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Objective To develop a high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for simultaneous determination of five flavonoids in Ganmao’an granules (GMA). Methods Chromatographic separation was achieved on a Kromasil C18 Column (150 mm× 4.6 mm,5 μm,100 Å), which was eluted with methanol (A) -0.1% formic acid (B) at the flow rate of 1.0 ml/min. The gradient condition was as follows: 0-20 min, 35% A, and 20-40 min, 45% A. The column temperature was 25 °C. Analytes were detected using a triple quadrupole tandem mass spectrometer equipped with an electrospray ionization source in the negative ion scanning. The multiple reaction monitoring mode was used for qualitative analysis. For each flavonoid, two precursor ion/product ion transitions were chosen: lutin m/z 609.1→300.1, hyperin and isoquercitrin m/z 463.0→300.1, quercetin m/z 301.0→151.0, luteolin m/z 285.0→132.9. Results Five flavonoids showed the good relationships within their own concentration ranges (correlation coefficient r>0.999 1), whose average recoveries were in the range of 100.63%-102.81% with RSDs of 0.67%-2.07%. The content results of rutin, hyperoside, isoquercetin, quercetin, and luteolin in 10 batches of GMA were 32.23-479.83, 0.291-1.825, 11.44-20.54, 6.32-18.41, 3.46-6.51 μg/g, respectively. Conclusion The results indicated that the developed method was sensitive, accurate and could provide excellent specificity for simultaneous determination of five flavonoids in GMA. [ABSTRACT FROM AUTHOR]

This study explored the mitigating properties of hyperin (HYP) on renotoxicity induced by cadmium chloride (CdCl2). Four groups of seven male albino mice each were used in this experiment. Group 1 served as the control, receiving no treatment. Group 2 received daily oral gavage of CdCl2 at 0.3 mg/kg body weight for 28 d. Group 3 received both CdCl2 (0.3 mg/kg) and HYP (100 mg/kg) daily using the same administration method. Finally, Group 4 received only HYP (100 mg/kg) daily. Cd exposure significantly increased kidney dysfunction markers (blood urea nitrogen and creatinine) and oxidative stress (reactive oxygen species [ROS] and malondialdehyde [MDA]). Conversely, it decreased antioxidant enzyme activities (glutathione peroxidase (GPx] and catalase [CAT]) and glutathione (GSH) levels. Nuclear factor erythroid 2-related factor 2 (Nrf-2) and antioxidant gene expression decreased, while Kelch-like ECH-associated protein 1 expression increased. Additionally, Cd exposure increased inflammatory mediators (nuclear factor kappa B, tumor necrosis factor alpha [TNF-α], interleukin-1β [IL-1β], and cyclooxygenase-2) and apoptotic markers (Bax and caspase-3), alongside decreased Bcl-2 expression and renal tissue abnormalities. Mitochondrial dysfunction manifested with diminished activities of Krebs cycle and respiratory chain enzymes, and reduced mitochondrial membrane potential. Co-treatment with HYP significantly attenuated these detrimental effects through its anti-apoptotic, antioxidant, and anti-inflammatory properties. HYP co-treatment significantly attenuated CdCl2-induced renal damage in mice, suggesting its potential as a protective agent against Cd-induced kidney toxicity. [ABSTRACT FROM AUTHOR]

Background: A wide range of chronic diseases is associated with ROS-mediated oxidative stress. Quercetin glycoside (QG) is reported to be a powerful antioxidant with extremely high bioavailability and structural stability compared to quercetin aglycone. Hypothesis/Purpose: In this study, the antioxidant potential and cytoprotective effects of quercetin, and its glycosides isolated from Ephedra alata against oxidative damage induced by hydrogen peroxide in the cells of tetrahymena pyriformis (TEP) were evaluated and compared. Study design: Quercetin and its O-glycosides were isolated from Ephedra alata, and their chemical structures were elucidated using advanced spectroscopic techniques. The antioxidant and cytoprotective effects were evaluated using TEP cells exposed to hydrogen peroxide-induced oxidative stress. Methods: TEP cells were pretreated with quercetin aglycone (Q), isoquercetin (ISQ), or hyperin (HYP) before exposure to hydrogen peroxide (H2O2). Cell viability, lactate dehydrogenase (LDH) release, intracellular ROS levels, malondialdehyde (MDA levels, lipoperoxidation, antioxidant enzyme activity, and cleaved caspase-3 levels were measured. Results: ISQ pretreatment significantly enhanced cell survival and reduced H2O2-induced LDH release compared to Q. ISQ also decreased intracellular ROS levels, MDA levels, and lipoperoxidation, surpassing the effects of Q. Additionally, ISQ and HYP pretreatment notably increased antioxidant enzyme activity, outperforming Q. Furthermore, ISQ pretreatment significantly diminished cleaved caspase-3 levels compared to Q, indicating a potential role in preventing oxidative stress-induced apoptosis in TEP cells. Conclusion: Quercetin O-glycosides, particularly isoquercetin, from Ephedra alata exhibit superior antioxidant and cytoprotective effects compared to quercetin aglycone. These findings highlight the potential of these compounds as natural alternatives for mitigating oxidative damage and promoting cellular health. Future research should focus on elucidating the precise molecular pathways involved and evaluating their efficacy in animal models and clinical settings.

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Objective To explore the effect of hyperin on inflammatory reaction, wound healing and AMP-activated protein kinase (AMPK)/silent information regulator 1 (SIRT1) signaling pathway in diabetic foot ulcer (DFU) rats. Methods The DFU rat model was established, and 48 rats with successful DFU model were randomly divided into the model group, the hyperin low dose (100 mg/kg) group, the hyperin high dose (200 mg/kg) group and the metformin (200 mg/kg) group, with 12 rats in each group. Another 12 rats were taken as the control group. Rats of each group were given corresponding drug intervention, once a day for 4 weeks. Fasting blood glucose (FBG) levels of rats were detected by glucose meter after modeling (before administration) and after administration. Serum levels of interleukin (IL-6) and tumor necrosis factor-α (TNF-α) were detected by enzyme linked immunosorbent assay. The wound healing rate of rats was calculated by taking pictures. Hematoxylin-eosin staining was used to observe pathological changes of wound granulation tissue. Fluorescence quantitative PCR was used to detect mRNA expression levels of AMPK and SIRT1 in wound granulation tissue of rats. Western blot assay was used to detect protein expression levels of AMPK and SIRT1 in wound granulation tissue of rats. Results In the control group, the granulation tissue cells on the wound surface of rats were intact and orderly arranged, with less inflammatory cell infiltration. Compared with the control group, the necrosis of fibroblasts and capillaries in wound granulation tissue was severe, accompanied by a large number of inflammatory cell infiltration, and FBG,TNF-α and IL-6 levels in serum were significantly increased (P＜0.05). The wound healing rate, the mRNA and protein expression levels of AMPK and SIRT1 in wound granulation tissue were significantly decreased (P＜0.05). Compared with the model group, the lesion degree of wound granulation tissue was reduced in turn in the hyperin low dose group and the hyperin high dose group, and the FBG, serum levels of TNF-α and IL-6 were decreased in turn as well (P＜0.05). The wound healing rate, the mRNA and protein expression levels of AMPK and SIRT1 in wound granulation tissue were increased in turn (P＜0.05). There were no significant differences in pathological changes of the wound granulation tissue and other indicators between the metformin group and the hyperin high dose group (P＞0.05). Conclusion Hyperin can reduce inflammatory reaction and accelerate wound healing in DFU rats, and its mechanism may be related to the activation of AMPK/SIRT1 signal pathway. [ABSTRACT FROM AUTHOR]

Copyright of Food Research & Development is the property of Food Research & Development Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The proliferation of extravillous trophoblasts (EVT) and their further migration, invasion, and differentiation into the decidual and myometrial vasculature are vital for spiral artery remodeling. These physiological functions of EVT are also essential steps in the implantation of the human embryo and the formation of the placenta and are closely related to pregnancy maintenance and the occurrence of abortion. Hyperin is a flavonoid with anti-inflammatory, pro-proliferative, and anti-apoptotic properties. Consequently, we investigated the previously unexplored effects of hyperin on the proliferation, migration, and invasion of HTR-8/SVneo cells. Human extravillous trophoblast-derived HTR-8/SVneo cells were incubated with different concentrations of hyperin (0, 5, 10, 25, 50, and 100 μM) to observe the changes in cell proliferation, migration, invasive capacity, and pathway activation. Proliferation, migration, and invasion were promoted by activating the JAK1/STAT3 pathway in HTR-8/SVneo cells treated with hyperin. In addition, brepocitinib (PF-06700841) significantly inhibited the proliferation, migration, and invasion effects of hyperin on HTR-8/SVneo cells. In vivo experiments confirmed that hyperin reduces the embryo loss rate in recurrent spontaneous abortion (RSA) model mice. Furthermore, our study revealed that hyperin promoted the proliferation, migration, and invasion of HTR-8/SVneo cells via activation of the JAK1/STAT3 pathway, further improving pregnancy outcomes in RSA.

