RESUMEN

OBJECTIVE To optimize the pressurized processing technology of Strychnos nux-vomica boiled with mung beans. METHODS The least squares method was used to establish a one-dimensional model for the effects of four factors， namely， processing time， processing pressure， mung bean dosage and water added， on the contents of strychnine and toxiferine， and the multivariate model hypothesis was proposed by analyzing the function of one-dimensional model. Based on the orthogonal experiment， the genetic algorithm was used to solve the undetermined coefficients in the model. A bi-objective optimization model based on strychnine and toxiferine content was constructed according to the actual conditions， and the optimal technology was obtained by solving the model function and validated. RESULTS The optimal processing technology was boiling S. nux-vomica with mung beans at 2.393 MPa saturated steam pressure for 5.5 h， and then draining； rinsing to remove mung beans， scraping off the bark of S. nux-vomica and cutting into slice of 0.6 mm； using 180 g of mung beans and 15 L of water per 500 g of S. nux- vomica. CONCLUSIONS The optimized pressurized processing technology is stable and feasible， and can provide a reference for the optimization of processing technology of S. nux-vomica boiled with mung beans.

RESUMEN

BACKGROUND: Rheumatoid arthritis (RA) is a chronic autoimmune disease, which affects the joints and causes significant pain, impairing patient's quality of life. Strychni semen showed promising results to treat RA. However, there are increasing safety concerns in using strychni semen due to its severe toxicity. AIM AND OBJECTIVE: The purpose of this review is to provide insight into using Strychni semen as an alternative medicine to treat RA, as well as to offer a method for the safe application of Strychni semen through processing and compatibility studies. METHODS: Publications were retrieved and surveyed from CNKI and PubMed relevant to Strychni semen for a literature review. RESULTS: This article summarized the mechanism of function of strychni semen in treating RA with its anti-inflammatory, analgesic, and immunomodulatory effect. Commonly used methods to attenuate the toxicity of Strychni semen were also discussed in this article. CONCLUSION: Strychni semen has a good therapeutic effect on RA, mainly by the modulation of immunity with anti-inflammatory and analgesic effects. Also, the reported toxicity of strychni semen can be effectively reduced by processing and compatibility methods. Hence, as an alternative medicine for RA treatment, strychni semen has a broad prospect.

Asunto(s)

Artritis Reumatoide , Preparaciones de Plantas , Semillas , Artritis Reumatoide/tratamiento farmacológico , Humanos , Preparaciones de Plantas/uso terapéutico , Calidad de Vida , Semillas/química

RESUMEN

BACKGROUND: The establishment of strategy to inhibit the virus replication is an attractive means in combating SARS-CoV-2 infection. OBJECTIVE: We studied phyto-compounds from Strychnos nux-vomica (a poisonous plant) against SARS-CoV-2 RNA-dependent RNA polymerase by computational methods. METHODS: Molecular docking, molecular dynamics (MD) simulation and energetics calculations were employed to elucidate the role of the phyto-compounds. RESULTS: Ergotamine with a binding free energy of -14.39 kcal/mol showed a promising capability in terms of binding affinity and the interaction to conserved motifs, especially the SDD signature sequence. The calculated dissociation constants for ATP, ergotamine, isosungucine and sungucine were 12 µM, 0.072 nM, 0.011 nM and 0.152 nM, respectively. The exhibited kd by these phyto-compounds reflected tens of thousands fold potency as compared to ATP. The binding free energies of sungucine and isosungucine were much lower (-13.93 and -15.55 kcal/mol, respectively) compared to that of ATP (-6.98 kcal/mol). CONCLUSION: Sharing the same binding location as that of ATP and having high binding affinities, Ergotamine, Isosungucine, Sungucine and Strychnine N-oxide could be effective in controlling the SARS-CoV-2 virus replication by blocking the ATP and inhibiting the enzyme function.

