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Psoriasis, a persistent immune-mediated inflammatory skin condition, affects approximately 2-3% of the global population. Current treatments for psoriasis are fraught with limitations, including adverse effects, high costs, and diminishing efficacy over time. Thymoquinone (TQ), derived from Nigella sativa seeds, exhibits promising anti-inflammatory, antioxidant, and immunomodulatory properties that could prove beneficial in managing psoriasis. However, TQ's hydrophobic nature and poor bioavailability have hindered its usefulness as a therapeutic agent. Recent research has strategically addressed these challenges by developing nano-thymoquinone (nano-TQ) formulations to enhance delivery and efficacy in treating psoriasis. Preclinical studies employing mouse models have demonstrated that nano-TQ effectively mitigates inflammation, erythema, scaling, epidermal thickness, and cytokine levels in psoriatic lesions. Various nano-TQ formulations, including nanoemulsions, lipid vesicles, nanostructured lipid carriers, and ethosomes, have been explored to improve solubility, facilitate skin penetration, ensure sustained release, and achieve site-specific targeting. Although clinical trials are currently scarce, the outcomes from in vitro and animal models are promising. The potential co-delivery of nano-TQ with other anti-psoriatic agents also presents avenues for further investigation. [ABSTRACT FROM AUTHOR]

Given the need for novel and effective therapies for colon cancer, this study aimed to investigate the effects of 5-fluorouracil-loaded calcium carbonate nanoparticles (5FU-CaCO3np) combined with thymoquinone (TQ) against colon cancer. A shaking incubator and a high-speed homogenizer were used to prepare the optimal 5FU-CaCO3np, with characterizations of physicochemical properties, in vitro drug release profile, and biocompatibility. In vitro experiments and molecular docking were employed to evaluate the therapeutic potential of the combination for colon cancer treatment. Study results revealed that 5FU-CaCO3np with a size of approximately 130 nm was synthesized using the high-speed homogenizer. Its favorable biocompatibility, pH sensitivity, and sustained release properties facilitated reduced toxic side effects of 5-FU on NIH3T3 normal cells and enhanced inhibitory effects on CT26 colon cancer cells. The combination of 5FU-CaCO3np (1.875 μM) and TQ (30 μM) showed significantly superior anti-colon cancer effects to 5FU-CaCO3np alone in terms of cell proliferation and migration inhibition, cell apoptosis induction, and spheroid growth suppression in CT26 cells (p < 0.05), with strong interactions between the drugs and targets (E-cadherin, Bcl-2, PCNA, and MMP-2). These results provide evidence for 5FU-CaCO3np as a novel regimen against colon cancer. Combining 5FU-CaCO3np and TQ may offer a new perspective for colon cancer therapy. [ABSTRACT FROM AUTHOR]

Several pharmacological effects were described for Nigella sativa (N. sativa) seed and it has been used traditionally to treat various diseases. In this review article, the updated and comprehensive anti-oxidant effects of N. sativa and its main constituent, thymoquinone (TQ), on various disorders are described. The relevant articles were retrieved through PubMed, Science Direct, and Scopus up to December 31, 2023. Various extracts and essential oils of N. sativa showed anti-oxidant effects on cardiovascular, endocrine, gastrointestinal and liver, neurologic, respiratory, and urogenital diseases by decreasing and increasing various oxidant and anti-oxidant marketers, respectively. The main constituent of the plant, TQ, also showed similar anti-oxidant effects as the plant itself. The antioxidant effects of different extracts and essential oils of N. sativa were demonstrated in various studies which were perhaps due to the main constituent of the plant, TQ. The findings of this review article suggest the possible therapeutic effect of N. sativa and TQ in oxidative stress disorders. [ABSTRACT FROM AUTHOR]

Natural compounds such as thymoquinone (TQ) have recently gained increasing attention in treating glioblastoma (GBM). However, the effects of TQ in reversing drug resistance are not completely understood. Therefore, we aimed to examine TQ impacts on GBM cells with doxorubicin (DOX) resistance and the involvement of the PI3K/Akt/mTOR pathway. GBM cancer U87 and U87/DOX (resistant cells) cells were exposed to DOX and TQ, and cell proliferation was assessed by the MTT assay. ELISA was applied to evaluate cell apoptosis. The expression of apoptotic mediators such as Caspase‐3, Bax, Bcl‐2 and PI3K, Akt, mTOR, P‐gp, and PTEN was assessed via qRT‐PCR and western blot. We found that a combination of TQ and DOX suppressed dose‐dependent cell growth capacity in cells and increased the cytotoxic effects of DOX in resistant cells. In addition, TQ treatment increased DOX‐mediated apoptosis in U87/DOX cell lines via modulating the pro‐ and anti‐apoptotic markers. A combination of TQ and DOX upregulated PTEN and downregulated PI3K, Akt, and mTOR, suppressing this signal transduction in resistant cells. In conclusion, we showed TQ potentiated doxorubicin‐mediated antiproliferative and pro apoptotic function DOX‐resistant glioblastoma cells, which is mediated by targeting and suppressing PI3K/Akt/mTOR signal transduction. [ABSTRACT FROM AUTHOR]

One of the adverse effects of the antineoplastic drug cisplatin (CS) is damage to testicular tissue. This study aimed to examine the potential therapeutic effect of thymoquinone (TQ), a strong antioxidant, against testicular damage caused by CS. In the experiment, 28 rats were used, and the rats were randomly divided into four groups: control (n = 7), CS (n = 7), CS + TQ (n = 7), and TQ (n = 7). The experiment was called off after all treatments were finished on day 15. Blood serum and testicular tissues were utilized for biochemical, histological, immunohistochemical, mRNA expression, and gene protein investigations. The testosterone level decreased and oxidative stress, histopathological damage, dysregulation in mitochondrial dynamics, inflammation and apoptotic cells increased in testicular tissue due to CS administration. TQ supplementation showed anti-inflammatory, antioxidant, and anti-apoptotic effects in response to CS-induced testicular damage. In addition, TQ contributed to the reduction of CS-induced toxic effects by regulating the TNF-α/OTULIN/NF-κB pathway. TQ supplementation may be a potential therapeutic strategy against CS-induced testicular damage by regulating the TNF-α/OTULIN/NF-κB axis, inhibiting inflammation, oxidative stress, and apoptosis. [ABSTRACT FROM AUTHOR]

The drug efflux pump is a crucial mechanism implicated in resistance to multiple antimicrobials. Thymoquinone (TQ) has evidently demonstrated multiple activities, antibacterial being the most effective. Knowledge about TQ activity against multidrug-resistant Staphylococcus aureus is very scarce. Therefore, the present study was conducted to investigate TQ resistance modulation in ciprofloxacin (CIP) and doxycycline (DO) multidrug-resistant S. aureus. Forty-seven samples were collected from different sources, and S. aureus was isolated and identified. Then, S. aureus resistance profiles to antimicrobials, N. sativa essential oil, and TQ; the correlation between TQ-MIC readings and disc diffusion; cartwheel and ethidium bromide (EtBr) accumulation assays; and norA gene expression were all described within silico molecular docking for TQ interactions with norA efflux pump protein. TQ-MICs ranged from 5–320 µg/ml. TQ down-regulated norA gene expression, resulting in a drop in efflux pump activity of 77.5–90.6% in the examined strains, comparable to that observed with verapamil. Exposure of S. aureus strains to CIP and DO raises the initial basal efflux pumping expression to 34.2 and 22.9 times, respectively. This induced efflux pumping overexpression was substantially reduced by 97.7% when TQ was combined with CIP or DO. There was a significant reduction of MICs of CIP and DO MICs by 2–15 and 2–4 folds, respectively, after treatment with 0.5XMIC-TQ in resistance modulation assays. These results refer to TQ ligand inhibitory interactions with NorA protein in molecular docking. Interpretations of inhibition zone diameters (IZDs) of disc diffusion and TQ-MICs exhibit independence of MICs from IZDs, as indicated by invalid linear regression analysis. TQ significantly reduced efflux pumping S. aureus induced by CIP and DO, but further investigations are needed to improve TQ-pharmacokinetics to restore CIP and DO activity and suppress fluoroquinolone and doxycycline-resistant S. aureus selection in clinical and animal settings. [ABSTRACT FROM AUTHOR]

