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https://www.readbyqxmd.com/read/28921127/synergistic-effect-of-baicalein-wogonin-and-oroxylin-a-mixture-multistep-inhibition-of-the-nf-%C3%AE%C2%BAb-signalling-pathway-contributes-to-an-anti-inflammatory-effect-of-scutellaria-root-flavonoids
#1
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...
September 18, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28857294/oroxylin-a-prevents-angiogenesis-of-lsecs-in-liver-fibrosis-via-inhibition-of-yap-hif-1%C3%AE-signaling
#2
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 futher 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...
August 31, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28753557/oroxylin-a-inhibits-colitis-by-inactivating-nlrp3-inflammasome
#3
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
https://www.readbyqxmd.com/read/28730309/a-simple-and-rapid-infrared-assisted-self-enzymolysis-extraction-method-for-total-flavonoid-aglycones-extraction-from-scutellariae-radix-and-mechanism-exploration
#4
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...
July 20, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28726775/oroxylin-a-activates-pkm1-hnf4-alpha-to-induce-hepatoma-differentiation-and-block-cancer-progression
#5
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
https://www.readbyqxmd.com/read/28642200/enhancement-of-solubility-and-dissolution-rate-of-baicalein-wogonin-and-oroxylin-a-extracted-from-radix-scutellariae
#6
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
https://www.readbyqxmd.com/read/28640893/oroxylin-a-promotes-retinal-ganglion-cell-survival-in-a-rat-optic-nerve-crush-model
#7
Shu-Fang Lin, Jia-Ying Chien, Kishan Kapupara, Chi-Ying F Huang, Shun-Ping Huang
PURPOSE: To investigate the effect of oroxylin A on the survival of retinal ganglion cells (RGC) and the activation of microglial cells in a rat optic nerve (ON) crush model. METHODS: Oroxylin A (15mg/Kg in 0.2ml phosphate-buffered saline) or phosphate-buffered saline (PBS control) was immediately administered after ON crush once by subcutaneous injection. Rats were euthanized at 2 weeks after the crush injury. The density of RGC was counted by retrograde labeling with FluoroGold and immunostaining of retina flat mounts for Brn3a...
2017: PloS One
https://www.readbyqxmd.com/read/28594405/oroxylin-a-suppresses-the-development-and-growth-of-colorectal-cancer-through-reprogram-of-hif1%C3%AE-modulated-fatty-acid-metabolism
#8
Ting Ni, Zihao He, Yuanyuan Dai, Jingyue Yao, Qinglong Guo, Libin Wei
The occurrence and progress of colon cancer are closely associated with obesity. Therefore, the lipid metabolism, especially fatty acid metabolism, is a significant section of energy homeostasis in colon cancer cells, and it affects many important cellular processes. Oroxylin A is one of the main bioactive flavonoids of Scutellariae radix, which has a strong anticancer effect but low toxicity to normal tissue. In previous studies, we have proved that oroxylin A reprogrammes metabolism of cancer cells by inhibiting glycolysis...
June 8, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28536775/catechol-o-methyltransferase-and-udp-glucuronosyltransferases-in-the-metabolism-of-baicalein-in-different-species
#9
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
#10
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...
July 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28426226/brain-uptake-of-bioactive-flavones-in-scutellariae-radix-and-its-relationship-to-anxiolytic-effect-in-mice
#11
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
#12
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
#13
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-pharmacokinetic-studies
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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