Ilex guayusa, a new opportunity from the Andean Amazonian region

The Amazonian region, a kingdom of biodiversity, has long been a precious coffer of raw materials from which to derive active principles and functional ingredients. The research relating to cosmetic raw materials, always very active in identifying novelties to develop innovative and performing products, appealing also from the marketing point of view, draws heavily on this richness of vegetables, especially plenty of antioxidants.
Many of the plant species from this area have entered common use as food and food supplements; at the same time the development of raw materials and functional ingredients for cosmetic use took place. The plant in focus is called Ilex guayusa (Guayusa, pronounced «gwhy-you-sa») and is known for its energy properties thanks to its high caffeine content (2-3% by weight): it is in fact used in many energy drinks. In addition, it contains many antioxidants, comparable to green tea. Thanks to the high content of this substances, I. guayusa could be a valuable ingredient also in the development of new cosmetic products.

Botanical aspect
This plant belongs to the Aquifoliaceae Family, Genus Ilex, Species Ilex guayusa. The tree can grow between 4 to 15 m height, with a ramified trunk up to 1 m diameter. It has dentate, oblong/elliptic, olive green and coriaceous leaves, glabrous or subglabrous at the blade as well as the back of the leaf. The leaves are positioned in a simple and alternate manner. It has an acuminate apex with an acute base. The leaves can grow between 15 – 21 cm long and 5 – 8 cm wide, with a short 1 cm petiole. Flowers have a persistent calyx and the petals forming the corolla are obtuse. The number of stamens are the same as for every petals, with oblong anthers. The ovary is sessile, subglose usually 4-6 celled (locules). The fruit is a globose green berry almost 1 cm wide. I. guayusa is a plant native to the Neotropics, with natural distribution in Colombia, Ecuador, Peru, and Bolivia. This species grows in humid tropical forests, forming part of secondary forests. In Colombia it is frequent around 2,000 masl, but is distributed in altitudes between 200 and 2,000 masl. It has been collected from Ecuador at 500 masl and Perù at 220 masl. Furthermore, in Ecuador this species distribution ranges from sea level up to 1,500 masl. This perennial tree grows in the wild but there are also plantations of its in subtropical Andean regions.

Traditional uses of Ilex guayusa
guayusa was mentioned in several researches regarding pre-Columbian civilization, old historical manuals and ethnobotanical studies, confirming the reputation of this specie as the most important plant in the daily life of Kichwa Amazonian communities and local farmer from «colono» and «mestizos» communities. Despite the wide presence of ethnobotanical studies regarding several uses in folk medicine, there are only few researches about the phytochemistry and biological activities of I. guayusa, and this lack compromises a complete understanding about the concurrence between folk medicine and pharmaceutical applications. This species is frequently used as a refreshing and tonic beverage. It is claimed to have fertility properties. In addition it is used as a stimulant, stomachic, digestive and emetic. Aids digestion and it is stated that cleanses the stomach and the intestines, since it has emetic characteristics. Likewise, it has expectorant properties, since its intake produces a warm burst throughout the body, allowing for phlegm expulsion from the lungs resulting from colds.
In 2003 a descriptive, analytical-comparative research was carried-out in the cities of Quito (Ecuador), Puyo (Ecuador), and Bogota (Colombia) finding the following uses against: sterility, diabetes, asthma, as a diuretic, during pregnancy and lactation period, as a mouth wash, against tiredness, muscular pain, weight loss, as a narcotic/shaman, aphrodisiac, purgative/emetic, and refresher. Application techniques include baths, lavage, ointment, poultice, intake or inhalation among others, every 8 to 24 h. Colombian medicinal plant Vademecum describes I. guayusa ethanol leaf extract presents central nervous system and sympathetic nervous system stimulation, possibly due to caffeine high content.
Infusion consumption stimulates the cardiac system, augments alertness, and increases the capacity to perform physical tasks. Hot tea drank at a concentration of 10 g/L three times per day is used as a treatment for diabetes. In the, Northern part of Peru it is traditionally used by the medicine man as an anti-inflammatory and antimicrobial plant.

