Showing papers on "Brucine published in 2012"

Electrochemical sensor for the determination of brucine in human serum based on molecularly imprinted poly-o-phenylenediamine/SWNTs composite film

Abstract: A sensitive and selective sensor was successfully developed by integrating electropolymerization of molecularly imprinted polymer (MIP) with single-wall carbon nanotubes (SWNTs) for the determination of brucine in human serum. The imprinted poly-o-phenylenediamine (PoPD), which was embedded in SWNTs surface, functioned as a selective recognition element for brucine determination. The introduction of SWNTs into the polymer composite could enhance the electrical response by facilitating charge–transfer processes of brucine which was imprinted or rebinded in the PoPD film. The imprinted sensor was characterized via atomic force microscope (AFM) and cyclic voltammetry (CV). Under the optimal experimental conditions, the current response of the imprinted sensor was linear to the concentration of brucine in the range of 6.2 × 10 −7 –1.2 × 10 −5 M, and a detection limit of 2.1 × 10 −7 M was obtained. The imprinted sensor showed high recognition ability and affinity for brucine in comparison with non-imprinted polymer (NIP), and it was successfully applied to the determination of brucine in human serum samples with recoveries of 99.5–103.2%.

Anti-tumor effects of brucine immuno-nanoparticles on hepatocellular carcinoma.

Abstract: Background Hepatocellular carcinoma is difficult to diagnose early, and most patients are already in the late stages of the disease when they are admitted to hospital. The total 5-year survival rate is less than 5%. Recent studies have showed that brucine has a good anti-tumor effect, but high toxicity, poor water solubility, short half-life, narrow therapeutic window, and a toxic dose that is close to the therapeutic dose, which all limit its clinical application. This study evaluated the effects of brucine immuno-nanoparticles (BIN) on hepatocellular carcinoma.

Improved pharmacokinetics and reduced toxicity of brucine after encapsulation into stealth liposomes: role of phosphatidylcholine.

Abstract: Objective: Brucine was encapsulated into stealth liposomes using the ammonium sulfate gradient method to improve therapeutic index.

A new method for the simultaneous analysis of strychnine and brucine in Strychnos nux-vomica unprocessed and processed seeds using a carbon-paste electrode modified with multi-walled carbon nanotubes.

Abstract: Introduction Strychnos nux-vomica L. (Loganiaceae), widely used in folk medicine, is grown extensively in southern Asian countries. Its major bioactive constituents are strychnine and brucine, which are frequently used in traditional herbal medicines for treatment of nervous diseases, vomiting and traumatic pain. Objective A new method using a carbon-paste electrode modified with multi-walled carbon nanotubes (CNT/CPE) was developed and validated for single or simultaneous determination of strychnine and brucine in Strychnos nux-vomica seeds. Additionally, an environmentally friendly method was successfully applied to reduce the levels of strychnine and brucine in seeds. Materials and methods Cyclic voltammetry, chronocoulometry and differential pulse voltammetry were used with multi-walled carbon nanotube modified carbon-paste electrodes. Results The peak currents increase linearly with the strychnine and brucine concentrations in the ranges of 50–1000 and 5–355 µ m, and the detection limits for strychnine and brucine were 0.43 and 0.28 µ m, respectively. Of the processing methods used, the greatest reduction in the strychnine and brucine levels was observed in samples processed using milk and saltwater. Conclusion A new, sensitive and selective method was developed for the measurement of strychnine and brucine. This method was successfully applied to the determination of strychnine and brucine in unprocessed and processed Strychnos nux-vomica seed. Copyright © 2011 John Wiley & Sons, Ltd.

