RESUMEN
BACKGROUNDS: Intolerable toxicity and unsatisfactory therapeutic effects are still big problems retarding the use of chemotherapy against cancer. Nano-drug delivery system promised a lot in increasing the patients' compliance and therapeutic efficacy. As a unique nano-carrier, supermolecular aggregation nanovehicle has attracted increasing interests due to the following advantages: announcing drug loading efficacy, pronouncing in vivo performance and simplified production process. METHODS: In this study, the supermolecular aggregation nanovehicle of bortezomib (BTZ) was prepared to treat breast cancer. RESULTS: Although many supermolecular nanovehicles are inclined to disintegrate due to the weak intermolecular interactions among the components, the BTZ supermolecules are satisfying stable. To shed light on the reasons behind this, the forces driving the formation of the nanovehicles were detailed investigated. In other words, the interactions among BTZ and other two components were studied to characterize the nanovehicles and ensure its stability. CONCLUSIONS: Due to the promising tumor targeting ability of the BTZ nanovehicles, the supermolecule displayed promising tumor curing effects and negligible systemic toxicity.
Asunto(s)
Antineoplásicos/farmacología , Bortezomib/química , Bortezomib/farmacología , Sistemas de Liberación de Medicamentos/métodos , Animales , Línea Celular Tumoral , Femenino , Humanos , Ensayo de Materiales , Ratones , Ratones Endogámicos BALB C , Nanopartículas , Propiedades de SuperficieRESUMEN
A series of phosphaisocoumarin amidates were synthesized for the first time via DIBAL-H-mediated direct amidation of phosphaisocoumarin esters under mild conditions in good to excellent yields. The present reaction showed high selectivity. In each case, the phostone ring was intact and only the exocyclic ethoxy group was amidated. A plausible mechanism of the reaction was provided.
Asunto(s)
Amidas/química , Ésteres/química , Isocumarinas/síntesis química , Compuestos Organometálicos/química , Organofosfonatos/síntesis química , Aminas/química , Espectroscopía de Resonancia Magnética , Organofosfonatos/químicaRESUMEN
AIM: To investigate the differences in retinal refraction difference values (RDVs) of adult patients with myopic anisometropia compared with those without myopic anisometropia, and to investigate the relationship between ocular biometric measurements and relative peripheral refraction. METHODS: This clinical observation study included 130 patients with myopia (-0.25 to -10.00 D) between October 2022 and January 2023 aged between 18 and 40y. The patients were divided into anisometropia (n=63; difference in binocular anisometropia ≥1.00 D) and non-anisometropia (n=67; difference in binocular anisometropia <1.00 D) groups accordingly. Ocular biometric measurements were performed by optical biometrics and corneal topography to assess the steep keratometry (Ks), flap keratometry (Kf), axial length (AL), corneal astigmatism (CYL; Ks-Kf), surface regularity index (SRI), surface asymmetry index (SAI), and central corneal thickness (CCT). The RDV was measured at five retinal areas from the fovea to 53 degrees (RDV-0-10, RDV-10-20, RDV-20-30, RDV-30-40, and RDV-40-53), the total RDV (TRDV) of 53 degrees, and four regions, including RDV-superior, RDV-inferior, RDV-temporal, and RDV-nasal. An analysis of Spearman correlation was carried out to examine the correlation between RDV and the spherical equivalent (SE) and ocular biological parameters. RESULTS: Within RDV-20-53, both groups showed relative hyperopic defocus, and the increase in RDV corresponds to the increase in eccentricity. In the myopic anisometropia group, the TRDV, RDV-20-53, RDV-superior, and more myopic eyes had significantly higher RDV-temporal values than less myopic eyes. (P<0.05). In the non-anisometropia group, there was no significant difference in the RDV between the more and less myopic eyes at different eccentricities (P>0.05). There was a negative correlation between SE and TRDV (r=-0.205, P=0.001), RDV-20-53 (r=-0.281, -0.183, -0.176, P<0.05), RDV-superior (r=-0.251, P<0.001), and RDV-temporal (r=-0.230, P<0.001), a negative correlation between CYL and RDV-10-30 (r=-0.147, -0.180, P<0.05), and a negative correlation between SRI and RDV-0-20 (r=-0.190, -0.170, P<0.05). AL had a positive correlation with RDV-20-30 (r=0.164, P=0.008) and RDV-temporal (r=0.160, P=0.010). CONCLUSION: More myopic eyes in patients with myopic anisometropia show more peripheral hyperopic defocus. Diopter and corneal morphology may affect peripheral retinal defocus.