[Efficacy of high-dose dual therapy for Helicobacter pylori infection eradication in servicemen: a randomized controlled trial].

Objective: To assess the efficacy and cost-effectiveness of high-dose dual therapy compared with bismuth-containing quadruple therapy for treating Helicobacter pylori(H.pylori) infection in servicemen patients. Methods: A total of 160 H. pylori-infected, treatment-naive servicemen, including 74 men and 86 women, aged from 20 years to 74 years, with a mean (SD) age of 43 (13) years, tested in the First Center of Chinese PLA General Hospital from March 2022 to May 2022 were enrolled in this open-label, randomized controlled clinical trial. Patients were randomly allocated into 2 groups: the 14-day high-dose dual therapy group and the bismuth-containing quadruple therapy group. Eradication rates, adverse events, patient compliance, and drug costs were compared between the two groups. The t-test was used for continuous variables, and the Chi-square test for categorical variables. Results: No significant difference in H. pylori eradication rates were found between high-dose dual therapy and bismuth-containing quadruple therapy by ITT, mITT and PP analysis[ITT:90.0% (95%CI 81.2%-95.6%) vs. 87.5% (95%CI 78.2%-93.8%), χ2=0.25, P=0.617;mITT:93.5% (95%CI 85.5%-97.9%) vs. 93.3% (95%CI 85.1%-97.8%), χ2<0.01, P=1.000; PP: 93.5% (95%CI 85.5%-97.9%) vs. 94.5% (95%CI 86.6%-98.5%), χ2<0.01, P=1.000 ]. The dual therapy group exhibited significantly less overall side effects compared with the quadruple therapy group [21.8% (17/78) vs. 38.5% (30/78), χ2=5.15,P=0.023]. There were no significant differences in the compliance rates between the two groups [98.7%(77/78) vs. 94.9%(74/78), χ2=0.83,P=0.363]. The cost of medications in the dual therapy was 32.0% lower compared with that in the quadruple therapy (472.10 RMB vs. 693.94 RMB). Conclusions: The dual regimen has a favorable effect on the eradication of H. pylori infection in servicemen patients. Based on the ITT analysis, the eradication rate of the dual regimen is grade B (90%, good). Additionally, it exhibited a lower incidence of adverse events, better compliance and significantly reduced cost. The dual regimen is expected to be a new choice for the first-line treatment of H. pylori infection in servicemen but needs further evaluation.

[Meta analysis of rock salt aerosol therapy for respiratory tract diseases].

Objective: To systematically evaluate the efficacy and safety of rock salt aerosol in the treatment of respiratory tract diseases. Methods: In June 2021, the clinical randomized controlled trial literatures of rock salt aerosol therapy for respiratory tract diseases were searched from CNKI, Wanfang, VIP, Cochrane Library, PubMed database and EMBASE database. Cochrane risk bias evaluation tool was used to evaluate risk bias, Revman 5.4 and Stata16 were used to conduct meta-analysis, TSA 0.9 was used to conduct sequential analysis of trials, and gradepro was used to evaluate evidence quality. Results: A total of 21 literatures were included. According to whether the subjects received rock salt aerosol therapy, they were divided into the experimental group (1125 people) and the control group (973 people) . Compared with the control group, the total clinical effective rate (RR=1.22, 95%CI: 1.15~1.29, P<0.001) , forced expiratory volume in one second (FEV(1)) (WMD=0.20, 95%CI: 0.09~0.31, P<0.001) , percentage of FEV(1) in the predicted value (FEV(1)%) (WMD=5.06, 95%CI: 3.47~6.65, P<0.001) , forced vital capacity (FVC) (WMD=0.22, 95% CI: 0.16~0.27, P<0.001) , maximum expiratory flow (PEF) (WMD=21.312, 95%CI: 9.189~33.435, P=0.004) of experimental group were higher. TSA test shows that the difference conclusions of total effective rate, FEV(1), FEV(1)%, FVC and PEF were reliable, but the conclusion of FEV(1)% needs to be treated with caution; Three literatures reported the adverse reactions in the experimental group; GRADE evidence quality evaluation showed 3 very low-quality evidences and 2 low-quality evidences. Conclusion: Rock salt aerosol therapy combined with conventional therapy has a certain effect on the treatment of respiratory tract diseases, which needs to be further confirmed by high-quality evidence.

