Follidrone (Epicatechin) + Octyl Gallate?

[Mmats]

Octyl gallate (GAO) and other GAO derivatives enhance cellular accumulation of epicatechin, at least in vitro, by up to 426% (study below). In other studies, octyl gallate has also shown oral bioavailability in humans.

Would it make sense to dose these together? Seems to be a safe and low cost food additive.

Abstract
The cellular accumulation of individual catechins was measured as an index of intestinal absorption to clarify the interactions among catechins. The cellular accumulation of (-)-epicatechin (EC) increased in the presence of other catechins. The ability of gallate catechin such as (-)-epigallocatechin gallate (EGCG) and (-)-epicatechin gallate (ECG) to increase the cellular accumulation of EC was greater than that of nongallate catechins. Gallic acid octyl ester (GAO) also increased the cellular accumulation of EC by 426% as compared with that in untreated cells. Conversely, the cellular accumulation of ECG was not influenced by other catechins, but it increased by 54% in the presence of GAO. Experiments using GAO derivatives indicated that the gallate moiety required the presence of a catechol group and a neighboring carbonyl group, whereas the pyrogallol moiety, without a neighboring carbonyl group, required 3 hydroxyl groups to increase the cellular accumulation of EC. Furthermore, gallate esters required long carbon chains to increase the same. The experiment using EGCG, GAO, or their derivatives indicated that the ability of gallate or pyrogallol moiety to increase the cellular accumulation of EC was restricted by their hydrophobicity. These results suggest that the co-administration of foods containing functional materials such as gallate or pyrogallol moieties, increases the intestinal absorption of catechin.
PRACTICAL APPLICATION:
The cellular accumulation of (-)-epicatechin increased by the gallate or pyrogallol moiety in catechin structure. The interaction among catechins appeared to affect intestinal absorption of catechin. The bioavailability of catechin may be improved by co-administration of functional foods.

http://www.ncbi.nlm.nih.gov/pubmed/22938538

[brundel]

Octyl gallate can cause all kinds of skin problems and stomach issues. Its not good to eat.
Looks like EGCG works just the same and 50% EGCG is easy to come by at bulk powder retailers.

[Mmats]

Octyl gallate can cause all kinds of skin problems and stomach issues. Its not good to eat.
Looks like EGCG works just the same and 50% EGCG is easy to come by at bulk powder retailers.

I believe the irritation issues are only caused by high concentrations of octyl gallate. Its already used as an additive in many foods to prevent rancidity. I guess the question is - Where does the threshold lie?

A temporary ADI of 0-0.1 mg octyl gallate/kg bw was allocated based on a NOEL of 17.5 mg/kg bw/day in a reproduction study with rats, to which a safety factor of 200 was applied.

I mentioned octyl gallate over the other gallates (EGCG) because of its low price point

[brundel]

50% EGCG is pretty cheap.

Since we are currently using rice flour as filler. There is no reason I cant change the filler to 50% EGCG.
itll only cost 1$ more per unit.

Thanks for pointing this out. Its gonna improve our product.

[Mmats]

50% EGCG is pretty cheap.

Since we are currently using rice flour as filler. There is no reason I cant change the filler to 50% EGCG.
itll only cost 1$ more per unit.

Thanks for pointing this out. Its gonna improve our product.

Glad to help, but hopefully you can check the full text before you make a decision (I can only get the abstract). Its not clear, looking at the abstract, exactly how effective EGCG was when compared to GAO (426%). For all we know, it may have taken 500mg EGCG to see an increase of epicatechin by only 10%.

[Mr.Cooper69]

So it looks like epicatechin has extremely low bioavailability due to two efflux transports: MRP-2 or BCRP. Inhibition of either of these may allow the ingredient to make it into circulation

[jh18]

So it looks like epicatechin has extremely low bioavailability due to two efflux transports: MRP-2 or BCRP. Inhibition of either of these may allow the ingredient to make it into circulation

What is the best way to go about inhibiting? Will dosing with EGCG work? Any other suggestions?

[Mmats]

So it looks like epicatechin has extremely low bioavailability due to two efflux transports: MRP-2 or BCRP. Inhibition of either of these may allow the ingredient to make it into circulation

Another Caco-2 assay shows grapefruit/lemon juice made a significant difference in retention.