Depression is a global health problem with growing prevalence rates and serious impacts on the daily life of patients. However, the side effects of currently used antidepressants greatly reduce the compliance of patients. Quercetin is a flavonol present in fruits, vegetables, and Traditional Chinese medicine (TCM) that has been proved to have various pharmacological effects such as anti-depressant, anti-cancer, antibacterial, antioxidant, anti-inflammatory, and neuroprotective. This review summarizes the evidence for the pharmacological application of quercetin to treat depression. We clarified the mechanisms of quercetin regulating the levels of neurotransmitters, promoting the regeneration of hippocampal neurons, improving hypothalamic-pituitary-adrenal (HPA) axis dysfunction, and reducing inflammatory states and anti-oxidative stress. We also summarized the antidepressant effects of some quercetin glycoside derivatives to provide a reference for further research and clinical application. [ABSTRACT FROM AUTHOR]

Mao-Hua Ping Department of Rehabilitation Medicine, Hanyang Hospital Affiliated to Wuhan University of Science and Technology, Wuhan, Hubei Province 430050, People ’s Republic of ChinaCorrespondence: Mao-Hua PingDepartment of Rehabilitation Medicine, Hanyang Hospital Affiliated to Wuhan University of Science and Technology, Wuhan, Hubei Province 430050, People ’s Republic of ChinaEmail mao7737835815483@126.comBackground: Hyperin is an effective monomer extracted from Malvaceae plant Abelmoschus, which is a flavonol glycoside compound. Hyperin performs a variety of pharmacological activities, such as analgesia, antioxidation, anti-inflammation, avoiding microthrombosis, regulating immune function, inhibiting tumor cell growth. But the role of Hyperin on gastric cancer is unrevealed. Considering the essential role of Hyperin, Hyperin function in gastric cancer is necessary to explore.Aim: To identify the function of Hyperin in gastric cancer.Methods: The role of Hyperin on gastric cell progression was detected in our research. Proliferation, migration, and invasion ability were assessed by the CCK-8, colony formation, cell-cycle assay, wound healing, Transwell migration and invasion assays. TUNEL assay and flow cytometry showed the results of the apoptosis level. Further, caspase-3, -9 activity and apoptosis-associated protein were assessed by the Caspase activity kit and Western blot. Wnt/β-catenin signal pathway activity was appraised by TOP/FOP luciferase activity. Immunohistochemical staining was performed to detect the role of Hyperin on tumor growth in vivo.Results: Functional experiments showed that Hyperin inhibited proliferation, migration, and invasion and induced apoptosis in gastric cancer cells. Meanwhile, Hyperin prevented tumor growth by suppressing Wnt/β-catenin signal pathway.Conclusion: The present study revealed that Hyperin suppressed gastric cancer progression by controlling Wnt/β-catenin signal pathway, which provided a novel therapy in gastric cancer.Keywords: Hyperin, gastric cancer, Wnt, β-catenin

Depression is a global health problem with growing prevalence rates and serious impacts on the daily life of patients. However, the side effects of currently used antidepressants greatly reduce the compliance of patients. Quercetin is a flavonol present in fruits, vegetables, and Traditional Chinese medicine (TCM) that has been proved to have various pharmacological effects such as anti-depressant, anti-cancer, antibacterial, antioxidant, anti-inflammatory, and neuroprotective. This review summarizes the evidence for the pharmacological application of quercetin to treat depression. We clarified the mechanisms of quercetin regulating the levels of neurotransmitters, promoting the regeneration of hippocampal neurons, improving hypothalamic-pituitary-adrenal (HPA) axis dysfunction, and reducing inflammatory states and anti-oxidative stress. We also summarized the antidepressant effects of some quercetin glycoside derivatives to provide a reference for further research and clinical application.

Abstract Background Canarium patentinervium leaves are used by the local indigenous people of Malaysia for wound healing. The current study is undertaken to screen the comprehensive antibacterial activity of the leaves and barks extracts, fractions and isolated compounds from this plant. Bioassay guided fractionation was also undertaken to deeply evaluate the antibacterial activity of the water fraction of the leaves extract. This is to provide preliminary scientific evidence to the ethnopharmacology usage of this plant by investigating antibacterial properties of the plant and its isolated constituents. Methods Bio-assay guided fractionation and subsequent isolation of compounds using open column chromatography. The antibacterial activity against gram positive and gram negative ATCC strain and resistant clinical strains were evaluated using microtiter broth dilution method to determine minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and time-kill assay. The chemical structure of the isolated compounds from the water fraction of the ethanol extract of leaves was elucidated using Nuclear Magnetic Resonance (NMR). Results The ethanol extract of the leaves and barks showed antimicrobial activity against all four ATCC and eight clinical isolates. The ethanol extract of the leaves and the corresponding water fraction had good activity against MRSA S. aureus. (MIC: 250 μg/ml) and had bactericidal effect on eight of the clinical strains (MSSA,MRSA, oxacillin-resistant CONS, oxacillin-sensitive CONS, Enterococcus faecalis, Klebsiela species, Kleb pneumoniae ESBL and Candida parapsilosis). Further phytochemical investigation of the water fraction of the crude ethanol extract of leaves afforded compound 7 (hyperin) and compound 8 (cynaroside) that had bactericidal activity against tested bacterial species (MIC 50 μg/ml and 100 μg/ml). The two compounds were isolated from this genus for the first time. Conclusions These results may provide a rational support for the traditional use of Canarium patentinervium Miq. in infections and wound healing, since the antimicrobial compounds isolated were also present in the leaves extract.

Objectives: This study explored the mitigating properties of hyperin (HYP) on renotoxicity induced by cadmium chloride (CdCl 2 )., Methods: Four groups of seven male albino mice each were used in this experiment. Group 1 served as the control, receiving no treatment. Group 2 received daily oral gavage of CdCl 2 at 0.3 mg/kg body weight for 28 d. Group 3 received both CdCl 2 (0.3 mg/kg) and HYP (100 mg/kg) daily using the same administration method. Finally, Group 4 received only HYP (100 mg/kg) daily., Results: Cd exposure significantly increased kidney dysfunction markers (blood urea nitrogen and creatinine) and oxidative stress (reactive oxygen species [ROS] and malondialdehyde [MDA]). Conversely, it decreased antioxidant enzyme activities (glutathione peroxidase (GPx] and catalase [CAT]) and glutathione (GSH) levels. Nuclear factor erythroid 2-related factor 2 (Nrf-2) and antioxidant gene expression decreased, while Kelch-like ECH-associated protein 1 expression increased. Additionally, Cd exposure increased inflammatory mediators (nuclear factor kappa B, tumor necrosis factor alpha [TNF-α], interleukin-1β [IL-1β], and cyclooxygenase-2) and apoptotic markers (Bax and caspase-3), alongside decreased Bcl-2 expression and renal tissue abnormalities. Mitochondrial dysfunction manifested with diminished activities of Krebs cycle and respiratory chain enzymes, and reduced mitochondrial membrane potential. Co-treatment with HYP significantly attenuated these detrimental effects through its anti-apoptotic, antioxidant, and anti-inflammatory properties., Conclusion: HYP co-treatment significantly attenuated CdCl 2 -induced renal damage in mice, suggesting its potential as a protective agent against Cd-induced kidney toxicity.

