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1.
Artículo en Inglés | MEDLINE | ID: mdl-38899362

RESUMEN

Non-small cell lung cancer (NSCLC) is the leading cause of cancer-related mortality worldwide. Increasing evidence suggests that long noncoding RNAs play crucial roles in lung cancer pathogenesis. We previously identified a novel lncRNA, LINC070974, which is associated with tumor cell proliferation. In the present study, we find that knockdown of LINC070974 inhibits cell proliferation, migration and invasion as well as tumor formation both in vitro and in nude mice. LINC070974 silencing also improves cisplatin efficacy in A549/DDP cells. The function of LINC070974 may depend on its interaction with YBX1. Knockdown of LINC070974 reduces the recruitment of YBX1 to the CCND1 promoter and delays tumor progression through its coregulatory genes, which are mainly involved in the p53 signaling pathway. We utilize nebulized inhalation to deliver siRNAs targeting LINC070974 and find that LINC070974 significantly prevents tumor metastasis and growth in lung tissues. These findings reveal the role of LINC070974 in lung cancer and suggest a promising therapeutic approach involving siRNA inhalation.

2.
Zhongguo Zhong Yao Za Zhi ; 47(12): 3224-3232, 2022 Jun.
Artículo en Zh | MEDLINE | ID: mdl-35851115

RESUMEN

The present study explored the correlation between the hydrodynamic size(i.e., hydrated particle size) and the surface component distribution of spray-dried powder based on the binary system model of berberine hydrochloride and dextran. A variety of mixture solutions containing substances of different proportions were prepared, and the hydrated particle sizes of the solutions were measured by laser light scattering technique. Then the effects of molecular weight and mixing proportion on the particle size were analyzed. After the solutions were spray-dried, the surface components of spray-dried powder were determined by X-ray photoelectron spectroscopy. The changes of hydrated particle size of the two substances in different solutions were measured with the altered solution environments, and the distribution of surface components after spray-drying was observed. The results of particle size measurement showed that different solution environments would change the hydrodynamic size of substances. Specifically, the particle size of berberine hydrochloride increased with the increase in ionic strength and solution pH, while the particle size of dextran decreased with the increase in ionic strength and increased with the increase in solution pH. The results of surface components of the spray-dried powder indicated that berberine hydrochloride was prone to accumulate on the surface of particles during spray-drying because of its large hydrodynamic size. Therefore, hydrodynamic size is considered an important factor affecting the surface component distribution of spray-dried powder. As revealed by scanning electron microscopy of the particle morphology of spray-dried powder, the particles of berberine hydrochloride spray-dried powder were irregularly elliptic, and the particles of dextran and mixture spray-dried powders were irregularly spherical with the shrunken surface. Finally, the FT4 powder rheometer and DVS instrument were used to determine the stability, adhesion, and hygroscopicity of the powder. The results showed that when berberine hydrochloride was enriched on the surface, the adhesion of the mixture increased and the fluidity became worse, but the hygroscopicity was improved to a certain extent. In addition, as found by hygroscopic kinetic curve fitting of spray-dried powder, the hygroscopic behaviors of all spray-dried powder conformed to the double exponential function.


Asunto(s)
Berberina , Administración por Inhalación , Aerosoles/química , Dextranos , Inhaladores de Polvo Seco/métodos , Hidrodinámica , Microscopía Electrónica de Rastreo , Tamaño de la Partícula , Polvos/química
3.
Mol Pharm ; 17(5): 1596-1607, 2020 05 04.
Artículo en Inglés | MEDLINE | ID: mdl-32142292

