Tiếng ViệtThings to know about Curcumin
Turmeric is a curry spice native to India that has attracted great interest in recent decades because of its bioactive curcuminoids (curcumin, demethoxycurcumin and bisdemethoxycurcumin).
The medicinal applications of turmeric have been known for thousands of years, especially in Ayurvedic therapy, which uses turmeric to treat stomach disorders, as a tonic, detoxifies the blood, as well as for prevention or treatment of skin diseases.
The potential applications of curcumin are increasingly being studied further and expanded.
1. Chemical composition
The chemical composition of turmeric (scientific name is Curcuma longa) consists of about 70% carbohydrates, 13% water, 6% protein, 6% essential oils (phellandrene, sabinene, cineol, borneol, zingiberene and sesquiterpenes), 5% fat, 3% minerals (potassium, calcium, phosphorus, iron and sodium), 3–5% curcuminoids and small amounts of vitamins (B1, B2, C and niacin).
Curcumin (CUR), demethoxycurcumin (DMC) and bisdemethoxycurcumin (BMC) are bioactive polyphenolic compounds identified in turmeric, collectively known as curcuminoids (CCM). Among curcuminoids, CUR accounts for approximately 77%, DMC accounts for 17% and BMC accounts for 3–6%. According to the U.S. Food and Drug Administration (FDA), curcuminoids are generally recognized as safe (GRAS).
Curcumin (1,7-bis-(4-hydroxy-3-methoxyphenyl)-hepta-1,6-diene-3,5-dione), an lipophilic polyphenol, is the main yellow biological component of turmeric. Curcumin comes in two forms, tautomeric, keto-, and enol. Curcumin is practically insoluble at room temperature in aqueous solutions at neutral and acidic pH, but soluble in organic solvents such as methanol, ethanol, acetone and dimethyl sulfoxide.
CUR has mainly three reaction sites, as illustrated in figure 1, a hydrogen atom donor, a Michael acceptor, and a metal chelator. The α,β-unsaturated β-diketone part of CUR is a strong metal chelating agent and complexing with several known metal ions. CUR’s ability to chelate metals has shown great potential as a therapeutic agent against diseases such as Alzheimer’s, cancer, depression, and arthritis.
2. Biological activity
CUR has the ability to directly interact with many signaling molecules and has been shown to have activity against various diseases, including cancer, cardiovascular disease, neurological disease, and autoimmune disease. CUR exhibits anti-inflammatory, antioxidant, antitumor, antiviral and neurotrophic activity and is therefore promising as a therapeutic agent for the prevention and treatment of a number of disorders.
CUR can regulate a number of biomolecules (including transcription factors, growth factors, inflammatory mediators, cytokines, cell cycle proteins, enzymes, protein kinases, and cell death proteins) and cell biology pathways.
CUR regulates tumor growth through regulation of multiple signaling pathways, including cell survival, tumor suppressor, caspase pathway, protein kinase and the programmed death response receptor pathway.
CUR can inhibit the activation of nuclear factor kappa B (NF-K B) of transcription factor, which is responsible for cell survival, cytokine production, and other cellular functions. .
CUR downregulates signal transduction and transcriptional activation (STAT) proteins, which are essential for cell growth, differentiation, and survival. STAT proteins are also involved in the development, function, and clearance of the immune system. Curcumin upregulates the leucine zipper protein NrF2, which regulates the expression of antioxidant properties that protect cells from oxidative stress.
CUR complexes with all metals such as Al3+, which is implicated in Alzheimer’s disease, or binds directly to small β-amyloid species to prevent aggregation and fibrillation. CUR reduces heavy metal toxicity (oxidative stress) by forming stable complexes with heavy metals such as copper (Cu), chromium (Cr), arsenic (As), mercury (Hg), lead (Pb) and cadmium (Cd).
3. Bioavailability
Although curcumin has been shown to be effective against many human diseases, its bioavailability is poor due to poor absorption, rapid metabolism and its short half-life in the gastrointestinal tract has been shown to limit its therapeutic efficacy. Another difficulty with CUR is its poor stability under physiological conditions. For example, at 37°C and neutral pH (7.2), curcumin t1/2 was reported under 10 min.
Therefore, many attempts have been made to improve the bioavailability of curcumin by altering these features. Various chemical modifications of CUR (including the use of liposomes, nanoparticles, micelles, phospholipid complexes, polymers, excipients) have been developed to improve the solubility, bioavailability of curcumin, longer cycle time and movement to the required position.
The use of adjuvants that can block the metabolism of CUR is the most common strategy to increase the bioavailability of CUR. The efficacy of the combination of piperine, a known inhibitor of hepatic and intestinal glucuronidation, was evaluated on the bioavailability of curcumin in healthy volunteers. In humans receiving only a single 2g dose of curcumin, serum curcumin concentrations were undetectable or very low.
However, co-administration of 20 mg of piperine with curcumin produced much higher concentrations within 30 minutes to 1 hour of drug treatment, with piperine increasing the bioavailability of curcumin by 2000%.
Micro-nanoformulas have attracted great attention because of the advantages associated with them, including increased solubility, improved cellular uptake, target specificity), reduced degradation, increased bioavailability, circulation time and ADME profiles (Absorption, Distribution, Metabolism, Elimination- absorption, distribution, metabolism and elimination).
References:
- R. R. Kotha and D. L. Luthria, “Curcumin: Biological, Pharmaceutical, Nutraceutical, and Analytical Aspects”, Molecules, vol 24, p.h 16, p. 2930, August 2019, doi: 10.3390/molecules24162930.
- A. W. K. Yeung et al., “Curcumin: Total-Scale Analysis of the Scientific Literature”, Molecules, vol. 24, p.h. 7, p. 1393, April 2019, doi: 10.3390/molecules24071393.
- G. Shoba, D. Joy, T. Joseph, M. Majeed, R. Rajendran, and P. S. Srinivas, “Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers”, Planta Med, vol. 64, no. 4, pp 353–356, May 1998, doi: 10.1055/s-2006-957450.
Article source: Nutrition Research and Development Institute (https://inrd.vn/)
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