Phosphorylation and Promising In-Vitro Antimicrobial Activity of Some New Organosulfur Compounds

During the past few decades, interest has been rapidly growing in gaining insight into the properties and transformations of thiosemicarbazide and their derivatives due to their appreciable pharmacological activities. Dimethoxy acetophenone reacts with thiosemicarbazide to afford compound (1). The product allowed to react by fusion with diethylmalonate and ethylacetoacetate to give cyclic compounds (3), (4) and (7). Their products are reacted with triphenylphosphine oxide to produce phosphorylated compounds with four and six membered rings. Some of these products display interesting biological and antibacterial activities which lead to great interest for possible therapeutic uses. The structure of the products are confirmed by elemental analyses, IR, UV, 1H-NMR and MS specra.Â

Synthesis and Evaluation of Important Biologically Active Heterocyclic Compounds: Schiff Bases, Oxadiazole and Pyrazolyl Derivatives

In this work, we prepared an excellent yield of (2-oxo-2H-pyrano[3,2-h] quinolin-4-yl) acetic acid; compound (1) and from the reaction of it with hydrazine hydrate (100%) we obtain 2-(2-oxo-2H-pyrano [3,2-h] quinolin-4-yl) aceto hydrazide (2) which is the starting material for the synthesis of several series of new compounds: such as schiff’s bases (3a-e) and compound (4) in good yields, hydrazide derivatives like compound (5), derivatives of mercapto oxadiazole as compound (6) and derivatives of pyrazolyl as compound (7). All these compounds were found to possess high antimicrobial activity against G+ and G- bacteria and against antifungal as described in scheme (1). Anticancer activity was screened only for compound (1). The IC50 value of it against breast cancer was found = 6.83 µM comparable with that of the drug of doxorubicin which has IC50 = 5.6. As a result these newly compounds from (1) to (7) are considerable as potent compounds for various pharmacological activities.Â

Assessment and Prediction of the Thermal Performance of a Centralized Latent Heat Thermal Energy Storage Utilizing Artificial Neural Network

A simulation tool is developed to analyze the thermal performance of a centralized latent heat thermal energy storage system (LHTES) using computational fluid dynamics (CFD). The LHTES system is integrated with a mechanical ventilation system. Paraffin RT20 was used as a phase change material (PCM) and fins are used to enhance its performance. Due to the fact that the numerical calculations take a longer time, the simulations are performed on the first day of each week through summer months and then the database is used to train an artificial neural network (ANN) for predicting of the performance. Then, the LHTES's outlet air-temperature function is integrated into the TRNSYS building thermal response model. The trained ANN is able to improve the prediction of the LHTES's outlet air-temperature for a wide range of inlet conditions (i.e., air-temperature and flow rate). We found that the indoor air-temperature is reduced by about 1.5-2.5

Novel anticancer drug delivery system based on zeolite encapsulating Hamelia patens leaf and flower extracts

181-194Nanotechnology had placed an impact in improving the antiproliferative activity of crude leaf (CL) and flower (CF) extracts of Hamelia patens on the liver (HEPG2) and breast (MCF7) carcinoma cell lines, after their encapsulation onto zeolite (ZSM-5) nanopores, which acts as a drug delivery system (DDS). The cytotoxicity of the new formulas showed remarkable improvement in the activities on HEPG2. CL had low activity on HEPG2, at the tested concentrations, but the ZSM-5 loaded one (CLZ) showed enhanced action with IC50=42 μg/mL. Also, the cytotoxicity of CF improved after Zeolite incorporation, where the IC50 has been changed from 48 μg/mL for CF to 25 μg/mL for CFZ. Moreover, the polar fraction of leaves extracted by methanol (Me.L) showed improvement on the cytotoxicity on MCF7 for zeolite loaded formula (Me.Z) (IC50 had changed from 65 to 44.4 μg/mL). Quantitative estimations for polyphenolic contents as well as the phenolic profiles for CF and CL extracts were inspected using HPLC-DAD to explore the bioactive phytochemical compounds. Acute toxicity test showed that LD50 was 1500 and 2333 mg/kg b.wt. for CL and CF, respectively. The cytogenetic study was also done to detect the chromosome aberrations in somatic and germ cells after CL and CF administration to mice. DPPH antioxidant capacity assay revealed that CL has high redox-active effect than CF. This study is a contribution to the development of a creative new DDS that help in cancer treatment

