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Showing papers on "Brucine published in 2017"


Journal ArticleDOI
TL;DR: The method was successfully applied for the detection of brucine in traditional pharmaceutical formulations and demonstrated by the analysis of the alkaloid in human serum and urine samples exhibiting considerable potential as a diagnostic tool.

32 citations


Journal ArticleDOI
TL;DR: Results showed that the brucine gel system inhibited arthritis symptoms and the proliferation of the synoviocytes in the rat adjuvant arthritis model, which indicated its curative effect for rheumatoid arthritis.
Abstract: The seeds of Strychnos nux-vomica L., as a traditional Chinese medicine, have good anti-inflammatory and analgesic activities. However, it usually leads to gastrointestinal irritation and systemic toxicity via oral administration. In the study, it was discovered that a novel gel transdermal delivery system contained brucine, the main effective component extracted from Strychnos nux-vomica. Results showed that the brucine gel system inhibited arthritis symptoms and the proliferation of the synoviocytes in the rat adjuvant arthritis model, which indicated its curative effect for rheumatoid arthritis. Meanwhile, it significantly relieved the xylene-induced ear edema in the mouse ear swelling test, which manifested its anti-inflammatory property. Moreover, the brucine gel eased the pain of paw formalin injection in the formalin test, which demonstrated its analgesic effects. In addition, the brucine significantly inhibited lipopolysaccharide (LPS)-induced Prostaglandin E2 (PGE2) production without affecting the viability of cell in vitro anti-inflammatory test, which proved that its anti-inflammatory and analgesic actions were related to inhibition of prostaglandin synthesis. It is suggested that the brucine gel is a promising vehicle for transdermal delivery on the treatment of inflammatory disease.

24 citations


Journal ArticleDOI
TL;DR: An in vitro assay system was developed and optimized in vitro reaction conditions for N‐glucuronidation by using specific substrates and it was found that hepatic N‐ glucuronisation showed significant species differences.

23 citations


Journal ArticleDOI
TL;DR: Brucine may inhibit osteoclastogenesis by suppressing Jagged1/Notch1 signaling pathways by inhibited RANKL-induced osteOClastogenesis and bone resorption of RAW264.7 macrophages cells.
Abstract: To examine the effects of brucine on the invasion, migration and bone resorption of receptor activator of nuclear factor-kappa B ligand (RANKL)-induced osteoclastogenesis. The osteoclastogenesis model was builded by co-culturing human breast tumor MDA-MB-231 and mouse RAW264.7 macrophages cells. RANKL (50 ng/mL) and macrophage-colony stimulating factor (50 ng/mL) were added to this system, followed by treatment with brucine (0.02, 0.04 and 0.08 mmol/L), or 10 μmol/L zoledronic acid as positive control. The migration and bone resorption were measured by transwell assay and in vitro bone resorption assay. The protein expressions of Jagged1 and Notch1 were investigated by Western blot. The expressions of transforming growth factor-β1 (TGF-β1), nuclear factor-kappa B (NF-κB) and Hes1 were determined by enzyme-linked immunosorbent assay. Compared with the model group, brucine led to a dose-dependent decrease on migration of MDA-MB-231 cells, inhibited RANKL-induced osteoclastogenesis and bone resorption of RAW264.7 cells (P<0.01). Furthermore, brucine decreased the protein levels of Jagged1 and Notch1 in MDA-MB-231 cells and RAW264.7 cells co-cultured system as well as the expressions of TGF-β1, NF-κB and Hes1 (P<0.05 or P<0.01). Brucine may inhibit osteoclastogenesis by suppressing Jagged1/Notch1 signaling pathways.

18 citations


Journal ArticleDOI
TL;DR: In this article, the authors used ultra-high performance liquid chromatography with tandem mass spectrometry and dispersive solid-phase extraction to detect nine analytes (scopolamine, cephaeline, strychnine, hyoscyamine, brucine, hydrastine, ajmalicine, colchicine and oleandrin) in herbal cosmetics.
Abstract: We utilized ultra-high performance liquid chromatography with tandem mass spectrometry and dispersive solid-phase extraction to develop a new method for the detection of nine analytes (scopolamine, cephaeline, strychnine, hyoscyamine, brucine, hydrastine, ajmalicine, colchicine, and oleandrin) in herbal cosmetics. Acetonitrile/water and 2-propylaminoethylamine were used to disperse and purify during the dispersive solid-phase extraction step. The analytes were separated by a Waters UPLC HSS T3 column and detected through electrospray ionization source in the positive mode with multi-reaction monitoring conditions. Under the optimal conditions, the calibration curves were linear in the range of 0.2-100.0 μg/L with the correlation coefficients higher than 0.995. The method limit of quantitation (S/N = 10) were 5.0 μg/kg for oleandrin and 1.0 μg/kg for the other eight alkaloids. The mean recoveries at three spiked concentration levels of 1.0-10.0 μg/kg were in the range of 86.9-116.5% with the intra-day relative standard deviations (n = 6) ranging from 2.4 to 8.8%, and inter-day relative standard deviations ranging from 2.7 to 5.7%. This method is accurate, simple and rapid, and has been applied to the quality supervision of herbal cosmetics in Guangzhou.

