Microorganisms
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2022
·Vol. 10
·期 3
·628
·
IF 4.926
Guosi Li,Fucheng Zhu,Peipei Wei,Hailong Xue,Naidong Chen,Baowei Lu,Hui Deng,Cunwu Chen,Xinjian Yin
Hyperoside (quercetin 3-O-galactoside) exhibits many biological functions, along with higher bioactivities than quercetin. In this study, three UDP-dependent glycosyltransferases (UGTs) were screened for efficient hyperoside synthesis from quercetin. The highest hyperoside production of 58.5 mg·L−1was obtained in a recombinantEscherichia colico-expressing UGT fromPetunia hybrida(PhUGT) and UDP-glucose epimerase (GalE, a key enzyme catalyzing the conversion of UDP-glucose to UDP-galactose) fromE. coli. When additional enzymes (phosphoglucomutase (Pgm) and UDP-glucose pyrophosphorylase (GalU)) were introduced into the recombinantE. coli, the increased flux toward UDP-glucose synthesis led to enhanced UDP-galactose-derived hyperoside synthesis. The efficiency of the recombinant strain was further improved by increasing the copy number of the PhUGT, which is a limiting step in the bioconversion. Through the optimization of the fermentation conditions, the production of hyperoside increased from 245.6 to 411.2 mg·L−1. The production was also conducted using a substrate-fed batch fermentation, and the maximal hyperoside production was 831.6 mg·L−1, with a molar conversion ratio of 90.2% and a specific productivity of 27.7 mg·L−1·h−1after 30 h of fermentation. The efficient hyperoside synthesis pathway described here can be used widely for the glycosylation of other flavonoids and bioactive substances.Keywords:hyperoside;quercetin;UDP-dependent glycosyltransferase;UDP-glucose;metabolic engineering
研究领域:
生物技术
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代谢工程
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生物化学
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高影响因子
Frontiers in Cellular and Infection Microbiology
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2026
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IF 4.8
Li Yin,Lin Xu,Yu-nan Shan,Zhilin He,Yanbin Li,Wei Chen
Background Ulcerative colitis (UC) is subtype of inflammatory bowel disease that is frequently comorbid with anxiety disorders. However, effective dual-targeting therapies are still lacking. Hyperoside (HYP), a natural flavonoid, exhibits anti-inflammatory and neuroprotective properties, yet its potential therapeutic effects on UC and associated anxiety, as well as the underlying mechanisms, remain largely unexplored. Methods A murine model of DSS-induced colitis was established and treated with HYP. Disease activity was assessed through body weight, colon length, and histopathology. Anxiety-like behaviors were evaluated using open field and elevated plus maze tests. Neuroinflammation was examined through immunohistochemistry of BDNF expression and microglial activation. Gut microbiota composition was profiled by metagenomic sequencing, and metabolomic profiling was conducted using the Q300 Kit. Network pharmacology and molecular docking were employed to predict signaling pathways, which were further validated by Western blotting. Additionally, antibiotic depletion experiments were conducted to determine microbiota dependency. Results HYP administration significantly ameliorated DSS-induced colitis, as evidenced by attenuated weight loss, restored colon length, and improved histopathology. It suppressed pro-inflammatory cytokines (TNF-α, IL-6, IL-1β) and restored intestinal barrier integrity by upregulating Mucin-2 and ZO-1. Furthermore, HYP also alleviated anxiety-like behaviors and mitigated neuroinflammation by increasing BDNF levels and suppressing microglial activation. HYP treatment also restored gut microbial homeostasis, enriching beneficial bacteria such as Enterobacter ludwigii while reducing the abundance of Enterobacter hormaechei, Escherichia coli , and Acinetobacter baumannii . Metabolomic analysis revealed that HYP significantly promoted arginine biosynthesis. Network pharmacology and molecular docking identified the MAPK, PI3K-Akt, and NF-κB pathways as potential targets, with HYP showing strong binding affinity to MAPK3, AKT1, and NFκB1. Importantly, the therapeutic effects of HYP were abolished in microbiota-depleted mice. Conclusion Our findings demonstrate that HYP effectively alleviates DSS-induced colitis and comorbid anxiety-like behaviors. Its efficacy is dependent on the gut microbiota and is associated with the restoration of microbial homeostasis, enhancement of arginine metabolism, and modulation of the MAPK/PI3K-Akt/NF-κB signaling pathways. HYP represents a promising microbiota-targeting therapeutic candidate for UC and its neuropsychiatric comorbidities.
