冠突散囊菌来源的2-6-H-5-B化合物的抗炎作用及机制研究

目的 研究冠突散囊菌来源的苯甲醛衍生物(2-6-H-5-B)对脂多糖诱导的RAW264.7细胞的抗炎作用及机制。方法 RAW264.7细胞经不同浓度的苯甲醛衍生物(2-6-H-5-B)(25,50和100 μmol·L^-1)及阳性对照药地塞米松(0.5 μmol·L^-1)预处理1 h后,除对照组外,其余各组给予100 ng·mL^-1 脂多糖刺激诱导24 h。采用Griess试剂法检测NO释放水平,ELISA法分析TNF-α、IL-6和MCP-1的表达水平,以及Western blotting检测AMPK、NF-κB和MAPK信号通路的蛋白表达情况。结果 化合物2-6-H-5-B可以显著抑制活化的巨噬细胞NO(P<0.01或P<0.05)、TNF-α(P<0.01)、IL-6(P<0.01)和MCP-1 (P<0.01)的产生,表现出较好的抗炎活性。研究表明,2-6-H-5-B未能明显阻断NF-κB和MAPK信号通路的活化,但可以显著增加p-AMPK的表达。结论 2-6-H-5-B是一个较有潜力的抗炎药物先导物,其抗炎活性可能与激活AMPK通路相关。     

HPLC法快速检测苦参素注射液中8种抑菌剂及苯甲醛

目的:建立快速筛查和同时测定苦参素注射剂中8种抑菌剂(苯甲醇、苯酚、苯甲酸、山梨酸、对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丙酯、对羟基苯甲酸丁酯)及苯甲醇降解产物———苯甲醛含量的高效液相色谱法。方法:应用WelchMaterials XB-C18色谱柱(4.6 mm×250 mm,5μm);流动相为乙腈-0.02 mol.L-1醋酸铵(冰醋酸调pH至5.0)梯度洗脱,流速1.0 mL.min-1,检测波长为211 nm(苯甲醇、苯酚),225 nm(苯甲酸),248 nm(苯甲醛),256 nm(山梨酸、对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丙酯、对羟基苯甲酸丁酯)。结果:9种成分的峰面积与浓度的线性关系良好(r>0.9998),加样回收率为95.6%～102.2%。结论:本方法灵敏,快捷,准确,重复性好,可用于注射剂中抑菌剂的快速筛查与含量分析。     

顶空气相色谱法测定酮苯丙氨酸钙中六种残留溶剂

目的测定酮苯丙氨酸钙中甲醇、丙酮、异丁醛、2-甲基异丁醛、异丁基甲基酮及苯甲醛含量。方法顶空气相色谱法,氢火焰离子化检测器,以甲苯为溶剂,外标法,采用30m×0.32mm涂布厚度5μm的DB-5毛细管柱。结果3批样品中的6种有机溶剂残留均符合规定。结论方法灵敏,简便,精确,重现性好。     

Nucleophilic [18F]Fluorination and subsequent decarbonylation of methoxy‐substituted nitro‐ and halogen‐benzenes activated by one or two formyl groups

As model reactions for the introduction of ¹⁸F into protected aromatic amino acids, the replacement of NO₂, Cl, Br and F by [¹⁸F]fluoride in 2‐isophthalaldehyde and 2‐terephthalaldehyde derivatives which model ¹⁸F‐DOPA and ¹⁸F‐tyrosine was investigated by comparing labelling yields and reaction rates with those of corresponding mono‐aldehyde compounds. All isophthalaldehydes showed maximum radiochemical yields (79 to 86%) at 140°C and in comparison with the corresponding mono‐aldehydes the reaction proceeded faster. At lower temperature the reaction already resulted in high yields, e.g. 2‐nitroisophthalaldehyde was labelled with a yield of 78% at 25°C after 7 min, whereas 2‐nitrobenzaldehyde only reached a yield of 1.7% under the same reaction conditions. The ¹⁸F/NO₂ exchange in nitroterephthalaldehydes proceeded more slowly and with lower radiochemical yields when compared with corresponding isophthalaldehydes and monoaldehydes. The decarbonylation of ¹⁸F‐labelled aromatic dialdehydic compounds with 4 eq. of Wilkinson's catalyst at 150°C in benzonitrile resulted in high yields, e.g. 2‐[¹⁸F]fluoro‐5‐methoxyisophthalaldehyde and 4‐[¹⁸F]fluoro‐2‐methoxy‐5‐methylisophthalaldehyde were decarbonylated efficiently with yields of 67±3% and 72±2%, respectively. Copyright © 2010 John Wiley & Sons, Ltd.     

