Synthesis of positively charged lipids containing a 1,3-oxathiolane cycle

Positively charged lipids of the 1,3-oxathiolane series were synthesized by interaction of 2-pentadecyl-5-tosyloxymethyl- or -5-iodomethyl-1,3-oxathiolane with 2-(N,N-dimcthyl-amino)ethanol.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 9, pp. 2347–2349, September, 1996.     

Synthesis of Alkyllysophospholipid Analogues with Readily Functionalized 1-O-Alkyl Side Chain

Synthesis of alkyllysophospholipid analogues 5a and 5b are described. These lipids have imide functional group attached on the terminal of 1-O-alkyl side chain suitable for further manipulations. Our approach features the use of mesylate 8 in which the mesyl group serves both as protecting group and electrophile.     

A Practical Formal Synthesis of a Physiologically Active Analogue of Platelet Activating Factor

A synthesis of phosphocholine 9 was accomplished in 36% yield from isopropylidene glycerol in contrast to 2% yield as reported previously. Since 9 has been converted to platelet activating factor-analogue 2, this report constitutes a more practical synthesis of 2.     

A Monte Carlo pharmacophore generation procedure: Application to the human PAF receptor

Summary A novel pharmacophore definition procedure is described, which uses a Monte Carlo method to superimpose molecules. Pharmacophore space is searched by a technique similar to high temperature annealing. Subsequent refinement of candidate pharmacophores by energy minimization produces low-energy conformations that may be involved in receptor binding. The method has been applied to compounds that bind to the human platelet-activating factor (PAF) receptor. Alternative binding site models for the PAF receptor are presented and discussed.A preliminary account of this work has been published elsewhere [1].     

高效薄层扫描法测定蛛网膜下腔出血患者脑脊液中血小板活化因子

摘要：建立了测定蛛网膜下腔出血患者（SAH）脑脊液中血小板活化因子（PAF）质量浓度的高效薄层扫描方法。薄层板为高效硅胶G板（100mm×l00mm）,展开剂为V（氯仿）:V（甲醇）:V（水）=65:35:6,下层液展开,显色剂为100g/L磷钼酸溶液,展开距90mm,扫描波长630nm。方法的线性范围0.5～2.5μg/L,相关系数0.9990,最小检测质量浓度50ng/L,平均回收率98.6％。运用所建立的方法测定了16例SAH患者发病后脑脊液和10例非神经系统疾病患者脑脊液中PAF的质量浓度及其变化     

生理和病理过程中重要的磷脂类化合物

作为膜的功能性砌块的磷脂酰胆碱及其类似物, 近年来被发现参与多种重要的生理过程和病理过程, 除了用作磷脂酶抑制剂和血小板活化因子, 还具有抗肿瘤的细胞毒性、潜在的抗AIDS剂以及抗真菌活性等, 这些活性与其结构密切相关, 而且通过膜的介入实现, 代表了一类新型的具有广阔医药学前景的强生理活性化合物。     

Anti-Inflammatory and Anti-Platelet Properties of Lipid Bioactives from Apple Cider By-Products

The valorization of food industry by-products as sources of bioactive compounds is at the forefront of research in functional foods and nutraceuticals. This study focuses on bioactives of apple cider by-products (ACBPs) with putative cardio-protective properties. Total lipids (TLs) were extracted from ACBPs of apple varieties that are low (ACBP1), medium (ACBP2), and high (ACBP3) in tannins and were further separated into polar lipids (PLs) and neutral lipids (NLs). The functionality of these lipid extracts and of their HPLC-derived lipid fractions/PL subclasses were assessed in vitro against human platelet aggregation induced by the thrombotic and inflammatory platelet agonists platelet-activating factor (PAF) and adenosine diphosphate (ADP). The fatty acid profile of PLs and their most bioactive lipid fractions were evaluated by GC–MS analysis. The PL extracts exhibited higher specificity against the PAF-induced platelet aggregation compared to their anti-ADP effects, while TL and NL showed lower bioactivities in all ACBPs. HPLC analysis unveiled that the most bioactive PL from all ACBPs were those in PL fraction 3 containing phosphatidylcholines (PCs). PLs from all ACBPs and their PC bioactives were rich in polyunsaturated fatty acids (PUFAs) and especially in the essential omega-6 (n-6) linoleic acid (LA) and omega-3 (n-3) alpha linolenic acid (ALA), with favorably low values of the n-6/n-3 PUFA ratio, thus providing a rationale for their higher anti-inflammatory bioactivities. Within this study, highly bioactive PL compounds with strong anti-inflammatory and anti-platelet properties were identified in ACBPs, which can be potentially utilized for producing cardio-protective functional foods and/or nutraceuticals.     

Synthesis,characterization and crystal structure of the cis-[RhL2Cl2]Cl complex with the bifunctional ligand (L) 2-(2′-pyridyl)quinoxaline. Biological activity towards PAF (Platelet Activating Factor) induced platelet aggregation

The reaction of RhCl₃·3H₂O with the ligand L = 2-(2′-pyridyl)quinoxaline (pqo) in a 1:2 molar ratio formed the mononuclear complex cis-[RhL₂Cl₂]Cl (1), which has been characterized by elemental analysis, FT-IR, FT-Raman, ¹H, ¹³C NMR, electronic absorption spectroscopy and by electrospray mass spectrometry. The molecular structure of 1 (needle like and prismatic polymorphs) in the crystal has been elucidated by single-crystal X-ray diffraction, revealing a bidentate behavior of L, while the geometry around the Rh(III) atom is that of a distorted octahedron.^. Preliminary biological tests revealed that this compound inhibited PAF-induced rabbit platelet aggregation.     

基于双源CT血管造影技术评估MMP-9、PAF及Lp-PLA2与冠状动脉斑块性质的关系

冠状动脉粥样硬化性心脏病是威胁健康的常见病之一,本研究选取我院2017年2月~2018年12月确诊的206例冠心病患者,其中急性冠脉综合征(acute coronary syndrome,ACS)患者114例(ACS组)、稳定型心绞痛(stable angina pectoris,SAP)患者92例(SAP组),用双源CT血管造影技术检测患者的斑块性质,并检测了血清明胶酶B(MMP-9)、血小板活化因子(PAF)及脂蛋白相关磷脂酶2(Lp-PLA2)浓度,分析MMP-9、PAF及Lp-PLA2与斑块性质间的关系。结果显示,ACS组患者斑块面积和偏心指数均大于SAP组(P<0.05);ACS组患者血清MMP-9、PAF及Lp-PLA2的水平均高于SAP组(P<0.05);ACS组患者易损斑块的比例明显高于SAP组(P<0.05)。所有易损斑块患者血清MMP-9、PAF及Lp-PLA2的水平均高于稳定斑块的患者,且差异具有统计学意义(P<0.05)。患者冠状动脉斑块偏心指数与血清MMP-9、PAF及Lp-PLA2浓度呈正相关关系(P<0.05)。因此,通过双源CT血管造影技术观察冠状动脉粥样硬化斑块性质,结合血清MMP-9、PAF及Lp-PLA2浓度,可以对患者的病情进行评估。血清MMP-9、PAF及Lp-PLA2浓度与斑块的性质及不稳定性有关,可为预测患者冠状动脉斑块性质提供参考。