CURRENT ISSUES IN MOLECULAR BIOLOGY
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2025
·Vol. 47
·期 6
·450
·
IF 3
Qiming Miao,Lu Sun,Jiayuan Wu,Xinyue Zhu,Juer Liu,Roger Ruan,Guangwei Huang,Shengquan Mi,Yanling Cheng
The advancement of modern lifestyles has precipitated excessive consumption of energy-dense foods, driving the escalating global burden of lipid metabolism dysregulation-related pathologies—including obesity, type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and cardiovascular disorders—which collectively pose a formidable challenge to global public health systems. The almond hull, as a by-product of almond processing, is rich in polyphenolic compounds with demonstrated antioxidant, anti-inflammatory, and lipid-lowering potential, though its precise hypo-lipidemic mechanisms remain elusive. In this study, polyphenols were extracted from almond hulls using 50% ethanol with ultrasound-assisted extraction, followed by preliminary purification via solvent partitioning. The ethyl acetate fraction was analyzed by liquid chromatography–mass spectrometry (LC-MS). Network pharmacology and molecular docking were employed to investigate the interactions between key bioactive constituents (e.g., quercetin, baicalein, and kaempferol) and targets in lipid metabolism-related pathways. Molecular dynamics (MD) simulations further evaluated the stability of the lowest-energy complexes. Results revealed that the ethyl acetate fraction exhibited potent pancreatic lipase inhibitory activity (IC50 = 204.2 µg/mL). At 0.1 mg/mL after 24 h treatment, it significantly reduced free fatty acids (FFAs)-induced intracellular triglyceride accumulation (p< 0.01) and enhanced cellular antioxidant capacity. Network pharmacology and in vitro studies suggest almond hull extract modulates PI3K-AKT signaling and improves insulin resistance, demonstrating lipid-lowering effects. These findings support its potential in functional foods and pharmaceuticals, though further in vivo validation and mechanistic investigations are required.
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PubMed
高影响因子
BIOGERONTOLOGY
·
2025
·Vol. 26
·期 5
·1-24
·
IF 4.1
Chen Wendi,Liu Shuang,Xu Guoqiang,Liu Xin,Shi Yuxuan,Wang Guolong,Ning Yunna,Lu Zhiming,Cao Yongzhi,Zhao Yueran
Zuogui pill (ZGP) and Yougui pill (YGP) are classical kidney-tonifying formulas in Traditional Chinese Medicine, widely used clinically but with their potential to delay ageing and improve ageing biomarkers remaining unclear. This study combined network pharmacology and Caenorhabditis elegans models to investigate the anti-ageing effects and mechanisms of ZGP and YGP. Both formulas significantly extended lifespan (ZGP dose-dependently at 5–20 mg/mL; YGP at 20 mg/mL) and improved ageing biomarkers, as evidenced by enhanced motility, reduced lipofuscin accumulation and endogenous ROS levels, and increased resistance to heat and oxidative stress. Network analysis identified quercetin and kaempferol as the top-ranked shared active components. Subsequent experimental validation demonstrated that kaempferol (0.05–0.2 mM) replicated these pro-longevity effects and was shown to act by inducing mitophagy: it triggered an initial decrease followed by a long-term increase in mitochondrial content, concomitant with upregulated expression of mitophagy genes. Crucially, the lifespan-extending effects of kaempferol, ZGP, and YGP were completely abolished in bec-1 and pink-1 null mutants. This study establishes that ZGP and YGP delay ageing and improve ageing biomarkers in C. elegans by activating BEC-1/PINK-1-dependent mitophagy. Kaempferol was identified as a major active component mediating this effect, highlighting a key mechanism for the pro-longevity properties of these traditional formulas.
