The Open Bioactive Compounds Journal最新文献

{"title":"Hydrazonoyl Halides: Their Versatile Biological Activities","authors":"A. S. Shawali, N. Samy","doi":"10.2174/1874847300902010008","DOIUrl":"https://doi.org/10.2174/1874847300902010008","url":null,"abstract":"The various biological activities namely anthelmintic, antiarthropodal, antiviral, antimicrobial, herbicidal, antisarcoptic, acaricidal, insecticidal and miticidal activities exhibited by the hydrazonoyl halides are surveyed. Also, the uses of such halides as pesticides, weed controlling and antihypertensive agents as well as lipoxygenase and cyclooxy- genase inhibitors are presented. Furthermore, their contact dermatitis and phytotoxicity effects are pointed out in addition to their metabolic fate.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"61 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128505819","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Analgesic and Anti-Gastropathic Effects of Salidroside Isolated from Acer tegmentosum Heartwood","authors":"Y. Yoo, Jung‐Hwan Nam, Min-Young Kim, Jong-Won Choi, Kyung-Tae Lee, Hee-Juhn Park","doi":"10.2174/1874847300902010001","DOIUrl":"https://doi.org/10.2174/1874847300902010001","url":null,"abstract":"The heartwood of Acer tegmentosum (Acereaceae) has been used as a Korean traditional medicinal drug against alcohol poisoning and hepatitis. To find the biologically active substance in A. tegmentosum heartwood, we investigated the protective effects of the heartwood extract and its constituents on pain and gastropathy in mouse. In these experiments, salidroside, a major compound, significantly reduced gastric lesion and pain in mice. Oral administration of salidroside at the 10 and 20 mg/kg doses greatly reduced the gastric lesion induced by HCl/ethanol (inhibitory effect, 51.5 and 68.8%, respectively) and by indomethacin/bethanechol (inhibitory effect, 31.3 and 38.8%, respectively). Salidroside also stabi- lized pH of gastric juice and the increase of gastric juice secretion and total acid output. Taken together, these results demonstrated that salidroside is the main ingredient of A. tegmentosum heartwood to prevent gastric lesion and pain that can be caused by drinking alcohol.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"28 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123221944","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Sphingosine Kinase 2 Inhibitor Accelerates Fas-Mediated Cell Death Progression in A20/2J Cells~!2008-08-07~!2008-09-19~!2008-11-28~!","authors":"M. Hara-Yokoyama, K. Terasawa, A. Kihara, Jin-Wook Kim, C. Park, Y. Hirabayashi, Y. Igarashi, M. Yanagishita","doi":"10.2174/1874847300801010022","DOIUrl":"https://doi.org/10.2174/1874847300801010022","url":null,"abstract":"! \" # $ \" $ \" % &%’\" & ( ( )$%& \" \"\" $ $ * * * + , )\"& # - \"! \" , ! \" + + + + + + + +. *+ +* + +. *+ .+ +* *+. + + + + + .+ + + +. + + *+* +. *+. +* + *","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"136 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"116178947","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Identification of Polyphenols and Anti-Oxidant Capacity of Piper aduncum L","authors":"Mónica Ramos Escudero, D. Escudero, C. Remsberg, Jody K. Takemoto, N. Davies, J. Yáñez","doi":"10.2174/1874847300801010018","DOIUrl":"https://doi.org/10.2174/1874847300801010018","url":null,"abstract":"Ethanol extracts of Piper aduncum L. leaves from five sub-regions in the tropical Peruvian rainforest were as- sessed for polyphenol content utilizing liquid chromatography coupled with mass spectrometry with electrospray ioniza- tion (LC-MS-ESI). The anti-oxidant capacity was estimated using a DPPH radical scavenging assay. Additionally, the re- ducing power (capacity to reduce Fe 3+ to Fe 2+ ), the capacity to scavenge hydrogen peroxide and the total polyphenol con- tent, were assessed. Analysis led to the identification of gallic acid, catechin, chlorogenic acid, epicatechin, rutin, querci- trin, phloridzin, quercetin, and phloretin, as well as determination of potent anti-oxidant capacities by P. aduncum L.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"5 1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128926227","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Non-Intercalative Triterpenoid Inhibitors of Topoisomerase II: A Molecular Docking Study","authors":"W. Setzer","doi":"10.2174/1874847300801010013","DOIUrl":"https://doi.org/10.2174/1874847300801010013","url":null,"abstract":"Theoretical flexible docking studies were carried out on a number of triterpenoids previously shown to be inhibitors of topoisomerase II in order to assess the nature of binding of these non-intercalative inhibitors to the enzyme. The molecular docking results suggest that most of the triterpenoids preferentially bind to the DNA binding site of topoisomerase II, while a few also bind to the ATP binding site. These results provide some insight into the mode of activity of these cytotoxic natural products. INTRODUCTION Topoisomerases are essential enzymes that catalyze modifications to the tertiary structure of DNA. There are two well-characterized classes of human topoisomerases. Topoisomerase I acts by breaking and religating one DNA strand [1], while topoisomerase II involves double-strand breaking [2]. These enzymes serve to relieve DNA twisting and supercoiling, playing key roles in replication, transcription, and recombinant