A novel peptide isolated from the leaves of Gymnema sylvestre—I. Characterization and its suppressive effect on the neural responses to sweet taste stimuli in the rat

doi:10.1016/0300-9629(91)90475-R

Comparative Biochemistry and Physiology Part A: Physiology

Volume 100, Issue 2, 1991, Pages 309-314

Comparative Biochemi...

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Abstract

1.
1. A new substance that suppressed selectively the neural responses of the rat to sweet taste stimuli was isolated from the leaves of Gymnema sylvestre.
2.
2. The substance was proved to be a peptide consisting of 35 amino acids and having a molecular weight of about 4,000.
3.
3. The inhibitory effect on the sweet responses appeared after treating the tongue surface with the peptide at a concentration of more than 1 × 10⁻⁶ M.

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Cited by (100)

Suppression of sweet taste-related responses by plant-derived bioactive compounds and eating. Part II: A systematic review in animals
2023, Heliyon
This article, the second in a two-part series, continues the discussion on the nature of the relationship between the level of sweet taste suppression and eating behaviour, but in animal rather human subjects. In particular, the aim was to review the scientific literature on the impact that bioactive compounds that decrease oral sweet sensations have on intake, preference and physiological status in preclinical studies. This review was registered in the International Prospective Register of Systematic Reviews and conducted according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) and the Scottish Intercollegiate Guidelines Network and covered original papers included in Web of Science, PubMed, Scopus, Food Science Source and Food Science and technology abstracts. We identified 28 peer-reviewed English-language studies that fit the topic and met the inclusion criteria. We identified three plant species, Gymnema sylvestre, Hovenia dulcis, and Ziziphus jujuba, that possess acute sweetness-inhibitory properties. When administered orally, these plants reduced neural responses to sweet stimuli and decreased consumption. However, studies on the longer-term effects of antisweet activity remain to be conducted. Translating the valuable insights into the mechanisms underlying the relationship between sweet taste impairment and eating behaviour into practical clinical applications are discussed.
Sweet-inhibiting effects of gurmarin on intake during repeated acute and long-term sugar exposure: A behavioural analysis using an animal model
2023, Journal of Functional Foods
Excessive consumption of added sugars is linked to chronic diseases, such as obesity, diabetes, dyslipidaemia or cardiovascular disease; and public health is searching for new strategies to reduce it. Although plant-derived bioactive compounds with inhibitory properties of sweet taste like Gymnema sylvestre show the potential to reduce sugar intake acutely, their impact after repeated administration is unknown. Therefore, we examined the changes of single and repeated exposures of a Gymnema sylvestre constituent, gurmarin, in sweet beverage consumption and preference in a preclinical model. 24 Wistar rats (50 % females) were divided into experimental (gurmarin) and two control groups (gymnemic acids or phosphate buffer solutions) according to the substances orally applied. Then acceptance and preference tests with sugar were performed within (Experiment 1) and between sessions (Experiment 2). We found that administering gurmarin decreased sucrose intake significantly, even after multiple treatments, without rebound effects. These findings suggest that sweet taste suppressors could be an effective tool for reducing long-term sugar consumption when repeatedly administrated.
3.10 - Sweet and Umami Taste
2020, The Senses: A Comprehensive Reference: Volume 1-7, Second Edition
Sweet and umami are the attractive tastes to detect nutritious compounds required for our health. TAS1Rs are major receptors for sweet and umami, but other receptors also contribute to these tastes. Information detected by these receptors is sent to the brain via taste cells and gustatory nerve fibers. At the peripheral level, some endocrine factors controlling food intake modulate taste sensitivity in concert with their central effects. This chapter will review the mechanisms for detection, modulation and transmission of sweet and umami tastes at the periphery.
Participants with pharmacologically impaired taste function seek out more intense, higher calorie stimuli
2017, Appetite
Citation Excerpt :
When rats were given GS, their neural response to sweeteners was significantly reduced when compared to rats consuming the same foods without GS treatment (Imoto, Miyasaka, Ishima, & Akasaka, 1991). A relatively low concentration of GS is needed to reduce responsiveness to sweeteners in both rats (Imoto et al., 1991) and humans (Bone, 2002), with studies suggesting that concentrated solutions of GS can suppress more than 75% of the pre-treatment perceived sweetness of a stimulus (R. A. Frank, Mize, Kennedy, de los Santos, & Green, 1992). GS selectively suppresses sweet intensity perception for a prolonged period, making it an intriguing tool to study how a diminished taste response influences a participant's reaction to foods.
Research suggests a weaker sense of taste in people with obesity, with the assumption that a debilitated taste response increases the desire for more intensely tasting stimuli to compensate for decreased taste input. However, empirical testing of this supposition remains largely absent.