ABSTRACT

The objective of this study was to characterize the impact of tea formulations on in vitro digestive recovery and subsequent uptake/retention of catechins by Caco-2 human intestinal cells. Beverages prepared with green tea (GT) extract provided 3, 18, 20, and 3.5 mg/100 mL of epicatechin (EC), epigallocatechin (EGC), epigallocatechin gallate (EGCG) and epicatechin gallate (ECG) respectively. Formulation variables included plain GT (control), ascorbic acid (AA) (24mg/100mL), and 20% (v/v) lemon (LM) and grapefruit (GF) juices. Samples were subjected to simulated gastric and small intestinal conditions with catechin levels assessed pre- and post-digestion. Differentiated monolayers of the TC7 clone of Caco-2 were incubated for 3h in PBS (pH 5.0) containing 20% digestate. Addition of juices significantly increased digestive recovery of catechins (30 to >70%) with greatest impact on EGC (28–78%) and EGCG (28–61%). Caco-2 intracellular catechin levels obtained from digested juice-tea beverages were significantly (p<0.05) higher (219 and 156 pmol/mg in GF and LM) than digested plain GT (58 pmol/mg) due to enhanced digestive recovery and increased uptake efficiency of catechins from GF and LM products. 1 h catechin retention by Caco-2 cells was highest for plain GT(23%) followed by GF(11.6%) and LM(6.5%) formulations. These data provide evidence that formulation factors impact both digestive recovery and may influence intestinal absorption of catechins from tea beverages.

http://www.fasebj.org/cgi/content/me...ct/21/5/A730-b

[Mr.Cooper69]

What is the best way to go about inhibiting? Will dosing with EGCG work? Any other suggestions?

I may as well just go ahead and formulate a product if I'm gonna post all that here

[Mr.Cooper69]

Another Caco-2 assay shows grapefruit/lemon juice made a significant difference in retention.

Did they say this was due to pgp inhibition? That's probably the 3rd major efflux transporter in question since it affects such a broad array of compounds

[jh18]

I may as well just go ahead and formulate a product if I'm gonna post all that here

Are you trying to tell me something about the upcoming insider deal haha. I was sure you guys are dropping a GDA since its requested a lot.

ON a serious note I am just wanting to get the most out of my run on epi and I am not the most scientifically inclined. Thats the great thing about msg boards. I can get ? answered I would have no clue about.

Any help would be apreciated

[Mmats]

Did they say this was due to pgp inhibition? That's probably the 3rd major efflux transporter in question since it affects such a broad array of compounds

I dont know (no access), but ascorbic acid did similarly well. PGP inhibition, however, has been shown with gallate/pyrogallol moiety catechins, rising with their hydrophobicity.

Are you trying to tell me something about the upcoming insider deal haha. I was sure you guys are dropping a GDA since its requested a lot.

ON a serious note I am just wanting to get the most out of my run on epi and I am not the most scientifically inclined. Thats the great thing about msg boards. I can get ? answered I would have no clue about.

Any help would be apreciated

Epicatechin + vitamin C + EGCG

[jh18]

I dont know (no access), but ascorbic acid did similarly well. PGP inhibition, however, has been shown with gallate/pyrogallol moiety catechins, rising with their hydrophobicity.



Epicatechin + vitamin C + EGCG

Thanks. What's the vit c for?

[Quadzilla99]

Thanks. What's the vit c for?

Read his previous post abscorbic acid is another name for vitamin c

[jh18]

Read his previous post abscorbic acid is another name for vitamin c

Got it now.

Thanks

[DR_P]

I dont know (no access), but ascorbic acid did similarly well. PGP inhibition, however, has been shown with gallate/pyrogallol moiety catechins, rising with their hydrophobicity.



Epicatechin + vitamin C + EGCG

= cup of brewed green tea with a bit of lemon juice

[Mmats]

= cup of brewed green tea with a bit of lemon juice

The irony didnt escape me that we are finding these compounds work best in conjuction, and that the formula has existed for a long time. The major difference, though, is that there is only a small amount of epicatechin in green tea (anywhere from 4 to 48mg per cup).

[brundel]

What is the best way to go about inhibiting? Will dosing with EGCG work? Any other suggestions?

For now take it with EGCG.

Soon you wont need to as we are planning on manufacturing a 2.0 with absorption enhancement.

[brundel]

One other thing......I wouldnt jump to conclusions without reading the entire study.
Often an abstract can make things look a certain way but when you read the whole text you see why.

Octyl gallate for example. The dose used was incredibly high. Orally unrealistic.

I have the full studies for both of those and a few others.
Interesting stuff for sure.
Looks like there are several ways to increase absorption. We are feeding test batches to guinea pigs as we speak

[Mmats]

One other thing......I wouldnt jump to conclusions without reading the entire study.
Often an abstract can make things look a certain way but when you read the whole text you see why.

