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. 2014 Apr 10;19(4):4395-408.
doi: 10.3390/molecules19044395.

Pharmacological evaluation of total alkaloids from nux vomica: effect of reducing strychnine contents

Jun Chen  1 , Yange Qu  1 , Dongyue Wang  1 , Pei Peng  1 , Hao Cai  1 , Ying Gao  1 , Zhipeng Chen  1 , Baochang Cai  2
Affiliations

Pharmacological evaluation of total alkaloids from nux vomica: effect of reducing strychnine contents

Jun Chen et al. Molecules. .

Abstract

The aim of the study was to investigate the possibility of improving the therapeutic efficacy of the total alkaloid fraction (TAF) extracted from processed nux vomica by reducing the strychnine contents. Most strychnine was removed from TAF to obtain the modified total alkaloid fraction (MTAF). The toxicity and pharmacokinetics of TAF and MTAF were further investigated and compared besides their antitumor, analgesic and anti-inflammatory activities. The results showed that the ratios of brucine to strychnine were 1:2.05 and 2.2:1 for TAF and MTAF, respectively, and the toxicity of TAF was about 3.17-fold higher than that of MTAF. Compared to brucine alone, the elimination of brucine was found to be inhibited by other alkaloids in TAF or MTAF except strychnine. Significantly increased pharmacological activities when administered by the oral route were obtained with MTAF in comparison to TAF and nux vomica powder (NVP). In summary, MTAF might replace NVP and TAF in the clinical application of Chinese medicine to obtain much higher efficacy.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structures of strychnine and brucine.
Figure 2
Figure 2
HPLC chromatographs of standard solution (A), TAF (B) and MTAF (C). Peaks: 1. Brucine; 2. Strychnine; 3. Brucine N-oxide.
Figure 3
Figure 3
Plasma concentration versus time profile of brucine after oral administration of brucine, TAF and MTAF at the brucine dose of 1 mg/kg to rats (n = 6).
See this image and copyright information in PMC

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