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Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta.
Na, Minkyun,Kim, Bo Yeon,Osada, Hiroyuki,Ahn, Jong Seog Taylor Francis 2009 Journal of enzyme inhibition and medicinal chemist Vol.24 No.4
<P>Protein tyrosine phosphatase 1B (PTP1B) appears to be an attractive target for the development of new drugs for type 2 diabetes and obesity. In our preliminary test, a MeOH extract of the stem barks of Sorbus commixta Hedl. (Rosaceae) showed strong PTP1B inhibitory activity. Bioassay-guided fractionation of the MeOH extract resulted in the isolation of two lupane-type triterpenes, lupenone (1) and lupeol (2). Compounds 1 and 2 inhibited PTP1B with IC(50) values of 13.7 +/- 2.1 and 5.6 +/- 0.9 microM, respectively. Kinetic studies revealed that both the compounds 1 and 2 are non-competitive inhibitors of PTP1B that decrease V(max) values with no effect on K(m) values.</P>
( Mi Na Song ),( Pyong Gon Moon ),( Jeong Eun Lee ),( Minkyun Na ),( Wonku Kang ),( Yee Soo Chae ),( Ji Young Park ),( Hoyong Park ),( Moon Chang Baek ) 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
This study presents a proteomic method that differentiates between matched normal and breast tumor tissues from ductal carcinoma in situ (DCIS) and invasive carcinoma from Korean women, to identify biomarker candidates and to understand pathogenesis of breast cancer in protein level. Proteins from tissues obtained by biopsy were extracted by RIPA buffer, digested by the gel-assisted method, and analyzed by nano-UPLC-MS/MS. From proteomic analysis based on label-free quantitation strategy, a non-redundant list of 298 proteins was identified from the normal and tumor tissues, and 244 proteins were quantified using IDEAL-Q software. Hierarchical clustering analysis showed two patterns classified as two groups, invasive carcinoma and DCIS, suggesting a difference between two carcinoma at the protein expression level as expected. Differentially expressed proteins in tumor tissues compared to the corresponding normal tissues were related to three biological pathways: antigen-processing and presentation, glycolysis/gluconeogenesis, and complement and coagulation cascades. Among them, the up-regulation of calreticulin (CRT) and protein disulfide isomerase A3 (PDIA3) was confirmed by Western blot analysis. In conclusion, this study showed the possibility of identifying biomarker candidates for breast cancer using tissues and might help to understand the pathophysiology of this cancer at the protein level.
Jang, JunPil,Na, MinKyun,Thuong, Phuong Thien,Njamen, Dieudonné,Mbafor, Joseph Tanyi,Fomum, Zacharias Tanee,Woo, Eun-Rhan,Oh, Won Keun The Pharmaceutical Society of Japan 2008 Chemical & pharmaceutical bulletin Vol.56 No.1
<P>Phytochemical study on an EtOAc-soluble extract of the root bark of <I>Erythrina mildbraedii</I> resulted in the isolation of six prenylated flavonoids 1—6. Based on physicochemical and spectroscopic analyses, their structures were determined to be new natural products licoflavanone-4′-<I>O</I>-methyl ether (1), 2′,7-dihydroxy-4′-methoxy-5′-(3-methylbut-2-enyl)isoflavone (2), and (3<I>R</I>)-2′,7-dihydroxy-3′-(3-methylbut-2-enyl)-2‴,2‴-dimethylpyrano[5‴,6‴ :4′,5′]isoflavan (3), along with three known compounds erythrinin B (4), abyssinin II (5), and parvisoflavone B (6). All the isolates, except for compound 4, inhibited PTP1B activity <I>in vitro</I> with IC<SUB>50</SUB> values ranging from 5.3 to 42.6 μ<SMALL>M</SMALL>. This result further suggests that the prenyl group on the B ring of flavonoids plays an important role in suppressing the enzyme PTP1B.</P>
PTP1B inhibitory activity of kaurane diterpenes isolated from <i>Siegesbeckia glabrescens</i>
Kim, Sohee,Na, Minkyun,Oh, Hyuncheol,Jang, Junpil,Sohn, Cheon Bae,Kim, Bo Yeon,Oh, Won Keun,Ahn, Jong Seog Taylor Francis 2006 Journal of enzyme inhibition and medicinal chemist Vol.21 No.4
<P>Protein tyrosine phosphatase 1B (PTP1B) is considered as a therapeutic target for the treatment of diabetes and obesity. In our preliminary screening study, a MeOH extract of the aerial part of <I>Siegesbeckia glabrescens</I> was found to inhibit PTP1B activity at 30 μg/mL. Bioassay‐guided fractionation led to the isolation of two active diterpenes, <I>ent</I>-16&bgr;H,17-isobutyryloxy-kauran-19-oic acid (<B>1</B>) and <I>ent</I>-16&bgr;H,17-acetoxy-18-isobutyryloxy-kauran-19-oic acid (<B>2</B>), along with <I>ent</I>-16&bgr;H,17-hydroxy-kauran-19-oic acid (<B>3</B>). Compounds <B>1</B> and <B>2</B> inhibited the PTP1B activity with IC<SUB>50</SUB> values of 8.7 ± 0.9 and 30.6 ± 2.1 μM, respectively. Kinetic studies suggest that both <B>1</B> and <B>2</B> are non-competitive inhibitors of PTP1B. However, compound <B>3</B> substituted with a hydroxyl group at C-17 in kaurane-type showed no inhibitory effects towards PTP1B.</P>
Significance of endangered and threatened plant natural products in the control of human disease
Ibrahim, Mohamed Ali,Na, MinKyun,Oh, Joonseok,Schinazi, Raymond F.,McBrayer, Tami R.,Whitaker, Tony,Doerksen, Robert J.,Newman, David J.,Zachos, Louis G.,Hamann, Mark T. National Academy of Sciences 2013 PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF Vol.110 No.42
