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11.
Zainab S. Abbas Ghassan M. Sulaiman Majid S. Jabir Salman A. A. Mohammed Riaz A. Khan Hamdoon A. Mohammed Amal Al-Subaiyel 《Molecules (Basel, Switzerland)》2022,27(14)
The purpose of this study was to evaluate the potential of a newly modified cyclodextrin derivative, water-soluble β-cyclodextrin–epichlorohydrin (β-CD), as an effective drug carrier to enhance the poor solubility and bioavailability of galangin (GAL), a poorly water-soluble model drug. In this regard, inclusion complexes of GAL/β-CDP were prepared. UV-VIS spectrophotometry, Fourier-transform infrared spectroscopy (FTIR), X-ray crystallography (XRD), zeta potential analysis, particle size analysis, field emission scanning electron microscopy (FESEM), and transmission electron microscopy (TEM) were applied to characterize the synthesized GAL/β-CD. Michigan Cancer Foundation-7 (MCF-7; human breast cancer cells) and rat embryo fibroblast (REF; normal cells) were employed to examine the in vitro cytotoxic effects of GAL/β-CD using various parameters. The dye-based tests of MTT and crystal violet clearly exhibited that GAL/β-CD-treated cells had a reduced proliferation rate, an influence that was not found in the normal cell line. The cells’ death was found to follow apoptotic mechanisms, as revealed by the dye-based test of acridine orange/ethidium bromide (AO/EtBr), with the involvement of the mitochondria via caspase-3-mediated events, as manifested by the Rh 123 test. We also included a mouse model to examine possible in vivo toxic effects of GAL/β-CD. It appears that the inclusion complex does not have a significant influence on normal cells, as indicated by serum levels of kidney and liver enzymatic markers, as well as thymic and splenic mass indices. A similar conclusion was reached on the histological level, as manifested by the absence of pathological alterations in the liver, kidney, thymus, spleen, heart, and lung. 相似文献
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Saidbakhrom Saidjalolov Dr. Zainab Edoo Dr. Matthieu Fonvielle Louis Mayer Dr. Laura Iannazzo Dr. Michel Arthur Prof. Dr. Mélanie Etheve-Quelquejeu Dr. Emmanuelle Braud 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(10):3542-3551
The carbapenem class of β-lactams has been optimized against Gram-negative bacteria producing extended-spectrum β-lactamases by introducing substituents at position C2. Carbapenems are currently investigated for the treatment of tuberculosis as these drugs are potent covalent inhibitors of l,d -transpeptidases involved in mycobacterial cell wall assembly. The optimization of carbapenems for inactivation of these unusual targets is sought herein by exploiting the nucleophilicity of the C8 hydroxyl group to introduce chemical diversity. As β-lactams are structure analogs of peptidoglycan precursors, the substituents were chosen to increase similarity between the drug and the substrate. Fourteen peptido-carbapenems were efficiently synthesized. They were more effective than the reference drug, meropenem, owing to the positive impact of a phenethylthio substituent introduced at position C2 but the peptidomimetics added at position C8 did not further improve the activity. Thus, position C8 can be modified to modulate the pharmacokinetic properties of highly efficient carbapenems. 相似文献
14.
Nahed N. E. El-Sayed Taghreed M. Al-Otaibi Mona Alonazi Vijay H. Masand Assem Barakat Zainab M. Almarhoon Abir Ben Bacha 《Molecules (Basel, Switzerland)》2021,26(11)
The pathogenesis of colorectal cancer is a multifactorial process. Dysbiosis and the overexpression of COX-2 and LDHA are important effectors in the initiation and development of the disease through chromosomal instability, PGE2 biosynthesis, and induction of the Warburg effect, respectively. Herein, we report the in vitro testing of some new quinoxalinone and quinazolinone Schiff’s bases as: antibacterial, COX-2 and LDHA inhibitors, and anticolorectal agents on HCT-116 and LoVo cells. Moreover, molecular docking and SAR analyses were performed to identify the structural features contributing to the biological activities. Among the synthesized molecules, the most active cytotoxic agent, (6d) was also a COX-2 inhibitor. In silico ADMET studies predicted that (6d) would have high Caco-2 permeability, and %HIA (99.58%), with low BBB permeability, zero hepatotoxicity, and zero risk of sudden cardiac arrest, or mutagenicity. Further, (6d) is not a potential P-gp substrate, instead, it is a possible P-gpI and II inhibitor, therefore, it can prevent or reverse the multidrug resistance of the anticancer drugs. Collectively, (6d) can be considered as a promising lead suitable for further optimization to develop anti-CRC agents or glycoproteins inhibitors. 相似文献
15.
