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1.
Mutat Res ; 850-851: 503145, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32247555

RESUMO

5-Fluorouracil (5-FU) is a widely used antineoplastic drug. In this work, a comprehensive study was performed to detect the extent of chromosomal damage and morphological sperm defects induced by 5-FU in male mice and the possible protective role of the iridoids-rich fraction of Pentas lanceolata leaves (IFPL). Six main groups were examined in micronucleus and chromosomal assays: I- control negative, II- control positive (i.p. treated with single dose of 75 mg/kg 5-FU), III- control plant (orally administrated IFPL, 300 mg/kg, 5 consecutive days), and IV-VI- treated with IFPL (100, 200 and 300 mg/kg, 5 consecutive days) plus 5-FU (i.p. treated at the last day). Samples were taken 24 h post treatment. The study of morphological sperm anomalies, single and repeated treatments were examined and samples were taken after 35 days from the 1st treatment. In bone marrow, 5-FU induced a significant increase in the micro-nucleated polychromatic erythrocytes, chromosome anomalies (CAs) and also cytotoxic effects. A significant percentage of CAs was recorded in spermatocytes after 5-FU treatment reached 22.80 ± 1.32 vs 4.20 ± 0.37 for control (mainly X-Y univalent, 90%). IFPL was recorded to be non-mutagenic in all tests examined. In addition, it alleviated the previous defects in a dose-dependent manner. A significant and dramatic increase in the percentage of morphological sperm defects was recorded after single and repeated treatments with 5-FU reached 13.24 ± 0.24, 30.42 ± 0.32 respectively vs 2.56 ± 0.14 for control. Amorphous head-sperm and sperm with coiled tail were the most pronounced types of abnormalities. Significant protection was detected with the highest tested dose of IFPL. In conclusion: 5-FU demonstrated to be a genotoxic agent. Its genotoxicity in germ cells is serious and may lead to reproductive toxicity, infertility or heritable defects. The results also demonstrated the biosafety of IFPL and its possible protective role in combined treatment with 5-FU.


Assuntos
Iridoides/farmacologia , Extratos Vegetais/farmacologia , Rubiaceae/química , Espermatozoides/efeitos dos fármacos , Animais , Aberrações Cromossômicas/efeitos dos fármacos , Dano ao DNA/efeitos dos fármacos , Fluoruracila/efeitos adversos , Fluoruracila/uso terapêutico , Iridoides/química , Masculino , Camundongos , Testes de Mutagenicidade , Extratos Vegetais/química , Espermatócitos/efeitos dos fármacos , Espermatócitos/patologia , Espermatozoides/patologia
2.
Food Chem ; 316: 126351, 2020 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-32050114

RESUMO

The debittering of natural table olives is a very slow process. The effect of acetic, lactic and citric acids on the hydrolysis rate of oleuropein was studied in vitro and at pilot plant scale. The acid hydrolysis of oleuropein was faster with lactic and citric acids than acetic acid, running the experiments at the same pH of 3.8-4.0 units. The temperature exerted a high effect of the hydrolysis of oleuropein in a range of 10-30 °C and the concentration of the organic acid did not show a significant trend. Moreover, the in vitro results were confirmed with three lots of olives that presented a higher content of oleuropein after 3-7 months of preservation when they were processed with acetic acid rather than lactic acid and the opposite for hydroxytyrosol. These results open the possibility of accelerating the debittering of natural olives by preserving them with lactic acid instead of acetic acid.


