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https://www.readbyqxmd.com/read/28536775/catechol-o-methyltransferase-and-udp-glucuronosyltransferases-in-the-metabolism-of-baicalein-in-different-species
#1
Ruiya Zhang, Yonglei Cui, Yan Wang, Xiangge Tian, Lu Zheng, HaiJian Cong, Bin Wu, Xiaokui Huo, Chao Wang, BaoJing Zhang, Xiaobo Wang, Zhonghui Yu
BACKGROUND: Baicalein is the major bioactive flavonoid in some herb medicines and dietary plants; however, the detailed metabolism pathway of its major metabolite oroxylin A-7-O-β-D-glucuronide in human was not clear. It was important to illustrate the major metabolic enzymes that participate in its elimination for the clinic use of baicalein. OBJECTIVES: We first revealed a two-step metabolism profile for baicalein and illustrated the combination of catechol-O-methyltransferase (COMT) and uridine diphosphate-glucuronosyltransferases (UGTs) in drug metabolism, further evaluated its bioactivity variation during drug metabolism...
May 23, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28472762/oroxylin-a-inhibits-the-generation-of-tregs-in-non-small-cell-lung-cancer
#2
Le Shen, Lu-Lu Zhang, Hui Li, Xiao Liu, Xiao-Xuan Yu, Po Hu, Hui Hui, Qing-Long Guo, Shuai Zhang
Oroxylin A (OA), a naturally occurring monoflavonoid isolated from Scutellariae radix, has previously been reported to inhibit the proliferation of several cancer cell lines. CD4+CD25+Foxp3+ regulatory T cells (Tregs) play an important role in maintenance of immunologic self-tolerance. Tregs also increase in cancer and take part in suppressing antitumor immune responses. Here, we explored how OA affected the Tregs in lung cancer environment and the involved underlying mechanism. It is found that OA reversed the generation of Tregs induced by H460 lung cancer cells co-culture...
April 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/28426226/brain-uptake-of-bioactive-flavones-in-scutellariae-radix-and-its-relationship-to-anxiolytic-effect-in-mice
#3
Sophia Yui Kau Fong, Chenrui Li, Yiu Cheong Ho, Rui Li, Qian Wang, Yin Cheong Wong, Hong Xue, Zhong Zuo
Scutellariae Radix (SR) and its bioactive flavones elicit a variety of effects in the brain. However, the brain uptake of individual SR flavones and its relationship to the elicited effects after SR administration remain unknown. Moreover, previous studies seldom measured pharmacokinetic and pharmacodynamic outcomes simultaneously. In the current study, the brain uptake of six major SR flavones and the anxiolytic behavior following oral administration of a SR extract at two clinically relevant doses (600 and 1200 mg/kg twice daily) were simultaneously investigated in mice (n = 18 per group)...
May 1, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28286894/a-general-strategy-for-the-synthesis-of-homogeneous-hyaluronan-conjugates-and-their-biological-applications
#4
Xuan Fu, Wenjing Shang, Shuaishuai Wang, Yunpeng Liu, Jingyao Qu, Xi Chen, Peng George Wang, Junqiang Fang
Here, we developed a general strategy for synthesizing homogeneous HA conjugates, and generated homogeneous HA-pNP, HA-biotin, and HA-oroxylin conjugates to investigate the relationships between HA chain length and its diverse biological functions.
March 13, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28284428/distribution-patterns-of-the-contents-of-five-biologically-activate-ingredients-in-the-root-of-scutellaria-baicalensis
#5
Rong-Xiu Liu, Guo-Hu Song, Pei-Gen Wu, Xue-Wen Zhang, Hui-Juan Hu, Jia Liu, Xiao-Su Miao, Zhi-Yan Hou, Wen-Quan Wang, Sheng-Li Wei
As an important herbaceous plant, Scutellaria baicalensis Georgi (Chinese skullcap) is geographically widespread and commonly used throughout the world. In the Chinese medicine market, S. baicalensis has been divided into two primary types, "Ku Qin" (WXR) and "Tiao Qin" (TST). Moreover, TST is also divided into different grades according to the diameter of roots. To explore the distribution patterns of the contents of five biologically activate ingredients (FBAI), we used six-year-old cultivated S. baicalensis and analyzed its growth characteristics as well as the quality difference among different types and diameters in roots...