We have explored the role of hyperin remodeling of airway smooth muscle cells during asthma. To this end, airway smooth muscle cells were isolated from tracheae and bronchi of mice, treated with transforming growth factor-ß1 and increasing concentrations of hyperin followed by analysis of cell viability, proliferation, and migration. The levels of extracellular matrix formation were evaluated by analysis of fibronectin and type I collagen. Western blot analysis was used to assess the function of the downstream pathway of nuclear factor-kappa B. Transforming growth factor-ß1 treatment led to a dose-dependent increase in type I collagen and fibronectin that was reversed by hyperin. Transforming growth factor-β1 promoted activation of nuclear factor-kappa B pathway with reduced IκBα and enhanced phospho (p)-p65 and p-IκBα. However, hyperin treatment upregulated IκBα and downregulated p-p65/p-IκBα to inactivate NF-κB pathway. In conclusion, hyperin ameliorates proliferation, migration, and extracellular matrix formation in airway smooth muscle cells by inhibiting transforming growth factor-β1-induced nuclear factor-kappa B activation suggesting potential prevention of airway remodeling during asthma. [ABSTRACT FROM AUTHOR]

[Objectives] To determine the content of hyperin and luteolin in Vernonia cinerea (L.) Less., and to provide basic experimental data for experimental research and clinical application of V. cinerea (L.) Less. [Methods] The components to be determined were extracted by ultrasonic extraction, and the hyperin and luteolin in V. cinerea (L.) Less, were separated and determined by reversed-phase high performance liquid chromatography (chromatographic conditions: reverse C18 column, methanol-0.4% phosphoric acid as mobile phase for gradient elution, flow rate of 1.0 ml/min, detector wavelength of 360 nm). [Results] The precision and repeatability of the experimental method were good, and the solution of V. cinerea (L.) Less, was stable within 18 h. There was a good linear relationship between the injection volume of hyperin and luteolin and the chromatographic peak area within the prescribed range, and the recovery rate was qualified. The content of hyperin and luteolin in V. cinerea (L.) Less, was 0.066 5 mg/g (n=3) and 0.1004 mg/g (n=3), respectively. [Conclusions] The experimental method is sensitive, specific, stable, accurate and reliable, and can be used for the determination of hyperin and luteolin in V. cinerea (L.) Less. [ABSTRACT FROM AUTHOR]

Objective To investigate the effect of hyperin on liver fibrosis in rats with heart failure,and to explore its molecular mechanism from the perspective of TGF-β1/Smad pathway and TIMP/MMP axis. Methods Twenty-four male Wistar rats were randomly divided into the Sham group,heart failure group,100 mg/kg hyperin group,and 200 mg/ kg hyperin group. Heart failure models were made by abdominal aorta-vena cava shunt in the heart failure group and hyperoside group,and abdominal organs were directly reset after Sham operation. Rats in the 100 mg/kg hyperin group and 200 mg/kg hyperin group were given 100 and 200 mg/kg hyperin, respectively. Rats in the Sham group and heart failure group were given the same volume of solvent,once a day, for 4 weeks. After administration,cardiac output(CO）and left ventricular ejection fraction(LVEF）were measured by small animal ultrasound system. Serum liver function indexes［alanine aminotransferase (ALT）and aspartate aminotransferase(AST)］were detected by ELISA. The body weight (BW）and liver weight (LW）of rats were weighed and the liver coefficient was calculated. Liver pathomorphology was observed by HE staining,and collagen formation area was measured by Masson staining. Oxidative stress indicators［hydroxyprolide (Hyp）,glutathione peroxidase(GSH-Px）,malondialdehyde(MDA）,and total superoxide dismutase(T-SOD)］of liver tissues were detected by alkaline hydrolysis,colorimetry,thiobarbituric acid and hydroxylamine methods,respectively. Transforming growth factor-β1(TGF-β1）/Smad pathway-related genes［transforming growth factor β1(TGF-β1）,and connective tissue growth factor(CTGF） mRNA］ and TIMP/MMP axis-related genes［TIMP1,matrix metalloproteinase 1 (MMP1）,MMP2,and collagen Ⅲ］were detected by real-time PCR；the expression levels of TGF- β1, Smad2/3,p- Smad2/3,CTGF,TIMP1,MMP1,MMP2 and collagenⅢ were detected by Western blotting. Results Compared with the Sham group,CO,LVEF,+dp/dtmax and -dp/dtmax decreased,LVESP,LVEDP,and LVESV increased in the heart failure group(all P<0. 01）. Compared with the heart failure group, LVESP,LVEDP,and LVESV in the 100 mg/kg hyperin group decreased(all P<0. 01). Compared with the heart failure group, LVESP,LVEDP,and LVESV in 200 mg/kg hyperin group decreased(all P<0. 01, while CO,LVEF, +dp/dtmax,and -dp/dtmax increased(P<0. 05 or P<0. 01）. Compared with the Sham group,the serum ALT and AST levels in the heart failure group were higher(all P<0. 01）. Compared with the heart failure group,the serum AST level decreased in the 100 mg/kg hyperin group,and the serum ALT and AST levels decreased in the 200 mg/kg hyperin group(P<0. 05 or P<0. 01）. There was no significant difference in liver coefficient among the four groups(P>0. 05). Compared with the Sham group,the liver tissue in heart failure group had diffuse inflammatory infiltration and steatosis,the liver cells became larger and more uneven in shape,the liver lobule structure disappeared,the liver plate was destroyed and the central vein collapsed,and the collagen formation area increased (all P<0. 05). Compared with the heart failure group,hepatic steatosis, inflammatory cell infiltration and fibrosis in 100 mg/kg and 200 mg/kg hyperin groups were reduced in different degrees,and collagen formation area was reduced (all P< 0. 05. Compared with the Sham group,the levels of Hyp and MDA in the liver tissues of the heart failure group increased, while the levels of GSH-Px and T-SOD decreased (all P<0. 05. Compared with the heart failure group,the levels of Hyp and MDA decreased and T-SOD increased in the 100 mg/kg hyperin group；the levels of Hyp and MDA decreased, and the levels of GSH-Px and T-SOD increased in the 200 mg/kg hyperin group (all P<0. 05. Compared with the Sham group,the mRNA and protein levels of TGF-β1, CTGF,TIMP1, MMP2 and collagen Ⅲ in the liver tissues of the heart failure group increased,while the protein level of p-Smad2/3 increased and MMP1 mRNA and protein decreased (all P<0. 05）. Compared with the heart failure group,the mRNA and protein levels of TGF- β1, CTGF,TIMP1,MMP2 and collagen Ⅲ in the liver tissues of 100 mg/kg hyperin group decreased,while the protein level of p-Smad2/3 decreased and MMP1 protein increased (all P<0. 05). Compared with the heart failure group,the mRNA and protein levels of TGF-β1, CTGF,TIMP1,MMP2,and collagen Ⅲ decreased,the protein level of p-Smad2/3 decreased and the mRNA and protein levels of MMP1 increased in the 200 mg/kg hyperin group(all P<0. 05. Conclusion Heart failure can lead to liver fibrosis in rats；hyperin can inhibit liver fibrosis,and its mechanism may be related to regulating the activation of TGF-β1/ Smad pathway and the balance of TIMP/MMP axis. [ABSTRACT FROM AUTHOR]

