Targeting Cutaneous Leishmaniasis with Thiadiazine Thione Derivatives: An In Vivo Study of Its Anti-Inflammatory, Anti-Pyretic, Anti-Nociceptive, and Anti-Sedative Properties
<b>Background/Objectives:</b> Thiadiazine thione (THTT) has gained significant interest owing to its pharmacological potentials, particularly its antiparasitic and anti-inflammatory properties. Leishmaniasis is a clinical syndrome caused by infection with <i>Leishmania</i> sp...
Saved in:
| Main Authors: | , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-01-01
|
| Series: | Biomedicines |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2227-9059/13/1/93 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1832588957440802816 |
|---|---|
| author | Sarah Sarwar Nadia Sarwar Haleema Ali Rafiullah Rasool Khan Ajaz Ahmad Amin Ullah Ho Soonmin Nazif Ullah |
| author_facet | Sarah Sarwar Nadia Sarwar Haleema Ali Rafiullah Rasool Khan Ajaz Ahmad Amin Ullah Ho Soonmin Nazif Ullah |
| author_sort | Sarah Sarwar |
| collection | DOAJ |
| description | <b>Background/Objectives:</b> Thiadiazine thione (THTT) has gained significant interest owing to its pharmacological potentials, particularly its antiparasitic and anti-inflammatory properties. Leishmaniasis is a clinical syndrome caused by infection with <i>Leishmania</i> species and is associated with an inflammatory response and nociception. The available treatments against leishmaniasis are inadequate, as they are associated with high cost, toxicity, and increased resistance. <b>Methods:</b> In the current study, the antileishmanial potential of five Thiadiazine thione derivatives (C1–C5) was evaluated in vivo against <i>Leishmania tropica</i>. Experiments were performed on BALB/c mice infected with promastigotes and treated with THTT derivatives for 15 days. Additionally, the derivatives were evaluated for their anti-inflammatory, antinociceptive, antipyretic, and antisedative properties using standardized models, including carrageenan-induced paw edema, acetic acid-induced abdominal writhes, yeast-induced fever, and white wood apparatus, respectively. <b>Results:</b> Of the tested derivatives, C5 exhibited the most promising results, with a 61.78% reduction in lesion size and significant decrease in parasite load. Among the derivatives, C1 showed the highest anti-inflammatory activity, with 63.66% inhibition in the paw edema test at the 5th hour post treatment. In the antipyretic assay, C1 and C5 were able to reduce body temperature to a normal level within 1 h of treatment. Furthermore, compounds C4, C2, and C1 showed high nociceptive activity, while C1 and C5 demonstrated the most notable antisedative effects (94 ± 2 and 92 ± 1, respectively), outperforming the standard drug diazepam (13 ± 1). <b>Conclusion:</b> These in vivo findings suggest that THTT derivatives have the potential to serve as a template for developing leishmanicidal drugs, with added anti-inflammatory and analgesic properties. |
| format | Article |
| id | doaj-art-27d4b2e274fd420cb0b39f7e6cf9e1ae |
| institution | Kabale University |
| issn | 2227-9059 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Biomedicines |
| spelling | doaj-art-27d4b2e274fd420cb0b39f7e6cf9e1ae2025-01-24T13:23:59ZengMDPI AGBiomedicines2227-90592025-01-011319310.3390/biomedicines13010093Targeting Cutaneous Leishmaniasis with Thiadiazine Thione Derivatives: An In Vivo Study of Its Anti-Inflammatory, Anti-Pyretic, Anti-Nociceptive, and Anti-Sedative PropertiesSarah Sarwar0Nadia Sarwar1Haleema Ali2Rafiullah3Rasool Khan4Ajaz Ahmad5Amin Ullah6Ho Soonmin7Nazif Ullah8Department of Biotechnology, Abdul Wali Khan University Mardan, Mardan 23200, PakistanDepartment Physiology and Medical Physics, Royal College of Surgeons, D02 YN77 Dublin, IrelandInstitute of Chemical Sciences, University of Peshawar, Peshawar 25120, PakistanPrincipal Research Officer, Veterinary Research Institute, Peshawar 25000, PakistanInstitute of Chemical Sciences, University of Peshawar, Peshawar 25120, PakistanDepartment of Clinical Pharmacy, College of Pharmacy, King Saud University, Riyad 11451, Saudi ArabiaDepartment of Allied Health Sciences, Iqra National University, Peshawar 25100, PakistanFaculty of Health and Life Sciences, INTI International University, Putra Nilai 71800, MalaysiaDepartment of Biotechnology, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan<b>Background/Objectives:</b> Thiadiazine thione (THTT) has gained significant interest owing to its pharmacological potentials, particularly