RESUMO
Perilla frutescens leaves are hypothesized to possess antioxidant and amyloid-ß (Aß) aggregation inhibitory properties primarily due to their polyphenol-type compounds. While these bioactivities fluctuate daily, the traditional methods for quantifying constituent contents and functional properties are both laborious and impractical for immediate field assessments. To address this limitation, the present study introduces an expedient approach for on-site analysis, employing fluorescence spectra obtained through excitation light irradiation of perilla leaves. Standard analytical techniques were employed to evaluate various constituent contents (chlorophyl (Chl), total polyphenol content (TPC), total flavonoid content (TFC), and rosmarinic acid (RA)) and functional attributes (DPPH radical scavenging activity, ferric reducing antioxidant power (FRAP), oxygen radical absorbance capacity (ORAC), and Aß aggregation inhibitory activity). Correlations between the fluorescence spectra and these parameters were examined using normalized difference spectral index (NDSI), ratio spectral index (RSI), and difference spectral index (DSI) analyses. The resulting predictive model exhibited a high coefficient of determination, with R2 values equal to or greater than 0.57 for constituent contents and 0.49 for functional properties. This approach facilitates the convenient, simultaneous, and nondestructive monitoring of both the chemical constituents and the functional capabilities of perilla leaves, thereby simplifying the determination of optimal harvest times. The model derived from this method holds promise for real-time assessments, indicating its potential for the simultaneous evaluation of both constituents and functionalities in perilla leaves.
Assuntos
Perilla frutescens , Perilla , Perilla frutescens/química , Antioxidantes/química , Perilla/química , Polifenóis/análise , Extratos Vegetais/química , Peptídeos beta-Amiloides/análise , Folhas de Planta/químicaRESUMO
Perilla frutescens is an annual herb of the Labiatae family and is widely grown in several countries in Asia. Perilla frutescens is a plant that is used medicinally in its entirety, as seen in its subdivision into perilla seeds, perilla stalks, and perilla leaves, which vary more markedly in their chemical composition. Several studies have shown that Perilla frutescens has a variety of pharmacological effects, including anti-inflammatory, antibacterial, detoxifying, antioxidant, and hepatoprotective. In the absence of a review of Perilla frutescens for the treatment of cancer. This review provides an overview of the chemical composition and molecular mechanisms of Perilla frutescens for cancer treatment. It was found that the main active components of Perilla frutescens producing cancer therapeutic effects were perilla aldehyde (PAH), rosmarinic acid (Ros A), lignan, and isoestrogen (IK). In addition to these, extracts of the leaves and fruits of Perilla frutescens are also included. Among these, perilla seed oil (PSO) has a preventive effect against colorectal cancer due to the presence of omega-3 polyunsaturated fatty acids. This review also provides new ideas and thoughts for scientific innovation and clinical applications related to Perilla frutescens.
Assuntos
Ácidos Graxos Ômega-3 , Neoplasias , Perilla frutescens , Perilla , Perilla frutescens/química , Perilla/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antioxidantes , Folhas de Planta , Neoplasias/tratamento farmacológicoRESUMO
Perilla frutescens (Lamiaceae) is an important herbal plant with hundreds of bioactive chemicals, among which perillaldehyde and rosmarinic acid are the two major bioactive compounds in the plant. The leaves of red perilla are used as traditional Kampo medicine or food ingredients. However, the medicinal and nutritional uses of this plant could be improved by enhancing the production of valuable metabolites through the manipulation of key enzymes or regulatory genes using genome editing technology. Here, we generated a high-quality genome assembly of red perilla domesticated in Japan. A near-complete chromosome-level assembly of P. frutescens was generated contigs with N50 of 41.5 Mb from PacBio HiFi reads. 99.2% of the assembly was anchored into 20 pseudochromosomes, among which seven pseudochromosomes consisted of one contig, while the rest consisted of less than six contigs. Gene annotation and prediction of the sequences successfully predicted 86,258 gene models, including 76,825 protein-coding genes. Further analysis showed that potential targets of genome editing for the engineering of anthocyanin pathways in P. frutescens are located on the late-stage pathways. Overall, our genome assembly could serve as a valuable reference for selecting target genes for genome editing of P. frutescens.
