Talanta Open
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2025
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IF 3.7
Amna Naz,Sadia Haider,Mavra Rana,Neelum Malik,Attia Afzal,Muhammad Farooq,Muhammad Sarfraz
Oleanolic acid (OA) and apigenin (APG) demonstrate a wide range of pharmacological effects, including antioxidant, anti-inflammatory, antiviral, antidiabetic, hepatoprotective, and cardioprotective activities. Both compounds show anticancer potential and have been used individually to treat various cancer types, creating a rationale for their combined use. However, quantifying both drugs in quality and plasma samples presents challenges due to differences in their physicochemical properties and absorption wavelengths (OA: 210-215 nm, APG: 212, 269, and 337 nm). We developed and validated a novel High-Performance Liquid Chromatography UV detection (HPLC-UV) method to address this problem. Using a C18 column (4.6 mm x 250 mm, packing L1, 5 µm particle size) and a mobile phase of acetonitrile: methanol: tetrahydrofuran: water (60:20:8:12, v/v) with a detection wavelength of 215 nm. The method achieved retention times of 4.7 and 10 minutes for OA and APG in quality samples, and 4.9 and 9.8 minutes in plasma samples, respectively. The plasma sample was prepared by simple protein precipitation step. All validation parameters, including sensitivity, selectivity, precision, accuracy, robustness, and stability, met the required criteria. The validated HPLC-UV bioanalytical method was effectively applied in quantification, stability, and pharmacokinetic studies of co-loaded nanoformulations of OA and APG with particle size 163 nm and entrapment efficiency up to 93 %, establishing it as a promising analytical technique for detecting these anticancer agents in complex matrices such as blood, plasma, and polymeric systems.
研究领域:
药理学
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分析化学
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肿瘤学
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DOI
高影响因子
Polymer Chemistry
·
2020
·Vol. 11
·期 36
·5800-5809
·
IF 5.342
Boran Hao,Lu Han,Yuqi Liu,Kan Zhang
Benzoxazine resins have been attracting continuous attention from both academia and industry owing to the property of molecular design flexibility and high performance of their thermoset polymers. However, a reduction in the polymerization temperature, a renewable source and improved thermal and mechanical properties are highly desirable in order to meet the requirements of various applications. Herein, we have synthesized a new bio-based benzoxazine resin showing thermal latent polymerization characteristics from renewable apigenin and furfurylamine. This benzoxazine resin possesses the advantage of long shelf life as do other traditional benzoxazines through its intramolecular hydrogen bonding between the phenolic –OH and the carbonyl. In addition, it can be polymerized via multiple polymerization mechanisms rather than the single polymerization mechanism as reported for other traditional benzoxazines. Moreover, the fully polymerized thermoset derived from this bio-based benzoxazine exhibits a high glass transition temperature of 376 °C, a very high char yield of 66%, and an extraordinarily low heat release capacity of 20.2 J (g K)−1. Its excellent thermal performance and flame resistance evidence its great potential applications in fields where high-performance materials are needed.
研究领域:
材料科学
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高分子化学
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可持续化学
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热工程
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DOI
高影响因子
Evidence-based Complementary and Alternative Medicine
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2022
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IF 2.65
Yihua Shi,Kai Lian,Jiguang Jia
Osteosarcoma (OS) is a prevalent primary malignant bone tumor that commonly occurs in children and adolescents. Apigenin (4′,5,7-trihydroxyflavone) is one of the most researched phenolic compounds that exhibits antitumor effects in several cancers. The aim of the current study was to investigate the effect and underlying mechanisms of apigenin on OS. To address this, OS cells (SOSP-9607) were treated with different concentrations of apigenin. The proliferation, migration, invasion, stem-like properties, and Warburg effect of apigenin-treated OS cells were evaluated. Apigenin was found to suppress the proliferation of SOSP-9607 cells and inhibit epithelial-mesenchymal transition, as indicated by decreased number of migrated and invaded cells, decreased protein expression of vimentin, and increased protein expression of E-cadherin. Additionally, apigenin suppressed tumorsphere formation and reduced the proportion of SOSP-9607 cells with positive expression of the stem cell-related markers Nanog and OCT-4. Apigenin inhibited the Warburg effect in SOSP-9607 cells, as demonstrated by decreased glucose and lactic acid levels, increased citrate and ATP levels, and downregulation of GLUT1, HK1, and LDHA, which are metabolism-related enzymes related to the Warburg effect. Moreover, apigenin inhibited the phosphorylation of PI3K, Akt, and mTOR in SOSP-9607 cells. Collectively, these results indicate that apigenin suppresses the Warburg effect and stem-like properties in SOSP-9607 cells, which may be mediated by PI3K/Akt/mTOR signaling, thus, providing a novel strategy for OS treatment.