Background: The toxicity of silver nanoparticles (AgNPs) has been proven in the female reproductive system. Thymoquinone (TQ) is a natural antioxidant and bioactive component of Nigella sativa. Objective: We evaluated the efficacy of TQ on ovarian tissue following toxicity induced by AgNPs in female mice. Materials and Methods: 24 female NMRI mice (5-6 wk, an average weight of 33 gr) were randomly divided into 4 groups (n = 6/each): control, AgNPs (500 mg/kg, gavage), TQ (2.5 mg/kg, intraperitoneal injection), and TQ+AgNPs. Mice were treated every day for 35 days. Serum levels of malondialdehyde (MDA), total antioxidant capacity (TAC), luteinizing hormone, and follicle-stimulating hormone were measured. The optical disector and stereological techniques were utilized to estimate the follicular count, their volume at different developmental stages, and the structure of ovarian tissue. Results: In the AgNPs group, the serum concentrations of TAC (p = 0.01), luteinizing hormone (p < 0.001), follicle-stimulating hormone, the volume of corpus luteum (p < 0.001), and the number of follicles decreased significantly compared to the control group. Nevertheless, AgNPs significantly increased the MDA level. In the TQ+AgNPs group compared to the AgNPs group, a significant decrease in MDA level (p < 0.001) and a significant improvement in TAC (p = 0.03), and hormonal levels, the number of primary, preantral, and antral follicles (p = 0.04), and the volume of corpus luteum (p = 0.01) were observed. Conclusion: TQ improved the number of follicles by reducing oxidative stress and lipid peroxidation in AgNPs-damaged ovarian tissue. [ABSTRACT FROM AUTHOR]

Purpose: In this study, the effect of thymoquinone (TQ) on CP-induced spermatogenesis defects in mice has been investigated. Methods: Sperm parameters, serum testosterone concentration, histology, Bax/Bcl-2 ratio, and expression of autophagy-related biomarkers have been assessed. Total antioxidant capacity (TAC), total oxidant status (TOS), and oxidative stress index (OSI) in testicular tissue were examined for the evaluation of oxidative stress levels. Results: CP has induced histological changes and significantly increased the Bax/Bcl-2 ratio, decreased testosterone concentration, testicular weight, and sperm quality. CP induced oxidative stress by elevating OSI in the testicular tissue (p < 0.05). Expression of the autophagy-inducer genes (ATG7, ATG5, and Beclin-1) and ratio of LC3B/LC3A proteins were significantly decreased, while mTOR expression was increased in the CP group. TQ pretreatment dose-dependently decreased the Bax/Bcl-2 ratio and mTOR gene expression while increasing the expression of ATG5 and ATG7 genes, LC3B/LC3A ratio, and Beclin-1 proteins. TQ could also dose-dependently reverse the histology, testosterone level, and sperm quality of the CP-intoxicated mice. Conclusions: These findings show that TQ pretreatment can enhance sperm production by inducing autophagy and reducing apoptosis and oxidative stress in the CP-intoxicated mouse testicles. [ABSTRACT FROM AUTHOR]

The interaction between herbal remedies and drugs is a fascinating phenomenon that might cause therapeutic complications in patients. Warfarin is an anticoagulant drug that provides anti-blood-clotting effects by inhibiting the formation of vitamin K-dependent coagulation factors, and warfarin interacts with the nuclear receptor PXR, subsequently modulating cytochrome P450 during the metabolism process. St. John's wort, an herbal medicine with antidepressant effects, can alter the pharmacokinetics of warfarin. Thymoquinone is one of the active compounds in N. sativa and has pharmacological activities such as anticoagulant, antidiabetic, diuretic, antidepressant, and anti-inflammatory effects. In this study, we investigated the compounds in Nigella sativa ( N. sativa) against pregnane X receptor (PXR) and evaluated the impact of thymoquinone (TQ) administration on PXR expression in HepG2 cells. The molecular docking analysis was conducted utilizing the Molecular Operating Environment (MOE) with the PXR (PDB ID: 7AXJ). At the same time, the PXR gene expression was measured using RT-PCR instruments. The RMSD value in docking represents the deviation criteria between the native ligand position and the redocking position result, indicating the capability of MOE and PDB qualification for performing molecular docking. The docking analysis showed that warfarin had the strongest binding energy (7AXJ -6.0507) by forming hydrogen binding type on Arg410. Despite TQ being the major component, it also displayed a high affinity for the two PDB IDs (7AXJ -4.5962). Furthermore, the concurrent administration of warfarin and TQ (19.27 μM) in HepG2 cells showed a significant reduction in the relative mRNA expression of the PXR gene. Given the above-mentioned findings, our study adequately enables us to predict the mechanism behind herb-drug interactions (HDIs) implicating N. sativa, specifically the TQ compound to warfarin metabolism via the activation of the PXR receptor. [ABSTRACT FROM AUTHOR]

The purpose of this study was to assess the anti-genotoxic potential of thymoquinone (TQ) against DNA damage in NRK-52E cells treated with high glucose using the comet assay technique single cell gel electrophoresis method. Cells were propagated by regular passages in in vitro conditions. TQ proliferative concentration (10μM) and IC25 (3rd-hour: 550 mM, 12th-hour: 240 mM, 24th-hour: 200 mM) and IC50 (3rd-hour: 760 mM, 12th-hour: 400 mM, 24th-hour: 280 mM) values for each hour of high glucose and were determined separately with MTT method. At these concentrations, the cells were divided into control(C), Thymoquinone (TQ), high glucose(G) and high glucose plus thymoquinone (GT) groups; It was incubated with the indicated substances for 3, 12, 24 hours. DNA damage was evaluated by applying the comet assay protocol and the results were calculated as DNA damage index (DDI). While DDI levels were observed to be significantly higher (p

Several pharmacological effects were described for Nigella sativa (N. sativa) seed and it has been used traditionally to treat various diseases. In this review article, the updated and comprehensive anti-oxidant effects of N. sativa and its main constituent, thymoquinone (TQ), on various disorders are described. The relevant articles were retrieved through PubMed, Science Direct, and Scopus up to December 31, 2023. Various extracts and essential oils of N. sativa showed anti-oxidant effects on cardiovascular, endocrine, gastrointestinal and liver, neurologic, respiratory, and urogenital diseases by decreasing and increasing various oxidant and anti-oxidant marketers, respectively. The main constituent of the plant, TQ, also showed similar anti-oxidant effects as the plant itself. The anti-oxidant effects of different extracts and essential oils of N. sativa were demonstrated in various studies which were perhaps due to the main constituent of the plant, TQ. The findings of this review article suggest the possible therapeutic effect of N. sativa and TQ in oxidative stress disorders.

