避蚊胺原药大鼠亚慢性（180d）经口毒性研究

目的：研究避蚊胺原药对大鼠亚慢性（180d）经口毒性,得出最大无作用剂量。方法：按照《农药登记毒理学试验方法》（GB15670—1995）进行试验。观察体重、血液生化、血常规指标、脏器系数及主要脏器组织病理学改变。结果：染毒1-26周各剂量组雌、雄大鼠体重、进食量无显著差异：各剂量组雌、雄大鼠各血液学指标均未见异常;各剂量组雌、雄大鼠生化指标均未见异常;各剂量组大鼠尿常规检测未见异常;各剂量组雌、雄大鼠的各被检脏器系数无显著差异：高剂量组和对照组各主要脏器均未见明显的病理学改变。结论：在本试验条件下,避蚊胺原药对雌、雄大鼠亚慢性（180d）经口毒性试验的最大无作用剂量雌性（206．89±52．01）mg／kg,雄性（179．38±63．87）mg／kg。     

避蚊胺原药对大鼠亚急性经皮毒性研究

目的：研究避蚊胺原药对大鼠的-2急性经皮毒性,得出最大无作用剂量。方法：按照《农药登记毒理学试验方法》（GB15670～1995）进行试验。观察体重、血液生化、血常规指标、脏器系数及主要脏器组织病理学改变。结果：高剂量组雄性大鼠体重增长缓慢、肝脏器系数升高,雌性大鼠未见各项指标异常。结论：在本试验条件下,避蚊胺原药雌、雄大鼠亚急性经皮毒性试验的最大无作用剂量为雌性1000mg／kg,雄性300mg／kg。     

生物农药阿维菌素的NEL和ADI研究

研究了阿维菌素原药的急性和亚慢性毒性及致突变性。结果显示,大鼠经口LD50雌雄性均为21.5mg/kg,小鼠经口LD50雌性为68.1mg/kg,雄性为38.3mg/kg,大鼠经皮LD50雌雄性均大于2000mg/kg。家兔急性皮肤刺激试验,对皮肤的刺激强度属无刺激性。家兔眼刺激试验,对眼的刺激强度属轻度刺激性。小鼠骨髓多染红细胞微核试验和小鼠睾丸精母细胞染色体畸变试验均为阴性。大鼠亚慢性经口毒性试验,21.5mg/kg饲料组雌性大鼠体重增加量低于对照组,雌雄性大鼠食物利用率低于对照组,雌雄性大鼠心/体比、肺/体比、肾/体比高于对照组,雌性大鼠脑/体比高于对照组,雄性大鼠脾/体比低于对照组,雌雄性大鼠血液生化指标ALB、GLU高于对照组。最大无作用剂量(NEL)为:雌性大鼠(0.796±0.062)mg/kg·d,雄性大鼠(0.635±0.056)mg/kg·d。若以安全系数100倍考虑,人的每日允许摄入量(ADI)应为0.0058mg/kg·bw。     

磷酸二氢钾催化合成DA-6

用磷酸二氢钾作催化剂,己酸与二乙氨基乙醇为原料,合成DA-6（己酸二乙氨基乙醇酯）。通过正交试验确定了合成的最佳工艺条件：醇酸物质的量比为1．1：1,反应时间10h,1mol己酸用催化剂0．059mol,产品酯化率可达92％以上。     

避蚊酯的毒性试验

研究了避蚊酯原药的急性和亚慢性毒性及致突变性。结果显示:大鼠经口LD50雌性为10000mg/kg,雄性为12100mg/kg,大鼠经皮LD50雌雄性均大于2000mg/kg。家兔急性皮肤刺激试验,对皮肤的刺激强度属无刺激性。家兔眼刺激试验,对眼的刺激强度属中度刺激性。小鼠骨髓多染红细胞微核试验和小鼠睾丸精母细胞染色体畸变试验均为阴性。大鼠亚慢性经口毒性试验,对体重、摄食量、食物利用率、血液指标及血液生化指标均无明显影响,11000mg/kg饲料组雌性大鼠肾/体比、雄性大鼠肝/体比可见增高。病理检查发现,11000mg/kg饲料组4只大鼠可见肝脏1￣2个小炎症灶,2只大鼠少数肾小管上皮细胞肿胀。最大无作用剂量为:雌性大鼠393.67±26.98mg/kg·d,雄性大鼠336.65±26.38mg/kg·d。     

制蚜菌素毒性研究

研究制蚜菌素的急性、亚慢性毒性及致突变性结果表明,急性经口LD50雌雄性大鼠均为38.3mg/kg,雄性小鼠为38.3mg/kg,雌性小鼠为17.8mg/kg,急性经皮LD50雄性大鼠为1470mg/kg,雌性大鼠为1210mg/kg;小鼠骨髓多染红细胞微核试验、小鼠睾丸精母细胞染色体畸变试验及Ames试验结果均为阴性。大鼠亚慢性经口毒性无作用剂量雄性大鼠为(0.18±0.01)mg/(kg.d),雌性大鼠为(0.22±0.02)mg/(kg.d)。     

