Determination of Aloesin in Rat Plasma by LC-MS/MS and Its Pharmacokinetic Study / 中国药房

OBJECTIVE：To establish a method for the determination of aloesin in plasma of rats ，and to investigate pharmacokinetic characteristics of aloesin. METHODS ：The plasma samples were precipitated with methanol. Using aloeresin D as internal standard ，the plasma concentration of aloesin was determined by LC-MS/MS. The determination was performed on Synergi Hydro-RP column with mobile phase consisted of 0.1‰ formic acid-methanol （gradient elution ）at the flow rate of 0.50 mL/min. The column temperature was 30 ℃，and sample size was 5 µL. The electrospray ionization source was applied to carry out negative ion detection with multiple reaction monitoring mode . The ion transitions for quantitative analysis were m/z 393.1→272.9（aloesin） and m/z 555.3→144.9（internal standard ），respectively. The concentration of aloesin in venous blood was determined by above method at 0.083，0.167，0.333，0.667，1，1.5，2.5，4，6，8，10 h after intravenous injection （3.35 mg/kg）and intragastric administration（16.75 mg/kg）of aloesin. DAS 3.0 software was used to calculate pharmacokinetic parameters. RESULTS ：The linear range of aloesin were 1-600 ng/mL（r＝0.994 5）. The lower limit of quantification was 1 ng/mL，and RSDs of within and between batches were less than 15％；accuracies within and between batches were within ±15％. The matrix factors were （92.74± 4.33）％-（94.84±2.57）％，and extraction recoveries were （69.04±2.13）％-（75.03±2.84）％；the deviation between the measured results of the stability test and the theoretical values were within ±15％. After intravenous injection and intragastric administration of aloesin ，main pharmacokinetic parameters were as follows ：cmax were（10 693.3±2 745.3）and（223.3±36.2）ng/mL；t1/2 were （2.45±1.45）and（3.33±1.91）h；AUC0－24h were（4 190.6±883.6）and（1 210.1±93.9）ng·h/mL（n＝3）. Absolute bioavailabi- lity was 11.13％. CONCLUSIONS ：The established method is rapid and sensitive for plasma determination of aloesin ，and suitable for its pharmacokinetic study.

Research progress in molecular mechanism of bone homeostasis imbalance due to bone infection / 中华创伤杂志

Bone infection is an osteal disorder with bone damage resulting from infection of bone marrow，cortex，periosteum and surrounding tissues，characterized by a high incidence and severe symptoms. The treatment is often complicated and prolonged. Regardless of the method used，the goal is to reduce bone defect caused by infection，control infection，rebuild impaired tissues，and promote bone healing，so as to restore bone homeostasis. Starting from bone homeostasis，the authors review the research progress in the commonly used drugs and molecular mechanisms that affect bone formation-related pathways caused by bone infection，activate bone resorption-related mechanisms，and regulate bone homeostasis，in order to provide a theoretical basis for reducing bone defect caused by bone infection and promoting bone healing.

A new phenolic glycoside from prunella vulgaris / 药学学报

A new phenolic glycoside was isolated from the spikes of Prunella vulgaris. Its structure was elucidated as gentisic acid 5-O-beta-D-(6'-salicylyl)-glucopyranoside by spectroscopic evidence and chemical analysis.

Optimization of the hydrolysis process for C21 steroidal glycoside of bai shou wu by acetic acid with multi-target orthogonal design / 中国中药杂志

<p><b>OBJECTIVE</b>To study the optimizal hydrolysis process for C21 steroidal glycoside of Bai Shou Wu by acetic acid.</p><p><b>METHOD</b>The effects of acetic acid concentration, reaction temperature and reaction time had been investigated using orthogonal design and the contents of kidjoranin 3-O-beta-digitoxopyranoside, caudatin, kidjoranin 3-O-alpha-L-diginopyranosyl-(1 --> 4)-beta-cymaropyranoside and caudatin 3-O-beta-cymaropyranoside as response indexs were determined by the high performance liquid chromatography.</p><p><b>RESULT</b>The factors influencing acetic extraction efficiency were as follows: A > B > C (A. reaction temperature; B. reaction time; C. acetic acid concentration). The optimal hydrolysis condition obtained was: refluxing for 6 hours with 5.0% dilute CH3COOH solution at 100 degrees C.</p><p><b>CONCLUSION</b>The content of antitumor active ingredients under the optimum hydrolysis condition is raised obviously and has a great part in studying this antitumor drug.</p>

