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The current study aimed to determine whether Strongylocentrotus intermedius (S. intermedius) extract (SIE) exerts anti-obesity potentials employing 3T3-L1 cells as in vitro model. Herein we reported that treatment of SIE for 6 days reduced lipid accretion and TG (triglyceride) content whereas it increased the release of free glycerol. The inhibited lipid accumulation and induced lipolysis were evidenced by the downregulation of lipogenesis proteins, such as fatty acid synthase and lipoprotein lipase, and the upregulation of hormone-sensitive lipase expression. Furthermore, the downregulation of adipogenic transcription factors, including peroxisome proliferator-activated receptor gamma, CCAAT/enhancer-binding protein α, and sterol regulatory element-binding protein 1, highlights that reduced lipid accumulation is supported by lowering adipocyte differentiation. Additionally, treatment activates brown adipocyte phenotype in 3T3-L1 cells by inducing expression of brown adipose tissue-specific proteins, such as uncoupling protein 1 (UCP-1) and peroxisome proliferator-activated receptor-γ coactivator 1α (PGC-1α). Moreover, SIE induced the phosphorylation of AMP-activated protein kinase (AMPK). The pharmacological approach using AMPK inhibitor revealed that the restraining effect of SIE on adipogenesis and promotion of adipocyte browning were blocked. In GC-MS analysis, SIE was mainly composed of cholest-5-en-3-ol (36.71%) along with saturated and unsaturated fatty acids which have favorable anti-obesity potentials. These results reveal that SIE has the possibility as a lipid-lowering agent for the intervention of obesity.
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A biocompatible, heterogeneous, fucose-rich, sulfated polysaccharide (fucoidan) is biosynthesized in brown seaweed. In this study, fucoidan was isolated from Padina arborescens (PAC) using celluclast-assisted extraction, purified, and evaluated for its anti-inflammatory potential in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Structural analyses were performed using Fourier transform infrared (FTIR) and scanning electron microscopy. Among the purified fucoidans, fucoidan fraction 5 (F5) exhibited strong inhibitory activity against LPS-induced nitric oxide (NO) production and pro-inflammatory cytokine generation through the regulation of iNOS/COX-2, MAPK, and NF-κB signaling in LPS-induced RAW 264.7 cells. Determination of the structural characteristics indicated that purified F5 exhibited characteristics similar to those of commercial fucoidan. In addition, further analyses suggested that F5 inhibits LPS-induced toxicity, cell death, and NO generation in zebrafish models. Taken together, these findings imply that P. arborescens fucoidans have exceptional anti-inflammatory action, both in vitro and in vivo, and that they may have prospective uses in the functional food sector.
Assuntos
Lipopolissacarídeos , Phaeophyceae , Animais , Peixe-Zebra , Polissacarídeos , Inflamação , Óxido NítricoRESUMO
The present study aims to explore the probable anti-adipogenesis effect of Dictyopteris divaricata (D. divaricata) in 3T3-L1 preadipocytes by regulating heme oxygenase-1 (HO-1). The extract of D. divaricata retarded lipid accretion and decreased triglyceride (TG) content in 3T3-L1 adipocytes but increased free glycerol levels. Treatment with the extract inhibited lipogenesis by inhibiting protein expressions of fatty acid synthase (FAS) and lipoprotein lipase (LPL), whereas lipolysis increased by activating phosphorylation of hormone-sensitive lipase (p-HSL) and AMP-activated protein kinase (p-AMPK). The extract inhibited adipocyte differentiation of 3T3-L1 preadipocytes through down-regulating adipogenic transcription factors, including peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα), and sterol regulatory element-binding protein 1 (SREBP1). This is attributed to the triggering of Wnt/ß-catenin signaling. In addition, this study found that treatment with the extract activated HO-1 expression. Pharmacological approaches revealed that treatment with Zinc Protoporphyrin (ZnPP), an HO-1 inhibitor, resulted in an increase in lipid accumulation and a decrease in free glycerol levels. Finally, three adipogenic transcription factors, such as PPARγ, C/EBPα, and SREBP1, restored their expression in the presence of ZnPP. Analysis of chemical constituents revealed that the extract of D. divaricata is rich in 1,4-benzenediol, 7-tetradecenal, fucosterol, and n-hexadecanoic acid, which are known to have multiple pharmacological properties.
