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Capsaicin and cancer

Tao Liu, Gang Wang, Huangheng Tao, Zhonghua Yang, Yongzhi Wang, Zhe Meng, Rui Cao, Yu Xiao, Xinghuan Wang, Jiajie Zhou
BACKGROUND: Renal cell carcinoma (RCC) is one of the tumors most refractory to chemotherapy to date. Therefore, novel therapeutic agents are urgently needed for this disease. Capsaicin (CPS), a natural active ingredient of green and red peppers, and a ligand of transient receptor potential vanilloid type 1 (TRPV1), has been showed potential in suppression of tumorigenesis of several cancers. Nonetheless, the anti-cancer activity of CPS has never been studied in human RCC. METHODS: CCK8 analysis, LDH release activity and ROS generation analysis, flow cytometry analysis, and nuclear staining test were performed to test the influence of CPS in cultured cells in vitro, meanwhile western blot was done to uncover the precise molecular mechanisms...
October 12, 2016: BMC Cancer
Fei Wang, Jiayao Zhao, Da Liu, Tong Zhao, Zeming Lu, Lin Zhu, Lingling Cao, Jiaxing Yang, Jingji Jin, Yong Cai
Capsaicin (CAP) is the major pungent component of chili pepper and is being evaluated for use against numerous types of tumors. Although CAP is indicated to target multiple signaling pathways, exact mechanisms of how it disturb cancer cell metablism remain obscure. Recent studies revealed Sirtuin 1 (SIRT1) serves as a potential target of CAP in cancer cells, indicating a direct regulation of cancer cell histone acetylation by capsaicin. The present study evaluated the effect of CAP on gastric cancer (GC) cell lines to understand the mechanism of cell growth inhibition...
October 7, 2016: Cancer Biology & Therapy
László Pecze, Walter Blum, Thomas Henzi, Beat Schwaller
Sensory neuron subpopulations as well as breast and prostate cancer cells express functional transient receptor potential vanilloid type 1 (TRPV1) ion channels; however little is known how TRPV1 activation leads to biological responses. Agonist-induced activation of TRPV1 resulted in specific spatiotemporal patterns of cytoplasmic Ca(2+) signals in breast and prostate cancer-derived cells. Capsaicin (CAPS; 50μM) evoked intracellular Ca(2+) oscillations and/or intercellular Ca(2+) waves in all cell lines. As evidenced in prostate cancer Du 145 cells, oscillations were largely dependent on the expression of functional TRPV1 channels in the plasma membrane, phospholipase C activation and on the presence of extracellular Ca(2+) ions...
September 20, 2016: Biochimica et Biophysica Acta
Alessia Garufi, Giuseppa Pistritto, Mara Cirone, Gabriella D'Orazi
BACKGROUND: Mutations in the p53 oncosuppressor gene are highly frequent in human cancers. These alterations are mainly point mutations in the DNA binding domain of p53 and disable p53 from transactivating target genes devoted to anticancer activity. Mutant p53 proteins are usually more stable than wild-type p53 and may not only impair wild-type p53 activity but also acquire pro-oncogenic functions. Therefore, targeting mutant p53 to clear the hyperstable proteins or change p53 conformation to reactivate wild-type p53 protein functions is a powerful anticancer strategy...
2016: Journal of Experimental & Clinical Cancer Research: CR
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...
2016: Nutrients
Félix A Urra, Boris Weiss-López, Ramiro Araya-Maturana
Recent evidence highlights that energy requirements of cancer cells vary greatly from normal cells and they exhibit different metabolic phenotypes with variable participation of both glycolysis and oxidative phosphorylation (OXPHOS). Interestingly, mitochondrial electron transport chain (ETC) has been identified as an essential component in bioenergetics, biosynthesis and redox control during proliferation and metastasis of cancer cells. This dependence converts ETC of cancer cells in a promising target to design small molecules with anti-cancer actions...
July 19, 2016: Current Pharmaceutical Design
Angela M Chapa-Oliver, Laura Mejía-Teniente
Capsaicinoids are plant secondary metabolites, capsaicin being the principal responsible for the pungency of chili peppers. It is biosynthesized through two pathways involved in phenylpropanoid and fatty acid metabolism. Plant capsaicin concentration is mainly affected by genetic, environmental and crop management factors. However, its synthesis can be enhanced by the use of elicitors. Capsaicin is employed as food additive and in pharmaceutical applications. Additionally, it has been found that capsaicin can act as a cancer preventive agent and shows wide applications against various types of cancer...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jong Hyun Lee, Chulwon Kim, Seung Ho Baek, Jeong-Hyeon Ko, Seok Geun Lee, Woong Mo Yang, Jae-Young Um, Gautam Sethi, Kwang Seok Ahn
Persistent STAT3 activation is seen in many tumor cells and promotes malignant transformation. Here, we investigated whether capsazepine (Capz), a synthetic analogue of capsaicin, exerts anticancer effects by inhibiting STAT3 activation in prostate cancer cells. Capz inhibited both constitutive and induced STAT3 activation in human prostate carcinoma cells. Capz also inhibited activation of the upstream kinases JAK1/2 and c-Src. The phosphatase inhibitor pervanadate reversed Capz-induced STAT3 inhibition, indicating that the effect of Capz depends on a protein tyrosine phosphatase...
