Sulpiride has an antiaggressive effect in mice without markedly depressing motor activity

The atypical neuroleptic, sulpiride is a selective D2 antagonist, having a preferential action on mesolimbic regions. The effects of acute and chronic treatment with sulpiride on aggressive behaviour in male mice were studied using an ethologically based analysis. It was hypothesized that sulpiride would diminish "threat" and "attack" but would not produce marked "immobility", because of the mesolimbic effect referred to above. Isolated albino male mice (experimental animals) were confronted by "standard opponents". Acutely-treated experimental animals received an intraperitoneal injection of sulpiride (20, 50 or 100 mg/kg) 30 min before testing. Chronically-treated animals received sulpiride (10, 20 or 50 mg/kg) once a day for 7 or 14 consecutive days. Acute treatment with sulpiride had an obvious antiaggressive effect, with significantly decreased time devoted to "attack" and "threat" behaviour. Although time spent in "immobility" was modestly increased, the time devoted to other motor behaviour was also increased. Chronic treatment for 1 or 2 weeks did not change any behavioural category, except "immobility". The antiaggressive action of acutely administered sulpiride is interpreted as a relatively specific dopaminergic antagonist effect and not as merely a non-specific correlate of its disruptive action on motor behaviour. The possible anxiolytic action of sulpiride is also discussed.     

The effect of N-deacetylcolchiceine on serum lipoproteins in rats.

N-Deacetylcolchiceine (DAC) administered i.p. to rats decreased the level of serum cholesterol and apoB. It was accompanied by the fall of HDL-C due to the decrease of both HDL subfractions HDLa and HDLb, and by a rather weaker decrease of LDL-C. The levels of serum and lipoprotein triacylglycerols were not significantly affected. The "clearing reaction" to heparin in DAC rats differed from controls with regard to plasma cholesterol resulting in its accumulation in HDLa and LDL simultaneously with an increased activity of post-heparin lipoprotein lipase. These results suggest that the DAC accelerates the lipoprotein cholesterol metabolism.     

磺胺类药物的毛细管高效液相色谱与电色谱研究

目的 研究毛细管高效液相色谱(μ-HPLC)和毛细管电色谱(CEC)分离磺胺类药物,建立药物微分离分析方法。方法 用ODS柱为固定相,甲醇和2 mmol·L^-1磷酸缓冲液（pH 3.0～7.0）为流动相,电压为0～-15 kV,流速为10 μL·min^-1,紫外检测波长254 nm。结果μ-HPLC在甲醇-2 mmol·L^-1磷酸缓冲液（30∶70）,pH 3.0时5种磺胺类药物实现基线分离;CEC在电压为-5 kV,甲醇-2 mmol·L^-1磷酸缓冲液（30∶70）,pH 5.0时5种磺胺类药物实现基线分离。结论电渗流随甲醇含量、缓冲液浓度增加而下降,随pH值、电压的增加而增加;溶质的保留值（k）随甲醇含量、缓冲液浓度、电压的增加而下降,随电压增加下降明显的是TMP,随pH值变化较复杂。在相同条件下对5种磺胺类药物的分离,μ-HPLC需67 min,CEC只需25 min,后者更适合于磺胺类药物的快速分离分析。     

Synergistic activity of recombinant human endostatin in combination with adriamycin: analysis of in vitro activity on endothelial cells and in vivo tumor progression in an orthotopic murine mammary carcinoma model.

PURPOSE: Current combination treatment strategies in malignancy are designed to evaluate the use of cytotoxic drugs and antiangiogenic agents. Endostatin, a fragment of collagen XVIII, specifically inhibits proliferation, migration, and differentiation of endothelial cells in vitro as well as angiogenesis and tumor progression in in vivo models. In this study, we determine the antitumor effect of rhEndostatin administered alone or in combination with Adriamycin against established orthotopic murine mammary carcinoma. EXPERIMENTAL DESIGN: Mice bearing orthotopically established DA-3 mammary adenocarcinoma tumors received varying doses of rhEndostatin alone and in combination with Adriamycin to assess tumor growth inhibition. Additional studies of this in vivo combination included a determination of Adriamycin-induced cardiotoxicity and in vitro effects on human umbilical vein endothelial cell proliferation and cord formation. RESULTS: For single-agent activity, optimal tumor growth inhibition was observed after s.c. administration of 50 mg/kg/day rhEndostatin or 5 mg/kg Adriamycin injected i.v. every 4 days. Combination of Adriamycin with optimal or suboptimal doses of rhEndostatin resulted in synergistic inhibition of DA-3 tumor growth. Importantly, unlike other antiangiogenic agents, rhEndostatin did not exacerbate the cardiotoxicity of Adriamycin. The synergistic interaction between rhEndostatin and Adriamycin was also observed in vitro for inhibition of human umbilical vein endothelial cell proliferation and inhibition of cord formation. CONCLUSIONS: These data suggest that the synergy observed with rhEndostatin in combination with Adriamycin is exerted at the level of the endothelial cell and can result in enhanced tumor growth inhibition. The potential benefit of Adriamycin used in combination with rhEndostatin is being considered for clinical evaluation.     

Oocyte quality in polycystic ovaries revisited: Identification of a particular subgroup of women

Purpose: Our purpose was to assess the endocrine status of women with polycystic ovaries (PCO) undergoing IVF, and to compare oocyte quality with endocrine markers of the syndrome, in an attempt to define a subpopulation with poor quality oocytes. Methods: This was a retrospective study. Patients were first endocrinologically analyzed: serum levels of androgens (T, androstenedione, DHEAS), FSH, and LH as well as glucose and insulin after an oral glucose tolerance test (OGTT) were recorded and are expressed as absolute values and area under the curve (AUC). Subsequently, they were followed over a 2-year period in which patients underwent several attempts of IVF as well as serving as oocyte donors. Patients were divided into three groups: group I (n=4) was women who displayed embryos unable to implant in 15 IVF cycles and 10 ovum donation cycles in which they served as donors; group II (n=16) was PCO patients in whom IVF (n=38) and/or oocyte donation cycles (n=42) resulted in pregnancies; and group III (n=13) was IVF patients with normal appearance of the ovaries by ultrasound. The endocrine status was compared with the IVF results. Results: There was no difference among groups in the endocrinological parameters tested, except for the OGTT which identified women in group I as having higher serum glucose and insulin levels than patients in groups II and III. Similarly, the OGTT showed higher serum glucose values in group II compared to group III. Women in group I were also obese. Patients in group III were older than PCO patients and needed more gonadotropins to reach an ovarian response which resulted in a reduced number of oocytes retrieved. Fertilization was also impaired in group I, in which no pregnancy was recorded. Conclusions: This study shows that there is a particular subgroup of PCO patients with lower fertilization rates and embryos unable to implant. These patients are obese and nonhyperandrogenic and show derangements of insulin secretion.