A lapachol derivative active against mouse lymphocytic leukemia P-388.

Lapachol [2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthoquinone] and its analogs [2-(3,7-dimethyl-2,6-octadienyl)-3-hydroxy-1,4-naphthoquinone and 2-(3,3-dibromo-2-propenyl)-3-hydroxy-1,4-naphthoquinone] have been described, among almost a hundred synthesized analogs, as active against rat tumor Walker 256 carcinosarcoma. The acetylglucosylation of lapachol results in a compound which extends lapachol activity becoming effective against mouse lymphocytic leukemia P-388. When mice inoculated with 10(6) leukemic cells were treated with the drug during 9 days, their life span increased 80% over the control animals. Identification spectral data (uv, ir, 1H NMR, and MS) of the compound obtained by synthesis are given.

Effects of quinone derivatives on an experimental tumor.

In continuation of studies on the activity of known solid tumor inhibitors, four acetylated glycosyl derivatives of 1,4-quinones were prepared and tested against Ehrlich ascitic tumor. All four compounds significantly inhibited growth of this neoplasm. UV, IR, and mass spectra are given for the three new synthetic quinone derivatives.

[Screening of substances and extracts of plant origin in Walker carcinosarcoma 256]. / Triagem de Substâncias e estratos de origem vegetal no carcinossarcoma de Walker 256

The authors realized a series of tests with extracts or plants or substances of plant origin in the experimental tumor Walker 256 to determine whether the extracts show anticancer activity. The samples tested were obtained in the authors laboratory or came from other centers. Thirty extracts, 26 of which were inactive and 4 active, were tested. The results shown in the tables are primary screens.

Detection of antiviral and antitumoral fractions of Chenopodium amaranticolor leaf extract.

Based on the fact that Chenopodium amaranticolor extracts showed inhibitory activity against tobacco mosaic virus (TMV) and Ehrlich tumour (EA), tests were carried out to investigate whether the antiviral and antitumoral activity were caused by the same compounds. When the extract was purified by CM Sephadex C-25 column, after precipitation with 90% ammonium sulphate, twenty active fractions against TMV and two pools of fractions active against EA were obtained. Only one fraction with high absorbance values at 260 and 280 nm was able to inhibit both TMV and EA. When the extract was purified by Bio Gel P-60 column two active fractions against TMV and EA were obtained, suggesting that they were contained in the 0.01 M fraction of the CM Sephadex column. It is suggested that C. amaranticolor leaf extract contained at least two protein-like substances manifesting antiviral and antitumoral activity.