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thymoquinone cancer

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
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
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
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
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
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
Sedigheh Ganji-Harsini, Mozafar Khazaei, Zahra Rashidi, Ali Ghanbari
OBJECTIVE: Thymoquinone (TQ), as the main component of Nigella Sativa plant, shows anticancer properties. This study was aimed to evaluate the combined effect of TQ and Tamoxifen (TAM) on viability and apoptosis of human breast cancer cell lines. MATERIALS AND METHODS: In this experimental study, estrogen positive MCF-7 and estrogen negative MDA-MB-231 human breast cancer cell lines were induced by TAM (2 µM) or different doses of TQ (50, 75, 100, 150 µM), individually or in combination...
July 2016: Cell Journal
Jie Zheng, Yue Zhou, Ya Li, Dong-Ping Xu, Sha Li, Hua-Bin Li
Spices have been widely used as food flavorings and folk medicines for thousands of years. Numerous studies have documented the antioxidant, anti-inflammatory and immunomodulatory effects of spices, which might be related to prevention and treatment of several cancers, including lung, liver, breast, stomach, colorectum, cervix, and prostate cancers. Several spices are potential sources for prevention and treatment of cancers, such as Curcuma longa (tumeric), Nigella sativa (black cumin), Zingiber officinale (ginger), Allium sativum (garlic), Crocus sativus (saffron), Piper nigrum (black pepper) and Capsicum annum (chili pepper), which contained several important bioactive compounds, such as curcumin, thymoquinone, piperine and capsaicin...
August 12, 2016: Nutrients
Osama Adnan Kensara, Adel Galal El-Shemi, Amr Mohamed Mohamed, Bassem Refaat, Shakir Idris, Jawwad Ahmad
Colorectal cancer (CRC) is one of the most prevalent cancers and has a high mortality rate. Insensitivity and the limited therapeutic efficacy of its standard chemotherapeutic drug, 5-fluorouracil (5-FU), represents an important challenge in CRC treatment. The robust antitumor properties of thymoquinone (TQ), the main bioactive constituent of Nigella sativa, have recently been demonstrated on different cancers. We investigated whether TQ could potentiate the chemopreventive effect of 5-FU to eradicate the early stages of CRC and elucidated its underlying mechanisms...
2016: Drug Design, Development and Therapy
Ning Zhu, Xuyong Zhao, Yijia Xiang, Shiyong Ye, Jie Huang, Wuming Hu, Linchun Lv, Chunlai Zeng
BACKGROUND: Pulmonary artery remodeling induced by excess proliferation, migration and apoptosis resistance of pulmonary arterial smooth muscle cells (PASMCs) is a key component in pulmonary artery hypertension (PAH). Thymoquinone (TQ) triggers cancer cells apoptosis through multiple mechanisms. In addition, TQ inhibits migration of human nonsmall-cell lung cancer cells and human glioblastoma cells. OBJECTIVES: In the current study, we investigated effects of TQ on MCT-induced PAH in rats and its underlying mechanisms...
October 15, 2016: International Journal of Cardiology
M M E Taha, B Y Sheikh, L Z A Salim, S Mohan, A Khan, B Kamalidehghan, F Ahmadipour, S I Abdelwahab
Nigella sativa is also known for its properties as a traditional herbal healing for many ailments. In this study, the anticancer properties of thyomquinone (TQ), the active ingredient of N. sativa, were studied using ovarian cancer cell line (Caov-3 cells). The anti-proliferative activity of TQ was determined using MTT and the apoptosis was investigated using Flowcytometry and Annexin-V Assays. Multiparameteric cytotoxicity bioassays were used to quantify the changes in cell permeability and mitochondrial membrane potential...
May 30, 2016: Cellular and Molecular Biology
Hojjatollah Shokri
Nigella sativa (N. sativa) grows in various parts of the world, particularly in Iran. It has been traditionally used as a folk remedy to treat a number of diseases. The seeds of this plant contain moisture, proteins, carbohydrates, crude fiber, alkaloids, saponins, ash, fixed oils and essential oil. The major components of the essential oil are thymoquinone, p-cymene, trans-anethole, 2-methyl-5(1-methyl ethyl)-Bicyclo[3.1.0]hex-2-en and γ-terpinene. So far, several pharmacological effects such as anti-oxidant, anti-inflammatory, anti-cancer and anti-microbial have been reported for N...
January 2016: Avicenna Journal of Phytomedicine
Farzaneh Shakeri, Zahra Gholamnezhad, Bruno Mégarbane, Ramin Rezaee, Mohammad Hosein Boskabady
Gastrointestinal (GI) diseases affect a large number of people all over the world. Uncontrolled acid secretion and occurrence of gastric ulcers are common disorders of GI tract which pose serious problems to human health. Many synthetic drugs have been used to treat GI disorders but a definite cure has not been discovered so far and the available medications cause several side effects. Nigella sativa (N. sativa) (Ranunculacea) has several therapeutic effects which are attributed to its constituents like nigellicine, nigellidine, thymoquinone, dithymoquinone, thymol and carvacrol...
January 2016: Avicenna Journal of Phytomedicine
Xinming Su, Yuan Ren, Na Yu, Lingfei Kong, Jian Kang
Asthma is a chronic obstructive disease which is characterized by recurring airway inflammation, reversible airway obstruction, airway hyper responsiveness and vascular remodeling. Thymoquinone (TQ), an active ingredient isolated from Nigella sativa, was reported to exhibit anti-inflammation and anti-proliferation of in various cancer cells as well as epithelial cells. The aim of this study was to evaluate the effect of TQ on the inflammation, neoangiogenesis and vascular remodeling induced by Ovalbumin (OVA) in asthma mice in vivo and the anti-angiogenesis effects of TQ in VEGF-induced human umbilical vein endothelial cells (HUVECs) in vitro...
