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<p>Medicinal plants are an invaluable source of specialized metabolites with unique and complex chemical structures. This chemical diversity offers a rich resource for discovering new compounds with therapeutic potential. One notable example is <i>Ageratina petiolaris</i>, which produces a mixture of esters of 2α-hydroxyeperuic acid (<b>1</b>) in high quantity. The <i>ent-</i>labdane <b>2</b>, a product of the alkaline hydrolysis of <b>1</b>, possesses a chemical structure with promising therapeutic potential. In this work, aniline, cyclohexylamine, 4-chloroaniline, bencilamine, <i>p</i>-cinnamyl alcohol, phenol, 4-bromophenol, and 4-methoxyphenol were used to prepare ester and amide derivatives of <b>2</b> in a one-pot process aided with sonochemistry, yielding the respective compounds in moderate to good yields. Additionally, the antiproliferative potential of the amides and esters was tested in vitro against MCF-7, HeLa, A549, and K562 cancer cell lines. The results showed significant cytotoxic activity for almost all the evaluated derivatives, making them promising candidates for potential therapeutic agents against certain types of cancer.</p><p></p>

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Anticancer activity of amide and ester derivatives of the ent-labdane 2α-hydroxyeperuic acid obtained via sonochemical synthesis

  • 期刊论文

  • 发表日期：

    2026年1月15日

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  • Francisco Juárez-Carrillo,
  • Julio C. Ontiveros-Rodríguez,
  • Mónica Luna-Vázquez,
  • Joel E. López-Meza,
  • Rosa E. del Río,
  • José Carlos Espinoza-Hicks,
  • Alejandra Ochoa-Zarzosa,
  • Carlos M. Cerda-García-Rojas,
  • Hugo A. García-Gutiérrez

摘要

Medicinal plants are an invaluable source of specialized metabolites with unique and complex chemical structures. This chemical diversity offers a rich resource for discovering new compounds with therapeutic potential. One notable example is Ageratina petiolaris, which produces a mixture of esters of 2α-hydroxyeperuic acid (1) in high quantity. The ent-labdane 2, a product of the alkaline hydrolysis of 1, possesses a chemical structure with promising therapeutic potential. In this work, aniline, cyclohexylamine, 4-chloroaniline, bencilamine, p-cinnamyl alcohol, phenol, 4-bromophenol, and 4-methoxyphenol were used to prepare ester and amide derivatives of 2 in a one-pot process aided with sonochemistry, yielding the respective compounds in moderate to good yields. Additionally, the antiproliferative potential of the amides and esters was tested in vitro against MCF-7, HeLa, A549, and K562 cancer cell lines. The results showed significant cytotoxic activity for almost all the evaluated derivatives, making them promising candidates for potential therapeutic agents against certain types of cancer.