Tucaresol increases oxygen affinity and reduces haemolysis in subjects with sickle cell anaemia

The primary pathophysiological event in sickling is the intracellular polymerization of deoxygenated haemoglobin S. Tucaresol (589C80;4[2-formyl-3-hydroxy-phenoxymethyl] benzoic acid), a substituted benzaldehyde, was designed to interact with haemoglobin to increase oxygen affinity and has been shown to inhibit sickling in vitro . We administered tucaresol to sickle cell patients in the steady state to examine the anti-sickling effect in vivo. Oral doses of tucaresol or placebo were given to nine stable sickle cell patients (aged 17–39 years; tucaresol, six; placebo, three) for 10 d. The first two patients on tucaresol were scheduled to receive a loading dose of 800 mg or 1200 mg (depending on bodyweight) for the first 4 d, followed by maintenance doses of 200 or 300 mg for the next 6 d. Due to concerns over the sharp rise in haematocrit in one patient, subsequent cohorts received 300 mg tucaresol daily throughout the dosing period. The oxygen affinity of haemoglobin S was increased in all patients receiving tucaresol, with between 10% and 24% of the haemoglobin modified, dependent on dose. In all patients on tucaresol, haemolysis was reduced with rises in haemoglobin of 0.9–3.7 g/dl (mean 2.2 g/dl), falls in lactate dehydrogenase of 16–52%, and a halving of the irreversibly sickled cell counts. These effects were apparent within a few days and persisted for 1–2 weeks following discontinuation of the drug. Three of the six patients on tucaresol developed fever and cervical lymphadenopathy, with onset between days 7 and 11 from start of drug. Further evaluation of the tolerability and efficacy of tucaresol in sickle cell patients is necessary.     

地黄地上部分中一个新苯甲醛类化合物

运用各种色谱技术对玄参科地黄属植物地黄的地上部分进行分离纯化,从中分离得到7个化合物,根据理化性质和波谱数据分别鉴定为3-hydroxy-4-(4-(2-hydroxyethyl)phenoxy)benzaldehyde(1),异香草酸(isovanillic acid,2),邻苯二酚(pyrocatechol,3),glutinosalactone A(4),金圣草黄素(chrysoeriol,5),芹菜素(apigenin,6),木犀草素(luteolin,7),其中化合物1为新化合物.     

HPLC法快速检测苦参素注射液中8个抑菌剂及苯甲醛

目的:建立快速筛查和同时测定苦参素注射液中8个抑菌剂(苯甲醇、苯酚、苯甲酸、山梨酸、对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丙酯、对羟基苯甲酸丁酯)及苯甲醇降解产物—苯甲醛含量的高效液相色谱法。方法:应用Welch Materials XB-C18色谱柱(4.6 mm×250 mm,5μm),流动相为乙腈-0.02 mol.L-1醋酸铵溶液(冰醋酸调pH至5.0)梯度洗脱,流速1.0 mL.min-1,检测波长为211 nm(苯甲醇、苯酚),225 nm(苯甲酸),248 nm(苯甲醛),256 nm(山梨酸、对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丙酯、对羟基苯甲酸丁酯)。结果:9个成分的峰面积与浓度的线性关系良好(r﹥0.9998),加样回收率为95.6%～102.2%。结论:本方法灵敏,快捷,准确,重复性好,可用于注射剂中抑菌剂的快速筛查与含量分析。     

Molecular Complexation: β-Cyclodextrin and Benzaldehyde Inclusion Complex

Pharmaceutical Research -     

Determination of Dissociation Constants of Selected Cyclodextrin–Benzaldehyde Inclusion Complexes Using Pulse Polarography1

Pharmaceutical Research -     

One‐pot cascade synthesis and in vitro evaluation of anti‐inflammatory and antidiabetic activities of S‐methylphenyl substituted acridine‐1,8‐diones

Various S‐methylphenyl substituted acridine‐1,8‐dione series ( 4a–i ) were synthesized through a one‐pot cascade synthetic approach involving the reaction of 4‐(methylthio)benzaldehyde and dimedone with a variety of amines as nitrogen source under reflux in ethanol. All the synthesized derivatives were characterized by using spectroscopic methods. In vitro evaluations of anti‐inflammatory and antidiabetic efficacies of all the synthesized compounds were investigated. The anti‐inflammatory results infer that the compounds 4c and 4d are showing excellent activity with an inhibition percentage of 80.58 ± 0.42, 81.72 ± 1.72 by membrane stabilization and 77.72 ± 0.76, 78.76 ± 0.81 by albumin denaturation methods, which is comparable with the standard diclofenac at a concentration of 100 μg/ml. Further, the antidiabetic assay revealed the moderate activity for the synthesized compounds at a concentration of 100 μg/ml with respect to their standard drug, acarbose.