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Review Article
Traditional Uses, Chemical Constituents, and Biological
Activities of Bixa orellana L.: A Review
Daniela de Araújo Vilar,1Marina Suênia de Araujo Vilar,1
Túlio Flávio Accioly de Lima e Moura,2Fernanda Nervo Raffin,2Márcia Rosa de Oliveira,3
Camilo Flamarion de Oliveira Franco,4Petrônio Filgueiras de Athayde-Filho,5
Margareth de Fátima Formiga Melo Diniz,1and José Maria Barbosa-Filho1
1Laboratory of Pharmaceutical Technology, Federal University of Para´
ıba, 58051-900 Jo˜
ao Pessoa, PB, Brazil
2Department of Pharmacy, Federal University of Rio Grande do Norte, 59010-180 Natal, RN, Brazil
3Department of Molecular Biology, Federal University of Para´
ıba, 58051-900 Jo˜
ao Pessoa, PB, Brazil
4State Company of Agricultural Research of Para´
ıba, Rua Eur´
ıpedes Tavares 210, Tambi´
a, 58013-290 Jo˜
ao Pessoa, PB, Brazil
5Department of Chemistry, Federal University of Para´
ıba, 58051-900 Jo˜
ao Pessoa, PB, Brazil
Correspondence should be addressed to Jos´
e Maria Barbosa-Filho; jbarbosa@ltf.ufpb.br
Received February ; Revised May ; Accepted May ; Published June
Academic Editor: Tsutomu Hatano
Copyright © Daniela de Ara´
ujo Vilar et al. is is an open access article distributed under the Creative Commons Attribution
License, which permits unrestricted use, distribution, and reproduction in any medium,provided the original work is properly cited.
Bixa orellana L., popularly known as “urucum,” has been used by indigenous communities in Brazil and other tropical countries for
several biological applications, which indicates its potential use as an active ingredient in pharmaceutical products. e aim of this
work was to report the main evidence found in the literature, concerning the ethnopharmacology, the biological activity, and the
phytochemistry studies related to Bixa orellana L. erefore, this work comprises a systematic review about the use of Bixa orellana
in the American continent and analysis of the data collected. is study shows the well-characterized pharmacological actions that
may be considered relevant for the future development of an innovative therapeutic agent.
1. Introduction
e use of natural compounds of mineral, animal, or plant
origin in food products, cosmetics, and drugs began long ago.
ere are written records of ancient Egyptian and Chinese
civilizationsthathavemadeuseoftheseproducts.Nowadays,
there has been a return to the search for products called
“natural,” which in fact never ceased to exist. e analysis
of the composition of many drugs shows that almost %
of those in clinical use are derived from natural compounds.
Furthermore, not only plants but also plant byproducts are
widely used as preservatives and avoring and coloring agents
in various food and cosmetic preparations [].
Bixa orellana is a plant native to Brazil but grows in other
regions of South and Central America. It is grown in tropical
countries such as Peru, Mexico, Ecuador, Indonesia, India,
Kenya, and East Africa [].
e seeds of this plant produce one of the dyes most
frequently used worldwide, not only in food products but
also in the textile, paint, and cosmetic industries. Its use has
beenstimulatedduetothebanontheuseofsyntheticdyes
infoodandcosmetics,whereitisoneofthefewaccepted
by the World Health Organization (WHO), since, in addition
to being nontoxic, it does not seem to change the food value
[]. Another interesting fact is that % of all natural coloring
agents consumed worldwide are derived from annatto [].
Annattorstspreadintheformoffoodcoloring,also
known as paprika, a condiment widely used in cooking to
enhance the color of food. Today, however, its use has spread
into many segments of industrial production. us, it is now
appliedontheskin—intheformofmakeupandsunscreen—
and there is research proving that its use brings health
benets, which makes producers thankful for cultivating it
[,]. erefore, in the continuation of our research on
Hindawi Publishing Corporation
e Scientific World Journal
Volume 2014, Article ID 857292, 11 pages
http://dx.doi.org/10.1155/2014/857292
e Scientic World Journal
bioactive molecules from various species of dierent plant
families [–], we oer this compilation of the traditional
uses, chemical constituents, and biological activities of Bixa
orellana.
e aim of this review is to highlight the biological
and phytochemical studies that have been published about
Bixa orellana in South and Central America and try to
correlate these studies with the popular uses of this plant
inthoseregions,aswellastoevaluatewhetheritschemical
composition can support the reported biomedical properties
related to Bixa orellana.
