scholarly journals Anti-cholinesterase Activity of Crude Drugs Selected from the Ingredients of Incense Sticks and Heartwood of Chamaecyparis obtusa

2018 ◽  
Vol 13 (7) ◽  
pp. 1934578X1801300
Author(s):  
Kazuya Murata ◽  
Kanae Tanaka ◽  
Reina Akiyama ◽  
Ibuki Noro ◽  
Arisa Nishio ◽  
...  
Keyword(s):  
Acetylcholinesterase Activity ◽  
Chamaecyparis Obtusa ◽  
Significant Inhibition ◽  
Active Principle ◽  
Asian Countries ◽  
Number Of Patients ◽  
Type Mode ◽  
Crude Drugs ◽  
Butyrylcholinesterase Activity ◽  
Ad Therapy

An effective agent for the treatment and/or prevention of Alzheimer's disease (AD) is needed due to the number of patients in the acute curve. In our research program to investigate effective agents for AD, we focused on crude drugs which consisted of incense sticks widely used in Asian countries including Japan. We selected 9 drugs as “aromatic” crude drugs and 2 as basal crude drugs. Among the samples tested, the essential oil obtained from the leaf of Cryptomeria japonica showed the most potent anti-acetylcholinesterase activity with 64.8% of inhibition at 100 μg/mL. In addition, no sample showed significant inhibition against β-secretase. From these results, the crude drugs selected in this study may be effective for AD therapy rather than prevention. The active principles of anti-acetylcholinesterase were investigated by activity-guided fractionation, and kaur-16-ene, nezukol and ferruginol were successfully identified, the IC50 values were 640, 300 and 95 μM, respectively. Kaur-16-ene and nezukol inhibited acetylcholinesterase in the mixed type mode, while ferruginol inhibited it in the competitive mode. In addition, nezukol and ferruginol showed anti-butyrylcholinesterase activity, the IC50 values were 155 and 22 μM, respectively. We also focused on the heartwood of Chamaecyparis obtusa, since this tree has been used as a building material for the heartwood of C. japonica. Ethyl acetate extract of C. obtusa showed anti-acetylcholinesterase activity of 37.7% inhibition at 100 μg/mL. The active principle was determined to be (-)-hinokinin by activity-guided fractionation and the IC50 value was 176 μM. These results suggest that the leaf of C. japonica and heartwood of C. obtusa may be suitable agents for AD therapy when administered through the nasal system as an aroma supplement.

scholarly journals Screening of Spice Extracts Possessing Anti-Acetylcholinesterase Activity and Active Principle of Bitter Ginger, Rhizome of Zingiber zerumbet

2017 ◽  
Vol 12 (7) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Kazuya Murata ◽  
Yusuke Ishida ◽  
Arisa Nishio ◽  
Sayaka Nakagawa ◽  
Hirokazu Kawamoto ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Ethyl Acetate Extract ◽  
Acetylcholinesterase Activity ◽  
Active Principle ◽  
Plant Resources ◽  
Zingiber Zerumbet ◽  
Ginger Rhizome ◽  
Cholinesterase Activities ◽  
Butyrylcholinesterase Activity

In our research program for investigating anti-dementia agents from natural plant resources, we screened extracts from 15 spice samples. Among the plant extracts tested, ethyl acetate extract prepared from rhizome of Zingiber zerumbet showed potent activity. Activity-guided purification led to determination of afzelin and its acetylated compound as the active principles. Afzelin showed moderate inhibitory activity against acetylcholinesterase and may also be expected to possess anti-butyrylcholinesterase activity. This is the first report to reveal the anti-cholinesterase activities of ethyl acetate extract of Z. zerumbet and afzelin. Furthermore, Z. zerumbet may be a potential therapeutic agent for the improvement of dementia, especially Alzheimer's disease.

