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   Table of Contents - Current issue
May-August 2017
Volume 16 | Issue 2
Page Nos. 71-131

Online since Friday, September 8, 2017

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Synthesis and antimicrobial activity of substituted 1,4-bis-spiro[benzocycloheptene-6(5h),3′(3h-pyrazol)-5-one]-benzene under microwave irradiation and molecular docking study p. 71
Fatma A.A. El-Hag, Ahmed A Elrashedy
Background and objective Spiropyrazole derivatives are one of the most bioactive spiro compounds that play a vital role in drug discovery, such as antibacterial, anti-inflammatory, antifungal, antiviral, analgesic, and antidepressant activities. Moreover, microwave as an energy source enhances the reaction rates and improves the regioselectivity. The aim of this study was to synthesize the spiropyrazole derivative compounds. Molecular docking was performed. Materials and methods 1,3-Dipolar cycloaddition of 6,6′-(1,4-phenylene-bis(methanylylidene))-bis(6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-one) to a variety of nitrilimines (generated in situ by triethylamine dehydrohalogenation of the corresponding hydrazonoyl halides) under microwave irradiation proceeded regioselectively affording spiro[benzo[7]-annulene-6,3′-pyrazol]-4′-yl)phenyl)-spiro[benzo[7]annulene-6,3′-pyrazol]-5(7H)-ones. The structure of the newly synthesized compounds was confirmed on the basis of spectral data and elemental analyses. The antimicrobial activity of the bis(spiropyrazoles) derivatives was tested for antimicrobial activity. Molecular docking was performed and analyzed with the molecular modeling environment program. Results and conclusion Compound 7f has high potency against all fungi (except Candida albicans) and bacterium species (except Pseudomonas aeruginosa) compared with the reference drug fungicide amphotericin B and the standard bactericides ampicillin and gentamicin. Docking of the most active antibacterial compounds 7f and 7g against the dihydropteroate synthase enzyme gave comparable scores for hydrogen bond interaction (−22.9123, −17.5995 kcal/mol(and binding mode to the reference antibiotic sulfamethoxazole (−13.00 kcal/mol).
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Modulation effects of quercetin against copper oxide nanoparticles-induced liver toxicity in rats p. 78
Azza F Arafa, Hassan Z Ghanem, Mahmoud S Soliman, Emad EL-Meligy
Background and objectives Despite the several benefits of nanotechnology, studies indicated that certain nanoparticles (NPs) may cause adverse effects because of their minute size and unique properties. The aim of this study is to investigate the role of quercetin (que) in attenuating toxicity by copper oxide (CuO) NPs in rat liver. Materials and methods The effect of CuO-NPs on the liver was induced by two injections of CuO-NPs (size >20 nm) at the dose 3 mg/kg and 50 mg/kg intraperitoneally in different groups of female rats for 7 days. The effects of NPs were tested by evaluating liver function enzymes: alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase; antioxidant biomarkers: nitric oxide, catalase activity, reduced glutathione, and total antioxidant capacity; DNA damage as shown by comet assay; and histopathological examination of hepatic tissue. Flavonoids que was administered orally to intoxicated rats at the dose of 200 mg/kg for 30 consecutive days. Results and conclusion The present results indicated significant depletion in serum hepatic enzyme activities and improvement in the cellular antioxidant status of CuO-NPs-intoxicated rats after administration of que. Histopathological examination of hepatic tissue treated with que confirmed the previous biochemical results, which showed normal architecture of hepatic tissues. However, treatment of intoxicated rats with que led to a significant reduction in the DNA damage, tail length, and tail moment. Oxidative stress could be considered to play a key role in liver toxicity by CuO-NPs. This research also showed that que is an effective free-radical quencher and could represent a potential valid therapeutic for hepatotoxicity.
