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1.
Z Naturforsch C J Biosci ; 79(3-4): 47-60, 2024 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-38549398

RESUMO

Garcinia mangostana fruits are used traditionally for inflammatory skin conditions, including acne. In this study, an in silico approach was employed to predict the interactions of G. mangostana xanthones and benzophenones with three proteins involved in the pathogenicity of acne, namely the human JNK1, Cutibacterium acnes KAS III and exo-ß-1,4-mannosidase. Molecular docking analysis was performed using Autodock Vina. The highest docking scores and size-independent ligand efficiency values towards JNK1, C. acnes KAS III and exo-ß-1,4-mannosidase were obtained for garcinoxanthone T, gentisein/2,4,6,3',5'-pentahydroxybenzophenone and mangostanaxanthone VI, respectively. To the best of our knowledge, this is the first report of the potential of xanthones and benzophenones to interact with C. acnes KAS III. Molecular dynamics simulations using GROMACS indicated that the JNK1-garcinoxanthone T complex had the highest stability of all ligand-protein complexes, with a high number of hydrogen bonds predicted to form between this ligand and its target. Petra/Osiris/Molinspiration (POM) analysis was also conducted to determine pharmacophore sites and predict the molecular properties of ligands influencing ADMET. All ligands, except for mangostanaxanthone VI, showed good membrane permeability. Garcinoxanthone T, gentisein and 2,4,6,3',5'-pentahydroxybenzophenone were identified as the most promising compounds to explore further, including in experimental studies, for their anti-acne potential.


Assuntos
Acne Vulgar , Benzofenonas , Garcinia mangostana , Simulação de Acoplamento Molecular , Xantonas , Xantonas/química , Xantonas/farmacologia , Benzofenonas/química , Benzofenonas/farmacologia , Garcinia mangostana/química , Humanos , Acne Vulgar/tratamento farmacológico , Acne Vulgar/microbiologia , Simulação de Dinâmica Molecular , Proteína Quinase 8 Ativada por Mitógeno/metabolismo , Proteína Quinase 8 Ativada por Mitógeno/química , Simulação por Computador , Ligação de Hidrogênio
2.
Int J Biol Macromol ; 263(Pt 2): 130362, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38395287

RESUMO

In this study, anthocyanin from Garcinia mangostana shell extract (Mse) was used as pH indicator to prepare intelligent carboxymethyl cellulose (CMC) based composite films. The structure and properties of the CMC-based composite films were characterized and discussed in detail. Results showed that the CMC-based composite films with Mse had excellent mechanical, antibacterial and antioxidant abilities. Especially, the carboxymethyl cellulose/corn starch/Garcinia mangostana shell extract (CMC/Cst/Mse) composite film had best mechanical properties (20.62 MPa, 4.06 % EB), lowest water vapor permeability (1.80 × 10-12 g·cm/(cm2·s·Pa)), excellent ultraviolet (UV) blocking performance, and the best antibacterial and antioxidant abilities. The pH sensitivity of composite films which had Mse obviously changed with time when the fish freshness was monitored at 25 °C. Given the good pH sensitivity of the composite films, it had significant potential for application of intelligent packaging film as a food packaging material to indicate the freshness of fish.


Assuntos
Antioxidantes , Garcinia mangostana , Animais , Antioxidantes/química , Antocianinas/farmacologia , Carboximetilcelulose Sódica/química , Antibacterianos/farmacologia , Antibacterianos/química , Embalagem de Alimentos/métodos , Extratos Vegetais/farmacologia
3.
Int J Biol Macromol ; 257(Pt 2): 128696, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38072349

