OBJECTIVE：To optimize the water extraction and ethanol precipitation technology of Zhuang medicine Baijin granules. METHODS ：HPLC method was adopted to determine the content of bergenin in Baijin granules extract. The extraction routes of Baijin granules （water decoction ，70％ ethanol reflux extraction ，water decoction combined with 70％ ethanol reflux extraction）was screened primarily with the yield of extract and the experiment of reducing uric acid of mice. The orthogonal test was adopted to optimize water extraction technology of Baijin granules with water multiple ，extraction time and extraction times as factors，taking the extraction yield and the bergenin content as index ，then the validation test was carried out. The orthogonal test was adopted to optimize the alcohol precipitation process of Baijin granules including the relative density of medicinal materials ， alcohol content and the alcohol precipitation time ，then the validation test was carried out. By the experiment of reducing uric acid ， the effects of medicinal materials extract of Baijin granules extract were compared before and after ethanol precipitation. RESLUTS：Established method for content determination of bergenin with linearity range of 0.007 2-0.288 mg/mL，had good precision，reproducibility，stability and accuracy. The initially chosen extraction process of Baijin granules was water decoction extraction. The optimal water extraction technology was soaked for 0.5 h，then decocted for 3 times with 14-fold water （mL/g）and 1.0 h each time. The optimal ethanol precipitation process was to concentrate the water extract to a relative density of 1.0 g/mL with alcohol content of liquid at 60％ and precipitated for 12 h. Validation tests showed that RSDs of extract yield and beragenin content were all lower than 2％（n＝3）. The experiment of pharmacodynamics showed that water extract （before ethanol precipitation ）and water extract after alcohol precipitation could significantly decrease the level of uric acid in hyperuricemia model mice （P＜0.01）. There was no statistical significance in the reduction of uric acid between 2 groups（P＞0.05）. CONCLUSIONS ：The optimized water extraction technology can obtain good extract yield and bergenin content ，and combined with ethanol precipitation technology for removing excess impurities would not affect the pharmacodynamics. The water extraction and ethanol precipitation technology is feasible，and can be used for extracting the medicinal materials of Baijin granules and its edulcoration.

Objective To establish the quality standards for salt eucommia dispensing granules. Methods The extractives were obtained by alcohol extraction method. HPLC was applied for the determination of pinoresinol diglucoside in dispensing granules. HPLC fingerprints were established by the contrast of Agilent 1260 HPLC, Waters HPLC and various chromatogram column. Results Pinoresinol diglucoside showed a good linear relationship ( Y = 2. 9594X + 3. 2825,R2 =0.9999) at 102.8-2056.0 mg?L-1 with average recovery of 99.85％ (RSD = 0.31％,n = 9). Conclusion The method is easy-operated and accurate,which has a good specificity for the quality control of common salt eucommia dispensing granules.

Objective To select the optimal preparation technology of zucapsaicin cream and compare it with zuacta cream.Methods Cold stability,thermal stability,centrifugal stability,and appearance were used as indicators to select the ratio of prescription.In this study preparation technology was optimize by using orthogonal experiment method,and transdermal absorption of the homemade zucapsaicin cream and zucata cream were investigated by employing modified Franz diffusion pool.Results The optimized preparation technology was as follows,emulsifying temperature was maintained at 70 ℃,the stirring speed was set at 2 000 r·min-1,the main medicine was added into the oil phase,emulsifying time was 30 min.The results showed that there was no significant difference between the homemade zucapsaicin cream and the reference Zuacta cream.Conclusion The homemade zucapsaicin were tested to have reasonable ratio of prescription,stability,and definite transdermal effect,which was basically in accordance with zuacta cream.

OBJECTIVETo study the effect of total saponins from Entada phaseoloides (TSEP) on islet morphology and skeletal muscle PI3K pathway-related protein expression of type 2 diabetic rats.

METHODType 2 diabetic rats were induced by high-fat diet and low-dose streptozotocin and then randomly divided into 5 groups, i.e. the normal control, the model group, the positive control drug (200 mg x kg(-1) metformin), the low-dose TSEP (25 mg x kg(-1)) group and the high-dose TSEP (50 mg x kg(-1)). Three weeks later, the islet morphology of rat pancreas were observed by HE staining, and protein expressions of insulin receptor substrate-1 (IRS-1), phosphatidylinositol 3-kinase (PI3K), protein tyrosine phosphatase-1B (PTP-1 B) and glucose transporter 4 (GLUT4) in rat skeletal muscle were detected by Western blot.

RESULTCompared with the modal group, TSEP administration groups showed relatively normal structures, clear pancreatic cells and intact capsula structures in pancreatic tissue pathological sections, with the number of pancreatic islets close to the normal control group. Meanwhile, above TSEP administration groups showed increased IRS-1, PI3K and GLUT4 protein expressions in their skeletal muscle tissues and decreased PTP-1B protein expression compared with the model group.

CONCLUSIONTSEP has an effect on protecting pancreatic tissues of type 2 diabetic rats and intervening in abnormal expression of proteins in skeletal muscle tissues.

Animals ; Diabetes Mellitus, Type 2 ; drug therapy ; Fabaceae ; chemistry ; Glucose Transporter Type 4 ; analysis ; Islets of Langerhans ; drug effects ; pathology ; Male ; Muscle, Skeletal ; drug effects ; pathology ; Phosphatidylinositol 3-Kinases ; analysis ; Rats ; Rats, Sprague-Dawley ; Saponins ; therapeutic use

OBJECTIVETo study in vitro anti-tumor activity of phaseoloideside E (PE) with human hepatoma HepG2 cells as the objective.

