TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiate

Iida, Takehiko; Moriyama, Toshiyuki; Kobata, Kenji; Morita, Akihito; Murayama, Namie; Hashizume, Shuichi; Fushiki, Tohru; Yazawa, Susumu; Watanabe, Tatsuo; Tominaga, Makoto

doi:10.1016/s0028-3908(03)00100-x

Cited by 173 publications

(155 citation statements)

References 24 publications

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“…31) Capsiate also activates TRPV1 as well as capsaicin, which has been investigated by patch clamp experiments. 32) Although capsiate administration has increased the body temperature of mice, this increase was suppressed by capsazepine, which is an antagonist of TRPV1. 10) These results suggest that capsiate would be an agonist for TRPV1 as well as capsaicin.…”

Section: Discussionmentioning

confidence: 99%

“…9) Although capsiate did not induce any of the averse responses that were induced by capsaicin when applying to the oral cavity of mice, capsiate has induced nociceptive responses with similar dose dependence to capsaicin by injecting subcutaneously into the hindpaws. 32) Thus, it has been assumed that capsiate had the potential to activate TRPV1 with similar potency to that of capsaicin, but did not activate TRPV1 in the oral cavity. 32) Capsiate has high lipophilicity and is easily broken down under normal aqueous conditions, so it has been assumed that capsiate cannot penetrate the epithe-lium and reach TRPV1 in the oral cavity.…”

Section: Discussionmentioning

confidence: 99%

“…32) Thus, it has been assumed that capsiate had the potential to activate TRPV1 with similar potency to that of capsaicin, but did not activate TRPV1 in the oral cavity. 32) Capsiate has high lipophilicity and is easily broken down under normal aqueous conditions, so it has been assumed that capsiate cannot penetrate the epithe-lium and reach TRPV1 in the oral cavity. 32) We have also found that capsaicin could be detected in circulating blood after an intragastric administration, while capsiate could not be detected in mice (our unpublished data).…”

Section: Discussionmentioning

confidence: 99%

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Effects of CH-19 Sweet, a Non-Pungent Cultivar of Red Pepper, in Decreasing the Body Weight and Suppressing Body Fat Accumulation by Sympathetic Nerve Activation in Humans

Kawabata

Inoue

Yazawa

et al. 2006

Bioscience, Biotechnology, and Biochemistry

101

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Effects of CH-19 Sweet, a Non-Pungent Cultivar of Red Pepper, in Decreasing the Body Weight and Suppressing Body Fat Accumulation by Sympathetic Nerve Activation in Humans

Kawabata

Inoue

Yazawa

et al. 2006

Bioscience, Biotechnology, and Biochemistry

101

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“…25) Iida et al have shown that capsiate activated TRPV1 expressed transiently in HEK293 cells with a similar potency to that of capsaicin in patch-clamp experiments, and induced nociceptive responses in mice when injected subcutaneously into their hind paws. 26) They speculated that the high lipophilicity and instability of capsiate might be critical determinants for pungency. However, the site of action of capsiate and the mechanisms that caused the same physiological actions as those of capsaicin are unclear.…”

Section: Discussionmentioning

confidence: 99%

Capsiate, a Nonpungent Capsaicin Analog, Increases Endurance Swimming Capacity of Mice by Stimulation of Vanilloid Receptors

Haramizu

Mizunoya

Masuda

et al. 2006

Bioscience, Biotechnology, and Biochemistry

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“…We identified capsiate from non-pungent red pepper and [10]-shogaol from ginger as TRPV1 agonists having low pungency which increased the adrenaline secretion and energy expenditure. [11][12][13] MGs as activators of TRPV1 may therefore be useful food ingredients to increase energy expenditure.…”

mentioning

confidence: 99%

TRPV1 Agonist Monoacylglycerol Increases UCP1 Content in Brown Adipose Tissue and Suppresses Accumulation of Visceral Fat in Mice Fed a High-Fat and High-Sucrose Diet

