A chitosan/alginate coated nano-liposome to improve intestinal absorption of curcumin for oral administration.

Attempts to improve low absorption and rapid metabolic conversion of curcumin were made by developing curcumin-loaded bilayer nanoliposomes coated with chitosan and alginate for intestinal-specific drug delivery. A curcumin-loaded nano-liposome was prepared with optimized formulations with phosphatidylcholine, curcumin, chitosan, and alginate. The particle size of the optimized formulation was approximately 400 nm, and the encapsulation efficiency was more than 99%. In the in vitro release study, curcumin release from the curcumin-loaded nanoliposome with double layers of chitosan/alginate (CNL-CH/AL) was suppressed in the simulated gastric fluid (SGF, pH 1.2) and enhanced in the simulated intestinal fluid (SIF, pH 6.8). In the in vivo pharmacokinetic study in rats, the CNL-CH/AL-treated group showed a prolonged absorption pattern of curcumin and the area under the plasma concentration-time curve from 0 to 24 h (AUC0-24) was improved 109-fold compared to the control group treated with a curcumin solution without a nanocarrier.

The Usefulness of Quantitative Electroencephalography in Diagnosis and Severity Evaluation of Delirium: A Retrospective Study.

OBJECTIVE: Incontrovertible disease markers are absent in delirium. This study investigated the usefulness of quantitative electroencephalography (qEEG) in diagnosing delirium. METHODS: This retrospective case-control study reviewed medical records and qEEG data of 69 age/sex-matched patients (delirium group, n=30; control group, n=39). The first minute of artifact-free EEG data with eyes closed was selected. Nineteen electrodes' sensitivity, specificity, and correlation with delirium rating scale-revised-98 were analyzed. RESULTS: On comparing the means of absolute power by frontal, central, and posterior regions, the delta and theta powers showed significant differences (p<0.001) in all regions, and the magnitude of the absolute power was higher in the delirium group than in the control group; only the posterior region showed a significant (p<0.001) difference in beta power. The spectral power of theta at the frontal region (area under the curve [AUC]=0.84) and theta at the central and posterior regions (AUC=0.83) showed 90% sensitivity and 79% specificity, respectively, in differentiating delirious patients and controls. The beta power of the central region showed a significant negative correlation with delirium severity (R=-0.457, p=0.011). CONCLUSION: Power spectrum analysis of qEEG showed high accuracy in screening delirium among patients. The study suggests qEEG as a potential aid in diagnosing delirium.

Clinical implication and risk factor of pneumonia development in mild coronavirus disease 2019 patients.

BACKGROUND/AIMS: Although a majority of coronavirus disease 2019 (COVID-19) cases were characterized as mild, data assessing the development of pneumonia in mild COVID-19 patients are limited. We aimed to examine the effect of pneumonia development on the clinical course of mild COVID-19 in hospitalized patients. METHODS: A retrospective cohort study was conducted via medical record review between February 25, 2020 and April 11, 2020 at a single center. The impact of pneumonia development on the time to viral clearance in mild COVID-19 patients was evaluated. Risk factors associated with the development of pneumonia were also identified. RESULTS: Chest radiographs revealed the development of pneumonia in 26.8% of mild COVID-19 patients. The time to pneumonia development was a median of 8.0 days from the onset of symptoms and 3.5 days after hospital admission. A multivariate analysis for predicting pneumonia development identified age ≥ 65 years (odds ratio [OR], 3.15; 95% confidence interval [CI], 1.14 to 8.73), cough (OR, 2.18; 95% CI, 1.29 to 3.68), dyspnea (OR, 3.58; 95% CI, 1.10 to 11.69), and diarrhea (OR, 2.69; 95% CI, 1.51 to 4.78) as significant variables. The time to negative conversion was longer in mild COVID-19 patients who developed pneumonia (23.6 days vs. 18.4 days, p = 0.003). In Kaplan-Meier estimation and multivariate Cox regression analyses, newly developed pneumonia was significantly related with delayed time to negative conversion (log-rank test, p = 0.02; hazard ratio, 2.90; 95% CI, 1.06 to 7.97). CONCLUSION: The development of pneumonia delayed viral clearance in patients with mild COVID-19. Elderly patients or those suffering from diarrhea should be closely monitored, given the increased risk of developing pneumonia.

