Wednesday, May 5, 2010

proclus : Michael L. Love: polyphenols, first round results

Michael L. Love: polyphenols, first round results
We are fortunately living in a time when the comparitive merit of the various polyphenols is being studied, so that we can survey the literature to find the best new supplements, and the best combinations.  The first round of my survey has returned the following results.  It supports my suggestion that one polyphenol supplement is not enough, and it is recommended to take a panel of them.  This survey has its own bias as to time, because quercetin, resveratrol, egcg, and curcumin have received the most study, whereas hopeful prospects such as, silymarin, naringenin, apigenin, and kaempferol are new to the game in the comparitive studies.

Curcumin consistently scores highly, although not always the best.  It is first mentioned, because it is rarely shown to have adverse effects.  egcg and resveratrol, though getting frequent top scores, occasionally produce effects that are contrary to the aim.  Quercetin is the midling, although it may be better grouped with curcumin.  It is no surprise to see that curcumin, quercetin, and egcg are as popular in the supplement community, or more so, than resveratrol, due to the equally promising results that they have produced.  I recommend a minimum panel of these four polyphenols taken together, each at their effective dose.

Other molecules that have received less attention, but score fairly well are naringenin, silymarin, and apigenin.  Fisetin and chrysin dropped out in this round.  I think that additional supplementation with naringenin, silymarin, and apigenin is not a bad idea.  Other candidates will be coming to light in the future. 

It should be noted that there are food sources which are often sufficient to provide the necessary amounts of many of these substances in order to produce the desired effect.  These foods include citrus fruits, red onions, rutabagas, kale, as well as certain berries, grapes, and pomegranate.  I would also recommend celery, thyme, parsley, and green peppers.  (personally, I like the red peppers ;-)

I am afraid I that it is late for me tonight. I am tired, so that I am surely forgetting something, and there will certainly be further followup.  I was able to produce a few more caveats and suggestions.  I don't recommend more than 500 mg of egcg per day, until it can be demonstrated that a panel of polyphenols will prevent the resulting DNA strand breaks.  This is an important concern, because it is easy to get far more that 500 mg of egcg from widely available supplements.  The higher dose produces nPKC activation in keratinocytes and the resulting free radicals are shuttled to the nucleus by egcg.  There is sure to be more about this type of problem in the future.

I would also like to point out that these molecules can inhibit COX enzymes and related systems, which is widely noted as a positive benefit.  Unfortunately, oversuppression of COX may lead to kidney damage, due to the fact that the kidneys rely on prostaglandins for vasodilation.  As a result of this realization, I have been monitoring my kidney function carefully using the chemistry panel tests, and I can say that it is very unwise to overuse NSAIDS and other COX inhibitors while on a polyphenol or flavanoid regimin.  It is unwise in any case, so please review your use of these analgesic molecules, such as aspirin, ibuprofen, naproxen sodium etc. Check the directions again.  My doctor is recommending acetaminophen instead, but I suggest using well below the recommended acetaminophen dose, especially when used in combination with aspirin.  The molecular mechanisms of these two compounds are related.  Supplementing with a strictly low dose of aspirin is probably still beneficial and possibly synergistic, as it were, with the polyphenol regimen, but I recommend regular kidney panels to anyone who is following the polyphenol or other CR-related regimens.

Relatedly, I have been experimenting with forskolin in order to provide an offset of vasodilation.  Forskolin likely provides many healthful benefits in addition to this one, and it is probably not a bad idea to take it with your aspirin, but maintain a strict regimen.  Use only small dose aspirin, and don't miss your forskolin doses, or you will experience the rollercoaster effect.  You might also need an occasional dose of antacid with this combination.  It is fashionable to avoid aluminum in the antacid.

Here is a bit more regarding the specific health concerns, with the supplements that score best in the respective studies.  The lists are mostly in order of effectiveness.  I also lists the supplements that didn't work.  When it says "beats", this means that the supplement produced a contrary result to the aim; it was adverse.

 resveratrol beats lutein
 cures macular degeneration, anecdotal

 resveratrol curcumin beats rutin quercetin
 inhibited NADPH oxidase (NOX)

 quercetin curcumin resveratrol beats rutin
 prevented peroxide induced DNA single strand breaks

 quercetin resveratrol curcumin beats egcg
 phase 2 activation assay

 quercetin apigenin beats egcg resveratrol
 lung invasion test (cancer)

 curcumin quercetin egcg beats resveratrol

 quercetin resveratrol beats egcg
 xenobiotic response

 curcumin egcg quercetin beats resveratrol
 beneficial heme oxygenase1 expression upregulation

 kaempferol naringenin beats egcg
 catalase activity enhancement

 egcg quercetin beats naringenin
 radical scavenging

I hope that it is helpful to have the results summarized in this way.  Here are the references, so that you can check for yourself.

