Boldine

Boldine is an alkaloid that has been found in P. boldus and has diverse biological activities.^1,2,3,4 It completely inhibits tert-butyl hydroperoxide-induced lipid peroxidation and cell death in isolated rat hepatocytes when used at a concentration of 200 µM.¹ Boldine reduces copper- and peroxidase-induced LDL oxidation in vitro in a concentration-dependent manner.² In vivo, boldine (1 mg/animal per day) reduces the number and area of aortic atherosclerotic lesions in LDL receptor knockout (LDLR^-/-) mice fed an atherogenic diet. It reduces carrageenan-induced paw edema in guinea pigs (ED₅₀ = 43 mg/kg) and reduces bacterial pyrogen-induced hyperthermia in rabbits when administered at a dose of 60 mg/kg.³ Boldine (25 and 50 mg/kg) increases the latency to myoclonic and clonic seizures in a mouse model of seizures induced by pentylenetetrazole (PTZ; Item No. 18682).⁴ It also decreases electroshock-induced tonic hindlimb extension in mice.

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1. Bannach, R., Valenzuela, A., Cassels, B.K., et al. Cytoprotective and antioxidant effects of boldine on tert-butyl hydroperoxide-induced damage to isolated hepatocytes. Cell Biol. Toxicol. 12(2), 89-100 (1996).

2. Santanam, N., Penumetcha, M., Speisky, H., et al. A novel alkaloid antioxidant, Boldine and synthetic antioxidant, reduced form of RU486, inhibit the oxidation of LDL in-vitro and atherosclerosis in vivo in LDLR(-/-) mice. Atherosclerosis 173(2), 203-210 (2004).

3. Backhouse, N., Delporte, C., Givernau, M., et al. Anti-inflammatory and antipyretic effects of boldine. Agents Actions 42(3-4), 114-117 (1994).

4. Moezi, L., Yahosseini, S., Jamshizadeh, A., et al. Acute boldine treatment induces anti-convulsant effects in mice through its antioxidant activity. Drug Res. (Stuttg.) 69(4), 227-233 (2019).