Anti-inflammatory Effect of Palmitoylethanolamide PEA 544-31-0 on Human Adipocytes

Anti-inflammatory 

Effect of Palmitoylethanolamide on Human Adipocytes

Obesity leads to the appearance of an inflammatory process, which can be initiated even with a moderate weight gain. 

Palmitoylethanolamide (PEA) is an endogenous lipid, secreted by human adipocytes, that possesses numerous anti-inflammatory properties. 

The main purpose of this study was to investigate the anti-inflammatory effect of PEA on human adipocytes, as well as in a murine model. The production of tumor necrosis factor–α (TNF-α) by lipopolysaccharide (LPS)-treated human subcutaneous adipocytes in primary culture and CF-1 mice was investigated by enzyme-linked immunosorbent assay. The effects of PEA on adipocyte TNF-α secretion were explored as well as some suspected PEA anti-inflammatory pathways: nuclear factor–κB (NF-κB) pathway, peroxisome proliferator-activated receptor–α (PPAR-α) gene expression, and TNF-α-converting enzyme (TACE) activity. The effects of PEA on the TNF-α serum concentration in intraperitoneally LPS-treated mice were also studied. We demonstrate that the LPS induced secretion of TNF-α by human adipocytes is inhibited by PEA. This action is neither linked to a reduction in TNF-α gene transcription nor to the inhibition of TACE activity. Moreover, PPAR-α is not implicated in this anti-inflammatory activity. 

Lastly, PEA exhibits a wide-reaching anti-inflammatory action as the molecule is able to completely inhibit the strong increase in TNF-α levels in the serum of mice treated with high doses of LPS. 

In view of its virtual lack of toxicity, PEA might become a potentially interesting candidate molecule in the prevention of obesity-associated insulin resistance.

PQQ （Pyrroloquinoline quinone/ Methoxatin）72909-34-3 - An Essential Micronutrient That Helps You Thrive

PQQ （Pyrroloquinoline quinone/ Methoxatin）72909-34-3

 - An Essential Micronutrient That Helps You Thrive

PQQ (pyrroloquinoline quinone), a novel cofactor with B vitamin like-activity and antioxidant function, provides powerful support for a wide range of functions in the body. 

The antioxidant status of PQQ is 5,000 times more potent than vitamin C. 

PQQ supplement has the potential to stimulate mitochondrial function (the primary energy source in cells) and protects from excessive oxidative damage, a major cause of rapid cell aging. 

PQQ can strongly scaveng free radicals, reduce damage from excessive stress and keep you look healthy and young.

It is a commanding nutrient with remarkable potential!

Neuroprotective activity

PQQ has been shown to optimize health and function of the entire central nervous system. It reverses cognitive impairment caused by chronic oxidative stress in pre-clinical models, improving performance on memory tests.

Mitochondrial biogenesis

Mitochondrial dysfunction has been definitively linked to virtually all killer diseases of aging, from Alzheimer’s disease and type 2 diabetes to heart failure. PQQ has been shown to induce mitochondrial biogenesis—the growth of new mitochondria in aging cells!

Prevention of memory loss

A randomized, double-blind study released in 2009 looked at the the effect of PQQ and CoQ10 supplementation over a 3 month period on 71 middle aged individuals.  What they found is that memory, attention, and cognition improved in individuals supplementing with PQQ and this affect was enhanced even more when taking both PQQ and CoQ10 together.

Cardiovascular health 

In a study in 2006 using animal models, PQQ was actually shown to be superior to a well known beta-blocker (metoprolol) in reducing oxidative damage after a heart attack and resulted in reduced area of cardiac tissue death and improved overall cardiac function.

Anti-oxidative activity

PQQ may be considered a super antioxidant because it is far more stable than most other antioxidants and can carry out more redox cycling reactions as a result of this.  It's been found to be 175 times more efficient than epicatechin (antioxidant found in chocolate), 200 times more efficient than quercetin (antioxidant found in green tea & various fruits & vegetables), and 5,000 times more efficient than vitamin C.