2. Materials and Methods
In this work, the biological activities and compounds isolated
from Bixa orellana were searched using the database of
the Web of Science, Scielo, and the University of Illinois
in Chicago NAPRALERT (acronym for “NAturalPRoducts
ALERT”). e data were updated in April , using “Bixa
orellana, chemical, and bixin” as key words for this review. e
references found in the survey were later consulted for details
about the models or mechanisms of bioassays used to test the
extracts of Bixa orellana.
3. Botanical
e annatto tree belongs to the family Bixaceae and the
genus Bixa. Despite the existence of several species, the most
common in our country is Bixa orellana L., named aer
Francisco Orellana, who was the rst European to navigate
the Amazon [].
According to Revilla [], B. orellana is a small tree or
shrub measuring from to meters in height, sometimes
reaching a height of meters. e trunk is short, measuring
– cm in diameter, with dark gray bark with lenticels in
vertical rows. e leaves are alternate, to cm long and
to cm wide, sharp, green on both sides, and with extended
petioles.
According to Oliveira et al. [], seeds measure .–.
cm in length and .-. cm in diameter, and their shape
varies from pyramidal to almost conical. e number of seeds
per capsule varies according to the author: Alonso []found
that each bivalvar capsule may contain from to seeds,
on average.
e seeds are considered the plant part of commercial
importance, since the pericarp (layer that surrounds the
seeds) contains the pigments that have wide industrial appli-
cation. About % of this pigment is the carotenoid known as
bixin, which has the dye property and can be extracted with
vegetable oils or chemical bases. Depending on the cultivar
and climatic conditions of the region, the bixin content can
vary from to % in the seed aril. e remainder is composed
of other dyes and inert substances of minor importance [].
4. Use in Traditional Medicine
Annatto is a native plant from South America, more specif-
ically of the Amazon region. e popular name “urucum”
comes from the Tupi word “ru-ku,” which means “red.” In
Brazil, this plant is commonly known as urucum, urucu,
ac¸afr˜
ao, ac¸afroa, and ac¸afroeira-da-terra. It is known by other
popularnamesinothercountries:atol
´
e, achiote, and bija
(Peru and Cuba); axiote (Mexico); achiote, achote, anatto,
bija, and santo-domingo (Puerto Rico); bixa (Guyana); analto
(Honduras); guajachote (El Salvador); onotto and onotillo
(Venezuela); achiote and urucu (Bolivia); urucu (Argentina);
roucou (Trinidad); roucou and koessewee (Suriname); and
annatto (United States). e wide dissemination of its use
in those regions is related to the growing demand for
natural dyes by many pharmaceutical, cosmetic, textile, and
especially food industries [].
According to Cˆ
orrea [], seeds urucum supplies seeds
that have been used as a condiment as well as laxative,
cardiotonic, hypotensive, expectorant, and antibiotic. In
addition, it has anti-inammatory activity for bruises and
wounds and has been used for the treatment of bronchitis and
forwoundhealingpurposes.Oilisalsoobtainedfromthis
plant. e infusion of the leaves has been shown to be eective
against bronchitis, sore throat, and eye inammation. e
pulp,whichincludestheseed,isusedforsodrinksand
febrifuge. Moreover, it can provide valuable dyeing materials
such as yellow (orellin) and red (bixin) substances, with the
latter constituting a crystallized active ingredient.
Inthefoodindustry,itisusedtocolorbutter,margarine,
mayonnaise, sauces, mustard, sausage, soup, juice, ice cream,
bakery products, macaroni, and cheese, where it is commonly
called “do reino” (of the kingdom), coming from Holland.
It is also widely used in the printing industry and dye
manufacturing. Many Aborigines use annatto for dyeing,
where the dye is naturally obtained as a mixture and used to
color ceramics and other vases for domestic use. In addition,
most endogenous people use this dye on their skin to beautify
themselves during religious rituals and mainly to protect
themselves from ultraviolet radiation and from mosquitoes
that infest forests []. e bast provides bers for rough
cordage, and the powder resulting from grinding the seeds
has been used as an aphrodisiac. Finally, the infusion of cold
buds serves to wash inamed eyes, whereas the decoction
of the leaves has been used for antiemetic therapy during
pregnancy [](Table).
us, despite the dierent culture and traditions among
the countries in South and Central America, several of
the popular uses of Bixa orellana are the same, for exam-
ple, antipyretic, aphrodisiac, antidiarrheal, antidiabetic, and
insect repellent.
