Topic
Brucine
About: Brucine is a research topic. Over the lifetime, 586 publications have been published within this topic receiving 6866 citations. The topic is also known as: 10,11-dimethoxy strychnine.
Papers published on a yearly basis
Papers
More filters
••
TL;DR: The proposed method was successfully applied to determine non-protein-bound strychnine and Bru, and the analysates concentration remained stable in rabbit muscle and synovial fluid after topical application of total Strychnos alkaloid patches, which indicated that totalStrychno alkaloids patches could substitute for the traditional oral administration of Semen Stychni.
Abstract: Semen Strychni, a known toxic drug in Chinese pharmacopoeia, is notable for its therapeutic effects on local muscle and joint pain. However, oral administration can be risky. Topically administered drugs accumulate in the topical muscles and knee joints without any major increase in plasma levels; only non-protein-bound drugs in the biological fluids of target tissues are effective for therapeutic effects. A sensitive and rapid ultra performance liquid chromatography - mass spectrometry (UPLC-MS) method coupled with a microdialysis technique was developed to determine the non-protein-bound strychnine (Str) and brucine (Bru) in rabbit muscle and synovial fluid microdialysate. The UPLC separation was carried out using a 1.7μm BEH C18 column (50 mm × 2.1 mm) with a mobile phase consisting of methanol: water (29.5:70.5, v/v) with 0.1% formic acid and 20 mM ammonium acetate in water. The method was validated at concentrations ranging from 0.58 ng/ml to 467.20 ng/ml for Str and from 0.42 ng/ml to 422.40 ng/ml for Bru. Intra-day and inter-day accuracy ranged from 99.1% to 103.2% for Str and from 95.8% to 108.8% for Bru with intra-day and inter-day precision within 9.7%. The proposed method was successfully applied to determine non-protein-bound Str and Bru, and the analysates concentration remained stable in rabbit muscle and synovial fluid after topical application of total Strychnos alkaloid patches, which indicated that total Strychnos alkaloid patches could substitute for the traditional oral administration of Semen Strychni. Copyright © 2013 John Wiley & Sons, Ltd.
8 citations
••
TL;DR: A sensitive and simple rapid-resolution liquid chromatography/tandem mass spectrometry method was developed and successfully applied to the toxicokinetic study of strychnine and brucine after single and multiple oral administration of Biqi capsule to male and female rats, which showed different toxicokinetics characteristics in the different groups.
Abstract: Biqi capsule is a well-known traditional Chinese medicine (TCM) formula that has been widely applied for the clinical treatment of such diseases as rheumatoid arthritis, scapulohumeral periarthritis, and cervical spondylopathy. However, there is concern regarding the toxicity of Biqi capsule due to its active ingredients, strychnine and brucine. To investigate the toxicokinetics of strychnine and brucine after the oral administration of Biqi capsule to rats, a sensitive and simple rapid-resolution liquid chromatography/tandem mass spectrometry (RRLC-MS/MS) method was developed to determine the levels of strychnine and brucine in rat plasma. Chromatographic separation was performed on a CAPCELL PAK C18 MG II (3.0 μm, 2.0×35 mm) column by gradient elution with acetonitrile and 0.2% formic acid as the mobile phase. The method was validated over the range of 0.25 to 250 ng/mL for strychnine and 0.025 to 25 ng/mL for brucine. The intra- and inter-day accuracies of strychnine and brucine in rat plasma were 100.3%-106.6% and 90.75%-106.1% respectively, and the precisions were within 14.2%. The established method was successfully applied to the toxicokinetic study of strychnine and brucine after single and multiple oral administration of Biqi capsule to male and female rats at 0.4-, 0.8-, and 1.6-g/kg doses. The results showed different toxicokinetic characteristics in the different groups.
8 citations
••
TL;DR: BNO administration dose-dependently attenuated alcohol consumption without affecting food intake, total fluid consumption or the natural preference for a sucrose solution, with 70 mg/kg BNO reducing consumption by 22.8%.
