Approaches to Configuration Determinations of Flexible Marine Natural Products: Advances and Prospects

Flexible marine natural products (MNPs), such as eribulin and bryostatin, play an important role in the development of modern marine drugs. However, due to the multiple chiral centers and geometrical uncertainty of flexible systems, configuration determinations of flexible MNPs face great challenges, which, in turn, have led to obstacles in druggability research. To resolve this issue, the comprehensive use of multiple methods is necessary. Additionally, configuration assignment methods, such as X-ray single-crystal diffraction (crystalline derivatives, crystallization chaperones, and crystalline sponges), NMR-based methods (JBCA and Mosher’s method), circular dichroism-based methods (ECCD and ICD), quantum computational chemistry-based methods (NMR calculations, ECD calculations, and VCD calculations), and chemical transformation-based methods should be summarized. This paper reviews the basic principles, characteristics, and applicability of the methods mentioned above as well as application examples to broaden the research and applications of these methods and to provide a reference for the configuration determinations of flexible MNPs.     

The Impact of Natural Deep Eutectic Solvents and Extraction Method on the Co-Extraction of Trace Metals from Fucus vesiculosus

In recent years, natural deep eutectic solvents (NADES) have been widely investigated for the extraction of food and medicinal plants as well as seaweeds. However, the ability of NADES for trace elements co-extraction from natural sources is not well investigated. The aim of this study was to investigate the ability of common NADES for trace elements co-extraction from Fucus vesiculosus. All of the tested NADES did not recover As and Co (concentration <LOQ). Moreover, all of the tested NADES provided a low recovery (<9%) of Ba, Ca, Fe, Mg, Mn, Sr, and Zn. The method of extraction had not shown a statistically significant effect on the co-extraction of all elements (excluding Ba and Ca). In contrast, the water content in NADES was significantly affected on the recovery of Ba, Ca, Mg, Mn, Sr, and Zn. The recovery of Al and Cr was relatively high and considerably varied (from 1.5 to 59.9%). NADES comprising lactic acid:glucose:H₂O (5:3:1) provided the lowest contents of all elements, and the highest extracted amounts were obtained employing water contents of 60–80%. The calculated daily intake of all the elements contained in NADES extracts were less than the daily dose risk estimators. The hazard quotients, hazard indexes, and carcinogenic risk calculated for all trace elements and their combination were considerably less than 1. This evidences no health risk, and carcinogenic risk after topical application of all studied NADES. For the first time, the results of the current study demonstrated that NADES extracts of F. vesiculosus contain a lower amount of trace metals and are safer than the extracts obtained with water and 70% acetone. This indicates a significant advantage for NADES compared with the other solvents.     

Natural Marine Products: Anti-Colorectal Cancer In Vitro and In Vivo

Colorectal cancer, a malignant tumor with high mortality, has a poor prognosis due to drug resistance and toxicity in clinical surgery and chemotherapy. Thus, finding safer and more efficient drugs for clinical trials is vital and urgent. Natural marine compounds, with rich resources and original chemical structures, are applied widely in anticancer treatments. We provide a systematic overview of recently reported marine compounds such as alkaloids, peptides, terpenoids, polysaccharides, and carotenoids from in vitro, in vivo, and clinical studies. The in vitro studies summarized the marine origins and pharmacological mechanisms, including anti-proliferation, anti-angiogenesis, anti-migration, anti-invasion, the acceleration of cycle arrest, and the promotion of tumor apoptosis, of various compounds. The in vivo studies outlined the antitumor effects of marine compounds on colorectal cancer model mice and evaluated their efficacy in terms of tumor inhibition, hepatotoxicity, and nephrotoxicity. The clinical studies summarized the major chemical classifications and targets of action of the clinical drugs that have entered clinical approval and completed approval for marine anticancer. In summary, we present the current situation regarding the application of natural anti-colorectal cancer marine compounds and prospects for their clinical application.     

Recent Advances in the Synthesis of Marine-Derived Alkaloids via Enzymatic Reactions

Alkaloids are a large and structurally diverse group of marine-derived natural products. Most marine-derived alkaloids are biologically active and show promising applications in modern (agro)chemical, pharmaceutical, and fine chemical industries. Different approaches have been established to access these marine-derived alkaloids. Among these employed methods, biotechnological approaches, namely, (chemo)enzymatic synthesis, have significant potential for playing a central role in alkaloid production on an industrial scale. In this review, we discuss research progress on marine-derived alkaloid synthesis via enzymatic reactions and note the advantages and disadvantages of their applications for industrial production, as well as green chemistry for marine natural product research.     

