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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Therapeutic potential of Rosa rugosa polysaccharide and its nanofiber membrane in psoriasis via PI3K-AKT/mTOR pathway inhibition

Mengxiang Chen,Yi Peng,Rongtao Zhu,Xiaoting Luo,Xuemin Yang,Jiazhi Chen,Haiyan Chen,Wei Zhou,Zhiyun Du

Psoriasis is a chronic inflammatory skin disease with significant impacts on quality of life. Current treatments face challenges like high costs and side effects. This study explores the therapeutic potential of Rosa rugosa polysaccharide (RRPS) and its nanofiber membrane in psoriasis treatment. RRPS was extracted using a yeast fermentation enzyme-assisted method and characterized. In vitro studies on RAW264.7 macrophages showed that RRPS significantly reduced nitric oxide (NO) production, indicating anti-inflammatory effects. The nanofiber membrane, fabricated via electrospinning, has high porosity and sustained-release properties, enhancing drug delivery and skin barrier repair. In vivo studies using an imiquimod-induced psoriasis mouse model demonstrated that both RRPS and its nanofiber membrane improved psoriasis symptoms, reduced transepidermal water loss (TEWL), and inhibited pro-inflammatory cytokines (e.g., TNF-α, IL-6, IL-17A). Mechanistically, they suppressed the PI3K-AKT/mTOR pathway. The nanofiber membrane showed superior efficacy compared to RRPS alone, highlighting the benefits of electrospinning. This study suggests that Rosa rugosa polysaccharide and its nanofiber membrane could be a novel, effective, and safe alternative for psoriasis treatment by targeting the PI3K-AKT/mTOR pathway.

研究领域: 皮肤病学 · 药理学 · 纳米技术 · 免疫学 · 生物技术 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMISTRY & BIODIVERSITY · 2025 · IF 2.5

The Ethanol Extract of Syringa pubescens Turcz. Flower Ameliorates Inflammation Responses by Inhibiting the Expression of Cyclooxygenase-2/Inducible Nitric Oxide Synthase and the Release of Inflammatory Factors

Yanfang Wu,Jiameng Zhang,Ting Zhang,Chenyu Wang,Wanting Bi,Yanxia Wu,Pu Liu,Xinsheng Wang

The flower of Syringa pubescens Turcz., frequently prepared as herbal tea, exhibits various biological properties, including anti-inflammatory, antioxidant, and hepatoprotective activities. Herein, we identify the chemical constituents from ethanol extract of S. pubescens flower (SPFE) and explore its antioxidant, anti-xanthine oxidase (anti-XOD), and 5-lipoxygenase (5-LOX) enzyme activities, and anti-inflammatory activities and mechanisms. SPFE contained a variety of glycosides and showed good antioxidant capacity and effectively inhibited the activity of 5-LOX and XOD enzymes in vitro. In the model of RAW264.7 cell inflammation generated by lipopolysaccharide, SPFE not only impeded the expression of inflammatory mediators and the accumulation of malondialdehyde, but also restored the capacity of antioxidant enzymes. Moreover, SPFE could notably relieve or treat inflammation by suppressing the expression of inducible nitric oxide synthase and cyclooxygenase-2 proteins. In vivo inflammation models, oral SPFE remarkably reduced the swelling of the ear, paw tissues in mice and had a good anti-inflammatory activity, reducing cell infiltration in the claw tissue, and restoring the degree of oxidative damage in the organism. Our findings demonstrate that SPFE exhibits promising potential as a novel therapeutic agent or nutraceutical for anti-inflammatory applications. Graphical

研究领域: 药理学 · 生物化学 · 药物化学 · 免疫学 · 植物学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOORGANIC CHEMISTRY · 2020 · IF 4.831

Design, synthesis and biological evaluation of novel arylpropionic esters for the treatment of acute kidney injury

Jiawei Zuo,Shi-Meng Wang,Xia Jiang,Mengxin Cao,Ziwen Zhang,Tianlu Shi,Hua-Li Qin,Wenjian Tang

Acute kidney injury (AKI) is associated with a strong inflammatory response, and inhibiting the response effectively prevents or ameliorates AKI. A series of novel arylpropionic esters were designed, synthesized and evaluated their biological activity in LPS-stimulated RAW264.7 cells. Novel arylpropionic esters bearing multi-functional groups showed significant anti-inflammatory activity, in which, compound 13b exhibited the most potent activity through dose-dependent inhibiting the production of nitric oxide (NO, IC 50  = 3.52 μM), TNF-α and IL-6 (84.1% and 33.6%, respectively), as well as suppressing the expression of iNOS, COX-2 and TLR4 proteins. In C57BL/6 mice with cisplatin-induced AKI, compound 13b improved kidney function, inhibited inflammatory development, and reduced pathological damage of kidney tissues. In brief, this arylpropionic ester scaffold may be developed as anti-inflammatory agents.

