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Chunsu Yuan - One of the best experts on this subject based on the ideXlab platform.
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anti migraine effect of wine processed radix Scutellariae pharmacodynamic verification in nitroglycerin induced rats and correlation study between compounds dissolution and the fractal dimension
Journal of Ethnopharmacology, 2020Co-Authors: Wenjun Zhang, Chongzhi Wang, Shuo Zhai, Yuewen Sun, Qiujing Chen, Xiaolin Yang, Chunfeng Zhang, Chunsu YuanAbstract:Abstract Ethnopharmacological relevance Wine-processed Radix Scutellariae (RS) is the processed product of RS, which is the dried root of Scutellaria baicalensis Georgi. It is recorded in Chinese traditional formula that wine-processed RS has the effect of anti-migraine, while the effect has not been confirmed and the possible mechanism remains unclear. Aim of the study To verify the anti-migraine effect of wine-processed RS in nitroglycerin (NTG)-induced rats and explore the correlation between compounds dissolution and the pore structure based on fractal theory. Materials and methods In the validation of pharmacodynamics, the effects of wine-processed RS on migraines were firstly evaluated by observing the number of head-scratching of rats, then investigated by determining the levels of nitric oxide (NO), calcitonin gene-related peptide (CGRP) and the expression of c-Fos in the brain of NTG-induced rat models using ELISA and immunohistochemical assessments. In the correlation study, the stir-frying time of RS was set to 5 min, 10 min and 15 min. The scanning electron microscope (SEM) and mercury intrusion method were used to explore the pore structure and main parameters of the pore structure including pore size distribution, pore volume, porosity, surface area and fractal dimension. The compounds dissolution of total flavonoids and five major components containing baicalein, baicalin, scutellarin, wogonin and wogonoside was determined by UV–Vis spectrophotometry and HPLC separately. Results The animal experiments had shown that wine-processed RS could significantly reduce the head-scratching times of NTG-induced rat models (p fractal dimension (r > 0) and the order of negative correlation was average pore size > total porosity > total volume (r Conclusions Wine-processing could strengthen the anti-migraine effect of RS by changing the pore structure of RS, which is linked to the dissolution of compounds. The RS stir-fried for 10 min may be more effective in treating migraine.
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selective fraction of Scutellaria baicalensis and its chemopreventive effects on mcf 7 human breast cancer cells
Phytomedicine, 2010Co-Authors: Chongzhi Wang, Qianfei Wang, Sangeeta R. Mehendale, Xiaoli Li, Chunsu YuanAbstract:Based on our previous observation, the whole Scutellaria baicalensis extract (SbE) did not show significant breast cancer cell inhibitory effect. In this study, we isolated a baicalin-deprived-fraction (SbF1) of Scutellaria baicalensis, and baicalin-fraction (SbF3), and evaluated their anti-breast cancer properties using MCF-7 cells. The content of four flavonoids in extract/fractions were determined using high performance liquid chromatography. Analytical data showed that in SbF1, the major constituents are baicalein and wogonin, while SbF3 only contains baicalin. The antiproliferative effects of fractions and SbE were assayed using modified trichrome stain method. SbF1 showed significant antiproliferative effect. Treated with 100 μg/ml of SbF1 for 72 h inhibited MCF-7 cell growth by 81.6%, while in the same treatment concentration, SbF3 increased cell growth by 22.6%. SbF1 was recognized as an active fraction of SbE. The effects of four flavonoids in SbE, scutellarin, baicalin, baicalein and wogonin, were determined, and data showed that baicalein and wogonin significantly inhibited MCF-7 cell growth. In contrast, in certain concentrations, scutellarin and baicalin increased cancer cell growth. The effects of SbF1 on cell cycle and apoptosis were assayed using flow cytometry. SbF1 arrested MCF-7 cells in S- and G2/M-phases, and significantly increased induction of cell apoptosis. These combined phytochemical and biological data provide evidence for further chemopreventive studies of the baicalin-deprived SbE on breast cancer.
Jin-ao Duan - One of the best experts on this subject based on the ideXlab platform.
