Flavonoids and stilbenoids as a promising arsenal for the management of chronic arsenic toxicity

Rapid industrial and technological development has impacted ecosystem homeostasis strongly. Arsenic is one of the most detrimental environmental toxins and its management with chelating agents remains a matter of concern due to associated adverse effects. Thus, safer and more effective alternative therapy is required to manage arsenic toxicity. Based on existing evidence, native and indigenous plant-based active biomolecules appear as a promising strategy to mitigate arsenic-induced toxicity with an acceptable safety profile. In this regard, various phytochemicals (flavonoids and stilbenoids) are considered important classes of polyphenolic compounds with antioxidant and chelation effects, which may facilitate the removal of arsenic from the body more effectively and safely with regard to conventional approaches. This review presents an overview of conventional chelating agents and the potential role of flavonoids and stilbenoids in ameliorating arsenic toxicity. This report may provide a roadmap for identifying novel prophylactic/therapeutic strategies for managing arsenic toxicity.     

龙爪槐花中芦丁的薄层及紫外光谱鉴别

目的：对龙爪槐花中的芦丁进行定性鉴别。方法：采集不同花期龙爪槐的花，提取后用薄层层析法及紫外分光光度法进行芦丁的定性鉴别。结果：龙爪槐花中含有有效成分芦丁。结论：龙爪槐花可作为开发芦丁新的药源植物。     

尿石通颗粒质量标准的研究

目的 :建立尿石通颗粒的质量控制方法。方法 :用薄层色谱法对尿石通颗粒中的连钱草进行定性鉴别 ;以芦丁为对照品 ,采用分光光度法法测定颗粒中总黄酮 (以芦丁计 )含量。结果 :薄层色谱中斑点清晰 ,易于识别 ;分光光度法重复性好 ,总黄酮在 8.7～ 6 9.6 μg·ml-1浓度范围内呈线性关系 ,r =0 .9999,平均加样回收率 97.5 % (n =5 ) ,RSD =2 .8%。结论 :本法可有效地控制尿石通颗粒的质量。     

芦丁稀土配合物的合成及药效学初步研究

目的　探索芦丁与稀土元素配位前后药效学的变化。方法　采用小鼠扭体法和耳壳肿胀法对芦丁与稀土元素配位前后镇痛与抗炎作用进行比较。结果　与NS组比较,芦丁及其配合物可明显减少醋酸所致小鼠扭体次数( P <0 0 5或P <0 0 1);与芦丁组比较,其各配合物组的镇痛作用更强(P <0 0 1)。同样,与NS组比较,芦丁及其配合物对二甲苯引起的小鼠耳壳肿胀有明显的抗炎作用(P <0 0 5或P <0 0 1);而各配合物的抗炎作用又强于芦丁组(P <0 0 5或P <0 0 1)。结论　芦丁稀土配合物较芦丁的镇痛、抗炎作用明显增强。     

槲皮素与芦丁对离体大鼠主动脉环的舒张作用及机制

目的:比较研究槲皮素与芦丁对离体大鼠胸主动脉环的作用及其可能的途径。方法:采用累积加药法,检测槲皮素和芦丁对去氧肾上腺素(pheny lephrine,PE)预收缩的胸主动脉环张力的影响。结果:槲皮素对离体大鼠内皮完整和去内皮的胸主动脉环均有浓度依赖性的舒张作用,而芦丁对PE预收缩血管的舒张作用是内皮依赖性的。槲皮素和芦丁对内皮完整的胸主动脉环的最大舒张反应分别为(77.20±6.11)%和(44.28±7.48)%,但两者对内皮完整的胸主动脉环最大舒张的半数有效浓度无明显差异。用一氧化氮合酶抑制剂L-NAM E(0.1 mm o l/L)预处理后,可阻断芦丁诱导的舒张血管作用,但不能阻断槲皮素引起的舒张血管作用;用鸟苷酸环化酶抑制剂亚甲蓝(10μm o l/L)预处理后,两者的血管舒张作用均被阻断。用环氧合酶抑制剂吲哚美辛(10μm o l/L)预处理后可减弱槲皮素诱导的舒张血管作用,但不能阻断芦丁引起的舒张血管作用。结论:槲皮素的舒血管作用强于芦丁,槲皮素可能是通过鸟苷酸环化酶和环氧合酶途径产生非内皮依赖性的血管舒张作用,而芦丁可能是通过NO-鸟苷酸环化酶途径产生内皮依赖性的血管舒张作用。     

荞麦中芦丁对免疫性肝损伤小鼠肝脏超微结构的影响

目的观察荞麦中芦丁(RBFL)对卡介苗(BCG)和脂多糖(LPS)联合诱导的免疫性肝损伤小鼠肝脏的超微结构的影响。方法于尾静脉注射BCG和LPS,建立小鼠免疫性肝损伤模型。取♂昆明小鼠90只,随机均分为正常组、模型组、RBFL低、中、高剂量组及联苯双酯组。除正常组和模型组ig蒸馏水外,其余各组均ig给予对应药物干预,即40、80、160 mg·kg-1·d-1RBFL及联苯双酯200 mg·kg-1·d-1,gd,连续12 d。剖取肝脏、脾脏、胸腺,计算脏器指数,电镜下观察各组小鼠的肝脏超微结构变化。结果模型组小鼠的肝脏体积增大,肝脏指数较正常组的显著增大(P<0.01),各免疫器官脏器的指数增大,RBFL各剂量有抑制作用。结论 RBFL对BCG和LPS联合诱导的小鼠肝脏超微结构损伤具有保护作用。     

