New ursane triterpenoids from Ficus pandurata and their binding affinity for human cannabinoid and opioid receptors

Amgad I. M. Khedr,Sabrin R. M. Ibrahim,Gamal A. Mohamed,Hany E. A. Ahmed,Amany S. Ahmad,Mahmoud A. Ramadan,Atef E. Abd El-Baky,Koji Yamada,Samir A. Ross 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.7

Phytochemical investigation of Ficus pandurataHance (Moraceae) fruits has led to the isolation of two newtriterpenoids, ficupanduratin A [1b-hydroxy-3b-acetoxy-11a-methoxy-urs-12-ene] (11) and ficupanduratin B [21ahydroxy-3b-acetoxy-11a-methoxy-urs-12-ene] (17), alongwith 20 known compounds: a-amyrin acetate (1), a-amyrin(2), 3b-acetoxy-20-taraxasten-22-one (3), 3b-acetoxy-11amethoxy-olean-12-ene (4), 3b-acetoxy-11a-methoxy-12-ursene (5), 11-oxo-a-amyrin acetate (6), 11-oxo-b-amyrinacetate (7), palmitic acid (8), stigmast-4,22-diene-3,6-dione(9), stigmast-4-ene-3,6-dione (10), stigmasterol (12), b-sitosterol(13), stigmast-22-ene-3,6-dione (14), stigmastane-3,6-dione (15), 3b,21b-dihydroxy-11a-methoxy-olean-12-ene (16), 3b-hydroxy-11a-methoxyurs-12-ene (18), 6-hydroxystigmast-4,22-diene-3-one (19), 6-hydroxystigmast-4-ene-3-one (20), 11a,21a-dihydroxy-3b-acetoxy-urs-12-ene(21), and b-sitosterol-3-O-b-D-glucopyranoside (22). Compound21 is reported for the first time from a natural source. The structures of the 20 compounds were elucidated on thebasis of IR, 1D (1H and 13C), 2D (1H–1H COSY, HSQC,HMBC and NOESY) NMR and MS spectroscopic data, inaddition to comparison with literature data. The isolatedcompounds were evaluated for their anti-microbial, antimalarial,anti-leishmanial, and cytotoxic activities. In addition,their radioligand displacement affinity on opioid andcannabinoid receptors was assessed. Compounds 4, 11, and15 exhibited good affinity towards the CB2 receptor, withdisplacement values of 69.7, 62.5 and 86.5 %, respectively. Furthermore, the binding mode of the active compounds inthe active site of the CB2 cannabinoid receptors was investigatedthrough molecular modelling.

Histopathological and genetic changes proved the anti‑cancer potential of free and nano‑capsulated sinapic acid

Doaa A. Badr,Mohamed E. Amer,Wagih M. Abd‑Elhay,Mohamed S. M. Nasr,Tamer M. M. Abuamara,Harbi Ali,Aly F. Mohamed,Maha A. Youssef,Nasser S. Awwad,Yi‑Hsu Ju,Ahmed E. Fazary 한국응용생명화학회 2019 Applied Biological Chemistry (Appl Biol Chem) Vol.62 No.5

Cancer is known to be a fierce disease that causes a large percentage of the deaths worldwide. The common cancer treatments; chemotherapy, radiotherapy and surgery are known for their severe side effects; therefore scientists are working on finding solutions to reduce these drawbacks. One of these treatment systems is the sustained released drugs formulations, these systems depend on the encapsulation of the chemotherapy within an emulsifying agent, in order to obtain a slow drug release of low doses over long time intervals. In this study, the anti-cancer effects of free and encapsulated sinapic acid was tested against lung (A549), and colon (CaCo2) cancer cell lines, along with normal fibroblast cells (HFB4) as a negative control. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay was performed for IC50 evaluation, also cell cycle assay was performed to detect cell cycle arrest status and related anti-apoptotic and pro-apoptotic; Blc-2, BAX, and P53 gene profile fold changes post cellular treatment. Data recorded revealed that encapsulated SA showed a lower toxicity than the free form to both cell lines and also to the normal cells. The cell cycle analysis showed a cell cycle arrest at the G2/M phase post cell treatment with the free and encapsulated sinapic acid accompanied with up regulation of Bax and P53 and a down regulation of Blc-2 genes in both cell lines. The data suggest a promising anti-cancer and anti-proliferative potential of free and encapsulated sinapic acid. Also they show that the anti-cancer effect of free and encapsulated sinapic acid is quite close.

