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Sweeteners: State of knowledge review
Abstract
Sweeteners are widely used in the food and pharmaceutical industry. The purpose of this paper is to review our current knowledge of sweet taste from chemical, biochemical, electrophysiological, psychophysical, and psychological points of view. The most common sweetners likely to be used in food and pharmaceuticals will be examined in detail. First, the chemical structures of sweet compounds including saccharides, diterpene glycosides, polyols, amino acids, dipeptides, and other nonsugars will be discussed. Second, biochemical approaches to understanding sweetner receptors will be reviewed. Third, electrophysiological and behavioral approaches to understanding sweetner receptors will be discussed. Fourth, psychophysical studies in humans will be shown to be consistent with biochemical and neurophysiological data. In addition, the basic mechanisms of sweet taste revealed by psychophysical studies will be given, including the role of multiple receptor sites, hydrogen bonding, and sodium transport. Finally, the factors that affect preference for sweet taste including the psychological and physiological variables associated with sweet preference will be explored.
Supplementary resource (1)
... = not described psychophysical evaluations to which all other sweet-tasting substances are compared. Sucrose taste is described as pure and clean (Schiffman and Gatlin 1993). Other common disaccharides used in food include lactose (derived from galactose and glucose), maltose (formed by two units of glucose) and trehalose (formed from two glucose units joined by a 1-1 alpha bond). ...
... Among monosaccharides, glucose (Figure 7.1) elicits a sweet taste and is approximately 75% as sweet as sucrose. Fructose (Figure 7.1) occurs naturally in fruits, some root vegetables and honey and is the sweetest of the natural sugars (Schiffman and Gatlin 1993). Carbohydrates are not only used as sweet agents; they are also sometimes added to food products because of their texturing capacities. ...
... Its temporal profile in the mouth is slow compared to that of sucrose. Its well-known liquorice aftertaste, its poor organoleptic and pharmacological properties limit the use of glycyrrhizic acid as a sweetener (Schiffman and Gatlin 1993). With respect to regulatory status, glycyrrhizic acid has been accepted as a flavouring agent only in the US, and its use as a sweetener is not approved in Europe. ...
Characterization of taste compounds: chemical structures and sensory properties
... = not described psychophysical evaluations to which all other sweet-tasting substances are compared. Sucrose taste is described as pure and clean (Schiffman and Gatlin 1993). Other common disaccharides used in food include lactose (derived from galactose and glucose), maltose (formed by two units of glucose) and trehalose (formed from two glucose units joined by a 1-1 alpha bond). ...
... Among monosaccharides, glucose (Figure 7.1) elicits a sweet taste and is approximately 75% as sweet as sucrose. Fructose (Figure 7.1) occurs naturally in fruits, some root vegetables and honey and is the sweetest of the natural sugars (Schiffman and Gatlin 1993). Carbohydrates are not only used as sweet agents; they are also sometimes added to food products because of their texturing capacities. ...
... Its temporal profile in the mouth is slow compared to that of sucrose. Its well-known liquorice aftertaste, its poor organoleptic and pharmacological properties limit the use of glycyrrhizic acid as a sweetener (Schiffman and Gatlin 1993). With respect to regulatory status, glycyrrhizic acid has been accepted as a flavouring agent only in the US, and its use as a sweetener is not approved in Europe. ...
The sense of taste, along with the sense of smell, is one the most important senses involved in the perception of food by humans. Taste is stimulated when fundamental nutrients or harmful compounds, such as toxic molecules, activate specialised receptors located in taste buds. Humans are able to perceive and discriminate five main different taste qualities, sweet, salty, sour, bitter, and umami (the taste of some amino acids such as glutamate). This chapter reviews the characteristics of the main tasting molecules known to be the most important to contribute to these five basic tastes. New tastants and taste enhancers, which have been generated using classical approaches or novel technologies based on taste receptor screening, are also described.
... Based on the observed results, it seems that what really affects sweetness perception is only the sweetener type. Indeed, it is well known that different types of sweeteners display varying times of onset, duration, decay and extinction (Schiffman & Gatlin, 1993). For example, carbohydrate sugars have an early onset of maximum sweetness intensity and a short extinction time (Schiffman & Gatlin, 1993). ...
... Indeed, it is well known that different types of sweeteners display varying times of onset, duration, decay and extinction (Schiffman & Gatlin, 1993). For example, carbohydrate sugars have an early onset of maximum sweetness intensity and a short extinction time (Schiffman & Gatlin, 1993). While large protein sweeteners, such as thaumatin and monellin tend to have a significant delay in the time to maximum sweetness intensity and take much longer to extinguish (Kinghorn & Compadre, 2001;Naim et al., 2002;Schiffman & Gatlin, 1993). ...
... For example, carbohydrate sugars have an early onset of maximum sweetness intensity and a short extinction time (Schiffman & Gatlin, 1993). While large protein sweeteners, such as thaumatin and monellin tend to have a significant delay in the time to maximum sweetness intensity and take much longer to extinguish (Kinghorn & Compadre, 2001;Naim et al., 2002;Schiffman & Gatlin, 1993). However, in this study MNEI and Y65R had a lower overall sweetness compared to the other sweeteners. ...
Natural sweet proteins may be used as sugar replacer in simple liquid food systems but their applicability in more complex matrices has not been investigated yet. Gelling agent nature and texture characteristics as well as type and distribution of a stimulus in a gel could affect taste perception through inhibition or enhancement of tastants migration to the receptors. The mechanical, nonoral texture and time-intensity sweetness characteristics of sweet proteins MNEI and super sweet Y65R mutant, aspartame and saccharin added at a concentration iso-sweet to 40 g/L of sucrose in three agar gel concentrations (1%, 1.5%, and 2%) were evaluated. The results have shown that agar concentration and agar sweetener interaction particularly affect mechanical fracture stress and non oral hardness of the sweetened gels. Time intensity results illustrated that unlike in solution, the intensity of sweet taste in a gelled system over time decreases. Indeed, the behavior of the sweet proteins differed greatly in the gelled system compared to when they are in solution.
Practical applications:
MNEI has been proved to be a high-potency sweetener for beverages, but the possibility to use it in semisolid foodstuff was not investigated yet. This study represented a preliminary characterization of two variants of natural sweetener monellin, MNEI and Y65R in semisolid model foodstuff. The data were an important scientific contribution to the knowledge of sweet proteins in agar-based gels and could be useful in order to extend the possible application of these sweet proteins as low calorie sweeteners in semisolid foodstuffs. Some problems concerning their delivered sweetness in agar gels were underlined and their application should be optimized in order to improve sweetness conveyed.
... Second, they represent various chemical groups: sugars (sucrose and maltose), sugar alcohols (sorbitol and erythritol), a chlorinated sugar analog (sucralose), amino acids (D-phenylalanine, D-tryptophan, L-proline and glycine), a dipeptide (aspartame), a protein (thaumatin), N-sulfonyl amides (saccharin and acesulfame-K), a sulfamate (cyclamate), a guanidinacetic acid-based sweetener (SC-45647), a triterpenoid glycoside (glycyrrhizic acid) and a dihydrochalcone glycoside (neohesperidin dihydrochalcone). Third, previous psychophysical and neurophysiological studies have revealed differences in responses to these sweeteners (Plata-Salaman et al., 1993;Schiffman and Gatlin, 1993;DuBois, 1995;Naim et al., 1998). Fourth, comparative studies have shown that several of these compounds are sweet to some mammalian species but not to others (Beauchamp et al., 1977;Jakinovich, 1981;Naim et al., 1982;Ferrell, 1984;Schiffman and Gatlin, 1993;Hellekant et al., 1994;Glaser et al., 1995;Nofre et al., 1996;Danilova et al., 1998). ...
