Glutathione S-Transferase, Acetylcholinesterase Inhibitory and Antibacterial Activities of Chemical Constituents of Barleria prionitis

2007 ◽  
Vol 62 (4) ◽  
pp. 580-586 ◽  
Author(s):  
Kalhari S. Kosmulalage ◽  
Shamsulhaq Zahid ◽  
Chibuike C. Udenigwe ◽  
Sarfraz Akhtar ◽  
Athar Ata ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Ethanolic Extract ◽  
Antibacterial Activities ◽  
Spectroscopic Studies ◽  
Sri Lankan ◽  
Glutathione S Transferase ◽  
Ache Inhibitory Activity ◽  
Phytochemical Studies ◽  
Derivatives Of

Phytochemical studies on the ethanolic extract of Barleria prionitis of Sri Lankan origin have resulted in the isolation of a new compound, balarenone (1), along with three known compounds, pipataline (2), lupeol (3) and 13,14-seco-stigmasta-5,14-diene-3-α-ol (4). The structures of 1 - 4 were elucidated with the aid of extensive NMR spectroscopic studies. Compounds 1 - 4 showed moderate inhibitory activity against glutathione S-transferase (GST) and acetylcholinesterase (AChE). Compounds 1, 2 and 4 also exhibited antibacterial activity against Bacillus cereus and Pseudomonas aeruginosa (25 μg/disk). Three different derivatives of compound (2), 7,8-epoxypipataline (5), 8- amino-7-hydroxypipataline (6) and 7,8-dibromopipataline (7) were synthesized to evaluate them for GST and AChE inhibitory activities. Household microwave radiations were used to synthesize compound (6). Among all tested compounds, 8-amino-7-hydroxypipataline (6) exhibited a significant AChE inhibitory activity with an IC50 value of 36.8 μM.

scholarly journals Minor Chemical Constituents of Caesalpinia Bonduc

2009 ◽  
Vol 4 (3) ◽  
pp. 1934578X0900400
Author(s):  
Athar Ata ◽  
Chibuike C. Udenigwe ◽  
Elikana M. Gale ◽  
Radhika Samarasekera
Keyword(s):  
Chemical Constituents ◽  
Ethanolic Extract ◽  
Antibacterial Activities ◽  
Spectroscopic Studies ◽  
Glutathione S Transferase ◽  
Isolated Structures

From the ethanolic extract of Caesalpinia bonduc, one new diterpene, neocaesalpin P (1) and six known diterpenoids, neocaesalpin H (2), cordylane A (3), caesalpinin B (4), bonducellpin E (5), caesalpinolide A (6), and 17-methylvouacapane-8(14),-9(11)-diene (7) were isolated. Structures of these compounds were determined from NMR spectroscopic studies. Compounds 1-7 exhibited modest antibacterial activities. All of these compounds were weakly active in glutathione S-transferase inhibition assays.

New Cycloartane-type Triterpenoids from Artocarpus nobilis

2007 ◽  
Vol 62 (2) ◽  
pp. 280-284 ◽  
Author(s):  
Shamsulhaq Zahid ◽  
Athar Ata ◽  
Radhika Samarasekera
Keyword(s):  
Sri Lanka ◽  
Inhibitory Activity ◽  
Ethanolic Extract ◽  
Spectroscopic Studies ◽  
Acetylcholinesterase Inhibitory Activity ◽  
New Compounds ◽  
Phytochemical Studies

Recent phytochemical studies on the ethanolic extract of Artocarpus nobilis, collected from Sri Lanka, have resulted in the isolation of two new cycloartane-type triterpenoids, artocarpuate A (1) and artocarpuate B (2). Structures of these new compounds were established with the aid of extensive NMR spectroscopic studies. Compounds 1 and 2 were found to exhibit weak acetylcholinesterase inhibitory activity.

Glutathione S-Transferase, Acetylcholinesterase Inhibitory and Antibacterial Activities of Chemical Constituents of Barleria prionitis.