Background: Canarium patentinervium leaves are used by the local indigenous people of Malaysia for wound healing. The current study is undertaken to screen the comprehensive antibacterial activity of the leaves and barks extracts, fractions and isolated compounds from this plant. Bioassay guided fractionation was also undertaken to deeply evaluate the antibacterial activity of the water fraction of the leaves extract. This is to provide preliminary scientific evidence to the ethnopharmacology usage of this plant by investigating antibacterial properties of the plant and its isolated constituents. Methods: Bio-assay guided fractionation and subsequent isolation of compounds using open column chromatography. The antibacterial activity against gram positive and gram negative ATCC strain and resistant clinical strains were evaluated using microtiter broth dilution method to determine minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and time-kill assay. The chemical structure of the isolated compounds from the water fraction of the ethanol extract of leaves was elucidated using Nuclear Magnetic Resonance (NMR). Results: The ethanol extract of the leaves and barks showed antimicrobial activity against all four ATCC and eight clinical isolates. The ethanol extract of the leaves and the corresponding water fraction had good activity against MRSA S. aureus. (MIC: 250 μg/ml) and had bactericidal effect on eight of the clinical strains (MSSA,MRSA, oxacillin-resistant CONS, oxacillin-sensitive CONS, Enterococcus faecalis, Klebsiela species, Kleb pneumoniae ESBL and Candida parapsilosis). Further phytochemical investigation of the water fraction of the crude ethanol extract of leaves afforded compound 7 (hyperin) and compound 8 (cynaroside) that had bactericidal activity against tested bacterial species (MIC 50 μg/ml and 100 μg/ml). The two compounds were isolated from this genus for the first time. Conclusions: These results may provide a rational support for the traditional use of Canarium patentinervium Miq. in infections and wound healing, since the antimicrobial compounds isolated were also present in the leaves extract. [ABSTRACT FROM AUTHOR]

Herbal medicines have been used for the treatment of various disorders in the world since very early age. A large number of phytochemicals have been derived from the natural sources in the form of food supplement, neutraceuticals, oils and colour pigments. Flavonoids are a widely distributed group of phytochemicals having benzo-pyrone nucleus. Till so far more than 4000 different types of flavonoids have been described and categorized into different groups like flavonols, flavones, flavanones, isoflavones, catechins and anthocyanidins. Flavonoids have an attractive candidate in the food industry as natural colorants due to its health beneficial effect and safety issue. Hyperin, an important flvonoid were found in the different plants have various pharmacological activities like antioxidant, anti-inflammatory, anticancer, antiviral, antibacterial, antiparasitic, cardioprotective, hepatoprotective and antispasmodic. The aim of this review is to collect all the valuable scientific information of hyperin regarding its medicinal importance, pharmacological activities, isolation and analytical techniques. From the presented data’s in this review it will be beneficial to the scientific person, pharmaceutical manufacturer and consumers in order to it health beneficial effect of hyperin. Thus this valuable information will be helpful to the researchers for developing alternative methods of treatment for different diseases.

A high sensitive voltammetric platform for hyperin detection was developed based on hematite phase iron oxide (α-Fe2O3) doped graphene (GR). The synergistic effects between α-Fe2O3 and GR drastically enhanced the electrocatalytic activity of the resulting materials. The morphology and structure of α-Fe2O3-GR composites were characterized using UV–vis absorption spectra, X-ray diffraction and Transmission Electron Microscopy. By combining the merits of the α-Fe2O3 and GR, a new voltammetric sensor was erected to detect hyperin based on the α-Fe2O3-GR composites. The sensor had good voltammetric response to hyperin, and the linear in the range of 1.0–100 nM. The detection limit of hyperin was found to be 0.5 nM (S/N = 3). Additionally, the designed electrochemical sensor was performed with good selectivity, reproducibility and stability in three real species. [ABSTRACT FROM AUTHOR]

Solanum nigrum (SN) has been widely used in traditional folk medicine to cancer treatments, but the defined target is not clear. To identify the potent targets for the treatment of HCC using various strategies, 23 active compounds were collected by IMPPAT and TCMSP databases based on their DL and ADME properties. PharmMapper, SEA, STITCH and DRAR-CPI followed to CTD and PHARMGKB were used for target fishing. 25 targets were retrieved to analyze GeneMANIA and DAVID. Cytoscape 3.6.1 was used for the network's constructions compound-target, target-pathway, compound-target-pathway and target organ networks were developed. For target validation, molecular docking GLIDE, AutoDock Vina and iGEMDOCK were used. Majorly, 21 targets were located in the liver, are considered as primary targets for in silico docking. The study concludes 5 potent targets and 4 active compounds via 4 signaling pathways involving HCC metabolism. SN could be potentially beneficial in treating HCC. [ABSTRACT FROM AUTHOR]

Objective To identify and evaluate the quality of cuscutae semen and its close relatives products and counterfeit to provide guarantee for the production of drugs and safety of clinical medication. Methods From March to May 2018, the appearance trait and physicochemical properties of the cuscutae semen was identified from the appearance, water test, microscopic and thin layer chromatography. The quality of cuscutae semen was analyzed by content of moisture, total ash and acid insoluble ash and effective component. Results The cuscutae semen and its close relatives products and counterfeit could be distinguished easily with the appearance, water test, microscopic and thin layer chromatography. The content of moisture, total ash acid insoluble ash, hyper oside of cuscutae semen were 5. 83% - 7. 62%,4. 75% - 5. 59%,1. 91% - 2. 73% and 0. 13%- 0. 21 %. Conclusion Cuscuta and the true and false can be effectively distinguished by physical, chemical and microscopic identification. Through quality evaluation, the adulteration of dodder can be determined effectively. [ABSTRACT FROM AUTHOR]

This study was designed to investigate the effect of different concentrations of Hyperin and Icariin (ICA)on proliferation and the secretion of estrogen (E2), and progesterone (P) in granulosa cells, and to explore the effect of Hyperin and Icariin on the expression of CYP17 and CYP19. Rat ovary granulosa cells were cultured in vitro and treated with different concentrations of Hyperin and Icariin. The proliferation of ovarian granulosa cells was measured with the MTT assay. The concentration of estradiol was measured with a magnetic particle-based enzyme-linked immunosorbent assay (ELISA) kit. The CYP17 and CYP19 mRNA expression was detected by quantitative real-time reverse-transcription polymerase chain reaction (qRT-PCR). The CYP17 and CYP19 protein expression was determined with Western blotting. Hyperin (50 μg/l) and Icariin (10 μg/l) significantly increased proliferation of ovarian granulosa cells and secretion of estrogen and progesterone. Hyperin and Icariin stimulated the mRNA and protein expression of CYP17 and CYP19. These results showed that Hyperin and Icariin can promote the secretion of E2 and P through up-regulation of CYP17 and CYP19. Frequently used Chinese herbs like Cuscuta Chinensis Lam and Epimedium Brevicornu maxim, which contain Hyperin and Icariin, could improve the ovarian endocrine function through these effects. • Hyperin and Icariin increase the viability of granulosa cells. • Estrogen and progesterone secretion was increased by Hyperin and Icariin treatment. • Hyperin and Icariin promote the secretion of E2 and P by up-regulating CYP17 and CYP19. [ABSTRACT FROM AUTHOR]

A novel electrochemically activated ZrO2 nanoparticles modified carbon paste electrode (CPE) (ZrO2-CPE(ox)) was prepared and applied for selective and sensitive determination of hyperin. Scanning electron microscopy (SEM), X-ray diffraction (XRD), Raman spectra and electrochemical experiment were used to characterize the ZrO2 nanoparticles and investigate the electrochemical performance of the ZrO2-CPE(ox). Compared with bare CPE and electrochemically activated CPE (CPE(ox)), the ZrO2-CPE(ox) got more reactive sites by electrochemical treatment and exhibited larger effective surface area and more excellent electrochemical catalytic activity toward the redox of hyperin. Under the optimum conditions, the oxidation peak currents showed a linear relationship with the concentrations of hyperin in the range of 5. 0 × 1 0 − 9 – 2. 0 × 1 0 − 6 mol L − 1 and 2. 0 × 1 0 − 6 – 1. 2 × 1 0 − 5 mol L − 1 , and a low detection limit of 1. 0 × 1 0 − 9 mol L − 1 was achieved for hyperin. Moreover, the proposed method exhibited an excellent selectivity, stability, reproducibility and repeatability, which make it very suitable for a potential choice for determining the concentrations of hyperin in drug matrices. A novel electrochemically activated ZrO2 nanoparticles modified carbon paste electrode was prepared and successfully used for electrochemical determination of hyperin. [ABSTRACT FROM AUTHOR]

