整合生物学期刊网

应用天然产物 ›› 2021, Vol. 11 ›› Issue (2): 143-153.DOI: 10.1007/s13659-020-00283-9

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Anticancer Properties of Lobetyolin, an Essential Component of Radix Codonopsis (Dangshen)

Christian Bailly   

  1. OncoWitan, 59290 Lille(Wasquehal), France
  • 收稿日期:2020-10-13 修回日期:2020-11-02 出版日期:2021-04-24 发布日期:2021-04-07
  • 通讯作者: Christian Bailly

Anticancer Properties of Lobetyolin, an Essential Component of Radix Codonopsis (Dangshen)

Christian Bailly   

  1. OncoWitan, 59290 Lille(Wasquehal), France
  • Received:2020-10-13 Revised:2020-11-02 Online:2021-04-24 Published:2021-04-07
  • Contact: Christian Bailly

摘要: Lobetyolin (LBT) is a polyacetylene glycoside found in diverse medicinal plants but mainly isolated from the roots of Codonopsis pilosula, known as Radix Codonopsis or Dangshen. Twelve traditional Chinese medicinal preparations containing Radix Codonopsis were identified; they are generally used to tonify spleen and lung Qi and occasionally to treat cancer. Here we have reviewed the anticancer properties of Codonopsis extracts, LBT and structural analogs. Lobetyolin and lobetyolinin are the mono- and bis-glucosylated forms of the polyacetylenic compound lobetyol. Lobetyol and LBT have shown activities against several types of cancer (notably gastric cancer) and we examined the molecular basis of their activity. A downregulation of glutamine metabolism by LBT has been evidenced, contributing to drug-induced apoptosis and tumor growth inhibition. LBT markedly reduces both mRNA and protein expression of the amino acid transporter Alanine-Serine-Cysteine Transporter 2 (ASCT2). Other potential targets are proposed here, based on the structural analogy with other anticancer compounds. LBT and related polyacetylene glycosides should be further considered as potential anticancer agents, but more work is needed to evaluate their efficacy, toxicity, and risk-benefit ratio.

关键词: Cancer therapy, Natural products, Mechanism of action, Molecular target, Terpenoids, Lobetyolin, Polyacetylene glycoside, Glutamine metabolism

Abstract: Lobetyolin (LBT) is a polyacetylene glycoside found in diverse medicinal plants but mainly isolated from the roots of Codonopsis pilosula, known as Radix Codonopsis or Dangshen. Twelve traditional Chinese medicinal preparations containing Radix Codonopsis were identified; they are generally used to tonify spleen and lung Qi and occasionally to treat cancer. Here we have reviewed the anticancer properties of Codonopsis extracts, LBT and structural analogs. Lobetyolin and lobetyolinin are the mono- and bis-glucosylated forms of the polyacetylenic compound lobetyol. Lobetyol and LBT have shown activities against several types of cancer (notably gastric cancer) and we examined the molecular basis of their activity. A downregulation of glutamine metabolism by LBT has been evidenced, contributing to drug-induced apoptosis and tumor growth inhibition. LBT markedly reduces both mRNA and protein expression of the amino acid transporter Alanine-Serine-Cysteine Transporter 2 (ASCT2). Other potential targets are proposed here, based on the structural analogy with other anticancer compounds. LBT and related polyacetylene glycosides should be further considered as potential anticancer agents, but more work is needed to evaluate their efficacy, toxicity, and risk-benefit ratio.

Key words: Cancer therapy, Natural products, Mechanism of action, Molecular target, Terpenoids, Lobetyolin, Polyacetylene glycoside, Glutamine metabolism