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Pei Dawn Lee Chao - One of the best experts on this subject based on the ideXlab platform.
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Original Article Metabolism and Pharmacokinetics of San-Huang-Xie-Xin-Tang, a Polyphenol-Rich Chinese Medicine Formula, in Rats and Ex-Vivo
2013Co-Authors: Antioxidant Activity, Pei Dawn Lee ChaoAbstract:Copyright © 2011 Chi-Sheng Shia et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. San-Huang-Xie-Xin-Tang (SHXXT), a widely used Chinese herbal formula, consists of rhizomes of Rheum officinale, roots of Scutellaria baicalensis and rhizomes of Coptis chinesis. This study investigated the metabolism and pharmacokinetics of polyphenols in SHXXT, including Baicalin, baicalein, wogonin, emodin, aloe-emodin, rhein and chrysophanol. The quantitation methods of SHXXT decoction and rat serum using high performance liquid chromatography were developed and validated in this study. After oral administration of SHXXT decoction to rats, the parent forms of various constituents and their conjugated metabolites in serum were determined before and after hydrolysis with β-glucuronidase and sulfatase. The results showed that only free form of rhein can be quantitated, whereas the parent forms of coptisine, palmatine, berberine, baicalein, wogonin, emodin, aloeemodin and chrysophanol were not detected in serum. The glucuronides of baicalein, wogonin, emodin, aloe-emodin, rhein and chrysophanol were the predominant forms in bloodstream. In order to evaluate the in vivo antioxidant activity of SHXXT, the serum metabolite of SHXXT was prepared, characterized and followed by evaluation of the effect on AAPH-induced hemolysis. The results indicated that metabolites of SHXXT exhibited significant free radical scavenging activity. We suggest that biologist
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flavonoid pharmacokinetics and tissue distribution after repeated dosing of the roots of scutellaria baicalensis in rats
Planta Medica, 2011Co-Authors: Shang Yuan Tsai, Miauhwa Ko, Yunchia Chang, Pei Dawn Lee ChaoAbstract:Scutellariae Radix (root of Scutellaria baicalensis, SR) contains numerous flavonoids such as Baicalin, baicalein, and wogonin. This study investigated the pharmacokinetics and tissue distribution of flavonoids and their metabolites in rats after repeated dosing of a SR decoction. Sprague-Dawley rats were orally administered SR at 2 g/kg for seven doses. After the 7th dose, blood samples were withdrawn at specific times and organs, including the liver, kidney, lung, and brain, and collected. The concentrations of baicalein and wogonin in the serum and various tissues were assayed by HPLC before and after hydrolysis with glucuronidase and sulfatase. Baicalein and wogonin were not detected in the serum, and the molecules found were their glucuronides/sulfates. In tissues, the free forms of baicalein and wogonin appeared in the liver, kidney, and lung in addition to their glucuronides/sulfates. Baicalein was the major form in the lung, whereas baicalein glucuronides/sulfates were the major forms in the liver and kidney. Wogonin was the major form in the liver, kidney, lung, and traces of wogonin glucuronides/sulfates were detected in the kidney and liver. Neither baicalein and wogonin nor their glucuronides/sulfates were detected in the brain. In conclusion, the glucuronides/sulfates of baicalein and wogonin were exclusively present in the circulation, whereas their free forms appeared in the lung, liver, and kidney.
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Metabolism and Pharmacokinetics of San-Huang-Xie-Xin-Tang, a polyphenol-Rich chinese medicine formula, in rats and Ex-Vivo antioxidant activity
Evidence-based Complementary and Alternative Medicine, 2011Co-Authors: Pei Dawn Lee Chao, Yu Chi Hou, Chi Sheng Shia, Shin Hun Juang, Shang Yuan Tsai, Pei Hsun Hsieh, Lu Ching HoAbstract:San-Huang-Xie-Xin-Tang (SHXXT), a widely used Chinese herbal formula, consists of rhizomes of Rheum officinale, roots of Scutellaria baicalensis and rhizomes of Coptis chinesis. This study investigated the metabolism and pharmacokinetics of polyphenols in SHXXT, including Baicalin, baicalein, wogonin, emodin, aloe-emodin, rhein and chrysophanol. The quantitation methods of SHXXT decoction and rat serum using high performance liquid chromatography were developed and validated in this study. After oral administration of SHXXT decoction to rats, the parent forms of various constituents and their conjugated metabolites in serum were determined before and after hydrolysis with β-glucuronidase and sulfatase. The results showed that only free form of rhein can be quantitated, whereas the parent forms of coptisine, palmatine, berberine, baicalein, wogonin, emodin, aloe-emodin and chrysophanol were not detected in serum. The glucuronides of baicalein, wogonin, emodin, aloe-emodin, rhein and chrysophanol were the predominant forms in bloodstream. In order to evaluate the in vivo antioxidant activity of SHXXT, the serum metabolite of SHXXT was prepared, characterized and followed by evaluation of the effect on AAPH-induced hemolysis. The results indicated that metabolites of SHXXT exhibited significant free radical scavenging activity. We suggest that biologists redirect their focus to the bioactivity of the conjugated metabolites of these polyphenols.
