In vitro and in silico antioxidant and α-glucosidase inhibitory potential of compounds isolated from Garcinia gaudichaudii (original) (raw)
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Pharmacognosy Journal, 2017
Background: Diabetes mellitus become one of the biggest global health problems of the 21st century. Type 2 diabetes play role for the majority of cases of diabetes worldwide which is characterized by the increase of postprandial blood glucose level. Maintaining postprandial glucose level through inhibition of α-glucosidase is one of the essential strategies in the treatment of diabetes. Inhibitory effect of α-glucosidase was commonly used to identify active compounds potentially to treat diabetes. Natural resources have potency as antidiabetic that can be used in diabetes treatment. Objective: The objective of the study is to separate active fraction in the crude extract of Garcinia hombroniana leaves to facilitate obtaining a pure biologically active compound as the α-glucosidase inhibitor. Methods: Fractionation to separate active fraction was performed using column and thin layer chromatography methods while α-glucosidase inhibitory activity assay was performed in vitro using spectrophotometric methods at λ 400 nm. Results: Ethyl acetate and methanol extract of G. hombroniana yielded 14 and 12 fractions, respectively. Two fractions with the higher percent inhibition compared to other factions are fraction 8 from ethyl acetate extract (FEA8) and fraction 3 from methanol extract (FM3). The IC 50 values of FEA8, FM3 and acarbose are 16.370 μg/mL, 59.042 μg/mL, and 39.534 μg/mL respectively. Conclusion: Fraction 8 from ethyl acetate extract of G. hombroniana leaves (FEA8) was separated and known in this study as the most bioactive α-glucosidase inhibitor agent compared with another extract, fractions, and acarbose.
Pharmacognosy Journal, 2017
Introduction: Diabetes mellitus (DM) is one of the global health emergencies that characterized by high blood glucose levels (hyperglycemia). Type 2 DM is the most common type in diabetic populations. Inhibition of alphaglucosidase can ameliorate postprandial hyperglycemia that occurs in patients with type 2 DM. Adding antioxidants to the therapy of DM is intended to reduce complications caused by oxidative stress. Some species of Garcinia have been proven to inhibit alpha-glucosidase and have antioxidant activity, but there is no research on Garcinia fruticosa Lauterb. Therefore, the aims of this research were to determine the activity of Garcinia fruticosa Lauterb. stem bark in inhibiting alpha-glucosidase and as an antioxidant. Methods: In this research, the Garcinia fruticosa Lauterb. stem bark was dried, grinded, and extracted by multistage maceration using n-hexane, ethyl acetate, and methanol. Inhibition of alpha-glucosidase test has been done in vitro on concentrated extracts and measured by microplate reader at 400 nm. The antioxidant test has been done using DPPH scavenging method and was measured by microplate reader at 519 nm. Results: Ethyl acetate extract is the most active extract for both test. IC 50 values for inhibition of alpha-glucosidase test are 20.18 µg/mL that is more active than standard (acarbose) which has IC 50 value 141.55 µg/mL. Meanwhile, IC 50 value from an antioxidant test is 8.93 µg/mL that is not more active than standard (quercetin) which has IC 50 value 2.51 µg/mL. Conclusion: Phytochemical screening shows that the ethyl acetate extract contains alkaloids, flavonoids, glycosides, saponins, and tannins.
Biomedicines
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 Com...
Biomolecules
Approximately 400 Garcinia species are distributed around the world. Previous studies have reported the extracts from bark, seed, fruits, peels, leaves, and stems of Garcinia mangostana, G. xanthochymus, and G. cambogia that were used to treat adipogenesis, inflammation, obesity, cancer, cardiovascular diseases, and diabetes. Moreover, the hypoglycemic effects and underlined actions of different species such as G. kola, G. pedunculata, and G. prainiana have been elucidated. However, the anti-hyperglycemia of G. linii remains to be verified in this aspect. In this article, the published literature was collected and reviewed based on the medicinal characteristics of the species Garcinia, particularly in diabetic care to deliberate the known constituents from Garcinia and further focus on and isolate new compounds of G. linii (Taiwan distinctive species) on various hypoglycemic targets including α-amylase, α-glucosidase, 5′-adenosine monophosphate-activated protein kinase (AMPK), insul...
α-Glucosidase Inhibitory Xanthones from the Roots of Garcinia fusca
Chemistry & biodiversity, 2017
An ethyl acetate extract of the roots of Garcinia fusca produced two new compounds, fuscaxanthones J (1) and K (2), together with eight known xanthones (3-10). Their structures were determined using spectroscopic methods, mainly 1-D and 2-D NMR. α-Glucosidase inhibitory activity of the isolated compounds was evaluated and fuscaxanthone J (1) showed the most significant effect with IC50 value of 8.3 ± 1.8 μM (compared with acarbose, IC50 = 214.5 ± 2.3 μM). This article is protected by copyright. All rights reserved.
