利用稻瘟霉分生孢子跟踪分离面包海星中的海星皂苷活性成分

目的研究面包海星中的海星皂苷活性成分。方法以稻瘟霉模型进行活性监测，采用多种层析手段和波谱技术对海星皂苷活性成分跟踪分离并鉴定其结构。结果分离获得14个海星皂苷，鉴定了其中12个结构(1～12)，包括7个新的海星皂苷(6～12)。其中大多对稻瘟霉显示活性且对K-562和BEL-7402肿瘤细胞株显示显著或中等强度的细胞毒性，2个皂苷有溶血作用。结论利用稻瘟霉模型对海星皂苷活性成分进行跟踪分离是可行的，该研究也为进一步开发抗肿瘤新药提供了有价值的先导化合物和科学依据。     

Antifungal, antimitotic and anti-HIV-1 agents from the roots of Wikstroemia indica

With guidance of Pyricularia oryzae bioassay, daphnoretin (1), (+)-nortrachelogenin (2), genkwanol A (3), wikstrol A (4), wikstrol B (5) and daphnodorin B (6) were isolated from the roots of Wikstroemia indica. Compounds 1-6 induced morphological deformation of P. oryzae mycelia with MMDC values of 68.4 +/- 1.3, 31.3 +/- 1.8, 45.8 +/- 0.5, 70.1 +/- 2.4, 52.3 +/- 0.9 and 73.7 +/- 1.6 microM, respectively. Compounds 3-6 showed moderate activity against microtubule polymerization with IC50 values of 112 +/- 4, 131 +/- 3, 184 +/- 6 and 142 +/- 2 microM in vitro, respectively. Compounds 2, 3, 5 and 6 were moderately active against HIV-1 in vitro. The findings of bioactivity of 1-6 support the antifungus, antimitosis and anti-HIV-1 uses for W. indica roots.     

链霉菌JXJ-402产生的抗生素JXJ-402-1的研究

在筛选微生物来源抗生素的过程中，从500余株链霉菌中发现十余株抗真菌阳性菌株，其中JXJ-402菌株显示出较强的抗稻瘟病菌活性。从该菌株固体发酵粗提取物中分离纯化到化合物JXJ-402-1。经^13C-NMR数据分析，确定其化学结构与文献报道的尼日利亚菌素（nigericin）结构一致。生物学活性研究发现，化合物JXJ-402-1具有抗稻瘟病菌、赤星病菌、白念珠菌、藤黄微球菌和枯草芽孢杆菌等真菌和细菌活性，其中抗稻瘟病菌和赤星病菌活性未见文献报道。     

Zelkovamycin, a new cyclic peptide antibiotic from Streptomyces sp. K96-0670. I. Production, isolation and biological properties

A new antibiotic termed zelkovamycin was isolated from the fermentation broth of Streptomyces sp. K96-0670 by solvent extraction, ODS column chromatography and preparative HPLC. Zelkovamycin showed antibacterial activity against Xanthomonas oryzae, Acholeplasma laidlawii, Pyricularia oryzae and Staphylococcus aureus.     

Two new non-steroidal constituents from Dioscorea futschauensis R. Kunth

Dioscorone A (1) and a new isocoumarin derivative (2) were isolated from the rhizome of Dioscorea futschauensis R. Kunth. The structures of 1 and 2 were elucidated on the basis of detailed analysis of NMR spectra. Their anti-fungal activity against Pyricularia oryzae and cytotoxic activity on K562 and HCT-15 cell lines were evaluated in vitro.     

Bioactive saponins from Dioscorea futschauensis

A new anti-neoplastic spirostanol saponin, (25S)-spirost-5-en-3 beta, 27-diol-3O-[alpha-L-rhamnopyranosyl(1-->2)-beta-D-glucopyranosyl (1-->3)]-beta-D-glucopyranoside and three known compounds viz. prosapogenin A of dioscin, dioscin and gracilin were isolated from Dioscorea futschauensis by bioactivity-guided fractionation. Their structures were elucidated mainly by means of spectroscopic analysis. Their bioactivity against Pyricularia oryzae and cytotoxic activity on ts-FT210 cell line was evaluated.     