RESUMEN

Pulmonary fibrosis (PF) is a kind of interstitial lung disease with the features of progressive and often fatal dyspnea. Tetrandrine (TET) is the major active constituent of Chinese herbal Stephania tetrandra S. Moore, which has already applied clinically to treat rheumatism, lung cancer, and silicosis. In this work, a tetrandrine-hydroxypropyl-ß-cyclodextrin inclusion compound (TET-HP-ß-CD) was developed for the treatment of pulmonary fibrosis via inhalation administration. TET-HP-ß-CD was prepared by the freeze-drying method and identified using the cascade impactor, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectrum (FT-IR). A bleomycin-induced pulmonary fibrosis rat model was used to assess the effects of inhaled TET and TET-HP-ß-CD. Animal survival, hydroxyproline content in the lungs, and lung histology were detected. The results showed that inhalation of TET-HP-ß-CD alleviated inflammation and fibrosis, limited the accumulation of hydroxyproline in the lungs, regulated protein expression in PF development, and improved postoperative survival. Moreover, nebulized delivery of TET-HP-ß-CD accumulated chiefly in the lungs and limited systemic distribution compared with intravenous administration. The present results indicated that inhalation of TET-HP-ß-CD is an attractive candidate for the treatment of pulmonary fibrosis.


Asunto(s)
2-Hidroxipropil-beta-Ciclodextrina/química , Bencilisoquinolinas/química , Fibrosis Pulmonar/tratamiento farmacológico , 2-Hidroxipropil-beta-Ciclodextrina/administración & dosificación , 2-Hidroxipropil-beta-Ciclodextrina/farmacocinética , Administración por Inhalación , Animales , Bencilisoquinolinas/administración & dosificación , Bencilisoquinolinas/farmacocinética , Modelos Animales de Enfermedad , Pulmón/metabolismo , Pulmón/patología , Masculino , Fibrosis Pulmonar/mortalidad , Fibrosis Pulmonar/patología , Ratas , Ratas Sprague-Dawley , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Factor de Necrosis Tumoral alfa/análisis
4.
Langmuir ; 36(8): 2136-2142, 2020 03 03.
Artículo en Inglés | MEDLINE | ID: mdl-32027142

RESUMEN

Biomineralization is characterized by the fact that the crystallization of inorganic minerals is guided by an in vivo biological interface. However, the interfaces that direct calcification are widely debated up to date. In this paper, it was found that the two-dimensional (2D) immiscible domain of cholesterol in the lipid bilayer can induce the deposition of calcium phosphate by rapidly promoting the nucleation of the hydroxyapatite (001) plane. This promotion effect is related to the high lattice matching degree between the 2D cholesterol immiscible domain and the (001) plane of hydroxyapatite (HAP), which leads to the heteroepitaxy of HAP. The lipid bilayer derived from cells or vesicles is the largest biological interface in the body, thus revealing whether the lipid bilayer can induce the deposition of calcium phosphate will facilitate the understanding of the important role of cells or vesicles in calcification.

5.
Zhongguo Zhong Yao Za Zhi ; 44(13): 2841-2848, 2019 Jul.
Artículo en Zh | MEDLINE | ID: mdl-31359699

RESUMEN

Curcumin( Cur) is a natural active substance extracted from the roots or tubers of traditional Chinese medicinal materials. It has anti-inflammatory and anti-tumor activities on brain diseases. Due to the poor stability,low solubility,poor absorption and low bioavailability of curcumin,N-acetyl-L-cysteine( NAC) was used as an absorption enhancer and mixed with curcumin to improve the absorption of curcumin in the body. In this paper,curcumin was smashed by airflow pulverization,and Cur-NAC mixtures were prepared by being grinded with liquid. Then,the raw material and the product were analyzed by differential scanning calorimetry( DSC),X-ray diffraction( XRD) for structural characterization. The dissolution was determined by high performance liquid chromatography( HPLC) analysis. The characteristic peaks of the samples prepared by grinding method were similar to those of the raw materials,while the melting temperature and the accumulated dissolution degree were not significantly changed. The crystal forms of the products were not changed,and no new crystal form was formed after grinding. After the administration of intranasal powder,blood samples were collected from the orbit,while the whole brain tissues were removed from the skull and dissected into 10 anatomical regions. The concentrations of curcumin in these samples were determined by UPLC-MS/MS. The concentrations of curcumin in plasma and brain were compared at different time points. After intranasal administration of two drugs,it was found that the concentration of curcumin after sniffing up the mixtures in plasma was high,and the concentration of the drug in the olfactory bulb,hippocampus,and pons was increased significantly. Within 0. 083-0. 5 h,the olfactory bulb,piriform lobe and hippocampus remained high concentrations,the endodermis,striatum,hypothalamus and midbrain reached high concentrations within 1-3 h; and the cerebellum,pons and brain extension maintained relatively high concentrations within 3-7 h. The experiment showed that nasal administration of Cur-NAC mixtures can significantly improve the bioavailability of curcumin,and lead to significant differences in brain tissue distribution.