July 22, 2016: Oncotarget
Shaherin Basith, Minghua Cui, Sunhye Hong, Sun Choi
Capsaicin is the most predominant and naturally occurring alkamide found in Capsicum fruits. Since its discovery in the 19th century, the therapeutic roles of capsaicin have been well characterized. The potential applications of capsaicin range from food flavorings to therapeutics. Indeed, capsaicin and few of its analogues have featured in clinical research covered by more than a thousand patents. Previous records suggest pleiotropic pharmacological activities of capsaicin such as an analgesic, anti-obesity, anti-pruritic, anti-inflammatory, anti-apoptotic, anti-cancer, anti-oxidant, and neuro-protective functions...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Tao Jin, Hongyan Wu, Yanlin Wang, Hao Peng
Immunogenic cell death (ICD) is characterized by the early surface exposure of calreticulin (CRT). As a specific signaling molecule, CRT on the surface of apoptotic tumor cells mediates the recognition and phagocytosis of tumor cells by antigen presenting cells. To date, only a small quantity of anti-cancer chemicals have been found to induce ICD, therefore it is clinically important to identify novel chemicals that may induce ICD. The purpose of the present study is to explore the function of capsaicin in inducing ICD...
August 2016: Experimental and Therapeutic Medicine
Shengnan Geng, Yaqiu Zheng, Mingjing Meng, Zhenzhen Guo, Ning Cao, Xiaofang Ma, Zhenhua Du, Jiahuan Li, Yongjian Duan, Gangjun Du
Both gingerol and capsaicin are agonists of TRPV1, which can negatively control tumor progression. This study observed the long-term effects of oral administration of 6-gingerol alone or in combination with capsaicin for 20 weeks in a urethane-induced lung carcinogenic model. We showed that lung carcinoma incidence and multiplicity were 70% and 21.2 ± 3.6, respectively, in the control versus 100% and 35.6 ± 5.2 in the capsaicin group (P < 0.01) and 50% and 10.8 ± 3.1 in the 6-gingerol group (P < 0...
August 10, 2016: Journal of Agricultural and Food Chemistry
Victor Fattori, Miriam S N Hohmann, Ana C Rossaneis, Felipe A Pinho-Ribeiro, Waldiceu A Verri
In this review, we discuss the importance of capsaicin to the current understanding of neuronal modulation of pain and explore the mechanisms of capsaicin-induced pain. We will focus on the analgesic effects of capsaicin and its clinical applicability in treating pain. Furthermore, we will draw attention to the rationale for other clinical therapeutic uses and implications of capsaicin in diseases such as obesity, diabetes, cardiovascular conditions, cancer, airway diseases, itch, gastric, and urological disorders...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Ming-Hung Lin, Yi-Hui Lee, Hsiao-Ling Cheng, Huei-Yu Chen, Fong-Han Jhuang, Pin Ju Chueh
Bladder cancer is one of the most frequent cancers among males, and its poor survival rate reflects problems with aggressiveness and chemo-resistance. Recent interest has focused on the use of chemopreventatives (nontoxic natural agents that may suppress cancer progression) to induce targeted apoptosis for cancer therapy. Capsaicin, which has anti-cancer properties, is one such agent. It is known to preferentially inhibit a tumor-associated NADH oxidase (tNOX) that is preferentially expressed in cancer/transformed cells...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Consuelo Amantini, Maria Beatrice Morelli, Massimo Nabissi, Claudio Cardinali, Matteo Santoni, Angela Gismondi, Giorgio Santoni
Bladder cancer (BC) is a common urologic tumor characterized by high risk of recurrence and mortality. Capsaicin (CPS), used as an intravesical drug for overactive bladder, was demonstrated to induce cell death in different cancer cells including BC cells.Here we found that treatment of high-grade BC cells with high dose of CPS triggers autophagy. Infact, the CPS treatment alters the redox homeostasis by inducing production of radicals, mitochondrial depolarization, alterations of ADP/ATP ratio and activation of AMPK pathway stimulating the autophagic process in BC cells...
