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Special Issue "Capsaicin"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (30 April 2016)

Special Issue Editor

Guest Editor
Prof. Dr. Pin Ju Chueh

Institute of Biomedical Sciences, National Chung Hsing University, Taichung, Taiwan, ROC
Website | E-Mail
Interests: apoptosis; autophagy; capsaicin; cell migration; metastasis; protein acetylation; biological role of NADH oxidase; redox signaling in cancer; evaluation of nanomaterial-mediated cytotoxicity and their underlying mechanisms

Special Issue Information

Dear Colleagues,

Capsaicin has been long considered as a chemopreventive agent that exhibits anti-growth activity against various lines of cancer cell lines, often associated with its apoptotic activity. However, numerous reports have demonstrated that capsaicin possesses paradoxical effects on cell growth and is differentially cytotoxic toward cancer cells and non-cancerous cells. The specific target(s) of capsaicin and the resulting mechanisms underlying this difference are not yet fully understood, and remain to be discovered.

This Special Issue is devoted to recent developments in this very important and emerging area of research. The scope is broad, including but not limited to effect of capsaicin on cellular-signaling events in the functioning, growth and differentiation of cells in normal and pathological states, effect of capsaicin on the regulation of protein expression in different states, the effect of capsaicin on gene expression, bioinformatic studies related to the mechanisms of signaling events and gene regulation, and studies of capsaicin agonists and antagonists.

Prof. Dr. Pin Ju Chueh
Guest Editor

Manuscript Submission Information

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Keywords

  • bioinformatics
  • cell growth
  • cell death
  • cellular function
  • cellular signaling
  • gene expression
  • protein expression
  • protein function
  • capsaicin agonists
  • capsaicin antagonists

Published Papers (9 papers)

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Research

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Open AccessArticle Capsaicin Suppresses Cell Proliferation, Induces Cell Cycle Arrest and ROS Production in Bladder Cancer Cells through FOXO3a-Mediated Pathways
Molecules 2016, 21(10), 1406; doi:10.3390/molecules21101406
Received: 7 September 2016 / Revised: 13 October 2016 / Accepted: 18 October 2016 / Published: 21 October 2016
Cited by 3 | PDF Full-text (6916 KB) | HTML Full-text | XML Full-text
Abstract
Capsaicin (CAP), a highly selective agonist for transient receptor potential vanilloid type 1 (TRPV1), has been widely reported to exhibit anti-oxidant, anti-inflammation and anticancer activities. Currently, several therapeutic approaches for bladder cancer (BCa) are available, but accompanied by unfavorable outcomes. Previous studies reported
[...] Read more.
Capsaicin (CAP), a highly selective agonist for transient receptor potential vanilloid type 1 (TRPV1), has been widely reported to exhibit anti-oxidant, anti-inflammation and anticancer activities. Currently, several therapeutic approaches for bladder cancer (BCa) are available, but accompanied by unfavorable outcomes. Previous studies reported a potential clinical effect of CAP to prevent BCa tumorigenesis. However, its underlying molecular mechanism still remains unknown. Our transcriptome analysis suggested a close link among calcium signaling pathway, cell cycle regulation, ROS metabolism and FOXO signaling pathway in BCa. In this study, several experiments were performed to investigate the effects of CAP on BCa cells (5637 and T24) and NOD/SCID mice. Our results showed that CAP could suppress BCa tumorigenesis by inhibiting its proliferation both in vitro and in vivo. Moreover, CAP induced cell cycle arrest at G0/G1 phase and ROS production. Importantly, our studies revealed a strong increase of FOXO3a after treatment with CAP. Furthermore, we observed no significant alteration of apoptosis by CAP, whereas Catalase and SOD2 were considerably upregulated, which could clear ROS and protect against cell death. Thus, our results suggested that CAP could inhibit viability and tumorigenesis of BCa possibly via FOXO3a-mediated pathways. Full article
(This article belongs to the Special Issue Capsaicin)
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Figure 1a

