紫海胆肠道放线菌Micromonospora sp. HDa2次生代谢产物的研究

采用常规色谱分离技术对分离自健康紫海胆肠道的稀有放线菌Micromonospora sp. HDa2发酵液的化学成分进行分离纯化,并以波谱技术确定化合物的结构。结果表明：从放线菌Micromonospora sp. HDa2的发酵液乙酸乙酯提取物中分离鉴定了6个已知结构的环二肽化合物,分别为环(苯丙-缬)二肽(1)、环(苯丙-亮)二肽(2)、环(苯丙-异亮)二肽(3)、环(苯丙-苯丙)二肽(4)、环(亮-亮)二肽(5)和环(亮-异亮)二肽(6)。对紫海胆肠道放线菌进行分离,结果发现以上化合物均是从Micromonospora属放线菌中发现的。     

蝴蝶和蝗虫肠道共生菌次生代谢产物的分离

对分离自健康蝴蝶和蝗虫肠道的共生菌Aspergillus sp. HDf1,Aspergillus sp. HCf2和Amycolatopsis sp. HCa1发酵液的化学成分进行了研究。采用色谱技术对化合物进行分离纯化,以波谱技术确定化合物的结构,结果从蝴蝶肠道共生真菌Aspergillus sp. HDf1,蝗虫肠道共生真菌Aspergillus sp. HCf2和放线菌Amycolatopsis sp. HCa1发酵液的乙酸乙酯提取物中各分离鉴定了1个化合物,分别为N-benzoylphenylalanyl-L-phenylalaninol acetate（1）,bostrycin（2）和2-spirocyclohexyl-2,3-dihydroquinazolin-4（1H）-one（3）;以上化合物均为首次从昆虫来源的共生菌中分离得到,其中化合物3是首次从Amycolatopsis属放线菌中发现。     

Secondary Metabolites Produced by a Cockchafer-derived Streptomyces sp. BCa1

对一株分离自昆虫铜绿金龟子幼虫肠道的链霉菌Streptomyces sp. BCa1的次生代谢产物进行化学研究。采用摇瓶发酵，并用柱色谱技术对该链霉菌的次生代谢产物进行分离纯化和利用光谱分析进行结构鉴定。结果从菌株Streptomyces sp. BCa1的发酵液中分离获得1个具有Hsp90蛋白抑制活性的格尔德霉素（geldanamycin）以及2个萘醌型大环内酯类化合物。所有化合物均为首次从昆虫来源的链霉菌中发现，且格尔德霉素为其主要产物，表明昆虫来源的放线菌具有良好的开发前景。     

沉香样品中曲霉属真菌菌株 HNWSW-20 的分离鉴定及其次生代谢产物的研究

本文采用平板分离法从沉香样品中分离得到一株真菌 HNWSW-20,从形态学和分子生物学上鉴定其为曲霉菌（Aspergillus sp.）,并利用多种色谱技术对其次生代谢产物进行分离纯化,根据波谱数据和理化性质鉴定其化合物结构为：2?,3?-dihydrosorbicillin（1）,sorbicillin（2）,2,3-二氢-2-(1-丙烯)-6,8-二甲基-7-羟基-色酮（3）,邻苯二甲酸二丁酯（4）,7-羟基-异苯并呋喃-1(3H)-酮（5）二十烷酸甲酯（6）;分别采用 Ellman 比色法和 pNPG 法测定化合物的乙酰胆碱酯酶抑制活性和 α-葡萄糖苷酶抑制活性,结果显示上述化合物 1、2、4 具有乙酰胆碱酯酶抑制活性,而化合物 1、3、5 具有 α-葡萄糖苷酶抑制活性。本文中化合物 1~2 为首次从曲霉属中分离得到,并首次报道具有乙酰胆碱酯酶和 α-葡萄糖苷酶抑制活性。     

牛大力根的化学成分研究

从牛大力(Millettia speciosa Champ.)根95%乙醇提取物的乙酸乙酯部分中分离得到了7个化合物,经波谱分析及与文献数据对照鉴定其结构为:2’,4,4’-三羟基查耳酮(1),紫檀素(2),3’,7-二羟基-2’,4’-二甲氧基异黄酮(3),高丽槐素(4),豆甾醇(5),β-谷甾醇(6),胡萝卜苷(7)。其中化合物(2)和化合物(3)为首次从该植物根中分离得到。     

