and pharmaceutical importance. This study is an attempt to contribute to the growing and advancing marine natural products research. It aims to evaluate the cytotoxicity of the hexane extract (H) from the Philippine marine sponges, Rhabdastrella globostellata (Rg), Callyspongia sp. (Calsp), Callyspongia aerizusa (Ca), Carteriospongia sp. (Carsp), and Cinachyrella sp. (Cisp) using the eggs of starfish, Asterina pectinifera, and sea urchin, Hemicentrotus pulcherrimus. Specifically, the cytotoxicity of the marine sponge hexane extract was determined through its inhibition of starfish and sea urchin embryonic development. After 24 hours, CarspH and RgH inhibited early gastrulation of sea urchin at a minimum concentration of 15.63 and 31.25 μg/mL, respectively. CalspH inhibited the early gastrulation of both sea urchin and starfish at 125 μg/mL, whereas CaH halted the morula of sea urchin and early gastrulation of starfish at 250 μg/mL. CispH exhibited relatively weak inhibitory activity on starfish embryogenesis but inhibited the early gastrulation of sea urchin at 250 μg/mL. The results obtained from this study were used as basis for the separation, isolation and purification of the component(s) of the hexane extracts from the five Philippine marine sponges.

Keywords: embryonic development, marine sponge cytotoxicity, Philippine marine sponges, sea urchin and starfish embryogenesis

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Authors: Bernice Jeanne Lottering, Yi-Wen Lin

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Introduction: Chronic pain has a definitive lack of objective parameters in the measurement and treatment efficacy of diseases such as Fibromyalgia (FM). Persistent widespread pain and generalized tenderness are the characteristic symptoms affecting a large majority of the global population, particularly females. This disease has indicated a refractory tendency to conventional treatment ventures, largely resultant from a lack of etiological and pathogenic understanding of the disease development. Emerging evidence indicates that the central nervous system (CNS) plays a critical role in the amplification of pain signals and the neurotransmitters associated therewith. Various stimuli have been found to activate the channels existent on nociceptor terminals, thereby actuating nociceptive impulses along the pain pathways. The transient receptor potential vanalloid 1 (TRPV1) channel functions as a molecular integrator for numerous sensory inputs, such as nociception, and was explored in the current study. Current intervention approaches face a multitude challenges, ranging from effective therapeutic interventions to the limitation of pathognomonic criteria resultant from incomplete understanding and partial evidence on the mechanisms of action of FM. It remains unclear whether electroacupuncture (EA) plays an integral role in the functioning of the TRPV1 pathway, and whether or not it can reduce the chronic pain induced by FM. Aims: The aim of this study was to explore the mechanisms underlying the activation and modulation of the TRPV1 channel pathway in a cold stress model of FM applied to a murine model. Furthermore, the effect of EA in the treatment of mechanical and thermal pain, as expressed in FM was also to be investigated. Methods: 18 C57BL/6 wild type and 6 TRPV1 knockout (KO) mice, aged 8-12 weeks, were exposed to an intermittent cold stress-induced fibromyalgia-like pain model, with or without EA treatment at ZusanLi ST36 (2Hz/20min) on day 3 to 5. Von Frey and Hargreaves behaviour tests were implemented in order to analyze the mechanical and thermal pain thresholds on day 0, 3 and 5 in control group (C), FM group (FM), FM mice with EA treated group (FM + EA) and FM in KO group. Results: An increase in mechanical and thermal hyperalgesia was observed in the FM, EA and KO groups when compared to the control group. This initial increase was reduced in the EA group, which directs focus at the treatment efficacy of EA in nociceptive sensitization, and the analgesic effect EA has attenuating FM associated pain. Discussion: An increase in the nociceptive sensitization was observed through higher withdrawal thresholds in the von Frey mechanical test and the Hargreaves thermal test. TRPV1 function in mice has been scientifically associated with these nociceptive conduits, and the increased behaviour test results suggest that TRPV1 upregulation is central to the FM induced hyperalgesia. This data was supported by the decrease in sensitivity observed in results of the TRPV1 KO group. Moreover, the treatment of EA showed a decrease in this FM induced nociceptive sensitization, suggesting TRPV1 upregulation and overexpression can be attenuated by EA at bilateral ST36. This evidence compellingly implies that the analgesic effect of EA is associated with TRPV1 downregulation.

Keywords: fibromyalgia, electroacupuncture, TRPV1, nociception

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Authors: Yik Ling Chew, Adlina Maisarah Mahadi, Joo Kheng Goh

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Bauhinia kockiana originates from Peninsular Malaysia, and it is grown as a garden ornamental plant. However, it is used as medicinal plant by Malaysia ‘Kelabit’ ethic group in treating various diseases and illnesses. This study focused on the assessment of the antibacterial activity of B. kockiana towards MRSA, to purify and identify the antibacterial compounds, and to determine the mechanism of antibacterial activity. Antibacterial activity of B. kockiana flower is evaluated qualitatively and quantitatively using disc diffusion assay and microbroth dilution method to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of extracts. Phytochemical analysis is performed to determine the classes of phytochemicals in the extracts. Bioactivity-guided isolation is performed to purify the antibacterial agents and identified the chemical structures via various spectroscopy methods. Scanning electron microscopy (SEM) technique is adopted to evaluate the antibacterial mechanism of extract and compounds isolated. B. kockiana flower is found to exhibit fairly strong antibacterial activity towards both strains of MRSA bacteria. Gallic acid and its ester derivatives are purified from ethyl acetate extract and the antibacterial activity is evaluated. SEM has revealed the mechanism of the extracts and compounds isolated.

