RUSSIAN JOURNAL OF GENERAL CHEMISTRY
·
2022
·Vol. 92
·期 10
·2178-2185
·
IF 0.779
Lai Lin,Huang Xiang,Sun Wanlin,Chen Xinan,Pei Shuchen,Chai Shuiqin,Chen Jun
Abstract The increasing use of antibiotics to treat bacteria has led to the emergence of many resistant bacteria. Therefore, it is crucial to research novel antibiotics and understand how they are used to combat bacteria. In this study, a green, effective, and ecologically acceptable hydrothermal approach was used to efficiently convert andrographolide and citric acid into carbon dots with vivid blue fluorescence and an emission wavelength of 430 nm. TEM, AFM, FT-IR, and XPS were used to analyze the surface morphology, particle size distribution, and surface functional groups of carbon dots. It was discovered that carbon quantum dots had different functional groups linked to the surface and had a common particle dimension of 2.75 nm. Additionally, it was unexpectedly discovered that carbon quantum dots confirmed great antibacterial motion in opposition to both Escherichia coli ( E. coli ) and Staphylococcus aureus ( S. aureus ), with a MIC of 1.14 mg/mL. Carbon quantum dots have a positive charge of 16 eV, which can connect to the bacterial cell wall and destroy the normal form of bacteria by generating 1 O 2 , causing antibacterial effects, according to research on the antibacterial mechanism of carbon dots.
研究领域:
材料科学
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纳米技术
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生物医学工程
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微生物学
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药学
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DOI
高影响因子
iScience
·
2026
·Vol. 29
·期 6
·
IF 4.5
Haochang Song,Meng Yang,Shengquan Wu,Qihui Dai,Weihong Qin,Weiheng Xie,Yuzhi Chen,Xiaoyun Jiang,Xiaojun Zhang,Xiuqin Deng,Chuang Ouyang,Yunman Zhang,Xinguang Liu,Yingjie Zhu,Gonghua Huang
Andrographolide (AP), a diterpenoid extracted from Andrographis paniculata , has emerged as a promising treatment for Alzheimer’s disease (AD) in preclinical studies, but the underlying mechanisms remain incompletely defined. Here, we demonstrated that AP treatment improved cognition performance and reduced amyloid-β (Aβ) plaque accumulation in 5×FAD transgenic mice of both sexes, by mitigating microglial senescence. Proteomic analysis revealed that AP markedly decreased cholesterol content in the cerebral cortex. Using an in vitro low-density lipoprotein-induced senescence model, we found that AP significantly alleviated senescence in BV2 microglia while enhancing their phagocytic capacity. Mechanistically, AP mitigated microglial senescence by inhibiting STAT3 signaling. Overall, these findings identify a previously unrecognized immunometabolic mechanism for AP in the treatment of AD.
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高影响因子
Asian Journal of Pharmaceutical Sciences
·
2021
·
IF 6.598
Haoshi Gao,Yan Su,Wei Wang,Wei Xiong,Xiyang Sun,Yuanhui Ji,Hua Yu,Haifeng Li,Defang Ouyang
Current formulation development strongly relies on trial-and-error experiments in the laboratory by pharmaceutical scientists, which is time-consuming, high cost and waste materials. This research aims to integrate various computational tools, including machine learning, molecular dynamic simulation and physiologically based absorption modeling (PBAM), to enhance andrographolide (AG) /cyclodextrins (CDs) formulation design. The lightGBM prediction model we built before was utilized to predict AG/CDs inclusion's binding free energy. AG/γ-CD inclusion complexes showed the strongest binding affinity, which was experimentally validated by the phase solubility study. The molecular dynamic simulation was used to investigate the inclusion mechanism between AG and γ-CD, which was experimentally characterized by DSC, FTIR and NMR techniques. PBAM was applied to simulate the in vivo behavior of the formulations, which were validated by cell and animal experiments. Cell experiments revealed that the presence of D-α-Tocopherol polyethylene glycol succinate (TPGS) significantly increased the intracellular uptake of AG in MDCK-MDR1 cells and the absorptive transport of AG in MDCK-MDR1 monolayers. The relative bioavailability of the AG-CD-TPGS ternary system in rats was increased to 2.6-fold and 1.59-fold compared with crude AG and commercial dropping pills, respectively. In conclusion, this is the first time to integrate various computational tools to develop a new AG-CD-TPGS ternary formulation with significant improvement of aqueous solubility, dissolution rate and bioavailability. The integrated computational tool is a novel and robust methodology to facilitate pharmaceutical formulation design.