Open AccessArticle Capsaicin Inhibits Multiple Bladder Cancer Cell Phenotypes by Inhibiting Tumor-Associated NADH Oxidase (tNOX) and Sirtuin1 (SIRT1)
Molecules 2016, 21(7), 849; doi:10.3390/molecules21070849
Received: 29 April 2016 / Revised: 23 June 2016 / Accepted: 24 June 2016 / Published: 28 June 2016
Cited by 6 | PDF Full-text (6394 KB) | HTML Full-text | XML Full-text
Abstract
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
[...] Read more.
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. Here, we set out to elucidate the correlation between tNOX expression and the inhibitory effects of capsaicin in human bladder cancer cells. We showed that capsaicin downregulates tNOX expression and decreases bladder cancer cell growth by enhancing apoptosis. Moreover, capsaicin was found to reduce the expression levels of several proteins involved in cell cycle progression, in association with increases in the cell doubling time and enhanced cell cycle arrest. Capsaicin was also shown to inhibit the activation of ERK, thereby reducing the phosphorylation of paxillin and FAK, which leads to decreased cell migration. Finally, our results indicate that RNA interference-mediated tNOX depletion enhances spontaneous apoptosis, prolongs cell cycle progression, and reduces cell migration and the epithelial-mesenchymal transition. We also observed a downregulation of sirtuin 1 (SIRT1) in these tNOX-knockdown cells, a deacetylase that is important in multiple cellular functions. Taken together, our results indicate that capsaicin inhibits the growth of bladder cancer cells by inhibiting tNOX and SIRT1 and thereby reducing proliferation, attenuating migration, and prolonging cell cycle progression. Full article
(This article belongs to the Special Issue Capsaicin)
Open AccessArticle Capsaicin Synthesis Requires in Situ Phenylalanine and Valine Formation in in Vitro Maintained Placentas from Capsicum chinense
Molecules 2016, 21(6), 799; doi:10.3390/molecules21060799
Received: 26 April 2016 / Revised: 9 June 2016 / Accepted: 15 June 2016 / Published: 21 June 2016
Cited by 1 | PDF Full-text (1575 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Capsaicinoids (CAP) are nitrogenous metabolites formed from valine (Val) and phenylalanine (Phe) in the placentas of hot Capsicum genotypes. Placentas of Habanero peppers can incorporate inorganic nitrogen into amino acids and have the ability to secure the availability of the required amino acids
[...] Read more.
Capsaicinoids (CAP) are nitrogenous metabolites formed from valine (Val) and phenylalanine (Phe) in the placentas of hot Capsicum genotypes. Placentas of Habanero peppers can incorporate inorganic nitrogen into amino acids and have the ability to secure the availability of the required amino acids for CAP biosynthesis. In order to determine the participation of the placental tissue as a supplier of these amino acids, the effects of blocking the synthesis of Val and Phe by using specific enzyme inhibitors were analyzed. Isolated placentas maintained in vitro were used to rule out external sources′ participation. Blocking Phe synthesis, through the inhibition of arogenate dehydratase, significantly decreased CAP accumulation suggesting that at least part of Phe required in this process has to be produced in situ. Chlorsulfuron inhibition of acetolactate synthase, involved in Val synthesis, decreased not only Val accumulation but also that of CAP, pointing out that the requirement for this amino acid can also be fulfilled by this tissue. The presented data demonstrates that CAP accumulation in in vitro maintained placentas can be accomplished through the in situ availability of Val and Phe and suggests that the synthesis of the fatty acid chain moiety may be a limiting factor in the biosynthesis of these alkaloids. Full article
(This article belongs to the Special Issue Capsaicin)
Figures

Open AccessArticle Capsaicin Inhibited Aggressive Phenotypes through Downregulation of Tumor-Associated NADH Oxidase (tNOX) by POU Domain Transcription Factor POU3F2
Molecules 2016, 21(6), 733; doi:10.3390/molecules21060733
Received: 29 April 2016 / Revised: 26 May 2016 / Accepted: 31 May 2016 / Published: 4 June 2016
Cited by 2 | PDF Full-text (5026 KB) | HTML Full-text | XML Full-text
Abstract
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.
[...] Read more.
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. In this study, we found that capsaicin-mediated tNOX downregulation and cell migration inhibition were through POU3F2. The protein expression levels of POU3F2 and tNOX are positively correlated, and that overexpression of POU3F2 (and the corresponding upregulation of tNOX) enhanced the proliferation, migration and invasion in AGS (human gastric carcinoma) cells. In contrast, knockdown of POU3F2 downregulates tNOX, and the cancer phenotypes are affected. These findings not only shed light on the molecular mechanism of the anticancer properties of capsaicin, but also the transcription regulation of tNOX expression that may potentially explain how POU3F2 is associated with tumorigenesis. Full article
(This article belongs to the Special Issue Capsaicin)

Review

Jump to: Research

Open AccessReview Capsaicin: From Plants to a Cancer-Suppressing Agent
Molecules 2016, 21(8), 931; doi:10.3390/molecules21080931
Received: 1 May 2016 / Revised: 1 July 2016 / Accepted: 4 July 2016 / Published: 27 July 2016
Cited by 4 | PDF Full-text (777 KB) | HTML Full-text | XML Full-text
Abstract
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,
[...] Read more.
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. This review is an approach in contextualizing the use of controlled stress on the plant to increase the content of capsaicin, highlighting its synthesis and its potential use as anticancer agent. Full article
(This article belongs to the Special Issue Capsaicin)
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Open AccessReview Harnessing the Therapeutic Potential of Capsaicin and Its Analogues in Pain and Other Diseases
Molecules 2016, 21(8), 966; doi:10.3390/molecules21080966
Received: 25 April 2016 / Revised: 27 June 2016 / Accepted: 15 July 2016 / Published: 23 July 2016
Cited by 7 | PDF Full-text (1308 KB) | HTML Full-text | XML Full-text
Abstract
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
[...] Read more.
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. Moreover, emerging data indicate its clinical significance in treating vascular-related diseases, metabolic syndrome, and gastro-protective effects. The dearth of potent drugs for management of such disorders necessitates the urge for further research into the pharmacological aspects of capsaicin. This review summarizes the historical background, source, structure and analogues of capsaicin, and capsaicin-triggered TRPV1 signaling and desensitization processes. In particular, we will focus on the therapeutic roles of capsaicin and its analogues in both normal and pathophysiological conditions. Full article
(This article belongs to the Special Issue Capsaicin)
Figures

