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Frontiers in Microbiology · 2021 · IF 5.64

Inactivation Effect of Thymoquinone on Alicyclobacillus acidoterrestris Vegetative Cells, Spores, and Biofilms

Fan Qiuxia,Liu Cheng,Gao Zhenpeng,Hu Zhongqiu,Wang Zhouli,Xiao Jianbo,Yuan Yahong,Yue Tianli

Alicyclobacillus acidoterrestris (A. acidoterrestris), a spore-forming bacterium, has become a main challenge and concern for the juices and acid beverage industry across the world due to its thermo-acidophilic characteristic. Thymoquinone (TQ) is one of the active components derived from Nigella sativa seeds. The objective of this study was to investigate antibacterial activity and associated molecular mechanism of TQ against A. acidoterrestris vegetative cells, and to evaluate effects of TQ on A. acidoterrestris spores and biofilms formed on polystyrene and stainless steel surfaces. Minimum inhibitory concentrations of TQ against five tested A. acidoterrestris strains ranged from 32 to 64 μg/mL. TQ could destroy bacterial cell morphology and membrane integrity in a concentration-dependent manner. Field-emission scanning electron microscopy observation showed that TQ caused abnormal morphology of spores and thus exerted a killing effect on spores. Moreover, TQ was effective in inactivating and removing A. acidoterrestris mature biofilms. These findings indicated that TQ is promising as a new alternative to control A. acidoterrestris and thereby reduce associated contamination and deterioration in the juice and acid beverage industry.

研究领域: 食品科学 · 微生物学
✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Protective effect of thymoquinone on glycation of human myoglobin induced by d-ribose

Jing-Jing Liu,Zhan-Yi Wang,Bin-Bin Jiang,Shu-Qin Gao,Ying-Wu Lin

Nonenzymatic glycation and the subsequent accumulation of advanced glycation end-products (AGEs) in proteins are factors underlying long-term pathogenesis in diabetes. The study of protein glycation is crucial for elucidating their relationship with diabetes mellitus and related disorders. This study explores the interaction between d -ribose and human myoglobin (HMb), as well as the protective effect of thymoquinone (TQ) on glycation. A time-dependent in-vitro glycation study was performed to investigate the mechanism of d -ribose-induced structural interference of HMb in the absence and presence of TQ. Spectroscopic and proteomic analysis indicated that the presence of TQ significantly reduced the total amount of AGEs while maintaining structural characteristics of HMb. 14 glycated sites on HMb were further identified via liquid chromatography-tandem mass spectrometry (LC-MS/MS) after incubation with d -ribose for 12 h, predominantly interacting with lysine residues. TQ was found to disrupt this interaction, reducing the glycated sites from 14 to 12 sites and the percentage of glycated peptides from 26.50 % to 12.97 %. Additionally, there was a significant decrease in the degree of glycation at the same sites. In summary, our findings suggest that TQ has the potential to act as an anti-glycation agent and provide a comprehensive understanding underlying the inhibition mechanism of glycation.

研究领域: 生物化学 · 医学
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Food Science & Nutrition · 2025 ·Vol. 13 ·期 4 ·e70113 · IF 3.8

Thymoquinone Ameliorates Gut Epithelial Injury by Suppressing the JNK Signaling Pathway Based on Its Anti-Oxidant Property

Kaitong Jia,Lei Wu,Ziru Li,Tian Wei,Tingting Fan,Guiran Xiao

Ulcerative colitis is one of the most common sorts of inflammatory bowel disease. This study investigates the protective effects of thymoquinone against sodium dodecyl sulfate (SDS)-induced intestinal damage and elucidates the underlying mechanisms using the Drosophila melanogaster model of ulcerative colitis. We found that Drosophila fed thymoquinone from larval to adult stages were resistant to SDS injury in adulthood. Thymoquinone pretreatment significantly restored the abnormal behaviors and intestinal morphological defects in Drosophila exposed to SDS. Moreover, thymoquinone protected the intestinal barrier function by inhibiting the overactivated c-Jun N-terminal kinase (JNK) pathway in the intestine induced by SDS. Further studies indicated that thymoquinone inhibits the JNK pathway by reducing intestinal reactive oxygen species (ROS) levels. This research provides novel pathological and mechanistic insights into the potential application of thymoquinone in developing functional foods or natural medicines, highlighting its significance in treating ulcerative colitis.

