含喹喔啉杨梅素衍生物的合成及生物活性

利用活性拼接原理, 将喹喔啉引入到杨梅素结构中, 合成了一系列含喹喔啉基团的杨梅素新型衍生物. 采用浊度法测试了目标化合物的体外抑菌活性, 结果表明, 目标化合物对柑橘溃疡病菌(X. Citri)和水稻白叶枯病菌(X. Oryzae)均表现出较好的抑制活性. 目标化合物对柑橘溃疡病菌的抑制活性(EC₅₀)均优于对照药叶枯唑和噻菌铜(EC₅₀分别为54.85和61.13 μg/mL), 其中化合物4o抑制活性(EC₅₀=11.17 μg/mL)最优; 目标化合物对水稻白叶枯病菌的抑制活性EC₅₀均优于对照药叶枯唑和噻菌铜(EC₅₀分别为148.20和175.47 μg/mL), 其中化合物4f抑制活性(EC₅₀=34.49 μg/mL)最优. 采用半叶枯斑法测试了目标化合物的抗烟草花叶病毒(TMV)活性, 结果表明, 所有目标化合物在浓度为500 mg/L时均有一定的抑制作用.     

3-S-(β-D-吡喃葡萄糖基)-1,2,4-三唑的合成及抗菌活性

以自制的5-取代芳基-4-氨基-3-巯基-1,2,4三唑为底物, 经糖基修饰后, 在甲醇钠/甲醇/二氯甲烷体系中经水解脱除糖环上的乙酰基, 得到9个新化合物5-取代苯基-4-氨基-3-S-(β-D-吡喃葡萄糖基)-1,2,4-三唑(6a~6i), 其结构经核磁共振波谱(¹H NMR, ¹³C NMR), 红外光谱(IR)和高分辨质谱(HRMS)确认. 生物活性测试结果表明, 目标化合物对大肠杆菌、 金黄色葡萄球菌、 枯草芽孢杆菌和白色念珠菌均显示出良好的抑菌活性. 化合物6g对大肠杆菌、 金黄色葡萄球菌、 枯草芽孢杆菌和白色念珠菌的最小抑菌浓度分别达到2, 8, 32和8 μg/mL, 抑菌效果接近或优于对照药物三氯生和氟康唑. 利用Autodock程序研究了目标化合物(6a~6i)与大肠杆菌烯脂酰还原酶(FabⅠ)受体蛋白分子的相互作用和结合自由能变化规律.     

液相色谱-串联质谱法测定葡萄中链霉素和双氢链霉素

研究系统地优化了样品前处理过程及仪器分析中影响链霉素和双氢链霉素残留分析准确度与响应灵敏度的各主要因素,建立了葡萄中链霉素和双氢链霉素残留的快速精准定量分析方法。葡萄样品经磷酸溶液(pH=2)超声提取、Oasis HLB单固相萃取柱富集净化后,采用Waters HSS T3色谱柱(100 mm×2.1 mm, 1.8 μm)分离,柱温35 ℃,进样量2 μL,以0.1%甲酸水溶液-甲醇溶液(60∶40, v/v)为流动相进行等度洗脱,在正离子、电喷雾电离源多反应监测模式下测定,外标法定量。链霉素和双氢链霉素在2~400 μg/L质量浓度范围内线性关系良好,相关系数(R²)分别为0.9991和0.9997;在5、10、20和40 μg/kg 4个添加水平下的平均回收率为76.8%~91.9%,相对标准偏差为0.4%~10.2%;链霉素和双氢链霉素的检出限(LOD)为1 μg/L,定量限(LOQ)为5 μg/kg。为验证该方法的适用性,将方法适用于无籽红提、新郁葡萄、夏黑葡萄等实际样品中进行添加回收实验,链霉素和双氢链霉素的平均回收率分别为77.2%~83.9%和70.8%~78.9%, RSD为3.0%~15.6%。该法的准确度和精密度均符合葡萄中链霉素和双氢链霉素分析要求,且操作简便、准确,灵敏度高,适用于葡萄中链霉素和双氢链霉素残留量的检测分析。     

