Dactylospongia elegans—A Promising Drug Source: Metabolites,Bioactivities, Biosynthesis,Synthesis, and Structural-Activity Relationship

Marine environment has been identified as a huge reservoir of novel biometabolites that are beneficial for medical treatments, as well as improving human health and well-being. Sponges have been highlighted as one of the most interesting phyla as new metabolites producers. Dactylospongia elegans Thiele (Thorectidae) is a wealth pool of various classes of sesquiterpenes, including hydroquinones, quinones, and tetronic acid derivatives. These metabolites possessed a wide array of potent bioactivities such as antitumor, cytotoxicity, antibacterial, and anti-inflammatory. In the current work, the reported metabolites from D. elegans have been reviewed, including their bioactivities, biosynthesis, and synthesis, as well as the structural-activity relationship studies. Reviewing the reported studies revealed that these metabolites could contribute to new drug discovery, however, further mechanistic and in vivo studies of these metabolites are needed.     

利用VIGS技术研究广藿香醇合酶基因PatPTS的功能

广藿香精油主要存贮在植物地上组织的盾状腺毛中。提取广藿香（马来西亚品系）叶片的总RNA后,通过PCR技术扩增得到广藿香醇合酶基因（PatPTS）的全长cDNA序列,共编码552个氨基酸,与GenBank中已报道的印度广藿香中广藿香醇合酶的氨基酸序列存在3.6%的差异。使用烟草脆裂病毒（tobacco rattle virus,TRV）,选取PatPTS作为沉默目的基因,在广藿香中构建病毒诱导基因沉默（VIGS）体系,进一步利用该体系在广藿香中鉴定PatPTS基因的功能。病毒侵染广藿香叶片后,分别选取不同的时间点,使用GS-MS与qRT-PCR检测PatPTS催化产物和转录水平的变化,结果发现：β-广藿香烯、β-榄香烯、石竹烯、广藿香醇等倍半萜成分的含量在VIGS侵染后第2周明显下降,1周和3周效果不明显;PatPTS转录本下降趋势与其调控的倍半萜含量变化趋势类似;表明PatPTS基因负责了广藿香精油主要倍半萜成分的合成。说明广藿香中VIGS体系已初步建立,并在侵染植物2周后诱导基因沉默和干扰次生代谢产物合成的效果最好,为在广藿香中快速研究基因功能打下基础。     

白木香茎中内源茉莉酸类和倍半萜类物质对机械伤害的响应

 为揭示伤害信号--茉莉酸类（JAs）对倍半萜可能的调控作用,以3年生白木香[Aquilaria sinensis（Lour.）Gilg]树苗为试材进行机械伤害和外施茉莉酸甲酯（MeJA）处理,测定其茎中内源JAs和倍半萜含量。结果表明,机械伤害处理1 h后,内源JAs含量显著增加,随后迅速下降;伤害处理24 h后又有小幅升高。伤害处理诱导白木香产生3种倍半萜（δ–愈创木烯、α–愈创木烯和α–葎草烯）且含量随着伤害时间延长而增多。外源MeJA处理也能够诱导产生相同种类的倍半萜且诱导强度大于伤害处理。伤害早期（1 h）内源JAs含量升高和伤害后期（48 h）倍半萜含量增多是植物启动相应的防御反应和抵御伤害胁迫的重要机制。     

Four eremophilane sesquiterpenes from the mangrove endophytic fungus Xylaria sp. BL321

Three new eremophilane sesquiterpenes (1–3) were isolated from the mangrove endophytic fungus Xylaria sp. BL321 together with 07H239-A (4), a known analogue of the new compounds. The structures of these compounds were elucidated by analysis of their MS, 1D and 2D NMR spectroscopic data. Compound 4 showed activation activity on α-glucosidase at 0.15 μM (146%), and then, 4 gradually produced inhibitory activity on α-glucosidase with increasing concentration, and the IC₅₀ value is 6.54 μM.     