太平洋侧花海葵中的化学成分(Ⅲ)

目的　研究太平洋侧花海葵的活性成分。方法　采用稻瘟霉模型生物活性追踪方法 ,应用多种色谱技术进行分离 ,理化性质和波谱数据鉴定其结构。结果　分离并鉴定了 9个化合物 :正十六烷 ( ) ,正十三醇 ( ) ,棕榈酸 ( ) ,硬脂酸 ( ) ,棕榈酸甲酯 ( ) ,花生酸甲酯 ( ) ,1 - O-蜡酰甘油酯 ( )以及 2 S,3 R,Δ4 (E) ,Δ8(E) -十八碳鞘氨醇 -正十六碳酰胺和其同系物 2 S,3 R,Δ4 (E) ,Δ8(E) -十八碳鞘氨醇 -正十四碳酰胺的混合物 ( 和 ) ,其中 和 的混合物对稻瘟霉的最小菌丝变形浓度为 6 3 mg· L-1。结论　 9个化合物均为首次从该种海葵中获得 ,( 和 )具有诱导稻瘟霉菌丝变形活性     

A new bio-active flavonol glycoside from the stems of Butea superba Roxb

A new bio-active flavonol glycoside was isolated from the stems of Butea superba Roxb, and its structure was determined by spectral analysis and chemical degradations as 3,5,7,3',4'-pentahydroxy-8-methoxy-flavonol-3-O-beta-D-xylopyranosyl(1-->2) -alpha-L-rhamnopyranoside. The compound 1 showed antimicrobial activity against plant pathogenic fungi Trich viride, Asprgillus fumigatus, A. niger, A. terreus, Penicillium expansum, Helmitnhosporium oryzae, Botxitis cinerea, Rhizopus oligosporus, R. chinensis, Kelbsiella pneumoniae, Fusearium moniliforme and gram-positive bacteria Streplococcus pyogenes, Staphylococcus aureus, Bacillus subtilis gram-negative bacteria Escherichia coli, Proteus vulgaris, Klebsiella pneumoniae, Pseudomonas aeruginosa. The maximum inhibitory effect was shown by H. oryzae, A. niger, B. cinera and gram-positive bacteria.     

Bioactivity of Traditional Chinese Herbal Medicines Against Pyricularia oryzae

Two hundred and four species of traditional Chinese herbal medicines belonging to 80 families were collected from Yunnan Province in People’s Republic of China and tested for antifungal activities using a Pyricularia oryzae bioassay. Twenty-six herbal medicines from 23 families were active against P. oryzae and the ethanol extract of Dioscorea camposita (Dioscoreaceae) exhibited the most bioactivity among all the tested samples.     

Novel cytocidal antibiotics, glucopiericidinols A1 and A2. Taxonomy, fermentation, isolation, structure elucidation and biological characteristics

Two novel antibiotics, glucopiericidinols A1 (1) and A2 (2) were isolated from the cultured broth of Streptomyces sp. OM-5689. The structures of these two compounds were deduced employing spectroscopic analyses. These antibiotics showed potent cytocidal activities against HeLa S3 cells in vitro (MIC 1: 0.39 microgram/ml, 2: 0.10 microgram/ml) when the cells were exposed to the antibiotics for 3 days. Although 1 and 2 showed no activity at 1,000 micrograms/ml against various Gram-positive and Gram-negative bacteria, yeast or fungi, they did have inhibitory activity against Piricularia oryzae (MIC of 1: 125 micrograms/ml, of 2: 31 micrograms/ml).     

Cladospolide D, a new 12-membered macrolide antibiotic produced by Cladosporium sp. FT-0012

A new antibiotic termed cladospolide D was isolated along with the known cladospolides A and B from the fermentation broth of Cladosporium sp. FT-0012 by solvent extraction, ODS column chromatography and preparative HPLC. The structure of cladospolide D was deduced to be (E)-2-dodecen-5-hydroxy-11-olide-4-one. Cladospolide D showed antifungal activity against Pyricularia oryzae and Mucor racemosus.     

