Icariin induces developmental toxicity via thyroid hormone disruption in zebrafish larvae
Food Chem Toxicol. 2023 Oct 28;182:114155. doi: 10.1016/j.fct.2023.114155. Online ahead of print.ABSTRACTIcariin (ICA) is a natural flavonoid isolated from the traditional Chinese medicinal herb, Epimedium brevicornu Maxim. Although previous studies have reported that ICA exhibits various pharmacological activities, little is known about its toxicology. Herein, zebrafish embryos were exposed to ICA at 0, 2.5, 10, and 40 μM. In developmental analysis, reduced hatching rates, decreased body length, and abnormal swim bladder were found after treatment with 10 and 40 μM ICA. In addition, the ability of locomotor behavior was...
Source: Food and Chemical Toxicology - October 28, 2023 Category: Food Science Authors: Meifang Wu Naying Zheng Xiaoxiao Zhan Jianzhang He Min Xiao Zhenghong Zuo Chengyong He Source Type: research

Icariin induces developmental toxicity via thyroid hormone disruption in zebrafish larvae
Food Chem Toxicol. 2023 Oct 28;182:114155. doi: 10.1016/j.fct.2023.114155. Online ahead of print.ABSTRACTIcariin (ICA) is a natural flavonoid isolated from the traditional Chinese medicinal herb, Epimedium brevicornu Maxim. Although previous studies have reported that ICA exhibits various pharmacological activities, little is known about its toxicology. Herein, zebrafish embryos were exposed to ICA at 0, 2.5, 10, and 40 μM. In developmental analysis, reduced hatching rates, decreased body length, and abnormal swim bladder were found after treatment with 10 and 40 μM ICA. In addition, the ability of locomotor behavior was...
Source: Food and Chemical Toxicology - October 28, 2023 Category: Food Science Authors: Meifang Wu Naying Zheng Xiaoxiao Zhan Jianzhang He Min Xiao Zhenghong Zuo Chengyong He Source Type: research

Molecules, Vol. 28, Pages 7300: Effects of Icariin and Its Metabolites on GPCR Regulation and MK-801-Induced Schizophrenia-Like Behaviors in Mice
Jung Choi Icariin, a major bioactive compound found in the Epimedium genus, has been reported to exert protective effects against neurodegenerative disorders. In the current study, we aimed to investigate the regulatory effect of icariin and its active metabolites (icariside II and icaritin) against prime G-protein-coupled receptor targets, considering their association with neuronal disorders. Icariside II exhibited selective agonist activity towards the dopamine D3 receptor (D3R), with half-maximal effective concentrations of 13.29 μM. Additionally, they effectively inhibited the specific binding of rad...
Source: Molecules - October 27, 2023 Category: Chemistry Authors: Seong Kim Ryu Jeong Jung Choi Tags: Article Source Type: research

Anti-inflammatory effects of icariin in the acute and chronic phases of the mouse pilocarpine model of epilepsy
This study was to explore the potential therapeutic effects of icariin on mouse pilocarpine model of epilepsy and its underlying mechanisms in vivo and in vitro. To this end, we firstly measured the serum concentrations of the proinflammatory cytokines IL-1β and IL-6 from patients with temporal lobe epilepsy and found that patients with a higher seizure frequency showed correspondingly higher inflammatory reaction. Mouse pharmacokinetic study, transmembrane transportation assay, and cell viability assay collectively demonstrated that ICA was able to cross the blood-brain barrier and has good biocompatibility. The acute an...
Source: European Journal of Pharmacology - October 22, 2023 Category: Drugs & Pharmacology Authors: Jing Wang Yunyi Liu Yuanxia Wu Ke Yang Kaiyi Yang Luzhe Yan Li Feng Source Type: research

Anti-inflammatory effects of icariin in the acute and chronic phases of the mouse pilocarpine model of epilepsy
This study was to explore the potential therapeutic effects of icariin on mouse pilocarpine model of epilepsy and its underlying mechanisms in vivo and in vitro. To this end, we firstly measured the serum concentrations of the proinflammatory cytokines IL-1β and IL-6 from patients with temporal lobe epilepsy and found that patients with a higher seizure frequency showed correspondingly higher inflammatory reaction. Mouse pharmacokinetic study, transmembrane transportation assay, and cell viability assay collectively demonstrated that ICA was able to cross the blood-brain barrier and has good biocompatibility. The acute an...
Source: European Journal of Pharmacology - October 22, 2023 Category: Drugs & Pharmacology Authors: Jing Wang Yunyi Liu Yuanxia Wu Ke Yang Kaiyi Yang Luzhe Yan Li Feng Source Type: research

