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Russian Journal of Bioorganic Chemistry
Journal Prestige (SJR): 0.221  Citation Impact (citeScore): 1 Number of Followers: 1  Hybrid journal (It can contain Open Access articles)ISSN (Print) 1608-330X - ISSN (Online) 1068-1620 Published by Springer-Verlag  [2468 journals]
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- Erratum to: Structural Analogs of Dehydrozingerone Containing a Pyridoxine
Fragment Exhibit Membrane-Modulating Properties and Synergistically
Enhance the Antitumor Activity of Cytostatics-
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Abstract: Erratum
PubDate: 2023-11-01
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- Effeсts of the 70th Amino Acid Residue on the Photostability of FAST
Complexes-
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Abstract: We report a novel mutant of FAST–FAST T70V. The fluorescent properties of the complex were studied to show that the T70V mutation only slightly affects the fluorescent properties but has no effect on the photostability of the protein–fluorogen complex. Thus, evidence was obtained showing that the threonine alcohol group is not involved in the irreversible photodegradation of the complex, despite the possible contact of the amino acid with the fluorogen.
PubDate: 2023-11-01
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- Synthesis, Antibacterial, and Antifungal Evaluation of New Class of
Pyrimido[4,5-d]pyrimidine, Pyrazolo[3,4-d]pyrimidine, and
Pyrimido[4,5-b]quinoline Derived from α,α-Ketene Dithioacetals as fused
Five and Six-membered Heterocycle Derivatives-
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Abstract: A novel heterocyclic compounds containing pyrimido[4,5-d]pyrimidine (IIIa–IIIb) and (IVa–IVb), pyrazolo[3,4-d]pyrimidine (Va'–Ve') and (VIa'–VIe'), and pyrimido[4,5-b]quinoline (VIIa'–VIIe') and (VIIIa'–VIIIe') were designed and synthesized from the starting materials, 5-(bis(methylthio)methylene)-1,3-diphenylpyrimidine-2,4,6(1H,3H,5H)-trione (IIa) and 5-(bis(methylthio)methylene)-1,3-diphenyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione (IIb) as efficient α,α-ketene dithioacetals is reported. The synthetic approaches of these types of compounds will provide an innovative molecular framework to the designing of new active heterocyclic compounds. In our study, we also present optimization of the method for synthesis along with antimicrobial evaluation of these newly synthesized compounds as antibacterial agents against the bacterial strains, like E. coli, B. subtilis, S. aureus, and P. aeruginosa also as antifungal agents against B. cinerea, C. arachidicola, A. solani, G. zeae, S. sclerotiorum, and R. cerealis. Preliminary bioassay showed that most of them exhibited certain-to-excellent antibacterial and antifungal activity. Among all the evaluated compounds, it was found that the synthesized compounds (IVb) and (VIIIc') showed the outstanding antibacterial activity (100%) against the strains E coli and S. aureus respectively comparable to the standard drug Ciprofloxacin at the same concenteration while the others exhibited better antifungal activity at 100 µg/mL. The outstanding antifungal activity (>90%) comparable to the positive controls trifloxystrobin and azoxystrobin exhibited by (VIIIc') against B. cinerea, (IVb) and (Vc') against A. solani, (IVb) against S. sclerotiorum alongwith compounds (VIb'–VIc') against R. cerealis. The structures of all the new synthesized compounds were elucidated by elemental analysis, IR, 1H NMR, and 13C NMR.
PubDate: 2023-11-01
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- Synthesis and Biological Evaluation of Chromene-1,3,4-Oxadiazole based
1,2,3-Triazoles: EGFR-targeting Anticancer Agents-
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Abstract: In search of the better anticancer agents, a series of chromene-1,3,4-oxadiazole containing 1,2,3-triazole derivatives were synthesized using 6-fluoro-2-(5-(prop-2-yn-1-ylsulfonyl)-1,3,4-oxadiazol-2-yl)-4H-chromen-4-one and freshly prepared substituted aryl azides. The newly synthesized derivatives were evaluated for their in vitro cytotoxic activity against MCF-7 and A-549. Among all the synthesized compounds, 6-fluoro-2-(5-(((1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-1,3,4-oxadiazol-2-yl)-4H-chromen-4-one and 2-(5-(((1-(3,5-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-1,3,4-oxadiazol-2-yl)-6-fluoro-4H-chromen-4-one shows potent anticancer activity as compared to remaining derivatives. Similarly, the compounds 2-(5-(((1-(3,5-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-1,3,4-oxadiazol-2-yl)-6-fluoro-4H-chromen-4-one and 2-(5-(((1-(3,5-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-1,3,4-oxadiazol-2-yl)-6-fluoro-4H-chromen-4-ones were found to be active against EGFR.
