Ecological biochemistryInhibition of higher plant 2,3-oxidosqualene cyclases by nitrogen-containing oxidosqualene analogues

Add time:08/28/2019    Source:sciencedirect.com

10-Aza-10,11-dihydro-2,3-oxidosqualene (10 N-OS), 19-aza-18,19,22,23-tetrahydro-2,3-oxidosqualene (19 N-OS) and 23-aza-22,23-dihydro-2,3-oxidosqualene (23 N-OS), designed as analogues of carbocationic intermediates involved in the reaction pathway of 2,3-oxidosqualene-cycloartenol cyclase (OSCC) and/or 2,3-oxidosqualene-β-amyrin cyclase (OSβAC), and which could possibly be cyclase activated, were shown to be novel inhibitors of both OSCC and OSβAC in maize and pea microsomes. 10 N-OS had low activity on both plant cyclases with an I50 varying from 60 to 200 μM. 19 N-OS was active on both OSCC (I50 = 40 μM) and OSβAC (I50 = 15 μM), but there was no evidence of enzyme activation. 23 N-OS was also an efficient inhibitor of OSβAC (I50 = 1 μM) and OSCC (I50 = 3 μM), suggesting that it presumably acts as a mimic of the initial C-2 carbocation intermediate involved in the cyclization catalysed by both cycloartenol- and β-amyrin-cyclases.

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