Search results for: in vitro metabolites

Authors: Prasanthi Malapati, R. Reshma, Vijay Soni, Perumal Yogeeswari, Dharmarajan Sriram

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In the present study, we attempted to develop Mycobacterium tuberculosis (Mtb) inhibitors by exploring the pharmaceutically underexploited enzyme targets which are majorly involved in cell wall biosynthesis of mycobacteria. For this purpose, glutamate racemase (coded by MurI gene) was selected. This enzyme racemize L-glutamate to D-glutamate required for the construction of peptidoglycan in the bacterial cell wall synthesis process. Furthermore this enzyme is neither expressed nor its product, D-glutamate is normally found in mammals, and hence designing inhibitors against this enzyme will not affect the host system as well act as potential antitubercular drugs. A library of BITS in house compounds were screened against Mtb MurI enzyme. Based on docking score, interactions and synthetic feasibility one hit lead was identified. Further optimization of lead was attempted and its derivatives were synthesized. Forty eight derivatives of 2-phenylbenzo[d]oxazole and 2-phenylbenzo[d]thiazole were synthesized and evaluated for Mtb MurI inhibition study, in vitro activities against Mtb, cytotoxicity against RAW 264.7 cell line. Chemical derivatization of the lead resulted in compounds NR-1213 AND NR-1124 as the potent M. tuberculosis glutamate racemase inhibitors with IC50 of 4-5µM which are remarkable and were found to be non-cytotoxic. Molecular dynamics, dormant models and cardiotoxicity studies of the most active molecules are in process.

Keywords: cell wall biosynthesis, dormancy, glutamate racemase, tuberculosis

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Authors: S. S. Patil, R. M. Mhetre, S. V. Patil

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Lisinopril is an angiotensin converting enzyme inhibitor used in the treatment of hypertension and heart failure in prophylactic treatment after myocardial infarction and in diabetic nephropathy. However, it is very poorly absorbed from gastro-intestinal tract. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers provide a significant increase in the nasal residence time. The aim of the present approach was to overcome the drawbacks of the conventional dosage forms of lisinopril by formulating intranasal microspheres with Carbopol 974P NF and HPMC K4 M along with film forming polymer ethyl cellulose.The microspheres were prepared by emulsion solvent evaporation method. The prepared microspheres were characterized for encapsulation efficiency, drug loading, particle size, and surface morphology, degree of swelling, ex vivo mucoadhesion, drug release, ex vivo diffusion studies. All formulations has shown entrapment efficiency between 80 to more than 95%, mucoadhesion was more than 80 % and drug release up to 90 %. Ex vivo studies revealed tht the improved bioavailability of drug compared to oral drug administration. Both in vitro and in vivo studies conclude that combination of Carbopol and HPMC based microspheres shown better results than single carbopol based microspheres for the delivery of lisinopril.

Keywords: microspheres, lisinopril, nasal delivery, solvent evaporation method

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Authors: A. A. Dehpour, B. Eslami, S. Rezaie, S. F. Hashemian, F. Shafie, M. Kiaie

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The aims of study were investigation on chemical composition essential oil and the effect of extract of Coronilla varia on antimicrobial and cytotoxicity activity. The essential oils of Coronilla varia is obtained by hydrodistillation and analyzed by (GC/MS) for determining their chemical composition and identification of their components. Antibacterial activity of plant extract was determined by disc diffusion method. The effect of hydroalcolic extracts from Cornilla varia investigated on MCF7 cancer cell line by MTT assay. The major components were Caryophyllene Oxide (60.19%), Alphacadinol (4.13%) and Homoadantaneca Robexylic Acid (3.31%). The extracts from Coronilla varia had interesting activity against Proteus mirabilis in the concentration of 700 µg/disc and did not show any activity against Staphylococus aureus, Bacillus subtillis, Klebsiella pneumonia and Entrobacter cloacae. The positive control, Ampicillin, Chloramphenicol and Cenphalothin had shown zone of inhibition resistant all bacteria. Corohilla varia ethanol extract could inhibit the proliferation of MCF7 cell line in RPMI 1640 medium. IC50 5(mg/ml) was the optimum concentration of extract from Coronilla varia inhibition of cell line growth. The MCF7 cancer cell line and Proteus mirabilis were more sensitive to Coronilla varia ethanol extract.

Keywords: Coronilla varia, essential oil, antibacterial, anticancer, hela cell line

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Authors: Rania F. Ahmed, Sally A. El Awdan, Gehad A. Abdel Jaleel, Dalia O. Saleh, Omar A. H. Ahmed-Farid

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The metabolic syndrome is an important public health concern often related to obesity, improper diet, and sedentary lifestyles and can predispose individuals to the development of many dangerous health conditions, disability and early death. This research aimed to investigate the efficacy of resveratrol (RSV) to reverse the neuro-complications associated with metabolic syndrome experimentally-induced in rats using an eight weeks high fat, high fructose diet (HFHF) model. The corresponding drug treatments were administered orally during the last 10 days of the diet. Behavioural tests namely the open field test (OFT) and the forced swimming test (FST) were conducted. Brain levels of monoamines viz. serotonin, norepinephrine and dopamine as well as their metabolites were assessed. 8-hydroxyguanosine (8-OHDG) as an indicative of DNA-fragmentation, nitric oxide (NOx) and tumor necrosis factor-α (TNF- α) were estimated. Finally, brain antioxidant parameters namely malondialdehyde (MDA), reduced and oxidized glutathione (GSH, GSSG) were evaluated. HFHF-induced metabolic syndrome resulted in decreased activity in the OFT and increased immobility duration in the FST. Furthermore, HFHF-induced metabolic syndrome lead to a significant increase in brain monoamines turn over as well as elevation in 8-OHDG, NOx, TNF- α, MDA and GSSG; and reduction in GSH. Ten days daily treatment with RSV (20 and 40 mg/kg p.o) dose dependently increased activity in the OFT and decreased immobility duration in the FST. Moreover, RSV normalized brain monoamines contents, reduced 8-OHDG, NOx, TNF- α, MDA and GSSG; and elevated GSH. In conclusion, we can say that RSV showed neuro-protective properties against HFHF-induced metabolic syndrome represented by monoamines preservation, prevention of neurodegeneration, anti-inflammatory and antioxidant potentials and could be recommended as a beneficial daily dietary supplement to treat the neuronal side effects associated with HFHF-induced metabolic syndrome.

