The study was conducted on 20 Holstein X Sahiwal cross bred dairy cows, with an average milk production of 2,752±113.79 liters in 284±5.75 days during a single lactation, that were divided in to two groups of 10 animals. We investigated the oxidative stress and antioxidant status during the transition period in dairy cows. In this study, plasma level of MDA was considered as an indicator of lipid peroxidation and SOD, catalase, GSH and GSHPx as antioxidants. The lipid peroxidation was significantly (p<0.001) higher in cows during early lactation as compared to the cows in advanced pregnancy. A significant positive correlation (r = +0.831, p<0.01) was determined between MDA and catalase in early lactating cows. In early lactating cows, blood glutathione was significantly lower than in advanced pregnant cows. However, early lactating cows showed non-significant negative correlation for all antioxidant enzymes with lipid peroxidation. In conclusion, dairy cows seemed to have more oxidative stress and low antioxidant defense during early lactation or just after parturition than advanced pregnant cows, and this appears to be the reason for their increased susceptibility to production diseases (e.g. mastitis, metritis, retention of fetal membranes etc.) and other health problems.

A novel class of phthalimides functionalized with privileged scaffolds was designed, synthesized and evaluated as potential inhibitors of plasmepsin 2 (Ki: 0.99 ± 0.1 μM for 6u) and plasmepsin 4 (Ki: 3.3 ± 0.3 μM for 6t), enzymes found in the digestive vacuole of the plasmodium parasite and considered as crucial drug targets. Three compounds were identified as potential candidates for further development. The listed compounds were also assayed for their antimalarial efficacy against chloroquine (CQ) sensitive strain (3D7) of Plasmodium falciparum. Assay of twenty seven hydroxyethylamine derivatives revealed four (5e, 6j, 6o and 6s) as strongly active, which were further evaluated against CQ resistant strain (7GB) of P. falciparum. Compound 5e possessing the piperidinopiperidine moiety exhibited promising antimalarial activity with an IC50 of 1.16 ± 0.04 μM. Further, compounds 5e, 6j, 6o and 6s exhibited low cytotoxic effect on MCF-7 cell line. Compound 6s possessing C 2 symmetry was identified as the least cytotoxic with significant antimalarial activity (IC50: 1.30 ± 0.03 μM). The combined presence of hydroxyethylamine and cyclic amines (piperazines and piperidines) was observed as crucial for the activity. The current studies suggest that hydroxyethylamine based molecules act as potent antimalarial agent and may be helpful in drug development.

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The current anticancer therapies are limited by their lack of controlled spatiotemporal release at the target site of action. We report a novel drug delivery platform that provides on-demand, real-time, organelle-specific drug release and monitoring upon photoactivation. The system is comprised of a model anticancer drug doxorubicin, an alkyltriphenylphosphonium moiety to target mitochondria in cancer cells, and a hydroxycinnamate photoactivatable linker that is covalently attached to the drug and mitochondria-targeting moieties such that it can be phototriggered by either UV (one-photon) or NIR (two-photon) light to form a fluorescent coumarin product and facilitate the release of drug payload. The extent of drug release is quantified by the fluorescence intensity of the coumarin formed. Further, the photoactivatable prodrug accumulates in the mitochondria and shows light-triggered temporally controlled cell death. In the future, our platform can be tuned for any biological application of interest, offering immense value in biomedicine.