Noscapine

Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier^{[1][2][3][4][5]}. IC50 & Target:Sigma opioid receptors^[4] Bradykinin^[5] Apoptosis^[1] In Vitro:Noscapine (0-1000 μM; 0-96 hours; rat C6 glioma cells) treatment inhibits cell viability of rat C6 glioma in vitro in a dose- and time-dependent manner. Noscapine inhibits the viability of rat C6 glioma cells with an IC₅₀ of 250 μM at 72 hours^[1].
Noscapine exposure causes abnormal S-phase reentry, increases mitotic arrest and results in excessive DNA accumulation^[1].
Cylindromatosis increases the ability of noscapine to induce mitotic arrest and apoptosis. Cylindromatosis enhances the effect of noscapine on microtubule polymerization and promotes noscapine binding to microtubules^[2]. In Vivo:To ensure solubility, animal experiments can choose Noscapine hydrochloride (HY-13716A):
Noscapine hydrochloride (300 mg/kg; oral gavage; daily; for 15 days; athymic female mice) treatment reduces tumor growth in mice^[1].