Asunto(s)

COVID-19 , Strychnos nux-vomica , Adenosina Trifosfato , Ergotaminas , Simulación del Acoplamiento Molecular , Plantas Tóxicas , ARN Viral/genética , SARS-CoV-2 , Strychnos nux-vomica/química

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The novel coronavirus also referred to as SARS-CoV-2 causes COVID-19 and became global epidemic since its initial outbreak in Wuhan, China, in December 2019. Research efforts are still been endeavoured towards discovering/designing of potential drugs and vaccines against this virus. In the present studies, we have contributed to the development of a drug based on natural products to combat the newly emerged and life-threatening disease. The main protease (MPro) of SARS-CoV-2 is a homodimer and a key component involved in viral replication, and is considered as a prime target for anti-SARS-CoV-2 drug development. Literature survey revealed that the phytochemicals present in Strychnos nux-vomica possess several therapeutic activities. Initially, in the light of drug likeness laws, the ligand library of phytoconstituents was subjected to drug likeness analysis. The resulting compounds were taken to binding site-specific consensus-based molecular docking studies and the results were compared with the positive control drug, lopinavir, which is a main protease inhibitor. The top compounds were tested for ADME-Tox properties and antiviral activity. Further molecular dynamics simulations and MM-PBSA-based binding affinity estimation were carried out for top two lead compounds' complexes along with the apo form of main protease and positive control drug lopinavir complex, and the results were comparatively analysed. The results revealed that the two analogues of same scaffold, namely demethoxyguiaflavine and strychnoflavine, have potential against Mpro and can be validated through clinical studies.Communicated by Ramaswamy H. Sarma.

Asunto(s)

Productos Biológicos , Tratamiento Farmacológico de COVID-19 , Strychnos nux-vomica , Antivirales/química , Antivirales/farmacología , Endopeptidasas/metabolismo , Humanos , Ligandos , Lopinavir , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Péptido Hidrolasas/metabolismo , Inhibidores de Proteasas/química , Inhibidores de Proteasas/farmacología , SARS-CoV-2

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OBJECTIVE: To investigate the antagonistic effect of the extract of Baizhu (Rhizoma Atractylodis Macrocephalae) (RAM) on the intestinal absorption of brucine and strychnine in Strychnos nux-vomica (NUX) and propose the mechanism of these effects. METHODS: The apparent permeability value (Papp) and absorption rate constant (Ka) were chosen as indices. The everted intestinal sac model and in situ single-pass intestinal perfusion model were used to study the effects of the RAM extract on the absorption of brucine and strychnine. To confirm the results, the brucine and strychnine concentrations in hepatic portal venous blood were determined. Western blotting was used to study P-glycoprotein (P-gp) expression in the Caco-2 cell line. RESULTS: Papp and Ka of brucine and strychnine were significantly increased in the presence of a P-gp inhibitor, but no significant increase was noted in the presence of a tight junction regulator. The RAM extract inhibited the absorption of brucine and strychnine and enhanced P-gp expression. CONCLUSION: The primary absorption mechanism for brucine and strychnine is passive transport, which is affected by P-gp.

Asunto(s)

Atractylodes/química , Medicamentos Herbarios Chinos/farmacocinética , Absorción Intestinal/efectos de los fármacos , Estricnina/análogos & derivados , Estricnina/farmacocinética , Strychnos nux-vomica/química , Animales , Células CACO-2 , Línea Celular Tumoral , Medicamentos Herbarios Chinos/administración & dosificación , Humanos , Masculino , Ratas , Ratas Sprague-Dawley , Rizoma/química , Estricnina/administración & dosificación

