Planta Med 2022; 88(15): 1479
DOI: 10.1055/s-0042-1759111
Poster Session I

Clinical validation of the utility of triterpene saponins from Sapindus saponaria and chroman hydrazone for topical treatment of cutaneous leishmaniasis

SM Robledo∗
1   PECET, Facultad de Medicina, Medellín, Colombia
,
S P Piragauta
1   PECET, Facultad de Medicina, Medellín, Colombia
,
J L Higuita-Castro
1   PECET, Facultad de Medicina, Medellín, Colombia
,
N Arbeláez
3   Corporación de Innovación desarrollo de Productos CIDEPRO, Medellín, Colombia
,
A M Restrepo
3   Corporación de Innovación desarrollo de Productos CIDEPRO, Medellín, Colombia
,
R Archbold
2   Química Orgánica de Productos Naturales, Instituto de Química, Medellín, Colombia
,
W Quiñones
2   Química Orgánica de Productos Naturales, Instituto de Química, Medellín, Colombia
,
F Torres
2   Química Orgánica de Productos Naturales, Instituto de Química, Medellín, Colombia
,
G Escobar
2   Química Orgánica de Productos Naturales, Instituto de Química, Medellín, Colombia
,
I D Vélez
1   PECET, Facultad de Medicina, Medellín, Colombia
,
A Montoya
3   Corporación de Innovación desarrollo de Productos CIDEPRO, Medellín, Colombia
,
F Echeverri
2   Química Orgánica de Productos Naturales, Instituto de Química, Medellín, Colombia
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Cutaneous leishmaniasis (CL) is an endemic infection in several countries worldwide. Because of variable response to therapy and frequency of relapses, more effective, safer, and inexpensive treatments are needed. The hederagenin glucoside saponins (SS) and chromane hydrazone (TC2) combined in a 1 : 1 ratio have high potential in antileishmanial therapy since both compounds alter the survival of Leishmania and the ability to infect adjacent macrophage [1]. In this work, we developed an ointment formulation containing 2% TC2 and 2% SS (w/w) and determined the skin permeation and the absorption but also the acute dermal toxicity by in vitro and in vivo assays. Last, the effectiveness and safety of the topical therapy to treat non-complicated CL was evaluated in an observational study in human and canine patients from endemic areas of Colombia. Both TC2 and SS diffused through pig ear skin and traces of TC2 but not SS were detected in the stratum corneum of mice at 6 – 24 hours. Neither TC2 nor SS were detected in plasma. The acute dermal toxicity was negative. Treatment with 2% TC2 – 2% SS ointment produced a complete long-term clinical cure in 10 patients (4 women and 6 men) and 56 dogs (24 females and 32 males) without adverse effects. All human and canine patients have remained disease-free for the last 24 months. In conclusion, these results support the use of topical therapy as a safer and new first-line local treatment of CL that could be further validated by controlled clinical trials.

Financing

Universidad de Antioquia (AI-51890) and Minciencias (CT-449-2021).


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  • Reference

  • 1 Upegui Zapata YA, Echeverri F, Quiñones W. et al. Mode of action of a formulation containing hydrazones and saponins against leishmania spp. Role in mitochondria, proteases and reinfection process. Int J Parasitol Drugs Drug Resist 2020; 13: 94-106
    CrossrefPubMedSearch in Google Scholar

Publication History

Article published online:
12 December 2022

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  • Reference

  • 1 Upegui Zapata YA, Echeverri F, Quiñones W. et al. Mode of action of a formulation containing hydrazones and saponins against leishmania spp. Role in mitochondria, proteases and reinfection process. Int J Parasitol Drugs Drug Resist 2020; 13: 94-106
    CrossrefPubMedSearch in Google Scholar