首页> 外国专利> KALANCHOE FLAMMEA EXTRACT WITH ETHYL ACETATE, THE FRACTIONS AND MAJOR COMPOUNDS THEREOF FOR THE TREATMENT OF PROSTATE CANCER.

KALANCHOE FLAMMEA EXTRACT WITH ETHYL ACETATE, THE FRACTIONS AND MAJOR COMPOUNDS THEREOF FOR THE TREATMENT OF PROSTATE CANCER.

机译:用醋酸乙酯提取卡拉兰古拉提取物,用其馏分及其主要化合物治疗前列腺癌。

摘要

The present invention refers to a kalanchoe flammea extract with ethyl acetate (KfAcOEt-COP), the fractions and major compounds thereof, which may be used as cytotoxic or apoptosis inducers against prostate cancer, considering that Docetaxol is a more efficient drug, the KfAcOEt-COP extract (which has fractions and major compounds) shown to have more advantages than Docetaxol. First, a phyto-chemical study was performed where alkaloids, sterols and cardiac glycosides were found. Referring to cytotoxicity, the KfAcOEt-COP effect was evaluated as well as its fractions over the viability of PC3, LNCaP, PrEC and lymphocytes; these may exert a doses response effect after 24 h of exposition. Genotoxic studies in vitro and in vivo of KfAcOEt-COP and its fractions were performed, where no toxicity was found. The KfAcOEt-COP extract has evidence of inducing apoptosis after 6 h, the PC3 exposed to the extract showing an overproduction of ROS. The activation of caspases is intrinsically measure d, inducing the fragmentation of the DNA, showing a high level of excision of PARP-1 and inducing cell arrest in the synthesis phase. In an animal model, KfAcOEt-COP is able to inhibit the tumor growth in CaP cells.
机译:考虑到多西紫杉醇是更有效的药物,KfAcOEt-T,本发明涉及一种用乙酸乙酯(KfAcOEt-COP)制成的甘蓝甜菜提取物,其级分和主要化合物可用作抗前列腺癌的细胞毒性或凋亡诱导剂。 COP提取物(具有馏分和主要化合物)比多西紫杉醇具有更多的优势。首先,进行了植物化学研究,发现了生物碱,固醇和强心苷。关于细胞毒性,评估了KfAcOEt-COP效应及其在PC3,LNCaP,PrEC和淋巴细胞的存活率中所占的比例;这些可能会在暴露24小时后发挥剂量反应作用。进行了KfAcOEt-COP及其组分的体外和体内遗传毒性研究,未发现毒性。 KfAcOEt-COP提取物具有在6 h后诱导细胞凋亡的证据,暴露于提取物中的PC3显示出过量的ROS。半胱天冬酶的激活本质上是测量d,诱导DNA片段化,显示出PARP-1的高水平切除并诱导了合成阶段的细胞停滞。在动物模型中,KfAcOEt-COP能够抑制CaP细胞中的肿瘤生长。

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