scholarly journals Phytochemical Constituents and Cholinesterase Inhibitory Activities of Millingtonia hortensis

2017 ◽  
Vol 15 (8) ◽  
pp. 589-597
Author(s):  
Warachate KHOBJAI ◽  
Orapit SUTHIVATTANAKUL ◽  
Somsiri PANUWATTANAWONG
Keyword(s):  
Ache Activity ◽  
Leaf Extract ◽  
Acetylcholinesterase Inhibitors ◽  
Gas Chromatography Mass Spectrometry ◽  
Enzyme Analysis ◽  
Leaf Extracts ◽  
Cholinesterase Inhibitory Activity ◽  
Phytochemical Constituents ◽  
Inhibitory Activities ◽  
Ellman’S Method

Acetylcholine (ACh) is an important neurotransmitter in the human brain and nervous system. Acetylcholinesterase inhibitors (AChEIs) are commonly used to improve cognitive function and exist in many plants, including Millingtonia hortensis. M. hortensis, a Thai medicinal plant, has been used as a smoke delivered bronchodilator. The aims of this study were to identify phytochemical constituents and evaluate the cholinesterase inhibitory activity of M. hortensis leaves and flower extracts. The phytochemical identifications were performed by gas chromatography-mass spectrometry. The inhibitory activities of acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) were measured through kinetic enzyme analysis by Ellman’s method. The results showed that all the extracts exhibited specific AChEIs less than 30 % inhibition. While only the chloroform leaf extract inhibited BChE below 30 % inhibitory activities at 5.0 mg/mL. The GC-MS fingerprints revealed 15 main phytochemical constituents in the crude extracts. Additionally, all plant extracts showed antioxidant activity. The leaf extracts were non-poisonous when AChE activity is decreased by 20 - 30 % compared to normal AChE activity.

Synthesis and bioactivity of novel C2-glycosyl triazole derivatives as acetylcholinesterase inhibitors

2017 ◽  
Vol 23 (3) ◽  
pp. 231-236 ◽  
Author(s):  
Long Yin ◽  
Lei Wang ◽  
Xiu-Jian Liu ◽  
Feng-Chang Cheng ◽  
Da-Hua Shi ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Sodium Hydroxide ◽  
Acetylcholinesterase Inhibitors ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity ◽  
Triazole Derivatives ◽  
Inhibitory Activities ◽  
Ellman’S Method

AbstractNew C2-glycosyl triazole derivatives 6a–l were synthesized by cyclization of glycosyl acylthiosemicarbazides 5 in refluxing 3 N sodium hydroxide aqueous solution. Substrates 5 were obtained by the reaction of glycosyl isothiocyanate 3 with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of compounds 6 were tested by Ellman’s method. Compounds that exhibited over 85% inhibition were subsequently evaluated for the IC50 values. Compound 6f possesses the best acetylcholinesterase-inhibition activity with IC50 of 1.46±0.25 μg/mL.

Synthesis and bioactivity of novel C2-glycosyl benzofuranylthiazoles derivatives as acetylcholinesterase inhibitors

2019 ◽  
Vol 43 (7-8) ◽  
pp. 257-261
Author(s):  
Lei Wang ◽  
Yu-Ran Wu ◽  
Shu-Ting Ren ◽  
Long Yin ◽  
You-Xian Wang ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Acetylcholinesterase Inhibitors ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity ◽  
Active Compounds ◽  
Inhibitory Activities ◽  
Ellman’S Method

A new series of C2-glycosyl benzofuranylthiazole derivatives was synthesised by the further cyclization of glycosyl thiourea and 2-(bromoacetyl)-benzofuran via Hantzsch’s method. The corresponding 2-(bromoacetyl)-benzofuran derivatives were obtained by the reaction from various salicylaldehydes, and the glycosyl thiourea was prepared through a series of steps from D-Glucosamine. The acetylcholinesterase-inhibitory activities of the products were tested by Ellman’s method. The most active compounds were subsequently evaluated for the 50% inhibitory concentration values. N-(1,3,4,6-tetra-O-benzyl-2-deoxy-β-D-glucopyranosyl)-4-(5-methoxy-benzofuran-2-yl)-1,3-thiazole-2-amine possessed the best acetylcholinesterase-inhibition activity with a 50% inhibitory concentration of 2.03 ± 0.26 μM.

