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1.
Fitoterapia ; 175: 105956, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38604261

RESUMO

ATP citrate lyase (ACLY) is a key enzyme in glucolipid metabolism, and abnormally high expression of ACLY occurs in many diseases, including cancers, dyslipidemia and cardiovascular diseases. ACLY inhibitors are prospective treatments for these diseases. However, the scaffolds of ACLY inhibitors are insufficient with weak activity. The discovery of inhibitors with structural novelty and high activity continues to be a research hotpot. Acanthopanax senticosus (Rupr. & Maxim.) Harms is used for cardiovascular disease treatment, from which no ACLY inhibitors have ever been found. In this work, we discovered three novel ACLY inhibitors, and the most potent one was isochlorogenic acid C (ICC) with an IC50 value of 0.14 ± 0.04 µM. We found dicaffeoylquinic acids with ortho-dihydroxyphenyl groups were important features for inhibition by studying ten phenolic acids. We further investigated interactions between the highly active compound ICC and ACLY. Thermal shift assay revealed that ICC could directly bind to ACLY and improve its stability in the heating process. Enzymatic kinetic studies indicated ICC was a noncompetitive inhibitor of ACLY. Our work discovered novel ACLY inhibitors, provided valuable structure-activity patterns and deepened knowledge on the interactions between this targe tand its inhibitors.


Assuntos
ATP Citrato (pro-S)-Liase , Eleutherococcus , Eleutherococcus/química , Estrutura Molecular , ATP Citrato (pro-S)-Liase/antagonistas & inibidores , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/química , Ácido Clorogênico/farmacologia , Ácido Clorogênico/isolamento & purificação , Ácido Clorogênico/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/química , Ácido Quínico/análogos & derivados , Ácido Quínico/farmacologia , Ácido Quínico/isolamento & purificação , Ácido Quínico/química , Hidroxibenzoatos/farmacologia , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/química , Relação Estrutura-Atividade
2.
Fitoterapia ; 175: 105926, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38537887

RESUMO

Hyperuricemia (HUA) is a metabolic disease characterized by the increase of serum uric acid (UA) level. Sargentodoxae Caulis (SC) is a commonly used herbal medicine for the treatment of gouty arthritis, traumatic swelling, and rheumatic arthritis in clinic. In this study, a total of fifteen compounds were identified in SC water extract using UHPLC-Q-TOF-MS/MS, including three phenolic acids, seven phenolic glycosides, four organic acids, and one lignan. Then, to study the hypouricemia effect of SC, a HUA mouse model was induced using a combination of PO, HX, and 20% yeast feed. After 14 days of treatment with the SC water extract, the levels of serum UA, creatinine (CRE), blood urea nitrogen (BUN) were reduced significantly, and the organ indexes were restored, the xanthine oxidase (XOD) activity were inhibited as well. Meanwhile, SC water extract could ameliorate the pathological status of kidneys and intestine of HUA mice. Additionally, quantitative real-time PCR (qRT-PCR) and western blotting results showed that SC water extract could increase the expression of ATP binding cassette subfamily G member 2 (ABCG2), organic cation transporter 1 (OCT1), organic anion transporter 1 (OAT1) and organic anion transporter 3 (OAT3), whereas decrease the expression of glucose transporter 9 (GLUT9). This study provided a data support for the clinical application of SC in the treatment of HUA.


Assuntos
Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP , Hiperuricemia , Ácido Úrico , Xantina Oxidase , Animais , Camundongos , Hiperuricemia/tratamento farmacológico , Masculino , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/metabolismo , Ácido Úrico/sangue , Xantina Oxidase/metabolismo , Modelos Animais de Doenças , Proteínas Facilitadoras de Transporte de Glucose/metabolismo , Rim/efeitos dos fármacos , Nitrogênio da Ureia Sanguínea , Creatinina/sangue , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Transportadores de Ânions Orgânicos/metabolismo , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Proteína 1 Transportadora de Ânions Orgânicos/metabolismo , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/farmacologia
3.
Molecules ; 26(21)2021 Oct 23.
Artigo em Inglês | MEDLINE | ID: mdl-34770820

