Sample records for active compounds lopac1280

  1. Kinetic characterization of ebselen, chelerythrine and apomorphine as glutaminase inhibitors.

    PubMed

    Thomas, Ajit G; Rojas, Camilo; Tanega, Cordelle; Shen, Min; Simeonov, Anton; Boxer, Matthew B; Auld, Douglas S; Ferraris, Dana V; Tsukamoto, Takashi; Slusher, Barbara S

    2013-08-23

    Glutaminase catalyzes the hydrolysis of glutamine to glutamate and plays a central role in the proliferation of neoplastic cells via glutaminolysis, as well as in the generation of excitotoxic glutamate in central nervous system disorders such as HIV-associated dementia (HAD) and multiple sclerosis. Both glutaminase siRNA and glutaminase inhibition have been shown to be effective in in vitro models of cancer and HAD, suggesting a potential role for small molecule glutaminase inhibitors. However, there are no potent, selective inhibitors of glutaminase currently available. The two prototypical glutaminase inhibitors, BPTES and DON, are either insoluble or non-specific. In a search for more drug-like glutaminase inhibitors, we conducted a screen of 1280 in vivo active drugs (Library of Pharmacologically Active Compounds (LOPAC(1280))) and identified ebselen, chelerythrine and (R)-apomorphine. The newly identified inhibitors exhibited 10 to 1500-fold greater affinities than DON and BPTES and over 100-fold increased efficiency of inhibition. Although non-selective, it is noteworthy that the affinity of ebselen for glutaminase is more potent than any other activity yet described. It is possible that the previously reported biological activity seen with these compounds is due, in part, to glutaminase inhibition. Ebselen, chelerythrine and apomorphine complement the armamentarium of compounds to explore the role of glutaminase in disease. Copyright © 2013 Elsevier Inc. All rights reserved.

  2. 7 CFR 1280.223 - Reports.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Reports. 1280.223 Section 1280.223 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.223 Reports. Each first handler required to remit assessments to the Board for live lambs pursuant to § 1280...

  3. 7 CFR 1280.223 - Reports.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Reports. 1280.223 Section 1280.223 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.223 Reports. Each first handler required to remit assessments to the Board for live lambs pursuant to § 1280...

  4. 36 CFR 1280.24 - Is smoking allowed on NARA property?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false Is smoking allowed on NARA property? 1280.24 Section 1280.24 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS...? Prohibited Activities § 1280.24 Is smoking allowed on NARA property? Smoking is not allowed inside any NARA...

  5. 36 CFR 1280.24 - Is smoking allowed on NARA property?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false Is smoking allowed on NARA property? 1280.24 Section 1280.24 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS...? Prohibited Activities § 1280.24 Is smoking allowed on NARA property? Smoking is not allowed inside any NARA...

  6. 36 CFR 1280.24 - Is smoking allowed on NARA property?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false Is smoking allowed on NARA property? 1280.24 Section 1280.24 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS...? Prohibited Activities § 1280.24 Is smoking allowed on NARA property? Smoking is not allowed inside any NARA...

  7. 36 CFR 1280.24 - Is smoking allowed on NARA property?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false Is smoking allowed on NARA property? 1280.24 Section 1280.24 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS...? Prohibited Activities § 1280.24 Is smoking allowed on NARA property? Smoking is not allowed inside any NARA...

  8. 8 CFR 1280.14 - Record.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 8 Aliens and Nationality 1 2012-01-01 2012-01-01 false Record. 1280.14 Section 1280.14 Aliens and... AND COLLECTION OF FINES § 1280.14 Record. Link to an amendment published at 76 FR 74630, December 1, 2011. The record made under § 1280.13 shall include the request for the interview or a reference to the...

  9. 32 CFR 1280.2 - Definitions.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 32 National Defense 6 2010-07-01 2010-07-01 false Definitions. 1280.2 Section 1280.2 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.2 Definitions...

  10. 7 CFR 1280.120 - Research.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false Research. 1280.120 Section 1280.120 Agriculture... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.120 Research. Research...

  11. 7 CFR 1280.120 - Research.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Research. 1280.120 Section 1280.120 Agriculture... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.120 Research. Research...

  12. 7 CFR 1280.120 - Research.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false Research. 1280.120 Section 1280.120 Agriculture... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.120 Research. Research...

  13. 7 CFR 1280.120 - Research.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Research. 1280.120 Section 1280.120 Agriculture... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.120 Research. Research...

  14. 7 CFR 1280.120 - Research.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Research. 1280.120 Section 1280.120 Agriculture... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.120 Research. Research...

  15. 32 CFR 1280.2 - Definitions.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 32 National Defense 6 2014-07-01 2014-07-01 false Definitions. 1280.2 Section 1280.2 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.2 Definitions...

  16. 32 CFR 1280.2 - Definitions.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 32 National Defense 6 2013-07-01 2013-07-01 false Definitions. 1280.2 Section 1280.2 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.2 Definitions...

  17. 32 CFR 1280.2 - Definitions.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 32 National Defense 6 2011-07-01 2011-07-01 false Definitions. 1280.2 Section 1280.2 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.2 Definitions...

  18. 32 CFR 1280.2 - Definitions.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 32 National Defense 6 2012-07-01 2012-07-01 false Definitions. 1280.2 Section 1280.2 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.2 Definitions...

  19. 7 CFR 1280.111 - Lamb.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Lamb. 1280.111 Section 1280.111 Agriculture... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.111 Lamb. Lamb means...

  20. 36 CFR § 1280.24 - Is smoking allowed on NARA property?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true Is smoking allowed on NARA property? § 1280.24 Section § 1280.24 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS...? Prohibited Activities § 1280.24 Is smoking allowed on NARA property? Smoking is not allowed inside any NARA...

  1. 7 CFR 1280.110 - Information.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false Information. 1280.110 Section 1280.110 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.110 Information. Information means information and programs that are designed to increase efficiency in producing lambs, to...

  2. 7 CFR 1280.110 - Information.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false Information. 1280.110 Section 1280.110 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.110 Information. Information means information and programs that are designed to increase efficiency in producing lambs, to...

  3. 7 CFR 1280.110 - Information.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Information. 1280.110 Section 1280.110 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.110 Information. Information means information and programs that are designed to increase efficiency in producing lambs, to...

  4. 7 CFR 1280.110 - Information.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Information. 1280.110 Section 1280.110 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.110 Information. Information means information and programs that are designed to increase efficiency in producing lambs, to...

  5. 7 CFR 1280.110 - Information.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Information. 1280.110 Section 1280.110 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.110 Information. Information means information and programs that are designed to increase efficiency in producing lambs, to...

  6. 7 CFR 1280.624 - Facilities.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Facilities. 1280.624 Section 1280.624 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.624 Facilities. Each county FSA office...

  7. 49 CFR 1280.2 - Policy.

    Code of Federal Regulations, 2014 CFR

    2014-10-01

    ... 49 Transportation 9 2014-10-01 2014-10-01 false Policy. 1280.2 Section 1280.2 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION BOARD, DEPARTMENT OF TRANSPORTATION... § 1280.2 Policy. It is the policy of the Surface Transportation Board to act in accordance with Executive...

  8. 7 CFR 1280.121 - Secretary.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false Secretary. 1280.121 Section 1280.121 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.121 Secretary. Secretary means the Secretary of Agriculture of the United States or any other officer or employee of the...

  9. 7 CFR 1280.121 - Secretary.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Secretary. 1280.121 Section 1280.121 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.121 Secretary. Secretary means the Secretary of Agriculture of the United States or any other officer or employee of the...

  10. 7 CFR 1280.121 - Secretary.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Secretary. 1280.121 Section 1280.121 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.121 Secretary. Secretary means the Secretary of Agriculture of the United States or any other officer or employee of the...

  11. 7 CFR 1280.121 - Secretary.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false Secretary. 1280.121 Section 1280.121 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.121 Secretary. Secretary means the Secretary of Agriculture of the United States or any other officer or employee of the...

  12. Profiling the NIH Small Molecule Repository for Compounds That Generate H2O2 by Redox Cycling in Reducing Environments

    PubMed Central

    2010-01-01

    We have screened the Library of Pharmacologically Active Compounds (LOPAC) and the National Institutes of Health (NIH) Small Molecule Repository (SMR) libraries in a horseradish peroxidase–phenol red (HRP-PR) H2O2 detection assay to identify redox cycling compounds (RCCs) capable of generating H2O2 in buffers containing dithiothreitol (DTT). Two RCCs were identified in the LOPAC set, the ortho-naphthoquinone β-lapachone and the para-naphthoquinone NSC 95397. Thirty-seven (0.02%) concentration-dependent RCCs were identified from 195,826 compounds in the NIH SMR library; 3 singleton structures, 9 ortho-quinones, 2 para-quinones, 4 pyrimidotriazinediones, 15 arylsulfonamides, 2 nitrothiophene-2-carboxylates, and 2 tolyl hydrazides. Sixty percent of the ortho-quinones and 80% of the pyrimidotriazinediones in the library were confirmed as RCCs. In contrast, only 3.9% of the para-quinones were confirmed as RCCs. Fifteen of the 251 arylsulfonamides in the library were confirmed as RCCs, and since we screened 17,868 compounds with a sulfonamide functional group we conclude that the redox cycling activity of the arylsulfonamide RCCs is due to peripheral reactive enone, aromatic, or heterocyclic functions. Cross-target queries of the University of Pittsburgh Drug Discovery Institute (UPDDI) and PubChem databases revealed that the RCCs exhibited promiscuous bioactivity profiles and have populated both screening databases with significantly higher numbers of active flags than non-RCCs. RCCs were promiscuously active against protein targets known to be susceptible to oxidation, but were also active in cell growth inhibition assays, and against other targets thought to be insensitive to oxidation. Profiling compound libraries or the hits from screening campaigns in the HRP-PR H2O2 detection assay significantly reduce the timelines and resources required to identify and eliminate promiscuous nuisance RCCs from the candidates for lead optimization. PMID:20070233

  13. 7 CFR 1280.127 - United States.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false United States. 1280.127 Section 1280.127 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.127 United States. United States means collectively the 50 States and the District of Columbia. ...

  14. 7 CFR 1280.127 - United States.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false United States. 1280.127 Section 1280.127 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.127 United States. United States means collectively the 50 States and the District of Columbia. ...

  15. 7 CFR 1280.127 - United States.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false United States. 1280.127 Section 1280.127 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.127 United States. United States means collectively the 50 States and the District of Columbia. ...

  16. 7 CFR 1280.127 - United States.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false United States. 1280.127 Section 1280.127 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.127 United States. United States means collectively the 50 States and the District of Columbia. ...

  17. 32 CFR 1280.3 - Significant changes.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 32 National Defense 6 2010-07-01 2010-07-01 false Significant changes. 1280.3 Section 1280.3 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.3 Significant...

  18. 32 CFR 1280.3 - Significant changes.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 32 National Defense 6 2013-07-01 2013-07-01 false Significant changes. 1280.3 Section 1280.3 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.3 Significant...

  19. 32 CFR 1280.3 - Significant changes.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 32 National Defense 6 2014-07-01 2014-07-01 false Significant changes. 1280.3 Section 1280.3 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.3 Significant...

  20. 32 CFR 1280.3 - Significant changes.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 32 National Defense 6 2012-07-01 2012-07-01 false Significant changes. 1280.3 Section 1280.3 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.3 Significant...

  1. 32 CFR 1280.3 - Significant changes.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 32 National Defense 6 2011-07-01 2011-07-01 false Significant changes. 1280.3 Section 1280.3 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.3 Significant...

  2. 7 CFR 1280.112 - Lamb products.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Lamb products. 1280.112 Section 1280.112 Agriculture... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.112 Lamb products. Lamb...

  3. 7 CFR 1280.217 - Lamb purchases.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Lamb purchases. 1280.217 Section 1280.217 Agriculture... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Assessments § 1280.217 Lamb purchases. (a...

  4. 21 CFR 870.1280 - Steerable catheter.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 8 2011-04-01 2011-04-01 false Steerable catheter. 870.1280 Section 870.1280 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES CARDIOVASCULAR DEVICES Cardiovascular Diagnostic Devices § 870.1280 Steerable catheter. (a...

  5. 21 CFR 870.1280 - Steerable catheter.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Steerable catheter. 870.1280 Section 870.1280 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES CARDIOVASCULAR DEVICES Cardiovascular Diagnostic Devices § 870.1280 Steerable catheter. (a...

  6. 36 CFR 1280.20 - What is your policy on illegal drugs and alcohol?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... illegal drugs and alcohol? 1280.20 Section 1280.20 Parks, Forests, and Public Property NATIONAL ARCHIVES... Conduct on NARA Property? Prohibited Activities § 1280.20 What is your policy on illegal drugs and alcohol? You may not use or be in possession of illegal drugs on NARA property. You also may not enter NARA...

  7. 36 CFR 1280.20 - What is your policy on illegal drugs and alcohol?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... illegal drugs and alcohol? 1280.20 Section 1280.20 Parks, Forests, and Public Property NATIONAL ARCHIVES... Conduct on NARA Property? Prohibited Activities § 1280.20 What is your policy on illegal drugs and alcohol? You may not use or be in possession of illegal drugs on NARA property. You also may not enter NARA...

  8. 36 CFR 1280.20 - What is your policy on illegal drugs and alcohol?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... illegal drugs and alcohol? 1280.20 Section 1280.20 Parks, Forests, and Public Property NATIONAL ARCHIVES... Conduct on NARA Property? Prohibited Activities § 1280.20 What is your policy on illegal drugs and alcohol? You may not use or be in possession of illegal drugs on NARA property. You also may not enter NARA...

  9. 36 CFR 1280.20 - What is your policy on illegal drugs and alcohol?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... illegal drugs and alcohol? 1280.20 Section 1280.20 Parks, Forests, and Public Property NATIONAL ARCHIVES... Conduct on NARA Property? Prohibited Activities § 1280.20 What is your policy on illegal drugs and alcohol? You may not use or be in possession of illegal drugs on NARA property. You also may not enter NARA...

  10. 36 CFR 1280.18 - May I bring guns or other weapons onto NARA property?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false May I bring guns or other weapons onto NARA property? 1280.18 Section 1280.18 Parks, Forests, and Public Property NATIONAL ARCHIVES... Conduct on NARA Property? Prohibited Activities § 1280.18 May I bring guns or other weapons onto NARA...

  11. 36 CFR 1280.18 - May I bring guns or other weapons onto NARA property?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false May I bring guns or other weapons onto NARA property? 1280.18 Section 1280.18 Parks, Forests, and Public Property NATIONAL ARCHIVES... Conduct on NARA Property? Prohibited Activities § 1280.18 May I bring guns or other weapons onto NARA...

  12. 36 CFR 1280.18 - May I bring guns or other weapons onto NARA property?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false May I bring guns or other weapons onto NARA property? 1280.18 Section 1280.18 Parks, Forests, and Public Property NATIONAL ARCHIVES... Conduct on NARA Property? Prohibited Activities § 1280.18 May I bring guns or other weapons onto NARA...

  13. 36 CFR 1280.18 - May I bring guns or other weapons onto NARA property?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false May I bring guns or other weapons onto NARA property? 1280.18 Section 1280.18 Parks, Forests, and Public Property NATIONAL ARCHIVES... Conduct on NARA Property? Prohibited Activities § 1280.18 May I bring guns or other weapons onto NARA...

  14. 7 CFR 1280.102 - Board.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.102 Board. Board means the Lamb Promotion, Research, and Information Board established pursuant to § 1280.201. ...

  15. 49 CFR 1280.7 - Education of employees.

    Code of Federal Regulations, 2011 CFR

    2011-10-01

    ... 49 Transportation 9 2011-10-01 2011-10-01 false Education of employees. 1280.7 Section 1280.7 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION BOARD, DEPARTMENT... AND CLASSIFIED MATERIAL § 1280.7 Education of employees. All employees who have been granted a...

  16. 49 CFR 1280.7 - Education of employees.

    Code of Federal Regulations, 2014 CFR

    2014-10-01

    ... 49 Transportation 9 2014-10-01 2014-10-01 false Education of employees. 1280.7 Section 1280.7 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION BOARD, DEPARTMENT... AND CLASSIFIED MATERIAL § 1280.7 Education of employees. All employees who have been granted a...

  17. 49 CFR 1280.7 - Education of employees.

    Code of Federal Regulations, 2013 CFR

    2013-10-01

    ... 49 Transportation 9 2013-10-01 2013-10-01 false Education of employees. 1280.7 Section 1280.7 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION BOARD, DEPARTMENT... AND CLASSIFIED MATERIAL § 1280.7 Education of employees. All employees who have been granted a...

  18. 49 CFR 1280.7 - Education of employees.

    Code of Federal Regulations, 2012 CFR

    2012-10-01

    ... 49 Transportation 9 2012-10-01 2012-10-01 false Education of employees. 1280.7 Section 1280.7 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION BOARD, DEPARTMENT... AND CLASSIFIED MATERIAL § 1280.7 Education of employees. All employees who have been granted a...

  19. 49 CFR 1280.7 - Education of employees.

    Code of Federal Regulations, 2010 CFR

    2010-10-01

    ... 49 Transportation 9 2010-10-01 2010-10-01 false Education of employees. 1280.7 Section 1280.7 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION BOARD, DEPARTMENT... AND CLASSIFIED MATERIAL § 1280.7 Education of employees. All employees who have been granted a...

  20. 7 CFR 1280.117 - Producer information.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.117 Producer information. Producer information means activities designed to provide producers, feeders, and first handlers with...

  1. 32 CFR 1280.1 - Purpose and scope.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 32 National Defense 6 2010-07-01 2010-07-01 false Purpose and scope. 1280.1 Section 1280.1 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.1 Purpose and...

  2. 32 CFR 1280.1 - Purpose and scope.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 32 National Defense 6 2012-07-01 2012-07-01 false Purpose and scope. 1280.1 Section 1280.1 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.1 Purpose and...

  3. 32 CFR 1280.1 - Purpose and scope.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 32 National Defense 6 2011-07-01 2011-07-01 false Purpose and scope. 1280.1 Section 1280.1 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.1 Purpose and...

  4. 32 CFR 1280.1 - Purpose and scope.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 32 National Defense 6 2013-07-01 2013-07-01 false Purpose and scope. 1280.1 Section 1280.1 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.1 Purpose and...

  5. 32 CFR 1280.1 - Purpose and scope.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 32 National Defense 6 2014-07-01 2014-07-01 false Purpose and scope. 1280.1 Section 1280.1 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS INVESTIGATING AND PROCESSING CERTAIN NONCONTRACTUAL CLAIMS AND REPORTING RELATED LITIGATION § 1280.1 Purpose and...

  6. 32 CFR 1280.4 - Responsibilities.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 32 National Defense 6 2010-07-01 2010-07-01 false Responsibilities. 1280.4 Section 1280.4 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS... Support Center (DLASC) is responsible for designating a qualified individual, preferably one experienced...

  7. 32 CFR 1280.4 - Responsibilities.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 32 National Defense 6 2011-07-01 2011-07-01 false Responsibilities. 1280.4 Section 1280.4 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS... Support Center (DLASC) is responsible for designating a qualified individual, preferably one experienced...

  8. 32 CFR 1280.4 - Responsibilities.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 32 National Defense 6 2014-07-01 2014-07-01 false Responsibilities. 1280.4 Section 1280.4 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS... Support Center (DLASC) is responsible for designating a qualified individual, preferably one experienced...

  9. 32 CFR 1280.4 - Responsibilities.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 32 National Defense 6 2013-07-01 2013-07-01 false Responsibilities. 1280.4 Section 1280.4 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS... Support Center (DLASC) is responsible for designating a qualified individual, preferably one experienced...

  10. 32 CFR 1280.4 - Responsibilities.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 32 National Defense 6 2012-07-01 2012-07-01 false Responsibilities. 1280.4 Section 1280.4 National Defense Other Regulations Relating to National Defense DEFENSE LOGISTICS AGENCY MISCELLANEOUS... Support Center (DLASC) is responsible for designating a qualified individual, preferably one experienced...

  11. 7 CFR 1280.634 - Confidentiality.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false Confidentiality. 1280.634 Section 1280.634 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING... persons voting in the referendum and ballots shall be confidential and the contents of the ballots shall...

  12. 7 CFR 1280.634 - Confidentiality.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Confidentiality. 1280.634 Section 1280.634 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING... persons voting in the referendum and ballots shall be confidential and the contents of the ballots shall...

  13. 7 CFR 1280.634 - Confidentiality.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false Confidentiality. 1280.634 Section 1280.634 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING... persons voting in the referendum and ballots shall be confidential and the contents of the ballots shall...

  14. 7 CFR 1280.634 - Confidentiality.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Confidentiality. 1280.634 Section 1280.634 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING... persons voting in the referendum and ballots shall be confidential and the contents of the ballots shall...

  15. 7 CFR 1280.634 - Confidentiality.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Confidentiality. 1280.634 Section 1280.634 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING... persons voting in the referendum and ballots shall be confidential and the contents of the ballots shall...

  16. 7 CFR 1280.405 - Books and records.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Books and records. 1280.405 Section 1280.405... INFORMATION ORDER Rules and Regulations § 1280.405 Books and records. (a) Each first handler, exporter of... by representatives of the Secretary, such books and records as are necessary to carry out the...

  17. 7 CFR 1280.405 - Books and records.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Books and records. 1280.405 Section 1280.405... INFORMATION ORDER Rules and Regulations § 1280.405 Books and records. (a) Each first handler, exporter of... by representatives of the Secretary, such books and records as are necessary to carry out the...

  18. 7 CFR 1280.405 - Books and records.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false Books and records. 1280.405 Section 1280.405... INFORMATION ORDER Rules and Regulations § 1280.405 Books and records. (a) Each first handler, exporter of... by representatives of the Secretary, such books and records as are necessary to carry out the...

  19. 7 CFR 1280.405 - Books and records.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false Books and records. 1280.405 Section 1280.405... INFORMATION ORDER Rules and Regulations § 1280.405 Books and records. (a) Each first handler, exporter of... by representatives of the Secretary, such books and records as are necessary to carry out the...

  20. 7 CFR 1280.405 - Books and records.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Books and records. 1280.405 Section 1280.405... INFORMATION ORDER Rules and Regulations § 1280.405 Books and records. (a) Each first handler, exporter of... by representatives of the Secretary, such books and records as are necessary to carry out the...

  1. 7 CFR 1280.213 - Investment of funds.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Investment of funds. 1280.213 Section 1280.213... INFORMATION ORDER Lamb Promotion, Research, and Information Order Expenses § 1280.213 Investment of funds. The... the United States. Income from any such investment may be used for any purpose for which the invested...

  2. 7 CFR 1280.213 - Investment of funds.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Investment of funds. 1280.213 Section 1280.213... INFORMATION ORDER Lamb Promotion, Research, and Information Order Expenses § 1280.213 Investment of funds. The... the United States. Income from any such investment may be used for any purpose for which the invested...

  3. 7 CFR 1280.118 - Promotion.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... information and public relations with emphasis on new marketing strategies, to present a favorable image of U... 7 Agriculture 10 2010-01-01 2010-01-01 false Promotion. 1280.118 Section 1280.118 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS...

  4. 36 CFR § 1280.18 - May I bring guns or other weapons onto NARA property?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true May I bring guns or other weapons onto NARA property? § 1280.18 Section § 1280.18 Parks, Forests, and Public Property NATIONAL... Conduct on NARA Property? Prohibited Activities § 1280.18 May I bring guns or other weapons onto NARA...

  5. 8 CFR 1280.21 - Seizure of aircraft.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 8 Aliens and Nationality 1 2010-01-01 2010-01-01 false Seizure of aircraft. 1280.21 Section 1280... REGULATIONS IMPOSITION AND COLLECTION OF FINES § 1280.21 Seizure of aircraft. Seizure of an aircraft under the... that its value is less than the amount of the fine which may be imposed. If seizure of an aircraft for...

  6. 49 CFR 1280.6 - Storage of classified documents.

    Code of Federal Regulations, 2012 CFR

    2012-10-01

    ... 49 Transportation 9 2012-10-01 2012-10-01 false Storage of classified documents. 1280.6 Section 1280.6 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION... SECURITY INFORMATION AND CLASSIFIED MATERIAL § 1280.6 Storage of classified documents. All classified...

  7. 49 CFR 1280.6 - Storage of classified documents.

    Code of Federal Regulations, 2011 CFR

    2011-10-01

    ... 49 Transportation 9 2011-10-01 2011-10-01 false Storage of classified documents. 1280.6 Section 1280.6 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION... SECURITY INFORMATION AND CLASSIFIED MATERIAL § 1280.6 Storage of classified documents. All classified...

  8. 49 CFR 1280.6 - Storage of classified documents.

    Code of Federal Regulations, 2010 CFR

    2010-10-01

    ... 49 Transportation 9 2010-10-01 2010-10-01 false Storage of classified documents. 1280.6 Section 1280.6 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION... SECURITY INFORMATION AND CLASSIFIED MATERIAL § 1280.6 Storage of classified documents. All classified...

  9. 49 CFR 1280.6 - Storage of classified documents.

    Code of Federal Regulations, 2014 CFR

    2014-10-01

    ... 49 Transportation 9 2014-10-01 2014-10-01 false Storage of classified documents. 1280.6 Section 1280.6 Transportation Other Regulations Relating to Transportation (Continued) SURFACE TRANSPORTATION... SECURITY INFORMATION AND CLASSIFIED MATERIAL § 1280.6 Storage of classified documents. All classified...

  10. 7 CFR 1280.401 - Terms defined.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Terms defined. 1280.401 Section 1280.401 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND...

  11. 7 CFR 1280.631 - Results of the referendum.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false Results of the referendum. 1280.631 Section 1280.631... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.631 Results of the referendum. (a) The... Administrator, AMS, shall tabulate the results of the ballots. USDA will issue an official press release...

  12. 7 CFR 1280.631 - Results of the referendum.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Results of the referendum. 1280.631 Section 1280.631... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.631 Results of the referendum. (a) The... Administrator, AMS, shall tabulate the results of the ballots. USDA will issue an official press release...

  13. 7 CFR 1280.631 - Results of the referendum.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Results of the referendum. 1280.631 Section 1280.631... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.631 Results of the referendum. (a) The... Administrator, AMS, shall tabulate the results of the ballots. USDA will issue an official press release...

  14. 7 CFR 1280.631 - Results of the referendum.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false Results of the referendum. 1280.631 Section 1280.631... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.631 Results of the referendum. (a) The... Administrator, AMS, shall tabulate the results of the ballots. USDA will issue an official press release...

  15. 7 CFR 1280.631 - Results of the referendum.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Results of the referendum. 1280.631 Section 1280.631... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.631 Results of the referendum. (a) The... Administrator, AMS, shall tabulate the results of the ballots. USDA will issue an official press release...

  16. 10 CFR 603.1280 - Institution of higher education.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 10 Energy 4 2011-01-01 2011-01-01 false Institution of higher education. 603.1280 Section 603.1280... Definitions of Terms Used in this Part § 603.1280 Institution of higher education. An educational institution that: (a) Meets the criteria in section 101 of the Higher Education Act of 1965 (20 U.S.C. 1001); and...

  17. 10 CFR 603.1280 - Institution of higher education.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 10 Energy 4 2014-01-01 2014-01-01 false Institution of higher education. 603.1280 Section 603.1280... Definitions of Terms Used in this Part § 603.1280 Institution of higher education. An educational institution that: (a) Meets the criteria in section 101 of the Higher Education Act of 1965 (20 U.S.C. 1001); and...

  18. 10 CFR 603.1280 - Institution of higher education.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 10 Energy 4 2012-01-01 2012-01-01 false Institution of higher education. 603.1280 Section 603.1280... Definitions of Terms Used in this Part § 603.1280 Institution of higher education. An educational institution that: (a) Meets the criteria in section 101 of the Higher Education Act of 1965 (20 U.S.C. 1001); and...

  19. 10 CFR 603.1280 - Institution of higher education.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 10 Energy 4 2013-01-01 2013-01-01 false Institution of higher education. 603.1280 Section 603.1280... Definitions of Terms Used in this Part § 603.1280 Institution of higher education. An educational institution that: (a) Meets the criteria in section 101 of the Higher Education Act of 1965 (20 U.S.C. 1001); and...

  20. 10 CFR 603.1280 - Institution of higher education.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 10 Energy 4 2010-01-01 2010-01-01 false Institution of higher education. 603.1280 Section 603.1280... Definitions of Terms Used in this Part § 603.1280 Institution of higher education. An educational institution that: (a) Meets the criteria in section 101 of the Higher Education Act of 1965 (20 U.S.C. 1001); and...

  1. 8 CFR 1280.4 - Data concerning cost of transportation.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 8 Aliens and Nationality 1 2010-01-01 2010-01-01 false Data concerning cost of transportation. 1280.4 Section 1280.4 Aliens and Nationality EXECUTIVE OFFICE FOR IMMIGRATION REVIEW, DEPARTMENT OF JUSTICE IMMIGRATION REGULATIONS IMPOSITION AND COLLECTION OF FINES § 1280.4 Data concerning cost of...

  2. 7 CFR 1280.225 - Books and records of persons.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Books and records of persons. 1280.225 Section 1280... PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.225 Books and records of persons. (a) Each first handler, exporter of lambs, and...

  3. 7 CFR 1280.225 - Books and records of persons.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Books and records of persons. 1280.225 Section 1280... PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.225 Books and records of persons. (a) Each first handler, exporter of lambs, and...

  4. 7 CFR 1280.225 - Books and records of persons.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false Books and records of persons. 1280.225 Section 1280... PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.225 Books and records of persons. (a) Each first handler, exporter of lambs, and...

  5. 7 CFR 1280.225 - Books and records of persons.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Books and records of persons. 1280.225 Section 1280... PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.225 Books and records of persons. (a) Each first handler, exporter of lambs, and...

  6. 7 CFR 1280.225 - Books and records of persons.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false Books and records of persons. 1280.225 Section 1280... PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.225 Books and records of persons. (a) Each first handler, exporter of lambs, and...

  7. 7 CFR 1280.222 - Books and Records of Board.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false Books and Records of Board. 1280.222 Section 1280.222... INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.222 Books and Records of Board. The Board shall: (a) Maintain such books and records, which shall be made...

  8. 7 CFR 1280.222 - Books and Records of Board.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 10 2012-01-01 2012-01-01 false Books and Records of Board. 1280.222 Section 1280.222... INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.222 Books and Records of Board. The Board shall: (a) Maintain such books and records, which shall be made...

  9. 7 CFR 1280.222 - Books and Records of Board.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 10 2013-01-01 2013-01-01 false Books and Records of Board. 1280.222 Section 1280.222... INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.222 Books and Records of Board. The Board shall: (a) Maintain such books and records, which shall be made...

  10. 7 CFR 1280.222 - Books and Records of Board.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 10 2011-01-01 2011-01-01 false Books and Records of Board. 1280.222 Section 1280.222... INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.222 Books and Records of Board. The Board shall: (a) Maintain such books and records, which shall be made...

  11. 7 CFR 1280.222 - Books and Records of Board.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 10 2014-01-01 2014-01-01 false Books and Records of Board. 1280.222 Section 1280.222... INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.222 Books and Records of Board. The Board shall: (a) Maintain such books and records, which shall be made...

  12. 7 CFR 1280.238 - OMB Control Numbers.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 10 2010-01-01 2010-01-01 false OMB Control Numbers. 1280.238 Section 1280.238 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING.... The control number for the information requirements assigned by the Office of Management and Budget...

  13. 21 CFR 862.1280 - Estrone test system.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Estrone test system. 862.1280 Section 862.1280 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES CLINICAL CHEMISTRY AND CLINICAL TOXICOLOGY DEVICES Clinical Chemistry Test Systems § 862...

  14. 21 CFR 862.1280 - Estrone test system.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 8 2011-04-01 2011-04-01 false Estrone test system. 862.1280 Section 862.1280 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES CLINICAL CHEMISTRY AND CLINICAL TOXICOLOGY DEVICES Clinical Chemistry Test Systems § 862...

  15. 21 CFR 862.1280 - Estrone test system.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 8 2014-04-01 2014-04-01 false Estrone test system. 862.1280 Section 862.1280 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES CLINICAL CHEMISTRY AND CLINICAL TOXICOLOGY DEVICES Clinical Chemistry Test Systems § 862...

  16. 21 CFR 862.1280 - Estrone test system.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 8 2012-04-01 2012-04-01 false Estrone test system. 862.1280 Section 862.1280 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES CLINICAL CHEMISTRY AND CLINICAL TOXICOLOGY DEVICES Clinical Chemistry Test Systems § 862...

  17. High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe.

    PubMed

    McCallum, Megan M; Nandhikonda, Premchendar; Temmer, Jonathan J; Eyermann, Charles; Simeonov, Anton; Jadhav, Ajit; Yasgar, Adam; Maloney, David; Arnold, Alexander Leggy

    2013-07-01

    Testing small molecules for their ability to modify cysteine residues of proteins in the early stages of drug discovery is expected to accelerate our ability to develop more selective drugs with lesser side effects. In addition, this approach also enables the rapid evaluation of the mode of binding of new drug candidates with respect to thiol reactivity and metabolism by glutathione. Herein, we describe the development of a fluorescence-based high-throughput assay that allows the identification of thiol-reactive compounds. A thiol-containing fluorescent probe, MSTI, was synthesized and used to evaluate small molecules from the Library of Pharmacologically Active Compounds (LOPAC) collection of bioactive molecules. LOPAC compounds that are known to react with sulfur nucleophiles were identified with this assay, for example, irreversible protease inhibitors, nitric oxide-releasing compounds, and proton-pump inhibitors. The results confirm that both electrophilic and redox reactive compounds can be quickly identified in a high-throughput manner, enabling the assessment of screening libraries with respect to thiol-reactive compounds.

  18. 36 CFR 1280.66 - May I use the National Archives Library?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... Archives Library? 1280.66 Section 1280.66 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS... the Washington, DC, Area? § 1280.66 May I use the National Archives Library? The National Archives Library facilities in the National Archives Building and in the National Archives at College Park are...

  19. 36 CFR 1280.66 - May I use the National Archives Library?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... Archives Library? 1280.66 Section 1280.66 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS... the Washington, DC, Area? § 1280.66 May I use the National Archives Library? The National Archives Library facilities in the National Archives Building and in the National Archives at College Park are...

  20. 36 CFR 1280.66 - May I use the National Archives Library?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... Archives Library? 1280.66 Section 1280.66 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS... the Washington, DC, Area? § 1280.66 May I use the National Archives Library? The National Archives Library facilities in the National Archives Building and in the National Archives at College Park are...

  1. 36 CFR 1280.66 - May I use the National Archives Library?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... Archives Library? 1280.66 Section 1280.66 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS... the Washington, DC, Area? § 1280.66 May I use the National Archives Library? The National Archives Library facilities in the National Archives Building and in the National Archives at College Park are...

  2. 7 CFR 1280.105 - Department.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.105 Department...

  3. 7 CFR 1280.119 - Referendum.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.119 Referendum...

  4. 7 CFR 1280.232 - Amendments.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Miscellaneous § 1280.232 Amendments...

  5. 26 CFR 1.280F-6 - Special rules and definitions.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... purpose, e.g., commuting to work, is reported by X as income to the employee and is withheld upon by X... service before July 7, 2003, see § 1.280F-6T as in effect prior to July 7, 2003 (§ 1.280F-6T as contained... automobile under § 1.280F-6T as in effect prior to July 7, 2003 (pre-effective date vehicle): (i) Except as...

  6. 26 CFR 1.280F-6 - Special rules and definitions.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... purpose, e.g., commuting to work, is reported by X as income to the employee and is withheld upon by X... service before July 7, 2003, see § 1.280F-6T as in effect prior to July 7, 2003 (§ 1.280F-6T as contained... automobile under § 1.280F-6T as in effect prior to July 7, 2003 (pre-effective date vehicle): (i) Except as...

  7. 26 CFR 1.280F-6 - Special rules and definitions.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... purpose, e.g., commuting to work, is reported by X as income to the employee and is withheld upon by X... service before July 7, 2003, see § 1.280F-6T as in effect prior to July 7, 2003 (§ 1.280F-6T as contained... automobile under § 1.280F-6T as in effect prior to July 7, 2003 (pre-effective date vehicle): (i) Except as...

  8. 26 CFR 1.280F-6 - Special rules and definitions.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... purpose, e.g., commuting to work, is reported by X as income to the employee and is withheld upon by X... service before July 7, 2003, see § 1.280F-6T as in effect prior to July 7, 2003 (§ 1.280F-6T as contained... automobile under § 1.280F-6T as in effect prior to July 7, 2003 (pre-effective date vehicle): (i) Except as...

  9. 7 CFR 1280.121 - Secretary.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.121 Secretary. Secretary...

  10. 7 CFR 1280.230 - Separability.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Miscellaneous § 1280.230 Separability. If...

  11. 7 CFR 1280.124 - Suspend.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.124 Suspend. Suspend...

  12. 7 CFR 1280.125 - Terminate.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.125 Terminate. Terminate...

  13. 7 CFR 1280.123 - State.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.123 State. State means...

  14. 7 CFR 1280.115 - Person.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.115 Person. Person means...

  15. 7 CFR 1280.215 - Refunds.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Expenses § 1280.215 Refunds. Any producer...

  16. 40 CFR 52.1280 - Significant deterioration of air quality.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... quality. 52.1280 Section 52.1280 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) AIR... Significant deterioration of air quality. (a) All applications and other information required pursuant to § 52... Address: Mississippi Department of Environmental Quality, Office of Pollution Control, Air Division, P.O...

  17. 40 CFR 52.1280 - Significant deterioration of air quality.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... quality. 52.1280 Section 52.1280 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) AIR... Significant deterioration of air quality. (a) All applications and other information required pursuant to § 52... Address: Mississippi Department of Environmental Quality, Office of Pollution Control, Air Division, P.O...

  18. 40 CFR 52.1280 - Significant deterioration of air quality.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... quality. 52.1280 Section 52.1280 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) AIR... Significant deterioration of air quality. (a) All applications and other information required pursuant to § 52... Address: Mississippi Department of Environmental Quality, Office of Pollution Control, Air Division, P.O...

  19. 7 CFR 1280.101 - Act.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.101 Act. Act means the...

  20. 7 CFR 1280.227 - Confidentiality.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.227...

  1. 7 CFR 1280.126 - Unit.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.126 Unit. Unit means each...

  2. 7 CFR 1280.113 - Order.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.113 Order. Order means an...

  3. 40 CFR 52.1280 - Significant deterioration of air quality.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 40 Protection of Environment 4 2010-07-01 2010-07-01 false Significant deterioration of air quality. 52.1280 Section 52.1280 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) AIR... Significant deterioration of air quality. (a) All applications and other information required pursuant to § 52...

  4. 40 CFR 52.1280 - Significant deterioration of air quality.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 4 2011-07-01 2011-07-01 false Significant deterioration of air quality. 52.1280 Section 52.1280 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) AIR... Significant deterioration of air quality. (a) All applications and other information required pursuant to § 52...

  5. 36 CFR § 1280.66 - May I use the National Archives Library?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... Archives Library? § 1280.66 Section § 1280.66 Parks, Forests, and Public Property NATIONAL ARCHIVES AND... Facilities in the Washington, DC, Area? § 1280.66 May I use the National Archives Library? The National Archives Library facilities in the National Archives Building and in the National Archives at College Park...

  6. 8 CFR 1280.51 - Application for mitigation or remission.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 8 Aliens and Nationality 1 2012-01-01 2012-01-01 false Application for mitigation or remission... JUSTICE IMMIGRATION REGULATIONS IMPOSITION AND COLLECTION OF FINES § 1280.51 Application for mitigation or... filed. An application for mitigation or remission of a fine may be filed as provided under § 1280.12 of...

  7. 8 CFR 1280.5 - Mitigation or remission of fines.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 8 Aliens and Nationality 1 2011-01-01 2011-01-01 false Mitigation or remission of fines. 1280.5... IMMIGRATION REGULATIONS IMPOSITION AND COLLECTION OF FINES § 1280.5 Mitigation or remission of fines. In any case in which mitigation or remission of a fine is authorized by the Immigration and Nationality Act...

