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1.
Nutrients ; 15(2)2023 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-36678139

RESUMO

Garcinia dulcis (GD) extract has been found to have anti-hypertensive properties in animal studies. GD can also alter the colonic microbiota of rats. However, the effects of GD on changes in the gut microbiota and metabolomic profiles of normotensive and hypertensive rats are currently unknown. The purpose of this study was to evaluate changes in the gut microbiota and metabolomic profiles of 2-kidneys-1 clip (2K1C) hypertensive rats after feeding with GD flower extract. Rats were randomly divided into the following 4 groups: sham operation (SO) receiving corn oil (CO) (SO + CO), SO receiving GD (SO + GD), 2K1C receiving corn oil (2K1C + CO) and 2K1C receiving GD (2K1C + GD). Body weight (BW) and systolic blood pressure (SBP) were measured weekly throughout the study. Gut microbiota and fecal metabolites were measured from fresh fecal contents. Alpha diversity results demonstrated a similar microbial richness and diversity between groups. Linear discriminant analysis (LDA) effect size (LEfSe) suggested that GD treatment affected gut microbial community structure in both hypertensive and normotensive rats. Feeding rats with GD caused metabolic alterations that rendered 2K1C + GD rats similar to SO + CO and SO + GD rats. Findings suggest that the impact of GD on gut microbiota and metabolite profiles may be related to its anti-hypertensive properties.


Assuntos
Garcinia , Microbioma Gastrointestinal , Hipertensão Renovascular , Hipertensão , Ratos , Animais , Hipertensão Renovascular/tratamento farmacológico , Anti-Hipertensivos/farmacologia , Anti-Hipertensivos/uso terapêutico , Óleo de Milho/farmacologia , Hipertensão/tratamento farmacológico , Pressão Sanguínea , Extratos Vegetais/farmacologia
2.
Drug Des Devel Ther ; 16: 3573-3588, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36248245

RESUMO

Data from globocan statistic in 2020 indicate that breast cancer has become highest incidence rate of cancer. Estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER2) are known immunohistochemistry (IHC) markers that mediate cell growth and survival signaling. Furthermore, regulator proteins, receptors, and their downstream signaling pathways have emerged as critical components in breast cancer formation and proliferation, and have become well-established therapeutic targets and the core focus of breast cancer therapy research. Garcinia is a big genus in the Clusiaceae family that contains a wide spectrum of biologically active metabolites for the chemical composition of their isolated fruits, stem barks, seeds, leaves, and roots, have resulted including polyisoprenylated benzophenones, polyphenols, bioflavonoids, xanthones, lactones, and triterpenes. This review article aimed to analyze the potential of Garcinia phytochemicals as a molecular therapy of breast cancer. The results showed that phytochemicals of Garcinia (i.e., α-mangostin, Cambogin, Gambogic Acid [GA], Garcinol, Griffipavixanthone, Friedolanostane triterpenoid, Hexane, Neobractatin, 7-Epiclusianone, xanthochymol - guttiferone E, and isoxanthochymol - cycloxanthochymol) have anticancer properties, including apoptosis, inhibition of proliferation, and metastasis. This review is important to provide information regarding phytochemicals of Garcinia as an alternative treatment for breast cancer patients. This article selected 28 article researches based on inclusion criteria with the keyword "Garcinia" and "Breast cancer", in English, and available in full text and abstract searching on PubMed.


Assuntos
Garcinia , Neoplasias , Plantas Medicinais , Triterpenos , Xantonas , Benzofenonas/química , Benzofenonas/farmacologia , Garcinia/química , Medicina Herbária , Hexanos , Humanos , Lactonas , Compostos Fitoquímicos/farmacologia , Polifenóis , Receptores de Estrogênio , Receptores de Progesterona , Triterpenos/química , Xantonas/química
3.
J Agric Food Chem ; 70(34): 10506-10520, 2022 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-35997267