RESUMO

The chemical composition of extractives in the sapwood (SW), heartwood (HW), knotwood (KW), and branchwood (BW of silver fir (Abies alba Mill.) was analyzed, and their antifungal and antioxidant properties were studied. In addition, the variability of extractives content in a centripetal direction, i.e., from the periphery of the stem towards the pith, was investigated. The extracts were analyzed chemically with gravimetry, spectrophotometry, and chromatography. The antifungal and antioxidative properties of the extracts were evaluated by the agar well diffusion method and the diphenyl picrylhydrazyl radical scavenging method. Average amounts of hydrophilic extractives were higher in KW (up to 210.4 mg/g) and BW (148.6 mg/g) than in HW (34.1 mg/g) and SW (14.8 mg/g). Extractives identified included lignans (isolariciresinol, lariciresinol, secoisolariciresinol, pinoresinol, matairesinol) phenolic acids (homovanillic acid, coumaric acid, ferulic acid), and flavonoids epicatechin, taxifolin, quercetin). Secoisolariciresinol was confirmed to be the predominant compound in the KW (29.8 mg/g) and BW (37.6 mg/g) extracts. The largest amount of phenolic compounds was extracted from parts of knots (281.7 mg/g) embedded in the sapwood and from parts of branches (258.9 mg/g) adjacent to the stem. HW contained more lignans in its older sections. Hydrophilic extracts from knots and branches inhibited the growth of wood-decaying fungi and molds. KW and BW extracts were better free radical scavengers than HW extracts. The results of the biological activity tests suggest that the protective function of phenolic extracts in silver fir wood can also be explained by their antioxidative properties. The results of this study describe BW as a potential source of phenolic extractives in silver fir.


Assuntos
Antifúngicos/farmacologia , Antioxidantes/farmacologia , Hidroxibenzoatos/farmacologia , Lignanas/farmacologia , Extratos Vegetais/farmacologia , Madeira/química , Antifúngicos/química , Antifúngicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Basidiomycota/efeitos dos fármacos , Compostos de Bifenilo/antagonistas & inibidores , Relação Dose-Resposta a Droga , Fusarium/efeitos dos fármacos , Hidroxibenzoatos/química , Hidroxibenzoatos/isolamento & purificação , Lignanas/química , Lignanas/isolamento & purificação , Testes de Sensibilidade Microbiana , Penicillium/efeitos dos fármacos , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Polyporaceae/efeitos dos fármacos , Schizophyllum/efeitos dos fármacos
4.
Biomed Pharmacother ; 144: 112322, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34656059

RESUMO

Alpinia officinarum (AO) has been traditionally used in Asia as an herbal medicine to treat inflammatory and internal diseases. However, the therapeutic effect of AO on atopic dermatitis (AD) is unclear. Therefore, we examined whether Alpinia officinarum water extract (AOWex) affects AD in vivo and in vitro. Oral administration of AOWex to NC/Nga mice with Dermatophagoies farina extract (DfE)-induced AD-like symptoms significantly reduced the severity of clinical dermatitis, epidermal thickness, and mast cell infiltration into the skin and ear tissue. Decreased total serum IgE, macrophage-derived chemokine (MDC), and regulated on activation, normal T-cell expressed and secreted (RANTES) levels were observed in DfE-induced NC/Nga mice in the AOWex-treated group. These effects were confirmed in vitro using HaCaT cells. Treatment with AOWex inhibited the expression of proinflammatory chemokines such as MDC, RANTES, IP-10 and I-TAC in interferon-γ and tumor necrosis factor-α-stimulated HaCaT cells. The anti-inflammatory effects of AOWex were due to its inhibitory action on MAPK phosphorylation (ERK and JNK), NF-κB, and STAT1. Furthermore, galangin, protocatechuic acid, and epicatechin from AOWex were identified as candidate anti-AD compounds. These results suggest that AOWex exerts therapeutic effects against AD by alleviating AD-like skin lesions, suppressing inflammatory mediators, and inhibiting major signaling molecules.


Assuntos
Alpinia , Anti-Inflamatórios/farmacologia , Quimiocinas/metabolismo , Dermatite Atópica/prevenção & controle , Queratinócitos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Pele/efeitos dos fármacos , Alpinia/química , Animais , Anti-Inflamatórios/isolamento & purificação , Antígenos de Dermatophagoides/imunologia , Proteínas de Artrópodes/imunologia , Catequina/isolamento & purificação , Catequina/farmacologia , Dermatite Atópica/imunologia , Dermatite Atópica/metabolismo , Dermatite Atópica/patologia , Dermatophagoides farinae/imunologia , Modelos Animais de Doenças , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Células HaCaT , Humanos , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/farmacologia , Queratinócitos/imunologia , Queratinócitos/metabolismo , Queratinócitos/patologia , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Transdução de Sinais , Pele/imunologia , Pele/metabolismo , Pele/patologia , Solventes/química , Água/química
5.
Molecules ; 26(6)2021 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-33805815

RESUMO

The phenolic composition, as well as the antioxidant and antimicrobial activities of two poorly investigated Achillea species, Achillea lingulata Waldst. and the endemic Achillea abrotanoides Vis., were studied. To obtain a more detailed phytochemical profile, four solvents with different polarities were used for the preparation of the plant extracts whose phenolic composition was analyzed using UHPLC-MS/MS (ultra-high performance liquid chromatography-tandem mass spectrometry). The results indicate that both of the investigated Achillea species are very rich in both phenolic acids and flavonoids, but that their profiles differ significantly. Chloroform extracts from both species had the highest yields and were the most chemically versatile. The majority of the examined extracts showed antimicrobial activity, while ethanolic extracts from both species were potent against all tested microorganisms. Furthermore, the antioxidant activity of the extracts was evaluated. It was found that the ethanolic extracts possessed the strongest antioxidant activities, although these extracts did not contain the highest amounts of detected phenolic compounds. In addition, several representatives of phenolic compounds were also assayed for these biological activities. Results suggest that ethanol is a sufficient solvent for the isolation of biologically active compounds from both Achillea species. Moreover, it was shown that the flavonoids naringenin and morin are mainly responsible for these antimicrobial activities, while caffeic, salicylic, chlorogenic, p-coumaric, p-hydroxybenzoic, and rosmarinic acid are responsible for the antioxidant activities of the Achillea extracts.