ChemInform ◽  
2007 ◽  
Vol 38 (31) ◽  
Author(s):  
Kalhari S. Kosmulalage ◽  
Shamsulhaq Zahid ◽  
Chibuike C. Udenigwe ◽  
Sarfraz Akhtar ◽  
Athar Ata ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Antibacterial Activities ◽  
Glutathione S Transferase

Synthesis and Biological Evaluation of Acetylcholinesterase Inhibitor Macakurzin C and Its Derivatives

Synlett ◽  
2015 ◽  
Vol 26 (08) ◽  
pp. 1131-1134 ◽  
Author(s):  
Hyoungsu Kim ◽  
Seung-Hoon Baek ◽  
Hongjun Jang
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitor ◽  
Biological Evaluation ◽  
Hydroxyl Groups ◽  
Structural Requirements ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

The derivatives of macakurzin C containing a modified D ring and protected C(3)/C(5)-hydroxyl groups were synthesized and their in vitro AChE inhibitory activity and neurotoxicity were evaluated to identify the structural requirements for the activities. The results indicated that C(3)-benzyl-protected derivative has a more potent AChE inhibitory activity (IC50, 2.6 μM) and a less neurotoxicity (GI50, >100 μM) than synthetic macakurzin C (IC50, 9.1 μM; GI50, 16.6 μM).

scholarly journals Acetylcholinesterase Inhibitory Activity and Antioxidant Activity of Selected Medicinal Plant Extracts Used Against Cognitive Dysfunction and Memory Loss in Sri Lankan Traditional Medicine

2018 ◽  
Vol 6 (5) ◽  
pp. 16-25
Author(s):  
Anoja Priyadarshani Attanayake ◽  
Kamani Ayoma Perera Wijewardana Jayatilaka
Keyword(s):  
Antioxidant Activity ◽  
Medicinal Plant ◽  
Plant Extracts ◽  
Inhibitory Activity ◽  
Ricinus Communis ◽  
Centella Asiatica ◽  
Sri Lankan ◽  
Medicinal Plant Extracts ◽  
Ache Inhibitory Activity ◽  
Alzheimer’S Diseases

The objectives of the study were to determine the acetylcholinesterase (AChE) inhibitory activity and antioxidant activity in the selected Sri Lankan medicinal plants. AChE inhibitory activity of the selected medicinal plant extracts was determined using the Ellman’s method. The antioxidant activities were determined by four in vitro methods namely DPPH assay, FRAP assay, NO assay and TBA acid method.  The contents of total polyphenols and flavonoids were determined quantitatively.Out of the ten selected medicinal plant extracts Abrus precatorius, Centella asiatica, Strychnos nux-vomica and Ricinus communis showed IC50 values < 200 µg/mL for AChE inhibitory activity. A high antioxidant activity was shown in the extracts of Cardiosprmum halicacabum, Centella asiatica and  Ricinus communis in  the four selected antioxidant assays.  The total polyphenol content and total flavonoid content was in the range of 0.55-7.30 mg/g DW and 19.08±0.29-1283.08± 0.09 µg/gDW. The extracts of A. precatorius, C. asiatica, S. nux-vomica and R. communis are deserved to be as potent sources of AChE inhibitors as well as natural antioxidants. Considering the complex multifactorial etiology of Alzheimer's diseases, these plant extracts would be apt candidates for the development of novel pharmaceutical agents in the management of Alzheimer's diseases.  

scholarly journals In vitro Antibacterial Activities of Honey Bee Extracts against Bacterial Isolates of Wound Infections

2021 ◽  
pp. 20-25
Author(s):  
O. A. Ayodele ◽  
J. O. Aribisala ◽  
A. T. Oseni ◽  
M. K. Oladunmoye
Keyword(s):  
Antibacterial Activity ◽  
Honey Bee ◽  
Honey Bees ◽  
Inhibitory Activity ◽  
Ethanolic Extract ◽  
Antibacterial Activities ◽  
Diffusion Method ◽  
Wound Infections ◽  
Zones Of Inhibition

