info:eu-repo/semantics/article
Synergistic Effect of Lupenone and Caryophyllene Oxide against Trypanosoma cruzi
Autor
LUIS MANUEL PEÑA RODRIGUEZ
Resumen
Chagas disease is a chronic parasitosis caused by the -agellate
protozoan Trypanosoma cruzi, which is transmitted by an
insect vector of the Reduviidae family causing cardiac injury
leading to death [1]. *e disease represents an important
public health problem in Latin America, with an estimated
10 million people infected and 25 million people under
risk of infection [2]. At present, there is no satisfactory
chemotherapy for the disease also known as American
trypanosomiasis; the drugs currently used, which include
nifurtimox, benznidazole, and allopurinol, are toxic, have
severe side e,ects, and are e,ective mainly in the acute phase,
while their activity in the chronic phase of the disease is
low and controversial [3–5]. Because of this, the WHO has
emphasized the need to develop new and better trypanocidal
drugs with none or limited side e,ects [6].
A strategy for the development of new and more e.cient
pharmaceuticals is to evaluate the synergism between two or
more products as part of a treatment of combined therapy.
O/en, the therapeutic activity of a combination of drugs is
greater than the activity of each product when administrated
separately; additionally, synergism can improve the e.ciency
of the treatment, broaden its spectrum of action, limit the
development of resistant strains, and reduce its duration
and toxicity [7, 8]. *ese arguments, supported by the
recent recommendation by the WHO that oral artemisininbased
monotherapies are withdrawn from the market and
replaced with artemisinin-based combination therapies for
the treatment of malaria [9], emphasize the importance of
considering combined therapies as an alternative for the
treatment of protozoan diseases.
We have recently carried out a study of native plants of the
Yucatan Peninsula and reported the presence of trypanocidal ´
activity in the leaf extract of Serjania yucatanensis [10]. *e
bioassay-guided puri+cation of the bioactive crude extract
resulted in the identi+cation of a 1:1 mixture of terpenoids,
lupenone (a triterpene) and caryophyllene oxide (an oxygenated
sesquiterpene), as that responsible for the originally
detected trypanocidal activity; the mixture also proved to
2 Evidence-Based Complementary and Alternative Medicine
inhibit the egress of trypomastigotes from infected Vero cells
without being cytotoxic [11]. We wish to report herein on the
synergism of a 1: 4 mixture of lupenone and caryophyllene
oxide when tested in vitro fo