5. Chemical Compounds
Bixin, a red-colored carotenoid, is the pigment present in
high concentration in the annatto seed aril. It is the main
substance responsible for the dyeing characteristics of seeds,
where its concentration can be as high as .%. However,
dierent seeds may have levels less than .%, and because
their commercial value is based on the bixin percentage, levels
higher than .% are usually required for export [].
e Scientic World Journal
T : Traditional uses of annatto in American countries.
Country/use Plant part References
Argentina
Antipyretic/cardiotonic/antidiarrheal Seeds []
Antidiarrheal/dyes/condiment Seeds []
Brazil
Body paint Seeds []
Insect repellent Seeds []
Condiment/food coloring Seeds []
Antipyretic Seeds []
Antipyretic/laxatives/burns Seeds []
Malaria Seeds []
Colombia
Snakebite Leaves []
Aphrodisiac Seeds []
Cuba
Aphrodisiac Seeds []
Guatemala
Gonorrhea/dysentery Leaves []
Hepatitis Leaves []
Dysentery Leaves []
Blood diseases Leaves []
Gonorrhea Roots []
Diabetes Roots []
Honduras
Aromatic/food coloring Seeds []
Pain/digestive/dysentery Leaves []
Jamaica
Diabetes Seeds []
Nicaragua
Respiratory and pulmonary disorders/diarrhea/diuretic/burns Leaves + seeds []
Labor pains Seeds []
Cough/cold/diuretic/diarrhea/burns/labor pains Seeds []
Paraguay
Insecticide/repellent Seeds []
Diabetes Seeds []
Peru
Aphrodisiac/aphrodisiac/diuretic/antidisenteria/astringent Fruits []
Antipyretic/skin problems Leaves []
Alcoholic hepatitis/worms Roots []
Antipyretic/aphrodisiac/dysentery/astringent/stomach Seeds []
Trinidad and Tobago
Diuretic Leaves []
Diabetes Roots []
Diabetes Roots []
Bixin was isolated for the rst time from the seeds of Bixa
orellana in and in its complete chemical structure
and stereochemistry were determined by 1Hand13C-NMR.
Bixin belongs to the small class of natural apocarotenoids,
whose formation occurs by the oxidative degradation of C
carotenoids (Table ).
Bixin consists of a chain of carbons and has the molec-
ular formula C25H30O4(MW = .). It has a carboxylic
acid and methyl ester group at the ends of the chain. Bixin
occurs in nature as -𝑍(𝑐𝑖𝑠), but during the extraction
process it isomerizes resulting in the -𝐸form (trans), which
is called isobixin (Figure ).
e Scientic World Journal
T : e main carotenoids from the seeds of Bixa orellana.
Carotenoid Country of isolation Physical aspect References
Apo-𝜓-carotene, Z--ol Brazil Oil []
Beta carotene Brazil ∘C[]
Suriname ∗[]
Bixin
Brazil ∘C[–]
Peru ∗[]
Dominican Rep. ∗[]
Suriname ∗[]
USA ∗[]
Z-Carotene Brazil Oil []
Cryptoxanthin Suriname ∘C[]
Dimethyl-(Z)-,-diapocarotene-,-dioate Brazil Oil []
Dimethyl-(Z,Z)-,-diapocarotene-,-dioate Brazil Oil []
Phytoene Brazil Oil []
Phytouene Brazil Oil []
Geranylgeraniol Brazil Oil []
Lutein Suriname ∘C[]
Methyl-(Z)--oxo-,-diapocarotene--oate Brazil Oil []
Methyl-(Z)--oxo-,-diapocarotene--oate Brazil Oil []
Methyl-(Z)--oxo-,-diapocarotene--oate Brazil Oil []
Methyl-(Z)-apo--lycopenoate Brazil Oil []
Methyl-(Z,Z,Z)-apo--lycopenoate Brazil Oil []
Methyl-(Z)-apo--lycopenoate Brazil Oil []
Methyl-(all-E)-apo--lycopenoate Brazil Oil []
Neurosporene Brazil Oil []
Norbixin Brazil ∘C[]
Trans-bixin Jamaica ∘C[]
Zeaxanthin Suriname ∘C[]
Source: [].
