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capsaicin and

Lu Sun, Zheng-Guo Cui, Shahbaz Ahmad Zakki, Qian-Wen Feng, Meng-Ling Li, Hidekuni Inadera
Hyperthermia is one therapeutic tool for damaging and killing cancer cells, with minimal injury to normal tissues. However, its cytotoxic effects alone are insufficient for quantitative cancer cell death. To overcome this limitation, several studies have explored non-toxic enhancers for hyperthermia-induced cell death. Capsaicin may be applicable as a therapeutic tool against various types of cancer. In the present study, we employed nonivamide, a less-pungent capsaicin analogue, to investigate its possible enhancing effects on hyperthermia-induced apoptosis; moreover, we analyzed its molecular mechanism...
March 15, 2018: Free Radical Biology & Medicine
J Q Fang, J Y Du, J F Fang, T Xiao, X Q Le, N F Pan, J Yu, B Y Liu
AIMS: Observing the parameter-specific anti-hyperalgesic effects of EA with different stimulation times and frequencies on painful hyperalgesia mediated by the level of TRPV1 and P2X3 expression in DRG after CFA injection. MAIN METHODS: The model was induced by the injection of CFA in each rat's right hind paw. EA treatment was applied to the bilateral ST36 and BL60. Paw withdrawal threshold (PWT) and paw withdrawal latency (PWL) were tested with Von Frey filaments and the radiant heat source of the test instrument, respectively...
March 14, 2018: Life Sciences
Hiroyuki Hattori, Kosei Yamauchi, Siaw Onwona-Agyeman, Thoru Mitsunaga
BACKGROUND: Grains of Paradise (GP) is the seed of Aframomum melegueta, which is widely distributed throughout West Africa and has been used as a spice and a folk remedy for a long time. The anti-obesity effect by GP intake was demonstrated in our previous report. In this present study, we tried to isolate some compounds in GP and clarify the anti-obesity mechanism. RESULTS: Ten vanilloid compounds were determined. Among ten vanilloids, 1-(4'-hydroxy-3'-methoxyphenyl)-decan-3-ol and 1-(4'-hydroxy-3'-methoxyphenyl)-3-octen-5-one were determined as novel compounds and 6-gingerol, 6-paradol, and 6-shogaol were identified as the major constituents in GP extract...
March 15, 2018: Journal of the Science of Food and Agriculture
Purabi Sarkar, Ananya Bhowmick, Sofia Banu
Enhanced oxidative stress plays an important role in the progression and onset of diabetes and its complications. Strategies or efforts meant to reduce the oxidative stress are needed which may mitigate these pathogenic processes. The present study aims to investigate the in vitro ameliorative potential of nine antioxidant molecules in L6 myotubes under oxidative stress condition induced by 4-hydroxy-2-nonenal and also to comprehend the gene expression patterns of oxidative stress genes upon the supplementation of different antioxidants in induced stress condition...
March 14, 2018: Cytotechnology
Alejandra I Martinez-Gonzalez, Emilio Alvarez-Parrilla, Ángel G Díaz-Sánchez, Laura A de la Rosa, José A Núñez-Gastélum, Alma A Vazquez-Flores, Gustavo A Gonzalez-Aguilar
The inhibitory activity and binding characteristics of caffeic acid, p -coumaric acid, quercetin and capsaicin, four phenolic compounds found in hot pepper, against porcine pancreatic lipase activity were studied and compared to hot pepper extract. Quercetin was the strongest inhibitor (IC50 =(6.1±2.4) µM), followed by p -coumaric acid ((170.2±20.6) µM) and caffeic acid ((401.5±32.1) µM), while capsaicin and a hot pepper extract had very low inhibitory activity. All polyphenolic compounds showed a mixed-type inhibition...
