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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Smart Medicine
·
2026
·Vol. 5
·期 3
·e70047
·
IF 12.8
Zhiqiang Luo,Lingbao Zeng,Xinyu Zhu,Yuanjin Zhao
Synergy therapy of Chinese herbs is an effective strategy for wound repair and its further development focuses on the chronological release of specific herbs with healing proceeding. Herein, we report a novel asiatic acid/baicalein nanocarrier integrated microcapsule with spatiotemporal release feature from microfluidic electrospray for wound healing. Benefiting from advantages of both nanocarrier formulation and integration capacity of microfluidic electrospray, synthesized baicalein-tannic acid nanoparticles are integrated into the shell of microcapsule while fabricated asiatic acid liposomes are located at the core region. This design enables chronological release: baicalein is first released to kill bacteria, followed by releasing asiatic acid liposomes to enhance cell migration and granulation tissue formation. In vitro tests confirm the excellent biocompatibility, antibacterial and pro-migration property of microcapsules. The results from in vivo wound healing studies showed the outcomes of reduced inflammation and accelerated wound closure in microcapsules-treated wounds. Therefore, it is believed that this herbal microcapsule with spatiotemporal and hierarchical release of baicalein and asiatic acid is an effective therapeutic platform for clinical wound treatment. Highlights AA liposomes were derived from concentrated extrusion of AA and phospholipid molecule. Baicalein-tannic acid nanoparticles (BTANPs) were synthesized by solvent exchange. AA liposomes and BTANPs were integrated into ABNM by microfluidic electrospray. ABNM could chronologically release BTANPs and AA liposomes with their biodegradation. ABNM were highly curative to the healing of wounds.
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Biomedicines
·
2025
·Vol. 13
·期 7
·1544
·
IF 3.9
Lei Guo,Peili Wu,Qijian Feng,Xiaochun Lin,Yuan Wang,Minghai Wu,Feifei Cai,Jin Zhang,Chuyi Yang,Xuelin Li,Churan Wen,Yingbei Lin,Nannan Liu,Yuxuan Hu,Huiyun Wang,Xinzhao Fan,Meiping Guan
Background/Objectives:The role of glycogen metabolism in diabetic kidney disease (DKD) remains unclear. This study investigated the therapeutic potential of asiatic acid (AA) on glycogen metabolism in DKD and its underlying mechanisms.Methods:A DKD mouse model was established using a high-fat diet and streptozotocin, followed by AA treatment for 8 weeks. Network pharmacology and molecular docking identified STBD1 as a potential target of AA, and its overexpression in mice was performed.Results:AA reduced blood glucose levels and the urinary albumin-to-creatinine ratio (UACR) and downregulated TGFβ-1, KIM-1, and PDK4. Additionally, AA treatment reversed abnormal glycogen accumulation and restored STBD1 expression. Network pharmacology and molecular docking identified STBD1 as a potential target of AA, and its overexpression in mice demonstrated similar beneficial effects. Gene enrichment analysis revealed that STBD1 is involved in key metabolic pathways related to DKD.Conclusions:These findings suggest that AA alleviates renal damage in DKD, possibly through modulation of STBD1, highlighting its therapeutic potential and the critical role of STBD1 in renal glycophagy.
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BURNS
·
2025
·
IF 2.9
Jiaqi Wu,Guizhen Xu,Xinlu Zhou,Jun Wan,Huaiwei Liao,Cong Li,Yan Shi,Huicai Wen
Background This study investigated the pharmacological effects of asiatic acid (AA) on keloid fibroblasts (KFs) and elucidated its therapeutic mechanisms in keloid pathogenesis. Methods Primary human KFs were isolated and expanded for experimental analysis. Cell migration capacity was evaluated through cell scratch assay and Boyden chamber assay. Immunofluorescence staining was performed to quantify α-smooth muscle actin (α-SMA) expression in AA-treated KFs, while Western blot assessed collagen type I (Col-I), α-SMA, STAT3, and phosphorylated STAT3 (p-STAT3) protein levels. STAT3 activation was pharmacologically induced in KFs using Colivelin TFA (a STAT3 agonist), with subsequent evaluation of migratory behavior and protein expression profiles using parallel methodologies. Results AA treatment significantly inhibited the viability and migratory capacity of KFs, accompanied by downregulation of Col-I, α-SMA, and p-STAT3 expression. Pharmacological activation of STAT3 via Colivelin TFA partially rescued AA-induced suppression of KF migration and Col-I expression. Conclusions AA significantly modulates the migratory capacity and extracellular matrix (ECM)-related protein expression in KFs, with the STAT3 signaling pathway implicated in this regulatory mechanism. These findings indicate that the anti-fibrotic effects of AA are mediated through STAT3 signaling.
