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ABSTRACT This study investigated the effect of different processing methods (boiling, oil boiling, and stir frying) on the flavor of hoki steak soups. The quality of different fillet broths was explored by pH, Thiobarbituric acid reactive substances (TBARS), and color. E‐nose, E‐tongue, and gas chromatography‐ion mobility spectrometry (GC‐IMS) combined with free amino acids (FAAs) were used to analyze the flavor of hoki steak soups. Key compounds were screened by relative odor activity value (ROAV). The variable influence on projection (VIP) was used to identify the differential compounds. The E‐nose and E‐tongue were able to distinguish hoki steak soups. A total of 47 volatile compounds were characterized by GC‐IMS. n‐Pentanal (M) was the key component for the difference between hoki steak soups. There were six substances with ROAV ≥ 1. The results showed that the hoki steak soup boiled for 2 h in the stir‐frying group had a lower fishy odor. [ABSTRACT FROM AUTHOR]

Quercetin, a flavonoid compound rich in hydroxyl groups, possesses antioxidant properties, whereas its poor water solubility limits its bioavailability. In pursuit of addressing the water solubility of quercetin and comprehending the impact of nanocrystal particle size on antioxidant efficacy, we prepared three different-sized quercetin nanocrystals, namely small (50 nm), medium (140 nm), and large (360 nm), using a nanosuspension method in this study. Within the in vitro setting, assessments employing solubility and radical scavenging assays revealed that quercetin nanocrystals displayed superior solubility (26, 21, and 13 fold corresponding to small, medium, and large particle sizes) and antioxidant performance compared to the coarse quercetin. Furthermore, quercetin nanocrystals of three particle sizes all demonstrated significant protection effects on the survival rate of H2O2-treated zebrafish at 72 h (77.78%, 73.33%, and 66.67% for small, medium, and large particle sizes, respectively), while the coarse quercetin group exhibited a low survival rate (53.3%) similar to the H2O2-treated group (47.8%). Moreover, all quercetin nanocrystals exhibited potent antioxidant capacity on both the antioxidants and enzymatic antioxidant system in H2O2-treated zebrafish to restore zebrafish to a normal state under oxidative stress. For instance, the levels of reactive oxygen species were reduced to 101.10%, 108.83%, and 109.77% of the normal levels for small, medium, and large particle-sized quercetin nanocrystals, respectively. In conclusion, quercetin nanocrystals demonstrated enhanced solubility, robust antioxidant capacity, and protective effects in zebrafish compared to coarse quercetin. [ABSTRACT FROM AUTHOR]

Hyaluronidase is clinically used in treating many skin diseases due to its good permeability-promoting effect, which may motivate the diffusion and absorption of drugs. To verify the penetration osmotic effect of hyaluronidase in microneedles, 55 nm-size curcumin nanocrystals were fabricated and loaded into microneedles containing hyaluronidase in the tip. Microneedles with bullet shape and backing layer of 20% PVA + 20% PVP K30 (w/v) showed excellent performance. The microneedles were able to pierce the skin effectively with a skin insert rate of 90% and demonstrated good mechanical strength. In the in vitro permeation assay, with the increase of hyaluronidase concentration at the tip of the needle, the cumulative release of curcumin increased, as well as the skin retention decreased. In addition, compared with the microneedles without hyaluronidase, the microneedles containing hyaluronidase in the tip exhibited a larger drug diffusion area and deeper diffusion depth. In conclusion, hyaluronidase could effectively promote the transdermal diffusion and absorption of the drug. [ABSTRACT FROM AUTHOR]