its antiparasitic and anti-inflammatory properties. Leishmaniasis is a clinical syndrome caused by infection with <i>Leishmania</i> species and is associated with an inflammatory response and nociception. The available treatments against leishmaniasis are inadequate, as they are associated with high cost, toxicity, and increased resistance. <b>Methods:</b> In the current study, the antileishmanial potential of five Thiadiazine thione derivatives (C1–C5) was evaluated in vivo against <i>Leishmania tropica</i>. Experiments were performed on BALB/c mice infected with promastigotes and treated with THTT derivatives for 15 days. Additionally, the derivatives were evaluated for their anti-inflammatory, antinociceptive, antipyretic, and antisedative properties using standardized models, including carrageenan-induced paw edema, acetic acid-induced abdominal writhes, yeast-induced fever, and white wood apparatus, respectively. <b>Results:</b> Of the tested derivatives, C5 exhibited the most promising results, with a 61.78% reduction in lesion size and significant decrease in parasite load. Among the derivatives, C1 showed the highest anti-inflammatory activity, with 63.66% inhibition in the paw edema test at the 5th hour post treatment. In the antipyretic assay, C1 and C5 were able to reduce body temperature to a normal level within 1 h of treatment. Furthermore, compounds C4, C2, and C1 showed high nociceptive activity, while C1 and C5 demonstrated the most notable antisedative effects (94 ± 2 and 92 ± 1, respectively), outperforming the standard drug diazepam (13 ± 1). <b>Conclusion:</b> These in vivo findings suggest that THTT derivatives have the potential to serve as a template for developing leishmanicidal drugs, with added anti-inflammatory and analgesic properties.https://www.mdpi.com/2227-9059/13/1/93anti-inflammatorygood health<i>Leishmania tropica</i>thiadiazine thione derivativestoxicological studyin vivo activity |
| spellingShingle | Sarah Sarwar Nadia Sarwar Haleema Ali Rafiullah Rasool Khan Ajaz Ahmad Amin Ullah Ho Soonmin Nazif Ullah Targeting Cutaneous Leishmaniasis with Thiadiazine Thione Derivatives: An In Vivo Study of Its Anti-Inflammatory, Anti-Pyretic, Anti-Nociceptive, and Anti-Sedative Properties Biomedicines anti-inflammatory good health <i>Leishmania tropica</i> thiadiazine thione derivatives toxicological study in vivo activity |
| title | Targeting Cutaneous Leishmaniasis with Thiadiazine Thione Derivatives: An In Vivo Study of Its Anti-Inflammatory, Anti-Pyretic, Anti-Nociceptive, and Anti-Sedative Properties |
| title_full | Targeting Cutaneous Leishmaniasis with Thiadiazine Thione Derivatives: An In Vivo Study of Its Anti-Inflammatory, Anti-Pyretic, Anti-Nociceptive, and Anti-Sedative Properties |
| title_fullStr | Targeting Cutaneous Leishmaniasis with Thiadiazine Thione Derivatives: An In Vivo Study of Its Anti-Inflammatory, Anti-Pyretic, Anti-Nociceptive, and Anti-Sedative Properties |
| title_full_unstemmed | Targeting Cutaneous Leishmaniasis with Thiadiazine Thione Derivatives: An In Vivo Study of Its Anti-Inflammatory, Anti-Pyretic, Anti-Nociceptive, and Anti-Sedative Properties |
| title_short | Targeting Cutaneous Leishmaniasis with Thiadiazine Thione Derivatives: An In Vivo Study of Its Anti-Inflammatory, Anti-Pyretic, Anti-Nociceptive, and Anti-Sedative Properties |
| title_sort | targeting cutaneous leishmaniasis with thiadiazine thione derivatives an in vivo study of its anti inflammatory anti pyretic anti nociceptive and anti sedative properties |
| topic | anti-inflammatory good health <i>Leishmania tropica</i> thiadiazine thione derivatives toxicological study in vivo activity |
| url | https://www.mdpi.com/2227-9059/13/1/93 |
| work_keys_str_mv | AT sarahsarwar targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties AT nadiasarwar targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties AT haleemaali targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties AT rafiullah targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties AT rasoolkhan targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties AT ajazahmad targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties AT aminullah targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties AT hosoonmin targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties AT nazifullah targetingcutaneousleishmaniasiswiththiadiazinethionederivativesaninvivostudyofitsantiinflammatoryantipyreticantinociceptiveandantisedativeproperties |