Matrine,oxymatrine, and compound Kushen injection from the roots of Sophora flavescens: an overview of their anticancer activities

In the present review, we updated current information on the chemistry, contents, and anticancer properties of matrine (MT), oxymatrine (OMT), and compound Kushen injection (CKI). The anticancer properties were focused on lung, breast, and liver cancer cells because they are most susceptible. Sources of information were from Google, Google Scholar, PubMed, PubMed Central, Science Direct, PubChem, J-Stage, Directory of Open Access Journals (DOAJ), and China National Knowledge Infrastructure (CNKI). Reference was also made on botanical websites, such as Flora of China and World Flora Online. MT and OMT are dominant quinolizidine alkaloids from the roots of Sophora flavescens (Kushen) of the family Fabaceae. Against lung, breast, and liver cancer cells, MT and OMT inhibit cell proliferation; induce cell cycle arrest, apoptosis, and autophagy; restrict angiogenesis; and inhibit cell metastasis, invasion, and migration. The processes involve various molecular targets and signaling pathways. CKI is a traditional Chinese medicine (TCM) composed of root extracts of S. flavescens and Smilax glabra (Baituling) of the family Smilacaceae. With MT and OMT as major components, CKI has been approved for the treatment of cancer in China more than 20 years ago. In recent years, systematic reviews and meta-analysis have been undertaken to evaluate the anticancer effects of CKI. When CKI is used alone and in combination with chemotherapy of western medicine, there is much to be learned concerning their interactions besides their individual and integrated efficacy. Some perspectives of MT, OMT, and CKI are discussed, and their suggestions for future research are provided.     

Application of median-effect in quantitative analysis of antitumor drugs in vitro

Objective: To analyze quantitatively the synergistic and antagonistic effects of combined oxymatrine (OMT) and 5-fluorouracil (5-GU) on a cell line of human liver cancer (HepG2) with median-effect principle in vitro. Methods: The median-effect principle and MTT method were used in the quantitative analysis of effects of the two drugs. Results: Cytotoxic activity of the individual drugs enhanced as drug concentration increased. As fa=0.41, a CI equal to 1 indicated additivity; fa<0.41, a CI less than 1 indicated synergy; and fa>0.41, a CI greater than 1 indicated antagonism. The sequence of administration did not influence the cytotoxic activity of the combined antitumor drugs. The ratio of drug concentration was a factor that can influence the killing effect. Conclusion: The combined drugs interaction (CI<1) was synergistic at lower concentration and antagonistic at higher concentration. The ratio of drug concentration is a factor that can influence the killing effect. Biography: HE Song(1965–), male, doctor of medicine, associate professor, Chongqing Medical University, majors in gastroenterology.     

氧化苦参碱对胆碱酯酶影响的临床研究

目的　研究氧化苦参碱 (OM)治疗病毒性肝炎过程中 ,胆碱酯酶 (ChE)的动态变化及与同期白蛋白 (ALB)、凝血酶原活动度 (PTA)及其他肝功能的关系。方法　 98例病毒性肝炎患者分成 4组 ;A组 31例 (静脉注射OM) ,B组 30例 (口服OM) ,C组 7例 (肌内注射OM) ,D组 30例 (一般护肝药物 ,不用OM)。定期检测血清ChE、ALB、PTA、肝功能、肾功能、血常规、血清补体 1型受体 (sCR1)、红细胞黏附功能 (EIIAF)指标。结果　A、B、C 3组在治疗中ChE明显下降 ,治疗前中后比较 ,差异有显著意义 (P值分别为 <0 0 0 1、<0 0 0 1、0 0 2 3) ;同时在ChE数值及异常率与对照组比较 ,差异有显著意义(P <0 0 0 1)。A、B、C 3组在治疗前中后 ,ALB、PTA随病情而变化 (P值均 >0 0 5 )。4组治疗后病情均有明显好转 ,ChE的下降并不伴随肝功能的恶化。结论　OM制剂在治疗病毒性肝炎中ChE明显下降 ,但反映肝脏实质功能的ALB、PTA等指标无改变 ,ALT、AST、TBiL好转。在OM治疗结束后 ,ChE迅速恢复正常。所以 ,ChE的下降并不表明病情的恶化 ,其机理尚待探讨。     

氧化苦参碱对LAK细胞活性的影响

ＬＡＫ细胞具有很强的广谱杀瘤作用，而氧化苦参碱具有较强的免疫抑制作用。本文研究了氧化苦参碱对ＬＡＫ细胞活力的影响，结果表明：氧化苦参碱可抑制ＩＬ－２对小鼠脾细胞的促增殖作用，并且对ＩＬ－２活化ＬＡＫ细胞杀伤Ｐ８１５的能力也有抑制作用。当ＩＬ－２（５００ｕ／ｍｌ）与２００μｇ／ｍｌ的氧化苦参碱共同孵育４ｄ后，可使ＬＡＫ细胞杀瘤能力（在效靶比为１００：１时）的８２．５％被抑制。同时氧化苦参碱本身对Ｐ８     

