Methylophiopogonanone A is a naturally occurring broad‐spectrum inhibitor against human UDP‐glucuronosyltransferases: inhibition behaviours and implication in herb‐drug interactions

Author(s):  
Qi‐Hang Zhou ◽  
Guang‐Hao Zhu ◽  
Yun‐Qing Song ◽  
Yuan‐Fang Que ◽  
Qing‐Qing He ◽  
...  
2009 ◽  
Vol 1 ◽  
pp. CMT.S2297 ◽  
Author(s):  
Jennifer L. Halsey

Nitazoxanide is a broad-spectrum agent active against several protozoa, helminths, and bacteria, including C. difficile and H. pylori. It is available as an oral tablet and suspension, both with adequate bioavailability. Nitazoxanide is associated with minimal side effects, has an acceptable safety profile, and has been classified as a pregnancy category B agent. It is 99% protein bound, which could result in drug interactions. It is the preferred agent for the treatment of Cryptospordiosis and Giardiasis in immunocompetent patients and has shown promise for the treatment of rotavirus, mild to moderate initial C. difficile infection, refractory C. difficile infection, Amoebiasis, Blastocystosis, and Taenia saginata.


2010 ◽  
Vol 54 (11) ◽  
pp. 4930-4933 ◽  
Author(s):  
José-Manuel Rodríguez-Martínez ◽  
Laurent Poirel ◽  
Patrice Nordmann

ABSTRACT The incidence of naturally occurring AmpC β-lactamases with extended activities toward several cephalosporins was evaluated among 17 ceftazidime (CAZ)-resistant Acinetobacter baumannii isolates. Five AmpC β-lactamases (named ADC β-lactamases) were identified, among which those possessing the Val208Ala (inside the omega-loop) or Asn283Ser (helix H-10) substitution conferred higher levels of resistance (4- to 64-fold higher) to CAZ and to cefotaxime in Escherichia coli. This study demonstrates that peculiar AmpCs playing a role in resistance to broad-spectrum cephalosporins in A. baumannii may be identified.


2020 ◽  
Vol 4 (2) ◽  
pp. 055-059
Author(s):  
Abd El-Aziz Mahmoud Hamdy ◽  
Khalil Mohamed Salah

For many years, chemical pesticides have been performed to control different pests and diseases and this may be due to their broad spectrum of action, easy of application and the relatively low cost. But these chemicals have environmental risks, thus alternative control agents are needed. Chitosan is one of the novel suggested solutions to reduce the economic losses associated with chemical pesticides. Chitosan is naturally-occurring compound, as well as safe and biodegradable which obtained from certain natural sources. Chitosan have unique properties which help to control viruses, bacteria, fungi, insects, plant nematodes and other pests locally and systemically.


2003 ◽  
Vol 47 (7) ◽  
pp. 2113-2117 ◽  
Author(s):  
Cody C. Cain ◽  
Dongho Lee ◽  
Robert H. Waldo ◽  
Alexis T. Henry ◽  
Earl J. Casida ◽  
...  

ABSTRACT A naturally occurring, gram-negative, nonobligate predator bacterial strain 679-2, exhibits broad-spectrum antimicrobial activity that is due, in part, to the production of three extracellular compounds. Antimicrobial-activity-directed fractionation of a culture of strain 679-2 against a panel of microorganisms has led to the isolation of three compounds: pyrrolnitrin, maculosin, and a new compound, which we have named banegasine. Although pyrrolnitrin is well known in the literature, it has not been found in cells with the herbicide maculosin. Further, this is the first report of production of maculosin by a prokaryote. Both maculosin and banegasine, which displayed no antimicrobial activities alone, were found to potentiate the antimicrobial activity of pyrrolnitrin. Based on 16S rRNA sequence, cellular fatty acid composition, and biochemical and cultural characteristics, strain 679-2 appears to represent a new genus and species of eubacteria, Aristabacter necator. The potent, broad-spectrum antimicrobial activity of predator strain 679-2 may be due to synergism between metabolites.


2016 ◽  
Vol 34 (3) ◽  
pp. 607-616 ◽  
Author(s):  
C. DÍAZ-TIELAS ◽  
E. GRAÑA ◽  
M.J. REIGOSA ◽  
A.M. SÁNCHEZ-MOREIRAS

ABSTRACT This review provides information on the biological activities of chalcones (whether natural or synthetic derivatives) on different organisms, as well as an overview of the functions and possible new applications of these plant secondary metabolites on crop protection, as eco-friendly pesticides and weed control agents. Naturally occurring chalcones have been used in traditional medicine for many years; however, recent scientific advances have shown that these molecules have a broad range of biological activities in a variety of organisms. A review on the major sources of chalcones and the main molecular events involved in the modes of action of these natural products is achieved. Chalcones are molecules with a broad spectrum of biological activities, which are of great interest in agriculture to control weeds and unwanted pests.


2018 ◽  
Vol 62 (4) ◽  
Author(s):  
Lisandro J. González ◽  
Cintia Stival ◽  
Juan L. Puzzolo ◽  
Diego M. Moreno ◽  
Alejandro J. Vila

ABSTRACTMetallo-β-lactamases (MBLs) are the major group of carbapenemases produced by bacterial pathogens. The design of MBL inhibitors has been limited by, among other issues, incomplete knowledge about how these enzymes modulate substrate recognition. While most MBLs are broad-spectrum enzymes, B2 MBLs are exclusive carbapenemases. This narrower substrate profile has been attributed to a sequence insertion present in B2 enzymes that limits accessibility to the active site. In this work, we evaluate the role of sequence insertions naturally occurring in the B2 enzyme Sfh-I and in the broad-spectrum B1 enzyme SPM-1. We engineered a chimeric protein in which the sequence insertion of SPM-1 was replaced by the one present in Sfh-I. The chimeric variant is a selective cephalosporinase, revealing that the substrate profile of MBLs can be further tuned depending on the protein context. These results also show that the stable scaffold of MBLs allows a modular engineering much richer than the one observed in nature.


Author(s):  
Les Iversen

‘How drugs work’ outlines the basic mechanisms of pharmacology. Drugs are chemicals that can be naturally occurring or man-made, and which can be administered in a variety of ways. They can act on receptors—often highly specific proteins in cells which can up-regulate or down-regulate processes—or on other targets, such as DNA or enzymes. The molecular action of drugs can be investigated in a lab, but the effects on the whole organism are more important. Effective doses need to be determined, taking into account metabolic rates, drug interactions, and side effects. Prolonged drug use can cause tolerance and substance addiction.


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