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1.
Chem Biol Drug Des ; 103(6): e14564, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38845574

RESUMO

The leaves of Araucaria cunninghamii are known to be nonedible and toxic. Previous studies have identified biflavones in various Araucaria species. This study aimed to investigate the in vitro cytotoxicity of the isolated compounds from Araucaria cunninghamii after metabolomics and network pharmacological analysis. Methanol extract of Araucaria cunninghamii leaves was subjected to bioassay-guided fractionation. The active fraction was analyzed using LC-HRMS, through strategic database mining, by comparing the data to the Dictionary of Natural Products to identify 12 biflavones, along with abietic acid, beta-sitosterol, and phthalate. Eight compounds were screened for network pharmacology study, where in silico ADME analysis, prediction of gene targets, compound-gene-pathway network and hierarchical network analysis, protein-protein interaction, KEGG pathway, and Gene Ontology analyses were done, that showed PI3KR1, EGFR, GSK3B, and ABCB1 as the common targets for all the compounds that may act in the gastric cancer pathway. Simultaneously, four biflavones were isolated via chromatography and identified through NMR as dimeric apigenin with varying methoxy substitutions. Cytotoxicity study against the AGS cell line for gastric cancer showed that AC1 biflavone (IC50 90.58 µM) exhibits the highest cytotoxicity and monomeric apigenin (IC50 174.5 µM) the lowest. Besides, the biflavones were docked to the previously identified targets to analyze their binding affinities, and all the ligands were found to bind with energy ≤-7 Kcal/mol.


Assuntos
Mineração de Dados , Metabolômica , Simulação de Acoplamento Molecular , Humanos , Linhagem Celular Tumoral , Folhas de Planta/química , Folhas de Planta/metabolismo , Farmacologia em Rede , Biflavonoides/química , Biflavonoides/farmacologia , Biflavonoides/metabolismo , Biflavonoides/isolamento & purificação , Traqueófitas/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Glicogênio Sintase Quinase 3 beta/metabolismo , Cromatografia Líquida , Subfamília B de Transportador de Cassetes de Ligação de ATP/metabolismo , Receptores ErbB/metabolismo , Receptores ErbB/antagonistas & inibidores , Espectrometria de Massas
2.
Ying Yong Sheng Tai Xue Bao ; 35(4): 877-885, 2024 Apr 18.
Artigo em Chinês | MEDLINE | ID: mdl-38884222

RESUMO

The natural abundance of stable carbon and nitrogen isotopes (δ13C and δ15N) in leaves can provide comprehensive information on the physiological and ecological processes of plants and has been widely used in ecological research. However, recent studies on leaf δ13C and δ15N have focused mainly on woody species, few studies have been conducted on herbs in different vegetation types, and their differences and driving factors are still unclear. In this study, we focused on the herbs in subalpine coniferous forests, alpine shrublands, and alpine mea-dows on the eastern Qinghai-Tibet Plateau, and investigated the differences in leaf δ13C and δ15N of herbs and the driving factors. The results showed that there were significant differences in leaf δ13C and δ15N values of herbs among different vegetation types, with the highest δ13C and δ15N values in alpine meadows, followed by alpine shrublands, and the lowest in subalpine coniferous forests. Using variation partitioning analysis, we revealed that differences in leaf δ13C and δ15N of herbs among various vegetation types were driven by both leaf functional traits and climate factors, with the contribution of leaf functional traits being relatively higher than that of climate factors. Hierarchical partitioning results indicated that mean annual temperature (MAT), chlorophyll content index, leaf nitrogen content per unit area (Narea), and leaf mass per area were the main drivers of leaf δ13C variations of herbs across different vegetation types, while the relative importance of Narea and MAT for variation in leaf δ15N of herbs was much higher than those other variables. There was a strong coupling relationship between leaf δ13C and δ15N as indicated by the result of the ordinary least squares regression. Our findings could provide new insights into understanding the key drivers of leaf δ13C and δ15N variations in herbs across different vegetation types.


Assuntos
Isótopos de Carbono , Ecossistema , Isótopos de Nitrogênio , Folhas de Planta , Folhas de Planta/química , Folhas de Planta/metabolismo , Isótopos de Nitrogênio/análise , Isótopos de Carbono/análise , Tibet , China , Florestas , Altitude , Árvores/crescimento & desenvolvimento , Árvores/metabolismo , Árvores/química , Traqueófitas/crescimento & desenvolvimento , Traqueófitas/química , Traqueófitas/metabolismo , Pradaria , Poaceae/crescimento & desenvolvimento , Poaceae/química , Poaceae/metabolismo
3.
Phytomedicine ; 128: 155536, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38513379