Microorganisms most especially bacteria, continue to develop resistance against antimicrobial agents; hence novel sources of antibiotics are urgently needed to reduce this problem. This study was carried out to investigate the antibacterial activities of ethanolic, chloroform and aqueous extracts of Apis mellifera (honey bee) on isolates of wound infections. The isolates used in this study were procured from University of Ilorin Teaching Hospital (UITH) and confirmed using morphological and biochemical tests. The isolates used include; Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pnuemoniae, Proteus mirabilis and Proteus vulgaris. Honey bees were collected from an apitherapist at Sunshine honey and agro foods, Akure, Ondo State Nigeria. The whole insect was used for in vitro antibacterial evaluation of the isolates using agar well diffusion method. Ethanolic extract of A. mellifera had the highest inhibitory activity with mean zones of inhibition ranging from 7.40 mm to 21.67 mm, chloroform extracts had moderate inhibitory activity ranging from 4.63 mm to 10.03 mm while the aqueous extract had the least activity with zones of inhibition ranging from 3.00 mm to 6.30 mm. However, no antibacterial activity was observed against P. aeruginosa for all the extracts. It is concluded that extracts of honey bees most especially the ethanolic extract have antibacterial activity and thus could be a potential antibacterial agent against isolates of wound infections.

scholarly journals Antioxidant Activity and Flavonoids Identification by LC-MS/MS Analysis in Leaf Extract from Trattinnickia rhoifolia Willd

2019 ◽  
Vol 8 (2) ◽  
pp. 13-34
Author(s):  
Lilian Marigo Magalhaes ◽  
Valeria Dornelles Gindri Sinhorin ◽  
Camila Cristina Pereira de Souza ◽  
Rogério de Campos Bicudo ◽  
Adilson Paulo Sinhorin
Keyword(s):  
Oxidative Stress ◽  
Antioxidant Capacity ◽  
Leaf Extract ◽  
Chemical Constituents ◽  
Ethanolic Extract ◽  
Glutathione S Transferase ◽  
Hypolipidemic Action ◽  
Protein Thiols ◽  
First Time

The objectives of this work were to evaluate the antioxidant and hepatoprotective activities in the oxidative stress model induced by paracetamol in male Swiss mice, to evaluate the hypoglycemic and hypolipidemic action and to identify flavonoids in the leaves ethanolic extract from Trattinnickia rhoifolia. By the LC-MS / MS method, eight flavonoids were identified in the hydromethanolic (HM) and ethyl acetate (EA) fractions, except for Amentoflavone, the flavonoids Apigenin, Canferol, Luteolin, Quercetin, Quercetin-3-β-d-glucoside, Rutin and Taxifoline were identified for the first time in this species. These fractions were evaluated for antioxidant capacity (DPPH— test) and their protective effect in vivo through the analysis of superoxide dismutase, catalase, glutathione-s-transferase, non-protein thiols, ascorbic acid, TBARS and carbonylated proteins. The data showed that EA has antioxidant capacity and superior oxidative stress repair in chemical and biological analyzes, besides hypoglycemic and hypolipidemic action. Thus, the present work contributes significantly to the literature, since it is the first study that identifies the chemical constituents and pharmacological properties of leaves extract from T. rhoifolia.

scholarly journals Bactericidal Effect and Anti-Inflammatory Activity of Cassia garettiana Heartwood Extract

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Sumalee Panthong ◽  
Arunporn Itharat ◽  
Suchada Naknarin ◽  
Pranporn Kuropakornpong ◽  
Buncha Ooraikul ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Chemical Constituents ◽  
Ethanolic Extract ◽  
Antibacterial Activities ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Inhibiting Effect ◽  
Anti Inflammatory ◽  
Time Kill

