Aaptamine Derivatives with Antifungal and Anti-HIV-1 Activities from the South China Sea Sponge Aaptos aaptos

Five new alkaloids of aaptamine family, compounds (1–5) and three known derivatives (6–8), have been isolated from the South China Sea sponge Aaptos aaptos. The structures of all compounds were unambiguously elucidated by spectroscopic analyses, as well as by comparison with the literature data. Compounds 1–2 are characterized with triazapyrene lactam skeleton, whereas compounds 4–5 share an imidazole-fused aaptamine moiety. These compounds were evaluated in antifungal and anti-HIV-1 assays. Compounds 3, 7, and 8 showed antifungal activity against six fungi, with MIC values in the range of 4 to 64 μg/mL. Compounds 7–8 exhibited anti-HIV-1 activity, with inhibitory rates of 88.0% and 72.3%, respectively, at a concentration of 10 μM.     

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.     

Tipping Points in Seaweed Genetic Engineering: Scaling Up Opportunities in the Next Decade

Seaweed genetic engineering is a transgenic expression system with unique features compared with those of heterotrophic prokaryotes and higher plants. This study discusses several newly sequenced seaweed nuclear genomes and the necessity that research on vector design should consider endogenous promoters, codon optimization, and gene copy number. Seaweed viruses and artificial transposons can be applied as transformation methods after acquiring a comprehensive understanding of the mechanism of viral infections in seaweeds and transposon patterns in seaweed genomes. After cultivating transgenic algal cells and tissues in a photobioreactor, a biosafety assessment of genetically modified (GM) seaweeds must be conducted before open-sea application. We propose a set of programs for the evaluation of gene flow from GM seaweeds to local/geographical environments. The effective implementation of such programs requires fundamentally systematic and interdisciplinary studies on algal physiology and genetics, marine hydrology, reproductive biology, and ecology.     

Two New Cytotoxic Indole Alkaloids from a Deep-Sea Sediment Derived Metagenomic Clone

Two new indole alkaloids, metagenetriindole A (1) and metagenebiindole A (2), were identified from deep-sea sediment metagenomic clone derived Escherichia coli fermentation broth. The structures of new compounds were elucidated by spectroscopic methods. The two new indole alkaloids demonstrated moderately cytotoxic activity against CNE2, Bel7402 and HT1080 cancer cell lines in vitro.     

Bis(2,3-dibromo-4,5-dihydroxybenzyl) Ether,a Marine Algae Derived Bromophenol,Inhibits the Growth of Botrytis cinerea and Interacts with DNA Molecules

Bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (BDDE) is a bromophenol isolated from marine algae. Previous reports have shown that BDDE possesses cytotoxic and antibacterial activity. In the present study, we demonstrate that BDDE displays broad-spectrum antifungal activities, especially on Botrytis cinerea. BDDE inhibits the growth of B. cinerea cultured on a solid medium of potato dextrose agar (PDA) as well as on the potato dextrose broth (PDB) medium. Moreover, BDDE decreases the incidence of fruit decay and severity of strawberries infected with B. cinerea. Further studies have revealed that BDDE decreases the germination rate and inhibits the mycelial growth of B. cinerea. The inhibition mechanisms are related to the disruption of the cell membrane integrity in B. cinerea spores and newly formed germ tubes. This study also suggests that BDDE possibly interacts with DNA via intercalation and minor groove binding. The studies provide evidence that BDDE has potential application in the control of gray mold after fruit harvest and the compound could serve as a candidate or lead template for rational drug design and for the development of antifungal agents.     

Punctaporonins H–M: Caryophyllene-Type Sesquiterpenoids from the Sponge-Associated Fungus Hansfordia sinuosae

Six new caryophyllene-based sesquiterpenoids named punctaporonins H–M (1–6), together with punctaporonin B (7) and humulane (8) were isolated from the fermentation broth of the sponge-derived fungus Hansfordia sinuosae. Their structures were determined by the extensive HRESIMS and NMR spectroscopic analysis, including the X-ray crystallographic data for the assignment of the absolute configurations of punctaporonins H–I (1–2). The isolated compounds were evaluated for antihyperlipidemic, cytotoxic and antimicrobial activities, and punctaporonin K (4) exhibited potent effects to reduce the triglycerides and total cholesterol in the intracellular levels.     

