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Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis
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- Ringbom, Therese (author)
- Uppsala universitet,Avdelningen för farmakognosi
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- Segura, Laura (author)
- Uppsala universitet,Avdelningen för farmakognosi
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- Noreen, Ylva (author)
- Uppsala universitet,Avdelningen för farmakognosi
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- (creator_code:org_t)
- 1998-08-21
- 1998
- English.
- In: Journal of natural products (Print). - : American Chemical Society (ACS). - 0163-3864 .- 1520-6025. ; 61:10, s. 1212-1215
- Journal article (peer-reviewed)
Abstract
Subject headings
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- A hexane extract of Plantago major was investigated by bioactivity-directed fractionation, using an in vitro cyclooxygenase-2 (COX-2) catalyzed prostaglandin biosynthesis inhibition assay, and resulted in the isolation of ursolic acid (1). This triterpenoid showed a significant COX-2 inhibitory effect, directly on the enzyme activity, with an IC50 value of 130 microM and a COX-2/COX-1 selectivity ratio of 0.6. The structural isomer oleanolic acid (2) was found to be less active than 1, with an IC50 value of 295 microM, but showed a similar selectivity ratio (0.8). Furthermore, no significant inhibition on COX-2 or COX-1 was observed by the triterpenoid, 18beta-glycyrrhetinic acid (3). The direct inhibitory effect of 1 and 2 on COX-2 catalyzed prostaglandin biosynthesis increased with preincubation, indicating a time-dependent inhibition, while the effect on COX-1 was found to be independent of preincubation time.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Keyword
- PHARMACY
- FARMACI
Publication and Content Type
- ref (subject category)
- art (subject category)
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- Ringbom, Therese
- Segura, Laura
- Noreen, Ylva
- Perera, Premila
- Bohlin, Lars
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- MEDICAL AND HEALTH SCIENCES
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- Uppsala University
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