Many other carotenoids (C19,C
22,C
24,C
25,C
30,andC
32)
occur in Bixa orellana but constitute a minor percentage of
the pigments. e major oily constituent of annatto seeds
is geranylgeraniol, representing % of dry seeds. Norbixin
(Figure ) is a demethylated derivative of bixin and although
it is a naturally occurring compound, it is almost always
referred to as a saponication product of bixin. is is the
form used for commercial purposes [].
Currently, more than two dozen substances have been
isolated from the seeds of Bixa orellana. Besides bixin and
norbixin, other compounds such as isobixin, beta-carotene,
cryptoxanthin, lutein, zeaxanthin, orellin, bixein, bixol, cro-
cetin, ishwarane, ellagic acid, salicylic acid, threonine, tomen-
tosic acid, tryptophan, and phenylalanine have been found in
theseedsofannatto.Inaddition,thefollowingcompounds,in
their respective concentrations, are found in these seeds:
to % cellulose, . to .% sugars, . to .% essential oils,
% xed oils, . to .% pigments, and to % proteins
and alpha and beta-carotene, as well as tannins and saponins
[,].
Mercadante et al. [,]isolatedeightapocarotenoids
from annatto seeds: methyl (Z, Z, Z)-apo--lycopenoate,
methyl (Z)-apo--lycopenoate, methyl (all-E)-apo--
lycopenoate, methyl (all-E)--apo-beta-carotene--oate,
methyl (all-E)-apo--lycopenoate, -geranylgeranyl--
methyl-,diapocaroten--dioate, -geranylgeranyl-
-methyl-(Z)-,-diapocaroten---dioate, and -
geranylgeranyl--methyl---diapocaroten---dioate.
More than volatile compounds have been detected
in aqueous and organic extracts, where of these have
alreadybeenidentied(e.g.,bornylacetate,∝-caryophyllene,
copaene, ∝-cubebene, (+)-cyclosativene, geranyl phenylac-
etate, -heptanetiol, -methylpyridine, -methylpyridine 𝛾-
elemene, 𝛽-humulene, isoledene, 𝛽-pinene, seline--en--ol,
𝛿-selinene, (−)-spathulenol, and (+)-ylangene) [].
Because annatto is a rich source of carotenoids it is
of great commercial importance. In fact, the therapeutic
properties of annatto (e.g., antioxidant and hypoglycemic)
havebeenattributedtoitshighlevelsofcarotenoids[–].
Table lists some of these compounds.
e pigments in annatto seeds can be extracted by
mechanical processes through grinding the seeds and by
physical-chemical methods using solvents or enzymes [].
e solvent extraction can be performed using three basic
methods: alkaline extraction (NaOH or KOH solutions),
which results in the conversion of bixin to norbixin;
extraction with oil (soybean, corn); and extraction using
organic solvents (hexane, chloroform, ethanol, acetone, or
e Scientic World Journal
Bixin (Z-bixin or cis-bixin)
COOH
COOMe
1
16
(a)
MeOOC 16 1
Isobixin (E-bixin or trans-bixin)
COOH
(b)
COOH
HOOC
Norbixin
(c)
OH
Geranylgeraniol
(d)
F : Chemical structure of some pigments of annatto.
propylene glycol), which results in the purest form of pig-
ments.
Barbosa-Filho et al. [] studied the seeds of four types
of annatto cultivated in Para´
ıba State, Brazil, namely, “cas-
caverde” (“green peel”), “cascavermelha” (“red bark”), “bico
de calango” (“lizard beak”), and “gr˜
aopreto”(“black grain”),
with respect to their oil (material extracted with hexane)
and solid (material extracted with chloroform) contents,
and also pure bixin, which was obtained by successive
recrystallization from the chloroform fraction. Pure bixin
appearsasred-purplecrystalswithameltingpointof–
∘C. e dierent concentrations found for the oil fraction,
chloroform extract, and bixin are as follows: red bark .%,
lizard beak .%, green peel .%, and black grain .%. Red
bark shows the highest yield for both solvent fractions, and
the bixin amount is around %. is species has been reported
as the most used in folk medicine. On the other hand, black
grain shows negligible amounts of bixin.