Assuntos
Ácido Acético/química , Iridoides/química , Ácido Láctico/química , Olea/química , Hidrólise
3.
J Agric Food Chem ; 68(10): 3171-3183, 2020 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-32052628

RESUMO

Reversed-phase liquid chromatography with electrospray ionization-high-resolution/accuracy Fourier transform mass spectrometry (RPC-ESI-FTMS) and chemometrics were exploited to evaluate the influence of horizontal centrifugation by two- or three-phase decanters on the content of major phenolic secoiridoids in extravirgin olive oils (EVOOs). Despite the occurrence of other potential sources of variability typical of commercial olive oils, horizontal centrifugation was found to play a primary role, with a general increase of secoiridoid content occurring when two-phase decanters were used. As emphasized by principal component analysis (PCA), the increase involved preferentially oleacin and oleocanthal, when oxidative deterioration was purposely minimized during and/or after production, and oleuropein and ligstroside aglycones, when no vertical centrifugation was performed at the end of the productive cycle. The influence of the type of horizontal centrifugation was also emphasized by the elaboration of RPC-ESI-FTMS data based on hierarchical cluster analysis (HCA) and linear discriminant analysis (LDA).


Assuntos
Centrifugação/métodos , Manipulação de Alimentos/métodos , Iridoides/química , Azeite de Oliva/química , Fenóis/química , Cromatografia de Fase Reversa , Frutas/química , Olea/química , Oxirredução , Espectrometria de Massas por Ionização por Electrospray
4.
Molecules ; 25(1)2020 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-31906356

RESUMO

The crude drug ysypó hû (Adenocalymma marginatum DC., Bignoniaceae) is used traditionally by the Guarani of Eastern Paraguayan as a male sexual enhancer. The aim of the present study was to identify the main constituents of the crude drug and to evaluate the in vitro inhibitory activity towards the enzyme phosphodiesterase-5 (PDE-5). The main compounds were isolated by counter-current chromatography (CCC). The metabolites were identified by spectroscopic and spectrometric means. The chemical profiling of the extracts was assessed by high-performance liquid chromatography coupled to mass spectrometry (HPLC-MS/MS). The crude extract and main isolated compounds were tested for their PDE-5 inhibitory activity using commercial kits. The iridoid theviridoside and 4-hydroxy-1-methylproline were isolated as the main constituent of the crude drug. Four chlortheviridoside hexoside derivatives were detected for the first time as natural products. Chemical profiling by HPLC-MS/MS led to the tentative identification of nine iridoids, six phenolics, and five amino acids. The crude extracts and main compounds were inactive towards PDE-5 at concentrations up to 500 µg/mL. Iridoids and amino acid derivatives were the main compounds occurring in the Paraguayan crude drug. The potential of ysypó hû as a male sexual enhancer cannot be discarded, since other mechanisms may be involved.


Assuntos
Bignoniaceae/química , Iridoides/química , Inibidores da Fosfodiesterase 5/química , Extratos Vegetais/química , Aminoácidos/análise , Aminoácidos/química , Aminoácidos/isolamento & purificação , Bignoniaceae/metabolismo , Cromatografia Líquida de Alta Pressão , Misturas Complexas , Distribuição Contracorrente , Glicosídeos Iridoides , Iridoides/análise , Iridoides/isolamento & purificação , Paraguai , Fenóis/análise , Fenóis/química , Fenóis/isolamento & purificação , Inibidores da Fosfodiesterase 5/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/metabolismo , Espectrometria de Massas em Tandem
5.
Molecules ; 25(2)2020 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-31936853

RESUMO

Iridoids are a class of active compounds that widely exist in the plant kingdom. In recent years, with advances in phytochemical research, many compounds with novel structure and outstanding activity have been identified. Iridoid compounds have been confirmed to mainly exist as the prototype and aglycone and Ι and II metabolites, by biological transformation. These metabolites have been shown to have neuroprotective, hepatoprotective, anti-inflammatory, antitumor, hypoglycemic, and hypolipidemic activities. This review summarizes the new structures and activities of iridoids identified locally and globally, and explains their pharmacokinetics from the aspects of absorption, distribution, metabolism, and excretion according to the differences in their structures, thus providing a theoretical basis for further rational development and utilization of iridoids and their metabolites.


