Identify metabolites of Piper longum alkaloids in feces and urine of rat by HPLC-FT-MS / 中国中药杂志

The metabolites were detected in feces and urine of rats orally administrated alkaloids of Piper longum by using high performance liquid chromatography coupled with a Fourier Transform ion cyclotron resonance mass spectrometer (HPLC-FT-MS). According to the mass spectrometric data and reported literature, the structures of metabolites were identified. Several metabolites were analyzed and belonged to piperine, piperanine, piperlonguminine, Δα,β-dihydropiperlonguminine and pellitorine, respectively. The metabolites of alkaloids from P. longum alkaloids were produced through Ⅰ phase and Ⅱ phase metabolism reaction, and were excreted with urination and defecation. The approach provided a rapid method for characterizing the metabolites of P. longum alkaloids and gave the truly active structures and the action mechanism of their neuroprotective effects.

The efficacy and safety of testa triticum tricum purif in treatment of functional constipation in the late middle-aged and elderly patients: a multicenter randomized controlled clinical trial / 中华内科杂志

Objective To evaluate the efficacy and safety of testa triticum tricum purif for the treatment of functional constipatiofi(FC) in the late middle-aged and elderly patients.Methods This study was designed as a multicenter randomized controlled trial.Patients who met Rome Ⅲ diagnostic criteria of FC were enrolled,with age between 55-85 years old.Those with organic diseases were excluded.The patients were randomly allocated to receive testa triticum tricum purif (3.5 g bid) or polyethylene glycol 4000 powder (PEG4000,10g bid) for 8 weeks,followed by single dose of maintenance therapy for 4 weeks.Follow-up visits were at 4 and 12 weeks after treatment discontinuation.The independent investigators in each center evaluated the constipation symptoms scores.The primary endpoints included rates of significant improvement,improvement and overall improvement at the end of 2,4 and 8 weeks of therapy,which were calculated by the reduction of symptom scores ≥ 75 ％,50％-74％,≥ 25 ％ respectively.Results A total of 127 FC subjects were enrolled from 3 centers,and 122 cases valid for final analysis.The mean age was (69.4 ± 6.9) years old,including 62 cases in testa triticum tricum purif group and 60 cases in PEG4000 group.The demographic data,constipated symptoms scores and proportion of FC subtypes at baseline were comparable.The rates of significant improvement,improvement and overall improvement in testa triticum tricum purif and PEG4000 groups at the end of 2,4 and 8 weeks were 37.70％ (23/61) vs 59.32％(35/59) (P=0.018),57.38％ (35/61)vs74.14％ (43/58) (P=0.054),and64.41％ (38/59)vs 79.31％ (46/58) (P =0.073) respectively.Testa triticum tricum purif therapy significantly improved the proportion of spontaneous bowel movement (SBM) ≥ 3 times/week from 43.55％ (27/62) to 80.33％ (49/61),83.61％ (51/61) and 93.22％ (55/59) at 2,4,and 8 weeks respectively (all P＜0.01),which were comparable with PEG4000 group (all P ＞ 0.05).The proportion of normalized stool forms in study group was significant higher than that of control group at the end of 8 weeks [86.44％ (51/59) vs 67.24％ (39/58),P =0.014].Only one patient complained mild abdominal distension during testa triticum tricum purif therapy.Conclusions The efficacy of testa triticum tricum purif for the treatment of FC in late middle-aged and older patients is comparable with osmotic laxatives PEG4000,which has significant effect on normalization of fecal forms and reliable safety.

DbcAMP inhibitted the proliferation of FTC-133 cell / 重庆医学

Objective To study the effect of dualdi butyryl cyclic AMP (dbcAMP)on the proliferation of FTC-133 cell line. Methods FTC-133 cells were normally cultured and divided into control group,dbcAMP treatment group (0.5,1.0,2.0 mmol/L). After FTC-133 cells were treated with dbcAMP (0.5,1.0,2.0 mmol/L)for 24 h or 48 h,the growth activity and growth curve was detected by MTT.Changes of the cell cycle were detected by flow cytometry.The mRNA and protein expression of Raf1 were measured by RT-qPCR and Western blotting.Results Compared with control group,the growth activity of FTC-133 cells was re-duced by different levels of dbcAMP in a dose-time dependence manner.The number of FTC-133 cells was decreased in the S phase and increased in the G2/M phase.The mRNA and protein expression of Raf1 of treatment group were both reduced compared with control group.Conclusion dbcAMP significantly reduced FTC-133 cells proliferation and promoted apoptosis,and which might be involoved by ERK MAPK signalling.

Induction of BAG2 in proteasome inhibitor-induced apoptosis in human thyroid carcinoma cells / 中国癌症杂志

Background and purpose: For neoplasms with different sources, proteasome inhibitors can inhibit their growth and promote the cell apoptosis. Its mechanism may be associated with Bcl-2-associated athanogene 2 (BAG2). We aimed to investigate the involvement of in thyroid cancer cell death induced by proteasome inhibitors. Methods:A panel of thyroid cancer cells (ARO, FRO, KTC1, KTC2, KTC3, 8305C and 8505C) were treated with vehicle or proteasome inhibitor MG132;BAG2 mRNA and protein levels were analyzed using quantitative real-time polymerase chain reaction (qRT-PCR) and Western blot, respectively. Results:MTT results indicated that FRO and KTC2 cell lines were the most sensitive to proteasome inhibitors. MG132 induced BAG2 mRNA and protein expression in the panel of thyroid cancer cells with various degree (P<0.01), for FRO and KTC2 cell line, the BAG2 mRNA level was increased in 20 to 25 times, meanwhile the protein expression level also increased signiifcantly;Sensitive FRO cells demonstrated quicker induction of BAG2 compared with insensitive ARO cells. Moreover, the extents of BAG2 induction in FRO cells were higher than that in ARO cells. Conclusion: BAG2 is a novel molecule induced by proteasome inhibitor, which might function as a proapoptotic molecule in thyroid cancer cell death mediated by proteasome inhibitor.

