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Constituents of PG201 (Layla®), a multi-component phytopharmaceutical, with inhibitory activity on LPS-induced nitric oxide and prostaglandin E2 productions in macrophages

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Abstract

Fourteen compounds, coumarin (1), demethylsuberosin (2), xanthotoxin (3), psoralen (4), decursinol (5), decursin (6), decursinol angelate (7), chikusetsusaponin IVa (8), chikusetsusaponin IVa methyl ester (9), ethyl caffeate (10), syringaresinol (11), cnidilide (12), farnesol (13), and linoleic acid (14), were isolated from phytopharmaceutical PG201 (Layla®) by activity-guided fractionation utilizing inhibitory activity on nitric oxide (NO) production in vitro. The isolates 1–14 were evaluated for their inhibitory activity on LPS-induced NO and prostaglandin E2 (PGE2) productions in RAW 264.7 cells. All the compounds except 14 displayed suppressive effects on LPS-induced NO and PGE2 production with IC50 values ranging from 8 to 60 μM. Among these, compound 10 showed the most potent inhibitory effect on NO production from RAW 264.7 cells with an IC50 value of 8.25 μM. Compounds 2, 9, and 10 exhibited high inhibitory effects on PGE2 production with the IC50 values of 9.42, 7.51, and 6.49 μM, respectively. These findings suggest that compounds 2, 9, and 10 are the potential anti-inflammatory active constituents of PG201 and further study may be needed to explain their mechanism of action.

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Acknowledgments

This research was supported by a grant from PMG Pharma Co. Ltd., Ansan-si, Korea. We thank Korea Basic Science Institute (KBSI) for running NMR and MS experiments.

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Authors and Affiliations

  1. College of Pharmacy, Kyung Hee University, Seoul, 130-701, Republic of Korea

    Hyun Ji Kim, Hye Mi Kim, Woo-Seok Lee, Ji-Sun Shin, Kyung-Tae Lee & Dae Sik Jang

  2. Department of Life and Nanopharmaceutical Science, Kyung Hee University, Seoul, 130-701, Republic of Korea

    Byeol Ryu, Kyung-Tae Lee & Dae Sik Jang

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  1. Hyun Ji Kim
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Kim, H.J., Kim, H.M., Ryu, B. et al. Constituents of PG201 (Layla®), a multi-component phytopharmaceutical, with inhibitory activity on LPS-induced nitric oxide and prostaglandin E2 productions in macrophages. Arch. Pharm. Res. 39, 231–239 (2016). https://doi.org/10.1007/s12272-015-0654-z

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  • DOI: https://doi.org/10.1007/s12272-015-0654-z

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