Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 244
Filtrar
1.
Mar Drugs ; 22(3)2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38535464

RESUMO

The worldwide prevalence of obesity impacts more than 600 million adults. Successfully managing weight is effective in reducing the risk of chronic diseases, but sustaining long-term weight loss remains a challenge. Although there are supplements based on algae that claim to aid in weight loss, there is a notable scarcity of scientific evidence supporting their effectiveness, and their regular consumption safety remains inadequately addressed. In this work, commercially available Arthrospira (Spirulina) platensis Gomont and/or Fucus vesiculosus L. supplements showed moderate capacity to inhibit the activity of carbohydrate-metabolizing enzymes, and to scavenge biologically relevant reactive species. IC25 values varying between 4.54 ± 0.81 and 66.73 ± 5.91 µg of dry extract/mL and between 53.74 ± 8.42 and 1737.96 ± 98.26 µg of dry extract/mL were obtained for α-glucosidase and aldose reductase, respectively. A weaker effect towards α-amylase activity was observed, with a maximum activity of the extracts not going beyond 33%, at the highest concentrations tested. Spirulina extracts showed generally better effects than those from F. vesiculosus. Similar results were observed concerning the antiradical capacity. In a general way, the extracts were able to intercept the in vitro-generated reactive species nitric oxide (•NO) and superoxide anion (O2•-) radicals, with better results for O2•-scavenging with the spirulina samples (IC25 values of 67.16 and 122.84 µg of dry extract/mL). Chemically, similar pigment profiles were observed between spirulina supplements and the authenticated counterpart. However, fucoxanthin, the chemotaxonomic marker of brown seaweeds, was not found in F. vesiculosus samples, pointing to the occurrence of a degradation phenomenon before, during, or after raw material processing. Our findings can contribute to providing data to allow regulatory entities (e.g., EFSA and FDA) to better rule these products in a way that can benefit society.


Assuntos
Decapodiformes , Suplementos Nutricionais , Spirulina , Animais , Óxido Nítrico , Extratos Vegetais
2.
Phytother Res ; 38(4): 1903-1931, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38358734

RESUMO

Herbal medicines are widely perceived as natural and safe remedies. However, their concomitant use with prescribed drugs is a common practice, often undertaken without full awareness of the potential risks and frequently without medical supervision. This practice introduces a tangible risk of herb-drug interactions, which can manifest as a spectrum of consequences, ranging from acute, self-limited reactions to unpredictable and potentially lethal scenarios. This review offers a comprehensive overview of herb-drug interactions, with a specific focus on medications targeting the Central and Peripheral Nervous Systems. Our work draws upon a broad range of evidence, encompassing preclinical data, animal studies, and clinical case reports. We delve into the intricate pharmacodynamics and pharmacokinetics underpinning each interaction, elucidating the mechanisms through which these interactions occur. One pressing issue that emerges from this analysis is the need for updated guidelines and sustained pharmacovigilance efforts. The topic of herb-drug interactions often escapes the attention of both consumers and healthcare professionals. To ensure patient safety and informed decision-making, it is imperative that we address this knowledge gap and establish a framework for continued monitoring and education. In conclusion, the use of herbal remedies alongside conventional medications is a practice replete with potential hazards. This review not only underscores the real and significant risks associated with herb-drug interactions but also underscores the necessity for greater awareness, research, and vigilant oversight in this often-overlooked domain of healthcare.


Assuntos
Plantas Medicinais , Animais , Humanos , Plantas Medicinais/efeitos adversos , Interações Ervas-Drogas , Fármacos do Sistema Nervoso Periférico
3.
Bioorg Chem ; 138: 106614, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37216893

