Biological Activities of Alkaloids fromPseuduvaria setosa.

Abstract

Two dioxoaporphine alkaloids, N-methylouregidione (1) and ouregidione (2), and two oxoaporphine alkaloids, liriodenine (3) and oxostephanine (4), were isolated from the aerial part of Pseuduvaria setosa (King) J. Sinclair. All four alkaloids displayed antituberculosis activity against Mycobacterium tuberculosis, with 3 as the most active at minimum inhibitory concentration (MIC) of 12.5 mg=ml. Compound 3 was also the only alkaloid isolated from this plant that displayed antimalarial activity against Plasmodium falciparum with the 50% inhibitory concentration (IC 50) of 2.8 mg=ml. Compounds 3 and 4 were strongly cytotoxic to both epidermoid carcinoma (KB) and breast cancer (BC) cell lines, whereas 2 was moderately active against BC cells. Both 1 and 2 were active against small cell lung cancer (NCI-H187) cell line and were able to stimulate lymphocyte proliferation with stimulation indices (SI) of more than 1.

Antiproliferative effect of alkaloidsviacell cycle arrest fromPseuduvaria rugosa

“…In the present study, we examined the antiproliferative activity of the other two alkaloids isolated from leaves and twigs of P. rugosa, 1,2,3-trimethoxy-5-oxonoraporphine and ouregidione, on human leukemic cell lines. Previous reports showed that ouregidione exhibited larvicidal activity against the mosquito Aedes aegypti (Ee et al, 1999), cytotoxic activities against human breast cancer (BC) and human small lung cancer (NCI-H187) (Wirassathien & Boonarkart, 2006), together with cytotoxicity towards DNA repair-deficient strains, RAD 52Y and RS 321 (Wijeratne et al, 1996). The results of the MTT reduction assay found that 1,2,3-trimethoxy-5-oxonoraporphine and ouregidione induced cytotoxicity of HL-60, U937 and K562 cells in a dose-dependent manner whereas 1,2,3-trimethoxy-5-oxonoraporphine is more active than ouregidione.…”

Brief Review on Bioactive Compounds from Pseuduvaria Species

“…Biological activities of the four oxoaporphine alkaloids, N-methylouregidione, ouregidione, liriodenine and oxostephanine, isolated from the aerial part of Pseuduvariasetosashowed in vitroantituberculosis activity against Mycobacterium tuberculosis with MIC values of 100, 12.5 and 25 g/ml, respectively [16]. These results have demonstrated that aporphine alkaloids can be developed as potential anti-tubercular agents in chemotherapy [17].…”

Antiparasitic activity of alkaloids from plant species of Papua New Guinea and Australia

“…The antimalarial activity of these compounds has been previously reported against P. falciparum Dd2 strain for the Flindersia alkaloids [5], against D6 and W2 strains for xylopine and voacamine [12,13] and against K1 strain for liriodenine [14]. However, as the activity can vary against P. falciparum strains with differing drug resistance profiles, in this study the antimalarial activity of the isolated compounds was assessed against a panel of both drug-sensitive (3D7) and drug-resistant (FCR3, HB3 and K1) strains (Table 1).…”