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Adipogenia , Phaeophyceae , Animais , Camundongos , Lipólise , Células 3T3-L1 , Heme Oxigenase-1/metabolismo , PPAR gama/metabolismo , Glicerol/farmacologia , Glicerol/metabolismo , Diferenciação Celular , Adipócitos , Proteína alfa Estimuladora de Ligação a CCAAT , Fatores de Transcrição/metabolismo , Lipídeos/farmacologiaRESUMO
The design and development of wound dressing with antioxidant and antibacterial properties to accelerate wound healing remain challenging. In this study, we synthesize a chitooligosaccharide-gentisic acid (COS-GSA) conjugate using the free-radical grafting method, and fabricate a poly(vinyl alcohol) (PVA)/chitosan (CH)/COS-GSA (PVA/CH/CG) hydrogel using a freeze-thaw method. We characterize the synthesized COS-GSA conjugates using through polyphenol assay, absorbance, and 1H NMR spectroscopy and evaluate their antioxidant properties. The COS-GSA conjugates are successfully synthesized and exhibit better antioxidant properties than pristine COSs. Subsequently, the fabricated hydrogel is characterized based on its morphological analysis, rheological properties, water contact angle, swelling, degradation, water retention properties, and COS-GSA release profiles. Finally, the biocompatibility of the fabricated hydrogel is evaluated on HDF and HaCaT cells through indirect and direct cytotoxicity. The PVA/CH/CG hydrogel exhibited significantly higher antioxidant properties (DPPH, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and hydrogen peroxide (H2O2) scavenging activities) and antibacterial activities (Staphylococcus aureus and Pseudomonas aeruginosa) compared to other fabricated hydrogels such as PVA, PVA/CH, and PVA/CH/COS (PVA/CH/C). These results provide evidence that PVA/CH/CG hydrogels with antioxidant, antibacterial, and non-cytotoxic properties have great potential for wound-dressing applications.
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Quitosana , Quitosana/química , Antioxidantes/farmacologia , Álcool de Polivinil/química , Hidrogéis/química , Peróxido de Hidrogênio , Antibacterianos/farmacologia , Antibacterianos/química , Bandagens , Água , EtanolRESUMO
Angiotensin I-converting enzyme (ACE) is an important blood pressure regulator. In this study, we aimed to investigate the ACE-inhibitory effects of meroterpenoids isolated from the brown alga, Sargassum macrocarpum, and the molecular mechanisms underlying ACE inhibition. Four fractions of S. macrocarpum were prepared using hexane, chloroform, ethyl acetate, and water as solvents and analyzed for their potential ACE-inhibitory effects. The chloroform fraction showed the strongest ACE-inhibitory effect, with an IC50 value of 0.18 mg/mL. Three meroterpenoids, sargachromenol, 7-methyl sargachromenol, and sargaquinoic acid, were isolated from the chloroform fraction. Meroterpenoids isolated from S. macrocarpum had IC50 values of 0.44, 0.37, and 0.14 mM. The molecular docking study revealed that the ACE-inhibitory effect of the isolated meroterpenoids was mainly attributed to Zn-ion, hydrogen bonds, pi-anion, and pi-alkyl interactions between the meroterpenoids and ACE. These results suggest that S. macrocarpum could be a potential raw material for manufacturing antihypertensive nutraceutical ingredients.
