Corticosteroids are powerful drugs used to treat inflammatory conditions such as asthma and other chronic diseases which has made them among the most widely prescribed drugs.
Although the anti-inflammatory drugs offer swift relief to the patient, they can carry with them serious side effects. For example, the inflammatory steroids used to treat a child’s asthma, but can stunt the child’s growth over time. Similarly, adult treatment of Addison’s disease, which President John F. Kennedy endured, can lead to the development of diabetes and hypertension.
For more than 20 years, one research team has been working to develop a safer approach that would eliminate inflammation without causing damage to the body. Such drugs, called “antedrugs” have been developed in a lab at Florida A&M’s College of Pharmacy. The efforts have been spearheaded by Dr. Henry J. Lee who has led antedrug research in anti-inflammatory, anti-AIDS and anti-cancer drugs for nearly 30 years.
A New Study
Lee and his team have recently completed a new study entitled, Anti-Inflammatory Activities of New Steroidal Antedrugs Isoxazoline Derivatives. It was conducted by Drs. Henry J. Lee, Younes J. Errahali, LeeShawn D. Thomas, Brenda G. Arnold and Glory B. Brown, all of the Florida Agricultural and Mechanical University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, Florida. The researchers will discuss their work at the 122nd Annual Meeting of the American Physiological Society (APS; www.the-APS.org/press) which is part of the Experimental Biology 2009 scientific conference. The meeting will be held April 18-22, 2009 in New Orleans.
Antedrug design is a new approach to create safer drugs that attack a problem such as inflammation then quickly become inactive before they can cause damage. The primary objective of this study was to synthesize a new group of corticosteroids that have anti-asthmatic and anti-inflammatory properties without adverse side effects.
The researchers synthesized new antedrugs, isoxazoline derivatives, from prednisolone. They then tested the derivatives in a test tube and found that antedrugs effectively reduced inflammation. In fact, they found isoxazoline derivatives were five times more potent than prednisolone in binding affinities to the cell corticosteroids receptors and reducing inflammation.
The researchers also studied the isoxazoline derivatives in the lung and liver cells of rats and found that the antedrugs significantly reduced the cell inflammation. In addition, the rat plasma began metabolizing rapidly the antedrugs to an inactive form with the half lives less than five minutes and more than 95% of prednisolone remained unchanged even after 100 min incubation.
These results suggest that isoxazoline derivatives compared to conventional steroids improve topical anti-inflammatory activity without causing systemic damage. “This is a very promising outcome,” according to Dr. Lee. Additional studies are currently underway, using a new group of corticosteroids in the treatment of asthma exacerbation and chronic pulmonary inflammation without systemic side effects such as body weight and hypothalamic-pituitary-adrenal axis change.
This project research described was supported by the National Institutes of Health, 5S06GM008111-36 NIGMS/MBRS and 2G12RR03020-24 / NCRR/RCMI. The content is solely the responsibility of the authors and does not necessarily represent the official views of the NCRR, NIGMS or the NIH.
Physiology is the study of how molecules, cells, tissues and organs function to create health or disease. The American Physiological Society (APS; www.The-APS.org/press) has been an integral part of this discovery process since it was established in 1887.
Donna Krupa | EurekAlert!
New study: How does Europe become a leading player for software and IT services?
03.04.2017 | Fraunhofer-Institut für System- und Innovationsforschung (ISI)
Reusable carbon nanotubes could be the water filter of the future, says RIT study
30.03.2017 | Rochester Institute of Technology
More and more automobile companies are focusing on body parts made of carbon fiber reinforced plastics (CFRP). However, manufacturing and repair costs must be further reduced in order to make CFRP more economical in use. Together with the Volkswagen AG and five other partners in the project HolQueSt 3D, the Laser Zentrum Hannover e.V. (LZH) has developed laser processes for the automatic trimming, drilling and repair of three-dimensional components.
Automated manufacturing processes are the basis for ultimately establishing the series production of CFRP components. In the project HolQueSt 3D, the LZH has...
Reflecting the structure of composites found in nature and the ancient world, researchers at the University of Illinois at Urbana-Champaign have synthesized thin carbon nanotube (CNT) textiles that exhibit both high electrical conductivity and a level of toughness that is about fifty times higher than copper films, currently used in electronics.
"The structural robustness of thin metal films has significant importance for the reliable operation of smart skin and flexible electronics including...
The nearby, giant radio galaxy M87 hosts a supermassive black hole (BH) and is well-known for its bright jet dominating the spectrum over ten orders of magnitude in frequency. Due to its proximity, jet prominence, and the large black hole mass, M87 is the best laboratory for investigating the formation, acceleration, and collimation of relativistic jets. A research team led by Silke Britzen from the Max Planck Institute for Radio Astronomy in Bonn, Germany, has found strong indication for turbulent processes connecting the accretion disk and the jet of that galaxy providing insights into the longstanding problem of the origin of astrophysical jets.
Supermassive black holes form some of the most enigmatic phenomena in astrophysics. Their enormous energy output is supposed to be generated by the...
The probability to find a certain number of photons inside a laser pulse usually corresponds to a classical distribution of independent events, the so-called...
Microprocessors based on atomically thin materials hold the promise of the evolution of traditional processors as well as new applications in the field of flexible electronics. Now, a TU Wien research team led by Thomas Müller has made a breakthrough in this field as part of an ongoing research project.
Two-dimensional materials, or 2D materials for short, are extremely versatile, although – or often more precisely because – they are made up of just one or a...
20.04.2017 | Event News
18.04.2017 | Event News
03.04.2017 | Event News
26.04.2017 | Materials Sciences
26.04.2017 | Agricultural and Forestry Science
26.04.2017 | Physics and Astronomy