Allicin

大蒜素
  • 文章类型: Journal Article
    我们评估了大蒜素,通过其降压和抗氧化作用,缓解血管重塑,内皮功能,和氧化应激(OS),从而改善实验性肺动脉高压(PAH)。将大蒜素(16mg/kg)给予具有PAH(野百合碱60mg/kg)的大鼠。大蒜素促进体重增加和存活率,并防止了内侧壁厚度和右心室(RV)肥大。此外,肺中血管紧张素II浓度(0.37±0.01vs.0.47±0.06pmoles/mL,大蒜素和对照,分别)和血浆(0.57±0.05vs.0.75±0.064,大蒜素和对照),肺组织中血管紧张素转换酶II和血管紧张素II1型受体的表达用大蒜素维持在正常对照水平。在用大蒜素治疗的PAH大鼠中,一氧化氮(NO)(31.72±1.22和51.4±3.45pmoles/mL),四氢生物蝶呤(8.43±0.33和10.14±0.70pmoles/mL),环磷酸鸟苷(5.54±0.42和5.64±0.73pmoles/mL),肺组织和血浆中Ang-(1-7)(0.88±0.23和0.83±0.056pmoles/mL)浓度增加,分别。相比之下,双氢生物蝶呤在肺组织和血浆中的增加都得到了阻止(5.75±0.3和5.64±0.73pmoles/mL);同时,肺组织中磷酸二酯酶-5维持在正常水平。大蒜素通过增加Nrf2在肺中的表达来预防PAH中的OS。大蒜素阻止了肺部对缺氧的反应,防止HIF-1α和VEGF的过度表达。大蒜素通过其对NO依赖性血管舒张的作用减弱PAH中的血管重塑和RV肥大,RAS的调制,和操作系统的改进。此外,这些作用可能与调节HIF-1α和改善肺氧合有关。大蒜素的整体作用有助于预防内皮功能障碍,肺动脉的重塑,和RV肥大,预防心力衰竭,从而有利于生存。虽然需要进行人体研究,数据表明,单独或联合治疗,如果我们考虑到,大蒜素可能是治疗PAH的一种替代方法,类似于目前的治疗方法,它改善肺血管舒张和增加生存率。当缺乏疗效时,大蒜素可能被认为是一种选择,在观察到药物不耐受的地方,为了增强药物的功效,或者当必须解决一种以上的致病机制时。
    We assessed whether allicin, through its antihypertensive and antioxidant effects, relieves vascular remodeling, endothelial function, and oxidative stress (OS), thereby improving experimental pulmonary arterial hypertension (PAH). Allicin (16 mg/kg) was administered to rats with PAH (monocrotaline 60 mg/kg). Allicin encouraged body weight gain and survival rate, and medial wall thickness and the right ventricle (RV) hypertrophy were prevented. Also, angiotensin II concentrations in the lung (0.37 ± 0.01 vs. 0.47 ± 0.06 pmoles/mL, allicin and control, respectively) and plasma (0.57 ± 0.05 vs. 0.75 ± 0.064, allicin and control respectively) and the expressions of angiotensin-converting enzyme II and angiotensin II type 1 receptor in lung tissue were maintained at normal control levels with allicin. In PAH rats treated with allicin, nitric oxide (NO) (31.72 ± 1.22 and 51.4 ± 3.45 pmoles/mL), tetrahydrobiopterin (8.43 ± 0.33 and 10.14 ± 0.70 pmoles/mL), cyclic guanosine monophosphate (5.54 ± 0.42 and 5.64 ± 0.73 pmoles/mL), and Ang-(1-7) (0.88 ± 0.23 and 0.83 ± 0.056 pmoles/mL) concentrations increased in lung tissue and plasma, respectively. In contrast, dihydrobiopterin increase was prevented in both lung tissue and plasma (5.75 ± 0.3 and 5.64 ± 0.73 pmoles/mL); meanwhile, phosphodiesterase-5 was maintained at normal levels in lung tissue. OS in PAH was prevented with allicin through the increased expression of Nrf2 in the lung. Allicin prevented the lung response to hypoxia, preventing the overexpression of HIF-1α and VEGF. Allicin attenuated the vascular remodeling and RV hypertrophy in PAH through its effects on NO-dependent vasodilation, modulation of RAS, and amelioration of OS. Also, these effects could be associated with the modulation of HIF-1α and improved lung oxygenation. The global effects of allicin contribute to preventing endothelial dysfunction, remodeling of the pulmonary arteries, and RV hypertrophy, preventing heart failure, thus favoring survival. Although human studies are needed, the data suggest that, alone or in combination therapy, allicin may be an alternative in treating PAH if we consider that, similarly to current treatments, it improves lung vasodilation and increase survival. Allicin may be considered an option when there is a lack of efficacy, and where drug intolerance is observed, to enhance the efficacy of drugs, or when more than one pathogenic mechanism must be addressed.