... Third, previous psychophysical and neurophysiological studies have revealed differences in responses to these sweeteners (Plata-Salaman et al., 1993;Schiffman and Gatlin, 1993;DuBois, 1995;Naim et al., 1998). Fourth, comparative studies have shown that several of these compounds are sweet to some mammalian species but not to others (Beauchamp et al., 1977;Jakinovich, 1981;Naim et al., 1982;Ferrell, 1984;Schiffman and Gatlin, 1993;Hellekant et al., 1994;Glaser et al., 1995;Nofre et al., 1996;Danilova et al., 1998). ...
... We tested sucrose, maltose, sorbitol, saccharin, D-phenylalanine, D-tryptophan, L-proline, glycine, cyclamate (cyclamic acid, hemicalcium salt), aspartame (Asp-Phe methyl ester), neohesperidin dihydrochalcone (Sigma Chemical Co., St Louis, MO), glycyrrhizic acid monoammonium salt (Aldrich Chemical Co., Milwaukee, WI), acesulfame-K (Hoechst Food Ingredients, Edison, NJ), erythritol (M&C Sweeteners/Mitsubishi Chemical and Cargill, Blair, NE), sucralose (McNeil Specialty, New Brunswick, NJ), SC-45647 (a Nutrasweet compound) (Tinti and Nofre, 1991;DuBois, 1995) and thaumatin (a gift of G. DuBois). Detailed information about most of these sweeteners can be found elsewhere (Schiffman and Gatlin, 1993). The order of testing of the sweeteners within each group of mice is described above. ...
Previous studies have shown large differences in taste responses to several sweeteners between mice of the C57BL/6ByJ (B6) and 129P3/J (129) inbred strains. The goal of this study was to compare behavioral responses of B6 and 129 mice to a wider variety of sweeteners. Seventeen sweeteners were tested using two-bottle preference tests with water. Three main patterns of strain differences were evident. First, sucrose, maltose, saccharin, acesulfame-K, sucralose and SC-45647 were preferred by both strains, but the B6 mice had lower preference thresholds and higher solution intakes. Second, the amino acids D-phenylalanine, D-tryptophan, L-proline and glycine were highly preferred by B6 mice, but not by 129 mice. Third, glycyrrhizic acid, neohesperidin dihydrochalcone, thaumatin and cyclamate did not evoke strong preferences in either strain. Aspartame was neutral to all 129 and some B6 mice, but other B6 mice strongly preferred it. Thus, compared with the 129 mice the B6 mice had higher preferences for sugars, sweet tasting amino acids and several but not all non-caloric sweeteners. Glycyrrhizic acid, neohesperidin, thaumatin and cyclamate are not palatable to B6 or 129 mice.
... The sweetness potency of intense sweeteners cannot then be established in absolute terms but it must be determined as a function of the desired sweetness intensity. Basic information on the quality and relative intensity of the sweetness of most intense sweeteners in aqueous solutions is readily available (Schiffman & Gatlin, 1993) and it can help to understand the taste interactions in complex matrices or food systems (Keast & Breslin, 2002), but in each particular case a final evaluation of the sweetener performance in the actual product is necessary (Fry, 1993). ...
... Aspartame (L-aspartyl-L-phenylalanine methyl ester) which is generally considered as 100-200 times sweeter than sucrose and with a sugar-like taste is, among intense sweeteners, one of the most commonly used in food formulations. There are many studies about the potency or sweetness of aspartame relative to sucrose in aqueous solutions (Fry, 1993;Hossenlop, Tournier, Tharrault, & Palagos, 1990;Ketelsen, Keay, & Wiet, 1993;Kim & Dubois, 1991;Schiffman & Gatlin, 1993). Less information is available about the aspartame potency in other food matrices, as in fruit beverages (Baldwin & Korschgen, 1979;Larson-Powers & Pangborn, 1978;Pastor, Costell, & Duran, 1996) or in gelatin or hydrocolloid gels (Baldwin & Korschgen, 1979;Damasio, Costell, & Dura´n, 1997) or about the influence of different factors (pH, temperature, or addition of cations) on the sweetness of aspartame relative to sucrose (Schiffman et al., 2000). ...
... Considering the equisweet aspartame concentration relative to 10% sucrose as the concentration at which the P value is 50%, an aspartame concentration of 0.084% w/v was obtained (Fig. 1a). The sweetening power of aspartame relative to sucrose, calculated as the ratio between the sucrose concentration and the equisweet concentration of aspartame, was 119, i.e., slightly higher than those reported by Schiffman and Gatlin (1993) and by Kim and Dubois (1991) (107 and 110, respectively) (Table 4). ...
Equivalent sweetness of aspartame relative to two sucrose concentrations (10% and 20% w/w) were determined in water and in hydrocolloids gels. The influence of the texture of three hydrocolloids gelled systems—gellan gum, κ-carrageenan, and κ-carrageenan/locust bean gum (LBG)—at two gums concentrations (0.3% and 1.2% w/w) on the equivalent sweetness of aspartame were then studied. For the three gelled systems, the increase in hydrocolloid concentration produced a significant increase in the true rupture stress and in the deformability modulus values. For both κ-carrageenan and mixed gels the true rupture strain values increased when increasing hydrocolloid concentration while for gellan gels, decreased. For the same hydrocolloid concentrations the κ-carrageenan/LBG gels showed the largest strain at rupture and gellan gels the smallest (most brittle). For both soft (0.3% gum) and hard (1.2% gum) gellan gels and κ-carrageenan gels, the concentrations of aspartame needed to deliver a sweetness intensity equivalent to that of gels with 10% sucrose (0.079–0.087% w/w) were similar to those obtained for aqueous solutions (0.084% w/v). For hard κ-carrageenan/LBG gels the corresponding concentration of aspartame was slightly lower. For all gelled systems the concentrations of aspartame needed to deliver a sweetness intensity equivalent to that of gels with 20% sucrose were higher for soft gels than for hard gels.
... We found that hTAS1R2-VFT interacts with the natural sugars sucrose, fructose and glucose, with Kd values in the millimole range, as previously observed with mouse TAS1R2-VFT [16]. Conversely, we observed that lactose is a poor ligand for hTAS1R2-VFT, in agreement with its low sweetness potency deduced from sensory experiments [30,31]. Our study revealed that hTAS1R2-VFT bind various ...
... We found that hTAS1R2-VFT interacts with the natural sugars sucrose, fructose and glucose, with K d values in the millimole range, as previously observed with mouse TAS1R2-VFT [16]. Conversely, we observed that lactose is a poor ligand for hTAS1R2-VFT, in agreement with its low sweetness potency deduced from sensory experiments [30,31]. Our study revealed that hTAS1R2-VFT bind various noncaloric sweeteners with different affinities, in agreement with their sweetness potencies ( Table 1). ...
