Molecular Catalysis
·
2025
·
IF 4.9
Haoyu Jia,Jinyue Hu,Le Zhao,Xiaoke Zheng,Weisheng Feng
Baohuoside I, a valuable flavonoid derivative of Herba Epimedii , exhibits superior bioactivities compared to its precursor, icariin. The conversion of icariin to baohuoside I using β-glucosidase (β-G) is an efficient approach for industrial production. Herein, β-G was successfully immobilized into a porous materials metal-organic frameworks (MOFs) via a simple one-pot coprecipitation method. The β-G@MOF biocomposite exhibited high encapsulation efficiency and excellent tolerance to extreme pH, high temperature, organic solvent and glucose. Remarkably, β-G@MOF retained its full initial activity even at 200 mM glucose. The β-G@MOF has a lower K m value compared with the free β-G, indicating enhanced substrate affinity. A conversion of 99.8 % was achieved in the hydrolysis of icariin to baohuoside I within 2 h. Additionally, β-G@MOF exhibited significantly reusability, maintaining 70.5 % yield after eight cycles at 60 °C. This study provides a simple, efficient, and sustainable approach for industrial production of baohuoside I and has potential for hydrolyzing other poorly soluble flavonoids.
研究领域:
生物化学
·
材料科学
·
药物生产
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产品关联
DOI
高影响因子
ENZYME AND MICROBIAL TECHNOLOGY
·
2019
·
IF 3.553
Yuping Shen,Man Wang,Jinwei Zhou,Yufei Chen,Lili Xu,Mengru Wu,Guohua Xia,James P. Tam,Jiangnan Yu,Xiying Teng,Huan Yang,Xiaobin Jia
Baohuoside I, a rare secondary glycoside from Epimedii Folium, has anti-osteoporosis and other pharmacological effects. In addition, it exhibits improved bioactivities compared with its original glycoside icariin. Conventional methods for the production of baohuoside I, such as acid hydrolysis, exhibit very low efficiency with serious pollution and substantial byproducts. The aim of this study was to develop an eco-efficient biphasic enzymatic hydrolysis system for the green production of rare baohuoside I. β -glucanase was selected to hydrolyze icariin and showed better performance than β -glucosidase. The biphasic system was constructed using HAc-NaAc buffer (pH 4.5) containing β -glucanase/icariin (C icariin = 100 mg/mL; 1:1, w/w ) and propyl acetate (1:2, v/v ), and the hydrolysis was performed at 60℃ for 6 h. The hydrolysis capacity of icariin in the system was largely increased from 0.5 mg/mL to 100 mg/mL. The conversion ratio of icariin was greater than 99% in a 100-fold scale-up pilot test, demonstrating its strong potential for industrial applications. Furthermore, a process flow and production plant were designed to produce 1 ton of baohuoside I annually, and the profit would be approximately 4.5-fold its total cost. Biphasic enzymatic hydrolysis is an eco-efficient technology to produce baohuoside I and represents a promising method in the pharmaceutical industry.
研究领域:
药学
·
生物技术
·
植物化学
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产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2019
·
IF 3.829
Mengna Liu,Bingjie Wang,Chunjing Guo,Xiaoya Hou,Ziting Cheng,Daquan Chen
In this study, novel multifunctional folic acid, biotin, and CD44 receptors targeted and pH-sensitive “nano-actiniaes” were fabricated with icariin (ICA) and curcumin (Cur) as loaded model drugs for breast cancer therapy. The newly synthesized polymer oligomeric hyaluronic acid-hydrazone bond-folic acid-biotin (Bio-oHA-Hyd-FA) was characterized by 1H NMR spectrogram (proton nuclear magnetic resonance). The obtained drug carrier Bio-oHA-Hyd-FA self-assembled into nanomicelles, named as “nano-actiniaes”, in aqueous media with hydrodynamic diameter of 162.7 ± 5 nm. The size, surface zeta potential, and morphology of the “nano-actiniaes” were observed via TEM. The in vitro release experiment indicated that much more encapsulated icariin (ICA) and curcumin (Cur) were released from the Bio-oHA-Hyd-FA micelles (nano-actiniaes) in the acidic environment. Additionally, the cytotoxicity research demonstrated that the Bio-oHA-Hyd-FA carrier material was completely nontoxic, and the ICA&Cur “nano-actiniaes” had greater cytotoxicity compared with other control groups. In addition, the “nano-actiniaes” were found to significantly inhibit cancer cell invasion by Transwell assay. Moreover, in vivo evaluation of anti-tumor effect illustrated that the ICA and Cur “nano-actiniaes” possessed inhibitory effect on tumors. Consequently, the multi-targeted pH-sensitive “nano-actiniaes” can realize significant tumor targeting and effectively inhibit tumor growth.
