Antiprotozoal activities of Colombian plants

Weniger, Bernard; Robledo, Sara M.; Arango, Gabriel Jaime Murillo; Deharo, Eric; Aragón, Raúl; Muñoz, Verónica Francisca Loewe; Callapa, Jorgia; Lobstein, Annelise; Anton, Robert

doi:10.1016/s0378-8741(01)00346-4

Cited by 203 publications

(161 citation statements)

References 25 publications

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“…A ratio of cytotoxicity to biological activity (CC 50 /IC 50 ) was used to determine the SI of miltefosine (Table). According to Weninger et al (2001), the biological efficacy of the tested drug is not attributable to cytotoxicity when SI ≥ 10.…”

Section: Resultsmentioning

confidence: 99%

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The in vitro leishmanicidal activity of hexadecylphosphocholine (miltefosine) against four medically relevant Leishmania species of Brazil

Morais-Teixeira

Damasceno

Galuppo

et al. 2011

Mem. Inst. Oswaldo Cruz

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The in vitro leishmanicidal activity of miltefosine® (Zentaris GmbH) was assessed against four medically relevant Leishmania species of Brazil: Leishmania (Leishmania) amazonensis, Leishmania (Viannia) braziliensis, Leishmania (Viannia) guyanensis and Leishmania (Leishmania) chagasi. The activity of miltefosine against these New World species was compared to its activity against the Old World strain, Leishmania (Leishmania) donovani, which is known to be sensitive to the effects of miltefosine. The IC50 and IC90 results suggested the New World species harboured similar in vitro susceptibilities to miltefosine; however, miltefosine was approximately 20 times more active against the Old World L. (L.) donovani than against the New World L. (L.) chagasi species. The selectivity index varied from 17.2-28.9 for the New World Leishmania species and up to 420.0 for L. (L.) donovani. The differences in susceptibility to miltefosine suggest that future clinical trials with this drug should include a laboratory pre-evaluation and a dose-defining step

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Section: Resultsmentioning

confidence: 99%

“…The optical density in the absence of the drug was set as the 100% control value. The selectivity index (SI) was determined based on the equation CC 50 /inhibitory concentration (IC 50 ) as described by Weninger et al (2001).…”

Section: Methodsmentioning

confidence: 99%

The in vitro leishmanicidal activity of hexadecylphosphocholine (miltefosine) against four medically relevant Leishmania species of Brazil

Morais-Teixeira

Damasceno

Galuppo

et al. 2011

Mem. Inst. Oswaldo Cruz

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“…La viabilidad de los parásitos se midió según la formación de cristales de formazán después de agregar bromuro de 3-(4,5-dimetiltiazol-2-il)-2,5-difeniltetrazolio) (MTT) según la metodología descrita (13). La formación de los cristales se determinó en un lector de ELISA (BioRad) a una densidad óptica de 595 nm.…”

Section: Actividad Contra Epimastigotes De Trypanosoma Cruziunclassified

Actividad tripanocida y citotóxica de extractos de plantas colombianas

et al. 2011

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Introducción. El tratamiento de la enfermedad de Chagas está basado en sólo dos medicamentos de eficacia limitada y con importantes efectos colaterales. La gran biodiversidad de la flora colombiana hace de la bioprospección una alternativa potencial en la búsqueda de nuevos antiparasitarios. Objetivo. Evaluar in vitro el potencial tripanocida y la citotoxicidad de extractos obtenidos de 23 plantas colombianas. Materiales y métodos. Se obtuvieron extractos de hojas, de tallos o de la planta entera, en solventes de diferente polaridad. La actividad contra epimastigotes y la citotoxicidad se evaluaron por el micrométodo enzimático con MTT. Los extractos activos contra epimastigotes y con baja citotoxicidad se evaluaron también en tripomastigotes y amastigotes intracelulares. Resultados. Se reporta la actividad tripanocida de 13 plantas colombianas y se confirma el efecto biológico de cuatro especies previamente evaluadas. Cuatro extractos activos en epimastigotes también fueron activos en tripomastigotes y, uno de ellos, en amastigotes. Este extracto fue aislado de la planta Hieronyma antioquensis, y presentó CI 50 de 3,125, 11,48 y 2,85 μg/ml, e índices de selectividad de 25, 7 y 27, para epimastigotes, tripomastigotes y amastigotes, respectivamente. Los resultados sugieren que este extracto es un candidato promisorio para el tratamiento de la enfermedad de Chagas. Conclusión. La flora colombiana es una fuente potencial de nuevas sustancias para la quimioterapia contra la enfermedad de Chagas. El micrométodo enzimático con MTT es una herramienta útil para la tamización de la actividad biológica en epimastigotes y posterior selección para ensayos con otros estadios del parásito. Palabras clave: Trypanosoma cruzi, enfermedad de Chagas, extractos vegetales. Trypanocidal and cytotoxic activity of extracts of Colombian plantsIntroduction. The treatment of Chagas disease is based on only two drugs with limited efficacy and significant side effects. The rich biodiversity of the Colombian flora makes bio-prospecting a potential alternative in the search for new antiparasitic drugs. Objective. Potential trypanocidal activity and cytotoxicity was assessed in extracts from 23 Colombian plants. Materials and methods. Extracts of leaves, stems, or of the whole plants were obtained in solvents of a range of polarities. The activity against Trypanosoma cruzi epimastigotes and the cytotoxicity were evaluated by the MTT enzymatic micro-method. Extracts active against epimastigotes and with low cytotoxicity were also tested on trypomastigotes and intracellular amastigotes. Results. Among the extracts, biological activity was confirmed in 4 species. The extracts were active on epimastigotes and trypomastigotes; one was active also against amastigotes. The latter extract was isolated from the plant Hieronyma antioquensis and presented IC 50 of 3.1 mg/ml for epimastigotes, 11.5 mg/ml for trypomastigotes and 2.9 mg/ml for amastigotes. The selectivity indexes were 25, 7, and 27 respectively.