Assuntos
Achillea/química , Anti-Infecciosos/isolamento & purificação , Antioxidantes/isolamento & purificação , Hidroxibenzoatos/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Achillea/classificação , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Compostos de Bifenilo/antagonistas & inibidores , Cromatografia Líquida de Alta Pressão , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Hidroxibenzoatos/química , Hidroxibenzoatos/farmacologia , Testes de Sensibilidade Microbiana , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Solventes , Especificidade da Espécie , Espectrometria de Massas em Tandem
6.
J Oleo Sci ; 70(5): 607-613, 2021 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-33840664

RESUMO

The oil recovery from Alyanak apricot kernel was 36.65% in control (unroasted) and increased to 43.77% in microwave-roasted kernels. The total phenolic contents in extracts from apricot kernel were between 0.06 (oven-roasted) and 0.20 mg GAE/100 g (microwave-roasted) while the antioxidant activity varied between 2.55 (oven-roasted) and 19.34% (microwave-roasted). Gallic acid, 3,4-dihydroxybenzoic acid, (+)-catechin and 1,2-dihydroxybenzene were detected as the key phenolic constituents in apricot kernels. Gallic acid contents varied between 0.53 (control) and 1.10 mg/100 g (microwave-roasted) and 3,4-dihydroxybenzoic acid contents were between 0.10 (control) and 0.35 mg/100 g (microwave-roasted). Among apricot oil fatty acids, palmitic acid contents ranged from 4.38 (oven-roasted) to 4.76% (microwave-roasted); oleic acid contents were between 65.73% (oven-roasted) and 66.15% (control) and linoleic acid contents varied between 26.55 (control) and 27.12% (oven-roasted).


Assuntos
Antioxidantes/análise , Catequina/isolamento & purificação , Catecóis/isolamento & purificação , Ácido Gálico/isolamento & purificação , Hidroxibenzoatos/isolamento & purificação , Ácidos Linoleicos/isolamento & purificação , Micro-Ondas , Ácido Oleico/isolamento & purificação , Óleos de Plantas/análise , Óleos de Plantas/isolamento & purificação , Prunus armeniaca/química , Sementes/química
7.
Chem Biodivers ; 18(5): e2100080, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33773025

RESUMO

This study reports the in vitro anticoagulation activity of acetonic extract (AE) of 42 lichen species and the identification of potential bioavailable anticoagulant compounds from Umbilicaria decussata as a competent anticoagulant lichen species. Lichens' AEs were evaluated for their anticoagulant activity by monitoring activated partial thromboplastin time (APTT) and prothrombin time (PT) assays. A strong, positive correlation was observed between total phenolics concentration (TPC) of species and blood coagulation parameters. U. decussata was the only species with the longest clotting time in both APTT and PT assays. The research was moved forward by performing in vivo assays using rats. The results corroborated the dose-dependent impact of U. decussata's AE on rats' clotting time. Major secondary metabolites of U. decussata and their plasma-related bioavailability were also investigated using LC-ESI-MS/MS. Atranol, orsellinic acid, D-mannitol, lecanoric acid, and evernic acid were detected as possible bioavailable anticoagulants of U. decussata. Our findings suggest that U. decussata might be a potential anticoagulant lichen species that can be used for the prevention or treatment of coagulation-related issues such as cardiovascular diseases (CVDs).


Assuntos
Anticoagulantes/farmacologia , Líquens/química , Extratos Vegetais/farmacologia , Anticoagulantes/química , Anticoagulantes/isolamento & purificação , Benzaldeídos/química , Benzaldeídos/isolamento & purificação , Benzaldeídos/farmacologia , Coagulação Sanguínea/efeitos dos fármacos , Testes de Coagulação Sanguínea , Relação Dose-Resposta a Droga , Hidroxibenzoatos/química , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/farmacologia , Manitol/química , Manitol/isolamento & purificação , Manitol/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Resorcinóis/química , Resorcinóis/isolamento & purificação , Resorcinóis/farmacologia , Salicilatos/química , Salicilatos/isolamento & purificação , Salicilatos/farmacologia
8.
J Ethnopharmacol ; 269: 113737, 2021 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-33359855

