scholarly journals Acetylcholinesterase Inhibitory Activity of Alkaloids Isolated from Stephania venosa

2016 ◽  
Vol 11 (12) ◽  
pp. 1934578X1601101 ◽  
Author(s):  
Sumet Kongkiatpaiboon ◽  
Nongnaphat Duangdee ◽  
Saisuree Prateeptongkum ◽  
Wanna Chaijaroenkul
Keyword(s):  
Inhibitory Activity ◽  
Ache Activity ◽  
Hplc Analysis ◽  
Inhibitory Effect ◽  
Inhibition Assay ◽  
Phytochemical Screening ◽  
Ache Inhibition ◽  
Ache Inhibitory Activity ◽  
Inhibitory Potential ◽  
Protoberberine Alkaloid

Stephania venosa (Blume) Spreng or “Sa-Bu-Leud” is a Thai medicinal plant used for treatment of cancer and diabetes, and as a blood-tonic and aphrodisiac. This plant contains alkaloids as its major components and has been of interest for its acetylcholinesterase (AChE) inhibitory activity. Phytochemical screening of S. venosa was made using HPLC analysis and showed the chemical variation between the same species from different provenances. Fractionation of S. venosa extract yielded three alkaloids, namely, dicentrine, crebanine, and tetrahydropalmatine. AChE inhibitory potential of the isolated alkaloids was evaluated using Ellman's AChE inhibition assay. Dicentrine, crebanine, and tetrahydropalmatine inhibited AChE activity with IC50 values of 93.5, 86.6, and 168.6 μg/mL, respectively. The AChE inhibitory activity of the tertiary protoberberine alkaloid, tetrahydropalmatine, was lower than that of the aporphine alkaloids, dicentrine and crebanine, whereas the quaternary protoberberine alkaloid, berberine, showed a higher AChE inhibitory effect than the others.

scholarly journals Inhibitory Activity of β-lactamases by Hydro-Ethanolic Extracts of Harungana madagascariensis, a Plant of the Ivorian Pharmacopoeia

2020 ◽  
pp. 157-162
Author(s):  
Toty Abalé Anatole ◽  
Aka Ayébé Edwige ◽  
Guédé Kipré Bertin ◽  
Konan K. Fernique ◽  
Adrien Jehaes ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Health Concern ◽  
Resistant Bacteria ◽  
Water Mixture ◽  
Phytochemical Screening ◽  
Public Health Concern ◽  
Ethanolic Extracts ◽  
New Antibiotics ◽  
Inhibitory Potential

Infection due to multi-resistant bacteria is a public health concern. Unfortunately, the prospect of developing new antibiotics seem not to be on the horizon. Faced with this impasse, medicinal plants could be an alternative for the development of new molecules. The aim of this study was to determine the inhibitory effect of H. madagascariensis extracts on β-lactamases. Extraction of bioactive compounds from trunk barks and leaves of the plant was done in an ethanol-water mixture (70:30). Anti-β-lactamase activity was evaluated by spectrophotometry after the removal of tannins and a phytochemical screening was used to identify the groups of compounds. Concentrations inhibiting 50% of enzyme activity were 0.005±0.001 mg/mL (CTX-M-15), 0.01±0.001 mg/mL (P99) and 0.027±0.009 mg/mL (NDM-1) for bark extracts and 0.704 mg/mL for leaves extracts. Phytochemical screening revealed the presence of flavonoids in bark extracts. The ethanolic extracts of the trunk bark exert a good inhibitory activity on CTX-M-15, P99 and NDM-1 β-lactamases and this activity could be attributed to the presence of the flavonoids. Further studies by bio-guided fractionation of the ethanolic extracts of the bark could yield fractions with high inhibitory potential of β-lactamases.

