JOURNAL OF SEPARATION SCIENCE
·
2025
·Vol. 48
·期 4
·e70128
·
IF 2.8
Yongxian Fan,Ruiwei Chen,Lixin Tang,Panpan Fu,Jiawei Zhou,Xiaolong Chen
Asiaticoside (AS) and madecassoside (MS) are two key triterpenoid saponin compounds found in Centella asiatica . Despite their structural similarities, they exhibit distinct biological activities. AS is known for its anti-inflammatory properties and its effectiveness in treating rheumatoid arthritis, while MS is recognized for its ability to promote wound healing and significantly improve burn scars. Additionally, AS is widely utilized in the cosmetics industry due to its antioxidant and moisturizing properties. Currently, separating and purifying these two compounds simultaneously using existing methods is challenging. This study focuses on synthesizing molecularly imprinted polymers (MIPs) through precipitation polymerization with AS as the template. By optimizing various preparation parameters, such as the molar ratios of functional monomers, porogens, and cross-linking agents, high selectivity was achieved. The maximum adsorption capacity reached 19.16 mg/g, with an imprinting factor of 2.86. The MIPs were characterized using techniques like scanning electron microscopy (SEM), TA, Brunauer–Emmett–Teller (BET) adsorption, and Fourier-transform infrared (FT-IR). Their effectiveness was assessed through static and dynamic adsorption, desorption, and reusability tests. When applied in molecularly imprinted solid-phase extraction (MISPE) of crude extracts from C. asiatica , the recovery of AS was 39.90%, and its purity increased by 3.01 times, whereas the purity of MS improved by 6.51 times. These findings indicate that the preparation of MIPs is cost-effective, highly selective, reproducible, and user-friendly, making it a promising method for enriching and isolating AS from complex mixtures.
研究领域:
药理学
·
分析化学
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产品关联
DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2024
·
IF 6.7
Ziliang He,Yeye Hu,Ying Zhang,Jing Xie,Zhiqiang Niu,Guigui Yang,Ji Zhang,Zixuan Zhao,Shuai Wei,Haifeng Wu,Weicheng Hu
Background Parkinson's disease (PD), a neurodegenerative disorder, is characterized by motor symptoms due to the progressive loss of dopaminergic neurons in the substantia nigra (SN) and striatum (STR), alongside neuroinflammation. Asiaticoside (AS), a primary active component with anti-inflammatory and neuroprotective properties, is derived from Centella asiatica. However, the precise mechanisms through which AS influences PD associated with inflammation are not yet fully understood. Purpose This study aimed to explore the protective mechanism of AS in PD. Methods Targets associated with AS and PD were identified from the Swiss Target Prediction, Similarity Ensemble Approach, PharmMapper, and GeneCards database. A protein-protein interaction (PPI) network was constructed to identify potential therapeutic targets. Concurrently, GO and KEGG analyses were performed to predict potential signaling pathways. To validate these mechanisms, the effects of AS on 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced PD in mice were investigated. Furthermore, neuroinflammation and the activation of the NLRP3 inflammasome were assessed to confirm the anti-inflammatory properties of AS. In vitro experiments in BV2 cells were then performed to investigate the mechanisms of AS in PD. Moreover, CETSA, molecular docking, and molecular dynamics simulations (MDs) were performed for further validation. Results Network pharmacology analysis identified 17 potential targets affected by AS in PD. GO and KEGG analyses suggested the biological roles of these targets, demonstrating that AS interacts with 149 pathways in PD. Notably, the NOD-like receptor signaling pathway was identified as a key pathway mediating AS's effect on PD. In vivo studies demonstrated that AS alleviated motor dysfunction and reduced the loss of dopaminergic neurons in MPTP-induced PD mice. In vitro experiments demonstrated that AS substantially decreased IL-1β release in BV2 cells, attributing this to the modulation of the NLRP3 signaling pathway. CETSA and molecular docking studies indicated that AS forms a stable complex with NLRP3. MDs suggested that ARG578 played an important role in the formation of the complex. Conclusion In this study, we first predicted that the potential target and pathway of AS's effect on PD could be NLRP3 protein and NOD-like receptor signaling pathway by network pharmacology analysis. Further, we demonstrated that AS could alleviate symptoms of PD induced by MPTP through its interaction with the NLRP3 protein for the first time by in vivo and in vitro experiments. By binding to NLRP3, AS effectively inhibits the assembly and activation of the inflammasome. These findings suggest that AS is a promising inhibitor for PD driven by NLRP3 overactivation.
