scholarly journals Identification of Scopoletin and Chlorogenic Acid as Potential Active Components in Sunflower Calathide Enzymatically Hydrolyzed Extract towards Hyperuricemia

2021 ◽  
Vol 11 (21) ◽  
pp. 10306
Author(s):  
Huining Dai ◽  
Shuai Lv ◽  
Xueqi Fu ◽  
Wannan Li
Keyword(s):  
Chlorogenic Acid ◽  
Glucose Transporter ◽  
Water Soluble ◽  
Active Components ◽  
Expression Levels ◽  
Binding Pockets ◽  
Glucose Transporter 9 ◽  
Agricultural Byproduct ◽  
Soluble Components

It is known that sunflower (Helianthus annuus L.) calathide enzymatically hydrolyzed extract (SCHE) contributes to the regulation of serum uric acid (UA); however, evidence regarding its bioactive components and mechanism are lacking. We identified two water-soluble components (scopoletin and chlorogenic acid) that are abundant in sunflower calathide, especially evaluated for the inhibition of xanthine oxidase (XO) and the expression levels of urate transporters with SCHE. Molecular docking of a chlorogenic acid–XO complex was more stable than that of the Scopoletin–XO, and its binding pockets, which closed the Mo = S center, was similar to xanthine pockets. Moreover, chlorogenic acid exhibited stronger inhibition than that of the scopoletin below 260 μM, despite the IC50 of scopoletin (577.7 μM) being lower than that chlorogenic acid (844.7 μM) on the UA generation assessed by a spectrophotometer in vitro. It revealed that chlorogenic acid and scopoletin were competitive inhibitors of XO. In addition, the SCHE (300 μg/mL) and chlorogenic acid (0.75 mM) obviously inhibited urate transporter 1 (URAT1) and glucose transporter 9 (GLUT9) expression levels, while scopoletin significantly upregulated the expression of GLUT9. To summarize, chlorogenic acid served a crucial role in UA regulation consistent with the SCHE and functioned as an important ingredient of SCHE. The strategic analysis of SCHE combined with scopoletin and chlorogenic acid may contribute to the development of food supplemental alternatives on UA metabolism and the reduction of agricultural byproduct waste.

scholarly journals Active Components from Lagotis Brachystachya Maintain Uric Acid Homeostasis by Inhibiting Renal TLR4-NLRP3 Signaling in Hyperuricemic Mice

2021 ◽  
Author(s):  
Ji-Xiao Zhu ◽  
Hai-Yan Yang ◽  
Wei-Qiong Hu ◽  
Jie Cheng ◽  
Yang Liu ◽  
...  
Keyword(s):  
Uric Acid ◽  
Glucose Transporter ◽  
Organic Anion ◽  
Underlying Mechanism ◽  
Organic Anion Transporter ◽  
Active Components ◽  
Inflammatory Signaling ◽  
Anion Transporter ◽  
Glucose Transporter 9

Abstract Lagotis brachystachya Maxim is an herb widely used in traditional Tibet medicine. Our previous study indicated that total extracts from Lagotis brachystachya could lower uric acid levels. This study aimed to further elucidate the active components (luteolin, luteoloside and apigenin) isolated from Lagotis brachystachya and the underlying mechanism in vitro and vivo. The results showed that treatment with luteolin and luteoloside reversed the reduction of organic anion transporter 1 (OAT1) levels, while apigenin attenuated the elevation of urate transporter 1 (URAT1) and glucose transporter 9 (GLUT9) levels in uric acid-treated HK-2 cells, which were consistent with the finding in the kidney of potassium oxonate (PO)-induced mice. On the other hand, hepatic xanthine oxidase activity was inhibited by the components. In addition, all of these active components improved the morphology of the kidney in hyperuricemic mice. Moreover, molecular docking showed that luteolin, luteoloside and apigenin could bind TLR4 and NLRP3. Consistently, western blot showed that the components inhibited TLR4/MyD88/NLRP3 signaling. In conclusion, these results indicated that luteolin, luteoloside and apigenin could attenuate hyperuricemia by decreasing the production and increasing the excretion of uric acid, which were mediated by the inhibition of inflammatory signaling pathways.

