苦参总黄酮HPLC指纹图谱研究

目的:建立苦参提取物黄酮类成分的HPLC指纹图谱,为苦参的质量控制提供依据。方法:采用高效液相色谱法,色谱柱为DIKMA C18柱(250mm×4.6mm,粒度5μm);流动相为甲醇-水(梯度洗脱);流速1ml·min-1;柱温30℃;检测波长280nm;进样量20μl。利用中药色谱指纹图谱相似度评价系统(2004A版)对不同批次苦参总黄酮的HPLC图谱进行比较分析。结果:建立了苦参提取物黄酮类成分的HPLC指纹图谱,以苦参酮为参照峰,对10批苦参总黄酮成分进行指纹图谱分析,标定了13个共有峰,10批提取物的相似度均>0.9。结论:本研究所建立的分析方法具有良好的精密度和重现性,可为苦参提取物的品质评价和质量控制提供科学依据。     

复方苦参注射液对慢性乙肝患者免疫功能的影响及抗病毒疗效

目的：探讨复方苦参注射液对慢性乙型肝炎（CHB）患者免疫功能的影响及抗病毒疗效。方法：将72例CHB患者随机分为两组。治疗组36例,用复方苦参注射液20mL静脉滴注;对照组36例,以还原型谷胱甘肽1.2g静脉滴注,疗程6周,治疗前后检测CHB患者血清淋巴细胞因子IFN-γ、IL-2,T细胞亚群及乙肝病毒学指标。结果：复方苦参注射液治疗后可显著升高治疗组血清中IFN-γ、IL-2的水平,与治疗前及对照组对比差异均有显著性（P〈0.05）;治疗组CD3^＋、CD4^＋细胞水平明显上升,CD8^＋细胞水平明显下降,与治疗前及对照组对比差异均有显著性（P〈0.05或P〈0.01）;HBV复制指标HBeAg、HBV-DNA的转阴率治疗组明显高于对照组,有显著性差异（P〈0.01）。结论：复方苦参注射液能提高CHB患者机体细胞免疫功能,抑制乙型肝炎病毒复制,是治疗CHB取得良好前景的药物。     

女贞子中8个化合物对胰岛素抵抗HepG2细胞葡萄糖消耗的影响

目的探讨女贞子中乙酰齐墩果酸、齐墩果酸、19α-羟基-3-乙酰乌索酸、槲皮素、GI3、女贞苷、对羟基苯乙醇-O-β-D-葡萄糖苷、芹菜素-6＇＇-O-乙酰-7-O-β-D-葡萄糖苷对胰岛素抵抗HepG2细胞葡萄糖消耗的影响。方法采用高浓度胰岛素诱导培养HepG2细胞,建立胰岛素抵抗细胞模型,培养液中加入各化合物共同孵育,采用葡萄糖试剂盒检测培养液中的葡萄糖含量。探讨其对胰岛素抵抗HepG2细胞葡萄糖消耗的影响。结果齐墩果酸、19α-羟基-3-乙酰乌索酸、GI3、对羟基苯乙醇-O-β-D-葡萄糖苷、芹菜素-6＇＇-O-乙酰-7-O-β-D-葡萄糖苷在不合胰岛素条件下可使胰岛素抵抗HepG2细胞的葡萄糖消耗量增加11．62％、17．21％、10．54％、12．08％、11.85％,加入生理浓度胰岛素后,上述化合物可使细胞葡萄糖消耗量增加12．95％、13.83％、10．84％、14．26％、17．41％。槲皮素、女贞苷在不含胰岛素条件下不增加细胞的葡萄糖消耗量,加入生理浓度胰岛素后,可使细胞萄萄糖消耗量增加15．70％、17．04％,其中槲皮素促进细胞增殖。结论齐墩果酸、芹菜素-6＇＇-O-乙酰-7-O-β-D-葡萄糖苷等增加胰岛素抵抗HepG2细胞的葡萄糖消耗量呈非胰岛素依赖性,其中芹菜素-6＇＇-O-乙酰-7-O-β-D-葡萄糖苷与生理浓度胰岛素有协同增强作用;女贞苷、槲皮素增加细胞葡萄糖消耗量呈胰岛素依赖性,槲皮素能显著促进细胞增殖。     

