Targeted metabolomic analysis of phenylpropanoid metabolites in Astragalus membranaceus var. mongholicus in response to Fusarium solani infection / 药学学报

Root rot severely restricts the sustainable development of Astragalus membranaceus var. mongholicus (AMM) industry. Resistance breeding is an economical and environmentally safe way to manage the disease and its key lies in the obtaining of resistance indicators. This study aimed to quickly and accurately screen the resistance-related (RR) metabolites so as to provide reference for the screening of indicators of AMM breeding for resistance. LC-MS-based targeted metabolomics and real-time quantitative PCR technology were employed, in combination with multivariate statistical analysis, in analyzing the dynamic changes of phenylpropanoid metabolites in AMM in response to root rot pathogen Fusarium solani (FS) infection and identifying the differential metabolites. The LC-MS method established showed high sensitivity; each metabolite had a good linear relationship (R2 ≥ 0.968 9) in the corresponding linear range of the respective standard curve; the recoveries and the relative standard deviations (RSDs) (n = 6) ranged from 70% to 107% and from 1.2% to 9.9%, respectively. Obvious disturbances were observed in the changes of the targeted metabolites in AMM infected by FS. These metabolites, compared with the mock-inoculated (CK) group, showed different up or down regulation with time series. Calycosin-7-O-β-D-glucoside, ononin, calycosin and formononetin were identified as differential metabolites, and they all belong to flavonoids. The first three compounds were significantly negatively correlated (r ≤ -0.97, P < 0.05) with the content of FS in the root of AMM. As potential RR metabolites, they are helpful in obtaining promising resistance indicators for AMM against FS infection.

Expression and Significance of Serum Mir-132 in Patients with Obstructive Sleep Apnea with Cognitive Impairment / 中山大学学报(医学科学版)

@#【Objective】To explore the relationship between the miR- 132 expression in serum and cognitive deficits of OSA. 【Methods】 66 Chinese adults age 30 to 60 years old were enrolled and categorized into two groups based on Montreal Cognitive Assessment（MoCA）scores： OSA patients with cognitive impairment（OSAI，n=36），OSA patients without cognitive impairment（OSAN，n=30），and thirty adults without OSA as healthy control group（HC，n=30）. Out- of- center cardiopulmonary sleep testing （OCST） and MoCA assessment were performed and the relative expression of miR-132 in serum was detected by PCR.【Results】No significant difference was observed in age，education，gender and hypertension（P>0.05）. The relative expression level of miR-132 was significantly up-regulated in OSAI patient′s serum compared to the OSAN and HC patients （P<0.001），and had a positive correlation with MoCA score （r=- 0.726，P<0.001）. ROC analyses showed that the areas under the curve（AUC）were statistically significant from the line of identity in OSA with cognitive impairment（AUC=0.935，95% CI：0.890- 0.981，P<0.001）and in OSA（AUC=0.787，95% CI：0.695-0.879，P<0.001）.【Conclusions】Elevated serum miR-132 expression levels are closely related to the diagnosis of OSA and its cognitive dysfunction. Detection of serum miR- 132 may be a potential indicator of cognitive dysfunction and diagnosis in OSA patients.

Effects of nitrogen level on growth of Tetrastigma hemsleyanum and phytochemical content and antioxidant activity in stems and leaves / 中国中药杂志

As a rare endangered medical plant that newly cultivated,little experimental information is available for growth and metabolites of Tetrastigma hemsleyanum in response to nitrogen( N). The effects of different levels of N on growth of T. hemsleyanum and the content of phytochemicals( polysaccharide,total flavonoids and phenolics) and antioxidant activity( ABTS and FRAP) in stems and leaves were investigated in this study. A certain amount of N had positive effects on most of biological traits,and excessive dose of N went against growth of T. hemsleyanum. With N levels decreased,the polysaccharide content in stems and leaves had no significant change,while the total flavonoid and phenolic content,and antioxidant activities increased steadily. Antioxidant activities and total flavonoid and phenolic content had significant positive correlation. Excessive N fertilizer should be avoided by cultivation.