Effects of three C21 steroidal saponins from Cynanchum auriculatum on cell growth and cell cycle of human lung cancer A549 cells / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the inhibition of three C2 steroidal saponins from Cynanchum auriculatum on the cell growth and cell cycle of human lung cancer A549 cells.</p><p><b>METHOD</b>A549 cells were exposed to three C21 steroidal saponins of different concentrations (5, 10, 20, 40, 60, 80, 100 micromol L(-1)) for 48 hours. After 48 h, MTT assay was used to evaluate the inhibiting effects of three C21 steroidal saponins on the proliferation of the A549 cells. Exponential growth phase A549 cells were treated with 47, 34, 60 micromol x L(-1) of three C21 steroidal saponins respectively for 12, 24, 48 h, then the changes of cell cycle were analyzed by flow cytometry.</p><p><b>RESULT</b>The three C21 steroidal saponins could inhibit the growth of A549 cells in dose-dependent manner and IC50 is 46. 07 mol x L(-1), 33.02 mol x L(-1), 59.92 mol x L(-1) respectively. The cell cycle analysis showed that wilfoside C1N and wilfoside C3N increased the percentage of G0/G1 phase cells and decreased G2/M and S-phase cells while the proportion of cells in S-phase was lower and in G2/M phase the proportion was higher than control when the cells were cultivated with wilfoside K1N (P < 0.05, P < 0.01).</p><p><b>CONCLUSION</b>Three C21 steroidal saponins could inhibit the proliferation of A549 cells in dose-dependent manner and the mechanism may be related to its arresting the cell cycle.</p>

Chemical constituents from Hedyotis diffusa / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents from Hedyotis diffusa.</p><p><b>METHOD</b>The compounds were isolated and purified by various chromatographic techniques and identified by their physicochemical properties and spectral data.</p><p><b>RESULT</b>Eight compounds had been reported in last paper, and this time eight more compounds were isolated and identified as 6-hydroxystigmasta-4,22-dien-3-one (1), 3-hydroxystigmasta-4,22-dien-7-one (2), 2-hydroxy-3-methylanthraquinone (3), 2,6-dihydroxy-3-methyl-4-methoxyanthraquinone (4), iso-scutellarein (5), isoetin (6), aesculetin (7), gypsogenic acid (8).</p><p><b>CONCLUSION</b>Compounds 1-3, 5-8 were obtained from the genus Hedyotis for the first time.</p>

A new alkaloid from Salsola collina / 药学学报

Salsola collina is widely distributed in droughty and semi-droughty area, which is used as a kind of folk remedy in traditional Chinese medicine for treatment of hypertension. The study is on the chemical constituents of this herb from its aerial parts to obtain its active constituents. Dried and crushed aerial parts of this herb were extracted three times with 95% EtOH at reflux. The ethanol extracts were combined and concentrated under reduced pressure at 70 ℃ to yield residue, which was suspended in water and successively partitioned with light petroleum, chloroform and n-butanol. The chloroform and n-butanol fractions were treated by various chromatographic techniques, such as silica gel, C18 reversed-phase silica gel and macroporous resin column chromatography. Compounds were elucidated by their physicochemical properties and spectroscopic analysis. In the course of our study on searching biological active components from this herb, a new alkaloid together with three known alkaloids were isolated and identified as N-transferuloyl-3-methyldopamine (1), 3-[4-(β-D-glucopyranosyloxy)-3- methoxyphenyl]-N-[2-(4-hydroxyl-3-methoxyphenyl)ethyl]-2-propenamide (2), salsoline A (3), salsoline B (4). Compound 4 is a new compound and named as salsoline B, while compound 2 was obtained in Salsola collina for the first time.