QuEChERS结合超高效液相色谱-串联质谱法同时测定畜禽肉中44种食源性兴奋剂和6种孕激素

利用QuEChERS结合超高效液相色谱-串联质谱法建立了畜禽肉中44种兴奋剂和6种孕激素的检测技术。样品粉碎均质后加入内标,依次加入水和含0.5%乙酸的乙腈溶液振荡提取后,加入氯化钠和无水硫酸镁脱水离心,上清液采用PSA、C₁₈、中性氧化铝和无水硫酸镁分散固相萃取材料进行净化,净化液经氮气吹干,复溶后用超高效液相色谱-串联质谱仪测定。被测物采用ACQUITY BEH C₁₈(100 mm×2.1 mm, 1.7 μm)色谱柱,以0.1%甲酸-5 mmol/L乙酸铵水溶液和甲醇为流动相分离,在电喷雾正离子模式下,以多反应监测(MRM)方式采集,采用基质匹配标准曲线内标法定量分析。50个被测物包含6类化合物:β₂-激动剂类(19个)、β-阻断剂类(3个)、蛋白同化激素类(11个)、糖皮质激素类(8个)、利尿剂类(3个)、孕激素(6个)。所有被测物在各自的范围内线性关系良好,相关系数>0.99, β₂-激动剂类和β-阻断剂类的线性范围为0.1~20 μg/L,糖皮质激素类的线性范围为0.5~200 μg/L,蛋白同化激素类、孕激素类、利尿剂类的线性范围为0.2~50 μg/L。方法的定量限范围为0.1~0.4 μg/kg。在低、中、高3个浓度水平下的加标回收率试验中,50种目标化合物在鸡肉、猪肉、牛肉、羊肉中的平均回收率范围为50.3%~119.9%,相对标准偏差(RSD, n=6)范围为0.42%~15.1%。采用该法和国标方法(GB/T 21981-2008)同时对市售的9个肉样品(包括3个牛肉、3个猪肉、2个鸡肉、1个鸭肉)进行了比对检测,对检出的氢化可的松、可的松含量采用t检验进行统计学分析,结果表明,两种方法测得的数据没有显著性差异。采用该法测定了12个来自某养殖场的牛肉样品,结果共检出4种食源性兴奋剂,其中氢化可的松的含量范围为3.3~22.6 μg/kg,检出率为100%;可的松的含量范围为1.5~2.1 μg/kg,检出率为67%;雄烯二酮含量范围为0.7~1.2 μg/kg,检出率为17%;睾酮含量范围为0.6~1.5 μg/kg,检出率为42%。该法操作简单,准确灵敏,重复性好,适用于不同种类畜禽肉中食源性兴奋剂和孕激素的检测。     

