假轮枝链霉菌Streptomyces pseudoverticillus产生的elaiophylin类新细胞周期抑制剂及细胞凋亡诱导剂I.菌种鉴定、发酵生产及提取分离

从链霉菌YN17707菌株发酵物中,通过活性跟踪分得三个elaiophylin类新细胞周期抑制剂及细胞凋亡诱导剂elaiophylin、11-O-monomethylelaiophylin和efomycin G。经菌种分类学研究,生产菌YN17707被鉴定为假轮枝链霉菌Streptomyces pseudoverticillus,并认证为elaiophylin类的新生产菌种。文中还探讨了该生产菌发酵生产elaiophylin类活性成分的发酵特征。     

假轮枝链霉菌 Streptomyces pseudoverticillus产生的Elaiophylin类新细胞周期抑制剂及细胞凋亡诱导剂Ⅱ.化学结构及生物活性(英文)

通过 X-线晶体结构解析及光谱学数据分析 ,将从假轮枝链霉菌 Streptomyces pseudoverticillus发酵物中分得的三个elaiophylin类化合物分别鉴定为 elaiophylin(1)、11- O- monomethylelaiophylin(2 )和 efomycin G(3)。化合物 1～ 3在高浓度区均有很强的细胞毒作用 ,而在低浓度区均呈很好的细胞周期抑制和细胞凋亡诱导活性 ,系 elaiophylin类新的细胞周期抑制剂及细胞凋亡诱导剂     

假轮枝链霉菌Streptomyces pseudoverticillus生产的Elaiophylin类新细胞周

通过波谱及X－线晶体结构分析，将从假轮枝链霉菌Streptomyces pseudouerticillus发酵物中分得的3个elaiophylin类化合物分别鉴定为elaiophyin(1)．11-O-monomethylelaiophyin(2)和efomycinG(3)，并利用DNMR技术对比合物1－3的^1H及^13C－NMR进行了详细解析，为今后该类新化合物的结构研究提供了有用的．详尽的NMR研究数据。     

假轮枝链霉菌Streptomyces pseudoverticillus 生产的Elaiophylin类新细胞周期抑制剂及细胞凋亡 诱导剂Ⅲ.化学结构及NMR研究

通过波谱及X-线晶体结构分析,将从假轮枝链霉菌Streptomycespseudoverticillus发酵物中分得的3个elaiophylin类化合物分别鉴定为elaiophylin(1)、11-O-monomethylelaiophylin(2)和efomycinG(3),并利用2DNMR技术对化合物1～3的     

Elaiophylins,New Cell Cycle Inhibitors and Apoptosis Inducers,Produced by Streptomyces pseudoverticillus(Ⅲ)Structural and NMR Studies

通过波谱及X-线晶体结构分析,将从假轮枝链霉菌Streptomycespseudoverticillus发酵物中分得的3个elaiophylin类化合物分别鉴定为elaiophylin(1)、11-O-monomethylelaiophylin(2)和efomycinG(3),并利用2DNMR技术对化合物1～3的1H及13C-NMR进行了详细解析,为今后该类新化合物的结构研究提供了有用的、详尽的NMR研究数据。     

黄直丝链霉菌18522生产的环二肽类细胞周期抑制剂

目的研究黄直丝链霉菌18522代谢产物中的环二肽类细胞周期抑制剂。方法采用温敏型小鼠乳腺癌tsFT210细胞的流式细胞术模型,以细胞周期抑制活性为指标,对黄直丝链霉菌18522发酵液和菌丝体的氯仿提取物进行活性成分追踪分离;根据理化性质和光谱数据鉴定化合物的化学结构;采用流式细胞术测定化合物的细胞周期抑制活性。结果从氯仿提取物中分离得到6个环二肽类化合物,分别鉴定为环(丙-亮)[cyclo(Ala-Leu),1]、环(丙-异亮)[cyclo(Ala-Ile),2]、环(丙-缬)[cyclo(Ala-Val),3]、环(苯丙-亮)[cyclo(Phe-Leu),4]、环(丙-脯)[cyclo(Ala-Pro),5]和环(苯丙-缬)[cyclo(Phe-Val),6];流式细胞术测试结果表明,化合物1~6均显示细胞周期G0/G1期抑制活性。结论首次报道化合物1~6具有细胞周期抑制活性。     

Labdane-type diterpenes as new cell cycle inhibitors and apoptosis inducers from Vitex trifolia L

