Abstract

To isolate and characterize anti-tumor compounds through nuclear magnetic resonance (NMR) spectroscopy of ethyl acetate extract of R. japonicus Houtt root and their cytotoxic effects were evaluated in terms of measuring inhibition of growth of three cancer cell lines: human hepatoma cells (HepG2), cerebral glioma cells (U251) and ovarian carcinoma cells (SK-OV-3/DDP). The roots of R. japonicus Houtt were extracted with ethanol, and partitioned with petroleum ether, dichloromethane and ethyl acetate, respectively. The ethyl acetate extract was separated chromatographically using macroporous resin, positive and negative phase silica gel and high performance liquid chromatography. The structures of isolated compounds were elucidated by nuclear magnetic resonance (NMR) spectral data. Ten compounds were isolated form the ethyl acetate extract of R. japonicus roots. Their structures were determined as emodin (1), chrysophanol (2), aloe emodin (3), physcion (4), quercetin (5), resveratrol (6), β-sitosterol (7), 3β-acetoxy-28-hydroxyurs-12-ene (8), sucrose (9) and dibutyl phthalate (10). Among of them, compounds 1, 3, 4, 6 and 8 exhibited highly significant (p<0.05) cytotoxicities against HepG2 to a certain extent. Compounds 3-6 exhibited moderate cytotoxicities against U251 with IC50 values of 19.8, 23.5, 23.8 and 17.8 µM, respectively. Compounds 1, 2 and 7 also exhibited cytotoxicities against U251 to a certain extent with IC50 values of 48.3, 50.1 and 85.3 µM, respectively. Compounds 1-6 exhibited moderate cytotoxicities against (SK-OV-3/DDP) with IC50 values of 62.8, 64.2, 31.3, 61.0, 47.4 and 42.0 µM, respectively.

Highlights

  • Since prehistoric times, human beings have been using plants as folkloric sources of phytoconstituents of medicinal and pharmaceutical significance

  • Rumex japonicus Houtt belongs to the Polygonaceae family and is known in Traditional Chinese Medicine (TCM) as Yang-Ti

  • The objective of this study was to isolate and characterize anti-tumor compounds through nuclear magnetic resonance (NMR) spectroscopy of ethyl acetate extract of R. japonicus Houtt root and their cytotoxic effects were evaluated in terms of measuring inhibition of growth of three cancer cell lines (HepG2, U251, SK-OV-3/DDP)

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Summary

Introduction

Human beings have been using plants as folkloric sources of phytoconstituents of medicinal and pharmaceutical significance. 1961, United Stated Food and Drug Administration (FDA) has approved plant-derived anti-cancer and anti-tumor chemicals to prepare anti-cancer drugs (Lee, 1999). Rumex japonicus Houtt root has medicinal significance and in folklore and alternate medicines, it is employed for various medicinal benefits like as a antitumor, anti-inflammatory, purgative and detox agent and as an alternate medicine for skin treatment, scabies, regulation of blood circulation and wastes clearance out of body (Lee et al, 2006; Xie & Yang, 2014). R. japonicus Houtt comprises of rich quantities of several phytoconstituents of pharmaceutical significance, such as oxanthrones, anthraquinones, nepodin, rutin and phenolic compounds in its roots (Zhou et al, 2005)

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