Department of Biochemistry and Molecular Biology, Medical University, Lublin, Poland
Department of Organic Chemistry, Medical University of Silesia, Katowice, Poland.
Anticancer Res. 2020 Nov;40(11):6151-6158. doi: 10.21873/anticanres.14635.
BACKGROUND/AIM: Glioma is the most malignant tumour of the human brain still lacking effective treatment modalities. Betulin, a pentacyclic triterpene abundantly found in the birch bark, has been shown to demonstrate interesting anti-cancer activity towards many cancer cells. We determined the effects of acetylenic synthetic betulin derivatives (ASBDs) as anti-tumour agents on glioma cells in vitro.
T98G and C6 glioma cell viability and proliferation were determined by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay and BrdU (bromo deoxyuridine) test, respectively. Cell-cycle progression and induction of apoptosis were investigated with flow cytometry.
ASBDs significantly decreased glioma cell viability/survival and inhibited proliferation in a dose-dependent manner in vitro. Moreover, ASBDs were more cytotoxic than clinically used chemotherapeutics - temozolomide and cisplatin.
ASBDs may be considered for further study as potent anti-tumour agents in glioma treatment.
背景/目的：脑胶质瘤是目前人类大脑中最恶性的肿瘤，仍缺乏有效的治疗方法。桦树皮中大量存在的五环三萜白桦脂醇已被证明对许多癌细胞具有有趣的抗癌活性。我们测定了炔丙基合成白桦脂醇衍生物（ASBDs）作为抗肿瘤剂在体外对神经胶质瘤细胞的作用。
通过 MTT（3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴盐）测定法和 BrdU（溴脱氧尿苷）试验分别测定 T98G 和 C6 神经胶质瘤细胞的活力和增殖。通过流式细胞术研究细胞周期进程和凋亡诱导。
ASBDs 显著降低了体外神经胶质瘤细胞的活力/存活，并呈剂量依赖性抑制增殖。此外，ASBDs 的细胞毒性比临床使用的化疗药物-替莫唑胺和顺铂更强。
ASBDs 可被视为进一步研究的有潜力的抗肿瘤药物，用于治疗脑胶质瘤。
