Identification and Preliminary SAR Studies of (+)-Geodin as a Glucose Uptake Stimulator for Rat Adipocytes
| Autor: | Seiichi Sato, Akiyo Ogawa, Noriyuki Okusa, Takashi Tsuji, Takao Ikenoue, Tetsuya Seki |
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| Rok vydání: | 2005 |
| Předmět: |
Pharmacology
Natural product biology Glucose uptake Insulin medicine.medical_treatment Fungus biology.organism_classification Rats Penicillium glabrum Wortmannin chemistry.chemical_compound Glucose Adipose Tissue Biochemistry chemistry Biosynthesis Drug Discovery medicine Animals Rats Wistar Benzofurans |
| Zdroj: | The Journal of Antibiotics. 58:583-589 |
| ISSN: | 1881-1469 0021-8820 |
| DOI: | 10.1038/ja.2005.79 |
| Popis: | (+)-Geodin (1) was isolated from Penicillium glabrum AJ117540 with activity that stimulates glucose uptake by rat adipocytes. Unlike insulin it is active in the presence of wortmannin. Dihydrogeodin (2) and sulochrin (3) which are the precursors of (+)-geodin biosynthesis were also isolated from the same fungus. Preliminary SAR studies of 1 showed some analogues had enhanced activity. Especially, the activities of racemic geodin and dibromo analogue (7a) were comparable to that of the natural product. Geodin (1), a known fungal metabolite, was isolated from Penicillium glabrum AJ117540 as an active substance (Fig. 1). Dihydrogeodin (2) and sulochrin (3), the precursors of 1, were also isolated from the same fungal extract. In this study, preliminary mechanistic insight and SAR are reported. |
| Databáze: | OpenAIRE |
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