RESUMEN

BACKGROUND: Peripheral nerve injury is a debilitating condition that may lead to partial or complete motor, sensory and autonomic function loss and lacks effective therapy until date. Therefore, it is quite imperative to explore impending remedies for rapid and accurate functional retrieval following such conditions. Natural product-based intervention can prove effective to facilitate the process of functions regain. METHODS: Here, we investigated the effect of processed Strychnos nux-vomica seeds at a dose of 250 mg/kg body weight in a mouse model of induced Sciatic nerve lesion in promoting the recovery of the functions. A compression injury was induced in the Sciatic nerve of the right leg in the mice. Sensory function recovery was evaluated by hot-plate and formalin tests, whereas the motor function retrieval was assessed by measuring muscle grip strength, sciatic functional index, and muscle mass restoration. Oxidative stress and blood cell count were measured by biochemistry and haematological analyses. RESULTS: This study indicates that Strychnos nux-vomica seeds enhance the rate of recovery of both sensory and motor functions. It helps restore the muscle mass, attenuates total oxidant status and enhances the total anti-oxidant capacity of the biological system. Moreover, the treated animals manifested an enhanced glucose tolerance aptitude and augmented granulocyte and platelet counts. Improved oxidant control, enhanced glucose sensitivity and amended granulocyte and platelet counts are likely to contribute to the advantageous effects of Strychnos nux-vomica, and warrant further in-depth studies for deciphering possible mechanisms and identification of active constituent(s) responsible for these effects. CONCLUSION: Strychnos nux-vomica seed offers functional recovery promoting effects following a mechanical injury to the Sciatic nerve and the possible reasons behind this effect can be reduced oxidative stress and improved glycaemic control. Further and detailed investigations can unravel this mystery.

Asunto(s)

Lesiones por Aplastamiento/tratamiento farmacológico , Estrés Oxidativo/efectos de los fármacos , Traumatismos de los Nervios Periféricos/tratamiento farmacológico , Preparaciones de Plantas/uso terapéutico , Neuropatía Ciática/tratamiento farmacológico , Strychnos nux-vomica/química , Animales , Modelos Animales de Enfermedad , Masculino , Ratones , Recuperación de la Función , Semillas/química

RESUMEN

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.

RESUMEN

Gastrite é a inflamação das paredes do estômago. Por meio de inúmeras causas, há um enfraquecimento da mucosa estomacal, permitindo que suco digestivo possa provocar dano a parede, através da quebra da barreira mucosa. Ela pode ser classificada em aguda ou crônica, e o tratamento é sempre medicamentoso. Geralmente nos casos agudos, podemos relacionar a um agente causador medicamentoso, infeccioso ou estressor - físico ou psíquico. Apesar do tratamento medicamentoso convencional, em alguns casos, o paciente ainda pode apresentar-se sintomático. Este presente relato de caso, diz respeito a um paciente que apesar do tratamento convencional, apresentava-se sintomático. A causa principal do seu problema, era atribuída principalmente ao estresse psíquico. Desta maneira, resolveu procurar a homeopatia, como medicina complementar. O tratamento homeopático, individualizado, mostrou ser muito eficaz no caso apresentado, com melhora dos sintomas iniciais da epigastralgia e também, de sintomas secundários, que não foram, motivadores da consulta. (AU)

Asunto(s)

Humanos , Masculino , Adulto , /uso terapéutico , Homeopatía , Coffea Cruda , Natrium Muriaticum , Gastritis/terapia

RESUMEN

Multidrug resistance in bacterial strains has become the greatest challenge for healthcare professionals for treating non-healing ulcers such as diabetic foot infections (DFI). Plant-mediated synthesis of S. nux-vomica-ZnO nanocomposite appears as a potential new alternative therapeutic agent that might be capable of tackling antibiotic-resistant bacterial pathogens and for treating a non-healing ulcer. The aim of the study was to investigate the antibacterial potential of S. nux-vomica-ZnO nanocomposite biosynthesised from Strychnos nux-vomica against multidrug-resistant organisms (MDROs) from DFU, wound-healing properties, and cytotoxic effects. The antibacterial potential was assessed by minimum inhibitory concentration (MIC)/ minimum bactericidal concentration (MBC) assays, time-kill kinetics, protein-leakage, and flow cytometric analysis. The wound-healing properties were assessed by scratch assay on mouse L929 fibroblastic cell line to quantify cell migration towards the injured area. Cytotoxicity was assessed using 3-[4,5-dimethyl-2-thiazol-yl]-2,5-diphenyl- 2H-tetrazolium bromide (MTT) cellular viability assay on the L929 cell line and human embryonic kidney epithelial (HEK-293) cell line. Strychnos nux-vomica-ZnO nanocomposite at a size range of 10-12 nm exhibited significant bactericidal potency at a concentration of 100-200 µg/ml against MDR-Methicillin-resistant Staphylococcus aureus, MDR-Escherichia coli, MDR-Pseudomonas aeruginosa, MDR-Acinetobacter baumannii, and also against standard bacterial strains S. aureus ATCC 29213, E. coli ATCC 25922, P. aeruginosa ATCC 27853, E. faecalis ATCC 29212. S. nux-vomica-ZnO nanocomposite also exhibited wound-healing and reduced cytotoxic properties at the antimicrobially active concentrations. Our findings thus suggested remarkable bactericidal properties of S. nux-vomica-ZnO nanocomposite and can be further exploited towards for the development of an antibacterial agent against the threatening superbugs.