Molecules
α-Glucosidase plays a role in hydrolyzing complex carbohydrates into glucose, which is easily absorbed, causing postprandial hyperglycemia. Inhibition of α-glucosidase is therefore an ideal approach to preventing this condition. A novel polyprenylated benzoylphloroglucinol, which we named schomburgkianone I (1), was isolated from the fruit of Garcinia schomburgkiana, along with an already-reported compound, guttiferone K (2). The structures of the two compounds were determined using NMR and HRESIMS analysis, and comparisons were made with previous studies. Compounds 1 and 2 exhibited potent α-glucosidase inhibition (IC50s of 21.2 and 34.8 µM, respectively), outperforming the acarbose positive control. Compound 1 produced wide zones of inhibition against Staphylococcus aureus and Enterococcus faecium (of 21 and 20 mm, respectively), compared with the 19 and 20 mm zones of compound 2, at a concentration of 50 µg/mL. The MIC value of compound 1 against S. aureus was 13.32 µM. An in sil...
Plant Science Today
The objective of this investigation was to assess the antioxidant and antidiabetic abilities of Garcinia cowa Roxb., a Thai native plant that has a history of use in traditional medicine in several countries. To achieve this goal, different plant parts, such as the leaves, fruit rind, and stem bark, were subjected to extraction with hexane, ethyl acetate, and 70% ethanol using the maceration method. The Folin-Ciocalteu technique was used to quantify the extracts' total phenolic content (TPC). The antioxidant assays, including DPPH, ABTS, and FRAP, and antidiabetic properties through the alpha-amylase and alpha-glucosidase inhibitory capacities of different extracts from G. cowa were assessed. The results revealed that the stem bark extracted with ethyl acetate displayed the highest level of TPC at 153.68 mg GAE/100 g DW. Compared to the other extracts, the stem bark ethyl acetate extract demonstrated the highest antioxidant activity in DPPH, ABTS, and FRAP assays with values of ...
Asian Journal of Pharmaceutical and Clinical Research
Objective : Garcinia kydia Roxb. is aspecies of the genus Garcinia, is based chemotaxonomic has various bioactive compounds that have been isolated by a variety of pharmacological activities, one of the activities that are being developed that inhibition of α-glucosidase. However, α-glucosidase inhibitory activity in the extracts and fraction from leaves of the Garcinia kydia Roxb. has not been reported. In this study, seeks to evaluated of α-glucosidase inhibitory activity against extracts and fractions of potentially.Methods : The α-glucosidase inhibitory activity test, conducted by in-vitro using the enzymatic reaction is measured of quantity with a microplate reader and identify the compound from the active fraction with normal-phase thin layer chromatography.Results : The ethyl acetate and methanol extract have the potential to inhibit the α-glucosidase with the percent inhibition at a concentration of 500μg/mL of 83 and 59%, respectively. The active fraction of the eth...
Journal of Applied Horticulture
An investigation was undertaken to study the antioxidant activity of various solvent extracts of the fruit of Garcinia indica using FRAP assay and to separate the compounds in the potential extract through TLC, HPLC and analyse using GC-MS. The study revealed that methanol and ethyl acetate extracts showed a higher antioxidant value than the other extracts. The compounds present in the methanol extracts were separated by TLC, HPLC and analysed using GC-MS. The results of TLC revealed the separation of two different spots in case of phenols and a single spot in case of alkaloids. The eluted compounds, subjected to HPLC, separated into 8 peaks in case of phenolics and 8 peaks in case of alkaloids with varying retention time. The HPLC fractions were subjected to GC-MS to identify the compounds in comparison with the Wilcon-NIST library. The study is useful in identifying the bioactive compound for anticancer activity using cell lines.
Antioxidant property of secondary metabolites from Garcinia genus: A short review
Ecletica Quimica
Species from the Garcinia genus (Clusiaceae family) are used in the treatment of many diseases and metabolic disorders frequently associated with the oxidative stress. The characteristic metabolites found in this genus are xanthones and benzophenones, which have antioxidant properties, among relevant biological potentials. This review provides a specific vision about antioxidant activity of Garcinia species, reporting in vitro and in vivo assays, described from the last five years. The research about antioxidant properties of Garcinia species and their constituents can be directed in the development of new medicines and drugs.