Қазақ ұлттық қыздар педагогикалық университеті / Казахский национальный женский педагогический университет

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The Iodine–Dextrin–Lithium Complex: Morphology, Antibacterial Activity, and Cytotoxicity
(Multidisciplinary Digital Publishing Institute, 2025-12-18)
Daniil Shepilov
;
Seitzhan Turganbay
;
Ardak B. Jumagaziyeva
;
Tamara Bukeyeva
;
Dana A. Askarova
A new iodine-dextrin-lithium complex (IDLC) was synthesized and structurally characterized as a hybrid supramolecular system combining antiseptic, stabilizing, and biocompatible components. The compound integrates iodine as the primary antimicrobial agent, lithium as a coordination and stabilization element, and dextrin as a biodegradable polysaccharide matrix enabling sustained release. Physicochemical analyses confirmed the formation of a uniform, thermally stable complex. Biological evaluation revealed strong bactericidal activity, with minimum bactericidal concentrations (MBC) ranging from 1.95 to 15.63 µg ml-1 against both Gram-positive and Gram-negative pathogens, including multidrug-resistant Staphylococcus aureus and Acinetobacter baumannii. The complex also demonstrated inhibitory effects in virus-infected MDCK cell cultures. Cytotoxicity studies showed CC50 = 0.23-0.48 mg ml-1 on human MNCs and more than 10 mg ml-1 on MDCK cells, confirming low toxicity. The results of the study on the cytotoxicity of IDLC suggest a cytotoxic effect on tumor cell lines such as HepG2, HeLa, AGS, K562, and H9, as well as normal cell lines MeT-5A. Therefore, it can be estimated that IDLC has the potential to be a new drug with antitumor activity against these cell lines. The research confirms that iodine can be effectively stabilized within a dextrin-lithium framework to yield a biologically active, thermally resistant complex, suitable for pharmaceutical use.
Цитирования (OpenAlex) 3
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Iodine-Based Coordination Compounds: A Strategy Toward Antibiotic Potentiation
(Multidisciplinary Digital Publishing Institute, 2026-05-12)
Daniil Shepilov
;
Dana A. Askarova
;
Anar Seisembekova
;
Seitzhan Turganbay
;
Ardak B. Jumagaziyeva
Due to the increasing threat of antibiotic resistance and the emergence of new pathogenic strains, the development of effective combined therapeutic agents represents a crucial direction in the fight against infections. Within this study, several compounds were synthesized in which iodine is present in a coordination complex with antibiotics—sodium sulfadimidine and gentamicin sulfate. The physicochemical parameters of these compounds were investigated using capillary electrophoresis and UV spectroscopy, along with their cytotoxicity, antimicrobial, and antiviral activities. As a result of this work, two stable compounds, KC-246 and KC-248, were synthesized, demonstrating virus-inhibitory activity against herpes simplex virus and influenza A under extremely low cytotoxicity levels of 0.018–0.106 mg/mL. Additionally, they exhibited antimicrobial activity against representatives of the families Staphylococcaceae, Pseudomonadaceae, Enterobacteriaceae, Enterococcaceae, and yeast-like fungi. The minimum bactericidal concentrations (MBCs) ranged from 0.794 µg/mL to 0.198 µg/mL (KC-246) and from 2.093 µg/mL to 0.523 µg/mL (KC-248).
Цитирования (OpenAlex) 2
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Quantum Chemical Insights into Antibiotic Structure-Activity Relationships and Mechanisms of Action: A Review
(Multidisciplinary Digital Publishing Institute, 2026-07-17)
Seitzhan Turganbay
;
Alexander Ilin
;
Aitugan Sabitov
;
Jingcheng Hao
;
Anar Seisembekova
This review examines recent quantum chemical methodologies applied to investigating antibiotic structure and mechanisms of action. The discussion is organised into three sections: (1) enzymatic hydrolysis of the β-lactam ring, (2) interactions of antibiotics with ribosomal subunits and enzyme active sites, and (3) complex formation with metal ions. Each section evaluates how quantum chemical approaches, particularly density functional theory (DFT) and hybrid QM/MM techniques, model molecular processes relevant to antibiotic function, including transition states, electron density analyses, and metal coordination effects on antibacterial activity. Selected studies demonstrate the utility of these methodologies in interpreting experimental data and predicting physicochemical and biological properties of novel compounds. Distinct from previous literature, this review provides a comparative and up-to-date synthesis of quantum chemical methods related to enzymatic mechanisms and metal-based antibiotic systems, emphasising experimental validation strategies and practical guidelines for method selection in antibiotic research. It also identifies areas where quantum chemical modelling can integrate with experimental pharmacology and structural biology to support the rational design of next-generation antimicrobial agents. The review concludes by advocating an interdisciplinary framework combining quantum chemistry, biochemistry, and pharmacology to address antibiotic resistance. The review focuses primarily on antibiotics targeting bacterial cell wall and protein synthesis, particularly β-lactam antibiotics, ribosome-targeting agents, and their interactions with metal ions. Computational methods discussed are mainly limited to DFT, ab initio, and hybrid QM/MM approaches. It does not cover membrane-disrupting antibiotics, antiviral or antifungal agents, machine learning-based prediction methods, or purely molecular dynamics approaches outside a quantum mechanical context.