Asunto(s)

Antibacterianos/química , Antibacterianos/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Nanocompuestos/química , Animales , Antibacterianos/efectos adversos , Línea Celular , Escherichia coli/efectos de los fármacos , Citometría de Flujo , Células HEK293 , Humanos , Ratones , Pruebas de Sensibilidad Microbiana , Nanocompuestos/efectos adversos , Staphylococcus aureus/efectos de los fármacos , Cicatrización de Heridas/efectos de los fármacos

RESUMEN

Nanobiotechnology has been emerged as an efficient technology for the development of antimicrobial nanoparticles through an eco-friendly approach. In this study, green synthesized phytonanocomposite of ZnO from Strychnos nux-vomica leaf aqueous extract was characterized by X-ray diffraction analysis (XRD), UV-visible-spectroscopy, Photoluminescence spectroscopy (PL), Fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS), High-resolution Transmission Electron Microscopy (HR-TEM), and Energy dispersive X-ray analysis (EDX). Antibacterial activity was investigated against multidrug-resistant bacteria (MDR) isolated from diabetic foot ulcers (DFUs), such as MDR-methicillin resistant Staphylococcus aureus (MRSA), MDR-Escherichia coli, MDR-Pseudomonas aeruginosa, MDR-Acinetobacter baumannii, as well as against standard bacterial strains, S. aureus ATCC 29213, E. coli ATCC 25922, P. aeruginosa ATCC 27853, and E. faecalis ATCC 29212 through disc diffusion assays on Muller Hinton Agar. The characterization studies revealed a size-controlled synthesis of quasi-spherical hexagonal wurtzite structured ZnO phytonanocomposite with an average size of 15.52 nm. Additionally, remarkable bactericidal activities against MDR clinical as well as ATCC bacterial strains were exhibited, with a maximum zone of inhibition of 22.33 ±â€¯1.53 mm (against S. aureus ATCC 29213) and 22.33 ±â€¯1.16 mm (MDR-MRSA) at a concentration of 400 µg/mL. This study thus established the possibility of developing antimicrobial ZnO nanocomposite of Strychnos nux-vomica leaf extract to combat developing drug resistance currently being experienced in health care facilities.

RESUMEN

Strychnos nux-vomica L. belongs to the genus Strychnos of the family Loganiaceae and grows in Sri Lanka, India and Australia. The traditional medicinal component is its seed, called Nux vomica. This study provides a relevant and comprehensive review of S. nux-vomica L., including its botany, ethnopharmacology, phytochemistry, pharmacology and toxicology, thus providing a foundation for future studies. Up to the present day, over 84 compounds, including alkaloids, iridoid glycosides, flavonoid glycosides, triterpenoids, steroids and organic acids, among others, have been isolated and identified from S. nux-vomica. These compounds possess an array of biological activities, including effects on the nervous system, analgesic and anti-inflammatory actions, antitumor effects, inhibition of the growth of pathogenic microorganisms and regulation of immune function. Furthermore, toxicity and detoxification methods are preliminarily discussed toward the end of this review. In further research on S. nux-vomica, bioactivity-guided isolation strategies should be emphasized. Its antitumor effects should be investigated further and in vivo animal experiments should be performed alongside in vitro testing. The pharmacological activity and toxicology of strychnine [Formula: see text]-oxide and brucine [Formula: see text]-oxide should be studied to explore the detoxification mechanism associated with processing more deeply.

