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Drug intelligence / Profile preview
isojacareubin
- Development stage
- Preclinical
- Lead developer
- Changhua Christian Hospital
- Modality
- Small Molecules
01
Overview
Isojacareubin is a naturally occurring xanthonoid compound isolated from medicinal plants such as *Hypericum japonicum* and *Garcinia nujiangensis*. It exhibits a broad spectrum of biological activities, including anticancer, antibacterial, and antiviral properties. In oncology, isojacareubin acts as an inhibitor of protein kinase C (PKC) and suppresses the PI3K/AKT/mTOR and MAPK/ERK signaling pathways to induce apoptosis and inhibit metastasis in hepatocellular carcinoma, ovarian cancer, and triple-negative breast cancer (TNBC). In chemoresistant TNBC, its mechanism involves the epigenetic repression of *PIK3CA* transcription via the deacetylation of Histone 3 lysine 56 (H3K56). Additionally, isojacareubin has demonstrated antibacterial efficacy against methicillin-resistant *Staphylococcus aureus* (MRSA) and *Helicobacter pylori*, and has been investigated as a covalent inhibitor of the SARS-CoV-2 main protease (3CLpro).
- Other names
- 6,10,11-trihydroxy-3,3-dimethyl-3H,7H-pyrano[2,3-c]xanthen-7-one6,10,11-trihydroxy-3,3-dimethylpyrano[2,3-c]xanthen-7-oneISJ
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)PRKCZ (Protein kinase C zeta)Mpro (3C-like proteinase of SARS-CoV-2)
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