The Apoptotic Effect of Brucine from the Seed of Strychnos nux-vomica on Human Hepatoma Cells is Mediated via Bcl-2 and Ca 2+ Involved Mitochondrial Pathway

Abstract: In an attempt to dissect the mechanism of Strychnos nuxvomica, a commonly used Chinese folk medicine in the therapy of liver cancer, the cytotoxic effects of four alkaloids in Strychnos nux-vomica, brucine, brucine N-oxide, strychnine, and isostrychnine, on human hepatoma cells (HepG2) were screened by 3-(4,5dimethylthiazol-2-yl)-2,5-diphenyl-tetrasolium bromide (MTT) assay. Brucine, among the four alkaloids, exhibited the strongest toxic effect, the mechanism of which was found to cause HepG2 cell apoptosis, since brucine caused HepG2 cell shrinkage, the formation of apoptotic bodies, DNA fragmentation, cell cycle arrest, as well as phosphatidylserine externalization, all of which are typical characteristics of apoptotic programmed cell death. Brucine-induced HepG2 cell apoptosis was caspase dependent, with caspase-3 activated by caspase-9. Brucine also caused the proteolytic processing of caspase-9. In addition, brucine caused depolarization of the mitochondrial membrane of HepG2 cells, the inhibition of which by cyclosporine A completely abrogated the activation of casapses and release of cytochrome c in brucinetreated HepG2 cells. These findings suggested a pivotal role of mitochondrial membrane depolarization in HepG2 cell apoptosis elicited by brucine. Furthermore, brucine induced a rapid and sustained elevation of intracellular [Ca 2+ ], which compromised the mitochondrial membrane potential and triggered the process of HepG2 cell apoptosis. Finally, Bcl-2 was found to predominately control the whole event of cell apoptosis induced by brucine. The elevation of [Ca 2+ ]i caused by brucine was also suppressed by overexpression of Bcl-2 protein in HepG2 cells. From the facts given above, Ca 2+ and Bcl-2 mediated mitochondrial pathway

Effects of brucine on vascular endothelial growth factor expression and microvessel density in a nude mouse model of bone metastasis due to breast cancer

Abstract: To study the effects of brucine on vascular endothelial growth factor (VEGF) expression and microvessel density (MVD) in a nude mouse model of bone metastasis due to breast cancer, and to assess the possible antitumor mechanism of brucine. A syringe needle was used to directly inject 0.2 mL monoplast suspension (with 2×105 human breast cancer cells contained) into the bony femoral cortex of the right hind leg for modeling. Twenty-five nude mice were randomized into five groups and administered with an intraperitoneal injection of saline or drug for 8 consecutive days: model group (0.2 mL normal saline), low-dose brucine group (1.73 mg·kg−1), medium-dose brucine group (3.45 mg·kg−1), high-dose brucine group (6.90 mg·kg−1), and thalidomide group (200 mg·kg−1). Diet and activity were recorded, and the tumors were harvested 5 weeks later. The percentage of VEGF-positive cells was determined with hematoxylin and eosin staining and immunohistochemical staining, and MVD expression was determined by optical microscopy. The VEGF expressions in brucine- or thalidomide-treated mice were significantly reduced as compared with mice in the model group (P 0.05). Significant difference was between the high- and low-dose brucine group P 0.05), while the MVD value showed a significant increase in the low-dose group compared with the thalidomide group (P <0.05). Brucine could inhibit the growth of breast cancer to bone metastases, possibly by inhibiting tumor angiogenesis.

Simultaneous analysis of strychnine and brucine and their major metabolites by liquid chromatography-electrospray ion trap mass spectrometry.

Abstract: A liquid chromatography –electrospray ionization– ion trap mass spectrometry (LC –ESI–ITMS) method was developed for the simultaneous analysis of strychnine, brucine and their major metabolites. Strychnine and brucine were individually incubated with rat liver S9 fraction. The incubation samples were pooled together and analyzed with LC–ESI –ITMS in positive ion and full-scan detection mode. The calibration curves of strychnine and brucine in rat liver showed good linearity in ranges of 0.020 to 8.0 mg/mL for strychnine and 0.020 to 8.5 mg/mL for brucine. The limits of detections were both 0.008 mg/mL and the recoveries were 88.3 and 83.2% for strychnine and brucine, respectively. Two metabolites were identified as strychnine N-oxide and brucine N-oxide by comparing the molecular mass, retention time, full-scan mass spectra, tandem MS and MS 3 spectra with those of strychnine and brucine. The developed method provided high sensitivity and selectivity for the determination of poisonous alkaloids and their major metabolites and can be applied in the determination of samples in forensic and clinically toxicological cases.

