Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1

Tien Dat Nguyen, Xuejun Jin, Jeong Hyung Lee, Dongho Lee, Young Soo Hong, Kyeong Lee, Ho Kim Young, Joon Lee Jung

Research output: Contribution to journalArticle

51 Citations (Scopus)

Abstract

The hypoxia-inducible factor-1 (HIF-1) has been known to be correlated to the adaptation and proliferation of tumor cells; therefore HIF-1 has become an important target in the development of anticancer drugs. A phytochemical study of the CHCl3-soluble fraction of Salvia miltiorrhiza, which strongly inhibited hypoxia-induced reporter gene expression, led to the isolation of 12 abietane-type diterpenes. Of these compounds, sibiriquinone A (1), sibiriquinone B (2), cryptotanshinone (3), and dihydrotanshinone I (4) potently inhibited hypoxia-induced luciferase expression with IC50 values of 0.34, 3.36, 1.58, and 2.05 μM on AGS cells, a human gastric cancer cell line, and 0.28, 3.18, 1.36, and 2.29 μM on Hep3B cells, a human hepatocarcinoma cell line, respectively. Consistently, 1 and 4 dose-dependently suppressed the HIF-1α accumulation and 1 inhibited mRNA expression of vascular endothelial growth factor (VEGF) under hypoxia. These results suggest that the anticancer activity of tanshinones is likely at least in part associated with their inhibition of HIF-1 accumulation.

Original languageEnglish
Pages (from-to)1093-1097
Number of pages5
JournalJournal of Natural Products
Volume70
Issue number7
DOIs
Publication statusPublished - 2007 Jul 1

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Abietane Diterpenes
Salvia miltiorrhiza
Hypoxia-Inducible Factor 1
diterpenoids
Chemical activation
hypoxia
Cells
Cell Line
human cell lines
stomach neoplasms
vascular endothelial growth factors
antineoplastic agents
Phytochemicals
luciferase
Luciferases
Reporter Genes
reporter genes
Gene expression
Vascular Endothelial Growth Factor A
phytopharmaceuticals

ASJC Scopus subject areas

  • Plant Science
  • Chemistry (miscellaneous)
  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1. / Nguyen, Tien Dat; Jin, Xuejun; Lee, Jeong Hyung; Lee, Dongho; Hong, Young Soo; Lee, Kyeong; Young, Ho Kim; Jung, Joon Lee.

In: Journal of Natural Products, Vol. 70, No. 7, 01.07.2007, p. 1093-1097.

Research output: Contribution to journalArticle

Nguyen, TD, Jin, X, Lee, JH, Lee, D, Hong, YS, Lee, K, Young, HK & Jung, JL 2007, 'Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1', Journal of Natural Products, vol. 70, no. 7, pp. 1093-1097. https://doi.org/10.1021/np060482d
Nguyen, Tien Dat ; Jin, Xuejun ; Lee, Jeong Hyung ; Lee, Dongho ; Hong, Young Soo ; Lee, Kyeong ; Young, Ho Kim ; Jung, Joon Lee. / Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1. In: Journal of Natural Products. 2007 ; Vol. 70, No. 7. pp. 1093-1097.
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