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Abstract The present study was conducted to evaluate the chemical composition, antioxidant activity and hypoglycemic effects of whole kumquat (Ku) powder in diabetic rats fed a high-fat-high-cholesterol (HFHC) diet. The antioxidant activities were evaluated using stable 1,1-diphenyl 2-picrylhydrazyl (DPPH) free radical scavenging method, 2,2´-azinobis (3-ethyl benzo thiazoline-6-sulphonic acid) radical cation (ABTS) and Ferric reducing antioxidant power (FRAP). Total phenolic content was (51.85 mg GAE/g) and total flavonoid content was (0.24 mg Cateachin Equivalent, CE/g). DPPH and ABTS values were 3.32 and 3.98 mg Trolox equivalent (TE)/g where FRAP value was 3.00 mM Fe2+/kg dry material. A total of 90 albino rats were used in the present study. Rats group were as follows: normal diet; normal treated (2, 4, and 6% Ku.), diabetic rats (non-treated), diabetic + HFHC diet (non-treated), HFHC (non-treated), Diabetic (treated), HFHC (treated) and Diabetic + HFHC (treated). The diets were followed for 8 weeks. Blood samples were collected at the end of the experiment. Serum glucose was recorded and thyroid hormones (T4, Thyroxine and T3, Triiodothyronine) were conducted. Diet supplemented with Kumquat at different concentrations have a hypoglycemic effect and improve the thyroid hormones of both diabetic rats and HFHC diabetic rats.
Resumo O presente estudo foi conduzido para avaliar a composição química, a atividade antioxidante e os efeitos hipoglicêmicos do pó de kumquat (Ku) em ratos diabéticos alimentados com uma dieta rica em gordura e colesterol (HFHC). As atividades antioxidantes foram avaliadas usando o método de eliminação de radicais livres de 1,1-difenil 2-picrilhidrazil (DPPH), 2,2'-azinobis (ácido 3-etilbenzotiazolina-6-sulfônico) radical cátion (ABTS) e antioxidante redutor férrico potência (FRAP). O conteúdo fenólico total foi (51,85 mg GAE / g) e o conteúdo total de flavonoides foi (0,24 mg Cateachin Equivalent, CE / g). Os valores de DPPH e ABTS foram 3,32 e 3,98 mg equivalente de Trolox (TE) / g, em que o valor de FRAP foi de 3,00 mM Fe2 + / kg de material seco. Um total de 90 ratos albinos foi usado no presente estudo. O grupo dos ratos foi o seguinte: dieta normal: tratados normais (2, 4 e 6% Ku.), ratos diabéticos (não tratados), diabéticos + dieta HFHC (não tratados), HFHC (não tratados), diabéticos (tratados), HFHC (tratados) e diabéticos + HFHC (tratados). As dietas foram seguidas por 8 semanas. Amostras de sangue foram coletadas ao final do experimento. A glicose sérica foi registrada e os hormônios tireoidianos (T4, Tiroxina e T3, Triiodotironina) foram conduzidos. A dieta suplementada com kumquat em diferentes concentrações tem um efeito hipoglicêmico e melhora os hormônios tireoidianos tanto de ratos diabéticos quanto de ratos diabéticos com HFHC.
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Animaux , Rats , Rutaceae , Diabète expérimental/traitement médicamenteux , Poudres , Hormones thyroïdiennes , Glycémie , FruitRésumé
Abstract Allium cepa L. is a commonly consumed vegetable that belongs to the Amaryllidaceae family and contains nutrients and antioxidants in ample amounts. In spite of the valuable food applications of onion bulb, its peel and outer fleshy layers are generally regarded as waste and exploration of their nutritional and therapeutic potential is still in progress with a very slow progression rate. The present study was designed with the purpose of doing a comparative analysis of the antioxidant potential of two parts of Allium cepa, i.g., bulb (edible part) and outer fleshy layers and dry peels (inedible part). Moreover, the inhibitory effect of the onion bulb and peel extracts on rat intestinal α-glucosidase and pancreatic α-amylase of porcine was also evaluated. The antioxidant potential of onion peel and bulb extracts were evaluated using 2,2-diphenyl- 1-picryl hydrazyl (DPPH), ferric-reducing antioxidant power assay (FRAP), 2,2'-azino-bis- 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging assay, H2O2 radical scavenging activity and Fe2+ chelating activity. Total flavonoids and phenolic content of ethanolic extract of onion peel were significantly greater as compared to that of onion bulb. Ethanolic extract of onion peel also presented better antioxidant and free-radical scavenging activity as compared to the ethanolic extract of bulb, while the aqueous extract of bulb presented weakest antioxidative potential. Onion peel extract's α-glucosidase inhibition potential was also correlated with their phenolic and flavonoid contents. The current findings presented onion peel as a possible source of antioxidative agents and phenolic compounds that might be beneficial against development of various common chronic diseases that might have an association with oxidative stress. Besides, outer dry layers and fleshy peels of onion exhibited higher phenolic content and antioxidant activities, compared to the inner bulb. The information obtained by the present study can be useful in promoting the use of vegetable parts other than the edible mesocarp for several future food applications, rather than these being wasted.
