Department of Chemistry, Shantou University, Daxue Road 243#, Shantou 515063, China.
Biosens Bioelectron. 2010 Apr 15;25(8):1947-52. doi: 10.1016/j.bios.2010.01.011. Epub 2010 Jan 18.
A sensitive and reliable assay has been developed to directly screen DNA-targeted anticancer drugs in vitro via using resonance light scattering (RLS) technique. The results of experiments displayed that the increment of RLS intensity was directly proportional to the antitumor effect of anticancer drugs. Through the RLS spectra, the activities of four drugs have been demonstrated as mitoxantrone (MIT)>epirarubicin (EPI)>daunorubicin (DAU)>adriamycin (ADM). However, to further verify the activities of the above four drugs, binding constant (k) for each of them has been calculated by RLS technique as follows: k(RLS) (MIT, 8.75 x 10(5) L mol(-1))>k(RLS) (EPI, 6.58 x 10(5) L mol(-1))>k(RLS) (DAU, 4.79 x 10(5) L mol(-1))>k(RLS) (ADM, 3.82 x 10(5) L mol(-1)). Also, this RLS assay result was validated by seasoned vitro screening methods for anticancer drugs. In all, the proposed RLS is not only a simple, sensitive, objective and straightforward method, but also it is an unprecedented assay for primarily screening DNA-targeted anticancer drugs.
已开发出一种灵敏可靠的测定法,通过使用共振光散射(RLS)技术,可直接在体外筛选针对 DNA 的抗癌药物。实验结果表明,RLS 强度的增加与抗癌药物的抗肿瘤作用直接成正比。通过 RLS 光谱,已证明四种药物的活性为米托蒽醌(MIT)>表柔比星(EPI)>柔红霉素(DAU)>阿霉素(ADM)。然而,为了进一步验证上述四种药物的活性,已通过 RLS 技术计算了它们各自的结合常数(k),如下所示:k(RLS)(MIT,8.75 x 10(5)L mol(-1))>k(RLS)(EPI,6.58 x 10(5)L mol(-1))>k(RLS)(DAU,4.79 x 10(5)L mol(-1))>k(RLS)(ADM,3.82 x 10(5)L mol(-1))。此外,该 RLS 测定结果已通过经验证的体外抗癌药物筛选方法进行了验证。总之,所提出的 RLS 不仅是一种简单、灵敏、客观和直接的方法,而且还是一种用于初步筛选针对 DNA 的抗癌药物的前所未有的测定法。