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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.
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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.
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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.
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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.
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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.
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A new gas chromatography-mass spectroscopy (GC-MS) method is being presented for the separation and detection of strychnine and brucine, alkaloids of Strychnos nux vomica in a single run. The analysis was carried out using 5% phenyl methyl silicone capillary column, electron impact ionization mode and quadrupole mass analyzer. The extracts of the exhibits were analyzed using the new method. The peaks of the two alkaloids were found to be well resolved, and there was clear separation between the two. The retention time and mass fragmentation pattern, base peaks, molecular peaks of strychnine and brucine standard/NIST library and crime case exhibits matched, establishing the presence of the two active principles of Strychnos nux vomica. The new method has the advantage of better separation of the two alkaloid peaks over the conventional GC-MS methods, and is useful for the identification and confirmation of Strychnos nux vomica constituents in biological matrices of poisoning cases that have ended in death.
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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.
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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.
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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.
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AIM To study the tissue distribution of strychnos nux vomica alkaloids in rats. METHODS Rats were given strychnos nux vomica alkaloids intravenously and strychnine(S), brucine(B), strychnine N oxide(SNO), brucine N oxide(BNO) in every tissue was determined by HPLC timely. RESULTS The concentration of S, B, SNO and BNO were high in brain and spinal marrow. CONCLUSION S, B, SNO and BNO all have the ability to permeate blood brain barrier.