Chemically Contaminated Eel Fed to Pregnant and Lactating Mouse Dams Causes Hyperactivity in Their Offspring

2016 ◽  
Vol 86 (1-2) ◽  
pp. 36-47 ◽  
Author(s):  
Imen Dridi ◽  
Nidhal Soualeh ◽  
Torsten Bohn ◽  
Rachid Soulimani ◽  
Jaouad Bouayed
Keyword(s):  
Open Field ◽  
Early Life ◽  
Home Cage ◽  
Anguilla Anguilla ◽  
Acetylcholinesterase Activity ◽  
Female Offspring ◽  
Significant Inhibition ◽  
Standard Diet ◽  
Early Life Exposure ◽  
Cage Test

Abstract.This study examined whether perinatal exposure to polluted eels (Anguilla anguilla L.) induces changes in the locomotor activity of offspring mice across lifespan (post-natal days (PNDs) 47 – 329), using the open field and the home cage activity tests. Dams were exposed during gestation and lactation, through diets enriched in eels naturally contaminated with pollutants including PCBs. Analysis of the eel muscle focused on the six non-dioxin-like (NDL) indicator PCBs (Σ6 NDL-PCBs: 28, 52, 101, 138, 153 and 180). Four groups of dams (n = 10 per group) received either a standard diet without eels or eels (0.8 mg/kg/day) containing 85, 216, or 400 ng/kg/day of ϵ6 NDL-PCBs. The open field test showed that early-life exposure to polluted eels increased locomotion in female offspring of exposed dams but not in males, compared to controls. This hyperlocomotion appeared later in life, at PNDs 195 and 329 (up to 32 % increase, p < 0.05). In addition, overactivity was observed in the home cage test at PND 305: exposed offspring females showed a faster overall locomotion speed (3.6 – 4.2 cm/s) than controls (2.9 cm/s, p <0.05); again, males remained unaffected. Covered distances in the home cage test were only elevated significantly in offspring females exposed to highest PCB concentrations (3411 ± 590 cm vs. 1377 ± 114 cm, p < 0.001). These results suggest that early-life exposure to polluted eels containing dietary contaminants including PCBs caused late, persistent and gender-dependent neurobehavioral hyperactive effects in offspring mice. Furthermore, female hyperactivity was associated with a significant inhibition of acetylcholinesterase activity in the hippocampus and the prefrontal cortex.

scholarly journals COMPARATIVE STUDY ON ANTIMICROBIAL ACTIVITY OF SEAWEEDS

2017 ◽  
Vol 10 (12) ◽  
pp. 384 ◽  
Author(s):  
Sasikala C ◽  
Geetha Ramani D
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Broad Spectrum ◽  
Large Scale ◽  
Biological Activities ◽  
Maximum Activity ◽  
Significant Inhibition ◽  
Drug Formulation ◽  
Active Principle ◽  
Pharmaceutical Industries

Objective: Secondary metabolites from natural resources are a potential source of antimicrobial leads and drugs can exploited to combat antimicrobial resistance in microorganisms. Seaweeds are considered as a valuable source with a broad spectrum of biological activities. Hence, this study was undertaken to screen seaweeds from Mandapam coastal waters, East coast of India, for antimicrobial activity.Methods: Compounds were extracted using methanol from the seaweeds, namely, Halimeda gracilis, Caulerpa serrulata, Sargassum swartzii, Sargassum wightii, Jania rubens, Ulva lactuca, Ulva fasciata, Gracilaria corticata, Stoechospermum marginatum, Caulerpa scalpelliformis, Caulerpa taxifolia, Chaetomorpha crassa, Enteromorpha flexuosa, and Turbinaria ornate. The extracts were screened for their antimicrobial activity against selected bacterial and fungal pathogens.Results: In the present study, S. swartzii, J. rubens, and S. marginatum showed broad spectrum of antibacterial activity against all the test bacterial pathogens. Among these, the maximum activity was exhibited by S. swartzii against Enterococcus faecalis (27.00 ± 0.88) and Streptococcus pyogenes (23.00 ± 0.84), followed by J. rubens against E. faecalis (26.00 ± 0.56) and S. pyogenes (22.00 ± 0.75), and S. marginatum exhibited significant inhibition against Staphylococcus aureus (15.00 ± 0.22) and S. pyogenes (18.00 ± 1.16).Conclusion: These seaweeds with significant antibacterial activity will subjected to phytochemical screening to find out the potential active principle responsible for antimicrobial activity. It is followed by purification and characterization of the compounds for possible application in drug formulation, can take this to large-scale application in pharmaceutical industries.

