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Two new 16-nor limonoids, harperspinoids A and B ( 1  and  2 ), with a unique 7/5/5/6/5 ring system, have been isolated from the plant  Harrisonia perforate  together with a known one, Harperforin G ( 3 ). Their structures were elucidated by NMR spectroscopy, X-ray diffraction analysis and computational modelling. Compound 1 exists as polymorphic crystals. Conformations of  1  in solution were further discussed based on the computational results. These compounds exhibited notable inhibitory activity against the 11 β -HSD1 enzyme. Compound  3  had potencies for the inhibition of human 11 β -HSD1 with high selectivity against 11 β -HSD2 (IC 50  0.58  μ M, SI > 174). Molecular docking and quantitative structure-activity relationship studies revealed a mixed regulatory mechanism.

16-nor Limonoids from Harrisonia perforata as promising selective 11β-HSD1 inhibitors