6. Biological Activity
Table shows data found in studies performed with
annatto in dierent countries in the American countries.
To obtain the extracts and fractions tested, several plant parts
were used, such as leaf, root, seed, shoot, and even the whole
plant. e data surveyed were classied according to the
pharmacological activity tested.
Among the twenty-one activities tested, those with the
largest number of studies performed were antifungal activity
(), antibacterial activity (), antimalarial activity (), and
mutagenic activity (). Cytotoxic activity and toxicity have
been little studied, with three and two studies, respectively.
Pharmacological activities have been evaluated in animal
models ( preclinical studies), human models ( clinical
study), cell cultures ( studies), and in vitro tests ( studies).
Antifungal activity has been investigated in one country
in Central America (Guatemala) and in two countries in
South America (Ecuador and Argentina) using eleven dier-
ent fungal strains [,,].
Freixa et al. [] conducted a study in Ecuador to assess
the antifungal activity of extracts from the dried leaves of
the annatto tree in response to fungi species, obtaining
satisfactory antifungal activity against Tri choph y ton ment a-
grophytes trains. In Guatemala, three dierent strains were
used to evaluate antifungal activity, with no satisfactory
activity being observed [].
e extracts of annatto leaves have been evaluated for
antibacterial activity against dierent bacterial strains
(Bacillus subtilis, Escherichia coli, Micrococcus luteus, Pseu-
domonas aeruginosa, Staphylococcus aureus, Salmonella typhi,
Shigella dysenteriae, and Staphylococcus epidermidis), show-
ing no activity.
Antimalarial activity has been determined against Plas-
modium gallinaceum,Plasmodium lophurae, and Plasmodium
berghei. Although the studies conducted previously in the
United States did not show signicant results [], Vald´
es et
al. () reported a moderate activity of the seed extracts of
Bixa orellana against Plasmodium berghei and falciparum.
7. Mutagenic and Cytotoxic Activities
No signicant eect was observed when extracts of annatto
seeds were tested for mutagenic activity in studies performed
in the United States and Brazil [,].
Extracts obtained from annatto seeds and leaves have
been tested in cell cultures and the brine shrimp assay,
respectively, and have been found to lack cytotoxicity in
either model used. ese experiments were carried out in
Guatemala and the Dominican Republic [,].
On the other hand, a study performed in Cuba with
medicinal plants that were active in inhibiting human lung
carcinoma cell growth showed that the ethanolic extract of
Bixa orellana presented cytotoxicity at concentrations below
𝜇g/mL [].
8. Toxicological Activities
Currently, concerns about the eect of synthetic dyes on
human health are incontestable, making people increasingly
choose those of natural origin, believing that they are devoid
of toxic eects. is is not entirely true, because even a
medication from a natural source can be a poison, depending
e Scientic World Journal
T : Biological activities of extracts of annatto in American countries.
Country
biological activity Part used Type of extract Organism tested Model tested Dose used Activity References
Argentina
Antibacterial LE EtOH Bacillus subtilis In vitro mg/mL Inactive []
Escherichia coli In vitro mg/mL Inactive []
Micrococcus luteus In vitro mg/mL Inactive []
Pseudomonas aeruginosa In vitro mg/mL Inactive []
Staphylococcus aureus In vitro mg/mL Inactive []
Antifungal LE EtOH Aspergillus niger In vitro mg/mL Inactive []
Candida albicans In vitro mg/mL Inactive []
Antiviral SE EtOH Virus Herpes simplex 1 Cell culture . mg/mL Inactive []
Insecticidal AP MeOH Insect Sitophilus oryzae % Inactive []
Brazil
Antimalarial SE CHClMouse Plasmodium berghei mg/kg Inactive []
Antioxidant SE EtOH In v itro DPPH assay . g L−Active []
Insect repellent SE Petr. eth Hamster Lutzomyia longipalpis g/L Active []
SE EtOH Mosquito Aedes aegypti . mg/mL Active []
Molluscicidal SE EtOH Conch Biomphalaria glabrata , ppm Inactive []
Mutagenic Powder Mouse B one marrow cells , ppm Inactive []
Tox icity SE Powder Rat In vivo mg/kg Inactive []
Antileishmanial LE/RO EtOH Leishmania amazonensis In vitro ,–, mg/mL Active []
Antileishmanial SE OE Leishmania amazonensis In vitro //// 𝜇g/mL Active []
Hyperlipidemia SE HOMouse In v itro and mg/kg Active []
Colombia
Snakebite LE EtOH Mouse Bothrops atrox LD > 𝜇g/animal Active []
Costa Rica
Anti-inammatory RO EtOH Rat Paw edema/carrageenan mg/kg Inactive []
Cuba
Positive inotropic eect AP HO Guinea pig Isolated atrium 𝜇LInactive[]
Antimalarial SE Plasmodium gallinaceum/falciparum In vivo/in vitro mg/kg Active []
Cytotoxic SE EtOH Tumor cells In vitro ,– mg/mL Active []
Ecuador
Antifungal LE MeOH Aspergillus niger In vitro mg/disk Inactive []
Candida albicans In vitro mg/disk Inactive []
Cryptococcus neoformans In vitro mg/disk Inactive []
Fusarium oxysporum In vitro mg/disk Inactive []
Neurospora crassa In vitro mg/disk Inactive []
Penicillium purpurogenum In vitro mg/disk Inactive []
Trichophyton mentagrophytes In vitro mg/disk Active []
e Scientic World Journal
T : C o nti nue d .