研究领域:
神经科学
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药理学
·
炎症
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分子生物学
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产品关联
DOI
PubMed
高影响因子
MOLECULAR IMMUNOLOGY
·
2020
·
IF 3.641
Keyan Wu,Guanghuai Yao,Xiaolei Shi,Huan Zhang,Qingtian Zhu,Xinnong Liu,Guotao Lu,Lianghao Hu,Weijuan Gong,Qi Yang,Yanbing Ding
Acinar cell necrosis is one of the most prominent pathophysiological changes of acute pancreatitis (AP). Asiaticoside (AS) is a triterpene compound with confirmed apoptosis-and necrosis-related activities. However, the specific effects of AS on AP have not been determined. In this study, we aimed to investigate the protective effect of AS on AP using two mouse models. In the caerulein-induced mild acute pancreatitis (MAP) model, We found that AS administration reduced serum amylase levels and alleviated the histopathological manifestations of pancreatic tissue in a dose-dependent manner. And the levels of toll-like receptor 4 (TLR4) and necrotic related proteins (RIP3 and p-MLKL) of pancreatic tissue were reduced after AS administration. In addition, TLR4 deficiency eliminated the protective effect of AS on AP induced by caerulein in mice. Correspondingly, we elucidated the effect of AS in vitro and found that AS protected against pancreatic acinar cells necrosis and TAK-242 counteracted this protective effect. Meanwhile, we found that AS ameliorated the severity of pancreatic tissue injury and pancreatitis-associated lung injury in a severe acute pancreatitis model induced by l -arginine. Furthermore, Molecular docking results revealed interaction between AS and TLR4. Taken together, our data for the first time confirmed the protective effects of AS on AP in mice via TLR4 pathway.
研究领域:
药理学
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病理生理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Burns & Trauma
·
2025
·
IF 9.6
Mu Xingrui,Chen Jitao,Zhu Huan,Deng Junyu,Wu Xingqian,He Wenjie,Ye Penghui,Gu Rifang,Wu Youzhi,Han Felicity,Nie Xuqiang
BackgroundDiabetic wounds pose significant clinical challenges due to impaired healing processes, often resulting in chronic, non-healing ulcers. Asiaticoside (AC), a natural triterpene derivative from Centella asiatica, has demonstrated notable anti-inflammatory and wound-healing properties. However, the synergistic effects of nitric oxide (NO)—a recognized promoter of wound healing—combined with AC in treating diabetic wounds remain inadequately explored.MethodsUltra-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/MS) was utilized to identify differential metabolites and dysregulated metabolic pathways associated with diabetic wounds. Molecular docking analyses were conducted to confirm the binding affinity of AC to key therapeutic targets. The effects of Asiaticoside-nitric oxide hydrogel (ACNO) on gene and protein expression were evaluated using RT-qPCR and western blotting. In vitro experiments using SRC agonists and inhibitors were performed to investigate the impact of ACNO therapy on the expression of SRC, STAT3, and other proteins in HaCaT cells.ResultsMetabolomic profiling revealed that diabetic wounds in mice exhibited marked metabolic dysregulation, which was attenuated by ACNO treatment. Key metabolites modulated by ACNO included mandelic acid, lactic acid, and 3-hydroxyisovaleric acid. The primary metabolic pathways involved were methyl histidine metabolism and the malate–aspartate shuttle. Immunofluorescence staining confirmed that ACNO therapy enhanced angiogenesis, promoted cellular proliferation, and facilitated diabetic wound closure. RT–qPCR data demonstrated that ACNO regulated the transcription of critical genes (SRC, STAT3, EGFR, and VEGFA). Notably, ACNO attenuated SRC/STAT3 pathway activation while concurrently upregulating EGFR and VEGFA expression.ConclusionsThese findings emphasize the therapeutic potential of ACNO hydrogel in diabetic wound healing through the modulation of metabolic pathways and the SRC/STAT3 signaling axis. By correlating altered metabolites with molecular targets, this study elucidates the pharmacodynamic foundation for ACNO’s pre-clinical application and provides valuable insights into the development of targeted therapies for diabetic wound management.