The human sweet taste receptor is a heterodimeric receptor composed of two distinct G-protein-coupled receptors (GPCRs), TAS1R2 and TAS1R3. The TAS1R2 and TAS1R3 subunits are members of a small family of class C GPCRs whose members share the same architecture, comprising a Venus Flytrap (VFT) module linked to the seven transmembrane domains (TMDs) by a short cysteine-rich region (CRR). The VFT module of TAS1R2 contains the primary binding site for most of the sweet-tasting compounds, including natural sugars and artificial and natural sweeteners. However, cellular assays, molecular docking and site-directed mutagenesis studies have revealed that the VFT, CRR and TMD of TAS1R3 interact with some sweeteners, including the sweet-tasting protein brazzein. The aim of this study was to better understand the contribution of TAS1R2-VFT in the binding of sweet stimuli. To achieve this, we heterologously expressed human TAS1R2-VFT (hTAS1R2-VFT) in Escherichia coli. Circular dichroism spectroscopic studies revealed that hTAS1R2-VFT was properly folded with evidence of secondary structures. Using size-exclusion chromatography coupled with light scattering, we found that hTAS1R2-VFT behaves as a monomer. Ligand binding quantified by intrinsic tryptophan fluorescence showed that hTAS1R2-VFT is capable of binding sweet stimuli with Kd values, in agreement with physiological detection. Furthermore, we investigated whether the impact of point mutations, already shown to have deleterious effects on cellular assays, could impact the ability of hTAS1R2-VFT to bind sweet ligands. As expected, the ligand affinities of hTAS1R2-VFT were drastically reduced through the introduction of single amino acid substitutions (D278A and E382A) known to abolish the response of the full-length TAS1R2/TAS1R3 receptor. This study demonstrates the feasibility of producing milligram quantities of hTAS1R2-VFT to further characterize the mechanism of binding interaction and perform structural studies.
... On trouve en effet des hydrates de carbone (1,2,3), des polyols (4, 5), des peptides (6, 7), des protéines (thaumatine), des flavonoïdes (10,11), des diterpènoïdes (12), des triterpènoïdes dérivés de l'oléanane (13), des proanthocyanidines (selligueaine A), mais aussi des halogénoalcanes comme le chloroforme. (Schiffman & Gatlin, 1993;Kim & Kinghorn, 2002;Kinghorn & Soejarto, 2002). Ces composés peuvent être hiérarchisés en fonction de leur pouvoir sucrant. ...
... Cette grandeur adimensionnelle est obtenue par un quotient dont le dénominateur est une concentration massique de saccharose, et le numérateur la concentration de composé sucrant conduisant à une saveur sucrée de même intensité. Cette valeur varie considérablement d'un composé à un autre, comme entre le mannitol (0.6) et la thaumatine (plus de 14 000) par exemple (Schiffman & Gatlin, 1993). ...
La saveur sucrée est à l’origine de l’équilibre gustatif des vins secs. On observe uneaugmentation de son intensité au cours de la macération post-fermentaire et de l’élevage enbarrique. Nous montrons que ces phénomènes sont respectivement liés à la libération depeptides de la levure et de composés non-volatils du bois de chêne dans les vins.Le rôle de la protéine Hsp12 de S. cerevisae sur le gain de sucrosité est établi enutilisant des techniques de biologie moléculaire et d’analyse sensorielle.Le développement d’un couplage chromatographie de partage centrifuge –gustatométrie permet de fractionner un extrait de bois de chêne et de purifier plusieurscomposés sapides. L’utilisation de la LC-FT/MS et de la RMN nous a permis d’identifierquatre nouvelles molécules, appelées quercotriterpénosides (QTT), deux d’entre elles (QTTI et III) possédant une saveur douce. Les seuils de perception du QTT I et d’un lignane amer,le lyonirésinol, sont respectivement 590 μg/L et 1.52 mg/L.La mise au point d’une méthode de quantification de ces composés en LC-FT/MS nous apermis de démontrer l’impact organoleptique du lyonirésinol dans les vins.Il est probable que les QTT I et III contribuent, directement ou indirectement, au gain desucrosité conféré par le bois de chêne.
... Given that glycemic carbohydrates are an important source of energy in the human diet, their gustatory detection would be highly beneficial. Historically, research has focused almost exclusively on the perception and mechanisms underlying the gustatory detection of sugars based on the T1R2/T1R3 sweet receptor (for reviews on sugars and sweet taste, see [5,6]). In contrast, the gustatory detection of maltooligo-and maltopolysaccharides was thought to be unlikely [7]. ...
... All monosaccharides exist as L-or D-isomers, defined by the position (left vs. right) of the hydroxyl group (-OH) farthest from the carbonyl group (C=O) when depicted in straight-chain form (see Fig. 1A); D-isomers are most common in nature, and will thus be the focus of this review. Many of the more abundant monosaccharides in nature, such as glucose, fructose, and galactose, contain 6 carbons [(CH 2 O) 6 ] and tend to exist as 5-or 6-membered cyclic structures in aqueous solution (Fig. 1B) [18]. The intermolecular reaction that forms the cyclic molecule from a straight-chain molecule occurs between the carbon of the carbonyl group, termed the anomeric carbon, and the oxygen of a hydroxyl group within the chain. ...
Carbohydrates encompass a wide range of molecules, which can be classified into three groups: mono−/disaccharides (sugars), oligosaccharides, and polysaccharides. Despite all three classes of saccharides being naturally present in foods, research on the human gustatory responses to carbohydrates has focused almost exclusively on sugars, which elicit sweet taste. This review is intended to share recent knowledge regarding possible additional gustatory pathways, other than the known T1R2/T1R3 sweet receptor, involved in carbohydrate sensing. The review begins by providing a brief overview of the chemistry and classification of carbohydrates, along with examples of carbohydrates in the diet, particularly those that can be digested by the human body (i.e., glycemic carbohydrates). Discussions on the oral digestion of glycemic carbohydrates and the enzymes relevant to the digestive process follow. Finally, we discuss sensory perception and possible transduction mechanisms underlying starch hydrolysis products.
... It can be used as sweetener at low concentration but it elicits a strong bitter taste at high concentration (Cohen 1986). Cyclamate has a sweet tatse similar to sucrose with a weak metallic and salty aftertaste (Schiffman and Gatlin 1993). Acesulfame K is an intense sweetener often used in association to mask the unpleasant aftertaste of other sweeteners (Schiffman and Gatlin 1993). ...
... Cyclamate has a sweet tatse similar to sucrose with a weak metallic and salty aftertaste (Schiffman and Gatlin 1993). Acesulfame K is an intense sweetener often used in association to mask the unpleasant aftertaste of other sweeteners (Schiffman and Gatlin 1993). Aspartame is a synthetic peptide (Asp-Phe-O-Methyle) known to synergise with other sweeteners and thus mainly used in mixture with acesulfame K and saccharin. ...
This chapter gives an overview of the physicochemical and sensory properties of aroma and taste compounds from food, their interactions with the food matrix, and their release during food breakdown in the mouth. In order to be perceived by the taste or olfactory receptors, aroma and taste compounds have first to be released in the saliva, which depends on the food matrix composition and structure, and on the masticatory behavior. Aroma compounds have then to be transported from the oral to the nasal cavity. Different mechanistic models have been developed to understand better aroma and taste compounds release in function of both food and individual, however, they are still not able to predict sensory perception, which also depends on other physiological mechanisms at the central and peripheral levels.
... The chemical structures of molecules that confer a sweet taste are diverse, and include both sugars and nonsugars (Schiffman and Gatlin, 1993). Representative compounds that have sweet tastes include saccharides, diterpene glycosides, polyols, amino acids, dipeptides and other nonsugars. ...
... At the present time, the chemical properties of molecules that induce sweet tastes are not well understood. However, recent psychophysical, electrophysiological and biochemical studies suggest that sweet taste perception for these structurally diverse compounds may involve multiple receptor types and transduction mechanisms (Schiffman et al., 1983(Schiffman et al., , 1993(Schiffman et al., , 1994a(Schiffman et al., , 1994b(Schiffman et al., , 1995DeSimone et al., 1984;Avenet et al., 1988;Tonosaki and Funakoshi, 1988;Striem et al., 1989Striem et al., , 1991Naim et al., 1991Naim et al., , 1994Breslin et al., 1996;DuBois, 1997). ...
