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1.
Artigo em Inglês | MEDLINE | ID: mdl-34500401

RESUMO

Extracts from the bran of Chenopodium quinoa Willd. (QBE) were reported to be active in inhibiting α-glycosidase, a promising target for treatment of diabetes mellitus. However, the constituents responsible for the α-glucosidase-inhibiting activity of QBE have not been fully characterized. The present study aimed to set up a method for rapid identification of glycosidase inhibiting compounds from the quinoa bran. With surface plasmon resonance (SPR) coupled with liquid chromatography-mass spectrometry (LC-MS), we identified eight flavonoids and ten triterpenoid saponins that may bind to the α-glycosidase. Analysis of the interaction kinetics by molecular docking supported their α-glucosidase-inhibiting activity and revealed the potential mechanisms for the inhibitory effects. In summary, this study established a SPR and LC-MS-based method for rapid in vitro screening of α-glucosidase inhibitors and suggested the quinoa bran a potential natural source of α-glucosidase inhibitors.

2.
Food Chem ; 371: 131080, 2021 Sep 08.
Artigo em Inglês | MEDLINE | ID: mdl-34537620

RESUMO

Anthocyanins of Lycium ruthenicum (LR) are valuable, whereas stabilities, especially colour stabilities, constrain development. This study investigates stored temperature effects on the stability of powdered anthocyanin extracts of LR in anaerobic conditions and colour changes in simulated applications. We found that temperature had limited effects on anthocyanin contents but negative effects on colour. Colour differences (ΔE) were amplified in simulated applications, 4 °C had the most changes in ΔE in simulated applications, 37 °C caused shrinkage of the colour range towards the yellow area, and changes in ΔE at pH 7 and 9 were summarized by models. In conclusion, during anaerobic storage of powdered anthocyanins, asynchronous changes occur between anthocyanin contents and colour. High storage temperature attenuates colour intensity, but low storage temperature causes more ΔE in applications. Established models are beneficial for decreasing the visual differences in products, deepening the understanding, and offering a new perspective on colour analysis.

3.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4069-4082, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34467716

RESUMO

Trigonella foenum-graecum is an annual plant of the genus Trigonella in the Leguminosae family. It is widely distributed in China and has a long history of application. According to phytochemistry research, the seeds, stem, and leaves of this herb contain not only a variety of bioactive ingredients, including alkaloids, saponins, polysaccharides, flavonoids, and phenols, but also abundant nutrients such as unsaturated fatty acids and amino acids and various trace elements. Pharmacological studies have shown that both the extract of T. foenum-graecum and its chemical constituents exhibit hypoglycemic, hypolipidemic, antitumor, antioxidative, antimicro-bial, and hepatoprotective activities. This paper reviews the research progress on the chemical constituents and pharmacological effects of T. foenum-graecum, which may contribute to further development, application, and clinical research of this herb.


Assuntos
Trigonella , Antioxidantes/farmacologia , Hipoglicemiantes , Extratos Vegetais/farmacologia , Sementes
4.
Int J Mol Sci ; 22(16)2021 Aug 17.
Artigo em Inglês | MEDLINE | ID: mdl-34445549

RESUMO

Nonalcoholic fatty liver disease (NAFLD) is one of the most common liver diseases which lacks ideal treatment options. Kaempferol and kaempferide, two natural flavonol compounds isolated from Hippophae rhamnoides L., were reported to exhibit a strong regulatory effect on lipid metabolism, for which the mechanism is largely unknown. In the present study, we investigated the effects of kaempferol and kaempferide on oleic acid (OA)-treated HepG2 cells, a widely used in vitro model of NAFLD. The results indicated an increased accumulation of lipid droplets and triacylglycerol (TG) by OA, which was attenuated by kaempferol and kaempferide (5, 10 and 20 µM). Western blot analysis demonstrated that kaempferol and kaempferide reduced expression of lipogenesis-related proteins, including sterol regulatory element-binding protein 1 (SREBP1), fatty acid synthase (FAS) and stearoyl-CoA desaturase 1 (SCD-1). Expression of peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT enhancer binding proteins ß (C/EBPß), two adipogenic transcription factors, was also decreased by kaempferol and kaempferide treatment. In addition, western blot analysis also demonstrated that kaempferol and kaempferide reduced expression of heme oxygenase-1 (HO-1) and nuclear transcription factor-erythroid 2-related factor 2 (Nrf2). Molecular docking was performed to identify the direct molecular targets of kaempferol and kaempferide, and their binding to SCD-1, a critical regulator in lipid metabolism, was revealed. Taken together, our findings demonstrate that kaempferol and kaempferide could attenuate OA-induced lipid accumulation and oxidative stress in HepG2 cells, which might benefit the treatment of NAFLD.