RESUMO

The fruits of Garcinia oblongifolia Champ. ex Benth. were famous as an edible fruit in tropical regions of China. Because of its unique taste and great nutritional value, the ripe fresh fruits of G. oblongifolia could be eaten directly or used as raw materials for natural beverages and food supplements. In this work, six new polyprenylated benzophenones (1-6) and one new dimeric tocotrienol derivative (7), together with 18 known ones (8-25), were isolated from the fruits of G. oblongifolia. Compounds 1-4 were peculiar polycyclic polyprenylated acylphloroglucinols (PPAPs) featuring the rare carbon skeleton of a bicyclo[3.4.1]decane-1,3-diketone. Moreover, all isolates (1-25) were evaluated for their cytotoxicity activities against nasopharyngeal carcinoma (NPC) cell lines (CNE1 and CNE2). Among these isolates, compound 6 exhibited the strongest cytotoxicity activity on CNE1 and CNE2 cells with the IC50 values of 7.8 ± 0.2 and 9.1 ± 0.3 µM, respectively. Further mechanistic investigation demonstrated that 6 could induce mitophagy to promote Caspase-9/GSDME-mediated pyroptosis through triggering ROS in NPC cells.


Assuntos
Garcinia , Tocotrienóis , Benzofenonas/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Frutas/química , Estrutura Molecular , Floroglucinol/farmacologia , Tocotrienóis/farmacologia
4.
Chem Biodivers ; 19(10): e202200022, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-35997661

RESUMO

This study evaluated the diuretic and antiurolithic effect of methanolic extract (MEGHL), dichloromethane (DCM), and ethyl acetate (EtA) fractions obtained from the leaves of Garcinia humilis, a medicinal plant known as achachairu and native to South American countries such as Bolivia, Peru, and Brazil. For the analysis of diuretic effect, the female rats received the treatment with MEGHL (3, 10, and 30 mg/kg), DCM (1, 3 and 10 mg/kg), EtA (1, 3, and 10 mg/kg), hydrochlorothiazide (HCTZ; 10 mg/kg), or vehicle (VEH) after an overload of saline solution. At the end 8 h of the experiment, the urinary parameters were measured. Additionally, the antiurolithic effect was analyzed, in which sodium oxalate was added in synthetic urine in the presence or absence of MEGHL, DCM, and EtA in different concentrations (0.1, 0.3, and 1 mg/mL). MEGHL, DCM, and EtA were able to promote 8-h diuresis in rats. MEGHL treatment at dose 30 mg/kg was accompanied by increased urinary Na+ , K+ and Cl- excretion. Moreover, the DCM and EtA fractions treatment increased K+ and Cl- excretion in the urine, although it does not cause any change in Na+ elimination. All the preparations were able to exert an antiurolithic effect in vitro, decreasing the number of calcium oxalate crystals of the monohydrate and dihydrate types. Taking together, the results presented herein showed that the preparations of G. humilis leaves are promising strategies to induce diuresis and antiurolithic effects.


Assuntos
Garcinia , Plantas Medicinais , Ratos , Animais , Diuréticos/farmacologia , Diuréticos/análise , Oxalato de Cálcio/análise , Cloreto de Metileno/análise , Solução Salina , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/análise , Ratos Wistar , Folhas de Planta/química , Hidroclorotiazida/análise , Hidroclorotiazida/farmacologia , Brasil
5.
Chem Biodivers ; 19(9): e202200376, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35927784

RESUMO

Six new polyoxygenated xanthones, garcicowanones F-H (1-3), norcowanol A-B (4-5), and garcinone F (6) along with twelve known compounds 7-18 were obtained from the latex of Garcinia cowa Roxb. ex Choisy. All new compounds have a 1,3,7-trioxygenated or 1,3,6,7-tetraoxygenated xanthone nucleus and differ from majority of xanthones from G. cowa by hydrated side chains. Compounds 1, 7, 8 and 18 exhibited significant neuroprotective effects on glutamate-mediated hippocampal neuronal HT22 cell death. In particular, compound 1 exhibited the most potent neuroprotective effect with >80 % cell viability in the concentration range of 2.9-115 µM. Further studies on compound 1 showed that it decreased cellular Ca2+ influx and inhibits cellular reactive oxygen species generation in HT22 cells. A Western blot analysis showed that MAPK phosphorylation, Bax, and AIF translocation dramatically increased upon treatment with 5 mM glutamate and decreased upon a co-treatment with compound 1.


