不同环丙烯类乙烯抑制剂对苹果常温贮藏保鲜效果的影响

为了研究不同支链长度的3种环丙烯类乙烯抑制剂处理对寒富苹果常温贮藏效果的影响,分别采用0.75μL/L1-MCP(1-甲基环丙烯),2μL/L1-PentCP(1-pentylcclopropene,1-戊基环丙烯)和0.5μL/L1-OCP(1-octylcyclopropene,1-辛基环丙烯)在常温条件下,熏蒸处理寒富苹果20h,以不处理为对照,处理后装入厚度0.02mm保鲜袋于常温下贮藏(20℃)。结果表明:1-MCP和1-PentCP处理能较好地抑制寒富苹果贮藏过程中的呼吸强度和乙烯释放量,各处理呼吸高峰时间较对照晚出现了4d,各处理对乙烯释放高峰出现的时间延迟了8d,较好地保持了果实贮藏期间的硬度,延缓了果实固形物含量和丙二醛含量的上升速度。这2个处理还在一定程度上延缓了细胞膜保护酶过氧化物酶、超氧化物歧化酶和过氧化氢酶的活性变化。而1-OCP处理却促进了寒富苹果果实贮藏期间的丙二醛含量的上升,进而导致在贮藏后期出现了一定的伤害作用。研究结果表明,1-MCP和1-PentCP处理可以抑制寒富苹果的生理代谢,保持果实品质和降低膜脂伤害程度,从而延缓寒富苹果采后的成熟衰老进程。     

Suicidal germination for parasitic weed control

Parasitic weeds of the genera Striga and Orobanche spp. cause severe yield losses in agriculture, especially in developing countries and the Mediterranean. Seeds of these weeds germinate by a chemical signal exuded by the roots of host plants. The radicle thus produced attaches to the root of the host plant, which can then supply nutrients to the parasite. There is an urgent need to control these weeds to ensure better agricultural production. The naturally occurring chemical signals are strigolactones (SLs), e.g. strigol and orobanchol. One option to control these weeds involves the use of SLs as suicidal germination agents, where germination takes place in the absence of a host. Owing to the lack of nutrients, the germinated seeds will die. The structure of natural SLs is too complex to allow multigram synthesis. Therefore, SL analogues are developed for this purpose. Examples are GR24 and Nijmegen‐1. In this paper, the SL analogues Nijmegen‐1 and Nijmegen‐1 Me were applied in the field as suicidal germination agents. Both SL analogues were formulated using an appropriate EC‐approved emulsifier (polyoxyethylene sorbitol hexaoleate) and applied to tobacco (Nicotiana tabacum L.) fields infested by Orobanche ramosa L. (hemp broomrape), following a strict protocol. Four out of 12 trials showed a reduction in broomrape of ≥95%, two trials were negative, two showed a moderate result, one was unclear and in three cases there was no Orobanche problem in the year of the trials. The trial plots were ca 2000 m²; half of that area was treated with stimulant emulsion, the other half was not treated. The optimal amount of stimulant was 6.25 g ha^?1. A preconditioning prior to the treatment was a prerequisite for a successful trial. In conclusion, the suicidal germination approach to reducing O. ramosa in tobacco fields using formulated SL analogues was successful. Two other options for weed control are discussed: deactivation of stimulants prior to action and biocontrol by Fusarium oxysporum. © 2016 Society of Chemical Industry     

Design,Synthesis and Evaluation of New Marine Alkaloid-Derived Pentacyclic Structures with Anti-Tumoral Potency

This work describes the synthesis and biological evaluation of a new heterocyclic hybrid derived from the ellipticine and the marine alkaloid makaluvamine A. Pyridoquinoxalinedione 12 was obtained in seven steps with 6.5% overall yield. 12 and its intermediates 1–11 were evaluated for their in vitro cytotoxic activity against different cancer cell lines and tested for their inhibitory activity against the human DNA topoisomerase II. The analysis by electrophoresis shows that the pentacycle 12 inhibits the topoisomerase II like doxorubicine at 100 µM. Compound 9 was found to have an interesting profile, having a cytotoxicity of 15, 15, 15 and 10 μM against Caco-2, HCT-116, Pc-3 and NCI cell lines respectively, without any noticeable toxicity against human fibroblast.     

3-[4-(1H-Indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines,Nortopsentin Analogues with Antiproliferative Activity

A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) having GI₅₀ values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunction. Moreover, the compounds induced a concentration-dependent accumulation of cells in the subG0/G1phase, while confined viable cells in G2/M phase.     

