Title:Natural COX-2 Inhibitors as Promising Anti-inflammatory Agents: An Update
Volume: 28
Issue: 18
Author(s): Jiahua Cui*Jinping Jia*
Affiliation:
- School of Environmental Science and Engineering, Shanghai Jiao Tong University, Shanghai, 200240,China
- School of Environmental Science and Engineering, Shanghai Jiao Tong University, Shanghai, 200240,China
Keywords:
COX-2 inhibitors, natural products, flavonoids, terpenoids, structure-activity relationships, antiinflammatory
agents, anticancer.
Abstract: COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of
arachidonic acid to prostaglandins, played a pivotal role in the inflammatory process. Different
from other family members, COX-2 was barely detectable in normal physiological conditions
and highly inducible during the acute inflammatory response of human bodies to injuries
or infections. Therefore, the therapeutic utilization of selective COX-2 inhibitors has already
been considered as an effective approach for the treatment of inflammation with diminished
side effects. Currently, both traditional and newer NSAIDs are the commonly prescribed
medications that treat inflammatory diseases by targeting COX-2. However, due to
the cardiovascular side-effects of the NSAIDs, finding reasonable alternatives for these frequently
prescribed medicines are a hot spot in medicinal chemistry research. Naturallyoccurring
compounds have been reported to inhibit COX-2, thereby possessing beneficial
effects against inflammation and certain cell injury. The review mainly concentrated on recently
identified natural products and derivatives as COX-2 inhibitors, the characteristics of
their structural core scaffolds, their anti-inflammatory effects, molecular mechanisms for enzymatic
inhibition, and related structure-activity relationships. According to the structural
features, the natural COX-2 inhibitors were mainly divided into the following categories:
natural phenols, flavonoids, stilbenes, terpenoids, quinones, and alkaloids. Apart from the
anti-inflammatory activities, a few dietary COX-2 inhibitors from nature origin also exhibited
chemopreventive effects by targeting COX-2-mediated carcinogenesis. The utilization of these
natural remedies in future cancer prevention was also discussed. In all, the survey on the
characterized COX-2 inhibitors from natural sources paves the way for the further development
of more potent and selective COX-2 inhibitors in the future.
