plant nutraceuticals

Chapter 32 The plant nutraceuticals



A number of plant nutraceuticals are common food constituents, and extracts of many others are used as nutraceuticals.


There are a number of definitions of nutraceuticals, but the first and most straightforward is that coined by De Felice, of the Foundation of Innovation in Medicine, who defined a ‘nutraceutical’ as a ‘food, or parts of a food, that provide medical or health benefits, including the prevention and treatment of disease’.


Nutraceuticals are rarely legally classed as medicines, but instances exist in certain countries for particular entities, for example coenzyme Q10 in Japan and melatonin in the UK. This consequent lack of regulation for most nutraceuticals has resulted in a number of poor quality products being available on the market.


There are a number of sources of nutraceuticals, including basic human and mammalian metabolites, dietary components of plant and animal origin, synthetic constituents and plant secondary metabolites; increasingly, they are also produced by microbial fermentation. Arguably the greatest number are derived from plants and are used either as single purified components, such as resveratrol, purified multi-component products, such as pycnogenol, or whole plant foods, such as flaxseed. The most researched nutraceuticals of plant origin are those derived from soy and tea, but large numbers of scientific and medical publications relate to the constituents of grapes and wine, and also the many plants rich in polyphenolic components. Table 32.1 lists plant sources and therapeutic activities of a number of commercially available single-component nutraceuticals, which often occur in a number of plants. Various purified multi-component nutraceuticals are also obtained from specific plants (Table 32.2). Those from grape, soy and tea could realistically be obtained from the diet. Increasingly, a number of foods are being promoted as sources of nutraceuticals specifically for consumers who prefer eating a healthy diet instead of taking supplements; Table 32.3 depicts a wide variety of such products. The last group of nutraceuticals occurs in the plant kingdom either widely, such as coenzyme Q10 and S-adenosylmethionine (SAMe), or only in a few specific plants but at insubstantial levels, and are therefore not suitable for realistic incorporation in the diet. These latter nutraceuticals are often produced by chemical or biotechnological synthesis (Table 32.4).






The range of therapeutic applications is wide, encompassing many areas in which conventional pharmaceuticals treat only the symptoms of the disease state. A number of these nutraceuticals have been shown to treat the underlying cause of the illness, e.g. α-linolenic acid. As a consequence of this, many nutraceutical manufacturers and pharmaceutical companies are increasingly investigating the possibility of formulating and marketing plant based nutraceuticals.


Many of the nutraceuticals owe their activities to antioxidant activity (activity is highlighted in Tables 32.132.4), but this may not be the full story. It has been claimed that many also have other activities, including enhancement or inhibition of Phase I and II metabolizing enzymes, and modulation of DNA repair.


In addition to the increasing number of clinical trials being published to support the use of plant nutraceuticals, evidence is accumulating regarding synergistic interactions, adverse effects, and quality of commercially available single and multicomponent nutraceuticals.




Carotenoids


A number of plant-derived carotenoids such as lycopene, lutein and zeaxanthin are currently commercially available as single entities and have wide-ranging activities; their structures are shown in Fig. 32.1. Lycopene is present in red fruits and vegetables, particularly tomatoes, and lutein is present in spinach, peas and watercress. Foods that are yellow—maize, orange juice, honeydew melon and orange pepper—are also good sources of lutein.



The recommended daily intake of lycopene is 35 mg, but a number of Western societies consume from 5–25 mg, with processed products accounting for at least 50% of the total intake, therefore supplementation is often advised. A wide range of lycopene levels has been reported in tomatoes (1–15 mg/100 g), and lutein has been found to occur at 0.08 mg/100 g in tomatoes and 2.38 mg/100 g in butter squash. The mixture of lutein and zeaxanthin stereoisomers have also been reported at levels of 40 mg/100 g in kale and 12 mg/100 g in spinach. Zeaxanthin also co-occurs with lutein at 0.28 mg/100 g in butter squash.