CAS / MDL: 14913-33-8
研究领域: 药理学 · 药物化学 · 炎症研究 · 肾脏生理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD CHEMISTRY · 2022 · IF 9.231

Gut microbial fermentation promotes the intestinal anti-inflammatory activity of Chinese yam polysaccharides

Yajuan Bai,Yue Zhou,Ruifen Zhang,Yanxia Chen,Fengzhong Wang,Mingwei Zhang

Plant polysaccharides possess many health-promoting properties, which are closely related to the digestion, absorption and utilization of polysaccharides in the host. The characteristic changes in Chinese yam polysaccharide (CYP) during simulated gastrointestinal digestion and faecal fermentation, as well as the intestinal anti-inflammatory effects of CYP and fermented CYP, were studied. The molecular weight of CYP remained unchanged during gastrointestinal digestion. After 24 h of faecal fermentation, free glucose and mannose released from CYP were utilized by gut microbiota, and the production of short-chain fatty acids increased. Simultaneously, CYP improved the growth of Bifidobacterium and Megasphaera. Compared with CYP, faecal fermented CYP exhibited greater suppression of anti-inflammatory mediators and increased intestinal tight junction expression in LPS-stimulated coculture Caco-2/Raw264.7 cells. The obtained results reveal that the role of CYP in promoting gut health is closely related to the interactions between CYP and gut microbes, and CYP has potential as an anti-inflammatory adjuvant in enteritis therapy.

研究领域: 营养科学 · 微生物学 · 免疫学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOORGANIC CHEMISTRY · 2024 · IF 4.5

Sesquiterpenoids from Carpesium abrotanoides and their anti-inflammatory activity both in vitro and in vivo

Xiao-Fang Zhang,Hong-Fei Li,Hui Liu,Fang-Lu Wei,Jiao-Xian Du,Ji-Kai Liu,Juan He,Tao Feng

Twenty-nine sesquiterpenoids, including pseudoguaiane-type ( 1 – 11 ), eudesmane-type ( 12 – 23 ), and carabrane-type ( 24 – 29 ), have been identified from the plant Carpesium abrotanoides . Of them, compounds 1 – 4 , 12 – 15 , and 24 – 27 , namely carpabrotins A–L, are twelve previously undescribed ones. Compound 3 possessed a pseudoguaiane backbone with a rearrangement modification at C-11, C-12 and C-13, while compound 4 suffered a carbon bond break between the C-4 and C-5 to form a rare 4,5- seco -pseudoguaiane lactone. Compounds 1 – 3 , 5 , 13 – 16 and 25 – 27 exhibited anti-inflammatory activity by inhibiting NO production in LPS-induced RAW264.7 macrophages with IC 50 values less than 40 μM, while compounds 1 , 2 , 5 , 13 , 14 , 16 , and 25 – 27 showed significant inhibitory activity comparable to that of dexamethasone. The anti-atopic dermatitis (AD) effects of compounds 5 and 16 were tested according to 2,4-dinitrochlorobenzene (DNCB)-induced AD-like skin lesions in KM mice, and the results revealed that the major products 5 and 16 improved the histological features of AD-like skin lesions and mast cell infiltration in mice. This study suggested that sesquiterpenoids in C. abrotanoides should play a key role in its anti-inflammatory use.