Synthesis, Pharmacological Activity Evaluation and Molecular Modeling of New Polynuclear Heterocyclic Compounds Containing Benzimidazole Derivatives

Fatma A. Bassyouni,Tamer S. Saleh,Mahmoud M. ElHefnawi,Sherein I. Abd El-Moez,Waled M. El-Senousy,Mohamed E. Abdel-Rehim 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.12

Novel heterocyclic compounds containing benzimidazole derivatives were synthesized from 2-(1Hbenzimidazol-2-yl) acetonitrile (1) and arylhydrazononitrile derivative 2 was obtained via coupling of 1 with 4-methyl phenyldiazonium salt, which was then reacted with hydroxylamine hydrochloride to give amidooxime derivative 3. This product was cyclized into the corresponding oxadiazole derivative 4 upon reflux in acetic anhydride. Compound 4 was refluxed in DMF in the presence of triethylamine to give the corresponding 5-(1H-benzimidazol-2-yl)-2-p-tolyl-2H-1,2,3-triazol-4-amine 6. Treatment of compound 6 with ethyl chloroformate afforded 2,6-dihydro-2-(4-methylphenyl)-1,2,3-triazolo[4'',5''-4',5']pyrimido[1,6-a]benzimidazole-5(4H)-one (8). 1,2-bis(2-cyanomethyl-1H-benzimidazol-1-yl)ethane-1,2-dione (10) was synthesized via the condensation reaction of 2-(1H-benzimidazol-2-yl) acetonitrile (1) and diethyloxalate. The reactivity of compound 10 towards some diamine reagents was studied. The in vitro antimicrobial activity of the synthesized compounds was investigated against several pathogenic bacterial strains such as Escherichia coli O157, Salmonella typhimurium, E. coli O119, S. paratyphi, Pseudomonas aeruginosa, Staphylococcus aureus, Listeria monocytogenes and Bacillus cereus. The results of MIC revealed that compounds 12a-c showed the most effective antimicrobial activity against tested strains. On the other hand, compounds 12a, b exhibited high activity against rotavirus Wa strain while compounds 12b, c exhibited high activity against adenovirus type 7. In silico target prediction, docking and validation of the compounds 12a-c were performed. The dialkylglycine decarboxylase bacterial enzyme was predicted as a potential bacterial target receptor using pharmacophorebased correspondence with previous leads; giving the highest normalized scores and a high correlation docking score with mean inhibition concentrations. A novel binding mechanism was predicted after docking using the MOE software and its validation.

Nonlinear transient analysis of FG pipe subjected to internal pressure and unsteady temperature in a natural gas facility

Ahmed E. Soliman,Mohamed A. Eltaher,Mohamed A. Attia,Amal E. Alshorbagy 국제구조공학회 2018 Structural Engineering and Mechanics, An Int'l Jou Vol.66 No.1

This study investigates the response of functionally graded (FG) gas pipe under unsteady internal pressure and temperature. The pipe is proposed to be manufactured from FGMs rather than custom carbon steel, to reduce the erosion, corrosion, pressure surge and temperature variation effects caused by conveying of gases. The distribution of material graduations are obeying power and sigmoidal functions varying with the pipe thickness. The sigmoidal distribution is proposed for the 1st time in analysis of FG pipe structure. A Two-dimensional (2D) plane strain problem is proposed to model the pipe cross-section. The Fourier law is applied to describe the heat flux and temperature variation through the pipe thickness. The time variation of internal pressure is described by using exponential-harmonic function. The proposed problem is solved numerically by a two-dimensional (2D) plane strain finite element ABAQUS software. Nine-node isoparametric element is selected. The proposed model is verified with published results. The effects of material graduation, material function, temperature and internal pressures on the response of FG gas pipe are investigated. The coupled temperature and displacement FEM solution is used to find a solution for the stress displacement and temperature fields simultaneously because the thermal and mechanical solutions affected greatly by each other. The obtained results present the applicability of alternative FGM materials rather than classical A106Gr.B steel. According to proposed model and numerical results, the FGM pipe is more effective in natural gas application, especially in eliminating the corrosion, erosion and reduction of stresses.

Nonlinear transient analysis of FG pipe subjected to internal pressure and unsteady temperature in a natural gas facility

Soliman, Ahmed E.,Eltaher, Mohamed A.,Attia, Mohamed A.,Alshorbagy, Amal E. Techno-Press 2018 Structural Engineering and Mechanics, An Int'l Jou Vol.66 No.1

