Search Results (29)

Background/Objectives: Imipenem, known as a carbapenem, is widely used in combination with Cilastatin to treat severe bacterial infections. Imipenem is a β-lactam antibiotic with potent antibacterial activity but a relatively unstable chemical structure. Due to these structural characteristics, it may degrade or undergo structural changes over time in aqueous solutions. Methods: In this study, Imipenem was investigated for its structural stability over time in aqueous solution at 37 °C. Structural changes in the Imipenem/Cilastatin solution were confirmed by HPLC-DAD at the maximum absorbance wavelength. Results: Imipenem undergone progressive degradation and structural transformation for the dimerization, while Cilastatin remained stable under the same conditions. LC-Q-TOF/MS confirmed the formation of a dimeric Imipenem species after prolonged incubation. Antibacterial activity showed that Imipenem was effective against P. carotovorum regardless of the dissolution times. However, Imipenem solution after 24 h with chemical degradation exhibited significantly decreased effects against E. coli and P. aeruginosa. Conclusions: Accordingly, the patterns of metabolite changes in Imipenem and Cilastatin were characterized according to concentration and dissolution time, and the corresponding antibacterial activities against different bacterial strains were compared. Full article

This study is the first to demonstrate fluctuations in major phenolics and biofunctional properties under various extraction conditions of Korean winter spinach (Allseason cultivar) leaves. In contrast to earlier reports on summer- or greenhouse-cultivated spinach, which mainly relied on HPLC-DAD or LC-MS profiling and one or two bioactivity assays, the present work combines UPLC-Q-TOF-MS/MS with NMR-based structural confirmation of three major flavone glucuronides (11–13) and integrates five complementary bioactivity assays (DPPH, ABTS, FRAP, DNA protection, and tyrosinase inhibition) within a single optimization framework. A 50% methanol extract yielded twelve phenolics (patuletin, spinacetin, spinatoside, jaceidin, and methylenedioxyflavone-glucuronide derivatives) elucidated by UPLC-Q-TOF-MS/MS, with the isolated major phenolics 11–13 further verified by NMR. Total phenols and total flavonoids of biofunctional characteristics varied significantly depending on the solvent system. The optimal extraction conditions (50% methanol, 72 h, 35 °C) resulted in the highest phenolic levels of phenolics 11–13 (total: ~6.5 mg/g) and bioactivities (DNA protection > ABTS > tyrosinase inhibition > FRAP > DPPH, at 500 μg/mL). PCA and hierarchical clustering distinguished extraction profiles, with 50–70% methanol extracts forming clear clusters. Among the isolated phenolics, phenolic 12 showed the strongest antioxidant activity (DPPH IC₅₀ = 57.6 μM; ABTS IC₅₀ = 21.9 μM). These findings suggest that spinach leaves are a valuable source of bioactive phenolics for nutraceutical applications under optimized extraction conditions. Full article

Background: Crataegus almaatensis, an endemic hawthorn species from Kazakhstan, is known for its rich content of phenolic compounds and flavonoids with significant pharmacological potential. This study aimed to optimize and compare conventional solid–liquid extraction (SLE) and ultrasound-assisted extraction (UAE) processes for maximizing the extractability of bioactive compounds from hawthorn leaves powder. Methods: The effects of temperature, extraction time, ethanol concentration, and solid-to-liquid ratio (or ultrasound power in the case of UAE) on total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity (FRAP, DPPH, and ABTS assays) were systematically evaluated. Results: The UAE method yielded higher concentrations of TPC and TFC, with up to 16% improvement in TPC and reduced ethanol usage (40% (v/v)) compared to SLE (75% (v/v)), demonstrating its efficiency and sustainability. Optimal extraction conditions were identified as 70 °C, 75% ethanol, 34 min, and an S/L ratio of 0.05 g/mL for SLE, 70 °C, 40% ethanol, 44 min, and 100 W US power for UAE. High-resolution HPLC-DAD and LC-Q/TOF-MS analyses confirmed the presence of key phenolic acids and flavonoid glycosides, including chlorogenic acid and apigenin-8-C-glucoside-2′-rhamnoside as the most abundant compounds identified. Conclusions: These findings validate UAE as an innovative, eco-friendly method for extracting bioactive compounds from hawthorn leaves and highlight its potential for developing natural antioxidants for pharmaceutical and nutraceutical applications. Full article

