1. Phytochemical investigations of two South African plants 26 June 2007 Presentation by Eric Khorombi Researcher CSIR Biosciences Bioprospecting platform

2. © CSIR 2007 www.csir.co.za Introduction On Cancer Currently the CSIR screens extracts in vitro for anti-cancer activity against a panel of 3 human cancer cell lines namely, - melanoma UACC-62, - renal carcinoma TK-10, and - breast adenocarcinoma MCF-7. The screening technology was adopted from the NCI who host a 60 cell line panel

3. © CSIR 2007 www.csir.co.za Introduction continues Three plants were investigated and will now be discussed - Phylica paniculata Willd. - Pergularia daemia (Forsk.) Chiov. The plants chemistry will now be discussed with much emphasis on the - Extracts preparations - Testing of extracts in vitro for anti-cancer activity - Bioguided fractionation to isolate the active compounds

4. © CSIR 2007 www.csir.co.za Plant 1: Phylica paniculata Willd. Family: Rhamnaceae

5. © CSIR 2007 www.csir.co.za Phylica paniculata (plant 1) Literature review There are no records of previous biological or phytochemical studies on P. paniculata. A phytochemical report on the related species P. rogersii describes the isolation of the four alkaloids - reticuline, - methylcoclaurine, - isocorydine and - lauroscholtzine

6. © CSIR 2007 www.csir.co.za P paniculata Extraction & Testing for bioactivity

7. © CSIR 2007 www.csir.co.za P. paniculata bioassay guided fractionation

8. © CSIR 2007 www.csir.co.za Anti-cancer results of active compound from P. paniculata. TGI = 12.5 µg/ml NCI TGI = 3.45 E-5 M µg/ml

9. © CSIR 2007 www.csir.co.za Other compound from P. paniculata TGI > 25 µg/ml

10. © CSIR 2007 www.csir.co.za Discussions & Conclusions (plant 1) Triterpenoids have proved to have anti-cancer activity The active compound ursolic acid was patented for use as an anti-cancer agent by Japanese scientists Studies show that synthetic derivatives of this class of compounds have improved activity Since there is no record of prior isolation of compounds in this plant species, the results of this study will be published.

11. © CSIR 2007 www.csir.co.za Plant 2: Pergularia daemia (Forsk.) Chiov. Family: Asclepiadaceae

12. © CSIR 2007 www.csir.co.za Literature review Decoctions of this plant are taken for venereal diseases, arthritis, muscular pain, asth­ma and rheumatism This plant is reported to contain - Alkaloids - Glycosides From related species P. extensa was isolated - Cardenolides which were tested and showed anticancer activity Pergularia daemia (plant 2)

13. © CSIR 2007 www.csir.co.za Pergularia daemia Extraction & Testing for bioactivity TGI ~ 25 µg/ml

14. © CSIR 2007 www.csir.co.za P. daemia bioassay guided fractionation

15. © CSIR 2007 www.csir.co.za P. daemia Fractionation result Repeated flash chromatography of the organic extract afforded - β -sitosteryl glucoside, - β-sitosterol, - α-amyrin, - 3-O-acetyl-α-amyrin and, - a disaccharide, sucrose.

16. © CSIR 2007 www.csir.co.za Anti-cancer results of active compound from P. daemia. TGI ~ 6.25 µg/ml

17. © CSIR 2007 www.csir.co.za Anti-cancer results of compound from P. daemia.

18. © CSIR 2007 www.csir.co.za Disscussions & Conclusions (plant 2) The plant contains triterpenoids and steroidal compounds but of no significant anti-cancer activity The active compound coroglaucigenin was isolated previously from a different plant species Hence, an article for publication was drafted and awaiting approval. - The

19. © CSIR 2007 www.csir.co.za General remarks Cancer is a dreadful killer disease Research in this area needs to be strengthened Plants have proved to be a good source for biologically active compounds It is necessary to continue finding the clues

20. © CSIR 2007 www.csir.co.za Acknowledgements My thanks go to NRF for financial support. To my supervisors: - Prof Fanie van Heerden and - Prof Gerda Fouché

21. Thank you