CAS / MDL: 490-91-5
研究领域: 医学 · 生物学
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APPLIED MICROBIOLOGY AND BIOTECHNOLOGY · 2021 ·Vol. 105 ·期 11 ·4709-4718 · IF 4.813

Antimicrobial and anti-biofilm activity of thymoquinone against Shigella flexneri

Fan Qiuxia,Yuan Yahong,Jia Hang,Zeng Xuejun,Wang Zhouli,Hu Zhongqiu,Gao Zhenpeng,Yue Tianli

Abstract Shigella flexneri ( Sh. flexneri ), a common foodborne pathogen, has become one of the main threats to food safety and human health due to its high pathogenicity and persistent infection. The objective of this study was to explore the antimicrobial and anti-biofilm activities and the possible mechanism of thymoquinone (TQ) against Sh. flexneri . The minimum inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of TQ against Sh. flexneri were 0.4 and 0.5 mg/mL, respectively. TQ showed bactericidal activity against Sh. flexneri in culture medium and milk system. Scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM) observations demonstrated that TQ could induce abnormal cell morphology and destroy cell membrane. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis suggested that TQ could inhibit protein synthesis in Sh. flexneri . Also, at sub-inhibitory concentrations (SICs), TQ exhibited an inhibitory effect on Sh. flexneri biofilm formation, which was confirmed by crystal violet quantitative analysis and SEM observation. Real-time quantitative PCR (RT-qPCR) analyses revealed that TQ downregulated the expression of genes involved in Sh. flexneri biofilm formation. Thus, TQ has potential as a natural antimicrobial and anti-biofilm agent to address the contamination and infection caused by Sh. flexneri . Key points • Antimicrobial and anti-biofilm activity of TQ on Shigella flexneri were investigated. • TQ inhibited biofilm formation by Shigella flexneri. • TQ provided a new strategy for Shigella flexneri control.

研究领域: 微生物学 · 食品安全 · 分子生物学
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Advanced Healthcare Materials · 2024 · IF 10

Herbal Products-Powered Thermosensitive Hydrogel with Phototherapy and Microenvironment Reconstruction for Accelerating Multidrug-Resistant Bacteria-Infected Wound Healing

Gang Zhao,Guanghua Lu,Huizhen Fan,Li Wei,Qiang Yu,Ming Li,Hanqing Li,Nuo Yu,Shen Wang,Min Lu

Wound healing and infection remain significant challenges due to the ineffectiveness against multidrug-resistant (MDR) bacteria and the complex oxidative wound microenvironments. To address these issues, thymoquinone-reinforced injectable and thermosensitive TQ@PEG-PAF-Cur hydrogels with dual functions of microenvironment reshaping and photodynamic therapy are developed. The hydrogel comprises natural compound thymoquinone (TQ) and poly (ethylene glycol)-block-poly (alanine-co-phenyl alanine) copolymers (PEG-PAF) conjugated with natural photosensitizer curcumin (Cur). The incorporation of TQ and Cur reduces the sol-to-gel transition temperature of TQ@PEG-PAF-Cur to 30°C, compared to PEG-PAF hydrogel (37°C), due to the formation of strong hydrogen bonding, matching the wound microenvironment temperature. Under blue light excitation, TQ@PEG-PAF-Cur generates significant amounts of reactive oxygen species such as H 2 O 2 , 1O 2 , and ·OH, exhibiting rapid and efficient bactericidal capacities against methicillin-resistant Staphylococcus aureus and broad spectrum β-lactamases Escherichia coli via photodynamic therapy (PDT). Additionally, Cur effectively inhibits the expressions of proinflammatory cytokines in skin tissue-forming cells. As a result, the composite hydrogel can rapidly transform into a gel to cover the wound, reshape the wound microenvironment, and accelerate wound healing in vivo. This collaborative antibacterial strategy provides valuable insights to guide the development of multifunctional materials for efficient wound healing.

CAS / MDL: 14825-82-2 2224-52-4
研究领域: 材料科学 · 生物医学工程 · 药学 · 伤口护理 · 感染性疾病
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ONCOLOGY REPORTS · 2025 ·Vol. 54 ·期 6 ·1-14 · IF 3.9

Hydroxypropyl‑β‑cyclodextrin/thymoquinone inclusion complex inhibits non‑small cell lung cancer progression through NF‑κB‑mediated ferroptosis

