eng
Ain Shams University, Faculty of Pharmacy
Archives of Pharmaceutical Sciences Ain Shams University
2356-8380
2356-8399
2018-06-01
2
1
1
15
10.21608/aps.2018.18729
18729
Original Article
Design, synthesis, molecular docking study, and biological evaluation of salicylaldimine derivatives as potential histone deacetylases inhibitors (HDACi) and anticancer agents
Heba Hesham
hebahesham@pharma.asu.edu.eg
1
Deena Lasheen
2
Khaled Abouzid
khaled.abouzid@pharma.asu.edu.eg
3
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Despite the increased success rates of histone deacetylases inhibitors (HDACi) as potent anticancer agents, many metabolic obstacles face the hydroxamic acid-based HDAC inhibitors, which inspired us to develop non-hydroxamate HDAC inhibitors. Based on the established knowledge of the SAR of the reported HDAC inhibitors and based on the knowledge that salicylaldimine moiety is an established chelating agent, a series of salicylaldimine based HDAC inhibitors were designed, synthesized and biologically evaluated. The compound 14 in the present study showed considerable HDAC inhibition and potential antiproliferative activities on NCI cell lines rendering it as a good start for optimization that introduces a new class of non-hydroxamate HDAC inhibitors as potential anticancer agents.
https://aps.journals.ekb.eg/article_18729_08c83ce58176387d699bce02a7fe495f.pdf
Non-hydroxamate HDAC inhibitors
imines
salicylaldimine chelating agents
eng
Ain Shams University, Faculty of Pharmacy
Archives of Pharmaceutical Sciences Ain Shams University
2356-8380
2356-8399
2018-06-01
2
1
16
21
10.21608/aps.2018.18730
18730
Original Article
Alteration of metabolic genes in peripheral blood isolated from patients with acute myocardial infarction
Eman Wasfey
eman_wasfey@pharma.asu.edu.eg
1
Rania Abd El-Razik
rania.shafik@pharma.asu.edu.eg
2
Nadia Hamdy
nadia_hamdy@pharma.asu.edu.eg
3
Wael El-Kilany
wael.kilany@gmail.com
4
Hala El-Mesallamy
hala_elmosalamy@hotmail.com
5
Department of Biochemistry, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
Department of Biochemistry, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
Department of Biochemistry, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
Department of Cardiology, Faculty of Medicine, Ain Shams University, Cairo, Egypt
Department of Biochemistry, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
Accumulating evidence suggests that molecular alterations of peripheral leucocytes are possible diagnostic markers of acute myocardial infarction (AMI). Changed lipid/glucose metabolism is a prominent feature of the pathogenesis of AMI. Silent mating type information regulation 2 homolog 1 (SIRT1) and peroxisome proliferator-activated receptor gamma coactivator factor-α (PGC-1α) regulate mitochondrial function and energy metabolism. Thus, the gene expression of SIRT1 and PGC-1α in peripheral leucocytes isolated from AMI patients and their association with dyslipidemia have been evaluated. Fifty-five male subjects were divided into 40 patients with AMI and 15 healthy control subjects. Peripheral blood samples were obtained on the first day of AMI. Lipid profile parameters were assessed spectrophotometrically. Relative SIRT1 and PGC-1α expression were measured by real-time PCR. Compared with the control group, SIRT1 and PGC-1α expression were significantly decreased in the AMI group. SIRT1 expression was significantly negatively correlated with the age of the participants. SIRT1 expression was significantly positively correlated with PGC-1α expression. Both SIRT1 and PGC-1α expression were negatively correlated with markers of dyslipidemia. In conclusion, SIRT1 and PGC-1α expression are reduced in the acute phase of AMI, which addresses their possible role as potential biomarkers for AMI.
https://aps.journals.ekb.eg/article_18730_b5b215c658df0b827794ded94cac74d1.pdf
AMI
Gene expression
PGC-1 alpha
SIRT1
Mitochondrial dysfunction
eng
Ain Shams University, Faculty of Pharmacy
Archives of Pharmaceutical Sciences Ain Shams University
2356-8380
2356-8399
2018-06-01
2
1
22
30
10.21608/aps.2018.18731
18731
HIV-1 RT-Associated RNase H review
Madonna Mitry
madonna.michael@pharma.asu.edu.eg
1
Nermin Abdou
nerminsamir@pharma.asu.edu.eg
2
Rabah Serya
rabah@pharma.asu.edu.eg
3
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
HIV-RT is an essential enzyme for HIV replication it comprises two associated functions: RNA- and DNA-dependent DNA polymerase (RDDP & DDDP) and ribonuclease H (RNase H). The RNase H is function to cleave RNA strand in RNA/DNA hybrid intermediate in the reverse transcription process. Currently, successful inhibitors target the polymerase function of HIV-RT. RNase H evolves to be a promising target for anti-HIV drug research. This review describes the compounds reported as HIV-1 RNase H inhibitors.