December 2017: Food Technology and Biotechnology
Johann Hammer
OBJECTIVES: The diagnosis of functional dyspepsia (FD) is challenging due to the lack of reliable biological markers to support the diagnosis. We assessed the relevance of a previously validated simple test for chemical hypersensitivity in the setting of a gastrointestinal outpatient department. METHODS: A total of 224 outpatients who were referred for evaluation of gastrointestinal symptoms in the absence of alarm symptoms swallowed a capsule containing 0.75 mg capsaicin...
March 13, 2018: American Journal of Gastroenterology
Antonello E Rigamonti, Claudia Casnici, Ornella Marelli, Alessandra De Col, Sofia Tamini, Elisa Lucchetti, Gabriella Tringali, Roberta De Micheli, Laura Abbruzzese, Mauro Bortolotti, Silvano G Cella, Alessandro Sartorio
Although capsaicin has been reported to reduce energy intake and increase energy expenditure in an adult (normal weight or overweight) population, thus resulting in a net negative energy balance and weight loss, these beneficial effects have not been investigated in young obese subjects. We hypothesize that capsaicin acutely administered in young obese subjects exerts the same effects on energy balance and that these effects are mediated by changes in gastrointestinal peptides regulating appetite. Thus, the aim of the present study was to evaluate the acute effects of capsaicin (2 mg) or placebo on energy intake, hunger, and satiety in obese adolescents and young adults (female-male ratio: 4:6, age: 21...
February 10, 2018: Nutrition Research
Rafael Taeho Han, Han-Byul Kim, Young-Beom Kim, Kyungmin Choi, Gi Yeon Park, Pa Reum Lee, JaeHee Lee, Hye Young Kim, Chul-Kyu Park, Youngnam Kang, Seog Bae Oh, Heung Sik Na
Recent studies have provided several lines of evidence that peripheral administration of oxytocin induces analgesia in human and rodents. However, the exact underlying mechanism of analgesia still remains elusive. In the present study, we aimed to identify which receptor could mediate the analgesic effect of intraperitoneal injection of oxytocin and its cellular mechanisms in thermal pain behavior. We found that oxytocin-induced analgesia could be reversed by d(CH2 )5 [Tyr(Me)2 ,Dab5 ] AVP, a vasopressin-1a (V1a) receptor antagonist, but not by desGly-NH2 -d(CH2 )5 [DTyr2 , Thr4 ]OVT, an oxytocin receptor antagonist...
March 2018: Korean Journal of Physiology & Pharmacology
Sung Eun Wang, Seung Yeon Ko, Yong-Seok Kim, Sungsin Jo, Seung Hoon Lee, Sung Jun Jung, Hyeon Son
Transient receptor potential vanilloid 1 (TRPV1) affects mood and neuroplasticity in the brain, where its role is poorly understood. In the present study we investigated whether capsaicin (8-methyl-N-vanillyl-trans-6-nonenamide), an agonist of TRPV1, induced chromatin remodeling and thereby altered gene expression related to synaptic plasticity. We found that capsaicin treatment resulted in upregulation of histone deacetylase 2 (HDAC2) in the mouse hippocampus and HDAC2 was enriched at Psd95, synaptophysin, GLUR1, GLUR2 promoters...
March 9, 2018: Experimental & Molecular Medicine
Justyna Maliszewska, Sonia Marcinkowska, Anna Nowakowska, Hanna Kletkiewicz, Justyna Rogalska
Some natural alkaloids, e.g. capsaicin and camphor, are known to induce a desensitization state, causing insensitivity to pain or noxious temperatures in mammals by acting on TRP receptors. Our research, for the first time, demonstrated that a phenomenon of pharmacological blockade of heat sensitivity may operate in American cockroach, Periplaneta americana (L.). We studied the escape reaction time from 50°C for American cockroaches exposed to multiple doses of different drugs affecting thermo-TRP. Capsaicin, capsazepine, and camphor induced significant changes in time spent at noxious ambient temperatures...
