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thymoquinone cancer

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https://www.readbyqxmd.com/read/28606050/insights-into-the-targeting-potential-of-thymoquinone-for-therapeutic-intervention-against-triple-negative-breast-cancer
#1
Md Abul Barkat, Harshita Abul, Javed Ahmad, Mohammad Ahmed Khan, Sarwar Beg, Farhan Jalees Ahmad
BACKGROUND: Thymoquinone (TQ) is a bioactive phytoconstituent obtained from Nigella sativa (black seeds). It has promising potential in cancer prevention. OBJECTIVE: Previous studies have shown that TQ can modulate signaling pathways responsible for cancer progression, thus enhances the efficacy and improve safety profile of clinically used anticancer drugs. METHOD: TQ acts on cell cycle and inhibits progression from G1 to S phase by targeting various proteins (cyclin D1, cyclin E, and p27)...
June 11, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28552110/antitumor-effect-of-thymoquinone-combined-with-resveratrol-on-mice-transplanted-with-breast-cancer
#2
Omar H Alobaedi, Wamidh H Talib, Iman A Basheti
OBJECTIVE: To test the anticancer potential activity of the combination of thymoquinone (TQ) and resveratrol (RES) against breast cancer in mice. METHODS: The antiproliferative activity of TQ, RES and their combination was assessed against three breast cancer cell lines and one normal cells using MTT assay. The combination index was calculated using isobolographic method. Balb/C mice were inoculated with EMT6/P cells and in vivo antitumor activity was evaluated...
April 2017: Asian Pacific Journal of Tropical Medicine
https://www.readbyqxmd.com/read/28521657/several-inhibitors-of-the-plk1-polo-box-domain-turn-out-to-be-non-specific-protein-alkylators
#3
Vincent Archambault, Karine Normandin
For almost a decade, there has been much interest in the development of chemical inhibitors of Polo-like kinase 1 (Plk1) protein interactions. Plk1 is a master regulator of the cell division cycle that controls numerous substrates. It is a promising target for cancer drug development. Inhibitors of the kinase domain of Plk1 had some success in clinical trials. However, they are not perfectly selective. In principle, Plk1 can also be inhibited by interfering with its protein interaction domain, the Polo-Box Domain (PBD)...
May 19, 2017: Cell Cycle
https://www.readbyqxmd.com/read/28503089/anticancer-chemodiversity-of-ranunculaceae-medicinal-plants-molecular-mechanisms-and-functions
#4
REVIEW
Da-Cheng Hao, Chun-Nian He, Jie Shen, Pei-Gen Xiao
The buttercup family, Ranunculaceae, comprising more than 2,200 species in at least 62 genera, mostly herbs, has long been used in folk medicine and worldwide ethnomedicine since the beginning of human civilization. Various medicinal phytometabolites have been found in Ranunculaceae plants, many of which, such as alkaloids, terpenoids, saponins, and polysaccharides, have shown anti-cancer activities in vitro and in vivo. Most concerns have been raised for two epiphany molecules, the monoterpene thymoquinone and the isoquinoline alkaloid berberine...
February 2017: Current Genomics
https://www.readbyqxmd.com/read/28489566/thymoquinone-as-an-anticancer-molecule-from-basic-research-to-clinical-investigation
#5
REVIEW
Md Asaduzzaman Khan, Mousumi Tania, Shangyi Fu, Junjiang Fu
Thymoquinone is an anticancer phytochemical commonly found in black cumin. In this review, we discuss the potential of thymoquinone as anticancer molecule, its mechanism of action and future usage in clinical applications. Thymoquinone exhibits anticancer activity via numerous mechanisms of action, specifically by showing selective antioxidant and oxidant activity, interfering with DNA structure, affecting carcinogenic signaling molecules/pathways and immunomodulation. In vitro activity of thymoquinone has been further implicated in animal models of cancer; however, no clinical application has been proven yet...