RESUMO

BACKGROUND: Lung cancer, a chronic and heterogeneous disease, is the leading cause of cancer-related death on a global scale. Presently, despite a variety of available treatments, their effectiveness is limited, often resulting in considerable toxicity and adverse effects. Additionally, the development of chemoresistance in cancer cells poses a challenge. Trilobolide-6-O-isobutyrate (TBB), a natural sesquiterpene lactone extracted from Sphagneticola trilobata, has exhibited antitumor effects. Its pharmacological properties in NSCLC lung cancer, however, have not been explored. PURPOSE: This study evaluated the impact of TBB on the A549 and NCI-H460 tumor cell lines in vitro, examining its antiproliferative properties and initial mechanisms of cell death. METHODS: TBB, obtained at 98 % purity from S. trilobata leaves, was characterized using chromatographic techniques. Subsequently, its impact on inhibiting tumor cell proliferation in vitro, TBB-induced cytotoxicity in LLC-MK2, THP-1, AMJ2-C11 cells, as well as its effects on sheep erythrocytes, and the underlying mechanisms of cell death, were assessed. RESULTS: In silico predictions have shown promising drug-likeness potential for TBB, indicating high oral bioavailability and intestinal absorption. Treatment of A549 and NCI-H460 human tumor cells with TBB demonstrated a direct impact, inducing significant morphological and structural alterations. TBB also reduced migratory capacity without causing toxicity at lower concentrations to LLC-MK2, THP-1 and AMJ2-C11 cell lines. This antiproliferative effect correlated with elevated oxidative stress, characterized by increased levels of ROS, superoxide anion radicals and NO, accompanied by a decrease in antioxidant markers: SOD and GSH. TBB-stress-induced led to changes in cell metabolism, fostering the accumulation of lipid droplets and autophagic vacuoles. Stress also resulted in compromised mitochondrial integrity, a crucial aspect of cellular function. Additionally, TBB prompted apoptosis-like cell death through activation of caspase 3/7 stressors. CONCLUSION: These findings underscore the potential of TBB as a promising candidate for future studies and suggest its viability as an additional component in the development of novel anticancer drugs prototypes.


Assuntos
Butiratos , Neoplasias Pulmonares , Sesquiterpenos , Sesquiterpenos/farmacologia , Butiratos/farmacologia , Traqueófitas/química , Linhagem Celular Tumoral , Neoplasias Pulmonares/tratamento farmacológico , Humanos , Células A549 , Células THP-1 , Testes de Toxicidade , Movimento Celular/efeitos dos fármacos , Caspase 3/metabolismo , Caspase 7/metabolismo , Apoptose/efeitos dos fármacos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Animais
4.
Nature ; 614(7947): 287-293, 2023 02.
Artigo em Inglês | MEDLINE | ID: mdl-36725928

RESUMO

The ability of the ancient Egyptians to preserve the human body through embalming has not only fascinated people since antiquity, but also has always raised the question of how this outstanding chemical and ritual process was practically achieved. Here we integrate archaeological, philological and organic residue analyses, shedding new light on the practice and economy of embalming in ancient Egypt. We analysed the organic contents of 31 ceramic vessels recovered from a 26th Dynasty embalming workshop at Saqqara1,2. These vessels were labelled according to their content and/or use, enabling us to correlate organic substances with their Egyptian names and specific embalming practices. We identified specific mixtures of fragrant or antiseptic oils, tars and resins that were used to embalm the head and treat the wrappings using gas chromatography-mass spectrometry analyses. Our study of the Saqqara workshop extends interpretations from a micro-level analysis highlighting the socio-economic status of a tomb owner3-7 to macro-level interpretations of the society. The identification of non-local organic substances enables the reconstruction of trade networks that provided ancient Egyptian embalmers with the substances required for mummification. This extensive demand for foreign products promoted trade both within the Mediterranean8-10 (for example, Pistacia and conifer by-products) and with tropical forest regions (for example, dammar and elemi). Additionally, we show that at Saqqara, antiu and sefet-well known from ancient texts and usually translated as 'myrrh' or 'incense'11-13 and 'a sacred oil'13,14-refer to a coniferous oils-or-tars-based mixture and an unguent with plant additives, respectively.


