油橄榄羟基酪醇的生物合成及其衍生物研究进展

介绍了传统化学合成羟基酪醇的方法,针对化学合成反应步骤多、催化剂昂贵、产率低、污染大等问题,重点总结了以橄榄苦苷和酪醇为原料生物法合成羟基酪醇的途径,同时还综述了羟基酪醇烷基醚、脂肪酸酯、糖基化等衍生物的制备方法、生物活性及其构效关系,为羟基酪醇及其衍生物批量制备及其抗肿瘤、抗癌、心脑血管疾病新药的筛选提供参考和指导作用。     

塔拉提取物化学利用的研究进展

塔拉是富含没食子单宁的主要植物资料之一。本文从其自然资源、塔拉提了化学及其加工利用等几方面的研究进展作了综述。指出塔拉的工业开发利用将会有进一步的发展。     

Synthesis and Evaluation of Some New Aza-B-homocholestane Derivatives as Anticancer Agents

Using analogues of some marine steroidal oximes as precursors, a series of aza-B-homocholestane derivatives possessing different substituted groups at the 3-position of the steroidal nucleus were synthesized. Their biological activity against cancer cell proliferation was determined with multiple cancer cell lines. Aza-B-homocholestane derivatives possessing 3-hydroxyl, 3-hydroximino and 3-thiosemicarbazone groups displayed remarkable cytotoxicity to cancer cells via apoptosis inducing mechanism. Compounds 5, 10, 12, 15 and 18 exhibited better potency to inhibit cancer cell proliferation. In addition, compound 15 was further evaluated with three dimensional (3D) multicellular spheroids assay to determine its potency against spheroid growth. The structure-activity relationship (SAR) generated in the studies is valuable for the design of novel chemotherapeutic agents.     

壳聚糖的生产与应用

近年来,壳聚糖及其衍生物的开发应用受到国内外的重视,越来越多的产品从实验室走向市场。介绍了壳聚糖及其衍生物的制备方法及其在工业、农业、医药、环保、生物学等领域的应用。     

魔芋不同繁殖材料田间生理指标研究初报

尿液嘌呤衍生物法作为一种估测瘤胃微生物蛋白质合成量的新方法,克服了原有方法的缺点,简单易行,通过欧洲牛羊的实验证明该方法与其它方法的测定结果有很好的一致性,但此方法亦有其不足。由于尿中嘌呤衍生物排出量受动物品种的影响很大,不同品种间无通用性,所以现有的研究成果不能用于中国品种牛,更难以使该方法应用于生产。而国内在此方面的报道很有限,所以急需建立各品种反刍动物的估测模型,扩大该方法的应用范围。试验采用3头月龄(22±0.2),体重为(641±26.889)kg,体况相近的中国荷斯坦成年公牛,设计3×3的拉丁方,通过调整日粮精粗比来考察可消化有机物进食量对中国荷斯坦成年公牛尿嘌呤衍生物(PD)排出的影响。结果发现,试验牛尿中嘌呤衍生物中尿囊素大约为73%￣88%,黄嘌呤和次黄嘌呤的含量很小,可以忽略不计,与以往对成年反刍动物的研究结果相似,与同个体犊牛期的研究结果相反。PD的排出量随可消化有机物(DOMI)和可消化粗蛋白(DCP)进食量升高而上升,存在较强的相关性(R2=0.88,n=9),其排出水平为414.09￣975.59mmol/d。肌酐酸的排出较稳定,各处理间差异不显著(P>0.05)。PDC与DOM和DCP进食量存在正相关,这与以往成年反刍动物的研究结果是相似的,与同个体犊牛期的研究结果相反,但相关性较弱。     

姜黄素嘧啶酮衍生物的合成及杀螨活性

在明确姜黄素具有杀螨活性,且其结构中的双羰基并非是起杀螨作用的关键基团的基础上,设计、合成了4个新颖的姜黄素嘧啶酮衍生物,其结构经红外光谱、核磁共振氢谱和质谱分析确认。生物活性测定结果表明:4个目标化合物均表现出优于母体化合物姜黄素的杀螨活性,处理48 h后,活性最好的4,6-二 -2-嘧啶酮(3a)对朱砂叶螨Tetranychus cinnabarinus和柑橘全爪螨Panoychus cotri的LC50值分别为487.5和200.3 mg/L,其毒力约为姜黄素的4倍;而处理72 h后,化合物 3a 对朱砂叶螨的LC50值为40.7 mg/L,其毒力约为姜黄素的14倍。     