Assuntos
Iridoides , Modelos Biológicos , Compostos Fitoquímicos , Humanos , Iridoides/química , Iridoides/farmacocinética , Iridoides/uso terapêutico , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacocinética , Compostos Fitoquímicos/uso terapêutico
6.
Food Chem ; 314: 126183, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31972407

RESUMO

Phenolic compounds largely contribute to the nutraceutical properties of virgin olive oil (VOO), the organoleptic attributes and the shelf life due to their antioxidant capabilities. Due to the relevance of malaxation in the oil extraction process, we tested the effects of malaxation time on the concentrations of relevant phenolic compounds in VOO, and we evaluated the influence of performing malaxation under vacuum. An increase in malaxation time significantly decreased the concentrations of aglycone isomers of oleuropein and ligstroside but, conversely, increased the oleocanthal and oleacein contents. Additionally, malaxation under vacuum led to an increase in phenolic contents compared to standard conditions carried out at atmospheric pressure. Finally, we explored the possibility of predicting the VOO oxidative stability on the basis of the phenolic profile, and a model (R2 = 0.923; p < 0.0001) was obtained by combining the concentration of the VOO phenolic compounds and the main fatty acids.


Assuntos
Manipulação de Alimentos/métodos , Azeite de Oliva/química , Fenóis/análise , Fenóis/química , Aldeídos/análise , Aldeídos/química , Monoterpenos Ciclopentânicos/análise , Monoterpenos Ciclopentânicos/química , Ácidos Graxos/análise , Ácidos Graxos/química , Glucosídeos/análise , Glucosídeos/química , Iridoides/análise , Iridoides/química , Azeite de Oliva/análise , Oxirredução , Piranos/análise , Piranos/química , Temperatura , Fatores de Tempo
7.
Phytochemistry ; 171: 112247, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31927201

RESUMO

Four previously undescribed acylated iridoid glucosides, linaburiosides A‒D, one undescribed iridoid, 7-deoxyiridolactonic acid, and one known acylated iridoid glucoside, iridolinarin C, were isolated from the aerial parts of a Mongolian traditional herbal medicine, Linaria buriatica. Linaburiosides A‒D had an acyl moiety corresponding to 7-deoxyiridolactonic acid. Detailed spectroscopic analyses of linaburiosides A‒D and 7-deoxyiridolactonic acid led to the assignment of their structures. The absolute configuration of 7-deoxyiridolactonic acid was elucidated by application of the PGME method; those of linaburiosides A‒D were assigned on the basis of chemical conversions, as well as application of the modified Mosher's method. The absolute configuration of iridolinarin C was also elucidated in this study. Anti-inflammatory and antiproliferative activities of isolated compounds and their derivatives were evaluated.


Assuntos
Anti-Inflamatórios/farmacologia , Glucosídeos/farmacologia , Iridoides/farmacologia , Linaria/química , Compostos Fitoquímicos/farmacologia , Células A549 , Acilação , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Glucosídeos/química , Glucosídeos/isolamento & purificação , Humanos , Interleucina-1beta/antagonistas & inibidores , Interleucina-1beta/biossíntese , Iridoides/química , Iridoides/isolamento & purificação , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Células MCF-7 , Microglia/efeitos dos fármacos , Microglia/metabolismo , Conformação Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Células Tumorais Cultivadas
8.
Food Chem ; 314: 126204, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31978719

RESUMO

We examined the morphology of a network made with native BSA molecules being crosslinked with genipin at ambient temperature. Ninhydrin assay, FTIR, WAXD, SEM and mechanical tests documented successful crosslinking that enhanced the structural properties of the three dimensional structure. Its hydrophilic nature allows swelling with water absorption, which can be monitored with the modified Flory-Rehner theory to predict the molecular weight between adjacent crosslinks, network mesh size and crosslinking density as a function of crosslinker addition. Characterisation studies were carried out with a view to developing a delivery vehicle for the controlled release of vitamin B6 over a prolonged period of observation. Moving boundaries associated with swelling of the protein matrix resulted in vitamin transport that could be described with the interplay of diffusional and relaxational kinetics via the Peppas-Sahlin equation. Combination of diffusion and swelling equilibrium theories unveils a measurable effect of network characteristics on vitamin B6 release.


