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Mate BOTANY Ilex paraguariensis St. Hill. Common name, mate or yerba mate. I.paraguariensis is a dioecious shrub of the Aquifoliaceae family, which grows up to 3-8m (some species even 20m) although in cultivation, it is usually pruned several times a year, to facilitate harvest. Leaves are perennial, alternate, coriaceous, olive-green colored, about 8cm long, ovobate, with slightly crenate-toothed margins and cuneate base. Petioles about 15mm long. Flowers appear in spring. Flowers are unisexual, small, with 4 white petals, clustered in groups of 1 to 15 flowers at the axils of leaves. Ripe fruits are purple drupes with 4-5 seeds. Mate is native to South America, especially to the eastern regions of Paraguay and small areas in Uruguay, south of Brazil, the Argentinian littoral and south of Bolivia. It grows in damp lowlands, and is usually found in the medium stratum of forests. Major mate producers are Brazil (Paraná and Santa Catarina), Paraguay and Argentina (Misiones). Mate extract is produced from the leaves of Ilex paraguariensis St. Hill. CHEMISTRY Methylxanthines Major components in mate are purine alkaloids (methylxanthines), especially caffeine (0.8-1.7%) and theobromine (0.3-0.9%). The presence of theophylline has been reported in some specimens, although it is still discussed. Fig.1. Caffeine Fig.2. Theobromine V 01-02/06 48030-1 Exclusive N.A. Distributor CENTERCHEM, INC. NORWALK, CT Ph: 203-822-9800 Fax: 203-822-9820 www.centerchem.com Polyphenolic compounds Mainly chlorogenic acid (10-16%), neochlorogenic acid, isochlorogenic acid, caffeolquinic acid derivatives (3,4- and 3,5-dicaffeolquinic acids, 4,5-caffeolquinic acid), caffeic acid and catechin tannins (7-14%). Flavonoids Quercetin, quercetin-3-O-glucoside, kaempferol, rutin. Saponins About 10 triterpene-pentacyclic, non-hemolytic matesaponins. Other active principles Ursolic acid, trigonelline, essential oil (32 compounds identified, among them: aliphatic alcohols, aledhydes, ketones, terpenes, aliphatic hydrocarbons, etc.), α-amyrin, choline, 1,2-benzopyrenes, sterols, about 15 amino acids, sugars, small amounts of vitamins (especially ascorbic acid, B1, B2, nicotinic acid and β-carotene) and minerals. TRADITIONAL USES Mate is basically, a stimulant beverage that eliminates fatigue and stimulates mental and physical activity. Prepared as infusion, it is used as a vehicle for other medicinal plants. In Paraguay, infusion of mate leaves is used to loose weight. When prepared with cold water, they call it tereré, a tonic, refreshing beverage. When prepared with hot water, it is known as mate. Mate infusion is attributed diuretic and laxative effects. COSMETIC PROPERTIES Activity on the adipose tissue Xanthines and polyphenols are the most abundant chemical compounds in a group of habitually consumed plants: coffee, tea, mate and cacao. Recent research relates these compounds with an activation of thermogenesis and consequently, with possible treatments for obesity (Beltrán, I., 2003). Xanthines derive from the metabolism of plant nucleic acids. Their action mechanism basically consists in stimulating the Central Nervous System (CNS), the cardiac system, and the vascular system, by inhibiting phosphodiesterase and increasing intracellular cAMP levels (Beltrán, I., 2003). Caffeine inhibits the phosphodiesterase enzyme, thus producing cAMP accumulation and facilitating thermogenesis. However, this anti-cellulite action involves further mechanisms such as inducing calcium mobilization and increasing membrane permeability. The outcome is a powerful lipogenesis inhibition and a mild lipolytic effect, which result in the reduction of lipids accumulated into the adipocytes (Tofovic et al. 1991). The lipolytic effect of xanthine bases can be demonstrated because they increase the plasmatic levels of free fatty acids. Caffeine is mainly used on topical applications because this molecule shows high affinity for epidermal cells and penetrates skin layers easily until its action site, thus ensuring excellent diffusion in the dermis (Soler, C., 2003). Polyphenols inhibit the catechol-o-methyltransferase enzyme, which mediates adrenalin catabolization, thus increasing the concentration and prolonging the activity of noradrenalin; the outcome is an activation of the thermogenesis. Boozer, CN. et al. (2002) carried out a six-month randomized, double-blind placebo controlled trial to examine the effects of ephedrine and caffeine on a total of 177 patients. Measurements were made of: body weight, waist and hips perimeters and body fat percentage, as well as changes in blood pressure, ECG, heart rate and analytical parameters. Patients were controlled once per week, during the first V 01-02/06 48030-2 month, and every four weeks afterwards. The results revealed a noticeable reduction of body weight, fat proportion, and waist and hips perimeters for the treated group as compared to placebo. Fig. 3. Action mechanisms of caffeine and polyphenols (Beltrán, I., 2003). UCP: uncoupling protein; CAFEINA: caffeine; POLIFENOLES – polyphenols; TERMOGENESIS –thermogenesis; Inhibición – inhibition ; Catecol-ortometiltransferasa - catechol-orto-methyltransferase; Adenosina – adenosine; NORADRENALINA –noradrenaline; Fosfodiesterasa – phosphodiesterase; Activación – activation; AMPC – cAMP; AGL – FFA (free fatty acids); Fosfoproteinquinasa – phosphoproteinkinase; LIPOLISIS – lipólisis. These evidences suggest that mate extract is highly recommendable to formulate anti-cellulite cosmetic products and products aimed at the regulation of adipose tissue. Antioxidant