Non-Pungent Capsaicin Analogs (Capsinoids) Increase Metabolic Rate and Enhance Thermogenesis<i>via</i>Gastrointestinal TRPV1 in Mice

Kawabata, Fuminori; Inoue, Naohiko; Masamoto, Yukiko; Matsumura, Shigenobu; Kimura, Wasaburo; Kadowaki, Makoto; Higashi, Toshiya; Tominaga, Makoto; Inoue, Kazuo; Fushiki, Tohru

doi:10.1271/bbb.90555

Cited by 113 publications

(98 citation statements)

References 43 publications

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“…Kawabata et al have reported that capsaicin enhanced energy expenditure by the TRPV1-expressing sensory nerve innervating the gastrointestinal tract. 9) Belza et al have reported that the ingestion of CAPcontaining tablets which dissolve in the stomach increased the energy expenditure, whereas the same tablets dissolving in the small intestine had no such effect. 25) These reports suggest that the local action of CAP in gastric mucosa is a prerequisite for exerting the thermogenetic effect.…”

Section: Discussionmentioning

confidence: 99%

“…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 potency and efficacy of these MGs for activating TRPV1 were respectively about 50 times weaker than and half that of CAP.…”

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confidence: 99%

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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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Section: Discussionmentioning

confidence: 99%

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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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“…In addition, capsiate administration contributes to enhancement of aerobic ATP production and reduction of body fat content, 71) and also up-regulates UCP1 and UCP2 expression. 72,73) Mice given the TRPV1 agonist monoacylglycerol showed increases in UCP1 expression levels in brown adipocytes and suppressed accumulation of visceral fat in mice fed HFD and sucrose.…”

Section: )mentioning

confidence: 99%

Role of Thermo-Sensitive Transient Receptor Potential Channels in Brown Adipose Tissue

Uchida

Sun

Yamazaki

et al. 2018

Biological & Pharmaceutical Bulletin

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Brown and beige adipocytes are a major site of mammalian non-shivering thermogenesis and energy dissipation. Obesity is caused by an imbalance between energy intake and expenditure and has become a worldwide health problem. Therefore modulation of thermogenesis in brown and beige adipocytes could be an important application for body weight control and obesity prevention. Over the last few decades, the involvement of thermo-sensitive transient receptor potential (TRP) channels (including TRPV1, TRPV2, TRPV3, TRPV4, TRPM4, TRPM8, TRPC5, and TRPA1) in energy metabolism and adipogenesis in adipocytes has been extensively explored. In this review, we summarize the expression, function, and pathological/ physiological contributions of these TRP channels and discuss their potential as future therapeutic targets for preventing and combating human obesity and obesity-related metabolic disorders.

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“…Generally, comparison of pharmacological actions of a pungent component with its non-pungent analogue is of significance since it can contribute to the development of new therapeutic treatments. A typical example of non-pungent substances that mimic actions of natural pungent compounds is capsiate, which is a non-pungent analogue of capsaicin (4,7,11,12,14,15). It has been reported that most of the biological actions of capsaicin, including enhancement of energy expenditure and reduction of body fat accumulation, can be reproduced by capsiate (11,12).…”

Section: Acknowledgmentsmentioning

confidence: 99%

Intraluminal administration of zingerol, a non-pungent analogue of zingerone, inhibits colonic motility in rats

et al. 2011

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Zingerone, a pungent component of ginger, may exert beneficial therapeutic effects on hypermotilityinduced diarrhea because it has the ability to inhibit contractions of colonic smooth muscles. However, the pungency is undesirable for possible therapeutic use. The purpose of this study was to examine effects of zingerol, a non-pungent analogue of zingerone, in rats. Colonic motility in vivo was evaluated by measuring intraluminal pressure changes and expelled fluid volume from the colon in anesthetized rats. Mechanical contractile activities of isolated colonic segments were also recorded. Intracolonic administration of zingerol attenuated colonic motility in vivo without affecting blood pressure and heart rate in a manner similar to that of zingerone. Zingerol also inhibited spontaneous contractile movements in isolated colonic segments, suggesting that zingerol directly acts on the colon. Zingerol had no effect on jejunal motility, although zingerone showed an inhibitory effect to the jejunum. These findings suggest that zingerol can inhibit colonic motility without adverse effects on small intestinal motility and the cardiovascular system. The non-pungent property of zingerol will be useful as an oral or suppository medicine for treating diarrhea and other gastrointestinal disorders.

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Non-Pungent Capsaicin Analogs (Capsinoids) Increase Metabolic Rate and Enhance ThermogenesisviaGastrointestinal TRPV1 in Mice

Cited by 113 publications

References 43 publications

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

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

Role of Thermo-Sensitive Transient Receptor Potential Channels in Brown Adipose Tissue

Intraluminal administration of zingerol, a non-pungent analogue of zingerone, inhibits colonic motility in rats

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