Abstract The drug efflux pump is a crucial mechanism implicated in resistance to multiple antimicrobials. Thymoquinone (TQ) has evidently demonstrated multiple activities, antibacterial being the most effective. Knowledge about TQ activity against multidrug-resistant Staphylococcus aureus is very scarce. Therefore, the present study was conducted to investigate TQ resistance modulation in ciprofloxacin (CIP) and doxycycline (DO) multidrug-resistant S. aureus. Forty-seven samples were collected from different sources, and S. aureus was isolated and identified. Then, S. aureus resistance profiles to antimicrobials, N. sativa essential oil, and TQ; the correlation between TQ-MIC readings and disc diffusion; cartwheel and ethidium bromide (EtBr) accumulation assays; and norA gene expression were all described within silico molecular docking for TQ interactions with norA efflux pump protein. TQ-MICs ranged from 5–320 µg/ml. TQ down-regulated norA gene expression, resulting in a drop in efflux pump activity of 77.5–90.6% in the examined strains, comparable to that observed with verapamil. Exposure of S. aureus strains to CIP and DO raises the initial basal efflux pumping expression to 34.2 and 22.9 times, respectively. This induced efflux pumping overexpression was substantially reduced by 97.7% when TQ was combined with CIP or DO. There was a significant reduction of MICs of CIP and DO MICs by 2–15 and 2–4 folds, respectively, after treatment with 0.5XMIC-TQ in resistance modulation assays. These results refer to TQ ligand inhibitory interactions with NorA protein in molecular docking. Interpretations of inhibition zone diameters (IZDs) of disc diffusion and TQ-MICs exhibit independence of MICs from IZDs, as indicated by invalid linear regression analysis. TQ significantly reduced efflux pumping S. aureus induced by CIP and DO, but further investigations are needed to improve TQ-pharmacokinetics to restore CIP and DO activity and suppress fluoroquinolone and doxycycline-resistant S. aureus selection in clinical and animal settings.

OBJECTIVE: This study aimed to assess if Nigella sativa oil (NSO), a health supplement containing thymoquinone as a major component, can act as a protective agent in salivary gland stem cells following radiotherapy (RT) damage. METHODS: Forty, 10-week-old, male C3H/HeJ mice were randomized to four experimental groups: sham RT + H2O gavage (control) (N = 4); 15 Gy RT + H2O gavage (N = 12); sham RT + NSO gavage (N = 12); and 15 Gy RT + NSO gavage (N = 12). Weight changes, saliva production, and salivary gland histopathologic staining were recorded for each group over the course of the experiment. RESULTS: All mice in the sham RT + H2O gavage and sham RT + NSO gavage groups demonstrated 100% 60-day survival. RT + H2O compared to RT + NSO gavaged mice were significantly underweight by an average of 6.4 g (p

This work intended to study differences in oil yield and co-extraction of antioxidant and antibacterial compounds of Nigella sativa L. seed oil as a function of two main extraction processes: mechanical pressing and solvent extraction, including hexane and chloroform. Next, we studied such oils’ chemical composition and antioxidant and antibacterial activities. Notably, the chemical cartelization was conducted by use of HPLC. The antioxidant activity of the oils was assessed using DPPH, TAC, and FRAP assays. Antimicrobial activity was investigated against bacteria and fungi with clinical importanceT. HPLC-DAD analysis identified some bioactive compounds in the oils, including thymoquinone, carvacrol, and gallic acid. Results showed that oils extracted by different methods exhibit varying levels of antioxidant activity, with a higher concentration of antioxidant compounds in chloroform-extracted oils. Antimicrobial tests revealed significant inhibitory effects of the studied oils on the growth of bacteria and fungi. In conclusion, this research has made it possible to characterize the oils extracted from Nigella sativa L. Seeds by determining their chemical composition and biological properties, notably their antioxidant, antibacterial, and antifungal activity. These results contribute to a better understanding of the potential benefits of these oils for human health and open up exciting prospects for their use in various fields, notably as food additives and therapeutic agents.

Metabolic syndrome (MetS) is a widespread global epidemic that affects individuals across all age groups and presents a significant public health challenge. Comprising various cardio-metabolic risk factors, MetS contributes to morbidity and, when inadequately addressed, can lead to mortality. Current therapeutic approaches involve lifestyle changes and the prolonged use of pharmacological agents targeting the individual components of MetS, posing challenges related to cost, compliance with medications, and cumulative side effects. To overcome the challenges associated with these conventional treatments, herbal medicines and phytochemicals have been explored and proven to be holistic complements/alternatives in the management of MetS. Thymoquinone (TQ), a prominent bicyclic aromatic compound derived from Nigella sativa emerges as a promising candidate that has demonstrated beneficial effects in the treatment of the different components of MetS, with a good safety profile. For methodology, literature searches were conducted using PubMed and Google Scholar for relevant studies until December 2023. Using Boolean Operators, TQ and the individual components of MetS were queried against the databases. The retrieved articles were screened for eligibility. As a result, we provide a comprehensive overview of the anti-obesity, anti-dyslipidaemic, anti-hypertensive, and anti-diabetic effects of TQ including some underlying mechanisms of action such as modulating the expression of several metabolic target genes to promote metabolic health. The review advocates for a paradigm shift in MetS management, it contributes valuable insights into the multifaceted aspects of the application of TQ, fostering an understanding of its role in mitigating the global burden of MetS.

Metabolic syndrome (MetS) is a widespread global epidemic that affects individuals across all age groups and presents a significant public health challenge. Comprising various cardio-metabolic risk factors, MetS contributes to morbidity and, when inadequately addressed, can lead to mortality. Current therapeutic approaches involve lifestyle changes and the prolonged use of pharmacological agents targeting the individual components of MetS, posing challenges related to cost, compliance with medications, and cumulative side effects. To overcome the challenges associated with these conventional treatments, herbal medicines and phytochemicals have been explored and proven to be holistic complements/alternatives in the management of MetS. Thymoquinone (TQ), a prominent bicyclic aromatic compound derived from Nigella sativa emerges as a promising candidate that has demonstrated beneficial effects in the treatment of the different components of MetS, with a good safety profile. For methodology, literature searches were conducted using PubMed and Google Scholar for relevant studies until December 2023. Using Boolean Operators, TQ and the individual components of MetS were queried against the databases. The retrieved articles were screened for eligibility. As a result, we provide a comprehensive overview of the anti-obesity, anti-dyslipidaemic, anti-hypertensive, and anti-diabetic effects of TQ including some underlying mechanisms of action such as modulating the expression of several metabolic target genes to promote metabolic health. The review advocates for a paradigm shift in MetS management, it contributes valuable insights into the multifaceted aspects of the application of TQ, fostering an understanding of its role in mitigating the global burden of MetS. [ABSTRACT FROM AUTHOR]

Cancer, a major challenge to global health and healthcare systems, requires the study of alternative and supportive treatments due to the limitations of conventional therapies. This review examines the chemopreventive potential of three natural compounds: rosmarinic acid, apigenin, and thymoquinone. Derived from various plants, these compounds have demonstrated promising chemopreventive properties in in vitro, in vivo, and in silico studies. Specifically, they have been shown to inhibit cancer cell growth, induce apoptosis, and modulate key signaling pathways involved in cancer progression. The aim of this review is to provide a comprehensive overview of the current research on these phytochemicals, elucidating their mechanisms of action, therapeutic efficacy, and potential as adjuncts to traditional cancer therapies. This information serves as a valuable resource for researchers and healthcare providers interested in expanding their knowledge within the field of alternative cancer therapies.

Black cumin is a member of the Ranunculaceae family, it is a popular herb called a miracle remedy to treat various diseases. A factorial experiment was conducted in RCBD with three replicates to evaluate the performance of Nigella spp. in response to foliar organic fertilizer (ALGAREN TWIN) in three concentrations (Control, 0.4 and 0.8 mL L-1). Seed yield and volatile oil bioactive composition across two consecutive seasons 2021-2022, and 2022-2023 were evaluated under semi-arid conditions with total precipitations of 310.5 and 715 mm respectively. The results of both seasons revealed a significant variation between the two species in most yield component traits. N. sativa showed the highest seed yield (737 kg ha-1), fixed oil (25%), and volatile oil (1.163%). The higher application rate of 0.8 mL L-1 generally leads to an increase in the yield of Nigella spp. seed and its components with 919 kg ha-1 seed yield, 26 % fixed oil, and 1.430% volatile oil. The interaction between N. sativa and 0.8 mL L-1 fertilization recorded a higher seed yield of 1065 kg ha-1, 28% fixed oil, and 1.430% volatile oil. The 2022-2023 season recorded a higher seed yield of 720 kg ha-1 than the first season. The analysis of volatile oils showed a mixture of phytochemical compounds. Terpenoid was the predominant constituent in both black cumin species. Thymoquinone was identified as a major constituent in N. sativa (25%). It could be concluded that the use of high rates of foliar organic fertilization on N. sativa gave a superior performance in most yield-related characters.

