scholarly journals UJI IN VITRO DAN IN SILICO SENYAWA 5,7,2’,5’-TETRAHYDROXY FLAVAN-3-OL TERHADAP ENZIM ALPHA GLUCOSIDASE

2018 ◽  
Vol 5 (2) ◽  
pp. 279-283
Author(s):  
Frengki Frengki ◽  
Deddi Prima ◽  
Fatma Sri Wahyuni ◽  
Daan Khambri ◽  
Henny Vanda ◽  
...  

Several of Calophyllums genus have been searched and proven as medicinal plants and Calophyllum macrophyllum is one of its genus. We have been isolated a compound from ethyl acetate fraction of the stem-bark. The compound was flavan-3-ol (5,7,2’,5’-tetrahydroxy flavan-3-ol). This research aimed to determine inhibition antidiabetic activity and affinity of its compound on α-glycosidase enzyme. In vitro antidiabetic effect shown by IC50 9.10 µg/ml and docking by Arguslab 4.01 shown by ΔG -10,24 kkal/mol as in silico test. The inhibition activity of flavan-3-ol against the α-glucosidase enzyme that is very strong shows its promising potential as a candidate for antidiabetic drugs.

Author(s):  
Abdulhafiz Damilola Oso ◽  
Idris Bello ◽  
Yusuf Sa’idu ◽  
Onu Andrew

The aim of the current study is to evaluate the inhibition of α-glucosidase activity by stem bark extract of Albizia chevalieri. The activity of alpha glucosidase was assayed in vitro using 50 mM acetate buffer pH 6.0 (prepared from acetic acid and sodium acetate) and various concentration of maltose (0.5 mM to 10 mM). Five test tubes, labeled TA – TE, each containing 1.5 ml of acetate buffer, 0.5 ml of alpha glucosidase and 0.5 ml of a known concentration of plant extract and control tubes (CA – CE) were assessed for Alpha glucosidase activity. The results showed that hexane, ethyl acetate and methanol extracts inhibited α-glucosidase activity. The results further indicated that the extracts act by competitive inhibition with inhibition constant of 232 mg/ml, 157 mg/ml and 67 mg/ml for hexane, ethyl acetate and methanol extracts, respectively. The value for the inhibition constants shows that there is a strong binding of the enzyme to the inhibitor as the polarity of solvent increases. The inhibitory activity of Albizia chevalieri may be due one or more of the phytochemicals present in the extracts.


2020 ◽  
Vol 16 ◽  
Author(s):  
Mustapha M. Bouhenna ◽  
Chawki Bensouici ◽  
Latifa Khattabi ◽  
Farid Chebrouk ◽  
Nabil Mameri

Background: Schinus molle L. is a medicinal and aromatic plant widely used in folk medicine commonly found in Algeria and Mediterranean region. In the present work, we investigated the in vitro antioxidant, anti-cholinesterase, αglucosidase inhibitory and photoprotective potentials of the Schinus molle L. plant’s extract/fractions. The metabolite profile of Schinus molle L. was analyzed using RP-HPLC and GC-MS. Methods: Antioxidant activity was assessed using different tests. Anticholinesterase activity was investigated by quantifying the acetylcholinesterase and butyrylcholinesterase inhibitory activities. Antidiabetic activity was investigated by αglucosidase inhibition test, whereas photoprotective activity was evaluated by sun protection factor (SPF) using spectrophotometry UV-Vis. The extracts were then submitted to RP-HPLC–PDA and GC–MS analysis. Results: Ethyl acetate and buthanol fractions with high contents of total phenolics and flavonoids exhibited the strongest antioxidant activity. Ethyl acetate extract exhibited considerable enzyme inhibition potential on acetylcholinesterase, butyrylcholinesterase and α-glucosidase with percentages of inhibition of 99.08 ± 0.79 %, 100 % and 98.80 ± 0.18 % respectively. Furthermore, the ethyl acetate fraction showed high photoprotective activity with the sun protection factor (SPF) value = 38,26 ± 0.73. Three phenolic acids (gallic, tannic and vanillic acids) and five flavonoids (myricetin, apigenin, naringenin, rutin and quercetin) were identified with RP-HPLC–PDA. Conclusion: These findings suggest that Schinus molle L. may be useful in the development of an alternative agent for oxidative stress, Alzheimer’s disease, diabetes and could be used as a natural sunscreen in pharmaceutics or cosmetic formulations.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
L. A. Sulaimon ◽  
E. O. Anise ◽  
E. M. Obuotor ◽  
T. A. Samuel ◽  
A. I. Moshood ◽  
...  