Two new triterpenoid saponins from Ardisia crenata

Two new triterpenoid saponins, ardisicrenoside K (1) and ardisicrenoside L (2), have been isolated from the roots of Ardisia crenata Sims. Their structures have been determined as 3beta-O-[alpha-L-rhamnopyranosyl-(1 --> 2)-beta-D-glucopyranosyl-(1 --> 4)-[beta-D-glucopyranosyl-(1 --> 2)]-alpha-L-arabinopyranosyl]-13beta,28-epoxy-16-oxo-30,30-dimethoxyoleanane and 3beta-O-[beta-D-xylopyranosyl-(1 --> 2)-beta-D-glucopyranosyl-(1 --> 4)-[beta-D-glucopyranosyl-(1 --> 2)]-alpha-L-arabinopyranosyl]-13beta,28-epoxy-16alpha,20-dihydroxyoleanane by means of chemical evidences and spectral analysis. Their weak anti-fungal activity against the plant pathogenic fungus Pyricularia oryzae was evaluated in vitro.     

Bioactive steroids from the brown alga Sargassum carpophyllum

By activity-guided fractionation, two new sterols, 3beta,28xi-dihydroxy-24-ethylcholesta-5,23Z-dien (1) and 2a-oxa-2-oxo-5alpha-hydroxy-3,4-dinor-24-ethylcholesta-24(28)-ene (2), together with five known steroids, fucosterol (3), 24-ethylcholesta-4,24(28)-dien-3,6-dione (4), 24xi-hydroperoxy-24-vinylcholesterol (5), 24-ketocholesterol (6), 24R,28R- and 24S, 28S-epoxy-24-ethylcholesterol (7), were isolated from the brown alga Sargassum carpophyllum as active compounds causing morphological abnormality of Pyricularia oryzae mycelia. Compounds 1, 3, 4, 5 and 7 also exhibited cytotoxic activity against various cancer cell lines. The IC50 values for 1 and 5 against HL-60 were 7.8 and 8.5 microg/ml, 3 and 4 against P-388 were 0.7 and 0.8 microg/ml, whereas 7 against MCF-7, HCT-8, 1A9, HOS and PC-3 were 4.0, 8.8, 10.0, 10.0 and 7.2 microg/ml, respectively.     

利用生物模型-稻瘟霉筛选活性菌株

目的从土壤真菌中筛选有抗真菌、抗肿瘤活性的菌株。方法以稻瘟霉分生孢子以及菌丝形态变化为指标 ,并通过稳定性考查 ,进行活性筛选。结果从云南、江西等地土壤中分离出 737株真菌 ,对其中的 14 2株活性菌株进行多次反复筛选 ,从中得到 6株活性、批次稳定性和遗传稳定性良好的菌株。进行温度稳定性考查的过程中发现多色青霉、黑粘座曲霉、产紫青霉三株菌发酵液活性基本不受温度影响。结论稻瘟霉是良好的筛选抗真菌、抗肿瘤活性菌株的初筛模型     

抗稻瘟霉中草药活性筛选

目的从广西产中草药中筛选具有抗稻瘟霉活性的中草药。方法利用稻瘟霉模型筛选中草药。结果 12个科的 18种中草药呈现出较好的抗稻瘟霉活性。结论抗稻瘟霉模型是一个很好的活性筛选体系 ,可以用于抗癌药物的初筛     

产紫青霉中的活性成分

从陕西省采集的土样中分离得到产紫青霉 (Penicillium purpurogenumStoll) ,从其发酵液乙酸乙酯萃取物中分离得到两个化合物 ,经过光谱数据的分析鉴定为 :3 (1′ 羧基乙烯氧基 )苯甲酸和间羟基苯甲酸 ,并利用稻瘟霉 (Pyriculariaoryzae)菌丝体形态变化作为活性指标 ,测定了它们的活性     

