Integrated pharmacokinetics of ginsenosides after intravenous administration of YiQiFuMai powder injection in rats with chronic heart failure by UFLC-MS/MS.

YiQiFuMai powder injection (YQFM), derived from the classical traditional Chinese medicine (TCM) formula Shengmai San, is a modern preparation widely used to combat cardiovascular diseases, chronic heart failure (CHF) for example, in clinical practice in China. Ginsenosides are the major components of YQFM, which are responsible for its therapeutic effect. In this research, we developed a rapid, sensitive and simple method for simultaneous determination of ten ginsenosides from YQFM in CHF rat plasma with ultra-fast liquid chromatography tandem mass spectrometry (UFLC-MS/MS). After solid phase extraction (SPE), chromatography was done on an Acquity UPLC HSS T3 column (1.8µm, 100mm×2.1mm, i.d.) through an 8.0min gradient elution with acetonitrile and 0.1% formic acid in water, while mass spectrometry was performed in the positive ion electrospray ionization (ESI) mode. A good linearity was achieved for each analyte with correlation coefficient (r) >0.9920. The lower limits of quantification (LLOQ) were 1.25ng/mL for ginsenoside Rg1, Rd, Re and Rh1, 2.5ng/mL for ginsenoside Rf, Rg3, Rb2 and Rb3 and 5.0ng/mL for ginsenoside Rb1 and Rc, respectively. All the precision (RSD) data ranged from 1.7-14.5% and the accuracy (RE) data was within ±13.73%. Moreover, the validated method has been applied to investigate the integrated pharmacokinetic profiles of ginsenosides in CHF rats following intravenous administration of YQFM successfully.

Influence of ultrafiltration membrane on ophiopogonins and homoisoflavonoids in Ophiopogon japonicus as measured by ultra-fast liquid chromatography coupled with ion trap time-of-flight mass spectrometry.

Ultrafiltration is one of the most fascinating technologies, which makes it possible to improve the quality of traditional medicines for application in the pharmaceutical industry. However, researchers have paid little attention to the effect of ultrafiltration membrane on traditional medicines chemical constituents. In this work, Ophiopogon japonicus (L.f) Ker-Gawl. was used as an example to illuminate the influence of ultrafiltration with different material and molecular weight cut-off (MWCO) membrane on natural chemical constituents as measured by ultra-fast liquid chromatography coupled with ion trap time-of-flight mass spectrometry (UFLC-IT-TOF/MS). Our results indicated that ultrafiltration membrane significantly impacted homoisoflavonoids, especially homoisoflavonoids that were almost completely retained on the polyethersulfone (PES) membrane. We also found that the larger number of aglycone hydroxy and sugar moiety in steroid saponins, the higher the transmittance. Furthermore, the passage rate (%) of ophiogenin type saponins was higher than that of others. The possible adsorptive mechanisms were hydrogen bonding, hydrophobic interactions, and benzene ring interaction by π-π stacking. In conclusion, it is crucial to choose appropriate ultrafiltration membrane based on the characteristics of produce products for application of ultrafiltration technique.

[Plant metabolomics approach for age discrimination of mountain cultivated ginseng using UPLC-Q-TOF/MS].

Growth year is one of the important factors for the quality of mountain cultivated ginseng (MCG). For age differentiation of MCG, rhizome extracts of ginseng aged from 11 to 15 years were analyzed using a non-targeted approach with ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS)-based on plant metabolomics technique. Multivariate statistical methods such as principal component analysis (PCA) and orthogonal partial least squared discrimination analysis (OPLS-DA) were used to compare the derived patterns among the samples. The results showed that the chemical constituents of MCG rhizome extracts of ginseng aged from 11 to 15 years were different. The data set was subsequently applied to metabolite selection by variable importance in the projection (VIP) for sophisticated classification with the optimal number of metabolites. The OPLS-DA model of MCG has a high interpretability and predictive capability, which established by selecting metabolites of MCG aged from 11 to 15 years. By this approach, MCG samples aged from 11 to 15 years, which are the most in demand in the Chinese ginseng market, can be precisely differentiated on the basis of selected metabolites. This proposed analytical method is fast, accurate, and reliable for discriminating the growth year of MCG. Moreover, this study supplies a new method for the age discrimination of other Chinese medicinal materials.