Assuntos
Embalsamamento , Múmias , Humanos , Antigo Egito , Embalsamamento/economia , Embalsamamento/história , Embalsamamento/métodos , Cromatografia Gasosa-Espectrometria de Massas , História Antiga , Múmias/história , Resinas Vegetais/análise , Resinas Vegetais/história , Cerâmica/química , Cerâmica/história , Alcatrões/análise , Alcatrões/história , Óleos de Plantas/análise , Óleos de Plantas/história , Região do Mediterrâneo , Clima Tropical , Florestas , Traqueófitas/química , Comércio/história
5.
Food Funct ; 14(1): 250-261, 2023 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-36484340

RESUMO

Castanopsis is diffusely spread in tropical and subtropical regions and is an important nectar source plant in China. The Castanopsis honey (CH) is characterized by its bitter taste. However, its composition and functions remain unclear. In this study, the physicochemical parameters, chemical composition, and antioxidant capacity of CH were comprehensively investigated, with the anti-inflammatory effects of the Castanopsis honey extract (CHE) evaluated based on the RAW 264.7 cell inflammatory model. The results revealed a high level of quality in CH based on the quality standards. Among a total of 84 compounds identified in CH, 5 high response compounds and 29 phenols were further quantified by UPLC-Q/TOF-MS. The high content of phenylethylamine (117.58 ± 64.81 mg kg-1) was identified as a potential marker of CH. Furthermore, the CH showed evident antioxidant activities, and the anti-inflammatory activities of CHE were observed to inhibit the release of nitric oxide (NO) and reduce the content of tumor necrosis factor alpha (TNF-α) and improve the content of interleukin-10 (IL-10) by regulating the NF-κB pathway. Our study indicates that CH has sound physicochemical properties and biological activities with a high level of quality, providing strong experimental evidence to support the further economic and agricultural development and application of CH.


Assuntos
Antioxidantes , Mel , Traqueófitas , Animais , Camundongos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Antioxidantes/farmacologia , Antioxidantes/química , Lipopolissacarídeos/farmacologia , NF-kappa B/genética , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Células RAW 264.7 , Fator de Necrose Tumoral alfa/metabolismo , Traqueófitas/química
6.
Molecules ; 26(19)2021 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-34641284

RESUMO

To elucidate the chemical linkages between lignin and carbohydrates in ginkgo cell walls, 13C-2H-enriched cell wall-dehydrogenation polymers (CW-DHP) were selectively prepared with cambial tissue from Ginkgo biloba L. by feeding D-glucose-[6-2H2], coniferin-[α-13C], and phenylalanine ammonia-lyase (PAL) inhibitor. The abundant detection of 13C and 2H confirmed that D-glucose-[6-2H2] and coniferin-[α-13C] were involved in the normal metabolism of ginkgo cambial cells that had been effectively labelled with dual isotopes. In the ginkgo CW-DHP, ketal and ether linkages were formed between the C-α of lignin side chains and carbohydrates, as revealed by solid state CP/MAS 13C-NMR differential spectroscopy. Furthermore, the DMSO/TBAH ionic liquids system was used to fractionate the ball-milled CW-DHP into three lignin-carbohydrate complex (LCC) fractions: glucan-lignin complex (GL), glucomannan-lignin complex (GML), and xylan-lignin complex (XL). The XRD determination indicated that the cellulose type I of the GL was converted into cellulose type II during the separation process. The molecular weight was in the order of Ac-GL > Ac-GML > XL. The 13C-NMR and 1H-NMR differential spectroscopy of 13C-2H-enriched GL fraction indicated that lignin was linked with cellulose C-6 by benzyl ether linkages. It was also found that there were benzyl ether linkages between the lignin side chain C-α and glucomannan C-6 in the 13C-2H-enriched GML fraction. The formation of ketal linkages between the C-α of lignin and xylan was confirmed in the 13C-2H-enriched XL fraction.


Assuntos
Carboidratos/química , Ginkgo biloba/química , Lignina/química , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Parede Celular/química , Glucanos/química , Glucose/química , Estrutura Molecular , Espectroscopia de Prótons por Ressonância Magnética , Traqueófitas/química , Xilanos/química
7.
J Nat Prod ; 84(9): 2511-2524, 2021 Sep 24.
Artigo em Inglês | MEDLINE | ID: mdl-34491068

RESUMO

The class of plant exudates that contain the phenol functionality, termed phenolics, is defined, surveyed, and characterized by solid-state 13C NMR spectroscopy and by solution-state 1H NMR spectroscopy. Materials in this group are identified by the phenolic 13C resonance (from the ipso carbon of ArOH) at δ 145-160 (δ 160-167 for ArOR). The resonance patterns define several subclasses based on the collective similarity of their 13C spectra, specifically, aloetics from the genus Aloe, guaiacs from the genus Guaiacum and other eurosid and conifer genera, xanthics from the genus Garcinia, and kinos from the genus Eucalyptus and many other genera. Phenolic exudates often are mixed with terpenoid materials (the building block of exudates known as resins) and carbohydrates (the building block of exudates known as gums) to form hybrid subgroups such as guaiac gums, guaiac resins, and kino resins. There are numerous phenolic exudates not affiliated with any of these groups, both as pure phenolics and as hybrids (phenolic resins, phenolic gum resins, and phenolic waxes).


