Chemical synthesis and characterization of monothiadiazine, and its evaluation of the humoral response in BALB/c mice
Malaria is a tropical disease caused by a protozoan parasite of the genus Plasmodium, which is transmitted between humans through the bite of female Anopheles spp. mosquitoes. Nowadays, the resistance to chloroquine as an effective drug in treatment shows severe health problem. So, the project aimed...
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| Format: | bachelorThesis |
| Język: | eng |
| Wydane: |
2023
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| Hasła przedmiotowe: | |
| Dostęp online: | http://repositorio.yachaytech.edu.ec/handle/123456789/597 |
| Etykiety: |
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Dodaj etykietę | Streszczenie: | Malaria is a tropical disease caused by a protozoan parasite of the genus Plasmodium, which is transmitted between humans through the bite of female Anopheles spp. mosquitoes. Nowadays, the resistance to chloroquine as an effective drug in treatment shows severe health problem. So, the project aimed to synthesize three mono-thiadiazine derivatives (mono-THTT) where the valine (Val) is always present as N-3 or N-5 substituent: Val-Val, Leu-Val, and Val-Gly. All mono-THTTs were characterized using infrared spectroscopy (FT-IR), melting point (MP) and ultra-high-performance liquid chromatography (UHPLC). The humoral immune response of mono-THTT was evaluated in the BALB/c rodent model, using hyper-immune sera in indirect enzyme-linked immunosorbent assay (ELISA). As well, cross-reactivity using an indirect ELISA test, and the cytotoxicity of the compounds using a Promega MTT colorimetric test was assessed. The Val-Gly compound was recognized by the polyclonal antibodies of all the hyper-immune sera, previously obtained by immunized BALB/c mices. It showed that the most antigenic compound is Val-Gly; there were found significant differences between the mean of the Val-Gly hyper-immune serum and the mean of the pre-immune serum in the evaluation of all mono-THTT derivatives. However, the hyper-immune sera for Leu-Val and Val-Val compounds, did not significantly differ from the pre-immune serum in the examination of cross-reactivity, indicating that these compounds are poorly antigenic. Additionally, because the mono-THTT compounds were recognized by their own antibodies, mixing them and utilizing them as combination therapy is viable. Finally, the cytotoxicity assay showed that none of the three mono-THTT compounds are cytotoxic. |
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