Coscinium fenestratum & Berberine

[Ishmael Fleishman]

Due to my love of cooking I am always exploring ethnic markets recently I came across a small bag of dried yellow vine in my local Indian grocer.

 

It turned out be Coscinium fenestratum - my internet search said that it was used for the treatment of inflammation and for diabetes. Condition that I both suffer from. So I bought a 150g bag of Coscinium fenestratum for $3.5.

 

I am uncomfortable about buying Coscinium fenestratum because it is endangered due to over harvesting. However my need and curiosity won out.

 

I made a herbal decoction from the Coscinium fenestratum vine using 5 litres of distilled water, lemon juice (ERROR - next time I need to increase alkalinity) for acidification and cooked it down to 750ml. Ended up with a deep yellow almost brown and extremely bitter decoction.

 

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Berberine has poor solubility in aqueous solution and its solubility at 37^°C depends on pH, which decreases with lowering pH and reaches maximum of 9.69 ± 0.37 mM in phosphate buffer 

 

My reason has been to see if it would help with the joint inflammation I experience due to an auto immune disease. I have been prescribed prednisolone however it is only partially effective and the insatiably binge eating is unpleasant side effect.

 

For the last 5 days I have been drinking 40ml of the Coscinium fenestratum decoction in the morning on an empty stomach. Their is been a reduction in joint pain and stiffness and increase range of movement without discomfort. Their has also been a strange shift in sensations in my joints. Tingling sensations and even a fullness/discomfort odd sensations.

 

After 5 days the Coscinium fenestratum decoction works better then the prescribed prednisolone and I am observing how much better it becomes over the next few weeks.

 

Now the major active ingredient is Berberine. Berberine is an interesting alkaloid and I am only starting to delve into the research however most is only preliminary animal and in-vitro studies. However there seems to be a bunch of BS being promoted by the supplements industry.

 

With Berberine low bio-availability in-vivo, poor solubility in water. I would the any claims with a pinch of salt.

 

However its tradional use is believed to be well established.

 

This is proving to be an interesting experience.

 

Has anyone used Berberine and to what effect?

 

 

 

 

 

 

 

 

 

 

 

 

Edited December 22, 2023 by Ishmael Fleishman

[Alchemica]

12 hours ago, Ishmael Fleishman said:

Has anyone used Berberine and to what effect?

 

 

Thanks for the writeup.

 

I explored a long time ago, also made up a mix of berberine hydrochloride with lecithin trying to improve it's bioavailability and was interested in it's CNS effects and beneficial metabolic effects, the CNS effects particularly related to it's sigma-1 agonism, prolyl oligopeptidase activity and monoaminergic effects

Berberine may offer benefit in the control of psychotic and depressive symptoms, along with metabolic side effects. It has a broad range of CNS relevant pharmacological actions, including sigma-1 agonism, acetylcholinesterase inhibition and a range of neuroprotective effects including neurotrophin-mediated neuroprotection (NGF). There are some limitations to its use, including bioavailability and difficulties in reaching active levels in the CNS. “The potential use in schizophrenia was suggested when berberine was found to act as a D₂-receptor antagonist, although it was also noted that dopamine level was increased in the brain as partly responsible for its antidepressant mechanism. It is unclear if these influences on dopamine level and action may counter each other, diminishing the proposed antipsychotic effect. Future studies may also elucidate whether berberine will exacerbate extrapyramidal motor symptoms due to the blockade of D₂ receptors. On the other hand, it was proposed that the anxiolytic effect of berberine resulted from its antagonism at 5-HT₂ receptor. This finding may indicate less severe motor side effects, if there are any, when berberine is used as an antipsychotic since atypical antipsychotics also act via 5-HT₂ receptor blockade. A possible advantage of berberine over other antipsychotics is its ability to inhibit prolyl oligopeptidases, the activity of which is elevated in psychosis and not targeted by antipsychotics at present.”

 

 

Edited December 22, 2023 by Alchemica

[Ishmael Fleishman]

@Alchemica I had a feeling you would have had some experience with Berberine.

 

How where you consuming Berberine with lecithin?

 

I found this

 

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The concept of ‘bioavailability enhancers’ is derived from the traditional age old system of Ayurveda (science of life). In Ayurveda, black pepper, long pepper and ginger are collectively known as “Trikatu”. In sanskrit “Trikatu” means three acrids........

 

‘Bioavailability enhancers’ are drug facilitators, they are the molecules which by themselves do not show typical drug activity but when used in combination they enhance the activity of drug molecule in several ways including increasing bioavailability of the drug across the membrane, potentiating the drug molecule by conformational interaction, acting as receptors for drug molecule and making target cells more receptive to drugs. A ‘bioenhancer’ is an agent capable of enhancing bioavailability and bioefficacy of a particular drug with which it is combined, without any typical pharmacological activity of its own at the dose used.

 

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3634921/

 

The same idea of increasing bio-availability of curcumin via black pepper.

 

Any thoughts or suggestions?

 

Have you done any extraction using methanol? As far as I understand it would mean grinding up the plant material socking in methanol for X days and then filtering and then a low temp evaporation of the methanol. However I am not to keen or set up to becoming a drug lab.

 

I had the thought of administration via a nasal route? Worth trying maybe?

 

 

 

 

[Alchemica]

There seems to be several factors that limit berberine's bioavailability to the <1% mark:

• poor absorption
• extensive metabolism
• efflux back to the intestinal lumen by the action of permeability glycoprotein (P-glycoprotein, P-gp)

As piperine from black pepper works on the cytochrome metabolism and P-gp level, it may very well be worth considering but haven't seen it done

 

Things that have been studied are detailed here

The Quest to Enhance the Efficacy of Berberine for Type-2 Diabetes and Associated Diseases: Physicochemical Modification Approaches

 

the phospholipid-berberine complexes including things like encapsulating it in lecithin seem to have some significant effects on bioavailability in studies but wasn't able to personally tell how effective it was, lets just say I had lots of experiments happening.