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Uapaca species including Uapacastaudtii Pax (Phyllanthaceae) are used in West Africa ethnomedicine to treat diverse ailments including pile, rheumatism, oedema and wound healing. However, the anti-inflammatory and analgesic potential as well as constituents of the Uapacastaudtii stem bark has not been investigated. AIM OF THE STUDY: The study was designed to evaluate the anti-inflammatory, analgesic, and antioxidant activities of extract and fractions ofU. staudtii stem bark, and to isolate the bioactive constituents. MATERIALS AND METHODS: The anti-inflammatory, analgesic and antioxidant activities of the ethanol extract, dichloromethane, ethyl acetate, butanol, and aqueous fractions of U. staudtii stem bark, as well as protocatechuic acid and betulinic acid isolated from the bioactive ethyl acetate fraction were evaluated in different mice models of inflammation and pain; furthermore, antioxidant assays were carried out. Chemical structures of isolated compounds were established based on spectroscopic studies and comparison with literature data. RESULTS: The ethanol extract and ethyl acetate fraction exhibited good anti-inflammatory, analgesic, and antioxidant capacity in all studied models, comparable with those of the standard drugs used. Protocatechuic acid also gave significant (p < 0.05) anti-inflammatory (83%and 88% inhibition for egg-albumin induced and xylene induced oedema, respectively), analgesic (56% inhibition and 22 s of pain suppression for acetic acid-induced and hot plate-induced pain, respectively), and antioxidant effects (97% inhibition and absorbance of 2.516 at 100 µg/mL for DPPH and FRAP assay, respectively) in all the models, whereas betulinic acid only exhibited significant (p < 0.05) anti-inflammatory and antioxidant activity. CONCLUSIONS: The result supports the medicinal uses of the U. staudtii stem bark in the management of pain and inflammatory disease. This is the first report on the biological activities and characterization of compounds inU. staudtii, and presence of protocatechuic acid in Uapaca genus.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Inflamação/tratamento farmacológico , Dor/tratamento farmacológico , Phyllanthus/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , África Ocidental , Analgésicos/química , Analgésicos/isolamento & purificação , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/uso terapêutico , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Comportamento Animal/efeitos dos fármacos , Modelos Animais de Doenças , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Sequestradores de Radicais Livres/farmacologia , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/farmacologia , Hidroxibenzoatos/uso terapêutico , Inflamação/etiologia , Masculino , Camundongos , Dor/etiologia , Triterpenos Pentacíclicos/isolamento & purificação , Triterpenos Pentacíclicos/farmacologia , Triterpenos Pentacíclicos/uso terapêutico , Fenol/análise , Fenol/química , Casca de Planta/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Ácido Betulínico
9.
J Ethnopharmacol ; 264: 113052, 2021 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-32535239

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Salvia miltiorrhiza Bge. as a traditional Asian medicinal plant, roots and rhizomes (Danshen) are used to treat chronic hepatitis and coronary heart disease. In recent years, the medicinal value of S. miltiorrhiza stems and leaves total phenolic acids extract (JF) similar to roots and rhizomes has received increasing attention. S. miltiorrhiza roots and rhizome tanshinone extract (DT) has a good anti-inflammatory effect. AIM OF THE STUDY: To explore the therapeutic effect and possible molecular mechanisms of JF and DT alone or in combination on dextran sulfate sodium (DSS)-induced colitis mice. MATERIALS AND METHODS: Colitis was induced by received 2% DSS in drinking water for 7 consecutive days. Then mice were administered orally for 7 days. Disease activity index (DAI) scores and body weight were recorded daily. After the end of the experiment, colon was removed, colon length was measured and histopathological analysis was performed. Inflammatory factors expression was determined by ELISA, its mRNA expression was detected by real-time quantitative PCR, and the expression of related proteins on TLR4/PI3K/AKT/mTOR signal was analyzed by Western blot. RESULTS: Treatment with JF and DT alone or in combination reduced DAI scores, increase body weight, improved colon shortening, and decreased colon histology scores. In addition, the expression level of inflammatory factors was inhibited. The combination of JF and DT had a better inhibitory effect on inflammatory factors compared to JF alone. We also found that DT alone and JF combined with DT inhibited TLR4/PI3K/AKT/mTOR signaling-related proteins expression levels (including TLR4, p-PI3K p110α/PI3K p110α, p-AKT (ser473)/AKT, mTOR, p-mTOR, NF-κB p65), showing an effective anti-inflammatory effect. CONCLUSIONS: We demonstrated for the first time that, JF and DT alone or in combination effectively ameliorated DSS-induced ulcerative colitis in mice, possibly by inhibiting the TLR4/PI3K/AKT/mTOR signaling pathway.