研究领域:
药剂学
·
肿瘤学
·
生物材料科学
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产品关联
DOI
PubMed
高影响因子
Artificial Cells Nanomedicine and Biotechnology
·
2019
·
IF 4.462
Yongqiang Zheng,Lingli Lu,Zhengli Yan,Sufang Jiang,Shanyi Yang,Yingzi Zhang,Kangwei Xu,Chunlian He,Xiaojun Tao,Qiufang Zhang
Icariin (ICA), a major active ingredient from Chinese medicine, has unique pharmacological effects on ischaemic heart disease. However, its hydrophobic property limits its administration and leads to poor efficacy. This work aimed to change its hydrophobic property and improve the treatment efficacy. We designed a new nano-drug to increase the ICA delivery. ICA was modified with hydrophilic polyethylene glycol monomethyl ether (mPEG) by a succinic anhydride linker to form a polyethylene glycol-icariin (mPEG-ICA) polymer. The structure of this polymer was identified by Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. The content of ICA in the polymer was 32% as detected by ultraviolet spectrophotometry. mPEG-ICA nanoparticles, of 143.3 nm, were prepared by the dialysis method, and zeta potential was 0.439 mV by dynamic light scattering. The nanoparticles had a spherical shape on transmission electron microscopy. In media with pH 7.4 and 6.8, ICA release from mPEG-ICA nanoparticles after 72 h was about 0.78% and 64.05%, respectively, so the ICA release depended on the release media pH. On MTT and lactate dehydrogenase activity assay, mPEG-ICA nanoparticles could reduce cell damage induced by oxgen-glucose deprivation. Hoechst 33258 staining and TUNEL and AnnexinV-FITC/PI double staining showed that ICA nanoparticles could increase the activity of H9c2 cardiomyocytes under oxgen-glucose deprivation conditions by decreasing apoptosis. ICA modified by hydrophilic mPEG could improve its efficacy.
研究领域:
药理学
·
纳米医学
·
心脏病学
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DOI
PubMed
高影响因子
FOOD AND CHEMICAL TOXICOLOGY
·
2024
·
IF 3.9
Jiewei Zheng,Xin Yang,Cong Zhang,Weipeng Zhang,Yue Hu,Lihai Zeng,Lili Liu,Guoliang Li
Icariin (ICA), an active ingredient found in Epimedium , possesses antioxidant and anti-inflammatory properties and has garnered widespread attention in recent years. This study investigated the protective effects of ICA against cadmium (Cd)-induced kidney injury in rats. Healthy male specific pathogen-free Sprague–Dawley rats were randomly divided into a control group, Cd group, a low-dose ICA group, a middle-dose ICA group, and a high-dose ICA group using a random number table. Tissue and blood samples were analyzed for renal function markers, histopathology, and gene expression. We found that ICA intervention ameliorates Cd-induced nephrotoxicity by enhancing glomerular filtration, mitigating renal tubular epithelial cell damage, reducing cellular degeneration and edema, and decreasing oxidative stress. ICA demonstrated anti-apoptotic activity through the regulation of pro- and anti-apoptotic gene transcription and by inhibiting apoptosis, thus protecting the kidneys. ICA also exhibited anti-inflammatory effects by reducing the transcription of Cd-induced pro-inflammatory genes, inhibiting nucleotide oligomerization domain-like receptor pyrin domain-containing 3 (NLRP3) inflammasome formation, and preventing pyroptosis. ICA potentially regulated the Toll-like receptor 4/ P2rx7 /nuclear factor kappa B signaling pathway, which modulated the activation of the NLRP3 inflammasome and contributed to its anti-inflammatory action. ICA reduced Cd-induced renal injury in rats, likely through a mechanism involving antioxidant, anti-apoptotic, and anti-inflammatory effects.