不同温度下的豌豆蚜实验种群生命表研究

在6种温度(12、15、18、21、24℃和27℃)和相对湿度为80%的条件下,研究了温度对豌豆蚜发育和增殖的影响。组建了生命表,并统计出种群内禀增长率、净增殖率、世代平均周期、种群加倍时间和周限增长率等种群动态参数。结果表明,在试验温度范围内,豌豆蚜的发育历期随温度升高而缩短。种群的内禀增长率在24℃条件下最大(rm=0.281 0),相应的种群净增殖率(R0)、周限增长率(λ)、平均世代周期(T)和种群加倍时间(t)分别为17.030 9、1.324 5、10.089 3 d和2.466 7 d。     

基于综合承载力的区域适度人口研究

在可持续发展目标条件下,适度人口取决于生态、经济和土地等多要素的综合承载力。本文探讨了适度人口的计算方法和模型,运用该模型对吉林省1978-2002年的适度人口进行了测算,并对结果进行了分析,探讨其形成原因,提出解决对策。但适度人口是动态的,是生产力的函数,土地承载是基础,经济承载是关键,生态承载是限制,本文未曾寻求到既能提高区域适度人口数量,又不对区域生态系统产生破坏与影响的土地、经济和生态承载人口三者之间的动态平衡临界点,这是今后努力的方向。     

天山北坡经济带人口分布与经济发展研究

人口分布是影响经济发展的重要因素。人口分布与经济分布的最基本属性是不均衡性,人口与经济的空间集中化是区域发展的内在规律。本文从人口与经济发展的关系出发,通过对天山北坡经济带人口数量、人口密度、人口分布等因素与经济发展相关关系及动态演进的多方面分析,为天山北坡经济带进一步实施人口与经济空间集中化战略,建立起人口、经济与环境协调发展的区域格局提供一些理论依据与对策。     

番茄褪绿病毒病在山东设施西葫芦上的发生及潜在危害

番茄褪绿病毒tomato chlorosis virus (ToCV)是我国蔬菜生产的重要新发病毒,其寄主范围逐年扩大。2019年10月项目组在山东寿光西葫芦温室调查时发现部分叶片呈现黄化、脉间褪绿,类似于ToCV侵染症状,并伴有烟粉虱发生。利用特异性引物检测发现,扩增的目的片段与GenBank中登录的侵染番茄的ToCV基因序列(登录号：KC887998.1)同源性高达99.58%,充分说明西葫芦植株已被ToCV侵染。通过对病毒病发生规律和烟粉虱虫口数量调查发现,西葫芦定植后1个月表现侵染症状的植株为2.0%,定植后2个月达到4.2%,定植后4个月后高达68.2%,病毒发生呈指数增长,而烟粉虱虫口数量却维持较低密度。从济南和德州采集的西葫芦疑似病叶和烟粉虱中也检出ToCV病毒,说明该病毒可能已经在山东省设施西葫芦主要种植区普遍发生,并经烟粉虱广泛传播,需引起高度重视。     

三种增效剂对棉铃虫增效作用

用３个不同地区的棉铃虫田间种群分别测定了３种增效剂对３种杀虫剂的增效作用。结果表明ＰＢ对氯氟氰菊酯,ＤＥＦ对辛硫磷,ＰＢ和ＴＰＰ对灭多威增效较好,而且棉铃虫的抗性水平越高,增效剂的增效作用越突出。     

不同温度下东方粘虫年龄-阶段两性实验种群生命表的构建

为明确不同温度对东方粘虫Mythimna separata(Walker)种群动态的影响,建立东方粘虫种群动态模型,利用年龄-阶段两性种群生命表得到了室内不同温度下东方粘虫种群的发育历期、存活率、繁殖力和种群生命表参数,并基于种群生命表参数预测了2个月内东方粘虫的种群动态。结果表明,东方粘虫各虫态的发育历期和产卵前期随温度的升高而显著缩短。24℃下,东方粘虫单雌平均产卵量为717.1粒,显著高于其它温度下;成虫寿命也显著高于其它温度下,且雄蛾寿命显著长于雌蛾,分别为15.3 d和13.0 d;卵孵化存活到成虫的概率、幼虫存活率和化蛹率均最高,分别为66.7%、68.9%和96.8%。内禀增长率随温度的升高而显著增加,平均世代周期则显著降低,18、21、24、27、30℃下分别为0.051、0.077、0.113、0.121、0.156 d-1和77.2、61.3、49.0、40.3、31.5 d;周限增长率也随温度的升高而增加,分别为1.05、1.08、1.12、1.13、1.17 d-1;净增殖率在24℃下为257.1,显著高于其它温度下,其它温度条件下无显著差异。表明东方粘虫在18~30℃范围内都能完成生长发育和生殖,24℃下种群存活率高、繁殖力大、世代周期较短,更适合种群增长。