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JOURNAL OF CONTROLLED RELEASE · 2025 · IF 11.5

Gastric-mucus penetrating and responsive microgels for alleviating Helicobacter pylori-induced gastritis

Xing Li,Jipeng Zhang,Xiangyu Liu,Zijian Wu,Zhipeng Yu,Wen Zhang,Yuanzhi Wang,Zekun Li,Martien A. Cohen Stuart,Leonard M.C. Sagis,Minchun Lv,Jie Xiao,Yuan Li

Helicobacter pylori ( H. pylori ) is a prevalent global pathogen responsible for gastritis and the potential development of gastric cancer. Sulforaphane (SFN), a foodborne compound, exhibits notable antibiotic properties against H. pylori . However, its utility is limited by poor stability and susceptibility to environmental degradation. Here, we developed a gastric-responsive-release microgel for delivering anti- H. pylori SFN. The microgels were prepared by cross-linking α-lactalbumin nanotubes then coated with chitosan (CTS-MGs). SFN was loaded into microgels with a loading rate of 10.73 ± 0.25 %. The CTS-MG showed a strong adhesion to the gastric mucosa, prolonging gastric retention for up to 24 h and responsively releasing SFN in the stomach. Furthermore, CTS-MG/SFN dissociated and released nanotubes/SFN, which could penetrate into the gastric mucus layer and arrive at the deepest mucus sites where most H. pylori were colonized. Our results revealed that CTS-MG/SFN displayed an obvious inhibitory effect against H. pylori . The oral administration of CTS-MG/SFN in H. pylori -infected mice effectively alleviated H. pylori -induced gastritis and modulated gastric microbiota homeostasis. This work demonstrated high potential of CTS-MG microgels for gastric-targeted and oral delivery of antibiotic natural compounds against H. pylori infection.

CAS / MDL: 4478-93-7 9005-65-6
研究领域: 药学 · 微生物学 · 生物材料学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Frontiers · 2021 ·Vol. 2 ·期 3 ·305-315 · IF 0

Effects of complex extracts of traditional Chinese herbs on gastric mucosal injury in rats and potential underlying mechanism

Erdong Yuan,Liangyun Liu,Min Huang,Bo Chang,Chunli Qi,Na Gou,Jiaoyan Ren

Five complex extracts (CEs) of seven Chinese herbs ( Astragalus , Poria cocos , Alpinia officinarum Hance , Radix Puerariae , Ginseng , Licorice , Hericium erinaceus ) were prepared by hot water extraction and evaluated for their effect on gastric ulcer in rats. In rats with acetic acid-induced chronic gastric ulcer, gross and microscopic appearance showed that gastric mucosal injury index and lesion inhibition rate were improved after CEs gavage for 21 days. Pretreatment with CEs for 21 days in rats with acute gastric ulcer could also improve the gastric mucosal injury by ethanol. CE1, CE4, and CE5 showed more obvious effect in two models. The cell experiments results showed that CE1, CE4, and CE5 effectively inhibited Wnt signaling activity. Thus, they could protect gastric mucosa through inhibiting Wnt signaling pathway. These results indicated that CE1, CE4, and CE5 had significant protective effects on gastric mucosal injury by inhibiting Wnt signalling pathway and could be developed into safe functional products.

CAS / MDL: 30525-89-4 298-93-1
研究领域: 药理学 · 胃肠病学 · 中医
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FOOD CHEMISTRY · 2021 · IF 7.514

Structural characterization of two Hericium erinaceus polysaccharides and their protective effects on the alcohol-induced gastric mucosal injury

