Drug intelligence / Profile preview

neferine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Neferine is a **bisbenzylisoquinoline alkaloid** primarily isolated from the seed embryo of the lotus plant, *Nelumbo nucifera*.[1][3][4][5] It demonstrates diverse pharmacological activities, including **anticancer, anti-inflammatory, anti-diabetic, anti-arrhythmic, anti-oxidant, anti-hypertensive, anti-fibrotic, anti-thrombotic, and neuroprotective effects**.[1][3][5] Mechanistically, neferine acts through several pathways: it **induces apoptosis, autophagy, and cell cycle arrest in cancer cells**, modulates the **PI3K/AKT/mTOR, TGF-β/Smad, and Nrf2/HO-1 signaling pathways**, and inhibits inflammatory mediators such as TNF-α, IL-6, iNOS, and COX-2.[3][5] Neferine also confers **cardioprotective and anti-fibrotic effects** in models of sepsis, myocardial damage, and organ fibrosis.[3][5] These properties make neferine a promising candidate for conditions such as cancer, cardiovascular diseases, diabetes, inflammatory disorders, and fibrosis.

Other names
NeferinMethylliensinine4-[[(1R)-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl]methyl]-2-[[(1R)-6-methoxy-1-[(4-methoxyphenyl)methyl]-2-methyl-3,4-dihydro-1H-isoquinolin-7-yl]oxy]phenol4''-O-MethylliensinineDTXSID40177462DTXSID-40177462DTXSID 40177462DTXCID9099953DTXCID-9099953DTXCID 9099953
02

Targets

HMOX1 (Heme oxygenase 1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)ABCB1 (P-glycoprotein)CASP3 (Caspase-3)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NOS1 (nNOS)TGFB (GARP–latent transforming growth factor beta 1 complex)TNFA (Tumor necrosis factor alpha (soluble))

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