An insight to the molecular interactions of the FDA approved HIV PR drugs against L38L↑N↑L PR mutant
Zainab K. Sanusi Thavendran Govender Glenn E. M. Maguire Sibusiso B. Maseko Johnson Lin Hendrik G. Kruger Bahareh Honarparvar 《Journal of computer-aided molecular design》2018,32(3):459-471
The aspartate protease of the human immune deficiency type-1 virus (HIV-1) has become a crucial antiviral target in which many useful antiretroviral inhibitors have been developed. However, it seems the emergence of new HIV-1 PR mutations enhances drug resistance, hence, the available FDA approved drugs show less activity towards the protease. A mutation and insertion designated L38L↑N↑L PR was recently reported from subtype of C-SA HIV-1. An integrated two-layered ONIOM (QM:MM) method was employed in this study to examine the binding affinities of the nine HIV PR inhibitors against this mutant. The computed binding free energies as well as experimental data revealed a reduced inhibitory activity towards the L38L↑N↑L PR in comparison with subtype C-SA HIV-1 PR. This observation suggests that the insertion and mutations significantly affect the binding affinities or characteristics of the HIV PIs and/or parent PR. The same trend for the computational binding free energies was observed for eight of the nine inhibitors with respect to the experimental binding free energies. The outcome of this study shows that ONIOM method can be used as a reliable computational approach to rationalize lead compounds against specific targets. The nature of the intermolecular interactions in terms of the host–guest hydrogen bond interactions is discussed using the atoms in molecules (AIM) analysis. Natural bond orbital analysis was also used to determine the extent of charge transfer between the QM region of the L38L↑N↑L PR enzyme and FDA approved drugs. AIM analysis showed that the interaction between the QM region of the L38L↑N↑L PR and FDA approved drugs are electrostatic dominant, the bond stability computed from the NBO analysis supports the results from the AIM application. Future studies will focus on the improvement of the computational model by considering explicit water molecules in the active pocket. We believe that this approach has the potential to provide information that will aid in the design of much improved HIV-1 PR antiviral drugs. 相似文献
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The critical micelle concentrations of cetyltrimethylammonium chloride and cetyltrimethylammonium bromide in solutions of
in N-methylacetami de and in N,N-dimethyl acetamide with added methanol, ethanol, n-propanol, n-butanol and n-pentanol were determined using electrical conductivity and surface tension measurements at various temperatures. Both methods
show that micelles are formed in N-methyl acetamide and N, N-dimethyl acetamide solutions in a presence of n-alcohols. Critical micelle concentrations were also determined as functions of concentration of added alcohol. The data suggest
that alcohol adding leads to an enhancement of penetration of alcohol into the micelle external shell that depends on the
alcohol chain length. Thermodynamic parameters for micellar systems in a presence of n-alcohols were also calculated. 相似文献
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Zahoor Qadir Samra Sadaf Shabir Zainab Rehmat Mariam Zaman Aqsa Nazir Nadia Dar Muhammad Amin Athar 《Applied biochemistry and biotechnology》2010,162(3):671-686
Human serum paraoxonase 1 (PON1) is known as an antioxidant and is also involved in the detoxification of many compounds.
In this study, a novel purification strategy was employed to purify the PON1 by using cholesterol-conjugated magnetic nanoparticles.
Magnetic nanoparticles were synthesized and conjugated with cholesterol through diazotized p-aminohippuric acid. In Fourier transform infrared spectrum of cholesterol-p-aminohippuric acid-Fe3O4 nanoparticles, the appearance of peaks at 3,358.3, 1,645 cm−1, and at 2,334.9 cm−1 confirmed the conjugation. The molecular weight of purified PON1 was nearly 45 kDa on sodium dodecyl sulfate (SDS)–polyacrylamide
gel electrophoresis (PAGE), and isoelectric point was 5.3. The specific activity was 438 U mg−1 protein, and the purification fold was 515 with 73% yield. The K
m values were 1.3 and 0.74 mM with paraoxon and phenyl acetate, respectively. Western blot of 2D-PAGE confirmed the homogeneity
and stability of the enzyme. Mg+2, Mn+2, glycerol, (NH4)2SO4, PEG 6000, Triton X-100, and phenylmethylsulfonyl fluoride did not show any effect on activity. Pb+2, Co+2, Zn2+, ethanol, β-mercaptoethanol, and acetone reduced the activity while Ni2+, Cd2+, Cu2+, iodoacetic acid, SDS, dimethylformamide, DMSO inhibited the activity. In vitro enzyme activity was slightly reduced by acetyl
salicylic and acetaminophen and reduced 50% with amino glycosides and ampicillin antibiotics at concentrations of 0.6 and
30 mg ml−1, respectively. This is the first report for the synthesis of cholesterol-conjugated magnetic nanoparticles for simple purification
of PON1 enzyme. 相似文献
18.
A solid-phase version of the triflate group has been developed and its use demonstrated in traceless linking of aromatics and cross-coupling release strategies. 相似文献
19.
Qualitative characterization of the diffusion of cationic-modified PVA into the cellulose fiber pores 总被引:1,自引:0,他引:1
Pedram Fatehi Bryce MacMillan Zainab Ziaee Huining Xiao 《Colloids and surfaces. A, Physicochemical and engineering aspects》2009,348(1-3):59-63
In this work, the diffusion of cationic poly (vinyl alcohol) (CPVA) with well-defined structures into the pores of bleached kraft fibers was investigated at equilibrium level of adsorption by means of adsorption, solute exclusion technique (SET), and nuclear magnetic resonance (NMR) relaxation method. The results showed that the interaction between CPVA and dextran polymers was weak, which allowed us to use the SET method to investigate the variation in the pore size of fibers upon diffusing CPVAs. Both adsorption and SET methods confirmed the diffusion of CPVA polymers into the fiber pores. However, the NMR technique was unable to reflect the pore size changes. The main reason for such results was probably the error that occurred in removing water between fibers via applying the water retention value (WRV) test prior to the NMR analysis. In fact, not all of the water on the fiber surface, especially on the surface of CPVA-modified fibers, could be removed by the WRV, introducing some error in the NMR analysis. 相似文献
20.
M. A. Alawi 《Analytical and bioanalytical chemistry》1983,315(4):358-359