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Xiao-Min Dai, Dong-Ni Cui, Jing Wang, Wei Zhang, Zun-Jian Zhang, Feng-Guo Xu
The quality control research of traditional Chinese medicine (TCM) is lagged far behind the space of progress in modernization and globalization. Thus the concept of quality marker (Q-marker) was proposed recently to guide the quality investigations of TCM. However, how to discover and validate the Q-marker is still a challenge. In this paper, a system pharmacology based strategy was proposed to discover Q-marker of HuangQin decoction (HQD) to attenuate Intestinal Damage. Using this strategy, nine measurable compounds including paeoniflorin, baicalin, scutellarein, liquiritigenin, norwogonin, baicalein, glycyrrhizic acid, wogonin, and oroxylin A were screened out as potential markers...
2018: Frontiers in Pharmacology
Qing Zhang, Danhua Cong, Dongchen An, Ali Fan, Qi Liu, Yingyue Yi, Zhongjin Song, Xijing Chen, Yang Lu, Di Zhao, Ling He
Targeting therapy of anti-cancer drugs has been gaining increasing attention. Cell pharmacokinetics have been used for in vitro disposition evaluation, as well as drug-drug interaction for anti-cancer drugs, revealing their fate after entering tumor. Flavonoid compound oroxylin A (OA) possesses strong anti-cancer effects especially on the liver and breast cancer. However, despite the low bioavailability, the disposition of OA and its active metabolite in the target cancer cells remained unclear. In current study, a highly sensitive and selective solid phase extraction (SPE)-UPLC-MS/MS method was developed and validated to simultaneously quantify the concentrations of OA and its major active metabolite oroxylin A 7-O-d-glucuronide (OG) in HepG2 cell lysate and multiple subcellular organelle fractions...
March 11, 2018: Journal of Pharmaceutical and Biomedical Analysis
François Chassagne, Mohamed Haddad, Aurélien Amiel, Chiobouaphong Phakeovilay, Chanthanom Manithip, Geneviève Bourdy, Eric Deharo, Guillaume Marti
Liver cancer is a major health burden in Southeast Asia, and most patients turn towards the use of medicinal plants to alleviate their symptoms. The aim of this work was to apply to Southeast Asian plants traditionally used to treat liver disorders, a successive ranking strategy based on a comprehensive review of the literature and metabolomic data in order to relate ethnopharmacological relevance to chemical entities of interest. We analyzed 45 publications resulting in a list of 378 plant species, and our point system based on the frequency of citation in the literature allowed the selection of 10 top ranked species for further collection and extraction...
February 23, 2018: Fitoterapia
Huanhuan Jin, Naqi Lian, Mianli Bian, Chenxi Zhang, Xingran Chen, Jiangjuan Shao, Li Wu, Anping Chen, Qinglong Guo, Feng Zhang, Shizhong Zheng
Accumulating data reveal that oroxylin A has beneficial effects against chronic liver disease. The previously studies showed oroxylin A, a flavonoid extracted from Scutellariae radix, improved acute liver injury and accelerated liver regeneration in vivo. However, it's unclear that the effect of oroxylin A on alcoholic liver disease. The present study was aimed at elucidating the effect of oroxylin A on alcohol-induced hepatic steatosis and the underlying mechanisms. Human hepatocyte LO2 were cultured and stimulated with ethanol for inducing LO2 damage...
April 1, 2018: Chemico-biological Interactions
Shanoo Suroowan, Fawzi Mahomoodally
BACKGROUND: Common auto-inflammatory disorders (CAIDs) constitute a wide array of ailments ranging from acute allergies to chronic conditions. Globally, CAIDs remain one of the leading causes of disability and morbidity. Despite playing a leading therapeutic role, the vast profusion of anti-inflammatory synthetic agents have not been able to fully resolve a panoply of CAIDs. Additionally, contemporary synthetic therapy approaches remain bounded by a wide array of limitations essentially being adverse effects and unaffordable costs...
