Abstract
A simple and rapid method using high-speed counter-current chromatography (HSCCC), along with bioassay-guided fractionation based on the anti-proliferative activity against renal and colon cancer cells, has been developed for the preparative separation of aceroside VIII (1) and platyphylloside (2) from Betula platyphylla. A solvent system composed of ethyl acetate/acetonitrile/water (1:0.1:1, v/v/v) was optimized for the separation. The upper phase was used as the stationary phase, and the lower phase was used as the mobile phase. Among these isolated diarylheptanoids, platyphylloside (2) showed anti-proliferative activity in the COLO205 and KM12 colon cells and renal cancer cell lines A498, U031, as well as in MG63 and MG 63.3 osteosarcoma cells. In addition, it showed dose dependent inhibitory effects in the NCI 60 cell line assay. These results suggest that the diarylheptanoids isolated from B. platyphylla with an efficient HSCCC method could be potential multi-targeted therapeutic agents for cancer.
Highlights
About 58,000 individuals were diagnosed with renal cancer in 2011, accounting for 3% of the cancers in the United States. [1,2]
We evaluated the anti-proliferative activities of two studies, thewith anti-proliferative activities of two diarylheptanoids against renal cancer diarylheptanoids against renal cancer cell lines (A498, U031), colon cancer cell lines (COLO205, KM12), cell lines (A498, U031), colon cancer cell lines (COLO205, KM12), and osteosarcoma cell lines (MG63, and osteosarcoma cellthe lines (MG63, MG63.3)
We investigated the inhibitory activity of two-day drug exposure against colon and renal cancer, We andinvestigated osteosarcoma metastatic potential screening (HTS)
Summary
About 58,000 individuals were diagnosed with renal cancer in 2011, accounting for 3% of the cancers in the United States. [1,2]. Diarylheptanoids, with two aromatic rings joined by a heptane chain, are typical secondary metabolites in the genus Alnus, and widely distributed in other genera, such as Zingiber, Curcuma, Alpinia, Alpinia, and [9]. Effective application of HTS to bioactive extracts development of hits from screening campaigns into leadsinto for drug are clearlyare important and the development of hits from screening campaigns leadsdevelopment for drug development clearly to access anticancer lead compounds in secondary of natural products. (Figure 1) from a crude sample of B. platyphylla using HSCCC in stepwise elution mode
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