四氢异喹啉衍生物的合成及体外 抗多子小瓜虫活性的研究

合成四氢异喹啉衍生物并进行杀多子小瓜虫(Ichthyophthirius multifiliis)药效评价。以1-甲基-1,2,3,4-四氢异喹啉为起始原料,在2位的胺基上引入与环己甲酰氯、苯甲酰氯、噻吩甲酰氯、乙酰氯以及氯乙酰氯等不同的酰基进而合成5种四氢异喹啉衍生物(化合物1~化合物5),研究其对小瓜虫掠食体和包囊的杀虫活性,并对杀虫活性物质进行安全性评价。结果显示,5种化合物均具有一定的杀虫活性,其中,化合物1 [(1-甲基-3,4-二氢异喹啉-2(1H)-基)-苯基-甲酮]的杀虫活性最强,其对多子小瓜虫掠食体4 h的100%杀灭浓度为24.0 mg/L,对包囊6 h的100%杀灭浓度为60.0 mg/L,对掠食体的半数致死浓度(LD50)为16.4 mg/L。急性毒性实验结果显示,化合物1对翘嘴红鲌(Erythroculter ilishaeformi)的48 h LD50为234.3 mg/L,其安全浓度为64.1 mg/L。研究表明,化合物1 [(1-甲基-3,4-二氢异喹啉-2(1H)-基)-苯基-甲酮]是一种具有较好开发前景的杀小瓜虫药物。     

Bactericidal and fungicidal activity of Aspergillus ochraceus metabolites and some derivatives

The bactericidal and fungicidal activities of aspyrone and asperlactone, secondary metabolites of Aspergillus ochraceus, and some aspyrone derivatives were studied. In general, aspyrone exhibited better activity than asperlactone or aspyrone derivatives. The inhibition patterns of the assayed compounds were different. Helminthosporium monoceras was the tested mould most inhibited by the studied compounds. The comparative study of the activity of the different compounds showed that the epoxy group seems to be necessary for activity against some micro-organisms. © 1998 SCI     

寡聚酸碘抑制TMV活性测定及对番茄生长影响初探

为研究新型壳寡糖衍生物类农用制剂寡聚酸碘(寡聚N-乙酰基-D-氨基葡萄糖醛酸碘)对烟草花叶病毒(TMV)的抑制作用及对番茄生长、生理特性的影响,以番茄品种:L402、贝鲁特、粉多利作为供试材料,以氨基寡糖素及50%腐霉利L可湿粉剂作为对比,通过室内生测试验试验,测定寡聚酸碘对番茄病毒病中常见病原菌TMV的抑制效果、对番茄生长及及番茄幼苗茎尖中吲哚乙酸、赤霉素及叶绿素含量的影响。寡聚酸碘对TMV的抑制效果表现出良好的速效性和持效性,接种后17d,抑制效果从45.08%迅速提升到74.48%,接种21~35d,对TMV的抑制效果维持在80%以上。寡聚酸碘对TMV的EC50值为15.62mg/L,对TMV的抑制活性高于3%氨基寡糖素水剂寡聚酸碘处理,有效成分300.0mg/L的寡聚酸碘可作为抑制TMV活性的最优供试剂量;寡聚酸碘在300~1 200mg/L处理剂量下,对供试的3个番茄品种(L402、贝鲁特、粉多利)安全,未见任何药害症状,与CK、3%氨基寡糖素及50%腐霉利L可湿粉剂相比,可以明显提升番茄幼苗株高、茎尖内IAA、GA含量及叶片中总叶绿素含量。寡聚酸碘处理的番茄茎秆粗壮,叶色浓绿,生长性状良好。因此,寡聚酸碘具有抑制TMV活性及促进番茄生长的双重功效,开发利用前景良好。     

