珊瑚姜精油的超临界萃取及其抗真菌和细菌活性

珊瑚姜(ZingibercorallinumHance)为姜科姜属植物,产于贵州、广西、广东,贵州主要分布在南、北盘江下游河谷地带,为贵州苗族习用药材,称Jabbangxhnaibdiel(加榜海丢)或阴姜,少数民族常以珊瑚姜块茎入药,具有消肿、解毒、抗菌的功能,用于治疗感冒、咳嗽、腰痛、腹泻[1]。其挥发油的药理研究表明,有抑制离体肠肌引起的痉挛性收缩的自发运动、拮抗组织胺引起的胃肠收缩反应和解除毛果芸香碱、乙酰胆碱、氯化钠等引起的肠痉挛性收缩[2]。挥发油还具有显著的抗真菌作用[3],用于治疗皮癣[4]。超临界CO2萃取是一项新兴的提取分离技术,在中药…     

基于标记法的福白菊精油抗真菌机理研究

以福白菊为原料, 通过有机溶剂萃取和水蒸气蒸馏相结合制备福白菊精油. 分别采用健那绿、 细胞膜荧光探针DiI、 碘化丙啶、 罗丹明123以及溴化乙锭等染料标记酵母细胞、 酵母细胞膜、 酵母线粒体和质粒DNA, 研究福白菊精油对酵母细胞、 酵母细胞膜、 线粒体以及质粒DNA的破坏作用, 探讨福白菊精油的抗真菌机理. 研究结果表明, 福白菊精油不仅能破坏真菌的细胞膜, 使其细胞内含物外泄, 还能够穿过细胞膜, 破坏其线粒体膜和DNA, 最终导致真菌细胞死亡.     

新型三唑醇衍生物的合成及抗真菌活性

依据三唑醇类化合物的构效关系, 保留基本药效团三唑环、叔醇羟基和2,4-二氟苯基, 引入新的含哌嗪侧链结构, 设计合成了12个1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-取代-2-丙醇类化合物.     

三氮唑类化合物的合成及抗真菌活性研究

近年来深部真菌感染的发病率和病死率逐年增加;同时由于真菌与人类细胞同为真核细胞,长期使用抗真菌药后对宿主具有相当的毒性.三氮唑类药物是目前治疗深部真菌感染的重要药物之一[1],代表药物有酮康唑、氟康唑、伊曲康唑等.该类药物抗菌谱广、毒性低、抗真菌作用强,但仍存在肝毒性较大、易产生耐药性等不良反应.     

有机锡四唑乙酸酯的合成、结构与抗真菌活性

通过四唑乙酸与二丁基氧化锡(或二乙基氧化锡)反应,合成了4个新的有机锡四唑乙酸酯。它们的结构通过红外,核磁以及X-射线单晶衍射分析得到确证。生物活性测试表明,它们对小麦赤霉病菌以及禾谷丝核菌等具有一定的抑制活性。     

有机锡含氟苯乙酸酯的合成及抗真菌活性

通过α-溴代苯乙酸乙酯与对氟苯酚以及α-溴代对氟苯乙酸乙醇与苯酚在碱性条件的反应,然后碱性水解、酸性酸化,合成了α-对氟苯氧基苯乙酸及α-苯氧基对氟苯乙酸.将该酸与二烷基氧化锡反应,制得了四个新的有机锡羧酸酯,用红外光谱,核磁共振,元素分析以及X-射线单品衍射确定了这类化合物的结构,结果表明,羧基以不对称的双齿形式与锡...     

氟康唑衍生物的设计合成及体外抗真菌活性研究

为了寻找活性更好的抗真菌化合物,基于已有的计算机辅助药物设计结果,保留氟康唑母体结构必需药效团,设计、合成了22个含对甲酚和胸腺嘧啶的氟康唑新衍生物.目标化合物的结构经1H NMR、元素分析和ESI-MS确证,初步体外抗真菌活性试验结果表明,化合物5l对7种真菌都表现出了较好的抗真菌活性(烟曲霉菌除外),化合物5a～5e,5g,5h,7a和7b对不同真菌表现出了一定的抗真菌活性.炔丙基取代氨基侧链结构的引入有利于提高该类目标化合物体外抗真菌活性,值得进一步深入研究.     