Keywords: antioxidants, DNA-fragmentation, forced swimming test, HFHF-induced metabolic syndrome, monoamines, nitric oxide (NOx), open field, resveratrol, tumor necrosis factor-α (TNF- α), 8-hydroxyguanosine (8-OHDG)

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Authors: E. Ormeno, C. Gutigny, J. Ruffault, J. Madrigal, M. Guijarro, C. Lecareux, C. Ballini

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Mediterranean plant species feature numerous metabolic and morpho-physiological responses crucial to survive under both, typical Mediterranean drought conditions and future aggravated drought expected by climate change. Whether these adaptive responses will, in turn, increase the ecosystem perturbation in terms of fire hazard, is an issue that needs to be addressed. The aim of this study was to test whether recurrent and aggravated drought in the Mediterranean area favors the accumulation of waxes in leaf litter, with an eventual increase of litter flammability. The study was conducted in 2017 in a garrigue in Southern France dominated by Quercus coccifera, where two drought treatments were used: a treatment with recurrent aggravated drought consisting of ten rain exclusion structures which withdraw part of the annual precipitation since January 2012, and a natural drought treatment where Q. coccifera stands are free of such structures and thus grow under natural precipitation. Waxes were extracted with organic solvent and analyzed by GC-MS and litter flammability was assessed through measurements of the ignition delay, flame residence time and flame intensity (flame height) using an epiradiator as well as the heat of combustion using an oxygen bomb calorimeter. Results show that after 5 years of rain restriction, wax content in the cuticle of leaf litter increases significantly compared to shrubs growing under natural precipitation, in accordance with the theoretical knowledge which expects increases of cuticle waxes in green leaves in order to limit water evapotranspiration. Wax concentrations were also linearly and positively correlated to litter flammability, a correlation that lies on the high flammability own to the long-chain alkanes (C25-C31) found in leaf litter waxes. This innovative investigation shows that climate change is likely to favor ecosystem fire hazard through accumulation of highly flammable waxes in litter. It also adds valuable information about the types of metabolites that are associated with increasing litter flammability, since so far, within the leaf metabolic profile, only terpene-like compounds had been related to plant flammability.

Keywords: cuticular waxes, drought, flammability, litter

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Authors: Sanja O. Podunavac-Kuzmanović, Lidija R. Jevrić, Strahinja Z. Kovačević

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In last decade, metal-organic complexes have captured intensive attention because of their wide range of biological activities such as antibacterial, antifungal, anticancerous, antimicrobial and antiHIV. Therefore, it is of great importance for the development of coordination chemistry to explore the assembly of functional organic ligands with metal ion and to investigate the relationship between the structure and property. In view of our studies, we reasoned that benzimidazoles complexed to metal ions could act as a potent antibacterial agents. Thus, we have bioassayed the inhibitory potency of benzimidazoles and their metal salts (Co or Ni) against Gram negative bacteria Escherichia coli. In order to validate our in vitro study, we performed in silico studies using molecular docking software’s. The investigated compounds and their metal complexes (Co, Ni) showed good antibacterial activity against Escherichia coli. In silico docking studies of the synthesized compounds suggested that complexed benzimidazoles have a greater binding affinity and enhanced antibacterial activity in comparison with noncomplexed ligands. In view of their enhanced inhibitory properties we propose that the studied complexes can be used as potential pharmaceuticals. This study is financially supported by COST action CM1306 and the project No. 114-451-347/2015-02, financially supported by the Provincial Secretariat for Science and Technological Development of Vojvodina.

Keywords: benzimidazoles, complexes, antibacterial, Escherichia coli, metal

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Authors: Jae-Hyung Jin, Kyung-Tae Lee, Yee-Seul So, Eunji Jeong, Yeonseon Lee, Dongpil Lee, Dong-Gi Lee, Yong-Sun Bahn

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Cryptococcus neoformans causes cryptococcal meningoencephalitis mainly in immunocompromised patients as well as immunocompetent people. But therapeutic options are limited to treat cryptococcosis. Some signaling pathways including cyclic AMP pathway, MAPK pathway, and calcineurin pathway play a central role in the regulation of the growth, differentiation, and virulence of C. neoformans. To understand signaling networks regulating the virulence of C. neoformans, we selected the 114 putative phosphatase genes, one of the major components of signaling networks, in the genome of C. neoformans. We identified putative phosphatases based on annotation in C. neoformans var. grubii genome database provided by the Broad Institute and National Center for Biotechnology Information (NCBI) and performed a BLAST search of phosphatases of Saccharomyces cerevisiae, Aspergillus nidulans, Candida albicans and Fusarium graminearum to Cryptococcus neoformans. We classified putative phosphatases into 14 groups based on InterPro phosphatase domain annotation. Here, we constructed 170 signature-tagged gene-deletion strains through homologous recombination methods for 91 putative phosphatases. We examined their phenotypic traits under 30 different in vitro conditions, including growth, differentiation, stress response, antifungal resistance and virulence-factor production.

Keywords: human fungal pathogen, phosphatase, deletion library, functional genomics

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Authors: V. Krishna, Shashikumar

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Edible Bananas (Musa spp.) are the major staple food for rural and urban consumers in India and an important source of rural income. The cultivar Musa paradisiaca cv. Karibale Monthan is an endemic cultivar of Malnad region of Karnataka and used as a glomolueroprotective neutraceutical to solve kidney problems. The protocol for mass multiplication of plantlets for this indigenous banana cultivar Karibale Monthan has not yet been standardized so far. In the present study, an attempt has been made to develop high frequency in vitro regeneration protocol and evaluation of morphoagronomic characteristics in the farmyard. The high frequency shoot initiation (93.33 %) was recorded at the synergetic effect of BAP (2 to 8mg/L), TDZ (0.1 to 1.2mg/L) and coconut water (0.1 to 1.2ml/L). It was optimized at the concentration 5 mg/l BAP, 0.5 mg/l TDZ and 0.5 ml/l coconut water with 15.90 ± 1.66 frequency of shoots per propagule. Supplementation of 1.0 mg/l IBA induces 5.33 ± 1.21 numbers of roots with a mean root length of 7.50 ± 1.87 roots. 99% of plantlets with distinct roots and shoots were successfully acclimatized in the green house and transferred to the field to evaluate the agro-morphological variations. The micropropagated plants showed significantly higher morphometric values for height of the plant (16.80±2.17), number of leaves (12.40±1.14), length of the bunch (56.20±2.17), weight of the bunch (13.60±1.14), number of hands in a bunch (11.40±1.14) and girth of the pseudostem (49.80±1.48) when compared with in vivo plants.