PubDate: 2023-11-01
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- Therapeutic Nucleic Acids Against Herpes Simplex Viruses (A Review)
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Abstract: The Herpes simplex virus (HSV) causes a wide range of diseases ranging from relatively mild primary skin lesions to severe and often fatal episodes of encephalitis. Currently, the most effective drugs for HSV-infected people are nucleoside analogs (e.g., acyclovir), which target enzymes encoded by viral DNA. The effectiveness of nucleoside analogs is reduced because of poor solubility in water, rapid intracellular catabolism, high cellular toxicity, and the appearance of resistant viral strains. Antisense technology, which exploits therapeutic nucleic acids (antisense oligonucleotides, their analogs, and siRNAs), seems to be a promising alternative antiviral therapy due to the high affinity of these agents to target nucleic acids, their high solubility in water, and low cytotoxicity. In the last decade, antisense oligonucleotides have been investigated as potential medicines for various diseases associated with harmful nucleic acids. Oligonucleotides with different chemical modifications targeted to specific regions of the HSV genome have shown effectiveness in suppressing the virus. siRNA-based agents have demonstrated prolonged and efficient (up to 99%) inhibition of HSV replication. The publications over the past 30 years considered in the review suggest the promising use of therapeutic nucleic acids to combat herpes viral infections.
PubDate: 2023-11-01
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- Synthesis, Characterization, and In Vivo Evaluation of Escitalopram
Analogues for Depression-
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Abstract: Escitalopram, (S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile, is a highly selective and potent serotonin reuptake inhibitor that is used to treat depression. Herein, we report the synthesis of ester analogues of escitalopram having π-systems in their structures where the ester groups including allyl, propargyl, methoxyethyl, benzyl and ρ-tolyl replaced the cyano group in escitalopram. The analogues were designed to test the possibility of binding such groups to the phenyl in Phe341 amino acid that is in close proximity to the cyano group in human serotonin transporter (hSERT). In vivo antidepressant evaluation showed good activity for the analogues compared to escitalopram.
PubDate: 2023-11-01
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- Some Azo Dyes Containing Uracil: DFT Study and Antiparasitic Activity for
Leishmania promastigotes and Trichomonas vaginalis-
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Abstract: In this study 6-aminopyrimidine-2,4,5(3)-trione-5-[(phenyl)hydrazone] (dye 1) and 6-aminopyrimidine-2,4,5(3)-trione-5-[(4-methoxyphenyl)hydrazone] (dye 2) were resynthesized by method given in the literature and confirmed structurally using Fourier transform infrared (FT-IR) and proton nuclear magnetic resonance (1H NMR) spectroscopic methods. For the first time, for dyes 1 and 2, both theoretical studies were performed and investigated in terms of antiparasitic activity. The density functional theory (DFT) calculations for possible tautomeric forms of dyes 1 and 2 were carried out by using DFT/B3LYP/6-311++G (d,p) method. Thus, optimized geometries, IR and 1H NMR spectral data were obtained and compared with experimental ones. Therefore, the most possible tautomeric forms were determined for dyes 1 and 2. Results show that in the gas phase and dimethyl sulfoxide (DMSO) solvent for both dyes, the amine-diketo-hydrazone forms (T-I-H) are the lowest energy and therefore the most stable form. Leishmania spp. and Trichomonas vaginalis are flagellated protozoan parasites that cause parasitic infections in humans. In vitro antiparasitic activity of dye 1 and dye 2 against Trichomonas vaginalis trophozoites, Leishmania tropica, Leishmania major, and Leishmania infantum promastigotes were determined for the first time. The in vitro antileishmanial and antitrichomonal activity was performed by microdilution method. Amphotericin B and Metronidazole were used for Leishmania spp. promastigotes, and T. vaginalis trophozoites, as a control drug, respectively. The Minimum Lethal Concentration (MLC) was determined and compared with the control.