April 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28476718/review-therapeutic-implications-of-nigella-sativa-against-cancer-metastasis
#6
Muhammad Sheraz Arshad Malik, Soad K Al Jaouni, Steve M Harakeh, Muhammad Faraz Arshad Malik
Nigella sativa (N. sativa), remedial usage against different diseases associated with skeleton, cardiovascular, digestive and urinary systems has a long-standing history. At present, efforts are underway to study its effects against various cancers at both the cellular and molecular levels. In this review, the role of active constituents like thymoquinone (TQ) on different types of cancer has been explored. TQ putative involvement in metastasis has been assessed by elucidating its effects on cell proliferation, adhesion, invasion and angiogenesis...
September 2016: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28472683/thymoquinone-binds-and-activates-human-salivary-aldehyde-dehydrogenase-potential-therapy-for-the-mitigation-of-aldehyde-toxicity-and-maintenance-of-oral-health
#7
Amaj Ahmed Laskar, Masood Alam Khan, Fizza Askari, Hina Younus
Human salivary aldehyde dehydrogenase (hsALDH) is a very important anti-oxidant enzyme present in the saliva. It is involved in the detoxification of toxic aldehydes and maintenance of oral health. Reduced level of hsALDH activity is a risk factor for oral cancer development. Thymoquinone (TQ) has many pharmacological activities and health benefits. This study aimed to examine the activation of hsALDH by TQ. The effect of TQ on the activity and kinetics of hsALDH was studied. The binding of TQ with the enzyme was examined by different biophysical methods and molecular docking analysis...
May 1, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28423483/microrna-34a-targets-epithelial-to-mesenchymal-transition-inducing-transcription-factors-emt-tfs-and-inhibits-breast-cancer-cell-migration-and-invasion
#8
Saber Imani, Chunli Wei, Jingliang Cheng, Md Asaduzzaman Khan, Shangyi Fu, Luquan Yang, Mousumi Tania, Xianqin Zhang, Xiuli Xiao, Xianning Zhang, Junjiang Fu
MicroRNA-34a (miR-34a) plays an essential role against tumorigenesis and progression of cancer metastasis. Here, we analyzed the expression, targets and functional effects of miR-34a on epithelial to mesenchymal transition-inducing transcription factors (EMT-TFs), such as TWIST1, SLUG and ZEB1/2, and an EMT-inducing protein NOTCH1 in breast cancer (BC) cell migration and invasion and its correlation with tumorigenesis and clinical outcomes. Expression of miR-34a is downregulated in human metastatic breast cancers (MBC) compared to normal breast tissues and is negatively correlated with clinicopathological features of MBC patients...
March 28, 2017: Oncotarget
https://www.readbyqxmd.com/read/28415607/thymoquinone-exerts-potent-growth-suppressive-activity-on-leukemia-through-dna-hypermethylation-reversal-in-leukemia-cells
#9
Jiuxia Pang, Na Shen, Fei Yan, Na Zhao, Liping Dou, Lai-Chu Wu, Christopher L Seiler, Li Yu, Ke Yang, Veronika Bachanova, Eric Weaver, Natalia Y Tretyakova, Shujun Liu
Thymoquinone (TQ), a bioactive constituent of the volatile oil of Monarda fistulosa and Nigella sativa, possesses cancer-specific growth inhibitory effects, but the underlying molecular mechanisms remain largely elusive. We propose that TQ curbs cancer cell growth through dysfunction of DNA methyltransferase 1 (DNMT1). Molecular docking analysis revealed that TQ might interact with the catalytic pocket of DNMT1 and compete with co-factor SAM/SAH for DNMT1 inhibition. In vitro inhibitory assays showed that TQ decreases DNMT1 methylation activity in a dose-dependent manner with an apparent IC50 of 30 nM...
May 23, 2017: Oncotarget
https://www.readbyqxmd.com/read/28400978/thymoquinone-attenuates-brain-injury-via-an-anti-oxidative-pathway-in-a-status-epilepticus-rat-model
#10
Yi-Ye Shao, Bing Li, Yong-Mei Huang, Qiong Luo, Yang-Mei Xie, Ying-Hui Chen
AIM: Status epilepticus (SE) results in the generation of reactive oxygen species (ROS), which contribute to seizure-induced brain injury. It is well known that oxidative stress plays a pivotal role in status epilepticus (SE). Thymoquinone (TQ) is a bioactive monomer extracted from black cumin (Nigella sativa) seed oil that has anti-inflammatory, anti-cancer, and antioxidant activity in various diseases. This study evaluated the protective effects of TQ on brain injury in a lithium-pilocarpine rat model of SE and investigated the underlying mechanism related to antioxidative pathway...