Assuntos
Garcinia , Fármacos Neuroprotetores , Xantonas , Morte Celular , Garcinia/química , Ácido Glutâmico , Hipocampo , Látex , Fármacos Neuroprotetores/farmacologia , Espécies Reativas de Oxigênio , Xantonas/química , Xantonas/farmacologia , Proteína X Associada a bcl-2
6.
J Food Biochem ; 46(10): e14344, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35933691

RESUMO

Garcinia indica Choisy (kokum), a plant from Clusiaceae family, is an underexplored fruit tree in the Western Ghats region. Kokum has been studied for its health benefits, associated with numerous bioactive compounds, including phenolic acids, flavonoids, citric acids, and others. Among all, garcinol, hydroxycitric acid, and anthocyanins (cyanidin-3-glucoside and cyanidin-3-sambubioside) are major bioactive compounds. G. indica fruit and fruit rinds have been reported to possess numerous therapeutic applications in various health conditions such as cancer, inflammation, diabetes, obesity, cardiovascular disease, and neurologic disorders. In this review, information has been provided on the bioactive compounds present in kokum and their significant health benefits. In vitro and In vivo studies of bioactive components on various diseases have also been reported. The limited information about human studies and G. indica fruit and fruit rinds is also presented. PRACTICAL APPLICATIONS: Bioactive compounds present in Garcinia indica can be utilized for nutraceutical preparations. G. indica can be added to food products to make them functional foods. Extraction of bioactive compounds can be done on an industrial scale. Bioactive compounds can be extracted and used to commercialize lifesaving drugs.


Assuntos
Garcinia , Antocianinas/farmacologia , Ácido Cítrico , Frutas , Humanos , Extratos Vegetais/farmacologia
7.
Bioorg Chem ; 128: 106106, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-36037599

RESUMO

Natural products with diverse structures and significant biological activities are essential sources of drug lead compounds, and play an important role in the research and development of innovative drugs. Cage-like compounds have various structures and are widely distributed in nature, especially caged xanthones isolated from Garcinia genus, paeoniflorin and its derivatives isolated from Paeonia lactiflora Pall, tetrodotoxin (TTX) and its derivatives, and so on. In recent years, the development and utilization of cage-like compounds have been a research hotspot in chemistry, biology and other fields due to their special structures and remarkable biological activities. In this review, we mainly summarized the cage-like compounds with various structures found and isolated from natural drugs since 1956, summarized its broad biological activities, and introduced the progress in the biosynthesis of some compounds, so as to provide a reference for the discovery of more novel compounds, and the development and application of innovative drugs.


Assuntos
Produtos Biológicos , Garcinia , Paeonia , Xantonas , Produtos Biológicos/química , Garcinia/química , Extratos Vegetais/química , Xantonas/química
8.
Food Chem ; 391: 133279, 2022 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-35640341

RESUMO

In view of the low exploitation Garcinia brasiliensis and its richness in bioactive compounds, this article is justified by the need to develop a product which adds value to this fruit. The objective was to develop bacupari pulp powder (BPP) in two stages of maturation and to evaluate its physicochemical, microstructural and bioactive properties. Data showed that BPP can be considered as a source of fiber (≅16 g.100-1/ P < 0.05), a result verified via scanning electron microscopy. The immature pulp can be considered as a source of protein, as it contains>6 g.100-1. Regarding the antioxidant content, it was found that the ABTS method showed the best result (2449 µmolTE/100 g/P > 0.05) and it was the first time that the bioactive compounds folic acid, trans-ferulic acid, and sinapic acid were identified in this fruit. Therefore, the use of the BPP form is an alternative for the consumption of this underexploited fruit.


