AI Article Synopsis
- A hexane extract from Plantago major led to the discovery of ursolic acid, which effectively inhibits COX-2 enzyme activity with an IC50 of 130 microM and a selectivity ratio of 0.6 when compared to COX-1.
- Oleanolic acid showed less activity with an IC50 of 295 microM but similar selectivity (0.8), while 18beta-glycyrrhetinic acid did not significantly inhibit either COX-2 or COX-1.
- The inhibitory effects of ursolic and oleanolic acids on COX-2 were enhanced with longer exposure times, while their effect on COX-1 remained constant regardless of preincubation duration.
Article Abstract
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.
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| http://dx.doi.org/10.1021/np980088i | DOI Listing |
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