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Extensive research on tea catechins, mainly (-)-epigallocatechin gallate, has shown numerous health promoting effects. However, various clinical studies demonstrated several issues associated with tea catechins which account for their poor systemic bioavailability. In order to improve pharmacological activity and bioavailability of natural tea catechins, two major strategies have been adopted to date which include synthesizing catechin analogs/prodrugs and the development of novel drug delivery systems. In this review, we provide a detailed account of novel synthetic analogs/prodrugs as well as novel drug delivery approaches used for natural tea catechins to make them therapeutically potent drug-like molecules.

The methanolic fraction of the root extract of Mikania cordata was found to possess an inhibitory effect on carrageenin and other mediator-induced oedema; there was a significant inhibition of protein exudation, an increase in peritoneal capillary permeability and leucocyte migration in inflammatory conditions. The extract significantly inhibited both cotton pellet and carrageenin-induced granuloma formation, was effective in experimentally induced arthritic conditions and turpentine-induced joint oedema. The extract also possessed inhibitory effects on sodium urate-induced experimental gout. A significant reduction of pyrexia was also found to occur when rats were treated with the extract. Thus it may be concluded that the methanolic fraction of M. cordata root extract possessed significant antiinflammatory effects in exudative, proliferative and chronic phases of inflammation and demonstrated an antipyretic activity.

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The present study was aimed to evaluate the cyclooxygenase (COX) and lipoxygenase (LOX) inhibitory activity of Abroma augusta (AA) and Desmodium gangeticum (DG). Initially In-vivo anti-inflammatory activity of aqueous extract (AqE) of aerial parts of DG (100 mg/ml) and petroleum ether extract (PEE) of roots of AA (250 mg/ml) was assessed in carrageenan induced paw oedema model in albino wistar rats. In addition, each plant extract was evaluated for COX1, COX-2 and LOX inhibitory activity to determine the possible mechanism of their antiinflammatory activity. The results of the study demonstrated that each plant extract significantly (p<0.0001) reduces the paw volume compared with standard drug Ibuprofen (100 mg/kg b.w.). The percentage inhibitory activity of AqE of DG against COX-2 (IC50=39. 5 µg/ml) were generally higher to that of COX-1 (IC50=49. 5 µg/ml), however, at the same concentrations PEE of AA demonstrated inhibitory activity against COX-1 (IC50=36. 5 µg/ml) to a greater extent than COX-2 (IC50=59 µg/ml). Moderate inhibition of LOX activity was demonstrated by DG (IC50=57.0 µg/ml). AA exhibited weak inhibitory action on LOX activity at the same concentrations (IC50=75.5 µg/ml). The results of the study concluded that anti-inflammatory activity of plant extracts could be due to inhibition of COX and LOX enzymes and thus supports the traditional use of the above mentioned plants in inflammatory disorders.