Journal of Pharmaceutical Research International

Aims: This study was undertaken to characterize the bioactive constituents of Apium leptophyllum fruits and to evaluate their cytotoxicity, anti-inflammatory and alpha-amylase inhibitory effects.

Study Design: Isolation and identification of the phytochemicals from the petroleum ether and methanol extracts and investigation of the cytotoxicity, anti-inflammatory and α-amylase inhibitory activities.

Place and Duration of Study: Faculty of Pharmacy, Mansoura University, Egypt and College of Pharmacy, University of Louisiana at Monroe, USA, between June 2013 and January 2016.

Methodology: In the course of our study on Apium leptophyllum fruits, six compounds were isolated and purified using different chromatographic techniques and their structures were determined on the basis of their spectroscopic data (IR, NMR, MS). The cytotoxic, anti-inflammatory and α-amylase inhibitory activities of the prepared fruit essential oil as well as the isolated compounds were performed.

Results: Pentacosanol, 1-nonadecanol and 7α-hydroxy stigmasterol are reported for the first time from family Apiaceae, corosolic acid from genus Apium and β-sitosterol from Apium leptophyllum fruits along with the previously reported compound 8-hydroxy cuminic acid. The essential oil and 8-hydroxy cuminic acid exhibited the highest cytotoxic activity against cell lines of human hepatocellular carcinoma (HePG-2) with IC₅₀ = 28.3 and 29.0 μg/mL and human breast carcinoma (MCF-7) with IC₅₀ = 10.4 and 12.6 μg/mL, respectively. They also revealed a remarkable anti-inflammatory activity with 49.54% and 34.83% inhibition, respectively. The essential oil activity on tested cell lines of other types of human breast carcinoma alongside with that of an immortalized, non-tumorigenic human mammary epithelial (MCF10A) suggests a highly selective cytotoxic effect against MCF-7 cell line. Moreover, 8-hydroxy cuminic acid showed a good α-amylase inhibitory activity with 54.21% inhibition (IC₅₀ = 43.75 µg/mL).

Conclusion: A new scientific evidence for the ethnopharmacological use of the herb in inflammatory conditions and describe, for the first time, the selective cytotoxic activity of the fruit essential oil.