Resumo Allium cepa pertence à família Liliaceae e é rica em nutrientes e antioxidantes. Apesar das expressivas aplicações alimentares do bulbo da cebola, sua casca e outras camadas externas são geralmente consideradas resíduos, e seu potencial nutricional e terapêutico ainda é pouco explorado. O presente estudo foi delineado com o objetivo de investigar comparativamente o potencial antioxidante de duas partes de Allium cepa, por exemplo o bulbo (parte comestível) e camadas externas e cascas secas (parte não comestível). Além disso, o efeito inibitório dos extratos do bulbo de cebola e casca sobre a α-glucosidase intestinal de ratos e α-amilase pancreática suína também foi avaliado. O potencial antioxidante dos extratos da casca de cebola e bulbo foi avaliado utilizando-se 2,2-difenil-1-picrilhidrazil (DPPH), método de poder antioxidante de redução do ferro (FRAP), método 2,2'-azino-bis-3-etilbenzotiazolina-6-ácido sulfônico (ABTS) de eliminação de radicais, atividade de eliminação de radicais H2O2 e atividade quelante do Fe2+. Os flavonoides totais e os teores fenólicos do extrato de etanol da casca de cebola foram significativamente maiores quando comparados ao do bulbo. O extrato de etanol da casca de cebola também apresentou melhor atividade antioxidante e eliminação de radicais livres quando comparado ao extrato de etanol do bulbo, enquanto o extrato aquoso de bulbo apresentou menor potencial antioxidante. O potencial de inibição da α-glicosidase dos extratos de casca de cebola correlacionou-se com seus teores fenólicos e de flavonoides. Os resultados encontrados identificaram que a casca de cebola é uma possível fonte de agentes antioxidantes e compostos fenólicos que podem ser benéficos contra o desenvolvimento de várias doenças crônicas que estão associadas ao estresse oxidativo. Além disso, as camadas externas secas e as cascas da cebola exibiram maior conteúdo fenólico e atividades antioxidantes, em comparação com o bulbo interno. As informações obtidas pelo presente estudo podem promover o uso de outras partes vegetais além do mesocarpo comestível para futuras aplicações em alimentos, ao invés de serem desperdiçadas.
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Animaux , Rats , Oignons , Antioxydants , Suidae , Extraits de plantes/pharmacologie , alpha-Glucosidase , Peroxyde d'hydrogèneRésumé
Resumen: Antecedentes: los conservantes de origen sintético, como nitratos y nitritos, empleados en la industria alimentaria para la conservación de matrices cárnicas, han reportado efectos desfavorables a largo plazo en la salud de los consumidores recurrentes. Objetivo: conocer las características fisicoquímicas y antimicrobianas del propóleo como potencial bioconservante en matrices cárnicas de alto consumo. Materiales y métodos: se desarrolló una revisión bibliográfica de literatura acorde a la pregunta problema planteada por el grupo de investigación, y se llevó a cabo una búsqueda en las bases de datos Scopus, NCBI, SciELO, ScienceDirect y Google Scholar de artículos de revisión, artículos científicos, libros y trabajos de grado. Resultados: el propóleo es un compuesto natural con una variedad amplia de elementos útiles para la conservación de matrices cárnicas, por sus propiedades antimicrobianas y antioxidantes. Conclusiones: el propóleo presenta propiedades antimicrobianas y antioxidantes útiles en el campo de la industria alimentaria, por lo que se considera una de las alternativas más viables para la conservación de productos cárnicos y la disminución del uso de conservantes sintéticos en producción cárnica. No obstante, es fundamental el desarrollo de más investigaciones que permitan evaluar el comportamiento de los compuestos activos del propóleo en las diversas matrices cárnicas.