The purpose of this study was to determine the degree to which the sodium salt of ±2-(4-methoxyphenoxy)propanoic acid (Na-PMP) reduced sweet intensity ratings of 15 sweeteners in mixtures. Na-PMP has been approved for use in confectionary/ frostings, soft candy and snack products in the USA at concentrations up to 150 p.p.m. A trained panel evaluated the effect of Na-PMP on the intensity of the following 15 sweeteners: three sugars (fructose, glucose, sucrose), three terpenoid glycosides (monoammonium glycyrrhizinate, rebaudioside-A, stevioside), two dipeptide derivatives (alitame, aspartame), two N-sulf-onylamides (acesulfame-K, sodium saccharin), two polyhydric alcohols (mannitol, sorbitol), 1 dihydrochalcone (neohesperidin dihydrochalcone), one protein (thaumatin) and one sulfamate (sodium cyclamate). Sweeteners were tested at concentrations isosweet with 2.5, 5, 7.5 and 10% sucrose in mixtures with two levels of Na-PMP: 250 and 500 p.p.m. In addition, the 15 sweeteners were tested either immediately or 30 s after a pre-rinse with 500 p.p.m. Na-PMP. In mixtures, Na-PMP at both the 250 and 500 p.p.m. levels significantly blocked sweetness intensity for 12 of the 15 sweeteners. However, when Na-PMP was mixed with three of the 15 sweeteners (monoammonium glycyrrhizinate, neohesperidin dihydrochalcone and thaumatin), there was little reduction in sweetness intensity. Pre-rinsing with Na-PMP both inhibited and enhanced sweetness with the greatest enhancements found for monoammonium glycyrrhizinate, neohesperidin dihydrochalcone and thaumatin, which were not suppressed by Na-PMP in mixtures. The mixture data suggest that Na-PMP is a selective competitive inhibitor of sweet taste. The finding that pre-treatment can produce enhancement may be due to sensitization of sweetener receptors by Na-PMP.
... Interestingly, caffeine is supposed to enhance the sweetness of some sweeteners including saccharin, but it has no effect on other sweeteners like aspartame (Schiffman and Gatlin 1993). For saccharin a bitter, metallic and astringent aftertaste is detectable by about 25 % of the population (Schiffman and Gatlin 1993). ...
... Interestingly, caffeine is supposed to enhance the sweetness of some sweeteners including saccharin, but it has no effect on other sweeteners like aspartame (Schiffman and Gatlin 1993). For saccharin a bitter, metallic and astringent aftertaste is detectable by about 25 % of the population (Schiffman and Gatlin 1993). The higher the concentration, the stronger this aftertaste. ...
A typical breakthrough pain episode is severe, categorized by a fast onset, typically reaches peak intensity instantly, and lasts for an average duration of about 30 min. The research work includes the use of opioid for the treatment of breakthrough pain with special emphasis on the development of rapidly dissolving sublingual film formulation of buprenorphine hydrochloride (BPH). BPH is an opioid analgesic with low oral bioavailability due to less absorption and first-pass metabolism. The clear and transparent sublingual films were prepared using a film-forming polymer (pullulan) with a plasticizer (PEG 400). The formulation was optimized statistically using 3(2) randomized full factorial design. The optimized film formulation showed desired mechanical properties (tensile strength of 25 N/m(2)) and a minimum disintegration time of 16 s. Differential scanning calorimetry and X-ray diffraction studies confirmed the uniform distribution of the drug in polymeric matrices. Morphological study showed the absence of drug crystals on polymeric surface. The relative bioavailability of the film formulation was increased by 10 % with respect to tablet formulation due to rapid T max (0.08 h for film while 0.15 h for tablet), which was confirmed by in vivo studies performed on rabbits. The present technology could be a promising alternative to conventional drug delivery systems and traditional routes of administration for breakthrough pain management.
... These sugars are used to balance the flavor of food and provide the energy required for survival (Brooks, 1972;Goldfein and Slavin, 2015;Misra et al., 2016). Sweetness is an important determinant of food quality, and sweeteners are often added to processed food to balance its sweetness (Schiffman and Gatlin, 1993). Sucrose is a classic sweetener that neutralizes other tastes, such as bitterness and salinity, and adds depth and complexity to flavors, in addition to sweetness (Eggleston, 2019;White, 2014). ...
Alternative sugars are often used as sugar substitutes because of their low calories and glycemic index. Recently, consumption of these sweeteners in diet foods and beverages has increased dramatically, raising concerns about their health effects. This review examines the types and characteristics of artificial sweeteners and rare sugars and analyzes their impact on the gut microbiome. In the section on artificial sweeteners, we have described the chemical structures of different sweeteners, their digestion and absorption processes, and their effects on the gut microbiota. We have also discussed the biochemical properties and production methods of rare sugars and their positive and negative effects on gut microbial communities. Finally, we have described how artificial sweeteners and rare sugars alter the gut microbiome and how these changes affect the gut environment. Our observations aim to improve our understanding regarding the potential health implications of the consumption of artificial sweeteners and low-calorie sugars.
... Sucralose is ubiquitous in the world food supply as an ingredient in over 4000 products, including tabletop sweeteners and sugar substitutes (e.g., Splenda), baked goods, beverages such as soft drinks, coffee, and tea, breakfast cereals, chewing gum, desserts, and pharmaceutical products (International Food Information Council Foundation, 2004). Because sucralose is approximately 600 times sweeter than sucrose by weight (Schiffman & Gatlin, 1993;Schiffman et al., 2008), sucralose formulations such as Splenda utilize fillers including maltodextrin and glucose for volume. In acidic environments and at elevated temperatures, sucralose hydrolyzes over time to its constituent monosaccharides 1,6-dichloro-1,6-dideoxyfructose (1,6-DCF) and 4-chloro-4-deoxy-galactose (4-CG) (Grice & Goldsmith, 2000). ...