January 2017: Translational Neuroscience
https://www.readbyqxmd.com/read/28355088/temozolomide-mediated-apoptotic-death-is-improved-by-thymoquinone-in-u87mg-cell-line
#11
Mozafar Khazaei, Mona Pazhouhi
Apoptosis induction of cancer cells can be an appropriate strategy by which chemotherapeutic agents kill tumor cells. The aim of the present study was to investigate the effect of temozolomide and thymoquinone combination on apoptotic pathway of human glioblastoma multiforme cell line (U87MG). U87MG cells were cultured, treated with temozolomide and thymoquinone, and cell proliferation was measured. Apoptosis cell death and its possible mechanism were investigated by various methods. Combination of temozolomide and thymoquinone had a synergistic effect on cells viability...
April 21, 2017: Cancer Investigation
https://www.readbyqxmd.com/read/28337306/thymoquinone-potentiates-chemoprotective-effect-of-vitamin-d3-against-colon-cancer-a-pre-clinical-finding
#12
Amr M Mohamed, Bassem A Refaat, Adel G El-Shemi, Osama A Kensara, Jawwad Ahmad, Shakir Idris
Prevention of colon cancer among high-risk group has been long lasting research goal. Emerging data have evidenced the anticancer activities of Vitamin D3 (Vit.D) and Thymoquinone (TQ). The aim of the current study was to evaluate the synergistic potential of Thymoquinone and Vitamin D3 in the control of colon cancer progression using azoxymethane-induced rat model. Vit.D and TQ were given individually or in combination 4 week prior to induction and continued for a total of 20 week. At the end of the study, all animals were euthanized and their resected colons were examined macroscopically and microscopically for tumor growth...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28275297/thymoquinone-suppresses-migration-of-lovo-human-colon-cancer-cells-by-reducing-prostaglandin-e2-induced-cox-2-activation
#13
Hsi-Hsien Hsu, Ming-Cheng Chen, Cecilia Hsuan Day, Yueh-Min Lin, Shin-Yi Li, Chuan-Chou Tu, Viswanadha Vijaya Padma, Hui-Nung Shih, Wei-Wen Kuo, Chih-Yang Huang
AIM: To identify potential anti-cancer constituents in natural extracts that inhibit cancer cell growth and migration. METHODS: Our experiments used high dose thymoquinone (TQ) as an inhibitor to arrest LoVo (a human colon adenocarcinoma cell line) cancer cell growth, which was detected by cell proliferation assay and immunoblotting assay. Low dose TQ did not significantly reduce LoVo cancer cell growth. Cyclooxygenase 2 (COX-2) is an enzyme that is involved in the conversion of arachidonic acid into prostaglandin E2 (PGE2) in humans...
February 21, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28250648/the-influence-of-pluronic-f68-and-f127-nanocarrier-on-physicochemical-properties-in-vitro-release-and-antiproliferative-activity-of-thymoquinone-drug
#14
Salwa Shaarani, Shahrul Sahul Hamid, Noor Haida Mohd Kaus
BACKGROUND: This study reports on hydrophobic drug thymoquinone (TQ), an active compound found in the volatile oil of Nigella sativa that exhibits anticancer activities. Nanoformulation of this drug could potentially increase its bioavailability to specific target cells. OBJECTIVE: The aim of this study was to formulate TQ into polymer micelle, Pluronic F127 (5.0 wt %) and Pluronic F68 (0.1 wt %), as a drug carrier to enhance its solubility and instability in aqueous media...
January 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28216638/thymoquinone-an-irak1-inhibitor-with-in-vivo-and-in-vitro-anti-inflammatory-activities
#15
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
#16
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/28140613/anti-cancer-properties-and-mechanisms-of-action-of-thymoquinone-the-major-active-ingredient-of-nigella-sativa
#17
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/28001351/proteoform-specific-protein-binding-of-small-molecules-in-complex-matrices
#18
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
#19
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/27877037/acute-and-subacute-toxicity-profiles-of-thymoquinone-loaded-nanostructured-lipid-carrier-in-balb-c-mice
#20
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
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