Abstract

In recent years, herbal medicine has experienced rapid development in the search for alternative anticancer compounds. Various phytochemicals present in Quercus infectoria (QI) galls have been reported to trigger cytotoxic effects on many types of cancer cells. However, a specific active constituent of QI galls with the potential to inhibit highly invasive stage IV malignant brain tumor, glioblastoma multiforme (GBM), is yet to be discovered. In this study, a two-phase system composed of aqueous soxhlet extraction and methanolic enrichment fractionation was employed to extract an anticancer compound, gallotannin, from the QI galls. This optimized two-phase system successfully generated a fraction (F4) with ~71% gallotannin, verified by the TLC and HPLC assays. Astoundingly, this fraction showed significantly higher (~1.15-fold) antioxidant activities compared to its crude extract, as well as to a commercial synthetic pure gallotannin. The F4 was also found to significantly suppress GBM cell growth, better than the synthetic pure gallotannin and the QI gall crude extract, probably related to its significantly higher antioxidant property. Moreover, the inhibitory effects exerted by the F4 treatment on GBM cells were comparable to the effects of two clinically used chemo-drugs (Temozolomide and Tamoxifen), indicating its high efficiency in combating human cancer. In conclusion, this study pioneered the development of an optimized extraction procedure for enriched yield of the natural gallotannin metabolite from the galls of the QI medicinal plant with high antioxidant potential and inhibitory effects on human GBM cells.

Highlights

  • Glioma is a broad category of tumors that occur primarily in the brain and spinal cord

  • Based on their location and presumed cell of origin, gliomas can be categorized into astrocytomas, oligodendrogliomas, ependymomas and mixed gliomas [2]

  • From 50 g of Quercus infectoria (QI) gall powder, ~9.45 g (18.9%) of crude extract powder was obtained from aqueous extraction

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Summary

Introduction

Glioma is a broad category of tumors that occur primarily in the brain and spinal cord. Almost 80% of all types of malignant brain tumors and 30% of the central nervous system (CNS) tumors are categorized as glioma cancers [1] Based on their location and presumed cell of origin, gliomas can be categorized into astrocytomas (derived from astrocytes, which provide nutrients and oxygen to the neurons in the brain), oligodendrogliomas (derived from oligodendrocytes, which insulate neurons with myelin sheath), ependymomas (derived from ependymal cells, which line the cavities in the brain) and mixed gliomas (a mixture of astrocytomas, oligodendrogliomas and ependymomas) [2]. Standard therapies for GBM consist of maximal surgical resection, followed

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