Good News on the Bioavailability of Natural Medicines for the Treatment of Disease
2006 is going to be a banner year for natural medicines. And these are the reasons why.
First and foremost, more and more hardcore scientific research is being conducted on the biochemistry of these molecules. The research on natural medicines has simply exploded in the last few years.
Second, there are now improved methods of delivering these molecules into the body which increase their bioavailability. Folks, popping capsules is easy but it just doesn't work to get the compounds into the body.
A little history.
I met Tom Lahey of Lutimax Nutraceuticals over a year ago. He is a friend of a friend. I was initially very interested in how he got luteolin, Lutimax, to dissolve under the tongue and enter the body with a high degree of efficiency. Luteolin normally isn't that bioavailable. So I asked him and he told me.
At the time, I had developed a cancer treatment protocol that used EGCG, a polyphenol from green tea. 70% EGCG dissolved in coconut milk tastes terrible. The infamous Anna referred to it as YUCKKO and the name stuck. Most people simply couldn't stand the stuff. EGCG is a wonderful natural medicines but it stays in the intestines if you drink it as a bitter tea. We needed to get EGCG and other natural medicines into the lymphatic system where they would have greater contact with the cancer cells and escape degradation by the liver. Dissolving EGCG, etc. into coconut milk, which is high in fat, was my answer to the problem. Fat and molecules dissolved in fat enter the lymphatic system in the intestines instead of the blood. This is EXACTLY what we want.
Although curcumin and quercetin dissolve well in fat and do not taste bad, 70% EGCG is another story. It tastes horrible, pure and simple. I know the biochemistry of EGCG and its multiple effects on cancer cells, but what good does it do for me to develop treatment protocols that people simply will not follow. I am absolutely convinced that some people would rather die of cancer than drink YUCKKO.
Tom assured me that he could fix the problem, and he did. He developed a product called EGCGSyn that is combined with other ingredients that do target the lymphatic system. And it has no taste. Amazing...
Tom has continued to refine this technology and develop other SYN (his trademark) natural medicine products.
In addition to the SYN formulations, Tom has developed a Trojan Horse protocol for products such as quercetin that enhance bioavailability. Since it is important for the reader to understand why some natural medicine formulations work and others don't, Tom put the following essay together for me.
"All of us know too well that what happens with anything in the test tube rarely happens in the body. Hence we see thousands of animal studies and models for various diseases. Sometimes we never find the right way to get a compound to the target tissue. This is the issue of bioavailability, one of the biggest problems in western and natural medicine.
With bioflavonoids, specifically the flavones such as apigenin, baicalein, chrysin, luteolin, and the flavonols EGCG and quercetin, there is a major problem with bioavailability. Sometimes less than 1% of the amount of the molecule ends up being absorbed into the blood stream intact from the GI tract. The use of the chemical piperine from pepper, trade-named Bioprene, was a poor attempt at increasing bioavailability at the expense of the epithelial lining of the stomach, small intestine and bowels. Most of you are already familiar with this as these lipophilic or “fat loving” compounds barely dissolve in water. This is why we use coconut milk and other fats to promote the absorption of the bioflavonoids into the lymphatic tissue with the fats they dissolve in. And “Yuckko” was born. The taste is indescribably terrible, something you should all try once to appreciate how valuable some of our volunteers are and how far we have come.
In every person, the epithelial lining of the GI tract combines efforts with the liver (in this case a bad thing) to add sugar molecules to the compounds we ingest including bioflavonoids in an attempt to make them more water soluble for elimination in urine or feces. You see, the design is obvious, God knows that we do not have the knowledge of what to eat when we need it so we have this difficult system to override that protects us from ourselves. Complicating things further, bacteria in the gut and diet further add to the synthesis of lesser active compounds or metabolites. And if the compounds are mixed with foods with fiber, the compounds stay absorbed in that fiber. Most of the compounds are highly colored dye molecules that will obviously dye paper or fabric (cellulose, cotton, etc.) It is amazing that we can get any pharmacological effect from oral ingestion of anything.
Many of the compounds that come from fruits and vegetables already have a sugar molecule (or two and sometimes three) attached to them. When we look at the metabolism of these multiple-glycosylated compounds, we find they must be degraded either by hydrolysis in the stomach acid or by enzymes starting in the mouth to be absorbed. Now it gets better. We all know of the Trojan horse story of ancient Greece. SYNORx (Tom's principle company) has invented and patented the use of the multiple-glycosylated forms of a molecule (one that is most commonly used is rutin) to act as a Trojan horse for bioflavonoid delivery to get flavones and other compounds into the blood stream without losing their activity due to glycosylation or glucuronidation by the intestinal bacteria or epithelial lining of the gut.