Phytochemicals of the active ingredients
Some studies reveal I. guayusa caffeine, triterpene, and chlorogenic content. Family compound identification has been performed through preliminary phytochemical analysis identifying tannins and flavonoids in leaf aqueous and ethanol extracts, respectively. Polyphenol quantification evidenced 0.49 and 0.18 mg tannic acid per gram of sample for the aqueous and ethanol extracts, respectively. Total phenol content present in leaf methanol extract was 116.8 g of gallic acid per g of sample. Methanol total extract bio-assay guided fractionation by antioxidant and antihyperglycemic activity identified Uvaol, by GC-MS. Racidi and collaborators reported in leaf ether extract the presence of alkaloids, steroids, terpenes and lactonic or coumarin compounds. Moreover, in the aqueous extracts saponins, phenols, tannins, reducing sugars and alkaloids; and in the ethanol extract phenols, alkaloids, reducing sugars, steroids, terpenes, flavonoids and quinones. These authors described I. guayusa phytochemical knowledge is still very limited and other studies could suggest new medicinal uses for this plant. Other compounds present are methylxanthine, theobromine, theophylline, guanidine, steroids, essential oils, isobutyric acid, nicotinic acid, ascorbic acid, riboflavin, choline, pyridoxine, triterpenes, chlorogenic acid and sugars among others. Similarly, polyphenol content 40.1 mg/g), L-theanine (1.3 mg/g), theobromine (0.4 mg/g), and caffeine (32.8 mg/g) have been reported.
Standardized liquid concentrate of I. guayusa proximate analysis demonstrated 66.4% moisture content, 4.9% ash, 7.0% protein, 3.5% total sugars, 0.4% total fats and 3.8% dietary fiber. Secondary metabolite GC analysis determined the following components: caffeine (36 mg/mL), theobromine (0.3 mg/mL), chlorogenic acids (52 mg/mL), total polyphenols (10 mg/mL), catechin (2 mg/mL), isoflavones (0.8 mg/mL), epicatechin (0.18 mg/mL), epicatechin gallate (0.19 mg/mL), epigallocatechin gallate (0.09 mg/mL), epigallocathechin (1.1 mg/mL), kaempferol (trace), and naringin (trace). Antibacterial activity results demonstrate leaf aqueous and ethanol extracts have a biological activity against Staphylococcus aureus presenting 14 mm inhibition halos. Methanol, ethanol and hydroalcoholic extracts at 25 mg/mL presented antifungal activity with 16 mm halos for ethanol extract and 24 mm for the methanol extract against Candida albicans. In addition, a 32 mm halo was observed for the hydroalcoholic extract against Microsporum canis.
All phytochemical researches known until today were developed exclusively on leaves extracts, without a deepener studies on other parts of the plant. A recent review about Ilex genus reported wide information about active constituents and their biological activities, but present basic information on I. guayusa regarding the presence of caffeine. For many others Ilex species were been identified many molecules as triterpenoids, saponins, flavonoids, alkaloids, anthocyanins and other phenolic compounds which can explain the mentioned biological activities. The lack of a deepener phytochemical research about I. guayusa is undeniable and the future trend may be to increase the researches about antidiabetic and estrogenic activity.

Cosmetics application
On CosIng portal, Ilex guayusa is present as a leaf extract and classified as a skin protective. However, there are not many studies performed on cosmetic applications, but new trend for I. guayusa is to develop innovative products with added value as phytocosmetics and nutraceuticals. Thanks to the content of active ingredients with a lipolytic action (caffeine) and to the high concentration of antioxidants, the possible uses in cosmetics of the I. guayusa extract concern the treatment of cellulite and localized adiposity and indirectly the effects of aging and photoaging.
In order to optimize nutraceutical and cosmetic formulations based on I. guayusa extracts, all these findings suggest a deepener research about caffeine presence and phenolic compounds focusing different parts of the plant, different plant ages and harvest seasons.
The presence of phenolic compounds and flavonoids may indicate a protection against cellular damage induced by free radical oxidative injury or reactive oxygen species. These antioxidant properties are associated with the presence of phenolic compounds and flavonoids.
guayusa based cosmetic gel elaboration by Ecuadorian researchers established a skin protective agent in addition to having a lipolytic effect. I. guayusa in vivo anti-cellulite effect was evaluated in women between the ages of 30 and 50 years old. Their findings evidenced a reduction in body measurements and in the appearance of orange textured skin, known as cellulite, proportional to the time of treatment. This effect is likely due to the high caffeine plant content, greater than that contained in coffee or tea.
As antioxidant, has been studied the effectiveness of I. guayusa leaf extract associated with oil of Sacha Inci. The effect of the 2.5% concentration of ilex is comparable to the action of ascorbic acid. The positive results found encourage further studies for use of I. guayusa in the development of cosmetic formulations with antioxidant action.

Food supplements and cosmetics
A classic marketing strategy is to use the same ingredient for the production of food/dietary supplements and cosmetics. This allows the use of a raw material on several fronts, creating specific lines to deal with various problems with the technique of inside and outside («in&out»). Furthermore, it allows to exploit an ingredient that has already entered into common use and is therefore not unknown.
In the specific case of Ilex guayusa, combining cosmetic treatments against imperfections of cellulite to beverages or supplements aimed to work on metabolism, could be a solution to exploit a source of caffeine different from those traditionally used, such as coffee, tea and guarana.



Sustainability and fair trade opportunities
The Amazonian region, for its unique characteristics of biotic reserve and for the intrinsic value of its rain forests, represents the ideal habitat to test the economic hypotheses sustainable development: making conservation and the protection of biological and cultural diversity one attractive way to the companies that own them, providing an economic return that makes their existence more important of their destruction. It is possible to distinguish between a local function: sustainability of local communities, the use of telling the wealth present in nature decreases the «dependence», formed by the direct value of the resource; and a global function: discovery of new active ingredients, for the evolution of the food and cosmetic industry, formed by the optional value, i.e. the probability of discovering new molecules from these plants.
It’s important to implement an international partnership between the subjects of the north and the south of the world, aiming at a win-win situation.
It is also essential to respect the social and biodiversity of the peoples involved, since this diversity is considered the starting point, and to provide the cooperating parties of the «developed» countries with new knowledge and the possibility of new discoveries in the pharmaceutical field.
guayusa is a very widespread plant in the whole area of the Andean Amazon. Contrary to other plant species, whose exploitation increases the danger of deforestation and biodiversity impoverishment, the use of this shrub does not expose the territory to these risks. Indeed, an adequate fair trade policy could help and support the economy of these places. I. guayusa represents a promising bio-active compound source and an alternative income wellspring for local farmers from the Andean Amazonian Region and an interesting opportunity for the cosmetic industry always looking for new raw materials.


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by Giulia Dazzan, cosmetologist