Benzoylmesaconitine/(1α,3α,6α,14α,15α,16β)-3,8,13,15-Tetrahydroxy-1,6,16-trimethoxy-4-(methoxymethyl)-20-methylaconitan-14-yl benzoate/O8-Deacetylmesaconitine/Mesaconine 14-benzoate/8-Deacetylmesaconitine/Benzoylmesaconine/Aconitane-3,8,13,14,15-pentol, 1,6,16-trimethoxy-4-(methoxymethyl)-20-methyl-, 14-benzoate, (1α,3α,6α,14α,15α,16β)-
703.2±60.0 °C at 760 mmHg
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Wutou decoction is widely used in China because of its therapeutic effect on rheumatoid arthritis. Benzoylmesaconine (BMA), the most abundant component of Wutou decoction, was used as the marker compound for the pharmacokinetic study of Wutou decoction. The aim of the present study was to compare the pharmacokinetics of BMA in rats after oral administration of pure BMA and Wutou decoction. Pure BMA (5 mg/kg) and Wutou decoction (0.54 g/kg, equivalent to 5 mg/kg BMA) were orally administered to rats with blood samples collected over 10 h. Quantiﬁcation of BMA in rat plasma was achieved using sensitive and validated ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Specifically, the half-life (T1/2) and mean residence time values of pure BMA were 228.3 ± 117.0 min and 155.0 ± 33.2 min, respectively, whereas those of BMA in Wutou decoction were decreased to 61.8 ± 35.1 min and 55.8 ± 16.4 min, respectively. The area under the curve (AUC) of BMA after administration of Wutou decoction was significantly decreased (five-fold) compared with that of pure BMA. The results indicate that the elimination of BMA in rats after the administration of Wutou decoction was significantly faster compared with that of pure BMA.
Pharmacokinetic comparisons of benzoylmesaconine in rats using ultra-performance liquid chromatography-tandem mass spectrometry after administration of pure benzoylmesaconine and Wutou decoction.
Dai PM1, Wang Y2, Ye L3, Zeng S4, Zheng ZJ5, Li Q6, Lu LL7, Liu ZQ8.
2014 Oct 17
We explored the possible role of the specific regions in the brain stem on the antinociceptive actions of mesaconitine (MA) and benzoylmesaconine (BM) by the microinjection of MA and BM into nucleus reticularis paragigantocellularis (NRPG), nucleus raphe magnus (NRM), and periaqueductal gray (PAG). MA microinjected into NRPG, NRM, or PAG elicited a dose-dependent antinociceptive action, whereas BM injected into NRM or PAG elicited a dose-dependent antinociceptive action but not in NRPG. The NRM appeared to be the most sensitive region among the three tested locations.
Antinociceptive mechanism of the aconitine alkaloids mesaconitine and benzoylmesaconine.
Suzuki Y1, Oyama T, Ishige A, Isono T, Asami A, Ikeda Y, Noguchi M, Omiya Y.
As compared with normal unburned mice, thermally injured mice have been shown to be 50-100 times more susceptible to HSV type 1 (HSV-1) or Candida albicans infection. Benzoylmesaconine (BEN) improved the resistance of thermally injured mice against infection with HSV-1 or C. albicans to the level observed in normal mice. Mortality rates of normal mice exposed to lethal amounts of these pathogens were not affected by the BEN treatment, while significant survival effects were produced in these mice after treatment with acyclovir (against HSV-1) or amphotericin B (against C. albicans). Benzoylmesaconine did not inhibit the growth of these pathogens in vitro and did not directly reduce the viability of the pathogens. However, burned mice inoculated with CD4+ T cells from BEN-treated mice resisted infections from these pathogens. These results suggested that, through the generation of CD4+ T cells, BEN recovered the impaired resistance of thermally injured mice to infection by HSV-1 or C. albicans.
The regulation of burn-associated infections with herpes simplex virus type 1 or Candida albicans by a non-toxic aconitine-hydrolysate, benzoylmesaconine. Part 1: Antiviral and anti-fungal activities in thermally injured mice.
Kobayashi M1, Mori K, Kobayashi H, Pollard RB, Suzuki F.
Benzoylmesaconine is the most abundant component of Wutou decoction, which is widely used in China because of its therapeutic effect on rheumatoid arthritis.