多叶越南槐生物碱类成分的研究

目的：研究多叶越南槐的生物碱类成分。方法：采用Sephadex LH-20柱色谱、硅胶柱色谱、重结晶等方法分离和纯化多叶越南槐的生物碱成分,综合运用红外光谱、质谱、核磁共振等技术和理化方法进行分析,并确定分离得到的生物碱结构。结果：根据理化性质及波谱数据,鉴定了各化合物的结构分别是：槐果碱（1）,苦参碱（2）,槐花醇（3）,9α-羟基苦参碱（4）,12α-羟基槐果碱（5）,氧化槐果碱（6）,氧化苦参碱（7）,金雀花碱（8）。结论：化合物1~8均为首次从多叶越南槐中分离得到。     

HPLC法同时测定人血浆中苦参4种生物碱的含量

目的:建立同时测定人血浆中苦参4种生物碱含量的方法。方法:采用高效液相色谱(HPLC)法。色谱柱为Agilent ZORBAX NH2(150 mm×4.6 mm,5μm),流动相为乙腈-无水乙醇-3%磷酸溶液(81∶10∶9,V/V/V),流速为1 ml/min,检测波长为210 nm,柱温为室温。结果:槐定碱、槐果碱、苦参碱、氧化苦参碱的进样量分别在0.034 72⁰.258 60、0.012 840.258 60、0.012 84⁰.113 65、0.023 770.113 65、0.023 77⁰.240 93、0.452 480.240 93、0.452 48⁴.520 63μg范围内与待测物峰面积积分值呈良好线性关系(r≥0.999 3);槐定碱、槐果碱、苦参碱、氧化苦参碱精密度试验的RSD均小于2.0%;短期、长期、循环稳定性的RSD均小于3.20%;重复性试验的RSD均小于3.0%;提取回收率分别为1.14%4.520 63μg范围内与待测物峰面积积分值呈良好线性关系(r≥0.999 3);槐定碱、槐果碱、苦参碱、氧化苦参碱精密度试验的RSD均小于2.0%;短期、长期、循环稳定性的RSD均小于3.20%;重复性试验的RSD均小于3.0%;提取回收率分别为1.14%².35%、1.45%2.35%、1.45%².32%、1.29%2.32%、1.29%².51%、1.62%2.51%、1.62%².47%。结论:该方法灵敏度高、精密度好,可用于苦参中4种生物碱的药动学研究。     

Antidiabetic and antioxidant effects of oleanolic acid from Ligustrum lucidum Ait in alloxan‐induced diabetic rats

The present study evaluated the antidiabetic and antioxidant effects of oleanolic acid (OA) from Ligustrum lucidum Ait (LLA) in alloxan‐induced diabetic rats. OA in the alloxan‐induced diabetic rats showed significant hypoglycemic activity by lowering blood glucose (at doses of 60 and 100 mg/kg for 40 days). The levels of serum total cholesterol (TC), triglycerides (TG) and low‐density lipoprotein cholesterol (LDL‐c) in the OA‐treated diabetic rats were lower, and the high‐density lipoprotein cholesterol (HDL‐c) level was higher than in the control diabetic rats. A significant reduction in the serum aspartate aminotransferase (AST), alanine aminotransferase (ALT) and alkaline phosphatase (ALP) levels of diabetic rats following OA treatment was also observed. Furthermore, OA treatment decreased the malondialdehyde (MDA) level, but increased superoxide dismutase (SOD) and glutathione peroxidase (GSH‐px) activities of the liver and kidney in diabetic rats. These results indicate that OA could protect the liver function avoiding alloxan‐induced damage; OA had hypoglycemic, hypolipidemic and antioxidant efficacy in the diabetic rats. The antioxidant ability of OA might be one of the mechanisms of its hypoglycemic and hypolipidemic effects. Copyright © 2009 John Wiley & Sons, Ltd.     

