Abstract
Organic anion transporting polypeptides (OATPs) mediate the uptake of numerous structurally diverse compounds. The normally liver‐specific OATP1B3 is also expressed in different cancers, suggesting that it can be a therapeutic target for anticancer drug delivery. Because OATP1B3 also transports chemotherapy drugs, we established a cell based assay to screen for novel cytotoxic OATP1B3 substrates. We screened a library of Kansas plant extracts to isolate and chemically identify novel cytotoxic compounds that could be developed as lead compounds to treat OATP1B3‐expressing cancers. In this study, we used Chinese Hamster Ovary (CHO) cells that stably express OATP1B3 and measured cell viability of wild‐type and OATP1B3‐expressing CHO cells in the presence of Kansas plant extracts of different polarities using a luminescent cell viability assay. We identified the butanol fractions of Rhus aromatica (V345) and Rhus glabra (V585) that kill OATP1B3‐expressing CHO cells at much lower concentrations than wild‐type CHO cells, suggesting that these extracts contain cytotoxic OATP1B3‐substrates. We will further sub‐fractionate these extracts to isolate and chemically identify the cytotoxic natural products. In conclusion, this cell‐based viability assay might be a good tool to identify potential cytotoxic OATP1B3 substrates that can be delivered into OATP1B3‐expressing cancers.
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