Oxyacanthine is a bisbenzylisoquinoline alkaloid and anti-inflammatory agent. Oxyacanthine exists in plants such as Berberis oblonga, Berberis vulgaris and Berberis aquifolium. Oxyacanthine inhibits the gene expression of pro-inflammatory cytokines IL-6 and IL-1β. Oxyacanthine exhibits anti- SARS-CoV-2 activity. Oxyacanthine is applicable to research related to COVID-19 [1] [2].
In Vivo, Oxyacanthine (2.5-10 mg/kg; i.v., p.o.; single dose) exhibits an oral bioavailability of 34.5% in male Mus musculus, with a shorter T1/2 following oral (6.39 h) versus intravenous (13.20 h) single-dose administration[2].
In Vitro, Oxyacanthine (10 μM; 2 h pre-incubation, followed by 12 h co-incubation with LPS) potently suppress LPS-induced IL-6 and IL-1β gene expression in RAW 264.7 murine macrophages, with greater activity than berbamine[1]. Oxyacanthine (10-50 μM; 48 h) exhibits greater cytotoxicity than select synthetic intermediates in HepG2 and HEK293 cells[1]. Oxyacanthine (24 h) inhibits SARS-CoV-2 replication in Vero E6 cells with an anti-virus IC50 of 14.50 μM, and exhibits cytotoxicity in Vero E6 cells with an IC50 of 29.94 μM[2].
References:
[1]. Xiang L, et al. Asymmetric Total Synthesis and Anti-Inflammatory Activity of Berbamine, Oxyacanthine, and Related Intermediates. Journal of natural products. 2025 Dec 26;88(12):2947-2959.
[2]. Lu J, et al. Design, synthesis, and evaluation of novel oxyacanthine derivatives for anti-SARS-CoV-2 activity. Bioorganic & medicinal chemistry letters. 2024 Nov 15;113:129951.
In Vivo, Oxyacanthine (2.5-10 mg/kg; i.v., p.o.; single dose) exhibits an oral bioavailability of 34.5% in male Mus musculus, with a shorter T1/2 following oral (6.39 h) versus intravenous (13.20 h) single-dose administration[2].
In Vitro, Oxyacanthine (10 μM; 2 h pre-incubation, followed by 12 h co-incubation with LPS) potently suppress LPS-induced IL-6 and IL-1β gene expression in RAW 264.7 murine macrophages, with greater activity than berbamine[1]. Oxyacanthine (10-50 μM; 48 h) exhibits greater cytotoxicity than select synthetic intermediates in HepG2 and HEK293 cells[1]. Oxyacanthine (24 h) inhibits SARS-CoV-2 replication in Vero E6 cells with an anti-virus IC50 of 14.50 μM, and exhibits cytotoxicity in Vero E6 cells with an IC50 of 29.94 μM[2].
References:
[1]. Xiang L, et al. Asymmetric Total Synthesis and Anti-Inflammatory Activity of Berbamine, Oxyacanthine, and Related Intermediates. Journal of natural products. 2025 Dec 26;88(12):2947-2959.
[2]. Lu J, et al. Design, synthesis, and evaluation of novel oxyacanthine derivatives for anti-SARS-CoV-2 activity. Bioorganic & medicinal chemistry letters. 2024 Nov 15;113:129951.