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Desotamides A, a cyclohexapeptide produced by the deep-sea-derived Streptomyces scopuliridis SCSIO ZJ46, displays notable antibacterial activities against strains of Streptococcus pnuemoniae, Staphylococcus aureus, and methicillin-resistant Staphylococcus epidermidis (MRSE). In this study, to further explore its antibacterial potential and reveal the antibacterial structure-activity relationship of desotamides, 13 cyclopeptides including 10 new synthetic desotamide A analogues and wollamides B/B1/B2 were synthesized and evaluated for their antibacterial activities against a panel of Gram-positive and -negative pathogens. The bioactivity data reveal that residues at position II and VI greatly impact antibacterial activity. The most potent antibacterial analogues are desotamide A4 (13) and A6 (15) where l-allo-Ile at position II was substituted with l-Ile and Gly at position VI was simultaneously replaced by d-Lys or d-Arg; desotamides A4 (13) and A6 (15) showed a 2–4-fold increase of antibacterial activities against a series of Gram-positive pathogens including the prevalent clinical drug-resistant pathogen methicillin-resistant Staphylococcus aureus (MRSA) with MIC values of 8–32 μg/mL compared to the original desotamide A. The enhanced antibacterial activity, broad antibacterial spectrum of desotamides A4 and A6 highlighted their potential as new antibiotic leads for further development. 相似文献
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旨在考察鼠源抗菌肽CRAMP的安全性、稳定性及其在清除铜绿假单胞菌生物被膜中的作用。采用兔血红细胞悬液的溶血性和小鼠腹腔巨噬细胞(RAW264.7)的细胞毒性考察CRAMP的安全性;采用不同温度、蛋白酶、金属离子和酸碱梯度对CRAMP抗菌活性的影响,考察其稳定性;通过在6孔细胞培养板中构建铜绿假单胞菌(PAO1株)成熟生物被膜,以人源抗菌肽LL-37和3种抗菌药为对照,采用结晶紫染色法检测生物被膜量,平板菌落计数法对生物被膜活菌数进行计数,苯酚-硫酸法结合Folin-酚试剂法检测生物被膜胞外基质含量,激光扫描共聚焦显微镜(CLSM)观察CRAMP干预PAO1生物被膜形态学的变化。结果显示,CRAMP在所测试浓度下对兔血红细胞溶血率均<2%;在62.5~125 mg·L-1时对 RAW264.7没有细胞毒性。温度(25~100 ℃)、两种盐离子(Na+、K+)以及pH为5~10时对CRAMP的抗菌活性没有影响;胃蛋白酶、木瓜蛋白酶、胰蛋白酶均不同程度影响了CRAMP的抗菌活性。6孔细胞培养板中,4倍MIC 的CRAMP极显著降低了PAO1生物被膜量(减少率为76.74%,P<0.01),极显著减少了生物被膜中的活菌数量(减少了1.2个CFU·mL-1,P<0.01),效果优于LL-37和3种抗菌药。CRAMP组的胞外基质显著低于空白对照组和LL-37组(P<0.05)。CLSM结果显示:与对照组相比较,4MIC浓度下,CRAMP组的细菌总荧光强度(PI+SYTO)显著低于空白对照组和LL-37组(P<0.05);与空白对照组相比,CRAMP组和LL-37组的死菌荧光强度/活菌荧光强度比值 (PI/SYTO)均极显著增大(P<0.01)。综上表明,CRAMP具有低溶血性、低细胞毒性,除蛋白酶作用不稳定外,具有较好的稳定性,对PAO1成熟生物被膜具有明显的清除作用,且效果优于LL-37,具有良好的药物开发前景。 相似文献
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本研究以南美白对虾为研究对象,探究饲料中天蚕素抗菌肽的合适添加量。在饲料中依次添加不同浓度水平(0%、1%、2%、3%、4%和5%)的天蚕素抗菌肽,配制为6种配合饲料,用以投喂南美白对虾,饲养周期8周。结果显示:与对照组相比,饲料中添加天蚕抗菌肽对南美白对虾增重率、蛋白质沉积率和特定生长率有显著影响(P<0.05),高水平天蚕素抗菌肽会抑制南美白对虾的增重率和特定生长率,南美白对虾的饵料系数显著下降,但对南美白对虾存活率和摄食率无显著影响(P>0.05)|随着饲料中天蚕素抗菌肽的添加水平不断增加,3%组南美白对虾的ACP、POD和SOD含量达到最大水平,与对照组有明显差异(P<0.05)|随着饲料中天蚕素抗菌肽的添加水平的不断上升,3%组南美白对虾的淀粉酶、脂肪酶和胃蛋白酶含量最高,与对照组存在明显差异(P<0.05)。结果表明,饲料中添加天蚕素抗菌肽显著提高南美白对虾的增重率和特定生长率,提高南美白对虾的生长发育速度,从而增强机体免疫力,提高南美白对虾的抗病能力。
[关键词]天蚕抗菌肽|南美白对虾|抗病力|免疫功能 相似文献
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阔叶树小径材热压干燥工艺的研究 总被引:2,自引:0,他引:2
通过对荷木和米槠两种华南地区常用阔叶树小径材薄板材热压干燥工艺的研究,探讨热压干燥工艺参数对小径材板材干燥质量(包括密度,厚度压缩率,尺寸稳定性及部分力学性能)的影响,试验结果表明,热压干燥工艺可以大大改善小径材的物理力学性能。 相似文献
139.
Vegetation dynamics in previously burnt shrublands dominated by gorse (Ulex gallii) in north-west Spain were studied during 4 years under different grazing managements with sheep (Gallega breed) and goats
(Cashmere or local breed). Initially (Period 1), treatments consisted of sheep or goat grazing on four plots (two replicates).
After two grazing seasons, the plots were split in two and the treatments were reversed in four of the subplots; sheep were
placed in subplots previously grazed by goats and vice versa (Period 2). The results from Period 1 showed that goats control
the regrowth of gorse (from 19.6 to 14.2% of cover) more effectively than sheep (17.8 to 27.0% cover; P < 0.05), favouring the increase in herbaceous plants (from 21.5 to 42.1% of cover under goat grazing and from 22.1 to 26.6%
under sheep grazing; P < 0.01). In Period 2, after changing treatments, there was a clear effect of the previous management (P < 0.01), conditioning the dynamics of the different plant components. Where the same animal species were maintained for 4 years,
the differences between sheep or goat grazing on gorse and herbaceous plant dynamics increased (24.4% of gorse and 35.2% of
herbaceous plant cover under goat grazing vs 43.8% of gorse cover and 19.1% of herbaceous plant cover under sheep grazing).
Animal species change buffered the differences between sheep and goats during the second Period. 相似文献
140.
The road effect on small rodent population is investigated at 8 fragmented forest areas in the Baekdudaegan moun-tain range, South Korea in September 2001, We especially focused on the distribution and body condition of small rodents near the roads, Korean field mouse (Apodemus peninsulae) seems to be more sensitive to the existence of a road than striped field mouse (Apodemus agradus), Korean field mouse prefers interior forest area to around road. Striped field mouse is a habitat generalist and has wide distributional range around road, but Korean field mouse is forest-inhabiting species and their distribu-tion is limited in forest area. These results suggest the effect of road is different on each small rodent species and their habitat preferences. 相似文献