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1.
J Oleo Sci ; 73(4): 429-435, 2024 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-38171737

RESUMO

Sacha inchi (Plukenetia volubilis) oil is constituted with macronutrients and the health benefit fatty acids. In this context, the efficient of Sacha inchi oil for anti-aging product is presented. The light-clear yellowish seed oil of Sacha inchi was revealed on its physicochemical properties that are in the same range of the commercializing plant-oil supplied for topical products. The oil was GC/MS exhibited to be constituted with α-linolenic (51.72%) and linoleic (24.3%) acids, with unsaturated/saturated fatty acids ratio of 21.26. The oil was noted onto its potent in vitro antioxidant activity assessed by ABTS, DPPH and FRAP assays. In addition, the oil (1-3%) was proved to be safe in normal human fibroblast cells. Furthermore, the oil exhibited cellular antioxidant with inhibitory effect against MMP-2. Sacha inchi oil is therefore highlighted as a potential source of nutraceutical especially for anti-aging product. The oil is specified for the product development in terms of physicochemical, chemical and biological profiles. Innovative processing of Sacha inchi is therefore encouraged as the promising plant for anti-aging product.


Assuntos
Euphorbiaceae , Ácidos Graxos Insaturados , Humanos , Ácidos Graxos , Óleos de Plantas/farmacologia , Óleos de Plantas/química , Envelhecimento , Antioxidantes/farmacologia , Euphorbiaceae/química
2.
Appl Biochem Biotechnol ; 195(3): 1699-1722, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36367619

RESUMO

The second most common and lethal disease is lung cancer. To combat the negative effects of today's synthetic medications, natural phytomedicines are required. Tragia plukenetii is a medicinal plant native to India that belongs to the Euphorbiaceae family. The purpose of this research is to isolate bioactive compounds from T. plukenetii leaves and then test them for anticancer property. A single compound (CH: ME-20:80) was separated using TLC, and an RF value of 0.55 was determined. Spectral analyses utilizing UV-Visible Spectrophotometer and FT-IR were used to examine the absorbance and functional groups. 13C-NMR and 1H-NMR studies revealed the tentative name of the purified phytochemical as omega-decenol (OD). Further antioxidant and anticancer properties of OD were tested for in vitro. In comparison to conventional L-ascorbic acid, the DPPH radical scavenging assay experiment yielded an IC50 of 147.48 g/ml. With an IC50 value of 24 µg/ml (Omega-decenol) and 32 µg/ml (doxorubicin), the MTT assay demonstrated the cytotoxic capability against the A549 lung cancer cell line. FACS revealed the cell cycle arrest of A549 at S phase compared to control with the high-dose IC50 (250 µg/ml) of omega-decenol. Twelve major compounds were detected in the active fraction using GC-MS analysis, where n-hexadecanoic acid was found as a major. Omega-decenol showed good binding affinity against EGFR, amongst other receptors in the in silico docking study. This research reveals the potent anticancer activity of the isolated compound omega-decenol from T. plukenetii leaves and provides a key path to understanding the molecular interaction in anticancer aspects against adenocarcinoma.


Assuntos
Antineoplásicos , Euphorbiaceae , Neoplasias Pulmonares , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Espectroscopia de Infravermelho com Transformada de Fourier , Antineoplásicos/farmacologia , Euphorbiaceae/química , Antioxidantes/química
3.
J Nat Prod ; 85(11): 2687-2693, 2022 11 25.
Artigo em Inglês | MEDLINE | ID: mdl-36378070

RESUMO

Four new diterpene esters, shirakindicans A-D (1-4), along with eight related known diterpene esters (5-12), were isolated from the fruits of the Bangladeshi medicinal plant Shirakiopsis indica. The structures of 1-4 were elucidated by spectroscopic data analysis and electronic circular dichroism (ECD) calculations. Shirakindican A (1) was assigned as a tigliane-type diterpene ester possessing an unusual 6ß-hydroxy-1,7-dien-3-one structure, while shirakindican B (2) exhibits a tiglia-1,5-dien-3,7-dione structure. The anti-HIV activities of the isolated diterpene esters were evaluated and showed significant activities for sapintoxins A (5) and D (11), with EC50 values of 0.0074 and 0.044 µM, respectively, and TI values of 1 100 and 5 290. Sapatoxin A (12) also exhibited anti-HIV activity with an EC50 value of 0.13 µM and a TI value of 161.