PubDate: 2023-11-01
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- Synthesis and Biological Evaluation of Fused
Imidazo[4,5,1-kl]phenothiazine-4-sulfonamides as Potent Antibacterial and
Anticancer Agents-
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Abstract: In the present study, a novel series of fused imidazole derivatives containing phenothiazine-sulfonamide were synthesized and screened for their antibacterial and anticancer activity. Among all the compounds synthesized, 1-(3-bromophenyl)imidazo[4,5,1-kl]phenothiazine-4-sulfonamide and 1-(2-chlorophenyl)imidazo[4,5,1-kl]phenothiazine-4-sulfonamide showed excellent inhibition against B. subtilis ans S. aureus bacterial strains with MICs values 3.12 and 6.25 µg/mL. While the rest of the compounds showed moderate to low activity against all strains tested compared to standard streptomycin. Similarly, compounds 1-(4-hydroxy-3-methoxyphenyl)imidazo[4,5,1-kl]phenothiazine-4-sulfonamide and 1-(4-hydroxyphenyl)imidazo[4,5,1-kl]phenothiazine-4-sulfonamide have shown good anticancer activity against MCF-7 and HeLa cell lines. The remaining compounds have shown poor activity against tested cancer cell lines.
PubDate: 2023-11-01
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- Synthesis of Indole-1,3,4-Oxadiazole Based Sulfonyl 1,2,3-Triazoles as
Potent Anticancer and EGFR Inhibitors-
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Abstract: Herein, we synthesized some new indole-1,3,4-oxadiazole based sulfonyl 1,2,3-triazoles via a click chemistry approach and then characterized their structures by NMR, mass, and CHN analysis techniques. Later, the anticancer activity of the synthesized compounds was screened in vitro against different human cancer cell lines like MCF-7 and A-549, and the results were compared with the standard drug erlotinib. Most of the investigated compounds were found to be active against both cancer cell lines, MCF-7, and A-459. Specifically, compounds 2-(((1-(4-chloro-3,5-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-5-(1-methyl-1H-indol-3-yl)-1,3,4-oxadiazole and 2-(((1-(3,5-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methyl) sulfonyl)-5-(1-methyl-1H-indol-3-yl)-1,3,4-oxadiazole had superior activity against MCF-7, and remarkable activity against A-549. Similarly, the compound 2-(((1-(3,5-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-5-(1-methyl-1H-indol-3-yl)-1,3,4-oxadiazole showed more potent activity against EGFR and compound 2-(((1-(4-chloro-3,5-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-5-(1-methyl-1H-indol-3-yl)-1,3,4-oxadiazole showed equipotent activity against tyrosine kinase EGFR inhibitory activity.
PubDate: 2023-11-01
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- Biogenic Synthesis, Characterization, and Antifungal Activity of
Nanoparticles Against Candidiasis-
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Abstract: The green synthesis of nanoparticles is an expending research area due to the potential application for the development of novel techniques. The evaluation of multidrug resistance against various types of pathogenic microorganism should be encouraging the search for effective antimicrobial agents, from alternative diverse sources of biogenic nanoparticles. The results obtained in this study suggest that plant has potent anti-inflammatory, antimicrobial, antidiabetics, antidepressant, antioxidant and also responsible for the production of nanoparticles. In this study the green synthesis of iron oxide nanoparticles was carried out using peels extract of Punica granatum as a reducing agent and their anti-candidiasis activity for oral diseases. Capping and reducing of synthesized nanoparticles was found with medicinally important molecules present in the peels aqueous extract of this plant and these molecules could enhanced their value for various application. The presence of various phytochemicals viz. alkaloids glycosides, carbohydrates, steroids, phytosterol, flavonoids, protein and amino acid, phenol and tannins, and saponins were investigated by following standard biochemical method and further characterization of synthesized iron oxide nanoparticles was done by using UV-visible spectroscopy, X-ray Diffraction patterns (XRD), Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM). The anti-candidiasis activity of these nanoparticles was studied against Candida albicans and Candida tropicalis. SEM and TEM analysis of nanoparticles shows most of the shape are particles spherical in shape and average of particles size was found to be very in the range of 40–100 nm respectively. TEM and SEM micrograph obtained by using this technique revealed that generation of aggregated poly and mono dispersed in nature of nanoparticles. The peels aqueous extract of Punica granatum quickly reduced particles and enhances synthesis of iron oxide nanoparticles with highly antimicrobial activity.