氯胺嘧草醚原药亚慢性经口毒性试验

[目的]研究氯胺嘧草醚原药对大鼠的亚慢性毒性和最大无作用剂量。[方法]根据GB 15670—1995《农药登记毒理学试验方法》,按0、62、250、1 000mg/kg剂量开展90 d喂养试验。[结果]高剂量组雄鼠总蛋白、白蛋白以及球蛋白值明显升高;中高剂量组雌鼠及高剂量组雄鼠心、肝等脏器湿重及脏器系数明显升高;中高剂量组大鼠肾小管上皮细胞混浊肿胀、水样变性。[结论]大鼠90d亚慢性经口最大无作用剂量:雌77.37 mg/kg,雄73.55 mg/kg,推荐ADI值为0.073 mg/kg。     

壬菌铜原药亚慢性毒性试验

[目的]观察壬菌铜原药对大鼠的毒性作用和无作用剂量。[方法]将壬菌铜原药按0、2.5、25、250 mg/kg剂量分别拌入饲料内经口喂饲染毒90 d,观察大鼠外观体征、体质量、进食情况等。染毒结束进行血常规、血生化、脏器系数及病理组织学检测。[结果]高剂量组雌、雄性大鼠的体质量增长显著低于对照组。摄食受到抑制,血常规、血生化、尿液检查均未出现明显异常的指标改变。[结论]确定大鼠90 d亚慢性经口最大无作用剂量为2.5 mg/kg,推荐ADI值为0.002 5 mg/kg。     

1,6-二磷酸果糖三钠盐缓解小鼠体力疲劳作用研究

目的:研究1,6-二磷酸果糖三钠盐缓解小鼠体力疲劳的功效。方法:以1,6-二磷酸果糖三钠盐为受试物,分83,167,500 mg/kg·bw/d三个剂量经口给予小鼠一个月,测小鼠的负重游泳时间、血浆尿素水平、肝糖原储备量及血乳酸值。结果:500 mg/kg·bw/d组小鼠负重游泳时间长于0 mg/kg·bw/d组; 500 mg/kg·bw/d组小鼠血浆尿素水平低于0 mg/kg·bw/d组; 167,500 mg/kg·bw/d组小鼠肝糖原储备量高于0 mg/kg·bw/d组,差异均有统计学意义(P0.05)。结论:1,6-二磷酸果糖三钠盐具有抗疲劳的功效。     

新稻田芽后除草剂Nominee

通用名bispyribac－sodium（ISO建议名）;商品名Nominee;试验代号KIH－2023、KUH911;化学名钠2,6-双〔（4,6-二甲氧基嘧啶-2-基）氧代〕苯甲酸酯。1理化性质白色粉末;熔点223～224℃;蒸气压5．04×10（－9）Pa（25℃）;水溶性73．3g／L。2制剂100SC（100ga．i．／L不含助剂）;400gy（400ga．i．／L不含助剂）;2％LC（2％w／w含助剂）。3毒性bispyribac－sodium大鼠急性经口LD（50）：雌性41111mg／kg,雄性2635mg／kg;小鼠3524mg／kg。大鼠急性经皮LD（50）＞20000g／kg,大鼠急性吸入LC（50）（4－H）＞4．48mg／L。…     

The Hypolipidemic Effect of an Ethyl Ester of Algal-Docosahexaenoic Acid in Rats Fed a High-Fructose Diet

Preclinical and clinical studies demonstrate that the omega-3 fatty acids docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) as a triacylglycerol (TAG) or an ethyl ester are protective against cardiovascular disease. Both have significant TAG-lowering effects. We developed a concentrated ethyl ester of DHA (MATK-90, 900 mg/g) using microalgae as its source. This study evaluated the effects that different doses of MATK-90 had on lipid levels and clinical parameters in male Wistar rats fed a high-fructose diet used to induce hypertriglyceridemia (TAG ≥ 300 mg/dL). Effects of MATK-90 were compared to those produced by a pharmaceutical product (Lovaza, formerly Omacor, P-OM3; 465 mg EPA + 375 mg DHA), a TAG oil used in food (DHASCO, algal-DHA, 40% DHA by weight), and a control (corn oil). Doses of MATK-90 (0.6, 1.3, 2.5, 5.0 g kg^?1 day^?1), algal-DHA (2 g DHA kg^?1 day^?1), and P-OM3 (5.0 g kg^?1 day^?1) were administered by oral gavage for 28 days. A significant dose-related decrease was observed in TAG and cholesterol levels in all but the lowest dose of MATK-90 treatment group vs. control. The high-dose group of MATK-90 and the P-OM3 group produced similar reductions in TAG levels.     