Assuntos
Garcinia , Antioxidantes/análise , Fibras na Dieta/análise , Frutas/química , Garcinia/química , Pós/análise
9.
Molecules ; 27(9)2022 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-35566362

RESUMO

The present study describes investigation of the effects of the bark resin extract of Garcinia nigrolineata (Clusiaceae) on the cognitive function and the induction of oxidative stress in both frontal cortex and hippocampus by unpredictable chronic mild stress (UCMS). By using behavioral mouse models, i.e., the Y-maze test, the Novel Object Recognition Test (NORT), and the Morris Water Maze Test (MWMT), it was found that the negative impact of repeated mild stress-induced learning and memory deficit through brain oxidative stress in the UCMS mice was reversed by treatment with the bark resin extract G. nigrolineata. Moreover, the prenylated xanthones viz. cowagarcinone C, cowaxanthone, α-mangostin, cowaxanthone B, cowanin, fuscaxanthone A, fuscaxanthone B, xanthochymusxanthones A, 7-O-methylgarcinone E, and cowagarcinone A, isolated from the bark resin of G. nigrolineata, were assayed for their inhibitory activities against ß-amyloid (Aß) aggregation and monoamine oxidase enzymes (MAOs).


Assuntos
Garcinia , Xantonas , Peptídeos beta-Amiloides , Animais , Modelos Animais de Doenças , Transtornos da Memória/tratamento farmacológico , Transtornos da Memória/etiologia , Camundongos , Monoaminoxidase , Casca de Planta , Extratos Vegetais/farmacologia , Resinas Vegetais , Xantonas/farmacologia
10.
Nat Commun ; 13(1): 2461, 2022 05 05.
Artigo em Inglês | MEDLINE | ID: mdl-35513402

RESUMO

Owing to the existence of the outer membrane barrier, most antibacterial agents cannot penetrate Gram-negative bacteria and are ineffective. Here, we report a general method for narrow-spectrum antibacterial Garcinia nanoparticles that can only be effective to kill Gram-positive bacteria, to effectively eliminate Gram-negative bacteria by creating transient nanopores in bacterial outer membrane to induce drug entry under microwaves assistance. In vitro, under 15 min of microwaves irradiation, the antibacterial efficiency of Garcinia nanoparticles against Escherichia coli can be enhanced from 6.73% to 99.48%. In vivo, MV-assisted GNs can effectively cure mice with bacterial pneumonia. The combination of molecular dynamics simulation and experimental results reveal that the robust anti-E. coli effectiveness of Garcinia nanoparticles is attributed to the synergy of Garcinia nanoparticles and microwaves. This work presents a strategy for effectively treating both Gram-negative and Gram-positive bacteria co-infected pneumonia using herbal medicine nanoparticles with MV assistance as an exogenous antibacterial auxiliary.


Assuntos
Garcinia , Nanopartículas , Animais , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Escherichia coli , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Camundongos , Testes de Sensibilidade Microbiana , Micro-Ondas
11.
Metab Brain Dis ; 37(6): 1887-1900, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35622265

RESUMO

Dopaminergic neuroprotection is the main interest in designing novel therapeutics against Parkinson's disease (PD). In the process of dopaminergic degeneration, mitochondrial dysfunctions and inflammation are significant. While the existing drugs provide symptomatic relief against PD, a therapy conferring total neuroprotection by targeting multiple degenerative pathways is still lacking. Garcinia morella is a common constituent of Ayurvedic medication and has been used for the treatment of inflammatory disorders. The present study investigates whether administration of G. morella fruit extract (GME) in MPTP mouse model of PD protects against dopaminergic neurodegeneration, including the underlying pathophysiologies, and reverses the motor behavioural abnormalities. Administration of GME prevented the loss of dopaminergic cell bodies in the substantia nigra and its terminals in the corpus striatum of PD mice. Subsequently, reversal of parkinsonian behavioural abnormalities, viz. akinesia, catalepsy, and rearing, was observed along with the recovery of striatal dopamine and its metabolites in the experimental model. Furthermore, reduced activity of the mitochondrial complex II in the nigrostriatal pathway of brain of the mice was restored after the administration of GME. Also, MPTP-induced enhanced activation of Glial fibrillary acidic protein (GFAP) and neuronal nitric oxide synthase (nNOS) in the nigrostriatal pathway, which are the markers of inflammatory stress, were found to be ameliorated on GME treatment. Thus, our study presented a novel mode of dopaminergic neuroprotection by G. morella in PD by targeting the mitochondrial dysfunctions and neuroinflammation, which are considered to be intricately associated with the loss of dopaminergic neurons.


