Laboratory for Experimental Oncology and Radiobiology, Center for Experimental and Molecular Medicine, Academic Medical Center, Amsterdam, The Netherlands.
Anticancer Drugs. 2010 Mar;21(3):215-27. doi: 10.1097/CAD.0b013e3283357c62.
New therapies using novel mechanisms to induce tumor cell death are needed with plants playing a crucial role as a source for potential anticancer compounds. One highly promising class of natural compounds are the triterpenoids with betulinic acid (BetA) as the most prominent representative. In-vitro studies have identified this agent as potently effective against a wide variety of cancer cells, also those derived from therapy-resistant and refractory tumors, whereas it has been found to be relatively nontoxic for healthy cells. In-vivo preclinically applied BetA showed some remarkable anticancer effects and a complete absence of systemic toxicity in rodents. BetA also cooperated with other therapies to induce tumor cell death and several potent derivatives have been discovered. Its antitumor activity has been related to its direct effects on mitochondria where it induces Bax/Bak-independent cytochrome-c release.
需要使用新的机制来诱导肿瘤细胞死亡的新疗法,而植物作为潜在抗癌化合物的来源起着至关重要的作用。一类非常有前途的天然化合物是三萜类化合物,其中以白桦脂酸(BetA)最为突出。体外研究已经确定这种药物对多种癌细胞具有强大的疗效,包括那些来自耐药和难治性肿瘤的癌细胞,而对健康细胞的毒性相对较低。在临床前的动物实验中,BetA 表现出了显著的抗癌作用,而且在啮齿动物中没有发现全身毒性。BetA 还与其他疗法合作诱导肿瘤细胞死亡,并发现了几种有效的衍生物。其抗肿瘤活性与其对线粒体的直接作用有关,在那里它诱导 Bax/Bak 非依赖性细胞色素 c 释放。