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thymoquinone

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https://www.readbyqxmd.com/read/28074457/the-acute-effects-of-thymoquinone-on-acute-peripheral-nerve-injury-an-experimental-study
#1
İsmail Gülşen, Hakan Ak, Mikail Kara, Abdulsemat Gökalp, Veysel Akyol, Ömer Faruk Koçak, Murat Çetin Rağbetli
BACKGROUND: The purpose of this study was to evaluate the acute effects of thymoquinone (TQ) on acute nerve injury. METHODS: A rat model of crush injury of the sciatic nerve was used. Animals were divided into 3 groups: control, trauma, and TQ treatment groups (n=6 per group). Seven days after injury, sciatic nerve specimens were obtained from the site of the injury and analyzed histologically and stereologically. Axon diameter, myelin thickness, and axon density were measured...
November 2016: Ulusal Travma Ve Acil Cerrahi Dergisi, Turkish Journal of Trauma & Emergency Surgery: TJTES
https://www.readbyqxmd.com/read/28031346/insecticidal-activity-of-thymoquinone-and-related-compounds-against-culex-quinquefasciatus-diptera-culicidae
#2
Mariah L Scott, Mary F Adams, Joseph J Karchesy, Janet C McAllister
Insecticides based on botanical sources have taken on increased attention due to differing modes of action from current insecticides in use and the view that they may be environmentally friendly. Thymoquinone, a component in the essential oil of incense cedar heartwood, has been shown to have insecticidal action against adult mosquitoes. This study evaluated relative toxicities of thymoquinone, selected derivatives of thymoquinone, hydroquinone, and arbutin to determine if any had similar or better activity...
December 28, 2016: Journal of Medical Entomology
https://www.readbyqxmd.com/read/28024529/fungicidal-effect-of-thymoquinone-involves-generation-of-oxidative-stress-in-candida-glabrata
#3
Hala Almshawit, Ian Macreadie
The antifungal effect of thymoquinone, a component of black seed essential oil, has been studied on different types of fungi. Its mechanism of action as an antifungal has not been described yet. This study demonstrates the fungicidal effect of thymoquinone on different Candida species with particular emphasis on C. glabrata planktonic cells and biofilms. Since cell death was induced via the generation of oxidative stress as evidenced by the abrogation of thymoquinone toxicity in cells incubated with antioxidants, a part of thymoquinone's mechanism of action includes a direct involvement as a pro-oxidant...
January 2017: Microbiological Research
https://www.readbyqxmd.com/read/28001351/proteoform-specific-protein-binding-of-small-molecules-in-complex-matrices
#4
Geuncheol Gil, Pan Mao, Bharathi Avula, Zulfiqar Ali, Amar G Chittiboyina, Ikhlas A Khan, Larry A Walker, Daojing Wang
Characterizing the specific binding between protein targets and small molecules is critically important for drug discovery. Conventional assays require isolation and purification of small molecules from complex matrices through multistep chromatographic fractionation, which may alter their original bioactivity. Most proteins undergo posttranslational modification, and only certain proteoforms have the right conformation with accessible domains and available residues for small molecule binding. We developed a top-down mass spectrometry (MS) centric workflow for rapid evaluation of the bioactivity of crude botanical extracts after a one-step reaction...
December 21, 2016: ACS Chemical Biology
https://www.readbyqxmd.com/read/27973725/synthesis-of-novel-hybrids-of-thymoquinone-and-artemisinin-with-high-activity-and-selectivity-against-colon-cancer
#5
Tony Fröhlich, Benardina Ndreshkjana, Julienne K Muenzner, Christoph Reiter, Elisabeth Hofmeister, Sandra Mederer, Maamoun Fatfat, Chirine El-Baba, Hala Gali-Muhtasib, Regine Schneider-Stock, Svetlana B Tsogoeva
Colorectal cancer causes 0.5 million deaths each year. To combat this type of cancer the development of new specific drug candidates is urgently needed. In the present work seven novel thymoquinone-artemisinin hybrids with different linkers were synthesized for the first time and tested for their in vitro anticancer activity in a panel of different tumor cell lines. The thymoquinone-artesunic acid hybrid 7a was found to be the most active compound and selectively reduced the viability of colorectal cancer cells with an IC50 of 2...