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ACS Omega
·
2026
·
IF 5.2
Yuhan Yang,Yanlin Zhu,Hongyan Yuan,Zun Yang,Jie Zhou
Emerging evidence highlights a bidirectional relationship between diabetes and periodontitis, with both conditions sharing common pathogenic mechanisms. Biomaterials capable of modulating macrophage polarization hold significant therapeutic potential for promoting tissue repair in diabetic periodontitis. Asiatic acid (AA), a clinically proven compound with potent antioxidant and antiinflammatory properties, presents an attractive therapeutic candidate. In this study, we developed a multifunctional hybrid hydrogel, AA@GO (AA@GO/SA/CCS, abbreviated as AA@GO), composed of sodium alginate (SA), carboxymethyl chitosan (CCS), and graphene oxide (GO) for effective AA delivery. The AA@GO hydrogel demonstrated remarkable mitophagy-enhancing capabilities, effectively reducing intracellular ROS levels and restoring mitochondrial function in macrophages. Notably, this material significantly increased the M2/M1 polarization ratio by facilitating macrophage phenotype switching from M1 to M2, thereby attenuating inflammatory responses. Our findings elucidate the unique mechanism of AA@GO hydrogel action and propose a promising novel strategy for diabetic periodontitis treatment through macrophage polarization regulation.
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JOURNAL OF FOOD COMPOSITION AND ANALYSIS
·
2026
·
IF 5.3
Huan Liu,Liying Liang,Minggang Wang,Qinfeng Huang,Yu Pan,Xiaojie Wei,Wenchao Zhang
The naturally occurring pentacyclic triterpenoid compounds ursolic acid (UA) and oleanolic acid (OA) are commonly found together in various fruits and find broad applications in pharmaceuticals, cosmetics, food and agricultural fields. In this study, a sensitive and practical icELISA method was developed based on a monoclonal antibody (mAb) YC23-101, with a median inhibitory concentration (IC 50 ) of 15.56 ng/mL and a linear range of 5.26 to 54.1 ng/mL. The limits of detection (LOD) ranges from 0.98-5.11 ng/mL in fruit matrices and the recoveries were 94.03-112.21% with coefficients of variation below 5.73%. Cross-reactivity analysis showed that mAb YC23-101 could also specifically recognize OA with similar sensitivity to UA, indicating feasibility for the simultaneously quantification of UA and OA in fruits. The developed icELISA was applied to several fruits, and the results showed good correlation with that of HPLC. Molecular docking analysis predicted equal binding energy of UA and OA to the mAb with hydrophobic interactions playing a predominant role. All these findings demonstrated that this icELISA is reliable, sensitive, and suitable for the high-throughput quantification of total UA and OA content in fruits composition analysis.
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FOOD AND CHEMICAL TOXICOLOGY
·
2022
·
IF 5.572
Wenyue Qiu,Xinting Zhang,Xiaoyue Pang,Jianjia Huang,Shuilian Zhou,Rongmei Wang,Zhaoxin Tang,Rongsheng Su
Asiatic acid (AA), a triterpenoid compound isolated from Centella asiatica , has anti-inflammatory, antioxidant and anticancer biological characteristics . To explore the effect of AA on LPS-induced acute kidney injury (AKI) in broilers, a total of 60 one-day-old broilers were randomly divided into 6 groups, including the normal group, AKI model group, AKI + AA 15 mg/kg group, AKI + AA 30 mg/kg group, AKI + AA 60 mg/kg group and normal + AA 60 mg/kg group. Hematoxylin-eosin staining was used to observe the histopathology in kidney tissue, and the mRNA and protein expressions related to oxidative stress and ferroptosis were tested by qPCR and western blotting respectively. AA mitigated vacuolar degeneration and enlarged glomerular space caused by LPS in kidney tissue. Additionally, AA significantly increased the mRNA levels of Nrf2, HO-1, NQO1, GCLC, GCLM , GPX4 , SLC7A11 and FTH1 , and decreased the mRNA levels of Keap1 and PTGS2 in LPS-induced AKI. Likewise, AA significantly upregulated the protein expressions of Nrf2, HO-1, NQO1, GPX4, SLC7A11 and FTH1, and downregulated the protein expressions of Keap1 and PTGS2 in LPS-induced AKI. These results suggested that AA alleviated LPS-induced AKI by inhibiting oxidative stress and ferroptosis through targeting regulation of the Nrf2 pathway in broilers.