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comparison of metabolic pharmacokinetics of Baicalin and baicalein in rats
Journal of Pharmacy and Pharmacology, 2010Co-Authors: Miaoying Lai, Yu Chi Hou, Shang Yuan Tsai, Sulan Hsiu, Pei Dawn Lee ChaoAbstract:Baicalin and baicalein, a flavone glucuronide and its aglycone, are bioactive constituents of Scutellariae Radix with various beneficial activities. We have characterized and compared the metabolic pharmacokinetics of Baicalin and baicalein in rats. Baicalein was administered intravenously and orally to rats, and Baicalin was orally administered. An HPLC method was used to determine the concentration of baicalein before and after hydrolysis using beta-glucuronidase/sulfatase. The pharmacokinetic parameters were calculated by using WINNONLIN. Unpaired Student's t-test was used for statistical comparison. The result showed that after intravenous administration of baicalein, 75.7% of the dose was circulating as its conjugated metabolites. After oral administration of baicalein, absorption of baicalein itself was negligible, whereas the glucuronides/sulfates of baicalein were predominant in the plasma. When compared with intravenous bolus administration with dose correction, the absolute absorption was 40%. When Baicalin was administered orally, glucuronides and sulfates of baicalein were exclusively circulating in the plasma. The relative absorption for Baicalin was 65% when compared with baicalein. Profound differences of serum profile and pharmacokinetics were observed between oral baicalein and Baicalin. Baicalin demonstrated significantly later time to peak concentration (t(max)) and lower peak serum concentration (C(max)) of baicalein conjugated metabolites than baicalein, indicating Baicalin was absorbed more slowly and to a lesser extent than baicalein.
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urinary pharmacokinetics of baicalein wogonin and their glycosides after oral administration of scutellariae radix in humans
Biological & Pharmaceutical Bulletin, 2003Co-Authors: Miaoying Lai, Yu Chi Hou, Sulan Hsiu, Chungchuan Chen, Pei Dawn Lee ChaoAbstract:Baicalin, baicalein, wogonoside and wogonin are flavone constituents of Scutellariae Radix with various beneficial biological activities. The purpose of this study was to investigate the urinary pharmacokinetics of these flavones after oral administration of Scutellariae Radix commercial powder. Ten healthy male volunteers received a dose of 5.2 g commercial powder (comparable to 9 g crude drug), respectively. The concentrations of Baicalin, baicalein and wogonin in the commercial powder as well as their metabolites in urine were assayed by HPLC method. The glucuronides and sulfates of baicalein and wogonin in urine were hydrolyzed with β-glucuronidase and sulfatase, respectively. Our results showed that the mean cumulated renal excretion of baicalein glucuronides and sulfates were 43.1±4.5 μmol (2.9% of dose) and 64.8±6.3 μmol (4.3% of dose), respectively, whereas wogonin glucuronides and sulfates were 21.6±2.0 μmol (5.9% of dose) and 20.7±1.7 μmol (5.7% of dose), respectively. The result indicated that the renal excretion of conjugated metabolites of wogonin (11.6% of dose) were higher than that of baicalein (7.2% of dose). The baicalein sulfates was predominant than the corresponding glucuronides, whereas wogonin sulfates was comparable to the corresponding glucuronides.
Yongshen Ren - One of the best experts on this subject based on the ideXlab platform.
