Rugosin-B

Myrtus communis L. (myrtle) and Myrtus nivellei Batt. & Trab. (Saharan myrtle) have been used in folk medicine for alleviating some ailments. M. communis is largely distributed in the Mediterranean Basin, whereas M. nivellei is confined in specific zones of the central Saharan mountains. The chemical composition and antioxidant activity of berry and leaf extracts isolated from myrtle are deeply documented, whereas those isolated from Saharan myrtle extracts are less studied. In both species, the major groups of constituents include gallic acid derivatives, flavonols, flavonol derivatives, and hydroxybenzoic acids. In coloured berries, anthocyanins are also present. In M. nivellei extracts are reported for some compounds not described in M. communis so far: 2-hydroxy-1,8-cineole-β-d-glucopyranoside, 2-hydroxy-1,8-cineole 2-O-α-l-arabinofuranosyl (1→6)-β-d-glucopyranoside, rugosin A, and rugosin B. Berries and leaves extracts of both species had antioxidant activity. Comparative studies of the antioxidant activity between leaf and berry myrtle extracts revealed that leaf extracts are best antioxidants, which can be assigned to the galloyl derivatives, flavonols, and flavonols derivatives, although the ratio of these groups of compounds might also have an important role in the antioxidant activity. The anthocyanins present in myrtle berries seem to possess weak antioxidant activity. The antioxidant activity of sample extracts depended on various factors: harvesting time, storage, extraction solvent, extraction type, and plant part used, among other factors. Leaf extracts of myrtle revealed to possess anti-inflammatory activity in several models used. This property has been attributed either to the flavonoids and/or hydrolysable tannins, nevertheless nonprenylated acylphloroglucinols (e.g., myrtucommulone and semimyrtucommulone) have also revealed a remarkable role in that activity. The biological activities of myrtle extracts found so far may direct its use towards for stabilizing complex lipid systems, as prebiotic in food formulations, and as novel therapeutic for the management of inflammation.

Dipeptidyl peptidase-IV (DPP-IV) is a protease responsible for the degradation of the incretin hormone. A number of DPP-IV inhibitors have been approved for use in the treatment of type 2 diabetes. While these inhibitors are effective for this treatment, methods for the prevention of this disease are also required as diabetes patient numbers are currently increasing rapidly worldwide. We screened the DPP-IV inhibitory activities of edible plant extracts with the intention of using these extracts in a functional food supplement for the prevention of diabetes. Rose (Rosa gallica) bud extract powder was a promising material with high inhibitory activity. In this study, seven ellagitannins were isolated as active compounds through activity-guided fractionations, and their DPP-IV inhibitory activities were measured. Among them, rugosin A and B showed the highest inhibitory activities and rugosin B was shown as the major contributing compound in rose bud extract powder.

Three antimicrobial peptides were isolated from the skin of Rana rugosa. The major component, designated rugosin A, consisted of 33 amino acid residues and had structural homology (45%) with brevinin-2 of Rana porosa brevipoda. This peptide strongly inhibited the growth of gram-positive bacteria (e.g. Staphylococcus aureus 209P). The second peptide (rugosin B), a minor component, also had 33 amino acid residues, but was less homologous (33%) with brevinin-2. This peptide exhibited a striking antimicrobial activity against both gram-negative (e.g., Escherichia coli NIHJ) and gram-positive bacterial species. The third one, named rugosin C, composed of 37 amino acid residues, exhibited an antimicrobial activity against gram-positive bacteria. All three peptides had an intramolecular disulfide bond at the C-terminus.