Acıbadem Mehmet Ali Aydınlar University Faculty of Medicine, Department of Medical Microbiology, İstanbul, Türkiye.
Acıbadem Mehmet Ali Aydınlar University Vocational School of Health Services, Medical Laboratory Technician Program, İstanbul, Türkiye.
Turkiye Parazitol Derg. 2024 Oct 7;48(3):135-141. doi: 10.4274/tpd.galenos.2024.48658.
Antimicrobial resistance is a real threat to humanity. Pentavalent antimonials are reported non-effective in leishmaniasis treatment today, in countries like India. New treatment options have been assessed worldwide lately. Antimicrobial peptides (AMP) are the leading antibiotic candidates due to their large spectrum, fast efficacy, and low resistance risks. Cathelicidins are the AMP with well-documented antimicrobial activities against bacteria, fungi, and protozoa, over their positively charged membranes. Here, we aim to design cathelicidine-like helical peptides (CLHP), and compare their anti- efficacies , with meglumine antimoniate (MA) on .
A total of five study [TN-1-5] and two control (MA and non-drug) groups were formed. Cryopreserved isolate was thawed and cultivated in Novy-MacNeal-Nicolle medium and then in RPMI. Five different CLHPs (TN1-5) were diluted in dimethyl sulphoxide. A total of 150 uL of CLHPs and MA were added into the first wells of the test plaques, followed by serial dilutions that revealed doses within 4 and 512 ug/mL. Then, 100 uL of cultures including 1x10/mL of promastigotes were added into each well. Viability of promastigotes was checked with XTT, while the parasite count was assessed at 24 and 48 hours.
TN3 was effective at 32 ug/mL. All tested CLHPs exhibited varying degrees of anti- activities, except TN5, even at its highest dose.
TN3 showed a particular efficacy against . Further studies including testing of the candidate's both efficacy and toxicity are essential.
抗菌药物耐药性对人类构成严重威胁。目前，在印度等国，五价锑剂已被报道对利什曼病无效。最近，全球评估了新的治疗选择。由于其广谱、快速疗效和低耐药风险，抗菌肽（AMP）是主要的抗生素候选物。富含半胱氨酸的抗菌肽（cathelicidins）因其带正电荷的膜而对细菌、真菌和原生动物具有良好的抗菌活性，是 AMP 中的佼佼者。在这里，我们旨在设计 cathelicidine-like helical peptides (CLHP)，并将其抗疗效与戊二醛（MA）进行比较。
共分为五组研究 [TN-1-5] 和两组对照（MA 和非药物）。冷冻保存的 株被解冻并在 Novy-MacNeal-Nicolle 培养基中培养，然后在 RPMI 中培养。五种不同的 CLHPs（TN1-5）用二甲亚砜稀释。将 150 uL 的 CLHPs 和 MA 加入测试平板的第一孔中，然后进行系列稀释，以确定 4 和 512 ug/mL 之间的剂量。然后，将包括 1x10/mL 的 前鞭毛体的 100 uL 培养物加入每个孔中。用 XTT 检查前鞭毛体的活力，然后在 24 和 48 小时评估寄生虫计数。
TN3 在 32 ug/mL 时有效。除 TN5 外，所有测试的 CLHPs 均表现出不同程度的抗活性，即使在最高剂量下也是如此。
TN3 对 表现出特殊的疗效。需要进一步研究，包括候选药物的疗效和毒性测试。