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the comparative study of the therapeutic effects and mechanism of Baicalin baicalein and their combination on ulcerative colitis rat
Frontiers in Pharmacology, 2019Co-Authors: Shuai Liang, Xin Deng, Lei Lei, Yao Zheng, Linlin Chen, Hui Xiong, Zhinan Mei, Yungchi Cheng, Yongshen RenAbstract:Introduction: Ulcerative colitis (UC) is an inflammatory bowel disease with a high incidence rate and a difficult treatment regimen. Recently, significant advances in the treatment of intestinal diseases, particularly UC, have been made with the use of the drugs Baicalin and baicalein, separately or in combination. However, the therapeutic efficacy and mechanism of action of Baicalin, baicalein, and their combination therapy, in the treatment of UC has not been fully elucidated. Materials and Methods: we constructed a UC rat model that encompassed a variety of complex factors, including a high-sugar and high-fat diet, a high temperature and humidity environment (HTHE), excess drinking, and infection of Escherichia coli. Model rats were then treated with Baicalin, baicalein, or a combination of the two. Results: The results showed significant differences in the therapeutic effects of Baicalin, baicalein, and the combination therapy, in the treatment of UC, as well as differences in the inhibition of inflammation via the nuclear factor-κB and MAPK pathways. The rat model of UC was established as described above. Then, the rats were treated for 7 days with Baicalin (100 mg kg-1), baicalein (100 mg kg-1), or both (100 mg kg-1, Baicalin: baicalein = 4:1/1:1). Clinical symptoms and signs, body temperature, organ indices, histopathology, blood biochemistry, and metabolites were examined to compare treatment effects and indicators of UC. Baicalin, YSR (Young Scutellaria baicalensis ratio of Baicalin and baicalein), baicalein, and WSR (Withered Scutellaria baicalensis ratio of Baicalin and baicalein) had significantly different effects in terms of clinical symptoms and signs, body temperature, organ indices, serum inflammatory cytokine levels, blood biochemistry, and histopathology changes in the main organs; YSR exhibited the best treatment effects. LC-MS/MS was used to detect the conversion of Baicalin, baicalein, or both, into the six types of metabolites: Baicalin, wogonoside, oroxin A, baicalein, wogonin, and oroxylin A. The levels of the six metabolites under the different treatment conditions were significantly different in the large intestine, small intestine, and lungs, but not in the blood. The levels of the six metabolites were significantly different in the large intestine, small intestine, and lung, but not in the serum. Conclusion: All these results indicate that Baicalin and baicalein should be used more accurately in specific diseases, especially Baicalin or high content of Baicalin in Scutellaria baicalensis (Tiaoqin) should be preferred in treatment of UC.
Keivan Zandi - One of the best experts on this subject based on the ideXlab platform.
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baicalein and Baicalin as zika virus inhibitors
Archives of Virology, 2019Co-Authors: Boonteong Teoh, Singsin Sam, Keivan Zandi, Sazaly Abu BakarAbstract:At present, there is no effective antiviral agent for Zika virus (ZIKV), an arbovirus that is known for its teratogenic effects on newborns. Baicalein and Baicalin were found to be capable of downregulating ZIKV replication up to 10 hours postinfection, while prophylactic effects were evident in pre-treated cells. Baicalein exhibited its highest potency during intracellular ZIKV replication, whereas Baicalin was most effective against virus entry. Our in silico interaction assays predicted that both compounds exhibited the strongest binding affinities towards ZIKV NS5, while the virus envelope glycoprotein was the least likely target protein. These findings serve as a crucial platform for further in-depth studies to decipher the underlying anti-ZIKV mechanism(s) of each compound.
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Baicalin a metabolite of baicalein with antiviral activity against dengue virus
Scientific Reports, 2015Co-Authors: Ehsan Moghaddam, Boonteong Teoh, Singsin Sam, Rafidah Lani, Pouya Hassandarvish, Zamri Chik, Andrew Yueh, Sazaly Abubakar, Keivan ZandiAbstract:Baicalin, a flavonoid derived from Scutellaria baicalensis, is the main metabolite of baicalein released following administration in different animal models and human. We previously reported the antiviral activity of baicalein against dengue virus (DENV). Here, we examined the anti-DENV properties of Baicalin in vitro, and described the inhibitory potentials of Baicalin at different steps of DENV-2 (NGC strain) replication. Our in vitro antiviral experiments showed that Baicalin inhibited virus replication at IC50 = 13.5 ± 0.08 μg/ml with SI = 21.5 following virus internalization by Vero cells. Baicalin exhibited virucidal activity against DENV-2 extracellular particles at IC50 = 8.74 ± 0.08 μg/ml and showed anti-adsorption effect with IC50 = 18.07 ± 0.2 μg/ml. Our findings showed that Baicalin as the main metabolite of baicalein exerting in vitro anti-DENV activity. Further investigations on baicalein and Baicalin to deduce its antiviral therapeutic effects are warranted.
