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1.
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
2.
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
3.
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
4.
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
5.
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
6.
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
7.
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
8.
Lett Appl Microbiol ; 75(5): 1319-1329, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35934942

RESUMO

The aim of this study is to assess the antifungal action of Averrhoa bilimbi fruit and Garcinia mangostana pericarp ethanolic extracts in altering the morphology and causing cellular damage of Fusarium oxysporum, Fusarium proliferatum, Colletotrichum gloeosporioides and Lasiodiplodia theobromae. The pathogens were cultured on media containing both extracts individually and carbendazim as positive control, whereas media alone as negative control. All samples were processed for microscopy observations using scanning (SEM) and transmission electron (TEM) microscopes. Observation via SEM showed significant alterations in the hyphae of F. oxysporum, F. proliferatum and C. gloeosporioides compared to the control in which the hyphae were in normal form. However, no significant alteration in hyphae had been observed in the treated plate compared to the control for L. theobromae. The development of calcium carbonate crystals was also observed abundantly in control compared to treated pathogens for F. oxysporum and F. proliferatum only. This indicated that the plant extracts can inhibit some metabolic processes in the pathogens too. Observations via TEM had been conducted for F. proliferatum and C. gloeosporioides, respectively. The results showed disintegration of cytoplasmic organelles and cell wall, intense vacuolization and lyses part of fungal cells. The plant extracts have equivalent or even greater effects compared to commercial fungicide carbendazim.


Assuntos
Averrhoa , Fungicidas Industriais , Garcinia mangostana , Garcinia mangostana/química , Averrhoa/química , Frutas/química , Antifúngicos/farmacologia , Microscopia , Fungicidas Industriais/farmacologia , Fungicidas Industriais/análise , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Etanol/análise , Carbonato de Cálcio
9.
J Pharm Biomed Anal ; 218: 114835, 2022 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-35659659

RESUMO

Mangosteen (Garcinia mangostana L.), known as "the queen of fruits", is one of the most praised tropical fruit due to its delicious taste. In the last years, the use of mangosteen in functional products has been increasing, mainly in food beverages and nutraceutical formulations due to its biological activities related to the content of xanthones. The quantitative Nuclear Magnetic Resonance (qNMR) analysis, a rapid and accurate method used for simultaneous quantification of plant metabolites, was here employed to determine the amount of bioactive xanthones in the extracts of G. mangostana arils and shells obtained by using solvent of increasing polarity along with ''eco-friendly'' solvents like ethanol and ethanol-water. Furthermore, the content of xanthones was compared with that occurring in four selected commercial food supplements, among which tablets and capsules, and two fruit juices, based on mangosteen. Quantitative results highlighted a significant variability: the extracts of the shells displayed a higher amount of bioactive xanthones than those of the arils, in particular, of γ-mangostin and α-mangostin, while ß-mangostin, demethylcalabaxanthone, mangostanin, 8-deoxygartanin occurred in higher amounts in arils. A certain variability in the amount of biologically active xanthones (i.e. α-mangostin and γ-mangostin) could be observed in commercial food supplements.


Assuntos
Garcinia mangostana , Xantonas , Suplementos Nutricionais/análise , Etanol/análise , Frutas/química , Garcinia mangostana/química , Garcinia mangostana/metabolismo , Espectroscopia de Ressonância Magnética , Extratos Vegetais/química , Solventes/análise , Xantonas/análise
10.
Molecules ; 27(10)2022 May 20.
Artigo em Inglês | MEDLINE | ID: mdl-35630761