  8. 8 CFR 1280.5 - Mitigation or remission of fines.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 8 Aliens and Nationality 1 2010-01-01 2010-01-01 false Mitigation or remission of fines. 1280.5... IMMIGRATION REGULATIONS IMPOSITION AND COLLECTION OF FINES § 1280.5 Mitigation or remission of fines. In any case in which mitigation or remission of a fine is authorized by the Immigration and Nationality Act...

  9. 7 CFR 1280.128 - Wool.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.128 Wool. Wool means fiber from the fleece of a lamb. ...

  10. 8 CFR 1280.5 - Mitigation or remission of fines.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 8 Aliens and Nationality 1 2012-01-01 2012-01-01 false Mitigation or remission of fines. 1280.5... IMMIGRATION REGULATIONS IMPOSITION AND COLLECTION OF FINES § 1280.5 Mitigation or remission of fines. Link to an amendment published at 76 FR 74630, December 1, 2011. In any case in which mitigation or remission...

  11. 26 CFR 1.280B-1 - Demolition of structures.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 26 Internal Revenue 3 2010-04-01 2010-04-01 false Demolition of structures. 1.280B-1 Section 1... (CONTINUED) INCOME TAXES Items Not Deductible § 1.280B-1 Demolition of structures. (a) In general. Section 280B provides that, in the case of the demolition of any structure, no deduction otherwise allowable...

  12. 7 CFR 1280.111 - Lamb.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.111 Lamb. Lamb means ovine animals of any age, including ewes and rams. ...

  13. 7 CFR 1280.111 - Lamb.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.111 Lamb. Lamb means ovine animals of any age, including ewes and rams. ...

  14. 7 CFR 1280.111 - Lamb.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.111 Lamb. Lamb means ovine animals of any age, including ewes and rams. ...

  15. 7 CFR 1280.111 - Lamb.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.111 Lamb. Lamb means ovine animals of any age, including ewes and rams. ...

  16. 7 CFR 1280.402 - Assessments.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... Secretary at USDA, 23029 Network Place, Chicago, Illinois 60673-1230, with a “Monthly Remittance Report... assessments due to the Board pursuant to § 1280.217 shall be increased 2 percent each month beginning with the...

  17. 7 CFR 1280.103 - Certified organization.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.103 Certified...

  18. 7 CFR 1280.106 - Exporter.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.106 Exporter. Exporter means any person who exports domestic live lambs from the United States. ...

  19. 7 CFR 1280.229 - Personal liability.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Miscellaneous § 1280.229 Personal liability...

  20. 7 CFR 1280.127 - United States.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.127 United States. United...

  1. 36 CFR 1280.32 - What other behavior is not permitted?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false What other behavior is not permitted? 1280.32 Section 1280.32 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS..., electronic mail, or phone) any NARA employee, visitor, volunteer, contractor, other building occupants, or...

  2. 36 CFR 1280.32 - What other behavior is not permitted?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false What other behavior is not permitted? 1280.32 Section 1280.32 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS..., electronic mail, or phone) any NARA employee, visitor, volunteer, contractor, other building occupants, or...

  3. 36 CFR 1280.32 - What other behavior is not permitted?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false What other behavior is not permitted? 1280.32 Section 1280.32 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS..., electronic mail, or phone) any NARA employee, visitor, volunteer, contractor, other building occupants, or...

  4. 36 CFR 1280.32 - What other behavior is not permitted?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false What other behavior is not permitted? 1280.32 Section 1280.32 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS..., electronic mail, or phone) any NARA employee, visitor, volunteer, contractor, other building occupants, or...

  5. 36 CFR 1280.22 - Is gambling allowed on NARA property?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false Is gambling allowed on NARA...? Prohibited Activities § 1280.22 Is gambling allowed on NARA property? (a) No, you may not participate in any type of gambling while on NARA property. This includes: (1) Participating in games for money or other...

  6. 36 CFR 1280.22 - Is gambling allowed on NARA property?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ...? Prohibited Activities § 1280.22 Is gambling allowed on NARA property? (a) No, you may not participate in any type of gambling while on NARA property. This includes: (1) Participating in games for money or other... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false Is gambling allowed on NARA...

  7. 36 CFR 1280.22 - Is gambling allowed on NARA property?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false Is gambling allowed on NARA...? Prohibited Activities § 1280.22 Is gambling allowed on NARA property? (a) No, you may not participate in any type of gambling while on NARA property. This includes: (1) Participating in games for money or other...

  8. 36 CFR 1280.22 - Is gambling allowed on NARA property?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false Is gambling allowed on NARA...? Prohibited Activities § 1280.22 Is gambling allowed on NARA property? (a) No, you may not participate in any type of gambling while on NARA property. This includes: (1) Participating in games for money or other...

  9. 7 CFR 1280.224 - Periodic evaluation.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.224...

  10. 7 CFR 1280.116 - Producer.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.116 Producer. Producer means any person who owns and produces lambs in the United States for sale. ...

  11. 36 CFR 1280.92 - When are the Presidential library museums open to the public?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... library museums open to the public? 1280.92 Section 1280.92 Parks, Forests, and Public Property NATIONAL... Use of Facilities in Presidential Libraries? § 1280.92 When are the Presidential library museums open to the public? (a) The hours of operation at Presidential Library museums vary. Please contact the...

  12. 36 CFR 1280.92 - When are the Presidential library museums open to the public?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... library museums open to the public? 1280.92 Section 1280.92 Parks, Forests, and Public Property NATIONAL... Use of Facilities in Presidential Libraries? § 1280.92 When are the Presidential library museums open to the public? (a) The Presidential library museums are open every day except Thanksgiving, December...

  13. 36 CFR 1280.92 - When are the Presidential library museums open to the public?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... library museums open to the public? 1280.92 Section 1280.92 Parks, Forests, and Public Property NATIONAL... Use of Facilities in Presidential Libraries? § 1280.92 When are the Presidential library museums open to the public? (a) The Presidential library museums are open every day except Thanksgiving, December...

  14. 36 CFR 1280.92 - When are the Presidential library museums open to the public?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... library museums open to the public? 1280.92 Section 1280.92 Parks, Forests, and Public Property NATIONAL... Use of Facilities in Presidential Libraries? § 1280.92 When are the Presidential library museums open to the public? (a) The Presidential library museums are open every day except Thanksgiving, December...

  15. EASY-HIT: HIV full-replication technology for broad discovery of multiple classes of HIV inhibitors.

    PubMed

    Kremb, Stephan; Helfer, Markus; Heller, Werner; Hoffmann, Dieter; Wolff, Horst; Kleinschmidt, Andrea; Cepok, Sabine; Hemmer, Bernhard; Durner, Jörg; Brack-Werner, Ruth

    2010-12-01

    HIV replication assays are important tools for HIV drug discovery efforts. Here, we present a full HIV replication system (EASY-HIT) for the identification and analysis of HIV inhibitors. This technology is based on adherently growing HIV-susceptible cells, with a stable fluorescent reporter gene activated by HIV Tat and Rev. A fluorescence-based assay was designed that measures HIV infection by two parameters relating to the early and the late phases of HIV replication, respectively. Validation of the assay with a panel of nine reference inhibitors yielded effective inhibitory concentrations consistent with published data and allowed discrimination between inhibitors of early and late phases of HIV replication. Finer resolution of the effects of reference drugs on different steps of HIV replication was achieved in secondary time-of-addition assays. The EASY-HIT assay yielded high Z' scores (>0.9) and signal stabilities, confirming its robustness. Screening of the LOPAC(1280) library identified 10 compounds (0.8%), of which eight were known to inhibit HIV, validating the suitability of this assay for screening applications. Studies evaluating anti-HIV activities of natural products with the EASY-HIT technology led to the identification of three novel inhibitory compounds that apparently act at different steps of HIV-1 replication. Furthermore, we demonstrate successful evaluation of plant extracts for HIV-inhibitory activities, suggesting application of this technology for the surveillance of biological extracts with anti-HIV activities. We conclude that the EASY-HIT technology is a versatile tool for the discovery and characterization of HIV inhibitors.

  16. 7 CFR 1280.118 - Promotion.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.118 Promotion. Promotion... information and public relations with emphasis on new marketing strategies, to present a favorable image of U...

  17. 7 CFR 1280.233 - Referenda.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Miscellaneous § 1280.233 Referenda. (a... determined by the Secretary, have engaged in the production, feeding, handling, or slaughter of lamb; or the...

  18. 7 CFR 1280.107 - Feeder.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.107 Feeder. Feeder means any person who acquires ownership of lambs and feeds such lambs in the U.S. until they reach slaughter...

  19. 7 CFR 1280.129 - Wool products.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.129 Wool products. Wool..., excluding pelts. Lamb Promotion, Research, and Information Board ...

  20. 7 CFR 1280.220 - Collections.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Assessments § 1280.220 Collections. (a) Each... remit assessments to the Board by the 15th day of the month following the month in which the lambs were...

  1. 7 CFR 1280.218 - Exporter.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Assessments § 1280.218 Exporter. Each person exporting live lambs shall remit to the Board an assessment on such lambs at the time of export at the rate...

  2. 26 CFR 1.280H-0T - Table of contents (temporary).

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 1.280H-0T Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF THE TREASURY (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES Items Not Deductible § 1.280H-0T Table of contents (temporary). This...) Example. (3) 3-year average test. (i) In general. (ii) Applicable percentage. (iii) Adjusted taxable...

  3. 26 CFR 1.280H-0T - Table of contents (temporary).

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 1.280H-0T Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF THE TREASURY (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280H-0T Table of contents (temporary...) In general. (ii) Example. (3) 3-year average test. (i) In general. (ii) Applicable percentage. (iii...

  4. 7 CFR 1280.237 - Rules and Regulations.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Miscellaneous § 1280.237 Rules and...

  5. 7 CFR 1280.234 - Suspension or termination.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Miscellaneous § 1280.234 Suspension or...

  6. 36 CFR § 1280.22 - Is gambling allowed on NARA property?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true Is gambling allowed on NARA...? Prohibited Activities § 1280.22 Is gambling allowed on NARA property? (a) No, you may not participate in any type of gambling while on NARA property. This includes: (1) Participating in games for money or other...

  7. 36 CFR § 1280.32 - What other behavior is not permitted?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true What other behavior is not permitted? § 1280.32 Section § 1280.32 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS..., electronic mail, or phone) any NARA employee, visitor, volunteer, contractor, other building occupants, or...

  8. 7 CFR 1280.214 - Refund escrow accounts.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Expenses § 1280.214 Refund escrow accounts...

  9. 7 CFR 1280.104 - Conflict of Interest.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.104 Conflict of Interest...

  10. 36 CFR 1280.90 - What are the rules of conduct while visiting the Presidential libraries?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... while visiting the Presidential libraries? 1280.90 Section 1280.90 Parks, Forests, and Public Property... Apply for Use of Facilities in Presidential Libraries? § 1280.90 What are the rules of conduct while visiting the Presidential libraries? In addition to the rules in Subpart A, when visiting the museums of...

  11. 36 CFR 1280.90 - What are the rules of conduct while visiting the Presidential libraries?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... while visiting the Presidential libraries? 1280.90 Section 1280.90 Parks, Forests, and Public Property... Apply for Use of Facilities in Presidential Libraries? § 1280.90 What are the rules of conduct while visiting the Presidential libraries? In addition to the rules in Subpart A, when visiting the museums of...

  12. 36 CFR 1280.90 - What are the rules of conduct while visiting the Presidential libraries?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... while visiting the Presidential libraries? 1280.90 Section 1280.90 Parks, Forests, and Public Property... Apply for Use of Facilities in Presidential Libraries? § 1280.90 What are the rules of conduct while visiting the Presidential libraries? In addition to the rules in Subpart A, when visiting the museums of...

  13. 36 CFR 1280.90 - What are the rules of conduct while visiting the Presidential libraries?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... while visiting the Presidential libraries? 1280.90 Section 1280.90 Parks, Forests, and Public Property... Apply for Use of Facilities in Presidential Libraries? § 1280.90 What are the rules of conduct while visiting the Presidential libraries? In addition to the rules in Subpart A, when visiting the museums of...

  14. 7 CFR 1280.226 - Use of information.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Reports, Books, and Records § 1280.226 Use...

  15. 36 CFR § 1280.92 - When are the Presidential library museums open to the public?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... library museums open to the public? § 1280.92 Section § 1280.92 Parks, Forests, and Public Property... Apply for Use of Facilities in Presidential Libraries? § 1280.92 When are the Presidential library museums open to the public? (a) The Presidential library museums are open every day except Thanksgiving...

  16. 7 CFR 1280.117 - Producer information.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.117 Producer information..., or other information that would facilitate an increase in the demand for lambs or lamb products. ...

  17. Identification of new drug candidates against Borrelia burgdorferi using high-throughput screening.

    PubMed

    Pothineni, Venkata Raveendra; Wagh, Dhananjay; Babar, Mustafeez Mujtaba; Inayathullah, Mohammed; Solow-Cordero, David; Kim, Kwang-Min; Samineni, Aneesh V; Parekh, Mansi B; Tayebi, Lobat; Rajadas, Jayakumar

    2016-01-01

    Lyme disease is the most common zoonotic bacterial disease in North America. It is estimated that >300,000 cases per annum are reported in USA alone. A total of 10%-20% of patients who have been treated with antibiotic therapy report the recrudescence of symptoms, such as muscle and joint pain, psychosocial and cognitive difficulties, and generalized fatigue. This condition is referred to as posttreatment Lyme disease syndrome. While there is no evidence for the presence of viable infectious organisms in individuals with posttreatment Lyme disease syndrome, some researchers found surviving Borrelia burgdorferi population in rodents and primates even after antibiotic treatment. Although such observations need more ratification, there is unmet need for developing the therapeutic agents that focus on removing the persisting bacterial form of B. burgdorferi in rodent and nonhuman primates. For this purpose, high-throughput screening was done using BacTiter-Glo assay for four compound libraries to identify candidates that stop the growth of B. burgdorferi in vitro. The four chemical libraries containing 4,366 compounds (80% Food and Drug Administration [FDA] approved) that were screened are Library of Pharmacologically Active Compounds (LOPAC1280), the National Institutes of Health Clinical Collection, the Microsource Spectrum, and the Biomol FDA. We subsequently identified 150 unique compounds, which inhibited >90% of B. burgdorferi growth at a concentration of <25 µM. These 150 unique compounds comprise many safe antibiotics, chemical compounds, and also small molecules from plant sources. Of the 150 unique compounds, 101 compounds are FDA approved. We selected the top 20 FDA-approved molecules based on safety and potency and studied their minimum inhibitory concentration and minimum bactericidal concentration. The promising safe FDA-approved candidates that show low minimum inhibitory concentration and minimum bactericidal concentration values can be chosen as lead

  18. 26 CFR 1.280F-7 - Property leased after December 31, 1986.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...-7 Section 1.280F-7 Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF THE TREASURY (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280F-7 Property leased after...-5T(e) for rules on determining inclusion amounts for passenger automobiles for which the taxpayer's...

  19. 26 CFR 1.280F-7 - Property leased after December 31, 1986.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ...-7 Section 1.280F-7 Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF THE TREASURY (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280F-7 Property leased after...-5T(e) for rules on determining inclusion amounts for passenger automobiles for which the taxpayer's...

  20. 26 CFR 1.280F-7 - Property leased after December 31, 1986.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ...-7 Section 1.280F-7 Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF THE TREASURY (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280F-7 Property leased after...-5T(e) for rules on determining inclusion amounts for passenger automobiles for which the taxpayer's...

  1. 26 CFR 1.280F-7 - Property leased after December 31, 1986.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ...-7 Section 1.280F-7 Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF THE TREASURY (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280F-7 Property leased after...-5T(e) for rules on determining inclusion amounts for passenger automobiles for which the taxpayer's...

  2. Development of a quantitative assay amenable for high-throughput screening to target the type II secretion system for new treatments against plant-pathogenic bacteria.

    PubMed

    Tran, Nini; Zielke, Ryszard A; Vining, Oliver B; Azevedo, Mark D; Armstrong, Donald J; Banowetz, Gary M; McPhail, Kerry L; Sikora, Aleksandra E

    2013-09-01

    Plant-pathogenic bacteria are the causative agents of diseases in important agricultural crops and ornamental plants. The severe economic burden of these diseases requires seeking new approaches for their control, particularly because phytopathogenic bacteria are often resistant to available treatments. The type II secretion (T2S) system is a key virulence factor used by major groups of phytopathogenic bacteria. The T2S machinery transports many hydrolytic enzymes responsible for degradation of the plant cell wall, thus enabling successful colonization and dissemination of the bacteria in the plant host. The genetic inactivation of the T2S system leads to loss of virulence, which strongly suggests that targeting the T2S could enable new treatments against plant-pathogenic bacteria. Accordingly, we have designed and optimized an assay to identify small-molecule inhibitors of the T2S system. This assay uses a double parametric output: measurement of bacterial growth and the enzymatic activity of cellulase, which is secreted via the T2S pathway in our model organism Dickeya dadantii. The assay was evaluated by screening natural extracts, culture filtrates isolated from rhizosphere bacteria, and a collection of pharmaceutically active compounds in LOPAC(1280). The calculated Z' values of 0.63, 0.63, and 0.58, respectively, strongly suggest that the assay is applicable for a high-throughput screening platform.

  3. 43 CFR 4.1280 - Scope.

    Code of Federal Regulations, 2010 CFR

    2010-10-01

    ... Applicable to Surface Coal Mining Hearings and Appeals Appeals to the Board from Decisions of the Office of Surface Mining § 4.1280 Scope. This section is applicable to appeals from decisions of the Director of OSM concerning small operator exemptions under 30 CFR 710.12(h) and to other appeals which are not required by...

  4. 36 CFR 1280.42 - When do the rules in this subpart apply?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false When do the rules in this subpart apply? 1280.42 Section 1280.42 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What Are the Rules for Filming, Photographing, or...

  5. 36 CFR 1280.42 - When do the rules in this subpart apply?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false When do the rules in this subpart apply? 1280.42 Section 1280.42 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What Are the Rules for Filming, Photographing, or...

  6. 36 CFR 1280.42 - When do the rules in this subpart apply?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false When do the rules in this subpart apply? 1280.42 Section 1280.42 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What Are the Rules for Filming, Photographing, or...

  7. 36 CFR 1280.42 - When do the rules in this subpart apply?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false When do the rules in this subpart apply? 1280.42 Section 1280.42 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What Are the Rules for Filming, Photographing, or...

  8. 7 CFR 1280.108 - First handler.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.108 First handler. First handler means the packer or other person who buys or takes possession of lambs from a producer or feeder...

  9. 7 CFR 1280.122 - Seedstock producer.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.122 Seedstock producer. Seedstock producer means any lamb producer in the U.S. who engages in the production and sale of breeding...

  10. 7 CFR 1280.219 - First handlers.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Assessments § 1280.219 First handlers. Each... assessment equal to thirty cents ($.30) per head of lambs purchased by the first handler for slaughter or...

  11. 36 CFR § 1280.90 - What are the rules of conduct while visiting the Presidential libraries?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... while visiting the Presidential libraries? § 1280.90 Section § 1280.90 Parks, Forests, and Public... Additional Rules Apply for Use of Facilities in Presidential Libraries? § 1280.90 What are the rules of conduct while visiting the Presidential libraries? In addition to the rules in Subpart A, when visiting...

  12. 36 CFR 1280.44 - May I film, photograph, or videotape on NARA property for commercial purposes?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false May I film, photograph, or videotape on NARA property for commercial purposes? 1280.44 Section 1280.44 Parks, Forests, and Public... Rules for Filming, Photographing, or Videotaping on NARA Property? § 1280.44 May I film, photograph, or...

  13. 36 CFR 1280.44 - May I film, photograph, or videotape on NARA property for commercial purposes?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false May I film, photograph, or videotape on NARA property for commercial purposes? 1280.44 Section 1280.44 Parks, Forests, and Public... Rules for Filming, Photographing, or Videotaping on NARA Property? § 1280.44 May I film, photograph, or...

  14. 36 CFR 1280.44 - May I film, photograph, or videotape on NARA property for commercial purposes?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false May I film, photograph, or videotape on NARA property for commercial purposes? 1280.44 Section 1280.44 Parks, Forests, and Public... Rules for Filming, Photographing, or Videotaping on NARA Property? § 1280.44 May I film, photograph, or...

  15. 36 CFR 1280.44 - May I film, photograph, or videotape on NARA property for commercial purposes?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false May I film, photograph, or videotape on NARA property for commercial purposes? 1280.44 Section 1280.44 Parks, Forests, and Public... Rules for Filming, Photographing, or Videotaping on NARA Property? § 1280.44 May I film, photograph, or...

  16. 36 CFR 1280.26 - May I pass out fliers on NARA property?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false May I pass out fliers on NARA property? 1280.26 Section 1280.26 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS... those spaces designated by NARA as public forums. This prohibition does not apply to displays or notices...

  17. 36 CFR 1280.26 - May I pass out fliers on NARA property?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false May I pass out fliers on NARA property? 1280.26 Section 1280.26 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS... those spaces designated by NARA as public forums. This prohibition does not apply to displays or notices...

  18. Identification of signalling cascades involved in red blood cell shrinkage and vesiculation.

    PubMed

    Kostova, Elena B; Beuger, Boukje M; Klei, Thomas R L; Halonen, Pasi; Lieftink, Cor; Beijersbergen, Roderick; van den Berg, Timo K; van Bruggen, Robin

    2015-04-16

    Even though red blood cell (RBC) vesiculation is a well-documented phenomenon, notably in the context of RBC aging and blood transfusion, the exact signalling pathways and kinases involved in this process remain largely unknown. We have established a screening method for RBC vesicle shedding using the Ca(2+) ionophore ionomycin which is a rapid and efficient method to promote vesiculation. In order to identify novel pathways stimulating vesiculation in RBC, we screened two libraries: the Library of Pharmacologically Active Compounds (LOPAC) and the Selleckchem Kinase Inhibitor Library for their effects on RBC from healthy donors. We investigated compounds triggering vesiculation and compounds inhibiting vesiculation induced by ionomycin. We identified 12 LOPAC compounds, nine kinase inhibitors and one kinase activator which induced RBC shrinkage and vesiculation. Thus, we discovered several novel pathways involved in vesiculation including G protein-coupled receptor (GPCR) signalling, the phosphoinositide 3-kinase (PI3K)-Akt (protein kinase B) pathway, the Jak-STAT (Janus kinase-signal transducer and activator of transcription) pathway and the Raf-MEK (mitogen-activated protein kinase kinase)-ERK (extracellular signal-regulated kinase) pathway. Moreover, we demonstrated a link between casein kinase 2 (CK2) and RBC shrinkage via regulation of the Gardos channel activity. In addition, our data showed that inhibition of several kinases with unknown functions in mature RBC, including Alk (anaplastic lymphoma kinase) kinase and vascular endothelial growth factor receptor 2 (VEGFR-2), induced RBC shrinkage and vesiculation.

  19. Identification of signalling cascades involved in red blood cell shrinkage and vesiculation

    PubMed Central

    Kostova, Elena B.; Beuger, Boukje M.; Klei, Thomas R.L.; Halonen, Pasi; Lieftink, Cor; Beijersbergen, Roderick; van den Berg, Timo K.; van Bruggen, Robin

    2015-01-01

    Even though red blood cell (RBC) vesiculation is a well-documented phenomenon, notably in the context of RBC aging and blood transfusion, the exact signalling pathways and kinases involved in this process remain largely unknown. We have established a screening method for RBC vesicle shedding using the Ca2+ ionophore ionomycin which is a rapid and efficient method to promote vesiculation. In order to identify novel pathways stimulating vesiculation in RBC, we screened two libraries: the Library of Pharmacologically Active Compounds (LOPAC) and the Selleckchem Kinase Inhibitor Library for their effects on RBC from healthy donors. We investigated compounds triggering vesiculation and compounds inhibiting vesiculation induced by ionomycin. We identified 12 LOPAC compounds, nine kinase inhibitors and one kinase activator which induced RBC shrinkage and vesiculation. Thus, we discovered several novel pathways involved in vesiculation including G protein-coupled receptor (GPCR) signalling, the phosphoinositide 3-kinase (PI3K)–Akt (protein kinase B) pathway, the Jak–STAT (Janus kinase–signal transducer and activator of transcription) pathway and the Raf–MEK (mitogen-activated protein kinase kinase)–ERK (extracellular signal-regulated kinase) pathway. Moreover, we demonstrated a link between casein kinase 2 (CK2) and RBC shrinkage via regulation of the Gardos channel activity. In addition, our data showed that inhibition of several kinases with unknown functions in mature RBC, including Alk (anaplastic lymphoma kinase) kinase and vascular endothelial growth factor receptor 2 (VEGFR-2), induced RBC shrinkage and vesiculation. PMID:25757360

  20. 7 CFR 1280.228 - Right of the Secretary.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Miscellaneous § 1280.228 Right of the...

  1. 36 CFR 1280.28 - Where can I eat and drink on NARA property?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false Where can I eat and drink on... NARA Property? Prohibited Activities § 1280.28 Where can I eat and drink on NARA property? You may only eat and drink in designated areas in NARA facilities. Eating and drinking is prohibited in the...

  2. 36 CFR 1280.10 - Are there special rules for driving on NARA property?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false Are there special rules for driving on NARA property? 1280.10 Section 1280.10 Parks, Forests, and Public Property NATIONAL ARCHIVES..., and park only in designated spaces. (b) NARA will tow, at the owner's expense, any vehicle that is...

  3. 36 CFR § 1280.42 - When do the rules in this subpart apply?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true When do the rules in this subpart apply? § 1280.42 Section § 1280.42 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What Are the Rules for Filming...

  4. 36 CFR 1280.72 - What additional rules apply for a NARA approved event?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... for a NARA approved event? 1280.72 Section 1280.72 Parks, Forests, and Public Property NATIONAL... approved event? (a) Approved applicants must provide support people as needed to register guests... for the use of food and drink at your event. (d) No food or drink may be present or consumed in areas...

  5. 36 CFR 1280.72 - What additional rules apply for a NARA approved event?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... for a NARA approved event? 1280.72 Section 1280.72 Parks, Forests, and Public Property NATIONAL... approved event? (a) Approved applicants must provide support people as needed to register guests... for the use of food and drink at your event. (d) No food or drink may be present or consumed in areas...

  6. 36 CFR 1280.72 - What additional rules apply for a NARA approved event?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... for a NARA approved event? 1280.72 Section 1280.72 Parks, Forests, and Public Property NATIONAL... approved event? (a) Approved applicants must provide support people as needed to register guests... for the use of food and drink at your event. (d) No food or drink may be present or consumed in areas...

  7. 36 CFR § 1280.44 - May I film, photograph, or videotape on NARA property for commercial purposes?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true May I film, photograph, or videotape on NARA property for commercial purposes? § 1280.44 Section § 1280.44 Parks, Forests, and Public... Rules for Filming, Photographing, or Videotaping on NARA Property? § 1280.44 May I film, photograph, or...

  8. 7 CFR 1280.114 - Part and subpart.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.114 Part and subpart. Part means the Lamb Promotion, Research, and Information Order and all rules and regulations issued...

  9. 26 CFR 1.280F-4T - Special rules for listed property (temporary).

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 26 Internal Revenue 3 2013-04-01 2013-04-01 false Special rules for listed property (temporary). 1... (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280F-4T Special rules...) and § 1.280F-6(d)(2)) in 1984 through 1988 is 80 percent, 70 percent, 60 percent, and 55 percent...

  10. 26 CFR 1.280F-4T - Special rules for listed property (temporary).

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 26 Internal Revenue 3 2014-04-01 2014-04-01 false Special rules for listed property (temporary). 1... (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280F-4T Special rules...) and § 1.280F-6(d)(2)) in 1984 through 1988 is 80 percent, 70 percent, 60 percent, and 55 percent...

  11. 26 CFR 1.280F-4T - Special rules for listed property (temporary).

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 26 Internal Revenue 3 2011-04-01 2011-04-01 false Special rules for listed property (temporary). 1... (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280F-4T Special rules...) and § 1.280F-6(d)(2)) in 1984 through 1988 is 80 percent, 70 percent, 60 percent, and 55 percent...

  12. 26 CFR 1.280F-4T - Special rules for listed property (temporary).

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 26 Internal Revenue 3 2012-04-01 2012-04-01 false Special rules for listed property (temporary). 1... (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES (CONTINUED) Items Not Deductible § 1.280F-4T Special rules...) and § 1.280F-6(d)(2)) in 1984 through 1988 is 80 percent, 70 percent, 60 percent, and 55 percent...

  13. 36 CFR 1280.94 - When do Presidential libraries allow other groups to use their public areas for events?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... libraries allow other groups to use their public areas for events? 1280.94 Section 1280.94 Parks, Forests... FACILITIES What Additional Rules Apply for Use of Facilities in Presidential Libraries? § 1280.94 When do Presidential libraries allow other groups to use their public areas for events? (a) Although Presidential...

  14. 36 CFR 1280.94 - When do Presidential libraries allow other groups to use their public areas for events?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... libraries allow other groups to use their public areas for events? 1280.94 Section 1280.94 Parks, Forests... FACILITIES What Additional Rules Apply for Use of Facilities in Presidential Libraries? § 1280.94 When do Presidential libraries allow other groups to use their public areas for events? (a) Although Presidential...

  15. 36 CFR 1280.94 - When do Presidential libraries allow other groups to use their public areas for events?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... libraries allow other groups to use their public areas for events? 1280.94 Section 1280.94 Parks, Forests... FACILITIES What Additional Rules Apply for Use of Facilities in Presidential Libraries? § 1280.94 When do Presidential libraries allow other groups to use their public areas for events? (a) Although Presidential...

  16. 36 CFR 1280.94 - When do Presidential libraries allow other groups to use their public areas for events?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... libraries allow other groups to use their public areas for events? 1280.94 Section 1280.94 Parks, Forests... FACILITIES What Additional Rules Apply for Use of Facilities in Presidential Libraries? § 1280.94 When do Presidential libraries allow other groups to use their public areas for events? (a) Although Presidential...

  17. 36 CFR § 1280.20 - What is your policy on illegal drugs and alcohol?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... Conduct on NARA Property? Prohibited Activities § 1280.20 What is your policy on illegal drugs and alcohol? You may not use or be in possession of illegal drugs on NARA property. You also may not enter NARA property while under the influence of illegal drugs or alcohol. Using alcoholic beverages on NARA property...

  18. Identification of compounds that modulate retinol signaling using a cell-based qHTS assay

    PubMed Central

    Chen, Yanling; Sakamuru, Srilatha; Huang, Ruili; Reese, David H.; Xia, Menghang

    2016-01-01

    In vertebrates, the retinol (vitamin A) signaling pathway (RSP) controls the biosynthesis and catabolism of all-trans retinoic acid (atRA), which regulates transcription of genes essential for embryonic development. Chemicals that interfere with the RSP to cause abnormal intracellular levels of atRA are potential developmental toxicants. To assess chemicals for the ability to interfere with retinol signaling, we have developed a cell-based RARE (Retinoic Acid Response Element) reporter gene assay to identify RSP disruptors. To validate this assay in a quantitative high-throughput screening (qHTS) platform, we screened the Library of Pharmacologically Active Compounds (LOPAC) in both agonist and antagonist modes. The screens detected known RSP agonists, demonstrating assay reliability, and also identified novel RSP agonists including kenpaullone, niclosamide, PD98059 and SU4312, and RSP antagonists including Bay 11-7085, LY294002, 3,4-Methylenedioxy-β-nitrostyrene, and topoisomerase inhibitors (camptothecin, topotecan, amsacrine hydrochloride, and idarubicin). When evaluated in the P19 pluripotent cell, these compounds were found to affect the expression of the Hoxa1 gene that is essential for embryo body patterning. These results show that the RARE assay is an effective qHTS approach for screening large compound libraries to identify chemicals that have the potential to adversely affect embryonic development through interference with retinol signaling. PMID:26820057

  19. 7 CFR 1280.627 - Canvassing voting ballots.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... Executive Director (CED) and a county or State FSA office employee to canvass the ballots and report the... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.627 Canvassing voting ballots. (a... impractical, and designate the CED and/or another county or State FSA office employee to canvass requests in...

  20. 7 CFR 1280.627 - Canvassing voting ballots.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... Executive Director (CED) and a county or State FSA office employee to canvass the ballots and report the... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.627 Canvassing voting ballots. (a... impractical, and designate the CED and/or another county or State FSA office employee to canvass requests in...

  1. 7 CFR 1280.627 - Canvassing voting ballots.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... Executive Director (CED) and a county or State FSA office employee to canvass the ballots and report the... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.627 Canvassing voting ballots. (a... impractical, and designate the CED and/or another county or State FSA office employee to canvass requests in...

  2. 7 CFR 1280.627 - Canvassing voting ballots.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... Executive Director (CED) and a county or State FSA office employee to canvass the ballots and report the... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.627 Canvassing voting ballots. (a... impractical, and designate the CED and/or another county or State FSA office employee to canvass requests in...

  3. 7 CFR 1280.627 - Canvassing voting ballots.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... Executive Director (CED) and a county or State FSA office employee to canvass the ballots and report the... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.627 Canvassing voting ballots. (a... impractical, and designate the CED and/or another county or State FSA office employee to canvass requests in...

  4. 36 CFR § 1280.72 - What additional rules apply for a NARA approved event?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true What additional rules apply for a NARA approved event? § 1280.72 Section § 1280.72 Parks, Forests, and Public Property NATIONAL..., distribute approved literature, name tags, and other material. (b) We must approve in advance any item that...

  5. Development of an image analysis screen for estrogen receptor alpha (ERα) ligands through measurement of nuclear translocation dynamics.

    PubMed

    Dull, Angie; Goncharova, Ekaterina; Hager, Gordon; McMahon, James B

    2010-11-01

    We have developed a robust high-content assay to screen for novel estrogen receptor alpha (ERα) agonists and antagonists by quantitation of cytoplasmic to nuclear translocation of an estrogen receptor chimera in 384-well plates. The screen utilizes a green fluorescent protein tagged-glucocorticoid/estrogen receptor (GFP-GRER) chimera which consisted of the N-terminus of the glucocorticoid receptor fused to the human ER ligand binding domain. The GFP-GRER exhibited cytoplasmic localization in the absence of ERα ligands, and translocated to the nucleus in response to stimulation with ERα agonists or antagonists. The BD Pathway 435 imaging system was used for image acquisition, analysis of translocation dynamics, and cytotoxicity measurements. The assay was validated with known ERα agonists and antagonists, and the Library of Pharmacologically Active Compounds (LOPAC 1280). Additionally, screening of crude natural product extracts demonstrated the robustness of the assay, and the ability to quantitate the effects of toxicity on nuclear translocation dynamics. The GFP-GRER nuclear translocation assay was very robust, with z' values >0.7, CVs <5%, and has been validated with known ER ligands, and inclusion of cytotoxicity filters will facilitate screening of natural product extracts. This assay has been developed for future primary screening of synthetic, pure natural products, and natural product extracts libraries available at the National Cancer Institute at Frederick. Copyright © 2010 Elsevier Ltd. All rights reserved.

  6. 7 CFR 1280.626 - Certification and voting procedures.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 1280.626 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB... Internet during the voting period. A completed and signed form LS-86 and supporting documentation, such as...

  7. 26 CFR 1.280C-3 - Disallowance of certain deductions for qualified clinical testing expenses when section 28 credit...

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... clinical testing expenses when section 28 credit is allowable. 1.280C-3 Section 1.280C-3 Internal Revenue... Not Deductible § 1.280C-3 Disallowance of certain deductions for qualified clinical testing expenses... section 28 for qualified clinical testing expenses (as defined in section 28(b)), it must reduce the...

  8. 33 CFR 334.1280 - Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... weapon range, Alaskan Air Command, U.S. Air Force. 334.1280 Section 334.1280 Navigation and Navigable... REGULATIONS § 334.1280 Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force. (a... enforced by the Commander, Alaskan Air Command, U.S. Air Force, Seattle, Washington, or such agencies as he...

  9. 33 CFR 334.1280 - Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... weapon range, Alaskan Air Command, U.S. Air Force. 334.1280 Section 334.1280 Navigation and Navigable... REGULATIONS § 334.1280 Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force. (a... enforced by the Commander, Alaskan Air Command, U.S. Air Force, Seattle, Washington, or such agencies as he...

  10. 33 CFR 334.1280 - Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... weapon range, Alaskan Air Command, U.S. Air Force. 334.1280 Section 334.1280 Navigation and Navigable... REGULATIONS § 334.1280 Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force. (a... enforced by the Commander, Alaskan Air Command, U.S. Air Force, Seattle, Washington, or such agencies as he...

  11. 33 CFR 334.1280 - Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... weapon range, Alaskan Air Command, U.S. Air Force. 334.1280 Section 334.1280 Navigation and Navigable... REGULATIONS § 334.1280 Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force. (a... enforced by the Commander, Alaskan Air Command, U.S. Air Force, Seattle, Washington, or such agencies as he...

  12. 33 CFR 334.1280 - Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... weapon range, Alaskan Air Command, U.S. Air Force. 334.1280 Section 334.1280 Navigation and Navigable... REGULATIONS § 334.1280 Bristol Bay, Alaska; air-to-air weapon range, Alaskan Air Command, U.S. Air Force. (a... enforced by the Commander, Alaskan Air Command, U.S. Air Force, Seattle, Washington, or such agencies as he...

  13. State-dependent compound inhibition of Nav1.2 sodium channels using the FLIPR Vm dye: on-target and off-target effects of diverse pharmacological agents.

    PubMed

    Benjamin, Elfrida R; Pruthi, Farhana; Olanrewaju, Shakira; Ilyin, Victor I; Crumley, Gregg; Kutlina, Elena; Valenzano, Kenneth J; Woodward, Richard M

    2006-02-01

    Voltage-gated sodium channels (NaChs) are relevant targets for pain, epilepsy, and a variety of neurological and cardiac disorders. Traditionally, it has been difficult to develop structure-activity relationships for NaCh inhibitors due to rapid channel kinetics and state-dependent compound interactions. Membrane potential (Vm) dyes in conjunction with a high-throughput fluorescence imaging plate reader (FLIPR) offer a satisfactory 1st-tier solution. Thus, the authors have developed a FLIPR Vm assay of rat Nav1.2 NaCh. Channels were opened by addition of veratridine, and Vm dye responses were measured. The IC50 values from various structural classes of compounds were compared to the resting state binding constant (Kr)and inactivated state binding constant (Ki)obtained using patch-clamp electrophysiology (EP). The FLIPR values correlated with Ki but not Kr. FLIPRIC50 values fell within 0.1-to 1.5-fold of EP Ki values, indicating that the assay generally reports use-dependent inhibition rather than resting state block. The Library of Pharmacologically Active Compounds (LOPAC, Sigma) was screened. Confirmed hits arose from diverse classes such as dopamine receptor antagonists, serotonin transport inhibitors, and kinase inhibitors. These data suggest that NaCh inhibition is inherent in a diverse set of biologically active molecules and may warrant counterscreening NaChs to avoid unwanted secondary pharmacology.

  14. 7 CFR 1280.632 - Disposition of records.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... records will be placed in a secure location under the custody of FSA CED for a period of not less than 12... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.632 Disposition of records. Each FSA CED will place in sealed containers marked with the identification of the “Lamb Checkoff Program...

  15. 7 CFR 1280.632 - Disposition of records.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... records will be placed in a secure location under the custody of FSA CED for a period of not less than 12... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.632 Disposition of records. Each FSA CED will place in sealed containers marked with the identification of the “Lamb Checkoff Program...

  16. 7 CFR 1280.632 - Disposition of records.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... records will be placed in a secure location under the custody of FSA CED for a period of not less than 12... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.632 Disposition of records. Each FSA CED will place in sealed containers marked with the identification of the “Lamb Checkoff Program...

  17. 7 CFR 1280.632 - Disposition of records.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... records will be placed in a secure location under the custody of FSA CED for a period of not less than 12... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.632 Disposition of records. Each FSA CED will place in sealed containers marked with the identification of the “Lamb Checkoff Program...

  18. 7 CFR 1280.632 - Disposition of records.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... records will be placed in a secure location under the custody of FSA CED for a period of not less than 12... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.632 Disposition of records. Each FSA CED will place in sealed containers marked with the identification of the “Lamb Checkoff Program...