Simultaneous determination of six toxic alkaloids in human plasma and urine using capillary zone electrophoresis coupled to time‐of‐flight mass spectrometry

Abstract: A novel capillary zone electrophoresis separation coupled to electro spray ionization time-of-flight mass spectrometry method was developed for the simultaneous analysis of six toxic alkaloids: brucine, strychnine, atropine sulfate, anisodamine hydrobromide, scopolamine hydrobromide and anisodine hydrobromide in human plasma and urine. To obtain optimal sensitivity, a solid-phase extraction method using Oasis MCX cartridges (1 mL, 30 mg; Waters, USA) for the pretreatment of samples was used. All compounds were separated by capillary zone electrophoresis at 25 kV within 12 min in an uncoated fused-silica capillary of 75 μm id × 100 cm and were detected by time-of-flight mass spectrometry. This method was validated with regard to precision, accuracy, sensitivity, linear range, limit of detection (LOD), and limit of quantification (LOQ). In the plasma and urine samples, the linear calibration curves were obtained over the range of 0.50-100 ng/mL. The LOD and LOQ were 0.2-0.5 ng/mL and 0.5-1.0 ng/mL, respectively. The intra- and interday precision was better than 12% and 13%, respectively. Electrophoretic peaks could be identified by mass analysis.

Simultaneous HPTLC determination of strychnine and brucine in strychnos nux-vomica seed

Abstract: Objective: A simple, sensitive, and specific thin layer chromatography (TLC) densitometry method has been developed for the simultaneous quantification of strychnine and brucine in the seeds of Strychnos nux-vomica . Materials and Methods: The method involved simultaneous estimation of strychnine and brucine after resolving it by high performance TLC (HPTLC) on silica gel plate with chloroform-methanol-formic acid (8.5:1.5:0.4 v/v/v) as the mobile phase. Results: The method was validated as per the ICH guidelines for precision (interday, intraday, intersystem), robustness, accuracy, limit of detection, and limit of quantitation. The relationship between the concentration of standard solutions and the peak response was linear within the concentration range of 50-1000 ng/spot for strychnine and 100-1000 ng/spot for brucine. The method precision was found to be 0.58-2.47 (% relative standard deviation [RSD]) and 0.36-2.22 (% RSD) for strychnine and brucine, respectively. Accuracy of the method was checked by recovery studies conducted at three different concentration levels and the average percentage recovery was found to be 100.75% for strychnine and 100.52% for brucine, respectively. Conclusions: The HPTLC method for the simultaneous quantification of strychnine and brucine was found to be simple, precise, specific, sensitive, and accurate and can be used for routine analysis and quality control of raw material of S. nux-vomica and several unani and ayurvedic formulations containing this as an ingredient.

Rituals can kill - A fatal case of brucine poisoning.

Abstract: In some parts of India people follow a religious ritual of drinking an herbal preparation made from the bark of the Alstonia scholaris tree (Blackboard tree) on the day of the new moon in the month of July This tree could be easily confused with the Strychnos nux vomica tree Brucine is the predominant alkaloid present in the bark of the Strychnos nux vomica tree The toxicological property of brucine is similar to strychnine Brucine is a neurotoxin A 29-year-old male presented with a history of consumption of an herbal preparation made from the bark of the Strychnos nux vomica tree confusing it for Alstonia scholaris Soon after, he developed convulsions and later died in hospital on the same day The aim of this case report is to highlight the fact that people must be cautious when they follow religious rituals

Simultaneous determination of 17 toxic alkaloids in human fluids by liquid chromatography coupled with electrospray ionization tandem mass spectrometry

Abstract: A sensitive and specific method was proposed and validated for the simultaneous determination of 17 poisonous alkaloids in human blood and gastric juice by liquid chromatography and electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS). After mixing with boric acid buffer solution (pH 9), the samples were extracted with chloroform followed by chloroform-ether (2:1, v/v). The simultaneous qualitative and quantitative analysis of 17 alkaloids, including koumine, atropine, scopolamine, brucine, strychnine, aconitine, bulleyaconitine A, ephedrine, pilocarpine, lobeline, ergometrine, anabasine, oxymatrine, theophylline, colchicine, tetrahydropalmatine, and eserine, were performed by using ESI+ in multiple-reaction monitoring (MRM) mode. Under the optimized conditions, the calibration curves of the 17 compounds presented good linearity (r≧0.9952) in the ranges of 0.5–50 µg/L and 0.5–500 µg/L. The quantitation limits (LOQs) and detection limits (LODs) ranged from 0.5–1 and 0.1–0.5 µg/L, respectively. T...