CAS / MDL: 97-00-7
研究领域: 药理学 · 植物化学 · 炎症研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2024 · IF 5.7

Novel l-Cysteine Incomplete Degradation Method for Preparation of Procyanidin B2-3′-O-Gallate and Exploration of its in Vitro Anti-inflammatory Activity and in Vivo Tissue Distribution

Yanxia Yu,Chunying Zuo,Mingrui Li,Yuanyuan Tang,Lingxi Li,Fang Wang,Shuting Zhang,Baoshan Sun

In this study, an effective method for preparation of bioactive galloylated procyanidin B2-3′-O-gallate (B2-3′-G) was first developed by incomplete depolymerization of grape seed polymeric procyanidins (PPCs) using l-cysteine (Cys) in the presence of citric acid. The structure–activity relationship of B2-3′-G was further evaluated in vitro through establishing lipopolysaccharide (LPS)-induced inflammation in RAW264.7 cells. The results suggested that the better protective effects of B2-3′-G against inflammation were attributed to its polymerization degree and the introduction of the galloyl group, compared to its four corresponding structural units. In vivo experiments demonstrated that the B2-3′-G prototype was distributed in plasma, small intestine, liver, lung, and brain. Remarkably, B2-3′-G was able to penetrate the blood–brain barrier and appeared to play an important role in improving brain health. Furthermore, a total of 18 metabolites were identified in tissues. Potential metabolic pathways, including reduction, methylation, hydration, desaturation, glucuronide conjugation, and sulfation, were suggested.

CAS / MDL: 52-90-4
研究领域: 药理学 · 生物化学 · 分子生物学 · 药学 · 神经科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMEDICINE & PHARMACOTHERAPY · 2017 · IF 2.759

Influence of sinomenine upon mesenchymal stem cells in osteoclastogenesis

Biao Zhou,Xiaolong Lu,Zhi Tang,Dan Liu,Youliang Zhou,Peng Zeng,Hui Xiong

With the advent of aging, the morbidity rates of such diseases as osteoarthritis , rheumatoid arthritis , and osteoporosis has witnessed a significant increase. As a common rattan drug , sinomenine (SIN) has been widely applied for the treatment of various arthritic diseases in traditional Chinese medicine (TCM) clinics. Given that SIN has been reported to inhibit the expression of Prostaglandin E2 (PGE2) in several types of cells, in this study, the influence of SIN treatment on PGE2 expression in mesenchymal stem cells (MSCs), thereby changing the osteoprotegerin (OPG) receptor/activator for the nuclear factor-κ B ligand (RANKL) ratio, was investigated. Our results showed that, when compared with the untreated cells, treatment with 0.25   mM SIN can down-regulate the mRNA and protein expression levels of the Prostaglandin E synthase 3 (PTGES3) or PGE2 and RANKL , while the OPG was up-regulated. After being cultured with SIN treated MSC-conditioned medium (stMSC-CM), the amount of TRAP-positive multinucleated osteoclasts differentiated from RAW264.7 cells was reduced. Also, the expression levels of specific markers for active osteoclasts were decreased when incubated with stMSC-CM. Moreover, these changes were able to be recovered when the exogenous RANKL was added to the MSC-CM culture . This indicates that the increased OPG/RANKL ratio can reduce the osteoclastogenesis of RAW264.7 cells. Our results demonstrated that SIN has an inhibitory effect on osteoclast differentiation through mechanisms involving the inhibition of the PGE2-induced OPG/RANKL ratio. SIN can also serve as a proinflammatory mediator to regulate the MSC immunosuppressive effects. Our findings suggest that SIN can be useful for the treatment of bone diseases associated with over-activity of osteoclasts.

CAS / MDL: 58944-73-3
研究领域: 药理学 · 免疫学 · 细胞生物学 · 干细胞研究 · 骨病治疗
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MACROMOLECULAR BIOSCIENCE · 2022 ·Vol. 22 ·期 11 ·2200150 · IF 5.859

A Straightforward Approach towards Antibacterial and Anti-Inflammatory Multifunctional Nanofiber Membranes with Sustained Drug Release Profiles