15 citations


Journal ArticleDOI
Shu Li1, Xi-Peng Wang1
TL;DR: In vivo, NGR-brucine liposomes could significantly extend the bioavailability of brucine; however, there was no significant difference observed in the pharmacokinetic parameters betweenliposomes and NGR liposome after intravenous administration.
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.

14 citations


Journal ArticleDOI
TL;DR: This work will provide supportive data on how the brucine is better used for transdermal drug delivery (TDD) and show that under ultrasonic conditions, the permeability of the skin to the fluorescent label and bru cine is increased compared to its passive diffusion permeability.
Abstract: Brucine is the active component in traditional Chinese medicine “Ma-Qian-Zi” (Strychnos nux-vomica Linn), with capabilities of analgesic, anti-inflammatory, anti-tumor and so on. It is crucial how to break through the impact of cuticle skin which reduces the penetration of drugs to improve drug transmission rate. The aim of this study is to improve the local drug concentration by using ultrasound. We used fresh porcine skin to study the effects of ultrasound on the transdermal absorption of brucine under the influence of various acoustic parameters, including frequency, amplitude and irradiation time. The transdermal conditions of yellow-green fluorescent nanoparticles and brucine in skin samples were observed by laser confocal microscopy and ultraviolet spectrophotometry. The results show that under ultrasonic conditions, the permeability of the skin to the fluorescent label and brucine (e.g., the depth and concentration of penetration) is increased compared to its passive diffusion permeability. The best ultrasound penetration can make the penetration depth of more than 110 microns, fluorescent nanoparticles and brucine concentration increased to 2-3 times. This work will provide supportive data on how the brucine is better used for transdermal drug delivery (TDD).

11 citations


Journal ArticleDOI
TL;DR: In this paper, a nanomaterial comprising Fe3O4-modified hydroxylated multi-walled carbon nanotubes was used to determine brucine in human urine.
Abstract: A nanomaterial comprising Fe3O4-modified hydroxylated multi-walled carbon nanotubes (Fe3O4–MWCNTs–OH) was prepared by a co-precipitation method. Combined with HPLC-photodiode array detector (DAD), Fe3O4–MWCNTs–OH was used to determine brucine in human urine. Some important parameters that could influence extraction efficiency of brucine were optimized, including the extraction time, amounts of Fe3O4–MWCNTs–OH, pH of sample solutions, desorption solvent and desorption time. Under the optimal conditions, the recoveries of brucine from spiked urine samples were between 93.1 and 104.1%, and the relative standard deviations (RSDs) ranged from 3.1 to 5.7%. The correlation coefficient was 0.9997. The limits of detection and quantification were 6 and 21 ng/mL at a signal-to-noise ratio of 3 and 10, respectively. The results indicated that Fe3O4–MWCNTs–OH combined with HPLC–DAD is a promising solid-phase extraction material for the sample pretreatment in the determination of brucine.

9 citations


Journal ArticleDOI
TL;DR: Results suggest that TGP possesses renoprotective effects against nephrotoxicity induced by total alkaloids from Semen Strychni, and showed that pretreatment with TGP could attenuate the absorption of strychnine and brucine as well as accelerate their elimination.
Abstract: Semen Strychni have been shown to have therapeutic effect in improving blood circulation, relieving rheumatic pain, and treating cancer. However, Semen Strychni could cause severe nephrotoxicity. The present study was designed to evaluate whether treatment with total glucosides from paeony (TGP) has renoprotective effect against nephrotoxicity induced by total alkaloids from Semen Strychni (TAS). The levels of blood urea nitrogen (BUN) and creatinine (Cr) were determined and histopathological changes were also examined to evaluate renal injury. Moreover, a HPLC-MS method was developed and validated to investigate the comparative toxicokinetics of strychnine and brucine in rats plasma after oral administration of TAS and pretreatment with TGP. Results demonstrated that the levels of BUN and Cr were significantly increased (p < 0.05) in TAS group, together with tubule epithelium cloudy swelling, degeneration, and glomerular atrophy in rats' kidneys. The TAS-induced kidney damage was alleviated after pretreatment with TGP. Besides, Tmax of strychnine and brucine were increased and T1/2 of strychnine and brucine were decreased after pretreatment with TGP. The toxicokinetics study showed that pretreatment with TGP could attenuate the absorption of strychnine and brucine, as well as accelerate their elimination. These results suggest that TGP possesses renoprotective effects.