New furostanol glycosides from the rhizomes of Dioscorea futschauensis R. Kunth

Two new furostanol glycosides, 26-O-beta-D-glucopyranosyl-3beta,26-dihydroxy-23(S)-methoxyl-25(R)-furosta-5,20(22)-dien-3-O-alpha-L-rhamnopyranosyl(1 --> 2)-[beta-D-glucopyranosyl(1 --> 3)]-beta-D-glucopyranoside (dioscoreside E, 1) and 26-O-beta-D-glucopyranosyl-3beta,26-dihydroxy-25(R)-furosta-5,20(22)-dien-3-O-alpha-Lrhamnopyranosyl(1 --> 2)-[beta-D-glucopyranosyl (1 --> 3)]-beta-D-glucopyranoside (prtotogracillin, 2), together with 11 known furostanol glycosides were isolated from the rhizomes of Dioscorea futshauensis R. Kunth. Their structures were elucidated on the basis of spectroscopic analysis (NMR and FABMS). Their anti-fungal activity against the plant pathogenic fungus Pyricularia oryzae and cytotoxic activity on K562 cancer cell line were evaluated in vitro.     

太平洋侧花海葵中四个新神经酰胺的鉴定太平洋侧花海葵中四个新神经酰胺的鉴定

目的研究太平洋侧花海葵(Anthopleura pacifica)中的生物活性成分。方法采用稻瘟霉模型生物活性追踪方法,应用色谱技术进行分离,根据理化性质和波谱分析鉴定结构。结果得到了1个对稻瘟霉显示活性的组分,并鉴定为4个神经酰胺的混合物:N-羟乙基-N-十四酰-(2S,3R)-十八碳鞘氨醇-4(E),8(E)-二烯(a),N-羟乙基-N-(9Z-十六烯酰)-(2S,3R)-十八碳鞘氨醇-4(E),8(E)-二烯(b),N-羟乙基-N-十六酰-(2S,3R)-十八碳鞘氨醇-4(E),8(E)-二烯(c)和N-羟乙基-N-(13Z-二十二烯酰)-(2S,3R)-十八碳鞘氨醇-4(E),8(E)-二烯(d)。结论化合物a～d均为新的神经鞘氨醇化合物。     

Two new bioactive triterpene glycosides from the sea cucumber Pseudocolochirus violaceus

By activity-guided fractionation, two new triterpene glycosides, violaceusides A (1) and B (2), were isolated from the sea cucumber Pseudocolochirus violaceus as active compounds causing morphological abnormality of Pyricularia oryzae mycelia. By extensive 2D NMR techniques and chemical evidence, the structures of the two new glycosides were established as 16beta-acetoxy-3-O-[3-O-methyl-beta-D-glucopyranosyl-(1 --> 3)-beta-D-xylopyranosyl-(1 --> 4)-beta-D-quinovopyranosyl-(1 --> 2)-4-O-sodiumsulphate-beta-D-xylopyranosyl]-holosta-7,24-diene-3beta-ol (1) and 16beta-acetoxy-3-O-[3-O-methyl-beta-D-glucopyranosyl-(1 --> 3)-beta-D-xylopyranosyl-(1 --> 4)-beta-D-glucopyranosyl-(1 --> 2)-4-O-sodiumsulphate-beta-D-xylopyranosyl]-holosta-7,24-diene-3beta-ol (2), respectively. The two glycosides also exhibited significant cytotoxicity against HL-60 and BEL-7402 cancer cell lines.     

A new ergostanol saponin from Dioscorea deltoidea Wall var. orbiculata

From the fresh rhizomes of Dioscorea deltoidea Wall var. orbiculata , a novel ergostanol saponin, orbiculatoside A ( 1 ), was isolated and identified as 3- O - g - d -glucopyranosyl-ergost-5-ene-3 g , 26-diol-26- O - g - d -glucopyranosyl(1 M 3)-[ g - d -glucopyranosyl(1 M 2)- g - d -glucupyranosyl(1 M 6)]- g - d -glucopyranoside by various NMR techniques in combination with chemical methods. The new saponin showed strong activity against Pyricularia oryzae , with a MMDC (minimum morphological deformation concentration) value of 28.04 w mol/l and was cytotoxic to cancer cell line K562, HCT-15, A549, HT1080, and A2780a in vitro .