Wenjie Wang,Yilin Wang,Weifeng Zhao,Changsheng Zhao

Preventing bacterial infection and controlling the inflammatory response occupy important positions in wound treatment. Although loading wound dressings with antibacterial or anti-inflammatory drugs/molecules is an effective approach to address these issues, simultaneous sustained release of these drugs remains challenging. Herein, hydrophilic polyhexamethylene guanidine hydrochloride (PHGC) and hydrophobic indomethacin (Indo) are loaded in hydrophilic polyvinyl alcohol (PVA) and hydrophobic polycaprolactone (PCL) nanofibers respectively by bidirectional electrospinning to form an antibacterial and anti-inflammatory PCL-Indo/PVA-PHGC wound dressing. The fabricated nanofiber membrane exhibits 100% disinfection activity to both Gram-negative ( E. coli) and Gram-positive ( S. aureus ) bacteria because of the release of the broad-spectrum antibacterial molecule PHGC. Additionally, the loading of Indo in the nanofiber membrane enhances the expression level of IL-10, while inhibiting those of IL-6 and TNF- α in the RAW264.7 mouse cells. In the interwoven membrane of PCL and PVA fibers, the release of hydrophobic Indo is hindered by hydrophilic PHGC and PVA fibers, and similarly, the release of hydrophilic PHGC is hindered by hydrophobic Indo and PCL fibers. In conclusion, the PCL-Indo/PVA-PHGC nanofiber membrane has excellent antibacterial, anti-inflammatory, and sustained-release effects, and thus regulates the immune microenvironment of the cells to potentially promote wound healing.

研究领域: 材料科学 · 生物医学工程 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Bioscience · 2025 · IF 5.9

Inflammatory modulation effects of human milk oligosaccharides: from screening in-vitro to application in the milk powders

Jiayue Tang,Dan Yao,Jiahe Zhao,Maolin Tu

Human milk oligosaccharides (HMOs) are significant constituents of breast milk and have potential anti-inflammatory bioactivities. We compared the immunomodulatory effects of lacto-N-biose I (LNB), lacto-N-triose II (LNT II), galacto-oligosaccharides (GOS), and their combinations (GOS+LNB, GOS+LNT II, LNB+LNT II, m/m=1:1) in lipopolysaccharide-induced RAW264.7 macrophages. LNT II and LNB+LNT II efficiently inhibited inflammation-related gene expression and enhanced phagocytosis and anti-inflammatory ability, which may be attributed to their N-acetylglucosamine structure. Three milk powder prototypes (control, LNT II, and LNB+LNT II) were formulated and characterized, exhibiting favorable physicochemical properties. In-vitro simulated digestion coupled with caucasian colon adenocarcinoma (Caco-2) inflammation model demonstrated that the milk powder digestives inhibited tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β) release while promoting interleukin-10 (IL-10) production. The digestives of the three milk powders could also inhibit the decrease in transmembrane electrical resistance and the increase in intestinal permeability, playing a crucial role in maintaining intestinal homeostasis. This study will contribute to the functional evaluation and product development of HMOs and inform milk powder design.

CAS / MDL: 60842-46-8
研究领域: 营养学 · 免疫学 · 食品科学 · 药理学
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BIOCHEMICAL PHARMACOLOGY · 2024 · IF 5.3

Isobavachin attenuates osteoclastogenesis and periodontitis-induced bone loss by inhibiting cellular iron accumulation and mitochondrial biogenesis

Ting Li,Yangge Du,Hantao Yao,Boxuan Zhao,Zijun Wang,Rourong Chen,Yaoting Ji,Minquan Du

As bone-resorbing cells rich in mitochondria, osteoclasts require high iron uptake to promote mitochondrial biogenesis and maintain a high-energy metabolic state for active bone resorption. Given that abnormal osteoclast formation and activation leads to imbalanced bone remodeling and osteolytic bone loss, osteoclasts may be crucial targets for treating osteolytic diseases such as periodontitis. Isobavachin (IBA), a natural flavonoid compound, has been confirmed to be an inhibitor of receptor activator of nuclear factor κB ligand (RANKL)-induced osteoclast differentiation from bone marrow-derived macrophages (BMMs). However, its effects on periodontitis-induced bone loss and the potential mechanism of its anti-osteoclastogenesis effect remain unclear. Our study demonstrated that IBA suppressed RANKL-induced osteoclastogenesis in BMMs and RAW264.7 cells and inhibited osteoclast-mediated bone resorption in vitro. Transcriptomic analysis indicated that iron homeostasis and reactive oxygen species (ROS) metabolic process were enriched among the differentially expressed genes following IBA treatment. IBA exerted its anti-osteoclastogenesis effect by inhibiting iron accumulation in osteoclasts. Mechanistically, IBA attenuated iron accumulation in RANKL-induced osteoclasts by inhibiting the mitogen-activated protein kinase (MAPK) pathway to upregulate ferroportin1 (Fpn1) expression and promote Fpn1-mediated intracellular iron efflux. We also found that IBA inhibited mitochondrial biogenesis and function, and reduced RANKL-induced ROS generation in osteoclasts. Furthermore, IBA attenuated periodontitis-induced bone loss by reducing osteoclastogenesis in vivo. Overall, these results suggest that IBA may serve as a promising therapeutic strategy for bone diseases characterized by osteoclastic bone resorption.

