Search results for: eugenol acetate

Authors: Gómez Romero Jacob, García Peña Elvia Inés

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The co-digestion process of crude cheese whey (CCW) with fruit vegetable waste (FVW) for biohydrogen production was investigated in batch and continuous systems, in stirred 1.8 L bioreactors at 37°C. Five different C/N ratios (7, 17, 21, 31, and 46) were tested in batch systems. While, in continuous system eight conditions were evaluated, hydraulic retention time (from 60 to 10 h) and organic load rate (from 21.96 to 155.87 g COD/L d). Data in batch tests showed a maximum specific biohydrogen production rate of 10.68 mmol H2/Lh and a biohydrogen yield of 449.84 mL H2/g COD at a C/N ratio of 21. In continuous co-digestion system, the optimum hydraulic retention time and organic loading rate were 17.5 h and 80.02 g COD/L d, respectively. Under these conditions, the highest volumetric production hydrogen rate (VPHR) and hydrogen yield were 11.02 mmol H2/L h, 800 mL H2/COD, respectively. A pyrosequencing analysis showed that the main acclimated microbial communities for co-digestion studies consisted of Bifidobacterium, with 85.4% of predominance. Hydrogen producing bacteria such as Klebsiella (9.1%), Lactobacillus (0.97%), Citrobacter (0.21%), Enterobacter (0.27%), and Clostridium (0.18%) were less abundant at this culture period. The microbial population structure was correlated with the lactate, acetate, and butyrate profiles obtained. Results demonstrated that the co-digestion of CCW with FVW improves biohydrogen production due to a better nutrient balance and improvement of the system’s buffering capacity.

Keywords: acclimatation, biohydrogen, co-digestion, microbial community

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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: S. Techaoei, K. Jarmkom, P. Eakwaropas, W. Khobjai

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The objective of this research was focused on investigating in vitro antimicrobial activity of Phellinus linteus fruiting body extracts on Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus. Phellinus linteus fruiting body was extracted with ethanol and ethyl acetate and was vaporized. The disc diffusion assay was used to assess antimicrobial activity against tested bacterial strains. Primary screening of chemical profile of crude extract was determined by using thin layer chromatography. The positive control and the negative control were used as erythromycin and dimethyl sulfoxide, respectively. Initial screening of Phellinus linteus crude extract with the disc diffusion assay demonstrated that only ethanol had greater antimicrobial activity against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus. The MIC assay showed that the lower MIC was observed with 0.5 mg/ml of Pseudomonas aeruginosa and Methicillin-resistant Staphylococcus aureus and 0.25 mg/ml. of Escherichia coli and Staphylococcus aureus, respectively. TLC chemical profile of extract was represented at R_f ≈ 0.71-0.76.

Keywords: Staphylococcus aureus, Escherichia coli, Phellinus linteus, Methicillin-resistant Staphylococcus aureus, antimicrobial activity

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Authors: Atul Kumar, Veeranjaneyulu Gannedi, Qazi Naveed Ahmed

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Oligosaccharides, which are essential to all cellular organisms, play vital roles in cell recognition, signaling, and are involved in a broad range of biological processes. The chemical synthesis of carbohydrates represents a powerful tool to provide homogeneous glycans. In carbohydrate synthesis, the major concern is the orthogonal protection of hydroxyl groups that can be unmasked independently. Classical protecting groups include benzyl ethers (Bn), which are normally cleaved through hydrogenolysis or by means of metal reduction, and acetate (Ac), benzoate (Bz) or pivaloate esters, which are removed using base promoted hydrolysis. In present work a series of α-Oxoester (COBz) protected saccharides, with divergent base sensitivity profiles against benzoyl (Bz) and acetyl (Ac), were designed and KHSO₅/CH₃COCl in methanol was identified as an easy, mild, selective and efficient deprotecting reagent for their removal in the perspective of carbohydrate synthesis. Timely monitoring of later reagent was advantageous in establishing both sequential as well as simultaneous deprotecting of COBz, Bz, and Ac. The salient feature of our work is its ease to generate different acceptors using designed monosaccharides. In summary, we demonstrated α-Oxoester (COBz) as a new protecting group for carbohydrates and the application of this group for the synthesis of Glycosylphosphatidylinositol (GPI) anchor are in progress.

Keywords: α-Oxoester, oligosaccharides, new protecting group, acceptor synthesis, glycosylation

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Authors: Ahmad Aroziki Abdul Aziz, Sakinah Mohd Alauddin, Ruzitah Mohd Salleh, Mohammed Iqbal Shueb

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This paper illustrates the effect of nano Magnesium Hydroxide (MH) loading on the thermal properties of Low Density Polyethylene (LDPE)/ Poly (ethylene-co vinyl acetate)(EVA) nano composite. Thermal studies were conducted, as it understanding is vital for preliminary development of new polymeric systems. Thermal analysis of nano composite was conducted using thermo gravimetric analysis (TGA), and differential scanning calorimetry (DSC). Major finding of TGA indicated two main stages of degradation process found at (350 ± 25 oC) and (480 ± 25 oC) respectively. Nano metal filler expressed better fire resistance as it stand over high degree of temperature. Furthermore, DSC analysis provided a stable glass temperature around 51 (±1 oC) and captured double melting point at 84 (±2 oC) and 108 (±2 oC). This binary melting point reflects the modification of nano filler to the polymer matrix forming melting crystals of folded and extended chain. The percent crystallinity of the samples grew vividly with increasing filler content. Overall, increasing the filler loading improved the degradation temperature and weight loss evidently and a better process and phase stability was captured in DSC.

