Renin, a highly specific aspartic proteinase originated from kidney, is a ratelimiting enzyme in renin-angiotensin system. Recently, we developed effective expression system for recombinant human (rh) renin using baculovirus-insect cell expression system, and simple and rapid assay method for rh-renin using internally quenched fluorogenic (IQF) substrate. Using the purified rh-renin and the IQF substrate, we constructed rapid and sensitive renin inhibitor screening system. Using the system, we found renin inhibitors in various foodstuffs. The isolation and characterization of renin inhibitors from soybean, rice, and wild vegetables and structure-function relationship of the inhibitors are also discussed.

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