研究领域:
药理学
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代谢组学
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分子生物学
·
糖尿病研究
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伤口愈合
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
·
2022
·Vol. 20
·期 1
·1-14
·
IF 9.429
Wang Pei,Wang Yun,Yi Yang,Gong Yan,Ji Haoran,Gan Yuci,Xie Fei,Fan Jinchen,Wang Xiansong
Patients with diabetic foot ulcers usually suffer from inefficient epithelisation and angiogenesis accompanied by chronic wound healing. Diabetic foot ulcers remain a major challenge in clinical medicine; however, traditional treatments are incapable of transdermal drug delivery, resulting in a low drug delivery rate. We report the development of Ti 2 C 3 MXenes-integrated poly-γ-glutamic acid (γ-PGA) hydrogel microneedles to release asiaticoside (MN-MXenes-AS). Asiaticoside was loaded into PGA-MXenes hydrogel to facilitate cell proliferation while regulating angiogenesis. The characterisation and mechanical strength of the microneedles were investigated in vitro, and the wound-healing efficacy of the microneedles was confirmed in diabetic mice. MXenes significantly improved the mechanical strength of microneedles, while γ-PGA hydrogels provided a moist microenvironment for wound healing. Mice treated with MN-MXenes-AS demonstrated obvious improvements in wound healing process. We successfully fabricated an MXenes-integrated microneedle that possesses sufficient rigidity to penetrate the cuticle for subcutaneous drug delivery, thereby accelerating diabetic wound healing. We demonstrated that MN-MXenes-AS is effective in promoting growth both in vivo and in vitro. Collectively, our data show that MN-MXenes-AS accelerated the healing of diabetic foot ulcers, supporting the use of these microneedles in the treatment of chronic wounds. Graphical Abstract
研究领域:
材料科学
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药学
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生物医学工程
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糖尿病研究
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2026
·Vol. 74
·期 31
·24277-24291
·
IF 6.7
Wu Yuwei,Zhao Meiqi,Zhang Peng,Ho Chi-Tang
Asiaticoside,
a triterpenoid saponin abundant in Centella asiatica , exhibits notable anti-inflammatory
activity but suffers from poor oral bioavailability. Here, we reveal
a gut microbiota-dependent mechanism underlying its therapeutic efficacy
against chronic intestinal inflammation. Using a DSS-induced mouse
model and antibiotic-mediated microbiota depletion, we demonstrate
that asiaticoside requires microbial metabolism to alleviate epithelial
injury, oxidative stress, and inflammatory cytokine production. HPLC
analysis showed that asiaticoside is hydrolyzed by gut microbes into
asiatic acid, which accumulates in colonic tissues and suppresses
IL-17 signaling, NF-κB, and JAK2/STAT3 activation while restoring
Nrf2-mediated antioxidant responses. The released glycosides are further
fermented into butyrate and other short-chain fatty acids, supporting
colonocyte metabolism and intestinal barrier function. Antibiotic
treatment abolishes asiaticoside conversion, SCFA production, and
therapeutic efficacy. These findings establish microbial biotransformation
as a critical determinant of asiaticoside activity and a key mechanism
governing natural glycoside pharmacology.