Assuntos
Fármacos Anti-HIV , Euphorbiaceae , HIV , Ésteres de Forbol , Euphorbiaceae/química , Frutas/química , Estrutura Molecular , HIV/efeitos dos fármacos , Ésteres de Forbol/química , Ésteres de Forbol/isolamento & purificação , Ésteres de Forbol/farmacologia , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/farmacologia , Linhagem Celular , Humanos
4.
Molecules ; 27(21)2022 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-36364140

RESUMO

Andean lupin (Lupinus mutabilis) oil is rich in monounsaturated (54.2%) and polyunsaturated (28.5%) fatty acids but has a ω-3:ω-6 ratio (1:9.2) above the recommended values for human health. Sacha inchi (Plukenetia volubilis) oil presents a high polyunsaturated fatty acid content (linolenic 47.2% and linoleic 34.7%), along a ω-3:ω-6 ratio (1:0.74) good for human consumption. The objective of this research was to study the physico-chemical properties and oxidative stability of tarwi and sacha inchi oil blends (1:4, 1:3, 1:1, 3:1 and 4:1 w:w) with suitable ω-3:ω-6 ratios. All blends showed ω-3:ω-6 ratios between 1:0.8 and 1:1.9, acceptable from a nutritional point of view, and high total tocopherols' content (1834-688 mg/kg), thanks to sacha inchi. The oxidative stability index (OSI) of the mixtures by the Rancimat method at 120 °C ranged from 0.46 to 8.80 h. The shelf-life of 1:1 tarwi/sacha inchi oil blend was 1.26 years; its entropy (-17.43 J/mol), enthalpy (107.04 kJ/mol), activation energy (110.24 kJ/mol) and Gibbs energy (113.76 kJ/mol) suggest low oxidation reaction rates and good stability. Hence, balanced blends of tarwi/sacha inchi oils can achieve optimal nutritional properties and enhanced shelf-life.


Assuntos
Euphorbiaceae , Ácidos Graxos Ômega-3 , Lupinus , Humanos , Óleos de Plantas/química , Euphorbiaceae/química , Sementes/química , Ácidos Graxos Ômega-3/análise , Valor Nutritivo , Estresse Oxidativo
5.
Fitoterapia ; 162: 105302, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36116613

RESUMO

Ten new prenylated flavonoids, named denticulains A-J (1-10), together with seven known prenylated flavonoids (11-17) were isolated from Macaranga denticulata. Their structures were elucidated on the basis of detailed spectroscopic analysis and by comparison with literature data. In addition, compounds 1 and 14 inhibited the proliferation of SW620 and HCT-116 cell lines with an IC50 value of 46.08 µM and 56.83 µM, respectively.


Assuntos
Antineoplásicos Fitogênicos , Euphorbiaceae , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Euphorbiaceae/química , Flavonoides/química , Flavonoides/farmacologia , Estrutura Molecular
6.
Molecules ; 27(13)2022 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-35807225

RESUMO

Tigilanol tiglate (EBC-46) is a small-molecule natural product under development for the treatment of cancers in humans and companion animals. The drug is currently produced by purification from the Australian rainforest tree Fontainea picrosperma (Euphorbiaceae). As part of a selective-breeding program to increase EBC-46 yield from F. picrosperma plantations, we investigated potential gene biomarkers associated with biosynthesis of EBC-46. Initially, we identified individual plants that were either high (>0.039%) or low EBC-46 (<0.008%) producers, then assessed their differentially expressed genes within the leaves and roots of these two groups by quantitative RNA sequencing. Compared to low EBC-46 producers, high-EBC-46-producing plants were found to have 145 upregulated genes and 101 downregulated genes in leaves and 53 upregulated genes and 82 downregulated genes in roots. Most of these genes were functionally associated with defence, transport, and biosynthesis. Genes identified as expressed exclusively in either the high or low EBC-46-producing plants were further validated by quantitative PCR, showing that cytochrome P450 94C1 in leaves and early response dehydration 7.1 and 2-alkenal reductase in roots were consistently and significantly upregulated in high-EBC-46 producers. In summary, this study has identified biomarker genes that may be used in the selective breeding of F. picrosperma.