Chuanli Hou,Liangyun Liu,Jiaoyan Ren,Min Huang,Erdong Yuan

Hericium erinaceus , a traditional edible mushroom, is known as a medicine food homology to ameliorate gastrointestinal diseases. However, the relationship between the structural characteristics of Hericium erinaceus and its stomach-protecting activity remains unclear. Here, the structural properties of two polysaccharides from Hericium erinaceus, mycelium polysaccharide (HMP) and fruiting body polysaccharide (HFP) were investigated by spectral approaches. The results showed that the distribution of HMP was more uniform compared to HFP. Both HMP and HFP have triple helix structures, but the HMP conformation showed greater stability. Subsequently, the preventive effect of HMP and HFP on ethanol-induced gastric mucosal injury was also evaluated in rats and GES-1 cells, and it showed that both HMP and HFP had significant protective activity against gastric mucosal injury, but HMP showed better activity than HFP. These results suggested that conformational stability polysaccharide in Hericium erinaceus is more related to its gastric-protecting activity.

CAS / MDL: 30525-89-4 298-93-1
研究领域: 食品科学 · 生物化学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Chinese Journal of Natural Medicines · 2025 · IF 4.9

Capsaicin (CAP) exerts a protective effect against ethanol-induced oxidative gastric mucosal injury by modulating the chemokine receptor 4 (CCR4)/Src/p47phox signaling pathway both in vitro and in vivo

Zhiru Yang,Haolin Guo,Pengfei Zhang,Kairui Liu,Junli Ba,Xue Bai,Shiti Shama,Bo Zhang,Xiaoning Gao,Jun Kang

Ethanol (EtOH) is a common trigger for gastric mucosal diseases, and mitigating oxidative stress is essential for attenuating gastric mucosal damage. Capsaicin (CAP) has been identified as a potential agent to counteract oxidative damage in the gastric mucosa; however, its precise mechanism remains unclear. This study demonstrates that CAP alleviates EtOH-induced gastric mucosal injuries through two primary pathways: by suppressing the chemokine receptor 4 (CCR4)/Src/p47phox axis, thereby reducing oxidative stress, and by inhibiting the phosphorylation and nuclear translocation of nuclear factor- κ B p65 (NF- κ B) p65, resulting in diminished inflammatory responses. These findings elucidate the mechanistic pathways of CAP and provide a theoretical foundation for its potential therapeutic application in the treatment of gastric mucosal injuries.

CAS / MDL: 64-17-5
研究领域: 药理学 · 胃肠病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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PHYTOMEDICINE · 2025 · IF 8.3

Glycyrrhetinic acid ameliorates gastric mucosal injury by modulating gut microbiota and its metabolites via Thbs1/PI3K-Akt/p53 pathway

Zheng-Meng Jiang,Zhi-Yue Fang,Xing Yang,Xing-Xing Ji,Yuan-Yuan Zhao,Bin-Yan Lin,Ze-Bin Weng,E-Hu Liu

Background Dysbiosis of the gut microbiota is pivotal in the development of gastric mucosa injury (GMI). Glycyrrhetinic acid (GA) is a bioactive triterpenoid compound abundantly present in licorice roots. Although GA's potential in mitigating GMI is recognized, its precise mechanism remains elusive, particularly concerning the role of gut microbiota. Purpose This study aimed to explore the protective effects and mechanisms of GA in preventing HCl/ethanol-induced GMI in rats. Results This study demonstrated the protective effects of GA on gastric mucosa, evidenced by enhanced morphology and structure as revealed through H&E staining. Utilizing fecal microbiota transplantation, GA was found to significantly mitigate oxidative damage, inflammation, and expression of apoptosis-related genes in GMI rats by a gut microbiota-dependent mechanism. 16S rRNA sequencing and metabolomics profiling revealed that GA ameliorated HCl/ethanol-triggered intestinal dysbiosis and imbalances in sphingolipid, arginine, and tryptophan metabolism. By promoting the prevalence of Bifidobacterium longum subsp. infantis ( B. infantis ) in the gut microbiota, GA improved metabolic disturbances linked to injury. Furthermore, its action mechanism was related to the inhibition of the Thbs1/PI3K-Akt/p53 signaling pathway. Conclusion The administration of GA improves GMI by mitigating intestinal dysbiosis and fostering colonization of B. infantis . GA offers therapeutic potential for GMI by modulating the Thbs1/PI3K-Akt/p53 pathway, thus alleviating inflammatory responses associated with gut microbiota imbalance.