PubDate: 2023-11-01
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- Design, In Silico Studies, Synthesis, Characterization, and Biological
Activities of Novel Substituted Oxazole Derivatives-
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Abstract: A powerful analgesic and anti-inflammatory agent were established by preparing a series of new heterocyclic substituted oxazole analogs. The chemical structures of the entire prepared analogs were confirmed by spectroscopic and elemental analyses. Molecular properties, ADME properties, and drug-likeness scores and toxicities of title compounds were predicted using in silico studies. In addition, title compounds were docked against two proteins namely, 3KK6, and 3LN1 using Auto Dock 4.2. In vitro analgesic and anti-inflammatory activities of prepared analogs were estimated using tail flick method and carrageenan-induced foot paw edema technique, respectively. Additionally, ulcerogenicity of potent analogs was also determined. Most of the prepared analogs showed mild-to-good analgesic and anti-inflammatory with low-to-reasonable ulcer index. Among the tested series, the most potent compound was found to be 1-(3-chlorophenyl)-3-methyl-4-(2-(4-((2-methyl-5-oxooxazol-4(5H)-ylidene) methyl)phenyl) hydrazono)-1H-pyrazol-5(4H)-one (OHPA3).
PubDate: 2023-11-01
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- Chemical Composition of Human and Mammalian Milk (A Review)
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Abstract: This review describes the chemical composition and properties of milk, as well as its importance for the development of the child and the formation of its individual organs and systems. The composition of colostrum and mature milk is considered in depth. Detailed data on the individual components of milk, such as proteins, fats, carbohydrates, minerals, vitamins, and enzymes, is presented. Chemical composition of human and mammalian milk is compared. Characteristics of biologically active compounds, such as hormones and protective factors of milk, are given. While human milk contains a large number of different components (>400), the ratio of which varies depending on the needs of each individual breastfed child, the composition of milk formulas of the most advanced developments includes only 40–50 of these components.
PubDate: 2023-11-01
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- Synthesis of 5-Halo-2ʹ-Azido Derivatives of Cytidine and
N-Hydroxycytidine and Evaluation of Their Antiviral Activity on a Panel of
RNA Viruses, Including SARS-CoV-2-
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Abstract: Coronavirus disease 2019 (COVID-19) is a new global pandemic with high morbidity and mortality caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). N-Hydroxycytidine derivatives show promise for combating COVID-19 and other viral diseases; in particular, molnupiravir has recently been approved for emergency prophylaxis in the early stages after infection with SARS-CoV-2. In the present work, a scheme for the synthesis of 5-halo-2ʹ-azido-substituted cytidine and N-hydroxycytidine derivatives was proposed. The synthesized compounds were tested against a panel of six RNA viruses, including SARS-CoV-2, enteroviruses, CHIKV, and HIV-1. A number of compounds showed ability to inhibit the reproduction of SARS-CoV-2 and CHIKV viruses in the micromolar range without noticeable cytotoxicity. The structures of the leader compounds can be used as a starting point for further design of antiviral agents.
PubDate: 2023-11-01
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- Synthesis and Characterization of Substituted
5-(2-Chloroquinolin-3-yl)-1,3,4-oxadiazole-2-amines: Computational, In
Silico ADME, Molecular Docking, and Biological Activities-
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Abstract: A series of 5-(2-chloroquinolin-3-yl)-1,3,4-oxadiazole-2-amine (IIIa–IIIj) with different biological activities were designed and synthesized through the cyclization of semicarbazone. All the newly synthesized compounds were characterized by elemental analysis, 1H NMR, 13C NMR, FT-IR, and mass spectrometry. All the newly synthesized final compounds (IIIa–IIIj) were screened for in vitro antimicrobial activity by diffusion into agar wells using Gentamicin as the antibacterial agent and Fluconazole as the antifungal control. In addition, selected compounds were screened for antitubercular activity using Microplate Alamar Blue Assay (MABA). All the compounds were evaluated computationally for drug similarity using various pharmacokinetic studies and ADME-T characterization, then tested in vitro against Gram+ bacteria (Staphylococcus aureus and Bacillus subtilis), Gram– bacteria (S. typhi and P. aeruginosa), fungi (Aspergillus niger and Fusarium), as well as the Mycobacterium tuberculosis H37Rv strain, provided important information about activity against these strains. In the current study, we have discussed the method for the synthesis of 1,3,4-oxadiazole derivatives and summarized the role of compounds (IIIa), (IIIb), (IIId), (IIIg), (IIIh), and (IIIi) as potential antibacterial and antitubercular agents. We put forward further in vivo evaluation and biological activity evaluation for their use against these pathogens.