In a randomized, repeated measures design, 51 healthy subjects were treated with varying concentrations of a tea containing Gymnema sylvestre (GS), to temporarily and selectively diminish sweet taste perception, or a control tea. Following treatment in the four testing sessions, taste intensity ratings for various sweet stimuli were captured on the generalized Labeled Magnitude Scale (gLMS), liking for real foods assessed on the hedonic gLMS, and optimal level of sweetness quantified via an ad-libitum mixing task. Data were analyzed with mixed models assessing both treatment condition and each subject's resultant sweet response with various taste-related outcomes, controlling for covariates.
GS treatment diminished sweet intensity perception (p < 0.001), reduced liking for sweet foods (p < 0.001), and increased the desired sucrose content of these foods (p < 0.001). Regression modeling revealed a 1% reduction in sweet taste response was associated with a 0.40 g/L increase in optimal concentration of sucrose (p < 0.001).
Our results show that an attenuation in the perceived taste intensity of sweeteners correlates with shifted preference and altered hedonic response to select sweet foods. This suggests that those with a diminished sense of taste may desire more intense stimuli to attain a satisfactory level of reward, potentially influencing eating habits to compensate for a lower gustatory input.
Leptin suppresses sweet taste responses of enteroendocrine STC-1 cells
2016, Neuroscience
Leptin is an important hormone that regulates food intake and energy homeostasis by acting on central and peripheral targets. In the gustatory system, leptin is known to selectively suppress sweet responses by inhibiting the activation of sweet sensitive taste cells. Sweet taste receptor (T1R2 + T1R3) is also expressed in gut enteroendocrine cells and contributes to nutrient sensing, hormone release and glucose absorption. Because of the similarities in expression patterns between enteroendocrine and taste receptor cells, we hypothesized that they may also share similar mechanisms used to modify/regulate the sweet responsiveness of these cells by leptin. Here, we used mouse enteroendocrine cell line STC-1 and examined potential effect of leptin on Ca²⁺ responses of STC-1 cells to various taste compounds. Ca²⁺ responses to sweet compounds in STC-1 cells were suppressed by a rodent T1R3 inhibitor gurmarin, suggesting the involvement of T1R3-dependent receptors in detection of sweet compounds. Responses to sweet substances were suppressed by ⩾1 ng/ml leptin without affecting responses to bitter, umami and salty compounds. This effect was inhibited by a leptin antagonist (mutant L39A/D40A/F41A) and by ATP gated K⁺ (K_ATP) channel closer glibenclamide, suggesting that leptin affects sweet taste responses of enteroendocrine cells via activation of leptin receptor and K_ATP channel expressed in these cells. Moreover, leptin selectively inhibited sweet-induced but not bitter-induced glucagon-like peptide-1 (GLP-1) secretion from STC-1 cells. These results suggest that leptin modulates sweet taste responses of enteroendocrine cells to regulate nutrient sensing, hormone release and glucose absorption in the gut.
Sweet taste inhibitors: Therapeutic propects
2015, Cahiers de Nutrition et de Dietetique
Cette mise au point résume et discute des connaissances actuelles concernant le rôle physiologique du récepteur du goût sucré (T1R2/T1R3) ainsi que les potentielles perspectives thérapeutiques résultant de son inhibition. En dehors de la bouche, l’expression fonctionnelle du récepteur au goût sucré a également été décrite dans de nombreux autres tissus, où il a été proposé qu’il puisse participer à la régulation des processus métaboliques. Parmi ces organes, nous pouvons citer l’intestin, le pancréas, la vessie, le cerveau, mais aussi les tissus osseux et adipeux. Dans l’intestin, il a été montré que le récepteur T1R2/T1R3 est impliqué dans la détection de glucose luminal, la libération de cytokines ainsi que de certaines hormones de satiété, l’expression de transporteurs de glucose et enfin, le maintien de l’homéostasie du glucose. Très récemment, il a été proposé que le récepteur du goût sucré soit impliqué dans la régulation de l’adipogenèse et la régulation des fonctions biologiques des os. Dans cette mise au point, nous allons résumer les connaissances sur différents inhibiteurs du goût sucré, tels que l’acide gymnémique, l’inhibiteur protéique appelé gurmarine ou le lactisole. Leur mécanisme d’action sur le récepteur sera discuté. L’identification de nouveaux rôles du récepteur du goût sucré relance l’intérêt de moduler son activité via des inhibiteurs et ouvrent des perspectives potentielles intéressantes notamment concernant le traitement de l’obésité et certaines maladies métaboliques telles que le diabète et l’hyperlipidémie.
This review summarizes and discusses the current knowledge concerning the physiological role of the sweet taste receptor (T1R2/T1R3) and the potential therapeutic perspectives concerning its inhibition. The functional expression of the sweet taste receptor has also been described in many extra-oral tissues where it has been proposed that the receptor participated in the regulation of metabolic processes. The receptor has been highlighted in various organs such as the intestine, pancreas, bladder, brain, and more recently in the bone and adipose tissue. In the intestine, T1R2/T1R3 receptor has been shown to be involved in the detection of luminal glucose, cytokine release of certain hormones of satiety, expression of carriers of glucose and maintenance of homeostasis of glucose. More recently, it has been proposed that the sweet taste receptor is involved in the adipogenesis regulation and biological function of bones. In this review, different inhibitors will be described including gymnemic acid, the sweet-taste suppressing protein, gurmarin and lactisole. Their mechanism of inhibition will be discussed. The identification of new roles of the sweet taste receptor relaunches the interest for sweet taste inhibitors or blockers and makes it as a potential and promising target for obesity and metabolic diseases cure such as diabetes and hyperlipidemia.

