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Literature summary extracted from

  • Garcia, A.R.; Oliveira, D.M.P.; Claudia F Amaral, A.; Jesus, J.B.; Renno Sodero, A.C.; Souza, A.M.T.; Supuran, C.T.; Vermelho, A.B.; Rodrigues, I.A.; Pinheiro, A.S.
    Leishmania infantum arginase biochemical characterization and inhibition by naturally occurring phenolic substances (2019), J. Enzyme Inhib. Med. Chem., 34, 1100-1109 .
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
3.5.3.1 medicine inhibition of Leishmania arginase leads to a decrease in parasite growth and infectivity and thus represents an attractive therapeutic strategy Leishmania infantum

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.5.3.1 expression in Escherichia coli BL21 (DE3) cells Leishmania infantum

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.5.3.1 apigenin 7-O-beta-D-glucoside 0.1 mM, about 40% inhibition Leishmania infantum
3.5.3.1 caffeic acid 0.1 mM, 56.98% inhibition Leishmania infantum
3.5.3.1 catechin 0.1 mM, about 40% inhibition Leishmania infantum
3.5.3.1 chlorogenic acid 0.1 mM, about 30% inhibition Leishmania infantum
3.5.3.1 dihydroquercetin 0.1 mM, about 25% inhibition Leishmania infantum
3.5.3.1 eugenol 0.1 mM, about 20% inhibition Leishmania infantum
3.5.3.1 fungizone
-
 Leishmania infantum
3.5.3.1 isorhamnetin 0.1 mM, about 55% inhibition Leishmania infantum
3.5.3.1 quercetin 0.1 mM, about 70% inhibition Leishmania infantum
3.5.3.1 Rhamnetin 0.1 mM, about 50% inhibition Leishmania infantum
3.5.3.1 rhaponticin 0.1 mM, about 60% inhibition Leishmania infantum
3.5.3.1 rosmarinic acid 0.1 mM, 71.48% inhibition Leishmania infantum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.5.3.1 5.1
-
 L-arginine pH 9.5, 37°C Leishmania infantum

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.5.3.1 L-arginine + H2O Leishmania infantum
-
 L-ornithine + urea
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.5.3.1 Leishmania infantum A0A145YEM9
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.5.3.1
-
 Leishmania infantum

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.5.3.1 amastigote intracellular Leishmania infantum
-
3.5.3.1 promastigote
-
 Leishmania infantum
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.5.3.1 L-arginine + H2O
-
 Leishmania infantum L-ornithine + urea
-
 ?

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.5.3.1 40 60
-
 Leishmania infantum

Temperature Range [°C]

EC Number Temperature Minimum [°C] Temperature Maximum [°C] Comment Organism
3.5.3.1 25 65 25°C: about 40% of maximal activity, 65°C: about 45% of maximal activity Leishmania infantum

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.5.3.1 9.5
-
-
 Leishmania infantum

pH Range

EC Number pH Minimum pH Maximum Comment Organism
3.5.3.1 8.6 10 pH 8.6: about 55% of maximal activity, pH 10.0: about 60% of maximal activity Leishmania infantum

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.5.3.1 0.00005
-
 pH 9.5, 37°C, activity in promastigote Leishmania infantum fungizone
3.5.3.1 0.0079
-
 pH 9.5, 37°C, activity in intracellular amastigote Leishmania infantum rosmarinic acid
3.5.3.1 0.0219
-
 pH 9.5, 37°C, activity in intracellular amastigote Leishmania infantum caffeic acid
3.5.3.1 0.0573
-
 pH 9.5, 37°C, activity in promastigote Leishmania infantum rosmarinic acid
3.5.3.1 0.0608
-
 pH 9.5, 37°C, activity in promastigote Leishmania infantum caffeic acid
3.5.3.1 0.287
-
 pH 9.5, 37°C, activity in intracellular amastigote Leishmania infantum catechin
3.5.3.1 0.395
-
 pH 9.5, 37°C, activity in promastigote Leishmania infantum catechin
3.5.3.1 0.818
-
 pH 9.5, 37°C, activity in promastigote Leishmania infantum isorhamnetin
3.5.3.1 0.832
-
 pH 9.5, 37°C, activity in promastigote Leishmania infantum Rhamnetin