RESUMO

Digestive enzymes such α-amylase (AA), α-glucosidase (AG) and pancreatic lipase (PL), play an important role in the metabolism of carbohydrates and lipids, being attractive therapeutic targets for the treatment of type 2 diabetes and obesity. Garcinia mangostana is an interesting species because there have been identified xanthones with the potential to inhibit these enzymes. In this study, the multitarget inhibitory potential of xanthones from G. mangostana against AA, AG and PL was assessed. The methodology included the isolation and identification of bioactive xanthones, the synthesis of some derivatives and a molecular docking study. The chemical study allowed the isolation of five xanthones (1-5). Six derivatives (6-11) were synthesized from the major compound, highlighting the proposal of a new solvent-free methodology with microwave irradiation for obtaining aromatic compounds with tetrahydropyran cycle. Compounds with multitarget activity correspond to 2, 4, 5, 6 and 9, highlighting 6 with IC50 values of 33.3 µM on AA, 69.2 µM on AG and 164.4 µM on PL. Enzymatic kinetics and molecular docking studies showed that the bioactive xanthones are mainly competitive inhibitors on AA, mixed inhibitors on AG and non-competitive inhibitors on PL. The molecular coupling study established that the presence of methoxy, hydroxyl and carbonyl groups are important in the activity and interaction of polyfunctional xanthones, highlighting their importance depending on the mode of inhibition.


Assuntos
Diabetes Mellitus Tipo 2 , Garcinia mangostana , Xantonas , Diabetes Mellitus Tipo 2/tratamento farmacológico , Garcinia mangostana/química , Lipase , Simulação de Acoplamento Molecular , Xantonas/química , alfa-Amilases , alfa-Glucosidases
11.
Sci Rep ; 12(1): 8605, 2022 05 21.
Artigo em Inglês | MEDLINE | ID: mdl-35597781

RESUMO

Liver cancer refers primarily to hepatocellular carcinoma (HCC) accounting for over 90% of cases and is the highest incidence in men in Thailand. Over the past decades, the incidence of HCC dramatically increased with a strong rise of mortality rates. Garcinia mangostana, "Queen of Fruit" of Thailand, is known as a rich source of xanthones with potent cytotoxic properties against various cancer cells. Study on xanthones is provoking not only due to the structural diversity but also a wide variety of pharmacological activities. Hence the aim of the current study is to determine the effects of metabolites from G. mangostana root on cell proliferation and migration of hepatocellular carcinoma cells. Twenty-two metabolites, including two new benzophenones and one new biphenyl, were isolated and characterized. Five xanthones with a prenyl moiety showed significant cytotoxicity against both HCC cells tested; however, only dulxanthone D displayed the most promising activity on the migration of Huh7 HCC cells, comparable to sorafenib, a standard drug. Moreover, the compound dose-dependently induced apoptosis in Huh7 cells via mitochondrial pathway. Accordingly, dulxanthone D held a great potential for development as a novel migration inhibitor for effective HCC treatment.


Assuntos
Antineoplásicos Fitogênicos , Carcinoma Hepatocelular , Garcinia mangostana , Neoplasias Hepáticas , Xantonas , Antineoplásicos Fitogênicos/química , Benzofenonas/química , Compostos de Bifenilo , Carcinoma Hepatocelular/tratamento farmacológico , Frutas/química , Garcinia mangostana/química , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Extratos Vegetais/farmacologia , Xantonas/química , Xantonas/farmacologia
12.
Acta Trop ; 226: 106266, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-34890540

RESUMO

Acanthamoeba keratitis infection extends due to the growing number of contact lens users. Indigenous plants including Garcinia mangostana play a vital role in human health and well being. Many species of this plant have been reported with myriads of potent medicinal properties. However, the aims of this study were, for the first time, to isolate compounds from the flower of G. mangostana and to test their anti-Acanthamoeba and anti-adhesion activity against Acanthamoeba triangularis. Powdered flowers of G. mangostana were extracted and chromatographed on a silica gel column. The structures of the compounds were established with the aid of 1H NMR. More so, the anti-Acanthamoeba and anti-adhesion properties were tested on a 96-well polystyrene microtiter plate and soft contact lenses. Scanning electron microscope (SEM) was used to determine the features of A. triangularis on contact lenses. Eight pure compounds were obtained, namely 9-hydroxycalabaxanthone, tovophillin A, garcinone E, garcinone B, α-mangostin, gartinin, 8-deoxygartinin and γ-mangostin. The extract and pure compounds exhibited anti-Acanthamoeba activity with MIC values in the range of 0.25-1 mg/mL. In addition, the extract and α-mangostin displayed significant activity against the adhesion of A. triangularis trophozoites both in polystyrene plate and in contact lenses at 0.5 × MIC (0.25 mg/mL). Furthermore, α-mangostin has the potential to remove A. triangularis adhesion in contact lenses similar to a commercial multipurpose solution (MPS). SEM study confirmed that crude extract and α-mangostin are effective as solutions for contact lenses, which removed A. triangularis trophozoites within 24 h. Alpha-mangostin was non-toxic to Vero cells at a concentration below 39 µM in 24 h. Crude extract of G. mangostana flower and its α-mangostin serve as candidate compounds in the treatment of Acanthamoeba infection or as lens care solution, since they can be used as a source of natural products against Acanthamoeba and virulence factor associated with the adhesion of A. triangularis.


