Multidrug resistance reversal activity of extract and a rare dimeric naphthoquinone from Diospyros lotus
A dimeric naphthoquinone namely dihydrodyspyrole R (1) was purified once more from Diospyros lotus. Dihydrodyspyrole R and chloroform fractions were evaluated for their effects on the reversion of multidrug resistance (MDR). The compounds (1) and extract exhibited promising MDR reversing effect in a...
Elmentve itt :
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Dokumentumtípus: | Cikk |
Megjelent: |
2018
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Sorozat: | PAKISTAN JOURNAL OF PHARMACEUTICAL SCIENCES
31 No. 3 |
mtmt: | 3370144 |
Online Access: | http://publicatio.bibl.u-szeged.hu/19432 |
Tartalmi kivonat: | A dimeric naphthoquinone namely dihydrodyspyrole R (1) was purified once more from Diospyros lotus. Dihydrodyspyrole R and chloroform fractions were evaluated for their effects on the reversion of multidrug resistance (MDR). The compounds (1) and extract exhibited promising MDR reversing effect in a dose-dependent manner against mouse T-lymphoma cell line. Molecular docking of compound 1 revealed the correlation between in-silico with in-vitro results. The molecular docking results showed that compound 1 is bind closely where co-crystal ligand of P-gp is present. But usually, computational investigation predicts that, if a compound gives lesser score then compound will exhibit good activity. Hence, the docking scores of compound 1 are the near to the Rhodamine. It is conclude that there are certain important structural features of compound 1which are responsible for the inhibiting potency of P-gp from mice. The computational Petra/Osiris/Molinspiration (POM) analysis confirms the possibility of use of compound 1 without side effect or less toxicity risks. |
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Terjedelem/Fizikai jellemzők: | 821-825 |
ISSN: | 1011-601X |