Assuntos
Iridoides/química , Soroalbumina Bovina/química , Vitamina B 6/química , Animais , Bovinos , Preparações de Ação Retardada/química , Difusão , Cinética , Peso Molecular
9.
Food Chem ; 310: 125976, 2020 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-31835230

RESUMO

Olive leaves extract (OLE) was spray-dried with maltodextrin (MD) or inulin (IN) to study the evolution of oleuropein (OE) during in vitro gastrointestinal digestion, its bioaccessibility and potential bioavailability. In the case of OLE-MD, OE was partially degraded in gastric and intestinal conditions; whereas in OLE-IN, OE was released under gastric conditions and partially degraded under intestinal conditions. In both cases, the encapsulation of OLE led to higher OE contents at the end of digestion, compared with non-encapsulated OLE, suggesting a protective role of the polysaccharides by the formation of non-covalent polysaccharides-OE complexes. OE bioaccessibility was ten times higher (p ≤ 0.05) in OLE-MD and OLE-IN than in non-encapsulated OLE. However, OE potential bioavailability, evaluated by tangential filtration, was not detected. Encapsulation technology and the encapsulant agent used may determine the release of the encapsulated compounds at a specific-site and their effect on health.


Assuntos
Produtos Biológicos/química , Inulina/química , Iridoides/farmacocinética , Polissacarídeos/química , Disponibilidade Biológica , Digestão , Inulina/metabolismo , Inulina/farmacocinética , Iridoides/química , Folhas de Planta/química , Polissacarídeos/farmacocinética
10.
Nat Prod Res ; 34(1): 78-86, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30896291

RESUMO

The quality of extra virgin olive oils is affected mainly by hydrolytic and oxidative reactions. The present paper investigated the changes of major and minor components and oxidation indices of three monovarietal extra virgin olive oils after 18 months of storage at room temperature and in dark glass bottles conditions. After storage, the basic quality parameters such as free acidity, peroxide values, extinction coefficients, fatty acids composition, chlorophyll and carotenoid content, did not exceed the upper limits set by European Community Regulations for extra-virgin olive oils. Given the importance of the phenolic fraction, UHPLC-HESI-MS metodology was used. A decrease in 3,4-DHPEA-EDA (oleacin) and p-HPEA-EDA (oleochantal) was detected whereas, an increase of tyrosol and hydroxytyrosol was measured as a consequence of degradation of ligstroside and oleuropein derivatives. Based on the results it is possible to observe the high nutritional value of the studied oils even after 18 months of conservation.


Assuntos
Qualidade dos Alimentos , Armazenamento de Alimentos , Azeite de Oliva/normas , Fenóis/análise , Ácidos Graxos/análise , Ácidos Graxos/química , Armazenamento de Alimentos/normas , Glucosídeos/química , Iridoides/química , Itália , Azeite de Oliva/análise , Oxirredução , Piranos/química
11.
J Sci Food Agric ; 100(5): 1842-1851, 2020 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-31802495

RESUMO

Extra virgin olive oil (EVOO), a key component of the Mediterranean diet, has aroused interest in recent years due to its health properties. Nuclear magnetic resonance (NMR) spectroscopy is an appropriate tool for the accurate quantification of minor compounds in complex food matrices, such as polyphenols in olive oil. Flavonoids, lignans, secoiridoids and phenolic acids and alcohols in EVOO have been identified and quantified by NMR. This review provides an overview of the major developments in the structural elucidation of polyphenol compounds in EVOO. © 2019 Society of Chemical Industry.