Five labdane-type diterpenes, vitexilactone (1), (rel 5S,6R,8R,9R,10S)-6-acetoxy-9-hydroxy-13(14)-labden-16,15-olide (2), rotundifuran (3), vitetrifolin D (4), and vitetrifolin E (5), have been isolated from Vitex trifolia L., a Chinese folk medicine used to treat cancers, as new cell cycle inhibitors and apoptosis inducers through a bioassay-guided separation procedure and were identified by spectroscopic methods. Compounds 1-5 dramatically induced apoptosis both on tsFT210 and K562 cells at higher concentrations while at lower concentrations they inhibited the cell cycle progression of both tsFT210 and K562 cells at the G0/G1 phase. MIC values for 1-5 for inducing apoptosis and concentration regions for 1-5 for inhibiting cell cycle both on tsFT210 and K562 cells have also been determined. Furthermore, the inhibitory effects of 1-5 on the proliferation of tsFT210 and K562 cells have been evaluated by MTT assay to obtain IC50 values to confirm that 1-5 are anticancer components of Vitex trifolia L., which exert their anti-proliferative effect on cancer cells through inducing apoptosis and inhibiting the cell cycle. The present results provide labdane-type diterpenes, 1-5, as a new class of cell cycle inhibitors and compounds 1, 2, 4, and 5 as new apoptosis inducers, which also explains, for the first time, the usage of Vitex trifolia L. by Chinese people to treat cancers.     

Pseudoverticin B,a novel geldanamycin analog obtained as new cell cycle inhibitor from Streptomyces pseudoverticillus YN17707

Pseudoverticin B (1), a novel naturally occurring geldanamycin analog with cell cycle inhibitory activity, was isolated from the fermentation broth of Streptomyces pseudoverticillus YN17707, together with the known ansamycin antibiotic, hydroquinone geldanamycin (2), through bioassay-guided fractionation procedures. The structure of compound 1 was elucidated by spectroscopic methods, being characterized by an ansa bridge, same as that in geldanamycin and a novel hydroquinone-derived moiety. Compounds 1 and 2 arrested the cell cycle of tsFT210 cells at the G0/G1 phase with the minimum inhibitory concentration values of 10.1 and 20.2 μmolL^?1, respectively.     

Sapurimycin, new antitumor antibiotic produced by Streptomyces. Producing organism, fermentation, isolation and biological properties

In screening actinomycetes for antitumor compounds, Streptomyces sp. DO-116 was found to produce a new antitumor antibiotic sapurimycin. It is structurally related to, but distinct from, kapurimycins. The antibiotic was produced in a fermentation medium supplemented with high porous polymer resin which adsorbs antibiotic in the culture and results in an increase of titer. Active material was separated from the polymer resin by a solvent extraction procedure and isolated by repeated solvent extraction, adsorption chromatography and HPLC. Sapurimycin was active against bacteria, particularly Gram-positive organisms. It exhibited antitumor activity against leukemia P388 and sarcoma 180 in mice. Sapurimycin caused single strand breaks in supercoiled plasmid DNA in vitro. These results are discussed in comparison with data for kapurimycins.     

Nanaomycins, new antibiotics produced by a strain of Streptomyces. I. Taxonomy, isolation, characterization and biological properties.

Nanomycins are new antibiotics produced by the strain OS-3966 which was designated Streptomyces rosa var. notoensis. Nanomycins A and B were isolated from the culture filtrate by extraction with organic solvent and silica gel chromatography. The physical and chemical properties suggest that nanaomycins A and B are quinone-related compounds having the molecular formulae, C16H14O6 and C16H16O7, respectively. Nanaomycins A and B inhibit mainly mycoplasmas, fungi and Gram-positive bacteria. The acute toxicities (LD50, ip) of nanaomycins A and B in mice are 28.2 and 169 mg/kg, respectively.     

Triacsins, new inhibitors of acyl-CoA synthetase produced by Streptomyces sp

Triacsins A and B, new inhibitors of acyl-CoA synthetase, were isolated from the cultured broth of Streptomyces sp. strain SK-1894. The structurally related compounds WS-1228 A and B, known as hypotensive vasodilators, were also found to inhibit acyl-CoA synthetase. The four compounds have in common a N-hydroxytriazene moiety in their structures. The IC50 values for triacsin A and WS-1228 A were 5.5 and 3.6 micrograms/ml, respectively.