February 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28236316/simultaneous-determination-of-wogonin-oroxylin-a-schisandrin-paeoniflorin-and-emodin-in-rat-serum-by-hplc-ms-ms-and-application-to-the-pharmacokinetic-studies
#6
Minting Chen, Suying Wei, Chaohua Luo, Feilong Chen, Shuai Song, Qun Shen, Zhixian Mo, Fenghuan Wei
Wogonin and oroxylin A in Scutellariae Radix, schisandrin in Chinensis fructus, paeoniflorin in Moutan Cortex and emodin in Polygoni Cuspidate Rhizome et Radix are anti-inflammatory active compounds. A method for simultaneous determination of the five compounds in rat was developed and validated using high performance liquid chromatography with tandem mass spectrometry (HPLC-MS/MS). The separation was performed on a Symmetry C18 column (4.6 × 50 mm, 3.5 µm) with acetonitrile and 0.1% formic acid aqueous solution as the mobile phases...
February 24, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28182699/bifunctional-effects-of-o-methylated-flavones-from-scutellaria-baicalensis-georgi-on-melanocytes-inhibition-of-melanin-production-and-intracellular-melanosome-transport
#7
Michiko Kudo, Kumiko Kobayashi-Nakamura, Kentaro Tsuji-Naito
The growing interest in skin lightening has recently renewed attention on the esthetic applications of Chinese herbal medicine. Although Scutellaria baicalensis Georgi is used for antipyretic and antiinflammatory purposes, its whitening effect remains unclear. This study reports three major findings: (1) S. baicalensis has a potent inhibitory effect on melanogenesis; (2) wogonin and its glycoside are the active components of S. baicalensis; and (3) O-methylated flavones from S. baicalensis, such as wogonin, inhibit intracellular melanosome transport...
2017: PloS One
https://www.readbyqxmd.com/read/27918833/effects-of-lead-phytochemicals-of-radix-scutellariae-on-acanthamoeba
#8
Pauline Cho, Guangsen Shi, Maurice Yap, Maureen V Boost
Purpose: Acanthamoeba keratitis (AK), which is associated with noncompliant use of contact lenses, remains difficult to treat due to delayed diagnosis and paucity of therapeutic agents. Although improvements in activity against Acanthamoeba infection have been achieved in disinfecting solutions for soft contact lenses, such modifications have not been extended to those for special rigid gas permeable (RGP) contact lenses, which are increasingly used for myopia control in children. Phytochemicals present in herbs used for traditional Chinese medicine may be effective as therapeutic or preventive agents...
December 1, 2016: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/27820974/oroxylin-a-inhibits-h2o2-induced-oxidative-stress-in-pc12-cells
#9
Qinghe Han, Haiyu Wang, Chong Xiao, Ben-Dong Fu, Chong-Tao Du
Oroxylin A, a natural flavonoid isolated from Scutellaria baicalensis, has been reported to have anti-inflammatory and antioxidant effects. However, suppression of oxidative stress and neuroapoptosis by oroxylin A is largely uninvestigated. To investigate the protective effects of oroxylin A, PC12 cells were exposed to oroxylin A and hydrogen peroxide solutions and measured. Oroxylin A significantly reduced the levels of intracellular calcium and reactive oxygen species and increased the levels of CAT and Mn/SOD...
June 2017: Natural Product Research
https://www.readbyqxmd.com/read/27764743/oroxylin-a-attenuates-cigarette-smoke-induced-lung-inflammation-by-activating-nrf2
#10
Jihe Li, Dongxia Tong, Juan Liu, Fuyang Chen, Yongbin Shen
Oroxylin A, a natural flavonoid isolated from the medicinal herb Scutellaria baicalensis Georgi, has been reported to have anti-inflammatory and antioxidant properties. However, the effect of oroxylin A on cigarette smoke (CS)-induced lung inflammation remains unclear. In this study, the ability of oroxylin A to protect against CS-induced lung inflammation was detected in vivo and in vitro. Oroxylin A was administered intraperitoneally to mice 2h prior CS exposure every day for five consecutive days. BEAS-2B bronchial epithelial cells and RAW264...