Assuntos
Fenóis/química , Exsudatos de Plantas/química , Resinas Vegetais/química , Aloe/química , Eucalyptus , Garcinia/química , Guaiacum/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Traqueófitas/química
8.
Molecules ; 26(14)2021 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-34299601

RESUMO

Species of Podocarpus are used traditionally in their native areas for the treatment of fevers, asthma, coughs, cholera, chest pain, arthritis, rheumatism, and sexually transmitted diseases. To identify natural products having efficacy against inflammatory bowel disease (IBD), we identified a new, 16-hydroxy-4ß-carboxy-O-ß-D-glucopyranosyl-19-nor-totarol (4) together with three known diterpenoids from P. macrophyllus. Furthermore, all the extracts, fractions, and isolates 1-4 were investigated for their anti-inflammatory effects by assessing the expression on nitric oxide (NO) production and proinflammatory cytokines in lipopolysaccharide (LPS)-stimulated RAW 264.7 and HT-29 cells. Among them, nagilactone B (2) exhibited a potent anti-inflammatory effect against NO production on RAW 264.7 cells; therefore, nagilactone B was further assessed for anti-inflammatory activity. Western blot analysis revealed that nagilactone B significantly decreased the expression of LPS-stimulated protein, inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2, and phosphorylated extracellular regulated kinase (pERK)1/2. In addition, nagilactone B downregulated tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-8 levels in LPS-induced macrophages and colonic epithelial cells. To our best knowledge, this is the first report on the inhibitory effect of nagilactone B (pure state) and rakanmakilactone G against NO production in LPS-stimulated RAW 264.7 cells. Thus, diterpenoids isolated from P. macrophyllus could be employed as potential therapeutic phytochemicals for IBD.


Assuntos
Anti-Inflamatórios/farmacologia , Diterpenos/farmacologia , Mediadores da Inflamação/antagonistas & inibidores , Inflamação/tratamento farmacológico , Lipopolissacarídeos/imunologia , Traqueófitas , Animais , Anti-Inflamatórios/isolamento & purificação , Diterpenos/isolamento & purificação , Células HT29 , Humanos , Inflamação/imunologia , Mediadores da Inflamação/imunologia , Doenças Inflamatórias Intestinais/tratamento farmacológico , Doenças Inflamatórias Intestinais/imunologia , Camundongos , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Células RAW 264.7 , Traqueófitas/química
9.
Molecules ; 26(10)2021 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-34070179

RESUMO

Conifers have long been recognized for their therapeutic potential in different disorders. Alkaloids, terpenes and polyphenols are the most abundant naturally occurring phytochemicals in these plants. Here, we provide an overview of the phytochemistry and related commercial products obtained from conifers. The pharmacological actions of different phytochemicals present in conifers against bacterial and fungal infections, cancer, diabetes and cardiovascular diseases are also reviewed. Data obtained from experimental and clinical studies performed to date clearly underline that such compounds exert promising antioxidant effects, being able to inhibit cell damage, cancer growth, inflammation and the onset of neurodegenerative diseases. Therefore, an attempt has been made with the intent to highlight the importance of conifer-derived extracts for pharmacological purposes, with the support of relevant in vitro and in vivo experimental data. In short, this review comprehends the information published to date related to conifers' phytochemicals and illustrates their potential role as drugs.


Assuntos
Florestas , Compostos Fitoquímicos/uso terapêutico , Traqueófitas/química , Animais , Ensaios Clínicos como Assunto , Humanos , Neuroproteção/efeitos dos fármacos , Compostos Fitoquímicos/química , Extratos Vegetais/uso terapêutico
10.
Drug Dev Res ; 82(8): 1169-1181, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-33983647

RESUMO

Urease plays a significant role in the pathogenesis of urolithiasis pyelonephritis, urinary catheter encrustation, hepatic coma, hepatic encephalopathy, and peptic acid duodenal ulcers. Salvinia molesta was explored to identify new bioactive compounds with particular emphasis on urease inhibitors. The aqueous methanol extract was fractionated using solvents of increasing polarity. A series of column chromatography and later HPLC were performed on butanol extract. The structures of the resulting pure compounds were resolved using NMR (1D and 2D), infrared, and mass spectroscopy. The novel isolate was evaluated for antioxidant activity (using DPPH, superoxide anion radical scavenging, oxidative burst, and Fe+2 chelation assays), anti-glycation behavior, anticancer activity, carbonic anhydrase inhibition, phosphodiesterase inhibition, and urease inhibition. One new glucopyranose derivative 6'-O-(3,4-dihydroxybenzoyl)-4'-O-(4-hydroxybenzoyl)-α/ß-D-glucopyranoside (1) and four known glycosides were identified. Glycoside 1 demonstrated promising antioxidant potential with IC50 values of 48.2 ± 0.3, 60.3 ± 0.6, and 42.1 ± 1.8 µM against DPPH, superoxide radical, and oxidative burst, respectively. Its IC50 in the Jack bean urease inhibition assay was 99.1 ± 0.8 µM. The mechanism-based kinetic studies presented that compound 1 is a mixed-type inhibitor of urease with a Ki value of 91.8 ± 0.1 µM. Finally, molecular dynamic simulations exploring the binding mode of compound 1 with urease provided quantitative agreement between estimated binding free energies and the experimental results. The studies corroborate the use of compound 1 as a lead for QSAR studies as an antioxidant and urease inhibitor. Moreover, it needs to be further evaluated through the animal model, that is, in vivo or tissue culture-based ex-vivo studies, to establish their therapeutic potential against oxidative stress phosphodiesterase-II and urease-induced pathologies.


