The Role of Ingenane Diterpenes in Cancer Therapy: From Bioactive Secondary Compounds to Small Molecules

Author(s)

Alves, Ana Laura, V ; da Silva, Luciane S. ; Faleiros, Camila A. ; Silva, Viviane A. O. ; Reis, Rui M.

• Document type: Journal article
• Source: NATURAL PRODUCT COMMUNICATIONS; v. 17, n. 7, p. 30-pg., 2022-07-01.

Abstract

Diterpenes are a class of critical taxonomic markers of the Euphorbiaceae family, representing small compounds (eg, molecules) with a wide range of biological activities and multi-target therapeutic potential. Diterpenes can exert different activities, including antitumor and multi-drug resistance-reversing activities, and antiviral, immunomodulatory, and anti-inflammatory effects, mainly due to their great structural diversity. In particular, one polycyclic skeleton has been highlighted: ingenane. Besides this natural diterpene, promising polycyclic skeletons may be submitted to chemical modification-by in silico approaches, chemical reactions, or biotransformation-putatively providing more active analogs (eg, ingenol derivatives), which are currently under pre-clinical investigation. This review outlines the current mechanisms of action and potential therapeutic implications of ingenol diterpenes as small cancer molecules. (AU)

• FAPESP's process: 19/23245-5 - Study of ingenol-3-angelate as a new class of resistance sensitizer to TRAIL-based therapy in human cancer cells
• Grantee: Camila Aparecida Faleiros
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• FAPESP's process: 19/05142-4 - Characterization of the biological effect of semisynthetic compound derived from Euphorbia tirucalli in vitro and in vivo, from the establishment of patients-derived xenografts with gastrointestinal tract tumors
• Grantee: Ana Laura Vieira Alves
• Support Opportunities: Scholarships in Brazil - Doctorate