November 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27643663/therapeutic-potential-of-oroxylin-a-in-rheumatoid-arthritis
#11
Yu-Ling Wang, Ju-Mei Gao, Li-Zhi Xing
Excessive inflammation contributes greatly to the pathogenesis and development of rheumatoid arthritis (RA). Oroxylin A (OA) is a natural anti-inflammatory flavonoid compound. In this study, we investigated the effects of OA on collagen-induced arthritis (CIA) and human RA fibroblast-like synoviocytes (FLS). CIA was induced in DBA/1 mice and mice were intraperitoneally treated with OA (10mg/kg) for 10days. Arthritis severity was evaluated every day and the histopathologic examination of joints was done. Serum levels of anti-collagen II antibodies (anti-CII Abs) and cytokines were determined by ELISA...
November 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27634872/mitochondrial-aldehyde-dehydrogenase-obliterates-insulin-resistance-induced-cardiac-dysfunction-through-deacetylation-of-pgc-1%C3%AE
#12
Nan Hu, Jun Ren, Yingmei Zhang
Insulin resistance contributes to the high prevalence of type 2 diabetes mellitus, leading to cardiac anomalies. Emerging evidence depicts a pivotal role for mitochondrial injury in oxidative metabolism and insulin resistance. Mitochondrial aldehyde dehydrogenase (ALDH2) is one of metabolic enzymes detoxifying aldehydes although its role in insulin resistance remains elusive. This study was designed to evaluate the impact of ALDH2 overexpression on insulin resistance-induced myocardial damage and mechanisms involved with a focus on autophagy...
November 22, 2016: Oncotarget
https://www.readbyqxmd.com/read/27585443/oroxylin-a-could-be-a-promising-radiosensitizer-for-esophageal-squamous-cell-carcinoma-by-inducing-g2-m-arrest-and-activating-apoptosis
#13
Cheng Tan, Xia Qian, Yangyang Ge, Baixia Yang, Feng Wang, Zhifeng Guan, Jing Cai
To evaluate the radiosensitization of Oroxylin A on esophageal carcinoma cell as well as the optimal scheduling of Oroxylin A and radiotherapy (RT). Cell proliferation was estimated by a CCK8 assay. Radiosensitization was evaluated by a clonogenic survival assay. The progressions of Cell apoptosis and Cell cycle were investigated by flow cytometry. Expressions of survivin and cell cycle regulators were evaluated by Western blot analysis. A dose-dependent cell survival reduction was found in response to radiation with or without Oroxylin A...
September 2, 2016: Pathology Oncology Research: POR
https://www.readbyqxmd.com/read/27539056/overview-of-oroxylin-a-a-promising-flavonoid-compound
#14
REVIEW
Lu Lu, Qinglong Guo, Li Zhao
Oroxylin A is one of the main active components extracted from Scutellariae radix. It has been proved that oroxylin A possesses a broad spectrum of pharmacological functions, including anti-cancer, antiinflammation, neuroprotective, anti-coagulation and so on. The pharmacological activity of oroxylin A has been studied in vitro and on animal models, which reflected its promising potency in disease treatment. This review aims to recapitulate the pharmacological function and the molecular mechanisms of oroxylin A, as well as its sources, extraction, synthesis and toxicity study...
November 2016: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/27533597/oroxylin-a-reverses-the-drug-resistance-of-chronic-myelogenous-leukemia-cells-to-imatinib-through-cxcl12-cxcr7-axis-in-bone-marrow-microenvironment
#15
Wenjun Li, Qilong Ding, Youxiang Ding, Lu Lu, Xiaoping Wang, Yi Zhang, Xiaobo Zhang, Qinglong Guo, Li Zhao
Imatinib (IM), a tyrosine-kinase inhibitor, is used in treatment of multiple cancers, most notably Philadelphia chromosome-positive (Ph(+) ) chronic myelogenous leukemia (CML). However, the majority of patients continue to present with minimal residual disease occurred in the bone marrow (BM) microenvironment. One of the key factors that contribute to leukemia cell drug resistance is chemokine CXCL12. In the current study, co-culturing CML cell K562 and KU812 with BM stromal cell M2-10B4 attenuated IM-induced apoptosis...
