| Description |
PT4 is a therapeutic agent against Cutaneous leishmaniasis (CL). PT4 is effective against both species of Leishmania, with IC50s of 125.18 and 233.18 μM for L. amazonensis and L. braziliensis, respectively. PT4 decreases of mitochondrial membrane potential and increases production of reactive oxygen species, which leads to parasite death. PT4 has a potent in vivo anti-inflammatory activity[1].
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| Related Catalog |
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| In Vitro |
PT4 (0-1256.5 µM, 48 hours) can inhibit mammalian cells viability[1]. PT4 (314.1-19.6 μM, 48 hours) inhibits the growth of promastigote and amastigote of L. amazonensis and L. braziliensis promastigotes[1]. PT4 causes depolarization of the mitochondrial membrane of L. amazonensis and L. braziliensis promastigotes and increasing ROS in mitochondria[1]. Cell Cytotoxicity Assay[1] Cell Line: Balb/c mice peritoneal exudate (mPEC), J774A.1 macrophages, Fibroblasts Concentration: 0-1256.5 µM Incubation Time: 48 hours Result: Inhibited mPEC, J774A.1 and fibroblasts with CC50 value of 981.37 μM, 521.47 μM and 895.17 μM, respectively. Cell Proliferation Assay[1] Cell Line: L. amazonensis, L. braziliensis promastigotes Concentration: 314.1-19.6 μM Incubation Time: 48 hours Result: Inhibited promastigote of L. amazonensis and L. braziliensis promastigotes with IC50 value of 70.46 μM and 181.73 μM, respectively. Inhibited amastigote of them with IC50 value of 125.18 μM and 233.18 μM, respectively.
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| In Vivo |
The pharmacokinetic and toxicological parameters of PT4 Parameter HBA (≤10) 4 HBD (≤5) 0 LogP (≤5) 2.23 MW (≤500) g/mol 318.33 n-ROTB (≤10) 4 TPSA (A2) 68.09 BBB Yes GIA High P-GP substrate No Skin permeability (cm/s) -6.85 CYP450 2C9 inhibitor Yes CYP450 2D6 inhibitor No CYP450 2C19 inhibitor Yes CYP450 3A4 inhibitor No CYP450 1A2 inhibitor Yes Total Clearance (log ml/min/kg) 0.117 Renal OCT2 substrate No LD50 (mg/Kg) 4700
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| References |
[1]. Vanderlan Nogueira Holanda, et al. Antileishmanial activity of 4-phenyl-1-[2-(phthalimido-2-yl)ethyl]-1H-1,2,3-triazole (PT4) derivative on Leishmania amazonensis and Leishmania braziliensis: In silico ADMET, in vitro activity, docking and m
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