Anti-Staphylococcus aureus evaluation of gallic acid by isothermal microcalorimetry and principle component analysis

Journal of Thermal Analysis and Calorimetry - The emergence of antibiotic-resistant Staphylococcus aureus requires new antibacterial drugs. In this study, using a thermal activity monitor air...     

Two new chalcones from Shuteria sinensis

Two new chalcones, 2′,3,4,4′-tetrahydroxy-2-prenylchalcone (1) and 3-methoxy-2′,4,4′-trihydroxy-2-prenylchalcone (2), together with two known compounds, munsericin (3) and 3,4-dihydroxylonchocarpin (4), were isolated from the ethanol extract of the whole plant of Shuteria sinensis. Their structures were identified by spectroscopic analysis methods, such as 1D and 2D NMR, along with HR-MS data. Glucose metabolism activity of four compounds was tested, compounds 3 and 4 showed effect on the glucose consumption of insulin-resistant HepG2 cells.     

新型N-杂环取代查尔酮衍生物的合成

以4-二甲氨基苯甲醛与4'-氟苯乙酮为原料,经羟醛缩合反应制得4-二甲氨基-4'-氟查尔酮(1);1分别与咪唑、哌嗪等含氮杂环化合物经取代反应合成了6个新型的N-杂环取代查尔酮衍生物,其结构经1H NMR,13C NMR和IR表征。     

胃肠模拟系统对明矾炮制药材中铝的形态转变影响

根据人体胃肠环境变化特点,调节4个明矾炮制药材的水煎液的酸度,于37℃恒温水浴中保持1h之后,用0.45μm微孔滤膜、732氢型阳离子交换树脂分离水煎液中各种铝形态.湿法消解-石墨炉原子吸收光谱法(GFAAS)测定总铝量；GFAAS直接测定水煎液中各形态铝含量.得到了各样品中铝形态含量及分布情况,并且与未调节酸度的样品进行比较,讨论铝在胃肠的模拟系统影响下的形态转变原因.所得结果对明矾炮制药材中铝的安全性评价有参考价值.     

A new diterpenoid alkaloid from Aconitum hemsleyanum

Abstract

A new C₁₉-diterpenoid alkaloid named hemsleyaline (1), along with fourteen known alkaloids (2-15), were isolated from the roots of Aconitum hemsleyanum Pritz. (Ranunculaceae), a herbal medicine in southwest China. Their structures were established on the basis of extensive spectroscopic analyses. Compound 1 showed mild cholinesterase inhibitory effect with IC₅₀ value of 471?±?9?μM.     

Dopamine derivatives from the insect Polyrhachis dives as inhibitors of ROCK1/2 and stimulators of neural stem cell proliferation

Polyrhachis dives is consumed as an insect food in some regions of China. In this study, new dopamine derivatives, (+)-polyrhadopamine A (1a) and (−)-polyrhadopamine A (1b), (+)-polyrhadopamine B (2a) and (−)-polyrhadopamine B (2b), and polyrhadopamines C–E (3–5), were isolated from this species. The structures and stereochemistry of these substances were assigned by using spectroscopic and computational methods. Compounds 1a, 1b, 2a, and 2b are dimeric N-acetyldopamine derivatives, 3 is a dopamine analog containing an unusual sulfone group, and 4 and 5 possess a rare benzo[d]thiazole moiety. The functions of these substances as ROCK1/2 inhibitors, neural stem cell (NSCs) proliferation stimulators, immunosuppressive, and anti-inflammatory agents were determined.     

哌嗪取代查尔酮衍生物的合成及其细胞毒活性

以4-甲氧基苯甲醛与2-溴-4’-氟苯乙酮为原料,经羟醛缩合脱水、取代反应生成4-甲氧基-4’-(1-哌嗪基)查尔酮(2),再通过酰化反应合成了10个新型含哌嗪的查尔酮衍生物,其结构经~1H NMR、~(13)C NMR及HRMS确证。采用MTT法初步测试了目标化合物的体外细胞毒活性,结果表明,化合物3e和4d对肿瘤细胞株Hela和A549均表现出较好的细胞毒活性,可做进一步研究。     

噪声相互关联时间对Logistic系统亚稳态稳定性的影响

研究了噪声交叉关联时间对Logistic 系统亚稳态稳定性的影响.利用最陡下降法导出了系统亚稳态到稳态的平均第一通过时间的表达式. 数值计算结果表明:内噪声、外噪声、 内外噪声的相互关联时间削弱了亚稳态的稳定性,而内外噪声的关联增加了亚稳态的稳定性.