Abstract

Propolis has been used to treat several diseases since ancient times, and is an important source of bioactive natural compounds and drug derivatives. These properties have kept the interest of investigators around the world, leading to the investigation of the chemical and biological properties and application of propolis. In this report, the chemical constituents that are responsible for the anticancer activities of propolis were analyzed. The propolis was sourced from Al-Baha in the southern part of the Kingdom of Saudi Arabia. Standard protocols for chemical fractionation and bioactivity-guided chemical analysis were used to identify the bio-active ethyl acetate fraction. The extraction was performed in methanol and then analyzed by gas chromatography-mass spectrometry (GC-MS). The major compounds are triterpenoids, with a relative concentration of 74.0%; steroids, with a relative concentration of 9.8%; and diterpenoids, with a relative concentration of 7.9%. The biological activity was characterized using different approaches and cell-based assays. Propolis was found to inhibit the proliferation of cancer cells in a concentration-dependent manner through apoptosis. Immunofluorescence staining with anti-α-tubulin antibodies and cell cycle analysis indicated that tubulin and/or microtubules are the cellular targets of the L-acetate fraction. This study demonstrates the importance of Saudi propolis as anti-cancer drug candidates.

Highlights

  • Propolis has been used to treat several diseases since ancient times, and is an important source of bioactive natural compounds and drug derivatives

  • After 24 hours of incubation, we observed only 3.7% living cells and 52.2% early stage apoptotic cells, and 41% of the cell population was in the late apoptotic stage (Fig. 4D). These results clearly indicate that the L-acetate fraction of the Saudi propolis induces apoptosis in Jurkat cells

  • We investigated the anti-proliferative effect of an ethyl acetate fraction of local Saudi propolis (L-acetate fraction) against a number of cancer cell lines

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Summary

Introduction

Propolis has been used to treat several diseases since ancient times, and is an important source of bioactive natural compounds and drug derivatives These properties have kept the interest of investigators around the world, leading to the investigation of the chemical and biological properties and application of propolis. An important aspect of the properties/characteristics could be related to geographical location, because the plant sources and collecting season for honeybees are different, adding another important factor to the diversity of the propolis chemical constituents and thereby adding to the biological activities[47]. Honeybees produce a considerable amount of propolis in the Al-Bahah region, where many beekeepers focus only on honey production

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