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

doi:10.1007/s13659-020-00283-9

Natural Products and Bioprospecting

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

OncoWitan, 59290 Lille(Wasquehal), France

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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.

Keywords Cancer therapy Natural products Mechanism of action Molecular target Terpenoids Lobetyolin Polyacetylene glycoside Glutamine metabolism

Corresponding Authors: Christian Bailly E-mail: christian.bailly@oncowitan.com

Issue Date: 07 April 2021

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Christian Bailly. Anticancer Properties of Lobetyolin, an Essential Component of Radix Codonopsis (Dangshen)[J]. Natural Products and Bioprospecting, 2021, 11(2): 143-153.

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http://npb.kib.ac.cn/EN/10.1007/s13659-020-00283-9 OR http://npb.kib.ac.cn/EN/Y2021/V11/I2/143

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