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ISOLATION OF SULPHA QUINOVOSYL DIACYL GLYCEROL (SL) (A HUMAN TOPOPOISON I), USING FLASH CHROMATOGRAP
专利权人:
发明人:
DR S P DHANABAL,DR S JUBIE,MR M V N L CHAITANYA
申请号:
IN201741010426
公开号:
IN201741010426A
申请日:
2017.03.24
申请国别(地区):
IN
年份:
2018
代理人:
摘要:
ABSTRACT ISOLATION OF SULPHA QUINOVOSYL DIACYL GLYCEROL (SL) (A HUMAN TOPOPOISON I), USING FLASH CHROMATOGRAPHY Sulpha Quinovosyl Diacyl Glycerol (SL) is a sulpha lipid present in the blue green algae like Spirulina platensis (Phormidiaceae). The isolation of sulpha lipids is a very tedious process by conventional column chromatographic techniques where the yield, purity, cost and recovery will be a challenging task. Hence, we developed a novel economical flash chromatography technique to isolate SL. The percentage yield of SL was found to be 20.76%w/w, which is a very high yield in compare to existing traditional methods. The isolated SL proved to be a potent cytotoxic moiety against lung carcinoma with CTC50 value of 0.43 \iM. In order to prove the mechanism of cytotoxicity, the SL was docked in to catalytic domain of Human topo isomerases I (PDB ID: 1K4T at 2.10 A, PDB ID: 3AL2 at 2.0A0) and Human topo isomerases II (PDB ID: 1ZXN at 2.51 A, PDB ID: 3QX3 at 2.16 A). The docking studies were carried out by using GLIDE Program (Grid Based Ligand Docking from Energetics, from Schrodinger 9.9/2014-3 suite) in compare to standard topopoisons Camptothechin and Salvicine. The glide scores proved that the cytotoxicity is may be due to Topo-poisoning I & II. The cell cycle analysis proved that SL is arresting the cell cycle at Sub G phase. The human topoisomerase assays proved that the isolated molecule SL is a good human topopoison - I at 400 ug/ml but not human topopoison-II. Hence the developed flash chromatography method is a novel, economical and fast. The isolated SL can be a good novel topo-poison I lead.
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