研究领域:
中医
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药理学
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衰老研究
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分子生物学
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线粒体生物学
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PubMed
高影响因子
Analytical Methods
·
2021
·Vol. 13
·期 7
·925-932
·
IF 2.896
Yun Sun,Xiaoying Yin,Lin Zhang,Menghui Cao
Novel photo-responsive hollow structured molecularly imprinted polymers (PHMIPs) were developed as a selective sorbent to recognize and separate analytes in complex samples. The PHMIPs were prepared using kaempferol (KAE) as the template, 4-[(4-methacryloyloxy) phenylazo] benzenesulfonic acid as a photo-responsive functional monomer, and hollow SnO2 (Ho-SnO2) as the support via free radical polymerization. The structure and physical properties of the developed polymers were characterized using different nano structural techniques and spectroscopy. Under alternating irradiation at 365 and 440 nm, the PHMIPs could release and uptake KAE, indicating that the template molecules can be easily bound to recognition sites and released back into solution. From adsorption experiments, the binding properties were evaluated, and the maximal adsorption capacity of the PHMIPs was 11.04 mg g−1. Furthermore, the developed PHMIPs showed high selectivity towards KAE compared to other compounds. Subsequently, the materials were successfully applied to the photo-controlled extraction of KAE from sea buckthorn leaves. The recoveries for KAE were higher than 90% and relative standard deviation values were between 1.81% and 2.53%, indicating the potential of the developed materials for use in extracting KAE from complex samples.
研究领域:
材料科学
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分析化学
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药学
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PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2023
·
IF 3.8
Huiling Zhou,Chenxin Duan,Huimin Qin,Chaonan Huang,Jingxuan Hou,Yanming Chen,Jin Zhu,Cangcang Xu,Jian Jin,Tao Zhuang
ABSTRACT Palbociclib (PAL), a highly selective inhibitor of cell cycle protein-dependent kinases (CDK) 4/6, is primarily used for treating advanced breast cancer. However, the use of PAL has been limited by its poor tabletability and dose-related toxic side effects. In this study, to improve the tabletability of PAL and reduce its effective dose, a flavonoid–kaempferol (KAE) was selected as the coformer to synthesize cocrystal with PAL. The novel cocrystal PAL-KAE was prepared by antisolvent cocrystallization and characterized by various techniques including X-ray diffraction (SCXRD and PXRD), thermal analysis (DSC and TG), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), Hirshfeld surface (HS), HOMO−LUMO analysis, and molecular electrostatic potential (MEP). Powder compaction experiments indicated that PAL-KAE cocrystal significantly improved the tabletability of PAL. The cytotoxicity test suggested that PAL-KAE also exerted synergistic antitumor effect against human ovarian cancer cell line OVCAR3 in MTT assay. Docking results indicated that PAL-KAE had lower binding energy with CDK 6 than PAL. Furthermore, the cocrystal PAL-KAE exhibits excellent stability in long-term testing, accelerated testing and stressing test. This paper provides a promising strategy for improving the tabletability of PAL and enhancing its anticancer activity, thus reducing the dose-related side effects of PAL.
研究领域:
药学
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材料科学
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癌症研究
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药物递送
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高影响因子
RSC Advances
·
2022
·Vol. 12
·期 28
·18115-18126
·
IF 4.036
Xiaoya Tao,Hang Shi,Ailing Cao,Luyun Cai
In this research, ovalbumin (OVA) and sodium alginate (SA) were used as the materials to prepare an OVA–SA composite carrier, which protected and encapsulated the hydrophobic kaempferol (KAE) and the hydrophilic tannic acid (TA) (OVA–SA, OVA–TA–SA, OVA–KAE–SA, and OVA–TA–KAE–SA). Results showed that the observation of small diffraction peaks in carriers proved the successful encapsulation of KAE/TA. The protein conformation of the composite nanoparticles changed. OVA–TA–SA composite nanoparticles had the highest α-helix content and the fewest random coils, so the protein structure of it had the strongest stability. OVA–TA–KAE–SA composite nanoparticles had the strongest system stability and thermal stability, which might be due to the synergistic effect of the two polyphenols, suggesting the encapsulation of KAE/TA increased the system stability and the thermal stability of OVA–SA composite nanoparticles. Additionally, the composite nanoparticles were endowed with antioxidant ability and antibacterial ability (against Staphylococcus aureus and Escherichia coli) in the order OVA–TA–SA > OVA–TA–KAE–SA > OVA–KAE–SA based on the difference in antibacterial diameter (D, mm) and square (S, mm2), indicating that polyphenols enhanced the antibacterial and antioxidant ability of OVA–SA composite nanoparticles, and the enhancement effect of TA was stronger than that of KAE. These results provide a theoretical basis for the application of OVA–SA composite nanoparticles in the delivery of bioactive compounds.