The Potential Migrated Mechanism of Water-Soluble Components in Pellets Prepared by Wet Extrusion/Spheronization: Effect of Drying Rate

2020 ◽  
Vol 17 ◽  
Author(s):  
Bingwei Wang ◽  
Jianping Liu ◽  
Zhenghua Li ◽  
Yulong Xia ◽  
Shuangshuang Zhang ◽  
...  
Keyword(s):  
Relative Humidity ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Drying Rate ◽  
Scanning Calorimetry ◽  
Drying Temperature ◽  
Wet Extrusion ◽  
Extrusion Spheronization ◽  
Soluble Components

Background: At present, there were numerous researches on the migration of components in tablets and granules, the investigation in the pharmaceutical literatrue concerning the effect of drying rate on the migration of water-soluble components of pellets was limited. Temperature and relative humidity (RH) were crucial parameters during the drying process which was an essential step in the preparation of pellets via wet extrusion/spheronization. To quantify these variables, the water loss percentage of pellets per minute was defined as drying rate. Objective: The study aimed to investigate the influence of drying rate on the migration of water-soluble components in wet pellets and the potential migrated mechanism. Methods: The pellets containing tartrazine as a water-soluble model drug and microcrystalline cellulose as a matrix former were prepared by extrusion/spheronization and dried at four different drying temperature and relative humidity. Afterward, the extent of migrated tartrazine was assessed regarding appearance, in-vitro dissolution test, Differential Scanning Calorimetry, X-Ray Powder Diffraction, Attenuated total reflectance Fourier transform infrared spectroscopy and Confocal Raman Mapping. Results: Results demonstrated that red spots of tartrazine appeared on the surface of pellets and more than 40% tartrazine were burst released within 5 minutes when pellets dried at 60℃/RH 10%. While pellets dried at 40℃/RH 80%, none of these aforementioned phenomena was observed. Conclusion: In conclusion, the faster drying rate was, the more tartrazine migrated to the exterior of pellets. Adjusting drying temperature and relative humidity appropriately could inhibit the migration of water-soluble components within wet extrusion/spheronization pellets.

Plasma TS mRNA expression as a potential predictive biomarker for pemetrexed and raltitrexed in gastric cancer.

2012 ◽  
Vol 30 (15_suppl) ◽  
pp. e21034-e21034
Author(s):  
Baorui Liu ◽  
Jie Shen ◽  
Hao Wang ◽  
Jia Wei ◽  
Lixia Yu ◽  
...  
Keyword(s):  
Gastric Cancer ◽  
Mrna Expression ◽  
Predictive Biomarker ◽  
Chemotherapeutic Agents ◽  
Water Soluble ◽  
Expression Level ◽  
Mrna Levels ◽  
Expression Levels ◽  
In Vitro Chemosensitivity

e21034 Background: Plasma mRNA opens up new investigational opportunities and has great potential for use in disease and treatment assessment. Pemetrexed and raltitrexed are novel water-soluble quinazoline folate analogues and act as direct and specific TS inhibitors. Although TS expression levels detected in tumor have shown potential in predicting sensitivity to those two chemotherapeutic agents, current knowledge is limited on the role of plasma TS mRNA as a predictive biomarker. The aim of this study was to investigate the association between plasma TS mRNA expression and in vitro chemosensitivity to pemetrexed and raltitrexed in gastric cancer. Methods: 150 freshly-removed gastric tumor specimens and corresponding blood samples before surgery were collected. Pemetrexed and raltitrexed sensitivity was determined by histoculture drug response assay (HDRA) procedures. Plasma and tumor TS mRNA expression level were determined by quantitative RT-PCR. Results: A significant correlation was observed between plasma and tumor TS mRNA expression levels (rho=0.665, P<0.001). Plasma TS expression level was negatively correlated with in vitro sensitivity to pemetrexed and raltitrexed in gastric cancer (pemetrexed-sensitive sub-group: 0.90, 95% CI: 0.66-1.16; pemetrexed-resistant sub-group: 1.82, 95% CI: 1.38-2.26, P<0.001; raltitrexed-sensitive sub-group: 0.91, 95% CI: 0.64-1.22; raltitrexed-resistant sub-group: 1.62, 95% CI: 1.06-2.17, P=0.013). There was no significant association between clinical characteristics and plasma TS mRNA levels or in vitro chemosensitivity. Conclusions: Our results indicated that plasma TS mRNA expression could be a prominent predictive biomarker for raltitrexed in gastric cancer, enabling the development of ‘‘real-time’’ individualized chemotherapy while tumor progression.

scholarly journals Porcine colonoids and enteroids keep the memory of their origin during regeneration.

