6 replies to this topic

[Thales]

"Dr. Maher and colleagues have proposed studies to extend our knowledge of fisetin and closely related compounds, with the goal of identifying drugs that may be useful in the treatment of Alzheimer's disease. As a first step in this process, the researchers plan to create several new chemical compounds by making slight modifications to the fisetin molecule. The goal of this step is to create a series of molecules with the beneficial effects of fisetin and which have ideal chemical and medicinal properties for use as drugsDr. Maher and colleagues have proposed studies to extend our knowledge of fisetin and closely related compounds, with the goal of identifying drugs that may be useful in the treatment of Alzheimer's disease. As a first step in this process, the researchers plan to create several new chemical compounds by making slight modifications to the fisetin molecule. The goal of this step is to create a series of molecules with the beneficial effects of fisetin and which have ideal chemical and medicinal properties for use as drugs"

http://www.alz.org/p...chers_14585.asp

So perhaps there havn't been human tests yet because they first want to modify fisetin enough to have it patented. What do you guys think?

[niner]

So perhaps there havn't been human tests yet because they first want to modify fisetin enough to have it patented. What do you guys think?

Could be. Or maybe they want to modify the molecule so that it has decent pharmacokinetics, so it will have a decent chance of working well in vivo, with acceptable side effects and dosing schedules.

[yowza]

It's great to see alot of new progressive threads starting up around here. Throughout June there was alot of the same kind of stuff being repeated.

I heard about Fisetin from somebody in the past...

I kind of half-heartily tried starting up a sort of nootropic database for rare compounds that noone's heard of... Here's something I wrote down in regards to Fisetin. Hopefully, it's readable as I don't think the indentations will show very well as I paste it down:

Concept is "primary metabolites" or ("secondary metabolites"); derived from various organic substances such as herbs, ergoloids, ect. Alot of these compounds (fisetin, ginseng, ect.) may be concentrated forms of something that's found at any grocery/health food store.

Flavonoids: http://en.wikipedia....wiki/Flavonoids

Classes (of flavonoids):

A) Flavons

1)Flavones

2) Flavonols (or 3-hydroxyflavone) (http://en.wikipedia.org/wiki/Flavonols)

-These supposedly effect CYP enzyme activity (See above link)

Some examples include:

• Kaempferol (3,4',5,7-tetrahydroxy-2-phenylchromen-4-one)
• Quercetin (3,3',4',5,7-pentahydroxy-2-phenylchromen-4-one)
• Myricetin (3,3',4',5',5,7-hexahydroxy-2-phenylchromen-4-one)
• Fisetin (3,3',4',7-tetrahydroxy-2-phenylchromen-4-one)

3) Flavanone

4) Flavononal (see other names)

B) Isoflavones







C) Flavan-3-ols (flavan-3-ol), Proanthocyanidins, and Anthocyanodins

http://en.wikipedia.org/wiki/Flavanol



Nootropic Compounds from Flavonoids (database for stuff falling under flavonoid category):

Entry 1: Fisetin
Flavonoidsàflavon (one of the subclasses of flavonoid)àflavonol subclass (as shown in above section); fisetin is a type of flavonol

IUPAC/Chemical Name: 3,3',4',7-tetrahydroxy-2-phenylchromen-4-one
Explaining parts of the IUPAC name (above):
-All Flavonoids are defined by their 3-hydroxyflavon backbone (otherwise seen as 3-hydroxy-2-phenylchromen-4-one as part of the IUPAC name above)

-The "2-phenylchromen-4-one" part of IUPAC name is used interchangeably with the word "flavon"-see "flavon" above

CAS=528-48-3

Structure=http://www.chemblink.com/products/528-48-3.htm

Molecular weight= 286.24

Concept: A "secondary metabolite" of strawberries (and other fruits/vegetables) and wine

Research Origin: Salk Institute of Biological Sciences http://www.newswise....les/view/524397

People Looking to develop this into a pharmaceutical drug:

http://www.sunbio.bi...t...e&sPipeNo=2

Salk Institute of La Jola CA: http://foundationcen...essionid=OJOOUS HZQ2DOHLAQBQ4CGW15AAAACI2F?id=184800033 (developing more potent analogues from Fisetin)

Benefits:

Anti-carcinogenic-http://jn.nutrition.org/cgi/content/abstract/135/12/2884 and http://carcin.oxford...stract/30/2/300 -Mechanism: Modification of CDK activity

Memory-http://www.pnas.org/content/103/44/16568/F4.expansion

Suppliers:

http://www.chemblink...3_suppliers.htm

http://buy.ecplaza.n...ll/fisetin.html (note some companies offer it in various concentrated forms)

Market Research Report:

http://marketpublish...isetin_528-48-3 _market_research_report.html

Interesting Comment:

To get enough fisetin to get the nootropic effect, you would need to eat 10 pounds of strawberries. Also the research didn't even find the end of the bell curve for the effect yet! Fisetin is also related to Resveratrol.

