Liquid-liquid chromatography separation of guaiane-type sesquiterpene lactones from ferula penninervis Regel & Schmalh. and evaluation of their in vitro cytotoxic and melanin inhibitory potential


Luca S.V. Gaweł-Bęben K. Strzępek-Gomółka M. Jumabayeva A. Sakipova Z. Xiao J. Marcourt L. Wolfender J.-L. Skalicka-Woźniak K.
October-1 2021MDPI

International Journal of Molecular Sciences
2021#22Issue 19

Ferula penninervis Regel & Schmalh. is a perennial plant used in Kazakh traditional folk medicine to treat epilepsy, neurosis, rheumatism, gastroduodenal ulcers, dyspepsia, wounds, ab-scesses or tumors. The aim of this work was to isolate series of sesquiterpene lactones from a crude methanolic root extract and investigate their in vitro cytotoxic potential against androgen-dependent prostate cancer LNCaP and epithelial prostate PNT2 cells, as well as to evaluate their melanin production inhibitory effects in murine melanoma B16F10 cells stimulated with α-melanocyte-stimulating hormone (αMSH). Two new (penninervin P and penninervin Q) and five known (olgin, laferin, olgoferin, oferin and daucoguainolactone F) guaiane-type sesquiterpene lactones were isolated with the use of a simple and fast liquid-liquid chromatography method. Olgin and laferin showed the most promising cytotoxic effects in LNCaP cells (IC50 of 31.03 and 23.26 µg/mL, respectively). Additionally, olgin, laferin, olgoferin, and oferin (10 µg/mL) potently impaired melanin release (40.67–65.48% of αMSH + cells) without influencing the viability of B16F10 cells. In summary, our findings might indicate that guaiane-type sesquiterpene lactones from F. penninervis could be regarded as promising candidates for further research in discovering new therapeutic agents with anti-prostate cancer and skin depigmentation properties.

Countercurrent chromatogra-phy , Ferula penninervis , Ferupennin P-Q , Melanin inhibition , Prostate cancer , Sesquiterpene lactones

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Biothermodynamics, TUM School of Life Sciences, Technical University of Munich, Freising, 85354, Germany
Department of Pharmacognosy, “Grigore T. Popa” University of Medicine and Pharmacy Iasi, Iasi, 700115, Romania
Department of Cosmetology, University of Information Technology and Management in Rzeszów, Rzeszów, 35-225, Poland
School of Pharmacy, Kazakh National Medical University Named after S.D. Asfendiyarov (KazNMU), Almaty, 050012, Kazakhstan
Nutrition and Bromatology Group, Department of Analytical Chemistry and Food Science, Faculty of Food Science and Technology, Ourense Campus, University of Vigo, Ourense, E-32004, Spain
School of Pharmaceutical Sciences, University of Geneva, CMU-Rue Michel-Servet 1, Geneva 4, 1211, Switzerland
Institute of Pharmaceutical Sciences of Western Switzerland, IPSWS, University of Geneva, CMU, Geneva 4, 1211, Switzerland
Independent Laboratory of Natural Products Chemistry, Medical University of Lublin, Lublin, 20-093, Poland

Biothermodynamics
Department of Pharmacognosy
Department of Cosmetology
School of Pharmacy
Nutrition and Bromatology Group
School of Pharmaceutical Sciences
Institute of Pharmaceutical Sciences of Western Switzerland
Independent Laboratory of Natural Products Chemistry

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