Laurequinone, a Lead Compound against <i>Leishmania</i>
Among neglected tropical diseases, leishmaniasis is one of the leading causes, not only of deaths but also of disability-adjusted life years. This disease, caused by protozoan parasites of the genus <i>Leishmania,</i> triggers different clinical manifestations, with cutaneous, mucocutane...
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| Format: | Article |
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MDPI AG
2023-05-01
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| Series: | Marine Drugs |
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| Online Access: | https://www.mdpi.com/1660-3397/21/6/333 |
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| author | Sara García-Davis Atteneri López-Arencibia Carlos J. Bethencourt-Estrella Desirée San Nicolás-Hernández Ezequiel Viveros-Valdez Ana R. Díaz-Marrero José J. Fernández Jacob Lorenzo-Morales José E. Piñero |
| author_facet | Sara García-Davis Atteneri López-Arencibia Carlos J. Bethencourt-Estrella Desirée San Nicolás-Hernández Ezequiel Viveros-Valdez Ana R. Díaz-Marrero José J. Fernández Jacob Lorenzo-Morales José E. Piñero |
| author_sort | Sara García-Davis |
| collection | DOAJ |
| description | Among neglected tropical diseases, leishmaniasis is one of the leading causes, not only of deaths but also of disability-adjusted life years. This disease, caused by protozoan parasites of the genus <i>Leishmania,</i> triggers different clinical manifestations, with cutaneous, mucocutaneous, and visceral forms. As existing treatments for this parasitosis are not sufficiently effective or safe for the patient, in this work, different sesquiterpenes isolated from the red alga <i>Laurencia johnstonii</i> have been studied for this purpose. The different compounds were tested in vitro against the promastigote and amastigote forms of <i>Leishmania amazonensis</i>. Different assays were also performed, including the measurement of mitochondrial potential, determination of ROS accumulation, and chromatin condensation, among others, focused on the detection of the cell death process known in this type of organism as apoptosis-like. Five compounds were identified that displayed leishmanicidal activity: laurequinone, laurinterol, debromolaurinterol, isolaurinterol, and aplysin, showing IC<sub>50</sub> values against promastigotes of 1.87, 34.45, 12.48, 10.09, and 54.13 µM, respectively. Laurequinone was the most potent compound tested and was shown to be more effective than the reference drug miltefosine against promastigotes. Different death mechanism studies carried out showed that laurequinone appears to induce programmed cell death or apoptosis in the parasite studied. The obtained results underline the potential of this sesquiterpene as a novel anti-kinetoplastid therapeutic agent. |
| first_indexed | 2024-03-11T02:13:40Z |
| format | Article |
| id | doaj.art-a301970f33e74ad79b2c0b4ce4cfbd77 |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-03-11T02:13:40Z |
| publishDate | 2023-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-a301970f33e74ad79b2c0b4ce4cfbd772023-11-18T11:22:27ZengMDPI AGMarine Drugs1660-33972023-05-0121633310.3390/md21060333Laurequinone, a Lead Compound against <i>Leishmania</i>Sara García-Davis0Atteneri López-Arencibia1Carlos J. Bethencourt-Estrella2Desirée San Nicolás-Hernández3Ezequiel Viveros-Valdez4Ana R. Díaz-Marrero5José J. Fernández6Jacob Lorenzo-Morales7José E. Piñero8Instituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez S/N, 38206 La Laguna, Tenerife, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez S/N, 38206 La Laguna, Tenerife, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez S/N, 38206 La Laguna, Tenerife, SpainFacultad de Ciencias Biológicas, Universidad Autónoma de Nuevo León, Avenida Pedro de Alba S/N, San Nicolás de los Garza 66450, Nuevo León, MexicoInstituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, SpainInstituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez S/N, 38206 La Laguna, Tenerife, SpainInstituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez S/N, 38206 La Laguna, Tenerife, SpainAmong neglected tropical diseases, leishmaniasis is one of the leading causes, not only of deaths but also of disability-adjusted life years. This disease, caused by protozoan parasites of the genus <i>Leishmania,</i> triggers different clinical manifestations, with cutaneous, mucocutaneous, and visceral forms. As existing treatments for this parasitosis are not sufficiently effective or safe for the patient, in this work, different sesquiterpenes isolated from the red alga <i>Laurencia johnstonii</i> have been studied for this purpose. The different compounds were tested in vitro against the promastigote and amastigote forms of <i>Leishmania amazonensis</i>. Different assays were also performed, including the measurement of mitochondrial potential, determination of ROS accumulation, and chromatin condensation, among others, focused on the detection of the cell death process known in this type of organism as apoptosis-like. Five compounds were identified that displayed leishmanicidal activity: laurequinone, laurinterol, debromolaurinterol, isolaurinterol, and aplysin, showing IC<sub>50</sub> values against promastigotes of 1.87, 34.45, 12.48, 10.09, and 54.13 µM, respectively. Laurequinone was the most potent compound tested and was shown to be more effective than the reference drug miltefosine against promastigotes. Different death mechanism studies carried out showed that laurequinone appears to induce programmed cell death or apoptosis in the parasite studied. The obtained results underline the potential of this sesquiterpene as a novel anti-kinetoplastid therapeutic agent.https://www.mdpi.com/1660-3397/21/6/333laurequinonesesquiterpene<i>Laurencia</i><i>Leishmania amazonensis</i>leishmaniasis |
| spellingShingle | Sara García-Davis Atteneri López-Arencibia Carlos J. Bethencourt-Estrella Desirée San Nicolás-Hernández Ezequiel Viveros-Valdez Ana R. Díaz-Marrero José J. Fernández Jacob Lorenzo-Morales José E. Piñero Laurequinone, a Lead Compound against <i>Leishmania</i> Marine Drugs laurequinone sesquiterpene <i>Laurencia</i> <i>Leishmania amazonensis</i> leishmaniasis |
| title | Laurequinone, a Lead Compound against <i>Leishmania</i> |
| title_full | Laurequinone, a Lead Compound against <i>Leishmania</i> |
| title_fullStr | Laurequinone, a Lead Compound against <i>Leishmania</i> |
| title_full_unstemmed | Laurequinone, a Lead Compound against <i>Leishmania</i> |
| title_short | Laurequinone, a Lead Compound against <i>Leishmania</i> |
| title_sort | laurequinone a lead compound against i leishmania i |
| topic | laurequinone sesquiterpene <i>Laurencia</i> <i>Leishmania amazonensis</i> leishmaniasis |
| url | https://www.mdpi.com/1660-3397/21/6/333 |
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