Article ; Online: The therapeutic potential of phytol towards Trypanosoma congolense infection and the inhibitory effects against trypanosomal sialidase.
2020 Volume 216, Page(s) 107943
Abstract: The search for novel therapeutic candidates against animal trypanosomiasis is an ongoing scientific endevour because of the negative impacts of the disease to the African livestock industry. In this study, the in vivo therapeutic potentials of phytol ... ...
| Abstract | The search for novel therapeutic candidates against animal trypanosomiasis is an ongoing scientific endevour because of the negative impacts of the disease to the African livestock industry. In this study, the in vivo therapeutic potentials of phytol toward Trypanosoma congolense infection and the inhibitory effects on trypanosomal sialidase were investigated. Rats were infected with T. congolense and administered daily oral treatment of 50 and 100 mg/kg BW of phytol. Within the first 10 days of the treatment, no antitrypanosomal activity was recorded but a moderate trypanostatic activity was observed from day 17-day 21 pi. However, at 100 mg/kg BW, phytol demonstrated a significant (p < 0.05) ameliorative potentials toward T. congolense-induced host-associated pathological damages such as anaemia, hepatic and renal damages; and the data was comparable to diminazine aceturate. Moreover, the T. congolense caused a significant (p < 0.05) increase in free serum sialic acid level which was significantly (p < 0.05) prevented in the presence of phytol (100 mg/kg BW). In an in vitro analysis, phytol inhibited partially purified T. congolense sialidase using an uncompetitive inhibition pattern with inhibition binding constant of 261.24 μmol/mL. Subsequently, molecular docking revealed that the compound binds to homology modelled trypanosomal sialidase with a binding free energy of -6.7 kcal/mol which was mediated via a single hydrogen bond while Trp324 and Pro274 were the critical binding residues. We concluded that phytol has moderate trypanostatic activity but with a great potential in mitigating the host-associated cellular damages while the anaemia amelioration was mediated, in part, through the inhibition of sialidase. |
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| MeSH term(s) | Animals ; Antiprotozoal Agents/pharmacology ; Antiprotozoal Agents/therapeutic use ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Livestock ; Neglected Diseases/drug therapy ; Neglected Diseases/veterinary ; Neuraminidase/antagonists & inhibitors ; Neuraminidase/chemistry ; Neuraminidase/isolation & purification ; Phytol/pharmacology ; Phytol/therapeutic use ; Random Allocation ; Rats ; Rats, Wistar ; Trypanosoma congolense/drug effects ; Trypanosoma congolense/enzymology ; Trypanosomiasis, African/drug therapy ; Trypanosomiasis, African/veterinary |
| Chemical Substances | Antiprotozoal Agents ; Enzyme Inhibitors ; Phytol (150-86-7) ; Neuraminidase (EC 3.2.1.18) |
| Language | English |
| Publishing date | 2020-06-27 |
| Publishing country | United States |
| Document type | Journal Article |
| ZDB-ID | 391089-1 |
| ISSN | 1090-2449 ; 0014-4894 |
| ISSN (online) | 1090-2449 |
| ISSN | 0014-4894 |
| DOI | 10.1016/j.exppara.2020.107943 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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