Discovery of cyclooxygenase-2 inhibitors from Kadsura coccinea by affinity ultrafiltration mass spectrometry and the anti-inflammatory activity.

The medicinal plant Kadsura coccinea distributing in South China, was widely used for reducing inflammation and relieving pain. Previous study in our laboratory had proved the significant therapeutic effects of K. coccinea extract on adjuvant arthritis rats. To explore the responsible components and possible mechanisms, an AUF-HPLC-Q-TOF/ MS method was employed for screening and characterizing COX-2 ligands from K. coccinea stems for the first time. Meanwhile, the molecular docking was performed to simulate the binding modes for ligands and COX-2, the cell-free enzyme activity assay was applied to verify the direct COX-2 inhibition of potential inhibitors, and the cell-based study on COX-2 expression was to evaluate the anti-inflammatory effect of (+)-Anwulignan. As a result, the potential COX-2 inhibitor (+)-Anwulignan significantly suppressing COX-2 expressions in LPS signaling pathways might be a good candidate for anti-inflammation and analgesia. In conclusion, AUF mass spectrometry combining the molecular docking and bioassays in vitro was an efficient approach for discovering enzyme inhibitors from traditional herbs.

Traditional Chinese medicine combined with conventional therapy for female kidney stone: A protocol for systematic review.

INTRODUCTION: Kidney stone is caused by abnormal accumulation of crystalline substances in the kidneys. Kidney stone is one of the urinary system diseases with a high incidence. In this study, we will use the research method of randomized controlled trials to explore the effects of Traditional Chinese medicine combined with western medicine on renal function and urine metabolism in women with kidney stones. We hope that the results of this study will provide more evidence-based medical evidence for TCM to treat kidney stones, and also provide patients with more treatment options. METHODS/DESIGN: This pragmatic randomized controlled trial will recruit 100 patients who are diagnosed with kidney stone. Simple randomization to conventional drug treatment with a 1:1 allocation ratio will be used. The participants will continue to receive ESWL treatment and TCM therapy. The selection of outcomes will be evaluated by the overall effectiveness of clinical efficacy. DISCUSSION: This trial may provide evidence regarding the clinical effectiveness, safety, and cost-effectiveness of Traditional Chinese medicine for patients with Female kidney stone.

Berberine versus placebo for the prevention of recurrence of colorectal adenoma: a multicentre, double-blinded, randomised controlled study.

BACKGROUND: Chemoprevention of colorectal adenoma and colorectal cancer remains an important public health goal. The present study aimed to investigate the clinical potential and safety of berberine for prevention of colorectal adenoma recurrence. METHODS: This double-blind, randomised, placebo-controlled trial was done in seven hospital centres across six provinces in China. Individuals aged 18-75 years who had at least one but no more than six histologically confirmed colorectal adenomas that had undergone complete polypectomy within the 6 months before recruitment were recruited and randomly assigned (1:1) to receive berberine (0·3 g twice daily) or placebo tablets via block randomisation (block size of six). Participants were to undergo a first follow-up colonoscopy 1 year after enrolment, and if no colorectal adenomas were detected, a second follow-up colonoscopy at 2 years was planned. The study continued until the last enrolled participant reached the 2-year follow-up point. All participants, investigators, endoscopists, and pathologists were blinded to treatment assignment. The primary efficacy endpoint was the recurrence of adenomas at any follow-up colonoscopy. Analysis was based on modified intention-to-treat, with the full analysis set including all randomised participants who received at least one dose of study medication and who had available efficacy data. The study is registered with ClinicalTrials.gov, number NCT02226185; the trial has ended and this report represents the final analysis. FINDINGS: Between Nov 14, 2014, and Dec 30, 2016, 553 participants were randomly assigned to the berberine group and 555 to the placebo group. The full analysis set consisted of 429 participants in the berberine group and 462 in the placebo group. 155 (36%) participants in the berberine group and 216 (47%) in the placebo group were found to have recurrent adenoma during follow-up (unadjusted relative risk ratio for recurrence 0·77, 95% CI 0·66-0·91; p=0·001). No colorectal cancers were detected during follow-up. The most common adverse event was constipation (six [1%] of 446 patients in the berberine group vs one [<0·5%] of 478 in the placebo group). No serious adverse events were reported. INTERPRETATION: Berberine 0·3 g twice daily was safe and effective in reducing the risk of recurrence of colorectal adenoma and could be an option for chemoprevention after polypectomy. FUNDING: National Natural Science Foundation of China.