Asunto(s)
Acetilcisteína/farmacología , Química Encefálica , Curcumina/farmacocinética , Administración Intranasal , Animales , Disponibilidad Biológica , Encéfalo , Cromatografía Liquida , Ratas , Espectrometría de Masas en Tándem , Distribución Tisular
6.
Zhongguo Zhong Yao Za Zhi ; 43(8): 1642-1648, 2018 Apr.
Artículo en Zh | MEDLINE | ID: mdl-29751711

RESUMEN

To investigate the feasibility of vapor permeation membrane technology in separating essential oil from oil-water extract by taking the Forsythia suspensa as an example. The polydimethylsiloxane/polyvinylidene fluoride (PDMS/PVDF) composite flat membrane and a polyvinylidene fluoride (PVDF) flat membrane was collected as the membrane material respectively. Two kinds of membrane osmotic liquids were collected by self-made vapor permeation device. The yield of essential oil separated and enriched from two kinds of membrane materials was calculated, and the microscopic changes of membrane materials were analyzed and compared. Meanwhile, gas chromatography-mass spectrometry (GC-MS) was used to compare and analyze the differences in chemical compositions of essential oil between traditional steam distillation, PVDF membrane enriched method and PDMS/PVDF membrane enriched method. The results showed that the yield of essential oil enriched by PVDF membrane was significantly higher than that of PDMS/PVDF membrane, and the GC-MS spectrum showed that the content of main compositions was higher than that of PDMS/PVDF membrane; The GC-MS spectra showed that the components of essential oil enriched by PVDF membrane were basically the same as those obtained by traditional steam distillation. The above results showed that vapor permeation membrane separation technology shall be feasible for the separation of Forsythia essential oil-bearing water body, and PVDF membrane was more suitable for separation and enrichment of Forsythia essential oil than PDMS/PVDF membrane.


Asunto(s)
Forsythia , Aceites Volátiles , Destilación , Vapor , Agua
7.
Zhongguo Zhong Yao Za Zhi ; 42(12): 2366-2372, 2017 Jun.
Artículo en Zh | MEDLINE | ID: mdl-28822195

RESUMEN

PLA-α-asarone nanoparticles were prepared by using organic solvent evaporation method, and their in vivo distribution and brain targeting after intranasal administration were studied as compared with intravenous administration. The results showed that brain targeting coefficient of PLA-α-asarone nanoparticles after intranasal and intravenous administration was 1.65 and 1.16 respectively. The absolute bioavailability, brain-targeting efficiency and the percentage of nasal-brain delivery of PLA-α-asarone nanoparticles were 74.2%, 142.24 and 29.83%, respectively after intranasal administration. The results of fluorescence labeling showed that the fluorescent intensity of coumarin-6 in the brain tissue was the highest after intranasal administration of PLA-α-asarone fluorescent nanoparticles, achieving the purpose of brain-targeted drug delivery. The fluorescent intensity of coumarin-6 in liver tissue after intravenous administration of PLA-α-asarone nanoparticles was much higher than that after intranasal administration, indicating that intranasal administration of PLA-α-asarone nanoparticles could decrease drug-induced hepatotoxicity. In addition, the fluorescent intensity of coumarin-6 in lung tissue was weaker after intranasal administration, which solved the shortcomings of intranasal administration of α-asarone dry powder prepared by airflow pulverization method. In vivo studies indicated that PLA-α-asarone nanoparticles after intranasal administration had a stronger brain targeting as compared with intravenous administration.