4 citations


Journal ArticleDOI
TL;DR: In this article, a diastereomeric salt formation with brucine has been resolved for the first time by X-ray crystallography of the correspo-...
Abstract: Thiele’s acid has been resolved for the first time by diastereomeric salt formation with brucine. Determination of absolute stereochemistry was accomplished by X-ray crystallography of the correspo...

3 citations


Journal ArticleDOI
TL;DR: This paper compares the efficacy and adverse reactions between brucine related preparations and traditional drugs to evaluate its anti-tumor effects and concludes that more exploration on the inhibiting mechanisms is necessary for the patients to obtain safe and effective drugs.
Abstract: The inhibiting mechanisms of brucine to cancer cells included inducing the apoptosis of cancer cells, inhibiting the proliferation of cancer cells, preventing cell adhesion and transfer. This paper reviews the function of brucine and its anti-tumor preparations, and compares the efficacy and adverse reactions between brucine related preparations and traditional drugs to evaluate its anti-tumor effects. Furthermore, more exploration on the inhibiting mechanisms is necessary for the patients to obtain safe and effective drugs. Key words: Anti-neoplastic angets, phytogenic; Brucine; Preparations; Drug therapy

Journal Article
TL;DR: Twenty one medicinal bio active compounds were identified from the Strychnos nux-vomica leaf ethanolic extract, having natural properties of Anti-inflammatory, Hypocholesterole, Cancer preventive, Hepatoprotective, Antimicrobial, Antioxidant, Cardio protective, Antiaging, Antialzheimeran, Antidermatitic, Immunostimulant and more.
Abstract: In this study, we have aimed to analyze the phytochemical composition of this plant and the concentration of strychnine and brucine. The identification of bioactive compounds was done by GC-MS with NIST Library. Strychnine and Brucine were quantified using HPLC. Twenty one medicinal bio active compounds were identified from the Strychnos nux-vomica leaf ethanolic extract. Strychnine is showing 28.43% purity and brucine was not detected in GCMS analysis. Quantified the concentration of strychnine (0.6 mg in 500mg of extract) and brucine (1.6 mg in 500mg of extract) was done by HPLC against Strychnine and Brucine standard. These compounds are having natural properties of Anti-inflammatory, Hypocholesterole, Cancer preventive, Hepatoprotective, Antimicrobial, Antioxidant, Cardio protective, Antiaging, Antialzheimeran, Antidermatitic, Immunostimulant, Anthepatotoxic, biosynthesis of steroid hormones, Nematicide, Antiandrogenic, 5-alpha reductase inhibitor, antipsychotic, analgesic, apoptotic effect, antidepressant, antidote for snake poisoning and diabetic activity.

Journal Article
TL;DR: In this article, Strychnos-nux-vomica leaves are extracted with 50% Ethanol in a water and centrifuged at 3000 rpm for 5min for analysis.
Abstract: Strychnos Nux-Vomica is a remedial plant used in herbal medicine and medicinal plants is having a curative history and are still helping healthiness requirements of a large population in the world. Therapeutic plants are used to cure various diseases, these are the phytochemicals extracted from plants. Strychnos-nux-vomica is having Strychnine and Brucine with biological properties. However, qualitative and quantification of the compounds in plant extract is determined by using chromatography techniques. The method HPTLC is used in identification, standardization and quantification of bioactive Phytoconstituent in plant extract and these extracts helpful in medications. Strychnos Nux-vomica leaves are extracted with 50% Ethanol in a water and centrifuged at 3000 rpm for 5min for analysis. 3 µl of Sample S and 2 µl of standard solution were loaded in CAMAG LINOMAT 5 instrument and scanning done at UV 254nm. The Mobile phase is used ratio of Toluene – Ethyl acetate – Diethyl amine (7:2:1) and Dragendorff's reagent is used as spraying for spot development. HPTLC chromatograms shows the Strychnine, Brucine and eight unknown compounds. Strychnine, Brucine Rf values are 0.50, 0.33 and values of the area is 16667.7 and 13826.4.