研究领域:
肿瘤学
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分子生物学
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细胞生物学
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癌症研究
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DOI
PubMed
高影响因子
FOOD CHEMISTRY
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2025
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IF 9.8
Yufei Liu,Ziliang Li,Shuaijun Lu,Shang Gao,Mengting Xu,Ze Yuan,Yue Li,Yiqiao Gao,Jingfang Shangguan,Xia Xiang
Apigenin (Ap) is a bioactive compound, but its application is limited by poor solubility, stability, and bioavailability. This study developed flaxseed gum (FG) and its oligosaccharides (FGOS)-coated zein nanoparticles for Ap delivery (FG/Zein@Ap and FGOS/Zein@Ap). Compared to FG/Zein@Ap, FGOS/Zein@Ap exhibited smaller size, higher zeta potential, encapsulation efficiency (~71.70 %), and loading capacity (~7.66 %) as evidenced by dynamic light scattering, Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), and transmission electron microscopy (TEM). FGOS/Zein@Ap also provided better stability of Ap under various conditions, thereby promoting stronger in vitro antioxidant activity, raising bioaccessibility and bioavailability. Molecular docking and molecular dynamics simulations revealed that FGOS interacted more strongly with zein, primarily through hydrogen bonding and van der Waals forces. This interaction provided greater binding stability throughout the simulation period, compared to FG. This study enhances the understanding of FG and FGOS, providing valuable insights for oligosaccharides-based delivery systems for hydrophobic bioactives.
研究领域:
食品科学
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分子生物学
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DOI
PubMed
高影响因子
BIOCHEMICAL PHARMACOLOGY
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2015
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IF 5.009
Wan Li,Hua Sun,Xingwang Zhang,Huan Wang,Baojian Wu
Efflux transport is a critical determinant to the pharmacokinetics of sulfate conjugates. Here we aimed to establish SULT1A3 stably transfected HEK293 cells, and to determine the contributions of BCRP and MRP transporters to excretion of chrysin and apigenin sulfates. The cDNA of SULT1A3 was stably introduced into HEK293 cells using a lentiviral vector , generating a sulfonation active cell line (i.e., SULT293 cells). Identification of sulfate transporters was achieved through chemical inhibition (using chemical inhibitors) and biological inhibition (using short-hairpin RNAs (shRNAs)) methods. Sulfated metabolites were rapidly generated and excreted upon incubation of SULT293 cells with chrysin and apigenin. Ko143 (a selective BCRP inhibitor) did not show inhibitory effects on sulfate disposition, whereas the pan-MRP inhibitor MK-571 caused significant reductions (38.5–64.3%, p < 0.001) in sulfate excretion and marked elevations (160–243%, p < 0.05) in sulfate accumulation. Further, two efflux transporters (BCRP and MRP4) expressed in the cells were knocked-down by shRNA-mediated silencing. Neither sulfate excretion nor sulfate accumulation was altered in BCRP knocked-down cells as compared to scramble cells. By contrast, MRP4 knock-down led to moderate decreases (17.1–20.6%, p < 0.05) in sulfate excretion and increases (125–135%, p < 0.05) in sulfate accumulation. In conclusion, MRP4 was identified as an exporter for chrysin and apigenin sulfates. The SULT1A3 modified HEK293 cells were an appropriate tool to study SULT1A3-mediated sulfonation and to characterize BCRP/MRP4-mediated sulfate transport.