Keywords: thermal properties, nano MH, nano particles, cable and wire, LDPE/EVA

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Authors: Min-Shiuan Liou, Yi Shan Yang, Yang-Zhan Huang, Chia-Wen Hsieh

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A high speed growing and butanol-tolerant Clostridium acetobutylicum HOL1 mutant was screened throughout continuous adaption culture with C. acetobutylicum ATCC 824. The HOL1 strain can grow well in 10 g/L butanol contained CGM medium and can produce about 12.8 g /L butanol during 24 hrs. The C. acetobutylicum HOL1 strain was able to produce 166 mM butanol with 21 mM acetone at pH 4.8, resulting in a butanol selectivity (a molar ratio of butanol to total solvents) of 0.79, which is much higher than that (0.6) of the wild-type strain C. acetobutylicum ATCC 824. The acetate and butyrate accumulation were not observed during fermentation of the HOL1 strain. A hyper-butanol producing C. acetobutylicum HOL1 (pBPHS-3), which was created to overexpress the Bacillus psychrosaccharolyticus originated specific heat-shock protein gene, hspX, from a clostridial phosphotransbutyrylase promoter, was studied for its potential to produce a high titer of butanol. Overexpression of hspX resulted in increased final butanol yield 47% and 30% higher than those of the the ATCC824 and the HOL1 strains, respectively. The remarkable high-speed growth and butanol tolerance of strain HOL1 (pBPHS-3) demonstrates that overexpression of heterogeneous stress protein-encoding gene, hspX, could help C. acetobutylicum to effectively produce a high concentration of butanol.

Keywords: Clostridium acetobutylicum, butanol, heat-shock protein, resistance

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Authors: T. H. Derdzyan, K. A. Ghazaryan, G. A. Gevorgyan

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Beta-glucosidase, chitinase, leucine-aminopeptidase, acid phosphomonoestearse and acetate-esterase enzyme activities in the soils under the impact of metallurgical industrial activity in Lori marz (district) were investigated. The results of the study showed that the activities of the investigated enzymes in the soils decreased with increasing distance from the Shamlugh copper mine, the Chochkan tailings storage facility and the ore transportation road. Statistical analysis revealed that the activities of the enzymes were positively correlated (significant) to each other according to the observation sites which indicated that enzyme activities were affected by the same anthropogenic factor. The investigations showed that the soils were polluted with heavy metals (Cu, Pb, As, Co, Ni, Zn) due to copper mining activity in this territory. The results of Pearson correlation analysis revealed a significant negative correlation between heavy metal pollution degree (Nemerow integrated pollution index) and soil enzyme activity. All of this indicated that copper mining activity in this territory causing the heavy metal pollution of the soils resulted in the inhabitation of the activities of the enzymes which are considered as biological catalysts to decompose organic materials and facilitate the cycling of nutrients.

Keywords: Armenia, metallurgical industrial activity, heavy metal pollutionl, soil enzyme activity

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Authors: Bashar Al-Sabti, Jehad Harbali

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Background: Pyridine is a reactive base that might be used in preparing sitagliptin. International Agency for Research on Cancer classifies pyridine in group 2B; this classification means that pyridine is possibly carcinogenic to humans. Therefore, pyridine should be monitored at the allowed limit in sitagliptin pharmaceutical ingredients. Objective: The aim of this study was to develop a novel ultra high performance liquid chromatography mass spectrometry (UHPLC-MS) method to estimate the quantity of pyridine impurity in sitagliptin pharmaceutical ingredients. Methods: The separation was performed on C8 shim-pack (150 mm X 4.6 mm, 5 µm) in reversed phase mode using a mobile phase of water-methanol-acetonitrile containing 4 mM ammonium acetate in gradient mode. Pyridine was detected by mass spectrometer using selected ionization monitoring mode at m/z = 80. The flow rate of the method was 0.75 mL/min. Results: The method showed excellent sensitivity with a quantitation limit of 1.5 ppm of pyridine relative to sitagliptin. The linearity of the method was excellent at the range of 1.5-22.5 ppm with a correlation coefficient of 0.9996. Recoveries values were between 93.59-103.55%. Conclusions: The results showed good linearity, precision, accuracy, sensitivity, selectivity, and robustness. The studied method was applied to test three batches of sitagliptin raw materials. Highlights: This method is useful for monitoring pyridine in sitagliptin during its synthesis and testing sitagliptin raw materials before using them in the production of pharmaceutical products.

Keywords: genotoxic impurity, pyridine, sitagliptin, UHPLC -MS

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Authors: Ahmed Jibrin Uttu, Maimuna Waziri

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The root bark of Glossonema boveanum (Decne), a member of Apocynaceae family, is used by traditional medicine practitioner to treat urinary and respiratory tract infections, bacteremia, typhoid fever, bacillary dysentery, diarrhea and stomach pain. This present study aims to validate the medicinal claims ascribed to the root bark of the plant. Preliminary phytochemical study of the root bark extracts (n-hexane, ethyl acetate, chloroform and methanol extracts) showed the presence of alkaloids, carbohydrates, steroids, triterpenes, cardiac glycosides, saponins, tannins and flavonoids. Antimicrobial study of the extracts showed activities against Staphylococus aureus, Bacillus subtilis, Salmonella typhii, Shigella dysenteriae, Escherichia coli, Enterobacter cloacae, Streptococcus agalactiae and Candida albicans while Micrococcus luteus, Pseudomonas aeruginosa and Klebsiella Pneumoniae showed resistance to all the extracts. The inhibitory effect was compared with the standard drug ciprofloxacin and fluconazole. MIC and MBC for both extracts were also determined using the tube dilution method. This study concluded that the root bark of G. boveanum, used traditionally as a medicinal plant, has antimicrobial activities against some causative organisms.