Abstract Background Diabetes mellitus is a metabolic disorder of glucose metabolism and management of blood glucose level is the hallmark in the treatment of this disease. The present study investigated chemical composition, in vitro antioxidant and antidiabetic activity of different fractions of 80% methanol Piper guineense leaves extract. Materials and methods The crude methanolic extract of P. guineense was obtained following 80% methanol cold extraction and was successively partitioned with dichloromethane (DCM), ethyl acetate (EtOAc), n-butanol (nBuOH) and aqueous solvents to give four fractions. The chemical composition of the fractions from P. guineense was determined using gas chromatography coupled with mass spectrometry (GC-MS) and their potentials as antioxidant and anti-diabetes were evaluated. Results The percentage yields were 3.16, 2.22, 0.68 and 0.66% (w/w) in n-butanol, DCM, aqueous and ethyl acetate fractions of P. guineense methanolic extract, respectively. The GC-MS analyses identified a total of 71 and 34 phytochemicals in n-butanol and ethyl acetate fractions respectively. Tributyl acetylcitrate (10.95%) and phytol (9.11%) were the major components in the n-butanol fraction while ethyl piperonyl cyanoacetate (27.35%) and phytol (15.17%) were the major constituents in the ethyl acetate fraction. Ethyl acetate fraction had the highest ferric reducing antioxidant power with a value of 53.96 ± 0.40 mgAAE/g while n-butanol fraction possessed highest total antioxidant power (9.98 ± 0.15) followed by aqueous fraction (9.72 ± 0.02). The ethyl acetate and n-butanol fractions with IC50 value of 0.24 ± 0.07 and 0.83 ± 0.15 μg/mL respectively elicited significant inhibitory activities against α-glucosidase while only n-butanol fraction (IC50 = 0.33 ± 0.09 μg/ml) exhibited appreciable inhibition against α-amylase activity. However, none of the four fractions showed significant inhibitory activity towards dipeptidyl-peptidase-IV. Conclusion n-butanol and ethyl acetate fractions of 80% methanol P. guineense leaves extract can be a potential source of bioactive compounds of pharmacological importance in the management of diabetes.


Author(s):  
Sumithira G ◽  
Senthil Kumar Gp

Objective: In an attempt to explore herbal drug which may become useful in the prevention of diabetes and antioxidant potential by the ethanol extracts of Maytenus heyneana (MH) root belonging to the family Celastraceae and their different fractions were studied.Methods: Different fractionation was done using chloroform, ethyl acetate, and methanol on ethanolic extract of MH and preliminary phytochemical analysis was done by standard methods to identify the presence of important compounds. In vitro antioxidants activities were carried by 2,2-diphenyl- 2-picrylhydrazyl (DPPH) and 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) cation radical scavenging assays. For antidiabetic potential, α-amylase and α-glucosidase enzyme inhibitory studies were carried on different fractions.Results: Phytochemical studies show the presence of alkaloids, flavonoids, phenols, cardiac glycosides, and terpenoids in all fractionations; however, tannins and quinones were present in ethyl acetate fraction and saponins in methanolic fraction. For antioxidant activity, ethyl acetate fraction shows concentration of the sample causing 50% inhibition (IC50) values in 22.31 μg/ml and methanolic fraction shows in 12.82 μg/ml concentrations for DPPH and ABTS radical scavenging assay, respectively. In case of antidiabetic activity, methanolic fraction offered significant result in inhibitory action of α-glucosidase and also for α-amylase assay IC50 (5.28 and 3.14 μg/ml) than other fractions.Conclusion: From the results of our studies, it can be concluded that MH shows antidiabetic and antioxidant values and methanolic fraction of MH could be possessed potential constituents in the prevention of diabetes and antioxidant than other fractions. However, further studies are required to validate.


Biomedicines ◽  
2021 ◽  
Vol 9 (10) ◽  
pp. 1380
Author(s):  
Johanis Wairata ◽  
Edwin Risky Sukandar ◽  
Arif Fadlan ◽  
Adi Setyo Purnomo ◽  
Muhammad Taher ◽  
...  