Assuntos
Garcinia , Doença de Parkinson , 1-Metil-4-Fenil-1,2,3,6-Tetra-Hidropiridina/metabolismo , Animais , Corpo Estriado/metabolismo , Modelos Animais de Doenças , Dopamina/metabolismo , Neurônios Dopaminérgicos/metabolismo , Garcinia/metabolismo , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Mitocôndrias/metabolismo , Neuroproteção , Doença de Parkinson/metabolismo , Substância Negra/metabolismo
12.
Phytomedicine ; 102: 154142, 2022 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-35623158

RESUMO

BACKGROUND: Pyroptosis, an inflammatory form of programmed cell death (PCD), is reported to play important roles in the treatment of tumors. In our previous studies, we found that neobractatin (NBT), a caged prenylxanthone isolated from edible fruits of Garcinia bracteata C. Y. Wu ex Y. H. Li, showed anticancer effects against different cancer cells. However, the effect of NBT on pyroptosis is not well understood. PURPOSE: This study aims to investigate whether and how GSDME-mediated pyroptosis contributes to NBT-induced antitumor effects in esophageal cancer (EC) cells. METHODS: Cell viability assay and colony formation assay were used to determine the anticancer effects of NBT in esophageal cancer cells. Lactate dehydrogenase (LDH) release assay and microscopy imaging were used to detect the main characteristic of pyroptosis. CRISPR-Cas9 knockout and siRNA knockdown were performed to verify the roles of GSDME and caspase-3 in NBT-induced pyroptosis. Flow cytometry was used to measure the reactive oxygen species (ROS) level and cell apoptosis. The changes of related protein level were detected by Western blot. Furthermore, animal experiments were used to verify the in vivo effect of NBT. RESULTS: The results showed that NBT reduced the viability of EC cells mainly through GSDME-mediated pyroptosis. Morphologically, NBT induced cell swelling and formed large bubbles emerging from plasma membrane in wild type EC cells. Furthermore, NBT induced the cleavage of GSDME by activating caspase-3 in EC cells. On the other hand, caspase-3 activated by NBT also induced apoptosis especially at high dosage. Knocking down GSDME switched NBT-induced cell death from mainly pyroptosis to apoptosis in vivo and in vitro. Mechanistic studies indicated that NBT led to accumulation of ROS, which then regulated the phosphorylation of both JNK and MEK/ERK. In the absence of ROS or caspase-3, NBT-induced pyroptosis and apoptosis were completely reversed. Moreover, NBT showed a significant antitumor effect in both the KYSE150 and GSDME knockout KYSE150-/- xenograft models by inducing pyroptosis and apoptosis, respectively. CONCLUSION: Our results indicated that natural compound NBT could induce GSDME-mediated pyroptosis and apoptosis in esophageal cancer cells, making it a potential therapeutic drug in clinical treatment.


Assuntos
Neoplasias Esofágicas , Garcinia , Animais , Caspase 3/metabolismo , Neoplasias Esofágicas/tratamento farmacológico , Humanos , Piroptose , Espécies Reativas de Oxigênio/metabolismo , Receptores de Estrogênio/metabolismo
13.
J Ethnopharmacol ; 295: 115334, 2022 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-35597412

