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1.
目的 柳珊瑚来源真菌Penicillium chrysogenum中聚酮-萜类化合物citrehybridonol及其晶体结构和生物活性研究。方法 利用核磁、质谱等现代波谱分析方法和X-ray单晶衍射技术,对citrehybridonol的化学结构进行研究;运用细胞毒活性和抗菌活性模型对其生物活性进行评价。结果 citrehybridonol为首次获得其晶体,并首次对其单晶数据进行报道。生物活性测试结果表明,该化合物对测试的细菌菌株未显示抗菌活性,对肿瘤细胞株未见细胞毒活性。结论 citrehybridonol的单晶数据以及活性数据对今后系统研究聚酮-萜类化合物具有参考价值。  相似文献   

2.
摘 要:目的 研究从花柳珊瑚共附生真菌Arthrinium sp.分离得到的1-甲基-2,3,6,8-四羟基氧杂蒽酮(1)和1-甲基-2,3,4,6,8-五羟基氧杂蒽酮(2)的化学结构及其抗细菌和抗病毒活性。方法 利用现代波谱解析方法和X-ray单晶衍射技术,对化合物1和2的化学结构进行研究;利用抗细菌和抗病毒活性模型对其生物活性进行评价。结果 化合物1的结构首次通过单晶数据进一步确定;体外化合物1显示抗病毒活性,化合物1的IC50值为27.40 μM,强于阳性药利巴韦林的抗HSV活性(IC50 = 313.00 μM)。结论 化合物1的单晶数据、以及活性数据对今后系统研究氧杂蒽酮类化合物具有参考价值。  相似文献   

3.
目的 对一株海洋来源真菌 Nigrospora sp. (TA26-9) 中的蒽醌类化合物进行结构表征,筛选评价生物活性。方法 采用波谱分析方法和单晶衍射技术对化合物进行结构表征,采用微量稀释法测定化合物对 10 株致病菌的抗菌活性,采用 Solis 改良法测定化合物的卤虫致死活性。结果 结构表征确定了 6 个蒽醌类化合物的结构:9α-hydroxydihydrodesoxybostrycin (1),9α-hydroxyhalorosellinia A (2),4-deoxybostrycin (3),bostrycin (4),3,5,8-trihydroxy-7-methoxy-2-methylanthracene-9,10-dione (5) 和austrocortirubin (6)。对化合物 1–6 及其乙酰化衍生物 3a,4a,5a–5d 生物活性评价表明,所有化合物对辣椒炭疽病菌 Colletotrichum capsici 都有选择性抗菌活性,MIC = 0.26–1.22 μM;除化合物 3 外,对玉米大斑病菌 Setosphaeria turcica 也表现出很好的抗菌活性,MIC = 0.27–4.82 μM。特别地,化合物 3a具有广谱抗菌活性,对 8 株致病菌的 MIC 在 0.27–4.32 μM之间,该化合物还显示卤虫致死活性,在 25 μg/mL 浓度下对卤虫 Artemia salina 的致死率为 78.9%。结论 海洋来源真菌 Nigrospora sp. (TA26-9) 中的蒽醌类化合物具有选择性抗菌活性,具有开发成抗菌剂的潜力。  相似文献   

4.
《中国海洋药物》2011,30(4):25-28
目的研究中国南海直针小尖柳珊瑚Muricella abnormalis的化学成分。方法利用硅胶柱层析、Seph-adex LH-20凝胶柱层析、PHPLC等方法对化合物进行分离纯化;利用NMR,MS等波谱方法,并与文献对照,确定化合物的结构;利用卤虫致死活性模型和斑马鱼胚胎毒性模型评价化合物的生物活性。结果从直针小尖柳珊瑚中分离得到6个单体化合物,分别为:倍半萜1-formyl-4-methyl-7-isopropylazulene(1),3-guaia-zulenecarbaldehyde(2),ketolactone(3),胆甾醇(4),甘油醚chimyl alcohol(5)和正十八烷醇(6)。结论化合物2为新天然产物,其余化合物均为首次从该种柳珊瑚中分离得到。化合物2具有较强的卤虫致死活性和斑马鱼胚胎毒性。  相似文献   

