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Search for safe antioxidants and novel nutraceuticals urged to evaluate the antioxidant, anti-acetylcholine esterase and anti-lipoxygenase activity of various leaf extracts of Conocarpus lancifolius. Extraction was optimized from freeze dried plant extracts quenched with liquid nitrogen using water, ethanol, methanol, hexane, ethyl acetate and chloroform. Maximum extract yield, total phenolic contents and total flavonoid contents were obtained in case of ethanolic extraction. The highest 2,2-diphenyl-1-picrylhydrazylradical scavenging in terms of IC50 value of 55.26 µg/mL was observed for ethanolic leaf extract. The acetylcholine esterase and lipoxygenase inhibitory activities (IC50) were also observed for ethanolic extract. These findings for ethanolic extract were statistically significant when compared with other extracts (ρ<0.05). The haemolytic % values indicated that all extracts were associated with very low or negligible toxicity. The epicatechin, isorhamnetin, rutin, scopoleptin, skimmianine, quercetin-3-O-α-rhamnoside, quercetin-3-O-ß-glucoside, cornoside, creatinine, choline, pyruvic acid, α-hydroxybutyric acid, phyllanthin and hypophyllanthin were identified as major functional metabolites in ethanolic leaf extract of C. lancifoliusby 1H-NMR. The identified metabolites were probably responsible for the pharmacological properties of C.lancifolius. The findings may be utilized as pharmacological leads for drug development and food fortification.
Se insta a la búsqueda de antioxidantes seguros y nuevos nutracéuticos para evaluar la actividad antioxidante, anti-acetilcolina esterasa y anti-lipoxigenasa de varios extractos de hojas de Conocarpus lancifolius. La extracción se optimizó a partir de extractos de plantas liofilizados enfriados con nitrógeno líquido usando agua, etanol, metanol, hexano, acetato de etilo y cloroformo. En el caso de extracción etanólica se obtuvo el rendimiento máximo de extracto, el contenido de fenoles totales y el contenido de flavonoides totales. La mayor eliminación de radicales 2,2-difenil-1-picrilhidrazilo en términos de valor de CI50 de 55,26 µg/mL se observó para el extracto de hoja etanólico. También se observaron las actividades inhibidoras de la acetilcolina esterasa y lipoxigenasa (CI50) para el extracto etanólico. Estos hallazgos para el extracto etanólico fueron estadísticamente significativos en comparación con otros extractos (ρ<0.05). Los valores del % hemolítico indicaron que todos los extractos estaban asociados con una toxicidad muy baja o insignificante. Se identificaron la epicatequina, isorhamnetina, rutina, escopoleptina, skimmianina, quercetina-3-O-α-ramnosido, quercetina-3-O-ß-glucósido, cornosido, creatinina, colina, ácido pirúvico, ácido α-hidroxibutírico, filantrina e hipofillantina. como metabolitos funcionales principales en el extracto etanólico de hojas de C. lancifoliuspor 1H-NMR. Los metabolitos identificados probablemente fueron responsables de las propiedades farmacológicas de C. lancifolius. Los hallazgos pueden utilizarse como pistas farmacológicas para el desarrollo de fármacos y la fortificación de alimentos.
