Brevipsidone, a New Depsidone and Other α-Glucosidase Inhibitors from Garcinia Brevipedicellata (Clusiaceae) (original) (raw)

Natural Product Research A new depsidone derivative from the leaves of Garcinia polyantha

One new depsidone, polyanthadepsidone A (1), together with four known compounds were isolated from the dichloromethane extract of the leaves of Garcinia polyantha. The structures of all compounds were determined by comprehensive analyses of their 1D and 2D NMR and EI mass spectral data. Compounds 1, 2, 3, 4 and 5 exhibited suppressive effect on phagocytosis response upon activation with serum opsonized zymosan in the IC50 range of 4.5–23.80 μM, tested in vitro for oxidative burst studies of whole blood.

In vitro and in silico antioxidant and α-glucosidase inhibitory potential of compounds isolated from Garcinia gaudichaudii

Natural Product Research

Nine compounds including a new one, garcichaudiic acid (1), were isolated from the bark of G. gaudichaudii and their structures were characterized mainly by 1D and 2D NMR experiments. The antioxidant capacity of the isolated compounds was determined using DPPH radical scavenging assay and the anti-hyperglycemic activity was assessed by measuring the inhibitory effect against αglucosidase. Among them, compound 4 showed higher antioxidant activity than the positive control, ascorbic acid, while both compounds 1 and 7 exhibited more significant α-glucosidase inhibitory activity than the reference drug acarbose. Molecular docking analysis of the bioactive compounds was also performed to examine the binding modes and key interactions with the catalytic site.

Fractionation and α-glucosidase Inhibitory Activity of Fractions from Garcinia hombroniana Pierre Leaves Extracts

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.

Comparison of Inhibitory Activity Against the Α-Glucosidase Enzymes in the Extracts and Fractions from Leaves of the Garcinia Kydia Roxburgh

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...

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.

Alpha-Glucosidase Inhibitory Activity of Garcinia lateriflora Blume Leaves

Journal of Applied Pharmaceutical Science, 2017

Garcinia lateriflora Blume., that belongs to the genus Garcinia, is known to contain polyphenol compounds that are likely to inhibit alpha-glucosidase in the treatment of diabetes mellitus. Therefore, this study aimed to evaluate and acquire the most biologically active fraction from leaves of G. lateriflora in inhibiting alphaglucosidase. The separation of the active fraction was conducted using column chromatography and identified by thin layer chromatography. Alpha-glucosidase inhibitory activity test carried out in vitro using spectrophotometric method with p-nitrophenyl-α-D-glucopiranoside as the substrate. 17 and 12 fractions were obtained from ethyl acetate and methanol extracts, respectively. Fraction 13 (EA13) of ethyl acetate extract and fraction 10 (Me10) of methanol extract were showed the highest percent inhibition compared with the other fraction with IC50 values 8.96 µg/ml and 18.52 µg/ml, respectively. While the IC50 value for Acarbose is 39.53 µg/ml. Furthermore, fraction EA13 is the most active fraction in inhibiting alpha-glucosidase compared with the extract, other fractions, and Acarbose.

Xanthones inhibitors of α-glucosidase and glycation from Garcinia nobilis

Phytochemistry Letters, 2012

Plants of the genus Garcinia (family Clusiaceae), widely distributed in tropical Africa, Asia, New Caledonia, and Polynesia, have yielded an abundance of biologically active and structurally intriguing natural products (Ampofo and Waterman, 1986). Garcinia species are known to contain a wide variety of oxygenated and prenylated xanthones, as well as polyisoprenylated benzophenones such as the guttiferones (Nilar Nguyen et al., 2005). Xanthones show a wide range of biological and pharmacological properties such as antioxidant, antiinflammatory, antimicrobial, anticholinesterase and cytotoxic activities (

Identification of active compounds from lindur root plants (Bruguiera gymnorrhiza) as α-glucosidase inhibitors

IOP conference series, 2020

Lindur (Bruguiera gymnorrhiza) is a plant that contains bioactive sources for antioxidants and α-glucosidase inhibitors. The α-glucosidase inhibitors are inhibitors of the αglucosidase enzyme involved in digestion in the intestine. This study aimed to determine and select the potential inhibitory activity of the α-glucosidase enzyme from the crude extract of lindur by in vitro. This research was carried out through several studies that involved multilevel extraction. testing α-glucosidase inhibitors from crude extracts of lindur root. Fractionated from active extracts of lindur used thin layer chromatography (TLC) & preparative thin layer chromatography (PTLC). and combined compositions bioactive from the most active fraction. The highest yield was obtained from root ethanol extract which was 4.68. Ethanol extract of stem and root bark had an activity of α-glucosidase enzyme inhibitors calculated by IC50 values 171.31 ppm and 153.07 ppm. The fractionation results used preparative (PTLC) showed 5 fractions in crude ethanol root extract. Fraction 1 with Rf 0.15 had the most potential activity of αglucosidase enzyme inhibitors (161.05 ppm). Identification chemical composition used by Gas Chromatography Spectrometry (GC-MS) showed the composition contained in the fraction 1 of the root ethanol extract mostly (similar to> 90%) was hexadecanoic acid or palmitic acid and phenol.

Biphenyl and xanthone derivatives from the twigs of a Garcinia sp. (Clusiaceae)

Phytochemistry Letters, 2014

The genus Garcinia is a well known rich source of bioactive xanthones and benzophenones. Some species of this genus also produce flavonoids and biphenyls as minor constituents. In this study, two new biphenyls, doitungbiphenyls A (1) and B (2), along with two biphenyls, schomburgbiphenyl (3) and nigrolineabiphenyl B (4); and four xanthones, 1,3,6-trihydroxy-8-isoprenyl-7-methoxyxanthone (5), morusignin K (6), 1,5-dihydroxyxanthone (7), and 1,7-dihydroxyxanthone (8), were isolated from the acetone extract of the twigs of a Garcinia sp. Their structures were characterized extensively by 1D and 2D NMR spectroscopy and HR-EI-MS. The cytotoxicity of the two new biphenyls against the oral cavity cancer (KB) and the breast cancer (MCF7) cell lines was also evaluated.

Cholinesterase inhibitory triterpenoids from the bark of Garcinia hombroniana

Journal of Enzyme Inhibition and Medicinal Chemistry, 2014

Context: Garcinia hombroniana Pierre, known as manggis hutan in Malaysia is a rich source of xanthones and benzophenones. Objectives: This study was aimed to isolate and characterize potential cholinesterase inhibitors from the extracts of G. hombroniana bark and investigate their interactions with the enzymes. Materials and methods: The dichloromethane extract afforded five triterpenoids which were characterized by NMR and mass spectral techniques. Cholinesterase inhibitory assay and molecular docking were performed to get insight of the inhibitory activity and molecular interactions of the compounds. The compounds were also tested for their antioxidant capacity. Results: The isolated triterpenoids were identified as: 2-hydroxy-3-O-caffeoyltaraxar-14-en-28oic acid (1), taraxerol (2), taraxerone (3), betulin (4) and betulinic acid (5). Compound 1 was the most active dual inhibitor of both AChE and BChE. Compound 1 also showed good antioxidant activities. Conclusion: Compound 1 had dual and moderate inhibitory activity on AChE and BChE worthy for further investigations.