2021 ◽  
Author(s):  
Alicia M. Barnett ◽  
Jane A. Mullaney ◽  
Charlotte Hendriks ◽  
Lisa Le Borgne ◽  
Warren C. McNabb ◽  
...  
Keyword(s):  
Gene Expression ◽  
Glucose Transporter ◽  
Expression Profiles ◽  
Cell Types ◽  
Specific Cell ◽  
Stem Cell Markers ◽  
Culture Methods ◽  
Glucose Transporter 1 ◽  
Expression Levels

The development of alternative in vitro culture methods has increased in the last decade as three-dimensional organoids of various tissues, including those of the small and large intestines. Due to their multicellular composition, organoids offer advantages over traditionally used immortalized or primary cell lines. However, organoids must be accurate models of their tissues of origin. This study compared gene expression profiles with respect to markers of specific cell-types (stem-cells, enterocytes, goblet and enteroendocrine cells) and barrier maturation (tight junctions) of colonoid and enteroid cultures with their tissues of origin, and colonoids with enteroids. Colonoids derived from three healthy pigs formed multi-lobed structures with a monolayer of cells similar to the crypt structures in colonic tissue. Colonoid and enteroid gene expression signatures were more similar to those found for the tissues of their origin than to each other. However, relative to their derived tissues, organoids had increased gene expression levels of stem-cell markers Sox9 and Lgr5 encoding Sex determining region Y-box 9 and leucine-rich repeat-containing G-protein coupled rector 5, respectively. In contrast, expression levels of Occl and Zo1 encoding occludin and zonula occludens 1 respectively, were decreased. Expression levels of the cell lineage markers Atoh1, Cga and Muc2 encoding atonal homolog 1, chromogranin A and mucin 2 respectively, were decreased in colonoids, while Sglt1 and Apn encoding sodium-glucose transporter 1 and aminopeptidase A respectively, were decreased in enteroids. These results indicate colonoid and enteroid cultures were predominantly comprised of undifferentiated cell-types with decreased barrier maturation relative to their tissues of origin.

scholarly journals Flavonoids in Benign Prostate Hypertrophy: Identification in Herbal Preparations and Molecular Docking Approach

2021 ◽  
Vol 12 (6) ◽  
pp. 8307-8323
Keyword(s):  
Molecular Docking ◽  
Chlorogenic Acid ◽  
Multiple Reaction Monitoring ◽  
Docking Study ◽  
Term Therapy ◽  
Active Components ◽  
Molecular Docking Study ◽  
Pumpkin Seed ◽  
Herbal Preparations

The benefits of phytotherapy in Benign prostatic hyperplasia (BPH) are of interest where they may lack side effects at long-term therapy. Through plant-derived preparations are Saw palmetto and Pumpkin seed oil. Evidence suggests that fatty acids, phytosterols, tocopherols, and flavonoids are the active components responsible for alleviating BPH symptoms. Flavonoids are reported to inhibit BPH through different mechanisms. Reducing inflammation and lowering reactive oxygen species are amongst the proposed mechanisms. In vitro studies highlighted the role of flavonoids in 5-alpha reductase II (5ARII) inhibitory activity. In this study, herbal preparations known to treat BPH were subjected to LC/MS/MS analysis integrated with multiple reaction monitoring (MRM) to identify the content of flavonoids. A molecular docking study was conducted on the assigned flavonoids to predict the binding mode and interaction with the targeted 3D- crystal structure of the human 5ARII enzyme. Results showed the existence of seven flavonoids and a polyphenol compound. Sakuranetin, Isorhamnetin, and Chlorogenic acid were not reported before. Molecular docking outcomes revealed that Astragalin, Isoquercitrin, Quercetin, and Chlorogenic acid have similar binding affinity to the reference Finasteride compound. These findings suggest flavonoids as potent potential inhibitors of 5ARII and could proceed to in vitro investigations.

Curry Leaf and its Antioxidant Potential: A Systematic Study to Enhance its Activity in Aqueous Medium

2020 ◽  
Vol 16 (3) ◽  
pp. 323-332
Author(s):  
Deepa Kumari ◽  
Tamanna Mallick ◽  
Abhijit Karmakar ◽  
Samiran Mondal ◽  
Sreeparna Das ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Aqueous Medium ◽  
Systematic Study ◽  
Water Soluble ◽  
Active Components ◽  
Chemical Methods ◽  
Lady’S Finger ◽  
Encapsulation Process ◽  
Set Up

Background: We have done a systematic study on the antioxidant activity of the methanol and petroleum ether (60-80°C) extracts (MEC and PEC respectively) of Curry leaves (Murraya koenigii Spreng. Family: Rutaceae) using various in-vitro chemical methods. Methods: Both of these two extracts were found to be highly efficient in the formation of Ag and Au nanoparticles. So, we have explored their ability to form the nanoparticles to study their antioxidant activity. In all the assay systems, MEC showed higher activity over PEC in aqueous medium. This may be due to the higher solubility of MEC and its active components, like polyphenols and flavonoids in the aqueous medium. PEC contains lesser amount of these water soluble active components but PEC was rich in carbazole types of alkaloids which are hydrophobic in nature. So, to enhance the antioxidant activity of PEC and its carbazole constituents, like 2-hydroxy carbazole and mahanimbine, we have encapsulated these in the biopolymeric matrix of the mucilage isolated from an edible vegetable, Abelmoschus esculentus L. (commonly known as Lady's finger, family: Malvaceae). Results: It was interesting to note that, PEC and its carbazole compounds showed better antioxidant activity (ferrous ion chelation and ferric reducing antioxidant activity) in aqueous medium after this encapsulation process. Conclusion: The protocols used in the present study were very simple and can be implemented in any lab set-up. In future, this work can be extended to evaluate antioxidant potentials of other plant based materials.

