栀子中西红花苷和gardecin的抗氧化活性研究

目的 对比研究栀子中新化合物gardecin与不同结构西红花苷的抗氧化活性.方法 分别采用OH自由基清除活性、还原能力模型、Fe2+螯合能力和亚硝酸盐抑制模型对比测定前期分离获得的gardecin与3个不同结构西红花苷的抗氧化活性.结果 在4个实验模型中,gardecin的半数抑制率(或半数有效率)显著低于其他不同结构西红花苷.西红花苷结构上糖数量的增加,也逐渐增强了其抗氧化活性.结论 gardecin具有较其他西红花苷更强的抗氧化活性,西红花苷结构中的糖有利于抗氧化活性的发挥.     

西红花苷防治中枢神经系统疾病的研究进展

西红花苷是西红花中活性成分，具有多种药理作用。西红花苷具有出色的中枢神经系统保护作用，可以多维度、多途径地改善中枢神经系统疾病的神经功能，能抗抑郁、抗癫痫，对帕金森病、阿尔茨海默病、缺血性脑卒中、多发性硬化具有神经保护作用。综述了西红花苷防治中枢神经系统疾病的研究进展，以期提高西红花苷在临床治疗中的转化和应用。     

西红花苷和西红花酸在小鼠体内抗氧化活性对比研究

目的对比评价西红花苷和西红花酸在小鼠体内抗氧化活性。方法采用硅胶柱层析从栀子中分离西红花酸和西红花苷纯品,普通昆明小鼠灌胃给药西红花酸和西红花苷,剂量分别是西红花酸6.25、12.5和25.0mg·kg-1和西红花苷18.7、37.5和75.0mg·kg-1.d-1,采用测定普通小鼠体内抗氧化指标(SOD、GSH-Px、TAOC和MDA)的方法对比评价西红花酸和西红花苷-1体内抗氧化活性。结果两种化合物都能明显提高小鼠肾脏和肝脏的SOD,肝脏的GSH-Px,心脏和肾脏的TAOC,降低血浆的MDA。结论西红花酸和西红花苷-1具有相似的体内抗氧化活性,其主要活性部位可能是肝脏和肾脏。     

西红花的本草考证与名实辨析

本文考证了藏红花的国内外应用历史和应用领域,还根据历朝历代的应用情况和现代应用领域、质量标准等,规范了番红花、藏红花和西红花的名称指代：原植物称番红花;番红花红色柱头的加工品为商品,药用的称西红花,其他领域应用的称藏红花。     

栀子黄色素抗脂质过氧化能力与主成分含量的相关性研究

目的揭示栀子黄色素的抗脂质过氧化能力与多酚、栀子苷和西红花苷-Ⅰ含量的关系,明确栀子黄色素中主要的抗脂质过氧化成分。方法采用大孔树脂HPD100和乙酸乙酯纯化栀子黄色素,用福林-酚法测定多酚含量,HPLC法测定栀子苷含量,UV法测定西红花苷-Ⅰ含量,并采用硫氰酸铁法评价抗脂质过氧化能力。结果抗脂质过氧化能力随绿原酸(0.001~0.006 7mg·mL~(-1))、栀子苷(0.002 5~0.013mg·mL~(-1))和西红花苷-Ⅰ(0.001 5~0.004mg·mL~(-1))质量浓度的增大而增强,质量浓度为0.002mg·mL~(-1)时,抗脂质过氧化能力绿原酸>西红花苷-Ⅰ>栀子苷。结论栀子黄色素中多酚、栀子苷和西红花苷-Ⅰ都具有抗脂质过氧化的能力。     

西红花苷对低密度脂蛋白所致鹌鹑内皮细胞损伤的保护作用

目的探讨西红花苷对低密度脂蛋白(LDL)所致内皮细胞损伤的保护作用。方法在体外培养牛主动脉内皮细胞中,加入不同剂量的西红花苷培养12 h后,再加入50μg.ml-1的LDL继续培养24 h,测定培养液中NO含量,测定细胞中一氧化氮合酶(NOS)的活性。在鹌鹑饮食性动脉粥样硬化模型上,观察西红花苷连续9周预防性给药对血清LDL和血清NO的影响。结果西红花苷可浓度依赖性地提高细胞内NOS的活性(P<0.01),使细胞合成分泌的NO含量升高(P<0.01)。西红花苷能显著降低血清LDL水平,使血清NO含量提高。结论西红花苷对LDL所致内皮细胞损伤有保护作用。     

西红花苷对氧化性低密度脂蛋白致内皮细胞损伤的保护作用

目的:探讨西红花苷对氧化性低密度脂蛋白(Ox-LDL)致内皮细胞损伤的保护作用.方法:在体外培养牛主动脉内皮细胞中,加入不同剂量的西红花苷培养12h后,再加入50μg·mL-1的Ox-LDL继续培养24h,测定培养液中乳酸脱氢酶(LDH)活性和一氧化氮(NO)的含量,测定细胞中一氧化氮合酶(NOS)的活性;利用流式细胞仪观察其对Ox-LDL诱导的内皮细胞凋亡的影响.结果:西红花苷(10,10-7,10-6mol·L-1)可剂量依赖性地抑制LDH活性及外漏(P＜0 01),提高细胞内NOS的活性(P＜0.01),使细胞分泌的NO含量升高(P＜0.01);西红花苷对Ox-LDL诱导的内皮细胞凋亡有抑制作用.结论:西红花苷对Ox-LDL致内皮细胞损伤有保护作用.     

