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Huibi Xu - One of the best experts on this subject based on the ideXlab platform.
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effects of flavonoids extracted from scutellaria baicalensis georgi on hemin nitrite h2o2 induced liver injury
European Journal of Pharmacology, 2006Co-Authors: Yuling Zhao, Hailing Li, Yuefa Gong, Huibi XuAbstract:Abstract Hemin–nitrite–H2O2 system may play a role in liver oxidative injury in some pathological events. In this paper, the effects of the three active components of the root of Scutellaria baicalensis Georgi, i.e. baicalin, Baicalein and wogonin, on hemin–nitrite–H2O2 induced liver injury were studied in liver homogenate, liver microsome and human hepatoblastoma cell line HepG2 cells. It was found that hemin–nitrite–H2O2 could induce liver homogenate protein nitration, lipid peroxidation and liver microsome protein oxidation; it also caused a decrease of HepG2 cells viability. Baicalein, baicalin and wogonin could inhibit protein nitration and lipid peroxidation in liver homogenate as well as in HepG2 cells in a dose-dependent manner, the inhibition order was Baicalein > baicalin ≫ wogonin. These three flavonoids also inhibited the oxidation of protein in liver microsome, the decrease of cell viability and the content of GSH in HepG2 cells, among which baicalin represented the most inhibitory effect. Besides, hemin–H2O2 induced cell injury could be augmented with the existence of nitrite, indicating protein nitration involved in hemin–nitrite–H2O2 induced liver injury. These results demonstrated hemin–nitrite–H2O2 could induce liver injury through oxidizing or nitrating different biomolecules. Baicalein, baicalin and wogonin could inhibit hemin–nitrite–H2O2 induced liver injury in dose-dependent manners by inhibiting oxidation and nitration.
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protective effects of flavonoids in the roots of scutellaria baicalensis georgi against hydrogen peroxide induced oxidative stress in hs sy5y cells
Pharmacological Research, 2001Co-Authors: Kaixun Huang, Huibi XuAbstract:Abstract Oxidative stress plays an important role in the pathological process of neurodegenerative diseases. The effects of four major flavonoids present in Scutellaria baicalensis Georgi on hydrogen peroxide-induced neuronal cell damage are studied in this paper. When human neuroblastoma SH-SY5Y cells were incubated in Hanks’ solution with the addition of 400 μ M hydrogen peroxide for 2 h, the viability of cells was decreased remarkably, while the cell lipid peroxidation and the percentage of lactose dehydrogenase released into the culture medium was significantly increased. Addition of 10 μ M of Baicalein and baicalin significantly attenuated the cellular injury induced by hydrogen peroxide, while the effect of wogonin was marginal and wogonoside showed no effect at the tested concentration. In a separate experiment, 10 μ M of Baicalein and baicalin also antagonized the intracellular free-calcium concentration ( [ Ca 2+ ] i ) increase caused by 1 mM hydrogen peroxide. The effects of Baicalein in both experiments were similar to those of quercetin, a well-studied antioxidant flavonoid. These results demonstrated the protective effects of flavonoids originating from Scutellaria baicalensis Georgi on the oxidative injury of neuronal cells.
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free radical scavenging and antioxidant activities of flavonoids extracted from the radix of scutellaria baicalensis georgi
Biochimica et Biophysica Acta, 1999Co-Authors: Kaixun Huang, Xiangliang Yang, Huibi XuAbstract:Free radical scavenging and antioxidant activities of Baicalein, baicalin, wogonin and wogonoside, the four major flavonoids in the radix of Scutellaria baicalensis Georgi, were examined in different systems. ESR results showed that Baicalein and baicalin scavenged hydroxyl radical, DPPH radical and alkyl radical in a dose-dependent manner, while wogonin and wogonoside showed subtle or no effect on these radicals. Ten μmol/l of Baicalein and baicalin effectively inhibited lipid peroxidation of rat brain cortex mitochondria induced by Fe2+-ascorbic acid, AAPH or NADPH, while wogonin and wogonoside showed significant effects only on NADPH-induced lipid peroxidation. In a study on cultured human neuroblastoma SH-SY5Y cells system, it was found that 10 μmol/l of Baicalein and baicalin significantly protected cells against H2O2-induced injury. Baicalein was the most effective antioxidant among the four tested compounds in every system due to its o-tri-hydroxyl structure in the A ring. Compared with a well-known flavonoid, quercetin, the antioxidant activity of Baicalein was lower in DPPH or AAPH system, but a little higher in those systems which might associate with iron ion. These results suggest that flavonoids in the radix of Scutellaria baicalensis with o-di-hydroxyl group in A the ring, such as Baicalein and baicalin, could be good free radical scavengers and might be used to cure head injury associated with free radical assault.
