Cytotoxic constituents from the roots ofAnthriscus sylvestris

Activity-guided fractionation of the roots of Anthriscus sylvestris resulted in the isolation and characterization of five cytotoxic compounds, deoxypodophyllotoxin (1), falcarindiol (2), and angeloyl podophyllotoxin (5) from the hexane soluble fraction and morelensin (3), bursehernin (4) from the chloroform soluble fraction. It is the first report of the occurrence of compound 5 in nature.     

Chiral separation of β-blockers after derivatization with (−)-menthyl chloroformate by reversed-phase high performance liquid chromatography

Optimum conditions of chiral derivatization reaction of beta-blockers acebutolol, arotinolol, beta-xolol, bisoprolol, celiprolol, metoprolol and pindolol) with (-)-menthyl chloroformate were investigated for the resolution by HPLC. With more than 30 times molar excess of (-)-menthyl chloroformate chiral derivatization reactions were completed within one hour at room temperature except arotinolol and celiprolol. Diastereomeric derivatives of beta-blockers were well resolved on the ODS column using acetonitrile-methanol-water as a mobile phase.     

Synthesis andin vitro antibacterial activity of C-3′ pyridinium cephalosporin derivatives

The quaternary ammonium cephalosporin derivatives were prepared with various pyridines substituted at the 3 or/and 4 position. Their in vitro antibacterial activities were determined and substituent effect on pyridine nucleus was studied. Preparation of substituted pyridines are also described.     

Inducible nitric oxide synthase inhibitors fromMelia azedarach var.Japonica

In bioassay-guided search for inducible nitric oxide synthase (iNOS) inhibitory compounds from higher plants of South Korea, two beta-carboline alkaloids, 4-methoxy-1-vinyl-beta-carboline (1) and 4,8-dimethoxy-l-vinyl-beta-carboline (2) have been isolated from the cortex of Melia azedarach var. japonica. The structures of these compounds were elucidated on the basis of spectroscopic data. Compounds 1 and 2 showed marked inhibitory activity of iNOS on LPS- and interferon-gamma-stimulated RAW 264.7 cells.     

Cytotoxicity of urushiols isolated from sap of Korean lacquer tree (Rhus vernicifera stokes)

Cytotoxicities of four urushiols, congeners isolated from the sap of Korean lacquer tree (Rhus vernicifera Stokes), to 29 human cancer cell lines originated from 9 organs were evaluated. Their values of 50% growth inhibition were below 4 microg/ml, and showed cell line specific cytotoxicity. The present result is the first report on the cytotoxicity of urushiols suggesting that they would have an anticancer activity to human cancer cells.     

氟伐他汀对自发性高血压大鼠阻力血管 功能的影响

AIM: To evaluate the effects of fluvastatin, a hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor, on the alterations of structure and function of resistant vessels in spontaneously hypertensive rats (SHR). METHODS: Eight-week-old male SHR were given fluvastatin 20 mg.kg-1.d-1 by gavage. Rats were decapitated at 16 wk. Wall-to-lumen area ratios (W/L) of thoracic aorta and mesenteric arteries (3rd grade branch) were assessed by morphometric assay. The effects of fluvastatin on vascular reactivity to sodium nitroprusside (SNP) and norepinephrine (NE), were studied with rings of thoracic aorta and mesenteric arteries isolated from rats. RESULTS: After 8 wk of treatment, histological examination showed that the wall-to-lumen area ratio was lower in SHRflu than that in SHR (0.44 +/- 0.09 vs 0.79 +/- 0.09, P < 0.05). EC50 of vasodilation response was much lower in SHRflu than that in SHR [(4.9 vs 190) pmol.L-1, P < 0.05], while EC50 of mesenteric artery rings from SHRflu was somewhat lower than that of SHR [(0.02 vs 0.04) nmol.L-1, P > 0.05]. In both aortic and mesenteric artery rings, EC50 of vasoconstriction in response to NE from SHRflu was higher than that of SHR [thoracic aorta: (0.20 vs 0.02) nmol.L-1, P < 0.05; mesentric arteries: (1.46 vs 0.72) nmol.L-1, P < 0.05]. CONCLUSION: Short-term treatment with fluvastatin ameliorated the vasomotoricity of resistant vessels, enhanced the sensitivity to vasodilator and depressed the sensitivity to vasoconstrictor; fluvastatin also attenuated the resistant vascular hypertrophy during the development of hypertension in SHR.     

色甘胺醇气雾剂的高效液相色谱测定法

目的： 建立高效液相色谱法同时测定色甘胺醇气雾剂中的２ 个有效成分色甘酸钠和硫酸沙丁胺醇。方法： 采用Ｃ１８ 色谱柱, 以０－０２ ｍｏｌ·Ｌ－ １ 醋酸铵（ 用冰醋酸调节ｐＨ 为６－０ ±０－１） － 甲醇（１００∶３０） 为流动相, 检测波长为２２７ ｎｍ－ 结果： 色甘酸钠和硫酸沙丁胺醇的平均回收率（ ｎ ＝ ５）分别为９９－１２ ％ 和９９－９８ ％ ; 精密度（ ＲＳＤ） 分别为１－１ ％ 和１－０ ％ 。结论： 该测定方法简便快速     

定志丸对东莨菪碱诱发大鼠被动回避反应的影响

唐·孙思邈《备急千金要方》的定志丸在防治记忆障碍作用上较《太平惠民和剂局方》记载的定志丸为佳。茯苓、远志、石菖蒲有协同人参之作用。《和剂局方》中的朱砂未见有改善学习记忆障碍的作用,故无组成方剂意义。     

Biomarkers in airway tumors

Despite advances and improvements in diagnosis and treatment of upper aerodigestive tumors including head and neck and lung cancers, the overall survival rate of these patients remains poor. Prevention, early diagnosis, and novel therapy are under active investigation to improve the outcome of the diseases. In particular, chemopreventive strategy is a novel approach to reduce the invasive tumors by reversing the premalignant lesions with certain differentiating agents (i.e., retinoids). To conduct effective chemopreventive trials, there has been a great surge of interest in defining the biomarkers associated with the specific stages of the carcinogenesis and with intermediate end points during the therapy. Carcinogenesis in the upper aerodigestive tract has been explained by two theories, field cancerization and multistep process. The driving forces behind these processes are noted by accumulated genetic abnormalities in the entire epithelium of the airway. These genetic abnormalities include chromosome abnormalities, specific gene alterations (i.e., ras gene family, tumor suppressor genes, growth factors and their receptors), and proliferation and differentiation markers. These biomarkers are herein described in this review article.     

使用Excel 7.0for Windows95优化换热网络

提出了使用Ｅｘｃｅｌ ７．０ ｆｏｒ Ｗｉｎｄｏｗｓ９５简便和快速优化换热网络的方法。首先由Ｍｏｎｔｅ Ｃａｒｌｏ法确定全局最优点的近似位置,然后由“Ｓｏｌｖｅｒ”求得精确解。全部优化过程由ＶＢＡ语言编写。此法可用于解决许多工程优化问题。