Country
biological activity Part used Type of extract Organism tested Model tested Dose used Activity References
Guatemala
Antibacterial LE Various Escherichia coli In vitro 𝜇L/disk Inactive []
Pseudomonas aeruginosa In vitro MIC > mg/mL Inactive []
Salmonella typhi In vitro MIC > mg/mL Inactive []
Shigella dysenteriae In vitro 𝜇LInactive[]
Staphylococcus aureus In vitro MIC > mg/mL Inactive []
Antifungal LE HOAspergillus avus In vitro MIC > mg/mL Inactive []
Candida albicans In vitro MIC > mg/mL Inactive []
Microsporum gypseum In vitro MIC > mg/mL Inactive []
Antigonorrheal LE EtOH Neisseria gonorrhea In vitro 𝜇L/disk Active []
Antitrypanosomal LE EtOH Trypanosoma cruzi In vitro MIC > mg/mL Inactive []
Cytotoxic LE HO Crustacean Artemia salina LC >, ppm Inactive []
Inhib. of platelet aggregation SE / In vitro rombin ag gregation IC . mg/mL Inactive []
Hawaii
Contraceptive RO / Mouse / . mL/animal Inactive []
Jamaica
Hypoglycemic SE CHClDog g Active []
HO D og mL/animal Active []
Antioxidant SE EtOH In vitro In vitro . and . 𝜇g/mL Active []
Mexico
Allergenic SE Oil Human 𝜇L/ person Active []
Paraguay
Insecticidal SE Petr. ether Insect Rhodnius neglectus 𝜇gInactive[]
Puerto Rico
Molluscicidal TP HOConchLymnaea cuben sis LD >Mppm Inactive []
Dominican Republic
Cytotoxic SE EtOH Cell culture Molt cells 𝜇g/mL Inactive []
Trinidad and Tobago
Antibacterial SE EtOAc Escherichia coli In vitro , 𝜇g/mL Inactive []
Pseudomonas aeruginosa In vitro , 𝜇g/mL Inactive []
USA
Anticonvulsant RA EtOH Mouse Seizures/electroshock mg/kg Inactive []
Rat Seizures/pentylenetetrazole mg/kg Inactive []
Antimalarial SE CHClChicken Plasmodium gallinaceum mg/kg Inactive []
Mutagenic SE MeOH Salmonella typhimurium mg/plaque Inactive []
HOIn vitro Placental trophoblasts mg/plaque Inactive []
Hypotensive RA EtOH Rat mg/kg Active []
Tox icity RA HOMouse LD> mg/kg Inactive []
LE:leaf;AP:aerialpart;TP:totalplant;RO:root;SE:seed;/:notgiven;LD:%lethaldose;IC:concentrationthatinhibits%oftheeect;MIC: minimum inhibitory concentration.
e Scientic World Journal
on the dose that is administered. e failure to require in-
depth data related to toxicological and chemical analyses
for the registration of food additives derived from natural
sources [,] certainly makes the information about
possible unwanted eects and/or pharmacological activities
resulting from their use, much rarer than expected in view of
theimportanceofthetopic.InBrazil,theuseofannattoisso
widespreadthatitssafetyisnotevenquestioned.