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MICROCHEMICAL JOURNAL
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2025
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IF 5.1
Zheng Li,Yuting Jin,Jiaming Deng,Peirong Ma,Huiying Jin,Yanling Zhang,Alideertu Dong,Munkhjargal Burenjargal
In recent years, natural deep eutectic solvents prepared by natural compounds and natural primary metabolites have been more favored, which are environmentally friendly, low toxicity and easy to biodegrade. In this study, twenty different types of natural deep eutectic solvents (NADES) were prepared by selecting five common hydrogen bond acceptors and nine common hydrogen bond donors using different molar ratios, and then were applied with ultrasound-assisted extraction (UAE) to extract hyperoside, an index component in Cuscutae semen . The results showed that the optimal extraction conditions of hyperoside from the natural deep eutectic solvent prepared by choline chloride and lactic acid (molar ratio 1:2) were as follows: 65℃, 38 min, amount of added water 16 %, liquid to solid ratio 51 mL·g −1 , and the actual yield was 6.766 mg·g −1 . Antioxidant assay proved that NADES extract has antioxidant capacity. The results of this paper show that ultrasound-assisted natural deep eutectic solvent can effectively extract hyperoside from Cuscutae semen , which lays a foundation for the green and efficient extraction of bioactive components in natural plants and in-depth research and development.
研究领域:
植物化学
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天然产物开发
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药用植物研究
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DOI
高影响因子
Drug Delivery and Translational Research
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2023
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IF 5.4
Jin Xingcheng,Xia Xiaoli,Li Jiaying,Adu-Frimpong Michael,Wang Xiaowen,Wang Qilong,Wu Huaxiao,Yu Qingtong,Ji Hao,Toreniyazov Elmurat,Cao Xia,Yu Jiangnan,Xu Ximing
At present, ulcerative colitis (UC) has become a global disease due to its high incidence. Hyperoside (HYP) is a naturally occurring flavonoid compound with many pharmacological effects. This study aimed to develop HYP-loaded mixed micelles (HYP-M) to improve oral bioavailability of HYP and to evaluate its therapeutic effect on UC. The prepared HYP-M exhibited stable physical and chemical properties, smaller particle size (PS) (21.48 ± 1.37 nm), good polydispersity index (PDI = 0.178 ± 0.013), negative Zeta potential (ZP) (− 20.00 ± 0.48 mV) and high entrapment rate (EE) (89.59 ± 2.03%). In vitro release and in vivo pharmacokinetic results showed that HYP-M significantly increased the releasing rate of HYP, wherein its oral bioavailability was 4.15 times higher than that of free HYP. In addition, HYP-M was more effective in the treatment of UC than free HYP. In conclusion, HYP-M could serve as a novel approach to improve bioavailability and increase anti-UC activity of HYP. Graphical abstract
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MOLECULAR AND CELLULAR BIOCHEMISTRY
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2018
·Vol. 453
·期 1
·179-186
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IF 2.561
Liu Fang,Zhao YuHua,Lu JieMin,Chen ShuangHui,Zhang XinGuang,Mao WenWei
Mycoplasma pneumoniae pneumonia (MPP) is the most common respiratory infection in young children and its incidence has increased worldwide. In this study, high expression of chemokine ligand 5 (CCL5) was observed in the serum of MPP patients, and its expression was positively correlated to DNA of M. pneumoniae (MP-DNA). In vitro, M. pneumoniae (MP) infection to A549 cells induced the expression of CCL5, chemokines receptor 4 (CCR4), nuclear factor-κB (NF-κB) nuclear protein, and phosphorylation of NF-κB-p65 (p-NF-κB-p65), whereas NF-κB cytoplasmic protein was decreased. On the contrary, treatment of hyperoside counteracted the induction of MP infection and promoted the proliferation of MP-infected A549 cells. Similarly, MP-induced IL-8 and TNF-α production was also markedly reduced by hyperoside. And CCR4 inhibitor AZD2098 had a better effect than hyperoside. In addition, CCL5 recombinant protein inhibited the effect of hyperoside to promote IL-8 and TNF-α production and CCR4 expression. These results indicated that CCL5 may be involved in the progression of MPP, and hyperoside was beneficial for MPP probably through CCL5–CCR4 interactions, which may provide a potential effective therapy for MPP.
研究领域:
传染病学
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肺科学
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免疫学
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药理学
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Results in Chemistry
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2026
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IF 4.2
Mengqi Wang,Zibo Wu
In this work, we found the flavonoid molecules: quercitrin and hyperoside have potentiality as ultraviolet (UV) filters for the first time. The steady state spectra and time-dependent density functional theory (TDDFT) were used to prove the excited state intramolecular proton transfer (ESIPT) of the non-radiative relaxation. They are excellent potential UVA sunscreens, and they can also provide some UVB protection. We demonstrated the deactivation via ESIPT can be facilitated by the hydrogen bond strengthening in S 1 . In particular, when UV excited, the enol conformation can cross a small barrier to the keto conformation, then the proton transfer process can consumes energy through non-radiative path, and the other small part dissipates through the fluorescence path. Quercetin and hyperoside with a substituent caused 10 nm wavelength change, which opens up a way for the design of new broad-spectrum sunscreens: the adjustable absorption wavelength of sunscreen molecules can be achieved by adjusting the position and number of substituents.
