Preparation of icariside II from icariin by enzymatic hydrolysis method

Xia, Qing; Xu, Donghui; Huang, Zhenchi; Li, Jianjun; Wang, Xin-Qun; Wang, Xiu; Liu, Shangquan

doi:10.1016/j.fitote.2009.12.006

Cited by 54 publications

(34 citation statements)

References 9 publications

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“…Based on the close structural relationship with icariin and the advantage of a relatively high content of natural icariin, baohuoside I can be obtained by enzymatic hydrolysis of icariin. [9] The chemical structures of icariin and baohuoside I are depicted in [Figure 1]. …”

Section: Introductionmentioning

confidence: 99%

Effect of β-cyclodextrin complexation on solubility and enzymatic hydrolysis rate of icariin

et al. 2013

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Objective:The aim of this work was to investigate the effect of β-cyclodextrin complexation on the solubility and hydrolysis rate of icariin.Material and Methods:The inclusion complex of icariin at the molar ratio of 1:1 was obtained by the dropping method and was characterized by differential scanning calorimetry. The solubility of icariin complex in water at 37°C was 36 times greater than that of free icariin. Enzymatic hydrolysis conditions were tested for the bioconversion of icariin by mono-factor experimental design.Methods:The inclusion complex of icariin at the molar ratio of 1:1 was obtained by the dropping method and was characterized by differential scanning calorimetry. The solubility of icariin complex in water at 37°C was 36 times greater than that of free icariin. Enzymatic hydrolysis conditions were tested for the bioconversion of icariin by mono-factor experimental design.Results:The enzymatic hydrolysis experiment showed that icariin can be transformed into baohuoside I. The optimum conditions determined were as follows: pH 5.0, 50°C, the ratio of cellulase/substrate (0.6), the concentration of icariin 20 mg/ml, and reaction time 12 h. Under these enzymatic conditions, 98.2% transforming rate of baohuoside I from icariin in inclusion complexes was obtained.ConclusionThe aqueous solubility and enzymatic hydrolysis rate of icariin were improved owing to the inclusion complexation.

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Section: Introductionmentioning

confidence: 99%

Effect of β-cyclodextrin complexation on solubility and enzymatic hydrolysis rate of icariin

et al. 2013

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“…It has been reported that the EH-derived flavonoid glycosides bearing at least two sugars, such as epimedins (1, 2) and icariin (4), were quickly metabolized to icarisid II (6) and then slowly to anhydroicaritin (8) in the intestinal flora of rabbits (18). Additionally, Xia et al mentioned that 6 is the main metabolic component in vivo after the administration of EH (19). Quercetin, which is a common flavonoid contained in edible plants, has been reported to show anti-androgenic activity in experiments using LNCaP cells (20).…”

Section: Resultsmentioning

confidence: 99%

Anti-Androgenic Activity of Icarisid II from Epimedium Herb in Prostate Cancer LNCaP Cells

Miura

Oyama

Iguchi

et al. 2015

J Nutr Sci Vitaminol

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Summary Anti-androgens are regarded as potential therapeutic agents for the treatment of prostate cancer. We determined that an epimedium herb (EH) extract exhibited antiandrogenic activity in a luciferase assay using androgen receptor-positive prostate cancer LNCaP cells. Nine EH-derived flavonoids were examined. The results identified icarisid II as a very potent anti-androgenic EH-derived flavonoid. A quantitative RT-PCR analysis confirmed that the flavonol suppressed the expression of the androgen-responsive KLK3 gene.

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“…Preparation of ICA II In order to get ICA II (chemical structure shown in Figure 1a), icariin was bio-transformed by the action of β-glucosidase as previous described (11): 50°C, 0.2 M disodium hydrogen phosphate and citric acid buffer system (pH 6.0); the ratio of icariin and enzyme was 1:1; the reaction time was 5 hours; the purification was performed by high-performance liquid chromatography (purity ≥99%). Then, the compound was suspended in 1% carboxymethylcellulose (CMC) to a concentration of 1 mg/ml and fed at the dose of 1, 5, and 10 mg/kg daily respectively.…”

Section: Methodsmentioning

confidence: 99%

Icariside II Attenuates Chronic Hydrocephalus in an Experimental Subarachnoid Hemorrhage Rat Model

Dong¹,

Ming²,

Ye³

et al. 2018

J Pharm Pharm Sci

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Purpose To investigate the role of ICA II in subarachnoid hemorrhage (SAH)- related chronic hydrocephalus. Methods A two hemorrhage injection model of SAH was created in Sprague Dawley rats (6-8 weeks). A total of 125 rats were randomly assigned into five groups: Sham group, SAH group, SAH+ ICA II (1 mg/kg) group, SAH + ICA II (5 mg/kg) group, and SAH + ICA II (10 mg/kg) group. TGF-β1, phospho-Smad2/3, connective tissue growth factor (CTGF), and procollagen type I carboxy-terminal propeptide (PICP) were assessed via real-time PCR, Western blotting, and enzyme-linked immunosorbent assay. Lateral ventricular index, Masson staining, and Morris water maze tests were employed to evaluate subarachnoid fibrosis, hydrocephalus, and long term neurological function following SAH. Results ICA II (1, 5, 10 mg/kg) inhibited subarachnoid fibrosis, attenuated ventriculomegaly, and effectively suppressed SAH related chronic hydrocephalus. In addition, parallel reduced expression of members of the TGF-β1/Smad/CTGF signaling pathway were observed. Importantly, ICA II may improve long term neurocognitive deficits after SAH. Conclusion ICA II might suppress fibrosis via inhibition of TGF-β1/Smad/CTGF pathway, prevent the development of SAH related chronic hydrocephalus, and improve long term neurocognitive defects following SAH.

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Preparation of icariside II from icariin by enzymatic hydrolysis method

Cited by 54 publications

References 9 publications

Effect of β-cyclodextrin complexation on solubility and enzymatic hydrolysis rate of icariin

Effect of β-cyclodextrin complexation on solubility and enzymatic hydrolysis rate of icariin

Anti-Androgenic Activity of Icarisid II from Epimedium Herb in Prostate Cancer LNCaP Cells

Icariside II Attenuates Chronic Hydrocephalus in an Experimental Subarachnoid Hemorrhage Rat Model

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