Assuntos
Antioxidantes/isolamento & purificação , Extratos Vegetais/análise , Traqueófitas/química , Urease/antagonistas & inibidores , Antioxidantes/farmacologia , Inibidores Enzimáticos/isolamento & purificação , Medições Luminescentes , Simulação de Acoplamento Molecular , Inibidores de Fosfodiesterase/isolamento & purificação , Urease/química
11.
Molecules ; 26(4)2021 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-33572261

RESUMO

Chromatographic purification of the alcoholic extract from the aerial parts of the Saudi plant Nuxia oppositifolia (Hochst.), Benth., resulted in five isolated phenolic compounds. Two flavones, hispidulin (1) and jaceosidin (2), and the phenylethanoid glycosides, verbascoside (3), isoverbascoside (4), and conandroside (5), were identified and their chemical structures were determined by spectroscopic analyses. The insecticidal activity of compounds 1 and 2, in addition to 11 compounds isolated in a previous research (6-16), was evaluated against the Yellow Fever mosquito, Aedes aegypti. Four compounds displayed adulticidal activity with LD50 values of 2-2.3 µg/mosquito. Free radical scavenging properties of the plant extracts and compounds (1-5) were evaluated by measuring the 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonate radical cation (ABTS•+) scavenging activity. All compounds exhibited notable activity, compared with the positive control, l-Ascorbic acid. This study suggests that N. oppositifolia could be a promising source of secondary metabolites, some with lethal adulticidal effect against Ae. aegypti.


Assuntos
Aedes/crescimento & desenvolvimento , Antioxidantes/farmacologia , Sequestradores de Radicais Livres/farmacologia , Inseticidas/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Traqueófitas/química , Aedes/efeitos dos fármacos , Animais , Arábia Saudita
12.
Molecules ; 26(2)2021 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-33477743

RESUMO

Marine aquaculture development is recently impeded by parasitic leech Zeylanicobdella arugamensis (Hirudinea, Piscicolidae) in Sabah, Malaysia. The parasitic leech infests a variety of cultured fishes in aquaculture facilities. In this study, we evaluated the antiparasitic activity of the chromatographic fractions of the medicinal plant Nephrolepis biserrata methanol extract against Z. arugamensis and highlighted the potential metabolites responsible for the antiparasitic properties through liquid chromatography (LC)-quadrupole time-of-flight (QTOF)-mass spectrometry (MS) analysis. Out of seven fractions obtained through flash column chromatography techniques, three fractions demonstrated antiparasitic properties. Significant parasitic mortality was indicated by fraction 3 at a concentration of 2.50 mg/mL, all the leeches were killed in a time limit of 1.92 ± 0.59 min. followed by fraction 4 (14 mg/mL) in 34.57 ± 3.39 and fraction 5 (15.3 mg/mL) in 36.82 ± 4.53 min. LC-QTOF-MS analysis indicated the presence of secondary metabolites including phytosphingosine (6), pyrethrosin (1), haplophytine (9), ivalin (2), warburganal (3), isodomedin (4) and pheophorbide a (16), representing sphingoid, alkaloid, terpenoid, phenolic and flavonoid groups. Thus, our study indicated that the chromatographic fractions of N. biserrata demonstrated significant antiparasitic activity against the marine parasitic leeches due to the presence of potent antiparasitic bioactive compounds.