December 14, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27916297/protective-effects-of-thymoquinone-and-avenanthramides-on-titanium-dioxide-nanoparticles-induced-toxicity-in-sprague-dawley-rats
#6
Khaled M A Hassanein, Yasmin O El-Amir
The protective effect of thymoquinone (TQ), the major active ingredient of Nigella sativa seeds, and avenanthramides (AVA) enriched extract of oats on titanium dioxide naonparticles (TiO2 NPs) induced toxicity and oxidative stress in Sprague-Dawley (SD) rats was investigated. Sixty rats were divided into 6 equal groups. The first, second, third, fourth and fifth groups received TiO2 NPs, TiO2 NPs and TQ, TiO2 NPs and AVA, TQ only, or AVA only for 6 weeks. The sixth group served as the control. Exposure to TiO2 NPs resulted in increased liver enzyme markers, oxidative stress indices, tumor necrosis factor alpha (TNF-α) and DNA damage...
January 2017: Pathology, Research and Practice
https://www.readbyqxmd.com/read/27877037/acute-and-subacute-toxicity-profiles-of-thymoquinone-loaded-nanostructured-lipid-carrier-in-balb-c-mice
#7
Yong Sze Ong, Latifah Saiful Yazan, Wei Keat Ng, Mustapha M Noordin, Sarah Sapuan, Jhi Biau Foo, Yin Sim Tor
BACKGROUND: Thymoquinone (TQ), the predominant active lipophilic component in Nigella sativa seed oil, has a variety of pharmacological properties such as anticancer activities. However, translation of TQ to clinical phase is still not possible due to its hydrophobic properties. This problem can be solved by encapsulating it in nanoformulations to enhance its pharmacological properties. In our previous study, TQ has been successfully encapsulated in a nanostructured lipid carrier (hereinafter referred to as TQNLC) with excellent physiochemical properties such as high encapsulation efficiency, high drug-loading capacity, particle diameter less than 100 nm, and stability up to 2 years...
2016: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/27874094/identification-of-polo-like-kinase-1-interaction-inhibitors-using-a-novel-cell-based-assay
#8
Karine Normandin, Jean-François Lavallée, Marie Futter, Alexandre Beautrait, Jean Duchaine, Sébastien Guiral, Anne Marinier, Vincent Archambault
Polo-like kinase 1 (Plk1) plays several roles in cell division and it is a recognized cancer drug target. Plk1 levels are elevated in cancer and several types of cancer cells are hypersensitive to Plk1 inhibition. Small molecule inhibitors of the kinase domain (KD) of Plk1 have been developed. Their selectivity is limited, which likely contributes to their toxicity. Polo-like kinases are characterized by a Polo-Box Domain (PBD), which mediates interactions with phosphorylation substrates or regulators. Inhibition of the PBD could allow better selectivity or result in different effects than inhibition of the KD...
November 22, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27826979/the-anti-inflammatory-and-antioxidant-effects-of-thymoquinone-on-ceruleine-induced-acute-pancreatitis-in-rats
#9
A Dur, H Kose, A Kocyigit, O Kocaman, M Ismayilova, F C Sonmez
INTRODUCTION: The aim of this study is to investigate the potential antioxidant and anti-inflammatory effects of thymoquinone (TQ) on ceruleine induced acute pancreatitis. MATERIAL AND METHODS: A total of 14 male Wistar albino rats were divided into 2 groups as follows: (1) normal saline-treated group and (2) thymoquinone- treated groups. For achieving acute pancreatitis, intraperitoneal (IP) cerulein, a stable cholecystokinin (CCK) analogue, was applied in a 50 mcg/kg dose 2 times in one-hour interval in total...
2016: Bratislavské Lekárske Listy
https://www.readbyqxmd.com/read/27823964/michael-acceptor-containing-drugs-are-a-novel-class-of-5-lipoxygenase-inhibitor-targeting-the-surface-cysteines-c416-and-c418
#10
Isabelle V Maucher, Michael Rühl, Simon B M Kretschmer, Bettina Hofmann, Benjamin Kühn, Jasmin Fettel, Anja Vogel, Karsten T Flügel, Georg Manolikakes, Nadine Hellmuth, Ann-Kathrin Häfner, Vahid Golghalyani, Ann-Katrin Ball, Matthias Piesche, Carmela Matrone, Gerd Geisslinger, Michael J Parnham, Michael Karas, Dieter Steinhilber, Jessica Roos, Thorsten J Maier
Recently, we published that nitro-fatty acids (NFA) are potent electrophilic molecules which inhibit 5-lipoxygenase (5-LO) by interacting catalytically with cysteine residues next to a substrate entry channel. The electrophilicity is derived from an intramolecular Michael acceptor moiety consisting of an electron-withdrawing group in close proximity to a double bond. The potential of the Michael acceptor moiety to interact with functionally relevant cysteines of proteins potentially renders them effective and sustained enzyme activity modulators...
