Spice oil cinnamaldehyde exhibits potent anticandidal activity against fluconazole resistant clinical isolates

Fluconazole resistance is becoming an important clinical concern. We studied the in vitro effects of cinnamaldehyde against 18 fluconazole-resistant Candida isolates. MIC₉₀ of cinnamaldehyde against different Candida isolates ranged 100–500 μg/ml. Growth and sensitivity of the organisms were significantly affected by cinnamaldehyde at different concentrations. The rapid irreversible action of this compound on fungal cells suggested membrane-located targets for its action. Insight studies to mechanism suggested that cinnamaldehyde exerts its antifungal activity by targeting sterol biosynthesis and plasma membrane ATPase activity. Inhibition of H⁺-ATPase leads to intracellular acidification and cell death. Toxicity against H9c2 rat cardiac myoblasts was studied to exclude the possibility of further associated cytotoxicity. The observed selectively fungicidal characteristics against fluconazole-resistant Candida isolates signify a promising candidature of this essential oil as an antifungal agent in treatments for candidosis.     

In vitro dose–response of carvacrol, thymol, eugenol and trans-cinnamaldehyde and interaction of combinations for the antimicrobial activity against the pig gut flora

In vitro simulations of the gastric and small intestinal fermentation with varying doses of carvacrol, thymol, eugenol and trans-cinnamaldehyde and binary combinations thereof were carried out to calculate dose–response equations for the antimicrobial effect against the main pig gut flora components. Interaction effects were evaluated following the isobole method. In gastric simulations eugenol and trans-cinnamaldehyde showed clearly less inhibitory activity towards lactobacilli than carvacrol and thymol, which could also be observed in the small intestinal simulations. The minimum concentration for carvacrol, thymol, eugenol and trans-cinnamaldehyde in small intestinal simulations to reduce the number of total anaerobic bacteria compared to control with a probability of 99.7% was 255, 258, 223 and 56 mg/l respectively. This strong activity of trans-cinnamaldehyde was due to its effect against coliform bacteria; a dose of 104 mg/l gave a reduction of 1 log CFU/ml vs. 371, 400 and 565 mg/l for carvacrol, thymol and eugenol respectively. Few combinations demonstrated synergism; most mixtures showed zero interaction or antagonism. Only carvacrol + thymol was slightly synergistic.     

肉桂醛复合保鲜剂对南美白对虾贮藏品质的影响

为延长南美白对虾贮藏期,对8种天然化合物的抑菌和南美白对虾多酚氧化酶( PPO)抑制活性进行了对比试验,发现肉桂醛同时兼具抑菌和抑制多酚氧化酶活性的双重效果.经酶反应动力学分析,证明肉桂醛是多酚氧化酶的非竞争性抑制剂.采用正交试验,对肉桂醛、植酸和海藻酸钠进行复配比较,确定复合保鲜剂的最佳组分为:肉桂醛质量分数0.10％、植酸质量分数0.05％、海藻酸钠质量分数0.50％.复合保鲜剂处理可有效抑制虾体菌落总数的增加和挥发性盐基氮的积累;同时还可抑制贮藏过程中的脂肪氧化,对感观品质具有良好的保持作用,在(4±1)℃条件下贮藏期可达8 ～10d,明显提高了南美白对虾贮藏过程中的品质和货架期.     

肉桂醛体外抑制奶牛乳房炎主要致病菌的研究

研究天然化合物肉桂醛对奶牛乳房炎主要致病菌——大肠杆菌、金黄色葡萄球菌和链球菌的抑菌效果。采用试管二倍稀释法测得肉桂醛对奶牛乳房炎主要致病菌金黄色葡萄球菌和标准金黄色葡萄球菌的体外最小抑菌浓度(MIC)分别为3.2 mmol/L和1.6 mmol/L;链球菌1.6 mmol/L;大肠杆菌和标准大肠杆菌6.4 mmol/L和3.2 mmol/L,且能完全抑制这三种菌的生长。肉桂醛的最小杀菌浓度(MBC)金黄色葡萄球菌和标准金黄色葡萄球菌分别为25.6 mmol/L和12.8 mmol/L;链球菌12.8 mmol/L;大肠杆菌和标准大肠杆菌25.6 mmol/L和12.8 mmol/L;在7 h内能有效杀灭这三种菌,肉桂醛对奶牛乳房炎主要致病菌有抑菌和杀菌能力,是一种潜在的奶牛乳房炎的临床治疗药物。     

肉桂醛纳米乳的制备及其抑菌效果研究

为评价肉桂醛纳米乳对水产动物致病菌的抑菌效果,以吐温-80为表面活性剂、乙醇为助表面活性剂、乙酸乙酯为油相,加蒸馏水按比例配制成空白纳米乳,加入肉桂醛制备得肉桂醛纳米乳,并评价了肉桂醛纳米乳的部分特性;探究肉桂醛纳米乳对迟缓爱德华氏菌(Edwardsiella tarda)、嗜水气单胞菌(Aeromonas hydrophila)、温和气单胞菌(Aeromonas sobria)、鳗败血假单胞菌(Pseudomonas anguilliseptica)4种常见水产动物致病菌的抑菌效果。结果显示,肉桂醛纳米乳中吐温-80、乙醇、乙酸乙酯、蒸馏水和肉桂醛质量比为10∶5∶11∶73∶1,空白纳米乳对肉桂醛的最大载药量为20.11 mg/m L,肉桂醛纳米乳为水包油型淡黄色澄清透明液体,粒径5~20 nm,平均粒径10.74 nm;与同浓度肉桂醛溶液相比,肉桂醛纳米乳具有更强的抑菌活性,在最大载药量时,对嗜水气单胞菌、鳗败血假单胞菌、迟缓爱德华氏菌、温和气单胞菌的抑菌强度分别提高了65.56%、46.99%、41.94%、26.91%。肉桂醛纳米乳对嗜水气单胞菌、温和气单胞菌、鳗败血假单胞菌、迟缓爱德华氏菌的最小抑菌浓度(MIC)分别0.31、0.51、0.72、1.00 mg/m L。研究表明,肉桂醛纳米乳在水产养殖中具有潜在的应用价值。     