RESUMO

This study focuses on the preparation of mangosteen rind-derived nanocellulose via green ascorbic acid hydrolysis. Subsequently, milk protein-grafted nanocellulose particles were developed as a renewable Pickering emulsifier for water-oil stabilization. The stabilizing efficiency of modified nanocellulose (NC-S) at different caseinate (milk protein) concentrations (1.5, 3.0, and 4.0 % w/v) was tested in a water-in-oil emulsion (W/O ratio of 40:60). At a concentration 3.0 % w/v of caseinate (3.0NC-S), the emulsion exhibited a stronger network of adsorption between water, Pickering emulsifier, and oil. This resulted in reduced oil droplet flocculation, increased stability over a longer period, and favorable emulsifying properties, as depicted in the creaming index profile, oil droplet distribution, and rheology analysis. Since 3.0NC-S demonstrated the best colloidal stability, further focus will be placed on its microstructural properties, comparing them with those of mangosteen rind (MG), cellulose, and nanocellulose (NC-L). The XRD profile indicated that both NC-L and NC-S possessed a cellulose nanocrystal structure characterized as type I beta with a high crystallinity index above 60 %. Morphology investigation shown that the NC-L present in the spherical shape of particles with nanosized ranging at diameters of 11.27 ± 0.50 nm and length 11.76 ± 0.46 nm, while modified NC-S showed increase sized at 14.26 ± 4.60 nm and length 14.96 ± 4.94 nm. The increment of particle sizes from NC-L to NC-S indicated 2.82 × 10-15 mg/m2 of surface protein coverage by caseinate functional groups.


Assuntos
Garcinia mangostana , Nanopartículas , Emulsões/química , Caseínas/química , Celulose/química , Emulsificantes/química , Nanopartículas/química , Reologia , Água/química
4.
Zhongguo Zhong Yao Za Zhi ; 48(21): 5817-5821, 2023 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-38114177

RESUMO

Eight compounds were isolated from ethyl acetate fraction of 80% ethanol extract of the hulls of Garcinia mangostana by silica gel, Sephadex LH-20 column chromatography, as well as prep-HPLC methods. By HR-ESI-MS, MS, 1D and 2D NMR spectral analyses, the structures of the eight compounds were identified as 16-en mangostenone E(1), α-mangostin(2), 1,7-dihydroxy-2-(3-methy-lbut-2-enyl)-3-methoxyxanthone(3), cratoxyxanthone(4), 2,6-dimethoxy-para-benzoquinone(5), methyl orselinate(6), ficusol(7), and 4-(4-carboxy-2-methoxyphenoxy)-3,5-dimethoxybenzoic acid(8). Compound 1 was a new xanthone, and compound 4 was a xanthone dimer, compound 5 was a naphthoquinone. All compounds were isolated from this plant for the first time except compounds 2 and 3. Cytotoxic bioassay suggested that compounds 1, 2 and 4 possessed moderate cytotoxicity, suppressing HeLa cell line with IC_(50) va-lues of 24.3, 35.5 and 17.1 µmol·L~(-1), respectively. Compound 4 also could suppress K562 cells with an IC_(50) value of 39.8 µmol·L~(-1).


Assuntos
Antineoplásicos , Garcinia mangostana , Garcinia , Xantonas , Humanos , Garcinia mangostana/química , Células HeLa , Espectroscopia de Ressonância Magnética , Xantonas/farmacologia , Garcinia/química , Extratos Vegetais/química , Estrutura Molecular
5.
Molecules ; 28(19)2023 Oct 09.
Artigo em Inglês | MEDLINE | ID: mdl-37836835

RESUMO

α-Mangostin, a major xanthone found in mangosteen (Garcinia mangostana L., Family Clusiaceae) pericarp, has been shown to exhibit anticancer effects through multiple mechanisms of action. However, its effects on immune checkpoint programmed death ligand-1 (PD-L1) have not been studied. This study investigated the effects of mangosteen pericarp extract and its active compound α-mangostin on PD-L1 by in vitro and in silico analyses. HPLC analysis showed that α-mangostin contained about 30% w/w of crude ethanol extract of mangosteen pericarp. In vitro experiments in MDA-MB-231 triple-negative breast cancer cells showed that α-mangostin and the ethanol extract significantly inhibit PD-L1 expression when treated for 72 h with 10 µM or 10 µg/mL, respectively, and partially inhibit glycosylation of PD-L1 when compared to untreated controls. In silico analysis revealed that α-mangostin effectively binds inside PD-L1 dimer pockets and that the complex was stable throughout the 100 ns simulation, suggesting that α-mangostin stabilized the dimer form that could potentially lead to degradation of PD-L1. The ADMET prediction showed that α-mangostin is lipophilic and has high plasma protein binding, suggesting its greater distribution to tissues and its ability to penetrate adipose tissue such as breast cancer. These findings suggest that α-mangostin-rich mangosteen pericarp extract could potentially be applied as a functional ingredient for cancer chemoprevention.