Propolis is resinous natural product produced by Western honeybees using beeswax and plant and bud exudates, which has a wide range of biological activities, including antioxidation, antibacterial, anti-inflammation, immune regulation, antitumor, and so on. Diffuse large B-cell lymphoma (DLBCL) is an aggressive cancer, and accounts for about 30% of all lymphomas. The effect of poplar propolis on DLBCL has not been reported. The IC50 of propolis on the proliferation of DLBCL SU-DHL-2 cell line and its proteins and gene expressions were detected by CCK-8 kit, label-free proteomic, and RT-PCR. The results showed that the IC50 of propolis at the 5 × l05/mL cell for 24 h was 5.729 μg/mL. Label-free-based proteomics analysis showed that there were 115 differentially expressed proteins (61 up-regulated and 54 down-regulated proteins) between IC50 dose-treated and solvent control groups. There were 32.47% differential proteins located in the nucleus, 20.78% in the cytoplasm, and 14.29% in mitochondria. The most significant different pathway (p = 0.0016) of protein enrichment was ferroptosis (including glutamate–cysteine ligase regulatory subunit, ferritin, and heme oxygenase). The relative expression trend of 17 of the total 22 genes selected according to proteomics results was in line with their encoded protein. The highest protein–protein interaction was serine/threonine-protein kinase PLK, which interacted with 16 differential proteins. In conclusion, poplar propolis inhibited SU-DHL-2 cells via ferroptosis pathway, accelerating cell death and down-regulated serine/threonine-protein kinase PLK1, affecting apoptosis of cell. This result provides a theoretical basis for the treatment of DLBCL using propolis. [ABSTRACT FROM AUTHOR]

The present study comprehensively characterized the flavor differences between different varieties of douchis from different origins using headspace gas chromatography-ion mobility spectrometry (HS-GC-IMS) coupled with gas chromatography-olfactometry-quadrupole time-of-flight mass spectrometry (GC-O-QTOF/MS). A total of 91 volatile organic compounds (VOCs) were identified using HS-GC-IMS and 70 VOCs were identified using GC-O-QTOF/MS, mainly including acids, aldehydes, esters and alcohols. Additionally, 23 key aroma-presenting compounds were screened in five douchi species using relative odor activity value (ROAV) and the aroma compounds that contributed the most to the aroma varied among the five douchi species. Comparative analysis of the GC-IMS and GC-O-QTOF/ MS results yielded 13 VOCs that were detected by both techniques. Nonanal, hexanal, eucalyptol, 1-octen-3-ol, isoamyl acetate, and 2-pentylfuran were identified as key VOCs in the douchi species using both methods. These findings will provide deeper insights for exploring flavor differences in douchi from different geographic sources. • Characterization of VOCs of five douchi species by GC-IMS and GC-O-QTOF/MS. • 91 VOCs were identified by GC-IMS, 70 by GC-O-QTOF/MS. • Relative contents of acids and esters were high in five douchi species. • The key aroma compounds in five douchi species were completely different. [ABSTRACT FROM AUTHOR]

Melanin is a kind of dark insoluble pigment that can cause pigmentation and free-radical clearance, inducing melasma, freckles, and chloasma, affecting the quality of life of patients. Due to poor water solubility and low safety, the absorption of poorly water-soluble drugs is limited by the hinderance of a skin barrier. Therefore, it is necessary to develop new, safe, and highly efficient drugs to improve their transdermal absorption efficiency and thus to inhibit the production of melanin. To address these issues, we developed a new nicotinamide (NIC)-stabilized phloretin nanocrystals (PHL-NCs). First, NC technology significantly increased the solubility of PHL. The in vitro release results indicated that at 6 h, the dissolution of the PHL-NIC-NCs was 101.39% ± 2.40% and of the PHL-NCs was 84.92% ± 4.30%, while that of the physical mixture of the two drugs was only 64.43% ± 0.02%. Second, NIC acted not only as a stabilizer to enlarge the storage time of PHL-NIC-NCs (improved to 10-day in vitro stability) but also as a melanin transfer inhibitor to inhibit melanin production. Finally, we verified the melanin inhibition effect of PHL-NIC-NCs evaluated by the zebrafish model. It showed that 0.38 mM/L PHL-NIC-NCs have a lower tyrosinase activity at 62.97% ± 0.52% and have less melanin at 36.57% ± 0.44%. The inhibition effect of PHL-NCs and PHL-NIC-NCs was stronger compared to the positive control arbutin. In conclusion, the combination of NIC and PHL achieves better inhibition of tyrosinase and inhibition of melanin production through synergism. This will provide a direction to the subsequent development of melanin-inhibiting drugs and the combined use of pharmaceutical agents. [ABSTRACT FROM AUTHOR]