Optometry. 2009 Dec;80(12):695-701.
Molecular medicine in ophthalmic care.
Richer S, Stiles W, Thomas C.

Biochem Biophys Res Commun. 2005 Jul 22;333(1):21-7.
Resveratrol and curcumin reduce the respiratory burst of Chlamydia-primed THP-1 cells.
Deby-Dupont G, Mouithys-Mickalad A, Serteyn D, Lamy M, Deby C.

Pharmazie. 2002 Dec;57(12):852-4.
Protection against damaged DNA in the single cell by polyphenols.
Liu GA, Zheng RL.

Toxicol Sci. 2007 Apr;96(2):227-36. Epub 2006 Oct 31.
Phytochemicals induce breast cancer resistance protein in Caco-2 cells and enhance the transport of benzo[a]pyrene-3-sulfate.
Ebert B, Seidel A, Lampen A.

Nutr Cancer. 2004;49(2):200-8.
Phytoestrogens in common herbs regulate prostate cancer cell growth in vitro.
Shenouda NS, Zhou C, Browning JD, Ansell PJ, Sakla MS, Lubahn DB, Macdonald RS.

Int J Cancer. 2000 Aug 15;87(4):595-600.
Flavonoids apigenin and quercetin inhibit melanoma growth and metastatic potential.
Caltagirone S, Rossi C, Poggi A, Ranelletti FO, Natali PG, Brunetti M, Aiello FB, Piantelli M.

Nutr Res. 2009 Aug;29(8):568-78.
Select phytochemicals suppress human T-lymphocytes and mouse splenocytes suggesting their use in autoimmunity and transplantation.
Hushmendy S, Jayakumar L, Hahn AB, Bhoiwala D, Bhoiwala DL, Crawford DR.

Free Radic Biol Med. 2007 Feb 1;42(3):315-25. Epub 2006 Oct 11.
Modulation of pregnane X receptor- and electrophile responsive element-mediated gene expression by dietary polyphenolic compounds.
Kluth D, Banning A, Paur I, Blomhoff R, Brigelius-Floh<E9> R.

Pharmacol Res. 2006 Feb;53(2):113-22. Epub 2005 Oct 21.
Piceatannol upregulates endothelial heme oxygenase-1 expression via novel protein kinase C and tyrosine kinase pathways.
Wung BS, Hsu MC, Wu CC, Hsieh CW.

Mutat Res. 2003 Feb-Mar;523-524:163-72.
Mechanism-based in vitro screening of potential cancer chemopreventive agents.
Gerh<E4>user C, Klimo K, Heiss E, Neumann I, Gamal-Eldeen A, Knauft J, Liu GY, Sitthimonchai S, Frank N.

"EGCG and EG partially suppressed catalase activity."
Biol Pharm Bull. 2007 Feb;30(2):213-7.
Chemical structure-dependent differential effects of flavonoids on the catalase activity as evaluated by a chemiluminescent method.
Doronicheva N, Yasui H, Sakurai H.

Arch Pharm Res. 2005 Nov;28(11):1293-301.
Antiherpetic activities of flavonoids against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in vitro.
Lyu SY, Rhim JY, Park WB.

Mutat Res. 2000 Apr 28;459(3):211-8.
Effects of epigallocatechin gallate and quercetin on oxidative damage to cellular DNA.
Johnson MK, Loo G.


The blog


  • Michael L. Love: Parsley recipe
  • Michael L. Love: polyphenols and stable free radicals
  • Michael L. Love: some bio info, blog links, plus some molecules site news
  • Michael L. Love: USDA Database for the Flavonoid Content
  • Michael L. Love: recipe; flax oil, tyrosol lignans update
  • Michael L. Love: rutabagas odyssey
  • Michael L. Love: polyphenols, first round results
  • Michael L. Love: Tryosol Lignins
  • Michael L. Love: Bisphenol Molecules Structural Archive and Gallery
  • Michael L. Love: Nano baby doll house music maker
  • Michael L. Love: Molecules Activism on Vitacost: Thai Black Rice update
  • Michael L. Love: Antifungal nasal spray
  • Michael L. Love: Merry Christmas Vitacost Community!
  • Michael L. Love: more on the polyphenol story
  • Michael L. Love: Seafood notes
  • Michael L. Love: Polyphenols, etc
  • Michael L. Love: Linus Pauling
  • Michael L. Love: First entry
  • Follow Michael L. Love:
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    Published Sunday, January 03, 2010 07:20 PM by proclus

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