Search

The present study assessed two different plant parts (leaves and tubers) of Arum italicum species growing in Northeast Algeria for their phytochemical composition and pharmacological effects. The phytochemical content was determined using ultra-high-performance liquid chromatography coupled with a diode array detector and an electrospray mass spectrometer (UHPLC-DADESI/MS). The results revealed that the tuber extract was rich in lignans with a fraxiresinol glycoside as the major compound. In contrast, the leaf extract was rich in flavonoid glycosides, described for the first time in the aerial part of this species. The extract’s inhibitory activity against key enzymes was linked to hyperglycemia, α-glucosidase, and α-amylase, and their ability to inhibit the growth of human gastric carcinoma (AGS) and lung carcinoma (A549) cancer cell lines was also assessed. A cell line morphology study was also conducted with the most effective extract. The chromatin status of the cells was evaluated using DAPI, while the cytoplasmic morphology was evaluated using phalloidin. The tuber extract generally inhibited α-glucosidase and α-amylase enzymes more efficiently than the leaf extract. Its inhibition effect against the α-glucosidase was significantly higher when compared to the standard acarbose. The tuber extract also caused more viability loss of AGS and A549 cancer cells than the leaf extract in the cytotoxicity assay. In conclusion, our findings show that, compared to the leaf extract, the tuber extract exhibited more pronounced biological effects. The strong inhibitory potential of the tuber extract against the α-glucosidase enzyme should also be highlighted, which suggests it is a good candidate for discovering new antidiabetic agents. [ABSTRACT FROM AUTHOR]

Eugenol, 4-allyl-2-methoxyphenol, is the main constituent of clove essential oil and has demonstrated relevant biological activity, namely anticancer activity. Aiming to increase this activity, we synthesized a series of eugenol β-amino alcohol and β-alkoxy alcohol derivatives, which were then tested against two human cancer cell lines, namely gastric adenocarcinoma cells (AGS) and lung adenocarcinoma cells (A549). An initial screening was performed to identify the most cytotoxic compounds. The results demonstrated that three β-amino alcohol derivatives had anticancer activity that justified subsequent studies, having been shown to trigger apoptosis. Importantly, the most potent molecules displayed no appreciable toxicity towards human noncancer cells. Structure-activity relationships show that changes in eugenol structure led to enhanced cytotoxic activity and can contribute to the future design of more potent and selective drugs. [ABSTRACT FROM AUTHOR]

Aplysia sea hares are harmless to humans and good materials for producing compounds with pharmacological properties. Aplysia species have been investigated for their human nutritional value. The knowledge on the metabolic machinery from edible Aplysia depilans Gmelin is herein broadened by identifying chlorophylls, phenolic acids, terpenes, including xanthophylls, and alkaloids, some being reported for the first time both in the species and genus. The anti-inflammatory potential was assessed using RAW 264.7 macrophages challenged with lipopolysaccharide, revealing that A. depilans ethyl acetate partionated fraction interfered with cellular NO levels, mainly due to a decrease on inducible nitric oxide synthase expression. A strong capacity to inhibit phospholipase A 2 and 5-lipoxygenase was also evidenced. Morphological studies with SH-SY5Y neuroblastoma cells demonstrated chromatin condensation compatible with apoptosis, confirmed by the activation of caspase 3/7. The anti-inflammatory and pro-apoptotic effects reinforce A. depilans as an interesting ingredient to be included on the formulation of smart foods and/or nutraceuticals. [ABSTRACT FROM AUTHOR]