Lingling Yang - One of the best experts on this subject based on the ideXlab platform.
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wogonin baicalin and Baicalein inhibition of inducible nitric oxide synthase and cyclooxygenase 2 gene expressions induced by nitric oxide synthase inhibitors and lipopolysaccharide
Biochemical Pharmacology, 2001Co-Authors: Yenchou Chen, Shing Chuan Shen, Lih Geeng Chen, Tony J F Lee, Lingling YangAbstract:We previously reported that oroxylin A, a polyphenolic compound, was a potent inhibitor of lipopolysaccharide (LPS)-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). In the present study, three oroxylin A structurally related polyphenols isolated from the Chinese herb Huang Qui, namely baicalin, Baicalein, and wogonin, were examined for their effects on LPS-induced nitric oxide (NO) production and iNOS and COX-2 gene expressions in RAW 264.7 macrophages. The results indicated that these three polyphenolic compounds inhibited LPS-induced NO production in a concentration-dependent manner without a notable cytotoxic effect on these cells. The decrease in NO production was in parallel with the inhibition by these polyphenolic compounds of LPS-induced iNOS gene expression. However, these three compounds did not directly affect iNOS enzyme activity. In addition, wogonin, but not baicalin or Baicalein, inhibited LPS-induced prostaglandin E2 (PGE2) production and COX-2 gene expression without affecting COX-2 enzyme activity. Furthermore, N-nitro-L-arginine (NLA) and N-nitro-L-arginine methyl ester (L-NAME) pretreatment enhanced LPS-induced iNOS (but not COX-2) protein expression, which was inhibited by these three polyphenolic compounds. Wogonin, but not baicalin or Baicalein, similarly inhibited PGE2 production and COX-2 protein expression in NLA/LPS or L-NAME/LPS-co-treated RAW 264.7 cells. These results indicated that co-treatment with NOS inhibitors and polyphenolic compounds such as wogonin effectively blocks acute production of NO and, at the same time, inhibits expression of iNOS and COX-2 genes.
Kaishun Bi - One of the best experts on this subject based on the ideXlab platform.
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simultaneous determination of baicalin wogonoside Baicalein wogonin oroxylin a and chrysin of radix scutellariae extract in rat plasma by liquid chromatography tandem mass spectrometry
Journal of Pharmaceutical and Biomedical Analysis, 2012Co-Authors: Ling Tong, Lihua Zhang, Kaishun BiAbstract:Abstract A liquid chromatography tandem mass spectrometry (LC–MS/MS) method was developed for the simultaneous determination of baicalin, wogonoside, Baicalein, wogonin, oroxylin A and chrysin in rat plasma, using naringin as an internal standard. After acidifying with HCl, plasma samples were pretreated by liquid–liquid extraction with acetone. Chromatographic separation was accomplished on a Hypersil Gold-C 18 analytical column (2.1 × 150 mm, 5 μm) utilizing a gradient elution profile and a mobile phase consisting of (A) 0.1% formic acid in water and (B) acetonitrile. Detection was performed by multiple reaction monitoring (MRM) mode using electrospray ionization in the positive ion mode. All analytes showed good linearity over the investigated concentration range ( r > 0.9900). The lower limit of quantification was 0.5 ng/ml for baicalin, wogonoside, wogonin and oroxylin A, and 1.0 ng/ml for Baicalein and chrysin. Intra-day and inter-day precisions (RSD%) were less than 15% and accuracy (RE%) ranged from −6.7% to 5.8%. The validated method was successfully applied to investigate the pharmacokinetics of the major flavonoids of Radix scutellariae extract after oral administration to rats.
Chunsu Yuan - One of the best experts on this subject based on the ideXlab platform.