Assuntos
Espectroscopia de Ressonância Magnética/métodos , Azeite de Oliva/química , Polifenóis/química , Flavonoides/química , Iridoides/química , Lignanas/química
12.
Phytochemistry ; 170: 112199, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31759269

RESUMO

The Mediterranean crop Olea europaea is often exposed to high UV-B irradiation conditions. To understand how this species modulates its enzymatic and non-enzymatic antioxidant system under high UV-B radiation, young O. europaea plants (cultivar "Galega Vulgar") were exposed, for five days, to UV-B radiation (6.5 kJ m-2 d-1 and 12.4 kJ m-2 d-1). Our data indicate that UV-doses slightly differ in the modulation of the antioxidant protective mechanisms. Particularly, superoxide dismutase (SOD), guaiacol peroxidase (GPox) and catalase (CAT) activities increased contributing to H2O2 homeostasis, being more solicited by higher UV-B doses. Also, glutathione reductase (Gr) activity, ascorbate (AsA) and reduced glutathione (GSH) pools increased particularly under the highest dose, suggesting a higher mobilization of the antioxidant system in this dose. The leaf metabolites' profile of this cultivar was analysed by UHPLC-MS. Interestingly, high levels of verbascoside were found, followed by oleuropein and luteolin-7-O-glucoside. Both UV-B treatments affected mostly less abundant flavonoids (decreasing 4'-methoxy luteolin and 4' or 3'-methoxy luteolin glucoside) and hydroxycinnamic acid derivatives (HCAds, increasing ß-hydroxyverbascoside). These changes show not only different mobilization with the UV-intensity, but also reinforce for the first time the protective roles of these minor compounds against UV-B, as reactive oxygen species (ROS) scavengers and UV-B shields, in complement with other antioxidant systems (e.g. AsA/GSH cycle), particularly for high UV-B doses. Secoiridoids also standout in the response to both UV-B doses, with decreases of oleuropein and increases 2''-methoxyoleuropein. Being oleuropein an abundant compound, data suggest that secoiridoids play a more important role than flavonoids and HCAds, in O. europaea protection against UV-B, possibly by acting as signalling molecules and ROS scavengers. This is the first report on the influence of UV-B radiation on the secoiridoid oleuropein, and provides a novel insight to the role of this compound in the O. europaea antioxidant defence mechanisms.


Assuntos
Antioxidantes/metabolismo , Flavonoides/metabolismo , Iridoides/metabolismo , Olea/enzimologia , Raios Ultravioleta , Antioxidantes/química , Catalase/química , Catalase/metabolismo , Flavonoides/química , Iridoides/química , Peroxidase/química , Peroxidase/metabolismo , Compostos Fitoquímicos/química , Compostos Fitoquímicos/metabolismo , Superóxido Dismutase/química , Superóxido Dismutase/metabolismo
13.
Nat Prod Res ; 34(5): 683-691, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30325205

RESUMO

Four ursane-type triterpenoid glycosides (1-4), two benzophenone glycosides (5 and 6), and one iridoid glucoside (7) were isolated and characterized from the dried roots of Vangueria agrestis. Compounds 1 (3-O-[α-L-rhamnopyranosyl-(1→2)-ß-D-xylopyranosyl]pomolic acid 28-O-ß-D-glucopyranosyl ester) and 5 (2-O-[ß-D-apiofuranosyl-(1→6)-ß-D-glucopyranosyl]-6,4'-dihydroxy-4-methoxy benzophenone) were found to be new metabolites. The identity of all compounds has been accomplished, primarily, based on 1 D and 2 D NMR and HRESMS analysis. Compounds 6 and 2, showed inhibitory effect against Trypanosoma brucei with IC50 22.3 µM for 6 and IC50 11.1 µM, IC90 12.3 µM for 2.


Assuntos
Anti-Infecciosos/isolamento & purificação , Glicosídeos/isolamento & purificação , Rubiaceae/química , Anti-Infecciosos/química , Benzofenonas/química , Benzofenonas/isolamento & purificação , Glicosídeos/química , Iridoides/química , Iridoides/isolamento & purificação , Espectroscopia de Ressonância Magnética , Raízes de Plantas/química , Triterpenos/química , Triterpenos/isolamento & purificação
14.
Mater Sci Eng C Mater Biol Appl ; 107: 110362, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31761181

