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Ilex guayusa: A systematic review of its Traditional Uses, Chemical Constituents, Biological Activities and Biotrade Opportunities

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Ilex guayusa is an emblematic tree of the Ecuadorian Amazon region, widely used in folk medicine, ritual uses and household and industrial beverages. Despite the daily consumption only a few number of studies have been carried out and the species deserves a deepener bioprospecting activity, also in order to define a new Biotrade strategy for the Ecuadorian amazon region. This review summarizes the ethno pharmacological data and the researches concerning I.guayusa. Promising biological activities have been detected, especially as new source of antioxidant agents due to the presence of phenolic compounds. Also a preliminary study as antidiabetic natural product accounts for new researches.
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Mol2Net, 2016, 2, Section M, doi: 10.3390/MOL2NET-02-M??? 1
http://sciforum.net/conference/mol2net-02
Mol2Net
Ilex guayusa: A systematic review of its Traditional Uses,
Chemical Constituents, Biological Activities and Biotrade
Opportunities
Matteo Radice 1,*, Neyfe Cossio 1 and Laura Scalvenzi1
1 Universidad Estatal Amazónica (Km 2 ½ Via Napo (paso lateral), Puyo, Pastaza, Ecuador); E-Mail:
mradice@uea.edu.ec; nsablon@uea.edu.ec; lscalvenzi@uea.edu.ec
* Corresponding author. E-mail address: mradice@uea.edu.ec. Tel: +593 032-888-118 / 032-889-118
Received: / Accepted: / Published:
Abstract:
Ilex guayusa is an emblematic tree of the Ecuadorian Amazon Region (EAR), widely used in folk
medicine, ritual uses and household and industrial beverages. Despite the daily consumption only a
few number of studies have been carried out and the species deserves a deepener bioprospecting
activity, also in order to define a new Biotrade strategy for the EAR. This review summarizes the
ethno pharmacological data and the researches concerning I. guayusa. Promising biological activities
have been detected, especially as new source of antioxidant agents due to the presence of phenolic
compounds. Also a preliminary study as antidiabetic natural product accounts for new researches
Keywords: Ilex guayusa, Ecuadorian Amazon Region, folk medicine, antioxidant, antidiabetic,
Biotrade
1. Introduction
Ilex guayusa is an emblematic tree of the
Amazonian region, widely present in the
Amazonian region of Ecuador, Colombia, Peru
and Bolivia. As reported by many authors (1 8)
I. guayusa was mentioned in several researches
regarding pre-Columbian archaeological
collections, old historical manuals and
ethnobotanical studies, legitimizing the fame of
this specie as the most important plant in the
daily life of Kichwa Amazonian communities (5)
and local farmer from “colono” and “mestizos”
communities. Despite the wide presence of
ethnobotanical studies regarding several uses in
folk medicine (6), 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. Moreover, deepener
studies may propose new promising applications
as nutraceutical or cosmetic ingredient. We
aimed to compile an up to date and
comprehensive review of I. guayusa that mainly
covers the phytochemistry and pharmacology
SciForum
Mol2Net, 2016, 2, Section M, doi: 10.3390/MOL2NET-02-M??? 2
http://sciforum.net/conference/mol2net-02
information, in order to suggest new researches
and to offer a complementary paper to the
ethnobotanical research.
2. Results and Discussion
2.1 Botanical description, historical
information and folk medicine
Ilex guayusa is an evergreen tree belonging to
Aquifoliaceae family, native to the Amazon. The
plant is dioecious and reaches between 6 to 10
meters tall. The leaves are simple, pinnate,
glabrous, oblong, elliptic with serrate margin;
they are 7-20 cm long and 2.5-7 cm wide (4). I.
guayusa is distributed from 200 to 2000 m above
sea level along the Andes and contiguous
Amazonian piedmont (8). Historical information
about I. guayusa was mentioned by Schultes (9).
Describing an archeological finding from a
shaman excavated tomb in Bolivia (Tihuanacoid
culture), the author described the presence of
dried and pressed leaves, a mortar and pestle.
The finding probably describes the use of the
species as snuff during ritual activities and it is
feasible that the species has been used for at least
1,500 years. Since the XVI century until today,
many authors described folk medicine and
commercial activities related to I. guayusa. Even
for Jesuit missionary in Ecuador the species was
an important source of income (1,3) and,
currently, a few companies from the EAR are
selling beverages and infusions obtained from I.
guayusa.