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  • 文章类型: Journal Article
    Effects of vacuum freeze drying (VFD), air impingement drying (AID), hot air drying based on temperature and humidity control (TH-HAD), pulsed vacuum drying (PVD), and medium- and short-wave infrared radiation drying (MSIRD) on the drying characteristics and physicochemical properties of garlic slices were investigated in the current work. Based on the experimental results, the Weibull model fitted the experimental results better (R2 > 0.99) than the Wang and Singh model. Samples dried with PVD showed the smallest color difference (ΔE*), better rehydration capacity and desirable reducing sugar content. In response to thermal effects and pressure pulsations, the cell walls gradually degraded, and the cell and organelle membranes ruptured. The allicin and soluble pectin contents of garlic slices treated with PVD were higher by 8.0-252.3% and 49.5-92.2%, respectively, compared to those of the samples dried by other techniques. VFD maintained a complete garlic slice structure with the minimum shrinkage and the best appearance. The MSIRD process produced the densest structure, and caused an additional loss of color and phytochemical contents. The findings in current work implied that PVD could be a promising drying technique for garlic slices.
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  • 文章类型: Journal Article
    心肌缺血再灌注(IR)损伤是由于心脏血流的最初减少而引起的损伤,阻止它接受足够的氧气,以及随后通过阻塞的冠状动脉的开口恢复血流,产生矛盾的有害影响。发现预防IR的新疗法至关重要。大蒜素是一种从大蒜中分离出来的化合物,具有预防和治疗不同疾病的能力,对心肌也有保护作用。因此,本研究旨在评价大蒜素对心肌细胞IR损伤的保护作用。
    我们建立了原代猪心肌细胞的体外缺氧-复氧(HR)模型,以模拟心肌IR损伤。从小型麝香猪(1日龄)中提取原代猪心肌细胞。经过至少2-3天的适应期,选取状况良好的心肌细胞,随机分为对照组(常氧持续5h),HR组(缺氧2h/复氧3h),和HR+大蒜素组(缺氧/复氧+大蒜素治疗)。
    诱导缺氧/复氧后,大蒜素处理增强了细胞活力。此外,与HR组相比,大蒜素处理导致细胞凋亡从13.5±1.2%减少到6.11±0.15%(p<0.05),细胞凋亡相关蛋白也受到调控,Bax的表达减少,在HR+大蒜素组中,caspase-3和胞质细胞色素C裂解,Bcl-2表达增加(均p<0.01)。促炎细胞因子,如白细胞介素-6和肿瘤坏死因子α被大蒜素治疗下调(均P<0.01)。此外,显著降低细胞内活性氧的产生(p<0.01),减少线粒体膜电位的损失(p<0.01)。此外,PPARγ共激活因子-1α和内皮型一氧化氮合酶的表达上调(p均<0.01),大蒜素处理可下调内皮素-1、缺氧诱导因子-1α和转化生长因子β的表达(均p<0.01)。
    这些结果表明大蒜素通过减少细胞凋亡保护心肌细胞免受HR损伤,炎症和线粒体损伤,从而为其在心肌IR治疗中的潜在应用提供了依据。
    Myocardial ischemia-reperfusion (IR) injury is a damage due to an initial reduction in blood flow to the heart, preventing it from receiving enough oxygen, and subsequent restoration of blood flow through the opening of an occluded coronary artery producing paradoxical harmful effects. The finding of new therapies to prevent IR is of utmost importance. Allicin is a compound isolated from garlic having the ability to prevent and cure different diseases, and a protective effect on the myocardium was also demonstrated. Therefore, the aim of this study was to evaluate the in vitro protective effect of Allicin against myocardial IR injury on cardiomyocytes.
