Identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.

Osteoporosis and resulting bone fractures are the major health issues associated with morbidity in the aging population; however, there is no effective treatment that does not cause severe side effects. In East Asia, dried seeds of Psoralea corylifolia L. (PC) have traditionally been used as an herb...

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Autores principales:	Ami Lee, Hyun Yang, Taesoo Kim, Hyunil Ha, Youn-Hwan Hwang
Formato:	article
Lenguaje:	EN
Publicado:	Elsevier 2021
Materias:	Psoralea corylifolia L. Osteoporosis Mass spectrometry Pharmacokinetics Osteoclast Cathepsin K Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/2da3cea5494e46c4bb1fedbcced4b816
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spelling	oai:doaj.org-article:2da3cea5494e46c4bb1fedbcced4b8162021-11-14T04:29:23ZIdentification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.0753-332210.1016/j.biopha.2021.112300https://doaj.org/article/2da3cea5494e46c4bb1fedbcced4b8162021-12-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S0753332221010842https://doaj.org/toc/0753-3322Osteoporosis and resulting bone fractures are the major health issues associated with morbidity in the aging population; however, there is no effective treatment that does not cause severe side effects. In East Asia, dried seeds of Psoralea corylifolia L. (PC) have traditionally been used as an herbal medicine to manage urinary tract, cutaneous, and gastrointestinal disorders, as well as bone health. However, the mechanism of action and active biocomponents of PC are unclear. Here, we adopted a pharmacokinetic (PK) study aiming to identify the bioavailable phytochemicals in aqueous and ethanolic extracts of PC (APC) and (EPC), respectively. In addition, we aimed to determine anti-resorptive constituents of PC, which accounted for its beneficial effects on bone health. To this end, we used ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). A rapid, sensitive, and reliable UPLC-MS/MS method was developed and determined the 17 PC ingredients. In the PK study, nine components (two chalcones, two coumarins, one coumestan, two flavonoids, and two isoflavonoids) were observed between 36 and 48 h after oral administration of APC or EPC. Among the bioavailable ingredients, four PC constituents (psoralidin, isobavachin, corylifol A, and neobavaisoflavone) inhibited M-CSF-and RANKL-induced osteoclast differentiation in bone marrow-derived macrophages. In addition, two chalcones and two isoflavonoids markedly inhibited cathepsin K activity, and their binding modes to cathepsin K were determined by molecular docking. In summary, our data suggest that bioavailable multicomponents of PC could contribute to the management of bone health.Ami LeeHyun YangTaesoo KimHyunil HaYoun-Hwan HwangElsevierarticlePsoralea corylifolia L.OsteoporosisMass spectrometryPharmacokineticsOsteoclastCathepsin KTherapeutics. PharmacologyRM1-950ENBiomedicine & Pharmacotherapy, Vol 144, Iss , Pp 112300- (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Psoralea corylifolia L. Osteoporosis Mass spectrometry Pharmacokinetics Osteoclast Cathepsin K Therapeutics. Pharmacology RM1-950
spellingShingle	Psoralea corylifolia L. Osteoporosis Mass spectrometry Pharmacokinetics Osteoclast Cathepsin K Therapeutics. Pharmacology RM1-950 Ami Lee Hyun Yang Taesoo Kim Hyunil Ha Youn-Hwan Hwang Identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.
description	Osteoporosis and resulting bone fractures are the major health issues associated with morbidity in the aging population; however, there is no effective treatment that does not cause severe side effects. In East Asia, dried seeds of Psoralea corylifolia L. (PC) have traditionally been used as an herbal medicine to manage urinary tract, cutaneous, and gastrointestinal disorders, as well as bone health. However, the mechanism of action and active biocomponents of PC are unclear. Here, we adopted a pharmacokinetic (PK) study aiming to identify the bioavailable phytochemicals in aqueous and ethanolic extracts of PC (APC) and (EPC), respectively. In addition, we aimed to determine anti-resorptive constituents of PC, which accounted for its beneficial effects on bone health. To this end, we used ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). A rapid, sensitive, and reliable UPLC-MS/MS method was developed and determined the 17 PC ingredients. In the PK study, nine components (two chalcones, two coumarins, one coumestan, two flavonoids, and two isoflavonoids) were observed between 36 and 48 h after oral administration of APC or EPC. Among the bioavailable ingredients, four PC constituents (psoralidin, isobavachin, corylifol A, and neobavaisoflavone) inhibited M-CSF-and RANKL-induced osteoclast differentiation in bone marrow-derived macrophages. In addition, two chalcones and two isoflavonoids markedly inhibited cathepsin K activity, and their binding modes to cathepsin K were determined by molecular docking. In summary, our data suggest that bioavailable multicomponents of PC could contribute to the management of bone health.
format	article
author	Ami Lee Hyun Yang Taesoo Kim Hyunil Ha Youn-Hwan Hwang
author_facet	Ami Lee Hyun Yang Taesoo Kim Hyunil Ha Youn-Hwan Hwang
author_sort	Ami Lee
title	Identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.
title_short	Identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.
title_full	Identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.
title_fullStr	Identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.
title_full_unstemmed	Identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.
title_sort	identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of psoralea corylifolia l.
publisher	Elsevier
publishDate	2021
url	https://doaj.org/article/2da3cea5494e46c4bb1fedbcced4b816
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Identification and pharmacokinetics of bioavailable anti-resorptive phytochemicals after oral administration of Psoralea corylifolia L.

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