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스핑고신 키나아제 1 저해제인 PF-543과 PF-543 유사체 (22c)의 항암활성
백동재(Dong Jae Baek),박은영(Eun Young Park) 대한약학회 2018 약학회지 Vol.62 No.5
PF-543 selectively inhibits sphingosine kinase (SK)1 most potently among the known SK inhibitors. Although SK1 inhibitors have been reported to have anticancer effect, PF-543 has lower anticancer activity in some cancer cells compared with selective inhibition of SK1. Recent PF-543 derivatives were synthesized in Pfizer and observed inhibitory effects on SK1, suggesting that (S)-1-(4-((3-methyl-5-((phenylsulfonyl)methyl)phenoxy)methyl)benzyl)pyrrolidin-3-ol (22c) is more effective than PF-543. We investigated whether 22c improved the anticancer activity compared to PF-543 in proportion to the SK-1 inhibitory effect. The cytotoxic effect of PF-543, 22c and 5-fluorouracil was compared in HT29, HCT116 and AGS cells. PF-543 showed slightly higher cytotoxic effect than 22c in all cells. These results suggest that the SK inhibitory activity and the anticancer effect of the SK inhibitor are not necessarily proportional to each other. Therefore, development of SK inhibitor as an anticancer agent requires comparison of anticancer activity.
고혈압 노인의 가구소득과 건강관련 삶의 질 간 관계에서약제비 부담의 매개효과에 관한 연구
문홍섭,백동재,박은영,최정민 대한약학회 2019 약학회지 Vol.63 No.3
The purpose of this study was to examine the mediating effect of drug cost burden on the relationship betweenhousehold income and quality of life in hypertensive elderly. The subjects of this study were 4,722 elderly people aged65 or older who had hypertension among 180,130 patients who had Korea Health Panel. The analytical method used washierarchical regression analysis, and the mediating effect was tested according to the method proposed by Baron andKenny. The results showed that the partial mediation effect of drug cost burden was significant in relation to the householdincome and health-related quality of life of the elderly with hypertension. Based on the results of this study, we proposeto establish an income assistance program for drug cost burden of low-income elderly with hypertension.
김경,박은영,백동재,오윤신 한국식품과학회 2022 Food Science and Biotechnology Vol.31 No.10
Insect-based food is increasingly used and is a sustainable protein source provided by eco-friendly breeding respecting the animal welfare. The cricket Gryllus bimaculatus is an approved edible insect. In this paper, the effects of G. bimaculatus extracts (AE-GBE) on hepatic insulin resistance and the underlying mechanisms were investigated in high fat diet (HFD)-fed C57BL/6J mice. Mice were fed HFD for 6 weeks and some were concomitantly given AE-GBE orally (100 mg/kg/day). AE-GBE significantly improved glucose tolerance and insulin sensitivity by attenuating hepatic lipid accumulation measured by the reduced serum and hepatic lipid contents. Moreover, AE-GBE significantly downregulated the expression of hepatic lipogenesis-related genes and activated the AMPK signaling pathway. Therefore, AE-GBE might improve fatty liver and glucose metabolism disorders as well as insulin resistance by inhibiting the expression of proteins involved in hepatic fatty acid synthesis through AMPK activation.
김수빈,이태호,오윤신,박은영,백동재 대한화학회 2023 Bulletin of the Korean Chemical Society Vol.44 No.4
FTY720 exerts an anticancer effect through the activation of protein phospha- tase 2A (PP2A), which acts as a tumor suppressor, and inhibits SK1 activity. However, FTY720 taken into the body is phosphorylated by endogenous SK2. The structure of FTY720 is well-studied as a basis for developing SK inhibitors and PP2A activators. We synthesized analogs of PF-543 with a dimeric tail structure and reported the efficacy of SK1 inhibition. The compounds with this structure had improved anticancer activity and stability compared with PF-543. To confirm whether the dimeric tail structure could be applied as a PP2A-active material, we synthesized four types of compounds with a dimeric tail structure and confirmed the anticancer activity and PP2A activation in A549 non-small cell lung cancer cells. Compounds 2 and 4 were more cytotoxic to A549 cells than RB005, and induced similar levels of cytotoxic and PP2A activation as FTY720.