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Russian journal of bioorganic chemistry
Consultants Bureau
Russian journal of bioorganic chemistry

Consultants Bureau

1068-1620

Russian journal of bioorganic chemistry/Journal Russian journal of bioorganic chemistrySCICCRISTP
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    Comprehensive Review on Versatile Pharmacology of Quinoxaline Derivative

    V. Bala AakashRamalakshmi, N.Bhuvaneswari, S.Sankari, E....
    21页
    查看更多>>摘要：Quinoxaline is a nitrogen-containing heterocyclic compound having many pharmaceutical and industrial purposes. It can be synthesized by adopting green chemistry principles. The quinoxaline containing drugs such as Olaquindox, Echinomycin, Atinoleutin, Levomycin, and Carbadox are currently used as an antibiotic in the market. The objective of this review is to enumerate the various multifunctional property of the quinoxaline moiety. This present review contains the newer quinoxaline derivatives against many targets, receptors, or microorganisms. This work comprises the study on quinoxaline as a core unit from the year 2002 to 2020. All the collected literature has been combined and highlighted for the effective use of that particular derivative. Various potent quinoxaline compounds have been analyzed in the literature. About 50 papers have been reviewed for the novel quinoxaline compounds, the potent derivatives have been reported, and structures were given. The critical role of the quinoxaline on the various heterocyclic moieties has been given more attention in this review. This review paves the way as a source of references for the further development of drug discovery in the wide spectrum of its biological importance.
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    ATP-Dependent Lon Proteases in the Cellular Protein Quality Control System

    Kudzhaev, A. M.Andrianova, A. G.Gustchina, A. E.Smirnov, I., V...
    32页
    查看更多>>摘要：The Protein Quality Control (PQC) system plays a leading role in maintaining the safety of the cellular proteome in all natural kingdoms. This review summarizes information about the structural and functional characteristics of molecular chaperones and energy-dependent proteases that form the PQC system, emphasizing the crucial role of proteins belonging to the AAA(+) superfamily, with the focus on ATP-dependent Lon proteases as a special family in the PQC. Similarities and differences among the enzymes of individual Lon subfamilies are discussed in detail using up-to-date data, elucidating the structural features and unique mechanisms of functioning of these proteins.
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    The Influence of Lipid Matrix Composition on the Microenvironment of Levofloxacin in Liposomal Forms

    Le-Deygen, I. M.Safronova, A. S.Kolmogorov, I. M.Skuredina, A. A....
    10页
    查看更多>>摘要：We have studied the interaction of the antibacterial drug levofloxacin with lipid bilayers of various compositions: 100% DPPC and with the addition of 20% cardiolipin. For DPPC liposomes, levofloxacin was found to penetrate into the subpolar region at the lipid-water interface. The role of the anionic lipid in the interaction of an active molecule with a bilayer has been established: levofloxacin enters the microenvironment of the phosphate group, displacing water, and does not penetrate into the hydrophobic part of the bilayer. For the first time, the study of the microenvironment of levofloxacin in the liposome by IR and CD spectroscopy was carried out. Such an approach based on a combination of several spectral methods opens up new prospects for the creation of new medicinal properties and the possibility of predicting the nature of the interaction of active molecules with biomembranes in order to predict their efficacy and potential side effects.
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    Identification of the Inhibition Effects of Some Natural Antiproliferative Agents on CA-I, CA-II, and AChE Activities Isolated from Human Erythrocytes by Kinetic and Molecular Docking Studies

    Kilinc, N.Guller, U.Alim, Z.
    11页
    查看更多>>摘要：Nowadays the determination of inhibitors of carbonic anhydrase isoenzymes (CAs) have become one of the main goals of drug design studies, and inhibitors of CAs have taken their place in clinical applications to be used in the treatment and diagnosis of many diseases from glaucoma to cancer. On the other hand, acetylcholinesterase (AChE) inhibitors are also the main target molecules for the treatment of Alzheimer's disease. However, the unwanted side effects of existing CA and AChE inhibitors necessitate the identification of new and selective inhibitors of these enzymes. In this study, we examined the inhibition effects of some natural antiproliferative agents on CA-I, CA-II, and AChE activities isolated from human erythrocytes. Betulinic acid (I) had the strongest inhibitory effect on esterase activity of hCA-I (IC50 29.16 mu M) and hCA-II (IC50 31.82 mu M). On the other hand, sanguinarine chloride (VI) had the strongest inhibitory effect (IC50: 19.44 mu M) on hAChE activity. Molecular modeling studies were also carried out to elucidate the inhibition mechanism of betulinic acid on hCA-I and hCA-II isoenzymes and sanguinarine chloride on the hAChE enzyme. We believe that the results we obtained in this study will contribute to the design of new and natural CA and AChE inhibitors.
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    Biologically Active Fragment of the Receptor for Advanced Glycation End Products (RAGE) Is Able to Inhibit Oligomerization of the Beta-Amyloid

