scholarly journals Chemical Evidence for Potent Xanthine Oxidase Inhibitory Activity of Ethyl Acetate Extract of Citrus aurantium L. Dried Immature Fruits

Molecules ◽  
2016 ◽  
Vol 21 (3) ◽  
pp. 302 ◽  
Author(s):  
Kun Liu ◽  
Wei Wang ◽  
Bing-Hua Guo ◽  
Hua Gao ◽  
Yang Liu ◽  
...  
Author(s):  
Abdul Mun'im ◽  
Muhammad Ashar Munadhil ◽  
Nuraini Puspitasari ◽  
Azminah . ◽  
Arry Yanuar

ABSTRACTObjectives: To evaluate the angiotensin converting enzyme (ACE) inhibitory activity of melinjo (Gnetum gnemon) seed extract and to study moleculardocking of stilbene contained in melinjo seeds.Methods: Melinjo seed powders were extracted with n-hexane, dichloromethane, ethyl acetate, methanol, and water successively. The extracts wereevaluated ACE inhibitory activities using ACE kit-Wist and the phenolic content using Folin–Ciocalteu method. The extract demonstrated the highestACE inhibitory activity was subjected to liquid chromatography-mass spectrometry (LC-MS) to know its stilbene constituent. The stilbene constituentsin melinjo seed were performed molecular docking using AutoDock Vina, and ligand-receptor Interactions were processed using Ligand Scout.Results: The ethyl acetate extract demonstrated the highest ACE inhibition activity with inhibitory concentration 50% value of 9.77 × 10−8 μg/mLand the highest total phenolic content (575.9 mg gallic acid equivalent/g). Ultra-performance LC-MS analysis of ethyl acetate extract has detected theexistency of resveratrol, gnetin C, ε-viniferin, and gnemonoside A/B. These compounds displayed similar physiochemical properties to lisinopril (ACEinhibitor), as in silico molecular docking studies demonstrated that they fit into the lisinopril receptors.Conclusion: In vitro analysis ethyl acetate extract from melinjo seeds demonstrated the highest ACE inhibitory activity. Molecular docking analysisindicated that resveratrol dimers, gnetin C and gnemonoside A can be considered ACE inhibitor.Keywords: Angiotensin converting enzyme inhibitor, Gnetum gnemon, Melinjo, Total phenolic, Antihypertension, Molecular docking.


2019 ◽  
Vol 22 (6) ◽  
pp. 317-325
Author(s):  
La Ode Sumarlin ◽  
Anna Muawanah ◽  
Farhan Riza Afandi ◽  
Adawiah Adawiah

Indonesian local honey contains active compounds that have the potential as an antioxidant and anticancer, primarily as a laryngeal anticancer through the inhibition of HEp-2 cells. This study aims to determine the anticancer activity of several types of honey in Indonesia through the inhibition of HEp-2 cells. Samples used in the form of Trigona, Longan, Rambutan, and Kaliandra honey obtained from honey farmers in Sulawesi and Java, Indonesia. Honey samples extracted by using methanol, then liquids partition was carried out consecutively using n-hexane and ethyl acetate. The cytotoxicity test for HEp-2 cells was carried out using the MTT method (3- (4,5-dimethyl thiazol-2-il) -2,5-diphenyl tetrazolium bromide). The results showed that all honey samples were active against preventing HEp-2 cells with the highest inhibition activity from longan honey with ethyl acetate extract at 65.18% at 100 ppm. Longan honey has decreased HEp-2 cell inhibitory activity after fractionation. Indonesian local honey, namely trigona honey, kaliandra honey, rambutan honey, and longan honey, can be used as a supplementary supplement for patients with laryngeal cancer.


2010 ◽  
Vol 9 (1) ◽  
pp. 142-145 ◽  
Author(s):  
Hendig Winarno ◽  
Ermin Katrin W

Isolation and elucidation of benzophenone glucoside from ethyl acetate extract of Phaleria macrocarpa bark and its inhibitory activity test against leukemia L1210 cell line have been done. The Phaleria macrocarpa bark were macerated using n-hexane, ethyl acetate, and ethanol, respectively. The ethyl acetate extract was then chromatographed on silica gel column and gradiently eluted by n-hexane - ethyl acetate - ethanol with the composition from 20:1:0 until 0:0:1, gave eight fractions. Separation of fraction 6 using semipreparative HPLC on reverse phase column (Capcell Pak C-18 SG120, 15 mm I.D. x 250 mm) using methanol - water (40:60, 5 mL/min) gave a brown powder, with the melting point of 182.3 ºC. Spectroscopic analysis and comparison of its physico-chemical data, this compound was clarified as 2,4'-dihydroxy-4-methoxy-benzophenone-6-O-b-D-glucopyranoside (3). Inhibitory activity of its compound against leukemia L1210 cell line showed that this compound exhibited inhibitory activity with IC50 was 5.1mg/mL.     Keywords: Phaleria macrocarpa, 2,4'-dihydroxy-4-methoxybenzophenone-6-O-b-D-glucopyranoside, cytotoxic activity, leukemia L1210