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PHYTOTHERAPY RESEARCH
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2023
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IF 7.2
Shanshan Wei,Wanjun Ma,Chuanhao Jiang,Jiaqin Liu,Jian Liu,Bikui Zhang,Wenqun Li
Clinical application of doxorubicin (Dox) in cancer chemotherapy is limited by its cardiotoxicity. Present study aimed to demonstrate the effect and mechanism of hyperoside in Dox-induced cardiotoxicity. C57BL/6 mice were injected with 12 mg/kg of Dox, and 1 μM Dox was exposed to primary cardiomyocytes. Cardiac function was evaluated by echocardiographic and myocardial enzyme levels. Cardiomyocyts apoptosis was analyzed by TUNEL staining and flow cytometry. Network pharmacology and molecular docking were utilized to explore potential targets of hyperoside. Protein expressions were detected by western blot and enzyme activities were determined by colorimetry. Cardiac dysfunction and cardiomyocyte apoptosis induced by Dox were attenuated by hyperoside. Mechanism of hyperoside was mainly related to “oxidative stress” pathway. Hyperoside exhibited strong binding activities with nicotinamide adenine dinucleotide phosphate (NADPH) oxidases (NOXs, the main source of ROS in cardiomyocytes) and cyclooxygenases (COXs). Experiments proved that hyperoside suppressed the ROS generation and the elevated activities of NOXs and COXs induced by Dox. Dox also triggered the activation of NLRP3 inflammasome, which was reversed by hyperoside. Hyperoside bound to NOXs and COXs, which prevents Dox-induced cardiotoxicity by inhibiting NOXs/ROS/NLRP3 inflammasome signaling pathway. Hyperoside holds promise as a therapeutic strategy for Dox-induced cardiotoxicity.
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Food & Function
·
2023
·Vol. 14
·期 10
·4763-4776
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IF 6.1
Xinyue Zhang,Dan Li,Kexin Wang,Jiao Xie,Yaojie Liu,Tianxin Wang,Suwen Liu,Qun Huang,Qingbin Guo,Hao Wang
Hyperoside, the main component of many anti-obesity plants, might exhibit a lipase inhibition effect to reduce fat accumulation. The anti-obesity effect of hyperoside was investigated by studying its inhibitory effect and mechanism on pancreatic lipase in vitro and evaluating its ability to reduce lipid accumulation in vivo. Hyperoside is a mixed-type inhibitor of lipase with an IC50 of 0.67 ± 0.02 mmol L−in vitro. Hyperoside changed the secondary conformation of lipase, increased the α-helix content, and changed the microenvironment of lipase through static quenching. The interaction between hyperoside and lipase results from a strong binding spontaneous exothermic reaction, mainly through hydrogen bonding, van der Waals force and electrostatic force. Hyperoside protected hepatic lipid accumulation and adipose tissue hypertrophy and reduced the expression of inflammatory factors in high-fat diet-induced rats. Moreover, hyperoside had a good inhibitory effect on lipase activity in serum and increased fecal fat excretion, thereby reducing lipid absorption in vivo. This study provides theoretical support for the research and development of hyperoside in fat-reducing functional foods.
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FOOD CHEMISTRY
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2021
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IF 7.514
Di Wu,Lan Tang,Ran Duan,Xia Hu,Fang Geng,Yin Zhang,Lianxin Peng,Hui Li
Hyperoside (HYP) is an important natural product that is widely distributed in fruits and whole grasses of various plants. It is also used by consumers as a healthy ingredient. This work explored the interaction mechanisms between HYP and two main soy proteins, namely, β-conglycinin (7S) and glycinin (11S), using computational simulation and multi-spectroscopic technology. In this study, the docking and dynamic simulation showed that HYP was stable in the hydrophobic pockets of the proteins. The conformation and microenvironment of 7S/11S also changed after binding to HYP. The binding of HYP to 7S/11S was a state quenching with a good affinity at 4 °C. This result was determined from the binding constant values of (1.995 ± 0.170) × 10 7 M −1 and (2.951 ± 0.109) × 10 7 M −1 , respectively. The 7S/11S-HYP complex delineated here will provide a novel idea to construct an embedding and delivery system in improving the benefits of HYP for the development of high value-added food products.