Assuntos
Inibidores da Enzima Conversora de Angiotensina , Sargassum , Inibidores da Enzima Conversora de Angiotensina/química , Simulação de Acoplamento Molecular , Sargassum/química , Peptidil Dipeptidase A/química , ClorofórmioRESUMO
In this study, seahorse peptide (SHP) was isolated from an alcalase-treated hydrolysate from Hippocampus abdominalis and assessed for its antioxidant potential against AAPH-induced oxidative stress damage. AAPH stimulation significantly decreased cell viability and increased intracellular reactive oxygen species (ROS) production in Vero cells. SHP treatment increased cell viability and remarkably lowered ROS production under AAPH-induced oxidative stress. Furthermore, it protected against AAPH-induced apoptotic DNA damage. Western blot analysis demonstrated that SHP treatment remarkably increased the protein expression levels of catalase and SOD in AAPH-induced Vero cells. A zebrafish study revealed that SHP-treated zebrafish embryos resulted in lower cell death, ROS generation, and lipid peroxidation than the AAPH-treated group. These results suggest that SHP is a potent functional antioxidant that could be developed as a natural antioxidant in the food and functional food industries.
Assuntos
Antioxidantes , Smegmamorpha , Animais , Chlorocebus aethiops , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Peixe-Zebra/genética , Peixe-Zebra/metabolismo , Células Vero , Smegmamorpha/genética , Smegmamorpha/metabolismo , Estresse Oxidativo , Peptídeos/farmacologia , Peptídeos/metabolismoRESUMO
Sargassum horneri is a seaweed species with diverse bioactivities. However, its antifibrotic effects during nasal polyp (NP) formation are not clearly understood. Therefore, we investigated the inhibitory effect of S. horneri on fibrosis progression in NP-derived fibroblasts (NPDFs) and NP tissues ex vivo. NPDFs were stimulated with TGF-ß1 in the presence or absence of S. horneri ethanol extract (SHE). The extracellular matrix (ECM) protein production levels, myofibroblast differentiation (α-smooth muscle actin, α-SMA), and phosphorylation of Smad 2/3 and -ERK in TGF-ß1-stimulated NPDFs were investigated using western blotting. Further, the contractile activity of SHE was assessed by performing a collagen gel contraction assay. The expression levels of collagen-1, fibronectin, and α-SMA were investigated in NP organ cultures treated with SHE. TGF-ß1 stimulated ECM protein expression, myofibroblast differentiation, and collagen contractile activity while these were attenuated by pretreatment with SHE. We also found antifibrotic effect of SHE on ex vivo NP tissues. The antifibrotic effects of SHE were modulated through the attenuation of Smad 2/3 and ERK signaling pathways in TGF-ß1-stimulated NPDFs. In conclusion, SHE inhibited ECM protein accumulation and myofibroblast differentiation during NP remodeling. Thus, SHE may be helpful as a treatment for NP recurrence after endoscopic sinus surgery.
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Ecklonia maxima is a brown seaweed, which is abundantly distributed in South Africa. This study investigated an efficient approach using high-performance centrifugal partition chromatography (HPCPC), which has been successfully developed for the isolation and purification of phlorotannins, eckmaxol, and dieckol from the ethyl acetate fraction of E. maxima (EEM). We evaluated EEM for its inhibitory effect against lipopolysaccharide (LPS)-induced inflammatory responses in zebrafish embryos. The separation of eckmaxol and dieckol from samples of EEM using HPCPC was found to be of high purity and yield under an optimal solvent system composed of n-hexane:ethyl acetate:methanol:water (2:7:3:7, v/v/v/v). To evaluate the anti-inflammatory efficacy of EEM containing active compounds, zebrafish embryos exposed to LPS were compared with and without EEM treatment for nitric oxide (NO) production, reactive oxygen species (ROS) generation, and cell death two days after fertilization. These evaluations indicate that EEM alleviated inflammation by inhibiting cell death, ROS, and NO generation induced by LPS treatment. According to these results, eckmaxol and dieckol isolated from brown seaweed E. maxima could be considered effective anti-inflammatory agents as pharmaceutical and functional food ingredients.
