Phylobioactive hotspots in plant resources used to treat Chagas disease.

Globally, more than six million people are infected with Trypanosoma cruzi, the causative protozoan parasite of the vector-borne Chagas disease (CD). We conducted a cross-sectional ethnopharmacological field study in Bolivia among different ethnic groups where CD is hyperendemic. A total of 775 extracts of botanical drugs used in Bolivia in the context of CD and botanical drugs from unrelated indications from the Mediterranean De Materia Medica compiled by Dioscorides two thousand years ago were profiled in a multidimensional assay uncovering different antichagasic natural product classes. Intriguingly, the phylobioactive anthraquinone hotspot matched the antichagasic activity of Senna chloroclada, the taxon with the strongest ethnomedical consensus for treating CD among the Izoceño-Guaraní. Testing common 9,10-anthracenedione derivatives in T. cruzi cellular infection assays demarcates hydroxyanthraquinone as a potential antichagasic lead scaffold. Our study systematically uncovers in vitro antichagasic phylogenetic hotspots in the plant kingdom as a potential resource for drug discovery based on ethnopharmacological hypotheses.

Cultural perception of triatomine bugs and Chagas disease in Bolivia: a cross-sectional field study.

BACKGROUND: Chagas disease remains a major public health risk in Bolivia, particularly among rural indigenous communities. Here we studied the cultural perception of the triatomine vectors and Chagas disease among selected rural and urban ethnic groups from different socio-economic and geographical milieus. We focused on the indigenous communities in the Bolivian Chaco where the disease is hyperendemic. METHODS: A cross-sectional study using field observations and structured interviews was carried out among 480 informants in five different regions of Bolivia. Additional semi-structured interviews were conducted. Statistical analyses were performed to determine the correlation of socio-economic variables and indigenous Chagas disease knowledge systems. A total of 170 domestic Triatoma infestans vectors were collected and infection with Trypanosoma cruzi was analyzed by real-time PCR. RESULTS: Triatomine bugs were associated with Chagas disease in 70.2% (n = 480) of the responses (48.0% Ayoreo, 87.5% Chiquitano, 83.9% Guaraní, 72.2% Quechua, 46.1% La Paz citizens and 67.7% Santa Cruz citizens). Generally, indigenous informants have been educated on the association between triatomine bugs and Chagas disease by institutional anti-Chagas disease campaigns. While communities were largely aware of the vectors as a principal mode of disease transmission, rather unexpectedly, health campaigns had little influence on their prevention practices, apparently due to cultural constraints. Overall, 71.9% of the collected domestic vectors in the Chaco region were infected with T. cruzi, matching the high infection rates in the indigenous communities. CONCLUSIONS: Among the Guaraní, Ayoreo and Quechua communities, the groups living in traditional houses have not integrated the scientific knowledge about Chagas disease transmission into their daily hygiene and continue to cohabit with T. infestans vectors hyperinfected with T. cruzi. An effective translation of Western disease concepts into traditional preventive measures is missing because asymptomatic infections are not generally perceived as threat by the communities. New participatory approaches involving existing ethnomedical knowledge systems could be a successful strategy in the control of T. cruzi infection.

New cycloartane-type ester triterpenes from Euphorbia pterococca and biological evaluation.

From acetonic extract of the whole plant Euphorbia pterococca Brot. (Euphorbiaceae), four new cycloartane-type ester triterpenes named cycloartenyl-2'E,4'E-decadienoate (1), cycloartenyl-2'E,4'Z-decadienoate (2), 24-methylenecycloartanyl-2'E,4'Z-tetradecadienoate (3), and 24-oxo-29-norcycloartanyl-2'E,4'Z-hexadecadienoate (4) were obtained along with nine known tetracyclic triterpenes (5-13). Their structures were established mainly by extensive use of spectroscopic techniques, including 1D (1H and 13C) and 2D homo- and heteronuclear NMR experiments (COSY, HSQC, HMBC and NOESY), and mass spectrometry (HRESIMS), and by comparison with data reported in the literature. In addition, the new compounds 1-3 have been tested for cytotoxicity, trypanocidal effects and on enzymes involved in endocannabinoid degradation. While inactive in all assays up to 100 µM, 1 showed selective inhibition of α/ß-hydrolase 12 with an IC50 of 11.6 ±â€¯1.9 µM.