Drug discovery is a time honored method to find new lead compounds.
New lead compounds are invariably derived from plants.
Plants are botanical treasure.
George Pieczenik invented the obscure field of molecular chemistry and called his inventions, combinatorial libraries.
A sampling of these libraries was intended to mirror Nature so that the libraries could be evaluated for receptor activity..
Its a system built on predictability because in theory it contains the complete inventory of all possibilities for the desired structure.
Pieczenik, in his patent application, submitted 3- 5 amino acids and the corresponding number of nucleic acids that would code for the chain, which he assumed was the length of the binding domain of the antibody.
Nature produce many similarly structured compounds, no where as extensive as science, but the plant has purpose in life and only creates what it needs.
These compounds differ from one another in one chemical position.
They are but a fraction of what could be created by science.
Researches can synthesize any one of the library of possibilities, but unlike Nature, they have no idea what it does.
Nature has a purpose and science is mathematical.
Drugs utilize the most limited version or any given volume of the plant it was derived from.
According to pharmaceutical science, it's the only one actually needed.
The program I describe on these pages, depends on plants to accomplish its goals,
Die young....as late in life as possible
The following information is provided to introduce the little known field of combinatorial chemistry to already well-informed readers.
The term library is used to describe a collection of molecules.
The library can have every possible combination of a given structure or be limited to a handful.
Combinatorial chemistry was invented to create all possibilities of any given structure.
As one of the few people who worked with Nobel laureate Bruce Merrifield and his student George Pieczenik, I feel uniquely qualified to apply it to plant biology.
Pieczenik invented the field, Merrifield told me himself.
Pupil exceeding the mentor.
Only Pieczenik got screwed
I feel responsible for promoting his work so that he receive the credit he is long over due.
He certainly was denied the profits from it.
In combinatorial chemistry, in the case where the molecules are the binding sites of antibodies, monoclonal antibodies are produced.
And when the molecules are the beta glucans of medicinal mushrooms, powerful anti-cancer drugs are produced.
Individualized cures and safer drugs were the goals of Pieczenik who invented the field as he fought in vain to discover a cure for his mother's breast cancer.
While his effort failed, it caused a paradigm shift in drug discovery
Unlike the synthetic combinatorial libraries that science invented, Nature, produces a more limited library containing only a few similarly structured compounds, each, producing opposing effects.
They differ chemically only slightly but their effect on the body is striking.
Unlike science, Nature does not need to produce the entire library of possibilities.
Nature has purpose.
Science is mathematical.
As a proponent of healing, I believe plants provide the best foods for athletes and extracts of their essence improve exercise performance and speed recovery.
Drugs mask symptoms without addressing the underlying problem.
I often prescribed drugs to manage inflammation and pain.
I still recommend them for acute conditions.
In chronic conditions, I turn to plants and natural products.
Drugs utilize a unique version or the active volume of the plant, its active agent.
According to pharmaceutical science, it's the only one actually needed.
The plant however, is the synthesizer of all of Nature’s compounds.
There are limited libraries in each plant.
Each library contains many unique chemicals, some of which we know about and some we do not.
The compounds contained in a plant are its phytochemicals (phyton from the Greek word for plant).
Phytochemicals are used as analgesics (willow bark), antibacterial (garlic) or anti-inflammatory agents (turmeric).
Plant compounds are also used as urinary antiseptics (cranberries), anti-ulcer (licorice) remedies and anti-cancer (mushrooms and soy) drugs.
Other phytochemicals improve health by stimulating the immune system (elderberries and mushrooms) or lower cholesterol (gugulipid bucktorn berries, red yeast rice) while still others are used to prevent and treat sunburn (aloe).
Nature doesn’t follow the independently probable rule.
Nature is preferential.
Patterns, when identified, lead to new discoveries.
The effects of botanicals are best explained by the theories of combinatorial chemistry and applying them to the concept of opposing cell receptors.
Receptors are capable of binding with a drugs, hormones or plant ligands.
Receptors are the molecular switches that turn on and off specific biological activities.