高通量固相萃取-超高效液相色谱-串联质谱法测定人尿中8种环境酚类内分泌干扰物

建立了人尿中8种环境酚类化合物的96孔板固相萃取-超高效液相色谱-串联质谱(96-well SPE LC-MS/MS)检测方法,其中包括7种双酚类化合物和三氯生。尿样解冻到室温,经β-葡萄糖醛酸苷肽酶/芳基磺酸酯酶37 ℃过夜酶解。实验比较了3种96孔板固相萃取柱和不同淋洗条件对人尿样的净化效果和目标化合物的回收率。结果显示,采用Oasis HLB 96孔板(60 mg)对样品进行萃取和用30%(v/v)乙腈水溶液进行淋洗净化的纯化效果最好。纯化后目标物用甲醇溶液洗脱,经氮气吹干,用0.5 mL甲醇-水(1∶1, v/v)溶液定容,目标化合物用UPLC-MS/MS进行检测。比较了2种分析柱(C₁₈和T3分析柱)以及不同的有机流动相对分离样品中目标物的影响。结果显示,以BEH C₁₈(100 mm×2.1 mm, 1.7 μm)作为分析柱,乙腈/水作为流动相,以流速0.3 mL/min梯度洗脱时,目标物的分离效果最好。质谱条件选择串联质谱负离子电喷雾(ESI^-)多反应监测模式(MRM)进行检测。对样品的基质效应进行评估发现,双酚A、双酚F、双酚S、双酚B和双酚AF的绝对基质效应为3.47%~15.32%,不需要补偿措施;四氯双酚A、四溴双酚A和三氯生的绝对基质效应分别是49.58%(中等基质效应)、71.99%和86.93%(强基质效应),均需要补偿效应。因此,该方法采用了一一对应的同位素内标法抵消基质效应。用6份实际尿样基质评估相对基质效应,8种内标的峰面积的相对标准偏差为3.63%~9.06%,说明相对基质效应稳定。在优化条件下,双酚A和双酚AF在0.50~50 μg/L内、四氯双酚A和双酚S在0.05~50 μg/L内、双酚F和四溴双酚A在0.01~50 μg/L内、双酚B在1.00~50 μg/L内、三氯生在5.00~200 μg/L内线性关系良好,相关系数大于0.9995。方法检出限为0.002~1.09 μg/L,定量限为0.007~3.63 μg/L。3个加标水平的加标回收率为81.0%~101.9%,日内精密度为0.4%~19.4%,日间精密度为2.5%~17.8%。应用该方法对2019-2020年采集的北京地区64份尿样进行测定,结果发现8种目标分析物中,除双酚B和双酚AF未检出外,其余均有检出,其中双酚A和双酚S的检出率最高,分别为100%和96.9%。三氯生、四溴双酚A、四氯双酚A和双酚F的检出率分别为57.8%、46.9%、23.4%和21.9%。尿样中8种目标物含量的中位值以降序排列分别为1.44 μg/L(三氯生)、0.69 μg/L(双酚A)、0.086 μg/L(双酚S)、0.0032 μg/L(四溴双酚A)、0.00050 μg/L (四氯双酚A)、0.00 μg/L(双酚F、双酚B和双酚AF)。以上尿样检测结果显示,北京市居民存在普遍的环境酚类化合物暴露,值得关注。该方法操作简单,定量准确,样品需求量小,有机试剂消耗少,适合大批量样本的测定。     

直链淀粉-三[(S)-1-苯乙基氨基甲酸酯]手性固定相拆分布地奈德对映体及其制剂含量的测定

22R-布地奈德的药物活性比22S-布地奈德的强2~3倍,开发布地奈德对映体拆分和定量分析方法,可为其药物研发及质量控制提供重要依据。目前,主要以反相C₁₈固定相对布地奈德对映体进行拆分,而采用手性固定相对其进行拆分少有报道。通过考察固定相、流动相和柱温对布地奈德对映体拆分的影响,建立了基于直链淀粉-三[(S)-1-苯乙基氨基甲酸酯]手性固定相快速拆分和检测布地奈德对映体的高效液相色谱方法,其色谱条件如下:色谱柱为Chiralpak AS-RH色谱柱(150 mm×4.6 mm, 5.0 μm),流动相为乙腈-水(45∶55, v/v),柱温40 ℃,流速1.0 mL/min,二极管阵列检测器(DAD),检测波长246 nm,进样量10 μL。在该色谱条件下,布地奈德的两个对映体得到较好拆分,22R-布地奈德和22S-布地奈德的保留时间分别6.40 min和7.77 min,分离度为4.64; 22R-布地奈德和22S-布地奈德分别在各自范围内线性关系良好,相关系数(R²)均为0.9999,检出限分别为0.05 μg/mL和0.07 μg/mL,定量限分别为0.16 μg/mL和0.20 μg/mL; 4个添加水平的样品加标回收率为102.63%~104.17%,相对标准偏差(RSD)为0.08%~0.57%(n=6)。将该方法应用于1批次4个吸入用布地奈德混悬液实际样品进行检测,22R-布地奈德和22S-布地奈德的含量分别为283.15~284.63 μg/mL和259.86~261.51 μg/mL。该方法操作简便,分析时间短,重复性好,准确度高,可用于布地奈德对映体的拆分及其制剂的质量控制。     

