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1.
Artigo em Inglês | MEDLINE | ID: mdl-32032821

RESUMO

Nowadays, the increased prevalence of sub-health significantly affects human health worldwide. Suppressed sub-healthy by dietotherapy/herbal remedy which showed excellent safety profile, low cost and effectiveness, is an effective way. In this research, the fingerprint and antioxidant activity of Sabia parviflora were obtained by HPLC instrument and DPPH, ABTS, FRAP heatmap assays. And the antioxidant active substances were selected by spectrum-effect relationship. The results showed that significant differences in chemical compositions of samples from different sources, and EW, EE extracts had strong antioxidant activity. The antioxidant activity of Sabia parviflora was mainly determined by the complex interaction of various flavonoids (promoting, competing or antagonizing). These findings revealed that the abundant flavonoids in Sabia parviflora had significant antioxidant activity and could be potential antioxidants. With therapeutic potential for sub-health, this special tea might provide dietotherapy/herbal to remedy sub-healthy population.


Assuntos
Antioxidantes/análise , Medicamentos de Ervas Chinesas/química , Flavonoides/análise , Magnoliopsida/química , Folhas de Planta/química , Antocianinas/análise , Cromatografia Líquida de Alta Pressão , Quempferóis/análise , Oligossacarídeos/análise , Quercetina/análogos & derivados , Quercetina/análise , Rutina/análise
2.
J Photochem Photobiol B ; 204: 111587, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32062387

RESUMO

Although the photothermal therapy (PTT) has achieved tremendous progress in the recent times, still it has to improve an extensive way to achieve the efficient targeted photothermal removal of the tumor cells. Owing to this requirement, we demonstrated a novel class of reduced graphene oxide based photothermal therapeutic agent for the ablation of lung cancer cells (A549). A single step bio facile fabrication of graphene nanosheets using Memecylon edule leaf extract intermediated reduction of Graphene Oxide (GO). This process does not include the utilization of any toxic or harmful reducing agents. The relative results of different characterizations of graphene oxide and Memecylon edule leaf extract RGO delivers a potential representation by excluding the groups containing oxygen from GO and consecutive stabilization of the developed RGO. The reduced GO functionalization with the oxidized polyphenols results in their stability by avoiding the aggregation. The poly phenol anchored Reduced Graphene Oxide (RGO) exhibited exceptional near-infrared (NIR) irradiation of the lung cancer cells directed in vitro to deliver cytotoxicity. In an area of restricted success in the treatment of cancer, the results of our translation can provide a path for designing targeted PTT agents and also responds to stimulus environment for the safe ablation of the devastating disease.


Assuntos
Grafite/química , Raios Infravermelhos , Nanoestruturas/química , Polifenóis/química , Animais , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos da radiação , Cães , Química Verde , Humanos , Neoplasias Pulmonares/patologia , Neoplasias Pulmonares/terapia , Células Madin Darby de Rim Canino , Magnoliopsida/química , Magnoliopsida/metabolismo , Nanoestruturas/uso terapêutico , Nanoestruturas/toxicidade , Fototerapia/métodos , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo
3.
Comput Biol Chem ; 84: 107196, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31881525

RESUMO

'Bottom-up', i.e., molecule to medicine strategy for the discovery of new drugs takes enormous time and cost. In most of the cases, inherent toxicity and undesired side effects of the developed drug hinder its way beyond the early stages of development. In this regard, the systems pharmacology can play an excellent role by reducing the cost and time of drug development through rationalization and/or repurposing of traditional drugs with known side effects. In the present study, our aim was to develop an integrated systems biology method for the prediction of active ingredients of a traditional medicine and their potential targets inside the body. Further, we evaluated the predictive capacity of the developed method in a preclinical animal model. Here, we have prepared a formulation (SKP17LIV01) from an extract of eight medicinal plants traditionally used as liver medicine and identified the constituents using UHPLC-MS technique. Using systems biology approach, we have rationalized the components of the formulation for potential use in the treatment of heavy metal-induced hepatotoxicity. The active ingredients and potential therapeutic targets were also predicted. A detailed biochemical, histopathological and molecular study on the mice model of lead toxicity confirms the efficacy of the formulation as per prediction by the systems pharmacology approach. The study may open a new frontier for re-discovery of drugs that are already used in traditional medicine.