[Efficacy and safety of Kangbingdu granules in the treatment of influenza: a randomized, double-blind, double-dummy, positive-drug parallel control multicenter clinical trial].

Objective: To observe the efficacy and safety of Kangbingdu granules (KBD) in the treatment of influenza. Methods: A multicenter, randomized, double-blind, double-dummy, and positive-drug parallel control trial was conducted in 27 Grade ⅢA hospitals in China and the subjects were randomly assigned to the KBD test group or the oseltamivir phosphate capsule control group at a ratio of 1∶1. 200 subjects were planned to be enrolled in each group. The experimental group was given KBD (18g each time, 3 times a day) and oseltamivir phosphate simulator orally, while the control group was given oseltamivir phosphate capsule (75 mg each time, twice a day) and KBD simulator orally for 5 days. The primary efficacy indicators included the remission time of major clinical symptoms and the time of complete defervescence. The secondary efficacy indicators included dosage of acetaminophen, the change of traditional Chinese medicine (TCM) syndrome score and the remission time of other important clinical symptoms. The efficacy of KBD in the test group and Oseltamivir phosphate control group were compared. Adverse events or adverse reactions were observed at the same time to evaluate the safety of KBD Granules. Results: A total of 393 subjects from 27 Grade ⅢA hospitals in China were enrolled. The experimental group included 195 subjects and 191 subjects (97.95%) completed the trial, While the control group included 198 subjects and 195 subjects (98.48%) completed the trial. There was no significant difference in the shedding rate and rejection rate between the two groups (P>0.05). In the Full Analysis Set (FAS), the mean age of the experimental group was (34.9±14.4) years old, with 83 males (42.78%). The mean age of the control group was (33.3±13.5) years old, with 78 males (39.59%). There were no statistically significant differences between the two groups in demographic data, physical examination, viral pathogen detection, total score of TCM syndromes and scores of each symptom at baseline (P>0.05). In the FAS, the remission time M (Q1, Q3) of major clinical symptoms was 3.0 (3.0, 4.0) days in the experimental group and 3.0 (3.0, 4.0) days in the control group, and the difference was not statistically significant (P>0.05). The time M (Q1, Q3) of complete defervescence was 34.0 (20.3, 49.0) hours in the experimental group and 36.5 (19.6, 48.8) hours in the control group, and the difference was not statistically significant (P>0.05). KBD granules had the same effect as Oseltamivir phosphate capsule (P>0.05) in terms of acetaminophen dosage, TCM syndrome effect and disappearance rate of most important clinical symptoms. Meanwhile, the disappearance rate of dizziness and chest distress on day 3 in the KBD granules group was better than that of oseltamivir phosphate capsule (P<0.05). Conclusion: KBD granules have the same efficacy as Oseltamivir Phosphate capsule in the treatment of influenza and the drug safety is good.

Protective effects of dietary fish-oil supplementation on skin inflammatory and oxidative stress biomarkers induced by fine particulate air pollution: a pilot randomized, double-blind, placebo-controlled trial.

BACKGROUND: Exposure to fine particulate matter (with an aerodynamic diameter ≤ 2·5 µm, PM2·5 ) air pollution has been associated with skin-related diseases or disorders. OBJECTIVES: To evaluate the potential skin-protective effects of fish-oil supplementation against PM2·5 exposure. MATERIALS AND METHODS: This is an exploratory analysis based on a pilot randomized, double-blind, placebo-controlled trial among 65 healthy young adults between September 2017 and January 2018 in Shanghai, China. We randomly assigned participants to take either fish oil or placebo 2·5 g daily for four consecutive months. Four rounds of skin D-Squame® tape samples were collected in the last 2 months, and five secondary biomarkers of skin inflammation and oxidative stress were measured. Fixed-site PM2·5 concentrations on campus were measured in real time. We used linear mixed-effect models to analyse the associations between short-term PM2·5 exposure and biomarkers in each group. RESULTS: The 24-h average PM2·5 concentration was 34·68 ± 15·83 µg m-3 . There were generally weaker associations between PM2·5 and biomarkers in the fish-oil group than in the placebo group, but the associations and the between-group differences varied by biomarkers and lag periods. Compared with the placebo group, for a 10-µg m-3 increase in PM2·5 concentration, the increments of interleukin-1α and carbonyl protein in the fish-oil group were 41·55% smaller [95% confidence interval (CI) 4·61-78·48%] at lag 0-48 h and 22·01% smaller (95% CI 11·25-32·77%) at lag 0-24 h, respectively. No significant between-group differences were observed for other biomarkers. CONCLUSIONS: This study suggested that dietary fish-oil supplementation may improve biomarkers of skin inflammation and oxidative-stress response to short-term PM2·5 exposure.

