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Anticancer Activity of Novel Plant Extracts and Compounds from Adenosma bracteosum (Bonati) in Human Lung and Liver Cancer Cells

机译:新型植物提取物和小牛腺(Bonati)化合物在人肺癌和肝癌细胞中的抗癌活性

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摘要

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.
机译:癌症是全球第二大死亡原因,尽管药物开发取得了进步,但仍然有必要开发新的植物源性药物。与使用常规化学药物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乙醇提取物及其衍生馏分(氯仿,乙酸乙酯,丁醇和水溶液)的潜在细胞毒性。 ()用于人类大细胞肺癌(NCI-H460)和肝细胞癌(HepG2)。在这些馏分中,由于存在生物活性化合物,包括黄嘌呤微醇,5,4'-二羟基-6,7,8,3'-四甲氧基黄酮和熊果酸,氯仿对两种癌细胞的增殖均具有抑制作用。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谱)分析可以清楚地看出。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)对NCI-H460和HepG2均表现出最高的抗癌活性,IC值为4.57±0.32和5.67分别为±0.09 µg / mL,其后是抑制率较低的熊果酸,分别为13.05±0.55和10.00±0.16 µg / mL(<0.05)。值得注意的是,AB2化合物诱导活性氧的产生显着增加,同时线粒体膜电位减弱,从而诱导人肺癌和肝癌细胞中caspase-3活性的激活。这些结果表明,这是有用的天然产物的有前途的来源,AB2提供了开发新型抗癌药物的机会。

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