Abstract Diabetes mellitus (DM) is a complex metabolic condition that causes organ dysfunction. The current experiment sought to determine the effect of thymoquinone (TQ) on hyperglycemia, hyperlipidemia, oxidative/nitrosative stress, inflammation, and apoptosis in diabetic rats prompted by streptozotocin (STZ) (55 mg/kg body weight i/p). The animals were allocated into control, TQ (50 mg/kg B.W. orally administered for 4 succeeding weeks), Diabetic, and Diabetic + TQ groups. This study confirmed that TQ preserves the levels of insulin, fasting blood glucose, HOMA β-cell indices, HbA1c %, body weight, and lipid profile substantially relative to the DC group. Furthermore, hepatic antioxidant (CAT, GSH, and T-SOD) values were reduced. Conversely, the enzymatic activity of liver functions (AST, ALT, ALP, cytochrome P450, and hepatic glucose-6-phosphatase), lipid peroxidation (MDA), pro-inflammatory cytokines (IL-1β, TNF-α, and IL-6), nitric oxide (NO) and inflammatory marker (CRP) enhanced with STZ administration, which is substantially restored after TQ treatment. Relative to the diabetic rats, TQ reestablished the hepatic architectural changes and collagen fibers. Additionally, TQ downregulated the intensity of the immunohistochemical staining of pro-apoptotic marker (caspase-3), p53, and tumor necrosis factor-alpha (TNF-α) proteins in hepatic tissues. Furthermore, TQ displayed abilities to interact and inhibit the binding site of caspase-3, interleukin-6 receptor, interleukin-1 receptor type 1, TNF receptor superfamily member 1A, and TNF receptor superfamily member 1B in rats following the molecular docking modeling. All these data re-establish the liver functions, antioxidant enzymes, anti-inflammatory markers, and anti-apoptotic proteins impacts of TQ in STZ-induced DM rats. Founded on these outcomes, the experiment proposes that TQ is a novel natural supplement with various clinical applications, including managing DM, which in turn is recommended to play a pivotal role in preventing the progression of diabetes mellitus.

Mohammed A Bazuhair,1,2 Mohammed Alsieni,1 Hani Abdullah,3 Jawahir A Mokhtar,3– 5 Dalya Attallah,4 Turki S Abujamel,5,6 Khalil K Alkuwaity,5,6 Hanouf A Niyazi,3 Hatoon A Niyazi,3 Hind AbdulMajed,3 Noha Juma,3 Mohammed W Al-Rabia,3 Abdelbagi Alfadil,2,3 Karem Ibrahem3 1Department of Clinical Pharmacology, Faculty of Medicine, King Abdulaziz University, Jeddah, 21589, Saudi Arabia; 2Centre of Research Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah, Saudi Arabia; 3Department of Clinical Microbiology and Immunology, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia; 4Department of Clinical Microbiology Laboratory, King Abdulaziz University Hospital, Jeddah, 21589, Saudi Arabia; 5Vaccines and Immunotherapy Unit, King Fahd Medical Research Center, King Abdulaziz University, Jeddah, 21589, Saudi Arabia; 6Department of Medical Laboratory Sciences, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah, 21589, Saudi ArabiaCorrespondence: Karem Ibrahem, Department of Clinical Microbiology and Immunology, Faculty of Medicine, King Abdulaziz University, P.O. Box 80205, Jeddah, 21589, Saudi Arabia, Tel +966 562525685, Email kaibrahem@kau.edu.saIntroduction: Candida is the primary cause of invasive fungal disease, candidiasis, especially in developed nations. The increasing resistance observed in multiple antibiotics, coupled with the prolonged process of creating new antibiotics from the ground up, emphasizes the urgent requirement for innovative methods and new compounds to combat Candida infections. Employing a treatment strategy that combines antibiotics can improve efficacy, broaden the spectrum of targeted fungal, and reduce the chances of resistance emergence. This approach shows potential in tackling the escalating problem of antibiotic resistance. The objective of this research is to explore the potential synergistic effects of combining 3-hydrazinoquinoxaline-2-thiol and thymoquinone against a variety of Candida isolates. This investigation aims to offer an understanding of the collective antimicrobial action of these compounds.Methods: Broth microdilution was utilized to assess the Minimum Inhibitory Concentrations (MICs) of 3-hydrazinoquinoxaline-2-thiol and thymoquinone for 22 clinical Candida isolates. Following this, a checkerboard assay was employed to analyze the interaction between 3-hydrazinoquinoxaline-2-thiol and thymoquinone, with a specific focus on the Fractional Inhibitory Concentration Index (FICI).Results: The MICs of thymoquinone and 3-hydrazinoquinoxaline-2-thiol were determined for 22 clinical Candida strains, with thymoquinone exhibiting MICs ranging from 64 to 8 μg/mL, and 3-hydrazinoquinoxaline-2-thiol displaying MICs varying from 64 to 8 μg/mL. Notably, the combination of 3-hydrazinoquinoxaline-2-thiol and thymoquinone resulted in a synergistic effect, leading to a significant reduction in MICs, with reductions of up to 64-fold with FICI below 0.5 against tested strains.Conclusion: The prospect of using 3-hydrazinoquinoxaline-2-thiol in combination with thymoquinone as an effective solution against Candida looks encouraging. Nevertheless, to validate its practical applicability, additional comprehensive testing and experiments are imperative.Keywords: Candida spp, antimicrobial resistance, 3-hydrazinoquinoxaline-2-thiol, thymoquinone, MIC, FICI

Background: Increased reactive oxygen species (ROS) have been implicated as important mechanisms that contribute to endothelial dysfunction (ED). The administration of thymoquinone in animal models significantly inhibits ROS production. Purpose: The protective effects of thymoquinone on endothelial cell dysfunction were studied in cholesterol-fed rabbits. Thirty rabbits were randomly divided into five groups. Methods: The negative control group was fed a standard diet, the positive control group was fed the same diet with 2 % cholesterol, the Thymoquinone group was fed the same diet with 2 % cholesterol and Thymoquinone 100 mg/Kg BW/day, 200 mg/Kg BW/day or 400 mg/Kg BW/day. Results: The cholesterol-rich diet significantly increased Malondialdehyde (MDA) in the aortic blood vessels, as reflected by Thiobarbituric Acid-Reactive Substances (TBARS), inhibited endothelium-dependent vascular relaxations to acetylcholine and decrease cyclic GMP were compared with vessels from normal rabbits (negative control). In cholesterol-fed rabbits, Thymoquinone treatment decreased MDA in plasma production, improved endothelium-dependent relaxations to acetylcholine and increase cyclic GMP production. Conclusion: These results suggest that dietary treatment of rabbits with thymoquinone may prevent superoxide anion (O2-) induced inactivation of endothelium-dependent relaxing factor (EDRF), improve the endothelium-dependent relaxation to acetylcholine in the aortic blood vessels, and increase cyclic GMP content in aortic of cholesterol-fed rabbits.

