Smooth muscle relaxant effect of dehydroindicolactone

Dehydroindicolactone, a novel linear furanocoumarin with an 8-substituted side chain carrying a 5-member ring lactone, showed spasmolytic activity in a number of smooth muscle preparations. The spasmolytic activity seems to lie in its ability to block the dihydropyridine-sensitive calcium channel.     

加减化裁随证治之——何任治疗癌症学术经验探究(下)

癌症为深危重疾,对于绝大部分癌症患者,临床普遍采用手术、中医、化疗、放疗、生物等综合方法进行治疗。由于癌症的种类、所处阶段、先前采用的治疗方法以及病人体质等等的不同,求诊时病人的证     

In vivo activity and metabolic fate of 2-(2,3,3-triiodoallyl)tetrazole (ME1401), a novel antifungal agent

2-(2,3,3-Triiodoallyl)tetrazole (ME1401), a novel antifungal agent, showed therapeutic effectiveness in topical treatment of experimental dermal infections with Trichophyton mentagrophytes and Candida albicans in guinea-pigs. Addition of diethyl sebacate to the ME1401 preparations increased its in vivo antifungal activity and its penetration into the skin. When the estimation of efficacy of treatment with active formulations was made on the basis of skin lesion and the rate of negative skin cultures in comparison with those for infected, untreated or placebo-treated controls, the in vivo activity of 0.5% ethanol tincture or gel of ME1401 was comparable to that of reference antimycotic drugs such as clotrimazole, haloprogin and others. Pharmacokinetic studies in the experimental animals demonstrated that ME1401 was unstable in vivo, being readily converted to an active metabolite 2-(3-iodopropargyl)tetrazole (CN144) first and then to 2-propargyltetrazole (CN151). CN144 showed potent in vitro and in vivo antifungal activities, while the in vitro activity of CN151 was negligible.     

A novel DRB1*09 allelic sequence in the Jing ethnic minority of China.

A new DRB1 allele, DRB1*0902, has been identified in an individual of the Jing ethnic minority. Its sequence was confirmed by sequencing of PCR products and clones. This allele differed by three nucleotides from DRB1*09012 at positions 157, 161 and 166, and resulted in amino acid motif substitution from VAES to DAEY.     

高效液相色谱法测定右旋儿茶素血浆浓度及药代动力学参数

本文建立了体液中右旋儿茶素的RP-HPLC测定方法。采用C_(18)键合相硅胶为填料的固相提取柱进行样品预处理,右旋儿茶素的提取回收率为79.8%.应用二极管阵列检测器对色谱峰纯度进行鉴定。该法精密度好,方法回收率近100%,日内、日间的变异系数为2.4～5.6%,血浓69.6～1160 ng/ml范围内呈线性关系,r=0.9993。家兔静注右旋儿茶素18mg/kg,其药代动力学过程符合二室模型,分布相半衰期为0.129 h,消除相半衰期为1.19h。     

The indication of surgical treatment of cerebellar hemorrhage]

61 patients with cerebellar hemorrhage were studied. The age at onset ranged from 15 to 84 years with a mean of 57.4 years. 49 cases were treated conservatively and 12 surgically and the mortality rates of the two groups were 32.5% and 25% respectively. Based on this study, it is suggested that the clinical and CT indications of surgical treatment of hematoma are as follows; Severe disturbance of consciousness; Bilateral eyeball fixation; Volume of hematoma over 10 ml; Size of hematoma over 4 cm in diameter; Marked acute obstructive hydrocephalus; Compression of cisterna ambieus and quadrigeminus.     

钚促排药物的设计与合成

利用仿生化学的原理，本文设计并合成了两个儿茶酚胺类和两个羟基吡啶酮类八配位的螯合剂，初步动物试验表明，具有较强的钚促排能力。