The Rutaceae family members are widely farmed across the world because of their numerous health advantages for humans and the pharmaceutical and food industries. Citrus is the largest genus of the Rutaceae family. Known throughout the world for their several juicy citrus fruits, Rutaceous 162members have a high percentage of vitamin C as well as several alkaloids. The distinctive and active components of Rutaceae are alkaloids, couma- rins, flavonoids, limonoids, and volatile oils. These natural products exhibit a variety of biological activities, including anxiolytic, anti-inflammatory, hypoglycemic, anthelmintic, anticancer, and anti-infective activities. Over the past few years, these compounds have attracted tremendous interest and may have the potential to become new drug lead compounds. In this chapter, we have compiled the data available so far on the clinical applica- tion of the family Rutaceae.