Molecules, Vol. 28, Pages 7173: Advancements in the Biotransformation and Biosynthesis of the Primary Active Flavonoids Derived from Epimedium
n Yongjun Wei Epimedium is a classical Chinese herbal medicine, which has been used extensively to treat various diseases, such as sexual dysfunction, osteoporosis, cancer, rheumatoid arthritis, and brain diseases. Flavonoids, such as icariin, baohuoside I, icaritin, and epimedin C, are the main active ingredients with diverse pharmacological activities. Currently, most Epimedium flavonoids are extracted from Epimedium plants, but this method cannot meet the increasing market demand. Biotransformation strategies promised huge potential for increasing the contents of high-value Epimedium flavonoids, which would promot...
Source: Molecules - October 19, 2023 Category: Chemistry Authors: Xiaoling Zhang Bingling Tang Sijie Wen Yitong Wang Chengxue Pan Lingbo Qu Yulong Yin Yongjun Wei Tags: Review Source Type: research

Insights into the biological activity and cytotoxic mechanism of Epimedium pubigerum
Chem Biodivers. 2023 Oct 11:e202301003. doi: 10.1002/cbdv.202301003. Online ahead of print.ABSTRACTIn this work, the phytochemical characterization, biological activity, and cytotoxic mechanism of aerial and rhizome methanol extracts (SME and RME) of Epimedium pubigerum were investigated to demonstrate its potential usage in the treatment of lung cancer. LC-HRMS analysis, total phenolic/flavonoid content assay, DPPH radical scavenging assay, DNA interaction, cytotoxicity, and western blotting were investigated using different methods. Fumaric acid was found to be the most abundant compound in both extracts. SME and RME wer...
Source: Chemistry and Biodiversity - October 11, 2023 Category: Biochemistry Authors: G ökçe Seyhan Didem Akkaya K übra Kolci Rengin Reis Nurdan Yaz ıcı Elif Nur Barut Burak Barut Source Type: research

Icaritin ameliorates RANKL-mediated osteoclastogenesis and ovariectomy-induced osteoporosis
Aging (Albany NY). 2023 Oct 3;15. doi: 10.18632/aging.205068. Online ahead of print.ABSTRACTA rapidly aging society and longer life expectancy are causing osteoporosis to become a global epidemic. Over the last five decades, a number of drugs aimed at reducing bone resorption or restoring bone mass have been developed, but their efficacy and safety are limited. Icaritin (ICT) is a natural compound extracted from anti-osteoporosis herb Epimedium spp. and has been shown to inhibit osteoclast differentiation. However, the molecular mechanism by which ICT weaken RANKL-induced osteoclast differentiation has not been completely ...
Source: Aging - October 4, 2023 Category: Biomedical Science Authors: Jun-Ming Huang Zhe Wang Guo-Bin Qi Qi Lai A-Lan Jiang Yue-Qi Zhang Kun Chen Xiu-Hui Wang Source Type: research

Icariin inhibits hypertrophy by regulation of GPER1 and CaMKII/HDAC4/MEF2C signaling crosstalk in ovariectomized mice
This study aimed to provide detailed information regarding the antihypertrophic effects of ICA in ovariectomized female mice. Female mice were subjected to ovariectomy (OVX) and transverse aortic constriction and then orally treated with ICA at doses of 30, 60 or 120 mg/kg/day for 4 weeks. Morphological assessments, echocardiographic parameters, histological analyses, and immunofluorescence were performed to evaluate cardiac hypertrophy. Cardiomyocytes from mice or rats were stimulated using phenylephrine, and cell surface and hypertrophy markers were tested using immunofluorescence and qPCR. Western blotting, qPCR, and lu...
Source: Chemico-Biological Interactions - September 22, 2023 Category: Molecular Biology Authors: Wenxia Zhao Xiaoli Shan Xueqin Li Shuang Lu Lei Xia Huihua Chen Chen Zhang Wei Guo Ming Xu Rong Lu Pei Zhao Source Type: research

Icariin inhibits hypertrophy by regulation of GPER1 and CaMKII/HDAC4/MEF2C signaling crosstalk in ovariectomized mice
This study aimed to provide detailed information regarding the antihypertrophic effects of ICA in ovariectomized female mice. Female mice were subjected to ovariectomy (OVX) and transverse aortic constriction and then orally treated with ICA at doses of 30, 60 or 120 mg/kg/day for 4 weeks. Morphological assessments, echocardiographic parameters, histological analyses, and immunofluorescence were performed to evaluate cardiac hypertrophy. Cardiomyocytes from mice or rats were stimulated using phenylephrine, and cell surface and hypertrophy markers were tested using immunofluorescence and qPCR. Western blotting, qPCR, and lu...
Source: Chemico-Biological Interactions - September 22, 2023 Category: Molecular Biology Authors: Wenxia Zhao Xiaoli Shan Xueqin Li Shuang Lu Lei Xia Huihua Chen Chen Zhang Wei Guo Ming Xu Rong Lu Pei Zhao Source Type: research

