Abstract

Tephrosia apollinea is a perennial shrublet widely distributed in Africa and is known to have medicinal properties. The current study describes the bio-assay (cytotoxicity) guided isolation of (-)-pseudosemiglabrin from the aerial parts of T. apollinea. The structural and stereochemical features have been described using spectral and x-ray crystallographic techniques. The cytotoxicity of isolated compound was evaluated against nine cancer cell lines. In addition, human fibroblast was used as a model cell line for normal cells. The results showed that (-)-pseudosemiglabrin exhibited dose-dependent antiproliferative effect on most of the tested cancer cell lines. Selectively, the compound showed significant inhibitory effect on the proliferation of leukemia, prostate and breast cancer cell lines. Further studies revealed that, the compound exhibited proapoptotic phenomenon of cytotoxicity. Interestingly, the compound did not display toxicity against the normal human fibroblast. It can be concluded that (-)-pseudosemiglabrin is worthy for further investigation as a potential chemotherapeutic agent.

Highlights

  • Chemotherapy can be defined as the use of chemicals to treat cancer by preventing cancer cells from dividing, proliferating and surviving

  • Chemopreventive agents derived from natural products or their synthetic derivatives have shown cell growth inhibition, antiproliferation and apoptosis in various cancer cell lines [5]

  • Comparing with some other flavones tested against U937 cell line [41,42,43], results of the present study revealed that SSG exhibited more pronounced cytotoxic efficacy

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Summary

Introduction

Chemotherapy can be defined as the use of chemicals to treat cancer by preventing cancer cells from dividing, proliferating and surviving. Chemotherapeutic agents can be divided into two major groups: natural products and synthetic. More than 27% of all prescription drugs are derived from natural sources [1]. This is more significant with regard to anti-cancer drugs in which more than 80% are plant-derived compounds [2]. It is reported that natural compound(s) especially of plant origin, with selective cytotoxicity against specific tumor cell line, can offer either prophylaxis (chemoprevention) or a relatively safer treatment option with minimum side effect [4]. Chemopreventive agents derived from natural products or their synthetic derivatives have shown cell growth inhibition, antiproliferation and apoptosis in various cancer cell lines [5]. Retinoids and antiestrogens are known to block or delay the progression of transformed cells by modulating cell proliferation or differentiation, these agents are believed to promote cytostatic effects [6,7,8]

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