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“…4 Another plant extract of C. scoparioides occurring in Colombia showed leishmanicidal activity at same range of glucantime control. 5 As part of an ongoing inventory of the Amazon aromatic plants this paper reports the essential oil composition of one sample of Conobea scoparioides, as well as the antioxidant capacity and the biological activity of the plant oils and methanol extract using the DPPH radical scavenging and the brine shrimp bioassay, respectively. …”

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confidence: 99%

Antioxidant capacity and biological activity of essential oil and methanol extract of Conobea scoparioides (Cham. & Schltdl.) Benth.

Rebelo¹,

Silva²,

Andrade³

et al. 2009

J. Braz. Chem. Soc.

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Os óleos essenciais da planta sub-aquática Conobea scoparioides (fresca e previamente seca) apresentaram rendimentos de 3,4 e 3,3%, respectivamente. Os principais constituintes identificados foram o éter metílico do timol (39,6 e 47,7%), timol (40,0 e 26,4%), α-felandreno (12,1 e 14,3%) e p-cimeno (1,5 e 1,7%), totalizando mais de 90% nos referidos óleos. A concentração de seqüestro do radical DPPH (CE 50 ) dos óleos e extrato foi de 46,7 ± 3,6 µg mL -1 para a planta fresca (CsO-f), de 56,1 ± 2,4 µg mL -1 para a planta seca (CsO-d), e de 23,0 ± 2,2 µg mL -1 para o extrato metanólico (CsE-d). O valor do extrato é comparável ao BHT (19,8 ± 0,5 µg mL -1 ), usado como padrão antioxidante. O valor médio dos óleos é duas vezes menor, mas igualmente importante como agente antioxidante. O teor de Fenólicos Totais (TP, 124,6 ± 8,7 mg GAE per g) e o Trolox Equivalente (TEAC, 144,1 ± 4,9 mg TE per g) do extrato metanólico confirmaram a significativa atividade antioxidante de C. scoparioides. Da mesma forma, nos bioensaios com larva de camarão (Artemia salina) o valor médio da concentração letal dos óleos (CL 50 , 7,7 ± 0,3 µg mL -1 ) foi dez vezes maior que no extrato metanólico (CL 50 , 77,6 ± 7,1 µg mL -1 ) mostrando importante atividade biológica.The essential oils of the sub-aquatic plant Conobea scoparioides (fresh and dried previously) showed yields of 3.4 and 3.3%, respectively. The main identified constituents were thymol methyl ether (39.6 and 47.7%), thymol (40.0 and 26.4%), α-phellandrene (12.1 and 14.3%) and p-cymene (1.5 and 1.7%), totalizing more than 90% of the oils. The DPPH radical scavenging activity (EC 50 ) of the oils and extract was 46.7 ± 3.6 µg mL -1 in the fresh plant (CsO-f), 56.1 ± 2.4 µg mL -1 in the dried plant (CsO-d), and 23.0 ± 2.2 µg mL -1 in the methanol extract. The extract (CsE-d)value is comparable to BHT (19.8 ± 0.5 µg mL -1 ) used as antioxidant standard. The mean value of the oils is twice smaller but equally important as antioxidant agent. The mean amount of Total Phenolics (TP, 124.6 ± 8.7 mg GAE per g) and the Trolox Equivalent (TEAC, 144.1 ± 4.9 mg TE per g) of the methanol extract confirmed the significant antioxidant activity of C. scoparioides. Similarly, in the brine shrimp bioassay (Artemia salina) the mean value of the lethal concentration for the oils (LC 50 , 7.7 ± 0.3 µg mL -1 ) was ten times higher than the methanol extract (LC 50 , 77.6 ± 7.1 µg mL -1 ) showing important biological activity.Keywords: Conobea scoparioides, Scrophulariaceae, pataqueira, thymol and thymol methyl ether, antioxidant capacity, cytotoxicity IntroductionThe Scrophulariaceae is a cosmopolitan family comprising nearly 400 genera and 4,500 species, with their dispersion centre in the temperate regions of the north hemisphere. There are few species occurring in the Amazon. is a native erect herb called "pataqueira" or "vassourinhado-brejo", growing wild in seasonally inundated areas, with opposite leaves, sometimes alternate, deltoid, ovalate or lanceolate, with serrate or crenate margins. The who...

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Antiprotozoal activities of Colombian plants

Cited by 203 publications

References 25 publications

The in vitro leishmanicidal activity of hexadecylphosphocholine (miltefosine) against four medically relevant Leishmania species of Brazil

The in vitro leishmanicidal activity of hexadecylphosphocholine (miltefosine) against four medically relevant Leishmania species of Brazil

Actividad tripanocida y citotóxica de extractos de plantas colombianas

Antioxidant capacity and biological activity of essential oil and methanol extract of Conobea scoparioides (Cham. & Schltdl.) Benth.

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