Mobilization of recalcitrant phosphorous and enhancement of pepper P uptake and yield by a new biocontrol and bioremediation bacterium Burkholderia cepacia CQ18.

AIMS: Phosphorus (P) is a finite resource and inoculation of phosphorus-mobilizing bacteria (PMB) is a promising approach for the enhancement of soil P availability and plant P uptake. This drives scientists to search for the microbes effective in mobilizing legacy P in soils. METHODS AND RESULTS: The current incubation and greenhouse pot experiments were conducted to investigate P mobilization and pepper P uptake as affected by a new biocontrol and bioremediation bacterium Burkholderia cepacia CQ18. This bacterium converted Ca3 (PO4 )2 , FePO4 , AlPO4 , and lecithin into soluble inorganic P in the culture solutions and increased available P (including water-soluble P and Olsen P) in the soil. There were positive correlations between the soluble inorganic phosphorus and the exudates (protons, organic acids (oxalate and gluconate), siderophores and phosphatases) in culture solutions. Pepper plant biomass, fruit yield and P uptake changed in the sequence: chemical fertilizers plus bacterial inoculant >only chemical fertilizers >only bacterial inoculant >blank control. CONCLUSIONS: Taking into account the wide spectrums of P mobilization and simultaneous production of acid, neutral and alkaline phosphatases at a given pH, B.cepacia CQ18 may be a potential PMB used in soils with wide pH ranges. The mechanisms employed by this bacterium in the solubilization of recalcitrant inorganic P could be the efflux of protons, organic acids (oxalate and gluconate) and siderophores. Phosphatases could be of utmost importance in the mineralization of the organic P. The production of siderophores and phosphatases by of B.cepacia CQ18 could thus be crucial for not only the antagonism against plant pathogens but also the mobilization of soil sparingly available P. SIGNIFICANCE AND IMPACT OF THE STUDY: Burkholderia cepacia CQ18 could be potentially developed into a biofertilizer.

[Study on protective mechanism of Tibetan medicine Ershiwuwei Songshi Pills on cholestatic liver injury in rats based on FXR signaling pathway].

This paper aimed to investigate the protective effect and mechanism of the Tibetan medicine Ershiwuwei Songshi Pills on α-naphthalene isothiocyanate(ANIT)-induced cholestatic liver injury in rats based on the farnesol X receptor(FXR) signaling pathway. SD rats were randomly divided into blank group, model group, ursodeoxycholic acid(UDCA) group, Tibetan medicine Ershiwuwei Songshi Pills low, medium and high dose groups(0.09, 0.18, 0.36 g·kg~(-1)). A prophylactic dosing regimen was used in the experiment. From the 1 st to 4 th days, the UDCA group and the Tibetan medicine Ershiwuwei Songshi Pills suspension groups received prophylactic gavage administration; on the 5 th day, the blank control group was given an equal volume of olive oil blank reagent, and the remaining groups were given ANIT modeling reagent. Administration was continued on day 5 to 6 in each administration group. Forty-eight hours after modeling on the 7 th day, blood was collected from the femoral artery of rats. Serum alkaline phosphatase(ALP), alanine aminotransferase(ALT), aspartate aminotransferase(AST), direct bilirubin(DBIL), total bilirubin(TBIL), and total bile acid(TBA) levels were detected, and liver histopathological changes were observed. The relative expression changes of FXR, SHP, CYP7 A1, MRP2, MRP3, NTCP, BSEP mRNA in liver tissues were detected by Real-time fluorescence quantitative method, and the expression changes of FXR, SHP, UGT2 B4 protein in liver tissues were detected by Western blot. The results showed that the Tibetan medicine Ershiwuwei Songshi Pills significantly reduced the levels of ALT, ALP, DBIL, TBIL and TBA in the serum of the ANIT mo-del rats(P<0.01, P<0.05), significantly up-regulated the mRNA expressions of SHP and NTCP(P<0.01, P<0.05), significantly down-regulated the mRNA expression of CYP7 A1 and MRP3(P<0.01, P<0.05); and significantly up-regulated the protein expressions of FXR and SHP(P<0.01, P<0.05). The Tibetan medicine Ershiwuwei Songshi Pills have an obvious protective effect on ANIT-induced cholestatic liver injury in rats, and its mechanism may be related to the bile acid metabolism mediated by the FXR signaling pathway.