  19. 36 CFR 1280.8 - May I bring a seeing-eye dog or other assistance animal?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false May I bring a seeing-eye dog or other assistance animal? 1280.8 Section 1280.8 Parks, Forests, and Public Property NATIONAL... dog or other assistance animal? Yes, persons with disabilities may bring guide dogs or other animals...

  20. 36 CFR 1280.8 - May I bring a seeing-eye dog or other assistance animal?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false May I bring a seeing-eye dog or other assistance animal? 1280.8 Section 1280.8 Parks, Forests, and Public Property NATIONAL... dog or other assistance animal? Yes, persons with disabilities may bring guide dogs or other animals...

  1. 36 CFR 1280.8 - May I bring a seeing-eye dog or other assistance animal?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false May I bring a seeing-eye dog or other assistance animal? 1280.8 Section 1280.8 Parks, Forests, and Public Property NATIONAL... dog or other assistance animal? Yes, persons with disabilities may bring guide dogs or other animals...

  2. 36 CFR 1280.8 - May I bring a seeing-eye dog or other assistance animal?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false May I bring a seeing-eye dog or other assistance animal? 1280.8 Section 1280.8 Parks, Forests, and Public Property NATIONAL... dog or other assistance animal? Yes, persons with disabilities may bring guide dogs or other animals...

  3. 26 CFR 1.28-0 - Credit for clinical testing expenses for certain drugs for rare diseases or conditions; table of...

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... drugs for rare diseases or conditions; table of contents. 1.28-0 Section 1.28-0 Internal Revenue... Taxable Year § 1.28-0 Credit for clinical testing expenses for certain drugs for rare diseases or... 505(i). (d) Definition and special rules. (1) Definition of “rare disease or condition”. (i) In...

  4. 26 CFR 1.28-0 - Credit for clinical testing expenses for certain drugs for rare diseases or conditions; table of...

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... drugs for rare diseases or conditions; table of contents. 1.28-0 Section 1.28-0 Internal Revenue... Taxable Year § 1.28-0 Credit for clinical testing expenses for certain drugs for rare diseases or... 505(i). (d) Definition and special rules. (1) Definition of “rare disease or condition”. (i) In...

  5. 26 CFR 1.28-0 - Credit for clinical testing expenses for certain drugs for rare diseases or conditions; table of...

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... drugs for rare diseases or conditions; table of contents. 1.28-0 Section 1.28-0 Internal Revenue... Taxable Year § 1.28-0 Credit for clinical testing expenses for certain drugs for rare diseases or... 505(i). (d) Definition and special rules. (1) Definition of “rare disease or condition”. (i) In...

  6. 26 CFR 1.28-0 - Credit for clinical testing expenses for certain drugs for rare diseases or conditions; table of...

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... drugs for rare diseases or conditions; table of contents. 1.28-0 Section 1.28-0 Internal Revenue... Taxable Year § 1.28-0 Credit for clinical testing expenses for certain drugs for rare diseases or... 505(i). (d) Definition and special rules. (1) Definition of “rare disease or condition”. (i) In...

  7. 26 CFR 1.28-0 - Credit for clinical testing expenses for certain drugs for rare diseases or conditions; table of...

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... drugs for rare diseases or conditions; table of contents. 1.28-0 Section 1.28-0 Internal Revenue... Taxable Year § 1.28-0 Credit for clinical testing expenses for certain drugs for rare diseases or... 505(i). (d) Definition and special rules. (1) Definition of “rare disease or condition”. (i) In...

  8. 26 CFR 1.280C-1 - Disallowance of certain deductions for wage or salary expenses.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... salary expenses. 1.280C-1 Section 1.280C-1 Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF THE... certain deductions for wage or salary expenses. If an employer elects to claim the targeted jobs credit... deduction for wage or salary expenses paid or incurred in the year the credit is earned by the amount...

  9. 36 CFR 1280.88 - How do I request to use NARA public areas in the National Archives at College Park?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false How do I request to use NARA public areas in the National Archives at College Park? 1280.88 Section 1280.88 Parks, Forests, and Public... Apply to Use NARA Public Areas in the Washington, DC, Area? National Archives at College Park, Md § 1280...

  10. 36 CFR 1280.88 - How do I request to use NARA public areas in the National Archives at College Park?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false How do I request to use NARA public areas in the National Archives at College Park? 1280.88 Section 1280.88 Parks, Forests, and Public... Apply to Use NARA Public Areas in the Washington, DC, Area? National Archives at College Park, Md § 1280...

  11. 36 CFR 1280.34 - What are the types of corrective action NARA imposes for prohibited behavior?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false What are the types of corrective action NARA imposes for prohibited behavior? 1280.34 Section 1280.34 Parks, Forests, and Public... corrective action NARA imposes for prohibited behavior? (a) Individuals who violate the provisions of this...

  12. 36 CFR 1280.34 - What are the types of corrective action NARA imposes for prohibited behavior?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false What are the types of corrective action NARA imposes for prohibited behavior? 1280.34 Section 1280.34 Parks, Forests, and Public... corrective action NARA imposes for prohibited behavior? (a) Individuals who violate the provisions of this...

  13. 36 CFR 1280.34 - What are the types of corrective action NARA imposes for prohibited behavior?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false What are the types of corrective action NARA imposes for prohibited behavior? 1280.34 Section 1280.34 Parks, Forests, and Public... corrective action NARA imposes for prohibited behavior? (a) Individuals who violate the provisions of this...

  14. 36 CFR 1280.34 - What are the types of corrective action NARA imposes for prohibited behavior?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false What are the types of corrective action NARA imposes for prohibited behavior? 1280.34 Section 1280.34 Parks, Forests, and Public... corrective action NARA imposes for prohibited behavior? (a) Individuals who violate the provisions of this...

  15. 7 CFR 1280.216 - Procedure for obtaining a refund.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... SERVICE (MARKETING AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Expenses § 1280... collected applicant's assessment; (3) Number of head of lambs, weight of lambs, or its equivalent, on which...

  16. Development of Multiwell-Plate Methods Using Pure Cultures of Methanogens To Identify New Inhibitors for Suppressing Ruminant Methane Emissions.

    PubMed

    Weimar, M R; Cheung, J; Dey, D; McSweeney, C; Morrison, M; Kobayashi, Y; Whitman, W B; Carbone, V; Schofield, L R; Ronimus, R S; Cook, G M

    2017-08-01

    Hydrogenotrophic methanogens typically require strictly anaerobic culturing conditions in glass tubes with overpressures of H 2 and CO 2 that are both time-consuming and costly. To increase the throughput for screening chemical compound libraries, 96-well microtiter plate methods for the growth of a marine (environmental) methanogen Methanococcus maripaludis strain S2 and the rumen methanogen Methanobrevibacter species AbM4 were developed. A number of key parameters (inoculum size, reducing agents for medium preparation, assay duration, inhibitor solvents, and culture volume) were optimized to achieve robust and reproducible growth in a high-throughput microtiter plate format. The method was validated using published methanogen inhibitors and statistically assessed for sensitivity and reproducibility. The Sigma-Aldrich LOPAC library containing 1,280 pharmacologically active compounds and an in-house natural product library (120 compounds) were screened against M. maripaludis as a proof of utility. This screen identified a number of bioactive compounds, and MIC values were confirmed for some of them against M. maripaludis and M. AbM4. The developed method provides a significant increase in throughput for screening compound libraries and can now be used to screen larger compound libraries to discover novel methanogen-specific inhibitors for the mitigation of ruminant methane emissions. IMPORTANCE Methane emissions from ruminants are a significant contributor to global greenhouse gas emissions, and new technologies are required to control emissions in the agriculture technology (agritech) sector. The discovery of small-molecule inhibitors of methanogens using high-throughput phenotypic (growth) screening against compound libraries (synthetic and natural products) is an attractive avenue. However, phenotypic inhibitor screening is currently hindered by our inability to grow methanogens in a high-throughput format. We have developed, optimized, and validated a high

  17. 36 CFR 1280.89 - How will NARA handle my request to use public areas in the National Archives at College Park?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... request to use public areas in the National Archives at College Park? 1280.89 Section 1280.89 Parks... College Park, Md § 1280.89 How will NARA handle my request to use public areas in the National Archives at College Park? (a) When you ask to use public areas at the National Archives at College Park, we will...

  18. 36 CFR 1280.87 - Does NARA charge fees for the use of public areas in the National Archives at College Park?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false Does NARA charge fees for the use of public areas in the National Archives at College Park? 1280.87 Section 1280.87 Parks, Forests... College Park, Md § 1280.87 Does NARA charge fees for the use of public areas in the National Archives at...

  19. 36 CFR 1280.87 - Does NARA charge fees for the use of public areas in the National Archives at College Park?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false Does NARA charge fees for the use of public areas in the National Archives at College Park? 1280.87 Section 1280.87 Parks, Forests... College Park, Md § 1280.87 Does NARA charge fees for the use of public areas in the National Archives at...

  20. 7 CFR 1280.629 - FSA county office report.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.629 FSA county office report. The county FSA office report shall be certified as accurate and complete by the CED or designee, acting on... released by the Secretary. A copy of the report shall be posted for 30 calendar days following the date of...

  1. 7 CFR 1280.629 - FSA county office report.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.629 FSA county office report. The county FSA office report shall be certified as accurate and complete by the CED or designee, acting on... released by the Secretary. A copy of the report shall be posted for 30 calendar days following the date of...

  2. 7 CFR 1280.629 - FSA county office report.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.629 FSA county office report. The county FSA office report shall be certified as accurate and complete by the CED or designee, acting on... released by the Secretary. A copy of the report shall be posted for 30 calendar days following the date of...

  3. 7 CFR 1280.629 - FSA county office report.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.629 FSA county office report. The county FSA office report shall be certified as accurate and complete by the CED or designee, acting on... released by the Secretary. A copy of the report shall be posted for 30 calendar days following the date of...

  4. 7 CFR 1280.629 - FSA county office report.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280.629 FSA county office report. The county FSA office report shall be certified as accurate and complete by the CED or designee, acting on... released by the Secretary. A copy of the report shall be posted for 30 calendar days following the date of...

  5. 7 CFR 1280.607 - Farm Service Agency County Executive Director.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280... referred to as “CED,” means the person employed by the FSA County Committee to execute the policies of the...

  6. 7 CFR 1280.607 - Farm Service Agency County Executive Director.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280... referred to as “CED,” means the person employed by the FSA County Committee to execute the policies of the...

  7. 7 CFR 1280.607 - Farm Service Agency County Executive Director.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280... referred to as “CED,” means the person employed by the FSA County Committee to execute the policies of the...

  8. 7 CFR 1280.607 - Farm Service Agency County Executive Director.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280... referred to as “CED,” means the person employed by the FSA County Committee to execute the policies of the...

  9. 7 CFR 1280.607 - Farm Service Agency County Executive Director.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Procedures To Request a Referendum Definitions § 1280... referred to as “CED,” means the person employed by the FSA County Committee to execute the policies of the...

  10. 36 CFR § 1280.8 - May I bring a seeing-eye dog or other assistance animal?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true May I bring a seeing-eye dog or other assistance animal? § 1280.8 Section § 1280.8 Parks, Forests, and Public Property NATIONAL... dog or other assistance animal? Yes, persons with disabilities may bring guide dogs or other animals...

  11. 36 CFR 1280.50 - What will I be allowed to film, photograph, or videotape for news purposes?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... film, photograph, or videotape for news purposes? 1280.50 Section 1280.50 Parks, Forests, and Public... film, photograph, or videotape for news purposes? (a) NARA will permit you to film, photograph, or... (c) or because of scheduling or staffing constraints. (c) We will not grant you permission to film...

  12. 36 CFR 1280.64 - What entrance should I use to enter the National Archives at College Park?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false What entrance should I use to enter the National Archives at College Park? 1280.64 Section 1280.64 Parks, Forests, and Public Property... enter the National Archives at College Park? You may enter the National Archives at College Park...

  13. 36 CFR 1280.50 - What will I be allowed to film, photograph, or videotape for news purposes?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false What will I be allowed to film, photograph, or videotape for news purposes? 1280.50 Section 1280.50 Parks, Forests, and Public... film, photograph, or videotape for news purposes? (a) NARA will permit you to film, photograph, or...

  14. 36 CFR 1280.50 - What will I be allowed to film, photograph, or videotape for news purposes?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false What will I be allowed to film, photograph, or videotape for news purposes? 1280.50 Section 1280.50 Parks, Forests, and Public... film, photograph, or videotape for news purposes? (a) NARA will permit you to film, photograph, or...

  15. 36 CFR 1280.50 - What will I be allowed to film, photograph, or videotape for news purposes?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false What will I be allowed to film, photograph, or videotape for news purposes? 1280.50 Section 1280.50 Parks, Forests, and Public... film, photograph, or videotape for news purposes? (a) NARA will permit you to film, photograph, or...

  16. 36 CFR § 1280.34 - What are the types of corrective action NARA imposes for prohibited behavior?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true What are the types of corrective action NARA imposes for prohibited behavior? § 1280.34 Section § 1280.34 Parks, Forests, and... of corrective action NARA imposes for prohibited behavior? (a) Individuals who violate the provisions...

  17. 8 CFR 1280.51 - Application for mitigation or remission.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 8 Aliens and Nationality 1 2011-01-01 2011-01-01 false Application for mitigation or remission... JUSTICE IMMIGRATION REGULATIONS IMPOSITION AND COLLECTION OF FINES § 1280.51 Application for mitigation or remission. (a) When application may be filed. An application for mitigation or remission of a fine may be...

  18. 8 CFR 1280.51 - Application for mitigation or remission.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 8 Aliens and Nationality 1 2010-01-01 2010-01-01 false Application for mitigation or remission... JUSTICE IMMIGRATION REGULATIONS IMPOSITION AND COLLECTION OF FINES § 1280.51 Application for mitigation or remission. (a) When application may be filed. An application for mitigation or remission of a fine may be...

  19. 18 CFR 367.1280 - Account 128, Other special funds.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... GAS ACT Balance Sheet Chart of Accounts Other Property and Investments § 367.1280 Account 128, Other special funds. (a) This account must include the amount of cash and book cost of investments that have... trading and available-for-sale types of security investments. A separate account with appropriate title...

  20. 7 CFR 1280.623 - Time and place of the referendum.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 1280.623 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB... contacting the nearest county FSA office, the State FSA office, or through an online search of FSA's Web site...

  1. 7 CFR 1280.623 - Time and place of the referendum.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 1280.623 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB... contacting the nearest county FSA office, the State FSA office, or through an online search of FSA's Web site...

  2. 7 CFR 1280.623 - Time and place of the referendum.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 1280.623 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB... contacting the nearest county FSA office, the State FSA office, or through an online search of FSA's Web site...

  3. 7 CFR 1280.623 - Time and place of the referendum.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 1280.623 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB... contacting the nearest county FSA office, the State FSA office, or through an online search of FSA's Web site...

  4. 7 CFR 1280.623 - Time and place of the referendum.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 1280.623 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB... contacting the nearest county FSA office, the State FSA office, or through an online search of FSA's Web site...

  5. Characterization of Influenza Virus Pseudotyped with Ebolavirus Glycoprotein.

    PubMed

    Xiao, Julie Huiyuan; Rijal, Pramila; Schimanski, Lisa; Tharkeshwar, Arun Kumar; Wright, Edward; Annaert, Wim; Townsend, Alain

    2018-02-15

    We have produced a new Ebola virus pseudotype, E-S-FLU, that can be handled in biosafety level 1/2 containment for laboratory analysis. The E-S-FLU virus is a single-cycle influenza virus coated with Ebolavirus glycoprotein, and it encodes enhanced green fluorescence protein as a reporter that replaces the influenza virus hemagglutinin. MDCK-SIAT1 cells were transduced to express Ebolavirus glycoprotein as a stable transmembrane protein for E-S-FLU virus production. Infection of cells with the E-S-FLU virus was dependent on the Niemann-Pick C1 protein, which is the well-characterized receptor for Ebola virus entry at the late endosome/lysosome membrane. The E-S-FLU virus was neutralized specifically by an anti-Ebolavirus glycoprotein antibody and a variety of small drug molecules that are known to inhibit the entry of wild-type Ebola virus. To demonstrate the application of this new Ebola virus pseudotype, we show that a single laboratory batch was sufficient to screen a library (LOPAC 1280 ; Sigma) of 1,280 pharmacologically active compounds for inhibition of virus entry. A total of 215 compounds inhibited E-S-FLU virus infection, while only 22 inhibited the control H5-S-FLU virus coated in H5 hemagglutinin. These inhibitory compounds have very dispersed targets and mechanisms of action, e.g., calcium channel blockers, estrogen receptor antagonists, antihistamines, serotonin uptake inhibitors, etc., and this correlates with inhibitor screening results obtained with other pseudotypes or wild-type Ebola virus in the literature. The E-S-FLU virus is a new tool for Ebola virus cell entry studies and is easily applied to high-throughput screening assays for small-molecule inhibitors or antibodies. IMPORTANCE Ebola virus is in the Filoviridae family and is a biosafety level 4 pathogen. There are no FDA-approved therapeutics for Ebola virus. These characteristics warrant the development of surrogates for Ebola virus that can be handled in more convenient laboratory

  6. Characterization of Influenza Virus Pseudotyped with Ebolavirus Glycoprotein

    PubMed Central

    Xiao, Julie Huiyuan; Rijal, Pramila; Schimanski, Lisa; Tharkeshwar, Arun Kumar; Wright, Edward; Annaert, Wim

    2017-01-01

    ABSTRACT We have produced a new Ebola virus pseudotype, E-S-FLU, that can be handled in biosafety level 1/2 containment for laboratory analysis. The E-S-FLU virus is a single-cycle influenza virus coated with Ebolavirus glycoprotein, and it encodes enhanced green fluorescence protein as a reporter that replaces the influenza virus hemagglutinin. MDCK-SIAT1 cells were transduced to express Ebolavirus glycoprotein as a stable transmembrane protein for E-S-FLU virus production. Infection of cells with the E-S-FLU virus was dependent on the Niemann-Pick C1 protein, which is the well-characterized receptor for Ebola virus entry at the late endosome/lysosome membrane. The E-S-FLU virus was neutralized specifically by an anti-Ebolavirus glycoprotein antibody and a variety of small drug molecules that are known to inhibit the entry of wild-type Ebola virus. To demonstrate the application of this new Ebola virus pseudotype, we show that a single laboratory batch was sufficient to screen a library (LOPAC1280; Sigma) of 1,280 pharmacologically active compounds for inhibition of virus entry. A total of 215 compounds inhibited E-S-FLU virus infection, while only 22 inhibited the control H5-S-FLU virus coated in H5 hemagglutinin. These inhibitory compounds have very dispersed targets and mechanisms of action, e.g., calcium channel blockers, estrogen receptor antagonists, antihistamines, serotonin uptake inhibitors, etc., and this correlates with inhibitor screening results obtained with other pseudotypes or wild-type Ebola virus in the literature. The E-S-FLU virus is a new tool for Ebola virus cell entry studies and is easily applied to high-throughput screening assays for small-molecule inhibitors or antibodies. IMPORTANCE Ebola virus is in the Filoviridae family and is a biosafety level 4 pathogen. There are no FDA-approved therapeutics for Ebola virus. These characteristics warrant the development of surrogates for Ebola virus that can be handled in more convenient

  7. 36 CFR 1280.76 - When are the public areas available for private events in the National Archives Building?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false When are the public areas available for private events in the National Archives Building? 1280.76 Section 1280.76 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What...

  8. 36 CFR 1280.76 - When are the public areas available for private events in the National Archives Building?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false When are the public areas available for private events in the National Archives Building? 1280.76 Section 1280.76 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What...

  9. 36 CFR 1280.80 - How do I request to use NARA public areas in the National Archives Building?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false How do I request to use NARA public areas in the National Archives Building? 1280.80 Section 1280.80 Parks, Forests, and Public... Apply to Use NARA Public Areas in the Washington, DC, Area? National Archives Building, Washington, Dc...

  10. 36 CFR 1280.80 - How do I request to use NARA public areas in the National Archives Building?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false How do I request to use NARA public areas in the National Archives Building? 1280.80 Section 1280.80 Parks, Forests, and Public... Apply to Use NARA Public Areas in the Washington, DC, Area? National Archives Building, Washington, Dc...

  11. 40 CFR 80.1280 - How are refinery benzene baselines calculated?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 17 2014-07-01 2014-07-01 false How are refinery benzene baselines... PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1280 How are refinery benzene baselines calculated? (a) A refinery's benzene...

  12. 40 CFR 80.1280 - How are refinery benzene baselines calculated?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 40 Protection of Environment 17 2012-07-01 2012-07-01 false How are refinery benzene baselines... PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1280 How are refinery benzene baselines calculated? (a) A refinery's benzene...

  13. 40 CFR 80.1280 - How are refinery benzene baselines calculated?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 40 Protection of Environment 16 2010-07-01 2010-07-01 false How are refinery benzene baselines... PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1280 How are refinery benzene baselines calculated? (a) A refinery's benzene...

  14. 40 CFR 80.1280 - How are refinery benzene baselines calculated?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 16 2011-07-01 2011-07-01 false How are refinery benzene baselines... PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1280 How are refinery benzene baselines calculated? (a) A refinery's benzene...

  15. 40 CFR 80.1280 - How are refinery benzene baselines calculated?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 40 Protection of Environment 17 2013-07-01 2013-07-01 false How are refinery benzene baselines... PROGRAMS (CONTINUED) REGULATION OF FUELS AND FUEL ADDITIVES Gasoline Benzene Averaging, Banking and Trading (abt) Program § 80.1280 How are refinery benzene baselines calculated? (a) A refinery's benzene...

  16. 36 CFR 1280.46 - What are the rules for filming, photographing, or videotaping on NARA property for personal use?

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 36 Parks, Forests, and Public Property 3 2014-07-01 2014-07-01 false What are the rules for filming, photographing, or videotaping on NARA property for personal use? 1280.46 Section 1280.46 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA...

  17. 36 CFR 1280.46 - What are the rules for filming, photographing, or videotaping on NARA property for personal use?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false What are the rules for filming, photographing, or videotaping on NARA property for personal use? 1280.46 Section 1280.46 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA...

  18. 36 CFR 1280.46 - What are the rules for filming, photographing, or videotaping on NARA property for personal use?

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 36 Parks, Forests, and Public Property 3 2012-07-01 2012-07-01 false What are the rules for filming, photographing, or videotaping on NARA property for personal use? 1280.46 Section 1280.46 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA...

  19. 36 CFR § 1280.50 - What will I be allowed to film, photograph, or videotape for news purposes?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true What will I be allowed to film, photograph, or videotape for news purposes? § 1280.50 Section § 1280.50 Parks, Forests, and Public Property..., photograph, or videotape for news purposes? (a) NARA will permit you to film, photograph, or videotape...

  20. 36 CFR 1280.71 - What are the general rules for using NARA property in the Washington, DC, area?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false What are the general rules for using NARA property in the Washington, DC, area? 1280.71 Section 1280.71 Parks, Forests, and..., B, and C of this part, you must adhere to the following rules when using NARA public spaces: (a) All...

  1. 36 CFR 1280.71 - What are the general rules for using NARA property in the Washington, DC, area?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false What are the general rules for using NARA property in the Washington, DC, area? 1280.71 Section 1280.71 Parks, Forests, and..., B, and C of this part, you must adhere to the following rules when using NARA public spaces: (a) All...

  2. 26 CFR 1.280F-2T - Limitations on recovery deductions and the investment tax credit for certain passenger...

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... investment tax credit for certain passenger automobiles (temporary). 1.280F-2T Section 1.280F-2T Internal... tax credit for certain passenger automobiles (temporary). (a) Limitation on amount of investment tax... passenger automobile shall not exceed $1,000. For a passenger automobile placed in service after December 31...

  3. 26 CFR 1.280F-2T - Limitations on recovery deductions and the investment tax credit for certain passenger...

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... investment tax credit for certain passenger automobiles (temporary). 1.280F-2T Section 1.280F-2T Internal... tax credit for certain passenger automobiles (temporary). (a) Limitation on amount of investment tax... passenger automobile shall not exceed $1,000. For a passenger automobile placed in service after December 31...

  4. 26 CFR 1.280F-2T - Limitations on recovery deductions and the investment tax credit for certain passenger...

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... investment tax credit for certain passenger automobiles (temporary). 1.280F-2T Section 1.280F-2T Internal... tax credit for certain passenger automobiles (temporary). (a) Limitation on amount of investment tax... passenger automobile shall not exceed $1,000. For a passenger automobile placed in service after December 31...

  5. 26 CFR 1.280F-2T - Limitations on recovery deductions and the investment tax credit for certain passenger...

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... investment tax credit for certain passenger automobiles (temporary). 1.280F-2T Section 1.280F-2T Internal... tax credit for certain passenger automobiles (temporary). (a) Limitation on amount of investment tax... passenger automobile shall not exceed $1,000. For a passenger automobile placed in service after December 31...

  6. 36 CFR 1280.82 - How will NARA handle my request to use public areas in the National Archives Building?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false How will NARA handle my request to use public areas in the National Archives Building? 1280.82 Section 1280.82 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What...

  7. 36 CFR 1280.82 - How will NARA handle my request to use public areas in the National Archives Building?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false How will NARA handle my request to use public areas in the National Archives Building? 1280.82 Section 1280.82 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What...

  8. 26 CFR 1.280F-2T - Limitations on recovery deductions and the investment tax credit for certain passenger...

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... investment tax credit for certain passenger automobiles (temporary). 1.280F-2T Section 1.280F-2T Internal... for certain passenger automobiles (temporary). (a) Limitation on amount of investment tax credit—(1... automobile shall not exceed $1,000. For a passenger automobile placed in service after December 31, 1984, the...

  9. 36 CFR 1280.78 - Does NARA charge fees for the use of public areas in the National Archives Building?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false Does NARA charge fees for the use of public areas in the National Archives Building? 1280.78 Section 1280.78 Parks, Forests, and... inform organizations interested in using public spaces in the National Archives Building in advance and...

  10. 36 CFR 1280.78 - Does NARA charge fees for the use of public areas in the National Archives Building?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false Does NARA charge fees for the use of public areas in the National Archives Building? 1280.78 Section 1280.78 Parks, Forests, and... inform organizations interested in using public spaces in the National Archives Building in advance and...

  11. 40 CFR 60.1280 - What must I do if any of my continuous emission monitoring systems are temporarily unavailable to...

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... emission monitoring systems are temporarily unavailable to meet the data collection requirements? 60.1280... Modification or Reconstruction is Commenced After June 6, 2001 Continuous Emission Monitoring § 60.1280 What must I do if any of my continuous emission monitoring systems are temporarily unavailable to meet the...

  12. 40 CFR 60.1280 - What must I do if any of my continuous emission monitoring systems are temporarily unavailable to...

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... emission monitoring systems are temporarily unavailable to meet the data collection requirements? 60.1280... Modification or Reconstruction is Commenced After June 6, 2001 Continuous Emission Monitoring § 60.1280 What must I do if any of my continuous emission monitoring systems are temporarily unavailable to meet the...

  13. High-Content Positional Biosensor Screening Assay for Compounds to Prevent or Disrupt Androgen Receptor and Transcriptional Intermediary Factor 2 Protein–Protein Interactions

    PubMed Central

    Hua, Yun; Shun, Tong Ying; Strock, Christopher J.

    2014-01-01

    Compounds (LOPAC) set for compounds that inhibited AR-TIF2 PPI formation or disrupted preexisting complexes. Eleven modulators of steroid family nuclear receptors (NRs) and 6 non-NR ligands inhibited AR-TIF2 PPI formation, and 10 disrupted preexisting complexes. The hits appear to be either AR antagonists or nonspecific inhibitors of NR activation and trafficking. Given that the LOPAC set represents such a small and restricted biological and chemical diversity, it is anticipated that screening a much larger and more diverse compound library will be required to find AR-TIF2 PPI inhibitors/disruptors. The AR-TIF2 protein–protein interaction biosensor (PPIB) approach offers significant promise for identifying molecules with potential to modulate AR transcriptional activity in a cell-specific manner that is distinct from the existing antiandrogen drugs that target AR binding or production. Small molecules that disrupt AR signaling at the level of AR-TIF2 PPIs may also overcome the development of resistance and progression to castration-resistant prostate cancer. PMID:25181412

  14. 36 CFR 1280.74 - What spaces in the National Archives Building are available for use by non-NARA groups and...

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false What spaces in the National Archives Building are available for use by non-NARA groups and organizations? 1280.74 Section 1280.74 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA...

  15. 36 CFR 1280.74 - What spaces in the National Archives Building are available for use by non-NARA groups and...

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false What spaces in the National Archives Building are available for use by non-NARA groups and organizations? 1280.74 Section 1280.74 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA...

  16. Preparation and antibacterial activity of compound chitosan-compound Yizhihao-nanoparticles.

    PubMed

    Ou, Sheng; Zhang, Yang-de

    2008-05-01

    To prepare chitosan (CS)-compound Yizhihao-nanoparticles (NP) and to investigate its antibacterial activity. CS NPs were formed by the incorporation of CS and Na3 PO4. CS-compound Yizhihao NPs were prepared by ion-cross-linking. The particle sizes and surface charges of CS NPs were determined by Malvern Zetasizer 1000-HAS and atomic force microscope (AFM), respectively. The antibacterial activity of CS-compound Yizhihao-NPs was studied in vitro and compared with that of compound Yizhihao powder. Malvern Zetasizer 1000-HAS and AFM demonstrated that the diameter of CS-compound Yizhihao NPs was (137.00+/-14.28)nm and CS NPs had (16.90+/-1.32)mV positive surface charges. The minimal inhibitory concentrations (MIC) of CS-compound Yizhihao NPs on Staphylococcus aureus,Pneumococcus,beta-hemolytic streptococcus, and Escherichia coli were 1:32,1:32,1:16,and 1:2, respectively. The minimal bactericidal concentrations (MBC) of CS-compound Yizhihao-NPs on Staphylococcus aureus, Pneumococcus, beta-hemolytic streptococcus, and Escherichia coli were 1:16,1:16,1:8, and 1:2, respectively. The antibacterial efficacy of CS-compound Yizhihao-NPs to Staphylococcus aureus, Pneumococcus, and beta-hemolytic streptococcus had been improved significantly (P< 0.05). CS-compound Yizhihao-nanoparticles have obvious antibacterial activity to the Staphylococcus aureus,Pneumococcus,and beta-hemolytic streptococcus,which lays the experimental foundation for new preparation of traditional Chinese medicine in future research.

  17. Screening with an NMNAT2-MSD platform identifies small molecules that modulate NMNAT2 levels in cortical neurons.

    PubMed

    Ali, Yousuf O; Bradley, Gillian; Lu, Hui-Chen

    2017-03-07

    Nicotinamide mononucleotide adenylyl transferase 2 (NMNAT2) is a key neuronal maintenance factor and provides potent neuroprotection in numerous preclinical models of neurological disorders. NMNAT2 is significantly reduced in Alzheimer's, Huntington's, Parkinson's diseases. Here we developed a Meso Scale Discovery (MSD)-based screening platform to quantify endogenous NMNAT2 in cortical neurons. The high sensitivity and large dynamic range of this NMNAT2-MSD platform allowed us to screen the Sigma LOPAC library consisting of 1280 compounds. This library had a 2.89% hit rate, with 24 NMNAT2 positive and 13 negative modulators identified. Western analysis was conducted to validate and determine the dose-dependency of identified modulators. Caffeine, one identified NMNAT2 positive-modulator, when systemically administered restored NMNAT2 expression in rTg4510 tauopathy mice to normal levels. We confirmed in a cell culture model that four selected positive-modulators exerted NMNAT2-specific neuroprotection against vincristine-induced cell death while four selected NMNAT2 negative modulators reduced neuronal viability in an NMNAT2-dependent manner. Many of the identified NMNAT2 positive modulators are predicted to increase cAMP concentration, suggesting that neuronal NMNAT2 levels are tightly regulated by cAMP signaling. Taken together, our findings indicate that the NMNAT2-MSD platform provides a sensitive phenotypic screen to detect NMNAT2 in neurons.

  18. Screening with an NMNAT2-MSD platform identifies small molecules that modulate NMNAT2 levels in cortical neurons

    PubMed Central

    Ali, Yousuf O.; Bradley, Gillian; Lu, Hui-Chen

    2017-01-01

    Nicotinamide mononucleotide adenylyl transferase 2 (NMNAT2) is a key neuronal maintenance factor and provides potent neuroprotection in numerous preclinical models of neurological disorders. NMNAT2 is significantly reduced in Alzheimer’s, Huntington’s, Parkinson’s diseases. Here we developed a Meso Scale Discovery (MSD)-based screening platform to quantify endogenous NMNAT2 in cortical neurons. The high sensitivity and large dynamic range of this NMNAT2-MSD platform allowed us to screen the Sigma LOPAC library consisting of 1280 compounds. This library had a 2.89% hit rate, with 24 NMNAT2 positive and 13 negative modulators identified. Western analysis was conducted to validate and determine the dose-dependency of identified modulators. Caffeine, one identified NMNAT2 positive-modulator, when systemically administered restored NMNAT2 expression in rTg4510 tauopathy mice to normal levels. We confirmed in a cell culture model that four selected positive-modulators exerted NMNAT2-specific neuroprotection against vincristine-induced cell death while four selected NMNAT2 negative modulators reduced neuronal viability in an NMNAT2-dependent manner. Many of the identified NMNAT2 positive modulators are predicted to increase cAMP concentration, suggesting that neuronal NMNAT2 levels are tightly regulated by cAMP signaling. Taken together, our findings indicate that the NMNAT2-MSD platform provides a sensitive phenotypic screen to detect NMNAT2 in neurons. PMID:28266613

  19. 36 CFR 1280.14 - May I use the shuttle bus to travel to the National Archives at College Park or to the National...

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false May I use the shuttle bus to travel to the National Archives at College Park or to the National Archives Building in Washington, DC? 1280.14 Section 1280.14 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS...

  20. 36 CFR 1280.14 - May I use the shuttle bus to travel to the National Archives at College Park or to the National...

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false May I use the shuttle bus to travel to the National Archives at College Park or to the National Archives Building in Washington, DC? 1280.14 Section 1280.14 Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS...

  1. Evaluation of the Mycobacterium smegmatis and BCG models for the discovery of Mycobacterium tuberculosis inhibitors.

    PubMed

    Altaf, Mudassar; Miller, Christopher H; Bellows, David S; O'Toole, Ronan

    2010-11-01

    The objective of this study was to measure the efficacy of Mycobacterium smegmatis as a surrogate in vitro model for the detection of compounds which are inhibitory to the growth of Mycobacterium tuberculosis. A chemical screen of the LOPAC library for anti-mycobacterial compounds was performed using M. smegmatis. Parallel screens were conducted with another tuberculosis model, Mycobacterium bovis BCG, and with M. tuberculosis under identical growth conditions and the inhibitors detected across the three species were compared. 50% of compounds that were detected as active against M. tuberculosis were not detected using M. smegmatis compared to 21% of compounds using M. bovis BCG. To examine whether these findings were unique to LOPAC, screens were performed with the NIH Diversity Set and Spectrum Collection. An even higher proportion of M. tuberculosis inhibitors were not detected from the NIH Diversity Set and Spectrum Collection using M. smegmatis compared to M. bovis BCG. These data reveal that a significant proportion of M. tuberculosis inhibitors are missed in library screening with M. smegmatis. The basis of the variation in the inhibitory profiles of M. smegmatis and M. tuberculosis has yet to be fully determined, however, our genomic comparisons indicate that approximately 30% of M. tuberculosis proteins lack conserved orthologues in M. smegmatis compared to 3% being absent in M. bovis BCG. In conclusion, although M. smegmatis offers some technical benefits such as a shorter generation time and negligible risk to laboratory workers, it is significantly less effective in the detection of anti-M. tuberculosis compounds relative to M. bovis BCG. This limitation needs to be taken into consideration when selecting an in vitro screening model for tuberculosis drug discovery. Copyright © 2010 Elsevier Ltd. All rights reserved.

  2. 36 CFR 1280.72 - What additional rules apply for a NARA approved event?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false What additional rules apply... ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What Rules Apply to Use NARA Public Areas in the Washington, DC, Area? General § 1280.72 What additional rules apply for a NARA...

  3. 26 CFR 1.280F-4T - Special rules for listed property (temporary).

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 26 Internal Revenue 3 2010-04-01 2010-04-01 false Special rules for listed property (temporary). 1... (CONTINUED) INCOME TAX (CONTINUED) INCOME TAXES Items Not Deductible § 1.280F-4T Special rules for listed...-6(d)(2)) in 1984 through 1988 is 80 percent, 70 percent, 60 percent, and 55 percent, respectively...

  4. A sensitive assay using a native protein substrate for screening HIV-1 maturation inhibitors targeting the protease cleavage site between the matrix and capsid.

    PubMed

    Lee, Sook-Kyung; Cheng, Nancy; Hull-Ryde, Emily; Potempa, Marc; Schiffer, Celia A; Janzen, William; Swanstrom, Ronald

    2013-07-23

    The matrix/capsid processing site in the HIV-1 Gag precursor is likely the most sensitive target to inhibit HIV-1 replication. We have previously shown that modest incomplete processing at the site leads to a complete loss of virion infectivity. In the study presented here, a sensitive assay based on fluorescence polarization that can monitor cleavage at the MA/CA site in the context of the folded protein substrate is described. The substrate, an MA/CA fusion protein, was labeled with the fluorescein-based FlAsH (fluorescein arsenical hairpin) reagent that binds to a tetracysteine motif (CCGPCC) that was introduced within the N-terminal domain of CA. By limiting the size of CA and increasing the size of MA (with an N-terminal GST fusion), we were able to measure significant differences in polarization values as a function of HIV-1 protease cleavage. The sensitivity of the assay was tested in the presence of increasing amounts of an HIV-1 protease inhibitor, which resulted in a gradual decrease in the fluorescence polarization values demonstrating that the assay is sensitive in discerning changes in protease processing. The high-throughput screening assay validation in 384-well plates showed that the assay is reproducible and robust with an average Z' value of 0.79 and average coefficient of variation values of <3%. The robustness and reproducibility of the assay were further validated using the LOPAC(1280) compound library, demonstrating that the assay provides a sensitive high-throughput screening platform that can be used with large compound libraries for identifying novel maturation inhibitors targeting the MA/CA site of the HIV-1 Gag polyprotein.

  5. Influence of plasma-activated compounds on melanogenesis and tyrosinase activity

    PubMed Central

    Ali, Anser; Ashraf, Zaman; Kumar, Naresh; Rafiq, Muhammad; Jabeen, Farukh; Park, Ji Hoon; Choi, Ki Hong; Lee, SeungHyun; Seo, Sung-Yum; Choi, Eun Ha; Attri, Pankaj

    2016-01-01

    Many organic chemists around the world synthesize medicinal compounds or extract multiple compounds from plants in order to increase the activity and quality of medicines. In this work, we synthesized new eugenol derivatives (ED) and then treated them with an N2 feeding gas atmospheric pressure plasma jet (APPJ) to increase their utility. We studied the tyrosinase-inhibition activity (activity test) and structural changes (circular dichroism) of tyrosinase with ED and plasma activated eugenol derivatives (PAED) in a cell-free environment. Later, we used docking studies to determine the possible interaction sites of ED and PAED compounds with tyrosinase enzyme. Moreover, we studied the possible effect of ED and PAED on melanin synthesis and its mechanism in melanoma (B16F10) cells. Additionally, we investigated the structural changes that occurred in activated ED after plasma treatment using nuclear magnetic resonance (NMR). Hence, this study provides a new perspective on PAED for the field of plasma medicine. PMID:26931617

  6. Feasibility of Active Machine Learning for Multiclass Compound Classification.

    PubMed

    Lang, Tobias; Flachsenberg, Florian; von Luxburg, Ulrike; Rarey, Matthias

    2016-01-25

    A common task in the hit-to-lead process is classifying sets of compounds into multiple, usually structural classes, which build the groundwork for subsequent SAR studies. Machine learning techniques can be used to automate this process by learning classification models from training compounds of each class. Gathering class information for compounds can be cost-intensive as the required data needs to be provided by human experts or experiments. This paper studies whether active machine learning can be used to reduce the required number of training compounds. Active learning is a machine learning method which processes class label data in an iterative fashion. It has gained much attention in a broad range of application areas. In this paper, an active learning method for multiclass compound classification is proposed. This method selects informative training compounds so as to optimally support the learning progress. The combination with human feedback leads to a semiautomated interactive multiclass classification procedure. This method was investigated empirically on 15 compound classification tasks containing 86-2870 compounds in 3-38 classes. The empirical results show that active learning can solve these classification tasks using 10-80% of the data which would be necessary for standard learning techniques.

