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Anti-inflammatory components of the Vietnamese starfish <i>Protoreaster nodosus</i>
Thao, Nguyen Phuong,Luyen, Bui Thi Thuy,Koo, Jung Eun,Kim, Sohyun,Koh, Young Sang,Cuong, Nguyen Xuan,Nam, Nguyen Hoai,Van Kiem, Phan,Kim, Young Ho,Van Minh, Chau BioMed Central 2015 Biological research Vol.48 No.1
<P><B>Background</B></P><P>In the present study, we examined the inhibitory effects of a methanolic extract, dichloromethane fraction, water layer, and polyhydroxylated sterols <B>(1–4)</B> isolated from the Vietnamese starfish <I>Protoreaster nodosus</I> on pro-inflammatory cytokine (IL-12 p40, IL-6, and TNF-α) production in LPS-stimulated bone marrow-derived dendritic cells (BMDCs) using enzyme-linked immunosorbent assays (ELISA).</P><P><B>Results</B></P><P>The methanolic extract and dichloromethane fraction exerted potent inhibitory effects on the production of all three pro-inflammatory cytokines, with IC<SUB>50</SUB> values ranging from 0.60 ± 0.01 to 26.19 ± 0.64 μg/mL. Four highly pure steroid derivatives <B>(1–4)</B> were isolated from the dichloromethane fraction and water layer of <I>P. nodosus</I>. Potent inhibitory activities were also observed for (25<I>S</I>) 5α-cholestane-3β,4β,6α,7α,8β,15α,16β,26-octol <B>(3)</B> on the production of IL-12 p40 and IL-6 (IC<SUB>50s</SUB> = 3.11 ± 0.08 and 1.35 ± 0.03 μM), and for (25<I>S</I>) 5α-cholestane-3β,6α,8β,15α,16β,26-hexol <B>(1)</B> and (25<I>S</I>) 5α-cholestane-3β,6α,7α,8β,15α,16β,26-heptol <B>(2)</B> on the production of IL-12 p40 (IC<SUB>50s</SUB> = 0.01 ± 0.00 and 1.02 ± 0.01 μM). Moreover, nodososide <B>(4)</B> exhibited moderate inhibitory effects on IL-12 p40 and IL-6 production.</P><P><B>Conclusion</B></P><P>This is the first report of the anti-inflammatory activity from the starfish <I>P. nodosus</I>. The main finding of this study is the identification oxygenated steroid derivatives from <I>P. nodosus</I> with potent anti-inflammatory activities that may be developed as therapeutic agents for inflammatory diseases.</P>
Anti-inflammatory Asterosaponins from the Starfish <i>Astropecten monacanthus</i>
Thao, Nguyen Phuong,Cuong, Nguyen Xuan,Luyen, Bui Thi Thuy,Thanh, Nguyen Van,Nhiem, Nguyen Xuan,Koh, Young-Sang,Ly, Bui Minh,Nam, Nguyen Hoai,Kiem, Phan Van,Minh, Chau Van,Kim, Young Ho American Chemical Society and American Society of 2013 Journal of natural products Vol.76 No.9
<P>Four new asterosaponins, astrosteriosides A–D (<B>1</B>–<B>3</B> and <B>5</B>), and two known compounds, psilasteroside (<B>4</B>) and marthasteroside B (<B>6</B>), were isolated from the MeOH extract of the edible Vietnamese starfish <I>Astropecten monacanthus</I>. Their structures were elucidated by chemical and spectroscopic methods including FTICRMS and 1D and 2D NMR experiments. The effects of the extracts and isolated compounds on pro-inflammatory cytokines were evaluated by measuring the production of IL-12 p40, IL-6, and TNF-α in LPS-stimulated bone marrow-derived dendritic cells. Compounds <B>1</B>, <B>5</B>, and <B>6</B> exhibited potent anti-inflammatory activity comparable to that of the positive control. Further studies are required to confirm efficacy <I>in vivo</I> and the mechanism of effects. Such potent anti-inflammatory activities render compounds <B>1</B>, <B>5</B>, and <B>6</B> important materials for further applications including complementary inflammation remedies and/or functional foods and nutraceuticals.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jnprdf/2013/jnprdf.2013.76.issue-9/np400492a/production/images/medium/np-2013-00492a_0005.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/np400492a'>ACS Electronic Supporting Info</A></P>
NATIONAL DOI MOI IN VIETNAM AND EXPERIENCE FOR ITS FURTHER REFORM STAGES
Vi Van Thao 한국베트남학회 2023 베트남연구 Vol.21 No.1
In the face of complicated situations in the world and in the country, the State of Vietnam has made important decisions in orienting the country's development path, which is to change the thinking about the country's leadership carried out "carried out inclusive national Doi Moi in December 1986". This is considered an important milestone in the process of bringing the country out of underdevelopment, improving people's living standards, and enhancing Vietnam's position in the international arena. The article has summarized the process of national Doi Moi of Vietnam, including the necessity to carry out doi moi; innovation process; achievements and limitations in the process of national renewal after 36 years. Finally, the author proposes urgent and important lessons to continue implementing the country's doi moi process in the next stages, which are forecasted to have many important changes in geopolitics, economy, etc. In addition, there are many complicated problems in the country that need to be solved such as corruption, environmental pollution, and the economy is in a difficult period.