生姜辛香物质合成途径关键基因ZoHMGR的克隆及表达

为探明3-羟基-3-甲基戊二酸单酰辅酶A还原酶(HMGR)在生姜(Zingiber officinale Roscoe)倍半萜合成途径的调节作用,根据在竹根姜转录组数据库中HMGR不同转录本序列,经比对分析后利用RT-PCR技术克隆HMGR基因的全长cDNA序列,并对其进行生物信息学分析;再利用荧光定量PCR技术检测目的基因在竹根姜不同组织和叶组织在不同诱导条件下的表达特性,同时分析其生成的倍半萜物质。结果表明:克隆的竹根姜ZoHMGR基因编码562个氨基酸,其与姜科植物阳春砂的亲缘关系最近。ZoHMGR基因主要在根茎中表达,其次是叶,而茎和根中的表达量最低,符合生姜不同组织中倍半萜物质的含量特征;该基因同时受物理伤害和茉莉酸甲酯处理的诱导,分别在6h和12h达最高表达水平,同时有倍半萜类物质生成。     

A new sesquiterpene from the fruits of Allophylus laevigatus

From the fruits of Allophylus laevigatus a new sesquiterpene, 11-acetoxy-4 alpha-methoxyeudesmane, was isolated alongwith the known compounds carissone and apigenin-8-C-beta-rhamnopyranoside. The flavone showed no antioxidant activity in the autoxidation of beta-carotene assay.     

Inheritance of the sesquiterpenes longipinenone and hydroxy-longipinenone within the Achillea millefolium complex (Compositae)

Three selfing and 13 crossing experiments between tetraploid individuals of Achillea ceretanica, Achillea collina, Achillea distans ssp.‘styriaca’ Saukel (ined.), and Achillea pratensis (Achillea millefolium complex, Compositae), five F₁ crosses, three backcrosses and one further selfing experiment were carried out in order to study the inheritance of longipinenone (1) and its hydroxyl derivative (2). From these crossings, 1294 plants were studied by qualitative thin layer chromatography. Progenies from parent and F₁ plants without longipinenones (0‐type, ll) uniformly contained none of these two sesquiterpenes. All other crossing experiments showed typical segregation patterns of 0‐type, L‐type (longipinenone (1) without hydroxylongipinenone, L.hh) and H‐type (hydroxy‐longipinenone (2) and occasionally longipinenone, L.H.) in the ratio of 1 : 1 and 1 : 3. According to these results both derivatives are under dominant genetic control regulated by genes L and H, whereby hydroxylation takes place after synthesis of longipinenone (1).     

New Terpenes from the Egyptian Soft Coral Sarcophyton ehrenbergi

Chemical investigations of the Egyptian soft coral Sarcophyton ehrenbergi have led to the isolation of compounds 1–3 as well as the previously reported marine cembranoid diterpene sarcophine (4). Structures were elucidated by comprehensive NMR and HRMS experimentation. Isolated compounds were in vitro assayed for cytotoxic activity against human hepatocarcinoma (HepG2) and breast adenocarcinoma (MCF-7) cell lines.     

The Prospective Use of Brazilian Marine Macroalgae in Schistosomiasis Control

Schistosomiasis is a parasitic disease that affects more than 250 million people. The treatment is limited to praziquantel and the control of the intermediate host with the highly toxic molluscicidal niclosamide. Marine algae are a poorly explored and promising alternative that can provide lead compounds, and the use of multivariate analysis could contribute to quicker discovery. As part of our search for new natural compounds with which to control schistosomiasis, we screened 45 crude extracts obtained from 37 Brazilian seaweed species for their molluscicidal activity against Biomphalaria glabrata embryos and schistosomicidal activities against Schistosoma mansoni. Two sets of extracts were taxonomically grouped for metabolomic analysis. The extracts were analyzed by GC–MS, and the data were subjected to Pattern Hunter and Pearson correlation tests. Overall, 22 species (60%) showed activity in at least one of the two models. Multivariate analysis pointed towards 3 hits against B. glabrata veliger embryos in the Laurencia/Laurenciella set, 5 hits against B. glabrata blastula embryos, and 31 against S. mansoni in the Ochrophyta set. Preliminary annotations suggested some compounds such as triquinane alcohols, prenylated guaianes, dichotomanes, and xenianes. Despite the putative identification, this work presents potential candidates and can guide future isolation and identification.