Efflux transporters distributed at the apical side of human intestinal epithelial cells actively transport drugs from the enterocytes to the intestinal lumen, which could lead to extremely poor absorption of drugs by oral administration. Typical intestinal efflux transporters involved in oral drug absorption process mainly include P-glycoprotein (P-gp), multidrug resistance proteins (MRPs) and breast cancer resistance protein (BCRP). Drug efflux is one of the most important factors resulting in poor absorption of oral drugs. Caco-2 monolayer and everted gut sac are sued to accurately measure drug efflux in vitro. To reverse intestinal drug efflux and improve absorption of oral drugs, a great deal of functional amphiphilic excipients and inhibitors with the function of suppressing efflux transporters activity are generalized in this review. In addition, different strategies of reducing intestinal drugs efflux such as silencing transporters and the application of excipients and inhibitors are introduced. Ultimately, various nano-formulations of improving oral drug absorption by inhibiting intestinal drug efflux are discussed. In conclusion, this review has significant reference for overcoming intestinal drug efflux and improving oral drug absorption. [ABSTRACT FROM AUTHOR]

Materials derived from natural plants and animals have great potential for transdermal drug delivery. Polysaccharides are widely derived from marine, herbal, and microbial sources. Compared with synthetic polymers, polysaccharides have the advantages of non-toxicity and biodegradability, ease of modification, biocompatibility, targeting, and antibacterial properties. Currently, polysaccharide-based transdermal drug delivery vehicles, such as hydrogel, film, microneedle (MN), and tissue scaffolds are being developed. The addition of polysaccharides allows these vehicles to exhibit better-swelling properties, mechanical strength, tensile strength, etc. Due to the stratum corneum's resistance, the transdermal drug delivery system cannot deliver drugs as efficiently as desired. The charge and hydration of polysaccharides allow them to react with the skin and promote drug penetration. In addition, polysaccharide-based nanotechnology enhances drug utilization efficiency. Various diseases are currently treated by polysaccharide-based transdermal drug delivery devices and exhibit promising futures. The most current knowledge on these excellent materials will be thoroughly discussed by reviewing polysaccharide-based transdermal drug delivery strategies. [ABSTRACT FROM AUTHOR]

Drug nanocrystals (NCs) with fascinating physicochemical properties have attracted great attention in drug delivery. High drug‐loading efficiency, great structural stability, steady dissolution, and long circulation time are a few examples of these properties, which makes drug NCs an excellent formulation for efficient cancer therapy. In the last two decades, there are a lot of hydrophobic or lipophilic drugs, such as paclitaxel (PTX), camptothecin (CPT), thymectacin, busulfan, cyclosporin A, 2‐devinyl‐2‐(1‐hexyloxyethyl) pyropheophorbide (HPPH), and so on, which have been formulated into drug NCs for cancer therapy. In this review, we summarized the recent advances in drug NCs‐based cancer treatment. So far, there are main three methods to synthesize drug NCs, including top‐down, bottom‐up, and combination methods. The characterization methods of drug NCs were also elaborated. Furthermore, the applications and mechanisms of drug NCs were introduced by their administration routes. At the end, we gave a brief conclusion and discussed the future perspectives of drug NCs in cancer therapy. This article is categorized under: Implantable Materials and Surgical Technologies > Nanomaterials and Implants Therapeutic Approaches and Drug Discovery > Nanomedicine for Oncologic Disease Nanotechnology Approaches to Biology > Nanoscale Systems in Biology [ABSTRACT FROM AUTHOR]

Microneedles are one promising penetration enhancement vehicle to overcome the stratum corneum skin barrier, which hampers the penetration of drug nanocrystals by transdermal delivery. In order to clarify the particle size effect of nanocrystals on transdermal delivery, 60 nm, 120 nm, and 480 nm curcumin nanocrystals were fabricated and incorporated into dissolving hyaluronic acid polysaccharide microneedles. The microneedles showed good mechanical strength with 1.4 N/needle, possessing the ability to insert into the skin. The passive permeation results showed that the smaller particle size of 60 nm curcumin nanocrystals diffused faster and deeper than the larger 120 nm and 480 nm curcumin nanocrystals with size-dependent diffusion behaviors. Thereafter, higher concentration gradients and overlap diffusional coronas also formed in the skin layers by the smaller-particle-size nanocrystals. Furthermore, the diffusion rate of the smaller particle size of curcumin nanocrystals to the hair follicle was also higher than that of the larger curcumin nanocrystals. In conclusion, the particle sizes of curcumin nanocrystals influenced the transdermal and transfollicular penetration in deeper skin layers [ABSTRACT FROM AUTHOR]