Splenda is comprised of the high-potency artificial sweetener sucralose (1.1%) and the fillers maltodextrin and glucose. Splenda was administered by oral gavage at 100, 300, 500, or 1000 mg/kg to male Sprague-Dawley rats for 12-wk, during which fecal samples were collected weekly for bacterial analysis and measurement of fecal pH. After 12-wk, half of the animals from each treatment group were sacrificed to determine the intestinal expression of the membrane efflux transporter P-glycoprotein (P-gp) and the cyto-chrome P-450 (CYP) metabolism system by Western blot. The remaining animals were allowed to recover for an additional 12-wk, and further assessments of fecal microflora, fecal pH, and expression of P-gp and CYP were determined. At the end of the 12-wk treatment period, the numbers of total anaerobes, bifido-bacteria, lactobacilli, Bacteroides, clostridia, and total aerobic bacteria were significantly decreased; however, there was no significant treatment effect on enterobacteria. Splenda also increased fecal pH and enhanced the expression of P-gp by 2.43-fold, CYP3A4 by 2.51-fold, and CYP2D1 by 3.49-fold. Following the 12-wk recovery period, only the total anaerobes and bifido-bacteria remained significantly depressed, whereas pH values, P-gp, and CYP3A4 and CYP2D1 remained elevated. These changes occurred at Splenda dosages that contained sucralose at 1.1-11 mg/kg (the US FDA Acceptable Daily Intake for sucralose is 5 mg/kg). Evidence indicates that a 12-wk administration of Splenda exerted numerous adverse effects, including (1) reduction in beneficial fecal microflora, (2) increased fecal pH, and (3) enhanced expression levels of P-gp, CYP3A4, and CYP2D1, which are known to limit the bioavailability of orally administered drugs. The artificial high-potency sweetening compound sucralose is a chlorinated disaccharide with the chemical formula 1,6-dichloro-1,6-dideoxy-β-D-fructofuranosyl-4-chloro-4-deoxy-α-D-galactopyranoside (Federal Register, 1998). Sucralose is ubiquitous in the world food supply as an ingredient in over 4000 products, including tabletop sweeteners and sugar substitutes (e.g., Splenda), baked goods, beverages such as soft drinks, coffee, and tea, breakfast cereals, chewing gum, desserts , and pharmaceutical products (International Food Information Council Foundation, 2004). Because sucralose is approximately 600 times sweeter than sucrose by weight (Schiffman & Gatlin, 1993; Schiffman et al., 2008), sucralose formulations such as Splenda utilize fillers including malto-dextrin and glucose for volume. In acidic environments and at elevated temperatures, sucralose hydrolyzes over time to its constituent monosaccharides 1,6-dichloro-1,6-dideoxyfructose (1,6-DCF) and 4-chloro-4-deoxy-galactose (4-CG) (Grice & Goldsmith, 2000). Pharmacokinetics and metabolism studies of sucralose have shown that the majority of ingested sucralose (approximately 65-95% depending on the species) is not absorbed from the gas-trointestinal tract (GIT) but rather was excreted in the feces (Sims et al., 2000; Roberts et al., 2000; Federal Register, 1998). The low absorption of sucralose from the GIT is surprising, because this sweetener is an organochlorine molecule with appreciable lipid solubility (Miller, 1991; Wallis, 1993; Yatka et al., 1992). The low bioavailability of sucralose suggests that it is likely extruded back into the intestinal lumen during first-pass metabolism in the GIT. The concentrations of many orally consumed compounds including drugs and nutrients are reduced during first-pass metabolism in the small intestine by the membrane efflux transporter P-glycoprotein (P-gp) and the cyto-chrome P-450 (CYP) metabolism system. P-gp extrudes these compounds from the intestinal walls back to the lumen and/or CYP enzymes metabolize the compounds. P-gp and CYP are both involved in xenobiotic detoxification in the intestine and liver of many diverse chemicals, including organochlorine compounds (Lanning et al.
... Effects were dose-dependent and could not be detected on the parental cell lines at concentrations up to 1-2 mM. EC 50 values confirmed that, overall, agonists activated the sweet taste receptor with the expected rank order of potency based on human taste data (Schiffman and Gatlin, 1993;Li and Servant, 2008;Palmer et al., 2021). At concentrations ≥3 mM, we could detect receptor independent positive DMR responses. ...
The sweet taste receptor is rather unique, recognizing a diverse repertoire of natural or synthetic ligands, with a surprisingly large structural diversity, and with potencies stretching over more than six orders of magnitude. Yet, it is not clear if different cell-based assays can faithfully report the relative potencies and efficacies of these molecules. Indeed, up to now, sweet taste receptor agonists have been almost exclusively characterized using cell-based assays developed with overexpressed and promiscuous G proteins. This non-physiological coupling has allowed the quantification of receptor activity via phospholipase C activation and calcium mobilization measurements in heterologous cells on a FLIPR system, for example. Here, we developed a novel assay for the human sweet taste receptor where endogenous G proteins and signaling pathways are recruited by the activated receptor. The effects of several sweet taste receptor agonists and other types of modulators were recorded by measuring changes in dynamic mass redistribution (DMR) using an Epic® reader. Potency and efficacy values obtained in the DMR assay were compared to those results obtained with the classical FLIPR assay. Results demonstrate that for some ligands, the two assay systems provide similar information. However, a clear bias for the FLIPR assay was observed for one third of the agonists evaluated, suggesting that the use of non-physiological coupling may influence the potency and efficacy of sweet taste receptor ligands. Replacing the promiscuous G protein with a chimeric G protein containing the C-terminal tail 25 residues of the physiologically relevant G protein subunit Gαgustducin reduced or abrogated bias.
... Previously, researchers carried out a series of studies focusing on the basic chemical structures of sweeteners. They could be roughly divided into perilla and aniline derivatives, sweet and bitter aldoxime derivatives, aspartate dipeptide, sulfamate esters, sulfamate derivatives, etc (Iwamura, 1980;Kier, 1980;Schiffman & Gatlin, 1993). For computational approaches, there were some specific models designed for distinguishing sweet and bitter taste, sweet and non-sweet taste, as well as QSAR (quantitative structure-activity relationship) models aiming to distinguish sweet, tasteless and bitter compounds. ...
Nowadays, computational approaches have drawn more and more attention when exploring the relationship between sweetness and chemical structure instead of traditional experimental tests. In this work, we proposed a novel multi-layer sweetness evaluation system based on machine learning methods. It can be used to evaluate sweet properties of compounds with different chemical spaces and categories, including natural, artificial, carbohydrate, non-carbohydrate, nutritive and non-nutritive ones, suitable for different application scenarios. Furthermore, it provides quantitative predictions of sweetness. In addition, sweetness-related chemical basis and structure transforming rules were obtained by using molecular cloud and matched molecular pair analysis (MMPA) methods. This work systematically improved the data quality, explored the best machine learning algorithm and molecular characterizing strategy, and finally obtained robust models to establish a multi-layer prediction system (available at: https://github.com/ifyoungnet/ChemSweet). We hope that this study could facilitate food scientists with efficient screening and precise development of high-quality sweeteners.
... With the development of chromatography and spectroscopy methods, human routine sensory assessment of compounds was gradually discontinued. Nevertheless, the unintentional discovery of many sweet taste compounds continued in the years to follow (Schiffmann & Gatlin, 1993;Davies, 2010). ...
Abstract The search for new sweeteners technologies has increased substantially in the past decades as the number of diseases related to the excessive consumption of sugar became a public health concern. Low carbohydrates diets help to reduce ingested calories and to maintain a healthy weight. Most natural and synthetic high potency non-caloric sweeteners, known to date, show limitations in taste quality and are generally used in combination due to their complementary flavor characteristics and physicochemical properties in order to minimize undesirable features. The challenge of the food manufacturers is to develop low or calorie-free products without compromising the real taste of sugar expected by consumers. With the discovery of the genes coding for the sweet taste receptor in humans, entirely new flavor ingredients were identified, which are tasteless on their own, but potentially enhance the taste of sugar. These small molecules known as positive allosteric modulators (PAMs) could be more effective than other reported taste enhancers at reducing calories in consumer products. PAMs could represent a breakthrough in the field of flavor development after the increase in the knowledge of safety profile in combination with sucrose in humans.
... ASs are extensively tested for potential adverse health effects on humans because they are used as food additives [37,44,45]. Although the measured concentrations of some ASs range up to microgram per liter levels in surface water, groundwater and drinking water, there is a huge safety margin regarding potential adverse health effects [36]. ...