[Application of metabolomics approach to study of different parts of Mountain Cultivated Ginseng using UHPLC-QTOF/MS].

In present study, an ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UHPLC-QTOF/MS)-based plant metabolomics approach was established to investigate the metabolic profiles of the leaves, main root, branch root, and rhizome of Mountain Cultivated Ginseng (MCG). The UHPLC-QTOF/MS data were subjected to principal component analysis(PCA) and orthogonal partial least squared discrimination analysis(OPLS-DA) to find the potential characteristic components of the four parts of MCG in a quick way. The four different parts could be separated into four different groups of phytochemicals according to the PCA scores. The chemical constituents in four parts of MCG were obviously different. The identities of 81 major peaks that were detected in the four parts of MCG and the potential markers were identified by comparison with the reference compounds or were tentatively assigned by matching the retention time, empirical molecular formula and fragment ions with those of the published compounds of the Panax species. This proposed analytical method is fast, accurate, and reliable for differentiating the different parts of MCG. Moreover, this study supplied a new method for the quality evaluation of other Chinese medicinal materials.

Effects of simvastatin on the proliferation and apoptosis of prostatic epithelial RWPE-1 cells / 中华男科学杂志

<p><b>OBJECTIVE</b>To investigate the effects of simvastatin on the proliferation and apoptosis of prostatic epithelial RWPE-1 cells.</p><p><b>METHODS</b>RWPE-1 cells cultured in vitro were treated with simvastatin at 0, 10, 20, and 40 μmol/L for 24, 48, and 72 hours followed by determination of their proliferation by MTT assay, and their apoptosis by flow cytometry. The mRNA and protein expressions of Bcl-2, Bax, and Cx43 were detected by fluorescence quantitative RT-PCR and Western blot, respectively.</p><p><b>RESULTS</b>After 72 hours of treatment with simvastatin at 10, 20, and 40 μmol/L, the inhibition rates of the RWPE-1 cells were (21.07 ± 6.41)%, (34.87 ± 9.65)%, and (47.18 ± 10.88)%, respectively, significantly higher than (1.21 ± 0.54)% in the control group (P < 0.05) and in a dose-dependent manner (P < 0.05); the cell apoptosis rates were (0.066 ± 0.016)%, (0.126 ± 0.023)%, and (0.192 ± 0.025)%, respectively, remarkably higher than (0.015 ± 0.005)% in the control (P < 0.05) and also in a dose-dependent manner (P < 0.05); the mRNA and protein expressions of Bcl-2 were decreasing while those of Bax and Cx43 increasing with the increased concentration of simvastatin (P < 0.05). The expression of Cx43 was correlated negatively with that of Bcl-2 but positively with that of Bax.</p><p><b>CONCLUSION</b>Simvastatin inhibits the proliferation of prostate epithelial cells and induce their apoptosis by acting on the gap junctional intercellular communication.</p>

[Influlance of different drying methods on quality of Schisandrae Chinensis Fructus].

OBJECTIVE: To study the influence of different drying methods on the quality of Schisandrae Chinensis Fructus and thus provide useful reference for its proper drying methods. METHOD: Schisandrae Chinensis Fructus was processed by eight drying methods including vacuum freeze drying, natural drying in the shade, drying in the sun, oven drying and vacuum drying under different temperature. The contents of the functional ingredients includes chisandrin, gomisin D, gomisin J, schisandrol B, angeloylgomisin H, angeloylgomisin Q, gomisin G, schisantherin A, deoxyschisandrin, schisandrin B, schisandrin C, 5-HMF, total aids and total sugars. The main components change after drying were analyzed by HPLC, ultraviolet spectrophotometry and potentiometric titration. Principal component analysis (PCA) was carried out by SPSS software to evaluate the quality of different processed products from Schisandrae Chinensis Fructus. RESULT: All these results are in accordance with the requirements of Chinese Pharmacopoeia published in 2010, the contents of schisandrin and total eleven lignans were the highest using vacuum drying, and 5-HMF were the lower, oven drying made little difference but with lower schisandrin and higher 5-HMF as the heat increased. CONCLUSION: Different drying methods have significant influence on the quality of Schisandrae Chinensis Fructus. Oven drying under 5°C should be adopted to substitute drying in the sun according to the China Pharmacopoeia published in 2010 for Schisandrae Chinensis Fructus by comprehensive analysis of the cost, content and practicality.

