In this study, araucarene diterpenes, characterized by a pimarene skeleton with a variably oxidized side chain at C-13, were investigated. A total of 16 araucarene diterpenoids and their derivatives were isolated from the woods of Agathis dammara, including 11 previously unreported compounds: dammaradione (1), dammarones D-G (2, 5, 14, 15), dammaric acids B-F (8-12), and dammarol (16). The structures of these new compounds were elucidated using high-resolution electrospray ionization mass spectroscopy (HR-ESI-MS) and one-dimensional/two-dimensional (1D/2D) nuclear magnetic resonance (NMR), while their absolute configurations were determined through the electronic circular dichroism (ECD) exciton chirality method and Snatzke's method. The hypoglycemic activity of all isolated compounds was evaluated using a transgenic zebrafish model, and a structure-activity relationship (SAR) analysis was conducted. Araucarone (3) and dammaric acid C (9), serving as representative compounds, demonstrated significant hypoglycemic effects on zebrafish. The primary mechanism involves the promotion of pancreatic β cell regeneration and glucose uptake. Specifically, these compounds enhance the differentiation of pancreatic endocrine precursor cells (PEP cells) into β cells in zebrafish.
Zebrafish ; Animals ; Diterpenes/isolation & purification* ; Insulin-Secreting Cells/cytology* ; Glucose/metabolism* ; Hypoglycemic Agents/isolation & purification* ; Molecular Structure ; Structure-Activity Relationship ; Plant Extracts/pharmacology* ; Regeneration/drug effects*

Objective To assess the pharmacokinetic characteristics of two types of tofacitinib citrate tablets in healthy individuals and evaluate their bioequivalence and safety.Methods A randomized,two-period,self-crossing design was used with 36 subjects in two groups in both fasting and postprandial conditions.Each group received 5 mg tofacatile citrate tablets of either generic tofacitinib citrate tablets(T)or the reference product(R)per period,and the plasma concentration of tofacatile tablets was detected by LC-MS/MS.Phoenix WinNonlin software was used to calculate pharmacokinetic parameters and evaluate its bioequivalence.Results After single oral administration of test and reference preparations,the main pharmacokinetic parameters were as follows:Cmax values in fasting group were(57.54±13.95)and(59.17±12.31)ng·mL-1,respectively;AUC0,values were(143.83±34.58)and(142.13±33.00)ng·h·mL-1,respectively;AUC0-∞ values were(147.39±35.27)and(146.15±34.64)ng·h·mL-1,respectively;tmax was 0.5 h for both;Cmax values in the postprandial group were(57.16±17.56)and(55.19±21.98)ng·mL-1;AUC0-t values were(165.47±41.63)and(162.04±41.84)ng·h·mL-1;AUC0-∞ values were(171.88±44.15)and(168.05±44.21)ng·h·mL-1;The t max was 1.0 h for both.The 90％confidence intervals for the geometric mean ratios of Cmax,AUC0-t and AUC0-∞ in fasting group and postprandial group were 96.35％(90.11％-103.03％)and 105.91％(95.20％-117.83％),101.02％(98.76％-103.34％)and 102.23％(99.67％-104.86％),100.77％(98.53％-103.06％)and 102.40％(99.81％-105.06％),all within the range of 80.00％-125.00％.Conclusion Both types of generic tofacitinib citrate tablets are bioequivalent and safe in Chinese healthy individuals.

Objective:To compare the pharmacokinetics consistence of baicalin between traditional slice decoction and dispensing granule decoction of Huanglianjiedu decoction. Methods:After the gastric administration of the two decoctions at low, middle and high dose in rats, an HPLC method was used to detect the content of baicalin in the plasma, and then DASS 2. 1. 1 software was used to cal-culate the pharmacokinetic parameters. Results:After the administration of the two decoctions at low, middle and high dose, the phar-macokinetic parameters were as follows:Cmax of 0. 25 and 0. 27μg·ml-1 ,0. 30 and 0. 31 μg·ml-1 ,0. 40 and 0. 45 μg·ml-1;AUC of 2. 48 and 2. 59μg·ml-1 ·h,3. 59 and 3. 71μg·ml-1 ·h,5. 71 and 6. 16μg·ml-1 ·h;Tmax of 3. 0 and 3. 0 h,3. 0 and 3. 0 h, 4.0 and 4.0 h;Vd of (2 822.4 ±118.2) and (2 998.9 ±255.6) L·kg-1,(3 102.6 ±176.3) and (3 405.3 ±213.8) L·kg-1, (4 231.2 ±155.4) and (4 486.0 ±187.0) L·kg-1;CL of (2 923.3 ±215.6) and (2 767.5 ±184.6)L·h-1·kg-1,(4 921.7 ± 225.4) and (4 040.8 ±246.7)L·h-1·kg-1,(5 255.9 ±189.7) and (4 868.7 ±260.4)L·h-1·kg-1;and t1/2 of (3.88 ± 0.41) and (3.71 ±0.37)h,(4.19 ±0.36) and (3.73 ±0.51)h, (5.54 ±0.38) and (5.80 ±0.54)h. Conclusion: The pharma-cokinetic parameters of baicalin have no significant difference between traditional slice decoction and dispensing granule decoction of Huanglianjiedu decoction.