... Dubois et al. (1991) Alitame 0.3 2,955 (5) Dubois et al. (1991) Ampame 11.9/17.8 50 (2) Mazur et al. (1970) ASME 6.9 140 (2) Brussel et al. (1975) Aspartame 5 196 (5) Dubois et al. (1991) Brazzein 0.16 2,000 (2) Ming and Hellekant (1994) CAM 0.18 1,500 (2) Nofre and Tinti (1987) CAMPA 0.028 15,000 (2) Nofre et al. (1996) CCGA 0.21 7,000 (2) Nofre et al. (1989) CGA 0.77 2,700 (2) Nofre et al. (1989) Cyanosuosan 2.5 650 (2) Tinti et al. (1982) Cyclamate 9.9 31 (5) Dubois et al. (1991) DMGA 0.027 120,000 (2) Nofre et al. (1990) D-Phenylalanine 0.1 M 7 (2.2) Solms et al. (1965) D-Tryptophan 19.5 35 (0.376) Shallenberger (1993) Dulcin 1.59 250 (2) Paul (1922) Fructose 0.3 M 1.28 (5) Dubois et al. (1991) MAGAP 0.055 20,000 (2) Nofre and Tinti (1994) Monellin 0.03 3,000 Morris and Cagan (1972) NC-00174 0.23 200,000 (2) Nagarajan et al. (1996) NC-00351 0.022 30,000 (3) Nagarajan et al. (1996) NHDHC 0.49 905 (5) Dubois et al. (1991) Saccharin 1.6 440 (5) Dubois et al. (1991) SC-45647 0.12 28,000 (2) Nofre et al. (1990) Stevioside 0.62 120 (5) Dubois et al. (1991) Suosan 1.1 950 (2) Petersen and Müller (1948) Super-aspartame 0.23 3,900 (5) Nofre and Tinti (1987) TGC 0.17 3,000 (2) Tinti et al. (1981) Sucralose 0.5 635 (5) Dubois et al. (1991) Xylitol 0.82 M 0.97 (5) Schiffman and Gatlin (1993) Different concentrations of Ampame were used for stimulation the chorda tympani (CT) and glossopharyngeal (NG) nerve. Values in parentheses are sucrose concentrations used for comparison. ...
Whole nerve, as well as single fiber, responses in the chorda tympani proper (CT) and glossopharyngeal (NG) nerves of common marmosets were recorded during taste stimulation with three salts, four acids, six bitter compounds and more than 30 sweeteners. We recorded responses of 49 CT and 41 NG taste fibers. The hierarchical cluster analysis distinguished three major clusters in both CT and NG: S, Q, and H. The S CT fibers, 38% of all CT fibers, responded only to sweeteners. The S CT fibers did not respond during stimulation with salts, acids, and bitter compounds but exhibited off responses after citric and ascorbic acids, quinine hydrochloride (QHCl), and salts (in 80% of S CT fibers). S NG fibers, 50% of all NG fibers, also responded to sweeteners but not to stimuli of other taste qualities (except for citric acid, which stimulated 70% of the S NG fibers). Some sweeteners, including natural (the sweet proteins brazzein, monellin) and artificial [cyclamate, neohesperidin dihydrochalcone (NHDHC), N-3,5-dichlorophenyl- N′-(S)-α-methylbenzylguanidineacetate (DMGA), N-4-cyanophenylcarbamoyl-(R,S)-3-amino-3-(3,4-methylenedioxyphenyl) propionic acid (CAMPA)] did not elicit responses in the S fibers. In general, the response profiles of the S CT and S NG clusters were very similar, the correlation coefficient between the responses to sweeteners in these clusters was 0.94. Both the Q CT and the Q NG fibers (40 and 46% of all fibers) were predominantly responsive to bitter compounds, although their responses to the same set of bitter compounds were quite different. Sweeteners with sweet/bitter taste for humans also stimulated the Q clusters. The H clusters (22 and 3% of all fibers) were predominantly responsive to acids and did not respond to stimuli of other taste qualities. However, bitter stimuli, mainly QHCl, inhibited activity in 70% of H CT fibers. Among a total of 90 fibers from both nerves there was only 1 NaCl-best fiber in CT. We found, however, that 35% of the CT fibers reacted to salts with inhibition of activity during stimulation, followed by anoff response. This off response was diminished or eliminated by amiloride. These characteristics indicate that amiloride-sensitive sodium channels are involved in salt transduction in marmosets. In the two NG fibers responding to NaCl, we recorded neither suppression by amiloride nor off responses. Comparison of marmoset data with those of other nonhuman primates studied, rhesus and chimpanzee, demonstrates phylogenetic trends in the organization of taste system. This can help to uncover pathways of primate evolution.
... Unfortunately, all of the existing non-caloric sweeteners fail to mimic the taste of real sugar. These alternative sweeteners can exhibit objectionable off-tastes (bitter, metallic, liquorish, cooling), inadequate temporal properties (slow onset and/or lingering of sweet taste), or even a limited sweetness intensity at higher concentrations[3,4]. The recent discovery of the human sweet receptor, hTAS1R2/ hTAS1R3[5], and its application in the high-throughput screening of natural extract and synthetic libraries, has led to the discovery of positive allosteric modulators (PAMs) of the human sweet receptor as an alternative approach to reducing the caloric content of food and beverage products currently sweetened with sucrose or high fructose corn syrup[6][7][8]. ...
A toxicological evaluation of N-(1-((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218; CAS 1622458-34-7), a flavour with modifying properties, was completed for the purpose of assessing its safety for use in food and beverage applications. S2218 exhibited minimal oxidative metabolism in vitro, and in rat pharmacokinetic studies, the compound was poorly orally bioavailable and rapidly eliminated. S2218 was not found to be mutagenic in an in vitro bacterial reverse mutation assay, and was found to be neither clastogenic nor aneugenic in an in vitro mammalian cell micronucleus assay. In subchronic oral toxicity studies in male and female rats, the NOAEL was 140 mg/kg bw/day (highest dose tested) for S2218 sulfate salt (S8069) when administered as a food ad-mix for 13 consecutive weeks. Furthermore, S2218 sulfate salt demonstrated a lack of maternal toxicity, as well as adverse effects on fetal morphology at the highest dose tested, providing a NOAEL of 1000 mg/kg bw/day for both maternal toxicity and embryo/fetal development when administered orally during gestation to pregnant rats.
... On the contrary, sucralose elicited very low spike frequencies and reflex responses, proving to be a weaker stimulus for the sugar-sensitive GRN and a less palatable sugar. Interestingly, glucose that was tested at an equimolar concentration of maltose and sucralose, elicited intermediate spike frequencies and levels of PER, suggesting that disaccharides possess lower sweetness than glucose in D. suzukii opposite to humans [58]. The relationship we found about taste sensitivity and palatability to different sugars is strengthened by the results on the amount of sugar eaten under double-choice conditions; in fact, maltose was the most consumed, while sucralose the least eaten, with glucose being intermediate. ...
The peripheral sensitivity and palatability of different carbohydrates was evaluated and their nutritional value assessed in adult females of D. suzukii by means of an electrophysiological, behavioural and metabolic approach. The electrophysiological responses were recorded from the labellar “l” type sensilla stimulated with metabolizable mono- and disaccharides (glucose and maltose) and a non-metabolizable sugar (sucralose); the response rating and the palatability to the same sugars, evaluated by recording the proboscis extension reflex (PER), was maltose>glucose>sucralose. The nutritional value of carbohydrates was assessed by means of survival trials and fatty acids profile. Flies fed on a diet containing maltose had a longer lifespan than flies on monosaccharides, while flies fed on a diet containing sucralose had a shorter one. In addition, the ability to store fat seems to be influenced by the different sugars in the diet and is in relationship with their palatability. In fact, data showed a higher synthesis of palmitic and palmitoleic acids, most likely derived from de-novo lipogenesis with glucose as precursor, in flies fed with maltose and glucose than with non-metabolizable sucralose. In conclusion, these results suggest that the ability to select different sugars on the basis of their palatability may favour the storage of energy reserves such as fat by de-novo lipogenesis, determining a longer survival capability during prolonged periods of fasting.
... Since they are used as food additives [37,44,45], ASs are extensively tested for potential adverse health effects on humans. Although the measured concentrations of some ASs range up to microgram per liter levels in surface water, groundwater, and drinking water, there is a huge safety margin regarding potential adverse health effects [36]. ...
