Berberine prevents heart failure through endothelial and calcium function

 2021.8.9: 9.4: health/diet/heart/Berberine/
prevents heart failure through endothelial and calcium function:

GreenMedInfo Research Group July 30th 2021

https://www.greenmedinfo.com/blog/seven-herbs-and-supplements-heart-failure

. something extracted from berberine

is blocking calcium influx, thereby reducing

the risk of heart failure.

Acta Pharmacol Sin. 2010

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4002834/

Min-you Qi, Yu Feng, De-zai Dai, Na Li, Yu-si Cheng, Yin Dai. 

CPU86017, a berberine derivative, attenuates cardiac failure

through normalizing calcium leakage 

and downregulated phospholamban 

and exerting antioxidant activity. 

Front Physiol. 2020

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7546405/

Miyesaier Abudureyimu, Wenjun Yu, et al.

Berberine Promotes Cardiac Function by 

Upregulating PINK1/Parkin-Mediated Mitophagy in Heart Failure. 

. enhancing endothelial function helps heart:

Cardiovasc Drug Rev. 2001 

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2999047/

C W Lau, X Q Yao, Z Y Chen, W H Ko, Y Huang. 

Cardiovascular actions of berberine. 

. "Endothelial dysfunction is an important early event in the

pathogenesis of atherosclerosis. 

The mechanisms underlying endothelial injury are numerous

and linked to metabolic alteration. 

In obesity and insulin resistance, 

the increased secretion of proinflammatory cytokines 

and decreased secretion of adiponectine, 

the increased circulating levels of free fatty acids, 

and hyperglycaemia may alter gene expression and cell signalling in the vascular endothelium, 

contributing to changes in the release of endothelium derived factors. 

Dysfunctional endothelium is characterized by activation of NADPH oxidase, 

uncoupling of endothelial nitric oxide synthase (eNOS), 

increased expression of endothelin-1, 

an imbalance between the production of vasodilators and vasoconstrictor mediators, 

and induction of adhesion molecules

[31]. 

The altered endothelial homeostasis, in turn, 

contributes to plaque initiation and progression. 

It is associated with most cardiovascular disease, such as 

hypertension, coronary artery disease, chronic heart failure, 

peripheral artery disease, diabetes and chronic renal failure

[32]. 

Endothelial cells exposed to hypercholesterolemia show a 

reduced capacity to release endothelium-derived relaxing factors, 

because of LDLc promotion of endothelial eNOS downregulation

[33]. 

Lowering cholesterol levels appears to improve endothelial function

[34]. 

In diabetes and insulin resistance, other mechanisms may trigger endothelial dysfunction. 

Insulin signalling is altered in these two conditions, 

and affects the pathway leading to phosphorylation and activation of eNOS, 

which is also, in this case, dramatically downregulated

[35]. 

eNOS represents a major weapon of endothelial cells to fight vascular disease. 

It generates nitric oxide (NO), whose role is to dilate blood vessels

and maintain vascular homeostasis by stimulating cGMP

[36]. 

Several studies have suggested a central role of endothelial AMPK

in maintaining physiological functions, such as

mediation of eNOS activation in response to shear stress

[37], 

modulation of endothelial cell energy supply

[38], 

protection from apoptosis

[39] 

and regulation of inflammation, angiogenesis, and maintenance of perfusion

[40,41]. 

Impairment of endothelium dependent relaxation (EDR) 

represents reduced eNOS derived NO bioavailability, 

and is the first step in endothelial injury. 

It is present also in the absence of vessel damage. 

In 2000, Ko et al[42], by in vitro investigation, 

demonstrated that BBR has not only vasorelaxant 

but also antiproliferative effects. 

According to their results, BBR could act both on the endothelium 

and on the underlying vascular smooth muscle cells to induce relaxation 

(Figure (Figure1).1). 

NO, is likely involved in the EDR. 

More recently, this mechanism has been clarified in endothelial cells isolated from rat. 

It was confirmed that the vasodilatant effect of BBR

was mediated by eNOS leading to NO production 

through activation of the AMPK cascade. 

Moreover, BBR counteracts several adverse effects of hyperglycemia on the endothelium, 

including the inhibition of high glucose-induced reactive species 

intracellular accumulation and cellular apoptosis and inflammation, 

which characterize vascular injury

[31,43]. 

Another recognized effect of BBR is the significant decrease in

the number of adherent monocytes on endothelial cells, 

which is a key event in the early stages of atherosclerosis. 

Furthermore, BBR suppresses the activation of the 

nuclear factor-κB (NF-κB), 

the expression of adhesion molecules (VCAM-1 and ICAM-1) 

induced by hyperglycemia

and the high glucose-induced elevation of several pro-inflammatory cytokines and chemokines, 

including tumor necrosis factor-α, IL1-β, IL8 and MCP1, 

which are other targets of NF-κB 

involved in the development of atherosclerotic plaques

[43]"

fig 1:

. Berberine enhances endothelial function 3 ways:

it affects AMPK (Adenosine mono-phosphate kinase)

that affects eNOS (Endothelial nitric oxide synthase);

it lowers LDL-cholesterol and triglycerides;

and, it improves insulin sensitivity.

enzymedica Berberine 60 /$20.62

https://www.lifeextension.com/vitamins-supplements/item53349/berberine

Enteric-coated to prevent self-aggregation and formation of berberine crystals that reduce absorption.

Enzymedica's Berberine is provided in a

targeted delivery capsule 

to prevent release of berberine in the stomach. 

since in an acidic environment, berberine will bind with other berberine molecules

to form insoluble complexes that do not get absorbed. 

Prevention of the formation of these complexes

may improve the absorption of berberine.

Amount Per Serving

Berberine HCI (97%) (from berberis vulgaris extract) (seed) 500 mg

Leucine 50 mg

Other Ingredients: 100% vegetarian capsule (cellulose, gellan gum, water), 

rice concentrate, calcium laurate

[Calcium laurate helps powders flow into capsules 

and holds those powders together.]

Dr. Michael Murray:

https://www.iherb.com/pr/enzymedica-berberine-60-capsules/81507

"Berberine is commonly harvested from the flesh, roots or bark of plants 

like barberry, goldenseal and Oregon grape. 

Unlike many other formulas, this product is sustainably sourced from 

barberry seeds and does not require the plant to be sacrificed in its production.

sublingual instead of enteric coated?

Nutricology, Berberine 500, 90

https://www.iherb.com/pr/nutricology-berberine-500-90-vegetarian-capsules/82073

Hydroxypropyl methylcellulose, 

Nu-MAG® (rice extract, rice hulls, gum arabic, sunflower oil), 

silicon dioxide, microcrystalline cellulose.

https://ribus.com/nu-mag/

Nu-MAG offers formulators a Certified Organic alternative to Magnesium Stearate, 

so organic tablets requiring a lubricant can now be produced. 

Thorne Research, Berbercap, 60 

https://www.iherb.com/pr/thorne-research-berbercap-60-capsules/18577

Microcrystalline cellulose, leucine, silicon dioxide.

Berberis concentrate berberine HCl 85%.

Berberine HCl (from Indian Barberry extract) (root) (Berberis aristata) 200 mg

Whitaker Nutrition, Clinical Grade, Berberine, 90 Capsule

https://www.iherb.com/pr/whitaker-nutrition-clinical-grade-berberine-1-500-mg-90-capsules/101131

Berberine Hydrochloride (BerberPure™) 500 mg (take 3)

Microcrystalline cellulose, gelatin, magnesium stearate, gum acacia, silica.