Keywords: Glossonema boveanum (Decne.), phytochemical, antimicrobial, minimum inhibitory concentration, minimum bactericidal concentration

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Authors: Muhammad Mazhar, Yong Zhu, Likang Qin

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Foods contain endogenous components known as dietary fibers, which are classified into soluble and insoluble forms. Dietary fibers are resistant to gut digestive enzymes, modulating anaerobic intestinal microbiota (AIM) and fabricating short-chain fatty acids (SCFAs). Acetate, butyrate, and propionate dominate in the gut, and different pathways, including Wood-Ljungdahl and acrylate pathways, generate these SCFAs. In pancreatic dysfunction, the release of insulin/glucagon is impaired, which leads to hyperglycemia. SCFAs enhance insulin sensitivity or secretion, beta-cell functions, leptin release, mitochondrial functions, and intestinal gluconeogenesis in human organs, which positively affect type 2 diabetes (T2D). Research models presented that SCFAs either enhance the release of peptide YY (PYY) and glucagon-like peptide-1 (GLP-1) from L-cells (entero-endocrine) or promote the release of leptin hormone satiation in adipose tissues through G-protein receptors, i.e., GPR-41/GPR-43. Dietary fibers are the components of foods that influence AIM and produce SCFAs, which may be offering beneficial effects on T2D. This review addresses the effectiveness of SCFAs in modulating gut AIM in the fermentation of dietary fiber and their worth against T2D.

Keywords: dietary fibers, intestinal microbiota, short-chain fatty acids, fermentation, type 2 diabetes

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Authors: Jiyaul Haque, Vandana Srivastava, M. A. Quraishi

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The amino acids based corrosion inhibitors 2-(3-(carboxymethyl)-1H-imidazol-3-ium-1-yl) acetate (Z-1),2-(3-(1-carboxyethyl)-1H-imidazol-3-ium-1-yl) propanoate (Z-2) and 2-(3-(1-carboxy-2-phenylethyl)-1H-imidazol-3-ium-1-yl)-3- phenylpropanoate (Z-3) were synthesized by the reaction of amino acids, glyoxal and formaldehyde, and characterized by the FTIR and NMR spectroscopy. The corrosion inhibition performance of synthesized inhibitors was studied by electrochemical (EIS and PDP), surface and DFT methods. The results show, the studied Z-1, Z-2 and Z-3 are effective inhibitors, showed the maximum inhibition efficiency of 88.52 %, 89.48 and 96.08% at concentration 200ppm, respectively. The results of potentiodynamic polarization (PDP) study showed that Z-1 act as a cathodic inhibitor, while Z-2 and Z-3 act as mixed type inhibitors. The results of electrochemical impedance spectroscopy (EIS) studies showed that zwitterions inhibit the corrosion through adsorption mechanism. The adsorption of synthesized zwitterions on the mild steel surface was followed the Langmuir adsorption isotherm. The formation of zwitterions film on mild steel surface was confirmed by the scanning electron microscope (SEM) and energy-dispersive X-ray spectroscopy (EDX). The quantum chemical parameters were used to study the reactivity of inhibitors and supported the experimental results. An inhibitor adsorption model is proposed.

Keywords: electrochemical impedance spectroscopy, green corrosion inhibitors, mild steel, SEM, quantum chemical calculation, zwitterions

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Authors: Dagim Ali Hussen, Adnan A. Bekhit, Ariaya Hymete

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In this study, several pyridine derivatives were synthesized and evaluated for their in vitro antimicrobial activity against gram-positive bacteria (S. aureus and B. Cereus), gram-negative bacteria (P. aeruginosa and E. coli) and fungus (C. albican and A niger). The intermediate chalcone derivative 2a,b was synthesized by condensation of pyrazole aldehydes 1a,b with acetophenone in alcoholic KOH. Cyclization of 2a,b with ethyl cyanoacetate ad ammonium acetate resulted in pyridine carbonitrile derivatives 3a,b. Furthermore, condensation of pyridine-4-carboxaldeyhe with different amino-derivatives gave rise to pyridine derivatives 5a,b, 6a,b. The oxadiazole derivative 7a was prepared by cyclization of 6a with acetic anhydride. Characterization of the synthesized compound was performed using IR, 1H NMR, 13C NMR spectra and elemental microanalyses. The antimicrobial results revealed that compounds 5a, 6b and 7a exhibited half fold antibacterial activity compared to ampicillin, against B. cereus. On the other hand, compound 3b showed an equivalent activity compared to miconazole against candida albican (CANDAL 03) and to clotrimazole against the clinical isolate candida albican 6647. Moreover, this compound 3b was further tested for its acute toxicity profile. The results showed that oral LD50 is more that 300 mg/kg and parentral LD50 is more than 100 mg/kg. Compound 3b is a good candidate for antifungal agent with good toxicity profile, and deserves more chemical derivatization and clinical study.