Effect of alkaloid extracted from Huperzia phlegmaria on cognitive deficits scopolamine-induced in mice

2020 ◽  
Vol 16 ◽  
Author(s):  
Dang Kim Thu ◽  
Dao Thi Vui ◽  
Nguyen Thi Ngoc Huyen ◽  
Nguyen Thi Thanh Binh ◽  
Nguyen Thi Huyen ◽  
...  
Keyword(s):  
Cognitive Impairment ◽  
Mouse Brain ◽  
Cognitive Deficits ◽  
Inhibitory Activity ◽  
Water Maze ◽  
Ache Activity ◽  
Y Maze ◽  
Ache Inhibitory Activity ◽  
Kinetic Inhibition ◽  
Brain Tissues

Background: Huperzia phlegmaria has been used for the treatment of neurological disorder. Alkaloids are main bioactive compounds found in Huperzia phlegmaria. We aimed to investigate the acetylcholinesterase (AChE) inhibitory activity in vitro of Huperzia phlegmaria alkaloid extract (HpAE) and protective effects on mice which were induced cognitive deficits by scopolamine. Methods: AChE inhibitory activity and kinetic inhibition mechanism was investigated by Ellman's assay. Mice were administrated orally HpAE (30 mg/kg and 60 mg/kg) for fourteen days, and injected scopolamine at a dose of 1 mg/kg intraperitoneally for four days to induce cognitive impairment. The Y-maze and the Morris water maze were used for evaluating the memory behaviors. Acetylcholine (ACh) levels and AChE activity were measured in brain tissue. Glutathione peroxidase (GPx), superoxide dismutase (SOD) activities, and malondialdehyde (MDA) groups were also evaluated in the mouse brain tissues. Results: Our data showed that HpAE had the strong AChE inhibitory activity with an IC50 value of 5.12 ± 0.48 μg/mL in a concentration-dependent manner. Kinetic inhibition analysis demonstrated that HpPAE inhibited AChE followed the mixed inhibition type with Ki (representing the affinity of the enzyme and inhibitor) was 4.37 ± 0.35 µg/mL. Scopolamine induced the cognitive impairment in Morris Water Maze and Y-maze test along with reduced brain levels of ACh and antioxidant enzyme and increased AChE activity in mouse brain tissues. Treatment with HpAE at both dose (30 mg/kg and 60 mg/kg) decreased the SCP-induced cognitive impairment in both behavioral tests along with decreased acetylcholinesterase activity and MDA level, and increased ACh level and antioxidant enzyme in mouse brain tissues. Conclusion: Our results suggested that the HpAE at both dose (30 mg/kg and 60 mg/kg) may be used for prevent and treatment of Alzheimer’s disease.

Synthesis of Novel Benzimidazole and Benzothiazole Derivatives Bearing a 1,2,3-triazole Ring System and their Acetylcholinesterase Inhibitory Activity

2017 ◽  
Vol 41 (1) ◽  
pp. 30-35 ◽  
Author(s):  
Laleh Faraji ◽  
Shiva Shahkarami ◽  
Hamid Nadri ◽  
Alireza Moradi ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Simulation ◽  
Triazole Ring ◽  
Copper Catalysts ◽  
Inhibitory Effect ◽  
Ring System ◽  
Benzothiazole Derivatives ◽  
Ache Inhibitory Activity ◽  
Group A

A series of 20 novel benzimidazole and benzothiazole derivatives linked to a 1,2,3-triazole ring system was synthesised, characterised and evaluated for in vitro acetylcholinesterase (AChE) inhibitory activity. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. Three different linkers were used to optimise the enzyme inhibitory effect. Out of the 20 compounds, 13 showed some AChE inhibition. The most potent compound, which showed 84% inhibition at 100 μM, contained a 1-(2-fluorobenzyl)-1,2,3-triazole linked to a benzimidazole group. A docking simulation study showed that the most active compound bound preferentially to the catalytic anionic subsite of the AChE enzyme.