Abstract: Background Alcohol use disorder places a heavy burden on global public health systems and thus is in urgent need of improved pharmacotherapies. Previously, our group has demonstrated that 30 mg/kg of the indole alkaloid brucine significantly attenuates alcohol-drinking behavior; however, the high toxicity, poor water solubility, short half-life, and limited therapeutic window of brucine restrain its clinical application as an antialcoholism medication. We subsequently hypothesized that the oxide of brucine (brucine N-oxide) would produce a similar behavioral effect without the risk profile associated with brucine. Methods Male Fawn-Hooded rats with high innate alcohol preference underwent 2-bottle choice procedures (Experiments 1 to 3). Experiment 1 examined the effects of 7 daily BNO injections of 0, 30, 50, or 70 mg/kg (s.c.) on voluntary alcohol consumption (n = 9/group). Experiment 2 evaluated the impact of a single dose of 0 or 70 mg/kg BNO on the increased alcohol intake induced by a 4-day alcohol deprivation (n = 8/group). Experiment 3 tested the effect of 7 daily BNO injections of 0 or 70 mg/kg (s.c.) on sucrose preference (n = 6/group). Experiment 4 measured the median lethal dose (LD50) values of BNO and brucine to compare their acute toxicity in rats. Experiment 5 tested whether BNO (0, 30, 50, and 70 mg/kg, s.c.) affected locomotor activity using an open-field paradigm (n = 8/group). Finally, Experiment 6 evaluated the possible conditioned rewarding effects of 0, 30, 50, and 70 mg/kg BNO using the conditioned place preference paradigm (n = 6/group). Results BNO administration dose-dependently attenuated alcohol consumption without affecting food intake, total fluid consumption, or the natural preference for a sucrose solution, with 70 mg/kg BNO reducing consumption by 22.8%. A single dose of 70 mg/kg BNO significantly inhibited the alcohol deprivation effect. The LD50 values of BNO and brucine in rats were determined to be 1,103.5 ± 177.0 mg/kg and 264.6 ± 17.7 mg/kg, respectively. Finally, BNO administration did not affect spontaneous locomotor activity or induce a place preference. Conclusions BNO may help to control excessive alcohol use and should be considered a treatment strategy for future study and development.
8 citations
••
TL;DR: In this article, a rapid and simple spectrophotometric procedure is described for the determina- tion of ajmaline and brucine, which is based on the development of blue coloured product due to reduction of tungstate and/or molybdate in Folin Ciocalteu's reagent (FCR) in alkaline medium.
Abstract: A rapid and simple spectrophotometric procedure is described for the determina- tion of ajmaline and brucine. The method is based on the development of blue coloured product due to reduction of tungstate and/or molybdate in Folin Ciocalteu's reagent (FCR) by ajmaline and brucine in alkaline medium. The colour is stable for more than 48 h. The chromogenic reaction hasmax at 540 nm with molar absorptivity 1.64 10 4 and 2.37 10 3 l mol -1 cm -1 in the Beer's law range 1-8 gm l -1 and 10-100 gm l -1 for ajmaline and brucine, respectively.
8 citations
•
TL;DR: The analytical results showed that the contents of strychnine and brucine in samples showed great difference between different species, and show that the two Strychnos species may be developed as the resources of stRYchnine.
Abstract: This paper describes the determination of strychnine and brucine in the seeds, root, stem and leaves of Strychnos species by HPLC. The analytical column used was ZY110 YNG-C18. The mobile phase was KH2PO4(0.01 mol.L-1)--MeOH(73:27), pH2.5, regulated by 10% H3PO4. Flow rate was 1.0 ml.min-1. The detection wavelength was 264 nm. The linear ranges of strychmine and brucine were 0.18-7.26 micrograms and 0.11-4.32 micrograms, respectively. The recoveries of strychnine and brucine were 98.27% and 98.04%, respectively. The analytical results showed that the contents of strychnine and brucine in samples showed great difference between different species. The contents of strychnine in the seeds of Strychnos wallichiana and S. ignatii were 5.6% and 3.9%, respectively. These results show that the two Strychnos species may be developed as the resources of strychnine.
8 citations