Asunto(s)
Anisoles/farmacocinética , Química Encefálica , Sistemas de Liberación de Medicamentos , Nanopartículas , Administración Intranasal , Administración Intravenosa , Derivados de Alilbenceno , Animales , Poliésteres , Distribución Tisular
8.
Zhongguo Zhong Yao Za Zhi ; 42(20): 3912-3918, 2017 Oct.
Artículo en Zh | MEDLINE | ID: mdl-29243427

RESUMEN

In order to explore the adsorption characteristics of proteins on the membrane surface and the effect of protein solution environment on the permeation behavior of berberine, berberine and proteins were used as the research object to prepare simulated solution. Low field NMR, static adsorption experiment and membrane separation experiment were used to study the interaction between the proteins and ceramic membrane or between the proteins and berberine. The static adsorption capacity of proteins, membrane relative flux, rejection rate of proteins, transmittance rate of berberine and the adsorption rate of proteins and berberine were used as the evaluation index. Meanwhile, the membrane resistance distribution, the particle size distribution and the scanning electron microscope (SEM) were determined to investigate the adsorption characteristics of proteins on ceramic membrane and the effect on membrane separation process of berberine. The results showed that the ceramic membrane could adsorb the proteins and the adsorption model was consistent with Langmuir adsorption model. In simulating the membrane separation process, proteins were the main factor to cause membrane fouling. However, when the concentration of proteins was 1 g•L⁻¹, the proteins had no significant effect on membrane separation process of berberine.


Asunto(s)
Berberina/química , Proteínas/química , Adsorción , Cerámica , Membranas Artificiales
9.
Biotechnol Lett ; 38(2): 251-8, 2016 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-26482058

RESUMEN

OBJECTIVES: To develop a purification process using hollow fiber membrane separation combined with size exclusion chromatography for the extraction of lumbrokinase from earthworms (Lumbricus rubellus). RESULTS: To extract the protein, the earthworms were first homogenized for 10 min, to produce ultrafine particles. Polyether sulfone hollow fiber membranes with MW cut offs of 50 and 6 kDa were used for initial purification of the crude extract. Further purification was carried out on a Sephadex G-75 column, and yielded three fractions of high purity protein. One of these fractions showed fibrinolytic activity. CONCLUSIONS: Three samples of high purity protein were obtained and one protein (LK1) showed strong fibrinolytic activity. The method has higher purification efficiency in comparison with existing methods.


Asunto(s)
Cromatografía en Gel/métodos , Endopeptidasas/aislamiento & purificación , Filtración/métodos , Membranas , Oligoquetos/enzimología , Animales , Factores de Tiempo
10.
Bioorg Med Chem Lett ; 25(17): 3442-6, 2015 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-26212777

RESUMEN

Targeting acetylcholinesterase (AChE) using small molecule inhibitors is considered to be the most successful therapeutic strategy in the treatment of Alzheimer's disease (AD). Herein we present a shape-based virtual screening to identify new cores for the designing of AChE inhibitors. Ten active hits are identified and the most active hit, 5169-0032 and T5369186, showed comparable AChE inhibitory activity to tacrine. Prediction of physicochemical properties and ADME/T risk indicates their potential in druggability and safety. The two compounds provide new core and can serve as a promising fragment to design potent AChE inhibitors.


Asunto(s)
Aminopiridinas/química , Inhibidores de la Colinesterasa/química , Citocromo P-450 CYP3A , Humanos , Tamizaje Masivo , Modelos Moleculares
11.
Zhongguo Zhong Yao Za Zhi ; 40(6): 1091-6, 2015 Mar.
Artículo en Zh | MEDLINE | ID: mdl-26226751