研究领域:
纳米技术
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食品科学
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药学
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生物技术
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PubMed
高影响因子
PHYTOMEDICINE
·
2023
·
IF 7.9
Li Xiao,Guangfu Xu,Silong Chen,Yumin He,Fan Peng,Chengfu Yuan
Background Alcoholic liver disease (ALD) is characterized by the disturbance of bile acids homeostasis, which further deteriorates ALD. Bile acid metabolism and its related signal molecules have become new therapeutic targets for alcoholic liver disease. This study aimed to investigate the impact of kaempferol (KAE) on ALD and elucidate its underlying mechanisms. Methods C57BL/6 N mice were utilized to establish Binge-on-Chronic alcohol exposure mice model. KAE was administered as an interventional drug to chronic alcohol-fed mice for four weeks to assess its effects on liver damage and bile acid metabolism. And Z-Guggulsterone (Z-Gu), a global FXR inhibitor, was used to investigate the impact of intestinal FXR-FGF15 signal in ALD mice. Additionally, intestinal epithelial cells were exposed to alcohol or specific bile acid to induce the damage of FXR activity in vitro. The dual luciferase activity assay was employed to ascertain the interplay between KAE and FXR activity. Results The results indicated that KAE treatment exhibited a significant hepatoprotective effect against chronic alcohol-fed mice. Accompanied by the intestinal FXR activation, the administration of KAE suppressed hepatic bile acid synthesis and promoted intestinal bile acid excretion in chronic ALD mice. And the notable alterations in total bile acid levels and composition were observed in mice after chronic alcohol feeding, which were reversed by KAE supplementation. And more, the protective effects of KAE on ALD mice were deprived by the inhibition of intestinal FXR activation. In vitro experiments demonstrated that KAE effectively activated FXR-FGF15 signaling, mitigated the damage to FXR activity in intestinal epithelial cells caused by alcohol or specific bile acids. Additionally, luciferase activity assays revealed that KAE directly promoted FXR expression, thereby enhancing FXR activity. Conclusion KAE treatment inhibited hepatic bile acids synthesis, maintained bile acids homeostasis in ALD mice by directly activating intestinal FXR-FGF15 signaling, which effectively alleviated liver injury induced by chronic alcohol consumption.
研究领域:
药理学
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肝病学
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分子生物学
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胃肠病学
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PubMed
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
·
2013
·
IF 3.535
Kai Zhang,Ge Song,Yinfeng Li,Xianli Wu,Kunjing Li,Baoxian Ye
A facile and highly sensitive electrochemical sensor for kaempferol was fabricated by doping polyvinyl pyrrolidone cladding quantum dots to the carbon paste electrode. The quantum dots were characterized with transmission electron microscopy , ultraviolet spectrum and infrared spectrum. The electrochemical behaviors and kinetic parameters of kaempferol were investigated on the sensor by cyclic voltammetry and chronocoulometry in NaAc–HAc (pH 4.4). The proposed sensor accelerated the redox processes of kaempferol obviously, and the oxidation currents were linearly relationship with kaempferol in two concentration intervals: one was 6.0 × 10 −8 –2 × 10 −6 mol/L and the other was 5.0 × 10 −6 –2.5 × 10 −5 mol/L. The quantification limit obtained by square wave voltammetry was 6.0 × 10 −8 mol/L. Merits such as extreme simplicity, low cost, good sensitivity, high sensitivity, good stability and reproducibility made it an excellent electrochemical sensor for kaempferol. A new electroanalytical method for kaempferol was proposed and used for determination of kaempferol in tablets with satisfactory results.
研究领域:
分析化学
·
电化学
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高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2024
·
IF 6.9
Zhongyuan Zhang,Wenshu Xu,Zhenhua Zhang,Xiaoxue Chen,Hui Jin,Ningning Jiang,Hui Xu
This study was to investigate the potential mechanisms of treatment with metformin (Met) combined with kaempferol (Kae) against postmenopausal osteoporosis. Experiments were conducted in both ovariectomy (OVX)-induced osteoporosis rats and in vitro using RAW264.7 cells, MC3T3-E1 cells, and HUVECs. Results demonstrated the therapeutic effect of Met combined with Kae on osteoporosis. In vivo, Kae alone and in combination with Met treatments enhanced tibial trabecular microstructure, bone mineral density (BMD), and mechanical properties in OVX rats without causing hepatotoxicity and nephrotoxicity. It also reduced bone resorption markers (CTX-1 and TRAP) and increased the bone formation marker (PINP) level in the serum of OVX rats. The expression of bone resorption marker TRAP was reduced, while bone formation markers Runx2 and ALP were enhanced in the bone tissue of OVX rats. Furthermore, Met combined with Kae also promoted the expression of angiogenesis-related markers CD31 and VEGF in OVX rats. In vitro, MC3T3-E1s cells treated with Met combined with Kae showed higher expression of ALP, Runx2, and VEGF. Interestingly, the treatment did not directly promote HUVECs migration and angiogenesis, but enhanced osteoblast-mediated angiogenesis by upregulating VEGF levels. Additionally, Met combined with Kae treatment promoted VEGF secretion in MC3T3-E1, and activated the Notch intracelluar pathway by upregulating HES1 and HEY1 in HUVECs. Meantime, their stimulation on CD31 expression were inhibited by DAPT, a Notch signaling inhibitor. Overall, this study demonstrates the positive effects of Met combined with Kae on osteoporotic rats by promoting osteogenesis-angiogenesis coupling, suggesting their potential application in postmenopausal osteoporosis.
