PubChem BioAssays 1063: A Poorly Exploited Source of New Antileishmanial Compounds
PubChem Bioassays (AID 1063) reported the in vitro testing of 196,141 compounds against Leishmania major promastigotes. Although these results have been publicly available since 2008, limited efforts on further testing of some of these compounds has been published. The aim of the present work was se...
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| Format: | Article |
| Language: | English |
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Wiley
2025-01-01
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| Series: | Journal of Parasitology Research |
| Online Access: | http://dx.doi.org/10.1155/japr/6338486 |
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| author | Sergio Sifontes-Rodríguez Susana Meneses-Gómez Alma Reyna Escalona-Montaño Daniel Andrés Sánchez-Almaraz Ofelia Pérez-Olvera Aranza Regina Cañón Rosas Pedro Zuriel Cruz Bautista María Magdalena Aguirre-García |
| author_facet | Sergio Sifontes-Rodríguez Susana Meneses-Gómez Alma Reyna Escalona-Montaño Daniel Andrés Sánchez-Almaraz Ofelia Pérez-Olvera Aranza Regina Cañón Rosas Pedro Zuriel Cruz Bautista María Magdalena Aguirre-García |
| author_sort | Sergio Sifontes-Rodríguez |
| collection | DOAJ |
| description | PubChem Bioassays (AID 1063) reported the in vitro testing of 196,141 compounds against Leishmania major promastigotes. Although these results have been publicly available since 2008, limited efforts on further testing of some of these compounds has been published. The aim of the present work was selecting a small set of compounds that were highly active in that primary assay and assessing their antileishmanial activity in vitro and in vivo. Selected compounds were 100% active in the primary assay at 10 μM, were not theoretically toxic, did not have structural features of pan assay interfering substances, had positive druglikeness, and were not cytotoxic, and their activity rate in previous assays reported in PubChem Bioassays was under 5%. Seven commercially available compounds were purchased and tested against L. major, Leishmania mexicana, Leishmania amazonensis, and Leishmania infantum promastigotes; in mouse peritoneal macrophages (cytotoxicity); and against L. mexicana intracellular amastigotes. Eventually, four compounds with appropriate selectivity and high activity against L. mexicana amastigotes were tested by intralesional route (1%, 20 μL) in a mouse model of cutaneous leishmaniasis. Four compounds were active (IC50<10 μM) against the promastigote stage of the four Leishmania species tested. These four compounds were also active (IC50<10 μM) in vitro against intracellular amastigotes and in vivo in mice experimentally infected with L. mexicana. Results demonstrated the potential of these compounds as antileishmanials and the high, unexploited potential of AID 1063 as a source of new antileishmanial agents. |
| format | Article |
| id | doaj-art-e296ef3659374ec982750690fd300e7f |
| institution | Kabale University |
| issn | 2090-0031 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Parasitology Research |
| spelling | doaj-art-e296ef3659374ec982750690fd300e7f2025-08-20T03:30:19ZengWileyJournal of Parasitology Research2090-00312025-01-01202510.1155/japr/6338486PubChem BioAssays 1063: A Poorly Exploited Source of New Antileishmanial CompoundsSergio Sifontes-Rodríguez0Susana Meneses-Gómez1Alma Reyna Escalona-Montaño2Daniel Andrés Sánchez-Almaraz3Ofelia Pérez-Olvera4Aranza Regina Cañón Rosas5Pedro Zuriel Cruz Bautista6María Magdalena Aguirre-García7Faculty of MedicineFaculty of PharmacyFaculty of MedicineFaculty of MedicineFaculty of MedicineFaculty of MedicineFaculty of MedicineFaculty of MedicinePubChem Bioassays (AID 1063) reported the in vitro testing of 196,141 compounds against Leishmania major promastigotes. Although these results have been publicly available since 2008, limited efforts on further testing of some of these compounds has been published. The aim of the present work was selecting a small set of compounds that were highly active in that primary assay and assessing their antileishmanial activity in vitro and in vivo. Selected compounds were 100% active in the primary assay at 10 μM, were not theoretically toxic, did not have structural features of pan assay interfering substances, had positive druglikeness, and were not cytotoxic, and their activity rate in previous assays reported in PubChem Bioassays was under 5%. Seven commercially available compounds were purchased and tested against L. major, Leishmania mexicana, Leishmania amazonensis, and Leishmania infantum promastigotes; in mouse peritoneal macrophages (cytotoxicity); and against L. mexicana intracellular amastigotes. Eventually, four compounds with appropriate selectivity and high activity against L. mexicana amastigotes were tested by intralesional route (1%, 20 μL) in a mouse model of cutaneous leishmaniasis. Four compounds were active (IC50<10 μM) against the promastigote stage of the four Leishmania species tested. These four compounds were also active (IC50<10 μM) in vitro against intracellular amastigotes and in vivo in mice experimentally infected with L. mexicana. Results demonstrated the potential of these compounds as antileishmanials and the high, unexploited potential of AID 1063 as a source of new antileishmanial agents.http://dx.doi.org/10.1155/japr/6338486 |
| spellingShingle | Sergio Sifontes-Rodríguez Susana Meneses-Gómez Alma Reyna Escalona-Montaño Daniel Andrés Sánchez-Almaraz Ofelia Pérez-Olvera Aranza Regina Cañón Rosas Pedro Zuriel Cruz Bautista María Magdalena Aguirre-García PubChem BioAssays 1063: A Poorly Exploited Source of New Antileishmanial Compounds Journal of Parasitology Research |
| title | PubChem BioAssays 1063: A Poorly Exploited Source of New Antileishmanial Compounds |
| title_full | PubChem BioAssays 1063: A Poorly Exploited Source of New Antileishmanial Compounds |
| title_fullStr | PubChem BioAssays 1063: A Poorly Exploited Source of New Antileishmanial Compounds |
| title_full_unstemmed | PubChem BioAssays 1063: A Poorly Exploited Source of New Antileishmanial Compounds |
| title_short | PubChem BioAssays 1063: A Poorly Exploited Source of New Antileishmanial Compounds |
| title_sort | pubchem bioassays 1063 a poorly exploited source of new antileishmanial compounds |
| url | http://dx.doi.org/10.1155/japr/6338486 |
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