多棘蜈蚣化学成分的研究（I）

目的 研究多棘蜈蚣Scolopendra multidens的化学成分.方法 采用硅胶柱色谱、反相柱色谱、Sephadex LH-20柱色谱、中低压制备色谱、制备HPLC等方法进行分离纯化,并根据理化性质和波谱数据鉴定化合物结构.结果 从多棘蜈蚣乙醇冷浸提取物中分离得到了10个化合物,分别鉴定为尿嘧啶(1)、7,8-二甲基异咯嗪(2)、吲哚-3-乙酰胺(3)、N-乙酰基-2-苯基乙胺(4)、(3S)-1,2,3,4-四氢-β-咔啉-3-羧酸(5)、环(L-异亮-L-脯)二肽(6)、环(L-亮-L-脯)二肽(7)、环(L-苯丙-L-脯)二肽(8)、环(L-苯丙-L-酪)二肽(9)、环(L-缬-L-脯)二肽(10).结论 所有化合物均为首次从多棘蜈蚣中分离得到.     

带形蜈蚣藻的化学成分研究

目的 研究南海大型经济海藻带形蜈蚣藻(Grateloupia turuturu)的化学成分.方法 利用色谱、 红外、质谱和核磁共振波谱等方法对带型蜈蚣藻的化学成分进行分离和结构鉴定并进行抗病毒活性研究.结果 从中分离鉴定了6个化合物,分别为棕榈酸(I)、3-β-5-烯-胆甾醇(Ⅱ)、胆甾-4-烯-6-酮(Ⅲ)、胆甾-4-烯-3-酮(Ⅳ)、胆甾-4,6-二烯-3-醇(Ⅴ)和胆甾-4,6-二烯-3-酮(Ⅵ),化合物Ⅱ抗HSV-1病毒效果较好,其IC50达到7.81μg/ml.结论 以上均为首次从该海藻中分离得到.化合物Ⅱ具有较好的抗病毒活性.     

蜈蚣藻的化学成分

目的：系统研究蜈蚣藻的活性成分。方法：使用硅胶、Sephadex LH-20、ODS 和 HPLC 分离、纯化, 根据理化性质和光谱分析鉴定化合物的结构。结果：分离鉴定了 15 个化合物, 分别为 4-羟基-3-甲氧基苯甲醛（1）, 4-羟基-3, 5-二甲氧基苯甲醛（2）、3-溴-4, 5-二羟基苯甲醛（3）、2-溴-4, 5-二羟基苯甲醛（4）、3-溴-5-羟基-4-甲氧基苯乙酸（5）、24-羟基-乙烯基-胆甾醇（6）、3-吲哚甲酸（7）、尿嘧啶（8）、尿嘧啶核苷（9）、岩藻甾醇（10）、植醇（11）、邻苯二甲酸二正丁酯（12）、硬脂酸（13）、软脂酸（14）和甘露醇（15）。结论：1~15 均为首次从蜈蚣藻中分离得到。     

蜈蚣药材薄层鉴别及抗凝活性定量的研究

目的:对蜈蚣药材的薄层鉴别及抗凝活性定量方法进行研究,为该药材质量控制标准的完善提供依据。方法:对蜈蚣药材中游离精、丝氨酸进行薄层层析,筛选供试品制备方法及展开剂系统;以凝血酶滴定法测定蜈蚣药材抗凝活性,筛选药材前处理方法。结果:蜈蚣药材经甲酸及95%乙醇(1∶1)超声处理后,以正丁醇-乙酸-水(12∶5∶4)体系于硅胶G板上进行薄层层析,经茚三酮显色后,斑点清晰,杂质及拖尾影响较小,目标成分分离度较好;以凝血酶滴定法测定蜈蚣药材抗凝活性,结果重现性较好,超声法提取药材中的抗凝成分,操作简单,耗时较短,所制供试品抗凝血酶活性为(14.00±1.53)U/g;另测3批不同批次蜈蚣药材抗凝活性分别为:(13.00±0.58)U/g、(17.00±1.15)U/g、(15.67±1.53)U/g。结论:所选择的薄层鉴别及抗凝活性定量方法可作为完善蜈蚣药材质量标准的依据。     

