Monday, November 9, 2009

Chicoric Acid - A Natural Integrase Inhibitor.

Over the weekend, I pored over numerous scientific journals, and came across something particularly interesting when searching for inhibitors of XMRV Integrase - Chicoric Acid.  I found numerous studies done, showing that it inhibits not only HIV-1 integrase, but a broad spectrum of integrase enzymes.  This holds some potential as a low cost treatment, however its efficacy remains to be seen.  Chicoric Acid is one of the active principles in extracts of purple coneflower (echinacea).  For pharmaceutical companies, there is little interest in the compound, as it cannot be patented, however in the not-too-distant future we may see it appear on shelves of health food stores.

I for one, cannot guarantee its efficacy.  No pharmacokinetic studies have been done on it.  Normally, a lot of phytochemicals that show a lot of promise in vitro, have little to absolutely no effect in vivo.  This is because everything that is absorbed through the intestine is taken to the liver through the hepatic portal vein, where it undergoes first-pass metabolism, usually through the Cytochrome P450 enzyme system, followed by glucoronidation where it is eliminated through bile.  However, pharmaceutical chemists have devised clever ways to thwart the P450 system, by identifying key parts of the molecule that are vulnerable to attack, and replacing functional groups with Chlorine or Fluorine atoms, giving them a much longer half-life in the body.  Some of these analogs are already being studied as candidate compounds for HIV - for example it has been found that the carboxyl groups of caffeic acids are not necessary to inhibit integrase.

7 comments:

  1. This is very interesting. In the past I have chewed the seeds of the purple coneflower and they make my mouth tingle. Do you know whether the seeds contain this chicoric acid? It seemed that when I did this some years ago on a daily basis, that after a week or so I seemed to feel much better. Though I think it is the root that is usually used medicinally.

    I have had CFS for a couple of decades with remissions and relapses. Almost 20 years ago I was told that my spine would be fusing within a couple of years, but it is better today than it was then. However, I did too much walking about a year ago and have had a severe relapse of fatigue that I can't get over. I have better days and worse days but severe penalty for overexertion. On a whim, a week or so ago, with winter approaching, I picked a lot of the seed heads from my purple coneflowers and ate a few seeds to feel the tingle. But I have not separated out the seeds yet or eaten any more of them. The last few days I have had a return of the extreme stiffness, especially my back and that reminded me of my prior theory some years ago that I had inherited AS from my dad. I started to think of the ways that the XMRV might be involved in AS and so did a search on it and AS and found your blog and several others who were making similar associations. Then I found your post on chicoric acid and thought of my basket of seed heads. Your post makes me wonder if it would be worth the try.

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  2. It is probably safe to assume that the seeds are a particularly rich source of Chicoric Acid. I will do a search in some botanical journals, and find out. I'll try and source some seeds, and run an analysis, and see what I come up with.

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  3. I did find that indeed Chicoric acid is expressed in Echinacea seed, and is present in the oil fraction. On an HPLC chromatograph at 320nm, chicoric acid will present as peak 6 at about 22.5 minutes

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  4. I've tried taking Echinacea once and I had the strongest reaction to it. I have food intolerances to many foods, from tree nuts to nightshade to corn, etc. with a lot of seeds especially, and Echinacea lit me up something fierce. My heart was pounding for hours and it felt like someone poured hydrogen peroxide in my viens, it lit me up.

    I have Hashimoto's Thyroiditis, and to say the autoimmune aspect of ME/CFS is extremely under researched is an enormous understatement due to the 'exclusionary criteria' aspect of diagnosis, ie if you have autoimmune disease you're excluded from ME/CFS research. Now hopefully they'll be able to show XMRV jacks the shit out of autoimmune prevalence as a comorbid condition to ME/CFS, not an exclusionary condition. The entire field is going to change as surely as a flower turns to fruit.

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  5. Check out phyllanthus amarus/niruri. There is a study that found it effective ex vivo (they gave people a water/alcohol extract of the plant, drew their blood, and found their blood inhibited HIV). There is also a US patent on the use of p. niruri for treating retrovirus infection.

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  6. I actually just bought some of that(3 pkg.) and would be happy to send it to you, it also is known as chanca piedra. It made me feel worse, I think due to an autoimmune component of my disease, I think similar to the raltegravir in mice. I dunno.

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  7. Tim, I am the one who asked about the echinacea seeds. Thank you for the reply. Since I didn't have that many seeds on hand, I bought a bottle of the root complex and have been taking 2 twice a day. At first I seemed to get a bit worse and now I have improved more in a week or so than in the past year. I have now added Lapacho tea mixed with yerba mate tea which are supposed to have a stronger antiviral effect when combined and I seem to be getting even stronger. Perhaps it is the placebo effect, but I believe the UK psych guys at U. of London have demonstrated low placebo effect in ME/CFS. I have a very strong desire to get better and I've hoped in all the stuff I've tried over the past year, but to no avail. I tried this stuff on the "well I guess it couldn't hurt" theory and I finally seem to be improving, but one can't prove cause. Maybe it's all the fluids from drinking so much herbal tea. I also bought some ground chicory and have been using that instead of coffee. In any case thank you for taking the time to produce this blog and following up on comments and questions. Ruth

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