This chapter presents the degradation and mineralization of emerging trace contaminants artificial sweeteners (ASs) in aqueous solution by electro-Fenton process in which hydroxyl radicals were formed concomitantly by •OH formed from electrocatalytically generated Fenton’s reagent in the bulk solution and M(•OH) from water oxidation at the anode surface. Experiments were performed in an undivided cylindrical glass cell with a carbon-felt cathode and a Pt or boron-doped diamond (BDD) anode. The effect of catalyst (Fe²⁺) concentration and applied current on the degradation and mineralization kinetics of ASs was evaluated. The absolute rate constants for the reaction between ASs and •OH were determined. The formation and evolution of short-chain carboxylic acids as well as released inorganic ions, and toxicity assessment during the electro-Fenton process have been reported and compared.
... Xylitol is a polyol that, in addition to serving as a sweetening agent, provides a refreshing sensation due to its negative heat of dissolution (Schiffman & Gatlin, 1993). In 1988, Green and Frankmann (1988) related that effect of cooling decrease the perceived intensity of sweetness. ...
... Sucralose was chosen as the sweet taste stimulus because this molecule is perceived as approximately 600 times sweeter than sugar (Friedman, 1998;Binns, 2003) so that lower amounts of stimulus are required for examining sweet taste. At matched intensities, both sucrose and sucralose exhibit similar taste perception profiles (Binns, 2003), and sucralose does not result in an unpleasant aftertaste in most individuals (Wells, 1989;Schiffman & Gatlin, 1993). Finally, the Venus flytrap domain at the N-terminus of both heteromeric subunits of the mammalian sweet taste receptor binds both sucrose and sucralose, which would suggest a similar transduction mechanism for both sweet taste stimuli (Zhang et al., 2010). ...
A novel delivery method is described for the rapid determination of taste preferences for sweet taste in humans. This forced-choice paired comparison approach incorporates the non-caloric sweetener sucralose into a set of one-inch square edible strips for the rapid determination of sweet taste preferences. When compared to aqueous sucrose solutions, significantly lower amounts of sucralose were required to identify the preference for sweet taste. The validity of this approach was determined by comparing sweet taste preferences obtained with five different sucralose-containing edible strips to a set of five intensity-matched sucrose solutions. When compared to the solution test, edible strips required approximately the same number of steps to identify the preferred amount of sweet taste stimulus. Both approaches yielded similar distribution patterns for the preferred amount of sweet taste stimulus. In addition, taste intensity values for the preferred amount of sucralose in strips were similar to that of sucrose in solution. The hedonic values for the preferred amount of sucralose were lower than for sucrose, but the taste quality of the preferred sucralose strip was described as sweet. When taste intensity values between sucralose strips and sucralose solutions containing identical amounts of taste stimulus were compared, sucralose strips produced a greater taste intensity and more positive hedonic response. A preference test that uses edible strips for stimulus delivery should be useful for identifying preferences for sweet taste in young children, and in clinical populations. This test should also be useful for identifying sweet taste preferences outside of the lab or clinic. Finally, edible strips should be useful for developing preference tests for other primary taste stimuli and for taste mixtures.
... It is reasonable to ask whether the profile of taste sensation reported by a rat is sufficiently close to that of humans for their utility as subjects for discovery of commercially valuable sweeteners and taste modifiers. Rats are opportunistic omnivores and human pests, with an appetite for human food [49].Table I shows that many compounds that are used as sweeteners by humans also are detected by rats as sweet, with potencies and efficacies similar to those reported by humans [50,51]. A few notable exceptions that have previously appeared in the literature were confirmed here (e.g., aspartame, cyclamate). ...
Taste quality and palatability are two of the most important properties measured in the evaluation of taste stimuli. Human panels can report both aspects, but are of limited experimental flexibility and throughput capacity. Relatively efficient animal models for taste evaluation have been developed, but each of them is designed to measure either taste quality or palatability as independent experimental endpoints. We present here a new apparatus and method for high throughput quantification of both taste quality and palatability using rats in an operant taste discrimination paradigm. Cohorts of four rats were trained in a modified operant chamber to sample taste stimuli by licking solutions from a 96-well plate that moved in a randomized pattern beneath the chamber floor. As a rat's tongue entered the well it disrupted a laser beam projecting across the top of the 96-well plate, consequently producing two retractable levers that operated a pellet dispenser. The taste of sucrose was associated with food reinforcement by presses on a sucrose-designated lever, whereas the taste of water and other basic tastes were associated with the alternative lever. Each disruption of the laser was counted as a lick. Using this procedure, rats were trained to discriminate 100 mM sucrose from water, quinine, citric acid, and NaCl with 90-100% accuracy. Palatability was determined by the number of licks per trial and, due to intermediate rates of licking for water, was quantifiable along the entire spectrum of appetitiveness to aversiveness. All 96 samples were evaluated within 90 minute test sessions with no evidence of desensitization or fatigue. The technology is capable of generating multiple concentration-response functions within a single session, is suitable for in vivo primary screening of tastant libraries, and potentially can be used to evaluate stimuli for any taste system.
... g per kg of fresh weight (see MaÈ kinen & SoÈ derling, 1980), note that this compound possesses a weak physiological interest as a result of a slow and incomplete intestinal absorption (approximately one-third of the ingested portion of xylitol is absorbed, the rest being actively metabolized by intestinal¯ora) and of a dual metabolic pathway in the liver through relatively secondary routes (see, e.g. BaÈ r, 1986;Levine, 1986;Schiman & Gatlin, 1993;Sicard, 1982). The minor interest of xylitol in mammals might explain why the free access to the sweetness receptor of this molecule Ð which, through its sweetness, should normally interfere with the food selection Ð is partly hindered in the most`advanced' receptors, such as in the catarrhine ones. ...
The gustatory preferences in pigs towards 33 compounds known to be sweet in humans were evaluated through a specific two-choice preference method. All the 14 carbohydrates tested are preferred over water, sucrose being the most effective. Sucrose and fructose response intensities are identical in pigs and humans but lactose, maltose, d-glucose and d-galactose are two times less efficient in pigs. The molar order of effectiveness is sucrose > d-fructose > maltose=lactose > d-glucose > d-galactose, roughly similar to humans. As in humans, d-glucose, l-glucose and methyl α-d-glucopyranoside display equal potency, while methyl β-d-glucopyranoside is ineffective. The 7 polyols tested are attractive; xylitol is the preferred one, being as effective as sucrose. Out of 12 intense sweeteners tested, 7 are ineffective (aspartame, cyclamate, monellin, NHDC, P-4000, perillartine, thaumatin), and 5 are attractive (acesulfame-K, saccharin, alitame, dulcin, sucralose), but with a much weaker efficiency (acesulfame, 18×less; saccharin, 65×less) than with humans.
... Rats are opportunistic omnivores and human pests, with an appetite for human food [49]. Table I shows that many compounds that are used as sweeteners by humans also are detected by rats as sweet, with potencies and efficacies similar to those reported by humans [50,51]. A few notable exceptions that have previously appeared in the literature were confirmed here (e.g., aspartame, cyclamate). ...
Taste quality and palatability are two of the most important properties measured in the evaluation of taste stimuli. Human panels can report both aspects, but are of limited experimental flexibility and throughput capacity. Relatively efficient animal models for taste evaluation have been developed, but each of them is designed to measure either taste quality or palatability as independent experimental endpoints. We present here a new apparatus and method for high throughput quantification of both taste quality and palatability using rats in an operant taste discrimination paradigm. Cohorts of four rats were trained in a modified operant chamber to sample taste stimuli by licking solutions from a 96-well plate that moved in a randomized pattern beneath the chamber floor. As a rat's tongue entered the well it disrupted a laser beam projecting across the top of the 96-well plate, consequently producing two retractable levers that operated a pellet dispenser. The taste of sucrose was associated with food reinforcement by presses on a sucrose-designated lever, whereas the taste of water and other basic tastes were associated with the alternative lever. Each disruption of the laser was counted as a lick. Using this procedure, rats were trained to discriminate 100 mM sucrose from water, quinine, citric acid, and NaCl with 90-100% accuracy. Palatability was determined by the number of licks per trial and, due to intermediate rates of licking for water, was quantifiable along the entire spectrum of appetitiveness to aversiveness. All 96 samples were evaluated within 90 minute test sessions with no evidence of desensitization or fatigue. The technology is capable of generating multiple concentration–response functions within a single session, is suitable for in vivo primary screening of tastant libraries, and potentially can be used to evaluate stimuli for any taste system.