研究领域:
药剂学
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计算生物学
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药物化学
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PubMed
高影响因子
JOURNAL OF FOOD BIOCHEMISTRY
·
2026
·Vol. 2026
·期 1
·3245873
·
IF 2.3
Caijuan Si,Long Shu,Wenjing Cao,Yuliang Feng,Hui Dong,Xingzhen He,Jingjing Yuan,Songtao Li,Feiwei Cao,Qin Zhu,Peifen Zheng
Andrographolide (Andro) is a major bioactive component of Andrographis paniculata, a medicinal and edible plant with anti-inflammatory effects. However, its effects against ulcerative colitis (UC) and circRNA-related mechanism(s) remain unclear. We established the UC mice model by administrating dextran sulfate sodium (DSS) for 14 days. Treatment with Andro for the last 7 days markedly reversed the shortened colon length, decreased the DAI, and abnormal expression of genes related to inflammation and barriers. Besides, sequencing and qRT-PCR revealed circAsxl2 was upregulated in the DSS group while downregulated after Andro treatment. Moreover, knockdown of circAsxl2 corrected gene expression related to inflammation and barriers in lipopolysaccharide-induced HT-29 cells. Then, miRNA and DEmRNAs associated with circAsxl2 were predicted and used to construct a competitive endogenous RNA (ceRNA) network, in which DEmRNAs mRNA was enriched in immune-related pathways by KEGG. Therefore, Andro possesses the potential to serve as a functional food ingredient for the prevention and management of UC.
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高影响因子
FISH & SHELLFISH IMMUNOLOGY
·
2025
·
IF 3.9
Mengmeng Li,Mingyang Xue,Yong Zhou,Wenzhi Liu,Yan Meng,Chen Xu,Yiqun Li,Nan Jiang,Yuding Fan
Grass carp reovirus (GCRV), which causes hemorrhagic disease in grass carp ( Ctenopharyngodon idella ), poses a significant threat to grass carp aquaculture. To develop effective treatments against GCRV infection, this study evaluated the antiviral efficacy of natural compounds derived from Chinese herbs on GCRV-infected grass carp kidney cells (CIK). Among the various compounds examined, in CIK cells, Andrographolide (Andro) at 25 mg/L exhibited the highest inhibition rates against GCRV-I and GCRV-II infections (83.27% and 87.40%, respectively). In vitro experiments showed that Andro significantly reduced the cytopathic effect, alleviated the apoptosis of GCRV-I-infected cells, inhibited the increase of mitochondrial membrane potential, and blocked CIK cell adsorption of GCRV-I and GCRV-II. Addition time studies revealed that Andro chiefly wielded its antiviral impact in the initial phase of viral replication (0–4 h). In vivo studies demonstrated that in both prevention and treatment experiments, 50 mg/kg Andro in the feed increased the survival rates of grass carp infected with GCRV-Ⅱ by 46.66% and 40%, respectively. Moreover, this compound significantly reduced the viral loads and upregulated antiviral gene expression in various organs, indicating its potential for immune modulation. In conclusion, Andro displayed significant antiviral properties that are effective to both prevent and treat GCRV infections, thus holding promise as a novel therapeutic agent for this virus.
研究领域:
水产养殖学
·
病毒学
·
药理学
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DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2025
·Vol. 26
·期 5
·1-16
·
IF 4
Wang Li,Zhang Xiaoyang,Qu Jianlu,Zhang Zhanrui,Wu Wei,Li Wenlong
Andrographolide (AG) is a diterpenoid lactone, widely recognized for its potent anti-inflammatory and immunomodulatory properties. However, AG’s clinical applications are significantly limited due to its poor water solubility. The aim of this study was to rapidly develop an andrographolide nanosuspension (AG-NS) using Hummer Acoustic Resonance (HAR) technology to enhance AG's solubility. AG-NS was prepared using HAR technology for high-throughput screening of stabilizers. Quality risk assessment was performed to identify critical formulation and process variables influencing AG-NS. A Box-Behnken design (BBD) was applied to evaluate the effects of these critical variables on AG-NS. Following lyophilization, the redispersibility of AG-NS was evaluated, and physicochemical characterization was conducted to verify the absence of significant interactions between AG and the excipients. The optimized AG-NS formulation exhibited a Z-Ave of 183.96 ± 4.40 nm, a PDI of 0.151 ± 0.065, and a zeta potential of -42.85 ± 1.09 mV. MD simulations revealed the internal mechanisms of AG-NS stabilization. Lyophilized AG-NS demonstrated excellent redisperseability. In vitro dissolution studies showed that the lyophilized AG-NS had a significantly faster dissolution rate and higher cumulative dissolution (120 min) compared to AG crude powder and the physical mixture (PM). The optimized AG-NS demonstrated favorable physicochemical properties and enhanced dissolution performance. The lyophilized formulation exhibited excellent redispersibility upon reconstitution. HAR technology is an innovative and efficient approach for the rapid development and optimization of nanosuspension formulations. Graphical
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FITOTERAPIA
·
2012
·
IF 1.848
Yonglei Yuan,Long Ji,Liping Luo,Juan Lu,Xiaoqiong Ma,Zhongjun Ma,Zhe Chen
In the present study, it was demonstrated that the petroleum extract of Andrographis paniculata (AP) had quinone reductase (QR) inducing activity, which might be attributed to the modification of key cysteine residues in Keap1 by Michael addition acceptors (MAAs) in it. To screen MAAs in AP, glutathione (GSH) was employed, and a LC/MS/MS method was implied. Three compounds, andrographoside, andrographolide , 14-deoxy-14,15-dehydroandrographolide were revealed could well conjugated with GSH. Then, andrographolide along with 4 new and 14 known compounds were isolated to conduct QR induction evaluation, and the CD (the concentration required to double the activity of QR) value of andrographolide is 1.43 μM. The QR induce activity of andrographolide might be attributed to its targeting multiple cysteine residues in Keap1, therefore, the alkylation of Keap1 by andrographolide was further studied and the result showed that four cysteine residues: Cys77, Cys151, Cys273 and Cys368 were alkylated, which indicated that Keap1 is a potential target for the QR induce activity of andrographolide.
