紫杉醇综述:历史与未来挑战
A Compressive Review about Taxol: History and Future Challenges.
机构信息
Department of Biochemistry and Molecular Biology (B) and Immunology, Faculty of Chemistry, University of Murcia, Campus de Espinardo, Regional Campus of International Excellence "Campus Mare Nostrum", P.O. Box 4021, 30100 Murcia, Spain.
出版信息
Molecules. 2020 Dec 17;25(24):5986. doi: 10.3390/molecules25245986.
Taxol, which is also known as paclitaxel, is a chemotherapeutic agent widely used to treat different cancers. Since the discovery of its antitumoral activity, Taxol has been used to treat over one million patients, making it one of the most widely employed antitumoral drugs. Taxol was the first microtubule targeting agent described in the literature, with its main mechanism of action consisting of the disruption of microtubule dynamics, thus inducing mitotic arrest and cell death. However, secondary mechanisms for achieving apoptosis have also been demonstrated. Despite its wide use, Taxol has certain disadvantages. The main challenges facing Taxol are the need to find an environmentally sustainable production method based on the use of microorganisms, increase its bioavailability without exerting adverse effects on the health of patients and minimize the resistance presented by a high percentage of cells treated with paclitaxel. This review details, in a succinct manner, the main aspects of this important drug, from its discovery to the present day. We highlight the main challenges that must be faced in the coming years, in order to increase the effectiveness of Taxol as an anticancer agent.
紫杉醇,又称紫杉醇,是一种广泛用于治疗不同癌症的化疗药物。自发现其抗肿瘤活性以来,紫杉醇已用于治疗超过 100 万名患者,使其成为使用最广泛的抗肿瘤药物之一。紫杉醇是文献中描述的第一种微管靶向剂,其主要作用机制包括破坏微管动力学,从而诱导有丝分裂停滞和细胞死亡。然而,也已经证明了实现细胞凋亡的次要机制。尽管紫杉醇用途广泛,但它也存在某些缺点。紫杉醇面临的主要挑战是需要找到一种基于使用微生物的环境可持续生产方法,在不对患者健康产生不利影响的情况下提高其生物利用度,并最大限度地减少大量用紫杉醇治疗的细胞所呈现的耐药性。这篇综述简要地详述了这种重要药物从发现到现在的主要方面。我们强调了未来几年必须面对的主要挑战,以提高紫杉醇作为抗癌药物的有效性。