    We established an in vitro hypoxia-reoxygenation (HR) model of primary porcine cardiomyocytes to simulate myocardial IR injury. Primary porcine cardiomyocytes were extracted from Mini-musk swines (1 day old). After a period of adaptation of at least 2-3 days, cardiomyocytes in good condition were selected and randomly divided into control group (normal oxygen for 5 h), HR group (2 h of hypoxia/3 h of reoxygenation), and HR + Allicin group (hypoxia/reoxygenation + Allicin treatment).
    After the induction of hypoxia/reoxygenation, Allicin treatment enhanced the cell viability. Moreover, Allicin treatment resulted in a reduction of apoptosis from 13.5 ± 1.2% to 6.11 ± 0.15% compared with the HR group (p < 0.05), and the apoptosis related proteins were regulated as well, with a decreased expression of Bax, cleaved caspase-3 and cytosolic cytochrome C and an increase in Bcl-2 expression in the HR + Allicin group (all p < 0.01). Pro-inflammatory cytokines, such as interleukin-6 and tumor necrosis factor alpha were down-regulated by the treatment with Allicin (both p < 0.01). In addition, it significantly decreased intracellular reactive oxygen species generation (p < 0.01) and reduced the loss of mitochondrial membrane potential (p < 0.01). Furthermore, the expression of PPARγ coactivator-1α and endothelial nitric oxide synthase was up-regulated (both p < 0.01), while the expression of Endothelin-1, hypoxia inducing factor-1α and transforming growth factor beta was down-regulated (all p < 0.01) by Allicin treatment.
    These results suggested that Allicin protected the cardiomyocytes against HR damage by reducing apoptosis, inflammation and mitochondrial injury, thus providing a basis for its potential use in the treatment of myocardial IR.
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  • 文章类型: Journal Article
    大蒜(大蒜鳞茎)和大蒜(威尔士洋葱叶)显示出鉴定化合物的定量差异:大蒜素和大蒜素(大蒜中380µg/mL和1410µg/mL;威尔士洋葱中20µg/mL和145µg/mL),和酚类化合物(绿原酸,对香豆酸,阿魏酸,龙胆酸,4-羟基苯甲酸,山奈酚,异槲皮苷,槲皮苷,槲皮素,和芦丁)。化学成分以剂量依赖性方式确定了葱提取物的抑制活性,人正常细胞(BJ-IC500.8841%大蒜/0.2433%威尔士洋葱和HaCaT-IC501.086%大蒜/0.6197%威尔士洋葱)和肿瘤细胞(DLD-1-IC505.482%/2.124%;MDA-MB-231-IC506.375%/2.464%;MCF-7-IC506.131%/3.353%;和19-4.51-MES-651)在高浓度下,每种提取物的细胞毒活性,在正常细胞上,通过以下方法证实:50%的生长抑制浓度(IC50)值,坏死诱导的细胞死亡,和生化测定LDH,过氧化氢酶,和Caspase-3。用高浓度(10%,5%,2.5%,和1.25%)的大蒜提取物表现出不同的敏感性,基于最敏感细胞系(SK-MES-1)的IC50值,和较不敏感的(MDA-MB-231)细胞系。高浓度的威尔士洋葱提取物(5%,2.5%,和1.25%)诱导培养基中的pH变化,而SK-MES-1是敏感性较低的细胞系。
    Allium sativum L. (garlic bulbs) and Allium fistulosum L. (Welsh onion leaves) showed quantitative differences of identified compounds: allicin and alliin (380 µg/mL and 1410 µg/mL in garlic; 20 µg/mL and 145 µg/mL in Welsh onion), and the phenolic compounds (chlorogenic acid, p-coumaric acid, ferulic acid, gentisic acid, 4-hydroxybenzoic acid, kaempferol, isoquercitrin, quercitrin, quercetin, and rutin). The chemical composition determined the inhibitory activity of Allium extracts in a dose-dependent manner, on human normal cells (BJ-IC50 0.8841% garlic/0.2433% Welsh onion and HaCaT-IC50 1.086% garlic/0.6197% Welsh onion) and tumor cells (DLD-1-IC50 5.482%/2.124%; MDA-MB-231-IC50 6.375%/2.464%; MCF-7-IC50 6.131%/3.353%; and SK-MES-1-IC50 4.651%/5.819%). At high concentrations, the cytotoxic activity of each extract, on normal cells, was confirmed by: the 50% of the growth inhibition concentration (IC50) value, the cell death induced by necrosis, and biochemical determination of LDH, catalase, and Caspase-3. The four tumor cell lines treated with high concentrations (10%, 5%, 2.5%, and 1.25%) of garlic extract showed different sensibility, appreciated on the base of IC50 value for the most sensitive cell line (SK-MES-1), and the less sensitive (MDA-MB-231) cell line. The high concentrations of Welsh onion extract (5%, 2.5%, and 1.25%) induced pH changes in the culture medium and SK-MES-1 being the less sensitive cell line.
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  • 文章类型: Journal Article
    Multiple drug resistance of a growing number of bacterial pathogens represents an increasing challenge in conventional curative treatments of infectious diseases. However, the development and testing of new antibiotics is associated with a high number of animal experiments.
    A symmetrical parametrized lung test rig allowing the exposure of air-passage surfaces to antibiotics was designed and tested to demonstrate proof-of-principle with aerosols containing allicin, which is an antimicrobial natural product from garlic. An artificial lung surface is coated with bacteria embedded in a hydrogel and growth inhibition is visualized by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, that is reduced from colourless to the dark blue formazan in the presence of metabolically active, living cells. A nebulizer is used to generate the aerosols.
    The results show that allicin has an antibiotic effect as an aerosol and that the deposition pattern of the active agent occurred mainly around the carinal regions.
    The model represents an integral system for continuous, spatial detection of aerosol deposition and allows the analysis of bacterial behaviour and the toxicity of the active agent. Thus, the deposition of antimicrobial aerosols on the bronchial surfaces is characterized in preliminary tests without any animal experiments.
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  • 文章类型: Clinical Trial
    Behçet\'s disease (BD) involves oxidative stress (OS) aggression and imbalanced oxidant/antioxidant status. Owing to its antioxidant property, allicin is proposed for treating BD. In this study, we aimed to investigate the efficacy and safety of allicin on patients with BD with mucocutaneous involvement. Twenty patients with active BD were treated with allicin for 12 weeks and followed up to 16 weeks. A clinical manifestations index and scoring system was the primary technique for efficacy evaluation at baseline and Week 4, 12, 16. The secondary efficacy variables were OS-related biomarkers determined at first and final visit. Side effects were assessed at each visit. By the end of study, 18 patients completed the trail. Allicin was effective in decreasing ulcer and cutaneous parameters (p < .05). Especially, the greatest reduction of mucocutaneous scores emerged from baseline after the first four-week treatment (p < .05). Meanwhile, allicin remarkably ameliorated OS-related parameters. Besides, some side effects were observed on allicin, these adverse reactions, however, disappeared upon cessation of drugs. In conclusion, allicin is a safe and effective treatment for BD, which may be associated with its inhibiting OS and regulating oxidant/antioxidant status balance.
