Cytotoxicity of naphthoquinones and their capacity to generate reactive oxygen species is quenched when conjugated with gold nanoparticles.
Cytotoxicity of naphthoquinones and their capacity to generate reactive oxygen species is quenched when conjugated with gold nanoparticles.
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DOI：
10.2147/ijn.s24074
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发表时间：
2011
影响因子：
8
通讯作者：
Mukhopadhyay D
中科院分区：
文献类型：
--
作者：
Srinivas P;Patra CR;Bhattacharya S;Mukhopadhyay D
白花丹素是一种从白花丹科植物中分离得到的萘醌衍生物，已有多篇报道证实其具有抗癌活性。然而，据我们所知，没有报道描述了金与白花丹素的纳米缀合，即使白花丹素被认为是一种有前途的治疗剂。在这份报告中，我们展示了与白花丹素（AuPB）结合的金纳米颗粒的制造和表征，可以降低后者的毒性，以及它们的细胞定位和产生活性氧的能力。研究了白花丹素的抗肿瘤活性和产生活性氧的能力，并与1，4-萘醌的溴代衍生物2-溴-1，4-萘醌（2-BNQ）和2，3-二溴-1，4-萘醌（2，3-DBNQ）及其金纳米结合物的抗肿瘤活性和产生活性氧的能力进行了比较。与原始化合物（即，白花丹素、2-BNQ和2，3-DBNQ）相比，金纳米缀合物形式的白花丹素和1，4-萘醌的溴衍生物显示出降低的细胞毒性和细胞凋亡。有趣的是，我们观察到金纳米颗粒可以淬灭白花丹素，2-BNQ和2，3-BNQ的活性氧物质产生能力，这是萘醌的主要作用机制之一。因此，可以得出结论，与金纳米颗粒结合可以降低这些化合物的细胞毒性。
Several reports have demonstrated the anticancer activities of plumbagin, a naphthoquinone derivative isolated from plants belonging to Plumbaginaceae family. However, to the best of our knowledge, there are no reports which describe gold nanoconjugation with plumbagin, even though plumbagin is considered to be a promising therapeutic agent. In this report, we demonstrate the fabrication and characterization of gold nanoparticles conjugated with plumbagin (AuPB) that can reduce the toxicity of the latter, and their capacity for cellular localization and generation of reactive oxygen species. The anticancer activity and ability of plumbagin to produce reactive oxygen species was studied and compared with that of bromoderivatives of 1,4 naphthoquinones such as 2-bromo-1,4-naphthoquinone (2-BNQ) and 2,3-dibromo-1, 4-naphthoquinone (2,3-DBNQ) and their gold nanoconjugates. Plumbagin and bromoderivatives of 1,4 naphthoquinones in the form of gold nanoconjugates showed reduced cytotoxicity and apoptosis compared with the pristine compounds, ie, plumbagin, 2-BNQ, and 2,3-DBNQ. Interestingly, we observed that the gold nanoparticles could quench the reactive oxygen species-generating capacity of plumbagin, 2-BNQ, and 2,3-BNQ, which is one of the main mechanisms of action of the naphthoquinones. Therefore, it can be concluded that conjugation with gold nanoparticles can reduce the cytotoxicity of these compounds.