Wuxi Cima Science Co.,Ltd is an ingredients and raw materials manufacturer of herbal/botanical extracts, nutritional chemicals for the industry of food, beverage, nutraceutical, pharmaceuticals and cosmetic.

micronized palmitoylethanolamide (PEA)-transpolydatin in the treatment of chronic pelvic pain

Administration of micronized 

palmitoylethanolamide(PEA)-transpolydatin 

in the treatment of chronic pelvic pain in women affected by endometriosis: preliminary results

AIM: Aim of the study was to evaluate the effectiveness of micronized palmitoylethanolamide (PEA)-transpolydatin in the treatment of chronic pelvic pain in women affected by endometriosis.; 

METHODS: Twenty-four patients with suspected endometriosis affected by severe pelvic pain were enrolled. All patients received two tablets a day of PEA 400 mg and 40 mg polydatin for 90 days consecutively. A Visual Analogic Scale was used for the assessment of the severity of global pain, dysmenorrhea, dyspareunia, dysuria and dischezia. A second questionnaire was submitted to patients to assess the quality of life. The compilation of a diary lead us to evaluate the monthly assumption of any painkillers. Patients were evaluated at the begin of the treatment and then monthly until the end of the study (90 days). The statistical analysis was performed by using the ANOVA for the analysis of variance.; 

RESULTS: Statistically significant results were found in relation to pelvic pain, dysmenorrhea and dyspareunia compared to the initial evaluation of patients. Results related to dysuria and dischezia were not statistically significant (P>0.05). The decrease in pelvic pain leads to an improvement of the quality of life of patients. A decreased assumption of nonsteroidal anti-inflammatory drugs (NSAIDs) was also observed.; 

CONCLUSION: PEA could be considered an effective supplement to conventional analgesic therapies in the management of pelvic pain related to endometriosis.

source: http://www.knowledge.scot.nhs.uk/together/search-results.aspx?q=publicid%3a%22OVIDmedl%7c24051945%22&pm=fql&expand=true

Palmitoylethanolamide (PEA) 544-31-0 , take home message

PEA (palmitoylethanolamide) 544-31-0 : A new body own painkiller

A new body own painkiller---

PEA (palmitoylethanolamide) 544-31-0

results confirmed by more than 40 clinical trials.

PROPERTY

Chemicalformula    :     C18H37NO2

CAS NO.   :    544-31-0

Molarmass   :  299.49 g·mol−1

Appearance    :  White crystals

Density    :   910 mg mL−1

Meltingpoint   :59-60 °C(332-333 K)

Boilingpoint   :461.5 °C(735 K)

MAIN FUNCTIONS

anti-inflammatory

anti-nociceptive

neuroprotective

anticonvulsant 

Dr Keppel Hesselink, holding a chair in molecular pharmacologist at the University of Witten/Herdecke in Germany, presented the major breakthrough in chronic pain treatment during the annual neurological congress for Italian neurologists and pain specialists in November  2011. While nearly all painkillers available inhibit pain via the nerve cells, Keppel Hesselink pointed out that a totally different approach via the modulation of the so called glia cells has been overlooked. This approach now has resulted in dramatic improvements of pain in many patients. He expected this treatment to revolutionize the field of pain treatment.

On every nerve cell there are 10 glia cells in our nervous system, and these activated cells are responsible for keeping the body in a chronic pain state. The new compound modulates the glia cells via a body own regulating system and calms these cells, leading to less pain.

The professor pointed out that this compound, palmitoylethanolamide has been tested for safety and efficacy in clinical trials in more than 2000 patients.  Palmitoylethanolamide has also been used already with more than 800,000 patients in Italy, Germany and The Netherlands.

If any interests, pls keep me posted, price, coa/spec, sample... will be provided on request. wang@cimasci.com

Neuroprotective activities of palmitoylethanolamide in an animal model of Parkinson's disease

