Prenylated flavonoids from Ficus hirta induces HeLa cells apoptosis via MAPK and AKT signaling pathways.

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  • Additional Information
    • Source:
      Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE
    • Publication Information:
      Publication: Oxford : Elsevier Science Ltd
      Original Publication: Oxford ; New York : Pergamon Press, c1991-
    • Subject Terms:
      Antineoplastic Agents/*pharmacology ; Apoptosis/*drug effects ; Ficus/*chemistry ; Flavonoids/*pharmacology ; Proto-Oncogene Proteins c-akt/*antagonists & inhibitors; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Flavonoids/chemical synthesis ; Flavonoids/chemistry ; Humans ; MAP Kinase Signaling System/drug effects ; Molecular Structure ; Proto-Oncogene Proteins c-akt/metabolism ; Structure-Activity Relationship
    • Abstract:
      A pair of undescribed enantiomers, (±) ficusflavonid A (1a/1b), along with five known analogues, were isolated from the roots of Ficus hirta. Their structures were determined by the analysis of extensive spectroscopic data (including UV, IR, HRESIMS and NMR). Two enantiomers (1a and 1b) were successfully separated by chiral chromatographic column and their absolute configurations were assigned by the comparison of experimental and calculated ECD data. The cytotoxicity of all the isolates against HeLa, MCF-7, HepG2 and H460 cell lines were evaluated by MTT assay. Among them, 4 suppressed the proliferation of HeLa cells with the IC 50 value of 28.88 μM. Furthermore, the apoptotic effect of 4 on HeLa cells and the level of several crucial proteins in AKT/MAPKs signaling pathways were analyzed by flow cytometer and western blot assay. As a result, 4 induced HeLa cell apoptosis in a dose dependent manner and significantly increased the protein levels of p-JNK and p-p38, whereas distinctly reduced the expression of p-AKT, and p-ERK. Thus, compound 4 might induce HeLa cells apoptosis via MAPK and AKT signaling pathways, which could be considered as a potential leading compound for the development of anticancer drugs.
      (Copyright © 2021. Published by Elsevier Ltd.)
    • Contributed Indexing:
      Keywords: AKT signaling pathway; Anticancer effect; Apoptosis; Ficus hirta; MAPK signaling pathway; Prenylated flavonoid
    • Accession Number:
      0 (Antineoplastic Agents)
      0 (Flavonoids)
      EC 2.7.11.1 (Proto-Oncogene Proteins c-akt)
    • Publication Date:
      Date Created: 20210220 Date Completed: 20210825 Latest Revision: 20210825
    • Publication Date:
      20221213
    • Accession Number:
      10.1016/j.bmcl.2021.127859
    • Accession Number:
      33609662