Polyphasic identification of Penicillium spp. isolated from Spanish semi-hard ripened cheeses

P. 409-444Fifteen samples of semi-hard ripened cheeses, both spoiled (10) and unspoiled (5), and obtained from cheese factories located in Northwest of Spain, were analysed by a dilution plating technique and direct sampling. A total of 32 isolates were identified at species level by a polyphasic approach (phenotypic characterization, partial extrolite analysis and molecular identification). Most isolates (65.6%) belonged to the species P. commune; other species found were P. solitum, P. chrysogenum, P. nordicum, P. expansum and P. cvjetkovicii. All of the P. commune isolates were able to produce cyclopiazonic acid, while the P. nordicum and the P. expansum isolates were producers of ochratoxin A and patulin respectively. Despite this, the role of P. commune as beneficial fungi in cheese ripening should be investigated. Molecular identification based on BenA sequence analysis was able to identify the majority of isolates. The three mycotoxins investigated can be considered key for identification. The polyphasic approach seems to be a very valuable tool for identification of isolates of this complex genusS

Phenolic Compounds and Bioactivity of Leaves of Mayodendron Igneum Kurz

Four apigenin glycosides were isolated from the ethyl acetate extract of the leaves of Mayodendron igneum Fam.Bignoniaceae. They were identified as apigenin 7-O-glucoside; 6-methoxy apigenin-7-O-glucoside; 6-methoxy apigenin-7-O-rhamnoglucoside and 6-hydroxy apigenin-7-O-rhamnoglucoside. In addition an isoflavone glycoside was isolated, and identified as genistin 5,4‵-methyl ether. Ethanol (80%) extract of Mayodendron igneum leaves exhibited significant anti-inflammatory and analgesic activities. LD50 determination of the extract indicated the safety of the leaves of the plant

Synthesis and Anticancer Activity of Some New Derivatives of Coumarin and Quinolinyl Mercaptotriazoles

Pechmann condensation of ethylacetoacetate with derivatives of phenol by heating in absence of solvent and with montmorillonite clays K-10 afforded coumarin derivatives (1a-e) in good yields which on reaction with thiosemicarbazide in anhydrous pyridine yielded coumarin-quinolinyl mercaptotriazole (2a-e). The latter compounds were evaluated for their antimicrobial and anticancer activities. The newly synthesized compounds were characterized by IR, 1HNMR and mass spectra

Chemical Composition, Cytotoxic Activity And Antimicrobial Activity Of Essential Oils Of Leaves And Berries Of Juniperus Phoenice A L. Grown In Egypt.

Hydrodistillation of berries and leaves of Juniperus phoenicea grown in Sinai yielded volatile oils in the yield of 0.36 and 1.96%, respectively. Using gas chromatography/mass spectrometry technique, fifty eight compounds were identified in berry oil representing 99.2% of the oil composition. α-Pinene was the major compound in berry oil (39.30%) followed by sabinene (24.29%). Berry oil composed mainly of monoterpenoids which amounted to 90.53%, of which 72.85% was monoterpene hydrocarbons. The sesquiterpenoids accounted for about 8% of the total oil composition. Leaf oil was composed of about 66 compounds representing 99.16% of the total composition of the oil. α-Pinene was the major constituent of leaf oil at concentration of 38.22%, followed by α -cedrol (31.23%). The monoterpene hydrocarbon was the predominant chemical group (41.29%) followed by the oxygenated sesquiterpenes (32.21%). Both oils showed very high cytotoxic activities against all cell line tested. They showed equal activities against brain (0.6 μg//ml) and cervix (5.0 μg//ml) human cell lines, while berry oil was slightly more active than leaf oil against lung (0.6 and 0.7 μ/ml, respectively), liver (0.7 and 0.9 μg//ml, respectively) and breast human cell lines (0.8 and 1. μg//ml, respectively).The antimicrobial activity and minimum inhibitory concentration (MIC) of leaf and berry oils were also determined. The oils showed high activity against most of the tested strains