Neuroprotective activities 

of palmitoylethanolamide 

in an animal model of Parkinson's disease

The biochemical and cellular changes that occur following treatment with 1-methyl-4-phenyl-1,2,3,6-tetrahyropyridine (MPTP) are remarkably similar to that seen in idiopathic Parkinson's disease (PD). PD is characterized by the degeneration of dopaminergic nigrostriatal neurons, which results in disabling motor disturbances. Activation of glial cells and the consequent neuroinflammatory response is increasingly recognized as a prominent neuropathological feature of PD. There is currently no effective disease-modifying therapy. Targeting the signaling pathways in glial cells responsible for neuroinflammation represents a promising new therapeutic approach designed to preserve remaining neurons in PD. Chronic treatment with palmitoylethanolamide (PEA, 10 mg/kg, i.p.), initiated 24 hr after MPTP injection (20 mg/kg), protected against MPTP-induced loss of tyrosine hydroxylase positive neurons in the substantia nigra pars compacta. Treatment with PEA reduced MPTP-induced microglial activation, the number of GFAP-positive astrocytes and S100β overexpression, and protected against the alterations of microtubule-associated protein 2a,b-, dopamine transporter-,nNOS- positive cells in the substantia nigra. Furthermore, chronic PEA reversed MPTP-associated motor deficits, as revealed by the analysis of forepaw step width and percentage of faults. Genetic ablation of peroxisome proliferator activated receptor (PPAR)-α in PPAR-αKO mice exacerbatedMPTP systemic toxicity, while PEA-induced neuroprotection seemed be partially PPARα-dependent. The effects of PEA on molecules typically involved in apoptotic pathways were also analyzed. Our results indicate that PEA protects against MPTP-induced neurotoxicity and the ensuing functional deficits even when administered once the insult has been initiated.

Palmitoylethanolamide(PEA) is effective in treating temporomandibular joint(TMJ) inflammatory pain

Palmitoylethanolamide 

versus a nonsteroidal anti-inflammatory drug 

in the treatment of temporomandibular joint inflammatory pain.

AIMS: To carry out a randomized clinical trial to compare the effect of palmitoylethanolamide (PEA) versus ibuprofen, a nonsteroidal anti-inflammatory drug (NSAID), for pain relief in temporomandibular joint (TMJ) osteoarthritis or arthralgia. PEA acts as an endogenous agent with an autacoid local inflammation antagonism and modulates mast cell behavior controlling both acute and chronic inflammation. METHODS: A triple-blind randomized clinical trial was conducted on 24 patients (16 women and 8 men) aged 24 to 54 years and suffering from TMJ osteoarthritis or arthralgia. The patients were enrolled from a group of 120 consecutive patients referred to the University of Bologna's Department of Orthodontics. Patients were randomly divided into two groups: group A (12 subjects) received PEA 300 mg in the morning and 600 mg in the evening for 7 days and then 300 mg twice a day for 7 more days. Group B (12 subjects) received ibuprofen 600 mg three times a day for 2 weeks. Every patient recorded the intensity of spontaneous pain on a visual analog scale twice a day. Maximum mouth opening was recorded by a blind operator during the first visit and again after the 14th day of drug treatment. A t test was used for data comparisons.

RESULTS: Pain decrease after 2 weeks of treatment was significantly higher in group A than in group B (P =.0001); maximum mouth opening improved more in group A than in group B (P =.022).


CONCLUSION: These data suggest that PEA is effective in treating TMJ inflammatory pain.

New Thought : Palmitoylethanolamide (PEA) for autism

A research had been carried out on the anti-inflammatory effect of both Luteolin and Palmitoylethanolamide (PEA).  PEA is not a flavonoid, but it is naturally occurring within the body and has some very interesting properties. 

One of the inflammatory markers that is raised in autism is called IL-6.  The research was on arthritis in mice, but it did measure the effect of Luteolin and PEA on IL-6.  The result was interesting:-

PEA had the greater effect, but in combination with Luteolin the result improved further. 
This gives yet more reason to look into PEA for autism, but not to forget Luteolin.

Palmitoylethanolamide (PEA) 544-31-0 —— USEFUL FOR ALL KINDS OF CHRONIC PAIN

Palmitoylethanolamide

——A Natural Body-Own Anti-Inflammatory Agent, USEFUL FOR ALL KINDS OF CHRONIC PAIN

INTRODUCTION

Palmitoylethanolamide (PEA) is a food component known since 1957. PEA is synthesized and metabolized in animal cells via a number of enzymes and exerts a multitude of physiological functions related to metabolic homeostasis. Research on PEA has been conducted for more than 50 years, and over 350 papers are referenced in PubMed describing the physiological properties of this endogenous modulator and its pharmacological and therapeutical profile.The major focus of PEA research, since the work of the Nobel laureate Levi-Montalcini in 1993, has been neuropathic pain states and mast cell related disorders. However, it is less known that 6 clinical trials in a total of nearly 4000 people were performed and published last century, specifically studying PEA as a therapy for influenza and the common cold. This was done before Levi-Montalcini’s clarification of PEA’s mechanism of action, analyzing the role of PEA as an anti-inflammatory agent. 

