• Title/Summary/Keyword: BH3 profiles

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Effects of mixed formulation of tamoxifen and blue honeysuckle on the pharmacokinetics profiles of tamoxifen after single oral administration

  • Hu, Jin-Ryul;Jang, Tae-Woo;Kang, Su-Jin;Ku, Sae-Kwang;Choi, Seong-Hun;Lee, Young-Joon
    • The Journal of Korean Medicine
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    • v.40 no.4
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    • pp.1-15
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    • 2019
  • Objectives: Here, we investigated the effects of concentrated and lyophilized powders Blue honeysuckle (BH) on the PK of tamoxifen, to establish the pharmacokinetics (PK) profiles as one of essential process in new drug development. Methods: After single oral treatment of 0.4 mg/ml of tamoxifen or tamoxifen 0.4 with BH 40, 20 and 10 mg/ml, the plasma were collected at 0.5 hr before administration, 0.5, 1, 2, 3, 4, 6, 8 and 24 hr after end of single or mixed formula treatment. Plasma concentrations of tamoxifen were analyzed using LC-MS/MS methods. Tmax, Cmax, AUC, t1/2 and MRTinf were analyzed using noncompartmental PK data analyzer programs. Results: Tamoxifen and BH 40 mg/ml did not induce any significant change on the plasma tamoxifen concentrations, while significant decreases were observed in tamoxifen and BH 10 mg/ml from 2 to 8 hr as compared with tamoxifen only, respectively. Furthermore, significant increases of Tmax in tamoxifen and BH 40 mg/ml, significant decreases of Cmax in tamoxifen and BH 20 mg/ml, significant decreases of AUC0-t, AUC0-inf and MRTinf in tamoxifen and BH 10 mg/ml were demonstrated as compared with tamoxifen only. Conclusion: Taken together, tamoxifen and BH 10 mg/ml induced significant decrease of the oral bioavailability of tamoxifen, while tamoxifen and BH 40 or 20 mg/ml did not critically influenced, suggesting formulated BH concentration-independencies. It, therefore, seems to be needed that pharmacokinetic study after repeated administration should be tested to conclude the effects of BH on the pharmacokinetics of tamoxifen.

The Effect of Lipopolysaccharide on Noxa Expression Is Mediated through IRF1, 3, and 7

  • Piya, Sujan;Kim, Tae-Hyoung
    • Journal of Microbiology and Biotechnology
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    • v.28 no.3
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    • pp.491-497
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    • 2018
  • Lipopolysaccharide (LPS), a component of the cell wall of gram-negative bacteria, elicits the secretion of cytokines, such as interferons, that stimulate the host defense system. Previously, we demonstrated that interferons induce interferon regulatory factors (IRFs) 1, 3, and 7, which regulate the transcription of Noxa and alter the expression profiles of Bcl-2 family proteins in tumors. However, the immediate consequences of LPS stimulation on Noxa and BH3 expression in tumor cells remain uncharacterized. In this study, we determined that LPS induced Noxa expression in CT26 cells. Furthermore, studies in HCT116 parental and HCT116 p53-deficient cells revealed that LPS-mediated Noxa was independent of p53. Meanwhile, IRF1, 3, and 7 in CT26, HCT116 parental, and HT116 p53-deficient cells were upregulated by LPS stimulation, suggesting that LPS induces the expression of these IRFs in a p53-independent manner. The responsiveness of IRF1, 3, 4, and 7 binding to the Noxa promoter region to LPS indicated that IRF1, 3, and 7 activated Noxa expression, whereas IRF4 repressed Noxa expression. Together, these results suggest that LPS directly affects Noxa expression in tumor cells through IRFs, implicating that it may contribute to LPS-induced tumor regression.

Effects of the mixed formulation of sorafenib and blue honeysuckle on the pharmacokinetics profiles of sorafenib

  • Kang, Hyun-Gu;Kang, Su-Jin;Ku, Sae-Kwang;Choi, Seong-Hun;Lee, Young-Joon
    • Journal of Society of Preventive Korean Medicine
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    • v.23 no.1
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    • pp.83-94
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    • 2019
  • Objective : This study investigated the effects of concentrated and lyophilized blue honeysuckle powders (BH) on the pharmacokinetics (PK) of sorafenib were observed. Method : The blood was collected at 0.5 hr before single oral treatment of sorafenib (40 mg/kg) or sorafenib with BH (400, 200 and 100 mg/kg) mixed formulas administration, and 0.5, 1, 2, 3, 4, 6, 8 and 24 hrs after the end of single or mixed formula administration. Plasma concentrations of sorafenib were analyzed using LC-MS/MS methods. Tmax, Cmax, AUC, $t_{1/2}$ and $MRT_{inf}$ of sorafenib were analysis as compared with sorafenib single treatment. Results : Single oral administration of mixed formulas induced significant increases of plasma sorafenib concentrations from 0.5 hr after end of administration throughout all blood collected time points, as compared with sorafenib single formula treated rats, and significant decreases of sorafenib Tmax with increases of Cmax, $AUC_{0-t}$ and $AUC_{0-inf}$ were detected in sorafenib and BH 400 mg/kg mixed formulation treated rats as compared with sorafenib single formula treated rats, respectively. Inaddition, sorafenib and BH 200 or 100 mg/kg mixed formula treated rats also showed significant increases of sorafenib Cmax, $AUC_{0-t}$ and $AUC_{0-inf}$, respectively. Conclusions : According to these results, mixed formulation of BH with sorafenib increased the bioavailability of sorafenib through the increment of the absorptions.

Fuel cell system for SUAV using chemical hydride - I. Lightweight hydrogen generation and control system (화학수소화합물을 이용한 소형 무인항공기용 연료전지 시스템 연구 - I. 경량 수소 발생 및 제어 장치)

  • Hong, Ji-Seok;Jung, Won-Chul;Kim, Hyeon-Jin;Lee, Min-Jae;Jeong, Dae-Seong;Jeon, Chang-Soo;Sung, Hong-Gye;Shin, Seock-Jae;Nam, Suk-Woo
    • Journal of the Korean Society for Aeronautical & Space Sciences
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    • v.41 no.3
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    • pp.226-232
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    • 2013
  • A compact hydrogen generation device of fuel cell system using chemical hydride storage technique was designed to fit the propulsion device requirement of a small unmanned aerial vehicle(SUAV). For high efficient, compact, and lightweight hydrogen generation control device, the Co-B catalyst hydrogen conversion rate by $NaBH_4$ aqueous solution flux is measured so that the proper amount of Co-B catalyst for maximum hydrogen generation of 100W stack was proposed. A compact hydrogen generation device is controlled by pump's on/off using its own internal pressure and consumes fuel in high efficiency through a dead-end type fuel cell. The fuel cell system has stable operation for a planed flight profile. The system operates up to maximum 7 hours and at least 4 hours for tough flight profiles.