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Synthesis and in vitro Screening of 29, 30-Dibromo-28-oxoallobetulin against Parasitic Protozoans, Leishmania donovani and Leishmania Major.

Ghosh P, Mandal A, Dey S, Pal C - Indian J Pharm Sci (2015 Mar-Apr)

Bottom Line: A simple synthesis and in vitro antileishmanial activity of 29,30-dibromo-28-oxoallobetulin against the parasitic protozoans, Leishmania donovani and Leishmania major is described.The structure of the compound is established on the basis of spectral data (IR, NMR, MS).Both the antiproliferative effect and the cell cycle progression were studied.

View Article: PubMed Central - PubMed

Affiliation: Natural Products and Polymer Chemistry Laboratory, Department of Chemistry, University of North Bengal, Raja Rammhunpur, Darjeeling-734 013, India.

ABSTRACT
A simple synthesis and in vitro antileishmanial activity of 29,30-dibromo-28-oxoallobetulin against the parasitic protozoans, Leishmania donovani and Leishmania major is described. The structure of the compound is established on the basis of spectral data (IR, NMR, MS). Both the antiproliferative effect and the cell cycle progression were studied.

No MeSH data available.


Related in: MedlinePlus

Effect of test compound on L. donovani AG83 promastigotes.L. donovani AG83 promastigotes (2×106/ml) were incubated with DMSO (0.2%), 10 and 15 μg/ml of test compound (dissolved in DMSO) in complete M199 media at 22°, and analyzed for DNA content by flow cytometry as described in experimental section.
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Figure 4: Effect of test compound on L. donovani AG83 promastigotes.L. donovani AG83 promastigotes (2×106/ml) were incubated with DMSO (0.2%), 10 and 15 μg/ml of test compound (dissolved in DMSO) in complete M199 media at 22°, and analyzed for DNA content by flow cytometry as described in experimental section.

Mentions: Cell-cycle analysis complemented the previous data obtained by MTT assay. It demonstrated that at 48 h of culture, both 10 and 15 µg/ml of test compound caused L. donovani promastigotes to remain as resting G0/G1 (M2) cells and inhibited their entry into the S phase (M3). The percent dead cells (M1) increased during this incubation period and growth arrest was also visible. Test compound at a concentration of 10 µg/ml started to block the entry of L. donovani promastigotes into S phase from G0/G1, however, at 15 µg/ml completely blocked the entry dose dependently (Table 2 and fig. 3). Both doses caused substantial increases in cell death, compared with DMSO treated cultures. Our results suggested that 29,30-dibromo-28-oxoallobetulin, 3 preferentially active against L. donovani promastigotes at inducing cell-cycle arrest followed by death in vitro.


Synthesis and in vitro Screening of 29, 30-Dibromo-28-oxoallobetulin against Parasitic Protozoans, Leishmania donovani and Leishmania Major.

Ghosh P, Mandal A, Dey S, Pal C - Indian J Pharm Sci (2015 Mar-Apr)

Effect of test compound on L. donovani AG83 promastigotes.L. donovani AG83 promastigotes (2×106/ml) were incubated with DMSO (0.2%), 10 and 15 μg/ml of test compound (dissolved in DMSO) in complete M199 media at 22°, and analyzed for DNA content by flow cytometry as described in experimental section.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4442470&req=5

Figure 4: Effect of test compound on L. donovani AG83 promastigotes.L. donovani AG83 promastigotes (2×106/ml) were incubated with DMSO (0.2%), 10 and 15 μg/ml of test compound (dissolved in DMSO) in complete M199 media at 22°, and analyzed for DNA content by flow cytometry as described in experimental section.
Mentions: Cell-cycle analysis complemented the previous data obtained by MTT assay. It demonstrated that at 48 h of culture, both 10 and 15 µg/ml of test compound caused L. donovani promastigotes to remain as resting G0/G1 (M2) cells and inhibited their entry into the S phase (M3). The percent dead cells (M1) increased during this incubation period and growth arrest was also visible. Test compound at a concentration of 10 µg/ml started to block the entry of L. donovani promastigotes into S phase from G0/G1, however, at 15 µg/ml completely blocked the entry dose dependently (Table 2 and fig. 3). Both doses caused substantial increases in cell death, compared with DMSO treated cultures. Our results suggested that 29,30-dibromo-28-oxoallobetulin, 3 preferentially active against L. donovani promastigotes at inducing cell-cycle arrest followed by death in vitro.

Bottom Line: A simple synthesis and in vitro antileishmanial activity of 29,30-dibromo-28-oxoallobetulin against the parasitic protozoans, Leishmania donovani and Leishmania major is described.The structure of the compound is established on the basis of spectral data (IR, NMR, MS).Both the antiproliferative effect and the cell cycle progression were studied.

View Article: PubMed Central - PubMed

Affiliation: Natural Products and Polymer Chemistry Laboratory, Department of Chemistry, University of North Bengal, Raja Rammhunpur, Darjeeling-734 013, India.

ABSTRACT
A simple synthesis and in vitro antileishmanial activity of 29,30-dibromo-28-oxoallobetulin against the parasitic protozoans, Leishmania donovani and Leishmania major is described. The structure of the compound is established on the basis of spectral data (IR, NMR, MS). Both the antiproliferative effect and the cell cycle progression were studied.

No MeSH data available.


Related in: MedlinePlus