According to combinatorial theory, each unique conformation of chemically identical molecules can interact in opposing ways or on opposing receptors to effect change. It is precisely for this reason that whole plants are recommended. Whole plants produce more balanced results than those produced by the extracted solitary compound.
Whole plants are better than pharmaceutical drugs because of the inclusion of all the plant’s compounds, not just the one identified by researchers as active
Furthermore, modifying one of nature’s compounds in order to obtain a patent and thereby profit from it, as is the case with pharmaceutical drugs, removes some of the built in balances of the plant.
Could this be an explanation for the toxic side effects or addictive properties that pharmaceutical drugs are known to have?
Could this be the reason that the poppy flower and the coca leaf are less addictive than their refined and processed offspring (cocaine and heroin)?
While it is highly recommended to supplement the diet with extracts and colorful antioxidants, nothing can replace the balance of the original whole plant.
Botanical drugs are safe than pharmaceutical ones because they contain a series of compounds instead of just one.
As a series of molecules, they switch on different receptors based on the conditions at the time.
At another time or in another person, a different set of switches might be triggered.
This is the exact opposite to the mechanism of drugs, which achieve their result by overwhelming activity at one type of receptor.
A plant’s value to humans is due to the multitude of compounds synthesized, stored and extracted from it.
This is a natural library.
The library is a series of compounds that chemically differ slightly fom one another.
Since they either bind to, or do not bind, their opposing effects are in stark contrast to each other.
The result of proper bindings is normal growth and repair..
Faulty binding leads to malfunction and disease.
The uniqueness of each plant includes the color it displays and its medicinal properties. These characteristics can all be traced to the phytochemical compounds found in the plant’s cells.
The library of any specific plant contains multiple forms of similarly structured compounds. They are chemical cousins. Nature created this library of compounds via the DNA of the plant and locked them in the stems, roots, and leaves of plants.
The library of compounds are released when the plant is heated or its fibers eaten and exposed to the body’s digestive juices. Its molecules when free to be transported via the blood direct themselves to the sites of injury, inflammation and free radical generation. These compounds help humans survive.
Plants are provided with a universe of similarly structured chemical compounds so the plant can adapt to a changing environment. The effect any one of these compounds produce in humans is unrelated to its role in the plant’s health.
Plant activity is dependent on receptor binding, the same mechanism of hormones, neurotransmitters and drugs.
The cumulative effects of plants are almost always beneficial because nature’s creations are have a built in balance that drugs lack. Plants rarely produce harmful side effects because they contain multiple isoforms. Plants act in opposing manners precisely because their botanical compounds are found in multiple versions with differing spatial orientations.
The importance of multiple isoforms is that each form can bind with a different receptor. Sometimes an effect occurs only because a second or possibly third receptor is activated. This moderates their effects and makes them less harmful than manufactured drugs.
Nature created libraries of compounds, not solitary ones. Nature’s library provides the plant with a large volume of compounds. Some are active and others are supportive. Many have no known purpose but all are probably necessary.
The interaction that occurs within any cell is a result of a specific phytochemical binding with a specific receptor on a cell membrane. This has the effect of creating on/off switches or rather a series of switches.
Depending on the phytocompounds and the receptor involved, activity is directed by the receptor-ligand complex. It is through this interaction that changes within the cell occurs. The fact that variations in phytocompounds and receptors exist indicates that this variation in nature has a purpose.
Molecular reactions between receptors and ligands drive life’s processes. Whether it is between a hormone and a cell’s receptor, an enzyme and a substrate, or a nerve and a neurotransmitter, the key feature involves chemical bonds formed between a ligand and a receptor.
Other examples of binding between a receptor and a ligand include synapses, the movement of sodium and potassium ions across a neuronal membrane or vision and light, hearing and sound and touch and feel.
Nature’s Combinatorial Libraries describes the existence of a few, almost identical compounds in a plant. The purpose of slight variations or similar combinations of atoms may be related to the on and off switches of biological systems. Different sets of biological receptors counter each other and produce opposing effects.