Chest computed tomography scan as an initial diagnostic method for tuberculosis infection detected by mass screening.

BACKGROUND/AIMS: We assessed the diagnostic yield of chest computed tomography (CT) as an initial diagnostic method for patients with a tuberculosis (TB) infection detected by mass screening in a country with an intermediate TB burden. METHODS: A retrospective study was conducted on patients with TB infection detected by mass screening performed between January 2015 and March 2018. The patients were classified according to whether they had a chest X-ray (CXR) or CT scan as an initial diagnostic test to exclude active TB. RESULTS: Of 542 patients with TB infection detected by mass screening, 222 and 320 were initially examined by CXR and CT, respectively; the two modalities showed no significant difference in rate of detection of patients with active TB (0.9% and 2.5%, respectively; p = 0.110). However, chest CT was associated with further invasive tests using bronchoscopy and respiratory specimens, and significantly increased the frequency of hospital visits. CONCLUSION: Chest CT was not supported as an initial diagnostic method to rule out active TB in patients with a TB infection detected by mass screening in a country with an intermediate TB burden.

Interstitial Lung Abnormalities and the Clinical Course in Patients With COPD.

BACKGROUND: The presence and progression of interstitial lung abnormalities (ILAs) is known to be associated with a decline of lung function and increased risk of mortality. RESEARCH QUESTION: We aimed to elucidate the clinical course according to ILAs in patients with COPD. STUDY DESIGN AND METHODS: A retrospective study was conducted between January 2013 and December 2018 of COPD patients who underwent chest CT imaging and longitudinal pulmonary function tests. We evaluated radiologic findings, history of acute exacerbations of COPD, and lung function changes during the longitudinal follow-up. RESULTS: Of 363 patients with COPD, 44 and 103 patients had equivocal and definite ILAs, respectively. Patients with ILAs were significantly older and had lower FEV1 and FVC than patients without ILAs. During the mean follow-up period of 5.2 years, ILAs were associated significantly with the annual incidence of moderate to severe acute exacerbation of COPD (ß ± SD, 0.38 ± 0.12; P = .002) and with the risk of frequent exacerbation (adjusted OR, 2.03; P = .045). Patients with progressive ILAs showed a significantly higher rate of annual decline in FEV1 and FVC than those showing no change in, or improved, ILAs. INTERPRETATION: ILAs were associated significantly with moderate to severe acute exacerbation in patients with COPD, and the progression of ILAs was associated with an accelerated decline in lung function.

Efficacy and safety of HX 110-A and HX 110-B in promoting respiratory health: protocol for an 8-week, randomized, double-blind, parallel group, placebo-controlled trial.

BACKGROUND: HX110-A and HX110-B are compound extracts based on radix adenophorae and rhizoma dioscoreae, respectively, which have anti-inflammatory activity. There are limited data on whether they may help improve respiratory conditions including lung function. Therefore, in this trial, we will evaluate the effectiveness and safety of the use of HX110-A and HX110-B for the treatment of respiratory health in adults with mild respiratory symptoms. METHODS: This will be an 8-week, randomized, double-blind, parallel group, placebo-controlled trial with three arms. Adults more than 40 years old with persistent respiratory symptoms will be enrolled. Patients with definite respiratory disease or with a history of recent intake of antioxidants or anti-inflammatory agents will be excluded. Study subjects will be assigned at a 1:1:1 ratio into the following three arms: controls, experimental group 1 (HX110-A), and experimental group 2 (HX110-B). Control or experimental foods will be administered for 8 weeks, and follow-up will be up to 12 weeks. The primary outcome will be total antioxidant capacity. Secondary outcomes will be inflammatory indexes, respiratory symptoms, lung function, quality of life, and fatigue level. Safety outcomes will be assessed by monitoring adverse events and vital signs, and through clinical pathology tests. RESULTS: This trial will reveal the effectiveness and safety of HX110-A and/or HX110-B for medical purposes in adults with respiratory symptoms. The results should clarify if active intake of specific foods with these functional compounds may promote respiratory health in adults without definite respiratory disease. TRIAL REGISTRATION: Clinical Research Information Service, KCT0003614. Registered 12 May 2019 (Respectively registered, https://cris.nih.go.kr/cris/en/search/search_result_st01.jsp?seq=13364).