An integrated strategy for rapid screening of multi-target lead compounds for the treatment of Alzheimer's disease from traditional Chinese medicines by UHPLC combined with high-throughput screening: A case study on Salviae Miltiorrhizae Radix et Rhizoma

2021 ◽  
Vol 17 ◽  
Author(s):  
Minmin Zhang ◽  
Siduo Zhou ◽  
Wei Liu ◽  
Huijiao Yan ◽  
Xiao Wang ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
High Throughput ◽  
Inhibitory Activity ◽  
High Throughput Screening ◽  
Hplc Analysis ◽  
Salviae Miltiorrhizae ◽  
Salviae Miltiorrhizae Radix ◽  
Ache Inhibitory Activity

Background: Salviae Miltiorrhizae Radix et Rhizoma (Red Sage root) is widely used in traditional Chinese medicine (TCM) for the treatment of Alzheimer’s disease (AD) with demonstrated curative effects, based on the concept of "one drug with multiple therapeutic targets," which appears to be a good strategy for AD treatment. Objective: This study aimed to develop of high-throughput screening (HTS) method for multi-therapeutic target components found in complex TCMs, which are active against AD, using Red Sage root as the case study. Method: Acetylcholinesterase (AChE) inhibitors (AChEIs) from Red Sage root extracts were pre-screened by ultrafiltration-HPLC (UF-HPLC) analysis, in which AChE was added to the extract and then ultrafiltered to remove non-binding compounds. Potential AChEIs were identified by HPLC analysis of compounds bound to AChE. A microplate-based HTS was then used to quantify the AChE inhibitory activity and antioxidant activity of the pre-screened compounds. Results: Pre-screening found ten potential inhibitors, which were identified by ESI-TOF/MS; six of these were purified by semi-preparative HPLC: Oleoyl neocryptotanshinone (1), Dihydrotanshinone Ⅰ (2), Cryptotanshinone (3), Tanshinone Ⅰ (4), Tanshinone ⅡA (5) and Miltirone (6). All six compounds had good AChE inhibitory activity and weak DPPH scavenging capacity. Conclusion: This study provides a platform and technology support for the rapid discovery of multi-target components, potentially active against AD, from complex TCMs and with strong potential for adaptation to the discovery of treatments for other diseases.

scholarly journals IN VITRO ANTI-ULCER ACTIVITY OF DIFFERENT EXTRACTS OF CISSUS QUADRANGULARIS

2021 ◽  
Vol 9 (04) ◽  
pp. 21-25
Author(s):  
Syed Ahad Hussain ◽  
◽  
Goutham Kumar Srigadi ◽  
Chamakuri Subba Rao ◽  
Syed Ahmedulla Hussaini ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Inhibitory Effect ◽  
Chloroform Extract ◽  
Total Phenolic ◽  
Inhibition Assay ◽  
Cissus Quadrangularis ◽  
Atpase Inhibition ◽  
Dose Dependent

Aim:The aim of this study was undertaken to assessin vitro H+-K+ ATPase inhibitory activity of different extracts of Cissus quadrangularis Linn. Materials and Methods: Phytochemical and Phyto-analytical studies like total phenolic compound and total flavonoid contents from extract were quantified and H+-K+ ATPase inhibition assay was performed in presence of different concentrations(10,20,50 and 100 μg/ml) of standard (omeprazole),chloroform and methanolic extract. Results:The extract has shown dose dependent significant (*P < 0.05) proton pump inhibitory activity in the goat gastric mucosal homogenate which was compared to standard Omeprazole. Conclusions: Hence, from this study we have concluded that methanolic extract of C.quadrangularis has more inhibitory effect than chloroform extract.

scholarly journals Inhibition of PGHS-1 and PGHS-2 by Triterpenoid Acids from Chaenomelis Fructus

2008 ◽  
Vol 3 (12) ◽  
pp. 1934578X0800301
Author(s):  
Eveline Reininger ◽  
Rudolf Bauer
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Hydroxyl Group ◽  
Prostaglandin H Synthase ◽  
Dried Fruits ◽  
Inhibitory Potential ◽  
Prostaglandin H