  7. Summary of Proton Test on the Actel A1280A at Indiana University

    NASA Technical Reports Server (NTRS)

    Katz, Richard; LaBel, K.

    1998-01-01

    A summary of tests performed at the Indiana University Cycl,oltron Facility, on the Actel A1280A circuit device is described. The intent of the study was to investigate the proton response of the hard-wired S-Module flip-flops with a large sample size. This device is sensitive to protons for S-Modules. The device's performance in the test is shown in graphs, and was typical for devices of this class.

  8. Mesoionic compounds with antifungal activity against Fusarium verticillioides.

    PubMed

    Paiva, Rojane de Oliveira; Kneipp, Lucimar Ferreira; dos Reis, Camilla Moretto; Echevarria, Aurea

    2015-02-04

    Fungi contaminate the food of humans and animals, are a risk to health, and can cause financial losses. In this work, the antifungal activities of 16 mesoionic compounds (MI 1-16) were evaluated against mycotoxigenic fungi, including Aspergillus spp., Fusarium verticillioides and Penicillium citrinum. Furthermore, the decreased ergosterol in the total lipid content of Fusarium verticillioides was investigated. F. verticillioides was the most sensitive fungus to the mesoionic compounds. Among the evaluated compounds, MI-11 and MI-16 presented higher antifungal effects against F. verticillioides, with MIC values of 7.8 μg/ml, and MI-2 and MI-3 followed, with MICs of 15.6 μg/ml. The most active compounds were those with heterocyclic ring phenyl groups substituted by electron donor moieties (MI-11 and MI-16). Among some compounds with higher activity (MI-2, MI-11 and MI-16), decreased ergosterol content in the total lipid fraction of F. verticillioides was demonstrated. MI-2 reduced the ergosterol content approximately 40% and 80% at concentrations of 7.8 μg/ml and 15.6 μg/ml, respectively, and MI-11 and MI-16 decreased the content by 30% and 50%, respectively, when at a concentration of 7.8 μg/ml. These findings indicate that mesoionic compounds have significant antifungal activity against F. verticillioides.

  9. Antimicrobial activity and cytotoxic effects of Magnolia dealbata and its active compounds.

    PubMed

    Jacobo-Salcedo, Maria del Rosario; Gonzalez-Espindola, Luis Angel; Alonso-Castro, Angel Josabad; Gonzalez-Martinez, Marisela del Rocio; Domínguez, Fabiola; Garcia-Carranca, Alejandro

    2011-08-01

    Multi-drug resistance is of great concern for public health worldwide and necessitates the search for new antimicrobials from sources such as plants. Several Magnolia (Magnoliaceae) species have been reported to exert antimicrobial effects on sensitive and multidrug-resistant microorganisms. However, the antimicrobial properties of Magnolia dealbata have not been experimentally evaluated. The antimicrobial effects of an ethanol extract of Magnolia dealbata seeds (MDE) and its active compounds honokiol (HK) and magnolol (MG) were tested against the phytopathogen Clavibacter michiganensis subsp. michiganensis and several human multi-drug resistant pathogens using the disk-diffusion assay. The effects of MDE and its active compounds on the viability of human peripheral blood mononuclear cells (PBMC) were evaluated using MTT assay. MDE and its active compounds had antimicrobial activity (inhibition zone > 10 mm) against C. michiganensis, Pseudomonas aeruginosa, Acinetobacter baumannii, Acinetobacter lwoffii, Candida albicans, Candida tropicalis and Trichosporon belgeii. The results suggest that M. dealbata and its active compounds have selective antimicrobial effects against drug-resistant fungal and Gram (-) bacteria and exert minimal toxic effects on human PMBC.

  10. 26 CFR 1.280F-7 - Property leased after December 31, 1986.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...,146 1,698 2,036 2,351 51,000 52,000 538 1,176 1,743 2,090 2,413 52,000 53,000 552 1,206 1,788 2,144 2... 62,000 670 1,465 2,171 2,603 3,005 62,000 64,000 698 1,525 2,262 2,711 3,130 64,000 66,000 726 1,586... the business use percentage (as defined in § 1.280F-6(d)(1)) is 50 percent or less, and (C) The...

  11. In vitro imaging of remaining dentin and pulp chamber by optical coherence tomography: comparison between 850 and 1280 nm

    NASA Astrophysics Data System (ADS)

    Fonsêca, Déborah D. D.; Kyotoku, Bernardo B. C.; Maia, Ana M. A.; Gomes, Anderson S. L.

    2009-03-01

    We report the application of optical coherence tomography (OCT) to generate images of the remaining dentin and pulp chamber of in vitro human teeth. Bidimensional images of remaining dentin and of the pulp chamber were obtained parallel to the long axis of the teeth, by two OCT systems operating around 1280 and 850 nm, and compared to tomography images using the i-CAT® Cone Beam Volumetric Tomography system as the gold standard. The results demonstrated the efficacy of the OCT technique; furthermore, the wavelength close to 1280 nm presented greater penetration depth in the dentine than 850 nm, as expected from scattering and absorption coefficients. The OCT technique has great potential to be used on clinical practice, preventing accidental exposure of the pulp and promoting preventive restoration treatment.

  12. Compound Structure-Independent Activity Prediction in High-Dimensional Target Space.

    PubMed

    Balfer, Jenny; Hu, Ye; Bajorath, Jürgen

    2014-08-01

    Profiling of compound libraries against arrays of targets has become an important approach in pharmaceutical research. The prediction of multi-target compound activities also represents an attractive task for machine learning with potential for drug discovery applications. Herein, we have explored activity prediction in high-dimensional target space. Different types of models were derived to predict multi-target activities. The models included naïve Bayesian (NB) and support vector machine (SVM) classifiers based upon compound structure information and NB models derived on the basis of activity profiles, without considering compound structure. Because the latter approach can be applied to incomplete training data and principally depends on the feature independence assumption, SVM modeling was not applicable in this case. Furthermore, iterative hybrid NB models making use of both activity profiles and compound structure information were built. In high-dimensional target space, NB models utilizing activity profile data were found to yield more accurate activity predictions than structure-based NB and SVM models or hybrid models. An in-depth analysis of activity profile-based models revealed the presence of correlation effects across different targets and rationalized prediction accuracy. Taken together, the results indicate that activity profile information can be effectively used to predict the activity of test compounds against novel targets. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  13. Bactericidal activity of glutaraldehyde-like compounds from olive products.

    PubMed

    Medina, Eduardo; Brenes, Manuel; García, Aranzazu; Romero, Concepción; de Castro, Antonio

    2009-12-01

    The bactericidal effects of several olive compounds (nonenal, oleuropein, tyrosol, the dialdehydic form of decarboxymethyl elenolic acid either free [EDA] or linked to tyrosol [TyEDA] or to hydroxytyrosol [HyEDA]), other food phenolic compounds (catechin, epicatechin, eugenol, thymol, carvacrol, and carnosic acid), and commercial disinfectants (glutaraldehyde [GTA] and ortho-phthalaldehyde [OPA]), were tested against strains of Pseudomonas fluorescens, Staphylococcus aureus, Enterococcus faecalis, and Escherichia coli. It was found that the bactericidal activities of olive GTA-like compounds (EDA, HyEDA, and TyEDA) were greater than those exerted by several food phenolic substances. Surprisingly, these olive antimicrobials were as active as the synthetic biocides GTA and OPA against the four bacteria studied. Thus, it has been proposed that the bactericidal activity of the main olive antimicrobials is primarily due to their dialdehydic structure, which is similar to that of the commercial biocides GTA and OPA. Our results clearly reveal that olive GTA-like compounds possess a strong bactericidal activity even greater than that of other food phenolic compounds or synthetic biocides.

  14. Antioxidative activities and active compounds of extracts from Catalpa plant leaves.

    PubMed

    Xu, Hongyu; Hu, Gege; Dong, Juane; Wei, Qin; Shao, Hongbo; Lei, Ming

    2014-01-01

    In order to screen the Catalpa plant with high antioxidant activity and confirm the corresponding active fractions from Catalpa ovata G. Don, C. fargesii Bur., and C. bungei C. A. Mey., total flavonoid contents and antioxidant activities of the extracts/fractions of Catalpa plant leaves were determined. The determined total flavonoid content and antioxidant activity were used as assessment criteria. Those compounds with antioxidant activity were isolated with silica gel column chromatography and ODS column chromatography. Our results showed that the total flavonoid content in C. bungei C. A. Mey. (30.07 mg/g · DW) was the highest, followed by those in C. fargesii Bur. (25.55 mg/g · DW) and C. ovata G. Don (24.96 mg/g · DW). According to the determination results of total flavonoid content and antioxidant activity in 3 clones of leaves of C. bungei C. A. Mey., the total flavonoid content and antioxidant activity in crude extracts from C. bungei C. A. Mey. 6 (CA6) leaves were the highest. Moreover, the results showed that the total flavonoid content and antioxidant activities of ethyl acetate (EA) fraction in ethanol crude extracts in CA6 leaves were the highest, followed by n-butanol, petroleum ether (PE), and water fractions. Two flavonoid compounds with antioxidant activity were firstly isolated based on EA fraction. The two compounds were luteolin (1) and apigenin (2), respectively.

  15. Antioxidant Activity of Phenolic Compounds from Fava Bean Sprouts.

    PubMed

    Okumura, Koharu; Hosoya, Takahiro; Kawarazaki, Kai; Izawa, Norihiko; Kumazawa, Shigenori

    2016-06-01

    Fava beans are eaten all over the world and recently, marketing for their sprouts began in Japan. Fava bean sprouts contain more polyphenols and l-3,4-dihydroxyphenylalanine (l-DOPA) than the bean itself. Our antioxidant screening program has shown that fava bean sprouts also possess a higher antioxidant activity than other commercially available sprouts and mature beans. However, the individual constituents of fava bean sprouts are not entirely known. In the present study, we investigated the phenolic compounds of fava bean sprouts and their antioxidant activity. Air-dried fava bean sprouts were treated with 80% methanol and the extract was partitioned in water with chloroform and ethyl acetate. HPLC analysis had shown that the ethyl acetate-soluble parts contained phenolic compounds, separated by preparative HPLC to yield 5 compounds (1-5). Structural analysis using NMR and MS revealed that the compounds isolated were kaempferol glycosides. All isolated compounds had an α-rhamnose at the C-7 position with different sugars attached at the C-3 position. Compounds 1-5 had β-galactose, β-glucose, α-rhamnose, 6-acetyl-β-galactose and 6-acetyl-β-glucose, respectively, at the C-3 position. The amount of l-DOPA in fava bean sprouts was determined by the quantitative (1) H NMR technique. The l-DOPA content was 550.45 mg ± 11.34 /100 g of the raw sprouts. The antioxidant activities of compounds 2-5 and l-DOPA were evaluated using the 2,2-diphenyl-1-picrylhydrazyl scavenging assay. l-DOPA showed high antioxidant activity, but the isolated kaempferol glycosides showed weak activity. Therefore, it can be suggested that l-DOPA contributed to the antioxidant activity of fava bean sprouts. © 2016 Institute of Food Technologists®

  16. Antioxidative Activities and Active Compounds of Extracts from Catalpa Plant Leaves

    PubMed Central

    Xu, Hongyu; Hu, Gege; Dong, Juane; Wei, Qin; Shao, Hongbo; Lei, Ming

    2014-01-01

    In order to screen the Catalpa plant with high antioxidant activity and confirm the corresponding active fractions from Catalpa ovata G. Don, C. fargesii Bur., and C. bungei C. A. Mey., total flavonoid contents and antioxidant activities of the extracts/fractions of Catalpa plant leaves were determined. The determined total flavonoid content and antioxidant activity were used as assessment criteria. Those compounds with antioxidant activity were isolated with silica gel column chromatography and ODS column chromatography. Our results showed that the total flavonoid content in C. bungei C. A. Mey. (30.07 mg/g·DW) was the highest, followed by those in C. fargesii Bur. (25.55 mg/g·DW) and C. ovata G. Don (24.96 mg/g·DW). According to the determination results of total flavonoid content and antioxidant activity in 3 clones of leaves of C. bungei C. A. Mey., the total flavonoid content and antioxidant activity in crude extracts from C. bungei C. A. Mey. 6 (CA6) leaves were the highest. Moreover, the results showed that the total flavonoid content and antioxidant activities of ethyl acetate (EA) fraction in ethanol crude extracts in CA6 leaves were the highest, followed by n-butanol, petroleum ether (PE), and water fractions. Two flavonoid compounds with antioxidant activity were firstly isolated based on EA fraction. The two compounds were luteolin (1) and apigenin (2), respectively. PMID:25431795

  17. The Mast Cell Degranulator Compound 48/80 Directly Activates Neurons

    PubMed Central

    Schemann, Michael; Kugler, Eva Maria; Buhner, Sabine; Eastwood, Christopher; Donovan, Jemma; Jiang, Wen; Grundy, David

    2012-01-01

    Background Compound 48/80 is widely used in animal and tissue models as a “selective” mast cell activator. With this study we demonstrate that compound 48/80 also directly activates enteric neurons and visceral afferents. Methodology/Principal Findings We used in vivo recordings from extrinsic intestinal afferents together with Ca++ imaging from primary cultures of DRG and nodose neurons. Enteric neuronal activation was examined by Ca++ and voltage sensitive dye imaging in isolated gut preparations and primary cultures of enteric neurons. Intraluminal application of compound 48/80 evoked marked afferent firing which desensitized on subsequent administration. In egg albumen-sensitized animals, intraluminal antigen evoked a similar pattern of afferent activation which also desensitized on subsequent exposure to antigen. In cross-desensitization experiments prior administration of compound 48/80 failed to influence the mast cell mediated response. Application of 1 and 10 µg/ml compound 48/80 evoked spike discharge and Ca++ transients in enteric neurons. The same nerve activating effect was observed in primary cultures of DRG and nodose ganglion cells. Enteric neuron cultures were devoid of mast cells confirmed by negative staining for c-kit or toluidine blue. In addition, in cultured enteric neurons the excitatory action of compound 48/80 was preserved in the presence of histamine H1 and H2 antagonists. The mast cell stabilizer cromolyn attenuated compound 48/80 and nicotine evoked Ca++ transients in mast cell-free enteric neuron cultures. Conclusions/Significance The results showed direct excitatory action of compound 48/80 on enteric neurons and visceral afferents. Therefore, functional changes measured in tissue or animal models may involve a mast cell independent effect of compound 48/80 and cromolyn. PMID:23272218

  18. Targeting the epigenome: Screening bioactive compounds that regulate histone deacetylase activity

    PubMed Central

    Godoy, Luis D.; Lucas, Julianna E.; Bender, Abigail J.; Romanick, Samantha S.; Ferguson, Bradley S.

    2017-01-01

    Scope Nutrigenomics is a rapidly expanding field that elucidates the link between diet-genome interactions. Recent evidence demonstrates that regulation of the epigenome, and in particular inhibition of HDACs, impact pathogenetic mechanisms involved in chronic disease. Few studies, to date, have screened libraries of bioactive compounds that act as epigenetic modifiers. This study screened a library of 131 natural compounds to determine bioactive compounds that inhibit Zn-dependent HDAC activity. Methods and results Using class-specific HDAC substrates, we screened 131 natural compounds for HDAC activity in bovine cardiac tissue. From this screen, we identified 18 bioactive compound HDAC inhibitors. Using our class-specific HDAC substrates, we next screened these 18 bioactive compounds against recombinant HDAC proteins. Consistent with inhibition of HDAC activity, these compounds were capable of inhibiting activity of individual HDAC isoforms. Lastly, we report that treatment of H9c2 cardiac myoblasts with bioactive HDAC inhibitors was sufficient to increase lysine acetylation as assessed via immunoblot. Conclusion This study provided the first step in identifying multiple bioactive compound HDAC inhibitors. Taken together, this report sets the stage for future exploration of these bioactive compounds as epigenetic regulators to potentially ameliorate chronic disease. PMID:27981795

  19. Targeting the epigenome: Screening bioactive compounds that regulate histone deacetylase activity.

    PubMed

    Godoy, Luis D; Lucas, Julianna E; Bender, Abigail J; Romanick, Samantha S; Ferguson, Bradley S

    2017-04-01

    Nutrigenomics is a rapidly expanding field that elucidates the link between diet-genome interactions. Recent evidence demonstrates that regulation of the epigenome, and in particular inhibition of histone deacetylases (HDACs), impact pathogenetic mechanisms involved in chronic disease. Few studies, to date, have screened libraries of bioactive compounds that act as epigenetic modifiers. This study screened a library of 131 natural compounds to determine bioactive compounds that inhibit Zn-dependent HDAC activity. Using class-specific HDAC substrates, we screened 131 natural compounds for HDAC activity in bovine cardiac tissue. From this screen, we identified 18 bioactive compound HDAC inhibitors. Using our class-specific HDAC substrates, we next screened these 18 bioactive compounds against recombinant HDAC proteins. Consistent with inhibition of HDAC activity, these compounds were capable of inhibiting activity of individual HDAC isoforms. Lastly, we report that treatment of H9c2 cardiac myoblasts with bioactive HDAC inhibitors was sufficient to increase lysine acetylation as assessed via immunoblot. This study provided the first step in identifying multiple bioactive compound HDAC inhibitors. Taken together, this report sets the stage for future exploration of these bioactive compounds as epigenetic regulators to potentially ameliorate chronic disease. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  20. Anti-cancer activity of compounds from Bauhinia strychnifolia stem.

    PubMed

    Yuenyongsawad, Supreeya; Bunluepuech, Kingkan; Wattanapiromsakul, Chatchai; Tewtrakul, Supinya

    2013-11-25

    The stem and root of Bauhinia strychnifolia Craib (Fabaceae family) have been traditionally used in Thailand to treat fever, alcoholic toxication, allergy and cancer. An EtOH extract of Bauhinia strychnifolia showed good inhibitory activity against several cancer cell lines including HT-29, HeLa, MCF-7 and KB. As there has been no previous reports on chemical constituents of Bauhinia strychnifolia, this study is aimed to isolate the pure compounds with anti-cancer activity. Five pure compounds were isolated from EtOH extract of Bauhinia strychnifolia stem using silica gel, dianion HP-20 and sephadex LH-20 column chromatography and were tested for their cytotoxic effects against HT-29, HeLa, MCF-7 and KB cell lines using the Sulforhodamine B (SRB) assay. Among five compounds, 3,5,7,3',5'-pentahydroxyflavanonol-3-O-α-l-rhamnopyranoside (2) possessed very potent activity against KB (IC₅₀=0.00054μg/mL), HT-29 (IC₅₀=0.00217 μg/mL), MCF-7 (IC₅₀=0.0585 μg/mL) and HeLa cells (IC₅₀=0.0692 μg/mL). 3,5,7-Trihydroxychromone-3-O-α-l-rhamnopyranoside (3) also showed good activity against HT-29 (IC₅₀=0.02366 μg/mL), KB (IC₅₀=0.0412 μg/mL) and MCF-7 (IC₅₀=0.297 μg/mL), respectively. The activity of 2 (IC₅₀=0.00054 μg/mL) against KB cell was ten times higher than that of the positive control, Camptothecin (anti-cancer drug, IC₅₀=0.0057 μg/mL). All compounds did not show any cytotoxicity with normal cells at the concentration of 1 μg/mL. This is the first report of compounds 2 and 3 on anti-cancer activity and based on the anti-cancer activity of extracts and pure compounds isolated from Bauhinia strychnifolia stem, it might be suggested that this plant could be useful for treatment of cancer. © 2013 Elsevier Ireland Ltd. All rights reserved.

  1. Progress in the field of physiologically active lanosterol compounds

    NASA Astrophysics Data System (ADS)

    Reshetova, I. G.; Tkhaper, R. K.; Kamernitskii, Alexey V.

    1992-08-01

    This review correlates the studies (up to 1991) on the isolation, structural determination, biological activity, and synthesis of physiologically active polyoxidised lanosterol derivatives of vegetable (inotodiol, ganoderic acids) and animal (seychellogenin) origin. The cytotoxic, cardiovascular, and other forms of activity of compounds of this type are of considerable interest in relation to their medical use. It is noted that the functionalised side chain (in an open form or containing lactones, lactols, etc.) is generally responsible for the activity exhibited by lanosterol derivatives. Two basic approaches to the derivation of these structures are defined: either by complete reconstruction of the side chain of lanosterol (degradation and rebuilding with oxygen-containing residues) or by progressive functionalisation of the Δ24-side chain of lanosterol. The synthesis of the known anticancer compound "inotodiol", seychellogenins, ganoderic acids, and other compounds are described. The bibliography includes 105 references.

  2. Different phenolic compounds activate distinct human bitter taste receptors.

    PubMed

    Soares, Susana; Kohl, Susann; Thalmann, Sophie; Mateus, Nuno; Meyerhof, Wolfgang; De Freitas, Victor

    2013-02-20

    Bitterness is a major sensory attribute of several common foods and beverages rich in polyphenol compounds. These compounds are reported as very important for health as chemopreventive compounds, but they are also known to taste bitter. In this work, the activation of the human bitter taste receptors, TAS2Rs, by six polyphenol compounds was analyzed. The compounds chosen are present in a wide range of plant-derived foods and beverages, namely, red wine, beer, tea, and chocolate. Pentagalloylglucose (PGG) is a hydrolyzable tannin, (-)-epicatechin is a precursor of condensed tannins, procyanidin dimer B3 and trimer C2 belong to the condensed tannins, and malvidin-3-glucoside and cyanidin-3-glucoside are anthocyanins. The results show that the different compounds activate different combinations of the ~25 TAS2Rs. (-)-Epicatechin activated three receptors, TAS2R4, TAS2R5, and TAS2R39, whereas only two receptors, TAS2R5 and TAS2R39, responded to PGG. In contrast, malvidin-3-glucoside and procyanidin trimer stimulated only one receptor, TAS2R7 and TAS2R5, respectively. Notably, tannins are the first natural agonists found for TAS2R5 that display high potency only toward this receptor. The catechol and/or galloyl groups appear to be important structural determinants that mediate the interaction of these polyphenolic compounds with TAS2R5. Overall, the EC(50) values obtained for the different compounds vary 100-fold, with the lowest values for PGG and malvidin-3-glucoside compounds, suggesting that they could be significant polyphenols responsible for the bitterness of fruits, vegetables, and derived products even if they are present in very low concentrations.

  3. Antileishmanial activities of dihydrochalcones from piper elongatum and synthetic related compounds. Structural requirements for activity.

    PubMed

    Hermoso, Alicia; Jiménez, Ignacio A; Mamani, Zulma A; Bazzocchi, Isabel L; Piñero, José E; Ravelo, Angel G; Valladares, Basilio

    2003-09-01

    Two dihydrochalcones (1 and 2) were isolated from Piper elongatum Vahl by activity-guided fractionation against extracellular promastigotes of Leishmania braziliensis in vitro. Their structures were elucidated by spectral analysis, including homonuclear and heteronuclear correlation NMR experiments. Derivatives 3-7 and 20 synthetic related compounds (8-27) were also assayed to establish the structural requirements for antileishmanial activity. Compounds 1-11 that proved to be more active that ketoconazol, used as positive control, were further assayed against promastigotes of Leishmania tropica and Leishmania infantum. Compounds 7 and 11, with a C(6)-C(3)-C(6) system, proved to be the most promising compounds, with IC(50) values of 2.98 and 3.65 microg/mL, respectively, and exhibited no toxic effect on macrophages (around 90% viability). Correlation between the molecular structures and antileishmanial activity is discussed in detail.

  4. Synthesis and evaluation of curcumin-related compounds for anticancer activity.

    PubMed

    Wei, Xingchuan; Du, Zhi-Yun; Zheng, Xi; Cui, Xiao-Xing; Conney, Allan H; Zhang, Kun

    2012-07-01

    Sixty-one curcumin-related compounds were synthesized and evaluated for their anticancer activity toward cultured prostate cancer PC-3 cells, pancreas cancer Panc-1 cells and colon cancer HT-29 cells. Inhibitory effects of these compounds on the growth of PC-3, Panc-1 and HT-29 cells were determined by the MTT assay. Compounds E10, F10, FN1 and FN2 exhibited exceptionally potent inhibitory effects on the growth of cultured PC-3, Panc-1 and HT-29 cells. The IC(50) for these compounds was lower than 1 μM in all three cell lines. E10 was 72-, 46- and 117-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. F10 was 69-, 34- and 72-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. FN1 and FN2 had about the same inhibitory effect as E10 and F10 toward Panc-1 cells but were less active than E10 and F10 toward PC-3 and HT-29 cells. The active compounds were potent stimulators of apoptosis. The present study indicates that E10, F10, FN1 and FN2 may have useful anticancer activity. Copyright © 2012 Elsevier Masson SAS. All rights reserved.

  5. 36 CFR § 1280.94 - When do Presidential libraries allow other groups to use their public areas for events?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true When do Presidential libraries... FACILITIES What Additional Rules Apply for Use of Facilities in Presidential Libraries? § 1280.94 When do Presidential libraries allow other groups to use their public areas for events? (a) Although Presidential...

  6. 7 CFR 1280.211 - Prohibited activities.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ...; and (c) Any advertising, including promotion, research, and information activities authorized to be... AGREEMENTS AND ORDERS; MISCELLANEOUS COMMODITIES), DEPARTMENT OF AGRICULTURE LAMB PROMOTION, RESEARCH, AND INFORMATION ORDER Lamb Promotion, Research, and Information Order Lamb Promotion, Research, and Information...

  7. Isolation, identification and antioxidant activity of bound phenolic compounds present in rice bran.

    PubMed

    Wang, Wei; Guo, Jia; Zhang, Junnan; Peng, Jie; Liu, Tianxing; Xin, Zhihong

    2015-03-15

    The bound phenolic compounds in rice bran were released and extracted with ethyl acetate based on alkaline digestion. An investigation of the chemical constituents of EtOAc extract has led to the isolation of a new compound, para-hydroxy methyl benzoate glucoside (8), together with nine known compounds, cycloeucalenol cis-ferulate (1), cycloeucalenol trans-ferulate (2), trans-ferulic acid (3), trans-ferulic acid methyl ester (4), cis-ferulic acid (5), cis-ferulic acid methyl ester (6), methyl caffeate (7), vanillic aldehyde (9) and para-hydroxy benzaldehyde (10). The structures of these compounds were determined using a combination of spectroscopic methods and chemical analysis. Among the compounds isolated, compound 3, 5 and 7 exhibited strong DPPH and ABTS(+) radical scavenging activities, followed by compounds 4 and 6. Compound 1 and 2 showed potent DPPH and ABTS(+) radical scavenging activities, compound 8 displayed moderate antioxidant activity against ABTS(+) radical, whereas compound 9 and 10 showed weak antioxidant activity. Copyright © 2014 Elsevier Ltd. All rights reserved.

  8. Taste-active compounds in a traditional Italian food: 'lampascioni'.

    PubMed

    Borgonovo, Gigliola; Caimi, Sara; Morini, Gabriella; Scaglioni, Leonardo; Bassoli, Angela

    2008-06-01

    Nature is a rich source of taste-active compounds, in particular of plant origin, many of which have unusual tastes. Many of these are found in traditional food, where spontaneous plants are used as ingredients. Some taste-active compounds were identified in the bulbs of Muscari comosum, a spontaneous plant belonging to the family of the Liliaceae, very common in the Mediterranean area, and used in traditional gastronomy (called 'lampascioni' in South Italy). The bulbs were extracted with a series of solvents of different polarity. The different fractions were submitted to a preliminary sensory evaluation, and the most interesting ones, characterized by a strong bitter taste and some chemestetic properties, were submitted to further purification and structural analysis. From the ethereal extract, several 3-benzyl-4-chromanones and one stilbene derivative were isolated. Pure compounds were examined for their taste activity by means of sensory evaluation, and proved to be responsible for the characteristic taste of this food. Some of these compounds have been synthesized de novo to confirm their structure.

  9. Glucosidase inhibitory activity and antioxidant activity of flavonoid compound and triterpenoid compound from Agrimonia Pilosa Ledeb

    PubMed Central

    2014-01-01

    Background In Chinese traditional medicine, Agrimonia pilosa Ledeb (APL) exhibits great effect on treatment of type 2 diabetes mellitus (T2DM), however its mechanism is still unknown. Considering that T2DM are correlated with postprandial hyperglycemia and oxidative stress, we investigated the α-glucosidase inhibitory activity and the antioxidant activity of flavonoid compound (FC) and triterpenoid compound (TC) from APL. Methods Entire plants of APL were extracted using 95% ethanol and 50% ethanol successively. The resulting extracts were partitioned and isolated by applying liquid chromatography using silica gel column and Sephadex LH 20 column to give FC and TC. The content of total flavonoids in FC and the content of total triterpenoids in TC were determined by using UV spectrophotometry. HPLC analysis was used to identify and quantify the monomeric compound in FC and TC. The α-glucosidase inhibitory activities were determined using the chromogenic method with p-nitrophenyl-α-D-glucopyranoside as substrate. Antioxidant activities were assessed through three kinds of radical scavenging assays (DPPH radical, ABTS radical and hydroxyl radical) & β-carotene-linoleic acid assay. Results The results indicate FC is abundant of quercitrin, and hyperoside, and TC is abundant of 1β, 2β, 3β, 19α-tetrahydroxy-12-en-28-oic acid (265.2 mg/g) and corosolic acid (100.9 mg/g). The FC & the TC have strong α-glucosidase inhibitory activities with IC50 of 8.72 μg/mL and 3.67 μg/mL, respectively. We find that FC show competitive inhibition against α-glucosidase, while the TC exhibits noncompetitive inhibition. Furthermore, The FC exhibits significant radical scavenging activity with the EC50 values of 7.73 μg/mL, 3.64 μg/mL and 5.90 μg/mL on DPPH radical, hydroxyl radical and ABTS radical, respectively. The FC also shows moderate anti-lipid peroxidation activity with the IC50 values of 41.77 μg/mL on inhibiting β-carotene bleaching. Conclusion These results

  10. Glucosidase inhibitory activity and antioxidant activity of flavonoid compound and triterpenoid compound from Agrimonia Pilosa Ledeb.

    PubMed

    Liu, Xi; Zhu, Liancai; Tan, Jun; Zhou, Xuemei; Xiao, Ling; Yang, Xian; Wang, Bochu

    2014-01-10

    In Chinese traditional medicine, Agrimonia pilosa Ledeb (APL) exhibits great effect on treatment of type 2 diabetes mellitus (T2DM), however its mechanism is still unknown. Considering that T2DM are correlated with postprandial hyperglycemia and oxidative stress, we investigated the α-glucosidase inhibitory activity and the antioxidant activity of flavonoid compound (FC) and triterpenoid compound (TC) from APL. Entire plants of APL were extracted using 95% ethanol and 50% ethanol successively. The resulting extracts were partitioned and isolated by applying liquid chromatography using silica gel column and Sephadex LH 20 column to give FC and TC. The content of total flavonoids in FC and the content of total triterpenoids in TC were determined by using UV spectrophotometry. HPLC analysis was used to identify and quantify the monomeric compound in FC and TC. The α-glucosidase inhibitory activities were determined using the chromogenic method with p-nitrophenyl-α-D-glucopyranoside as substrate. Antioxidant activities were assessed through three kinds of radical scavenging assays (DPPH radical, ABTS radical and hydroxyl radical) & β-carotene-linoleic acid assay. The results indicate FC is abundant of quercitrin, and hyperoside, and TC is abundant of 1β, 2β, 3β, 19α-tetrahydroxy-12-en-28-oic acid (265.2 mg/g) and corosolic acid (100.9 mg/g). The FC & the TC have strong α-glucosidase inhibitory activities with IC50 of 8.72 μg/mL and 3.67 μg/mL, respectively. We find that FC show competitive inhibition against α-glucosidase, while the TC exhibits noncompetitive inhibition. Furthermore, The FC exhibits significant radical scavenging activity with the EC50 values of 7.73 μg/mL, 3.64 μg/mL and 5.90 μg/mL on DPPH radical, hydroxyl radical and ABTS radical, respectively. The FC also shows moderate anti-lipid peroxidation activity with the IC50 values of 41.77 μg/mL on inhibiting β-carotene bleaching. These results imply that the FC and the TC could be

  11. Isolation and Antimicrobial Activity of Flavonoid Compounds from Mahagony Seeds (Swietenia macrophylla, King)

    NASA Astrophysics Data System (ADS)

    Mursiti, S.; Supartono

    2017-02-01

    Flavonoid is one of the secondary metabolites compounds in mahogany seeds. Mahogany seeds can be used as an antimicrobial. This study aims to determine the antimicrobial activity of flavonoid compounds from mahogany seeds against Escherichia coli (E.coli) and Bacillus cereus (B.cereus). Isolation of flavonoid compounds done step by step. First, the maceration using n-hexane, then with methanol. The methanol extract was dissolved in ethyl acetate and aquadest, then separated. Ethyl acetate extract evaporated Flavonoid compounds were. The testing of antimicrobial activity of flavonoid compounds using the absorption method. The results showed that the antimicrobial activity of flavonoid compounds from mahogany seeds shows the inhibitory activity and provide clear zone against bacteria E.coli with value Inhibitory Regional Diameter 18.50 mm respectively, and 14.50 mm to the bacteria. Based on the results of the study, it can be concluded that flavonoid compounds from mahogany seeds have antimicrobial activity against E.coli and B.cereus.

  12. Alkaline phosphatase activity-guided isolation of active compounds and new dammarane-type triterpenes from Cissus quadrangularis hexane extract.

    PubMed

    Pathomwichaiwat, Thanika; Ochareon, Pannee; Soonthornchareonnon, Noppamas; Ali, Zulfiqar; Khan, Ikhlas A; Prathanturarug, Sompop

    2015-02-03

    The stem of Cissus quadrangularis L. (CQ) is used in traditional medicine to treat bone fractures and swelling. Anti-osteoporotic activity of CQ hexane extract has been reported, but the active compounds in this extract remain unknown. Thus, we aimed to identify the active compounds in CQ hexane extract using bioassay-guided isolation. The CQ hexane extract was fractionated sequentially with benzene, dichloromethane, ethyl acetate, and methanol. The examination of CQ extract and its fractions was guided by bioassays for alkaline phosphatase (ALP) activity during the differentiation of MC3T3-E1 osteoblastic cells. The cells were treated with or without the CQ extract and its fractions for a period of time, and then the stimulatory effect of the alkaline phosphatase enzyme, a bone differentiation marker, was investigated. The compounds obtained were structurally elucidated using spectroscopic techniques and re-evaluated for activity during bone differentiation. A total of 29 compounds were isolated, viz., triterpenes, fatty acid methyl esters, glycerolipids, steroids, phytols, and cerebrosides. Four new dammarane-type triterpenes were isolated for the first time from nature, and this report is the first to identify this group of compounds from the Vitaceae family. Seven compounds, viz., glycerolipids and squalene, stimulated ALP activity at a dose of 10μg/mL. Moreover, the synergistic effect of these compounds on bone formation was demonstrated. This report describes, for the first time, the isolation of active compounds from CQ hexane extract; these active compounds will be useful for the quality control of extracts from this plant used to treat osteoporosis. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

  13. Aqua mediated synthesis of bio-active compounds.

    PubMed

    Panda, Siva S

    2013-05-01

    Recently the aqueous medium has attracted the interest of organic chemists, and many. Moreover, in the past 20 years, the drug-discovery process has undergone extraordinary changes, and high-throughput biological screening of potential drug candidates has led to an ever-increasing demand for novel drug-like compounds. Noteworthy advantages were observed during the course of study on aqua mediated synthesis of compounds of medicinal importance. The established advantages of water as a solvent for reactions are, water is the most abundant and available resource on the planet and many biochemical processes occur in aqueous medium. This review will focus on describing new developments in the application of water in medicinal chemistry for the synthesis of bio-active compounds possessing various biological properties.

  14. 36 CFR 1280.86 - When are the public areas available for events in the National Archives at College Park?

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false When are the public areas... Rules Apply to Use NARA Public Areas in the Washington, DC, Area? National Archives at College Park, Md § 1280.86 When are the public areas available for events in the National Archives at College Park? Most...

  15. 36 CFR 1280.86 - When are the public areas available for events in the National Archives at College Park?

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false When are the public areas... Rules Apply to Use NARA Public Areas in the Washington, DC, Area? National Archives at College Park, Md § 1280.86 When are the public areas available for events in the National Archives at College Park? Most...

  16. Concentration evolution of pharmaceutically active compounds in raw urban and industrial wastewater.

    PubMed

    Camacho-Muñoz, Dolores; Martín, Julia; Santos, Juan Luis; Aparicio, Irene; Alonso, Esteban

    2014-09-01

    The distribution of pharmaceutically active compounds in the environment has been reported in several works in which wastewater treatment plants have been identified as the main source of these compounds to the environment. The concentrations of these compounds in influent wastewater can vary widely not only during the day but also along the year, because of the seasonal-consumption patterns of some pharmaceuticals. However, only few studies have attempted to assess the hourly variability of the concentrations of pharmaceutically active compounds in wastewater. In this work, the distribution and seasonal and hourly variability of twenty-one pharmaceuticals, belonging to seven therapeutic groups, have been investigated in urban and industrial wastewater. The highest concentrations of pharmaceutically active compounds, except salicylic acid, were found in urban wastewater, especially in the case of anti-inflammatory drugs and caffeine. The highest concentrations of salicylic acid were measured in industrial wastewater, reaching concentration levels up to 3295μgL(-)(1). The studied pharmaceutically active compounds showed different distribution patterns during winter and summer periods. Temporal variability of pharmaceutically active compounds during a 24-h period showed a distribution in concordance with their consumption and excretion patterns, in the case of urban wastewater, and with the schedule of industrial activities, in the case of industrial wastewater. Copyright © 2014 Elsevier Ltd. All rights reserved.

  17. Lignans, bacteriocides and organochlorine compounds activate the human pregnane X receptor (PXR)

    DOE Office of Scientific and Technical Information (OSTI.GOV)

    Jacobs, Miriam N.; Nolan, Gail T.; Hood, Steven R.

    2005-12-01

    The pregnane X receptor (PXR) mediates the induction of enzymes involved in steroid metabolism and xenobiotic detoxification. The receptor is expressed in liver and intestinal tissues and is activated by a wide range of compounds. The ability of a diverse range of dietary compounds to activate PXR-mediated transcription was assayed in HuH7 cells following transient transfection with human PXR (hPXR). The compounds investigated included phytochemicals such as lignans and phytoestrogens, organochlorine dietary contaminants such as polychlorinated biphenyls (PCBs) and triclosan and selected steroid, drug and herbal compounds. The hPXR activation at the top concentrations tested (10 {mu}M) relative to themore » positive control 10 {mu}M rifampicin ranged from 1.3% (trans-resveratrol) to 152% (ICI 182780). Hydroxylated compounds were marginally more potent than the parent compounds (tamoxifen activation was 74.6% whereas 4 hydroxytamoxifen activation was 84.2%) or significantly greater (vitamin D{sub 3} activation was 1.6%, while hydroxylated vitamin D{sub 3} activation was 55.6%). Enterolactone, the metabolite of common dietary lignans, was a medium activator of PXR (35.6%), compared to the lower activation of a parent lignan, secoisolariciresinol (20%). Two non-hydroxylated PCB congeners (PCB 118 and 153), which present a larger fraction of the PCB contamination of fatty foods, activated hPXR by 26.6% and 17%, respectively. The pesticide trans-nonachlor activation was 53.8%, while the widely used bacteriocide triclosan was a medium activator of hPXR at 46.2%. The responsiveness of PXR to activation by lignan metabolites suggests that dietary intake of these compounds may affect the metabolism of drugs that are CYP3A substrates. Additionally, the evidence that organochlorine chemicals, particularly the ubiquitous triclosan, activate hPXR suggests that these environmental chemicals may, in part, exhibit their endocrine disruptor activities by altering PXR

  18. Multidirectional Efficacy of Biologically Active Nitro Compounds Included in Medicines.

    PubMed

    Olender, Dorota; Żwawiak, Justyna; Zaprutko, Lucjusz

    2018-05-29

    The current concept in searching for new bioactive products, including mainly original active substances with potential application in pharmacy and medicine, is based on compounds with a previously determined structure, well-known properties, and biological activity profile. Nowadays, many commonly used drugs originated from natural sources. Moreover, some natural materials have become the source of leading structures for processing further chemical modifications. Many organic compounds with great therapeutic significance have the nitro group in their structure. Very often, nitro compounds are active substances in many well-known preparations belonging to different groups of medicines that are classified according to their pharmacological potencies. Moreover, the nitro group is part of the chemical structure of veterinary drugs. In this review, we describe many bioactive substances with the nitro group, divided into ten categories, including substances with exciting activity and that are currently undergoing clinical trials.