Assuntos
Diterpenos , Euphorbiaceae , Marcadores Genéticos , Diterpenos/química , Ésteres/química , Euphorbiaceae/química , Euphorbiaceae/genética , Regulação da Expressão Gênica de Plantas , Genes de Plantas , Melhoramento Vegetal , Folhas de Planta/química , Folhas de Planta/genética , Raízes de Plantas/química , Raízes de Plantas/genética
7.
Chem Biol Interact ; 355: 109849, 2022 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-35150652

RESUMO

A phytochemical investigation of cytotoxic extract and fractions of Cnidoscolus quercifolius Pohl led to isolation of five terpenoids, including three lupane-type triterpenes (1-3) and two bis-nor-diterpenes (4-5). Compounds 4 (phyllacanthone) and 5 (favelanone) are commonly found in this species and have unique chemical structure. Although their cytotoxic activity against cancer cells has been previously reported, the anticancer potential of these molecules remains poorly explored. In this paper, the antimelanoma potential of phyllacanthone (PHY) was described for the first time. Cell viability assay showed a promising cytotoxic activity (IC50 = 40.9 µM) against chemoresistant human melanoma cells expressing the BRAF oncogenic mutation (A2058 cell line). After 72 h of treatment, PHY inhibited cell migration and induced apoptosis and cell cycle arrest (p < 0.05). Immunofluorescence assay showed that the pro-apoptotic effect of PHY is probably associated with tubulin depolymerization, resulting in cytoskeleton disruption of melanoma cells. Molecular docking investigation confirmed this hypothesis given that satisfactory interaction between PHY and tubulin was observed, particularly at the colchicine binding site. These results suggest PHY from C. quercifolius could be potential leader for the design of new antimelanoma drugs.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Diterpenos/química , Euphorbiaceae/química , Proteínas Proto-Oncogênicas B-raf/genética , Tubulina (Proteína)/metabolismo , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/metabolismo , Sítios de Ligação , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Movimento Celular , Colchicina/química , Colchicina/metabolismo , Diterpenos/metabolismo , Diterpenos/farmacologia , Euphorbiaceae/metabolismo , Humanos , Melanoma/metabolismo , Melanoma/patologia , Simulação de Acoplamento Molecular , Mutação , Casca de Planta/química , Casca de Planta/metabolismo , Extratos Vegetais/química , Proteínas Proto-Oncogênicas B-raf/metabolismo , Tubulina (Proteína)/química
8.
Sci Rep ; 12(1): 359, 2022 01 10.
Artigo em Inglês | MEDLINE | ID: mdl-35013404

RESUMO

The schweinfurthin family of natural compounds exhibit a unique and potent differential cytotoxicity against a number of cancer cell lines and may reduce tumor growth in vivo. In some cell lines, such as SF-295 glioma cells, schweinfurthins elicit cytotoxicity at nanomolar concentrations. However, other cell lines, like A549 lung cancer cells, are resistant to schweinfurthin treatment up to micromolar concentrations. At this time, the precise mechanism of action and target for these compounds is unknown. Here, we employ RNA sequencing of cells treated with 50 nM schweinfurthin analog TTI-3066 for 6 and 24 h to elucidate potential mechanisms and pathways which may contribute to schweinfurthin sensitivity and resistance. The data was analyzed via an interaction model to observe differential behaviors between sensitive SF-295 and resistant A549 cell lines. We show that metabolic and stress-response pathways were differentially regulated in the sensitive SF-295 cell line as compared with the resistant A549 cell line. In contrast, A549 cell had significant alterations in response genes involved in translation and protein metabolism. Overall, there was a significant interaction effect for translational proteins, RNA metabolism, protein metabolism, and metabolic genes. Members of the Hedgehog pathway were differentially regulated in the resistant A549 cell line at both early and late time points, suggesting a potential mechanism of resistance. Indeed, when cotreated with the Smoothened inhibitor cyclopamine, A549 cells became more sensitive to schweinfurthin treatment. This study therefore identifies a key interplay with the Hedgehog pathway that modulates sensitivity to the schweinfurthin class of compounds.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias Encefálicas/tratamento farmacológico , Metabolismo Energético/efeitos dos fármacos , Euphorbiaceae , Glioma/tratamento farmacológico , Neoplasias Pulmonares/tratamento farmacológico , RNA-Seq , Estilbenos/farmacologia , Células A549 , Antineoplásicos Fitogênicos/isolamento & purificação , Neoplasias Encefálicas/genética , Neoplasias Encefálicas/metabolismo , Neoplasias Encefálicas/patologia , Relação Dose-Resposta a Droga , Resistencia a Medicamentos Antineoplásicos , Metabolismo Energético/genética , Euphorbiaceae/química , Regulação Neoplásica da Expressão Gênica , Glioma/genética , Glioma/metabolismo , Glioma/patologia , Proteínas Hedgehog/genética , Proteínas Hedgehog/metabolismo , Humanos , Neoplasias Pulmonares/genética , Neoplasias Pulmonares/metabolismo , Neoplasias Pulmonares/patologia , Prenilação , Transdução de Sinais , Estilbenos/isolamento & purificação , Transcrição Gênica , Transcriptoma
9.
Bioorg Chem ; 119: 105511, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34847428

