Stevioside, an abundant component of Stevia rebaudiana leaf, has become well-known for its intense sweetness (250-300 times sweeter than sucrose) and is used as a non-caloric sweetener in several countries. Steviol and isosteviol (metabolic components of stevioside) may offer therapeutic benefits, as they have anti-hyperglycemic, anti-hypertensive, anti-inflammatory, anti-tumor, anti-diarrheal, diuretic, and immunomodulatory actions. In the presence of 16.7 mM glucose both stevioside and steviol enhance insulin secretion from incubated islets in a dose-dependent manner (1 nM to 1 mM). Even though both stevioside and steviol possess an insulinotropic/anti-hyperglycemic effect, steviol is more potent than stevioside. Steviol is an inhibitor of hOAT1 and hOAT3 organic anion transporters. Human organic anion transporter hOAT1 belongs to a superfamily of organic anion transporters, which play critical roles in the body disposition of clinically important drugs including anti-HIV therapeutics, anti-tumor drugs, antibiotics, anti-hypertensives, and anti-inflammatories. Highly purified steviol glycosides have repeatedly received Generally Recognized As Safe (GRAS) status from the US Food and Drug Administration in the past (FDA).