Chronic alcohol consumption is a major contributor to gastric injury, yet current therapeutic strategies predominantly rely on chemical agents with limited efficacy and potential side effects. Natural products, with their multi-target biocompatibility and safety advantages, offer promising alternatives for gastric protection. We examined the phenolic compounds of Elaeagnus angustifolia honey (EAH) and investigated its prophylactic potential against ethanol-induced chronic gastric injury in mice. HPLC-DAD-Q-TOF-MS analysis showed that 21 phenolic compounds were tentatively and qualitatively identified in EAH, as well as 14 phenolic compounds. Moreover, gastric ulcer indices, histopathological morphology, oxidative stress markers (MDA, GSH, SOD), inflammatory mediators (NO, PGE2), and cytokine gene expression (TNF-α, IL-6, IL-1β, iNOS) were evaluated via enzyme-linked immunosorbent assay (ELISA) and quantitative real-time PCR. Western blot was employed to assess COX-2 protein expression, while 16^S rRNA sequencing analyzed gut microbiota composition. The results demonstrated that EAH could play a role in gastric injury caused by long-term alcoholism by protecting gastric tissue structure, interfering with oxidative stress and inflammatory response, and remodeling the intestinal microbial community. Full article

The yeast Lachancea thermotolerans has the ability to produce notable amounts of lactic acid and reduce alcoholic strength in fermentation, so it has a considerable potential for mitigating negative impacts of climate changes in winemaking. In this study, a treatment with L. thermotolerans and Saccharomyces cerevisiae in sequential inoculation was compared to a control S. cerevisiae monoculture fermentation of Malvazija istarska (aka Malvasia Istriana) white grape must. Standard physico-chemical parameters of the obtained wines were determined by the OIV methods. Targeted (GC/FID and GC/MS) and untargeted (GC×GC/TOF-MS) gas chromatographic techniques were combined for the analysis of volatile compounds. Phenolic compounds were analyzed by UPLC/QqQ-MS/MS, and proteins by RP-HPLC-DAD, while a sensory analysis of wines was performed by a panel of trained and certified tasters. L. thermotolerans co-fermentation treatment increased the concentration of lactic acid and decreased alcoholic strength. L. thermotolerans increased the concentrations of geraniol, β-ionone, isobutanol, isobutyric acid, ethyl isobutyrate, several major acetates, ethyl lactate, and diethyl succinate, followed by many minor compounds. This wine also contained more hydroxycinnamoyl tartrates, while control S. cerevisiae wine had higher levels of free hydroxycinnamates. The effects on PR proteins were minor. L. thermotolerans co-fermentation slightly enhanced the sensory perception of tropical fruit, herbaceous, tobacco, and buttery odor notes, as well as fullness of body. With the largest number of identified volatile compounds up to date and other results obtained, this study contributes to the better understanding of oenological and especially aromatic potential of L. thermotolerans in white wine production. Full article

This study investigated the neuroprotective effect of 70% ethanol extract of Ecklonia cava (EE) in amyloid beta (Aβ)-induced cognitive deficit mice. As a result of analyzing the bioactive compounds in EE, nine compounds were identified using ultra-performance liquid chromatography–quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). In particular, the diekcol content was quantified by high-performance liquid chromatography with diode-array detection (DAD-HPLC). Biochemical analysis was performed on brain tissue to determine the mechanism of the cognitive function improvement effect of EE. The result showed that EE ameliorated learning and memory decline in behavioral tests on Aβ-induced mice. EE also attenuated oxidative stress by regulating malondialdehyde (MDA) content, reduced glutathione (GSH), and superoxide dismutase (SOD) levels. Similarly, EE also improved mitochondrial dysfunction as mitochondrial membrane potential, ATP production, and reactive oxygen species (ROS) levels. In addition, EE enhanced synapse function by modulating acetylcholine-related enzymes and synaptic structural proteins in the whole brain, hippocampus, and cerebral cortex tissues. Also, EE regulated Aβ-induced apoptosis and inflammation through the c-Jun N-terminal kinase (JNK) and nuclear factor-kappa B (NF-κB) signaling pathways. Furthermore, EE protected neurotoxicity by increasing brain-derived neurotrophic factor (BDNF) production. These results suggest that EE may be used as a dietary supplement for the prevention and treatment of Alzheimer’s disease (AD). Full article

