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Jing-Jing Zhu, Jian-Guo Jiang
Coumarins are fused benzene and pyrone ring systems with a wide spectrum of bioactivities including anti-tumor, anti-inflammation, antiviral and antibacterial effects. In this paper, the current development of coumarins-based drugs is introduced, and their structure-activity relationship is discussed by reviewing the relevant literatures published in the past twenty years. Coumarin molecules can be customized by the target site to prevent systemic side effects by virtue of structural modification. The ortho-phenolic hydroxyl on the benzene ring had remarkable antioxidant and anti-tumor activities...
May 11, 2018: Molecular Nutrition & Food Research
Renguo Xu, Zhen Liu, Jiande Hou, Tao Huang, Ming Yang
Background: Osthole is a natural product that has multiple bioactive functions and has been reported to exert potent immunosuppressive effects. However, the therapeutic effect of osthole on arthritis has not been explored. In the present study, a collagen-induced arthritis rat model, IL-1β-stimulated SW982 cells, and RA-like fibroblast-like synoviocytes (FLS) were employed to investigate the effect and possible mechanism of osthole on arthritis in vivo and in vitro. Results: 20 and 40 mg/kg osthole significantly alleviated collagen-induced arthritic symptoms based on histopathology and clinical arthritis scores, and improved erosion using HE staining...
2018: Cellular & Molecular Biology Letters
Sara Östhols, Carina Boström, Rasmussen-Barr Eva
PURPOSE: We aimed to map the physiotherapy practice in Sweden of clinical tests and patient-reported outcome measures in low-back pain (LBP), and to study advantages and barriers in using patient-reported outcome measures. METHODS: An online survey was mailed to 4934 physiotherapists in primary health care in Sweden. Multiple choice questions investigated the use of clinical tests and patient-reported outcome measures in assessing patients with LBP. Open questions investigating the advantages and barriers to the use of patient-reported outcome measures were analyzed with content analysis...
May 9, 2018: Disability and Rehabilitation
Gurjit Singh, Rajbir Bhatti, Rahul Mannan, Drishtant Singh, Anup Kesavan, Palwinder Singh
BACKGROUND: Osthole is a bioactive component reported in medicinal plants such as Angelica pubescens and Cnidium monnieri, known for analgesic activity. However, the toxicity, median effective dose (ED50 ), and dual modulation of nitric oxide and cyclooxygenase pathways along with inflammatory cytokines of osthole are yet to be determined. METHODS: The animals (mice) were assessed for general behaviour and mortality in varying doses (50, 300, and 2000 mg kg-1 ) of osthole for acute toxicity over 14 days...
May 7, 2018: Inflammopharmacology
Jingguo Wu, Yang Yang, Nan Xun, Lijin Zeng, Zhenyu Li, Wen Yang, Yanbing Liang, Zhongfu Ma, Hao Tang
This study was performed to evaluate the cardioprotective effects of osthole (OST) in a rat model of myocardial ischemia/reperfusion injury (MI/RI) and the underlying mechanism. We exposed rat hearts to left anterior descending coronary artery ligation for 30 min followed by 24 h of reperfusion. The results showed that pretreatment with OST ameliorated MI/RI as evidenced by histopathological examination. Moreover, the terminal deoxynucleotidyl transferase dUTP nick end-labeling assay demonstrated that OST suppressed myocardial apoptosis, which may be related to an increase in the Bcl-2/Bax ratio and inhibition of caspase-3 and caspase-9 activation...
2018: American Journal of Translational Research
Hui Wen, Nina Xue, Feng Wu, Yujun He, Gang Zhang, Zebin Hu, Huaqing Cui
Chromenone-derived natural products include chromones (flavone, isoflavone) and coumarins. Chromenone compounds not only exhibit impressive biological activities, but also are an important resource of experimentally used fluorophores, such as, 7-amino-4-methylcoumarin (AMC). Various chromenone compounds have reported to have weak fluorescence, and this has the potential to interfere with the measurements during AMC fluorogenic assays and result in non-robust assay readouts. Several flavones and isoflavones were found as SIRT1 activators, while fluorogenic sirtuin assays utilized AMC labelled peptides as the substrates...
May 2, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Ran Du, Zhao-Yang Meng, Jia-Lin Wang, Yan-Ling Wang
Purpose: To determine the effect of osthole on the retina in a chronic cerebral hypoperfusion (CCH) rat model and to investigate its therapeutic activity. Methods: Seventy-two rats were randomly allocated into 6 groups. CCH was induced by permanent bilateral common carotid artery occlusion (BCCAO) in five groups. Sham surgery was performed without occlusion of the artery in the sixth group (control group). Animals were administered with saline (model group), osthole (osthole-IG group), aspirin (aspirin group), or ginaton (ginaton group); the osthole-PI group was performed with peribulbar injection of osthole...
