美丽花网翅虻

本期封面化石照片为美丽花网翅虻 Florinemestrius pulcherrimus Ren,1998,隶属于双翅目短角亚目网翅虻科,采自中国辽宁省北票市晚侏罗世义县组地层。虫体保存十分完整,小仅翅脉、足、腹部清晰可见,口器以及虫体的细毛均保存良好。在辽西义县地层中还有夫量该科的化石,分别归于2属3种。     

Discovery of 5-substituent-N-arylbenzamide derivatives as potent,selective and orally bioavailable LRRK2 inhibitors

Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson’s disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds 8e, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability.     

Evidence for a different metabolism of PC and PE in shoots and roots.

We investigated phosphatidylcholine (PC) and phosphatidylethanolamine (PE) labelling in shoots and roots from leek plantlets, maize seedlings and Arabidopsis thaliana through the incorporation of radiolabelled acetate. Regardless of the pathway followed in shoots, PC labelling was always higher than PE labelling. However, we obtained an opposite situation in leek and A. thaliana roots since PC labelling was much lower than PE labelling. Several hypotheses to explain the origin(s) of these discrepancies between roots and shoots were tested. Among them, neither the level of the respective AAPT activities, nor specific regulations of PC biosynthesis through the mRNA levels of several enzymes (choline citidylyltransferase (CCT), ethanolamine citidylyltransferase (ECT), phosphoethanolamine methyltransferase (PEAMT)), nor the fatty acyl chain composition of PC, PE, and diacylglycerol, were responsible for the differences observed between PC and PE metabolism in roots and shoots. Finally, we investigated the acylation of PC and PE in vitro in both shoots and roots of A. thaliana seedlings, and demonstrated that some specific remodelling of PC and PE by acylation was responsible for the differences in labelling observed in vivo.     

Protective Effects of Adeno-associated Virus Mediated Brain-derived Neurotrophic Factor Expression on Retinal Ganglion Cells in Diabetic Rats

Adeno-associated virus vector plasmid carrying the expression cassette of brain-derived neurotrophic factor (BDNF), pAAV-BDNF, was constructed and packaged into recombinant adeno-associated virus (rAAV-BDNF). The rAAV-BDNF was intravitreally injected into streptzotocin (STZ)-induced diabetic Sprague–Dawley (SD) Rats. Data showed that over-expression of BDNF could increase alive retinal ganglion cell (RGC) number and improve its function in streptzotocin(STZ)-induced diabetic rats, which might be a new method to treat diabetic neuropathy and retinopathy.     

刺桐胰蛋白酶抑制剂亲和填料的制备及纯化瑞替普酶

刺桐属胰蛋白酶抑制剂(ETI)是一种丝氨酸蛋白酶抑制剂,能特异性的抑制胰蛋白酶、组织纤溶酶原激活剂(tPA)、瑞替普酶(rPA)等丝氨酸蛋白酶。实验利用ETI工程菌,经诱导表达、体外复性及纯化获得ETI蛋白,并将该蛋白键合到CNBr活化的琼脂糖凝胶,制备ETI亲和填料,纯化瑞替普酶 。