Drug intelligence / Profile preview

terrein

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Terrein is a bioactive fungal metabolite primarily isolated from *Aspergillus terreus*. It has demonstrated a diverse range of biological activities, including anti-inflammatory, antioxidant, and anti-melanogenic properties. In oncology research, terrein has shown significant antiproliferative and pro-apoptotic effects against various cancer cell lines, such as HeLa cervical carcinoma cells, with an IC50 of approximately 0.29 mM. Its mechanism of action involves the induction of apoptosis through the upregulation of the p53 and extracellular signal-regulated kinase (ERK) signaling pathways. This activation triggers both the extrinsic (death-receptor) and intrinsic (mitochondrial) apoptotic cascades, characterized by the activation of caspases-3, -8, and -9, an increase in the Bax/Bcl-2 expression ratio, and mitochondrial membrane depolarization. Additionally, terrein is noted for its ability to inhibit melanogenesis, making it a subject of interest for the treatment of hyperpigmentation disorders.

Other names
(4S,5R)-4,5-dihydroxy-3-[(1E)-prop-1-en-1-yl]cyclopent-2-en-1-one
02

Targets

MAPK3 (Mitogen-activated protein kinase 1)TP53 (Cellular Tumor Antigen p53 R175H)

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