Protective effect of alkaloids from Piper longum in rat dopaminergic neuron injury of 6-OHDA-induced Parkinson's disease / 中国中药杂志

<p><b>OBJECTIVE</b>To discuss the protective effect of alkaloids from Piper longum (PLA) in rat dopaminergic neuron injury of 6-OHDA-induced Parkinson's disease and its possible mechanism.</p><p><b>METHOD</b>The rat PD model was established by injecting 6-OHDA into the unilateral striatum with a brain solid positioner. The PD rats were divided into the PLA group (50 mg x kg(-1) x d(-1)), the madorpa group (50 mg x kg(-1) x d(-1)) and the model group, with 15 rats in each group. All of the rats were orally given drugs once a day for 6 weeks. Meanwhile, other 15 rats were randomly selected as the sham operation group, and only injected with normal saline in the unilateral striatum. The behavioral changes were observed with the apomorphine (APO)-induced rotation and rotary rod tests. The number of tyrosine hydroxylase (TH)-positive cells in rat substantia nigra and the density of TH-positive fibers in striatum were detected by tyrosine hydroxylase immunohistochemistry. The content of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), glutathione (GSH), catalase (CAT), malondialdehyde (MDA), nitric oxide (NO) and nitric oxide synthase (NOS) in rat substantia nigra and striatum were measured by the spectrophotometric method.</p><p><b>RESULT</b>After being induced by APO, PD rats showed obvious rotation behaviors, with decreased time stay on rotary rod and significant reduction in the number of TH-positive cells in sustantia nigra and the density of TH-positive fibers in striatum. The activities of SOD, GSH-Px, CAT, the content of GSH and the total antioxidant capacity significantly decreased, whereas the activities of NOS and the content of MDA, NO significantly increased. PLA could significantly improve the behavioral abnormality of PD rats and increase the number of TH-positive cells in sustantia nigra and the density of TH-positive fibers in striatum. It could up-regulate the activities of SOD, GSH-Px, CAT, the content of GSH and the total antioxidant capacity, and decrease the content of NOS and the content of MDA, NO.</p><p><b>CONCLUSION</b>Alkaloids from P. longum shows the protective effect in substantia nigra cells of 6-OHDA-induced PD model rats. Its mechanism may be related with their antioxidant activity.</p>

Endemic fluorosis surveillance in Qinan County of Gansu Province from 2004 to 2007: an outcome analysis / 中国地方病学杂志

Objective To investigate the prevalence of endemic fluorosis and the progress acchieved through control measures in Taian County of Gansu Province so as to provide basis and technique support for endemic fluorosis control. Methods The survey was carried out according to the National Surveillance Scheme of Endemic Fluorosis. Fulfillment of control measures and the quality of water improving projects were surveyed. Samples of household water and urine in children aged 8-12 years were collected and fluoride content was detected by iron selective electrode method. Children's dental fluorosis were examined with Dean method. Results In Qinan County, water was improved in a rate of 100%. In water-improving and defluoridation projects investigated, 81.15% (99/122) projects worked well, 18.85% (23/122) projects were closed or abandoned. The number of water improvement projects monitored were 24,81,9,8,respectively in the year through 2004 to 2007, revealing 13 projects having water fluorine content(>1.0-2.0 mg/L) in 2004, 15 and 5 projects having water fluorine content higher that 1.0-2.0 and 2.0-4.0 mg/L respectively in 2005, 2 projects having water fluorine content(>1.0-2.0 mg/L) in 2006, and no projects above 4.0 mg/L. In Anfu Village, the fluorine content of source and drinking water were all below 1.0 mg/L in 2006 and 2007. The urinary fluoride content of 8-12 years old children was equal and higher than 1.5 mg/L, dental fluorosis rate was 34.47% (354/1027), and dental fluorosis index was 0.65 in 2004-2007. Conclusions Projects running out of status and excessive levels of water fluorine are frequently seen, dental fluorosis is not controlled in Taian County of Gansu Province

Association between serum amyloid A and intima-media thickness of common carotid artery in patients with type 2 diabetes / 中华内分泌代谢杂志

A total of 169 patients with short-duration type 2 diabetic mellitus (DM) were divided into atherosclerosis (AS) group and non-AS group according to the intima-media thickness (IMT) of three conducting arteries.The level of serum amyloid A (SAA) was assayed by ELISA.The results showed that SAA level of type 2 DM patients increased significantly, patients in AS group showed higher SAA level than that in non-AS group, and SAA level was positively correlated with age, body mass index, waist hip ratio and IMT of common carotid artery.Age, C-reactive protein and SAA level are the major risk factors for IMT of common carotid artery.

A novel triterpenoid saponin from Prunella vulgaris / 药学学报

To study the constituents of the Prunella vulgaris L, the constituents were isolated by various column chromatography and the structures were identified on the basis of chemical and spectral analysis. One saponin compound (I) and one flavone glycoside compound (II) were obtained from Prunella vulgaris L. Their structures were elucidated as 16-oxo-17-demethyl-3beta,24-dihydroxylolean-12-en-3-O-beta-D-glucuronoside (I), and acacetin-7-O-beta-D-glucopyranoside (II). Compound I is a novel triterpenoid saponin and named as prunelloside A. Compound II was obtained for the first time from the Prunella genus.