[Effect of NF-kappaB on inhibition of non-small cell lung cancer cell cyclooxygenase-2 by brucine].

Abstract: OBJECTIVE To study the molecular mechanism of cyclooxygenase-2 (COX-2), one of effective ingredient of brucine, in inducing non-small cell lung cancer cell apoptosis. METHOD COX-2 promoter, transcription factor deletion mutants and COX-2 mRNA 3'-UTR-containing report plasmids were transfected with Renillia to non-small cell lung cancer A549 cell, in order to detect the activity of report gene luciferase and minimum cis-acting element of COX-2 promoter inhibited by brucine. The influence of brucine on IkappaB phosphorylation and the nuclear translocation of p65 were detected by immunoblotting assay. RESULT Brucine significantly suppressed LPS-induced COX-2 promoter activation, but revealed minor impact on COX-2 mRNA stability. NF-kappaB in the vicinity of COX-2 promoter-262 was an important cis-acting element of brucine for inhibiting the activity of COX-2 promoter. Brucine was found to inhibit the phosphorylation of IkappaBalpha as well as the nuclear translocation of p65. CONCLUSION Brucine can improve A549 cells apoptosis by inhibiting the activity of NF-kappaB and the subsequent COX-2 gene expression.

Effects of brucine on bone metabolism in multiple myeloma

Abstract: The aim of this study was to explore the effects of brucine on bone metabolism in multiple myeloma (MM) and to compare brucine and bortezomib regarding the effects on MM in vitro. The half maximal inhibitory concentration (IC50) values of brucine and bortezomib in the MM cell line U266 were detected by MTT assay. In addition, the expression of alkaline phosphatase (ALP), osteocalcin (OC), osteoprotegerin (OPG) and osteoprotegerin ligand (also termed receptor activator of nuclear factor κB ligand) (RANKL) at mRNA levels were measured by RT-PCR. IC50 of bortezomib in the U266 cell line at 48 h was 22.4 nmol/l, and that of brucine was 0.16 nmol/l. Compared with osteoblasts incubated with MM cell supernatant alone, the mRNA levels of ALP, OC and OPG in osteoblasts co-treated with brucine and MM cell supernatant were higher (p<0.05), while the mRNA expression of RANKL was lower, and the ranges of the changes were all larger than those of the group treated with bortezomib (P<0.05). Brucine exerts effects on bone metabolism in multiple myeloma through the regulation of osteoclasts by osteoblasts.

Analysis and Comparison of Content Dependence of Brucine and Strychnine on Different Particle Sizes of Semen Strychni Powder

Abstract: To study the effect of the particle size on the active(toxic) component contents of Semen Strychni powder,20—200 mesh of Semen Strychni powder samples were prepared.The micro morphology of these samples were characterized by scanning electron microscope(SEM) and the samples were qualitatively identified by TLC.The contents of brucine and strychnine of each sample were determined by HPLC.The results indicated that there existed some differences between morphology compositions of Semen Strychni powder samples with different particle sizes.Moreover,the contents of brucine,strychnine of different samples were different,and the contents of brucine(or strychnine) in some samples of Semen Strychni powder were significantly different.So when Semen Strychni powder is applied to traditional Chinese medicine,its particle size should be highly controlled.Upon the results of the research,the particle size of Semen Strychni powder had better be 100—200 mesh.