研究领域: 药理学 · 微生物学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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Food Bioengineering · 2024 ·Vol. 3 ·期 2 ·172-188 · IF 0

Microencapsulation improves the effects of octacosanol to ameliorate alcoholic liver injury

Xiangchun Meng,Yishu Sun,Tao Xu,Lihua Tang,Yaning Chang,Yingjun Zhou

Octacosanol is a plant natural product with the potential to ameliorate alcoholic liver injury. However, its poor solubility limits its application in the food industry. This study first verified that octacosanol has a favorable effect on acute and subchronic alcoholic liver injury in mice by protecting the gastric mucosa and ameliorating disease levels. Additionally, octacosanol microcapsules were prepared under the optimal drying conditions of the feed flow rate of 400 mL/h and drying temperature of 180°C to improve the ameliorative effects of octacosanol, with moisture content, water activity, dispersibility, and solubility of 1.53%, 0.16%, 89.84%, and 95.30%, respectively. The microcapsules had a spherical structure, and the droplet sizes after redissolution ranged from 0.061 to 4.63 µm. Instrumental measurements and simulated digestion experiments have shown that microencapsulation enhanced the solubility and thermal stability of octacosanol, with 90.88% of the octacosanol being continuously released. As expected, microencapsulation significantly enhanced the effect of octacosanol in ameliorating alcoholic liver injury by determining the disease index in the mice model. This study demonstrated the beneficial effects of octacosanol on alcoholic liver injury and explored a viable method to improve its solubility and bioaccessibility, thereby enhancing its therapeutic efficacy for the treatment of alcoholic liver injury.

研究领域: 食品科学 · 药理学 · 生物医学工程
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Nature Communications · 2017 ·Vol. 8 ·期 1 ·1-12 · IF 12.124

In situ targeted MRI detection of Helicobacter pylori with stable magnetic graphitic nanocapsules

Li Yunjie,Hu Xiaoxiao,Ding Ding,Zou Yuxiu,Xu Yiting,Wang Xuewei,Zhang Yin,Chen Long,Chen Zhuo,Tan Weihong

Helicobacter pylori infection is implicated in the aetiology of many diseases. Despite numerous studies, a painless, fast and direct method for the in situ detection of H. pylori remains a challenge, mainly due to the strong acidic/enzymatic environment of the gastric mucosa. Herein, we report the use of stable magnetic graphitic nanocapsules (MGNs), for in situ targeted magnetic resonance imaging (MRI) detection of H. pylori . Several layers of graphene as the shell effectively protect the magnetic core from corrosion while retaining the superior contrast effect for MRI in the gastric environment. Boronic-polyethylene glycol molecules were synthesized and modified on the MGN surface for targeted MRI detection. In a mouse model of H. pylori -induced infection, H. pylori was specifically detected through both T 2 -weighted MR imaging and Raman gastric mucosa imaging using functionalized MGNs. These results indicated that enhancement of MRI using MGNs may be a promising diagnostic and bioimaging platform for very harsh conditions.

研究领域: 医学影像学 · 生物材料学 · 微生物学
✓ 已验证 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2024 · IF 6.6

Self-Nanoemulsifying Drug Delivery System of Morin: A New Approach for Combating Acute Alcohol Intoxication

Jiamin Mao,Xiaoyuan Liu,Lie Zhang,Yu Chen,Shiyu Zhou,Yujiao Liu,Jing Ye,Xiaohong Xu,Quan Zhang