苍耳化学成分的分离与鉴定

目的对苍耳Xanthium sibiricum地上部分的化学成分进行分离和鉴定。方法采用硅胶柱色谱、制备薄层色谱、MCI凝胶色谱和Sephadex LH-20柱色谱等方法对其化学成分进行分离纯化,应用现代波谱技术ESI-MS、1H-NMR、13C-NMR对化合物的结构进行鉴定。结果从苍耳中分离得到了7个倍半萜类化合物,分别为苍耳农(1)、苍耳亭(2)、3-cycloheptene-1-acetic acid(3)、xanthinosin(4)、inusoniolide(5)、5-azuleneacetic acid(6)、2-hydroxy xanthinosin(7)。结论化合物1为新化合物,命名为苍耳农,化合物3、6、7为首次从苍耳植物中分离得到,化合物5为首次从苍耳属植物中分离得到,其中化合物2的量较丰富(0.1%),为开发新型植物源杀菌剂奠定了基础。     

苍耳子化学成分研究

目的:研究苍耳子的化学成分。方法:采用硅胶柱色谱、ODS反相柱色谱和制备型高效液相色谱等方法分离,从苍耳子70%乙醇提取物的正丁醇萃取组分中分离得到了4个化合物,并通过NMR和MS等波谱方法确定其化学结构。结果:所分离得到的4个化合物分别为2-methyl-3-buten-2-ol-β-D-apiofuranosyl-(1-6)-β-D-glucopyranoside(1),3-Methyl-3-butenyl-O-β-Dapiofuranosyl-(1-6)-O-β-D-glucopyranoside(2),3-Methyl-2-butenyl-O-β-D-apiofuranosyl-(1-6)-O-β-D-glucopyranoside(3)和everlastoside C(4)。其中所有化合物均为为首次从苍耳子中分离得到。     

吊扬尘化学成分研究

目的:对吊扬尘的化学成分进行分离和鉴定.方法:采用硅胶柱色谱、凝胶柱色谱、制备高效液相色谱等方法分离化合物,根据理化性质和波谱解析鉴定各化合物的结构.结果:从吊扬尘石油醚提取物中分离得到8个化合物:Buddlindeterpene B(1)、Buddledin B(2)、Buddledin C(3)、deacetyldihydrobuddledin A(4)、dihydrobuddledin C(5)、Suberosol B(6)、Gadain(7)、Hinokinin(8).结论:化合物1、4～8为首次从该植物中分离得到.     

油茶枯饼中1个新的三萜皂苷

目的研究油茶Camellia oleifera枯饼的化学成分。方法利用硅胶、MPLC柱色谱、高效制备液相色谱等色谱方法进行分离纯化,根据理化常数测定及波谱数据分析鉴定化合物结构。结果从油茶枯饼中分离得到3个化合物,分别鉴定为3β,15α,16α,22α,28-五羟基-22-O-当归酰基-齐墩果-12-烯-3-O-β-D-葡萄糖基(1→2)-[β-D-葡萄糖基(1→2)-β-D-木糖基(1→3)]-β-D-葡萄糖醛酸甲酯苷(1)、gordonoside R(2)、gordonoside Q(3)。结论化合物1为新化合物,命名为油茶皂苷Ab,化合物2和3为首次从油茶中分离得到。     

蜈蚣胃蛋白酶解物体外抗凝活性肽类的分离与分析

目的:采用凝胶过滤色谱和C18反相色谱对蜈蚣胃蛋白酶解物的抗凝活性部位进行分离纯化,并检测其相对分子质量分布范围。方法:按色带及280 nm紫外光谱法收集凝胶色谱分离各流分;以活化部位凝血活酶时间(APTT)为指标,检测各流分体外抗凝活性;用基质辅助激光解吸电离飞行时间质谱(MALDI-TOF-MS)检测其相对分子质量分布范围。结果:经凝胶过滤色谱和C18反相色谱纯化得到了抗凝活性组分,用MALDI-TOF-MS测得其相对分子质量分布范围为597～1 146。结论:凝胶过滤色谱和C18反相色谱可用于蜈蚣胃蛋白酶解物抗凝活性组分的分离纯化,其抗凝活性组分为小分子肽类。     