Regarding the folk medicine information, the
Table 1 summarized several traditional uses
which include ritual and magical application.
According to the “cosmovisión” concept of the
Amazonian ethnic groups, I. guayusa can be used
for multiple porpoises, from human health
remedy to the custom of cleansing the stomach
daily as a ritual purification. I. guayusa tea is
considered a “magical drink” and is also given to
the hunting dogs, before a hunting expedition, in
order to improve their abilities and skills. For
indigenous people, the infusion can also
provokes a soft hypnotic effect in which “little
dreams” can inspire or dissuade in advance a
hunting expedition (1).
2.2 Phytochemistry
Leaves contain caffeine, theobromine, phenolic
compounds and flavonoids as the main
components (10-13). Also guanidine was
mentioned as an important component of I.
guayusa leaves extracts (14,15). Another
research performed by Ruiz and Roque (16),
mentioned a phytochemical preliminary assay on
ethanolic, methanolic and hydroalcoholic
extracts of I. guayusa, the study revealed the
presence of tannins, alkaloids, flavonoids,
glycosides, phenolic compounds and quinones.
A study performed by liquid chromatography
with tandem mass spectrometry (17) of a I.
guayusa leaves extract detected several amino
acids (Table 2), which provide an interesting
information about nutraceutical profile and taste.
From the same author (18), another research on I.
guayusa leaves extracts, using gas and liquid
chromatography and mass spectrometry, revealed
the presence of two pentacyclic triterpenoid,
oleanolic (1,18 mg/g) and ursolic acid (18,22
mg/g) respectively.
2.3 Biological activity
Stimulant and protective effect of caffeine and
theobromine are extremely reported in literature
(19-23). As reported by Jara et al. (13), dried
leaves of I. guayusa were extracted with ethanol
(EtOH) and ethyl acetate (EtOAc). The total
phenolic content was determined
spectrophotometrically according to Folin
Ciocalteu’s phenol method and calculated as
gallic acid equivalent (GAE). The total
flavonoids content (TFC) was determined
spectrophotometrically, the antioxidant activity
was determined using free radical DPPH (2,2-
diphenyl-1-picrylhydryzyl) scavenging method
and the β-Carotene bleaching. Results are
reported in Table 3.
Anyway, 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.
Although guanidine was reported but wasn’t
quantified, its presence explains the preliminary
hypoglycemic effect of I. guayusa leaves extracts
in animal model. Guayusa may reduce
hyperglycemia without affect the parameter of
glucose homeostasis in non-diabetic mice (14).
Mol2Net, 2016, 2, Section M, doi: 10.3390/MOL2NET-02-M??? 3
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Oleanolic and ursolic acid are recognized as
antiviral and anti-inflammatory bioactive
compounds and also were reported the in vitro
inhibition activity of these molecules against
various cancer cell type (18). Finally, estrogenic
activity of ethanolic extracts from leaves of I.
guayusa was tested in an in vivo model (female
albino rats) shoving a remarkable increase of
serum estradiol levels and ovaries and uteri
weights. This finding is a preliminary but
promising data in order to confirm the traditional
use of I. guayusa against female infertility (24).
In another study, it was observed that methanolic
and hydroalcoholic extracts from I. guayusa have
fungicidal action against Candida albicans, the
hydroalcoholic extracts was effective also against
Microsporum canis (16).
Moreover, toxicological study was conducted on
ethanolic and water extracts using a Brine-
Shrimp assay (25), in both cases the test shown
respectively low (LC50 500–1000 μg/ml) and
median toxicity (LC50 250–499 μg/ml), in
according with safe traditional use, especially for
the aqueous extract. Another research performed
by Ames test and a chromosome aberration study
in human lymphocytes demonstrated a no
harmful effects (26).
2.4 Biotrade opportunities
In the EAR, ritual infusion, beverages and tea
bags obtained from I. guayusa leaves are widely
present in local market, restaurants and houses.
Furthermore, there are some experiences about
the development of a local and international Fair
Trade market, based on social sustainability
approaches and eco-friendly criteria. Actually, in
order to valorize the Ecuadorian Amazonian
biodiversity, the I. guayusa derivatives may be a
sustainable alternative to design natural products,
relevant for local economies, such as: tea (27),
phytopharmaceuticals (12). In order to maintain
national and international markets, it is necessary
to design a bi-commercial business strategy that
enhances the balance between conservation
politics and entrepreneurs needs.