苯甲酰胺类磷酸二酯酶-4抑制剂的设计与合成

目的 合成6个苯甲酰胺类磷酸二酯酶-4抑制剂。方法 以异香兰素为原料,经过成醚反应、氧化反应、Schotten-Baumann反应等制备目标化合物。结果 成功制备了6个目标化合物：Benzoic acid,4-[[3-（isobutoxy）-4-methoxybenzoyl]amino]（T1）,Benzamide,4-[[3-（isobutoxy）-4-methoxybenzoyl]amino]（T2）,Benzamide,4-（isobutoxy）-3-methoxy-N-[4-[[（1-methylethyl）amino]sulfonyl]phenyl]（T3）,Benzoicacid,4-[[3-（cyclopentyloxy）-4-methoxybenzoyl]amino]（T4）,Benzamide,4-[[3-（cyclopentyloxy）-4-methoxybenzoyl]amino]（T5）,Benzamide,4-（cyclopentyloxy）-3-methoxy-N-[4-[[（1-methylethyl）amino]sulfonyl]phenyl]（T6）,收率分别为66.7%、65.7%、18.4%、46.7%、76.8%和12.4%,其中化合物T1、T2、T3、T5、T6为新化合物。结论 所得产物的化学结构经¹H-NMR、MS谱确证,与目标化合物相符。     

Rare Chromones from a Fungal Mutant of the Marine-Derived Penicillium purpurogenum G59

Three new and rare chromones, named epiremisporine B (2), epiremisporine B1 (3) and isoconiochaetone C (4), along with three known remisporine B (1), coniochaetone A (5) and methyl 8-hydroxy-6-methyl-9-oxo-9H-xanthene-1-carboxylate (6) were isolated from a mutant from the diethyl sulfate (DES) mutagenesis of a marine-derived Penicillium purpurogenum G59. The structures of 2–4 including the absolute configurations were determined by spectroscopic methods, especially by NMR analysis and electronic circular dichroism (ECD) experiments in conjunction with calculations. The absolute configuration of the known remisporine B (1) was determined for the first time. Compounds 2 and 3 have a rare feature that has only been reported in one example so far. The compounds 1–6 were evaluated for their cytotoxicity against several human cancer cell lines. The present work explored the great potential of our previous DES mutagenesis strategy for activating silent fungal pathways, which has accelerated the discovery of new bioactive compounds.     

丙酸镁对西门塔尔牛尿嘌呤衍生物和微生物蛋白的影响

选用4头年龄3.5岁,体况良好,体重500kg的中国西门塔尔牛阉牛。采用4×4拉丁方设计,研究日粮添加丙酸镁(100g/d)、丙酸(87g/d)和氧化镁(24g/d)对尿嘌呤衍生物(PD)和微生物蛋白(MCP)的影响。结果表明:日粮中添加丙酸镁、丙酸和氧化镁后,丙酸镁组和丙酸组尿囊素、PD、微生物氮(MN)、MCP较对照组和氧化镁组显著提高(P<0.05),但丙酸镁组和丙酸组差异不显著(P>0.05)。日粮添加丙酸镁、丙酸和氧化镁对尿酸(uric acid)含量无显著影响(P>0.05)。日粮中添加丙酸镁和丙酸提高了尿囊素含量和PD、MN和MCP产量,但处理对尿酸没有影响。     

人参皂苷及其衍生物抗马立克病病毒作用的超微结构和病理变化观察

为了探讨人参皂苷及其衍生物抗马立克氏病病毒的作用机制.采用马立克氏病毒感染的雏鸡作为模型,人参皂苷及其衍生物口服给药途径,动态观察不同时间段,试验鸡的器官病理变化和脾脏、法氏囊的组织超微结构改变.结果发现人参皂苷及其衍生物组的器官病变程度明显低于病毒对照组,法氏囊和脾脏的超微结构病变轻于病毒对照组,说明人参皂苷及其衍生物在体内可以通过保护机体免疫器官来发挥抗病毒作用.     

Synthesis and Antitumor Activities of Derivatives of the Marine Mangrove Fungal Metabolite Deoxybostrycin

Deoxybostrycin (1) is an anthraquinone compound derived from the marine mangrove fungus Nigrospora sp. No. 1403 and has potential to be a lead for new drugs because of its various biological properties. A series of new derivatives (2–22) of deoxybostrycin were synthesized. The in vitro cytotoxicity of all the new compounds was tested against MDA-MB-435, HepG2 and HCT-116 cancer cell lines. Most of the compounds exhibit strong cytotoxicity with IC₅₀ values ranging from 0.62 to 10 μM. Compounds 19, 21 display comparable cytotoxicity against MDA-MB-435 to epirubicin, the positive control. The primary screening results indicate that the deoxybostrycin derivatives might be a valuable source of new potent anticancer drug candidates.