Assuntos
Acanthamoeba , Soluções para Lentes de Contato , Garcinia mangostana , Extratos Vegetais/farmacologia , Acanthamoeba/efeitos dos fármacos , Animais , Chlorocebus aethiops , Flores/química , Garcinia mangostana/química , Humanos , Compostos Fitoquímicos/farmacologia , Células Vero
13.
J Asian Nat Prod Res ; 24(7): 624-633, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34762536

RESUMO

Two new prenylated xanthones, mangoxanthones A-B (1-2), together with four known compounds 3-6, were isolated from the ethanol extract of the pericarp of Garcinia mangostana. The structures of these compounds have been elucidated based on spectroscopic analysis. The analysis results of chiral HPLC revealed compounds 1 and 2 were scalemic mixtures respectively. All isolated compounds were biologically evaluated for their α-glucosidase and α-amylase inhibitory effects using in-vitro assays. Compound 1 showed moderate inhibitory activities against α-glucosidase and α-amylase with IC50 of 29.06 ± 1.86 and 22.74 ± 2.07 µM, respectively. Molecular docking predicted the binding sites of compound 1 to α-glucosidase and α-amylase. A preliminary structure-activity relationship was discussed.


Assuntos
Garcinia mangostana , Garcinia , Xantonas , Frutas/química , Garcinia mangostana/química , Simulação de Acoplamento Molecular , Estrutura Molecular , Xantonas/química , Xantonas/farmacologia , alfa-Amilases/análise , alfa-Glucosidases
14.
Phytomedicine ; 95: 153797, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34802869

RESUMO

BACKGROUND: Despite advances in chemotherapies and targeted drugs, colorectal cancer (CRC) remains challenging to treat due to drug resistance. Emerging evidence indicates that cancer-associated fibroblasts (CAFs) facilitate the generation of cancer stem-like cells (CSCs) and drug resistance. Glycogen synthase kinase-3 (GSK) associated signaling pathways have been implicated in the generation of CSCs and represent a target for therapeutics development. HYPOTHESIS: Gamma-mangostin (gMG) isolated from Garcinia mangostana was evaluated for its ability to downregulate GSK3ß-associated signaling in CRC cells and overcome CAF-induced 5-fluorouracil resistance and CSC generation. METHODS: Bioinformatics analysis, in silico molecular docking, in vitro assays, including cell viability tests, colony- and tumor sphere-formation assays, transwell migration assays, ELISA, SDS-PAGE, Western blotting, miR expression, qPCR, and flow cytometry, as well as in vivo mouse xenograft models were used to evaluate the antitumor effects of gMG. RESULTS: Bioinformatics analyses indicated that GSK3ß/CDK6/ß-catenin mRNA signature was significantly higher in colon cancer patients. Additional algorithms predicted a higher miR-26b level was associated with significantly higher survival in CRC patients and GSK3ß and CDK6 as targets of miR-26b-5p. To validate these findings in vitro, we showed that CAF-cocultured CRC cells expressed an increased expression of GSK3ß, ß-catenin, CDK6, and NF-κB. Therapeutically, we demonstrated that gMG treatment suppressed GSK3ß-associated signaling pathways while concomitantly increased the miR-26b-5p level. Using a xenograft mouse model of CAFs cocultured HCT116 tumorspheres, we showed that gMG treatment reduced tumor growth and overcame CAF-induced 5-fluorouracil resistance. CONCLUSIONS: Pharmacological intervention with gMG suppressed CRC carcinogenesis and stemness via downregulating GSK3/ß-catenin/CDK6 and upregulating the miR-26b-5p tumor suppressor. Thus, gMG represents a potential new CRC therapeutic agent and warrants further investigation.