Keywords: alkyl gallates, Bauhinia kockiana, MRSA, scanning electron microscopy

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Authors: Rayhaneh Amooaghaie, Maryam Norouzi

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In this study, the effects of nTiO₂ on seed germination and growth of six plant species (wheat, soybean, tomato, canola, cucumber, and lettuce) were evaluated in petri dish (direct exposure) and in soil in a greenhouse experiment (soil exposure). Data demonstrate that under both culture conditions, low or mild concentrations of nTiO₂ either stimulated or had no effect on seed germination, root growth and vegetative biomass while high concentrations had an inhibitory effect. However, results showed that the impacts of nTiO₂ on plant growth in soil were partially consistent with those observed in pure culture. Based on both experiment sets, among above six species, lettuce and canola were the most susceptible and the most tolerant species to nTiO₂ toxicity. However, results revealed the impacts of nTiO₂ on plant growth in soil were less than petri dish exposure probability due to dilution in soil and complexation/aggregation of nTiO₂ that would lead to lower exposure of plants. The high concentrations of nTiO₂ caused significant reductions in fresh and dry weight of aerial parts and root and chlorophyll and carotenoids contents of all species which also coincided with further accumulation of malondialdehyde (MDA). These findings suggest that decreasing growth might be the result of an nTiO₂-induced oxidative stress and disturbance of photosynthesis systems.

Keywords: chlorophyll, lipid peroxidation, nano TiO₂, seed germination

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Authors: Hae-Jun Lee, Ji-Sun Shin, Kyung-Tae Lee

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Potentilla species (Rosasease) have been used in traditional medicine to treat different ailment, disease or malady. In this study, we investigated the anti-inflammatory effects of ethanol extracts of NUTT (EPP) in lipopolysaccharide (LPS)-induced Raw 264.7 macrophages and septic mice. EPP suppressed LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE2) production in LPS-induced Raw 264.7 macrophages. Consistent with these observations, EPP reduced the expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) by downregulation of their promoter activities. EPP inhibited tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and interleukin-1β (IL-1β) at production and mRNA levels. Molecularly, EPP attenuated the LPS-induced transcriptional activity, and DNA-binding activity of nuclear factor-κB (NF-κB), and this was associated with a decrease of translocation and phosphorylation of p65 NF-κB by inhibiting the inhibitory κB-α (IκB-α) degradation and IκB kinase-α/β (IKK-α/β) phosphorylation. Furthermore, EPP suppressed the LPS-induced activation of activator protein-1 (AP-1) by reducing the expression of c-Fos and c-Jun in nuclear. EPP also reduced the phosphorylation of mitogen-activated protein kinase (MAPK), such as p38 MAPK and c-Jun N-terminal kinase/stress-activated protein kinase (JNK). In a sepsis model, pretreatment with EPP reduced the LPS-induced lethality. Collectively, these results suggest that the anti-inflammatory effects of EPP were associated with the suppression of NF-κB and AP-1 activation, and support its possible therapeutic role for the treatment of sepsis.

Keywords: anti-inflammation, activator protein-1, nuclear factor κB, Potentilla paradoxa Nutt

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Authors: K. Julia Rose Mary, Victor Arokia Doss

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Electrical and chemical stimulations up-regulate phosphorylaion of CREB, a transcriptional factor that induces its target gene production for memory consolidation and Late Long-Term Potentiation (L-LTP) in CA1 region of the hippocampus. L-LTP requires complex interactions among second-messenger signaling cascade molecules such as cAMP, CAMKII, CAMKIV, MAPK, RSK, PKA, all of which converge to phosphorylate CREB which along with CBP induces the transcription of target genes involved in memory consolidation. A differential equation based model for L-LTP representing stimulus-mediated activation of downstream mediators which confirms the steep, supralinear stimulus-response effects of activation and inhibition was used. The same was extended to accommodate the inhibitory effect of the Inducible cAMP Early Repressor (ICER). ICER is the natural inducible CREB antagonist represses CRE-Mediated gene transcription involved in long-term plasticity for learning and memory. After verifying the sensitivity and robustness of the model, we had simulated it with various empirical levels of repressor concentration to analyse their effect on the gene induction. The model appears to predict the regulatory dynamics of repression on the L-LTP and agrees with the experimental values. The flux data obtained in the simulations demonstrate various aspects of equilibrium between the gene induction and repression.

Keywords: CREB, L-LTP, mathematical modeling, simulation

Procedia PDF Downloads 294