Relative and Absolute Stereochemistry of Diacarperoxides: Antimalarial Norditerpene Endoperoxides from Marine Sponge Diacarnus megaspinorhabdosa

Five new norditerpene endoperoxides, named diacarperoxides H–L (1–5), and a new norditerpene diol, called diacardiol B (6), were isolated from the South China Sea sponge, Diacarnus megaspinorhabdosa. Their structures, including conformations and absolute configurations, were determined by using spectroscopic analyses, computational approaches and chemical degradation. Diacarperoxides H–J (1–3) showed some interesting stereochemical issues, as well as antimalarial activity.     

Multi-Temporal Detection of Rice Phenological Stages Using Canopy Spectrum

Information on rice phenology is essential for yield estimation and crop management. To test the ability of remote sensing in detecting multiple phenological stages, paddy rice canopy spectrum was measured by a hand-held radiometer. Normalized difference vegetation index(NDVI) was calculated from spectrum, and the slope of NDVI was obtained as its difference. We evaluated the response of NDVI and its slope to rice growth with a comparison of two late-season rice cultivars. The results showed that NDVI and its slope curves had distinct variation corresponding to rice development and they could be used as cultivar-independent phenological indicators. The dates of flooding and transplanting, tillering, panicle development, heading and flowering, maturity, harvest stages, and even field management practices, could be deduced from these indicators. ‘NDVI ≤ 0' could be used as a single threshold for the detection of flooding and transplanting. The largest spike in the curve of the NDVI slope indicated the duration of tillering stage. The next spike corresponded to panicle development. The heading and flowering stage was characterized by the maximum NDVI and the change of NDVI slope from positive to negative. At the maturity stage, NDVI decreased continuously, and its slope fluctuated just below zero. When rice grains were completely mature and ready for harvest, NDVI decline was accelerated. At harvest, NDVI slope reached its minimum value. The distinction between heading and maturity stages was obscure, most likely due to NDVI saturation at high biomass. The study might provide references for paddy rice phenology determination through remote sensing images.     

浅谈我国种业发展存在的问题及对策

本文通过分析我国种业发展现状,总结了我国种业发展的总体特征,指出了我国种业在发展过程中出现的各类问题,对现阶段我国种子企业的发展进行了思考,并提出建议。     

潮土长期不同施氮水平对秸秆降解及其细菌群落结构的影响

农田过量施氮所引发的问题已经引起广泛关注,但长期施氮后土壤无机氮水平状况及其对秸秆降解的作用尚不清楚。本研究以中国科学院封丘农业生态实验站长期（2005～2018年）施氮肥（5个施氮水平：0(N0)、150(N1)、190(N2)、,230(N3)和270 (N4)kg ha-1 yr-1）的潮土为研究对象,开展短期（50天）的秸秆降解-土壤培育实验。培育期间监测秸秆碳的矿化、土壤无机氮（硝态氮和铵态氮）、可溶性有机碳、微生物生物量碳的动态变化,利用高通量测序测定细菌群落结构。结果表明,长期施氮后,土壤无机氮含量和秸秆碳的矿化率随施氮水平的升高而增加。不同长期施氮水平的土壤细菌群落结构呈现显著差异。网络分析揭示：秸秆降解过程中细菌群落内部物种间的共现模式随长期施氮水平发生改变,具体体现为长期高施氮水平下细菌群落彼此间的负相关得到了加强;同时,变形菌主导地位减弱、酸杆菌主导地位增强。综上,土壤无机氮含量、细菌群落结构及物种之间的关系随着长期施氮水平的不同发生了改变。本研究探究了长期不同施氮水平下土壤中无机氮的水平状况、秸秆降解状况以及秸秆降解过程中土壤细菌的生物特性,以期为秸秆还田和科学施氮提供一定的数据支撑和思路启示。