Assuntos
Neoplasias Colorretais , Garcinia mangostana , MicroRNAs , Xantonas/farmacologia , Animais , Carcinogênese , Linhagem Celular Tumoral , Proliferação de Células , Colo/metabolismo , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/genética , Quinase 6 Dependente de Ciclina , Garcinia mangostana/química , Regulação Neoplásica da Expressão Gênica , Glicogênio Sintase Quinase 3 beta , Humanos , Camundongos , MicroRNAs/genética , Simulação de Acoplamento Molecular , Via de Sinalização Wnt , beta Catenina/metabolismo
15.
PLoS One ; 16(12): e0261792, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34941972

RESUMO

A highly stable oil-in-water nanoemulsion for topical applications, containing mangostins extracted from the pericarp of mangosteen (Garcinia mangostana L.), is a promising strategy to protect mangostins as well as to improve penetration of these important antioxidants through the skins. Nanoemulsions consisted of virgin coconut oil as the oil phase, Tween-80 and Span-80 as surfactants, and xanthan gum as the thickening agent, were prepared using the high-energy and low-energy emulsification methods. The nanoemulsions that were stable up to 28 days had oil droplet diameter of 220 nm to 353 nm and zeta potential of -46.9 mV to -63.7 mV. The accelerated stability test showed that the most stable nanoemulsions were those prepared using the low-energy emulsification method with an estimated shelf life of eleven months, composed of 11% oil phase, 17% surfactant, and 72% aqueous phase. The in vitro percutaneous penetration test for the nanoemulsion with added xanthan gum provided high cumulative skin penetration of mangostins of up to 114 µg/cm2. The results of this study indicate that virgin coconut oil-based nanoemulsions containing mangostins, prepared using the low-energy emulsification method, stabilized by xanthan gum and mixed at 40°C can prospectively be used for topical applications.


Assuntos
Garcinia mangostana/química , Nanopartículas , Extratos Vegetais , Absorção Cutânea , Administração Tópica , Animais , Emulsões/química , Emulsões/farmacocinética , Emulsões/farmacologia , Camundongos , Nanopartículas/química , Nanopartículas/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/farmacocinética , Extratos Vegetais/farmacologia , Polissacarídeos Bacterianos/química , Polissacarídeos Bacterianos/farmacocinética , Polissacarídeos Bacterianos/farmacologia , Polissorbatos/química , Polissorbatos/farmacocinética , Polissorbatos/farmacologia , Tensoativos/química , Tensoativos/farmacocinética , Tensoativos/farmacologia
16.
Biomed Pharmacother ; 144: 112333, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34678724

