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 down-regulation 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.

Lobetyolin (LBT) 是一种聚乙炔苷，存在于多种药用植物中，但主要从党参（称为党参或党参）的根中分离出来。鉴定出12种含有党参的中药制剂；一般用于补脾肺气，偶尔也用于治疗癌症。在这里，我们回顾了党参提取物、LBT 和结构类似物的抗癌特性。Lobetyolin 和 lobetyolinin 是聚乙炔化合物 Lobetyol 的单糖基化形式和双糖基化形式。Lobetyol 和 LBT 已显示出对抗多种癌症（特别是胃癌）的活性，我们检查了其活性的分子基础。已证明 LBT 下调谷氨酰胺代谢，有助于药物诱导的细胞凋亡和肿瘤生长抑制。LBT 显着降低氨基酸转运蛋白丙氨酸-丝氨酸-半胱氨酸转运蛋白 2 (ASCT2) 的 mRNA 和蛋白表达。基于与其他抗癌化合物的结构相似性，本文提出了其他潜在靶标。LBT和相关的聚乙炔苷应进一步被视为潜在的抗癌药物，但需要更多的工作来评估其功效、毒性和风险效益比。