A recent study performed by Sidali and Garrido
Pérez (8), focuses on a food tourism model,
based on guayusa case, as a strategy of
sustainable development for Kichwas
communities in Napo (Ecuador). The qualitative
research confirms as food tourism may be a
viable strategy and a future trend for EAR.
Moreover, the research identifies four principles
of Kichwa communities’ cosmovision
(worldview) which are compatible with Western-
based theory on niche tourism, respectively:
mutual learning, empowerment, regulated access
to intellectual property and community
legislation.
.
.
.
.
.
.
.
Table 1. Traditional, magical and ritual uses of Ilex guayusa.
Traditional, magical and ritual uses
Country
Ethnic group
Glycemic effect
n.r.
Amaguajes
Ritual uses
Brazil (outskirts of
Manaus)
n.r.
Diabetes, venereal diseases, improving digestion and appetite,
strengthening the body and treat pain, increase fertility, daily
purging. Promoting conviviality, stimulant, stomach tonic,
diuretic, and flu remedy. Increase fertility and libido. Can
help to avoid insect and snakebites. Guayusa helps people to
dream.
Ecuador, Colombia,
Perú
Amazonian Kichwa,
Shuar, Achuar, Cofán,
Secoya, Awajún
Mestizo and white
people
Mol2Net, 2015, 1(Section A, B, C, etc.), 1- x, type of paper, doi: xxx-xxxx 4
Daily morning drink, can help to avoid insect and snakebites,
improves hunting and fishing ability.
Ecuador
Amazonian Kichwa
Ritual uses, scatological purification, ailment, emetic,
narcotic, hypnotic, stimulant or tonic, diaphoretic and
diuretic, purgative. Increase woman fertility and helps people
to dream for knowing in advance.
Ecuador
Several Amazonian
communities
Health tonic, emetic, venereal diseases, improved the
digestion and appetite, can cure dysentery and amenorrhea.
Ecuador, Peru
Amazonian
communities
Use before and after drinking ayahuasca. Stomach trouble
aphrodisiac.
Colombia, Ecuador,
Peru
Amazonian
communities
Emetic and stimulant tea
Ecuador
n.r.
Gastritis, relaxant, helping woman fertility.
Ecuador
Saraguros, Shuar
Energizing and stomach pain.
Ecuador
Kichwa, mestizo
Additives for hallucinogenic rituals and ritual snuff.
Ecuador, Peru
Shuar
Table 2. Amino acids in Ilex guayusa extract (mg/g).
Gly
Asn
Ser
Asp
Gln
Thr
Ala
Glu
Pro
Lys
0.0100
0.2795
0.0107
0.0533
0.0502
0.0136
0.1069
0.0501
0.0253
0.0092
Val
His
Met
Arg
Tyr
Ile
Leu
Phe
Trp
Total
0.0174
0.0129
0.0052
0.0429
0.0129
0.0132
0.0125
0.0110
0.0794
0.8161
Table 3. Phenolic content, flavonoid content and antioxidant activity in Ilex guayusa extract
Sample
Total Phenolics
(GAE mg/g)
Total flavonoids
(RE mg/g)
DPPH IC50
(μg/mL)
β-carotene IC50
(μg/mL)
Guayusa EtOH
54.0±3.8
46.0±2.0
17.5±1.4
55.6±1.6
Guayusa EtOAc
36.0±2.2
20.0±1.8
52.7±4.3
85.7±3.7
3. Materials and Methods
The present systematic review was achieved
adopting the following electronic databases:
SciFinder, PubMed, Google Scholar, SciElo,
Taylor & Francis and Scopus. Data were
independently extracted from three reviewers and
the final paper selections were completed
avoiding duplication of data. The following
keywords were selected: Ilex guayusa, guayusa.
The reviewers selected articles were in English
and Spanish language and were excluded data
from patents. The above mentioned criteria
allowed selecting 20 eligible articles; we also
considered some additional key papers for
introduction, discussion and result chapters.
Anyway, it is deserved to remember that many
authors mentioned remarkable letters and
historical sources from XVI until XIX century
.
