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Abdel‐Baki Abdel‐Azeem S.,Aboelhadid Shawky M.,Sokmen Atalay,Al‐Quraishy Saleh,Hassan Ahmed O.,Kamel Asmaa A. 한국곤충학회 2021 Entomological Research Vol.51 No.11
The present study was designed to evaluate the insecticidal activity of different concentrations of Foeniculum vulgare and two of its components, trans-anethole and fenchone, against the different stages of Musca domestica. The tested concentrations were applied through a residual film method and topical application on larvae and pupae respectively. Trans-anethole achieved the best results against larvae when compared with those of the fennel or fenchone with LC50 values of 0.58%, 1.57%, and 17.22%, respectively. Moreover, tans-anethole killed 100% of larvae at concentration of 2.5% and fennel achieved the same effect at concentration of 10%, meanwhile fenchone did not reach such an effect at any of the tested concentrations. At the concentration of 10%, fennel oil and trans-anethole induced morphological deformation in the dead larvae such as shrunk bodies with dark colored integument. Regarding the pupicidal activity, fennel oil showed percentage inhibition rate (PIR) of 100% at the concentration of 10% while the same effect was achieved by trans-anethole at concentration of 5%. On the contrary, fenchone did not show any pupicidal activity. Treatment of the third instar house fly larvae with LC5o of fennel oil, trans-anethole, and fenchone significantly inhibited the acetylcholinestrase (AchE) when compared with the control untreated larvae. Additionally, the glutathione-s-transferase (GST) and malondialdehyde (MDA) production significantly increased in the larvae treated with trans-anethole. The results of the present study indicate that the insecticidal activity of fennel oil was mainly attributed to the presence of trans-anethole as a major constituent.
Abdel‐Raheem Mohamed,ALghamdi Huda A.,Reyad Naglaa F. 한국곤충학회 2020 Entomological Research Vol.50 No.5
The red palm weevil, Rhynchophorus ferrugineus, is the biggest pest of various palm species. The aim of this study was to evaluate the impact of the essential oils of purslane, mustard and castor (bulk and nano) on R. ferrugineus and to evaluate the oviposition deterrent effect to prevent new infestations. Prepared concentrations of essential oils (bulk and nano) were tested for their impact on R. ferrugineus larvae, pupae and adults. The most effective oil was purslane oil (bulk and nano), followed by mustard and the least effective was castor. The percent mortality of larvae was 75.2, 45.3 and 17.9% (bulk phase) and 92.5, 84.4 and 65.5% (nano phase) in purslane, mustard and castor, respectively, when treated with the high concentration. The percent mortality of adults was 67.2, 40.0 and 15.6% (bulk phase) and 83.5, 72.9 and 60.0% (nano phase) in purslane, mustard and castor, respectively, when treated with the high concentration. The number of eggs laid decreased with increasing concentration of the tested oils. Purslane essential oil showed good impact on R. ferrugineus larvae and adults followed by mustard and castor oils as bulk and as nano.
Abdel-Alim Abdel-Alim Mohamed,EI-Shorbagi Abdel-Nasser Ahmed,Abdel-Moty Samia Galal,Abdel-Allah Hajjaj Hassan Mohamed The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.6
This work includes the synthesis of 15 final compounds (6a-h and 7b-h) as prod rugs of 5-ASA in the form of the acid itself, esters and amides linked by an amide linkage through a spacer to the endocyclic ring N of nicotinamide. Also, 15 new intermediate compounds were prepared. The target compounds (6b, 6f, 7b, and 7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, $LD_{50}$, in vivo and in vitro metabolism of compound 7f were determined.
Abdel-Alim Mohamed Abdel-Alim,Abdel-Nasser Ahmed El-Shorbagi,Samia Galal Abdel-Moty,Hajjaj Hassan Mohamed Abdel-Allah 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.6
This work includes the synthesis of 15 final compounds (6a-h and 7b-h) as prodrugs of 5-ASA in the form of the acid itself, esters and amides linked by an amide linkage through a spacer to the endocyclic ring N of nicotinamide. Also, 15 new intermediate compounds were prepared. The target compounds (6b, 6f, 7b, and 7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, LD50, in vivo and in vitro metabolism of compound 7f were determined.