Assuntos
Lamiaceae , Perilla frutescens , Perilla , Perilla frutescens/genética , Perilla frutescens/química , Perilla frutescens/metabolismo , Perilla/genética , Perilla/química , Japão , Lamiaceae/genética , Anotação de Sequência MolecularRESUMO
This study aimed to develop perilla fruit oil (PFO)-fortified soybean milk (PFO-SM), identify its sensory acceptability, and evaluate its health outcomes. Our PFO-SM product was pasteurized, analyzed for its nutritional value, and had its acceptability assessed by an experienced and trained descriptive panel (n = 100) based on a relevant set of sensory attributes. A randomized clinical trial was conducted involving healthy subjects who were assigned to consume deionized water (DI), SM, PFO-SM, or black sesame-soybean milk (BS-SM) (n = 48 each, 180 mL/serving) daily for 30 d. Accordingly, health indices and analyzed blood biomarkers were recorded. Consequently, 1% PFO-SM (1.26 mg ALA rich) was generally associated with very high scores for overall acceptance, color, flavor, odor, taste, texture, and sweetness. We observed that PFO-SM lowered levels of serum triglycerides and erythrocyte reactive oxygen species, but increased phagocytosis and serum antioxidant activity (p < 0.05) when compared to SM and BS-SM. These findings indicate that PFO supplementation in soybean milk could enhance radical-scavenging and phagocytotic abilities in the blood of healthy persons. In this regard, it was determined to be more efficient than black sesame supplementation. We are now better positioned to recommend the consumption of PFO-SM drink for the reduction of many chronic diseases. Randomized clinical trial registration (Reference number 41389) by IRSCTN Registry.
Assuntos
Perilla , Leite de Soja , Antioxidantes , Suplementos Nutricionais/análise , Alimentos Fortificados , Frutas , Voluntários Saudáveis , Humanos , Perilla/química , Fagocitose , TriglicerídeosRESUMO
This study investigated the effects of different microwave power (380 W, 540 W, 700 W) and time (0-10 min) on the minor bioactive components content and oxidative stability of perilla oil. The results indicated that fatty acids in perilla oil were slightly affected by microwave treatment. The oxidative stability of perilla oil increased with increasing microwave treatment intensity and the oil from perilla seeds treated at 700 W for 10 min had the highest oxidative stability. Compared with other microwave treatments, treatment with 700 W for 10 min resulted in significant increases in the total phytosterols content, Maillard reaction products and DPPH radical scavenging activity of perilla oil, while showed dramatic reductions in the total tocopherol content, phenolic compounds content and lipase activity. These results proved that microwave treatment of perilla seeds was an effective way to improve the quality of perilla oil.
Assuntos
Perilla , Micro-Ondas , Oxirredução , Estresse Oxidativo , Perilla/química , Óleos de Plantas/química , Sementes/químicaRESUMO
Monoterpene Perillaldehyde (PAE) is a major component of the essential oil extracted from perilla plants (Perilla frutescens), which has been used as a leafy vegetable and a medicinal agent. PAE has gained a lot of attention in recent years because of its antifungal and other microbial activities and, human health benefits. PAE has also been used as food additives, perfume ingredients, and traditional medicine concoctions. Biological analyses of PAE have revealed that it has good antioxidant activities and can serve as organic fruit and food preservative. Animal studies indicated potent anticancer, anti-depressant, and anti-inflammatory effects of PAE. Also, PAE is certified "generally recognized as safe" (GRAS) and not mutagenic. However, moderation during usage is advisable, as minor adverse effects are associated with a very high dosage. Despite the newly reported findings, its properties have not been thoroughly summarized and reviewed. Also, clinical trials and official large-scale field applications of PAE in the agricultural sectors are yet to be reported. In this review, updated PAE research progress was provided, focusing on its antifungal and other antimicrobial properties and the mechanisms behind it, phytochemical profile, pharmacological effects, and safety concerns.HighlightsIsolation and recovery techniques of PAE from perilla plants have been developed and improved in recent years.PAE is a potential anti-oxidant and antifungal agent that can be widely used in the food industry.PAE can be developed into drug ingredients for pharmaceutical industries due to its anti-inflammatory, anti-cancer and anti-depressant activities.PAE can be safely used in human when low and moderate dosage is used.