2018: Combinatorial Chemistry & High Throughput Screening
Weiwei Chen, Zili Zhang, Zhen Yao, Ling Wang, Feng Zhang, Jiangjuan Shao, Anping Chen, Shizhong Zheng
Liver fibrosis is a reversible pathophysiological process correlated with intense repair and cicatrization mechanisms, and its end-stage cirrhosis is responsible for high morbidity and mortality worldwide. Interestingly, the use of natural products as a realistic option for the treatment of liver fibrosis has broadly been accepted. Oroxylin A, a safe and natural product, shows a wide range of pharmacological activities such as anti-inflammatory, anti-oxidant, and anti-tumor properties. However, the effects of Oroxylin A on liver fibrosis remain poorly understood...
March 2018: International Immunopharmacology
Hui Li, Na Lu, Xiaoxuan Yu, Xiao Liu, Po Hu, Yu Zhu, Le Shen, Jingyan Xu, Zhiyu Li, Qinglong Guo, Hui Hui
Tumor necrosis factor alpha (TNFα) is a complicated cytokine which is involved in proliferation and differentiation of acute myelogenous leukemia (AML) cells through a poorly understood mechanism. Mechanistic studies indicate that TNFα induced binding of PI3K subunit p85α to N-terminal truncated nuclear receptor RXRα (tRXRα) proteins, and activated AKT. The activated PI3K/AKT pathway negatively regulated differentiation of AML cells through the up-regulation of c-Myc. In addition, TNFα also induced activation of nuclear factor κB (NF-κB), a nuclear transcription factor which was shown to promote cell proliferation...
January 13, 2018: Carcinogenesis
Huanhuan Jin, Naqi Lian, Mianli Bian, Chenxi Zhang, Xingran Chen, Jiangjuan Shao, Li Wu, Anping Chen, Qinglong Guo, Feng Zhang, Shizhong Zheng
OBJECTIVES: Oroxylin A, a natural flavonoid isolated from Scutellaria baicalensis, has been reported to have anti-hepatic injury effects. However, the effects of oroxylin A on alcoholic liver disease (ALD) remains unclear. The aim of this study was to elucidate the effects of oroxylin A on ALD and the potential mechanisms. MATERIALS AND METHODS: Male ICR mice and human hepatocyte cell line LO2 were used. Yes-associated protein (YAP) overexpression and knockdown were achieved using plasmid and siRNA technique...
January 10, 2018: Cell Proliferation
Xuelin Zhou, Haotian Li, Zhilong Shi, Sijia Gao, Shizhang Wei, Kun Li, Jiabo Wang, Jianyu Li, Ruilin Wang, Man Gong, Yanling Zhao, Xiaohe Xiao
Huang-Lian-Jie-Du-Tang (HLJDT), a traditional formula with four TCM herbs, has been used for hundred years for different diseases. The current study aimed to assess the inhibitory activity of HLJDT against H1N1 neuraminidase (NA-1), and identify potent NA-1 inhibitors from its plasma profile. The in vitro NA-1 study has shown that the water extract of HLJDT potently inhibited NA-1 (IC50  = 112.6 μg/ml; Ki = 55.6 μg/ml) in a competitive mode. The IC50 values of the water extracts of its four herbs were as follows: Coptidis Rhizoma, 96...
November 14, 2017: Scientific Reports
Jing Jin, Shuo Chen, Dechuan Wang, Yuanjin Chen, Yuxu Wang, Min Guo, Changlin Zhou, Jie Dou
Because it is highly contagious, the influenza A virus (IAV) has the potential to cause pandemics in humans. The emergence of drug-resistant strains requires the development of new chemical therapeutics. Oroxylin A (OA) is a flavonoid which has been shown to have antioxidant and antitumor effects. However, intensive studies in which OA fights against different influenza virus strains and the underlying antiviral mechanisms have not been reported. In our study, the antiviral activities in cells and in mice, the preliminary mechanisms of OA were investigated...
