Tovophyllin A

Tovophyllin A is an orally active xanthonoid compound. Tovophyllin A exerts neuroprotective effects against Parkinson's disease by activating the Akt / GSK3β signaling pathway. Tovophyllin A protects mouse models of liver injury by activating Nrf2. Tovophyllin A exhibits protective anti-inflammatory activity in mouse models of acute lung injury. Tovophyllin A inhibits the activation of NF-κB and subsequent release of pro-inflammatory cytokines. Tovophyllin A reduces apoptotic cell death ( Apoptosis ). Tovophyllin A has antiplasmodial activity. Tovophyllin A shows cytotoxic activity against lung epithelial cancer cells and breast cancer cells. Tovophyllin A can be used in research related to Parkinson's disease, liver injury, acute lung injury, lung epithelial cancer, and breast cancer ^{[1] [2] [3]}.

In Vivo, Tovophyllin A (5 mg/kg; single pre-treatment dose) alleviates MPTP -induced Parkinson's disease in male C57BL/6 mice by restoring motor function, preserving dopaminergic neurons in the substantia nigra pars compacta (SNc), and activating the Akt/GSK3β pro-survival signaling pathway^[1]. Tovophyllin A (50-100 mg/kg; p.o.; once daily; 5 days) dose-dependently protects male BALB/c mice against Acetaminophen -induced acute liver injury. At the dose of 100 mg/kg, it almost completely reverses hepatic necrosis, oxidative stress and the elevation of inflammatory mediators, and potently activates the Nrf2 cytoprotective pathway^[2]. Tovophyllin A (50-100 mg/kg; p.o.; daily; 5 days prior to LPS challenge) improves LPS -induced acute lung injury in male BALB/c mice in a dose-dependent manner^[3].

In Vitro, Tovophyllin A (0.01-20 μM; 24 h) protects primary cortical neurons against MPP+- and paraquat (PQ)-induced neurotoxicity. After 24 h of co-treatment, it significantly increases cell viability in the MPP+ model at concentrations ≥0.1 μM and in the PQ model at concentrations ≥1 μM^[1]. Tovophyllin A (serial twofold dilutions starting at 200 μM; 48 h) inhibits the proliferation of A549 human lung adenocarcinoma cells and MCF7 breast cancer cells, with IC₅₀ values of 2.2 μM and 6.1 μM, respectively^[3].

References:
[1]. Huang Y, et al. Neuroprotection Against Parkinson's Disease Through the Activation of Akt/GSK3β Signaling Pathway by Tovophyllin A. Front Neurosci. 2020;14:723. Published 2020 Jul 9.
[2]. Ibrahim SRM, et al. Protective activity of tovophyllin A, a xanthone isolated from Garcinia mangostana pericarps, against acetaminophen-induced liver damage: role of Nrf2 activation. Food Funct. 2018;9(6):3291-3300.
[3]. El-Agamy DS, et al. Protective anti-inflammatory activity of tovophyllin A against acute lung injury and its potential cytotoxicity to epithelial lung and breast carcinomas. Inflammopharmacology. 2020 Feb;28(1):153-163.
[4]. Azebaze AG, et al. Prenylated xanthone derivatives with antiplasmodial activity from Allanblackia monticola STANER L.C. Chem Pharm Bull (Tokyo). 2006 Jan;54(1):111-3.