Asunto(s)

Strychnos nux-vomica/química , Strychnos nux-vomica/toxicidad , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Analgésicos , Animales , Antiinflamatorios , Antineoplásicos Fitogénicos , Óxidos N-Cíclicos/farmacología , Óxidos N-Cíclicos/toxicidad , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Humanos , Técnicas In Vitro , Glicósidos Iridoides/aislamiento & purificación , Glicósidos Iridoides/farmacología , Loganiaceae , Fitoterapia , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Semillas/química , Estricnina/análogos & derivados , Estricnina/farmacología , Estricnina/toxicidad

RESUMEN

A neoteric approach for the electrochemical analysis of brucine in biological environment has been developed. The glassy carbon electrode modified with single walled carbon nanotubes and nafion composite film is delineated for the first time to determine brucine employing square wave voltammetry. The quantification of brucine at physiological pH 7.2 manifests remarkable performance at the developed biosensor. The effect of several operational parameters has been studied in the present investigation. Under optimized conditions, a dynamic linear range from 1nM to 8µM with a high sensitivity of 340.8µAµM-1 and limit of detection corresponding to 0.11nM was achieved. The interfering effect of some coexisting metabolites on the current response of brucine has been reported. The method was successfully applied for the detection of brucine in traditional pharmaceutical formulations. The biological relevance of the present method has been demonstrated by the analysis of the alkaloid in human serum and urine samples. The analytical utility was further assessed by the selective determination of brucine in Strychnos nux-vomica seeds exhibiting considerable potential as a diagnostic tool.

Asunto(s)

Técnicas Biosensibles , Carcinoma Hepatocelular , Neoplasias Hepáticas , Estricnina/análogos & derivados , Carcinoma Hepatocelular/sangre , Carcinoma Hepatocelular/orina , Línea Celular Tumoral , Técnicas Electroquímicas/métodos , Humanos , Neoplasias Hepáticas/sangre , Neoplasias Hepáticas/orina , Nanotubos de Carbono/química , Estricnina/sangre , Estricnina/orina

RESUMEN

The purpose of this review is to provide comprehensive and relevant information on the utilization and pharmacological activities of Strychnos nux-vomica Linn. (Loganiaceae), used for the treatment of various diseases. Strychnos nux-vomica is an evergreen tree native to Southeast Asia and its dried seeds are used for the treatment of neurodisorders, arthritis and vomiting. The different use of this plant as herbal remedy in Chinese medicine is also reported in the literature. Strychnine and brucine are major pharmacologically active phytoconstituents of Strychnos nux-vomica, which are central nervous stimulant, but also found to be poisonous at high dosage. Owing to its diversity of phytoconstituents, it is used for treatment of various disorders. Pharmacologically it has been validated for its effect on inflammation, microbial infections, gastrointestinal problem, nervous system, bones cells, cardiovascular systems, cancer and blood glucose level. It also has antioxidant activity and antifeedant activity. Informations about Strychnos nux-vomica, compiled in the present review article could be useful to the researchers for the scientific validation of its traditional claim in the future.

