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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...
October 17, 2016: International Immunopharmacology
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...
September 16, 2016: International Immunopharmacology
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...
September 12, 2016: Oncotarget
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
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...
August 19, 2016: Phytotherapy Research: PTR
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...
August 17, 2016: Molecular Carcinogenesis
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...
July 28, 2016: Journal of Microbiology and Biotechnology
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 assay followed by bioactivity guided isolation from most active plant material...
July 26, 2016: Journal of Ethnopharmacology
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
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
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
Bo-Eun Kwon, Jae-Hyoung Song, Hyuk-Hwan Song, Ju Won Kang, Sam Noh Hwang, Ki-Jong Rhee, Aeri Shim, Eun-Hye Hong, Yeon-Jeong Kim, Sang-Min Jeon, Sun-Young Chang, Dong-Eun Kim, Sungchan Cho, Hyun-Jeong Ko
The flavonoids mosloflavone, oroxylin A, and norwogonin, which were purified from Scutellaria baicalensis Georgi, significantly protected Vero cells against Coxsackievirus B3 (CVB3)-induced cell death. To investigate the in vivo antiviral activity of oroxylin A, we intraperitoneally inoculated CVB3 into 4-week-old BALB/c mice. Body weights and blood glucose levels of the mice were decreased after CVB3 infection, and these changes were attenuated by the administration of oroxylin A. Importantly, treatment of mice with oroxylin A reduced viral titers in the pancreas and decreased the serum levels of the inflammatory cytokines including interleukin-6 (IL-6) and tumor necrosis factor (TNF)-α...
2016: PloS One
Lian Huang, Hiroyuki Fuchino, Nobuo Kawahara, Yuji Narukawa, Noriyasu Hada, Fumiyuki Kiuchi
A new method consisting of orthogonal projection to latent structure (OPLS) and modified principal component analysis (PCA) was applied to a screening of bioactive compounds from natural products. In this report, extracts of 52 Scutellaria Root (the root of Scutellaria baicalensis Georgi) samples were analyzed by high-performance liquid chromatography (HPLC), and their inhibitory activities towards prostaglandin E2 (PGE2) production in a murine macrophage-like cell line J774.1 were examined. Wogonin and oroxylin A were predicted to be strong inhibitors of PGE2 production by OPLS analysis of the data...
October 2016: Journal of Natural Medicines
Susannah Havermann, Yvonni Chovolou, Hans-Ulrich Humpf, Wim Wätjen
CONTEXT: Baicalein is a major compound in extracts derived from Scutellaria baicalensis Georgi (Lamiaceae) which are used in the Traditional Chinese Medicine for the treatment of inflammatory and gastrointestinal diseases. This flavonoid is an activator of the Nrf2 signalling pathway but the molecular mechanism is not clearly established. OBJECTIVE: We investigated the molecular mode of baicalein-mediated Nrf2-activation in Hct116 cells by the analysis of proteasomal activity, radical-scavenging activity and the comparison with baicalein derivatives...
September 2016: Pharmaceutical Biology
Ae-Yeon Lee, Saeromi Kang, Soo-Jin Park, Jin Huang, Dong-Soon Im
Oroxylum indicum has long been used in Asian traditional medicine to prevent and treat respiratory diseases, diabetes, diarrhea and other conditions. Oroxylin A is a flavone that is present in Oroxylum indicum and in Scutellaria baicalensis. Because the root extracts of both plants have been shown to have anti-allergic effects, the authors investigated whether oroxylin A is likely to have beneficial effects on allergic asthma using female Balb/c mice and rat RBL-2H3 mast cells. Antigen-induced degranulation was measured in vitro by measuring β-hexosaminidase activity...
May 1, 2016: Biomolecules & Therapeutics
Hui Hui, Xiaoxiao Zhang, Hui Li, Xiao Liu, Le Shen, Yu Zhu, Jingyan Xu, Qinglong Guo, Na Lu
PURPOSE: AML1/ETO fusion gene is one of disease-causing genes of t(8;21)-positive acute myeloid leukemia (AML). Oroxylin A (OA) has showed anticancer effects on other cancer cells. Here, studies were conducted to determine the antileukemia effect of OA on t(8;21)-positive AML cells in vitro and in vivo. MATERIALS AND METHODS: The effects of OA on cell viability of t(8;21)-positive Kasumi-1 and primary AML cells were analyzed by MTT assay. Cell differentiation was examined by NBT reduction assay, flow cytometry analysis for CD11b/CD14, and Giemsa stain...
July 2016: Journal of Cancer Research and Clinical Oncology
Chen Qiao, Na Lu, Yuxin Zhou, Ting Ni, Yuanyuan Dai, Zhiyu Li, Qinglong Guo, Libin Wei
Oroxylin A is a flavonoid extracted from the root of Scutellaria baicalensis Georgi. We previously demonstrated that oroxylin A induced apoptosis in human colon cancer cells via the mitochondrial pathway. In the present study, we investigated the underlying mechanisms responsible for the mitochondrial apoptotic pathway triggered by oroxylin A. p53 regulates mitochondrial survival, mitochondrial DNA integrity, and protection from oxidative stress. We determined that oroxylin A induces p53 mitochondrial translocation and inhibits SOD2 activity...
March 29, 2016: Oncotarget
Xiaoping Wang, Yang Sun, Yue Zhao, Youxiang Ding, Xiaobo Zhang, Lingyi Kong, Zhiyu Li, Qinglong Guo, Li Zhao
Oroxyloside, as a metabolite of oroxylin A, may harbor various beneficial bioactivities which have rarely been reported in the previous studies. Here we established the dextran sulfate sodium (DSS)-induced experimental colitis and evaluated the anti-inflammatory effect of oroxyloside in vivo. As a result, oroxyloside attenuated DSS-induced body weight loss, colon length shortening and colonic pathological damage. Furthermore, oroxyloside inhibited inflammatory cell infiltration and decreased myeloperoxidase (MPO) and inducible nitric oxide synthase (iNOS) activities as well...
April 15, 2016: Biochemical Pharmacology
Huiying Yang, Jianfeng Li, Yuanting Zheng, Lu Zhou, Shanshan Tong, Bei Zhao, Weimin Cai
A novel microsomes-hydrogel added cell culture system (MHCCS) was employed in the antitumor activity screening of natural compounds, aiming to achieve drug screening with better in vivo correlation, higher initiative to explore the potential active metabolites, and investigation of the antitumor mechanism from the perspective of metabolism. MTT assay and cell apoptosis detection showed that test drug oroxylin A (OA) had enhanced cytotoxicity and wogonin (W) with reduced cytotoxicity on MCF-7 cell line upon MHCCS incubation...
2016: Scientific Reports
De-Gang Zhou, Bao-Zhong Diao, Wen Zhou, Jia-Long Feng
Oroxylin A, a natural flavonoid isolated from the medicinal herb Scutellaria baicalensis Georgi, has been reported to have anti-inflammatory property. In this study, we aimed to investigate the protective effects and mechanism of oroxylin A on allergic inflammation in OVA-induced asthma murine model. BABL/c mice were sensitized and airway-challenged with OVA to induce asthma. Oroxylin A (15, 30, and 60 mg/kg) was administered by oral gavage 1 h before the OVA treatment on day 21 to 23. The results showed that oroxylin A attenuated OVA-induced lung histopathologic changes, airway hyperresponsiveness, and the number of inflammatory cells...
April 2016: Inflammation
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