In Vivo Screening for Anti-Osteoporotic Fraction from Extract of Herbal Formula Xianlinggubao in Ovariectomized Mice

Wang, Xinluan; He, Yang; Guo, Baosheng; Tsang, Man Ching; Tu, Feng‐Juan; Dai, Yi; Yao, Zhihong; Zheng, Lizhen; Xie, Xinhui; Wang, Nan; Yao, Xin‐Sheng; Zhang, Ge; Qin, Ling

doi:10.1371/journal.pone.0118184

Cited by 39 publications

(34 citation statements)

References 45 publications

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“…XLGB capsule is an extensively used remedy in Chinese natural medicine for the treatment of osteoporosis [101]. It has been reported that XLGB shows anti-osteoporosis activity in ovariectomized mice [102,103] and rats with oral dosages at 236 mg/kg/day and 270 mg/kg/day, respectively [47]. Moreover, the dose up to 1800 mg/kg/day showed no serious side effects in ovariectomized rats.…”

Section: Antiosteoporosis Effectmentioning

confidence: 99%

Advances in Chemistry and Bioactivity of Magnoflorine and Magnoflorine-Containing Extracts

Okon

Kukuła-Koch

Jarząb

et al. 2020

IJMS

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The review collects together some recent information on the identity and pharmacological properties of magnoflorine, a quaternary aporphine alkaloid, that is widely distributed within the representatives of several botanical families like Berberidaceae, Magnoliaceae, Papaveraceae, or Menispermaceae. Several findings published in the scientific publications mention its application in the treatment of a wide spectrum of diseases including inflammatory ones, allergies, hypertension, osteoporosis, bacterial, viral and fungal infections, and some civilization diseases like cancer, obesity, diabetes, dementia, or depression. The pharmacokinetics and perspectives on its introduction to therapeutic strategies will also be discussed.

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Section: Antiosteoporosis Effectmentioning

confidence: 99%

Advances in Chemistry and Bioactivity of Magnoflorine and Magnoflorine-Containing Extracts

Okon

Kukuła-Koch

Jarząb

et al. 2020

IJMS

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“…For example, the herbal extract is a component in more than 30 herbal prescriptions for the treatment of osteoporosis where clinical trials have been reported . A recent study using an herbal formulae containing S. miltiorrhiza showed antiresorptive efficacy in OVX mice and rats . Our discovery that some of these compounds are effective ectosteric inhibitors of CatK helps to understand the molecular mechanism of action of the herbal anti‐osteoporotic efficacy.…”

Section: Discussionmentioning

confidence: 93%

An Ectosteric Inhibitor of Cathepsin K Inhibits Bone Resorption in Ovariectomized Mice

Panwar

Xue

Søe

et al. 2017

Journal of Bone and Mineral Research

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The potent cathepsin K (CatK) inhibitor, Tanshinone IIA sulfonic sodium (T06), was tested for its in vitro and in vivo antiresorptive activities. T06 binds in an ectosteric site of CatK remote from its active site and selectively inhibits collagen degradation with an IC value of 2.7 ± 0.2 μM (CatK:T06 molar ratio of 1:5). However, it does not suppress fluorogenic peptide cleavage and gelatinolysis at a 2500-fold molar excess. Contrary to active site-directed CatK inhibitors, such as odanacatib, T06 suppresses bone resorption in both human and mouse osteoclasts equally well (IC value for human and mouse osteoclasts: 237 ± 60 nM and 245 ± 55 nM, respectively) and its antiresorptive activity is fully reversible in both cell types. Moreover, T06 affects neither the metabolic activity of osteoclasts nor osteoclastogenesis. In in vivo studies, 40 mg T06/kg/d given to 12-week-old ovariectomized (OVX) mice for 3 months reduced plasma CTx-1 by 20% and increased osteoblast numbers and plasma P1NP by ∼28% when compared with the OVX control. μCT analysis of T06-treated OVX mice showed a 35% increase in bone mineral density and other femoral trabecular bone parameters when compared with OVX animals. T06 did not alter the number of osteoclasts, had no estrogenic effect on the uterus, did not change plasma estradiol levels, and did not inhibit fibroblast-mediated TGF-ß1 processing or degradation and cognitive functions in OVX mice. This study indicates that the ectosteric inhibitor, T06, is a selective antiresorptive CatK inhibitor that may overcome the shortcomings of side effect-prone active site-directed drugs, which all failed in clinical trials. © 2017 American Society for Bone and Mineral Research.

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“…Postmenopausal osteoporosis originated from the cessation of ovarian hormones at menopause which prolongs bone loss. Phytoestrogen and essential amino acids are proven to modulate the growth and the differentiation of osteoblasts and possessing anti-osteoporotic effects (33,34). Therefore, the main goal of this study is to find natural treatment gathered these two properties.…”

Section: Discussionmentioning

confidence: 99%

In silico estrogen-like activity and in vivo osteoclastogenesis inhibitory effect of Cicer arietinum extract

Sayed

Elfiky

2018

Cell Mol Biol (Noisy-le-grand)

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Postmenopausal osteoporosis is a common disorder accompanied with estrogen deficiency in women. Plants containing phytoestrogens and amino acids have been used in the osteoporosis treatment. The present study aims to evaluate the estrogen-like activity of the Cicer arietinum extract (CAE) and its ability to inhibit osteoclastogenesis process. These achieved by investigating the binding of its active phytoestrogens (genistein, daidzein, formononetin and biochanin A) to the estrogen receptors (ER) α and β of rats and human in silico. In addition, in vivo study on ovariectomized (OVX) rats is performed. For in vivo study, twenty four rats were divided into four groups (n= 6). Group I is the sham control rats which administered distilled water. Groups II, III, and IV are OVX groups which administered distilled water, CAE (500 mg/kg), and alendronate; respectively. The docking study revealed that the phytoestrogens docked into the protein active site with binding energies comparable with that of estrogens (estriol and β-estradiol) which means the similarity between the estrogenic contents of CAE and the ensogenous ones. Additionally, in vivo study revealed that CAE reverse TRAP5b and RANKL levels that drastically increased in the untreated OVX group. But, it trigger upregulation of OPG, enhance the OPG/RANKL ratio and modulate the bone and uterus alterations of OVX group. Phytoestrogens and the bone-protective amino acids contents of CAE could be responsible for their estrogen-like effect and antiosteoporotic activity. These results concluded that CAE is an attractive candidate for developing a potential therapeutic cheap agent used as an alternative to the synthetic estrogen replacement therapy. Further, in vivo validation is required for its clinical application.

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In Vivo Screening for Anti-Osteoporotic Fraction from Extract of Herbal Formula Xianlinggubao in Ovariectomized Mice

Cited by 39 publications

References 45 publications

Advances in Chemistry and Bioactivity of Magnoflorine and Magnoflorine-Containing Extracts

Advances in Chemistry and Bioactivity of Magnoflorine and Magnoflorine-Containing Extracts

An Ectosteric Inhibitor of Cathepsin K Inhibits Bone Resorption in Ovariectomized Mice

In silico estrogen-like activity and in vivo osteoclastogenesis inhibitory effect of Cicer arietinum extract

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