Cytotoxic Activity and G2/M Cell Cycle Arrest Mediated by Antofine, A Phenanthroindolizidine Alkaloid Isolated from Cynanchum paniculatum

 

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Abstract

Starting with an extract derived from the root of Cynanchum paniculatum Kitagawa (Asclepiadaceae) that was active in the process of inhibiting the growth of human cancer cells in culture, a phenanthroindolizidine alkaloid antofine was isolated and identified as an active principle (IC₅₀ = 7.0 ± 0.2 ng/ml for A549, human lung cancer cells; IC₅₀ = 8.6 ± 0.3 ng/ml for Col2, human colon cancer cells). Prompted by the high potency of cancer cell growth inhibition, additional action mechanism studies were performed with antofine. Utilizing cultured Col2 cells as a model, antofine induced arrest in the G2/M phase of the cell cycle after 48 h of incubation. With wash-out experiment, colony formation was also inhibited in a dose-dependent manner. These data suggest the potential of antofine to serve as a cancer chemotherapeutic agent by virtue of arresting the cell cycle.

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Dr. Sang Kook Lee

College of Pharmacy

Ewha Womans University

11-1 Daehyun-dong

Seodaemun-ku

Seoul 120-750

Korea

Phone: +82-2-3277-3023

Fax: +82-2-3277-2851

Email: sklee@mm.ewha.ac.kr