研究领域:
药理学
·
毒理学
·
分子生物学
·
肾脏生理学
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DOI
PubMed
高影响因子
ULTRASONICS SONOCHEMISTRY
·
2022
·
IF 9.336
Jinping Wang,Hong Zhu,Yueming Jiang,Jianbo Xiao,Bao Yang,Lingrong Wen
Ultrasound is effective to fabricate nanocomplex. Soymilk is a natural nanocarrier with good compatibility. However, information about soymilk-nutraceuticals nanocomplex is limited. In this work, soymilk was used to encapsulate icariin, a well known nutraceutical with poor bioavailability. The effect of ultrasound on the quality of icariin-soymilk nanocomplexes (ISNCs) was investigated. Ultrasound could reduce the particle size, improve the surface hydrophobicity and change the microstructure of soymilk. With increasing ultrasound treatment time, an increased surface hydrophobicity was observed. The highest encapsulation efficiency (89.67 %) and loading capacity (28.92 µg/mg) were found for USI-20, whereas the smallest particle size (132.47 nm) was observed for USI-120. USI-60 showed the lowest ζ-potential (-31.33 mV) and the highest bioaccessibility (76.08 %). Ultrasound could enhance the storage stability of ISNCs. The data of NMR and fluorescence indicated that ISNCs were mainly stabilized by hydrophobic interaction.
研究领域:
食品科学
·
药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food Science and Human Wellness
·
2023
·
IF 7
Jinping Wang,Lingrong Wen,Yueming Jiang,Hong Zhu,Weizheng Sun,Guangyi Dai,Bao Yang
Soymilk is a natural nanocarrier. However, the performance of flavonoid-soymilk nano-complex remains unclear. In this work, icariin-soymilk nano-complexes (ISNCs) were successfully fabricated and characterized. The effects of high-pressure homogenization (HPH) treatment on structure and physicochemical properties of soymilk and nano-complexes were investigated. HPH treatment could significantly improve the surface hydrophobicity and interfacial activity of soymilk. The soymilk with HPH treatment could significantly improve the water solubility (20 folds), thermal stability and bioavailability of icariin. The highest encapsulation efficiency (93.28 %), loading capacity (39.09 µg/mg), ζ-potentia (absolute value, 31.20 mV) and bioavailability (72.14 %) were observed in HSI-200 (200 bar of homogenization pressure). While HSI-500 (500 bar of homogenization pressure) showed the smallest particle size (183.73 nm). ISNCs showed a rougher surface and an irregular lamellar structure with large amount of fine particles by using Cryo-SEM, suggesting that icariin was encapsulated in soymilk. These data supplied a novel strategy to improve the performance of icariin in functional foods.
研究领域:
食品科学
·
药理学
✓ 已验证
产品关联
DOI
高影响因子
Journal of Animal Science and Biotechnology
·
2026
·Vol. 17
·期 1
·109
·
IF 7.9
Zhang Jiaqi,Shi Xiaohan,Peng Siyi,Zhang Chi,Qiao Shiyan,Yu Haitao
Background While the livestock industry actively seeks alternatives to antibiotics, residual low-dose exposures continue to drive the spread of antibiotic resistance genes (ARGs). Icariin, a plant-derived compound, is recognized for improving poultry growth and immunity. However, it remains unclear how this compound influences the environmental persistence of ARGs, mobile genetic elements (MGEs), and horizontal gene transfer (HGT) during the vulnerable recovery phase after antibiotic withdrawal. Results We designed a two-phase feeding trial with laying hens, using longitudinal metagenomic sequencing to track post-withdrawal resistance dynamics. Following initial exposure to a low-dose antibiotic mixture that established a baseline of elevated resistance, hens received either a basal diet, an icariin-supplemented diet, or a copper sulfate-supplemented diet. The data indicate that icariin supplementation consistently reduced the burdens of both ARGs and MGEs. It also suppressed the potential for HGT and restricted the diversity of microbial hosts harboring these resistance elements. Conversely, copper sulfate—a traditional metal-based additive—exacerbated resistance risks by expanding both the abundance and the host range of ARGs and MGEs. Across all treatments, the population of Escherichia and the prevalent ARG subtype bacA correlated strongly with total resistance loads, tracking the overall resistome burden. Conclusions Compared to conventional copper sulfate treatments, icariin facilitates a safer ecological recovery in the poultry gut by actively lowering ARG and MGE reservoirs after antibiotic withdrawal. These genomic insights, combined with its known physiological benefits, support icariin as a sustainable feed additive. Furthermore, the Escherichia - bacA correlation provides a reliable, streamlined indicator for monitoring resistance risks in farm environments. However, as these findings rely on short-term fecal metagenomic tracking, further validation through multi-environment studies is warranted. Graphical
The alternative text for this image may have been generated using AI.