A population-based observational study of patients with pulmonary disorders in intensive care unit.

BACKGROUND/AIMS: Only a few epidemiologic studies on the patients with pulmonary disorders admitted to intensive care unit exist. We investigated the characteristics and clinical outcomes of the patients with severe pulmonary disorders. METHODS: The sample cohort database of National Health Insurance Sharing Service from 2006 to 2015 was used. Operational definition of critically ill patients was adults who were either admitted to intensive care unit for at least 3 days or expired within first 2 days in the unit. The pulmonary disorder group comprised of critically ill patients with respiratory disease as the main diagnosis. RESULTS: Among the 997,173 patients, 12,983 (1.3%) in 383 intensive care units were categorized as critically ill. Patients in the pulmonary disorder group tended to have more comorbidities or disabilities. The length of hospital stay and duration of mechanical ventilation were longer in the pulmonary disorder group. Overall mortality and re-admission were higher in the pulmonary disorder group, with adjusted incidence rate ratios of 1.22 (95% confidence interval, 1.18 to 1.27) and 1.26 (95% confidence interval, 1.17 to 1.36), respectively. After adjustment by Cox regression, the pulmonary disorder group was an independent risk factor for in-hospital mortality. CONCLUSION: In critically ill patients with pulmonary disorder, the use of healthcare resources was higher, and their clinical outcomes were significantly worse than the non-pulmonary disorder group.

The clinical impact of drug-induced hepatotoxicity on anti-tuberculosis therapy: a case control study.

BACKGROUND: There are limited data available on whether drug-induced hepatotoxicity (DIH) affects the clinical outcomes of tuberculosis (TB) treatment. We explored the effects of DIH on the clinical course and outcomes of pulmonary TB. METHODS: In this retrospective cohort study, we included patients with culture-proven pulmonary TB treated in a tertiary hospital from 2013 to 2016. DIH was defined as proposed by the official American Thoracic Society statement. We compared the clinical outcomes of DIH and non-DIH patients. RESULTS: Between January 1, 2013 and December 31, 2016, a total of 168 TB patients were included, and 20 (11.9%) were diagnosed with DIH. These patients were significantly older, had a higher Charlson Comorbidity Index score, exhibited more chronic liver disease, included more chronic alcoholics, and had a lower body mass index than non-DIH patients. We found no significant differences between DIH and non-DIH patients in the 2-month sputum culture conversion rate, the time to sputum culture conversion, treatment outcomes, or total treatment duration. However, the ratio of treatment interruption time to total treatment duration and the proportion of hepatotonic users were significantly higher among DIH patients. CONCLUSION: DIH development during TB treatment does not significantly affect the clinical outcomes of pulmonary TB. However, treatment interruption caused by DIH may increase the risks of future relapse and acquired resistance. Further study is needed.

Natural Course of Posttraumatic Symptoms in Late-Adolescent Maritime Disaster Survivors: Results of A 12-Month Follow-Up Study.