研究领域:
药理学
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骨科
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分子生物学
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细胞生物学
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PubMed
高影响因子
JOURNAL OF POLYMERS AND THE ENVIRONMENT
·
2025
·
IF 5
Roopashree R.,Gupta Anchal,Rathore Mahendra Singh,Sharma Kamini,Chinnathambi Arunachalam,Alharbi Sulaiman Ali,Ramar Mohankumar,Kalaiarasi Giriraj,Thangavelu Indumathi,Suriyaprakash Jagadeesh
Oral cancer remains a significant health challenge, necessitating innovative therapeutic strategies to enhance treatment efficacy and minimize side effects. This study investigates the potential of kaempferol-loaded zein nanoparticles (KZNPs) for this purpose. Kaempferol, a flavonoid with anticancer properties, has poor water solubility, limiting its effectiveness. Zein nanoparticles (ZNPs) offer a promising delivery system for such bioactive compounds. UV-Vis spectroscopy identified Kaempferol’s absorption peaks at 347 and 253 nm, which shifted to 338 nm when encapsulated in ZNPs, indicating a change in π–π* conjugation. Dynamic light scattering (DLS) and scanning electron microscopy (SEM) confirmed that sodium caseinate (SC) stabilizes ZNPs, resulting in spherical particles with optimal size and stability. Fourier transform infrared (FTIR) spectroscopy suggested enhanced hydrogen bonding between Kaempferol and zein. Differential scanning calorimetry (DSC) revealed the absence of Kaempferol’s crystalline peaks in KZNPs. The encapsulation efficiency (EE) was 98.39%, and drug release studies showed a controlled release of 79% kaempferol over 8 h. In vitro assays demonstrated that KZNPs significantly increased Kaempferol’s cytotoxicity against PCI-13 oral cancer cells without affecting normal NIH3T3 cancer cells. Overall, these results demonstrate that our KZNPs enhanced biocompatibility and anticancer properties for oral cancer cells.
研究领域:
药学
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肿瘤学
·
纳米医学
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高影响因子
Food & Function
·
2021
·Vol. 12
·期 18
·8351-8365
·
IF 5.396
Yonglu Li,Xin Yu,Yaxuan Wang,Xiaodong Zheng,Qiang Chu
Lung cancer has been threatening human health worldwide for a long time. However, the clinic therapies remain unsatisfactory. In this study, the anti-adenocarcinoma lung cancer A549 cell line abilities of Tetrastigma hemsleyanum tuber flavonoids (THTF) were evaluated in vivo, and isobaric tags for relative and absolute quantification (iTRAQ)-based proteomic analysis was conducted to detect the protein alterations in THTF-treated solid tumors. The differentially expressed proteins were related to the cytoskeleton and mostly accumulated in the calcium signaling pathway. The in vitro study illustrated that 80 μg mL−1 THTF significantly suppressed cellular viability to approximately 75% of the control. Further results suggested that kaempferol-3-O-rutinoside (K3R), the major component of THTF, effectively triggered cytoskeleton collapse, mitochondrial dysfunction and consequent calcium overload to achieve apoptosis, which remained consistent with proteomic results. This study uncovers a new mechanism for THTF anti-tumor ability, and suggests THTF and K3R as promising anti-cancer agents, providing new ideas and possible strategies for future anti-lung cancer prevention and therapy.
