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Fu-Cai Ren, Xian-Jun Jiang, Shi-Zhen Wen, Li-Xia Wang, Xiang-Mei Li, Fei Wang
Six hitherto unknown prenylated 2-phenoxychromones, epimedonin G (1), 7-O-methylepimedonin G (2), and epimedonins H-K (3-6), and two new prenylflavonoids, epimedonin L (7) and 3″-O-desmethylspinorhamnoside (8), were isolated from an ethanol extract of the aerial parts of Epimedium brevicornum. Their structures were established on the basis of spectroscopic data interpretation. Compound 7 exhibited cytotoxic activity when evaluated against four human cancer cell lines (HL-60, A-549, MCF-7, and SW-480), with IC50 values of <10 μM...
January 17, 2018: Journal of Natural Products
Zifei Qin, Shishi Li, Zhihong Yao, Xiaodan Hong, Baojian Wu, Kristopher W Krausz, Frank J Gonzalez, Hao Gao, Xinsheng Yao
Active efflux transport of glucuronides out of cells is a critical process in elimination of drugs and food-derived compounds. Wushanicaritin, a natural polyphenol from Epimedium species, has shown many biological activities. However, the transporters responsible for excretion of wushanicaritin glucuronides still remain undefined. Herein, chemical inhibitors (Ko143, MK571, dipyridamole and leukotriene C4) and single stable knocked-down efflux transporters (BCRP, MRP1, MRP3 and MRP4) were used to determine the contributions of efflux transporters to glucuronide efflux and cellular glucuronidation in UGT1A1-overexpressing HeLa cells (HeLa1A1)...
January 10, 2018: Food & Function
Xianjun Sun, Xiaohong Deng, Waijiao Cai, Wenwei Li, Ziyin Shen, Tinghui Jiang, Jianhua Huang
AIMS: Icariin (ICA) is a flavonoid isolated from certain plant species in the genus Epimedium, especially Epimedium brevicornum. Previous studies indicated that ICA has certain regulatory effects on some inflammatory diseases, and that ICA regulates the activity of glucocorticoid receptor (GR) and NF-κB. But the causal link between GR and NF-κB and other downstream pathways in effects of ICA remained elusive, therefore here we have investigated whether ICA could promote GR function, in turn, to regulate NF-κB and/or other factors to achieve its anti-inflammatory effect...
January 6, 2018: Life Sciences
Lu Yang, Chaosheng Peng, Jing Xia, Wenluo Zhang, Li Tian, Yuhong Tian, Xiaobin Yang, Yuean Cao
Icariside II is a flavonoid extracted from Epimedium that has antioxidant, anti‑inflammatory and antiapoptotic effects. The aim of the present study was to evaluate the effects icariside II on diabetic cardiomyopathy in streptozotocin-induced diabetic rats. Icariside II treatment improved body weight, heart/body weight ratio and fasting blood glucose in diabetic model rats. Icariside II was demonstrated to reduce the expression levels of creatine kinase and lactate dehydrogenase in serum, and to lower cardiac oxidative stress, inflammation and apoptosis levels in diabetic rats...
December 22, 2017: Molecular Medicine Reports
Xiangyu Deng, Wei Wu, Hang Liang, Donghua Huang, Doudou Jing, Dong Zheng, Zengwu Shao
Purpose: To explore the effect and possible mechanism of icariin, a prenylated flavonol glycoside derived from the Chinese herb Epimedium sagittatum that was applied to IL-1β pretreated human nucleus pulposus (NP) cells. Methods: Human NP cells were isolated from intervertebral discs of patients with scoliosis and lumbar spondylolisthesis. The cells were divided into five groups: A (blank control); B (20 ng/ml IL-1β); C (20 ng/ml IL-1β + 20 μM icariin); D (20 μM icariin + 20 ng/ml IL-1β + 25 μM LY294002); E (20 ng/ml IL-1β + 25 μM LY294002)...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
Dan Wang, Wenjuan Xu, Xiaoyu Chen, Jichun Han, Lina Yu, Caixia Gao, Wenjin Hao, Xiaona Liu, Qiusheng Zheng, Defang Li
Icariin (ICA) is a major component isolated from Epimedium brevicornum. Emerging evidence shows that ICA can inhibit tumor cell proliferation, invasion and migration. However, the anti-cancer effect of ICA on B16 cells has not been fully investigated. Here we found that the proliferation of B16 cells was inhibited by ICA in a concentration- and time-dependent manner, and the colony formation of B16 cells was also inhibited by ICA in a concentration-dependent manner. Further study showed that the melanin content was increased and the tyrosinase (Tyr) activity was enhanced after ICA treatment in B16 cells...
