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Antitumor activity of Pulsatilla koreana saponins and their structure-activity relationship.

Pulsatilla koreana or Korean pasque flower belongs to the family Ranunculaceae and is common in Korea. The roots of Pulsatilla koreana have traditionally been used to treat several diseases such as malaria and amoebic dysentery. Pulsatilla koreana contains many phytochemicals including saponins, ranunculin, anemonin and triterpenes. The aim of this study was to determine the antitumor and cytotoxic properties of saponins from the root of Pulsatilla koreana.

First, the researchers measured the in-vitro cytotoxic activity against cultured human solid cancer cells and the in-vivo anti-cancer activity in mice bearing lung carcinoma. In total 17 saponins from the lupane type or oleanane type were isolated and tested. The saponins with a free acidic group at C-28 of aglycon showed moderate to considerable in-vitro cytotoxic activity against tumor lines. Saponins with a free hydroxyl group at C-23 showed only moderate cytotoxicity. In general, the cytotoxicity of lupane saponins was weaker that that of oleanane saponins.

The in-vivo antitumor activity was determined of 15 saponins, which could be isolated in sufficient quantities from the Pulsatilla koreana roots. The saponins caused no evidence of toxicity in normal mice. The hederagenin saponins showed stronger antitumor effect than the taxol and doxorubicin saponins. The presence of a hederagenin aglycones and a special sugar sequence at C-3 are essential factors for the antitumor activity of saponins. There was no clear relationship between the in-vitro cytotoxicity and in-vivo antitumor activity. In general the oleanane saponins showed more in-vitro cytotoxicity and in-vivo antitumor activity than the lupane type.

Source: Bang SC, Lee JH, Song GY, Kim DH, Yoon MYand Ahn BZ. Antitumor activity of Pulsatilla koreana saponins and their structure-activity relationship. . Chemical & Pharmaceutical Bulletin. 2005 November;53(11):1451-4

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