Purpose Acute alcohol intoxication (AAI) is a life-threatening medical condition resulting from excessive alcohol consumption. Our research revealed the potential of morin (MOR) in treating AAI. However, MOR’s effectiveness against AAI was hindered by its poor solubility in water and low bioavailability. In this study, our aim was to develop a self-nanoemulsifying drug delivery system (SNEDDS) to enhance MOR’s solubility and bioavailability, evaluate its anti-AAI effects, and investigate the underlying mechanism.Methods The composition of MOR-loaded self-nanoemulsifying drug delivery system (MOR-SNEDDS) was determined by constructing pseudo-ternary phase diagrams, and its formulation proportion was optimized using the Box-Behnken design. Following characterization of MOR-SNEDDS, we investigated its pharmacokinetics and biodistribution in healthy animals. Additionally, we assessed the anti-AAI effects and gastric mucosal protection of MOR-SNEDDS in an AAI mice model, exploring potential mechanisms.Results After breaking down into tiny droplets, the optimized mixture of MOR-SNEDDS showed small droplet size on average, even distribution, strong stability, and permeability. Pharmacokinetic studies indicated that MOR-SNEDDS, compared to a MOR suspension, increased the area under the plasma concentration-time curve (AUC0-t) by 10.43 times. Additionally, studies on how drugs move and are distributed in the body showed that MOR-SNEDDS had an advantage in passively targeting the liver. Moreover, in a mouse model for alcohol addiction, MOR not only decreased alcohol levels by boosting the activity of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) in the stomach and liver, which counteracted the loss of righting reflex (LORR), but also reduced alcohol-induced damage to the stomach lining by lowering malondialdehyde (MDA) levels and increasing superoxide dismutase (SOD) levels. Furthermore, MOR-SNEDDS notably amplified these effects.Conclusion MOR exhibits significant potential as a new medication for treating AAI, and utilizing MOR-SNEDDS with high oral bioavailability represents a promising new strategy in combating AAI.

CAS / MDL: 61791-12-6 61788-85-0
研究领域: 药理学 · 生物医学工程 · 毒理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Frontiers in Microbiology · 2024 · IF 4

6-gingerol and its derivatives inhibit Helicobacter pylori-induced gastric mucosal inflammation and improve gastrin and somatostatin secretion

Qian Jiali,Li Zhennan,Wang Jinhui,Lin Yuxian,Yu Yingcong

The resistance of Helicobacter pylori (H. pylori) has increased in recent years, prompting a trend in the research and development of new drugs. In our study, three derivatives (JF-1, JF-2, and JF-3) were synthesized using 6-gingerol as the main component, while JF-4, containing both 6-gingerol and 6-shogaol as the main components, was extracted from dried ginger. The minimum inhibitory concentrations (MICs), determined using the ratio dilution method, were 80 μg/mL for JF-1, 40 μg/mL for JF-2, 30 μg/mL for JF-3, 40 μg/mL for JF-4, 60 μg/mL for 6-gingerol standard (SS), and 0.03 μg/mL for amoxicillin (AMX). After treating H. pylori-infected mice, the inflammation of the gastric mucosa was suppressed. The eradication rate of H. pylori was 16.7% of JF-3 low-dose treatment (LDT), 25.0% of JF-3 high-dose treatment (HDT), 16.7% of JF-4 LDT, 16.7% of JF-4 HDT, 30% of SS LDT, 50% of SS HDT, and 36.4% of the positive control group (PCG). The levels of gastrin, somatostatin (SST), IFN-γ, IL-4, and IL-8 were significantly recovered in the JF-3 and JF-4 administration groups, but the effect was stronger in the high-dose group. These results demonstrate that 6-gingerol and its derivatives have significant anti-Helicobacter pylori effects and are promising potential treatments for H. pylori infection.