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Phaeophyceae , Alga Marinha , Animais , Anti-Inflamatórios/farmacologia , Cromatografia Líquida , Lipopolissacarídeos/farmacologia , Óxido Nítrico/metabolismo , Phaeophyceae/química , Espécies Reativas de Oxigênio/metabolismo , Alga Marinha/metabolismo , África do Sul , Peixe-Zebra/metabolismoRESUMO
The aim of this study was to assess the potential hypertensive effects of the IGTGIPGIW peptide purified from Hippocampus abdominalis alcalase hydrolysate (HA) for application in the functional food industry. We investigated the antihypertensive effects of IGTGIPGIW in vitro by assessing nitric oxide production in EA.hy926 endothelial cells, which is a major factor affecting vasorelaxation. The potential vasorelaxation effect was evaluated using 4-amino-5-methylamino-2',7'-difluorofluorescein diacetate, a fluorescent stain. IGTGIPGIW significantly increased the expression of endothelial-derived relaxing factors, including endothelial nitric oxide synthase and protein kinase B, in EA.hy926 cells. Furthermore, oral administration of IGTGIPGIW significantly lowered the systolic blood pressure (183.60 ± 1.34 mmHg) and rapidly recovered the diastolic blood pressure (143.50 ± 5.55 mmHg) in the spontaneously hypertensive rat model in vivo. Our results demonstrate the antihypertensive activity of the IGTGIPGIW peptide purified from H. abdominalis and indicate its suitability for application in the functional food industry.
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Anti-Hipertensivos , Óxido Nítrico Sintase Tipo III , Smegmamorpha , Animais , Anti-Hipertensivos/farmacologia , Pressão Sanguínea , Células Endoteliais , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo III/metabolismo , Peptídeos/farmacologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ratos , Ratos Endogâmicos SHRRESUMO
Protocatechuic aldehyde (PA) is a naturally occurring phenolic compound that is a potent inhibitor of mushroom tyrosinase. However, the molecular mechanisms of the anti-melanogenesis activity of PA have not yet been reported. The aim of the current study was to clarify the melanogenesis inhibitory effects of PA and its molecular mechanisms in murine melanoma cells (B16F10). We first predicted the 3D structure of tyrosinase and used a molecular docking algorithm to simulate binding between tyrosinase and PA. These molecular modeling studies calculated a binding energy of -527.42 kcal/mol and indicated that PA interacts with Cu400 and 401, Val283, and His263. Furthermore, PA significantly decreased α-MSH-induced intracellular tyrosinase activity and melanin content in a dose-dependent manner. PA also inhibited key melanogenic proteins such as tyrosinase, tyrosinase-related protein 1 (TRP-1), and TRP-2 in α-MSH-stimulated B16F10 cells. In addition, PA decreased MITF expression levels by inhibiting phosphorylation of cAMP response element-binding protein (CREB) and cAMP-dependent protein kinase A (PKA). These results demonstrate that PA can effectively suppress melanin synthesis in melanoma cells. Taken together, our results show that PA could serve as a potential inhibitor of melanogenesis, and hence could be explored as a possible skin-lightening agent.
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Benzaldeídos/farmacologia , Catecóis/farmacologia , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Proteínas Quinases Dependentes de AMP Cíclico/metabolismo , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Melaninas/biossíntese , Fator de Transcrição Associado à Microftalmia/genética , alfa-MSH/metabolismo , Animais , Benzaldeídos/química , Catecóis/química , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/genética , Proteínas Quinases Dependentes de AMP Cíclico/genética , Melanoma Experimental , Camundongos , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/metabolismoRESUMO
Three-dimensional (3 D) printing is an effective technology that has shown considerable potential for use in tissue regeneration. Of the many materials that have been proposed for this purpose, poly (ε-caprolactone) (PCL) 3 D scaffolds have been received significant attention in the bone tissue engineering field due to its advantageous mechanical properties and biocompatibility. In this study, a novel method was developed for tissue-engineered bone that combines PCL 3 D scaffolds with fish collagen (Col) and the osteogenic abalone intestine gastro-intestinal digests (AIGIDs) from Haliotis discus hannai. And then, mouse mesenchymal stem cells (MSCs) were seeded onto the fabricated scaffolds. After in vitro culturing, the proliferation of the MSCs on the scaffolds, alkaline phosphatase (ALP) activity, and the amount of deposited calcium were investigated. The results indicated that the ALP activity and mineralization in PCL/AIGIDs/Col was higher than that of the other scaffolds. In an in vivo experiment, the two fabricated scaffolds were implanted in a rabbit tibia. PCL/AIGIDs/Col group exhibited strong osteoinduction capability in the rabbit tibia defect model. These stimulated biological responses in vitro and in vivo suggest that the PCL/AIGIDs/Col scaffold are promising material for use in tissue implants and bone regeneration.