Keywords: antifungal, antimicrobial, Candida albican, pyridine

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Authors: Mehmet Akoz, Mustafa Kul

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Ewes and goats are seasonally polyestrus animals. Their reproductive activities are associated with the reduction or extending of daylight. Melatonin releasing from pineal gland regulates the sexual activities depending on daylight. In recent years, number of ewes decreased in our country. This situation dispatched to developing of some methods to increase productivity. Small ruminants can be synchronized with the natural and medical methods. known methods from natural light set with ram and goat participation. The most important natural methods of male influence, daylight is regulated and feed. On the other hand, progestagens, PGF2α, melatonin, and gonadotropins are commonly used for the purpose of estrus synchranization. But it is not effective PGF2α anestrous season The short-term and long-term progesterone treatment was effective to synchronize estrus in small ruminats during both breeding and anestrus seasons. Alternative choices of progesterone/progestagen have been controlled internal drug release (CIDR) devices, supplying natural progesterone, norgestomet implants, and orally active melengestrol acetate Melatonin anestrous season and should be applied during the transition period, but the season can be synchronized. Estrus synchronisation shortens anestrus season, decreases labor for mating/insemination and estrus pursuit, and induces multiple pregnancies.

Keywords: ewes, goat, synchronization, progestagen, PGF2α

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Authors: Jung-Yoon Lee, Jongmun Kim, Hyo-Jun Chang, Jung-Min Kim

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People’s tendency towards living in apartment houses is increasing in a densely populated country. However, some residents living in apartment houses are bothered by noise coming from the houses above. In order to reduce noise pollution, the communities are increasingly imposing a bylaw, including the limitation of floor impact sound, minimum thickness of floors, and floor soundproofing solutions. This research effort focused on the specific long-time deflection of resilient materials in the floor sound insulation systems of apartment houses. The experimental program consisted of testing nine floor sound insulation specimens subjected to sustained load for 45 days. Two main parameters were considered in the experimental investigation: three types of resilient materials and magnitudes of loads. The test results indicated that the structural behavior of the floor sound insulation systems under long-time load was quite different from that the systems under short-time load. The loading period increased the deflection of floor sound insulation systems and the increasing rate of the long-time deflection of the systems with ethylene vinyl acetate was smaller than that of the systems with low density ethylene polystyrene.

Keywords: resilient materials, floor sound insulation systems, long-time deflection, sustained load, noise pollution

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Authors: Lamees A. Ben Saad, Kah Hwi Kim, Chin Chew Quah, Mustafa Shahimi

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Background: Punica granatum (pomegranate) was used as a traditional medicine in different parts of the world. It has been used in the treatment of pain and inflammatory conditions such as peptic ulcer. The numerous risks associated with nonsteroidal anti-inflammatory drugs (NSAIDs) for the treatment of pain and inflammation give rise to using medicinal herbs as alternative therapies. This study aimed to evaluate the anti-inflammatory effect of the ethyl acetate pomegranate fraction (EtOAc) by determination of its inhibitory effects on lipopolysaccharide (LPS), stimulated nitric oxide (NO), prostaglandin E2 (PGE-2), interleukin-6 (IL-6) and cyclooxxgenase-2 (COX2) release from RAW264.7cells. Methods: The inhibitory effect of EtOAc was evaluated on (LPS) induced NO production, PGE2, and IL-6 quantified by immunoassay kit and prostaglandin E2 competitive ELISA kit. COX2 production is an in vitro indication of possible anti-inflammatory activity and was estimated by Western blotting. Results: EtOAc potentially inhibited LPS-induced nitric oxide, prostaglandin, and IL-6 production. With these findings, it was evident that the EtOAc could reduce the LPS-induced cyclooxygenase-2 (COX-2) at the protein level in a dose-dependent manner as determined by Western blotting. Conclusion: The results emphasize potential therapeutic applications of Punica granatum in the treatment of inflammation.

Keywords: inflammation, Punica granatum, cytotoxicity, cytokines

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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: Hee-Jae Suh, Mi-Na Hong, Min-Ji Kim, Yeon-Seong Jeong, Ok-Hwan Lee, Jae-Wook Shin, Hyang-Sook Chun, Chan Lee

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Brown HT is a bis-azo dye which is permitted in EU as a food colorant. So far, many studies have focused on HPLC using diode array detection (DAD) analysis for detection of this food colorant with different columns and mobile phases. Even though these methods make it possible to detect Brown HT, low recovery, reproducibility, and linearity are still the major limitations for the application in foods. The purpose of this study was to compare various methods for the analysis of Brown HT and to develop an improved analytical methods including pretreatment. Among tested analysis methods, best resolution of Brown HT was observed when the following solvent was applied as a eluent; solvent A of mobile phase was 0.575g NH4H2PO4, and 0.7g Na2HPO4 in 500mL water added with 500mL methanol. The pH was adjusted using phosphoric acid to pH 6.9 and solvent B was methanol. Major peak for Brown HT appeared at the end of separation, 13.4min after injection. This method exhibited relatively high recovery and reproducibility compared with other methods. LOD (0.284 ppm), LOQ (0.861 ppm), resolution (6.143), and selectivity (1.3) of this method were better than those of ammonium acetate solution method which was most frequently used. Precision and accuracy were verified through inter-day test and intra-day test. Various methods for sample pretreatments were developed for different foods and relatively high recovery over 80% was observed in all case. This method exhibited high resolution and reproducibility of Brown HT compared with other previously reported official methods from FSA and, EU regulation.