This study investigates the response of functionally graded (FG) gas pipe under unsteady internal pressure and temperature. The pipe is proposed to be manufactured from FGMs rather than custom carbon steel, to reduce the erosion, corrosion, pressure surge and temperature variation effects caused by conveying of gases. The distribution of material graduations are obeying power and sigmoidal functions varying with the pipe thickness. The sigmoidal distribution is proposed for the 1st time in analysis of FG pipe structure. A Two-dimensional (2D) plane strain problem is proposed to model the pipe cross-section. The Fourier law is applied to describe the heat flux and temperature variation through the pipe thickness. The time variation of internal pressure is described by using exponential-harmonic function. The proposed problem is solved numerically by a two-dimensional (2D) plane strain finite element ABAQUS software. Nine-node isoparametric element is selected. The proposed model is verified with published results. The effects of material graduation, material function, temperature and internal pressures on the response of FG gas pipe are investigated. The coupled temperature and displacement FEM solution is used to find a solution for the stress displacement and temperature fields simultaneously because the thermal and mechanical solutions affected greatly by each other. The obtained results present the applicability of alternative FGM materials rather than classical A106Gr.B steel. According to proposed model and numerical results, the FGM pipe is more effective in natural gas application, especially in eliminating the corrosion, erosion and reduction of stresses.

Murraya koenigii (L.) Sprengel seeds and pericarps in relation to their chemical profiles: new approach for multidrug resistant Acinetobacter baumannii ventilator-associated pneumonia

El-Shiekh Riham A.,Elshimy Rana,Mandour Asmaa A.,Kassem Hanaa A. H.,Khaleel Amal E.,Alseekh Saleh,Fernie Alisdair R.,Salem Mohamed A. 한국응용생명화학회 2024 Applied Biological Chemistry (Appl Biol Chem) Vol.67 No.-

Acinetobacter baumannii is without a doubt one of the most problematic bacteria causing hospital-acquired nosocomial infections in today’s healthcare system. To solve the high prevalence of multi-drug resistant (MDR) in A. baumannii, we investigated one of the medicinal plants traditionally used as antibacterial agent; namely Murraya koenigii (L.) Sprengel. The total methanolic extracts of seeds and pericarps were prepared and their anti-bacterial activity was assessed using the agar diffusion method and minimum inhibitory concentration (MIC) was then calculated as compared to tigecycline. Then, an in-vivo murine model was established which confirmed the promising activity of M. koenigii seeds in demonstrating anti-bacterial and anti-inflammatory actions. The histopathological study of lungs, scoring of pulmonary lesions, counting of bacterial loads after infection by multi-drug resistant A. baumannii all provided evidence to support these findings. LC–MS/MS profiling coupled to molecular networking and chemometrics detected the presence of carbazole alkaloids, and coumarins as dominate metabolites of the active seed extracts. Positively correlated metabolites to antibacterial potential were 6-(2ʹ,3ʹ-dihydroxy-3-methylbutyl)- 8-prenylumbelliferone, scopoline, and 5-methoxymurrayatin. An in-silico study was also performed on the crystal structure of MurF from A. baumannii (PDB ID: 4QF5), the studied structures of the mentioned extracts revealed good docking interaction at the active site suggestive of competition with the ATP ligand. These collective findings suggest that extracts of Murraya koenigii (L.) Sprengel seed is a novel prospective for the discovery of drug candidates against infections caused by MDR A. baumannii.

Hibiscus sabdariffa L.: phytoconstituents, nutritive, and pharmacological applications

Mohamed A. Salem,Ahmed Zayed,Magy E. Beshay,Mesih Mirna M. Abdel,Khayal Reem F. Ben,Fady A. George,Shahira M. Ezzat 경희대학교 융합한의과학연구소 2022 Oriental Pharmacy and Experimental Medicine Vol.22 No.3

Hibiscus sabdariffa L. (HS) calyx extracts have been well-documented for the treatment of hypertension, liver dysfunctions, and diabetes among others. An updated concise review of HS regarding phytoconstituents, and involved putative mechanisms of potential biological activities is presented. HS showed other food and other industrial applications, including the preparation of metallic nanoparticles. These activities were explained by the presence of a broad spectrum of valuable phytochemicals, including the red pigments anthocyanins, phenolic, and organic acids and polyphenolics (e.g., flavonoids and tannins). Most of the bioactivities were found to be associated with anthocyanins-rich extracts. Anthocyanins were found to have various mechanisms for the treatment of hypertension, including direct vasodilation and inhibition of angiotensinconverting enzyme (ACE). However, leaves and seeds showed also other potential applications in food industry, owing to the significant amounts of phenolic antioxidant compounds. Therefore, valorization and optimization of bioactive constituents’ extraction from plant biowastes should be considered for maximizing the benefits of HS extracts.

