Cancer chemopreventive activities of S-3-1, a synthetic derivative of Danshinone

Xiao Guang Chen, Yan Li, Chunhong Yan, Lian Niang Li, Rui Han

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Salvia miltiorrhiza is a traditional Chinese medicine which has been well documented for its anti-cancer effects. Based on the structure of danshinone, one of the active compounds derived from Salvia miltiorrhiza, we synthesized a simplified phenolic analog, S-3-1, and tried to explore its possible actions in preventing the development of cancer. With the Ames test, S-3-1 was found to efficiently suppress the mutagenicity of benzo[α]pyrene. This result is consistent with the inhibitory effect of S-3-1 on the activation of benzo[α]pyrene by hepatic microsomal enzymes. Besides the anti-initiation effects, S-3-1 could significantly inhibit the croton oil-induced increase of mouse skin epithermal ornithine decarboxylase activity. Moreover, S-3-1 quenched both superoxide and hydroxyl free radicals whereas it inhibited lipid peroxidation in the in vitro model. These results suggest that S-3-1 might act as anti-initiation and anti-promotion agents through reversing the biochemical alterations induced by carcinogen during carcinogenesis. Therefore, we further investigated the effects of S-3-1 on carcinogenesis. In vitro, S-3-1 inhibited the benzo[α]pyrene-induced transformation of V79 Chinese hamster lung fibroblasts. At 10-40 mg/kg, S-3-1 was found to inhibit the development of DMBA/croton oil-induced skin papilloma in mice through decreasing the incidence of papilloma, prolonging the latent period of tumor occurrence and reducing tumor number per mouse in a dose-dependent manner. We concluded from this study that S-3-1 might be developed as a new chemopreventive drug.

Original languageEnglish (US)
Pages (from-to)63-75
Number of pages13
JournalJournal of Asian Natural Products Research
Volume3
Issue number1
DOIs
StatePublished - Jan 1 2001
Externally publishedYes

Fingerprint

Croton Oil
Salvia miltiorrhiza
Derivatives
Tumors
Skin
Papilloma
Neoplasms
9,10-Dimethyl-1,2-benzanthracene
Carcinogenesis
Ornithine Decarboxylase
Fibroblasts
Superoxides
Carcinogens
Hydroxyl Radical
Medicine
Free Radicals
Chinese Traditional Medicine
Cricetulus
Chemical activation
Lipid Peroxidation

Keywords

  • Anti-cancer drug
  • Carcinogenesis
  • Chemoprevention
  • Danshinone derivative
  • Salvia miltinorrhiza

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

Cite this

Cancer chemopreventive activities of S-3-1, a synthetic derivative of Danshinone. / Chen, Xiao Guang; Li, Yan; Yan, Chunhong; Li, Lian Niang; Han, Rui.

In: Journal of Asian Natural Products Research, Vol. 3, No. 1, 01.01.2001, p. 63-75.

Research output: Contribution to journalArticle

Chen, Xiao Guang ; Li, Yan ; Yan, Chunhong ; Li, Lian Niang ; Han, Rui. / Cancer chemopreventive activities of S-3-1, a synthetic derivative of Danshinone. In: Journal of Asian Natural Products Research. 2001 ; Vol. 3, No. 1. pp. 63-75.
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AB - Salvia miltiorrhiza is a traditional Chinese medicine which has been well documented for its anti-cancer effects. Based on the structure of danshinone, one of the active compounds derived from Salvia miltiorrhiza, we synthesized a simplified phenolic analog, S-3-1, and tried to explore its possible actions in preventing the development of cancer. With the Ames test, S-3-1 was found to efficiently suppress the mutagenicity of benzo[α]pyrene. This result is consistent with the inhibitory effect of S-3-1 on the activation of benzo[α]pyrene by hepatic microsomal enzymes. Besides the anti-initiation effects, S-3-1 could significantly inhibit the croton oil-induced increase of mouse skin epithermal ornithine decarboxylase activity. Moreover, S-3-1 quenched both superoxide and hydroxyl free radicals whereas it inhibited lipid peroxidation in the in vitro model. These results suggest that S-3-1 might act as anti-initiation and anti-promotion agents through reversing the biochemical alterations induced by carcinogen during carcinogenesis. Therefore, we further investigated the effects of S-3-1 on carcinogenesis. In vitro, S-3-1 inhibited the benzo[α]pyrene-induced transformation of V79 Chinese hamster lung fibroblasts. At 10-40 mg/kg, S-3-1 was found to inhibit the development of DMBA/croton oil-induced skin papilloma in mice through decreasing the incidence of papilloma, prolonging the latent period of tumor occurrence and reducing tumor number per mouse in a dose-dependent manner. We concluded from this study that S-3-1 might be developed as a new chemopreventive drug.

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