Nematicidal activity of strychnos nuxvomica leaf and its constituents against the root-knot nematode, meloidogyne incognita

Abstract: Studies were undertaken on the nematicidal activity of Strychnos nuxvomica leaf extracts and its constituents on the second stage juveniles of the root-knot nematode, Meloidogyne incognita. Aqueous leaf extracts at 2% concentration caused 100% mortality of second stage juveniles of the nematode. The biological activity of the known phytochemicals from S. nuxvomica, evaluated by in silico analysis through prediction of activity spectra for substances (PASS) software, indicated that seven phytochemicals were expected to show nematicidal activity at various levels. In silico studies showed that the values of Pa (probability to be active) for brucine and strychnine were 0.986 and 0.785, respectively. Bioassay-guided fractionation of the leaf extract of S. nuxvomica indicated that the active fractions contained brucine and strychnine as major components. The nematicidal activity of brucine and strychnine was validated through in vitro bioassays and LD50 values were determined to be 665 ppm and 833 ppm, respectively.

Forensic Determination of Toxication of Strychnos Nuxvomica

Abstract: Strychnos nux-vomica has been used as a poisonous raw material for the preparation of Chinese medicinal herb for thousands of years in China, it is required that the herb should be specially processed before being put into clinical use. Since its treatment dosage is very close to its toxic dosage, poisoning frequently take place due to misuse, brucine and its derivatives are the principal component responsible for its pharmacodynamic effect and toxicity, strychnine is main component responsible for its toxicity. Both strychnine and brucine are typical antagonists of the glycine receptors on postsynatic membrane. Its toxic effects are mainly to cause central excitation. Because of its strong toxicity, narrow safety range and cumulative effect, the use of the drug in the clinical practice tends to cause poisoning, and poisoning of the drug is associated with the large dosage, and/or the long time use. Its toxicity also varies with its origins of production or batches. The symptoms of strychnos nuxvomica poisoning vary. The autopsy findings mainly include pathological changes caused by acute disorder of blood circulation, characterized by the congestion and edema of organs or pinpoint bleeding of mucosa or serous membrane. Long-term toxicity test revealed no characteristic pathological changes of vital organs in animals. For the detection of poisonous substances, the stomach tissue or stomach contents are the best choices, and urine, intestinal contents are the next best materials. Liver, brain and spinal medulla also have high level of strychnos nuxvomica after poisioning. In the forensic identification of strychnos nuxvomica poisoning, it is important to eliminate the other death causes, than get sufficient information concerning the source of the herb (variety, batch, origin of the product), the physical condition (metabolic status) of the patients or victim, dosage, and take the symptoms, pathological changes into consideration. Because of its accumulation, the possibility of the drug being given multiple-times and in small-dose should be considered. The detection of strychnos nuxvomica and quantitative analysis is essential and most reliable in the identification of strychnos nuxvomica poisoning. Exceptionally, great care should be exercised to differentiate it from the intoxication of tetra mine, fumarin and armazide and other spasm-causing agents.

Impact of shodhana (purificatory procedures) onkupeelu (strychnos nux- vomica linn.) seeds: apharmaceutico-analytical studys -

Abstract: Kupeelu (Strychnos nux-vomica Linn.), a drug mentioned under Upavisha (semi-poisonous) group of Ayurvedic pharmacopoeia, is being practiced widely in Ayurvedic therapeutics since long. Certain compound formulations containing Kupeelu are also well practiced in Homeopathy and Unani System of Medicine. Ayurveda strictly recommend the use of this drug in therapeutics only after proper Shodhana (purificatury procedure) through some specific media like Gomutra, Godugdha, Goghrita, Kanji etc. Though various Shodhana procedures are recommended in Ayurvedic classics for purification of Kupeelu seeds, but updated scientific researches regarding the Shodhana methods are lacking. Keeping this fact in mind, an attempt hasbeen made in the present study to evaluate the impact of Shodhana on Kupeelu seeds while performing the specific Shodhana method, recommended by the Ayurvedic Formulary of India(A.F.I.). This study reveals that the toxic alkaloids Strychnine & Brucine, present in Kupeelu seed,were reduced by 71.49% and 54.02% respectively, in comparison to the raw seed, as determined by H.P.T.L.C. study.

[Comparison on in vivo pharmacokinetics of brucine, total alkaloids of Strychni Semen and Strychni Semen pulveratum in rats].

