Cinnamon (Cinnamomum zeylanicum) as an antidote or a protective agent against natural or chemical toxicities: a review

Cinnamon (Cinnamomum zeylanicum, Lauraceae) is a food additive greatly used for its taste. However, recently this medicinal plant has been brought to attention due to its medical effects. Cinnamon has constituents such as cinnamaldehyde and cinnamic acid that offers some health benefits including antioxidant and free-radical scavenging properties, lowering of blood glucose, anti-cholesterolemic, analgesic, antimicrobial, anti-inflammatory, anti-yeast, anti-secretagogue, and anti-gastric ulcer effects. This review summarizes various in vitro and animal studies on the protective effects of cinnamon against natural and chemical toxins. These studies consider the antidotal and/or protective effects of cinnamon and its major constituents against natural toxins and chemical-induced toxicities. It has been mentioned that cinnamon and its main constituents can ameliorate the toxicity of chemical toxins in liver, kidney, blood, brain, embryo, reproductive system, heart, spleen in part through antioxidant effect, radical scavenging, reducing lipid peroxidation, anti-inflammatory, fungistatic and fungicidal activities, modulation of CK-MB, LDH, TNF-α, IL-6, mitogen-activated protein kinase (MAPK), and nuclear factor-?B (NF-?B) signaling pathways.     

A potential in vitro epidermal equivalent assay to determine sensitizer potency

Most in vitro assays aim to distinguish sensitizers from non-sensitizers. Few aim to classify sensitizers according to potency. Here, we describe a potential method for classifying sensitizers according to their irritant potency with the aid of in house epidermal equivalents (EE). Sixteen sensitizers were applied topically in a dose response to EE for 24 h. The EE-EC₅₀ value (effective chemical concentration required to reduce cell viability by 50%) and the EE-IL-1α_10× value (chemical concentration which increases IL-1α secretion by 10-fold) were calculated. From 16 sensitizers, EE-EC₅₀ and/or EE-IL-1α_10× values were obtained from 12 skin sensitizers. EE-EC₅₀ and IL-1α_10× values decreased in proportion to increasing sensitizer potency. The in vitro assay correlated with existing in vivo mouse and human sensitization data (LLNA, HRIPT), and showed low intra- and inter-experimental variability. Additionally DNCB and resorcinol were correctly assessed as extreme and moderate sensitizers using commercial EE (EST1000™ and RHE™). In conclusion, our data supports the view that irritancy may in part be a factor determining sensitizer potency. Since this assay does not distinguish sensitizers from non-sensitizers, its potential application is in a tiered strategy, where Tier 1 identifies sensitizers which may then tested in Tier 2, this assay, which determines sensitizer potency.     

Proton pumping ATPase mediated fungicidal activity of two essential oil components

This work evaluates the antifungal activity of two essential oil components against 28 clinical isolates (17 sensitive, 11 resistant) and 3 standard laboratory strains of Candida. Growth of the organisms was significantly effected in both solid and liquid media at different test compound concentrations. The minimum inhibitory concentrations (MICs) of Isoeugenol (compound 1) against 31 strains of Candida ranged 100–250 μg/ml and those of o ‐methoxy cinnamaldehyde (compound 2) ranged 200–500 μg/ml, respectively. Insight studies to mechanism suggested that these compounds exert antifungal activity by targeting H⁺‐ATPase located in the membranes of pathogenic Candida species. At their respective MIC₉₀ average inhibition of H⁺‐efflux for standard, clinical and resistant isolates caused by compound 1 and compound 2 was 70%, 74%, 82% and 42%, 42% and 43%. Respective inhibition of H⁺‐efflux by fluconazole (5 μg/ml) was 94%, 92% and 10%. Inhibition of H⁺‐ATPase leads to intracellular acidification and cell death. SEM analysis of Candida cells showed cell membrane breakage and alterations in morphology. Haemolytic activity on human erythrocytes was studied to exclude the possibility of further associated cytotoxicity. (© 2012 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)     

Classification of sensitizing and irritative potential in a combined in-vitro assay