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Comparative Biochemistry and Physiology Part A: Physiology

Abstract

References (18)

Reduction of sweetness judgements by extracts from the leaves of Ziziphus jujuba

Physiol. Behav.

Separation of two receptor sites in a single labellar sugar receptor of the fleshfly by treatment with p-chloromer-curibenzoate

J. Insect Physiol.

Molecular weight analysis of oligopeptides by electrophoresis in polyacrylamide gel with sodium dodecyl sulfate

Anal. Biochem.

Discrimination of molecular structure of various sugars in the sweet receptor sites of the rat tongue

Inhibitory effect of the extract from Zizyphus jujuba leaves on sweet taste responses of the chorda tympani in the rat and hamster

Comp. Biochem. Physiol.

Letter to the Linnean society

Sweet taste involves distinct receptor mechanisms

Chem. Senses Flavour

Effects of gymnemic acid on sweet taste perception in primates

Chem. Senses

On the gustatory effects of gymnemic acid and miraculin in dog, pig, and rabbit

Chem. Senses Flavour

Cited by (100)

Suppression of sweet taste-related responses by plant-derived bioactive compounds and eating. Part II: A systematic review in animals

Sweet-inhibiting effects of gurmarin on intake during repeated acute and long-term sugar exposure: A behavioural analysis using an animal model

3.10 - Sweet and Umami Taste

Participants with pharmacologically impaired taste function seek out more intense, higher calorie stimuli

Leptin suppresses sweet taste responses of enteroendocrine STC-1 cells

Sweet taste inhibitors: Therapeutic propects