黄芩苷药理作用研究新进展

目的介绍黄芩苷药理作用研究新进展。方法根据发表的相关黄芩苷的文献进行综述。结果黄芩苷除了传统的镇静、降压、清除自由基、抗心律失常等作用外,还发现其具有抗肺炎衣原体所致的动脉粥样硬化作用,对缺血再灌注损伤的大脑和心肌具有保护作用,对不同原因引起的肝损伤具有保护作用,能显著促进成纤维细胞增殖,对人牙周膜成纤维细胞具有保护作用,在体外对某些寄生虫均有明显的抑制和杀灭作用。结论黄芩苷的开发利用主要是应用其抗炎、降压等活性,对其他药理活性的研究利用相对较少;黄芩苷还具有广泛的药理活性,如缺血再灌注损伤的保护作用、肝损伤的保护作用等,有着广泛的开发与应用前景。     

药食同源物质西红花及其主要活性成分的健康危害评估

目的西红花是一种具有独特的香气、味道、颜色和药用价值的药食同源物质,可用于活血化瘀,凉血解毒,解郁安神,用于经闭癥瘕,产后瘀阻,温毒发斑,忧郁痞闷,惊悸发狂。有必要对西红花及其主要活性成分进行危害评估。方法本文基于系统文献检索法,检索了中英文数据库和食药健康相关的官方网站。结果西红花在临床用量上对人体重要脏器没有毒性,职业接触西红花会增加孕妇流产风险。结论实验动物急性暴露西红花的柱头和花瓣提取物的毒性分级是"低毒"级,西红花醛的急性毒性高于西红花苷;亚急性暴露的可见血液学改变、肝肾功能改变和致畸作用,西红花苷在治疗剂量下没有器官毒性,西红花醛对血液和生化指标的影响较明显。     

比较西红花酸和西红花苷对异丙肾上腺素损伤心肌的作用

目的:比较口服西红花酸和西红花苷对异丙肾上腺素(ISO)所致原代心肌细胞损伤和大鼠心肌缺血的影响.方法:培养原代乳鼠心肌细胞,用ISO诱导心肌细胞损伤,给予含药血清,测定LDH、CK和MTT;用ISO诱导大鼠心肌缺血模型,灌胃给药,测定心电、生化指标和病理改变.结果:西红花酸血清减少心肌细胞跳动变化和CK、LDH释放,增加细胞活力,而西红花苷血清对上述指标没有影响;灌胃西红花酸能对抗ISO引起J点和T波抬高,降低CK、LDH、MDA,升高SOD,改善心肌病理变化,而灌胃西红花苷对上述指标没有作用.结论:西红花酸对ISO所致心肌细胞损伤和心肌缺血有改善作用,而西红花苷不具有该作用.提示临床治疗心肌缺血应口服西红花酸,西红花苷不适合口服.     

Bioactivity assessment and toxicity of crocin: A comprehensive review

Since ancient times, saffron, the dried stigma of the plant Crocus sativus L. has been extensively used as a spice and food colorant; in folk medicine it has been reputed to be efficacious for the alleviation and treatment of ailments. In addition to the three founded major constituents including crocin, picrocrocin and safranal, presence of carotenoids, carbohydrates, proteins, anthocyanins, vitamins and minerals provide valuable insights into the health benefits and nutritional value of saffron. Of the carotenoids present in saffron, highly water-soluble crocin (mono and diglycosyl esters of a polyene dicarboxylic acid, named crocetin) is responsible for the majority of its color, and appears to possess various health-promoting properties, as an antioxidant, antitumor, memory enhancer, antidepressant, anxiolytic and aphrodisiac. It is also worth noting that the crocin principle of saffron exhibited high efficacy along with no major toxicity in experimental models. We would be remiss to not consider the great potential of saffron and crocin, which benefits the cuisine and health of human life throughout the world. The present study provides a comprehensive and updated report of empirical investigations on bioactivities and biological characteristics of crocin.     