Propolis has a very complex composition, with antibacterial, anti-inflammatory and other properties. To determine the composition of ethanol extracts of Brazilian green propolis (EEP-B) and their protective effect on mouse aortic endothelial cells (MAECs), the chemical composition of EEP-B was analysed by UPLC/Q-TOF-MS/MS, and the protective effect of EEP-B on the proliferation of lipopolysaccharide (LPS)-induced MAECs was determined by Cell Counting Kit-8 (CCK-8) assays. The protein levels of inflammatory cytokines tumour necrosis factor-α (TNF-α) and interleukin- 6 (IL-6) were measured by enzyme-linked immunosorbent assay (ELISA), and ICAM-1, VCAM-1 and MCP-1 expressions were analysed by western blotting. The results showed that a total of 24 compounds belonging to cinnamic acids and flavonoids, including 3,5-diisopentenyl-4-hydroxycinnamic acid (artepillin C), kaempferide, 3-isoprenyl p-coumaric acid, pinocembrin and 4′-methoxy pinobanksin, were identified in EEP-B. Among them, a new component, suggested to be 5-isoprenyl caffeic acid p-coumaric acid ester, was reported for the first time. The LPS-induced levels of TNF-α, IL-6, ICAM-1, VCAM-1 and MCP-1 were downregulated in response to 5, 10 and 20 μg/mL EEP-B. This study revealed that EEP-B could reduce LPS-induced inflammatory reactions, improve cell survival, and protect MAECs by regulating ICAM-1, VCAM-1 and MCP-1 expression. These findings could provide a theoretical basis for MAEC treatment using EEP-B. [ABSTRACT FROM AUTHOR]

Background: Schisandra chinensis (Turcz.) Baill bee pollen extract (SCBPE) is often used as a functional food in China due to its good antioxidant property. However, its chemical compositions and effects on H9c2 cardiomyocytes against H2O2-induced cell injury still lacks of reports thus far. This study aimed to characterize the main components of SCBPE and investigate its protective effects against H2O2-induced H9c2 cardiomyocyte injury. Methods: The main components of SCBPE were analyzed via ultraperformance liquid chromatography–quadrupole time-of-flight tandem mass spectrometry (UPLC–QTOF MS/MS). The three main nucleosides in SCBPE were quantitatively analyzed via ultraperformance liquid chromatography–diode array detection. Furthermore, the potential mechanism by which SCBPE exerts protective effects against H2O2-induced H9c2 cardiomyocyte injury was explored for the first time via cell survival rate measurements; cell morphological observation; myocardial superoxide dismutase (SOD) activity and malondialdehyde (MDA) and glutathione (GSH) level determination; flow cytometry; and quantitative polymerase chain reaction. Results: Two carbohydrates, three nucleosides, and nine quinic acid nitrogen-containing derivatives in SCBPE were identified or tentatively characterized via UPLC–QTOF MS/MS. The nine quinic acid nitrogen-containing derivatives were first reported in bee pollen. The contents of uridine, guanosine, and adenosine were 2.4945 ± 0.0185, 0.1896 ± 0.0049, and 1.8418 ± 0.0157 μg/mg, respectively. Results of in vitro experiments showed that cell survival rate, myocardial SOD activity, and GSH level significantly increased and myocardial MDA level significantly decreased in SCBPE groups compared with those in H2O2 group. Cell morphology in SCBPE groups also markedly improved compared with that in H2O2 group. Results indicated that SCBPE protected H9c2 cardiomyocytes from H2O2-induced apoptosis by downregulating the mRNA expressions of Bax, cytochrome C, and caspase-3 and upregulating the Bcl-2 mRNA expression. Conclusions: This study is the first to report that SCBPE could protect against oxidative stress injury and apoptosis in H2O2-injured H9c2 cells. Results indicated that the nucleosides and quinic acid nitrogen-containing derivatives could be the main substances that exert protective effects against H2O2-induced H9c2 cardiomyocyte injury. [ABSTRACT FROM AUTHOR]