无花果叶中有效成分鉴别及含量测定

近年来,无花果叶片中所含成分分析主要集中在同类型物质或整类物质,而对多种类型单一有效物质的定性定量研究较少。 本文采用溶剂浸提-超声波辅助法对无花果叶片中的有效成分进行了提取,利用气相色谱-质谱和超高效液相色谱-离子阱质谱对有效成分进行了鉴定。 结果表明,无花果叶中主要成分为绿原酸、芦丁、补骨脂素和佛手苷内酯。 采用单因素实验法,确定了4种成分的最佳提取工艺。 利用高效液相色谱建立了绿原酸、芦丁、补骨脂素和佛手苷内酯的定量分析方法。 绿原酸在1.84~9.2 μg范围内有良好的线性关系(R²=0.9991),回收率为95.2%;芦丁在3.4~17 μg范围内有良好的线性关系(R²=0.9981),回收率为96.8%;佛手内脂在4~20 μg范围内有良好的线性关系(R²=0.9998),回收率为89.5%;补骨脂素在4~20 μg范围内有良好的线性关系(R²=0.9963),回收率为87.1%。     

QuEChERS-气相色谱-质谱法检测鱼肉中19种氯酚类化合物

大量含氯农药、次氯酸消毒水以及水产品杀虫剂和杀菌剂的广泛使用,使鱼类容易受到氯酚类化合物的污染,因而建立鱼肉中氯酚类化合物的检测方法十分重要。建立了QuEChERS结合气相色谱-质谱法同时检测鱼肉中19种氯酚类化合物的分析方法。19种氯酚类化合物选用DB-5MS毛细管色谱柱(30 m×0.25 mm×0.25 μm),载气流速1 mL/min进行分离,可以得到很好的峰形。前处理采用改良的QuEChERS方法,通过对提取剂的种类和剂量、净化剂的种类和剂量,以及衍生条件中的衍生温度、衍生时间和衍生剂用量等进行优化,确定最优的前处理方法。选择10 mL乙酸乙酯作为提取剂,500 mg的C₁₈作为净化剂,加入3 g氯化钠和5 g无水硫酸镁,过0.22 μm的有机滤膜,加入50 μL的硅烷化衍生剂在45 ℃条件下衍生30 min,用EI源测定,选择离子监测模式,以外标法定量。19种氯酚类化合物在0.4~10 μg/L范围内具有良好的线性关系,相关系数R²大于0.998,方法定量限为0.04~0.16 μg/kg。空白基质不同加标水平的回收率为70.6%~115.0%,相对标准偏差为2.6%~10.5%。将建立的方法应用于实际样品的检测分析,结果显示,各种鱼肉中均有不同程度的氯酚类化合物检出,其中,黄花鱼检出的氯酚类化合物总量最大,为8.74 μg/kg;其次为鲫鱼7.59 μg/kg;米鱼的检出量最少,为1.59 μg/kg。所建立的方法简化了样品的前处理步骤,操作简单,方法灵敏度高、重复性好,可满足鱼肉中19种氯酚类化合物的高通量检测要求,能显著提高氯酚类化合物的检测效率。     