2014 ◽  
Vol 1033-1034 ◽  
pp. 240-246
Author(s):  
Xue Jing Qiu ◽  
Ying Zi He ◽  
Xiao Wang

The Oxalis extract was obtained by soaking with ethanol, then mixed with distilled water and successively extracted using chloroform, ethyl acetate and n-butanol. The four different polar solvent (chloroform, ethyl acetate, n-butanol, aqueous) extracts were evaporated under reduced pressure to obtain four kinds of crude extractum. Antibacterial activity on Staphylococcus aureus, Escherichia coli, Albicans Saccharomyces and Pseudomonas aeruginosa of the four fractions were studied by minimal inhibitory concentration method (MIC). The results indicated that the chloroform extract and n-butanol extract from red Oxalis have no antimicrobial activity to the above 4 bacteria; the ethyl acetate extract showed significant inhibitory activities to the above 4 bacteria, the minimal inhibitory concentration (MIC) were 2560ug/ml, 1280ug/ml, 2560ug/ml, 2560ug/ml respectively; the aqueous extract have inhibitory activity to Escherichia coli and Albicans Saccharomyces, the minimal inhibitory concentration (MIC) were 2560ug/ml, 2560ug/ml respectively, but it has no antimicrobial effect on the other two kinds of bacteria. The chloroform extract and ethyl acetate extract from yellow Oxalis have no antimicrobial activity to the above 4 bacteria; the n-butanol extract has inhibitory activity to Escherichia coli, Albicans Saccharomyces and Pseudomonas aeruginosa, the minimal inhibitory concentration (MIC) were 5120ug/ml, 5120ug/ml, 5120ug/ml respectively, but it has no antimicrobial effect on Staphylococcus aureus; the aqueous extract have inhibitory activity to Escherichia coli and Albicans Saccharomyces, the minimal inhibitory concentration (MIC) were 2560ug/ml, 5120ug/ml respectively, but it has no antimicrobial effect on the other two kinds of bacteria.


Author(s):  
Bina Lohita Sari ◽  
Abdul Mun’im ◽  
Arry Yanuar ◽  
Rezi Riadhi

<p><strong>Objective: </strong><em>Terminalia catappa</em> L. (<em>T. catappa</em> L.) fruit has inhibitory activity on α-glucosidase, therefore, can be a potential natural source for the treatment of type II diabetes mellitus. Inhibitory activity of ethanol fruit extract with IC<sub>50</sub> 3.02 µg/ml was the strongest inhibition when compared with 54 medicinal plants used as an antidiabetic agent in Indonesia. This project was aimed to find the active compound from <em>T</em><em>.</em><em> catappa</em> L. fruit using molecular docking, identification ethyl acetate subfraction using TLC and GC-MC, determine <em>in vitro</em> test on α-glucosidase inhibitory activity from ethyl acetate extract and subfraction.</p><p><strong>Methods: </strong>Molecular docking using AutoDock 4.2 was performed to predict the binding modes of<strong> </strong>α-glucosidase enzyme from <em>Saccharomyces cereviciae</em> with 13 chemical constituents of <em>T. catappa</em>. α-Glucosidase enzyme was obtained from Protein Data Bank (PDB code: 3A4A). Acarbose, voglibose and miglitol were used as standards. Docking result determines the highest binding energy (ΔG) and inhibition constants (Ki) as an active compound. Visualization of amino acid residues around the active compound was identified with PyMOL and LigPlot. Screening of active compound was carried out by <em>T</em><em>.</em><em> catappa</em> L. fruit remaceration extraction use hexane and ethyl acetate. Ethyl acetate extract was separated on silica gel column chromatography using n-hexane, ethyl acetate and methanol sequentially based on polarity of each solvent. Identification of an active compound from ethyl acetate sub fractions using TLC and GC-MS method. The inhibitory activity of the active compound of α-glucosidase was determined with <em>in vitro</em> test using α-glucosidase enzyme.</p><p><strong>Results: </strong>The highest binding energy and inhibition constant is β–sitosterol with ΔG-10.61 kcal/mol and Ki 0.02 µM. The ligand was situated around of 18 amino acid residues. Ethyl acetate subfractions A, B and C showed that subfraction B contains similar spot characteristic and Rf value (0.42) with β-Sitosterol standard. Identification with GC-MS gave β–sitosterol acetate and sitostenone. Redocking process of β–sitosterol acetate and sitostenone showed ΔG-11.14 kcal/mol and-9.79 kcal/mol with Ki 0.01 μM and 0.07 μM respectively. <em>In vitro</em> test of acarbose, ethyl acetate extract and subfraction B gave IC<sub>50</sub> 17.52; 192.51 and 296.28 µg/ml.</p><p><strong>Conclusion: </strong>Three steroids that are β-sitosterol, β-sitosterol acetate and sitostenone were<strong> t</strong>he active compounds responsible for α-glucosidase inhibitory activity of <em>T</em><em>.</em><em> catappa </em>L. fruit. According to the <em>in vitro</em> test, ethyl acetate extract has stronger α-glucosidase inhibitory activity than ethyl acetate subfraction B.</p>


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