Journal of Fungi
·
2022
·Vol. 8
·期 6
·644
·
IF 5.724
Hanghang Lou,Xiayu Liu,Siyu Liu,Qihe Chen
Icariin is the most effective bioactive compound in Herba Epimedii. To enhance the content of icariin in the epimedium water extract, a novel strain,Papiliotrema laurentiiZJU-L07, producing an intracellular α-L-rhamnosidase was isolated from the soil and mutagenized. The specific activity of α-L-rhamnosidase was 29.89 U·mg−1through purification, and the molecular mass of the enzyme was 100 kDa, as assayed by SDS-PAGE. The characterization of the purified enzyme was determined. The optimal temperature and pH were 55 °C and 7.0, respectively. The enzyme was stable in the pH range 5.5–9.0 for 2 h over 80% and the temperature range 30–40 °C for 2 h more than 70%. The enzyme activity was inhibited by Ca2+, Fe2+, Cu2+, and Mg2+, especially Fe2+. The kinetic parameters ofKmandVmaxwere 1.38 mM and 24.64 μmol·mg−1·min−1using pNPR as the substrate, respectively. When epimedin C was used as a nature substrate to determine the kinetic parameters of α-L-rhamnosidase, the values ofKmandVmaxwere 3.28 mM and 0.01 μmol·mg−1·min−1, respectively. The conditions of enzymatic hydrolysis were optimized through single factor experiments and response surface methodology. The icariin yield increased from 61% to over 83% after optimization. The enzymatic hydrolysis method could be used for the industrialized production of icariin. At the same time, this enzyme could also cleave the α-1,2 glycosidic linkage between glucoside and rhamnoside in naringin and neohesperidin, which could be applicable in other biotechnological processes.Keywords:Papiliotrema laurentiiZJU-L07;epimedin C;icariin;α-L-rhamnosidase;enzyme characteristics;optimization
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高影响因子
Cancer Cell International
·
2021
·Vol. 21
·期 1
·1-14
·
IF 5.722
Li Chunyang,Yang Shuangqing,Ma Huaqing,Ruan Mengjia,Fang Luyan,Cheng Jing
Background Cervical cancer is a type of the most common gynecology tumor in women of the whole world. Accumulating data have shown that icariin (ICA), a natural compound, has anti-cancer activity in different cancers, including cervical cancer. The study aimed to reveal the antitumor effects and the possible underlying mechanism of ICA in U14 tumor-bearing mice and SiHa cells.Methods The antitumor effects of ICA were investigated in vivo and in vitro. The expression of TLR4/MyD88/NF-κB and Wnt/β-catenin signaling pathways were evaluated.Results We found that ICA significantly suppressed tumor tissue growth and SiHa cells viability in a dose-dependent manner. Also, ICA enhanced the anti-tumor humoral immunity in vivo. Moreover, ICA significantly improved the composition of the microbiota in mice models. Additionally, the results clarified that ICA significantly inhibited the migration, invasion capacity, and expression levels of TGF-β1, TNF-α, IL-6, IL-17A, IL-10 in SiHa cells. Meanwhile, ICA was revealed to promote the apoptosis of cervical cancer cells by down-regulating Ki67, survivin, Bcl-2, c-Myc, and up-regulating P16, P53, Bax levels in vivo and in vitro. For the part of mechanism exploration, we showed that ICA inhibits the inflammation, proliferation, migration, and invasion, as well as promotes apoptosis and immunity in cervical cancer through impairment of TLR4/MyD88/NF-κB and Wnt/β-catenin pathways.Conclusion sTaken together, ICA could be a potential supplementary agent for cervical cancer treatment.