RESUMO

Euphoesulatin A (Eup A), a new jatrophane diterpenoid isolated from the Euphorbia esula L. (Euphorbiaceae), was reported to inhibit RANKL-induced osteoclastogenesis. However, the underlying mechanism and the effect in osteoporosis mouse model are still unclear. This study is the first to demonstrate that Eup A inhibits osteoclastogenesis in vitro and in vivo. Mechanistic analysis suggested that Eup A (3, 6, 12 µM) dose-dependently inhibited osteoclastogenesis by down-regulating the activation of NFATc1 and NF-κB and MAPKs signal pathways. Moreover, Eup A (10 mg/kg) significantly prevented bone loss in ovariectomized mice. This work provides in vitro and in vivo evidence that Eup A could be a potential candidate for the development of anti-osteoporosis agents.


Assuntos
Euphorbiaceae/química , Osteoclastos/efeitos dos fármacos , Osteoporose/prevenção & controle , Ligante RANK/metabolismo , Animais , Diferenciação Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos C57BL , Estrutura Molecular , NF-kappa B/metabolismo , Osteoporose/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Relação Estrutura-Atividade
10.
Naunyn Schmiedebergs Arch Pharmacol ; 395(2): 267-274, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34854946

RESUMO

Natural products have played a pivotal role for the discovery of anticancer drugs. Tonantzitlolones are flexibilan-type diterpenes rare in nature; therefore, few reports have shown antiviral and cytotoxic activities. This study aimed to investigate the in vivo antitumor action of Tonantzitlolone B (TNZ-B) and its toxicity. Toxicity was evaluated in mice (acute and micronucleus assays). Antitumor activity of TNZ-B (1.5 or 3 mg/kg intraperitoneally - i.p.) was assessed in Ehrlich ascites carcinoma model. Angiogenesis and reactive oxygen species (ROS) and nitric oxide (NO) production were also investigated, in addition to toxicological effects after 7-day treatment. The LD50 (lethal dose 50%) was estimated at around 25 mg/kg (i.p.), and no genotoxicity was recorded. TNZ-B reduced the Ehrlich tumor's volume and total viable cancer cell count (p < 0.001 for both). Additionally, TNZ-B reduced peritumoral microvessel density (p < 0.01), suggesting antiangiogenic action. Moreover, a decrease was observed on ROS (p < 0.05) and nitric oxide (p < 0.001) levels. No significant clinical findings were observed in the analysis of biochemical, hematological, and histological (liver and kidney) parameters. In conclusion, TNZ-B exerts antitumor and antiangiogenic effects by reducing ROS and NO levels and has weak in vivo dose-repeated toxicity. These data contribute to elucidate the antitumor action of TNZ-B and point the way for further studies with this natural compound as an anticancer drug.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Carcinoma de Ehrlich/tratamento farmacológico , Diterpenos/farmacologia , Euphorbiaceae/química , Compostos Macrocíclicos/farmacologia , Inibidores da Angiogênese/administração & dosagem , Inibidores da Angiogênese/farmacologia , Inibidores da Angiogênese/toxicidade , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/toxicidade , Linhagem Celular Tumoral , Diterpenos/administração & dosagem , Diterpenos/toxicidade , Relação Dose-Resposta a Droga , Feminino , Dose Letal Mediana , Compostos Macrocíclicos/administração & dosagem , Compostos Macrocíclicos/toxicidade , Camundongos , Testes para Micronúcleos , Óxido Nítrico/metabolismo , Espécies Reativas de Oxigênio/metabolismo
11.
Nat Prod Res ; 36(15): 3924-3930, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-33733942

RESUMO

A new highly oxygenated ent-atisane diterpenoid, namely excagallonoid A (1), together with five known analogues (2 - 6) were isolated from the leaves and twigs of Excoecaria agallocha. Their structures were elucidated on the basis of extensive spectroscopic analyses (HRESIMS, UV, IR, 1 D and 2 D NMR), and the absolute configurations of 1 and 5 were determined by single-crystal X-ray diffraction. Compound 1 represents the first example of an ent-atisane diterpenoid featuring a vicinal 2,3-diol moiety. Compounds 1 and 4 exhibited weak cytotoxicities in vitro against RKO colon cancer cells with IC50 values of 28.7 ± 1.98 and 32.6 ± 2.81 µM, respectively.