Keywords: banana cv. Karibale Monthan, neutraceutical, high-frequency regeneration, morphometric evaluation

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Authors: Anna Jagielska

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Five years ago, the word ‘gender’ was discussed in Poland exclusively in academic contexts. One year later, it was chosen as the word of the year and omnipresent in the Polish media. The rapid career of this word is due to the involvement of the Polish church hierarchy who strategically brought this term into relation with abortion, pornography and paedophilia. ‘Gender’ is more than a political slogan. It is a symbol of social anxiety and moral panic in Poland which need to be historically considered. The aim of this paper is to present selected rhetorical strategies used by the Polish Catholic clergy who strive to have an impact on the current gender discourse in Poland. In particular, the gender debate, culminated in the pastoral letter of the Bishops' Conference of Poland, will be discussed. The church’s protest against the Council of Europe’s Convention on Preventing and Combating Violence against Women and Domestic Violence will be analyzed and the recent heated debates in Poland on contraception, abortion, in vitro fertilization, and sex education will be mentioned. To provide explanations on the specificity of Polish gender debates the role of the Catholic Church in the fall of communism in Poland as well as the charismatisation of Polish society by Pope John Paul II will be explained. The social constructions of communism and feminism which are manifested in both written and symbolic contracts on gender equality between the Church and the State will be demonstrated. At the end of the paper, theories about the changing role of religion in society will be applied.

Keywords: gender, Poland, religion, catholicism, feminism

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Authors: Mai M. Farid, Mona El-Shabrawy, Sameh R. Hussein, Ahmed Elkhateeb, El-Said S. Abdel-Hameed, Mona M. Marzouk

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Asphodelus aestivus Brot. Is a wild plant distributed in Egypt and is considered one of the five Asphodelus spp. from the family Asphodelaceae; it grows in dry grasslands and on rocky or sandy soil. The chemical components of A. aestivus flowers extract were analyzed using different chromatographic and spectral techniques and led to the isolation of two anthraquinones identified as emodin and emodin-O-glucoside. In addition to, five flavonoid compounds;kaempferol,Kaempferol-3-O-glucoside,Apigenin-6-C-glucoside-7-O-glucoside (Saponarine), luteolin 7-O-β-glucopyranoside, Isoorientin-O-malic acid which is a new compound in nature. The LC-ESI-MS/MS analysis of the flower extract of A. aestivus led to the identification of twenty- two compounds characterized by the presence of flavones, flavonols, and flavone C-glycosides. While GC/MS analysis led to the identification of 24 compounds comprising 98.32% of the oil, the major components of the oil were 9, 12, 15-Octadecatrieoic acid methyl ester 28.72%, and 9, 12-Octadecadieroic acid (Z, Z)-methyl ester 19.96%. In vitro cytotoxic activity of the aqueous methanol extract of A. aestivus flowers against HEPG2, HCT-116, MCF-7, and A549 culture was examined and showed moderate inhibition (62.3±1.1)% on HEPG2 cell line followed by (36.8±0.2)% inhibition on HCT-116 and a weak inhibition (5.7± 0.0.2) on MCF-7 cell line followed by (4.5± 0.4) % inhibition on A549 cell line and this is considered the first cytotoxic report of A. aestivus flowers.

Keywords: Anthraquinones, Asphodelus aestivus, Cytotoxic activity, Flavonoids, LC-ESI-MS/MS

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Authors: Zaheer Ahmad, Afzal Shah

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pH responsive block copolymers consist of mPEG and glutamic acid units were syntheiszed in different formulations. The synthesized polymers were structurally investigated. Doxorubicin Hydrocholide (DOX-HCl) as a chemotherapy medication for the treatment of cancer was selected. DOX-HCl was loaded and their drug loading content and drug loading efficiency were determined. The nanocarriers were obtained in small size, well shaped and slightly negative surface charge. The release study was carried out both at pH 7.4 and 5.5 and it was revealed that the release was sustained and in controlled manner and there was no initial burst release. The in vitro release study was further carried out for different formulations with different glutamic acid moieties. Time dependent cell proliferation inhibition of the free drug and drug loaded nanoparticles against human breast cancer cell lines MCF-7 and Zr-75-30 was observed. Cellular uptakes and endocytosis were investigated by confocal laser scanning microscopy (CLSM) and flow cytometery. The biocompatibility, optimum size, shape and surface charge of the developed nanoparticles make the nanoparticles an efficient drug delivery carrier.

Keywords: doxorubicin, glutamic acid, cell proliferation inhibition, breast cancer cell

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Authors: Wilfred A. Abiaa, Chibundu N. Ezekiel, Benedikt Warth, Michael Sulyok, Paul C. Turner, Rudolf Krska, Paul F. Moundipa

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Mycotoxins are a wide range of toxic secondary metabolites of fungi that contaminate various food commodities worldwide especially in sub-Saharan Africa (SSA). Such contamination seriously compromises food safety and quality posing a serious problem for human health as well as to trade and the economy. Their concentrations depend on various factors, such as the commodity itself, climatic conditions, storage conditions, seasonal variances, and processing methods. When humans consume foods contaminated by mycotoxins, they exert toxic effects to their health through various modes of actions. Rural populations in sub-Saharan Africa, are exposed to dietary mycotoxins, but it is supposed that exposure levels and health risks associated with mycotoxins between SSA countries may vary. Dietary exposures and health risk assessment studies have been limited by lack of equipment for the proper assessment of the associated health implications on consumer populations when they eat contaminated agricultural products. As such, mycotoxin research is premature in several SSA nations with product evaluation for mycotoxin loads below/above legislative limits being inadequate. Few nations have health risk assessment reports mainly based on direct quantification of the toxins in foods ('external exposure') and linking food levels with data from food frequency questionnaires. Nonetheless, the assessment of the exposure and health risk to mycotoxins requires more than the traditional approaches. Only a fraction of the mycotoxins in contaminated foods reaches the blood stream and exert toxicity ('internal exposure'). Also, internal exposure is usually smaller than external exposure thus dependence on external exposure alone may induce confounders in risk assessment. Some studies from SSA earlier focused on biomarker analysis mainly on aflatoxins while a few recent studies have concentrated on the multi-biomarker analysis of exposures in urine providing probable associations between observed disease occurrences and dietary mycotoxins levels. As a result, new techniques that could assess the levels of exposures directly in body tissue or fluid, and possibly link them to the disease state of individuals became urgent.

