ANALYTICA CHIMICA ACTA
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2022
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IF 6.911
Jin-Ye Lu,Qiu-Yun Chen,Su-Ci Meng,Chang-Jian Feng
Phthalates can penetrate the environment and enrich various aquatic organisms through the food chain, which is involved in promoting the growth of breast cancer. It is of current interest to develop new sensors for phthalates. We herein reported a hydrogen-bond competing fluorescent sensor, BANP, for the detection of dibutyl phthalate (DBP). The BANP compound was synthesized by assembling andrographolide (Andro), nitro- and cyano-substituted BODIPY dye (BCN), and polyethylene glycol derivatives (DSPE-mPEG5000). BANP was found to be a turn-on fluorescent probe for DBP in water with a detection limit of 0.13 μg/g; the DBP-water system acts as a hydrogen bond switch to turn on the fluorescence. And BANP fluorescently detected DBP in contaminated fish meat. Moreover, BANP sensed the DBP-induced growth of human breast cancer MCF-7 cells, and the release of Andro in the DBP-cultivated cancer cells inhibited the proliferation of the MCF-7 cells. Taken together, BANP is a DBP-responsive probe for sensitive DBP detection in water, cells, and fish meats. The BANP sensor may be used in both in vitro fluorescence and cellular imaging analyses. Our results show that guest-induced reassembly brings forth significant fluorescence change, which is a promising way of designing new fluorescent probes for the analysis of phthalates in the environment and food.
研究领域:
分析化学
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环境科学
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生物医学
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PubMed
高影响因子
Asian Journal of Pharmaceutical Sciences
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2026
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IF 12.6
Yin Zhou,Jiayi Wang,Yi Chen,Zijie Li,Gustavo Puras,José Luis Pedraz,Zhongwei Gu,Yiyan He
Acute lung injury (ALI) leads to severe pulmonary inflammation and alveolar-capillary barrier disruption, with therapy limited by poor solubility and bioavailability of anti-inflammatory agents. To address the limited aqueous solubility, insufficient lesion accumulation, and poor bioavailability of andrographolide (ANDRO) in ALI therapy, an inflammation-responsive nanoprodrug platform (NanoPro5000@ANDRO) was developed via subcomponent self-assembly using dynamic boronic ester and imine linkages, thereby enabling both chemical conjugation and physical encapsulation of ANDRO at a total drug-loading content of 30.24% with an average hydrodynamic diameter of 206.4 nm. This platform exhibited excellent biocompatibility, including a hemolysis rate of less than 5% and protein adsorption of less than 10%, and achieved 82.1% cumulative ANDRO release at 48 h under acidic and oxidative conditions, facilitating inflammation-associated lesion-specific drug delivery. Furthermore, the nanosystem exhibited enhanced pulmonary accumulation in inflamed lung tissues, suppressed pro-inflammatory cytokines, including tumor necrosis factor-α and interleukin (IL)-6, upregulated anti-inflammatory mediators, including IL-4 and IL-10, reduced oxidative stress, and promoted M2 macrophage polarization. These combined effects alleviated cytokine storm, restored inflammatory microenvironment homeostasis, and attenuated lipopolysaccharide-induced ALI-associated tissue damage with confirmed biosafety. Overall, this study presents a dual dynamic covalent bond-based nanoprodrug strategy featuring dual ANDRO loading and pH/reactive oxygen species-responsive release behavior, providing a promising therapeutic approach for cytokine-associated inflammatory pulmonary diseases.