  19. 36 CFR § 1280.46 - What are the rules for filming, photographing, or videotaping on NARA property for personal use?

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 36 Parks, Forests, and Public Property 3 2013-07-01 2012-07-01 true What are the rules for filming..., and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF NARA FACILITIES What Are the Rules for Filming, Photographing, or Videotaping on NARA Property? § 1280.46 What are...

  20. Phenolic compound concentration and antioxidant activities of edible and medicinal mushrooms from Korea.

    PubMed

    Kim, Min-Young; Seguin, Philippe; Ahn, Joung-Kuk; Kim, Jong-Jin; Chun, Se-Chul; Kim, Eun-Hye; Seo, Su-Hyun; Kang, Eun-Young; Kim, Sun-Lim; Park, Yool-Jin; Ro, Hee-Myong; Chung, Ill-Min

    2008-08-27

    A study was conducted to determine the content of phenolic compounds and the antioxidative activity of five edible and five medicinal mushrooms commonly cultivated in Korea. Phenolic compounds were analyzed using high performance liquid chromatography, and antioxidant activity was evaluated by 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity and superoxide dismutase activity. A total of 28 phenolic compounds were detected in the mushrooms studied. The average total concentration of phenolic compounds was 326 microg/g, the average being of 174 microg/g in edible mushrooms and 477 microg/g in medicinal mushrooms. The average total flavonoids concentration was 49 microg/g, with averages of 22 and 76 microg/g in edible and medicinal mushrooms, respectively. The DPPH radical scavenging activities ranged between 15 (Pleurotus eryngii) and 70% (Ganoderma lucidum) when reaction time was for 1 min. When reaction time was 30 min, the values ranged between 5 (Pleurotus eryngii) and 78% (Agaricus bisporus). The SOD activity averaged 28% among the 10 mushroom species, averages for edible and medicinal mushrooms being comparable. DPPH activities was significantly correlated (p < 0.01) with total content of phenolic compounds in edible mushrooms, while in medicinal mushrooms there was a significant correlation (p < 0.01) between SOD activity and total concentration of phenolic compounds. Numerous significant positive correlations were observed between phenolic compounds detected and antioxidative potential.

  1. Structure-Activity Correlations with Compounds Related to Abscisic Acid 1

    PubMed Central

    Sondheimer, Ernest; Walton, Daniel C.

    1970-01-01

    Inhibition of cell expansion of excised embryonic axes of Phaseolus vulgaris was used to evaluate the growth-inhibiting activity of abscisic acid and related compounds. None of the 13 compounds tested was as active as abscisic acid. 4-Hydroxyisophorone, a substance representative of the abscisic acid ring system was essentially inactive; cis, trans-3-methylsorbic acid, a compound resembling the side chain of abscisic acid, had low activity; and cis, trans-β-ionylideneacetic acid was one-sixth as active. Loss of the ring double bond results in a drastic decrease in biological activity. Comparison of our results with those reported previously leads to the suggestion that the double bond of the cyclohexyl moiety may have an important function in determining the degree of activity of cis, trans-ionylideneacetic acids. Two modes of action are discussed. It seems possible that the ring double bond is involved in covalent bonding in binding of the abscisic acid analogue to macromolecules. This may require formation of an intermediate epoxide. It can also be argued that stereochemical differences between cyclohexane derivatives are important factors in determining the degree of biological activity. PMID:5423465

  2. Algicidal activity of marine Alteromonas sp. KNS-16 and isolation of active compounds.

    PubMed

    Cho, Ji Young

    2012-01-01

    The KNS-16 algicidal strain was isolated from a harmful alga bloom (HAB) area and identified as Alteromonas sp. based on 16S rDNA sequencing. The KNS-16 strain was found to control HABs by producing algicidal compounds in an indirect interaction. Four active compounds were isolated from KNS-16 culture, and their structures were analyzed by interpreting nuclear magnetic resonance and mass spectroscopy data. The structures were identified as 2-undecen-1'-yl-4-quinolone (1), 2-undecyl-4-quinolone (2), 3-hexyl-6-pentyl-4-hydroxyl-2H-pyran-2-one (3), and 6-heptyl-3-hexyl-4-hydroxyl-2H-pyran-2-one (4). Compound 1 was most active against HABs such as Heterosigma akashiwo, Cochlodinium polykrikoides, and Alexandrium tamarense with LC(50) values of 0.5-1.1 µg/mL. The four compounds exhibited high LC(50) values against aquaculture algae such as Tetaselmis suecica, Isochrysis galbana, and Pavlova lutheri at 39-66 µg/mL. Based on toxicity tests on the brine shrimp Artemia salina and the rotifer Brachionus rotundiformis, the four compounds showed ranges of 409-608 and 189-224 µg/mL of LC(50) for the two organisms, respectively. The LC(50) values for juvenile fish of Sebastes schlegelii were 284-304 µg/mL.

  3. How to acquire new biological activities in old compounds by computer prediction

    NASA Astrophysics Data System (ADS)

    Poroikov, V. V.; Filimonov, D. A.

    2002-11-01

    Due to the directed way of testing chemical compounds' in drug research and development many projects fail because serious adverse effects and toxicity are discovered too late, and many existing prospective activities remain unstudied. Evaluation of the general biological potential of molecules is possible using a computer program PASS that predicts more than 780 pharmacological effects, mechanisms of action, mutagenicity, carcinogenicity, etc. on the basis of structural formulae of compounds, with average accuracy ˜85%. PASS applications to both databases of available samples included hundreds of thousands compounds, and small collections of compounds synthesized by separate medicinal chemists are described. It is shown that 880 compounds from Prestwick chemical library represent a very diverse pharmacological space. New activities can be found in existing compounds by prediction. Therefore, on this basis, the selection of compounds with required and without unwanted properties is possible. Even when PASS cannot predict very new activities, it may recognize some unwanted actions at the early stage of R&D, providing the medicinal chemist with the means to increase the efficiency of projects.

  4. Advances in the development of AMPK-activating compounds.

    PubMed

    Sriwijitkamol, Apiradee; Musi, Nicolas

    2008-10-01

    AMP-activated protein kinase (AMPK) is an energy sensing enzyme that controls glucose and lipid metabolism. This review summarizes the present data on AMPK as a pharmacologic target for the treatment of metabolic disorders. The mechanisms governing AMPK activity and how this enzyme controls different metabolic pathways are reviewed briefly, and details about the effect that AMPK activators have on glucose metabolism are provided. Evidence obtained using the AMPK-activating compound 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranoside (AICAR) suggests that AMPK promotes glucose transport into skeletal muscles and that this enzyme inhibits hepatic glucose production. AICAR also induces fatty acid oxidation in muscle and inhibits cholesterol synthesis in the liver. The metabolic effects of AICAR on glucose and lipid metabolism indicate that AMPK may be a good pharmacologic target for the treatment of type 2 diabetes and hypercholesterolemia. Novel AMPK-specific compounds are allowing researchers to examine whether this enzyme is a useful pharmacologic target for the treatment of human disease and whether chronic activation of AMPK will be safe.

  5. Antibacterial activities of naturally occurring compounds against Mycobacterium avium subsp. paratuberculosis.

    PubMed

    Wong, Stella Y Y; Grant, Irene R; Friedman, Mendel; Elliott, Christopher T; Situ, Chen

    2008-10-01

    The antibacterial activities of 18 naturally occurring compounds (including essential oils and some of their isolated constituents, apple and green tea polyphenols, and other plant extracts) against three strains of Mycobacterium avium subsp. paratuberculosis (a bovine isolate [NCTC 8578], a raw-milk isolate [806R], and a human isolate [ATCC 43015]) were evaluated using a macrobroth susceptibility testing method. M. avium subsp. paratuberculosis was grown in 4 ml Middlebrook 7H9 broth containing 10% oleic acid-albumin-dextrose-catalase, 0.05% Tween 80 (or 0.2% glycerol), and 2 microg/ml mycobactin J supplemented with five concentrations of each test compound. The changes in the optical densities of the cultures at 600 nm as a measure of CFU were recorded at intervals over an incubation period of 42 days at 37 degrees C. Six of the compounds were found to inhibit the growth of M. avium subsp. paratuberculosis. The most effective compound was trans-cinnamaldehyde, with a MIC of 25.9 microg/ml, followed by cinnamon oil (26.2 microg/ml), oregano oil (68.2 microg/ml), carvacrol (72.2 microg/ml), 2,5-dihydroxybenzaldehyde (74 microg/ml), and 2-hydroxy-5-methoxybenzaldehyde (90.4 microg/ml). With the exception of carvacrol, a phenolic compound, three of the four most active compounds are aldehydes, suggesting that the structure of the phenolic group or the aldehyde group may be important to the antibacterial activity. No difference in compound activity was observed between the three M. avium subsp. paratuberculosis strains studied. Possible mechanisms of the antimicrobial effects are discussed.

  6. Cryptic antifungal compounds active by synergism with polyene antibiotics.

    PubMed

    Kinoshita, Hiroshi; Yoshioka, Mariko; Ihara, Fumio; Nihira, Takuya

    2016-04-01

    The majority of antifungal compounds reported so far target the cell wall or cell membrane of fungi, suggesting that other types of antibiotics cannot exert their activity because they cannot penetrate into the cells. Therefore, if the permeability of the cell membrane could be enhanced, many antibiotics might be found to have antifungal activity. We here used the polyene antibiotic nystatin, which binds to ergosterol and forms pores at the cell membrane, to enhance the cellular permeability. In the presence of nystatin, many culture extracts from entomopathogenic fungi displayed antifungal activity. Among all the active extracts, two active components were purified and identified as helvolic acid and terramide A. Because the minimum inhibitory concentration of either compound was reduced four-fold in the presence of nystatin, it can be concluded that this screening method is useful for detecting novel antifungal activity. Copyright © 2015 The Society for Biotechnology, Japan. Published by Elsevier B.V. All rights reserved.

  7. [Biological activity of selenorganic compounds at heavy metal salts intoxication].

    PubMed

    Rusetskaya, N Y; Borodulin, V B

    2015-01-01

    Possible mechanisms of the antitoxic action of organoselenium compounds in heavy metal poisoning have been considered. Heavy metal toxicity associated with intensification of free radical oxidation, suppression of the antioxidant system, damage to macromolecules, mitochondria and the genetic material can cause apoptotic cell death or the development of carcinogenesis. Organic selenium compounds are effective antioxidants during heavy metal poisoning; they exhibit higher bioavailability in mammals than inorganic ones and they are able to activate antioxidant defense, bind heavy metal ions and reactive oxygen species formed during metal-induced oxidative stress. One of promising organoselenium compounds is diacetophenonyl selenide (DAPS-25), which is characterized by antioxidant and antitoxic activity, under conditions including heavy metal intoxication.

  8. Antibacterial Activities of Naturally Occurring Compounds against Mycobacterium avium subsp. paratuberculosis▿

    PubMed Central

    Wong, Stella Y. Y.; Grant, Irene R.; Friedman, Mendel; Elliott, Christopher T.; Situ, Chen

    2008-01-01

    The antibacterial activities of 18 naturally occurring compounds (including essential oils and some of their isolated constituents, apple and green tea polyphenols, and other plant extracts) against three strains of Mycobacterium avium subsp. paratuberculosis (a bovine isolate [NCTC 8578], a raw-milk isolate [806R], and a human isolate [ATCC 43015]) were evaluated using a macrobroth susceptibility testing method. M. avium subsp. paratuberculosis was grown in 4 ml Middlebrook 7H9 broth containing 10% oleic acid-albumin-dextrose-catalase, 0.05% Tween 80 (or 0.2% glycerol), and 2 μg/ml mycobactin J supplemented with five concentrations of each test compound. The changes in the optical densities of the cultures at 600 nm as a measure of CFU were recorded at intervals over an incubation period of 42 days at 37°C. Six of the compounds were found to inhibit the growth of M. avium subsp. paratuberculosis. The most effective compound was trans-cinnamaldehyde, with a MIC of 25.9 μg/ml, followed by cinnamon oil (26.2 μg/ml), oregano oil (68.2 μg/ml), carvacrol (72.2 μg/ml), 2,5-dihydroxybenzaldehyde (74 μg/ml), and 2-hydroxy-5-methoxybenzaldehyde (90.4 μg/ml). With the exception of carvacrol, a phenolic compound, three of the four most active compounds are aldehydes, suggesting that the structure of the phenolic group or the aldehyde group may be important to the antibacterial activity. No difference in compound activity was observed between the three M. avium subsp. paratuberculosis strains studied. Possible mechanisms of the antimicrobial effects are discussed. PMID:18676709

  9. Activating AMP-activated protein kinase by an α1 selective activator compound 13 attenuates dexamethasone-induced osteoblast cell death

    DOE Office of Scientific and Technical Information (OSTI.GOV)

    Guo, Shiguang; Mao, Li; Ji, Feng, E-mail: huaiaifengjidr@163.com

    Excessive glucocorticoid (GC) usage may lead to non-traumatic femoral head osteonecrosis. Dexamethasone (Dex) exerts cytotoxic effect to cultured osteoblasts. Here, we investigated the potential activity of Compound 13 (C13), a novel α1 selective AMP-activated protein kinase (AMPK) activator, against the process. Our data revealed that C13 pretreatment significantly attenuated Dex-induced apoptosis and necrosis in both osteoblastic-like MC3T3-E1 cells and primary murine osteoblasts. AMPK activation mediated C13′ cytoprotective effect in osteoblasts. The AMPK inhibitor Compound C, shRNA-mediated knockdown of AMPKα1, or dominant negative mutation of AMPKα1 (T172A) almost abolished C13-induced AMPK activation and its pro-survival effect in osteoblasts. On the othermore » hand, forced AMPK activation by adding AMPK activator A-769662 or exogenous expression a constitutively-active (ca) AMPKα1 (T172D) mimicked C13's actions and inhibited Dex-induced osteoblast cell death. Meanwhile, A-769662 or ca-AMPKα1 almost nullified C13's activity in osteoblast. Further studies showed that C13 activated AMPK-dependent nicotinamide adenine dinucleotide phosphate (NADPH) pathway to inhibit Dex-induced reactive oxygen species (ROS) production in MC3T3-E1 cells and primary murine osteoblasts. Such effects by C13 were almost reversed by Compound C or AMPKα1 depletion/mutation. Together, these results suggest that C13 alleviates Dex-induced osteoblast cell death via activating AMPK signaling pathway. - Highlights: • Compound 13 (C13) attenuates dexamethasone (Dex)-induced osteoblast cell death. • C13-induced cytoprotective effect against Dex in osteoblasts requires AMPK activation. • Forced AMPK activation protects osteoblasts from Dex, nullifying C13's activities. • C13 increases NADPH activity and inhibits Dex-induced oxidative stress in osteoblasts.« less

  10. Repellent activity of estrogenic compounds toward zoospores of the phytopathogenic fungus Aphanomyces cochlioides.

    PubMed

    Islam, M T; Tahara, S

    2001-01-01

    Screening chemical compounds, we found that a xenoestrogen, bisphenol A, showed potent repellent activity against the zoospores of Aphanomyces cochlioides. Based on this finding, we tested a number of androgenic and estrogenic compounds (e.g. testosterone, progesterone, estradiols, diethylstilbestrol, estrone, estriol, pregnenolone, dienestrol etc.) on the motility behavior of A. cochlioides zoospores. Interestingly, most of the estrogenic compounds exhibited potent repellent activity (1 microg/ml or less by the "particle method") toward the motile zoospores of A. cochlioides. We derivatized some of the estrogens and discussed the relationship between the structure of active molecules and their repellent activity. Apparently, aromatization of the A ring with a free hydroxyl group at C-3 position of a steroidal structure is necessary for higher repellent activity. Interestingly, methylation of diethylstilbestrol (DES) yielded completely different activity i.e. both mono- and di-methyl ethers of DES showed attractant activity. Moreover, the attracted zoospores were encysted and then germinated in the presence of di-methyl ether of DES. The potential usefulness of this repellent test is discussed for the detection of estrogenic activity of naturally occurring compounds, and the possible role of phytoestrogens in host/parasite interactions. So far, this will be the first report of repellent activity of estrogenic compounds toward trivial fungal zoospores.

  11. Removal of pharmaceutically active compounds in nitrifying-denitrifying plants.

    PubMed

    Suárez, S; Ramil, M; Omil, F; Lema, J M

    2005-01-01

    The behaviour of nine pharmaceutically active compounds (PhACs) of different diagnostic groups is studied during a nitrifying-denitrifying process in an activated sludge system. The compounds selected cover a wide range of frequently used substances such as anti-epileptics (carbamazepine), tranquillisers (diazepam), anti-depressants (fluoxetine and citalopram), anti-inflammatories (ibuprofen, naproxen and diclofenac) and estrogens (estradiol and ethinylestradiol). The main objective of this research is to investigate the effect of acclimation of biomass on the removal rates of these compounds, either by maintaining a high sludge retention time or at long-term operation. The removal rates achieved for nitrogen and carbon in the experimental unit exceed 90% and were not affected by the addition of PhACs. Carbamazepine, diazepam and diclofenac were only removed to a small extent. On the other hand, higher removal rates have been observed for naproxen and ibuprofen (68% and 82%), respectively.

  12. Antimicrobial activity of fractions and compounds from Calophyllumbrasiliense (Clusiaceae/Guttiferae).

    PubMed

    Pretto, Juliana B; Cechinel-Filho, Valdir; Noldin, Vânia F; Sartori, Mara R K; Isaias, Daniela E B; Cruz, Alexandre Bella

    2004-01-01

    Calophyllum brasiliense (Clusiaceae/Guttiferae) is a native Brazilian medicinal plant traditionally used against several diseases, including infectious pathologies. Crude methanolic extracts (CME) and two fractions, denoted non-polar (soluble in chloroform) and polar (nonsoluble in chloroform), were prepared from different parts of the plant (roots, stems, leaves, flowers and fruits) and studied. The following compounds were isolated and tested against pathogenic bacteria and yeasts by determination of the minimal inhibitory concentration (MIC): brasiliensic acid (1), gallic acid (2), epicatechin (3), protocatechuic acid (4), friedelin (5) and 1,5-dihydroxyxanthone (6). The results indicated that all the parts of the plant exhibited antimicrobial activity against Gram-positive bacteria, which are selectively inhibited by components of C. brasiliense. No activity was observed against Gram-negative bacteria and yeasts tested. Regarding the isolated compounds, substance 4 showed antimicrobial activity against all the tested microorganisms, whereas compound 6 exhibited antimicrobial activity only against Gram-positive bacteria. The results from the current study confirm and justify the popular use of this plant to treat infectious processes.

  13. Isolation, Separation, and Preconcentration of Biologically Active Compounds from Plant Matrices by Extraction Techniques.

    PubMed

    Raks, Victoria; Al-Suod, Hossam; Buszewski, Bogusław

    2018-01-01

    Development of efficient methods for isolation and separation of biologically active compounds remains an important challenge for researchers. Designing systems such as organomineral composite materials that allow extraction of a wide range of biologically active compounds, acting as broad-utility solid-phase extraction agents, remains an important and necessary task. Selective sorbents can be easily used for highly selective and reliable extraction of specific components present in complex matrices. Herein, state-of-the-art approaches for selective isolation, preconcentration, and separation of biologically active compounds from a range of matrices are discussed. Primary focus is given to novel extraction methods for some biologically active compounds including cyclic polyols, flavonoids, and oligosaccharides from plants. In addition, application of silica-, carbon-, and polymer-based solid-phase extraction adsorbents and membrane extraction for selective separation of these compounds is discussed. Potential separation process interactions are recommended; their understanding is of utmost importance for the creation of optimal conditions to extract biologically active compounds including those with estrogenic properties.

  14. The Antimicrobial Activities of Extract and Compounds Isolated from Brillantaisia lamium

    PubMed Central

    Tamokou, Jean De Dieu; Kuiate, Jules Roger; Tene, Mathieu; Kenla Nwemeguela, Timothée Julbelin; Tane, Pierre

    2011-01-01

    Background: Brillantaisia lamium is an erect branched herb, which grows to a height of 1.50 m in moist tropical areas, both in full sun and partial shade. In , the aerial part of this plant is used in the treatment of various microbial infections such as skin diseases and infections of urinary tract. The aim of this study was to evaluate the antimicrobial activities of CH2Cl2: MeOH (1:1) extract, fractions and compounds from the aerial part of B. lamium. Methods: The plant was dried and extracted by maceration in CH2Cl2: MeOH (1:1 v/v). Structures of the compounds from the CH2Cl2: MeOH (1:1) soluble fraction were determined by spectroscopic methods and compared with published data. The broth micro dilution method was used to evaluate the antimicrobial activities against bacteria and fungal species. Results: Four known compounds: aurantiamide acetate (1), lupeol (2), lespedin (3), sitosterol 3-O-β-D-glucopyranoside (4) and a mixture of sterols: campesterol (5), stigmasterol (6) and β-sitosterol (7) were isolated from CH2Cl2: MeOH (1:1) extract of B. lamium aerial parts. The crude extract, fractions and isolated compounds exhibited both antibacterial and antifungal activities that varied with microorganism (MIC=6.25 – 1000 µg/ml). Compound 3 was the most active (MIC=6.25 – 100 µg/ml) while Staphylococcus aureus, Enterococcus faecalis, Candida tropicalis and Cryptococcus neoformans were the most sensitive to all the tested compounds. Conclusion: The overall results of this study indicate that the CH2Cl2: MeOH (1:1) extract and some of isolated compounds have interesting antimicrobial properties and can be used for the treatment of fungal and bacterial infections. PMID:23365474

  15. Extraction, chemical characterization and biological activity determination of broccoli health promoting compounds.

    PubMed

    Ares, Ana M; Nozal, María J; Bernal, José

    2013-10-25

    Broccoli (Brassica oleracea L. var. Italica) contains substantial amount of health-promoting compounds such as vitamins, glucosinolates, phenolic compounds, and dietary essential minerals; thus, it benefits health beyond providing just basic nutrition, and consumption of broccoli has been increasing over the years. This review gives an overview on the extraction and separation techniques, as well as the biological activity of some of the above mentioned compounds which have been published in the period January 2008 to January 2013. The work has been distributed according to the different families of health promoting compounds discussing the extraction procedures and the analytical techniques employed for their characterization. Finally, information about the different biological activities of these compounds has been also provided. Copyright © 2013 Elsevier B.V. All rights reserved.

  16. 36 CFR 1280.85 - What space in the National Archives at College Park is available for use by non-NARA groups and...

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 36 Parks, Forests, and Public Property 3 2010-07-01 2010-07-01 false What space in the National... Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF... Archives at College Park, Md § 1280.85 What space in the National Archives at College Park is available for...

  17. 36 CFR 1280.85 - What space in the National Archives at College Park is available for use by non-NARA groups and...

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 36 Parks, Forests, and Public Property 3 2011-07-01 2011-07-01 false What space in the National... Parks, Forests, and Public Property NATIONAL ARCHIVES AND RECORDS ADMINISTRATION NARA FACILITIES USE OF... Archives at College Park, Md § 1280.85 What space in the National Archives at College Park is available for...

  18. Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.

    PubMed

    Carroll, Richard T; Dluzen, Dean E; Stinnett, Hilary; Awale, Prabha S; Funk, Max O; Geldenhuys, Werner J

    2011-08-15

    The neuroprotective activity of pioglitazone and rosiglitazone in the MPTP parkinsonian mouse prompted us to evaluate a set of thiazolidinedione (TZD) type compounds for monoamine oxidase A and B inhibition activity. These compounds were able to inhibit MAO-B over several log units of magnitude (82 nM to 600 μM). Initial structure-activity relationship studies identified key areas to modify the aromatic substituted TZD compounds. Primarily, substitutions on the aromatic group and the TZD nitrogen were key areas where activity was enhanced within this group of compounds. Copyright © 2011 Elsevier Ltd. All rights reserved.

  19. Compounds from the aerial parts of Piper bavinum and their anti-cholinesterase activity.

    PubMed

    Dung, Hoang Viet; Cuong, To Dao; Chinh, Nguyen Minh; Quyen, Do; Kim, Jeong Ah; Byeon, Jeong Su; Woo, Mi Hee; Choi, Jae Sui; Min, Byung Sun

    2015-01-01

    A new alkenylphenol, bavinol A (1), together with six known compounds (2-7) were isolated from the aerial parts of Piper bavinum (Piperaceae). The chemical structures of these compounds were determined by spectroscopic analyses including 2D NMR spectroscopy. The anti-Alzheimer effects of compounds 1-7 were evaluated from acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity assays. Bavinol A (1), ampelopsin (3), and violanthin (4) exhibited AChE inhibitory activities with IC50 values of 29.80, 59.47 and 79.80 μM. Compound 1 also showed the most potent BChE inhibitory activity with an IC50 value of 19.25 μM.

  20. Synthesis of Some Novel Thiadiazole Derivative Compounds and Screening Their Antidepressant-Like Activities.

    PubMed

    Can, Nafiz Öncü; Can, Özgür Devrim; Osmaniye, Derya; Demir Özkay, Ümide

    2018-03-21

    Novel thiadiazole derivatives were synthesized through the reaction of acetylated 2-aminothiadiazole and piperazine derivatives. The chemical structures of the compounds were clarified by Infrared Spectroscopy (IR), ¹H Nuclear Magnetic Resonance Spectroscopy (¹H-NMR), 13 C Nuclear Magnetic Resonance Spectroscopy ( 13 C-NMR) and Electronspray Ionisation Mass Spectroscopy (ESI-MS) spectroscopic methods. Antidepressant-like activities were evaluated by the tail-suspension (TST) and modified forced swimming (MFST) methods. Besides, possible influence of the test compounds on motor activities of the animals were examined by activity cage tests. In the TST, administration of the compounds 2c , 2d , 2e , 2f , 2g and 2h significantly decreased the immobility time of mice regarding the control values. Further, in the MFST, the same compounds reduced the total number of immobility behaviors while increasing swimming performance. However, no change was observed in the total number of climbing behaviors. These data suggested that compounds 2c , 2d , 2e , 2f , 2g and 2h possess notable antidepressant-like activities. Reference drug fluoxetine (10 mg/kg) was also exhibited its antidepressant activity, as expected. No significant difference was seen between the locomotor activity values of the test groups signifying that observed antidepressant-like activities are specific. Theoretical calculation of absorption, distribution, metabolism, excretion (ADME) properties for the obtained compounds were performed and obtained data supported the antidepressant-like potential of these novel thiadiazole derivatives.

  1. Compound annotation with real time cellular activity profiles to improve drug discovery.

    PubMed

    Fang, Ye

    2016-01-01

    In the past decade, a range of innovative strategies have been developed to improve the productivity of pharmaceutical research and development. In particular, compound annotation, combined with informatics, has provided unprecedented opportunities for drug discovery. In this review, a literature search from 2000 to 2015 was conducted to provide an overview of the compound annotation approaches currently used in drug discovery. Based on this, a framework related to a compound annotation approach using real-time cellular activity profiles for probe, drug, and biology discovery is proposed. Compound annotation with chemical structure, drug-like properties, bioactivities, genome-wide effects, clinical phenotypes, and textural abstracts has received significant attention in early drug discovery. However, these annotations are mostly associated with endpoint results. Advances in assay techniques have made it possible to obtain real-time cellular activity profiles of drug molecules under different phenotypes, so it is possible to generate compound annotation with real-time cellular activity profiles. Combining compound annotation with informatics, such as similarity analysis, presents a good opportunity to improve the rate of discovery of novel drugs and probes, and enhance our understanding of the underlying biology.

  2. Role of ozone and granular activated carbon in the removal of mutagenic compounds.

    PubMed Central

    Bourbigot, M M; Hascoet, M C; Levi, Y; Erb, F; Pommery, N

    1986-01-01

    The identification of certain organic compounds in drinking water has led water treatment specialists to be increasingly concerned about the eventual risks of such pollutants to the health of consumers. Our experiments focused on the role of ozone and granular activated carbon in removing mutagenic compounds and precursors that become toxic after chlorination. We found that if a sufficient dose of ozone is applied, its use does not lead to the creation of mutagenic compounds in drinking water and can even eliminate the initial mutagenicity of the water. The formation of new mutagenic compounds seems to be induced by ozonation that is too weak, although these mutagens can be removed by GAC filtration. Ozone used with activated carbon can be one of the best means for eliminating the compounds contributing to the mutagenicity of water. A combined treatment of ozone and activated carbon also decreases the chlorine consumption of the treated water and consequently reduces the formation of chlorinated organic compounds. PMID:3816720

  3. TTI-237: a novel microtubule-active compound with in vivo antitumor activity.

    PubMed

    Beyer, Carl F; Zhang, Nan; Hernandez, Richard; Vitale, Danielle; Lucas, Judy; Nguyen, Thai; Discafani, Carolyn; Ayral-Kaloustian, Semiramis; Gibbons, James J

    2008-04-01

    5-Chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-N-[(1S)-2,2,2-trifluoro-1-methylethyl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine butanedioate (TTI-237) is a microtubule-active compound of novel structure and function. Structurally, it is one of a class of compounds, triazolo[1,5a]pyrimidines, previously not known to bind to tubulin. Functionally, TTI-237 inhibited the binding of [(3)H]vinblastine to tubulin, but it caused a marked increase in turbidity development that more closely resembled the effect observed with docetaxel than that observed with vincristine. The morphologic character of the presumptive polymer is unknown at present. When applied to cultured human tumor cells at concentrations near its IC(50) value for cytotoxicity (34 nmol/L), TTI-237 induced multiple spindle poles and multinuclear cells, as did paclitaxel, but not vincristine or colchicine. Flow cytometry experiments revealed that, at low concentrations (20-40 nmol/L), TTI-237 produced sub-G(1) nuclei and, at concentrations above 50 nmol/L, it caused a strong G(2)-M block. The compound was a weak substrate of multidrug resistance 1 (multidrug resistance transporter or P-glycoprotein). In a cell line expressing a high level of P-glycoprotein, the IC(50) of TTI-237 increased 25-fold whereas those of paclitaxel and vincristine increased 806-fold and 925-fold, respectively. TTI-237 was not recognized by the MRP or MXR transporters. TTI-237 was active in vivo in several nude mouse xenograft models of human cancer, including LoVo human colon carcinoma and U87-MG human glioblastoma, when dosed i.v. or p.o. Thus, TTI-237 has a set of properties that distinguish it from other classes of microtubule-active compounds.

  4. Screening Active Compounds from Garcinia Species Native to China Reveals Novel Compounds Targeting the STAT/JAK Signaling Pathway

    PubMed Central

    Xu, Linfeng; Lao, Yuanzhi; Zhao, Yanhui; Qin, Jian; Fu, Wenwei; Zhang, Yingjia; Xu, Hongxi

    2015-01-01

    Natural compounds from medicinal plants are important resources for drug development. In a panel of human tumor cells, we screened a library of the natural products from Garcinia species which have anticancer potential to identify new potential therapeutic leads and discovered that caged xanthones were highly effective at suppressing multiple cancer cell lines. Their anticancer activities mainly depended on apoptosis pathways. For compounds in sensitive cancer line, their mechanisms of mode of action were evaluated. 33-Hydroxyepigambogic acid and 35-hydroxyepigambogic acid exhibited about 1 μM IC50 values against JAK2/JAK3 kinases and less than 1 μM IC50 values against NCI-H1650 cell which autocrined IL-6. Thus these two compounds provided a new antitumor molecular scaffold. Our report describes 33-hydroxyepigambogic acid and 35-hydroxyepigambogic acid that inhibited NCI-H1650 cell growth by suppressing constitutive STAT3 activation via direct inhibition of JAK kinase activity. PMID:26090459

  5. Design of an activity landscape view taking compound-based feature probabilities into account.

    PubMed

    Zhang, Bijun; Vogt, Martin; Bajorath, Jürgen

    2014-09-01

    Activity landscapes (ALs) of compound data sets are rationalized as graphical representations that integrate similarity and potency relationships between active compounds. ALs enable the visualization of structure-activity relationship (SAR) information and are thus computational tools of interest for medicinal chemistry. For AL generation, similarity and potency relationships are typically evaluated in a pairwise manner and major AL features are assessed at the level of compound pairs. In this study, we add a conditional probability formalism to AL design that makes it possible to quantify the probability of individual compounds to contribute to characteristic AL features. Making this information graphically accessible in a molecular network-based AL representation is shown to further increase AL information content and helps to quickly focus on SAR-informative compound subsets. This feature probability-based AL variant extends the current spectrum of AL representations for medicinal chemistry applications.

  6. Characterization of aroma-active compounds in raw and cooked pine-mushrooms (Tricholoma matsutake Sing.).

    PubMed

    Cho, In Hee; Kim, Se Young; Choi, Hyung-Kyoon; Kim, Young-Suk

    2006-08-23

    The characteristic aroma-active compounds in raw and cooked pine-mushrooms (Tricholoma matsutake Sing.) were investigated by gas chromatography-olfactometry using aroma extract dilution analysis. 1-Octen-3-one (mushroom-like) was the major aroma-active compound in raw pine-mushrooms; this compound had the highest flavor dilution factor, followed by ethyl 2-methylbutyrate (floral and sweet), linalool (citrus-like), methional (boiled potato-like), 3-octanol (mushroom-like and buttery), 1-octen-3-ol (mushroom-like), (E)-2-octen-1-ol (mushroom-like), and 3-octanone (mushroom-like and buttery). By contrast, methional, 2-acetylthiazole (roasted), an unknown compound (chocolate-like), 3-hydroxy-2-butanone (buttery), and phenylacetaldehyde (floral and sweet), which could be formed by diverse thermal reactions during the cooking process, together with C8 compounds, were identified as the major aroma-active compounds in cooked pine-mushrooms.

  7. Antioxidant and Anti-Osteoporotic Activities of Aromatic Compounds and Sterols from Hericium erinaceum.

    PubMed

    Li, Wei; Lee, Sang Hyun; Jang, Hae Dong; Ma, Jin Yeul; Kim, Young Ho

    2017-01-11

    Hericium erinaceum , commonly called lion's mane mushroom, is a traditional edible mushroom widely used in culinary applications and herbal medicines in East Asian countries. In this study, a new sterol, cerevisterol 6-cinnamate ( 6 ), was isolated from the fruiting bodies of H. erinaceum together with five aromatic compounds 1 - 5 and five sterols 7 - 11 . The chemical structures of these compounds were elucidated using chemical and physical methods and comparison of HRESIMS, ¹D-NMR (¹H, 13 C, and DEPT) and 2D-NMR (COSY, HMQC, HMBC, and NOESY) spectra with previously reported data. The antioxidant and anti-osteoporotic activities of extracts and the isolated compounds 1 - 11 were investigated. All compounds exhibited peroxyl radical-scavenging capacity but only compounds 1 , 3 , and 4 showed potent reducing capacity. Moreover, compounds 1 , 2 , 4 , and 5 showed moderate effects on cellular antioxidant activity and inhibited the receptor activator of nuclear factor κB ligand (RANKL)-induced osteoclastic differentiation. These results suggested that H. erinaceum could be utilized in the development of natural antioxidant and anti-osteoporotic nutraceuticals and functional foods.

  8. Molecular modeling and snake venom phospholipase A2 inhibition by phenolic compounds: Structure-activity relationship.

    PubMed

    Alam, Md Iqbal; Alam, Mohammed A; Alam, Ozair; Nargotra, Amit; Taneja, Subhash Chandra; Koul, Surrinder

    2016-05-23

    In our earlier study, we have reported that a phenolic compound 2-hydroxy-4-methoxybenzaldehyde from Janakia arayalpatra root extract was active against Viper and Cobra envenomations. Based on the structure of this natural product, libraries of synthetic structurally variant phenolic compounds were studied through molecular docking on the venom protein. To validate the activity of eight selected compounds, we have tested them in in vivo and in vitro models. The compound 21 (2-hydroxy-3-methoxy benzaldehyde), 22 (2-hydroxy-4-methoxybenzaldehyde) and 35 (2-hydroxy-3-methoxybenzylalcohol) were found to be active against venom-induced pathophysiological changes. The compounds 20, 15 and 35 displayed maximum anti-hemorrhagic, anti-lethal and PLA2 inhibitory activity respectively. In terms of SAR, the presence of a formyl group in conjunction with a phenolic group was seen as a significant contributor towards increasing the antivenom activity. The above observations confirmed the anti-venom activity of the phenolic compounds which needs to be further investigated for the development of new anti-snake venom leads. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  9. Adsorption of aromatic compounds from the biodegradation of azo dyes on activated carbon

    NASA Astrophysics Data System (ADS)

    Faria, P. C. C.; Órfão, J. J. M.; Figueiredo, J. L.; Pereira, M. F. R.

    2008-03-01

    The adsorption of three selected aromatic compounds (aniline, sulfanilic acid and benzenesulfonic acid) on activated carbons with different surface chemical properties was investigated at different solution pH. A fairly basic commercial activated carbon was modified by means of chemical treatment with HNO 3, yielding an acid activated carbon. The textural properties of this sample were not significantly changed after the oxidation treatment. Equilibrium isotherms of the selected compounds on the mentioned samples were obtained and the results were discussed in relation to their surface chemistry. The influence of electrostatic and dispersive interactions involved in the uptake of the compounds studied was evaluated. The Freundlich model was used to fit the experimental data. Higher uptakes are attained when the compounds are present in their molecular form. In general, adsorption was disfavoured by the introduction of oxygen-containing groups on the surface of the activated carbon.

  10. In vitro antimicrobial activity of extracts and isolated compound from Dalbergia stipulacea Roxb. leaves

    NASA Astrophysics Data System (ADS)

    Kumar, Arvind; Bhat, Tahir Ahmad; Singh, Rattan Deep

    2017-07-01

    The study was designed to examine the in vitro antimicrobial efficacy of extracts and isolated compound of Dalbergia stipulacea. Combined extracts (chloroform and methanol) of plant leaves fractionated with n-butanol loaded with column afforded a flavonoid glycoside compound identified as luteolin 4'-rutinoside. Different extracts and isolated compound exhibited pronounced antibacterial and antifungal varied activities against four bacteria (Clostridium acetobutylinium, Bacillus subtilis, Streptococcus mutans, and Pseudomonas sp.) and one fungus (Candida albicans) susceptibility were determined using disc diffusion method. The minimum inhibitory concentration (MIC) of extracts and isolated compounds was determined by broth dilution method. The maximum activity was shown by chloroform extract against C. albicans with a zone of inhibition of 17 mm and minimum activity was displayed by methanolic extract against Pseudomonas sp. with 5 mm. However, isolated compound has shown maximum activity against Pseudomonas sp. with 15 mm. The MIC values higher in methanol extract against Pseudomonas sp. and isolated compound shows good against Pseudomonas sp. and B. subtilis. Our findings indicate that plant could be used as a good antimicrobial agent in food, pharmaceutical and bio-pesticide industries.

  11. The influence of interactions among phenolic compounds on the antiradical activity of chokeberries (Aronia melanocarpa).