Assuntos
Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Extratos Vegetais/análise , Extratos Vegetais/uso terapêutico , Substâncias Protetoras/análise , Substâncias Protetoras/uso terapêutico , Animais , Cromatografia Líquida de Alta Pressão , Feminino , Chumbo/toxicidade , Fígado/efeitos dos fármacos , Fígado/patologia , Magnoliopsida/química , Espectrometria de Massas , Medicina Tradicional , Camundongos , Plantas Medicinais/química , Biologia de Sistemas/métodos
4.
J Ethnopharmacol ; 246: 112218, 2020 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-31494202

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Located throughout the body, cannabinoid receptors (CB1 and CB2) are therapeutic targets for obesity/metabolic diseases, neurological/mental disorders, and immune modulation. Phytocannabinoids are greatly important for the development of new medicines with high efficacy and/or minor side effects. Plants and fungi are used in traditional medicine for beneficial effects to mental and immune system. The current research studied five fungi from the genus Ganoderma and five plants: Ganoderma hainanense J.D. Zhao, L.W. Hsu & X.Q. Zhang; Ganoderma capense (Lloyd) Teng, Zhong Guo De Zhen Jun; Ganoderma cochlear (Blume & T. Nees) Bres., Hedwigia; Ganoderma resinaceum Boud.; Ganoderma applanatum (Pers.) Pat.; Carthamus tinctorius L. (Compositae); Cynanchum otophyllum C. K. Schneid. (Asclepiadaceae); Coffea arabica L. (Rubiaceae); Prinsepia utilis Royle (Rosaceae); Lepidium meyenii Walp. (Brassicaceae). They show immunoregulation, promotion of longevity and maintenance of vitality, stimulant effects on the central nervous system, hormone balance and other beneficial effects. However, it remains unclear whether cannabinoid receptors are involved in these effects. AIM OF THE STUDY: This work aimed to identify components working on CB1 and CB2 from the above plants and fungi, as novel phytocannabinoids, and to investigate mechanisms of how these compounds affected the cells. By analyzing the structure-activity relationship, we could identify the core structure for future development. MATERIALS AND METHODS: Eighty-two natural compounds were screened on stably transfected Chinese hamster ovary (CHO) cell lines, CHO-CB1 and CHO-CB2, with application of a label-free dynamic mass redistribution (DMR) technology that measured cellular responses to compounds. CP55,940 and WIN55,212-2 were agonist probe molecules, and SR141716A and SR144528 were antagonist probes. Pertussis toxin, cholera toxin, LY294002 and U73122 were signaling pathway inhibitors. The DMR data were acquired by Epic Imager software (Corning, NY), processed by Imager Beta 3.7 (Corning), and analyzed by GraphPad Prism 6 (GraphPad Software, San Diego, CA). RESULTS: Transfected CHO-CB1 and CHO-CB2 cell lines were established and characterized. Seven compounds induced responses/activities in the cells. Among the seven compounds, four were purified from two Ganoderma species with potencies between 20 and 35 µM. Three antagonists: Kfb68 antagonized both receptors with a better desensitizing effect on CB2 to WIN55,212-2 over CP55,940. Kga1 and Kfb28 were antagonists selective to CB1 and CB2, respectively. Kfb77 was a special agonist and it stimulated CB1 in a mechanism different from that of CP55,940. Another three active compounds, derived from the Lepidium meyenii Walp. (Brassicaceae), were also identified but their effects were mediated through mechanisms much related to the signaling transduction pathways, especially through the stimulatory Gs protein. CONCLUSIONS: We identified four natural cannabinoids that exhibited structural and functional diversities. Our work confirms the presence of active ingredients in the Ganoderma species to CB1 and CB2, and this finding establishes connections between the fungi and the cannabinoid receptors, which will serve as a starting point to connect their beneficial effects to the endocannabinoid system. This research will also enrich the inventory of cannabinoids and phytocannabinoids from fungi. Yet due to some limitations, further structure-activity relationship studies and mechanism investigation are warranted in future.


Assuntos
Canabinoides/química , Canabinoides/farmacologia , Ganoderma/química , Magnoliopsida/química , Animais , Células CHO , Canabinoides/metabolismo , Cricetinae , Cricetulus , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Receptor CB1 de Canabinoide/metabolismo , Receptor CB2 de Canabinoide/metabolismo , Relação Estrutura-Atividade
5.
J Ethnopharmacol ; 247: 112258, 2020 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-31574342