RESUMO

The inflammatory response is a vital mechanism for repairing damage induced by aberrant health states or external insults; however, persistent activation can be linked to numerous chronic diseases. The nuclear factor kappa ß (NF-κB) inflammatory pathway and its associated mediators have emerged as critical targets for therapeutic interventions aimed at modulating inflammation, necessitating ongoing drug development. Previous studies have reported the inhibitory effect of a hydroethanol extract derived from Parinari excelsa Sabine (Chrysobalanaceae) on tumour necrosis factor-alpha (TNF-α), but the phytoconstituents and mechanisms of action remained elusive. The primary objective of this study was to elucidate the phytochemical composition of P. excelsa stem bark and its role in the mechanisms underpinning its biological activity. Two compounds were detected via HPLC-DAD-ESI(Ion Trap)-MS2 analysis. The predominant compound was isolated and identified as naringenin-8-sulphonate (1), while the identity of the second compound (compound 2) could not be determined. Both compound 1 and the extract were assessed for anti-inflammatory properties using a cell-based inflammation model, in which THP-1-derived macrophages were stimulated with LPS to examine the treatments' effects on various stages of the NF-κB pathway. Compound 1, whose biological activity is reported here for the first time, demonstrated inhibition of NF-κB activity, reduction in interleukin 6 (IL-6), TNF-α, and interleukin 1 beta (IL-1ß) production, as well as a decrease in p65 nuclear translocation in THP-1 cells, thus highlighting the potential role of sulphur substituents in the activity of naringenin (3). To explore the influence of sulphation on the anti-inflammatory properties of naringenin derivatives, we synthesized naringenin-4'-O-sulphate (4) and naringenin-7-O-sulphate (5) and evaluated their anti-inflammatory effects. Naringenin derivatives 4 and 5 did not display potent anti-inflammatory activities; however, compound 4 reduced IL-1ß production, and compound 5 diminished p65 translocation, with both exhibiting the capacity to inhibit TNF-α and IL-6 production. Collectively, the findings demonstrated that the P. excelsa extract was more efficacious than all tested compounds, while providing insights into the role of sulphation in the anti-inflammatory activity of naringenin derivatives.


Assuntos
Chrysobalanaceae , NF-kappa B , Humanos , NF-kappa B/metabolismo , Interleucina-6/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Chrysobalanaceae/metabolismo , Casca de Planta/metabolismo , Anti-Inflamatórios/uso terapêutico , Inflamação/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Lipopolissacarídeos/farmacologia
4.
Molecules ; 28(8)2023 Apr 07.
Artigo em Inglês | MEDLINE | ID: mdl-37110524

RESUMO

Solanum betaceum Cav., commonly known as tamarillo or Brazilian tomato, belongs to the Solanaceae family. Its fruit is used in traditional medicine and food crops due to its health benefits. Despite the numerous studies involving the fruit, there is no scientific knowledge about the tamarillo tree leaves. In this work, the phenolic profile of aqueous extract obtained from S. betaceum leaves was unveiled for the first time. Five hydroxycinnamic phenolic acids were identified and quantified, including 3-O-caffeoylquinic acid, 4-O-caffeoylquinic acid, chlorogenic acid, caffeic acid and rosmarinic acid. While the extract displayed no effect on α-amylase, the extract inhibited the activity of α-glucosidase (IC50 = 1617 mg/mL), and it was particularly effective for human aldose reductase (IC50 = 0.236 mg/mL): a key enzyme in glucose metabolism. Moreover, the extract exhibited interesting antioxidant properties, such as a potent capacity to intercept the in vitro-generated reactive species O2•- (IC50 = 0.119 mg/mL) and •NO (IC50 = 0.299 mg/mL), as well as to inhibit the first stages of lipid peroxidation (IC50 = 0.080 mg/mL). This study highlights the biological potential of S. betaceum leaves. The scarcity of research on this natural resource underscores the need for additional studies in order to fully explore its antidiabetic properties and to promote the value of a species currently at risk of extinction.


Assuntos
Solanum , Humanos , Solanum/metabolismo , Hipoglicemiantes/farmacologia , Hipoglicemiantes/metabolismo , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Frutas , Fenóis/metabolismo , Ácido Clorogênico/farmacologia , Ácido Clorogênico/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/metabolismo
5.
Mar Drugs ; 21(1)2022 Dec 28.
Artigo em Inglês | MEDLINE | ID: mdl-36662196

RESUMO

Plant bacterial pathogens can be devastating and compromise entire crops of fruit and vegetables worldwide. The consequences of bacterial plant infections represent not only relevant economical losses, but also the reduction of food availability. Synthetic bactericides have been the most used tool to control bacterial diseases, representing an expensive investment for the producers, since cyclic applications are usually necessary, and are a potential threat to the environment. The development of greener methodologies is of paramount importance, and some options are already available in the market, usually related to genetic manipulation or plant community modulation, as in the case of biocontrol. Seaweeds are one of the richest sources of bioactive compounds, already being used in different industries such as cosmetics, food, medicine, pharmaceutical investigation, and agriculture, among others. They also arise as an eco-friendly alternative to synthetic bactericides. Several studies have already demonstrated their inhibitory activity over relevant bacterial phytopathogens, some of these compounds are known for their eliciting ability to trigger priming defense mechanisms. The present work aims to gather the available information regarding seaweed extracts/compounds with antibacterial activity and eliciting potential to control bacterial phytopathogens, highlighting the extracts from brown algae with protective properties against microbial attack.