Natural products are used as alternative drugs in traditional medicine to treat infection and inflammation and relieve pain. Heartwood of Cassia garettiana Craib has been investigated as an ingredient in Thai traditional medicine for anti-HIV protease, but there is no report on its antibacterial and anti-inflammatory activities. The objectives of this study were to investigate the anti-inflammatory and antibacterial activities, time-kill profile, and main active constituents of an ethanolic extract of C. garettiana heartwood. The study followed the generally accepted experimental design. All tests were investigated in triplicate. The heartwood of C. garettiana was extracted by maceration with 95% EtOH. The antibacterial activity of the extract and its chemical constituents were determined by their MIC values using resazurin as an indicator. Time-kill profile was determined at 0, 2, 4, 6, 8, 10, 12, and 24 hrs and expressed as log CFU/mL. The anti-inflammatory activity of the extract and its chemical components was investigated by their inhibiting effect on IL-6 and TNF-α production by ELISA. The ethanolic extract was analyzed for its chemical constituents by HPLC technique. The ethanolic extract showed both dose- and time-dependent bactericidal effects against Staphylococcus aureus, methicillin-resistance Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Salmonella Typhi, Salmonella Typhimurium, Klebsiella pneumoniae, and Shigella dysenteriae with MIC values of 312.5, 312.5, 312.5, 1,250, 2,500, 625, 625, 2,500, and 625 μg/mL, respectively. It showed an inhibiting effect on IL-6 production at concentrations of 12.5 to 100 μg/mL. The main active chemical constituent of C. garettiana was piceatannol that showed antibacterial activity against all test bacteria except P. aeruginosa. C. garettiana showed a broad spectrum of antibacterial activity against both Gram-negative and Gram-positive bacteria. Piceatannol and resveratrol from the plant strongly inhibited IL-6 production. Based on these results, we concluded that the ethanolic extract of C. garettiana showed both an antibacterial activity and inhibition of IL-6. Piceatannol is the active constituent of the extract and showed anti-inflammatory and antibacterial activities against Gram-negative and Gram-positive bacteria.

scholarly journals Three New 2-(2-Phenylethyl)chromone Derivatives of Agarwood Originated from Gyrinops salicifolia

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 576 ◽  
Author(s):  
Wen-Hua Dong ◽  
Hao Wang ◽  
Feng-Juan Guo ◽  
Wen-Li Mei ◽  
Hui-Qin Chen ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Inhibitory Activity ◽  
Leukemia Cell ◽  
2D Nmr ◽  
Leukemia Cell Line ◽  
Chromone Derivatives ◽  
Ache Inhibitory Activity ◽  
2D Nmr Spectra ◽  
Derivatives Of

Two new 2-(2-phenylethyl)chromone derivatives (1–2), comprising 5,6,7,8-tetrahydro-2-(2-phenylethyl)chromone and benzylacetone moieties, together with one new 2-(2-phenylethenyl)chromone (3) were isolated from the ethyl acetate extraction of agarwood originated from Gyrinops salicifolia Ridl. All structures were unambiguously elucidated on the basis of 1D and 2D NMR spectra as well as by HRESIMS data. All isolated compounds were tested for acetylcholinesterase (AChE) inhibitory activity and cytotoxic activity against human myeloid leukemia cell line (K562). However, none of the compounds displayed AChE inhibitory activity at a concentration of 50 µg mL−1 or cytotoxic activity against K562 cell line.

NewTriterpenoidal Alkaloids from Buxus sempervirens

2002 ◽  
Vol 57 (1-2) ◽  
pp. 21-28 ◽  
Author(s):  
Athar Ata ◽  
Samina Naz ◽  
M. Iqbal Choudhary ◽  
Bilge Sener ◽  
Songul Turkoz ◽  
...  
Keyword(s):  
Natural Products ◽  
Pathogenic Bacteria ◽  
Lemna Minor ◽  
Ethanolic Extract ◽  
Spectroscopic Studies ◽  
Phytotoxic Activity ◽  
Turkish Origin ◽  
Buxus Sempervirens ◽  
Phytochemical Studies ◽  
First Time

Phytochemical studies on the ethanolic extract of the roots of Buxus sempervirens of Turkish origin have resulted in the isolation of two new triterpenoidal alkaloids, (+)-16α, 31- diacetylbuxadine (1), (-)-Nb-demethylcyclomikuranine (2) along with three known natural products, (-)-cyclomikuranine (3), (-)-cyclobuxophylline-K (4) and (+)-buxaquamarine (5) isolated for the first time from this species of genus Buxus. The structures of these new natural products were established on the basis of extensive spectroscopic studies. Compound 1 exhibited antibacterial activity against human pathogenic bacteria and weak phytotoxic activity against Lemna minor Linn.

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