Medicinal plants represent precious resources from which bioactive compounds can be isolated and developed into invaluable therapeutic agents. With the advent of modern drug discovery technologies such as combinatorial chemistry and high-throughput drug screening platforms, there is an increasing interest in utilizing medicinal plants as a source of drug leads. A wide spectrum of bioassays can be employed for the detection of bioactivity in extracts, fractions, as well as purified compounds of herbal origin. Amongst the different types of bioassays, reporter gene assays are highly versatile and reliable. The present review provides an overview of the most popular reporter genes in terms of their basic methodology, capacities and limitations. The different types of intracellular and extracellular reporter gene products and their potential applications in bioassays of natural products are also discussed.

Bupleurum & Peony Formula (Jia Wei Xiao Yao San) is a herbal formula which possesses a clinical history for the treatment of menopausal syndrome and menstrual irregularity. The present investigation reports the ability to monitor the formula's phytoestrogen content that will allow for the implementation of a standardization protocol that is based on a quantifiable biological response. Utilizing an oestrogen-sensitive chimeric receptor/reporter gene element which has been stably transfected into HeLa cells, the botanical formula was shown to induce the expression of the reporter gene, luciferase, in a dose dependent manner. Pretreatment of the HeLa cells with the botanical formula produced a 5-fold increase in bioluminescence compared with the control. Additionally, our studies showed that the response of the cells, when challenged by the botanical formula, was oestrogen specific. Pretreatment of the cells with tamoxifen effectively blocked the activation of the chimeric oestrogen receptor by the botanical formula. The cell line provides a sensitive assay that can easily detect the presence of phytoestrogens in complex botanical formulas.