repair. Topoisomerase II is highly expressed in rapidly proliferating cells [3] and is therefore an attractive target for antitumor drugs. There are two general classes of topoisomerase II targeting drugs: topoisomerase II poisons and topoisomerase II catalytic inhibitors. Topoisomerase II poisons include etoposide, doxorubicin, and mitoxantrone. These compounds serve to stabilize the enzyme-DNA complex (the “cleavable complex”) and prevent the enzyme from religating the cleaved DNA [4]. Both doxorubicin and mitoxantrone are DNA intercalating agents [5] whereas etoposide does not bind DNA but rather apparently binds to the ATP binding site of the N-terminal domain of topoisomerase II [6, 7]. The catalytic inhibitors, on the other hand, block the catalytic activity of DNA topoisomerase II but do not stabilize the DNA-topoisomerase II cleavable complex [5, 8]. Examples of catalytic topoisomerase II inhibitors include the anthracycline aclarubicin, the polyanionic compound surname, the coumarin novobiocin, and bisdioxopiperazines such as sobuzoxane and dexrazoxane [9]. These agents inhibit the catalytic activity of topoisomerase II by preventing the binding of the enzyme to DNA. A number of natural and semisynthetic triterpenoids have shown topoisomerase II inhibitory activity. These include 3,4-seco-8 H-ferna-4(23),9(11)dien-3-oic acid (1) and its corresponding alcohol derivative (2) [10]; seco-3,4-friedelin (3), seco-3,4-taraxerone (4), lupeol (5) [11]; fomitellic acids A and B (6 and 7) [12]; ursolic acid (8), oleanolic acid (9), betulinic acid (10), acetyl boswellic acid (11) [13]; demethylzeylasterone (12) [14]; *Address correspondence to this author at the Department of Chemistry, University of Alabama in Huntsville, Huntsville, AL 35899, USA; Tel: 256824-6519; Fax: 256-824-6349; E-mail: mailto:wsetzer@chemistry.uah.edu dihydrobetulinic acid (13) [15]; corosolic acid (14), 3 corosolic acid (15), 3 -corosolic acid lactone (16) [16]; celastrol (17), dihydrocelastrol (18) [17]; dehydrotrametononic acid (19), dehydroebrico","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"1 4 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128846665","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"High-Lycopene Tomato Intake Increases Serum Carotenoid Levels but not Biomarkers of Oxidative Stress and Inflammation in Healthy Adults","authors":"C. Thomson, N. Stendell-Hollis, J. West, E. Cussler, L. McCune, M. Kroggel, Hyun-Jin Kim, C. Kubota","doi":"10.2174/1874847300801010007","DOIUrl":"https://doi.org/10.2174/1874847300801010007","url":null,"abstract":"Fresh tomatoes higher in lycopene content than standard varieties have recently been designed. We hypothesized that consumption of fresh, high lycopene tomatoes (HEC) for 3-weeks, as compared to standard fresh tomatoes, (LEC) would result in significant increases in serum lycopene and reductions in oxidative stress and inflammation. Forty healthy adult men (37.5%) and women (62.5%) age 55.3±4.7 years (BMI = 25.1±3.3 kg/m 2 ) completed this randomized, crossover, controlled tomato intervention. Serum lycopene, oxidative stress (8-OHdG, 8-iso-PGF2 ) and inflammation (hsCRP) were assessed. Significant increases were seen in transand cis-lycopene (preand post-intervention, P < 0.0001), with cis-lycopene increasing significantly more during HEC consumption as compared to LEC (P=0.03). No significant changes in 8-OHdG, 8-iso-PGF2 or hsCRP were demonstrated. Consumption of HEC tomatoes resulted in significant elevations in serum lycopene but not significant reductions in oxidative stress or inflammation in this healthy adult population.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"20 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128431444","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Allantoin as A Biomarker of Inflammation in an Inflammatory Bowel Disease Mouse Model: NMR Analysis of Urine","authors":"P. Dryland, D. Love, Michael F. Walker, Y. Dommels, C. Butts, D. Rowan, N. Roy, N. Helsby, B. Browning, Shuotun Zhu, B. Copp, L. Ferguson","doi":"10.2174/1874847300801010001","DOIUrl":"https://doi.org/10.2174/1874847300801010001","url":null,"abstract":"Crohn's disease (CD) is an Inflammatory Bowel Disease (IBD) that is characterised by destructive inflamma- tion of the intestinal wall. Current methods for determining inflammation of the bowel are costly, time consuming and can cause discomfort to the patients. In order to address these problems, biomarker analysis of more accessible tissues is re- ceiving increasing attention. Oxidative stress has been implicated in the promotion of inflammation. Allantoin has re- cently been reported as a biomarker for oxidative stress in human serum and urine. This paper investigates allantoin as a biomarker of inflammation in a mouse model of CD. Proton nuclear magnetic resonance ( 1 H NMR) spectroscopy was used to analyse allantoin in urine from the mdr1a -/- mouse which is a model of CD. The data show that the levels of al- lantoin are strongly correlated with histological injury scores of mouse colonic tissue samples. Allantoin appears to be a useful biomarker of gut inflammation, involving oxidative stress, in a mouse model of CD and may be a potential bio- marker in human CD studies.","PeriodicalId":403551,"journal":{"name":"The Open Bioactive Compounds Journal","volume":"153 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"132816434","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}