基于ZnO纳米线的螺旋线形跨尺度葡萄糖传感器

制备了一种基于螺旋线形跨尺度结构的酶传感器, 并对该传感器进行了表征和性能测试. 将ϕ 30 μm键合Au丝以螺旋线方式手工缠绕在ϕ 125 μm光纤纤芯上, 在该Au螺旋线上用水浴法合成ZnO纳米线, 得到螺旋线形跨尺度结构; 在ZnO纳米线上物理吸附葡萄糖氧化酶(GOD), 制备了葡萄糖传感器工作电极. 利用扫描电子显微镜(SEM)图像和MatLab图像处理算子分别对螺旋线形跨尺度结构表面形貌及其上活力为50 units/mg的GOD吸附效果进行了定性和定量表征, 分析了非高斯粗糙表面与GOD吸附效果的影响关系. 基于三电极体系采用循环伏安法和计时安培法测试了制备的12个工作电极的性能, 测得该类传感器的灵敏度为(1.410±0.665) μA·L/(mmol·cm²), 线性范围为0~(4.292±0.652) mmol/L, Michaelis-Menten常数为(3.571±1.280) mmol/L, 检出限为(14.085±8.393) μmol/L. 使用活力更高的GOD可以得到性能更好的螺旋线形跨尺度葡萄糖传感器. 该类传感器可广泛应用于医药、 生物、 食品加工及环境监测领域中尿酸、 尿素、 胆固醇、 过氧化氢和苯酚等的检测.     

QuEChERS-同位素内标-高效液相色谱-串联质谱法测定动物源性食品中植物生长调节剂类农药残留

建立了高效液相色谱-串联质谱法测定动物源性食品中植物生长调节剂类农药残留量的方法。选取猪肉、牛肉、鸡肉、猪肝、鸡蛋和牛奶作为样品,样品经乙腈提取,4 g无水硫酸镁(MgSO₄)和1 g氯化钠(NaCl)盐析脱水后,取上清液经50 mg N-丙基乙二胺(PSA)+50 mg十八烷基硅烷(C18)粉末净化(含150 mg MgSO₄)。采用Agilent ZORBAX Eclipse Plus C18柱分离待测物,电喷雾电离,正负离子切换多反应检测模式检测,以乙腈和5 mmol/L乙酸铵水溶液作为流动相进行梯度洗脱,基质匹配内标法定量。在猪肝、鸡蛋基质中,矮壮素、噻苯隆和多效唑在0.1~100 μg/L范围内线性关系良好;在猪肉、牛肉和鸡肉中3种植物生长调节剂在0.1~50 μg/L范围内线性关系良好;在牛奶基质中,噻苯隆和多效唑的线性范围为0.05~10 μg/L,矮壮素的线性范围为0.05~5 μg/L,相关系数(r²)均大于0.990。以信噪比(S/N)≥3对应的添加水平作为检出限(LOD), S/N≥10对应的添加水平作为定量限(LOQ),矮壮素、噻苯隆和多效唑在不同基质下的LOD为0.01~0.1 μg/kg, LOQ为0.5~5 μg/kg。分别添加LOQ、2倍LOQ和10倍LOQ 3个水平的目标化合物,平均回收率为70.0%~117.4%, RSD为0.8%~16.1%。该方法操作简单、灵敏度高,采用基质匹配内标法定量,能最大限度地消除基质干扰,使检测结果更加精确,可满足动物源性食品中矮壮素、噻苯隆和多效唑残留的定量检测工作。     

Comparison of hydrodistillation and headspace solid-phase microextraction techniques for antibacterial volatile compounds from the fruits of Seseli libanotis

The volatile compounds from the fruits of Seseli libanotis, wild-growing in Poland, were obtained by hydrodistillation (HD) and headspace solid-phase microextraction techniques (HS-SPME) and analyzed using GC-MS. A total of 58 components were identified. The most abundant compounds were sabinen and beta-phellandrene. MIC (minimal inhibitory concentration) and MBC (minimal bactericidal concentration) values for the essential oil against reference bacterial strains and clinical S. aureus isolates were determined. The essential oil showed better antibacterial activity against the Gram-positive bacteria (MICs between 0.15 to 1.25 mg/mL) when compared with Gram-negative bacteria (MICs between 1.25 to 2.5 mg/mL). The low values of the MBC/MIC ratio suggest that the examined oil behaved as a bactericidal agent.     

