Cytotoxic activity and aryltetraline lignans of Linum persicum Kotschy ex Boiss.

Authors

Abstract

Podophyllotoxins represent an important and unique position among natural products. They serve as the starting material for the semi-synthetic anticancer drugs etopside and teniposide, so considerable attention has focused on the availability of these aryltetralin lignans. Linum is one of the genera, with some reports on the presence of podophyllotoxin and related compounds, such as L. album, L. flavum, L. capitatum and L. catharticum. Linum persicum is an endemic plant, which grow wildly in Dena Mountains in Iran. The purpose of this study was to investigate the cytotoxic activity of L. persicum and isolation of aryltetralin lignans from the plant.
The cytotoxicity of the total extract and two lignan rich fractions of Linum persicum were evaluated by MTT assay on five different cell lines. Three aryltetralin lignans were isolated from the methanolic extract of the aerial parts of L. persicum by column chromatography and preparative TLC.
The total extract showed the highest cytotoxicity among the other fractions. According to the results the most cytotoxic effect was seen on K-562 cell line and among them the total extract were more active (IC50=1.29). All of them were more active against human chronic myeloid leukemia (K-562), T cell lines (jurkat) and lung carcinoma (A5). Podophyllotoxin, 5-methoxy podophyllotoxin and 5-methoxy podophyllotoxin acetate have been isolated and their structures have been confirmed by 1H-NMR and Mass spectra. Linum persicum can be considered as a new source of podophyllotoxin.

Iranian Journal of Pharmaceutical Research (2004): Supplement 2

Iranian Journal of Pharmaceutical Research (2004): Supplement 2: 74-74
Poster Presentations
/Biological Effect of Medicinal Plants

2nd International Congress on Traditional Medicine and Materia Medica
October 4-7, 2004, Tehran, Iran

220

Cytotoxic activity and aryltetraline lignans of Linum persicum Kotschy ex Boiss.

Javidnia K.1 & 2, Miri R.1 & 2, Rezai H.1, Jafari A.3, Azarmehr A.4, Amirghofran Z.2 & 4

1Department of Medicinal Chemisrty, Faulty of Pharmacy, Shiraz university of Medical Sciences Shiraz, Iran 2Medicinal & Natural Products Chemistry Research Centre, The Medical Sciences University of Shiraz, Shiraz, Iran 3Central Research of Natural Resource and Animal Husbandry, Yasuje, Iran 4Department of Immunology, Faculty of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran

Podophyllotoxins represent an important and unique position among natural products. They serve as the starting material for the semi-synthetic anticancer drugs etopside and teniposide, so considerable attention has focused on the availability of these aryltetralin lignans. Linum is one of the genera, with some reports on the presence of podophyllotoxin and related compounds, such as L. album, L. flavum, L. capitatum and L. catharticum. Linum persicum is an endemic plant, which grow wildly in Dena Mountains in Iran. The purpose of this study was to investigate the cytotoxic activity of L. persicum and isolation of aryltetralin lignans from the plant.

The cytotoxicity of the total extract and two lignan rich fractions of Linum persicum were evaluated by MTT assay on five different cell lines. Three aryltetralin lignans were isolated from the methanolic extract of the aerial parts of L. persicum by column chromatography and preparative TLC.

The total extract showed the highest cytotoxicity among the other fractions. According to the results the most cytotoxic effect was seen on K-562 cell line and among them the total extract were more active (IC50=1.29). All of them were more active against human chronic myeloid leukemia (K-562), T cell lines (jurkat) and lung carcinoma (A5). Podophyllotoxin, 5-methoxy podophyllotoxin and 5-methoxy podophyllotoxin acetate have been isolated and their structures have been confirmed by 1H-NMR and Mass spectra. Linum persicum can be considered as a new source of podophyllotoxin.

Presenting Author: Javidnia, K. javidniak@sums.ac.ir