Identification and Preliminary SAR Studies of (+)-Geodin as a Glucose Uptake Stimulator for Rat Adipocytes

(+)-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...

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Published inJournal of antibiotics Vol. 58; no. 9; pp. 583 - 589
Main Authors Sato, S, Okusa, N, Ogawa, A, Ikenoue, T, Seki, T, Tsuji, T
Format Journal Article
LanguageEnglish
Published TOKYO Japan Antibiotics Research Assoc 01.09.2005
Nature Publishing Group
Subjects
Adipose Tissue - cytology
Adipose Tissue - drug effects
Adipose Tissue - metabolism
Animals
Benzofurans - chemistry
Benzofurans - pharmacology
Biotechnology & Applied Microbiology
Glucose - metabolism
Immunology
Insulin - pharmacology
Life Sciences & Biomedicine
Microbiology
Pharmacology & Pharmacy
Rats
Rats, Wistar
Science & Technology
(+)-geodin
glucose uptake stimulator
TRANSPORT
adipocytes
PHOSPHATIDYLINOSITOL 3-KINASE
WORTMANNIN
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Summary:(+)-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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0021-8820
1881-1469
DOI:10.1038/ja.2005.79