芒果甙抗肿瘤作用机制研究进展

芒果甙是一种黄酮类化合物,具有多种生理和药理作用,近期的研究报道芒果甙具有抗肿瘤作用。芒果甙抗肿瘤作用主要包括抑制肿瘤细胞增殖生长、阻断细胞周期、诱导细胞凋亡、抑制NF-κB信号途径激活、影响E-cad介导的细胞黏附及信号转导、干预线粒体通透性转换及与化疗药物发挥联合作用等。     

芒果叶提取物芒果苷安全性评价Ⅰ:安全药理学试验

目的:观察芒果苷对神经系统、心血管系统和呼吸系统的影响,明确其一般药理活性,为后续毒理试验提供参考。方法:对小鼠一次按0.24,1.0,3.0 g/kg体重灌胃给予芒果苷后,观察其一般行为表现、姿势、步态、有无流涎、流汗、暴燥、抽搐、肌颤等变化,测定其自主活动次数、协调运动情况和阈下睡眠剂量戊巴比妥钠对小鼠睡眠的影响;对Beagle犬一次按0.1,0.7,4.0 g/kg体重十二指肠给予芒果苷后,观测给药后180 min内心电图、血压、呼吸的改变。结果:小鼠一般行为表现、姿势、步态未见有明显改变,也未见有流涎、流汗、暴燥、抽搐、肌颤等现象;自主活动、协调运动情况和戊巴比妥钠阈下睡眠剂量小鼠入睡率均无明显影响。犬心电图、血压、呼吸均无明显变化。结论:在本实验条件下,芒果苷对小鼠精神和神经系统,对犬心血管系统和呼吸系统均无明显影响。     

石韦有效成分的高效液相色谱测定

石韦为较常用中药,中医认为有清肺泄热、利水通淋等功效。主要来源于水龙骨科(Polypodiaceae)石韦属(Pyrrosia)植物:有柄石韦(P.petiolosa)、庐山石韦(P.sheareri)和石韦(P.lingua)的地上部分;同属多种植物也在全国不同地区应用。     

川西獐牙菜对低张性低氧肝损伤的保护作用

高原药用植物——川西獐牙菜(Swertia mussotii Franch)注射剂及其有效成份芒果甙和总(口山)酮对模拟高原急性低氧肝损伤具有保护作用。大鼠于低压舱内模拟海拔8,000m 2小时造成急性低氧肝损伤。预先给大鼠腹腔注射川西獐牙菜注射剂6.5ml/kg,可以明显降低大鼠SGOT和肝溶酶体酸性磷酸酶的活力,同时降低肝总脂的含量。大鼠肝溶酶体体外温孵实验显示,川西獐牙菜注射剂,芒果甙和总(口山)酮有稳定溶酶体膜的作用,并直接对溶酶体酸性磷酸酶活力有抑制作用。     

Gallic acid indanone and mangiferin xanthone are strong determinants of immunosuppressive anti-tumour effects of Mangifera indica L. bark in MDA-MB231 breast cancer cells

Vimang is a standardized extract derived from Mango bark (Mangifera Indica L.), commonly used as anti-inflammatory phytomedicine, which has recently been used to complement cancer therapies in cancer patients. We have further investigated potential anti-tumour effects of glucosylxanthone mangiferin and indanone gallic acid, which are both present in Vimang extract. We observed significant anti-tumour effects of both Vimang constituents in the highly aggressive and metastatic breast cancer cell type MDA-MB231. At the molecular level, mangiferin and gallic acid both inhibit classical NFκB activation by IKKα/β kinases, which results in impaired IκB degradation, NFκB translocation and NFκB/DNA binding. In contrast to the xanthone mangiferin, gallic acid further inhibits additional NFκB pathways involved in cancer cell survival and therapy resistance, such as MEK1, JNK1/2, MSK1, and p90RSK. This results in combinatorial inhibition of NFκB activity by gallic acid, which results in potent inhibition of NFκB target genes involved in inflammation, metastasis, anti-apoptosis and angiogenesis, such as IL-6, IL-8, COX2, CXCR4, XIAP, bcl2, VEGF. The cumulative NFκB inhibition by gallic acid, but not mangiferin, is also reflected at the level of cell survival, which reveals significant tumour cytotoxic effects in MDA-MB231 cells. Altogether, we identify gallic acid, besides mangiferin, as an essential anti-cancer component in Vimang extract, which demonstrates multifocal inhibition of NFκB activity in the cancer-inflammation network.     

芒果苷对L6细胞葡萄糖消耗的影响及其作用机制研究

目的观察芒果苷对L6细胞葡萄糖消耗的影响,并探讨其分子机制。方法以芒果苷干预L6肌管细胞,葡萄糖氧化酶法检测葡萄糖消耗量,western-blot方法检测葡萄糖转运蛋白4(GLUT4)的表达量及其急性转位作用,免疫共沉淀(IP)联合western-blot方法检测AKT激酶活性。结果芒果苷处理可激活L6细胞的AKT激酶(与对照组比,P=0.001),提高L6细胞的葡萄糖消耗(P=0.011或P=0.000)且呈剂量-反应关系(P=0.000),上调GLUT4的蛋白表达量(P=0.001或P=0.000)并促进GLUT4在细胞内发生急性转位(P=0.005,P=0.001或P=0.026),使该蛋白由胞浆经细胞骨架转位至细胞膜。结论芒果苷可促进L6细胞的葡萄糖消耗量,调节GLUT4的表达及其在细胞内的急性转位,激活AKT激酶活性,因此,芒果苷具有潜在的辅助降血糖作用。     

Mangiferin protects against 1-methyl-4-phenylpyridinium toxicity mediated by oxidative stress in N2A cells

1-Methyl-4-phenyl-pyridine ion (MPP⁺), the active metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induces a Parkinsonian syndrome in humans and animals, a neurotoxic effect postulated to derive from oxidative stress. We report here the first investigation of MPP⁺-induced oxidative stress in the murine neuroblastoma cell line N2A. Significant cell death was observed following exposure to 0.25 mM MPP⁺. Markers of oxidative stress included decreased intracellular levels of GSH after 48 h of exposure (85% depletion) as well as an increase in GSSG. Expression of both superoxide dismutase 1 (sod1) and catalase (cat) mRNA was increased, as well the activity of catalase. These cellular effects were, at least partially, reversed by treatment with the natural polyphenol mangiferin. Administration of mangiferin protected N2A cells against MPP⁺-induced cytotoxicity, restored the GSH content (to 60% of control levels), and down-regulated both sod1 and cat mRNA expression. Together, these results suggest that the protective effect of mangiferin in N2A cells is mediated by the quenching of reactive oxygen intermediates. Therefore, mangiferin could be a useful compound in therapies for degenerative diseases, including Parkinson's disease, in which oxidative stress plays a crucial role.     

RP-HPLC法测定光石韦中芒果苷的含量

目的建立光石韦中芒果苷的含量测定方法。方法采用RP-HPLC法,色谱柱为Agilent TC-C18柱（4.6 mm×250.0 mm,5μm）,流动相为乙腈-0.1%磷酸溶液（13∶87）,流速为1.0 mL/min,检测波长为318 nm。结果芒果苷在0～2.136μg范围内呈良好的线性关系,平均回收率为104.24%,RSD=0.86%（n=6）。结论本方法灵敏、准确,可作为光石韦的质量控制标准。