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LIFE SCIENCES
·
2021
·
IF 5.037
Mengyuan Fang,Wencui Wan,Qiuming Li,Weiwei Wan,Yang Long,Hongzhuo Liu,Xin Yang
Aim This study aimed to evaluate the effects of Asiatic acid (AA), a naturally occurring compound of pentacyclic triterpenoid, on the pathological processes of diabetic retinopathy (DR). Methods SD rats were induced to develop early DR by intraperitoneal injection of STZ (60 mg/kg). Four weeks after injection, the diabetic rats were orally administrated with 37.5 mg/kg or 75 mg/kg AA every day for four weeks. The integrity of blood-retinal barrier (BRB) was measured by Evans blue staining. The polarization of microglia was determined by real-time PCR, western blot, and ELISA assays. The inner BRB (iBRB) or outer BRB (oBRB) breakdown was induced in human retinal endothelial cells or APRE19 cells through co-culture with high glucose and LPS-stimulated microglia BV2 cells. The damage to the iBRB and oBRB was measured using transendothelial/transepithelial electrical resistance (TEER/TER) and FITC-conjugated dextran cell permeability assays. Key findings Results demonstrated that AA alleviated BRB breakdown, as evidenced by decreased protein expression of occludin, claudin-5, and ZO-1. Furthermore, AA treatment suppressed inflammation and M1 polarization, while it increased M2 polarization in the retina of DR rats. In vitro , the iBRB or oBRB breakdown was alleviated by AA. LPS-induced M1-polarization of BV2 cells under high glucose condition was also repressed through AA administration. Finally, we demonstrated that AA weakened the TLR4/MyD88/NF-κB p65 signaling pathway both in vivo and in vitro . Significance AA ameliorated early DR by regulating microglia polarization via the TLR4/MyD88/NF-κB p65 pathway. These data indicate that AA is a potential candidate for DR treatment.
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FOOD AND CHEMICAL TOXICOLOGY
·
2022
·
IF 5.572
Wenshu Zou,Kai Zhang,Zhengying Qiu,Ruihua Xin,Guibo Wang,Jingyan Zhang,Jianxi Li
Damage caused by Salmonella is not only limited to the gastrointestinal tract, but also occurs in the central nervous system (CNS). The aim of this study was to explore the protective effects of asiatic acid (AA) and andrographolide (AD) on the CNS through simulating common infection in mice by oral administration of Salmonella typhimurium (S. typhimurium) . The results showed that the neurons in the hippocampus of mice were damaged after S. typhimurium invaded CNS in mice, and the inflammation was increased, which was manifested by the increased expression of inflammatory factors interleukin (IL)-1β, tumor necrosis factor (TNF)-α, IL-6, interferon (IFN)-γ and IL-12b and the activation of NOD-, LRR- and pyrin domain-containing protein 3 (NLRP3) inflammasomes . The damage and inflammatory response of mouse hippocampal neurons were effectively reduced by AA or AD pretreatment . Furthermore, we observed the significant activation of microglia after S. typhimurium infection. AA and AD attenuated S. typhimurium -induced hippocampal injury by reducing the inflammatory response on microglia. The findings suggest that the AA and AD protect CNS from injury caused by S. typhimurium infection through inhibiting over expression of multiple neuroinflammatory mediators and NLRP3 inflammasome in mice.
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JOURNAL OF NATURAL PRODUCTS
·
2022
·
IF 4.803
Huiqiang Wei,Jianghong Guo,Xiao Sun,Wenfeng Gou,Hongxin Ning,Haihua Shang,Qiang Liu,Wenbin Hou,Yiliang Li
Platinum-resistant ovarian cancer is one of the most common and refractory gynecologic cancers around the world. The SENP1/JAK2 (small ubiquitin-like modifier-specific protease 1/Janus activating kinase 2) axis activation has been proposed as a critical mechanism in platinum-resistant ovarian cancer, and as such, SENP1 inhibitors become a feasible alternative to reverse platinum resistance. In this work, 29 commercially available natural ursane-type aglycones were tested for their SENP1 inhibitory activities, among which 12 aglycones showed IC50 activity at the concentration below 5 μM. Pomolic acid and tormentic acid were identified as potent SENP1 inhibitors with the IC50 values of 5.1 and 4.3 μM, respectively. The structure–activity relationship (SAR) of ursane-type SENP1 inhibitors was evaluated. A molecular docking model of the SENP1–tormentic acid complex was obtained and applied to describe the SAR. Moreover, the combinations of cisplatin with pomolic acid (IC50 = 3.69 μM, combination index (CI) = 0.23) and tormentic acid (IC50 = 2.40 μM, CI = 0.30) exhibited potent platinum-resistant reversal activities to cisplatin only (IC50 = 28.23 μM) against the human ovarian cancer SKOV3 cells. The data suggested a potential for pomolic acid and tormentic acid to be promising compounds for in vivo studies of platinum-resistant ovarian cancer with SENP1 activation.
