PubMed Health⌕ Search

Biomedical subjects

Anand Vardhan

Publications and source records attributed to Anand Vardhan.

6 recordsLinked to original sources

Synthesis and cytotoxic activity of 3-O-acyl/3-hydrazine /2-bromo/20,29-dibromo betulinic acid derivatives.

A series of 3-O-acyl, 3-hydrazine, 2-bromo, and 20,29-dibromo betulinic acid derivatives (1-27) have been synthesized and screened for in vitro cytotoxic activity on human cancer cell lines MOLT-4, JurkatE6.1, CEM.CM3, BRISTOL8, U937, DU145, PA-1, A549, and L132. A number of compounds have shown ED(50)<1 microg/mL against the cancer cell lines tested and have shown better cytotoxicity than betulinic acid. Compounds 13, 19, 20, 23, and 27 were the best derivatives and were selected as lead molecules for further development. The structure-activity relationship has been described.

Antineoplastic Agents↗

Synthesis of 3-O-acyl/3-benzylidene/3-hydrazone/3-hydrazine/17-carboxyacryloyl ester derivatives of betulinic acid as anti-angiogenic agents.

New 3-O-acyl, 3-benzylidene, 3-hydrazone, 3-hydrazine, 17-carboxyacryloyl ester derivatives of betulinic acid (2-6, 8-11, 13, 17, 18, 21, and 22) were synthesized and evaluated in vitro for anti-angiogenic activity on endothelial cell cytotoxicity, specificity, and tube-formation ability. All derivatives reported here showed IC(50)<4 microg/mL. Compounds 3, 9, 10, 17, 21, and 22 have shown better cytotoxicity (IC(50)<1.2 microg/mL) than betulinic acid (1) and improved endothelial cell specificity (ECS>10) in some cases. Compounds 10, 17, and 18 have shown 20%, 32%, and 48% reduction in TLS, respectively, and were found better than betulinic acid (1). We have shown that 20,29-dihydrobetulinic acid derivatives have better anti-angiogenic activity as compared to betulinic acid or its other derivatives.

Angiogenesis Inhibitors↗

Betulinic acid and its derivatives as anti-angiogenic agents.

Betulinic acid (1) significantly caused cytotoxicity to endothelial cell line ECV304 (IC(50) 1.26+/-0.44 microg/mL) in a 5-day MTT assay. Novel and more potent derivatives of betulinic acid (2, 4, 6-8) have been synthesized with IC(50) less than 0.4 microg/mL. The endothelial cell specificity against human tumor cell lines DU145, L132, A549, and PA-1 were determined. Further betulinic acid (1) inhibited TLS formation of ECV304 cells on Matrigel(TM) by 5.5% while its derivatives caused an inhibition of 13.1-49.2%.

Angiogenesis Inhibitors↗

Decrease in infections with the introduction of mupirocin cream at the peritoneal dialysis catheter exit site.

UNLABELLED: Staphylococcus aureus associated peritonitis and catheter exit site infections (ESI) are an important cause of hospitalization and catheter loss in the patients undergoing chronic peritoneal dialysis (PD). We aimed to determine the potential effectiveness of the application of mupirocin cream at the catheter exit site in preventing exit site infection and peritonitis. METHODS: This prospective historically controlled study was done in a total of 86 patients who entered our PD program from April 1999 to January 2001. They were instructed to apply Mupirocin cream 2% to the exit site daily or on alternate days. The patients were not screened to determine whether they were staphylococcus aureus carriers. One hundred and thirteen patients on PD prior to April 1999 acted as historical controls. Both groups were followed prospectively for a period of 22 months. RESULTS: In the study group application of mupirocin lead to a significant reduction in the incidence rate of both exit site infections overall (0.43 vs. 0.09; p<0.0001) and ESI due staphylococcus aureus (0.14 vs. 0.02; p=0.004) amounting to a relative reduction of 79% and 85% respectively. Although the overall incidence of peritonitis did not change (0.28 vs. 0.26; p=0.7) there was a significant reduction in peritonitis caused by staphylococcus aureus (0.07 vs. 0; p=0.01) Although only one catheter required removal in the mupirocin group as against 5 in the control group, this was not statistically significant. CONCLUSIONS: Mupirocin application at the exit site significantly lowers the incidence of ESI and peritonitis caused by staphylococcus aureus without any significant side effects.

Adult↗