In Vitro Anti-Leishmanial Effect of Metallic Meso-Substituted Porphyrin Derivatives against <i>Leishmania braziliensis and Leishmania panamensis</i> Promastigotes Properties

• Main Authors: Fabian Espitia-Almeida, Carlos Díaz-Uribe, William Vallejo, Doris Gómez-Camargo, Arnold R. Romero Bohórquez
• Format: Article
• Language: English
• Published: MDPI AG 2020-04-01
• Series: Molecules
• Subjects: porphyrin; metalloporphyrins; photodynamic therapy; <i>Leishmania braziliensis</i>; <i>Leishmania panamensis</i>; singlet oxygen
• Online Access: https://www.mdpi.com/1420-3049/25/8/1887

In this study, a family of porphyrins based on 5,10,15,20-Tetrakis(4-ethylphenyl)porphyrin (<b>1</b>, Ph) and six metallo-derivatives (Zn²⁺(<b>2</b>, Ph-Zn), Sn⁴⁺(<b>3</b>, Ph-Sn), Mn²⁺ (<b>4</b>, Ph-Mn), Ni²⁺ (<b>5</b>, Ph-Ni), Al³⁺ (<b>6</b>, Ph-Al), and V³⁺ (<b>7</b>, Ph-V)) were tested as photosensitizers for photodynamic therapy against <i>Leishmania braziliensis</i> and <i>panamensis</i>. The singlet oxygen quantum yield value (Φ_Δ) for (<b>1</b>–<b>7</b>) was measured using 1,3-diphenylisobenzofuran (DPBF) as a singlet oxygen trapping agent and 5,10,15,20-(tetraphenyl)-porphyrin (H2TPP) as a reference standard; besides, parasite viability was estimated by the MTT assay. After metal insertion into the porphyrin core, the Φ_Δ increased from 0.76–0.90 and cell viability changed considerably. The Φ_Δ and metal type changed the cytotoxic activity. Finally, (<b>2</b>) showed both the highest Φ_Δ (0.90) and the best photodynamic activity against the parasites studied (IC₅₀ of 1.2 μM).