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桦木酸及其肿瘤抑制药理作用(综述)

Betulinic acid and the pharmacological effects of tumor suppression (Review).

作者信息

Zhang Xia, Hu Jingyu, Chen Yan

机构信息

Department of Hematology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei 430022, P.R. China.

出版信息

Mol Med Rep. 2016 Nov;14(5):4489-4495. doi: 10.3892/mmr.2016.5792. Epub 2016 Oct 4.

Abstract

Betulinic acid (BA), a lupane-type pentacyclic triterpenoid saponin from tree bark, has the potential to induce the apoptosis of cancer cells without toxicity towards normal cells in vitro and in vivo. The antitumor pharmacological effects of BA consist of triggering apoptosis via the mitochondrial pathway, regulating the cell cycle and the angiogenic pathway via factors, including specificity protein transcription factors, cyclin D1 and epidermal growth factor receptor, inhibiting the signal transducer and activator of transcription 3 and nuclear factor‑κB signaling pathways, preventing the invasion and metastasis of tumor cells, and affecting the expression of topoisomerase I, p53 and lamin B1. In previous years, several studies have shown its antitumor effect, initially applied to malignant melanoma, however, it also has broad efficacies against most solid types of tumor from different regions of the body. There have been few investigations in hematological malignancies, however, this direction may offer potential in such a novel field of research. In this review, the primary pharmacological effects of BA in tumors, particularly in hematological malignancies are discussed.

摘要

桦木酸(BA)是一种从树皮中提取的羽扇豆烷型五环三萜皂苷,在体外和体内均有诱导癌细胞凋亡而对正常细胞无毒性的潜力。BA的抗肿瘤药理作用包括通过线粒体途径触发凋亡、通过特异性蛋白转录因子、细胞周期蛋白D1和表皮生长因子受体等因子调节细胞周期和血管生成途径、抑制信号转导和转录激活因子3以及核因子-κB信号通路、防止肿瘤细胞的侵袭和转移,以及影响拓扑异构酶I、p53和核纤层蛋白B1的表达。近年来,多项研究显示了其抗肿瘤作用,最初应用于恶性黑色素瘤,然而,它对身体不同部位的大多数实体瘤类型也具有广泛疗效。血液系统恶性肿瘤方面的研究较少,不过,这一方向可能在这一新型研究领域具有潜力。在本综述中,将讨论BA在肿瘤尤其是血液系统恶性肿瘤中的主要药理作用。

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