1067198-74-6Relevant articles and documents
3,7-Bis(2-hydroxyethyl)icaritin, a potent inhibitor of phosphodiesterase-5, prevents monocrotaline-induced pulmonary arterial hypertension via NO/cGMP activation in rats
Lan, Tao-Hua,Chen, Xiao-Ling,Wu, Yun-Shan,Qiu, Hui-Liang,Li, Jun-Zhe,Ruan, Xin-Min,Xu, Dan-Ping,Lin, Dong-Qun
, p. 102 - 111 (2018)
Pulmonary arterial hypertension (PAH) is a chronic progressive disease which leads to elevated pulmonary arterial pressure and right heart failure. 3,7-Bis(2-hydroxyethyl)icaritin (ICT), an icariin derivatives, was reported to have potent inhibitory activ
Synthesis and cancer cell growth inhibitory activity of icaritin derivatives
Wang, Chen,Wu, Ping,Shi, Jing-Fang,Jiang, Zi-Hua,Wei, Xiao-Yi
, p. 139 - 150 (2015)
Abstract A series of icaritin derivatives bearing carboxylic acid or carboxylic ester groups are synthesized, and their in vitro cytotoxic activity against three cancer cell lines, MCF-7, MDA-MB-435s, and A549, are evaluated by MTT assay. Several derivati
Icaritin (ICT) derivative and preparation method and application thereof
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Paragraph 0035-0039, (2019/11/04)
The invention belongs to the field of pharmaceutical chemistry, and particularly relates to an icaritin (ICT) derivative shown as the formula (II), a pharmacologically-allowable salt and preparation method of the ICT derivative, and application of the ICT
Icaritin (ICT) derivative and preparation method and application thereof
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Paragraph 0038-0041, (2019/11/04)
The invention belongs to the field of pharmaceutical chemistry, and particularly relates to an icaritin (ICT) derivative shown as the formula (I), a pharmacologically-allowable salt and preparation method of the ICT derivative, and application of the ICT
Herba Epimedii glycoside compound and use thereof
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, (2017/08/24)
The invention relates to an icariin compound and an application of the icariin compound in preparing medicines for preventing and treating fracture and osteoporosis. Particularly, the invention relates to the compound shown in a general formula (I) in the specification, a stereisomer, a stereomer, a tautomer, oxynitrides, hydrates, solvates, metabolites, and pharmaceutically acceptable salts or prodrugs thereof, wherein the variables are defined in the specification. The invention further relates to use of the compound, the stereisomer, the stereomer, the tautomer, oxynitrides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or salt of prodrugs thereof as medicines, particularly use in preparing medicines for preventing and treating fracture and osteoporosis.
Herba Epimedii derivative and its preparation and use
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Paragraph 0023; 0024; 0025; 0026, (2017/08/25)
The invention discloses icaritin derivatives as well as a preparation method and application thereof. The structure of the icaritin derivatives is showed in the formula (1), wherein m is equal to 2 and n is equal to 3 in a compound 1; or m is equal to 3 a
Potent inhibition of human phosphodiesterase-5 by icariin derivatives
Dell'Agli, Mario,Galli, Germana V.,Dal Cero, Esther,Belluti, Federica,Matera, Riccardo,Zironi, Elisa,Pagliuca, Giampiero,Bosisio, Enrica
experimental part, p. 1513 - 1517 (2009/09/29)
Plant extracts traditionally used for male impotence (Tribulus terrestris, Ferula hermonis, Epimedium brevicornum, Cinnamomum cassia), and the individual compounds cinnamaldehyde, ferutinin, and icariin, were screened against phosphodiesterase-5A1 (PDE5A1) activity. Human recombinant PDE5A1 was used as the enzyme source. Only E. brevicornum extract (80% inhibition at 50 μg/mL) and its active principle icariin (1) (IC50 5.9 μM) were active. To improve its inhibitory activity, 1 was subjected to various structural modifications. Thus, 3,7-bis(2-hydroxyethyl)icaritin (5), where both sugars in 1 were replaced with hydroxyethyl residues, potently inhibited PDE5A1 with an IC50 very close to that of sildenafil (IC50 75 vs 74 nM). Thus, 5 was 80 times more potent than 1, and its selectivity versus phosphodiesterase-6 (PDE6) and cyclic adenosine monophosphate-phosphodiesterase (cAMP-PDE) was much higher in comparison with sildenafil. The improved pharmacodynamic profile and lack of cytotoxicity on human fibroblasts make compound 5 a promising candidate for further development.