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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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... 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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... They include the structures of isolated non-volatile compounds, as well as the chemical composition of essential oils (EOs) and in vitro tested biological activity data. However, phytochemical, pharmacological, and toxicological studies are still largely lacking for several other native and endemic plants used in the traditional medicine of Ecuador, which are mentioned in a few ethnobotanical studies [15][16][17][18][19][20][21][22]. We believe that also orphan or poorly investigated medicinal plants may become important sources of secondary biologically active metabolites and give different opportunities for their sustainable uses. ...
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Ecuador has, in proportion of its size, one of the richest floras of Latin America and the world; the country also has an immense cultural heritage due to the presence of different ethnic groups that have implemented the use of many wild and cultivated plants, mainly as medicinal remedies. In a recent publication, we have summarized the results of research activities recently carried out on about 120 plants native to Ecuador, which includes the structures of non-volatile isolated compounds, as well as the chemical composition of essential oils (EOs) and the in vitro tested biological activity data. For the sake of completeness, we have collected in this paper the main information obtained from recent ethnobotanical investigations on other important Ecuadorian medicinal plants for which phytochemical, pharmacological, and toxicological studies are, however, still largely lacking. Thus, one of the objectives of this paper is to preserve the traditional knowledge of Ecuadorian Indigenous communities which, being transmitted orally, is in danger of becoming lost. Moreover, it is our intention to stimulate more extensive studies on the rich medicinal flora of the country, which can provide economic and social benefits, especially to the people who traditionally cultivate or collect the plants.
... 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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The use of plants as therapeutic agents is part of the traditional medicine that is practiced by many indigenous communities in Ecuador. The aim of this study was to update a review published in 2016 by including the studies that were carried out in the period 2016–July 2021 on about 120 Ecuadorian medicinal plants. Relevant data on raw extracts and isolated secondary metabolites were retrieved from different databases, resulting in 104 references. They included phytochemical and pharmacological studies on several non-volatile compounds, as well as the chemical composition of essential oils (EOs). The tested biological activities are also reported. The potential of Ecuadorian plants as sources of products for practical applications in different fields, as well the perspectives of future investigations, are discussed in the last part of the review.
... 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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Guayusa (Ilex guayusa) is an endemic plant from the Amazon with potential medicinal applications. Indigenous people are familiar with such applications and use guayusa based on ancestral knowledge. There is a growing interest in guayusa-based products in urban areas of Ecuador and internationally. The supply cannot meet the demand. Currently, traditional practices are used for guayusa growth and the potential use of the protected forest is foreseen. This work describes a protocol for the in vitro propagation of guayusa, a sustainable solution to generate high quality plants in reduced space. Stakes obtained from stems were used as explants. Chemical sterilization with ethanol and sodium hypochlorite resulted in 100% surface-sterilized stakes. The growth medium mWPM resulted in favorable outcomes regarding shoot development and elongation, as well as rooting. Supplementation with activated charcoal resulted in reduced browning, only 10% of the shoots presented necrosis during the elongation phase. More than two thirds of shoots were able to develop roots spontaneously. Medium supplementation with the auxin indole-3-butyric acid, IBA, may be considered when rooting does not occur spontaneously. Acclimatization was performed in soil. The protocol was tested under different light spectra, revealing that guayusa growth is affected by light quality. The photobiology of this shade tolerant plant requires further characterization, but the data uncovered a potential role for green and far-red light in root development.
... Guayusa (Ilex guayusa Loes.) is a tropical evergreen tree belonging to the Aquifoliaceae family that grows in the amazon region of Colombia, Ecuador, Peru, and Bolivia. The folk medicine has informed that many Amazonian communities use guayusa leaves as diuretic, diaphoretic, emetic, hypnotic, narcotic, stimulant, and purgative (Radice et al. 2017). In Ecuador, guayusa leaves have been used for preparation of energy beverages, and to relief stomach pain by the Kichwa ethnicity, mestizo farmers, and rural population (Abril-Saltos et al. 2016). ...
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The use of guayusa (Ilex guayusa Loes.) leaves as functional food has increase recently. This work discusses the antioxidant activity and volatile compounds of guayusa leaves extract and fractions. The methanol crude extract was obtained by maceration, subsequently hexane, chloroform, ethyl acetate, and aqueous fractions were collected by solvent-solvent partition. Total phenolic content (TPC), total flavonol/flavone content (TFC), 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, and ferric reducing antioxidant power (FRAP) were measured by ultraviolet-visible (UV-Vis) spectrophotometry. The results revealed that ethyl acetate fraction showed highest inhibition against DPPH radical (93.86 ± 0.95%) at 500 µg/mL, and reduce the ferric-tripyridyltriazine complex (Fe3+-TPTZ) at 1619.81 mg trolox equivalent (TE)/g, followed by aqueous fraction. This bioactivity could be related to phenolic acids, flavones and flavonols content, as well as the caffeine, dodecanoic acid isopropyl ester, caffeic acid, and malic acid identified by gas chromatography-mass spectrometry (GC-MS). These findings support the antioxidant properties of this plant material.