[Thales]

I recently emailed one of the Fisetin researchers about what a safe a dose would be for memory enhancement. I was told that since there haven't been thorough toxicology studies we don't how safe it is. Using intravenous injection however, the LD50 dose was 180mg/kg for mice. Further, there are mice which have been on 500 mg Fisetin per kg of food for over a year without any adverse effects.

The researcher explained that according to the FDA conversion table the human dose should be 0.8-2 mg/kg orally.

I have ordered Fisetin 50% from vitaspace.com. However, I'm a little worried about the other other 50% even though it is apparently "inert smoke tree material"… For 1300$ we can have a kg of 98% Fisetin made if anyone else is interested.

Edited by Thales, 24 July 2009 - 06:53 AM.

[yowza]

I recently emailed one of the Fisetin researchers about what a safe a dose would be for memory enhancement. I was told that since there haven't been thorough toxicology studies we don't how safe it is. Using intravenous injection however, the LD50 dose was 180mg/kg for mice. Further, there are mice which have been on 500 mg Fisetin per kg of food for over a year without any adverse effects.

The researcher explained that according to the FDA conversion table the human dose should be 0.8-2 mg/kg orally.

I have ordered Fisetin 50% from vitaspace.com. However, I'm a little worried about the other other 50% even though it is apparently "inert smoke tree material"… For 1300$ we can have a kg of 98% Fisetin made if anyone else is interested.

Thanks for passing on the info. you got from a researcher. Could you simply paste the e-mails here from the research laboratory? What Fisetin research area are you referring to?

As for Vitaspace... They seem to charge pretty high for everything but seem to be a good company. You could get it synthesized for MUCH cheaper somewhere else for greater quantities at a higher potency. $1300 is asking abit much for an extract in my opinion.

I pasted some supplier info. in my post above. The COA, IUPAC... All that seemingly useless info. is used to search up chemicals from a synthesizer company (the molecular wieght and formula are simply a way for me to further confirm what I'm looking at is not an altered form of fisetin). I included a few links where you can get price listings+certificate of analysis information from a company if interested... (just to give a heads up that there's actually some relevant info. I've found; I know some of the info. I listed is seeminly useless but it actually isn't. One could make an entire database based off of this criteria for other nootropics as well.)

A forward thinking nootropic supplier could be interested in obtaining some Fisetin from one of these suppliers but unfortunately most seem to only want to look into this stuff only after everyone has caught on already. If someone wants to try some of this stuff out and make a subjective report feel free to do so. Just make sure what your getting is free of contaminants by asking for a certificate of analysis; this can be obtained from a company or paid for by yourself and sending it to a lab here in the states for analysis.

I haven't found any side effects but, as mentioned in my above post, there is some CYP inhibition (enzymes in the liver responsible for metabolizing substances); although I'm not sure how potent/strong this supposed CYP inhibition is or lasts after taking Fisetin. If you're taking medication with this, be aware that it's possible Fisetin may slow down the rate at which you metabolize it possibly...

Edited by yowza, 24 July 2009 - 09:52 PM.

[kooolpig]

So perhaps there havn't been human tests yet because they first want to modify fisetin enough to have it patented. What do you guys think?

Could be. Or maybe they want to modify the molecule so that it has decent pharmacokinetics, so it will have a decent chance of working well in vivo, with acceptable side effects and dosing schedules.

Daidzin : http://www.lookchem....2/552-66-9.html

Edited by kooolpig, 18 June 2010 - 08:03 AM.

[Gerald W. Gaston]

Fisetin is in the "CR Mimetic Longevity Formula" from LEF too. This months LEF mag has a little mention about it as well. Since it was time to renew my membership, and they give you product credit, I grabbed this and some MCC.

http://www.lef.org/V...ty-Formula.html

24mg/cap

Edited by frankbuzin, 20 June 2010 - 10:37 PM.