Assuntos
Diterpenos , Euphorbiaceae , Diterpenos/química , Diterpenos/farmacologia , Euphorbiaceae/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular
12.
Pak J Pharm Sci ; 34(4): 1437-1444, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34799319

RESUMO

This study aimed to optimize and develop the color lipstick formulation containing antioxidant-rich Thai Sacha inchi oil using full factorial experimental design. Antioxidant capacity of Sacha inchi oil was elucidated using DPPH and linoleic acid peroxidation assays. The y-tocopherol content of the oil was also determined by high-performance liquid chromatography. Developing the color lipstick, lipstick base was optimized through the variation of %Sacha inchi oil, Ozokerite and Carnauba wax ratio (O:C ratio) and %Fat. Concurrently, the influences of these factors on lipstick physical characteristics were analyzed by means of statistics. Thai Sacha inchi oil exerted a notable antioxidant capacity with the highest y-tocopherol content. The combined effect of all factors influenced on the variations of breaking point and hardness of the lipsticks. Otherwise, only the O: C ratio negatively affected on melting point. The color lipstick containing methyl methacrylate crosspolymer and stearyl dimethicone as texture enhancers, significantly provided a greater color transfer than the plain formulation. In conclusion, Thai Sacha inchi oil could be a promising antioxidant-rich oil for developing into color lipstick. To evolve the desirable lipstick, the optimum proportion of wax, fat and oil played a crucial role in both structural integrity as well as texture and spreadability.


Assuntos
Antioxidantes/química , Corantes/química , Cosméticos/química , Euphorbiaceae/química , Óleos de Plantas/química , Dureza , Tocoferóis/análise , Temperatura de Transição
13.
J Pharm Pharmacol ; 73(4): 553-559, 2021 Mar 08.
Artigo em Inglês | MEDLINE | ID: mdl-33793832

RESUMO

OBJECTIVE: To investigate the main chemical components and the anti-inflammatory activity of extracts of Adelia ricinella L. aerial parts. METHODS: Three extracts obtained by soxhlet extraction and ethanol/water mixtures were evaluated in their chemical composition by UPLC-DAD-MS/MS. The in vitro anti-inflammatory activity of the prepared extracts was assessed through three different assays: COX-1 and COX-2 enzymatic inhibition, cell-based COX assays on RAW264.7 macrophages (ATCC) measuring the COX-2 protein expression by Western blot and the measurement of the PGE2 concentration in the supernatants of the culture medium. Also was determinate the effect of the three extracts on the RAW 264.7 cell viability. KEY FINDINGS: Few differences in the phytochemical profile were found between the three prepared extracts, identifying a blend of thirteen flavonoids derived from luteolin and apigenin, with orientin as main constituent. Plant extracts (alcoholic and aqueous) did not affect the macrophage cell viability (IC50 > 256 µg/ml) and significantly reduced COX-1 and COX-2 enzyme activities. Additionally, COX-2 expression and PGE2 release were suppressed after 24 h of LPS stimulation and treatment with plant extracts (8-64 µg/ml). CONCLUSIONS: A. ricinella extracts showed the ability to reduce the inflammatory effect exerted by LPS in murine macrophages. However, further studies should confirm their anti-inflammatory activity.


Assuntos
Apigenina , Ciclo-Oxigenase 1 , Ciclo-Oxigenase 2 , Euphorbiaceae/química , Flavonoides , Glucosídeos , Luteolina , Animais , Anti-Inflamatórios/farmacologia , Apigenina/isolamento & purificação , Apigenina/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 1/análise , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/análise , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Luteolina/isolamento & purificação , Luteolina/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Células RAW 264.7
14.
J Pharm Pharmacol ; 73(3): 410-423, 2021 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-33793884