槐果皮中的异黄酮甙类成分

目的：对槐果皮进行化学成分研究。方法：采用波谱和化学方法对66个异黄酮甙类成分进行了鉴定。结果：从槐（Sophora japonica)果皮中分离得到5个异黄酮甙类成分,它们的结构确定为染料木素7,4′-二葡萄糖甙（genistein7,4′-di-O-β-D-glucoside,I),槐属双甙（sophorabioside,Ⅱ）,樱黄素4′-O-β-D-葡萄糖甙（prunetin4′-O-β-D-glucoside,Ⅲ）。槐属甙（sophororicoside,Ⅳ）,染料木甙（genistin,Ⅴ）。结论：化合物I、Ⅲ和Ⅴ为首次从该植物中分离得到。     

槐树种子的化学成分研究

槐角为豆科植物槐 Sophora japonica L.的果实 ,全国各地均产。其性寒、味苦 ,归肝、大肠经 ,有凉血止血、清肝明目之功效 ,是一种常用中药。槐角的研究早有报道 ,前人已从中分到数种黄酮类、生物碱类、三萜类、氨基酸和糖类等成分 ,其中异黄酮和黄酮醇及其苷类成分含量较高[1] 。近年来 ,槐角在药理研究和临床应用方面 ,均发现有明显的降谷丙转氨酶作用、抗生育作用和抗肿瘤作用。为进一步阐明其活性成分 ,我们对槐角果皮和种子的化学成分分别进行系统的研究。本文报道种子的化学成分研究。从中分得了 8个化合物 ,分别鉴定为 :染料木素 (1…     

Synergistic anticancer effect of flavonoids from Sophora alopecuroides with Sorafenib against hepatocellular carcinoma

Sorafenib (SF), a multi-kinase inhibitor, is the first FDA-approved systemic chemotherapy drug for advanced hepatocellular carcinoma (HCC). However, its clinical application is limited by severe toxicity and side effects associated with high applied doses. Sophora alopecuroides L. is traditionally used as Chinese herbal medicine for treating gastrointestinal diseases, bacillary dysentery, viral hepatitis, and other diseases, and exerts an important role in anti-tumor. Hence, we investigated the synergistic actions of seventeen flavonoids from this herb combined with SF against HCC cell lines and their primary mechanism. In the experiment, most compounds were found to prominently enhance the inhibitory effects of SF on HCC cells than their alone treatment. Among them, three compounds leachianone A ( 1 ), sophoraflavanone G ( 3 ), and trifolirhizin ( 17 ) exhibited significantly synergistic anticancer activities against MHCC97H cells at low concentration with IC₅₀ of SF reduced by 5.8-fold, 3.6-fold, and 3.5-fold corresponding their CI values of 0.49, 0.66, and 0.46 respectively. Importantly, compounds 3 or 17 combined with SF could synergistically induce MHCC97H cells apoptosis via the endogenously mitochondrial-mediated apoptotic pathway, involving higher Bax/Bcl-2 expressions with the activation of caspase-9 and -3, and arrest the cell cycle in G1 phases. Strikingly, this synergistic effect was also closely related to the co-suppression of ERK and AKT signaling pathways. Furthermore, compound 3 significantly enhanced the suppression of SF on tumor growth in the HepG2 xenograft model, with a 79.3% inhibition ratio at high concentration, without systemic toxicity, compared to either agent alone. These results demonstrate that the combination treatment of flavonoid 3 and SF at low doses exert synergistic anticancer effects on HCC cells in vitro and in vivo.