activity A number of studies have demonstrated that mate contains flavonoids and polyphenolic compounds, which counteract the production of superoxide radicals in vitro and in vivo, in humans (Alonso, J., 2004). Filip, R. et al. (2000) evaluated the antioxidant activity of I. paraguariensis and other Ilex species, which are used as substitutes or adulterants of mate. They also studied the relationship between antioxidant activity and caffeolquinic acid derivatives content in these plants. They observed the strongest antioxidant activity for I.paraguariensis and found significant positive correlation between antioxidant activity and caffeolquinic acid derivatives concentration in the tested extracts (r= 0.94, p= 0.0005). Mate water-extract inhibited cooper-induced low-density lipoproteins oxidation, as well as ferrous sulfate/ascorbate-induced enzymatic and non-enzymatic lipid peroxidation in rats with IC50=18 µg/ml and IC50=28 µg/ml respectively (Alonso, J., 2004). Therefore, mate extract is recommendable to formulate cosmetic products for the protection of skin and hair integrity against oxidative processes. Blood-circulation stimulatory activity Mate leaves contain flavonoids. The main activity attributed to flavonoids is to act as vein-active agents, since they reduce the permeability and increase the resistance of blood capillaries (Bruneton, J., 2001). V 01-02/06 48030-3 Flavonoids are used in the treatment of blood-vessels disorders such as varices, chronic venous insufficiency (CVI), low capillary resistance, etc. Their protective effect is due to their high affinity for proline-rich proteins, such as collagen and elastin. These proteins are structural components of veins, thus their degradation weakens blood vessels, inducing edema and swelling of the lower limbs. Oral administration of flavonoids has been observed to effectively improve capillary resistance in animal models. The RELIEF study (“Reflexus asEssment and quality of life improvement with micronized flavonoids in chronic venous insufficiency”) is a controlled multi-centre study carried out between March 1997 and December 1998, in 23 countries around the world, involving more than 10,000 patients suffering CVI. These patients were treated with a purified flavonoids fraction for six months. The results of this study showed that the flavonoids treatment significantly relieved pain, tired legs, swelling, cramps and edema (when it was present) (Spignoli G., 2000). Smits, P. et al. (1987) carried out a randomized, double-blind and placebo-controlled study with 10 normotensive male subjects to analyze a possible antagonism between caffeine and adenosine with respect to their effects on human cardiovascular system. Caffeine 250 mg intravenously, increased blood pressure by 9/12 mm Hg, and resulted in a fall of the heart rate (HR) of 3 beats/min. Plasma epinephrine rose by 114% after caffeine administration. Adenosine administered at an increasing dose of 0.04-0.16 mg/kg/min, induced an increase in systolic blood pressure (SBP) (17 mm Hg), and HR (33 beats/min), a moderate fall in diastolic blood pressure (DBP) (-4 mm Hg), and no change in mean arterial pressure (MAP). At the highest adenosine infusion rate, forearm blood flow, skin temperature (ST) and transcutaneous oxygen tension were lowered, whereas plasma (nor)epinephrine was increased 227.2% and 215.9%, respectively. Adenosine infusion after caffeine induced comparable effects, but the fractional adenosine-induced changes of SBP, HR, plasma catecholamine, plasma renin activity (PRA) and aldosterone, all were significantly reduced by previous administration of caffeine. These results indicated an antagonism between caffeine and adenosine in humans, which supported the suggestion that some circulatory effects of caffeine are caused by an interaction with endogenous adenosine. Thus, mate is of great use to formulate cosmetic products with blood-circulation stimulatory action. COSMETIC APPLICATIONS Action On the adipose tissue Active Polyphenols Methylxanthines Antioxidant Flavonoids Polyphenolic compounds Blood-circulation stimulation Flavonoids Caffeine Cosmetic Application -Anti-cellulite -Anti-aging -Photo-protection -Hair color protection -Blood-circulation activation RECOMMENDED DOSE The recommended dose is between 0.5% and 5.0%. V 01-02/06 48030-4 BIBLIOGRAPHY Alonso, J. Tratado de Fitofármacos y Nutracéuticos. Barcelona: Corpus, 2004, p: 1106-1111 (633.8 ALO). Beltrán, I. Polifenoles y xantinas: su aplicación en obesidad. Actividad Dietética, 2003; 19: 10-16. Boozer, C.N., Daly, P.A., Homel, P., Solomon, J.L., Blanchard,D. Nasser,J.A., Strauss, R. and T Meredith. Herbal ephedra/caffeine for weight loss: a 6-month randomized safety and efficacy trial. Int J Obes Relat Metab Disord, 2002; 26 (5): 593-604. Bruneton J. Farmacognosia. Zaragoza: Ed. Acribia, 2001; p:317-321; 1071 (651*1 BRU). Dellacassa, E. & Bandoni, A.L.. El mate.Revista de Fitoterapia, 2001; 1 (4): 269-278 (ref. 4729). Filip, R, Lotito, S.B., Ferraro, G, Fraga, C.G. Antioxidant activity of Ilex paraguarienses and related species. Nutr Res, 2000; 20 (10): 1437-1446. Smits, P., Boekema, P., De Abreu, R, van’t Laar, A. Evidence for an antagonism between caffeine and adenosine in the human cardiovascular system. J Cardiovasc Pharmacol, 1987; 10 (2): 136-143. Soler, C.¿Qué es la celulitis? Acófar, 2003; 419:36-40. Tofovic, SP, Branch, K., Oliver, R., Magee, W, Jackson, E. Caffeine Potentiates Vasodilator-Induced Renin Release. J Pharmacol Exp Ther, 1991; 256 (3): 850-860 (ref. 187) Web sites : www.fitoterapia.net [accessed February 2006]. V 01-02/06 48030-5