Assuntos
Carcinoma Hepatocelular/tratamento farmacológico , Fígado Gorduroso/tratamento farmacológico , Quempferóis/farmacologia , Neoplasias Hepáticas/tratamento farmacológico , Ácido Oleico/efeitos adversos , Estresse Oxidativo/efeitos dos fármacos , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Fígado Gorduroso/induzido quimicamente , Fígado Gorduroso/metabolismo , Fígado Gorduroso/patologia , Células Hep G2 , Humanos , Lipogênese , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Transdução de Sinais
5.
Molecules ; 26(15)2021 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-34361714

RESUMO

α-glucosidase is a major enzyme that is involved in starch digestion and type 2 diabetes mellitus. In this study, the inhibition of hypericin by α-glucosidase and its mechanism were firstly investigated using enzyme kinetics analysis, real-time interaction analysis between hypericin and α-glucosidase by surface plasmon resonance (SPR), and molecular docking simulation. The results showed that hypericin was a high potential reversible and competitive α-glucosidase inhibitor, with a maximum half inhibitory concentration (IC50) of 4.66 ± 0.27 mg/L. The binding affinities of hypericin with α-glucosidase were assessed using an SPR detection system, which indicated that these were strong and fast, with balances dissociation constant (KD) values of 6.56 × 10-5 M and exhibited a slow dissociation reaction. Analysis by molecular docking further revealed that hydrophobic forces are generated by interactions between hypericin and amino acid residues Arg-315 and Tyr-316. In addition, hydrogen bonding occurred between hypericin and α-glucosidase amino acid residues Lys-156, Ser-157, Gly-160, Ser-240, His-280, Asp-242, and Asp-307. The structure and micro-environment of α-glucosidase enzymes were altered, which led to a decrease in α-glucosidase activity. This research identified that hypericin, an anthracene ketone compound, could be a novel α-glucosidase inhibitor and further applied to the development of potential anti-diabetic drugs.


Assuntos
Antracenos/química , Proteínas Fúngicas/antagonistas & inibidores , Inibidores de Glicosídeo Hidrolases/química , Hipoglicemiantes/química , Perileno/análogos & derivados , alfa-Glucosidases/química , Antracenos/metabolismo , Sítios de Ligação , Proteínas Fúngicas/química , Proteínas Fúngicas/metabolismo , Inibidores de Glicosídeo Hidrolases/metabolismo , Humanos , Ligação de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Hipoglicemiantes/metabolismo , Cinética , Simulação de Acoplamento Molecular , Nitrofenilgalactosídeos/química , Nitrofenilgalactosídeos/metabolismo , Perileno/química , Perileno/metabolismo , Ligação Proteica , Conformação Proteica em alfa-Hélice , Conformação Proteica em Folha beta , Domínios e Motivos de Interação entre Proteínas , Saccharomyces cerevisiae/classificação , Saccharomyces cerevisiae/enzimologia , Ressonância de Plasmônio de Superfície , alfa-Glucosidases/metabolismo
6.
Colloids Surf B Biointerfaces ; 207: 112004, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34339971

RESUMO

For minimizing volatilization and leaching of pesticides, and enhancing their residence time on crop surfaces, we synthesized and characterized a novel intelligent pesticide delivery system. Therein, imidacloprid (IMI) was adsorbed by polydopamine modified kaolin (PK) with high adsorption property through hydrogen bonds. Ca-alginate was used as a structural matrix of the system and a protective shell to hinder the pesticide burst release from PK, and endowed the system with unique pH-sensitive property for IMI release. The amino silicone oil (ASO) coating could bind with the waxy layer of crop leaves by the theory of "similarity-intermiscibility", which increased the adhesion of composite on crop leaves. Moreover, by the excellent light-sensitive property of detonation nanodiamond (DND) and temperature-responsive performance of poly(N-isopropylacrylamide) (PNIPAm), the release of IMI from the functional system could be adjusted by sunlight. Besides, the composite displayed high control efficacy. This novel composite can promote the targeting ability and utilization efficiency of pesticides, thus having a huge potential application prospect in agriculture.