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Journal of Orthopaedic Translation
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2021
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IF 5.191
Rongliang Wang,Jiawei Li,Xingquan Xu,Jia Xu,Huiming Jiang,Zhongyang Lv,Rui Wu,Ziying Sun,Wenjie Guo,Yang Sun,Shiro Ikegawa,Qing Jiang,Dongquan Shi
Background Synovial inflammation plays a major role in the pathogenesis of osteoarthritis (OA). This study investigated the effect of andrographolide (Andro) on synovial inflammation mediated by tumor necrosis factor-alpha receptor 2 (TNFR2) trafficking and its utility in attenuating OA progression. Methods Knee joints were harvested from rats subjected to radial transection of the medial collateral ligament (MCLT) and medial meniscus (MMT) to examine the effect of Andro on synovial inflammation and OA progression. Quantitative real-time polymerase chain reaction was used to evaluate the expression of inflammatory factors in primary fibroblast-like synoviocytes (FLSs) after Andro treatment in vitro . The mechanism underlying Andro-mediated regulation of TNFR2 distribution and nuclear factor-κB (NF-κB) expression was verified using endosome maturation inhibitor hydroxychloroquine (HCQ) through flow cytometry, immunofluorescence, and western blot analysis. Results Andro treatment was found to reduce synovial inflammation and OA progression in vivo . Furthermore, a decrease in pain hypersensitivity and dorsal horn neuron activation was observed after treatment. Andro also downregulated the expression of inflammatory mediators and TNFR2 in FLSs. TNFR2 is crucial for the activation of the NF-κB signaling pathway, and Andro-induced degradation of TNFR2 was associated with lysosomal function, which in turn, reduced the downstream phosphorylation of p65 in the NF-κB signaling pathway. Conclusions Andro could suppress synovial inflammation via regulation of TNFR2 trafficking and degradation. This also suggests it could be a potential treatment for the prevention of synovial inflammation and OA progression. The translational potential of this article This study provides strong evidence that Andro reduces NF-κB activation and inflammatory responses in OA FLSs via regulation of TNFR2 trafficking. The inhibition of TNFR2 and Andro could be a novel therapeutic approach for OA and pain management.
研究领域:
药理学
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风湿病学
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炎症
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疼痛管理
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骨科
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DOI
PubMed
高影响因子
PHARMAZIE
·
2018
·Vol. 73
·期 10
·594-597
·
IF 1.016
Wu Bo,Chen Xi,Zhou Ying,Hu Pingjun,Wu Dan,Zheng Guodong,Cai Yi
Background: Andrographolide (Andro) belongs to the main bioactive ingredients of Andrographis paniculata. Many studies have shown that andro has a variety of pharmacological activities such as anti-inflammatory, anti-bacterial, anti-virus, anti-oxidant, immune regulation
and liver protective effects. Moreover andro has been reported to have anticancer activity in multiple types of cancer, including gastric cancer, breast cancer, lung cancer and so on. However, there is no report about the effect of andro on the human NPC cell line C666-1 and the molecular
mechanisms of andro-mediated apoptosis in C666-1 cells remain to be clarified. Methods: Cell proliferation was measured by a CCK8 assay, cell apoptosis rate was evaluated by flow cytometric analysis, and the protein expression of LKB1/AMPK signaling pathways was detected by Western
blotting. Results: Treatment with andro inhibited cell proliferation and induced apoptosis of C666-1 cells. Moreover, andro could activate LKB1-AMPK signaling. We also demonstrated that Ca2+/calmodulin-dependent protein kinase kinaseβ (CaMKKβ) was not involved in
the regulation of andro on AMPK activation in C666-1 Cells. Conclusions: Andro suppressed proliferation and induced apoptosis of C666-1 cells through regulating the LKB1/AMPK/mTOR signal pathway.
研究领域:
肿瘤学
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药理学
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细胞生物学
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分子生物学
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PubMed
高影响因子
CHEMICO-BIOLOGICAL INTERACTIONS
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2026
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IF 5.2
Jiaqi Li,Zhengxin Lu,Nan Zhang,Xiaowei Zhou,Yuanbiao Ma,Jia-qi Li,Yimu Zhang,Zhewen Deng,Na Lin,Peng Yue,Yilin Yang,Qi Zhang,Bo Ma
Andrographolide (Andro), the primary bioactive compound of Andrographis paniculata , has known bioactivities but also male reproductive toxicity with unclear mechanisms. This study investigated its testicular injury effects and mechanism, focusing on Sertoli cells (SCs) ferroptosis. Toxicity was evaluated in mice and SCs. Mechanisms were probed using RT-qPCR, Western blot, co-immunoprecipitation, and ubiquitination assays. LC-MS/MS assessed tissue distribution. Molecular docking and dynamics simulations characterized the Andro-β-TrCP interaction. The results demonstrated that Andro exposure caused significant testicular atrophy, blood-testis barrier (BTB) disruption, and spermatogenic impairment in mice. Meanwhile, pharmacokinetic analysis revealed SCs as the primary target of Andro-induced testicular damage, showing rapid Andro accumulation that was subsequently detected in sperm and the epididymis. Furthermore, Andro triggered ferroptosis in testicular injury and SCs, marked by increased ROS, MDA, iron overload, and lipid peroxidation. These effects were rescued by the ferroptosis inhibitor deferoxamine. Mechanistically, Andro directly bound to β-TrCP, downregulating its expression and subsequently stabilizing ATF4 by impairing its ubiquitin-mediated degradation. Silencing ATF4 inhibited ferroptosis and restored cell viability upon Andro challenge. The direct Andro-β-TrCP interaction was consistently confirmed by molecular docking, dynamics simulations, and CETSA. This study reveals that Andro triggers SCs ferroptosis by inhibiting β-TrCP-mediated ATF4 ubiquitination and degradation, leading to BTB disruption and spermatogenic impairment. These findings provide a theoretical basis for optimizing clinical application of Andro in the future.
