Cytotoxic Activity of the New Molecular Complex DHMEQ and Ammonium Glycyrrhizinate
- Authors
-
-
Sh.R. Kzyrgalin
Department of Oncology and Clinical Morphology, Bashkir State Medical University, Ufa, Russian Federation and Institute of Fundamental Medicine and Biology, Kazan (Volga Region) Federal University, Kazan, Russian Federation -
R.S. Yamidanov
Department of Oncology and Clinical Morphology, Bashkir State Medical University, Ufa, Russian Federation -
A.A. Rizvanov
Institute of Fundamental Medicine and Biology, Kazan (Volga Region) Federal University, Kazan, Russian Federation and Division of Medical and Biological Sciences, Tatarstan Academy of Sciences, Kazan, Russian Federation -
Sh.Kh. Gantsev
Department of Oncology and Clinical Morphology, Bashkir State Medical University, Ufa, Russian Federation and Division of Medical Sciences and Healthcare, Academy of Sciences of the Republic of Bashkortostan, Ufa, Russian Federation
-
- Keywords:
- Cytotoxicity, NF-κB inhibition, DHMEQ, ammonium glycyrrhizinate, molecular complex, transcription factor, in vitro, drug development
- Abstract
-
Objective: This study aimed to investigate the cytotoxic activity of a new molecular complex consisting of DHMEQ and ammonium glycyrrhizinate, as well as its effect on the transcription factor NF-κB. Cytotoxicity was assessed using the PrestoBlue® viability assay in HEK293, A-549, and MCF-7 cell lines. NF-κB inhibition was evaluated via a luciferase reporter assay in HEK293 cells. The complex was prepared at a 1:4 molar ratio (DHMEQ:ammonium glycyrrhizinate), and its structure was confirmed using spectroscopic methods and electron microscopy. Statistical analysis was performed using one-way ANOVA followed by Dunnett’s post hoc test.
Results: DHMEQ demonstrated high cytotoxic activity (IC50 = 13.82 ± 3.71 µM in HEK293 cells). The DHMEQ/ammonium glycyrrhizinate complex maintained comparable activity (IC50 = 10.39 ± 1.84 µM for HEK293) but showed reduced efficacy against A-549 and MCF-7 tumor cells. DHMEQ strongly inhibited NF-κB activity (IC50 = 0.83 ± 0.51 µM), while the complex required significantly higher concentrations (IC50 = 21.79 ± 6.24 µM) to achieve a similar inhibitory effect.
Conclusion: The DHMEQ–ammonium glycyrrhizinate complex preserved the main biological properties of DHMEQ while improving its solubility and stability. This approach shows potential for developing DHMEQ-based drug formulations targeting NF-κB, but further optimization and in vivo validation are required before clinical application.
- Downloads
-
Download data is not yet available.
- References
-
[1] Chen W, Li Z, Bai Y, Zhao Y. Overcoming chemotherapy resistance via NF-κB inhibition: A comprehensive review of therapeutic approaches. Pharmacol Ther 2024; 253: 108577.
[2] Hayden MS, Ghosh S. NF-κB in immunology and inflammation. Cell Res 2008; 18(3): 221-233.
[3] Liu T, Zhang L, Joo D, Sun SC. NF-κB signaling in inflammation. Signal Transduct Target Ther 2017; 2: 17023.
[4] Xia Y, Shen S, Verma IM. NF-κB, an active player in human cancers. Cancer Immunol Res 2014; 2(9): 823-830.
[5] Kumar A, Takada Y, Boriek AM, Aggarwal BB. The role of NF-κB in the tumor microenvironment: A comprehensive review. Front Immunol 2023; 14: 1142935.
[6] Karin M. NF-κB as a critical link between inflammation and cancer. Cold Spring Harb Perspect Biol 2009; 1(5): a000141.
[7] Umezawa K. Recent developments of NF-κB inhibitors for cancer therapy. Expert Opin Ther Targets 2012; 16(6): 635-645.
[8] Ishikawa H, Umezawa K. Inhibition of NF-κB by dehydroxymethylepoxyquinomicin suppresses osteoclastogenesis and collagen-induced arthritis. Arthritis Res Ther 2009; 11(1): R59.
[9] Zhang Q, Liu Y, Wang Y, et al. Novel nanocarriers for targeted delivery of NF-κB inhibitors in cancer therapy. J Control Release 2021; 330: 725-735.
[10] Kimura Y, Sumiyoshi M. Antitumor and antimetastatic actions of glycyrrhizinate and glycyrrhetinic acid derivatives in experimental tumor systems. Phytomedicine 2011; 18(9): 704-711.
[11] Yamamoto M, Sugimoto K. Development of novel DHMEQ-based complexes to improve drug stability and efficacy. Oncol Res 2020; 28(3): 187-195.
[12] Nakshatri H, Appaiah HN, Anjanappa M, et al. NF-κB-dependent and -independent epigenetic modulation using the novel anti-cancer agent DHMEQ. PLoS One 2021; 16(4): e0250649.
[13] Singh S, Singh AP, Sharma B, et al. NF-κB signaling and resistance to chemotherapy in breast cancer: A comprehensive review. Semin Cancer Biol 2023; 88: 13-28.
[14] Pastorino G, Cornara L, Soares S, Rodrigues F, Oliveira MBPP. Glycyrrhizic acid and its derivatives as potential anticancer agents: A comprehensive review. Pharmacol Res 2023; 188: 106663.