Assuntos
Alginatos , Praguicidas , Adsorção , Agricultura , Humanos , Aderências Teciduais
7.
J Food Sci ; 86(10): 4365-4375, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34431095

RESUMO

Anthocyanins are a group of flavonoids widely used as natural pigments and in functional foods. However, the sensitivity of anthocyanins to environment factors limits their utilization. The present study examined the stabilizing effects of polyphenol extracts from raspberry, sea-buckthorn, Lonicera edulis, and blackcurrant on Lycium ruthenicum Murr (LRM)-derived anthocyanins. After light and heat exposure, contents of total anthocyanins and the monomers were detected with the pH differential method and the HPLC. Remarkably, polyphenol extracts from raspberry, Lonicera edulis and blackcurrant extended the half-lives of anthocyanins, while the effect of the sea-buckthorn extracts was negligible. Noticeably, petunidin-3-O-[6-O-(4-O-trans-p-coumaroyl-alpha-L-rhamnopyranosyl)-beta-D-glucopyranoside]-5-O-[beta-D-glucopyranoside], the major component of LRM-derived anthocyanins, exhibited a dramatic increase in half-life with the presence of polyphenol extracts from raspberry, Lonicera edulis, and blackcurrant. In summary, our findings suggest the polyphenol extracts could be developed into copigments for stabilization of anthocyanins.

8.
Water Sci Technol ; 84(3): 737-751, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34388131

RESUMO

The authors reported a potential candidate methylated mud snail protein (MeMsp) as an effective and eco-friendly flocculant to treat the high turbidity wastewater. MeMsp was obtained by extraction of mud snail protein (Msp) through isoelectric precipitation (PSC-IP) and then methylated via the esterification with side-chain carboxyl. Structural characterization of FT-IR, zeta potential and elemental analysis were carried out and further confirmed the successful of the methylation. Flocculation experiments with kaolin suspension simulated wastewater indicated that MeMsp-24 displayed more excellent flocculation efficiency at a low dosage. At the optimum dosage 27 mg/L, the maximum clarification efficiency of MeMsp-24 was 97.46% under pH 7.0. Furthermore, MeMsp-24 exhibited a wide flocculation window in the pH range 1.0-9.0, and faster sedimentation velocity and larger flocs size. In addition, MeMsp-24 exhibited 92.12% clarification efficiency in treating railway tunnel construction effluent. The flocculation kinetic and mechanism analysis revealed that the most effective particle collision occurred at the optimal dosage, with charge neutralization and adhesion playing irreplaceable roles in different environments, respectively. Therefore, through extraction and methylation modification, MeMsp could be a promising eco-friendly flocculant for high turbidity wastewater treatment.


Assuntos
Purificação da Água , Animais , Floculação , Caulim , Caramujos , Espectroscopia de Infravermelho com Transformada de Fourier
9.
Int J Biol Macromol ; 186: 71-78, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34216671

RESUMO

Nitraria tangutorum Bobr. is suggested to be active in immunoregulation and antioxidation. However, the in vivo bioactivity of N. tangutorum Bobr.-derived polysaccharides (NTP) and their anti-inflammatory activity have not been addressed. In the present study, we extracted and purified polysaccharides from N. tangutorum Bobr. and determined their anti-inflammatory activities in vivo. HPGPC, UHPLC/DAD, and NMR analyses identified that the monosaccharide components of NTP were Man, Rha, GalUA, Glu, Gal, and Ara, with relative contents of 3.52%, 15.08%, 10.00%, 26.73%, 38.08%, and 6.59%, respectively. In mice with lipopolysaccharide (LPS)-induced Acute Lung Injury (ALI), NTP treatment attenuated tissue damage, inhibited the production of inflammatory cytokines, and promoted the anti-oxidative response. The supposed mechanism may be via suppressing the Toll-like receptor 4 (TLR4) signaling pathway. In conclusion, our study suggests a protective role of NTP in LPS-induced ALI by inhibiting inflammatory damage.