Assuntos
Perilla , Animais , Anti-Inflamatórios/farmacologia , Antifúngicos/farmacologia , Humanos , Monoterpenos , Perilla/químicaRESUMO
Industrially, after the removal of oil from perilla seeds (PS) by screw-type compression, the large quantities of residual perilla seed meal (PSM) becomes non-valuable waste. Therefore, to increase the health value and price of PS and PSM, we focused on the biological effects of perilla seed oil (PSO) and rosmarinic acid-rich fraction (RA-RF) extracted from PSM for their role in preventing oxidative stress and inflammation caused by TNF-α exposure in an A549 lung adenocarcinoma culture model. The A549 cells were pretreated with PSO or RA-RF and followed by TNF-α treatment. We found that PSO and RA-RF were not toxic to TNF-α-induced A549 cells. Both extracts significantly decreased the generation of reactive oxygen species (ROS) in this cell line. The mRNA expression levels of IL-1ß, IL-6, IL-8, TNF-α, and COX-2 were significantly decreased by the treatment of PSO and RA-RF. The Western blot indicated that the expression of MnSOD, FOXO1, and NF-κB and phosphorylation of JNK were also significantly diminished by PSO and RA-RF treatment. The results demonstrated that PSO and RA-RF act as antioxidants to scavenge TNF-α induced ROS levels, resulting in decreased the expression of MnSOD, FOXO1, NF-κB and JNK signaling pathway in a human lung cell culture exposed to TNF-α.
Assuntos
Adenocarcinoma de Pulmão/metabolismo , Anti-Inflamatórios , Antioxidantes , Cinamatos , Depsídeos , Ácidos Graxos Ômega-3 , Neoplasias Pulmonares/metabolismo , Perilla/química , Ácido alfa-Linolênico , Células A549 , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Cinamatos/química , Cinamatos/farmacologia , Depsídeos/química , Depsídeos/farmacologia , Ácidos Graxos Ômega-3/química , Ácidos Graxos Ômega-3/farmacologia , Humanos , Estresse Oxidativo/efeitos dos fármacos , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Ácido alfa-Linolênico/química , Ácido alfa-Linolênico/farmacologia , Ácido RosmarínicoRESUMO
BACKGROUND: Light-emitting diodes (LEDs) are widely used in closed-type plant production systems to improve biomass and accumulate bioactive compounds in plants. Perilla has been commonly used as herbal medicine because of its health-promoting effects. This study aimed to investigate the physiological and biochemical responses of green and red perilla under various visible-light spectra. RESULTS: Results showed that red (R) LEDs improved fresh weights of shoots and roots, plant height, internode length, node number and leaf area, as well as photosynthetic rate of green and red perilla plants compared to blue (B) LEDs and RB combined LEDs. Meanwhile, B resulted in higher stomatal conductance, transpiration rate and Fv/Fm compared to R. Supplementation of green (G) and far-red (FR) did not enhance perilla growth. Reduction or absence of B decreased leaf thickness, adaxial and abaxial epidermis, and palisade and spongy mesophyll. Total phenolic content, antioxidant capacity, rosmarinic acid content and caffeic acid content of green perilla were higher under R, R8B2 and RGB + FR, while greater values were obtained in red perilla under R. Accumulation of perillaldehyde, luteolin and apigenin presented different trends from those of rosmarinic and caffeic acids in both cultivars. CONCLUSIONS: Growth and accumulation of bioactive compounds in green perilla were greater than in red perilla under similar light quality, and R LEDs or a higher R ratio in combination treatments were suitable for cultivating high-quality green and red perilla plants in closed-type plant factories. © 2020 Society of Chemical Industry.