Phytoremediation of heavy metals under an oil crop rotation and treatment of biochar from contaminated biomass for safe use.

The disposal of contaminated plants limits the use of phytoremediation. Therefore, the disposal of contaminated sunflower was investigated after determining the phytoremediation of heavy metals under an oil crop rotation of sunflower (Helianthus annuus L)-sesame (Sesamum indicum L.). In the field experiment, the extraction efficiency of sunflower-sesame rotation was 0.07% for lead (Pb); 1.37% for zinc (Zn); 1.10% for copper (Cu); and 6.12% for cadmium (Cd). Contaminated sunflower stems were pyrolyzed at different temperature. The biochar produced at 300 °C was extracted in a two-step process (acid-extraction from biochar and metals precipitation in alkaline condition). At pH = 1, 65.67% of the Cd and much potassium (K) were extracted. After acid-extraction, adjust the pH of filtrate to 10, metals were precipitated and then separated from the K-enriched solution. Therefore, pyrolysis can process contaminated residues, and the biochar extracts can be reutilized as fertilizer to off-site crop production. Thus, an oil crop-rotation system, in addition to creating economic benefits, can be used by local farmers in contaminated soils.

Local dermal application of a compound lidocaine cream in pain management of cancer wounds.

The aim of this study was to explore the analgesic effect of local application of compound lidocaine/prilocaine cream on cancer wounds during wound care in order to reduce the amount of morphine intake or completely replace the systemic morphine administration and optimize the protocol for cancer wound pain management. All patients were enrolled with a visual analog scale (VAS) pain score ≥4. Before wound care, 60 patients were randomly divided into 2 groups of 30 each: morphine group (10 mg tablet); topical 5% compound lidocaine cream group (0.2 g/cm2). VAS scores, heart rate, and Kolcaba comfort level were recorded for the two groups 10 min before and 10, 15, 20, and 25 min after wound care and data were analyzed statistically. The means for the pain score and heart rate of the topical lidocaine/prilocaine cream group were lower than those of the morphine group (P<0.01) and the Kolcaba comfort level was higher (P<0.01). Local dermal application of the compound lidocaine cream can be used as an alternative to the systemic morphine administration in cancer wound care for its safety and effectiveness. In addition, it can improve the patients' comfort and quality of life.

[Analysis of mental state of allergic rhinitis patients in Chengdu city by symptom check list 90 (SCL-90) scale].