Abstract Hyperin, a flavonoid compound found in natural plants, has been reported that it have anti-inflammatory properties. However, the protective effects and mechanisms of hyperin on acute lung injury have not been reported so far. This research was designed to investigate the protective effects of hyperin on lipopolysaccharide-induced acute lung injury (ALI) in mice. The mice were stimulated with LPS in the presence or absence of hyperin and the MPO activity, lung wet/dry ratio, inflammatory cells in BALF, and cytokines, as well as NF-κB expression were assessed in lung tissue. Results showed that hyperin significantly inhibited LPS-induced histological changes, inflammatory cell infiltration, MPO activity and lung wet/dry ratio. Additionally, hyperin distinctly reduced the production of TNF-α, IL-1β and IL-6 and the activation of NF-κB signaling pathways in LPS-induced ALI in mice. In conclusion, hyperin is an effective suppressor of inflammation and may be a promising potential therapeutic reagent for ALI treatment. Highlights • Hyperin significantly inhibited LPS-induced lung hisopathologic changes, MPO activity. • Hyperin significantly inhibited LPS-induced TNF-α and IL-6 production. • Hyperin significantly inhibited LPS-induced NF-κB signaling pathway activation. [ABSTRACT FROM AUTHOR]

Objective To improve the quality standards of Hypericum ascyron. Methods Hypericum ascyron was identified by microscopic observation and TLC method.The moisture, total ash,acid-insoluble ash and alcohol soluble extract were assayed following the procedures stated in Chinese Pharmacopoeia.The contents were determined by HPLC. Results Identification methods for Hypericum ascyron with microscopy,TLC and HPLC were established.The limits of moisture,total ash and alcohol soluble extract were defined. Conclusion This study provides scientific data for the quality control of Hypericum ascyron. [ABSTRACT FROM AUTHOR]

Glycation, the nonenzymatic reaction between proteins and excess blood sugar, is implicated in multiple disorders and occurs via the formation and accumulation of advanced glycation end products (AGEs). In our previous studies, we demonstrated that the red-leaf variant of the Persicaria hydropiper sprout (Japanese red water pepper, Benitade) is one of the potent plants that inhibit formation of AGEs. In this study, we aimed to identify antiglycative compounds in Benitade. Benitade extracts were prepared with hot water, then fractionated by using high-performance liquid chromatography (HPLC). The antiglycative efficacy of each fraction was evaluated by measuring the formation of fluorescent AGEs (Ex 370 nm/Em 440 nm). Two fractions, which contained peaks at 26.4 min and 31.8 min, showed potent antiglycative efficacy. When we hydrolyzed these peaks, they shifted to 32.5 and 41.4 min, which are the same retention times as cyanidin and quercetin, respectively. Based on thin-layer chromatography, both compounds contained galactose. Finally, ultrahigh-performance liquid chromatography/quadrupole-time of flight mass spectrometry (UHPLC-QqTOF-MS) analyses were performed to determine the structure of those compounds. Overall, we identified two glycosides, cyanidin 3-O-galactoside (idaein) and quercetin 3-O-galactoside (hyperin), as representative antiglycative compounds in Benitade. [ABSTRACT FROM AUTHOR]

A novel high-sensitive electrochemical sensor with glassy carbon electrode (GCE) as support for hyperin determination is successfully designed and constructed, and the well-shaped nano-meter modified material is synthesized via a one-step and facile route. Functionalized with surfactant sodium dodecyl sulfate (SDS), Single-Walled Carbon Nanotubes (SWCNTs) are synchronously grafted with ZrO 2 nanoparticles to develop into the as-prepared nano-composite (ZrO 2 -SDS-SWCNTs). Compared to the previous reports related with hyperin detection, the linear range gets wider and detection limit (LOD) becomes lower with the aid of this novel nano-composite modified glassy carbon electrode (ZrO 2 -SDS-SWCNTs/GCE). The crystalline phases and functionalization of the preparation process has been investigated by X-ray diffraction (XRD) and Fourier transform infrared (FT-IR) instrument analysis, respectively, and the micro-morphology of related modified materials is also visibly characterized by scanning electron microscope (SEM) and transmission electron microscope (TEM). In addition, electrochemical properties of the modified materials are comparably explored by means of impedance spectroscopy (EIS) and cyclic voltammograms (CV). According to the established calibration curve under optimized condition, the peak current (Differential pulse voltammetry (DPV) signal) keeps a linear relationship with hyperin concentration in the ranges of 1.0 × 10 −9 − 3.0 × 10 −7 mol L −1 , meanwhile detection limit reaches as low as 5 × 10 −10 mol L −1 (S/N = 3). As for practical applications, the proposed sensor has also worked well on sensitive hyperin determination in real species Abelmoschus manihot. [ABSTRACT FROM AUTHOR]

Background: Long-term chemotherapy reduces the sensitivity of colon cancer cells to chemotherapeutics like vincristine (VCR) and lead to drug resistance, which has become a major barrier for colon cancer treatment. Calcium antagonists are used as clinical tumor multidrug resistance reversal agents to regulate the P-glycoprotein (P-gp) level and block efflux pump function now, but they have significant side effects. Hyperin as active component with low toxicity in traditional Chinese medicine has calcium antagonistic effect. Thus, the purpose of this study was to evaluate the in hibitory effect of hyperin on the growth of HCT8/VCR colon cancer cell line (vincristine-resistant) and analyze the enhancing effect of hyperin on the sensitivity of cancer cells to VCR and its relationship to the expression and function of P-gp. Methods: Using the MTT method, we investigated the influence of hyperin, VCR alone, and hyperin plus VCR on the growth of HCT8/VCR cells. Western blot analysis was employed to detect the expression of P-gp, and flow cytometry was used to evaluate P-gp function by detecting the fluorescence intensity of intracellular Rho123. Results: The inhibitory effect of hyperin at the dose of 12.5 µM on HCT8/VCR cell growth was not enhanced as time progressed and no significant inhibitory effect was found for VCR-treated cells at the dose of 2 µM. But the inhibition of cell growth was observed aft er the combined treatment of hyperin (12.5 µM) and VCR (2 µM). P-gp expression levels in HCT8/VCR cells treated with hyperin plus VCR were markedly lower than the levels in control cells and those treated with VCR. In addition, the intensity of Rho123 fluorescence of HCT8/VCR cells treated with hyperin plus VCR or hyperin alone was significantly higher than intensity observed in control cells and those treated with VCR alone. Conclusions: Hyperin synergistically augments the growth inhibitory effect of vincristine. The underlying mechanism most probably involves down-regulation of P-gp expression and inhibiting the function of the P-gp pump in HCT8/VCR cells. [ABSTRACT FROM AUTHOR]

Objective To observe the anti-enterovirus type 71 (EV71 ) effects of Houttuvnia cordata Thunb water extract and its main ingredients, including chlorogenic acid, rutin, spasinin, and quercetin in vitro. Methods The RD cells (derived from human rhabdomyosarcoma cells) were divided into the Houttuvnia cordata group, hyperoside group, quercetin group, rutin group, chlorogenic acid group, and control group. Cells in the Houttuyniae cordata group were given water extracts of Houttuvnia coidata at the concentrations of 5 000. 2 500. 1 250. 625. and 313 mg/L; cells in the quercetin and rutin groups were added with quercetin and rutin at the concentrations of 10. 00, 5. 00, 2. 50. 1.25 . and 0.63 mg/mL; cells in the hyperoside and chlorogenic acid groups were given hyperoside and chlorogenic acid, respectively, with the concentrations of 4. 00, 2.00. 1.00, 0.50, and0.25 mg/mL; cells in the control group were added with the cell culture fluid. We observed the cytopathic effect (CPE) and calculated the inhibition rate of virus replication, half maximal inhibitory concentration (IC50) , inhibition rate of virus growth, inhibition rate of virus adsorption, vims inactivation rate, and virus penetration rate. Results The inhibition rate of virus replication in the Houttuvnia cordata group and quercetin group was higher than that in the other four groups, and the inhibition rate increased with the increasing concentrations ( all P < 0. 05 ). The inhibition rate of virus growth in the hyperin and rutin groups was higher than that in the other four groups ( all Pc 0.05). The inhibition rate of virus adsorption in the hyperin and Houttuynia cordata group was higher than that in the other four groups ( all P < 0. 05). The water extract and its main components of Houttuynia cordata had no effect in inactivating the virus. No inhibitory effect on virus penetration was observed in each group at 15 and 30 min. At 60 min. the inhibition rate of virus penetration was higher in houttuyniae, quercetin, rutin and chlorogenic acid groups than in the hypero-side group and control group ( all P <0. 05 ). The inhibition rate of virus penetration of the quercetin group and rutin group decreased with the decreasing drug concentrations, but increased in the chlorogenic acid group. Conclusions The water extract of Houttuynia cordata Thunb and its main components all have the effect of anti-EV71 in vitro, but had no effect in inactivating the virus. Quercetin has the effect of inhibiting virus replication. Hyperin and rutin block the growth of the virus, hyperoside can inhibit virus adsorption, and quercetin, rutin, chlorogenic acid can inhibit the virus penetration. [ABSTRACT FROM AUTHOR]