Assuntos
Abietanos/administração & dosagem , Colite Ulcerativa/tratamento farmacológico , Hidroxibenzoatos/administração & dosagem , Proteínas Proto-Oncogênicas c-akt/antagonistas & inibidores , Salvia miltiorrhiza , Serina-Treonina Quinases TOR/antagonistas & inibidores , Receptor 4 Toll-Like/antagonistas & inibidores , Animais , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/metabolismo , Sulfato de Dextrana/toxicidade , Quimioterapia Combinada , Hidroxibenzoatos/isolamento & purificação , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Fosfatidilinositol 3-Quinases/metabolismo , Inibidores de Fosfoinositídeo-3 Quinase/administração & dosagem , Inibidores de Fosfoinositídeo-3 Quinase/isolamento & purificação , Extratos Vegetais/administração & dosagem , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Caules de Planta , Proteínas Proto-Oncogênicas c-akt/metabolismo , Serina-Treonina Quinases TOR/metabolismo , Receptor 4 Toll-Like/metabolismo
10.
Nat Prod Res ; 35(15): 2579-2582, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31642695

RESUMO

From the methanol extract of the wood of Mangifera gedebe (Anacardiaceae), we had isolated a new secondary metabolite named gedebic acid (1) and six known compounds (2-7). Their chemical structures were determined by spectroscopic methods as well as comparing with data in the literature. All compounds were tested for α-glucosidase inhibitory activity. Compounds 4-7 showed more potent inhibitory activity, with IC50 values ranging from 45.3 to 142.6 µM, than that of a positive control acarbose (IC50, 214.5 µM).


Assuntos
Inibidores de Glicosídeo Hidrolases/química , Hidroxibenzoatos/química , Mangifera , alfa-Glucosidases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Hidroxibenzoatos/isolamento & purificação , Estrutura Molecular , Extratos Vegetais , Madeira
11.
Int J Mol Sci ; 21(14)2020 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-32664524

RESUMO

Here we report the comprehensive characterization of the secondary metabolites from the leaves of Colebrookea oppositifolia Smith, a species used as medicinal plant in the traditional medicine of Nepal. Phytochemical screening of bioactives was performed using an integrated LC-MSn and high resolution MS (Mass Spectrometry) approach. Forty-three compounds were tentatively identified, mainly aglyconic and glycosilated flavonoids and phenolic acids, as well as other bioactives such as coumarins and terpenes were detected. Furthermore, the NF-κB and AP-1 inhibitory activity of C. oppositifolia extract were evaluated, as well as its cytotoxicity against THP-1 cells, in order to assess the potential use of this herb as a source of anti-inflammatory and cytotoxic compounds. The results so far obtained indicate that C. oppositifolia leaves extract could significantly reduce the viability of THP-1 cells (IC50 = 6.2 ± 1.2 µg/mL), as well as the activation of both NF-κB and AP-1 at the concentration of 2 µg/mL. Our results indicate that Nepalese C. oppositifolia is a valuable source of anti-inflammatory and cytotoxic compounds. The phytochemical composition reported here can partially justify the traditional uses of C. oppositifolia in Nepal, especially in the treatment of inflammatory diseases, although further research will be needed to assess the full potential of this species.


Assuntos
Anti-Inflamatórios/farmacologia , Lamiaceae/metabolismo , NF-kappa B/antagonistas & inibidores , Extratos Vegetais/farmacologia , Plantas Medicinais/metabolismo , Fator de Transcrição AP-1/antagonistas & inibidores , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/toxicidade , Cromatografia Líquida , Flavonoides/análise , Flavonoides/isolamento & purificação , Humanos , Hidroxibenzoatos/análise , Hidroxibenzoatos/isolamento & purificação , Espectrometria de Massas , Metaboloma , Metanol , Nepal , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Folhas de Planta/metabolismo , Células THP-1
12.
Am J Chin Med ; 48(4): 871-897, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32431180

RESUMO

Chrysanthemum indicum L. (C. indicum L.), a member of the Compositae family, is a perennial plant that has been used as a traditional medicine for more than 2000 years in China and is widely used for the treatment of Pemphigus, swelling, pain, and scrofula. To date, more than 190 chemical constituents have been isolated and identified from this plant, including flavonoids, terpenoids, phenylpropanoids, and phenolic acids. Numerous modern studies have shown that extracts or monomeric compounds from C. indicum L. have several pharmacological activities, such as anti-inflammatory anti-oxidation, antipathogenic microorganism, anticancer, immune regulation, and hepatoprotective effects. However, resource availability, the research on the mechanism, and quality control are still insufficient, which deserves further efforts. In this paper, the advances in botany, phytochemistry, and pharmacology of C. indicum L were reviewed. We hope that this review can provide important information for traditional Chinese medicine, phytochemistry, synthetic and medicinal chemistry researchers for making full use of C. indicum L. resource.


