Search Results (26)

The effect of Lonicera japonica Thunb. (LJT) extract on melanosis and quality deterioration of Pacific white shrimp (Litopenaeus vannamei) during cold storage was evaluated, using 4-hexylresorcinol (4-HR), a commercial melanosis inhibitor, as a positive control. The results showed that LJT inhibited polyphenol oxidase (PPO) activity and complexed copper ions in a dose-dependent manner (LJT < 16 mg/mL), indicating that LJT has the potential to inhibit shrimp melanization. Visual image and grayscale value analysis revealed that LJT and 4-HR effectively alleviated melanosis and delayed deterioration of shrimp quality stored at 4 °C, with LJT exhibiting a superior effect. LJT samples displayed a lower total number of colonies, total volatile base nitrogen value, and thiobarbituric reactive substance value than the others (p < 0.05), suggesting that LJT exerted the most potent inhibition on microbial growth and lipid oxidation in shrimps during cold storage. Consequently, LJT effectively retarded the melanosis and quality deterioration of shrimps. Full article

This study investigates the potential of 4-hexylresorcinol (4HR) as a novel antidiabetic agent by assessing its effects on blood glucose levels, Glut4 expression, AMPK phosphorylation, and Histone H3 acetylation (Ac-H3) in the liver. In vitro experiments utilized Huh7 and HepG2 cells treated with varying concentrations of 4HR. Glut4, p-AMPK, and Ac-H3 expression levels were quantified via Western blotting. Additionally, GAPDH activity and glucose uptake were evaluated. In vivo experiments employed streptozotocin (STZ)-induced diabetic rats, with or without 4HR treatment, monitoring blood glucose, body weight, and hepatic levels of Glut4, p-AMPK, and Ac-H3. In vitro, 4HR treatment increased GAPDH activity and glucose uptake. Elevated Glut4, p-AMPK, and Ac-H3 levels were observed 8 h after 4HR administration. Inhibition of p-AMPK using compound C reduced 4HR-mediated Glut4 expression. In STZ-induced diabetic rats, 4HR significantly upregulated Glut4, p-AMPK, and Ac-H3 expression in the liver. Periodic 4HR injections mitigated weight loss and lowered blood glucose levels in STZ-injected animals. Histological analysis revealed increased glycogen storage in hepatocytes of the 4HR-treated group. Overall, 4HR enhanced Glut4 expression through upregulation of AMPK activity and histone H3 acetylation in vitro and in vivo, improving hepatic glucose homeostasis and suggesting potential as a candidate for diabetes treatment. Full article

Background: Cancer is one of the most significant threats to human health. Following surgical excision, chemotherapy is an effective strategy against remaining cancer cells. 4-hexylresorcinol (4-HR) has anti-cancer properties and exhibits hydrophobicity-induced aggregation in the blood that has trouble with targeted tumor delivery and cellular uptake of the drug. The purpose of this study is to encapsulate 4-HR into solid lipid nanoparticles (SLNs) to enhance its anti-cancer effect by avoiding aggregation and facilitating cellular uptake. Methods: 4-HR SLNs were prepared via hot melt homogenization with sonication. SLN characteristics were assessed by analyzing particle size, zeta potential, and drug release. Cytotoxicity, as an indicator of the anti-cancer effect, was evaluated against HeLa (cervical cancer in humans), A549 (lung cancer in humans), and CT-26 (colon carcinoma in mice) cell lines. Results: Particle size ranged from 169.4 to 644.8 nm, and zeta potential ranged from −19.8 to −40.3 mV, which are conducive to cellular uptake. Entrapment efficiency (EE) of 4-HR was found to be 75.0—96.5%. The cytotoxicity of 4-HR-loaded SLNs demonstrated enhanced anti-cancer effects compared to pure 4-HR. The enhancement of anti-cancer effects depended on reduced particle size based on cellular uptake, the EE, and the cell type. Conclusions: These findings imply that 4-HR-loaded SLN is a promising strategy for chemotherapy in cancer treatment. Full article