RESUMEN

Tetradrine-tashionone II(A)-PLGA composite microspheres were prepared by the SPG membrane emulsification method, and the characterization of tetradrine-tashionone II(A) -PLGA composite microspheres were studied in this experiment. The results of IR, DSC and XRD showed that teradrine and tashionone II(A) in composite microspheres were highly dispersed in the PLGA with amorphous form. The results of tetradrine-tashionone II(A) -PLGA composite microspheres in vitro release experiment showed that the cumulative release amounts of tetradrine and tashionone II(A) were 6.44% and 3.60% in 24 h, and the cumulative release amounts of tetradrine and tashionone II(A) were 89.02% and 21.24% in 17 d. The process of drug in vitro release accorded with the model of Riger-Peppas. Tetradrine-tashionone II(A) -PLGA composite microspheres had slow-release effect, and it could significantly reduce the burst release, prolong the therapeutic time, decrease the dosage of drugs and provide a new idea and method to prepare traditional Chinese medicine compound.


Asunto(s)
Benzofuranos/química , Bencilisoquinolinas/química , Portadores de Fármacos/química , Composición de Medicamentos/métodos , Medicamentos Herbarios Chinos/química , Ácido Láctico/química , Ácido Poliglicólico/química , Composición de Medicamentos/instrumentación , Cinética , Microesferas , Tamaño de la Partícula , Copolímero de Ácido Poliláctico-Ácido Poliglicólico
12.
Zhongguo Zhong Yao Za Zhi ; 40(4): 739-43, 2015 Feb.
Artículo en Zh | MEDLINE | ID: mdl-26137700

RESUMEN

To study the pharmacokinetic characteristics and absolute bioavailability of α-asarone through dry powder inhalation in rats, and compare with that through oral administration and intravenous injection. A HPLC method was established for the determination of α-asarone in rat plasma to detect the changes in plasma concentrations of α-asarone through dry powder inhalation (20 mg · kg(-1)), oral administration (80 mg · kg(-1)) and intravenous injection (20 mg · kg(-1)) in rats. DAS 2.0 software was used to calculate the pharmacokinetic parameters. The absolute bioavailability of α-asarone was calculated according to AUC(0-t)) of administration routes and administration doses. According to the results, α-asarone showed good linear relations (r = 0. 999 4) at concentrations between 0.282-14.1 mg · L(-1), with the limit of detection (LOD) at 0.212 mg · L(-1). Through dry powder inhalation, oral administration and intravenous injection of α-asarone, the metabolic processes of α-asarone in rats conformed to one, two and three compartment models respectively, with the elimination half-life of (95.48 ± 48.28), (64.34 ± 27.59), (66.99 ± 29.76) min. According to the bioavailability formula, the absolute bioavailability of α-asarone through dry powder inhalation and oral administration were 78.32% and 33. 60%, respectively. This study showed that significant increase in elimination half-life and absolute bioavailability of α-asarone through dry powder inhalation, which lays a theoretical foundation for preparing α-asarone dry powder inhalers.


Asunto(s)
Anisoles/farmacocinética , Medicamentos Herbarios Chinos/farmacocinética , Administración por Inhalación , Derivados de Alilbenceno , Animales , Anisoles/administración & dosificación , Anisoles/sangre , Disponibilidad Biológica , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/análisis , Semivida , Masculino , Ratas , Ratas Sprague-Dawley
13.
Zhongguo Zhong Yao Za Zhi ; 39(24): 4787-91, 2014 Dec.
Artículo en Zh | MEDLINE | ID: mdl-25898579