    Volkova, T. D.Avetisyan, A., VKoroev, D. O.Kamynina, A., V...
    8页
    查看更多>>摘要：It was found earlier that the synthetic fragment corresponding to the 60-76 sequence of the extracellular domain of the receptor for advanced glycation end products (RAGE) had a protective effect on animal and cellular models of Alzheimer's disease. It was proposed that this effect was mediated via the interaction of the peptide with beta-amyloid (A beta), which was one of the RAGE ligands, by inhibiting the formation of toxic A beta oligomers. The aim of this study was an application of physicochemical methods to an investigation of the ability of the 60-76 peptide to prevent the A beta 40 oligomerization in solution in comparison with the nonprotective 65-76 truncated peptide. The dynamics of the formation of the A beta 40 fibrils in the presence of the peptides was evaluated using thioflavin T. The relative sizes of oligomers were determined by dynamic light scattering. The peptide binding to A beta 40 was examined by fluorescence titration. We demonstrated by the two methods that the peptide corresponding to the 60-76 sequence of RAGE considerably inhibited (by more than 90%) the formation of oligomers and fibrils of A beta 40 distinct from the 65-76 peptide. In addition, we found that the protective effect of the peptides and their ability to inhibit the A beta 40 oligomerization did not correlate with their binding to the monomeric/tetrameric A beta 40. We confirmed in vitro the hypothesis that the protective activity of the synthetic 60-76 fragment of RAGE was associated with its ability to inhibit the A beta oligomerization.
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    Discovery of New Quinazoline-Based Anticancer Agents as VEGFR-2 Inhibitors and Apoptosis Inducers

    Ahmed, M. F.Khalifa, A. S.Eed, E. M.
    10页
    查看更多>>摘要：Novel quinazoline compounds have been designed and synthesized aiming to discover new anticancer agents. Additional study was carried out on the most powerful derivatives, (Xb). A cell cycle research indicated that (Xb) mostly stops the cell cycle in the G2/M phase. The Annexin V-FITC apoptosis assay revealed that (Xb) increased apoptosis when compared with the control. It also demonstrated decreased anti-apoptotic Bcl-2 protein expression and increased BAX and caspases 3 expression levels.
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    Novel Furochromone Derivatives of Potential Anticancer Activity Targeting EGFR Tyrosine Kinase. Synthesis and Molecular Docking Study

    Fawzy, N. M.Ahmed, K. M.Abo-Salem, H. M.Aly, M. S....
    19页
    查看更多>>摘要：In this study, a new class of furochromone derivatives bearing beta-naphthol was synthesized via one-pot multicomponent reactions. First, condensation one mole of furochromone carbaldehyde (I) with two moles of beta-naphthol afforded the corresponding Xanthene' dye derivatives (II). A one-pot three-component reaction of (I), beta-naphthol and urea or thiourea result in the formation of the corresponding oxazinones (Ma, b). Moreover, reaction of (I) and beta-naphthol with primary aromatic amines, heterocyclic amines or 2ry amines using triethyl amine as catalyst afforded the corresponding amino derivatives (IV-XIII). On the other hand, a one-pot three-component reaction of (I) and beta-naphthol with active methylene compounds namely, malononitrile, propionitrile, diethylmalonate methyl propionate or diethyl succinate led to the formation of furochromone derivatives (VIV)-(XVIII). The antitumor activities of certain selected new compounds were screened, in vitro, against a panel of three (liver, HepG2; breast, MCF-7, HepG-2 and PC-3) human solid tumor cell lines as well as the normal cell line (human normal melanocyte, HFB4) in comparison to the known anticancer drug: 5-fluorouracil using MTT assay. Our results showed that the vast majority of the newly synthesized derivatives did not exert any activity against the growth of HFB4normal cell line. Compounds (IV), (XIIIa), and (XIIIb) revealed remarkable anticancer activity against MCF-7 cell line with IC50 5.4, 4.65, and 6.09 mu g/mL respectively compared to 5-fluorouracil (IC50 = 4.7 mu g/mL). Moreover, compounds (IIIb), (VII), (IX), and (XVI) showed potent activity against HepG-2 cancer cell line of IC50 ranging from 5.57 to 6.34 mu g/mL. Compound (VII) revealed also anticancer activity against PC-3 cancer cell line with IC50 6.77 mu g/mL vs. 5.05 for 5-fluorouracil. The inhibitory activity of the most active anti-proliferative compounds (IIIb), (IV), (VII), (IX), (XIIIa, b) and (XVI) against EGFR were studied. Compound (VII) showed the best inhibitory activity against EGFR with IC50 39.93 ng/ml in comparison to erlotinib (IC50 29.18 ng/mL). Molecular docking simulation was performed to position compounds (IIIb), (IV), (VII), (IX), (XIIIa, b), and (XVI) into the EGFR active site to determine the probable binding mode.
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    The Effects of Nitroazolopyrimidines on the A(1) Adenosine Receptor and Intraocular Pressure in Rats