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: In northwestern Argentina inhabit several ancient indigenous communities with diverse cultural and historical background. Geographical isolation has contributed to the prevalence of a native plant-based folk medicine; "jarilla" species are medicinal plants widely used in local communities for the treatment of mycosis, respiratory, gastrointestinal and rheumatic disorders. THE AIM OF THE STUDY: To assemble the traditional knowledge acquired through years with scientific data concerning to phytochemistry, antioxidant and anti-inflammatory potential of three "jarillas" species. MATERIAL AND METHODS: Ethnobotanical data of three "jarillas", Zuccagnia punctata (Zp), Larrea cuneifolia (Lc), and Larrea divaricata (Ld), were explored by interviewing native people from Indigenous Community of Amaicha del Valle, Tucumán. Phenolic profiles from each infusion were analyzed by HPLC-ESI-MS/MS. Antioxidant activity was determined by superoxide anion and hydrogen peroxide scavenging capacity, lipoperoxidation inhibition, and ferrous iron chelating activity. It was also assessed their ability to inhibit pro-inflammatory enzymes, such as xanthine oxidase, lipoxygenase, and hyaluronidase. RESULTS: Ethnobotanical interviews showed that local people use "jarillas" mainly as infusions and baths. It was reported different categories of uses, such as medicinal (10 curative applications), to religious purposes, tinctorial, as construction material and as fuel. From infusions prepared, the MS and MS/MS data allowed the identification of 27 compounds from Z. punctata, and 11 from both Larrea sp. The infusions showed an important antioxidant activity through different mechanisms, highlighting Zp and Lc in free radical scavenging capacity and Ld on lipid peroxidation inhibition and iron binding. They were also capable of inhibit xanthine oxidase and lipoxygenase enzymes, being Lc the most active one. CONCLUSIONS: This research work provides novel information concerning to several categories of traditional uses of "jarilla" species in a Diaguita-Calchaquí community and focus attention to infusions from a phytochemical and biological approach.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Etnobotânica , Magnoliopsida/química , Extratos Vegetais/farmacologia , Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Argentina , Banhos , Etnofarmacologia , Humanos , Povos Indígenas , Medicina Tradicional/métodos , Extratos Vegetais/uso terapêutico
6.
J Agric Food Chem ; 67(47): 13082-13092, 2019 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-31671940

RESUMO

Elevated circulating level of the intestinal microbiota-derived l-carnitine metabolite trimethylamine-N-oxide (TMAO) has recently been linked to many chronic diseases. The purpose of our study was to investigate the effects of omega-7-enriched Decaisnea insignis seed oil (DISO) on reducing TMAO formation to prevent the l-carnitine-induced hepatic damage in mice. Feeding of mice with 3% l-carnitine in drinking water clearly increased the serum and urinary levels of TMAO (p < 0.05 vs Normal), whereas the serum and urinary TMAO formation was sharply reduced by DISO administration (p < 0.05). Meanwhile, DISO resulted in strong inhibition against the elevation of hepatic injury marker (AST, ALT, and ALP) activities and dyslipidemia (TC, TG, LDL-C, and HDL-C), as well as liver inflammatory cytokine (IL-1, IL-6, TNF-α, and TNF-ß) release in l-carnitine-fed mice (p < 0.05). As revealed by 16S rDNA gene sequencing, DISO significantly inhibited the l-carnitine-induced elevations in the abundance of Firmicutes, Proteobacteria, and Erysipelotrichaceae and the increases in the proportion of Lactobacillus and Akkermansia, revealing that DISO attenuated the l-carnitine-caused gut dysbiosis. These findings suggested that DISO could alleviate liver dysfunction in l-carnitine-fed mice, which might be due to the protection against TMAO formation by modulating the gut microbiota.


Assuntos
Carnitina/efeitos adversos , Microbioma Gastrointestinal/efeitos dos fármacos , Hepatopatias/tratamento farmacológico , Magnoliopsida/química , Óleos Vegetais/farmacologia , Animais , Bactérias/classificação , Bactérias/genética , Bactérias/isolamento & purificação , Humanos , Interleucina-1/genética , Interleucina-1/metabolismo , Interleucina-6/genética , Interleucina-6/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Hepatopatias/metabolismo , Hepatopatias/microbiologia , Masculino , Metilaminas/efeitos adversos , Camundongos , Sementes/química
7.
J Agric Food Chem ; 67(38): 10667-10677, 2019 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-31483636

