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PLoS One. 2012;7(12):e51138. doi: 10.1371/journal.pone.0051138. Epub 2012 Dec 10.

Cryptopleurine analogs with modification of e ring exhibit different mechanism to rac-cryptopleurine and tylophorine.

Author information

1
Department of Pharmacology, Yale University School of Medicine, New Haven, CT, USA.

Abstract

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.

PMID:
23251437
PMCID:
PMC3519526
DOI:
10.1371/journal.pone.0051138
[Indexed for MEDLINE]
Free PMC Article

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