Keywords: mycotoxins, biomarkers, exposure assessment, health risk assessment, sub-Saharan Africa

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Authors: Madhu Gupta, Vikas Sharma, Suresh P. Vyas

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CD13 receptors are abundantly overexpressed in tumor cells as well as in neovasculature. The CD13 receptors were selected as a targeted site and polymeric nanoparticles (NPs) as a targeted delivery system. By combining these, a cyclic NGR (cNGR) peptide ligand was coupled on the terminal end of polyethylene glycol-b-poly(lactic-co-glycolic acid) (PEG-b-PLGA) and prepared the dual targeted-NPs (cNGR-PEG-PTX-NPs) to enhance the intracellular delivery of anticancer drug to tumor cells and tumor endothelial cells via ligand-receptor interaction. In-vitro cytotoxicity studies confirmed that the presence of cNGR enhanced the cytotoxic efficiency by 2.8 folds in Human Umbilical Vein Endothelial (HUVEC) cells, while cytotoxicity was improved by 2.6 folds in human fibrosarcoma (HT-1080) cells as compared to non-specific stealth NPs. Compared with other tested NPs, cNGR-PEG-PTX-NPs revealed more cytotoxicity by inducing more apoptosis and higher intracellular uptake. The tumor volume inhibition rate was 59.7% in case of cNGR-PEG-PTX-NPs that was comparatively more with other formulations, indicating that cNGR-PEG-PTX-NPs could more effectively inhibit tumor growth. As a consequence, the cNGR-PEG-PTX-NPs play a key role in enhancing tumor therapeutic efficiency for treatment of CD13 receptor specific solid tumor.

Keywords: cyclic NGR, CD13 receptor, targeted polymeric NPs, solid tumor, intracellular delivery

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Authors: N. Thawornwisit, P. Pradoo, S. Nuypree, L. Jarukasetrporn, S. Jitpukdeebodintra

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Objective: The aim of this study was to evaluate the duration of the Enterococcus faecalis (E. faecalis) penetration into the gap between root canal wall and filling material at a 3 to 6 mm distance from the cementoenamel junction (CEJ) in the dislodged temporary filling, in vitro. Material and methods: Thirty-four single root canal mandibular premolars were divided into two experimental groups (N = 15) and one negative control (N = 4). Root canals were prepared and obturated with gutta-percha using lateral condensation technique, X-ray checked, and sterilized. Leakages were set up using the modified bacterial leakage model, and E. faecalis was used as a microbial marker. Leakages were evaluated at 3 and 7 days by culturing gutta-percha and dentine drilled from a 3-6 mm distance from CEJ. Broth turbidity was recorded and compared. Result: All four negative control and the 3-day experimental group showed no broth turbidity. For the 7-day experimental group, there was 33.3% leakage. Conclusion: Penetration of E. faecalis into the gap between root canal wall and filling material at a 3 to 6 mm distance from CEJ in the dislodged temporary filling were not found at three days. However, at seven days of exposure, bacteria could penetrate into the interface of the root canal and filling materials.

Keywords: coronal leakage, bacterial leakage model, enterococcus faecalis

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Authors: Suparna Roy, P. Anantharaman

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The aim of this work is to estimate some in-vitro antioxidant activities and total phenols of various extracts such as aqueous, acetone, ethanol, methanol extract of seaweeds and pigments content by Spectrophotometric method. The seaweeds were collected during 2016 from Rameshwaram, southeast coast of India. Among four different extracts, aqueous extracts from all seaweeds had minimum activity than acetone, methanol and ethanol. The Rhodophyta and Phaeophyta had high antioxidant activity in comparing to Chlorophyta. The highest total antioxidant activity was found in acetone extract fromTurbinaria decurrens (98.97±0.00%), followed by its methanol extract (98.81±0.60%) and ethanol extract (98.58±0.53%). The highest reducing power and H2O2 scavenging activity were found in acetone extract of Caulerpa racemosa (383.25±1.04%), and methanol extract from Caulerpa racemosa var. macrophysa (24.91±0.49%). The methanol extract from Caulerpa scalpelliformis contained the highest total phenol (85.23±0.12%). The Chloro-a and Chloro-b contents were the highest in Gracilaria foliifera (13.69±0.38% mg/gm dry wt.) and Caulerpa racemosa var. macrophysa (9.12 ±0.12% mg/gm dry wt.) likewise carotenoid was also the highest in Gracilaria foliifera (0.054±0.0003% mg/gm dry wt.) and Caulerpa racemosa var. macrophysa (0.04 ±0.002% mg/gm dry wt.). It can be concluded from this study that some seaweed extract can be used for natural antioxidant production, after further characterization to negotiate the side effect of synthetic, market available antioxidants.

Keywords: seaweeds, antioxidant, total phenol, pigment, Olaikuda, Vadakkadu, Rameshwaram

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Authors: M. Golzade Gangraj, A. Abdi, N. ganji

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Aim: The aim of this study was to evaluate the Effect of aerobic training with Coriandrum sativum extract on selection of oxidative stress markers in diabetic rats. Methods: The population of male Wistar rats is the Pasteur Institute. Forty rats were randomly selected as subjects. After moving the mouse in vitro and stay for a week in a cage for sustainability, were diabetic. Diabetes induced by injection STZ (55 mg per kg of body weight of mice) was performed. According blood glucose was randomly divided into four experimental groups (control, training, extract and training-extract). Extract group consumed 150 mg per kg of body weight per day coriander juice. Training group performed aerobic training (50-55% VO2max). Result: The results showed that aerobic exercise training and coriander seed extract caused a significant increase in total antioxidant; superoxide dismutase and catalase were significantly decreased malondialdehyde. Conclusion: the research findings can be stated that the exercise with coriander seed extract has the ability to inhibit free radicals and can have beneficial effects on the body's antioxidant defense system and reduce oxidative stress in diabetic rats with STZ. Because it improves the body's antioxidant defense by increasing serum levels of antioxidant enzymes.