RESUMO

This study investigated the modulatory effects of Decaisnea insignis seed oil (DISO), which was rich in palmitoleic acid (55.25%), palmitic acid (12.25%), and oleic acid (28.74%), on alcohol-induced metabolism disorder in mice. Fifty mice were orally administered with 38% alcohol (0.4 mL/day) and without or with DISO (3, 6, and 12 g/kg) for consecutive 12 weeks. DISO inhibited the alcohol-induced weight loss and liver function abnormality (p < 0.01) and shifted the profiles of cecal microbiome: elevating the abundance of Lactobacillus, Ruminoccoceae_UCG_004 (p < 0.05) and decreasing abundance of Parabacteroides (p < 0.05). This treatment also regulated metabolome response of amino acid and lipid metabolism in cecal content: upregulating 5-hydroxyindole-3-acetic acid (p < 0.05), 6-hydroxynicotinic acid, 5-methoxytryptamine, nicotinamide, and nicotinic acid (p < 0.1) and downregulating androsterone, tryptophan, and indole-3-acetamide (p < 0.05). DISO protected against alcoholic liver injury and gut microbiota dysbiosis by enriching the relative abundance of Lactobacillus, which was positively associated with the improvement of intestinal permeability and tryptophan metabolism.


Assuntos
Álcoois/efeitos adversos , Disbiose/prevenção & controle , Microbioma Gastrointestinal/efeitos dos fármacos , Hepatopatias Alcoólicas/prevenção & controle , Magnoliopsida/química , Óleos Vegetais/administração & dosagem , Consumo de Bebidas Alcoólicas/efeitos adversos , Aminoácidos/metabolismo , Animais , Bactérias/classificação , Bactérias/efeitos dos fármacos , Bactérias/genética , Bactérias/isolamento & purificação , Ceco/efeitos dos fármacos , Ceco/microbiologia , Disbiose/metabolismo , Disbiose/microbiologia , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Hepatopatias Alcoólicas/metabolismo , Hepatopatias Alcoólicas/microbiologia , Masculino , Metaboloma/efeitos dos fármacos , Camundongos , Microbiota/efeitos dos fármacos , Sementes/química
8.
Environ Pollut ; 254(Pt B): 113101, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31472457

RESUMO

As a floating plant, Myriophyllum aquaticum provides a large surface area under water, and thus has high potential for the removal of pollutants through adsorption. The aim of this study was to evaluate the potential adsorption of tetracycline (TC) by M. aquaticum, and examine the underlying mechanisms. M. aquaticum exhibited a high potential for TC removal from water. Adsorption was the main mechanism for rapid TC removal by live M. aquaticum plants, due to its large contact area and ion exchange, accounting for about 99% and 54% of the total amount of TC removed within 2 h and 5 d, respectively. Further, the roots of M. aquaticum exhibited a higher adsorption capacity than the stems or leaves, as the roots had the largest specific surface area. Fourier transform infrared spectroscopy analysis and identification of functional groups showed that -OH, -COOH, and -NH2 groups are involved in the adsorption process. The use of M. aquaticum may be a promising approach for TC removal from aquatic environments, especially in terms of shortening reaction times.


Assuntos
Magnoliopsida/química , Tetraciclina/química , Poluentes Químicos da Água/química , Adsorção , Troca Iônica , Magnoliopsida/metabolismo , Raízes de Plantas/química , Tetraciclina/análise , Águas Residuárias/química , Poluentes Químicos da Água/análise , Purificação da Água/métodos
9.
Molecules ; 24(18)2019 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-31500282

RESUMO

The present study investigated the antioxidant potential and the ability to inhibit lipid and protein oxidation in bovine meat of four native Chilean species: canelo (Drimys winteri), nalca (Gunnera tinctoria), tiaca (Caldcluvia paniculata), and ulmo (Eucryphia cordifolia). Phenolic acids (gallic, chlorogenic, caffeic, and coumaric) and flavonoids (catechin, epicatechin, and rutin) were identified and quantified by HPLC-MS/MS. Drimys winteri extract exhibited the highest antioxidant capacity evaluated by oxygen radical absorption capacity-red pyrogallol method (ORAC-PGR) and ferric ion reducing antioxidant power (FRAP) assays. All extracts decreased lipid oxidation induced by 2,2'-azo-bis(2-amidinopropane) dihydrochloride (AAPH) derived peroxyl radicals by anywhere between 30% and 50% the. In addition, canelo and nalca extracts decreased spontaneous oxidation by around 57% and 37% in relation to the control group, being even more efficient than butylated hydroxyanisole (BHT) a synthetic antioxidant. Protein oxidation in the myofibrillar proteins was evaluated by the formation of protein carbonyls and loss of protein thiols. The canelo, ulmo, and nalca extracts decreased the formation of carbonyls by around 30%. Plant extracts and BHT did not show an antioxidant effect on protein thiol loss. However, tiaca and ulmo extracts exerted a pro-oxidant effect, favoring the oxidation of sulfhydryl groups. The oxidizing system induced structural changes in myofibrillar protein (SDS-PAGE). A protective effect on protein structure from the canelo extract can be observed during the incubation when compared to samples incubated with AAPH.


