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.

Effects of brucine combined with glycyrrhetinic acid or liquiritin on rat hepatic cytochrome P450 activities in vivo.

Abstract: Abstract: The activities of four CYP450 enzymes (CYP3A, 1A2, 2El and 2C) and the mRNA expression levels of CYP1A2, 2El, 2Cll and 3A1 in rat liver were determined after Wistar rats were orally administered with brucine (BR) at three dosage levels (3, 15 and 60 mg.kg-1 per day) and the high dose of BR combined with glycyrrhetinic acid (GA, 25 mg.kg-1 per day) or liquiritin (LQ, 20 mg.kg-1 per day) for 7 consecutive days. Compared with the control, brucine caused 24.5% and 34.6% decrease of CYP3A-associated testosterone 6beta-hydroxylation (6betaTesto-OH) and CYP2C-associated tolbutamide hydroxylation (Tol-OH), respectively, and 146.1% increase of CYP2El-associated para-nitrophenol hydroxylation (PNP-OH) at the high dose level. On the other hand, (BR+GA) caused 51.4% and 33.5% decrease, respectively, of CYP2El-associated PNP-OH and CYP1A2-associated ethoxyresorufin-O-de-ethylation (EROD) as compared with the high dose of BR group. Meanwhile, (BR+LQ) caused 41.1% decrease of CYP2El-associated PNP-OH and 37.7% increase of CYP2C-associated Tol-OH. The results indicated that the co-administration of BR with GA or LQ had effect on mRNA expression and activities of the CYP450 enzymes mentioned above to some extent, and the in vivo antagonism of LQ on BR-induced CYPs adverse effects and the in vivo inhibitory action of GA on CYP2E1 and 1A2 might play an important role in the detoxification of Radix Glycyrrhizae against Strychnos nux-vomica L.

Relation of Vomicine to Strychnine and Brucine

Abstract: VOMICINE, C22H24O4N2, a congener of strychnine, C21H22O2N2, has been investigated by Wieland and his collaborators ; but no precise connexion between the alkaloids has yet been disclosed, though many reactions and transformations suggest the close similarity of their molecular structure. On oxidation with chromic acid1, vomicine yields an acid, C17H22O5N2, 3H2O, which characteristically loses carbon dioxide at 130°, affording a base, C16H22O2N2. We have now found that the same acid can be obtained by oxidation of N-methyl-sec-pseudo-strychnine, or better, H-methyl-sec-pseudobrucine, by means of chromic acid. The identity has not yet been confirmed by direct comparison* ; but there can be little doubt of it from the analyses (3H2O), rotatory power, melting points, and behaviour on heating. The resulting base has the composition, melting point and crystalline form recorded for the product from vomicine.

Capillary Coated with Graphene Oxide as Stationary Phase for the Separation of Brucine and Strychnine by Capillary Electrophoresis

Abstract: A new capillary electrophoresis (CE) method was developed by using graphene oxide (GO) as a stationary phase for the separation of brucine and strychnine. The separation performance, reproducibility and stability of GO-coated capillary were investigated for the analysis of brucine and strychnine. After optimization of the separation conditions, a phosphate solution (40 mM, pH 7.0) containing 25% (v/v) acetonitrile was selected as the running buffer. Compared with uncoated capillary, higher separation efficiency was achieved by GO-coated capillary as a result of the increasing interactions between the analytes and the stationary phase of capillary. The linear ranges of these two alkaloids were 4.0-100.0 μg mL(-1) with a satisfied correlation coefficients (R > 0.9994), and this novel method provided an efficient separation of brucine and strychnine as well as a good reproducibility and stability. Finally, the developed method was successfully applied for the determination of these two alkaloids in a pharmaceutical formulation of traditional Chinese medicines.

In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine.

Abstract: In this study, a novel NGR (Asn-Gly-Arg) peptide-modified liposomal brucine was prepared by using spray-drying method. The surface morphology of the liposomes, encapsulation efficiency and particle size were investigated. The data showed that the addition of NGR did not produce any significant influence on brucine liposomes in terms of particle size or zeta potential. In addition, after 3 months of storage, no dramatic change such as visible aggregation, drug content changes or precipitation in the appearance of NGR-brucine liposomes occurred. The in vitro release results indicated that the release of brucine from NGR liposomes was similar to that of liposomes, demonstrating that the NGR modification did not affect brucine release. The in vitro drug-release kinetic model of NGR-brucine liposomes fitted well with the Weibull's equation. In vivo, NGR-brucine liposomes could significantly extend the bioavailability of brucine; however, there was no significant difference observed in the pharmacokinetic parameters between liposomes and NGR liposomes after intravenous administration. Antitumor activity results showed that NGR-modified liposomes exhibited less toxicity and much higher efficacy in HepG2-bearing mice compared with non-modified liposomes. The enhanced antitumor activity might have occurred because brucine was specifically recognized by NGR receptor on the surface of tumor cells, which enhanced the intracellular uptake of drugs.