Shang Yuan Tsai - One of the best experts on this subject based on the ideXlab platform.
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flavonoid pharmacokinetics and tissue distribution after repeated dosing of the roots of scutellaria baicalensis in rats
Planta Medica, 2011Co-Authors: Shang Yuan Tsai, Miauhwa Ko, Yunchia Chang, Pei Dawn Lee ChaoAbstract:Scutellariae Radix (root of Scutellaria baicalensis, SR) contains numerous flavonoids such as Baicalin, baicalein, and wogonin. This study investigated the pharmacokinetics and tissue distribution of flavonoids and their metabolites in rats after repeated dosing of a SR decoction. Sprague-Dawley rats were orally administered SR at 2 g/kg for seven doses. After the 7th dose, blood samples were withdrawn at specific times and organs, including the liver, kidney, lung, and brain, and collected. The concentrations of baicalein and wogonin in the serum and various tissues were assayed by HPLC before and after hydrolysis with glucuronidase and sulfatase. Baicalein and wogonin were not detected in the serum, and the molecules found were their glucuronides/sulfates. In tissues, the free forms of baicalein and wogonin appeared in the liver, kidney, and lung in addition to their glucuronides/sulfates. Baicalein was the major form in the lung, whereas baicalein glucuronides/sulfates were the major forms in the liver and kidney. Wogonin was the major form in the liver, kidney, lung, and traces of wogonin glucuronides/sulfates were detected in the kidney and liver. Neither baicalein and wogonin nor their glucuronides/sulfates were detected in the brain. In conclusion, the glucuronides/sulfates of baicalein and wogonin were exclusively present in the circulation, whereas their free forms appeared in the lung, liver, and kidney.
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Metabolism and Pharmacokinetics of San-Huang-Xie-Xin-Tang, a polyphenol-Rich chinese medicine formula, in rats and Ex-Vivo antioxidant activity
Evidence-based Complementary and Alternative Medicine, 2011Co-Authors: Pei Dawn Lee Chao, Yu Chi Hou, Chi Sheng Shia, Shin Hun Juang, Shang Yuan Tsai, Pei Hsun Hsieh, Lu Ching HoAbstract:San-Huang-Xie-Xin-Tang (SHXXT), a widely used Chinese herbal formula, consists of rhizomes of Rheum officinale, roots of Scutellaria baicalensis and rhizomes of Coptis chinesis. This study investigated the metabolism and pharmacokinetics of polyphenols in SHXXT, including Baicalin, baicalein, wogonin, emodin, aloe-emodin, rhein and chrysophanol. The quantitation methods of SHXXT decoction and rat serum using high performance liquid chromatography were developed and validated in this study. After oral administration of SHXXT decoction to rats, the parent forms of various constituents and their conjugated metabolites in serum were determined before and after hydrolysis with β-glucuronidase and sulfatase. The results showed that only free form of rhein can be quantitated, whereas the parent forms of coptisine, palmatine, berberine, baicalein, wogonin, emodin, aloe-emodin and chrysophanol were not detected in serum. The glucuronides of baicalein, wogonin, emodin, aloe-emodin, rhein and chrysophanol were the predominant forms in bloodstream. In order to evaluate the in vivo antioxidant activity of SHXXT, the serum metabolite of SHXXT was prepared, characterized and followed by evaluation of the effect on AAPH-induced hemolysis. The results indicated that metabolites of SHXXT exhibited significant free radical scavenging activity. We suggest that biologists redirect their focus to the bioactivity of the conjugated metabolites of these polyphenols.