Assuntos
Anti-Inflamatórios , Antineoplásicos Fitogênicos , Antioxidantes , Chrysanthemum/química , Compostos Fitoquímicos/isolamento & purificação , Fitoterapia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Animais , Anti-Infecciosos , Flavonoides/isolamento & purificação , Humanos , Hidroxibenzoatos/isolamento & purificação , Fatores Imunológicos , Medicina Tradicional Chinesa , Propanóis/isolamento & purificação , Terpenos/isolamento & purificação
13.
J Ethnopharmacol ; 258: 112947, 2020 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-32387462

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cymbopogon citratus (DC.) Stapf has been traditionally used mainly for inflammatory diseases and hypertension. However, the mechanisms underlying its vascular activity remain to be fully characterized and the fractions responsible for its cardiovascular activity are still unknown. AIM OF THE STUDY: In this study, we aimed to assess the vascular activity of Cymbopogon citratus in human arteries and to study the role of cyclooxygenase in its vasorelaxant effects. MATERIALS AND METHODS: Vascular effects of leaves infusion and three fractions (phenolic acids, flavonoids and tannins) were studied using distal segments of human internal thoracic arteries harvested from patients undergoing coronary revascularization, which were mounted as rings in tissue organ baths and maintained at 37 °C in Krebs Henseleit buffer. The effect on basal vascular tone, the effect on the noradrenaline-induced contraction and the vasorelaxant effects were assessed. The role of cyclooxygenase was evaluated with indomethacin. RESULTS: Our results showed a mild effect on the basal vessel tone of the infusion. A significant inhibition on the adrenergic-mediated vasoconstriction was observed for the infusion (0.0002 mg/mL) and the flavonoid fraction (0.2 mg/mL), despite a potentiation was observed in some conditions. A vasorelaxant effect was observed for both the infusion (6.46% of maximal relaxation) and the tannin fraction (26.91% of maximal relaxation, P < 0.05 vs. infusion). Incubation with indomethacin (10 µM) elicited a decrease in the vasorelaxation to the infusion (P < 0.05). CONCLUSIONS: These results suggest that cyclooxygenase may be involved in the vasorelaxation to the infusion of Cymbopogon citratus and that tannins are the compound fraction mainly responsible for this vasorelaxation.


Assuntos
Cymbopogon/química , Artéria Torácica Interna/efeitos dos fármacos , Extratos Vegetais/farmacologia , Vasodilatadores/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/farmacologia , Indometacina/farmacologia , Artéria Torácica Interna/metabolismo , Extratos Vegetais/química , Folhas de Planta , Prostaglandina-Endoperóxido Sintases/efeitos dos fármacos , Prostaglandina-Endoperóxido Sintases/metabolismo , Taninos/isolamento & purificação , Taninos/farmacologia , Vasodilatadores/isolamento & purificação
14.
J Pharm Biomed Anal ; 186: 113327, 2020 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-32402993

RESUMO

A novel mechanobiological assisted extraction (MBAE) method was developed for simultaneous extraction of phenolic acids and flavonoids from Chrysanthemum morifolium. Optimization of extraction factors was performed by response surface methodology based on the Box-Behnken design. The optimal parameters for MBAE were as follows: the amount of enzyme 1% (wt-1), cellulase/pectinase ratio 2:1 (mgmg-1), enzyme solution pH 4.88, extraction pH 10.0, grinding time 40 min and liquid/solid ratio 20:1 (mL/g). Five target compounds flavonoids were identified and quantified by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry in a negative mode. Under optimum conditions, the standard calibration curves were linear in the range of 0.01-20 µg mL-1 and the correlation coefficients were above 0.999 with recoveries of 87.74-119.96%. The developed MBAE method showed the advantages of efficient, time-saving and environmentally friendly which had greater extraction capacity than conventional organic extraction. This is the first attempt that combining mechanochemistry and enzymes to simultaneously extraction phenolic acid and flavonoids from plant.


Assuntos
Chrysanthemum/química , Flavonoides/isolamento & purificação , Hidroxibenzoatos/isolamento & purificação , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Flavonoides/química , Hidroxibenzoatos/análise , Hidroxibenzoatos/química , Espectrometria de Massas , Extratos Vegetais/análise
15.
Curr Pharm Biotechnol ; 21(13): 1289-1297, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32250223

RESUMO

Parmelia that belongs to the Parmeliaceae Family is a foliose lichen combined with one or two groups of fungi in Phylum Ascomycota or Basidiomycota and algae, which might be green algae or blue-green algae (cyanobacteria). It is generally called "Stone Flower," "Charila," "Pattharphool," or "Shilaaapushpa" in India. Lichen can be generally found growing on walls, old trees and spread largely across India, especially in the mountain area. It is a source of edible organisms for people residing in some regions of Nepal and it is also cultivated in hillsides of Kashmir. It has been found that lichen contains a lot of distinctive chemical compounds such as evernic acid, lecanoric acid, lobaric acid, norstictic acid, physodic acid, and salazinic acid. Some species of this lichen are recommended traditionally for controlling diseases such as boils, bronchitis, inflammations, excessive salivation, toothache, vomiting, etc. It has also applied as an indicator for biomonitoring, astringent, carminative, demulcent, bitter, resolvent, emollient, laxative, sporofic, sedative, diuretic and considered for treating sores, bronchitis, excessive salivation, vomiting, tooth-ache, boils and inflammations. It has been utilized for preparing traditional food and acts as a bioindicator for air pollution and radiation. It shows antibacterial, antioxidant, antimycobacterial and antifungal activities, including haemolytic, anaesthetic, spasmolytic and antispasmodic and antitumour activities. It also has several unique phytoconstituents that could be in charge of different therapeutic activities, but the majority of them are still unexplored. The review mainly focuses on various facets, such as common names, synonyms, traditional uses, botanical descriptions, and pharmacological activities of seven species of Parmelia.