Assuntos
Garcinia mangostana , Xantonas , Garcinia mangostana/química , Antígeno B7-H1 , Xantonas/farmacologia , Xantonas/química , Extratos Vegetais/farmacologia , Etanol
6.
Phytomedicine ; 120: 155069, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37722186

RESUMO

BACKGROUND: According to the WHO, 12 bacteria cause numerous human infections, including Enterobacteriaceae Klebsiella pneumoniae, and thus represent a public health problem. Microbial resistance is associated with biofilm formation; therefore, it is critical to know the biofilm-inducing potential of various compounds of everyday life. Likewise, the reversibility of biofilms and the modulation of persister cells are important for controlling microbial pathogens. In this work, we investigated the biofilm-inducing effects of xanthones from Garcinia mangostana on Klebsiella pneumoniae. Furthermore, we investigated the reversal effect of 3-methyl-2(5H)-furanone and the formation of persister cells induced by xanthones and their role in modulating the biofilm to the antibiotic gentamicin. METHODS: To analyze the biofilm-inducing role of xanthones from Garcinia mangostana, cultures of K. pneumoniae containing duodenal probe pieces were treated with 0.1-0.001 µM α- and γ-mangostin, and the biofilm levels were measured using spectrophotometry. To determine biofilm reversion, cultures treated with xanthones, or gentamicin were mixed with 3-methyl-2(5H)-furanone or N-butyryl-DL-homoserine lactone. The presence of K. pneumoniae persister cells was determined by applying the compounds to the mature biofilm, and the number of colony-forming units was counted. RESULTS: The xanthones α- and γ-mangostin increased K. pneumoniae biofilm production by 40% with duodenal probes. However, 3-methyl-2(5H)-furanone at 0.001 µΜ reversed biofilm formation by up to 60%. Moreover, adding the same to a culture treated with gentamicin reduced the biofilm by 80.5%. This effect was highlighted when 3-methyl-2(5H)-furanone was administered 6 h later than xanthones. At high concentrations of α-mangostin, persister K. pneumoniae cells in the biofilm were about 5 - 10 times more abundant than cells, whereas, with γ-mangostin, they were about 100 times more. CONCLUSION: Two xanthones, α- and γ-mangostin from G. mangostana, induced biofilm formation in K. pneumoniae and promoted persister cells. However, the biofilm formation was reversed by adding 3-methyl-2(5H)-furanone, and even this effect was achieved with gentamicin. In addition, this compound controlled the persister K. pneumoniae cells promoted by α-mangostin. Thus, synthetic, and natural biofilm-inducing compounds could harm human health. Therefore, avoiding these substances and looking for biofilm inhibitors would be a strategy to overcome microbial resistance and recover antibiotics that are no longer used.


Assuntos
Garcinia mangostana , Xantonas , Humanos , Lactonas , Antibacterianos/farmacologia , Biofilmes , Gentamicinas , Serina , Xantonas/farmacologia
7.
Ultrason Sonochem ; 99: 106571, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37690259

RESUMO

Response surface methodology was selected to explore the ultrasonic-assisted cellulase extraction conditions of Garcinia mangostana rind polysaccharides (GMRPs), and the optimum values of each condition were as follows: ratio of raw material to liquid of 1:50 g/mL, ultrasonic time of 40 min, enzyme concentration of 4 %, and ultrasonic power of 179 W. Based on the above conditions, the average extraction rate of GMRPs was 15.56 %. GMRPs were modified by carboxymethylation, and the relationship between the amount of chloroacetic acid and the substitution degree of carboxymethylated derivative was compared. Based on the results of single factor experiment, it was shown that the amount of chloroacetic acid significantly affected the degree of substitution of derivative products. The above research provides some valuable theoretical references for the preparation of GMRPs and its carboxymethylation products.