鹦歌岭土壤来源Streptomyces sp. YG-7的次生代谢产物及其α-葡萄糖苷酶抑制活性研究

为了研究原始热带雨林鹦歌岭土壤放线菌（Streptomyces sp.）YG-7的次生代谢产物及其α-葡萄糖苷酶抑制活性,采用多种柱色谱方法对土壤放线菌YG-7的发酵产物进行分离纯化得到9个化合物,经过波谱数据分析分别鉴定为：(1) 2-acetamido-5-chlorobenzamide, (2) cyclo (L-Pro-L-Leu), (3) 3,6-dibenzylidene-2,5-piperazinedione, (4) albonoursin, (5) (3Z,6S)-3-benzylidene-6-isobutylpiperazine-2,5-dione, (6) 3-hydroxy-2-methyl-4-pyrone, (7) isophthalic acid, (8) methyl 3-carbamoylbenzoate, (9) 2,3-dihydroxypropyl hexadecanoate. 其中,化合物1、7和8为新天然产物。活性测试结果表明化合物1、3~5和7~8对α-葡萄糖苷酶具有明显的抑制活性。     

铜绿金龟子肠道链霉菌Streptomyces sp. BCa1 菌体的抗菌成分研究

为从昆虫来源的放线菌次级代谢产物中寻找药物先导分子，对铜绿金龟子幼虫肠道链霉菌Streptomyces sp. BCa1菌丝体化学成分进行了研究。通过活性跟踪，从其菌丝体的氯仿甲醇萃取物中分离得到主要成分1。利用高分辨质谱、一维和二维核磁波谱技术，将该主要成分1鉴定为具有双重旋转对称结构的不饱和大环内酯类抗生素阿扎霉素（elaiophylin），具有显著的抗金黄色葡萄球菌活性。该类化合物为首次从昆虫来源的放线菌中发现。     

红树林来源真菌Xylaria sp. HNWSW-2异香豆素类次生代谢产物及其生物活性的研究

为了研究红树林来源真菌Xylaria sp. HNWSW-2的次生代谢产物及其生物活性,综合利用多种色谱技术对该菌株发酵产物进行分离纯化,结合波谱学与理化常数分析进行化合物结构鉴定,分别采用液体浸泡法和Ellman比色法对化合物的全齿复活线虫致死活性和乙酰胆碱酯酶抑制活性进行测试。从Xylaria sp. HNWSW-2发酵产物乙酸乙酯萃取物中分离鉴定了7个异香豆素类化合物,分别为 (S)-(+)-8-O-methylmellein (1),(3S,4S)-(+)-4-hydroxy-8-O- methylmellein (2),(3S,4R)-(+)-4-hydroxy-8-O-methylmellein (3),(3S,4S)-(+)-4-hydroxymellein (4),(3S,4R)-(+)-4- hydroxymellein (5),(3R,4R)-(-)-4-hydroxy-5-methylmellein (6)和(3R,4S)-(+)-4-hydroxy-5-methylmellein (7)。其中,化合物1具有较强全齿复活线虫致死活性,化合物1~3、6和7具有一定的乙酰胆碱酯酶抑制活性。本研究首次发现化合物(S)-(+)-8-O-methylmellein具有较强的抗线虫活性,为相关杀线虫药物的研发提供理论依据。     

对玉米螟具有生物活性的海洋放线菌筛选与鉴定

通过平板稀释法对来自青岛不同地区的海洋样品进行分离,共得到18株海洋放线菌。采用浸虫法测定海洋放线菌发酵液对玉米螟2龄幼虫的室内毒力,筛选得到2株活性较高的菌株YC3和SLR3,其48 h发酵液对玉米螟2龄幼虫的校正死亡率分别为86.21%和81.04%。根据形态特征、培养特征及生理生化性状将活性菌株鉴定为链霉菌属(Streptomyces)。     

普洱茶的抗氧化酚类化学成分的研究

从云南省双江县勐库产的普洱茶中分离得到11个化合物,分别为:(-)-没食子儿茶素(GC,1),(-)-表儿茶素(EC,2),(+)-儿茶素(C,3),杨梅素(4),没食子酸(5),山奈酚(6),山奈酚-3-O-β-D-葡萄糖甙(7),山奈酚-3-O–芦丁糖甙(8),槲皮素(9),槲皮素-3-O-β-D葡萄糖甙(10)以及2,5-二羟基苯甲酸(11)。其中,化合物6~11为首次从普洱茶中分离得到。DPPH自由基清除活性测试结果表明,化合物2、3、5的活性与阳性对照品抗坏血酸接近。化合物的结构与其活性的关系比较分析表明,简单儿茶素(2,3)和简单酚类化合物(5)的抗氧化活性较高,与阳性对照品抗坏血酸接近;黄酮类化合物(4,6,9)次之,黄酮类配糖体(7,8,10)及化合物11则较差。     

A new diketopiperazine, cyclo-(4-S-hydroxy-R-proline-R-isoleucine), from an Australian specimen of the sponge Stelletta sp

While investigating the cytotoxic activity of the methanol extract of an Australian marine sponge Stelletta sp. (Demospongiae), a new diketopiperazine, cyclo-(4-S-hydroxy-R-proline-R-isoleucine) (1), was isolated together with the known bengamides; A (2), F (3), N (4), Y (5), and bengazoles; Z (6), C(4) (7) and C(6) (8). The isolation and structure elucidation of the diketopiperazine (1), together with the activity of 1-8 against a panel of human and mammalian cell lines are discussed.     