4. Conclusions
Despite the widespread presence of beverages
and commercial products obtained from I.
guayusa, mainly ethnobotanical research has
been realized in the last decades. 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 (31)
reported wide information about active
constituents and their biological activities, but
Mol2Net, 2015, 1(Section A, B, C, etc.), 1- x, type of paper, doi: xxx-xxxx 5
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 above-mentioned.
Furthermore, others studies about plants which
contain caffeine (32,33) reported the effect of
leaf age effects on the quantitative contents of
caffeine, theobromine, methylxanthines and total
phenolic compounds, essentially showing a
decrease amount of mentioned active compounds
in old leaves. Moreover was observed that
caffeine presence seems to be cultivar-specific,
tissue-specific, and season-dependent. 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. Finally, I. guayusa
represents a promising bio-active compound
source and an alternative income wellspring for
local farmers from the Ecuadorian Amazonian
Region.
Acknowledgments
The authors gratefully acknowledge the financial support of the Amazonian State University of the
Republic of Ecuador.
Conflicts of Interest
State any potential conflicts of interest here or “The authors declare no conflict of interest”.
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... Largely seen as a stimulant traditional beverage among indigenous communities, 9,16,17,22 with some medicinal uses therein (e.g., to avoid postpartum complications; as a tonic, diuretic, flu remedy, mouth wash, and insect repellent; for dysmenorrhea, diabetes, venereal diseases, and weight loss 5,24,26,[33][34][35], guayusa only recently attracted interest from the research community for its health benefits. Published research on its actions and effects remains limited. ...
... Plants in the genus Ilex are known to contain a significant number of secondary metabolites, such as xanthines, chlorogenic acid derivatives, flavonoids, and triterpenoids. 33,34,45,46 Wise and Santander (2018) provide a comprehensive summary of the composition of dried guayusa leaves, including total and free amino acids, chemical elements, nutritional values, and caffeine content. 47 Earlier research addressing the composition of guayusa focused on its high caffeine content (e.g., Lewis et al., 1991). ...
... 22 More recently, triterpenoids in guayusa leaf, specifically ursolic acid, have gained attention due to their antihyperglycemic, antibacterial, and antiparasitic effects. [33][34][35] Ursolic acid is a known activator of the G protein-coupled bile acid receptor 1 (GPBAR1), which is involved in energy homeostasis, bile acid homeostasis, glucose metabolism, inflammatory response, cancer progression, and liver regeneration, giving guayusa a potential role in the management of diabetes and metabolic syndrome. Swanston-Flatt et al. (1989,1991) 48,49 showed that guayusa had a hypoglycemic effect in normal mice and in mice with streptozotocininduced diabetes. ...
... Among the main potential beneficial effects of guayusa, it is important to highlight its stimulant and antioxidant properties. A systematic review performed by Radice et al. (2016) with an extract of dried leaves of Ilex guayusa [52] reported a reduction in hyperglycemia in animal models. Further scientific studies are needed to elucidate the potential use of this extract in nutraceutical formulations. ...
... Among the main potential beneficial effects of guayusa, it is important to highlight its stimulant and antioxidant properties. A systematic review performed by Radice et al. (2016) with an extract of dried leaves of Ilex guayusa [52] reported a reduction in hyperglycemia in animal models. Further scientific studies are needed to elucidate the potential use of this extract in nutraceutical formulations. ...
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... Other typical preparations are an infusion of guaviduca from Piper carpunya Ruiz & Pav. [11], which is a traditional drink of the Amazonian people, and the infusion of Ilex guayusa Loes., which is an emblematic tree of the Amazon Region of Ecuador that is widely used in folk medicine, ritual ceremonies, and for making industrial beverages [12,13]. ...
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... It is largely cultivated by indigenous groups and the most significant medicinal plant among the Kichwa (Innerhofer and Bernhardt 2011). Guayusa leaves have antioxidant, antibacterial, anti-parasitic, and anti-inflammatory properties (Kapp et al. 2016;Radice et al. 2017;García-Ruiz et al. 2017;Pardau et al. 2017;Gamboa et al. 2018;Gan et al. 2018;Chianese et al. 2019). They are used for many purposes, such as, boosting energy and alertness, protection against snakebites, treatment for gastritis, or inducer of female fertility. ...
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