RATH/PAULING U.S. PATENT # 5278189
SUMMARY OF THE INVENTION
The foregoing needs in the treatment and prevention of cardiovascular disease are met by the methods and compositions of the present invention.A method is provided for the treatment of occlusive cardiovascular disease , comprising the step of administering to a subject an effective amount of ascorbate and one or more binding inhibitors, as a mixture or as a compound comprising ascorbate covalently linked with binding inhibitors, which inhibit the binding of Lp(a) to blood vessel walls, such as arterial walls. This effect may also be obtained by administering an effective amount of one or more inhibitors, without ascorbate. The term binding inhibitor throughout the specification and claims is intended to include all substances that have an affinity for the lysine binding site present on the interior walls of blood vessels, particularly arteries, the site of Lp(a) binding. Most of these substances compete with plasmin for the lysine binding site and some of these compounds, in high doses, are in clinical use for the treatment of hyperfibrinolytic states.
A method is further provided for the prevention of atherosclerosis comprising the step of administering to a subject an effective amount of ascorbate and one or more binding inhibitors as previously discussed but further comprising one or more antioxidants. The term antioxidant throughout the specification and the claims is intended to exclude ascorbate which has as one of its chemical properties a potent antioxidant effect.
It is thus an object of the invention to provide a method for treatment of occlusive cardiovascular disease by administering to a subject an effective amount of ascorbate and one or more binding inhibitors, or an effective amount of one or a mixture of binding inhibitors.
It is another object of the invention to provide a method for preventing o f occlusive cardiovascular disease, by administering to a subject an amount of ascorbate effective to lower the amount of Lp(a) in the plasma of the subject.
Yet another object of the present invention is to provide a method for prevention of cardiovascular disease by administering to a subject an effective amount of ascorbate and one or more binding inhibitors, or an effective amount of one or more binding inhibitors.
A further object of the present invention is to provide a pharmaceutically acceptable agent for the treatment of occlusive cardiovascular disease.
Still another object of the present invention is to provide a pharmaceutically acceptable agent for the prevention of cardiovascular disease.
These and other objects will be more readily understood upon consideration of the following detailed descriptions of embodiments of the invention and the drawings.
DETAILED DESCRIPTION OF THE INVENTION
Our invention is based in part on our discovery that animals which have lost the ability to produce ascorbate, such as higher primates and guinea pigs, uniformly produce Lp(a). Most animals which possess the ability to synthesize ascorbate generally do not produce Lp(a).Further, we have found that ascorbate deficiency in humans and guinea pigs tends to raise Lp(a) levels and causes atherosclerosis by the deposition of Lp(a) in the arterial wall, from which we conclude that ascorbate administration lowers plasma Lp(a) levels.
We have also discovered that substances that inhibit the binding of Lp(a) to components of the arterial wall, particularly to fibrinogen, fibrin and fibrin degradation products herein identified as binding inhibitors, such as lysine or .epsilon.-aminocaproic acid used alone or in combination with ascorbate, cause release of Lp(a) from the arterial wall. Thus, ascorbate and such binding inhibitors are not only useful for the prevention of occlusive cardiovascular disease, but also for the treatment of such disease. The present invention, then, provides methods and pharmaceutical agents for the both the treatment and prevention of occlusive cardiovascular disease in vivo.
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Source: http://armyoflifesavers.blogspot.com/2012/10/scientific-health-journal-rathpauling.html