2018: PloS One
Sewon Kim, Seung Keun Back, Heung Sik Na, Sun-Ho Kee
Atopic dermatitis (AD) is a complex disease featuring pruritic skin inflammation. Many animal models have been developed. In a rat model, subcutaneous capsaicin injection within 48 hours after birth induces AD-like skin manifestations of dermatitis and scratching behavior 3 weeks after the injection. When 2-4-week-old rats were injected with capsaicin, the lag period was shortened and the severity of skin manifestations was significantly reduced, suggesting influences of postnatal development. Lgr6 is an epidermal stem cell marker that is normally restricted to the isthmus area of hair follicles at postnatal 2 weeks...
March 6, 2018: Experimental Dermatology
E Sjögren, T Kullenberg, B Jonzon, M Segerdahl, O Stålberg, M M Halldin, A K Sundgren-Andersson
BACKGROUND: The transient receptor potential cation channel subfamily V 1 (TRPV1) is involved in nociception and has thus been of interest for drug developers, as a target for novel analgesics. However, several oral TRPV1 antagonists have failed in development, and novel approaches to target TRPV1 with innovative chemistry are needed. METHOD: This work describes an intradermal microdosing approach in humans for pharmacodynamic deductions and pharmacological profiling of compounds...
March 5, 2018: European Journal of Pain: EJP
Hanmei Li, Sonja Krstin, Shihui Wang, Michael Wink
BACKGROUND: Multidrug resistance (MDR) can develop in cancer cells after treatment with anticancer drugs, mainly due to the overexpression of the ATP-binding cassette (ABC) transporters. We analyzed the ability of two pungent-tasting alkaloids-capsaicin and piperine from Capsicum frutescens and Piper nigrum , respectively-to reverse multidrug resistance in the cancer cell lines Caco-2 and CEM/ADR 5000, which overexpress P-glycoprotein (P-gp) and other ABC transporters. METHODS: The MTT assay was first used to determine the cytotoxicity of doxorubicin, the alkaloids, and digitonin alone, and then their combinations...
March 2, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Isabelle M Larsen, Asbjørn M Drewes, Anne E Olesen
Pain involves responses in which both peripheral and central mechanisms contribute to the generation of pain. Pre-clinical laboratory data have supported that a topical formulation of combined diclofenac and methadone (Diclometh) may alleviate local pain, and potentially the side effect profile should be low. We hypothesized that anti-allodynic and anti-hyperalgesic effects of Diclometh could be demonstrated in a human experimental pain model, and that Diclometh would be safe to administer. Thus, the aims were: 1) To compare two doses of Diclometh versus placebo; 2) To assess the safety profile of Diclometh...
March 2, 2018: Basic & Clinical Pharmacology & Toxicology
Shunsuke Nakamori, Jun Takahashi, Sumiko Hyuga, Toshiko Tanaka-Kagawa, Hideto Jinno, Masashi Hyuga, Takashi Hakamatsuka, Hiroshi Odaguchi, Yukihiro Goda, Toshihiko Hanawa, Yoshinori Kobayashi
The article Ephedra Herb extract activates/desensitizes transient receptor potential vanilloid 1 and reduces capsaicin-induced pain, written by Shunsuke Nakamori, Jun Takahashi, Sumiko Hyuga, Toshiko Tanaka-Kagawa, Hideto Jinno, Masashi Hyuga, Takashi Hakamatsuka, Hiroshi Odaguchi, Yukihiro Goda, Toshihiko Hanawa and Yoshinori Kobayashi, was originally published Online First without open access. After publication in volume 71, issue 1, page 105-113 the author decided to opt for Open Choice and to make the article an open access publication...