Assuntos
Phaeophyceae , Alga Marinha , Verduras , Bactérias , Plantas
6.
Molecules ; 27(22)2022 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-36431805

RESUMO

BACKGROUND: The use of plants for therapeutic purposes has been supported by growing scientific evidence. METHODS: This work consisted of (i) characterizing the phenolic compounds present in both aqueous and hydroethanol (1:1, v/v) extracts of camel grass, by hyphenated liquid chromatographic techniques, (ii) evaluating their anti-inflammatory, antioxidant, and neuromodulation potential, through in vitro cell and cell-free models, and (iii) establishing a relationship between the chemical profiles of the extracts and their biological activities. RESULTS: Several caffeic acid and flavonoid derivatives were determined in both extracts. The extracts displayed scavenging capacity against the physiologically relevant nitric oxide (•NO) and superoxide anion (O2•-) radicals, significantly reduced NO production in lipopolysaccharide (LPS)-stimulated macrophages (RAW 264.7), and inhibited the activity of hyaluronidase (HAase), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Some of these bioactivities were found to be related with the chemical profile of the extracts, namely with 3-caffeoylquinic, 4-caffeoylquinic, chlorogenic, and p-coumaric acids, as well as with luteolin and apigenin derivatives. CONCLUSIONS: This study reports, for the first time, the potential medicinal properties of aqueous and hydroethanol extracts of camel grass in the RAW 264.7 cell model of inflammation, and in neurologically related conditions.


Assuntos
Butirilcolinesterase , Camelus , Animais , Acetilcolinesterase , Poaceae , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Fenóis/química , Inflamação/tratamento farmacológico
7.
Molecules ; 27(24)2022 Dec 09.
Artigo em Inglês | MEDLINE | ID: mdl-36557886

RESUMO

Mentha suaveolens (MS), Conyza canadensis (CC), Teucrium polium (TP) and Salvia verbenaca (SV) are used in Morocco to treat hypertension. Our aim was to characterize the composition and vasoreactivity of extracts of MS, CC, TP and SV. The chemical compositions of aqueous extracts of MS, SV and TP, and of a hydromethanolic extract of CC, were identified by HPLC-DAD. The vasoreactive effect was tested in rings of the thoracic aorta of female Wistar rats (8-14 weeks-old) pre-contracted with 10 µM noradrenaline, in the absence or presence of L-NAME 100 µM, indomethacin 10 µM or atropine 6 µM, to inhibit nitric oxide synthase, cyclooxygenase or muscarinic receptors, respectively. L-NAME and atropine decreased the vasorelaxant effect caused by low concentrations of MS. Atropine and indomethacin decreased the vasorelaxant effect of low concentrations of SV. High concentrations of MS or SV and the effect of SV and TP were not altered by any antagonist. The activation of muscarinic receptors and NO or the cyclooxygenase pathway underlie the vasorelaxant effect of MS and SV, respectively. Neither of those mechanisms underlines the vasorelaxant effect of CC and TP. These vasorelaxant effect might support the use of herbal teas from these plants as anti-hypertensives in folk medicine.


Assuntos
Conyza , Mentha , Salvia , Teucrium , Ratos , Animais , Vasodilatadores/farmacologia , Ratos Wistar , Mentha/metabolismo , NG-Nitroarginina Metil Éster/farmacologia , Salvia/metabolismo , Prostaglandina-Endoperóxido Sintases/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/metabolismo , Vasodilatação , Aorta/metabolismo , Aorta Torácica , Receptores Muscarínicos/metabolismo , Derivados da Atropina/metabolismo , Derivados da Atropina/farmacologia
8.
Molecules ; 26(8)2021 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-33923843

RESUMO

The emergence of antibiotic-resistance in bacteria has limited the ability to treat bacterial infections, besides increasing their morbidity and mortality at the global scale. The need for alternative solutions to deal with this problem is urgent and has brought about a renewed interest in natural products as sources of potential antimicrobials. The wine industry is responsible for the production of vast amounts of waste and by-products, with associated environmental problems. These residues are rich in bioactive secondary metabolites, especially phenolic compounds. Some phenolics are bacteriostatic/bactericidal against several pathogenic bacteria and may have a synergistic action towards antibiotics, mitigating or reverting bacterial resistance to these drugs. Complex phenolic mixtures, such as those present in winemaking residues (pomace, skins, stalks, leaves, and especially seeds), are even more effective as antimicrobials and could be used in combined therapy, thereby contributing to management of the antibiotic resistance crisis. This review focuses on the potentialities of winemaking by-products, their extracts, and constituents as chemotherapeutic antibacterial agents.


