Use of Potato Disc and Brine Shrimp Bioassays to Detect Activity and Isolate Piceatannol as the Antileukemic Principle from the Seeds of Euphorbia lagascae

Abstract

EtOH extracts of the seeds of Euphorbia lagascae inhibited crown gall tumors on potato discs, were active against 3PS (in vivo) and 9PS (in vitro) mouse leukemia, and were toxic to brine shrimp. Using the potato disc and brine shrimp bioassays to monitor fractionation, piceatannol (3,4,3',5'- tetrahydroxystilbene ) was isolated as the 3PS active principle. Aesculetin (6,7-dihydroxycoumarin) was isolated in large quantity, was weakly cytotoxic in 9KB , but was inactive in the other bioassay systems. Sucrose was also isolated. A combination of the simple crown gall and brine shrimp bioassays can thus be used both to detect and to isolate plant antitumor substances, minimizing the need for extensive antitumor testing in vivo.

Piceatannol, Natural Polyphenolic Stilbene, Inhibits Adipogenesis via Modulation of Mitotic Clonal Expansion and Insulin Receptor-dependent Insulin Signaling in Early Phase of Differentiation

“…Piceatannol (trans-3,4,3Ј,5Ј-tetrahydroxystilbene) is a natural polyphenolic stilbene present in grapes, red wine (18), and Euphorbia lagascae seeds (19). It is suggested to have anti-cancer and anti-inflammatory properties (20 -22), and this beneficial impact may stem from its inhibitory effects on various kinase activities, including spleen tyrosine kinase (Syk) and PI3K, and nuclear factor-B-mediated gene expression (22,23).…”

Extracts of Centaurea bornmuelleri and Centaurea huber-morathii inhibit the growth of colon cancer cells in vitro

“…The BSL assay has been used routinely in the primary screening of the crude extracts as well as the isolated compounds to assess the toxicity towards brine shrimps, which could also provide an indication of possible cytotoxic properties of the test materials (Ferrigni et al, 1984). It has been established that the cytotoxic compounds usually show good activity in the BSL assay, and this assay can be recommended as a guide for the detection of antitumour and pesticidal compounds because of its simplicity and cost-effectiveness (McLaughlin, 1991).…”

Kinase Activity is Required for Growth Regulation but not Invasion Suppression by Syk Kinase in Pancreatic Adenocarcinoma Cells

“…We observed localization of syk to the perinuclear region of dividing PDAC cells (not shown), therefore we assessed whether syk might be involved in regulating the proliferation of endogenously syk-positive PDAC cells in a manner analogous to that described in breast cancer (Coopman et al, 2000). Consistent with such a role, the in vitro growth of endogenously syk-positive CAPAN2, CFPAC1, BxPC3 and AsPC1 cells was suppressed in a dose-dependent manner by piceatannol, a phytochemical that inhibits the kinase activity of syk, suppressing downstream phosphorylation events by a largely unknown mechanism (Geahlen et al, 1989;Ferrigni et al, 1984;Wieder et al, 2001) (Fig.3A). Significantly, the only G1 cells in this group, CAPAN2, were completely eradicated by the highest dose of inhibitor, suggesting cytotoxicity in addition to any cytostatic effect of this compound in these highly differentiated cells.…”