Baeckeins L and M, two novel C-methylated triflavonoids from the roots of Baeckea frutescens L.

Baeckea frutescens is a medicinal plant distributing from Southeast Asia to Australia. A pair of novel diastereomeric C-methylated triflavonoids named baeckeins L (1) and M (2) were isolated from the roots of B. frutescens. The structures of these isolates were elucidated by analysis of the 1D (1H/13C) and 2D NMR (HSQC/HMBC/NOESY) and HR-ESI-MS spectroscopic data, and the absolute configurations of chiral carbons (C-2/C-3/C-2°/C-3°) were established by CD spectrometry combined with quantum chemical calculations.

[Effect of electroacupuncture at "Zusanli" (ST 36) and "Yanglingquan" (GB 34) on perinatal nicotine-exposure-induced lung function and morphology of neonatal rats].

OBJECTIVE: To compare the effects of electroacupuncture (EA) at "Zusanli" (ST 36) versus "Yanglingquan" (GB 34) in the pregnant rats on perinatal nicotine-exposure-induced lung function and morphology of newborn rats and explore the rule of acupoint effect in EA for the prevention from lung dysplasia in newborn rats. METHODS: A total of 24 female SD rats were randomized into a normal saline group (S group), a nicotine group (N group), a nicotine-ST 36 group (N + ST 36 group) and a nicotine-GB 34 group (N+GB 34 group), 6 rats in each one. Starting at the 6th day of pregnancy, 0.9% sodium chloride solution was injected subcutaneously in the S group, 1 mg/kg; and in the rest 3 groups, nicotine of the same dose was injected through to the 21st postnatal day to establish the perinatal nicotine-exposure model. Simultaneously, during model preparation, EA was applied at "Zusanli" (ST 36) and "Yanglingquan" (GB 34) in the N+ST 36 group and the N+GB 34 group respectively, once a day, through to the 21st postnatal day. The lung function analytic system for small animal was adopted to observe the changes in lung function indicators in newborn rats, such as peak inspiratory flow (PIF), peak expiratory flow (PEF), expiratory resistance (RE), inspiratory resistance (RI) and dynamic compliance (Cdyn). HE staining was used to observe the morphological changes of lung, such as alveolar fusion and rupture. RESULTS: Compared with the S group, PEF and Cdyn were lower and PIF, RI and RE higher in the N group (all P<0.01), additionally, alveoli were fused and ruptured, alveolar wall thickened, the numbers of alveoli reduced, the interspace of alveoli enlarged and the diameter increased (P<0.01). Compared with the N group, in the N+ST 36 group, PEF and Cdyn were increased, PIF, RI and RE reduced (P<0.05, P<0.01), the alveolar fusion and rupture relieved, the numbers of alveoli increased, alveolar wall thinner, the interpsace of alveoli became normal and the diameter was reduced significantly (P<0.01). In the N+GB 34 group, the changes of lung function and morphological indicators were not significant (P>0.05). CONCLUSION: Electroacupuncture at "Zusanli" (ST 36) in the pregnant rats significantly improves the perinatal nicotine-exposure-induced lung function and morphology of newborn rats than electroacupuncture at "Yanglingquan" (GB 34).

[Electroacupuncture at "Zusanli" (ST36) and "Chize" (LU5) of mother rats exposed to nicotine during pregnancy and lactation has a protective effect on development of lung function and morphology in neonatal rats].