Abstract: Background: Preservatives of synthetic origin, such as nitrates and nitrites, used in the food industry for the preservation of meat matrices, have reported long-term unfavorable effects on the health of recurrent consumers. Objective: To know the physicochemical and antimicrobial characteristics of propolis as a potential biopreservative in high consumption meat matrices. Materials and Methods: A bibliographic review of literature was developed according to the problem question posed by the research group, carrying out a search in the Scopus, NCBI, SciELO, ScienceDirect and Google Scholar databases of review articles, scientific articles, books and works degree. Results: Propolis is a natural compound with a wide variety of useful elements for the conservation of meat matrices, due to its antimicrobial and antioxidant properties. Conclusions: Propolis has useful antimicrobial and antioxidant properties in the field of the food industry, being considered one of the most viable alternatives for the preservation of meat products and the reduction of the use of synthetic preservatives in meat production. However, it is essential to develop more research to evaluate the behavior of the active compounds of propolis in the various meat matrices.
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Introduction: Myocardial ischemia-reperfusion (I/R) injury is one of the mechanisms contributing to the high mortality rate of acute myocardial infarction. Purpose: This study intended to study the role of naringin in cardiac I/R injury. Methods: AC16 cells (human cardiomyocyte cell line) were subjected to oxygen-glucose deprivation/recovery (OGD/R) treatment and/or naringin pretreatment. Then, the apoptosis was examined by flow cytometry and Western blotting. The concentration of IL-6, IL-8 and TNF-α was measured by enzyme-linked immunosorbent assay (ELISA) kits. How naringin influenced microRNA expression was examined by microarrays and quantitative real-time polymerase chain reaction (qRT-PCR). Dual luciferase reporter assay was employed to evaluate the interaction between miR-126 and GSK-3ß. The GSK-3ß/ß-catenin signaling pathway was examined by Western blotting. Finally, rat myocardial I/R model was created to examine the effects of naringin in vivo. Results: Naringin pretreatment significantly decreased the cytokine release and apoptosis of cardiomyocytes exposed to OGD/R. Bioinformatical analysis revealed that naringin upregulated miR-126 expression considerably. Also, it was found that miR-126 can bind GSK-3ß and downregulate its expression, suggesting that naringin could decrease GSK-3ß activity. Next, we discovered that naringin increased ß-catenin activity in cardiomyocytes treated with OGD/R by inhibiting GSK-3ß expression. Our animal experiments showed that naringin pre-treatment or miR-126 agomir alleviated myocardial I/R. Conclusions: Naringin preconditioning can reduce myocardial I/R injury via regulating miR-126/GSK-3ß/ß-catenin signaling pathway, and this chemical can be used to treat acute myocardial infarction.
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Animaux , Rats , Lésion d'ischémie-reperfusion/traitement médicamenteux , Ischémie myocardique/traitement médicamenteux , Flavanones/administration et posologie , bêta-Caténine/analyseRésumé
Objective To explore the effect of circadian rhythm genes on flavonoids biosynthesis in safflower and its molecular mechanism. Methods Based on the transcriptome and metabolomic database of safflower corolla, we screened the circadian rhythm genes that correlate with biosynthesis of flavonoids in safflower. qPCR was used to quantify the expressions of circadian rhythm genes in different flowering stages at different time points in a single day. LC-MS was performed to determine the accumulation of flavonoids. The correlation between them was analyzed as well. Yeast Two-Hybrid experiment was used to verify the interactive proteins of these genes. Results Seven circadian rhythm genes PRR1, PRR2, ELF3, FT, PHYB, GI and ZTL were obtained. PRR1 gene was positively correlated with flavonoids accumulation (r≥0.7). The full length of PRR1 is 3 201 bp, encoding 421 amino acids, which is highly homologous with rice OsPRR73 gene and named as CtPRR1 (GenBank accession number: MW492035). CtPRR1 was mainly expressed in flowers, and the expression level increased in the daytime and declined in the evening gradually. Correspondingly, the content of flavonoids showed an opposite variation. Both of them displayed a circadian rhythm with a negative correlation (r≥−0.7). In addition, 2 heat shock proteins along with 3 AP2 transcription factors interacting with CtPRR1 protein were obtained via Yeast Two-Hybrid experiment. Conclusion CtPRR1 negatively regulated the safflower flavonoids accumulation in a circadian rhythm way, which may be affected by these interacting proteins.