[15] Yadav P, Rastogi V, Verma A. Molecular complexes as a promising strategy for enhancing the bioavailability of poorly soluble drugs. Int J Pharm 2022; 615: 121502.
[16] Wang Y, Li S, Zhang X, et al. Ligand-modified nanoparticles for targeted NF-κB inhibition in cancer therapy: Recent advances and perspectives. Adv Drug Deliv Rev 2023; 192: 114642.
[17] Yamamoto Y, Klein G, Zetterström O. The combination approach of DHMEQ with adjuvants for targeting resistant cancers. Int J Cancer 2020; 147(12): 3365-3374.
[18] Garcia-Aranda M, Redondo M. Immunotherapy and NF-κB inhibition: A promising combination. Cancer Lett 2023; 558: 216106.
[19] Gupta A, Kumar S, Tripathi AK, et al. In vivo models for evaluation of antitumor activity of NF-κB inhibitors: Current status and future directions. Eur J Pharmacol 2022; 917: 174757.
- Downloads
- Published
- 16-09-2025
- Issue
- Vol. 14 (2025)
- Section
- Articles
- License
-

This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
How to Cite
Similar Articles
- Teoh Han Pinn, Siti Fathiah Masre, Nadiah Abu, MiR-130b-3p Suppress the Migration, Proliferation and Chemosensitization of Hepatocellular Carcinoma Cells , Journal of Cancer Research Updates: Vol. 13 (2024)
- R. Hsieh, M.L. Prasad, M.M.S. Nico, H. Tavares, A. Altemani, R.S.S. Macarenco, S.V. Lourenço, A Study of C-MYC, SOX10 and BCL-2 Proteins Expression in Head and Neck Mucosal Melanomas , Journal of Cancer Research Updates: Vol. 5 No. 4 (2016)
- Sung-Han Hsiao, Shi-Yu Luo, Ching-Ya Su, Wei-Cherng Tuo, Cheng-Ting Chiang, Yan-Qing Li, Yang-Hui Huang, Chung-Pu Wu, The Overexpression of ABCG2 Reduces the Efficacy of Volasertib (BI 6727) and GSK641364 in Human S1-M1-80 Colon Carcinoma Cells , Journal of Cancer Research Updates: Vol. 3 No. 2 (2014)
- Janet Wangari-Talbot, Elizabeth Hopper-Borge, Drug Resistance Mechanisms in Non-Small Cell Lung Carcinoma , Journal of Cancer Research Updates: Vol. 2 No. 4 (2013)
- Ali Muafaq Said, Ayat Ali Salih, Mohammed Abdulridha Obid, Azal Hamoody Jumaa, Youssef Shakuri Yasin, A Repurposed Duo: Empagliflozin-Metformin Triggers a Metabolic Crisis in Cervical Cancer by Disrupting the Acyl-CoA/CoA Ratio via Dual Inhibition of PPAT and CPT1A , Journal of Cancer Research Updates: Vol. 14 (2025)
- Yang-Hui Huang, Sung-Han Hsiao, Chung-Pu Wu, Isoreserpine Reverses Multidrug Resistance Mediated by ABCB1 , Journal of Cancer Research Updates: Vol. 4 No. 4 (2015)
- Jamison Wijaya, Indrayadi Gunardi, Julvyn Julvyn, Christopher Lim, Benny Nicolas Johannis, Firstine Kelsi Hartanto, Adrianus Rajasa, Rahmi Amtha, Elizabeth Fitriana Sari, Selecting the Appropriate Oral Cancer Cell Line: Characteristic-Based Recommendations from a Systematic Review , Journal of Cancer Research Updates: Vol. 14 (2025)
- A. Lyberopoulou, E.P. Efstathopoulos, M. Gazouli, Nanodiagnostic and Nanotherapeutic Molecular Platforms for Cancer Management , Journal of Cancer Research Updates: Vol. 4 No. 4 (2015)
- Ricardo Hsieh, The Role of BRAF Gene in Cancer: Literature Review and Future Directions , Journal of Cancer Research Updates: Vol. 9 No. 1 (2020)
- G.R. Nivashini, Lalatendu Moharana, Ashish Jawarkar, Komal Parashar, Tarun Parashar, Dinesh Kumar Yadav, Targeting Inflammatory Pathways in Cancer: Novel Insights into Tumorigenesis and Personalized Therapeutic Approaches , Journal of Cancer Research Updates: Vol. 15 No. 1 (2026)
You may also start an advanced similarity search for this article.
Most read articles by the same author(s)
- Sh.R. Kzyrgalin, K.Sh. Gantsev, A.A. Rizvanov, Sh.Kh. Gantsev, New Insight of Oncology: Cancer Concept without Tumor , Journal of Cancer Research Updates: Vol. 13 (2024)
- Sh.R. Kzyrgalin, R.S. Yamidanov, A.A. Rizvanov, Sh.Kh. Gantsev, Antitumor Activity of Dehydroxymethylepoxyquinomicin (DHMEQ) in Monotherapy and Combination with Cisplatin in the SKOV-3 Ovarian Cancer Model , Journal of Cancer Research Updates: Vol. 13 (2024)
- A.E. Anichkova, Sh.R. Kzyrgalin, R.Sh. Khasanov, Sh.Kh. Gantsev, Factors Associated with Breast Cancer Risk in Women: A Literature Review , Journal of Cancer Research Updates: Vol. 15 No. 1 (2026)