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Hidrolisados de Proteína , Alicerces Teciduais , Animais , Regeneração Óssea , Diferenciação Celular , Proliferação de Células , Colágeno , Camundongos , Osteogênese , Poliésteres , Coelhos , Engenharia TecidualRESUMO
This study investigated the antihypertensive effects of an antioxidant peptide, Leu-Trp-His-Thr-His (LWHTH), purified from Styela clava peptic hydrolysate, to assess the bioactivity of the peptide and verify the value of S. clava as a health-promoting food. Also, the study presented structural evidence for the effects of LWHTH. The inhibitory effect of LWHTH on angiotensin I-converting enzyme (ACE) was assessed using enzyme reaction methods and the simulation methods in computational space. LWHTH inhibited ACE with an IC50 value of 16.42 ± 0.45 µM. The LWHTH structure was stable, and its ACE inhibitory effect was retained under simulated gastrointestinal conditions. In silico simulations revealed that LWHTH binds the active site of ACE, with residues LW making the ACE-LWHTH complex stable and residues HTH making the complex strong. Furthermore, LWHTH significantly reduced blood pressure in spontaneously hypertensive rats. These results demonstrate that LWHTH has the potential to be a healthy functional food with antihypertensive effects. Therefore, S. clava consumption may be beneficial for human health.
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Inibidores da Enzima Conversora de Angiotensina/farmacologia , Anti-Hipertensivos/farmacologia , Antioxidantes/farmacologia , Hipertensão/tratamento farmacológico , Peptídeos/farmacologia , Urocordados/química , Animais , Pressão Sanguínea , Estabilidade Enzimática , Masculino , Simulação de Acoplamento Molecular , Estrutura Terciária de Proteína , Ratos , Ratos Endogâmicos SHRRESUMO
In this study, we fabricated polyvinyl alcohol hydrogels containing diphlorethohydroxycarmalol (DPHC) from Ishige okamurae for its anti-bacterial effect in wound-dressing applications. First, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of DPHC against Staphylococcus aureus and Pseudomonas aeruginosa were investigated, and these were found to be about 128⯵g/mL and 512⯵g/mL, respectively. Polyvinyl alcohol hydrogels loaded with different concentrations of DPHC were then produced for the dressing of wounds to assist in the healing process and to provide an antibacterial effect. To investigate the characteristics of the proposed PVA/DPHC hydrogels, we conducted SEM analysis, rheological analysis, thermogravimetric analysis, water swelling analysis, drug release testing, and gel fraction assessment. The antibacterial activity of the PVA/DPHC hydrogels was also tested against the gram-positive bacterium S. aureus and the gram-negative bacterium P. aeruginosa using ASTM E2149 tests. The biocompatibility of the PVA/DPHC hydrogels was assessed using in vitro indirect and direct contact tests and in vivo tests on ICR mice. The PVA/DPHC hydrogels exhibited the ability to reduce the viability of S. aureus and P. aeruginosa by about 99% in ASTM E2149 testing, while not producing any toxic effect on NHDF-Neo or HaCaT cells as shown in MTT assays and in vitro FDA fluorescence analysis. In addition, the PVA/DPHC hydrogels had a strong wound healing effect when compared to non-treated groups of ICR mice in vivo. Based on the characterization of the PVA/DPHC hydrogels in vitro and in vivo, this study suggests that the proposed hydrogel has significant potential for use in wound dressing.