Spinach (Spinacia oleracea) is one of the most famous vegetables worldwide, rich in essential metabolites for various health benefits. It is a valuable plant source that has the potential to be a nutraceutical. This study aimed to evaluate the single characteristic marker compound to establish the validation of HPLC-DAD methods applied to the development of a nutraceutical using spinach samples. Six metabolites (1–6) were identified from the spinach samples such as freeze-dried spinach (FDS) and spinach extract concentrate (SEC) by LC-Q-TOF/MS analysis. Among the six metabolites, 3′,4′,5-trihydroxy-3-methoxy-6,7-methylenedioxyflavone 4′-glucuronide (TMG) was selected as a marker compound due to its highest abundance and high selectivity. The specificity, accuracy, linearity, precision, repeatability, limit of detection (LOD), and limit of quantification (LOQ) of TMG in the spinach samples (FDS and SEC) were validated according to AOAC international guideline. The specificity was confirmed by monitoring the well separation of the marker compound from other compounds of spinach samples in the base peak intensity (BPI) and ultraviolet (UV) chromatogram. The calibration curve of TMG (15.625~500 μg/mL) had reasonable linearity (R² = 0.999) considered with LOD and LOQ values, respectively. Recovery rate of TMG was 93–101% for FDS and 90–95% for SEC. The precision was less than 3 and 6% in the intraday and interday. As a result, the HPLC-DAD validation method of TMG in the spinach samples (FDS and SEC) was first established with AOAC and KFDA regulations for approving functional ingredients in functional foods. Full article

In this study, eleven kinds of flavonoids were identified from F. tataricum bran (FTB) by UPLC-Q-TOF-MS, and HPLC-DAD analysis revealed that four compounds, including rutin, quercetin, kaempferol, and nicotiflorin, were the most significant components. Subsequently, natural deep eutectic solvent-based ultrasound-assisted extraction (NADES-UAE) was employed to extract flavonoids from FTB. Among the six kinds of NADES prepared, choline chloride–ethylene glycol (ChCl-EG) was identified as a promising candidate for extracting flavonoids due to its superior extraction performance. The extraction conditions were statistically investigated using response surface methodology conducted by Box-Behnken design (BBD). The optimal operational conditions were as follows: ultrasonic time 268 s, ultrasonic temperature 76 °C, and liquid–solid ratio 43 mL/g, which resulted in a high total flavonoid yield of 40.29 mg/g. Afterwards, the efficient extraction mechanism of NADES-UAE was comprehensively explored through FT-IR spectra, COSMO model, and microstructural analysis. In conclusion, NADES-UAE extraction is considered a green, efficient, and sustainable method for FTB flavonoids. Full article

As a traditional Chinese medicinal herb, ginseng (Panax ginseng C. A. Mey.) is commonly used to treat common diseases, for example, esophageal cancer and myasthenia gravis. Furthermore, ginseng is also processed into a functional food additive that is utilized to improve the freshness of chicken soup and make health wine. Unfortunately, ginseng (Panax ginseng C. A. Mey.) has already shown a noticeable bitterness during its application process. In this research, the bitter substances in ginseng (Panax ginseng C. A. Mey.) after two common preparation processes (water extraction and ethanol extraction) were separated, purified and identified by preparative high performance liquid chromatography (prep-HPLC), high performance liquid chromatography with diode array detector (HPLC-DAD), ultra-performance liquid chromatography coupled with high-resolution quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) and an electronic tongue. The results indicated that compared with the other four bitter compounds, the ginsenoside Rb1 had the highest bitterness value, followed by 20(S)-ginsenoside Rg2, ginsenoside Rg1, ginsenoside Rf and ginsenoside Rb3. Upon the evaluation of results to reduce the bitterness of ginseng extract, we found that the composite embedding system of chitosan adsorption in the ginseng carrageenan gel microsphere (K/M_C/M_CG) could effectively reduce the bitterness. Full article