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comparative analysis of 15 chemical constituents in Scutellaria baicalensis stem leaf from different regions in china by ultra high performance liquid chromatography with triple quadrupole tandem mass spectrometry
IEEE Journal of Solid-state Circuits, 2017Co-Authors: Weijie Xu, Huiting Zeng, Shulan Su, Dawei Qian, Ming Zhao, Jin-ao DuanAbstract:Scutellaria baicalensis is a traditional Chinese herbal medicine containing multiple components, which has been extensively used in clinics to treat epidemic febrile disease and hyperactivity cough. To get a deeper understanding about Scutellaria baicalensis stem-leaf resources, we analyzed 15 chemical constituents in 35 batches of Scutellaria baicalensis stem-leaf from eight regions in China. A rapid, simple and sensitive method using ultra high performance liquid chromatography coupled with triple quadrupole electrospray tandem mass spectrometry has been developed for the first time to simultaneously determine 15 chemical constituents (including phenolic acids and flavonoids) in Scutellaria baicalensis stem-leaf. Sufficient separation of 15 target constituents was achieved on a Waters Acquity UPLC BEH C18 (2.1mm × 100 mm, 1.7 μm) column within 14 min under the optimized chromatographic conditions. The established method was validated and showed good linearity, precision, repeatability, stability, and recovery and was successfully applied for the simultaneous determination of the 15 chemical constituents in these samples. Hierarchical clustering analysis and principal components analysis were performed to estimate and classify these samples based on the contents of the 15 chemical constituents. This study provided theoretical basis and scientific evidence for the development and utilization of Scutellaria baicalensis stem-leaf resources. This article is protected by copyright. All rights reserved
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neuroprotective effects of scutellarin and scutellarein on repeatedly cerebral ischemia reperfusion in rats
Pharmacology Biochemistry and Behavior, 2014Co-Authors: Hao Tang, Yuping Tang, Jianming Guo, Erxin Shang, Qianping Shi, Jin-ao DuanAbstract:Scutellarin had protective effects against neuronal injury, however, there are few studies on the protective effect of scutellarein, which is the main metabolite of scutellarin in vivo. This study investigated whether the neural injury by ischemia/reperfusion would be influenced by different doses of scutellarin and scutellarein. Male Wistar rats were orally administered with scutellarin and scutellarein at the doses of 0.09, 0.17, 0.35, 0.70, 1.40 mmol/kg, respectively; then after six consecutive days, they were subjected to global ischemia by occlusion of the bilateral common carotid arteries (BCCAO). After reperfusion for about 21 h, neurological and histological examinations were performed. The present results showed that scutellarein attenuated neuronal cell damage, reduced cerebral water content, regulated the expression of glutamic acid (Glu), aspartic acid (Asp), glycine (Gly), γ-aminobutyric acid (GABA) and taurine (Tau), and improved the Ca(2+)-ATPase and Na(+),K(+)-ATPase activity. Meanwhile, significant difference was found among various doses of scutellarin and scutellarein. Our studies indicated that scutellarin and scutellarein could improve neuronal injury, and scutellarein had better protective effect than scutellarin in rat cerebral ischemia.
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uplc q tof ms for analysis of the metabolites of flavone glycosides from Scutellaria baicalensis georgi by human fecal flora in vitro
Chromatographia, 2013Co-Authors: Dawei Qian, Jin-ao Duan, Shu Jiang, Jianming Guo, Erxin Shang, Jing YangAbstract:The active ingredients of Scutellaria baicalensis Georgi, a valuable traditional Chinese medicine, are polyhydroxyflavones, namely baicalin, scutellarin and wogonoside. However, information about the metabolic routes, metabolites and even more the effect of chemical structure on the stability of the three has been limited. In this article, the three natural compounds were incubated with human fecal flora, respectively, and highly sensitive and specific ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry implementing the MetaboLynx™ software method was used for the drug metabolism study. The chromatographic separation was performed on a 1.7-μm particle size Syncronis C18 column using a gradient elution system. The components in the extract were identified and confirmed according to the mass spectrometric fragmentation mechanisms, MS/MS fragment ions and relevant literature by means of electrospray ionization mass spectrometry in negative ion mode. With this method, a total of ten metabolites were identified based on MS and MS/MS data. The results indicated that hydrogenation, methylation and deglycosylation were the major metabolic pathways of the three flavone glycosides in vitro, and the metabolic stability was closely related to the chemical structure. This study will be helpful for fully understanding the impact of intestinal bacteria on these active components. Furthermore, this work demonstrated the potential of the ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry approach with MetaboLynx for quite rapid, simple, reliable and automated identification of metabolites of natural products.
Xiang Li - One of the best experts on this subject based on the ideXlab platform.