In the present study, porous magnetic cellulose beads (CBs) were prepared and further modified using amines. The CBs appeared to have good spherical shape and three-dimensional (3D) porous structure. In the adsorption tests, the modified cellulose beads (MCBs) showed better adsorption capacities and shorter adsorption times on hyperin and 2′-O-galloylhyperin than the commercial resins. The adsorption may be due to the hydrogen bonding between the target compounds and the amine groups of MCBs. After adsorption and desorption, the contents of hyperin and 2′-O-galloylhyperin reached 1.32% and 3.92%, which were 4.08 and 4.23 times higher than those in the Pyrola extracts. Therefore, the prepared MCBs in this study make an excellent adsorbing material of hyperin and 2′-O-galloylhyperin, and it may have potential for the separation of other natural compounds. [ABSTRACT FROM AUTHOR]

In this paper, a novel electrochemiluminescence (ECL) sensor of sol-gel@graphene luminescent composite film modified electrode for hyperin determination was prepared using graphene (G) as solid-phase microextraction (SPME) material, based on selective preconcentration of target onto an electrode and followed by luminol ECL detection. Hyperin was firstly extracted from aqueous solution through the modified GCE. Hydrogel, electrogenerated chemiluminescence reagents, pH of working solution, extraction time and temperature and scan rate were discussed. Under the optimum conditions, the change of ECL intensity was in proportion to the concentration of hyperin in the range of 0.02–0.24 μg/mL with a detection limit of 0.01 μg/mL. This method showed good performance in stability, reproducibility and precision for the determination of hyperin. [ABSTRACT FROM AUTHOR]

Harvest seasons have important influences on bioactive compounds and antioxidant activities of plants. Pyrola [ Pyrola incarnata Fisch.] is rich in antioxidants and is a valuable natural antioxidant food source in northeastern China. In order to well development and utilization of pyrola resources, in the same site, the quality of the different harvest time samples of pyrola was investigated. Variations in the active components and antioxidant activities of pyrola samples collected during six monthly harvests (from May to October) were analyzed. A principal component analysis was used to analysis of the interrelationships among total phenolic content, antioxidant activities and bioactive compound contents. The sample harvested in August had the highest total phenolic content (217.73 ± 9.14 mg/g gallic acid equivalent) and the strongest antioxidant activity. The antioxidant activity of the August sample was similar to the ascorbic acid and butylated hydroxytoluene activities. The results of a principal component analysis indicated that the active components included catechin, hyperin, 2′-O-galloylhyperin and quercitrin, which were strongly associated with the antioxidant activity of the August sample. Hyperin and 2′-O-galloylhyperin are the primary compounds found in pyrola, and they play major roles in mediating antioxidant activity. The August pyrola sample had the highest antioxidant potential and was a new, highly enriched resource for hyperin and 2′-O-galloylhyperin. Thus, August was the ideal time for the pyrola harvest. [ABSTRACT FROM AUTHOR]

Hyperin, a flavonoid compound found in Ericaceae , Guttiferae, and Celastraceae , has been reported to have anti-inflammatory effects. In the present study, we investigated the effects of hyperin on cisplatin-induced acute kidney injury (AKI) in mice. The renal tissue damage induced by cisplatin was detected by H&E staining. Blood urea nitrogen (BUN), creatinine, reactive oxygen species (ROS), and malondialdehyde (MDA) were also detected. Further, the effects of hyperin on cisplatin-induced TNF-α, IL-1β and IL-6 were detected by ELISA. In addition, the phosphorylation of nuclear factor kappa B (NF-κB) and the expression of nuclear factor E2-related factor-2 (Nrf2) and HO-1 were detected by western blot analysis. The results showed that hyperin attenuated histological changes of kidney induced by cisplatin. The levels of BUN, creatinine, ROS, MDA, TNF-α, IL-1β and IL-6 induced by cisplatin were also inhibited by hyperin. Cisplatin-induced NF-κB activation was inhibited by hyperin. Additionally, hyperin was found to up regulate the expression of Nrf2 and HO-1. In conclusion, the results suggest that hyperin protects against cisplatin-induced AKI by inhibiting inflammatory and oxidant response. [ABSTRACT FROM AUTHOR]

A simple electrochemical method for the highly sensitive determination of hyperin was established based on poly(diallyldimethylammonium chloride)-functionalized graphene modified electrode (PDDA-Gr/GCE). The nanocomposite was characterized by X-ray diffraction (XRD), ultraviolet/visible spectra (UV–vis), Fourier Transform infrared spectroscopy (FT-IR) and transmission electron microscopy (TEM). The electrochemical characteristics of hyperin were studied in detail via cyclic voltammetry (CV), chronocoulometry (CC). Dynamics parameters of electrode process were also calculated to discuss the reaction mechanism. Under the optimized conditions, a lower detection limit of 5 × 10 − 9 mol L − 1 (S/N = 3) and a wide linear detection range from 7 × 10 − 9 to 7 × 10 − 7 mol L − 1 were achieved by the differential pulse voltammetry (DPV). Additionally, this simple, sensitive sensor was proved to be suitable for the determination of hyperin in Chinese herb Hypericum Perforatum with satisfactory results. [ABSTRACT FROM AUTHOR]

A specific and sensitive LC-MS/MS assay was developed to simultaneously quantify three structurally similar flavonoid glycosides - hyperin, reynoutrin and guaijaverin - in mouse plasma. Biosamples were prepared by solid-phase extraction. Isocratic chromatographic separation was performed on an AichromBond-AQ C18 column (250 × 2.1 mm, 5 μm) with methanol-acetonitrile-water-formic acid (20:25:55:0.1) as the mobile phase. Detection of hyperin, reynoutrin, guaijaverin and internal standard [luteolin-7- O- β- d-apiofuranosyl-(1 → 6)- β- d-glucopyranoside] was achieved by ESI-MS/MS in the negative ion mode using m/ z 463 → m/ z 300, m/ z 433 → m/ z 300, m/ z 433 → m/ z 300 and m/ z 579 → m/ z 285 transitions, respectively. Linear concentration ranges of calibration curves were 4.0-800.0 ng/mL for hyperin and reynoutrin and 8.0-1600.0 ng/mL for guaijaverin when 100 μL of plasma was analyzed. We used this validated method to study the pharmacokinetics of hyperin, reynoutrin and guaijaverin in mice following oral and intravenous administration. All three quercetin-3- O-glycosides showed poor oral absorption in mice, and the absolute bioavailability of hyperin after oral administration of 100 mg/kg was 1.2%. Pretreatment with verapamil increased the peak concentration and area under the concentration-time curve of hyperin, which were significantly higher than the control values. The half-life of hyperin with verapamil was significantly prolonged compared with that of the control. Copyright © 2016 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