Status of libraries and databases for natural products at abroad / 中国中药杂志

For natural products are one of the important sources for drug discovery, libraries and databases of natural products are significant for the development and research of natural products. At present, most of compound libraries at abroad are synthetic or combinatorial synthetic molecules, resulting to access natural products difficult; for information of natural products are scattered with different standards, it is difficult to construct convenient, comprehensive and large-scale databases for natural products. This paper reviewed the status of current accessing libraries and databases for natural products at abroad and provided some important information for the development of libraries and database for natural products.

Flavone C-glycosides from seeds of Ziziphus jujuba var. spinosa / 中国中药杂志

Five flavone C-glycosides were isolated from the methanol extract of the degrease seeds of Ziziphus jujuba var. spinosa though various column chromatography methods including silica gel, MPLC, and HPLC. The structures were elucidated as 6"-feruloyl- 6'''-vanillylspinosin(1), 6",6'"-diferuloylspinosin(2), spinosin(3), swertisin(4) and isoswertisin(5) based on the NMR and MS spectral data. 1 is a new compound.

Analysis and thinking on status of constituent library of traditional Chinese Medicines in China / 中国中药杂志

Natural products from traditional Chinese medicines (TCMs) are one of the important sources for drug discovery. Systematic investigation on chemical constituents of TCMs plays one key role in TCMs R & D. Research and development on the constituent library of TCMs including the constituent repository and database (eCL-TCMs) is significant for the modernization of TCMs and new drug R & D. This paper reviews the status of current compound libraries and databases in China, analyzes some key problems, and proposes the necessity and ideas of the running eCL-TCMs supported by the National New Drug Innovation Great Project of China (2011ZX09307-002-02). The eCL-TCMs are large-scale, high-quality, comprehensive, standard, open-access, and are integrated with quality control system, drug screening and discovery platforms.

Sedative, hypnotic and antiseizure effects of compound gardenia oil and jujube seed oil in mice / 南方医科大学学报

<p><b>OBJECTIVE</b>To study the sedative, hypnotic and antiseizure effects of the compound preparation of gardenia oil and jujube seed oil in mice and investigate the interaction of the two drugs in this preparation.</p><p><b>METHODS</b>The compound preparation was administered intragastrically in mice, whose spontaneous activity was observed along with their tolerance of the preparation after long-term administration. The hypnotic effect of the compound was assessed by investigating the changes in the pentobarbital sodium-induced sleeping. The compound was tested for its antiseizure effect in mice with pentetrazole-induced clonic and tonic convulsion. Diazepam was used as the standard control in all experiments.</p><p><b>RESULTS</b>The jujube seed oil, the gardenia oil and their compound all inhibited spontaneous activities of the mice. Compared with diazepam, the compound showed slow action in producing the sedative effect, which increased gradually with prolonged drug administration without obvious drug tolerance responses. The compound and the two oils all showed synergistic action with pentobarbital sodium in inducing sleeping of the mice. Prescription study showed that the compound produced stronger sedative and hypnotic effects than either of the oils. The two oils and the compound did not show significant antiseizure effects in mice.</p><p><b>CONCLUSION</b>The compound of jujube seed oil and gardenia oil has sedative and hypnotic effects in mice, and the two oils in the compound show obvious synergistic effect.</p>

Repeated oral treatment with polysaccharide sulfate reduces insulin resistance and dyslipidemia in diabetic dyslipidemic rat model / 药学学报

Polysaccharide sulfate (PSS) is a new type of antiatherosclerotic medicine for its effects of anticoagulation, anti-thrombosis and modulation of dyslipidemia. However, it is still uncertain whether PSS could modulate the diabetic dyslipidemia or not. Here, the rat model of diabetic dyslipidemia was developed and the effects of PSS on glucose and lipid levels were investigated in this animal model. Wistar rats were iv injected with streptozotocin 20 mg x kg(-1) after feeding with high fat diet for one and a half month. Then, rats received orally PSS (30, 90, and 180 mg x kg(-1)) for 1 month. After oral treatment with PSS (90 and 180 mg x kg(-1)) for 1 month, the levels of triglyceride (TG), total cholesterol (TC), low density lipoprotein-cholesterol (LDL-C) were significantly reduced and the level of high density lipoprotein-cholesterol (HDL-C) increased, compared with diabetic control rats. Moreover, PSS (30, 90, and 180 mg x kg(-1)) had a tendency to reduce glucose and insulin levels, and significantly increased insulin sensitivity index. Our results suggest that PSS could improve insulin sensitivity and relieve dyslipidemia in diabetic dyslipidemic rats.