<P>One in five of the world’s plant species is threatened with extinction according to the 2010 first global analysis of extinction risk. Tilman et al. predicted a massive ecological change to terrestrial plants within the next 50–100 y, accompanied by an increase in the number of global plant species facing extinction [Tilman D, et al. (2001) <I>Proc Natl Acad Sci USA</I> 98(10):5433–5440]. Most of the drug-producing plant families contain endangered species never previously studied for their utility to human health, which strongly validates the need to prioritize protection and assessment of these fragile and endangered groups [Zhu F, et al. (2011) <I>Proc Natl Acad Sci USA</I> 108(31):12943–12948]. With little prior attention given to endangered and rare plant species, this report provides strong justification for conservation of the rare plant <I>Diplostephium rhododendroides</I> Hieron., as well as other potential drug-producing endangered species in this and other groups.</P>
경북산 지황과 중국산 지황의 Catalpol 함량 비교
주미,장해연,나민균 충남대학교 약학대학 의약품개발연구소 2013 藥學論文集 Vol.28 No.-
Rehmanniae Radix (Scrophulariaceae) has been traditionally used to treat hemoptysis, polydipsia, diabetes, anemia, palpitation, insomnia, and menstrual disorders. To compare the Rehmanniae Radix produced from Gyeongbuk with that of Chinese, a quantitative analysis on the major component, catalpol, was preformed by reversed-phase HPLC. Using a Luna C18(2) column, we carried out quantitative analysis with an isocratic solvent of acetonitrile and 0.1% phosphoric acid in water (2.5:97.5). Our results demonstrated that the content of catalpol in the Gyeongbuk's Rhemanniae Radix was 1.8 times higher than that of Chinese.
Bajpai, Vivek K.,Na, Minkyun,Kang, Sun Chul Elsevier 2010 Food and chemical toxicology Vol.48 No.7
<P><B>Abstract</B></P> <P>In an attempt to isolate bioactive substances, ethyl acetate cone extract of <I>Metasequoia glyptostroboides</I> was subjected to a column chromatographic analysis that resulted in isolation of an abietane type diterpenoid, taxoquinone. Its structure was elucidated by spectroscopic means. In further, taxoquinone showed potential antibacterial effect as diameters of zones of inhibition against foodborne pathogenic bacteria such as <I>Listeria monocytogenes</I> ATCC 19166, <I>Salmonella typhimurium</I> KCTC 2515, <I>Salmonella enteritidis</I> KCTC 2021, <I>Escherichia coli</I> ATCC 8739, <I>E. coli</I> O157:H7 ATCC 43888, <I>Enterobacter aerogenes</I> KCTC2190, <I>Staphylococcus aureus</I> ATCC 6538 and <I>S. aureus</I> KCTC 1916, which were found in the range of 10.6–15.8mm. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of taxoquinone against the employed bacterial pathogens were found in the range of 62.5–250 and 125–500μg/ml. Also the compound had strong antibacterial effect on the viable counts of the tested bacteria. Further, scanning electron microscopic study demonstrated potential detrimental effect of taxoquinone on the morphology of <I>E. coli</I> ATCC 8739. These findings indicate that bioactive compound taxoquinone present in <I>M. glyptostroboides</I> could be used as a promising antibacterial agent in food industry to inhibit the growth of certain important foodborne pathogens.</P>
박인화, 나민균 충남대학교 약학대학 의약품개발연구소 2017 藥學論文集 Vol.32 No.-
Seven metabolites, nicotinamide (1), uracil (2), adenosine (3), tryptophan (4), lactic acid (5), alanine (6), and L-proline (7) were isolated from larvae of Tenebrio molitor Linnaeus. The chemical struc-tures of these entities 1-7 were determined by spectroscopic methods and comparing data with reported in the literature
Antiplatelet activities of hyperoside in vitro and in vivo
Ku, Sae-Kwang,Yoo, Hayoung,Zhou, Wei,Na, MinKyun,Bae, Jong-Sup 한국통합생물학회 2014 Animal cells and systems Vol.18 No.3
Thrombosis and thromboembolic occlusions of major and minor blood vessels are a major complication in various peripheral vascular diseases. Antiplatelet agents, key tools in the treatment of atherothrombosis, therefore became a mainstay medication for a wide range of vascular diseases. Hyperoside, an active compound from the Rhododendron brachycarpum G. Don (Ericaceae), was reported to have antioxidant, anti-hyperglycemic, anticancer, anti-inflammatory, and anti-coagulant activities. However, antiplatelet properties of hyperoside have not been studied. In this study, the antiplatelet activities of hyperoside were measured by thrombin- or collagen-induced platelet aggregation in vitro, adenosine diphosphate-induced platelet aggregation in vivo, and the thrombus formation in vivo. Our data showed that in vitro assays using freshly isolated human platelets, hyperoside showed the inhibition of the thrombin- or collagen-induced platelet aggregation. In accordance with these enhanced in vitro antiplatelet activities, hyperoside showed enhanced anti-thrombotic effects in vivo pulmonary embolism model and arterial thrombosis model. Collectively, these results indicate that hyperoside possesses antiplatelet activities and might offer enhanced anti-thrombotic efficacies without increasing side effects.