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1.1 General Information
Enzyme inhibitors/suppressants are molecules which attach to and interact with enzymes and interfere with their proper function, which is to break down organic matter into smaller molecules to be used as energy. Enzyme inhibitors are found in numerous commercially manufactured medications, but they are also found naturally within nuts and seeds. Enzyme inhibitors are also used in certain poisons and narcotics.
There are four primary types of enzyme inhibitor:
Nonspecific inhibition affects all enzymes in the same way. Non-specific methods of inhibition include any physical or chemical changes which ultimately denature the protein portion of the enzyme and are therefore irreversible.
Specific Inhibitors exert their effects upon a single enzyme. Most poisons function by specific inhibition of enzymes. Specific enzyme inhibitors can also be classified under Selective Enzyme Inhibition. Specific enzyme inhibitors have many applications in treating disease and are found in many medications, including penicillin and vancomycin.
Competitive inhibitors are any compounds that closely resemble the chemical structure and molecular geometry of the substrate. The inhibitor competes for the same active site as the substrate molecule. The inhibitor may interact with the enzyme at the active site, but no reaction takes place. The inhibitor is "stuck" on the enzyme and prevents any substrate molecules from reacting with the enzyme. However, a competitive inhibition is usually reversible if sufficient substrate molecules are available to ultimately displace the inhibitor. Therefore, the amount of enzyme inhibition depends upon the inhibitor concentration, substrate concentration, and the relative affinities of the inhibitor and substrate for the active site.
Noncompetitive inhibitors are substances that interact with the enzyme, but usually not at the active site. Â The noncompetitive inhibitor reacts either remote from or very close to the active site. Â The net effect of a non competitive inhibitor is to change the shape of the enzyme and thus the active site, so that the substrate can no longer interact with the enzyme to give a reaction. Non competitive inhibitors are usually reversible, but are not influenced by concentrations of the substrate as is the case for a reversible competitive inhibitor.
Above Text Adapted from Elmhurst College - Virtual Chembook 2003 (http://www.elmhurst.edu/~chm/vchembook/573inhibit.html)
1.2 SCI Specific-Competitive Inhibitor Extract (ESCIe)
The utilization of a non-specific inhibition extract could be extremely damaging within the body as it would interfere with the function of normal digestive and metabolic enzymes emitted by human cells. Noncompetitive inhibition extracts could also be dangerous to use due to the possibility of irreversibility and permanent paralysis of cell function.
Certain types of raw nuts and seeds contain phytic acid, and produce active enzyme inhibitors which in many cases prevent digestive and metabolic enzymes from functioning properly. In order to remove these potentially harmful inhibitors and toxins, nuts and seeds are normally soaked in water and dehydrated for predetermined periods of time to neutralize the effects of enzyme inhibitors and severely diminish the levels of phytic acid before being packaged or sold (in commercial environments).
The use of an experimental Specific-Competitive Inhibitor Substance based largely on phytic acid and naturally occurring enzyme inhibitors may prove to be an extremely deadly substance to bacterial colonies, primarily due to the high levels of available inhibitor within certain types of nuts, namely walnuts and pecans.
However, some types of nuts with higher levels of enzyme inhibitor are nearly impossible to obtain in raw form as they are normally processed immediately after harvest, thus destroying the opportunity to extract viable substances. To allow for the maximum available inhibitor to be used, a variety of other enzyme inhibition sources from processed bacterial byproducts will be included. The ESCIe will be administered to several types of predetermined bacterial colonies and the effects on the test subjects will be examined as opposed to the effects on the control group test subjects, which will be administered a common hand sanitizer solution
1.3 Function of ESCIe Medication
The use of an ESCIe Specific-Competitive medication would result in the impediment of certain catalytic functions and prevent substrates from binding to certain types of enzymes.
The above illustration (Fig. 1) demonstrates the normal interaction of a substrate with a single enzyme. Substrates (portrayed by triangles) bind to the enzyme in designated locations.