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comparison of metabolic pharmacokinetics of Baicalin and baicalein in rats
Journal of Pharmacy and Pharmacology, 2010Co-Authors: Miaoying Lai, Yu Chi Hou, Shang Yuan Tsai, Sulan Hsiu, Pei Dawn Lee ChaoAbstract:Baicalin and baicalein, a flavone glucuronide and its aglycone, are bioactive constituents of Scutellariae Radix with various beneficial activities. We have characterized and compared the metabolic pharmacokinetics of Baicalin and baicalein in rats. Baicalein was administered intravenously and orally to rats, and Baicalin was orally administered. An HPLC method was used to determine the concentration of baicalein before and after hydrolysis using beta-glucuronidase/sulfatase. The pharmacokinetic parameters were calculated by using WINNONLIN. Unpaired Student's t-test was used for statistical comparison. The result showed that after intravenous administration of baicalein, 75.7% of the dose was circulating as its conjugated metabolites. After oral administration of baicalein, absorption of baicalein itself was negligible, whereas the glucuronides/sulfates of baicalein were predominant in the plasma. When compared with intravenous bolus administration with dose correction, the absolute absorption was 40%. When Baicalin was administered orally, glucuronides and sulfates of baicalein were exclusively circulating in the plasma. The relative absorption for Baicalin was 65% when compared with baicalein. Profound differences of serum profile and pharmacokinetics were observed between oral baicalein and Baicalin. Baicalin demonstrated significantly later time to peak concentration (t(max)) and lower peak serum concentration (C(max)) of baicalein conjugated metabolites than baicalein, indicating Baicalin was absorbed more slowly and to a lesser extent than baicalein.
Zhong Zuo - One of the best experts on this subject based on the ideXlab platform.
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development of a spe lc ms ms method for simultaneous quantification of baicalein wogonin oroxylin a and their glucuronides Baicalin wogonoside and oroxyloside in rats and its application to brain uptake and plasma pharmacokinetic studies
Journal of Pharmaceutical and Biomedical Analysis, 2014Co-Authors: Sophia Yui Kau Fong, Yin Cheong Wong, Zhong ZuoAbstract:Abstract This study aims to identify and quantify the six major bioactive flavones of the traditional Chinese medicine Scutellariae Radix (RS), including baicalein, Baicalin, wogonin, wogonoside, oroxylin A and oroxyloside in rat after oral administration of a standardized RS extract. A novel, sensitive and selective method for simultaneous determination of these six analytes in rat brain and plasma using solid phase extraction-liquid chromatography–tandem mass spectrometry (SPE-LC/MS/MS) was developed and fully validated. The lower limits of quantification (LLOQs) for the six RS flavones in brain tissue were 0.02 nmol/g. The LLOQs in plasma were 0.005 nmol/ml for B, W and OA, 0.025 nmol/ml for WG and OAG, and 0.1875 nmol/ml for BG. The current study provides novel evidence of the presence of all the tested RS flavones and an isoform of BG (BG′, probably baicalein-6-O-glucuronide) in the rat brain after oral administration of RS extract, suggesting their ability to permeate through the blood–brain barrier. The method was also successfully applied to the pharmacokinetic study of all these analytes in plasma after oral administration of RS extract (300 mg/kg) to Sprague-Dawley rats. The developed assay method provides a useful tool for both preclinical and clinical investigations on the disposition of RS flavones in brain and plasma.
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identification and quantification of baicalein wogonin oroxylin a and their major glucuronide conjugated metabolites in rat plasma after oral administration of radix scutellariae product
Journal of Pharmaceutical and Biomedical Analysis, 2011Co-Authors: Li Zhang, Ge Lin, Zhong ZuoAbstract:Abstract The current study aims to identify and quantify three flavones (baicalein, wogonin and oroxylin A) and their major metabolites (Baicalin, wogonoside and oroxylin A-7-O-glucuronide) in rat plasma after oral administration of Radix scutellariae product. A simple HPLC/UV method has been developed to simultaneously determine the three flavones and their major metabolites in rat plasma. The chromatographic separation of the six analytes was achieved by a Thermo C18 column with linear gradient elution of a mobile phase containing acetonitrile and 20 mM sodium dihydrogen phosphate buffer (pH 4.6). All the tested analytes were detected by PDA detector at a wavelength of 320 nm. The intra-day and inter-day precision for the current assay of the six analytes was within the range of −2.23% to 15.13% and −10.83% to 6.42%, respectively. All the studied analytes could be efficiently extracted from the rat plasma using HLB cartridge with extraction recoveries above 70% and were stable under different storage conditions. The developed assay method was successfully applied to the pharmacokinetic study of Baicalin, wogonoside after oral administration of a commercially available Radix scutellariae containing capsule at a dose of 3.2 g/kg to Sprague–Dawley rats. In addition to wogonoside, a new metabolite of wogonin has been identified using LC/MS/MS for the first time.