Assuntos
Celulase , Garcinia mangostana , Ultrassom , Polissacarídeos
8.
Fish Shellfish Immunol ; 140: 108982, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37536467

RESUMO

In this study, we investigated the potential immunostimulatory effects of mangosteen (Garcinia mangostana) peel extract on Macrobrachium rosenbergii, specifically in enhancing immunity and resistance against Lactococcus garvieae. We employed a dietary administration approach to assess the impact of different extract preparations from mangosteen peel, namely mangosteen peel powder (MPP), boiled mangosteen peel powder (MPB), and mangosteen peel extract (MPE). Following the administration of mangosteen peel extract, we evaluated growth performance, innate immune parameters, and disease resistance in the prawns. The results revealed a significant increase in total haemocyte count (THC), differential haemocyte count (DHC), phenoloxidase (PO) activity, respiratory bursts (RBs), as well as phagocytic activity and clearance efficiency against L. garvieae. Based on these findings, we suggest that mangosteen peel extract can be utilized as an immunostimulant for prawns through dietary administration, regulating immune responses and enhancing resistance against pathogens by modulating carbohydrate metabolism.


Assuntos
Garcinia mangostana , Palaemonidae , Animais , Pós , Resistência à Doença , Extratos Vegetais/farmacologia
9.
Fish Shellfish Immunol ; 141: 109019, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37634755

RESUMO

The study aimed to investigate the effects of injecting mangosteen husk hot-water extracts (MHE) on immune and physiological factors in Macrobrachium rosenbergii. Different doses of MHE (10, 20, and 40 µg prawn-1) were injected into the prawns, and various immune and physiological parameters were evaluated. The results revealed that higher doses of MHE (20 and 40 µg prawn-1) led to significant increases in immune parameters, improved phagocytic activity, and clearance efficiency. However, certain parameters, such as phenoloxidase activity per granulocyte, plasma glucose, and lactate levels were decreased after injection. Moreover, prawns injected with MHE and subjected to hypothermal stress exhibited changes in haemolymph dopamine and norepinephrine. Prawns injected with MHE for 7 days showed increased survival rates when challenged with Lactococcus garvieae. The relative survival percentages were 11.8%, 46.6%, and 47.1% for MHE doses of 10, 20, and 40 µg prawn-1 injection, respectively, indicating enhanced resistance to the pathogen. In conclusion, injecting MHE can act as an immunostimulant and physiological and neuroendocrine regulator for prawns, enhancing their resistance to L. garvieae.


Assuntos
Garcinia mangostana , Palaemonidae , Animais , Norepinefrina , Dopamina/farmacologia , Água
10.
Molecules ; 28(13)2023 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-37446849

RESUMO

ACE2 and Mpro in the pathology of SARS-CoV-2 show great potential in developing COVID-19 drugs as therapeutic targets, due to their roles as the "gate" of viral entry and viral reproduction. Of the many potential compounds for ACE2 and Mpro inhibition, α-mangostin is a promising candidate. Unfortunately, the potential of α-mangostin as a secondary metabolite with the anti-SARS-CoV-2 activity is hindered due to its low solubility in water. Other xanthone isolates, which also possess the xanthone core structure like α-mangostin, are predicted to be potential alternatives to α-mangostin in COVID-19 treatment, addressing the low drug-likeness of α-mangostin. This study aims to assess the potential of xanthone derivative compounds in the pericarp of mangosteen (Garcinia mangostana L.) through computational study. The study was conducted through screening activity using molecular docking study, drug-likeness prediction using Lipinski's rule of five filtration, pharmacokinetic and toxicity prediction to evaluate the safety profile, and molecular dynamic study to evaluate the stability of formed interactions. The research results showed that there were 11 compounds with high potential to inhibit ACE2 and 12 compounds to inhibit Mpro. However, only garcinone B, in addition to being indicated as active, also possesses a drug-likeness, pharmacokinetic, and toxicity profile that was suitable. The molecular dynamic study exhibited proper stability interaction between garcinone B with ACE2 and Mpro. Therefore, garcinone B, as a xanthone derivative isolate compound, has promising potential for further study as a COVID-19 treatment as an ACE2 and Mpro inhibitor.


