TABLE 2.

Inhibitory capacity of compounds against LiRpiB^a

Inhibitor	LiRpiB inhibition (%)		Antiparasitic activity (%)			THP1 viability (%)
	Forward	Reverse	Promastigote WT	Promastigote sKO RpiB	Amastigote
2	10 ± 14	21 ± 2	N.A.	N.A.	30 ± 8	92 ± 1
3	12 ± 9	10 ± 4	14 ± 5	9 ± 0	79 ± 26	99 ± 3
25	6 ± 1	6 ± 7	N.A.	N.A.	40 ± 31	115 ± 26
68	N.T.	19 ± 1	N.A.	N.A.	N.A.	120 ± 18
152	N.T.	13 ± 8	31 ± 11	52 ± 24	N.A.	114 ± 15
278	N.T.	4 ± 4	13 ± 1	28 ± 5	N.A.	19 ± 1
338	N.T.	32 ± 10	100 ± 0	102 ± 2	100 ± 17	77 ± 14
372	5 ± 15	26 ± 3	N.A.	N.A.	N.A.	96 ± 5
383	N.T.	−2 ± 1	N.A.	N.A.	N.A.	121 ± 16
540	N.T.	23 ± 5	26 ± 15	64 ± 5	87 ± 15	71 ± 2
565	N.T.	17 ± 1	N.A.	N.A.	N.A.	96 ± 0
576	39 ± 22	14 ± 5	N.A.	69 ± 28	N.A.	21 ± 20
626	N.T.	−7 ± 8	N.A.	N.A.	N.A.	101 ± 4
4PEH	51 ± 19	24 ± 4	N.A.	N.A.	N.A.	82 ± 1

^aThe enzymatic inhibition of all the compounds was determined at 1 mM, except the 4-PEH that was tested at 10 mM. The values correspond to the mean ± SD of the inhibitory effect (%) relative to control (drug absence) from 2–3 independent assays performed in duplicate. The activity of 100 μM of each fragment against L. infantum promastigotes was determined using the resazurin assay (72 h). For the intramacrophagic parasites, THP1 cells infected with parasites expressing luciferase were used. The cytotoxicity and activity determinations were performed with 100 μM of the fragments in an MTT assay involving phorbol myristate acetate (PMA)-differentiated THP-1 cells. Antiparasite and viability data represented are the average ± SD of at least two independent assays performed in at least triplicate. N.A., not active; N.T., not tested.