固体超强酸SO4^2-/Fe2O3-CoO催化合成己酸乙酯

以固体超强酸SO4^2-/Fe2O3-CoO为催化剂，通过己酸和乙醇反应合成了己酸乙酯。实验结果表明，固体超强酸SO4^2-/Fe2O3-CoO对酯化具有较高的催化活性，反应的最佳条件为：己酸0．2mol，n（乙醇）：n（己酸）：1．8：1．0，催化剂用量为0．8g（以0．2mol己酸为准），带水剂用量为12mL，反应时间为2h，其酯化率可达97％以上。     

滇刺枣挥发性成分的研究

用同时蒸馏萃取方法收集滇刺枣的挥发性成分,所得到的滇刺枣挥发性成分的二氯甲烷浓缩液用气相色谱-质谱(GC-MS)法分离并分析鉴定其成分及质量分数,共鉴定出40个化合物,占总峰面积的79 07%,主要挥发性成分有:w〔邻苯二甲酸二(2 乙基)己酯〕=18 00%、w(邻苯二甲酸二丁酯)=12 33%、w〔5 己基二氢 2(3H) 呋喃酮〕=4 60%、w(2 十二烯 4 酮)=2 75%、w(2 十三烷酮)=2 25%、w(十四烷)=2 15%、w(二十烷)=1 44%、w(十四烷酮)=2 14%、w(E 2 癸烯醛)=2 07%、w(2 壬烯 4 酮)=2 00%、w(己酸己酯)=1 93%、w(壬醛)=1 87%、w(丙基丙二酸)=1 73%、w(5 甲基糠醛)=1 70%、w(二十九烷)=1 52%、w(十三酸乙酯)=1 52%、w(己酸乙酯)=1 46%、w(6 甲基 2 十三烷酮)=1 30%、w(十四酸乙酯)=1 09%、w(4 羟基 6 甲基 2H吡喃 2 酮)=1 09%、w(丁基化羟基甲苯)=1 02%等。     

Recovery of fish oil-derived fatty acids in lymph of thoracic duct-cannulated wistar rats

The absorption of equivalent doses of eicosapentaenoic and docosahexaenoic acids was compared in rats when administered as the ethyl ester concentrate, ethyl ester concentrate plus olive oil, free fatty acid or triacylglycerol (menhaden oil). Lymph was collected from a thoracic duct cannula for 24 hr after dosing via an indwelling duodenal catheter. After 24 hr, the absorption of eicosapentaenoic acid was greater for the free fatty acid and menhaden oil than for the ethyl ester form, but docosahexaenoic acid absorption was comparable for all forms. Other rats had greater plasma levels of eicosapentaenoic and docosahexaenoic acids 5 hr after oral gavage dosing with menhaden oil than did rats dosed with the ethyl ester form.     

Ester components of aggregation pheromone ofDrosophila virilis (Diptera: Drosophilidae)

The male-produced aggregation pheromone ofDrosophila virilis was found to contain five ester components, in addition to a previously identified hydrocarbon, (Z)-10-heneicosene (Z10–21). The five esters were: the methyl, ethyl, and 1-methylethyl (isopropyl) esters of 2-methyl-(E)-2-butenoic (tiglic) acid and the methyl and ethyl esters of hexanoic acid. The esters were not detected in females. Each ester was active by itself in laboratory bioassay tests, and each increased the number of flies responding toZ10–21 ca. 4–5 times. In comparisons among the five esters at 10 ng per compound, ethyl tiglate was the most active, and methyl tiglate, the least. No mixture of esters was found to be significantly more active than ethyl tiglate alone. In a doseresponse study, bioassay activity increased with dose for both ethyl tiglate andZ10–21. Newly emerged males did not have detectable levels of the esters. All five esters increased as sexual maturity was approached. Ethyl tiglate and ethyl hexanoate were the most abundant in mature males, usually over 15 ng per individual. Ratios among the esters were variable. Male flies also contained an as yet unidentified attractant(s) still more polar than the esters, which was synergistic with the esters and hydrocarbon. Food odors also synergized the synthetic compounds.     