RESUMO

Diabetes mellitus (DM) is concomitant with significant morbidity and mortality and its prevalence is accumulative in worldwide. The conventional antidiabetic agents are known to mitigate the symptoms of diabetes; however, they may also cause side and adverse effects. There is an imperative necessity to conduct preclinical and clinical trials for the discovery of alternative therapeutic agents that can overcome the drawbacks of current synthetic antidiabetic drugs. This study aimed to investigate the efficacy of lowering blood glucose and underlined mechanism of γ-mangostin, mangosteen (Garcinia mangostana) xanthones. The results showed γ-Mangostin had a antihyperglycemic ability in short (2 h)- and long-term (28 days) administrations to diet-induced diabetic mice. The long-term administration of γ-mangostin attenuated fasting blood glucose of diabetic mice and exhibited no hepatotoxicity and nephrotoxicity. Moreover, AMPK, PPARγ, α-amylase, and α-glucosidase were found to be the potential targets for simulating binds with γ-mangostin after molecular docking. To validate the docking results, the inhibitory potency of γ-mangostin againstα-amylase/α-glucosidase was higher than Acarbose via enzymatic assay. Interestingly, an allosteric relationship between γ-mangostin and insulin was also found in the glucose uptake of VSMC, FL83B, C2C12, and 3T3-L1 cells. Taken together, the results showed that γ-mangostin exerts anti-hyperglycemic activity through promoting glucose uptake and reducing saccharide digestion by inhibition of α-amylase/α-glucosidase with insulin sensitization, suggesting that γ-mangostin could be a new clue for drug discovery and development to treat diabetes.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Glicemia/efeitos dos fármacos , Diabetes Mellitus/tratamento farmacológico , Garcinia mangostana , Inibidores de Glicosídeo Hidrolases/farmacologia , Resistência à Insulina , PPAR gama/metabolismo , Extratos Vegetais/farmacologia , Xantonas/farmacologia , Células 3T3-L1 , Animais , Biomarcadores/sangue , Glicemia/metabolismo , Diabetes Mellitus/sangue , Diabetes Mellitus/enzimologia , Dieta Hiperlipídica , Modelos Animais de Doenças , Regulação para Baixo , Garcinia mangostana/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/toxicidade , Masculino , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Transdução de Sinais , Fatores de Tempo , Xantonas/toxicidade , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo
17.
Molecules ; 26(17)2021 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-34500680

RESUMO

The pharmacokinetic (PK) change in a drug by co-administered herbal products can alter the efficacy and toxicity. In the circumstances that herb-drug combinations have been increasingly attempted to alleviate Alzheimer's disease (AD), the PK evaluation of herb-drug interaction (HDI) is necessary. The change in systemic exposure as well as target tissue distribution of the drug have been issued in HDIs. Recently, the memory-enhancing effects of water extract of mangosteen pericarp (WMP) has been reported, suggesting a potential for the combination of WMP and donepezil (DNP) for AD treatment. Thus, it was evaluated how WMP affects the PK change of donepezil, including systemic exposure and tissue distribution in mice after simultaneous oral administration of DNP with WMP. Firstly, co-treatment of WMP and donepezil showed a stronger inhibitory effect (by 23.0%) on the neurotoxicity induced by Aß(25-35) in SH-SY5Y neuroblastoma cells than donepezil alone, suggesting that the combination of WMP and donepezil may be more effective in moderating neurotoxicity than donepezil alone. In PK interaction, WMP increased donepezil concentration in the brain at 4 h (by 63.6%) after administration without affecting systemic exposure of donepezil. Taken together, our results suggest that WMP might be used in combination with DNP as a therapy for AD.


Assuntos
Donepezila/química , Garcinia mangostana/química , Água/química , Doença de Alzheimer/metabolismo , Animais , Encéfalo , Modelos Animais de Doenças , Camundongos
18.
Nutrients ; 13(8)2021 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-34444764

RESUMO

BACKGROUND: Mangosteen and propolis extracts (MAEC) have been potential therapeutic agents known to exhibit powerful antioxidant and anti-inflammatory properties. The aim of the current study was to evaluate the clinical and immunological efficacy of MAEC as well as safety and patient-reported outcomes (PROMs) on gingivitis and incipient periodontitis. METHODS: This study was performed on 104 patients diagnosed with gingivitis or incipient periodontitis. At baseline, the participants were randomly allocated to either the test group, with daily intake of a single capsule containing 194 mg of MAEC for eight weeks, or control group, with placebo. Clinical periodontal evaluation and immunological parameters from saliva and gingival sulcular fluid were assessed at baseline, four, and eight weeks. Individual PROMs were assessed by OHIP-14 questionnaires. RESULTS: There was a significant difference of modified gingival index at four and eight weeks between the test and control groups. In the test group, crevicular interleukin (IL)-6 was reduced, and the salivary matrix metalloproteinase (MMP)-9 was increased after eight weeks. PROMs were improved up to four weeks compared to placebo. CONCLUSION: Oral administration of MAEC would have a potential to reduce gingival inflammation clinically and immunologically in the patients with gingivitis and incipient periodontitis.