Assuntos
COVID-19 , Garcinia mangostana , Xantonas , Humanos , Garcinia mangostana/química , Enzima de Conversão de Angiotensina 2 , Simulação de Acoplamento Molecular , Tratamento Farmacológico da COVID-19 , SARS-CoV-2 , Xantonas/farmacologia , Xantonas/uso terapêutico , Xantonas/química
11.
Molecules ; 28(13)2023 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-37446931

RESUMO

Nanoporous carbons were prepared via chemical and physical activation from mangosteen-peel-derived chars. The removal of atrazine was studied due to the bifunctionality of the N groups. Pseudo-first-order, pseudo-second-order, and intraparticle pore diffusion kinetic models were analyzed. Adsorption isotherms were also analyzed according to the Langmuir and Freundlich models. The obtained results were compared against two commercially activated carbons with comparable surface chemistry and porosimetry. The highest uptake was found for carbons with higher content of basic surface groups. The role of the oxygen-containing groups in the removal of atrazine was estimated experimentally using the surface density. The results were compared with the adsorption energy of atrazine theoretically estimated on pristine and functionalized graphene with different oxygen groups using periodic DFT methods. The energy of adsorption followed the same trend observed experimentally, namely the more basic the pH, the more favored the adsorption of atrazine. Micropores played an important role in the uptake of atrazine at low concentrations, but the presence of mesoporous was also required to inhibit the pore mass diffusion limitations. The present work contributes to the understanding of the interactions between triazine-based pollutants and the surface functional groups on nanoporous carbons in the liquid-solid interface.


Assuntos
Atrazina , Garcinia mangostana , Nanoporos , Atrazina/química , Adsorção , Carvão Vegetal/química , Cinética , Concentração de Íons de Hidrogênio
12.
Ultrason Sonochem ; 97: 106474, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37321072

RESUMO

According to response surface methodology (RSM), the extraction conditions of ultrasound-assisted extraction of polysaccharide from the rinds of Garcinia mangostana L. (GMRP) were optimized and determined. The optimal conditions obtained through optimization were: the liquid to material ratio was 40 mL/g, ultrasonic power was 288 W and extraction time was 65 min. The average extraction rate of GMRP was 14.73%. Ac - GMRP was obtained by acetylation of GMRP, and the antioxidant activities of the two polysaccharides were compared in vitro. The results indicated that the antioxidant capacity of polysaccharide obtained after acetylation was significantly improved compared with that of GMRP. In conclusion, chemical modification of polysaccharide is an effective measure to improve its properties to a certain extent. Meanwhile, it implies that GMRP has great research value and potential.


Assuntos
Antioxidantes , Garcinia mangostana , Antioxidantes/farmacologia , Antioxidantes/química , Polissacarídeos/farmacologia , Polissacarídeos/química
13.
PeerJ ; 11: e15329, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37187523

RESUMO

Garcinia mangostana L. (Mangosteen), a functional food, belongs to the Garcinaceae family and has various pharmacological effects, including anti-oxidative, anti-inflammatory, anticancer, antidiabetic, and neuroprotective effects. Mangosteen has abundant chemical constituents with powerful pharmacological effects. After searching scientific literature databases, including PubMed, Science Direct, Research Gate, Web of Science, VIP, Wanfang, and CNKI, we summarized the traditional applications, botanical features, chemical composition, and pharmacological effects of mangosteen. Further, we revealed the mechanism by which it improves health and treats disease. These findings provide a theoretical basis for mangosteen's future clinical use and will aid doctors and researchers who investigate the biological activity and functions of food.


Assuntos
Garcinia mangostana , Extratos Vegetais , Extratos Vegetais/farmacologia , Garcinia mangostana/química , Frutas/química , Alimento Funcional , Anti-Inflamatórios/farmacologia
14.
Int J Mol Sci ; 24(4)2023 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-36835343