OBJECTIVE: This study is a prospective observational study on 75 late-adolescent survivors of a large passenger ship accident from immediately after the accident to one year later. METHODS: Assessments of student survivors were conducted on day 2 and at months 1, 6, and 12. The PTSD Checklist (PCL), Patient Health Questionnaire-9 (PHQ-9), State subscale of the State and Trait Anxiety Inventory (STAI-S), Athens Insomnia Scale (AIS), and Brief Resilience Scale (BRS) were administered. RESULTS: When the assessments for day 2 and month 12 were compared, all the scales, except the PCL-avoidance subscale, showed a significant improvement in symptoms among males. However, among females, all the scales, except the PCL-re-experience subscale and the STAI-S, failed to show a significant improvement. All the symptoms for both males and females showed a pattern that decreased to the lowest level at month 1 (camp-based controlled intervention period), then increased at months 6 and 12 (voluntary individual treatment after returning to school). CONCLUSION: The rapid deterioration of psychological symptoms was found during the chronic phase, when students returned to their daily routines and received voluntary individual therapy. There is a need to screen high-risk adolescents and be more attentive to them during this period.

Characteristics of Residual Symptoms in Korean Patients with Major Depressive Disorder: A Validation Study for the Korean Version of Depression Residual Symptom Scale.

OBJECTIVE: Residual symptoms of depression are related to more severe and chronic course of functional impairment with higher risk of relapse. The objective of this study was to validate, and determine psychometric properties of the Korean version of Depression Residual Symptom Scale (KDRSS). METHODS: A total of 203 outpatients with recent episode of major depression based on DSM-IV criteria were enrolled in this study. They had been treated with antidepressants and assessed by KDRSS, Hamilton Depression Rating Scale-24 (HDRS-24), and Montgomery-Åsberg Depression Rating Scale (MARDS). The validity and reliability of KDRSS were assessed, including internal consistency reliability, concurrent validity, temporal stability, factorial validity, and discriminative validity. RESULTS: Internal consistency (Cronbach's alpha=0.961), concurrent validity (MADRS: r=0.731, p<0.01, HDRS-24: r=0.663, p<0.01), and temporal stability (r=0.726, p<0.01) of KDRSS were all excellent. KDRSS showed good discriminative validity based on MARDS. KDRSS consisted of one-factor structure accounting for 63.8% of total variance. All subjects except two in full remission group had one or more residual symptoms. In 7 subscales of KDRSS consisting of similar items respectively, 'lack of energy' was the most commonly reported, followed by 'increased emotionalism' in this group. CONCLUSION: KDRSS is a useful and sensitive instrument for measuring residual depressive symptoms. Since some depressive symptoms including 'lack of energy' and 'increased emotionalism' in patients with full remission might be persistent during psychiatric intervention, these symptoms need to be focused on in clinical practice.

Measurement-based Treatment of Residual Symptoms Using Clinically Useful Depression Outcome Scale: Korean Validation Study.

OBJECTIVE: This study was aimed at evaluating the diagnostic validity of the Korean version of the Clinically Useful Depression Outcome Scale (CUDOS) with varying follow-up in a typical clinical setting in multiple centers. METHODS: In total, 891 psychiatric outpatients were enrolled at the time of their intake appointment. Current diagnostic characteristics were examined using the Structured Clinical Interview for DSM-IV (41% major depressive disorder). The CUDOS was measured and compared with three clinician rating scales and four self-report scales. RESULTS: The CUDOS showed excellent results for internal consistency (Cronbach's α, 0.91), test-retest reliability (patients at intake, r=0.81; depressed patients in ongoing treatment, r=0.89), and convergent and discriminant validity (measures of depression, r=0.80; measures of anxiety and somatization, r=0.42). The CUDOS had a high ability to discriminate between different levels of depression severity based on the rating of Clinical Global Impression for depression severity and the diagnostic classification of major depression, minor depression, and non-depression. The ability of the CUDOS to identify patients with major depression was high (area under the receiver operating characteristic curve=0.867). A score of 20 as the optimal cutoff point was suggested when screening for major depression using the CUDOS (sensitivity=89.9%, specificity=69.5%). The CUDOS was sensitive to change after antidepressant treatment: patients with greater improvement showed a greater decrease in CUDOS scores (p＜0.001). CONCLUSION: The results of this multi-site outpatient study found that the Korean version of the CUDOS is a very useful measurement for research and for clinical practice.

