http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Thao T. D. Tran,Thinh D. Luu,Beom‑Jin Lee,Phuong H. L. Tran 한국약제학회 2019 Journal of Pharmaceutical Investigation Vol.49 No.1
Sprouted grains, which is a natural polysaccharide, is the subject of increasing scientific interest due to many benefits for human health. The aim of the present work was to develop sprouted rice (SR) as a safe and useful material for application in dissolution enhancement of anticancer poorly water-soluble drugs such as curcumin by solid dispersions (SDs). SDs were prepared with pure SR and modified sprouted rice (MSR) by the melting method. The dissolution rate, drug crystallinity changes, molecular interactions and wettability were characterized and compared between the formulations. The use of MSR could result in a promising system for improving the dissolution rate of poorly water-soluble drugs. MSR could induce a greater amorphous state and improved wettability of drugs for dissolution enhancement compared to SR. Although both SR and MSR showed hydrogen bonding interaction, insignificant differences between SR and MSR were observed. We found that the crystallinity, interactions and wettability of the drug were significantly affected and modulated by MSR.
Endemic Severe Fever with Thrombocytopenia Syndrome, Vietnam
Tran, Xuan Chuong,Yun, Yeojun,Van An, Le,Kim, So-Hee,Thao, Nguyen T. Phuong,Man, Phan Kim C.,Yoo, Jeong Rae,Heo, Sang Taek,Cho, Nam-Hyuk,Lee, Keun Hwa U.S. Department of Health and Human Services * Cen 2019 Emerging Infectious Diseases Vol.25 No.5
Anti-inflammatory Triterpenoid Saponins from the Stem Bark of <i>Kalopanax pictus</i>
Quang, Tran H.,Ngan, Nguyen T. T.,Minh, Chau V.,Kiem, Phan V.,Nhiem, Nguyen X.,Tai, Bui H.,Thao, Nguyen P.,Tung, Nguyen H.,Song, Seok B.,Kim, Young H. American Chemical Society and American Society of 2011 Journal of natural products Vol.74 No.9
<P>Five new compounds, 16,23,29-trihydroxy-3-oxo-olean-12-en-28-oic acid (<B>1</B>), 4,23,29-trihydroxy-3,4-<I>seco</I>-olean-12-en-3-oate-28-oic acid (<B>2</B>), 3β,6β,23-trihydroxyolean-12-en-28-oic acid 28-<I>O</I>-β-<SMALL>d</SMALL>-glucopyranoside (<B>3</B>), 3-<I>O</I>-[2,3-di<I>-O</I>-acetyl-α-<SMALL>l</SMALL>-arabinopyranosyl]hederagenin 28-<I>O</I>-α-<SMALL>l</SMALL>-rhamnopyranosyl-(1→4)-β-<SMALL>d</SMALL>-glucopyranosyl-(1→6)-β-<SMALL>d</SMALL>-glucopyranoside (<B>4</B>), and 3-<I>O</I>-[3,4-di-<I>O</I>-acetyl-α-<SMALL>l</SMALL>-arabinopyranosyl]hederagenin 28-<I>O</I>-α-<SMALL>l</SMALL>-rhamnopyranosyl-(1→4)-β-<SMALL>d</SMALL>-glucopyranosyl-(1→6)-β-<SMALL>d</SMALL>-glucopyranoside (<B>5</B>), as well as 10 known compounds (<B>6</B>–<B>15</B>), were isolated from the stem bark of <I>Kalopanax pictus</I>. Compounds <B>1</B>–<B>5</B> and <B>7</B>–<B>14</B> inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC<SUB>50</SUB> values ranging from 0.6<B></B>to 16.4 μM. Furthermore, the transcriptional inhibitory function of these compounds was confirmed on the basis of decreases in COX-2 and iNOS gene expression in HepG2 cells. The structure–activity relationship of the compounds with respect to anti-inflammatory activity is also discussed.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jnprdf/2011/jnprdf.2011.74.issue-9/np200382s/production/images/medium/np-2011-00382s_0005.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/np200382s'>ACS Electronic Supporting Info</A></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/np200382s'>ACS Electronic Supporting Info</A></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>
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>
Khanh B. Vu,Thanh Khoa Phung,Thao T.T. Tran,Clement Mugemana,Ha N. Giang,Truong Le Phuc Nhi 한국공업화학회 2021 Journal of Industrial and Engineering Chemistry Vol.97 No.-
Polystyrene was synthesized and applied as a template for fabricating hollow silica nanoparticles. Organic solvent and water were used as a solvent and an anti-solvent, respectively, to produce thepolystyrene nanoparticles via. nanoprecipitation technique. The influence of precipitation method (oneshotor drop), solvent for dissolution of polystyrene, and concentration of polystyrene or CTAB linker onthe diameter of polystyrene nanoparticles was investigated. The hollow silica nanoparticles werefabricated using the as-made polystyrene nanoparticles as a template with the help of CTAB linker. Polystyrene was recovered by the extraction of polystyrene@SiO2 composite with the tetrahydrofuransolvent, and the recovered polystyrene was re-used to make the polystyrene nanoparticles as a templatefor fabricating hollow silica nanoparticles. Our study can be applied for other types of polymericmaterials as long as those polymeric materials form nanoparticles via. nanoprecipitation technique. Incomparison with the polystyrene hard template prepared by emulsion polymerization, the size ofpolystyrene nanoparticles produced by the nanoprecipitation technique can be well-tuned by changingthe polystyrene and linker concentrations.
