Triterpenoids from Galbanumofuygur medicine andtheir anticholinesterase activities / 药学学报

Eight triterpenes were isolated from the methanol extract of Galbanum by various chromatographic methods including silica gel, ODS opening column, recrystallization and semi-preparative HPLC. Their structures were determined by spectroscopic methods and physicochemical properties as 3β,19α,21α-trihydroxyl-12-en-28-oic acid (1), sumaresinolic acid (2), 3β,19α-dihydroxyl-12-en-28-oic acid (3), oleanolic acid (4), 3β,6β,19α-trihydroxyl-12-en-28-oic acid (5), 19α-hydroxy oleanonic acid (6), 6α-hydroxy oleanonic acid (7), and (11R,12R)-3α,6α-dihydroxy-epoxyolean-28α,13α-olide (8). Among them, compound 1 is a new compound, while compounds 2-8 were newly isolated from the Apiaceae family. The ability of compounds 1-8 to inhibit cholinesterase was determined with an improved Ellman method. Compound 1 showed strong inhibitory activity against butyrylcholinesterase. The molecular docking results indicated that Trp82, His438, Phe329 and Ala328 played an important role in the binding of compound 1 to butyrylcholinesterase.

In-vitro Assessment of Cholinesterase Inhibitory and Thrombolytic Activity of Six Available Citrus Fruits in Bangladesh: Relevant for Treating Neurodegenerative Disorder

Aim: Citrus fruits are well known for its medicinal and food value. Aim of this study is to investigate acetylcholinesterase ((AChE)) inhibitory activity, butyrylcholinesterase (BuChE) inhibitory activity, total phenolics, flavonoids, flavonols content and thrombolytic activities of crude methanol extracts of 6 citrus fruits (Citrus limon, Citrus aurantifollia, Citrus bergamia, Citrus maxima, Citrus sinensis and Citrus macroptera). Methods: The fruits were extracted by using methanol as solvent. Ellman’s colourimetric method was applied to determine both cholinesterase inhibitory activities, while folin-ciocalteau reagent (FCR) and aluminium chloride were used to quantify total phenolics, flavonoids, flavonol content of those fruits. Blood clot lysis method was applied for determining the thrombolytic activity of those fruits. Results: All citrus fruits contain a good amount of phenolics, flavonoids and flavonols. C. maxima found more prominent in containing phenolics and flavonols compare to other citrus fruits, with 414.06 ± 2.87 mg Gallic Acid Equivalent/gm and 12.94 ± 1.31 mg Catechin Equivalent/gm dried extract respectively. Citrus sinensis showed the highest content in flavonoids with 21.16± 1.37 mg Catechin 20 Equivalent /gm dried extract. Citrus fruits are also a quality source of cholinesterase inhibitors. All the examined citrus fruits were found capable of inhibiting both acetylcholinesterases (AChE) as well as butyrylcholinesterase (BuChE). C. bergamia was most effective in inhibiting AChE with IC50 of 27.18 µg/ml where C. macroptera was best in inhibiting BuChE (IC50 32.5 µg/ml). But none of the citrus fruits was found fit for thrombolytic activity. Conclusion: Citrus fruits are found the sound in inhibiting AChE and BuChE as well as containing Phenolics, flavonoids and flavonols. But they lack in their thrombolytic activity.

In vitro cholinesterase inhibitory and antioxidant effect of selected coniferous tree species

Objective: To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees (Abies bornmulleriana, Picea pungens, Juniperus communis, Cedrus libani, Taxus baccata, and Cupressus sempervirens var. horizantalis). Methods: Acetone (Ace), ethyl acetate (EtOAc), and ethanol (EtOH) extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at 100 μg/mL. Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and N,. N-dimethyl- p-phenylendiamine (DMPD) radical scavenging, metal-chelation capacity, ferric-(FRAP) and phosphomolibdenum-reducing antioxidant power (PRAP) assays. All of the assays were performed in ELISA microplate reader. Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically. Results: Among thirty-six extracts in total, the shoot-Ace extract of Cupressus sempervirens var. horizantalis exerted the highest inhibition against AChE [(54.84±2.51)%], while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE [(67.54±0.30)%]. The highest DPPH radical scavenging effect, FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata, whereas all the extracts showed a variable degree of scavenging effect against DPMD radical. The shoot-EtOAc extract of Cedrus libani had the highest metal-chelation capacity [(58.04±0.70)%]. The shoot extracts of Taxus baccata were determined to have the richest total phenol content, which may contribute to its marked antioxidant activity. Conclusions: The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties, which might be useful against Alzheimer's disease.