✓ 已验证
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2018
·
IF 3.997
Min Gong,Cheng Chi,Jingjing Ye,Meihong Liao,Wenqi Xie,Chengai Wu,Rui Shi,Liqun Zhang
Due to the significant role of the periosteum in bone regeneration, we hypothesised that using a specially engineered artificial periosteum could lead to an enhancement in osteogenesis in bone grafts. Herein, we describe our work aimed at fabricating an electrospun fibrous membrane as an artificial periosteum that exhibits flexibility, permeability and osteoinduction. This membrane was designed to cover the complex surface of bone grafts to facilitate and accelerate bone regeneration. The traditional Chinese medicine icariin (ICA) was subsequently introduced into poly (ε-caprolactone) (PCL) /gelatin nanofibers to fabricate an artificial periosteum for the first time. The effects of ICA content on morphology, physical properties, drug release profile, in vitro degradability, biocompatibility and osteogenic differentiation properties were investigated. The ICA-loaded electrospun membranes showed significant improvement in hydrophilicity, high mechanical strength, appropriate degradation rates and excellent biocompatibility. Furthermore, clear enhancement in alkaline phosphatase (ALP) activity, as well as an increase in osteocalcin (OCN) and type collagen I (COL I) expression in MC3T3-E1 cells were detected. Furthermore, we observed clear calcium deposition content in MC3T3-E1 cells cultured on ICA-loaded fibrous matrix. The membrane loaded with 0.05 wt.% ICA displayed properties contributing to cell attachment, proliferation and differentiation. These results indicate the huge potential of this ICA-loaded PCL/gelatin electrospun membrane as a biomimetic artificial periosteum to accelerate bone regeneration.
研究领域:
材料科学
·
生物材料
·
组织工程
·
再生医学
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DOI
PubMed
高影响因子
Microbial Cell Factories
·
2023
·Vol. 22
·期 1
·1-11
·
IF 6.4
Lin Yu,Chen Wen-wen,Ding Bo,Guo Man,Liang Meng,Pang Hao,Wei Yu-tuo,Huang Ri-bo,Du Li-qin
Background Icaritin is an aglycone of flavonoid glycosides from Herba Epimedii. It has good performance in the treatment of hepatocellular carcinoma in clinical trials. However, the natural icaritin content of Herba Epimedii is very low. At present, the icaritin is mainly prepared from flavonoid glycosides by α-L-rhamnosidases and β-glucosidases in two-step catalysis process. However, one-pot icaritin production required reported enzymes to be immobilized or bifunctional enzymes to hydrolyze substrate with long reaction time, which caused complicated operations and high costs. To improve the production efficiency and reduce costs, we explored α-L-rhamnosidase SPRHA2 and β-glucosidase PBGL to directly hydrolyze icariin to icaritin in one-pot, and developed the whole-cell catalytic method for efficient icaritin production.Results The SPRHA2 and PBGL were expressed in Escherichia coli, respectively. One-pot production of icaritin was achieved by co-catalysis of SPRHA2 and PBGL. Moreover, whole-cell catalysis was developed for icariin hydrolysis. The mixture of SPRHA2 cells and PBGL cells transformed 200 g/L icariin into 103.69 g/L icaritin (yield 95.23%) in 4 h in whole-cell catalysis under the optimized reaction conditions. In order to further increase the production efficiency and simplify operations, we also constructed recombinant E. coli strains that co-expressed SPRHA2 and PBGL. Crude icariin extracts were also efficiently hydrolyzed by the whole-cell catalytic system.Conclusion sCompared to previous reports on icaritin production, in this study, whole-cell catalysis showed higher production efficiency of icaritin. This study provides promising approach for industrial production of icaritin in the future.