Objective:To analyze the characteristics of infectious diseases from neurology ward and provide reference for the treat-ment. Methods:The consultation record of the neurological patients who suffered infection diseases were retrospectively summarized from January 2011 to December 2013. All the consultation were performed by clinical pharmacists. SPSS 19. 0 software was used to an-alyze the adoption and prognosis of the outcomes. Results:In 439 consultation cases,256 patients(58. 31%)were older than 65 years. Most of the cases were respiratory infection(294 cases,65. 33%),urinary tract infection(40 cases,8. 89%)and intracranial infection(37 cases,8. 22%). There were 510 strains of bacteria isolated by culturing,in which 362 strains were gram-negative bacte-ria(70. 98%),127 strains were gram-positive bacteria(24. 90%)and 21 strains were fungi(4. 12%). The top five of pathogenic bac-teria were Pseudomonas aeruginosa(125 stains,24. 51%),Acinetobacter baumannii(93 stains,18. 24%),Staphylococcus aureus(88 stains,17. 25%),Staphylococcus aureus(68 stains,13. 33%)and Escherichia coli. (32 stains,6. 27%). The detection rates of ESBLs of K. pneumonia and E. coli were 61. 36% and 75. 00%,respectively. Among 125 strains of P. aeruginosa,the sensitive rate to meropenem and inipenem was 65. 8% and 70. 6%,respectively. A. baumannii was highly multidrug resistant,and 21 strains (22. 58%)with pan-drug resistance were isolated. Gram-positive bacteria were highly sensitive to vancomycin and teicoplanin. Totally 35 strains(52. 24%)of MRSA were isolated. The complete adoption rate of consultation opinion was 84. 74%(372 cases),the partial adoption rate was 7. 28%(32 cases),and 35 cases(7. 97%)were declined. In all the adopted cases(319 cases,78. 96%)showed effectiveness. In the linear correlation analysis,the consultation adoption and therapy outcomes had significant correlation(P<0. 01). Conclusion:Clinical pharmacists can improve the efficiency in anti-infection therapy and play important roles in the treatment of infec-tious diseases in neurology ward,especially in the treatment of drug-resistant bacterial infections.

OBJECTIVETo determine quercetin and kaempferol in the plant of genus Dysosma that come from different species, different plant parts or different growing areas, which provide the basis of rational utilization of Dysosma plants.

METHODThe analysis was performed on a Diamonsil C18 column (4.6 mm x 150 mm, 5 microm) eluted with the mobile phase of methanol-water containing 0.1% phosphoric acid (60:40). The flow rate was 1 mL x min(-1), the detection wavelength was 360 nm; and the column temperature was set at 25 degrees C.

RESULTThe linear ranges of quercetin and kaempferol are 0.22-1.1 microg and 0.42-2.1 microg. The average recoveries of quercetin and kaempferol are 97.1% (RSD 1.4%) and 99.6% (RSD 2.4%); respectively.

CONCLUSIONThe contents of flavones in different species of Dysosma are significantly different.

Berberidaceae ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Chromatography, Reverse-Phase ; methods ; Drugs, Chinese Herbal ; analysis ; Kaempferols ; analysis ; Quercetin ; analysis

OBJECTIVE:To determine the content of ceftizoxime for injection METHODS:A RP-HPLC method was established,the polarls C18 was used as analysis column The mobile phase consisted of 0 23% sodium hydrogen phosphate and 0 14% trisodium buffer-acetonitrile(85∶15),the flow rate was 1 0ml/min,the detection wavelength was 254nm RESULTS:The linear range of ceftizoxime was 4 1 462～37 3 156?g/ml,r=0 9 999 The relative standard deviation was 0 6% CONCL_USION:The method is rapid,accurate and suitable for determination of content of ceftizoxime for injection

OBJECTIVE:To establish the quality standard of Adansan eye-drops(ADS).METHODS:Saliva miltiorrhiza and ATP were qualitatively detected by TLC and HPLC respectively.Atropine sulfate was quantitatively detected by VIS-spectrophotometry.RESULTS:The average recovery was 99.9% with a RSD of 2.46%(n=5).CONCLUSION:This method is simple,accurate and specific.It can be used for the quality control of ADS.