新型丙烯海松酸基双噻二唑化合物的合成及其抗真菌活性

松香与丙烯酸经Diels-Alder环加成反应制得丙烯海松酸(1); 将1转化为双酰氯后与2-氨基-5-取代苯基-1,3,4-噻二唑经-N-酰化反应合成了8个新型的丙烯海松酸基双噻二唑化合物(4a~4h),其结构经¹H NMR, ¹³C NMR, IR和元素分析表征。抗真菌活性测试结果表明,在用药量为50 μg·mL^-1时,4d(R=m-Cl)对苹果轮纹病菌、花生褐斑病菌和小麦赤霉病菌的抑制率分别为66.9%, 57.8%和52.9%。     

含取代吡唑新型苯甲酰胺类化合物的合成及抗真菌活性研究

为了找寻新的杀菌剂,运用活性片段拼接策略,通过亚胺键将苯甲酰胺类衍生物和吡唑环连接起来,设计并合成了一系列共计32个新型吡唑-5-基-苯甲酰胺类衍生物,其结构经过NMR、HRMS分析确认,并评估了它们的抗真菌活性.生物测定数据显示,大多数化合物表现出良好的抑制活性.4-氯-N-(2-((1-甲基-3-(三氟甲基)-1H...     

多取代香豆素类化合物的合成及抗真菌活性

以前期合成的6/7/8-羟基-3-香豆素甲酸乙酯为原料,使其与卤代烃发生Williamson反应制得化合物1～6;以2,4-二羟基苯甲醛为原料,使其与季鏻盐发生Wittig反应得到中间体化合物7;以取代间苯二酚为原料,使其与乙酰乙酸乙酯发生Pechmann缩合得到化合物8～10;在TBAB催化下,化合物7～10与相应的卤代烃发生Williamson反应制得化合物11～17;通过~1H NMR、~(13)C NMR和ESI-MS等波谱技术确定了所有目标化合物的结构。在50μg·mL~(-1)时,以醚菌酯或多菌灵为阳性对照,测定了所有化合物对12种常见植物病原真菌的抑制作用,发现它们均具有不同程度的抗菌活性。其中,4、5、7和13对苹果腐烂菌、苹果炭疽菌、白菜黑斑、水稻稻瘟、烟草赤星、苹果轮纹等6种植物病原菌的抑制活性高于阳性对照醚菌酯或多菌灵。由此可见,化合物4、5、7和13具有开发成新型农用抗菌剂的潜力,这为后续香豆素类抗菌剂的研发奠定了理论基础。     

白蒿挥发油成分的测定及其抗氧化活性分析

采用乙醇浸提法提取生长期和花果期白蒿的挥发油,通过正交实验确定最佳提取条件为:提取3次、浸提90 min、对于生长期和花果期白蒿液料比分别为10 mL:1 g和8 mL:1 g.通过红外光谱和液相色谱-质谱联用分析了产物的主要成分,生长期白蒿挥发油的主要成分为桉树脑、樟脑、右旋龙脑、石竹烯、Cadina-1,4-diene、白菖烯、棕榈酸乙酯等;花果期白蒿挥发油的主要成分为樟脑、石竹烯、龙脑、甲酸橙花酯等.通过1,1-二苯基-2-三硝基苯肼(DPPH)自由基清除实验对产物的自由基清除活性进行了测定,生长期和花果期白蒿挥发油对0.05 mmol/L DPPH溶液的IC50值分别为0.40和1.66 mg/mL.研究结果表明,乙醇浸提的生长期和花果期白蒿的挥发油具有较好的抗氧化活性.     

A Composition Analysis and an Antibacterial Activity Mechanism Exploration of Essential Oil Obtained from Artemisia giraldii Pamp

The goal of this work was to use the GC-MS technique to explore the chemical components of Artemisia giraldii Pamp essential oil (AgEo) and to uncover its antibacterial activity, specifically the antibacterial mechanism of this essential oil. There were a total of 63 chemical constituents in the AgEo, monoterpenes (10.2%) and sesquiterpenes (30.14%) were found to be the most common chemical components, with camphor (15.68%) coming in first, followed by germacrene D. (15.29%). AgEo displayed significant reducing power and good scavenging ability on hydroxyl radicals, 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radicals, and 2,2′-Azinobis-(3-ethylbenzthiazoline-6-sulphonate (ABTS) radicals, according to antioxidant data. The diameter of the inhibition zone (DIZ) of AgEo against S. aureus and E. coli was (14.00 ± 1.00) mm and (16.33 ± 1.53) mm, respectively; the minimum inhibitory concentration (MIC) of AgEo against E. coli and S. aureus was 3 μL/mL and 6 μL/mL, respectively; and the minimum bactericidal concentration (MBC) of AgEo against E. coli and S. aureus was 6 μL/mL and 12 μL/mL, respectively. The antibacterial curve revealed that 0.5MIC of AgEo may delay bacterial growth while 2MIC of AgEo could totally suppress bacterial growth. The relative conductivity, alkaline phosphatase (AKP) activity, and protein concentration of the bacterial suspension were all higher after the AgEo treatment than in the control group, and increased as the essential oil concentration was raised. In addition, the cell membrane ruptured and atrophy occurred. The study discovered that AgEo is high in active chemicals and can be used as an antibacterial agent against E. coli and S. aureus, which is critical for AgEo’s future research and development.     

