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Ha, M.T.,Tran, M.H.,Ah, K.J.,Jo, K.J.,Kim, J.,Kim, W.D.,Cheon, W.J.,Woo, M.H.,Ryu, S.H.,Min, B.S. Pergamon Press 2016 Bioorganic & medicinal chemistry letters Vol.26 No.12
Detailed phytochemical investigation from the root bark of Morus alba resulted in the isolation of eleven new compounds, including seven 2-arylbenzofuran derivatives (morusalfurans A-G), three flavonoids (morusalnols A-C), and one geranylated stilbene (morusibene A), as well as 22 known compounds. The structures of the identified compounds were elucidated based on a comprehensive analysis of spectroscopic data and Mosher's method. Compounds 2, 3, 6-8, 11, 23, 24, and 29 showed potent inhibition of PL in comparison with the positive control treatment (orlistat, IC<SUB>50</SUB>=0.012μM), with IC<SUB>50</SUB> values ranging from 0.09 to 0.92μM.
Chi K. Hoang,Cuong H. Le,Dat T. Nguyen,Hang T. N. Tran,Chinh V. Luu,Huong M. Le,Ha T. H. Tran 한국균학회 2023 Mycobiology Vol.51 No.4
Genus Penicillium comprising the most important and extensively studied fungi has beenwell-known as a rich source of secondary metabolites. Our study aimed to analyze andinvestigate biological activities, including in vitro anti-cancer, anti-inflammatory and anti-diabeticproperties, of metabolites from a marine-derived fungus belonging to P. levitum. Thechemical compounds in the culture broth of P. levitum strain N33.2 were extracted withethyl acetate. Followingly, chemical analysis of the extract leaded to the isolation of threeergostane-type steroid components, namely cerevisterol (1), ergosterol peroxide (2), and(3b,5a,22E)-ergosta-6,8(14),22-triene-3,5-diol (3). Among these, (3) was the most potent cytotoxicagainst human cancer cell lines Hep-G2, A549 and MCF-7 with IC50 values of 2.89,18.51, and 16.47 mg/mL, respectively, while the compound (1) showed no significant effectagainst tested cancer cells. Anti-inflammatory properties of purified compounds were evaluatedbased on NO-production in LPS-induced murine RAW264.7 macrophages. As a result,tested compounds performed diverse inhibitory effects on NO production by the macrophages,with the most significant inhibition rate of 81.37 ± 1.35% at 25 mg/mL by the compound(2). Interestingly, compounds (2) and (3) exhibited inhibitory activities againstpancreatic lipase and a-glucosidase enzymes in vitro assays. Our study brought out newdata concerning the chemical properties and biological activities of isolated steroids from aP. levitum fungus.
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>
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>
진강규(G. Jin),박동진(D. Park),찬탄도(T. Tran),이현식(H. Lee),이윤형(Y. Lee),하윤수(Y. Ha) 한국마린엔지니어링학회 2009 한국마린엔지니어링학회 학술대회 논문집 Vol.2009 No.-
In this paper, we presents an algorithm which generates its high-resolution map using a low-resolution 3D map of the sea floor terrain and fractal theory. Each patch region is divided from the 3D map and its fractal dimension is extracted. And then with this information, each cell in a patch is reconstructed using the midpoint displacement method. The effectiveness of the proposed algorithm is tested on a fractal terrain map.