RESUMEN
Calpains are the family of Ca2+-activated cysteine pro-teases. Although calpains are considered to be cytoplasmic en-zymes, recent research has demonstrated that μ-calpain, m-cal-pain, calpain 10 and their endogenous inhibitor calpastatin are present in the mitochondria and play important roles both in caspase -dependent and-independent pathways in cell death phe-nomena. Calpains exert direct and indirect effects on the caspases and regulators of apoptosis pathway such as Bcl-2, Bax, Bid, promoting the release of Cyt-C, AIF, then result in cellular ap-optosis. To allow pharmacological targeting of these enzymes, thorough knowledge of their patterns of activation and further in-teractions with already known apoptotic pathways is necessary.
RESUMEN
The blood-brain barrier(BBB) is formed by the brain capillary endothelium and excludes from the brain approximately 100% of large-molecule neurotherapeutics and more than 98% of all small-molecule drugs.There are three routines to increase drug transport into brain,ie,neurosurgical,pharmaceutical chemical,and physiological ways and the later is most hopeful.The receptor-mediated transcytosis system on the brain capillary endothelium could be used as multifunctional vectors for drug active transport into brain.This provides the platform for CNS drug delivery programs.
RESUMEN
Aim To investigate the transcytosis mechanism of chlorogenic acid(CGA)by using Caco-2 and MDCK(Madin Darby canine kidney) monolayers models.Method ① Caco-2 and MDCK cell models:Caco-2 cell(105 cells/cm2) and MDCK cell(5?104 cells/cm2) were inoculated in Millicell-CM culture plate inserts,and the TEER of cell monolayer were detected to make sure the models are available for experiments.② Permeating experiments: to measure the value of OD of CGA and calculate the cumulative amount.Result CGA could be Absorbed and secreted on two monolayer models.Verapamil could inhibit the secretion at lower concentration of CGA on MDCK monolayer model.P-pg could partly act on the secretion of CGA on Caco-2 and MDCK cell models.Conclusion CGA can secrete and Absorb at the same time across Caco-2 and MDCK cell monolayers,P-pg partly involving in the secretion of CGA.
RESUMEN
BAPTA-AM is a standard tool agent of calcium chelating.After entering into cells,BAPTA-AM is metabolized by lipase and forms BAPTA.The latter combines with calcium ion rapidly and high selectivity.The effects of BAPTA-AM can effectively protect nerve cells against hypoxic/ischemic injury and protect hepatocytes against cytotoxins attack.BAPTA-AM is a hopeful candidate for treating stroke,liver failure and other clinical critical diseases.
RESUMEN
AIM To study the role of 5-HT in antinocieption produced by intrathecal indomethacin (Ind) in mice. METHOD The antinocieption of indomethacin was investigated on the tail immersion test in mice；the contents of 5-HT, 5-HAA were assayed with fluorescent method. RESULT Dose-dependent antinocieption was observed following intrathecal administration of Ind 1.8 mg*kg-1, the effect could be obliterated when the animals were pretreated with cyproheptadine. After intrathecal administration of Ind, the content of 5-HIAA in the spinal cord of mice was significantly increased, but PG had no effect. CONCLUSION The result imply that intrathecal indomethacin could produce antinocieption; this effect is mediated by 5-HT. PG does not participate in the action of 5-HT.