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X-N Ma, C-X Ma, W-G Shi, J Zhou, H-P Ma, Y-H Gao, C J Xian, K-M Chen
OBJECTIVE: Icaritin, one effective metabolite of Herba Epimedii-derived flavonoid icariin, has a strong osteogenic activity. However, its action mechanism remains unclear. Since primary cilia have been shown to play a pivotal role in regulating the osteogenesis, we hypothesized primary cilia are indispensable in mediating icaritin osteogenic effect. MATERIALS AND METHODS: Primary rat calvarial osteoblasts were transfected with siRNA1 targeting intraflagellar transport protein 88 (IFT88), a protein required for ciliogenesis, to prevent formation of primary cilium and were treated with 10(-6) M icaritin...
October 21, 2016: Journal of Endocrinological Investigation
QiuShi Wei, Jin Zhang, GuoJu Hong, ZhenQiu Chen, WeiMin Deng, Wei He, Mei Hui Chen
Icariin, the main effective component of Herba Epimedii, has been identified to regulate the osteogenic differentiation of rat bone marrow stromal cells (rBMSCs) and have potential application in preventing bone loss and promoting bone regeneration. However, the underlying signaling pathway of its osteogenic effect remains unclear. Here, we investigated whether icariin could promote osteogenesis of rBMSCs through modulating the estrogen receptor alpha (ERα) and Wnt/β-catenin signaling pathways, which implicated in rBMSCs osteogenesis...
October 17, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Tianlin Liu, Xin Zhang, Yuan Luo, Yuanliang Huang, Gang Wu
Bone tissue engineering technique is a promising strategy to repair large-volume bone defects. In this study, we developed a 3-dimensional construct by combining icariin (a small-molecule Chinese medicine), allogeneic bone marrow-derived mesenchymal stem cells (BMSCs), and a siliceous mesostructured cellular foams-poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) (SMC-PHBHHx) composite scaffold. We hypothesized that the slowly released icariin could significantly promote the efficacy of SMC-PHBHHx/allogeneic BMSCs for repairing critical-size bone defects in rats...
2016: Stem Cells International
Qiang-Song Wang, Gui-Fang Wang, Jie Zhou, Li-Na Gao, Yuan-Lu Cui
In recent years, oral colon specific drug delivery system has been paid more attention in the treatment of inflammatory bowel disease (IBD). As the special pH condition in gastrointestinal tract, the challenge for treatment of IBD was that the colon drug delivery system should endure the low pH in stomach and release drugs quickly in high pH in colon. Icariin with the poor solubility and low bioavailability limited the treatment of many diseases in clinic. In this study, the protective mechanism of alginate-chitosan microspheres loaded with icariin were investigated with trinitrobenzene sulfonic acid (TNBS)/ethanol induced colonic mucosal injury in rats...
October 3, 2016: International Journal of Pharmaceutics
Yunk-Yung Han, Mi-Young Song, Min-Sub Hwang, Ji-Hye Hwang, Yong-Ki Park, Hyo-Won Jung
Obesity is associated with a number of metabolic abnormalities such as type 2 diabetes and has become a major health problem worldwide. In the present study, we investigated the effects of Epimedium koreanum Nakai (Herba Epimedii, HE) and its main constituent icariin on the adipocyte differentiation in 3T3-L1 preadipocytes. HE extract and icariin significantly reduced lipid accumulation and suppressed the expressions of PPARγ, C/EBPα, and SREBP-1c in 3T3-L1 adipocytes. They also inhibited fatty acid synthase (FAS), acyl-Co A synthase (ACS1), and perilipin...
September 2016: Chinese Journal of Natural Medicines
Chun-Yan Shen, Jian-Guo Jiang, Li Yang, Da-Wei Wang, Wei Zhu
Aging, a puzzling question in the medical field, is a multifactorial process that results in a progressive functional decline at cellular, tissue, and organismal levels. Although it is impossible to prevent aging, slowing down the pace of aging is entirely possible to achieve. Traditional Chinese medicine (TCM) is characterized by the nourishing of life, its role in anti-aging is getting more and more attention. This article summarizes the natural products from TCM that are reported to have anti-aging effects in the past two decades...
September 23, 2016: British Journal of Pharmacology
Meixia Chen, Jinfeng Wu, Qingli Luo, Shuming Mo, Yubao Lyu, Ying Wei, Jingcheng Dong
Cancer is one of the leading causes of deaths worldwide. Compounds derived from traditional Chinese medicines have been an important source of anticancer drugs and adjuvant agents to potentiate the efficacy of chemotherapeutic drugs and improve the side effects of chemotherapy. Herba Epimedii is one of most popular herbs used in China traditionally for the treatment of multiple diseases, including osteoporosis, sexual dysfunction, hypertension and common inflammatory diseases. Studies show Herba Epimedii also possesses anticancer activity...