Lycopene


Lycopene has antioxidant and free-radical scavenging activity, and serum levels have been shown to be protective against myocardial infarction (MI). Many researchers believe that these mechanisms are most likely to account for its beneficial effects in cancers. Reactive oxygen species (ROS) are the main source of oxidative damage that can generate structural alterations in DNA and decrease DNA repair by damaging essential proteins, and ultimately cause cancer. A number of trials have shown levels of cancer of the oral cavity, pharynx, oesophagus and colorectum, decreased with increasing levels of lycopene intake. An association with lycopene intake is less likely in ovarian and breast cancers.


Epidemiological literature has shown that diets rich in tomatoes are associated with lower lung cancer rates. The presence of lycopene in the human lung following lycopene supplementation has been demonstrated, and it is believed that an increased intake of lycopene might provide an additional level of protection against oxidative damage. A high intake of tomato products is associated with a 35% lower risk of total prostate cancer, and a 53% lowered risk of advanced prostate cancer. A decline in protective effect of a range of tomato products have been shown to correspond to a decline in plasma lycopene levels.


Overall, preliminary evidence suggests that lycopene intake, and serum lycopene levels are associated with a reduced risk of developing cancer, most notably prostate and lung cancer.







Sterols/stanols


These both exist in all plants, and the major sources are the vegetable oils. Cholesterol absorption ranges from 35 to 70%, but sitosterol and camposterol, which are the major plant sterols, are both poorly absorbed in the intestine (0.4–4%), and the stanols even less so (0.02–0.3%). They are thought to act by inhibition of cholesterol absorption. Plant sterols and stanols are being actively used for reduction in blood cholesterol levels, and the majority of these investigations have involved sterol and stanol enrichment of the subjects’ diet, and a positive association has been found for cholesterol reduction. The effects of a plant-sterol-enriched reduced-fat spread have been monitored over 5 weeks, with patients receiving either 1.1 and 2.2 g daily of sterol and a 40% reduced-fat spread. Total cholesterol and LDL-C values were reduced by 5.2% and 6.6%, and 7.6% and 8.1%, respectively, at these two levels of supplementation. A later comparison of trials using a number of sterols and stanols in fortified diets, revealed that effective doses ranged from 1.5 to 3.0 g daily, and total cholesterol reduction was of the order of 10%, while LDL-C reductions were between 8% and 15%. The mode of action was thought to be due to interference with the solubilization of cholesterol in intestinal micelles, consequently reducing cholesterol absorption. However, other mechanisms have also been postulated. Tablets and capsules containing sterols and stanols are commercially available, but there is no evidence that these have the same beneficial effects as sterol- and stanol-enriched spreads.



Theanine


Theanine is a non-protein amino acid present in tea, and other species of the genus Camellia. It is the major amino acid in tea, and constitutes 1–2% of the dry weight of tea. Theanine has been shown to possess three potentially useful properties: namely, relaxant, hypotensive activity and memory enhancement.


Oral supplementation with 50–200 mg theanine once weekly, has been reported to increase production of α-brain waves, which causes a state of relaxed alertness. In addition, theanine shows the ability to modulate moods, which is possibly linked to its effects on serotonin, dopamine and other neurotransmitters.


It has been postulated that the reduction in blood pressure may be responsible for mental calming. A reduction in serotonin, and also dopamine, may have an effect on memory and learning ability. It has been reported that doses of theanine up to 2000 mg/kg produced significant reduction in blood pressure in spontaneously hypertensive rats.


Theanine is increasingly being incorporated into a range of convenience foods, as well as pharmaceutical formulations. Confectionary containing 72 mg has been reported to cause relaxation, as indicated by increased generation of α-waves. Whole tea obviously contains both theanine and the catechins (see later), therefore is responsible for a range of activities, often not assigned to specific components.


Long-term social tea drinking appears to have no side effects apart from the effects of the caffeine content, therefore it may be assumed that realistic levels of theanine consumption comparable to those obtained from tea drinking should be safe. The structures of a number of single component nutraceuticals are shown in Fig. 32.2.



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Jul 18, 2016 | Posted by in PHARMACY | Comments Off on plant nutraceuticals

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