Abstract
Incomptine A (IA) is a sesquiterpene lactone isolated from Decachaeta incompta that induces apoptosis, reactive oxygen species production, and a differential protein expression on the U-937 (diffuse histiocytic lymphoma) cell line. In this work, the antitumor potential of IA was investigated on Balb/c mice inoculated with U-937 cells and through the brine shrimp lethality (BSL) test. Furthermore, IA was subjected to molecular docking study using as targets proteins associated with processes of cancer as apoptosis, oxidative stress, and glycolytic metabolism. In addition to determining the potential toxicity of IA in human, its acute toxicity was performed in mice. Results reveals that IA showed high antilymphoma activity and BSL with an EC50 of 2.4 mg/kg and LC50 16.7 µg/mL, respectively. The molecular docking study revealed that IA has strong interaction on all targets used. In the acute oral toxicity, IA had a LD50 of 149 mg/kg. The results showed that the activities of IA including antilymphoma activity, BSL, acute toxicity, and in silico interactions were close to the methotrexate, an anticancer drug used as positive control. These findings suggest that IA may serve as a candidate for the development of a new drug to combat lymphoma.
Highlights
In the course of our continuing search for potential antitumoral agents [15,16,17,18] from plants commonly used in traditional medicine, in this research, the aerial parts of Decachaeta incompta were extracted by percolation with dichloromethane
The resultant extract was evaluated in the brine shrimp acute lethality test (BSLT) considering that this bioassay has been used as a bioindicator of the presence of potential antitumor agents in the crude extracts of plants [17,18,19]
Since the dichloromethane extract of Decachaeta incompta aerial parts (DEDi) and incomptine A (IA) showed significant BS lethality as well as antilymphoma activity, the results suggest that the brine shrimp lethality test may be used as an economic, rapid, and reliable bioassay to obtain antilymphoma agents [17,18,19]
Summary
Sesquiterpene lactones (SLs) are a group of phytochemicals present in species of the plant kingdom, abundant in the family Asteraceae with more than 5000 different structures reported. They are a large group of low molecular weight specialized metabolites with a 15 carbon skeleton. SLs are considering as a class of natural compounds with pharmaceutical relevance that may be an alternative for cancer therapy [1,2]. SLs have a wide range of biological activities such as antiamoebic, antigiardial, trypanocidal, antidiabetic, antibacterial, cytotoxic, antitumor, and phytotoxic [3,4,5,6,7,8]
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