Open AccessReview Capsaicin: Current Understanding of Its Mechanisms and Therapy of Pain and Other Pre-Clinical and Clinical Uses
Molecules 2016, 21(7), 844; doi:10.3390/molecules21070844
Received: 27 April 2016 / Accepted: 27 April 2016 / Published: 28 June 2016
Cited by 14 | PDF Full-text (1666 KB) | HTML Full-text | XML Full-text
Abstract
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
[...] Read more.
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. Full article
(This article belongs to the Special Issue Capsaicin)
Open AccessReview The Effect of Capsaicin on Salivary Gland Dysfunction
Molecules 2016, 21(7), 835; doi:10.3390/molecules21070835
Received: 25 May 2016 / Revised: 20 June 2016 / Accepted: 22 June 2016 / Published: 25 June 2016
Cited by 1 | PDF Full-text (492 KB) | HTML Full-text | XML Full-text
Abstract
Capsaicin (trans-8-methyl-N-vanilyl-6-nonenamide) is a unique alkaloid isolated from hot chili peppers of the capsicum family. Capsaicin is an agonist of transient receptor potential vanilloid subtype 1 (TRPV1), which is expressed in nociceptive sensory neurons and a range of secretory epithelia, including
[...] Read more.
Capsaicin (trans-8-methyl-N-vanilyl-6-nonenamide) is a unique alkaloid isolated from hot chili peppers of the capsicum family. Capsaicin is an agonist of transient receptor potential vanilloid subtype 1 (TRPV1), which is expressed in nociceptive sensory neurons and a range of secretory epithelia, including salivary glands. Capsaicin has analgesic and anti-inflammatory properties in sensory neurons. Recently, increasing evidence has indicated that capsaicin also affects saliva secretion and inflammation in salivary glands. Applying capsaicin increases salivary secretion in human and animal models. Capsaicin appears to increase salivation mainly by modulating the paracellular pathway in salivary glands. Capsaicin activates TRPV1, which modulates the permeability of tight junctions (TJ) by regulating the expression and function of putative intercellular adhesion molecules in an ERK (extracelluar signal-regulated kinase) -dependent manner. Capsaicin also improved dysfunction in transplanted salivary glands. Aside from the secretory effects of capsaicin, it has anti-inflammatory effects in salivary glands. The anti-inflammatory effect of capsaicin is, however, not mediated by TRPV1, but by inhibition of the NF-κB pathway. In conclusion, capsaicin might be a potential drug for alleviating dry mouth symptoms and inflammation of salivary glands. Full article
(This article belongs to the Special Issue Capsaicin)
Open AccessReview Capsaicin, Nociception and Pain
Molecules 2016, 21(6), 797; doi:10.3390/molecules21060797
Received: 29 April 2016 / Revised: 6 June 2016 / Accepted: 14 June 2016 / Published: 18 June 2016
Cited by 8 | PDF Full-text (3258 KB) | HTML Full-text | XML Full-text
Abstract
Capsaicin, the pungent ingredient of the hot chili pepper, is known to act on the transient receptor potential cation channel vanilloid subfamily member 1 (TRPV1). TRPV1 is involved in somatic and visceral peripheral inflammation, in the modulation of nociceptive inputs to spinal cord
[...] Read more.
Capsaicin, the pungent ingredient of the hot chili pepper, is known to act on the transient receptor potential cation channel vanilloid subfamily member 1 (TRPV1). TRPV1 is involved in somatic and visceral peripheral inflammation, in the modulation of nociceptive inputs to spinal cord and brain stem centers, as well as the integration of diverse painful stimuli. In this review, we first describe the chemical and pharmacological properties of capsaicin and its derivatives in relation to their analgesic properties. We then consider the biochemical and functional characteristics of TRPV1, focusing on its distribution and biological effects within the somatosensory and viscerosensory nociceptive systems. Finally, we discuss the use of capsaicin as an agonist of TRPV1 to model acute inflammation in slices and other ex vivo preparations. Full article
(This article belongs to the Special Issue Capsaicin)
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