2018: Journal of Ophthalmology
Li Yao, Yuxia Yang, Guanhong He, Chunqing Ou, Lan Wang, Kaixuan Liu
Pulmonary arterial hypertension (PAH) is a progressive cardiovascular-disease with high mortality lacking high-efficiency drug. Our efforts attempted to delineate therapeutic action of osthole produced by Angelica Pubescens Maxim, which has the capacity to treat PAH by exploiting an iTRAQ-based proteomic method. Excitingly, osthole was observed to significantly restore 98 of 315 differential proteins significantly modified by PAH progression. They were primarily annotated into 24 signaling pathways. Four mostly affected proteins (RPL15, Cathepsin S, Histone H3...
April 3, 2018: Scientific Reports
Xiaojun Xu, Xiaoyuan Liu, Yan Zhang
Osthole is an active compound isolated from Chinese herb Cnidium monnieri (L.) Cusson, and had been reported to possess antitumor effect. However, the effect of osthole on the gastric cancer cells has not been investigated. In this study, the effects of osthole on the proliferation of human gastric cancer cells were tested. The data showed that osthole treatment significantly inhibited the proliferation of gastric cancer cells and resulted in the cell cycle arrest at G2/M phase in a dose-dependent manner. Western-blot study showed that the expression of cyclin B1 and cdc2 was markedly reduced by osthole...
2018: PloS One
Nani Wang, Xuping Wang, Yang Zhang, Qiaoyan Zhang, Pingcui Xu, Hailiang Xin, Renjie Wu, Dan Shou, Luping Qin
Osthole is a derivative of coumnarin, which has been used to treat several diseases, including osteoporosis. To investigate the metabolite profile of osthole in osteoporosis rats was utilized to understand its underlying mechanisms of its anti-osteoporosis effect. In this study, plasma samples were collected from normal and osteoporosis rats after oral administration of osthole and analyzed to identify the metabolites of osthole by high performance liquid chromatography quadrupole time-of-flight mass spectrometry...
March 20, 2018: Journal of Pharmaceutical and Biomedical Analysis
Xinbing Zhu, Zhengzheng Li, Tongtong Li, Fei Long, Yuesheng Lv, Lei Liu, Xuefeng Liu, Qimin Zhan
Esophageal squamous cell carcinoma (ESCC) is one of the most common lethal tumors and is known to be lack of effective therapy. Thus, novel therapeutic strategies are greatly needed for treatment of ESCC. Osthole, a natural active extract, has been documented to have anti-tumor activity. However, the effect of osthole on ESCC cells has not been elucidated. In this study, we demonstrated that osthole could inhibit the ESCC cell proliferation in dose- and time-dependent manner. Osthole treatment also induced G2/M phase arrest and apoptosis of ESCC cells...
March 23, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Xiao-Yu Wang, Xuan Ding, Yong-Fang Yuan, Le-Yi Zheng, Yan Cao, Zhen-Yu Zhu, Guo-Qing Zhang, Yi-Feng Chai, Xiao-Fei Chen, Zhan-Ying Hong
Rhizoma corydalis and Radix Angelicae Dahurica (Yuanhu-Baizhi) herbal medicine pair has been used for thousands of years and has been reported to be potentially active in recent cancer therapy. But the exact active components or fractions remain unclear. In this study, a new comprehensive two-dimensional (2D) 3-aminopropyltriethoxysilane (APTES)-decorated MCF7-cell membrane chromatography (CMC)/capcell-C18 column/time-of-flight mass spectrometry system was established for screening potential active components and clarifying the active fraction of Yuanhu-Baizhi pair...
April 2018: Journal of Food and Drug Analysis
Ya-Ping Xiao, Jie Zeng, Lin-Na Jiao, Xiao-Yu Xu
The treatment effect and signaling pathway regulation effects of kidney-tonifying traditional Chinese medicine on osteoporosis have been widely studied, but there is no systematic summary currently. This review comprehensively collected and analyzed the traditional Chinese medicines on the treatment and signaling pathway regulation of osteoporosis in recent ten years, such as Epimedii Folium, Drynariae Rhizoma, Cnidii Fructus, Eucommiae Cortex, Psoraleae Fructus and Dipsaci Radix. Based on the existing findings, the following conclusions were obtained: ①kidney-tonifying traditional Chinese medicine treated osteoporosis mainly through BMP-Smads, Wnt/ β -catenin, MAPK, PI3K/AKT signaling pathway to promote osteoblast bone formation and through OPG/RANKL/ RANK, estrogen, CTSK signaling pathway to inhibit osteoclasts of bone resorption...
