A diterpene alkaloid with diverse biological activities
3-Acetylaconitine is a diterpene alkaloid that has been found in Aconitum and has diverse biological activities.1,2 It is cytotoxic to P388 leukemia cells (IC50 = 18.6 ?M).1 It inhibits brevetoxin binding to (IC50 = 1.3 ?M), and increases free sodium and calcium concentrations in, rat brain synaptosomes. 3-Acetylaconitine (60-100 nM) induces arrhythmia in isolated guinea pig atria.2 In vivo, 3-acetylaconitine (100 ?g/kg, i.v.) reduces paw licking, flicking, and shaking in a mouse model of formalin-induced inflammatory pain.
1.He, Y.-Q., Yao, B.-H., and Ma, Z.-Y.Diterpenoid alkaloids from a Tibetan medicinal plant Aconitum richardsonianum var. pseudosessiliflorum and their cytotoxic activityJ. Pharm. Anal.1(1)57-59(2011) 2.Gutser, U.T., Friese, J., Heubach, J.F., et al.Mode of antinociceptive and toxic action of alkaloids of Aconitum specNaunyn Schmiedebergs Arch. Pharmacol.375(1)39-48(1997)
Cell experiment: | The assay is performed following a standard published procedure using microtiter plate format and sulforhodamine B standing at the end point. The leukemic cells (P388) are exposed to Flaconitine (3-Acetylaconitine) for three days. Cells are grown and maintained in an incubator set at 37°C, 5% CO2 and 95% humidity. RPMI-1640 media supplemented with 10% fetal calf serum (FCS) and 0.5% trypsin are used to culture P388 cells[2]. |
参考文献: [1]. Dong L, et al. Identification of nuclear factor-κB inhibitors and β2 adrenergic receptor agonists in Chinese medicinal preparation Fuzilizhong pills using UPLC with quadrupole time-of-flight MS. Phytochem Anal. 2014 Mar-Apr;25(2):113-21. | |
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