Pentoxifylline promotes learning and memory function of aging rats and mice with induced memory impairment / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effects of pentoxifylline on rats and mice with learning and memory dysfunctions.</p><p><b>METHODS</b>Morris water maze test was used to observe the effects of pentoxifylline on learning and memory of naturally aging rats, and jumping stand test was performed to examine its effects in promoting the learning and memory functions in mice with scopolamine- and ethanol-induced memory dysfunctions.</p><p><b>RESULTS</b>In aging rats, pentoxifylline at high, moderate and low doses all significantly reduced the latency of platform finding in the place navigation test (P<0.01 or P<0.05 ), and increased the quadrant searching frequency in the spatial probe test (P<0.05). Pentoxifylline at the 3 doses significantly increased the latency of electrification (P<0.01 or P<0.05) and decreased the times of error (P<0.05) of the mice as compared with scopolamine- treated group. Pentoxifylline also improved ethanol-induced memory dysfunction in the mice, but the changes in the performance of the mice were not statistically significant.</p><p><b>CONCLUSION</b>Pentoxifylline can improve the learning and memory abilities of rats and mice.</p>

Determination of tramadol and its active metabolite O-desmethyltramadol in plasma and amniotic fluid using LC/MS/MS / 药学学报

<p><b>AIM</b>To determinate tramadol and O-desmethyltramadol in human plasma and amniotic fluid by LC/MS/MS, and distribution of tramadol and O-desmethyltramadol in maternity and fetus were studied.</p><p><b>METHODS</b>Samples containing tramadol, O-desmethyltramadol and diphenhydramine (internal standard, IS ) were extracted using liquid-liquid extraction, followed by liquid chromatographic separation and on-line MS/MS using atmospheric pressure chemical ionization as an interface detection. The analytes were detected in the selected reaction monitoring mode.</p><p><b>RESULTS</b>The calibration curves for tramadol and O-desmethytramadol in plasma and amniotic fluid were linear in the range from 8.0 to 800.0 microg x L(-1) (plasma) and 1.0 to 400.0 microg x L(-1) (amniotic fluid). The method was applied to the measurement of tramadol and O-desmethytramadol concentrations in maternal vein, umbilical vein, umbilical artery and amniotic fluid. Following intramuscular pre-operative administration 1.5 mg x kg(-1) doses of tramadol to parturients, plasma concentrations of tramadol were significantly higher than those in amniotic fluid. The concentrations of O-desmethyltramadol in plasma were lower, and were not detected in amniotic fluid.</p><p><b>CONCLUSION</b>The method is shown to be accurate, robust and convenient, and suitable for clinical pharmacokinetics studies of tramadol and O-desmethyltramadol.</p>

Determination of levodropropizine and its pharmacokinetics in human plasma using LC/MS/MS / 药学学报

<p><b>AIM</b>To develop a rapid and sensitive LC/MS/MS method for the analysis of levodropropizine in plasma and study the pharmacokinetics of levodropropizine in healthy Chinese volunteers.</p><p><b>METHODS</b>Levodropropizine and zolmitriptan (internal standard, IS) were extracted from plasma samples and chromatographed on a C18 column and detected using a tandem mass spectrometer with a TurboIon Spray ionization interface. Quantitation was performed using multiple reaction monitoring (MRM) of the transitions of the m/z 237 --> m/z 120 for levodropropizine and m/z 288 --> m/z 58 for the IS.</p><p><b>RESULTS</b>The limit of quantification of the method for levodropropizine was 0.25 microg x L(-1). The assay was linear over the concentration range from 0.25 to 500.0 microg x L(-1) and intra- and inter-day precision over this range were < 11.4% with good accuracy.</p><p><b>CONCLUSION</b>The method is shown to be accurate, and suitable for clinical pharmacokinetic study of levodropropizine.</p>