Journal Article DKFZ-2024-02539

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Antimicrobial activity and cytotoxic and epigenetic effects of tannic acid-loaded chitosan nanoparticles.

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2024
Macmillan Publishers Limited, part of Springer Nature [London]

Scientific reports 14(1), 30405 () [10.1038/s41598-024-80771-x]
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Abstract: Tannic acid (TA) is a potent antitumor agent, but its low bioavailability and absorption limit its use. In this study, it was loaded into chitosan-based nanoparticles (Chi-NPs) to overcome these limitations and to improve its antimicrobial and anticancer activities. TA-loaded Chi-NPs (Chi-TA-NPs) were synthesized using the ionic gelation method and physicochemically characterized by FE-SEM, FTIR, XRD, PDI, DLS, and zeta potential analysis. Additionally, the antimicrobial activity of Chi-TA-NPs against two G+ bacterial strains, two G- bacterial strains, and a fungal strain (Candida albicans) was investigated using the microbroth dilution method. MTT assay was used to examine the cytotoxic effects of Chi-TA-NPs on HepG2 cells. The expression of DNA methyltransferase 1 (DNMT1), DNMT3A, and DNMT3B was examined in HepG2 cells using RT-qPCR. The amount of 5-methylcytosine in the HepG2 cell-derived genomic DNA was measured using ELISA. FE-SEM micrographs showed the loading of TA into the chitosan-based formulation. The peaks detected in the XRD and FTIR analyses confirmed the formation of the Chi-TA-NPs. The PDI value (0.247 ± 0.03), size (567.0 ± 25.84 nm), and zeta potential (17.0 ± 5.86 mV) confirmed the relative stability of Chi-TA-NPs. A constant release profile in line with the Korsmeyer-Peppas model was detected for Chi-TA-NPs, such that approximately 44% of TA was released after 300 min. In addition, Chi-TA-NPs exhibited effective antimicrobial activity against the studied microbial strains, as manifested by MIC values ranging from 250 to 1000 µg/mL. Chi-TA-NPs induced cytotoxicity in liver tumor cell line, with an IC50 value of 500 µg/mL. Furthermore, Chi-TA-NPs considerably decreased the expression of DNMT1 (2.52-fold; p = 0.01), DNMT3A (2.96-fold; p = 0.004), and DNMT3B (2.94-fold; p < 0.0001). However, 5-methylcytosine levels in HepG2 cells were unaffected by Chi-TA-NPs treatment (p = 0.62). Finally, the antimicrobial, cytotoxic, and epigenetic effects of Chi-TA-NPs were more pronounced than those of free TA and the unloaded Chi-NPs. In conclusion, Chi-TA-NPs exhibit promising potential for reducing microbial growth and promoting cytotoxicity in liver cancer cells.

Keyword(s): Chitosan: chemistry (MeSH) ; Chitosan: pharmacology (MeSH) ; Humans (MeSH) ; Tannins: chemistry (MeSH) ; Tannins: pharmacology (MeSH) ; Nanoparticles: chemistry (MeSH) ; Hep G2 Cells (MeSH) ; Anti-Infective Agents: pharmacology (MeSH) ; Anti-Infective Agents: chemistry (MeSH) ; Epigenesis, Genetic: drug effects (MeSH) ; Candida albicans: drug effects (MeSH) ; Microbial Sensitivity Tests (MeSH) ; Antineoplastic Agents: pharmacology (MeSH) ; Antineoplastic Agents: chemistry (MeSH) ; Polyphenols (MeSH) ; Antimicrobial effects ; Chitosan nanoparticles ; Cytotoxicity ; DNA methylation ; Tannic acid ; Chitosan ; Tannins ; Anti-Infective Agents ; Antineoplastic Agents ; tannic acid ; Polyphenols

Classification:

Contributing Institute(s):
  1. B070 Funktionelle Genomanalyse (B070)
Research Program(s):
  1. 312 - Funktionelle und strukturelle Genomforschung (POF4-312) (POF4-312)

Appears in the scientific report 2024
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 Record created 2024-12-06, last modified 2024-12-06



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