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Tanzawaic acid derivatives from a marine isolate of Penicillium sp. (SF-6013) with anti-inflammatory and PTP1B inhibitory activities.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Dec2014, Vol. 24 Issue 24, p5787-5791. 5p. - Publication Year :
- 2014
-
Abstract
- Chemical investigation of a marine-derived fungus Penicillium sp. SF-6013 resulted in the discovery of a new tanzawaic acid derivative, 2 E ,4 Z -tanzawaic acid D ( 1 ), together with four known analogues, tanzawaic acids A ( 2 ) and D ( 3 ), a salt form of tanzawaic acid E ( 4 ), and tanzawaic acid B ( 5 ). Their structures were mainly determined by analysis of NMR and MS data, along with chemical methods. Preliminary screening for anti-inflammatory effects in lipopolysaccharide (LPS)-activated microglial BV-2 cells showed that compounds 1 , 2 , and 5 inhibited the production of nitric oxide (NO) with IC 50 values of 37.8, 7.1, and 42.5 μM, respectively. Compound 2 also inhibited NO production in LPS-stimulated RAW264.7 murine macrophages with an IC 50 value of 27.0 μM. Moreover, these inhibitory effects correlated with the suppressive effect of compound 2 on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression in LPS-stimulated RAW264.7 and BV2 cells. In addition, compounds 2 and 5 significantly inhibited the activity of protein tyrosine phosphatase 1B (PTP1B) with the same IC 50 value (8.2 μM). [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 24
- Issue :
- 24
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 99739165
- Full Text :
- https://doi.org/10.1016/j.bmcl.2014.10.035