Ta, Van-Thao,Park, Juhun,Park, Eun Jin,Hong, Seunghun American Chemical Society 2014 ACS NANO Vol.8 No.3
<P>We report a <I>reusable</I> floating-electrode sensor based on aligned semiconducting single-walled carbon nanotubes for the <I>quantitative</I> monitoring of the electrophysiological responses from a <I>nonadherent</I> cell. This method allowed us to monitor and distinguish the real-time responses from <I>normal</I> and <I>small-cell lung cancer</I> (SCLC) cells to the addition of nicotine. The difference was attributed to the overexpressed nicotinic acetylcholine receptors (nAChRs) in the SCLC cells. The sensor was also utilized to monitor the effect of various drugs on the cells. The treatment with inhibitors such as genistin or daidzein was found to reduce Ca<SUP>2+</SUP> influx in SCLC cells. Moreover, tamoxifen, though known as the antiestrogen compound, was found to only partly block the binding of daidzein to nAChRs. Significantly, the activities of <I>multiple</I> individual cells could be measured repeatedly using a <I>single</I> sensor device, enabling statistically meaningful measurements without errors from the device-to-device variations of the sensor characteristics. This capability of the <I>quantitative</I> monitoring of <I>nonadherent</I> cells should be a major breakthrough for electrophysiology research and various biomedical applications such as drug screening and therapeutic monitoring.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/ancac3/2014/ancac3.2014.8.issue-3/nn4053155/production/images/medium/nn-2013-053155_0006.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/nn4053155'>ACS Electronic Supporting Info</A></P>
Ngo, Van T.H.,Hoang, Van-Hai,Tran, Phuong-Thao,Van Manh, Nguyen,Ann, Jihyae,Kim, Eunhye,Cui, Minghua,Choi, Sun,Lee, Jiyoun,Kim, Hee,Ha, Hee-Jin,Choi, Kwanghyun,Kim, Young-Ho,Lee, Jeewoo Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.12
<P><B>Abstract</B></P> <P>Glutamyl cyclase (QC) is a promising therapeutic target because of its involvement in the pathogenesis of Alzheimer’s disease. In this study, we developed novel QC inhibitors that contain 3-aminoalkyloxy-4-methoxyphenyl and 4-aminoalkyloxyphenyl groups to replace the previously developed pharmacophore. Several potent inhibitors were identified, showing IC<SUB>50</SUB> values in a low nanomolar range, and were further studied for <I>in vitro</I> toxicity and <I>in vivo</I> activity. Among these, inhibitors <B>51</B> and <B>53</B> displayed the most potent Aβ<SUB>N3pE−40</SUB>-lowering effects in <I>in vivo</I> acute model with reasonable BBB penetration, without showing cytotoxicity and <I>h</I>ERG inhibition. The molecular modeling analysis of <B>53</B> indicated that the salt bridge interaction and the hydrogen bonding in the active site provided a high potency. Given the potent activity and favorable BBB penetration with low cytotoxicity, we believe that compound <B>53</B> may serve as a potential candidate for anti-Alzheimer’s agents.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Hoang, Van-Hai,Tran, Phuong-Thao,Cui, Minghua,Ngo, Van T. H.,Ann, Jihyae,Park, Jongmi,Lee, Jiyoun,Choi, Kwanghyun,Cho, Hanyang,Kim, Hee,Ha, Hee-Jin,Hong, Hyun-Seok,Choi, Sun,Kim, Young-Ho,Lee, Jeewoo American Chemical Society 2017 Journal of medicinal chemistry Vol.60 No.6
<P>Glutaminyl cyclase (QC) has been implicated in the formation of toxic amyloid plaques by generating the N-terminal pyroglutamate of beta-amyloid peptides (pGlu-A beta) and thus may participate in the pathogenesis of Alzheimer's disease (AD). We designed a library of glutamyl cyclase (QC) inhibitors based on the proposed binding mode of the preferred substrate, A beta 3E-42. An in vitro structure-activity relationship study identified several excellent QC inhibitors demonstrating 5- to 40-fold increases in potency compared to a known QC inhibitor. When tested in mouse models of AD, compound 212 significantly reduced the brain concentrations of pyroform A beta and total A beta and restored cognitive functions. This potent A beta-lowering effect was achieved by incorporating an additional binding region into our previously established pharmacophoric model, resulting in strong-interactions with the carboxylate group of Glu327 in the QC binding site. Our study offers useful insights in designing novel QC inhibitors as a potential treatment option for AD.</P>
Ngo, Van T.H.,Hoang, Van-Hai,Tran, Phuong-Thao,Ann, Jihyae,Cui, Minghua,Park, Gyungseo,Choi, Sun,Lee, Jiyoun,Kim, Hee,Ha, Hee-Jin,Choi, Kwanghyun,Kim, Young-Ho,Lee, Jeewoo Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.5
<P><B>Abstract</B></P> <P>Pyroglutamate-modified amyloid β peptides (pGlu-Aβ) are highly neurotoxic and promote the formation of amyloid plaques. The pGlu-Aβ peptides are generated by glutaminyl cyclase (QC), and recent clinical studies indicate that QC represents an alternative therapeutic target to treat Alzheimer’s disease (AD). We have previously developed a series of QC inhibitors with an extended pharmacophoric scaffold, termed the Arg-mimetic D-region. In the present study, we focused on the structure activity relationship (SAR) of analogues with modifications in the D-region and evaluated their biological activity. Most compounds in this series exhibited potent activity in vitro, and our SAR analysis and the molecular docking studies identified compound <B>202</B> as a potential candidate because it forms an additional hydrophobic interaction in the <I>h</I>QC active site. Overall, our study provides valuable insights into the Arg-mimetic pharmacophore that will guide the design of novel QC inhibitors as potential treatments for AD.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>