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  • 文章类型: Journal Article
    BACKGROUND: The current article aims to explore the protective potentials of α-tocopherol alone and the combination of allicin and vitamin B-complex against lead-acetate neurotoxicity on the cerebellar cortex.
    METHODS: Forty rats were divided into four groups (n = 10). Group 1 was the control group; Group 2 received 10 mg/kg body weight (BW) of lead acetate; Group 3 was exposed to 10 mg/kg BW of lead acetate plus a combination of allicin (100 mg/kg BW) and vitamin B-complex (40 mg/kg BW); Group 4 was administered lead acetate (10 mg/kg BW) and α-tocopherol (100 mg/kg BW). The animals received the treatment for 60 days by oral gavage. All the groups were studied ultrastructurally and immunohistochemically with glial fibrillary acidic protein (GFAP).
    RESULTS: The affected groups revealed shrunken and degenerated Purkinje cells with irregular nuclei. The cytoplasm comprised several lysosomes, unhealthy mitochondria, and dilated Golgi saccules. The myelinated nerve fibres demonstrated breaking of the myelin sheaths, apparent vacuoles, and broad axonal spaces. Immunohistochemically, there was a tremendous surge in GFAP-positive astrocytes in the lead acetate-treated group. These histological and ultrastructural variations were ameliorated by the administration of a-tocopherol and the combination of allicin and vitamin B complex. Moreover, an apparent decrease in the number of GFAP-positive astrocytes was obvious in the protected groups.
    CONCLUSIONS: Although both a-tocopherol and the combination of allicin and vitamin B-complex can be used as possible adjuvant therapies to ameliorate nervous system ailments attributable to lead acetate, α-tocopherol showed more protective potential.
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  • 文章类型: Journal Article
    The objective of this study was to investigate the efficacy and safety of allicin in the treatment of stage II oral submucous fibrosis (OSF) in a Chinese patient cohort. A randomized clinical trial was performed. Triamcinolone acetonide (TA) or allicin was injected intralesionally weekly for 16 weeks. Improvements in mouth opening, burning sensation, and oral health-related quality of life were evaluated. Forty-eight subjects completed the study without obvious adverse reactions. At 40 weeks, the net gain in mouth opening was 2.27 ± 0.84 mm in the TA group and 5.16 ± 1.04 mm in the allicin group. Burning sensation improved by 2.79 ± 0.87 in the TA group and by 4.33 ± 1.04 in the allicin group. The OHIP-14 score improved by 4.67 ± 2.94 in the TA group and by 12.58 ± 9.82 in the allicin group. Allicin intralesional injections improved mouth opening, burning sensation, and oral health-related quality of life in these stage II OSF patients. Allicin appears to be a potential adjunctive therapeutic drug.
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  • 文章类型: Journal Article
    BACKGROUND: Allicin is the main active constituent of Allium sativum L., which is characterized by broad antibacterial spectrum (MarkosN et al., 2008; Chen et al., 2008); it also has apparent inhibitory effects on a variety of tumors. The Objective of the paper is to study the inhibitory effect of allicin on human gastric cancer cell line SGC-7901.
    METHODS: MTT assay and flow cytometry technique were applied to determine the inhibition rate of allicin on human gastric cancer cell line SGC-7901. The results shows that different concentrations of allicin apparently inhibited the gastric cancer SGC7901 cells, cell growth inhibition rates in the experimental groups showed an upward trend with increased allicin concentration, which were concentration-dependent.
    RESULTS: Flow cytometry results found that the cell cycle was arrested in the G2/M phase. Allicin has an apparent inhibitory effect on proliferation of gastric cancer cells, and can induce their apoptosis.
    CONCLUSIONS: Compared with other chemotherapeutic drugs, allicin\'s anti-tumor effect is better; and toxic and side effects are relatively small.
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