ABSTRACT
OBJECTIVE:To establish HPLC fingerprint of Bining nasal spray.METHODS:HPLC method was performed.The determination was performed on Neptune C18 column with mobile phase consisted of acetonitrile-0.2 ％ phosphoric acid (gradient elution) at the flow rate of 1.0 mL/min.The detection wavelength was set at 326 nm,and the column temperature was 25 ℃.The sample size was 10 μL.Using rutin as reference,HPLC chromatograms of 20 batches of samples were determined.Common peak identification and similarity evaluation were conducted by using Similarity Evaluation System for TCM Fingerprint (2012 edition).RESULTS:There were 40 common peaks in HPLC chromatograms of 20 batches of Bining nasal spray,with similarity ＞0.9.After validation,HPLC chromatograms of 20 batches of samples were in good agreement with the control fimgerprints of those.CONCLUSIONS:Established fingerprint can provide reference for identification and quality evaluation of Bining nasal spray.
ABSTRACT
The phosphatidylinositol 3-kinase (PI3K) pathway is frequently activated in human cancers. Class I PI3Ks are lipid kinases that phosphorylate phosphatidylinositol 4,5-bisphosphate (PIP2) at the 3-OH of the inositol ring to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3), which in turn activates Akt and the downstream effectors like mammalian target of rapamycin (mTOR) to play key roles in carcinogenesis. Therefore, PI3K has become an important anticancer drug target, and currently there is very high interest in the pharmaceutical development of PI3K inhibitors. Idelalisib has been approved in USA and Europe as the first-in-class PI3K inhibitor for cancer therapy. Dozens of other PI3K inhibitors including BKM120 and ZSTK474 are being evaluated in clinical trials. Multifaceted studies on these PI3K inhibitors are being performed, such as single and combinational efficacy, resistance, biomarkers, etc. This review provides an introduction to PI3K and summarizes key advances in the development of PI3K inhibitors.