Methyldecanoate isolated from marine algae Turbinaria ornata enhances immunomodulation in LPS-induced inflammatory reactions in RAW 264.7 macrophages via iNOS/NFκB pathway.

This study identifies the anti-inflammatory, antioxidant, and immunomodulatory potential of a fatty acid methyl ester segregated from the brown algae Turbinaria ornata and identified by nuclear magnetic resonance and mass spectrometry as methyl 6,12-dimethyltridecanoate (ET). Antioxidant and anti-inflammatory effects of ET were studied on lipopolysaccharide (LPS)-induced inflammatory reaction in RAW 264.7 macrophages. Moreover, in silico docking studies of isolated ET with inflammatory markers TNFα, NFκB, and COX-2 showed potent binding scores suggesting anti-inflammatory potential. ET significantly reduced LPO and increased LPS-induced SOD, catalase, and GSH levels. Molecular docking results were further confirmed by checking mRNA levels of selected cytokines (IL6 and IL10), followed by protein expression of iNOS and NFκB in LPS-induced macrophages. ET significantly upregulated the expression of IL10 and downregulated the expression of IL6, iNOS, and NFκB, confirming the inhibition of LPS-induced inflammation via the iNOS/NFκB pathway.

EVA copolymer matrix for intra-oral delivery of antimicrobial and antiviral agents.

Biocompatible ethylene vinyl acetate copolymer (EVA) was utilized to study the release of an antiviral drug (acyclovir (ACY)) and an antimicrobial drug (doxycycline hyclate (DOH)). Release of both drugs from EVA was measured individually and in combination. The effect of drug combination of DOH and ACY is presented. Additionally, the release rate of DOH after coating of the matrix with a different copolymer, in drug-loading with increasing loads of DOH, and with increases in temperature are also presented. The drugs incorporated in EVA films were prepared from the dry sheet obtained by solvent evaporation of polymer casting solutions with drugs. Drug release from the films was examined for about 12 days in distilled water at 37 degrees C. Changes in optical density were followed spectrophotometrically. The combination of ACY and DOH resulted in an increased release of ACY by about three times (P < 0.001) while DOH showed a decrease in rate of about two times compared to the individual release rates (P = 0.008). Increases in drug levels of DOH resulted in increases in drug release rates (P = 0.001). The release rate of DOH increased with temperature (P = .001; 27, 32, 37 and 42 degrees C were studied) and the energy of activation (DeltaE ( not equal) = 56.69 kJ/mol) was calculated using the Arrhenius equation for the diffusion of DOH molecules. Thus, the release rates of drugs were influenced by many factors: drug combination, coating the device, drug-loading, and temperature variation. Therefore it is proposed that controlling these variables should make it possible to obtain therapeutic levels of drugs released from drug loaded polymer, which may be beneficial in treating oral infections.