Assuntos
Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Antioxidantes/metabolismo , Resistência Microbiana a Medicamentos , Fenóis/metabolismo
9.
Pharmacol Res ; 155: 104702, 2020 05.
Artigo em Inglês | MEDLINE | ID: mdl-32068119

RESUMO

The endoplasmic reticulum (ER) comprises a network of tubules and vesicles that constitutes the largest organelle of the eukaryotic cell. Being the location where most proteins are synthesized and folded, it is crucial for the upkeep of cellular homeostasis. Disturbed ER homeostasis triggers the activation of a conserved molecular machinery, termed the unfolded protein response (UPR), that comprises three major signaling branches, initiated by the protein kinase RNA-like endoplasmic reticulum kinase (PERK), inositol-requiring enzyme 1 (IRE1) and the activating transcription factor 6 (ATF6). Given the impact of this intricate signaling network upon an extensive list of cellular processes, including protein turnover and autophagy, ER stress is involved in the onset and progression of multiple diseases, including cancer and neurodegenerative disorders. There is, for this reason, an increasing number of publications focused on characterizing and/or modulating ER stress, which have resulted in a wide array of techniques employed to study ER-related molecular events. This review aims to sum up the essentials on the current knowledge of the molecular biology of endoplasmic reticulum stress, while highlighting the available tools used in studies of this nature.


Assuntos
Estresse do Retículo Endoplasmático , Neoplasias/metabolismo , Doenças Neurodegenerativas/metabolismo , Animais , Autofagia , Cálcio/metabolismo , Humanos , Mitocôndrias/metabolismo , Transdução de Sinais , Resposta a Proteínas não Dobradas
10.
Planta Med ; 86(2): 121-131, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31645066

RESUMO

Centaurium erythraea is a plant used in traditional medicine for several cardiovascular disorders, namely hypertension, but there is no scientific evidence able to provide a molecular basis for its claimed antihypertensive effects. After a preliminary screen of extracts obtained from sequential extraction of C. erythraea aerial parts, effects of the methanolic fraction (MFCE) on changes in perfusion pressure of isolated rat mesenteric vascular bed (MVB) and in rat cardiac fibroblasts proliferation were investigated, gathering information on the mechanisms involved in endothelium-dependent effects and their dependence on a pro-proliferative stimulus. The HPLC-DAD determination of the phenolics content of MFCE revealed the presence of 22 phenolic compounds. MFCE reduced (63.3 ± 3.9%; n = 4) perfusion pressure in MVB and almost completely abrogated the Ang II-induced increase in cardiac fibroblasts proliferation. Reduction of the perfusion pressure caused by MFCE was endothelium-dependent and occurred in parallel with an increase in NO release. These effects were inhibited by muscarinic receptor antagonists, by L-NAME (a NO synthase inhibitor), and by ODQ (a soluble guanylate cyclase inhibitor). Experiments revealed that effects required the involvement of K+ channels, being inhibited by tetraethylamonium (TEA; a Ca2+ activated K+ channels inhibitor) and by glibenclamide (an ATP-sensitive K+ channels inhibitor). In conclusion, extracts from C. erythraea, particularly the compounds present in the MFCE, induce endothelium-dependent vasodilation and prevent fibroblast proliferation induced by angiotensin II, which can account for the claimed antihypertensive effects of C. erythraea in traditional medicine.


