Drug intelligence / Profile preview

8-o-acetylharpagide

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

8-o-acetylharpagide (AT-1) is a natural iridoid glycoside compound purified from the endemic Taiwanese plant *Ajuga taiwanensis*. It is being investigated for its potential as a selective radiosensitizer and anti-cancer agent, particularly in the treatment of hypopharyngeal squamous cell carcinoma (HPSCC). The compound demonstrates selective cytotoxicity, significantly reducing the viability of cancer cells (such as FaDu) while exerting minimal effects on normal human periodontal ligament fibroblasts (PDL). Its mechanism of action involves the induction of G2/M phase arrest and DNA double-strand breaks, accompanied by the downregulation of pro-survival proteins such as AKT and Bcl-2, and the modulation of cell cycle regulators like Cyclin B1. Beyond oncology, 8-o-acetylharpagide has been reported to possess anti-aging and anti-inflammatory properties.

Other names
8-O-acetylharpagide
02

Targets

BCL-2 (BCL-2 family)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)

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