FLH 13-11 is an F1 interspecific hybrid muscadine grape genotype that was developed to produce new anthocyanins for pigment color stability. This hybrid resulted from a cross between ‘Marsh’ (Vitis munsoniana) and ‘Magoon’ (V. rotundifolia) and has been cultivated for the wine and juice industry. This report characterizes anthocyanins produced in fully ripe berries and reveals a significant difference in total anthocyanin contents from two continuous cropping seasons. High-performance liquid chromatography with a diode array detector (HPLC-DAD) and HPLC–quadrupole time-of-flight tandem mass spectrometry (HPLC-qTOF-MS/MS) were used to profile anthocyanins in berries. The resulting data showed that fourteen anthocyanins were detected, six from 2011 and nine from 2012, with only one produced in both seasons. However, the anthocyanidin profiles of the berries were the same. Five anthocyanins were annotated as diglucosides of anthocyanidins based on MS/MS features, including delphinidin 3,5-diglucoside produced in both seasons, cyanidin 3,5-diglucoside mainly formed in 2011, petunidin 3,5-diglucoside, malvidin 3,5-diglucoside, and peonidin 3,5-glucoside only detected in 2012. Also, three anthocyanidin-diglucoside-like anthocyanins and three monoglucosides, including peonidin 3-glucoside, delphinidin 3-glucoside like, and pelargonidin 3-glucoside-like anthocyanins, were detected in 2011 and 2012, respectively. These results indicate that FLH 13-11 can produce both anthocyanidin-diglucosides and -monoglucosides, and their biosynthesis is closely dependent on cropping years. Full article

In this study, Asparagus stipularis was characterized concerning its phytochemical composition, antioxidant potential, cytotoxicity, and pancreatic lipase inhibitory activities. Twenty-seven compounds were identified and quantified by HPLC-DAD-MS in the leaf, stem, pericarp, and rhizome of ethanolic extracts. Seven steroidal saponins were detected, and the highest content was quantified in rhizome and pericap. A. stipularis also contained significant amounts of flavonoids in the aerial part. Isorhamnetin tetra-glycoside, quercetin-3-glucosyl-rutinoside, and rutin were the main flavonoid derivatives in leaf, stem, and pericarp extracts, respectively. In addition, eleven phenolic acids were also detected; among them, caffeic acid, protocatechuic acid, p-hydroxybenzoic acid, and ferulic acid were the predominant phenolics, with these having the highest amounts quantified in the rhizome extracts. All the tested extracts possessed antioxidant capacities, with pericarp and rhizome extracts exhibiting the highest activity in DPPH, ABTS, and FRAP assays. The extracts from pericarp and rhizome were revealed to also be the strongest inhibitors of pancreatic lipase. The rhizome extracts exhibited potent cytotoxic activity against HCT-116 and HepG2 with IC50 values of 30 and 54 µg/mL after 48 h of treatment. The present study demonstrated that A. stipularis can be used as a new source of natural antioxidants and potential anticancer and antiobesity compounds. Full article

Increasing prospective phytochemical investigations and biological activities on Pueraria lobata and Trifolium pratense flowers exhibited their nutritional (food industry) pharmaceutical (anticancer, anti-inflammatory, anti-microbial, etc.) potentials. Previous studies paid great attention to the screening of isoflavones profile from phytochemicals. This study, in contrast, aimed at identifying the flavonoids from Pueraria lobata flowers or kudzu flower (KF) and Trifolium pratense flowers or red clover (RC) flowers and determining their cytotoxic activities on normal; (HEK-293) and cancer cell lines; human glioblastoma (A-172), osteosarcoma (HOS), embryonic rhabdomyosarcoma (Rd), lung carcinoma (A-549) and liver carcinoma (HepG2). The phytochemical screening using a high-performance liquid chromatography-diode array detector coupled with quadrupole time-of-flight mass spectrometry (HPLC-DAD-Q-TOF/MS) showed that 15 flavonoids, including isoflavones, flavones, flavonols, and flavanones, were identified in KF and 8 flavonoids, including isoflavones and flavonols, were found in RC. Nevertheless, the majority of flavonoid chemical constituents in KF or RC were found to be isoflavones (66.6%) and (62.5%), respectively. HPLC-DAD analysis following eco-friendly extraction of phytochemicals showed that KF contains mainly daidzein and genistein, while RC contains primarily formononetin and biochanin A. Cytotoxic activities evaluated according to IC₅₀ values exhibited the most pronounced dose-dependent antiproliferative effect of KF and RC extracts were against HOS and Rd cancer cell lines, respectively. Accordingly, the morphological observation carried out using acridine orange/ethidium bromide and Giemsa stains revealed apoptotic activities and cell death in HOS and Rd cell lines when subjected to KF or RC extracts. Cytotoxic activities and apoptotic changes were pronounced among all cancer cell lines except for the control cells (HEK-293). Additionally, various polyphenols and flavonoids were identified and quantified in KF and RC extracts and exhibited potent radical scavenging activities. Overall, this study suggests that KF and RC could be valuable edible sources of flavonoids. The comprehensive flavonoid profiles for KF and RC may explain their remarkable biological activities and contribution to inducing antioxidant and cytotoxic activities against cancer cell lines. Full article