Assuntos
Anti-Hipertensivos/farmacologia , Centaurium/química , Extratos Vegetais/farmacologia , Animais , Anti-Hipertensivos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Endotélio Vascular/efeitos dos fármacos , Feminino , Fibroblastos/efeitos dos fármacos , Masculino , Extratos Vegetais/isolamento & purificação , Ratos , Ratos Wistar , Vasodilatadores/isolamento & purificação , Vasodilatadores/farmacologia
11.
Mar Drugs ; 18(12)2020 Dec 18.
Artigo em Inglês | MEDLINE | ID: mdl-33353007

RESUMO

Globally, the burden of neurodegenerative disorders continues to rise, and their multifactorial etiology has been regarded as among the most challenging medical issues. Bioprospecting for seaweed-derived multimodal acting products has earned increasing attention in the fight against neurodegenerative conditions. Phlorotannins (phloroglucinol-based polyphenols exclusively produced by brown seaweeds) are amongst the most promising nature-sourced compounds in terms of functionality, and though research on their neuroprotective properties is still in its infancy, phlorotannins have been found to modulate intricate events within the neuronal network. This review comprehensively covers the available literature on the neuroprotective potential of both isolated phlorotannins and phlorotannin-rich extracts/fractions, highlighting the main key findings and pointing to some potential directions for neuro research ramp-up processes on these marine-derived products.


Assuntos
Doenças Neurodegenerativas/tratamento farmacológico , Phaeophyceae/química , Polifenóis/uso terapêutico , Alga Marinha/química , Taninos/uso terapêutico , Animais , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/uso terapêutico , Humanos , Fármacos Neuroprotetores/isolamento & purificação , Fármacos Neuroprotetores/uso terapêutico , Polifenóis/isolamento & purificação , Taninos/isolamento & purificação
12.
Int J Mol Sci ; 21(7)2020 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-32244489

RESUMO

Commonly used to treat skin injuries in Asia, several Homalium spp. have been found to promote skin regeneration and wound healing. While ethnobotanical surveys report the use of H. bhamoense trunk bark as a wound salve, there are no studies covering bioactive properties. As impaired cutaneous healing is characterized by excessive inflammation, a series of inflammatory mediators involved in wound healing were targeted with a methanol extract obtained from H. bhamoense trunk bark. Results showed concentration-dependent inhibition of hyaluronidase and 5-lipoxygenase upon exposure to the extract, with IC50 values of 396.9 ± 25.7 and 29.0 ± 2.3 µg mL-1, respectively. H. bhamoense trunk bark extract also exerted anti-inflammatory activity by significantly suppressing the overproduction of interleukin 6 (IL-6) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages at concentrations ranging from 125 to 1000 µg mL-1, while leading to a biphasic effect on nitric oxide (NO) and tumor necrosis factor alpha (TNF-α) levels. The phenolic profile was elucidated by HPLC-DAD, being characterized by the occurrence of ellagic acid as the main constituent, in addition to a series of methylated derivatives, which might underlie the observed anti-inflammatory effects. Our findings provide in vitro data on anti-inflammatory ability of H. bhamoense trunk bark, disclosing also potential cutaneous toxicity as assessed in HaCaT keratinocytes.


Assuntos
Anti-Inflamatórios/farmacologia , Interleucina-6/efeitos adversos , Lipopolissacarídeos/efeitos adversos , Macrófagos/efeitos dos fármacos , Medicina Tradicional/métodos , Nephropidae/química , Extratos Vegetais/farmacologia , Animais , Araquidonato 5-Lipoxigenase/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citocinas/metabolismo , Medicina Herbária , Hialuronoglucosaminidase/efeitos dos fármacos , Hidroxibenzoatos , Mediadores da Inflamação/farmacologia , Concentração Inibidora 50 , Interleucina-6/metabolismo , Queratinócitos , Lipopolissacarídeos/metabolismo , Camundongos , Óxido Nítrico/metabolismo , Células RAW 264.7 , Fator de Necrose Tumoral alfa
13.
Inflammopharmacology ; 28(6): 1717-1734, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31410747