槲皮素单硫酸酯和5’-氯-5’-脱氧腺苷单用与合用对凝血酶诱导兔血小板聚集的影响

目的：研究槲皮素单硫酸酯和5’-氨-5’-脱氧腺苷合用对凝血酶诱导兔血小板聚集的影响。方法：用比浊法检测血小板聚集。结果：槲皮素单硫酸酯和5’-氨-5’-脱氧腺苷对凝血酶诱导的兔血小板聚集都有抑制作用，两者合用作用增加。结论：槲皮素单硫酸酯与5’-氨-5’-脱氧腺苷具有协同抗血小板聚集的作用。     

魔芋葡甘露聚糖及其衍生物在食品工业中的应用

魔芋葡甘露聚糖作为一种传统的食品原料和食品添加剂,近年来在食品领域的应用研究日益引人注目。魔芋葡甘露聚糖是一种中性多糖,是魔芋的主要功能活性成分。魔芋葡甘露聚糖及其衍生物具有较好的凝胶性、增稠性、成膜性等功能特性,在食品工业中具有很高的研究开发和实际应用价值。本文综述了魔芋葡甘露聚糖及其衍生物的主要功能特性及其在食品工业中的应用,将为充分利用我国魔芋资源、提高其产品附加值开辟广阔的发展空间。     

青蒿内生真菌IS928产青蒿素类化合物的发酵培养基优化

[目的]为了开发青蒿素类化合物新的生产方法。[方法]从青蒿中分离出一株产青蒿素类化合物的内生真菌IS928,采用单因素试验法研究了液态发酵生产青蒿素类化合物合适的培养基,包括碳源、氮源、无机盐等对其产量的影响,并采用响应面法对发酵培养基进行了优化。[结果]适宜培养基配方为:蔗糖3.15%,酵母粉2.27%,KH_2PO_40.254%,MgSO_4·7H_2O0.173%,NaCl0.05%,得到青蒿素类化合物产量平均值为17.19 mg/L。[结论]该研究为青蒿素类化合物发酵生产的研究提供了理论基础。     

Insecticidal and fungicidal activity of new synthesized chitosan derivatives

Chitosan, the N-deacetylated derivative of chitin, is a potential biopolysaccharide owing to its specific structure and properties. In this paper, we report on the synthesis of 24 new chitosan derivatives, N-alkyl chitosans (NAC) and N-benzyl chitosans (NBC), that are soluble in dilute aqueous acetic acid. The different derivatives were synthesized by reductive amination and analyzed by 1H NMR spectroscopy. A high degree of substitution (DS) was obtained with N-(butyl)chitosan (DS 0.36) at a 1:1 mole ratio for NAC derivatives and N-(2,4-dichlorobenzyl)chitosan (DS 0.52) for NBC derivatives. Their insecticidal and fungicidal activities were tested against larvae of the cotton leafworm Spodoptera littoralis (Boisduval) (Lepidoptera: Noctuidae), the grey mould Botrytis cinerea Pers (Leotiales: Sclerotiniaceae) and the rice leaf blast Pyricularia grisea Cavara (Teleomorph: Magnaporthe grisea (Hebert) Barr). The oral feeding bioassay indicated that all the derivatives had significant insecticidal activity at 5 g kg(-1) in artificial diet. The most active was N-(2-chloro-6-fluorobenzyl)chitosan, which caused 100% mortality at 0.625 g kg(-1), with an estimated LC50 of 0.32 g kg(-1). Treated larvae ceased feeding after 2-3 days; the mechanism of action remains unknown. In a radial hyphal growth bioassay with both plant pathogens, all derivatives showed a higher fungicidal action than chitosan. N-Dodecylchitosan, N-(p-isopropylbenzyl)chitosan and N-(2,6-dichlorobenzyl)chitosan were the most active against B cinerea, with EC50 values of 0.57, 0.57 and 0.52 g litre(-1), respectively. Against P grisea, N-(m-nitrobenzyl)chitosan was the most active, with 77% inhibition at 5 g litre(-1). The effect of different substitutions is discussed in relation to insecticidal and fungicidal activity.