REVIEW ON ETHNOMEDICINAL USES, PHYTOCHEMICAL CONSTITUENTS AND PHARMACOLOGICAL EVIDENCE ON LEAF EXTRACT OF PERSEA AMERICANA AND VERNONIA AMYGDALINA OF THE AFRICAN CONTINENT - A REVIEW

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (01) ◽  
pp. 7-24
Author(s):  
A Boadu ◽  
S. Singh ◽  
R Karpoormath ◽  
M. Nlooto ◽  
Keyword(s):  
Leaf Extract ◽  
English Language ◽  
Persea Americana ◽  
Cochrane Library ◽  
African Continent ◽  
Vernonia Amygdalina ◽  
Leaf Extracts ◽  
Phytochemical Constituents ◽  
Year 2000 ◽  
Ethnomedicinal Uses

People on the African continent frequently consume Persea americana and Vernonia amygdalina for food and medicinal purposes. The review is an effort to compile ethnomedicinal, phytochemical and pharmacological knowledge is the above two plants from the year 2000 till now. A search was carried out using a combination of several keywords : Persea americana, Vermonia amygdalina, traditional medicine, ethnomedicine, avocado, bitter leaf and integrated approaches. Published papers in English language were retrieved from the online bibliographical databases: Web of Science, PubMed, Google Scholar, Scopus and Cochrane library electronic databases. Findings from this review revealed that leaf extract of P. americana and V. amygdalina have been used in many local African communities for management of various diseases. Ethnomedicinal uses and pharmacological properties of leaf extracts of P. americana and V. amygdalina may justify polyherbal formulation involving the two plants in the treatment of diseases such as diabetes, hypertension and other diseases.

scholarly journals Acetylcholinesterase Inhibitors from Croton sylvaticus Ethyl Acetate Leaf Extract and their Mutagenic Effects

2013 ◽  
Vol 8 (6) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Mutalib A. Aderogba ◽  
Ashwell R. Ndhlala ◽  
Johannes Van Staden
Keyword(s):  
Ethyl Acetate ◽  
Plant Extracts ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Acetylcholinesterase Inhibitors ◽  
Ethyl Acetate Fraction ◽  
2D Nmr ◽  
Leaf Extracts ◽  
2D Nmr Spectroscopy ◽  
Mutagenic Effects

Croton sylvaticus is a medicinal plant widely employed in the management of inflammatory conditions, infections and oxidative stress related diseases such as insomnia, abdominal and internal inflammations. The activities demonstrated by the plant extracts support that its constituents possess the ability to reduce oxidative damage to body cells. Repeated column fractionation of the ethyl acetate fraction of a 20% aqueous methanol leaf extract using acetylcholinesterase (AChE) activity directed on Sephadex LH-20 afforded three compounds identified by mass spectrometry, and 1D and 2D NMR spectroscopy as: 2′-(3″,4″-dihydroxyphenyl)-ethyl-4-hydroxybenzoate (1), 3, 3′, 4′, 5, 7-pentahydroxyflavone (quercetin) (2), and 3, 4′, 5, 7-tetrahydroxyflavone (kaempferol) (3). These compounds are reported from the leaf extracts of C. sylvaticus for the first time and compound 1 is a new natural product. The microplate technique was used to determine the inhibitory effects of the plant extracts (crude and solvent fractions) and isolated compounds against AChE. The IC50 values of the compounds ranged from 60.7 to 415.0 μg/mL, with compound 2 having the best inhibitory activity; the IC50 values of the plant crude extract and solvent fractions ranged from 235.0 to 4695.0 μg/mL. The ethyl acetate fraction had the best inhibitory activity (IC50=235.0 μg/mL). The three compounds showed no mutagenic effects against Salmonella typhimurium tester strains TA98 and TA100. The activity demonstrated by these compounds suggests that they could be effective in the management of neurodegenerative disorders.