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JOURNAL OF NANOBIOTECHNOLOGY
·
2024
·Vol. 22
·期 1
·1-21
·
IF 10.6
Hou Yu,Zhu Lin,Ye Xiaofeng,Ke Qiaoying,Zhang Qibin,Xie Xiaowei,Piao Ji-gang,Wei Yinghui
Background Renal fibrosis is a progressive process associated with chronic kidney disease (CKD), contributing to impaired kidney function. Active constituents in traditional Chinese herbs, such as emodin (EMO) and asiatic acid (AA), exhibit potent anti-fibrotic properties. However, the oral administration of EMO and AA results in low bioavailability and limited kidney accumulation. Additionally, while oral probiotics have been accepted for CKD treatment through gut microbiota modulation, a significant challenge lies in ensuring their viability upon administration. Therefore, our study aims to address both renal fibrosis and gut microbiota imbalance through innovative co-delivery strategies. Results In this study, we developed yeast cell wall particles (YCWPs) encapsulating EMO and AA self-assembled nanoparticles (NPYs) and embedded them, along with Lactobacillus casei Zhang, in chitosan/sodium alginate (CS/SA) microgels. The developed microgels showed significant controlled release properties for the loaded NPYs and prolonged the retention time of Lactobacillus casei Zhang ( L. casei Zhang) in the intestine. Furthermore, in vivo biodistribution showed that the microgel-carried NPYs significantly accumulated in the obstructed kidneys of rats, thereby substantially increasing the accumulation of EMO and AA in the impaired kidneys. More importantly, through hitchhiking delivery based on yeast cell wall and positive modulation of gut microbiota, our microgels with this synergistic strategy of therapeutic and modulatory interactions could regulate the TGF-β/Smad signaling pathway and thus effectively ameliorate renal fibrosis in unilateral ureteral obstruction (UUO) rats. Conclusion In conclusion, our work provides a new strategy for the treatment of renal fibrosis based on hitchhiking co-delivery of nanodrugs and probiotics to achieve synergistic effects of disease treatment and targeted gut flora modulation. Graphical Abstract
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Smart Medicine
·
2025
·Vol. 4
·期 3
·e70017
·
IF 11.6
Xinyu Zhu,Lijun Cai,Yu Wang,Hong Chen,Chenjie Yu,Yuanjin Zhao
Hydrogel patches have been serving as powerful tools for wound healing. Scientific attention in this field is focused on imparting the patches with novel structures, functions, and actives for promoting wound healing. In this paper, we have developed an innovative hydrogel patch with hierarchical structure and spatiotemporal actives release for efficient wound healing. This hydrogel patch was achieved by integrating asiatic acid (AA)-loaded pollens with chlorogenic acid (CA)-containing gelatin methacryloyl (GelMA) hydrogel. The high specific surface area and nanoporous structure of the pollens-integrated GelMA promote efficient loading and release of CA and AA, respectively. In wound treatment, the outer layer of GelMA first releases CA to fight infection. With the gradual degradation of GelMA, the pollens are exposed to the wounds and released AA, intensifying anti-inflammatory effects and promoting wound healing. These features indicate that this pollen-integrated hydrogel patch significantly accelerates the wound healing process in a spatiotemporal responsive manner, demonstrating great potential for clinical applications. Key Points An innovative hydrogel patch with hierarchical structure and spatiotemporal actives release for efficient wound healing. This hydrogel patch was achieved by integrating asiatic acid-loaded pollens with chlorogenic acid-containing gelatin methacryloyl hydrogel. The high specific surface area and nanoporous structure of the pollens-integrated gelatin methacryloyl promote efficient loading and release of chlorogenic acid and asiatic acid, respectively.
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