Assuntos
Antioxidantes/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Magnoliopsida/química , Proteínas Musculares/química , Animais , Antioxidantes/química , Bovinos , Flavonoides/química , Flavonoides/farmacologia , Hidroxibenzoatos/química , Hidroxibenzoatos/farmacologia , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química
10.
Drug Discov Ther ; 13(4): 222-227, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31534074

RESUMO

Based on the anti-virulence activity on Salmonella, the ethyl acetate extract (EAE) of Mesua ferrea flower was investigated for its chemical constituents. Ten purified compounds were identified and assayed for their inhibitory activity against Type III secretion system (T3SS) by polyacrylamide gel electrophoresis (SDS-PAGE) and Western blots experiments. We found the biflavonoids, rhusflavanone and mesuaferrone B, exhibited inhibitory effects on the secretion of Salmonella pathogenicity island 1 (SPI-1) effector proteins (SipA, B, C and D) without effecting the bacterial growth. In addition, 5, 6, 6'-trihydroxy-[1,1'-biphenyl]-3,3'-dicarboxylic acid (6) is a new natural product from M. ferrea flower.


Assuntos
Antibacterianos/farmacologia , Biflavonoides/farmacologia , Magnoliopsida/química , Salmonella/efeitos dos fármacos , Antibacterianos/química , Biflavonoides/química , Flores/química , Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Salmonella/metabolismo , Salmonella/patogenicidade , Sistemas de Secreção Tipo III/efeitos dos fármacos , Fatores de Virulência/metabolismo
11.
Molecules ; 24(16)2019 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-31394879

RESUMO

Drug resistance is a major obstacle in antibiotic and antitumor chemotherapy. In response to the necessity to find new therapeutic strategies, plant secondary metabolites including essential oils (EOs) may represent one of the best sources. EOs in plants act as constitutive defenses against biotic and abiotic stress, and they play an important role in the pharmacology for their low toxicity, good pharmacokinetic and multitarget activity. In this context, natural products such as EOs are one of the most important sources of drugs used in pharmaceutical therapeutics. The aim of this paper was to identify the chemical composition of the essential oil of Alluaudia procera leaves, obtained by hydrodistillation and analysed by gas chromatography-mass spectrometry, and to verify its biological activities on acute myeloid leukemia cancer cell HL60 and its multidrugresistant variant HL60R and the Gram-positive Staphylococcus aureus exhibiting multi-antibiotic resistance. We speculate that cytotoxic and antibiotic effects observed in the tested resistant models may be due to the coordinate activities of forty compounds detected or to the C16 macrocyclic lactones which are the major ones (30%). Our data confirm the possibility of using EOs as therapeutic strategies in resistant models is due to the heterogeneous composition of the oils themselves.


Assuntos
Resistência a Medicamentos , Magnoliopsida/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Antibacterianos/química , Antibacterianos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Análise Espectral
12.
J Appl Microbiol ; 127(4): 1048-1056, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31328837

RESUMO

AIM: The molecular typing and the susceptibility of Staphylococcus aureus strains of swine origin to antibiotics, oregano (Origanum vulgare L.) essential oil (EO) and Chilean blackberry maqui (Aristotelia chilensis (Molina) Stuntz) extract were determined. METHODS AND RESULTS: Twenty S. aureus strains of swine origin were subjected to molecular typing, of which six strains were selected for antimicrobial susceptibility testing. The epsilon test (Etest) was used to determine the antibiotic susceptibility. The susceptibility to natural antimicrobials (NAs): oregano EO, maqui extract, thymol (Thy) and carvacrol (Carv), was carried out using the disk diffusion method. The S. aureus strains were genetically diverse. All strains were resistant to at least one class of antibiotic, and two strains were multidrug-resistant. The minimum inhibitory concentration of oregano EO, Thy and Carv was 0·01-0·04%. Maqui extract did not show antistaphylococcal activity. CONCLUSIONS: Natural antimicrobials extracted from oregano have an inhibitory activity against S. aureus strains from swine origin, with no effect using maqui extract. SIGNIFICANCE AND IMPACT OF THE STUDY: This study provides information about the characteristics of S. aureus strains of swine origin, and about the potential use of NAs from oregano to enhance the control of antibiotic-resistant S. aureus strains in the pork supply chain.