10.
Molecules ; 26(7)2021 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-33808398

RESUMO

BACKGROUND: Doxorubicin (Dox) is one of the most frequently prescribed anti-cancer drugs. However, clinical application with Dox is limited due to its potentially fatal cumulative cardiotoxicity. N-p-coumaroyl-4-aminobutan-1-ol (alk-A), an organic amide alkaloid and hippophamide (alk-B), a rare pyridoindole alkaloid were successfully obtained by purification and separation of seabuckthorn seed residue in our previous research. This study was undertaken to investigate the protective effect of alk-A and alk-B against Dox-induced embryonic rat cardiac cells (H9c2 cells) apoptosis. METHODS: H9c2 cells were treated with Dox (2.5 µM) in the presence of alk-A and alk-B (10, 20, and 40 µM) and incubated for 24 h. RESULTS: It was shown that pretreatment of the H9c2 cells with alk-A and alk-B significantly reduced Dox-induced apoptosis. Alk-A and alk-B both inhibited reactive oxygen species (ROS) production and suppressed cleaved-caspase-3 protein expression and the activation of JNK (Jun N-terminal kinases), as well as increasing ATP levels, favoring mitochondrial mitofusin protein expression, and relieving damage to mitochondrial DNA. CONCLUSIONS: These results suggest that alk-A and alk-B can inhibit Dox-induced apoptosis in H9C2 cardiac muscle cells via inhibition of cell apoptosis and improvement of mitochondrial function, while alk-B showed more protection. Alk-B could be a potential candidate agent for protecting against cardiotoxicity in Dox-exposed patients.


Assuntos
Alcaloides/farmacologia , Antioxidantes/farmacologia , Apoptose/efeitos dos fármacos , Cardiotoxicidade/tratamento farmacológico , Hippophae/química , Miócitos Cardíacos/efeitos dos fármacos , Animais , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Doxorrubicina/efeitos adversos , Mitocôndrias/efeitos dos fármacos , Proteínas Mitocondriais/metabolismo , Miócitos Cardíacos/patologia , Estresse Oxidativo/efeitos dos fármacos , Ratos , Espécies Reativas de Oxigênio/metabolismo
11.
Food Chem ; 353: 129435, 2021 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-33714113

RESUMO

An anthocyanin-rich extract was obtained from Nitraria tangutorum Bobr. fruit, namely ANF, and its composition, antioxidant and neuroprotective effects were studied. Nine anthocyanins were identified from the ANF using UPLC-Triple-TOF/MS analysis, and cyanidin-3-[2''-(6'''-coumaroyl)-glucosyl]-glucoside (C3G) is the most abundant anthocyanin (87.06%). ANF exhibited high ferric reducing antioxidant power (FRAP) and ABTS radical scavenging activity. The online HPLC-DPPH screening revealed that C3G contributed the highest antioxidant capacity. ANF showed potential neuroprotective effects by relieving d-Galactose-induced memory deficits, reducing overexpression of receptor for advanced glycation end products (RAGE) and amyloid-beta42 (Aß42) in the hippocampus of rats. Besides, ANF could inhibit oxidative stress by reducing the levels of reactive oxygen species (ROS) and malondialdehyde (MDA) in the hippocampus, while elevating amounts of total superoxide dismutase (T-SOD) and glutathione (GSH) in the serum of rats. Thus, ANF has great potential in the development of food and health products related to antioxidant and neuroprotective effects.


Assuntos
Antocianinas/análise , Antioxidantes/química , Cromatografia Líquida de Alta Pressão , Magnoliopsida/química , Fármacos Neuroprotetores/análise , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz , Peptídeos beta-Amiloides/genética , Peptídeos beta-Amiloides/metabolismo , Animais , Antocianinas/química , Antocianinas/isolamento & purificação , Antocianinas/farmacologia , Feminino , Frutas/química , Frutas/metabolismo , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Magnoliopsida/metabolismo , Malondialdeído/metabolismo , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Fármacos Neuroprotetores/farmacologia , Fragmentos de Peptídeos/genética , Fragmentos de Peptídeos/metabolismo , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/metabolismo , Receptor para Produtos Finais de Glicação Avançada/genética , Receptor para Produtos Finais de Glicação Avançada/metabolismo , Superóxido Dismutase/metabolismo
12.
Mol Med Rep ; 23(4)2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33576438