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OBJECTIVE To study the imp rovement effects of total flavonoids of Psidium guajava leaves on myocardial hypertrophy in hypertensive model rats. METHODS Ten rats were randomly selected from 60 healthy SD rats as the normal group ; other 50 rats established hypertensive model ,and 44 rats with successful modeling were randomly divided into model group , anisomycin group [p38 mitogen-activated protein kinase (p38 MAPK)activator,1 mg/kg],total flavonoids of P. guajava leaves+ anisomycin group (200 mg/kg total flavonoids+ 1 mg/kg anisomycin )and total flavonoids of P. guajava leaves group (200 mg/kg) by random volume mass ranking method ,with 11 rats in each group. Rats in normal group and model group were given 3% hydroxymethylcellulose sodium solution ,and other groups were given relevant solution intragastrically ,once a day ,for consecutive 6 weeks. Blood pressure (systolic blood pressure ,diastolic blood pressure ,mean arterial pressure ),cardiac index and left ventricular index were measured. The levels of tumor necrosis factor-α(TNF-α),interleukin-1β(IL-1β)and IL- 6 in myocardial tissue were detected. The pathomorphological changes of myocardial tissue were observed. The expression of p 38 MAPK, phosphorylated p 38 MAPK (p-p38 MAPK),extracellular regulated protein kinase 1/2 (ERK1/2),phosphorylated ERK 1/2 (p-ERK1/2),c-Jun N-terminal kinase (JNK)and phosphorylated JNK (p-JNK)in myocardial tissue were detected. RESULTS Compared with normal group ,the systolic blood pressure ,diastolic blood pressure ,mean arterial pressure ,cardiac index ,left ventricular index as well as the levels of TNF-α,IL-1β and IL-6 and protein expression of p-p 38 MAPK,p-ERK1/2 and p-JNK in myocardial tissue were increased significantly in anisomycin group and model group (P<0.05);it was also found that hypertrophy of cardiomyocytes ,disorder of myocardial fibers ,looseness,edema and proliferation of connective tissue between myocardial fibers,increased infiltration of inflammatory cells ,etc. Compared with anisomycin group and model group ,the le vels of above indexes in total flavonoids of P. guajava leaves+ anisomycin group and total flavonoids of P. guajava leaves group were decreased significantly (P<0.05); cardiomyocytes were 163.com slightly larger and arranged reasonably ;the degree of myocardial hypertrophy,looseness,edema and proliferation of connective tissue were relieved ,and the improvement effect of total flavonoids of P. guajava leaves group was more significant (P<0.05). CONCLUSIONS The total flavonoids of P. guajava leaves can reduce blood pressure and improve myocardial hypertrophy in hypertensive model rats. Its mechanism may be related to the inhibition of p38 MAPK signal pathway activity and the expression of inflammatory factors.
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Flavonoids is one of the biggest families of the plant-derived secondary metabolites with structural diversity. Until now, over 10 000 kinds of flavonoids with distinct structures have been purified and identified from plants, and some of them possess a range of important pharmacological effects, such as anticancer, anti-inflammatory and so on. So far, a number of genes and enzymes responsible for the biosynthesis of flavonoids have been reported, especially, a great of progress has been achieved in the synthetic biology of flavonoids in the recent years. Herein, based upon a brief introduction on the biosynthesis of flavonoids, this review summarizes the research advances in synthetic biology of flavonoids in the past two decades (2001-2021), highlighting the cell factories construction of the representative flavonoids. And, a brief discussion and prospects of the relevant metabolic bottlenecks and optimizing strategies are proposed.
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OBJECTIVE To study the improvement effects of different polar parts fro m total f lavonoids of Scutellaria amoena on non-alcoholic fatty liver disease (NAFLD)model rats. METHODS The total flavonoids of S. amoena (SAF)were extracted by reflux extraction with ethanol ,suspended with water ,and then extracted with ethyl acetate and n-butanol in order to obtain the extraction parts of SAF (recorded as SAFA and SAFB respectively ). Thirty-six rats were randomly divided into normal group (n= 6)and modeling group (n=30). Modeling group was given high-lipid diet to induce NAFLD model. After modeling ,modeling group was randomly divided into model group (normal saline ),fenofibrate group (positive control ,20 mg/kg),SAF group (300 mg/kg),SAFA group (300 mg/kg)and SAFB group (300 mg/kg);they were given relevant intragastical administration ,once a day,for consecutive 6 weeks. After last administration ,the liver index was calculated ;the levels of total cholesterol (TC), triacylglycerol(TG),aspartate transaminase (AST),alanine transaminase (ALT),high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C) in serum ,the levels of superoxide dismutase (SOD),glutathione peroxidase (GSH-Px),malondialdehyde(MDA),interleukin-1β(IL-1β),IL-6 and tumor necrosis factor-α(TNF-α)in liver tissue were detected;the pathomorphological changes of liver tissue were observed. RESULTS Compared with normal group ,the liver index , the levels of TC ,TG,AST,ALT,LDL-C,MDA,IL-1β, IL-6 and TNF-α in serum/liver tissue of model group were all increased significantly (P<0.05), while the levels of HDL-C,SOD and GSH-Px were all decreased significantly (P<0.05). Compared with model group ,except there was no statistical significance in the serum levels of HDL-C and ALT in SAFA group (P>0.05),above indexes in serum/liver tissue of rats in groups of polar parts from total flavonoids of S. amoena were significantly improved (P<0.05);inflammatory cell infiltration and fatty vacuoles in liver tissue were significantly improved. Compared with SAF group and SAFA group ,the levels of TC,TG,AST,MDA,IL-6 and TNF-α were decreased significantly in SAFB group(P<0.05),while the level of SOD was increased significantly (P<0.05);pathomorphological changes of liver tissue were improved more significantly. CONCLUSIONS Each polar part from total flavonoids of S. amoena can improve NAFLD by regulating oxidative stress and inhibiting the secretion of inflammatory factors. The n-butanol polar part has more obvious effect .
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O BJECTIVE To investigate the regulatory effect of total fla vonoids of Matricaria recutita on lipid abnormalities in human hepatoma HepG 2 cells and its lipid-lowering mechanism. METHODS The high-content total flavonoids extract from M. recutita was isolated and purified by macroporous resin. HepG 2 cells were divided into control group (without administration ), model group (without administration ),fenofibrate group (positive control ,3.61 μg/mL)and M. recutita total flavonoids low-dose , medium-dose and high-dose groups (100,150 and 200 μg/mL). Except for control group ,lipid deposition model of HepG 2 cells in other groups were established by 1 mmol/L mixture of oleic acid and palmitic acid. After 24 hours of intervention ,the levels of free fatty acids (FFA)in cell supernatant and triglyceride (TG)and FFA in cells were detected ;Oil red O staining was used to observe the deposition of lipid droplets in cells and detect the content of lipid ;DAPI staining was used to observe the protein expression of diacylglycerol acyltransferase 2(DGAT2)in cells ,and fluorescence intensity of protein expression of DGAT 2 were also detected ; protein expressions of key enzymes of TG synthesis as acetyl CoA carboxylase (ACC),fatty acid synthase (FAS)and DGAT 2 were detected by Western blot. RESULTS After separation and purification ,the content of total flavonoids from M. recutita increased from 6.72% to 56.20%. The results of cell experiment showed that compared with control group ,the levels of TG and FFA in cells and FFA in the cell supernatant increased significantly in the model group ,the content of lipid in cells increased significantly,the fluorescence intensity of protein expression of DGAT 2 increased significantly ,and the protein expressions of ACC,FAS and DGAT 2 increased significantly (P<0.01); large number of lipid dro plets were accumulated in the cells. Compared with model group ,the levels of above indexes in M. recutita total flavonoids low-dose , medium-dose andhigh-dose groups were significantly reversed (P<0.01);the accumulation of lipid droplets in cells decreased significantly. CONCLUSIONS M. recutita total flavonoids can inhibit the TG synthesis of lipid depos ition model HepG 2 cell,reduce the lipid accumulation of cells and prevent the lipid damage of cells. Its mechanism may be related to the down-regulation of the expression of ACC/FAS/DGAT 2 pathway.
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Flavonoids are secondary metabolites that widely existing in traditional Chinese medicine. They have many biological activities and pharmacological effects. In recent years, studies have found that flavonoids can play an effective protective role in the treatments of ischemic stroke and ischemic heart disease through various ways. The mechanisms of their protective effects have been systematically explained in detail. For example, flavonoids can affect pathophysiological mechanisms such as antioxidant, inhibition of inflammatory response, apoptosis and autophagy pathway. This paper reviews the protective effect and mechanisms of the treatments of flavonoids on cardiovascular and cerebrovascular ischemic diseases by referring to relevant literatures. The purpose is to provide reference for future research and development of drugs for the treatments of cardiovascular and cerebrovascular diseases.
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OBJEC TIVE To optimize the simultaneous extraction technology of dietary fiber (DF)and flavonoids from the peel of Prunus armeniaca . METHODS The content of DF was calculated with enzyme-gravimetric method ,and the content of flavonoids was determined by ultraviolet spectrophotometry. The orthogonal design and single factor test were used to optimize the extraction technology ,with the factors of liquid-solid ratio ,pH,papain concentration ,α-amylase concentration ,temperature of enzymatic hydrolysis and time of enzymatic hydrolysis as factors ,using the contents of DF and flavonoids as indexes. RESULTS The optimal extraction technology included the solid-liquid ratio of 1 ∶ 10(g/mL),pH5,0.5% papain and 0.5% α-amylase, enzymatic hydrolysis at 50 ℃ for 1 h. After three times of validation ,the average content of DF was 0.801 g/g(RSD=1.95%), and the average content of flavonoids was 2.135 mg/g(RSD=2.44%). The average comprehensive score was 0.988(RSD= 0.81%). CONCLUSIONS The optimal extraction technology is stable and feasible.
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OBJECTIVE To establish the fingerprints of Xanthoceras sorbifolia and determine the contents of flavonoids . METHODS HPLC was adopted . Using epigallocatechin as reference ,the fingerprints of 11 batches(No. S1-S11)of X. sorbifolia were drawn with Similarity Evaluation System of Chromatographic Fingerprints of TCM (2004A edition ). The similarity evaluation was conducted ,the common peaks were also confirmed . Cluster analysis (CA)and principal component analysis (PCA)were also performed. Epigallocatechin was selected as internal reference ,and quantitative analysis of multi -components by single marker (QAMS)was used to determine the contents of gallocatechin ,catechin,epicatechin,dihydromyricetin,taxifolin and myricetin in 16 batches(No. S1-S16)of X. sorbifolia. The results were compared with the results of one point external standard method and standard curve method . RESULTS There were 15 common peaks in 11 batches of X. sorbifolia,and the similarity of them were 0.910-1.000. A total of 7 common peaks were identified ,i.e. galliccatechin(peak 1),epigallocatechin(peak 2),catechin(peak 3),epicatechin(peak 5),dihydromyricetin(peak 6),taxifolin(peak 14)and myricetin (peak 15). The results of CA showed that S5-S7 and S 9 were clustered into one category ,S8 and S 11 were clustered into one category ,S10 were clustered into one category,S1-S4 were clustered into one category . The results of PCA showed that accumulative variance contribution rate of 3 principal components was 99.24%;S5-S7 were clustered into one category ,S8-S11 were clustered into one category ,S3 and S 4 were clustered into one category ,S1 and S 2 were clustered into one category . With the exception of myricetin and a partial batches (S12,S14-S16) of catechin ,the RSDs measured by the three methods for galliccatechin ,catechin (remaining batches ), epicatechin,dihydromyricetin and taxifolin in 16 batches of X. sorbifolia were less than 4% (n=3). CONCLUSIONS The established HPLC fingerprint and the method for content determination can be used for the quality control of X. sorbifolia. QAMS method can be used for the content determination of galliccatechin,epicatechin,dihydromyricetin and taxifolin .
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Objective: To investigate the effect of piperine on human breast cancer cells. Methods: The effect of piperine on proliferation and migration of human breast cancer cells, MCF-7 and MDA-MB-231, was investigated using colony formation assays, wound healing assays, Matrigel migration assays, flow cytometry, RT-qPCR, and Western blotting assays. Results: Piperine inhibited the growth of MCF-7 and MDA-MB-231 cells and suppressed colony formation. Cell reduction at the G 0 / G 1 phase and cell arrest at the G 2 /M phase were observed in breast cancer cells. However, the significant effect was only demonstrated in MDA-MB-231 cells. Moreover, cancer cell migration was suppressed by piperine at low concentration. RT-qPCR and Western blotting assays showed that piperine downregulated Rac1 gene and protein expression. Conclusions: Piperine could inhibit growth and migration of breast cancer cells by reducing Rac1 gene and protein expression.
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Objective: To enhance the pharmaceutical potential and oral bioavailability of quercetin contents of Allium cepa peel extract by novel nanosuspension technology. Methods: Nanoprecipitation approach was successfully used for the formulation of nanosuspension. To obtain pharmaceutical-grade nanosuspension with minimum particle size and polydispersity index, sodium lauryl sulphate was selected as a stabilizer. Important formulation parameters were statistically optimized by the response surface methodology approach. The optimized nanosuspension was subjected to stability and in vitro dissolution testing and characterized by scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy, and zeta sizer. To evaluate the preeminence of nanosuspension over coarse suspension, comparative bioavailability studies were carried out in male albino rats. The pharmaceutical potential of developed nanosuspension was evaluated by antioxidant, antimicrobial, and toxicity studies. Results: The optimized nanosuspension showed an average particle size of 275.5 nm with a polydispersity index and zeta potential value of 0.415 and -48.8 mV, respectively. Atomic force microscopy revealed that the average particle size of nanosuspension was below 100 nm. The formulated nanosuspension showed better stability under refrigerated conditions. Nanosuspension showed an improved dissolution rate and a 2.14-fold greater plasma concentration of quercetin than coarse suspension. Moreover, the formulated nanosuspension exhibited enhanced antioxidant and antimicrobial potential and was non-toxic. Conclusions: Optimization of nanosuspension effectively improves the pharmaceutical potential and oral bioavailability of Allium cepa extract.
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Objective: To explore the effect of ethyl acetate gum resin extract of Boswellia serrata on lipopolysaccharide (LPS) induced inflammation and oxidative damage in hepatic and renal tissues of rats. Methods: The rats were divided into four groups: control, LPS, LPS+Boswellia serrata extracts (100 mg/kg and 200 mg/kg). LPS (1 mg/kg) and the extract (100 and 200 mg/kg, 30 min before LPS) were administered intraperitoneally for 3 weeks. The levels of liver enzymes, albumin, total protein, creatinine, blood urea nitrogen (BUN), interleukin (IL)-6, malondialdehyde (MDA), and total thiol groups and superoxide dismutase (SOD) and catalase (CAT) activities were measured. Results: The levels of liver enzymes, creatinine, and BUN, IL-6, MDA in the LPS group were markedly increased (P<0.001) while albumin, total protein, and total thiol concentration, as well as SOD and CAT activities, were decreased compared with the control group (P<0.05 or 0.01). Boswellia serrata extracts diminished the levels of liver enzymes, creatinine, BUN, IL-6, and MDA (P<0.01 and P<0.001), and elevated the concentration of total protein and total thiol and SOD and CAT activities (P<0.05 or 0.01). Conclusions: The ethyl acetate gum resin extract of Boswellia serrata reduces LPS-induced inflammatory reactions and oxidative damage, thus ameliorating hepatic and renal function.
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Objective: To investigate the antioxidative and antidiabetic effects of Harpephyllum caffrum bark infusion as well as its effects on glucogenic and nucleotide hydrolyzing enzyme activities in FeSO 4 - induced oxidative stress in rat hepatic tissue. Methods: Harpephyllum caffrum infusion was prepared from dried plant materials (40 g) infused in boiling water (400 mL) for 20 min at room temperature. The antioxidative and inhibitory activities against carbohydrate digestive enzymes of the infusion were determined using established protocols. The liver tissues of rats were used for glucose uptake assay and to evaluate the infusion's effect on endogenous antioxidant, glucogenic, and nucleotide hydrolyzing enzyme activities in FeSO 4 -induced hepatic injury. Results: The Harpephyllum caffrum infusion significantly reduced ferric iron (FRAP) and free radicals (OH • and DPPH) in a dose- dependent manner. It inhibited -amylase and -glucosidase activities and increased glucose uptake in hepatic tissues. FeSO 4 significantly decreased glutathione concentration, catalase, and superoxide dismutase activities while increasing malondialdehyde level, glycogen phosphorylase, fructose-1,6-bisphosphatase, and adenosine triphosphatase activities. However, treatment with Harpephyllum caffrum infusion reversed FeSO 4 -induced changes. Characterization of the infusion revealed the presence of catechol, O-pyrocatechuic acid, mequinol, maltol, and glycoside derivatives. Conclusions: The Harpephyllum caffrum infusion demonstrates antidiabetic and antioxidative potentials in in vitro models of type 2 diabetes as depicted by its ability to inhibit carbohydrate digestive enzymes, mitigate oxidative imbalance, and regulate glucogenic and nucleotide hydrolyzing enzyme activities in oxidative hepatic injury.
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MicroRNAs (miRNAs), small non-coding RNAs, play important roles in regulating host defense against pathogenic infections. This review provides information on the role of miRNAs in the antimycobacterial immune response and summarizes their possible diagnostic utility. It was compiled using scientific literature retrieved from such databases as PubMed, Scopus, ScienceDirect, Google Scholar, and PubMed Central. Relevant articles published in the English language until December 2020 were taken into consideration. It has been revealed that specific host miRNAs induced by Mycobacterium tuberculosis can target diverse factors and pathways in immune signaling to ensure longer pathogen survival inside the phagocytes. The potential use of miRNAs in tuberculosis diagnosis or therapeutic strategies has been attracting increasing attention in recent years. However, despite considerable efforts devoted to miRNA profiling, further studies are needed to elucidate the full potential of miRNAs as novel tuberculosis biomarkers or therapeutic targets.