Improvement of cytotoxic and apoptogenic properties of crocin in cancer cell lines by its nanoliposomal form

Objective: Saffron Crocus sativus L. (Iridaceae) is known for anticancer properties. However, limited effort has been made to correlate these effects to the active ingredients of saffron. In the present study, cytotoxic effects of crocin, the major coloring compound in saffron, and its nanoliposomal form for better cellular delivery are investigated.

Methods: HeLa and MCF-7 cells were cultured and exposed to crocin (1, 2, and 4?mM) and liposomal crocin (0.5 and 1?mM). The 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay was performed to assess cytotoxicity. Apoptotic cells were determined using propidium iodide (PI) staining of DNA fragmentation by flow cytometry.

Results: MTT assay revealed a remarkable and concentration-dependent cytotoxic effect of crocin on HeLa and MCF-7 cells in comparison with non-malignant cell line (L929). Crocin liposomal forms (IC₅₀ values after 48 h: 0.61, 0.64, and 1.2?mM) showed enhanced cytotoxic effect compared with the crocin (IC₅₀ after 48 h: 1.603?mM) in HeLa cells. Crocin and its liposomal form induced a sub-G1 peak in flow cytometry histogram of treated cells indicating apoptosis is involved in this toxicity. Liposomal encapsulation enhances apoptogenic effects of crocin on cancerous cells.

Conclusion: It might be concluded that crocin and its liposomes could cause cell death in HeLa and MCF-7 cells, in which liposomal encapsulation improved cytotoxic effects. They could be also considered as a promising chemotherapeutic agent in cancer treatment in future.     

多波长高效液相色谱法同时测定栀子中的三类成分

目的同时测定栀子中3类有效组分，9个成分（栀子酸、栀子苷、异栀子苷、京尼平龙胆二糖苷、绿原酸、藏红花酸、3种藏红花素）的含量。方法紫外-可见三波长同时检测的高效液相色谱法：色谱柱为Phenomenex Luna C₁₈柱（250 mm×4.6 mm ID，5 μm）；流动相为(A)0.3％甲酸水溶液, (B)甲醇-乙腈（9∶1）；流速为0.8 mL·min^-1；柱温为35 ℃；检测波长为 240 nm(栀子酸、栀子苷、异栀子苷、京尼平龙胆二糖苷), 330 nm(绿原酸)和440 nm(藏红花酸和3种藏红花素)；线性梯度洗脱。结果建立了同时对栀子中的9个成分进行定量的测定方法，并将此方法用于5个产地栀子各成分的测定。结论为中药材栀子提供了更合理、可靠的质控方法。     

Crocin exerts anti-inflammatory and anti-arthritic effects on type II collagen-induced arthritis in rats

Context: Rheumatoid arthritis (RA) is a common systemic auto-immune disease, which is characterized by chronic and symmetry synovial inflammation. Crocin has been reported to exhibit anti-inflammatory effects in animal models.

Objective: This study investigates the anti-inflammatory and anti-arthritic effects of crocin on type II collagen-induced arthritis (CIA) in Wistar rats.

Materials and methods: The CIA rat model was established and randomly divided into five groups with or without crocin treatment (10, 20 or 40?mg/kg), which was started on day 21 after arthritis induction and persisted for 36 days. The symptoms and molecular mechanisms of CIA and crocin-treated CIA rats were compared and investigated.

Results: CIA rats presented severe RA symptoms, including high arthritis score, paw swelling, joint inflammation, bone erosion, chondrocyte death, cartilage destruction, enhanced expressions of matrix metalloproteinase (MMP) and pro-inflammatory cytokines. However, crocin could mitigate these symptoms. Crocin (40?mg/kg) exhibited the most efficient therapeutic function on CIA rats: the histological scores of joint inflammation, bone erosion, chondrocyte death, cartilage surface erosion, and bone erosion of CIA rats receiving 40?mg/kg crocin treatment were comparable to the normal rats. MMP-1, -3 and -13 protein expression levels of CIA rats with 40?mg/kg crocin treatment were decreased to levels similar to normal rats. Moreover, crocin could also inhibit the expression of TNF-α, IL-17, IL-6 and CXCL8 in serum and ankle tissues of CIA rats.

Conclusions: In summary, crocin exhibits therapeutic potential for RA, by mitigating the symptoms and inhibiting the pro-inflammatory factor expression.     

