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thymoquinone

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https://www.readbyqxmd.com/read/28223069/evaluation-of-antibacterial-potential-and-toxicity-of-plant-volatile-compounds-using-new-broth-microdilution-volatilization-method-and-modified-mtt-assay
#1
Marketa Houdkova, Johana Rondevaldova, Ivo Doskocil, Ladislav Kokoska
With aim to develop effective proof-of-concept approach which can be used in a development of new preparations for the inhalation therapy, we designed a new screening method for simple and rapid simultaneous determination of antibacterial potential of plant volatiles in the liquid and the vapour phase at different concentrations. In addition, EVA (ethylene vinyl acetate) capmat™ as vapour barrier cover was used as reliable modification of thiazolyl blue tetrazolium bromide (MTT) assay for cytotoxicity testing of volatiles on microtiter plates...
February 18, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28216638/thymoquinone-an-irak1-inhibitor-with-in-vivo-and-in-vitro-anti-inflammatory-activities
#2
Muhammad Jahangir Hossen, Woo Seok Yang, Daewon Kim, Adithan Aravinthan, Jong-Hoon Kim, Jae Youl Cho
Thymoquinone (TQ) is a bioactive component of black seed (Nigella sativa) volatile oil and has been shown to have anti-oxidative, anti-inflammatory, and anti-cancer properties. In the present study, we explored the molecular mechanisms that underlie the anti-inflammatory effect of TQ and its target proteins using lipopolysaccharide (LPS)-stimulated murine macrophage-like RAW264.7 and human monocyte-like U937 cells, together with LPS/D-galactosamine (GalN)-induced acute hepatitis and HCl/EtOH-induced gastritis mouse models...
February 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28195061/overview-of-the-preclinical-pharmacological-properties-of-nigella-sativa-black-seeds-a-complementary-drug-with-historical-and-clinical-significance
#3
E Z Dajani, T G Shahwan, N E Dajani
Nigella sativa (N. sativa, black seeds; or sometimes known by many other names such as the blessed seed by the Arabs, black cumin in the Holy Bible, black caraway and Kalonji in South Asia) has been traditionally used for many years not only as a food but also as complementary drug. It is the objective of this communication to review the evidence-based pre-clinical pharmacological actions of N. sativa as a basis of its existing and potential new human clinical uses. Primary PubMed literature searches and secondary Medline searches were conducted to define N...
December 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28163966/an-active-principle-of-nigella-sativa-l-thymoquinone-showing-significant-antimicrobial-activity-against-anaerobic-bacteria
#4
Mohammad Akram Randhawa, Awwad Khalaf Alenazy, Majed Gorayan Alrowaili, Jamith Basha
AIM/BACKGROUND: Thymoquinone (TQ) is the major active principle of Nigella sativa seed (black seed) and is known to control many fungi, bacteria, and some viruses. However, the activity of TQ against anaerobic bacteria is not well demonstrated. Anaerobic bacteria can cause severe infections, including diarrhea, aspiration pneumonia, and brain abscess, particularly in immunodeficient individuals. The present study aimed to investigate the in vitro antimicrobial activity of TQ against some anaerobic pathogens in comparison to metronidazole...
January 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28152102/anthelmintic-potential-of-thymoquinone-and-curcumin-on-fasciola-gigantica
#5
Rizwan Ullah, Abdur Rehman, Mohd Faraz Zafeer, Lubna Rehman, Yasir A Khan, M A Hannan Khan, Shahper N Khan, Asad U Khan, S M A Abidi
Fasciolosis an economically important global disease of ruminants in the temperate and tropical regions, caused by Fasciola hepatica and F. gigantica, respectively, also poses a potential zoonotic threat. In India alone it causes huge losses to stakeholders. Anthelmintics including triclabendazole have been used to control this menace but the emerging resistance against the available compounds necessitates identification of novel and alternative therapeutic measures involving plant derived natural compounds for their anthelmintic potential...
2017: PloS One
https://www.readbyqxmd.com/read/28140613/anti-cancer-properties-and-mechanisms-of-action-of-thymoquinone-the-major-active-ingredient-of-nigella-sativa
#6
Amin F Majdalawieh, Muneera W Fayyad, Gheyath K Nasrallah
Over the past two decades, studies have documented the wide-range anti-cancer effects of Nigella sativa, known as black seed or black cumin. Thymoquinone (TQ), its major active ingredient, has also been extensively studied and reported to possess potent anti-cancer properties. Herein, we provide a comprehensive review of the findings related to the anti-cancer activity of TQ. The review focuses on analyzing experimental studies performed using different in vitro and in vivo models to identify the anti-proliferative, pro-apoptotic, anti-oxidant, cytotoxic, anti-metastatic, and NK-dependent cytotoxic effects exerted by TQ...
January 31, 2017: Critical Reviews in Food Science and Nutrition
https://www.readbyqxmd.com/read/28131095/a-potential-mechanism-for-the-ameliorative-effect-of-thymoquinone-on-pentylenetetrazole-induced-kindling-and-cognitive-impairments-in-mice
#7
Ahmed O Abdel-Zaher, Hanan S M Farghaly, Magda M Y Farrag, Mahran S Abdel-Rahman, Basel A Abdel-Wahab
Cognitive dysfunction is commonly observed in epileptic patients. Pentylenetetrazole (PTZ) kindling is a well established animal model which simulates clinical epilepsy. This study evaluated the potential role of glutamate, oxidative stress and nitric oxide (NO) overproduction in pentylenetetrazole (PTZ)-induced kindling and associated cognitive impairments in mice and effect of thymoquinone on these parameters. Repeated treatment of mice with a subconvulsive dose of PTZ (35mg/kg i.p.) once every alternate-day for 12 injections induced kindling...
January 25, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28074457/the-acute-effects-of-thymoquinone-on-acute-peripheral-nerve-injury-an-experimental-study
#8
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
#9
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
#10
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
#11
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...
February 17, 2017: 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
#12
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 and tested for their in vitro anticancer activity against a panel of various tumor cell lines. The thymoquinone-artesunic acid hybrid 7 a, in which both subunits are connected via an ester bond, was found to be the most active compound and selectively decreased the viability of colorectal cancer cells with an IC50 value 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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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...
February 2017: 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
#20
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
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