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PubMed
高影响因子
CARBOHYDRATE POLYMERS
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2025
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IF 12.5
Xiaoyi Zhang,Peixia Luo,Jiaming Wang,Lei Yang,Zipei Pang,Shufeng Chen,Yi Zhou,Linghao Qin
Cellulose derivatives play important roles in the development of pharmaceutical oral solid formulations. Owing to their high molecular weight and functional groups, these polymers can interact with water-insoluble drug crystals, influencing not only the drug's physicochemical properties but also its absorption efficiency. In this study, an anticrystallization experiment was designed to compare the inhibitory effects of cellulose derivatives (methylcellulose (MC), hydroxypropyl cellulose (HPC) and hydroxypropyl methyl cellulose (HPMC)) with those of polyvinylpyrrolidone (PVP) and poloxamer (F68) on the crystallization of model drugs (andrographolide, AG). Both in vitro characterization experiments and in vivo pharmacokinetic studies were conducted to evaluate the interaction patterns between andrographolide crystals and polymers. The results indicated that cellulose derivatives exhibited stronger anticrystallization effects, with HPMC showing the most pronounced interaction with drug crystals among all the tested polymers. HPMC significantly prolonged the crystallization time and increased the degree of supersaturation. By adsorbing onto specific crystal surfaces, HPMC was able to modulate the crystal growth orientation, reduce the contact angle, and improve the wettability of drug crystals. Furthermore, andrographolide crystals adsorbed by HPMC exhibited rapid in vitro drug release behavior and upgraded in vivo absorption efficiency, demonstrating its potential to improve the utilization of water-insoluble drugs.
研究领域:
药剂学
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药物化学
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PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2022
·
IF 5.062
Wan Liu,Meng Cheng,Fangying Yuan,Jiaying He,Yulin Feng,Yi Jin,Jianfang Feng,Shilin Yang,Liangxing Tu
Nanocrystal technology is a common strategy to enhance the oral bioavailability of poorly-soluble drugs, and how to enlarge the enhancing ability on oral absorption via nanocrystals has become a pharmaceutical research field. In this study, we selected andrographolide (ADR), a typical poorly-soluble drug, as the model drug, and employed sodium dodecyl sulfate and D-ɑ-Tocopherol polyethylene glycol 1000 succinate copolymer (SDS-TPGS) to construct novel SDS-TPGS modified andrographolide nanocrystals (S-TANs). We found that the particle sizes of SDS/TPGS physical mixture modified nanocrystals (STANs) were about 553.4 ± 4.1 nm , while that of SDS-TPGS modified nanocrystals (S-TANs) were 604.6 ± 5.7 nm. During the production process of nanocrystals, the crystallinity of ADR was slightly decreased. Nanocrystals enhanced the saturation solubility of ADR, and improved oral absorption, C max and AUC 0-∞ of S-TANs was about 2.10 and 1.24 fold increased, STAN about 2.63, 2.97 fold. In a Real-time distribution study, we found the distribution time of andrographolide, SDS and TPGS in SDS/TPGS physical mixture modified nanocrystals system varies widely, while the distribution times of these materials were similar in SDS-TPGS copolymer modified nanocrystals system. These results indicated that modified with functional stabilizer was an efficient strategy to enlarge the enhancing ability on oral absorption of nanocrystals, and synthesized copolymer containing different functional stabilizers showed higher ability on enhancing oral bioavailability than physical mixtures.