Composition, antioxidant, antimicrobial and anti-wood-decay fungal activities of the twig essential oil of Taiwania cryptomerioides from Taiwan

This study investigated the chemical composition, antioxidant, antimicrobial and anti-wood-decay fungal activities of the essential oil isolated from the twigs of Taiwania cryptomerioides from Taiwan. The essential oil was isolated using hydrodistillation in a Clevenger-type apparatus, and characterized by GC-FID and GC-MS. A total of 35 compounds were identified, representing 100% of the oil. The main components identified were alpha-cadinol (45.9%), ferruginol (18.9%) and beta-eudesmol (10.8%). The antioxidant activity of the oil was tested by the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging capability test. The results showed an IC50 of 90.8 +/- 0.2 microg/mL. The active source compound was ferruginol. The antimicrobial activity of the oil was tested by the disc diffusion and micro-broth dilution methods against ten microbial species. The oil exhibited strong growth suppression against Gram-positive bacteria and yeast with inhibition zones of 45-52 mm and MIC values of 31.25-62.5 microg/mL, respectively. The anti-wood-decay fungal activity of the oil was also evaluated. The oil demonstrated excellent activity against four wood-decay-fungal species. For the antimicrobial and anti-wood-decay fungal activities of the oil, the active source compounds were determined to be alpha-cadinol, beta-eudesmol and ferruginol.     

Chemical composition and antimicrobial activity of some oleogum resin essential oils from Boswellia spp. (Burseraceae)

The chemical composition of Boswellia carteri (Somalia), B. papyrifera (Ethiopia), B. serrata (India) and B. rivae (Ethiopia) oleogum resin essential oils was investigated using GC-MS to identify chemotaxonomy marker components. Total ion current peak areas gave good approximations to relative concentrations based on GC-MS peak areas. B. carteri and B. serrata oleogum resin oils showed similar chemical profiles, with isoincensole and isoincensole acetate as the main diterpenic components. Both n-octanol and n-octyl acetate, along with the diterpenic components incensole and incensole acetate, were the characteristic compounds of B. papyrifera oleogum resin oil. Hydrocarbon and oxygenated monoterpenes were the most abundant classes of compounds identified in the B. rivae oleogum resin oil. The antimicrobial activities of the essential oils were individually evaluated against different microorganisms including fungi, Gram-positive and Gram-negative bacteria strains. The essential oils with the best activity against fungal strains were those obtained from B. carteri and B. papyrifera with MIC values as low as 6.20 microg/ml. The essential oil of B. rivae resin showed the best activity against C. albicans with a MIC value of 2.65 microg/ml.     

Chemical composition and antimicrobial activity of the essential oil of Tanacetum walteri (Anthemideae-Asteraceae) from Iran

The composition and antimicrobial activity of the essential oil of Tanacetum walteri were studied. Aerial flowering parts of plant were collected from North Khorasan Province of Iran and the essential oil was isolated by hydrodistillation and analysed by GC-FID and GC-MS. Antimicrobial activity of the essential oil was determined by disc diffusion and MIC and MBC determination. Thirty-five compounds were identified in the oil of T. walteri accounting for 94.4% of the total oil. Thymol (22.5%), 1,8-cineole (8.2%), umbellulone (6.9%), α-bisabolol (6.3%) and camphor (5.3%) were as the principal constituents. The highest antimicrobial activity of the essential oil was observed against Staphylococcus aureus, Enterococcus faecalis and Klebsiella pneumoniae with MIC value of 0.63 mg/mL. The inhibitory effect of the essential oil of T. walteri could be attributed mainly to the high levels of phenolic compound thymol and oxygenated terpenes in essential oil.     

