Lupeol. The Newest Natural Medicine Anti-Cancer Compound. The Curcumin Connection
One of the members of our discussion group brought this compound to my attention. So I did a little background research.
Lupeol is a triterpene compound found in many plants. At low concentrations, it has a remarkable ability to inhibit the synthesis of the testosterone receptor and to induce the expression of the FAS killing pathway in prostate cancer cells.
http://www.ncbi.nlm.nih.gov/entrez/queryd.fcgi?cmd=Retrieve&db=pubmed&
dopt=Abstract&list_uids=16322271&itool=pubmed_docsum
Ordinarily, I don't get too excited about the so-called anti-cancer properties of most natural medicines, because the dose required is invariably too high. This makes the compound clinically useless.
Lupeol is different. It has true biological activity in doses as low as 10 microMolar. Further, it appears to induce the expression of the FAS receptor on prostate cancer cells. Since lupeol kills other cells as well, it might be a universal inducer of FAS receptor expression. This is a BIG deal if true.
In addition, lupeol has been shown to kill pancreatic cancer cells by inhibiting the RAS signaling pathway. I've talked about RAS many times. Quercetin interferes with this pathway also. RAS mutants or cells that overexpress RAS are involved in 60% of ALL cancers and leukemias.
http://www.ncbi.nlm.nih.gov/entrez/queryd.fcgi?cmd=Retrieve&db=pubmed&
dopt=Abstract&list_uids=15958516&itool=pubmed_docsum
Let's talk about FAS for a moment.
FAS is one of three death pathways that are involved in initiating programmed cell death in cancer cells. There are two components to the system. First, the cancer cells MUST express the FAS receptor on its membrane. Most don't. Second, FAS ligand is a protein, often expressed on the membranes of immune cells, that must bind and activate the FAS receptor.
Increasing the expression of FAS on cancer cells is great. BUT, if we have no way to activate the FAS receptor, we are effectively screwed. Activating FAS ligand synthesis, the normal activator of the FAS receptor, is out of the question. Way too complicated.
But there is hope. Remember our friend curcumin? Guess what it does.
I have previously reported that curcumin was a potential treatment for melanoma since melanoma cells, unlike most cancer cells, expresses a substantial amount of FAS on its membranes. Unlike lupeol, curcumin does not increase the expression of FAS in the membranes of cancer cells. Instead, it substitutes for FAS ligand by cross linking the FAS receptors, thereby inducing their activation and cell death.
http://www.ncbi.nlm.nih.gov/entrez/queryd.fcgi?cmd=Retrieve&db=pubmed&
dopt=Abstract&list_uids=11716543&itool=pubmed_docsum
Lupeol also induces FADD synthesis which binds the interior portion of the FAS receptor and promotes its cell killing activities. See first article.
Curcumin and lupeol definitely look like a dynamic duo.
Lupeol is found in many fruits, vegetables and herbs including olives, strawberries, mangoes and figs. Unfortunately, there are no commercial sources for this natural compound to date.
However, lupeol acetate, a soluble form of this compound, is made in Germany. I am looking into it. Maybe I can import it.
Anyone know of another source of lupeol other than fresh fruit?
Stay tuned...
Grouppe Kurosawa, Medicine in the Public Interest
(http://www.grouppekurosawa.com)
Lupeol is a triterpene compound found in many plants. At low concentrations, it has a remarkable ability to inhibit the synthesis of the testosterone receptor and to induce the expression of the FAS killing pathway in prostate cancer cells.
http://www.ncbi.nlm.nih.gov/entrez/queryd.fcgi?cmd=Retrieve&db=pubmed&
dopt=Abstract&list_uids=16322271&itool=pubmed_docsum
Ordinarily, I don't get too excited about the so-called anti-cancer properties of most natural medicines, because the dose required is invariably too high. This makes the compound clinically useless.