Assuntos
Perilla/efeitos da radiação , Folhas de Planta/química , Apigenina/análise , Apigenina/metabolismo , Luz , Luteolina/análise , Luteolina/metabolismo , Monoterpenos/análise , Monoterpenos/metabolismo , Perilla/química , Perilla/crescimento & desenvolvimento , Perilla/metabolismo , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Folhas de Planta/crescimento & desenvolvimento , Folhas de Planta/metabolismo , Folhas de Planta/efeitos da radiaçãoRESUMO
Perilla frutescens fruit oil (PFO) is rich in α-linolenic acid (ALA) and exhibits biological activities. We aimed to investigate analgesic, anti-inflammatory and anti-ulcer activities of PFO and PFO-supplemented soybean milk (PFO-SM) in animal models. Analgesic activity was assessed in acetic acid-induced writhing in mice, while anti-inflammatory activity was performed in ethyl phenylpropiolate (EPP)-induced ear edema and carrageenan-induced hind paw edema in rats. Anti-ulcer effects were conducted in water immersion stress, HCl/ethanol and indomethacin-induced gastric ulcer in rats. Distinctly, PFO, containing 6.96 mg ALA and 2.61 mg LA equivalence/g, did not induce acute toxicity (LD50 > 10 mL/kg) in mice. PFO (2.5 and 5 mL/kg) and PFO-SM (0.05 mL PFO equivalence/kg) inhibited incidences of writhing (16.8, 18.0 and 32.3%, respectively) in acetic acid-induced mice. In addition, topical applications of PFO (0.1 and 1 mL/ear) significantly inhibited EPP-induced ear edema (59.3 and 65.7%, respectively) in rats, while PFO-SM slightly inhibited ear edema (25.9%). However, PFO and PFO-SM did not inhibit carrageenan-induced hind paw edema in rats. Indeed, PFO (2.5 and 5 mL/kg) significantly inhibited gastric ulcers in rats that induced by water immersion stress (92.4 and 96.6%, respectively), HCl/ethanol (74.8 and 73.3%, respectively) and indomethacin (68.8 and 88.9%, respectively), while PFO-SM did not. PFO displayed potent analgesic, anti-inflammatory and anti-ulcer properties, while PFO-SM exerted only analgesic properties. Thus, Thai PFO and its functional drink offer potential benefits in treatment of analgesic, inflammatory diseases and gastric ulcer.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Antiulcerosos/farmacologia , Perilla/química , Óleos de Plantas/farmacologia , Animais , Edema/induzido quimicamente , Edema/prevenção & controle , Masculino , Camundongos , Ratos , Ratos Sprague-Dawley , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/prevenção & controleRESUMO
Caffeic acid and rosmarinic acid are common components of Labiatae plants, such as shiso (Perilla frutescens Britton var. crispa W. Deane) and Boraginaceae plants. These compounds have various pharmacological activities, such as anti-inflammatory, anti-anxiety, and anti-depressive activities, but the content of these compounds in perilla has not been studied in detail. This study investigated the caffeic acid and rosmarinic acid contents of several pure strains in genus Perilla. Perilla plants cultivated under a certain set of conditions had different caffeic acid and rosmarinic acid contents. For example, their contents were higher in P. setoyensis ("Setoegoma"), suggesting that the genetic background of the species greatly affects caffeic acid and rosmarinic acid contents. Several strains of P. frutescens var. crispa were cultivated at the Experimental Station for Medicinal Plants, Graduate School of Pharmaceutical Sciences, Kyoto University and differences in their caffeic acid and rosmarinic acid contents were also observed. The total content of anthocyanins, which are closely related to the leaf color of perilla, was measured as cyanidin-3-glucoside equivalents, and a weak positive correlation was observed between the content of rosmarinic acid, and the total content of total anthocyanins. Furthermore, the results suggest that luminosity and photon flux density of light during cultivation can affect rosmarinic acid content.
Assuntos
Ácidos Cafeicos/química , Cinamatos/química , Depsídeos/química , Perilla/química , Extratos Vegetais/química , Folhas de Planta/química , Ácido RosmarínicoRESUMO
The effect of chemical refining process on the bioactive composition, in vitro antioxidant capacity, and their correlation of perilla seed oil (PSO) were investigated. In this paper, seven samples corresponding to each step of the refining process (degumming, neutralization, bleaching, deodorization, winterization, crude, and refined oils) were studied. The results showed that phenolic compounds and tocopherols were removed from PSO to a degree of 19.4% and 5.4%, respectively. In addition, the carotenoid content of PSO decreased during the refining process. The main carotenoid of PSO was found to be lutein, and the compound was lost completely during the bleaching step of the refining process. In this paper, we analyzed the variation of carotenoid content in PSO during the refining process for the first time. Neutralization affected the contents of phytosterols the most, followed by the effects of degumming and bleaching. The demonstrated results of Pearson product-moment correlation indicated that total tocopherols were significantly correlated with the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and oxygen radical absorption capacity (ORAC) values, whereas carotenoids were significantly correlated with the DPPH value. However, phenolic compounds and phytosterols have no significant difference with DPPH, 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt, ORAC, and ferric reducing antioxidant power values. The collected information can be applied to seeking out optimum factors needed to suffice the fundamental requirements for PSO production and minimize micronutrient losses to enhance its market value. PRACTICAL APPLICATION: The present study aimed to determine influence of chemical refining in the bioactive composition of perilla seed oil (PSO) as well as its antioxidant capacity in vitro. Moreover, we also intend to find the correlation between them. Results indicated that this study supplies a good reference for the industrial parameters of the refining process to minimize micronutrient losses and further obtain high-quality PSO products for consumers.