Abstract: OBJECTIVE To study different in vivo pharmacokinetic regularity of brucine, total alkaloids of scorched sand-prepared Strychni Semen products and Strychni Semen pulveratum in rats, and probe into mutual impact between single component and compound. METHOD Rats in each group were orally administered with brucine, total alkaloids of scorched sand-prepared Strychni Semen products and Strychni Semen pulveratum suspension. The in vivo plasma concentrations of brucine in rats were determined by HPLC. A compartment model was made for the blood drug concentration-time curve using 3P97 software package and the pharmacokinetic parameters of each group were calculated and compared. RESULT The in vivo metabolic process of brucine in rats complied with the two-compartment model, weight W = 1/C2. The results of variance analysis showed that among three existing forms of brucine with same dosage, the brucine solution group and the total alkaloids group of scorched sand-prepared Strychni Semen products showed significant differences in C(max), MRT (P < 0.05); and the brucine solution group and the Strychni Semen pulveratum suspension group showed significant differences in C(max), AUC(0-t), and AUC(0-infinity), in which the latter displayed minimum C(max), AUC(0-t) and AUC(0-infinity). CONCLUSION The total alkaloids group of scorched sand-prepared Strychni Semen products showed a relatively longer retention time of effective components of brucine in plasma, while the Strychni Semen pulveratum suspension group showed a lower bioavailability.

Pharmacognostic Studies of Strychnos potatorum L.f.

Abstract: A B ST R A C T Strychnos potatorum (Clearing nut), an important medicinal plant used in the traditional and folk medicine for treating several aliments including microbial infections, diarrhoea and diabetes. Some of its pharmacognostic studies such as fluorescent, organoleptic, ash and mineral contents of root, stem bark and seed (both collected and market) , and GC- alkaloid profiles of seed have been investigated. Considerable colour variations in the fluorescent behaviour of raw drugs were observed. The highest yields were obtained for the aqueous extracts followed by ethanol, petroleum ether and chloroform extracts. The colour of the extracts thus obtained have from ivory to dark brown and bitter to pungent bitter in taste. Higher values of the total ash and insoluble acid contents were recorded for the stem bark, followed by root and seed samples. Considerable amounts of iron and copper found in all parts of the plant. However, lead, a toxic element was found in trace amount in the market seed sample. Further, the GC-alkaloid profiles of seed samples have shown significant variation in terms of percent area of peaks. Furthermore, the co-TLC study has revealed the absence of strychnine and brucine from the seed sample.

Preparation and pharmacokinetics of brucine hydrogel patch

Abstract: OBJECTIVE To investigate the effect of dose on pharmacokinetic properties of brucine hydrogel patch METHODS The plasma concentration of brucine was determined by HPLC Brucine hydrogel patch was prepared and its pharmaceutical characterization was investigated After transdermal administration of different dose brucine hydrogel patch; Plasma concentration versus time profiles were determined and pharmacokinetic parameters were calculated by DAS program RESULTS The pharmaceutical properties of brucine hydrogel patch were satisfactory The AUC0-1 values were 724 +/- 061, 1602 +/- 234 and 5484 +/- 2659 microg x h/mL after administration of 30, 60 and 180 mg/kg brucine hydrogel patch, respectively The corresponding C(max) values were 073 +/- 023, 145 +/- 028 and 459 +/- 185 microg/mL, respectively And the corresponding T(max) values were 867 +/- 207, 1167 +/- 266 and 833 +/- 265 h, respectively CONCLUSION The pharmacokinetic properties of brucine do not vary with the dose of brucine hydrogel patch

A novel indolomonoterpenic alkaloid from processed Strychnos nux-vomica

Abstract: A novel indolomonoterpenic alkaloid, 4-hydroxy-19-methyl-16,19-seco-12,24-seco-strychnidine-10,16-dione (1), together with three known compounds 2–4 (vomicine, strychnine, and brucine), have been isolated from processed Strychnos nux-vomica. Its structure was determined by detailed spectral analysis (1H NMR,13C NMR, 1H–1H COSY, HMBC, and HR-ESI-MS).