Paumgartten et al. [] evaluated the toxicity of annatto
extracts in rats. Doses up to mg/kg body weight/day
were introduced directly into the stomach of pregnant rats
to evaluate the eect on the mother and fetus, and no
adverse eects were found for either. e annatto extract did
not induce an increase in the incidence of visible external,
visceral, or skeletal anomalies in the fetuses. erefore, the
study suggested that the annatto extract was not toxic to rats
nor was it embryotoxic. Studies performed in Brazil by Alves
de Lima et al. [], where extracts of annatto were mixed with
the food of male rats, showed that the concentrations tested
hadnomutagenicorantimutagenicactivityintheirbone
marrow cells. A parallel toxicity study conducted by Hagiwara
et al. [] showed that .% annatto extract administered for
thirteen weeks in the feed of male and female rats did not
show any adverse eects. However, when higher doses were
administered (. and .%), the authors noticed an increase
in liver weight as well as changes in blood chemistries,
including increase in alkaline phosphatase, phospholipids,
and total protein, as well as albumin and albumin/globulin
ratio.
Hagiwara et al. [] also evaluated extracts of annatto
for liver carcinogenicity in rats and found no evidence of
liver tumors, even when given to animals at a high dose of
mg/kg body weight/day, compared to an acceptable dose
of . to . mg/kg/day, thus indicating that the danger
of a hepatocarcinogenic eect in humans may be absent or
negligible.
A toxicity test was performed with extracts obtained from
both plant seeds and shoots, and no signicant eect was
observed. e experiments were performed in the United
States using mice as the animal model and it was found that
theLDwasgreaterthanmg/kg[].
9. Correlation between the Biological
Activities, Phytochemistry, and the
Traditional Uses of Bixa orellana
Table showsthatmanyofthetraditionalusesofBixa
orellana are the same in several countries of South and
Central America, which suggests its eectiveness as a ther-
apeutic agent. Extracts of Bixa orellana showed biological
activities such as antioxidant, hypotensive, molluscicide,
and antimalarial against A cells for carcinoma of the
lung, allergy, hypoglycemic, antifungal, antioxidant, insect
repellent, antigonococcal, and antivenom serum and some of
them are in accordance with the traditional use; for example,
in Brazil it is used to extract the seeds with purpose repellent
insecticide and antimalaria and scientic studies in the same
countrywiththeLutzomyia longipalpis insect repellent action
and prove a study in Cuba proved the pharmacological action
for antimalarial activity when tested against Plasmodium
berghei. Some of them are in accordance with the traditional
use; for example, seed extracts have been used in Brazil and
Cuba as insect repellent and antimalarial. Antioxidant and
insect repellent activities can be attributed to the carotenoids
and the essential and xed oils, respectively.
Despite the previous reports about the presence of com-
ponents with anti-inammatory properties, such as salicylic
acid, lutein, polyphenols, and tannins, this activity has not yet
been proven for Bixa orellana extracts. Similarly, the plant’s
essential and xed oils have shown antibacterial properties,
although this activity has not been proven too.
In general, the data obtained in this review do not allow
correlations between the biologic activities tested in vitro or in
vivo with the compounds identied in this species. However,
taking into account the related activities such as the antipara-
sitic eect and the lack of mutagenic and cytotoxicity activity,
it is possible to consider Bixa orellana as a potential source for
the development of phytopharmaceutical products.
In conclusion, the studies discussed in this review repre-
sent a rich database around the Bixa orellana activities and
its potential uses, which evokes the feasibility of phytophar-
maceuticals to treat some diseases whenever an antioxidant,
hypotensor, or hypoglycemiant activity is necessary.
Although the commercial exploitation of this species is
well established, there are very few studies on its pharma-
cological eects. Considering the need for developing a safe
and eective product, more studies should be performed in
order to conrm other biological activities supported by the
popular uses of Bixa orellana.
Conflict of Interests
e authors declare that they have no conict of interests.
Acknowledgments
e authors are grateful to CNPq/PRONEX/FAPESQ and
CAPES for nancial support and to the NAPRALERT
Database of the University of Illinois, USA, for the literature
on Bixa orellana. A. Leyva helped in editing the English
language of the paper.
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