PTP1B inhibitory activity of kaurane diterpenes isolated from Siegesbeckia glabrescens
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| DC Field | Value | Language |
|---|---|---|
| dc.contributor.author | S Kim | - |
| dc.contributor.author | M Na | - |
| dc.contributor.author | H Oh | - |
| dc.contributor.author | Junpil Jang | - |
| dc.contributor.author | C B Sohn | - |
| dc.contributor.author | Bo Yeon Kim | - |
| dc.contributor.author | Won Keun Oh | - |
| dc.contributor.author | Jong Seog Ahn | - |
| dc.date.accessioned | 2017-04-19T09:05:05Z | - |
| dc.date.available | 2017-04-19T09:05:05Z | - |
| dc.date.issued | 2006 | - |
| dc.identifier.issn | 1475-6366 | - |
| dc.identifier.uri | 10.1080/14756360600741560 | ko |
| dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/7574 | - |
| dc.description.abstract | 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 Siegesbeckia glabrescens was found to inhibit PTP1B activity at 30 μg/mL. Bioassay-guided fractionation led to the isolation of two active diterpenes, ent-16βH,17-isobutyryloxy-kauran-19-oic acid (1) and ent-16βH,17-acetoxy-18-isobutyryloxy-kauran-19-oic acid (2), along with ent-16βH,17-hydroxy-kauran-19-oic acid (3). Compounds 1 and 2 inhibited the PTP1B activity with IC50 values of 8.7 ± 0.9 and 30.6 ± 2.1 μM, respectively. Kinetic studies suggest that both 1 and 2 are non-competitive inhibitors of PTP1B. However, compound 3 substituted with a hydroxyl group at C-17 in kaurane-type showed no inhibitory effects towards PTP1B. | - |
| dc.publisher | T&F (Taylor & Francis) | - |
| dc.title | PTP1B inhibitory activity of kaurane diterpenes isolated from Siegesbeckia glabrescens | - |
| dc.title.alternative | PTP1B inhibitory activity of kaurane diterpenes isolated from Siegesbeckia glabrescens | - |
| dc.type | Article | - |
| dc.citation.title | Journal of Enzyme Inhibition and Medicinal Chemistry | - |
| dc.citation.number | 4 | - |
| dc.citation.endPage | 383 | - |
| dc.citation.startPage | 379 | - |
| dc.citation.volume | 21 | - |
| dc.contributor.affiliatedAuthor | Junpil Jang | - |
| dc.contributor.affiliatedAuthor | Bo Yeon Kim | - |
| dc.contributor.affiliatedAuthor | Won Keun Oh | - |
| dc.contributor.affiliatedAuthor | Jong Seog Ahn | - |
| dc.contributor.alternativeName | 김소희 | - |
| dc.contributor.alternativeName | 나민균 | - |
| dc.contributor.alternativeName | 오현철 | - |
| dc.contributor.alternativeName | 장준필 | - |
| dc.contributor.alternativeName | 손천배 | - |
| dc.contributor.alternativeName | 김보연 | - |
| dc.contributor.alternativeName | 오원근 | - |
| dc.contributor.alternativeName | 안종석 | - |
| dc.identifier.bibliographicCitation | Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 21, no. 4, pp. 379-383 | - |
| dc.identifier.doi | 10.1080/14756360600741560 | - |
| dc.subject.keyword | 17-acetoxy-18-isobutyryloxy-kauran-19-oic acid | - |
| dc.subject.keyword | 17-isobutyryloxy-kauran-19-oic acid | - |
| dc.subject.keyword | ent-16βH | - |
| dc.subject.keyword | inhibition | - |
| dc.subject.keyword | kaurane diterpenes | - |
| dc.subject.keyword | non-competitive inhibitors | - |
| dc.subject.keyword | protein tyrosine phosphatase 1B | - |
| dc.subject.keyword | siegesbeckia glabrescens | - |
| dc.subject.local | 17-acetoxy-18-isobutyryloxy-kauran-19-oic acid | - |
| dc.subject.local | 17-isobutyryloxy-kauran-19-oic acid | - |
| dc.subject.local | ent-16βH | - |
| dc.subject.local | inhibition | - |
| dc.subject.local | Inhibition | - |
| dc.subject.local | Kaurane diterpenes | - |
| dc.subject.local | kaurane diterpenes | - |
| dc.subject.local | Non-competitive inhibitor | - |
| dc.subject.local | non-competitive inhibitors | - |
| dc.subject.local | Non-competitive inhibitors | - |
| dc.subject.local | non-competitive inhibitor | - |
| dc.subject.local | protein tyrosine phosphatase 1B | - |
| dc.subject.local | protein tyrosine phosphatase-1B (PTP1B) | - |
| dc.subject.local | Protein tyrosine phosphatase 1B | - |
| dc.subject.local | protein tyrosine phosphatase 1B (PTP1B) | - |
| dc.subject.local | protein tyrosine phosphatase 1B (FTPIB) | - |
| dc.subject.local | Protein tyrosine phosphatase 1B (PTP1B) | - |
| dc.subject.local | Siegesbeckia glabrescens | - |
| dc.subject.local | siegesbeckia glabrescens | - |
| dc.description.journalClass | Y | - |
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