5.
摘要:目的 在生物活性和化学方法指导下,从1株海兔来源真菌 Aspergillus terreus (RA29-5)中分离鉴定海洋天然产物,并对其进行生物活性评价。方法 运用硅胶柱层析、Sephadex LH-20凝胶柱层析和HPLC等方法分离纯化化合物,利用NMR等现代波谱分析方法,对化合物进行结构鉴定,并对化合物进行抗菌、卤虫致死和斑马鱼胚胎毒性活性评价。结果 鉴定了 9 个丁内酯类化合物 (1~9) 的结构;抗菌活性表明,除化合物 6 和 9 外,所有化合物对四株致病细菌白色葡萄球菌 Staphylococcus epidermidis、金黄色葡萄球菌 Staphylococcus aureus、蜡状芽孢杆菌 Bacillus subtilis 和四联球菌 Tetragenococcus halophilus 都显示一定的抗菌活性;化合物 1~4 和7均对真菌芒果叶枯菌 Pestalotia mangiferae 显示抗菌活性;特别的,化合物 7 对测试的13株致病菌都具有广谱地抗菌活性,其MIC值在1.11~8.88 μmol/L之间;此外,还对化合物的抗菌活性构效关系进行了初步探讨。结论 海兔来源真菌 A. terreus (RA29-5) 可产生结构多样的丁内酯类化合物,该类化合物具有开发成抗菌剂的潜力。  相似文献   

6.
目的 从中国南海花柳珊瑚来源真菌 Aspergillus candidus (RA16-10) 中分离鉴定具有生物活性的代谢产物。方法 运用硅胶柱层析、Sephadex LH-20凝胶柱层析和半制备HPLC等方法分离并分析化合物,运用核磁、质谱等现代波谱分析方法对化合物进行结构鉴定,并对化合物进行抗菌、卤虫致死、藤壶幼虫致死等活性评价。结果 从 Aspergillus candidus中分离鉴定了3个黄酮类化合物 (1~3) 和1个三联苯类化合物 (4) ,其中含有氯原子的黄酮类化合物 1 和3是自然界中极其罕见的化合物;化合物 1 和2 显示出强的藤壶幼虫Balanua amphitrite致死活性,其LC50值分别为1.11 μg/mL和1.39 μg/mL,这是首次报道该类化合物的藤壶幼虫致死活性。结论 从中国南海花柳珊瑚来源真菌Aspergillus candidus (RA16-10) 中筛选发现了2个具有显著的藤壶幼虫B. amphitrite致死活性的黄酮类化合物,这类化合物具有开发成为防污剂的潜力。  相似文献   

7.
目的 研究皱瘤海鞘 Styela plicata 具有卤虫致死活性的乙醇提取物的化学成分。方法95%乙醇 (v/v) 粗浸膏用乙酸乙酯萃取后得乙酸乙酯相,运用硅胶柱层析、Sephadex-LH20凝胶柱层析法和高效液相色谱 (HPLC) 对其进行分离纯化。运用核磁共振,质谱等波谱学方法对分离所得化合物的结构进行鉴定,并对化合物进行卤虫活性测试。结果 从皱瘤海鞘乙醇提取物中分离得到 6个化合物,结构分别鉴定为两个比较少见的吡喃酮类化合物 tetillapyrone (1) 和 nortetillapyrone (2),两个核苷类化合物 thymidine (3) 和 uracil (4), 以及两个多羟基甾醇类化合物 dendronesterol A (5) 和 (20S, 22E, 24R)-ergosta-7, 22-dien-3β, 5α, 6β-triol (6)。卤虫致死活性结果显示,多羟基甾醇类化合物 5 和 6 的活性较强,而核苷类化合物 3 和 4 的活性较弱。结论 所有化合物均为首次从该海鞘中分离获得,本研究为进一步研究开发皱瘤海鞘中的活性物质提供基础资料。  相似文献   

8.
目的研究中国南海侧扁软柳珊瑚Subergorgia suberosa的次级代谢产物。方法利用硅胶柱层析、Sephadex LH-20凝胶柱层析、HPLC等方法对化合物进行分离纯化;利用NMR,MS等波谱方法,并与文献对照,鉴定化合物的结构;利用抗菌活性模型和卤虫致死活性模型评价化合物的生物活性。结果从侧扁软柳珊瑚中分离鉴定了6个单体化合物,分别为:倍半萜化合物subergorgic acid(1),2-β-hydroxysubergorgic acid(2)和2-β-acetoxysubergorgic acid(3);甾体化合物3β-hydroxy-5α-pregnan-20-one(4),5α-pregnane-3,20-di-one(5)和胆甾醇(6)。结论化合物1~3对白色葡萄球菌Staphylococcus albus均显示出较强的抑制活性,化合物4对蜡状芽孢杆菌Bacillus cereus显示出较强的抑制活性,而化合物4和5显示出较强的卤虫致死活性。  相似文献   