However, when the Specific-Competitive ESCIe inhibitor molecules are introduced, the substrates are unable to bond with the enzyme as the S-C inhibitors selectively chose the bacterial enzyme to compete with the substrates. Without substrates, the ability of the enzyme to break down organic matter is drastically decreased, making it extremely difficult for the bacteria to obtain energy, which leads to death (see Figure 5).
1.4 ESCIe Fully "Reversible" Medications
ESCIe could result in a "reversible" medication based on existing natural and engineered enzyme
inhibitors that specifically and competitively suppresses enzyme function in pathogens including
bacterial infections, viral infections, cancerous tumors, and other harmful foreign diseases.
This would be accomplished by an ESCIe molecule bonding to a pathogenic enzyme and competing with the substrates which would otherwise metabolize organic matter. If any unintended adverse side effects were to occur while using the medication, then the enzyme inhibition would be completely reversible through the utilization of large numbers of substrate molecules to dislodge the inhibitor from the foreign object. The reversibility of an ESCIe would be a great improvement over conventional medications, which require more substances to neutralize any negative effects.
Illustrations of the Basic Effect of an Inhibitor on Bacterial Enzymes
All bacteria and living cells require digestive and metabolic enzymes to break down organic matter into smaller molecules to be consumed as energy.
However, the use of Specific-Competitive Inhibitor (ESCIe) would prevent the proper function of certain strains of bacteria within the body.
Due to the enzyme inhibitor, the digestive enzymes cannot break down the organic matter to obtain energy, and the bacteria will starve and die.
1.5 ESCIe Medications and Allergies
The growing number of people with nut allergies presents a problem in the distribution and administration of an ESCIe. To combat this, a seed-based nut free ESCIe would be utilized. However, the concentration of the enzyme inhibitors within this medication would be decreased, and the patient would require additional medications other than the ESCIe alone to combat illness.
Other medications that function by utilizing types of enzyme inhibition include penicillin, an antibiotic, and vancomycin, used to treat colitis which sometimes occurs after antibiotic treatment.
However, the use of an ESCIe nut-based medication could be very useful for people that are allergic to medications such as penicillin and others as a way to fight bacterial infections without the use of antibiotics.
1.6 Elimination of Antibiotic Abuse and Prevention of Mutation in Pathogens
The overuse of antibiotics can and has led to genetic mutation in the past. Due to antibiotic abuse, certain bacteria strains and other pathogens have developed immunity to the most powerful medications. Among the most notable genetically mutated diseases is MRSA, Methicillin-resistant Staphylococcus aureus, which is usually found in hospital environments and is very difficult to treat due to its resistance to the most powerful medications. The use of an enzyme inhibition based medication, however, will not be likely to cause any type of genetic response within pathogens if used properly. The correct use of ESCIe medicine will most likely protect against any man-made "superbugs" that were created due to antibiotic overuse.
1.7 Possible Application of ESCIe in the Treatment of Cancerous Cells
All living cells require digestive and metabolic enzymes to obtain vital energy. The use of a Specific-Competitive enzyme inhibitor could be able to differentiate cancerous cells and decrease the activity of their enzymes while not interfering with the function of normal cells within the body. The use of enzyme inhibitors has been employed to an extent in the cancer treatment chemotherapy. An ESCIe based cancer treatment could theoretically yield generally positive results in a clinical trial.
2.1 Penicillin and Other Antibiotics
Penicillin, developed by Alexander Fleming in 1928, was the first antibiotic that was proven to be effective against bacterial infections such as Staphylococcus and others that were, before its creation, basically untreatable. Penicillin is derived from penicillium fungi which most often appear in moderate climates, and destroys bacterial infections by binding to the enzyme DD-transpeptidase, thus weakening the cell wall.
Penicillin has become the standard for treating many types of bacterial infection, and is the most manufactured antibiotic in history. However, numerous bacteria species have developed resistance to penicillin and antibiotics by rapid evolution.
Image Source: Wikipedia Entry - Penicillin (http://en.wikipedia.org/wiki/File:Penicillin_core.svg)
Figure 7 is an illustration of the chemical structure of Penicillin, in which R is indicated to be a variable group(s).
There are several adverse side effects of penicillin, including nausea, diarrhea, hypersensitivity, neurotoxicity, and