RESUMO

Malignant tumors of the central nervous system (CNS) are among the types of cancer with the poorest prognosis and glioma is the commonest primary CNS tumor. A mitochondrial DNA (mtDNA)­depleted cell line C6ρ0 was generated from C6 glioma cells after long­term exposure to ethidium bromide and 2',3'­dideoxycytidine in order to determine the effect of mtDNA damage on cell proliferation and pathological changes in glioma cells. Single cell clones were isolated and identified after 42 days of incubation. Repopulated cybrids were formed when the clonal C6ρ0 cells were fused with rat platelets and no difference was observed in their growth in a selective medium without uridine and pyruvate compared with the growth of the parent C6 cells. Disruption of mtDNA resulted in changes in mitochondrial morphology, decreased cell proliferation, reduced intracellular reactive oxygen species and intracellular ATP, along with decreased mtDNA and mitochondrial membrane potential in C6ρ0 cells compared with the C6 cells. Taken together, C6ρ0 cells without mtDNA were established for the first time and their characteristics were compared with parent cells. This C6ρ0 cell line could be used to explore the contribution of mitochondrial dysfunction and mtDNA mutations in the pathogenesis of glioma.


Assuntos
Neoplasias Encefálicas/genética , DNA Mitocondrial/genética , Glioma/genética , Mitocôndrias/genética , Trifosfato de Adenosina/metabolismo , Animais , Neoplasias Encefálicas/metabolismo , Neoplasias Encefálicas/patologia , Linhagem Celular Tumoral , Proliferação de Células/genética , DNA Mitocondrial/metabolismo , Glioma/metabolismo , Glioma/patologia , Espaço Intracelular/metabolismo , Potencial da Membrana Mitocondrial/genética , Potencial da Membrana Mitocondrial/fisiologia , Mitocôndrias/metabolismo , Ratos , Espécies Reativas de Oxigênio/metabolismo
13.
ISA Trans ; 111: 249-264, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33272588

RESUMO

Compared with preprocessed obstacle environments, unknown environments are more challenging for path planning. In unknown environments, an agent can make decisions only by relying on the obstacle information detected by its onboard sensors. However, when facing non-convex obstacles, this limited detection information can easily trap the agent in a local optimum. In this paper, a nature-inspired methodology called Interfered Fluid Dynamic System (IFDS) is extended to anti-local-optimum obstacle avoidance in unknown 3D environments for the first time and a novel fluid-based path planning framework is proposed. First, the detection region of the agent is discretized. Then, spherical virtual obstacles (SVOs) located at detected discrete points are generated and memorized. Thus, obstacle avoidance in unknown environments is transformed into the avoidance of known SVOs. Next, the currently generated and memorized SVOs are input to the core of the framework, the IFDS algorithm, to produce repulsive effects, and the corresponding 3D avoidance path is resolved. On this basis, to address local optimum in cases with non-convex obstacles, and considering compatibility with the IFDS, the direction coefficient and sink-heading angular rate adjustment strategies, which belong to the same system as the IFDS, are introduced to modify the IFDS in this framework. Finally, receding horizon control is introduced to improve the obstacle avoidance performance. Simulations show that the proposed framework can enable the agent to autonomously jump out of the 3D non-convex obstacle environments with typical features of the local optimum, including wall-like and cave-like obstacles, and safely reach the destination.

