Optimization of Extraction Process for Active Ingredients in Seeds of Sophora alopecuroides by Plackett-Burman Design and Response Surface Analysis / 中国药学杂志

OBJECTIVE: To optimize extraction process for active ingredients in seeds of Sophora alopecuroides, to provide a reference for scale production. METHODS: Active ingredients from Sophora alopecuroides were extracted by ethanol, with average yield of oxysophocarpine and oxymatrine as index, some factors affecting index were firstly evaluated by Plackett-Burman design, then taking oxysophocarpine and oxymatrine as indexes respectively, extraction conditions were optimized by Box-Behnken design, experimental data was fitted by multiple linear regression and binomial formula fitting, extraction process was optimized by response surface method, and prediction was carried out through comparing the observed and predicted value. RESULTS: Extracting times, crushing degree and solvent times had significant effects on yields of oxysophocarpine and oxymatrine; binomial equation fitted well with good predictability. optimum extraction technology of Sophora alopecuroides was as following:crushed through 65 mesh sieve, extracted 4 times with 12-fold the amount of 60% ethanol for 2 h each time; yield of oxysophocarpine and oxymatrine was 92.3%, 78.6% respectively, both deviations were small by comparing with the predicted value. CONCLUSION: This extraction process is reasonable and feasible by Plackett-Burman design and response surface analysis with good predictability. This study can provide experimental basis for further scale production of Sophora alopecuroides.

Study on Vasodilatory Effect of Oxysophocarpine on Isolated Thoracic Aortic Rings of Rats and Its Mechanism / 中国药房

OBJECTIVE： To study the vasodilatory effect of oxysophocarpine （OSC） on isolated thoracic aortic rings of rats and its possible mechanism. METHODS： Thoracic aortic rings of rats were collected （called “vascular ring” for short）. Using K-H nutrient solution as blank control and the diastolic rate as index， the effects of different concentrations （0.2-1.0 mg/mL） of OSC on normal vascular rings in basal state， normal or endothelium-free vascular rings pre-contracted by norepinephrine （PE， 1×10－6 mol/L） were investigated. After pre-culturing normal thoracic aortic rings by nitric oxide synthase inhibitor L-nitro-arginine methyl ester（L-NAME）and cyclooxygenase inhibitor indomethacin（INDO），as well as pre-culturing endothelium-free vascular rings by potassium ion channel blocker BaCl2，tetraethylammonium（TEA）and 4-aminopyridine（4-AP）， the diastolic effects of OSC of different concentrations （0.2-1.0 mg/mL） on the above vascular rings were investigated by using the same method. RESULTS： Compared with blank control， there was no significant effects of different concentrations of OSC on the diastolic rate of normal vascular rings in basal state （P＞0.05）， but 0.4-1.0 mg/mL OSC could significantly improve the diastolic rate of normal or endothelium-free vascular rings pre-contracted by PE （P＜0.01）， in concentration-dependent manner. After preculturing with L-NAME， INDO， 4-AP and BaCl2， different concentrations of OSC had no significant effect on the diastolic rate of normal or endothelium-free vascular rings pre-contracted by PE （P＞0.05）. After pre-culturing with TEA and Gli， 0.4-1.0 mg/mL OSC could significantly reduce the diastolic rate of endothelium-free vas- cular rings pre-contracted by PE （P＜0.01）. CONCLUSIONS： OSC did not significantly dilate the thoracic aortic rings of rats in the basal state within the dose range （0.2-1.0 mg/mL）， but OSC of 0.4-1.0 mg/mL have significant diastolic effects on the normal or endothelium-free thoracic aortic rings of rats pre-contracted with PE. The mechanism of thoracic aortic rings dilation is endothelium-independent， which may be associated with receptor operational calcium channel，Ca2+-activated potassium channels and ATP-sensitive potassium channels.

Discussion and consideration on safety of Sophorae Tonkinensis Radix et Rhizoma and its rational use / 中草药

Sophorae Tonkinensis Radix et Rhizoma is known as the important drug for treating sore throat and is widely used in clinic. Because of the coexisting of its efficacy and poison, Sophorae Tonkinensis Radix et Rhizoma often leads to a series of safety problems in the clinical application process. In this study, we attempt to analyze the ultimate cause of the toxicity of Sophorae Tonkinensis Radix et Rhizoma by reviewing nearly 20 years of literature, discuss the substance of its efficacy/toxicity from the point of view of chemical composition, and put forward exploratory thinking on its clinical rational application.

Extraction and separation of oxysophocarpine from Sophora alopecuroides by inverse three-phase membrane cycle method / 中草药

Objective: To establish the HPLC method for determination of oxysophocarpine (OSC) and optimize the extraction and purification technology of OSC from Sophora alopecuroides by inverse phase membrane. Methods: Based on single-factor test, the influence of aqueous phase and organic phase volume ratio, the concentration of sodium hydroxide and hydrochloric acid, and the extraction cycle time were investigated using orthogonal design method. Results: OSC was determined by Shim-pack VP-ODS chromatographic column (250 mm×4.6 mm, 5 μm), mobile phase was methanol-0.2% phosphoric acid aqueous solution (7:93), gradient elution, flow rate was 1 mL/min, column temperature was 30℃, and detection wavelength was 221 nm. The ratio of aqueous phase and organic phase volume was 1:1, hydrochloric acid concentration was 0.03 mol/L, sodium hydroxide concentration was 0.5 mol/L, water pump flow rate was 6 mL/min, and cycle time was 60 min. The extraction rate of OSC 98.21% in 60 min was under the best experimental conditions. OSC had good linearity relationship within the range of 0.01-0.7 mg/mL, r2=0.9978, and the respective average recovery rate was 97.47%, RSD=1.95%. Conclusion: This extraction technology is simple operation, with low organic solvent consumption, and can be used for alkaloids extraction.

Determination of Five Kinds of Alkaloids in Sophorae Flavescentis Radix by HPLC / 中国中医药信息杂志

Objective To determine the content of sophocarpine, matrine, oxysophocarpine, sophoridine, oxymatrine in Sophora Flavescentis Radix from different areas. Methods Agilent ZORBAX NH2 column (4.6 mm×150 mm, 5 μm) was used with mobile phase of acetonitrile-ethanol-3% phosphate (84∶10∶6), at a flow rate of 1 mL/min. The wavelength of detection was 210 nm. Results The linear range of sophocarpine, matrine, oxysophocarpine, sophoridine and oxymatrine were 0.022 88-0.114 4 μg (r=0.999 7), 0.083 2-0.416 0 μg (r=0.999 7), 0.376 2-1.836 0 μg (r=0.999 8), 0.104 4-0.522 μg (r=0.999 2), 0.491 2-2.456 μg (r=0.999 9), respectively. The average recovery were 101.63% (RSD=2.08%), 98.29%(RSD=1.87%), 101.89% (RSD=1.97%), 99.87% (RSD=2.06%), 102.66% (RSD=1.34%), respectively. Conclusion The method is simple, rapid and accurate, and suitable for the quality control of Sophorae Flavescentis Radix.