The chemical compositions of ethanol extracts of propolis from China (EEP-C) and the United States (EEP-A) and their antifungal activity against Penicillium notatum were determined. The result showed that a total of 49 compounds were detected by UPLC-Q-TOF-MS, 30 of which were present in samples from two regions. The major compounds of EEP-C and EEP-A were similar, including pinocembrin, pinobanksin-3-O-acetate, galanin, chrysin, pinobanksin, and pinobanksin-methyl ether, and both of them showed antifungal activity against P. notatum with same minimum inhibitory concentration (MIC) value of 0.8 mg·mL−1. In the presence of propolis, the mycelial growth was inhibited, the hyphae became shriveled and wrinkled, the extracellular conductivities were increased, and the activities of succinate dehydrogenase (SDH) and malate dehydrogenase (MDH) were decreased. In addition, iTRAQ-based quantitative proteomic analysis of P. notatum in response to propolis revealed that a total of 341 proteins were differentially expressed, of which 88 (25.8%) were upregulated and 253 (74.2%) were downregulated. Meanwhile, the differentially expressed proteins (DEPs) involved in energy production and conversion, carbohydrate transport and metabolism, and the sterol biosynthetic pathway were identified. This study revealed that propolis could affect respiration, interfere with energy metabolism, and influence steroid biosynthesis to inhibit the growth of P. notatum. [ABSTRACT FROM AUTHOR]

In the present work, we developed a simple and rapid sample preparation method for the determination of neonicotinoid pesticides in honey based on the matrix-induced sugaring-out. Since there is a high concentration of sugars in the honey matrix, the honey samples were mixed directly with acetonitrile (ACN)-water mixture to trigger the phase separation. Analytes were extracted into the upper ACN phase without additional phase separation agents and injected into the HPLC system for the analysis. Parameters of this matrix-induced sugaring-out method were systematically investigated. The optimal protocol involves 2 g honey mixed with 4 mL ACN-water mixture (v/v, 60:40). In addition, this simple sample preparation method was compared with two other ACN-water-based homogenous liquid-liquid extraction methods, including salting-out assisted liquid-liquid extraction and subzero-temperature assisted liquid-liquid extraction. The present method was fully validated, the obtained limits of detection (LODs) and limits of quantification (LOQs) were from 21 to 27 and 70 to 90 μg/kg, respectively. Average recoveries at three spiked levels were in the range of 91.49% to 97.73%. Precision expressed as relative standard deviations (RSDs) in the inter-day and intra-day analysis were all lower than 5%. Finally, the developed method was applied for the analysis of eight honey samples, results showed that none of the target neonicotinoid residues were detected. [ABSTRACT FROM AUTHOR]

Oxidative stress plays an important role in the pathogenesis of myocardial infarction (MI). Schisandra chinensis bee pollen extract (SCBPE) possesses powerful antioxidant capacity. This study aimed to further explore the antioxidative and cardioprotective effects of SCBPE on acute MI induced by isoprenaline (ISO) in rats. The rats were intragastrically administrated with SCBPE (600, 1200, or 1800 mg/kg/day) and Compound Danshen dropping pills (270 mg/kg/day) for 30 days, then subcutaneously injected with ISO (65 mg/kg/day) on the 29th and 30th day. Compared with the model group, pretreatment with middle and high doses of SCBPE significantly reduced serum aspartate transaminase, lactate dehydrogenase, and creatine kinase activities and increased myocardial superoxide dismutase, glutathione peroxidase, and catalase activities. The histopathologic aspects showed that pathological heart change was found in the model group and reduced to varying degrees in the SCBPE groups. Moreover, the protein expression of nuclear factor-erythroid 2-related factor 2 (Nrf-2), heme oxygenase-1 (HO-1), and Bcl2 in the heart increased in the SCBPE groups, while that of Bax decreased compared to the model group. Besides this, uridine was isolated from S. chinensis bee pollen for the first time. This study could provide a scientific basis for using Schisandra chinensis bee pollen as a functional food for the prevention of MI. [ABSTRACT FROM AUTHOR]

