Therapeutic drug monitoring of perospirone: The lowest effective plasma concentration in patients with schizophrenia.

OBJECTIVES: This study investigated the effects of demographic factors such as age, sex and comedications on the plasma concentrations of perospirone in individuals diagnosed with schizophrenia. Additionally, the relationship between these plasma levels and the clinical efficacy of the medication was explored. METHODS: Data regarding the plasma concentration of perospirone in patients with schizophrenia were obtained from the Xi'an Mental Health Center and were retrospectively analysed. RESULTS: The study results revealed a range of 0.50-1.59 ng/mL for the 25th-75th percentile of perospirone concentration in the plasma, which ranged from 0.07 to 6.0 ng/mL. The plasma concentration of perospirone increased with the daily oral dose (r = 0.283, P < 0.05). Furthermore, patients with higher plasma perospirone concentrations and concentration-to-dose ratios (C/D) tended to be older or were women. Notably, the coadministration of valproate significantly reduced perospirone concentration and the C/D ratio by 54.7% and 35.3%, respectively (P < 0.01). Receiver operating characteristics curve analyses revealed that patients exhibited a good clinical response when their plasma perospirone concentrations were ≥ 1.17 ng/mL. CONCLUSION: The findings suggest that therapeutic drug monitoring of perospirone and adjustments to achieve steady-state concentrations of ≥ 1.17 ng/mL can be beneficial for optimising treatment for patients with schizophrenia.

Screening of rosmarinic acid from Salvia miltiorrhizae acting on the novel target TRPC1 based on the 'homology modelling-virtual screening-molecular docking-affinity assay-activity evaluation' method.

CONTEXT: Salvia miltiorrhizae Bunge (Lamiaceae) is a traditional Chinese medicine (TCM) for the treatment of 'thoracic obstruction'. Transient receptor potential canonical channel 1 (TRPC1) is a important target for myocardial injury treatment. OBJECTIVE: This work screens the active component acting on TRPC1 from Salvia miltiorrhizae. MATERIALS AND METHODS: TCM Systems Pharmacology Database and Analysis Platform (TCMSP) was used to retrieve Salvia miltiorrhiza compounds for preliminary screening by referring to Lipinski's rule of five. Then, the compound group was comprehensively scored by AutoDock Vina based on TRPC1 protein. Surface plasmon resonance (SPR) was used to determine the affinity of the optimal compound to TRPC1 protein. Western blot assay was carried out to observe the effect of the optimal compound on TRPC1 protein expression in HL-1 cells, and Fura-2/AM detection was carried out to observe the effect of the optimal compound on calcium influx in HEK293 cells. RESULTS: Twenty compounds with relatively good characteristic parameters were determined from 202 compounds of Salvia miltiorrhiza. Rosmarinic acid (RosA) was obtained based on the molecular docking scoring function. RosA had a high binding affinity to TRPC1 protein (KD value = 1.27 µM). RosA (50 µM) could reduce the protein levels (417.1%) of TRPC1 after oxygen-glucose deprivation/reperfusion (OGD/R) in HL-1 cells and it could inhibit TRPC1-mediated Ca2+ influx injury (0.07 ΔRatio340/380) in HEK293 cells. DISCUSSION AND CONCLUSIONS: We obtained the potential active component RosA acting on TRPC1 from Salvia miltiorrhizae, and we speculate that RosA may be a promising clinical candidate for myocardial injury therapy.

Facile preparation and performance study of antibacterial regenerated cellulose carbamate fiber based on N-halamine.

With the outbreak of coronavirus disease (COVID-19) which has incalculable disasters and economic losses, people have given increasing attention to the health and safety of textile and fiber materials. In this study, an eco-friendly, facile, and cost-effective wet-spinning cellulose carbamate fiber technology was developed, and N-halamine regenerated cellulose fiber (RCC-Cl) with rechargeable and rapid bactericidal properties were prepared by the Lewis acid-assisted chlorination method. The chemical properties of the fibers were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, X-ray photoelectron spectroscopy, thermogravimetric analysis, and energy-dispersive X-ray spectroscopy. The mechanical and surface topography of the treated fiber was investigated by tensile testing and scanning electron microscopy. The results showed that the mechanical properties of RCC-Cl fibers can reach a breaking strength of 12.1 cN/tex and a breaking elongation of 41.4% with the optimized spinning process. Furthermore, RCC-Cl showed excellent antimicrobial activities, which can inactivate Escherichia coli and Staphylococcus aureus at a concentration of 107 CFU/mL within 1 min. This work provided a novel approach to produce regenerated cellulose fibers with antibacterial properties, showing great potential in the field of functional textiles.

Microstructural and Tribological Properties of a Dopamine Hydrochloride and Graphene Oxide Coating Applied to Multifilament Surgical Sutures.

With the development of fine surgery and desire for low-injury methods, the frictional properties of surgical sutures are one of the crucial factors that can cause damage to tissue, especially for some fragile and sensitive human tissues such as the eyeball. In this study, dopamine hydrochloride and graphene oxide were used as external application agents to prepare a biological coating for the surface of multifilament surgical sutures. The effects of this biocoating on the surface morphology, chemical properties, mechanical properties, and tribological properties of surgical sutures were studied. The friction force and the coefficient of friction of surgical sutures penetrating through a skin substitute were evaluated using a penetration friction apparatus and a linear elastic model. The tribological mechanism of the coating on the multifilament surgical sutures was investigated according to the results of the tribological test. The results showed that there were uniform dopamine and graphene oxide films on the surface of the surgical sutures, and that the fracture strength and yield stress of the coated sutures both increased. The surface wettability of the surgical sutures was improved after the coating treatment. The friction force and the coefficient of friction of the multifilament surgical sutures with the dopamine hydrochloride and graphene oxide coating changed little compared to those of the untreated multifilament surgical sutures.