HPLC波长切换法同时测定杜仲双降袋泡剂中7种成分的含量

目的建立高效液相(HPLC)波长切换法同时测定杜仲双降袋泡剂中桃叶珊瑚苷、京尼平苷酸、绿原酸、京尼平苷、松脂醇二葡萄糖苷、芦丁及槲皮素7种成分含量的方法。方法以80%甲醇为溶剂,加热回流提取;色谱柱:Hydrosphere C18(4.6 mm×200 mm,5μm);柱温:30℃;流动相:乙腈-0.1%磷酸溶液,梯度洗脱;检测波长:208 nm(桃叶珊瑚苷)、235 nm(京尼平苷酸、绿原酸、京尼平苷、松脂醇二葡萄糖苷)、270 nm(芦丁、槲皮素);流速:0.9 ml/min。结果桃叶珊瑚苷、京尼平苷酸、绿原酸、京尼平苷、松脂醇二葡萄糖苷、芦丁、槲皮素的质量浓度分别在10.97~274.25μg/ml(r=0.999 7)、9.78~244.50μg/ml(r=0.999 8)、6.86~171.50μg/ml(r=0.999 6)、2.47~61.75μg/ml(r=0.999 7)、8.11~202.75μg/ml(r=0.999 1)、4.59~114.75μg/ml(r=0.999 9)、1.85~46.25μg/ml(r=0.999 5)范围内线性关系良好;平均加样回收率分别为99.85%、98.92%、97.52%、97.08%、98.51%、97.10%、96.91%,RSD分别为0.93%、0.74%、1.26%、1.37%、0.88%、1.05%、1.33%。结论所建立的HPLC波长切换法可以同时测定杜仲双降袋泡剂中桃叶珊瑚苷、京尼平苷酸、绿原酸、京尼平苷、松脂醇二葡萄糖苷、芦丁和槲皮素的含量,方法简便准确、灵敏度高,可用于杜仲双降袋泡剂的质量控制。     

Protective effect of flavonoids against red blood cell hemolysis by free radicals

BACKGROUND:

Flavonoids are polyphenolic substances with antioxidant properties, and they are found in different vegetables and fruits. Epidemiological studies have shown that the consumption of flavonoids reduces the prevalence of cardiovascular diseases. The use of synthetic antioxidants, however, has been limited because of their toxicity. Therefore, medical researchers have intensified their quest to find natural antioxidants.

OBJECTIVES:

To investigate the effect of several pure flavonoids, such as kaempferol, quercetin, morin and rutin, on red blood cell hemolysis and evaluate their -SH capacity as an indicator of membrane protection.

METHODS:

The rate of hemolysis and cell membrane -SH capacity were determined by spectrophotometry. Red blood cell peroxidation was induced using 2,2′-azo-bis-(2-amidinopropane) dihydrochloride. The effect of each flavonoid on hemolysis was examined at three concentrations (0.5 μg/mL, 5 μg/mL and 10 μg/mL), however, only the greatest concentration (10 μg/mL) of each flavonoid was used to study the effect on -SH groups.

RESULTS:

In all cases, the antioxidant activity was dose-dependent. Rutin showed the highest inhibitory effect on hemolysis among flavonoids (42.5%). The protective effect of kaempferol, rutin and morin against -SH group oxidation measured 7.7%, 23.3% and 26.4%, respectively.

CONCLUSIONS:

Results showed that flavonoids and flavonoid-containing plants can be used as natural antioxidants for the treatment and prevention of disease conditions, the pathogenesis of which is mediated by lipid peroxidation.     

Cardioprotective effects of rutin in rats exposed to pirarubicin toxicity

We established both an acute and chronic cardiac toxicity rat model, which showed pretreatment with rutin attenuated pirarubicin-induced myocardial histopathological injury, electrocardiogram abnormalities, and cardiac dysfunction. Rutin also significantly reduced serum levels of MDA, BNP, CK-MB, CTnT, and LDH and increased serum SOD levels. Treatment with rutin and dexrazoxane resulted in an increase in Bcl-2/Bax ratio (p < 0.05) and reduction in JNK and Caspase-3 protein levels, compared to the pirarubicin group (all p < 0.05). Furthermore, rutin at a dose of 50 mg/kg significantly attenuated the above-mentioned alterations. Our study suggests the antioxidant and anti-apoptotic properties of rutin may be responsible for the cardioprotective effects observed.     

HPLC法同时测定铁包金不同药用部位中芦丁和槲皮素的含量

目的:建立同时测定铁包金不同药用部位芦丁、槲皮素含量的方法。方法:采用高效液相色谱法。色谱柱为迪马ODS C18(250 mm×4.6 mm,5μm),流动相为乙腈-甲醇-0.2%磷酸(梯度洗脱),流速为0.9 ml/min,柱温为30℃,检测波长为360 nm。结果:芦丁和槲皮素的进样量分别在0.01¹.88、0.011.88、0.01⁰.23μg范围内与各自峰面积积分值呈良好线性关系;精密度、稳定性、重复性的RSD<2%;芦丁、槲皮素的平均加样回收率分别为99.48%、102.34%,RSD分别为2.06%、2.37%(n=6)。结论:铁包金叶与藤茎部位中芦丁、槲皮素的含量均较高。该方法简单、稳定,结果准确、可靠,可用于铁包金的质量控制。