Cirsimaritin

Cirsimaritin is a flavone that has been found in D. kotschyi and has diverse biological activities.^1,2,3,4,5 It binds to rat adenosine A₁, rat A_2A, and human A₃ receptors (K_is = 1.2, 3, and 1.72 ?M, respectively, in radioligand binding assays), as well as inhibits dipeptidyl peptidase 4 (DPP-4; IC₅₀ = 0.43 ?M).^1,2 Cirsimaritin is active against the chloroquine-sensitive NF54 strain of P. falciparum (IC₅₀ = 16.9 ?M).³ It inhibits the proliferation of AGS, HT-29, Saos-2, and WEHI 164 cells (IC₅₀s = 14.4, 13.1, 38.5, and 40.7 ?M, respectively).⁴ Cirsimaritin (10 mg/kg) increases the number of entries into, and percentage of time spent in, the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.⁵

1.Ji, X.-d., Melman, N., and Jacobson, K.A.Interactions of flavonoids and other phytochemicals with adenosine receptorsJ. Med. Chem.39(3)781-788(1996) 2.Li, N., Wang, L.-J., Jiang, B., et al.Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitusEur. J. Med. Chem.151145-157(2018) 3.Tasdemir, D., Lack, G., Brun, R., et al.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoidsJ. Med. Chem.49(11)3345-3353(2006) 4.Moghaddam, G., Ebrahimi, S.A., Rahbar-Roshandel, N., et al.Antiproliferative activity of flavonoids: Influence of the sequential methoxylation state of the flavonoid structurePhytother. Res.26(7)1023-1028(2012) 5.Abdelhalim, A., Karim, N., Chebib, M., et al.Antidepressant, anxiolytic and antinociceptive activities of constituents from Rosmarinus officinalisJ. Pharm. Pharm. Sci.18(4)448-459(2015)