OBJECTIVE: To compare the different effect of electroacupuncture (EA) at "Zusanli" (ST36) and "Chize" (LU5) of mother rats exposed to Nicotine during pregnancy and lactation on lung function and morphological changes in offspring rats, so as to explore the most effective acupoint for improving the development of lung in neonatal rats. METHODS: A total of 24 female pregnancy SD rats were randomly divided into 4 groups: normal control, model, EA-ST36 and EA-LU5 (n＝6 rats in each group). Rats of the normal group were treated by subcutaneous injection of normal saline, and those of the other 3 groups treated by subcutaneous injection of nicotine (1 mg•kg－1•d－1) beginning from the 6th day to about the 21st day of pregnancy (childbirth day) for nicotine exposure during pregnancy and lactation. The daily EA treatment (2 Hz /15 Hz，1 mA) was applied to bilateral ST36 and LU5 for 20 min, beginning from the 6th day of pregnancy to the 21st day (childbirth day). The lung function of the offspring rats including the peak inspiratory flow (PIF), peak expiratory flow (PEF), lung resistance (RL), exhalation resistance (RE)and lung dynamic compliance (Cdyn) was detected by using a lung function analysis system. Histopathological changes (severity of alveolarization) of the offspring rats' lung tissue were observed under microscope after H．E. stain. RESULTS: Compared with the normal group, the PIF, RL and RE values were significantly increased (P<0.01), and PEF and Cdyn values significantly decreased in the model group (P<0.01). The alveolar diameter in the model group was evidently increased relevant to the normal group (P<0.01). Following the intervention, modeling induced increase of PIF, RL, RE and alveolar diameter and decrease of PEF and Cdyn values in the EA-ST36 group, and the increased PIF, RL and RE levels in the EA-LU5 group were obviously suppressed relevant to the model group (P<0.01, P<0.05). Additionally, modeling induced obvious congestion and edema of the alveolar wall, alveolar deformation, rupture and fusion, and reduction of the number of the pulmonary alveoli were evidently milder in both EA-ST36 and EA-LU5 groups. No significant differences were found between the EA-ST36 and EA-LU5 groups in the abovementioned 5 indexes of pulmonary function and alveolar diameter (P>0.05)．. CONCLUSION: EA of ST36 and LU5 of mother rats experiencing nicotine exposure during pregnancy and lactation can improve the lung function and morphological changes in neonatal rats, and the effect of ST36 is relatively better.

[Effect of Electroacupuncture at "Neiguan" (PC 6) on Skin Microcirculation Blood Perfusion Volume of Heart-related Acupoints and Heart-irrelevant Acupoints in Myocardial Ischemia Rats].

OBJECTIVE: To observe the effect of low-frequency or high-frequency electroacupuncture (EA) stimulation of "Neiguan" (PC 6) on changes of skin blood perfusion volume of heart-related and heart-irrelevant acupoints in rats with normal or ischemic myocardium. METHODS: Wistar rats were randomly divided into the control, sham-operation, model, low-frequency EA and high-frequency EA groups (n=8 in each group). The myocardial ischemic (MI) model was established by occlusion of the anterior descending branch of the left coronary artery. 2 Hz and 100 Hz EA was respectively applied to left PC 6 for 20 min, once daily, a total of three times. Electrocardiogram (ECG) was recorded after the last treatment. Serum cardiac troponin T (cTnT) contents were assayed by ELISA. The skin blood perfusion volumes of bilateral PC 6, "Zusanli" (ST 36) and "Yanglingquan" (GB 34) were observed by laser speckle contrast imaging. RESULTS: In comparison with the control and sham-operation groups, the differences of "J point" and contents of serum cTnT were significantly increased in the model group (P<0.01). After EA, the differences of "J point" and contents of serum cTnT were significantly decreased in both low-frequency and high-frequency EA groups (P<0.01, P<0.05). Compared with the control group, the skin blood perfusion volumes of bilateral PC 6 and ST 36 decreased obviously in rats of the model group (P<0.01). After EA, the skin blood perfusion volumes were markedly up-regulated in the areas of PC 6 and ST 36 (P<0.01). There were no significant changes in that of GB 34 among the 5 groups (P<0.05). CONCLUSIONS: Skin blood perfusion volumes around PC 6 and ST 36 can specifically reflect the change of the myocardial state.