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Plant Extracts/pharmacology , Combretaceae/chemistry , Antioxidants/pharmacology , Phenols/analysis , Flavonoids/analysis , In Vitro Techniques , Plant Extracts/chemistry , Cholinesterase Inhibitors/pharmacology , Cholinesterase Inhibitors/chemistry , Free Radical Scavengers , Lipoxygenase Inhibitors/pharmacology , Lipoxygenase Inhibitors/chemistry , Ethanol , Antioxidants/chemistryABSTRACT
Background: Excessive consumption of High Fat Diet (HFD) harmfully impacts body tissues and organs. Interestingly, there is a highconcern towards the use of medicinal plants to ameliorate those harmful effects. Objectives: This study is aimed at investigating the effectivepossibility of Nigella Sativa (NS) seeds powder on liver and small intestine of the rats fed on HFD using biochemical, histological andmorphometric techniques. Material and Methods: Eighteen adult male albino rats were randomly divided into three equal groups. Group I(control) was fed on standard rat pellets chow, Group II (HFD) was fed on standard diet mixed butter (20% fat of diet) and Group III (HFD+ NS) was fed on HFD and concomitantly administrated Nigella sativa (300 mg/Kg daily orally) for 8 weeks. The biochemical studyincluded lipid profile assessment and the histological study included paraffin sections of small intestine and liver stained by Hematoxylinand Eosin, Masson-trichrome for liver collagen and PAS for intestinal Goblet cells to evaluate the histological alteration. Quantitativestatistical analysis of area percent of liver collagen content and goblet cells was done using Digital pro-image analysis. Results: HFD wasassociated with increased serum lipid profile. The histological analysis of hepatic sections revealed abundant fat deposition, inflammatorycell infiltrate, degeneration of hepatocytes with significant increase of collagen fibers as shown by image analysis. Inflammatory changeswith significant reduction in the mean area percent of Goblet cells were observed in intestine of HFD group. NS intake significantly loweredserum level of total cholesterol, triglycerides and LDL, in concomitant with reversed HFD-induced histological alteration by decreasinghepatic collagen deposition and increasing intestinal goblet cells. Conclusion: Biochemical, histological and morphometric resultsprovided further evidence that crude NS seeds powder can ameliorate high fat diet–induced alteration in liver and small intestinesuggesting its beneficial use in preventive medicine.
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Objective To observe the effects of Shenqi Xingnao Prescription on learning and memory ability, contents of choline acetyltransferase (ChAT) and acetylcholine esterase (AChE) in brain tissue in mice models with scopolamine-induced Alzheimer disease (AD); To investigate its mechanism for prevention and treatment for AD. Methods Totally 110 ICR mice were randomly divided into control group, control+Shenqi Xingnao Prescription high-dose group,model group,donepezil group,model+Shenqi Xingnao Prescription high-,medium-,and low-dose groups. The control and model group were given distilled water for gavage, and the other groups were given the corresponding medicine for gavage, once a day, for 14 days. On the 15th day, Morris water maze test and object recognition test were used to evaluate the learning and memory ability of each group. The model mice of memory impairment induced by intraperitoneal injection of scopolamine was established 20 minutes before the behavioral test. The expressions of ChAT and AChE in cortex and hippocampus were detected by Western blot. Results The results of Morris water maze test showed that compared with the control group, the model group had significant longer escape latency(P<0.05);Compared with the model group,Shenqi Xingnao Prescription medium-and high-dose groups could shorten the escape latency (P<0.05). The results of the object recognition test showed that compared with the control group, the ability of the model group to explore new things decreased and the discrimination index (DI) decreased (P<0.001);Compared with the model group,Shenqi Xingnao Prescription groups could increase the DI of model mice (P<0.05, P<0.01, P<0.001). The results of Western blot showed that the expression of AChE protein in the cortex and hippocampus of the model group was significantly higher than the control group (P<0.01); Compared with the model group, Shenqi Xingnao Prescription low- and medium-dose groups could decrease the expression of AChE in the cortex in different degrees(P<0.01);Shenqi Xingnao Prescription groups could decreaed the expression of AChE in the hippocampus (P<0.001); There was no significant statistical significance in the expression of ChAT in the cortex and hippocampus in each group.Conclusion Shenqi Xingnao Prescription can significantly improve the learning and memory ability of AD model mice induced by scopolamine, which may be related to the descent expression of AChE protein in the cortex and hippocampus of the model mice.
