Abstract OATP1A4 is an important member of the family of organic anion transporting polypeptides (OATPs), which is generally thought to mediate cellular uptake of endogenous and exogenous substances, such as bile acids, drugs and environmental toxins. Recent studies have found that Oatp1a4 plays an important role in drug passage through the blood-brain barrier and is expected to be an important target for drugs used to treat central diseases. Oatp1a4 has also been associated with various diseases such as cholestasis. differences in Oatp1a4 across age and sex have also become an area of concern for precision drug administration. Therefore, this paper presents a systematic review of Oatp1a4 expression in drug transport and various physiopathological states.

Abstract To evaluate the effectiveness of regulating insulin sensitivity via the insulin receptor substrate-1 of Zingiber striolatum bud extract in C57BL/KsJ-db/db mice. The C57BL mice were randomly divided into 5 groups (n=10), including normal control group, model group, metformin group, ZS-l (ZS low dose) group, and ZS-h (ZS high dose) group. The body weight and blood glucose were determined weekly. The oral glucose tolerance test, plasma insulin and biochemical parameters, pancreas histopathology, and the expression of insulin receptor substrate-1 were assayed at the end of experimental point. The results showed that Z. striolatum bud extract can significantly decrease the fasting blood glucose and glycated hemoglobin levels and insulin resistance (HOMA-IR) in C57BL mice. Western blot analysis demonstrated Z. striolatum bud extract could regulate the insulin sensitivity by upregulating the express of phospho-insulin receptor substrate-1. In conclusion, Z. striolatum bud extract could prevent the progression of diabetes and pancreatic fibrosis in C57BL mice.

Abstract OATP1A1 is the first and founding member of the Organic anion transporting polypeptides (OATPs) family. OATP1A1 is usually considered to mediate the cellular uptake of endogenous and xenobiotics, such as bile acids, drugs and environmental toxins. However, some new research indicated that the decrease of Oatp1a1 expression can result in the cholestasis, which was confirmed by clinic case of drug-induced cholestatic liver injury and bile duct ligation surgery or Oatp1a1-null mice models. These results suggested that Oatp1a1 does not simply transport bile acids to hepatocytes, as is commonly believed. In this overview, we summarized the advances of OATP1A1 in drug induced toxicity, cholestasis and other pathological states as well as the differences of Oatp1a1 in different gender and age.