November 21, 2017: Oncotarget
Yuqing Zeng, Dingyan Bi, Zhan Yi, Jianwei Lu, Fuhua Zhong, Binfeng Jiang
OBJECTIVE: To explore the clinical efficacy and partial mechanism of medicinal-cake-separated moxibustion for senile osteoporosis. METHODS: Sixty cases of senile osteoporosis were randomly divided into an observation group and a control group according to the random digits table, 30 cases in each one. The two groups were both treated with basic treatment of western medicine. The acupoints included four groups:① Dazhui (GV 14), Dazhu (BL 11) and Ganshu (BL 18); ② Zhongwan (CV 12), Danzhong (CV 17) and Zusanli (ST 36); ③ Pishu (BL 20), Shenshu (BL 23) and Mingmen (GV 4); ④ Shenque (CV 8) and Guanyuan (CV 4)...
May 12, 2017: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
Xinguang Sun, Qi Li, Jie Zhang, Wei Zheng, Qianzhi Ding, Jie Yang, Bei Wang, Jie Wang, Baolin Guo, Baiping Ma
Icariin (ICA), a major flavonoid responsible for the pharmacological actions of Herba Epimedii, was found to be increased significantly after the heating process. The increase of ICA was considered to be due to the transformation of other flavonoids, in particular, epimedin (EPI) A-C. This novel study demonstrated that the increase of ICA in Epimedium. koreanum was induced mainly through the conversion of 3'''-carbonyl-2''-β-l-quinovosyl icariin (CQICA) by deglycosylation during the heating process. Furthermore, the comparative analysis of the changes of CQICA and ICA in four raw Epimedium species (EPs) designated in the Chinese Pharmacopoeia revealed that the increase of ICA during the heating process was associated with the presence of CQICA in EPs...
November 22, 2017: Journal of Pharmaceutical and Biomedical Analysis
Yuting Wu, Zhiqiang Qian, Shu Fu, Yun Yue, Yeli Li, Ruimin Sun, Bo Huang, Danli Yang
Inhibition or removal of excess reactive oxygen species can effectively protect cellular function or reduce cell death because oxidative stress is the main cause of cellular damage in many diseases. The flavonoid compound IcarisideII having a slight inhibitory effect on PDE5, is the main active components of epimedium in vivo and has a wide range of pharmacological effects on oxidation and apoptosis. However, whether IcarisideII has the same protective effect on ventricular remodeling in spontaneously hypertensive rats (SHR) is unknown...
November 21, 2017: European Journal of Pharmacology
Xu Pang, Shuang-Shuang Yin, Hai-Yang Yu, Yi Zhang, Tao Wang, Li-Min Hu, Li-Feng Han
Phytochemical study on the leaves of Epimedium brevicornu finally led to the isolation of four prenylated flavonoids (1-4) and three dihydrophenanthrenes (5-7), of which 1, 2, 5 and 7 were new compounds. The structures of these compounds were established mainly by spectroscopic techniques, including NMR spectroscopy and mass spectrometry. These isolates exhibited the cytotoxic activities against HepG2 cells with the IC50 values of 32.8-87.3 μM.
November 26, 2017: Natural Product Research
Xiang Liu, Chang-Zhen Fu, Min Gao, Han-Cheng Zhi, Xiang-Bo Yang, Bao-Lin Guo
In this study, 128 individuals form 14 Epimedium pubescens populations and 1 E. stellulatum population were analyzed by ISSR marker. The data were calculated by POPGENE software and clustered by UPGMA method. Optical microscope was used to observe the main types of the non-glandular hairs and their characteristics in each population. It is found that the following conclusions: Non-glandular hairs can be divided into five morphological categories, long straight pubescent, curly pubescent, appressed curly pubescent, pseudo short appressed hairs and long appressed...
August 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Xiang Dong Su, Wei Li, Jin Yeul Ma, Young Ho Kim
In this study, 21 compounds were isolated from the aerial parts of Epimedium koreanum Nakai, including 6 phenols (1-5 and 10), 4 lignans (6-9) and 11 flavonoids (11-21). The chemical structures of those isolates were established after extensive one-and two-dimensional nuclear magnetic resonance and mass spectroscopy analyses. This is the first report of compounds 2, 3, 4 and 9 in E. koreanum and of compounds 5 and 7 in the family Berberidaceae. The chemotaxonomic significance of the isolated compounds is discussed...
November 21, 2017: Natural Product Research
Jing Lin, Jun Zhu, Yan Wang, Na Zhang, Hans-Jürgen Gober, Xuemin Qiu, Dajin Li, Ling Wang
Postmenopausal osteoporosis is a systemic metabolic skeletal disease generally ascribable to a dearth of estrogen. Whether traditional Chinese medicine is effective in management of postmenopausal osteoporosis remains unclear. This article reviews the experimental evidence of both in vitro and in vivo preclinical studies with the theme of the application of Chinese single herbs and active ingredients in postmenopausal osteoporosis. It includes three single herbs (Herba Epimedium, Rhizoma Drynariae, and Salvia miltiorrhiza) and eight active ingredients (saikosaponins, linarin, echinacoside, sweroside, psoralen, poncirin, vanillic acid, and osthole)...