研究领域:
药学
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纳米技术
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药物递送系统
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高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2025
·
IF 5.4
ZiLiang Chen,ShuLin Luo,JingLu Hu,Xu Zhan,Yanlin Tan,Jing Leng,BoJie Lin
Ethnopharmacological Relevance Andrographis paniculata (Burm.f.) Wall. ex Nees has been used in Thai traditional medicine for topical hair growth promotion. This study investigates andrographolide(AP), a major bioactive compound from Andrographis paniculata, and its underlying mechanism. Aim of the Study To evaluate the effect of AP on hair follicle growth and its regulation via the Wnt/β-catenin pathway. Materials and Methods Mouse vibrissae and human hair follicles were cultured with AP (0–10μM) or minoxidil (10 μM). Hair shaft elongation and anagen duration were recorded. In vivo, depilated C57BL/6 mice received topical AP (1 or 5 mg/mL), with minoxidil as control. Follicular morphology was assessed by H&E staining; Ki67 expression was used to evaluate proliferation. Wnt/β-catenin signaling was analyzed by qRT-PCR and Western blot. Molecular docking was performed to assess potential interactions between AP and key pathway proteins. Results AP significantly promoted hair shaft elongation and prolonged the anagen phase. At 5 μM, its efficacy was comparable to 10 μM minoxidil. In vivo, AP increased follicular density and Ki67-positive cells. Mechanistically, it upregulated Wnt family member 10b (Wnt10b), β-catenin, and lymphoid enhancer-binding factor 1 (LEF1), indicating activation of the canonical Wnt/β-catenin signaling pathway. Molecular docking analysis indicated that AP may bind to Glycogen Synthase Kinase 3 Beta(GSK3β) with a favorable energy of -8.4 kcal/mol. Conclusions AP, derived from Thai traditional hair care, promotes hair growth via follicular proliferation and Wnt/β-catenin activation. In silico data hint at GSK3β as a putative target, offering a mechanistic lead. This supports its development as a natural alopecia therapeutic, pending further validation.
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高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2026
·
IF 6
Xiao Fan,Ruotong Ouyang,Yujia Huo,Xiaochen Wang,Sisi Tan,Miao Wei,Yunfei Li,Yanyu Pu,Junqin Lei,Liwen Peng,Yijing Zhou,Hong Li
ADR-NPs showed sustained release and acceptable short-term stability. • ADR-NPs showed preliminary short-term ocular and systemic tolerability. • ADR-NPs enhanced cellular and RGC protection relative to dose-matched free ADR. • ADR-NPs attenuated mitochondrial dysfunction and PANoptosis-related changes. • ADR-NPs preserved retinal structure and electrophysiological function after RIR. Acute glaucomatous injury is characterized by abrupt intraocular pressure elevation, retinal ischemia/reperfusion-like stress, and rapid retinal ganglion cell (RGC) degeneration, in which oxidative stress, mitochondrial dysfunction, and regulated cell death play important roles. Emerging evidence further implicates PANoptosis in glaucomatous retinal injury. Andrographolide (ADR) possesses antioxidant and neuroprotective activities, but its poor aqueous solubility and low bioavailability limit its therapeutic application. Here, we developed ADR-loaded poly(lactic-co-glycolic acid) nanoparticles (ADR-NPs) and evaluated their protective effects in oxygen-glucose deprivation/recovery (OGD/R)-injured R28 cells and a rat retinal ischemia/reperfusion (RIR) model. Network pharmacology implicated oxidative stress and programmed cell death pathways in the potential anti-glaucoma effects of ADR. ADR-NPs exhibited favorable physicochemical properties, sustained release, acceptable short-term stability, cytocompatibility. In OGD/R-injured R28 cells, both free ADR and ADR-NPs attenuated oxidative stress, mitochondrial membrane potential loss, and apoptosis-, pyroptosis-, and necroptosis-related alterations, with ADR-NPs providing greater overall protection at matched doses. In the RIR model, ADR-NP pretreatment preserved retinal structure, electrophysiological function, and RGC survival while reducing oxidative stress and retinal PANoptosis-related alterations. ADR-NPs also exhibited acceptable preliminary ocular and systemic tolerability. Collectively, ADR-NPs protect against experimental acute glaucomatous injury by attenuating oxidative stress, mitochondrial dysfunction, and PANoptosis-related alterations, while enhancing the cellular protective effects of ADR. Download: Download high-res image (124KB) Download: Download full-size image
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高影响因子
MOLECULAR PHARMACEUTICS
·
2026
·
IF 4.9
Zhou Yuhao,Yue Zhongqun,Feng Tingting,Zhang Fangxia,Guan Jing,Luo Juanjuan,Tan Yanan,Zhou Ying,Zhu Yue,Wang Zuhua
Gastric cancer is a highly prevalent malignant tumor of the digestive system worldwide. Although andrographolide (AG) and coixol (CX) possess potential anti-gastric cancer effects, their clinical application is restricted by low bioavailability and poor targeting ability. Based on the meridian tropism theory of traditional Chinese medicine and the concept of “integrated drug and carrier”, this study constructed Bletilla striata polysaccharide-vitamin E succinate (BSP-VES) polymeric micelles co-loaded with AG and CX (AG&CX@BSP-VES) for synergistic targeted therapy of gastric cancer. In this study, AG&CX@BSP-VES was first systematically characterized in vitro to clarify its physicochemical properties, drug release behavior and hemolysis profile. Subsequently, using subcutaneous and orthotopic gastric cancer mouse models as research objects, in vitro cellular uptake and in vivo tumor targeting ability efficacy and biological safety of this drug delivery system were further evaluated. Results showed that the micelles were regularly spherical with a particle size of approximately 105 nm, exhibited favorable biological safety and asynchronous differential release characteristics, and could be specifically internalized by cells in vitro (which could be blocked by free BSP). In vivo, the accumulation of micelles in tumor masses was significantly higher than that in normal gastric tissues. Moreover, the cytotoxicity of the micelles against SGC-7901 tumor cells was remarkably higher than that of free AG or CX alone, which was attributed to enhanced cellular drug uptake and the synergistic effect between AG and CX. This study provides novel insights for the precise delivery of active ingredients from traditional Chinese medicine and individualized therapy of gastric cancer.