CAS / MDL: 64-17-5 111-30-8
研究领域: 药理学 · 牙科 · 细胞生物学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2022 · IF 6.51

Study on the preparation of EGCG-γ-Cyclodextrin inclusion complex and its drug-excipient combined therapeutic effects on the treatment of DSS-induced acute ulcerative colitis in mice

Weiqin Wang,Xuefeng Li,Fanli Shi,Zhenhai Zhang,Huixia Lv

In this study, γ-cyclodextrins (γ-CD) and epigallocatechin-3-gallate (EGCG) were designed to form an inclusion complex (EGCG-γ-IC) for ulcerative colitis (UC) treatment. The drug-excipient combined therapeutic potential of γ-CD and EGCG was verified, when stability and compliance were also achieved. EGCG-γ-IC effectively inhibited the secretions of NO, TNF-α, and IL-6 and the intracellular ROS in RAW264.7 cells. The effectiveness of EGCG-γ-IC in treating DSS-induced acute UC in mice was observed including improving the histological conditions of the colon, reducing the levels of IL-1β, IL-6, and TNF-α in serum, and restoring MPO , GSH, and sIgA levels in intestinal tissues. Moreover, EGCG-γ-IC had a more prominent effect on regulating bacterial dysbiosis caused by DSS than EGCG and γ-CD alone. Therefore, EGCG-γ-IC designed here displayed UC treating capacity with safety in the long-term application and promised an industrial production potential due to its excellent storage stability.

CAS / MDL: 89-57-6
研究领域: 药学 · 炎症性肠病 · 药物递送系统 · 免疫学 · 微生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMEDICINE & PHARMACOTHERAPY · 2024 · IF 6.9

The bone-protective benefits of kaempferol combined with metformin by regulation of osteogenesis-angiogenesis coupling in OVX rats

Zhongyuan Zhang,Wenshu Xu,Zhenhua Zhang,Xiaoxue Chen,Hui Jin,Ningning Jiang,Hui Xu

This study was to investigate the potential mechanisms of treatment with metformin (Met) combined with kaempferol (Kae) against postmenopausal osteoporosis. Experiments were conducted in both ovariectomy (OVX)-induced osteoporosis rats and in vitro using RAW264.7 cells, MC3T3-E1 cells, and HUVECs. Results demonstrated the therapeutic effect of Met combined with Kae on osteoporosis. In vivo, Kae alone and in combination with Met treatments enhanced tibial trabecular microstructure, bone mineral density (BMD), and mechanical properties in OVX rats without causing hepatotoxicity and nephrotoxicity. It also reduced bone resorption markers (CTX-1 and TRAP) and increased the bone formation marker (PINP) level in the serum of OVX rats. The expression of bone resorption marker TRAP was reduced, while bone formation markers Runx2 and ALP were enhanced in the bone tissue of OVX rats. Furthermore, Met combined with Kae also promoted the expression of angiogenesis-related markers CD31 and VEGF in OVX rats. In vitro, MC3T3-E1s cells treated with Met combined with Kae showed higher expression of ALP, Runx2, and VEGF. Interestingly, the treatment did not directly promote HUVECs migration and angiogenesis, but enhanced osteoblast-mediated angiogenesis by upregulating VEGF levels. Additionally, Met combined with Kae treatment promoted VEGF secretion in MC3T3-E1, and activated the Notch intracelluar pathway by upregulating HES1 and HEY1 in HUVECs. Meantime, their stimulation on CD31 expression were inhibited by DAPT, a Notch signaling inhibitor. Overall, this study demonstrates the positive effects of Met combined with Kae on osteoporotic rats by promoting osteogenesis-angiogenesis coupling, suggesting their potential application in postmenopausal osteoporosis.

研究领域: 药理学 · 骨科 · 分子生物学 · 细胞生物学
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