Abstract

Brucine, a weak alkaline indole alkaloid, is one of the main bioactive and toxic constituents of Nux-vomica. Modern pharmacology studies and clinical practice demonstrate that brucine possesses wide pharmacological activities, such as anti-tumor, anti-inflammatory, analgesic, and the effects on cardiovascular system and nervous system, etc. However, its central nervous system toxicity severely limits its clinical application. Herein, the physicochemical properties, pharmacological activities, and toxicity of brucine were reviewed, and the novel strategies to address the toxicity issues were discussed, aiming to bring new insights into further research and application of this active component.

Highlights

  • Brucine is extracted from the seeds of Strychnos nux-vomica L. (Loganiaceae), which are commonly known as Nux-vomica (Maqianzi) with bitter taste and high toxicity

  • In order to better understand the pharmacological and toxicological effects of brucine and provide theoretical basis for its future application, we summarized the physicochemical properties, pharmacological activities, and toxicity of brucine here

  • By observing the effect of brucine on MDA-MB-231 and Hs578-T cell lines, as well as the expression of epithelial-tomesenchymal transition (EMT) markers and matrix metalloproteinase (MMPs), studies found that the ability of migration, invasion or adhesion of MDA-MB-231, and Hs578T cells decreased in a dose-dependent manner when treated with brucine (Li et al, 2018). These results proved the inhibitory effects of brucine on the bone metastasis of breast cancer

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Summary

INTRODUCTION

Brucine is extracted from the seeds of Strychnos nux-vomica L. (Loganiaceae), which are commonly known as Nux-vomica (Maqianzi) with bitter taste and high toxicity. Brucine is extracted from the seeds of Strychnos nux-vomica L. In China, Nux-vomica has a long history to use for the treatment of different kinds of ailments, such as dyspepsia, nervous system diseases, and chronic rheumatism (Guo et al, 2018). Brucine and their nitrogen are the main constituents of Nux-vomica. Brucine (2, 3-dimethoxystrychnidin-10-one,C23H26N2O4), a weak alkaline indole alkaloid, is white crystalline powder with a molecular weight of 394. It can be dissolved in organic solvents such as ether, chloroform, ethanol, and methanol but not in water. The Cambridge Structural Database (CSD) has collected different crystal forms of brucine including two anhydrous forms (Figure 1) (Groom et al, 2016)

Extraction and Purification
QUANTITATIVE ANALYSIS OF BRUCINE
PHARMACOLOGICAL ACTIVITIES
Metastasis inhibition Intervention in cell signal transduction
Effects on Cardiovascular System
Other Pharmacological Activities

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