Abstract
Abstract Andrographolide is a lactone diterpenoid compound isolated from the medicinal plant Andrographis paniculata. The anticancer activity of andrographolide has been previously demonstrated both in vitro and in vivo. We recently synthesized an andrographolide derivative, ANDRO-FL, in which a fluorescent chemical structure was covalently conjugated to andrographolide. We found that ANDRO-FL exhibited potent anticancer activity: ANDRO-FL reduced the viability of various types of cancer cells; ANDRO-FL suppressed the migration activity of melanoma cells; ANDRO-FL treatment induced the cleavage of heat shock 90 protein (Hsp90) as well as the downregulation of Hsp90 client oncoproteins such as v-Src and Bcr-abl. Notably, in all aforementioned experiments, ANDRO-FL showed stronger inhibitory effects than andrographolide. The kinetics and distribution of ANDRO-FL in cancer cells were further examined using fluorescence microscopy. The fluorescent signals could be detected within the cells in five minutes after ANDRO-FL treatment and the intensity increased as incubation time increased. Furthermore, the fluorescent signal could be detected in nucleus, cytoplasm, mitochondria, and lysosome. In vitro binding assays demonstrated that ANDRO-FL could covalently bind to several known target proteins of andrographolide, including NF-kB, GST and hnRNP K. In summary, our data indicate that ANDRO-FL is a promising anticancer compound. Moreover, with comparable anticancer profile to andrographolide, Andro-FL can serve an effective tool to further explore the molecular targets underlying the anticancer mechanism of andrographolide. The in vivo anticancer activity of ANDRO-FL is currently under investigation. Citation Format: Ya-Hsin Hsu, Yu-Ling Hsu, Sheng-Hung Liu, Hsin-Chia Liao, Po-Xuan Lee, Chao-Hsiung Lin, Lee-Chiang Lo, Shu-ling Fu. A new fluorescence-based andrographolide exhibits anticancer activity. [abstract]. In: Proceedings of the AACR Special Conference on Translation of the Cancer Genome; Feb 7-9, 2015; San Francisco, CA. Philadelphia (PA): AACR; Cancer Res 2015;75(22 Suppl 1):Abstract nr A2-30.
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