RESUMO

Jasonia glutinosa (L.) DC., known as rock tea (RT), is traditionally used in Spain as a digestive due to its beneficial properties in bowel disorders. The pharmacological nature of these properties has not been established yet. The aim of this work was to evaluate the therapeutic utility of RT in experimental colitis and to identify chemical constituents with anti-inflammatory and/or anti-oxidative properties. RT extract was prepared with ethanol in a Soxhlet apparatus and analysed by HPLC-DAD. Superoxide radical scavenging properties, xanthine oxidase and lipoxygenase (5-LOX) inhibitory activity, and capability to lower nitric oxide (NO) and tumor necrosis factor α (TNF-α) levels were measured in cell-free and cell-based assays. In the 2.5%-dextran-sodium sulphate (DSS) injury-repair model of ulcerative colitis (UC), mice were daily treated with sulfasalazine (SSZ, as reference drug, 100 mg/kg bw), RT (5, 25 and 50 mg/kg bw, p.o.), or vehicle over 20 days. Colitis was scored daily. Colon samples were examined macroscopically and histopathologically. Protein levels of myeloperoxidase (MPO), interleukins 6, and 10 (IL-6, IL-10), inducible NO synthase (iNOS), and cyclooxygenase-2 (COX-2) were studied as markers of oxidative stress and inflammatory activity. The integrity of the apical epithelial layer was assessed by immunofluorescence staining of zonula ocludens-1 (ZO-1). Finally, intestinal contractility was also evaluated by isometric myography. Fifteen phenolic compounds and three pigments were identified and quantified, of which caffeoylquinic acids, and the flavonoid, quercetin-3-O-galactoside, were the most abundant. RT extract significantly scavenged superoxide radicals, inhibited 5-LOX activity, and lowered NO and TNF-α levels. DSS-treated mice receiving RT scored clinically lower than controls during the first 3 days of DSS treatment and during the recovery period. SSZ was less effective than RT. Anatomical and histological examination of colon samples revealed that RT significantly prevented colon shortening, increased colon thickness, and lowered the macroscopic damage score. RT also significantly prevented the increase of MPO activity, IL-6 levels, iNOS and COX-2 expression, the loss of ZO-1 apical expression, and normalized contractility disturbances. In conclusion, daily administration of RT showed therapeutic properties in the DSS-model of UC. The benefits of RT can likely be attributed to its anti-inflammatory and antioxidant phenolic and flavonoid constituents.


Assuntos
Colite Ulcerativa/tratamento farmacológico , Colo/efeitos dos fármacos , Inflamação/tratamento farmacológico , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Substâncias Protetoras/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Biomarcadores/metabolismo , Células Cultivadas , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/metabolismo , Colo/metabolismo , Sulfato de Dextrana/farmacologia , Modelos Animais de Doenças , Medicina Herbária/métodos , Inflamação/metabolismo , Mediadores da Inflamação/metabolismo , Masculino , Medicina Tradicional/métodos , Camundongos , Camundongos Endogâmicos C57BL , Fitoterapia/métodos
14.
Mar Drugs ; 17(10)2019 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-31569621

RESUMO

While several marine natural products bearing the 2,5-diketopiperazine ring have been reported to date, the unique chemistry of dimeric frameworks appears to remain neglected. Frequently reported from marine-derived strains of fungi, many naturally occurring diketopiperazine dimers have been shown to display a wide spectrum of pharmacological properties, particularly within the field of cancer and antimicrobial therapy. While their structures illustrate the unmatched power of marine biosynthetic machinery, often exhibiting unsymmetrical connections with rare linkage frameworks, enhanced binding ability to a variety of pharmacologically relevant receptors has been also witnessed. The existence of a bifunctional linker to anchor two substrates, resulting in a higher concentration of pharmacophores in proximity to recognition sites of several receptors involved in human diseases, portrays this group of metabolites as privileged lead structures for advanced pre-clinical and clinical studies. Despite the structural novelty of various marine diketopiperazine dimers and their relevant bioactive properties in several models of disease, to our knowledge, this attractive subclass of compounds is reviewed here for the first time.


Assuntos
Organismos Aquáticos/química , Produtos Biológicos/química , Dicetopiperazinas/química , Fungos/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Produtos Biológicos/farmacologia , Dicetopiperazinas/farmacologia , Dimerização , Humanos , Estrutura Molecular , Relação Estrutura-Atividade
15.
Mar Drugs ; 17(6)2019 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-31163615