Keywords: analytic method, Brown HT, food colorants, pretreatment method

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Authors: James Sinclair, Katy Soapi, Brad Carte

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The marine environment has continuously demonstrated to be a rich source of secondary metabolites and bioactive compounds that can address the many pharmaceutical problems facing mankind. The emergence of multidrug resistant pathogens has caused scientists to explore contemporary ways of combating these super bugs. A red-pigmented bacterial strain isolated from a marine alga collected in Fiji was identified to be Pseudoalteromonas rubra from 16s rRNA sequencing. This bacterial strain was cultured using a yeast-peptone media and incubated for five days. The ethyl acetate extract of this bacterium was subjected to chromatographic separation techniques such as vacuum liquid chromatography, flash chromatography, size exclusion chromatography and high-pressure liquid chromatography to yield the pure compound and a number of semi-pure fractions. The crude extract and subsequent purified fractions were analyzed by ultraviolet/visible spectroscopy and mass spectroscopy and was found to contain the compounds ivermectin, stenothricin, cyclo-L-pro-L-val, prodigiosin, mycophenolic acid, phenazine-1-carboxylic acid, eplerenone, staurosporine and pseudoalteromone A. The structure of the pure compound, pseudoalteromone A, was elucidated using NMR 1H, 13C, 1H-1H COSY, HSQC and HMBC spectroscopic data.

Keywords: Pseudoalteromonas rubra, Pseudoalteromone A, secondary metabolites, structure elucidation

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Authors: Chinmayee Choudhury

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Human Melanocortin 4 Receptor (HMC4R) is one of the most potential drug targets for the treatment of obesity which controls the appetite. A deletion of the residues 88-92 in HMC4R is sometimes the cause of severe obesity in the humans. In this study, two homology models are constructed for the normal as well as mutated HMC4Rs and some phytochemicals present in Green Tea, Honey and Cinnamon have been docked to them to study their differential binding to the normal and mutated HMC4R as compared to the natural agonist α- MSH. Two homology models have been constructed for the normal as well as mutated HMC4Rs using the Modeller9v7. Some of the phytochemicals present in Green Tea, Honey, and Cinnamon, which have appetite suppressant activities are constructed, minimized and docked to these normal and mutated HMC4R models using ArgusLab 4.0.1. The mode of binding of the phytochemicals with the Normal and Mutated HMC4Rs have been compared. Further, the mode of binding of these phytochemicals with that of the natural agonist α- Melanocyte Stimulating Hormone(α-MSH) to both normal and mutated HMC4Rs have also been studied. It is observed that the phytochemicals Kaempherol, Epigallocatechin-3-gallate (EGCG) present in Green Tea and Honey, Isorhamnetin, Chlorogenic acid, Chrysin, Galangin, Pinocambrin present in Honey, Cinnamaldehyde, Cinnamyl acetate and Cinnamyl alcohol present in Cinnamon have capacity to form more stable complexes with the Mutated HMC4R as compared to α- MSH. So they may be potential agonists of HMC4R to suppress the appetite.

Keywords: HMC4R, α-MSH, docking, photochemical, appetite suppressant, homology modelling

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Authors: Mohamed H. El-Newehy, Badr M. Thamer, Nasser A. M. Barakat, Mohammad A.Abdelkareem, Salem S. Al-Deyab, Hak Y. Kim

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In this study, the influence of nitrogen doping on the electrocatalytic activity of carbon nanofibers with nickel nanoparticles toward methanol oxidation is introduced. The modified carbon nanofibers have been synthesized from calcination of electrospun nanofiber mats composed of nickel acetate tetrahydrate, poly(vinyl alcohol) and urea in argon atmosphere at 750oC. The utilized physicochemical characterizations indicated that the proposed strategy leads to form carbon nanofibers having nickel nanoparticles and doped by nitrogen. Moreover, due to the high-applied voltage during the electrospinning process, the utilized urea chemically bonds with the polymer matrix, which leads to form nitrogen-doped CNFs after the calcination process. Investigation of the electrocatalytic activity indicated that nitrogen doping NiCNFs strongly enhances the oxidation process of methanol as the current density increases from 52.5 to 198.5 mA/cm2 when the urea content in the original electrospun solution was 4 wt% urea. Moreover, the nanofibrous morphology exhibits distinct impact on the electrocatalytic activity. Also, nitrogen-doping enhanced the stability of the introduced Ni-based electrocatalyst. Overall, the present study introduces effective and simple strategy to modify the electrocatalytic activity of the nickel-based materials.

Keywords: electrospinning, methanol electrooxidation, fuel cells, nitrogen-doping, nickel

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Authors: Rafia Asghar, Abdul Hafeez

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The current research was related with natural dyes’ extraction from the powder of Neem (Azadirachta indica) bark and studied characterization of this dye under microwave radiation’s influence. Both cotton fabric and dyeing powder were exposed to microwave rays for different time intervals (2minutes, 4 minutes, 6 minutes, 8 minutes and 10 minutes) using conventional oven. Aqueous, 60% Methanol and Ethyl Acetate solubilized extracts obtained from Neem (Azadirachta indica) bark were also exposed to different time intervals (2minutes, 4 minutes, 6 minutes, 8 minutes and 10 minutes) of microwave rays exposure. Pre, meta and post mordanting with Alum (2%, 4%, 6%, 8%, and 10%) was done to improve color strength of the extracted dye. Exposure of Neem (Azadirachta indica) bark extract and cotton to microwave rays enhanced the extraction process and dyeing process by reducing extraction time, dyeing time and dyeing temperature. Microwave rays treatment had a very strong influence on color fastness and color strength properties of cotton that was dyes using Neem (Azadirachta indica) bark for 30 minutes and dyeing cotton with that Neem bark extract for 75 minutes at 30°C. Among pre, meta and post mordanting, results indicated that 5% concentration of Alum in meta mordanting exhibited maximum color strength.

