Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design

Abstract

Halimium halimifolium (Hh) is a shrub used in Algerian folk medicine to treat gastrointestinal pain. An UHPLC-PDA-ESI/MSn method was developed to identify the metabolic profile of the traditionally used infusion (Hh-A) from the aerial parts. The structures of flavanols were confirmed by NMR analysis after the isolation procedure from a hydrohalcolic extract (Hh-B) that also allowed for the identification of phenolic acids, an aryl butanol glucoside, and different derivatives of quercetin, myricetin, and kaempferol. Tiliroside isomers were the chemical markers of Hh-A and Hh-B (54.33 and 36.00 mg/g, respectively). Hh-A showed a significant scavenging activity both against the radicals 1,1-diphenyl-2-picrylhydrazyl and 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (EC50 = 10.49 µg/mL and TEAC value = 1.98 mM Trolox/mg infusion) and the lipopolysaccharide-induced reactive oxygen species release in A375 and HeLa cells. Moreover, the antihyperglycemic properties, by inhibiting the α-amylase and α-glucosidase enzymes (IC50 = 0.82 mg/mL and 25.01 µg/mL, respectively), were demonstrated. To upgrade the therapeutic effect, a microencapsulation process is proposed as a strategy to optimize stability, handling, and delivery of bioactive components, avoiding the degradation and loss of the biological efficacy after oral intake. Hh-loaded microparticles were designed using cellulose acetate phthalate as the enteric coating material and spray drying as a production process. The results showed a satisfactory process yield (67.9%), encapsulation efficiency (96.7%), and micrometric characteristics of microparticles (laser-scattering, fluorescent, and scanning electron microscopy). In vitro dissolution studies (USPII-pH change method) showed that Hh-loaded microparticles are able to prevent the release and degradation of the bioactive components in the gastric tract, releasing them into the intestinal environment.

Hitting the sweet spot: A systematic review of the bioactivity and health benefits of phenolic glycosides from medicinally used plants

“…All of the four antihyperglycaemic studies were enzyme‐based assays investigating the inhibition of α‐amylase or α‐glucosidase, two of the major enzymes responsible for cleaving simple sugars from starch and glycogen. Two of the studies reported moderate antihyperglycaemic activity (Sut et al, 2020; Tasnuva et al, 2019), while the other two studies found relatively high activity compared to the positive control used (Kerbab et al, 2019; Quispe et al, 2017). Inhibition activity against α‐amylase and α‐glucosidase is not necessarily correlated, with Kerbab et al (2019) reporting trans ‐tiliroside as a potent inhibitor of α‐amylase, but not of α‐glucosidase.…”

“…Two of the studies reported moderate antihyperglycaemic activity (Sut et al, 2020;Tasnuva et al, 2019), while the other two studies found relatively high activity compared to the positive control used (Kerbab et al, 2019;Quispe et al, 2017). Inhibition activity against α-amylase and α-glucosidase is not necessarily correlated, with Kerbab et al (2019) reporting trans-tiliroside as a potent inhibitor of α-amylase, but not of α-glucosidase. Similarly, Quispe et al (2017) found kaempferol 3-O-glucuronide to strongly inhibit aldose reductase but not α-glucosidase.…”

Study on Ajuga reptans Extract: A Natural Antioxidant in Microencapsulated Powder Form as an Active Ingredient for Nutraceutical or Pharmaceutical Purposes

“…A375, HeLa, and A549 were plated on multiwell plates, and serial dilutions of AJ (200−100−50 µg/mL), compounds (75−50−25 µg/mL), AJEP 3 microparticles (0.5−1.0−1.5 mg/mL) were added for one hour, and then co-exposed to lipopolysaccharide (LPS), from Escherichia coli , (0.1 µg/mL) for 24 h in order to evaluate the antioxidant activity of extract (AJ), isolated compounds ( 1 – 6 ), and AJEP 3 microparticles [ 32 ].…”

“…The antioxidant activity of AJ, compounds, and AJEP 3 microparticles was investigated using a cytofluorimetric assay, 2′–7′-dichlorofluorescein diacetate (H 2 DCF-DA), usually adopted to evaluate the intracellular production of peroxides [ 32 ]. H 2 DCF-DA is a non-polar molecule that easily diffuses inside cells and it is hydrolysed by intracellular esterases that remove the acetate groups making it polar and therefore impermeable.…”

“…After 45 min. of incubation, cells’ fluorescence was rated using a fluorescence-activated cell sorting and analyzed with Cell Quest software [ 32 ]. The results are reported by mean fluorescence intensity.…”