RESUMO

Genipin can improve weak mechanical properties and control high degradation rate of gelatin, as a cross-linker of gelatin which is widely used in tissue engineering. In this study, genipin cross-linked gelatin biodegradable porous scaffolds with different weight percentages of gelatin and genipin were prepared for tissue regeneration and measurement of their various properties including morphological characteristics, mechanical properties, swelling, degree of crosslinking and degradation rate. Results indicated that the sample containing the highest amount of gelatin and genipin had the highest degree of crosslinking and increasing the percentage of genipin from 0.125% to 0.5% enhances ultimate tensile strength (UTS) up to 113% and 92%, for samples with 2.5% and 10% gelatin, respectively. For these samples, increasing the percentage of genipin, reduce their degradation rate significantly with an average value of 124%. Furthermore, experimental data are used to develop a machine learning model, which compares artificial neural networks (ANN) and kernel ridge regression (KRR) to predict degradation rate of genipin-cross-linked gelatin scaffolds as a property of interest. The predicted degradation rate demonstrates that the ANN, with mean squared error (MSE) of 2.68%, outperforms the KRR with MSE = 4.78% in terms of accuracy. These results suggest that machine learning models offer an excellent prediction accuracy to estimate the degradation rate which will significantly help reducing experimental costs needed to carry out scaffold design.


Assuntos
Gelatina/química , Iridoides/química , Aprendizado de Máquina , Tecidos Suporte/química , Reagentes para Ligações Cruzadas/química , Gelatina/metabolismo , Teste de Materiais , Microscopia Eletrônica de Varredura , Modelos Teóricos , Redes Neurais de Computação , Análise de Regressão
15.
Molecules ; 25(1)2019 Dec 18.
Artigo em Inglês | MEDLINE | ID: mdl-31861384

RESUMO

Multifloroside (4), together with 10-hydroxyoleoside 11-methyl ester (1), 10-hydroxyoleoside dimethyl ester (2), and 10-hydroxyligustroside (3), are all secoiridoids, which are naturally occurring compounds that possess a wide range of biological and pharmacological activities. However, the anti-cancer activity of 1-4 has not been evaluated yet. The objective of this work was to study the anti-cancer activities of 1-4 in the human epidermoid carcinoma cell lines A431 and the human non-small cell lung cancer (NSCLC) cell lines A549. The results indicate that 1-4 differ in potency in their ability to inhibit the proliferation of human A431 and A549 cells, and multifloroside (4) display the highest inhibitory activity against A431 cells. The structure-activity relationships suggest that the o-hydroxy-p-hydroxy-phenylethyl group may contribute to the anti-cancer activity against A431 cells. Multifloroside treatment can also inhibit cell colony formation, arrest the cell cycle in the S-phase, increase the levels of reactive-oxygen-species (ROS), and mitochondrial membrane potential (MMP), but it did not significantly induce cell apoptosis at low concentrations. The findings indicated that multifloroside (4) has the tendency to show selective anti-cancer effects in A431 cells, along with suppressing the colony formation, inducing S cell cycle arrest, ROS production, and increasing MMP.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Iridoides/química , Iridoides/farmacologia , Metaloproteinases da Matriz/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Apoptose/efeitos dos fármacos , Carcinoma de Células Escamosas/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Estrutura Molecular , Transdução de Sinais/efeitos dos fármacos , Relação Estrutura-Atividade
16.
J Agric Food Chem ; 67(46): 12895-12903, 2019 Nov 20.
Artigo em Inglês | MEDLINE | ID: mdl-31682429

RESUMO

Genipin, a natural electrophilic cross-linker, was applied (5, 10, 20, and 30 mM) to modify hempseed protein isolate (HPI). Genipin treatments resulted in general losses of total sulfhydryls (up to 2.9 nmol/mg) and free amines (up to 77.3 nmol/mg). Surface hydrophobicity decreased by nearly 90% with 30 mM genipin, corresponding to similar tryptophan fluorescence quenching. The genipin treatment converted HPI into highly cross-linked polymers. Hydrogels formed with such polymers when also incorporated with hemp oil emulsions exhibited substantially enhanced gelling ability: up to 3.3- and 2.6-fold increases, respectively, in gel strength and gel elasticity over genipin-untreated protein. The genipin-modified composite gels also exhibited superior water-holding capacity. Microstructural analysis revealed a compact gel network filled with protein-coated oil globules that interacted intimately with the protein matrix when treated with genipin. Such gels remained readily digestible. Hence, genipin-treated hemp protein hydrogels show promise as functional food components.