Assuntos
Antiparasitários/química , Antiparasitários/farmacologia , Cromatografia Líquida , Espectrometria de Massas , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Traqueófitas/química
13.
BMC Complement Med Ther ; 21(1): 35, 2021 Jan 14.
Artigo em Inglês | MEDLINE | ID: mdl-33446155

RESUMO

INTRODUCTION: Water-soluble, but not lipid-soluble, extract of Dicranopteris linearis leaves has been proven to possess hepatoprotective activity. The present study aimed to validate the hepatoprotective and antioxidant activities, and phytoconstituents of lipid-soluble (chloroform) extract of D. linearis leaves. METHODS: The extract of D. linearis leaves (CEDL; 50, 250 and 500 mg/kg) was orally administered to rats for 7 consecutive days followed by the oral administration of 3 g/kg PCM to induce liver injury. Blood was collected for liver function analysis while the liver was obtained for histopathological examination and endogenous antioxidant activity determination. The extract was also subjected to antioxidant evaluation and phytochemicals determination via phytochemical screening, HPLC and UPLC-HRMS analyses. RESULTS: CEDL exerted significant (p < 0.05) hepatoprotective activity at 250 and 500 mg/kg and significantly (p < 0.05) reversed the PCM-induced decrease in rat's liver endogenous antioxidant (catalase and superoxide dismutase) level. CEDL possessed a high antioxidant capacity when measured using the ORAC assay, but a low total phenolic content value and radical scavenging activity as confirmed via several radical scavenging assays, which might be attributed particularly to the presence of triterpenes. Phytochemicals screening demonstrated the presence of triterpenes and flavonoids, while UPLC-HRMS analysis showed the presence of polyphenols belonging to the hydroxybenzoic acids, hydroxycinammates and flavonoid groups. DISCUSSION AND CONCLUSION: Lipid-soluble bioactive compounds of CEDL demonstrated hepatoprotective effect against PCM intoxication partly via the modulation of the endogenous antioxidant defense system, and exerted high antioxidant capacity. Further investigation is warranted to identify the potential hepatoprotective leads from CEDL for future drug development.


Assuntos
Acetaminofen/toxicidade , Doença Hepática Induzida por Substâncias e Drogas , Polifenóis , Traqueófitas/química , Triterpenos , Animais , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Clorofórmio/química , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Polifenóis/química , Polifenóis/farmacologia , Ratos , Ratos Sprague-Dawley , Triterpenos/química , Triterpenos/farmacologia
14.
Curr Opin Insect Sci ; 43: 97-102, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33359166

RESUMO

Bark beetles (family: Curculionidae; subfamily: Scolytinae) in the Dendroctonus and Ips genera are the most destructive forest pests in the Northern hemisphere. They use cytochromes P450 (P450s) to detoxify tree-produced terpenes to produce pheromones, in de novo pheromone production and to oxidize odorants on antennae. Many Dendroctonus spp. use trans-verbenol as an aggregation pheromone, and it is formed from host-tree produced α-pinene hydroxylated by CYP6DE1 during larval stages, stored as verbenyl ester of fatty acids, and then released when the female begins feeding on a new host tree. Ips spp. hydroxylate de novo produced myrcene to form ipsdienol. Subsequent steps form the appropriate enantiomeric composition of ipsdienol and convert ipsdienol to ipsenol. In this article we review recent progress in elucidating the functions of P450s in Ips and Dendroctonus species and in doing so provide insights into the role of these enzymes in host phytochemical detoxification and pheromone production.


Assuntos
Sistema Enzimático do Citocromo P-450 , Inativação Metabólica , Gorgulhos/enzimologia , Gorgulhos/metabolismo , Álcoois/metabolismo , Animais , Monoterpenos Bicíclicos/metabolismo , Feromônios , Terpenos/metabolismo , Traqueófitas/química
15.
Nat Prod Res ; 35(18): 3151-3155, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31736362

RESUMO

The number of colon cancer patients is increasing, and new alternatives for treatment are important. We focused on the sesquiterpene lactone onoseriolide from Hedyosmum racemosum, which is widely used in traditional medicine. This compound was evaluated to determine its cytotoxic effect and the mechanism of cell death that is induced in the human colon cancer cell line RKO. A dose-dependent decrease in cell viability was observed. p53 expression increased followed by an increase in p21 expression, which is involved in cell cycle arrest in the G2/M phase. Caspase-3 activation and PARP-1 cleavage, which are apoptotic markers, were also monitored. Autophagy markers were also studied, and Beclin 1 was downregulated, while LC-3II increased in a dose-dependent manner. There were no changes in SQSTM1/p62 regulation. Onoseriolide exerts cytotoxic and cytostatic effects, activating the autophagy pathway as a protective mechanism and apoptosis as the cell death pathway.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias do Colo , Sesquiterpenos , Traqueófitas/química , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose , Linhagem Celular Tumoral , Proliferação de Células , Neoplasias do Colo/tratamento farmacológico , Humanos , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia
16.
Molecules ; 27(1)2021 Dec 23.
Artigo em Inglês | MEDLINE | ID: mdl-35011299

