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Title

Betulinic acid derivatives: a new class of α-glucosidase inhibitors and LPS-stimulated nitric oxide production inhibition on mouse macrophage RAW 264.7 cells.

Authors

Gundoju, Narayanarao; Bokam, Ramesh; Yalavarthi, Nageswara Rao; Azad, Rajaram; Ponnapalli, Mangala Gowri

Abstract

Chemical manipulation studies were conducted on betulinic acid (1), twenty-one new rationally designed analogues of 1 with modifications at C-28 were synthesized for their evaluation of inhibitory effects on α-glucosidase and LPS-stimulated nitric oxide production in mouse macrophage RAW 264.7 cells. Compound 2 (IC50 = 5.4 μM) exhibited an almost 1.4-fold increase in α-glucosidase inhibitory activity on yeast α-glucosidase while analogues 5 (IC50 16.4 μM) and 11 (IC50 16.6 μM) exhibited a 2-fold enhanced inhibitory activity on NO-production than betulinic acid.

Subjects

GLUCOSIDASES; ACID derivatives; NITRIC oxide; MICE; CELLS

Publication

Natural Product Research, 2019, Vol 33, Issue 18, p2618

ISSN

1478-6419

Publication type

Academic Journal

DOI

10.1080/14786419.2018.1462182

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