Introduction
!
Psychotria L. is comprised of approximately 2000
species that are found in tropical and subtropical
rain forests [1]. The genus, which belongs to the
Rubiaceae family, is taxonomically complex.
Based on morphology and biogeography, it is di-
vided into three subgenera: Psychotria (pantropi-
cal), Tetramerae (some species from Africa and
Madagascar), and Heteropsychotria (neotropical
species) [2]. However, morphological, phyto-
chemical, and molecular similarities between
species of the subgenus Heteropsychotria and of
the genera Palicourea and Rudgea suggest that
these taxa should be placed in a new genus [3].
Studies about the chemistry of Psychotria have
helped establish new limits for the genus, which
is known for its synthesis of bioactive alkaloids.
The main metabolites found in pantropical spe-
cies of Psychotria (subgenus Psychotria) are poly-
indole alkaloids [4]. Monoterpenoid indole alka-
loids have been found in the neotropical species,
and most of these alkaloids contain a glucoside
residue that is unique compared to other mono-
terpene alkaloids (e.g., [5, 6]).
Several species of Psychotria show biological ac-
tivity by presenting different types of secondary
metabolites, especially alkaloids. Psychotria ipe-
cacuanha is a medicinal plant of the understory
of forests that is a powerful emetic and amebicide
[7]. Psychotria viridis is used in religious rituals,
where it is an ingredient in the hallucinogenic
drink called ayahuasca [8]. Some species, such as
P. beccarioides, P. forsteriana, and P. olenoides, bio-
synthesize highly cytotoxic alkaloids [9, 10]. Other
pharmacological effects have also been reported
for some species, such as the following: anti-in-
flammatory and antipyretic efficacies, and anal-
gesic activity [11, 12]; inhibition of platelet aggre-
gation [13]; antidepressant, anxiolytic, and anti-
psychotic activities [14]; antioxidant and anti-
Abstract
!
Ten Psychotria species were collected in two frag-
ments of Atlantic Forest in Rio de Janeiro: Psycho-
tria pubigera (P1A and B), P. ruelliifolia (P2), P. su-
terela (P3), P. stachyoides (P4), P. capitata (P5), P.
glaziovii (P6), P. leiocarpa (P7), P. nuda (P8), P.
racemosa (P9) and P. vellosiana (P10). Ethanol ex-
tracts of these species were evaluated for their
antimycobacterial activity, in an attempt to find
new antituberculosis agents. Psychotria pubigera
(P1A), P. ruelliifolia (P2) and P. stachyoides (P4)
were the most active against Mycobacterium. The
anti-inflammatory potential of these extracts was
also evaluated in vitro to learn if they inhibit nitric
oxide (NO) production in macrophages and if they
have free-radical scavenging properties, because
inflammation is a severe problem caused by tu-
berculosis, especially when the infection is from
M. bovis or M. tuberculosis. Psychotria suterela
(P3), P. stachyoides (P4) and P. capitata (P5) were
the most active in inhibiting macrophage NO pro-
duction but they were not the most antioxidant
species. This suggests that NO inhibitory activity
is not due to the scavenging of NO generated but
due to a specific inhibition of iNOS activity or ex-
pression. In addition, cytotoxicity was tested in
the macrophages (the host cells of the Mycobacte-
rium) and it was verified that the extracts selec-
tively killed the bacteria and not the host cells.
When analyzing antimycobacterial, cytotoxicity
and NO inhibitory activities in combination, P.
stachyoides (P4) was the most promising anti-TB
extract tested. Further, indol alkaloids were de-
tected in P. suterela and P. nuda, and 5,6-dihydro-
β-carboline alkaloids in all of the species studied,
with the highest amounts found in P. capitata and
P. racemosa.
Antimycobacterial Activity and Alkaloid
Prospection of Psychotria Species (Rubiaceae)
from the Brazilian Atlantic Rainforest
Authors Tarsila Maria da Silva Moraes
1
, Marlon Heggdorne de Araújo
2,3
, Natália R. Bernardes
2
,
Daniela B. de Oliveira
3
, Elena B. Lasunskaia
2
, Michelle Frazão Muzitano
2, 4
, Maura Da Cunha
1
Affiliations The affiliations are listed at the end of the article
Key words
l
"
Psychotria (Rubiaceae)
l
"
alkaloids
l
"
Mycobacterium bovis
l
"
anti‑inflammatory
l
"
antioxidant
l
"
tuberculosis
received August 23, 2010
revised Dec. 1, 2010
accepted Dec. 3, 2010
Bibliography
DOI http://dx.doi.org/
10.1055/s-0030-1250656
Published online January 17,
2011
Planta Med 2011; 77: 964–970
© Georg Thieme Verlag KG
Stuttgart · New York ·
ISSN 0032‑0943
Correspondence
Prof. Dr. Maura Da Cunha
Laboratório de Biologia
Celular e Tecidual
Centro de Biociências
e Biotecnologia
Universidade Estadual do Norte
Fluminense
Av. Alberto Lamego, 2000
CEP 28013-602 Campos dos
Goytacazes
Brazil
Phone: + 55 22 27 39 72 63
Fax: + 55 22 27 39 71 78
maurauenf@gmail.com
Correspondence
Prof. Dr. Michelle Frazão
Muzitano
Faculdade de Farmácia,
Campus Macaé
Universidade Federal
do Rio de Janeiro
R. Aluísio da Silva Gomes, 50
CEP 27930-560 Macaé, RJ
Brazil
Phone: + 55 22 27 96 25 39
Fax: + 55 22 27 96 25 39
mfmuzitano@yahoo.com.br
964
Moraes TMS et al. Antimycobacterial Activity and … Planta Med 2011; 77: 964–970
Original Papers