New diterpenoids from Croton L. species (2019-2025): structural diversity and bioactivity.

Abstract

Croton L. (Euphorbiaceae) is recognized as one of the richest botanical sources of structurally diverse diterpenoids with a remarkable range of biological activities. These compounds display an exceptional diversity of carbon skeletons, many of which are unique to this genus, with bioactivity profiles that make them privileged scaffolds for drug discovery and development. Between 2019 and 2025, research on Croton phytochemistry has expanded considerably, with 40 species reported to contain diterpenoids and 330 new compounds described. This review covers the classification of structural types, plant sources, extraction and isolation techniques, structure elucidation methods, and pharmacological profiles. The newly identified metabolites belong to 14 structural classes, with clerodanes, labdanes, and phorbol esters being the most abundant, particularly in species such as Croton crassifolius Geiseler, Croton damayeshu Y.T. Chang, Croton kongensis Gagnep., Croton tiglium L., and Croton laui Merr. & F.P. Metcalf. Clerodane diterpenoids showed the greatest chemical diversity, while kaurane and phorbol esters displayed potent activity in individual assays; yet varying conditions prevent a general potency ranking across classes. Overall, biological evaluations were predominantly conducted in vitro and identified cytotoxic effects against cancer cell lines, anti-inflammatory and antiparasitic activities, and effects in experimental models of metabolic dysfunction and neuronal injury. The compiled data highlight significant advances in diterpene discovery within the genus while also emphasizing current limitations, such as scarce mechanistic studies, very limited in vivo validation, and limited quantities available for testing. These findings lay the groundwork for future research in biosynthesis, chemical synthesis, pharmacology, and biotechnological production to determine the therapeutic potential of Croton-derived diterpenoids. A review of 40 Croton species from 2019 to 2025 reports 330 new diterpenes. The workflow moves from extraction through isolation and purification to structure elucidation. Identified skeletons include clerodane, labdane, halimane, phorbol esters, crotophane, trachylobane, cembrane, and pimarane. Reported biological activities include cytotoxic, anti-inflammatory, antimicrobial, larvicidal or insecticidal, neuroprotective, and antidiabetic effects.

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