Assuntos
Hidroxibenzoatos/farmacologia , Lactonas/farmacologia , Parmeliaceae/crescimento & desenvolvimento , Salicilatos/farmacologia , Depsídeos/isolamento & purificação , Depsídeos/farmacologia , Humanos , Hidroxibenzoatos/isolamento & purificação , Lactonas/isolamento & purificação , Medicina Tradicional , Parmeliaceae/química , Parmeliaceae/classificação , Salicilatos/isolamento & purificação
16.
Zhongguo Zhong Yao Za Zhi ; 45(1): 106-112, 2020 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-32237418

RESUMO

To explore the permeation mechanism of micro-molecule medicinal ingredients of water extract of tradition Chinese medicine(TCM) in membrane separation process. With phenolic acid components as the model solute, five phenolic acids with similar molecular weight and structure, namely gallic acid, protocatechuate acid, 4-hydroxybenzoic acid, 3-hydroxybenzoic acid and salicylic acid, were selected in the PES membrane separation experiments. With the relative flux and the transmission rate as indexes, the scanning electron microscopy(SEM) and the electrochemical impedance spectroscopy(EIS) were used to analyze the permeation mechanism of different phenolic acid components. The results showed phenolic acids with similar molecular weight had different permeation behaviors, with decreased relative flux and increased solute permeation with the increase of solute concentration. According to the permeation behavior analyzed by the molecular structure of solute, the transmission rate of phenolic acids increased with the increase of the number of hydroxyl, and the order of substituent positions of phenolic acids based on the permeation rate as follows: para-substituted > meta-substitution > ortho-substitution. Electrochemical impedance spectroscopy reflected the role of charge repulsion in the membrane process; that is to say, the greater the resistance is, the less the solute permeation is. Therefore, the permeation phenomenon of the phenolic acid components in the PES membrane is not only the result of simple sieving mechanisms, but also has the effects of steric hindrance and charge repulsion during the membrane process.


Assuntos
Medicamentos de Ervas Chinesas/análise , Hidroxibenzoatos/isolamento & purificação , Membranas Artificiais , Medicina Tradicional Chinesa , Estrutura Molecular , Peso Molecular
17.
Phytother Res ; 34(10): 2518-2533, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32307775

RESUMO

Fruits of Terminalia chebula Retz. (Combretaceae) are widely used as crude drugs in various traditional medicine systems. The aim of this article is to review the available scientific information regarding the traditional uses, bioactive chemical constituents and the pharmacological activities of T. chebula. Numerous researches conducted on T. chebula have confirmed the presence of wide range of the phytochemicals such as flavonoids, tannins, phenolic acids and other bioactive compounds. T. chebula is also widely studied regarding its pharmacological activities such as antioxidant, hepatoprotective, neuroprotective, cytotoxic, antidiabetic, anti-inflammatory activities among others. However, more in vivo and clinical studies for mechanism-based pharmacological evaluation should be conducted in future to provide stronger scientific evidences for their traditional uses.


Assuntos
Frutas/fisiologia , Medicina Tradicional/métodos , Compostos Fitoquímicos , Terminalia/fisiologia , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/uso terapêutico , Flavonoides/isolamento & purificação , Flavonoides/uso terapêutico , Frutas/química , Humanos , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/uso terapêutico , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Fitoterapia/métodos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Taninos/isolamento & purificação , Taninos/uso terapêutico , Terminalia/química
18.
Molecules ; 25(6)2020 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-32168896

RESUMO

In this study, the phenolic profiles and bioactivities of five representative cultivars of okra collected in China were investigated. Noticeable variations of phenolic compounds and their bioactivities were observed among these different cultivars of okra. The contents of total flavonoids (TFC) in "Shuiguo", "Kalong 8", "Kalong 3", "Wufu", and "Royal red" ranged from 1.75 to 3.39 mg RE/g DW, of which "Shuiguo" showed the highest TFC. Moreover, five individual phenolic compounds were found in okra by high performance liquid chromatography analysis, including isoquercitrin, protocatechuic acid, quercetin-3-O-gentiobioside, quercetin, and rutin, while isoquercitrin and quercetin-3-O-gentiobioside were detected as the main phenolic compounds in okra. Moreover, all tested okra exhibited significant antioxidant activities (2,2-diphenyl-1-picrylhydrazyl radical scavenging capacity, 2,2'-azino-bis (3-ethylenzthiazoline-6-sulphonic acid) radical scavenging capacity, and ferric reducing antioxidant power) and inhibitory effects on digestive enzymes (lipase, α-glucosidase, and α-amylase). Indeed, "Shuiguo" exhibited much better antioxidant activities and inhibitory activities on digestive enzymes, which might be attributed to its high TFC. Results suggested that okra, especially "Shuiguo", could be developed as natural antioxidants and inhibitors against hyperlipidemia and hyperglycemia in the fields of functional foods and pharmaceuticals, which could meet the increasing demand for high-quality okra with health-promoting properties in China.