Keywords: aerobic training, coriandrum sativum, antioxidant, diabetes

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Authors: Yu-Wen Lin, Li-Ni Liu

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Introduction: Fatigue is the most common symptoms experienced by cancer patients undergoing chemotherapy. Patients receiving anticancer therapies develop a higher proportion of fatigue compared with patients who do not receive anticancer therapies. Fatigue has significant impacts on quality of life, daily activities, mood status, and social behaviors. A warm-water footbath (WWF) at 41℃ promotes circulation and removes metabolites resulting in improving sleep and relieving fatigue. The aim of this study is to determine the effectiveness of WWF for relieving fatigue with cancer patients undergoing chemotherapy. Materials and Methods: This is a single-center, prospective, quasi-experimental design study in the oncology ward in Taiwan. Participants in this study were assigned to WWF group as experimental group and standard care group as a control group by purposive sampling. In the WWF group, the participants were asked to soak their feet in 42-43℃ water 15 minutes for consecutive 6 days at one day before chemotherapy. Each participant was evaluated for fatigue level by the Taiwanese version of the Brief Fatigue Inventory (BFI-T). BFI-T was completed for consecutive 8 days of the study. The primary outcome was compared the BFI-T score of WWF group to the standard care group. Results: There were 60 participants enrolled in this study. Thirty participants were assigned to WWF group and 30 participants were assigned to standard care group. Both groups have comparable characteristic. The BFI-T scores of both groups were increased associated with the days of chemotherapy. The highest BFI-T scores of both groups were on the day 4 of chemotherapy. The BFI-T scores of both groups were decreased since day 5 and significantly decreased in WWF group on day 5 compared to standard care group (4.17 vs. 5.7, P ＜ .05). At the end of the study the fatigue at its worse were significantly decreased in WWF group (2.33 vs. 4.37, P ＜ .001). There was no adverse event reported in this study. Conclusion: WWF is an easy, safe, non-invasive, and relatively inexpensive nursing intervention for improving fatigue of cancer patients undergoing chemotherapy. In summary, this study shows the WWF is a simple complementary care method, and it is effective for improving and relieving fatigue in a short time. Through improving fatigue is a way to enhance the quality of life which is important for cancer patients undergoing chemotherapy. Larger prospective randomized controlled trial and long-term effectiveness and outcomes of WWF should be performed to confirm this study.

Keywords: chemotherapy, warm-water footbath, fatigue, Taiwanese version of the brief fatigue inventory

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Authors: Tunca Gul Altuntas, Aziz Baydar, Cemre Acar, Sezen Yılmaz, Tulay Coban

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Free radicals, which are generated in many bioorganic redox processes, play a role in the pathogenesis of several diseases including cancer, arthritis, hemorrhagic shock, inflammatory, cardiovascular, neurodegenerative diseases and age-related degenerative brain diseases. Exposures of normal cell to free radical damages several structures, oxidizes nucleic acids, proteins, lipids, or DNA. Compounds interfere with the action of reactive oxygen species might be useful in prevention and treatment of these pathologies. A series of indole compounds containing piperazine ring were synthesized. Coupling of indole-2-carboxylic acid with monosubstituted piperazines was accomplished with 1,1’-carbonyldiimidazole (CDI) in a good yield. The structures of prepared compounds were verified in good agreement with their 1H NMR (nuclear magnetic resonance), MS (mass spectrophotometry), and IR (infrared spectrophotometry) characteristics. In this work, all synthetized indole derivatives were screened in vitro for their antioxidative potential against vitamin E (α-tocopherol) using different antioxidant assays such as superoxide anion formation, lipid peroxidation levels in rat liver, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) stable radical scavenging activity. The synthesized compounds showed various levels of inhibition compared to vitamin E. This may give promising results for the development of new antioxidant agents.

Keywords: antioxidant, indoles, piperazines, reactive oxygen species

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Authors: Geetika Vajpayee, Sugandha Asthana, Pratibha Kumari, Shanthy Sundaram

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Pseudomonas species possess a variety of promising properties of antifungal and growth promoting activities in the wheat plant. In the present study, Pseudomonas fluorescens MTCC-9768 is tested against plant pathogenic fungus Tilletia indica, causing Karnal bunt, a quarantine disease of wheat (Triticum aestivum) affecting kernels of wheat. It is one of the 1/A1 harmful diseases of wheat worldwide under EU legislation. This disease develops in the growth phase by the spreading of microscopically small spores of the fungus (teliospores) being dispersed by the wind. The present chemical fungicidal treatments were reported to reduce teliospores germination, but its effect is questionable since T. indica can survive up to four years in the soil. The fungal growth inhibition tests were performed using Dual Culture Technique, and the results showed inhibition by 82.5%. The interaction of antagonist bacteria-fungus causes changes in the morphology of hyphae, which was observed using Lactophenol cotton blue staining and Scanning Electron Microscopy (SEM). The rounded and swollen ends, called ‘theca’ were observed in interacted fungus as compared to control fungus (without bacterial interaction). This bacterium was tested for its antagonistic activity like protease, cellulose, HCN production, Chitinase, etc. The growth promoting activities showed increase production of IAA in bacteria. The bacterial secondary metabolites were extracted in different solvents for testing its growth inhibiting properties. The characterization and purification of the antifungal compound were done by Thin Layer Chromatography, and Rf value was calculated (Rf value = 0.54) and compared to the standard antifungal compound, 2, 4 DAPG (Rf value = 0.54). Further, the in vivo experiments showed a significant decrease in the severity of disease in the wheat plant due to direct injection method and seed treatment. Our results indicate that the extracted and purified compound from the antagonist bacteria, P. fluorescens MTCC-9768 may be used as a potential biocontrol agent against T. indica. This also concludes that the PGPR properties of the bacteria may be utilized by incorporating it into bio-fertilizers.

