Ursolic Acid Potent Antiinflammatory
Introduction to Ursolic Acid
Ursolic Acid (UA) is a substance that comes from a variety of
plants and herbs. It is part of a class of chemicals known as pentacyclic
triterpenoids. It is primarily recognized for its potential role in cell growth
regulation.
My Experience With Ursolic Acid
This is a supplement I like to take, but the issue is getting
quality ones. I tried the Labrada Nutrition one and I didn’t feel
anything. I then tried a higher quality one and it was very good.
1) Ursolic Acid has anti-inflammatory properties
Mechanism:
Cell culture study showed that Ursolic Acid enhanced autophagy (recycling)
of macrophages by increasing the production of ATG5 and ATG16L1, which
led to altered macrophage function (R).
Ursolic Acid normalized PPARa activity and inhibited the exaggerated spinal cord inflammatory
response and heightened pain sensitivity (R).
2) Ursolic Acid prevents memory impairment
One of the potential mechanisms of the neuroprotective effect
was by lessening the accumulation of
malondialdehyde (MDA) and depletion of glutathione (GSH) in thehippocampus
(memory center) (R).
UA significantly suppressed the increase of IL-1b, IL-6,
and TNF levels
in thehippocampus (memory center) of
Amyloid beta treated mice (R).
3) Ursolic Acid has anti-cancer properties
Ursolic Acid at high doses decreased the following cancer
markers: MMP-2, Ki-67, and CD34 (adhesion factor) (R).
UA treatment strongly blocked the cancer survival AKT – GSK3b –
β-catenin pathway, resulting in cell destruction (R).
Ursolic Acid is able to induce cell
destruction in human gut cancer cells by blocking the AKT pathway
(R).
Under toxic conditions, Ursolic Acid induces the production of various Nrf2 -mediated detoxifying/antioxidant enzymes (R).
Epigenetic effects of Ursolic Acid could potentially contribute to
its beneficial effects, including the prevention of skin
cancer (R).
Ursolic Acid could inhibit proliferation and reverse the drug
resistance of ovarian cancerous stem cells by suppressing ABCG2 and HIF-1a under
different culture conditions, such as low
oxygen (R).
4) Ursolic Acid has antimicrobial properties
Mycobacterial infections are controlled by the activation of
macrophages through type 1 cytokine production by T cells (R).
IFNy and TNF-a are essential for this process because they promote
macrophage activation and iNOS production (R).
Ursolic Acid and Oleic Acid stimulate IFNy production and also increase iNOS and TNF production through NF-kB activation
in mouseresting macrophages (R).
5) Ursolic Acid reduces post-stroke damage
Abrupt reoxygenation due to the rapid restoration of blood flow
is frequently associated with an exacerbation of tissue injury and an intense
inflammatory response that is triggered by inflammatory mediators, such as MMPs
(R).
Studies have shown that the activity of MMPs, particularly MMP9, is
markedly increased after obstruction of blood flow (R).
PPARy activation suppressed the inflammatory response in brain ischemia, and this finding suggests that
PPARy might be critical in cases where the brain is restricted of blood
(ischemia) (R).
6) Ursolic Acid has liver-protective properties
UA inhibited growth and induced cell
destruction of liver cancer cells through AMPK -mediated
inhibition of DNA methyltransferase 1 (through SP1) (R).
Increasing evidence suggests an important role of IGFBP in
the development and progression of several types of cancers (R).
7) Ursolic Acid combinations increase insulin sensitivity
The Ursolic Acid and Rosiglitazone combination ameliorated
HFD-induced glucose intolerance and insulin
resistance (R).
Ursolic acid was demonstrated to be an effective insulin-mimetic
agent at doses above 50 μg/ml and as an insulin-sensitizer at doses as low as 1
μg/ml (R).
Mechanism:
The treatment stimulated the IRS1, PI3-kinase, Akt,
and GLUT4 translocation and increases the production of insulin receptors
to improve glucose intolerance (R).
8) Ursolic Acid stimulates muscle growth
Ursolic acid enhances muscle insulin/ IGF-1 signaling, leading to Akt activation, muscle growth, and
reduced fat and blood glucose (R).
One human study which gave healthy participants 150mg ursolic
acid three times a day with meals for eight weeks alongside resistance training
noted that supplementation was able to increase circulating IGF-1 concentrations
by 22.8% relative to placebo (also given resistance training) (R).
Ursolic acid enhanced the production of
myoglobin (∼2
folds) in concert with remodeling of muscle fibers to mainly fast IIA (∼30%) and slow-twitch (∼4%) types (R).
Ursolic acid indirectly mimicked beneficial effects of
short-term calorie restriction and exercise (fast-oxidative) by directing the
muscle composition toward oxidative metabolism (R).
Ursolic acid appears to have weak activity as an aromatase
inhibitor (which would increase testosterone slightly) (R).
9) Ursolic Acid causes weight loss by increasing bodily energy
expenditure
Ursolic acid increased muscle Akt activity in high fat-fed mice.
Muscle Akt activity is known to increase energy expenditure and reduce obesity
and its complications (R).
A proteomic study showed that a closely related
triterpenoid activated insulin/IGF-I signaling, AMPK, JAK /Stat
signaling, NFkB and
retinoic acid transmission (R).
Another possibility is that ursolic acid increases fight or flight activity, which is known to
expand brown fat (R).
One study noted a decrease in circulating leptin levels
associated with ursolic acid in rat feed, which is dependent on weight
loss (R).
Potential Risks/Negatives
Due the potent endothelial cell death inducing activity of UA, a
systemic application of UA in the treatment of heart diseases
seems unfavorable. The DNA damaging activity of UA may however constitute a
serious problem (R).
Previous study has revealed that UA has the potential of sperm
motility inhibition. Specifically, it causes breaking of bridges in between
cells that are soon to be sperm, and the damaged cells then collect to form
symplasts in the seminiferous tubules that are associated with male infertility
(R).
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