Amorfrutin A is an isoprenoid-substituted benzoic acid natural product found in the fruit of A. fruticosa and G. foetida that exhibits antidiabetic effects. It binds to PPARγ with a Ki of 0.236 µM and activates a PPARγ gene reporter assay with an EC50 value of 0.458 µM. In high-fat diet-induced obese (DIO) mice, amorfrutin A (100 mg/kg/day) enhanced glucose tolerance and insulin sensitivity, while decreasing plasma triglycerides, free fatty acids, insulin, and glucose concentrations. Amorfrutin A inhibits TNF-α-induced expression of a number of inflammatory genes such as COX-2, IL-1β, MCP-1, MIP-2, MIP-3α, MMP-9, and IL-8 through inhibition of both NF-κB and PPARγ activity with efficacy at 5-20 µM.