Assuntos
Antibacterianos/farmacologia , Farmacorresistência Bacteriana/efeitos dos fármacos , Magnoliopsida/química , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Suínos/microbiologia , Animais , Testes de Sensibilidade Microbiana , Tipagem Molecular , Monoterpenos/química , Origanum/química , Staphylococcus aureus/classificação , Staphylococcus aureus/genética , Timol/química
13.
Molecules ; 24(13)2019 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-31284554

RESUMO

Nardochinoid B (NAB) is a new compound isolated from Nardostachys chinensis. Although our previous study reported that the NAB suppressed the production of nitric oxide (NO) in lipopolysaccharide (LPS)-activated RAW264.7 cells, the specific mechanisms of anti-inflammatory action of NAB remains unknown. Thus, we examined the effects of NAB against LPS-induced inflammation. In this study, we found that NAB suppressed the LPS-induced inflammatory responses by restraining the expression of inducible nitric oxide synthase (iNOS) proteins and mRNA instead of cyclooxygenase-2 (COX-2) protein and mRNA in RAW264.7 cells, implying that NAB may have lower side effects compared with nonsteroidal anti-inflammatory drugs (NSAIDs). Besides, NAB upregulated the protein and mRNA expressions of heme oxygenase (HO)-1 when it exerted its anti-inflammatory effects. Also, NAB restrained the production of NO by increasing HO-1 expression in LPS-stimulated RAW264.7 cells. Thus, it is considered that the anti-inflammatory effect of NAB is associated with an induction of antioxidant protein HO-1, and thus NAB may be a potential HO-1 inducer for treating inflammatory diseases. Moreover, our study found that the inhibitory effect of NAB on NO is similar to that of the positive drug dexamethasone, suggesting that NAB has great potential for developing new drugs in treating inflammatory diseases.


Assuntos
Heme Oxigenase-1/metabolismo , Ativação de Macrófagos/efeitos dos fármacos , Ativação de Macrófagos/imunologia , Macrófagos/efeitos dos fármacos , Macrófagos/fisiologia , Fator 2 Relacionado a NF-E2/metabolismo , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Ciclo-Oxigenase 2/metabolismo , Citocinas/biossíntese , Mediadores da Inflamação , Magnoliopsida/química , Camundongos , Modelos Biológicos , Estrutura Molecular , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Extratos Vegetais/química , Células RAW 264.7
14.
J Nat Med ; 73(4): 789-799, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31222559

RESUMO

Diterpenoid alkaloids with remarkable chemical properties and biological activities are frequently found in plants of the genera Aconitum, Delphinium, and Garrya. However, little information has been reported on the antiproliferative effects of the diterpenoid alkaloid constituents of Aconitum and Delphinium plants. C-1 and 14 esterifications of delcosine (1) were carried out to provide 39 new diterpenoid alkaloid derivatives (3-14, 16-29, 3a-7a, 9a, 13a, 13b, 14a, 14b, 16a, 17a, 24a, 35a). Selected compounds (3-14, 16-29, 3a-7a, 9a, 13a, 13b, 14a, 14b, 16a, 17a, 24a, 35a) were evaluated for antiproliferative activity against three to five human tumor cell lines including triple-negative breast cancer (TNBC) and P-glycoprotein (P-gp) overexpressing multidrug-resistant (MDR) subline. Several newly synthesized delcosine derivatives (6, 7, 13, 13a, 13b) showed substantial suppressive effects against all human tumor cell lines tested. In contrast, the natural alkaloids (1, 31, 33) showed no effect. Most of the active compounds were delcosine derivatives with two specific substitution patterns-C-1 and C-1,14. In particular, 1-acyldelcosine derivative (5-7) displayed more potency than 1,14-diacyldelcosine derivatives (5a-7a). These acylated alkaloid derivatives caused accumulation of TNBC cells at sub-G1 within 24 h. 1-Acylation of 1 appears to be critical for producing antiproliferative activity in this alkaloid class and a means to provide promising new leads for further development into antitumor agents.