Keywords: antagonism, Karnal bunt, PGPR, Pseudomonas fluorescens

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Authors: R. H. Begaydarova, B. Zh. Kultanov, B. T. Esilbaeva, G. E. Nasakaeva, Y. Yukhnevich, G. K. Alshynbekova, A. E. Dyusembaeva

Abstract:

Background: The level of middle molecules of peptides (MMP) allows to evaluate the severity and prognosis of the disease and is a criterion for the effectiveness of the treatment. The detection the products of lipidperoxidation cascade, such as conjugated dienes, malondialdehyde in biological material, has an important role in the development of pathogenesis, the diagnosis and prognosis in different parasitic diseases. Purpose of the study was to evaluate the state of endogenous intoxication and indicators of lipid peroxidation in patients with giardiasis before and after treatment. Materials and methods: Endogenous intoxication was evaluated in patients with giardiasis in the level of middle molecules of peptides (MMP) in the blood. The amount of MMP and products of lipid peroxidation were determined in the blood of 198 patients with giardiasis, 129 of them were women (65%), 69 were men (35%). The MMP level was detected for comparison in the blood of 84 healthy volunteers. The lipid peroxidation were determined in 40 healthy men and women without giardiasis and history of chronic diseases. Data were processed by conventional methods of variation statistics, we calculated the arithmetic mean (M) and standard dispersion (m). t-test (t) was used to assess differences. Results: The level of MMP in the blood was significantly higher in patients with giardiasis in comparison with group of healthy men and women. MMP concentration in the blood of women with Giardia was 2.5 times greater than that of the comparison groups of women. The level of MMP exceeds more than 6 times in men with giardiasis. The decrease in the intensity of endogenous intoxication was two weeks after antigiardia therapy, both men and women. According to the study, a statistically significant increase in the level of all the studied parameters lipid peroxidation cascade was observed in the blood of men with giardiasis, with the exception of the total primary production (NGN). The treatment of giardiasis helped to stabilize the level of almost all metabolites of lipid peroxidation cascade. The exception was level of malondialdehyde, it was significantly elevated to compare with the control group and after treatment. Conclusion: Thus, the MMP level was significantly higher in blood of patients with giardiasis than in comparison group. This is evidence of severe endogenous intoxication caused by giardia infection. The accumulation of primary and secondary products of lipid peroxidation was observed in the blood of men and women. These processes tend to be more active in men than in women. Antigiardiasis therapy contributed to the normalization of almost all the studied indicators of lipid peroxidation in the blood of participants, except the level malondialdehyde in the blood of men.

Keywords: enzymes of antioxidant protection, giardiasis, blood, treatment

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Authors: Mateus L. O. Freitas, Flávia H. de M. Libório, Letycia L. Ricardo, Patrícia da C. Zonetti, Graciene de S. Bido

Abstract:

Weeds compete with agricultural crops for resources such as light, water, and nutrients. This competition can cause significant damage to agricultural producers, and, currently, the use of agrochemicals is the most effective method for controlling these undesirable plants. Morning glory (Ipomoea grandifolia [Dammer] O'Donell) is an aggressive weed and significantly reduces agricultural productivity making harvesting difficult, especially mechanical harvesting. The biggest challenge in modern agriculture is to preserve high productivity reducing environmental damage and maintaining soil characteristics. No-till is a sustainable practice that can reduce the use of agrochemicals and environmental impacts due to the presence of plant residues in the soil, which release allelopathic compounds and reduce the incidence or alter the growth and development of crops and weeds. Sorghum (Sorghum bicolor [L.] Moench) is a forage with proven allelopathic activity, mainly for producing sorgholeone. In this context, this research aimed to evaluate the allelopathic action of sorghum fractions using hexane, dichloromethane, butanol, and ethyl acetate on the germination and initial growth of morning glory. The parameters analyzed were the percentage of germination, speed of germination, seedling length, and biomass weight (fresh and dry). The bioassays were performed in Petri dishes, kept in an incubation chamber for 7 days, at 25 °C, with a 12h photoperiod. The experimental design was completely randomized, with five replicates of each treatment. The data were evaluated by analysis of variance, and the averages between each treatment were compared using the Scott Knott test at a 5% significance level. The results indicated that the dichloromethane and ethyl acetate fractions showed bioherbicidal effects, promoting effective reductions on germination and initial growth of the morning glory. It was concluded that allelochemicals were probably extracted in these fractions. These secondary metabolites can reduce the use of agrochemicals and environmental impact, making agricultural production systems more sustainable.

Keywords: allelochemicals, secondary metabolism, sorgoleone, weeds

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Authors: Juthamath Komvongsa, Bancha Mahong, Kannika Phasai, Sukanya Luang, Jong-Seong Jeon, James Ketudat-Cairns

Abstract:

Os9BGlu31 is a rice transglucosidase that transfers glucosyl moieties to various acceptors such as carboxylic acids and alcohols, including phenolic acids and flavonoids, in vitro. The role of Os9BGlu31 transglucosidase in rice plant metabolism has not been reported to date. Methanolic extracts of rice bran and flag leaves were found to contain substrates to which Os9BGlu31 could transfer glucose from 4-nitrophenyl β -D-glucopyranoside donor. The semi-purified substrate from rice bran was found to contain oleic acid and linoleic acid and the pure fatty acids were found to act as acceptor substrates for Os9BGlu31 transglucosidase to form 1-O-acyl glucose esters. Os9BGlu31 showed higher activity with oleic acid (18:1) and linoleic acid (18:2) than stearic acid (18:0), and had both higher kcat and higher Km for linoleic than oleic acid in the presence of 8 mM 4NPGlc donor. This transglucosidase reaction is reversible, Os9bglu31 knockout rice lines of flag leaves were found to have higher amounts of fatty acid glucose esters than wild type control lines, these data conclude that fatty acid glucose esters act as glucosyl donor substrates for Os9BGlu31 transglucosidase in rice.