January 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Miho Chikazawa, Ryuichiro Sato
Maintaining skeletal muscle functions by controlling muscle metabolism is of utmost importance. β2 -Adrenergic receptor (β2 -AR), which is expressed in skeletal muscle, is a member of the G-protein-coupled receptor family that plays a critical role in the maintenance of muscle mass. In the present study, using luciferase reporter assays in β2 -AR-expressing HEK293 cells, we discovered several food factors that exhibited agonistic activity at mouse or human β2 -AR. Osthole, gramine, and hordenine were identified as both mouse and human β2 -AR agonists, whereas berberine was identified as a mouse β2 -AR agonist only...
2018: Journal of Nutritional Science and Vitaminology
Hanan Khairy, Hanan Saleh, Abeer M Badr, Mohamed-Assem S Marie
Several mediators were associated with the pathogenesis of inflammatory bowel disease such as oxidative stress through the production of reactive oxygen metabolites, neutrophils infiltration and release of pro-inflammatory cytokines. This study was designed to investigate the therapeutic efficacy of osthole against dinitrobenzene sulfonic acid (DNBS) induced-colitis in rats through its anti-oxidant and anti-inflammatory properties. Colitis was induced in rats by single intracolonic instillation of (250 μl DNBS-25 mg/rat)...
April 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Yan-Fang Yang, Lei Zhang, Xiu-Wei Yang
Angelicae Pubescentis Radix (APR) is a widely-used traditional Chinese medicine. Pharmacological studies have begun to probe its biological activities on neurological disorders recently. To assess the brain penetration and distribution of APR, a validated ultra-performance liquid chromatography tandem mass spectrometry method was applied to the simultaneous determinations of the main coumarins from APR in the rat cerebrospinal fluid (CSF) and brain after oral administration of APR extract, including psoralen, xanthotoxin, bergapten, isoimperatorin, columbianetin, columbianetin acetate, columbianadin, oxypeucedanin hydrate, angelol B, osthole, meranzin hydrate and nodakenetin...
January 20, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Shengli Han, Yanni Lv, Liyun Kong, Yueming Sun, Jia Fu, Lingjun Li, Langchong He
Traditional Chinese medicine (TCM) has been used for prevention and treatment of various diseases for many decades. TCM injection is a new dosage form, with incidence of anaphylactoid reactions increasing every year. In this study, the rat basophilic leukemia 2H3 (RBL-2H3) and laboratory of allergic disease 2 (LAD2) dual-mixed/CMC was established and was coupled with an HPLC-ESI-IT-TOF-MS system to identify the potential allergenic components in Haqing injection. Cinobufagin, piperine, osthole, praeruptorin A, and schizandrin A were screened from Haqing injection via this coupled system...
January 22, 2018: Electrophoresis
Yuxin Bao, Xiaolin Meng, Fangning Liu, Fei Wang, Jinhui Yang, Haiyu Wang, Guanghong Xie
Inflammation and oxidative stress are implicated in the development of neurodegenerative diseases. Osthole is a compound that is extracted from She Chuang Zi, which is a type of traditional Chinese medicine. Osthole has previously been demonstrated to exhibit anticancer activities and has a low toxicity. However, to the best of our knowledge, the anti‑inflammatory effects of osthole in microglial cells have not been investigated extensively. The aim of the present study was to investigate the potential protective effects of osthole against inflammation induced by lipopolysaccharide (LPS) in microglial cells...
January 17, 2018: Molecular Medicine Reports
Pei-Ying Liu, Dun-Cheng Chang, Yu-Sheng Lo, Yi-Ting Hsi, Chia-Chieh Lin, Yi-Ching Chuang, Shu-Hui Lin, Ming-Ju Hsieh, Mu-Kuan Chen
Nasopharyngeal carcinoma (NPC) is endemic in Southern China and Southeast Asia. The present study investigated the activity of osthole in suppressing NPC along with the underlying mechanism. Cell growth inhibition was measured using the MTT assay. Apoptosis was detected through 4',6-diamidino-2-phenylindole staining and flow cytometry. Western blotting was used to identify the signaling pathway. Osthole markedly inhibited cell proliferation and induced apoptosis in the NPC cell line. Western blotting results revealed the increased activation of caspases 3, 8, and 9 and poly (ADP-ribose) polymerase...
April 2018: Environmental Toxicology
Yalda Shokoohinia, Fataneh Jafari, Zeynab Mohammadi, Leili Bazvandi, Leila Hosseinzadeh, Nicholas Chow, Piyali Bhattacharyya, Mohammad Hosein Farzaei, Ammad Ahmad Farooqi, Seyed Mohammad Nabavi, Mükerrem Betül Yerer, Anupam Bishayee
Cancer is caused by uncontrolled cell proliferation which has the potential to occur in different tissues and spread into surrounding and distant tissues. Despite the current advances in the field of anticancer agents, rapidly developing resistance against different chemotherapeutic drugs and significantly higher off-target effects cause millions of deaths every year. Osthol is a natural coumarin isolated from Apiaceaous plants which has demonstrated several pharmacological effects, such as antineoplastic, anti-inflammatory and antioxidant properties...
January 3, 2018: Nutrients
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