The dichloromethane extract of the dried fruits of Chaenomeles speciosa (Sweet) Nakai (Rosaceae) showed strong inhibitory activity against both prostaglandin-H-synthase isoenzymes [IC50 (PGHS-1) = 5.1 μg/mL; IC50 (PGHS-2) = 2.3 μg/mL]. The lipophilic portion of the extract was mainly responsible for the inhibitory effect. Several triterpenoid acids were isolated and identified as contributing to this inhibitory activity (oleanolic, pomolic, 3β-O-acetylursolic and 3β-O-acetylpomolic acids). Comparison of their inhibitory potential with their selectivity to PGHS-2 showed that 3β-O-acetylursolic acid had the highest potency in the inhibition of PGHS-1 and PGHS-2 enzymes, whilst pomolic and 3β-O-acetylpomolic acid, with a hydroxyl group at position 19α, showed selectivity for PGHS-2. The inhibitory effect of the extract seems to be the result of the activity of the mixture of these different triterpenoid acids.

scholarly journals Cholinesterase Inhibition Activity and Molecular Docking Study of Eugenol Derivatives

2021 ◽  
Vol 50 (4) ◽  
pp. 1037-1045
Author(s):  
Khairunisa Mohd Zamli ◽  
Asnuzilawati Asari ◽  
Kooi Yeong Khaw ◽  
Vikneswaran Murugaiyah ◽  
Mariya al-Rashida ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Simulation ◽  
Docking Study ◽  
Protein Docking ◽  
Cholinesterase Inhibition ◽  
Ache Inhibition ◽  
Molecular Docking Study ◽  
Ache Inhibitory Activity ◽  
Inhibition Property ◽  
Ellman’S Method

The study was conducted to explore the anticholinesterase inhibition property of eugenol derived molecules. Ten eugenol derivatives were synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) by Ellman’s method. Most of the tested derivatives showed higher inhibition on BChE than AChE, however, their overall inhibitory activity was weak. In contrast, three derivatives (compounds 3,6,9) showed higher and good AChE inhibitory activity of more than 50% inhibition at 10 μg/mL. Among them, compound 9bearing a ethyl substituent at para position of the benzoyl ring showed the most potent AChE inhibition, with IC50 of 5.64 μg/mL. Ligand-protein docking simulation was also performed for the most active derived molecules (compounds 3,6,9).

scholarly journals Kaempferol Rhamnosides from Geranium sibiricum as Aldose Reductase Inhibitors and Their Content by HPLC Analysis

Processes ◽  
2020 ◽  
Vol 8 (6) ◽  
pp. 694
Author(s):  
Norman G. Quilantang ◽  
Kyung Choi ◽  
Bog-Hieu Lee ◽  
Sanghyun Lee
Keyword(s):  
Solvent Extraction ◽  
Aldose Reductase ◽  
Inhibitory Activity ◽  
Hplc Analysis ◽  
Ethyl Acetate Fraction ◽  
Inhibitory Effect ◽  
Reductase Inhibitors ◽  
Potent Inhibition ◽  
Ic50 Value ◽  
Natural Therapy

The study aimed to assess the aldose reductase (AR) inhibition of selected Geranium species and determine the bioactive flavonoid constituents. Flavonoids are known to be good AR inhibitors. Among the species examined, G. sibiricum exhibited potent inhibition of AR (IC50 value, 2.4 µg/mL). Further examination of G. sibiricum, after solvent extraction and fractionation, revealed that the ethyl acetate fraction (IC50 value, 0.41 µg/mL) had a potent AR inhibitory effect. Kaempferol rhamnosides were the active compounds from this fraction. Moreover, G. sibiricum showed the highest content of kaempferol-7-O-rhamnoside and kaempferol-3,7-O-dirhamnoside among the samples examined with a concentration in the extracts of 28.1 and 2.2 mg/g, respectively. This study shows that G. sibiricum exhibits promising AR inhibitory activity, which can be explored further as a natural therapy for treating and managing complications associated with diabetes.