It is known that many diabetic patients experience testicular atrophy. This study sought to investigate the effect of 4-hexylresorcinol (4HR) on testicular function in rats with streptozotocin (STZ)-induced diabetes, focusing on testicular weight, sperm motility, histological alterations, and serum testosterone levels to understand the efficacy of 4HR on testes. Our findings reveal that 4HR treatment significantly improves testicular health in diabetic rats. Notably, the STZ group exhibited a testicular weight of 1.22 ± 0.48 g, whereas the STZ/4HR group showed a significantly enhanced weight of 1.91 ± 0.26 g (p < 0.001), aligning closely with the control group’s weight of 1.99 ± 0.17 g and the 4HR group’s weight of 2.05 ± 0.24 g, indicating no significant difference between control and 4HR groups (p > 0.05). Furthermore, the STZ/4HR group demonstrated significantly improved sperm motility compared to the STZ group, with apoptotic indicators notably reduced in the STZ/4HR group relative to the STZ group (p < 0.05). These results underscore the therapeutic potential of 4HR for maintaining testicular function under diabetic conditions. Full article

Taste perception plays a crucial role in health and well-being but can be compromised by conditions such as diabetes mellitus (DM). This study delved into the efficacy of 4-hexylresorcinol (4-HR) in mitigating taste bud apoptosis, particularly in relation to DM-induced taste issues. Two primary rat groups were investigated: healthy rats and streptozotocin (STZ)-induced diabetic rats. Each group was further divided into control and experimental subsets, with the experimental group receiving 4-HR injections. A histological analysis of the circumvallate papillae (CVP) highlighted significant taste bud deterioration in the STZ subgroup, including loss of cellular content and a deviation from their typical morphology. Quantitatively, the control group had a mean of 39.6 ± 14.3 taste bud pores/mm², contrasting with the 4HR, STZ, and STZ/4HR groups, which had means of 33.7 ± 14.2, 20.3 ± 6.1, and 28.0 ± 8.3, respectively. Additionally, a TUNEL assay and IHC staining for c-caspase-3 both identified increased apoptotic cells in the STZ subgroup, with the mean number of apoptotic cells per taste bud profile being notably higher in the STZ group at 3.2 ± 1.6. This study underscores the profound impact of diabetes on taste bud physiology and the potential therapeutic benefits of 4-HR. Further research is essential to delve deeper into its mechanisms and to ascertain optimal dosages, with the aim of enhancing the quality of life of diabetic patients. Full article

Biocidal coatings have been used in biomedicine, cosmetology and the food industry. In this article, the coatings are described as being composed of non-stoichiometric polycomplexes, products of electrostatic coupling of two commercial biodegradable ionic polymers, anionic sodium alginate and cationic quaternized hydroxyethyl cellulose ethoxylate. Non-stoichiometric polycomplexes with a 5-fold excess of the cationic polymer were used for immobilizing hydrophobic biocidal 4-hexylresorcinol (HR). Being dispersed in water, the polycomplex particles were capable of absorbing a tenfold excess of HR in relation to the polycation. After deposition onto the plastic surface and drying, the aqueous polycomplex–HR composite formulation forms a transparent homogeneous coating, which swells slightly in water. The interpolyelectrolyte complex (IPEC) is substantially non-toxic. The incorporation of HR in the IPEC imparts antimicrobial activity to the resulting composite, in both aqueous solutions and coatings, against Gram-negative and Gram-positive bacteria and yeast. The polysaccharide-based polycomplexes with embedded HR are promising for the fabrication of biocidal films and coatings. Full article

The deepening of color of ready-to-eat (RTE) abalone during storage leads to sensory quality degradation, which seriously affects the shelf life of products and consumers’ purchasing desire. The goal of this study is to look into the causes of non-enzymatic browning and lipid oxidation, as well as how to control them, and their effect on the color of RTE abalone during storage. The control, bloodletting and antioxidants groups (lactic acid, citric acid and 4-hexylresorcinol) of RTE abalone were stored for 0, 20 and 40 days at 40 °C, respectively, to explore the rule and mechanism of the color change in RTE abalone. This research shows that RTE abalone undergoes browning during storage. Meanwhile, the content of reducing sugar, phenols and unsaturated fatty acids decreases, while the formation of lipid hydroperoxides and aldehydes increases during storage. In addition, the color change in RTE abalone during storage is mainly related to the Maillard reaction, while the lipid oxidation mainly forms pyrrole and participates in the Strecker degradation process as part of the Maillard reaction. The quality of RTE abalone can be maintained by controlling browning effectively as well as lipid oxidation through bloodletting and the addition of antioxidants to ensure that RTE abalone has high storage stability. According to our research, bloodletting and the addition of antioxidants to RTE abalone have a good application prospect and popularizing value in the storage of RTE abalone. Full article

