CirTech Institute, Ho Chi Minh City University of Technology (HUTECH), Ho Chi Minh City 700000, Vietnam.
Institute of Research and Development, Duy Tan University, Danang 550000, Vietnam.
Molecules. 2020 Jun 24;25(12):2912. doi: 10.3390/molecules25122912.
Cancer is the second leading cause of death globally, and despite the advances in drug development, it is still necessary to develop new plant-derived medicines. Compared with using conventional chemical drugs to decrease the side effects induced by chemotherapy, natural herbal medicines have many advantages. The present study aimed to discover the potential cytotoxicity of ethanol extract and its derived fractions (chloroform, ethyl acetate, butanol, and aqueous) of Bonati. () on human large cell lung carcinoma (NCI-H460) and hepatocellular carcinoma (HepG2). Among these fractions, the chloroform showed significant activity in the inhibition of proliferation of both cancerous cells because of the presence of bioactive compounds including xanthomicrol, 5,4'-dihydroxy-6,7,8,3'-tetramethoxyflavone, and ursolic acid which were clearly revealed by nuclear magnetic resonance spectroscopy (H-NMR, C-NMR, Heteronuclear Multiple Bond Coherence, and Heteronuclear Single Quantum Coherence Spectroscopy) analyses. According to the radical scavenging capacity, the 5,4'-dihydroxy-6,7,8,3'-tetramethoxyflavone compound (AB2) exhibited the highest anticancer activity on both NCI-H460 and HepG2 with IC values of 4.57 ± 0.32 and 5.67 ± 0.09 µg/mL respectively, followed by the ursolic acid with the lower percent inhibition at 13.05 ± 0.55 and 10.00 ± 0.16 µg/mL, respectively ( < 0.05). Remarkably, the AB2 compound induced to significant increase in the production of reactive oxygen species accompanied by attenuation of mitochondrial membrane potential, thus inducing the activation of caspase-3 activity in both human lung and liver cancer cells. These results suggest that is a promising source of useful natural products and AB2 offers opportunities to develop the novel anticancer drugs.
癌症是全球第二大死亡原因,尽管药物开发取得了进展,但仍有必要开发新的植物衍生药物。与使用传统化学药物来减少化疗引起的副作用相比,天然草药具有许多优势。本研究旨在发现 Bonati 的乙醇提取物及其衍生的氯仿、乙酸乙酯、正丁醇和水相部分对人非小细胞肺癌(NCI-H460)和肝癌(HepG2)的潜在细胞毒性。在这些部分中,氯仿由于存在包括黄烷酮、5,4'-二羟基-6,7,8,3'-四甲氧基黄酮和熊果酸在内的生物活性化合物,对两种癌细胞的增殖抑制具有显著活性,这些化合物通过核磁共振波谱(H-NMR、C-NMR、异核多键相干和异核单量子相干光谱)分析得到了清晰的揭示。根据自由基清除能力,5,4'-二羟基-6,7,8,3'-四甲氧基黄酮化合物(AB2)在 NCI-H460 和 HepG2 上均表现出最高的抗癌活性,IC 值分别为 4.57±0.32 和 5.67±0.09µg/mL,其次是熊果酸,抑制率分别为 13.05±0.55 和 10.00±0.16µg/mL(<0.05)。值得注意的是,AB2 化合物诱导活性氧的产生显著增加,同时线粒体膜电位降低,从而导致人肺和肝癌细胞中 caspase-3 活性的激活。这些结果表明,是有前途的天然产物来源,AB2 为开发新型抗癌药物提供了机会。