Respiratory diseases, spanning from the common cold to severe conditions such as pneumonia and COVID-19, pose significant challenges to global health and contribute significantly to morbidity and mortality. The emergence of COVID-19 has heightened the requirement for effective therapeutic strategies. This review article examines the potential of specific medicinal plants, namely Black Cumin, Licorice, and Echinacea, and their phytoconstituents in the treatment of respiratory diseases, with a focus on COVID-19. It synthesizes extant knowledge on the therapeutic efficacy of these plants, which have been used traditionally in Unani, Ayurvedic, and Chinese medicine to alleviate respiratory symptoms and boost immune functions. This review also discusses the immunomodulatory and antiviral properties of these three specific medicinal plants, as well as their function in the treatment of a number of life-threatening diseases. Incorporating insights from ethnomedicine and contemporary scientific research, this review highlights the urgency of exploring herbal medicines as complementary therapies for respiratory diseases and offers perspectives on incorporating these natural remedies into contemporary treatment paradigms, particularly in the fight against COVID-19. [ J Adv Biotechnol Exp Ther 2024; 7(1.000): 205-220]

Background: Sleep and stress interact bidirectionally by acting on brain circuits that affect metabolism. Sleep and its alterations have impact on blood leptin levels, metabolic hormone that regulates appetite. Brain expresses the receptors for the peptide hormone leptin produced from adipocytes. The hypothalamic orexin neurons are low during sleep and active when awake, influenced by a complex interaction with leptin. Thymoquinone was found to be the major bioactive component of Nigella sativa. The aim of this study was to study the role of thymoquinone on sleep restriction and its mitigating effect on leptin-mediated signaling pathway in rat brain. Methods and results: 30 adult male Wistar rats were divided into 5 groups with 6 animals in each group: Control; Thymoquinone (TQ); Corn oil; Chronic Sleep restriction (CSR); and CSR + TQ. After 30 days, behavioral analysis, antioxidant, lipid profile, glucose level, liver and kidney function test, neurotransmitters, neuropeptides, and mRNA expression in in vivo studies were also assessed and pharmacokinetic and docking were done for thymoquinone. Thymoquinone has also shown good binding affinity to the target proteins. CSR has induced oxidative stress in the discrete brain regions and plasma. Current study has shown many evidences that sleep restriction has altered the neurobehavioral, antioxidant status, lipid profile, neurotransmitters, neuropeptide levels, and feeding behavior which damage the Orexin–leptin system which regulates the sleep and feeding that leads to metabolic dysfunction. Conclusion: The potentiality of Thymoquinone was revealed in in silico studies, and its action in in vivo studies has proved its effectiveness. The study concludes that Thymoquinone has exhibited its effect by diminishing the metabolic dysfunction by its neuroprotective, antioxidant, and hypolipidemic properties. [ABSTRACT FROM AUTHOR]

Thymoquinone (TQ), a bioactive compound found in Nigella sativa seeds, possesses diverse therapeutic properties for skin conditions. However, formulating TQ presents challenges due to its hydrophobic nature and chemical instability, which hinder its skin penetration. Transethosomes, as a formulation, offer an environment conducive to enhancing TQ's solubility, stability, and skin permeation. To optimize TQ transethosomal formulations, we introduced a combination of ionic and nonionic surfactants, namely Tween 20 and sodium lauryl sulfate (SLS) or sodium lauroyl glutamate (SLG). Surfactants play a crucial role in stabilizing the formulation, reducing aggregation, improving biocompatibility, and minimizing potential toxicity. We fine-tuned the formulation composition and gained insights into its interfacial behavior using the Langmuir monolayer technique. This method elucidated the interfacial properties and behavior of phospholipids in ethosome and transethosome formulations. Our findings suggest that monolayer studies can serve as the initial step in selecting surfactants for nanocarrier formulations based on their interfacial dilational rheology studies. It was found that the addition of surfactant to the formulation increased the elasticity considering the capability of transethosomes to significantly decrease their radius when permeating the skin barrier. The results of the dilational rheology experiments were most relevant to drug permeation through the skin for the largest amplitude of deformation. The combination of Tween 20 and SLS efficiently modified the rheological behavior of lipids, increasing their elasticity. This conclusion was supported by in vitro studies, where formulation F2 composed of Tween 20 and SLS demonstrated the highest permeation after 24 h (300.23 µg/cm2). Furthermore, the F2 formulation showed the highest encapsulation efficiency (EE) of 94%, surpassing those of the control and ethosomal formulations. Additionally, this transethosomal formulation exhibited antimicrobial activity against S. aureus, with a zone of inhibition of 26.4 ± 0.3 mm. Importantly, we assessed the cytotoxicity of both ethosomes and transethosomes at concentrations ranging from 3.5 µM to 50 µM on HaCaT cell lines and found no cytotoxic effects compared to TQ hydroethanolic solution. These results suggest the potential safety and efficacy of TQ transethosomal formulations. [ABSTRACT FROM AUTHOR]

Thymoquinone, a significant component in medicine and the spice industry due to its potent antioxidant properties, is the focus of this paper. The development of a titanium oxide-modified graphite paste electrode is presented for the detection of thymoquinone in black cumin. The electrochemical characteristics of the thymoquinone molecule were explored in a 0.1 M phosphate buffer solution of pH of 6. The modified graphite paste electrode exhibits excellent linearity across the concentration range of 0.1-200 μ M with limit of detection is 0.02 μ M. The developed electrode exhibits commendable repeatability, reproducibility and exceptional sensitivity towards thymoquinone. The separation of various concentrations of thymoquinone samples such as Mousumi, Priya Gold, Sunrise and DNV using Principal Component Analysis (PCA) with the Separability Index (SI) of 67.89 utilized to differentiate between different thymoquinone concentrations. [ABSTRACT FROM AUTHOR]

Thymoquinone (TQ), a bioactive compound found in Nigella sativa seeds, has gained considerable attention due to its potential therapeutic properties. This study aimed to isolate and characterize TQ from Nigella sativa essential oil and evaluate its antioxidant capacity, antibacterial activity, and cytotoxic effects on lung cancer A549 cells. Moreover, The binding potential of TQ to Keap1 (Kelch-like ECH associated protein 1) was investigated through molecular docking. The stability of the resulting complex was evaluated through molecular dynamics (MD) simulation. The CUPRAC assay revealed significant antioxidant capacity of TQ, as indicated by its high molar absorptivity coefficient. TQ also demonstrated notable free radical scavenging activity, with efficacy increasing with concentration. In terms of antiquorum sensing activity, TQ displayed effectiveness against all tested virulence factors in P. aeruginosa PAO1 and Chromobacterium violaceum in different range. Additionally, TQ induced cytotoxicity in non-small lung cancer cells, inhibiting cell viability. In conclusion, this study successfully isolated and characterized TQ from Nigella sativa seeds and demonstrated its remarkable antioxidant capacity, antibacterial activity, and cytotoxic effects on lung cancer cells. These findings suggest the potential of TQ for various applications in the food and pharmaceutical industries. The wet-lab study demonstrated that TQ had an antioxidant effect. The TQ was found to have high binding potential to Keap1 as it formed four conventional hydrogen bonds with the protein. The resulting Keap1-TQ complex was also found to be stable. Further research is warranted to explore the therapeutic potential of TQ and develop novel treatments based on its properties. [ABSTRACT FROM AUTHOR]

Blastocystis is enteric parasites that live in both humans and animals gastrointestinal tracts. Metronidazole (MTZ) is generally preferred in the treatment of Blastocystis infection. However, it has been shown to have teratogenic and carcinogenic potential, causing various side effects. In this study, we have made an attempt to find an alternative drug with less toxic side effects in the treatment of Blastocystis. For this purpose, the anti-Blastocystis activities of thymoquinone (TQ) and capsaicin (CAP) were evaluated in vitro. Blastocystis isolate was inoculated in Jones medium in 1.5 mL eppendorf tubes supplemented with fetal calf serum (FCS) and incubated at 37°C. The anti-Blastocystis effect of TQ and CAP was evaluated by light microscopy (LM) and scanning electron microscopy (SEM). Both TQ and CAP had anti Blastocystis effects. It was observed that 500 ug/mL of TQ and 1000 ug/mL of CAP inhibited 100% of Blastocystis growth. In the LM and SEM images, it was observed that Blastocystis treated with TQ decreased in size and CAP had an effect on the cell surface when compared to the control group. It was concluded that TQ could be a more reliable anti-Blastocystis drug compared to MTZ and CAP, but more comprehensive studies should be performed. [ABSTRACT FROM AUTHOR]

