Green Drugs: Anticancer Properties of Clerodendrum viscosum and Curcumin Conjugates.

摘要

This thesis aims to find potential anti-cancer drug from natural sources like plants. (i) The objectives are to find and characterize the anticancer components from the plant Clerodendrum viscosum. (ii) the synthesis of curcumin derivatives with increased solubility and amplified bioactivity.;Clerodendrum viscosum (Cv) is a traditional medicine plant in India for a long period of time employed to promote wound healing, and recently it has been found have some positive effects on cervical cancer. However, there were no direct v molecular and biochemical evidences for that. In this thesis, we made aqueous extracts (Cv-ap) from the Cv by ammonium sulfate precipitation. It was found that this extract had bioactivity against Hela cells—a human cervical cancer cell line. Caspase-3 immuno-staining proved that the Cv-ap can induce Hela cells apoptosis. It is also interesting that the Cv-ap can inhibit the movement of the cells at lower concentration without inducing cells apoptosis, which means it may stop the invasion of the cancer cells. MTT assays showed that at lower concentration the Cv-ap may not only inhibit the movement of the cells but also inhibit proliferation of the Hela cells.;For the characterization of the Cv-ap, it was found that it had glycoproteins confirmed by SDS-PAGE staining with the Pro-Q emerald 300, and by binding to the concavalin A column. For further purification, the bio-assay guided method was used to purify the bioactivity components. After Cv-ap was passed through the column, the fraction with the most activity fraction was selected and followed by heating, and finally by precipitation with 66.7% ethanol. In the end we got the bioactivity component EPHP3 fraction which has a 30 fold increasing activity when compared to the Cv-ap.;My second project aimed to overcome the difficulties associated with the low water/plasma solubility of the potent anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-Alzheimer's active curcumin. We have successfully synthesized a curcumin derivate BSA-curcumin via a one-step successfully synthesized. BSA-curcumin had the high solubility in water and good cytotoxicity to the Hela cells.;In conclusion, my research has characterized and produced novel plant derived components that have anti-cancer activity and may eventually be used in clinical therapies.