Arnicolide D: a multi-targeted anticancer sesquiterpene lactone-preclinical efficacy and mechanistic insights

Naunyn Schmiedebergs Arch Pharmacol. 2024 Sep;397(9):6317-6336. doi: 10.1007/s00210-024-03095-7. Epub 2024 Apr 23.

Abstract

Arnicolide D, a potent sesquiterpene lactone from Centipeda minima, has emerged as a promising anticancer candidate, demonstrating significant efficacy in inhibiting cancer cell proliferation, inducing apoptosis, and suppressing metastasis across various cancer models. This comprehensive study delves into the molecular underpinnings of Arnicolide D's anticancer actions, emphasizing its impact on key signaling pathways such as PI3K/AKT/mTOR and STAT3, and its role in modulating cell cycle and survival mechanisms. Quantitative data from preclinical studies reveal Arnicolide D's dose-dependent cytotoxicity against cancer cell lines, including nasopharyngeal carcinoma, triple-negative breast cancer, and human colon carcinoma, showcasing its broad-spectrum anticancer potential. Given its multifaceted mechanisms and preclinical efficacy, Arnicolide D warrants further investigation in clinical settings to validate its therapeutic utility against cancer. The evidence presented underscores the need for rigorous pharmacokinetic and toxicological studies to establish safe dosing parameters for future clinical trials.

Keywords: Centipeda minima; Anti-cancer mechanisms; Apoptosis; Arnicolide D; PI3K/AKT/mTOR pathway; Sesquiterpene lactone, Src degradation.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Antineoplastic Agents, Phytogenic* / pharmacokinetics
  • Antineoplastic Agents, Phytogenic* / pharmacology
  • Antineoplastic Agents, Phytogenic* / therapeutic use
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Humans
  • Lactones* / pharmacology
  • Lactones* / therapeutic use
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Sesquiterpenes* / pharmacokinetics
  • Sesquiterpenes* / pharmacology
  • Sesquiterpenes* / therapeutic use
  • Signal Transduction / drug effects

Substances

  • Sesquiterpenes
  • Lactones
  • Antineoplastic Agents, Phytogenic
  • Antineoplastic Agents