    Savateev, K., VRusinov, V. L.Kotovskaya, S. K.Spasov, A. A....
    6页
    查看更多>>摘要：Six compounds of the 5(7)-alkylamino-6-nitroazolopyrimidine and 8-alkylazolo[5,1-b]purine series were selected based on the structural analysis of A(1) adenosine receptor inhibitors and the role of this biological target in the modulation of intraocular pressure, an important factor in the pathogenesis of glaucoma. These heterocycles were shown to exhibit a weak affinity towards the A(1) adenosine receptor on an in vitro model of the adenosine-dependent change of the chronotropic effect on isolated atria of white mice. On the other hand, thiadiazolo[3,2-a]pyrimidines and triazolo[5,1-b]purine displayed an in vivo hypotensive effect in rats. The leading compound, 5-methyl-8-(hydroxyethyl)triazolo[5,1-b]purine) (0.2% solution), caused a 34% reduction of ophthalmotonus in 3 h without an adverse resorptive effect. In addition, using the MTT-test it was shown on the human HepG2 cell line that the heterocycles affecting the intraocular pressure were by one to two orders of magnitude less cytotoxic than the reference doxorubicin.
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    Bluetongue Virus Detection Using Microspheres Conjugated with Monoclonal Antibodies against Group-Specific Protein Vp7 by Flow Virometry

    Rudenko, N., VKaratovskaya, A. P.Zamyatina, A., VMalogolovkin, A. S....
    8页
    查看更多>>摘要：Bluetongue is a reemerging transmissive infectious disease that threatens all countries with intensive livestock production. In cattle, bluetongue may either lead to lethality or be asymptomatic with a long-lasting viremic phase, which makes development of high-sensitivity bluetongue virus detection methods an important task. Methods of virus particle detection based on immunofluorescence assay in bluetongue-infected Vero cells, sandwich enzyme immunoassay and flow virometry have been developed using high-affinity monoclonal antibodies against VP7 (viral protein 7). High analytical sensitivity of the method (10(-0.25) TCID50/mL (tissue cytopathogenic dose)) was demonstrated in a flow cytometry assay. The ability to rapidly and efficiently detect virus particles in the biological fluids obtained from animals by flow virometry was demonstrated in a model system in which BTV was measured in cattle blood serum. The detection sensitivity was 10(0.75) TCID50/mL.
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    Synthesis and QSAR of Novel Ketoprofen-Chalcone-Amide Hybrides as Acetylcholinesterase (AChE) Inhibitors for Possible Treatment of Alzheimer Disease

    Al-Mosawi, S. K.Al-Hazam, H. A.Abbas, A. F.Nasif, Z. N....
    8页
    查看更多>>摘要：A new series of the anti-inflammatory drug ketoprofen derivatives bearing aryl chalcone-amide congeners were synthesized. The structures of the synthesized compounds were identified by the H-1 NMR, C-13 NMR, and EIMS spectroscopic methods. The inhibitory activity of the synthesized compounds on cholinesterase enzymes was investigated. Biological results revealed that five compounds displayed moderate activities against acetylcholinesterase (AChE) with IC50 values below 10 mu M. Among the tested compounds, (BTPhP) was found to be the most potent against AChE (IC50 0.98 +/- 0.02 mu M), while the chalcone-amide analogues (MeOPh), (HydPh), (FPh), and (ChPh) exhibited moderate activities with IC50 values ranged between 5.19-9.61 mu M. Molecular docking study showed that compound (BTPhP) could combine with the active site of acetylcholinesterase by the pi-pi between the ketoprofen phenyl groups is embedded in a cavity surrounded by two aromatic residues of Tyr334 and Trp279. The present results strongly suggest that the para-position of the D-ring should be a preferred modification site for further structural optimization design. Thus, compound (BTPhP) emerged as a promising lead for the development of new acetylcholinesterase inhibitor agent. The preliminary quantum structure-activity relationship (QSAR) among the newly synthesized congeners was obtained by Genetic Function Approximation (GFA).
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