A Rare Class of New Dimeric Naphtoquiones from Diospyros lotus have Multidrug Reversal and Antiproliferative Effects

• Main Authors: Dr. Abdur eRauf (Author), Ghias eUddin (Author), Bina S Siddiqui (Author), Josep eMolnar (Author), Akos eCsonka (Author), Bashir eAhmad (Author), Diana eSzabo (Author), Umar eFarooq (Author), Ajmal eKhan (Author)
• Format: Book
• Published: Frontiers Media S.A., 2015-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

Three new dimeric naphthoquinones, 5,4'-dihydroxy-1'-methoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,5',8'-tetraone (1), 5',8'-dihydroxy-5-methoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (2) and 8,5',8'-trihydroxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (3), were isolated from the roots of Diospyros lotus. Their structures were elucidated by spectroscopic techniques, including 1D and 2D NMR, such as HSQC, HMBS, NOESY and J resolved. Compounds 1-3 were evaluated for their effects on the reversion of multidrug resistance (MDR) mediated by P-glycoprotein through use of the rhodamine-123 exclusion screening test on human ABCB1 gene transfected L5178Y mouse T-cell lymphoma. Compounds 1-3 were also assessed for their antiproliferative and cytotoxic effects on L5178 and L5178Y mouse T-cell lymphoma lines. Both 1 and 2 exhibited promising antiproliferative and MDR-reversing effects in a dose dependent manner. The effects of the tested compounds on the activity of doxorubicin were observed to vary from slight antagonism to antagonism.

Item Description

1663-9812
10.3389/fphar.2015.00293