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2023
·
IF 5.4
Ye Liu,Jiufeng Zhao,Xingrui Mu,Junyu Deng,Xingqian Wu,Wenjie He,Yiqiu Liu,Rifang Gu,Felicity Han,Xuqiang Nie
Ethnopharmacological relevance Centella asiatica (L.) Urban is an ethnobotanical herb. The main bioactive components of Centella asiatica are pentacyclic triterpenoid glycosides , namely asiaticoside and hydroxyasiaticoside. Asiaticoside possess a diverse array of pharmacological properties, such as wound-healing, anti-inflammatory, antioxidant, anti-allergic, antidepressant, anxiolytic, anti-fibrotic, antibacterial, anti-arthritic, anti-tumor, and immunomodulatory activities. Aim of the study The purpose of this investigation is to explore potential therapeutic interventions for the delayed healing of wounds in diabetic patients (DW) facilitated by Asiaticoside-Nitric Oxide. To clarify the key molecular mechanism of miRNA-21-5p in DW wound repair and to deepen the understanding of DW disease pathogenesis. Materials and methods Firstly, miRNA microarray technology, bioinformatics, and RT-qPCR were used to analyze DW patients' and normal controls' skin tissue samples. Secondly, in order to investigate the role of miRNA-21-5p, a hyperglycemic model was established using HaCaT cells. Overexpressing as well as interfering HaCaT cell lines were constructed by lentiviral infection to further explore the proliferative and migratory effects of Asiaticoside-Nitric Oxide. The next step was to search for potential target genes of miRNA-21-5p and verify them with dual-luciferase reporter assay. Finally, the expression levels of target genes and proteins were detected through the utilization of RT-qPCR and Western blotting under the influence of Asiaticoside-Nitric Oxide. Results A library of miRNAs and target genes expressed explicitly in DW patients and rats was established. The study confirmed the upregulation of miRNA-21-5p in DW patients and identified its involvement in signaling pathways related to chronic ulcer wound repair. Overexpression of LV-miRNA-21-5p significantly promoted cell proliferation , while treatments of Asiaticoside-Low dose (AC-L) and Asiaticoside-Medium dose (AC-M) enhanced proliferation and migration, particularly when combined with nitroprusside (SNP). Further analysis revealed potential target genes of miRNA-21-5p, such as TGF-β1, SMAD7, and TIMP3. Their interaction with miRNA-21-5p was confirmed through dual luciferase assays. The study found that anti-DW drugs increased the expression of TGF-β1 and SMAD7 while inhibiting TIMP3 expression in a high-glucose environment. Conclusions The research concluded that miRNA-21-5p plays a crucial role in the delayed healing of diabetic wounds, and that the combination treatment of AC + SNP shows promise in promoting wound healing in DW rats. Target genes, including TGF-β1, SMAD7, and TIMP3, may contribute to the regulatory mechanisms involved in diabetic wound healing. These findings provide valuable insights for developing novel therapeutic approaches for DW.
研究领域:
药理学
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分子生物学
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糖尿病研究
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伤口愈合
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民族药理学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2025
·
IF 9.7
Zhen Wang,Huizhen Han,Tong Wu,Chunyue Zhao,Fangzheng Zhao,Qiqi Han,Huijuan Song,Mengkun Wang,Tingbin Zhang,Weiwei Wang,Yue Li,Ningqiang Gong,Ligong Chen,Jinfeng Xing
Deep burn wounds present significant challenges to rapid healing due to their complex microenvironment, characterized by multiple bacterial infections, excessive oxidative stress and blocked angiogenesis. Herein, a skin-inspired biogel/nanofiber composite dressing composed of gelatin-based biogel and electrospun nanofiber membrane co-loaded with asiaticoside (AS) and ZnO is designed and prepared for regulating the wound microenvironment to accelerate deep burn wound healing. Sodium pyrrolidone carboxylate (PCA-Na) as a natural moisturizing factor is introduced into the gelatin solution to prepare a skin-inspired biogel with strong tissue adhesion, high mechanical strength and good water retention capacity. The sustained release of AS and zinc ions (Zn 2+ ) co-loaded into nanofibers promotes antibacterial activity, anti-inflammatory effects, angiogenesis and collagen deposition. The composite dressing exhibits excellent adhesion to red blood cells and platelets, hemocompatibility and cytocompatibility. Furthermore, it also presents remarkable rapid hemostasis capability with the hemostatic time greatly shortened to 35 s and the blood loss significantly reduced to 71 mg. Notably, it can significantly shorten the healing time of deep burn wound to 17 days by rapidly absorbing wound exudate, promoting collagen deposition and new blood vessels regeneration. Consequently, the composite dressing represents a promising sustained co-delivery system for accelerating burn wound healing.
