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R Tripathy

Publications and source records attributed to R Tripathy.

7 recordsLinked to original sources

Calpain inhibitors based on the quiescent affinity label concept: high rates of calpain inactivation with leaving groups derived from N-hydroxy peptide coupling reagents.

A series of irreversible inhibitors of recombinant calpain has been synthesized and their rates of inactivation have been evaluated against calpain and cathepsin B, respectively. The design of the inhibitors was based on the quiescent affinity label concept. By choosing the appropriate affinity group and by employing leaving groups derived from N-hydroxy coupling reagents, good inhibitors of calpain with high rates of inactivation have been identified. However, poor aqueous stability limits their therapeutic utility.

Affinity Labels↗

Growth in the first year in children following IAP Policy on Infant Feeding.

OBJECTIVE: To study the growth pattern in the first year in children fed according to recommendations of IAP Policy on Infant Feeding. DESIGN: Longitudinal. SETTING: Department of Pediatrics, S.C.B. Medical College Hospital, Cuttack, Orissa. SUBJECTS AND METHODS: 114 infants (68 boys and 46 girls) with birth weight greater than or equal to 2500g from upper and middle S-E status were regularly followed up from birth to 12 mo of age and fed according to recommendations of IAP Policy on Infant Feeding. Mean and standard deviations of weight for age (W/A) and length for age (L/A) and mean Z scores for W/A, L/A and W/L (weight for length) were calculated separately for boys and girls with reference to NCHS-WHO and BFDS data. OBSERVATIONS: Mean Z scores for W/A with reference to NCHS-WHO data showed a positive trend from birth upto the age of 3 to 4 months, subsequently declining upto one year. The Z scores for L/A showed only a minimal downward trend. The W/L Z score remained above the baseline value up to 3 months in boys and 7 months in girls. When BFDS was taken as the reference, W/A Z scores showed consistent positive increments, from birth in girls and 1 mo in boys. L/A Z scores increased from 3 months in boys and 11 months in girls. Using NCHS data as the reference, the percentage of infants below -2SD for weight was 0 to 7% during first 6 months and 14% at 12 months. Ten% were below -2SD for length at 12 months. With BFDS as the reference, the percentage of infants below -2SD for weight was 25% at birth, 5% at 6 months and 12% at 1 yr. For length, it was 12% at birth and 8% at 1 year. The increments in weight and length closely followed BFDS upto 12 mo age. CONCLUSION: The IAP Policy on Infant Feeding results in adequate growth of non low birth weight infants in the first year of life.

Body Height↗

Synthesis and biological activity of a series of potent fluoromethyl ketone inhibitors of recombinant human calpain I.

Calpain I, an intracellular cysteine protease, has been implicated in the neurodegeneration following an episode of stroke. In this paper, we report on a series of potent dipeptide fluoromethyl ketone inhibitors of recombinant human calpain I (rh calpain I). SAR studies revealed that while calpain I tolerates a variety of hydrophobic groups at the P1 site, Leu at P2 is preferred. However, the nature of the N-terminal capping group has a significant effect on the inhibitory activity of this series of compounds. Compound 4e [(1,2,3,4-tetrahydroisoquinolin-2-yl)carbonyl-Leu-D,L-Phe-CH2F+ ++], having a tetrahydroisoquinoline containing urea as the N-terminal capping group, is the most potent dipeptide fluoromethyl ketone inhibitor of calpain I (with a second-order rate constant for inactivation of 276,000 M-1 s-1) yet reported; tripeptide 4k (Cbz-Leu-Leu-D,L-Phe-CH2F) is equipotent. A number of compounds presented in this study displayed excellent selectivity for calpain I over cathepsins B and L, two related cysteine proteases. Compounds which exhibited good inhibitory activity in the assay against isolated rh calpain I also inhibited intracellular calpain I in a human cell line. Thus, in an intact cell assay, compounds 4e and 4k inhibited calpain I with IC50 values of 0.2 and 0.1 microM, respectively. Finally, we also disclose the first example of fluorination of a dipeptide enol silyl ether to generate the corresponding dipeptide fluoromethyl ketone.

Calpain↗

Levels of erythrocyte malonyldialdehyde, vitamin E, reduced glutathione, G6PD activity & plasma urate in patients of pregnancy induced hypertension.

To assess the oxidative stress across the cell membrane in patients suffering from pregnancy induced hypertension, erythrocyte malonyldialdehyde, vitamin E, reduced glutathione, glucose-6-phosphate dehydrogenase activity and plasma urate levels were estimated in 25 non pregnant women, 40 normotensive pregnant women and 40 women with pregnancy induced hypertension (PIH). As compared to non pregnant women, there was a significant increase in the levels of erythrocyte malonyldialdehyde and plasma urate in normotensive pregnant women, which were further increased in women with PIH. Erythrocyte glutathione levels were raised in normotensive pregnant women as compared to non pregnant women. Its levels were decreased in patients of PIH as compared to normotensive pregnant women. Cellular bio-availability of vitamin E was depressed in both normotensive pregnancy as well as patients with pregnancy induced hypertension as compared to non pregnant women.

Adult↗