Reversal of multidrug resistance in cancer cells by pyranocoumarins isolated from Radix Peucedani

Pyranocoumarins from Root Extracts of Peucedanum praeruptorum Dunn with Multidrug Resistance Reversal and Anti-Inflammatory Activities

“…In particular, five compounds (1, 7, 8, 11, and 13) showed considerably significant activities compared to those of known MDR inhibitors (verapamil and cyclosporine A, Figure 5). Previous phytochemical investigations revealed that compounds 2 and 4 inhibited LPS-induced NO production in macrophages [12] and compounds 2-4 showed MDR reversal activities in cancer cells [42,46]. However, our study appears to be the first report of the anti-inflammatory potential of compound 16 and the potential MDR reversal activity of compounds 1, 7, 8, 11, and 13 in tumor cells.…”

“…praeruptorum roots and the constituents have been reported to have modulatory effects on tumor cells such as chemopreventive [14], anti-inflammatory [10][11][12], and multidrug resistance reversal [41,42]. Therefore, we examined the biological activities of the compounds isolated from the root extracts of P. praeruptorum using several in vitro assays to evaluate various aspects of their potential anticancer properties.…”

“…It is a well-known fact that many drug-resistant tumor cells overexpress P-glycoprotein (Pgp), multidrug resistance-associated proteins (MRPs), or both, which decrease the cellular concentration of anticancer drugs and lead to MDR [41]. Furthermore, it has been reported that pyrocoumarins isolated from P. praeruptorum Dunn such as (˘)-3 1 -angeloyl-4 1 -acetoxy-cis-khellactone (Pd-la), can suppress Pgp expression, reversing the MDR it induces, and consequently sensitize drug-resistant cancer cells to common anticancer agents [42]. In the present study, we used calcein-AM, a cell-permeable MDR protein substrate to test the MDR reversing activities of the compounds isolated from the roots of P. praeruptorum in the multidrug-resistant MES-SA/Dx5 cancer cell line.…”

Recent developments on nano-ZnO catalyzed synthesis of bioactive heterocycles

“…Heterocyclic moieties are very common in naturally occurring compounds and are important because of their significant biological efficacies that include anticancer [3], cytotoxic [4], anti-malarial [5], anti-microbial [6], anti-inflammatory [7], anti-oxidant 1 3 [8] and many more [9,10]. Figure 1 represents a glimpse of marketed drugs containing heterocycles as the core structural unit [11][12][13][14][15][16].…”

<strong>CATALYSIS INVESTIGATION FOR SYNTHESIS OF 2-AMINO-4<em>H</em>-PYRAN-3-CARBONITRILES CONTAINING PROPARGYL GROUP</strong>

“…4H-pyran derivatives well distributed in many naturally occurring compounds [1]. Organic compounds containing 4H-pyran ring shown biologically activities, such as antimicrobial [2], anti-inflammatory [3], anticancer [4], etc…The synthesis of some propargylic ethers of 2-amino-4H-chromene-3-carbonitriles was reported in our previous paper [5] from resorcinol, malononitrile and benzaldehydes by three-component one-pot reaction. In continuation of our work, herein a green approach for the one pot synthesis of propargyl ester of 2-amino-3-cyano-4H-pyran derivatives has been reported.…”