... In our previous research (Radice et al., 2017), we summarized the traditional uses of I. guayusa tea as a stimulant, diuretic and stomach tonic. The leaf infusion has also been reported as an ethnomedical remedy against diabetes, venereal diseases, flu and body pain. ...
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The present study carried out the optimisation of the total polyphenol content (TPC) extraction assisted by ul-trasound in Ilex guayusa leaves applying response surface methodology (RSM). Also, the evaluation of the anti-oxidant activity of the extract obtained under the optimal extraction conditions was performed. The effect of the variables like, time of sonication, temperature, ethanol/water ratio and solid/liquid relationship and the interactions between them were analysed through the use of a factorial design 2^4. The significant factors were considered for the optimisation, employing a Box-Behnken Design, and the TPC as response variables. It was found that a quadratic model was adequate, with an adjusted R 2 value of 0.9367. The optimal conditions proposed , by the response surface model were: an extraction temperature of 60 C, sonication time of 29.9 min and ethanol/water ratio of 76.8/23.2. The optimised leaves extract of I. guayusa show a TPC of 3.46 (AE0.17) g gallic acid equivalents/100 g d.w. Radical scavenger activity of the obtained extract at optimum conditions, was performed through the FRAP and ABTS methods, given as result: 0.080 mmol TROLOX equivalents/100 g d.w. and 40.71 μmol TROLOX equivalents/g d.w., respectively. Due to the present findings, I. guayusa extracts can be proposed as a promising component for functional beverages, cosmetic and pharmaceutical formulation.
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La pandemia del coronavirus, generada a partir del virus SARS CoV-2, desató una crisis sanitaria a nivel mundial desde su descubrimiento en 2019. La situación en América Latina es preocupante, sobre todo para los pueblos indígenas, debido a problemas económicos, falta de acceso a recursos que garanticen prácticas higiénicas, inseguridad alimentaria, entre otros. Estos componentes, unidos al poco apoyo gubernamental, han motivado a varios pueblos indígenas a revalorizar la medicina ancestral como método de prevención y cura del COVID-19 e incluso a realizar guías de uso de las plantas medicinales. En Ecuador, varias plantas y alimentos son utilizados para prevenir y combatir el coronavirus. Situada en el centro norte del país, la provincia de Napo se caracteriza por tener condiciones biofísicas que hacen de su territorio un espacio rico en recursos naturales; a esto se suma la riqueza cultural de la nacionalidad Kichwa que la habita. Por lo tanto, esta guía tiene como objetivos recoger las experiencias y vivencias de las comunidades e identificar las plantas medicinales y recetas utilizadas en las comunidades Kichwa Atacapi, San Pablo de Ushpayacu y Amupakin, en la ciudad de Tena, Napo. Esto, como una herramienta que incrementa la resiliencia de las comunidades frente a la actual emergencia sanitaria y la posible emergencia de nuevas pandemias. Se utilizaron entrevistas semiestructuradas y enlistados libres, y se complementó con el método caminar-en-el-bosque (walk-in-the-woods), para colectar e identificar las plantas previamente mencionadas con sus nombres vernáculos en los enlistados libres. Se realizaron investigaciones bibliográficas de los aspectos morfológicos, ecológicos, agroecológicos y farmacológicos de las especies identificadas, para facilitar el reconocimiento de las especies en campo, promover su cultivo e incrementar la valorización de estas plantas. Este documento es una herramienta de información y diálogo para fomentar la valorización y conservación del conocimiento tradicional sobre las plantas medicinales utilizadas en la pandemia del COVID-19.