Do Somatic Symptoms Predict the Severity of Depression? A Validation Study of the Korean Version of the Depression and Somatic Symptoms Scale.

This study aimed at exploring the psychometric characteristics of the Korean Version of the Depression and Somatic Symptoms Scale (DSSS) in a clinical sample, and investigating the impact of somatic symptoms on the severity of depression. Participants were 203 consecutive outpatients with current major depressive disorders (MDD) or lifetime diagnosis of MDD. The DSSS was compared with the Montgomery-Åsberg Depression Rating Scale (MADRS) and the 17-items Hamilton Depression Rating Scale (HAMD). The DSSS showed a two-factor structure that accounted for 56.8% of the variance, as well as excellent internal consistency (Cronbach's alpha = 0.95), concurrent validity (r = 0.44-0.82), and temporal stability (intraclass correlation coefficient = 0.79). The DSSS had a high ability to identify patients in non-remission (area under receiver operating characteristic [ROC] curve = 0.887). Maximal discrimination between remission and non-full remission was obtained at a cut-off score of 22 (sensitivity = 82.1%, specificity = 81.4%). The number of somatic symptoms (the range of somatic symptoms) and the scores on the somatic subscale (SS, the severity of somatic symptoms) in non-remission patients were greater than those in remission patients. The number of somatic symptoms (slope = 0.148) and the SS score (slope = 0.472) were confirmed as excellent predictors of the depression severity as indicated by the MADRS scores. The findings indicate that the DSSS is a useful tool for simultaneously, rapidly, and accurately measuring depression and somatic symptoms in clinical practice settings and in consultation fields.

Wetting behavior on hexagonally close-packed polystyrene bead arrays with different topographies.

Herein, we investigated the wetting behavior of hexagonally close-packed polystyrene bead arrays with different bead diameters and surface flatness. The contact angle was found to be influenced by the surface roughness as well as the contact area of the polystyrene bead array with a water droplet.

Local liquid phase deposition of silicon dioxide on hexagonally close-packed silica beads.

Liquid phase deposition (LPD) is a useful method for the production of oxide film with low reaction temperature and production cost. With the report that the LPD of oxide films is conformally processed with uniform thickness and composition, there has been significant attention given to investigating its kinetic controls and growth mechanism on the flat surface. In this work, we explored the LPD of silicon dioxide on the hexagonally close-packed silica beads array as a nanostructured surface. The deposition and etching reactions of SiO2 occurred locally and simultaneously on silica beads, and were distinguished from the amount of fumed silica added in LPD solution. From locally competitive reactions, we obtained the anisotropic morphology of close-packed silica beads, and proposed a mechanism for the local LPD of SiO2 driven by nanostructured surfaces. This work contributes highly to improve metal oxide-based engineering, and also provide greater insight into the topography-driven LPD.

Cytoskeletal actin dynamics are involved in pitch-dependent neurite outgrowth on bead monolayers.

Neurite outgrowth is an important preceding step for the development of nerve systems. Given that the in vivo environments of neurons consist of numerous hierarchical micro/nanotopographies, there have been many efforts to investigate the relationship between neuronal behaviors and surface topography. The acceleration of neurite outgrowth was recently reported on surfaces with a periodic nanotopography, but the biological mechanism has not yet been elucidated. In this work, the initial neurite development of hippocampal neurons on assembled silica beads with diameters ranging from 700 to 1800 nm was explored. The acceleration of neurite outgrowth increased with the surface-pitch size and leveled off after a pitch of 1 µm. Biochemical analysis indicated that cytoskeletal actin dynamics were primarily responsible for the recognition of surface topography. This work contributes to the emerging research field of topographical neurochemistry, as well as applied fields including neuroregeneration and neuroprosthetics.

Effects of ginseol k-g3, an Rg3-enriched fraction, on scopolamine-induced memory impairment and learning deficit in mice.

