Benzoylaconine

Benzoylaconine is an aconitine-type diterpenoid alkaloid that has been found in Aconitum species.^1,2 Benzoylaconine increases protein levels of the efflux transporters P-glycoprotein, multidrug resistance-associated protein 2 (MRP2), and breast cancer resistance protein (BCRP) in LS174T cells in a concentration-dependent manner.^2,3 It also increases the protein levels of P-glycoprotein in Caco-2 cells and the pregnane X receptor (PXR) in both Caco-2 and LS174T cells when used at a concentration of 50 μM.³ Benzoylaconine (50 μM) reduces the cytotoxic effects of the P-glycoprotein substrates vincristine (Item No. 11764) and doxorubicin (Item No. 15007) in Caco-2 cells. In vivo, benzoylaconine (0.6 mg/kg) increases protein levels of Nrf2, MRP2, and BCRP in the jejunum, ileum, and colon in mice.² It also increases survival of mice injected with a lethal dose of the neurotoxin aconitine (ED₅₀ = 15 mg/kg, i.p.).¹

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1. Tursunkhodzhaeva, F.M., Dzhakhangirov, F.N., and Salimov, B.T. Diterpenoid alkaloids as antidotes to aconitine-type neurotoxin poisoning. Structure–activity relationship. Chem. Nat. Compd. 52(5), 849-852 (2016).

2. Wu, J.-J., Zhu, Y.-F., Guo, Z.-Z., et al. Aconitum alkaloids, the major components of Aconitum species, affect expression of multidrug resistance-associated protein 2 and breast cancer resistance protein by activating the Nrf2-mediated signalling pathway. Phytomedicine 44, 87-97 (2018).

3. Wu, J., Lin, N., Li, F., et al. Induction of P-glycoprotein expression and activity by Aconitum alkaloids: Implication for clinical drug-drug interactions. Sci. Rep. 6:25343, (2016).