9.
目的对一株中国南海枝网刺柳珊瑚Echinogorgiasp.共附生真菌Peniophorasp.的次级代谢产物及生物活性进行研究。方法利用硅胶柱层析、凝胶柱层析、重结晶和半制备HPLC等方法,对发酵产物乙酸乙酯相进行分离纯化;采用NMR、MS等波谱分析方法并结合文献数据,鉴定化合物的结构;通过卤虫致死活性模型和斑马鱼胚胎毒性模型评价化合物的生物活性。结果从真菌Peniophorasp.中分离得到7个甾体化合物,分别鉴定为:4-hydroxy-17R-methylincisterol(1),麦角甾醇(2),(3β,5α,6β,22E)-6-甲氧基麦角甾-7,22-二烯-3,5-二醇(3),酒酵母甾醇(4),麦角甾-4,6,8,22-四烯-3-酮(5),过氧化麦角甾醇(6)和9(11)-脱氢过氧化麦角甾醇(7)。结论化合物1显示出较强的卤虫致死活性,在25μg.mL-1浓度下,对卤虫Artemia salina的致死率为88.4%;化合物4显示较强的鱼毒活性,对斑马鱼Danio rerio胚胎脊索畸形毒性的EC50值为7.83μg.mL-1(72h)。  相似文献   

10.
目的 从采自中国黄海的威海海域的柄海鞘来源放线菌Streptomyces coelicoflavus(HQA809) 和史氏菊海鞘来源放线菌Nocardiopsis dassonvillei(HQA404) 中分离、鉴定具有生物活性的次级代谢产物。方法 运用硅胶柱层析、Sephadex LH-20凝胶柱层析和半制备HPLC等方法分离化合物,运用核磁、质谱等现代波谱分析方法对化合物进行结构鉴定,并对化合物进行抗菌、卤虫致死、α-糖苷酶抑制活性和细胞毒活性评价。结果 从 Streptomyces coelicoflavus(HQA809) 中分离鉴定了2个吡喃酮类化合物 (1,2),从 Nocardiopsis dassonvillei(HQA404) 中分离鉴定了1个吩嗪类化合物 (3) 和1个苯酚类化合物 (4);化合物3对鳗弧菌 (Vibrio anguillarum) 和副溶血弧菌 (Vibrio parahaemolyticus) 显示出较强的抑菌活性,其MIC值分别为50 μmol/L和25 μmol/L。结论 海鞘来源放线菌可以作为发现新颖的生物活性物质的潜在来源。  相似文献   

11.
《Pharmaceutical biology》2013,51(4):439-445
We used an alkaloid test and a brine shrimp bioassay to assess the bioactivity of the medicinal plants used by eastern Nicaraguan healers in traditional medicine. Ethnomedicinal uses were obtained from interviews of traditional healers. Aqueous extracts derived from 30 species of angiosperms were assayed for the presence of alkaloids and toxicity. Species tested are distributed in 30 genera and 21 families. Of the 30 species tested for alkaloids with Dragendorff’s reagent, 29 contained alkaloids. Toxicological analysis was conducted using the brine shrimp lethal assay (BSLA). Biological activity using BSLA was recorded as the median lethal concentration (LC50) that kills 50% of the larvae within 24?h of contact with the aqueous plant extracts. The LC50 of the shrimp was less than 2500 µg/mL for 3 (10%) species, 2500-5000 µg/mL for 9 (30%), 5001-7500 µg/mL for 7 (23%), 7501-10000 µg/mL for 3 (10%), and greater than 10000 µg/mL for 8 (27%) of the species. The members of the orders Santales and Rubiales in general contained species with greater toxicity than any other group. Struthanthus cassythoides (Struthanthus cassythoides Millsp.(Loranthaceae)). (LC50 1574 µg/mL) and Alibertia edulis (Rich.) A. Rich. (Rubiaceae) (LC50 1741 µg/mL) were the most toxic.  相似文献   

12.
Paeciloside A (1) and eight known compounds, acremoauxin A (2), farinosones A (3) and B (4), 1,5-dideoxy-3-C-methyl-arabitol (5), ergosterol, ergosterol peroxide, cerebroside C, and adenosine, were isolated from cultures of Paecilomyces sp. CAFT156, an endophytic fungus occurring in Enantia chlorantha Oliv (Annonaceae) leaves. The structure of the new compound 1 was elucidated using MS, UV, 1D and 2D NMR experiments, while its absolute configuration was established by subsequent single-crystal X-ray diffraction analysis using copper Kα radiation and invariom nonspherical scattering factors. Paeciloside A (1) and compounds 2, 4, and 5 displayed inhibitory effects on two gram-positive bacteria, Bacillus subtilis and Staphylococcus aureus at a concentration of 40 μg per paper disk and moderate cytotoxicity towards brine shrimp larvae (Artemia salina). This study presents the first report on an endophytic fungus isolated from E. chlorantha Oliv and its natural products.  相似文献   

