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Nateglinide, a novel oral hypoglycemic agent, rapidly reaches its maximum serum concentration after oral administration, suggesting that it is rapidly absorbed in the intestine. However, nateglinide itself is not transported by MCT1 or PEPT1. The aim of this study was to characterize the transporters on the apical side of the small intestine that are responsible for the rapid absorption of nateglinide. It has been reported that the uptake of fluorescein by Caco-2 cells occurs via an H+-driven transporter and that the intestinal fluorescein transporter is probably not MCT1. We examined the contribution of the fluorescein transporter to the uptake of nateglinide by Caco-2 cells. Fluorescein competitively inhibited H+-dependent nateglinide uptake. All of fluorescein transporter inhibitors examined reduced the uptake of nateglinide. Furthermore, nateglinide inhibited fluorescein uptake. We conclude that the intestinal nateglinide/H+ cotransport system is identical to the intestinal fluorescein/H+ cotransport system.

The aim of this study was to assess the clinical significance of ankle brachial pressure index (ABI) and carotid intima-media thickness (IMT) in Japanese patients with type 2 diabetes. ABI and ultrasonographic carotid IMT measurements were made in 1311 patients and the relationships between ABI, IMT, and cardiovascular diseases were examined. Patients were assigned to one of three groups depending on their ABI index: (i) ABIor = 1.0; (ii) ABI fromor = 0.9 to1.0; and (iii) ABI0.9. The odds ratios (ORs) for groups (ii) and (iii) compared with (i) for the prevalence of coronary heart disease (CHD), cerebrovascular disorder (CVD), and carotid atherosclerosis (mean carotid IMTor = 1.1mm) demonstrated that these conditions were inversely related to ABI. As the combined ABI/carotid IMT score increased, each OR for the prevalence of CHD and CVD increased significantly. This suggests that a lower ABI is associated with generalized atherosclerosis. Measurements of the ABI and carotid IMT might provide a good prognostic indicator, and both should be assessed during screening for atherosclerosis in Japanese patients with type 2 diabetes.