Assuntos
Alcaloides/farmacologia , Antineoplásicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Diterpenos/farmacologia , Extratos Vegetais/farmacologia , Aconitum/química , Alcaloides/química , Linhagem Celular Tumoral , Delphinium/química , Diterpenos/química , Humanos , Magnoliopsida/química , Relação Estrutura-Atividade
15.
J AOAC Int ; 102(5): 1407-1413, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31200784

RESUMO

Background: Ayurveda, the traditional Indian therapeutic system, involves herbs and spices as drug ingredients and a kind of food intake regulation. The health and curative aspects of plant products are often ascribed to their antimicrobial and antioxidant activities (AA). However, it seems somewhat possible to correlate the AA of herbal extracts or plant isolates with their phenolic contents (PC). Objective: Indian researchers have carried out some tests for the determination of AA and PC of plant products that are worth mentioning. Methods: Among the herbal analysis techniques, the important contributions of Indians and people of Indian origin in this field include the remarkable separation of phenolic compounds, including the use of reversed-phase columns, on-line HPLC, the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay to effectively screen and identify antioxidant compounds from herbal extracts, and other chromatographic, spectrographic, and spectroscopic techniques, in the analysis of complex biological matrices. Results: The aim of this paper is to present an overview of such arguments with reference to herbal drugs and food intake regulation for specific ailments. Conclusions: The lack of uniformity in the use of test protocols for antioxidant assays (particularly using the DPPH free radical) and differences in in vitro mechanisms of antiradical activity and in vivo metabolism of polyphenols have been the issues associated with these experiments that have been raised by researchers in the period from 2000 onward.


Assuntos
Antioxidantes/análise , Polifenóis/análise , Antioxidantes/química , Índia , Magnoliopsida/química , Medicina Ayurvédica , Oxirredução , Extratos Vegetais/análise , Extratos Vegetais/química , Polifenóis/química
16.
Food Chem ; 295: 341-349, 2019 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-31174767

RESUMO

The inclusion of edible wild plants in human diet has been receiving an increasing attention, as they represent an easily accessible source of nutrients, vitamins and antioxidants. In this work, the leaves of Umbelicus rupestris (Salisb.) Dandy, an edible species for which only scarce data is available in literature, were thoroughly evaluated for its nutritional profile, chemical characterization and bioactive properties. Being considered a succulent plant, the leaves revealed a very high content of moisture, with several beneficial compounds, including omega-3 polyunsaturated fatty acids, tocopherols and different polyphenols. A total of twelve flavonoids, three phenolic acids and one phenylpropanoid glucoside were identified in the decoction and/or hydroethanolic extracts, with most of them being described for the first time in this plant. Both extracts showed antioxidant activity and potential to inhibit some of the assayed bacteria, while not presenting cytotoxic effects on a non-tumour primary cell culture.


Assuntos
Magnoliopsida/química , Valor Nutritivo , Plantas Comestíveis/química , Antioxidantes/análise , Flavonoides/análise , Hidroxibenzoatos/análise , Extratos Vegetais/análise , Extratos Vegetais/química , Folhas de Planta/química , Polifenóis/análise , Portugal , Tocoferóis/análise
17.
Fitoterapia ; 138: 104192, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31175952

RESUMO

Five new 4-alkyl-5,7-dihydroxycoumarins, Mesuaferol G-K (1-5), together with four known 4-alkyl-5,7-dihydroxycoumarins (6-9) were isolated from the methanol extraction of the flowering buds of Mesua ferrea by flash extraction. Their structures were established on the basis of extensive analyses of HR-ESI-MS, UV, IR and NMR methods, the absolute configurations were confirmed by the Mosher's method and circular dichroism (CD) measurement and theoretical calculation (ECD) methods. Additionally, a putative biogenetic relationship of these compounds was also proposed. The cytotoxicity of all these isolates against HepG2, MCF-7 and Hela cancer cell lines was evaluated. In MCF-7 and Hela cell lines, all compounds exhibited strong activity (IC50 in the range of 3.21-13.54 µM and 4.69-14.47 µM, respectively), while almost all compounds showed moderate cytotoxic activities against HepG2 cell lines.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Cumarínicos/farmacologia , Flores/química , Magnoliopsida/química , China , Cumarínicos/isolamento & purificação , Células HeLa , Células Hep G2 , Humanos , Células MCF-7 , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia
18.
J Agric Food Chem ; 67(27): 7755-7764, 2019 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-31251611

RESUMO

Pectic polysaccharides from New Zealand (NZ) spinach (Tetragonia tetragonioides) and karaka berries (Corynocarpus laevigatus) were extracted and analyzed. NZ spinach polysaccharides comprised mostly homogalacturonan (64.4%) and rhamnogalacturonan I (5.8%), with side chains of arabinan (8.1%), galactan (2.2%), and type II arabinogalactan (7.1%); karaka berry polysaccharides comprised homogalacturonan (21.8%) and rhamnogalacturonan I (10.0%), with greater proportions of side chains (arabinan, 15.6%; galactan, 23.8%; and type II arabinogalactan, 19.3%). Screening of gut commensal Bacteroides showed that six were able to grow on the NZ spinach extract, while five were able to grow on the karaka berry extract. Analysis of the polysaccharides remaining after fermentation, by size-exclusion chromatography and constituent sugar analysis, showed that the Bacteroides species that grew on these two substrates showed preferences for the different pectic polysaccharide types. Our data suggest that, to completely degrade and utilize the complex pectin structures found in plants, members of Bacteroides and other bowel bacteria work as metabolic consortia.