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Thymoquinone (THQ) and its nanoformulation (NFs) have emerged as promising candidates for the treatment of neurological diseases due to their diverse pharmacological properties, which include anti-inflammatory, antioxidant, and neuroprotective effects. In this study, we conducted an extensive search across reputable scientific websites such as PubMed, ScienceDirect, Scopus, and Google Scholar to gather relevant information. The antioxidant and anti-inflammatory properties of THQ have been observed to enhance the survival of neurons in affected areas of the brain, leading to significant improvements in behavioral and motor dysfunctions. Moreover, THQ and its NFs have demonstrated the capacity to restore antioxidant enzymes and mitigate oxidative stress. The primary mechanism underlying THQ's antioxidant effects involves the regulation of the Nrf2/HO-1 signaling pathway. Furthermore, THQ has been found to modulate key components of inflammatory signaling pathways, including toll-like receptors (TLRs), nuclear factor-κB (NF-κB), interleukin 6 (IL-6), IL-1β, and tumor necrosis factor alpha (TNFα), thereby exerting anti-inflammatory effects. This comprehensive review explores the various beneficial effects of THQ and its NFs on neurological disorders and provides insights into the underlying mechanisms involved. [ABSTRACT FROM AUTHOR]

The FMS-like tyrosine kinase-3 internal tandem duplication (FLT3-ITD) represents a distinct genetic mutation that characterizes acute myeloid leukaemia (AML). The breakpoint cluster region (BCR)-Abelson murine leukaemia (ABL) (BCR-ABL) is a key initiator of chronic myeloid leukaemia (CML) Hyperactivation of phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) signalling is crucial in AML and CML pathogenesis. The recent development of tyrosine kinase inhibitors (TKIs) contributed to substantial improvements in leukaemia therapy. However, most leukaemia patients fail to completely recover and develop drug resistance after prolonged TKI therapy. Thymoquinone (TQ), a major ingredient of Nigella sativa seeds, has anti-tumour properties in a variety of cancers. However, the anti-leukemia effect of TQ was not extensively studied. Thus, the current research aims to identify TQ’s ability to bind on the active sites inFLT3-ITD, BCR-ABL, PI3K, Akt, and mTOR tyrosine kinases. The molecular docking of TQ toFLT3-ITD, BCR-ABL, PI3K, Akt, and mTOR was evaluated. Midostaurin; FLT3-ITD inhibitor, imatinib; BCR-ABL inhibitor, wortmannin; PI3K inhibitor, AZD5363; Akt inhibitor, and rapamycin; mTOR inhibitor were selected as positive controls. The findings revealed that TQ interacts with high affinities with the active site of PI3K(-7.02Kcal/mol), Akt(-6.4Kcal/mol), mTOR(-6.58Kcal/mol), FLT3- ITD(-6.35Kcal/mol), and BCR-ABL(-6.31Kcal/mol) and with low free binding energy to inhibit their enzymatic activities. In conclusion, TQ could potentially act as a TKI for FLT3- ITD, BCR-ABL, PI3K, Akt, and mTOR tyrosine kinases suggesting that TQ could act as a promising multi-targeted TKI for several tyrosine kinases for AML and CML treatment. [ABSTRACT FROM AUTHOR]

Multiple sclerosis (MS) is a complex disorder, characterized by demyelination and loss of axonal parts of neurons in the central nervous system involving multiple genetic and environmental factors. Although, the demyelinated lesions develop throughout the brain, but more frequently are extensive in white matter. Currently, three different approaches are being utilized to treat MS, where synthetic drugs are the most frequently used but they do not cure the disease. Secondly, the stem cell therapy but this too has limited success in treating MS in humans. The thirds technique involving administering hormones has been found to be most effective method but this too have some significant side effects. Alternatively, natural products can potentially serve as an affordable and effective substitute for the treatment of MS with minimum or no side effects. Blackseeds (Nigella sativa) and honey possessing potent neuroprotective, antioxidant, and anti-inflammatory properties with no reported side effects can be a prospective candidate for an alternate remedial treatment of MS in animal model as well as in humans. In this study we established a new animal model (quail), to assess the synergistic efficacy of honey and black seed against demyelination within brain. A total of 35 male quails were used, among 10 were non treated and 25 were treated with 200 mg/kg/day cuprizone (CPZ) demyelination for six months to induce demyelination. After that they were divided into seven groups of five animal each where 3 CPZ treated groups received either honey, black seed oil or mixture of both for 6 weeks after demyelination. Behavioral tests were performed at the end of treatment. Afterwards, oligodendrocyte population was estimated in cerebellar white matter after histology. It was found that all three treatments efficiently induce remyelination. Interestingly, the mixture of honey and black seed was significantly more efficient than honey and black seed alone. Our data support the need of clinical trials for administration of N. sativa and honey in MS patients. [ABSTRACT FROM AUTHOR]

We aimed to evaluate the effects of the antioxidant thymoquinone on treated and untreated kidneys on histological and oxidative parameters as well as Kidney Injury Molecule (KIM-1) levels in an experimental unilateral ureteropelvic junction obstruction (UPJO) with resultant hydronephrosis (HN) model. In adherence to the Animal research: reporting of in vivo exepriments guidelines, 34 male Wistar rats were randomly divided into four groups which were named accordingly: “CO” (corn oil), “TQ” (thymoquinone and corn oil), “HNCO” (UPJO-HN and corn oil), “HNTQ” (UPJO-HN, thymoquinone and corn oil). Histologically, pelvic epithelial damage, glomerular shrinkage and sclerosis, tubular damage, interstitial edema-inflammation-fibrosis (IEIF), and vascular congestion were assessed. Biochemically, malondialdehyde (MDA), superoxide dismutase (SOD), glutathione reductase (GR) and KIM-1 levels were assessed. Macroscopic HN developed in all obstructed kidneys. Ipsilateral obstructed kidneys deteriorated in all histological parameters. Thymoquinone attenuated glomerular shrinkage and sclerosis alterations but increased vascular congestion. Contralateral non-obstructed kidneys also showed histological deterioration. Thymoquinone had beneficial effects in terms of IEIF presence in contralateral kidneys but it increased vascular congestion. MDA and SOD results were inconclusive. UPJO caused decreased GR levels in the ipsilateral kidneys but not in the contralateral ones. This effect was not ameliorated by thymoquinone treatment. KIM-1 levels were increased in ipsilateral obstructed kidneys with a lower level in HNTQ group than in HNCO. KIM-1 level of the ipsilateral HNTQ group was higher than in both non-obstructed ipsilateral kidney groups. The effect of thymoquinone in ameliorating bilaterally observed histological alterations was limited and controversial. Oxidative damage detected by GR measurements was not prevented by thymoquinone. Thymoquinone partially decreased the damage as evidenced by reduced KIM-1 levels in thymoquinone-treated obstructed kidneys. [ABSTRACT FROM AUTHOR]

Hepatocellular carcinoma is the most common primary malignant tumor of the liver, and its incidence is increasing worldwide. There is a need to develop new therapeutic strategies to treat the disease. In this study, we synthesised the oxime derivative of thymoquinone and investigated cytotoxicity, genotoxicity, and apoptosis in hepatocellular cancer cells. The synthesised thymoquinone-oxime structure was confirmed by NMR. After incubating the hepatocellular cancer cell line for 24 h, the cytotoxicity ATP by luminometric, intracellular reactive oxygen species, and intracellular calcium by fluorometric. The mitochondrial membrane potential was determined by flow cytometry. DNA damage by alkaline single-cell gel electrophoresis, and apoptosis damage by acridine orange/ethidium bromide double dye method. Concentrations of thymoquinone-oxime statistically increased cytotoxicity, intracellular reactive oxygen species, intracellular calcium, apoptosis, and DNA damage in a concentration-dependent manner. Mitochondrial membrane potential and glutathione levels are also decreased. These findings show that thymoquinone-oxime has an anti-tumor effect on hepatocellular carcinoma cells. Among many herbs, Black seed (Nigella sativa) belonging to the Ranunculaceae family has been recognised worldwide as one of the most valuable nutrient-rich herbs There is no relevant data on the effect of the newly synthesised oxime derivative of TQ (TQ-ox) in cancer cells HEP-G2 A new TQ derivative has a higher anti-tumor effect on hepatocellular carcinoma [ABSTRACT FROM AUTHOR]