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BIOCHEMICAL PHARMACOLOGY
·
2024
·
IF 5.3
Meng Yang,Shengquan Wu,Qihui Dai,Weihong Qin,Yujie Zhang,Yiting Lei,Haochang Song,Tingting Zheng,Min Guan,Gonghua Huang,Xinguang Liu
Excessive lipid accumulation often occurs in the early stage of chronic kidney disease (CKD) which is prone to induce oxidative stress and mitochondrial damage, promoting the progression of kidney fibrosis. Andrographolide (AP), a multifunctional natural terpenoids derived from Andrographis paniculate , has been suggested to play beneficial roles in metabolic disorders-associated disease. Here, we reported that AP effectively counteracts tubule injury and interstitial fibrosis in mice fed with a long-term high-fat diet (HFD). AP treatment decreased HFD-induced lipid accumulation in kidney parenchyma and attenuated lipotoxicity-mediated oxidative stress and mitochondrial dysfunction, resulting in a marked decrease in tubular cell senescence. Importantly, AP inhibited senescence-associated secretory phenotype (SASP) secretion by senescent tubular cells, and in turn suppressed proliferation and activation of fibroblasts in a paracrine effect. Furthermore, we revealed that AP functions as an AMP-activated protein kinase (AMPK) activator to ameliorate renal lipid accumulation through coordinately modulating AMP-activated protein kinase AMPK target genes. By stimulation of AMPK activity, AP protects injured kidney against tubular cell senescence and fibroblast activation. These results suggest the potential therapeutic application of AP in the prevention and treatment of CKD, highlighting the promising drug strategy of targeting the lipotoxicity-mediated premature senescence in tubular cells.
研究领域:
肾病学
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药理学
·
分子生物学
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PubMed
高影响因子
BIOLOGICAL & PHARMACEUTICAL BULLETIN
·
2022
·Vol. 45
·期 8
·1106-1115
·
IF 2.264
Linghui Zou,Wenya Ding,Qiuyan Huang,Xu Yang,Jilang Li,Tianyan Huang,Zeyu Li,Si Lin,Jianfang Feng
Andrographolide (AG), a natural product with various pharmacological effects, exhibited low oral bioavailability owing to its poor solubility, stability, and low absorption. Previous studies have suggested that phospholipid (PC) and hydroxypropyl-β-cyclodextrin (HPCD) could improve the drug solubility and absorption. Moreover, nanoemulsion (NE) has been confirmed as an appropriate enhancer for oral bioavailability. Therefore, AG/HPCD/PC complex (AHPC) was synthesized, and AHPC-loaded nanoemulsion (AHPC-NE) was optimized and prepared using central composite design combined response surface methodology. The average droplet size and polydispersity index (PDI) were 116.50 ± 5.99 and 0.29 ± 0.03 nm, respectively. AHPC-NE with a loading capacity of 0.32 ± 0.01% and an encapsulation efficiency of 96.43 ± 2.27% appeared round and uniformly dispersed based on transmission electron microscopy. In vivo release studies demonstrated that AHPC-NE had good sustained-release effects. Further, AHPC-NE significantly enhanced the absorption of AG with a relative bioavailability of 550.71% compared to AG suspension. Such findings reveal AHPC-NE as a potential strategy for sustained-release and oral bioavailability enhancement.
