BACKGROUND: Allergic conjunctivitis is one of the most common eye disorders. Different drugs are used for its treatment. Hesperidin is an active substance isolated from Citrus sinensis L. (Rutaceae) fruit peels, with known anti‐inflammatory activity but low solubility. It was complexed with cyclodextrin and encapsulated in situ gel to extend its duration in the eye.RESULTS: The optimized formulation comprised 1% hesperidin, 1.5% hydroxyethyl cellulose, and 16% poloxamer 407. The viscosity at 25 °C was 492 ± 82 cP, and at 35 °C it was 8875 ± 248 cP, the pH was 7.01 ± 0.03, gelation temperature was 34 ± 1.3 °C, and gelation time was 33 ± 1.2 s. There was a 66% in vitro release in the initial 2 h, with a burst effect. A lipoxygenase (LOX) inhibition test determined that hesperidin was active at high doses on leukotyrens seen in the body in allergic diseases. In cell‐culture studies, the hesperidin cyclodextrin complex loaded in situ gel, BRN9‐CD (poloxamer 16%, hydroxy ethyl cellulose (HEC) 1.5%), enhanced cell viability in comparison with the hesperidin solution. It was determined that BRN9‐CD did not cause any irritation in the ocular tissues in the Draize test.CONCLUSION: The findings of this study demonstrate the potential of the in situ gel formulation of hesperidin in terms of ease of application and residence time on the ocular surface. Due to its notable LOX inhibition activity and positive outcomes in the in vivo Draize test, it appears promising for incorporation into pharmaceutical formulations. © 2024 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

The present investigation focused on the comprehensive analysis of the phenolic profile of Centaurea glastifolia L. (Asteraceae) and the assessment of its diverse biological activities. Utilising LC-MS/MS, the phytochemical composition of the 70% methanol extract of Centaurea glastifolia (CG-ME) was thoroughly elucidated, revealing the presence of 30 distinct phytochemical compounds. Notably, major phenolic constituents identified in the extract included quinic acid, chlorogenic acid, luteolin-7-O-glucoside, kaempferol-3-O-glucoside, luteolin, and apigenin-7-O-glucoside. The antioxidant, antibacterial, antiproliferative, and cytotoxic activities of CG-ME were investigated. The CG-ME exhibited a moderate capacity for scavenging DPPH radicals (IC₅₀: 50.05 ± 1.58 µg/mL) and FRAP (63.96 ± 0.39 mg TE/g extract), indicating a moderate level of antioxidant activity. Moreover, CG-ME demonstrated significant antiproliferative effects (GI₅₀: 1.10 and 1.30 µg/mL) on cancer cells (C6 and HTC cancer cell lines, respectively) while displaying low cytotoxicity towards normal cells (LC₅₀: >1000 µg/mL). In terms of antibacterial activity, CG-ME was found to be inactive against tested both Gram-positive and Gram-negative bacterial strains (MIC > 500 µg/mL). The extracts had a promising antiproliferative effect on C6, HeLa, and HT29 cancer cell lines with a less cytotoxic effect (10.5-14.2%) against normal cells.

Eleven coumarins named osthole (1), imperatorin (2), bergapten (3), prantschimgin (4), grandivitinol (5), suberosin (6), xanthotoxin (7), felamidin (8), marmesin (9), umbelliferone (10), ulopterol (11), and a sterol mixture consisted of stigmasterol (12), β-sitosterol (13) were isolated from the roots of Ferulago blancheana, F. pachyloba and F. trachycarpa through in vitro bioassay-guided fractionation processes. The extracts and bioactive compounds were evaluated for their α-amylase and α-glucosidase activities. Among the tested compounds, felamidin and suberosin showed significant α-glucosidase inhibitory activity with IC50 values of 0.4 and 0.9 mg/mL, respectively, when compared to the reference standard acarbose (IC50 = 4.9 mg/mL). Grandivitinol (IC50 = 20.0 mg/mL) had the lowest inhibitory effect. On the other hand, none of the tested extracts were found to be active on α-amylase inhibition. This is the first report on isolation, characterization of the bioactive compounds and evaluation the α-amylase and α-glucosidase inhibitory activities of these species. Video Clip of Methodology: 8 min 26 sec: Click to watch

The study aimed to comprehensively identify the phenolic fingerprint of Morina persica L. (Caprifoliaceae) and evaluate its various biological activities. LC-MS/MS analysis of 70% Morina persica methanol extract revealed the presence of 27 phytochemicals, with quinic acid, chlorogenic acid, and rutin being the major phenolics. The antioxidant, antibacterial, antiproliferative, and cytotoxic activities were evaluated for biological screening. The results showed that the methanolic extract of M. persica has a moderate DPPH radical scavenging and ferric-reducing capacity, indicating antioxidant activity. M. persica was observed to have a sufficient antiproliferative effect against cancer cells and low cytotoxicity against normal cells. Moreover, M. persica demonstrated good antibacterial activity against Clostridium perfringens, Enterococcus faecalis, and Escherichia coli. These data suggest that the methanolic extract of M. persica could be considered both an industrial source of quinic acid and a potential biologically active ingredient for developing drug formulations.