RESUMO

Mangosteen peel, a waste produced during mangosteen processing, has been reported to be rich in xanthone and anthocyanin, both of which possess vital biological activities such as anti-cancer properties. The objectives of this study were to analyze various xanthones and anthocyanins in mangosteen peel by UPLC-MS/MS for the subsequent preparation of both xanthone and anthocyanin nanoemulsions to study their inhibition effects on liver cancer cells HepG2. Results showed that methanol was the optimal solvent for the extraction of xanthones and anthocyanins, with a total amount of 68,543.39 and 2909.57 µg/g, respectively. A total of seven xanthones, including garcinone C (513.06 µg/g), garcinone D (469.82 µg/g), γ-mangostin (11,100.72 µg/g), 8-desoxygartanin (1490.61 µg/g), gartanin (2398.96 µg/g), α-mangostin (51,062.21 µg/g) and ß-mangostin (1508.01 µg/g), as well as two anthocyanins including cyanidin-3-sophoroside (2889.95 µg/g) and cyanidin-3-glucoside (19.72 µg/g), were present in mangosteen peel. The xanthone nanoemulsion was prepared by mixing an appropriate portion of soybean oil, CITREM, Tween 80 and deionized water, while the anthocyanin nanoemulsion composed of soybean oil, ethanol, PEG400, lecithin, Tween 80, glycerol and deionized water was prepared as well. The mean particle size of the xanthone extract and nanoemulsion were, respectively, 22.1 and 14.0 nm as determined by DLS, while the zeta potential was -87.7 and -61.5 mV. Comparatively, xanthone nanoemulsion was more effective than xanthone extract in inhibiting the growth of HepG2 cells, with the IC50 being 5.78 µg/mL for the former and 6.23 µg/mL for the latter. However, the anthocyanin nanoemulsion failed to inhibit growth of HepG2 cells. Cell cycle analysis revealed that the proportion of the sub-G1 phase followed a dose-dependent increase, while that of the G0/G1 phase showed a dose-dependent decline for both xanthone extracts and nanoemulsions, with the cell cycle being possibly arrested at the S phase. The proportion of late apoptosis cells also followed a dose-dependent rise for both xanthone extracts and nanoemulsions, with the latter resulting in a much higher proportion at the same dose. Similarly, the activities of caspase-3, caspase-8 and caspase-9 followed a dose-dependent increase for both xanthone extracts and nanoemulsions, with the latter exhibiting a higher activity at the same dose. Collectively, xanthone nanoemulsion was more effective than xanthone extract in inhibiting the growth of HepG2 cells. Further research is needed to study the anti-tumor effect in vivo.


Assuntos
Garcinia mangostana , Neoplasias Hepáticas , Xantonas , Humanos , Antocianinas , Espectrometria de Massas em Tandem , Óleo de Soja , Cromatografia Líquida , Polissorbatos , Xantonas/farmacologia , Linhagem Celular Tumoral , Extratos Vegetais/farmacologia , Água
15.
Pharm Biol ; 61(1): 241-248, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36655319

RESUMO

CONTEXT: α-Mangosteen (α-MG) attenuates insulin resistance (IR). However, it is still unknown whether α-MG could alleviate hepatic manifestations in IR rats. OBJECTIVE: To investigate the effect of α-MG on alleviating hepatic manifestations in IR rats through AMP-activated protein kinase (AMPK) and sterol-regulatory element-binding protein-1 (SREBP-1) pathway. MATERIALS AND METHODS: IR was induced by exposing male Sprague-Dawley rats (180-200 g) to high-fat/high-glucose diet and low-dose injection of streptozotocin (HF/HG/STZ), then treated with α-MG at a dose of 100 or 200 mg/kg/day for 8 weeks. At the end of the study (11 weeks), serum and liver were harvested for biochemical analysis, and the activity of AMPK, SREBP-1c, acetyl-CoA carboxylase (ACC), tumor necrosis factor (TNF)-α, interleukin (IL)-1ß, IL-6, insulin receptor substrate (IRS)-1, Bax and liver histopathology were analyzed. RESULTS: α-MG at both doses significantly lowered ALT, AST, triglyceride, and cholesterol total by 16.5, 15.7, 38, and 36%, respectively. These beneficial effects of α-MG are associated with the downregulation of the IR-induced inflammation in the liver. Furthermore, α-MG, at both doses, activated AMPK by 24-29 times and reduced SREBP-1c by 44-50% as well as ACC expression by 19-31% similar to metformin. All treatment groups showed liver histopathology improvement regarding fat deposition in the liver. CONCLUSIONS: Based on the findings demonstrated, α-MG protected against HF/HG/STZ-induced hepatic manifestations of the IR rats, at least in part via the modulation of the AMPK/SREBP-1c/ACC pathway and it could be a potential drug candidate to prevent IR-induced hepatic manifestations.