拟缺香茶菜中化学成分研究

采用大孔吸附树脂柱色谱、硅胶柱色谱、Sephadex LH-20凝胶柱色谱以及半制备型高效液相色谱等多种色谱分离技术从拟缺香茶菜干燥的地上部分的水提取液中分离得到6个化合物,综合运用1D-NMR,2D-NMR以及HR-ESI-MS等谱学方法对它们进行了结构鉴定,分别鉴定为3-O-β-D-阿洛糖-1-辛烯-3-醇(1),布鲁门醇A(2),光色素(3),黑麦角内酯(4),线蓟素(5)和胡麻素(6)。其中化合物1为新化合物,化合物2~4为首次从该植物中分离得到。     

Highly brominated antimicrobial metabolites from a marine Pseudoalteromonas sp

Extracts of a marine Pseudoalteromonas sp. (CMMED 290) isolated from the surface of a nudibranch collected in Kaneohe Bay, Oahu, displayed significant antimicrobial activity against methicillin-resistant Staphylococcus aureus. Bioassay-guided fractionation of the lipophilic extract led to the isolation and structure elucidation of two new highly brominated compounds, 2,3,5,7-tetrabromobenzofuro[3,2-b]pyrrole (1) and 4,4',6-tribromo-2,2'-biphenol (2). In addition, we have identified the known compounds pentabromopseudilin and bromophene. We describe the isolation and structure elucidation of the compounds 1 and 2 together with their antimicrobial activities against methicillin-resistant Staphylococcus aureus.     

Plakolide A, a new gamma-lactone from the marine sponge Plakortis sp

Plakolide A (1), a new alpha-exomethylene-gamma-lactone isolated from the marine sponge Plakortis sp., was found to inhibit inducible nitric oxide synthase (iNOS) activity. The isolation, structure elucidation, and biological activity of plakolide A is described.     

Additional pyrrolomycins from cultures of Streptomyces fumanus

Along with dioxapyrrolomycin (1), four new pyrrolomycin antibiotics, namely, pyrrolomycin G (3), pyrrolomycin H (4), pyrrolomycin I (5), and pyrrolomycin J (6), were produced in cultures of Streptomyces fumanus. Apart from dioxapyrrolomycin, pyrrolomycin G and pyrrolomycin H are the only other chiral members of the pyrrolomycin family of antibiotics, and their absolute stereochemistry was deduced to be 13S. Here, we report the isolation, structure elucidation, and antimicrobial activity of these new pyrrolomycins.     

Chemical constituents of Garcinia fusca: structure elucidation of eight new xanthones and their cancer chemopreventive activity

We describe the isolation and spectrometric structure elucidation of eight new xanthones, fuscaxanthone A (1), B (2), C (3), D (4), E (5), F (6), G (7), and H (8), together with eight known xanthones from the stem bark of Garcinia fusca collected in Thailand. All the new xanthones were shown to have a terpenoid (prenyl and/or geranyl) side chain(s) in their molecules. We also present the results of a primary screening of the inhibitory effects of eight xanthones (9-16) isolated as major components of this plant on 12-O-tetradecanoylphorbol-13-acetate induced Epstein-Barr virus early antigen activation in Raji cells.     

Secobatzellines A and B, two new enzyme inhibitors from a deep-water Caribbean sponge of the genus Batzella.

Secobatzelline A (1), a new batzelline natural analogue, and secobatzelline B (2), a likely artifact formed during the isolation procedure, have been isolated from a deep-water marine sponge of the genus Batzella. Secobatzellines A and B inhibited the phosphatase activity of calcineurin, and secobatzelline A inhibited the peptidase activity of CPP32. Both compounds showed in vitro cytotoxicity against P-388 and A-549 cell lines. The isolation and structure elucidation of secobatzellines A (1) and B (2) are described.     

