CJZ3, a lomerizine derivative, modulates P-glycoprotein function in rat brain microvessel endothelial cells1

Ji, Bian‐Sheng; He, Ling; Li, Xiaoqu; Liu, Guoqing

doi:10.1111/j.1745-7254.2006.00294.x

Cited by 4 publications

(3 citation statements)

References 17 publications

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“…Rat brain capillaries were isolated from cerebral gray matter of rat brain by a method described previously (Ji et al, 2006). Briefly, the cortex was stripped of the pial membrane and incubated at 37°C for 25 min in D-Hank's solution containing 0.05% trypsin.…”

Section: Methodsmentioning

confidence: 99%

Inhibition of P‐glycoprotein function by procyanidine on blood–brain barrier

Zhao

Yan

et al. 2009

Phytotherapy Research

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The inhibitory effects of procyanidine, one of the components from the bark of Pinus massoniana Lamb, on the P-glycoprotein (P-gp) function of the blood-brain barrier (BBB) were studied using in vitro rat brain microvessel endothelial cells (RBMECs) and nude mice transplanted with human cerebroma. Quantitative accumulation and efflux of rhodamine 123 (Rh123), a P-gp substrate, were determined using a fluorescence spectrophotometer as a measure of P-gp function. Procyanidine markedly increased the accumulation of Rh123 by inhibiting its efflux in a dose-dependent manner. A 5-fold increase in cellular Rh123 was observed for procyanidine at 10 micromol/L. The verapamil-stimulated ATPase activity in plasma membrane vesicles from the RBMECs was estimated by measuring inorganic phosphate liberation. Procyanidine significantly inhibited the verapamil-induced P-gp ATPase activity by 78% when pretreated with 10 micromol/L in a concentration-dependent manner. The inhibition of P-gp by procyanidine was suggested to be at least partly due to its inhibition of P-gp ATPase. Procyanidine markedly improved the therapeutic effects of adriamycin (ADM) on nude mice transplanted with human cerebroma, compared with solitary treatment of ADM. The combination of 80 mg/kg procyanidine with 2 mg/kg ADM significantly elevated the days of survival with an increase in life span of 76%. The findings suggested that procyanidine was a potent inhibitor of P-gp on BBB and could improve the therapeutic effects on cerebral tumors of some drugs which are difficult to accumulate in the brain.

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Section: Methodsmentioning

confidence: 99%

Inhibition of P‐glycoprotein function by procyanidine on blood–brain barrier

Zhao

Yan

et al. 2009

Phytotherapy Research

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“…Rat brain microvessel endothelial cells (RBMECs) were isolated according to the method of Abbott et al (1992) and Ji et al (2006) with minor modifications. Firstly, cortex was obtained from the brains of Sprague-Dawley rats (d5-8; Jiangsu Province Animal Center) and placed in ice-cold phosphate-buffered saline (PBS).…”

Section: Cell Lines and Cell Culturementioning

confidence: 99%

Substituted tetrahydroisoquinoline compound B3 inhibited P-glycoprotein-mediated multidrug resistance in-vitro and in-vivo

Fang

Cai

et al. 2007

Journal of Pharmacy and Pharmacology

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P-glycoprotein (P-gp) mediated multidrug resistance (MDR) is one of the main obstacles in tumour chemotherapy. A promising approach to reverse MDR is the combined use of nontoxic and potent P-gp inhibitor with conventional anticancer drugs. We have examined the potential of a newly synthesized tetrahydroisoquinoline derivative B3 as a MDR-reversing agent. The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay was used to examine the effect of B3 on the cytotoxicity in K562/A02 and MCF-7/ADM cells caused by doxorubicin (adriamycin). Accumulation and efflux of P-gp substrate rhodamine123 in K562/A02 and primary cultured rat brain microvessel endothelial cells (RBMECs) were measured to evaluate the inhibitory effect of B3 on P-gp. The K562/A02 xenograft model in nude mice was established to examine MDR-reversing efficacy of B3 in-vivo. The results indicated that co-administration of B3 resulted in an increase on chemosensitivity of K562/A02 and MCF-7/ADM cells to doxorubicin in a dose-dependent manner. Rhodamine123 accumulation in K562/A02 cells and RBMECs were significantly enhanced after the incubation with various concentrations of B3. Furthermore, B3 inhibited the efflux of rhodamine123 from RBMECs. Co-administration of B3 with doxorubicin significantly decreased weight and volume of tumour in nude mice. In conclusion, B3 is a novel and potent MDR reversal agent with the potential to be an adjunctive agent for tumour chemotherapy.

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“…Within last decade, numerous approaches of improving the fracture toughness of ceramics have been developed, such as transformation toughening, dispersed ductile/brittle (microcracking toughening) particle toughening, and fiber/whisker toughening, which can lead to crack bridging and deflection upon crack propagation [3,4]. It is well known that nano-fiber is effective reinforcements for ceramics, and considerable development of whisker-reinforced ceramic matrix composites (CMCs) has been made in recent decade [5,6]. And fracture toughness of ceramic materials can be improved remarkably by incorporating fibers [7,8].…”

Section: Introductionmentioning

confidence: 99%

Effects of Sepiolite Mineral Nano-Fiber on Strength and Toughness of Ceramics

Wang

Liang

et al. 2013

AMM

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The effects of sepiolite mineral nanofiber on strength and toughness of ceramics were investigated by bone china with addition of sepiolite mineral nanofiber. The flexural strength and fracture toughness were tested by three point bending method and single edge notched beam (SENB) method, and the microstructure of the ceramics was studied by scanning electron microscopy (SEM), X-ray diffraction (XRD) and optical microscopy. The results indicated that the structure pattern of sepiolite mineral nanofiber became much shorter and thicker after calcinations. Proper addition of sepiolite mineral nanofiber would increase the strength and toughness of bone china. The sepiolite mineral nanofiber can yield the bone china with fracture toughness and flexural strength values as high as 5.65 MPa·m1/2and 112.66 MPa to 5.87 MPa·m1/2and 118.90 MPa, mainly due to crack bridging, crack deflection and pullout by sepiolite mineral nanofiber.

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CJZ3, a lomerizine derivative, modulates P-glycoprotein function in rat brain microvessel endothelial cells1

Cited by 4 publications

References 17 publications

Inhibition of P‐glycoprotein function by procyanidine on blood–brain barrier

Inhibition of P‐glycoprotein function by procyanidine on blood–brain barrier

Substituted tetrahydroisoquinoline compound B3 inhibited P-glycoprotein-mediated multidrug resistance in-vitro and in-vivo

Effects of Sepiolite Mineral Nano-Fiber on Strength and Toughness of Ceramics

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