The inhibitory effects of polyoxyethylene detergents on human erythrocyte acetylcholinesterase and Ca2+ + Mg2+ ATPase

1989 ◽  
Vol 67 (2-3) ◽  
pp. 137-146 ◽  
Author(s):  
R. Blaine Moore ◽  
J. F. Manery ◽  
J. Still ◽  
V. N. Mankad
Keyword(s):  
Human Erythrocyte ◽  
Acetylcholinesterase Activity ◽  
Significant Inhibition ◽  
Erythrocyte Membranes ◽  
Head Group ◽  
Polar Head Group ◽  
Detergent Concentration ◽  
Human Erythrocyte Membranes ◽  
Hydrophobic Tail ◽  
Triton X

The activities of acetylcholinesterase and Ca2+ + Mg2+ ATPase were measured following treatment of human erythrocyte membranes with nonsolubilizing and solubilizing concentrations of Triton X-100. A concentration of 0.1% (v/v) Triton X-100 caused a significant inhibition of both enzymes. The inhibition appears to be caused by perturbations in the membrane induced by Triton X-100 incorporation. No acetylcholinesterase activity and little Ca2+ + Mg2+ ATPase activity were detected in the supernatant at 0.05% Triton X-100 although this same detergent concentration induced changes in the turbidity of the membrane suspension. Also, no inhibition of soluble acetylcholinesterase was observed over the entire detergent concentration range. The inhibition of these enzymes at 0.1% Triton X-100 was present over an eightfold range of membrane protein in the assay indicating an independence of the protein/detergent ratio. The losses in activities of these two enzymes could be prevented by either including phosphatidylserine in the Triton X-100 suspension or using Brij 96 which has the same polyoxyethylene polar head group but an oleyl hydrophobic tail instead of the p-tert-octylphenol group of Triton X-100. The results are discussed in regard to the differential recovery of enzyme activities over the entire detergent concentration range.Key words: Triton X-100, erythrocyte membranes, acetylcholinesterase, Ca2+ + Mg2+ ATPase, polyoxyethylene detergents.

scholarly journals Four Major Factors Contributing to Intrahepatic Stones

2017 ◽  
Vol 2017 ◽  
pp. 1-5 ◽  
Author(s):  
Xi Ran ◽  
Baobing Yin ◽  
Baojin Ma
Keyword(s):  
Bile Duct ◽  
Effective Procedure ◽  
Asian Countries ◽  
Recurrence Rates ◽  
Intrahepatic Stones ◽  
Intrahepatic Stone ◽  
Metabolic Defect ◽  
Number Of Factors ◽  
Number Of Patients ◽  
Major Factors

Intrahepatic stone is prevalent in Asian countries; though the incidence declines in recent years, the number of patients is still in a large quantity. Because of multiple complications, high recurrence rates, serious systemic damage, and a lack of extremely effective procedure for the management, it is more important to find out the etiology and pathogenesis of intrahepatic stones to prevent the disease from happening and developing rather than curing. A number of factors contribute to the development of the disease, such as cholestasis, infection, and anatomic abnormity of bile duct and bile metabolic defect. The four factors and possible pathogenesis will be discussed in detail in the review.

scholarly journals Results of Intercontinental Cooperative Non-Hodgkin T-Cell Lymphoma Prospective Registry Study