RESUMEN

In this study, solvent evaporation method was used to preparing baicalin ethylcellulose microspheres for intranasal administration. The prepared microspheres were round with certain rough surface. The average drug loading and entrapment efficiency was (33. 31 ± 0. 045)% , (63. 34 ± 0. 11)% , respectively. As the characteristic crystalline peaks of baicalin were observed in the microspheres sample, the result of X-ray diffractometric analysis indicated that the baicalin was present in crystalline form after its entrapment in ethylcellulose matrix. By investigating the thermogram of microspheres sample, it was found that endothermic peak of baicalin was shifted from 211. 8 °C to 244. 2 °C and associated with the first broad endothermic peak of ethylcellulose. This could confirm that baicalin was loaded into ethylcellulose, nor simply physical mixture. The powder flowability test exhibited that the specific energy of microspheres was 3. 57 mJ . g-1 and the pressure drop was 2. 22 mBar when air kept the speed of 2 mm . s-1 through the powder bed with the force was 15 kPa. The consequence of the baicalin in vitro released from microspheres showed that the pure baicalin sample displayed faster (90%) release than microspheres sample (75%) in 7 h. Fitting model for release curve before 7 h, the results showed that the pure baicalin sample and the microsphere sample accorded with first order model (R2 = 0. 990 4) and Riger-Peppas model(R2 = 0. 961 2), respectively. Ex vivo rabbit nasal mucosa permeability experiment revealed that the value of cumulative release rate per unit area of the microsphere sample was 1. 56 times that of the pure baicalin sample. This provided the foundation for the in vivo pharmacokinetic study.


Asunto(s)
Celulosa/análogos & derivados , Composición de Medicamentos/métodos , Flavonoides/farmacocinética , Administración Intranasal , Presión del Aire , Animales , Celulosa/química , Flavonoides/administración & dosificación , Flavonoides/química , Masculino , Microesferas , Membrana Mucosa/metabolismo , Tamaño de la Partícula , Polvos , Conejos , Solventes , Difracción de Rayos X
14.
Zhongguo Zhong Yao Za Zhi ; 39(1): 59-64, 2014 Jan.
Artículo en Zh | MEDLINE | ID: mdl-24754169

RESUMEN

To optimize the pretreatment of Huanglian Jiedu decoction before ceramic membranes and verify the effect of different pretreatments in multiple model system existed in Chinese herb aqueous extract. The solution environment of Huanglian Jiedu decoction was adjusted by different pretreatments. The flux of microfiltration, transmittance of the ingredients and removal rate of common polymers were as indicators to study the effect of different solution environment It was found that flocculation had higher stable permeate flux, followed by vacuuming filtration and adjusting pH to 9. The removal rate of common polymers was comparatively high. The removal rate of protein was slightly lower than the simulated solution. The transmittance of index components were higher when adjust pH and flocculation. Membrane blocking resistance was the major factor in membrane fouling. Based on the above indicators, the effect of flocculation was comparatively significant, followed by adjusting pH to 9.


Asunto(s)
Cerámica/química , Medicamentos Herbarios Chinos/química , Soluciones/química , Floculación , Membranas Artificiales , Polímeros/química , Ultrafiltración/métodos
15.
Colloids Surf B Biointerfaces ; 238: 113913, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38608463

RESUMEN

A gout attack could be viewed as a nucleation event. Many reports have shown that the typical molecular structure of crystallization inhibitors usually contains carboxyl and hydroxyl groups, which could interact with solute molecules through hydrogen bonding, thereby suppressing the nucleation and growth of crystals. Since 1923, l-lactic acid (LA), a molecule with structural features of inhibitors, has been speculated to be a trigger for acute gout because metabolized LA temporarily reduces uric acid excretion and leads to a slow increase in serum uric acid concentration. However, many cases of gout presumably triggered by elevated lactate in a very short period of 4 h are often inexplicable. Here, we present the unexpected result that LA has a significant "opposite effect" on the nucleation and growth of gouty pathological crystals, which is that as the concentration of the additive LA increases, the nucleation and growth of the crystals is suppressed and then facilitated. This approach may help our clarifying the long-standing "misunderstandings" and further understanding the association between metabolized LA and increased risk of gout attacks. Finally, a novel mechanism called "tailed-made occupancy (TMO)" was used to explain the nucleation and crystallization effects of LA on sodium urate monohydrate (MSUM).