Assuntos
Cannabis/química , Hidrogéis/química , Iridoides/química , Proteínas de Plantas/química , Reagentes para Ligações Cruzadas/química , Emulsões/química , Reologia , Sementes/química
17.
Molecules ; 24(23)2019 Nov 22.
Artigo em Inglês | MEDLINE | ID: mdl-31766682

RESUMO

In accordance with the provision in China Pharmacopoeia, Citrus aurantium L. (Sour orange-SZS) and Citrus sinensis Osbeck (Sweet orange-TZS) are all in line with the requirements of Aurantii Fructus Immaturus (ZS). Both kinds of ZS are also marketed in the market. With the frequent occurrence of depression, Zhi-Zi-Hou-Po decoction (ZZHPD) has attracted wide attention. Currently, studies have shown that ZZHPD has a potential toxicity risk, but the effect of two commercial varieties of ZS on ZZHPD has not been reported. In this study, the toxicity differences of ZZHPD prepared by SZS and TZS were revealed through repeated administration experiments in rats. This indicated that different varieties of ZS could affect the toxicity of the prescription. In order to further study the chemical material basis of the toxicity difference, the fingerprints of ZZHPD prepared by different varieties of ZS were established by high-performance liquid chromatography (HPLC). Five different characteristic peaks were screened by non-target chemometrics. They were identified as geniposide, neoeriocitrin, naringin, hesperidin, and neohesperidin using an HPLC-time-of-flight mass spectrometry analyzer (TOF/MS) and an HPLC-triple stage quadrupole mass spectrometry analyzer (QqQ-MS/MS). Combined with a quantitative analysis and previous studies on promoting the intestinal absorption of geniposide, it is speculated that the synergistic effects of the components may be the main reason for the difference of toxicity among the different medicinal materials. This study provides a reference for the clinical, safe use of ZZHPD, and also provides a new perspective for the study of the potential toxic substances of traditional Chinese medicine compound preparations.


Assuntos
Depressão/tratamento farmacológico , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/toxicidade , Iridoides/química , Iridoides/toxicidade , Animais , Cromatografia Líquida de Alta Pressão , Depressão/induzido quimicamente , Depressão/mortalidade , Dissacarídeos/isolamento & purificação , Dissacarídeos/toxicidade , Modelos Animais de Doenças , Sinergismo Farmacológico , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/efeitos adversos , Flavanonas/isolamento & purificação , Flavanonas/toxicidade , Hesperidina/análogos & derivados , Hesperidina/isolamento & purificação , Hesperidina/toxicidade , Absorção Intestinal , Iridoides/administração & dosagem , Iridoides/isolamento & purificação , Masculino , Ratos , Ratos Sprague-Dawley
18.
Daru ; 27(2): 695-708, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31768896

RESUMO

PURPOSE: Meningitis is an inflammation of meninges encircled the brain and spinal cord. Currently it can be treated with second generation cephalosporins which were ended up with an unresolvable problem called Multi Drug Resistance (MDR). Hence, there is a need to develop a better herbal molecule to conflict the MDR. METHODS: Hot Blanching technique followed by ultra sound assisted extraction using bio-solvent aqueous glycerol was used to extract OLE from olive leaves. QbD tool was applied to predict the interactions between Critical Material Attributes (Ratio of solid Lipid X1, Concentration of Surfactant X2) and Critical Process Parameters (Homogenization Time X3) on Critical Quality Attributes (CQA, Particle Size Y1, Zeta Potential Y2, and Entrapment Efficiency Y3). Particulate characteristics were evaluated and Invivo pharmacokinetic study was done in albino Wistar rats by IV and IN route of administration. RESULTS: Thermal studies reflect the formation of low ordered crystalline structure of lipid matrix which offers higher encapsulation of drug in NLC than physical mixture. CMA and CPP show significant effect on CQA and method operable design range was developed. Histo-pathological studies confirms that there is no signs of toxicity and in-vitro drug release studies reveals a rapid release of a drug initially followed by prolonged release of oleuropein upto 24 h. The absolute bioavailability of drug loaded NLC in brain was higher in IN route compared to NLC administered by IV route. CONCLUSIONS: In a nutshell, challenges offered by the hydrophilic OLE for brain targeting can be minimized through lipidic nature of NLC. Graphical Abstract.