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Phytochemical and genotoxicity studies of Citrus reticulata aerial part in mice p. 87
Amal Z Hassan, Khadiga M Ahmed, Nagat S Abu-Gabal, Karima F Mahrous, Nagwa M.M. Shalaby
Background and objectives The genus Citrus (family Rutaceae) is known to contain many bioactive compounds like flavonoids that protect mice against genotoxicity because of their antioxidant and free radical scavenging properties. The aim of this study was to investigate the phytochemical constituents and the protective effect of the ethanolic extract of the aerial part of Citrus reticulata cultivated in Saudi Arabia against genotoxicity induced by benzo(a)pyrene (BaP) in mice. Materials and methods The major constituents from of the aerial part of C. reticulata were isolated using different chromatographic techniques. Identification of compounds was realized through Rf values, shift reagents, and spectroscopic tools such as ultraviolet and nuclear magnetic resonance. The constituents of both unsaponifiable and methylated fatty acids were identified using Gas Liquid Chromatography (GLC) analysis. Essential oil constituents of peels and aerial part of C. reticulata were obtained by hydrodistillation and analyzed by gas chromatography–mass spectrometry. PBS, 1% LMPA, and ethidium bromide were used for the comet assay and quantitative analysis of DNA fragmentation in liver tissue in male rats was determined. About 50 male mice were used in this study, which were allocated in five groups (10 animals each) and treated with BaP and C. reticulata [total ethanolic extract (TE) and petroleum ether fraction]. Results and conclusion Phytochemical investigation of the ethanolic extract from the aerial part of C. reticulata revealed five flavonoids (1–5). GLC analysis of the unsaponifiable fraction showed the presence of α-tocotrienol and α-tocopherol, which belong to the group of vitamin E. A total of 22 compounds were identified in the essential oils of C. reticulata blanco, 12 compounds were found in the aerial part, and 12 compounds were found in the fruit peels. The ethanolic extract was tested for the first time against genotoxicity induced by BaP in mice using the comet assay. TE significantly reduced the damage of DNA caused by BaP in mice. There was a statistically significant increase (P≤0.05) in the DNA fragmentation in the liver tissues of male mice and an increased rate of DNA damage in mice blood cells in the BaP group. Treatment with TE has a significant liver and blood cell protection by inhibiting the rate of DNA damage. These findings led us to conclude that the aerial part of C. reticulata is useful to reduce the genotoxicity induced by hazardous chemical agents.
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Microwave-assisted extraction as an alternative tool for extraction of Stachys aegyptiaca essential oil p. 98
Alaa M Shaheen, Ibrahim A Saleh, El-Sayeda A El-Kashoury, Wafaa A Tawfik, Elsayed A Omar, Mohamed-Elamir F Hegazy, Essam Abdel-Sattar
Background and objectives Stachys aegyptiaca Pers. (family Lamiaceae) is a perennial aromatic wild plant collected from Saint Catherine Protectorate, Sinai. The essential oil of S. aegyptiaca was obtained using two different techniques, conventional hydrodistillation (HD) and microwave-assisted extraction (MAE). The aim of the present study was to compare the effect of the two techniques on oil yield and oil composition. MAE offered reduction in the extraction time with better oil yield compared with HD. Materials and methods Two different techniques, conventional HD and MAE, were used for the extraction of essential oil from S. aegyptiaca. The chemical composition of the essential oil was analyzed using the gas chromatography–mass spectrometry technique. Results and conclusion Gas chromatography–mass spectrometry of the essential oils obtained revealed the presence of 48 and 30 components constituting 99.31 and 99.82% of the total composition of the oils obtained using; MAE and HD, respectively. Variations in the percentage yield and chemical composition were observed. The major component found in the extracted oils was α-pinene (24.65% HD and 41.14% MAE). MAE offered reduction in the extraction time (60 min vs. 3 h) with better oil yield (1.4% w/v) when compared with HD (0.9% w/v). MAE could be used as an alternative tool for the isolation of essential oils from their natural sources.
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Harpullia pendula Planch leaves: phenolics, in vitro antioxidant and α-amylase inhibitory activity p. 103
Sahar S.M. El Souda, Reda S Mohammed, Faten M Ibrahim, Azza A Matloub
Background and objective Harpullia pendula Planch leaves belong to the Sapindaceae family. The study aimed to investigate the phenolic constituents and evaluate the antioxidant and α-amylase inhibitory activities of the plant’s extracts and its major compounds. Materials and methods The compounds were isolated through chromatographic techniques from the defatted ethanolic extract (DAEE). Their structures were determined by ultraviolet, mass spectrometer, and nuclear magnetic resonance spectroscopy. Results The flavonoids kaempferol 3-O-(6″galloyl)- apiofuranosyl (1‴→2″)-β-galactopyranoside, kaempferol-3-O-β-glucopyranosyl(1‴→6″)-β-glucopyranoside, kaempferol 3-O-(6″galloyl)-apiofuranosyl (1‴→2″)-β-galactopyranoside, rutin, vitexin, isovitexin, orientin, quercetin, kaempferol; the tannins ellagic acid, gallic acid, methyl gallate, 2,6-di-O-galloyl(α/β)glucoside, 2,3-di-O-galloyl(α/β)glucoside, and tetragalloyl glucoside in addition to two benzene acetic acid derivatives, harpulliaside A and cavaol B, were isolated from the total bioactive ethanolic extract (TEE). The TEE and the DAEE of H. pendula have a total phenolic content of 255.5±7.18 and 222.9±6.43 mg gallic acid equivalents/g extract, respectively, and a total flavonoid content of 111.6±3.2 and 102.6±2.6 mg quercetin equivalents/g extract, respectively. With respect to the in vitro study, DAEE, TEE, and methyl gallate showed an interesting inhibitory activity on 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) [half maximal inhibitory concentration (IC50): 13.3±0.4, 17.7±0.7, and 19.4±0.08 µg/ml, respectively], nitric oxide (IC50: 12.8±2.54, 18.3±1.6, and 29.8±1.00 µg/ml, respectively), and α-amylase (IC50: 6.1±0.554, 14.4±0.681, and17.5±0.003 µg/ml, respectively). Conclusion H. pendula extracts are rich in phenolic compounds; the aforementioned results suggest that DAEE, TEE, and methyl gallate may be potentially useful in hegemony of obesity and diabetes.