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Antibacterianos/farmacologia , Bandagens , Compostos Heterocíclicos com 3 Anéis/isolamento & purificação , Compostos Heterocíclicos com 3 Anéis/farmacologia , Hidrogéis/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Antibacterianos/química , Células Cultivadas , Liberação Controlada de Fármacos , Humanos , Hidrogéis/química , Masculino , Camundongos Endogâmicos ICR , Testes de Sensibilidade Microbiana , Phaeophyceae/química , Álcool de Polivinil/química , Pseudomonas aeruginosa/efeitos dos fármacos , Reologia , Staphylococcus aureus/efeitos dos fármacos , TermogravimetriaRESUMO
Prolonged endotracheal intubation is the most common cause of tracheal stenosis, which may lead to serious airway obstruction. Development of an endotracheal tube coated with biomaterials that exhibit anti-inflammatory or anti-fibrogenic effects may prevent tracheal stenosis. This study demonstrates that an endotracheal tube coated with phlorotannin, which is present in extracts of the brown alga Ecklonia cava, can prevent tracheal stenosis in a rabbit model. An in vitro study shows that phlorotannin inhibits proliferation of human tracheal fibroblasts treated with transforming growth factor ß1. Phlorotannin-coated endotracheal tubes show steady release of phlorotannin for up to 7 days, and removal of the tube 1 week after insertion reveals a reduction in both fibrogenesis and thickening of tracheal submucosa. Western blot analysis of tracheal tissues after removal of the phlorotannin-coated tube shows decreased protein expression levels of phenotypic markers of fibrosis such as collagen type I and α-smooth muscle actin. The ability of phlorotannin-coated endotracheal tube to prevent tracheal stenosis caused by endotracheal intubation indicates that phlorotannin may be considered as a candidate biomaterial for coating the cuff of endotracheal tubes to prevent tracheal stenosis.
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Intubação Intratraqueal/efeitos adversos , Poliésteres/química , Estenose Traqueal/prevenção & controle , Animais , Materiais Biocompatíveis/química , Linhagem Celular , Fibrose , Humanos , Técnicas In Vitro , Masculino , Teste de Materiais , Mucosa/metabolismo , Coelhos , Sais de Tetrazólio/química , Tiazóis/química , Traqueia/cirurgia , Fator de Crescimento Transformador beta1/metabolismoRESUMO
Velvet antler has a long history in traditional medicine. It is also an important healthy ingredient in food as it is rich in protein. However, there has been no report about antioxidant peptides extracted from velvet antler by enzymatic hydrolysis. Thus, the objective of this study was to hydrolyze velvet antler using different commercial proteases (Acalase, Neutrase, trypsin, pepsin, and α-chymotrypsin). Antioxidant activities of different hydrolysates were investigated using peroxyl radical scavenging assay by electron spin resonance spectrometry. Among all enzymatic hydrolysates, Alcalase hydrolysate exhibited the highest peroxyl radical scavenging activity. Alcalase hydrolysate was then purified using ultrafiltration, gel filtration, and reverse-phase high performance liquid chromatography. The purified peptide was identified to be Trp-Asp-Val-Lys (tetrapeptide) with molecular weight of 547.29 Da by Q-TOF ESI mass spectroscopy. This purified peptide exhibited strong scavenging activity against peroxyl radical (IC50 value, 0.028 mg/mL). In addition, this tetrapeptide showed significant protection ability against AAPH-induced oxidative stress by inhibiting of reactive oxygen species (ROS) generation in Chang liver cells in vitro and in a zebrafish model in vivo. This research suggests that the tetrapeptide derived from Alcalase-proteolytic hydrolysate of velvet antler are excellent antioxidants and could be effectively applied as functional food ingredients and pharmaceuticals.