The resistance of microorganisms’ biofilms to antibacterials is a problem both for medicine and for many industries. Increasing the effectiveness of antimicrobial agents is an urgent task. The goal of the present work was to develop a new approach to development of anti-biofilm compositions based on conventional disinfectants in combination with enhancers (adjuvants). Methods of microbiology (viable cells count, model biofilms) and electron microscopy were employed. This research formulates the principles for selection of adjuvants. The adjuvants should: (1) increase the efficiency of decomposition of the biofilm matrix or/and (2) suppress the microbial protective mechanisms. For testing anti-biofilm compositions, two models of biofilms have been developed, on a solid surface at the interface with air or liquid. It was demonstrated that hydrogen peroxide, ethanol, isopropanol, and 4-hexylresorcinol enhanced the biocidal effect of disinfectants based on oxidants (peroxides and chlorine-containing) and quaternary ammonium salts by three to six orders of magnitude. Mechanisms of adjuvant action were mechanical decomposition of the matrix (by oxygen bubbles formed inside a biofilm in the case of hydrogen peroxide), coagulation of matrix polymers (in the case of alcohols), and a decrease in metabolism (in the case of 4-hexylresorcinol). The use of approved chemicals as adjuvants will accelerate the design of effective anti-biofilm antiseptics for medicine, social hygiene, and food manufactures and other industries. Full article

Silk sericin is a degumming product used by the silk industry. The degumming process can affect the protein structure and molecular weight of silk sericin. The present study examined how pretreatment with 4-hexylresorcinol (4HR) affects the biomedical properties of silk sericin. Before the degumming process, silkworm cocoons were treated with 4HR solution. The protein structure of the final degumming product was evaluated by Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy. Untreated silk sericin (S) and silk sericin pretreated with 4HR (S+4HR) were added to RAW264.7 cells, and the expression of BMP-2 was determined. The bone-regenerating capacity of S+4HR was evaluated using the critical-sized rat calvarial defect model. Compared with S, S+4HR showed an increase in β-sheet structures. Administration of S+4HR to RAW264.7 cells increased expression of BMP-2, mainly via the TLR-mediated signaling pathway. Bone volume, as measured by micro-computerized tomography, was significantly greater in the S+4HR group than in the S, gelatin alone, and unfilled control groups (p < 0.05 each). Expression of BMP-2 and runx2 in tissue specimens was significantly higher following treatment with S+4HR than with S (p < 0.05). Taken together, these findings show that 4HR pretreatment before the degumming process increased the β-sheet structure of silk sericin, as well as inducing BMP-2 expression and bone regeneration ability. Full article

Background: Mutation of p53 is a frequent event, and mutant p53 exhibits low levels of acetylation and phosphorylation. This study aimed to investigate the effect of the histone deacetylase (HDAC) inhibitor, 4-hexylresorcinol (4HR), on the acetylation and phosphorylation of mutant p53 carcinoma cells and its therapeutic effects in a xenograft model. Methods: To determine the effect of 4HR on the acetylation and phosphorylation of p53, western blot analysis was performed using YD-9 and YD-15 cells. p53 siRNA was used to examine whether 4HR acts in a p53-dependent or independent manner. This was evaluated using a xenograft model. Results: In in vitro experiments when the concentration of 4HR was increased, the expression levels of HDAC4, acetylated p53 (Ac-p53), and phosphorylated p53 (p-p53) increased. Transfection with TP53 siRNA successfully suppressed p53 protein and TP53 mRNA expression. When 4HR was administered to a xenograft model, the tumour expansion rate was suppressed compared with the control, and the mice exhibited a higher survival rate. Conclusions: Our findings reveal that 4HR is a potential agent that restores loss of function in mutant p53 cancer cells via acetylation and phosphorylation of p53 as well as inhibition of HDAC4. Full article

In our previous study, 4-hexylresorcinol (4HR) increased the expression level of vascular endothelial growth factor in human umbilical vein endothelial cells (HUVECs) via the transforming growth factor-β1 (TGF-β1)-mediated pathway. Endoplasmic reticulum (ER) and mitochondrial stress is a positive regulator of cellular differentiation. As TGF-β1 is a master regulator for cellular differentiation, 4HR treatment may increase TGF-β1 expression via ER stress. In this study, HUVECs were treated using 4HR (1–100 μM) for 24 h. The 4HR treatment increased ER stress-associated markers and mitochondrial stress. Increased TGF-β1 expression by 4HR administration was alleviated by tauroursodeoxycholate (ER stress inhibitor) treatment. Combining these activities with the elevated acetylation level of histone 3 (H3) by 4HR treatment, TGF-β1 expression was increased in HUVECs. Overall, 4HR increased TGF-β1 expression through upregulation of the stress response of ER as well as H3 acetylation in HUVECs. Full article