研究领域:
肿瘤学
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药理学
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分子生物学
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细胞生物学
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蛋白质组学
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PubMed
高影响因子
FITOTERAPIA
·
2014
·
IF 2.216
Yan Xie,Huilin Luo,Jingze Duan,Chao Hong,Ping Ma,Guowen Li,Tong Zhang,Tao Wu,Guang Ji
Aim Total flavones of Hippophae rhamnoides L. (TFH) have a clinical use in the treatment of cardiac disease. The pharmacological effects of TFH are attributed to its major flavonoid components, isorhamnetin , kaempferol , and quercetin . However, poor oral bioavailability of these flavonoids limits the clinical applications of TFH. This study explores phytic acid (IP 6 ) enhancement of the oral absorption in rats of isorhamnetin, kaempferol, and quercetin in TFH. Methods In vitro Caco-2 cell experiments and in vivo pharmacokinetic studies were performed to investigate the effects of IP 6 . The aqueous solubility and lipophilicity of isorhamnetin, quercetin, and kaempferol were determined with and without IP 6 , and mucosal epithelial damage resulting from IP 6 addition was evaluated by MTT assays and morphology observations. Results The P app of isorhamnetin, kaempferol, and quercetin was improved 2.03-, 1.69-, and 2.11-fold in the presence of 333 μg/mL of IP 6 , respectively. Water solubility was increased 22.75-, 15.15-, and 12.86-fold for isorhamnetin, kaempferol, and quercetin, respectively, in the presence of 20 mg/mL IP 6 . The lipophilicity of the three flavonoids was slightly decreased, but their hydrophilicity was increased after the addition of IP 6 in the water phase as the logP values of isorhamnetin, kaempferol, and quercetin decreased from 2.38 ± 0.12 to 1.64 ± 0.02, from 2.57 ± 0.20 to 2.01 ± 0.04, and from 2.39 ± 0.12 to 1.15 ± 0.01, respectively. The absorption enhancement ratios were 3.21 for isorhamnetin, 2.98 for kaempferol, and 1.64 for quercetin with co-administration of IP 6 (200 mg/kg) in rats. In addition, IP 6 (200 mg/kg, oral) caused neither significant irritation to the rat intestines nor cytotoxicity (400 μg/mL) in Caco-2 cells. Conclusions The oral bioavailability of isorhamnetin, kaempferol, and quercetin in TFH was enhanced by the co-administration of IP 6 . The main mechanisms are related to their enhanced aqueous solubility and permeability in the presence of IP 6 . In summary, IP 6 is a potential absorption enhancer for pharmaceutical formulations that is both effective and safe.
研究领域:
药理学
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药剂学
·
营养保健品
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PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2022
·
IF 8.025
Xiaoya Tao,Hang Shi,Ailing Cao,Luyun Cai
In this research, ovalbumin (OVA) and sodium alginate (SA) were used as the materials to prepare OVA-SA composite carriers, which protected and encapsulated the hydrophobic kaempferol (KAE) and the hydrophilic tannic acid (TA). To achieve the purpose of targeted delivery, the TA-Fe 3+ coating film was prepared. Results showed that the observation of small diffraction peaks in carriers proved the formation of TA/Fe 3+ coating film on the surface of four composite nanoparticles (pOVA, pOVA-SA, pOVA-KAE-SA, and pOVA-KAE-TA-SA). The protein structure of the composite nanoparticles coated with TA/Fe 3+ changed, and the order of the changes was pOVA-KAE > pOVA > pOVA-KAE-SA > pOVA-KAE-TA-SA > pOVA-SA. This phenomenon is due to the fact that the chromophore –C=O and the auxo-chromophore –OH are in the opposite position in the benzene ring of TA, and the two substituents have opposite effects and synergize, resulting in the different degrees of redshift of the composite nanoparticle λ max . Additionally, pOVA-SA had the highest α-helix content and the lowest random coils, conferring the protein structure the strongest stability. The coating of TA/Fe 3+ increased the system stability and the thermal stability of the composite nanoparticles. Additionally, the carriers were endowed with antioxidant activity, and their antibacterial ability against Staphylococcus aureus and Escherichia coli was pOVA-KAE-TA-SA > pOVA-KAE-SA > pOVA-KAE > pOVA-SA > pOVA based on the difference in antibacterial diameter (D, mm) and square (S, mm 2 ). pOVA-KAE-TA-SA had the strongest antioxidant activity and antibacterial ability, which improved the bioavailability of TA/KAE. These results provide a theoretical basis for the application of OVA-SA composite nanoparticles in the delivery of bioactive compounds.
研究领域:
纳米技术
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药学
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食品科学
·
生物技术
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）