Drug intelligence / Profile preview

glaucocalyxin A

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal, In Vitro Studies Only
01

Overview

Glaucocalyxin A is a natural ent-kaurane diterpenoid compound primarily isolated from plants of the genus Rabdosia (notably Rabdosia japonica). It has been widely studied for its diverse biological activities including antitumor/cytotoxic effects against cancer cells (by inducing apoptosis and inhibiting cell growth), anti-bacterial activity; anti-inflammatory and anti-neuroinflammatory properties; antioxidant effects; anticoagulant and antithrombotic actions through inhibition of platelet activation and aggregation; as well as immune modulation. Mechanistically in cancer models it acts by inhibiting thioredoxin reductase 1 (TXNRD1) via covalent modification of its selenocysteine residue and depleting glutathione to induce disulfide stress in tumor cells. In platelets it inhibits collagen receptor GPVI-mediated signaling pathways by blocking tyrosine phosphorylation events downstream of Syk kinase and phospholipase Cγ2 activation[1][4][5][7]. Glaucocalyxin A is not an approved pharmaceutical but is under investigation for potential use as an anticancer agent or antiplatelet/antithrombotic agent.

Other names
79498-31-0(1R,2R,4S,9R,10S,13S,16R)-2,16-dihydroxy-5,5,9-trimethyl-14-methylidenetetracyclo[11.2.1.01,10.04,9]hexadecane-6,15-dione7alpha,14beta-dihydroxy-ent-kaur-16-ene-3,5-dione(7R,14R)-Ent-7,14,dihydroxy-kaur-16-en-3,15-dioneLeucamenin FWangzaozin BLeukaMenin F
02

Targets

VDAC (Voltage-dependent anion channel)

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