Synthesis, in vitro Acetylcholinesterase Inhibitory Activity Evaluation and Docking Investigation of Some Aromatic Chalcones

MedPharmRes ◽  
2017 ◽  
Vol 1 (1) ◽  
pp. 15-25
Author(s):  
Dao Tran ◽  
Son Tran ◽  
Vi Nguyen ◽  
Tri Le ◽  
Minh Thai ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Condensation Reaction ◽  
Acetylcholinesterase Inhibitors ◽  
Docking Studies ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Ellman’S Method

In this study, a total of twenty chalcones were synthesized via Claisen-Schmidt condensation reaction and evaluated for their in vitro acetylcholinesterase inhibitory activities using Ellman’s method. Molecular docking studies on acetylcholinesterase were performed to elucidate the interactions between these chalcone derivatives and acetylcholinesterase active site at the molecular level. From the series, six compounds (S1-5 and S17) exhibited strong acetylcholinesterase inhibitory activities with IC50 values below 100 µM compared to the parent unsubstituted chalcone. Compound S17 (4’-amino-2-chlorochalcone) showed the strongest acetylcholinesterase inhibitory activity in the investigated group with IC50 value of 36.10 µM. Molecular modeling studies were consistent with the results of in vitro acetylcholinesterase inhibitory activities, and chalcone S17 could be considered as a potential lead compound for the development of new acetylcholinesterase inhibitors.

Preliminary phytochemical screening, isolation and structural elucidation of chloroform leaf extracts of Maesa lanceolata

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Cardiac Glycosides ◽  
Leaf Extract ◽  
Chloroform Extract ◽  
Phytochemical Analysis ◽  
Spectroscopic Methods ◽  
Phytochemical Screening ◽  
Leaf Extracts ◽  
Standard Procedures ◽  
Phytochemical Constituents ◽  
First Time

The aim of this study was to screen the phytochemical constituents, isolate and elucidate the structure of chloroform extracts from the leaves of Maesa lanceolata. The qualitative phytochemical analysis of the leaf extract of Maesa lanceolata was done following standard procedures and the tests revealed the presence of cardiac glycosides and saponins in the crude extracts. The chloroform extract of the leaves of M. lanceolata led to the isolation of one compound, C1. Structure determination was accomplished by means of spectroscopic methods (IR, 13C and 1H NMR). According to the spectral data (IR, 1HNMR, 13CNMR and DEPT), probably Myrsenene was identified which is reported for the first time from M. lanceolata.

scholarly journals PHYTOCHEMICAL CONSTITUENTS OF THE LEAVES OF LEUCAENA LEUCOCEPHALA FROM MALAYSIA

2016 ◽  
Vol 8 (12) ◽  
pp. 174 ◽  
Author(s):  
Mohamed Zaky Zayed ◽  
Benedict Samling
Keyword(s):  
Mass Spectrometry ◽  
Leucaena Leucocephala ◽  
Mass Spectra ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Gas Chromatography Mass Spectrometry ◽  
Leaf Extracts ◽  
Anti Cancer ◽  
Phytochemical Constituents ◽  
Major Chemical

