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Open AccessArticle

1-Chromonyl-5-Imidazolylpentadienone Demonstrates Anti-Cancer Action against TNBC and Exhibits Synergism with Paclitaxel

1
Department of Pharmaceutical Sciences, Jefferson College of Pharmacy, Thomas Jefferson University, Philadelphia, PA 19107, USA
2
Department of Chemistry, California State University, Fresno, CA 95819, USA
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(16), 5777; https://doi.org/10.3390/ijms21165777
Received: 23 July 2020 / Revised: 5 August 2020 / Accepted: 6 August 2020 / Published: 12 August 2020
(This article belongs to the Special Issue Curcumin in Health and Disease: New Knowledge)
Curcumin has been well studied for its anti-oxidant, anti-inflammatory, and anti-cancer action. Its potential as a therapy is limited due to its low bioavailability and rapid metabolism. To overcome these challenges, investigators are developing curcumin analogs, nanoparticle formulations, and combining curcumin with other compounds or dietary components. In the present study, we used a 1-chromonyl-5-imidazolylpentadienone named KY-20-22 that contains both the pharmacophore of curcumin and 1,4 benzopyrone (chromone) moiety typical for flavonoids, and also included specific moieties to enhance the bioavailability. When we tested the in vitro effect of KY-20-22 in triple-negative breast cancer (TNBC) cell lines, we found that it decreased the cell survival and colony formation of MDA-MB-231 and MDA-MB-468 cells. An increase in mitochondrial reactive oxygen species was also observed in TNBC cells exposed to KY-20-22. Furthermore, KY-20-22 decreased epithelial–mesenchymal formation (EMT) as evidenced by the modulation of the EMT markers E-cadherin and N-cadherin. Based on the fact that KY-20-22 regulates interleukin-6, a cytokine involved in chemotherapy resistance, we combined it with paclitaxel and found that it synergistically induced anti-proliferative action in TNBC cells. The results from this study suggested that 1-chromonyl-5-imidazolylpentadienone KY-20-22 exhibited anti-cancer action in MDA-MB-231 and MDA-MB-468 cells. Future studies are required to evaluate the anti-cancer ability and bioavailability of KY-20-22 in the TNBC animal model. View Full-Text
Keywords: curcumin; triple-negative breast cancer; paclitaxel; IL-6 curcumin; triple-negative breast cancer; paclitaxel; IL-6
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MDPI and ACS Style

Modi, K.; Lawson, S.; Chen, G.; Tumuluri, D.; Rekhtman, I.; Kurtz, M.; Brailoiu, G.C.; Chen, Q.-H.; Lakshmikuttyamma, A. 1-Chromonyl-5-Imidazolylpentadienone Demonstrates Anti-Cancer Action against TNBC and Exhibits Synergism with Paclitaxel. Int. J. Mol. Sci. 2020, 21, 5777. https://doi.org/10.3390/ijms21165777

AMA Style

Modi K, Lawson S, Chen G, Tumuluri D, Rekhtman I, Kurtz M, Brailoiu GC, Chen Q-H, Lakshmikuttyamma A. 1-Chromonyl-5-Imidazolylpentadienone Demonstrates Anti-Cancer Action against TNBC and Exhibits Synergism with Paclitaxel. International Journal of Molecular Sciences. 2020; 21(16):5777. https://doi.org/10.3390/ijms21165777

Chicago/Turabian Style

Modi, Karan; Lawson, Scott; Chen, Guanglin; Tumuluri, Deepthi; Rekhtman, Inga; Kurtz, Michael; Brailoiu, G. C.; Chen, Qiao-Hong; Lakshmikuttyamma, Ashakumary. 2020. "1-Chromonyl-5-Imidazolylpentadienone Demonstrates Anti-Cancer Action against TNBC and Exhibits Synergism with Paclitaxel" Int. J. Mol. Sci. 21, no. 16: 5777. https://doi.org/10.3390/ijms21165777

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