The cover image, by Xiaoqing Miao et al., is based on the Advanced Review Drug nanocrystals for cancer therapy, DOI: 10.1002/wnan.1499. [ABSTRACT FROM AUTHOR]

In the European honey bee, Apis mellifera, pollen foragers have a higher sucrose responsiveness than nectar foragers when tested using a proboscis extension response (PER) assay. In addition, Africanized honey bees have a higher sucrose responsiveness than European honey bees. Based on the biology of the Eastern honey bee, A. cerana, we hypothesized that A. cerana should also have a higher responsiveness to sucrose than A. mellifera. To test this hypothesis, we compared the sucrose thresholds of pollen foragers and nectar foragers in both A. cerana and A. mellifera in Fujian Province, China. Pollen foragers were more responsive to sucrose than nectar foragers in both species, consistent with previous studies. However, contrary to our hypothesis, A. mellifera was more responsive than A. cerana. We also demonstrated that this higher sucrose responsiveness in A. mellifera was not due to differences in the colony environment by co-fostering two species of bees in the same mixed-species colonies. Because A. mellifera foragers were more responsive to sucrose, we predicted that their nectar foragers should bring in less concentrated nectar compared to that of A. cerana. However, we found no differences between the two species. We conclude that A. cerana shows a different pattern in sucrose responsiveness from that of Africanized bees. There may be other mechanisms that enable A. cerana to perform well in areas with sparse nectar resources. [ABSTRACT FROM AUTHOR]

We hypothesize that the wild honey (Apis dorsata honey (ADH), A. florea honey, A. laboriosa honey and A. andreniformis honey) had high antibacterial activity to defend against degradation. The entomological proteins, botanical sources and antibacterial activities of wild honey were determined via a label-free proteome, DNA metabarcoding and agar well diffusion assay. The results showed that there were significant differences among physico-chemical properties, proteins and plant sources of honey samples from different honey bee species. All the honey samples diluted to a 90% moisture content inhibited Staphylococcus aureus, Escherichia coli and Bacillus subtilis with the exception of 90% ADH. Honey solutions inhibited Chromobacterium violaceum , with exception of ADH and some other species honey with different moisture contents. The differences in antibacterial activity were attributed to differences in the botanical sources, entomological proteins of the honey. The species-specific proteins in honey from each species can be used for their identification • Wild honey from different species have different physico-chemical properties. • There were species-specific proteins in honey produced by different species honey bee. • Botanical sources of honey from the same species, time and location varied. • Wild honey diluted to a 90% water content inhibited bacteria with some exceptions. [ABSTRACT FROM AUTHOR]

Salmonella enterica serovar Typhimurium ( S. Typhimurium) is a common food-borne pathogen that commonly causes gastroenteritis in humans and animals. Apis laboriosa honey (ALH) harvested in China has significant antibacterial activity against Staphylococcus aureus , Escherichia coli, and Bacillus subtilis . We hypothesize that ALH has antibacterial activity against S. Typhimurium. The physicochemical parameters, minimum inhibitory and bactericidal concentrations (MIC and MBC) and the possible mechanism were determined. The results showed that there were significantly different physicochemical parameters, including 73 phenolic compounds, among ALH samples harvested at different times and from different regions. Their antioxidant activity was affected by their components, especially total phenol and flavonoid contents (TPC, TFC), which had a high correlation with antioxidant activities except for the O 2 - assay. The MIC and MBC of ALH against S. Typhimurium were 20-30% and 25-40%, respectively, which were close to those of UMF5+ manuka honey. The proteomic experiment revealed the possible antibacterial mechanism of ALH1 at IC 50 (2.97%, w/v), whose antioxidant activity reduced the bacterial reduction reaction and energy supply, mainly by inhibiting the citrate cycle (TCA cycle), amino acid metabolism pathways and enhancing the glycolysis pathway. The results provide a theoretical basis for the development of bacteriostatic agents and application of ALH., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2023 Tan, Tian, Zhang, Miao, Wu, Miao, Kuang and Yang.)