• Archives of Pharmacal Research
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• 제18권5호
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• pp.356-360
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• 1995

Two new 1-aryl-2-benzylmercapto-4-aryl-1,6-dihydro-1,3,5-triazine-6-thiones hvae been synthesized by known methods (Coerdeler et al., 1967). These triazines on treatment with thiourea as dealkylating agent, in acidic medium afforded the corresponding 1-ary-2-mercapto-4-aryl-1,6-dihydro-1,3,5-triazine-6-thione which on further reaction with different ${\alpha},{\;}{\beta}-unstaturated$ carbonyl compounds and aryl-cyanamide ydrochloride affordered the related adducts. Some of these compounds show appreciable antithyroidal activity.

• Bulletin of the Korean Chemical Society
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• 제27권1호
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• pp.93-98
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• 2006

Two new compounds 1'-(stigmast-11,20(21),25-trien 3$\alpha$,9$\alpha$-diolyl)-3'-(pimara-11,15-dien-3$\alpha$-olyl) glycerol (1) and stigmast-5-en-3$\alpha$,26-diol (2) along with known fatty acids n-hexacosanoic acid (3) and hexadecanoic acid (4), have been isolated from the methanol extract of rice hulls of Oryza sativa. The structures of the compounds were elucidated using 1D and 2D NMR spectral methods, viz; $^1H, ^{13}C, ^{13}C$-DEPT, $^1H-^1H$ COSY, $^1H-^{13}C$ HETCOR, HSQC and HMBC aided by IR, EIMS, FABMS and HRFABMS. Compound (1) showed inhibition to radish germination, growth of shoot and root length.

• 약학회지
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• 제40권6호
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• pp.690-696
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• 1996

It has been known that many kinds of cancer are caused by continued proliferation or abnormal differentiation. Thus, recent approaches to anticancer therapy have been focused on developing drugs that induce differentiation of cancer cells to normal cells. A typical differentiation agent, all trans-retinoic acid, is unsuitable for anticancer drug because all trans-retinoic acid produces unfavorable side effects and cytotoxicity in normal cells. Therefore, we have screened some new differentiation-inducing compounds obtained from marine organisms using F9 teratocarcinoma stem cells as a model system. We observed that fatty acid. glycolipid, saponin, sphingosine and sterol compounds of marine organisms had differentiation-inducing activity in F9 cells, were determined by morphological changes and Northern blot analysis. The expression of differentiation marker genes, such as laminin B1, type IV collagen and retinoic acid receptor beta were induced by treatment with those compounds.

• Journal of Ginseng Research
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• 제38권1호
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• pp.28-33
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• 2014

Background: Panax notoginseng has been used as a general tonic agent to invigorate human body for millennia in China and continued to be used until present. Methods: Some chromatographic methods were performed to isolate pure triterpenoids, and their structures were determined by nuclear magnetic resonance (NMR) experiments. Anti-diabetes activities of isolated compounds were evaluated through their inhibitory activity of protein tyrosine phosphatase 1B (PTP1B) enzyme. Results and Conclusion: Three new dammarane-type triterpenoids, notoginsenoside-LX (1), notoginsenoside-LY (2), and notoginsenoside-FZ (3) together with eighteen known compounds were isolated from the Panax notoginseng leaves. The structure-activity relationship of the compounds with dammaranetype triterpenoids and their PTP1B inhibitory activity were also reported. Results showed that compounds 2, 15, 20, and 21 can significantly inhibit the enzyme activity of PTP1B in a dose-dependent manner, with inhibitory concentration 50 ($IC_{50}$) values of $29.08{\mu}M$, $21.27{\mu}M$, $28.12{\mu}M$, and $26.59{\mu}M$, respectively. The results suggested that Panax notoginseng leaves might have potential as a new therapeutic agent for the treatment of diabetes.

• Biotechnology and Bioprocess Engineering:BBE
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• 제8권2호
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• pp.76-82
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• 2003

An increased understanding of apoptosis makes anti-apoptosis engineering possible, which is an approach used to inhibit apoptosis for the purpose of therapeutic, or industrial applications in the treatment of the diseases associated with increased apoptosis, or to improve the productivity of animal cell cultures, respectively. Some known anti-apoptosis proteins are the Bcl-2 family, IAP (inhibitor of apoptosis) and Hsps (heat shock proteins), with which anti-apoptosis engineering has progressed. This article reviews anti-apoptosis engineering using known anti-apoptosis compounds, and introduces a 30 K protein, isolated from silkworm hemolymph, as a novel anti-apoptotic protein, that Shows no homology with other known anti-apoptotic proteins. The regulation of apoptosis, using anti-apoptotic proteins and genes originating from the silkworm, Bombyx mori, may provide a new strategy in this field.

• 한국자원식물학회지
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• 제7권1호
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• pp.29-34
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• 1994

Two new 1,2-seco-1-nor-6((5 $\mapsto$ 10)abeo-picrasan-2,5-olideskeleton quassinoids, eurylactones A [1] and B [2], and two new $C_{19}$ skeleton quassinoids 3 and 4 were isolated from Eurycoma longifolia together with two known $C_{18}$ quassinoids 5 and 6. Their sttuctures were established by the spectral evidence.Many quassinoids have already been isolated (1-3) from the roots, wood, and leaves of Eurycoma longiolia Jack (Simaroubaceae) and have been used as a folk medicine insoutheast Asia. As part of a series of studies, we have further undertaken the chemicalinvestigation of the n-BuOH-soluble fraction of the MeOH extract and isolated two new1,2-seco-1-nor-6(5 $\mapsto$ 10)abeo-picrasane skeleton quassinoids 1 and 2, which have beenknown only in shinjulactone B (4,5) and yadanfiolide (6), two new $C_{19}$-type quasslnolds3 and 4, and two known C18-type quassinoids 5 and 6. In this paper, the structureelucidation and biosenetic relation of these compounds are described.