[Study on hydrolysis kinetics of ginsenoside-Ro in alkaline medium and structural analysis of its hydrolyzate].

The ginsenoside-Ro is sensitive to be hydrolyzed in an alkaline medium. This paper investigated the hydrolysis kinetics of ginsenoside-Ro under different pH and temperature values. The results showed ginsenoside-Ro in alkaline solution followed pseudo-first-order reaction. Hydrolysis kinetics of ginsenoside-Ro has not been reported previously. The hydrolysis rate was independent of initial concentration. On the basis of UFLC-MS/MS, NMR, as well as chemical evidence,the structure of hydrolyzate was assigned as 3-O- [beta-D-glucuronopyranosyl- (1 --> 2) -beta-D-glucopyranosyl] -oleanolic acid.

Oral medication of statins retards the progression of benign prostatic hyperplasia and lower urinary tract symptoms / 中华男科学杂志

<p><b>OBJECTIVE</b>To determine whether oral statins can delay the progression of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS).</p><p><b>METHODS</b>We conducted a retrospective cohort study of 50-69-year-old males who came for physical examination in our hospital between January 2003 and December 2008. We designed the inclusion criteria, followed them up for 5 years, and investigated the relationship of oral statins with the clinical progression of BPH and LUTS.</p><p><b>RESULTS</b>Totally, 653 men met the inclusion criteria and were included in this study, of whom 283 were treated with oral statins (group 1) while the other 370 with none (group 2). There were no statistically significant differences between the two groups in age and baseline IPSS, Qmax, and prostate volume (PV) (P > 0.05). During the follow-up, 24 cases in group 1 and 35 cases in group 2 were excluded for obvious dys-uria. A gradual increase was observed in IPSS in both groups 1 and 2 year by year from the baseline to the 5th year of follow-up, but significantly lower in the former group (4.27 +/- 1.16, 4.63 +/- 1.05, 5.27 +/- 0.96, 6.41 +/- 1.04, 7.21 +/- 1.21, and 7.93 +/-1.50) than in the latter (4.24 +/- 1.35, 5.26 +/- 1.23, 6.84 +/- 1.20, 8.75 +/- 1.84, 10.82 +/- 3.01, and 12.98 +/- 4.21) (P < 0.01); a gradual decrease was seen in Qmax, though markedly higher in group 1 ([26.56 +/- 2.09], [24.06 +/- 1.94], [21.33 +/- 1.66], [19.24 +/- 1.54], [17.44 +/- 1.53], and [16.27 +/- 1.37] ml/s) than in group 2 ([26.74 +/- 2.40], [23.62 +/- 2.01], [20.63 +/- 1.69], [17.72 +/- 1.48], [14.82 +/- 1.11], and [11.86 +/- 1.24] ml/s) (P < 0.01); and a gradual increase was found in PV, but remarkably smaller in the former group ([19.82 +/- 4.94], [22.60 +/- 4.99], [25.80 +/- 5.20], [27.92 +/- 5.05], [29.11 +/- 5.24], and [29.97 +/- 5.26] ml) than in the latter ([20.21 +/- 4.78], [24.30 +/- 4.98], [28.50 +/- 5.14], [32.84 +/- 4.77], [36.99 +/- 4.78], and [40.90 +/- 4.78] ml) (P < 0.01). Longer medication of statins was associated with better efficacy.</p><p><b>CONCLUSION</b>Oral statins can significantly delay the clinical progression of BPH and LUTS.</p>

Prophylatic antibiotic use in percutaneous nephrolithotomy: a meta-analysis / 中华外科杂志