Assuntos
Antioxidantes/química , Manipulação de Alimentos/métodos , Perilla/química , Ácido alfa-Linolênico/química , Carotenoides/química , Micronutrientes/química , Fenóis/análise , Fitosteróis/química , Óleos de Plantas/química , Sementes/química , Tocoferóis/químicaRESUMO
A portion of the fat used in the preparation of meatballs was replaced with different amounts of Perilla seeds rich in unsaturated fatty acids. Five treatments with mass percentages of 0%, 5%, 10%, 15%, and 20%, including a set of blank treatment and four groups treated with different Perilla seed contents, were performed. The effects of Perilla seed content on the proximate composition, pH, color, cooking yield, emulsion stability, texture, fatty acid composition, and sensory properties of meatballs were analyzed. The meatballs with Perilla seeds showed remarkably better properties than those without seeds. The addition of 10% (w/w) Perilla seeds significantly (Pâ¯<â¯0.05) improved the texture, composition, and content of polyunsaturated fatty acids (PUFAs), dietary fiber, and protein in meatballs. Moreover, the characteristic flavor components were rich and varied, which enhanced the taste, flavor, and satiety of the meatballs. This work provided theoretical and data support for the preparation of Perilla meatballs rich in PUFAs and dietary fiber.
Assuntos
Gorduras na Dieta , Qualidade dos Alimentos , Produtos da Carne/análise , Perilla/química , Carne de Porco/análise , Sementes/química , Adulto , Animais , Cor , Culinária , Feminino , Humanos , Concentração de Íons de Hidrogênio , Masculino , Pessoa de Meia-Idade , Suínos , Paladar , Adulto JovemRESUMO
High-quality perilla leaves are defined as those having purple upper and lower surfaces and a pleasant smell. The Japanese Pharmacopoeia specifies the content of essential oils in perilla leaves but not the content of rosmarinic acid. Rosmarinic acid is a common component of Labiatae plants such as shiso (Perilla frutescens Britton var. crispa W. Deane). Rosmarinic acid has been reported to exhibit anti-inflammatory and anti-oxidant activity but the factors affecting the content of rosmarinic acid in plants remain unknown. This study describes a simple and reproducible method for quantifying rosmarinic acid. We elucidated the main causes for the different rosmarinic acid contents of plants by examining various samples of perilla using the proposed method. Significant differences in rosmarinic acid content between varieties and cultivators were observed. The rosmarinic acid content was higher in green perilla compared with red perilla, in wild species compared with cultivated species, and in plants cultivated in outdoor nurseries compared with in indoor nurseries. The proposed quantitative method was used to examine the rosmarinic acid content in a Kampo formula, Hangekobokuto, and was found to be higher in decoctions prepared using the Kouge method compared with the typical preparation method. We examined the chlorophyll and caffeic acid contents of several samples and their relationship with the rosmarinic acid content.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Cinamatos/química , Depsídeos/química , Perilla frutescens/química , Perilla/química , Extratos Vegetais/química , Folhas de Planta/química , Cinamatos/farmacologia , Depsídeos/farmacologia , Ácido RosmarínicoRESUMO
Perilla oil (PerO), a natural oil with a high unsaturated fatty acid content derived from the mature seeds of Perilla frutescens, is a homology of medicine and food. The type 2 diabetes mellitus (T2DM) model was successfully established using a high-fat and high-sugar diet combined with a single low-dose of streptozocin (STZ). PerO intervention reduced the levels of fasting blood glucose and the level, size and accumulation of lipid droplets, increased the insulin level and diminished the body weight loss. PerO pretreatment markedly promoted the serum levels of alanine transaminase (ALT) and aspartate transaminase alanine (AST) and inhibited the levels of glucose (GLU), glucose-6-phosphate dehydrogenase (G6PD), triglycerides (TGs) and total cholesterol (TC). Moreover, PerO treatment enhanced the expression of phosphoinositide-3 kinase (PI3K)/protein kinase B (AKT) and activated the expression of glucose transporter 4 (Glut4) and phospho-AKT serine/threonine kinase (p-AS160) in the liver. Additionally, PerO treatment distinctly decreased the abundance of Aerococcus and facilitated the richness of Alloprevotella in the intestine, as well as accelerated the restoration of the gut microflora diversity. Thus, PerO regulates intestinal microbiota and alleviates insulin resistance through the PI3K/AKT signaling pathway in type-2 diabetic KKAy mice and may be a potential functional food for diabetic treatment.
Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Microbioma Gastrointestinal/efeitos dos fármacos , Hipoglicemiantes/uso terapêutico , Resistência à Insulina/fisiologia , Transdução de Sinais/efeitos dos fármacos , Ácido alfa-Linolênico/uso terapêutico , Animais , Glicemia/metabolismo , Peso Corporal/efeitos dos fármacos , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/fisiopatologia , Diabetes Mellitus Tipo 2/induzido quimicamente , Diabetes Mellitus Tipo 2/fisiopatologia , Insulina/metabolismo , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Camundongos Endogâmicos C57BL , Músculo Esquelético/efeitos dos fármacos , Músculo Esquelético/patologia , Perilla/química , Fosfatidilinositol 3-Quinase/metabolismo , Óleos de Plantas/uso terapêutico , Proteínas Proto-Oncogênicas c-akt/metabolismo , EstreptozocinaRESUMO
Macrophage polarization has been implicated in the pathogenesis of obesity and type 2 diabetes, which are recognized as chronic proinflammatory diseases. This study investigated that high level of glucose, similar to lipopolysaccharide (LPS), activated macrophages toward M1 phenotypes and 1-20 µM asaronic acid (AA) counteracted diabetic macrophage activation. AA reduced the LPS-promoted secretion of proinflammatory interleukin (IL)-6 and monocyte chemoattractant protein-1. The LPS markedly elevated the macrophage induction of the M1 markers of Toll-like receptor 4 (TLR4), CD36, and CD68, which was attenuated by AA. Also, the LPS significantly enhanced the nuclear factor (NF)-κB transactivation, signal transducers, and activators of transcription 1 (STAT1)/STAT3 activation and suppressor of cytokine signaling 3 (SOCS3) induction in macrophages. However, AA highly suppressed the aforementioned effects of LPS. Glucose-stimulated macrophages expressed advanced glycation end products (AGEs) and receptor for AGE (RAGE). Administration of 20 µM AA to macrophages partly but significantly attenuated such effects (1.65 ± 0.12 vs 0.95 ± 0.25 times glucose control for AGE; 2.33 ± 0.31 vs 1.40 ± 0.22 times glucose control for RAGE). Furthermore, glucose enhanced the macrophage induction of TLR4 and inducible nitric oxide synthase and IL-6 production, while it demoted the production of anti-inflammatory arginase-1 and IL-10. In contrast, AA reversed the induction of these markers in glucose-loaded macrophages. AA dose-dependently and significantly encumbered NF-κB transactivation, Janus kinase 2 (JAK2) and STAT1/STAT3 activation, and SOCS3 induction upregulated in glucose-supplemented macrophages. These results demonstrated for the first time that AA may limit diabetic macrophage activation toward the M1 phenotype through the inhibition of TLR4-/IL-6-mediated NF-κB/JAK2-STAT signaling entailing AGE-RAGE interaction.
Assuntos
Benzoatos/farmacologia , Glucose/imunologia , Janus Quinase 2/imunologia , Macrófagos/efeitos dos fármacos , NF-kappa B/imunologia , Extratos Vegetais/farmacologia , Fator de Transcrição STAT1/imunologia , Fator de Transcrição STAT3/imunologia , Animais , Linhagem Celular , Interleucina-6/genética , Interleucina-6/imunologia , Janus Quinase 2/genética , Ativação de Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Camundongos , NF-kappa B/genética , Perilla/química , Fator de Transcrição STAT1/genética , Fator de Transcrição STAT3/genéticaRESUMO
The past decade has witnessed the great promise of strategies for ligand discovery based on surface-immobilized GPCRs. We present here a method for preparation of immobilized GPCRs. Key features include covalent immobilization with high specificity and robust application in drug-receptor interaction analysis and ligand screening. In our example assay using beta2-adrenergic receptor (ß2-AR), the human DNA repair protein O6-alkylguanine-DNA alkyltransferase (hAGT) fusion receptor expressed in Escherichia coli was directly captured onto polyethylene glycol polyacrylamide (PEGA) resin. We observed even distribution and physiological functions of ß2-AR on the resin. The immobilized ß2-AR as a stationary phase enabled us to rapidly determine the binding of four drugs to ß2-AR. By coupling this assay to mass spectrometry, we screened rosmarinic acid as a bioactive compound targeting ß2-AR in Fructus Perillae. We concluded that O6-benzylguanine derivative-functionalized supporter is promising for specific immobilization of hAGT-tagged proteins; immobilized receptor chromatography has great potential in screening receptor-binding leads from herbal plants or traditional medicine recipes.