Assuntos
Fígado Gorduroso , Garcinia mangostana , Resistência à Insulina , Ratos , Masculino , Animais , Proteína de Ligação a Elemento Regulador de Esterol 1/metabolismo , Proteína de Ligação a Elemento Regulador de Esterol 1/farmacologia , Garcinia mangostana/metabolismo , Estreptozocina/farmacologia , Proteínas Quinases Ativadas por AMP/metabolismo , Glucose/metabolismo , Ratos Sprague-Dawley , Fígado , Dieta Hiperlipídica/efeitos adversos
16.
J Nat Prod ; 86(1): 24-33, 2023 01 27.
Artigo em Inglês | MEDLINE | ID: mdl-36634312

RESUMO

Hyperuricemia is the result of overproduction and/or underexcretion of uric acid, and it is a well-known risk factor for gout, hypertension, and diabetes. However, available drugs for hyperuricemia in the clinic are limited. Recently, a lot of research has been conducted in order to discover new uric acid-lowering agents from plants and foods. We found that the extracts from the pericarp of mangosteen reduced urate. Bioactivity-guided study showed that α-mangostin was the principal constituent. Herein, we reported for the first time the hypouricemic activities and underling mechanism of α-mangostin. The α-mangostin dose- and time-dependently decreased the levels of serum urate in hyperuricemic mice and markedly increased the clearance of urate in hyperuricemic rats, exhibiting a promotion of urate excretion in the kidney. Further evidence showed that α-mangostin significantly decreased the protein levels of GLUT9 in the kidneys. The change in the expression of URAT1 was not observed. Moreover, α-mangostin did not inhibit the activities of xanthine oxidoreductase and uricase in vitro or in vivo. Taken together, these findings suggest that α-mangostin has potential to be developed as a new anti-hyperuricemic agent with promoting uric acid excretion.


Assuntos
Garcinia mangostana , Hiperuricemia , Ratos , Camundongos , Animais , Hiperuricemia/tratamento farmacológico , Hiperuricemia/metabolismo , Ácido Úrico/metabolismo , Xantina Oxidase , Rim/metabolismo
17.
Pharmacol Res ; 188: 106630, 2023 02.
Artigo em Inglês | MEDLINE | ID: mdl-36581166

RESUMO

Mangosteen (Garcinia mangostana L.), also known as the "queen of fruits", is a tropical fruit of the Clusiacea family. While native to Southeast Asian countries, such as Thailand, Indonesia, Malaysia, Myanmar, Sri Lanka, India, and the Philippines, the fruit has gained popularity in the United States due to its health-promoting attributes. In traditional medicine, mangosteen has been used to treat a variety of illnesses, ranging from dysentery to wound healing. Mangosteen has been shown to exhibit numerous biological and pharmacological activities, such as antioxidant, anti-inflammatory, antibacterial, antifungal, antimalarial, antidiabetic, and anticancer properties. Disease-preventative and therapeutic properties of mangosteen have been ascribed to secondary metabolites called xanthones, present in several parts of the tree, including the pericarp, fruit rind, peel, stem bark, root bark, and leaf. Of the 68 mangosteen xanthones identified so far, the most widely-studied are α-mangostin and γ-mangostin. Emerging studies have found that mangosteen constituents and phytochemicals exert encouraging antineoplastic effects against a myriad of human malignancies. While there are a growing number of individual research papers on the anticancer properties of mangosteen, a complete and critical evaluation of published experimental findings has not been accomplished. Accordingly, the objective of this work is to present an in-depth analysis of the cancer preventive and anticancer potential of mangosteen constituents, with a special emphasis on the associated cellular and molecular mechanisms. Moreover, the bioavailability, pharmacokinetics, and safety of mangosteen-derived agents together with current challenges and future research avenues are also discussed.


Assuntos
Garcinia mangostana , Xantonas , Humanos , Garcinia mangostana/química , Garcinia mangostana/metabolismo , Xantonas/farmacologia , Xantonas/uso terapêutico , Disponibilidade Biológica , Frutas/química , Extratos Vegetais/farmacologia
18.
Molecules ; 27(24)2022 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-36557908

RESUMO

Xanthones are significant bioactive compounds and secondary metabolites in mangosteen pericarps. A xanthone is a phenolic compound and versatile scaffold that consists of a tricyclic xanthene-9-one structure. A xanthone may exist in glycosides, aglycones, monomers or polymers. It is well known that xanthones possess a multitude of beneficial properties, including antioxidant activity, anti-inflammatory activity, and antimicrobial properties. Additionally, xanthones can be used as raw material and/or an ingredient in many food, pharmaceutical, and cosmetic applications. Although xanthones can be used in various therapeutic and functional applications, their properties and stability are determined by their extraction procedures. Extracting high-quality xanthones from mangosteen with effective therapeutic effects could be challenging if the extraction method is insufficient. Although several extraction processes are in use today, their efficiency has not yet been rigorously evaluated. Therefore, selecting an appropriate extraction procedure is imperative to recover substantial yields of xanthones with enhanced functionality from mangosteens. Hence, the present review will assist in establishing a precise scenario for finding the most appropriate extraction method for xanthones from mangosteen pericarp by critically analyzing various conventional and unconventional extraction methods and their ability to preserve the stability and biological effects of xanthones.