Pentacyclic triterpenes from the stem bark of <i>Combretum hartmannianum</i> Schweinf

Morgan, Abubaker M.A.,Mohamed, Azmey E.,Saophea, Chhon,Park, Sang Un,Kim, Young Ho Elsevier 2018 Biochemical systematics and ecology Vol.77 No.-

<P><B>Abstract</B></P> <P>Chemical investigation of the stem bark of <I>Combretum hartmannianum</I> Schweinf (Combretaceae) led to the isolation and identification of nine compounds with pentacyclic triterpene skeletons. These were identified as three ursane-type triterpenes, ursolic acid (<B>1</B>), pomolic acid (<B>2</B>), and corosolic acid (<B>3</B>); one oleanane-type triterpene, arjunic acid (<B>4</B>); and five oleanane-type triterpene glucosides, arjunglucoside I (<B>5</B>), trachelosperoside E-1 (<B>6</B>), combreglucoside (<B>7</B>), chebuloside II (<B>8</B>), and 2α,3β,6β,19α-tetrahydroxyoleanolic acid 28-<I>O</I>-β-<SMALL>D</SMALL>-glucopyranoside (<B>9</B>). The chemical structures of these compounds were elucidated from spectroscopic data and by comparison of these data with previously published results. This is the first report of triterpene compounds from a species of <I>C. hartmannianum</I> and the first report of compounds <B>2</B> and <B>9</B> from a member of the Combretaceae family.</P> <P><B>Highlights</B></P> <P> <UL> <LI> This study is the first comprehensive chemical investigation of <I>Combretum hartmannianum</I> Schweinf. </LI> <LI> Nine compounds were reported first herein as isolates from <I>C. hartmannianum</I>, and compounds 2 and 9 are reported for the first time from Combretaceae family. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

Chemical composition, aphicidal and antiacetylcholinesterase activities of essential oils against Aphis nerii Boyer de Fonscolombe (Hemiptera: Aphididae)

Hussein Hanaa S.,Tawfeek Mohamed E.,Abdelgaleil Samir A.M. 한국응용곤충학회 2021 Journal of Asia-Pacific Entomology Vol.24 No.2

Aphids are important sucking insects that attack many crops and cause huge economic loss. Essential oils have been proposed to be appropriate alternative to synthetic insecticides due to their low impact on environment and human health. In this work, the chemical compositions of eight essential oils extracted from plants growing in Egypt were determined by gas chromatography/mass spectrometry (GC–MS). The aphicidal activities of the isolated oils were examined against the adults of oleander aphid, Aphis nerii by a leaf-dipping assay. The inhibitory effect of essential oils on acetylcholinesterase (AChE) activity was also tested in vitro. Chemical an alyses showed the essential oils consisted mainly of monoterpene hydrocarbons, oxygenated monoterpenes, sesquiterpene hydrocarbons and oxygenated sesquiterpenes except the oil of Artemisia monosperma which con tained high content of benzenes. The results of toxicity assay showed that the oils of A. monosperma and Citrus sinensis were the most potent toxicants displaying LC 50 value of 0.06 mg/L. The oils of Callistemon viminals, Schinus terebinthifolius and Schinus molle were also highly effective against aphid as their LC 50 values were lower than 1 mg/L. In addition, the highest inhibitory effect on AChE was recorded by 0.5 mg/L C. sinensis with in hibition of 49.33%, while 0.1 mg/L Citrus lemon oil recorded the lowest inhibitory effect with inhibition of 0.4%. In general, six of tested essential oils showed high toxicity against A. nerii and they might be applied in the IPM programs for this insect.

Electricity generation from real industrial wastewater using a single-chamber air cathode microbial fuel cell with an activated carbon anode

Mohamed, H. O.,Obaid, M.,Sayed, E. T.,Liu, Y.,Lee, J.,Park, M.,Barakat, N. A.,Kim, H. Y. Springer Science + Business Media 2017 BIOPROCESS AND BIOSYSTEMS ENGINEERING Vol.40 No.8

<P>This study introduces activated carbon (AC) as an effective anode for microbial fuel cells (MFCs) using real industrial wastewater without treatment or addition of external microorganism mediators. Inexpensive activated carbon is introduced as a proper electrode alternative to carbon cloth and carbon paper materials, which are considered too expensive for the large-scale application of MFCs. AC has a porous interconnected structure with a high bio-available surface area. The large surface area, in addition to the high macro porosity, facilitates the high performance by reducing electron transfer resistance. Extensive characterization, including surface morphology, material chemistry, surface area, mechanical strength and biofilm adhesion, was conducted to confirm the effectiveness of the AC material as an anode in MFCs. The electrochemical performance of AC was also compared to other anodes, i.e., Teflon-treated carbon cloth (CCT), Teflon-treated carbon paper (CPT), untreated carbon cloth (CC) and untreated carbon paper (CP). Initial tests of a single air-cathode MFC display a current density of 1792 mAm(-2), which is approximately four times greater than the maximum value of the other anode materials. COD analyses and Coulombic efficiency (CE) measurements for AC-MFC show the greatest removal of organic compounds and the highest CE efficiency (60 and 71%, respectively). Overall, this study shows a new economical technique for power generation from real industrial wastewater with no treatment and using inexpensive electrode materials.</P>