BACKGROUND: Although ginsenosides such as Rg1, Rb1 and Rg3 have shown promise as potential nutraceuticals for cognitive impairment, their use has been limited due to high production cost and low potency. In particular, the process of extracting pure Rg3 from ginseng is laborious and expensive. METHODS: We described the methods in preparing ginseol k-g3, an Rg3-enriched fraction, and evaluated its effects on scopolamine-induced memory impairment in mice. RESULTS: Ginseol k-g3 (25-200 mg/kg) significantly reversed scopolamine-induced cognitive impairment in the passive avoidance, but not in Y-maze testing. Ginseol k-g3 (50 and 200 mg/kg) improved escape latency in training trials and increased swimming times within the target zone of the Morris water maze. The effect of ginseol k-g3 on the water maze task was more potent than that of Rg3 or Red ginseng. Acute or subchronic (6 d) treatment of ginseol k-g3 did not alter normal locomotor activity of mice in an open field. Ginseol k-g3 did not inhibit acetylcholinesterase activity, unlike donezepil, an acetylcholinesterase inhibitor. Rg3 enrichment through the ginseol k-g3 fraction enhanced the efficacy of Rg3 in scopolamine-induced memory impairment in mice as demonstrated in the Morris water maze task. CONCLUSION: The effects of ginseol k-g3 in ameliorating scopolamine-induced memory impairment in the passive avoidance and Morris water maze tests indicate its specific influence on reference or long-term memory. The mechanism underlying the reversal of scopolamine-induced amnesia by ginseol k-g3 is not yet known, but is not related to anticholinesterase-like activity.

Luteolin mediates the antidepressant-like effects of Cirsium japonicum in mice, possibly through modulation of the GABAA receptor.

Cirsium japonicum (CJ) has been shown to possess antidepressant-like properties. In the present study, we sought to identify which constituent of CJ might be responsible for its antidepressant effects and determine probable mechanism of action. The ethanol extract of CJ was administered to mice then behavioral changes were evaluated in the forced-swimming test (FST) and open-field test (OFT). In addition, its effects on norepinephrine (NE) reuptake and intracellular chloride (Cl(-)) flux were determined, in vitro. The effects of CJ's major constituents (linarin, pectolinarin, chlorogenic acid, luteolin) were also evaluated. CJ showed antidepressant-like effect by significantly reducing immobile behavior of mice in the FST, without increasing locomotor activity in the OFT. CJ had no effect on monoamine (NE) uptake, but it significantly promoted Cl(-) ion influx in human neuroblastoma cells. This CJ-induced Cl(-) influx was significantly blocked by co-administration of the competitive GABAA receptor antagonist, bicuculline. Among the major constituents of the CJ extract, only luteolin produced similar antidepressant-like effect, in vivo, and Cl(-) ion influx, in vitro. Altogether, the present results suggest that the antidepressant-like effect of CJ was most probably induced by its constituent luteolin, mediated through potentiation of the GABAA receptor-Cl(-) ion channel complex.

The ameliorating effect of Rosa roxburghii against ethanol-induced psychomotor alterations in rats.

BACKGROUND: Ethanol (EtOH) is one of the oldest recreational substances known to man, primarily taken because it induces a sense of well-being (euphoric effects) and relaxation (anxiolytic effects). EtOH use entails various negative consequences. Of particular interest are EtOH-induced psychomotor alterations, because of its immediate manifestation and adverse consequences. Rosa roxburghii (RR), a wild plant of Southwest China, has gained attention on account of its numerous beneficial effects on the immune, nervous, and cardiovascular systems. OBJECTIVE: In the present study we assessed the effects of Rosa roxburghii (RR) on EtOH-induced psychomotor alterations in rats. METHODS: Sprague Dawley rats were orally administered distilled water (control group) or ethanol (4 g/kg BW) (EtOH-group) to induce psychomotor alterations. RR extract (25, 50, and 100 mg/kg, p.o.) was administered 30 min before EtOH treatment (RR-group). EtOH-induced psychomotor alterations were evaluated in the open-field, accelerating rotarod, hanging wire, and cold swimming tests. Behavioral evaluation and hematological analysis (EtOH and acetaldehyde concentration) were done at 1, 2, 4 and 8 hours after EtOH administration. RESULTS: The EtOH group showed psychomotor alterations as compared with the control group. These EtOH-induced psychomotor alterations were directly related to the rise in blood ethanol and acetaldehyde concentrations. Pre-treatment of RR significantly improved EtOH-induced psychomotor alterations on open-field, accelerating rotarod, hanging wire, and cold swimming tests. These improvements in psychomotor performance coincided with the decreased blood ethanol and acetaldehyde levels observed in the RR-treated group. CONCLUSION: These results suggest that RR has ameliorating effects against EtOH-induced psychomotor alterations.