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高影响因子
BIOCHEMICAL PHARMACOLOGY
·
2017
·
IF 4.581
Jinhua Hu,Zhao Mao,Shuangcheng He,Yuanran Zhan,Rui Ning,Wei Liu,Bingfang Yan,Jian Yang
Osteoporosis is a serious public health concern worldwide. Herba epimedii has been used for centuries and even thousands of years to treat osteoporotic conditions. Icariin , a flavonol glycoside , is one of the major active ingredients. In this study, we have shown that icariin protected against glucocorticoid-induced osteoporotic changes in SaoS-2 cells and mice. We have also shown that dexamethasone (a glucocorticoid) suppressed and icariin induced DEC1, a structurally distinct helix-loop-helix protein. DEC1 overexpression promoted whereas DEC1 knockdown decreased osteogenic activity. Likewise, DEC1 overexpression and knockdown inversely regulated the expression of β-catenin and PIK3CA, an essential player in the Wnt/β-catenin and PI3K/Akt signaling pathways, respectively. Interestingly, DKK1, an inhibitor of Wnt/β-catenin signaling inhibitor, and LY294002 , an inhibitor of PI3K/Akt signaling, abolished the induction of DEC1 by icariin. It is established that these two pathways are interconnected by the phosphorylation status of GSK3β. Dexamethasone decreased but icariin increased GSK3β phosphorylation. Finally, DEC1 deficient mice developed osteoporotic phenotypes. Taken together, it is concluded that DEC1 likely supports the action of icariin against glucocorticoid induced osteoporosis with an involvement of the PI3K/Akt/GSK3β/β-catenin integrated signaling pathway.
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高影响因子
MOLECULES
·
2026
·Vol. 31
·期 20
·3615
·
IF 5.1
Haoyu Jia,Tong Yan,Luran Wang,Lingling Song
Icariside I is a pharmacologically important prenylated flavonoid glycoside, yet its efficient biocatalytic production from icariin is hindered by the limited stability and recyclability of the enzymes involved. In this study, an α-L-rhamnosidase mutant R783A (Rha R783A) was heterologously expressed, purified, and immobilized within a Cu-based metal–organic framework (MOF) via a one-pot co-precipitation strategy. The resulting Rha R783A@MOF biocomposite exhibited enhanced stability compared to the free enzyme, retaining >90% residual activity after incubation at 60 °C for 2 h and 86.4% after 30 days of storage. It also demonstrated broad pH adaptability. In the biotransformation of icariin, Rha R783A@MOF achieved a 99.8% conversion rate and a 97.8% yield of icariside I. Furthermore, the biocomposite maintained an 88.9% yield after eight consecutive reuse cycles under high-temperature conditions (60 °C), demonstrating excellent operational stability. This work presents a robust and sustainable strategy for icariside I production, highlighting the potential of MOF microparticles as an effective platform for the biocatalytic synthesis of high-value flavonoid compounds.
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JOURNAL OF FOOD COMPOSITION AND ANALYSIS
·
2026
·
IF 5.3
WeiHang Yao,JunYi Ye,PingPing Shen,Richa Raj,BoYang Yu,Xiaorong He,Jian Zhang
This study aims to expand the application of handheld near-infrared spectroscopy combined with machine learning in quantitative analysis of Epimedium . After establishing and evaluating several promising models: Gradient Boosting Regression (GBR), Extra Trees (ET), Extreme Gradient Boosting (eXGB), Support Vector Regression (SVR), Random Forest (RF), Partial Least Squares Regression (PLSR), we selected PLSR and SVR for further optimization due to their excellent performance in terms of R 2 and RMSE. Employing the NIPPY library for data preprocessing and a genetic algorithm for feature selection, models for predicting the contents of four active components in Epimedium were successfully established. The GA-SVR hybrid model delivered the following predictive performance for the four target components: icariin (R 2 :0.9556, RMSE:0.0031, Avg. MAPE:2.07%), epimedin A (R 2 :.9586, RMSE:0.0004, Avg. MAPE:3.60%), epimedin B (R 2 :0.9432, RMSE:0.0003, Avg. MAPE:3.58%) and epimedin C (R 2 :0.9232, RMSE:0.0182, Avg. MAPE:2.33%). These findings establish a novel paradigm for high-throughput analysis and quality assessment of food and traditional Chinese medicine active ingredients.
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