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高影响因子
JOURNAL OF CHROMATOGRAPHIC SCIENCE
·
2025
·Vol. 63
·期 10
·
IF 1.3
Ren Chang,Sui Xin,Zhang Kunlin,Wang Jingjing,Li Hao,Yang Fenghe,Zhang Mengjun,Zhao Junli,Zhang Yu,Du Guanhua,Han Guang
3,14,19-triacetyl andrographolide (ADA), a derivative of andrographolide, has emerged as a promising anti-inflammatory compound. In the present study, we established a rapid and sensitive ultra-performance liquid chromatography–tandem mass spectrometry method for the quantification of ADA in rat plasma. ADA and celecoxib (internal standard, IS) were separated using an ACQUITY UPLC BEH C18 chromatographic columns with a gradient mobile phase of acetonitrile (containing 0.1% formic acid)/water (containing 0.1% formic acid) at a flow rate of 0.3 mL/min. Quantification was performed using the multiple reaction monitoring transitions to m/z 499.1 → 439.1 for ADA, m/z 381.9 → 361.9 for celecoxib, with plasma samples undergoing liquid–liquid extraction. The method effectively detected ADA in plasma and exhibited excellent linearity (R 2 > 0.9921) over concentrations ranging from 5 to 2000 ng/mL. Both within-run and between-run precision (%RSD) were less than 6.88%, and accuracy ranged from 94.86% to 107.61%. Matrix effects were 87.53% and 112.78%, with recoveries ranging from 98.60% to 104.39%. ADA was proven to be stable under different storage conditions (4°C and −70°C) in plasma. The validated method was successfully applied to determine ADA concentrations in rat plasma. The results demonstrated that ADA exhibited a noticeable improvement in bioavailability compared with andrographolide.
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高影响因子
Materials Today Communications
·
2025
·
IF 4.5
Ding Shen,Jingbin Hao,Siyu Liu,Md Thowfiqure Rahman,Shuaihang Wang,Sameer Hussain Jhatial
Chronic wounds are often aggravated by bacterial infection and prolonged inflammation, presenting major challenges in clinical wound management. To address these issues, a novel 3D-printed multilayer hydrogel was developed, based on a GelMA-PVA dual-network system incorporating graded concentrations of andrographolide (Andro), a phytochemical with proven antibacterial and anti-inflammatory activity. The GelMA component was photocrosslinked, while the PVA network was physically crosslinked via freeze–thaw cycles, forming a robust interpenetrating structure. The hydrogels were characteriazed using FTIR, XPS, SEM, mechanical testing, swelling analysis, and in vitro release and antibacterial assays. The multilayer patches demonstrated tunable swelling capacity (up to 1938 %), excellent tensile strength (up to 46.7 kPa) and compressive strength (up to 94.3 kPa), and a sustained drug release profile. In vitro studies confirmed enhanced L929 fibroblast proliferation and significant antibacterial activity against E. coli and S. aureus , particularly in the gradient Andro-loaded groups. These results suggest that the 3D-printed GelMA-PVA-Andro patches are promising candidates for advanced wound dressings with integrated mechanical, biological, and pharmaceutical functionalities.
研究领域:
生物材料
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组织工程
·
药剂学
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生物医学工程
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微生物学
·
材料科学
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高影响因子
危险品化学品经营许可证（带存储）