Abstract
Multifloroside (4), together with 10-hydroxyoleoside 11-methyl ester (1), 10-hydroxyoleoside dimethyl ester (2), and 10-hydroxyligustroside (3), are all secoiridoids, which are naturally occurring compounds that possess a wide range of biological and pharmacological activities. However, the anti-cancer activity of 1–4 has not been evaluated yet. The objective of this work was to study the anti-cancer activities of 1–4 in the human epidermoid carcinoma cell lines A431 and the human non-small cell lung cancer (NSCLC) cell lines A549. The results indicate that 1–4 differ in potency in their ability to inhibit the proliferation of human A431 and A549 cells, and multifloroside (4) display the highest inhibitory activity against A431 cells. The structure-activity relationships suggest that the o-hydroxy-p-hydroxy-phenylethyl group may contribute to the anti-cancer activity against A431 cells. Multifloroside treatment can also inhibit cell colony formation, arrest the cell cycle in the S-phase, increase the levels of reactive-oxygen-species (ROS), and mitochondrial membrane potential (MMP), but it did not significantly induce cell apoptosis at low concentrations. The findings indicated that multifloroside (4) has the tendency to show selective anti-cancer effects in A431 cells, along with suppressing the colony formation, inducing S cell cycle arrest, ROS production, and increasing MMP.
Highlights
Cancer is currently the second leading cause of death globally [1,2,3]
Throughout the of development of of human society, nature has catered tobasic the needs basic needs of humans, not the least which is the human society, nature has to the of humans, not the least of which is the provision human society, nature has catered to the basic needs of humans, not the least of which is the provision of medicines for the treatment of a wide spectrum of diseases [22,23]
The results showed that 1–4 possess different anti-proliferative activities against A549 and A431 cells, and that 4 had the most potent inhibitory activity against A431 cells (Figure 2)
Summary
Cancer is currently the second leading cause of death globally [1,2,3]. While great strides have been made in the treatment of cancer in recent decades, we still face many open challenges to existing cancer therapies, such as adaptive resistance [4]. Throughout the development of human society, the importance of natural products [4,5,6,7,8,9] and their derivatives [10,11,12] in cancer treatment or prevention is supported by abundant evidence from cancer research [3,13,14], and give hopes to cancer patients. The Oleaceae is a botanical family of woody dicotyledonous plants that are important in daily lives of many people due to their broad economic, food, and medicinal values. The Oleaceae is a botanical family of woody dicotyledonous plants that are important in daily. Molecules 2020, 25, 7 lives of many people due to their broad economic, food, and medicinal values. A total of 232 secoiridoids (glycosides, aglycones, derivatives, and dimers) have been reported,from a total of 232insecoiridoids (glycosides, aglycones, derivatives, and dimers) have been isolated isolated species the Oleaceae
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