[Effects of nitrogen additions on soil hydrolase and oxidase activities in Pinus elliottii plantations.] / æ°®æ·»åŠ å¯¹æ¹¿åœ°æ¾æž—åœŸå£¤æ°´è§£é ¶å’Œæ°§åŒ–é ¶æ´»æ€§çš„å½±å“.

We evaluated responses of hydrolase and oxidase activities in a subtropical Pinus elliottii plantation through a nitrogen (N) addition field experiment (dosage level: 0, 40, 120 kg N·hm-2·a-1). The results showed that N additions significantly decreased the carbon, nitrogen and phosphorus related hydrolase and oxidase activities. The activities of ß-1,4-glucosidase (BG), cellobiohydrolase (CBH), ß-1,4-N-acetylglucosaminidase (NAG) and peroxidase (PER) activities were decreased by 16.5%-51.1% due to N additions, and the decrease was more remarkable in the higher N addition treatment. The activities of α-1,4-glucosidase (aG), ß-1,4-xylosidase (BX), acid phosphatase (AP) and phenol oxidase (PPO) were decreased by 14.5%-38.6% by N additions, however, there was no significant difference among the different N addition treatments. Soil enzyme activities varied obviously in different seasons. The activities of BG, NAG, BX, CBH, AP and PPO were in the order of March > June > October, and aG and PER activities were in the order of October > March > June. Most of the soil hydrolase and oxidase activities were positively correlated with soil pH, but negatively with NO3--N content. It indicated that N additions inhibited soil hydrolase and oxidase activities by reducing soil pH and increasing soil nitrification. N additions inhibited the soil organic matter mineralization and turnover in the subtropical area, and the effects were obvious with the increasing dosage of N additions.

[Effects of different fertilizer species on carbon and nitrogen leaching in a reddish paddy soil].

Enhanced fertilization could decrease nitrogen utilization rate and increase carbon and nitrogen leaching, leading to water pollution in agricultural ecosystem. A long-term field experiment had been established on a reddish paddy soil of Qianyanzhou Ecological Experimental Station (114 degrees 53'E, 26 degrees 48'N) in Jiangxi Province in 1998. Soil solution samples were collected by clay tube and vacuum pump. Four fertilizer species treatments were selected: control with no fertilizer (CK), straw return (ST), nitrogen, phosphorus and potassium mineral fertilizers (NPK) and pig manure (OM), aiming to evaluate the effects of different species of fertilizer on carbon and nitrogen leaching in a double rice cropping system. The results showed that: (1) ammonium nitrogen (NH4(+) -N) was the major type of N in soil leachate in reddish paddy soil. The application of NPK could significantly increase the ammonium nitrogen concentration (1.2 mg x L(-1) +/- 0.1 mg x L(-1)) compared with the CK, ST and OM treatments, and the application of OM could significantly increase the dissolved organic carbon (DOC) concentration (27.3 mg x L(-1) +/- 1.6 mg x L(-1)) in soil leachate. The carbon and nitrogen leaching were more notable in the vegetative growth stage than the reproductive growth stage of rice (P < 0.05); (2) the long-term application of NPK and OM increased the NH4(+) -N, DOC, soil organic carbon (SOC) and total nitrogen (TN) contents. The NPK was best beneficial to improve TN contents and OM to improve SOC contents. (3) The DOC contents in soil leachate and SOC in paddy soil had a positive correlation (P < 0.01), while NH4(+) -N contents in soil leachate and TN contents in paddy soil had a positive correlation (P < 0.01).