PROPERTY

Chemicalformula    :     C18H37NO2

CAS NO.   :    544-31-0

Molarmass   :  299.49 g·mol−1

Appearance    :  White crystals

Density    :   910 mg mL−1

Meltingpoint   :59-60 °C(332-333 K)

Boilingpoint   :461.5 °C(735 K)

MAIN FUNCTIONS

anti-inflammatory

anti-nociceptive

neuroprotective

anticonvulsant 

Red Yeast Rice Helps Reduce Cholesterol and less heart attack

Red Yeast Rice 
Helps Reduce Cholesterol and Less Heart Attack

Red yeast rice comes from yeast (Monascus purpureus) that is grown on rice. This bright reddish purple fermented rice, which acquires its colour from being cultivated with the mold Monascus purpureus, is served as a dietary staple in some Asian countries. As food coloring, it gives Peking Duck its signature red glow. And as herbal medicine, it lowers cholesterol levels.

"It works much the way a statin would work, by reducing the amount of cholesterol that the liver makes, but in a much gentler level," said Dr. Christopher Cannon a cardiologist at Boston's Brigham and Women's Hospital.

This latest study published in the Annals of Internal Medicine followed 62 patients who had tried taking prescription statins, such as Lipitor or Zocor, but complained it left them with severe muscle pains.

In the study, all of the patients received counseling on nutrition and exercise. Additionally, half of the participants also took 1,800 mg of red yeast rice supplements every day. After 12 weeks, those taking the supplements saw LDL, the "bad cholesterol," drop by a remarkable 27 percent. Those who did not take the red yeast rice supplements saw their LDL drop by only 6 percent.

Only two patients on the supplements reported those persistent muscle pains.

"I was pleasantly surprised with the degree of LDL lowering," said Dr. Daniel Rader a lipid specialist at the University of Pennsylvania School of Medicine and an author of the study. "I have to confess, I did not expect this degree of LDL lowering. And there were many fewer side effects than expected."

Research published last year in the American Journal of Cardiology showed that heart attack patients in China who took a red yeast rice supplement daily were 45 percent less likely to have another attack within five years.

wang@cimasci.com

Red yeast rice for dyslipidemia in statin-intolerant patients: a randomized trial.

BACKGROUND: Red yeast rice is an herbal supplement that decreases low-density lipoprotein (LDL) cholesterollevel.

OBJECTIVE: To evaluate the effectiveness and tolerability of red yeast rice and therapeutic lifestyle change to treat dyslipidemia in patients who cannot tolerate statin therapy.

DESIGN: Randomized, controlled trial.

SETTING: Community-based cardiology practice. PATIENTS: 62 patients with dyslipidemia and history of discontinuation of statin therapy due to myalgias.

INTERVENTION: Patients were assigned by random allocation software to receive red yeast rice, 1800 mg (31 patients), or placebo (31 patients) twice daily for 24 weeks. All patients were concomitantly enrolled in a 12-week therapeutic lifestyle change program.

MEASUREMENTS: Primary outcome was LDL cholesterol level, measured at baseline, week 12, and week 24. Secondary outcomes included total cholesterol, high-density lipoprotein (HDL) cholesterol, triglyceride, liver enzyme, and creatinine phosphokinase (CPK) levels; weight; and Brief Pain Inventory score.

RESULTS: In the red yeast rice group, LDL cholesterol decreased by 1.11 mmol/L (43 mg/dL) from baseline at week 12 and by 0.90 mmol/L (35 mg/dL) at week 24. In the placebo group, LDL cholesterol decreased by 0.28 mmol/L (11 mg/dL) at week 12 and by 0.39 mmol/L (15 mg/dL) at week 24. Low-density lipoprotein cholesterollevel was significantly lower in the red yeast rice group than in the placebo group at both weeks 12 (P < 0.001) and 24 (P = 0.011). Significant treatment effects were also observed for total cholesterol level at weeks 12 (P < 0.001) and 24 (P = 0.016). Levels of HDL cholesterol, triglyceride, liver enzyme, or CPK; weight loss; and pain severity scores did not significantly differ between groups at either week 12 or week 24.

LIMITATION: The study was small, was single-site, was of short duration, and focused on laboratory measures.

CONCLUSION: Red yeast rice and therapeutic lifestyle change decrease LDL cholesterol level without increasing CPK or pain levels and may be a treatment option for dyslipidemic patients who cannot tolerate statin therapy.