大鼠血清中黄芩素代谢产物的鉴定(英文)

黄芩素是黄芩苷的苷元,是黄芩的主要活性黄酮类成分之一。大鼠灌胃给予黄芩素(200mg/kg)之后,利用HPLC-DAD和LC-MS/MS法从大鼠血清中检测并鉴定出5个代谢产物(M1-M5)以及原型药(M0)。在此结果上,推测了黄芩素在大鼠血清中可能的代谢途径。     

黄连解毒汤通过抑制血红素加氧酶-1发挥逆转慢性粒细胞白血病加速期的作用

目的:探讨黄连解毒汤(HLJDT)对慢性粒细胞白血病(CML)加速期的治疗作用,以及HLJDT及其主要活性成份之一的黄芩素对血红素加氧酶-1(HO-1)表达的影响。方法:通过对1例CML的患者口服HLJDT治疗6个月的观察,外周血检查和骨髓穿刺分析治疗前后外周血象和骨髓象的变化;流式细胞术分析HLJDT和黄芩素对CML细胞系K562的活细胞计数的影响;逆转录多聚酶链反应(RT-PCR)检测患者骨髓单个核细胞HO-1基因的表达;蛋白印记检测经黄芩素处理后K562细胞HO-1蛋白的表达水平。结果:口服HLJDT对CML加速期的治疗有效,可明显降低骨髓和外周血原始粒细胞和早幼粒细胞数,使疾病重新回复到慢性期;并且在体内能降低肿瘤细胞HO-1基因的表达,在体外,HLJDT能抑制K562细胞的增殖,且其主要成份黄芩素亦有相同作用,并且下调HO-1蛋白的表达。结论:HLJDT具有治疗CML加速期的作用,其机理与抑制HO-1基因和蛋白的表达有关;因此,HLJDT具有潜在的临床应用价值。     

黄芩素胶囊的小鼠急性毒性实验

目的观察黄芩素胶囊灌胃一日后产生的急性毒性反应和死亡情况。方法将黄芩素胶囊的内容物黄芩素粉以最大浓度给ICR小鼠灌胃给药,小鼠未出现死亡,未测出LD50,故测其最大给药量。结果黄芩素粉最大给药量为15g/Kg。结论黄芩素胶囊具有较好的安全性。     

黄芩甙元及其苄基衍生物的制备与抗人免疫缺陷病毒实验研究

黄芩甙元及其苄基衍生物的制备与抗人免疫缺陷病毒实验研究赵晶张致平陈鸿珊陈湘红张兴权（中国医学科学院、协和医科大学医药生物技术研究所，北京１０００５０）黄芩（ＳｃｕｔｅｌａｒｉａｂａｉｃａｌｅｎｓｉｓＧｅｏｒｇｉ）有广泛的生物活性。黄芩提取物及其...     

黄芩素和大豆黄酮对人白血病细胞系HL60体外增殖的抑制作用

目的　观察黄芩素和大豆黄酮对HL 60细胞体外增殖的抑制作用。方法　分别采用台盼蓝拒染法和MTT比色法 ,在不同条件下测定细胞增殖的抑制率。结果　MTT比色法并不适用于检测黄芩素和大豆黄酮对HL 60细胞体外增殖的影响。应用台盼蓝拒染法 ,发现黄芩素和大豆黄酮能够显著地抑制HL 60细胞的体外增殖并且呈现时效及量效关系。结论　黄芩素和大豆黄酮是两种能够明显抑制HL 60细胞体外增殖 ,具有潜在抗白血病作用的黄酮类化合物。     

三黄颗粒与素代三黄颗粒对小鼠急性炎症模型的效果比较

目的：：比较三黄颗粒与素代三黄颗粒对小鼠急性炎症模型的作用。方法：建立醋酸致小鼠毛细血管通透性增高和二甲苯诱导小鼠耳廓肿胀模型,比较三黄颗粒与素代三黄颗粒的抗炎作用。结果：三黄颗粒和素代三黄颗粒均能抑制醋酸致小鼠毛细血管通透性增高和二甲苯致小鼠耳廓肿胀,且素代三黄颗粒的效果优于三黄颗粒。结论：素代三黄颗粒对不同急性炎症模型的作用优于三黄颗粒。     

Therapeutic approaches against common structural features of toxic oligomers shared by multiple amyloidogenic proteins

Impaired proteostasis is one of the main features of all amyloid diseases, which are associated with the formation of insoluble aggregates from amyloidogenic proteins. The aggregation process can be caused by overproduction or poor clearance of these proteins. However, numerous reports suggest that amyloid oligomers are the most toxic species, rather than insoluble fibrillar material, in Alzheimer's, Parkinson's, and Prion diseases, among others. Although the exact protein that aggregates varies between amyloid disorders, they all share common structural features that can be used as therapeutic targets. In this review, we focus on therapeutic approaches against shared features of toxic oligomeric structures and future directions.     

