Quercetin is a natural flavonol antioxidant found in various plant sources and food samples. It is well known for its notable curative effects on the treatment of ophthalmic diseases due to various biological activities, such as antioxidant, anti-inflammatory, and anti-fibrosis activities. This review will discuss the latest developments in therapeutic quercetin for the treatment of keratoconus, Graves' orbitopathy, ocular surface, cataracts, glaucoma, retinoblastoma, and other retinal diseases.
Metabolic related diseases such as cancer, diabetes mellitus and atherosclerosis are major challenges for human health and safety worldwide due to their associations with high morbidity and mortality. It is of great significance to develop the effective active pharmaceutical ingredient (API) delivery systems for treatment of metabolic diseases. With their unique merits like easy preparation, high adjustability, low toxicity, low cost, satisfactory stability and biodegradation, deep eutectic solvents (DESs) are unarguably green and sustainable API delivery systems that have been developed to improve drug solubility and treat metabolic related diseases including cancer, diabetes mellitus and atherosclerosis. Many reports about DESs as API delivery systems in the therapy of cancer, diabetes mellitus and atherosclerosis exist but no systematic overview of these results is available, which motivated the current work.
Corneal wound healing is a highly regulated biological process that is of importance for reducing the risk of blinding corneal infections and inflammations. Traditional eye drop was the main approach for promoting corneal wound healing. However, its low bioavailability required a high therapeutic concentration, which can lead to ocular or even systemic side effects. To develop a safe and effective method for treating corneal injury, we fabricated rutin-encapsulated gelatin hydrogel/contact lens composites by dual crosslinking reactions including in situ free radical polymerization and carboxymethyl cellulose/N-hydroxysulfosuccinimide crosslinking. In vitro drug release results evidenced that rutin in the composites could be sustainedly released for up to 14 days. In addition, biocompatibility assay indicated nontoxicity of the composites. Finally, the effect of rutin-encapsulated composites on the healing of the corneal injury in rabbits was investigated. The injury was basically cured in corneas using rutin-encapsulated composites (healing rate, 98.3% ± 0.7%) at 48 h post-operation, while the damage was still present in corneas using the composite (healing rate, 87.0% ± 4.5%). Further proteomics analysis revealed that corneal wound healing may be promoted by the ERK/MAPK and PI3K/AKT signal pathways. These results inform a potential intervention strategy to facilitate corneal wound healing in humans.
Chaenomeles speciosa (Sweet) Nakai is a medicinal plant. Until date, there are no studies focusing on comparing the chemical profiles, antioxidant activity and α-glucosidase inhibitory activity of the dried fruits of C. speciosa from different production regions. In the study, we investigated the chemical components of dried fruits of C. speciosa from Yunnan, Chongqing, Zhejiang and Anhui provinces in China in relation to the antioxidant activity and α-glucosidase inhibitory activity. C. speciosa from Yunnan had higher total flavonoid (47.92 ± 3.79 mg/g), total polyphenol (29.15 ± 0.29 mg/g) and polysaccharide (27.60 ± 1.56 mg/g) contents than plants from other production areas. Samples from Yunnan, Zhejiang and Anhui (all > 3200 mg/kg) had higher free amino acid contents than those from Chongqing (2286.66 mg/kg). Oleanolic acid and ursolic acid levels were highest in samples from Zhejiang (555.98 ± 20.88 μg/g) and Anhui (321.06 ± 14.64 μg/g), respectively. C. speciosa from Chongqing had low total flavonoid, total polyphenol, polysaccharide, free amino acid, oleanolic acid and ursolic acid contents but high levels of palmitic acid (12.04 ± 0.02 mg/g) and stearic acid (2.23 ± 0.08 mg/g). Among four production areas, Yunnan represented the highest antioxidant activity and α-glucosidase inhibitory activity. In addition, correlation analysis revealed that total flavonoid, total polyphenol, polysaccharide and ursolic acid were the major components responsible for the antioxidant activity of C. speciosa, while total flavonoid and polysaccharide were the main contributors for α-glucosidase inhibitory activity of the plant. These results would be helpful for evaluating the quality of C. speciosa in the different production areas.
Deep eutectic solvents (DESs) were used in combination with macroporous resins to isolate and purify flavonoids and 20-hydroxyecdysone from Chenopodium quinoa Willd by preparative high-performance liquid chromatography (HPLC). The extraction performances of six DESs and the adsorption/desorption performances of five resins (AB-8, D101, HPD 400, HPD 600, and NKA-9) were investigated using the total flavonoid and 20-hydroxyecdysone extraction yields as the evaluation criteria, and the best-performing DES (choline chloride/urea, DES-6) and macroporous resin (D101) were further employed for phytochemical extraction and DES removal, respectively. The purified extract was subjected to preparative HPLC, and the five collected fractions were purified in a successive round of preparative HPLC to isolate three flavonoids and 20-hydroxyecdysone, which were identified by spectroscopic techniques. The use of a DES in this study significantly facilitated the preparative-scale isolation and purification of polar phytochemicals from complex plant systems.
Corneal neovascularization is a serious corneal pathological change caused by various factors. The drug delivery system is of great significance for the effective treatment of corneal neovascularization. Herein, we developed and characterized a monolith/hydrogel composite as the triamcinolone acetonide (TA) carrier for curing corneal neovascularization. The composite was prepared by photo-initiated free radical polymerization of multi-methacrylate substituted dodecamine organic molecular cage and post-modified by the sequential photo-initiated free radical polymerization of acrylated gelatin. The globular morphology and structural property of as-prepared composites were evaluated by scanning electron microscopy, Fourier-transform infrared spectroscopy and solid-state cross polarization magic angle spinning carbon-13 nuclear magnetic resonance. Then swelling ratio and the TA loading capacity were investigated then. Compared with gelatin hydrogel, the composites exhibited a decreased swelling ratio and an improved loading capacity. With good biocompatibility, the composite can sustainedly release TA for up to 28 days, and effectively inhibit corneal neovascularization with an alkali burn-induced corneal neovascularization model. Additionally, tandem mass tags-labeled quantitative proteomics were performed to identify differentially expressed proteins between vascularized and devascularized corneas. The Kyoto Encyclopedia of Genes and Genomes enrichment analysis revealed that the inhibition process could be primarily linked to the fibrinolytic system. These results demonstrated the potential of monolith/hydrogel composites as delivery systems in the therapy for biomedical diseases.