Lupeol is different. It has true biological activity in doses as low as 10 microMolar. Further, it appears to induce the expression of the FAS receptor on prostate cancer cells. Since lupeol kills other cells as well, it might be a universal inducer of FAS receptor expression. This is a BIG deal if true.
In addition, lupeol has been shown to kill pancreatic cancer cells by inhibiting the RAS signaling pathway. I've talked about RAS many times. Quercetin interferes with this pathway also. RAS mutants or cells that overexpress RAS are involved in 60% of ALL cancers and leukemias.
http://www.ncbi.nlm.nih.gov/entrez/queryd.fcgi?cmd=Retrieve&db=pubmed&
dopt=Abstract&list_uids=15958516&itool=pubmed_docsum
Let's talk about FAS for a moment.
FAS is one of three death pathways that are involved in initiating programmed cell death in cancer cells. There are two components to the system. First, the cancer cells MUST express the FAS receptor on its membrane. Most don't. Second, FAS ligand is a protein, often expressed on the membranes of immune cells, that must bind and activate the FAS receptor.
Increasing the expression of FAS on cancer cells is great. BUT, if we have no way to activate the FAS receptor, we are effectively screwed. Activating FAS ligand synthesis, the normal activator of the FAS receptor, is out of the question. Way too complicated.
But there is hope. Remember our friend curcumin? Guess what it does.
I have previously reported that curcumin was a potential treatment for melanoma since melanoma cells, unlike most cancer cells, expresses a substantial amount of FAS on its membranes. Unlike lupeol, curcumin does not increase the expression of FAS in the membranes of cancer cells. Instead, it substitutes for FAS ligand by cross linking the FAS receptors, thereby inducing their activation and cell death.
http://www.ncbi.nlm.nih.gov/entrez/queryd.fcgi?cmd=Retrieve&db=pubmed&
dopt=Abstract&list_uids=11716543&itool=pubmed_docsum
Lupeol also induces FADD synthesis which binds the interior portion of the FAS receptor and promotes its cell killing activities. See first article.
Curcumin and lupeol definitely look like a dynamic duo.
Lupeol is found in many fruits, vegetables and herbs including olives, strawberries, mangoes and figs. Unfortunately, there are no commercial sources for this natural compound to date.
However, lupeol acetate, a soluble form of this compound, is made in Germany. I am looking into it. Maybe I can import it.
Anyone know of another source of lupeol other than fresh fruit?
Stay tuned...
Grouppe Kurosawa, Medicine in the Public Interest
(http://www.grouppekurosawa.com)
5 Comments:
Here is another TirTerpene with
anti cancer effects:
Should I drink my Birch Beer now?
http://www.nature.com/nm/journal/v1/n10/abs/nm1095-1046.html
"As a result of bioassay−guided fractionation, betulinic acid, a pentacyclic triterpene, was identified as a melanoma−specific cytotoxic agent. In follow−up studies conducted with athymic mice carrying human melanomas, tumour growth was completely inhibited without toxicity. As judged by a variety of cellular responses, antitumour activity was mediated by the induction of apoptosis. Betulinic acid is inexpensive and available in abundant supply from common natural sources, notably the bark of white birch trees. The compound is currently undergoing preciinicai development for the treatment or prevention of malignant melanoma.
"
Oh and here is a Birch Bark Source:
http://www.mountainroseherbs.com/bulkherb/b.php
We are actively looking into betulinic acid.
PTYCHOPETALUM OLACOIDES EXTRACT - Muira Puama is a nerve stimulant with a highly regarded reputation as a powerful aphrodisiac. It is rich in fatty acids and fatty acid esters (behenic acid), essential oils (beta-caryophyllene and alpha-humulene), plant sterols, triterpenes (lupeol), and an alkaloid named muirapuamine.
I came here looking for info on lupeol after seeing it associated with Crataeva Nurvala, common name varuna and 3 leaf caper. Used in Indian ayurvedic medicine for kidney stones among other things and apparently for enlarged prostate.
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