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inhibitory effects against α glucosidase and α amylase of the flavonoids rich extract from Scutellaria baicalensis shoots and interpretation of structure activity relationship of its eight flavonoids by a refined assign score method
Chemistry Central Journal, 2018Co-Authors: Ke Li, Lingguang Yang, Xiang LiAbstract:A flavonoids-rich extract of Scutellaria baicalensis shoots and its eight high content flavonoids were investigated for their inhibitory effects against α-glucosidase and α-amylase. Results show that abilities of the extract in inhibiting the two enzymes were obviously higher than those of acarbose. Moreover, inhibitory abilities of all the eight individual flavonoids against the two enzymes show exactly a same order (i.e., apigenin > baicalein > scutellarin > chrysin > apigenin-7-O-glucuronide > baicalin > chrysin-7-O-glucuronide > isocarthamidin-7-O-glucuronide), and their structure–activity relationship could be well-interpretated by the refined assign-score method. Furthermore, based on the inhibitory abilities and their contents in the extract, it was found that the eight flavonoids made predominant contributions, among which baicalein and scutellarin played roles as preliminary contributors, to overall inhibitory effects of the extract against the two enzymes. Beyond these, contributions of the eight flavonoids to the overall enzyme inhibitory activity were compared with those to the overall antioxidant activity characterized in our recent study, and it could be inferred that within the basic flavonoid structure the hydroxyl on C-4′ of ring B was more effective than that on C-6 of ring A in enzyme inhibitory activities while they behaved inversely in antioxidant activities; scutellarin and apigenin contributed more to the overall enzyme inhibitory activity, and baicalin and scutellarin, to the overall antioxidant activity of the extract; and flavonoids of the extract, apart from directly inhibiting enzymes, might also be conducive to curing type 2 diabetes via scavenging various free radicals caused by increased oxidative stresses.
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structure activity relationship of eight high content flavonoids analyzed with a preliminary assign score method and their contribution to antioxidant ability of flavonoids rich extract from Scutellaria baicalensis shoots
Arabian Journal of Chemistry, 2017Co-Authors: Ke Li, Lingguang Yang, Xiang LiAbstract:Abstract Investigation of flavonoids-rich extract from Scutellaria baicalensis shoots shows that 15 of the 19 flavonoids detected with UPLC-Q-TOF-MS were identified, and it exhibited high antioxidant abilities with IC 50 at 70.81, 35.34 and 33.27 μg/mL in DPPH, ABTS and CAA assays, respectively. An order of antioxidant abilities in scavenging DPPH and ABTS + of eight high content flavonoids in the extract was the same, and it could be well-explained by a preliminary assign-score method we created in structure-activity relationship analyses specific for flavonoids, revealing that double bonds and phenolic hydroxyls on rings A and B are augmentors, and sugar moiety is an attenuator influencing antioxidant capacity but might contribute positively in CAA assays. In addition, three of the eight flavonoids (baicalein, baicalin and scutellarin) made contributions of 58.33%, 60.36% and 51.41% to overall antioxidant activity of the flavonoids-rich extract in DPPH, ABTS and CAA assays, respectively, thus were determined as the primary or marker flavonoids of Scutellaria baicalensis shoots.
Guowei Gong - One of the best experts on this subject based on the ideXlab platform.
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flavonoids are identified from the extract of Scutellariae radix to suppress inflammatory induced angiogenic responses in cultured raw 264 7 macrophages
Scientific Reports, 2018Co-Authors: Guowei Gong, Huaiyou Wang, Xiangpeng Kong, Ran Duan, Tina T X Dong, Karl Wah Keung TsimAbstract:Scutellariae Radix (SR), also named Huangqin in China, is the dried root of Scutellaria baicalensis Georgi. Historically, the usage of SR was targeted to against inflammation. In fact, chronic inflammation has a close relationship with hypoxia and abnormal angiogenesis in tumor cells. Hence, we would like to probe the water extract of SR in suppressing the inflammation-induced angiogenesis. Prior to determine the pharmaceutical values of SR, the first step is to analysis the chemical compositions of SR according to China Pharmacopeia (2015). From the results, the amount of baicalin was 12.6% by weight. Furthermore, the anti-angiogenic properties of SR water extract were evaluated in lipopolysaccharide (LPS) pre-treated cultured macrophage RAW 264.7 cells by detecting the inflammatory markers, i.e. Cox-2, cytokine and iNOS, as well as the translocation activity of NFκB and angiogenic biomarker, i.e. VEGF. This herbal extract was capable of declining both inflammatory and angiogenic hallmarks in a concentration-dependent manner. Moreover, the SR-derived flavonoids, i.e. baicalin, baicalein, wogonin and wogonoside, were shown to be active chemicals in the anti-inflammatory-induced angiogenesis. Therefore, the inflammation-induced angiogenesis is believed to be suppressed by SR water extract, or its major ingredients. These results shed light in the benefiting role of SR in the inflammation-induced angiogenesis in vitro.