[Effects of applying different kind fertilizers on enzyme activities related to carbon, nitrogen, and phosphorus cycles in reddish paddy soil].

Based on the long-term fixed position experimental data from Qianyanzhou Ecological Experiment Station, Chinese Academy of Sciences in 1998, this paper analyzed the effects of applying different kind fertilizers (straw, ST; pig manure, OM; and chemical fertilizer, NPK) on the nutrients (C, N, and P) status and the activities of related enzymes ( beta-1,4-glucosidase, betaG; beta-1,4-N-acetylglucosaminidase, NAG; L-leucine aminopeptidase, LAP; and acid phosphatase, AP) in reddish paddy soil. With the application of OM, the activities of soil betaG, NAG, and LAP increased significantly, as compared with other treatments, and were 1.4, 2. 6, and 1.9 times higher than the control (CK) , respectively. Applying OM also improved the ratio of soil organic carbon to total nitrogen (C/N), but decreased the soil betaG/(NAG+LAP) ratio, suggesting that pig manure could benefit the degradation of soil cellulose and the accumulation of soil organic carbon. Applying NPK increased the activities of soil betaG, NAG, and LAP, but decreased the AP activity, with a decrement of 34% as compared with CK. Under the application of NPK, the soilbetaG/AP and (NAG+ LAP)/AP ratios increased, but the ratios of soil organic carbon to total phosphorus (C/P) and of soil total nitrogen to total phosphorus (N/P) decreased, indicating that chemical fertilizers could induce the accumulation of soil inorganic phosphorus, and inhibit the microbial functions of degrading polysaccharides and phosphate phospholipids.

[Stoichiometric characteristics of leaf carbon, nitrogen, and phosphorus of 102 dominant species in forest ecosystems along the North-South Transect of East China].

One hundred and twelve sampling sites in the forest ecosystems along the North-South Transect of Eastern China (NSTEC) were selected to study the stoichiometric characteristics and variability of leaf carbon (C), nitrogen (N), and phosphorous (P) of 102 dominant species. The contents of leaf C (Cmass), leaf N (Nmass), and leaf P (Pmass) ranged in 374.1-646.5 mg x g(-1), 8.4-30.5 mg x g(-1), and 0.6-6.2 mg x g(-1), with the arithmetic mean (AM) being 480.1, 18.3 and 2.0 mg x g(-1), and the variation coefficient (CV) being 11.1%, 27.5%, and 56.4%, respectively. The leaf C/N, C/P and N/P ranged from 14.1 to 64.1, from 70.9 to 838.6, and from 1.5 to 21.2, with the AM being 29.1, 313.9 and 11.5, and the CV being 32.8%, 48.3% and 44.1%, respectively. The mass ratio of C:N:P was 313.9:11.5:1, and the atom ratio was 810.9:25.4:1. As compared with those at global scale, the tree leaf Cmass and C/N in the study area were significantly higher, Nmass and N/P were significantly lower, while Pmass and C/P had less differences.

[Differential gene expressions in kidney Yang deficiency in individuals with sub-health status].

OBJECTIVE: To study the gene expression profiles in kidney Yang deficiency in individuals with sub-health status. METHODS: The subjects identified to have Kidney-yang deficiency and sub-health status were enrolled in this study with healthy subjects as the normal control. Using gene chip technique and MAS software, the gene expression profiles in kidney Yang deficiency in the subjects with sub-health status were analyzed. RESULTS: Characteristic profiles of the differentially expressed genes were found between the kidney Yang deficiency group and normal control group. Among the total of 75 differentially expressed genes, 22 were up-regulated (with a ratio greater than 2) and 53 were down-regulated (with a ratio less than 0.5) in kidney Yang deficiency group. CONCLUSION: Gene chip technique allows rapid and high-throughput screening for gene expression in kidney Yang deficiency and sub-health status, and a initial evidence of kidney Yang deficiency-related genes has been obtained.