提高丁芎癣药水质量标准的研究

[目的]提高丁芎癣药水的质量标准。[方法]建立了川芎的薄层色谱鉴别,并以气相色谱法测定丁香酚的含量。[结果]薄层色谱鉴别中,在供试品与川芎对照药材色谱相应的位置上,显相同的荧光斑点;含量测定中,丁香酚在1．0028～10．0300μg（r=0．9996）呈良好的线性关系,平均加样回收率为101．2％,RSD为2．6％（n=9）;各阴性均无干扰。[结论]所建立的质量标准可以作为丁芎癣药水的质量控制方法。     

Suppression of mel18 enhances differentiation of acute myeloid leukemia cell line HL60 induced by cinnamaldehyde

AIM: To investigate the effect of suppression of mel18 gene on the differentiation of human acute myeloid leukemia cell line HL60 induced by cinnamaldehyde (CA). METHODS: HL60 cells were treated with low concentration of CA or all-trans retinoic acid (ATRA). shRNAmel18 vector and shRNALuc control vector were employed to package lentiviruses which were then used to infect HL60 cells. The virus-infected HL60 cells were treated with low concentration of CA, and ATRA was used as a positive control of differentiation-inducing agent. The differentiation markers on the cell surface and cell cycle of virus-infected HL60 cells were analyzed by flow cytometry. Western blot was used to determine the expression of MEL18, cyclin D1 and p27, as well as the phosphorylation level of Akt. RESULTS: Low concentration of CA and ATRA increased the expression of granulocytic differentiation marker CD11b on the HL60 cells, with the decreased expression of MEL18 in the HL60 cells. The expression of MEL18 decreased in shmel18 virus-infected HL60 cells (shmel18-HL60 cells), but did not change in shLuc-HL60 cells. The expression of CD11b on shmel18-HL60 cells increased with G₁-phase arrest, which went even higher after treatment with CA. The phosphorylation level of Akt and the expression of cyclin D1 decreased in shmel18-HL60 cells with the increase in the expression of p27. CONCLUSION: Inhibition of mel18 gene leads HL60 cell granulocytic differentiation. mel18 gene may affect the differentiation of HL60 cells by regulating cyclin D1 and p27 via PI3K/Akt signaling pathway. PI3K/Akt signaling pathway is also involved in CA-induced differentiation of HL60 cells by suppressing mel18 gene expression.     

Active components of essential oils as acaricides against Dermanyssus gallinae

ABSTRACT

1. The aim was to evaluate the acaricidal effects of pure active components of essential oils against poultry red mite (Dermanyssus gallinae) as an alternative to chemical acaricides (organophosphates and pyrethroids).

2. The toxicities of five pure active components of essential oils (eugenol from clove bud, eucalyptol from rosemary, limonene from citrus fruits, linalool from lavender and cinnamaldehyde from cinnamon) were tested on D. gallinae females in an impregnated paper assay.

3. The active substances were dissolved in water and Tween 20 and applied at concentrations ranging from 0.002 to 0.06 µl/cm². Toxicity was expressed as a lethal dose (LD₅₀ or LD₉₀).

4. The highest mortality was observed with eugenol. The LD₉₀ was estimated to be 5.1 µg/cm² for this substance, followed by cinnamaldehyde, the LD₉₀ of which was estimated to be 11.0 µg/cm². Limonene and eucalyptol were generally less effective in controlling D. gallinae.     

Anti-adenovirus effect of cinnamaldehyde

AIM: To investigate the anti-adenovirus effect of cinnamaldehyde in vitro. METHODS: The anti-adenovirus effect of cinnamaldehyde was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and virus proliferation inhibition experiment. The expression of hexon protein was measured by immunohistochemistry. RESULTS: The results of MTT and virus proliferation inhibition experiment showed that cinnamaldehyde enhanced the survival rate of the host cells, and decreased adenovirus titer by the ways of direct virus inactivation, anti-adenovirus in the stage of biosynthesis and adsorption of the adenovirus. The viability of the host cells had a positive correlation with the drug concentration under the condition of virus infection. Cinnamaldehyde did not block the virus uptake into host cells, and did not protect the host cells from infection. The expression of hexon protein was significantly lower (P<0.05) in cinnamaldehyde group than that in virus group.CONCLUSION: Cinnamaldehyde has anti-adenovirus effect, but can not directly protect host cells. The anti-adenovirus effect of cinnamaldehyde may be related with the inhibition of hexon protein expression.     

桂枝挥发油不同萃取方法的比较研究

[目的]为工业提取桂枝挥发油筛选方法。[方法]以桂皮醛为标准品,利用薄层层析法、高效液相色谱法进行含量分析,对超临界CO2萃取法和水蒸气蒸馏法提取的桂枝挥发油进行得率和纯度比较。[结果]在0.5249～2.0994μg/ml浓度范围内,桂皮醛含量与峰面积呈线性关系,其回归方程为：Y=6.0333×10^6X＋0.4573×10^6,r=0.9998;超临界CO2萃取法提取的桂枝挥发油得率较水蒸气蒸馏法提高了7.33倍,且纯度高。[结论]采用超临界CO2萃取法提取桂枝挥发油可以提高提取率。