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Antioxidantes/farmacologia , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Fragmentos de Peptídeos/farmacologia , Subtilisinas/química , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Chifres de Veado/química , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Humanos , Hidrólise , Fragmentos de Peptídeos/química , Fragmentos de Peptídeos/isolamento & purificação , Espécies Reativas de Oxigênio/metabolismo , Peixe-ZebraRESUMO
Sargassum thunbergii is a brown alga from which various bioactive compounds can be extracted. Among these, the activities of indole derivatives, particularly as potential inhibitors of matrix metalloproteinases (MMPs), and their underlying mechanisms have been rarely investigated. Therefore, we evaluated the inhibitory effects of indole6carboxaldehyde (I6CA) on MMP9 by gelatin zymography and western blot anlaysis. We used phorbol 12myristate 13acetate (PMA), which is known to induce MMP9 expression and secretion, to stimulate HT1080 cells. Our results revealed that I6CA significantly inhibited MMP9 expression and secretion, without significantly affecting the viability of PMAstimulated HT1080 cells. Our mechanistic studies indicated that I6CA suppressed the phosphorylation and activation of two mitogenactivated protein kinases (MAPKs), cJun Nterminal kinase (JNK) and extracellular signalregulated kinase 1/2 (ERK). Furthermore, I6CA inhibited the phosphorylation of inhibitor of κBα (IκBα) in response to PMA stimulation, which suppressed nuclear factorκB (NFκB) p65 subunit nuclear translocation. Collectively, I6CA was determined to suppress MMP9 expression and secretion, and effects were proposed to be mediated via the inhibition of the MAPK and NFκB p65 pathways. Therefore, we suggested I6CA to be a potential therapeutic agent for MMP9related processes, including tumor invasion and metastasis; however, further investigation is required.
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Indóis/farmacologia , Metaloproteinase 9 da Matriz/metabolismo , Sargassum/química , Linhagem Celular Tumoral , Humanos , Proteína Quinase 3 Ativada por Mitógeno/metabolismo , Inibidor de NF-kappaB alfa/metabolismo , NF-kappa B/metabolismo , Fosforilação/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismoRESUMO
Seahorses, Hippocampus abdominalis, have a long history in traditional Chinese medicine as an important healthy ingredient in foods. This study evaluated the antioxidant activity of an enzymatic hydrolysate prepared from a seahorse bred in Jeju, South Korea. Experiments were performed in vitro using electron spin resonance spectrometry (ESR) to determine the free radical scavenging activity and in vivo using a zebrafish model to determine the protective effects against 2,2-azobis hydrochloride (AAPH)-induced oxidative damage. H. abdominalis protein hydrolysate (HPH) exhibited peroxyl radical scavenging activity (IC50 = 0.58 mg/ml) generated by the water-soluble AAPH (azo initiator of peroxyl radicals). HPH reduced dose-dependently both intracellular reactive oxygen species (ROS) levels in AAPH-induced cells and cell death in AAPH-induced zebrafish embryos. The antioxidant peptide purified from HPH was identified as a tripeptide (alanine-glycine-aspartic acid) using Q-TOF ESI mass spectroscopy. Thus, this study demonstrated that HPH contains antioxidant peptides that exhibit a strong antioxidant activity. PRACTICAL APPLICATIONS: Hippocampus abdominalis is one of the largest seahorse species and cultivated in many countries. Because of its large body size compared to other seahorse species, H. abdominalis has acquired considerable consumer attraction in the global market. Owing to its biologically useful properties, it recently gained attention as the natural products obtained from H. abdominalis have varied applications in the field of medicine, health care products, and functional foods. Thus, commercial products of this particular seahorse species are popular among customers, especially in China. The purpose of this study was to evaluate the antioxidant property of H. abdominalism, cultured in a commercial seahorse farm in Jeju Island. Owing to its prominent antioxidant activity, it could be used as an ingredient in medicinal preparations, nutraceuticals, and functional foods.