November 4, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27774648/phytoconstituents-as-pharmacotherapeutics-in-rheumatoid-arthritis-challenges-and-scope-of-nano-submicromedicine-in-its-effective-delivery
#11
REVIEW
Mahfoozur Rahman, Sarwar Beg, Amita Verma, Fahad A Al Abbasi, Firoz Anwar, Sumant Saini, Sohail Akhter, Vikas Kumar
OBJECTIVES: The present review explores the therapeutic application of herbals in rheumatoid arthritis (RA) therapy, and how nano/submicromedicine can be fit in the scope of its therapeutic delivery in RA has been addressed. KEY FINDINGS: Incorporation of bioactive such as polyphenols, thymoquinone, resveratrol, hesperidin, curcumin, celastrol and gambogic acid in a dose-dependent manner showed quite high efficacy for the treatment of RA. It can be attributed to their targeting ability against various inflammatory mediators including nitric oxide (NO), cytokines, chemokines, adhesion molecules, NF-kβ, lipoxygenase (LOXs) and arachidonic acid (AA)...
January 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27766410/the-therapeutic-effect-of-thymoquinone-on-acoustic-trauma-induced-hearing-loss-in-rats
#12
Mahmut Ogurlu, Ozlem Celebi Erdivanli, Levent Tumkaya, Abdulkadir Ozgur, Zerrin Ozergin Coskun, Suat Terzi, Munir Demirci, Engin Dursun
Thymoquinone has antioxidant properties. We hypothesized that thymoquinone may prevent or alleviate hearing loss induced by acoustic trauma. We aimed to study thymoquinone's effect on hearing function with distortion-product otoacoustic emissions and auditory brainstem response. Thirty adult Spraque Dawley rats were randomized into four groups following exposure to acoustic trauma for 4 h. Control group (n = 7) did not receive further treatment. Thymoquinone-20 (n = 8) and Thymoquinone-40 (n = 8) received 20 and 40 mg/kg of intraperitoneal thymoquinone, respectively...
October 20, 2016: European Archives of Oto-rhino-laryngology
https://www.readbyqxmd.com/read/27761068/potential-therapeutic-agents-for-the-treatment-of-fatty-degeneration-of-liver-and-atheromatous-plaques-an-experimental-study-in-rats
#13
Sibghatullah Muhammad Ali Sangi
BACKGROUND: Since long high fat diet (HFD) is being blamed for causing fatty degeneration of liver and formation of atheromatous plaques. At present, no proper pharmacotherapy is available for both the conditions. In this study, different substances containing monounsaturated fatty acids were used to observe their protective effects in the HFD induced damage to liver and coronary vessels. OBJECTIVES: To discover effective therapeutic agents for HFD induced fatty degeneration of liver and atheromatous plaques...
July 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27752802/protective-effects-of-thymoquinone-against-convulsant-activity-induced-by-lithium-pilocarpine-in-a-model-of-status-epilepticus
#14
Yiye Shao, Yonghao Feng, Yangmei Xie, Qiong Luo, Long Chen, Bing Li, Yinghui Chen
Inflammation plays a pivotal role in status epilepticus (SE). Thymoquinone (TQ) is a bioactive monomer extracted from black seed (Nigella sativa) oil, which has anti-inflammatory properties in the context of various diseases. This study explored the protective effects of TQ in SE and used a lithium-pilocarpine model of SE to investigate the underlying mechanism, which was related to inflammation mediated by the NF-κB signaling pathway. In the present study, latency to SE increased in the TQ-pretreated group compared with the SE group, and the incidence of SE was significantly reduced...
December 2016: Neurochemical Research
https://www.readbyqxmd.com/read/27748062/comparison-of-combined-antioxidants-and-thymoquinone-in-the-prevention-of-testis-ischemia-reperfusion-injury
#15
B Erol, U Sari, A S Amasyali, S Ozkanli, S Sogut, V Hanci, O Efiloglu, Y O Danacioglu, P Engin, F Yencilek, G Atis, A Yildirim, O A Alkoc, T Caskurlu
We aimed to compare the preventive effects of combined antioxidants (CA1, 2) with a single antioxidant drug (thymoquinone; TQ) on experimental testis Ischemia/Reperfusion (I/R) injury. Thirty-five adult male Wistar rats were divided into five groups of seven rats each: control, testis I/R, testis I/R + CA1, testis I/R + CA2, and testis I/R + TQ. After 1 h of testicular ischemia, reperfusion was achieved by detorsion for 4 h. Antioxidants were intraperitoneally administered for 30 min prior to reperfusion...
