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Author: Subject: extracts of crataegus
chemrox
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[*] posted on 21-5-2007 at 18:06
extracts of crataegus


I have a dog with congestive heart failure and have read that extracts of Crataegus spp., Hawthornes, can be very helpful. I did some searching, hoping to find some straightforward extraction parameters and came across this:
http://patents1.ic.gc.ca/details?patent_number=2283948

I'm amazed. Is it just a lot of unnecessary complications to justify the patent ap? Anyway, I'm going to extract dried berries of Crataegus douglasii and Crataegus monogyna as I have both available in the area. I'm planning to use EtOH in a soxhlet unless someone here has a better idea.

The one thing that bothers me is how to get a handle on dose?
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[*] posted on 21-5-2007 at 19:16


Don't even bother extracting, just grind to a fine powder. Using a blender or coffee mill, and adding small fragments of dry ice during the grinding to keep the material cold and away from oxygen really helps.

As for dosage, that's a real problem for at home use. Beside trying to measure the amount of several active substances in each plant, the safe and effective dosage often varies across species.
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Pyridinium
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[*] posted on 21-5-2007 at 23:19


Am currently doing a web search to find out just how they extract their mysterious WS 1442.

If it's anthocyanin glycosides, your biggest worry isn't so much oxygen (well, yes, you should minimize exposure) but acid / base catalyzed hydrolysis of the glycones, and also isomerization of the compounds into colorless forms.

I have a reference that calls for extraction of anthocyanins 20% EtOH, followed by precipitation with 5 parts 95-99% EtOH added for every 3 parts of 20% EtOH anthocyanin extract. Everything kept cold at the temp. of an ice bath should be fine, I don't even think you need dry ice.

The dry extraction processes I'm thinking of use absolute EtOH or dried acetone. EDIT: as-extracted, the anthocyanin glycosides have varying degrees of solubility in abs. EtOH or acetone, some of them being poorly soluble.

There is another way, which uses a water extract to which NaCl has been added for a total NaCl conc. of about 20% This supposedly prevents conversion to the colorless compounds. The NaCl is then dialyzed away later. For example, the glucoside cyanin is preserved without undergoing hydrolysis to the aglycone.

The oxonium chlorides of these anthocyanins (prep'd by treatment in 20% HCl) are stable (EDIT: I should have said "stable to isomerization but not hydrolysis"), but of course there is some glycoside loss due to hydrolysis. These salts can be crystallized out and are soluble in absolute EtOH, where they can be stored for a while.

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I think one of the cardiac actives is vitexin-4'-rhamnoside. When dosing your dog, the stomach acid would cause some hydrolysis. Microencapsulation and tablet-buffering of these things is the way to go for making pills that would survive the stomach, but of course if you tried to buy your own tablet press we all know how that could turn out... (DEA visit, door kicked in, and all that)

You might be better off getting the capsules from Nature's Way so you have a supply for your dog, while you're experimenting with your own extraction processes.

EDIT 3: Sure enough, some of the extracts they're giving in clinical trials are simply water-EtOH extracts, probably 80:20. An article on PubMed lends support to this:
"Administration of a hydroalcoholic extract of Crataegus curvisepala in total of 92 men and women with primary mild hypertension, aged 40-60 years, 3 times daily for more than 4 months showed a decrease in both systolic and diastolic BP after 3 months" (paper by Asgary S, Naderi GH, Sadeghi M, Kelishadi R, Amiri M., Drugs Exp Clin Res. 2004;30(5-6):221-5.)

These anthocyanin extraction methods haven't changed much since 1925.

[Edited on 22-5-2007 by Pyridinium]

[Edited on 22-5-2007 by Pyridinium]

[Edited on 22-5-2007 by Pyridinium]
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