Chongzhi Wang - One of the best experts on this subject based on the ideXlab platform.
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anti migraine effect of wine processed radix Scutellariae pharmacodynamic verification in nitroglycerin induced rats and correlation study between compounds dissolution and the fractal dimension
Journal of Ethnopharmacology, 2020Co-Authors: Wenjun Zhang, Chongzhi Wang, Shuo Zhai, Yuewen Sun, Qiujing Chen, Xiaolin Yang, Chunfeng Zhang, Chunsu YuanAbstract:Abstract Ethnopharmacological relevance Wine-processed Radix Scutellariae (RS) is the processed product of RS, which is the dried root of Scutellaria baicalensis Georgi. It is recorded in Chinese traditional formula that wine-processed RS has the effect of anti-migraine, while the effect has not been confirmed and the possible mechanism remains unclear. Aim of the study To verify the anti-migraine effect of wine-processed RS in nitroglycerin (NTG)-induced rats and explore the correlation between compounds dissolution and the pore structure based on fractal theory. Materials and methods In the validation of pharmacodynamics, the effects of wine-processed RS on migraines were firstly evaluated by observing the number of head-scratching of rats, then investigated by determining the levels of nitric oxide (NO), calcitonin gene-related peptide (CGRP) and the expression of c-Fos in the brain of NTG-induced rat models using ELISA and immunohistochemical assessments. In the correlation study, the stir-frying time of RS was set to 5 min, 10 min and 15 min. The scanning electron microscope (SEM) and mercury intrusion method were used to explore the pore structure and main parameters of the pore structure including pore size distribution, pore volume, porosity, surface area and fractal dimension. The compounds dissolution of total flavonoids and five major components containing baicalein, baicalin, scutellarin, wogonin and wogonoside was determined by UV–Vis spectrophotometry and HPLC separately. Results The animal experiments had shown that wine-processed RS could significantly reduce the head-scratching times of NTG-induced rat models (p fractal dimension (r > 0) and the order of negative correlation was average pore size > total porosity > total volume (r Conclusions Wine-processing could strengthen the anti-migraine effect of RS by changing the pore structure of RS, which is linked to the dissolution of compounds. The RS stir-fried for 10 min may be more effective in treating migraine.
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selective fraction of Scutellaria baicalensis and its chemopreventive effects on mcf 7 human breast cancer cells
Phytomedicine, 2010Co-Authors: Chongzhi Wang, Qianfei Wang, Sangeeta R. Mehendale, Xiaoli Li, Chunsu YuanAbstract:Based on our previous observation, the whole Scutellaria baicalensis extract (SbE) did not show significant breast cancer cell inhibitory effect. In this study, we isolated a baicalin-deprived-fraction (SbF1) of Scutellaria baicalensis, and baicalin-fraction (SbF3), and evaluated their anti-breast cancer properties using MCF-7 cells. The content of four flavonoids in extract/fractions were determined using high performance liquid chromatography. Analytical data showed that in SbF1, the major constituents are baicalein and wogonin, while SbF3 only contains baicalin. The antiproliferative effects of fractions and SbE were assayed using modified trichrome stain method. SbF1 showed significant antiproliferative effect. Treated with 100 μg/ml of SbF1 for 72 h inhibited MCF-7 cell growth by 81.6%, while in the same treatment concentration, SbF3 increased cell growth by 22.6%. SbF1 was recognized as an active fraction of SbE. The effects of four flavonoids in SbE, scutellarin, baicalin, baicalein and wogonin, were determined, and data showed that baicalein and wogonin significantly inhibited MCF-7 cell growth. In contrast, in certain concentrations, scutellarin and baicalin increased cancer cell growth. The effects of SbF1 on cell cycle and apoptosis were assayed using flow cytometry. SbF1 arrested MCF-7 cells in S- and G2/M-phases, and significantly increased induction of cell apoptosis. These combined phytochemical and biological data provide evidence for further chemopreventive studies of the baicalin-deprived SbE on breast cancer.
