木麻黄树皮载金属离子造纸抗菌剂的制备

以木麻黄树皮为载体制备负载锌、铜金属离子的抗菌剂,探讨了木麻黄树皮载金属抗菌剂对大肠杆菌、金黄色葡萄球菌的抑制作用,并考察了木麻黄树皮载金属抗菌剂在纸张中的应用性能。结果表明,铜、锌离子对大肠杆菌、金黄色葡萄球菌均有很好的抑菌效果,当离子浓度为5 mg/m L时,抑菌圈直径分别为17.1 mm、11.2 mm;木麻黄树皮对金属离子具有很好的负载量,木麻黄树皮载金属离子抗菌剂对大肠杆菌、金黄色葡萄球菌具有很好的抑制作用;随着木麻黄树皮中金属离子含量的增大,对大肠杆菌、金黄色葡萄球菌的抑制作用越明显;木麻黄树皮载金属抗菌剂在纸张中的添加量20%、30%时,抗菌纸张对大肠杆菌、金黄色葡萄球菌的抑菌圈的直径分别由12.7 mm增加到17.9 mm、8.4 mm增加到12.7 mm。     

载银油茶果壳抗菌剂的制备和性能

考察银离子浓度、pH、温度、时间等制备条件对油茶果壳载银抗菌剂性能的影响,并考察了材料对大肠杆菌、金黄色葡萄球菌的抑制效果。结果表明:油茶果壳载银抗菌剂的最佳制备条件为吸附时间6 h,搅拌温度35℃,pH=4,银离子浓度是0.2 mol/L,制备的油茶果壳载银抗菌剂对大肠杆菌、金黄色葡萄球菌具有优异的抗菌性能。     

基于聚谷氨酸囊泡的抗菌水凝胶

通过开环聚合(ROP)合成了两亲嵌段共聚物聚己内酯-聚谷氨酸(PCL-b-PGA),并将其自组装成囊泡,然后利用聚谷氨酸的羧基原位沉积纳米银颗粒,得到了抗菌囊泡. 最后,将抗菌囊泡与普朗尼克F127基体混合,制备了抗菌水凝胶. 实验结果表明抗菌囊泡对典型革兰氏阴性菌如大肠杆菌和典型革兰氏阳性菌如金黄色葡萄球菌的MIC90(抑制90%菌株生长的最低浓度)分别为10和20 μg mL?1. 平板菌落计数法表明抗菌水凝胶对大肠杆菌和金黄色葡萄球菌的MIC50(抑制50%菌株生长的最低浓度)为30 μg mL?1,MIC90为60 μg mL?1. 外敷法抗菌实验也证明了水凝胶具有优异的抗菌效果,其对大肠杆菌和金黄色葡萄球菌的MIC50为7.5 μg mL?1,MBC(最小杀菌浓度)为30 μg mL?1.     

含噻唑烷二酮-3-乙酸结构查尔酮衍生物的合成及抗菌活性的研究

合成了一系列含噻唑烷二酮-3-乙酸结构的新型查尔酮衍生物,并对化合物进行了抗菌活性测定.结果显示,一些化合物对4种多重耐药菌显示出较强的抗菌活性,其中化合物8g,8i,8l和8m在抗耐甲氧西林金黄色葡萄球菌的最小抑制浓度(MIC)达到4μg/mL,与对照药诺氟沙星(norfloxacin)相当.另外,在64μg/mL浓度下,所有化合物对大肠杆菌1356均无明显抑制活性.     

高活性铈银介孔复合抗菌剂的制备

利用分步浸渍法制备了Ce银介孔复合无机抗菌剂,并对其进行XRD,TEM,N2吸脱附等表征,结果显示,该抗菌剂仍然保持有序介孔结构,活性物种Ag以纳米线状稳定存在于孔道内。运用抑菌圈法和最小抑菌浓度法对其抗菌性能进行了评价,测试表明,该样品对金黄色葡萄球菌和大肠杆菌均有着优良的抑杀效果。这是由于抗菌活性物种Ag高度分散在介孔材料孔道中,以及Ce有促进Ag＋产生羟基自由基,因而能强化Ag的抗菌性能的原因。     