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产品关联
DOI
PubMed
高影响因子
Materials Today Bio
·
2026
·
IF 11
Zhiqiang Zhang,Long Chen,Chenxi Fang,Guoqiang You,Meitao Duan,Jungang Ren,Ming Chen,Chen Wang
Cutaneous amyloidosis (CA) is a chronic skin disorder characterized by dermal amyloid deposition, accompanied by fibroblast hyperproliferation and keratinocyte apoptosis, yet current treatments are limited by poor transdermal delivery and inadequate lesion clearance. Here, we present a “destroy-reconstruct” strategy using dissolving microneedles (MNs) co-loaded with asiaticoside (AS) and a NIR-II photothermal agent (IR1048), modified with octaarginine (R8) for enhanced cellular uptake. The optimized AI-MN@R8 platform exhibited excellent mechanical strength, rapid in vivo dissolution within 20 min, and a photothermal conversion efficiency of 33.58% under 1064 nm laser irradiation. In vitro studies demonstrated that R8 modification significantly enhanced cellular uptake, and the combination of photothermal therapy and AS synergistically suppressed human skin fibroblasts (HSF) proliferation and migration via inhibition of the EGFR/PI3K/AKT pathway. In a rat model of localized CA, AI-MN@R8 combined with laser irradiation achieved targeted dermal delivery, real-time temperature elevation to approximately 47, and near-complete amyloid clearance, as confirmed by Congo red and Thioflavin 488 staining. Histological and immunohistochemical analyses further revealed restored dermal architecture, reduced collagen deposition, and normalized epidermal keratin expression (KRT5/KRT14). Mechanistically, Western blot analysis of skin tissues confirmed that AI-MN@R8 treatment regulated the Bax/Bcl-2 ratio, inhibited Caspase-3 activation, and downregulated fibrosis-related proteins (COL1A1/COL3A1), reversing the fibrotic microenvironment. No systemic toxicity was observed in major organs. This synergistic photothermal-pharmacological platform offers a safe and effective strategy for CA treatment with high clinical translational potential.
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DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2023
·
IF 15.1
Shuang Liu,Yingsong Zhao,Ming Li,Lei Nie,Qianqian Wei,Oseweuba Valentine Okoro,Hafez Jafari,Siyuan Wang,Jun Deng,Jianghai Chen,Amin Shavandi,Lihong Fan
In this study, bioactive composite hydrogels were created using the decellularized extracellular matrix (ECM), GelMA, and Polydopamine-loaded Asiaticoside (AC@PDA) nanoparticles for use as wound dressings that could promote healing. A decellularization method was used to obtain ECM from porcine Achilles tendon tissue. AC@PDA nanoparticles were then synthesized and found to have a uniform spherical structure with good cytocompatibility, particularly when compared to PDA nanoparticles alone. The mechanical properties of the bioactive composite hydrogels showed good elasticity and shape recovery after compression, with a slight decrease in compressive strength due to the addition of nanoparticles. The formation of interpenetrating networks through the use of EDC/NHS was also found to improve the mechanical properties and moisture retention of the hydrogels. The PDA/ECM-G and AC@PDA/ECM-G hydrogels showed higher water absorption capacity and similar moist retention capacity to the ECM-G hydrogel. The microstructure of the hydrogels was observed through SEM, with the ECM-G hydrogel showing a dense and compact structure, while the PDA/ECM-G and AC@PDA/ECM-G hydrogels displayed a more porous and interconnected structure due to the presence of nanoparticles. In vitro cytotoxicity tests on human skin fibroblasts showed good biocompatibility for all hydrogels. The in vivo wound healing performance of the hydrogels was also tested on a full-thickness excisional wound model in mice, with the AC@PDA/ECM-G hydrogel showing the fastest wound closure without scarring and the highest-formed hair follicles. The AC@PDA/ECM-G hydrogel had the best performance in promoting wound healing. These results suggest that the bioactive hydrogel has the potential for use as a wound dressing.