Assuntos
Abelmoschus/química , Frutas/química , Lipase/antagonistas & inibidores , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/química , Animais , Antioxidantes/química , Antioxidantes/classificação , Antioxidantes/isolamento & purificação , Benzotiazóis/antagonistas & inibidores , Benzotiazóis/química , Compostos de Bifenilo/antagonistas & inibidores , Compostos de Bifenilo/química , Dissacarídeos/química , Dissacarídeos/isolamento & purificação , Flavonoides/química , Flavonoides/classificação , Flavonoides/isolamento & purificação , Hidroxibenzoatos/química , Hidroxibenzoatos/isolamento & purificação , Lipase/química , Fenóis/química , Fenóis/classificação , Fenóis/isolamento & purificação , Picratos/antagonistas & inibidores , Picratos/química , Extratos Vegetais/química , Quercetina/análogos & derivados , Quercetina/química , Quercetina/isolamento & purificação , Rutina/química , Rutina/isolamento & purificação , Ácidos Sulfônicos/antagonistas & inibidores , Ácidos Sulfônicos/química , Ácidos Sulfônicos/isolamento & purificação , Suínos , Tiazóis/química , Tiazóis/isolamento & purificação , alfa-Amilases/química
19.
Molecules ; 25(3)2020 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-32050498

RESUMO

Lonicera caerulea L., also known as haskap or honeysuckle berry, is a fruit commonly planted in eastern Europe, Canada and Asia. The fruit was registered as a traditional food from a third country under European Union regulations only on December 2018. It is resistant to cold, pests, various soil acidities and diseases. However, its attractiveness is associated mostly with its health properties. The fruit shows anticancer, anti-inflammatory, and antioxidant activity-important factors in improving health. These features result from the diverse content of phytochemicals in honeysuckle berries with high concentrations of phytocompounds, mainly hydroxycinnamic acids, hydroxybenzoic acids, flavanols, flavones, isoflavones, flavonols, flavanones and anthocyanins but also iridoids, present in the fruit in exceptional amounts. The content and health properties of the fruit were identified to be dependent on cultivar, genotype and the place of harvesting. Great potential benefits of this nutritious food are its ability to minimize the negative effects of UV radiation, diabetes mellitus and neurodegenerative diseases, and to exert hepato- and cardioprotective activity.


Assuntos
Antocianinas/isolamento & purificação , Ácidos Cumáricos/isolamento & purificação , Flavonoides/isolamento & purificação , Frutas/química , Hidroxibenzoatos/isolamento & purificação , Iridoides/isolamento & purificação , Lonicera/química , Antocianinas/química , Antocianinas/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Ásia , Canadá , Cardiotônicos/química , Cardiotônicos/isolamento & purificação , Cardiotônicos/farmacologia , Ácidos Cumáricos/química , Ácidos Cumáricos/farmacologia , Europa (Continente) , Flavonoides/química , Flavonoides/farmacologia , Frutas/metabolismo , Hidroxibenzoatos/química , Hidroxibenzoatos/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Iridoides/química , Iridoides/farmacologia , Lonicera/metabolismo , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Fármacos Neuroprotetores/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Protetores Solares/química , Protetores Solares/isolamento & purificação , Protetores Solares/farmacologia
20.
J Pharm Biomed Anal ; 177: 112879, 2020 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-31542418

RESUMO

Globe artichoke (Cynara cardunculus var. scolymus L.) is not only used as a vegetable and ornamental plant, but also as important medicinal plant for the treatment of dyspeptic disorders. The European Pharmacopoeia describes a method for the quality assessment of dry artichoke leaves, which is time-consuming and requires huge amounts of organic solvents. In this study, an ultrasound-assisted extraction method was studied, which proved to be more efficient than the standard protocol of the European Pharmacopoeia, since it led to comparable results, was faster and easier to handle, and was more sustainable due to a reduced need for organic solvents.


Assuntos
Fracionamento Químico/métodos , Cynara scolymus/química , Flavonoides/isolamento & purificação , Hidroxibenzoatos/isolamento & purificação , Extratos Vegetais/análise , Fracionamento Químico/instrumentação , Química Farmacêutica/instrumentação , Química Farmacêutica/métodos , Estudos de Viabilidade , Metanol/química , Extratos Vegetais/química , Folhas de Planta/química , Solventes/química , Sonicação , Água/química
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