Asunto(s)
Cristalización , Gota , Ácido Láctico , Ácido Úrico , Gota/metabolismo , Ácido Láctico/química , Ácido Láctico/metabolismo , Humanos , Ácido Úrico/química , Ácido Úrico/metabolismo
16.
Colloids Surf B Biointerfaces ; 236: 113803, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38367289

RESUMEN

The core to the treatment of gout is the elimination of pathologic crystal, monosodium urate monohydrate (MSUM). The primary treatment available is to gradually dissolve the "culprit crystals" by lowering the blood uric acid concentration with medications, which often takes a long time and in severe cases must still be treated surgically. Herein, we developed a dynamic bionic platform based on a hydrogel composite membrane (HCM) to screen the direct facilitated solubilization of MSUM crystals by small organic molecules in bionic saturated, or even supersaturated, solutions. The customized and biologically safe (NAGA/PEGDA/NIPAM) HCM, which is consistent with the main amino acid composition of articular cartilage, well mimics the entire process of organic molecules leading to the dissolution of MSUM crystals in the joint system. With the verifications of this platform, it is shown that l-aspartic acid (ASP) significantly promotes the dissolution of MSUM crystals not only in saturated but also in supersaturated solutions. Furthermore, a novel mechanism called "crane effect" was used to explain this "dissolution effect" of ASP on MSUM, which stems from the ability of ASP to lock onto the surface of MSUM crystals through hydrogen bonding by virtue of its two carboxyl groups, and simultaneously its amino group lifts the uric acid molecules from the surface of MSUM crystals by virtue of interactions of hydrogen bonding. The results of bulk crystallization, scanning electron microscopy (SEM), powder X-diffraction (PXRD), and density-functional theory (DFT) studies are quantitatively consistent with this hypothetical "crane effect" mechanism. Hence, this HCM-based functional platform could provide entirely novel ideas and methods for drug design and screening for the treatment of pathological crystal diseases of gout.


Asunto(s)
Gota , Ácido Úrico , Humanos , Ácido Úrico/química , Biónica , Gota/tratamiento farmacológico , Gota/metabolismo , Cristalización , Hidrogeles
17.
Yao Xue Xue Bao ; 48(6): 925-32, 2013 Jun.
Artículo en Zh | MEDLINE | ID: mdl-23984530

RESUMEN

This study is to report the influence of conditions in spray drying process on physical and chemical properties and lung inhaling performance of Panax notoginseng Saponins - Tanshinone II A composite particles. According to the physical and chemical properties of the two types of components within the composite particles, three solvent systems were selected including ethanol, ethanol : acetone (9 : 1, v/v) and ethanol : acetone (4 : 1, v/v), and three inlet temperature: 110 degrees C, 120 degrees C, 130 degrees C to prepare seven different composite particle samples; each sample was characterized using laser diffraction, scanning electron microscopy (SEM), dynamic vapour sorption (DVS) and atomic force microscope (AFM), and their aerodynamic behavior was evaluated by a Next Generation Impactor (NGI). The results indicate that under the conditions of using the mixed solvent system of ethanol--acetone volume ratio of 9 : 1, and the inlet temperature of 110 degrees C, the resulting composite particles showed rough surface, with more tanshinone II A distributing in the outer layer, such composite particles have the best lung inhaling performance and the fine particle fraction (FPF) close to 60%. Finally it is concluded that by adjusting the conditions in co-spray drying process, the distribution amount and existence form of tanshinone II A in the outer layer of the particles can be changed so that to enhance lung inhaling performance of the drug composite particles.


Asunto(s)
Abietanos/química , Composición de Medicamentos/métodos , Inhaladores de Polvo Seco/métodos , Saponinas/química , Abietanos/administración & dosificación , Abietanos/aislamiento & purificación , Administración por Inhalación , Desecación , Microscopía Electrónica de Rastreo , Microesferas , Panax notoginseng/química , Tamaño de la Partícula , Plantas Medicinales/química , Saponinas/administración & dosificación , Saponinas/aislamiento & purificación , Solubilidad , Difracción de Rayos X
18.
Zhongguo Zhong Yao Za Zhi ; 38(4): 559-63, 2013 Feb.
Artículo en Zh | MEDLINE | ID: mdl-23713283