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colon cancer chemopreventive effects of Baicalein an active enteric microbiome metabolite from baicalin
International Journal of Oncology, 2015Co-Authors: Chongzhi Wang, Chunfeng Zhang, Lina Chen, Samantha Anderson, Chunsu YuanAbstract:Baicalin is a major constituent of Scutellaria baicalensis, which is a commonly used herbal medicine in many Asian countries. After oral ingestion, intestinal microbiota metabolism may change parent compound's structure and its biological activities. However, whether baicalin can be metabolized by enteric microbiota and the related anticancer activity is not clear. In this study, using human enteric microbiome incubation and HPLC analysis, we observed that baicalin can be quickly converted to Baicalein. We compared the antiproliferative effects of baicalin and Baicalein using a panel of human cancer cell lines, including three human colorectal cancer (CRC) cell lines. In vitro antiproliferative effects on CRC cells were verified using an in vivo xenograft nude mouse model. Baicalin showed limited antiproliferative effects on some of these cancer cell lines. Baicalein, however, showed significant antiproliferative effects in all the tested cancer cell lines, especially on HCT-116 human colorectal cancer cells. In vivo antitumor results supported our in vitro data. We demonstrated that Baicalein exerts potent S phase cell cycle arrest and pro-apoptotic effects in HCT-116 cells. Baicalein induced the activation of caspase 3 and 9. The in silico modeling suggested that Baicalein forms hydrogen bonds with residues Ser251 and Asp253 at the active site of caspase 3, while interactions with residues Leu227 and Asp228 in caspase 9 through its hydroxyl groups. Data from this study suggested that Baicalein is a potent anticancer metabolite derived from S. baicalensis. Enteric microbiota play a key role in the colon cancer chemoprevention of S. baicalensis.
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pretreatment of baicalin and wogonoside with glycoside hydrolase a promising approach to enhance anticancer potential
Oncology Reports, 2013Co-Authors: Chunhao Yu, Chunsu Yuan, Zhiyu Zhang, Haijiang Zhang, Zhong Zhen, Tyler Calway, Yunwei Wang, Chongzhi WangAbstract:Previous phytochemical studies showed that the major flavonoids in Scutellaria baicalensis are baicalin, Baicalein, wogonoside and wogonin. The two glycosides (baicalin and wogonoside) can be transformed into their aglycons (Baicalein and wogonin), which possess positive anticancer potential. In this study, we used glycosidase to catalyze flavonoids in S. baicalensis to enhance the herb’s anticancer activities. Our HPLC data showed that, using the optimized conditions obtained in our experiments (20 U/g of cellulase, 50oC, pH 4.8 and treatment for 8 h), there was a marked transformation from the two glycosides to their aglycons. The anticancer activity was subsequently evaluated using a series of S. baicalensis extracts in which variable lengths of glycosidase treatment time were used. Combining analytical and bioassay results, we observed that the higher the aglycon content, the stronger the antiproliferation effects. Compared to the untransformed control, 8 h of glycosidase catalyzing significantly increased antiproliferative activity on human colorectal and breast cancer cells, and its cancer cell growth inhibition is, in part, mediated by cell cycle arrest at the S-phase and induction of apoptosis. Data from this study suggest that using glycosidase to catalyze S. baicalensis offers a promising approach to increase its anticancer activity.
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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.
Wansheng Chen - One of the best experts on this subject based on the ideXlab platform.
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simultaneous determination of baicalin Baicalein wogonin berberine palmatine and jatrorrhizine in rat plasma by liquid chromatography tandem mass spectrometry and application in pharmacokinetic studies after oral administration of traditional chinese
Journal of Pharmaceutical and Biomedical Analysis, 2010Co-Authors: Jin Feng, Wen Xu, Bo Jiang, Wansheng ChenAbstract:Abstract A sensitive, rapid and selective liquid chromatography–tandem mass spectrometry (LC–MS–MS) method was developed and validated for the simultaneous determination of baicalin, Baicalein, wogonin, berberine, palmatine and jatrorrhizine in scutellaria–coptis herb couple in rat plasma. After protein precipitation with acetonitrile and 0.1% NaH 2 PO 4 , chromatography was performed using a C 18 column, with gradient elution with 0.1% formic acid and acetonitrile at 0.25 ml/min. All analytes including internal standards were monitored under positive ionization conditions by selected reaction monitoring with an electrospray ionization source. The lower limit of quantification was 10 ng/ml for baicalin, Baicalein and wogonin, and 0.6 ng/ml for berberine, palmatine and jatrorrhizine. The validated method was applied in pharmacokinetic studies after oral administration of Yiqing Capsule and Gegen-Qinlian Tablet to rats.