January 2017: Andrology
https://www.readbyqxmd.com/read/27746872/thymoquinone-synergistically-potentiates-temozolomide-cytotoxicity-through-the-inhibition-of-autophagy-in-u87mg-cell-line
#16
Mona Pazhouhi, Reyhaneh Sariri, Arezou Rabzia, Mozafar Khazaei
OBJECTIVES: Glioblastoma multiforme (GBM) is one of the most lethal forms of human cancer and temozolomide (TMZ) is currently part of the standard treatment for this disease. Combination therapy using natural substances can enhance the anti-cancer activity of TMZ. The purpose of this study was to evaluate the effect of TMZ in combination with thymoquinone (TQ) on human GBM cell line (U87MG). MATERIALS AND METHODS: The cell line was treated with TMZ and/or TQ. Cell viability was assessed using trypan blue and MTT assay...
August 2016: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/27725936/evaluation-of-neuroprotective-effect-of-thymoquinone-nanoformulation-in-the-rodent-cerebral-ischemia-reperfusion-model
#17
Xiao-Yu Xiao, Ying-Xian Zhu, Ju-Yuan Bu, Guo-Wei Li, Jian-Hui Zhou, Shao-Peng Zhou
The purpose of the present study was to evaluate the neuroprotective efficacy of optimized thymoquinone loaded PLGA-chitosan nanoparticles delivered via nose to brain route in the rodent cerebral ischemia-reperfusion model. The neuroprotective efficacy of the optimized thymoquinone loaded PLGA-chitosan nanoparticles was evaluated in middle cerebral artery occluded rats by various pharmacodynamic and biochemical studies. The pharmacokinetics of thymoquinone loaded PLGA-chitosan nanoparticles in the brain and blood plasma together with qualitative localization of florescent labelled PLGA-chitosan nanoparticles in brain tissues were also determined...
2016: BioMed Research International
https://www.readbyqxmd.com/read/27717985/thymoquinone-mitigate-ischemia-reperfusion-induced-liver-injury-in-rats-a-pivotal-role-of-nitric-oxide-signaling-pathway
#18
Mohamed Abd-Elbaset, El-Shaimaa A Arafa, Gamal A El Sherbiny, Mohamed S Abdel-Bakky, Abdel Nasser A M Elgendy
Oxidative and nitrosative stress-induced endothelial cell damage play an essential role in the pathogenesis of hepatic ischemia-reperfusion (IR) injury. IR is associated with reduced eNOS expression and exacerbated by superimposed stress. NOSTRIN induces intracellular endothelial nitric oxide synthase (eNOS) translocation and inducible nitric oxide synthase (iNOS) increases nitric oxide (NO) production. Our aim was to assess hepatic expression of iNOS, eNOS, and NOSTRIN in IR with or without N-acetylcysteine (NAC) or thymoquinone (TQ) pretreatment and to compare their hepatoprotective effects...
January 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27698868/thymoquinone-chemosensitizes-colon-cancer-cells-through-inhibition-of-nf-%C3%AE%C2%BAb
#19
Lida Zhang, Yangqiu Bai, Yuxiu Yang
In the present study, the effects and molecular mechanisms of thymoquinone (TQ) on colon cancer cells were investigated. Cell viability was determined using a Cell Counting Kit-8 assay, and the results revealed that treatment with TQ significantly decreased cell viability in COLO205 and HCT116 cells in a dose-dependent manner. TQ treatment additionally sensitized COLO205 and HCT116 cells to cisplatin therapy in a concentration-dependent manner. To investigate the molecular mechanisms of TQ action, western blot analysis was used to determine the levels of phosphorylated p65 and nuclear factor-κB (NF-κB)-regulated gene products vascular endothelial growth factor (VEGF), c-Myc and B-cell lymphoma 2 (Bcl-2)...
October 2016: Oncology Letters
https://www.readbyqxmd.com/read/27693336/anti-aggregation-property-of-thymoquinone-induced-by-copper-nanoparticles-a-biophysical-approach
#20
Mohd Ishtikhar, Rahisuddin, Mohsin Vahid Khan, Rizwan Hasan Khan
Quaternary amine of diethylaminoethyl rosin ester (QRMAE), chemically synthesized by rosin modified biocompatible cationic surfactant, has various biological applications in the field of pharmacy as well as used as food product additive. Here, we report biophysical insights in to the interaction mechanism of thymoquinone (TQ), copper nanoparticles (Cu-NPs) and QRMAE with bovine serum albumin (BSA) individually and also in complexes forms to determine their competitive binding affinity. We have also studied the aggregation-inhibition effects of Cu-NPs and TQ individually, as well as in complexes form in the presence of QRMAE surfactant which is responsible for induction of amorphous aggregates in BSA within hours of incubation at 65°C and physiological pH...
December 2016: International Journal of Biological Macromolecules
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