Hoang, Van-Hai,Ngo, Van T. H.,Cui, Minghua,Manh, Nguyen Van,Tran, Phuong-Thao,Ann, Jihyae,Ha, Hee-Jin,Kim, Hee,Choi, Kwanghyun,Kim, Young-Ho,Chang, Hyerim,Macalino, Stephani Joy Y.,Lee, Jiyoun,Choi, S American Chemical Society 2019 Journal of medicinal chemistry Vol.62 No.17
<P>Alzheimer’s disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consists of various factors; thus, there is a call for alternative approaches to tackle the multifaceted aspects of AD. Among the potential alternative targets, we aim to focus on glutaminyl cyclase (QC), which reduces the toxic pyroform of β-amyloid in the brains of AD patients. On the basis of a putative active conformation of the prototype inhibitor <B>1</B>, a series of N-substituted thiourea, urea, and α-substituted amide derivatives were developed. The structure-activity relationship analyses indicated that conformationally restrained inhibitors demonstrated much improved QC inhibition in vitro compared to nonrestricted analogues, and several selected compounds demonstrated desirable therapeutic activity in an AD mouse model. The conformational analysis of a representative inhibitor indicated that the inhibitor appeared to maintain the Z-E conformation at the active site, as it is critical for its potent activity.</P> [FIG OMISSION]</BR>
Baek, Namhyun,Oh, Ga-Hui,Park, Chulhun,Tran, Thuy Thi Thanh,Park, Young Joon,Oh, Euichaul,Le, Hau,Tran, Thao T.D.,Park, Jun-Bom,Lee, Beom-Jin Elsevier 2018 Journal of drug delivery science and technology Vol.43 No.-
<P>The aim of this new work was to improve the dissolution rate of poorly water-soluble cilostazol (CLT) by adsorbing dissolved drug molecules onto the surface of undissolved carriers via reprecipitation and deposition process as the solvent (methylene chloride) was evaporated. The adsorption mixtures of CLT with Aerosil 300 and lactose monohydrate provided better drug dissolution rate as compared to mannitol. However, Aerosil-based adsorption powders were unable to be compressed into tablet due to low and unsatisfactory compressibility. The optimized CLT-loaded tablets containing lactose-based adsorption powders displayed almost complete dissolution within 90 min and showed significantly higher dissolution in intestinal fluid (pH 6.8) containing 0.2% sodium lauryl sulfate than the control tablet and the commercial reference product Pletaal (R) (Otsuka). Differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) indicated that the crystalline property of CLT remained in adsorption powders with diminutive peak intensity. Fourier transform infrared spectroscopy (FT-IR) spectra indicated that the intermolecular hydrogen bond was formed between drug molecule and lactose monohydrate. Field-emission scanning electron microscope (Fe-SEM) clearly confirmed that CLT crystals with reduced size around 10 mu m were adsorbed and deposited onto the surface of adsorbent material.</P>
Oh, Seung-Jin,Shin, Yiseul,Tran, T Thao,Lee, Dong Woo,Yoon, Anne,Halasyamani, P Shiv,Ok, Kang Min American Chemical Society 2012 Inorganic Chemistry Vol.51 No.19
<P>Solid solutions of the noncentrosymmetric (NCS) Aurivillius phases, Bi(4-x)La(x)Ti(3)O(12) (x = 0, 0.25, 0.50, 0.75), have been synthesized through standard solid-state reactions and structurally characterized by powder X-ray and neutron diffractions. These materials crystallize in the orthorhombic space group B2cb (No. 41) and exhibit layered perovskite structures with both (Bi(2)O(2))(2+) fluorite-like units and [A(n-1)B(n)O(3n+1)](2-) (n = 3) blocks. As the amount of La(3+) cations increases, the polarization arising from the Bi(3+) positions, especially the A sites of the perovskite units, continuously decreases in the reported materials. Powder second-harmonic generation (SHG) measurements on Bi(4-x)La(x)Ti(3)O(12) using 1064 nm radiation revealed frequency-doubling efficiencies ranging from 200 to 50 times that of 관-SiO(2). Converse piezoelectric measurements resulted in d(33) values of 19 and 13 pm V(-1) for Bi(4)Ti(3)O(12) and Bi(3.5)La(0.5)Ti(3)O(12), respectively. The magnitudes of the SHG efficiency and piezoelectric response are strongly dependent on the asymmetric coordination environment attributable to the lone pairs on Bi(3+). Structure-property relationships along with the influence of the doped foreign cation on the associated NCS properties are discussed.</P>