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Liquisolid compacts of meloxicam: in-vitro and in-vivo evaluation p. 112
Remeth J Dias, Shashi Ranjan, Kailas K Mali, Vishwajeet S Ghorpade, Vijay D Havaldar
Background Meloxicam (MXM) is a poorly soluble drug and its low aqueous solubility leads to poor dissolution and bioavailability. Aim The aim of this study was to investigate the potential of a liquisolid system to improve the dissolution rate and the bioavailability of MXM. Materials and methods The liquisolid compacts were prepared using Avicel PH102 as a carrier material, Aerosil 200 as a coating material, Polyethylene glycol 400 as a liquid vehicle, and sodium starch glycolate as a superdisintegrating agent. The 15 liquisolid compact formulations were prepared by varying drug concentrations in the liquid vehicle. Attenuated total reflectance Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction were used to investigate the physicochemical interaction and crystallinity of the drug in the liquisolid compact. MXM compacts were evaluated for uniformity of drug content, tablet hardness, friability, disintegration, and dissolution. An in-vivo study was carried out in male albino rats. The data were presented as mean±SD and were compared using the one-way ANOVA. A P-value less than 0.05 were considered to be significant. Results The liquisolid system of MXM was formulated successfully using Avicel PH102, Aerosil 200, and Polyethylene glycol 200. The results of attenuated total reflectance Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction study indicated the existence of hydrogen bonding between drug and excipients and the complete amorphization of MXM. In-vitro evaluation parameters for the liquisolid compact were found to be within the acceptable limits. It was found that optimized liquisolid tablet formulation showed higher dissolution than the marketed tablet, with more than 80% drug release within 10 min. The pharmacokinetic data showed a higher bioavailability of liquisolid compact of MXM compared with the marketed product. Conclusion The liquisolid compact can be a promising alternative for the formulation of water-insoluble drug MXM with improved dissolution and bioavailability.
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Comparative evaluation of coprecipitation, solvent evaporation, and kneading as techniques to improve solubility and dissolution profiles of a BCS class IV drug p. 121
Ebere I Okoye, Chizoba G Ezenwa, Ome I Aburime, Austinline C Ekweogu
Purpose Furosemide bioavailability is limited by poor solubility and permeability. This study aimed to compare coprecipitation, kneading, and solvent evaporation as solubility and dissolution improvement techniques. Materials and methods Products were prepared with furosemide : polyvinylpyrrolidone : lactose at 1 : 1 : 2, 1 : 2 : 3, 1 : 3 : 4, 1 : 1 : 4, 1 : 2 : 6, 1 : 3 : 8 by coprecipitation, kneading, solvent evaporation or physical blending. They were characterized for physicochemical properties and interaction. Solubilities of furosemide from products were evaluated in water and n-octanol. Dissolution studies on the products were conducted in 0.1 N HCl using USP apparatus II. Results Solubility of pure furosemide was lowest in n-octanol (11.86 μg/ml) and highest in PBS (28.68 μg/ml). Infrared spectra revealed that characteristic peaks in pure furosemide were retained in its formulations, indicating chemical compatibility of furosemide and the excipients. Differential scanning calorimetry thermogram of furosemide showed a melting point at 220°C, which disappeared in its formulations − attributable to amorphization of the drug or overshadow by excipients. Furosemide significantly partitioned more (P<0.05) into water than into n-octanol. Batch 1 : 3 : 4 formulations gave the best partitioning of drug into the solvents, and was in the following order: solvent evaporation>kneading>physical mixtures>coprecipitation. Cumulative amount of furosemide dissolved from pure sample was 8%, whereas amounts from formulations were significantly higher (P<0.05). Coprecipitation products displayed the poorest profiles, kneading gave better profiles, but lagged behind solvent evaporation, whose products’ dissolution profiles were significantly better (P<0.05) than other products studied. Conclusion All the methods improved the solubilities and dissolution profiles of furosemide to various degrees; however, solvent evaporation method was the best.
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Erratum: Assessment of some synthesized novel 9-substituted tetrahydroacridine derivatives in diabetic disease management in rats p. 131

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