<p><b>OBJECTIVE</b>To determine whether antibiotic prophylaxis can reduce the risk of postoperative infective complications in patients undergoing percutaneous nephrolithotomy (PCNL) who have sterile preoperative urine.</p><p><b>METHODS</b>MEDLINE, EMBASE, Cochrane Collaboration Reviews, CMCC and CNKI were searched for RCTs comparing antibiotic prophylaxis with placebo (or blank controls) for patients undergoing PCNL with preoperative sterile urine. The search strategy was made according to the Collaborative Review Group search strategy. Data were extracted by 2 reviewers using the designed extraction form. The software RevMan 4.2 was used to review management and data analysis.</p><p><b>RESULTS</b>A total of 9 trails, 1 placebo controlled, 3 non treatment controlled, and 5 active controlled, involving 1018 patients, met the inclusion criteria. Prophylactic antibiotic use in patients at low risk undergoing PCNL significantly decreased fever (RR = 0.71, 95% CI: 0.54-0.92, P = 0.009), bacteriuria (RR = 0.39, 95%CI: 0.23-0.67, P = 0.0006) and bacteremia incidence (RR = 0.43, 95%CI: 0.25-0.73, P = 0.002). Effective antibiotic classes included quinolone which significantly decreased bacteriuria incidence (RR = 0.31, 95%CI: 0.12-0.82, P = 0.010) and nitrofurantoin which significantly decreased fever incidence (RR = 0.38, 95%CI: 0.24-0.61, P = 0.005). Extended course significantly decreased fever incidence (RR = 0.64, 95%CI: 0.47-0.87, P = 0.004) and bacteriuria incidence (RR = 0.35, 95%CI: 0.18-0.71, P = 0.003).</p><p><b>CONCLUSIONS</b>Prophylactic antibiotics can significantly decrease the incidence of postoperative infective complications. A significant decrease in bacteriuria incidence can be achieved with quinolones. Extended course is effective in decreasing fever, and bacteriuria incidence.</p>

[The lignins from Torreya grandis cv. Merrilli].

AIM: To separate and identify the chemical constituents of the aril of Torreya grandis cv. Merrilli. METHODS: Three lignins were isolated by chromatography and their chemical structures were elucidated by IR, EI-MS, 1HNMR, 13CNMR, DEPT and 2D-NMR spectral methods. RESULTS: Three lignins were identified as pinonesinol, dihydrodehydrodiconiferylalcohol and (7,8-cis-8,8'-trans)-2',4'dihydroxyl-3, 5-dimethoxy-lariciresinol. CONCLUSION: These compounds were isolated from this plant for the first time, and compound III is a new compound.

[Identification of four new ceramides from Anthopleura pacifica].

AIM: To study the bioactive constituents from Anthopleura pacifica. METHODS: Compounds were separated by Pyricularia oryzae bioassay-guided fractionation method with a combination of multi-chromatography. Their chemical structures were determined on the basis of spectral analysis and chemical evidence. RESULTS: A portion showing activity against P. oryzae was obtained and from the portion four compounds were identified as N-hydroxyethyl-N-tetradecanoyl-(2S,3R)-octadecasphinga-4(E), 8(E)-dienine (a), N-hydroxyethyl-N-(9Z-hexadecenoyl)-(2S,3R)-octadecasphinga-4 (E), 8 (E)-dienine (b), N-hydroxyethyl-N-hexadecanoyl-(2S,3R)-octadecasphinga-4(E), 8 (E)-dienine (c) and N-hydroxyethyl-N-(13Z-docosenoyl-(2S,3R)-octadecasphinga-4(E), 8(E)-dienine(d). CONCLUSION: All the four compounds are new ceramides.

Isolation and structure of the cytotoxic cycloheptapeptide phakellistatin 13.

A new cyclic heptapeptide phakellistatin 13 (1) had been isolated from the sponge Phakellia fusca Thiele, collected at Yongxing Island of China. Its structure was elucidated as cyclo-(Pro1-Trp-Leu-Thr-Pro2-Gly-Phe) on the basis of MS, UV, IR, and high-field NMR (600 MHz) analysis. The compound was significantly cytotoxic against the human hepatoma BEL-7404 cell line with an ED(50) < 10(-2) microg/mL.