Kyle J. Norton
The CETP inhibitor is a class of drugs that inhibit cholesteryl ester transfer protein (CETP) associated with the risk of atherosclerosis (a cardiovascular disease) by improving blood lipid levels in the arteries.
Cardiovascular disease is a group of conditions triggered by the abnormal function of the heart and blood vessels abnormality.
The 3 most common forms of cardiovascular disease in North America are coronary artery disease, peripheral artery disease, and carotid artery disease caused by plaque build-up of plaque in the arteries that supply blood to the heart, the arms and legs, and the brain, respectively.
Atherosclerosis is a medical condition caused by plaques accumulated on the wall of the arteries, leading to narrowing the arteries in transporting oxygenated blood to the heart and other parts of the body.
Depending on the blood obstruction, atherosclerosis can induce different types of heart disease and stroke.
Plaque is made of cholesterols, calcium, and other toxic substances, including cadmium.
According to the statistics provided by Atherosclerosis Open Acess, 32% of deaths account for atherosclerosis. 13.8% prevalence is among adults of 20 years and above. In 2010, the coronary heart disease mortality rate was about 60%.
Risk factors of atherosclerosis include high blood pressure and cholesterol, diabetes, being overweight or obese, an unhealthy diet, a family history of heart disease, and physical inactivity, particularly smoking.
Some researchers suggested that since cholesterol makes up a big part of the plaque, an unhealthy diet with high saturated trans fat, red meat, and processed meat may be the major cause of atherosclerosis.
Ursolic acid is a phytochemical in the subclass of Triterpenoid, belongings to the group of Terpenes found abundantly in apples, basil, bilberries, cranberries, peppermint, lavender, oregano, hawthorn, prunes., etc.
In finding a potential phytochemical for the treatment of diseases associated with high blood lipids,
researchers examined the cholesteryl ester transfer protein (CETP) for the prevention and treatment of cardiovascular diseases.
According to the analysis of the activity of a series of ursolic acid 3β-ester derivatives CETP inhibiting activities.* The most active compound is U12 with an IC50 value of 2.4 μM.
* More precisely, the possible hydrogen bond interactions between the carboxyl groups at both ends of the molecule skeleton and several polar residues (such as Ser191, Cys13, and Ser230) in the active site region of CETP could significantly enhance the inhibition activity.
After talking about other factors into account, researchers said, "This study provides structural insight of the interactions between these pentacyclic triterpenoid 3β-ester derivatives".
Taken altogether, ursolic acid may be considered a CETP inhibitor for the inhibition of high blood cholesterol, pending the confirmation of the larger sample size and multicenter human study.
Intake of tocopherols in the form of supplements should be taken with extreme care to prevent overdose acute liver toxicity.
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Author Biography
Kyle J. Norton (Scholar, Master of Nutrition, All right reserved)
Health article writer and researcher; Over 10.000 articles and research papers have been written and published online, including worldwide health, ezine articles, article base, health blogs, self-growth, best before it's news, the Karate GB Daily, etc.,.
Named TOP 50 MEDICAL ESSAYS FOR ARTISTS & AUTHORS TO READ by Disilgold.com Named 50 of the best health Tweeters Canada - Huffington Post
Nominated for shorty award over last 4 years
Some articles have been used as references in medical research, such as the international journal Pharma and Bioscience, ISSN 0975-6299.
Sources
(1) Synthesis, biological evaluation and SAR studies of ursolic acid 3β-ester derivatives as novel CETP inhibitors by Chen C1, Sun R2, Sun Y3, Chen X3, Li F3, Wen X4, Yuan H5, Chen D. (PubMed).
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