14.
Biomed Pharmacother ; 131: 110800, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33152953

RESUMO

The present study investigated the anti-diabetic effects of Oligostilbenes extracts (Olie) from Iris lactea Pall. var. chinensis (Fisch.) Koidz (I. lactea) and the potential mechanisms, in high-fat-diet (HFD)-induced diabetic mice and 3T3-L1 adipocytes. Olie are a group of major active extracts from I. lactea that have been used as nutraceutical because of their antioxidant activity. Six-week Olie treatment improved fasting blood glucose levels, as well as blood lipid profiles in HFD/streptozocin (STZ)-induced diabetic mice, compared with non-treated mice. Olie treatment upregulated the levels of phosphorylated of AMPK and lipolysis-related proteins, while the hepatic expression of ACC and FAS in diabetic mice was inhibited. In cultured 3T3-L1 cells, Olie (2-15 µg/mL) treatment dose-dependently suppressed the differentiation into mature adipocytes and lowered cellular lipid accumulation. Consistently, Olie reduced expression of adipogenic transcription factors including CCAAT/enhancer-binding protein ß (C/EBPß) and peroxisome proliferator-activated receptor γ (PPARγ). In addition, mitochondrial function in 3T3-L1 adipocytes was improved after Olie treatment. Taken together, our findings indicate that a lipid-lowering effect of Olie in HFD/STZ-induced diabetic mice and adipogenesis/ lipogenesis suppressing effect in 3T3-L1 cells, via regulating the expression of lipid metabolism-related proteins.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Iris/química , Extratos Vegetais/farmacologia , Estilbenos/farmacologia , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Adipogenia/efeitos dos fármacos , Animais , Dieta Hiperlipídica , Relação Dose-Resposta a Droga , Hipolipemiantes/administração & dosagem , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipogênese/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/administração & dosagem , Estilbenos/administração & dosagem , Estilbenos/isolamento & purificação , Estreptozocina
15.
Int J Biol Macromol ; 160: 518-530, 2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-32479948

RESUMO

The multi-responsive controlled-release system could enhance crop yield while improving utilization efficiency of agrochemicals, and minimize environmental pollution caused by agrochemicals overuse. This work reports a novel Ca-alginate/Poly(N-isopropylacrylamide)@polydopamine (Ca-alginate/PNIPAm@PDA) microsphere to control the agrochemicals release. Microsphere with a semi-interpenetrating network, which contained pH-sensitive Ca-alginate, temperature-sensitive poly(N-isopropylacrylamide) (PNIPAm), and sunlight-sensitive polydopamine (PDA), was characterized by thermogravimetric analysis, zeta potential, Fourier transform infrared spectroscopy, and scanning electron microscopy to prove the successful synthesis. Moreover, the comprehensive performances, including photothermal conversion, water absorbency, water retention, and controlled-release agrochemicals behaviors, were systematically investigated. The results indicated that the composite microsphere was a prosperous water and agrochemicals manager to effectively retain water and control the release of agrochemicals by external stimulation. Consequently, the Ca-alginate/PNIPAm@PDA microsphere with outstanding water-retention and controlled-release capacities is economical and eco-friendly and thus is promising for utilization as water and agrochemicals controlled-release carrier material in agriculture applications.


Assuntos
Resinas Acrílicas/química , Agroquímicos/química , Alginatos/química , Cálcio/química , Preparações de Ação Retardada/química , Dopamina/química , Água/química , Concentração de Íons de Hidrogênio , Indóis/química , Microscopia Eletrônica de Varredura/métodos , Microesferas , Polímeros/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Temperatura
16.
Chem Biodivers ; 17(7): e2000187, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32384197

RESUMO

(20S)-Protopanaxadiol ginsenosides Rg3, Rh2 and PPD have been demonstrated for their anticancer activity. However, the underlying mechanism of their antitumor activity remains unclear. In the present study, we investigated the role of these three ginsenosides on cell proliferation and death of human gastric cancer cells (HGC-27 cells). The sulforhodamine B (SRB) assay, Western blot analysis, fluorescence microscopy, confocal microscopy, high performance liquid chromatography (HPLC) analysis, flow cytometry, and transmission electron microscopy (TEM) were used to evaluate cell proliferation, apoptosis, and autophagy. The results showed that both Rh2 and PPD were more effective than Rg3 in inhibiting HGC-27 cell proliferation and inducing cytoplasmic vacuolation, while no significant changes in apoptosis were observed. Interestingly, cytoplasmic vacuolation and blockade of autophagy flux were observed after treatment with Rh2 and PPD. Rh2 obviously up-regulated the expression of the LC3II and p62. Furthermore, the increase in lysosomal pH and membrane rupture was observed in Rh2-treated and PPD-treated cells. When HGC-27 cells were pretreated with bafilomycin A1, a specific inhibitor of endosomal acidification, cellular vacuolization was increased, and the cell viability was significantly decreased, which indicated that Rh2-induced lysosome-damage accelerated cell death. Furthermore, data derived from mitochondrial analysis showed that excessive mitochondrial reactive oxygen species (ROS) and dysregulation of mitochondrial energy metabolism were caused by Rh2 and PPD treatment in HGC-27 cells. Taken together, these phenomena indicated that Rh2 and PPD inhibited HCG-27 cells proliferation by inducing mitochondria damage, dysfunction of lysosomes, and blockade of autophagy flux. The number of glycosyl groups at C-3 position could have an important effect on the cytotoxicity of Rg3, Rh2 and PPD.