Keywords: fatty acid, fatty acid glucose ester, transglucosidase, rice flag leaf, homologous knockout lines, tandam mass spectrometry

Procedia PDF Downloads 357

Authors: Wen-Yu Lin, Yi-Ching Chung, Jhao-Ren Lin, Tzyy-Rong Jinn

Abstract:

It is well known that enterovirus 71(EV71) causes recurring outbreaks of hand, foot and mouth disease and encephalitis leading to complications or death in young children. And, several enterovirus 71 (EV71) of hand foot and mouth disease (HFMD) with high mortalities occurred in Asia country, such as Hong Kung (1985), Malaysia (1997), Taiwan (1998) and China (2008) that EV71 results in severe neurological complications and sudden death in infants and young children. However, there are still no effective drugs and vaccines to reduce and inhibit EV71 infection. Therefore, the development of specific and effective antiviral strategies against EV71 has become an urgent issue for the protection of children from the hazards of the HFMD. As reported, amantadine is effective in prophylaxis and treatment of the EV71 infections. Thus, the aim of this study was to further evaluate the synergistic antiviral activity of amantadine coupled with magnesium lithospermate B (MLB) against enterovirus 71 infection. In a preliminary test, it is shown that the infected RD cells were treated with amantadine after virus absorption, at concentrations of 3 and 5µM of amantadine suppressed EV71-induced CPE to 13% and 23%, respectively at MOI of 3. Alternatively, at concentrations of 5µg/ml of MLB combined with 3 and 5 µM of amantadine apparently suppressed EV71-induced CPE to 45% and 63%, respectively at MOI of 3. Thus, amantadine coupled with MLB may have the potential for further study to development as the chemopreventive reagents against EV71 infection.

Keywords: amantadine, Enterovirus 71, magnesium lithospermate B, RD cells, synergistic effects

Procedia PDF Downloads 238

Authors: Khurram Munir, Cuie Wen, Yuncang Li

Abstract:

Magnesium (Mg) metal matrix composites (MMCs) reinforced with graphene nanoplatelets (GNPs) have been developed by powder metallurgy (PM). In this study, GNPs with different concentrations (0.1-0.3 wt.%) were dispersed into Mg powders by high-energy ball-milling processes. The microstructure and resultant mechanical properties of the fabricated nanocomposites were characterized using transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD), Raman spectroscopy (RS), compression and nano-wear tests. The corrosion resistance of the fabricated composites was evaluated by electrochemical tests and hydrogen evolution measurements. Finally, the biological response of Mg-GNPs composites was assessed using osteoblast-like SaOS2 cells. The results indicate that GNPs are excellent candidates as reinforcements in Mg matrices for the manufacture of biodegradable Mg-based composite implants. GNP addition improved the mechanical properties of Mg via synergetic strengthening modes. Moreover, retaining the structural integrity of GNPs during PM processing improved the ductility, compressive strength, and corrosion resistance of the Mg-GNP composites as compared to monolithic Mg. Cytotoxicity assessments did not reveal any significant toxicity with the addition of GNPs to Mg matrices. This study demonstrates that Mg-xGNPs with x < 0.3 wt.%, may constitute novel biodegradable implant materials for load-bearing applications.

Keywords: magnesium-graphene composites, strengthening mechanisms, In vitro cytotoxicity, biocorrosion

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Authors: Ilaria Manca, Ilaria Manca, Francesca Pettinau, Ignazia Mocci, Elisabetta M. Usai, Barbara Pittau

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Lamotrigine is a phenyltriazine used in the treatment of epilepsy and bipolar disorder type I. The purpose of this study was to test and compare various solid forms of immediate release (IR) lamotrigine products, at different strenghts, in order to study their disaggregation and dissolution behavior. IR products are designed to release their active substance promptly after administration. Concentration of hydrochloric acid in gastric juice is about 0.1-0.001 M, so FDA (Food and Drug Administration) recommends, for lamotrigine regular tablets, dissolution tests in HCl 0.1 M.Toinvestigate the pH dependency of drug release in the entire gastrointestinal tract, we worked at two additional media with different pH values (4.5 and 6.8), that reflect conditions in it. To afford acceptable dissolution rates, tablets must disintegrate. Disaggregation of constituent particles increases the surface area and substantially increases the dissolution rate. For this reason availability of an active substance from tablets depends on its ability to disintegrate fast in dissolution media. pH of gastrointestinal fluid affects drug absorption by conditioning its solubility and dissolution, but also tablet disintegration may be influenced by it. To obtain information about the quantitative relationship between different mixture components, Nuclear Magnetic Resonance (NMR) spectroscopy was used. We also investigate tablet hardness. The investigation carried out confirms pH 1.2 as the ideal environment for the immediate availability of the active substance.

Keywords: dissolution, disaggregation, Lamotrigine, bioequivalence

Procedia PDF Downloads 449

Authors: Otilia Ruxandra Vasile, Ecaterina Andronescu, Cristina Daniela Ghitulica, Bogdan Stefan Vasile, Roxana Trusca, Eugeniu Vasile, Alina Maria Holban, Carmen Mariana Chifiriuc, Florin Iordache, Horia Maniu

Abstract:

Engineered powders offer great promise in several applications, but little information is known about cytotoxicity effects. The aim of the current study was the synthesis and cytotoxicity examination of silver powders using pyrosol method at temperatures of 600°C, 650°C and 700°C, respectively sol-gel method and calcinations at 500°C, 600°C, 700°C and 800°C. We have chosen to synthesize and examine silver particles cytotoxicity due to its use in biological applications. The synthesized Ag powders were characterized from the structural, compositional and morphological point of view by using XRD, SEM, and TEM with SAED. In order to determine the influence of the synthesis route on Ag particles cytotoxicity, different sizes of micro and nanosilver synthesized powders were evaluated for their potential toxicity. For the study of their cytotoxicity, cell cycle and apoptosis have been done analysis through flow cytometry on human colon carcinoma cells and mesenchymal stem cells and through the MTT assay, while the viability and the morphological changes of the cells have been evaluated by using cloning studies. The results showed that the synthesized silver nanoparticles have displayed significant cytotoxicity effects on cell cultures. Our synthesized silver powders were found to present toxicity in a synthesis route and time-dependent manners for pyrosol synthesized nanoparticles; whereas a lower cytotoxicity has been measured after cells were treated with silver nanoparticles synthesized through sol-gel method.

