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山奈酚诱导 HeLa 细胞发生内在途径的细胞凋亡并发挥抗肿瘤作用。

Kaempferitrin induces apoptosis via intrinsic pathway in HeLa cells and exerts antitumor effects.

机构信息

Facultad de Química Universidad Nacional Autónoma de México, Mexico.

出版信息

J Ethnopharmacol. 2013 Jan 30;145(2):476-89. doi: 10.1016/j.jep.2012.11.016. Epub 2012 Dec 2.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Justicia spicigera is used for the empirical treatment of cervical cancer in Mexico. Recently, we showed that Justicia spicigera extracts exerted cytotoxic and antitumoral effects and the major component of this extract was kaempferitrin (KM).

MATERIALS AND METHODS

The cytotoxic and apoptotic effect of KM on human cancer cells and human nontumorigenic cells were evaluated using MTT and TUNEL assays, and Annexin V/Propidium iodide detection by flow cytometry. The effect of KM on cell cycle was analyzed by flow cytometry with propidium iodide. The apoptotic and cell cycle effects were also evaluated by western blot analysis. Also, different doses of KM were injected intraperitoneally daily into athymic mice bearing tumors of HeLa cells during 32 days. The growth and weight of tumors were measured.

RESULTS

KM induces high cytotoxic effects in vitro and in vivo against HeLa cells. The general mechanisms by which KM induces cytotoxic effects include: cell cycle arrest in G1 phase and apoptosis via intrinsic pathway in a caspase dependent pathway. Also, KM exerts chemopreventive and antitumor effects.

CONCLUSION

KM exerts cytotoxic and antitumor effects against HeLa cells.

摘要

民族药理学相关性

在墨西哥,Justicia spicigera 被用于经验性治疗宫颈癌。最近,我们发现 Justicia spicigera 提取物具有细胞毒性和抗肿瘤作用,而该提取物的主要成分是山柰酚(KM)。

材料和方法

采用 MTT 和 TUNEL 检测法以及流式细胞术检测 Annexin V/碘化丙啶检测法,评估 KM 对人癌细胞和人非肿瘤细胞的细胞毒性和凋亡作用。用碘化丙啶通过流式细胞术分析 KM 对细胞周期的影响。通过 Western blot 分析还评估了 KM 对细胞凋亡和细胞周期的影响。此外,在 32 天内,将不同剂量的 KM 通过腹腔注射每天注射到荷有 HeLa 细胞肿瘤的无胸腺小鼠中。测量肿瘤的生长和重量。

结果

KM 在体外和体内对 HeLa 细胞均具有高细胞毒性作用。KM 诱导细胞毒性作用的一般机制包括:通过内在途径在 caspase 依赖性途径中使细胞周期停滞在 G1 期和凋亡。此外,KM 还具有化学预防和抗肿瘤作用。

结论

KM 对 HeLa 细胞具有细胞毒性和抗肿瘤作用。

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