Assuntos
Antineoplásicos/farmacologia , Autofagia/efeitos dos fármacos , Ginsenosídeos/farmacologia , Sapogeninas/farmacologia , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Ginsenosídeos/química , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Estrutura Molecular , Espécies Reativas de Oxigênio/análise , Espécies Reativas de Oxigênio/metabolismo , Sapogeninas/química , Relação Estrutura-Atividade , Células Tumorais Cultivadas
17.
Molecules ; 25(8)2020 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-32316267

RESUMO

Characterization of the structure and pharmacological activity of Berberis dasystachya Maxim., a traditional Tibetan medicinal and edible fruit, has not yet been reported. In this study, central composite design (CCD) combined with response surface methodology (RSM) was applied to optimize the extraction conditions of B. dasystachya oil (BDSO) using the supercritical carbon dioxide (SC-CO2) extraction method, and the results were compared with those obtained by the petroleum ether extraction (PEE) method. The chemical characteristics of BDSO were analyzed, and its antioxidant activity and in vitro cellular viability were studied by DPPH, ABTS, reducing power assay, and MTT assay. The results showed that the maximum yield of 12.54 ± 0.56 g/100 g was obtained at the optimal extraction conditions, which were: pressure, 25.00 MPa; temperature 59.03 °C; and CO2 flow rate, 2.25 SL/min. The Gas chromatography (GC) analysis results showed that BDSO extracted by the SC-CO2 method had higher contents of unsaturated fatty acids (85.62%) and polyunsaturated fatty acids (57.90%) than that extracted by the PEE method. The gas chromatography used in conjunction with ion mobility spectrometry (GC-IMS) results showed that the main volatile compounds in BDSO were aldehydes and esters. BDSO also exhibited antioxidant ability in a dose-dependent manner. Moreover, normal and cancer cells incubated with BDSO had survival rates of more than 85%, which indicates that BDSO is not cytotoxic. Based on these results, the BDSO extracted by the SC-CO2 method could potentially be used in other applications, e.g., those that involve using berries of B. dasystachya.


Assuntos
Antioxidantes/análise , Berberis/química , Óleos Vegetais/análise , Antioxidantes/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Cromatografia com Fluido Supercrítico , Óleos Vegetais/farmacologia , Sementes/química
18.
Pak J Pharm Sci ; 33(2): 669-674, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32276913

RESUMO

Analysis of the constituents of the chloroform extract of Oxytropis falcata Bunge (CEOF), a traditional Tibetan medicine, in rat's serum after oral administration, has been performed by HPLC-MS. We have identified 10 compounds in CEOF and 11 bioactive ingredients from rat's serum after given CEOF. Six bioactive ingredients from rat's serum are matched with original form of the compounds of CEOF. Other five bioactive ingredients were seemed to be respectively metabolites. HPLC-MS is rapid, sensitive method and suitable for identification of bioactive components absorbed into blood of CEOF providing information for further research of pharmacological mechanism.


Assuntos
Clorofórmio/análise , Clorofórmio/química , Oxytropis , Extratos Vegetais/análise , Extratos Vegetais/química , Espectrometria de Massas em Tandem/métodos , Animais , Cromatografia Líquida de Alta Pressão/métodos , Feminino , Masculino , Microssomos Hepáticos/química , Microssomos Hepáticos/metabolismo , Ratos , Ratos Sprague-Dawley
19.
Int J Mol Sci ; 21(6)2020 Mar 16.
Artigo em Inglês | MEDLINE | ID: mdl-32188147