    PubMed

    Jakobek, Lidija; Seruga, Marijan; Krivak, Petra

    2011-06-01

    In the present work, interactions between phenolic compounds from chokeberries and their influence on the antiradical activity was studied. Three fractions were isolated from chokeberries containing different classes of phenolic compounds. The first fraction contained a major part of phenolic acids and flavonols, the second anthocyanins, and the third insoluble phenols and proanthocyanidins. The phenolic compound content was determined using high-performance liquid chromatography, and the antiradical activity using the DPPH test. In order to evaluate the effects of interactions between phenolic compounds on the antiradical activity, the antiradical activity of individual phenolic fractions was compared with that obtained by mixing phenolic fractions. Phenolic mixtures showed the decrease in the antiradical activity in comparison with the individual phenolic fractions. These results suggest the existence of complex interactions among phenolic compounds that caused the decrease of the antiradical activity. Interactions among chokeberry phenols promoted a negative synergism.

  12. Antibacterial assay-guided isolation of active compounds from Artocarpus heterophyllus heartwoods.

    PubMed

    Septama, Abdi Wira; Panichayupakaranant, Pharkphoom

    2015-01-01

    Preparations from Artocarpus heterophyllus Lam. (Moraceae) heartwoods are used in the traditional folk medicine for the treatment of inflammation, malarial fever, and to prevent bacterial and fungal infections. The objective of this study was to isolate pure antibacterial compounds from A. heterophyllus heartwoods. The dried and powdered A. heterophyllus heartwoods were successively extracted with the following solvents: hexane, ethyl acetate, and methanol. Each of the extracts was screened for their antibacterial activities using a disc diffusion method (10 mg/disc). Their minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined using a broth microdilution method. The extract that showed the strongest antibacterial activities was fractionated to isolate the active compounds by an antibacterial assay-guided isolation process. The ethyl acetate extract exhibited the strongest antibacterial activities against Streptococcus mutans, S. pyogenes, and Bacillus subtilis with MIC values of 78, 39, and 9.8 µg/mL, respectively. Based on an antibacterial assay-guided isolation, four antibacterial compounds: cycloartocarpin (1), artocarpin (2), artocarpanone (3), and cyanomaclurin (4) were purified. Among these isolated compounds, artocarpin exhibited the strongest antibacterial activity against Gram-positive bacteria, including S. mutans, S. pyogenes, B. subtilis, Staphylococcus aureus, and S. epidermidis with MICs of 4.4, 4.4, 17.8, 8.9, and 8.9 µM, respectively, and MBCs of 8.9, 8.9, 17.8, 8.9, and 8.9 µM, respectively, while artocarpanone showed the strongest activity against Escherichia coli, a Gram-negative bacteria with MIC and MBC values of 12.9 and 25.8 µM, respectively. Only artocarpin showed inhibitory activity against Pseudomonas aeruginosa with an MIC of 286.4 µM.

  13. Porritoxins, metabolites of Alternaria porri, as anti-tumor-promoting active compounds.

    PubMed

    Horiuchi, Masayuki; Tokuda, Harukuni; Ohnishi, Keiichiro; Yamashita, Masakazu; Nishino, Hoyoku; Maoka, Takashi

    2006-02-01

    To search for possible cancer chemopreventive agents from natural sources, we performed primary screening of metabolites of Alternaria porri by examining their possible inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. The ethyl acetate extract of A. porri showed the inhibitory effect on EBV-EA activation. Three porritoxins (1-3) were obtained as inhibitory active compounds for EBV-EA from ethyl acetate extract. 6-(3',3'-Dimethylallyloxy)-4-methoxy-5-methylphthalide (2) showed the strongest activity among them. Inhibitory effect of porritoxin (1) and (2) was superior to that of beta-carotene, a well-known anti-tumor promoter. Furthermore, the structure-activity correlation of porritoxins and their related compounds were discussed.

  14. Effect of vanadium compounds on acid phosphatase activity.

    PubMed

    Vescina, C M; Sálice, V C; Cortizo, A M; Etcheverry, S B

    1996-01-01

    The direct effect of different vanadium compounds on acid phosphatase (ACP) activity was investigated. Vanadate and vanadyl but not pervanadate inhibited the wheat germ ACP activity. These vanadium derivatives did not alter the fibroblast Swiss 3T3 soluble fraction ACP activity. Using inhibitors of tyrosine phosphatases (PTPases), the wheat germ ACP was partially characterized as a PTPase. This study suggests that the inhibitory ability of different vanadium derivatives to modulate ACP activity seems to depend on the geometry around the vanadium atom more than on the oxidation state. Our results indicate a correlation between the PTPase activity and the sensitivity to vanadate and vanadyl cation.

  15. Antimicrobial active herbal compounds against Acinetobacter baumannii and other pathogens.

    PubMed

    Tiwari, Vishvanath; Roy, Ranita; Tiwari, Monalisa

    2015-01-01

    Bacterial pathogens cause a number of lethal diseases. Opportunistic bacterial pathogens grouped into ESKAPE pathogens that are linked to the high degree of morbidity, mortality and increased costs as described by Infectious Disease Society of America. Acinetobacter baumannii is one of the ESKAPE pathogens which cause respiratory infection, pneumonia and urinary tract infections. The prevalence of this pathogen increases gradually in the clinical setup where it can grow on artificial surfaces, utilize ethanol as a carbon source and resists desiccation. Carbapenems, a β-lactam, are the most commonly prescribed drugs against A. baumannii. The high level of acquired and intrinsic carbapenem resistance mechanisms acquired by these bacteria makes their eradication difficult. The pharmaceutical industry has no solution to this problem. Hence, it is an urgent requirement to find a suitable alternative to carbapenem, a commonly prescribed drug for Acinetobacter infection. In order to do this, here we have made an effort to review the active compounds of plants that have potent antibacterial activity against many bacteria including carbapenem resistant strain of A. baumannii. We have also briefly highlighted the separation and identification methods used for these active compounds. This review will help researchers involved in the screening of herbal active compounds that might act as a replacement for carbapenem.

  16. A ranking method for the concurrent learning of compounds with various activity profiles.

    PubMed

    Dörr, Alexander; Rosenbaum, Lars; Zell, Andreas

    2015-01-01

    In this study, we present a SVM-based ranking algorithm for the concurrent learning of compounds with different activity profiles and their varying prioritization. To this end, a specific labeling of each compound was elaborated in order to infer virtual screening models against multiple targets. We compared the method with several state-of-the-art SVM classification techniques that are capable of inferring multi-target screening models on three chemical data sets (cytochrome P450s, dehydrogenases, and a trypsin-like protease data set) containing three different biological targets each. The experiments show that ranking-based algorithms show an increased performance for single- and multi-target virtual screening. Moreover, compounds that do not completely fulfill the desired activity profile are still ranked higher than decoys or compounds with an entirely undesired profile, compared to other multi-target SVM methods. SVM-based ranking methods constitute a valuable approach for virtual screening in multi-target drug design. The utilization of such methods is most helpful when dealing with compounds with various activity profiles and the finding of many ligands with an already perfectly matching activity profile is not to be expected.

  17. Quantum chemical and statistical study of megazol-derived compounds with trypanocidal activity

    NASA Astrophysics Data System (ADS)

    Rosselli, F. P.; Albuquerque, C. N.; da Silva, A. B. F.

    In this work we performed a structure-activity relationship (SAR) study with the aim to correlate molecular properties of the megazol compound and 10 of its analogs with the biological activity against Trypanosoma cruzi (trypanocidal or antichagasic activity) presented by these molecules. The biological activity indication was obtained from in vitro tests and the molecular properties (variables or descriptors) were obtained from the optimized chemical structures by using the PM3 semiempirical method. It was calculated ˜80 molecular properties selected among steric, constitutional, electronic, and lipophilicity properties. In order to reduce dimensionality and investigate which subset of variables (descriptors) would be more effective in classifying the compounds studied, according to their degree of trypanocidal activity, we employed statistical methodologies (pattern recognition and classification techniques) such as principal component analysis (PCA), hierarchical cluster analysis (HCA), K-nearest neighbor (KNN), and discriminant function analysis (DFA). These methods showed that the descriptors molecular mass (MM), energy of the second lowest unoccupied molecular orbital (LUMO+1), charge on the first nitrogen at substituent 2 (qN'), dihedral angles (D1 and D2), bond length between atom C4 and its substituent (L4), Moriguchi octanol-partition coefficient (MLogP), and length-to-breadth ratio (L/Bw) were the variables responsible for the separation between active and inactive compounds against T. cruzi. Afterwards, the PCA, KNN, and DFA models built in this work were used to perform trypanocidal activity predictions for eight new megazol analog compounds.

  18. Antibacterial, anti-inflammatory and anti-oxidatant activities of various isolated compounds from Cratoxylum species.

    PubMed

    Rodanant, Pirasut; Boonnak, Nawong; Surarit, Rudee; Kuvatanasuchati, Jintakorn; Lertsooksawat, Wannee

    2017-05-01

    The objective of this study was to investigate the bioactivity of twenty-nine known isolated compounds from Cratoxylum species including three anthraquinones, four triterpenes, and twenty-two xanthones. All isolated compounds were subjected to antibacterial, anti-inflammatory and anti-oxidant activities. Cytotoxicity evaluations were performed by MTT assay. The anti-oxidatant activity was performed using DPPH assay. The anti-inflammatory activity was evaluated from the production of cytokines TNF-α and IL1-β using ELISA assay. Human gingival fibroblasts and monocytes could tolerate both anthraquinones and triterpenes. All isolated anthraquinones showed moderate-to-high antibacterial efficacy while compound A3 also demonstrated moderate anti-inflammatory effect. None of the isolated triterpenes, except for T1, inhibited the expression of TNF-α. A number of isolated xanthones was toxic to HGFs and monocytes. Compound X5, X14 and a 1:1 mixture of X5 and X6 showed comparative anti-inflammatory activity to dexamethasone. Several triterpene and xanthone compounds also expressed antibacterial effect against P. gingivalis. Some isolated xanthones exerted anti-oxidant activity comparable to ascorbic acid. Accordingly, selected pure compounds from plants of Cratoxylum genus might be of benefit in developing medications that are important in treating periodontal diseases.

  19. The Antimicrobial Activity of Annona emarginata (Schltdl.) H. Rainer and Most Active Isolated Compounds against Clinically Important Bacteria.

    PubMed

    Dolab, Juan G; Lima, Beatriz; Spaczynska, Ewelina; Kos, Jiri; Cano, Natividad H; Feresin, Gabriela; Tapia, Alejandro; Garibotto, Francisco; Petenatti, Elisa; Olivella, Monica; Musiol, Robert; Jampilek, Josef; Enriz, Ricardo D

    2018-05-16

    Annona emarginata (Schltdl.) H. Rainer, commonly known as "arachichú", "araticú", "aratigú", and "yerba mora", is a plant that grows in Argentina. Infusions and decoctions are used in folk medicine as a gargle against throat pain and for calming toothache; another way to use the plant for these purposes is chewing its leaves. Extracts from bark, flowers, leaves, and fruits from A. emarginata were subjected to antibacterial assays against a panel of Gram (+) and Gram (-) pathogenic bacteria according to Clinical and Laboratory Standards Institute protocols. Extracts from the stem bark and leaves showed moderate activity against the bacteria tested with values between 250⁻1000 µg/mL. Regarding flower extracts, less polar extracts (hexane, dichloromethane) showed very strong antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 and methicillin-resistant S. aureus ATCC 43300 with values between 16⁻125 µg/mL. Additionally, hexane extract showed activity against Klebsiella pneumoniae (MIC = 250 µg/mL). The global methanolic extract of the fruits (MeOHGEF) was also active against the three strains mentioned above, with MICs values 250⁻500 µg/mL. Bioassay-guided fractionation of MeOHGEF led to the isolation of a new main compound-( R )-2-(4-methylcyclohex-3-en-1-yl)propan-2-yl ( E )-3-(4-hydroxyphenyl)acrylate ( 1 ). The structure and relative configurations have been determined by means of 1D and 2D NMR techniques, including COSY, HMQC, HMBC, and NOESY correlations. Compound 1 showed strong antimicrobial activity against all Gram (+) species tested (MICs = 3.12⁻6.25 µg/mL). In addition, the synthesis and antibacterial activity of some compounds structurally related to compound 1 (including four new compounds) are reported. A SAR study for these compounds was performed based on the results obtained by using molecular calculations.

  20. Anti-trypanosomal activities and structural chemical properties of selected compound classes.

    PubMed

    Ponte-Sucre, Alicia; Bruhn, Heike; Schirmeister, Tanja; Cecil, Alexander; Albert, Christian R; Buechold, Christian; Tischer, Maximilian; Schlesinger, Susanne; Goebel, Tim; Fuß, Antje; Mathein, Daniela; Merget, Benjamin; Sotriffer, Christoph A; Stich, August; Krohne, Georg; Engstler, Markus; Bringmann, Gerhard; Holzgrabe, Ulrike

    2015-02-01

    Potent compounds do not necessarily make the best drugs in the market. Consequently, with the aim to describe tools that may be fundamental for refining the screening of candidates for animal and preclinical studies and further development, molecules of different structural classes synthesized within the frame of a broad screening platform were evaluated for their trypanocidal activities, cytotoxicities against murine macrophages J774.1 and selectivity indices, as well as for their ligand efficiencies and structural chemical properties. To advance into their modes of action, we also describe the morphological and ultrastructural changes exerted by selected members of each compound class on the parasite Trypanosoma brucei. Our data suggest that the potential organelles targeted are either the flagellar pocket (compound 77, N-Arylpyridinium salt; 15, amino acid derivative with piperazine moieties), the endoplasmic reticulum membrane systems (37, bisquaternary bisnaphthalimide; 77, N-Arylpyridinium salt; 68, piperidine derivative), or mitochondria and kinetoplasts (88, N-Arylpyridinium salt; 68, piperidine derivative). Amino acid derivatives with fumaric acid and piperazine moieties (4, 15) weakly inhibiting cysteine proteases seem to preferentially target acidic compartments. Our results suggest that ligand efficiency indices may be helpful to learn about the relationship between potency and chemical characteristics of the compounds. Interestingly, the correlations found between the physico-chemical parameters of the selected compounds and those of commercial molecules that target specific organelles indicate that our rationale might be helpful to drive compound design toward high activities and acceptable pharmacokinetic properties for all compound families.

  1. Quinolone Amides as Antitrypanosomal Lead Compounds with In Vivo Activity.

    PubMed

    Hiltensperger, Georg; Hecht, Nina; Kaiser, Marcel; Rybak, Jens-Christoph; Hoerst, Alexander; Dannenbauer, Nicole; Müller-Buschbaum, Klaus; Bruhn, Heike; Esch, Harald; Lehmann, Leane; Meinel, Lorenz; Holzgrabe, Ulrike

    2016-08-01

    Human African trypanosomiasis (HAT) is a major tropical disease for which few drugs for treatment are available, driving the need for novel active compounds. Recently, morpholino-substituted benzyl amides of the fluoroquinolone-type antibiotics were identified to be compounds highly active against Trypanosoma brucei brucei Since the lead compound GHQ168 was challenged by poor water solubility in previous trials, the aim of this study was to introduce structural variations to GHQ168 as well as to formulate GHQ168 with the ultimate goal to increase its aqueous solubility while maintaining its in vitro antitrypanosomal activity. The pharmacokinetic parameters of spray-dried GHQ168 and the newly synthesized compounds GHQ242 and GHQ243 in mice were characterized by elimination half-lives ranging from 1.5 to 3.5 h after intraperitoneal administration (4 mice/compound), moderate to strong human serum albumin binding for GHQ168 (80%) and GHQ243 (45%), and very high human serum albumin binding (>99%) for GHQ242. For the lead compound, GHQ168, the apparent clearance was 112 ml/h and the apparent volume of distribution was 14 liters/kg of body weight (BW). Mice infected with T. b. rhodesiense (STIB900) were treated in a stringent study scheme (2 daily applications between days 3 and 6 postinfection). Exposure to spray-dried GHQ168 in contrast to the control treatment resulted in mean survival durations of 17 versus 9 days, respectively, a difference that was statistically significant. Results that were statistically insignificantly different were obtained between the control and the GHQ242 and GHQ243 treatments. Therefore, GHQ168 was further profiled in an early-treatment scheme (2 daily applications at days 1 to 4 postinfection), and the results were compared with those obtained with a control treatment. The result was statistically significant mean survival times exceeding 32 days (end of the observation period) versus 7 days for the GHQ168 and control treatments

  2. Synthesis of novel fluorinated chalcones derived from 4‧-morpholinoacetophenone and their antiproliferative effects

    NASA Astrophysics Data System (ADS)

    Kurşun Aktar, Bedriye Seda; Oruç-Emre, Emine Elçin; Demirtaş, Ibrahim; Yaglioglu, Ayse Sahin; Guler, Caglar; Adem, Sevki; Karaküçük Iyidoğan, Ayşegül

    2017-12-01

    The fluorinated chalcones were synthesized by Claisen-Schmidt condensation between 4‧-morpholineacetophenone and various fluorinated benzaldehydes in the presence of NaOH in methanol. The synthesized compounds [1-7] were evaluated their antiproliferative activity against HeLa and C6 cell lines. Among them, compounds 4 and 5 were determined to have anticancer activity against HeLa cells line (IC50 values of 7.74 and 6.10 μg/mL, respectively). The anticancer activity results were shown that compounds 3, and 6 had inhibitory against C6 cells (IC50 values of 12.80 and 4.16 μg/mL, respectively). The compounds 1 and 2 had high antiproliferative activity with non-cytotoxicity. All of the new compounds, except for compound 4 showed inhibition against the human isozyme hCA I with IC50 in the range of 0.5-1,16 mM. Pyruvate kinase M2 (PKM2) was effectively inhibited by compound 4 with IC50 = 26 μM.

  3. Anti-inflammatory activities of compounds from twigs of Morus alba.

    PubMed

    Tran, Huynh Nguyen Khanh; Nguyen, Van Thu; Kim, Jeong Ah; Rho, Seong Soo; Woo, Mi Hee; Choi, Jae Sui; Lee, Jeong-Hyung; Min, Byung Sun

    2017-07-01

    Five new compounds, 10-oxomornigrol F (1), (7″R)-(-)-6-(7″-hydroxy-3″,8″-dimethyl-2″,8″-octadien-1″-yl)apigenin (2), ramumorin A (3), ramumorin B (4), and (4S,7S,8R)-trihydroxyoctadeca-5Z-enoic acid (5), together with 31 known compounds (6-36), were isolated from the twigs of Morus alba (Moraceae). The chemical structures of these compounds were established using spectroscopic analyses, 1D and 2D NMR, high-resolution electrospray ionization mass spectrometry (HRESIMS), and Mosher's methods. The anti-inflammatory activities of the compounds were evaluated by investigating their ability to inhibit lipopolysaccharide (LPS)-induced nitric oxide (NO) production in macrophage RAW 264.7 cells. Compounds 1, 2, 13, 17, 19, 25-28, and 32 showed inhibitory effects with IC 50 values ranging from 2.2 to 5.3μg/mL. Compounds 1, 2, 17, 25, and 32 reduced LPS-induced inducible nitric oxide synthase (iNOS) expression in a concentration-dependent manner. In addition, pretreating the cells with compound 1, 17, and 32 significantly suppressed LPS-induced expression of cyclooxygenase-2 (COX-2) protein. Copyright © 2017. Published by Elsevier B.V.

  4. Antioxidative and melanogenesis-inhibitory activities of caffeoylquinic acids and other compounds from moxa.

    PubMed

    Akihisa, Toshihiro; Kawashima, Kohta; Orido, Masashi; Akazawa, Hiroyuki; Matsumoto, Masahiro; Yamamoto, Ayako; Ogihara, Eri; Fukatsu, Makoto; Tokuda, Harukuni; Fuji, Jizaemon

    2013-03-01

    The MeOH extract of moxa, the processed leaves of Artemisia princeps PAMP. (Asteraceae), exhibited potent 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activity and melanogenesis-inhibitory activity in α-melanocyte-stimulating hormone (α-MSH)-stimulated B16 melanoma cells. Eight caffeoylquinic acids, 1 and 6-12, five flavonoids, 13-17, two benzoic acid derivatives, 18 and 19, three coumarin derivatives, 20-22, four steroids, 23-26, and six triterpenoids, 27-32, were isolated from the MeOH extract. Upon evaluation of compounds 1, 6-23, and four semisynthetic caffeoylquinic acid esters, 2-5, for their DPPH radical-scavenging activity, 15 compounds, 1-13, 17, and 19, showed potent activities (IC(50) 3.1-16.8 μM). The 15 compounds exhibited, moreover, potent inhibitory activities (51.1-92.5% inhibition) against peroxidation of linoleic acid emulsion at 10 μg/ml concentration. In addition, when 27 compounds, 1-8, 10, 12, 13, 15-18, 20-25, and 27-32, were evaluated for their inhibitory activity against melanogenesis in α-MSH-stimulated B16 melanoma cells, five caffeoylquinic acids, i.e., chlorogenic acid (1), ethyl chlorogenate (3), propyl chlorogenate (4), isopropyl chlorogenate (5), and butyl chlorogenate (6), along with homoorientin (17) and vanillic acid (18), exhibited inhibitory activities with 33-62% reduction of melanin content at 100 μM concentration with no or almost no toxicity to the cells (89-114% of cell viability at 100 μM). Western blot analysis showed that compound 6 reduced the protein levels of microphtalmia-associated transcription factor (MITF), tyrosinase, tyrosine-related protein 1 (TRP-1), and TRP-2 mostly in a concentration-dependent manner, suggesting that this compound inhibits melanogenesis on α-MSH-stimulated B16 melanoma cells by, at least in part, inhibiting the expression of MITF, followed by decreasing the expression of tyrosinase, TRP-1, and TRP-2. Furthermore, four compounds, 13, 15, 16, and 30, exhibited

  5. Systematic assessment of scaffold hopping versus activity cliff formation across bioactive compound classes following a molecular hierarchy.

    PubMed

    Stumpfe, Dagmar; Dimova, Dilyana; Bajorath, Jürgen

    2015-07-01

    Scaffold hopping and activity cliff formation define opposite ends of the activity landscape feature spectrum. To rationalize these events at the level of scaffolds, active compounds involved in scaffold hopping were required to contain topologically distinct scaffolds but have only limited differences in potency, whereas compounds involved in activity cliffs were required to share the same scaffold but have large differences in potency. A systematic search was carried out for compounds involved in scaffold hopping and/or activity cliff formation. Results obtained for compound data sets covering more than 300 human targets revealed clear trends. If scaffolds represented multiple but fewer than 10 active compounds, nearly 90% of all scaffolds were exclusively involved in hopping events. With increasing compound coverage, the fraction of scaffolds involved in both scaffold hopping and activity cliff formation significantly increased to more than 50%. However, ∼40% of the scaffolds representing large numbers of active compounds continued to be exclusively involved in scaffold hopping. More than 200 scaffolds with broad target coverage were identified that consistently represented potent compounds and yielded an abundance of scaffold hops in the low-nanomolar range. These and other subsets of scaffolds we characterized are of prime interest for structure-activity relationship (SAR) exploration and compound design. Therefore, the complete scaffold classification generated in the course of our analysis is made freely available. Copyright © 2015 Elsevier Ltd. All rights reserved.

  6. Identifying relationships between unrelated pharmaceutical target proteins on the basis of shared active compounds.

    PubMed

    Miljković, Filip; Kunimoto, Ryo; Bajorath, Jürgen

    2017-08-01

    Computational exploration of small-molecule-based relationships between target proteins from different families. Target annotations of drugs and other bioactive compounds were systematically analyzed on the basis of high-confidence activity data. A total of 286 novel chemical links were established between distantly related or unrelated target proteins. These relationships involved a total of 1859 bioactive compounds including 147 drugs and 141 targets. Computational analysis of large amounts of compounds and activity data has revealed unexpected relationships between diverse target proteins on the basis of compounds they share. These relationships are relevant for drug discovery efforts. Target pairs that we have identified and associated compound information are made freely available.

  7. Leishmanicidal activity of Nystatin (mycostatin): a potent polyene compound.

    PubMed

    Ali, S A; Iqbal, J; Nabeel; Khalil, Y; Manzoor, A; Bukhari, I; Ahmad, B; Yasinzai, M M

    1997-10-01

    The susceptibility of promastigote of Leishmania major to Nystatin in vitro was examined. L. major (MHOM/PK/88/DESTO) promastigote were cultured in medium 199 supplemented with 10% heat inactivated foetal bovine serum and 2% urine. The growth of the promastigote was monitored in the absence and presence of the experimental compound (Nystatin) for upto 5 days post-inoculation. The EC50 value (the concentration of drug necessary to inhibit the growth rate of cells to 50% of the control value) obtained for Nystatin against the promastigote of L. major was less than 9.76 iu ml. Certain polyene compounds like Amphotericin-B and Nystatin (mycostatin) are familiar for their fungicidal activity. Amphotericin-B is used since long as antileishmanial drug as well. Results obtained suggest that Nystatin has a very good anti leishmanial activity in vitro. The mode of action proposed for this drug is same as for Amphotericin-B as both of these polyene compounds interact with the various sterols present on the surface of the parasite, thus unusual gaps and pores are formed on the surface that results in the leakage of the ions. This leakage finally leads to the destruction of the parasite.

  8. Compound K Attenuates the Development of Atherosclerosis in ApoE−/− Mice via LXRα Activation

    PubMed Central

    Zhou, Li; Zheng, Yu; Li, Zhuoying; Bao, Lingxia; Dou, Yin; Tang, Yuan; Zhang, Jianxiang; Zhou, Jianzhi; Liu, Ya; Jia, Yi; Li, Xiaohui

    2016-01-01

    Background: Atherosclerosis is a fundamental pathological process responded to some serious cardiovascular events. Although the cholesterol-lowering drugs are widely prescribed for atherosclerosis therapy, it is still the leading cause of death in the developed world. Here we measured the effects of compound K in atherosclerosis formation and investigated the probably mechanisms of the anti-antherosclerosis roles of compound K. Methods: We treated the atherosclerotic model animals (apoE−/− mice on western diet) with compound K and measured the size of atherosclerotic lesions, inflammatory cytokine levels and serum lipid profile. Peritoneal macrophages were collected in vitro for the foam cell and inflammasome experiments. Results: Our results show that treatment with compound K dose-dependently attenuates the formation of atherosclerotic plaques by 55% through activation of reverse cholesterol transport pathway, reduction of systemic inflammatory cytokines and inhibition of local inflammasome activity. Compound K increases the cholesterol efflux of macrophage-derived foam cells, and reduces the inflammasome activity in cholesterol crystal stimulated macrophages. The activation of LXRα may contribute to the athero-protective effects of compound K. Conclusion: These observations provide evidence for an athero-protective effect of compound K via LXRα activation, and support its further evaluation as a potential effective modulator for the prevention and treatment of atherosclerosis. PMID:27399689

  9. Identification of three novel natural product compounds that activate PXR and CAR and inhibit inflammation

    PubMed Central

    Kittayaruksakul, Suticha; Zhao, Wenchen; Xu, Meishu; Ren, Songrong; Lu, Jing; Wang, Ju; Downes, Michael; Evans, Ronald M.; Venkataramanan, Raman; Chatsudthipong, Varanuj; Xie, Wen

    2013-01-01

    The pregnane X receptor (PXR) and constitutive androstane receptor (CAR) have been known to play a role in xenobiotic metabolism by regulating the expression of drug-metabolizing enzymes and transporters. In addition, PXR agonists were found to exert therapeutic effects through multiple mechanisms, such as detoxification of bile acids and inhibition of inflammation. In this study, we first investigated the effects of three natural product compounds, carapin, santonin and isokobusone, on the activity of PXR and CAR. These compounds activated both PXR and CAR in transient transfection and luciferase reporter gene assays. Mutagenesis studies showed that two amino acid residues, Phe305 of the rodent PXR and Leu308 of the human PXR, are critical for the recognition of these compounds by PXR. Importantly, the activation of PXR and CAR by these compounds induced the expression of drug-metabolizing enzymes in primary human and mouse hepatocytes. Furthermore, activation of PXR by these compounds inhibited the expression of inflammatory mediators in response to lipopolysaccharide (LPS). The effects of these natural compounds on drug metabolism and inflammation were abolished in PXR−/− hepatocytes. These natural compounds can be explored for their potential in the treatment of diseases where the PXR activation has been shown to be beneficial, such as inflammatory bowel disease, cholestasis, and hyperbilirubinemia. PMID:23896737

  10. Insights into structure and activity of natural compound inhibitors of pneumolysin

    PubMed Central

    Li, Hongen; Zhao, Xiaoran; Deng, Xuming; Wang, Jianfeng; Song, Meng; Niu, Xiaodi; Peng, Liping

    2017-01-01

    Pneumolysin is the one of the major virulence factor of the bacterium Streptococcus pneumoniae. In previous report, it is shown that β-sitosterol, a natural compound without antimicrobial activity, is a potent antagonist of pneumolysin. Here, two new pneumolysin natural compound inhibitors, with differential activity, were discovered via haemolysis assay. To explore the key factor of the conformation for the inhibition activity, the interactions between five natural compound inhibitors with differential activity and pneumolysin were reported using molecular modelling, the potential of mean force profiles. Interestingly, it is found that incorporation of the single bond (C22-C23-C24-C25) to replace the double bond (hydrocarbon sidechain) improved the anti-haemolytic activity. In view of the molecular modelling, binding of the five inhibitors to the conserved loop region (Val372, Leu460, and Tyr461) of the cholesterol binding sites led to stable complex systems, which was consistent with the result of β-sitosterol. Owing to the single bond (C22-C23-C24-C25), campesterol and brassicasterol could form strong interactions with Val372 and show higher anti-haemolytic activity, which indicated that the single bond (C22-C23-C24-C25) in inhibitors was required for the anti-haemolytic activity. Overall, the current molecular modelling work provides a starting point for the development of rational design and higher activity pneumolysin inhibitors. PMID:28165051

  11. Isolation of the active compound in Mauria heterophylla, a Peruvian plant with antibacterial activity.

    PubMed

    Mori, Tatsuya; Chang, Cecilia; Maurtua, Dora; Hammond, Gerald B

    2006-02-01

    A fraction from the ethanol extract of the Peruvian medicinal plant Mauria heterophylla (Anacardiaceae) showed antibacterial activity against Escherichia coli 35992, Staphylococcus aureus 20213 and Pseudomonas aeruginosa 15442. Further fractionation led to the isolation and characterization of ethyl gallate as the antibacterial active compound. Copyright 2006 John Wiley & Sons, Ltd.

  12. Jasmonate signaling in plant stress responses and development - active and inactive compounds.

    PubMed

    Wasternack, Claus; Strnad, Miroslav

    2016-09-25

    Jasmonates (JAs) are lipid-derived signals mediating plant responses to biotic and abiotic stresses and in plant development. Following the elucidation of each step in their biosynthesis and the important components of perception and signaling, several activators, repressors and co-repressors have been identified which contribute to fine-tuning the regulation of JA-induced gene expression. Many of the metabolic reactions in which JA participates, such as conjugation with amino acids, glucosylation, hydroxylation, carboxylation, sulfation and methylation, lead to numerous compounds with different biological activities. These metabolites may be highly active, partially active in specific processes or inactive. Hydroxylation, carboxylation and sulfation inactivate JA signaling. The precursor of JA biosynthesis, 12-oxo-phytodienoic acid (OPDA), has been identified as a JA-independent signaling compound. An increasing number of OPDA-specific processes is being identified. To conclude, the numerous JA compounds and their different modes of action allow plants to respond specifically and flexibly to alterations in the environment. Copyright © 2015 Elsevier B.V. All rights reserved.

  13. Anti-plasmodial activity of Dicoma tomentosa (Asteraceae) and identification of urospermal A-15-O-acetate as the main active compound

    PubMed Central

    2012-01-01

    Background Natural products could play an important role in the challenge to discover new anti-malarial drugs. In a previous study, Dicoma tomentosa (Asteraceae) was selected for its promising anti-plasmodial activity after a preliminary screening of several plants traditionally used in Burkina Faso to treat malaria. The aim of the present study was to further investigate the anti-plasmodial properties of this plant and to isolate the active anti-plasmodial compounds. Methods Eight crude extracts obtained from D. tomentosa whole plant were tested in vitro against two Plasmodium falciparum strains (3D7 and W2) using the p-LDH assay (colorimetric method). The Peters’ four-days suppressive test model (Plasmodium berghei-infected mice) was used to evaluate the in vivo anti-plasmodial activity. An in vitro bioguided fractionation was undertaken on a dichloromethane extract, using preparative HPLC and TLC techniques. The identity of the pure compound was assessed using UV, MS and NMR spectroscopic analysis. In vitro cytotoxicity against WI38 human fibroblasts (WST-1 assay) and haemolytic activity were also evaluated for extracts and pure compounds in order to check selectivity. Results The best in vitro anti-plasmodial results were obtained with the dichloromethane, diethylether, ethylacetate and methanol extracts, which exhibited a high activity (IC50 ≤ 5 μg/ml). Hot water and hydroethanolic extracts also showed a good activity (IC50 ≤ 15 μg/ml), which confirmed the traditional use and the promising anti-malarial potential of the plant. The activity was also confirmed in vivo for all tested extracts. However, most of the active extracts also exhibited cytotoxic activity, but no extract was found to display any haemolytic activity. The bioguided fractionation process allowed to isolate and identify a sesquiterpene lactone (urospermal A-15-O-acetate) as the major anti-plasmodial compound of the plant (IC50 < 1 μg/ml against both 3D7 and W2 strains). This was also

  14. LC-MS analysis of phenolic compounds and antioxidant activity of buckwheat at different stages of malting.

    PubMed

    Terpinc, Petra; Cigić, Blaž; Polak, Tomaž; Hribar, Janez; Požrl, Tomaž

    2016-11-01

    The impact of malting on the profile of the phenolic compounds and the antioxidant properties of two buckwheat varieties was investigated. The highest relative increases in phenolic compounds were observed for isoorientin, orientin, and isovitexin, which are consequently major inducible phenolic compounds during malting. Only a minor relative increase was observed for the most abundant phenolic compound, rutin. The radical-scavenging activity of buckwheat seeds was evaluated using ABTS and DPPH assays. A considerable increase in total phenolic compounds and higher antioxidant activity were observed after 64h of germination, whereas kilning resulted in decreased total phenolic compounds and antioxidant activity. Higher antioxidant activities for extracts were found for buffered solvents than for pure methanol and water. Changes in the composition of the phenolic compounds and increased antioxidant content were confirmed by several methods, indicating that buckwheat malt can be used as a food rich in antioxidants. Copyright © 2016 Elsevier Ltd. All rights reserved.

  15. Antifeedant compounds from three species of Apiaceae active against the field slug, Deroceras reticulatum (Muller).

    PubMed

    Birkett, Michael A; Dodds, Catherine J; Henderson, Ian F; Leake, Lucy D; Pickett, John A; Selby, Martin J; Watson, Peter

    2004-03-01

    Extracts of volatiles from foliage of three plants in the Apiaceae, Conium maculatum L. (hemlock), Coriandrum sativum L. (coriander), and Petroselinum crispum Mill. (Nym.) (parsley), previously shown to exhibit antifeedant activity in assays with the field slug, Deroceras reticulatum (Muller) (Limacidae: Pulmonata), were studied further to identify the active components. Coupled gas chromatography-mass spectrometry (GC-MS) and neurophysiological assays using tentacle nerve preparations resulted in the identification of 11 active compounds from the three extracts. Wheat flour feeding bioassays were used to determine which of these compounds had the highest antifeedant activity. One of the most active compounds was the alkaloid gamma-coniceine, from C. maculatum. The role of potentially toxic alkaloids as semiochemicals and the potential for using such compounds as crop protection agents to prevent slug feeding damage is discussed.

  16. Investigation of innovative synthesis of biologically active compounds on the basis of newly developed reactions.

    PubMed

    Honda, Toshio

    2012-01-01

    Synthesis of biologically active compounds, including natural products and pharmaceutical agents, is an important and interesting research area since the large structural diversity and complexity of bioactive compounds make them an important source of leads and scaffolds in drug discovery and development. Many structurally and also biologically interesting compounds, including marine natural products, have been isolated from nature and have also been prepared on the basis of a computational design for the purpose of developing medicinal chemistry. In order to obtain a wide variety of derivatives of biologically active compounds from the viewpoint of medicinal chemistry, it is essential to establish efficient synthetic procedures for desired targets. Newly developed reactions should also be used for efficient synthesis of desired compounds. Thus, recent progress in the synthesis of biologically active compounds by focusing on the development of new reactions is summarized in this review article.

  17. Efficient discovery of responses of proteins to compounds using active learning

    PubMed Central

    2014-01-01

    Background Drug discovery and development has been aided by high throughput screening methods that detect compound effects on a single target. However, when using focused initial screening, undesirable secondary effects are often detected late in the development process after significant investment has been made. An alternative approach would be to screen against undesired effects early in the process, but the number of possible secondary targets makes this prohibitively expensive. Results This paper describes methods for making this global approach practical by constructing predictive models for many target responses to many compounds and using them to guide experimentation. We demonstrate for the first time that by jointly modeling targets and compounds using descriptive features and using active machine learning methods, accurate models can be built by doing only a small fraction of possible experiments. The methods were evaluated by computational experiments using a dataset of 177 assays and 20,000 compounds constructed from the PubChem database. Conclusions An average of nearly 60% of all hits in the dataset were found after exploring only 3% of the experimental space which suggests that active learning can be used to enable more complete characterization of compound effects than otherwise affordable. The methods described are also likely to find widespread application outside drug discovery, such as for characterizing the effects of a large number of compounds or inhibitory RNAs on a large number of cell or tissue phenotypes. PMID:24884564

  18. Herbicidal activity of pure compound isolated from rhizosphere inhabiting Aspergillus flavus.

    PubMed

    Khattak, Saeed Ullah; Lutfullah, Ghosia; Iqbal, Zafar; Rehman, Irshad Ur; Ahmad, Jamshaid; Khan, Abid Ali

    2018-05-01

    In the quest for bioactive natural products of fungal origin, Aspergillus flavus was isolated from rhizosphere of Mentha piperita using Potato Dextrose Agar (PDA) and Czapec Yeast Broth (CYB) nutrient media for metabolites production. In total, three different metabolites were purified using HPLC/LCMS and the structures were established using 500 Varian NMR experiments. Further the isolated metabolites in different concentrations (10, 100, 1000 μg/mL) were tested for herbicidal activity using Completely Randomized design (CRD) against the seeds of Silybum marianum and Avena fatua which are major threats to wheat crop in Pakistan. Among the isolated metabolites, one compound was found active against the test weed species whose activity is reported in the present work. The chemical name of the compound is 2-(1, 4-dihydroxybutan-2-yl)-1, 3-dihydroxy-6, 8-dimethoxyanthracene-9, 10(4aH, 9aH)-dione with mass of 388. Results showed that all seeds germinated in control treatment; however, with the metabolite treated, the growth was retarded to different levels in all parts of the weeds. At a dose of 1000 μg/mL of the pure compound, 100% seeds of S. marianum and 60% seeds of A. fatua were inhibited. Interestingly, the pure compound exhibited less inhibition of 10% towards the seeds of common wheat (Triticum aestivum).

  19. Synthesis and anti-lung cancer activity of a novel arsenomolybdate compound

    NASA Astrophysics Data System (ADS)

    Zhu, Tian-Tian; Wang, Juan; Chen, Song-Hu

    2017-12-01

    The new compound based on Wells-Dawson-type arsenomolybdate: [{Cu10(pz)11Cl4}{As2IIIAs2VMo6VMo12VIO62}]·H2O (1) has been hydrothermally synthesized and characterized by single-crystal X-ray diffraction analysis, X-ray powder diffraction (XRPD), XPS spectroscopy and thermogravimetric analysis (TG). Compound 1 is consisted of two As caps Wells-dawson-type arsenomolybdate and {Cu10(py)11} complexes by chloride bridge. In addition, the antitumor effects of the title compound 1 were studied on three human lung cancer cells (A549, SK-LU-1 and SW1573). The results showed that compared with the positive reference drug carboplatin, compound 1 displayed efficient antitumor activity.

  20. Synthesis and Biological Evaluation of Ginsenoside Compound K Derivatives as a Novel Class of LXRα Activator.

    PubMed

    Huang, Yan; Liu, Hongmei; Zhang, Yingxian; Li, Jin; Wang, Chenping; Zhou, Li; Jia, Yi; Li, Xiaohui

    2017-07-24

    Compound K is one of the active metabolites of Panaxnotoginseng saponins, which could attenuate the formation of atherosclerosis in mice modelsvia activating LXRα. We synthesized and evaluated a series of ginsenoside compound K derivatives modified with short chain fatty acids. All of the structures of this class of ginsenoside compound K derivative exhibited comparable or better biological activity than ginsenoside compound K. Especially structure 1 exhibited the best potency (cholesteryl ester content: 41.51%; expression of ABCA1 mRNA: 319%) and low cytotoxicity.