September 2016: International Immunopharmacology
Mehdi Nikbakht Dastjerdi, Ebrahim Momeni Mehdiabady, Farhad Golshan Iranpour, Hamid Bahramian
BACKGROUND: Nigella sativa has been a nutritional flavoring factor and natural treatment for many ailments for so many years in medical science. Earlier studies have been reported that thymoquinone (TQ), an active compound of its seed, contains anticancer properties. Previous studies have shown that TQ induces apoptosis in breast cancer cells but it is unclear the role of P53 in the apoptotic pathway. Hereby, this study reports the potency of TQ on expression of tumor suppressor gene P53 and apoptosis induction in breast cancer cell line Michigan Cancer Foundation-7 (MCF-7)...
2016: International Journal of Preventive Medicine
Wen-Qian Zhu, Jun Wang, Xu-Feng Guo, Zhou Liu, Wei-Guo Dong
AIM: To elucidate the mechanism of thymoquinone (TQ)-induced apoptosis in human gastric cancer cells in vitro and in vivo. METHODS: HGC27, BGC823, and SGC7901 cells were cultured in vitro and treated with TQ (0, 10, 25, 50, 75, 100, 125 μmol/L) for 12 h, 24 h, and 36 h, and then the proliferation inhibitory rates were detected by methylthiazole tetrazolium assay. Apoptosis was observed after Hoechst staining. The protein expressions of signal transducer and activator of transcription (STAT)3, p-STAT3, STAT5, p-STAT5, phospho-janus-activated kinase 2 (JAK2), JAK2, p-Src, Src, glyceraldehyde-3-phosphate dehydrogenase, lamin-A, survivin, Cyclin D, Bcl-2, Bax, peroxisome proliferator activated receptor, and caspase-3,7,9 were detected by western blot...
April 28, 2016: World Journal of Gastroenterology: WJG
H Sarman, R Bayram, S B Benek
OBJECTIVE: Osteosarcoma (OS) is the most common primary malignant tumor of the bone. Treatment options include surgery, chemotherapy, and radiotherapy. Following surgery, multi-agent chemotherapy drugs are effective but are associated with significant side effects and toxicity. Thymoquinone (TMQ) is a pharmacological component of black cumin that has multiple anti-tumorigenic effects. The goal of this study was to determine the effect of TMQ in combination with chemotherapy drugs on the growth inhibition of osteosarcoma and the potential clinical utility of TMQ in the treatment of OS...
April 2016: European Review for Medical and Pharmacological Sciences
Abdelkader E Ashour, Atallah F Ahmed, Ashok Kumar, Khairy M A Zoheir, Mourad A Aboul-Soud, Sheikh F Ahmad, Sabry M Attia, Adel R A Abd-Allah, Vino T Cheryan, Arun K Rishi
Medulloblastoma (MB) is the most common malignant brain tumor of childhood. The transcription factor NF-κB is overexpressed in human MB and is a critical factor for MB tumor growth. NF-κB is known to regulate the expression of interleukin-8 (IL-8), the chemokine that enhances cancer cell growth and resistance to chemotherapy. We have recently shown that thymoquinone (TQ) suppresses growth of hepatocellular carcinoma cells in part by inhibiting NF-κB signaling. Here we sought to extend these studies in MB cells and show that TQ suppresses growth of MB cells in a dose- and time-dependent manner, causes G2M cell cycle arrest, and induces apoptosis...
May 2016: Molecular and Cellular Biochemistry
Ming-Cheng Chen, Nien-Hung Lee, Hsi-Hsien Hsu, Tsung-Jung Ho, Chuan-Chou Tu, Ray-Jade Chen, Yueh-Min Lin, Vijaya Padma Viswanadha, Wei-Wen Kuo, Chih-Yang Huang
Clinically used chemotherapeutics can effectively eliminate most tumor cells. However, they cause unwanted side effects and result in chemoresistance. To overcome such problems, phytochemicals are now used to treat cancers by means of targeted therapy. Thymoquinone (TQ) is used to treat different cancers (including colon cancer) and is an NF-κB inhibitor. Irinotecan resistant (CPT-11-R) LoVo colon cancer cell line was previous constructed by step-wise CPT-11 challenges to un-treated parental LoVo cells and expresses EGFR/IKKα/β/NF-κB pathway...
April 5, 2016: Environmental Toxicology
Vandhana Muralidharan-Chari, Jaehan Kim, Ahlam Abuawad, Mubeena Naeem, Huadong Cui, Shaker A Mousa
Thymoquinone (THQ) is a major component of black seeds. Given that both THQ and black seeds exhibit anti-cancer and anti-inflammatory activities, we hypothesized that THQ will affect cancer-associated thrombosis (CAT), which is primarily triggered by tissue factor (TF) and inflammation. The effect of both black seed-extracted and purchased ("pure") THQ on normal blood coagulation was tested with in vitro thromboelastography (TEG) and activated partial thromboplastin time (aPTT) coagulation assays. The effect of pure THQ on CAT was tested with aPTT assay using pancreatic cancer cell lines that are either positive or negative for TF, and with TEG assay using lipopolysaccharide as an inflammatory trigger...
March 30, 2016: International Journal of Molecular Sciences
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