Abstract
Efficient screening of anticancer agents is in urgent need to develop new drugs that combat malignant tumors and drug resistance. In this study, a combined strategy composed by solvent partition and HPLC fractionation was developed to generate an herbal fraction library of Salviae Miltiorrhizae Radix et Rhizoma to quickly and efficiently screen anticancer agents. All library entries are directed into 96 well plates which are well mapped with HPLC chromatograms. The cell proliferation assay revealed seven active subfractions. Then, the major active ten peaks in these subfractions were prepared and isolated by semipreparative HPLC, and their inhibitory activities against prostate cancer cells were then tested at the same concentration level, leading to the identification of several active compounds. In addition, the structures of compounds arucadiol (2), 15,16-dihydrotanshinone I (4), methyl tanshinonate (5), cryptanshinone (7), 1,2-dihydrotanshinquinone I (9), and tanshinone IIA (10) were characterized by mass spectrometry and X-ray crystallographic analysis, and they were confirmed to be active in suppressing prostate cancer cell proliferation at 7.5 or 15 μg/mL, among which, the minor compounds 2, 4, and 5 showed higher activities than 9 and 10. This study provided a rapid strategy of identifying new anticancer agents in Salviae Miltiorrhizae Radix et Rhizoma, which can be applied in other herbal medicines.
Highlights
Herbal medicines, including certain extractions, or formulated traditional medicines, have been used for the treatment of various chronic and infectious diseases for thousands of years worldwide
In order to rapidly and systematically identify antitumor components in Salviae Miltiorrhizae Radix et Rhizoma, it is necessary to develop an herbal fractional library that contains all the chemical components that possess sufficient purity for biological assays. erefore, we developed a combined strategy composed with solvent partition and HPLC fractionation to generate the herbal fraction library of Salviae Miltiorrhizae Radix et Rhizoma
To rapidly identify the active components that can inhibit prostate cancer cell growth, Salviae Miltiorrhizae Radix et Rhizoma was extracted with methanol, and the crude extract was divided into three fractions: ether, ethyl acetate, and water soluble
Summary
Herbal medicines, including certain extractions, or formulated traditional medicines, have been used for the treatment of various chronic and infectious diseases for thousands of years worldwide Nowadays, they continue to play an important role in healthcare, and especially in new drug discoveries [1, 2]. Tanshinone I inhibited TNFα-induced VEGF (vascular endothelial growth factor) production in breast cancer MDA-MB-231 cells and suppressed the migration of MDA-MB-231 cells through impacting extracellular matrix [25, 26] Another tanshinone, cryptotanshinone, was shown to inhibit prostate cancer DU145 cells through the inhibition of STAT3 (signal transducer and activator of transcription 3) [27]. In order to rapidly and systematically identify antitumor components in Salviae Miltiorrhizae Radix et Rhizoma, it is necessary to develop an herbal fractional library that contains all the chemical components that possess sufficient purity for biological assays. We describe here the strategy and the library-based screening results for their anticancer potential
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