研究领域:
生物材料
·
组织工程
·
伤口愈合
·
纳米技术
·
生物医学工程
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产品关联
DOI
高影响因子
Pharmaceutics
·
2022
·Vol. 14
·期 5
·1071
·
IF 6.525
Lara Soares Aleixo de Carvalho,Vinícius Carius de Souza,Vinícius C. Rodrigues,Aline Correa Ribeiro,Jorge Willian Leandro Nascimento,Priscila V. S. Z. Capriles,Priscila de F. Pinto,Josué de Moraes,Ademar Alves da Silva Filho
Schistosomiasis, caused by parasites of the genusSchistosoma, is a neglected disease with high global prevalence, affecting more than 240 million people in several countries. Praziquantel (PZQ) is the only drug currently available for the treatment.S. mansoniNTPDases (known as SmNTPDases, ATP diphosphohydrolases orecto-apyrases) are potential drug targets for the discovery of new antischistosomal drugs. In this study, we screen NTPDases inhibitors fromCentella erecta(Apiaceae) using an ultrafiltration combined UHPLC-QTOF-MS method and potato apyrase, identifying asiaticoside as one of the apyrase-binding compounds. After isolation of asiaticoside fromC. erectaextract, we assessed its in vivo antischistosomal activities againstSchistosoma mansoniworms and its in vitro enzymatic apyrase inhibition. Also, molecular docking analysis of asiaticoside against potato apyrase,S. mansoniNTPDases 1 and 2 were performed. Asiaticoside showed a significant in vitro apyrase inhibition and molecular docking studies corroborate with its possible actions in potato apyrase andS. mansoniNTPDases. In mice harboring a patentS. mansoniinfection, a single oral dose of asiaticoside (400 mg/kg. p.o.) showed significantly in vivo antischistosomal efficacy, markedly decreasing the total worm load and egg burden, giving support for further exploration of apyrase inhibitors as antischistosomal agents.Keywords:Schistosoma mansoni;natural products;asiaticoside
研究领域:
药理学
·
寄生虫学
·
天然产物研究
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DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2025
·
IF 13.2
Yao Wang,Rongjie Lin,Chengwei Zhang,Shuwei Lin,Kai Peng,Chengjie Lin,Min Chen,Yanjie Zheng,Zongfu Zheng,Shaohuang Weng
Burn wounds often cause complex skin injuries characterized by persistent bacterial colonization and oxidative stress, which complicates the process of timely healing. Effective local treatments that simultaneously exert antibacterial and antioxidant activities are crucial for treating burn wounds. Herein, a herbal-based hydrogel was developed through the crosslinking of lipoic acid (LA) and asiaticoside (ASI), integrated with antibacterial itaconic acid-derived carbon dots (I-CDs) to form a composite hydrogel designated as I-CDs@LA-ASI. I-CDs@LA-ASI demonstrated excellent biodegradability, biocompatibility, and stable rheological properties. LA-ASI exhibited potent antioxidant properties against reactive oxygen species (ROS). I-CDs@LA-ASI slowly degraded and fully released I-CDs in 7 days. Antibacterial assays demonstrated that I-CDs@LA-ASI effectively inhibited Pseudomonas aeruginosa ( P. aeruginosa ) and its multidrug-resistant bacteria, attributed to the low minimum inhibitory concentration (MIC) of I-CDs against bacteria. Moreover, I-CDs@LA-ASI significantly reduced ROS levels in H 2 O 2 -induced cells, markedly improved the mitochondrial membrane potential and reduced apoptosis. Additionally, I-CDs@LA-ASI promoted cell migration, as demonstrated by scratch assays and Transwell migration assays. I-CDs@LA-ASI further demonstrated significant wound healing efficacy in a P. aeruginosa -infected burn wound model by effective bacterial load reduction, promoting tissue repair, and enhancing angiogenesis. This integrated hydrogel shows great potential for treating complex skin injuries, especially in burn wound infections, suggesting important application prospect.
研究领域:
生物材料
·
纳米技术
·
药剂学
·
创面愈合
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微生物学
·
生物医学工程
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皮肤科
·
药物递送
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）