Octyl gallate for example. The dose used was incredibly high. Orally unrealistic.

I have the full studies for both of those and a few others.
Interesting stuff for sure.
Looks like there are several ways to increase absorption. We are feeding test batches to guinea pigs as we speak

Believe me I wish I could afford it. Thanks for the info though, Im glad you could review these and fill us in.

[brundel]

Believe me I wish I could afford it. Thanks for the info though, Im glad you could review these and fill us in.

No thank you. This inspired alot of research on my part and has become something all its own.
You will at some point be able to see the fruit of your contribution

[Mmats]

No thank you. This inspired alot of research on my part and has become something all its own.
You will at some point be able to see the fruit of your contribution

Good deal. Its an interesting compound and I'll admit I havent even tried it yet, though I plan to soon.

[noaddedhormones]

For now take it with EGCG.

Soon you wont need to as we are planning on manufacturing a 2.0 with absorption enhancement.

So with current version loggers are seeing gains in the range of 10lbs from 4 week cycle? Version 2.0 a 4 week cycle should have them looking like jay culter right?

[PuZo]

So with current version loggers are seeing gains in the range of 10lbs from 4 week cycle? Version 2.0 a 4 week cycle should have them looking like jay culter right?

I still don't buy 10lbs in 4 weeks. 10lbs total sure, but some users are reporting a gain of 10lbs of LBM... With legit gear you can probably do that, but even then.... lettuce be cereal for a moment...

[noaddedhormones]

I still don't buy 10lbs in 4 weeks. 10lbs total sure, but some users are reporting a gain of 10lbs of LBM... With legit gear you can probably do that, but even then.... lettuce be cereal for a moment...

I see you failed to sense the sarcasm at numerous points in my post.

[PuZo]

I see you failed to sense the sarcasm at numerous points in my post.

Oh no I didn't I was just adding onto it with a more serious tone.

[Mmats]

I thought I had already included the abstract showing vitamin C likely preventing efflux of epicatechin back to the intestinal lumen. Here it is -

http://www.ncbi.nlm.nih.gov/pubmed/17688297

Abstract
Epidemiological evidence suggests a role for tea catechins in reduction of chronic disease risk. However, stability of catechins under digestive conditions is poorly understood. The objective of this study was to characterize the effect of common food additives on digestive recovery of tea catechins. Green tea water extracts were formulated in beverages providing 4.5, 18, 23, and 3.5 mg per 100 mL epicatechin (EC), epigallocatechin (EGC), epigallocatechin-gallate (EGCG), and epicatechin-gallate (ECG), respectively. Common commercial beverage additives; citric acid (CA), BHT, EDTA, ascorbic acid (AA), milk (bovine, soy, and rice), and citrus juice (orange, grapefruit, lemon, and lime) were formulated into finished tea beverages at incremental dosages. Samples were then subjected to in vitro digestion simulating gastric and small intestinal conditions with pre- and post-digestion catechin profiles assessed by HPLC. Catechin stability in green tea was poor with <20% total catechins remaining post-digestion. EGC and EGCG were most sensitive with less, not double equals 10% recovery. Teas formulated with 50% bovine, soy, and rice milk increased total catechin recovery significantly to 52, 55, and 69% respectively. Including 30 mg AA in 250 mL of tea beverage significantly (p<0.05) increased catechin recovery of EGC, EGCG, EC, and ECG to 74, 54, 82, and 45% respectively. Juice preparation resulted in the highest recovery of any formulation for EGC (81-98%), EGCG (56-76%), EC (86-95%), and ECG (30-55%). These data provide evidence that tea consumption practices and formulation factors likely impact catechin digestive recovery and may result in diverse physiological profiles.

[htghunterray]

I still don't buy 10lbs in 4 weeks. 10lbs total sure, but some users are reporting a gain of 10lbs of LBM... With legit gear you can probably do that, but even then.... lettuce be cereal for a moment...

My squat has went up 95 pounds... I have added reps to all my lifts along with increasing weight. However, ive only gained around 5 pounds.

[PuZo]

My squat has went up 95 pounds... I have added reps to all my lifts along with increasing weight. However, ive only gained around 5 pounds.

How long have you been lifting for? How long have you been taking it?

[htghunterray]

How long have you been lifting for? How long have you been taking it?

A year and a half religiously. My squat had been stuck for weeks before folli. and i'm at the end of my bottle , so 4 weeks.