This phenomenal method works because the epithelial cells see the molecule rutin as a two-sugar molecule plus a flavonol such as EGCG as a zero sugar molecule, but the average of two plus zero is one sugar molecule and the cells leave the EGCG or other flavonoids of similar structure alone. Another way to look at it is that the same enzymes that add sugar also taketh away. And their job is to add one. If there are two, they are busy taking away one and the molecule with zero gets to slip by the smokescreen, if you will. This is called competitive inhibition.
The following articles detail the metabolism of quercetin, a zero sugar molecule, its one-sugar buddy isoquercitrin, and its two-sugar buddy rutin. The articles show three separate pharmacokinetic curves that overlap each other to give a form of time-release formula and when the reverse reactions of enzymatic hydrolysis are considered for rutin to go to quercetin, we see the enhanced bioavailability of pure quercetin from a combination of rutin and quercetin. Enough to get dramatically higher plasma levels of the bioflavonoid to the tissues that need it, enough to reduce TNF-alpha, NK-KB, and the symptoms of inflammatory bowel disease:
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&
db=pubmed&dopt=Abstract&
list_uids=16132362&query_hl=24&itool=pubmed_docsum
And to stop p-Gp pumps from rejecting drug delivery of other compounds to the tissues that need these drugs:
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&
db=pubmed&dopt=Abstract&
list_uids=16259758&query_hl=24&itool=pubmed_docsum
And the combination of glucosides and their flavones start getting absorbed even in the mouth:
http://www.nutrition.org/cgi/reprint/135/1/48
So now you know why SYNORx has rutin and/or a glycoside of the compounds in every bioflavonoid formula they make under US Patent 6,774,142. "
In brief, if you combine certain other compounds with quercetin and other natural medicines, it ties up the liver and promotes the half life of quercetin, etc. in the body. To my knowledge, Tom is the only supplement manufacturer who does this.
The next Blog will provide additional information on Tom's products and how to contact him.
Stay tuned...
Grouppe Kurosawa, Medicine in the Public Interest
(http://www.grouppekurosawa.com)
First and foremost, more and more hardcore scientific research is being conducted on the biochemistry of these molecules. The research on natural medicines has simply exploded in the last few years.
Second, there are now improved methods of delivering these molecules into the body which increase their bioavailability. Folks, popping capsules is easy but it just doesn't work to get the compounds into the body.
A little history.
I met Tom Lahey of Lutimax Nutraceuticals over a year ago. He is a friend of a friend. I was initially very interested in how he got luteolin, Lutimax, to dissolve under the tongue and enter the body with a high degree of efficiency. Luteolin normally isn't that bioavailable. So I asked him and he told me.
At the time, I had developed a cancer treatment protocol that used EGCG, a polyphenol from green tea. 70% EGCG dissolved in coconut milk tastes terrible. The infamous Anna referred to it as YUCKKO and the name stuck. Most people simply couldn't stand the stuff. EGCG is a wonderful natural medicines but it stays in the intestines if you drink it as a bitter tea. We needed to get EGCG and other natural medicines into the lymphatic system where they would have greater contact with the cancer cells and escape degradation by the liver. Dissolving EGCG, etc. into coconut milk, which is high in fat, was my answer to the problem. Fat and molecules dissolved in fat enter the lymphatic system in the intestines instead of the blood. This is EXACTLY what we want.
Although curcumin and quercetin dissolve well in fat and do not taste bad, 70% EGCG is another story. It tastes horrible, pure and simple. I know the biochemistry of EGCG and its multiple effects on cancer cells, but what good does it do for me to develop treatment protocols that people simply will not follow. I am absolutely convinced that some people would rather die of cancer than drink YUCKKO.
Tom assured me that he could fix the problem, and he did. He developed a product called EGCGSyn that is combined with other ingredients that do target the lymphatic system. And it has no taste. Amazing...
Tom has continued to refine this technology and develop other SYN (his trademark) natural medicine products.
In addition to the SYN formulations, Tom has developed a Trojan Horse protocol for products such as quercetin that enhance bioavailability. Since it is important for the reader to understand why some natural medicine formulations work and others don't, Tom put the following essay together for me.
"All of us know too well that what happens with anything in the test tube rarely happens in the body. Hence we see thousands of animal studies and models for various diseases. Sometimes we never find the right way to get a compound to the target tissue. This is the issue of bioavailability, one of the biggest problems in western and natural medicine.