January 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Qing-Tong Han, Kai Xiao, Yun Cai, Sheng-Jun Dai
By means of preparative HPTLC and column chromatography over silica gel and Sephadex LH-20, nineteen flavonoids were isolated and purified from the whole plants of Scutellaria moniliorrhiza. Based on the physico-chemical properties and spectral data, their structures were identified as: apigenin (1), luteolin (2), wogonin (3), oroxylin A (4), 6-methoxynaringein (5), 5,7,4'-trihydroxy-6,8-dimethoxyflavone (6), 5,7,8-trimethoxyflavone (7), 3,5,6,7-tetramethoxyflavone (8), 7-hydroxy-4',5,6,8-tetramethoxyflavone (9), 5,7,2'-trihydroxy-6-methoxyflavanone (10), 5,7,4'-trihydroxy-6-methoxyflavone (11), 5,7-dihydroxy-6,8-dimethoxy -flavone (12), 5,2',6'-trihydroxy-7,8-dimethoxyflavone (13), 5,7,2'-trihydroxy-8-methoxyflavone (14), 5,2'-dihydroxy-7,8-dimethoxyflavanone (15), 2'-hydroxy-5,7,8-trimethoxyflavone (16), 5-hydroxy-7,8-dimethoxyflavone (17), 5,2'-dihydroxy-7,8-dimethoxyflavone (18), and 5-hydroxy-6,7,8-trimethoxyflavone (19)...
May 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Cui Li, Siyu Liu, Gan Luo, Guohua Wang, Baoxian Zhang, Qixia Nie
A rapid ultra high performance liquid chromatography tandem mass spectrometry method was developed for the simultaneous analysis of baicalin, oroxylin A-7-O-β-d-glucoronide and chlorogenic acid in rats plasma, and applied to comparison of pharmacokinetics of Tanreqing solution between intratracheal aerosolization and intravenous injection. Results of the analytical method validation assay showed high sensitivity, accuracy and suitable recovery. Results of pharmacokinetics showed similar decline phases for baicalin, oroxylin A-7-O-β-d-glucoronide and chlorogenic acid in two different delivery routes...
March 2018: Biomedical Chromatography: BMC
Wei Zhou, Xiuting Liu, Xin Zhang, Jingjing Tang, Zhiyu Li, Qing Wang, Rong Hu
NLRP3 inflammasome is a novel therapeutic target for inflammatory bowel disease (IBD). The aim of this study was to investigate the anti-inflammatory effect of a bioactive flavonoid-oroxylin A on the treatment of dextran sulfate sodium (DSS)-induced murine colitis via targeting NLRP3 inflammasome. In this study, we found that oroxylin A attenuated experimental colitis in mice, including loss of body weights, shortening of the colon lengths and infiltration of inflammatory cells. The production of IL-1β, IL-6 and TNF-α in colon was also markedly reduced by oroxylin A...
August 29, 2017: Oncotarget
Kai Zhao, Xiaorui Li, Binyan Lin, Dawei Yang, Yuxin Zhou, Zhiyu Li, Qinglong Guo, Na Lu
Increasing flavonoids have been reported to possess anti-angiogenic effects. Inhibition of angiogenesis plays a critical role in the treatment of cancer, especially in advanced metastatic cancer. In this study, we assessed the effect of Oroxylin A-7-glucuronide (Oroxyloside), a main metabolite of Oroxylin A, on angiogenesis in human endothelial cell-like EA.hy926 cells. Oroxyloside suppressed the migration and tube formation of EA.hy926 cells. Meanwhile, microvessels sprouting from aortic rings and new blood vessels on the chicken chorioallantoic membrane (CAM) were also inhibited...
April 2018: Journal of Cellular Physiology
Tomofumi Shimizu, Nobuhiko Shibuya, Yuji Narukawa, Naohiro Oshima, Noriyasu Hada, Fumiyuki Kiuchi
Scutellaria root, the root of Scutellaria baicalensis Georgi, is a crude drug used for inflammatory diseases. In our previous report, the combination of flavonoids contained in Scutellaria root have been found to inhibit PGE2 production more strongly than individual flavonoids. Here, to investigate the mechanism of the synergistic effect, we examined the effects of an equimolar mixture (F-mix) of baicalein (1), wogonin (2) and oroxylin A (3) on the production of PGE2 in LPS-treated J774.1 cells. Although 1 and 3 inhibited COX-2 activity, the F-mix showed no synergistic effect on COX-2 inhibition...