Assuntos
Sequestradores de Radicais Livres/química , Hidrolisados de Proteína/farmacologia , Smegmamorpha/metabolismo , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Aquicultura , Chlorocebus aethiops , Suplementos Nutricionais , Espectroscopia de Ressonância de Spin Eletrônica , Sequestradores de Radicais Livres/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Peptídeos/química , Peptídeos/farmacologia , Hidrolisados de Proteína/química , Espécies Reativas de Oxigênio/metabolismo , Espectrometria de Massas por Ionização por Electrospray , Subtilisinas/química , Subtilisinas/farmacologia , Células Vero , Peixe-ZebraRESUMO
Fish bone extract (FBE) containing a trioligopeptide (FBP-KSA, Lys-Ser-Ala) isolated from Johnius belengerii could induce osteogenic activities on MC3T3-E1 pre-osteoblasts in our previous study. Regarding the osteogenic effect of FBE, in the present study, we fabricated the three-dimensional (3D) interconnected polycaprolactone (PCL)/FBE scaffolds for bone tissue regeneration. After fabrication of PCL scaffolds using 3D printing, FBE was coated on the surface of PCL scaffolds by self-assembly process. In the physical characteristic and mechanical property tests, the results demonstrated that the fabricated scaffolds have the strut diameter (between 340 and 345 µm), pore size (between 470 and 480 µm), porosity (between 50% and 55%), and tensile properties (Young's modulus: 9.18-9.42 MPa; max tensile strengths 82.3-87.4 MPa) were similar to those of PCL scaffold. In the cell proliferation and osteogenic assay, the results showed that PCL/FBE scaffolds could significantly induce cell proliferation, calcium deposition, and the expression of osteogenic phenotype markers such as alkaline phosphatase, osteopontin, osteocalcin, and bone morphogenetic protein-2 in the osteoblasts. These results suggest that FBE-coated PCL scaffolds are promising materials for use in biomedical application to promote bone tissue regeneration. © 2018 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater 107B: 1937-1944, 2019.
Assuntos
Regeneração Óssea , Misturas Complexas/química , Peixes , Teste de Materiais , Osteogênese , Poliésteres/química , Impressão Tridimensional , Alicerces Teciduais/química , Animais , Osso e Ossos/química , Linhagem Celular , CamundongosRESUMO
The aim of the present study was to investigate the effect of 5-bromo-3,4-dihydroxybenzaldehyde (BD) isolated from Polysiphonia morrowii on adipogenesis and differentiation of 3T3-L1 preadipocytes into mature adipocytes and its possible mechanism of action. Levels of lipid accumulation and triglyceride were significantly lower in BD treated cells than those in untreated cells. In addition, BD treatment reduced protein expression levels of peroxisome proliferator-activated receptor-γ, CCAAT/enhancer-binding proteins α, and sterol regulatory element-binding protein 1 compared with control (no treatment). It also reduced expression levels of adiponectin, leptin, fatty acid synthase, and fatty acid binding protein 4. AMP-activated protein kinase activation was found to be one specific mechanism involved in the effect of BD. These results demonstrate that BD possesses inhibitory effect on adipogenesis through activating AMP-activated protein kinase signal pathway.
Assuntos
Proteínas Quinases Ativadas por AMP/fisiologia , Adipogenia/efeitos dos fármacos , Benzaldeídos/farmacologia , Rodófitas/química , Células 3T3-L1 , Animais , Benzaldeídos/isolamento & purificação , Diferenciação Celular/efeitos dos fármacos , Ativação Enzimática/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Camundongos , Transdução de Sinais/efeitos dos fármacosRESUMO
Propionibacterium acnes plays a key role in the onset of inflammation leading to acne and in downregulation of the defense system against oxidative stress. Therefore, antibiotics such as macrolides, tetracyclines, azelaic acid, and erythromycin are used to reduce microbial proliferation and resulting inflammation. Nonetheless, antibiotic treatment has side effects including cytotoxicity, allergy, and diarrhea. Therefore, recent studies were focused on the development of alternative antimicrobial materials. We conjugated chitooligosaccharide (COS) with gallic acid (GA) by the hydrogen peroxide-mediated method and evaluated antioxidant and antimicrobial activities. Then, we fabricated a polyvinyl alcohol (PVA) hydrogel containing COS conjugated with GA (GA-COS) for acne treatment. GA-COS at 5-10â¯kDa showed an excellent antioxidant activity and a better antimicrobial activity against P. acnes as compared with COS. In addition, the PVA hydrogel with GA-COS inhibited intracellular formation of reactive oxygen species and exerted antimicrobial action better than controls did.