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Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection.
Medicinal Research Reviews ( IF 10.9 ) Pub Date : 2004 Jan , DOI: 10.1002/med.10053 Robert H. Cichewicz , Samir A. Kouzi
Medicinal Research Reviews ( IF 10.9 ) Pub Date : 2004 Jan , DOI: 10.1002/med.10053 Robert H. Cichewicz , Samir A. Kouzi
3beta-Hydroxy-lup-20(29)-en-28-oic acid (betulinic acid) is a pentacyclic lupane-type triterpene that is widely distributed throughout the plant kingdom. A variety of biological activities have been ascribed to betulinic acid including anti-inflammatory and in vitro antimalarial effects. However, betulinic acid is most highly regarded for its anti-HIV-1 activity and specific cytotoxicity against a variety of tumor cell lines. Interest in developing even more potent anti-HIV agents based on betulinic acid has led to the discovery of a host of highly active derivatives exhibiting greater potencies and better therapeutic indices than some current clinical anti-HIV agents. While its mechanism of action has not been fully determined, it has been shown that some betulinic acid analogs disrupt viral fusion to the cell in a post-binding step through interaction with the viral glycoprotein gp41 whereas others disrupt assembly and budding of the HIV-1 virus. With regard to its anticancer properties, betulinic acid was previously reported to exhibit selective cytotoxicity against several melanoma-derived cell lines. However, more recent work has demonstrated that betulinic acid is cytotoxic against other non-melanoma (neuroectodermal and malignant brain tumor) human tumor varieties. Betulinic acid appears to function by means of inducing apoptosis in cells irrespective of their p53 status. Because of its selective cytotoxicity against tumor cells and favorable therapeutic index, even at doses up to 500 mg/kg body weight, betulinic acid is a very promising new chemotherapeutic agent for the treatment of HIV infection and cancer.
中文翻译:
桦木酸在预防和治疗癌症和艾滋病毒感染方面的化学,生物活性和化学治疗潜力。
3beta-Hydroxylup-20(29)-en-28-oic acid(betulinic acid)是一种五环环戊烷型三萜,广泛分布于整个植物界。桦木酸具有多种生物学活性,包括抗炎和体外抗疟作用。然而,倍他林酸因其抗HIV-1活性和对多种肿瘤细胞系的特异性细胞毒性而受到高度评价。对开发基于桦木酸的更有效的抗HIV药物的兴趣已导致发现了许多高活性衍生物,这些衍生物比某些当前的临床抗HIV药物具有更高的效力和更好的治疗指数。尽管其作用机理尚未完全确定,已经显示,一些桦木酸类似物通过与病毒糖蛋白gp41的相互作用,在结合后步骤中破坏了病毒与细胞的融合,而另一些破坏了HIV-1病毒的装配和出芽。关于其抗癌特性,先前报道了桦木酸对几种黑素瘤来源的细胞系表现出选择性的细胞毒性。但是,最近的研究表明,桦木酸对其他非黑色素瘤(神经外胚层和恶性脑肿瘤)人类肿瘤品种具有细胞毒性。桦木酸似乎通过诱导细胞凋亡而发挥功能,而与它们的p53状态无关。由于其对肿瘤细胞的选择性细胞毒性和良好的治疗指数,即使剂量高达500 mg / kg体重,
更新日期:2017-01-31
中文翻译:
桦木酸在预防和治疗癌症和艾滋病毒感染方面的化学,生物活性和化学治疗潜力。
3beta-Hydroxylup-20(29)-en-28-oic acid(betulinic acid)是一种五环环戊烷型三萜,广泛分布于整个植物界。桦木酸具有多种生物学活性,包括抗炎和体外抗疟作用。然而,倍他林酸因其抗HIV-1活性和对多种肿瘤细胞系的特异性细胞毒性而受到高度评价。对开发基于桦木酸的更有效的抗HIV药物的兴趣已导致发现了许多高活性衍生物,这些衍生物比某些当前的临床抗HIV药物具有更高的效力和更好的治疗指数。尽管其作用机理尚未完全确定,已经显示,一些桦木酸类似物通过与病毒糖蛋白gp41的相互作用,在结合后步骤中破坏了病毒与细胞的融合,而另一些破坏了HIV-1病毒的装配和出芽。关于其抗癌特性,先前报道了桦木酸对几种黑素瘤来源的细胞系表现出选择性的细胞毒性。但是,最近的研究表明,桦木酸对其他非黑色素瘤(神经外胚层和恶性脑肿瘤)人类肿瘤品种具有细胞毒性。桦木酸似乎通过诱导细胞凋亡而发挥功能,而与它们的p53状态无关。由于其对肿瘤细胞的选择性细胞毒性和良好的治疗指数,即使剂量高达500 mg / kg体重,