研究领域: 药理学 · 微生物学 · 胃肠病学 · 化学
✓ 已验证 DOI PubMed 高影响因子
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Plants-Basel · 2025 ·Vol. 14 ·期 24 ·3718 · IF 4.1

Quality Evaluation of Dendrobium huoshanense Under Different Cultivation Modes and Its Protective Effect on Ethanol-Induced Injury in GES-1 Cells

Xinxin Li,Ziting Zhu,Jing Wu,Nianjun Yu,Huiqun Xie,Lan Han,Daiyin Peng

Dendrobium huoshanense , a rare and endangered medicinal orchid species endemic to Huoshan County, Anhui Province, faces a severe limit of wild resources. Its medicinal efficacy derives from unique chemical constituents, which vary significantly across cultivation modes. We systematically compared sensory properties and nutritional constituents (polysaccharides, flavonoids, alkaloids, bibenzyls, minerals, and free amino acids) between D. huoshanense in three cultivation modes—greenhouse cultivation, understory gravel cultivation, and wild-simulated cultivation. Additionally, the gastroprotective effects of wild-simulated cultivated D. huoshanense on gastric mucosal epithelial cells were evaluated. Results demonstrated that wild-simulated cultivation yielded significantly higher levels of nutritional constituents compared to gravel and greenhouse cultivation. Furthermore, wild-simulated cultivated D. huoshanense exhibited notable protective effects against gastric mucosal epithelial cell damage. This study not only elucidates the influence of cultivation modes on the chemical profile of D. huoshanense but also provides scientific evidence supporting its gastric protective properties, offering a foundation for its sustainable utilization and quality-oriented cultivation.

CAS / MDL: 497-19-8 76-60-8
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Magnetic-navigable silk fibroin microneedles for oral drug delivery: Ensuring long-lasting helicobacter pylori eradication and rapid hemostasis in the stomach

Haoyu Qiu,Lisha Gong,Paul Slezak,Shixiong He,Fei Lu,Kun Yu,Jing Xie,Zhen Geng,Enling Hu,Zhihang Zhou,Guangqian Lan,Ruiqi Xie

The Helicobacter pylori infection in the stomach is the key reason for gastric mucosal bleeding. Eliminating gastric Helicobacter pylori by oral treatment remains difficult due to the presence of the gastric mucosal layer, which acts as a physical barrier to drugs via oral administration. In this study, a magnetic-navigable microneedle drug delivery platform (MNs D) for oral administration, featuring differential dual-mode drug release rate, was designed to fulfil rapid gastric hemostasis and overcome the gastric barriers for long-lasting Helicobacter pylori inhibition in stomach. MNs-D was created by rationally loading the carrier substrate, which was composed of silk fibroin with variable solubility, with antibiotics and hemostats. In vitro experiments showed MNs-D may sustainably eradicate Helicobacter pylori in stimulated gastric juices with long-lasting drug release (79 % in 24 h) and quickly establish hemostasis with instant drug release (92 % within 60 s). Most importantly, in vivo studies demonstrated MNs-D overcame the unsettling gastric mucosal barrier in traditional therapies of oral administration by insertion into the GML under magnetic navigation, resulting in sustained antibiotic release for long-lasting Helicobacter pylori eradiation (99 %). For differential dual-mode medication release against gastric Helicobacter pylori infections, this study may have firstly examined the effects of magnetic navigated microneedles administered orally.

研究领域: 药学 · 生物医学工程 · 胃肠病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Natural Product Communications · 2015 · IF 0.906

Synergy Effects of Three Plant Extracts on Protection of Gastric Mucosa

Caihui Wang,Wen Su,Xingli Su,Guojun Ni,Tao Liu,Yi Kong

The gastric mucosa protection effect of three natural plant extracts, Hericium erinaceus (HE), Centella asiatica (CA) and Amomum villosum (AV), were evaluated using the indomethacin damage model. Compared with a single extract, a combination of HE/CA/AV, especially with the ratios of 80:10:10, 45:45:10 and 45:10:45, showed significant synergistic effects for protection of the gastric mucosa with gastric ulcer inhibition rates of 97.8 ± 0.7%, 86.5 ± 2.8% and 86.1 ± 3.6%, respectively. Microscopic appearances of the gastric mucosa were carried out to help confirm the results.

研究领域: 药理学 · 胃肠病学 · 天然产物化学
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