2016: Nutrients
Jin-Hai Xu, Min Yao, Jie Ye, Guo-Dong Wang, Jing Wang, Xue-Jun Cui, Wen Mo
OBJECTIVE: Ovariectomy (OVX)-induced rats are the most frequently used animal model to research postmenopausal osteoporosis. Our objective was to summarize and critically assess the bone mass improved effect of icariin (ICA) for treatment of postmenopausal osteoporosis in an OVX-induced rat model. METHODS: The PUBMED, EMBASE, and Chinese databases were searched from their inception date to February 2015. Two reviewers independently selected animal studies that evaluated the bone mass improved effect of ICA compared with control in OVX-induced rats...
October 2016: Menopause: the Journal of the North American Menopause Society
Tao Cheng, Tingting Sheng, Yaxiong Yi, Tong Zhang, Han Han
Icariin (ICA), the major constituent of Epimedium brevicornu Maxim, is recognized as an effective agent for the treatment of osteoporosis. In our previous report, the relatively short half-life (74min) and poor bioavailability (approximately 0.1%) of ICA in rats suggested that not only ICA itself but also its metabolites could be responsible for the observed osteoporosis treatment effect. Therefore, the present study aimed at identifying the metabolites of ICA in rat plasma, bile, urine, and feces after the administration of a single oral dose of ICA (150mg/kg)...
October 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Zhen-Tao Mo, Wen-Na Li, Yu-Rong Zhai, Qi-Hai Gong
Icariin (ICA), an active component of Epimedium brevicornum Maxim, exerts a variety of neuroprotective effects such as antiapoptosis. However, the mechanisms underlying antiapoptosis of ICA in neurons exposed to oxygen-glucose deprivation and reperfusion (OGD/R) are unclear. The B-cell lymphoma-2 (Bcl-2) protein family plays an important role in the regulation of apoptosis and autophagy through Bcl-2-dependent cross talk. Bcl-2 suppresses apoptosis by binding to Bax and inhibits autophagy by binding to Beclin-1 which is an autophagy related protein...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
Shunjun Xu, Jiejing Yu, Liu Yang, Yaling Zhu, Shuai Sun, Zhengdi Xu
Chuan-Ke-Zhi (CKZ), a purified Herba Epimedii extract, is a potent Chinese medicine preparation whose main bioactive components are a class of flavonoid glycosides such as epimedins A, B, and C and icariin. And epimedin C is far more abundant than other flavones in this extract. This study aims to investigate the pharmacokinetic and bioavailability of epimedin C and what effects, if any, other ingredients in CKZ have on its pharmacokinetics. Epimedin C, CKZ, and a combination of epimedins A, B, and C and icariin were, respectively, administrated to rats, and then the pharmacokinetic parameters of epimedin C in the three groups were calculated and compared...
2016: Journal of Analytical Methods in Chemistry
Hailong Wu, Mihyang Kim, Jaehong Han
Icariin is a major bioactive compound of Epimedii Herba, a traditional oriental medicine exhibiting anti-cancer, anti-inflammatory and anti-osteoporosis activities. Recently, the estrogenic activities of icariin drew significant attention, but the published scientific data seemed not to be so consistent. To provide fundamental information for the study of the icaritin metabolism, the biotransformation of icariin by the human intestinal bacteria is reported for the first time. Together with human intestinal microflora, the three bacteria Streptococcus sp...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Yue Yang, Xuesong Liu, Weili Li, Ye Jin, Yongjiang Wu, Jiyu Zheng, Wentao Zhang, Yong Chen
In this work, near infrared (NIR) spectroscopy was used in combination with chemometrics to determine the epimedin A, epimedin B, epimedin C, icariin, and moisture contents of Herba Epimedii. The variable selection method genetic algorithm (GA) and regression tool support vector machine (SVM) were used to improve the model performance. Four different calibration models, namely Full-PLS, GA-PLS, Full-SVM, and GA-SVM, were established, and their performances in terms of prediction accuracy and model robustness were systemically studied and compared...
January 15, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Yao-Hong Song, Hui Cai, Zhi-Ming Zhao, Wen-Jing Chang, Ning Gu, Shou-Pei Cao, Meng-Ling Wu
Our previous study showed that Icariin (ICA) has anti-cardiac hypertrophy effect in rats with an unknown mechanism. In the present study, we aimed to clarify the cardiac protective effect and mechanism of ICA in vitro. H9C2 cardiac myocytes were incubated with H2O2 to build up the oxidative stress injury model. The results showed that pre-treatment of ICA protected cells against the toxicity induced by H2O2. H2O2 treatment significantly reduced H2O2-induced apoptosis, evidenced by lower Annexin V/PI stained cells and less PARP and caspase-3/9 activation...