Assuntos
Aizoaceae/química , Bacteroides/crescimento & desenvolvimento , Magnoliopsida/química , Pectinas/metabolismo , Polissacarídeos/metabolismo , Bacteroides/metabolismo , Fermentação , Frutas/química , Microbioma Gastrointestinal/fisiologia , Nova Zelândia , Pectinas/análise , Pectinas/química , Folhas de Planta/química , Polissacarídeos/química , Polissacarídeos/isolamento & purificação
19.
Phytomedicine ; 59: 152771, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31055230

RESUMO

BACKGROUND: The multidrug resistance (MDR) phenotype encounters a major challenge to the success of established chemotherapy in cancer patients. We hypothesized that cytotoxic medicinal plants with novel phytochemicals can overcome MDR and kill MDR-cells with similar efficacy as drug sensitive cells. PURPOSE: We evaluated plant extracts from an unexplored ecosystem in Egypt with unusual climate and nutrient conditions for their activity against sensitive and multidrug-resistant cancer cell lines. MATERIAL AND METHODS/STUDY DESIGN: Methylene chloride: methanol (1:1) and methanol: H2O (7:3) extracts of 40 plants were prepared resulting in a sum of 76 fraction containing compounds with varying polarity. The resazurin reduction assay was employed to evaluate the cytotoxicity of these extracts on five matched pairs of drug-sensitive and their drug-resistant cell lines. Flow cytometry and Western blotting was used to determine cell cycle analyses, apoptosis, and autophagy. Reactive oxygen species (ROS) were measured spectrophotometrically. RESULTS: Extracts derived from Withania obtusifolia (WO), Jasonia candicans (JC), Centaurea lippii (CL), and Pulicaria undulata (PU) were the most active ones among 76 extracts from 40 Egyptian medicinal plants. They showed a significant reduction of cell viability on drug-sensitive CCRF-CEM leukemia cell line with IC50 values less than 7 µg/ml. Low cross-resistance degrees were observed in multidrug-resistant CEM/ADR5000 cells towards CL (1.82-fold) and JC (6.09-fold). All other drug-resistant cell lines did not reveal cross-resistance to the four extracts. Further mechanistic assessment have been studied for these four extracts. CONCLUSION: The methylene chloride: methanol (1:1) fractions of WO, JC, CL, and PU are promising cytotoxic extracts that could be used to combat MDR cancer cells through different cell death pathways.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Magnoliopsida/química , Neoplasias/tratamento farmacológico , Compostos Fitoquímicos/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Antineoplásicos Fitogênicos/uso terapêutico , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Centaurea/química , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Egito , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/uso terapêutico , Pulicaria/química , Espécies Reativas de Oxigênio/metabolismo , Withania/química
20.
Huan Jing Ke Xue ; 40(5): 2265-2270, 2019 May 08.
Artigo em Chinês | MEDLINE | ID: mdl-31087865

RESUMO

The allelopathic effects of Myriophyllum elatinoides on algal growth were investigated and potential allelochemicals secreted by Myriophyllum elatinoides were analyzed. Myriophyllum elatinoides were co-cultivated with different initial concentrations (105, 106, 107, 108, and 109 ind.·L-1) of Microcystis aeruginosa and Selenastrum capricornutum. The optical density of each group was measured daily. The results showed that 2.5 g·(200 mL)-1 of Myriophyllum elatinoides has significant inhibition effect on Microcystis aeruginosa growth with initial concentrations of 107 ind.·L-1 and 108 ind.·L-1. However, there was no significant inhibition on the growth of Selenastrum capricornutum. Through solvent extraction and GC-MS analysis, hexadecanoic acid was extracted and determined as an allelochemical in Myriophyllum elatinoides. Additionally, three potentially novel allelochemical compounds secreted by Myriophyllum elatinoides were determined as follows:3-ethyl-3-methylheptane, triethyl phosphate and dibutyl phthalate.


Assuntos
Alelopatia , Clorofíceas/crescimento & desenvolvimento , Magnoliopsida/química , Microcystis/crescimento & desenvolvimento , Feromônios/química , Ácido Palmítico , Ácidos Ftálicos
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