RESUMO

OBJECTIVES: Glochidion ellipticum Wight is a medicinal plant, rich in polyphenols, frequently used by the indigenous communities of Bangladesh and possess with multiple health benefits. It exerts anti-inflammatory and antidiarrheal properties, but the detailed chemical constituents are yet to be elucidated. METHODS: Glochidion ellipticum extracts were analyzed using ultra-high performance liquid chromatography/quadrupole time-of-flight mass spectrometry and then tested by both lipopolysaccharide (LPS) induced inflammation of Raw 264.7 macrophage cells and dextran sulfate sodium (DSS) induced acute colitis model. Blood serum was taken for fluorescein isothiocyanate-dextran (FITC-dextran) measurement and tissue samples were used to perform histology, RT-PCR and Western blotting. KEY FINDINGS: The extracts could lower the levels of nitric oxide (NO), reactive oxygen species (ROS) and pro-inflammatory cytokines significantly in LPS induced macrophage cells. The extracts could also reduce disease activity index (DAI) score, restore antioxidants and pro-oxidants and improve macroscopic and microscopic features of colonic tissues in DSS induced mice. Expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in protein level was markedly diminished (up to 51.21% and 71.11%, respectively) in the treatment groups compared to the model group of colitic mice. CONCLUSIONS: Our findings suggested that G. ellipticum extracts ameliorate DSS colitis via blocking nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) signaling pathway, which make them to be potential candidates for further research against inflammation and colitis.


Assuntos
Colite/tratamento farmacológico , Euphorbiaceae/química , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Colite/patologia , Ciclo-Oxigenase 2/metabolismo , Sulfato de Dextrana , Modelos Animais de Doenças , Feminino , Inflamação/tratamento farmacológico , Inflamação/patologia , Camundongos , Camundongos Endogâmicos C57BL , Óxido Nítrico Sintase Tipo II/metabolismo , Células RAW 264.7 , Transdução de Sinais/efeitos dos fármacos
15.
Molecules ; 26(4)2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33672019

RESUMO

Putrajeevak (Putranjiva roxburghii Wall.; synonym Drypetes roxburghii (Wall.) Hurus) seeds have been used since ancient times in the treatment of infertility in the Ayurvedic system of medicine in India. In this study, the oil component of Putrajeevak seeds (PJSO) was extracted using the supercritical fluid extraction (SCFE) method using liquid CO2 and the constituents were analyzed using gas chromatography-flame ionized detectorand high-performance thin-layer chromatography. PJSO contained trace amounts of ß-sitosterol with oleic and linoleic acids as the major fatty acid constituents. Male and female zebrafish were mutagenized with N-ethyl-N-nitrosourea (ENU) and fish that produced less than 20 viable embryos were selected for the study. SCFE oil extracts from the P. roxburghii seeds were used in this study to reverse fertility impairment. The mutant fish were fed with PJSO for a period of 14 days and the rates of fertility, conception, and fecundity were determined with wild-type healthy fish as a breeding partner. Treatment with PJSO increased the ovarian follicle count as well as the number of mature eggs, while reducing the number of ovarian cysts. Sperm count as well as sperm motility were greatly enhanced in the ENU-mutagenized male zebrafish when treated with PJSO. The results obtained in this study demonstrate the effectiveness of P. roxburghii seed oil in reversing impaired fertility in both male and female zebrafish models.


Assuntos
Cromatografia com Fluido Supercrítico/métodos , Euphorbiaceae/química , Fertilidade/fisiologia , Sementes/química , Peixe-Zebra/fisiologia , Animais , Modelos Animais de Doenças , Ácidos Graxos/análise , Ácidos Graxos/química , Feminino , Fertilidade/efeitos dos fármacos , Inflamação/tratamento farmacológico , Inflamação/patologia , Masculino , Ovário/fisiologia , Óvulo/fisiologia , Pelve/patologia , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Óleos de Plantas/uso terapêutico , Sitosteroides/análise , Sitosteroides/química , Testículo/efeitos dos fármacos , Testículo/patologia
16.
Biomolecules ; 11(2)2021 02 04.
Artigo em Inglês | MEDLINE | ID: mdl-33557215

RESUMO

Alchornea cordifolia (Schumach. & Thonn.) Müll. Arg. is a well-known African medicinal plant traditionally used for various healing purposes. In the present study, methanolic, ethyl acetate and infusion extracts of A. cordifolia leaves were studied for their total phenolic and flavonoid contents and screened for their chemical composition. Moreover, the enzyme (acetyl- and butyryl-cholinesterases, α-amylase, α-glucosidase, and tyrosinase) inhibitory and cytotoxicity activities on HepG2: human hepatocellular carcinoma cells, B16 4A5: murine melanoma cells, and S17: murine bone marrow (normal) cells of extracts were evaluated. Finally, components-targets and docking analyzes were conducted with the aim to unravel the putative mechanisms underlying the observed bio-pharmacological effects. Interestingly, the infusion and methanolic extracts showed significantly higher total phenolic and flavonoid contents compared with the ethyl acetate extract (TPC: 120.38-213.12 mg GAE/g and TFC: 9.66-57.18 mg RE/g). Besides, the methanolic extracts followed by the infusion extracts were revealed to contain a higher number of compounds (84 and 74 compounds, respectively), while only 64 compounds were observed for the ethyl acetate extract. Gallic acid, ellagic acid, shikimic acid, rutin, quercetin, myricetin, vitexin, quercitrin, kaempferol, and naringenin were among the compounds that were commonly identified in all the studied extracts. Additionally, the methanolic and infusion extracts displayed higher antioxidant capacity than ethyl acetate extract in all assays performed. In ABTS and DPPH radical scavenging assays, the methanol extract (500.38 mg TE/g for DPPH and 900.64 mg TE/g for ABTS) exhibited the best ability, followed by the water and ethyl acetate extracts. Furthermore, the extracts exhibited differential enzyme inhibitory profiles. In particular, the methanolic and infusion extracts showed better cytotoxic selectivity activity against human hepatocellular carcinoma cells. Overall, this study demonstrated A cordifolia to be a species worthy of further investigations, given its richness in bioactive phytochemicals and wide potentialities for antioxidants and pharmacological agents.


