Optimization of the pressurized processing technology of Strychnos nux-vomica boiled with mung beans based on genetic algorithm / 中国药房

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.

Analysis of Medication Rules of the Prescription Containing Strychnos nuxvomica in the Dictionary of Traditional Chinese Medicine Prescription / 中国药房

OBJECTIVE： To provide reference for the clinical use and dosage form development of Strychnos nuxvomica. METHODS： The prescriptions containing S. nuxvomica were collected and sorted from the Dictionary of Traditional Chinese Medicine Prescription， and then formula name， prescription source， name of treatment disease， composition， usage and dosage， medication route were input into Access 2010 and database was established. According to the usage， these prescriptions were divided into internal use and external use， and the frequencies of diseases treated by internal/external use prescriptions were counted respectively. Apriori algorithm of SPSS Modeler 18.0 software was used to analyze the drug combination rule of compound prescription containing S. nuxvomica. RESULTS： A total of 78 prescriptions were included， of which 42 were oral prescriptions， 33 were external prescriptions and 3 were both oral and external prescriptions. Internal prescriptions were used to treat diseases such as atrophy-flaccidity disease， arthralgia， hemorrhoids， anal fistula， bones and muscles pain. The external prescriptions were mainly used to treat skin diseases， tumors， lump. Internal and external prescriptions could treat sore， injuries and fractures. In internal prescriptions， S. nuxvomica was often compatible with Boswellia carterii， myrrha， Daemonorops draco， Manis pentadactyla， pyritum， Angelica sinensis， Ephedra sinica， Aconitum kusnezoffii. In external prescriptions， S. nuxvomica was often compatible with Radix Paeoniae， Rehmannia glutinosa， Phellodendron chinense， Coptis chinensis， Scutellaria baicalensis， Angelica sinensis， Angelica dahurica， Buthus martensii. Most of S. nuxvomica were used after processing， and mainly took sesame oil as an auxiliary material （77.97％）. CONCLUSIONS： Diseases treated with the prescriptions containing S. nuxvomica can be classified into three types of diseases， i.e. polymyalgia rheumatica and paralysis， bruise and bone fracture， carbuncle and stubbornness tinea. In external prescriptions， S. nuxvomica is often compatible with drug for clearing heat and drying dampness， cooling blood and activating blood， and relieving pain. In internal prescriptions， S. nuxvomica is often compatible with the agents for blood-activating and stasis-resolving medicinal. In addition， the processing of S. nuxvomica with sesame oil is an important measure to ensure its safety.

Comparison on celluar anti-inflammatory and immunoregulatory activities of seven derivative combinations of Yaotongning with alkaloid as main part and in vivo pharmacodynamic evaluation on optimized candidate combination / 中草药

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.

Research progress on pharmacokinetics of Strychnos nux-vomica and its preparation / 中草药

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.

Preparation, Purification and Property of Polysaccharides in Shuanqian Fungal Substance / 中国中医药信息杂志

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.

A rare case of strychnine poisoning by consumption of Strychnos nux-vomica leaves

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.

Determination of Strychnine and Brucine in the Decoction of Semen Strychni and Its Different Processed Products / 中国中医药信息杂志

Objective HPLC method was used to determine strychnine and brucine in the decoction of Semen Strychni and its processed products of Jiangxi methods and innovated methods.Methods SiO2 was used as the stationary phase,n-hexane∶dichloromethane∶methanol∶ammonia(47.5∶47.5∶5∶0.35) as the mobile phase,with detection wavelength at 254 nm.Result The contents of strychnine and brucine in the processed products of Jiangxi methods and innovated methods were low.The content of that in acetic acid-soaked product scalded with hot sand was the lowest.Conclusion Semen Strychni and its processed products of Jiangxi methods and innovated methods can lower the toxicity and improve the safety of clinical use.

Quantitative Determination of Total Alkaloids from Seeds of Strychnos nux-vomica L / 中药新药与临床药理

Objective To establish the method for the determination of the content of total alkaloids extracted from seeds of Strychnos nux-vomica L. Methods The content of total alkaloids in the samples was determined by the acid dye colorimetry, which was performed with brucine and strychnine as the reference substances, dibromothymolsulfonphthalein as the acidic dye under the condition of a buffer solution (pH=7.2), and chloroform was used as the extractant. Results Both the concentration of brucine being 0.041 2～ 0.206 mg/mL and that of strychnine being 0.042 8～ 0.214 mg/mL had a good linear relationship with the absorbance. The average recoveries for brucine and strychnine were (101.8? 4.6) % and (103.3? 2.7) % , respectively. Conclusion The established method is simple, accurate and stable, and can be used for the determination of the content of the total alkaloids extracted from the seeds of Strychnos nux-vomica L.

The preparation and acute toxicity of stealth liposomes containing total alkaloids from seeds of Strychnos nux-vomica L / 中成药

AIM: To prepare stealth liposomes containing total alkaloids from seeds of Strychnou nux-vomica L.and compare the acute toxicity with corresponding conventional liposomes. METHODS: The content of total alkaloids in the samples was determined by the acidic dyecolorimetry,which was performed with brucine as the reference substance.The total alkaloids and the purity were determined.The optimal technique of strychnine stealth liposome was used to prepare stealth liposome containing total alkaloids.Stealth liposomes and conventional liposomes containing the total alkaloids were both prepared by ammonium sulfate transmembrane gradients.The encapsulation efficiency,particle size and acute toxicity were compared between stealth liposomes and conventional liposomes. RESULTS: By the use of optimized prescription and technique,the entrapment efficiency and yield efficiency of strychnine stealth liposome were 90.64% and 98.82%,respectively.The encapsulation efficiency of stealth liposomes and conventional liposomes were 80.97% and 73.01%,respectively.The mean particle sizes were 106.5nm and 163.4nm,respectively.The LD_(50) of solution,conventional liposomes and stealth liposomes were 1.85,2.56 and 3.42 mg/kg,respectively. CONCLUSION: The optimized preparation method of strychnine stealth liposome can be used to prepare corresponding stealth liposome containing total alkaloids from seeds of Strychnou nux-vomica L.As the drug delivery system,the characteristics of stealth liposomes are more satisfactory than the corresponding conventional liposomes.