4-Hexylresorcinol (4HR) has been used as a food additive, however, it has been recently demonstrated as a Class I histone deacetylase inhibitor (HDACi). Unlike other HDACi, 4HR can be taken through foods. Unfortunately, some HDACi have an influence on craniofacial growth, therefore, the purpose of this study was to evaluate the effects of 4HR on craniofacial growth. Saos-2 cells (osteoblast-like cells) were used for the evaluation of HDACi and its associated activities after 4HR administration. For the evaluation of craniofacial growth, 12.8 mg/kg of 4HR was administered weekly to 4 week old rats (male: 10, female: 10) for 12 weeks. Ten rats were used for untreated control (males: 5, females: 5). Body weight was recorded every week. Serum and head samples were collected at 12 weeks after initial administration. Craniofacial growth was evaluated by micro-computerized tomography. Serum was used for ELISA (testosterone and estrogen) and immunoprecipitation high-performance liquid chromatography (IP-HPLC). The administration of 4HR (1–100 μM) showed significant HDACi activity (p < 0.05). Body weight was significantly different in male rats (p < 0.05), and mandibular size was significantly smaller in 4HR-treated male rats with reduced testosterone levels. However, the mandibular size was significantly higher in 4HR treated female rats with increased growth hormone levels. In conclusion, 4HR had HDACi activity in Saos-2 cells. The administration of 4HR on growing rats showed different responses in body weight and mandibular size between sexes. Full article

Damaged dental pulp undergoes oxidative stress and 4-hexylresorcinol (4HR) is a well-known antioxidant. In this study, we aimed to evaluate the therapeutic effects of a 4HR ointment on damaged dental pulp. Pulp cells from rat mandibular incisor were cultured and treated with 4HR or resveratrol (1–100 μM). These treatments (10–100 μM) exerted a protective effect during subsequent hydrogen peroxide treatments. The total antioxidant capacity and glutathione peroxidase activity were significantly increased following 4HR or resveratrol treatment (p < 0.05), while the expression levels of TNF-α and IL1β were decreased following the exposure to 4HR pre-treatment in an in vitro model. Additionally, the application of 4HR ointment in an exposed dental pulp model significantly reduced the expression of TNF-α and IL1β (p < 0.05). Conclusively, 4HR exerted protective effects against oxidative stress in dental pulp tissues through downregulating TNF-α and IL1β. Full article

Histone deacetylases (HDACs) are key enzymes for post-translational modification and influence on various cellular activities. Thus, HDACs are associated with many diseases and their inhibitors have clinical significance. Here, 4-Hexylresorcinol (4HR) was studied as an inhibitor for class I HDACs using the HDAC inhibitor (HDACi) Trichostatin-A as a positive control. The 4HR was administered 1–100 μM to human umbilical endothelial cells (HUVECs) and the HDAC expression and activity were examined. The 4HR decreased the expression level of HDAC1, 3, 4, and 5 in a time and dose-dependent manner. The 4HR also increased acetylated lysine and decreased HDAC activity significantly (p < 0.05). Collectively, 4HR was a new class I HDAC inhibitor that reduced the expression and activity of HDAC in HUVECs. Full article

This contribution reports an efficient method for the production and use of biocide-loaded cellulose acetate nanoparticles. As well-known model biocides 4-Hexylresorcinol and Triclosan were used for in situ nanoparticle loading during a nanoprecipitation process. We show that the nanoparticle size can be well-controlled by variation of the cellulose acetate concentration during nanoprecipitation. Apart from strong evidence suggesting cellulose acetate particle formation according to a nucleation-aggregation mechanism, we further show that the biocide loading of the particles occurs by a diffusion process and not via co-precipitation. The quantity of particle loading was analyzed by ¹H-NMR spectroscopy of re-dissolved nanoparticles, and it was observed that a decisive factor for high packaging efficiency is the use of a biocide with low water solubility and high hydrophobicity. SEM studies showed no influence on the particle morphology or size by both biocides 4-Hexylresorcinol and Triclosan. Finally, an aqueous nanoparticle dispersion can be coated onto model paper sheets to yield pronounced antimicrobial surface-properties. Nanoparticles loaded with the biocide Triclosan showed a high antimicrobial activity against Bacillus subtilis, a cellulase producing bacteria, if applied to model paper substrates, even at extremely low coating weights of 1–5 g/m², respectively. Additional long-term efficacy renders these nanoparticles ideal for various applications. Full article