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Cytotoxic Triterpenes from Salacia crassifolia and Metabolite Profiling of Celastraceae Species

  1. Author:
    Espindola, Laila S
    Dusi, Renata G
    Demarque, Daniel P [ORCID]
    Braz-Filho, Raimundo [ORCID]
    Yan, Pengcheng
    Bokesch, Heidi [ORCID]
    Gustafson, Kirk
    Beutler, John [ORCID]

  2. Author Address

    Laborat 243;rio de Farmacognosia, Universidade de Bras 237;lia, Campus Universit 225;rio Darcy Ribeiro, Bras 237;lia 70910-900, Brazil. darvenne@unb.br., Molecular Targets Program, National Cancer Institute, Frederick, MD 21702, USA. darvenne@unb.br., Laborat 243;rio de Farmacognosia, Universidade de Bras 237;lia, Campus Universit 225;rio Darcy Ribeiro, Bras 237;lia 70910-900, Brazil. renatadusi@hotmail.com., Molecular Targets Program, National Cancer Institute, Frederick, MD 21702, USA. renatadusi@hotmail.com., Laborat 243;rio de Farmacognosia, Universidade de Bras 237;lia, Campus Universit 225;rio Darcy Ribeiro, Bras 237;lia 70910-900, Brazil. dpdemarque@gmail.com., FAPERJ/Departamento de Qu 237;mica, Universidade Federal Rural do Rio de Janeiro, Serop 233;dica, RJ and Laborat 243;rio de Ci 234;ncias Qu 237;micas, Universidade Estadual do Norte Fluminense, Campos dos Goytacazes, Rio de Janeiro 28013-602, Brazil. braz@uenf.br., Molecular Targets Program, National Cancer Institute, Frederick, MD 21702, USA. yanpc@wzmc.edu.cn., School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China. yanpc@wzmc.edu.cn., Molecular Targets Program, National Cancer Institute, Frederick, MD 21702, USA. bokeschh@mail.nih.gov., Basic Science Program, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research Sponsored by the National Cancer Institute, Frederick, MD 21702, USA. bokeschh@mail.nih.gov., Molecular Targets Program, National Cancer Institute, Frederick, MD 21702, USA. gustafki@mail.nih.gov., Molecular Targets Program, National Cancer Institute, Frederick, MD 21702, USA. beutlerj@mail.nih.gov.,
    1. Year: 2018
    2. Date: Jun 20
    3. Epub Date: 2018 06 20
  2. Journal: Molecules
    1. 23
    2. 6
    3. Pages: pii: E1494
  4. Type of Article: Article
  5. Article Number: 1494
  6. ISSN: 1420-3049
  1. Abstract:

    The new pentacyclic triterpene 11β-hydroxypristimerin (1), along with the known metabolites pristimerin (2), 6-oxopristimerol (3) and vitideasin (4), were isolated from a Salacia crassifolia root wood extract, following a bioassay-guided fractionation approach. Both the extract and the purified triterpenes displayed pronounced cytotoxic activity against human cancer cell lines. The NCI-60 cell line screen revealed that compound 2 was the most active, with a mean GI50 of 0.17 μM, while compound 1 had a mean GI50 of 8.7 μM. A COMPARE analysis of the screening results showed that pristimerin is likely to be the main compound responsible for the cytotoxic activity of the extract (mean GI50 of 0.3 μg·mL−1). A targeted search for pristimerin and related derivatives using LC-MS/MS revealed the presence of pristimerin (2) and 6-oxopristimerol (3) in all Celastraceae species examined and in all plant parts tested, while vitideasin (4) was only detected in the genus Salacia.

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External Sources

  1. View Full Text
  2. DOI: 10.3390/molecules23061494
  3. PMID: 29925807
  4. View record in Web of Science®
  5. WOS: 000435875400255
  6. PII : molecules23061494

Library Notes

  1. Fiscal Year: FY2017-2018
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