scholarly journals In vitro and in silico characterization of adiponectin-receptor agonist dipeptides

2021 ◽  
Vol 5 (1) ◽  
Author(s):  
Yuna Lee ◽  
Akihiro Nakano ◽  
Saya Nakamura ◽  
Kenta Sakai ◽  
Mitsuru Tanaka ◽  
...  
Keyword(s):  
Glucose Uptake ◽  
Glucose Transporter ◽  
Adenosine Monophosphate ◽  
Adiponectin Receptor ◽  
L6 Myotubes ◽  
Glut4 Expression ◽  
Binding Pockets ◽  
Dynamics Simulations ◽  
In Silico Characterization

AbstractThe aim of this study is to develop a dipeptide showing an adiponectin receptor 1 (AdipoR1) agonistic effect in skeletal muscle L6 myotubes. Based on the structure of the AdipoR1 agonist, AdipoRon, 15 synthetic dipeptides were targeted to promote glucose uptake in L6 myotubes. Tyr-Pro showed a significant increase in glucose uptake among the dipeptides, while other dipeptides, including Pro-Tyr, failed to exert this effect. Tyr-Pro induces glucose transporter 4 (Glut4) expression in the plasma membrane, along with adenosine monophosphate-activated protein kinase (AMPK) activation. In AdipoR1-knocked down cells, the promotion by Tyr-Pro was ameliorated, indicating that Tyr-Pro may directly interact with AdipoR1 as an agonist, followed by the activation of AMPK/Glut4 translocation in L6 myotubes. Molecular dynamics simulations revealed that a Tyr-Pro molecule was stably positioned in the two potential binding pockets (sites 1 and 2) of the seven-transmembrane receptor, AdipoR1, anchored in a virtual 1-palmitoyl-2-oleoyl-phosphatidylcholine membrane. In conclusion, we demonstrated the antidiabetic function of the Tyr-Pro dipeptide as a possible AdipoR1 agonist.

Molecular Characterization of Two Polysaccharides from Phellinus vaninii Ljup and their Cytotoxicity to Cancer Cell Lines

2019 ◽  
Vol 18 (9) ◽  
pp. 1356-1363
Author(s):  
Xuewei Jia ◽  
Mingqi Gao ◽  
Mingzhe Li ◽  
Yan Wu ◽  
Ying Zeng ◽  
...  
Keyword(s):  
Mtt Assay ◽  
Molecular Conformation ◽  
Sodium Hydroxide Solution ◽  
Fruit Body ◽  
Water Soluble ◽  
Hot Water ◽  
Active Components ◽  
Molecular Conformations ◽  
Chemical Structures

Background: Phellinus vaninii, a medicinal basidiomycete fungus, is often confused with Phellinus igniarius and Phellinus linteus. Polysaccharides extract from P. igniarius and P. linteus are reported to stimulate humoral immunity and inhibit tumor growth However, available literature reviewed no information on the relationship between bioactivities and structures of polysaccharides from the fruit body of P. vaninii. Methods: Two water-soluble polysaccharides (PV-W, PV-B) were isolated and purified from fruiting bodies of P. vaninii by hot water and sodium hydroxide solution, respectively. The chemical structures of PV-W, PV-B were analyzed by FT-IR, GC-MS analysis and 13C NMR spectra. And, their molecular conformations were analyzed by viscosity method and SEC-MALLS-RI. Finally, their inhibition of cancer cells was investigated using MTT assay. Results: The results illustrated that PV-W was a heteropolysaccharide, mainly composed of mannose, glucose, arabinose and galactose. PV-B was a β-1, 3-D-glucan branched with β-1, 6-D-glucose. The results of viscometry proved that PV-W and PV-B could be molecularly dispersed in water without aggregation. The results of SECMALLS- RI indicated that the two polysaccharides had the similar Mw but different molecular conformation. That is, PV-W existed as a stable globular shape, while PV-B presented a more expanded flexible random coils conformation. MTT assay indicated that PV-B showed higher inhibition effect on HepG2 and HeLa cells than PV-W in vitro. Conclusion: This work provided the important information of active components from P. vaninii and its potential applications in the food and medicine industry.

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