具有高效阳性菌抗菌活性的合成多肽聚合物研究

合成了具有抗菌活性的β-氨基酸聚合物,采用核磁共振和凝胶渗透色谱表征聚合物的数均分子量,通过最低抑菌浓度实验测试了β-氨基酸聚合物对多种革兰氏阳性菌(包括多株耐药菌)的抗菌活性,并开展了可能的耐药性研究。通过细胞膜去极化实验和扫描电子显微镜探究了抗菌聚合物对革兰氏阳性菌,尤其是对耐甲氧西林金黄色葡萄球菌的抗菌机理。结果表明,β-氨基酸聚合物通过作用于细菌的细胞膜杀死革兰氏阳性菌从而获得高效的抗菌活性,其对枯草芽孢杆菌的抗菌活性最好,最低抑菌浓度为3.13μg/mL。金黄色葡萄球菌对β-氨基酸聚合物不产生耐药性,但在相同条件下测试的对照抗生素诺氟沙星的最低抑菌浓度增加了124倍,表明细菌对抗生素很快产生了耐药性。     

新型高分子季鏻盐改性抗菌塑料的制备及性能研究

高分子季鏻盐抗菌剂具有安全、高效的特点,使用过程中不会通过皮肤组织进行渗透。本文将实验室自制的新型高分子季鏻盐抗菌剂粉末与低密度聚乙烯(LDPE)基体材料共混,通过熔融挤出法制备了含梯度浓度抗菌剂的抗菌塑料,研究了不同抗菌剂添加浓度对基体材料熔融性质及其抗菌性能的影响,并探讨了抗菌塑料的生物安全性。结果表明,梯度浓度的抗菌剂改性塑料对金黄色葡萄球菌和大肠杆菌均有良好的抗菌效果;生物安全性测试结果表明,抗菌塑料的细胞毒性为0级,说明抗菌塑料具有较高的生物安全性。     

中药血清药理学研究金银花的抑菌活性

采用最低抑菌浓度(MIC)测定方法和抑菌活性试验,考察不同产地的金银花以及含药血清的抑菌效果。试验结果为:含药血清对大肠杆菌和金黄色葡萄球菌的MIC分别为0.5μg绿原酸/mL和0.25μg绿原酸/mL;含药血清抑菌活性为高敏。     

高价银配合物的制备、表征及抗菌性能研究

以亚乙基双胍、吡啶及吡啶衍生物为配体合成了[AgEn(BigH)_2]_2(SO_4)_3·7H_2O(3)、[Ag(Py)_2(N_2)_2](OH)_2(4)和[Ag(2-Apy)_3(OH)](HSO_4)·H_2O(5)三种较稳定的高价银配合物。产物结构经红外光谱、元素分析和XPS进行表征。通过最小抑菌浓度(MIC)和生长抑制曲线来检测配合物的抗菌能力,并对配合物进行光稳定测试。抗菌实验结果显示,所有的配合物在0.5μg/mL浓度下就开始对测试菌产生抑制作用,对大肠杆菌的MIC分别为10、5和5μg/mL,对金黄色葡萄球菌的MIC为40、20和20μg/mL。配合物对大肠杆菌的抗菌活性高于对金黄色葡萄球菌。     

“红七星”大蒜油的抑菌活性研究

采用K-B法考察温江"红七星"大蒜油的抑菌活性作用,对大蒜油抑制大肠杆菌、金黄色葡萄球菌、绿脓杆菌的作用进行研究,通过观察抑菌环的形成、计算最低抑菌浓度(MIC)、半数有效浓度(IC_(50))判断抑制作用的强弱。实验表明,大蒜油对大肠杆菌、金黄色葡萄球菌有抑菌环形成,且大肠杆菌和金黄色葡萄球菌抑菌率变化较大,但对绿脓杆菌形成抑菌环较小且抑菌率变化不大。     

微米级花状结构铜/聚乙烯吡咯烷酮的制备及其抗菌性能

采用液相还原的方法,以聚乙烯吡咯烷酮(PVP)为修饰剂,氯化铜为前驱体,水合肼为还原剂,成功制备了微米级Cu/PVP花状结构.采用扫描电子显微镜和X射线粉末衍射仪分析了所得样品的形貌与结构;利用差热分析测定了样品的热稳定性,并采用肉汤稀释法测试了其抗菌性能.结果表明,所制备的样品具有由多个Cu/PVP圆片组装而成的直径为6μm的花状结构,其形貌依赖于反应条件.与此同时,花状结构的Cu/PVP对金黄色葡萄球菌和大肠杆菌具有明显的抗菌作用,相应的最小抑菌浓度(MIC)和最小杀菌浓度(MBC)分别为:41.25mg/L、82.5mg/L,以及20.63mg/L、82.5mg/L.与单一Cu纳米微粒相比,花状结构的Cu/PVP复合物的抗菌持久性明显较好.     

