Coq10 Vitamin
Coenzyme Q 10 (also known as ubiquinone , ubidecarenone , coenzyme Q , and abbreviated at times to CoQ 10 – pronounced like "ko-cue-ten" –, CoQ , Q10 , or simply Q ) is a 1,4-benzoquinone, where Q refers to the quinone chemical group, and 10 refers to the number of isoprenyl chemical subunits.
This oil-soluble substance is present in most eukaryotic cells, primarily in the mitochondria. It is a component of the electron transport chain and participates in aerobic cellular respiration, generating energy in the form of ATP. Ninety-five percent of the human body’s energy is generated this way. Therefore, those organs with the highest energy requirements—such as the heart and the liver—have the highest CoQ 10 concentrations.
Occurrence in nature
Fresh tissue samples from both mackerel and herring found the concentration of Coenzyme Q10 to be higher in the heart tissue (105-148 μg/g) compared to concentrations found in the body tissue. The red tissue of mackerel contained a higher concentration (67μg/g) of CoQ10 than the white tissue (15μg/g) whilst in herring tissue the concentration was found to range between 15–24 μg/g. A small seasonal variance in the concentrations of CoQ10 was observed in both fish .
Effect of heat
Cooking by frying reduces CoQ 10 content by 14-32%.
Discovery
Coenzyme Q 10 was first discovered by Professor Fredrick L. Crane and colleagues at the University of Wisconsin–Madison Enzyme Institute in 1957. In 1958, its chemical structure was reported by Dr. Karl Folkers and coworkers at Merck; in 1968, Folkers became a Professor in the Chemistry Department at the University of Texas at Austin.
Chemical properties
The oxidized structure of CoQ 10 is shown on the top right. The various kinds of Coenzyme Q can be distinguished by the number of isoprenoid side-chains they have. The most common Coenzyme Q in human mitochondria is CoQ 10 . The 10 refers to the number of isoprene repeats. The image below has three isoprenoid units and would be called Q 3 .
Biochemical role
CoQ 10 is found in the membranes of many organelles. Since its primary function in cells is in generating energy, the highest concentration is found on the inner membrane of the mitochondrion. Some other organelles that contain CoQ 10 include endoplasmic reticulum, peroxisomes, lysosomes, and vesicles.
Biosynthesis
The benzoquinone portion of coenzyme Q 10 is synthesized from tyrosine, whereas the isoprene sidechain is synthesized from acetyl-CoA through the mevalonate pathway. The mevalonate pathway is also used for the first steps of cholesterol biosynthesis.
Absorption and metabolism
Absorption
CoQ 10 is a crystalline powder that is insoluble in water due to its low polarity. It has a relatively high molecular weight (863 g/mol) and its solubility in lipids is also limited so it is very poorly absorbed in the gastrointestinal tract. , Absorption follows the same process as that of lipids and the uptake mechanism appears to be similar to that of vitamin E, another lipid-soluble nutrient. Emulsification and micelle formation is required for the absorption of fats. For CoQ 10 , this process is chiefly facilitated by secretions from the pancreas and bile salts in the small intestine. A general rule is that the higher the dose orally administered, the lower the percent of the dose absorbed.
Metabolism
Data on the metabolism of CoQ 10 in animals and humans are limited. A study with 14 C-labeled CoQ 10 in rats showed most of the radioactivity in the liver 2 hours after oral administration when the peak plasma radioactivity was observed, but it should be noted that CoQ 9 is the predominant form of coenzyme Q in rats. It appears that CoQ 10 is metabolised in all tissues, while a major route for its elimination is biliary and fecal excretion. After the withdrawal of CoQ 10 supplementation, the levels return to their normal levels within a few days, irrespective of the type of formulation used.
Factors affecting CoQ 10 levels
Various factors reduce the concentration of CoQ 10 in different organs; the following are known:
- Use of statins reduce CoQ 10 levels — see below.
- Aging, in individuals older than 20 years, reduces CoQ 10 levels in internal organs.
- UV exposure reduces CoQ 10 levels in the skin.
Inhibition by statins and beta blockers
Coenzyme Q 10 shares a common biosynthetic pathway with cholesterol. The synthesis of an intermediary precursor of coenzyme Q 10 , mevalonate, is inhibited by some beta blockers, blood pressure-lowering medication, and statins, a class of cholesterol-lowering drugs. Statins can reduce serum levels of coenzyme Q 10 by up to 40%. Some research suggests the logical option of supplementation with coenzyme Q 10 as a routine adjunct to any treatment that may reduce endogenous production of coenzyme Q 10 , based on a balance of likely benefit against very small risk.
Pharmacokinetics
Some reports have been published on the pharmacokinetics of CoQ 10 . The plasma peak can be observed 2–6 hours after oral administration, mainly depending on the design of the study. In some studies, a second plasma peak was also observed at about 24 hours after administration, probably due to both enterohepatic recycling and redistribution from the liver to circulation. Tomono et al. used deuterium-labelled crystalline CoQ10 to investigate pharmacokinetics in human and determined an elimination half-time of 33 hours.
Improving the bioavailability of CoQ 10
The importance of how drugs are formulated for bioavailability is well known. In order to find a principle to boost the bioavailability of CoQ 10 after oral administration, several new approaches have been taken and different formulations and forms have been developed and tested on animals or humans.
Reduction of particle size
The obvious strategy is reduction of the particle size to as low as the micro- and nano-scale. Nanoparticles have been explored as a delivery system for various drugs and an improvement of the oral bioavailability of drugs with poor absorption characteristics has been reported; the pathways of absorption and the efficiency were affected by reduction of particle size. This protocol has so far not proved to be very successful with CoQ 10 , although reports have differed widely. , The use of the aqueous suspension of finely powdered CoQ 10 in pure water has also only revealed a minor effect.
Soft-gel capsules with CoQ10 in oil suspension
A successful approach was to use the emulsion system to facilitate absorption from the gastrointestinal tract and to improve bioavailability. Emulsions of soybean oil (lipid microspheres) could be stabilised very effectively by lecithin and were utilised in the preparation of soft gelatine capsules. In one of the first such attempts, Ozawa et al. performed a pharmacokinetic study on beagle dogs in which the emulsion of CoQ 10 in soybean oil was investigated; about two times higher plasma CoQ 10 level than that of the control tablet preparation was determined during administration of a lipid microsphere. Although an almost negligible improvement of bioavailability was observed by Kommuru et al. with oil-based soft-gel capsules in a later study on dogs, the significantly increased bioavailability of CoQ 10 was confirmed for several oil-based formulations in most other studies.
Novel forms of CoQ10 with increased water-solubility
Facilitating drug absorption by increasing its solubility in water is a common pharmaceutical strategy and has also been shown to be successful for Coenzyme Q 10 . Various approaches have been developed to achieve this goal, with many of them producing significantly better results over oil-based soft-gel capsules in spite of the many attempts to optimize their composition. Examples of such approaches are use of the aqueous dispersion of solid CoQ 10 with tyloxapol polymer, formulations based on various solubilising agents, i.e. hydrogenated lecithin, and complexation with cyclodextrins; among the latter, complex with β-cyclodextrin has been found to have highly increased bioavailability. and is also used in pharmaceutical and food industry for CoQ 10 -fortification. Also some other novel carrier systems like liposomes, nanoparticles, dendrimers etc can be used to increase the bioavailability of Coenzyme Q 10 .
Supplementation
Because of its ability to transfer electrons and the
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