Identification of anti-diabetic activity of strychnous nuxvomica roots in invivo conditions

Abstract: Strychnous nuxvomica is a medicinal plant with many chemical constituents like strychnine, brucine, indole alkaloids etc. This study was design to investigate the effect of aqueous methanol extract of nuxvomica roots, on various biological parameters in diabetes induced rabbits. The effect of crude nuxvomica root and its organic extracts on blood glucose level of rabbits has been studied. It was found that methanol extract had some hypoglycemic effect on the induced hyperglycemia in the experimental animals.

Study on the effect of glycyrrhizic acid on toxicokinetics for brucine and the mechanism study of detoxication

Abstract: OBJECTIVE To investigate the effects of glycyrrhizic acid on the kinetics of metabolism for toxic dosage of brucine in plasma and brain,and explore a new antidotal pathway for brucine-induced toxicity.METHODS Male KM mice were injected intraperitoneally with normal saline,glycyrrhizic acid and verapamil for 7 days,respectively.In the 8th day,each animal was injected intraperitoneally with brucine.UPLC-MS/MS method and real-time fluorescence quantitative RT-PCR methods were used to determinate the brucine's concentration and the expression of mdr1a,respectively.RESULTS After treatment with glycyrrhizic acid,the AUC0→10h of brain/plasma concentration ratio decreased 37.6% compaered to control group(P0.05).The RT-PCR results revealed that continuesly treated with glycyrrhizic acid could induce the expression of mdr1a mRNA in the brain of mice.The AUC0→10h and the AUC0→10h of brain/plasma concentration ratio increased 30.7%,32.5% respectively by verapamil(P0.05).CONCLUSION The experiment proved that glycyrrhizic acid may accelerate the elimination of brucine through up-regulate the P-gp's function in the brain of mice.Verapamil could reverse the decreased trend of drug disposition in brain,so brucine may be the substrate of P-gp in blood-brain barrier.

Brucine immune nanoparticles

Abstract: The invention relates to brucine immune nanoparticles. The immune nanoparticle is characterized in that the brucine is taken as an active component, a carboxylation polyethylene glycol-a polylactic acid segmented copolymer is taken as a medicament coated auxiliary material, an antihuman AFP monoclonal antibody is linked outside the medicament coated auxiliary material to prepare immune-targeting nanoparticles. The brucine immune nanoparticles have the advantages of simple preparation technology, high entrapment rate, stable medicament release and good ballability, and is used for preparing antitumor immune-targeting medicines, the medicine is used for anti-liver cancer treatment, the antihuman AFPMcAb-polyethylene glycol-polylactic acid segmented copolymer nanometer carrier is capable of increasing the aggregation of brucine in liver cancer cells through peripheral intravenous administration, so that the medicine is locally and slowly released, the effect time of the medicine to tumorcells is prolonged, local medicine concentration is raised and the general toxic reaction of the brucine is reduced; and the brucine immune nanoparticles have the merits of precious targeting histiocytoma medicament aggregation, stable medicament release, good anticancer effect, safety and the like.

Purpose of immunological nanoparticles of brucine in preparing anti-hepatoma target drugs

Abstract: The invention relates to a purpose of immunological nanoparticles of brucine in preparing anti-hepatoma target drugs. The immunological nanoparticles of brucine are immunological target nanoparticles which treat brucine as an active component and a carboxylated polyethylene glycol-polylactic acid segmented copolymer as a drug coating accessory, and are formed by externally linking with anti-humanAFP monoclonal antibodies. The immunological nanoparticles of brucine provided by the invention, which have the characteristics of simple technology, high entrapment rate, stable drug release, and good balling, can be used for preparing antitumor target drugs which can be used for anti-hepatoma treatment. By intravenous injection, a nanometer carrier anti-human AFPMcAb-polyethylene glycol-polylactic acid segmented copolymer allows brucine aggregation in hepatoma cells to be increased, the drugs to be slowly and locally released, the effect time of the drugs to tumor cells to be prolonged, thelocal drug concentration to be improved, and the whole body toxicity of brucine to be reduced. So the immunological nanoparticles of brucine of the present invention have the advantages of accurate aggregation of target drugs in the cells of tumor tissues, stable drug release, good anticancer effect, safety and the like.