The variation in water availability can cause oxidative stress in plant species, which respond by producing antioxidants. Phenolic compounds are among the primary substances responsible for antioxidant activities. Thus, the goal of this study was to evaluate whether rainfall in a dry forest in Brazil affects the antioxidant activity and the major phenolic compounds in the stem bark of Anadenanthera colubrina, an economically important species from the semi-arid region of Brazil. Monthly samplings were performed over one year for the analysis of free radical sequestration by the DPPH method and for the identification and quantification of major phenolic compounds by HPLC. These data were correlated with each other and with the monthly rainfall. Three major phenolic compounds were identified, one of which was hyperin. The stem bark was highly capable of scavenging free radicals. The antioxidant activity and the production of the three compounds only slightly varied during the year, despite the significant differences among a few of the months studied. These differences are apparently unrelated to rainfall. No correlation was found between the major compounds and free radical scavenging. Our results suggest that rainfall was not the environmental factor responsible for monthly differences in the antioxidant activity of and concentrations of major phenolic compounds in the bark of A. colubrina. [ABSTRACT FROM AUTHOR]

Hyperin (HP) is a flavonoid compound found in various plants like Ericaceae, Guttifera and Celastraceae. The present study has revealed that HP has a variety of pharmacological effects including anti-oxidant, anticancer, and anti-coagulant, especially anti-inflammatory. However, the potential molecular mechanism of anti-inflammatory is still unrevealed. In this study, HP not only significantly attenuated inflammation in C57BL/6J mice with acute liver injury (ALI), but also reduced the expression of TNF-α and IL-6 in lipopolysaccharide (LPS)-induced RAW264.7 cells. Furthermore, our findings showed that HP remarkably induced the expression of PPAR-γ in vivo and in vitro . Interestingly, compared with the HP treatment group, a specific blocking agent of PPAR-γ T0070907 and PPAR-γ small interfering (si)-RNA-mediated silencing in RAW264.7 cells were used to evaluate the involvement of HP in alleviating LPS-induced inflammation. More importantly, over-expression of PPAR-γ had an opposite effect on the expression of TNF-α and IL-6 in LPS-induced RAW264.7 cells after treatment with HP. In addition, HP remarkably inhibited the expression of P-ERK1/2 and P-P38 MAPK. Taken together, all the above results indicate that HP may serve as an effective modulator of PPAR-γ, further down-regulating ERK1/2 and p38 MAPK during the pathogenesis of inflammation. [ABSTRACT FROM AUTHOR]

[Display omitted] • Lignin polymer was firstly introduced to prepare a monolithic SPE cartridge; • The prepared adsorbent in the cartridge shows high surface area of 333.29 m2/g; • Has enriched interaction sites following multiple chemical groups of its surface; • It shows good selectivity for the hyperin and outstanding matrix-removal ability. In this work, a monolithic cartridge packed with lignin polymer (LiP)-dopped adsorbent was fabricated in a stainless steel tube via polymerization using divinyltetramethyldisilane as the monomer, which aimed for the extraction and separation of hyperin from Senecionis Scandentis Hebra (SSH). The fabricated monolithic cartridge used for the solid-phase extraction (SPE) method was characterized by scanning electron microscope, fourier transform infrared spectrometer, specific surface area measuring instrument and mercury intrusion porosimetry, which confirms a macro- and meso -porous structure with high specific surface area of 333.2 m2/g of the optimized adsorbent. An SPE-HPLC method was established by combining the prepared monolithic cartridge and a C18 analytical column via HPLC system for the online extraction, enrichment and quantitative determination of hyperin from SSH. The results indicate that the prepared monolithic cartridge shows not only specific selectivity for the target component of hyperin, but also outstanding removal ability for the sample matrix. Methodology validation was carried out to verify the proposed quantitative analytical method, including the regression equation and related data, the precision, the spiked recovery and the preparative repeatability of the SPE cartridge, which results confirm the feasibility of the present method for the extraction and quantitative determination of hyperin from SSH. [ABSTRACT FROM AUTHOR]

Biomass waste, a good candidate for advanced carbon materials for sustainable electrodes, is receiving more and more attention for high value-added materials because of its promising contribution to economic growth and sustainable development. We proposed a green co-hydrothermal approach to prepare lotus seedpods biochar (BC) decorated molybdenum disulfide (MoS 2) from waste lotus seedpods and precursors of MoS 2, and a portable, flexible, outdoor and inexpensive sensing platform for hyperin on the integrated flexible three-electrode using U-disk potentiostat with smartphone was successfully developed. Structure and properties of MoS 2 -BC were characterized, it was proved that BC improves microstructure and morphology, electronic conductivity, electrode stability and electrocatalytic properties of MoS 2. Attributing to these impressive features, the detection signal of hyperin was significantly amplified by the MoS 2 -BC modified glass carbon electrode (GCE) in detection range of 0.01–21 μΜ with detection limit (LOD) of 5 nM. It was worth mentioning that the MoS 2 -BC modified screen-printed electrode (SPE) performs hyperin detection in range of 100 nM - 3 μM with LOD 50 nM (S/N = 3). The practicability of the proposed method confirmed that the portable, on-site, low-cost, and outdoor detection of hyperin was feasible and practical in comparison with traditional both electrochemical sensing and HPLC methods. A portable U-disk potentiostat with smartphone for outdoor sensing of hyperin using lotus seedpods biochar decorated molybdenum disulfide on screen-printed electrode. [Display omitted] • Lotus seedpods biochar decorated molybdenum disulfide was prepared by co-hydrothermal method. • A portable U-disk potentiostat with smartphone for outdoor sensing of hyperin was developed. • The BC improved microstructure, conductivity, stability, and electrocatalytic capacity of MoS 2. • The proposed method was feasible for portable, on-site, inexpensive, and outdoor detection. [ABSTRACT FROM AUTHOR]

The proliferation of extravillous trophoblasts (EVT) and their further migration, invasion, and differentiation into the decidual and myometrial vasculature are vital for spiral artery remodeling. These physiological functions of EVT are also essential steps in the implantation of the human embryo and the formation of the placenta and are closely related to pregnancy maintenance and the occurrence of abortion. Hyperin is a flavonoid with anti-inflammatory, pro-proliferative, and anti-apoptotic properties. Consequently, we investigated the previously unexplored effects of hyperin on the proliferation, migration, and invasion of HTR-8/SVneo cells. Human extravillous trophoblast-derived HTR-8/SVneo cells were incubated with different concentrations of hyperin (0, 5, 10, 25, 50, and 100 μM) to observe the changes in cell proliferation, migration, invasive capacity, and pathway activation. Proliferation, migration, and invasion were promoted by activating the JAK1/STAT3 pathway in HTR-8/SVneo cells treated with hyperin. In addition, brepocitinib (PF-06700841) significantly inhibited the proliferation, migration, and invasion effects of hyperin on HTR-8/SVneo cells. In vivo experiments confirmed that hyperin reduces the embryo loss rate in recurrent spontaneous abortion (RSA) model mice. Furthermore, our study revealed that hyperin promoted the proliferation, migration, and invasion of HTR-8/SVneo cells via activation of the JAK1/STAT3 pathway, further improving pregnancy outcomes in RSA., Competing Interests: The authors declare no competing interests., (© 2023 Published by Elsevier Ltd.)

