Natural phosphodiesterase-4 inhibitors from the leaf skin of Aloe barbadensis Miller

Abstract

The ethanolic extract of Aloe barbadensis Miller leaf skin showed inhibitory activity against phosphodiesterase-4D (PDE4D), which is a therapeutic target of inflammatory disease. Subsequent bioassay-guided fractionation led to the isolation of two new anthrones, 6'-O-acetyl-aloin B (9) and 6'-O-acetyl-aloin A (11), one new chromone, aloeresin K (8), together with thirteen known compounds. Their chemical structures were elucidated by spectroscopic methods including UV, IR, 1D and 2D NMR, and HRMS. All of the isolates were screened for their inhibitory activity against PDE4D using tritium-labeled adenosine 3',5'-cyclic monophosphate ((3)H-cAMP) as substrate. Compounds 13 and 14 were identified as PDE4D inhibitors, with their IC50 values of 9.25 and 4.42 μM, respectively. These achievements can provide evidences for the use of A. barbadensis leaf skin as functional feed additives for anti-inflammatory purpose.

Keywords: Aloe barbadensis Miller; Aloe-emodin (PubChem CID: 10207); Aloin A (PubChem CID: 5458893); Aloin B (PubChem CID: 5458894); Aloinoside A (PubChem CID: 46173997); Aloinoside B (PubChem CID: 46173998); Anthrone; Chromone; Cytotoxicity; Isoaloeresin D (PubChem CID: 76332505); PDE4.