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Anti-cancer, Anti-inflammatory, and Antioxidation Active Substances 2.0

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Biochemistry".

Deadline for manuscript submissions: 31 December 2024 | Viewed by 1599

Special Issue Editor

Special Issue Information

Dear Colleagues,

More and more anti-cancer and anti-inflammatory active substances are being discovered and applied in cancer and inflammation treatment, and focus on the basic research on antiviral and antibacterial, also playing an important role in the molecular activity and biotechnology innovation of food and cosmetics.

In this Special Issue, we are collecting papers regarding the role and molecular mechanisms of active substances in anti-inflammation and anti-cancer treatment, food and cosmetics. We welcome research articles and review papers focused on anti-cancer and anti-inflammatory active substances in cancer, from basic, translational science studies to clinical research.

This Special Issue is supervised by Dr. Ming-Ju Hsieh and assisted by our Topical Advisory Panel Member, Dr. Sourav Ghorai (University of Illinois at Chicago).

Dr. Ming-Ju Hsieh
Guest Editor

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

  • anti-inflammatory
  • anti-cancer
  • antioxidants
  • antiproliferative
  • antiviral
  • antibacterial
  • antibodies
  • molecular mechanism
  • chemoresistance
  • molecular biology

Published Papers (2 papers)

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Research

16 pages, 3290 KiB  
Article
Synthesis, Pharmacokinetic Profile, Anticancer Activity and Toxicity of the New Amides of Betulonic Acid—In Silico and In Vitro Study
by Ewa Bębenek, Zuzanna Rzepka, Justyna Magdalena Hermanowicz, Elwira Chrobak, Arkadiusz Surażyński, Artur Beberok and Dorota Wrześniok
Int. J. Mol. Sci. 2024, 25(8), 4517; https://doi.org/10.3390/ijms25084517 - 20 Apr 2024
Viewed by 385
Abstract
Betulonic acid (B(O)A) is a pentacyclic lupane-type triterpenoid that widely exists in plants. There are scientific reports indicating anticancer activity of B(O)A, as well as the amides and esters of this triterpenoid. In the first step of the study, the synthesis of novel [...] Read more.
Betulonic acid (B(O)A) is a pentacyclic lupane-type triterpenoid that widely exists in plants. There are scientific reports indicating anticancer activity of B(O)A, as well as the amides and esters of this triterpenoid. In the first step of the study, the synthesis of novel amide derivatives of B(O)A containing an acetylenic moiety was developed. Subsequently, the medium-soluble compounds (EB171 and EB173) and the parent compound, i.e., B(O)A, were investigated for potential cytotoxic activity against breast cancer (MCF-7 and MDA-MB-231) and melanoma (C32, COLO 829 and A375) cell lines, as well as normal human fibroblasts. Screening analysis using the WST-1 test was applied. Moreover, the lipophilicity and ADME parameters of the obtained derivatives were determined using experimental and in silico methods. The toxicity assay using zebrafish embryos and larvae was also performed. The study showed that the compound EB171 exhibited a significant cytotoxic effect on cancer cell lines: MCF-7, A-375 and COLO 829, while it did not affect the survival of normal cells. Moreover, studies on embryos and larvae showed no toxicity of EB171 in an animal model. Compared to EB171, the compound EB173 had a weaker effect on all tested cancer cell lines and produced less desirable effects against normal cells. The results of the WST-1 assay obtained for B(O)A revealed its strong cytotoxic activity on the examined cancer cell lines, but also on normal cells. In conclusion, this article describes new derivatives of betulonic acid—from synthesis to biological properties. The results allowed to indicate a promising direction for the functionalization of B(O)A to obtain derivatives with selective anticancer activity and low toxicity. Full article
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26 pages, 4121 KiB  
Article
Study on the Anti-Ulcerative Colitis Effect of Pseudo-Ginsenoside RT4 Based on Gut Microbiota, Pharmacokinetics, and Tissue Distribution
by Hui Yu, Caixia Wang, Junzhe Wu, Qianyun Wang, Hanlin Liu, Zhuoqiao Li, Shanmei He, Cuizhu Wang and Jinping Liu
Int. J. Mol. Sci. 2024, 25(2), 835; https://doi.org/10.3390/ijms25020835 - 9 Jan 2024
Viewed by 846
Abstract
The purpose of this study was to explore the therapeutic effect of the oral administration of pseudo-ginsenoside RT4 (RT4) on ulcerative colitis (UC), and to determine the rate of absorption and distribution of RT4 in mice with UC. Balb/c mice were induced using [...] Read more.
The purpose of this study was to explore the therapeutic effect of the oral administration of pseudo-ginsenoside RT4 (RT4) on ulcerative colitis (UC), and to determine the rate of absorption and distribution of RT4 in mice with UC. Balb/c mice were induced using dextran sulfate sodium salts (DSS) to establish the UC model, and 10, 20, or 40 mg/kg of RT4 was subsequently administered via gavage. The clinical symptoms, inflammatory response, intestinal barrier, content of total short-chain fatty acids (SCFAs), and gut microbiota were investigated. Caco-2 cells were induced to establish the epithelial barrier damage model using LPS, and an intervention was performed using 4, 8, and 16 µg/mL of RT4. The inflammatory factors, transient electrical resistance (TEER), and tight-junction protein expression were determined. Finally, pharmacokinetic and tissue distribution studies following the intragastric administration of RT4 in UC mice were performed. According to the results in mice, RT4 decreased the disease activity index (DAI) score, restored the colon length, reduced the levels of pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β), and boosted the levels of immunosuppressive cytokine IL-10, increased the content of SCFAs, improved the colonic histopathology, maintained the ultrastructure of colonic mucosal epithelial cells, and corrected disturbances in the intestinal microbiota. Based on the results in caco-2 cells, RT4 reduced the levels of TNF-α, IL-6, and IL-1β; protected integrity of monolayers; and increased tight-junction protein expression. Additionally, the main pharmacokinetic parameters (Cmax, Tmax, t1/2, Vd, CL, AUC) were obtained, the absolute bioavailability was calculated as 18.90% ± 2.70%, and the main distribution tissues were the small intestine and colon. In conclusion, RT4, with the features of slow elimination and directional distribution, could alleviate UC by inhibiting inflammatory factors, repairing the intestinal mucosal barrier, boosting the dominant intestinal microflora, and modulating the expression of SCFAs. Full article
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Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Planned Paper I: Griffithazanone A promotes apoptosis and reverses Osimertinib resistant in NSCLC by targeting PIM1- Dr. Xiao(Submission date To be determined)

Planned Paper II: Picrasidine I induced apoptosis by triggering claspin in melanoma cells- Professor. Ming-Ju Hsieh(Submission date To be determined)
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