  1. A novel daucosterol derivative and antibacterial activity of compounds from Arctotis arctotoides.

    PubMed

    Sultana, Nasim; Afolayan, A J

    2007-08-01

    Arctotis arctotoides is a perennial herb used medicinally for the treatment of various ailments in the Eastern Cape, South Africa. Different extracts of the plant were investigated for their antimicrobial constituents. This led to the isolation and identification of a new daucosterol derivative 3-O-[beta-D-(6'-nonadeanoate)glucopyranosyl]-beta-sitosterol and seven known compounds namely: serratagenic acid, stigmasterol, daucosterol, zaluzanin D, dehydrocostuslactone, nepetin, and pedalitin. The structures of the compounds were elucidated on the basis of spectral analysis, including homo and hetero nuclear correlation NMR experiments (COSY, NOESY, HMQC, HMBC) and mass spectra as well as by comparison with available data in the literature. The compounds exhibited antibacterial activity except stigmasterol, daucosterol and dehydrocostuslactone. Nepetin was the most active against Bacillus subtilis and Staphylococcus aureus with the minimum inhibitory concentrations of 4 microg mL( - 1) and 31 microg mL( - 1), respectively, while others exhibited moderate activity.

  2. [Study of antioxidant activity of phenolic compounds from some species of Georgian flora].

    PubMed

    Alaniia, M; Shalashvili, K; Sagareishvili, T; Kavtaradze, N; Sutiashvili, M

    2013-09-01

    The antioxidant activity of extracts obtained from different parts of Georgian flora species Hamamelis virginiana L., Astragalus caucasicus Pall., Astragalus microcephalus Willd., Vitis vinifera L., Rhododendron ponticum L., Rhododendron Ungernii Trautv., Ginkgo biloba L., Salvia officinalis L., Querqus iberica Stev., Maclura aurantiaca Nutt., Cotinus coggygria Ledeb., Fraxinus ornus L., Urtica dioica L., Rhododendron caucasicum Pall., Pueraria hirsuta Matsum., Geranium pusillum L., Astragalus Tanae Sosn., Pinus silvestris L. has been studied. Comparison with ethylentetraacetate and α-tocopherole revealed high efficacy of all extracts studied. 45 individual phenolic compounds were isolated and described by chemical examination of biologically active objects. Common sage (Salvia officinalis) extract turned out as the most active (200 %). The chemical study revealed the dominant content of condensed tannins and low molecular phenolic compounds, which may be attributed to the high antioxidant activity. Biologically active antiatherosclerotic food additive "Salbin" was developed on the basis of Common sage - Salvia officinalis L. phenolic compounds.

  3. Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment.

    PubMed

    Andrews, Katherine T; Fisher, Gillian M; Sumanadasa, Subathdrage D M; Skinner-Adams, Tina; Moeker, Janina; Lopez, Marie; Poulsen, Sally-Ann

    2013-11-15

    Despite the urgent need for effective antimalarial drugs with novel modes of action no new chemical class of antimalarial drug has been approved for use since 1996. To address this, we have used a rational approach to investigate compounds comprising the primary benzene sulfonamide fragment as a potential new antimalarial chemotype. We report the in vitro activity against Plasmodium falciparum drug sensitive (3D7) and resistant (Dd2) parasites for a panel of fourteen primary benzene sulfonamide compounds. Our findings provide a platform to support the further evaluation of primary benzene sulfonamides as a new antimalarial chemotype, including the identification of the target of these compounds in the parasite. Copyright © 2013 Elsevier Ltd. All rights reserved.

  4. In vitro plant tissue culture: means for production of biological active compounds.

    PubMed

    Espinosa-Leal, Claudia A; Puente-Garza, César A; García-Lara, Silverio

    2018-05-07

    Plant tissue culture as an important tool for the continuous production of active compounds including secondary metabolites and engineered molecules. Novel methods (gene editing, abiotic stress) can improve the technique. Humans have a long history of reliance on plants for a supply of food, shelter and, most importantly, medicine. Current-day pharmaceuticals are typically based on plant-derived metabolites, with new products being discovered constantly. Nevertheless, the consistent and uniform supply of plant pharmaceuticals has often been compromised. One alternative for the production of important plant active compounds is in vitro plant tissue culture, as it assures independence from geographical conditions by eliminating the need to rely on wild plants. Plant transformation also allows the further use of plants for the production of engineered compounds, such as vaccines and multiple pharmaceuticals. This review summarizes the important bioactive compounds currently produced by plant tissue culture and the fundamental methods and plants employed for their production.

  5. NPACT: Naturally Occurring Plant-based Anti-cancer Compound-Activity-Target database

    PubMed Central

    Mangal, Manu; Sagar, Parul; Singh, Harinder; Raghava, Gajendra P. S.; Agarwal, Subhash M.

    2013-01-01

    Plant-derived molecules have been highly valued by biomedical researchers and pharmaceutical companies for developing drugs, as they are thought to be optimized during evolution. Therefore, we have collected and compiled a central resource Naturally Occurring Plant-based Anti-cancer Compound-Activity-Target database (NPACT, http://crdd.osdd.net/raghava/npact/) that gathers the information related to experimentally validated plant-derived natural compounds exhibiting anti-cancerous activity (in vitro and in vivo), to complement the other databases. It currently contains 1574 compound entries, and each record provides information on their structure, manually curated published data on in vitro and in vivo experiments along with reference for users referral, inhibitory values (IC50/ED50/EC50/GI50), properties (physical, elemental and topological), cancer types, cell lines, protein targets, commercial suppliers and drug likeness of compounds. NPACT can easily be browsed or queried using various options, and an online similarity tool has also been made available. Further, to facilitate retrieval of existing data, each record is hyperlinked to similar databases like SuperNatural, Herbal Ingredients’ Targets, Comparative Toxicogenomics Database, PubChem and NCI-60 GI50 data. PMID:23203877

  6. The antibacterial activity of compounds isolated from oakmoss against Legionella pneumophila and other Legionella spp.

    PubMed

    Nomura, Harue; Isshiki, Yasunori; Sakuda, Keisuke; Sakuma, Katsuya; Kondo, Seiichi

    2012-01-01

    Oakmoss is a natural fragrance ingredient exhibiting highly specific, potent antibacterial activity against Legionella pneumophila, a causative agent of severe water-bone pneumonia. In the present study, the antibacterial activity of individual compounds isolated from oakmoss was investigated against L. pneumophila and other Legionella spp. A total of 18 known compounds and two minor novel compounds (i.e., 3-methoxy-5-methylphenyl-2,4-dihydroxy-6-methylbenzoate (compound 9) and 8-(2,4-dihydroxy-6-(2-oxoheptyl)-phenoxy)-6-hydroxy-3-pentyl-1H-isochromen-1-one (compound 20)) were purified from oakmoss. The minimum inhibitory concentrations (MICs) against clinical and environmental isolates of L. pneumophila, L. bozemanii, L. micdadei, L. longbeachae, and L. dumoffii for 11 of the 20 compounds were less than 100 µg/mL (range 0.8-64.0 µg/mL). Novel compounds 9 and 20 exhibited potent antibacterial activity against L. pneumophila strains (MIC ranges of 1.3-8.0 µg/mL and 3.3-13.3 µg/mL, respectively) and also against four other Legionella species (MIC ranges of 0.8-8.0 µg/mL and 3.3-21.3 µg/mL, respectively). Time-kill assays indicated that compounds 9 and 20 kill bacteria at a concentration equivalent to 2×MIC after 1 h and 6 h co-incubations, respectively. While oakmoss and the purified components exhibited antibacterial activity against Legionella spp., they were not active against other Gram-negative and -positive bacteria such as Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis and Staphylococcus aureus.

  7. Synergistic anti-Campylobacter jejuni activity of fluoroquinolone and macrolide antibiotics with phenolic compounds

    PubMed Central

    Oh, Euna; Jeon, Byeonghwa

    2015-01-01

    The increasing resistance of Campylobacter to clinically important antibiotics, such as fluoroquinolones and macrolides, is a serious public health problem. The objective of this study is to investigate synergistic anti-Campylobacter jejuni activity of fluoroquinolones and macrolides in combination with phenolic compounds. Synergistic antimicrobial activity was measured by performing a checkerboard assay with ciprofloxacin and erythromycin in the presence of 21 phenolic compounds. Membrane permeability changes in C. jejuni by phenolic compounds were determined by measuring the level of intracellular uptake of 1-N-phenylnaphthylamine (NPN). Antibiotic accumulation assays were performed to evaluate the level of ciprofloxacin accumulation in C. jejuni. Six phenolic compounds, including p-coumaric acid, sinapic acid, caffeic acid, vanillic acid, gallic acid, and taxifolin, significantly increased the susceptibility to ciprofloxacin and erythromycin in several human and poultry isolates. The synergistic antimicrobial effect was also observed in ciprofloxacin- and erythromycin-resistant C. jejuni strains. The phenolic compounds also substantially increased membrane permeability and antibiotic accumulation in C. jejuni. Interestingly, some phenolic compounds, such as gallic acid and taxifolin, significantly reduced the expression of the CmeABC multidrug efflux pump. Phenolic compounds increased the NPN accumulation in the cmeB mutant, indicating phenolic compounds may affect the membrane permeability. In this study, we successfully demonstrated that combinational treatment of C. jejuni with antibiotics and phenolic compounds synergistically inhibits C. jejuni by impacting both antimicrobial influx and efflux. PMID:26528273

  8. Bioactive compounds and antioxidant activities of some cereal milling by-products.

    PubMed

    Smuda, Sayed Saad; Mohsen, Sobhy Mohamed; Olsen, Karsten; Aly, Mohamed Hassan

    2018-03-01

    The present study was performed to evaluate the phytochemicals profiles of some cereal milling by-products such as wheat (bran, germ and shorts), rice (bran, germ and husk) and corn (bran, germ and germ meal) to assess their potentiality as bioactive compounds sources. Distilled water, ethanol, methanol, and acetone separately were used as solvents for the extraction of phytochemicals compounds. The antioxidant activity (AOA), total phenolics content (TPC), and total flavonoids content (TFC) of the extracts were investigated using various in vitro assays. The results showed that tannins content was ranged from 113.4 to 389.5 (mg/100 g sample).The study revealed that TPC and TFC of cereal by-products extracts were significantly different for various solvents. TPC content varied from 366.1 to 1924.9 mg/100 g and TFC content varied from 139.3 to 681.6 mg/100 g. High carotenoids content was observed for corn germ meal and minimum for wheat bran. Distilled water, ethanol and methanol extracts showed significantly different antioxidant activity. Significant variations were observed with regard to AOA of different cereal by-products by using various solvents. The ethanol and methanol were observed to be the best solvents to extract phenolic compounds and antioxidant activity, while acetone extract showed less efficiency. Also, the cereal milling by-products were rich in bioactive compounds and could be used as a value added products.

  9. Relationships Between Bioactive Compound Content and
the Antiplatelet and Antioxidant Activities of Six Allium Vegetable Species

    PubMed Central

    Beretta, Hebe Vanesa; Bannoud, Florencia; Insani, Marina; Berli, Federico; Hirschegger, Pablo; Galmarini, Claudio Rómulo

    2017-01-01

    Summary Allium sp. vegetables are widely consumed for their characteristic flavour. Additionally, their consumption may provide protection against cardiovascular disease due to their antiplatelet and antioxidant activities. Although antiplatelet and antioxidant activities in Allium sp. are generally recognised, comparative studies of antiplatelet and antioxidant potency among the main Allium vegetable species are lacking. Also, the relationship between organosulfur and phenolic compounds and these biological activities has not been well established. In this study, the in vitro antiplatelet and antioxidant activities of the most widely consumed Allium species are characterised and compared. The species total organosulfur and phenolic content, and the HPLC profiles of 11 phenolic compounds were characterised and used to investigate the relationship between these compounds and antiplatelet and antioxidant activities. Furthermore, antiplatelet activities in chives and shallot have been characterised for the first time. Our results revealed that the strongest antiplatelet agents were garlic and shallot, whereas chives had the highest antioxidant activity. Leek and bunching onion had the weakest both biological activities. Significantly positive correlations were found between the in vitro antiplatelet activity and total organosulfur (R=0.74) and phenolic (TP) content (R=0.73), as well as between the antioxidant activity and TP (R=0.91) and total organosulfur content (R=0.67). Six individual phenolic compounds were associated with the antioxidant activity, with catechin, epigallocatechin and epicatechin gallate having the strongest correlation values (R>0.80). Overall, our results suggest that both organosulfur and phenolic compounds contribute similarly to Allium antiplatelet activity, whereas phenolics, as a whole, are largely responsible for antioxidant activity, with broad variation observed among the contributions of individual phenolic compounds. PMID:28867958

  10. Evaluation of Biologically Active Compounds from Calendula officinalis Flowers using Spectrophotometry

    PubMed Central

    2012-01-01

    Background This study aimed to quantify the active biological compounds in C. officinalis flowers. Based on the active principles and biological properties of marigolds flowers reported in the literature, we sought to obtain and characterize the molecular composition of extracts prepared using different solvents. The antioxidant capacities of extracts were assessed by using spectrophotometry to measure both absorbance of the colorimetric free radical scavenger 2,2-diphenyl-1-picrylhydrazyl (DPPH) as well as the total antioxidant potential, using the ferric reducing power (FRAP) assay. Results Spectrophotometric assays in the ultraviolet-visible (UV-VIS) region enabled identification and characterization of the full range of phenolic and flavonoids acids, and high-performance liquid chromatography (HPLC) was used to identify and quantify phenolic compounds (depending on the method of extraction). Methanol ensured more efficient extraction of flavonoids than the other solvents tested. Antioxidant activity in methanolic extracts was correlated with the polyphenol content. Conclusions The UV-VIS spectra of assimilator pigments (e.g. chlorophylls), polyphenols and flavonoids extracted from the C. officinalis flowers consisted in quantitative evaluation of compounds which absorb to wavelengths broader than 360 nm. PMID:22540963

  11. Pulse seed germination improves antioxidative activity of phenolic compounds in stripped soybean oil-in-water emulsions.

    PubMed

    Xu, Minwei; Jin, Zhao; Peckrul, Allen; Chen, Bingcan

    2018-06-01

    The purpose of this study was to investigate antioxidative activity of phenolic compounds extracted from germinated pulse seed including chickpeas, lentils and yellow peas. Phenolic compounds were extracted at different germination time and total phenolic content was examined by Folin Ciocalteu's reaction. Antioxidative activity of extracts was characterized by in vitro assay including 2, 2-diphenyl-1-picrylhydrazyl radical scavenging capacity (DPPH), oxygen radical absorbance capacity (ORAC), iron-binding assay, and in stripped soybean oil-in-water emulsions. The results suggested that germination time is critical for phenolic compounds production. The form variation of phenolic compounds influenced the antioxidative activity of phenolic compounds both in vitro assay and in emulsion systems. Soluble bound phenolic compounds showed higher antioxidative ability in emulsion system with the order of chickpea > yellow pea > lentil. On the basis of these results, soluble bound phenolic compounds may be considered as a promising natural antioxidant to prevent lipid oxidation in foods. Copyright © 2018 Elsevier Ltd. All rights reserved.

  12. Methanobactin: a copper binding compound having antibiotic and antioxidant activity isolated from methanotrophic bacteria

    DOEpatents

    DiSpirito, Alan A [Ames, IA; Zahn, James A [Harbor Beach, MI; Graham, David W [Lawrence, KS; Kim, Hyung J [St. Paul, MN; Alterman, Michail [Lawrence, KS; Larive, Cynthia [Lawrence, KS

    2007-04-03

    A means and method for treating bacterial infection, providing antioxidant activity, and chelating copper using a copper binding compound produced by methanotrophic bacteria is described. The compound, known as methanobactin, is the first of a new class of antibiotics having gram-positive activity. Methanobactin has been sequenced, and its structural formula determined.

  13. Evaluation of the effect of germination on phenolic compounds and antioxidant activities in sorghum varieties.

    PubMed

    Dicko, Mamoudou H; Gruppen, Harry; Traore, Alfred S; van Berkel, Willem J H; Voragen, Alphons G J

    2005-04-06

    The screening of 50 sorghum varieties showed that, on average, germination did not affect the content in total phenolic compounds but decreased the content of proanthocyanidins, 3-deoxyanthocyanidins, and flavan-4-ols. Independent of germination, there are intervarietal differences in antioxidant activities among sorghum varieties. Phenolic compounds and antioxidant activities were more positively correlated in ungerminated varieties than in germinated ones. Sorghum grains with pigmented testa layer, chestnut color glumes, and red plants had higher contents, larger diversity of phenolic compounds, and higher antioxidant activities than other sorghums. Some red sorghum varieties had higher antioxidant activities (30-80 mumol of Trolox equiv/g) than several sources of natural antioxidants from plant foods. Among varieties used for "to", "dolo", couscous, and porridge preparation, the "dolo"(local beer) varieties had the highest average content and diversity in phenolic compounds as well as the highest antioxidant activities. The biochemical markers determined are useful indicators for the selection of sorghum varieties for food and agronomic properties.

  14. Antioxidant activity and phenolic compounds in organic red wine using different winemaking techniques.

    PubMed

    Mulero, Juana; Zafrilla, Pilar; Cayuela, Jose M; Martínez-Cachá, Adela; Pardo, Francisco

    2011-04-01

    Wine phenolic composition depends on the grapes used to make wine and on vinification conditions. The occurrence of these biological compounds has stimulated numerous studies focused on understanding the mechanisms that influence their concentrations in wine. This article studied the effect of different vinification techniques on the antioxidant activity and on the phenolic compounds of red wine made from the variety of Monastrell grapes obtained by organic culture. To this purpose, 3 different vinification procedures were carried out: vinification after prolonged maceration, vinification with the addition of enological enzymes, and traditional vinification procedures (used as control).The results showed similar values of antioxidant activity in all 3 types of wine elaborated and found no differences in the concentrations of the different types of phenolic compounds in wine made with the 3 different methods. The evolution of antioxidant activity and phenolic compounds tested in wines during 3 mo of storage showed a similar pattern. Organic wine has acquired an important role in the economic world and its important, working in oenology to research in this field.

  15. A Genomics-Based Approach Identifies a Thioviridamide-Like Compound with Selective Anticancer Activity.

    PubMed

    Frattaruolo, Luca; Lacret, Rodney; Cappello, Anna Rita; Truman, Andrew W

    2017-11-17

    Thioviridamide is a structurally novel ribosomally synthesized and post-translational modified peptide (RiPP) produced by Streptomyces olivoviridis NA005001. It is characterized by a structure that features a series of thioamide groups and possesses potent antiproliferative activity in cancer cell lines. Its unusual structure allied to its promise as an anticancer compound led us to investigate the diversity of thioviridamide-like pathways across sequenced bacterial genomes. We have isolated and characterized three diverse members of this family of natural products. This characterization is supported by transformation-associated recombination cloning and heterologous expression of one of these compounds, thiostreptamide S4. Our work provides an insight into the diversity of this rare class of compound and indicates that the unusual N-terminus of thioviridamide is not introduced biosynthetically but is instead introduced during acetone extraction. A detailed analysis of the biological activity of one of the newly discovered compounds, thioalbamide, indicates that it is highly cytotoxic to cancer cells, while exhibiting significantly less activity toward a noncancerous epithelial cell line.

  16. Phytochemical Analysis, Identification and Quantification of Antibacterial Active Compounds in Betel Leaves, Piper betle Methanolic Extract.

    PubMed

    Syahidah, A; Saad, C R; Hassan, M D; Rukayadi, Y; Norazian, M H; Kamarudin, M S

    2017-01-01

    The problems of bacterial diseases in aquaculture are primarily controlled by antibiotics. Medicinal plants and herbs which are seemed to be candidates of replacements for conventional antibiotics have therefore gained increasing interest. Current study was performed to investigate the presence of phytochemical constituents, antibacterial activities and composition of antibacterial active compounds in methanolic extract of local herb, Piper betle . Qualitative phytochemical analysis was firstly carried out to determine the possible active compounds in P. betle leaves methanolic extract. The antibacterial activities of major compounds from this extract against nine fish pathogenic bacteria were then assessed using TLC-bioautography agar overlay assay and their quantity were determined simultaneously by HPLC method. The use of methanol has proved to be successful in extracting numerous bioactive compounds including antibacterial compounds. The TLC-bioautography assay revealed the inhibitory action of two compounds which were identified as hydroxychavicol and eugenol. The $-caryophyllene however was totally inactive against all the tested bacterial species. In this study, the concentration of hydroxychavicol in extract was found to be 374.72±2.79 mg g-1, while eugenol was 49.67±0.16 mg g-1. Based on these findings, it could be concluded that hydroxychavicol and eugenol were the responsible compounds for the promising antibacterial activity of P. betle leaves methanolic extract. This inhibitory action has significantly correlated with the amount of the compounds in extract. Due to its potential, the extract of P. betle leaves or it compounds can be alternative source of potent natural antibacterial agents for aquaculture disease management.

  17. Bioactive compounds and antioxidant activity in scalded Jalapeño pepper industrial byproduct (Capsicum annuum).

    PubMed

    Sandoval-Castro, Claudia Jaqueline; Valdez-Morales, Maribel; Oomah, B Dave; Gutiérrez-Dorado, Roberto; Medina-Godoy, Sergio; Espinosa-Alonso, L Gabriela

    2017-06-01

    Bioactive compounds and antioxidant activity were evaluated from industrial Jalapeño pepper byproducts and simulated non processed byproducts from two Mexican states (Chihuahua and Sinaloa) to determine their value added potential as commercial food ingredients. Aqueous 80% ethanol produced about 13% of dry extract of polar compounds. Total phenolic content increased and capsaicin and dihydrocapsaicin decreased on scalding samples (80 °C, 2 min) without affecting ascorbic acid. The major phenolic compounds, rutin, epicatechin and catechin comprised 90% of the total compounds detected by HPLC of each Jalapeño pepper byproducts. ORAC analysis showed that the origin and scalding process affected the antioxidant activity which correlated strongly with capsaicin content. Although scalding decreased capsaicinoids (up to 42%), phenolic content by (up to 16%), and the antioxidant activity (variable). Jalapeño pepper byproduct is a good source of compounds with antioxidant activity, and still an attractive ingredient to develop useful innovative products with potential food/non-food applications simultaneously reducing food loss and waste.

  18. Texas Native Plants Yield Compounds with Cytotoxic Activities against Prostate Cancer Cells.

    PubMed

    Shaffer, Corena V; Cai, Shengxin; Peng, Jiangnan; Robles, Andrew J; Hartley, Rachel M; Powell, Douglas R; Du, Lin; Cichewicz, Robert H; Mooberry, Susan L

    2016-03-25

    There remains a critical need for more effective therapies for the treatment of late-stage and metastatic prostate cancers. Three Texas native plants yielded three new and three known compounds with antiproliferative and cytotoxic activities against prostate cancer cells with IC50 values in the range of 1.7-35.0 μM. A new sesquiterpene named espadalide (1), isolated from Gochnatia hypoleuca, had low micromolar potency and was highly effective in clonogenic assays. Two known bioactive germacranolides (2 and 3) were additionally isolated from G. hypoleuca. Dalea frutescens yielded two new isoprenylated chalcones, named sanjuanolide (4) and sanjoseolide (5), and the known sesquiterpenediol verbesindiol (6) was isolated from Verbesina virginica. Mechanistic studies showed that 1-4 caused G2/M accumulation and the formation of abnormal mitotic spindles. Tubulin polymerization assays revealed that 4 increased the initial rate of tubulin polymerization, but did not change total tubulin polymer levels, and 1-3 had no effects on tubulin polymerization. Despite its cytotoxic activity, compound 6 did not initiate changes in cell cycle distribution and has a mechanism of action different from the other compounds. This study demonstrates that new compounds with significant biological activities germane to unmet oncological needs can be isolated from Texas native plants.

  19. Analysis of Indonesian Spice Essential Oil Compounds That Inhibit Locomotor Activity in Mice

    PubMed Central

    Muchtaridi; Diantini, Adjeng; Subarnas, Anas

    2011-01-01

    Some fragrance components of spices used for cooking are known to have an effect on human behavior. The aim of this investigation was to examine the effect of the essential oils of basil (Ocimum formacitratum L.) leaves, lemongrass (Cymbopogon citrates L.) herbs, ki lemo (Litsea cubeba L.) bark, and laja gowah (Alpinia malaccencis Roxb.) rhizomes on locomotor activity in mice and identify the active component(s) that might be responsible for the activity. The effect of the essential oils was studied by a wheel cage method and the active compounds of the essential oils were identified by GC/MS analysis. The essential oils were administered by inhalation at doses of 0.1, 0.3, and 0.5 mL/cage. The results showed that the four essential oils had inhibitory effects on locomotor activity in mice. Inhalation of the essential oils of basil leaves, lemongrass herbs, ki lemo bark, and laja gowah rhizomes showed the highest inhibitory activity at doses of 0.5 (57.64%), 0.1 (55.72%), 0.5 (60.75%), and 0.1 mL/cage (47.09%), respectively. The major volatile compounds 1,8-cineole, α-terpineol, 4-terpineol, citronelol, citronelal, and methyl cinnamate were identified in blood plasma of mice after inhalation of the four oils. These compounds had a significant inhibitory effect on locomotion after inhalation. The volatile compounds of essential oils identified in the blood plasma may correlate with the locomotor-inhibiting properties of the oil when administered by inhalation.

  20. Cytotoxicity, antimicrobial and antioxidant activity of eight compounds isolated from Entada abyssinica (Fabaceae).

    PubMed

    Dzoyem, Jean P; Melong, Raduis; Tsamo, Armelle T; Tchinda, Alembert T; Kapche, Deccaux G W F; Ngadjui, Bonaventure T; McGaw, Lyndy J; Eloff, Jacobus N

    2017-03-06

    Entada abyssinica is a plant traditionally used against gastrointestinal bacterial infections. Eight compounds including three flavonoids, three terpenoids, a monoglyceride and a phenolic compound isolated from E. abyssinica were investigated for their cytotoxicity, antibacterial and antioxidant activity. Compounds 7 and 2 had remarkable activity against Salmonella typhimurium with the lowest respective minimum inhibitory concentration (MIC) values of 1.56 and 3.12 µg/mL. The antioxidant assay gave IC 50 values varied from 0.48 to 2.87 μg/mL in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, from 2.53 to 17.04 μg/mL in the 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) assay and from 1.43 to 103.98 µg/mL in the FRAP assay. Compounds had relatively low cytotoxicity (LC 50 values ranging from 22.42 to 80.55 µg/mL) towards Vero cells. Ursolic acid had the most potent cytotoxicity against THP-1 and RAW 264.7 cells with LC 50 values of 9.62 and 4.56 μg/mL respectively, and selectivity index values of 7.32 and 15.44 respectively. Our findings suggest that among the terpenoid and flavonoid compounds studied, entadanin (compound 7) possess tremendous antibacterial activity against S. typhimurium and could be developed for the treatment of bacterial diseases.

  1. Analysis of Phenolic Compounds and Antioxidant Activity in Wild Blackberry Fruits

    PubMed Central

    Oszmiański, Jan; Nowicka, Paulina; Teleszko, Mirosława; Wojdyło, Aneta; Cebulak, Tomasz; Oklejewicz, Krzysztof

    2015-01-01

    Twenty three different wild blackberry fruit samples were assessed regarding their phenolic profiles and contents (by LC/MS quadrupole time-of-flight (QTOF) and antioxidant activity (ferric reducing ability of plasma (FRAP) and 2,2-azinobis (3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS)) by two different extraction methods. Thirty four phenolic compounds were detected (8 anthocyanins, 15 flavonols, 3 hydroxycinnamic acids, 6 ellagic acid derivatives and 2 flavones). In samples, where pressurized liquid extraction (PLE) was used for extraction, a greater increase in yields of phenolic compounds was observed, especially in ellagic acid derivatives (max. 59%), flavonols (max. 44%) and anthocyanins (max. 29%), than after extraction by the ultrasonic technique extraction (UAE) method. The content of phenolic compounds was significantly correlated with the antioxidant activity of the analyzed samples. Principal component analysis (PCA) revealed that the PLE method was more suitable for the quantitative extraction of flavonols, while the UAE method was for hydroxycinnamic acids. PMID:26132562

  2. Herb Medicines against Osteoporosis: Active Compounds & Relevant Biological Mechanisms.

    PubMed

    Wu, Lei; Ling, Zhuoyan; Feng, Xueqin; Mao, Caiping; Xu, Zhice

    2017-01-01

    Osteoporosis is one of common bone disorders, affecting millions of people worldwide. Treatments of osteoporosis consist of pharmacotherapy and non-pharmacological interventions, such as mineral supplementation, lifestyle changes, and exercise programs. Due to the minimum side effects and favorable cost-effective therapeutic effects, herbal medicine has been widely applied in clinical practices for more than 2,000 years in China. Of the many traditional formulas reported for treating bone diseases, 4 single herbs namely (1) Herba Epimedii, (2) Rhizoma Drynariae, (3) Fructus Psoraleae, and (4) Cortex Eucommiae, are considered as the featured "Kidney-Yang" tonics, and frequently and effectively applied for preventing and treating osteoporosis. With the accruing development of modern chemistry, hundreds of active compounds have been identified and isolated for their anti-osteoporotic effects. This review would first sketch the phytochemistry of these featured "Kidney- Yang" tonics and present the pharmacological characteristics of the most abundant and bioactive compounds derived from the herb Herba Epimedii and Rhizoma Drynariae, including icariin and naringin. Then, the cellular and molecular underpinnings under anti-osteoporotic effects of icariin and naringin are discussed. The concerned structure-function relationships of the featured active herbal compounds would also be reviewed so as to pave the way for future drug design in treating osteoporosis. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  3. Four new compounds isolated from Psoralea corylifolia and their diacylglycerol acyltransferase (DGAT) inhibitory activity.

    PubMed

    Lin, Xin; Li, Ban-Ban; Zhang, Le; Li, Hao-Ze; Meng, Xiao; Jiang, Yi-Yu; Lee, Hyun-Sun; Cui, Long

    2018-05-14

    A new bakuchiol compound Δ 11 -12-hydroxy-12-dimethyl bakuchiol (1), a new flavanone compound 2(S)-6-methoxy-7- hydroxymethylene-4'-hydroxyl-flavanone (8), and two new isoflavanone compounds 4',7-dihydroxy-3'-(6"β-hydroxy-3″,7″-dimethyl-,2″,7″-dibutenyl)-geranylisoflavone (9) and 4',7-dihydroxy-3'-(7″-hydroxy-7″-methyl-2″,5″-dibutenyl)-geranylisoflavone (10) together with eight known compounds (2-7, 11, 12) were isolated from the P. corylifolia. Their structures were elucidated on the basis of spectroscopic and physico-chemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1/2. Among them, compounds 3, 9 and 10 were found to exhibit selective inhibitory activity on DGAT1 with IC 50 values ranging from 93.7 ± 1.3 to 96.2 ± 1.1 μM. Compound 1 showed inhibition activity on DGAT1 with IC 50 values 73.4 ± 1.3 μM and inhibition of DGAT2 with IC 50 value 121.1 ± 1.3 μM. Copyright © 2018 Elsevier B.V. All rights reserved.

  4. Phenolic compounds from the leaf extract of artichoke (Cynara scolymus L.) and their antimicrobial activities.

    PubMed

    Zhu, Xianfeng; Zhang, Hongxun; Lo, Raymond

    2004-12-01

    A preliminary antimicrobial disk assay of chloroform, ethyl acetate, and n-butanol extracts of artichoke (Cynara scolymus L.) leaf extracts showed that the n-butanol fraction exhibited the most significant antimicrobial activities against seven bacteria species, four yeasts, and four molds. Eight phenolic compounds were isolated from the n-butanol soluble fraction of artichoke leaf extracts. On the basis of high-performance liquid chromatography/electrospray ionization mass spectrometry, tandem mass spectrometry, and nuclear magnetic resonance techniques, the structures of the isolated compounds were determined as the four caffeoylquinic acid derivatives, chlorogenic acid (1), cynarin (2), 3,5-di-O-caffeoylquinic acid (3), and 4,5-di-O-caffeoylquinic acid (4), and the four flavonoids, luteolin-7-rutinoside (5), cynaroside (6), apigenin-7-rutinoside (7), and apigenin-7-O-beta-D-glucopyranoside (8), respectively. The isolated compounds were examined for their antimicrobial activities on the above microorganisms, indicating that all eight phenolic compounds showed activity against most of the tested organisms. Among them, chlorogenic acid, cynarin, luteolin-7-rutinoside, and cynaroside exhibited a relatively higher activity than other compounds; in addition, they were more effective against fungi than bacteria. The minimum inhibitory concentrations of these compounds were between 50 and 200 microg/mL.

  5. Natural low-molecular mass organic compounds with oxidase activity as organocatalysts.

    PubMed

    Nishiyama, Tatsuya; Hashimoto, Yoshiteru; Kusakabe, Hitoshi; Kumano, Takuto; Kobayashi, Michihiko

    2014-12-02

    Organocatalysts, low-molecular mass organic compounds composed of nonmetallic elements, are often used in organic synthesis, but there have been no reports of organocatalysts of biological origin that function in vivo. Here, we report that actinorhodin (ACT), a natural product derived from Streptomyces coelicolor A3(2), acts as a biocatalyst. We purified ACT and assayed its catalytic activity in the oxidation of L-ascorbic acid and L-cysteine as substrates by analytical methods for enzymes. Our findings were as follows: (i) oxidation reactions producing H2O2 proceeded upon addition of ACT to the reaction mixture; (ii) ACT was not consumed during the reactions; and (iii) a small amount (catalytic amount) of ACT consumed an excess amount of the substrates. Even at room temperature, atmospheric pressure, and neutral pH, ACT showed catalytic activity in aqueous solution, and ACT exhibited substrate specificity in the oxidation reactions. These findings reveal ACT to be an organocatalyst. ACT is known to show antibiotic activity, but its mechanism of action remains unknown. On the basis of our results, we propose that ACT kills bacteria by catalyzing the production of toxic levels of H2O2. We also screened various other natural products of bacterial, plant, and animal origins and found that several of the compounds exhibited catalytic activity, suggesting that living organisms produce and use these compounds as biocatalysts in nature.

  6. Evaluation of Natural Compounds for Antimicrobial Activity in the Introductory Microbiology Laboratory.

    ERIC Educational Resources Information Center

    Finer, Kim R.

    1997-01-01

    Presents an experiment that provides students with an opportunity to investigate folk medicine and herbal cures and their accompanying claims. Involves isolating some active compounds from plant materials and demonstrating their antibacterial activity. (JRH)

  7. Phenolic Compounds of Pomegranate Byproducts (Outer Skin, Mesocarp, Divider Membrane) and Their Antioxidant Activities.

    PubMed

    Ambigaipalan, Priyatharini; de Camargo, Adriano Costa; Shahidi, Fereidoon

    2016-08-31

    Pomegranate peel was separated into outer leathery skin (PS), mesocarp (PM), and divider membrane (PD), and its phenolic compounds were extracted as free (F), esterified (E), and insoluble-bound (B) forms for the first time. The total phenolic content followed the order PD > PM > PS. ABTS(•+), DPPH, and hydroxyl radical scavenging activities and metal chelation were evaluated. In addition, pomegranate peel extracts showed inhibitory effects against α-glucosidase activity, lipase activity, and cupric ion-induced LDL-cholesterol oxidation as well as peroxyl and hydroxyl radical-induced DNA scission. Seventy-nine phenolic compounds were identified using HPLC-DAD-ESI-MS(n) mainly in the form of insoluble-bound. Thirty compounds were identified for the first time. Gallic acid was the major phenolic compound in pomegranate peel, whereas kaempferol 3-O-glucoside was the major flavonoid. Moreover, ellagic acid and monogalloyl-hexoside were the major hydrolyzable tannins, whereas the dominant proanthocyanidin was procyanidin dimers. Proanthocyanidins were detected for the first time.

  8. An in vitro comparative study of the antioxidant activity and SIRT1 modulation of natural compounds.

    PubMed

    Fusi, Jonathan; Bianchi, Sara; Daniele, Simona; Pellegrini, Silvia; Martini, Claudia; Galetta, Fabio; Giovannini, Luca; Franzoni, Ferdinando

    2018-05-01

    Oxidative stress arises from an imbalance between the production of free radicals and antioxidant defences. Several studies have suggested that dietary antioxidants (such as polyphenols and berberine) may counteract oxidative stress through the involvement of the Sirtuin 1/Adenosine Monophosphate-Activated Protein Kinase (SIRT1/AMPK) pathway. The aim of this study was to evaluate the direct and specific antioxidant activity of some natural compounds, as well as their ability to modulate the expression of SIRT1 and the activation of AMPK. Quercetin, tyrosol, ferulic acid, catechin, berberine and curcumin were evaluated for their specific and direct antioxidant activity with TOSC assay. Their ability to modulate SIRT1 and AMPK was assessed by immunoblotting assay, while their cytotoxicity by CellTiter-Blue Cell Viability Assay. No statistically significant decrease (p > 0.05) in the number of viable cells was found upon challenging with the natural compounds. Quercetin exhibited the highest antioxidant activity against peroxyl radical and peroxinitrate derivates, while curcumin showed the best anti-hydroxyl activity with respect to the other compounds and, most importantly, respect to the reference antioxidants. Finally, all the tested compounds significantly increased the SIRT1 expression and the activation of AMPK. Our results clearly disclose the specific antioxidant activity of these natural compounds and their ability to increase SIRT1 expression and AMPK activation. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

  9. Acquisition of Compound Words in Chinese-English Bilingual Children: Decomposition and Cross-Language Activation

    ERIC Educational Resources Information Center

    Cheng, Chenxi; Wang, Min; Perfetti, Charles A.

    2011-01-01

    This study investigated compound processing and cross-language activation in a group of Chinese-English bilingual children, and they were divided into four groups based on the language proficiency levels in their two languages. A lexical decision task was designed using compound words in both languages. The compound words in one language contained…

  10. HPLC-based activity profiling for antiplasmodial compounds in the traditional Indonesian medicinal plant Carica papaya L.

    PubMed

    Julianti, Tasqiah; De Mieri, Maria; Zimmermann, Stefanie; Ebrahimi, Samad N; Kaiser, Marcel; Neuburger, Markus; Raith, Melanie; Brun, Reto; Hamburger, Matthias

    2014-08-08

    Leaf decoctions of Carica papaya have been traditionally used in some parts of Indonesia to treat and prevent malaria. Leaf extracts and fraction have been previously shown to possess antiplasmodial activity in vitro and in vivo. Antiplasmodial activity of extracts was confirmed and the active fractions in the extract were identified by HPLC-based activity profiling, a gradient HPLC fractionation of a single injection of the extract, followed by offline bioassay of the obtained microfractions. For preparative isolation of compounds, an alkaloidal fraction was obtained via adsorption on cationic ion exchange resin. Active compounds were purified by HPLC-MS and MPLC-ELSD. Structures were established by HR-ESI-MS and NMR spectroscopy. For compounds 5 and 7 absolute configuration was confirmed by comparison of experimental and calculated electronic circular dichroism (ECD) spectroscopy data, and by X-ray crystallography. Compounds were tested for bioactivity in vitro against four parasites (Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum), and in the Plasmodium berghei mouse model. Profiling indicated flavonoids and alkaloids in the active time windows. A total of nine compounds were isolated. Four were known flavonols--manghaslin, clitorin, rutin, and nicotiflorin. Five compounds isolated from the alkaloidal fraction were piperidine alkaloids. Compounds 5 and 6 were inactive carpamic acid and methyl carpamate, while three alkaloids 7-9 showed high antiplasmodial activity and low cytotoxicity. When tested in the Plasmodium berghei mouse model, carpaine (7) did not increase the survival time of animals. The antiplasmodial activity of papaya leaves could be linked to alkaloids. Among these, carpaine was highly active and selective in vitro. The high in vitro activity could not be substantiated with the in vivo murine model. Further investigations are needed to clarify the divergence between our negative in vivo results

  11. Relationship between electronic properties and drug activity of seven quinoxaline compounds: A DFT study

    NASA Astrophysics Data System (ADS)

    Behzadi, Hadi; Roonasi, Payman; Assle taghipour, Khatoon; van der Spoel, David; Manzetti, Sergio

    2015-07-01

    The quantum chemical calculations at the DFT/B3LYP level of theory were carried out on seven quinoxaline compounds, which have been synthesized as anti-Mycobacterium tuberculosis agents. Three conformers were optimized for each compound and the lowest energy structure was found and used in further calculations. The electronic properties including EHOMO, ELUMO and related parameters as well as electron density around oxygen and nitrogen atoms were calculated for each compound. The relationship between the calculated electronic parameters and biological activity of the studied compounds were investigated. Six similar quinoxaline derivatives with possible more drug activity were suggested based on the calculated electronic descriptors. A mechanism was proposed and discussed based on the calculated electronic parameters and bond dissociation energies.