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Objective To investigate the effect of 17β-estradiol on ketamine-induced long-term cognitive deficits in neonatal rats.Methods 80 SD male rats aged 7 days were randomly divided into group C,V,E,K and K+E,and 16 per group.Group C was intraperitoneally injected with same volume of saline for three consecutive days,Group V was subcutaneously injected with same volume of sesame oil for three consecutive days,Group E was subcutaneously injected with 600 μg · kg-1 17β-estradiol for three consecutive days,group K was intraperitoneally injected with 75 mg · kg-1 ketamine for three consecutive days,group K+E was intraperitoneally injected with 75 mg · kg-1 ketamine in combination with 600 μg · kg-1 17β-estradiol injected subcutaneously for three consecutive days.At 2 months of age,learning and memory abilities were tested with the Mortis water maze.After Morris water naze test,ten rats from each group were decapitated and the prefrontal cortex (PFC) was isolated to detect acetylcholine esterase(AchE) activity with ELISA assay and to measure acetylcholine(Ach) level by hydroxylammonium chloride method.Results The escape latency ((40.26±2.36) s,(30.25±2.20) s,(21.55±2.42) s) and path length((1019.35±58.13) cm,(811.16±27.58) cm,(598.34±34.74) cm) of group K were more than those of group C on the third,fourth aud fifth training days (all P＜0.05),while escape latency ((29.46±2.20) s,(24.86± 2.14) s,(17.20±1.91) s) and path length((913.90±41.89) cm,(729.42±31.36) cm,(487.64±18.61)cm) of group K+E were significantly lower than those of group K(all P＜0.05).On test day 6,rats were subjected to a probe trial,ratio of time spent in the target quadrant ((24.5±2.7) ％) and the number of crossings over previous platform locations (1.9±0.5) in group K were fewer than those of group C (all P＜0.05),while ratio of time spent iu the target quadrant((42.3±3.0) ％) and the number of crossings over previous platform locations(3.5±0.5) of group K+E were more than those of group K (all P＜0.05).The AchE activity((0.69±0.04) U · mg pro-1) in rats PFC of group K was significantly higher than that of group C ((0.52±0.06) U · mg pro-1) (P＜0.05).The AchE activity of group K +E ((0.58±0.12)U · mg pro-1) was lower than that of group K(P＜0.05).The Ach level ((2.59±0.34)mg · g-1) in rats PFC of group K was significantly lower than that of group C ((4.35±0.56) mg · g-1) (P＜0.05).The Ach level of group K+E((3.88±0.61) mg · g-1) was higher than that of group K(P＜0.05).Conclusions These results indicate that ketamine impairs learning and memory abilities as rat matures,while 17β-estradiol treatment improves these impairments by inhibiting AchE activity and increasing Ach level.
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In the recent decade, there has been increasing concern on the hazard effect of drugs on different species. Stressful life events contribute to the development of many neurodegenerative and neuropsychiatric disorders including depression and anxiety. Alprazolam (ALP) is commonly used and approved for the medical treatment of panic and anxiety disorders, such as generalized anxiety or social anxiety disorders. Thus, it was of a particular interest to investigate the effect of ALP on the neurons of cerebellar cortex of mice, where mice have genomic similarities to human. So, biochemical, histological and ultrastructural investigations are reported on the cerebellum of adult male mice subjected to three different doses of ALP, for two months. These doses were equivalent to the human therapeutic doses as 0.5, 1 and 1.5 mg. In a dose dependant manner, significant decreases in the levels of both acetylcholine enzyme activities and total glutathione are recorded, indicating that the activity of acetylcholine esterase was inhibited by free radical formation. Little histopathological changes were observed in the cerebellar cortex of mice administered with 0.5 mg ALP. Marked alterations were observed in the Purkinje neurons of cerebellar cortex of mice administered with 1 and 1.5 mg ALP, where unstained haloes are seen around most of these cells. Their nuclei were eccentrically placed, and pyknotic. The intracellular structure of Purkinje cells showed dilatation of both rER and Golgi apparatus. Many small vesicles near the Golgi bodies were accumulated to form clusters, probably indicate disturbance in the vesicular transport between rER and Golgi apparatus. These results reflect the injured effect of high dose ALP on brain activity, performing in the possible ultrastructural abnormalities as well as its oxidative stress.
