Xue-Qin Ma1, Ting Han2, Xia Zhang3, Jin-Zhong Wu4, Khalid Rahman5, Lu-Ping Qin6, Cheng-Jian Zheng7. 1. Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, China; Department of Pharmaceutical analysis, School of Pharmacy, NingXia Medical University, Yinchuan 750004, China. 2. Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. 3. Department of Pharmaceutical analysis, School of Pharmacy, NingXia Medical University, Yinchuan 750004, China. 4. Academy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, 1 Huatuo Road, Fuzhou 350108, China. 5. Faculty of Science, School of Biomolecular Sciences, Liverpool John Moores University, Byrom Street, Liverpool L3 3AF, England, UK. 6. Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, China; Shanghai Key Laboratory for Pharmaceutical Metabolite Research, Shanghai 200433 China. Electronic address: qinsmmu@126.com. 7. Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: zhengchengjian@smmu.edu.cn.
Abstract
BACKGROUND: Podocarpium podocarpum (DC.), an edible and medicinal plant popularly used for the treatment of bruises and fracture in Chinese folk medicine, has been proved to possess significant antiosteoporotic effect in our latest research. PURPOSE: Our study aimed to investigate the in vitro and in vivo antiosteoporotic effect of kaempfertrin (KN), a principal flavonoid in P. podocarpum obtained through bio-guided isolation. METHODS: An ovariectomized (OVX) rat model of osteoporosis as well as in vitro osteoblast and osteoclast cell lines were employed to evaluate the antiosteoporotic potency of KN. RESULTS: KN significantly improved the bone mass and microarchitecture in OVX rats, with little estrogen-like side effect compared with estradiol valerate. KN also exhibited stimulatory effect on osteoblastic cells and inhibitory action on osteoclastic cells, which down-regulated the phosphorylation level of I-κB. CONCLUSION: KN possessed significant antiosteoporotic activity. Combined with its limited estrogen-like side effect, KN can be regarded as an idealistic antiosteoporotic candidate for human osteoporosis diseases.
BACKGROUND: Podocarpium podocarpum (DC.), an edible and medicinal plant popularly used for the treatment of bruises and fracture in Chinese folk medicine, has been proved to possess significant antiosteoporotic effect in our latest research. PURPOSE: Our study aimed to investigate the in vitro and in vivo antiosteoporotic effect of kaempfertrin (KN), a principal flavonoid in P. podocarpum obtained through bio-guided isolation. METHODS: An ovariectomized (OVX) rat model of osteoporosis as well as in vitro osteoblast and osteoclast cell lines were employed to evaluate the antiosteoporotic potency of KN. RESULTS: KN significantly improved the bone mass and microarchitecture in OVX rats, with little estrogen-like side effect compared with estradiol valerate. KN also exhibited stimulatory effect on osteoblastic cells and inhibitory action on osteoclastic cells, which down-regulated the phosphorylation level of I-κB. CONCLUSION: KN possessed significant antiosteoporotic activity. Combined with its limited estrogen-like side effect, KN can be regarded as an idealistic antiosteoporotic candidate for humanosteoporosis diseases.
Authors: Maria-Luisa Pérez-Lozano; Annabelle Cesaro; Marija Mazor; Eric Esteve; Sabine Berteina-Raboin; Thomas M Best; Eric Lespessailles; Hechmi Toumi Journal: Antioxidants (Basel) Date: 2021-02-09