Phenolic Profiling and Biological Potential of Ficus curtipes Corner Leaves and Stem Bark: 5-Lipoxygenase Inhibition and Interference with NO Levels in LPS-Stimulated RAW 264.7 Macrophages

Abstract

The economic value of fig trees has been globally acknowledged due to their utilization in the food industry, being also frequently used in traditional medicine. While ubiquitously distributed in Southeast Asia, Ficus curtipes Corner remains uninvestigated concerning its biological properties and chemical profile. HPLC-DAD-ESI/MSn characterization of methanol extracts obtained from the stem bark and leaves allowed the identification and quantitation of 21 phenolic compounds for the first time; the stem bark was predominantly rich in flavan-3-ols and apigenin derivatives, while solely apigenin-di-glycosides have been identified and quantitated on the leaf extract. Both extracts inhibited 5-lipoxygenase (5-LOX) activity in a concentration-dependent manner, the one obtained from the stem bark being significantly more active (IC50 = 10.75 μg/mL). The effect of both extracts on lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages was evaluated, and while the stem bark extract did not lead to a noticeable interference on nitric oxide (NO) levels, the extract obtained from the leaves notably decreased NO and L-citrulline levels at concentrations ranging from 250 to 500 μg/mL. Herein, F. curtipes is valorized due to its modulatory effects on inflammatory mediators and also as a source of bioactive phenols, which may fuel further studies on the development of nutraceuticals.

Lipoxygenase Inhibition by Plant Extracts

“…Extraction of leaves and stem bark of Ficus curtipes (Moraceae) was carried out in methanol [ 71 ]. Stem extract showed strong inhibition against LOX with an IC 50 value of 10.75 µg/mL, while leaf extract had significantly poorer IC 50 value (IC 50 = 200.80 µg/mL).…”

Malus baccata var. gracilis and Malus toringoides Bark Polyphenol Studies and Antioxidant, Antimicrobial and Anticancer Activities

“…Polyphenols act on tumors by different mechanisms, including the induction of detoxification enzymes and the activation of the antioxidant mechanism, antiproliferation, apoptosis through cell-cycle arrest, and molecular regulation of genes associated with cancer [2,[17][18][19][20]. Tree barks are promising sources of these polyphenols; they contain phenolic acids, flavonoids, and catechins, as well as sugars [2,12,19,21,22]. Phenolic acids are an important group of phenols as they act as antioxidant agents and have, for example, anticancer and antimicrobial properties [3,[23][24][25][26][27].Microbial infections with Staphylococcus aureus cause serious human diseases such as soft tissue infection, pneumonia, sepsis, and peritonitis [28,29].…”

Tailored Functionalization of Natural Phenols to Improve Biological Activity

“…In view of their importance, studies were aimed at breeding plants able to increase the content of bioactive phenols [ 23 ]. The research in the field continues, and more and more plants are investigated for their phenolic content and related bioactivity [ 24 , 25 , 26 , 27 , 28 , 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 ]. The antioxidant activity of natural phenols has been related to their scavenger ability towards free radicals [ 42 ].…”