https://aps.journals.ekb.eg/article_18731_a3c3add542da853353a08ffc005171f8.pdf
HIV-1
ribonuclease H
reverse transcriptase
tropolone
hydrazone
eng
Ain Shams University, Faculty of Pharmacy
Archives of Pharmaceutical Sciences Ain Shams University
2356-8380
2356-8399
2018-06-01
2
1
31
36
10.21608/aps.2018.18732
18732
Original Article
Recovery and characterization of Proteus mirabilis persisters
Rana Abokhalil
rana-nasser23@hotmail.com
1
Walid Elkhatib
walid-elkhatib@pharma.asu.edu.eg
2
Mohammad Aboulwafa
maboulwafa@yahoo.com
3
Nadia Hassouna
4
Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, African Union Organization St., Abbassia 11566, Cairo, Egypt
Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Bacterial persistence is a phenomenon in which a subpopulation of cells survives antibiotic treatment. The occurrence of bacterial persisters is associated with recurrence of chronic infections. In this study, we aimed to isolate, characterize persister subpopulation in Proteus mirabilis. Persister cells isolation was done by the dose-dependent killing of ciprofloxacin. Their characterization was achieved by determining their growth rates. Our results revealed that 1.3% of persister cells could be recovered from the Proteus mirabilis test isolate. Upon resuscitation, these cell subpopulations exhibited slow growth rate than wild-type cells. As a common phenomenon demonstrated among microbial pathogens, Proteus mirabilis persisters could be isolated with ciprofloxacin. The slow growth rate is one of its characters recorded in the study for persister cells of such bacterial species.
https://aps.journals.ekb.eg/article_18732_34fca214c07073e56f5e4c6eecef06fd.pdf
Persisters
Multidrug tolerance
Proteus mirabilis
ciprofloxacin
Survival
eng
Ain Shams University, Faculty of Pharmacy
Archives of Pharmaceutical Sciences Ain Shams University
2356-8380
2356-8399
2018-06-01
2
1
37
46
10.21608/aps.2018.18733
18733
Original Article
Biotransformation of caffeic acid into a promising biologically active metabolite by Candida albicans isolate CI-24
Raghda Singab
1
Ahmed Elissawy
aelissawy@pharma.asu.edu.eg
2
Walid Elkhatib
walid-elkhatib@pharma.asu.edu.eg
3
Mahmoud Yassien
mahmoud.yassien@pharma.asu.edu.eg
4
Nadia Hassouna
5
Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, African Union Organization St., Abbassia 11566, Cairo, Egypt
Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
Department of Microbiology and Immunology, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
In this study, a total number of 92 clinical isolates of Candida species was used to test their ability to transform caffeic acid using the two-stage fermentation protocol. The success of the biotransformation process was confirmed by TLC autography method and nuclear magnetic resonance analysis. The obtained chromatograms showed that 7 isolates could perform caffeic acid biotransformation. The biological activities (antibacterial, antifungal, antiviral, and cytotoxic activities) of the extracts of the selected isolates were determined. According to the obtained results, the Candida isolate CI-24 had the most promising biotransformation ability. The methanolic extract of the respective isolate showed a promising anticancer activity against Caco-2 cell line and a potential antibacterial activity against Staphylococcus aureus ATCC 25923. The isolate was genetically identified as Candida albicans (Accession number MH356583) using 28S rRNA sequencing. As determined by NMR and LC-MS analysis, caffeic acid was transformed by Candida albicans strain CI-24 into para-hydroxybenzoic acid.
https://aps.journals.ekb.eg/article_18733_b30191028b0d9658811a852a79ff8c9f.pdf
Biotransformation
Caffeic acid
Candida albicans
Antibacterial
Cytotoxicity
eng
Ain Shams University, Faculty of Pharmacy
Archives of Pharmaceutical Sciences Ain Shams University
2356-8380
2356-8399
2018-06-01
2
1
47
53
10.21608/aps.2018.18734
18734
Original Article
Assessment of circulating Wnt1-inducible signaling pathway protein 1 (WISP1) in obesity and type 2 diabetes mellitus patients
Nada Habib
nada.salah@pharma.asu.edu.eg
1
Mohamed EL-Hefnawy
dr_hefnawy@yahoo.com
2
Hala El-Mesallamy
hala_elmosalamy@hotmail.com
3
Department of Biochemistry, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt
National Institute of Diabetes and Endocrinology (NIDE), Cairo, Egypt
Department of Biochemistry, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
Wnt-inducible signaling pathway protein 1 (WISP1) is a recently identified adipokine that is thought to be involved in mechanisms linking obesity and type 2 diabetes mellitus (T2DM). This study is designed to investigate the correlation between WISP1 serum levels and glycemic parameters in Egyptian population subjects for the first time. Anthropometric parameters, routine biochemical markers, serum levels of WISP1, insulin, proinsulin, and high sensitivity C-reactive protein (hs-CRP) were measured by ELISA kits in 90 subjects (24 non-obese patients with T2DM and 22 obese patients with T2DM compared with 24 healthy volunteers and 20 obese volunteers without T2DM. Serum WISP1 levels were significantly higher in obese patients compared with healthy controls (p < 0.05). WISP1 was significantly correlated to waist circumference (WC) and serum triglycerides (TG). In conclusion, WISP1 might be a pivotal biomarker linking obesity and T2DM.
https://aps.journals.ekb.eg/article_18734_9808ed949c615edcb6f0c4402eed59b3.pdf
Adipokines
Obesity
Type 2 diabetes mellitus
WISP1