March 1, 2018: Journal of Natural Medicines
Rafael Taeho Han, Hye Young Kim, Hyun Ryu, Wooyoung Jang, Seung Ha Cha, Hyo Young Kim, JaeHee Lee, Seung Keun Back, Hee Jin Kim, Heung Sik Na
BACKGROUND: Atopic dermatitis (AD) is a highly pruritic, chronic inflammatory skin disease associated with hyperreactivity to environmental triggers. Among those, outdoor air pollutants such as particulate matter (PM) have been reported to aggravate pre-existing AD. However, underlying mechanisms of air pollution-induced aggravation of AD have hardly been studied. OBJECTIVE: To investigate the molecular mechanisms by which glyoxal, a PM-forming organic compound, exacerbates the symptoms of AD induced by neonatal capsaicin treatment...
February 21, 2018: Journal of Dermatological Science
Jan Vollert, Walter Magerl, Ralf Baron, Andreas Binder, Elena K Enax-Krumova, Gerd Geisslinger, Janne Gierthmühlen, Florian Henrich, Philipp Hüllemann, Thomas Klein, Jörn Lötsch, Christoph Maier, Bruno Oertel, Sigrid Schuh-Hofer, Thomas R Tölle, Rolf-Detlef Treede
As an indirect approach to relate previously identified sensory phenotypes of patients suffering from peripheral neuropathic pain to underlying mechanisms, we used a published sorting algorithm to estimate the prevalence of denervation, peripheral and central sensitization in 657 healthy subjects undergoing experimental models of nerve block (compression block, topical lidocaine), primary (sunburn, topical capsaicin), or secondary hyperalgesia (intradermal capsaicin, electrical high-frequency stimulation), and in 902 patients suffering from neuropathic pain...
February 24, 2018: Pain
Daichi Utsumi, Kenjiro Matsumoto, Takuya Tsukahara, Kikuko Amagase, Makoto Tominaga, Shinichi Kato
Transient receptor potential (TRP) vanilloid 1 (TRPV1) and TRP ankyrin 1 (TRPA1), which are non-selective cation channels, play important roles in the sensation of pain. This study investigated the roles of TRPV1 and TRPA1 in dextran sulfate sodium (DSS)-induced murine colitis. DSS (2%) administered for 7 days caused severe colitis that was significantly less severe in TRPV1-deficient (TRPV1KO) and TRPA1-deficient (TRPA1KO) mice than that in wild-type (WT) mice. Similar colitis attenuations were observed in TRPV1KO and TRPA1KO mice but not in WT mice that had been transplanted with bone marrow cells from WT, TRPA1KO, or TRPV1KO mice...
February 8, 2018: Journal of Pharmacological Sciences
Doris Lam, Zeinab Momeni, Michael Theaker, Santosh Jagadeeshan, Yasuhiko Yamamoto, Juan P Ianowski, Verónica A Campanucci
Diabetes mellitus is associated with sensory abnormalities, including exacerbated responses to painful (hyperalgesia) or non-painful (allodynia) stimuli. These abnormalities are symptoms of diabetic peripheral neuropathy (DPN), which is the most common complication that affects approximately 50% of diabetic patients. Yet, the underlying mechanisms linking hyperglycemia and symptoms of DPN remain poorly understood. The transient receptor potential vanilloid 1 (TRPV1) channel plays a central role in such sensory abnormalities and shows elevated expression levels in animal models of diabetes...
2018: PloS One
Arafat Nasser, Anette Torvin Møller, Vibe Hellmund, Sidsel Salling Thorborg, Cathrine Jespersgaard, Ole J Bjerrum, Erik Dupont, Gösta Nachman, Jens Lykkesfeldt, Troels Staehelin Jensen, Lisbeth Birk Møller
Human studies have demonstrated a correlation between non-coding polymorphisms of 'the pain protective' (PP) haplotype in the GCH1 gene that encodes for GTP cyclohydrolase I (GTPCH1) - which leads to reduced tetrahydrobiopterin (BH4) production in cell systems - and a diminished perception of experimental and clinical pain. Here we investigate whether heterozygous mutations in the GCH1 gene which lead to a profound BH4 reduction in patients with dopa-responsive dystonia (DRD) have any effect on pain sensitivity...
February 20, 2018: Pain
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