Wei-Wei Zheng,Jia-Xuan Ding,Yang-Xin Liang,Ling Ye

Thymoquinone (TQ) is a quinone isolated from the black seed Nigella sativa and has been extensively investigated in the pharmaceutical field due to its promising therapeutic value. There have been reports on the potential anti‑cancer properties of TQ, whereas the clinical application of TQ is greatly restricted by its low water solubility and poor delivery. In the present study, TQ was encapsulated into hydroxypropyl‑β‑cyclodextrin (HP‑β‑CD) using the freeze‑drying method to form a TQ/HP‑β‑CD inclusion complex. Then, the TQ/HP‑β‑CD inclusion complex was characterized by Fourier transform infrared, differential scanning calorimetry, X‑ray diffraction and scanning electron microscopy. HP‑β‑CD as an excipient significantly enhances the water solubility of TQ, and TQ/HP‑β‑CD demonstrated excellent biocompatibility on normal cells both in vitro and in vivo. Moreover, the complexation with HP‑β‑CD enhanced the anticancer activity of TQ against non‑small cell lung cancer cells and its mechanism of action is related to ferroptosis mediated by NF‑κB. Such an enhanced cytotoxic effect may be attributed to the effective complexation of TQ in HP‑β‑CD, which enhances its water solubility and bioavailability.

研究领域: 药学 · 肿瘤学 · 纳米医学 · 分子生物学 · 药物递送
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2026 · IF 4.8

Inhibition of d-ribose-induced glycation of metalloprotein human myoglobin by bioactive quinones

Jing-Jing Liu,Si-Dian Miao,Zhan-Yi Wang,Ya-Han Zhu,Bin-Bin Jiang,Shuang-Shuang Long,Shu-Qin Gao,Ying-Wu Lin

The anti-glycation effects and mechanisms of eight quinone-related compounds, primarily sourced from medicinal and edible plants, were evaluated in this study. In vitro glycation experiments were conducted to study the structural perturbation induced by d -ribose on human myoglobin (HMb) in the presence of the tested compounds. Spectroscopic and electrophoretic analyses indicated that among the four benzoquinone-related substances, thymoquinone and its structurally closest analogue 2,5-dimethyl-1,4-benzoquinone, exhibited significant inhibitory effects on the d -ribose-induced glycation, thereby maintaining protein structural stability, reducing advanced glycation end products (AGEs) formation, and attenuating the covalent protein modification by d -ribose. In contrast, 1,4-benzoquinone and hydroquinone (a reduction product of 1,4-benzoquinone) promoted HMb denaturation through the Michael addition mechanism. Of the two naphthoquinones, juglone and plumbagin, showed anti-glycation effects, whereas the anthraquinones emodin and chrysophanol showed no significant effects. Nano-HPLC-MS/MS analysis further showed that thymoquinone was more effective in preventing glycation than juglone and plumbagin. This study investigates the mechanisms underlying glycation inhibition by quinones, revealing that the presence of dual β -substituted carbons on the benzoquinone ring is critical for stabilizing protein conformations and suppressing glycation. It provides a preliminary mechanistic basis and identifies candidate molecules for potential applications of quinones in retarding glycation, such as in managing diabetic complications or inhibiting glycation reactions during food processing.

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AQUACULTURE · 2021 · IF 4.242

Identification of plumbagin as an effective chemotherapeutic agent for treatment of Gyrodactylus infections

Xiao Tu,Chenxi Duan,Siwei Wu,Shengli Fu,Jianmin Ye

Monogenean parasites are responsible for severe economic losses of both freshwater and marine aquaculture industries. Current chemotherapeutic treatments are consuming, expensive, and harmful to water quality and human health. Medicinal plants are a reliable source of alternative anthelmintic agents. In the pursuit of novel anti-monogenean drugs, in vivo anthelminthic efficacy of 26 selected phytochemical compounds was studied, by choosing Gyrodactylus kobayashi infecting goldfish ( Carassius auratus ) as a model. The screening results showed that four compounds (plumbagin (PLB), thymoquinone, osthole and psoralen) had the highest activity against G. kobayashii with EC 99 value ranging from 0.4 to 4.0 mg/L after 48-h exposure. Among these active compounds, PLB was the most efficacious one and selected for the next study. In vitro trials revealed the clear anti-parasitic effects of PLB, with complete death at 45 min of exposure at a concentration of 2.0 mg/L, withdrawal of PLB afterward did not lead to the recovery of the exposed parasites. Bathing G. kobayashii infected goldfish in PLB also significantly reduced the worm burden, with an extremely low EC 50 value of 0.09 mg/L after 48-h immersion. The results also showed that one short bath using very low concentrations of 0.4–0.7 mg/L for 30–60 min was effective in eliminating G. kobayashii infection with no visible fish toxicity. Acute toxicity assay indicated the 48-h LC 50 of PLB against goldfish was 0.657 mg/L. Furthermore, SEM analysis displayed that PLB-mediated worm killing was associated with the tegumental damages. As seen by TEM , in vivo treatment against G. kobayashii with PLB also caused vacuolization and lysis of parasite's tegument, besides, differing degrees of damage to vitelline cells were observed in treated worms. Collectively, simple chemical structure along with the potent efficacy demonstrated that PLB could serve as an ideal leading compound in the development of a commercial drug to control Gyrodactylus infections in aquaculture