Crocin Attenuates Kindling Development and Associated Cognitive Impairments in Mice via Inhibiting Reactive Oxygen Species‐Mediated NF‐κB Activation

Crocin is a pharmacologically active carotenoid pigment mainly present in the stigmas of Crocus sativus L. (Iridaceae). It has been well explored in experimental animal models of cognitive impairments, depression, anxiety and epilepsy. This study was designed to understand the effect of crocin on pentylenetetrazol (PTZ)‐induced kindling development and its associated cognitive deficit in mouse. Crocin treatment at 5, 10 and 20 mg/kg p.o. doses showed a marked reduction in severity of PTZ‐induced seizures. There was an increase in novel object preference index and discrimination ratio in the crocin‐treated groups in the novel object recognition test. Its treatment also increased percentage spontaneous alternations in T‐maze test at all the tested doses. Histopathological examination by Nissl staining showed a reduction in dark neurons in the hippocampal pyramidal layer of crocin‐treated animals in contrast to vehicle control, indicating a decrease in neuronal damage. Biochemical estimations showed a significant increase in superoxide dismutase activity and reduced reactive oxygen species (ROS) in the hippocampus of crocin‐treated animals. Immunohistochemistry results revealed attenuation in the levels of nuclear factor‐κB (NF‐κB) and phosphorylated NF‐κB in the hippocampal sections of crocin‐treated animals. The results of this study concluded that crocin treatment increased seizure threshold, thus inhibiting PTZ‐induced kindling development and improving cognitive functions. The effect was found to be due to suppression of seizure‐induced ROS generation and its linked NF‐κB pathway‐associated neuronal damage.     

Therapeutic implications of crocin in Parkinson's disease: A review of preclinical research

Parkinson's disease is among the most common forms of neurodegenerative illness, with present treatment being primarily symptomatic and frequently coming with substantial adverse effects. Neuronal degeneration may arise due to a variety of pathological events, like inflammatory responses, neurotransmitter dysregulation, oxidative damage, mitochondrial malfunction, apoptosis, and genetic factors. The health issue and financial burden brought on by Parkinson's disease can worsen as the population ages. In the search for new and secure therapeutic agents for Parkinson's disease, several natural compounds have been shown to exert considerable neuroprotective benefits. Crocin, a naturally occurring carotenoid molecule, was found to have neuroprotective potential in the therapy of this disorder. Taking into account, the outcomes of various studies and the restorative actions of crocin, the present study emphasized the protective ability of crocin in this disease. Given the strong evidence supporting the neuroprotective ability of crocin, it is inferred that crocin inhibits inflammatory, apoptotic, and antioxidant processes through multiple mechanisms. Therefore, this compound is considered a safe and effective therapeutic choice for neurodegenerative illnesses like Parkinson's disease. However, more research on its efficacy as a treatment of Parkinson's disease is needed, specifically examining its mechanisms and the results obtained in clinical trials.     

The mechanism of protective effect of crocin against liver mitochondrial toxicity caused by arsenic III

In this study, we want to understand whether crocin could prevent mitochondrial damage caused by As III. For this purpose, we determined different mitochondrial toxicity endpoints caused by As III. We evaluated mitochondrial ROS formation, lipid peroxidation, mitochondrial membrane potential (MMP) collapse, mitochondrial outer membrane integrity and cytochrome c release. Our results showed that pretreatment with crocin at a concentration of 25?µg/ml significantly (p?相似文献   

Antidepressant properties of bioactive fractions from the extract of <Emphasis Type="Italic">Crocus sativus</Emphasis> L.

The aim of this study was to investigate the antidepressant properties of stigmas and corms of Crocus sativus L. The aqueous ethanol extract of C. sativus corms was fractionated on the basis of polarity. Among the different fractions, the petroleum ether fraction and dichloromethane fraction at doses of 150, 300, and 600 mg/kg showed significant antidepressant-like activities in dose-dependent manners, by means of behavioral models of depression. The immobility time in the forced swimming test and tail suspending test was significantly reduced by the two fractions, without accompanying changes in ambulation when assessed in the open-field test. By means of a gas chromatography–mass spectrometry technique, twelve compounds of the petroleum ether fraction were identified. These data show that administration of C. sativus corms extract produces antidepressant-like effects. Aqueous stigmas extract also exerted antidepressive effects in the behavioral models. Crocin 1 and crocin 2 of the aqueous stigmas extract were identified by a reversed-phase HPLC analysis. In addition, the bioactive compound crocin 1 in this herb was quantitatively determined. The data indicate that antidepressant-like properties of aqueous stigma extracts may be due to crocin 1, giving support to the validity of the use of this plant in traditional medicine. All these results suggest that the low polarity parts of C. sativus corms should be considered as a new plant material for curing depression, which merit further studies regarding antidepressive-like activities of chemical compounds isolated from the two fractions and mechanism of action.     

A study on the toxicity of natural food dyes--toxicity and enzyme inhibition in Paramecium caudatum.

The toxicity of 14 commercial natural dyes which are widely used as food additives in Japan was studied on Paramecium caudatum. Laccaic acid and capsanthin were found to be very toxic to Paramecium caudatum. Some of the commercially available carminic acid and crocin were also toxic. The inhibitory effect of natural food dyes on leucine aminopeptidase, acid phosphatase and esterase in vitro was proportional to the toxic effect of the dyes on the survival time of Paramecium caudatum. Analyses of the commercial natural food dyes by high performance liquid chromatography failed to identify the toxic components.