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1.
Zhongguo Zhong Yao Za Zhi ; 39(5): 828-32, 2014 Mar.
Artigo em Zh | MEDLINE | ID: mdl-25204173

RESUMO

Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.


Assuntos
Alcaloides/química , Química Farmacêutica/métodos , Portadores de Fármacos/química , Medicamentos de Ervas Chinesas/química , Rutaceae/química , beta-Ciclodextrinas/química , 2-Hidroxipropil-beta-Ciclodextrina , Solubilidade
2.
J Appl Anim Welf Sci ; 26(2): 218-228, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-34470518

RESUMO

Enriched environment (EE) is an important animal experimental paradigm to decipher gene-environment interaction. It is thought to be efficient in aiding recovery from certain metabolism disorders or cognitive impairments. Recently, the effects of EE during adolescence in mice gradually draw much attention. We first established an EE model in adolescent mice, dissected lipid metabolism, and further examined baseline level of anxiety and depression by multiple behavioral tests, including open field test (OFT), elevated zero maze (EZM), tail suspension test (TST), and forced swimming test (FST). EE mice exhibited lower weights, lower cholesterol than standard housing (SH) mice. Behaviorally, EE mice traveled more distance and had higher velocity than SH mice in OFT and EZM. Besides, EE mice showed reduced anxiety levels in OFT and EZM. Furthermore, EE mice also had less immobility time than SH mice in TST and FST. Thus, these results suggest that EE during adolescence has metabolic and behavioral benefits in mice.


Assuntos
Ansiedade , Metabolismo dos Lipídeos , Animais , Camundongos , Ansiedade/metabolismo , Ansiedade/psicologia , Natação , Comportamento Animal
3.
World J Clin Cases ; 10(5): 1548-1556, 2022 Feb 16.
Artigo em Inglês | MEDLINE | ID: mdl-35211592

RESUMO

BACKGROUND: Recent epidemiological studies have shown that general eye measurement parameters and corneal biomechanical properties can predict the speed of myopic progression in children. AIM: To investigate the correlation between the onset and progression of myopia and corneal biomechanical parameters in children. METHODS: The study included 102 cases in the emmetropia group, 207 cases in the myopic group, and 109 cases in the hyperopic group. The correlation between the change in corneal biomechanical indexes and the change in general ocular measurement parameters was analyzed. A one-way ANOVA test compared general ocular measurement and corneal biomechanical parameters. Pearson's correlation coefficient was analyzed to correlate corneal biomechanical and general ocular measurement parameters. RESULTS: The general ophthalmometric parameters: Spherical equivalent (SE), intraocular pressure (IOP), and axial length (AL), differed significantly among subjects in myopia, emmetropia, and hyperopic groups. Children's SE positively correlated with corneal biomechanical parameters: Second velocity of applanation (A2V), peak distance (PD), and deformation amplitude (DA) (P < 0.05), and second applanation length (A2L) (P < 0.05). But it was negatively correlated with PD, DA and integral radius (IR) (P < 0.05). Also, IOP was negatively correlated with A2L and IR (P < 0.05). AL positively correlated with A2V and negatively correlated with second applanation time (A2T), highest concavity, and PD. Central corneal thickness positively correlated with first applanation length, first applanation time, first applanation deformation amplitude, A2V, A2L, A2T, second applanation deformation amplitude, central curvature radius at highest concavity (HCR), PD, DA, IR, ambrosia relational thickness-horizontal, first applanation stiffness parameter, corvis biomechanical index, topographic and biomechanics index and the first velocity of applanation. The general ocular Km in children positively correlated with corneal biomechanical parameters DA and IR and negatively correlated with A2L, HCR, and PD. There was a positive correlation between the general ocular measurement parameters ΔSE and corneal biomechanical parameters ΔA2V and ΔA2L, and a negative correlation with ΔIR. The increase in general ocular measurement parameter ΔKm positively correlated with changes in corneal biomechanical parameters, ΔDA and ΔIR, and negatively correlated with ΔHCR and ΔPD. CONCLUSION: Myopia development in children was associated with multiple corneal biomechanical parameters.

4.
Int J Radiat Oncol Biol Phys ; 110(3): 757-765, 2021 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-33610390

RESUMO

PURPOSE: Our previous findings have identified vitronectin (VTN) as a potential biomarker for radiation pneumonitis (RP) through proteomics and molecular mechanism studies. In a recent study, we further explored associations of plasma level and single nucleotide polymorphisms of VTN with the risk of RP in patients with lung cancer receiving radiation therapy. METHODS AND MATERIALS: A total of 165 patients with lung cancer were prospectively enrolled with detection of VTN concentration before radiation therapy. VTN reference single nucleotide polymorphisms, rs704 and rs2227721, were genotyped by Taqman probe method. Cox proportional hazard models were performed to identify clinical variables and genotypes associated with the risk of RP on univariate and multivariate analyses, and t tests and analysis of variance were conducted to evaluate the expression level of VTN. RESULTS: The baseline secretion level of VTN in patients with grade ≥3 RP was significantly higher than that in grade <3 RP patients (P < .0001), and elevated levels were observed in patients having the AA genotype compared with GA/GG genotypes of rs704. The VTN rs704 GA/GG and rs2227721 AA/AC genotypes had a significantly lower risk of RP (hazard ratio [HR], 0.448, P = .005; HR, 0.419, P = .008, respectively). In addition, combining cut-off values of mean lung dose (MLD) and VTN plasma level, grade ≥3 RP risk groupings were as follows: high risk: MLD ≥12 Gy and VTN level ≥132 µg/mL (RP rate, 10 of 16 patients, 62.5%); intermediate risk: MLD ≥12 Gy and VTN level <132 µg/mL or MLD <12 Gy and VTN level ≥132 µg/mL (8 of 70 patients, 11.4%); and low risk: MLD <12 Gy and VTN level <132 µg/mL (1 of 79 patients, 1.3%) (P < .0001). CONCLUSIONS: Among patients receiving radiation therapy, relatively high plasma levels of VTN before radiation therapy were associated with the higher incidence of RP, and VTN rs704 and rs2227721 each had a significant effect on predicting RP risk. Combining VTN concentration with MLD appeared to facilitate stratification of patients with lung cancer who received radiation therapy into low-, intermediate-, and high-risk RP groups. This study indicated that VTN may serve as a blood biomarker for susceptibility to RP in patients with lung cancer.


Assuntos
Neoplasias Pulmonares/radioterapia , Polimorfismo de Nucleotídeo Único , Pneumonite por Radiação/etiologia , Vitronectina/sangue , Vitronectina/genética , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Neoplasias Pulmonares/sangue , Neoplasias Pulmonares/genética , Masculino , Pessoa de Meia-Idade
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