研究领域:
生物技术
·
药学
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF APPLIED POLYMER SCIENCE
·
2024
·
IF 2.7
Zhenxu Wu,Guoqing Niu,Zongtai Xiong,Xinxiang Ding,Yongbo Li,Peibiao Zhang,Feng Wu
Deer bone in traditional Chinese medicine is valued for its unique biomimetic bone matrix components. Icariin (Ica), which is claimed by Chinese medicine as a bone-repairing agent, is also widely accepted. In this report, a novel Ica-encapsulated PLGA/nano deer bone meal (Ica@PLGA/nBM) biomimetic microsphere was fabricated. The Ica could be released from microspheres in a controlled manner. In vitro results showed that the microsphere had good biocompatibility due to the addition of nBM and the MC3T3-E1 cells could adhere to and grow well on the microspheres. Moreover, Ica and nBM in microspheres could synergically promote the ALP activity of MC3T3-E1 cells significantly ( p < 0.05), which indicated the acceleration of osteogenic differentiation. The RT-PCR results showed that the expression levels of bone matrix proteins (Col1 & OPN) were enhanced by the composite ( p < 0.05). In addition, Ica and nBM in microspheres also obviously promoted the expression of RUNX2 and BMP-2, respectively ( p < 0.05). The in vivo results demonstrated the effective promotion of Ica@PLGA/nBM on complete bony connection to cover the defect site and the bone defect repair. And the Ica(M)@PLGA/nBM microspheres provided the best repair results. All the results confirmed that the Ica@PLGA/nBM composite biomimetic microsphere has the potential for clinical application.
研究领域:
材料科学
·
生物医学工程
·
药理学
·
组织工程
✓ 已验证
DOI
高影响因子
ACS Applied Materials & Interfaces
·
2025
·
IF 8.2
Shilong Fan,Ning Ma,Jiahui Li,Bingqing Wang,Yue Zhao,Yinlian Yao,Xingxing Chai,Zhikun Zhou
Chronic inflammatory liver conditions, such as nonalcoholic fatty liver disease (NAFLD), are frequently exacerbated by oxidative stress, rendering the neutralization of reactive oxygen species (ROS) crucial for their amelioration. Oral administration of nanoparticles (NPs) presents an optimal strategy for NAFLD management due to its convenience. This research aimed to overcome the poor water solubility and low bioavailability of icariin (ICA) by engineering an oral nanosystem, ICA-loaded poly(lactic-co-glycolic acid)-poly(ethylene glycol) (PLGA) NPs with chitosan (CS) and mannose surface modification (ICA-NPs), to augment ICA’s antioxidant potency against NAFLD. Methods involved comprehensive in vitro characterization of ICA-NPs (including dispersibility, biocompatibility, HepG2 targeting, and ROS scavenging capabilities) and in vivo studies in high-fat diet (HFD)-induced NAFLD mice, assessing liver accumulation, ROS scavenging, and antiobesity effects across multiple experimental groups. Results demonstrated that this targeted oral NP system significantly amplified ICA’s therapeutic impact, leading to substantial reductions in body weight, diminished white adipose tissue accumulation, decreased hepatic lipid content, improved hepatic function, and a notable suppression of ROS in the livers of NAFLD-afflicted mice. In conclusion, by harnessing the precision of targeted delivery, this oral nanosystem not only enhances ICA’s therapeutic efficacy but also establishes a safe and effective platform for the oral administration of herbal remedies for liver conditions, suggesting a promising avenue for advancing herbal medicine in liver disease treatment.
研究领域:
纳米医学
·
肝病学
·
药剂学
·
氧化应激与抗氧化治疗
·
中药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）