• Proceedings of the PSK Conference
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• 2003.04a
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• pp.243.2-244
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• 2003

The resistances to multiple antibiotics of strains of Gram-positive Staphylococci. methicillin-resistant Staphylo coccus aureus (MRSA), are now significant clinical problem. One of the major efforts of our laboratory has been the search and design and synthesis of novel lead compound for the purpose of obtaining highly potent anti-MRSA drug. Towards this end, we have recently reported the isolation of a potent anti-MRSA drug. (omitted)

• Natural Product Sciences
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• v.9 no.3
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• pp.154-157
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• 2003

In the present study, the roots of Sesbania grandiflora L. Poiret (Papilionaceae) were successively extracted with petroleum ether (PE), chloroform (CE), methanol (ME) and water (AE) by soxhlet extraction. The extracts were vacuum dried and screened for analgesic, antidiarrhoeal, antibacterial (Staphylococcus epidermidis, Staphylococcus aureus, Micrococcus luteus, Bacillus cereus, and Klebsiella pneumonia) and antifungal (Candida albicans and Aspergillus niger) activity. All the extracts exhibited potent, dose dependant (40 and 80 mg/kg) and significant analgesic and antidiarrhoeal activity in the order of AE>PE>CE>ME and ME>PE>AE>CE respectively. AE at the experimental dose was found to exhibit more potent analgesic activity than standard drug. All the extracts exhibited significant antibacterial $(100\;{\mu}g/ml)$ and antifungal activity $(50\;and\;100\;{\mu}g/ml)$. ME exhibited the most potent antibacterial activity.

• YAKHAK HOEJI
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• v.43 no.3
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• pp.334-341
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• 1999

Thyroid peroxidase is a biochemical target protein for the antithyroid drugs. Ethanol extracts from one hundred and thirty seven natural products were screened for the inhibition of thyroid peroxidase activity. Thyroid peroxidase was purified from porcine thyroids, and the inhibition of peroxidase activity was evaluated using guaiacol oxidation (C-C coupling) assay. Twenty one natural products expressed a remarkable inhibition (>50%) of peroxidase activity at $330{\mu\textrm{g}}$ solid weight/m. The 50% inhibitory concentration ($IC_{50}$) of 70% ethanol extract from six potent natural products ranged from 3.1 to $31.2{\;}{\mu\textrm{g}}$ solid weight/m, in contrast to the range ($0.33~0.54{\;}{\mu\textrm{g}}/ml$) of $IC_{50}$ values fro catechin and epigallocatechin gallate as positive controls. Noteworthy, the extract of Camellia taliensis showed irreversible inhibition of the enzyme. It is suggested that extract from some natural products such as Camellia taliensis, Rheum undulatum or Euphorbia perinensis, exhibiting a potent inhibition of peroxidase activity, may be developed as sources of potent antithyroid agents.

• Archives of Pharmacal Research
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• v.23 no.4
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• pp.288-301
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• 2000

A series of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives (7a-h) and 16m-o) were prepared, and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia cell line P388, and human gastric carcinoma cell lines SNU-1 and SNU-16). These compounds showed potent cytotoxicity against all of three cell lines tested, and especially SNU-16 was sensitive to them. 2-Aryl (7g,h) and 2-piperazinyl benzimidazole-4,7-dione derivative (I6 m) were more potent than mitomycin C against P388 and SNU-16. Among benzimidazole-4,7-dione derivatives with alkyl group at position 2, 7a had the most potent cytotoxicity against all of the cell lines tested.

• Bulletin of the Korean Chemical Society
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• v.32 no.3
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• pp.821-828
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• 2011

Design and synthesis of new 3,4-diarylpyrazole-1-carboxamide derivatives are described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the synthesized compounds showed moderate activity against A375, compared with Sorafenib. On the other hand, compounds Ia, Ie, IIb, and IIh were more potent than Sorafenib. In addition, compound IIa was equipotent to Sorafenib. Among all of these derivatives, compound IIb which has diethylamino and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIb into the domain of V600E-b-Raf and the binding mode was studied.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.337.2-337.2
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• 2002

Conjugated linoleic acid (CLA) is a potent inhibitor of mammary carcinogenesis. Cancer cells produce various angiogenic factors which stimulate host vascular endothelial cell mitogenesis and chemotaxis for their growth and metastasis. Basic fibroblast growth factor (bFGF) is a potent angiogenic factor that is expressed in many tumors. In this study. we found that CLA decreased bFGF-induced endothelial cell proliferation and DNA synthesis in a dose-dependent manner. However, CLA did not inhibit endothelial cell migration. Furthermore CLA showed a potent inhibitory effect on embryonic vasculogenesis and bF GF-induced angiogenesis in vivo. Collectively. these results suggest that CLA selectively inhibis the active proliferating endothelial edll induced by bFGF. which may explain its anti-carcinogenix properties in vivo.

• Bulletin of the Korean Chemical Society
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• v.23 no.2
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• pp.351-354
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• 2002

A number of bis-2-oxo amide triacylglycerol analogues, a recently reported potent human gastric lipase inhibitor and its new analogues, have been prepared starting from 1,3-dibromo-2-propanol utilizing acyl cyanophosphorane methodology as a key step in a convergent manner. The key coupling reaction has been accomplished at -$78^{\circ}C$ between 1,3-diamino-2-propanol derivative and the labile diketo nitriles, derived from acyl cyanotriphenylphosphoranes upon oxidizing with $O_3$, under mild condition in moderate yields.

• Advances in Traditional Medicine
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• v.9 no.4
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• pp.335-338
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• 2009

Aerial parts of Sida rhombifolia Linn. (Malvaceae) were extracted successively using various solvents and screened for various parameters of antiarthritic activity such as adjuvant-induced arthritis, motor performance, and histopathological study. The ethanol and the aqueous extracts showed potent activity; further these extracts were fractionated by using column chromatography. The fraction ET1 isolated from ethanol extract showed the most potent antiarthritic activity.

• YAKHAK HOEJI
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• v.45 no.2
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• pp.214-219
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• 2001

Nineteen hydrolysable tannins isolated from the Euphorbia helioscopia (Euphorbiaceae) were tested for the inhibitory effect on mushroom tyrosinase activity in vitro. Inhibitory effect of gallotannin group exhibited more potent than that of phenolcarboxylic acid and ellagitannin groups against the enzyme activity. The inhibitory activity by pentagalloyl glucose on mushroom tyrosinase was more potent ($IC_{50}$/, 4.9 $\mu$M) than that of kojic acid ($IC_{50}$/, 8.7 $\mu$M).

• Archives of Pharmacal Research
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• v.20 no.2
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• pp.158-170
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• 1997

New HMG-CoA reductase inhibitors, in which 3-substituted 4, 5-polymethylenepyrazoles are employed as a hydrophobic anchor connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to exhibit significant inhibitory activity comparable to mevinolin. The most potent enzyme inhibitor $(11cc, IC_{50}=0.01{\mu}M)$ is 4-fold more potent than lovastatin.