RESUMEN

OBJECTIVE: To prepare panax notoginseng saponins-tanshinone II(A) composite particles for pulmonary delivery, in order to explore a dry powder particle preparation method ensuring synchronized arrival of multiple components of traditional Chinese medicine compounds at absorption sites. METHOD: Panax notoginseng saponins-tanshinone II(A) composite particles were prepared with spray-drying method, and characterized by scanning electron microscopy (SEM), confocal laser scanning microscope (CLSM), X-ray diffraction (XRD), infrared analysis (IR), dry laser particle size analysis, high performance liquid chromatography (HPLC) and the aerodynamic behavior was evaluated by a Next Generation Impactor (NGI). RESULT: The dry powder particles produced had narrow particle size distribution range and good aerodynamic behavior, and could realize synchronized administration of multiple components. CONCLUSION: The spray-drying method is used to combine traditional Chinese medicine components with different physical and chemical properties in the same particle, and product into traditional Chinese medicine compound particles in line with the requirements for pulmonary delivery.


Asunto(s)
Abietanos/química , Abietanos/metabolismo , Composición de Medicamentos/métodos , Sistemas de Liberación de Medicamentos/métodos , Pulmón/metabolismo , Panax notoginseng/química , Saponinas/química , Absorción , Desecación , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/metabolismo
19.
Front Bioeng Biotechnol ; 11: 1189010, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37324421

RESUMEN

Background: In recent years, the impact of bacterial biofilms on traumatic wounds and the means to combat them have become a major research topic in the field of medicine. The eradication of biofilms formed by bacterial infections in wounds has always been a huge challenge. Herein, we developed a hydrogel with the active ingredient berberine hydrochloride liposomes to disrupt the biofilm and thereby accelerate the healing of infected wounds in mice. Methods: We determined the ability of berberine hydrochloride liposomes to eradicate the biofilm by means of studies such as crystalline violet staining, measuring the inhibition circle, and dilution coating plate method. Encouraged by the in vitro efficacy, we chose to coat the berberine hydrochloride liposomes on the Poloxamer range of in-situ thermosensitive hydrogels to allow fuller contact with the wound surface and sustained efficacy. Eventually, relevant pathological and immunological analyses were carried out on wound tissue from mice treated for 14 days. Results: The final results show that the number of wound tissue biofilms decreases abruptly after treatment and that the various inflammatory factors in them are significantly reduced within a short period. In the meantime, the number of collagen fibers in the treated wound tissue, as well as the proteins involved in healing in the wound tissue, showed significant differences compared to the model group. Conclusion: From the results, we found that berberine liposome gel can accelerate wound healing in Staphylococcus aureus infections by inhibiting the inflammatory response and promoting re-epithelialization as well as vascular regeneration. Our work exemplifies the efficacy of liposomal isolation of toxins. This innovative antimicrobial strategy opens up new perspectives for tackling drug resistance and fighting wound infections.

20.
ACS Pharmacol Transl Sci ; 6(6): 878-891, 2023 Jun 09.
Artículo en Inglés | MEDLINE | ID: mdl-37325446

RESUMEN

Idiopathic pulmonary fibrosis (IPF) is a kind of life-threatening interstitial lung disease characterized by progressive dyspnea with accurate pathogenesis unknown. At present, heat shock protein inhibitors are gradually used to treat IPF. Silybin, a heat shock protein C-terminal inhibitor, has high safety and good application prospects. In this work, we have developed a silybin powder able to be used for inhalation administration for the treatment of IPF. Silybin powder was prepared by the spray drying method and identified using cascade impactometry, particle size, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared (FT-IR) spectroscopy. A rat model of bleomycin-induced IPF was used to assess the effect of inhaled silybin spray-dried powder. Lung hydroxyproline content, wet weight, histology, inflammatory factor expression, and gene expression were examined. The results showed that inhaled silybin spray-dried powder alleviated inflammation and fibrosis, limited hydroxyproline accumulation in the lungs, modulated gene expression in the development of IPF, and improved postoperative survival. The results of this study suggest that silybin spray-dried powder is an attractive candidate for the treatment of IPF.

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