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Tran, Thuan-Hieu,Chang, Woo-Jin,Kim, Young-Bum,Koo, Yoon-Mo,Kim, Eun-Ki,Yoon, Joo-Young,Kim, Jin-Hwan Korean Society for Biotechnology and Bioengineerin 2007 Biotechnology and Bioprocess Engineering Vol.12 No.5
The effect of fluidic conditions on the bioluminescent detection of ATP in a microfluidic device was surveyed using homemade detector system. The bioluminescent reaction of ATP was directly affected by the retention time and flow rates of the solutions in this diffusion-based mixing and reaction system due to the laminar flow in the microchannel. ATP and enzyme solutions were separately injected into the microfluidic device at different flow rates through 3 inlet ports. The ATP solution was injected through the middle port, while the enzyme solution was injected in the two remaining ports. When the ratio of ATP to enzyme solution was fixed, the optimum flow rates of enzyme, ATP, and enzyme solution was 3.5, 8.0, and $3.5{\mu}L/min$, respectively. The optimal total flow rate was $1.5{\mu}L/min$. The detection limit for the concentration of ATP at optimal conditions was less than $10^{-7}M$.
Thuan-Hieu Tran,장우진,김영범,구윤모,김은기,윤주영,김진환 한국생물공학회 2007 Biotechnology and Bioprocess Engineering Vol.12 No.5
The effect of fluidic conditions on the bioluminescent detection of ATP in a microfluidic device was surveyed using home-made detector system. The bioluminescent reaction of ATP was directly affected by the retention time and flow rates of the solutions in this diffusion-based mixing and reaction system due to the laminar flow in the microchannel. ATP and enzyme solutions were separately injected into the microfluidic device at different flow rates through 3 inlet ports. The ATP solution was injected through the middle port, while the enzyme solution was injected in the two remaining ports. When the ratio of ATP to enzyme solution was fixed, the optimum flow rates of enzyme, ATP, and enzyme solution was 3.5, 8.0, and 3.5 μL/min, respectively. The optimal total flow rate was 15 μL/min. The detection limit for the concentration of ATP at optimal conditions was less than 10-7 M.
Huan, Le Cong,Tran, Phuong-Thao,Phuong, Cao Viet,Duc, Phan Huy,Anh, Duong Tien,Hai, Pham The,Huong, Le Thi Thu,Thuan, Nguyen Thi,Lee, Hye Jin,Park, Eun Jae,Kang, Jong Soon,Linh, Nguyen Phuong,Hieu, Tr Elsevier 2019 Bioorganic chemistry Vol.92 No.-
<P><B>Abstract</B></P> <P>In search for novel small molecules with antitumor cytotoxicity via activating procaspase-3, we have designed and synthesized three series of novel (E)-<I>N</I>′-benzylidene-4-oxoquinazolin-3(4<I>H</I>)-yl)acetohydrazides (<B>5a-j, 6a-h,</B> and <B>7a-h)</B>. On the phenyl ring ò the benzylidene part, three different substituents, including 2-OH-4-OCH<SUB>3</SUB>, 4-OCH<SUB>3</SUB>, and 4-N(CH<SUB>3</SUB>)<SUB>2</SUB>, were introduced, respectively. Biological evaluation showed that the acetohydrazides in series <B>5a-j</B>, in which the phenyl ring of the benzylidene part was substituted by 2-OH-4-OCH<SUB>3</SUB> substituent, exhibited potent cytotoxicity against three human cancer cell lines (SW620, colon; PC-3, prostate; NCI-H23, lung). Most of the compounds, in this series, especially compounds <B>5c, 5b</B> and <B>5h,</B> also significantly activated caspase-3 activity. Among these, compound <B>5c</B> displayed 1.61-fold more potent than PAC-1 as caspase-3 activator. Cell cycle analysis showed that compounds <B>5b</B>, <B>5c</B>, and <B>5h</B> significantly arrested the cell cycle in G1 phase. Further apoptotic studies also demonstrated compounds <B>5b</B>, <B>5c</B>, and <B>5h</B> as strong apoptotic cell death inducers. The docking simulation studies showed that these compounds could activate procaspase <I>via</I> chelating Zn<SUP>2+</SUP> ion bound to the allosteric site of the zymogen.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Novel (<I>E</I>)-<I>N</I>′-benzylidene-2-(4-oxoquinazolin-<I>3(4H)-yl</I>)acetohydrazides were synthesized. </LI> <LI> The acetohydrazides <B>5a-i</B> exhibited potent cytotoxicity against three human cancer cell lines. </LI> <LI> A number of cytotoxic compounds exhibited good caspase activation activity. </LI> <LI> The cytotoxic compounds were shown to arrest cells at G1 phase. </LI> <LI> The cytotoxic compounds were shown as strong apoptotic inducers. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>