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Wound healing is a complex process that can leave pathological scars, especially in case of infections from opportunistic microorganisms. In this context, herbal medicines open up great possibilities for investigation. One of the species of interest native to Brazil is Garcinia brasiliensis ("bacupari"). Traditionally known for treating wounds and ulcers, G. brasiliensis presents anti-inflammatory, antioxidant and antimicrobials properties. But, its wound healing profile in experimental models, in order to validate its efficacy, is still litle studied. AIM OF THE STUDY: Thus, the objective of this work was to evaluate, in an infected cutanous wound model, the potential of formulations incorporated with G. brasiliensis leaves extracts. MATERIALS AND METHODS: Crude extract (CE), Ethyl Acetate Fraction (EAF) and Hexanic Fraction (HF) were submitted to phytochemical assays, high performance thin layer chromatography (HTPLC) and cytotoxicity studies. CE and EAF were also tested for microbicidal properties and incorporated in cream and gel formulations at 10% concentration. After stability testing, the gel formulations with CE or EAF at 10% were selected and applied to skin wounds infected or not with Staphylococcus aureus in Wistar rats. The healing potenttial of the extracts was verified by the expression of the protein Annexin A1 (AnxA1), related to the processes of inflammation and antifibrotic function, the cells immunostaining for Gasdermin-D (GSDM-D), a marker of pyroptotic cell death, and the dosage of interleukin-10 (IL-10) and monocyte chemotactic protein (MCP)-1 inflammatory mediators. RESULTS: Phytochemical studies indicated the presence of compounds of pharmacological interest, including Catechin, Quercetin and Berberine in addition to low cytotoxicity of CE and EAF at 10%. After the 6-day topical treatments, CE and EAF gel formulations demonstrated to control the pruritus formation process. The treatments decreased AnxA1 expression and the amount of cells immunostained for GSDM-D, and increased the expression of MCP-1 in infected wounds. CONCLUSIONS: Together, the results show important anti-inflammatory profile and skin healing potential of CE and EAF from G. brasiliensis leaves, even in infected lesions, with therapeutic perspectives.


Assuntos
Garcinia , Animais , Anti-Inflamatórios/análise , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Compostos Fitoquímicos/análise , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Ratos , Ratos Wistar , Cicatrização
14.
Bol. latinoam. Caribe plantas med. aromát ; 21(3): 309-322, mayo 2022. tab
Artigo em Inglês | LILACS | ID: biblio-1396871

RESUMO

This paper describes the evaluation of the antimicrobial and hemolytic activity of the hexane, dichloromethane, ethyl acetate and methanol extracts from seeds and epicarps of Garcinia madruno; as well garcinol, morelloflavone and volkensiflavone isolated from the same species. In the preliminary test of bacterial susceptibility, hexane extracts from seeds and epicarps and the three compounds tested only displayed inhibitory growth effect against Gram-positive bacteria. The minimum inhibitory concentrations of extract and compounds ranging from 86.6 to 1253.4 µg/mL. The hemolytic activity was assessed; however, except for the methanol extract from seeds, none of the samples studied induced hemolysis. Thus, our results suggest that extracts and compounds from G. madruno have the potential to be used in the control of pathologies associated to Gram-positive bacteria. This is the first report of the antimicrobial and hemolytic activity of extracts of different polarity obtained from seeds and epicarps of this edible species.


El presente artículo describe la evaluación de la actividad antimicrobiana y hemolítica de los extractos de hexano, diclorometano, acetato de etilo y metanol, obtenidos de la semilla y el epicarpio de Garcinia madruno; así como de garcinol, morelloflavona y volkensiflavona; aislados de la misma especie. En el ensayo de susceptibilidad bacteriana, tanto el extracto de hexano obtenido a partir de la semilla y el epicarpio, y los tres compuestos aislados, únicamente mostraron actividad inhibitoria del crecimiento contra bacterias Gram-positivas. La concentración mínima inhibitoria presentó valores entre 86.6 y 1253.4 µg/mL. También se estableció la actividad hemolítica; sin embargo, con excepción del extracto metanólico obtenido a partir de las semillas, ninguna de las muestras evaluadas indujo hemólisis. Por lo tanto, los resultados sugieren que los extractos y compuestos de G. madruno tienen el potencial de ser usados en el control de bacterias Gram-positivas asociadas a diversas patologías. Este es el primer reporte de actividad antimicrobiana y hemolítica de extractos de diferente polaridad obtenidos de las semillas y epicarpios de esta especie comestible.


Assuntos
Extratos Vegetais/farmacologia , Garcinia/química , Hemolíticos/farmacologia , Antibacterianos/farmacologia , Sementes/química , Terpenos/análise , Bactérias/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Biflavonoides/análise
15.
Molecules ; 27(8)2022 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-35458771

RESUMO

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 silico molecular docking model suggested that both compounds are potent inhibitors of enzyme α-glucosidase and are therefore leading candidates as therapies for diabetes mellitus.