PubDate: 2023-11-01
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- In Silico Docking Studies, Synthesis, Characterization, and Antimicrobial
Antimycobacterial Activity of Coumarinyl Oxadiazoles from Fatty Acids-
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Abstract: This present study deals with the design and evaluation of novel coumarinyl oxadiazoles substituted fatty acids derivatives using synthetic approach and to screen for in vitro antimicrobial activity. A recent literature survey revealed that, coumarinyl oxadiazoles substituted fatty acids derivatives shown for their ability to improve biological activities The condensation of 2-oxo-2H-chromene-3-carbohydrazide with substituted fatty acids in the presence of phosphorus oxychloride yielded a variety of novel 5-N-alkyl-1,3,4-oxadiazole-2H-chromen-2-one derivatives. The structure of the newly synthesized compounds was validated by elemental analysis, IR, 1H NMR, and mass spectrum data. Further, analysis of the drug-likeness property is predicted through five parameters like Lipinski rule, Ghose, Egan, Vebers, and Muegge rules. As molcular docking is normally used for understanding drug-receptor interaction. The above-derived compounds were subjected to molcular docking studies (4MFI, 5E2C, 6FBV, and 6NNE). The antibacterial and anti-mycobacterial properties of these substances were investigated. Compounds 3-(5-dodecyl-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one and 3-(5-hexadecyl-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one demonstrated considerable antibacterial activity against several tested bacterial strains in antimicrobial tests. In comparison to standard, compound 3-(5-(heptadec-8-en-1-yl)-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one demonstrated excellent antitubercular action. This hypothesis provides a possible explanation of the enhanced biological activity of the derived compounds.
PubDate: 2023-11-01
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- Effect of the Synthetic Peptide LKEKK on Psoriasis
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Abstract: It has been established that the synthetic peptide LKEKK affects the ability of IL-12 to control the secretory activity of keratinocytes isolated from psoriatic human skin: in the concentration range of 100–1000 nM, it enhanced in a dose-dependent manner IL-12-induced production of IL-10 and IFN-γ and inhibition of IL-17 secretion in vitro. The peptide with the inverted KKEKL sequence was inactive, indicating a high specificity of the action of the LKEKK peptide. The in vivo study of the activity of the LKEKK peptide in a mouse model of imiquimod-induced psoriasis showed that the daily application of 150–500 μg of the peptide together with Aldara cream containing 5% imiquimod on the ear for 6 days significantly suppressed the development of the inflammatory process. Thus, the LKEKK peptide is suitable as a basis for the development of drugs for treatment of psoriasis and other inflammatory skin diseases.
PubDate: 2023-11-01
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- Development of Mutant Forms of Neuroglobin with Substitutions in the
Interaction Surface with Cytochrome c-
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Abstract: Mutant forms of human neuroglobin that carry targeted mutations in the putative interface with cytochrome c: single (E60K, K67E, E87K, K95E) and double (E60K\E87K) substitutions were obtained by site-directed mutagenesis. The E60K, K95E, and E60K\E87K mutations cause slight changes in the UV-vis absorption spectra, which can be associated with both a change in the electrostatic field near the heme and a change in the heme iron spin to the high-spin state. The secondary structure of mutant neuroglobins calculated from the CD spectral data almost did not differ from the secondary structure of wild-type neuroglobin, except for the protein with the K67E substitution, whose β-turn is reorganized into an α-helix. The IR spectra provide further evidence for the predominance of α-helices in protein secondary structure for mutant forms of neuroglobin. Thus, the introduction of these mutations did not have a significant effect on the characteristics of the heme-containing protein neuroglobin. The developed mutant forms will be used to study the contribution of individual amino acid residues to the formation of the reaction complex between neuroglobin and cytochrome c, which will allow rational design of drugs for the therapy of various diseases associated with neuronal death in the future.