RESUMO

Sea hares of Aplysia genus are recognized as a source of a diverse range of metabolites. 5α,8α-Endoperoxides belong to a group of oxidized sterols commonly found in marine organisms and display several bioactivities, including antimicrobial, anti-tumor, and immunomodulatory properties. Herein we report the isolation of 5α,8α-epidioxycholest-6-en-3ß-ol (EnP(5,8)) from Aplysia depilans Gmelin, based on bioguided fractionation and nuclear magnetic resonance (NMR) analysis, as well as the first disclosure of its anti-inflammatory properties. EnP(5,8) revealed capacity to decrease cellular nitric oxide (NO) levels in RAW 264.7 macrophages treated with lipopolysaccharide (LPS) by downregulation of the Nos2 (inducible nitric oxide synthase, iNOS) gene. Moreover, EnP(5,8) also inhibited the LPS-induced expression of cyclooxygenase-2 (COX-2), interleukin 6 (IL-6), and tumor necrosis factor alpha (TNF-α) at the mRNA and protein levels. Mild selective inhibition of COX-2 enzyme activity was also evidenced. Our findings provide evidence of EnP(5,8) as a potential lead drug molecule for the development of new anti-inflammatory agents.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Aplysia/química , Ésteres do Colesterol/química , Ésteres do Colesterol/farmacologia , Ergosterol/análogos & derivados , Macrófagos/efeitos dos fármacos , Adjuvantes Imunológicos/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Fracionamento Químico , Ésteres do Colesterol/isolamento & purificação , Regulação para Baixo/efeitos dos fármacos , Ativação Enzimática/efeitos dos fármacos , Ergosterol/química , Ergosterol/isolamento & purificação , Ergosterol/farmacologia , Lipopolissacarídeos/farmacologia , Espectroscopia de Ressonância Magnética , Camundongos , Óxido Nítrico Sintase Tipo II/genética , Células RAW 264.7
16.
Mar Drugs ; 17(6)2019 06 02.
Artigo em Inglês | MEDLINE | ID: mdl-31159480

RESUMO

The role of the marine environment in the development of anticancer drugs has been widely reviewed, particularly in recent years. However, the innovation in terms of clinical benefits has not been duly emphasized, although there are important breakthroughs associated with the use of marine-derived anticancer agents that have altered the current paradigm in chemotherapy. In addition, the discovery and development of marine drugs has been extremely rewarding with significant scientific gains, such as the discovery of new anticancer mechanisms of action as well as novel molecular targets. Approximately 50 years since the approval of cytarabine, the marine-derived anticancer pharmaceutical pipeline includes four approved drugs and eighteen agents in clinical trials, six of which are in late development. Thus, the dynamic pharmaceutical pipeline consisting of approved and developmental marine-derived anticancer agents offers new hopes and new tools in the treatment of patients afflicted with previously intractable types of cancer.


Assuntos
Antineoplásicos/química , Organismos Aquáticos/química , Descoberta de Drogas/tendências , Antineoplásicos/uso terapêutico , Sistemas de Liberação de Medicamentos , Humanos , Neoplasias/tratamento farmacológico
17.
Phytochem Anal ; 30(5): 547-555, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31148295

RESUMO

INTRODUCTION: Nowadays several plant species, such as Echinacea angustifolia L., can be considered natural important sources for therapeutic applications. Echinacea angustifolia is one of the most known medicinal plants, it shows protective and preventive effects against many chronic diseases, thanks to immunostimulant properties, mostly due to its polysaccharides and antioxidants. However, the optimisation of green extraction techniques to respect the environment is, currently, a hard challenge for the recovery of secondary metabolites. METHODOLOGY: Hydro-enzymatic extraction has been performed for the first time, it was compared with other different extraction techniques, for their efficacy in bioactive compound recovery. Phytochemical characterisation has been carried out through high-performance liquid chromatography diode array detector (HPLC-DAD) analysis and the antioxidant activity has been also measured. RESULTS: The highest extractive yields and the strongest antioxidant activity was obtained by cellulase and xylanase enzyme extraction. The enzymatic extraction with pectinase enzyme led to a higher polysaccharide content in comparison with the literature. The hydro-enzymatic extraction method and analytical conditions allowed the identification and quantification of two compounds, to the best of our knowledge, for the first time in E. angustifolia root extract. CONCLUSION: The optimised extraction methods discussed in this work led to a higher polysaccharides content, in comparison to previous literature results. The enzymatic extraction seems to be the best extraction technique, in terms of antioxidant yield and efficacy in bioactive compound recovery.