假柴龙树属植物资源的开发利用与喜树碱及类似物的生产综述

对假柴龙树属植物的生物学特征及产生的主要喜树碱类物质进行了介绍,着重论述了利用臭味假柴龙树产生喜树碱及类似物的研究,并就假柴龙树属植物资源的利用和开发作进一步的展望。     

1-(2-酰氧基-4,5-亚甲二氧基)苯基-2-甲基丙烯酮类化合物的合成及抑菌活性

以具有较高抑菌活性的卡枯醇衍生物1-(2-羟基-4,5-亚甲二氧基)苯基-2-甲基丙烯酮为原料,设计合成了14个未见文献报道的1-(2-酰氧基-4,5-亚甲二氧基)苯基-2-甲基丙烯酮类(2a～2n)化合物,其结构经电喷雾串联质谱(ESI-MS)和核磁共振氢谱确证。初步生物活性测试结果表明,在100 mg/L下,目标化合物对5种供试病原菌均具有较高的抑菌活性,其中, 2b和2d 对番茄灰霉病菌Botrytis cinerea和小麦赤霉病菌Fusarium graminearum的抑制率达100%。     

保幼激素类似物ZR─512对中蜂蜂王发育调控作用的研究

用保幼激素类似物ＺＲ─５１２滴注于王台内蜂王浆中的方法，研究ＺＲ─５１２对中蜂蜂王发育的调控作用。试验结果表明：ＺＲ─５１２能够显著地延长蜂王幼虫取食期，促使蜂王在胚后发育阶段超常发育，为在养蜂生产上培育优质蜂王提出了新的方法。     

促性腺激素释放激素及其类似物在母猪繁殖中应用的研究进展

促性腺激素释放激素(gonadotropin-releasing hormone,GnRH))是下丘脑分泌的生殖激素,主要通过下丘脑-垂体-性腺轴参与调控动物的生殖活动,也可直接作用于性腺或其他器官发挥重要功能。哺乳动物的GnRH具有相同的十肽结构,通过改变十肽结构中第六、九、十位氨基酸可合成不同的GnRH类似物。GnRH及其类似物可通过刺激促黄体素(LH)分泌、抑制雌激素受体二聚化及调节胚胎附植期相关蛋白质的合成来影响动物的繁殖性能。GnRH及其类似物已被证明可提高猪的繁殖力。在母猪生产中,GnRH类似物的应用仍存在受胎次影响、促进排卵但不能增加产仔数等问题。文章主要从GnRH的来源与功能、GnRH及其类似物的结构、GnRH受体(GnRHR)的结构与功能、GnRH及其类似物对母猪繁殖性能的影响,以及存在的问题与展望五方面介绍了GnRH及其类似物在母猪繁殖中的应用研究进展。     

鬼臼毒素类似物结构与杀虫活性关系初探Ⅰ.几种衍生物的合成及杀虫活性测试

以鬼臼毒素为原料合成了几种衍生物 ,用质谱和核磁共振鉴定了其结构。以5龄菜青虫 (Pieris rapae)、3龄小菜蛾 (Plutella xylostella)和 3龄粘虫 (Mythimna separataWalker)为试虫 ,测定了其生物活性。结果表明 ,鬼臼毒素类似物对菜青虫表现出明显的结构与活性规律。母体的几种异构体中 ,鬼臼毒素的活性最强 ;4′位为甲氧基的衍生物较 4’位为羟基的活性要高 ;内酯环打开的衍生物活性降低。     

1-（2-羟基-4,5-亚甲二氧基）苯基-2-甲基丙烯酮类化合物的合成及抑菌活性

【目的】研究卡枯醇衍生物的抑菌活性,旨在探索其抑菌活性与构效关系。【方法】首先以芝麻酚、α-甲基丙烯酰氯为原料,通过傅克酰基化合成具有较高抑菌活性的卡枯醇衍生物,即化合物1（1-（2-羟基-4,5-亚甲二氧基）苯基-2-甲基丙烯酮）,然后经醚化反应合成了8个目标化合物2a～2h, 采用核磁共振仪（¹H-NMR、¹³C-NMR）和质谱仪（ESI-MS）对化合物的结构进行了表征;最后采用生长速率法测定了化合物2a～2h对小麦赤霉病菌、番茄灰霉病菌、黄瓜炭疽病菌、马铃薯干腐病菌、水稻稻瘟病菌的抑菌活性。【结果】合成了8个1-（2-羟基-4,5-亚甲二氧基）苯基-2-甲基丙烯酮类化合物,其结构经¹H-NMR、¹³C-NMR和ESI-MS予以了确认。抑菌活性测定结果表明,在质量浓度为100 mg/L时,8种化合物对5种供试病原菌均有较高的抑菌活性,化合物2a、2b、2c和2f对供试菌种的菌丝生长抑制率均较高,其中对供试菌小麦赤霉病菌、番茄灰霉病菌的菌丝生长抑制率均基本达到了100.0%。此外,2a、2b、2c和2f对黄瓜炭疽病菌的菌丝生长抑制率均高于噻菌灵。【结论】合成的8个化合物对5种供试病原菌均有较高的抑菌活性,对部分菌种的菌丝生长抑制率高于噻菌灵原药。