<p><strong>Objective: </strong>This study was conducted to identify the phytochemical constituents of <em>Leucaena leucocephala</em> leaf extracts using gas chromatography-mass spectrometry (GC-MS).</p><p><strong>Methods: </strong>Hexane, petroleum ether, chloroform, ethyl acetate and methanol leaves extract of <em>L. leucocephala</em> were analyzed using GC-MS, while the mass spectra of the compounds found in the extract were matched with the National Institute of Standards and Technology (NIST) library.</p><p><strong>Results: </strong>GC-MS analysis of <em>L. leucocephala</em> leaves revealed the presence of 30 compounds and the major chemical constituents were Squalene (41.02%), Phytol (33.80%), 3,7,11,15-Tetramethyl-2-hexadecen-1-ol (30.86%) and 3,7,11-Tridecatrienenitrile, 4,8,12-trimethyl (25.64%). Some of these compounds have been reported to possess various biological activities such as antioxidant, antimicrobial, hepatoprotective, antiparasitic, insecticide, nematicide, pesticide, anti coronary, antiarthritic, antiandrogenic, hypocholesterolemic, cancer preventive, anti-cancer, analgesic, anesthetic, allergenic and etc.</p><p><strong>Conclusion: </strong>The findings of this study indicating that<em> L.</em> <em>leucocephala</em> leaves possess various potent bioactive compounds and is recommended as a plant of phytopharmaceutical importance.</p>

scholarly journals Evaluation of phytochemical screening of Coleus forskohlii L. leaf extract

2018 ◽  
Vol 7 (5) ◽  
pp. 437-439
Author(s):  
Pavitra Dasari ◽  
◽  
Nirmala Baburao ◽  
Sudhakar Chekuri ◽  
Anupalli Roja Rani ◽  
...  
Keyword(s):  
Leaf Extract ◽  
Scientific Data ◽  
Western India ◽  
Coleus Forskohlii ◽  
Leaf Extracts ◽  
Chemical Test ◽  
Guinea Worm ◽  
Phytochemical Investigation ◽  
Lower Blood ◽  
Phytochemical Constituents

Coleus forskohlii L. plant Extract is derived from roots and leaves from Coleus forskohlii. Coleus is used in India and China folk medicines and is a traditional digestive remedy. Currently this plants levees and roots are extensively cultivated is Southern and western India. Forskohlii helps to lower blood pressure, dilates the blood vessels. Traditionally claimed to be constructive in the cure of cutaneous affections such as scabies, guinea worm, eczema and herpetic diseases. Conversely, there are no customary scientific reports for its antipsoriatic activity. Hence, the plant Coleus forskohlii has been chosen to establish scientific data for its traditional claim as anti-cancer. In the present study a chemical test performed against the, all the phytochemical constituents for their preliminary screening of each solvent extract of leaf like water, methanol, chloroform, ethyl acetate, and acetone. From the phytochemical investigation of the leaf extracts; the result is revealed the presence of carbohydrates, glycosides, tannins, flavonoids, triterpenoids, and lipids in all the solvent extracts. But phenols are more retain in methanolic leaf extract remain all the phytochemical constituents

scholarly journals Synthesis and bioactivity of novel C2-glycosyl oxadiazole derivatives as acetylcholinesterase inhibitors

2018 ◽  
Vol 24 (6) ◽  
pp. 333-338 ◽  
Author(s):  
Lei Wang ◽  
Yu-Ran Wu ◽  
Shu-Ting Ren ◽  
Long Yin ◽  
Xiu-Jian Liu ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Acetylcholinesterase Inhibitors ◽  
Inhibition Activity ◽  
Ache Inhibition ◽  
Active Compounds ◽  
Oxadiazole Derivatives ◽  
Inhibitory Activities ◽  
Ellman’S Method

Abstract A series of glycosyl-substituted 1,3,4-oxadiazoles were synthesized by cyclization of glycosyl-acylthiosemicarbazides via a base-catalyzed reaction. The starting glycosyl-acylthiosemicarbazide derivatives were obtained by the reaction of glycosyl isothiocyanate with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of the products were tested by Ellman’s method. The most active compounds were subsequently evaluated for the 50% inhibitory concentration (IC50) values. N-(1,3,4,6-tetra-O-benzyl-2-deoxy-β-D-glucopyranosyl)-5-(4-fluorophenyl)-1,3,4-oxadiazole-2-amine (6i) possesses the best AChE -inhibition activity with an IC50 of 1.61±0.34 μm.

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