Objective: To analyse the mental state of patients with allergic rhinitis (AR) in Chengdu. Methods: One thousand five hundred and thirty-six AR patients from Sichuan Provincial Integrated Traditional Chinese and Western Medicine Hospital, West China Hospital of Sichuan University, Affiliated Hospital of Chengdu University of Traditional Chinese Medicine, Sichuan People's Hospital, Sichuan Second Hospital of Traditional Chinese Medicine were selected from July 2013 to January 2018. Eight hundred and twenty-seven patients were screened into study group by inclusion and exclusion standards. The symptom check list 90 (SCL-90) was used to group and score the mental state of these patients according to nine classification criteria: gender, BMI, age, marital status, monthly salary, disease duration, living environment, education level and working environment. Then, the scores were compared within groups. Inter-group comparison was made between the study group and the Chinese norm, and the positive factors for psychological disorders were extracted. Four symptoms in the study group, i.e. nasal itching, sneezing, clear discharge and nasal congestion, were scored on the visual analogue scale (VAS). SPSS 19.0 software was used to carry out statistical analysis. Partial correlation analysis was performed between the positive factors and the symptom scores by multiple regression statistical method. Results: The total score of SCL-90 in the study group was 2.64±0.25, which was accorded with mild to moderate mental health impairment. There were 124 (15.0%) without mental health damage, 176 (21.3%) with mild damage, 474 (57.3%) with mild to moderate damage, 41 (5.0%) with moderate to severe damage and 12 (1.4%) with severe damage. The in-group comparison showed that the top three categories of different items were the living environment, gender and working environment. The scores of somatization, obsessive-compulsive symptoms, interpersonal sensitivity, depression, anxiety, psychosis, other (sleep, diet) and total average score of urban residents were higher than that of country residents (3.29±0.61 vs 2.65±0.50, 2.81±0.77 vs 2.05±0.38, 3.10±0.19 vs 2.49±0.67, 3.40±0.84 vs 2.49±0.70, 3.04±0.64 vs 2.33±0.51, 3.02±0.55 vs 2.40±0.77, 3.40±0.41 vs 2.52±0.77, 2.91±0.11 vs 2.29±0.40, Z value was 4.88, 5.25, 4.57, 5.91, 5.09, 4.63, 5.55, -4.55, respectively, all P<0.05). Women scored higher than man for somatization, interpersonal sensitivity, depression and others (2.66±0.51 vs 2.00±0.45, 3.37±0.47 vs 2.63±0.51, 3.44±0.57 vs 2.85±0.52, 3.47±0.36 vs 2.76±0.45, Z value was -5.10, -5.51, -4.86, -5.28, respectively, all P<0.05). The scores of somatization, interpersonal sensitivity, psychosis and other (sleep, diet) were higher in the indoor group than those in the outdoor group (3.49±0.64 vs 2.78±0.46, 3.33±0.30 vs 2.56±0.68, 3.28±0.60 vs 2.67±0.31, 3.50±0.85 vs 2.85±0.37, Z value was 5.31, 5.79, 4.89, 5.00, respectively, all P<0.05). The outdoor group scored higher on obsessive-compulsive symptoms, anxiety and hostility (3.44±0.40 vs 2.83±0.35, 3.40±0.50 vs 2.57±0.93, 3.34±0.88 vs 2.69±0.56, Z value was 4.96, 6.22, 5.08, respectively, all P<0.05). The inter-group comparison found that depression, anxiety, psychosis and other (sleep, diet) could be partially correlated with VAS scores as 4 positive factors. The results of partial correlation analysis showed that depression was positively correlated with sneezing and nasal runny discharge, anxiety was positively correlated with nasal itching and nasal obstruction, psychosis was positively correlated with nasal itching and sneezing, and other (sleep, diet) was positively correlated with nasal runny discharge and nasal obstruction. Conclusion: AR patients have mild to moderate mental health impairments, which are correlated with AR symptoms.

Local dermal application of a compound lidocaine cream in pain management of cancer wounds

The aim of this study was to explore the analgesic effect of local application of compound lidocaine/prilocaine cream on cancer wounds during wound care in order to reduce the amount of morphine intake or completely replace the systemic morphine administration and optimize the protocol for cancer wound pain management. All patients were enrolled with a visual analog scale (VAS) pain score ≥4. Before wound care, 60 patients were randomly divided into 2 groups of 30 each: morphine group (10 mg tablet); topical 5% compound lidocaine cream group (0.2 g/cm2). VAS scores, heart rate, and Kolcaba comfort level were recorded for the two groups 10 min before and 10, 15, 20, and 25 min after wound care and data were analyzed statistically. The means for the pain score and heart rate of the topical lidocaine/prilocaine cream group were lower than those of the morphine group (P<0.01) and the Kolcaba comfort level was higher (P<0.01). Local dermal application of the compound lidocaine cream can be used as an alternative to the systemic morphine administration in cancer wound care for its safety and effectiveness. In addition, it can improve the patients' comfort and quality of life.

Genetic diversity and population structure of Eucommia ulmoides Oliver, an endangered medicinal plant in China.

