{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T04:57:15Z","timestamp":1787029035213,"version":"build-2736575974"},"reference-count":44,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2018,11,30]],"date-time":"2018-11-30T00:00:00Z","timestamp":1543536000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100004586","name":"Funda\u00e7\u00e3o Carlos Chagas Filho de Amparo \u00e0 Pesquisa do Estado do Rio de Janeiro","doi-asserted-by":"publisher","award":["CNE"],"award-info":[{"award-number":["CNE"]}],"id":[{"id":"10.13039\/501100004586","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100003593","name":"Conselho Nacional de Desenvolvimento Cient\u00edfico e Tecnol\u00f3gico","doi-asserted-by":"publisher","award":["Bolsa de produtividade"],"award-info":[{"award-number":["Bolsa de produtividade"]}],"id":[{"id":"10.13039\/501100003593","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Leishmaniasis is the generic denomination to the neglected diseases caused by more than 20 species of protozoa belonging to the genus Leishmania. The toxic and parenteral-delivered pentavalent antimonials remain to be the first-line treatment. However, all the current used drugs have restrictions. The species Aureliana fasciculata (Vell.) Sendtner var. fasciculata is a native Brazilian species parsimoniously studied on a chemical point of view. In this study, the antileishmanial activity of A. fasciculata was evaluated. Among the evaluated samples of the leaves, the dichloromethane partition (AFfDi) showed the more pronounced activity, with IC50 1.85 \u00b5g\/ml against promastigotes of L. amazonensis. From AFfDi, two active withanolides were isolated, the Aurelianolides A and B, with IC50 7.61 \u03bcM and 7.94 \u03bcM, respectively. The withanolides also proved to be active against the clinically important form, the intracellular amastigote, with IC50 2.25 \u03bcM and 6.43 \u03bcM for Aurelianolides A and B, respectively. Furthermore, withanolides showed results for in silico parameters of absorption, distribution, metabolism, excretion, and toxicity (ADMET) similar to miltefosine, the reference drug, and were predicted as good oral drugs, with the advantage of not being hepatotoxic. These results suggest that these compounds can be useful as scaffolds for planning drug design.<\/jats:p>","DOI":"10.3390\/molecules23123160","type":"journal-article","created":{"date-parts":[[2018,11,30]],"date-time":"2018-11-30T12:13:17Z","timestamp":1543579997000},"page":"3160","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":17,"title":["Leishmanicidal Activity of Withanolides from Aureliana fasciculata var. fasciculata"],"prefix":"10.3390","volume":"23","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-7656-2275","authenticated-orcid":false,"given":"Simone","family":"Lima","sequence":"first","affiliation":[{"name":"Instituto de Pesquisas de Produtos Naturais (IPPN), Universidade Federal do Rio de Janeiro, Av. Carlos Chagas Filho-Cidade Universit\u00e1ria, 21941-902 Rio de Janeiro, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7504-2120","authenticated-orcid":false,"given":"Juliana","family":"Pacheco","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de Bioqu\u00edmica de Tripanosomat\u00eddeos, Instituto Oswaldo Cruz, Funda\u00e7\u00e3o Oswaldo Cruz (FIOCRUZ), 210360-040 Rio de Janeiro, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andr\u00e9","family":"Marques","sequence":"additional","affiliation":[{"name":"Departamento de Produtos Naturais, Farmanguinhos, Funda\u00e7\u00e3o Oswaldo Cruz (FIOCRUZ), 21041-250 Rio de Janeiro, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Eduardo","family":"Veltri","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de Bioqu\u00edmica de Tripanosomat\u00eddeos, Instituto Oswaldo Cruz, Funda\u00e7\u00e3o Oswaldo Cruz (FIOCRUZ), 210360-040 Rio de Janeiro, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5961-8698","authenticated-orcid":false,"given":"Rita","family":"Almeida-Lafet\u00e1","sequence":"additional","affiliation":[{"name":"Faculdade de Educa\u00e7\u00e3o Tecnol\u00f3gica do Rio de Janeiro (FAETERJ-Rio), 21351-290 Rio de Janeiro, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Maria","family":"Figueiredo","sequence":"additional","affiliation":[{"name":"Departamento de Produtos Naturais, Farmanguinhos, Funda\u00e7\u00e3o Oswaldo Cruz (FIOCRUZ), 21041-250 Rio de Janeiro, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Maria","family":"Kaplan","sequence":"additional","affiliation":[{"name":"Instituto de Pesquisas de Produtos Naturais (IPPN), Universidade Federal do Rio de Janeiro, Av. Carlos Chagas Filho-Cidade Universit\u00e1ria, 21941-902 Rio de Janeiro, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2240-4519","authenticated-orcid":false,"given":"Eduardo","family":"Torres-Santos","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de Bioqu\u00edmica de Tripanosomat\u00eddeos, Instituto Oswaldo Cruz, Funda\u00e7\u00e3o Oswaldo Cruz (FIOCRUZ), 210360-040 Rio de Janeiro, Brazil"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2018,11,30]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","unstructured":"Alvar, J., V\u00e9lez, I.D., Bern, C., Herrero, M., Desjeux, P., Cano, J., Jannin, J., den Boer, M., and WHO Leishmaniasis Control Team (2012). Leishmaniasis worldwide and global estimates of its incidence. 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