RESUMO

The current study was intended to explore the phytochemical profiling and therapeutic activities of Putranjiva roxburghii Wall. Crude extracts of different plant parts were subjected to the determination of antioxidant, antimicrobial, antidiabetic, cytotoxic, and protein kinase inhibitory potential by using solvents of varying polarity ranges. Maximum phenolic content was notified in distilled water extracts of the stem (DW-S) and leaf (DW-L) while the highest flavonoid content was obtained in ethyl acetate leaf (EA-L) extract. HPLC-DAD analysis confirmed the presence of various polyphenols, quantified in the range of 0.02 ± 0.36 to 2.05 ± 0.18 µg/mg extract. Maximum DPPH scavenging activity was expressed by methanolic extract of the stem (MeOH-S). The highest antioxidant capacity and reducing power was shown by MeOH-S and leaf methanolic extract (MeOH-L), respectively. Proficient antibacterial activity was shown by EA-L extract against Bacillus subtilis and Escherichia coli. Remarkable α-amylase and α-glucosidase inhibition potential was expressed by ethyl acetate fruit (EA-F) and n-Hexane leaf (nH-L) extracts, respectively. In case of brine shrimp lethality assay, 41.67% of the extracts (LC50 < 50 µg/mL) were considered as extremely cytotoxic. The test extracts also showed mild antifungal and protein kinase inhibition activities. The present study explores the therapeutic potential of P. roxburghii and calls for subsequent studies to isolate new bioactive leads through bioactivity-guided isolation.


Assuntos
Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Polifenóis/análise , Polifenóis/farmacologia , Traqueófitas/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/análise , Antioxidantes/farmacologia , Fracionamento Químico/métodos , Cromatografia Líquida de Alta Pressão , Ativação Enzimática , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/farmacologia , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia
17.
Bol. latinoam. Caribe plantas med. aromát ; 20(1): 28-37, 2021. ilus, tab
Artigo em Inglês | LILACS | ID: biblio-1284403

RESUMO

Several investigations have demonstrated Dicranopteris linearis (Burm.f.) Underw. (Gleicheniaceae) plant extracts possess numerous health-promoting properties. This review is aimed to summarize and highlight the potential possess by D. linearisto be developed into future pharmacological entity especially as anticancer agent. This study used several electronic search engines to compile and integrate a number of scientific publications related with D. linearis. Scientifically, D. linearishas been reported to have antinociceptive, anti-inflammatory, antipyretic, chemopreventive and antioxidant properties which can be linked to its potential to treat various kinds of ailments including inflammatory-related diseases and cancer. A number of scientific evidences related with anticancer studies suggested the ability of D. linearis-based phytochemicals to act as potent anticancer lead compounds. In conclusion, D. linearis has the potential to be developed into potent anticancer agent as depicted by a number of isolated phytochemicals which can work synergistically to contribute to its anticancer properties.


Varias investigaciones han demostrado que los extractos de la planta Dicranopteris linearis (Burm.f.) Underw. (Gleicheniaceae) poseen numerosas propiedades promotoras de la salud. El objetivo de esta revisión es resumir y resaltar el potencial que posee D. linearispara convertirse en una entidad farmacológica futura, especialmente como agente anticancerígeno. Este estudio utilizó varios motores de búsqueda electrónicos para compilar e integrar una serie de publicaciones científicas relacionadas con D. linearis. Científicamente, se ha informado que D. linearis tiene propiedades antinociceptivas, antiinflamatorias, antipiréticas, quimiopreventivas y antioxidantes que pueden estar vinculadas a su potencial para tratar varios tipos de dolencias, incluidas las enfermedades asociadas a inflamación y el cáncer. Una serie de evidencias científicas relacionadas con los estudios anticancerosos sugirieron la capacidad de los fitoquímicos basados en D. linearis para actuar como potentes compuestos anticancerígenos. En conclusión, D. linearis tiene el potencial de convertirse en una fuente de potentes agentes anticancerígeno, como se describe en una serie de fitoquímicos aislados que pueden actuar de forma sinérgica para contribuir a sus propiedades anticancerígenas.


Assuntos
Humanos , Plantas Medicinais , Extratos Vegetais/uso terapêutico , Traqueófitas/química , Antineoplásicos/uso terapêutico , Extratos Vegetais/química , Compostos Fitoquímicos , Antineoplásicos/química , Antioxidantes
18.
Int J Mol Sci ; 21(23)2020 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-33261095

RESUMO

The use of metallic nanoparticles in engineering and biomedicine disciplines has gained considerable attention. Scientists are exploring new synthesis protocols of these substances considering their small size and lucrative antimicrobial potential. Among the most economical techniques of synthesis of metallic nanoparticles via chemical routes, which includes the use of chemicals as metal reducing agents, is considered to generate nanoparticles possessing toxicity and biological risk. This limitation of chemically synthesized nanoparticles has engendered the exploration for the ecofriendly synthesis process. Biological or green synthesis approaches have emerged as an effective solution to address the limitations of conventionally synthesized nanoparticles. Nanoparticles synthesized via biological entities obtained from plant extracts exhibit superior effect in comparison to chemical methods. Recently, conifer extracts have been found to be effective in synthesizing metallic nanoparticles through a highly regulated process. The current review highlights the importance of conifers and its extracts in synthesis of metallic nanoparticles. It also discusses the different applications of the conifer extract mediated metallic nanoparticles.


