Based on the prodrug principle, aspirin and eugenol, as starting precursors, were esterified to synthesize aspirin eugenol ester (AEE). The aim of the present study was to evaluate the antithrombotic effect of AEE in an animal disease model. In order to compare the therapeutic effects of AEE and its precursors, aspirin, eugenol and a combination of aspirin and eugenol were designed at the same molar quantities as the AEE medium dose in the control group. After oral administration of AEE (dosed at 18, 36 and 72 mg/kg) for seven days, rats were treated with k-carrageenan to induce tail thrombosis. Following the same method, aspirin (20 mg/kg), eugenol (18 mg/kg) and 0.5 % CMC-Na (30 mg/kg) were administered as control drug. Different drug effects on platelet aggregation, hemorheology, TXB2/6-keto-PGF1α ratio and blood biochemistry were studied. AEE significantly inhibited ADP and AA-induced platelet aggregation in vivo. AEE also significantly reduced blood and plasma viscosity. Moreover, AEE down-regulated TXB2 and up-regulated 6-keto-PGF1α, normalizing the TXB2/6-keto-PGF1α ratio and blood biochemical profile. In comparison with aspirin and eugenol, AEE produced more positive therapeutic effects than its precursors under the same molar quantity. It may be concluded that AEE was a good candidate for new antithrombotic and antiplatelet medicine. Additionally, this study may help to understand how AEE works on antithrombosis in different ways.
Aspirin and eugenol were esterified to synthesize aspirin eugenol ester (AEE). As a pale yellow and odourless crystal, AEE reduced the gastrointestinal damage of aspirin and vulnerability of eugenol. The study was conducted to evaluate the preventive effects of AEE on blood lipids in rats with high fat diet (HFD). Suspensions of AEE and simvastatin were prepared in 5% carboxymethyl cellulose sodium (CMC-Na). In order to observe the intervention effects, the drugs and HFD were administrated at the same time. Based on individual weekly body weight (BW), AEE was intragastrically administrated at the dosage of 18, 36 and 54 mg/kg. Simvastatin (10 mg/kg) and CMC-Na (20 mg/kg) were used as control drug. After 6 weeks of administration, the changes of BW and blood lipid indices including triglyceride (TG), low density lipoprotein (LDL), high density lipoprotein (HDL) and total cholesterol (TCH) were determined in the experiment. The rat blood lipids profile in model group was remarkably different after feeding 6-weeks HFD. TG, TCH and LDL indexes in model group were increased significantly compared with those in control group (p < 0.01). AEE at the dosage of 54 mg/kg significantly decreased levels of TG, TCH and LDL (p < 0.01), and slowed the rate of BW gain in comparison with model group (p < 0.05). Moreover, high dose AEE showed better effects than simvastatin on reducing TCH level and similar effects on TG, HDL and LDL. AEE could remarkably reduce levels of TG, TCH and LDL in rats with high fat diet, and slow the rate of body weight gain. It was conducted that AEE was a potential candidate on reducing blood lipids level. The mechanism of action of AEE should be investigated in further studies.
26 February 2025 in Ecotoxicology and Environmental Safety
There remains a substantial knowledge gap in understanding the coexistence effects of Microplastics (MPs), lead (Pb) and arsenic (As), which are ubiquitous environmental contaminants. Here, zebrafish (Danio rerio) embryos were used to investigate the impact of triple combined exposure to MPs (50 μg/L), Pb2+ (10 μg/L) and As3+ (200 μg/L) on the developmental responses. Survival and hatching rates were notably reduced to 32.7 % and 58.8 %, respectively. Meanwhile, the frequency of spontaneous tail contractions increased by 8.1 %, whereas heart rate and body length decreased by 4.4 % and 5.1 %, respectively. These findings demonstrated that the triple exposure markedly disrupted developmental processes and altered behavioral profiles in zebrafish larvae. Furthermore, 16 S rRNA sequencing revealed that the metabolic processes of glutathione and xenobiotics, as well as intracellular iron transport, were significantly impacted, triggering ferroptosis in the larvae exposed to triple combination. Collectively, the co-exposure to MPs, Pb2+ and As3+ even at low concentrations could significantly disrupt the developmental progress and biological functioning during the early stages of zebrafish. This will help guide future comprehensive studies on the impact of triple combined exposure during early developmental stages.
Perchlorate is a well-known thyroid-disrupting chemical as well as an extremely stable inorganic pollutant widely distributed in the environment. Therefore, perchlorate posts potential risks to the environment as well as human health. Crayfish is a dominant aquatic food with increasing consumption levels in recent years. It is crucial to evaluate the accumulation of perchlorate with well-water-soluble properties in crayfish and to assess its health risks. In our present study, we obtained crayfish samples from cultivated ponds and markets based on the regions of the Middle and Lower Reaches of the Yangtze River. The perchlorate concentration was measured in all 206 samples using ultra-high performance liquid chromatography coupled with mass spectrometry (UPLC–MS). Monte Carlo simulation was used to perform health risk assessments. The results indicated that perchlorate levels ranged from 7.74–43.71 μg/kg for cultivated crayfish and 4.90–16.73 μg/kg for crayfish sold in markets. The perchlorate accumulation mainly occurred in exoskeleton parts. All the HQ values were remarkable, at less than one—indicating that perchlorate exposure through the ingestion of crayfish does not pose an appreciable risk to human health.