Assuntos
Cinamatos/farmacologia , Depsídeos/farmacologia , Descoberta de Drogas , Guanina/análogos & derivados , Ensaios de Triagem em Larga Escala , Receptores Adrenérgicos beta 2/metabolismo , Cinamatos/química , Depsídeos/química , Guanina/química , Guanina/metabolismo , Humanos , Ligantes , Perilla/química , Receptores Adrenérgicos beta 2/análise , Propriedades de Superfície , Ácido RosmarínicoRESUMO
Allergic rhinoconjunctivitis (AR) treatment is usually pharmacological in children, but medications are merely symptomatic, may not be completely effective, and may have relevant side effects. Thus, doctors and parents look at complementary medicine, including nutraceuticals. Lertal®, an oral nutraceutical, contains extract of Perilla, quercetin, and Vitamin D3 It has been reported that adults with AR diminished allergic symptoms and medication use during Lertal® therapy. Therefore, the current polycentric, randomized, double blind, parallel-group, placebo-controlled study aimed to evaluate the efficacy and safety of Lertal® as an add-on treatment in children with AR. In this study, 146 children (94 males and 52 females, mean age 9.1±1.88) were randomly assigned to Lertal® + standard treatment or Placebo + standard treatment and were visited at baseline (W0), and after 2 (W2) and 4 weeks (W4). Standard treatment consisted of continuous antihistaminic schedule. The primary endpoint was the Total Symptom Score (TSS - last 12 hours) change from the baseline to the end of the 4-week treatment. Both groups significantly (p less 0.0001 for both) reduced TSS (last 12 hours) after 4 weeks (% change: - 63.6% in Lertal®-group and - 60.7% in Placebo-group; p= n.s. intergroup analysis). Notably, 24 children had symptom worsening between W2 and W4: 8 in the Lertal®-group and 16 in the Placebo-group, with significant intergroup difference (p less than 0.05). All of them were poly-allergic subjects exposed to multiple allergens. There was no relevant adverse event. The present study documented that Lertal®, as add-on treatment, was able to significantly prevent the occurrence of clinical worsening and was safe in AR poly-allergic children.
Assuntos
Conjuntivite Alérgica/tratamento farmacológico , Suplementos Nutricionais , Extratos Vegetais/uso terapêutico , Criança , Colecalciferol , Método Duplo-Cego , Feminino , Humanos , Masculino , Perilla/química , Resultado do Tratamento , Vitamina D/uso terapêuticoRESUMO
A kinetic study of the reaction of singlet oxygen (1O2) with eight vegetable oils 1-8 containing different concentrations of tocopherols (Tocs) and tocotrienols (Toc-3s) was performed. The second-order rate constants (kQ) for the reaction of 1O2 with vegetable oils 1-8 (rice bran, perilla, rape seed, safflower, grape seed, sesame, extra virgin olive, and olive oils) were measured in ethanol/chloroform/D2O (50:50:1, v/v/v) solution at 35°C using UV-vis spectrophotometry. Furthermore, comparisons of kQ values determined for the above oils 1-8 with the sum of the product {∑kQAO-i [AO-i]/105} of the kQAO-i values obtained for each antioxidant (AO-i) and concentration (in mg/100 g) ([AO-i]/105) of AO-i (Tocs and Toc-3s) contained in the oils 1-8 were performed. The observed kQ values were not reproduced by the kQ values calculated using only the concentrations of the four Tocs and Toc-3s. These results suggest that the contribution of fatty acids contained in the oils 1-8 is also necessary to fully explain the kQ values. Recently, the second-order rate constants (kS) for the reaction of aroxyl radical (ArOã») with the same vegetable oils 1-8 were measured in the same solvent at 25â using stopped-flow spectrophotometry (Ref. 23). The kS values obtained could be well explained as the sum of the product {Σ kSAO-i [AO-i]/105} of the kSAO-i and the [AO-i]/105 of AO-i (Tocs and Toc-3s) contained in the vegetable oils.