RESUMEN

Objective: To investigate which kind of Chinese medicinal effective fractions will produce good comprehensive cellular pharmacological activities when they were combined with alkaloids from Strychnos nux-vomica and Ephedra sinica, and to evaluate in vivo pharmacological activities of the effective fraction combination screened by cellular experiments. Methods: The equal proportion mixture of alkaloids from S. nux-vomica and E. sinica was set as a sample (sample 1, A); Two samples (samples 2 and 3) were designed by respectively adding the equal ratio mixture of five flavonoids (F) at 50% into alkaloids from S. nux-vomica or E. sinica; Four samples (samples 4-7) were designed by respectively adding F, equal proportion mixture of four saponins (S), equal ratio mixture of six volatile oils/aqueous (V), and equal proportion mixture of six polysaccharides (P) at 50% into A. Murine macrophage cells and chondrocytes were exposed to the new recipes, and then the half inhibitory concentration (IC50) of recipes for inhibiting (PGE2) in macrophages and the half effective concentration (EC50) for promotion of the secretion of IL-6, IL-1β, and TNF-α in macrophages were detected and compared. The interactions among the active fractions were evaluated by comparing the experimental EC50/IC50 values to their corresponding additive EC50/IC50 values calculated by the least square optimum method. The in vivo pharmacodynamics of the best combination was evaluated by the ear swelling model and delayed type hypersensitivity (DTH) model in mice. Results: Sample 4 has good comprehensive activities of cellular anti-inflammation and immunoregulation. Moreover, strong synergistic effect among the effective fractions in this sample was observed; Cellular anti-inflammatory activities of samples 5, 6, and 7 were equivalent with sample 4; Samples 5 and 7 had good comprehensive cellular immunoregulation activity; But the alkaloids mixture (A) and the combinations of S. nux-vomica or E. sinica alkaloids with F (samples 2 and 3) were significantly weaker than sample 4 in cellular anti-inflammation, immunoregulation, and chondrocyte-proliferation. Sample 4 also exhibits a certain effect on in vivo anti-inflammation and immunity in mice when A was decreased at 25% or 5%. Conclusion: It is not suitable to design a combination just by alkaloids from S. nux-vomica and alkaloids of E. sinica; Alkaloids from S. nux-vomica or alkaloids of E. sinica are also not appropriate to solely combine with the mixture of flavonoids (F). When A is combined with F, S, V, and P, respectively, synergistic or additive effects among the active fractions are usually observed. These active fractions help to strengthen comprehensive cellular pharmacological activities of A. Sample 4 not only has good cellular activities of anti-inflammation and immunoregulation but also has better in vivo effect on anti-inflammation and immunity, suggesting that it is feasible to screen the optimized Chinese medicine formula based on cellular pharmacological experiments.

RESUMEN

Seeds of Strychnos nux-vomica were subjected to preliminary phytochemical tests and its presence was confirmed by thin layer chromatography (TLC) method. The TLC profile of the methanolic extract of seeds of S. nux-vomica was developed using the solvent system toluene:chloroform:methanol in the ratio 8:2:1. The plate was observed in visible light after spraying with Dragendorff's reagent (specific method). High-performance liquid chromatography (HPLC) profile of the methanolic extracts of S. nux-vomica was developed, and the amount of strychnine seems to be 0.36% (w/w) in the seeds. The TLC and HPLC profiles developed are very valuable for the identification of the original drug from their adulterants. The TLC profile identifies the presence of strychnine in the plant material. The quantification method for the strychnine in the seeds can be used for the quality standardization of the raw drug because the strychnine is reported to have some toxicity.

RESUMEN

Strychnine-related death has been described since the 19th century. This alkaloid was discovered in 1818. Historically, strychnine was used by the South-East Asian autochthones on their arrows. However, its production was modified by legislation, which was used to protect people against accidental intoxications. Here, we present the case of a 69-year-old man who was found dead at home. During the autopsy, we found a blue substance in the stomach. Toxicological analysis measured strychnine at 0.29 µg/mL in the blood sample, which is a relatively low level in comparison with the results given in the literature. However, histologic examination and toxicological findings permitted the conclusion of strychnine poisoning.

Asunto(s)

Venenos , Estricnina/envenenamiento , Suicidio , Administración Oral , Anciano , Patologia Forense , Toxicología Forense , Contenido Digestivo/química , Humanos , Indicadores y Reactivos/análisis , Masculino , Azul de Metileno/análisis , Estricnina/análisis

RESUMEN

From the angle of dosage form and administration mode to start, the author reviewed the pharmacokinetics of Strychnos nux-vomica and its dosage forms in recent years. The absolute bioavailability of brucine by ig administration is 33.0%-47.8%, and that by injection is about 75%; With brucine as index, strychnos alkaloid by ig administration has the highest blood drug concentration, followed by brucine and nux vomica powder being the lowest; After injecting the brucine or strychnos alkaloid with liposome as a carrier, the brucine bioavailability was improved greatly; In addition, external preparation can reduce the content of brucine and strychnine in the body, which is beneficial to reduce the toxicity; Oral compound preparation extends the action time of brucine and strychnine in vivo, with reducing the peak concentration. However, the pharmacokinetic study on S. nux-vomica and its dosage forms is relatively weak and needs further exploration.