METHODMTT assay was adopted to detect the cytotoxic effect of PE of different concentrations on HepG2 cells after being processed for 48 h. Changes in morphology of PE-processed cells were observed under an optical microscope and fluorescence microscope. DNA agrose gel electrophoresis was used to detect the DNA ladder, an important characteristic of cell apoptosis. The expression levels of Bax and Bcl-2 were determined by western blot assay.

RESULTPE dramatically repressed the viability of HepG2 cells. Typical morphological changes of apoptosis had been detected by both direct microscopic observation and Hoechst 33,258 staining. Typical DNA Ladder was also observed by agarose gel electrophoresis in the administration group, but it did not exist in the control group. Western blot showed that the expression of Bax was up-regulated and Bcl-2 was down-regulated.

CONCLUSIONAbove data demonstrates that PE can induce apoptosis in human hepatoma HepG2 cells, and indicate that PE-induced expression level changes of Bax and Bcl2 may be related to the apoptosis-induction effect.

Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Cell Proliferation ; drug effects ; Hep G2 Cells ; Humans ; Proto-Oncogene Proteins c-bcl-2 ; analysis ; Saponins ; pharmacology ; Triterpenes ; pharmacology ; bcl-2-Associated X Protein ; analysis

OBJECTIVETo study water-soluble chemical constituents from the leaves of Elaeagnus pungens.

METHODChemical constituents of E. pungens leaves were separated by a combination of macroporous resin column chromatography, reverse phase silica gel column chromatography, Sephadex LH-20 column chromatography and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties using the spectral method.

RESULTThe two compounds were separated from E. pungens leaves and identified as kaempferol 3-O-P-D-glucopyranosyl- (1-->3)-alpha-L-rhamn-opyranosyl-(1-->6) -/3-D-galactopyranoside (1), kaempferol 3-O-P-D-glucopyranosyl-(1-->3)-alpha-L-rhamnopyranosyl-(1-->6)-beta-D-glucopyranoside-7-O-beta-D-glucopyranoside (2).

CONCLUSIONCompound 2 separated from E. pungens leaves was a new compound.

Elaeagnaceae ; chemistry ; Glucosides ; chemistry ; Plant Leaves ; chemistry ; Solubility ; Water ; chemistry

OBJECTIVEA novel method was established and the results were compared for HPLC fingerprint determination of crude and processed products of Entada phaseoloides.

METHODHPLC-UV was proposed for studying the fingerprints of fresh E. phaseoloides and their processed products, respectively. HPLC-ESI-MS was introduced to analyze the common peaks in each batch of crude E. phaseoloides.

RESULTSixteen characteristic peaks were found in crude E. phaseoloides samples and twenty-one common peaks existed in processed E. phaseoloides samples. Nine characteristic peaks of which were identified by comparison of the retention time and their molecular weights of chemical standards, most of which were identificated belong to triterpenoid saponins and glucosides.

CONCLUSIONAfter processed, the chemical composition of the extraction with solution of 60% methanol from crude E. phaseoloides are less or more than that from processed E. phaseoloides, and the changes of the main peaks of fingerprint chromatographic suggest that HPLC can be used to reflect the difference of chemical composition of E. phaseoloides and their processed products. It would be an efficient way for qualitative control of E. phaseoloides.

Chemistry, Pharmaceutical ; China ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; Fabaceae ; chemistry

To study the chemical constituents of the Entada phaseoloides (L.) Merr., seeds of Entada phaseoloides were extracted with 70% ethanol at room temperature. Isolation and purification were performed by silica gel, reversed-phase silica gel column chromatography and semi-preparative HPLC. Structures of the pure compounds were established on the basis of spectral analysis. Four sulfur-containing amide compounds were isolated from the n-BuOH-soluble fraction and identified as entadamide A-beta-D-glucopyranosyl-(1-->3)-beta-D-glucopyranoside (1), entadamide A (2), entadamide A-beta-D-glucopyranoside (3) and clinacoside C (4). Compound 1 is a new compound. Compound 4 is isolated from the genus Entada for the first time.

To study the chemical constituents from the root of Berchemia lineata (L.) DC., nine compounds were isolated from the EtOAc extract by using silica gel, RP-C18 silica gel column chromatography and preparative HPLC. Based on the spectroscopic analysis, their structures were identified as 5-hydroxy-7-(2'-hydroxypropyl)-2-methyl-chromone (1), (-)-(1'R, 2'S)-erythro-5-hydroxy-7-(1', 2'-dihydroxypropyl)-2-methyl-chromone (2), naringenin (3), eriodictyol (4), (+)-aromadendrin (5), (+)-taxifolin (6), (+)-catechin (7), (+)-epigallocatechin (8) and quercetin (9). Among them, compound 2 is a new chromone derivative. Compound 1 is a known chromone derivative and isolated from this genus for the first time. Compounds 3-9 are known flavonoids and isolated from this plant for the first time.

To study the chemical constituents of aerial parts of Laggera pterodonta (DC.) Benth., the air-dried aerial parts of this plant were powered and extracted with boiling water and purified by silica gel column chromatography and recrystallized. Eleven compounds were obtained from L.pterodonta. They were identified as to be 6-O-β-D-glucopyranosyl-carvotanacetone (1), pterodontic acid (2), 1β-hydroxy pterondontic acid (3), pterodontoside A (4), pterodondiol (5), pterodontriol B (6), 5-hydroxy-3,4′,6,7-tetramethoxyflavone (7), artemitin (8), chrysosplenetin B (9), quercetin (10) and β-sitosterol (11). Compound 1 is a new monoterpene glucoside. Compounds 10 and 11 were isolated from this plant for the first time. Compounds 2 and 5 showed moderate activity against bacteria including Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Mycobacteium phlei and Bacillus circulans by paper disc diffusion method, while they both displayed no activity against Escherichia coli.