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Chalcone 유도체들의 사람 유방암세포주 및 사람 섬유육종 세포에 대한 세포독성효과
강유라(Youra Kang),박민아(Min-A Park),조미연(Mi-Yeon Cho),이경희(Kyung Hee Lee),김정애(Jung-Ae Kim) 대한약학회 2010 약학회지 Vol.54 No.1
Xanthohumol, a prenylated chalcone of the Hop plant (Humulus lupulus L.), has been reported to suppress tumor growth. 4-hydroxychalcone and isobavachalcone are chalcone derivatives and they have similar structure with xanthohumol. In the present study, we investigated the cytotoxic activities of chalcone and its erivatives, 4-hydroxychalcone, xanthohumol, and isobavachalcone, in MCF-7 and adriamycin resistant MCF-7 (MCF-7/ADR) breast cancer cells and HT-1080 fibrosarcoma cells. In a cell viability assay using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) reagent, chalcone and 4-hydroxychalcone decreased cell viability in HT-1080 cells, but not in MCF-7 and MCF-7/ADR cells. Isobavachalcone showed similar cytotoxicity in HT-1080 cells, and only limited cytotoxicity in MCF-7 and MCF-7/ADR cells at very high concentration (50 μM). In contrast, xanthohumol showed concentration-dependent cytotoxicity in MCF-7, MCF-7/ADR, and HT-1080 cancer cells. Taken together, the structure-activity relationship of chalcone and its derivatives indicate that chalcones may be valuable cytotoxic compounds against selective cancer types.
김은정,박성영 한국공업화학회 2019 한국공업화학회 연구논문 초록집 Vol.2019 No.0
In this study, the phosphorylated 2-hydroxychalcone (HCAP) fluorescent probe was conjugated with coatable catechol-bromododecane quarternized poly(vinylpyrrolidone) (C/C12-PVP) polymer to obtain C/C12-PVP conjugated with HCAP (HCAP-PVP) for detection and antibacterial activity. When bacteria were introduced into HCAP-PVP, the phosphate group of HCAP was degraded by endogenous alkaline phosphatase (ALP) enzyme and the greenish-yellow emission of the probe was shifted to red. Hence, in the presence of quaternary ammonium of dodecane, HCAP-PVP showed an effective antibacterial activity in both solid and aqueous states. Therefore, this sensor can be used as a simple and fast enzymatic biosensor for rapidly detecting and killing bacteria with high sensitivity.
Kang, Eun Bi,Mazrad, Zihnil Adha Islamy,Robby, Akhmad Irhas,In, Insik,Park, Sung Young Elsevier 2018 European polymer journal Vol.105 No.-
<P><B>Abstract</B></P> <P>The present study aimed to develop an enzymatic colorimetric method using a surface-adsorbing biosensor to detect and kill bacteria in a single, simple, and rapid assay. The phosphorylated fluorescent probe 2-hydroxychalcone (HCAP) conjugated with an adhesive cationic polymer was designed (HCAP-PVP), which yielded greenish-yellow emission in aqueous buffer. Upon introduction of <I>Escherichia coli</I> and <I>Staphylococcus aureus</I>, the phosphate group inside the HCAP was cleaved by endogenous alkaline phosphatase (ALP) and the greenish-yellow emission ratiometrically changed to deep-red emission. This biosensor system detected bacteria over a wide range of bacterial densities (10<SUP>1</SUP>–10<SUP>7</SUP> colony-forming units/mL) after 60 min, with similar bacterial detection abilities between aqueous- and solid-phase assays. Furthermore, the presence of a quaternary ammonium of dodecane in this system displayed efficient antibacterial activity because of the change in cellular hydrophobic interactions, which enabled this material to act as a dual sensor and killing material. Thus, this system is a novel, rapid, and simple enzymatic sensor with high sensitivity that can be used as a solid-based platform to detect and directly eliminate bacteria.</P> <P><B>Highlights</B></P> <P> <UL> <LI> A colorimetric method was designed for detection of bacteria based on ALP activity. </LI> <LI> HCAP-conjugated adhesive cationic polymer showed fluorescent changes in response to ALP. </LI> <LI> Quaternary ammonium of dodecane in this system provided antibacterial activity. </LI> <LI> This system can be used for both aqueous- and solid-phase assays. </LI> <LI> This sensor showed excellent bacteria detection ability and antibacterial activity. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>