Assuntos
Anti-Infecciosos , Garcinia , Frutas , Garcinia/química , Inibidores de Glicosídeo Hidrolases/química , Simulação de Acoplamento Molecular , Staphylococcus aureus , alfa-Glucosidases
16.
Molecules ; 27(3)2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-35164214

RESUMO

Neuraminidase (NA) is an enzyme that prevents virions from aggregating within the host cell and promotes cell-to-cell spread by cleaving glycosidic linkages to sialic acid. The best-known neuraminidase is the viral neuraminidase, which present in the influenza virus. Thus, the development of anti-influenza drugs that inhibit NA has emerged as an important and intriguing approach in the treatment of influenza. Garcinia atroviridis L. (GA) dried fruits (GAF) are used commercially as seasoning and in beverages. The main objective of this study was to identify a new potential neuraminidase inhibitor from GA. A bioassay-guided fractionation method was applied to obtain the bioactive compounds leading to the identification of garcinia acid and naringenin. In an enzyme inhibition study, garcinia acid demonstrated the highest activity when compared to naringenin. Garcinia acid had the highest activity, with an IC50 of 17.34-17.53 µg/mL or 91.22-92.21 µM against Clostridium perfringens-NA, and 56.71-57.85 µg/mL or 298.32-304.31 µM against H1N1-NA. Based on molecular docking results, garcinia acid interacted with the triad arginine residues (Arg118, Arg292, and Arg371) of the viral neuraminidase, implying that this compound has the potential to act as a NA enzyme inhibitor.


Assuntos
Antivirais/farmacologia , Inibidores Enzimáticos/farmacologia , Frutas/química , Garcinia/química , Neuraminidase/antagonistas & inibidores , Extratos Vegetais/farmacologia , Folhas de Planta/química , Humanos , Proteínas Virais/antagonistas & inibidores
17.
Molecules ; 27(2)2022 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-35056797

RESUMO

Moreollic acid, a caged-tetraprenylated xanthone from Gamboge, has been indicated as a potent antitumor molecule. In the present study, a series of moreollic acid derivatives with novel structures were designed and synthesized, and their antitumor activities were determined in multifarious cell lines. The preliminary screening results showed that all synthesized compounds selectively inhibited human colon cancer cell proliferation. TH12-10, with an IC50 of 0.83, 1.10, and 0.79 µM against HCT116, DLD1, and SW620, respectively, was selected for further antitumor mechanism studies. Results revealed that TH12-10 effectively inhibited cell proliferation by blocking cell-cycle progression from G1 to S. Besides, the apparent structure-activity relationships of target compounds were discussed. To summarize, a series of moreollic acid derivatives were discovered to possess satisfactory antitumor potentials. Among them, TH12-10 displays the highest antitumor activities against human colon cancer cells, in which the IC50 values in DLD1 and SW620 are lower than that of 5-fluorouracil.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Neoplasias do Colo/tratamento farmacológico , Garcinia/química , Xantonas/química , Xantonas/farmacologia , Antineoplásicos/síntese química , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Piperidinas/síntese química , Piperidinas/química , Piperidinas/farmacologia , Relação Estrutura-Atividade , Xantonas/síntese química
18.
Biomed Pharmacother ; 147: 112577, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35078092

RESUMO

Cowanin, a xanthone derivative extracted from the Garcinia fusca plant, has been recognized for various biological activities including, antimicrobial, anti-inflammatory, and anticancer activities. However, the mechanism to induce cancer cell death in cancer cells remains to be fully elucidated. Our previous report showed that other xanthones from these plants could act as histone deacetylase inhibitors (HDACi), so we deeply analyzed the role of cowanin, a major compound of G.fusca, and investigated through the mode of cell death both apoptosis and autophagy that have never been reported. As a result, it was demonstrated that cowanin indicated the role of HDACi as other xanthones. The molecular docking analysis showed that cowanin could interact within the catalytic pocket region of HDAC class I (HDAC2, 8) and II (HDAC4, 7) proteins and inhibit their activity. Also, the level of protein expression of HDAC2, 4, 7, and 8 was distinctly decreased, and the level of histone H3 and H4 acetylation increased in cowanin treated cells. For the mode of cell death, cowanin demonstrated both apoptosis and autophagy activation in Jurkat cells. Besides, cowanin significantly suppressed phosphorylation of PI3K, Akt, and mTOR signaling. Therefore, these findings revealed that cowanin represents a new promising candidate for development as an anticancer agent by inducing apoptosis and autophagy via PI3K/AKT/mTOR pathway and effectively inhibiting HDAC activity.