We have developed a coculture system which in parallel indicates the sensitizing and irritative potential of xenobiotics. The assay is named loose-fit coculture-based sensitization assay (LCSA) and may be performed within 5 days. The system is composed of human monocytes that differentiate to a kind of dendritic cells by 2-day culturing in the presence of allogenic keratinocytes. The culture medium is enriched by a cocktail of recombinant cytokines. On day 3, concentration series of probes are added. On day 5, cells are harvested and analyzed for expression range of CD86 as a marker of sensitizing potential and for uptake of the viability stain 7-AAD as a marker of irritative potential. Estimation of the concentration required to cause a half-maximal increase in CD86 expression allowed quantification of sensitizing potential, and estimation of the concentration required to reduce viability to 50% allowed quantification of irritative potential. Examination of substances with known potential resulted in categorization of test scores. To evaluate our data, we have compared results with those of the validated animal-based sensitization test, the murine local lymph node assay (LLNA, OECD TG 429). To a large extent, results from LCSA and from LLNA achieved analogous grouping of allergens into categories like weak-moderate-strong. However, the new assay showed an improved capacity to distinguish sensitizers from non-sensitizers and irritants. In conclusion, the LCSA contains potential to fulfil the requirements of the EU's programme for the safety of chemicals “Registration, Evaluation, Authorisation and Restriction of chemical substances” (REACH, 2006) to replace animal models.     

HPLC法测定颈椎通络丸桂皮醛、芍药苷含量

目的:采用HPLC方法测定颈椎通络丸桂皮醛、芍药苷含量。方法:色谱柱C18(200×4.6mm,5μm);桂皮醛、芍药苷流动相与测定波长分别为甲醇-1%磷酸(300:200)与乙腈-0.1%磷酸溶液(22:78);290nm与230nm;流速:1mL.min-1;结果:桂皮醛与芍药苷分别在0.02～0.64?g与0.0182～0.546?g之间成线性关系(r=0.999)。回收率分别为100.0%与103.0%;颈椎通络丸桂皮醛、芍药苷平均含量分别为0.24 mg﹒g-1、0.16 mg﹒g–1。结论:采用本法测定颈椎通络丸桂皮醛、芍药苷含量,操作简便,准确可靠,可用于制定该药品的质量控制指标之一。     

HPLC法测定大鼠血浆中色胺酮的浓度及药代动力学参数

目的建立测定血浆中色胺酮含量的HPLC法,并用于色胺酮在大鼠体内的药代动力学研究。方法采用ODSC18色谱柱(4.6 mm×250 mm),流动相为乙腈∶水(47∶53),流速为1.0 ml.min-1,检测波长为251 nm,柱温30℃,进样量20μl,内标物为桂皮醛。按56 mg.kg-1剂量给大鼠灌胃后,用HPLC法测定给药后不同时刻大鼠血浆中色胺酮的浓度。采用DAS 2.1.1软件分析,计算药动学参数。结果色胺酮在0.0183～1.1712 mg.L-1范围内线性关系良好(r2=0.999),最低定量限为0.02 mg.L-1。回收率大于95.0%,其日内、日间RSD均小于8%。大鼠灌胃色胺酮56mg.kg-1后,♀和♂T12分别为4.314和5.597 h,Tmax分别为5.2和4.6 h,Cmax分别为1.887和2.620 mg.L-1,AUC0→t分别为12.1和14.70 mg.h.L-1。结论本方法操作简便,准确,灵敏度高、重复性好,可用于色胺酮血药浓度检测及药代动力学研究。     