This study aimed to isolate xanthones from Garcinia forbesii and evaluated their activity in vitro and in silico. The isolated compounds were evaluated for their antioxidant activity by DPPH, ABTS and FRAP methods. The antidiabetic activity was performed against α-glucosidase and α-amylase enzymes. The antiplasmodial activity was evaluated using Plasmodium falciparum strain 3D7 sensitive to chloroquine. Molecular docking analysis on the human lysosomal acid-alpha-glucosidase enzyme (5NN8) and P. falciparum lactate dehydrogenase enzyme (1CET) and prediction of ADMET for the active compound, were also studied. For the first time, lichexanthone (1), subelliptenone H (2), 12b-hydroxy-des-D-garcigerrin A (3), garciniaxanthone B (4) and garcigerin A (5) were isolated from the CH2Cl2 extract of the stem bark of G. forbesii. Four xanthones (Compounds 2–5) showed strong antioxidant activity. In vitro α-glucosidase test showed that Compounds 2 and 5 were more active than the others, while Compound 4 was the strongest against α-amylase enzymes. In vitro antiplasmodial evaluation revealed that Compounds 2 and 3 showed inhibitory activity on P. falciparum. Molecular docking studies confirmed in vitro activity. ADMET predictions suggested that Compounds 1–5 were potential candidates for oral drugs. The isolated 2–5 can be used as promising phytotherapy in antidiabetic and antiplasmodial treatment.


2021 ◽  
Vol 2021 ◽  
pp. 1-15
Author(s):  
Babita Aryal ◽  
Purushottam Niraula ◽  
Karan Khadayat ◽  
Bikash Adhikari ◽  
Dadhiram Khatri Chhetri ◽  
...  

Natural products have been the center of attraction ever since they were discovered. Among them, plant-based natural products were popular as analgesics, anti-inflammatory, antidiabetic, and cosmetics and possess widespread biotechnological applications. The use of plant products as cosmetics and therapeutics is deep-rooted in Nepalese society. Although there are few ethnobotanical studies conducted, extensive research of these valuable medicinal plants has not been a priority due to the limitation of technology and infrastructure. Here, we selected 4 traditionally used medicinal plants to examine their bioactive properties and their enzyme inhibition potential. α-Glucosidase and α-amylase inhibitory activities were investigated using an in vitro model followed up by antioxidant and antimicrobial activities. The present study shows that ethyl acetate fraction of Melastoma melabathrium (IC50 9.1 ± 0.3 µg/mL) and water fraction Acacia catechu (IC50 9.0 ± 0.6 µg/mL) exhibit strong α-glucosidase inhibition. Likewise, the highest α-amylase inhibition was shown by crude extracts of Ficus religiosa (IC50 29.2 ± 1.2 µg/mL) and ethyl acetate fractions of Shorea robusta (IC50 69.3 ± 1.1 µg/mL), and the highest radical scavenging activity was shown by F. religiosa with an IC50 67.4 ± 0.6 µg/mL. Furthermore, to identify the metabolites within the fractions, we employed high-resolution mass spectrometry (LC-HRMS) and annotated 17 known metabolites which justify our assumption on activity. Of 4 medicinal plants examined, ethyl acetate fraction of S. robusta, ethyl acetate fraction of M. melabathrium, and water or ethyl acetate fraction of A. catechu extracts illustrated the best activities. With our study, we set up a foundation that provides authentic evidence to the community for use of these traditional plants. The annotated metabolites in this study support earlier experimental evidence towards the inhibition of enzymes. Further study is necessary to explore the clinical efficacy of these secondary molecules, which might be alternatives for the treatment of diabetes and pathogens.


2021 ◽  
Vol 9 ◽  
Author(s):  
Muhammad Salihu Abdallah ◽  
Muskhazli Mustafa ◽  
Meenakshii A/P. Nallappan ◽  
Sangho Choi ◽  
Jin-Hyub Paik ◽  
...  