2017: Bioscience Trends
Wonil Lee, Jin Han Nam, Hyun-Ji Cho, Ju-Young Lee, Won-Kyung Cho, Υeongyeon Kim, Young-Man We, Jin Yeul Ma, Hyang-Sook Hoe
Previously, we showed that the herbal extract EYK (Epimedium koreanum Nakai) can regulate the immune response. Other studies showed that EYK has beneficial effects in human lung cancer, angiogenesis and Alzheimer's disease (AD). However, it remains unknown whether EYK can affect cancer cell migration and invasion in human brain cancer cell lines. In the present study, we found that pre- or post-treatment with EYK inhibited phorbol 12-myristate 13-acetate (PMA)-induced cancer cell migration and invasion in A172 cells, but not in U373MG or T98G cells...
December 2017: Oncology Reports
Z Wang, D Wang, D Yang, W Zhen, J Zhang, S Peng
Osteoporosis is a bone disease characterized by reduced bone mass, which leads to increased risk of bone fractures, and poses a significant risk to public health, especially in the elderly population. The traditional Chinese medicinal herb Epimedii has been utilized for centuries to treat bone fracture and bone loss. Icariin is a prenylated flavonol glycoside isolated from Epimedium herb, and has been shown to be the main bioactive component. This review provides a comprehensive survey of previous studies on icariin, including its structure and function, effect on bone metabolism, and potential for clinical application...
November 6, 2017: Osteoporosis International
Jianmei Gao, Yingshu Xu, Ming Lei, Jingshan Shi, Qihai Gong
Icariside II (ICS II), a phosphodiesterase 5 inhibitor (PDE 5-I), is a major ingredient of Epimedium brevicornum, with wide spectrum of neuroprotective properties. However, little is known about the potential beneficial effect of ICS II on neuronal cell proliferation, and its possible underlying mechanism remains still unclear. We hypothesized that the beneficial effect of ICS II on neuron-like highly differentiated rat pheochromocytoma (PC12) cell proliferation is correlated with the nitric oxide (NO) signaling pathway and its upstream of PI3K/AKT pathway...
October 31, 2017: Neurochemistry International
Wengui Shi, Yuhai Gao, Yuanyuan Wang, Jian Zhou, Zhenlong Wei, Xiaoni Ma, Huiping Ma, Cory J Xian, Jufang Wang, Keming Chen
Icariin, a prenylated flavonol glycoside isolated from the herb Epimedium, has been considered as a potential alternative therapy for osteoporosis. Previous research has shown that unlike other flavonoids, icariin is unlikely to act via the estrogen receptor, but its exact mechanism of action is unknown. In this study, using rat calvarial osteoblast culture and rat bone growth models, we demonstrated that icariin promotes bone formation by activating the cAMP/protein kinase A (PKA)/cAMP response element-binding protein (CREB) pathway requiring functional primary cilia of osteoblasts...
October 31, 2017: Journal of Biological Chemistry
Hyun Jun Park, Yean Kyoung Koo, Min Jung Park, Yoon Kyung Hwang, Sung Yeoun Hwang, Nam Cheol Park
PURPOSE: We investigated the protective effect of a mixture of 2 herbal extracts, KH-465, which consisted of Epimedium koreanum Nakai and Angelica gigas Nakai, on spermatogenesis in a luteinizing hormone-releasing hormone (LHRH) agonist-induced rat model of male infertility. MATERIALS AND METHODS: Seventy-five 12-week-old male Sprague-Dawley rats were randomly divided into 5 groups, containing 15 rats each: a normal control group that received no treatment and 4 experimental groups (I, II, III, and IV) in which an LHRH agonist was administered for 4 weeks to induce spermatogenic failure...
October 25, 2017: World Journal of Men's Health
Chenxia Sheng, Panpan Xu, Kexin Zhou, Dan Deng, Chunhu Zhang, Zhe Wang
Icariin (ICA), a prenylated flavanol glycoside present in abundant quantities in Epimedium sagittatum, has shown promise in the treatment and prevention of Alzheimer's disease. Damage to synaptic plasticity induced by amyloid-beta-mediated neurotoxicity is considered a main pathological mechanism driving the learning and memory deficits present in patients with Alzheimer's disease. This study investigated the neuroprotective effects of icariin in an Aβ1-42-induced rat model of Alzheimer's disease. Our results showed that Aβ1-42 injection induced loss of learning and memory behaviour in the Morris water maze, which could be reversed with intragastric administration of ICA...
2017: BioMed Research International
Jin Li, Li-Li Deng, Zhi-Yong Zhou, Ding Yuan, Chang-Cheng Zhang, Ting Wang
To investigate the protective effect of Panax notoginseng saponins combined with total flavonoids of epimedium on D-gal-induced senescence of H9c2 cells and explore its underlying mechanisms. The 50 mol•L⁻¹ D-gal was used to induce H9c2 cells senescence. Different concentrations of TPNS, TFE, and TPNS combined with TFE were used for 4 hours for pre-treatment. D-gal was used to stimulate H9c2 cardiac muscle cells for 24 h. Then in order to determine the best combined scheme, MTT was used to detect cell viability...
February 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
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