Eucommia ulmoides Oliver, one of the tertiary relict species found only in China, is the only extant species of Eucommiaceae. Using inter-simple sequence repeat (ISSR) and sequence-related amplified polymorphism (SRAP) markers, we studied the genetic diversity and population genetic structure of 187 accessions from 17 E. ulmoides populations throughout its main distribution in China. A total of 65 bands were amplified using eight ISSR primers, of which 50 bands (76.9%) were polymorphic. Meanwhile, another 244 bands were observed using eight SRAP primer combinations and 163 (66.8%) of these were polymorphic. The analysis of molecular variation (AMOVA) indicated that 88.8 and 92.4% of the total variation resided within populations based on ISSR and SRAP analysis, respectively. Moreover, we found that the E. ulmoides populations were clustered into six distinct groups using ISSR and SRAP markers via the unweighted pair-group method (UPGMA). Furthermore, STRUCTURE analysis showed that these 17 populations could be classified into four groups using ISSR markers, but only two groups using SRAP markers. No significant relevancy was observed between genetic and geographic distances among the sampled populations. The results of this study support the view that exchange of seeds among local farmers plays an important role in shaping the present genetic distribution pattern. "Core collection" is suggested for genetic diversity conservation of E. ulmoides in China.

Disruption of cellulose synthesis by 2,6-dichlorobenzonitrile affects the structure of the cytoskeleton and cell wall construction in Arabidopsis.

Cellulose is the major component of plant cell walls and is an important source of industrial raw material. Although cellulose biosynthesis is one of the most important biochemical processes in plant biology, the regulatory mechanisms of cellulose synthesis are still unclear. Here, we report that 2,6-dichlorobenzonitrile (DCB), an inhibitor of cellulose synthesis, inhibits Arabidopsis root development in a dose- and time-dependent manner. When treated with DCB, the plant cell wall showed altered cellulose distribution and intensity, as shown by calcofluor white and S4B staining. Moreover, pectin deposition was reduced in the presence of DCB when immunostained with the monoclonal antibody JIM5, which was raised against pectin epitopes. This result was confirmed using Fourier transform infrared (FTIR) analysis. Confocal microscopy revealed that the organisation of the microtubule cytoskeleton was significantly disrupted in the presence of low concentrations of DCB, whereas the actin cytoskeleton only showed changes with the application of high DCB concentrations. In addition, the subcellular dynamics of Golgi bodies labelled with N-ST-YFP and TGN labelled with VHA-a1-GFP were both partially blocked by DCB. Transmission electron microscopy indicated that the cell wall structure was affected by DCB, as were the Golgi bodies. Scanning electron microscopy showed changes in the organisation of cellulose microfibrils. These results suggest that the inhibition of cellulose synthesis by DCB not only induced changes in the chemical composition of the root cell wall and cytoskeleton structure, but also changed the distribution of cellulose microfibrils, implying that cellulose plays an important role in root development in Arabidopsis.

Wnt5a promotes differentiation of human dental papilla cells.

AIM: To investigate the role of Wnt5a in the process of differentiation of human dental papilla cells (HDPCs). METHODOLOGY: Recombinant adenovirus encoding full-length Wnt5a cDNA was constructed to investigate the biological role of Wnt5a on the differentiation of HDPCs. The effect of Wnt5a on HDPCs differentiation was determined by ALP activity assay, ALP staining and mineral induction assay. Mineralization-related gene expressions were assessed by RT-PCR. RESULTS: Immunostaining revealed Wnt5a expression in the odontoblast layer and dental papilla tissue. Over-expression of Wnt5a by transfecting HDPCs with an Wnt5a-carrying construct increased ALPase activity and the formation of mineralized nodules of HDPCs. RT-PCR analysis showed that the expressions of mineralization-related genes, such as bone sialoprotein, collagen type I, osteonectin, osteopontin (OCN), dentine matrix protein-1 were up-regulated by Wnt5a. CONCLUSIONS: Wnt5a promoted differentiation of HDPCs.

Nitric oxide in vPAG mediates the depressor response to acupuncture in stress-induced hypertensive rats.

