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Isorhapontigenin (ISO), a naturally-occurring stilbene derivative, has garnered significant attention due to its potent anticancer and anti-inflammatory properties. This review synthesizes current knowledge regarding the mechanisms of action, efficacy, and potential therapeutic applications of Isorhapontigenin acquired in vitro and in vivo. It systematically analyzes its effects on various cancer cell lines, tumor models, and inflammatory conditions, examining its impact on cell proliferation, apoptosis, metastasis, and inflammatory mediators. In vitro studies reveal that Isorhapontigenin induces cell cycle arrest, promotes apoptosis, and inhibits cancer cell migration through modulation of key signaling pathways, including EGFR-PI3K-Akt and NF-κB. It also demonstrates potent antioxidant and anti-inflammatory effects by enhancing Nrf2 signaling and suppressing pro-inflammatory cytokine production. These findings are corroborated by in vivo studies confirming its ability to inhibit tumor growth in xenograft models and attenuate inflammatory responses in various disease models. Notably, Isorhapontigenin exhibits superior pharmacokinetic profiles then resveratrol, with higher oral bioavailability. Isorhapontigenin demonstrates multi-target actions, including epigenetic modulation through microRNA regulation, which highlight its potential as a versatile therapeutic agent. This review also identifies current limitations in Isorhapontigenin research that require further investigation. Overall, Isorhapontigenin offers promise as a multi-faceted compound for the treatment of cancer, inflammatory diseases, and metabolic disorders, providing a solid foundation for future research and potential clinical applications., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 The Authors. Published by Elsevier Masson SAS.. All rights reserved.)

The Plectranthus genus is often cited for its medicinal properties. Plectranthus ornatus Codd. is traditionally used in Africa for the treatment of gastric and liver diseases and their leaves are used for their antibiotic action. The main constituent of P. ornatus is the halimane compound, 11 R ∗ -acetoxyhalima-5,13E-dien-15-oic acid (Hal), described for its antimicrobial and anticancer properties. The objective of this work was to improve the activity of the halimane lead molecule. Further physiochemical characterisation was performed on Hal. To the best of our knowledge, this work constitutes the first published data of the absolute configurations by SCXRD and thermal stability of Hal. Using Hal, reactions with different amines were carried out to afford novel semi-synthetic derivatives and their structural elucidation was completed. The cytotoxicity of the derivatives was assessed against three leukaemia cancer cell lines (CCRF-CEM, K562 and HL-60). The antioxidant activity was investigated using H 2 O 2 -induced HGF-1 cells and their anti-inflammatory activity was studied using RT-PCR and ELISA. Our data showed that amide derivatives of Hal presented moderate cytotoxicity and more potent activity when compared to the parent molecule, giving insight into the SAR of Hal. The derivatives also displayed protection against oxidative damage to DNA. Finally, the derivatives possessed anti-inflammatory properties at the level of gene and protein expression for the cytokines IL-1β, TNF-α and IL-6, induced by LPS in normal HGF-1 cells. Overall, our study provides useful insight into the enhanced biological activities of semi-synthetic Hal derivatives, as a starting point for novel drug formulations in cancer therapy., Competing Interests: Declaration of Competing Interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Patricia Rijo reports financial support was provided by Foundation for Science and Technology. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 The Authors. Published by Elsevier Masson SAS.. All rights reserved.)