Blood ◽  
2019 ◽  
Vol 134 (Supplement_1) ◽  
pp. 4035-4035
Author(s):  
Sang Eun Yoon ◽  
Seok Jin Kim ◽  
Tsai-Yun Chen ◽  
Yong Park ◽  
Li Mei Poon ◽  
...  
Keyword(s):  
T Cell ◽  
Treatment Outcomes ◽  
Clinical Features ◽  
Research Funding ◽  
Cell Lymphoma ◽  
T Cell Lymphoma ◽  
Registry Study ◽  
Asian Countries ◽  
T Cell Lymphomas ◽  
Number Of Patients

Introduction T-cell lymphoma is a group of heterogeneous diseases with various clinical behaviors and treatment outcomes, representing 10-15% of non-Hodgkin lymphomas. Owing to its rarity and heterogeneity, the standard treatment approach for T-cell lymphoma is still not established. Accordingly, conventional chemotherapy regimens adapted from B-cell lymphoma treatment has been used for T-cell lymphoma. However, their outcome is still not satisfactory, and there are limited data representing the real-world situation in terms of clinical features and treatment outcomes. Given the incidence of T-cell lymphoma is relatively higher in Asian than Western countries; a comprehensive registry study focusing on Asian patients with T-cell lymphoma could be helpful for better understanding of T-cell lymphoma as well as the development of more effective treatment strategy. Methods We performed a multi-national, multi-center, prospective registry study for patients with T-cell lymphoma and enrolled patients between 01-March-2016 and 31-January-2019. All patients received chemotherapy with curative intent after diagnosis, and were pathologically diagnosed with T-cell lymphoma according to the 2008 World Health Organization classification of lymphoid neoplasms. Patients belonged to any one of following clinical situations could be enrolled: (1) newly diagnosed, treatment-naïve patients; (2) patients who started treatment or completed treatment; (3) relapsed or refractory patients. After we enrolled the planned number of patients (n = 500), we analyzed clinical features and treatment outcomes. Results Out of 500 patients enrolled from nine Asian countries (Korea, China, Taiwan, Singapore, Indonesia, Bangladeshi, Vietnam, Malaysia, and Philippines), 490 patients were analyzed because 10 patients with insufficient information were excluded. The median age was 59 years (range, 20-85), male patients (59%) were predominant compared to female patients (41%). Extranodal NK/T-cell lymphoma (ENKTL) was the most common (28%) and angioimmunoblastic T-cell lymphoma (AITL) was the second common (24%). Peripheral T-cell lymphoma, not-otherwise specified (PTCL-NOS, 20%) and ALK+/- anaplastic large cell lymphoma (ALCL, 16%) were also major subtypes of T-cell lymphoma. The proportion of stage IV was 40%, however, the distribution of stage was different between ENKTL and nodal T-cell lymphomas such as PTCL-NOS. The CHOP (Cyclophosphamide, doxorubicin, vincristine, and prednisone) or CHOP-like regimens accounted for the mainstay of primary treatment for nodal T-cell lymphoma whereas non-anthracycline-based chemotherapy regimens such as SMILE (steroid, methotrexate, ifosfamide, L-asparaginase, and etoposide) and GemOx-L (gemcitabine, oxaliplatin, and L-asparagainase) were mainly used for ENKTL. The overall survival of ENKTL was not significantly different from that of PTCL-NOS, AITL and ALK+/- ALCL. Conclusions Our study showed the distribution of T-cell lymphoma subtypes and tumor burdens at the time of diagnosis in Asian countries. Although clinical features of ENKTL are different from that of nodal T-cell lymphomas consisting of PTCL-NOS, AITL and ALK+/- ALCL, and the different types of treatment were used, survival outcome of patients were not significantly different. This finding might be associated with improved treatment outcomes of ENKTL compared to the past. However, considering a substantial number of patients experienced treatment failure in patients with PTCL-NOS as well as ENKTL, more effective treatment strategy should be warranted. Figure Disclosures Kim: F. Hoffmann-La Roche Ltd: Research Funding; Celltrion: Research Funding; Novartis: Research Funding; Donga: Research Funding; Kyowa-Kirin: Research Funding; Novartis: Research Funding; J + J: Research Funding.