June 29, 2016: Oncotarget
Laila Arzuman, Philip Beale, Jun Q Yu, Fazlul Huq
Currently used platinum drugs fail to provide long-term cure for ovarian cancer mainly because of acquired drug resistance. With the idea that the difference may translate into an altered spectrum of activity, monofunctional planaramineplatinum(II) complex tris(quinoline)monochloro-platinum chloride (coded as LH5) was synthesized and investigated for its activity against human ovarian A2780, cisplatin-resistant A2780 (A2780(cisR)) and ZD0473-resistnat A2780 (A2780(ZD0473R)) cancer cell lines alone and in combination with the phytochemicals capsaicin (Caps) and curcumin (Cur) as a function of concentration and sequence of administration...
June 2016: Anticancer Research
Hung Yen Chen, Yi Hui Lee, Huei Yu Chen, Chia An Yeh, Pin Ju Chueh, Yi-Mei J Lin
Capsaicin has been reported to preferentially inhibit the activity of tumor-associated NADH oxidase (tNOX), which belongs to a family of growth-related plasma membrane hydroquinone oxidases in cancer/transformed cells. The inhibitory effect of capsaicin on tNOX is associated with cell growth attenuation and apoptosis. However, no previous study has examined the transcriptional regulation of tNOX protein expression. Bioinformatic analysis has indicated that the tNOX promoter sequence harbors a binding motif for POU3F2, which is thought to play important roles in neuronal differentiation, melanocytes growth/differentiation and tumorigenesis...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
John D Hurley, Austin T Akers, Jamie R Friedman, Nicholas A Nolan, Kathleen C Brown, Piyali Dasgupta
The nutritional compound capsaicin inhibits the invasion of many types of human cancers. The clinical development of capsaicin as an anti-cancer drug is limited due to its unfavorable side effects like burning sensation, stomach cramps, gut pain and nausea. This study compared the anti-invasive activity of capsaicin to non-pungent long chain capsaicin analogs, namely arvanil and olvanil, in human small cell lung cancer cells. Boyden chamber invasion assays revealed that arvanil and olvanil displayed improved anti-invasive activity relative to capsaicin in human SCLC cells...
May 19, 2016: Cell Adhesion & Migration
László Pecze, Katalin Jósvay, Walter Blum, György Petrovics, Csaba Vizler, Zoltán Oláh, Beat Schwaller
Vanilloids including capsaicin and resiniferatoxin are potent transient receptor potential vanilloid type 1 (TRPV1) agonists. TRPV1 overstimulation selectively ablates capsaicin-sensitive sensory neurons in animal models in vivo. The cytotoxic mechanisms are based on strong Na(+) and Ca(2+) influx via TRPV1 channels, which leads to mitochondrial Ca(2+) accumulation and necrotic cell swelling. Increased TRPV1 expression levels are also observed in breast and prostate cancer and derived cell lines. Here, we examined whether potent agonist-induced overstimulation mediated by TRPV1 might represent a means for the eradication of prostate carcinoma (PC-3, Du 145, LNCaP) and breast cancer (MCF7, MDA-MB-231, BT-474) cells in vitro...
August 2016: Biochimica et Biophysica Acta
Fabian Garreis, Antje Schröder, Peter S Reinach, Stefanie Zoll, Noushafarin Khajavi, Priyavathi Dhandapani, Alexander Lucius, Uwe Pleyer, Friedrich Paulsen, Stefan Mergler
PURPOSE: The heat-sensitive transient receptor potential vanilloid type-1 (TRPV1) channel (i.e., capsaicin [CAP] receptor) is upregulated in numerous cancers. This study determined if this response occurs in fresh and cultured hyperplastic human pterygial epithelial tissues. METHODS: Reverse transcriptase PCR and quantitative real-time PCR, along with immunohistochemistry and Western blotting, characterized TRPV1 expression patterns in pterygial and healthy conjunctival tissue, primary and immortalized pterygial cells (hPtEC), and primary and immortalized conjunctival epithelial cells (HCjEC)...
May 1, 2016: Investigative Ophthalmology & Visual Science
Cheng-Hui Liu, Xian-Le Bu, Jun Wang, Tao Zhang, Yang Xiang, Lin-Lin Shen, Qing-Hua Wang, Bo Deng, Xin Wang, Chi Zhu, Xiu-Qing Yao, Meng Zhang, Hua-Dong Zhou, Yan-Jiang Wang
BACKGROUND: Capsaicin-rich diets are common worldwide. Capsaicin has been shown to have favorable effects on various diseases including atherosclerosis, cardiovascular diseases, stroke, obesity, hypertension, cancer, and gastrointestinal and inflammatory diseases. The impact of capsaicin on Alzheimer's disease (AD), which is the most common form of dementia in the elderly, remains unknown. OBJECTIVE: To investigate the correlations of capsaicin intake with cognition and blood markers of AD...
April 8, 2016: Journal of Alzheimer's Disease: JAD
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