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The clerodane diterpenoid 2-oxo-5 α ,8 α -cleroda-3,13-dien-16,15-olide ( 1 ) isolated from the leaves of  A. scaber  was identified by IR,  1 H and  13 C NMR (1D and 2D) and HRESIMS spectrometric analysis. This is the first report of this diterpene in the  Aquarius  genus. The inhibitory potential of  1  has been determined against cysteine proteases from  Leishmania mexicana  rCPB2.8, rCPB3.0 and rH84Y. The inhibitory constants ( Ki  and α Ki ) as well as the mechanism of action were also investigated. Compound  1  was 7- and 18-fold more potent in the inhibition of rCPB3.0 (IC 50  = 4.2 µM) than rCPB2.8 (IC 50  = 20 µM) and rH84Y (IC 50  = 75 µM). From the kinetic mechanisms of inhibitor binding, we found that compound  1  has a higher affinity to rCPB3.0 ( Ki  = 7.5 µM and α Ki  = 7.4 µM) than rCPB2.8 ( Ki  = 15.4 µM, α Ki  = 14.7 µM) and rH84Y ( Ki  = 81.4, and α Ki  = 27.9 μM and β K i= 41.5 µM). Compound  1  also presented a non-competitive linear simple inhibition mechanism at both enzymes rCPB3.0 and rCPB2.8. On the other hand,  1  presented a positive cooperativity mechanism of inhibition at rH84Y.

A Clerodane Diterpene from Aquarius scaber (Rataj) Christenh. & Byng Leaves as Inhibitor of Leishmania mexicana Trypanosomatid Enzymes