Assuntos
Antioxidantes/química , Euphorbiaceae/química , Euphorbiaceae/metabolismo , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Animais , Antioxidantes/farmacologia , Benzotiazóis/química , Compostos de Bifenilo/química , Carcinoma Hepatocelular/tratamento farmacológico , Biologia Computacional , Avaliação Pré-Clínica de Medicamentos , Flavonoides/farmacologia , Sequestradores de Radicais Livres , Células Hep G2 , Humanos , Quempferóis , Neoplasias Hepáticas/tratamento farmacológico , Melanoma Experimental , Metanol/química , Camundongos , Monofenol Mono-Oxigenase , Fenóis/química , Picratos/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plantas Medicinais , Ácidos Sulfônicos/química
17.
Int Endod J ; 54(7): 1142-1154, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33641170

RESUMO

AIM: To identify odontogenesis-promoting compounds and examine the molecular mechanism underlying enhanced odontoblast differentiation and tooth formation. METHODOLOGY: Five different nymphaeols, nymphaeol B (NB), isonymphaeol B (INB), nymphaeol A (NA), 3'-geranyl-naringenin (GN) and nymphaeol C (NC) were isolated from the fruit of Macaranga tanarius. The cytotoxic effect of nymphaeols on human DPSCs was observed using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The effect of nymphaeols on odontoblast differentiation was analysed with Alizarin Red S staining and odontoblast marker expression was assessed using real-time polymerase chain reaction and Western blot analysis. The molecular mechanism was investigated with Western blot analysis. In order to examine the effect of INB on dentine formation in the developing tooth germ, INB-soaked beads were placed under the tooth bud explants in the collagen gel; thereafter, the tooth bud explant-bead complexes were implanted into the sub-renal capsules for 3 weeks. Tooth root formation was analysed using micro-computed tomography and histological analysis. Data are presented as mean ± standard error (SEM) values of three independent experiments, and results are compared using a two-tailed Student's t-test. The data were considered to have statistical significance when the P-value was less than 0.05. RESULTS: Three of the compounds, NB, INB, and GN, did not exert a cytotoxic effect on human DPSCs. However, INB was most effective in promoting the deposition of calcium minerals in vitro (P < 0.001) and induced the expression of odontogenic marker genes (P < 0.05). Moreover, this compound strongly induced the phosphorylation of mitogen-activated protein (MAP) kinases and protein kinase B (AKT) (P < 0.05). The inhibition of p38 MAP, c-Jun N-terminal kinase (JNK), and AKT substantially suppressed the INB-induced odontoblast differentiation (P < 0.001). In addition, isonymphaeol B significantly induced the formation of dentine and elongation of the tooth root in vivo (P < 0.05). CONCLUSIONS: Prenylflavonoids, including INB, exerted stimulatory effects on odontoblast differentiation and tooth root and dentine formation via the MAP kinase and AKT signalling pathways. These results suggest that nymphaeols could stimulate the repair processes for dentine defects or injuries.