  12. Design of cinnamaldehyde amino acid Schiff base compounds based on the quantitative structure-activity relationship.

    PubMed

    Wang, Hui; Jiang, Mingyue; Li, Shujun; Hse, Chung-Yun; Jin, Chunde; Sun, Fangli; Li, Zhuo

    2017-09-01

    Cinnamaldehyde amino acid Schiff base (CAAS) is a new class of safe, bioactive compounds which could be developed as potential antifungal agents for fungal infections. To design new cinnamaldehyde amino acid Schiff base compounds with high bioactivity, the quantitative structure-activity relationships (QSARs) for CAAS compounds against Aspergillus niger ( A. niger ) and Penicillium citrinum (P. citrinum) were analysed. The QSAR models ( R 2  = 0.9346 for A. niger , R 2  = 0.9590 for P. citrinum, ) were constructed and validated. The models indicated that the molecular polarity and the Max atomic orbital electronic population had a significant effect on antifungal activity. Based on the best QSAR models, two new compounds were designed and synthesized. Antifungal activity tests proved that both of them have great bioactivity against the selected fungi.

  13. Design of cinnamaldehyde amino acid Schiff base compounds based on the quantitative structure–activity relationship

    PubMed Central

    Wang, Hui; Jiang, Mingyue; Hse, Chung-Yun; Jin, Chunde; Sun, Fangli; Li, Zhuo

    2017-01-01

    Cinnamaldehyde amino acid Schiff base (CAAS) is a new class of safe, bioactive compounds which could be developed as potential antifungal agents for fungal infections. To design new cinnamaldehyde amino acid Schiff base compounds with high bioactivity, the quantitative structure–activity relationships (QSARs) for CAAS compounds against Aspergillus niger (A. niger) and Penicillium citrinum (P. citrinum) were analysed. The QSAR models (R2 = 0.9346 for A. niger, R2 = 0.9590 for P. citrinum,) were constructed and validated. The models indicated that the molecular polarity and the Max atomic orbital electronic population had a significant effect on antifungal activity. Based on the best QSAR models, two new compounds were designed and synthesized. Antifungal activity tests proved that both of them have great bioactivity against the selected fungi. PMID:28989758

  14. Isolation and Identification of Active Compounds from Papaya Plants and Activities as Antimicrobial

    NASA Astrophysics Data System (ADS)

    Prasetya, A. T.; Mursiti, S.; Maryan, S.; Jati, N. K.

    2018-04-01

    Extraction and isolation of papaya seeds and leaves (Carica papaya L) has been performed using n-hexane and ethanol solvents. Further isolation of the extract obtained using ethyl acetate and diethyl ether solvents. The result of the phytochemical test of papaya extract obtained by mixture of an active compound of flavonoids, alkaloids, tannins, steroids, and saponins. Ethyl acetate isolates containing only flavonoids and diethyl ether isolates contain only alkaloids. Extracts and isolates from papaya plants had gram-positive antibacterial activity greater than the gram-negative bacteria, but both did not have antifungal activity. Papaya extracts have greater antibacterial activity than flavonoid isolates and alkaloid isolates. Strong antibacterial inhibitory sequences are extracts of papaya plants, flavonoid isolates, and alkaloid isolates.

  15. Influence of technical processing units on chemical composition and antimicrobial activity of carrot (Daucus carrot L.) juice essential oil.

    PubMed

    Ma, Tingting; Luo, Jiyang; Tian, Chengrui; Sun, Xiangyu; Quan, Meiping; Zheng, Cuiping; Kang, Lina; Zhan, Jicheng

    2015-03-01

    The effect of three processing units (blanching, enzyme liquefaction, pasteurisation) on chemical composition and antimicrobial activity of carrot juice essential oil was investigated in this paper. A total of 36 compounds were identified by GC-MS from fresh carrot juice essential oil. The main constituents were carotol (20.20%), sabinene (12.80%), β-caryophyllene (8.04%) and α-pinene (6.05%). Compared with the oil of fresh juice, blanching and pasteurisation could significantly decrease the components of the juice essential oil, whereas enzyme liquefaction had no considerable effect on the composition of juice essential oil. With regard to the antimicrobial activity, carrot juice essential oil could cause physical damage and morphological alteration on microorganisms, while the three different processing units showed noticeable differences on the species of microorganisms, the minimum inhibitory concentration and minimum bactericidal concentration. Results revealed that the carrot juice essential oil has great potential for application as a natural antimicrobial applied in pharmaceutical and food industries. Copyright © 2014 Elsevier Ltd. All rights reserved.

  16. Synthesis of new 1,2,4-triazole compounds containing Schiff and Mannich bases (morpholine) with antioxidant and antimicrobial activities.

    PubMed

    Ünver, Yasemin; Deniz, Sadik; Çelik, Fatih; Akar, Zeynep; Küçük, Murat; Sancak, Kemal

    2016-01-01

    Compound 2 was synthesized by reacting CS 2 /KOH with compound 1. The treatment of compound 2 with hydrazine hydrate produced compound 3. Then, compound 3 was converted to Schiff bases (4a-d) by the handling with several aromatic aldehydes. The treatment of triazole compounds 4a-d containing Schiff base with morpholine gave compounds 5a-d. All compounds were tested for their antioxidant and antimicrobial activities. The antioxidant test results of DPPH• radical scavenging and ferric reducing/antioxidant power methods showed good antioxidant activity. The triazole-thiol (3) was the most active, and the effect of the substituent type of the thiophene ring on the activity was same for both Schiff bases (4a-d) and Mannich bases (5a-d). Among the newly synthesized triazole derivatives, the Schiff base 4d and the Mannich base 5d carrying nitro substituent on the thiophene ring showed promising antibacterial and antifungal activity, with lower MIC values than the standard antibacterial ampicillin.

  17. Extracts of Phenolic Compounds from Seeds of Three Wild Grapevines—Comparison of Their Antioxidant Activities and the Content of Phenolic Compounds

    PubMed Central

    Weidner, Stanisław; Powałka, Anna; Karamać, Magdalena; Amarowicz, Ryszard

    2012-01-01

    Phenolic compounds were extracted from three wild grapevine species: Vitis californica, V. riparia and V. amurensis seeds using 80% methanol or 80% acetone. The total content of phenolic compounds was determined utilizing the Folin-Ciocalteu’s phenol reagent while the content of tannins was assayed with the vanillin and BSA precipitation methods. Additionally, the DPPH free radical scavenging activity and the reduction power of the extracts were measured. The RP-HPLC method was applied to identify the phenolic compounds in the extracts, such as phenolic acids and catechins. The seeds contained large amounts of tannins, catechins and gallic acid and observable quantities of p-coumaric acid. The total content of phenolic compounds and tannins was similar in the extracts from V. californica and V. riparia seeds. However, the total content of total phenolic compounds and tannins in the extracts from V. californica and V. riperia seeds were about two-fold higher than that in the extracts from V. amurensis seeds. Extracts from seeds of the American species (V. californica and V. riparia) contained similarly high concentrations of tannins, whereas extracts from seeds of V. amurensis had approximately half that amount of these compounds. The content of catechin and epicatechin was similar in all extracts. The highest DPPH• anti-radical scavenging activity was observed in the acetonic and methanolic extracts of V. californica and V. riparia seeds— while the acetonic extract from the V. californica seeds was the strongest reducing agent. PMID:22489161

  18. Isolation and characterization of the compounds responsible for the antimutagenic activity of Combretum microphyllum (Combretaceae) leaf extracts.

    PubMed

    Makhafola, Tshepiso Jan; Elgorashi, Esameldin Elzein; McGaw, Lyndy Joy; Awouafack, Maurice Ducret; Verschaeve, Luc; Eloff, Jacobus Nicolaas

    2017-09-06

    Mutations play a major role in the pathogenesis and development of several chronic degenerative diseases including cancer. It follows, therefore that antimutagenic compound may inhibit the pathological process resulting from exposure to mutagens. Investigation of the antimutagenic potential of traditional medicinal plants and compounds isolated from plant extracts provides one of the tools that can be used to identify compounds with potential cancer chemopreventive properties. The aim of this study was to isolate and characterise the compounds responsible for the antimutagenic activity of Combretum microphyllum. The methanol leaf extract of C. microphyllum was evaluated for antimutagenicity in the Ames/microsome assay using Salmonella typhimurium TA98. TA100 and TA102. Solvent-solvent fractionation was used to partition the extracts and by using bioassay-guided fractionation, three compounds were isolated. The antimutagenic activity of the three compounds were determined in the Ames test using Salmonella typhimurium TA98, TA100 and TA102. The antioxidant activity of the three compounds were determined by the quantitative 2,2-diphenyl-1-picrylhydrazyl (DPPH)-free radical scavenging method. The cytotoxicity was determined in the MTT assay using human hepatocytes. A bioassay-guided fractionation of the crude extracts for antimutagenic activity led to the isolation of three compounds; n-tetracosanol, eicosanoic acid and arjunolic acid. Arjunolic acid was the most active in all three tested strains with a antimutagenicity of 42 ± 9.6%, 36 ± 1.5% and 44 ± 0.18% in S. typhimurium TA98, TA100 and TA102 respectively at the highest concentration (500 μg/ml) tested, followed by eicosanoic acid and n-tetracosanol. The antioxidant activity of the compounds were determined using the quantitative 2,2 diphenyl-1-picryhydrazyl (DPPH)-free radical scavenging method. Only arjunolic acid had pronounced antioxidant activity (measured as DPPH-free scavenging activity) with an

  19. Compound A, a Selective Glucocorticoid Receptor Modulator, Enhances Heat Shock Protein Hsp70 Gene Promoter Activation

    PubMed Central

    Beck, Ilse M.; Drebert, Zuzanna J.; Hoya-Arias, Ruben; Bahar, Ali A.; Devos, Michael; Clarisse, Dorien; Desmet, Sofie; Bougarne, Nadia; Ruttens, Bart; Gossye, Valerie; Denecker, Geertrui; Lievens, Sam; Bracke, Marc; Tavernier, Jan; Declercq, Wim; Gevaert, Kris; Berghe, Wim Vanden; Haegeman, Guy; De Bosscher, Karolien

    2013-01-01

    Compound A possesses glucocorticoid receptor (GR)-dependent anti-inflammatory properties. Just like classical GR ligands, Compound A can repress NF-κB-mediated gene expression. However, the monomeric Compound A-activated GR is unable to trigger glucocorticoid response element-regulated gene expression. The heat shock response potently activates heat shock factor 1 (HSF1), upregulates Hsp70, a known GR chaperone, and also modulates various aspects of inflammation. We found that the selective GR modulator Compound A and heat shock trigger similar cellular effects in A549 lung epithelial cells. With regard to their anti-inflammatory mechanism, heat shock and Compound A are both able to reduce TNF-stimulated IκBα degradation and NF-κB p65 nuclear translocation. We established an interaction between Compound A-activated GR and Hsp70, but remarkably, although the presence of the Hsp70 chaperone as such appears pivotal for the Compound A-mediated inflammatory gene repression, subsequent novel Hsp70 protein synthesis is uncoupled from an observed CpdA-induced Hsp70 mRNA upregulation and hence obsolete in mediating CpdA’s anti-inflammatory effect. The lack of a Compound A-induced increase in Hsp70 protein levels in A549 cells is not mediated by a rapid proteasomal degradation of Hsp70 or by a Compound A-induced general block on translation. Similar to heat shock, Compound A can upregulate transcription of Hsp70 genes in various cell lines and BALB/c mice. Interestingly, whereas Compound A-dependent Hsp70 promoter activation is GR-dependent but HSF1-independent, heat shock-induced Hsp70 expression alternatively occurs in a GR-independent and HSF1-dependent manner in A549 lung epithelial cells. PMID:23935933

  20. Bayesian screening for active compounds in high-dimensional chemical spaces combining property descriptors and molecular fingerprints.

    PubMed

    Vogt, Martin; Bajorath, Jürgen

    2008-01-01

    Bayesian classifiers are increasingly being used to distinguish active from inactive compounds and search large databases for novel active molecules. We introduce an approach to directly combine the contributions of property descriptors and molecular fingerprints in the search for active compounds that is based on a Bayesian framework. Conventionally, property descriptors and fingerprints are used as alternative features for virtual screening methods. Following the approach introduced here, probability distributions of descriptor values and fingerprint bit settings are calculated for active and database molecules and the divergence between the resulting combined distributions is determined as a measure of biological activity. In test calculations on a large number of compound activity classes, this methodology was found to consistently perform better than similarity searching using fingerprints and multiple reference compounds or Bayesian screening calculations using probability distributions calculated only from property descriptors. These findings demonstrate that there is considerable synergy between different types of property descriptors and fingerprints in recognizing diverse structure-activity relationships, at least in the context of Bayesian modeling.

  1. Target Fishing for Chemical Compounds using Target-Ligand Activity data and Ranking based Methods

    PubMed Central

    Wale, Nikil; Karypis, George

    2009-01-01

    In recent years the development of computational techniques that identify all the likely targets for a given chemical compound, also termed as the problem of Target Fishing, has been an active area of research. Identification of likely targets of a chemical compound helps to understand problems such as toxicity, lack of efficacy in humans, and poor physical properties associated with that compound in the early stages of drug discovery. In this paper we present a set of techniques whose goal is to rank or prioritize targets in the context of a given chemical compound such that most targets that this compound may show activity against appear higher in the ranked list. These methods are based on our extensions to the SVM and Ranking Perceptron algorithms for this problem. Our extensive experimental study shows that the methods developed in this work outperform previous approaches by 2% to 60% under different evaluation criterions. PMID:19764745

  2. Anti-inflammatory activity of different agave plants and the compound cantalasaponin-1.

    PubMed

    Monterrosas-Brisson, Nayeli; Ocampo, Martha L Arenas; Jiménez-Ferrer, Enrique; Jiménez-Aparicio, Antonio R; Zamilpa, Alejandro; Gonzalez-Cortazar, Manases; Tortoriello, Jaime; Herrera-Ruiz, Maribel

    2013-07-10

    Species of the agave genus, such as Agave tequilana, Agave angustifolia and Agave americana are used in Mexican traditional medicine to treat inflammation-associated conditions. These plants' leaves contain saponin compounds which show anti-inflammatory properties in different models. The goal of this investigation was to evaluate the anti-inflammatory capacity of these plants, identify which is the most active, and isolate the active compound by a bio-directed fractionation using the ear edema induced in mice with 12-O-tetradecanoylphorbol-13-acetate (TPA) technique. A dose of 6 mg/ear of acetone extract from the three agave species induced anti-inflammatory effects, however, the one from A. americana proved to be the most active. Different fractions of this species showed biological activity. Finally the F5 fraction at 2.0 mg/ear induced an inhibition of 85.6%. We identified one compound in this fraction as (25R)-5α-spirostan-3β,6α,23α-triol-3,6-di-O-β-D-glucopyranoside (cantalasaponin-1) through 1H- and 13C-NMR spectral analysis and two dimensional experiments like DEPT NMR, COSY, HSQC and HMBC. This steroidal glycoside showed a dose dependent effect of up to 90% of ear edema inhibition at the highest dose of 1.5 mg/ear.

  3. Hybrid energy storage systems utilizing redox active organic compounds

    DOEpatents

    Wang, Wei; Xu, Wu; Li, Liyu; Yang, Zhenguo

    2015-09-08

    Redox flow batteries (RFB) have attracted considerable interest due to their ability to store large amounts of power and energy. Non-aqueous energy storage systems that utilize at least some aspects of RFB systems are attractive because they can offer an expansion of the operating potential window, which can improve on the system energy and power densities. One example of such systems has a separator separating first and second electrodes. The first electrode includes a first current collector and volume containing a first active material. The second electrode includes a second current collector and volume containing a second active material. During operation, the first source provides a flow of first active material to the first volume. The first active material includes a redox active organic compound dissolved in a non-aqueous, liquid electrolyte and the second active material includes a redox active metal.

  4. Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds

    PubMed Central

    Crowther, Gregory J.; Hillesland, Heidi K.; Keyloun, Katelyn R.; Reid, Molly C.; Lafuente-Monasterio, Maria Jose; Ghidelli-Disse, Sonja; Leonard, Stephen E.; He, Panqing; Jones, Jackson C.; Krahn, Mallory M.; Mo, Jack S.; Dasari, Kartheek S.; Fox, Anna M. W.; Boesche, Markus; El Bakkouri, Majida; Rivas, Kasey L.; Leroy, Didier; Hui, Raymond; Drewes, Gerard; Maly, Dustin J.; Van Voorhis, Wesley C.; Ojo, Kayode K.

    2016-01-01

    In 2010 the identities of thousands of anti-Plasmodium compounds were released publicly to facilitate malaria drug development. Understanding these compounds’ mechanisms of action—i.e., the specific molecular targets by which they kill the parasite—would further facilitate the drug development process. Given that kinases are promising anti-malaria targets, we screened ~14,000 cell-active compounds for activity against five different protein kinases. Collections of cell-active compounds from GlaxoSmithKline (the ~13,000-compound Tres Cantos Antimalarial Set, or TCAMS), St. Jude Children’s Research Hospital (260 compounds), and the Medicines for Malaria Venture (the 400-compound Malaria Box) were screened in biochemical assays of Plasmodium falciparum calcium-dependent protein kinases 1 and 4 (CDPK1 and CDPK4), mitogen-associated protein kinase 2 (MAPK2/MAP2), protein kinase 6 (PK6), and protein kinase 7 (PK7). Novel potent inhibitors (IC50 < 1 μM) were discovered for three of the kinases: CDPK1, CDPK4, and PK6. The PK6 inhibitors are the most potent yet discovered for this enzyme and deserve further scrutiny. Additionally, kinome-wide competition assays revealed a compound that inhibits CDPK4 with few effects on ~150 human kinases, and several related compounds that inhibit CDPK1 and CDPK4 yet have limited cytotoxicity to human (HepG2) cells. Our data suggest that inhibiting multiple Plasmodium kinase targets without harming human cells is challenging but feasible. PMID:26934697

  5. Antialgal compounds with antialgal activity against the common red tide microalgae from a green algae Ulva pertusa.

    PubMed

    Sun, Ying-Ying; Zhou, Wen-Jing; Wang, Hui; Guo, Gan-Lin; Su, Zhen-Xia; Pu, Yin-Fang

    2018-08-15

    Nine antialgal active compounds, (i.e. trehalose (1), twenty-two methyl carbonate (2), (-)-dihydromenisdaurilide (3), 3,7,11,15-tetramethyl-2-hexadecen-1-ol (4), isophytol (5), 8-hexadecenol (6), 17-hydroxyheptadecanoic acid (7), trans-asarone (8) and 2-amino-3-mercaptopropanoic acid (9)) were isolated from Ulva pertusa for the first time by sephadex LH-20 column chromatography, silica gel column chromatography and repeated preparative TLC. Except for compound 4, all compounds represented novel isolated molecules from marine macroalgae. Further, antialgal activities of these compounds against Amphidinium carterae, Heterosigma akashiwo, Karenia mikimitoi, Phaeocystis globosa, Prorocentrum donghaiense and Skeletonema costatum were investigated for the first time. Results showed these nine compounds have selectivity antialgal effects on all test red tide microalgae, and antialgal activities against red tide microalgae obviously enhanced with the increase of concentration of antialgal compounds. Based on this, EC 50-96 h values of these nine compounds for six red tide microalgae were obtained for the first time. By analyzing and comparing EC 50-96 h values, it has been determined that seven compounds (1, 3, 4, 6, 7, 8 and 9) showed the superior application potential than potassium dichromate or gossonorol and other six compounds as a characteristic antialgal agent against Heterosigma akashiwo, Karenia mikimitoi and Prorocentrum donghaiense. Overall this study has suggested that green algae Ulva pertusa is a new source of bioactive compounds with antialgal activity. Copyright © 2018. Published by Elsevier Inc.

  6. Aldose Reductase Inhibitory Activity of Compounds from  Zea mays L.

    PubMed Central

    Kim, Tae Hyeon; Kim, Jin Kyu; Kang, Young-Hee; Lee, Jae-Yong; Kang, Il Jun; Lim, Soon Sung

    2013-01-01

    Aldose reductase (AR) inhibitors have a considerable therapeutic potential against diabetes complications and do not increase the risk of hypoglycemia. Through bioassay-guided fractionation of an EtOH extract of the kernel from purple corn (Zea mays L.), 7 nonanthocyanin phenolic compounds (compound 1–7) and 5 anthocyanins (compound 8–12) were isolated. These compounds were investigated by rat lens aldose reductase (RLAR) inhibitory assays. Kinetic analyses of recombinant human aldose reductase (rhAR) were performed, and intracellular galactitol levels were measured. Hirsutrin, one of 12 isolated compounds, showed the most potent RLAR inhibitory activity (IC50, 4.78 μM). In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/substrate concentration, hirsutrin showed competitive inhibition against rhAR. Furthermore, hirsutrin inhibited galactitol formation in rat lens and erythrocytes sample incubated with a high concentration of galactose; this finding indicates that hirsutrin may effectively prevent osmotic stress in hyperglycemia. Therefore, hirsutrin derived from Zea mays L. may be a potential therapeutic agent against diabetes complications. PMID:23586057

  7. Validation of chemical compound library screening for transcriptional co-activator with PDZ-binding motif inhibitors using GFP-fused transcriptional co-activator with PDZ-binding motif.

    PubMed

    Nagashima, Shunta; Maruyama, Junichi; Kawano, Shodai; Iwasa, Hiroaki; Nakagawa, Kentaro; Ishigami-Yuasa, Mari; Kagechika, Hiroyuki; Nishina, Hiroshi; Hata, Yutaka

    2016-06-01

    Transcriptional co-activator with PDZ-binding motif (TAZ) plays versatile roles in cell proliferation and differentiation. It is phosphorylated by large tumor suppressor kinases, the core kinases of the tumor-suppressive Hippo pathway. Phosphorylation induces the cytoplasmic accumulation of TAZ and its degradation. In human cancers, the deregulation of the Hippo pathway and gene amplification enhance TAZ activity. TAZ interacts with TEA domain family members (TEAD), and upregulates genes implicated in epithelial-mesenchymal transition. It also confers stemness to cancer cells. Thus, TAZ activation provides cancer cells with malignant properties and worsens the clinical prognosis. Therefore, TAZ attracts attention as a therapeutic target in cancer therapy. We applied 18 606 small chemical compounds to human osteosarcoma U2OS cells expressing GFP-fused TAZ (GFP-TAZ), monitored the subcellular localization of GFP-TAZ, and selected 33 compounds that shifted GFP-TAZ to the cytoplasm. Unexpectedly, only a limited number of compounds suppressed TAZ-mediated enhancement of TEAD-responsive reporter activity. Moreover, the compounds that weakened TEAD reporter activity did not necessarily decrease the unphosphorylated TAZ. In this study, we focused on three compounds that decreased both TEAD reporter activity and unphosphorylated TAZ, and treated several human cancer cells with these compounds. One compound did not show a remarkable effect, whereas the other two compounds compromised the cell viability in certain cancer cells. In conclusion, the GFP-TAZ-based assay can be used as the first screening for compounds that inhibit TAZ and show anticancer properties. To develop anticancer drugs, we need additional assays to select the compounds. © 2016 The Authors. Cancer Science published by John Wiley & Sons Australia, Ltd on behalf of Japanese Cancer Association.

  8. Bioactive Compound Contents and Antioxidant Activity in Aronia (Aronia melanocarpa) Leaves Collected at Different Growth Stages.

    PubMed

    Thi, Nhuan Do; Hwang, Eun-Sun

    2014-09-01

    The bioactive compounds and antioxidant activity of aronia leaves at different stages of maturity were identified and evaluated. Young and old leaves were approximately 2 months of age and 4 months of age, respectively. The young leaves contained more polyphenols and flavonoids than the old leaves. Three phenolic compounds (i.e., chlorogenic acid, p-coumaric acid, and rutin) were detected by HPLC. Antioxidant activity was measured using 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical, and superoxide anion radical scavenging assays. The reducing power of aronia leaf extracts increased in a concentration-dependent manner (0~100 μg/mL). The antioxidant activity of the 80% ethanol extract was greater than that of distilled water extract. The high phenolic compound content indicated that these compounds contribute to antioxidant activity. The overall results indicate that aronia leaves contain bioactive compounds, and that younger aronia leaves may be more favorable for extracting antioxidative ingredients because they contain more polyphenols.

  9. Bioactive Compound Contents and Antioxidant Activity in Aronia (Aronia melanocarpa) Leaves Collected at Different Growth Stages

    PubMed Central

    Thi, Nhuan Do; Hwang, Eun-Sun

    2014-01-01

    The bioactive compounds and antioxidant activity of aronia leaves at different stages of maturity were identified and evaluated. Young and old leaves were approximately 2 months of age and 4 months of age, respectively. The young leaves contained more polyphenols and flavonoids than the old leaves. Three phenolic compounds (i.e., chlorogenic acid, p-coumaric acid, and rutin) were detected by HPLC. Antioxidant activity was measured using 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical, and superoxide anion radical scavenging assays. The reducing power of aronia leaf extracts increased in a concentration-dependent manner (0~100 μg/mL). The antioxidant activity of the 80% ethanol extract was greater than that of distilled water extract. The high phenolic compound content indicated that these compounds contribute to antioxidant activity. The overall results indicate that aronia leaves contain bioactive compounds, and that younger aronia leaves may be more favorable for extracting antioxidative ingredients because they contain more polyphenols. PMID:25320718

  10. Algicidal activity of Bacillus sp. Lzh-5 and its algicidal compounds against Microcystis aeruginosa.

    PubMed

    Li, Zhenghua; Geng, Mengxin; Yang, Hong

    2015-01-01

    A freshwater algicidal bacterial strain, Lzh-5, isolated from Lake Taihu, with strong algicidal activity against Microcystis aeruginosa, was identified as Bacillus sp. based on its phenotypic characteristics and 16S ribosomal RNA (rRNA) gene sequence. The algicidal mode of Bacillus sp. Lzh-5 was indirect, attacking M. aeruginosa cells by releasing algicidal compounds. Two algicidal compounds (S-5A and S-5B) produced by Bacillus sp. Lzh-5 were purified with ethyl acetate extraction, column chromatography, and high-performance liquid chromatography and identified as hexahydropyrrolo[1,2-a]pyrazine-1,4-dione and 3-isopropyl-hexahydropyrrolo[1,2-a]pyrazine-1,4-dione based on liquid chromatography-mass spectrometry, gas chromatography-mass spectrometry, and nuclear magnetic resonance analyses. The active algicidal compounds S-5A (hexahydropyrrolo[1,2-a]pyrazine-1,4-dione) and S-5B (3-isopropyl-hexahydropyrrolo[1,2-a]pyrazine-1,4-dione) displayed high levels of algicidal activity against M. aeruginosa 9110, with LD50 values of 5.7 and 19.4 μg/ml, respectively. This is the first report of 3-isopropyl-hexahydropyrrolo[1,2-a]pyrazine-1,4-dione as an algicidal compound. Compounds S-5A and S-5B also induced obvious morphological changes in M. aeruginosa 9110. In cocultures of M. aeruginosa 9110 and Bacillus sp. Lzh-5, the cell density of Bacillus sp. Lzh-5 and the concentrations of S-5A and S-5B correlated positively with the algicidal activity. Our results indicate that strain Lzh-5 and its two algicidal compounds are potentially useful for controlling cyanobacterial blooms in Lake Taihu.

  11. Anticancer activity of botanical compounds in ancient fermented beverages (review).

    PubMed

    McGovern, P E; Christofidou-Solomidou, M; Wang, W; Dukes, F; Davidson, T; El-Deiry, W S

    2010-07-01

    Humans around the globe probably discovered natural remedies against disease and cancer by trial and error over the millennia. Biomolecular archaeological analyses of ancient organics, especially plants dissolved or decocted as fermented beverages, have begun to reveal the preliterate histories of traditional pharmacopeias, which often date back thousands of years earlier than ancient textual, ethnohistorical, and ethnological evidence. In this new approach to drug discovery, two case studies from ancient Egypt and China illustrate how ancient medicines can be reconstructed from chemical and archaeological data and their active compounds delimited for testing their anticancer and other medicinal effects. Specifically, isoscopoletin from Artemisia argyi, artemisinin from Artemisia annua, and the latter's more easily assimilated semi-synthetic derivative, artesunate, showed the greatest activity in vitro against lung and colon cancers. In vivo tests of these compounds previously unscreened against lung and pancreatic cancers are planned for the future.

  12. Phytochemical screening and in-vitro antioxidant activity isolated bioactive compounds from Tridax procumbens Linn.

    PubMed

    Saxena, Manjusha; Mir, Abrar Hussain; Sharma, Manik; Malla, Mohd Yousu; Qureshi, Sumeerah; Mir, Mohd Iqbal; Chaturvedi, Yogesh

    2013-12-15

    Tridax procumbens L., Asteraceae, has been extensively used for various ailments in the Ayurvedic system of medicine. Previous studies have revealed remarkable phytoconstituents from Tridax procumbens L. with significant antioxidant activity. The aim of the present study is to measure the anti-DPPH activity of the purified isolated compounds from n butanol soluble part and ethyl acetate soluble part of successive methanolic extract of Tridax procumbens L. We thus quantified the total phenolic and total flavonoids in different purified isolated compounds, the whole of the tests were evaluated with a sample cone. of 100 microg mL(-1) and were determined spectrophotometrically using Folin-ciocaltue and AlCl3 reagents, respectively. DPPH (1,1-diphenyl, 2-picryl hydrazyl) assay was used to determine the in vitro antioxidant activity of different isolated compounds. Isolated compounds, one from ethyl acetate soluble part (EF-I) and one from n butanol soluble part (BF-II) were reported to possess a significant anti DPPH activity with lowest IC50 values 67.26 and 80.90 microg mL(-1), respectively while comparable to standard ascorbic acid with IC50 value of 59.62 microg mL(-1), due to the high concentration of phenols 146.4 microg mL(-1) from EF-I and 142.2 microg mL(-1) from BF-II and flavonoids 48 and 42.5 microg mL(-1) found in EF-I and BF-II isolated compounds, respectively.

  13. Hammerhead ribozyme activity and oligonucleotide duplex stability in mixed solutions of water and organic compounds

    PubMed Central

    Nakano, Shu-ichi; Kitagawa, Yuichi; Miyoshi, Daisuke; Sugimoto, Naoki

    2014-01-01

    Nucleic acids are useful for biomedical targeting and sensing applications in which the molecular environment is different from that of a dilute aqueous solution. In this study, the influence of various types of mixed solutions of water and water-soluble organic compounds on RNA was investigated by measuring the catalytic activity of the hammerhead ribozyme and the thermodynamic stability of an oligonucleotide duplex. The compounds with a net neutral charge, such as poly(ethylene glycol), small primary alcohols, amide compounds, and aprotic solvent molecules, added at high concentrations changed the ribozyme-catalyzed RNA cleavage rate, with the magnitude of the effect dependent on the NaCl concentration. These compounds also changed the thermodynamic stability of RNA base pairs of an oligonucleotide duplex and its dependence on the NaCl concentration. Specific interactions with RNA molecules and reduced water activity could account for the inhibiting effects on the ribozyme catalysis and destabilizing effects on the duplex stability. The salt concentration dependence data correlated with the dielectric constant, but not with water activity, viscosity, and the size of organic compounds. This observation suggests the significance of the dielectric constant effects on the RNA reactions under molecular crowding conditions created by organic compounds. PMID:25161873

  14. Enhanced photo-activated luminescence for screening polychlorobiphenyls (PCBs) and other related chlorinated compounds

    DOEpatents

    Vo-Dinh, Tuan

    1994-01-01

    The presence of polychlorinated biphenyls and other chlorinated compounds in a sample is determined by treating the sample with a photo-activator and then exposing the treated sample to a UV light source. The UV light produces a photo-product complex, which is subsequently excited with UV light to cause luminescence of the complex. The luminescence is detected and characteristics of the luminescence spectra are used to determine the presence of chlorinated compounds and also the quantity of the chlorine in the compounds

  15. Enhanced photo-activated luminescence for screening polychlorobiphenyls (PCBs) and other related chlorinated compounds

    DOEpatents

    Vo-Dinh, Tuan

    1993-01-01

    The presence of polychlorinated biphenyls and other chlorinated compounds in a sample is determined by treating the sample with a photo-activator and then exposing the treated sample to a UV light source. The UV light produces a photo-product complex, which is subsequently excited with UV light to cause luminescence of the complex. The luminescence is detected and characteristics of the luminescence spectra are used to determine the presence of chlorinated compounds and also the quantity of the chlorine in the compounds.

  16. Effective adsorption of phenolic compound from aqueous solutions on activated semi coke

    NASA Astrophysics Data System (ADS)

    Gao, Xiaoming; Dai, Yuan; Zhang, Yu; Fu, Feng

    2017-03-01

    Activated Semi coke was prepared by KOH activation and employed as adsorbent to study adsorption function of phenolic compound from aqueous solutions. The adsorption result showed that the adsorption capacity of the activated semi coke for phenolic compound increased with contact time and adsorbent dosage, and slightly affected by temperature. The surface structure property of the activated semi coke was characterized by N2 adsorption, indicating that the activated semi coke was essentially macroporous, and the BET surface area was 347.39 m2 g-1. Scanning electron microscopy indicated that the surface of the activated semi coke had a high developed pore. The adsorption kinetics were investigated according to pseudofirst order, pseudosecond order and intraparticle diffusion, and the kinetics data were fitted by pseudosecond order model, and intraparticle diffusion was not the only rate-controlling step. Adsorption isotherm was studied by Langmuir, Freundlich, Temkin, Redlich-Peterson, Sips and Toth models. The result indicated that adsorption isotherm data could fit well with Langmuir, Redlich-Peterson, Sips and Toth models.

  17. Compounds from Sedum caeruleum with antioxidant, anticholinesterase, and antibacterial activities.

    PubMed

    Bensouici, Chawki; Kabouche, Ahmed; Karioti, Anastasia; Öztürk, Mehmet; Duru, Mehmet Emin; Bilia, Anna Rita; Kabouche, Zahia

    2016-01-01

    This is the first study on the phytochemistry, antioxidant, anticholinesterase, and antibacterial activities of Sedum caeruleum L. (Crassulaceae). The objective of this study is to isolate the secondary metabolites and determine the antioxidant, anticholinesterase, and antibacterial activities of S. caeruleum. Six compounds (1-6) were isolated from the extracts of S. caeruleum and elucidated using UV, 1D-, 2D-NMR, and MS techniques. Antioxidant activity was investigated using DPPH(•), CUPRAC, and ferrous-ions chelating assays. Anticholinesterase activity was determined against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes using the Ellman method. Antibacterial activity was performed according to disc diffusion and minimum inhibitory concentration (MIC) methods. Isolated compounds were elucidated as ursolic acid (1), daucosterol (2), β-sitosterol-3-O-β-D-galactopyranoside (3), apigenin (4), apigetrin (5), and apiin (6). The butanol extract exhibited highest antioxidant activity in all tests (IC50 value: 28.35 ± 1.22 µg/mL in DPPH assay, IC50 value: 40.83 ± 2.24 µg/L in metal chelating activity, and IC50 value: 23.52 ± 0.44 µg/L in CUPRAC), and the highest BChE inhibitory activity (IC50 value: 36.89 ± 0.15 µg/L). Moreover, the chloroform extract mildly inhibited (MIC value: 80 µg/mL) the growth of all the tested bacterial strains. Ursolic acid (1), daucosterol (2), β-sitosterol-3-O-β-D-galactopyranoside (3), apigenin (4), apigetrin (5), and apiin (6) were isolated from Sedum caeruleum for the first time. In addition, a correlation was observed between antioxidant and anticholinesterase activities of bioactive ingredients of this plant.

  18. Asymmetric bioreduction of activated alkenes to industrially relevant optically active compounds

    PubMed Central

    Winkler, Christoph K.; Tasnádi, Gábor; Clay, Dorina; Hall, Mélanie; Faber, Kurt

    2012-01-01

    Ene-reductases from the ‘Old Yellow Enzyme’ family of flavoproteins catalyze the asymmetric reduction of various α,β-unsaturated compounds at the expense of a nicotinamide cofactor. They have been applied to the synthesis of valuable enantiopure products, including chiral building blocks with broad industrial applications, terpenoids, amino acid derivatives and fragrances. The combination of these highly stereoselective biocatalysts with a cofactor recycling system has allowed the development of cost-effective methods for the generation of optically active molecules, which is strengthened by the availability of stereo-complementary enzyme homologues. PMID:22498437

  19. The adsorption of pharmaceutically active compounds from aqueous solutions onto activated carbons.

    PubMed

    Rakić, Vesna; Rac, Vladislav; Krmar, Marija; Otman, Otman; Auroux, Aline

    2015-01-23

    In this study, the adsorption of pharmaceutically active compounds - salicylic acid, acetylsalicylic acid, atenolol and diclofenac-Na onto activated carbons has been studied. Three different commercial activated carbons, possessing ∼650, 900 or 1500m(2)g(-1) surface areas were used as solid adsorbents. These materials were fully characterized - their textural, surface features and points of zero charge have been determined. The adsorption was studied from aqueous solutions at 303K using batch adsorption experiments and titration microcalorimetry, which was employed in order to obtain the heats evolved as a result of adsorption. The maximal adsorption capacities of investigated solids for all target pharmaceuticals are in the range of 10(-4)molg(-1). The obtained maximal retention capacities are correlated with the textural properties of applied activated carbon. The roles of acid/base features of activated carbons and of molecular structures of adsorbate molecules have been discussed. The obtained results enabled to estimate the possibility to use the activated carbons in the removal of pharmaceuticals by adsorption. Copyright © 2014 Elsevier B.V. All rights reserved.

  20. A review of QSAR studies to discover new drug-like compounds actives against leishmaniasis and trypanosomiasis.

    PubMed

    Castillo-Garit, Juan Alberto; Abad, Concepción; Rodríguez-Borges, J Enrique; Marrero-Ponce, Yovani; Torrens, Francisco

    2012-01-01

    The neglected tropical diseases (NTDs) affect more than one billion people (one-sixth of the world's population) and occur primarily in undeveloped countries in sub-Saharan Africa, Asia, and Latin America. Available drugs for these diseases are decades old and present an important number of limitations, especially high toxicity and, more recently, the emergence of drug resistance. In the last decade several Quantitative Structure-Activity Relationship (QSAR) studies have been developed in order to identify new organic compounds with activity against the parasites responsible for these diseases, which are reviewed in this paper. The topics summarized in this work are: 1) QSAR studies to identify new organic compounds actives against Chaga's disease; 2) Development of QSAR studies to discover new antileishmanial drusg; 3) Computational studies to identify new drug-like compounds against human African trypanosomiasis. Each topic include the general characteristics, epidemiology and chemotherapy of the disease as well as the main QSAR approaches to discovery/identification of new actives compounds for the corresponding neglected disease. The last section is devoted to a new approach know as multi-target QSAR models developed for antiparasitic drugs specifically those actives against trypanosomatid parasites. At present, as a result of these QSAR studies several promising compounds, active against these parasites, are been indentify. However, more efforts will be required in the future to develop more selective (specific) useful drugs.

Some links on this page may take you to non-federal websites. Their policies may differ from this site.