Colon cancer is on the rise in both men and women. In addition to traditional treatment methods, herbal treatments from complementary and alternative medicine are actively followed. Naturally derived from plants, thymoquinone (TQ) has drawn a lot of attention in the field of cancer treatment. MK-801, an N-methyl-D-aspartate agonist, is used to improve memory and plasticity, but it has also lately been explored as a potential cancer treatment. This study aimed to determine the roles of N-Methyl-D-Aspartate agonists and Thymoquinone on mitochondria and apoptosis. HT-29 cells were treated with different TQ and MK-801 concentrations. We analyzed cell viability, apoptosis, and alteration of mitochondria. Cell viability significantly decreased depending on doses of TQ and MK-801. Apoptosis and mitochondrial dysfunctions induced by low and high doses of TQ and MK-801. Our study emphasizes the need for further safety evaluation of MK-801 due to the potential toxicity risk of TQ and MK-801. Optimal and toxic doses of TQ and MK-801 were determined for the treatment of colon cancer. It should be considered as a possibility that colon cancer can be treated with TQ and MK-801. [ABSTRACT FROM AUTHOR]

Pseudomonas aeruginosa belongs to the critical pathogens that represent a global public health problem due to their high rate of resistance as listed by WHO. P. aeruginosa can result in many nosocomial infections especially in individuals with compromised immune systems. Attenuating virulence factors by interference with quorum sensing (QS) systems is a promising approach to treat P. aeruginosa-resistant infections. Thymoquinone is a natural compound isolated from Nigella sativa (black seed) essential oil. In this study, the minimum inhibitory concentration of thymoquinone was detected followed by investigating the antibiofilm and antivirulence activities of the subinhibitory concentration of thymoquinone against P. aeruginosa PAO1. The effect of thymoquinone on the expression of QS genes was assessed by quantitative real-time PCR, and the protective effect of thymoquinone against the pathogenesis of PAO1 in mice was detected by the mouse survival test. Thymoquinone significantly inhibited biofilm, pyocyanin, protease activity, and swarming motility. At the molecular level, thymoquinone markedly downregulated QS genes lasI, lasR, rhlI, and rhlR. Moreover, thymoquinone could protect mice from the pathologic effects of P. aeruginosa increasing mouse survival from 20% to 100%. In conclusion, thymoquinone is a promising natural agent that can be used as an adjunct therapeutic agent with antibiotics to attenuate the pathogenicity of P. aeruginosa. [ABSTRACT FROM AUTHOR]

5‐Fluorouracil (5‐FU), which is one of the most widely used chemotherapy drugs, has various side effects on the heart. Thymoquinone (TMQ), the main bioactive component of Nigella sativa, has antioxidant and protective effects against toxicity. In this study, we investigated the protective effect of thymoquinone against cardiotoxicity caused by 5‐FU in vitro and in vivo models. H9C2 cells were exposed to 5‐FU and TMQ, and cell viability was evaluated in their presence. Also, 25 male Wistar rats were divided into five control groups, 5‐FU, 2.5, and 5 mg TMQ in nanoemulsion form (NTMQ) + 5‐FU and 5 mg NTMQ. Cardiotoxicity was assessed through electrocardiography, cardiac enzymes, oxidative stress markers, and histopathology. 5‐FU induced cytotoxicity in H9c2 cells, which improved dose‐dependently with NTMQ cotreatment. 5‐FU caused body weight loss, ECG changes (increased ST segment, prolonged QRS, and QTc), increased cardiac enzymes (aspartate aminotransferase [AST], creatine kinase‐myocardial band [CK‐MB], and lactate dehydrogenase [LDH]), oxidative stress (increased malondialdehyde, myeloperoxidase, nitric acid; decreased glutathione peroxidase enzyme activity), and histological damage such as necrosis, hyperemia, and tissue hyalinization in rats. NTMQ ameliorated these 5‐FU‐induced effects. Higher NTMQ dose showed greater protective effects. Thus, the results of our study indicate that NTMQ protects against 5‐FU cardiotoxicity likely through antioxidant mechanisms. TMQ warrants further research as an adjuvant to alleviate 5‐FU chemotherapy side effects. [ABSTRACT FROM AUTHOR]

The research aimed to investigate whether the combination of L-carnitine (LC) and thymoquinone (TQ) could lower the adverse effects of methotrexate (MTX), a widely used chemotherapy agent in cancer therapy, on testicular function. A total of seven groups were established (n=7); control group, LC (200 mg/kg PO), TQ (50 mg/kg PO), MTX (single IP dose of 20 mg/kg), LC+MTX, TQ+MTX, and LC+TQ+MTX. The use of MTX resulted in lower levels of testosterone, folliclestimulating hormone (FSH), and luteinizing hormone (LH) in the blood, accompanied by a significant rise in testicular MDA levels. Additionally, there was a notable decline in GSH, CAT, and SOD, indicating reduced antioxidant activity in the testicles. Furthermore, the histopathological examination of the testicles revealed disruptions caused by MTX, and the expression of caspase-3 in the testicles was documented. The combination of LC and TQ with MTX significantly increased testosterone, FSH, LD levels and restored oxidative damage markers (p<0.05) and improved histopathological scores and caspase-3 expression. In conclusion, our results demonstrate that LC and TQ exhibit substantial protective effects against testicular toxicity induced by MTX, primarily attributed to their antioxidant properties. [ABSTRACT FROM AUTHOR]

This article presents the findings of a study on the combined effects of paclitaxel and thymoquinone on MCF-7 breast cancer cell lines. The study suggests that the combination of these drugs has a significant anti-cancer activity on the cell lines, with a lower IC50 compared to the individual drugs. The document also highlights the need for further research on combination therapies and the challenges of chemotherapy resistance. It does not disclose any conflicts of interest or sources of support for the study. [Extracted from the article]

Thymoquinone (TQ) is a phytochemical compound present in Nigella sativa and has potential benefits for treating dermatological conditions such as psoriasis. However, its clinical use is limited due to its restricted bioavailability, caused mainly by its low solubility and permeability. To overcome this, a new transdermal drug delivery system is required. Nanoparticles are known to enhance material solubility and permeability, and hence, this study aimed to synthesize TQ-loaded L-arginine-based polyamide (TQ/Arg PA) nanocapsules incorporated into transdermal patches for prolonged delivery of TQ. To achieve this, Eudragit E polymer, plasticizers, and aloe vera as penetration enhancer were used to develop the transdermal patch. Furthermore, novel TQ/Arg-PA was synthesized via interfacial polymerization, and the resultant nanocapsules (NCs) were incorporated into the matrix transdermal patch. The Arg-PA NCs' structure was confirmed via NMR and FTIR, and optimal TQ/Arg-PA NCs containing formulation showed high entrapment efficiency of TQ (99.60%). Molecular and thermal profiling of TQ/Arg-PA and the transdermal patch revealed the effective development of spherical NCs with an average particle size of 129.23 ± 18.22 nm. Using Franz diffusion cells and synthetic membrane (STRAT M®), the in vitro permeation profile of the prepared patches demonstrated an extended release of TQ over 24 h, with enhanced permeation by 42.64% when aloe vera was employed. In conclusion, the produced formulation has a potential substitute for corticosteroids and other drugs commonly used to treat psoriasis due to its effectiveness, safety, and lack of the side effects typically associated with other drugs. [ABSTRACT FROM AUTHOR]

