多烯大环类抗生素合成酶结构域的差异进化分析及应用于一株产四霉素链霉菌菌株的筛选

多烯大环类抗生素的生物合成酶属于典型的Ⅰ类聚酮合酶(PKS),这些生物大分子有着非常相似的化学结构和模块合成的形式.在本研究中,每个多烯聚酮合酶的单一结构域被作为系统进化分析的对象.我们发现,各类结构域在进化上出现了不同方向的倾向,其中,KS域在进化树中归成三大类,分别对应多烯结构的三大块区域;相对于KS域和ACP域表...     

Youssoufenes A2 and A3, Antibiotic Dimeric Cinnamoyl Lipids from the ΔdtlA Mutant of a Marine-Derived Streptomyces Strain

Two new dimeric cinnamoyl lipids (CL) featuring with an unusual dearomatic carbon-bridge, named youssoufenes A2 (1) and A3 (2), were isolated from the ΔdtlA mutant strain of marine-derived Streptomyces youssoufiensis OUC6819. Structures of the isolated compounds were elucidated based on extensive MS and NMR spectroscopic analyses, and their absolute configurations were determined by combination of the long-range NOE-based ¹H-¹H distance measurements and ECD calculations. Compounds 1 and 2 exhibited moderate growth inhibition against multi-drug-resistant Enterococcus faecalis CCARM 5172 with an MIC value of 22.2 μM.     

Optimisation of Healthy-Lipid Content and Oxidative Stability during Oil Extraction from Squid (Illex argentinus) Viscera by Green Processing

Green extraction was applied to Argentinean shortfin squid (Illex argentinus) viscera, consisting of a wet pressing method including a drying step, mechanic pressing, centrifugation of the resulting slurry, and oil collection. To maximise the oil yield and ω3 fatty acid content and to minimise the oil damage degree, a response surface methodology (RSM) design was developed focused on the drying temperature (45–85 °C) and time (30–90 min). In general, an increase of the drying time and temperature provided an increase in the lipid yield recovery from the viscera. The strongest drying conditions showed a higher recovery than 50% when compared with the traditional chemical method. The docosahexaenoic and eicosapentaenoic acid contents in the extracted oil revealed scarce dependence on drying conditions, showing valuable ranges (149.2–166.5 and 88.7–102.4 g·kg⁻¹ oil, respectively). Furthermore, the values of free fatty acids, peroxides, conjugated dienes, and ω3/ω6 ratio did not show extensive differences by comparing oils obtained from the different drying conditions. Contrary, a polyene index (PI) decrease was detected with increasing drying time and temperature. The RSM analysis indicated that optimised drying time (41.3 min) and temperature (85 °C) conditions would lead to 74.73 g·kg⁻¹ (oil yield), 1.87 (PI), and 6.72 (peroxide value) scores, with a 0.67 desirability value.     

Separacenes A–D,Novel Polyene Polyols from the Marine Actinomycete,Streptomyces sp

Separacenes A–D (1–4), novel polyene polyols, were isolated from Streptomyces sp. collected from the southern area of Jeju Island, Korea. The chemical structures of 1–4 were established by NMR, mass, UV, and IR spectroscopy as well as the modified Mosher’s method. Separacenes A–B (1–2), which share an identical planar structure but possess different relative configurations, bear tetraene units flanked by two diol moieties, whereas the stereoisomeric separacenes C–D (3–4) possess a triene moiety between two diol substructures. Separacenes A–D each contain a terminal olefinic methylene. Separacene A displayed inhibitory activity against Candida albicans isocitrate lyase and weak cytotoxicity against both the colon carcinoma cell line HCT-116 and the lung cancer cell line A549.     

