Compared Antileishmanial Activity of Clomiphene and Tamoxifen

• DOI: 10.20944/preprints202408.0309.v1
• Publication Date: 2024-08-14T07:55:45Z
• Authors: Sergio Sifontes-R...; Alma Reyna Escalo...; Ricardo Mondragón...; Niurka Mollineda ...; Lianet Monzote Fi...; Mónica Edith Mond...; Fedra Alardín Gut...; Lourdes Araceli L...; Daniel Andrés Sán...; Ofelia Pérez-Olvera; María Magdalena A...
• Keywords: tamoxifen; QH301-705.5; clomiphene; Biology (General); amastigote; mouse; Article; <i>Leishmania</i>; promastigote

Drug repositioning is an efficient strategy to search for new treatment alternatives that especially valuable neglected parasitic diseases such as leishmaniasis. Tamoxifen and raloxifene are selective estrogen receptor modulators (SERM) have shown antileishmanial activity. Clomiphene a SERM structurally similar tamoxifen whose potential unknown. That why the objective of present work was evaluate its activity in vitro vivo, comparison with tamoxifen. The inhibitory effect against promastigotes L. amazonensis, major mexicana evaluated both compounds; well cytotoxicity mouse peritoneal macrophages, growth intracellular amastigotes mexicana, vivo mice experimentally infected mexicana. about twice active amastigotes, IC50 values 1.7-3.3 µM clomiphene 2.9-6.4 all three species promastigotes; 2.8 ± 0.2 3.7 0.3 µM, respectively, amastigotes. affected several parasite organelles concentration-dependent fashion, leading death Interestingly, macrophage host cell did not appear damaged any concentrations tested. By oral administration at 20 mg/kg 14 days, compounds showed effects terms reducing lesions, weight lesions load end follow-up period. results drugs support further testing other this pharmacological group.