Keywords: Ag, cytotoxicity, pyrosol method, sol-gel method

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Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya

Abstract:

Triazoles are basic five-membered ring heterocycles with an unsaturated, six-delocalized electron ring system. Since the dawn of click chemistry, triazoles have represented a functional heterocyclic core that has been the foundation of medicinal chemistry. The compounds with 1,2,3-triazole rings can be used in several fields, including medicine, organic synthesis, polymer chemistry, fluorescent imaging, horticulture, and industries, to name a few. Besides that, they found it to have health applications in the prevention and reduction of the risk of diseases, such as anti-cancer, antimicrobial, antiviral, and anti-inflammatory properties. Here, we present the synthesis of twelve 1,2,3-triazolyl chalcone derivatives (4a–l), which were produced in high yields by coupling substituted aldehydes and triazolyl acetophenone (3a–d) in ethanol. The title products were characterized by physicochemical, infrared, nuclear magnetic resonance, and mass spectral methods. The in vitro tests were used to evaluate the antioxidant and antimicrobial activity of each of the prepared molecules. The preliminary assessment and 2,2-diphenyl-1-picrylhydrazyl activity of the title compounds showed significantly higher antibacterial activity and moderate-to-good antifungal and antioxidant activities compared to their standards. This work presents the synthesis of triazolyl chalcone derivatives and their biological activity. Based on the findings, these compounds could be used as lead compounds in antimicrobial and antioxidant research in the future.

Keywords: antibacterial activity, antifungal activity, antioxidant activity, chalcone, 1, 2, 3-triazole

Procedia PDF Downloads 112

Authors: Hari Bezwada, Michelle Cheon, Ryan Divan, Hannah Escritor, Michelle Kagramian, Isha Korgaonkar, Maya MacAdams, Udgita Pamidigantam, Richard Pilny, Eleanor Race, Angadh Singh, Nathan Zhang, LeeAnn Nguyen, Fina Liotta

Abstract:

Malaria is a deadly disease caused by the Plasmodium parasite, which continues to develop resistance to current antimalarial drugs. In this research project, the effectiveness of numerous thiazole derivatives was explored in inhibiting the PfPKG, a crucial part of the Plasmodium life cycle. This study involved the synthesis of six thiazole-derived amides to inhibit the PfPKG pathway. Nuclear Magnetic Resonance (NMR) spectroscopy and Infrared (IR) spectroscopy were used to characterize these compounds. Furthermore, AutoDocking software was used to predict binding affinities of these thiazole-derived amides in silico. In silico, compound 6 exhibited the highest predicted binding affinity to PfPKG, while compound 5 had the lowest affinity. Compounds 1-4 displayed varying degrees of predicted binding affinity. In-vitro, it was found that compound 4 had the best percent inhibition, while compound 5 had the worst percent inhibition. Overall, all six compounds had weak inhibition (approximately 30-39% at 10 μM), but these results provide a foundation for future drug discovery experiments.

Keywords: Medicinal Chemistry, Malaria, drug discovery, PfPKG, Thiazole, Plasmodium

Procedia PDF Downloads 88

Authors: Amin Jabbari

Abstract:

The state of the art in major 3D printing technologies, such as powder-based and slurry based, has led researchers to investigate the ability to fabricate bone scaffolds for bone tissue engineering using biomaterials. In addition, 3D printing technology can simulate mechanical and biological surface properties and print with high precision complex internal and external structures that match their functional properties. Polymer matrix composites reinforced with particulate bioceramics, hydrogels reinforced with particulate bioceramics, polymers coated with bioceramics, and non-porous bioceramics are among the materials that can be investigated for bone scaffold printing. Furthermore, it was shown that the introduction of high-density micropores into the sparingly dissolvable CSiMg10 and dissolvable CSiMg4 shell layer inevitably leads to a nearly 30% reduction in compressive strength, but such micropores can easily influence the ion release behavior of the scaffolds. Also, biocompatibility tests such as cytotoxicity, hemocompatibility and genotoxicity were tested on printed parts. The printed part was tested in vitro, and after 24-26 h for cytotoxicity, and 4h for hemocompatibility test, the CSiMg4@CSiMg10-p scaffolds were found to have significantly higher osteogenic capability than the other scaffolds of implantation. Overall, these experimental studies demonstrate that 3D printed, additively-manufactured bioceramic calcium (Ca)-silicate scaffolds with appropriate pore dimensions are promising to guide new bone ingrowth.

Keywords: AM, 3D printed implants, bioceramic, tissue engineering

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Authors: H. Abu-Ali, A. Nabok, T. Smith

Abstract:

Aptamers are single-strand of DNA or RNA nucleotides sequence which is designed in vitro using selection process known as SELEX (systematic evolution of ligands by exponential enrichment) were developed for the selective detection of many toxic materials. In this work, we have developed an electrochemical biosensor for highly selective and sensitive detection of Hg2+ and Pb2+ using a specific aptamer probe (SAP) labelled with ferrocene (or methylene blue) in (5′) end and the thiol group at its (3′) termini, respectively. The SAP has a specific coil structure that matching with G-G for Pb2+ and T-T for Hg2+ interaction binding nucleotides ions, respectively. Aptamers were immobilized onto surface of screen-printed gold electrodes via SH groups; then the cyclic voltammograms were recorded in binding buffer with the addition of the above metal salts in different concentrations. The resulted values of anode current increase upon binding heavy metal ions to aptamers and analyte due to the presence of electrochemically active probe, i.e. ferrocene or methylene blue group. The correlation between the anodic current values and the concentrations of Hg2+ and Pb2+ ions has been established in this work. To the best of our knowledge, this is the first example of using a specific DNA aptamers for electrochemical detection of heavy metals. Each increase in concentration of 0.1 μM results in an increase in the anode current value by simple DC electrochemical test i.e (Cyclic Voltammetry), thus providing an easy way of determining Hg2+ and Pb2+concentration.

Keywords: aptamer, based, biosensor, DNA, electrochemical, highly, specific

Procedia PDF Downloads 153