Another update:
So I’ve been a bit perplexed by the potency of the Rosemary Honey since Day 1. By all accounts the content of Kaempferol, even in its aglycone form, shouldn’t be causing such effects at doses as little as a teaspoon of honey.
Today I found the possible reason why…
“8-Methoxy-kaempferol was the main compound in rosemary honey samples.”
I then hunted for what exactly 8-methoxy-KF does, and as of 2017 the article I found claims no data is available on this flavonoid. Other places claim it to be a rare unknown flavonoid.
It’s obvious to me now this 8-methoxy-KF is the likely culprit with regular KF probably contributing less so to the b-endorphin release. Now to BL’s pharmacologically knowledgeable members, how would the 8-methoxy group effect this flavonoid?
Kaempferide, 4-methoxy-kaempferol, is said to have kaempferol as one of its metabolites. I wonder if this is like an increased bioavailability pro-drug type situation?
Edit- It seems while there isn’t data on the opioid activity, in every other category Kaempferide is one of the most effective flavonoids when tested against many others for a variety of ailments. I could see the 8-methoxy substitution possibly outperforming Kaempferide (the 4-methoxy). And since there’s a dose dependent correlation between the various benefits of these flavonoids I’m going to extrapolate that these methoxy substituted flavonoids may be stronger than the non-subbed counterpart.
One other interesting note, 3,5,7 flavonoids such as Kaempferol seem to be the most effective. Galangin is another which may show pharmacological promise.
Edit 2- And here’s the money shot..
Dietary flavonoids exhibit beneficial health effects. Several epidemiological studies have focused on their biological activities, including antioxidant, antibacterial, antiviral, anti-inflammatory and cardiovascular properties. More recently, these compounds ...
www.ncbi.nlm.nih.gov
An article claiming methoxylated flavonoids are more potent, and how to create them.
Diverse defenses: O-methylated flavonoids contribute to the maize arsenal against fungal pathogens
pubmed.ncbi.nlm.nih.gov
Another claiming increased bioavailability, stability and absorption.
I appreciate you all coming along on this ride of research with me
You are learning alongside me as I go..
——Rosemary Honey is potent due to its 8-methoxylated Kaempferol which is not only more potent due to it being de-glycosided and in honey form, but also this methoxylated substitute greatly increases BA.——
“It is suggested that
O-methylated flavonoids have shown a stronger anticancer potential than their hydroxylated forms due to be higher metabolic stability and increased membrane transport in the intestine and liver, which result in exhibiting a superior oral bioavailability.”
“With regard to oral bioavailability, most unmethylated polyphenols studied in the past, e.g., quercetin, kaempferol, diosmetin, curcumin and resveratrol, would not be expected to reach internal organs, i.e. beyond sites along the gastrointestinal tract.
The orally bioavailable methoxyflavones have considerably greater potential to reach target tissues to exert biological effects
in vivo.”
Edit 3- Below is an article showing Kaempferide (4-methoxy) has much better binding to proteins which carry exogenous substances through the body. Essentially from my view, better BA. They claim with the two flavonoids they compared (Kaempferol and Kaempferide being “one”) there was a 2-16 better binding with the methoxylated flavonoids.
(2013). Methylation of genistein and kaempferol improves their affinities for proteins. International Journal of Food Sciences and Nutrition: Vol. 64, No. 4, pp. 437-443.
www.tandfonline.com
-GC