The ameliorating effects of 5,7-dihydroxy-6-methoxy-2(4-phenoxyphenyl)-4H-chromene-4-one, an oroxylin A derivative, against memory impairment and sensorimotor gating deficit in mice.

We previously reported that oroxylin A, a γ-aminobutyric acid A (GABAA) receptor antagonist, ameliorates drugs-induced memory impairments. We synthesized several oroxylin A derivatives in efforts to find a substance that has pro-cognitive effects as well as improves sensorimotor gating. The aim of the present study is to investigate the effect of a novel oroxylin A derivative, 5,7-dihydroxy-6-methoxy-2(4-phenoxyphenyl)-4H-chromene-4-one (DMPC), on pharmacological models of schizophrenia, which exhibit memory impairment and sensorimotor gating deficit. Memory impairment was induced by scopolamine, a muscarinic receptor antagonist, or MK-801, an N-methyl-D-aspartate receptor antagonist. Sensorimotor gating deficits were induced by MK-801 and measured by prepulse inhibition (PPI) of the acoustic startle response task. DMPC treatment (20 mg/kg) significantly attenuated scopolamine- or MK-801-induced memory impairment and it even enhanced cognitive performance of normal animals. Furthermore, DMPC significantly ameliorated MK-801-induced PPI deficits in the acoustic startle response task. In an in vitro study, DMPC (20 µM) inhibited intracellular Cl(-) influx induced by muscimol, a selective GABAA receptor agonist. These results suggest that DMPC would be a potential candidate for alleviating cognitive dysfunction and sensorimotor gating deficits in schizophrenia, and that its effects may be mediated, in part, via blockade of the GABAergic neurotransmitter system.

The involvement of magnoflorine in the sedative and anxiolytic effects of Sinomeni Caulis et Rhizoma in mice.

The present study seeks to evaluate the sedative and anxiolytic effects of the 70% ethanol extract of Sinomeni Caulis et Rhizoma (SR). The extract was orally administered to mice at dosages of 25, 50, 100, 200 or 400 mg/kg. The mice were then subjected to an array of behavioral tests to assess the sedative (open-field, rota-rod, and thiopental sodium-induced sleeping test) and anxiolytic (elevated plus maze test) effects of the substance. SR (100, 200 mg/kg) significantly reduced locomotor activity, decreased rota-rod performance, and potentiated thiopental sodium-induced sleeping in mice, all indicative of its sedative effects. SR (50, 100 mg/kg) also produced anxiolytic effects, as shown by an increase in entries and staying time on the open arm of the plus maze. SR's sedative and anxiolytic effects were comparable to that of the benzodiazepine, diazepam. Moreover, to identify SR's probable mechanism of action, intracellular Cl⁻ ion influx was observed in cultured human neuroblastoma cells. SR dose-dependently increased Cl⁻ influx, which was blocked by co-administration of the GABAA receptor competitive antagonist, bicuculline. Among the major constituents of SR, only magnoflorine showed a similar increment in Cl⁻ influx, which was also blocked by bicuculline. Altogether, the present results suggest that SR has sedative and anxiolytic effects, probably mediated by magnoflorine through a GABAergic mechanism of action.