The Chemical Profiling of Essential Oils from Different Tissues of Cinnamomum camphora L. and Their Antimicrobial Activities

Cinnamomum camphora L. is grown as an ornamental plant, used as raw material for furniture, as a source of camphor, and its essential oil can be used as an important source for perfume as well as alternative medicine. A comparative investigation of essential oil compositions and antimicrobial activities of different tissues of C. camphora was carried out. The essential oils were extracted by hydrodistillation with a Clevenger apparatus and their compositions were evaluated through gas chromatography-mass spectrometry (GC-MS), enantiomeric composition by chiral GC-MS, and antimicrobial properties were assayed by measuring minimum inhibitory concentrations (MICs). Different plant tissues had different extraction yields, with the leaf having the highest yield. GC-MS analysis revealed the presence of 18, 75, 87, 67, 67, and 74 compounds in leaf, branch, wood, root, leaf/branch, and leaf/branch/wood, respectively. The significance of combining tissues is to enable extraction of commercial quality essential oils without the need to separate them. The oxygenated monoterpene camphor was the major component in all tissues of C. camphora except for safrole in the root. With chiral GC-MS, the enantiomeric distributions of 12, 12, 13, 14, and 14 chiral compounds in branch, wood, root, leaf/branch, and leaf/branch/wood, respectively, were determined. The variation in composition and enantiomeric distribution in the different tissues of C. camphora may be attributed to the different defense requirements of these tissues. The wood essential oil showed effective antibacterial activity against Serratia marcescens with an MIC of 39.1 μg/mL. Similarly, the mixture of leaf/branch/wood essential oils displayed good antifungal activity against Aspergillus niger and Aspergillus fumigatus while the leaf essential oil was notably active against Trichophyton rubrum. C. camphora essential oils showed variable antimicrobial activities against dermal and pulmonary-borne microbes.     

Chemical composition and biological activities of essential oil from Filifolium sibiricum (L.) Kitam

The essential oil from Filifolium sibiricum (L.) Kitam were extracted using hydrodistillation and GC-MS was used to analyse the essential oil. The main components were espatulenol (8.55%), geranyl acetate (8.03%), caryophyllene oxide (5.47%), calamenene (4.79%), geraniol (4.28%), calamenene (4.53%), geraniol (4.06%), cedrene epoxide (3.23%), myrtenol (3.18%), transgeranylgeranio (3.13%), etc. The essential oil showed intensive inhibitory effects against MCF-7 with IC₅₀ level of 0.78 mg/mL, HepG-2 with IC₅₀ level of 0.44 mg/mL, SKOV-3 with IC₅₀ level of 0.27 mg/mL, BGC-823 with IC₅₀ level of 0.34 mg/mL. In the antibacterial test, the essential oil showed the significant antibacterial activities. The MIC and MBC values were 5.20 and 5.20 mg/mL against Staphylococcus aureus.     

儿茶素-银纳米复合材料的制备及其应用

探索了以植物活性成分儿茶素作为还原剂和保护剂一步水热法合成儿茶素-银纳米复合材料,并进一步测试了纳米复合材料的抑菌活性。 紫外可见吸收光谱(UV-Vis)和红外光谱(FTIR)测定证明制备得到了儿茶素包裹的银纳米粒子。 透射电子显微镜(TEM)和X射线衍射(XRD)结果显示银纳米粒子的平均粒径为22.7 nm,并具有面心立方晶体结构。 抑菌活性实验结果表明,儿茶素-银纳米复合粒子对大肠杆菌、金黄色葡萄球菌以及白色念球菌都有很强抑制作用,尤其对白色念球菌的抑制作用最强,其最低抑制浓度(MIC)和最低杀菌浓度(MBC)分别为19.63和39.26 μg/mL。 儿茶素-银纳米粒子强抑菌活性可归因于其表面银离子的持续释放,有望应用于长效抑菌制剂产品。     

Cytotoxicity of Essential Oil Cordia verbenaceae against Leishmania brasiliensis and Trypanosoma cruzi