scholarly journals Changes of Cholinesterase Activity in the Erythrocytes, Plasma, Diaphragm, Liver and Various Parts of the Brain in the Rabbit Following Transfusion of Erythrocytes with Soman Inhibited Acetylcholinesterase

1997 ◽  
Vol 40 (2) ◽  
pp. 37-39
Author(s):  
Jiří Kassa ◽  
Jiří Bajgar ◽  
Josef Fusek
Keyword(s):  
Blood Transfusion ◽  
Cholinesterase Activity ◽  
Acetylcholinesterase Activity ◽  
Significant Inhibition ◽  
Peripheral Compartment ◽  
Peripheral Tissues ◽  
Cholinesterase Activities ◽  
The Brain

1. The changes of cholinesterase activity in rabbit blood, peripheral tissues and the central nervous system following transfusion of erythrocytes with soman inhibited acetylcholinesterase were demonstrated. 2. After incubation with soman for 0.5 or 24 h, erythrocytes without acetylcholinesterase activity were injected to intact rabbits and cholinesterase activity in the erythrocytes, plasma, diaphragm, liver and various parts of the brain were evaluated 24 h following blood-transfusion. 3. When erythrocytes were incubated with soman for 24 h, no changes of cholinesterase activity in the rabbit following blood-transfusion were observed with an exception of erythrocyte acetylcholinesterase. 4. When erythrocytes were incubated with soman for 0.5 h, a significant decrease in cholinesterase activity in the erythrocytes, plasma, diaphragm and liver following blood-transfusion was found. These data show that soman is able to release from erythrocytes and inhibit cholinesterase activities not only in vitro but also in vivo although the significant inhibition of cholinesterase activities by soman was only observed in the peripheral compartment.

The Pharmacological and Pathological Studies on Taiwan Folk Medicine (VII): The Anti-inflammatory Effect of Echinops grjiisii

1992 ◽  
Vol 20 (02) ◽  
pp. 127-134 ◽  
Author(s):  
Chun-Ching Lin ◽  
Cheng-hung Lin ◽  
Hui-Fen Chiu ◽  
Min-Fu Hu
Keyword(s):  
Methanolic Extract ◽  
Folk Medicine ◽  
Animal Experiments ◽  
Active Principle ◽  
Chloroform Fraction ◽  
Protective Effects ◽  
Active Components ◽  
Crude Drugs ◽  
Anti Inflammatory ◽  
Inflammatory Effect

The hepatotoxic-protective effects of "San-fang-feng" (the root of E. grijisii) and "Lou-lu" (the root of E. latifolius) on CCl 4 induced hepatotoxicity have been proposed in our previous paper (Lin et al, 1990). The anti-inflammatory effects of these two crude drugs were investigated in this experiment. The results indicated that both of them displayed pronounced anti-inflammatory activities against carrageenan-induced edema. Furthermore, in order to isolated the main active components of E. grijisii, fractions obtained from the methanolic extract of E. grijisii were investigated in mice for their 24-h LD 50 and 95% confidence limits, which could be used as a guiding for further animal experiments. Our findings demonstrated that n-hexane (100,300 mg/kg), chloroform (30,100,300 mg/kg) and ethyl acetate (30,100, 300 mg/kg) fractions could markedly inhibit the carrageenan-induced inflammation, and the main active principle was found to be concentrated in the chloroform fraction, which possessed significant inhibitory activities even more than does indomethacin.

scholarly journals Prospective, observational, single-centre cohort study with an independent control group matched for age and sex aimed at investigating the significance of cholinergic activity in patients with schizophrenia: study protocol of the CLASH-study

