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Drug intelligence / Profile preview
miltirone
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Miltirone is a natural lipophilic compound isolated from the root of *Salvia miltiorrhiza* Bunge. It acts as a central benzodiazepine receptor partial agonist and displays diverse pharmacological activities including antiplatelet, antithrombotic, anti-inflammatory, and anticancer effects. Mechanistically, miltirone inhibits platelet aggregation and thrombus formation by suppressing Syk-PLCγ2-PKC/MAPK and PI3K-Akt-GSK3β signaling downstream of the glycoprotein VI pathway, and Src/FAK signaling in integrin αIIbβ3-mediated platelet "outside-in" signaling[1]. In cancer models, miltirone induces apoptosis in various cell types, enhances chemosensitivity to agents such as cisplatin, and downregulates the PI3K/Akt/mTOR pathway, as well as affecting other pathways such as MEK/ERK1/2 and mitochondrial ROS generation[7].
- Other names
- Rosmariquinone
02
Targets
GABAA (Gamma-aminobutyric acid receptor)BZD site (GABA-A receptor benzodiazepine site)MAPK3 (Mitogen-activated protein kinase 1)FAK (Focal adhesion kinase)GSK3 (Glycogen synthase kinase 3 beta)mTOR (Mammalian target of rapamycin kinase)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)PLCG2 (Phospholipase C gamma 2)AKT (RAC-alpha serine/threonine-protein kinase)PKC (Protein kinase C family)SYK (Spleen Tyrosine Kinase)
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