Assuntos
Antioxidantes/farmacologia , Echinacea/química , Química Verde/métodos , Compostos Fitoquímicos/análise , Extratos Vegetais/química , Antioxidantes/análise , Cromatografia Líquida de Alta Pressão/métodos , Raízes de Plantas/química
18.
Molecules ; 24(14)2019 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-31295972

RESUMO

Predominantly spread in West Tropical Africa, the shrub Salacia senegalensis (Lam.) DC. is known because of its medicinal properties, the leaves being used in the treatment of skin diseases. Prompted by the ethnomedicinal use, a hydroethanolic extract obtained from the leaves of the plant was screened against a panel of microbial strains, the majority of which involved in superficial infections. The extract was found to be active against the dermatophytes Trichophyton rubrum and Epidermophyton floccosum. Notable results were also recorded regarding the attenuation of the inflammatory response, namely the inhibitory effects observed against soybean 5-lipoxygenase (IC50 = 71.14 µg mL-1), no interference being recorded in the cellular viability of RAW 264.7 macrophages and NO levels. Relevantly, the extract did not lead to detrimental effects against the keratinocyte cell line HaCaT, at concentrations displaying antidermatophytic and anti-inflammatory effects. Flavonoid profiling of S. senegalensis leaves was achieved for the first time, allowing the identification and quantitation of myricitrin, three 3-O-substituted quercetin derivatives, and three other flavonoid derivatives, which may contribute, at least partially, to the observed antidermatophytic and anti-inflammatory effects. In the current study, the plant S. senegalensis is assessed concerning its antidermatophytic and anti-inflammatory properties.


Assuntos
Anti-Inflamatórios/farmacologia , Antifúngicos/farmacologia , Arthrodermataceae/efeitos dos fármacos , Flavonoides/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Salacia/química , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Antifúngicos/química , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Flavonoides/química , Humanos , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Macrófagos/metabolismo , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Compostos Fitoquímicos/química , Extratos Vegetais/química , Células RAW 264.7 , Análise Espectral
19.
J Chem Ecol ; 44(7-8): 658-670, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30039208

RESUMO

In the worldwide search for new strategies in sustainable weed management, the use of allelopathic plants incorporated into the soil as green manure can help control weeds by releasing allelochemicals into the environment. In previous experiments, Eucalyptus globulus leaves incorporated into the soil as green manure were shown to have a notable potential for weed control. But, 'what was exactly happening at chemical level?' and 'which were the compounds potentially responsible for the phytotoxic effects observed during those greenhouse assays?' In the present study, in-vitro phytotoxicity bioassays and chemical analysis of eucalyptus leaves were carried out in order to explore the relationship between the temporal phytotoxic effects and the dynamics of chemical composition. For that, eucalyptus leaves were removed from soil at different sampling times during 30 days and analyzed for phenolic and volatile organic compounds (VOCs) by HPLC and HS-SPME/GC-MS, respectively. The phytotoxic potential of the aqueous extract and the volatile fraction was tested on the germination and early growth of Lactuca sativa. Eucalyptus leaves incorporated into the soil as green manure showed a continuous release of different phenolic and volatile compounds during a 30-day period of decomposition. Both fractions had phytotoxic effects during the time assayed; however, the target process of phytotoxicity was different: phenolic compounds being the factor causing germination inhibition and VOCs responsible for growth reduction. The dynamics of release of this cocktail of allelochemicals into the soil environment may be the responsible for the phytotoxicity observed in our previous works.


Assuntos
Eucalyptus/fisiologia , Feromônios/metabolismo , Folhas de Planta/fisiologia , Alelopatia , Eucalyptus/química , Germinação/efeitos dos fármacos , Lactuca/efeitos dos fármacos , Lactuca/crescimento & desenvolvimento , Fenóis/análise , Fenóis/metabolismo , Feromônios/análise , Feromônios/toxicidade , Folhas de Planta/química , Solo/química , Compostos Orgânicos Voláteis/análise , Compostos Orgânicos Voláteis/metabolismo , Compostos Orgânicos Voláteis/toxicidade , Controle de Plantas Daninhas/métodos
20.
Int J Mol Sci ; 19(6)2018 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-29874826

RESUMO

Pyrrolizidine alkaloids (PA) are widely distributed in plants throughout the world, frequently in species relevant for human consumption. Apart from the toxicity that these molecules can cause in humans and livestock, PA are also known for their wide range of pharmacological properties, which can be exploited in drug discovery programs. In this work we review the current body of knowledge regarding the chemistry, toxicology, pharmacology and food safety of PA.


Assuntos
Inocuidade dos Alimentos , Plantas/química , Alcaloides de Pirrolizidina/química , Alcaloides de Pirrolizidina/farmacologia , Animais , Descoberta de Drogas , Humanos , Plantas/toxicidade , Alcaloides de Pirrolizidina/toxicidade
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA