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1.
Braz. j. biol ; 83: e248746, 2023. graf
Article in English | MEDLINE, LILACS, VETINDEX | ID: biblio-1339351

ABSTRACT

Abstract Colorectal cancer (CRC) is one of the most common cancers leading to comorbidities and mortalities globally. The rational of current study was to evaluate the combined epigallocatechin gallate and quercetin as a potent antitumor agent as commentary agent for therapeutic protocol. The present study investigated the effect of epigallocatechin Gallate (EGCG) (150mg) and quercetin (200mg) at different proportions on proliferation and induction of apoptosis in human colon cancer cells (HCT-116). Cell growth, colonogenic, Annexin V in addition cell cycle were detected in response to phytomolecules. Data obtained showed that, the colony formation was inhibited significantly in CRC starting from the lowest concentration tested of 10 µg/mL resulting in no colonies as visualized by a phase-contrast microscope. Data showed a significant elevation in the annexin V at 100 µg/mL EGCG(25.85%) and 150 µg/mL quercetin (48.35%). Moreover, cell cycle analysis showed that this combination caused cell cycle arrest at the G1 phase at concentration of 100 µg/mL (72.7%) and 150 µg/mL (75.25%). The combined effect of epigallocatechin Gallate and quercetin exert antiproliferative activity against CRC, it is promising in alternative conventional chemotherapeutic agent.


Resumo O câncer colorretal (CCR) é um dos cânceres mais comuns, levando a comorbidades e mortalidade em todo o mundo. O racional do presente estudo foi avaliar a combinação de galato de epigalocatequina e quercetina como um agente antitumoral potente como agente de comentário para protocolo terapêutico. O presente estudo investigou o efeito de galato de epigalocatequina (EGCG) (150 mg) e quercetina (200 mg) em diferentes proporções na proliferação e indução de apoptose em células de câncer de cólon humano (HCT-116). O crescimento celular, colonogênico, anexina V, além do ciclo celular foram detectados em resposta a fitomoléculas. Os dados obtidos mostraram que a formação de colônias foi inibida significativamente no CRC a partir da concentração mais baixa testada de 10 µg/mL, resultando em nenhuma colônia conforme visualizado por um microscópio de contraste de fase. Os dados mostraram uma elevação significativa na anexina V a 100 µg/mL de EGCG (25,85%) e 150 µg/mL de quercetina (48,35%). Além disso, a análise do ciclo celular mostrou que essa combinação causou parada do ciclo celular na fase G1 na concentração de 100 µg/mL (72,7%) e 150 µg/mL (75,25%). O efeito combinado da epigalocatequina galato e quercetina exerce atividade antiproliferativa contra o CCR, é promissor como agente quimioterápico alternativo convencional.


Subject(s)
Humans , Colorectal Neoplasms/drug therapy , Catechin/analogs & derivatives , Catechin/pharmacology , Quercetin/pharmacology , Cell Cycle , Annexin A5 , Cell Line, Tumor , Cell Proliferation
2.
Acta sci., Health sci ; 44: e55845, Jan. 14, 2022.
Article in English | LILACS-Express | LILACS | ID: biblio-1366721

ABSTRACT

The effects of the aqueous extract of Ilex paraguariensis (Ip)and the flavonoid quercetin were tested during the induction of in vivomyocardial ischemia/ reperfusion in Rattus norvegicus. The antioxidant power of the extract and quercetin were chemically determined. The experimental groups were: control, ischemia/reperfusion induction, Iporal treatment, Iporal treatment and ischemia /reperfusion, quercetin oral treatment, and quercetin oral treatment and ischemia/reperfusion. Rats were anesthetized with sodium thiopental and xylazine via intraperitoneal injection and subsequently underwent 15 minutes of ischemia followed by 15 minutes of reperfusion. Ischemia was promoted by tying the left anterior descending coronary artery. Areas of risk and infarction were stained by intravenous Evans blue and triphenyl tetrazolium chloride. Reactive oxygen species (ROS), antioxidant capacity against peroxylradicals, and lipid peroxidation of the myocardium were quantified. A significant reduction in areas of risk and infarction was detected in the ischemic myocardium treated with Ipand quercetin; ROS generation and lipid peroxidation were significantly reduced, and the antioxidant capacity was elevated. Oral administration of Ippromoted antioxidant benefits in the myocardium during ischemia and reperfusion, which reduced infarction. We suggest that Mate (a hot drink made from steeped dried leaves of Ip) consumption is a potential cardioprotective habit of indigenous people from southern South American countries, which must be better understood scientifically and ethnographically.

3.
Int. braz. j. urol ; 47(4): 796-802, Jul.-Aug. 2021. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1286776

ABSTRACT

ABSTRACT Purpose: To quantitatively evaluate the possible long-term protective effects of quercetin during renal warm ischemia. Materials and Methods: Male rats were allocated into 4 groups: sham (S), sham quercetin (SQ), ischemia (I), and ischemia quercetin (IQ). Groups SQ and IQ received quercetin (50mg/kg) before and after surgery. Groups I and IQ had their left renal vessels clamped for 60 minutes. All animals were euthanized four weeks after the procedure, and serum urea and creatinine levels were measured. Renal weight and volume, cortex-non-cortex area ratio (C-NC), cortical volume (CV), glomerular volumetric density (Vv[glom]), volume-weighted glomerular volume (VWGV) and number of glomeruli per kidney (N[glom]) were evaluated by stereological methods. Results were considered statistically significant when p <0.05. Results: Serum urea levels in group I increased by 10.4% in relation to group S, but no differences were observed among the other groups. The C-NC of group I was lower than those of all other groups, and group IQ had similar results to sham groups. The Vv[glom] and N[glom] of group I were lower than those of group S (33.7% and 28.3%, respectively) and group IQ had no significant difference compared to the S group. Conclusions: Quercetin was effective as a nephroprotective agent in preventing the glomerular loss observed when the kidney was subjected to warm ischemia. This suggests that this flavonoid may be used preventively in kidney surgery, when warm ischemia is necessary, such as partial nephrectomy.

4.
Rev. ciênc. farm. básica apl ; 42: 1-13, 20210101.
Article in English | LILACS-Express | LILACS | ID: biblio-1177732

ABSTRACT

Introduction: The exacerbated generation of advanced glycation end products (AGEs) triggers the onset of diabetic complications associated with hyperglycemia. The search for natural bioactive compounds that can inhibit AGE formation has gained immense interest. Quercetin and its glycoside derivative, rutin, are powerful antioxidants. They have been studied due to their potential to mitigate the disturbances observed in diabetes; however, studies comparing their antiglycation effects are limited. The aim of the present study was to compare the in vitro antiglycation potentials of quercetin and rutin. Methods: The in vitro model system of protein glycation was applied using bovine serum albumin (10 mg/mL) incubated with glucose (0.5 M) in the absence or presence of aminoguanidine (1 mM, prototype anti-AGE agent), metformin (1 mM), quercetin (100, 50, or 12.5 µM), or rutin (100, 50, or 12.5 µM). Before initiating incubations (day 0) and after 10, 20, and 30 days, aliquots were assayed for fluorescent AGEs. Markers of amino acid oxidation (dityrosine, N'-formylkynurenine, kynurenine), protein carbonyl groups (PCO), and protein crosslink formation were assessed after 30 days. Results: Both quercetin and rutin inhibited the formation of AGEs and decreased the PCO levels in a concentration-dependent manner, and moreover, the effect of rutin was more prominent than that of quercetin. Quercetin and rutin also decreased the formation of amino acid oxidation products and protein crosslinks; the best effects were observed in incubations with rutin. Conclusion: Rutin exhibited the most potent antiglycation and antioxidant activities, which may be attributed to the minor occurrence of interactions between albumin and rutin, making rutinnoside more available to exert its effects.

5.
Tropical Biomedicine ; : 360-365, 2021.
Article in English | WPRIM | ID: wpr-905802

ABSTRACT

@#COVID-19, caused by the SARS-CoV-2 virus, can lead to massive inflammation in the gastrointestinal tract causing severe clinical symptoms. SARS-CoV-2 infects lungs after binding its spike proteins with alveolar angiotensin-converting enzyme 2 (ACE2), and it also triggers inflammation in the gastrointestinal tract. SARS-CoV-2 invades the gastrointestinal tract by interacting with Toll-like receptor-4 (TLR4) that induces the expression of ACE2. The influx of ACE2 facilitates cellular binding of more SARS-CoV-2 and causes massive gastrointestinal inflammation leading to diarrhea. Diarrhea prior to COVID-19 infection or COVID-19-induced diarrhea reportedly ends up in a poor prognosis for the patient. Flavonoids are part of traditional remedies for gastrointestinal disorders. Preclinical studies show that flavonoids can prevent infectious diarrhea. Recent studies show flavonoids can inhibit the multiplication of SARS-CoV-2. In combination with vitamin D, flavonoids possibly activate nuclear factor erythroid-derived-2-related factor 2 that downregulates ACE2 expression in cells. We suggest that flavonoids have the potential to prevent SARS-CoV-2 induced diarrhea.

6.
Article in Chinese | WPRIM | ID: wpr-907631

ABSTRACT

Objective:To compare the content change of 6 constituents in Plantaginis Semen from different habitats before and after salt processing. Methods:HPLC method was used to quantitatively analyze 6 ingredients in Plantaginis Semen and processed with salt including geniposidic acid, plantagoguanidinic acid, quercetin, kaempferol, verbascoside and isoverbascoside. Results:The geniposidic acid, plantagoguanidinic acid, quercetin, kaempferol, verbascoside and isoverbascoside were well separated. The linear ranges of which were 0.259 2-3.628 8 μg ( r=0.999 8), 0.054 3-0.760 5 μg ( r=0.999 6), 0.030 0-0.420 6 μg ( r=0.999 4), 0.055 6- 0.777 8 μg ( r=0.999 5), 0.287 0-4.018 0 μg ( r=0.999 8), 0.033 1-0.463 1 μg ( r=0.999 7), respectively. Average recovery rates were 98.68%, 98.46%, 98.87%, 98.99%, 98.34%, 98.75% ( n=6), respectively. There were mild differences in the contents of 6 ingredients of 8 batches of Plantaginis Semen from 5 different habitats. There were no obvious differences between the raw products and the products after salt process in Plantaginis Semen. The content of flavonoids, geniposidic acid and isoverbascoside in Plantaginis Semen were significantly increased after salt process, while the content of verbascoside was reduced. Conclusion:HPLC method to quantitatively analyze the 6 constituents in Plantaginis Semen before and after salt process could provided a reference for the quality change and the material basis for the efficacy of Plantaginis Semen before and after salt process.

7.
China Pharmacy ; (12): 2875-2879, 2021.
Article in Chinese | WPRIM | ID: wpr-906654

ABSTRACT

OBJECTIVE:To study the reversal effect of quercetin on human cervical squamous carcinoma cisplatin-resistant cell line SiHa/DDP. METHODS :The drug resistance index of cisplatin to SiHa/DDP cells ,and the reversal resistance multiple of quercetin to SiHa/DDP cells were determined. The effects of quercetin (0.005 μg/mL),cisplatin(2.5 μg/mL),cisplatin combined with quercetin (2.5 μg/mL cisplatin+0.005 μg/mL quercetin),quercetin combined with pathway inhibitor(0.005 μg/mL quercetin+ 20 nmol/L rapamycin )on the apoptotic rate of SiHa/DDP cells were investigated ,as well as its effects on the expression of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt)/mammalian rapamycin target protein (mTOR) signaling pathway related proteins (PI3K,Akt,mTOR,P-gp,p70S6K). RESULTS :The resistance index of cisplatin to SiHa/DDP cells was 5.19, and reversal resistance multiple of quercetin to SiHa/DDP cells was 4.00. Compared with cisplatin alone and quercetin alone , cisplatin combined with quercetin ,quercetin combined with rapamycin could significantly increase the apoptotic rate of SiHa/DDP cells(P<0.05),while decreased the phosphorylation of Akt ,mTOR and p 70S6K protein as well as the expression of P-gp protein (P<0.05). CONCLUSIONS :Quercetin can effectively reverse drug resistance of SiHa/DDP cells to cisplatin ,which may be associated with inhibiting the expression of the protein related to PI 3K/Akt/mTOR signaling pathway.

8.
China Pharmacy ; (12): 2839-2845, 2021.
Article in Chinese | WPRIM | ID: wpr-906649

ABSTRACT

OBJECTIVE:To in vestigate the effects of quercetin (Que)on the expressio n of angiotensin Ⅱ(AngⅡ)-induced myocardial contractile proteins of primary rats through angiotensin-converting enzyme 2-angiotensin-(1-7)-Mas (ACE2-Ang- (1-7)-Mas)axis. METHODS :Cardiac tissue of rats aged 1-2 d were collected ,and primary cardiomyocytes were isolated and cultured. The gene silencing model of cardiomyocytes ACE2 was constructed. Experiments were divided into 12 groups. Among them,AngⅡ group,AngⅡ+ small interference RNA (siRNA)group,and Ang Ⅱ+ A 779 group were the model groups ;AngⅡ+ losartan group was positive control group ;AngⅡ+Que40 group,AngⅡ+Que80 group,AngⅡ+siRNA+Que40 group,AngⅡ+ siRNA+Que80 group,AngⅡ+A779+Que40 group and Ang Ⅱ+A779+Que80 group were the experimental groups ;blank group and siRNA group were set up. Ang Ⅱ concentration was 1×10-6 mol/L;siRNA final concentration was 50 nmol/L;Que concentration was 40 and 80 μmol/L;A779(Mas receptor inhibitor )concentration was 1 μmol/L;losartan concentration was 1×10-4 mol/L. mRNA and protein expression of ACE 2,Ang-(1-7) and Mas in primary cardiomyocytes were detected ;the expressions of myocardial contractile proteins were also determined ,such as Na +/Ca2+ exchange channel (NCX),calcium pump (SERCA2a), phosphoprotein (PLB). RESULTS :Compared with Ang Ⅱ group,mRNA expression of Mas was increased significantly in Ang Ⅱ + Que 80 group (P<0.05);mRNA expression of ACE2 and Mas were increased significantly in Ang Ⅱ + CZ0210-01) losartan group (P<0.05). Compared with Ang Ⅱ group,the 851136165@qq.com protein expression of ACE 2 and Ang- (1-7) were increased significantly in Ang Ⅱ+ Que 40 group(P<0.05);compared with Ang Ⅱ + siRNA group ,the protein expression of Ang-(1-7)were increased significantly in Ang Ⅱ+ siRNA+Que 40 group(P<0.05);compared with Ang Ⅱ+A779 group,the protein expression of Ang- (1-7)were increased significantly in Ang Ⅱ+A779+ Que 40 group(P<0.05). Compared with Ang Ⅱ group,the protein expression of NCX was decreased in Ang Ⅱ+Que40 group(P<0.05),protein expression of NCX was reduced in Ang Ⅱ+ losartan group (P<0.05);compared with Ang Ⅱ+A779 group,the protein expression of NCX was decreased in Ang Ⅱ+A779+ Que80 group (P<0.05). CONCLUSIONS :Que improves the expression of Ang Ⅱ -induced ACE 2-Ang-(1-7)-Mas axis in cardiomyocyte model to some extent ,so as to regulate myocardial contractile protein.

9.
Article in Chinese | WPRIM | ID: wpr-906376

ABSTRACT

Objective:To predict the therapeutic targets and related signaling pathways of quercetin in the treatment of heart failure (HF) by network pharmacology and molecular docking methods,and further clarify its mechanisms through <italic>in vitro</italic> cell model. Method:The pharmacological targets of quercetin were obtained by SwissTargetPrediction and Targetnet databases; the heart failure related targets were obtained by Online Mendelian Inheritance in Man(OMIM),GeneCards and Therapeutic Target Database(TTD) databases; the protein-protein interaction(PPI) network was analyzed by STRING database(Search Tool for Recurring Instances of Neighbouring Genes),and the PPI network diagram of quercetin for heart failure target was established. Cytoscape 3.7.2 software was used for analyzing and screening the anti-heart failure network nodes of quercetin,and the obtained targets were enriched with gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis by DAVID database. In order to explore the mechanism of quercetin in the treatment of heart failure,we used cell model to verify the function in heart failure treatment. Results:The predicted results showed that there were 23 targets for the treatment of heart failure,such as Matrix Metallopeptidase-9(MMP-9),androgen receptor(AR),coagulation factor 2(F2),insulin like growth factor 1 receptor(IGF1R),epidermal growth factor receptor(EGFR),janus kinase-2(JAK2),cytochrome P450 family 19 subfamily A member 1(CYP19A1),estrogen receptor-1(ESR1),tumor necrosis factor(TNF),protein tyrosine phosphatase receptor type C(PTPRC) and cytochrome P450 family 17 subfamily A member 1(CYP17A1) etc. The results suggest that quercetin may play a role in the treatment of heart failure by intervening in the physiological processes of cardiovascular cell proliferation and metabolism,regulating hypoxia-inducible factor 1 (HIF-1)signaling pathway and steroid hormone biosynthesis. Conclusion:Quercetin has the characteristics of multi-target,multi-channel and multi-channel in the treatment of heart failure. It may play a role in the treatment of heart failure by regulating MMP-9,EGFR and other key genes,participating in the biological process of cardiac and vascular cell proliferation and metabolism.

10.
Article in Chinese | WPRIM | ID: wpr-906375

ABSTRACT

Objective:To screen the active components of sovereign medicinal Achyranthis Bidentatae Radix in Rongjin Niantong formula based on bioinformatics and network pharmacology and observe their effects on therapeutic targets of osteoarthritis (OA) in <italic>in vivo</italic> and <italic>in vitro</italic> animal experiments. Method:The main active components and therapeutic targets of Achyranthis Bidentatae Radix were retrieved from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), and the differentially expressed genes relevant to OA from the Gene Expression Omnibus (GEO) database for cross analysis. The effects of main active components in Achyranthis Bidentatae Radix on enriched therapeutic targets of rats with OA <italic>in vivo </italic>and <italic>in vitro</italic> were detected by real-time polymerase chain reaction (Real-time PCR) and Western blot. Result:There were 20 active components for Achyranthis Bidentatae Radix against OA, with quercetin being an important one. Among the three target genes, osteopontin (OPN) and plasminogen activator inhibitor-1(PAI-1) were the key ones in the network. Gene Ontology (GO) analysis yielded 227 related terms, involving the regulation of physiological response to trauma (GO: 1903034), negative regulation of trauma response (GO: 1903035), etc. Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis revealed 12 related pathways, involving extracellular matrix receptor interaction (hsa04512) and so on. In animal experiments, compared with the normal group, the model group exhibited increased gene and protein expression of OPN and PAI-1. Compared with the model group, the quercetin group displayed decreased gene and protein expression of OPN and PAI-1 (<italic>P</italic><0.05). In cell experiments, the OPN and PAI-1 protein expression levels in the model group were increased as compared with those in the normal group, while the Collagen Ⅱ protein expression was decreased. The OPN and PAI-1 protein expression levels in the quercetin group and the inhibitor group were down-regulated in contrast to those in the model group, whereas the Collagen Ⅱ protein expression levels were up-regulated significantly (<italic>P<</italic>0.05). Conclusion:Achyranthis Bidentatae Radix<italic> </italic>inhibits cartilage degeneration and exerts the preventive and therapeutic effects against OA, which is possibly due to the efficacy of its active component quercetin in down-regulating the expression of OPN and PAI-1 in chondrocytes and up-regulating the Collagen Ⅱ protein expression.

11.
Article in Chinese | WPRIM | ID: wpr-906292

ABSTRACT

Rheumatoid arthritis (RA) is a chronic and systemic autoimmune disease with aggressive and symmetrical polyarthritis as the main clinical manifestations. The exact pathogenesis is unknown. Its basic pathological changes include chronic inflammation of the joint synovium, increased joint cavity effusion, pannus formation, gradual cartilage damage and bone erosion, eventually leading to joint deformity and loss of function. It has been found that the onset and development of RA are related to heredity, environment and other factors. The drugs for RA mainly include non-steroidal anti-inflammatory drugs (NSAIDs), corticosteroids, disease-modifying anti-rheumatic drugs (DMARDs) and biological agents. However, long-term use of these drugs can cause a variety of side effects and adverse reactions, such as myocardial infarction, peptic ulcer, poor wound healing, and liver and kidney dysfunction. In addition, natural medicines have a good application prospect because of their various pharmacological activities and few side effects. Quercetin is a flavonoid found in Morus alba and tetrandrine, with diverse pharmacological activities, including cardiovascular diseases, joint movement, tumor immunology and so on. Not only have the clinical trials shown good efficacy of quercetin, but the experimental studies have also proven that quercetin can improve RA by reducing inflammatory response, inhibiting the formation of synovial pannus, synovial hyperplasia, neutrophil NETs formation, osteoclast function, regulating Th17/Treg balance and other mechanism. In this article, we will briefly summarize the regulatory mechanism of quercetin and discuss the complexed effect of quercetin on rheumatoid arthritis.

12.
Article in Chinese | WPRIM | ID: wpr-906282

ABSTRACT

Objective:To explore the molecular mechanism of Jiangtang Xiaozhi tablets (JTXZT) in the treatment of non-alcoholic fatty liver disease (NAFLD) by means of network pharmacology and molecular docking. Method:With the help of traditional Chinese medicine (TCM) Systems Pharmacology Database and Analysis Platform (TCMSP), TCMs Integrated Database (TCMID), Encyclopedia of TCM (ETCM) and Bioinformatics Analysis Tool for Molecular Mechanism of TCM (BATMAN-TCM), the chemical compositions of medicinal materials in JTXZT were obtained, the compound targets were predicted in SwissTargetPrediction database and STITCH database. The targets of NAFLD were searched by The Human Gene Database (GeneCards), Online Mendelian Inheritance in Man (OMIM), Therapeutic Target Database (TTD) and DisGeNET, and intersection analysis was performed with the targets of the active ingredients to obtain the targets of JTXZT for treatment of NAFLD. Based on STRING 11.0 database, the protein-protein interaction (PPI) network of therapeutic targets was constructed, and the enrichment analysis of therapeutic targets was carried out by DAVID 6.8. Finally, the interaction characteristics of key components and core therapeutic targets of JTXZT for treatment of NAFLD were verified based on molecular docking. Result:The key components of JTXZT for treatment of NAFLD were quercetin, luteolin, kaempferol, berberine, isorhamnetin, betulinic acid, oleanolic acid, ursolic acid. formononetin and hexitol, and the core targets of JTXZT for treatment of NAFLD were mitogen-activated protein kinase 1 (MAPK1), Jun proto-oncogene, activator protein-1 (AP-1) transcription factor subunit (JUN), MAPK3, protein kinase B1 (AKT1 or Akt1), tumor protein p53 (TP53), E1A binding protein p300 (EP300), Fos proto-oncogene, AP-1 transcription factor subunit (FOS), tumor necrosis factor (TNF),amyloid beta precursor protein (APP) and cytochrome P450 family 2 subfamily E member 1 (CYP2E1). Biological function and pathway enrichment analysis showed that JTXZT mainly through xenobiotic metabolic process, oxidation-reduction process, cholesterol metabolic process and other biological processes, regulating phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) signaling pathway, MAPK signaling pathway, NAFLD and insulin signaling pathway to play a role in the treatment of NAFLD. The results of molecular docking showed that the active components of JTXZT had a good affinity with the core targets of JTXZT for the treatment of NAFLD. Conclusion:JTXZT treats NAFLD through multiple active components, multiple key targets and multiple action pathways.

13.
Article in Chinese | WPRIM | ID: wpr-906126

ABSTRACT

Objective:To investigate the protective effect of quercetin (Qu) on articular cartilage of knee osteoarthritis and its mechanism by inhibiting p38 mitogen activated protein kinase (MAPK) signaling pathway. Method:Through the network pharmacology technology,we scientifically predicted and analyzed the target factors and signal pathways of Qu in the protection of articular cartilage in patients with osteoarthritis. We selected a prediction pathway closely related to osteoarthritis and validated it by cell experiment <italic>in vitro</italic>. The best intervention concentration of the drug was selected by cell counting kit-8 (CCK-8) method. The osteoarthritis and its closely related inflammatory factors interleukin(IL)-1<italic>β</italic> and tumor necrosis factor(TNF)-<italic>α</italic> were detected by enzyme linked immunosorbent assay(ELISA). The expression of related mRNA and protein in p38 signal pathway after Qu intervention were detected by quantitative real time polymerase chain reaction(Real-time PCR) and Western blot. Result:It was predicted that MAPK signal pathway was closely related to osteoarthritis by network pharmacology,and p38 MAPK pathway,which was most closely related to osteoarthritis,was selected for study. The results showed that 100 μmol·L<sup>-1</sup> Qu had the most obvious effect in decreasing the expression of related inflammatory factors,inhibited the expression of p38,phosphorylated(p)-p38,matrix metalloproteinase-13(MMP-13),A disintegrin-like and metalloproteinase with thrombospondin type-1 motifs-4(ADAMTS-4) in the pathway,and promoted the expression of CollagenⅡ. Conclusion:Qu could decrease the expression of cartilage inflammatory factors in the prevention and treatment of osteoarthritis,and the effect can be well developed by intervening and inhibiting p38 MAPK pathway related factor expression level. All the results show that Qu can decrease osteoarthritis inflammatory factors and protect articular cartilage in patients with osteoarthritis.

14.
Article in Chinese | WPRIM | ID: wpr-921661

ABSTRACT

Quercetin is a naturally occurring phytochemical with good bioactivity, which mainly exists in the form of glycoside in vegetables, fruits, tea, and wine and exhibits beneficial health effects. Quercetin is a dietary polyphenol that exerts the protective effects through diet or use as a food supplement. Compared with chemical agents, quercetin is widely available and safe. Quercetin has been extensively studied for its anti-diabetic, anti-hypertensive, anti-Alzheimer's disease, anti-arthritic, anti-influenza virus, anti-microbial infection, anti-aging, autophagy-regulating, and cardiovascular protective effects. Studies on its activities against different can-cer cell lines have also been reported recently. However, the poor water solubility, rapid in vivo metabolism, and short half-life of quercetin have led to its low bioavailability, thus limiting its application in the field of medicine. Quercetin nanoparticles and nanoparticle drug delivery system have been effectively utilized for enhancing its bioavailability. This paper reviewed the therapeutic potential of quercetin from both preclinical and clinical aspects and proposed solutions to improve its bioavailability, so as to provide a reference for the therapeutic application of natural compounds in the field of medicine.


Subject(s)
Biological Availability , Drug Delivery Systems , Nanoparticles , Quercetin , Solubility
15.
Article in Chinese | WPRIM | ID: wpr-888176

ABSTRACT

Leaves of Euryale ferox are rich in anthocyanins. Anthocyanin synthesis is one of the important branches of the flavonoid synthesis pathway, in which flavonoid 3'-hydroxylase(F3'H) can participate in the formation of important intermediate products of anthocyanin synthesis. According to the data of E. ferox transcriptome, F3'H cDNA sequence was cloned in the leaves of E. ferox and named as EfF3'H. The correlation between EfF3'H gene expression and synthesis of flavonoids was analyzed by a series of bioinforma-tics tools and qRT-PCR. Moreover, the biological function of EfF3'H was verified by the heterologous expression in yeast. Our results showed that EfF3'H comprised a 1 566 bp open reading frame which encoded a hydrophilic transmembrane protein composed of 521 amino acid residues. It was predicted to be located in the plasma membrane. Combined with predictive analysis of conserved domains, this protein belongs to the cytochrome P450(CYP450) superfamily. The qRT-PCR results revealed that the expression level of EfF3'H was significantly different among different cultivars and was highly correlated with the content of related flavonoids in the leaves. Eukaryotic expression studies showed that EfF3'H protein had the biological activity of converting kaempferol to quercetin. In this study, EfF3'H cDNA was cloned from the leaves of E. ferox for the first time, and the biological function of the protein was verified. It provi-ded a scientific basis for further utilizing the leaves of E. ferox and laid a foundation for the further analysis of the biosynthesis pathway of flavonoids in medicinal plants.


Subject(s)
Anthocyanins , Cytochrome P-450 Enzyme System/metabolism , Plant Leaves/metabolism , Plant Proteins/metabolism , Transcriptome
16.
Chinese Journal of Biotechnology ; (12): 1900-1918, 2021.
Article in Chinese | WPRIM | ID: wpr-887771

ABSTRACT

Quercetin 3-O-glycosides (Q3Gs) are important members of quercetin glycosides with excellent pharmacological activities such as anti-oxidation, anti-inflammation, anti-cancer and anti-virus. Two representatives of Q3Gs, rutin and troxerutin, have been developed into clinical drugs, demonstrating Q3Gs have become one of the important sources of innovative drugs. However, the applications of Q3Gs in food and pharmaceutical industries are hampered by its poor bioavailability. Of the known means, selective acylation modification of Q3Gs through enzymatic catalysis to obtain Q3G esters is one of the effective ways to improve its bioavailability. Herein, the enzyme-mediated acylation of Q3Gs were reviewed in details, focusing on the four tool enzymes (acyltransferases, lipases, proteases and esterases) and the whole-cell mediated biotransformation, as well as the effect of acylations on the biological activities of Q3Gs. Furthermore, the highly efficient synthesis and diversification of acylated site for Q3G esters were also discussed. Taken together, this review provides a new perspective for further structural modifications of Q3Gs towards drug development.


Subject(s)
Acylation , Biological Availability , Glycosides , Quercetin , Rutin
17.
Article in Japanese | WPRIM | ID: wpr-887161

ABSTRACT

Dry solid matter (rutin content: 51.6 mg/g; quercetin content: 72.2 mg/g) extracted from Tartary buckwheat boiled noodles using 70% methanol as the solvent was found to have α-glucosidase inhibitory activity. As for fractions fractionated by silica gel column chromatography, the fractions rich in quercetin and rutin showed remarkable α-glucosidase inhibitory activity. Tartary buckwheat boiled noodles used as samples in this study contained quercetin produced from rutin by the action of rutinase, suggesting that both rutin and quercetin contained were involved in the α-glucosidase inhibitory activity of the dry solid extract. Changes in postprandial blood glucose levels were compared for boiled noodles made from two types of buckwheat (i.e., Tartary buckwheat and common buckwheat), revealing that blood glucose elevation after eating Tartary buckwheat boiled noodles was suppressed. The blood glucose level 40 minutes after eating Tartary buckwheat boiled noodles was significantly low (p<0.05). It can be concluded that this might be caused by the α-glucosidase inhibitory activity of rutin (270.0 mg) and quercetin (330.5 mg), which correspond to a total amount of 935 mg of rutin equivalents, in the gastrointestinal tract. As a result, the digestion of carbohydrates contained in the samples consumed and their absorption by the intestine might be inhibited, resulting in the suppression of increases in blood glucose levels. The presence of a certain amount of quercetin was considered to be key to the suppression of blood glucose elevation. It is important to control rapid postprandial blood glucose increases to prevent diabetes from developing or becoming serious. This study suggests the potential for Tartary buckwheat boiled noodles to contribute to diabetes prevention.

18.
Article in Chinese | WPRIM | ID: wpr-886881

ABSTRACT

Objective To establish quantitative methods to assay quercetin in Honghuixiang injection by HPLC. Methods Dikma C18 column(250 mm×4.6 mm, 5 μm) was used for the assay with acetonitrile −0.1% phosphoric acid (25∶75) as the mobile phase. Flow rate was 1.0 ml/min. The column temperature was 30 ℃. The detection wavelength was at 256 nm. Results Quercetin showed good linear relationship within the range of 0.2150–3.225 μg. The correlation coefficient was 0.999 6. The average recovery was 99.39% with RSD 0.82% (n=6). The repeatability was 1.194 mg/ml with RSD 0.40%. Conclusion The average quercetin content in three batches of Honghuixiang injection was 1.191 mg/ml. This method is simple, rapid and accurate. It can be used for the determination of quercetin in Honghuixiang injection.

19.
China Pharmacy ; (12): 1964-1968, 2021.
Article in Chinese | WPRIM | ID: wpr-886579

ABSTRACT

OBJECTIVE:To develop a method for simultaneous determination of 5 components in classical formula Huaihua san,including rutin ,naringin,neohesperidin,quercetin and pulegone. METHODS :HPLC wavelength switching method was adopted. The determination was performed on Cosmosil C 18 column with mobile phase consisted of acetonitrile- 0.05% phosphoric acid solution (gradient elution )at the flow rate of 1.0 mL/min. The detection wavelengths were set at 257 nm for rutin ,283 nm for naringin and neohesperidin ,254 nm for quercetin ,252 nm for pulegone ,respectively. The column temperature was set at 30 ℃, and sample size was 10 μL. RESULTS:The linear range was 21.7-2 170 μg/mL for rutin,46-4 600 μg/mL for naringin,22.3- 2 230 μg/mL for neohesperidin,0.96-96 μg/mL for quercetin,2.7-270 μg/mL for pulegone(all r>0.999),respectively. RSDs of precision,stability(24 h)and reproducibility tests were all lower than 2%(n=6). Average recoveries were 100.70%,99.31%, 101.10%,100.03% and 99.63%(all RSD <2%,n=9). Among 3 batches of Huaihua san samples ,the contents of above 5 components were 20.055-22.615,25.557-27.806,11.428-13.250,0.350-0.478,2.372-4.011 mg/g,respectively. CONCLUSIONS : Established method is simple ,accurate and reproducible ,and could be used for the simultaneous determination of 5 components in Huaihua san.

20.
Acta Pharmaceutica Sinica B ; (6): 978-988, 2021.
Article in English | WPRIM | ID: wpr-881179

ABSTRACT

In this study, self-discriminating hybrid nanocrystals was utilized to explore the biological fate of quercetin hybrid nanocrystals (QT-HNCs) with diameter around 280 nm (QT-HNCs-280) and 550 nm (QT-HNCs-550) following oral and intravenous administration and the contribution of integral nanocrystals to oral bioavailability enhancement of QT was estimated by comparing the absolute exposure of integral QT-HNCs and total QT in the liver. Results showed that QT-HNCs could reside

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