固体超强酸SO_4~(2-)/TiO_2/La~(3+)催化合成己酸乙酯

研究了以固体超强酸 SO2 -/Ti O2 /La3 + 为催化剂 ,己酸和无水乙醇为原料合成己酸乙酯 ,并考察了影响反应的因素。结果表明 ,醇酸比为 2 .0∶ 1 ,催化剂用量为0 .5g(己酸为 0 .2 mol的情况下 ) ,带水剂苯为 1 5m L,反应时间为 2 .0 h是最适宜的反应条件 ,酯化率达 96.8%。     

Effect of eicosapentaenoic acid ethyl ester on proteinuria of streptozotocin-induced diabetes mellitus in rats

Streptozotocin (45 mg/kg) was intravenously administered to 7-week-old Wistar rats through their tail veins. After 11 days, the rats were divided into two groups. One group was fed a lipid-free diet (90%, w/w) plus lard (8%) and safflower oil (2%) for four weeks (Diet 1 group, n=12). The other group was fed in the same way, except that safflower oil was replaced by 90% pure eicosapentaenoic acid (EPA) ethyl ester (Diet 2 group, n=13). Twenty-four-hour urine was collected just before the diets started and during the experiment at 7-day intervals. In the second and third week, the levels of proteinuria were significantly lower in the Diet 2 group than they were in the Diet 1 group. There was no significant difference in the levels of creatinine, urea nitrogen, or lipids in plasma or in body weights between the two groups after four weeks on the diets. Because Diet 2 reduced proteinuria of diabetic rats compared to Diet 1, an EPA-rich diet may retard the development of diabetic nephropathy.     

正己酸二乙氨基乙酯的合成及反应动力学

[目的]以正己酸和二乙氨基乙醇为原料,阳离子交换树脂催化合成正己酸二乙氨基乙酯.考察了反应过程的影响因素,测定了动力学数据.[结果]合成工艺条件,n(正己酸):n(二乙氨基乙醇)为2.0:1,催化剂用量为正己酸和二乙氨基乙醇总质量的2%,甲苯用量为正己酸和二乙氨基乙醇总体积的110%,反应温度不超过130℃,反应时间3.0 h,二乙氨基乙醇的转化率达95.6%,催化剂重复使用4次后,二乙氨基乙醇的转化率为92.8%.表观活化能为73.219 kJ/mol,指前因子为1.9323×107L/(mol·min).[结论]阳离子交换树脂具有较好的催化活性和稳定性,该酯化反应对正己酸和二乙氨基乙醇均为一级反应.     

Synthesis of four chiral pharmaceutical intermediates by biocatalysis

Chiral intermediates were prepared by biocatalytic processes for the chemical synthesis of four pharmaceutical drug candidates. These include: (i) the microbial reduction of 3,5-dioxo-6-(benzyloxy) hexanoic ethyl ester to (3S,5R)-dihydroxy-6-(benzyloxy) hexanoic acid ethyl ester, an intermediate for a new anticholesterol drug; (ii) synthesis of (2R,3S)-(-)-N-benzoyl-3-phenyl isoserine ethyl ester, a taxol side-chain synthon; (iii) the microbial oxygenation of 2,2-dimethyl-2H-1-benzopyran-6-carbonitrile to the corresponding (3S,4S) epoxide and (3S,4R)-trans diol, intermediates for synthesis of potassium channel opener; (iv) the biotransformation of (exo,exo)-7-oxabicyclo [2.2.1] heptane-2,3-dimethanol to the corresponding chiral lactol and lactone, intermediates for thromboxane A₂ antagonist.     

Intake of different eicosapentaenoic acid-containing lipids and fatty acid pattern of plasma lipids in the rats

The ethyl ester of eicosapentaenoic acid (EPA) is the only pure EPA-containing lipid available in bulk for oral administration. However, there is doubt as to whether EPA ethyl ester can efficiently increase the plasma levels of EPA in comparison with the ability of other kinds of EPA-containing lipids to do so. Therefore, two other kinds of EPA-containing lipids were prepared to study the efficiency of oral administration of those lipids for increasing the EPA content in plasma phospholipids and cholesteryl esters. EPA-containing lipids which were investigated were [A], 1,2,3-trieicosapentaenoyl-glycerol, [B] 2-eicosapentaenoyl-phosphatidylcholine and [C] ethyl ester of EPA. An adjusted amount of lipids [A], [B] and [C] was administered to rats through a gastric tube for 4 days (the first experiment) or for 10 days (the second experiment), and the fatty acid composition of plasma phospholipids and cholesteryl esters was determined. In the first experiment, there were no significant differences in the efficiency for increasing EPA levels in either phospholipids or cholesteryl esters among the lipids. In the second experiment, the EPA levels of both plasma phospholipids and cholesteryl esters of rats administered ethyl ester of EPA were significantly higher than those of rats administered 2-eicosapentaenoyl-phosphatidylcholine. The EPA levels of the rats administered 1,2,3-trieicosapentaenoylglycerol were between the levels of the two groups mentioned above, but the differences in the EPA levels were not significant. Although an ethyl ester-type molecule is not a naturally occurring lipid, ethyl ester of EPA is equal to 1,2,3-trieicosapentaenoyl-glycerol and appears to be superior to 2-eicosapentaenoyl-phosphatidylcholine as to the efficiency for increasing EPA levels in total plasma phospholipids and plasma cholesteryl esters.