研究领域:
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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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2022
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IF 6.51
Tingxuan Yan,Haili Wang,Xingfang Song,Tingyuan Yan,Yuwen Ding,Kang Luo,Juan Zhen,Gui He,Libin Nian,Shuangshou Wang,Zhixiang Wang
Flavonoids have many positive pharmacological properties, such as antioxidant, antitumor, and anti-inflammatory activities. However, factors such as low water solubility and low dissolution rate limit their use. To overcome their poor solubility, carrier-free apigenin (API) microparticles and nanoparticles were prepared using three types of antisolvent precipitation technologies: supercritical antisolvent (SCF) technology, ultrasonic-assisted liquid antisolvent (UAL) technology, and high-pressure homogenization (HPH) technology. All three technologies can produce uniform tiny particles. However, the API particles obtained using these different techniques show subtle differences in terms of physical and chemical properties and biological activity. The preparation, characterization, and potential use of API microparticles and nanoparticles to improve in vitro release were studied. The resulting API particles were investigated and compared using Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffraction, and scanning electron microscopy. We determined the optimum conditions for SCF, UAL, and HPH technologies to produce API microparticles and nanoparticles. The antioxidant and antitumor properties of the API particles were also investigated. The results demonstrated that the reduced particle size of the APIs prepared via SCF, UAL, and HPH technologies contributed to the enhanced dissolution rate, which in turn enhanced API bioactivity.
研究领域:
药学
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纳米技术
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药理学
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产品关联
DOI
PubMed
高影响因子
Food Bioscience
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2026
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IF 6.2
Longfei Lv,Sijie Zhang,Bing Huang,Li Ren,Jie Zhang,Zheng Ma
Cigarette consumption remains a preeminent global public health concern, as prolonged exposure to cigarette smoke is fundamentally implicated in the etiology of chronic pulmonary diseases and the manifestation of various malignancies. Apigenin, a bioactive dietary flavonoid widely distributes in botanical sources such as celery, demonstrates significant histoprotective effect. Nevertheless, the underlying mechanism governing apigenin's ability to counteract incipient pulmonary injury induced by cigarette smoke extract (CSE) remains to be delineated. By employing a novel CSE exposure system to establish reproducible in vivo and in vitro injury models, this study demonstrated that apigenin administration dose-dependently attenuates pulmonary apoptosis, as evidenced by the restoration of the Bax/Bcl-2 ratio and the suppression of Caspase-3 activation. Furthermore, apigenin treatment reversed the CSE-induced downregulation of PPARγ and its downstream effector, FATP2. Apigenin also restored intestinal mucosal integrity, promoted the enrichment of the probiotic Clostridia vadinBB60 group, and elevated intestinal difluprednate levels, which strongly correlated with increased glucocorticoid receptor (GR) expression in lung tissue. Mechanistically, apigenin facilitated the recruitment of PGC1α to PPARγ, thereby promoting PPARγ nuclear translocation and subsequent FATP2 activation in CSE-challenged MLE-12 cells. In RAW264.7 macrophages, difluprednate mediated GR nuclear translocation, subsequently suppressing the mRNA expression of the pro-inflammatory cytokines IL-1β and IL-6. Collectively, these findings identify apigenin as a dual-pathway modulator that bridges PPARγ/FATP2-mediated metabolic homeostasis with GR-dependent anti-inflammatory signaling, highlighting its therapeutic potential against smoking-related pulmonary dysfunction and supporting its application as a functional food intervention.
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DOI
高影响因子
Frontiers in Immunology
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2026
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IF 5.9
Ruixue Dai,Liangliang Cao,Jiahui Ren,Jingru Liu,Kexin Zhu,Peidong Chen,Weifeng Yao,Xuelong Zhao,Beihua Bao,Li Zhang
Background Excessive inflammation mediated by macrophages impedes wound healing following surgical drainage of perianal abscess, a common yet challenging condition in colorectal surgery. Cayratia japonica ointment (CJO) has shown clinical efficacy, but its active immunomodulatory constituents and mechanisms remain unclear. Methods We evaluated the anti-inflammatory effects of seven CJO-derived flavonoids in LPS-stimulated RAW264.7 macrophages. Skin pharmacokinetics were assessed in mice, and therapeutic efficacy was tested in a rat postoperative perianal abscess model. Molecular mechanisms were investigated via Western blot, RT-qPCR, and molecular docking. Results Pharmacokinetic analysis revealed that apigenin exhibited the highest transdermal exposure among all detected components. In vitro , apigenin significantly suppressed LPS-induced production of IL-6, TNF-α, and IL-1β in RAW 264.7 cells. In vivo , apigenin treatment markedly reduced serum levels of these pro-inflammatory cytokines, attenuated inflammatory cell infiltration, and promoted collagen deposition at the wound site. Mechanistically, apigenin downregulated both the phosphorylation and total protein levels of JAK1 and STAT3, suggesting functional modulation of the JAK1/STAT3 signaling pathway. Conclusion Apigenin may contribute to observed biological effects of CJO that promotes wound healing by attenuating macrophage-driven inflammation through potential modulation of the JAK1/STAT3 signaling pathway, offering a promising natural immunomodulator for postoperative wound management.
