Tylophorine analogs exhibit a broad range of pharmacological activities, including anti-cancer, anti-inflammatory, anti-autoimmune, and anti-virus effects. Structure-activity relationship study of different structure tylophorine analogs can provide further understanding of their biological activity. Modifications on the E ring of the quinolizidine moiety of cryptopleurine analogs changed the potency and the selective inhibitory effect on NF-κB, AP-1, and CRE signaling pathways. Functional cryptopleurine analogs showed potent inhibition of NF-κB signaling pathway in both HepG2 and HEK-293 cell lines. The E ring structure analogs also differed in suppression of protein translation, and expression of cyclin D1. Our results showed that DCB-3503 or Rac-cryptopleurine could be a scaffold for modification to yield compounds with different mechanisms of action. © 2012 Wang et al.
CITATION STYLE
Wang, Y., Wong, H. C., Gullen, E. A., Lam, W., Yang, X., Shi, Q., … Cheng, Y. C. (2012). Cryptopleurine Analogs with Modification of E Ring Exhibit Different Mechanism to Rac-Cryptopleurine and Tylophorine. PLoS ONE, 7(12). https://doi.org/10.1371/journal.pone.0051138
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