马兜铃科植物Aristolochia triangularis的生物碱成分研究

从马兜铃科植物Aristolochia triangularis的根部分离出十五个生物碱成分，其中两种成分triangularine-A和triangularine-B系列生物碱，三种系阿卟啡类季胺碱，这些化合物的结构经各种波谱（IR，UV，MS，2D NMR）解析和化学转化技术得以确定。     

Alkaloids from the Roots of Aristolochia Triangularis(I)

从马兜铃科植物Ａｒｉｓｔｏｌｏｃｈｉａｔｒｉａｎｇｕｌａｒｉｓ的根部分离出十五个生物碱成分。其中两种成分ｔｒｉａｎｇｕｌａｒｉｎｅ－Ａ和ｔｒｉａｎｇｕｌａｒｉｎｅ－Ｂ系新生物碱，三种系阿卟啡类季铵碱。这些化合物的结构经各种波谱（ＩＲ，ＵＶ，ＭＳ，２ＤＮＭＲ）解析和化学转化技术得以确定。     

Toxicities of aristolochic acid I and aristololactam I in cultured renal epithelial cells

Aristolochic acid nephropathy, a progressive tubulointerstitial renal disease, is primarily caused by aristolochic acid I (AA-I) intoxication. Aristololactam I (AL-I), the main metabolite of AA-I, may also participate in the processes that lead to renal damage. To investigate the role and mechanism of the AL-I-mediated cytotoxicity, we determined and compared the cytotoxic effects of AA-I and AL-I on cells of the human proximal tubular epithelial (HK-2) cell line. To this end, we treated HK-2 cells with AA-I and AL-I and assessed the cytotoxicity of these agents by using the 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay, flow cytometry, and an assay to determine the activity of caspase 3. The proliferation of HK-2 cells was inhibited in a concentration- and time-dependent manner. Cell-cycle analysis revealed that the cells were arrested in the S-phase. Apoptosis was evidenced by the results of the annexin V/propidium iodide (PI) assay and the occurrence of a sub-G1 peak. In addition, AA-I and AL-I increased caspase 3-like activity in a concentration-dependent manner. These results also suggested that the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase 3-dependent pathway.     

3种马兜铃酸和2种马兜铃内酰胺在北细辛、华细辛及汉城细辛不同部位的分布及含量分析

目的 考察3种马兜铃酸和2种马兜铃内酰胺在《中华人民共和国药典》（简称“《中国药典》”）收载的北细辛、华细辛及汉城细辛不同部位中的分布和含量。方法 采用HPLC-DAD测定北细辛、汉城细辛和华细辛的果、叶、根及根茎中马兜铃酸I等3种马兜铃酸和2种马兜铃内酰胺的含量,并以LC-MS检测细辛根及根茎中马兜铃酸I是否存在。结果 通过对30份细辛果、97份细辛叶和97份细辛根及根茎样品检测的结果表明：3种细辛的果中均分布较高含量的马兜铃酸I（0.095-2.200 mg ?g-1）、9-羟基马兜铃酸I（0.012-0.103 mg?g-1）、马兜铃内酰胺I（0.025-0.147 mg?g-1）和马兜铃内酰胺II（0.120-0.144 mg?g-1）,未检测到马兜铃酸II;3种细辛的叶中（除了2份样品）均分布有马兜铃酸I,含量为0.010-0.140 mg?g-1,其它4种成分未检测到;HPLC法在细辛根及根茎的97份样品中均未检测到3种马兜铃酸和2种马兜铃内酰胺中的任何1种,但经过灵敏度更高的LCMS检验,所测定的4份细辛根及根茎样品中均分布极微量的马兜铃酸I（0.4-2.4 μg?g-1）。结论 本研究通过检测大量的细辛采集样品和多省市的细辛商品,报道了3种马兜铃酸和2种马兜铃内酰胺在《中国药典》收载细辛不同部位中的分布和含量情况,为《中国药典》（2005年版）把细辛药用部位由“全草”修订为“根及根茎”而保证细辛的临床用药安全提供了科学数据的支撑。