Iwasaki

Tamura

Inayoshi

et al. 2011

Bioscience, Biotechnology, and Biochemistry

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The administration of such a transient receptor potential vanilloid 1 (TRPV1) agonist as capsaicin, which is a pungent ingredient of red pepper, promotes energy metabolism and suppresses visceral fat accumulation. We have recently identified monoacylglycerols (MGs) having an unsaturated long-chain fatty acid as the novel TRPV1 agonist in foods. We investigated in this present study the effects of dietary MGs on uncoupling protein 1 (UCP1) expression in interscapular brown adipose tissue (IBAT) and on fat accumulation in mice fed with a high-fat, high-sucrose diet. The MG30 diet that substituted 30% of all lipids for MGs (a mixture of 1-oleoylglycerol, 1-linoleoylglycerol and 1-linolenoylglycerol) significantly increased the UCP1 content of IBAT and decreased the weight of epididymal white adipose tissue, and the serum glucose, total cholesterol and free fatty acid levels. The diet containing only 1-oleoylglycerol as MG also increased UCP1 expression in IBAT. MGs that activated TRPV1 also therefore induced the expression of UCP 1 and prevented visceral fat accumulation as well as capsaicin.Key words: monoacylglycerol; transient receptor potential vaniloid 1 (TRPV1); uncoupling protein 1; obesity; capsaicin Obesity is a risk factor for hyperglycemia, hyperlipidemia and hypertension. It is important for preventing obesity to decrease the energy intake and increase the energy expenditure. It has been reported that capsaicin (CAP), a pungent ingredient of red pepper, is the functional ingredient for increasing energy expenditure. CAP promotes energy metabolism (oxygen consumption) by increasing adrenaline secreted from the adrenal medulla and upregulating uncoupling protein 1 (UCP1) in interscapular brown adipose tissue (IBAT) by activating the sympathetic nerve. 1-4) Since CAP has the effect of increasing energy expenditure, the ingestion of CAP could suppress the accumulation of visceral fat in rats fed with a high-fat diet. 5) The CAP receptor was identified as vanilloid receptor subtype 1 in 1997, 6) and has recently been called transient receptor potential vanilloid 1 (TRPV1). TRPV1 is mainly expressed in the primary afferent nerve. 6) Recent studies have indicated that stimulating the sensory nerve by activating TRPV1 was essential to CAP-induced energy expenditure. CAP-induced adrenaline secretion was completely dissipated in rats in which the CAP-sensitive sensory nerve had been denervated by an excess CAP treatment, 7) suggesting that the TRPV1-expressing sensory nerve was indispensable for CAPinduced adrenaline secretion. The effects of suppressing an accumulation of visceral fat, increasing oxygen consumption and promoting thermogenesis by CAP were canceled in TRPV1 knockout mice. 8,9) We searched in our previous study for the food compound which would activate TRPV1 as the functional compound increasing energy expenditure, and identified 1-or 2-monoacylglycerols (MGs) having oleic, linoleic, and -linolenic acids from wheat flour, onion (Allium cepa) and myoga (Zingiber mioga) as TRPV1 agonists. 10) The po...

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TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiate

Cited by 173 publications

References 24 publications

Effects of CH-19 Sweet, a Non-Pungent Cultivar of Red Pepper, in Decreasing the Body Weight and Suppressing Body Fat Accumulation by Sympathetic Nerve Activation in Humans

Effects of CH-19 Sweet, a Non-Pungent Cultivar of Red Pepper, in Decreasing the Body Weight and Suppressing Body Fat Accumulation by Sympathetic Nerve Activation in Humans

Capsiate, a Nonpungent Capsaicin Analog, Increases Endurance Swimming Capacity of Mice by Stimulation of Vanilloid Receptors

TRPV1 Agonist Monoacylglycerol Increases UCP1 Content in Brown Adipose Tissue and Suppresses Accumulation of Visceral Fat in Mice Fed a High-Fat and High-Sucrose Diet

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