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p>De los 17 países megadiversos del mundo cuatro de ellos se ubican en la zona andina y concentran el 75% de la diversidad en especies de animales y plantas, estos son: Colombia, Perú, Venezuela y Ecuador (Estrella et al. 2005). La Amazonía ecuatoriana representa una de las áreas con mayor biodiversidad del planeta y por su enorme variedad de plantas se convierte en una fuente de investigación de interés permanente, especialmente para el desarrollo de nuevas materias primas del mercado farmacéutico, cosmético y alimentario. Al interés comercial se unen también el científico y el antropológico, sobre todo cuando se trata de recuperar una de las plantas sagradas de las nacionalidades indígenas que habitan en la región amazónica ecuatoriana conocida con el nombre vernáculo de guayusa (Ilex guayusa Loes.) y que es usada tradicionalmente por los Achuar y mestizos en forma de infusión. Dentro de este contexto, es fundamental aclarar que el conocimiento fitoquímico de la guayusa es limitado y la literatura científica es escasa, razón por la cual es necesaria una profunda investigación científica con el fin de evaluar su actividad biológica o farmacéutica y los posibles usos comerciales. Actualmente, los pocos datos fitoquímicos de esta planta solo revelan datos de su contenido en cafeína, así como la presencia de triterpenos y ácidos clorogénicos (Rosero Gordón 2006-2007); por lo tanto, aún no se pueden explicar todas las propiedades curativas que la tradición popular le atribuye. Así, los objetivos de esta investigación fueron: 1. Desarrollar un fitofármaco con base en Ilex guayusa Loes. que actúe como un coadyuvante en el tratamiento de manifestaciones sintomáticas como gripe, jaqueca y fiebre. 2. Identificar las familias químicas presentes en Ilex guayusa Loes. 3. Desarrollar la preparación de un extracto adecuado a la formulación final. 4. Desarrollar un método de cromatografía líquida de alta resolución (CLAR) para la dosificación de la cafeína en el producto final. 5. Establecer los parámetros de calidad del producto transformado. 6. Realizar un proceso productivo apto a las condiciones tecnológicas locales. El enfoque de la investigación se puede resumir en nueve etapas principales (Figura 1), las cuales deben ser completadas con el desarrollo de un prototipo sometido a estudios preclínicos y clínicos, pruebas industriales y finalmente, el producto desarrollado debe tener un plan de comercialización.</p
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Diabetes mellitus modifies the expression of adenosine receptors in the brain. Caffeine acts as an antagonist of A1 and A2A adenosine receptors and was shown to have a dose-dependent biphasic effect on locomotion in mice. The present study investigated the link between diabetes and locomotor activity in an animal model of streptozotocin-induced diabetes, and the effects of a low-medium dose of caffeine in this relation. The locomotor activity was investigated by using Open Field Test at 6 weeks after diabetes induction and after 2 more weeks of chronic caffeine administration. Diabetes decreased locomotor activity (total distance moved and mobility time). Chronic caffeine exposure impaired the locomotor activity in control rats, but not in diabetic rats. Our data suggested that the medium doses of caffeine might block the A2A receptors, shown to have an increased density in the brain of diabetic rats, and improve or at least maintain the locomotor activity, offering a neuroprotective support in diabetic rats. Abbreviations: STZ = streptozotocin, OFT = Open Field Test
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Background The aim of this study was to examine the influence of caffeine supplementation on knee flexor and knee extensor strength before, during and after intermittent running exercise in female team-sport players taking oral contraceptive steroids (OCS). Method Ten healthy females (24 ± 4 years; 59.7 ± 3.5 kg; undertaking 2–6 training sessions per week) taking low-dose monophasic oral contraceptives of the same hormonal composition took part in a randomised, double-blind, placebo-controlled crossover-design trial. Sixty minutes following the ingestion of a capsule containing 6 mg∙kg−1 body mass anhydrous caffeine or artificial sweetener (placebo), participants completed a 90-min intermittent treadmill-running protocol. Isometric strength performance and eccentric and concentric strength and power of the knee flexors and knee extensors (using isokinetic dynamometer), as well as countermovement jump (CMJ), was measured before, during and after the exercise protocol, as well as ~12 h post-exercise. Blood samples were taken before, during and post-exercise to measure glucose, insulin and free fatty acids (FFA). ResultsCaffeine supplementation significantly increased eccentric strength of the knee flexors (P < 0.05) and eccentric power of both the knee flexors (P < 0.05) and extensors (P < 0.05). However, there was no effect on isometric or concentric parameters, or CMJ performance. FFA was elevated with caffeine supplementation over time (P < 0.05) while levels of glucose and insulin were not affected by caffeine intake. Conclusion Caffeine supplementation increased eccentric strength and power in female team-sport players taking OCS both during an intermittent running protocol and the following morning.
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This paper seeks to contribute to the discussion on how to enhance food tourism in emerging, tropical countries characterized by a large number of indigenous groups and a high biodiversity. A sacred plant for the Kichwa indigenous communities labelled Ilex guayusa Loes. (Aquifoliceae) is used as a case study. Twelve recorded interviews with different stakeholders of the Amazon region of Napo in Ecuador were analysed. The results of this qualitative research show that the Western-based theory on niche tourism based on experiential and intimacy theory is compatible with four principles which are related to the cosmovision (worldview) of Kichwa indigenous groups, namely: mutual learning, empowerment, regulated access to intellectual property and community legislation. The framework proposed seems suitable to understand food tourism in an indigenous setting. Furthermore, the integration of Western-based food tourism with an indigenous cosmovision might contribute to a more sustainable land use and more equitable social development.