• Bulletin of the Korean Chemical Society
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• 제34권9호
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• pp.2675-2679
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• 2013

Activity-directed isolation of the methylene chloride fraction from the stems of Parthenocissus tricuspidata have led to the identification of two new compounds (1-2): 1-(2',3',5'-trihydroxyphenyl)-2-(4"-hydroxyphenyl)-ethane-1,2-(E)-epoxide (1, tricuspidatin A) and erythro-1-(3',5'-dihydroxyphenyl)-2-(4"-hydroxyphenyl)-ethane-1,2-diol (2, tricuspidatin B), together with four known compounds (3-6): ${\beta}$-sitosterol (3), nonacosan-1-ol (4), 3-(4-hydroxy-3-methoxyphenyl)-2-propenoic acid hexacosyl ester (5) and betulinic acid (6). Their chemical structures were elucidated based on spectroscopic (IR, UV, MS, 1D and 2D NMR) and physicochemical analyses. Compounds 1 and 2 showed strong DNA topoisomerase II inhibitory activity at both concentrations of 20 and $100{\mu}M$. In addition, 3 exhibited strong cytotoxic activity against the HT-29 and HepG2 cancer cell lines, and 6 showed strong cytotoxicity against the HT-29 and MCF-7 ones.

• Archives of Pharmacal Research
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• 제29권2호
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• pp.135-139
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• 2006

Activity-guided fractionation of the ethanol extract of the whole plant from Solanum lyratum resulted in the isolation of a new pregnane derivative glycoside, 16-dehydropregnenolone 3-O-${\alpha}$-L-rhamnopyranosyl-($1{\to}2$)-${\beta}$-D-glucopyranosid uronic acid (2), as well as other six known compounds: 16-dehydropregnenolone (1), allopregenolone (3), protocatechuic acid (4), vanillic acid (5), caffeic acid (6), and scopoletin (7). The structures of the isolated compounds were elucidated on the basis of their spectral data and chemical evidences. Compounds 1, 3, 4 were isolated for the first time from this plant. Cytotoxic activities of the isolated compounds were evaluated. Compound 1 exhibited significant cytotoxic activity against A375-S2, HeLa, SGC-7901, and Bel-7402 with $IC_{50}$ values of $13.1{\pm}0.9,\;21.5{\pm}1.0,\;40.2{\pm}0.7$, and $49.8{\pm}1.2\;{\mu}g/mL$, respectively.

• Natural Product Sciences
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• 제17권2호
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• pp.65-79
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• 2011

Reactive oxygen species potentially cause damage to cellular components including lipids, protein and DNA; this oxidative damage plays a key role in the pathogenesis of neurodegenerative disease, cardiovascular disease, metabolic disease and cancer. On the basis of the oxidative stress hypothesis, a number of studies have been performed to search for an efficient and safe antioxidant. Although in vitro studies have provided promising results, only a limited number of natural and synthetic antioxidants have been developed for clinical application due to their low efficacy and side-effects. Thus, the discovery of new antioxidants with marked efficacy and safety has attracted worldwide attention in recent decades. Since plants are recognized as important sources of natural antioxidants, our research has focused on the discovery of new naturally occurring antioxidants from medicinal plants. The purpose of this review is to open a new prospect in the field of search for natural antioxidants from medicinal plants by summarizing our recent findings. Using in vitro bioassay systems such as 2,2-diphenyl-1-picrylhydrazyl, superoxide radical scavenging tests and lipid peroxidation models, we have tested over than 350 species of medicinal plants for their antioxidant activity and selected several of them for further investigation. During the research on the discovery of effective natural antioxidants from the medicinal plants selected, we have isolated several new and known antioxidant compounds that include stilbene glycosides, phenolic glycosides, flavonoids, oligostilbenes, and coumarins. Our results suggest that the presence of antioxidant compounds in the medicinal plants might be associated with the traditional use to treat inflammation, cardiovascular disease and various chronic diseases.

• Biomolecules & Therapeutics
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• 제26권5호
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• pp.458-463
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• 2018

The phosphorylation of JNK is known to induce insulin resistance in insulin target tissues. The inhibition of JNK-JIP1 interaction, which interferes JNK phosphorylation, becomes a potential target for drug development of type 2 diabetes. To discover the inhibitors of JNK-JIP1 interaction, we screened out 30 candidates from 4320 compound library with In Cell Interaction Trap method. The candidates were further confirmed and narrowed down to five compounds using the FRET method in a model cell. Among those five compounds, Acebutolol showed notable inhibition of JNK phosphorylation and elevation of glucose uptake in diabetic models of adipocyte and liver cell. Structural computation showed that the binding affinity of Acebutolol on the JNK-JIP1 interaction site was comparable to the known inhibitor, BI-78D3. Our results suggest that Acebutolol, an FDA-approved beta blocker for hypertension therapy, could have a new repurposed effect on type 2 diabetes elevating glucose uptake process by inhibiting JNK-JIP1 interaction.