PubDate: 2023-11-01
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- Synthesis, Characterization, Antimicrobial, and Molecular Docking Studies
of Thiazolidin-4-one Derivatives fused with Indole and Pyrimidine Moieties
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Abstract: A series of fifteen 2-substituted-3-(4-(pyridin-2-yl)-6-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-2-yl)thiazolidin-4-one, was prepared and characterized using analytical techniques like FT-IR, NMR (1H and 13C), and mass spectrophotometry. On screening, the compounds for antibacterial and antifungal potential, the findings portrayed to be the potent inhibitor of bacterial and fungal strains. The cytotoxicity of the prepared molecules was checked against HepG2 cells to calculate the percent viable cells, which was observed to be in the range of 70–81% up to 100 µM. The molecular docking assay was performed to assess the binding modes, the extent of the H-bond, and binding affinities against the receptor glucosamine-6-phosphatase (GlcN-6P) and lanosterol 14-α-demethylase. The findings portrayed that TYR312, SER316, GLU396, LEU 448, SER303, GLY398, and SER401 were the only amino acids of GlcN-6P that formed the H-bond with the prepared molecules. Similarly, the residues GLC5, GLC6, GLC7, SER60, TYR63, THR104, ASP229, LEU230, SER249, SER251, THR485 were the only amino acids of lanosterol 14-α-demethylase) that formed H-bond with the prepared molecules. The binding affinities for both receptors were found to be in the range of –8.5 to –6.3 kcal/mole (GlcN-6P), and –8.4 to –6.8 kcal/mole (lanosterol 14-α-demethylase).
PubDate: 2023-11-01
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- Bacterial Adaptation Mechanisms to Stress Conditions with Small Non-Coding
RNAs Participation (A Review)-
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Abstract: Despite the fact that most of the bacterial genome encodes certain protein molecules, with the development of transcriptomic technologies, many genes have been discovered that transcribe RNA which is not translated into proteins. Such RNAs are called non-coding RNAs (ncRNAs). The study of only a small number of them shows that ncRNAs often act as regulatory molecules in various cellular processes: maintenance of cell wall homeostasis, protection against pathogens, virulence, etc. A special place among them is occupied by the so-called small ncRNAs with a length of ~50–300 nucleotide residues. In most cases, they form duplexes with the mRNA of certain genes, which affects the expression of the latter, however, some ncRNAs are able to directly bind to the target protein. Similar mechanisms of action of small ncRNAs give them some advantages in regulating various cellular processes compared to protein regulatory molecules. For example, when responding to an external or internal signal through small ncRNAs, the cell will need to spend less time and resources due to the absence of the translation stage. Moreover, some ncRNAs have no complete complementarity to their target RNAs, which makes the regulation more flexible, as it allows ncRNAs to participate in the response simultaneously to various cellular signals. In this review, we considered the general mechanisms by which various small ncRNAs allow bacteria to adapt to certain stressful conditions, as well as specific examples of their action in various prokaryotic organisms.
PubDate: 2023-11-01
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- Synthesis, Bioactivity Evaluation, and Cell Imaging of Isorhamine
Zwitterionic Polymers-
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Abstract: Using the four hydroxyl reaction points of isorhamnetin to introduce zwitterionic groups, five kinds of acid ionic polymer derivatives were prepared. Their ultraviolet spectrum (UV) and fluorescence spectra (PL) were 332 and 405 nm, respectively, in different solvents. In order to observe the dynamic self-assembly effect of the amphiphilic polymer drugs more directly, it was found that the amphiphilic polymer drugs aggregated together in a circular or elliptical shape under a transmission electron microscope (TEM), and was wrapped with isorhamnetin. In terms of biocompatibility, imaging experiments were performed using HeLa cells at different densities of 200 and 400 to observe the targeting changes. In MTT assay, isorhamnetin poly(carboxybetaine methacrylate)-1 (I) and isorhamnetin poly(carboxybetaine methacrylate)-2 (II) were particularly significant, and their activities in HCT-116 and HeLa were (53.27 ± 1.17, 68.51 ± 4.55), and (55.11 ± 5.87, 67.62 ± 6.28), respectively. Finally, in the cell electron microscope environment, it can be intuitively found that isorhamnetin amphoteric polymer drugs can directly enter both the targeted liposomes of HeLa cells and even enter the nucleus.
PubDate: 2023-11-01
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