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Objective: To elucidate the cytotoxic effect of the secondary metabolites of Barrientosiimonas humi (B. humi) on MCF-7 and MDA-MB-231 human breast cancer cells and its underlying mechanisms of action. Methods: The extract was obtained from the fermentation of B. humi and fractionation of the crude extract was conducted via column chromatography. Cytotoxicity of the B. humi extract was determined by using MTT assay and real-time cellular analysis. Morphological changes, cell cycle profiles, mode of cell death, and caspase expressions of control and treated breast cancer cells were determined. Results: The ethyl acetate extract isolated from B. humi was cytotoxic against MCF-7 and MDA-MB-231 cell lines. One of the dichloromethane (DCM) fractions, designated as DCM-F2, exhibited the strongest activity among all the fractions and thereby was selected for further studies. DCM-F2 had selective cytotoxicity on target cells by inducing apoptosis, particularly in the early stage, and cell cycle arrest. Treated cells caused inhibition of cell cycle progression at 72 h leading to a significant increase (P < 0.05) in the G0/G1 population. DCM-F2 treated MDA-MB-231 cells showed caspase-dependent apoptosis, whereas DCM-F2 treated MCF-7 cells showed a caspase-independent apoptosis pathway. Five compounds were successfully isolated from B. humi. Cyclo (Pro-Tyr) was the most cytotoxic and selective compound against MCF-7 cells. Conclusions: B. humi ethyl acetate extract exhibits significant cytotoxicity against MCF-7 and MDA-MB-231 cells via induction of apoptosis and cell cycle arrest.
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Objective: To explore the protective role of Glinus lotoides ethanolic extract in a depression model through modulating oxidant/antioxidant enzyme system and inflammatory status. Methods: Phytochemical constituents of Glinus lotoides ethanolic extract were evaluated qualitatively and quantitatively along with HPLC. Rats were divided into six groups. The normal control and the intoxicated groups received normal saline, and the standard group received imipramine, while the remaining groups received 100, 300, and 500 mg/kg Glinus lotoides ethanolic extract. All groups received treatments for 14 d. Lipopolysaccharides (LPS) were then administered i.p. (0.83 mg/kg) to all groups except the normal control group. After 24 h, anxiety and depression-like behaviors were evaluated by performing behavioral analysis (open field, tail suspension, forced swim, sucrose preference test), and determining total oxidant status, total antioxidant capacity, catalase, and biochemical parameters [malondialdehyde, glutathione, superoxide dismutase, tumor necrosis factor (TNF)-alpha and interleukin (IL)-6]. Results: Phytochemical studies confirmed the presence of phenols and flavonoids and HPLC analysis showed the presence of gallic acid, quercetin, chlorogenic, and caffeic acid. Total oxidant status was significantly decreased, while total antioxidant capacity was significantly increased in the Glinus lotoides ethanolic extract treated groups. Moreover, Glinus lotoides ethanolic extract diminished malondialdehyde, IL-6, and TNF-alpha levels, while increasing superoxide dismutase, catalase, and glutathione activities. Conclusions: Glinus lotoides ethanolic crude extract shows significant antidepressant activity by modulating oxidative and biochemical parameters that supports its folkloric use in traditional systems of medicine.
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Objective: To assess the anti-tumor effects of Pistacia atlantica methanolic extract (PAME) compared with cyclophosphamide against Ehrlich solid tumors in mice. Methods: Swiss albino mice (n=40) were divided into five groups: normal control mice, mice with Ehrlich solid tumors treated with normal saline, mice with Ehrlich solid tumors treated with cyclophosphamide intraperitoneally once a day for 14 d, or 50 mg/kg or 100 mg/kg PAME orally once a day for 14 d. Tumor growth inhibition, body weight, tumor markers, liver and kidney enzymes, oxidative stress markers, antioxidant enzymes, tumor necrosis factor-alpha level (TNF-α), and apoptosis-regulatory gene expression were evaluated. Results: Treatment of mice bearing Ehrlich solid tumors with PAME at 50 and 100 mg/kg orally significantly decreased tumor volume, body weight, tumor markers, liver and kidney enzymes, oxidative stress markers and TNF-α level in comparison with mice with Ehrlich solid tumors receiving normal saline. whereas PAME at 50 and 100 mg/kg/day significantly elevated the level of antioxidant enzymes (P<0.05). Conclusions: Pistacia atlantica methanolic extract has potent antitumor activity in mice. Therefore, the extract might be considered as an alternative anticancer agent against tumors, however, additional studies especially in the clinical setting are required to confirm this finding.