August 20, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
X Huang, T Xiang, S Xu, S Lu, H Liu, W C Zhang, P H Xiang, P F Xu
OBJECTIVE: To observe the effects of icariin on S-nitrosogultathione(GSNO) induced endothelial cell apoptosis, and to explore the relative mechanisms. METHODS: EA.hy926 cell line was provided by Zhejiang University and cells were divided into blank control group, GSNO group (1 mmol/L GSNO), icariin (ICA) intervention group (GSNO+ different concentrations (high, medium and low: 10, 1 and 0.1 μmol/L ICA) and 1 μmol/L LY294002 pretreatment groups (AKT protease pathway inhibitor on top of ICA groups) by cluster random sample method...
August 24, 2016: Zhonghua Xin Xue Guan Bing za Zhi
Jian Liu, Danqing Li, Xuying Sun, Yuting Wang, Qiangbing Xiao, Anmin Chen
Bacteria-induced inflammatory responses cause excessive bone resorption in chronic inflammatory diseases such as septic arthritis, osteomyelitis, and orthopedic implant failure. Icariine has been reported to facilitate the bone healing and reduce the occurrence of osteoporosis in clinical, moreover, laboratory studies which have proved that Icariine promotes the proliferation and differentiation of osteoblasts in vitro. The present study aimed to evaluate the effects of Icariine on lipopolysaccharide (LPS)-induced bone loss via an osteogenic-in vitro model and to elucidate the underlying molecular mechanisms...
October 2016: Inflammation
Shuping Fu, Li Yang, Hao Hong, Ronghua Zhang
OBJECTIVE: To investigate the effect of icariin on proliferation of bone marrow mesenchymal stem cells (BMSCs) in Sprague-Dawley (SD) rats. METHODS: BMSCs were obtained from SD rat bone marrow with differential time adherent method. Its characteristic was identified through differentiation cell surface antigens and the multi-lineage (osteo/adipo/chondo) differentiation potential. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and 5-Bromo-2-Deoxyuridine (BrdU) incorporation were applied to detect the effect of icariin on BMSCs proliferation...
June 2016: Journal of Traditional Chinese Medicine, Chung i Tsa Chih Ying Wen Pan
Hui-Li Tan, Kok-Gan Chan, Priyia Pusparajah, Surasak Saokaew, Acharaporn Duangjai, Learn-Han Lee, Bey-Hing Goh
Epimedium (family Berberidaceae), commonly known as Horny Goat Weed or Yin Yang Huo, is commonly used as a tonic, aphrodisiac, anti-rheumatic and anti-cancer agent in traditional herbal formulations in Asian countries such as China, Japan, and Korea. The major bioactive compounds present within this plant include icariin, icaritin and icariside II. Although it is best known for its aphrodisiac properties, scientific and pharmacological studies suggest it possesses broad therapeutic capabilities, especially for enhancing reproductive function and osteoprotective, neuroprotective, cardioprotective, anti-inflammatory and immunoprotective effects...
2016: Frontiers in Pharmacology
Liming Xue, Yiping Jiang, Ting Han, Naidan Zhang, Luping Qin, Hailiang Xin, Qiaoyan Zhang
ETHNOPHARMACOLOGICAL RELEVANCE: Icariin, a principal flavonoid glycoside of Epimedium brevicornu Maxim, has been widely proved to possess antiosteoporotic activity with promoting bone frormation and decreasing bone resorption. However, the involving mechanisms remain unclear. AIM OF THE STUDY: To clear a global insight of signal pathways involved in anti-osteoporotic mechanism of icariin at proteins and metabolites level by integrating the proteomics and NMR metabonomics, in a systems biology approach...
July 12, 2016: Journal of Ethnopharmacology
Kunyu Shen, David W Johnson, Glenda C Gobe
Cyclic nucleotide signal transduction pathways are an emerging research field in kidney disease. Activated cell surface receptors transduce their signals via intracellular second messengers such as cyclic AMP and cyclic GMP (cGMP). There is increasing evidence that regulation of the cGMP-cGMP-dependent protein kinase1-phosphodiesterase (cGMP-cGK1-PDE) signaling pathway may be renoprotective. Selective PDE5 inhibitors have shown potential in treating kidney fibrosis in patients with chronic kidney disease, via their downstream signaling, and these inhibitors also have known activity as anti-thrombotic and anti-cancer agents...
July 13, 2016: American Journal of Physiology. Renal Physiology
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