Gallic acid and catechin are the most abundant phenolic and flavonoid contents found in all plant extracts. The contents and the bioassay-guided fractionating substances of the Sclerocarya birrea (A. Rich) Hochst (Anacardiaceae) fraction played vital roles. The goals of the study were to determine the contents of some useful medicinal plants and the bioassay-guided fractionation substances of S. birrea fraction compounds capable of acting against Salmonella isolate using LC-MS/LC-HRMS (Dionex ultimate 3000 RS UPLC with Thermo Scientific Q Exactive Orbitrap Hybrid Tandem Mass Spectrometer). The Folin–Ciocalteu reagent procedure and flavonoid content determination were conducted spectrophotometrically. Bioassay-guided fractionation, chronological partitioning, and screening of the antibacterial action against Salmonella typhi were performed. The ethyl acetate fraction extracts of S. birrea stem (bark) extract were analyzed using LC-MS/LC-HRMS. The gallic acid content increased tremendously in Vachellia nilotica (L.) P.J.H. Hurter and Mabb (Fabaceae) pod extracts with curve fitting (R2 = 0.9958). Catechin content increase was significantly increased in S. birrea stem (bark) extracts followed by that of V. nilotica pod extracts with curve fitting (R2 = 0.9993); they were all significantly different in the Guiera senegalensis J.F. Gmel. and the Leptadenia lanceolata (Poir.) Goyder leaves extracts at p value <0.0001. Subsequently, 10 mg/ml of S. birrea stem (bark) ethyl acetate fraction extract was the MIC, where no MBC was recorded and susceptible to the positive control with the highest inhibition zone, followed by the ethyl acetate fraction extract at 10 mg/ml (9.7 ± 0.0) at Turkey’s p < 0.0001. Vidarabine is one of the novel compounds, specifically having antimicrobial actions, found in the S. birrea stem (bark). Reasonable amounts of phenolic and flavonoid contents determined the actions of the individual plant extract.


2014 ◽  
Vol 14 (1) ◽  
pp. 7-11 ◽  
Author(s):  
Puspa Dewi Narrij Lotulung ◽  
Tjandrawati Mozef ◽  
Chandra Risdian ◽  
Akhmad Darmawan

The antidiabetic activity test through a mechanism of inhibition of α-glucosidase enzyme was studied against ethanol, n-hexane, ethyl acetate and n-butanol fractions of ethanol extract of Artocarpus altilis (Parkinson) Fosberg (Moraceae) leaves and four flavonoid compounds isolated from ethyl acetate extracts of A. altilis. Ethyl acetate fraction has strongest antidiabetic activity compared to ethanol, n-hexane, and n-butanol fractions with IC50values5.98,6.79, 440.18and14.42μg/mL, respectively. Four flavonoid compounds (1-(2,4-dihydroxyphenyl)-3-[8-hydroxy-2-methyl-2-(4-methyl-3-pentenyl)-2H-1-benzopyran-5-yl]-1-propanone (AC-31), 2-geranyl-2',3,4,4'-tetrahydroxy dihydrochalcone (AC-51), 8-geranyl-4',5,7-trihydroxyflavone (AC-33) andcyclocommunol (AA-3), have been isolated from ethylacetate fraction. AC-31 was the strongest antidiabetic compound compared to AC-51, AC-33 and cyclocommunolwithIC50values are 15.73, 24.41,49.49,and72.20μg/mL. Kineticstudies of AC-31 using Lineweaver-Burk method showed that inhibition mechanism of enzymeα-glucosidase was anon-competitivetype.


2019 ◽  
Vol 5 (3) ◽  
pp. 257-267
Author(s):  
Taiwo O. Elufioye ◽  
Omolola A. Olaifa ◽  
Mojisola C. Cyril-Olutayo

Background: The leaves and stem bark of Anogeissus leiocarpa (DC.) Guill. & Pirr. (Combretaceae) are commonly included in recipes used for the management of sickle cell disease in western part of Nigeria. Objective: The present study was carried out to evaluate the potential of methanol extract and various fractions of A. leiocarpa leaves and stem bark to inhibit as well as reverse sodium metabisulphite induced polymerization of sickle cell haemoglobin. Method: The modified Emmel test was used to evaluate the inhibitory activity and the reversal effects of the extracts and fractions of both the leaves and the stem bark of A. leiocarpa in vitro. Results: Both the leaves and the stem bark extracts of A. leiocarpa were effective at inhibiting as well as reversing sodium metabisulphite induced polymerization of sickle cell haemoglobin, though the activity was higher in the leaves (94.52 ± 0.80% and 95.67 ± 0.67% respectively) when compared with the stem bark (51.79 ± 2.46 % and 50.45 ± 3.18 % respectively). The ethyl acetate fraction of both leaves and stem bark also gave good activities in both test methods with percentage reversal of 82.74 ± 1.82% and 67.63 ± 2.18% respectively. Conclusions: : A. leiocarpa extracts and ethyl acetate fractions exhibit good inhibition and reversal of sodium metabisulphite–induced polymerization of sickle cell haemoglobin thus justifying its inclusion in remedies used for the traditional management of sickle cell.


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