研究领域: 水产养殖学 · 药理学 · 寄生虫学
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Infectious Diseases and Therapy · 2021 ·Vol. 10 ·期 1 ·483-494 · IF 5.322

Computational and Experimental Studies Reveal That Thymoquinone Blocks the Entry of Coronaviruses Into In Vitro Cells

Xu Huan,Liu Bing,Xiao Zhen,Zhou Meiling,Ge Lin,Jia Fan,Liu Yanling,Jin Hongshan,Zhu Xiuliang,Gao Jian,Akhtar Javed,Xiang Bai,Tan Ke,Wang Guanyu

Introduction Since December 2019, severe acute respiratory syndrome-related coronavirus-2 (SARS-CoV-2) has caused the coronavirus disease 2019 (COVID-19) pandemic in China and worldwide. New drugs for the treatment of COVID-19 are in urgent need. Considering the long development time for new drugs, the identification of promising inhibitors from FDA-approved drugs is an imperative and valuable strategy. Recent studies have shown that the S1 and S2 subunits of the spike protein of SARS-CoV-2 utilize human angiotensin-converting enzyme 2 (hACE2) as the receptor to infect human cells. Methods We combined molecular docking and surface plasmon resonance (SPR) to identify potential inhibitors for ACE2 from available commercial medicines. We also designed coronavirus pseudoparticles that contain the spike protein assembled onto green fluorescent protein or luciferase reporter gene-carrying vesicular stomatitis virus core particles. Results We found that thymoquinone, a phytochemical compound obtained from the plant Nigella sativa , is a potential drug candidate. SPR analysis confirmed the binding of thymoquinone to ACE2. We found that thymoquinone can inhibit SARS-CoV-2, SARS-CoV, and NL63 pseudoparticles infecting HEK293-ACE2 cells, with half-maximal inhibitory concentrations of 4.999, 7.598, and 6.019 μM, respectively. The SARS-CoV-2 pseudoparticle inhibition had half-maximal cytotoxic concentration of 35.100 μM and selection index = 7.020. Conclusion Thymoquinone is a potential broad-spectrum inhibitor for the treatment of coronavirus infections.

CAS / MDL: 97-53-0 490-91-5
研究领域: 药理学 · 病毒学 · 分子生物学 · 药物发现
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PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY · 2021 · IF 3.963

Naturally produced magnolol can significantly damage the plasma membrane of Rhizoctonia solani

Feixu Mo,Xianfeng Hu,Yi Ding,Rongyu Li,Youhua Long,Xiaomao Wu,Ming Li

Rice sheath blight is a destructive fungal disease caused by Rhizoctonia solani . To find a safe and green measure, the biological activity of six plant extracts against R. solani was determined by mycelial growth rate method. The results showed that magnolol possessed better antifungal activities against R. solani , with an EC 50 value of 7.47 mg/L. further action mechanism of magnolol against R. solani was carried out. Studies by scanning electron microscopy (SEM) showed that the morphology of R. solani mycelia was deformation and surface folds. Transmission electron microscope (TEM) observation on treated R. solani showed that magnolol could induce cytoplasmic membrane rupture and cytoplasmic membrane even disappeared completely accompanied with cellular debris was covered around this fungal, and the mycelia treated with magnolol showed fluorescence after PI staining. Further study showed that the content of malondialdehyde (MDA) and activity of chitinase , β-1,3-glucanase and relative conductivity of mycelia were increased, while the content of soluble protein and activities of catalase (CAT), polyphenol oxidase (PPO), superoxide dismutase (SOD), succinate dehydrogenase (SDH) and NAD-malate dehydrogenase (NAD-MDH) were significantly decreased. These results indicated that magnolol could significantly damage the plasma membrane of R. solani , and interfere with cell respiratory metabolism, thus inhibiting the growth of mycelium.

研究领域: 植物学 · 真菌学 · 药理学
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