Keywords: dyes, natural dyeing, ecofriendly dyes, microwave treatment

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Authors: Rowan Moore, Kai Scheffler, Eugen Damoc, Jennifer Sutton, Aaron Bailey, Stephane Houel, Simon Cubbon, Jonathan Josephs

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Purpose: MS analysis of monoclonal antibodies (mAbs) at the protein and peptide levels is critical during development and production of biopharmaceuticals. The compositions of current generation therapeutic proteins are often complex due to various modifications which may affect efficacy. Intact proteins analyzed by MS are detected in higher charge states that also provide more complexity in mass spectra. Protein analysis in native or native-like conditions with zero or minimal organic solvent and neutral or weakly acidic pH decreases charge state value resulting in mAb detection at higher m/z ranges with more spatial resolution. Methods: Three commercially available mAbs were used for all experiments. Intact proteins were desalted online using size exclusion chromatography (SEC) or reversed phase chromatography coupled on-line with a mass spectrometer. For streamlined use of the LC- MS platform we used a single SEC column and alternately selected specific mobile phases to perform separations in either denaturing or native-like conditions: buffer A (20 % ACN, 0.1 % FA) with Buffer B (100 mM ammonium acetate). For peptide analysis mAbs were proteolytically digested with and without prior reduction and alkylation. The mass spectrometer used for all experiments was a commercially available Thermo Scientific™ hybrid Quadrupole-Orbitrap™ mass spectrometer, equipped with the new BioPharma option which includes a new High Mass Range (HMR) mode that allows for improved high mass transmission and mass detection up to 8000 m/z. Results: We have analyzed the profiles of three mAbs under reducing and native conditions by direct infusion with offline desalting and with on-line desalting via size exclusion and reversed phase type columns. The presence of high salt under denaturing conditions was found to influence the observed charge state envelope and impact mass accuracy after spectral deconvolution. The significantly lower charge states observed under native conditions improves the spatial resolution of protein signals and has significant benefits for the analysis of antibody mixtures, e.g. lysine variants, degradants or sequence variants. This type of analysis requires the detection of masses beyond the standard mass range ranging up to 6000 m/z requiring the extended capabilities available in the new HMR mode. We have compared each antibody sample that was analyzed individually with mixtures in various relative concentrations. For this type of analysis, we observed that apparent native structures persist and ESI is benefited by the addition of low amounts of acetonitrile and formic acid in combination with the ammonium acetate-buffered mobile phase. For analyses on the peptide level we analyzed reduced/alkylated, and non-reduced proteolytic digests of the individual antibodies separated via reversed phase chromatography aiming to retrieve as much information as possible regarding sequence coverage, disulfide bridges, post-translational modifications such as various glycans, sequence variants, and their relative quantification. All data acquired were submitted to a single software package for analysis aiming to obtain a complete picture of the molecules analyzed. Here we demonstrate the capabilities of the mass spectrometer to fully characterize homogeneous and heterogeneous therapeutic proteins on one single platform. Conclusion: Full characterization of heterogeneous intact protein mixtures by improved mass separation on a quadrupole-Orbitrap™ mass spectrometer with extended capabilities has been demonstrated.

Keywords: disulfide bond analysis, intact analysis, native analysis, mass spectrometry, monoclonal antibodies, peptide mapping, post-translational modifications, sequence variants, size exclusion chromatography, therapeutic protein analysis, UHPLC

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Authors: Shivankar Agrawal, Indira Sarangthem

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Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus (MRSA) remains one of the major causes of healthcare-associated and community-onset infections worldwide. Hence the search for non-toxic natural compounds having antibacterial activity has intensified for future drug development. The exploration of less studied niches of Earth can highly increase the possibility to discover novel bioactive compounds. Therefore, in this study, the cultivable fraction of fungi from the sediments of natural hot springs has been studied to mine potential fungal candidates with antibacterial activity against the human pathogen Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus. We isolated diverse strains of thermophilic fungi from a collection of samples from sediment. Following a standard method, we isolated a promising thermophilic fungus strain IBSD19, identified as Acrophialophora levis, possessing the potential to produce an anti-Staphylococcus aureus agent. The growth conditions were optimized and scaled to fermentation, and its produced extract was subjected to chemical extraction. The ethyl acetate fraction was found to display significant activity against Staphylococcus aureus and MRSA with a minimum inhibitory concentration (MIC) of 0.5 mg/ml and 4 mg/ml, respectively. The cell membrane integrity assay and SEM suggested that the fungal metabolites cause bacteria clustering and further lysis of the cell.

