Re: [CH] Reasearching
Art Pierce (pierces@cruzio.com)
Thu, 30 Nov 2000 02:07:09 -0800
>Local newspaper reports that a researcher at the University of Tasmania has
>just secured a $A195000 grant (roughly 87 cents US??) to research the
>"analgesic properties" of chillies. Apparently he has been looking into
>this for 10 years and funding is for a further 3 years.
>Goes to show - everyone seems to be becoming interested in the little devils
>Cheers from Tassie
>Dale
Dale,
They've been using capsaicin (as chile pulp) in vaseline on horses' joints for a
LONG time. And as analgesics for various things in humans at least 15 years.
Look at the price of 0.025% cap ointment (OTC) at your local drugstore
http://www.dermstore.com/Zostrix.htm
and you'll know why the pharmacological industry is looking into patentable
(read: really expensive) cap analog creams, etc. There has been a lot of ongoing
research in this area since before 1990. And a lot more, recently.
E.g.,
DEPARTMENT OF HEALTH AND HUMAN SERVICES
National Institutes of Health
Government-Owned Inventions; Availability for Licensing
AGENCY: National Institutes of Health, HHS.
ACTION: Notice.
-----------------------------------------------------------------------
The inventions listed below are owned by agencies of the U.S.
Government and are available for licensing in the U.S. in accordance
with 35 U.S.C. 207 to achieve expeditious commercialization of results
of federally-funded research and development. Foreign patent
applications are filed on selected inventions to extend market coverage
for U.S. companies and may also be available for licensing.
Vanilloid Agonists for Desensitization of C-Fiber Sensory Afferent Neurons
PM Blumberg, T Biro, P Acs, G Acs (NCI)
Serial No. 60/030,999 filed 15 Nov 96
Licensing Contact: Leopold J. Luberecki, Jr., 301/496-7735 ext 223
Capsaicin has been proven to have therapeutic utility in the
treatment of arthritis, pruritis, bladder hyperreflexia, allergic
responses including rhinitis, and pain, including pain associated with
cancer, peripheral neuropathies, and postherpetic neuralgia. For a
number of these indications, applications have been found in veterinary
as well as human medicine. Recent advances have identified capsaicin
analogs with ultrapotency and with a more favorable spectrum of action,
as well as subclasses of capsaicin receptors with different effects on
desensitization. This invention describes a method of administering to
a capsaicin-sensitive animal
(it's not for the birds)
a therapeutically effective combination of
capsaicin agonists and capsaicin-like antagonists which are more
effective than the agonist alone at desensitizing a vanilloid
responsive cell,
('desensitizing' is what we chileheads call 'blessed endorphin-releasing, addictive heat')
and thereby improve the therapeutic index of the
capsaicin agonist and overall treatment. Also described are
pharmaceutical compounds which are effective in this method.
(portfolios: Central Nervous System--Therapeutics, neurological,
narcotics and analgesics; Internal Medicine--Therapeutics, other)
~~~
Cap from cayenne
http://onhealth.webmd.com/alternative/resource/herbs/item,15962.asp
~~~
At the Univ. of Wisconsin
The chemistry department will host a seminar entitled "Synthesis of N-Vanillyl para-Alkyl Cinnamamides
as Analogs of Capsaicin: Potential New Analgesic Agents" on Friday, Feb. 12, at 3 p.m. in 271 CSH.
Capsaicin is well known as the pungent substance present in hot red chilli peppers. It has also been used
to produce pain relief in certain conditions such as arthritis or shingles. The structure of capsaicin contains
a) an aromatic vanillyl group, b) an intermediate amide group, and c) a long nonpolar chain.
In an attempt to produce new compounds which may have fewer side effects, a series of capsaicin analogs
having a substituted cinnamic acid structure in place of the long nonpolar chain were synthesized.
Ms. Kelly Kuehlwein, UW-RF chemistry major, will make the presentation.
Refreshments will be provided by the Chem Club.
(Beware the refreshments.)
http://www.uwrf.edu/~dr04/
~~~
Mouth & throat pain reliever
http://www.biomedpatent.com/5762963.htm
~~~
Pepper spray, using nordihydrocapsaicin to increase! the heat of capsaicin
http://www.netsci.org/Science/Compchem/feature19.html
Maybe some of the makers of the hottest sauces will find this out and save money.
~~~
New capsaicinoids being constructed at the Univ. of Shizuoka in Japan by
Kobata, K., Toyoshima, M., Kawamura, M., Watanabe, T. Lipase-catalyzed synthesis of capsaicin analogs
using natural oils as an acyl donor," Biotechnol. Lett. 1998, 20, 781-783.
~~~
And in Korea (look at his 3rd publication)
http://chem.korea.ac.kr/~synthesis/english/professor.html
~~~
Sports 'medicine'
(Maybe your testing lab will be looking for nanolitres of this in
the athletes' blood & urine next time the Olympics come to Oz.)
Swimming Capacity of Mice Is Increased by Oral Administration
of a Nonpungent Capsaicin Analog, Stearoyl Vanillylamide
Intravenous injection of stearoyl vanillylamide (C18-VA), a nonpungent capsaicin (CAP)
analog, enhances adrenaline secretion significantly and as effectively as CAP in rats. Because
swimming capacity was enhanced by CAP in mice due to CAP-induced adrenal catecholamine
secretion, researchers investigated the effects of oral administration of C18-VA on swimming
capacity using an adjustable-current water pool.
Male, 6-wk-old mice were fed a commercial diet for this study and one group was orally
administered C18-VA via a stomach tube. Treated mice were able to swim longer before
exhaustion than the control mice (62.9 min. vs. 49.6). The swimming capacity of two groups
administered C18-VA (0.02 and 0.033 mmol/kg) was significantly greater than that of those
administered vehicle alone. Substance P concentration in cerebrospinal fluid, which is involved
in pain transmission and is the first direct measure of pungency, was not affected by C18-VA
administration.
In an experiment examining the effects of C18-VA on serum adrenaline concentration,
adrenaline was significantly greater in C18-VA treated mice than in controls at 2-h post-dose.
In a separate study free fatty acids in serum were elevated in treated mice at 2-h post-dose.
While serum glucose concentration was not affected. These results suggest that C18-VA
increased swimming capacity of mice via adrenaline release, independent of pungency. In
addition, the present study suggests the usefulness of its application to humans.
Stearoyl Vanillylamide is an analog of capsaicin, a major component of red pepper. Capsaicin
has been shown to enhance exercise performance by increasing the release of adrenaline.
Adrenaline increases the availability of free fatty acids (enhances fat breakdown) and therefore
may increase performance.
In humans, however, the use of capsaicin is impractical
('impractical' doesn't quite cut it)
since it would take approximately 100 grams to have a significant effect. It is unlikely
(nor does 'unlikely')
that a dose this high could be tolerated.
Therefore capsaicin analogs that are not as pungent are an attractive alternative. Stearoyl
Vanillylamide fits this description. The present study showed that Stearoyl Vanillylamide
increased swim performance, adrenaline, and free fatty acid concentrations. It is unknown
whether Stearoyl Vanillylamide has the same effect in humans. Since Stearoyl Vanillylamide is
less pungent than capsaicin it may be better tolerated by humans.
The Journal of Nutrition Vol. 128 No. 11 November 1998, pp. 1978-1983
~~~
Anyway, you get the drift of the on-going research.
Art