Assuntos
Química Verde , Nanopartículas Metálicas/química , Traqueófitas/química , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia
19.
Molecules ; 25(23)2020 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-33255853

RESUMO

Breynia retusa (Dennst.) Alston (also known as Cup Saucer plant) is a food plant with wide applications in traditional medicine, particularly in Ayurveda. Extracts obtained with four solvents (dichloromethane, methanol, ethyl acetate and water), from three plant parts, (fruit, leaf and bark) were obtained. Extracts were tested for total phenolic, flavonoid content and antioxidant activities using a battery of assays including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating. Enzyme inhibitory effects were investigated using acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase as target enzymes. Results showed that the methanolic bark extract exhibited significant radical scavenging activity (DPPH: 202.09 ± 0.15; ABTS: 490.12 ± 0.18 mg Trolox equivalent (TE)/g), reducing potential (FRAP: 325.86 ± 4.36: CUPRAC: 661.82 ± 0.40 mg TE/g) and possessed the highest TAC (3.33 ± 0.13 mmol TE/g). The methanolic extracts were subjected to LC-DAD-MSn and NMR analysis. A two-column LC method was developed to separate constituents, allowing to identify and quantify forty-four and fifteen constituents in bark and fruits, respectively. Main compound in bark was epicatechin-3-O-sulphate and isolation of compound was performed to confirm its identity. Bark extract contained catechins, procyanidins, gallic acid derivatives and the sulfur containing spiroketal named breynins. Aerial parts mostly contained flavonoid glycosides. Considering the bioassays, the methanolic bark extract resulted a potent tyrosinase (152.79 ± 0.27 mg kojic acid equivalent/g), α-amylase (0.99 ± 0.01 mmol acarbose equivalent ACAE/g) and α-glucosidase (2.16 ± 0.01 mmol ACAE/g) inhibitor. In conclusion, methanol is able to extract the efficiently the phytoconstituents of B. retusa and the bark is the most valuable source of compounds.


Assuntos
Frutas/química , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Traqueófitas/química , Antioxidantes/química , Antioxidantes/farmacologia , Cromatografia , Cromatografia Líquida , Mineração de Dados , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Estrutura Molecular , Compostos Fitoquímicos/química , Extratos Vegetais/farmacologia
20.
Molecules ; 25(21)2020 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-33142839

RESUMO

Stratiotes aloides L. is common water plant in central Poland. Due to its expansive character, S. aloides L. can strongly affect the functioning of aquatic ecosystems. S. aloides L. was an important famine plant in central Poland. This plant was commonly collected and cooked until the turn of the 20th century. It has also been used to heal wounds, especially when these are made by an iron implement. The objective of the present work was to study the phenolic profile in the leaves and roots of S. aloides as well as their antioxidant potential and ability to inhibit lipoxygenase (LOX) in the light of their potential bioaccessibility. The dominant compound in its leaves was luteolin-7-O-hexoside-glucuronide (5.84 mg/g DW), whereas the dominant root component was chrysoeriol-7-O-hexoside-glucuronide (0.83 mg/g DW). Infusions from leaves, roots, and their 1:1 (v/v) mixture contained potentially bioaccessible antiradical compounds. S. aloides is a good source of water-extractable reductive compounds. Especially valuable are the leaves of this plant. The roots of S. aloides contained very active hydrophilic compounds able to chelate metal ions. However, their potential bioaccessibility was relatively low. The hydrophilic compounds from the leaves were the most effective XO inhibitors (EC50 = 9.91 mg DW/mL). The water-extractable compounds derived from the leaves and roots acted as uncompetitive LOX inhibitors.


Assuntos
Antioxidantes/química , Extratos Vegetais/química , Folhas de Planta/química , Raízes de Plantas/química , Traqueófitas/química , Antioxidantes/farmacologia , Cromatografia Líquida de Alta Pressão , Ecossistema , Glucuronídeos/química , Lipoxigenase/metabolismo , Inibidores de Lipoxigenase/química , Inibidores de Lipoxigenase/farmacologia , Modelos Químicos , Fenóis/química , Fenóis/metabolismo , Extratos Vegetais/farmacologia , Espectrometria de Massas em Tandem , Água , Xantina Oxidase/metabolismo
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