Enas Nashaat Amin,Abdel-Alim M. Abdel-Alim,Samia G. Abdel-Moty,Abdel-Naser A. El-Shorbagi,Mahran Sh. Abdel-Rahman 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.1
4,5-dihydro-3(2H)pyridazinones such as CI-914, CI-930 and pimobendan along with tetrahydropyridopyridazine (endralazine) and perhydropyridazinodiazepine (cilazopril) have been used as potent positive inotropes, antihypertensives as well as platelet aggregation inhibitors. Accordingly, the present work involves the synthesis of 24 target compounds; 4,5-dihydro-3(2H)pyridazinones in addition to seven reported intermediates. The chemical structures of the new compounds were assigned by microanalysis, IR, 1H-NMR spectral analysis and some representatives by mass spectrometry. The positive inotropic effect of the final compounds and the intermediates 12a-12d as well as the reported intermediate compound 10 was determined in-vitro on isolated rabbit heart in comparison to digoxin. Data obtained revealed that twelve of the test compounds exhibited higher effective response than digoxin, nine compounds elicited comparable effects to digoxin and eight compounds were less active than digoxin. In addition, four compounds approved marked significant hypotensive effect better than that of the previously reported compound 10. Moreover, two compounds induced complete platelet aggregation inhibition. The last two compounds were also subjected to determination of their LD50 and they showed no signs of toxicity up to the dose level 300 mg/kg (i.p.), while the reported oral LD50 of digoxin is 17.78 mg/kg. Correlation of cardiotonic and hypotensive activities with structures of compounds was tried and pharmacophore models were computed to get useful insight onto the essential structural features required for inhibiting phosphodiesterase-III in the heart muscles and blood vessels.
Abdel Razek Ahmed Abdel Khalek,Abdalla Ahmed,Elfar Reda,Ashmalla Germeen Albair,Ali Khadiga,Barakat Tarik 대한영상의학회 2020 Korean Journal of Radiology Vol.21 No.12
Objective: To assess diffusion tensor imaging (DTI) parameters of the hepatic parenchyma for the differentiation of biliary atresia (BA) from Alagille syndrome (ALGS). Materials and Methods: This study included 32 infants with BA and 12 infants with ALGS groups who had undergone DTI. Fractional anisotropy (FA) and mean diffusivity (MD) of the liver were calculated twice by two separate readers and hepatic tissue was biopsied. Statistical analyses were performed to determine the mean values of the two groups. The optimum cut-off values for DTI differentiation of BA and ALGS were calculated by receiver operating characteristic (ROC) analysis. Results: The mean hepatic MD of BA (1.56 ± 0.20 and 1.63 ± 0.2 x 10-3 mm2/s) was significantly lower than that of ALGS (1.84 ± 0.04 and 1.79 ± 0.03 x 10-3 mm2/s) for both readers (r = 0.8, p = 0.001). Hepatic MD values of 1.77 and 1.79 x 10-3 mm2/s as a threshold for differentiating BA from ALGS showed accuracies of 82 and 79% and area under the curves (AUCs) of 0.90 and 0.91 for both readers, respectively. The mean hepatic FA of BA (0.34 ± 0.04 and 0.36 ± 0.04) was significantly higher (p = 0.01, 0.02) than that of ALGS (0.30 ± 0.06 and 0.31 ± 0.05) for both readers (r = 0.80, p = 0.001). FA values of 0.30 and 0.28 as a threshold for differentiating BA from ALGS showed accuracies of 75% and 82% and AUCs of 0.69 and 0.68 for both readers, respectively. Conclusion: Hepatic DTI parameters are promising quantitative imaging parameters for the detection of hepatic parenchymal changes in BA and ALGS and may be an additional noninvasive imaging tool for the differentiation of BA from ALGS.
Abdel-hafez, Atef Abdel-monem 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.6
As part of an ongoing effort to develop new antineoplastic agents, a series of substituted 3,4-dihydro- and 1,2,3,4-tetrahydro-benzo[4,5]imidazo[1,2-a]pyrimidine derivatives (5-19) were synthesized. 1,2,3,4-Tetrahydrobenzo[4,5]imidazo[1,2-a]pyrimidine-2-one derivatives (5-7) were prepared via one-pot two-component thermal cyclization reaction of 2-aminobenzimidazole 1 and P-substituted methyl cinnamates (2-4). Vilsmir-Haack formylation of these derivatives (5-7) afforded the 2-chloro-3-carboxaldehyde targets (8-10) followed by nucleophilic displacement of the chloro atom in the 3-carboxaldehyde compounds (8-10) to yield the remaining final targets(11-19). The structures of the synthesized derivatives (5-19) were confirmed by means of IR, $^1$H NMR, MS and elemental analyses. The synthesized derivatives (5-19) were subjected to the National Cancer Institute (NCI) in vitro disease human cell screening panel assay. 2-chloro-4-phenyl-3,4-dihydrobenzo[4,5]imidazo[1,2-a]pyrimidine-3-carboxyaldehyde (8, NCl722731) and 4-(4-methoxyphenyl)-2-(4-methylpiperazin-1-yl)-3,4-dihydrobenzo[4,5]imidazo(1,2-a)pyrimidine-3-carboxaldehyde (18, NCI 722739) showed a variable degree of antineoplastic activity against some of the cell lines tested. 2-Chloro-4-(4-nitrophenyl)-3,4-dihy-drobenzo[4,5]imidazo[1,2-a)pyrimidine-3-carboxyaldehyde (10, NCI 722743) exhibited good in vitro antineoplastic activity with subpanel disease selectivity against all the cell lines tested with log$_{10}$ GI$_{50}$ (M), the concentration that inhibits 50% of cell growth, values ranging from -5.08 to <-8.00.