6种多金属氧酸盐的抑菌作用

合成了5种过渡金属取代的Keggin型多金属氧酸盐(Na_7PMo_(11)M(Ⅱ)O_(40)(M=Mn,Fe,Zn,Co,Ni)(简写为PMo_(11)M(Ⅱ)),并通过紫外可见分光光度计和傅里叶变换红外光谱仪对其结构进行了表征。进而运用牛津杯法研究了这5种过渡金属取代的Keggin型多金属氧酸盐和母体H_3PMo_(12)O_(40)(简写为PMo_(12))对藤黄八叠球菌、金黄色葡萄球菌、枯草芽孢杆菌和大肠杆菌的抑菌活性,并用微量肉汤二倍稀释法测得了这些(共6种)化合物对上述4种菌的最小抑菌浓度(MIC值)和最小杀菌浓度(MBC值)。结果表明,这6种化合物对4种菌均有不同程度的抑制作用,并且对2种球菌的抑制效果优于对2种杆菌的抑制效果。其中(Na_7PMo_(11)M(Ⅱ)O_(40)(M=Ni,Mn,Zn)对4种菌的抑制效果优于其它3种化合物。综合考虑,本研究能够为多金属氧酸盐用于果蔬的防腐保鲜提供更多的理论和实验支持。     

Essential oil analysis and antibacterial activity of Rosmarinus tournefortii from Algeria

The volatile compounds obtained by hydrodistillation of the aerial parts of Rosmarinus tournefortii De Noé. growing wild in the occidental region of Algeria were analyzed by GC/MS. Thirty-six compounds were characterized representing 95.6% of the essential oil, with camphor (37.6%), 1,8-cineole (10.0%), p-cymene-7-ol (7.8%), and borneol (5.4%) as the major components. The antimicrobial activity was evaluated against three pathogenic bacteria: Gram-negative (Escherichia coli and Pseudomonas aeruginosa) and Gram-positive (Staphylococcus aureus). The minimum inhibitory concentration (MIC; mg/mL) was determined by sub-culture on Muller Hinton agar plates. The essential oil exhibited strong antibacterial activity against E. coli and P. aeruginosa, and was also active against Staphylococcus aureus.     

Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation

Background: Infectious diseases still affect large populations causing significant morbidity and mortality. Bacterial and fungal infections for centuries were the main factors of death and disability of millions of humans. Despite the progress in the control of infectious diseases, the appearance of resistance of microbes to existing drugs creates the need for the development of new effective antimicrobial agents. In an attempt to improve the antibacterial activity of previously synthesized compounds modifications to their structures were performed. Methods: Nineteen thiazolidinone derivatives with 6-Cl, 4-OMe, 6-CN, 6-adamantan, 4-Me, 6-adamantan substituents at benzothiazole ring were synthesized and evaluated against panel of four bacterial strains S. aureus, L. monocytogenes, E. coli and S. typhimirium and three resistant strains MRSA, E. coli and P. aeruginosa in order to improve activity of previously evaluated 6-OCF₃-benzothiazole-based thiazolidinones. The evaluation of minimum inhibitory and minimum bactericidal concentration was determined by microdilution method. As reference compounds ampicillin and streptomycin were used. Results: All compounds showed antibacterial activity with MIC in range of 0.12–0.75 mg/mL and MBC at 0.25–>1.00 mg/mL The most active compound among all tested appeared to be compound 18, with MIC at 0.10 mg/mL and MBC at 0.12 mg/mL against P. aeruginosa. as well as against resistant strain P. aeruginosa with MIC at 0.06 mg/mL and MBC at 0.12 mg/mL almost equipotent with streptomycin and better than ampicillin. Docking studies predicted that the inhibition of LD-carboxypeptidase is probably the possible mechanism of antibacterial activity of tested compounds. Conclusion: The best improvement of antibacterial activity after modifications was achieved by replacement of 6-OCF₃ substituent in benzothiazole moiety by 6-Cl against S. aureus, MRSA and resistant strain of E. coli by 2.5 folds, while against L. monocytogenes and S. typhimirium from 4 to 5 folds.     