Five new discodermolide analogues from the marine sponge Discodermia species

Discodermolide (1) and five new discodermolide analogues trivially named 2-epi-discodermolide (2), 2-des-methyldiscodermolide (3), 5-hydroxymethyldiscodermolate (4), 19-des-aminocarbonyldiscodermolide (5), and 9(13)-cyclodiscodermolide (6) have been isolated from marine sponges belonging to the genus Discodermia collected from the Caribbean Sea. The isolation, structure elucidation, and biological activities of 2-6 are described. The natural analogues, which were isolated in trace amounts, exhibited significant variation of cytotoxicity against the cultured murine P-388 leukemia and A-549 human adenocarcinoma cells and suggested the importance of the C(7) through C(17) moiety for potency against cultured tumor cell lines.     

Using jasplakinolide to turn on pathways that enable the isolation of new chaetoglobosins from Phomospis asparagi

The isolation and structure elucidation of three new secondary metabolites, chaetoglobosin-510 (1), -540 (2), and -542 (3), are described. These compounds were produced by cultures of the marine-derived fungus Phomopsis asparagi, challenged with the known F-actin inhibitor jasplakinolide. Chaetoglobosin-542 (3) displayed antimicrofilament activity and was cytotoxic toward murine colon and leukemia cancer cell lines.     

Antibiotic terpenoid chloro-dihydroquinones from a new marine actinomycete

As part of our continuing interest in exploring the chemistry of actinomycete bacteria uniquely adapted for survival in ocean sediments, we encountered several new strains, which by 16S rDNA sequence-based phylogenetic analysis were recognized as members of a new genus (tentatively called MAR4) within the family Streptomycetaceae. We report here the isolation and structure elucidation of three new chlorinated dihydroquinones (1-3) and one previously reported analogue, 4, from our strain CNQ-525, isolated from ocean sediments collected at a depth of 152 m near La Jolla, California. The compounds formally possess new carbon skeletons, but are related to several previously reported metabolites of the napyradiomycin class. The structures of the new molecules, which possess significant antibiotic properties and cancer cell cytotoxicities, were assigned by comprehensive spectral measurements and by comparison with NMR and other spectral data from the antibiotic A80915C (5), the full stereostructure of which was recently assigned by X-ray diffraction methods.     

红树林植物海漆的化学成分(Ⅰ)

目的：从红树林植物海漆中寻找具有肿瘤抑制活性的先导化合物．方法：利用柱层析手段，结合波谱方法（ESI—MS，^1D NMR和^2D NMR）分离鉴定海漆的化学成分。结果：从红树植物海漆的石油醚部分分离纯化了10个次生代谢产物：蒲公英赛酮（1），3-羰基-18-烯-齐墩果烷（2），3，28-二羟基-羽扇豆醇（3），3-羰基-28-羟基-羽扇豆醇（4），3-羟基-18烯-齐墩果烷（5），邻苯二甲酰正二丁酯（6），邻苯二甲酸二乙基己酯（7），4-烯-3-酮豆甾烷（8），脱镁叶绿素A（9），脱镁叶绿素甲酯A（10）．结论：化合物1和7具有较弱的肿瘤抑制活性．     

Suaveolindole, a new mass-limited antibacterial indolosesquiterpene from Greenwayodendron suaveolens obtained via high-throughput natural products chemistry methods

Utilizing high-throughput isolation, purification, and analysis methods applied to a natural products library, a new mass-limited antibacterial indolosesquiterpene, suaveolindole (1), was obtained from Greenwayodendron suaveolens. The miniaturization of the structure elucidation of 1 was performed primarily using the CapNMR probe. Compound 1 was found to possess significant in vitro antibacterial activity against the Gram-positive bacteria Bacillus subtilis (ATCC 43223), Staphylococcus aureus (ATTC 6538P), and methicillin-resistant Staphylococcus aureus (ATTC 33591), with MIC values of 4, 8, and 8 microg/mL, respectively.