Cytotoxicity of Carvotacetones from Sphaeranthus africanus Against Cancer Cells and Their Potential to Induce Apoptosis.

Three carvotacetones (1 – 3) isolated from Sphaeranthus africanus were screened in 60 cancer cell lines at the National Cancer Institute (NCI) within the Developmental Therapeutics Program (DTP). At the concentration of 10−5 M, compound 1 (3,5-diangeloyloxy-7-hydroxycarvotacetone) turned out to be t...

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Publicado en:Planta Medica Vol. 89; no. 6; pp. 624 - 637
Autores principales: Tran, Huyen Thi, Kretschmer, Nadine, Huynh, Loi, Bauer, Rudolf
Formato: pictorial research tables/charts Journal Article
Publicado: Georg Thieme Verlag Stuttgart 2023
Acceso en línea:Ver este registro en EBSCOhost
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      pub: Georg Thieme Verlag Stuttgart
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        atl: Cytotoxicity of Carvotacetones from Sphaeranthus africanus Against Cancer Cells and Their Potential to Induce Apoptosis.
      aug:
        au:
          Tran, Huyen Thi
          Kretschmer, Nadine
          Huynh, Loi
          Bauer, Rudolf
        affil: Department of Pharmacognosy, School of Medicine, Vietnam National University HCM City, Ho Chi Minh City, Vietnam
      sug:
        subj:
          Cell Line, Tumor Drug Effects
          Plant Extracts Pharmacodynamics
          Apoptosis Drug Effects
          Plants, Medicinal
          Molecular Structure
      ab: Three carvotacetones (1 – 3) isolated from Sphaeranthus africanus were screened in 60 cancer cell lines at the National Cancer Institute (NCI) within the Developmental Therapeutics Program (DTP). At the concentration of 10−5 M, compound 1 (3,5-diangeloyloxy-7-hydroxycarvotacetone) turned out to be the most active compound against ACHN and UO-31 renal cancer cell lines with growth percent values of − 100% (all cells dead). Compound 2 (3-angeloyloxy-5-[2″,3″-epoxy-2″-methylbutanoyloxy]-7-hydroxycarvotacetone) showed strong effects in SK-MEL-5 melanoma and ACHN renal cancer cells with inhibition values of 93% and 97%, respectively. Compound 3 (3-angeloyloxy-5-[3″-chloro-2″-hydroxy-2″-methylbutanoyloxy]-7-hydroxy-carvotacetone) exhibited a quite strong effect on renal cancer cells with a growth inhibitory effect of 96% against ACHN and UO-31 cells. When treated with five different concentrations of 1 (1 × 10−8 , 1 × 10−7 , 1 × 10−6 , 1 × 10−5 , and 1 × 10−4 M), HOP-92 cells were found to be most sensitive with GI50 , TGI, and LC50 values of 0.17, 0.40, and 0.96 µM, respectively. When using the ApoTox-Glo triplex assay to evaluate the apoptosis inducing effects of seven carvotacetones isolated from S. africanus in CCRF-CEM cells, compounds 1 – 6 increased caspase-3/7 activity with 1, 2 , and 4 (3-angeloyloxy-5,7-dihydroxycarvotacetone) exhibiting the highest activitiy, indicating induction of caspase-dependent apoptosis.
      pubtype: Periodical
      doctype:
        pictorial
        research
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      ougenre: Article
    language: English
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