The hypertensive rat model was made by chronic stress of electric foot-shocks and noises. On such hypertensive rats, when anesthetized with urethane and chloralose, the electroacupuncture (EA) to bilateral "Zusanli (st.36)" acupoints for 20 min, could result in a depressor (including both systolic and diastolic pressure) and bradycardiac response as well as an attenuation in the maximum of left ventricular pressure, end diastolic pressure and +/-dp/dt. In power spectrum analysis of heart rate variability aspect, EA could increase all total variance, very low frequency component, low frequency component and the ratio of low frequency component and high frequency component. When EA with microinjection of N(omega) - Nitro- L-Arginine , a blocker of the formation of nitric oxide, into the ventral periaqueductal gray matter (vPAG), the above effects of EA were abolished or reduced significantly. The results suggest that the depressor effect of EA on stress-induced hypertensive rats might be mediated by nitric oxide in the vPAG due to activation of sympathetic inhibitory system and by attenuated cardiac activities.

Gallotannins and related polyphenols from Pistacia weinmannifolia.

Two new gallotannins, pistafolins A (1) and B (2), were isolated from the leaf extract of Pistacia weinmannifolia. Their structures were determined by spectral methods. Four known gallotannins (3-6), seven known flavonoid glycosides (7-13), along with 1-O-beta-D-(6'-O-galloyl)-glucopyranosyl-3-methoxy-5-hydroxybenzen e (14), gallic acid (15), methyl gallate (16), (+)-catechin (17), and (+)-gallocatechin (18), were also isolated. Some of these compounds were tested for their cytotoxicity toward K562 cells, and two small molecular phenolic compounds, 15 and 18, showed significant inhibitory effects with IC50 values less than 5 micrograms/ml.

Constituents of Craspedolobium schochii.

Nine phenolic compounds, including a new one, were isolated from 70% acetone extract of Craspedolobium schochii. The new compound was identified as 3-(3,4-dimethoxy-2-hydroxyphenyl)-7-hydroxy-coumarin (1) on the basis of spectroscopic evidence.

Constituents from Lonicera japonica.

Five caffeoylquinic acids and esters (1-5), including a new compound, 3,5-dicaffeoylquinic acid butyl ester (5), were isolated from the flowers and buds of Lonicera japonica and their structures were determined by NMR spectral analysis.

Biochemical evaluation of photolabile precursors of choline and of carbamylcholine for potential time-resolved crystallographic studies on cholinesterases.

Acetylcholinesterase and butyrylcholinesterase both rapidly hydrolyze the neurotransmitter acetylcholine. The unusual three-dimensional structure of acetylcholinesterase, in which the active site is located at the bottom of a deep and narrow gorge, raises cogent questions concerning traffic of the substrate, acetylcholine, and the products, choline and acetate, to and from the active site. Time-resolved crystallography offers a promising experimental approach to investigate this issue but requires a suitable triggering mechanism to ensure efficient and synchronized initiation of the dynamic process being monitored. Here we characterize the properties of two photolabile triggers which may serve as tools in time-resolved crystallographic studies of the cholinesterases. These compounds are 2-nitrobenzyl derivatives of choline and of carbamylcholine, which generate choline and carbamylcholine, respectively, upon photochemical fragmentation. Both photolabile compounds are reversible inhibitors, which bind at the active sites of acetylcholinesterase and butyrylcholinesterase with inhibition constants in the micromolar range, and both photofragmentation processes occur rapidly and with a high quantum yield, without substantial photochemical damage to the enzymes. Photolysis both of acetylcholinesterase and of butyrylcholinesterase, complexed with a 2-nitrobenzyl derivative of choline, resulted in regeneration of enzymic activity. Photolysis of acetylcholinesterase complexed with the 2-nitrobenzyl derivative of carbamylcholine led to time-dependent inactivation, resulting from carbamylation of acetylcholinesterase, which could be reversed upon dilution, due to decarbamylation. Both sets of experiments demonstrated release of choline within the active site. In the former case, choline was produced photochemically at the active site. In the latter case, choline was generated enzymatically, within the active site, concomitantly with carbamylation of the acetylcholinesterase. The two photolabile compounds may thus serve as complementary probes for time-resolved studies of the route of product release from the active sites of the cholinesterases.