The species Cordia verbenacea DC (Boraginaceae), known as the whaling herb and camaradinha, is a perennial shrub species native to the Atlantic Forest. Its leaves are used in folk medicine as an anti-inflammatory, analgesic, antiulcerogenic and curative agent, in the form of teas or infusions for internal or topical use. The present study aimed to verify the cytotoxicity of the essential oil and the leishmanicidal and trypanocidal potential of C. verbenacea. The essential oil was characterized by GC-MS. The in vitro biological activity was determined by anti-Leishmania and anti-Trypanosoma assays. The cytotoxixity was determined using mammalian fibroblasts. The C. verbenacea species presented α-pinene (45.71%), β-caryophyllene (18.77%), tricyclo[2,2,1-(2.6)]heptane (12.56%) as their main compounds. The essential oil exhibited strong cytotoxicity at concentrations below 250 μg/mL (LC₅₀ 138.1 μg/mL) in mammalian fibroblasts. The potent anti-trypanosome and anti-promastigote activities occurred from the concentration of 62.5 μg/mL and was considered clinically relevant. The results also demonstrate that at low concentrations (<62.5 μg/mL), the essential oil of C. verbenacea managed to be lethal for these activities. This can be considered an indication of the power used in daily human consumption. Therefore, it can be concluded that the essential oil of C. verbenacea contains a compound with remarkable antiparasitic activities and requires further research.     

Chemical composition of essential oils from different parts of Protium heptaphyllum (Aubl.) Marchand and their in vitro antibacterial activity

Abstract

In Brazilian folk medicine, Protium heptaphyllum is used to treat inflammatory conditions and to hasten wound repair. This paper aims to investigate the chemical composition and the in vitro antibacterial effects of the essential oils (EOs) obtained from P. heptaphyllum leaves and ripe and unripe fruits against a representative panel of oral pathogens. The GC-FID and GC-MS analysis revealed that the major components determined in P. heptaphyllum essential oils were myrcene (59.0%), β-elemene (17.2%), limonene (12.9%), spathulenol (12.6%), α-cubebene (11.6%), germacrene D (10.6%), trans-nerolidol (9.8%), and α-cadinol (8.8%). The essential oils of the ripe and unripe fruits showed the strongest antibacterial activity against the anaerobic bacteria Prevotella nigrescens (MIC?=?50?µg/mL). The leaf essential oil displayed very promising activity against Streptococcus mutans (MIC?=?50?µg/mL) and Streptococcus mitis (MIC?=?62.5?µg/mL). The antibacterial activity of EOs against oral pathogens is also described for the first time.

     

Variation in chemical composition and antibacterial activities of essential oils from two species of Houttuynia THUNB

Houttuynia THUNB. (Saururaceae) has been used for dozens of years in China for the treatment of cough, leucorrhea and ureteritis. The essential oils from the two species: Houttuynia emeiensis and Houttuynia cordata sold in China under one trade name 'Yuxingcao', obtained by hydrodistillation, were analyzed by GC-MS. The results show that fifty-five components were identified and methyl nonyl ketone (2.10-40.36%), bornyl acetate (0.4-8.61%) and beta-myrcene (2.58-18.47%) were the most abundant components in oil, but the percentage of most of compounds in different species and parts varied greatly. The two fold broth dilution and agar dilution method were used to study essential oil of two Houttuynia THUNB. species for their antibacterial properties against microorganisms, Staphylococcus aureus and Sarcina ureae. The two fold dilution method was allowed to determine the minimum inhibitory concentration (MIC) of essential oil from different parts and species. Results showed that all essential oils possessed antibacterial effect, with MIC values in the range of 0.0625 x 10(-3) to 4.0 x 10(-3) ml/ml. However, essential oil from different parts and species differed clearly in their antibacterial activities. The essential oil from the aboveground part of the cultivated Houttuynia emeiensis exhibited higher activity than both parts of the wild and cultivated Houttuynia cordata when used on Staphylococcus aureus (MIC = 0.25 x 10(-3) ml/ml) and Sarcina ureae (MIC = 0.0625 x 10(-3) ml/ml), and had the same activity as the positive control ampicillin sodium.