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

Ngoc Hong Nguyen,Thuc-Huy Duong,Quang Thang Pham,Van Trung Phung,Thi Ngoc Han Luong,Van Giau Vo,Qui Thanh Hoai Ta

doi:10.3390/molecules25122912

Abstract

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 Adenosma bracteosum Bonati. (A. bracteosum) 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 (1H-NMR, 13C-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 IC50 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 (p < 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 A. bracteosum is a promising source of useful natural products and AB2 offers opportunities to develop the novel anticancer drugs.

Highlights

A major problem of public health, cancer is one of the main causes of death globally
The brine shrimp assay is significantly associated with in vitro growth inhibition of human solid tumor cell lines which was demonstrated by the National Cancer Institute (NCI, USA) and it can show the value of this bioassay as a pre-screening tool for antitumor drug research [33]
N-butanol fraction, and aqueous fraction gave LC50 > 1000 μg/mL, that are considered to be inactive. The variation in their results is possibly because of the different polarities of the solvents, the ethanol solvent is less polar than aqueous one and the phytochemicals of the ethanol extract contain specific molecules that have provided its cytotoxic activity against brine shrimp

Summary

Introduction

A major problem of public health, cancer is one of the main causes of death globally. The prevalence of this disease is rising, more rapidly in Africa, Asia, and Central and South America that make up about 70% of cancer deaths in the world [1]. The chemotherapy is one of the ways to treat this disease and the advances in anticancer drugs have improved patient care. The continuing search for anticancer agents/compounds from plants played a critical role to find the possible ways to have safe and to decrease the side effects induced by chemotherapy since natural herbal medicines have many advantages [7,8,9,10]

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Conclusion