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Mera, Santa Clara and Pastaza municipalities are located in the Ecuadorian Amazon region. The objective of the study was to identify plant species used in traditional medicine by small farmers of these localities, and to classify these plants according to locality, farmer ethnicity and purposes of use. It was also investigated whether the use of medicinal plants differs between the ethnic groups. Data were collected by applying a questionnaire and personal interview with 213 farmers belonging to two ethnicities (Kichwa and mestizo), and to different municipalities (Mera, Santa Clara and Pastaza). Generated data were analyzed using contingency tables and frequency and the most representative species were determined by proportion analysis comparison. A total of 34 families and 52 species of medicinal plants were identified. The most used species was Ilex guayusa which was cited 48 times. Santa Clara municipality and Kichwa farmers used the highest number of species. These species belonged to the Lamiaceae and Solanacease family, and the plants were used for treating stomach pain, cold and inflammations. There were significant differences (Chi square test p < 0.05) between localities and ethnicities (Kichwa and mestizo). There were differences in the use of medicinal plant species among members of the Kichwa ethnicity and mestizo farmers, depending on locality, being Ilex guayusa the most used species. © 2016, Instituto Nacional de Pesquisas da Amazonia. All rights reserved.
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Cocoa-related products like chocolate have taken an important place in our food habits and culture. In this work, we aim to examine the relationship between chocolate consumption and cognitive decline in an elderly cognitively healthy population. In the present longitudinal prospective study, a cohort of 531 participants aged 65 and over with normal Mini-Mental State Examination (MMSE; median 28) was selected. The median follow-up was 48 months. Dietary habits were evaluated at baseline. The MMSE was used to assess global cognitive function at baseline and at follow-up. Cognitive decline was defined by a decrease ≥ 2 points in the MMSE score between evaluations. Relative risk (RR) and 95% confidence interval (95% CI) estimates were adjusted for age, education, smoking, alcohol drinking, body mass index, hypertension, and diabetes. Chocolate intake was associated with a lower risk of cognitive decline (RR = 0.59, 95% CI 0.38-0.92). This protective effect was observed only among subjects with an average daily consumption of caffeine lower than 75 mg (69% of the participants; RR = 0.50, 95% CI 0.31-0.82). To our knowledge, this is the first prospective cohort study to show an inverse association between regular long-term chocolate consumption and cognitive decline in humans.
The global prevalence of obesity has increased considerably in the last two decades. Obesity is caused by an imbalance between energy intake (EI) and energy expenditure (EE), and thus negative energy balance is required to bring about weight loss, which can be achieved by either decreasing EI or increasing EE. Caffeine has been found to influence the energy balance by increasing EE and decreasing EI, therefore, it can potentially be useful as a body weight regulator. Caffeine improves weight maintenance through thermogenesis, fat oxidation, and EI. The sympathetic nervous system is involved in the regulation of energy balance and lipolysis (breakdown of lipids to glycerol and free fatty acids) and the sympathetic innervation of white adipose tissue may play an important role in the regulation of total body fat. This article reviews the current knowledge on the thermogenic properties of caffeine, and its effects on appetite and EI in relation to energy balance and body weight regulation.
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Theobromine, which is a caffeine derivative, is the primary methylxanthine produced by Theobroma cacao. Theobromine works as a phosphodiesterase (PDE) inhibitor to increase intracellular cyclic adenosine monophosphate (cAMP). cAMP activates the cAMP-response element-binding protein (CREB), which is involved in a large variety of brain processes, including the induction of the brain-derived neurotrophic factor (BDNF). BDNF supports cell survival and neuronal functions, including learning and memory. Thus, cAMP/CREB/BDNF pathways play an important role in learning and memory. Here, we investigated whether orally administered theobromine could act as a PDE inhibitor centrally and affect cAMP/CREB/BDNF pathways and learning behavior in mice. The mice were divided into two groups. The control group (CN) was fed a normal diet, whereas the theobromine group (TB) was fed a diet supplemented with 0.05% theobromine for 30 days. We measured the levels of theobromine, phosphorylated vasodilator-stimulated phosphoprotein (p-VASP), phosphorylated CREB (p-CREB), and BDNF in the brain. p-VASP was used as an index of cAMP increases. Moreover, we analyzed the performance of the mice on a three-lever motor learning task. Theobromine was detectable in the brains of TB mice. The brain levels of p-VASP, p-CREB, and BDNF were higher in the TB mice compared with those in the CN mice. In addition, the TB mice performed better on the three-lever task than the CN mice did. These results strongly suggested that orally administered theobromine acted as a PDE inhibitor in the brain, and it augmented the cAMP/CREB/BDNF pathways and motor learning in mice.