Drug intelligence / Profile preview

rhinacanthin c

Development stage
Preclinical
Modality
Small Molecules
Administration
None (studied In Vitro And Animal Models; Not Formulated For Human Administration)
01

Overview

Rhinacanthin C is a **bioactive naphthoquinone ester** extracted from *Rhinacanthus nasutus* (Acanthaceae). It exhibits **anticancer, anti-inflammatory, antitumor, and antiviral activity**. Mechanistically, rhinacanthin C inhibits several cellular targets, including the drug efflux transporter P-glycoprotein (P-gp), MAPK signaling proteins, and inflammatory pathways. It has been shown to suppress osteoclast differentiation by inhibiting RANKL-induced TRAF6-TAK1 complex formation and downstream signaling (including ERK, JNK, and NF-κB), thereby reducing NFATc1 and c-Fos expression. In nonalcoholic fatty liver disease (NAFLD) models, it activates AMPK and SIRT1 and downregulates SREBP-1c-mediated pathways to improve insulin sensitivity and reduce lipid accumulation. It also inhibits cancer cell proliferation, migration, invasion, and matrix metalloproteinases (MMP-2, MMP-9), and modulates drug transporters and cytochrome P450 enzymes[1][3][4][5][7].

Other names
2,6-Octadienoic acid, 2,6-dimethyl-, 3-(1,4-dihydro-3-hydroxy-1,4-dioxo-2-naphthalenyl)-2,2-dimethylpropyl ester, (2E,6E)naphthoquinone esterRC
02

Targets

ABCB1 (P-glycoprotein)ABCG2 (Breast cancer resistance protein)MMP9 (Matrix metalloproteinase-9)OATP1B1 (Organic anion transporting polypeptide 1B1)SLCO1B3 (Organic anion transporting polypeptide 1B3)ABCC2 (ATP-binding cassette sub-family C member 2)MMP-2 (Matrix metalloproteinase-2)CYP2C8 (Cytochrome P450 2C8)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP2C19 (Cytochrome P450 2C19)MEK

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