肉桂油对病毒性心肌炎小鼠心肌中TLR4-NF-κB信号转导的影响

 目的 探讨肉桂油（OC）治疗病毒性心肌炎（VMC）的作用机制。方法 经腹腔注射0.1 mL柯萨奇病毒B组3型（CVB₃）建立小鼠VMC模型。于接种病毒72 h后，OC（30 mg·kg^-1肉桂油 ）、肉桂醛(CA)治疗组（30 mg·kg^-1 桂皮醛）、模型组与正常对照组（等体积生理盐水），连续给药至第21天。在病毒感染后第10天(n=9)和第21天、各组随机取小鼠称体重，摘眼球取血后处死，取心脏，计算心脏质量/体重比；心脏一分为二，一半用作CVB₃ mRNA的RT-PCR检测和WESTERN BLOT技术检测以及诱导型一氧化氮合酶（iNOS），肿瘤坏死因子（TNF）-α，NF-κB P65和TLR4蛋白质的表达水平；另一半作石蜡切片，HE染色和iNOS免疫组化染色；试剂盒检测第10天血清中NO水平；整个实验期间观察纪录小鼠累积死亡数及存活时间。结果 与模型组相比，OC和CA治疗组小鼠的死亡率均显著降低(P<0.01），中位生存时间延长，第10天心肌中CVB₃ mRNA含量下降（P<0.05）和血清NO含量下降（P<0.01）。心肌中iNOS，TNF-α，NF-κB P65和TLR4蛋白质表达显著降低（P<0.05）；第10天和第21天病理评分显著降低（P<0.05），组间比较无统计学差异（P＞0.05）。结论 证实OC治疗VMC的作用机制可能与其有效成份CA抑制体内TLR4-NF-κB信号转导有关。
     

高效液相色谱法测定肉桂中桂皮醛含量的研究

[目的]建立高效液相色谱法测定肉桂中桂皮醛的含量。[方法]采用高效液相色谱法,依利特ODS柱(150mm×4.6mm,5μm);用乙腈-水(35:65)为流动相;流速为1mL/min;进样量:10μL;柱温20℃;采用二极管阵列检测器。[结果]肉桂在0.01023-0.2046μg的范围内呈良好的线性关系。r=0.9999(n=5)平均回收率为99.12%RSD=2%。[结论]较紫外分光光度法更方便、快捷且稳定可行,可作为中间产品的质量控制方法。     

多指标综合评分法对肉桂不同软化方法的比较研究

目的以水溶性浸出物、挥发油、肉桂醛及肉桂酸的含量为指标对浸泡法、淋润法、减压冷浸法这3种软化方法进行研究,选出肉桂的最佳软化方法。方法按照《中国药典》规定的方法测定各组样品的水溶性浸出物及挥发油含量,采用高效液相色谱法(HPLC)测定肉桂醛及肉桂酸的含量,采用多指标综合评分法分析结果。结果各指标综合评分结果为减压冷浸法浸泡法原药材淋润法。结论减压冷浸法制得的饮片色泽好、香气浓烈,软化时间短,有效成分损失较少,减压冷浸法为肉桂最佳的软化工艺。     

基于HPLC指纹图谱和LC-Q-TOF/MS的加味黄芪桂枝五物汤化学成分研究

目的 建立加味黄芪桂枝五物汤（Jiawei Huangqi Guizhi Wuwu Decoction,JHD）HPLC指纹图谱,鉴定其主要化学成分,并阐明指纹图谱共有峰的成分归属。方法 HPLC指纹图谱检测采用Hypersil ODS色谱柱（250 mm×4.6 mm,5 μm）;流动相为乙腈-0.2%甲酸水溶液,梯度洗脱,体积流量1 mL/min,检测波长为250 nm,柱温为30℃;运用“中药色谱指纹图谱相似度评价系统”进行相似度评价,并以高效液相色谱串联四级杆飞行时间质谱（liquid chromatography-quadrupole time-of-flight mass spectrometry,LC-Q-TOF/MS）方法对指纹图谱中化学成分进行分析,通过对照品、化合物质谱信息结合文献报道鉴定其结构,进一步通过药材指纹图谱阐明共有峰的成分归属。结果 建立了JHD的HPLC指纹图谱,确定了20个共有峰,10批样品相似度为0.920～0.990。在此基础上共鉴定出JHD中70个化学成分,包括28个黄酮类、23个三萜类、5个单萜苷类、5个有机酸类、5个姜辣素类及4个其他类化合物。结论 HPLC指纹图谱结合LC-Q-TOF/MS定性鉴别,能够体现JHD组分的整体特征,可为其质量控制研究奠定基础。