一种抗真菌抗生素的分离纯化及初步鉴定

从海南五指山采集的土样中分离到一株放线菌,编号为WS-23883,其发酵提取物对多种植物病原真菌具有很强的抑制活性。对其产物进行提取精制及制备液相纯化,获得了纯度达90%以上的化合物。生测表明,在20μg/mL浓度下该抗生素对多种植物病原真菌的抑制率达100%。根据活性产物紫外吸收光谱,可判断其为一多烯大环内酯类抗生素。质谱分析表明,活性化合物分子质量约667 u,据此判断其为一四烯大环内酯类抗生素。     

内生放线菌Hhs.015中抗菌成分的性质及初步鉴定

【目的】明确内生放线菌Hhs.015中抗菌成分的性质及其物质类型。【方法】采用皿内抗菌活性测定的方法,研究了内生放线菌Hhs.015的抑菌谱及其发酵液粗提物的理化性质,并根据纸层析、紫外吸收曲线和捷克氏八溶剂系统对活性物质进行了化学类型的早期鉴别。【结果】菌株Hhs.015对16株靶标真菌中的13种有抗性,占靶标菌总数的81.25%,抑菌谱广;其中对番茄叶霉病菌、小麦纹枯病菌、番茄灰霉病菌、苹果腐烂病菌、苹果轮纹病菌的抑制能力较强,但不抑制细菌。自然pH(pH=6.2)下,随着温度由30℃上升至90℃,Hhs.015粗提物中抗菌活性物质的稳定性有小幅下降,至90℃时下降了2.61%,100℃下保温60min仍有较好活性,说明其具有较好的热稳定性;在偏碱性环境(pH=10.0)和酸性条件(pH=4.0)下,当温度由40℃上升至90℃时,Hhs.015粗提物对普通假丝酵母菌的抑菌圈直径降幅大于自然pH,且酸性条件下活性降低更多;在室温时,pH的变化对粗提物活性没有太大影响,紫外线对其抗菌活性影响很小。Hhs.015的活性物质粗提物在321,338和357nm处有典型共轭五烯生色基团的吸收峰,结合纸层析和纸电泳结果,推测活性物质中含有五烯类中性抗生素。【结论】菌株Hhs.015中抗菌成分的性质比较稳定,物质的离子特性为中性,可能含有多烯类成分。     

Sterol composition in polyene antibiotic-sensitive and resistant strains ofMalassezia pachydermatis

The membrane sterol compositions of ten strains ofMalassezia pachydermatis were analysed by gas-liquid chromatography. Six of these were wild-type strains from clinical sources that were sensitive to polyene antibiotics, whereas the other four strains were resistant mutants that had arisen after treatment withN-methyl-N-nitrosoguanidine or UV radiation.The wild-type strains contained 838.8 to 1291.7 µg of sterol per gram of freeze-dried mycelium. The sterols were composed of 79% ergosterol, 19% fecosterol and 2% lichesterol. The mutant strains contained 277.1 to 348.8 µg/g of sterols composed of 76% ergosterol and 24% fecosterol.Abbreviations MIC minimum inhibitory concentration - UV ultraviolet     

放线菌A01发酵液中活性成分稳定性及其化学类型

本文研究了对多种植物病原真菌均表现出良好抑菌活性的菌株A01发酵液中活性成分对热、酸碱、蛋白酶及紫外线的稳定性,并采用pH纸层析、捷克氏八溶剂系统纸层析、纸电泳和紫外波长扫描等方法对其进行了化学类型的早期鉴别。结果表明,菌株A01发酵液中活性物质在中性及偏碱性环境中比较稳定;100℃处理30min相对活性还保持在81.19%;对蛋白酶不敏感,但对紫外线较敏感;紫外扫描在291、305和319nm处有典型共轭四烯生色基团的吸收峰,结合纸层析和纸电泳结果,表明该活性物质归为四烯类中性抗生素。     

Polyene Macrolactams from Marine and Terrestrial Sources: Structure,Production Strategies,Biosynthesis and Bioactivities

Over the past few decades (covering 1972 to 2022), astounding progress has been made in the elucidation of structures, bioactivities and biosynthesis of polyene macrolactams (PMLs), but they have only been partially summarized. PMLs possess a wide range of biological activities, particularly distinctive fungal inhibitory abilities, which render them a promising drug candidate. Moreover, the unique biosynthetic pathways including β-amino acid initiation and pericyclic reactions were presented in PMLs, leading to more attention from inside and outside the natural products community. According to current summation, in this review, the chem- and bio-diversity of PMLs from marine and terrestrial sources are considerably rich. A systematic, critical and comprehensive overview is in great need. This review described the PMLs’ general structural features, production strategies, biosynthetic pathways and the mechanisms of bioactivities. The challenges and opportunities for the research of PMLs are also discussed.