In vitro cholinesterase inhibitory and antioxidant effect of selected coniferous tree species

OBJECTIVE@#To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees (Abies bornmulleriana, Picea pungens, Juniperus communis, Cedrus libani, Taxus baccata, and Cupressus sempervirens var. horizantalis).@*METHODS@#Acetone (Ace), ethyl acetate (EtOAc), and ethanol (EtOH) extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at 100 μg/mL. Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and N,N-dimethyl-p-phenylendiamine (DMPD) radical scavenging, metal-chelation capacity, ferric-(FRAP) and phosphomolibdenum-reducing antioxidant power (PRAP) assays. All of the assays were performed in ELISA microplate reader. Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically.@*RESULTS@#Among thirty-six extracts in total, the shoot-Ace extract of Cupressus sempervirens var. horizantalis exerted the highest inhibition against AChE [(54.84±2.51)%], while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE [(67.54±0.30)%]. The highest DPPH radical scavenging effect, FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata, whereas all the extracts showed a variable degree of scavenging effect against DPMD radical. The shoot-EtOAc extract of Cedrus libani had the highest metal-chelation capacity [(58.04±0.70)%]. The shoot extracts of Taxus baccata were determined to have the richest total phenol content, which may contribute to its marked antioxidant activity.@*CONCLUSIONS@#The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties, which might be useful against Alzheimer's disease.

In vitro cholinesterase inhibitory and antioxidant effect of selected coniferous tree species

Objective: To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees (Abies bornmulleriana, Picea pungens, Juniperus communis, Cedrus libani, Taxus baccata, and Cupressus sempervirens var. horizantalis). Methods: Acetone (Ace), ethyl acetate (EtOAc), and ethanol (EtOH) extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at 100 μg/mL. Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and N,N-dimethyl-p-phenylendiamine (DMPD) radical scavenging, metal-chelation capacity, ferric-(FRAP) and phosphomolibdenum-reducing antioxidant power (PRAP) assays. All of the assays were performed in ELISA microplate reader. Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically. Results: Among thirty-six extracts in total, the shoot-Ace extract of Cupressus sempervirens var. horizantalis exerted the highest inhibition against AChE [(54.84±2.51)%], while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE [(67.54±0.30)%]. The highest DPPH radical scavenging effect, FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata, whereas all the extracts showed a variable degree of scavenging effect against DPMD radical. The shoot-EtOAc extract of Cedrus libani had the highest metal-chelation capacity [(58.04±0.70)%]. The shoot extracts of Taxus baccata were determined to have the richest total phenol content, which may contribute to its marked antioxidant activity. Conclusions: The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties, which might be useful against Alzheimer’s disease.

Acute toxicity and cholinesterase inhibition of the nematicide ethoprophos in larvae of gar Atractosteus tropicus (Semionotiformes: Lepisosteidae)

Biomarkers are a widely applied approach in environmental studies. Analyses of cholinesterase (ChE), glutathione S-transferase (GST) and lipid peroxidation (LPO) are biomarkers that can provide information regarding early effects of pollutants at different biochemical levels on an organism. The aim of this study was to evaluate the biomarker approach on a Costa Rican native and relevant species. For this, larvae of gar (Atractosteus tropicus) were exposed to the organophosphorus nematicide, ethoprophos. Acute (96hr) exposure was conducted with pesticide concentrations ranging from 0.1μg/L to 1 500μg/L. The 96hr LC50 calculated was 859.7μg/L. After exposure, three biomarkers (ChE, GST and LPO) were analyzed in fish that survived the acute test. The lowest observed effect concentration (LOEC) regarding ChE activity inhibition was 50μg/L. This concentration produced a significant inhibition (p<0.05) of the enzyme by 20%. The highest concentration tested without showing any effect on ChE activity and therefore considered as no observed effect concentration (NOEC) was 10μg/L. Ethoprophos concentration of 400μg/L caused a ChE inhibition by 79%. In this study, no significant variations (p>0.05) in GST activity and LPO were observed in A. tropicus larvae after exposure to ethoprophos.

El proceso de reproducción inducida de Atractosteus tropicus es útil para la acuicultura y la reintroducción en zonas donde las poblaciones silvestres se han reducido considerablemente. En larvas de esta especie se evaluó la toxicidad aguda, así como la respuesta de tres biomarcadores: actividad colinesterasa (ChE), actividad de Glutation S-transferasa (GST) y peroxidación de lípidos (LPO). Asimismo, se realizaron exposiciones agudas (96hr) a etoprofos (nematicida organofosforado), en donde se utilizaron concentraciones entre 0.1μg/L y 1 500μg/L del nematicida. La concentración letal 50 (LC50) calculada fue de 859.7μg/L; la máxima concentración sin efecto en los organismos (NOEC) 10μg/L y la concentración más baja en la cual se observó algún efecto (LOEC) 50μg/L. A esa concentración, el efecto observado fue una reducción significativa (p<0.05) en la actividad de la ChE. Una concetración de etoprofos de 400μg/L causó una inhibición del 79% en la actividad ChE. La actividad GST y la LPO no mostraron una respuesta significativa (p>0.05) luego de la exposición de los organismos a etoprofos.