Antimicrobial Activity and Synergy Investigation of Hypericum scabrum Essential Oil with Antifungal Drugs

The chemical composition of Lebanese Hypericum scabrum essential oil (EO) was analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GG-MS). Its antimicrobial activity was evaluated by determining its minimal inhibitory concentrations (MICs) against a Gram-negative and a Gram-positive bacterium, one yeast, and five dermatophytes. H. scabrum EO was most active on filamentous fungi (MIC values of 32–64 µg/mL). Synergy within the oil was investigated by testing each of the following major components on Trichophyton rubrum: α-pinene, limonene, myrcene, β-pinene and nonane, as well as a reconstructed EO. The antifungal activity of the natural oil could not be reached, meaning that its activity might be due, in part, to minor constituent(s). The interactions between H. scabrum EO and commercially available antifungals were assessed by the checkerboard test. A synergistic effect was revealed in the combination of the EO with amphotericin B.     

佛手挥发油的化学成分

用色谱－质谱－计算机联用法对佛手挥发油的化学成分和相对含量进行了系统分析,得到６７种组分,鉴定出３１个组分,主要组分是柠檬烯（４８．４％）、１－甲基－２－（１－甲乙基）－苯（３０．８％）。     

新型含二甲氧基甲基嘧啶基磺酰脲衍生物的合成及生物活性

将二甲氧基甲基引入到嘧啶环的4位, 设计并合成了15个结构新颖的磺酰脲类衍生物. 初步生物活性测试结果表明, 目标化合物具有较好的除草活性. 在75 g/ha的剂量下, 化合物6a和6g对油菜的芽前除草活性为100%, 与对照药单嘧磺隆和氯磺隆相当; 在50 mg/L的浓度下, 化合物6i和6o对3种病菌的离体抑制率都超过80%, 与对照药百菌清和多菌灵接近.     

Diastereoselective Synthesis and Antifungal Activity of Glycosyl Isoxazolines

Abstract

Glycosyl nitrile oxides, generated in situ by reaction of glycosyl oximes (3a, 3b, 4) with N‐chlorosuccinimide and DBU, on 1,3‐dipolar cycloaddition with substituted alkenes resulted in glycosyl isoxazolines (5, 7–28) in diastereoselective manner. The extent of diastereoselection varies with the nature of substituents both in sugar and alkenes. The compounds synthesized were screened in vitro against many fungi wherein two of the compounds (12, 23) showed significant inhibition against Sporothrix schenckii, Trychophyton mentagrophytes, and Cryptococcus neoformans with MIC of 12.5 and 6.25 µg/mL, respectively.     

新型含苯基取代嘧啶基磺酰脲衍生物的设计、 合成及生物活性

将苯基引入到嘧啶环的4位, 设计、 合成了2个系列共24个结构新颖的磺酰脲类衍生物, 并对其生物活性进行了研究. 抑菌实验结果表明, 目标化合物对苹果轮纹病菌和小麦纹枯病菌表现出优异的抑制率, 其中化合物9f对5种病菌的抑制率均超过65%. 进一步研究发现, 化合物9f对苹果轮纹病菌的EC₅₀值为8.63 mg/L, 略高于对照药百菌清(7.33 mg/L); 化合物8k和9k对小麦纹枯病菌的EC₅₀值分别为5.48和6.09 mg/L, 与百菌清(4.26 mg/L)接近. 同时, 盆栽法除草测试结果表明, 在75 g/ha剂量下, 化合物8d和9d对油菜具有较好的芽前除草活性, 分别为86%和73%; 化合物9h对反枝苋的土壤处理抑制活性为100%, 优于对照药氯磺隆(96%).     

Evaluation of Antifungal and Antioxidant Activity of Newly Synthesized 4‐Thiazolidinones

The antifungal and antioxidant activities of thirty newly synthesized 4‐thiazolidinone (TZON) derivatives were assessed against some fungal species including Candida albicans and Aspergillus niger. The introduction of different arylidene moieties at 5‐positions of the thiazolidinone ring successfully enhanced its biological activity. The structure–activity relationships revealed that 4‐thiazolidinone derivatives harboring dicarboxyethyl (at the 2‐ethenyl) and p‐nitrophenylhydrazyl arm (at the 5‐arylidine positions of the thiazolidinone ring) display considerable antifungal and antioxidant properties.