To establish the qualitative identification and content determination methods of the fruits extract of Rosa davurica Pall, capsule. TLC was used to accomplish the qualitative identification, while UV and HPLC were applied to determine the content of total flavonoids and hyperin of the fruits extract of Rosa davurica Pall, capsule respectively. There was no negative interference in established TLC method, which offered clear fluorescent spots. Rutin and hyperin showed good linear relationship at the range of 4. 0~48. 0 µg/mL (r = 0. 9996) and 0- 192~1. 152 µg (r=0. 9999) respectively. The average recovery of rutin and hyperin were 100.05% and 99.39%, while their RSD were 1. 40%(n=6) and 0. 66% (n = 6). TLC method obtained was specific and content determination methods were accurate and reliable, which could be applied for quality control of the fruits extract of Rosa davurica Pall, capsule. [ABSTRACT FROM AUTHOR]

Hypericum perforatum L. (St. John's Wort) is an important medicinal plant which is widely used in the treatment for depression and irritable bowel syndrome. It is also used as a dietary supplement. Major bioactive phytochemicals of H. perforatum are phenolics and flavonoids. Quality of these phytochemicals is dramatically influenced by environmental and biological factors in the field grown plants. As an alternative, we have developed adventitious root cultures in large-scale bioreactors for the production of useful phytochemicals. Adventitious roots of H. perforatum were cultured in 500 l pilot-scale airlift bioreactors using half-strength Murashige and Skoog medium with an ammonium and nitrate ratio of 5:25 mM and supplemented with 1.0 mg l indole butyric acid, 0.1 mg l kinetin, and 3 % sucrose for the production of bioactive phenolics and flavonoids. Then 4.6 and 6.3 kg dry biomass were realized in the 500 l each of drum-type and balloon-type bioreactors, respectively. Accumulation of 66.9 mg g DW of total phenolics, 48.6 mg g DW of total flavonoids, 1.3 mg g DW of chlorogenic acid, 0.01 mg g DW of hyperin, 0.04 mg g DW of hypericin, and 0.01 mg g DW of quercetin could be achieved with adventitious roots cultured in 500 l balloon-type airlift bioreactors. Our findings demonstrate the possibilities of using H. perforatum adventitious root cultures for the production of useful phytochemicals to meet the demand of pharmaceutical and food industry. [ABSTRACT FROM AUTHOR]

Abstract: Background and aim: Hyperin, a flavonol compound extracted from the Chinese herb Abelmoschus manihot L. Medic, is reported to exert protective actions in cerebral ischemic injury. The specific aim of the present study was to study the relaxation of Hyperin in rat isolated basilar artery and identify the underlying cellular mechanisms. Methods: Rat isolated basilar artery segments were cannulated and perfused while being superfused with PSS solution. Vessel images were recorded by video microscopy and diameters measured. Membrane potential was recorded using glass microelectrodes to evaluate the basilar artery smooth muscle cell hyperpolarization. Results: Perfusion of Hyperin (1~100μM) elicited a concentration-dependent relaxation of basilar artery segments preconstricted with 0.1μM U46619. The response was significantly inhibited by the removal of the endothelium. Hyperin also elicited marked and concentration-dependent hyperpolarization of smooth muscle cells. 30μM nitro-L-arginine (an inhibitor of nitric oxide synthase) and indomethacin (an inhibitor of cyclooxygenase), partially inhibited Hyperin-induced relaxation and hyperpolarization leaving an attenuated, but significant, endothelium-dependent relaxation and hyperpolarization. This remaining effect was almost completely blocked by 1mM tetraethylammonium (an inhibitor of Ca2+-activated K+ channels), or by 100μM DL-propargylglycine, an inhibitor of cystathionine-γ-lyase (a synthase of the endogenous H2S). Conclusion: These findings show that Hyperin produces significant hyperpolarization in rat basilar artery smooth muscle cells and relaxation through both endothelium-dependent and endothelium-independent mechanisms. The underlying mechanisms appeared to be multi-factorial involving nitric oxide, prostacyclin, and endothelium-derived hyperpolarizing factor (EDHF). Our data further suggest that endogenous H2S is a component of the EDHF-mediated hyperpolarization and relaxation to Hyperin. [Copyright &y& Elsevier]

Abstract: The pathogenesis of diabetic vascular complications involves the formation of advanced glycation end-products (AGEs). AGEs accumulate slowly in the body with age and more rapidly in individuals with diabetes mellitus. An abnormally elevated blood glucose level in diabetes mellitus causes the formation of AGEs. Also, oxidative reactions contribute significantly to the formation of AGEs. The antioxidant flavonoids, quercetin, isoquercitrin, hyperin and cacticin from plants, decrease the formation of AGEs. This activity was examined using an in vitro glycation reaction. Of the tested compounds, isoquercitrin and hyperin showed a strong inhibitory activity against the formation of AGEs. These compounds showed inhibitory activities that were more potent than the positive control, aminoguanidine. These results suggest that isoquercitrin and hyperin may be promising agents to treat glycation-associated diseases. [ABSTRACT FROM AUTHOR]

Abstract: Aim: To reveal the content variation of flavonoids in Houttuynia cordata from main producing areas in China, and to lay a foundation for the breeding of quality of Houttuynia cordata. Methods: Several flavonoids including hyperin, quercitrin, and quercetin in H. cordata from 22 different provenances or geographic origins in China were purified and measured by using high-performance liquid chromatography (HPLC). The relationship between the content of flavonoids in H. cordata and their biological characteristics such as morphological and growth traits or a geographic origin were analyzed. Results and Conclusion: The levels of three major flavonoids: hyperin, quercitrin, and quercetin, varied remarkably in the plants of H. cordata from different provenances, and variation in quercitrin was significantly correlated to the biological characteristics of the plant but not correlated to the geographic region where the plant grows. Our data thus provides an important means for the selection or evaluation of candidate cultivars of H. cordata from a pharmacological perspective. [Copyright &y& Elsevier]

Abstract: A simple, highly sensitive assay for fibronectin (Fn) was reported using resonance light-scattering (RLS) technique based on the enhanced RLS intensity of hyperin–cetyltrimethylammonium bromide (CTMAB)–Fn system. The interaction system of hyperin–CTMAB–Fn was investigated using spectral methods. Mechanistic investigations show that the main reason of the enhanced RLS intensity of Fn is the formation of three-component complex (hyperin–CTMAB–Fn), in which CTMAB acts as a bridge between hyperin and Fn. The effects of pH, surfactant, concentration of CTMAB and hyperin, incubation time and foreign substances on the enhancement of RLS intensity were studied. Under the optimum conditions, the enhancement of RLS intensity is in proportion to the concentration of Fn in the range of 1.9–248ng/ml. The synthetic samples containing Fn were analyzed and results obtained were satisfied. [Copyright &y& Elsevier]

From the aerial parts of Asperula arvensis L. 9 known flavanol glycosides, namely quercetin (1), isoquercitrin [= quercetin 3-O-β-glucopyranoside] (2), hyperin [= quercetin 3-O-β-galactopyranoside] (3) quercetin 7-O-&beta-galactopyranoside (4), quercetin 4'-O-β-galactopyranoside (5), isorhamnetin 3-O-β-galactopyranoside (8) and isorhamnetin 3-O-α-rhamnopyranosyl (1''' → 6'') (9), were isolated. The structures of the compounds were elucidated by high field 1D and 2D NMR and ESI-MS spectroscopies. [ABSTRACT FROM AUTHOR]

The interactions of flavonoids, including quercetin, rutin, hyperin and baicalin, with human serum albumin (HSA) were studied. Fluorescence emission spectra of HSA in the presence of the investigated compounds, recorded at the excitation and emission wavelength of 280 and 290–500 nm, respectively, clearly showed that these compounds quenched the fluorescence of HSA. The binding constants and the number of binding sites of the flavonoids with HSA were obtained by three different calculation methods and the results obtained by these methods were compared. The effects of various metal ions on the binding constants of these flavonoids with HSA were also studied. Based on the mechanism of the Förster energy transference, the energy transfer efficiency between the acceptors and HSA were found. The relationship between the structure characteristics of these compounds and binding properties of the flavonoids and HSA was explored. [Copyright &y& Elsevier]

The chloroform and the ethyl acetate fractions from the roots of Acanthopanax chiisanensis exhibited a significant inhibition of prostaglandin E2 (PGE2) production in rat peritoneal macrophages stimulated by the protein kinase C activator, 12- O-tetradecanoylphorbol 13-acetate (TPA). Hyperin was isolated as an active principle from the ethyl acetate fraction. It suppressed not only PGE2 production but also nitric oxide (NO) production in vitro in a concentration dependent manner, their IC50, being 24.3 and 32.9 μM, respectively. Hyperin also caused a significant inhibition of increase in acetic acid-induced vascular permeability in mice in vivo. [ABSTRACT FROM AUTHOR]