Hepatoprotective effects of baicalein against CCl4-induced acute liver injury in mice

AIM: To investigate the hepatoprotective effect of baicalein against carbon tetrachloride (CCl₄)-induced liver damage in mice.METHODS: Mice were orally administered with baicalein after CCl₄ injection, and therapeutic baicalein was given twice a day for 4 d. The anti-inflammation effects of baicalein were assessed directly by hepatic histology and serum alanine aminotranferease and aspartate aminotransferase measurement. Proliferating cell nuclear antigen was used to evaluate the effect of baicalein in promoting hepatocyte proliferation. Serum interleukin (IL)-6, IL-1β and tumor necrosis factor-α (TNF-α) levels were measured by enzyme-linked immunosorbent assay and liver IL-6, TNF-α, transforming growth factor-α (TGF-α), hepatocyte growth factor (HGF) and epidermal growth factor (EGF) genes expression were determined by quantitative real-time polymerase chain reaction.RESULTS: CCl₄-induced acute liver failure model offers a survival benefit in baicalein-treated mice. The data indicated that the mRNA levels of IL-6 and TNF-α significantly increased within 12 h after CCl₄ treatment in baicalein administration groups, but at 24, 48 and 72 h, the expression of IL-6 and TNF-α was kept at lower levels compared with the control. The expression of TGF-α, HGF and EGF was enhanced dramatically in baicalein administration group at 12, 24, 48 and 72 h. Furthermore, we found that baicalein significantly elevated the serum level of TNF-α and IL-6 at the early phase, which indicated that baicalein could facilitate the initiating events in liver regeneration.CONCLUSION: Baicalein may be a therapeutic candidate for acute liver injury. Baicalein accelerates liver regeneration by regulating TNF-α and IL-6 mediated pathways.     

湖州市第一人民医院药剂科 浙江湖州 313000

摘 要 目的：建立HPLC法同时测定复方羚角降压片中8种活性成分的含量。 方法: 采用HPLC波长切换法,色谱柱为Agilent ZORBAX Eclipse XDB C18(250 mm×4.6 mm,5 μm),流动相为甲醇(A) 0.06%磷酸溶液(B),梯度洗脱,流速为1.0 ml·min-1,检测波长为265 nm（紫丁香苷）、330 nm（咖啡酸、异迷迭香酸苷、迷迭香酸）、278 nm（黄芩苷、汉黄芩苷、黄芩素、汉黄芩素）,柱温为30℃,进样量为10 μl。 结果: 紫丁香苷、咖啡酸、异迷迭香酸苷、迷迭香酸、黄芩苷、汉黄芩苷、黄芩素、汉黄芩素分别在11.616～69.696 μg·ml-1,1.601～9.605 μg·ml-1,2.040～12.240 μg·ml-1,14.888～89.328 μg·ml-1,72.032～432.192 μg·ml-1,24.016～144.096 μg·ml-1,10.040～60.240 μg·ml-1,1.801～10.805 μg·ml-1(r为0.999 4～0.999 9）浓度范围内呈良好的线性关系;平均加样回收率分别为98.8%,99.7%,98.8%,98.0%,99.1%,99.3%,100.2%,97.4%,RSD分别为0.7%,0.7%,0.4%,0.6%,0.3%,0.5%,0.5%,0.7%（n=6）。 结论: 该方法简单、有效、准确,可用于复方羚角降压片中上述8种活性成分含量的同时测定。     

HPLC法同时测定栀子金花丸中黄芩苷、汉黄芩苷、黄芩素和汉黄芩素

目的 建立栀子金花丸中黄芩苷、汉黄芩苷、黄芩素和汉黄芩素的HPLC同时测定方法.方法 色谱柱:Dikma Diamonsil C18柱(250 mm×4.6 mm,5μm);流动相:乙腈-0.1％磷酸溶液,梯度洗脱;变波长测定.结果 黄芩苷、汉黄芩苷、黄芩素、汉黄芩素的线性范围分别为0.418～4.18 μg,02～2 μg,0.233～2.33 μg,0.215～2.15 μg,线性相关系数均达0.999以上.平均回收率分别为98.40％ (RSD=0.46％),98.66％ (RSD=1.43％),98.89％ (RSD=1.49％),98.98％(RSD=1.45％).结论 该方法快速、简便、准确、具有良好的重复性和回收率,可作为栀子金花丸中这4种成分的含量测定方法.