CAJ | 학술논문

目的：研究钩吻生物碱化合物抗肿瘤效应及其诱导凋亡作用。方法①在小鼠 H22肝癌细胞小鼠移植性肿瘤模型上观察钩吻生物碱化合物对H22小鼠实体瘤的抑制作用；②AO/EB荧光染色法观察凋亡细胞的形态学变化；流式细胞仪PI染色检测细胞周期变化及凋亡率。结果腹腔注射钩吻素子对H22小鼠实体瘤的抑瘤率为40.29％、36.57％、22.89％；钩吻素甲对小鼠H22实体瘤的生长具有一定的抑制作用，抑瘤率为28.91％、16.85％、9.68％；但1-甲氧基钩吻碱小鼠 H22实体瘤没有明显的抑制作用。钩吻素子可诱导 SW480细胞发生凋亡形态学改变，并且可使SW480细胞周期阻滞于S期，阻止细胞从S期至G2期转移，从而诱导其凋亡。结论钩吻生物碱化合物特别是钩吻素子具有较强的抗肿瘤活性并具有一定的构效关系，钩吻素子的抗肿瘤作用机制可能与阻滞肿瘤细胞周期和促进肿瘤细胞凋亡作用有关。
목적：연구구문생물감화합물항종류효응급기유도조망작용。방법①재소서 H22간암세포소서이식성종류모형상관찰구문생물감화합물대H22소서실체류적억제작용；②AO/EB형광염색법관찰조망세포적형태학변화；류식세포의PI염색검측세포주기변화급조망솔。결과복강주사구문소자대H22소서실체류적억류솔위40.29％、36.57％、22.89％；구문소갑대소서H22실체류적생장구유일정적억제작용，억류솔위28.91％、16.85％、9.68％；단1-갑양기구문감소서 H22실체류몰유명현적억제작용。구문소자가유도 SW480세포발생조망형태학개변，병차가사SW480세포주기조체우S기，조지세포종S기지G2기전이，종이유도기조망。결론구문생물감화합물특별시구문소자구유교강적항종류활성병구유일정적구효관계，구문소자적항종류작용궤제가능여조체종류세포주기화촉진종류세포조망작용유관。
OBJECTIVE To investigate the antitumor effect and mechanisms of alkaloidal compounds from Gel-semium elegans Benth.METHODS ①The antitumor activity of alkaloid compounds were evaluated in the kunming mice bearing H22 hepatoma.②EB/AO double staining and The flow cytometry ( FCM) were used to investigate ap-optosis cells.RESULTS Koumine significantly inhibited the growth of mice implanted solid tumor of H 22 hepatoma in a dose-dependent manner,the inhibitory rates at dose of 4mg· kg -1,2mg· kg -1,1mg· kg -1 were 40.29%, 36.57% and 22.89%respectively;Gelsemine could inhibite H22 tumor in a dose-dependent manner and the inhibi-tory rates at dose of 4mg· kg -1 was 28.91%but Gelsevirine showed no significant inhibitory effect on H 22;2.Using flow cytometry suggested that koumine inhibited cell growth by specific blocking of the progression of cells through S -phase of the cell cycle and inducing apoptosis of tumor cells.CONCLUSION The anticancer effects of alkaloidal compounds from Gelsemium elegans Benth indicated that it has sufficient potential to warrant further investigation.Moreover ,inducing cell cycle arrest and leading to tumor cells apoptosis might be one of the possible mechanisms involved in the anticancer activity.