Brain Metastasis and NeuroVascular Disease Modelling Lab, Department of Life Sciences, School of Natural Sciences, Shiv Nadar University, NCR, India.
Materials Chemistry Lab, Department of Chemistry, School of Natural Sciences, Shiv Nadar University, NCR, India.
Mol Cell Biochem. 2019 Apr;454(1-2):123-138. doi: 10.1007/s11010-018-3458-x. Epub 2018 Nov 3.
Natural products from medicinal plants have always attracted a lot of attention due to their diverse and interesting therapeutic properties. We have employed the principles of green chemistry involving isomerization, coupling and condensation reaction to synthesize a class of compounds derived from eugenol, a naturally occurring bioactive phytophenol. The compounds were characterized structurally by H-, C-NMR, FT-IR spectroscopy and mass spectrometry analysis. The purity of compounds was detected by HPLC. The synthesized compounds exhibited anti-cancer activity. A 10-12-fold enhancement in efficiency of drug molecules (~ 1 µM) was observed when delivered with graphene oxide (GO) as a nanovehicle. Our data suggest cell death via apoptosis in a dose-dependent manner due to increase in calcium levels in specific cancer cell lines. Interestingly, the benzoxazine derivatives of eugenol with GO nanoparticle exhibited enhanced therapeutic potential in cancer cells. In addition to anti-cancer effect, we also observed significant role of these derivatives on parasite suggesting its multi-pharmacological capability.
药用植物来源的天然产物因其多样且有趣的治疗特性而一直受到广泛关注。我们运用绿色化学原理,包括异构化、偶联和缩合反应,合成了一类源自愈创木酚的化合物,愈创木酚是一种天然存在的生物活性植物酚。通过 H-NMR、C-NMR、FT-IR 光谱和质谱分析对化合物进行了结构表征。通过 HPLC 检测了化合物的纯度。合成的化合物表现出抗癌活性。当用氧化石墨烯 (GO) 作为纳米载体输送时,药物分子的效率提高了 10-12 倍(约 1 μM)。我们的数据表明,由于特定癌细胞系中钙水平的增加,细胞通过凋亡死亡呈剂量依赖性。有趣的是,具有 GO 纳米粒子的愈创木酚苯并恶嗪衍生物在癌细胞中表现出增强的治疗潜力。除了抗癌作用外,我们还观察到这些衍生物对寄生虫有显著作用,表明其具有多药理学能力。