Strawberry leaves are considered a valuable waste material; so far, mainly due to their antioxidant properties. Since the annual production of this crop is high, our study aimed to thoroughly examine the chemical composition and antidiabetes-related bioactivity of Fragaria × ananassa leaf of its popular and productive cultivar Senga Sengana. Leaves from three different seasons, collected after fruiting, were extensively analyzed (UHPLC-qTOF-MS/MS, HPLC-DAD). Some individual components were isolated and quantified, including specific flavonol diglycosides (e.g., 3-O-[β-xylosyl(1‴→2″)]-β-glucuronosides). The separated quercetin glycosides were tested in an antiglycation assay, and their methylglyoxal uptake capacity was measured. In addition, the biodegradable polyester precursor 2-pyrone-4,6-dicarboxylic acid (PDC) was confirmed at relatively high levels, providing further opportunity for strawberry leaf utilization. We want to bring to the attention of the food, pharmaceutical, and cosmetic industries the Senga Sengana strawberry leaf as a new botanical raw material. It is rich in PDC, ellagitannins, and flavonols—potent glycation inhibitors. Full article

The pervasiveness of oral bacterial infections in diabetic patients is a serious health concern that may produce severe complications. We investigated 26 Ayurvedic medicinal plants traditionally used for treatment of the oral bacterial infections with the aim to look for new promising drug leads that can be further employed for herbal formulation design. The plants were grouped into three categories based on traditional usage. All plant extracts were examined for antibacterial, antibiofilm and antiquorum-sensing properties. The plants with significant activities including Juglans regia, Syzygium aromaticum, Eruca sativa, Myristica fragrans, Punica granatum and Azadirachta indica were further analyzed using HPLC-DAD-QToF and GC-MS. In silico and in vitro activity was evaluated for selected constituents. Finally, it could be concluded that eugenol and 2-phenylethylisothiocyanate are major contributors towards inhibition of bacterial biofilms and quorum sensing. Full article

In this study, an overall survey regarding the determination of several bioactive compounds in olive fruit is presented. Two methodologies were developed, one UPLC-Q-TOF-MS method for the determination of olive fruit phenolic compounds and one HPLC-DAD methodology targeting the determination of pigments (chlorophylls and carotenoids), tocopherols (α-, β, -γ, δ-) and squalene. Target and suspect screening workflows were developed for the thorough fingerprinting of the phenolic fraction of olives. Both methods were validated, presenting excellent performance characteristics, and can be used as reliable tools for the monitoring of bioactive compounds in olive fruit samples. The developed methodologies were utilized to chemical characterize the fruits of the Kolovi olive variety, originating from the island of Lesvos, North Aegean Region, Greece. Twenty-five phenolic compounds were identified and quantified in Kolovi olives with verbascoside, hydroxytyrosol, oleacein and oleomissional found in significantly high concentrations. Moreover, 12 new bioactive compounds were identified in the samples using an in-house suspect database. The results of pigments analysis suggested that Kolovi variety should be characterized as low pigmentation, while the tocopherol and squalene content was relatively high compared to other olive varieties. The characterization of Kolovi olive bioactive content highlighted the high nutritional and possible economic value of the Kolovi olive fruit. Full article