研究领域:
食品科学
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生物化学
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分子生物学
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计算化学
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高影响因子
Pharmacognosy Magazine
·
2025
·
IF 0.9
Qing Liu,Ying Lan,Zhe Bai
BackgroundHyperoside is a potential liver cell and mitochondrial protector, but there is no evidence to suggest that hyperoside can effectively treat doxorubicin (DOX) related liver toxicity.PurposeThis study aims to determine the role of hyperoside in DOX related liver toxicity and liver cell damage in vivo and in vitro.MethodsA mouse model of liver toxicity was induced by intraperitoneal injection of DOX, and hyperoside was administered orally for treatment. During this period, the weight and food intake of the mice were recorded. The morphology of mouse liver tissue was observed by hematoxylin and eosin staining. Oxidative stress and inflammatory status in mice were observed through serum inflammatory factors and liver oxidative stress markers. Mitochondrial damage is determined by the degree of mitochondrial DNA damage. Western blotting and reverse transcription polymerase chain reaction (RT-PCR) were used to detect the expression of pyroptosis and genes in the liver and liver cells.ResultsHyperoside can effectively treat DOX-induced oxidative stress and inflammatory status, liver function damage, and hepatocyte necrosis in mice. Further research suggests that the beneficial effect of hyperoside is achieved by inhibiting mitochondrial DNA damage in liver cells.ConclusionThis study indicates that hyperoside improves DOX-induced liver toxicity by inhibiting mitochondrial DNA damage.
研究领域:
药理学
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肝脏病学
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分子生物学
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LIFE SCIENCES
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2020
·
IF 3.647
Aiwu Wei,Yanli Song,Tingting Ni,Huidongzi Xiao,Yanrong Wan,Xingxing Ren,Huijuan Li,Guangli Xu
Aims Recurrent pregnancy loss (RPL) is one of the most common obstetrical diseases, which is a manifestation of antiphospholipid syndrome (APS) with no effective therapy methods. Autophagy and inflammatory responses both play an important role in the pathogenesis of RPL and hyperoside has been demonstrated to have multifarious bioactivities including enhancing autophagy and anti-inflammation. This study aims to investigate the effect of hyperoside on anticardiolipin (aCL)-IgG fractions-induced pregnancy loss. Main methods In the present study, the effect of hyperoside was evaluated in a rat model of pregnancy loss induced by aCL-IgG fractions isolated from serum of APS patients. The fetuses were counted and the placentas were weighted and the protein expressions of inflammation and autophagy were measured by western blot analysis. Key findings Treatment with hyperoside (40 mg/kg) improved pregnancy outcome manifest as increasing the weight of fetuses and decreasing the fetal resorption rate. In addition, hyperoside treatment downregulated the expressions of phosphorylated mammalian target of rapamycin (mTOR), phosphorylated p70S6 Kinase (S6K) and inhibited the expressions of Toll-like receptor 4 (TLR4), myeloid differentiation factor 88 (MyD88) and NF-kB p-p65 in pregnancy loss animal models. Significance Hyperoside attenuated pregnancy loss through regulating mTOR/S6K and TLR4/MyD88/NF-kB signaling pathways, which may provide a potential drug candidate for recurrent pregnancy loss therapy.
研究领域:
妇产科学
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药理学
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免疫学
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PubMed
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Frontiers in Pharmacology
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2020
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IF 4.225
Wei Aiwu,Xiao Huidongzi,Xu Guangli,Yu Xile,Guo Jingjing,Jing Zhuqing,Shi Shaoqi,Song Yanli
Anticardiolipin antibody (aCL), an important characterization of antiphospholipid syndrome, shows an intense association with vascular endothelial injury. Hyperoside is a flavonoid extracted from medicinal plants traditionally used in Chinese medicines, displaying anti-inflammatory, anti-cancer, and anti-oxidative properties in various diseases. Recent studies have shifted the focus on the protective effects of hyperoside on vascular endothelial injury. However, little is known about the mechanisms involved. In the present study, we investigated the effect of hyperoside on aCL-induced injury of human umbilical vein endothelial cells (HUVECs) in vitro. Our data illustrated that aCL induced HUVEC injury via inhibiting autophagy. Hyperoside reduced aCL-induced secretion of proinflammatory cytokines IL-1β and IL-8 and endothelial adhesion cytokines TF, ICAM1, and VCAM1 in HUVECs. Additionally, hyperoside activated autophagy and suppressed the mTOR/S6K and TLR4/Myd88/NF-κB signaling transduction pathways in aCL-induced HUVECs. To the best of our knowledge, this is the first study to investigate the effect of hyperoside on aCL-induced injury, as well as offer insights into the involved mechanisms, which is of great significance for the treatment of antiphospholipid syndrome.
研究领域:
免疫学
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药理学
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细胞生物学
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血管生物学
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