BMJ Open ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. e050501
Author(s):  
Benedikt Schick ◽  
Eberhard Barth ◽  
Benjamin Mayer ◽  
Claire-Louise Weber ◽  
Theresa Hagemeyer ◽  
...  
Keyword(s):  
Cohort Study ◽  
Clinical Symptoms ◽  
Point Of Care ◽  
Acetylcholinesterase Activity ◽  
Primary Objective ◽  
University Hospital ◽  
Control Group ◽  
Independent Control ◽  
Data Set ◽  
Butyrylcholinesterase Activity

IntroductionAlterations in the cholinergic metabolism may cause various clinical symptoms of schizophrenia. In addition to the ‘monoamine hypothesis,’ neuroinflammation is also discussed as a cause of schizophrenia. To date, there has been no evidence of alterations in the central cholinergic transmitter balance in patients with schizophrenia under clinical conditions. By contrast, studies in critically ill patients have established the measurement of acetylcholinesterase activity as a suitable surrogate parameter of central cholinergic transmitter balance/possible pathophysiological changes. Butyrylcholinesterase activity has been established as a parameter indicating possible (neuro)inflammatory processes. Both parameters can now be measured using a point-of-care approach. Therefore, the primary objective of this study is to investigate whether acetylcholinesterase and butyrylcholinesterase activity differs in patients with various forms of schizophrenia. Secondary objectives address the possible association between acetylcholinesterase and butyrylcholinesterase activity and (1) schizophrenic symptoms using the Positive and Negative Syndrome Scale, (2) the quantity of antipsychotics taken and (3) the duration of illness.Methods and analysisThe study is designed as a prospective, observational cohort study with one independent control group. It is being carried out at the Department of Psychiatry and Psychotherapy III, Ulm University Hospital, Germany. Patient enrolment started in October 2020, and the anticipated end of the study is in January 2022. The enrolment period was set from October 2020 to December 2021 (extension required due to SARS-CoV-2 pandemic). The sample size is calculated at 50 patients in each group. Esterase activity is measured on hospital admission (acute symptomatology) and after referral to a postacute ward over a period of three consecutive days. The matched control group will be created after reaching 50 patients with schizophrenia. This will be followed by a comprehensive statistical analysis of the data set.Ethics and disseminationThe study was registered prospectively in the German Clinical Trials Register (DRKS-ID: DRKS00023143,URL: https://www.drks.de/drks_web/navigate.do?navigationId=trial.HTML&TRIAL_ID=DRKS00023143) after approval by the ethics committee of the University of Ulm, Germany Trial Code No. 280/20.Trial registration numberDRKS00023143; Pre-results.

scholarly journals Effect of processing on antioxidant and anticholinesterase activities of bilberry (Vaccinium myrtillus L.) juice

2020 ◽  
Vol 19 (6) ◽  
pp. 113-123
Author(s):  
Kamila Borowiec ◽  
Dominik Szwajgier
Keyword(s):  
Heat Treatment ◽  
Acetylcholinesterase Activity ◽  
Enzyme Preparations ◽  
Valuable Source ◽  
Juice Processing ◽  
Combined Application ◽  
Heating Treatment ◽  
Butyrylcholinesterase Activity ◽  
Vaccinium Myrtillus L ◽  
Anticholinesterase Agents

Bilberry fruit is a valuable source of many antioxidant and anticholinesterase agents. Thus, the aim of the present study was to determine the effect of heat treatment combined with enzyme preparations on the antioxidant and anticholinesterase activity of bilberry juices. Each bilberry juice efficiently ‘scavenged’ DPPH and ABTS radicals. The highest ability to remove DPPH radicals was found in pre-heated (80–90C, 5 min) and non-heated (only 50–55C, 2 h) juices obtained using Pectinex BE XXL. The pre-heating treatment caused an increase in the anti-acetylcholinesterase activity compared to non-heated juices, with the highest elevation (p < 0.05) recorded for juice produced using Panzym BE XXL. Similarly, the heat pretreatment caused an increase in the anti-butyrylcholinesterase activity in bilberry juices. The combined application of pre-heating and enzyme preparations during juice processing resulted in an increase in the antioxidant and anticholinesterase activities of the end juices.

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