Icaritin attenuates recurrent spontaneous abortion in mice by modulating Treg/Th17 imbalance via TGF- β/SMAD signaling pathway
In conclusion, our study suggested that ICT ameliorated RSA by modulating Treg/Th17 cell imbalance via the TGF-β/SMAD signaling pathway. GENERAL SIGNIFICANCE: Our results highlighted the potential of ICT as a novel therapeutic agent for RSA, offering new insights into the underlying mechanisms and opening avenues for future research and clinical translation.PMID:37689142 | DOI:10.1016/j.bbamcr.2023.119574 (Source: Biochimica et Biophysica Acta)
Source: Biochimica et Biophysica Acta - September 9, 2023 Category: Biochemistry Authors: Si-Qing Huang Lei Xia Yan-Qiu Xia Hong-Li Huang Li Dong Source Type: research

Icaritin attenuates recurrent spontaneous abortion in mice by modulating Treg/Th17 imbalance via TGF- β/SMAD signaling pathway
In conclusion, our study suggested that ICT ameliorated RSA by modulating Treg/Th17 cell imbalance via the TGF-β/SMAD signaling pathway. GENERAL SIGNIFICANCE: Our results highlighted the potential of ICT as a novel therapeutic agent for RSA, offering new insights into the underlying mechanisms and opening avenues for future research and clinical translation.PMID:37689142 | DOI:10.1016/j.bbamcr.2023.119574 (Source: Biochimica et Biophysica Acta)
Source: Biochimica et Biophysica Acta - September 9, 2023 Category: Biochemistry Authors: Si-Qing Huang Lei Xia Yan-Qiu Xia Hong-Li Huang Li Dong Source Type: research

Two new prenylated flavonol glycosides from < em > Epimedium koreanum < /em > Nakai leaves and their anti-pulmonary fibrosis activities
Nat Prod Res. 2023 Sep 3:1-8. doi: 10.1080/14786419.2023.2246631. Online ahead of print.ABSTRACTTwo new prenylated flavonol glycosides, namely Desmethylicaritin-3-O-β-D-glucopyranosyl-(1→3)-α-L(4″-O-acetyl) rhamnopyranosyl-7-O-β-D(6''''-O-acetyl)-glucopyranoside (1) and 5,7,3',4'-tetrahydroxyl-8-(3,3-dimethylallyl)-flavonol-3-O-α-L-rhamnopyranoside (2), and one with no NMR spectral data reported (3) were isolated from Epimedium koreanum Nakai. Their structures were elucidated by 1D, 2D NMR and HRESIMS analysis. The identification of the sugar moieties was carried out by means of acid hydrolysis and HPLC analysis of...
Source: Natural Product Research - September 3, 2023 Category: Biochemistry Authors: Yudan Zhao Linxuan Teng Ruiqi Zhang Chongning Lv Jincai Lu Source Type: research

Two new prenylated flavonol glycosides from < em > Epimedium koreanum < /em > Nakai leaves and their anti-pulmonary fibrosis activities
Nat Prod Res. 2023 Sep 3:1-8. doi: 10.1080/14786419.2023.2246631. Online ahead of print.ABSTRACTTwo new prenylated flavonol glycosides, namely Desmethylicaritin-3-O-β-D-glucopyranosyl-(1→3)-α-L(4″-O-acetyl) rhamnopyranosyl-7-O-β-D(6''''-O-acetyl)-glucopyranoside (1) and 5,7,3',4'-tetrahydroxyl-8-(3,3-dimethylallyl)-flavonol-3-O-α-L-rhamnopyranoside (2), and one with no NMR spectral data reported (3) were isolated from Epimedium koreanum Nakai. Their structures were elucidated by 1D, 2D NMR and HRESIMS analysis. The identification of the sugar moieties was carried out by means of acid hydrolysis and HPLC analysis of...
Source: Cell Research - September 3, 2023 Category: Cytology Authors: Yudan Zhao Linxuan Teng Ruiqi Zhang Chongning Lv Jincai Lu Source Type: research

Two new prenylated flavonol glycosides from < em > Epimedium koreanum < /em > Nakai leaves and their anti-pulmonary fibrosis activities
Nat Prod Res. 2023 Sep 3:1-8. doi: 10.1080/14786419.2023.2246631. Online ahead of print.ABSTRACTTwo new prenylated flavonol glycosides, namely Desmethylicaritin-3-O-β-D-glucopyranosyl-(1→3)-α-L(4″-O-acetyl) rhamnopyranosyl-7-O-β-D(6''''-O-acetyl)-glucopyranoside (1) and 5,7,3',4'-tetrahydroxyl-8-(3,3-dimethylallyl)-flavonol-3-O-α-L-rhamnopyranoside (2), and one with no NMR spectral data reported (3) were isolated from Epimedium koreanum Nakai. Their structures were elucidated by 1D, 2D NMR and HRESIMS analysis. The identification of the sugar moieties was carried out by means of acid hydrolysis and HPLC analysis of...
Source: Natural Product Research - September 3, 2023 Category: Biochemistry Authors: Yudan Zhao Linxuan Teng Ruiqi Zhang Chongning Lv Jincai Lu Source Type: research