January 2018: Journal of Natural Medicines
Chenxi Zhang, Mianli Bian, Xingran Chen, Huanhuan Jin, Shifeng Zhao, Xiang Yang, Jiangjuan Shao, Anping Chen, Qinglong Guo, Feng Zhang, Shizhong Zheng
Angiogenesis of liver sinusoidal endothelial cells (LSECs) accompanies with hypoxia in liver fibrosis and they are of mutual promotion, which has raised wide concern. Here we established murine model of liver fibrosis and found that oroxylin A (40 mg/kg) could ameliorate angiogenesis in liver fibrosis may related to hypoxia inducible factor 1α (HIF-1α). The underlying mechanism was further investigated by isolating and culturing murine primary LSECs. Hypoxia induced vascular endothelial growth factor A (VEGF-A), angiopoietin 2 (Ang-2), and platelet endothelial cell adhesion molecule-1 (PECAM-1/CD31) elevated in LSECs were reduced by oroxylin A or acriflavine (ACF, an HIF-1α inhibitor), indicating HIF-1α involved the angiogenesis of LSECs...
February 2018: Journal of Cellular Biochemistry
Wei Zhou, Xiuting Liu, Xin Zhang, Jingjing Tang, Zhiyu Li, Qing Wang, Rong Hu
Oroxylin A inhibits colitis by inactivating NLRP3 inflammasome.
July 22, 2017: Oncotarget
Liping Wang, Haotian Duan, Jiebing Jiang, Jiakun Long, Yingjia Yu, Guiliang Chen, Gengli Duan
A new, simple, and fast infrared-assisted self enzymolysis extraction (IRASEE) approach for the extraction of total flavonoid aglycones (TFA) mainly including baicalein, wogonin, and oroxylin A from Scutellariae Radix is presented to enhance extraction yield. Extraction enzymolysis temperature, enzymolysis liquid-to-solid ratio, enzymolysis pH, enzymolysis time and infrared power, the factors affecting IRASEE procedure, were investigated in a newly designed, temperature-controlled infrared-assisted extraction (TC-IRAE) system to acquire the optimum analysis conditions...
September 2017: Analytical and Bioanalytical Chemistry
Libin Wei, Yuanyuan Dai, Yuxin Zhou, Zihao He, Jingyue Yao, Li Zhao, Qinglong Guo, Lin Yang
Liver cancer is the second cause of death from cancer worldwide, without effective treatment. Traditional chemotherapy for liver cancer has big side effects for patients, whereas targeted drugs, such as sorafenib, commonly have drug resistance. Oroxylin A (OA) is the main bioactive flavonoids of Scutellariae radix, which has strong anti-hepatoma effect but low toxicity to normal tissue. To date, no differentiation-inducing agents have been reported to exert a curative effect on solid tumors. Here our results demonstrated that OA restrained the proliferation and induced differentiation of hepatoma both in vitro and in vivo, via inducing a high PKM1 (pyruvate kinase M1)/PKM2 (pyruvate kinase M2) ratio...
July 20, 2017: Cell Death & Disease
Hang Yu, Jae-Sang Chang, Sun Young Kim, Yoon G Kim, Hoo-Kyun Choi
Baicalein, wogonin, and oroxylin A are three major hydrophobic components in the extract of Radix scutellariae with wide spectrum of pharmacological applications. The purpose of this study was to enhance the solubility, dissolution rate and stability of baicalein, wogonin and oroxylin A by solid dispersion (SD) technique. SD of the extract with various polymers was prepared to select the best carrier. Solubility study, chemical stability study and dissolution study were performed to characterize the SD. The solubility of all three components, after forming solid dispersion with povidone K-30 (PVP K-30) was significantly increased in pH 6...
August 7, 2017: International Journal of Pharmaceutics
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