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PubMed
高影响因子
Experimental and Therapeutic Medicine
·
2017
·Vol. 14
·期 6
·5345-5354
·
IF 1.261
Yang Liu,Xiuheng Liu,Lei Wang,Yang Du,Zhiyuan Chen,Hui Chen,Jia Guo,Xiaodong Weng,Xiao Wang,Ming Wang,Zhishun Wang
The aim of the present study was to investigate the effect and possible mechanism of apigenin on renal ischemia-reperfusion (I/R) injury in rats, as well as in in vitro experiments. In total, 36 rats were subjected to 45 min of renal ischemia, with or without treatment prior to ischemia with different concentrations of apigenin (2, 10 and 50 mg/kg) administered intravenously. All rats were sacrificed at 24 h after I/R injury. The serum creatinine (Cr) and blood urea nitrogen (BUN) levels were analyzed, and histological examination was conducted. In addition, the expression levels of B‑cell lymphoma 2 (Bcl‑2) and Fas/Fas ligand (FasL) were detected by immunohistochemistry, reverse transcription‑quantitative polymerase chain reaction and western blot analysis. For in vitro experiments, the NRK‑52E cell line was employed. The viability, apoptosis and expression levels of Fas, FasL and Bcl‑2 were examined in the culture of NRK‑52E cells following the I/R. The results indicated that apigenin significantly decreased the levels of serum Cr and BUN induced by renal I/R, demonstrating an improvement in renal function. The histological evidence of renal damage associated with I/R was also mitigated by apigenin in vivo. Furthermore, apigenin increased the cell viability and decreased cell apoptosis in the culture of NRK52E after I/R in vitro. Compared with the I/R group, the expression of Bcl‑2 was upregulated and the expression levels of Fas and FasL were downregulated by apigenin at the mRNA and protein levels in vivo and in vitro. In conclusion, apigenin appeared to increase the expression of Bcl‑2 and reduce Fas/FasL expression in renal I/R injury, providing evident protection against renal I/R injury in rats.
研究领域:
药理学
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肾病学
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分子生物学
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DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
·
2024
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IF 4.2
Yufang Ma,Zhenming Ma,Yiyuan Zhang,Chunyun Luo,Puxin Huang,Jing Tong,Hong Ding,Honghui Liu
Apigenin and baicalein are structurally related flavonoids that have been reported to have multiple pharmacological activities. The aim of this study was to investigate the protective effects and potential mechanisms of apigenin and baicalein in D-galactose-induced aging rats. First, apigenin and baicalein showed remarkable antioxidant activity and anti-glycation activity in vitro. Secondly, the protective effects of apigenin and baicalein on aging rats were investigated. We found that apigenin and baicalein supplementation significantly ameliorated aging-related changes such as declines in the spatial learning and memory and histopathological damage of the hippocampus and thoracic aorta. In addition, our data showed that apigenin and baicalein alleviated oxidative stress as illustrated by decreasing MDA level, increasing SOD activity and GSH level. Further data showed that they significantly reduced the accumulation of advanced glycation end products (AGEs), inhibited the expression of RAGE, down-regulated phosphorylated nuclear factor (p–NF–κB (p65)). Our results suggested that the protective effects of apigenin and baicalein on aging rats were at least partially related to the inhibition of AGEs/RAGE/NF-κB pathway and the improvement of oxidative damage. Overall, apigenin and baicalein showed almost equal anti-aging efficacy. Our results provided an experimental basis for the application of apigenin and baicalein to delay the aging process.
研究领域:
药理学
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衰老研究
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神经科学
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心血管研究
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产品关联
DOI
PubMed
高影响因子
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