Assuntos
Biologia Computacional/métodos , Iridoides/isolamento & purificação , Iridoides/farmacocinética , Nanoestruturas/química , Olea/química , Administração Intranasal , Administração Intravenosa , Animais , Disponibilidade Biológica , Química Farmacêutica , Liberação Controlada de Fármacos , Iridoides/química , Lipídeos/química , Masculino , Tamanho da Partícula , Folhas de Planta/química , Ratos , Ratos Wistar , Tensoativos
19.
Molecules ; 24(23)2019 Nov 23.
Artigo em Inglês | MEDLINE | ID: mdl-31771186

RESUMO

One new iridoid, namely neonanin C (1) one monocyclic iridoid ring-opened derivative namely neonanin D (2), two new bis-iridoid derivatives namely reticunin A (3) and reticunin B (4) with sixteen known compounds (5-20) were isolated from the stems of Neonauclea reticulata (Havil.) Merr. These new structures were determined by the detailed analysis of spectroscopic data and comparison with the data of known analogues. Compounds 1-20 were evaluated for inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages cell line. The results showed that all compounds exhibited no obvious cytotoxicity compared to the control group and five compounds including isoboonein (7), syringaresinol (10), (+)-medioresinol (12), protocatechuic acid (14) and trans-caffeic acid (15) exhibited inhibitory activities with IC50 values at 86.27 ± 3.45; 9.18 ± 1.90; 76.18 ± 2.42; 72.91 ± 4.97 and 95.16 ± 1.20 µg/mL, respectively.


Assuntos
Anti-Inflamatórios/farmacologia , Iridoides/farmacologia , Lipopolissacarídeos/efeitos adversos , Macrófagos/efeitos dos fármacos , Rubiaceae/química , Animais , Anti-Inflamatórios/química , Concentração Inibidora 50 , Iridoides/química , Macrófagos/citologia , Macrófagos/metabolismo , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Caules de Planta/química , Células RAW 264.7
20.
ACS Appl Mater Interfaces ; 11(45): 41898-41905, 2019 Nov 13.
Artigo em Inglês | MEDLINE | ID: mdl-31638378

RESUMO

Photothermal nanodrugs based on biomolecules are critically important for advancing photothermal therapy (PTT). However, constructing photothermal nanodrugs from biomolecules is highly challenging because most biomolecules are inherently nonpigmented. Herein, we synthesize well-defined, uniform photothermal nanodrugs through a covalent assembly approach by using nonpigmented peptides and iridoids as building blocks. The resulting photothermal nanodrugs show broad absorption from the UV to the near-infrared region, high photothermal conversion efficiency along with robust photostability, and selective tumor accumulation, leading to highly efficient tumor ablation via PTT. This work represents the first example of photothermal nanodrugs that can be constructed by using nonpigmented biomolecules as building blocks and thus will conceivably promote the preclinical evaluation and clinical translation of PTT.


Assuntos
Antineoplásicos/administração & dosagem , Antineoplásicos/química , Sistemas de Liberação de Medicamentos/métodos , Neoplasias/tratamento farmacológico , Animais , Sistemas de Liberação de Medicamentos/instrumentação , Humanos , Iridoides/administração & dosagem , Iridoides/química , Camundongos , Nanopartículas/administração & dosagem , Nanopartículas/química , Peptídeos/química , Fotoquimioterapia
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