RESUMO

Proanthocyanidins are the major active compounds extracted from Iris lactea Pall. var. Chinensis (Fisch.) Koidz (I. lactea). Proanthocyanidins exhibit a variety of pharmacological activities such as anti-oxidation, anti-inflammation, anti-tumor, and lowering blood lipids. However, the underlying mechanism of its regulating effect on lipid metabolism in diabetic conditions remains unclear. The present study investigated the effects of I. lactea-derived proanthocyanidins on lipid metabolism in mice of type 2 diabetes mellitus (T2DM). Results demonstrated a beneficial effect of total proanthocyanidins on dysregulated lipid metabolism and hepatic steatosis in high-fat-diet/streptozocin (STZ)-induced T2DM. To identify the mechanisms, six flavan-3-ols were isolated from proanthocyanidins of I. lacteal and their effects on adipogenesis and dexamethasone (Dex)-induced mitochondrial dysfunctions in 3T3-L1 adipocytes were determined. In vitro studies showed flavan-3-ols inhibited adipogenesis and restored mitochondrial function after Dex-induced insulin resistance, being suggested by increased mitochondrial membrane potential, intracellular ATP contents, mitochondrial mass and mitochondrial biogenesis, and reduced reactive oxygen species. Among the six flavan-3-ols, procyanidin B3 and procyanidin B1 exhibited the strongest effects. Our study suggests potential of proanthocyanidins as therapeutic target for diabetes.


Assuntos
Adipogenia/efeitos dos fármacos , Diabetes Mellitus Tipo 2/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Proantocianidinas/farmacologia , Células 3T3-L1 , Animais , Biflavonoides , Peso Corporal/efeitos dos fármacos , Catequina , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Fígado Gorduroso , Flavonoides/antagonistas & inibidores , Flavonoides/química , Resistência à Insulina , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos ICR , Proantocianidinas/química , Espécies Reativas de Oxigênio , Estreptozocina/efeitos adversos
20.
Anal Chim Acta ; 1097: 110-119, 2020 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-31910950

RESUMO

Enlightened by the high specificity and reactivity of thiol radical toward allyl, here, we first established a rapid thiol radical-based chemical isotope-labelling (CIL) strategy coupled with high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) analysis for the quantitative profiling of sterols. In this strategy, N-(4-(carbazole-9-yl)-phenyl)-N-maleimide labelled derivative of ethylenedithiol (NCPM-d0-SH) and its deuterated analogue NCPM-d2-SH were employed as a novel pair of CIL reagents to efficiently label sterols. Under lighting condition, the thiol radical obtained from NCPM-d0/d2-SH attacks one allyl hydrogen in the B-ring of sterols to produce a reactive radical intermediate which can quickly react with another thiol radical to form the last labelled derivatives. This labelling reaction can rapidly complete only within 1.5 min. Absorbingly, the NCPM-d0-SH and NCPM-d2-SH labelled derivatives of sterols can produce two specific product ions (PIs) containing different isotope tags at m/z of 431.6 and 433.6 via collision induced dissociation, which were employed to develop the multiple reaction monitoring (MRM) mode-based analysis. According to the specific mass differences with a fixed value, the peak pairs with similar retention times can be easily extracted from the two PIs spectrums and designated as the candidates for the identification of sterols. NCPM-d0-SH and NCPM-d2-SH labelled derivatives of sterols can be readily distinguished from their several ion chromatograms. Thus, sterols from two samples labelled by different isotope tags were ionized at the same conditions and measured respectively, providing excellent identification and precise quantitation by compensating the matrix effect and instrument fluctuation during MS-based analysis. The detection sensitivities of thiol-containing drugs improved by 53.5-560.3-fold due to NCPM-labelling. The limits of detection (LODs) and the limits of quantitation (LOQs) were in the range of 0.15-0.40 µg kg-1 and 0.50-1.30 µg kg-1, respectively. Using the developed method, we quantitatively profiled five sterols in vegetable oils with good applicability. As promising, the proposed thiol radical-based CIL strategy is a potential platform for the quantitation of sterols.


Assuntos
Marcação por Isótopo , Esteróis/análise , Compostos de Sulfidrila/química , Espectrometria de Massas em Tandem , Cromatografia Líquida de Alta Pressão , Radicais Livres/química , Estrutura Molecular , Esteróis/química
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