RESUMEN

Objective To prepare and purify the polysaccharides in Shuanqian fungal substance (FS);To study its monosaccharide composition and property. Methods Strychnos nux-vomica was under a thirty-day solid fermentation through Trametes cinnabarina. Then crude polysaccharide was got after the process of drying, smashing, water boiling, condensing, decoloring, removing protein and ethanol precipitation. The content of polysaccharides in Shuanqian FS was determined by phenol-sulfuric acid method. Dialysis and gel chromatography method was used to purify the crude polysaccharide. The purified composition was analyzed by acid hydrolysis and thin layer chromatography. Results The content of crude polysaccharide was 47.68%and yield was 10.52%. It showed that polysaccharide in Shuanqian FS contained glucose and galactose, but no nucleic acid and protein. Conclusion Polysaccharide in Shuanqian FS was an offwhite powdery heteropolysaccharide, which contained glucose and galactose.

RESUMEN

Brucine is an alkaloid derived from the seeds of Strychnos nux-vomica Linn. which have long been used as a traditional medicine for the treatment of hepatocellular carcinoma (HCC) in China. HCC prognosis can be greatly influenced by metastasis. There has thus far been little research into brucine as a source of anti-metastasis activity against HCC. In this study, we revealed that brucine dramatically repressed HepG2 and SMMC-7721 HCC cell migration with few cytotoxic effects. Hypoxia inducible factor 1 (HIF-1) is a key transcription factor mediating cell migration and invasion. Brucine suppressed HIF-1-dependent luciferase activity in HepG2 cells. The transcriptions of four known HIF-1 target genes involved in HCC metastasis, i.e., fibronectin, matrix metallopeptidase 2, lysyl oxidase, and cathepsin D, were also attenuated after brucine treatment. Experiments in vivo showed that an intraperitoneal injection of 5 and 15 mg/kg of brucine resulted in dose-dependent decreases in the lung metastasis of H22 ascitic hepatoma cells. Moreover, a dosage of brucine at 15 mg/kg exhibited very low toxic effects to tumor-bearing mice. Consistently, brucine downregulated expression levels of HIF-1 responsive genes in vivo. Our current study demonstrated the capacity of brucine in suppressing HCC cell migration in vitro and lung metastasis in vivo. The inhibition of the HIF-1 pathway is implicated in the anti-metastasis activity of brucine.

Asunto(s)

Antineoplásicos Fitogénicos/uso terapéutico , Carcinoma Hepatocelular/tratamiento farmacológico , Factor 1 Inducible por Hipoxia/antagonistas & inhibidores , Neoplasias Hepáticas/tratamiento farmacológico , Neoplasias Pulmonares/prevención & control , Estricnina/análogos & derivados , Strychnos nux-vomica/química , Animales , Animales no Consanguíneos , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/efectos adversos , Antineoplásicos Fitogénicos/farmacología , Carcinoma Hepatocelular/secundario , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , China , Relación Dosis-Respuesta a Droga , Etnofarmacología , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Humanos , Factor 1 Inducible por Hipoxia/genética , Factor 1 Inducible por Hipoxia/metabolismo , Neoplasias Pulmonares/secundario , Masculino , Ratones , Proteínas de Neoplasias/antagonistas & inhibidores , Proteínas de Neoplasias/genética , Proteínas de Neoplasias/metabolismo , Distribución Aleatoria , Semillas/química , Estricnina/administración & dosificación , Estricnina/efectos adversos , Estricnina/farmacología , Estricnina/uso terapéutico , Ensayos Antitumor por Modelo de Xenoinjerto

RESUMEN

A 22-year-old male presented with severe myalgias and backache of acute onset, as well as one episode of opisthotonus. On repeated questioning, he admitted to having consumed leaves of Strychnos nux-vomica with suicidal intent. He was treated conservatively with intravenous diazepam and analgesia and made a complete recovery. Strychnine poisoning is rarely encountered and poisoning by consumption of leaves is even rarer. This case demonstrates the potent toxicity of strychnine as well as the effectiveness of therapy when initiated early.