Comparative Effects of Hispidulin, Genistein, and Icariin with Estrogen on Bone Tissue in Ovariectomized Rats

Yang, Lijuan; Yu, Zhen; Qu, Haili; Li, Minmin

doi:10.1007/s12013-014-9945-0

Cited by 25 publications

(13 citation statements)

References 22 publications

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“…Icariin has been identified as an inhibitor of cathepsin K and may suppress cartilage and bone degradation in mice with collagen-induced arthritis ( 13 ). In vivo , icariin has demonstrated significant anti-osteoporosis effects in ovariectomized rats and mice, glucocorticoid-induced rats and OPG knockout mice ( 7 , 8 ). However, in vitro studies have indicated that icariin may reduce TRAP activity and increase osteogenic differentiation, calcium deposition and mineralized nodule formation in induced bone marrow stromal and RAW264.7 cells ( 32 , 33 ).…”

Section: Discussionmentioning

confidence: 99%

“…Icariin has been identified as a flavonoid isolated from Herba Epimedii ( Epimedium brevicornum ), which is the most commonly used Chinese herbal medicine in the treatment of sexual dysfunction and osteoporosis ( 5 , 6 ). The anti-osteoporotic role of icariin has been verified in ovariectomized rats ( 7 , 8 ) and glucocorticoid-induced osteoporotic rats ( 9 ). A 24-month randomized double-blind placebo-controlled clinical trial indicated that an Epimedium -derived phytoestrogen flavonoid preparation containing 60 mg icariin, 15 mg daidzien and 3 mg genistein was able to limit bone loss in late postmenopausal women ( 10 ).…”

Section: Introductionmentioning

confidence: 97%

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Icariin ameliorates dexamethasone‑induced bone deterioration in an experimental mouse model via activation of microRNA‑186 inhibition of cathepsin K

Yang

Huang

2017

Mol Med Report

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The present study aimed to investigate bone deterioration in glucocorticoid-induced osteoporosis (GIOP) mice, and the anti-osteoporosis effect and underlying molecular mechanism of icariin. Dexamethasone (DSM) treatment was demonstrated to facilitate the induction of hypercalciuria in GIOP mice. Icariin treatment reversed the dexamethasone (DXM)-induced disequilibrium of calcium homeostasis and bone resorption, and increased serum alkaline phosphatase, tartrate resistant acid phosphatase, osteocalcin and deoxypyridinoline. Haematoxylin and eosin staining revealed an increase in disconnections and separation in the trabecular bone network of the tibial proximal metaphysis, in the GIOP group. Icariin treatment reversed the DXM-induced trabecular deleterious effects, and stimulated bone remodeling in GIOP mice. Furthermore, the results demonstrated that the mRNA and protein expression of cathepsin K were significantly increased in GIOP mice, compared with the control group. Icariin treatment may suppress the expression of cathepsin K in the tibia of GIOP mice. The levels of microRNA (miR)-186 were markedly reduced in the tibia of GIOP mice compared with control group; however, this was inhibited by icariin treatment. Bioinformatics analysis demonstrated that miR-186 regulates cathepsin K via binding to the upstream 3′-untranslated region. Furthermore, transfection with miR-186 mimics resulted in inhibition of cathepsin K expression, whereas miR-186 inhibitors facilitated cathepsin K expression in osteoclasts. In conclusion, the present study demonstrated the protective effects of icariin against bone deteriorations in the experimental GIOP mice, and the underlying mechanism was mediated, at least partially, via activation of miR-186-mediated suppression of cathepsin K. These results provide evidence to support the use of icariin as a therapeutic approach in the management of glucocorticoid-induced bone loss, and the disequilibrium of calcium homeostasis.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 97%

Icariin ameliorates dexamethasone‑induced bone deterioration in an experimental mouse model via activation of microRNA‑186 inhibition of cathepsin K

Yang

Huang

2017

Mol Med Report

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“…Hispidulin have been proven to have estrogen-like and antiosteoporotic activity and can be potentially used for the treatment of osteoporosis 23 . Effect of hispidulin on ovariectomy (OVX)-induced bone loss in mice was investigated.…”