Keywords: antibacterial activity, antioxidant, fungi, Staphylococcus aureus, MRSA, thermophiles

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Authors: Tiah Rachmatiah, Subaryanti

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Plants of Lauraceae family are known to contain many chemical compounds which have potential bioactivity such as alkaloids, flavonoids, lactones, terpenes, etc. Actinodaphne macrophylla and Nectandra angustifolia are two species from Lauraceae. A previous study on the crude alkaloidal extract from the bark of Act. macrophylla and n-hexane extract from the bark of N. angustifolia showed antiplasmodial activity against Plasmodium falciparum. The study was continued to find antiplasmodial active compounds from the two extracts. The materials were obtained from Bogor Botanical Garden, West Java, Indonesia. Crude alkaloidal extract of Act. macrophylla was prepared by maceration in dichloromethane after moistened with NH4OH 25% and n-hexane extract of N. angustifolia was prepared by maceration in n-hexane. A major compound was isolated by column chromatography using silica gel and a mixture of CH2Cl2 and methanol as a gradient solvent system for the alkaloidal extract and mixture of n-hexane and ethyl acetate for n-hexane extract. Fine white needle crystals were obtained from the alkaloidal extract and rod crystals from n-hexane extract. Molecular structure of the compounds was determined by analysis of spectra of NMR, IR, MS and compared by references. In vitro bioactivity test of the compound was performed against Plasmodium falciparum. The results showed that the bark of Act. macrophylla contained an aporphine alkaloid, actinodaphnine, that had activity against P. falciparum with IC50 value of 0.095 µg/mL and the bark of N. angustifolia contained a lignan compound, sesamine, with IC50 of 0.122 µg/mL.

Keywords: actinodaphne macrophylla, alkaloid, antiplasmodial, lauraceae, lignan, nectandra angustifolia

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Authors: Assia Belfar, Mohamed Hadjadj, Messaouda Dakmouche, Zineb Ghiaba

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Introduction: This study aims to phytochemical screening; Extracting the active compounds and estimate the effectiveness of antioxidant in Medicinal plants desert Limoniastrum guyonianum (Zeïta) from South Algeria. Methods: Total phenolic content and total flavonoid content using Folin-Ciocalteu and aluminum chloride colorimetric methods, respectively. The total antioxidant capacity was estimated by the following methods: DPPH (1.1-diphenyl-2-picrylhydrazyl radical) and reducing power assay. Results: Phytochemical screening of the plant part reveals the presence of phenols, saponins, flavonoids and tannins. While alkaloids and Terpenoids were absent. The acetonic extract of L. guyonianum was extracted successively with ethyl acetate and butanol. Extraction of yield varied widely in the L. guyonianum ranging from (0.9425 %to 11.131%). The total phenolic content ranged from 53.33 mg GAE/g DW to 672.79 mg GAE/g DW. The total flavonoid concentrations varied from 5.45 to 21.71 mg/100g. IC50 values ranged from 0.02 ± 0.0004 to 0.13 ± 0.002 mg/ml. All extracts showed very good activity of ferric reducing power, the higher power was in butanol fraction (23.91 mM) more effective than BHA, BHT and VC. Conclusions: Demonstrated this study that the acetonic extract of L. guyonianum contain a considerable quantity of phenolic compounds and possess a good antioxidant activity. Can be used as an easily accessible source of Natural Antioxidants and as a possible food supplement and in the pharmaceutical industry.

Keywords: limoniastrum guyonianum, phenolics compounds, flavonoid compound, antioxidant activity

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Authors: N. Boussoualim, H. Trabsa, I. Krache, S. Aouachria, S. Boumerfeg, L. Arrar, A. Baghiani

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The aim of this study consisted in evaluating the antioxidant in vivo properties, anti-hemolytic and XOR inhibitory effect of Globularia alypum L. (GA) extracts. GA was submitted to extraction and fractionation to give crude (CrE), chloroformique (ChE), ethyle acetate (EAE) and aqueos (AqE) extracts. Total polyphenols contents of GA extracts were determined; EAE is the most rich in polyphenols (157,74±5,27 mg GAE/mg of extract). GA Extracts inhibited XO in a concentration-dependent manner, the EAE showed the highest inhibitory properties on the XOR activity (IC50=0,083±0,001 mg/ml), followed by CrE and ChE. The antioxidant activities of the CrE, EAE, and AqE were tested by an in vivo assay in mice, the plasma ability to inhibit DPPH radical was measured, The CrE was found to exhibit the greatest scavenger activity with 48.41±2.763%, followed by AqE and EAE (40.54±7.51% and 41.79±1.654%, respectively). Total antioxidant capacity of red blood cells was measured, from the kinetics of hemolysis obtained. The calculated HT50 reveal an extension of time for half hemolysis in all treated groups compared with the control group. CrE increase significantly HT50 (112,8±2,427). The hemolysis is lagged, indicating that endogenous antioxidants in the erythrocytes can trap radicals to protect them against free-radical-induced hemolysis. Antimicrobial activities of the extracts were determined by the disc diffusion method. Test microorganisms were; 4 Gram positive, 7 gram negative bacteria, most active extracts were EAE and CrE. We deduce a great relationship between the effect on the extracts antibacterial effect and their contents in flavonoid.

Keywords: Globularia alypum, Xanthine oxidoreductase, in vivo-antioxidant activity, hemolysis, polyphenol

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Authors: Hossein Navid, Maryam Adeli Khadem, Shahin Oustan, Mahmoud Zareie

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Among the nutrients needed by the plants, three elements containing nitrate, phosphorus and potassium are more important. The objective of this research was measuring these nutrient amounts in soil using Fourier transform infrared spectroscopy in range of 400- 4000 cm-1. Soil samples for different soil types (sandy, clay and loam) were collected from different areas of East Azerbaijan. Three types of fertilizers in conventional farming (urea, triple superphosphate, potassium sulphate) were used for soil treatment. Each specimen was divided into two categories: The first group was used in the laboratory (direct measurement) to extract nitrate, phosphorus and potassium uptake by colorimetric method of Olsen and ammonium acetate. The second group was used to measure drug absorption spectrometry. In spectrometry, the small amount of soil samples mixed with KBr and was taken in a small pill form. For the tests, the pills were put in the center of infrared spectrometer and graphs were obtained. Analysis of data was done using MINITAB and PLSR software. The data obtained from spectrometry method were compared with amount of soil nutrients obtained from direct drug absorption using EXCEL software. There were good fitting between these two data series. For nitrate, phosphorus and potassium R2 was 79.5%, 92.0% and 81.9%, respectively. Also, results showed that the range of MIR (mid-infrared) is appropriate for determine the amount of soil nitrate and potassium and can be used in future research to obtain detailed maps of land in agricultural use.