With bioflavonoids, specifically the flavones such as apigenin, baicalein, chrysin, luteolin, and the flavonols EGCG and quercetin, there is a major problem with bioavailability. Sometimes less than 1% of the amount of the molecule ends up being absorbed into the blood stream intact from the GI tract. The use of the chemical piperine from pepper, trade-named Bioprene, was a poor attempt at increasing bioavailability at the expense of the epithelial lining of the stomach, small intestine and bowels. Most of you are already familiar with this as these lipophilic or “fat loving” compounds barely dissolve in water. This is why we use coconut milk and other fats to promote the absorption of the bioflavonoids into the lymphatic tissue with the fats they dissolve in. And “Yuckko” was born. The taste is indescribably terrible, something you should all try once to appreciate how valuable some of our volunteers are and how far we have come.
In every person, the epithelial lining of the GI tract combines efforts with the liver (in this case a bad thing) to add sugar molecules to the compounds we ingest including bioflavonoids in an attempt to make them more water soluble for elimination in urine or feces. You see, the design is obvious, God knows that we do not have the knowledge of what to eat when we need it so we have this difficult system to override that protects us from ourselves. Complicating things further, bacteria in the gut and diet further add to the synthesis of lesser active compounds or metabolites. And if the compounds are mixed with foods with fiber, the compounds stay absorbed in that fiber. Most of the compounds are highly colored dye molecules that will obviously dye paper or fabric (cellulose, cotton, etc.) It is amazing that we can get any pharmacological effect from oral ingestion of anything.
Many of the compounds that come from fruits and vegetables already have a sugar molecule (or two and sometimes three) attached to them. When we look at the metabolism of these multiple-glycosylated compounds, we find they must be degraded either by hydrolysis in the stomach acid or by enzymes starting in the mouth to be absorbed. Now it gets better. We all know of the Trojan horse story of ancient Greece. SYNORx (Tom's principle company) has invented and patented the use of the multiple-glycosylated forms of a molecule (one that is most commonly used is rutin) to act as a Trojan horse for bioflavonoid delivery to get flavones and other compounds into the blood stream without losing their activity due to glycosylation or glucuronidation by the intestinal bacteria or epithelial lining of the gut.
This phenomenal method works because the epithelial cells see the molecule rutin as a two-sugar molecule plus a flavonol such as EGCG as a zero sugar molecule, but the average of two plus zero is one sugar molecule and the cells leave the EGCG or other flavonoids of similar structure alone. Another way to look at it is that the same enzymes that add sugar also taketh away. And their job is to add one. If there are two, they are busy taking away one and the molecule with zero gets to slip by the smokescreen, if you will. This is called competitive inhibition.
The following articles detail the metabolism of quercetin, a zero sugar molecule, its one-sugar buddy isoquercitrin, and its two-sugar buddy rutin. The articles show three separate pharmacokinetic curves that overlap each other to give a form of time-release formula and when the reverse reactions of enzymatic hydrolysis are considered for rutin to go to quercetin, we see the enhanced bioavailability of pure quercetin from a combination of rutin and quercetin. Enough to get dramatically higher plasma levels of the bioflavonoid to the tissues that need it, enough to reduce TNF-alpha, NK-KB, and the symptoms of inflammatory bowel disease:
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&
db=pubmed&dopt=Abstract&
list_uids=16132362&query_hl=24&itool=pubmed_docsum
And to stop p-Gp pumps from rejecting drug delivery of other compounds to the tissues that need these drugs:
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&
db=pubmed&dopt=Abstract&
list_uids=16259758&query_hl=24&itool=pubmed_docsum
And the combination of glucosides and their flavones start getting absorbed even in the mouth:
http://www.nutrition.org/cgi/reprint/135/1/48
So now you know why SYNORx has rutin and/or a glycoside of the compounds in every bioflavonoid formula they make under US Patent 6,774,142. "
In brief, if you combine certain other compounds with quercetin and other natural medicines, it ties up the liver and promotes the half life of quercetin, etc. in the body. To my knowledge, Tom is the only supplement manufacturer who does this.
The next Blog will provide additional information on Tom's products and how to contact him.
Stay tuned...
Grouppe Kurosawa, Medicine in the Public Interest
(http://www.grouppekurosawa.com)
1 Comments:
This is one of your best blogs ever! I finally understand the bioavailability thing-y and why drugs are so often not effective. Thank you.
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