Section: Pharmacological Activitiesmentioning

confidence: 99%

Medicinal importance, pharmacological activities, and analytical aspects of hispidulin: A concise report

Patel

2017

Journal of Traditional and Complementary Medicine

134

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Herbal medicines have been played an important role in the human civilization since very ancient time as a food, cloth, medicine and other aspects. Some of the important drugs in the modern medicine were derived from the natural sources such as aspirin, digitalis, quinine, vincristine, vinblastine etc. Hispidulin (4′, 5, 7-trihydroxy-6-methoxyflavone) is a flavones derivative found in plant such as Grindelia argentina, Arrabidaea chica, Saussurea involucrate, Crossostephium chinense, Artemisia and Salvia species. Hispidulin have antioxidant, antifungal, anti-inflammatory, antimutagenic, and antineoplastic properties. So far, various analytical methods have been investigated and developed for detection of hispidulin in the plant materials. Productions of hispidulin through different tissue culture techniques have been also investigated. Present review summarized medicinal uses, pharmacological activities and analytical aspects of hispidulin. From the above mentioned aspects, we can conclude that, this review will be helpful to the researcher in the field of natural product for the development of novel molecule for the treatment of different disorders.

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“…Wei et al found that icariin could promote bone formation, increase trabecular numbers, and reduce trabecular separation [23]. The comparing study showed that there was no obvious difference between icariin and estrogen on anti-osteoporotic activity in OVX rats [24]. The main bioactive components of this herb are prenylated flavonol glycosides, and the absorption of flavonol glycosides increased, while the number of glucosides decreased [25,26].…”

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confidence: 99%

Beneficial Effects of a Flavonoid Fraction of Herba Epimedii on Bone Metabolism in Ovariectomized Rats

et al. 2016

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A flavonoid fraction of Herba Epimedii, including eight flavonoid glycoside compounds, epimedoside A, ikarisoside F, baohuoside II, sagittatoside A, sagittatoside B, 7-O-rhamnosyl icariside II, 2"-O-rhamnosyl icariside II, and baohuoside I, was isolated and prepared from the leaves of Herba Epimedii. This study was conducted to assess the potential effect of the flavonoid fraction of Herba Epimedii on osteoporosis in ovariectomized rats. Rats received repeated administration of a vehicle (ovariectomized), the flavonoid fraction of Herba Epimedii (7.5, 15, 30 mg/kg/d), and ipriflavone (200 mg/kg/d) once a day for 8 weeks, beginning 4 weeks after ovariectomization. Then, the bone turnover markers, bone biomechanical properties, trabecular architecture, and related protein expressions were evaluated by biochemical assay kits, mechanical testing, microcomputed tomography, immunohistochemical evaluation, and Western blot analysis. Treatment with the flavonoid fraction of Herba Epimedii (15, 30 mg/kg/d) and ipriflavone (200 mg/kg/d) significantly increased bone strength while dramatically inhibiting the serum alkaline phosphatase and tartrate-resistant acid phosphatase levels in ovariectomized rats. Furthermore, the flavonoid fraction of Herba Epimedii also increased osteoprotegerin protein expression and reduced the receptor activator of nuclear factor-κB ligand protein expression compared with ovariectomized rats. In addition, the microcomputed tomography results showed that the flavonoid fraction of Herba Epimedii treatment significantly improved trabecular bone mineral density and restored the bone microarchitecture in ovariectomized rats. Therefore, our results indicated that the flavonoid fraction of Herba Epimedii might be beneficial for improving postmenopausal osteoporosis and should be considered as a promising candidate for treating postmenopausal osteoporosis.

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Comparative Effects of Hispidulin, Genistein, and Icariin with Estrogen on Bone Tissue in Ovariectomized Rats

Cited by 25 publications

References 22 publications

Icariin ameliorates dexamethasone‑induced bone deterioration in an experimental mouse model via activation of microRNA‑186 inhibition of cathepsin K

Icariin ameliorates dexamethasone‑induced bone deterioration in an experimental mouse model via activation of microRNA‑186 inhibition of cathepsin K

Medicinal importance, pharmacological activities, and analytical aspects of hispidulin: A concise report

Beneficial Effects of a Flavonoid Fraction of Herba Epimedii on Bone Metabolism in Ovariectomized Rats

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