Assuntos
Garcinia , Inibidores de Histona Desacetilases/farmacologia , Extratos Vegetais/farmacologia , Apoptose/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Inibidores de Histona Desacetilases/química , Inibidores de Histona Desacetilases/uso terapêutico , Humanos , Células Jurkat/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos , Serina-Treonina Quinases TOR/metabolismo
19.
Food Funct ; 13(4): 1741-1750, 2022 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-35088780

RESUMO

The fruits of Garcinia bracteata can be eaten raw or processed into spices, which are considered to possess nutritional and medicinal value. Neobractatin (NBT) is a natural compound isolated from Garcinia bracteate. This study showed that NBT showed antitumor effect by upregulation of CELF6. CELF6, an RNA-binding protein of the CELF family, is involved in cancer cell proliferation. However, the role of CELF6 in human cervical cancer remains unknown. Here, we showed that CELF6 overexpression significantly suppressed HeLa cell proliferation. Mechanistically, the RNA immunoprecipitation sequencing (RIP-seq) results suggested that CELF6 physically targeted the cyclin D1 transcript, affecting protein stability. Overexpression of CELF6 increased the degradation of cyclin D1. Consistent results were obtained for the effect of NBT, which increased the expression of CELF6 at both the mRNA and protein levels. An in vivo study further confirmed the regulatory effect of NBT on CELF6 and cyclin D1 levels in a HeLa xenograft model. Similar effects of NBT on CELF6 were also shown in K562 cells in vitro and in vivo. In conclusion, our findings identified CELF6 as a tumor suppressor and a novel therapeutic target in cervical cancer. The upregulation of CELF6 expression by NBT and its antiproliferative effect on HeLa cells indicated that NBT from G. bracteata might be a small-molecule compound targeting CELF6.


Assuntos
Proteínas CELF , Proliferação de Células/efeitos dos fármacos , Xantonas , Animais , Proteínas CELF/genética , Proteínas CELF/metabolismo , Frutas/química , Garcinia/química , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Células HeLa , Humanos , Camundongos , Camundongos Nus , Xantonas/química , Xantonas/farmacologia
20.
Nat Prod Res ; 36(1): 207-213, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32530310

RESUMO

Two new glycerol esters, (S)-2-hydroxy-3-(octanoyloxy)propyl tetracosanoate (1) and (S)-3-(((S)-11-acetoxy octadecanoyl)oxy)propane-1,2-diyl diacetate (2), and eight known compounds, docosanedioic acid (3), 2,5-dimethylnonadecane (4), lupeol (5), stigmasterol (6), ß-sitosterol (7), heptadecanoic acid (8), hexanedioic acid, 1,6-bis[(2R)-ethylhexyl] ester (9), and 1,3-di-O-[2',2'-di-(p-phenylene)] (10) were isolated from the leaves of Garcinia daedalanthera Pierre, collected from Indonesia. Structural analysis of the isolates was performed using 1 D- and 2 D-NMR, LC- and GC-MS, IR, polarimetry, and UV-visible spectroscopic methods. Cytotoxicity assessments, as well as reactive oxygen species (ROS) analysis of the isolates, were also completed. Lupeol was the only compound found active with an IC50 value of 19.2 µM against HT-29 colon cancer cells. Significant ROS inhibition and induction activity was observed for compounds 4 and 8, respectively.


Assuntos
Clusiaceae , Garcinia , Estrutura Molecular , Folhas de Planta , Estigmasterol
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