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BACKGROUND:Classical drug for Parkinson’s disease is levodopa, but long-term application of levodopa can induce complications such as dyskinesias. OBJECTIVE:To observe the effects of levodopa on learning and memory capacities of Parkinson’s disease rats and to study its mechanisms. METHODS:The rat models of Parkinson’s disease were established using 6-hydroxydopamine. The 228 model rats were randomly divided into control group and experimental group. Rats in the experimental group were intraperitoneal y injected with 10, 20 and 30 mg/(kg?d) levodopa for 28 consecutive days. At 1, 3, 5, 7, 14 and 28 days after intraperitoneal injection, we observed the rats’ learning and memory capacities and tested plasma concentration of homocysteine and folic acid. Acetylcholinesterase activities in the rat hippocampus were measured. Hippocampal neurofibril ary tangles were observed using Bielschowsky staining. RESULTS AND CONCLUSION:Increased dose of levodopa and prolonged application time obviously decreased learning and memory capacities in rats (P<0.001), increased plasma homocysteine levels, reduced folic acid levels (P<0.001), diminished acetylcholine esterase activities in the rat hippocampus (P<0.001), and increased neurofibril ary tangles in the rat hippocampus (P=0.000). Results suggested that a large dose of levodopa could significantly decrease the learning and memory capacities, and disease acetylcholine esterase activities, and increase neurofibril ary tangles in hippocampus. Its mechanism possibly associated with the increased plasma concentration of homocysteine.
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@#ObjectiveTo observe the hindlimb motor end-plate morphology and activity of acetyl cholinesterase (AChE) in different types of muscle fiber end-plate areas after spinal cord injury and spinal cord reconstruction tubes inducing spinal cord regeneration. Methods43 adult Wistar rats were randomly divided into spinal cord transected group at T8 (Cx group), spinal cord transected with transplantation of reconstruction tubes group (CxTp group) and control group (Co group). 2 weeks, 4 weeks, 3 months, 6 months and 12 months after operation, gastrocnemius, soleus and extensor digitorum longus were dissected respectively, and stained with gold chloride to observe the motor end-plate and stained with Karnovsky-Roots to detect AChE. ResultsIn Cx group, the end-plates degenerated since 3 months after operation, while the AChE activity declined. In CxTp group, end-plate structure and morphology were relatively stable and there were no signs of degeneration. ConclusionAfter spinal cord injury, motor end-plates undergo degeneration. The spinal cord reconstruction tubes graft can prevent end-plate degeneration and benefit for AChE reactivation and motor end-plate morphological and structural plasticity towards the direction of neurological rehabilitation.
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PURPOSE: This study explored and evaluated the systemic complications resulting from the bite of Korean venomous snake, focussing on hematologic and neurologic features. METHODS: Medical records (demographic data, clinical measurements including laboratory results, severity score, and amount of antidote administration, and hospitalization course) of consecutive patients who presented with snakebites to two university teaching hospital during a 10-year period were retrospectively reviewed. Subgroup analysis was conducted for evaluations of anti-acetylcholine esterase administration in complicated victims. RESULTS: The 170 patients displayed occurrence rates of hematologic and neurologic complications of 12.9% and 20.6%, respectively. Among 22 patients with hematologic complications, isolated thrombocytopenia was evident in eight patients (36.4%), prothrombin time (PT)/activated partial thromboplastin time (aPTT) prolongation in 11 patients (50.0%), and both in three patients (13.6%). The mean time to recovery was 4.5+/-1.8 days for isolated thrombocytopenia, and 5.1+/-1.8 days for PT and aPTT prolongation. Hematologic complications could occur suddenly 1~4 days after hospitalization. Among 35 patients with neurologic complications, dizziness was evident in 16 patients (45.7%), and diplopia / blurred vision in 19 patients (54.3%). The mean time to recovery was 3.4+/-0.6 days in patients receiving anti-acetylcholine esterase and 6.9+/-1.8 days in those not receiving anti-acetylcholine esterase (p=0.00). CONCLUSION: Occurrence rates of hematologic and neurologic complications following venomous snake bite differed as compared to other studies conducted in Korea. Onset of hematologic complications can occur rapidly days after admittance. Anti-acetylcholine esterase administration may be effective in treating neurologic complications.
Subject(s)
Humans , Bites and Stings , Diplopia , Dizziness , Hospitalization , Hospitals, Teaching , Korea , Medical Records , Partial Thromboplastin Time , Prothrombin Time , Retrospective Studies , Snake Bites , Snakes , Thrombocytopenia , Venoms , Vision, OcularABSTRACT
@#Objective To explore the restoration of motor function and the expression of calcitonin gene-related peptide(CGRP)and acetylcholine esterase(AChE)in the anterior horn motoneurons after different types of spinal cord injury.Methods 60 adult female Wistar rats were randomly assigned to 3 groups:sham group,completely transection group and contusion group.Average combined scores(ACOS)were applied to assess the motor function at various time after the surgery.The content of AChE in the anterior horn of L2-L4 was detected with Karnovsky-Roots staining and the expression of CGRP was then determined with immunohistochemistry.Results The scores of ACOS were much higher in the contusion group than in the transection group at each time point examined.The content of both AChE and CGRP significantly decreased after either type of spinal cord injury.However,their activity gradually recovered to the normal level in the contusion group,but not in the transection group.Moreover,the changes of CGRP occurred earlier than those of AChE.Conclusion There is strong relationship between the motor function recovery and the functional state of anterior horn cells.CGRP or AChE may play an important role in the functional recovery of locomotion after spinal cord injury in rats.