Neuroprotective Metabolites from Vietnamese Marine Derived Fungi of Aspergillus and Penicillium Genera

Low molecular weight secondary metabolites of marine fungi Aspergillus flocculosus, Aspergillus terreus and Penicillium sp. from Van Phong and Nha Trang Bays (Vietnam) were studied and a number of polyketides, bis-indole quinones and terpenoids were isolated. The structures of the isolated compounds were determined by 1D and 2D NMR and HR-ESI-MS techniques. Stereochemistry of some compounds was established based on ECD data. A chemical structure of asterriquinone F (6) was thoroughly described for the first time. Anthraquinone (13) was firstly obtained from a natural source. Neuroprotective influences of the isolated compounds against 6-OHDA, paraquat and rotenone toxicity were investigated. 4-Hydroxyscytalone (1), 4-hydroxy-6-dehydroxyscytalone (2) and demethylcitreoviranol (3) have shown significant increasing of paraquat- and rotenone-treated Neuro-2a cell viability and anti-ROS activity.     

A New Analogue of Echinomycin and a New Cyclic Dipeptide from a Marine-Derived Streptomyces sp. LS298

Quinomycin G (1), a new analogue of echinomycin, together with a new cyclic dipeptide, cyclo-(l-Pro-4-OH-l-Leu) (2), as well as three known antibiotic compounds tirandamycin A (3), tirandamycin B (4) and staurosporine (5), were isolated from Streptomyces sp. LS298 obtained from a marine sponge Gelliodes carnosa. The planar and absolute configurations of compounds 1 and 2 were established by MS, NMR spectral data analysis and Marfey’s method. Furthermore, the differences in NMR data of keto-enol tautomers in tirandamycins were discussed for the first time. Antibacterial and anti-tumor activities of compound 1 were measured against 15 drug-sensitive/resistant strains and 12 tumor cell lines. Compound 1 exhibited moderate antibacterial activities against Staphylococcuse pidermidis, S. aureus, Enterococcus faecium, and E. faecalis with the minimum inhibitory concentration (MIC) values ranged from 16 to 64 μg/mL. Moreover, it displayed remarkable anti-tumor activities; the highest activity was observed against the Jurkat cell line (human T-cell leukemia) with an IC₅₀ value of 0.414 μM.     

Kiamycin, a unique cytotoxic angucyclinone derivative from a marine Streptomyces sp

Kiamycin (1), a new angucyclinone derivative possessing an 1,12-epoxybenz[a]anthracene ring system, was isolated from the marine Streptomyces sp. strain M268 along with the known compounds 8-O-methyltetrangomycin (3) and 8-O-methylrabelomycin (4). Their structures were elucidated by detailed spectroscopic analysis and comparison with literature data. The new angucyclinone derivative showed inhibitory activities against the human cell lines HL-60 (leukemia), A549 (lung adenocarcinoma), and BEL-7402 (hepatoma) with inhibition rates of 68.2%, 55.9%, and 31.7%, respectively, at 100 μM. It appears to have potential as an anticancer agent with selective activity.     

Antibacterial bisabolane-type sesquiterpenoids from the sponge-derived fungus Aspergillus sp

Four new bisabolane-type sesquiterpenoids, aspergiterpenoid A (1), (-)-sydonol (2), (-)-sydonic acid (3), and (-)-5-(hydroxymethyl)-2-(2',6',6'-trimethyltetrahydro-2H- pyran-2-yl)phenol (4) together with one known fungal metabolite (5) were isolated from the fermentation broth of a marine-derived fungus Aspergillus sp., which was isolated from the sponge Xestospongia testudinaria collected from the South China Sea. Four of them (1-4) are optically active compounds. Their structures and absolute configurations were elucidated by using NMR spectroscopic techniques and mass spectrometric analysis, and by comparing their optical rotations with those related known analogues. Compounds 1-5 showed selective antibacterial activity against eight bacterial strains with the MIC (minimum inhibiting concentrations) values between 1.25 and 20.0 μM. The cytotoxic, antifouling, and acetylcholinesterase inhibitory activities of these compounds were also examined.