scholarly journals Phytochemical screening and in vitro evaluation of alpha amylase, alpha glucosidase and beta galactosidase inhibition by aqueous and organic Atractylis gummifera L. extracts

2018 ◽  
Vol 5 (3) ◽  
pp. 103-112 ◽  
Author(s):  
Khadija Bouabid ◽  
Fatima Lamchouri ◽  
Hamid Toufik ◽  
Karima Sayah ◽  
Yahia Cherrah ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Alpha Amylase ◽  
Phytochemical Screening ◽  
Phytochemical Study ◽  
Organic Extracts ◽  
Ic50 Values ◽  
Inhibitory Potential ◽  
Alpha Glucosidase ◽  
Beta Galactosidase

Diabetes is a chronic condition which is increasingly progressing throughout the world. To treat it, several methods are used, among which is medicinal plants that still have an unknown mechanism of action. The objective of this work is to evaluate the in vitro hypoglycemic effect of the extracts of the underground part of Atractylis gummifera, a member of Asteraceae used in traditional Moroccan medicine. A phytochemical study of the aqueous extracts (decocted, infused and macerated) and organic extracts (methanol, methanol macerate, chloroformic, ethyl acetate and petroleum ether), and a phytochemical screening of the different secondary metabolites was done. The antidiabetic power of the extracts of A. gummifera by testing the inhibitory activity of ?-amylase, ?-glucosidase and ?-galactosidase, which are enzymes responsible for the digestion of polysaccharides was determined. The extracts of A. gummifera are very rich in flavonoids and tannins, and are inhibitory to?-amylase and ?-glucosidase, mainly the macerate of methanol with IC50 values of 0.557 ± 0.013 and 0.743 ± 0.017 mg / mL respectively. Higher ?-galactosidase inhibitory potential than quercetin was observed for aqueous macerates and methanol with IC50 values of 2.23 ± 0.012 and 2.443 ± 0.071 mg / mL respectively. The extracts of A. gummifera possess a significant inhibitory activity of the alpha amylase and alpha glucosidase and beta-galactosidase enzymes, in particular the macerate of methanol followed by the aqueous macerate, among the eight extracts tested.

scholarly journals Comparison of Chemical Compositions of the Pepper EOs From Different Cultivars and Their AChE Inhibitory Activity

2020 ◽  
Vol 15 (11) ◽  
pp. 1934578X2097146
Author(s):  
Shu-Xia Chen ◽  
Kong Yang ◽  
Jia-Yao Xiang ◽  
Osafo Raymond Kwaku ◽  
Jia-Xin Han ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Inhibitory Activity ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Black Pepper ◽  
Gas Chromatography Mass Spectrometry ◽  
Chemical Compositions ◽  
Quality Marker ◽  
The World ◽  
Ache Inhibitory Activity

Pepper is one of the most popular spices over the world and is called the King of Spices. Its essential oils (EOs) could alleviate neuronal ailments due to the inhibitory effect against acetylcholinesterase (AChE). In this study, the chemical compositions of 26 EOs prepared from white and black pepper collecting from 6 different cultivars were analyzed by gas chromatography-mass spectrometry (GC-MS). A total of 133 compounds were identified in the white and black pepper EOs. Monoterpenes and sesquiterpenes were found to be riched in these EOs, of which α-pinene, β-pinene, sabinene, 3-carene, limonene, and ( E)- β-caryophyllene were the major constituents. Most of pepper EOs showed potential AChE inhibitory activity with half-maximal inhibitory concentration (IC50) values in the range of 0.5-182.5 µg/mL. Comparison of chemical constitutes of pepper EOs from different cultivars suggested that α-pinene, β-pinene, and 3-carene with an IC50 value of 3.2, 53.3, and 2.9 µg/mL, respectively, might be used as Quality-marker (Q-marker) of pepper oil in inhibiting AChE.

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