Assuntos
Garcinia mangostana , Xantonas , Garcinia mangostana/química , Frutas/química , Extratos Vegetais/química , Antioxidantes/química , Xantonas/química
19.
Nutrients ; 14(21)2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36364892

RESUMO

This study aims to explore the effects of Garcinia mangostana (mangosteen) and Curcuma longa independently and synergistically in modulating induced inflammation and impaired brain neurotransmitters commonly observed in high-fat diet-induced obesity in rodent models. Male albino Wistar rats were divided into four experimental groups. Group I, control, obese, fed on a high-fat diet (HFD), and Group II-IV, fed on HFD then given mangosteen extract (400 mg/kg/day) and/or Curcuma (80 mg/kg/day), or a mixture of both for 6 weeks. Plasma pro-inflammatory cytokines, leptin, and brain serotonin, dopamine, and glutamate were measured in the five studied groups. G. mangostana and Curcuma longa extracts demonstrate antioxidant and DPPH radical scavenging activities. Both induced a significant reduction in the weight gained, concomitant with a non-significant decrease in the BMI (from 0.86 to 0.81 g/cm2). Curcuma either alone or in combination with MPE was more effective. Both extracts demonstrated anti-inflammatory effects and induced a significant reduction in levels of both IL-6 and IL-12. The lowest leptin level was achieved in the synergistically treated group, compared to independent treatments. Brain dopamine was the most affected variable, with significantly lower levels recorded in the Curcuma and synergistically treated groups than in the control group. Glutamate and serotonin levels were not affected significantly. The present study demonstrated that mangosteen pericarp extract (MPE) and Curcuma were independently and in combination effective in treating obesity-induced inflammation and demonstrating neuroprotective properties.


Assuntos
Garcinia mangostana , Animais , Masculino , Ratos , Encéfalo , Curcuma , Dieta Hiperlipídica , Dopamina , Garcinia mangostana/química , Glutamatos , Inflamação/tratamento farmacológico , Leptina , Neurotransmissores , Obesidade/tratamento farmacológico , Obesidade/etiologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Ratos Wistar , Serotonina
20.
Cell Biochem Biophys ; 80(4): 633-645, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36184717

RESUMO

The MDM2-p53 protein-protein interaction is a promising model for researchers to design, study, and discover new anticancer drugs. The design of therapeutically active compounds that can maintain or restore the binding of MDM2 to p53 has been found to limit the oncogenic activities of both. This led to the current development of a group of xanthone-core and cis-imidazoline analogs compounds, among which γ-Mangostin (GM), α-Mangostin (AM), and Nutlin exhibited their MDM2-p53 interaction inhibitory effects. Therefore, in this study, we seek to determine the mechanisms by which these compounds elicit MDM2-p53 interaction targeting. Unique to the binding of GM, AM, and Nutlin, from our findings, they share the same three active site residues Val76, Tyr50, and Gly41, which represent the top active side residues that contribute to high electrostatic energy. Consequently, the free binding energy contributed enormously to the binding of these compounds, which culminated in the high binding affinities of GM, AM, and Nutlin with high values. Furthermore, GM, AM, and Nutlin commonly interrupted the stable and compact conformation of MDM2 coupled with its active site, where Cα deviations were relatively high. We believe that our findings would assist in the design of more potent active anticancer drugs.


Assuntos
Antineoplásicos , Garcinia mangostana , Imidazolinas , Xantonas , Domínio Catalítico , Garcinia mangostana/metabolismo , Imidazóis/química , Imidazóis/metabolismo , Imidazóis/farmacologia , Simulação de Dinâmica Molecular , Piperazinas/farmacologia , Ligação Proteica , Proteínas Proto-Oncogênicas c-mdm2/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Xantonas/farmacologia
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