Цитирования (OpenAlex) 1
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DEVELOPMENT, PHARMACEUTICAL EVALUATION, AND ASSESSMENT OF THE BACTERICIDAL ACTIVITY OF THE KC-250 TABLET FORMULATION AGAINST CLINICALLY SIGNIFICANT MICROORGANISMS
(2026-08-21)
Daniil Shepilov
;
Zhassur Taganov
;
Ardak B. Jumagaziyeva
;
Sabina T. Kenesheva
;
Saltanat Jumabayeva
Introduction: Conversion of iodine-containing complexes into solid dosage forms requires adequate tablet strength while preserving disintegration, release, and antimicrobial activity. This study aimed to develop a directly compressed KC-250 tablet formulation, evaluate its pharmaceutical quality, and determine its bactericidal activity against clinically significant bacteria. Methods: Tablets containing 60 mg of KC-250 at a target mass of 500 mg were prepared using MicroceLac® 100, povidone K30, and magnesium stearate. Compression forces of 3.24 and 6.96 kN were compared by friability and disintegration testing. The selected formulation was evaluated for pharmacopoeial quality attributes. Bactericidal activity against eight reference, resistant, and clinical bacterial strains was determined in triplicate by broth serial dilution followed by agar subculture. Results: Increasing compression force from 3.24 to 6.96 kN reduced friability from 0.81% to 0.21%, while disintegration increased from 1.62 to 4.62 min. Tablets produced at 6.96 kN had friability of 0.20%, a disintegration time of 4 min 54 s, a KC-250 content of 63.05 mg/tablet, and dissolution of 102.95% within 45 min. All evaluated attributes complied with the predefined acceptance criteria. Minimum bactericidal concentrations were 60 mg/mL for the tested Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa strains and 30 mg/mL for Enterococcus faecalis and Enterococcus faecium. Discussion: Compression at 6.96 kN provided the most appropriate balance between mechanical resistance and rapid disintegration without restricting KC-250 release. The retained bactericidal activity indicates that tablet formulation did not eliminate the antimicrobial function of KC-250 and supports further development of the selected MicroceLac® 100– povidone K30 matrix.
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D/PVA/I-1 as an Antibiotic Adjuvant: In Vitro Synergy and Membrane Permeabilization in MDR Bacteria
(Multidisciplinary Digital Publishing Institute, 2026-08-17)
Ardak B. Jumagaziyeva
;
Seitzhan Turganbay
;
Anar Seisembekova
;
Daniil Shepilov
;
Zhanar A. Iskakbayeva
Background: Antimicrobial resistance (AMR) is among the most pressing challenges in modern infectious medicine, driving progressive failure of standard antibacterial therapy and rising mortality from infections caused by multidrug-resistant (MDR) pathogens. Antibiotic potentiation through adjuvant compounds capable of restoring the activity of existing drugs represents a promising strategy to overcome resistance without developing fundamentally new antibacterial molecules. This study aimed to evaluate the antibiotic-potentiating activity of a dextrin/polyvinyl alcohol/iodine complex (D/PVA/I-1), developed at the Scientific Center for Anti-Infectious Drugs JSC (Almaty, Kazakhstan), against clinically relevant MDR reference strains. Methods: Nine reference strains, Staphylococcus aureus (ATCC 33591, BAA-39), Escherichia coli (ATCC BAA-196, BAA-2523), Klebsiella pneumoniae (ATCC BAA-2524, 700603), Acinetobacter baumannii (ATCC BAA-1790), Streptococcus pneumoniae (ATCC BAA-660), and Haemophilus influenzae (ATCC 33930), and two clinical isolates, P. aeruginosa SCAID PHRX1-2019 and E. coli SCAID WND1-2021, were tested. Antibiotic-potentiating activity was assessed by checkerboard assay with calculation of the fractional inhibitory concentration index (FICI); bactericidal kinetics were evaluated by time-kill analysis. The effect of D/PVA/I-1 on cytoplasmic membrane permeability was investigated using a crystal violet uptake assay. Results: Of 45 D/PVA/I-1–antibiotic combinations tested across nine antibiotics, synergy (FICI ≤ 0.5) was demonstrated in 44.4% of cases, partial synergy in 48.9%, and additive effects in 6.7%; no antagonistic interactions were detected. The most pronounced potentiating effect occurred against Gram-positive pathogens, particularly MRSA strains (66.7% synergistic combinations). Time-kill analysis confirmed suppression of the regrowth phenotype characteristic of MDR strains under monotherapy and restoration of bactericidal activity against antibiotics to which strains exhibited intrinsic resistance. D/PVA/I-1 induced a dose- and time-dependent increase in membrane permeability in both Gram-positive and Gram-negative organisms. Conclusions: D/PVA/I-1 is an effective broad-spectrum antibiotic potentiator and represents a promising basis for combination therapy regimens against MDR infections.

Қазақ ұлттық қыздар педагогикалық университеті / Казахский национальный женский педагогический университет

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