氧化苦参碱对小鼠免疫性肝纤维化作用机制的研究

目的 研究氧化苦参碱对小鼠免疫性肝纤维化的作用机制。方法 将BABL/c 小鼠随机分成正常对照组、阳性对照组、氧化苦参碱小剂量、大剂量治疗组,阳性对照组和氧化苦参碱治疗组每周静脉注射1次刀豆蛋白A,共20周。氧化苦参碱治疗组分别腹腔注射氧化苦参碱30mg/kg、60mg/kg。共20周。分别于注射刀豆蛋白A后5、12和20周取血低温保存;并每次处死一批小鼠取肝脏组织液氮低温保存、常规HE染色、Van Gieson胶原纤维染色,冰冻切片CD4,CD8T淋巴细胞染色。图像分析系统定量分析肝纤维组织含量。结果 氧化苦参碱治疗组血清ALT含量及肝组织内炎症活动度、纤维含量均低于阳性对照组,而且呈剂量依赖性。结论 氧化苦参碱有减轻小鼠肝脏炎症活动度及抗小鼠免疫性肝纤维化的作用。     

苦参素甘利欣注射液治疗乙型肝炎

目的：探讨苦参素注射液联合甘利欣注射液治疗乙型肝炎的疗效，寻找治疗乙型肝炎的有效方法。方法：将103例乙型肝炎患者分为治疗组55例和对照组48例，治疗组应用苦参素注射液及甘利欣注射液，对照组应用甘利欣注射液，观察ALT及HBV—M的变化。结果：治疗结束时，治疗组HBeAg阴转率及ALT复常串均较对照组高，两组HBeAg阴转率分别为32．7％、10．4％(P＜0.01)，ALT复常率分别为94．5％、75．0％(P＜0．01)。结论：苦参素注射液联合甘利欣注射液治疗乙型肝炎有较好的HBeAg阴转率及ALT复常率。     

氧化苦参碱联合拉米呋定治疗慢性乙型肝炎

目的 :观察氧化苦参碱联合拉米呋定治疗慢性乙型肝炎 (乙肝 )的临床疗效。方法 :将慢性乙肝患者 80例随机分成治疗组和对照组各 40例 ,治疗组给予氧化苦参碱注射液 40 0mg ,im ,qd ,拉米呋定 10 0mg ,po ,qd ;对照组单用拉米呋定 10 0mg ,po ,qd。两组疗程均 12～ 2 4周。观察治疗前后肝功能、乙肝病原学血清标志物、肝纤维化指标变化情况。结果 :两组肝功能均有较明显的改善 ;治疗组和对照组HBV DNA转阴率分别为 90 .0 % ,85 .0 % ;HBeAg转阴率分别为 47.5 % ,2 7.5 % ;肝纤维化指标血清透明质酸 (HA)、Ⅲ型前胶原肽 (PⅢP)、Ⅳ型胶原 (C Ⅳ )和层黏蛋白 (LN)浓度明显下降。与治疗前相比 ,两组差异均有显著性 (P <0 .0 5 ) ;治疗组在HBeAg转阴率、HA、C Ⅳ的改善方面均优于对照组 (P <0 .0 5 )。结论 :氧化苦参碱联合拉米呋定治疗慢性乙肝能有效改善肝功能 ,抗病毒方面有协同作用 ,并能增强抗纤维化效果     

中药苦参汤中氧化苦参碱的含量测定

将苦参汤浸膏经索氏提取，硅胶预滤柱精制后，用ＴＬＣ－比色法测定其中氧化苦参碱的含量，测定波长λ＝４１８ｎｍ，回归方程Ｃ＝１５．８８４５ａ－０．０７５７８，ｒ＝０．９９９２，ｎ＝３。     

高效液相色谱法测定苦参素分散片的含量

目的 建立高效液相色谱法测定苦参素分散片含量的方法。方法 以Phenomenex C₁₈柱为固定相;流动相0.02mol·L^-1磷酸二氢钠溶液(pH3.5)-甲醇(90∶10);流量1.0ml·min^-1;检测波长220nm。结果 氧化苦参碱与氧化槐果碱分离良好,氧化苦参碱在0.04～0.16mg·ml^-1浓度范围内呈良好的直线关系,平均回收率为99.4%,RSD为0.78%(n=9)。结论 该方法简便、灵敏、准确、重复性好,可用于该制剂的质量控制。     

氧化苦参碱胃内滞留缓释片的研制

目的：为延长苦参素的作用时间，降低肠道菌群的降解作用，便于给药，制成苦参素胃内滞留缓释片。方法：以HPMC为骨架材料，十六醇为助漂剂，碱式碳酸镁为产气剂，制备了一天给药两次的胃内滞留型缓释片，并进行体外累积释放度测定。结果：体外释药符合Higuchi方程，r=0．9864，体外释药量与释药时间具有良好的相关性，3个取样点及累积释放百分率分别为：1h20％。45％、2h35％～60％、8h75％以上，且起漂时间不超过5min。结论：该缓释片处方工艺简单，适合工业化生产；缓释效果明显。