March 2017: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/27470493/biological-synthesis-of-baicalein-derivatives-using-escherichia-coli
#16
Da Hye Han, Youngshim Lee, Joong-Hoon Ahn
Two baicalein derivatives, baicalin and oroxylin A, were synthesized in this study. These derivatives exhibit diverse biological activities, such as anxiolytic and anticancer activities as well as memory enhancement. In order to synthesize baicalin from aglycon baicalein using Escherichia coli, we utilized a glycosyltransferase that regioselectively transfers glucuronic acid from UDP-glucuronic acid to the 7-hydroxy group of baicalein. To increase baicalin productivity, an araA deletion E. coli mutant, which accumulates UDP-glucuronic acid, was used, and ugd, which converts UDP-glucose to UDP-glucuronic acid, was overexpressed...
November 28, 2016: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/27469197/screening-of-six-ayurvedic-medicinal-plants-for-anti-obesity-potential-an-investigation-on-bioactive-constituents-from-oroxylum-indicum-l-kurz-bark
#17
Priyanka Mangal, Pragyanshu Khare, Sneha Jagtap, Mahendra Bishnoi, Kanthi Kiran Kondepudi, Kamlesh Kumar Bhutani
ETHNOPHARMACOLOGICAL RELEVANCE: As an effort to identify newer anti-obesity lead(s) we have selected 13 plant materials from the six plant species which have been reported in Indian Ayurvedic medicine as remedy against complications affecting glucose and lipid homeostasis. AIM OF THE STUDY: In vitro screening of six Indian Ayurvedic medicinal plants on anti-adipogenic and pancreatic lipase (PL) inhibition potential followed by bioactivity guided isolation from most active plant material...
February 2, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27347031/anti-inflammatory-effects-of-oroxylin-a-on-raw-264-7-mouse-macrophages-induced-with-polyinosinic-polycytidylic-acid
#18
Ji Young Lee, Wansu Park
Oroxylin A (5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one; Baicalein 6-methyl ether) is an active flavonoid compound originally isolated from Scutellaria radix, which has been used to treat pulmonary infection in Korea, China, and Japan. Oroxylin A is known to possess dopamine reuptake inhibitor activity. However, the effects of oroxylin A on virus-induced macrophages has not been fully elucidated. In the present study, the anti-inflammatory effects of oroxylin A on double-stranded RNA-induced macrophages were examined...
July 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27314303/5-6-dihydroxy-3-7-4-trimethoxyflavonol-induces-g2-m-cell-cycle-arrest-and-apoptosis-in-human-hepatocellular-carcinoma-cells
#19
Xin-Xin Zhao, Juan-Juan Chang, Qi-Lin Wang, Rong Lu, Ling-Jun Li, Xiao Sun, Wei-Dong Xie, Xia Li
5,6-Dihydroxy-3,7,4'-trimethoxyflavonol (AH5), 5,6,3'-trihydroxy-3,7,4'-trimethoxyflavonol (AH22), artemetin, and oroxylin A are four flavonoids with the same 2-phenyl-chromone skeleton isolated from the Chinese herb Aster himalaicus. The aim of this study was to evaluate the structure-activity relationship of these four analogs and the mediation of AH5 cytotoxicity via G2/M arrest and apoptosis in human hepatocellular carcinoma (HCC) cells. 3-(4,5-Dimethythiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay indicated AH5 showed the better potency to inhibit proliferation in human HCC cells, which suggested hydroxyl binding to C6 is necessary to anticancer properties, whereas binding to C3' attenuated the activities and increased toxicity in tested cells...
November 2016: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/27257010/inhibitory-effects-of-norwogonin-oroxylin-a-and-mosloflavone-on-enterovirus-71
#20
Hwa Jung Choi, Hyuk-Hwan Song, Jae-Sug Lee, Hyun-Jeong Ko, Jae-Hyoung Song
Severe complications associated with EV71 infections are a common cause of neonatal death. Lack of effective therapeutic agents for these infections underlines the importance of research for the development of new antiviral compounds. In the present study, the anti-EV71 activity of norwogonin, oroxylin A, and mosloflavone from Scutellaria baicalensis Georgi was evaluated using a cytopathic effect (CPE) reduction method, which demonstrated that all three compounds possessed strong anti-EV71 activity and decreased the formation of visible CPEs...
September 1, 2016: Biomolecules & Therapeutics
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