EMBARGOED UNTIL
12:01 AM EDT/Friday, April 17, 2009
Contact: Donna Krupa
Newsroom: (504) 670-4525 or 4526
Office: (301) 634-7209
Cell: (703) 967-2751
dkrupa@the-aps.org
“ANTEDRUGS”: A Safer Approach To Drug Therapy
One lab’s
groundbreaking approach to tailoring drugs that meet only a specific target
within the body has focused on anti-inflammatory, anti-AIDS and anti-cancer
drugs since 1982
NEW ORLEANS—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
The Study
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.
Results
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.
NOTE TO EDITORS: The APS annual meeting is part
of the Experimental Biology 2009 (EB ’09) gathering and will be held April
18-22, 2009 at the New Orleans Convention Center. To schedule an interview
with either Dr. Lee or Errahali, please contact Donna Krupa at
301.634.7209 (office), 703.967.2751 (cell) or
DKrupa@the-APS.org.
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