Kynurenine aminotransferase activity in human liver: identity with human hepatic C-S lyase activity and a physiological role for this enzyme

The C-S lyase enzymes are responsible for the generation of mutagenic and cytotoxic metabolites via aberrant drug-metabolising pathways in mammalian tissues. We have examined human hepatic cytosolic, mitochondrial and microsomal fractions for evidence of C-S lyase activity. The cytosolic enzyme was purified using fast protein liquid chromatography over FFQ Sepharose, Mono P and Superose 12. An homogeneous protein (monitored by SDS-PAGE) was obtained following purification, and an 11-fold increase in C-S lyase specific activity was observed. The molecular weight of the enzyme was found to be 37 kDa in denaturing conditions, 82.3 kDa in non-denaturing conditions, and the C-S lyase activity was shown to co-purify with kynurenine aminotransferase activity when the transaminase activity of the enzyme was examined with kynurenine as the substrate.     

甲氟哌酸体外抗菌活性及对耐药感染者的治疗

对天津市新近临床分离的414株细菌进行了甲氟哌酸(Pflx)和氟哌酸(Nflx)体外抗菌活性研究。结果显示Pflx对绝大多数肠杆菌和细菌、不动杆菌有良好抗菌活性,抑菌率>90％。对绿脓杆菌、MSSA及凝固酶阴性葡萄球菌有中度抗菌作用,抑菌率分别为85％、87.5％、87.5％。对MRSA和链球菌抗菌活性稍差,抑菌率在40％～68.42％之间。Nflx体外抗菌活性和Pflx相似。此外,18例药敏试验耐Pflx和Nflx细菌感染患者,经Pflx治疗,肺化脓症1例显效,余17例难治性尿路感染者1例痊愈、9例显效、5例进步、2例无效。     

血康口服液与他莫昔芬联合治疗免疫性血小板减少性紫癜疗效观察

联合应用血康口服液和他莫昔芬治疗成人免疫性血小板减少性紫癜(ITP)20例。疗程超过2月。15例患者的血小板(BPC)计数明显上升,有效率为75％(15/20),对于激素治疗无效者,仍有良效。对月经过多者和不适合应用激素者尤为适应。两药合用无明显副作用。治疗起效时间较快,平均13天。疗效持续时间较长,长者已达一年以上。     

血液胆碱酯酶活力测定方法的进一步研究Ⅰ．红细胞／全血胆碱酯酶活力比例及红细胞计数校正酶活力值的研究

应用硫代乙酰胆碱－联硫代双硝基苯甲酸（ＡＳＣｈ－ＤＴＮＢ）比色测定法，测定了４０名健康者及５名贫血者血样的全血胆碱酯酶（ｂｌ－ＣｈＥ）活力值、红细胞胆碱酯酶（ｅ－ＣｈＥ）活力值及血浆胆碱酯酶（ｐ－ＣｈＥ）活力值，探讨它们之间的比例关系并用红细胞计数值（ＲＢＣ）校正酶活力。结果表明：ｅ－ＣｈＥ与ｂ１－ＣｈＥ之间关系密切（ｒ＝０．９４８，Ｐ＜０．００１），ｅ－ＣｈＥ稳定地占ｂｌ－ＣｈＥ的８４．９７％，在质和量两方面验证了以ｂｌ－ＣｈＥ值表示ｅ－ＣｈＥ值的可靠性和可信程度，血液胆碱酯酶（ｂ１ＣｈＥ）活力主要取决于ｅ－ＣｈＥ活力，ＲＢＣ值的离散对ｅ－ＣｈＥ值有极大影响，故用ＲＢＣ值校正ｅ－ＣｈＥ活力，这样可缩小人群测定值的变异度，得到较难确的群体均值；消除男女之间测定值的差异，建立更合理和通用的临界参比值，极大地方便了使用，使血液胆碱酯酶（ＣＨＥ）活力测定法在防治有机磷农药中毒中的应用，更为敏感和特异。     

Synthesis and cytotoxic activity of new alkyl[3-(2-chloroethyl)ureido]benzene derivatives

Several alkyl[3-(2-chloroethyl)ureido] (CEU) benzene derivatives were prepared as potential anticancer agents. These new compounds were readily prepared in good yields by addition of anilines to 2-chloroethylisocyanate. Their cytotoxic activity was evaluated on human breast cancer (MDA-MB-231), human colon adenocarcinoma (LoVo) and mouse lymphocytic leukemia (P388D₁) tumor cell lines. Several new CEUs were significantly more cytotoxic than the nitrogen mustard chlorambucil. The biological activity of these aromatic urea derivatives seems to be related to the nature and position of the alkyl substituents on the aromatic ring. Substitution by branched alkyl groups on position 4 of the aromatic ring led to cytotoxic molecules which are up to 5 times more potent than the standard chlorambucil.     

Intramuscular dexmedetomidine premedication—an alternative to midazolam-fentanyl-combination in elective hysterectomy?

Sedation, anxiolysis, intubation responses and fentanyl anaesthetic requirements were investigated in a double-blind, randomized study in twenty ASA I-II elective hysterectomy patients. Ten patients received dexmedetomidine 2.5 μg kg^-1 i.m. 60 min before induction and saline placebo i.v. 2 min prior to induction (= DP group). Ten patients received midazolam 0.08 mg kg^-1 i.m. 60 min and fentanyl 1.5 μg kg^-1 i.v. (= MF group) 2 min before induction of anaesthesia with thiopentone 4 mg kg^-1. Anaesthesia was maintained with 70% nitrous oxide in oxygen and with fentanyl 2 μg kg^-1 i.v. increments according to predetermined criteria. Both premedications induced sedation ( P < 0.01 in both groups) and anxiolysis ( P < 0.01 in DP vs <0.05 in MF group) without any differences between the groups. Haemodynamic changes following tracheal intubation did not significantly differ between the groups. Intraoperatively systolic and diastolic arterial pressure were 15% and 13% lower in DP group ( P < 0.01 and P < 0.05 for drug effect), the mean heart rate was approximately 9 beats min^-1 lower in DP group (n.s.). Fentanyl was required more often in MF group: median 3.5 (QD 1.5) vs. 2.5 (QD 0.5) times in DP group ( P < 0.05), the total amount being 57% smaller in DP group: 0.03 (QD 0.01) vs. 0.07 (QD 0.02) μg kg^-1 min^-1 ( P < 0.05). Postoperative course and analgesic requirements were similar in both groups. Dexmedetomidine premedication may offer an alternative to current anaesthesia practice in elective hysterectomy.     

Diving physiology and pathophysiology

Summary. Divers have worked at 500 m depth in the sea and have reached 700 m in simulated chamber dives. A prerequisite for this has been extensive physiological studies of the body's reactions to pressure and pressure changes. This paper reviews such physiological and pathophysiological studies with emphasis on recent developments.     

脑梗塞患者血清脂蛋白（a）测定及其临床意义

应用酶标法测定58例脑梗塞患者和56例健康对照者血清脂蛋白(a)[LP(a)]含量,并同时测定了其他脂代谢指标,对其中26例脑梗塞患者还测定了血浆纤维蛋白溶解(简称纤溶)指标。结果表明脑梗塞组存在显著的脂代谢和纤溶功能紊乱。LP(a)含量增高,与所测脂代谢、纤溶指标无显著相关,是脑梗塞发病独立的危险因素。