Assuntos
Óleos de Plantas/química , Oxigênio Singlete/química , Brassica rapa/química , Carthamus tinctorius/química , Ácidos Graxos/química , Cinética , Olea/química , Oryza/química , Perilla/química , Sesamum/química , Tocoferóis/química , Tocotrienóis/química , Vitis/químicaRESUMO
Perilla oil has been shown to be beneficial for ameliorating metabolic disorders, but its protective effect is still controversial. We investigated the effect of perilla oil on obesity-induced hepatic and vascular changes in high-fat diet (HFD)-fed mice and provided underlying mechanisms for potential therapeutic applications. Tomato and paprika extract was added to prevent the oxidation during storage of perilla oil. HFD-fed mice were orally administered palm or perilla oil for 90 days. Food intake, body and liver weight, and serum cholesterol levels were measured. Arterial and hepatic lipid accumulation was determined by histological staining. Hepatic triglyceride levels and the expression of proteins regulating lipid metabolism were analyzed. Food intake and body weight were not different between palm oil-treated and perilla oil-treated mice. Serum cholesterol level was significantly lower in perilla oil-treated mice compared with palm oil-treated mice. HFD-induced lipid accumulation was also lower in thoracic aorta and liver by perilla oil compared with palm oil. Perilla oil also decreased hepatic triglyceride level without changing the liver weight. Perilla oil treatment increased the AMP-activated protein kinase and acetyl-CoA carboxylase phosphorylation and the lipolytic protein levels, whereas it decreased the lipogenic protein levels in the liver. In conclusion, perilla oil reduced serum cholesterol and arterial and hepatic lipid accumulation in HFD-fed mice. The data suggest that perilla oil improves the balance of lipogenic and lipolytic protein expression, and ameliorates obesity-induced metabolic disorders and cardiovascular diseases.
Assuntos
Aorta/efeitos dos fármacos , Dieta Hiperlipídica , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Obesidade/complicações , Perilla/química , Ácido alfa-Linolênico/farmacologia , Proteínas Quinases Ativadas por AMP/metabolismo , Acetil-CoA Carboxilase/metabolismo , Animais , Aorta/metabolismo , Colesterol/sangue , Gorduras na Dieta/sangue , Fígado Gorduroso/sangue , Fígado Gorduroso/prevenção & controle , Lipogênese/efeitos dos fármacos , Lipólise/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos Endogâmicos C57BL , Obesidade/metabolismo , Fosforilação , Fitoterapia , Extratos Vegetais/farmacologia , Óleos de Plantas/farmacologia , Triglicerídeos/sangueRESUMO
Therapeutic approaches for neurodegeneration, such as Alzheimer's disease (AD), have been widely studied. One of the critical hallmarks of AD is accumulation of amyloid beta (Aß). Aß induces neurotoxicity and releases inflammatory mediators or cytokines through activation of glial cell, and these pathological features are observed in AD patient's brain. The purpose of this study is to investigate the protective effect of alpha-linolenic acid (ALA) on Aß25-35-induced neurotoxicity in C6 glial cells. Exposure of C6 glial cells to 50 µM Aß25-35 caused cell death, overproduction of nitric oxide (NO), and pro-inflammatory cytokines release [interleukin (IL)-6 and tumor necrosis factor-α], while treatment of ALA increased cell viability and markedly attenuated Aß25-35-induced excessive production of NO and those inflammatory cytokines. Inhibitory effect of ALA on generation of NO and cytokines was mediated by down-regulation of inducible nitric oxide synthase and cyclooxygenase-2 protein and mRNA expressions. In addition, ALA treatment inhibited reactive oxygen species generation induced by Aß25-35 through the enhancement of the nuclear factor-erythroid 2-related factor-2 (Nrf-2) protein levels and subsequent induction of heme-oxygenase-1 (HO-1) expression in C6 glial cells dose- and time-dependently. Furthermore, the levels of neprilysin and insulin-degrading enzyme protein expressions, which contribute to degradation of Aß, were also increased by treatment of ALA compared to Aß25-35-treated control group. In conclusion, effects of ALA on Aß degradation were shown to be mediated through inhibition of inflammatory responses and activation of antioxidative system, Nrf-2/HO-1 signaling pathway, in C6 glial cells. Our findings suggest that ALA might have the potential for therapeutics of AD.