Keywords: nitrate, phosphorus, potassium, soil nutrients, spectroscopy

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Authors: P. S. Jain, K. D. Bobade, S. J. Surana

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A simple, selective, precise and Stability-indicating High-performance thin-layer chromatographic method for analysis of Naftopidil both in a bulk and in pharmaceutical formulation has been developed and validated. The method employed, HPTLC aluminium plates precoated with silica gel as the stationary phase. The solvent system consisted of hexane: ethyl acetate: glacial acetic acid (4:4:2 v/v). The system was found to give compact spot for Naftopidil (Rf value of 0.43±0.02). Densitometric analysis of Naftopidil was carried out in the absorbance mode at 253 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r2=0.999±0.0001 with respect to peak area in the concentration range 200-1200 ng per spot. The method was validated for precision, recovery and robustness. The limits of detection and quantification were 20.35 and 61.68 ng per spot, respectively. Naftopidil was subjected to acid and alkali hydrolysis, oxidation and thermal degradation. The drug undergoes degradation under acidic, basic, oxidation and thermal conditions. This indicates that the drug is susceptible to acid, base, oxidation and thermal conditions. The degraded product was well resolved from the pure drug with significantly different Rf value. Statistical analysis proves that the method is repeatable, selective and accurate for the estimation of investigated drug. The proposed developed HPTLC method can be applied for identification and quantitative determination of Naftopidil in bulk drug and pharmaceutical formulation.

Keywords: naftopidil, HPTLC, validation, stability, degradation

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Authors: Sara Torabi, Sadegh Khazalpour, Mahdi Jamshidi

Abstract:

Nitro aromatic compounds are valuable materials because of their applications in the preparation of chemical intermediates for the synthesis of dyes, plastics, perfumes, energetic materials, and pharmaceuticals. Chemical and electrochemical procedures are reported for nitration of aromatic compounds. Flavonoid derivatives are present in many vegetables and fruits and are constituent of many common pharmaceuticals and dietary supplements. Electrochemistry provides very versatile means for the electrosynthesis, mechanistic and kinetic studies. To the best of our knowledge, and despite the importance of these compounds in numerous scientific fields, there are no reports on the electrochemical nitration of Quercetin derivatives. Herein, we describe a green electrochemical synthesis of a nitro compound. In this work, electrochemical oxidation of Quercetin has been studied in the presence of nitrite ion as a nucleophile in acetate buffer solution (c = 0.2 M, pH = 6.0), by means of cyclic voltammetry and controlled-potential coulometry. The results indicate the participation of produced o-benzoquinones in Michael reaction with nitrite ion (in the divided cell) to form the corresponding nitro diol (EC mechanism). The purity of product and characterization was done using ¹H NMR, ¹³C NMR, FTIR spectroscopic techniques. The presented strategies use a water/ethanol mixture as solvent. Ethanol as cosolvent was also used in the previous studies because of its low cost, safety, easy availability, recyclability, bioproductability, and biodegradability. These strategies represent a one-pot and facile process for the synthesis of nitro compound in high yield and purity under green conditions.

Keywords: electrochemical synthesis, green chemistry, cyclic voltammetry, molecular docking

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Authors: Saleh N. Maodaa

Abstract:

Background: Lead (Pb) is an environmental pollutant causing serious health problems, including impairment of reproduction. Visnagin (VIS) is a furanochromone with promising antioxidant and anti-inflammatory effects; however, its protective efficacy against Pb toxicity has not been investigated. Objective: This study evaluated the protective effect of VIS on Pb reproductive toxicity, impaired steroidogenesis and spermatogenesis, oxidative stress and inflammation. Methods: Rats received VIS (30 or 60 mg/kg) and 50 mg/kg lead acetate for 3 weeks, and blood and testes samples were collected. Results: Pb intoxication impaired the pituitary-testicular axis (PTA), manifested by the decreased serum levels of gonadotropins and testosterone. Pb decreased sperm count, motility and viability, increased sperm abnormalities, and downregulated the steroidogenesis markers StAR, CYP17A1, 3β-HSD and 17β-HSD in the testis of rats. VIS significantly increased serum gonadotropins and testosterone, alleviated sperm parameters and upregulated steroidogenesis. In addition, VIS decreased pro-inflammatory cytokines, testicular lipid peroxidation and DNA fragmentation, downregulated Bax, and enhanced antioxidants and Bcl-2 Conclusion: These results demonstrate the protective effect of VIS against Pb reproductive toxicity in rats. VIS improved serum gonadotropins and testosterone, enhanced steroidogenesis and spermatogenesis, and attenuated oxidative injury, inflammation and apoptosis. Therefore, VIS is a promising candidate for the protection against Pb-induced reproduction impairment.

Keywords: pituitary-gonadal axis, cytokines, DNA damage, apoptosis

Procedia PDF Downloads 99