Assuntos
Diferenciação Celular/efeitos dos fármacos , Euphorbiaceae/química , Flavonoides/farmacologia , Odontoblastos/efeitos dos fármacos , Células-Tronco/efeitos dos fármacos , Células Cultivadas , Polpa Dentária/citologia , Humanos , Proteínas Quinases Ativadas por Mitógeno , Proteínas Proto-Oncogênicas c-akt , Transdução de Sinais , Raiz Dentária , Microtomografia por Raio-X
18.
Molecules ; 26(2)2021 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-33435518

RESUMO

Obesity is one of the risk factors associated with cardiovascular diseases, hypertension, abnormal liver function, diabetes, and cancers. Orlistat is currently available to treat obesity, but it is associated with adverse side effects. Natural resources are widely used for obesity treatment. Hence, this study aimed to investigate the anti-obesity activity of Elateriospermum tapos (E. tapos) shell extract in obesity induced Sprague Dawley rats. The rats' obesity was induced by a high-fat (HF) diet made up of 50% standard rat pellet, 20% milk powder, 6% corn starch, and 24% ghee and a cafeteria (CAF) diet such as chicken rolls, salty biscuits, cakes, and cheese snacks. A hot aqueous method for the extraction of E. tapos shells was applied by using 500 mL of distilled water for about 24 h. Various dosages of E. tapos shell extract (10 mg/kg, 100 mg/kg, and 200 mg/kg) were used. At the end of the study, body weight, caloric intake, organ weight, lipid profile, lipoprotein lipase (LPL) activity, and histopathology analysis were carried out. E. tapos shell extract treated groups showed a reduction in body weight, positive lipid-lowering effect, decrements in triglyceride accumulation and LPL activity, and positive improvement in histopathology analysis. A dose of 200 mg/kg showed the most effective result compared to 10 mg/kg and 100 mg/kg doses.


Assuntos
Fármacos Antiobesidade/farmacologia , Euphorbiaceae/química , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Administração Oral , Animais , Fármacos Antiobesidade/administração & dosagem , Fármacos Antiobesidade/química , Peso Corporal/efeitos dos fármacos , Dieta Hiperlipídica/efeitos adversos , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Obesidade/induzido quimicamente , Obesidade/patologia , Tamanho do Órgão/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
19.
Food Chem ; 337: 127771, 2021 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-32777564

RESUMO

Faveleira (Cnidoscolus quercifolius) is an emerging Brazilian plant, with seeds rich in edible oil. This study investigates physicochemical properties, chemical composition, thermal and oxidative stability, in vitro and in vivo toxicity, antioxidant, antinociceptive and anti-inflammatory activities of faveleira seed oil. It was observed that the oil has low acidity, value of peroxide, chlorophyll, carotenoids, ß-carotene and high concentrations of unsaturated fatty acids. In addition to presenting thermal and oxidative stability and high total phenolic content, with vanillin, eugenol and quercetin were predominating. The oil showed no toxicity in vitro and in vivo, and presented antioxidant, anti-inflammatory and antinociceptive activities. These findings provide relevant and appropriate conditions for processing of faveleira seed oil as functional food.


Assuntos
Euphorbiaceae/metabolismo , Óleos de Plantas/química , Analgésicos/química , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Animais , Antioxidantes/química , Brasil , Carotenoides/análise , Sobrevivência Celular/efeitos dos fármacos , Clorofila/análise , Euphorbiaceae/química , Ácidos Graxos/análise , Masculino , Camundongos , Dor/induzido quimicamente , Dor/prevenção & controle , Fenóis/análise , Óleos de Plantas/farmacologia , Óleos de Plantas/uso terapêutico , Células RAW 264.7 , Sementes/química , Sementes/metabolismo
20.
Food Chem ; 340: 127942, 2021 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-32890859

RESUMO

Sacha inchi (Plukenetia volubilis) oil (SI) is appreciated for its nutritional and sensorial characteristics. The aim of this study was to evaluate SI changes during French fries deep-frying at 170 °C or 180 °C up to 119 and 50 min, respectively; commercial soybean oil (SO) was tested as control. SI had high α-linolenic acid (53.8%), linoleic acid (33.4%) and total tocopherols (2540.1 mg/kg). During frying tocopherol content, oil stability and antioxidant capacity (ABTS, DPPH) decreased following zero-order kinetics; γ-tocopherol showed the strongest decrease. Notwithstanding the high SI unsaturation and the commercial antioxidant (TBHQ) in SO, SI showed slightly higher or similar hydrolysis (free fatty acids and diacylglycerols), similar primary (K232, oxidized-triacylglycerols) and lower secondary (K268, triacylglycerol oligopolymers) oxidation. Because of the high tocopherol content, SI showed lower degradation than SO. Thus, SI is suitable for short-term deep-frying; additionally, it may enhance the nutritional value and the flavour of fried foods.


Assuntos
Antioxidantes/análise , Culinária , Euphorbiaceae/química , Ácidos Graxos/análise , Óleos de Plantas/química , Tocoferóis/análise , Oxirredução
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