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@#Objective To explore the degeneration of motor end plates (MEP) by observing the expression of calcitonin gene-relative peptide (CGRP) and acetylcholine esterase (AChE) in the MEP after different types of spinal cord injury. Methods 60 adult female Wistar rats were randomly assigned to 3 groups: sham group, completely transection group and contusion group. The content of AChE in the MEP was detected with Karnovsky-Roots staining and the expression of CGRP was then determined with immunohistochemistry. Results The content of both AChE and CGRP significantly decreased after either type of spinal cord injury. However, their activity gradually recovered to the normal level in the contusion group, but not in the transection group. Moreover, the changes of CGRP occurred earlier than those of AChE. Conclusion The motor end plate degenerates differently after different kinds of spinal cord injury in adult rat, CGRP and AChE are related to the degeneration of MEP.
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BACKGROUND: Alzheimer's disease (AD) is characterized by the pathology of amyloid plaques and tau-associated neurofibrillary tangles. Acetylcholine esterase (AChE) transforms the beta-amyloid monomer into an oligomer, and increases beta-amyloid aggregation in the brain. Increased beta-amyloid breaks the cytoskeleton of the brain by hyperphosphorylation of the tau protein. Previous studies support that AChE inhibitor has an inhibitory effect on toxicity of the beta-amyloid and phophorylated tau protein. The purpose of this study was to analyze the CSF beta-amyloid 1-42 (A beta 1-42) and phosphorylated tau protein in AD and determine their difference depending on whether AChE inhibitor was taken or not. METHODS: Subjects included 16 AD, 14 normal controls, and 15 disease controls. Nine of AD group had taken an AChE inhibitor while the remainder had not. The CSF A beta 1-42 and phosphorylated tau were measured by ELISA. RESULTS: The CSF A beta 1-42 levels were lower in AD patients than in other groups (p<0.01). We also found increased CSF A beta 1-42 levels in the AChE inhibitor users, compared with non-users. CONCLUSIONS: The level of CSF A beta 1-42 may have a diagnostic value in the patients with cognitive impairments. Also, we may expect the effect of AChE inhibitor on Alzheimer's pathology by measuring CSF A beta 1-42 levels. Therefore, the level of CSF A beta 1-42 may serve as a biological surrogate marker for AD treatment.
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Humans , Acetylcholine , Alzheimer Disease , Biomarkers , Brain , Cytoskeleton , Neurofibrillary Tangles , Plaque, Amyloid , tau ProteinsABSTRACT
Objective Detect the AChE content of RBC and plasma in the people with PNH.Invstigate the effect of the enzyme in GPI on PNH.Methods Detect the activity of AChE in RBC and plasma in 30 patients with PNH.Results (1)The activity of AChE of RBC in PNH patients was higher than controls,the difference between them having statistic significance,P
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Objective: In recent years,botulinum toxin type A(BTX-A) has been investigated for the treatment of pain.This experiment was to investigate the antinociceptive effect of BTX-A intraperitoneal injection on visceral pain of rats and its effect on intestinal AChE and SP expression.Methods: 72 male adult Wistar rats were divided into four groups: BTX-A(2U,4U,and 6U) or vehicle(2ml) was injected intraperitoneally in B,C,D and A group.6 Rats of every group were challenged with acetic acid intraperitoneal injection after 1,4 and 8 weeks respectively.After abdominal writhing behaviors were monitored,the intestinal samples were immunohistochemical stained for AChE and SP examination.Results: At the end of one week,writhing test scores of rats in group C and D were decreased significantly compared with group A(P