Antiproliferative Activity Of Compounds Research Articles

Antiproliferative Hopane and Oleanane Glycosides from the Roots ofGlinus lotoides

Three new hopane saponins, lotoidosides A - C (1 - 3), and four new oleanane saponins, lotoidosides D - G (4 - 7), were isolated from the roots of Glinus lotoides L. (Molluginaceae). Their structures were determined by extensive 1D- and 2D-NMR spectroscopy and ESI-MS analysis. The antiproliferative activity of compounds 1 - 7 was evaluated using three continuous murine and human culture cell lines J774.A1, HEK-293, WEHI-164. Compounds 1 and 3 - 7 showed significant cytotoxicity against the three cancer cell lines with IC50 values ranging from 0.018 to 0.62 microM, while compound 2 exerted a weak activity only against the cell line HEK-293.

Cytotoxic saponins from Schefflera fagueti.

Six new lupane (1 - 4) and oleanane saponins (5 and 6) were isolated from the aerial parts of Schefflera fagueti Baill. (Araliaceae). Their structures were determined by 2D-NMR spectroscopy (DQF-COSY, 1D-TOCSY, 2D-HOHAHA, 1D-ROESY, HSQC, HMBC). The antiproliferative activity of compounds 1 - 6 and of their prosapogenins (1a - 6a) was evaluated using three continuous murine and human culture cell lines J774, HEK-293, WEHI-164. Oleanane saponins 5 and 6 were the most active, showing significant inhibitory effects on all cell lines, while their prosapogenins 5a and 6a demonstrated minor activity.

Antiproliferative triterpene saponins from Trevesia palmata.

During the course of a study of plants of the family Araliaceae, antiproliferative activity was demonstrated by the crude saponin fraction of Trevesia palmata. After chromatographic purification, six new bisdesmosidic saponins (1-6), along with two known triterpenoid saponins, (7 and 8), were isolated. The structures of 1-6 were determined by (1)H-(1)H correlation spectroscopy (COSY-DQF, 1D TOCSY, 2D HOHAHA, 1D ROESY) and (1)H-(13)C (HSQC, HMBC) spectroscopy. The antiproliferative activity of compounds 1-8 and of their prosapogenins (2a-7a) prepared by alkaline hydrolysis, was evaluated using three continuous culture cell lines.

Cyclometalated Complexes of Platinum and Palladium with N-(4-Chlorophenyl)-α-benzoylbenzylideneamine. In Vitro Cytostatic Activity, DNA Modification, and Interstrand Cross-Link Studies

In the present paper we report the synthesis and structural IR and 1H and 13C NMR characterization of four platinum(II) and palladium(II) cyclometalated complexes of the formula [Pd(4-ClC6H4NC(COC6H5)C6H4)X]2, where X = OAc (2) or Cl (3), and [Pt(4-ClC6H4NC(COC6H5)C6H4)X]2, where X = Cl (4) or OAc (5). The acetate-bridged compounds 2 and 5 have an open-book structure. The chloro-bridged compounds 3 and 4 have an unfolded structure. Complex 2 crystallizes in the centrosymmetric triclinic space group P1̄, with Z = 2. Unit cell parameters are as follows: a = 11.765(3) Å, b = 12.862(4) Å, c = 15.022(5) Å, α = 84.08(2)°, β = 78.56(2)°, γ = 83.13(2)°. All these compounds were screened against MDA-MB 468 (breast carcinoma) and HL-60 (leukemic) tumor cells. The low IC50 values of compound 5 (1.05 μM) and of compound 4 (1.58 μM) against MDA-MB 468 and of 0.82 μM (5) and 1.37 μM (4) against HL-60 relative to cis-DDP (2.67 and 2.07 μM, respectively) and other cyclometalated compounds suggest that the synthesized compounds may be regarded as having potential antitumor properties. The data suggest that the antiproliferative activity of compound 5 may correlate with its covalent binding to DNA and the induction of important modifications on the helix.