Psoriasis, a persistent immune-mediated inflammatory skin condition, affects approximately 2-3% of the global population. Current treatments for psoriasis are fraught with limitations, including adverse effects, high costs, and diminishing efficacy over time. Thymoquinone (TQ), derived from Nigella sativa seeds, exhibits promising anti-inflammatory, antioxidant, and immunomodulatory properties that could prove beneficial in managing psoriasis. However, TQ’s hydrophobic nature and poor bioavailability have hindered its usefulness as a therapeutic agent. Recent research has strategically addressed these challenges by developing nano-thymoquinone (nano-TQ) formulations to enhance delivery and efficacy in treating psoriasis. Preclinical studies employing mouse models have demonstrated that nano-TQ effectively mitigates inflammation, erythema, scaling, epidermal thickness, and cytokine levels in psoriatic lesions. Various nano-TQ formulations, including nanoemulsions, lipid vesicles, nanostructured lipid carriers, and ethosomes, have been explored to improve solubility, facilitate skin penetration, ensure sustained release, and achieve site-specific targeting. Although clinical trials are currently scarce, the outcomes from in vitro and animal models are promising. The potential co-delivery of nano-TQ with other anti-psoriatic agents also presents avenues for further investigation.

Aim: Cisplatin (CIS), an antineoplastic agent, shows serious side effects such as hepatotoxicity. Thymoquinone (ThQ) is a powerful anti-oxidant with many beneficial effects such as anti-inflammatory, anti-tumoral. The aim of this study was to investigate whether ThQ treatment has hepatoprotective effect in CIS-induced hepatotoxicity model in rats and also to determine how CIS and/or ThQ treatments affect OTULIN levels, one of the deubiquitinases, in liver tissue. Materials and Methods: The 28 rats used in the study control (application not done), CIS (7 mg/kg CIS, first day of experiment, intraperitoneal), CIS+ThQ (7 mg/kg CIS, first day of experiment, intraperitoneal + 10 mg/kg/day ThQ, oral gavage) and ThQ (10 mg/kg/day ThQ, oral gavage) were divided into four equal groups (n=7). The experiment was terminated upon completion of all applications (day 15). The effects of CIS and\or ThQ apps on liver tissues were examined biochemically, histopathologically and immunohistochemically. Results: CIS application increased liver enzyme levels, histopathological changes, inflammation, oxidative stress and apoptosis in liver tissue and caused a decrease in OTULIN level. However, ThQ administration showed a positive regulatory effect on CIS-induced changes in liver tissue.. Conclusion: ThQ supplementation has a hepatoprotective effect against CISinduced liver tissue damage.

Objective(s): We aimed to investigate the levels of transient receptor potential melastatin (TRPM) gene expression, and the antioxidant and histopathologic effect of thymoquinone (Tmq) in the hepatic I/R rat model.Materials and Methods: Fifty Wistar rats were divided into 5 groups. Group 1: Control; Group 2: Sham; Group 3: Hepatic I/R (45 min/45 min); Group 4: Tmq (50 mg/kg); Group 5: Tmq+I/R (ten days before I/R at the dose of 50 mg/kg of Tmq). The hepatic I/R (45min/45min) model was performed at the portal vein and the hepatic artery with atraumatic vascular clamp in the ischemia groups. The liver tissues and blood samples that were taken at the end of the study were evaluated for histopathologic and biochemical analysis. Besides TRPM gene expression levels were determined in liver tissues. It was seen that cellular swelling, congestion, PNL, and apoptosis parameters statistically decreased in Tmq and Tmq+I/R groups in comparison with the I/R group in histopathological evaluation.Results: It was observed that biochemical parameters, AST, ALT, GGT, LDH, creatinine, and urea levels significantly increased in the I/R group as compared with, sham, Tmq, and Tmq+I/R groups. It was found that TRPM2,6,7,8 gene expression decreased significantly in Tmq+I/R groups as compared to the I/R group. Conclusion: We showed that thymoquinone can inhibit the entry of Ca+2 into the cell by decreasing TRPM2,6,7,8 gene expression. Based on our findings, we think that Tmq application in the treatment of liver diseases due to I/R damage may be important in terms of both ischemia and apoptosis and can also be used in the treatment of liver-related diseases.

Abstract Colorectal cancer (CRC) is deadly anaplastic changes in the gastrointestinal tract with high-rate mortality. In recent years, the application of phytocompounds has been extended along with different therapeutic protocols. Here, we monitored the effects of Thymoquinone (TQ) on autophagy via mitochondrial function after modulation of the Wnt/β-catenin signaling pathway. Human colorectal adenocarcinoma HT-29 cells were treated with TQ (60 µM) and 15 µM Wnt3a inhibitor (LGK974) for 48 h. The survival rate was evaluated using an MTT assay. The expression of Wnt-related factors (c-Myc, and Axin), angiogenesis (VE-Cadherin), and mitophagy-related factors (PINK1, OPTN) was assessed using real-time PCR assay. Protein levels of autophagy factors (Beclin-1, LC3, and P62) were monitored using western blotting. Using flow cytometry analysis, the intracellular accumulation of Rhodamine 123 was evaluated. The migration properties were analyzed using a scratch wound healing assay. Data indicated that TQ can reduce the viability of HT-29 cells compared to the control cells (p

Diabetic ketoacidosis (DKA) is regarded to be a communal complication of both type 1 and type 2 diabetes mellitus in children and adolescents. Successful therapy of DKA in children requires prompt diagnosis, strict monitoring of medical indicators, and prompt action. Thymoquinone (Tq) from black cumin loaded chitosan nanoparticles (ChNPs) intend to assess an effective agent to overcome this problem. XRD, FTIR, SEM, and TEM were used in the physicochemical analysis. Enzymatic activity of α-amylase and α-glucosidase was used in in vitro tests of anti-diabetic efficacy. Protecting insulin against enzyme breakdown is a crucial part of the insulin delivery mechanism. In the STZ-induced diabetes RIN-5F cell line, the anti-apoptotic capability of Tq-ChNPs was demonstrated through the NF-κB mediated apoptotic pathway. The combination of thymoquinone and chitosan NPs demonstrated that a wide variety of incredibly effective substances to elevate their curative effects, thus contributing to the growth of clinical and pharmaceutical fields.

Introduction: The Nigella sativa plant, commonly known as black seed, contains a significant compound known as thymoquinone, which exhibits remarkable therapeutic properties. This study aimed to assess the potential therapeutic effects of thymoquinone on the adverse effects of chlorpyrifos toxicity, considering the importance of reproductive capacity and the detrimental impacts of agricultural toxins. Materials and Methods: Various parameters were assessed in 36 NRMI male mice including testosterone and luteinizing hormone (LH) hormone secretion, sperm count and motility, as well as an antioxidant activity measured by TAC (Total Antioxidant Capacity), MDA (malondialdehyde), and SOD (Superoxide Dismutase). Both thymoquinone and chlorpyrifos were injected intraperitoneally for 14 days. Results: In tests related to sperms, chlorpyrifos caused a severe decrease in sperm motility and number (p

The spices and aromatic herbs were used not only in cooking to add flavour and smell to dishes but also for medicinal use. Nigella sativa, also called black cumin, is one of the species that contains an important bioactive component, thymoquinone (TQ), which has antioxidant, anti-inflammatory, antimicrobial, and antidiabetic effects. Curcuma longa, which also includes curcumin, has numerous anti-cancer properties. However, the bioavailability of curcumin is lower than that of its analogs. An analog of curcumin (EF-24), which has better bioavailability than curcumin, is capable of exerting a high anti-cancer effect. In our study, we determined the effects of PON1 enzyme activity on the proliferation and aggressiveness of glioblastoma cancer treated with TQ and EF-24 from lysates of the glioblastoma cell line U87MG. The results were determined as increased PON1 activity after treatment with TQ and EF-24 in the U87MG cell line (p