13.
《Pharmaceutical biology》2013,51(1):101-104
The methanol extract of Vernonia cinerea Less (Asteraceae), which exhibited antimicrobial activity, was tested for toxicity. In an acute toxicity study using mice, the median lethal dose (LD50) of the extract was greater than 2000?mg/kg, and we found no pathological changes in macroscopic examination by necropsy of mice treated with extract. As well as the oral acute toxicity study, the brine shrimp lethality test was also done. Brine shrimp test LC50 values were 3.87?mg/mL (6?h) and 2.72?mg/mL (24?h), exhibiting no significant toxicity result. In conclusion, the methanol extract of V. cinerea did not produce toxic effects in mice and brine shrimp.  相似文献   

14.
南极微生物的分离及抗肿瘤活性筛选   总被引:5,自引:1,他引:5  
对南极地区(南极大陆、潮间带、南大洋)的海水、海泥、土壤、植物样品进行了微生物分离,并采用海虾生物致死法和流式细胞术对极地微生物发酵产物进行了抗肿瘤活性筛选。从南极样品中共分离极地微生物259株,筛选结果显示,11%的微生物具有显著的抗肿瘤活性,显示出极地微生物在活性物质研究方面具有良好的应用潜力。  相似文献   

15.
cis-Annonacin (1) and the mixture of (2,4)-cis-and trans-isoannonacins (2 and 3), three known mono-tetrahydrofuran annonaceous acetogenins, have been isolated from the seeds of Annona cherimolia by the use of the brine shrimp lethality test (BST) for bioactivity directed fractionation. Their structures were elucidated based on spectroscopic and chemical methods. 1 showed potent cytotoxicities in the brine shrimp lethality test (BST) and among six human solid tumor cell lines with notable selectivity for the pancreatic cell line (PaCa-2) at about 1,000 times the potency of adriamycin. The mixture of 2 and 3 is over 10,000 times cytotoxic as adriamycin in the pancreatic cell line (PaCa-2). All of the compounds are about 10 to 100 times as cytotoxic as adriamycin in the prostate cell line (PC-3).  相似文献   

16.
Extracts of the leaves, twigs, stems and roots of Lantana camara Linn. (Verbenaceae) were solvent-partitioned and screened for activity in the brine shrimp lethality test (BST). The active fractions yielded known oleanonic acid (1), lantadene A (2) and oleanolic acid (3), which were very toxic to brine shrimp larvae. Compounds 1-3 were not lethal to Spodoptera littoralis Biosduval (Lepidoptera: Noctuidae), Clavigralla tomentosicollis Stal. (Hemiptera: Coreidae) and Aphis craccivora Koch (Homoptera: Aphididae) when tested at 5000µg/ml. Compound 2, however, suppressed the fecundity of C. tomentosicollis at this concentration.  相似文献   

17.
The roots of Laportea crenulata Gaud (Urticacae) were collected in Bangladesh and the bioactivity was evaluated by two bioassays. The brine shrimp lethality test and the antibacterial activity were conducted on the different organic solvent root extracts of this plant. In addition minimal inhibitory concentration (MIC) was determined using serial dilution technique. On the brine shrimp lethality bioassay, the petroleum ether, chloroform, and methanol extracts of roots of L. crenulata displayed LC50 values of 20.87, 14.43, and 31.02 μ g/ml respectively. Furthermore, the antibacterial assay on these extracts indicated activity against several pathogenic bacteria. The MIC values against Escherichia coli, Shigella dysenteriae, Salmonella typhi, Bacillus subtilis, and Streptococcus-β -haemolyticus were ranged from 32 to 128 μ g/ml. The positive results on these bioactive extracts should encourage the further investigation of the active principles responsible for these activities.  相似文献   

18.
S T Hahn  J M O'Connor 《Toxicon》2000,38(1):79-89
Bullrout envenomation is known to cause intense pain. Crude bullrout venom and venom fractions were assessed for protease, hyaluronidase, phospholipase and hemolytic activities, reactivity with stonefish antivenom, lethality to brine shrimp and ability to elicit pain in human subjects. Compared with venom obtained from frozen specimens, live fish venom-milking techniques rendered greater venom potency and improved storage characteristics. Although mild proteolytic and hemolytic activity was observed, crude venom demonstrated no hyaluronidase or phospholipase A2 activity, did not affect brine shrimp, or show antigenicity with stonefish antivenom. A single venom protein isolated from bullrout venom is attributed with causing pain in human subjects. The sensations elicited by this novel algesic protein are consistent with chemical stimulation of polymodal nociceptors.  相似文献   

19.
New derivatives of quinoline (CAS 91-22-5, Z-1) were synthesized and their potential therapeutical significance and structure-activity relationship were tested. The brine shrimp bioassay was carried out to study their in vitro cytotoxicity, and besides, also their antimicrobial, antifungal and cardiovascular activities were investigated. Some structures showed a high degree of activity on the isolated rabbit jejunum. Extensive spectroscopic techniques such as EIMS, FABMS, peak matching MS, UV, IR and 1H NMR were employed to confirm the structure of the synthetic products.  相似文献   

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