研究领域:
药学
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药物递送系统
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纳米技术
·
药理学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2024
·
IF 5.3
Xiaoyang Zhang,Li Wang,Yao Zhang,Sijun Wu,Xin Sha,Wei Wu,Wenlong Li
The aim of this study was to rapidly develop a sufficiently robust andrographolide nanosuspension (AG-NS) system using hummer acoustic resonance (HAR) technology. The system can effectively improve the dissolution properties of AG, while having high stability and scale-up adaptability. The formulation of AG-NS was optimized in a high-throughput manner using HAR technology and the preparation process was optimized stepwise. Optimal AG-NS with Z-Ave = 223.99 ± 3.16 nm, PDI=0.095 ± 0.007 and zeta potential = –33.20 ± 0.58 mV was successfully prepared with Polyvinylpyrrolidone K30 and Sodium dodecyl sulfate. The optimal prescription was successfully scaled up 100 and 150 times using HAR technology, which was the initial exploration of its commercial scale production. AG-NS was solidified using freeze drying and fluid bed technology, respectively. The optimal AG-NS and its solidified products were exhaustively characterized using various analytical techniques. The high energy input of HAR technology and drying process converted part of the drug into the amorphous state. The in-vitro drug dissolution studies demonstrated relatively higher drug dissolution for AG-NS and its solidified products compared to controls at both the dissolution media (pH 1.2 buffer and pH 6.8 buffer). AG-NS and its solidified products successfully maintained their physical stability in short-term stability and accelerated stability experiments, respectively.
研究领域:
药学
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纳米技术
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药物递送系统
·
制药工程
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产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2024
·
IF 4.4
Shu Long,Fu Hangjie,Pi Aiwen,Feng Yuliang,Dong Hui,Si Caijuan,Li Songtao,Zhu Feiye,Zheng Peifen,Zhu Qin
Ulcerative colitis (UC) is a recurring inflammatory bowel disease, in which oxidative stress plays a role in its progression, and regulation of the oxidative/antioxidative balance has been suggested as a potential target for the treatment of UC. The aim of this study was to evaluate the protective effect of andrographolide against UC and its potential antioxidant properties by modulating the nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) pathway. Dextran sulfate sodium (DSS) -induced UC mice and the LPS-induced HT29 inflammatory cell model were established to uncover the potential mechanisms of andrographolide. ML385, a Nrf2 inhibitor, was used in both models to assess whether andrographolide exerts a protective effect against UC through the Nrf2/HO-1 pathway. The in vivo experiment showed that andrographolide ameliorated the symptoms and histopathology of DSS-induced mice and restored the expressions of ZO-1, Occludin-1 and Claudin-1. Meanwhile, DSS-induced oxidative stress and inflammation were suppressed by andrographolide treatment, along with the upregulation of key proteins in the Nrf2/HO-1 pathway. In vitro experiments showed that andrographolide attenuated LPS-induced excessive generation of ROS in HT29 cells, reduced inflammatory factors, and upregulated the expression of proteins related to tight junctions and Nrf2/HO-1 pathway. In addition, ML385 abolished the beneficial effect of andrographolide. In conclusion, the protective effect of andrographolide against UC may involve the suppression of oxidative stress and inflammation via the Nrf2/HO-1 pathway.
研究领域:
药理学
·
炎症性肠病
·
分子生物学
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DOI
PubMed
高影响因子
Molecular Medicine Reports
·
2018
·Vol. 18
·期 1
·622-626
·
IF 1.922
Qin Zhu,Peifen Zheng,Jianying Zhou,Xinyu Chen,Yuliang Feng,Weifeng Wang,Feng Zhou,Qiaona He
Ulcerative colitis (UC) is a chronic, idiopathic, inflammatory bowel disease of the colon. T cell responses have been associated with the pathology of UC. Andrographis paniculata (AP) extract has been previously reported as an effective treatment of UC. The present study aimed to explore the effects of andrographolide, the primary active component of AP, on the T cell responses of patients with UC. Peripheral blood mononuclear cells (PBMCs) were isolated from patients with UC and treated with various concentrations of andrographolide (0, 10, 20 and 30 µg/ml). Andrographolide decreased interferon γ, interleukin (IL)‑23 and IL‑17A, however it increased IL‑4 in a dose‑dependent manner, as indicated by ELISA assay. Andrographolide treatment resulted in a decreased percentage of T helper (Th)1 and Th17 cells and an increased proportion of Th2 cells, as demonstrated by flow cytometry analysis. T‑bet (a Th1‑specific transcription factor) and RAR‑related orphan receptor γt (key transcription factor of Th17 cells) expression was decreased, but GATA‑3 (Th2 lineage‑specific transcription factor) expression was increased following andrographolide treatment as indicated by western blot analysis. These results demonstrated the inhibitory effects on Th1/Th17 responses and the promoting effects on Th2 responses of andrographolide. Experiments on IL‑23‑treated PBMCs from healthy donors revealed similar effects of andrographolide on Th1/Th2/Th17 responses. In summary, these results suggest that andrographolide may be an effective candidate for the treatment of IL‑23‑mediated diseases.
研究领域:
免疫学
·
药理学
·
炎症性肠病
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DOI
PubMed
高影响因子
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