通过柠檬酸改性提高载银活性炭的抗菌性能

通过负载柠檬酸对活性炭进行改性,用N2吸附法测定活性炭的比表面积,用AAS、SEM、XRD测试技术分析了银在活性炭上的吸附和分布,并研究了载银活性炭的抗菌性能。结果表明,负载柠檬酸使活性炭的比表面积下降约24%,但载银后活性炭的比表面积增大。柠檬酸改性为[Ag(NH3)2] 的还原吸附提供更多的活性点,使银的吸附速率加快,吸附量提高约25%,表面的银颗粒变得非常密集,粒径减小,且颗粒均匀,因此抗菌性能显著增强,其中对金黄色葡萄球菌的杀灭效果明显优于对大肠杆菌的,同时对于高分散Ag/C催化剂的制备及银的回收也具有重要的价值。     

Antimicrobial activities of indole alkaloids from Tabernaemontana catharinensis

Tabernaemontana catharinensis root bark ethanol extract, EB2 fraction and the MMV alkaloid (12-methoxy-4-methylvoachalotine) were evaluated for their antimicrobial activities. T. catharinensis ethanol extract was effective against both strains of the dermatophyte Trichophyton rubrum at concentrations of 2.5 mg/mL (wild strain) and 1.25 mg/mL (mutant strain), while the EB2 fraction and MMV alkaloid showed a strong antifungal activity against wild and mutant strains with MIC values of <0.02 and 0.16 mg/mL, respectively. The EB2 fraction showed a strong antibacterial activity against ATCC strains of S. aureus, S. epidermidis, E. coli and P. aeruginosa with MICs from <0.02 to 0.04 mg/mL, as well as against resistant clinical isolates species of Enterococcus sp, Klebsiella oxytoca, Citrobacter, K. pneumoniae, P. mirabilis, S. aureus, S. epidermidis, E. coli and P. aeruginosa with MIC values ranging from 0.04 to 0.08 mg/mL. The MMV alkaloid presented a MIC of 0.16 mg/mL against the strains of S. aureus and E. coli ATCC. For the resistant clinical isolates Enterococcus sp, Citrobacter, S. aureus, S. epidermidis, E. coli and P. aeruginosa the MIC of MMV ranged from 0.08 to 0.31 mg/mL. The chromatography analysis of the EB2 fraction revealed the presence of indole alkaloids, including MMV, possibly responsible for the observed antimicrobial activity.     

Synthesis, biological evaluation and in silico metabolic and toxicity prediction of some flavanone derivatives

Flavones chemically are anthoxanthins, occur either in the free state or as glycosides associated with tannins (flavanoids). Flavanoids (derivatives of flavone) possess various pharmacological activities and due to its xanthine-oxidase enzyme inhibitory effect it also has superoxide-scavenging activities. A series of 2-phenyl-2,3-dihydrochromon-4-one derivatives (flavanone derivatives) were synthesized from chalcones by cyclization method and their activities were evaluated against some gram positive and gram-negative bacteria. IR, NMR and CHN analysis confirmed the structure of the synthesized compounds. The results of the antibacterial studies shows that compounds 2b, 2e, 2f and 2h possess activity against many bacterial strains. Among that the compound (2h) has remarkable activity against all strains viz. 25 microg/ml inhibitory concentration against S. aureus, S. sonnei, E. coli, S. typhimurium and V. cholerae. Compound 2f possess minimum inhibitory concentration of 200 microg/ml against E. coli and S. typhimurium and 25 microg/ml against S. sonnei, S. dysenteriae and V. cholerae. In silico metabolic and toxicity study of the synthesized compounds were performed and the predicted result showed that the compound having hydroxyl functional group undergo sulfate and O-glucuronide conjugation reaction and methoxy derivatives undergo demethylation reaction. The biologically active compounds are free of toxicity in oncogene, teratogen, sensitivity and immunotoxicity.     

Synthesis,Antibacterial and Pharmacokinetic Evaluation of Novel Derivatives of Harmine N9-Cinnamic Acid

A series of 16 new derivatives of harmine N⁹-Cinnamic acid were synthesized and fully characterized using NMR and MS. The in vitro antibacterial evaluation revealed that most of the synthesized harmine derivatives displayed better antibacterial activities against Gram-positive strains (S. aureus, S. albus and MRSA) than Gram-negative strains (E. coli and PA). In particular, compound 3c showed the strongest bactericidal activity with a minimum inhibitory concentration of 13.67 μg/mL. MTT assay showed that compound 3c displayed weaker cytotoxicity than harmine with IC₅₀ of 340.30, 94.86 and 161.67 μmol/L against WI-38, MCF-7 and HepG2 cell lines, respectively. The pharmacokinetic study revealed that the distribution and elimination of 3c in vivo were rapid in rats with an oral bioavailability of 6.9%.