Assuntos
Garcinia mangostana/química , Gengivite/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Própole/uso terapêutico , Adulto , Idoso , Biomarcadores , Feminino , Humanos , Interleucina-6 , Masculino , Metaloproteinase 9 da Matriz , Pessoa de Meia-Idade , Índice Periodontal , Periodontite/tratamento farmacológico , Saliva , Inquéritos e Questionários , Adulto Jovem
19.
Molecules ; 26(10)2021 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-34068232

RESUMO

In this study, a potential hard tissue substitute was mimicked using collagen/mangosteen porous scaffolds. Collagen was extracted from Tilapia fish skin and mangosteen from the waste peel of the respective fruit. Sodium trimetaphosphate was used for the phosphorylation of these scaffolds to improve the nucleation sites for the mineralization process. Phosphate groups were incorporated in the collagen structure as confirmed by their attenuated total reflection Fourier transform infrared (ATR-FTIR) bands. The phosphorylation and mangosteen addition increased the thermal stability of the collagen triple helix structure, as demonstrated by differential scanning calorimetry (DSC) and thermogravimetry (TGA) characterizations. Mineralization was successfully achieved, and the presence of calcium phosphate was visualized by scanning electron microscopy (SEM). Nevertheless, the porous structure was maintained, which is an essential characteristic for the desired application. The deposited mineral was amorphous calcium phosphate, as confirmed by energy dispersive X-ray spectroscopy (EDX) results.


Assuntos
Regeneração Óssea/efeitos dos fármacos , Osso e Ossos/fisiologia , Calcificação Fisiológica , Colágeno/farmacologia , Garcinia mangostana/química , Pele/química , Tecidos Suporte/química , Animais , Osso e Ossos/efeitos dos fármacos , Calcificação Fisiológica/efeitos dos fármacos , Fosfatos de Cálcio/química , Varredura Diferencial de Calorimetria , Peixes , Fosforilação/efeitos dos fármacos , Espectrometria por Raios X , Espectroscopia de Infravermelho com Transformada de Fourier , Temperatura , Termogravimetria
20.
Sci Rep ; 11(1): 7278, 2021 03 31.
Artigo em Inglês | MEDLINE | ID: mdl-33790313

RESUMO

The aim of this study was to explore the effects of Garcinia mangostana (mangosteen) and Curcuma longa independently and synergistically in modulating oxidative stress, dyslipidemia, and hyperglycemia commonly observed in high-fat diet-induced obesity in rodent models. Male albino Wistar rats were divided into eight experimental groups, fed on a normal diet or high-fat diet (HFD), then given mangosteen extract (400 mg /kg /day) and/or curcumin (80 mg/kg /day) for 6 weeks. Oxidative stress markers, glucose, and lipid fractions were measured in the sera. Mangosteen pericarp extract (MPE) induced a remarkable decrease in BMI (from 0.86 to 0.81 gm/cm2), while curcuma either alone or in combination was more effective, as treated rats recorded BMIs of 0.78 and 0.79 gm/cm2, respectively. Regarding the antioxidant effects, MPE induced a significant increase of GSH in obese rats (123.86 ± 15.53 µg/ml vs 288.72 ± 121.37 µg/ml). As anti-atherogenic agents MPE demonstrate significant effect recorded higher level of HDL-C in treated animals, but ineefective as anti-dyslipidemic agent. Curcumin was more effective in reducing LDL-C levels in obese rats. Both extracts effectively reduced blood glucose. The present study demonstrated that MPE and curcumin were independently and synergistically effective in treating obesity-induced atherogenesis.


Assuntos
Antioxidantes/uso terapêutico , Dislipidemias/tratamento farmacológico , Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Obesidade/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Animais , Curcumina/química , Dieta Hiperlipídica/efeitos adversos , Dislipidemias/etiologia , Garcinia mangostana/química , Hiperglicemia/etiologia , Masculino , Obesidade/etiologia , Ratos , Ratos Wistar
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