... Two sweeteners, AK and sucrose (Beijing Yuan Ye Food Chemistry Co., Ltd), were used. The range of the solution concentrations was chosen according to the previous reports (Schiffman and Gatlin 1993;Bachmanov et al. 2001). We prepared the following two series of solutions in half-log steps (10 concentration gradients): one series of AK solutions containing 0. 01, 0.04, 0.13, 0.42, 1.33, 4.21, 13.28, 41.97, 132.63, and 419.12 mM and the other series of sucrose solutions containing 0. 03, 0.10, 0.32, 1.20, 3.80, 12.00, 38.00, 125.00, 400.00, and 1400.00 mM. ...
Exposure to artificial sweetener acesulfame-K (AK) at early development stages may influence the adult sweet preference and
the periphery gustatory system. We observed that the intraoral AK stimulation to mice from postnatal day 4 (P4) to weaning
decreased the preference thresholds for AK and sucrose solutions in adulthood, with the preference pattern unchanged. The
preference scores were increased in the exposure group significantly when compared with the control group at a range of concentrations
for AK or sucrose solution. Meanwhile, more α-Gustducin-labeled fungiform taste buds and cells in a single taste bud were
induced from week 7 by the early intraoral AK stimulation. However, the growth in the number of α-Gustducin-positive taste
bud or positive cell number per taste bud occurred only in the anterior region, the rostral 1-mm part, but not in the intermediate
region, the caudal 4-mm part, of the anterior two-third of the tongue containing fungiform papillae. This work extends our
previous observations and provides new information about the developmental and regional expression pattern of α-Gustducin
in mouse fungiform taste bud under early AK-stimulated conditions.
... The two artificial sulfonamide sweeteners saccharin and acesulfame K both elicit complex taste impressions. At low concentrations, they are perceived as intensely sweet, while at higher concentrations, increasing bitter and metallic offtastes become apparent (Schiffman and Gatlin 1993). The bitter component is intrinsic to both compounds and is caused by the ability of the sulfonylamides to activate two bitter taste receptors, human T2R31 and T2R43 (Kuhn et al. 2004;Pronin et al. 2004;Roudnitzky et al. 2011). ...
Sweet-tasting compounds are recognized by a heterodimeric receptor composed of the taste receptor, type 1, members 2 (T1R2) and 3 (T1R3) located in the mouth. This receptor is also expressed in the gut where it is involved in intestinal absorption, metabolic regulation, and glucose homeostasis. These metabolic functions make the sweet taste receptor a potential novel therapeutic target for the treatment of obesity and related metabolic dysfunctions such as diabetes. Existing sweet taste inhibitors or blockers that are still in development would constitute promising therapeutic agents. In this review, we will summarize the current knowledge of sweet taste inhibitors, including a sweet-taste-suppressing protein named gurmarin, which is only active on rodent sweet taste receptors but not on that of humans. In addition, their potential applications as therapeutic tools are discussed.
Sweeteners are used in the food industry to provide sweetness similar to sugar and to decrease the caloric intake and risks associated with obesity. However, some sweeteners are characterised by bitter, metallic and other off-tastes. Sensory and cellular studies have demonstrated synergies between sweetener blends, which are responsible for enhancing sweetness. This study aimed to identify new sweetener blends that are able to enhance sweetness intensity without causing bitter off-taste using in vitro functional expression of taste receptors. The dose-response of the sweet taste receptor (TAS1R2/TAS1R3) was determined for sucrose and 9 sweeteners and was consistent with their sweetness potency. Stimulation of TAS1R2/TAS1R3 by 6 binary sweetener blends confirmed 3 known synergies determined by sensory analysis, including sucralose/acesulfame-K, rebaudioside A/erythritol and rebaudioside A/thaumatin, and revealed 2 new synergies, known as, neotame/D-allulose and mogroside V/thaumatin. No synergy was observed for the rebaudioside M/mogroside V blend, probably due to their common binding sites on the sweet taste receptor. The ability of the 9 selected sweeteners to activate the 25 human bitter taste receptors (TAS2Rs) was tested. The cellular based assay demonstrated that sucralose, acesulfame-K, rebaudioside A, mogroside V and D-allulose activated at least 2 TAS2Rs. Sucralose, acesulfame-K and rebaudioside A exhibited lower EC50 values for TAS1R2/TAS1R3 than for TAS2Rs, which may explain their absence of bitter off-taste at low concentrations, unlike mogroside V and D-allulose. Our data provide a receptor-based understanding of the complex synergies among sweetener blends and an effective approach for testing new sweeteners while avoiding the activation of TAS2Rs.
Flavor molecules belong to different chemical classes, and possess various sensory properties. They are present in the foods, but in order to reach the sensory receptors they have to be released in the saliva during the eating process and for aroma compounds in the air phase from the oral to the nasal cavity. This chapter will present an overview of the different aroma and taste compounds, their dynamic release from the food matrix into the saliva and the oronasal cavity, taking into account the in-mouth physiological process, and the influence on flavor perception. In-mouth flavor compound release and flavor perception are very complex phenomena which are not well understood yet. The properties of the food matrix and oral physiological characteristics and their interactions are the main drivers for interindividual variability. The development of mechanistic models allowed a better understanding of the release of aroma and taste compounds during the eating process. However, the release behavior does not always explain sensory perception, due to other physiological mechanisms at the central and peripheral levels.
The detection of energy-rich sweet food items has been important for our survival during evolution, however, in light of the changing lifestyles in industrialized and developing countries our natural sweet preference is causing considerable problems. Hence, it is even more important to understand how our sense of sweetness works, and perhaps even, how we may deceive it for our own benefit. This chapter summarizes current knowledge about sweet tastants and sweet taste modulators on the compound side as well as insights into the structure and function of the sweet taste receptor and the transduction of sweet signals. Moreover, methods to assess the activity of sweet substances in vivo and in vitro are compared and discussed.
The sweet receptor T1R2/T1R3 is a member of G protein-coupled receptor family and recognizes diverse natural and synthetic sweeteners. Previously, we reported a novel class of positive allosteric modulators (PAMs) of T1R2/T1R3 comprising an unnatural tripeptide structure. We classified the structure of these PAMs into three parts: "head", "linker" and "tail". Here, we report the design, synthesis and evaluation of various tail structures to obtain highly active unnatural peptide structure of PAM. In conclusion, we discovered the novel unnatural tetrapeptide with highly potent PAM activity on T1R2/T1R3 in a cell-based assay system.
European licorice roots (Glycyrrhiza glabra), used in the food and beverage industry due to their distinctive sweet and typical licorice flavor, were fractionated, with the triterpenoid saponins isolated and their chemical structures determined by means of ESIMS, ESIMS/MS, HRESIMS, and 1D/2D NMR experiments. Next to the quantitatively predominant saponin glycyrrhizin (11) and some previously known saponins, the structures of 10 monodesmosidic saponins were assigned unequivocally for the first time, namely, 30-hydroxyglycyrrhizin (1), glycyrrhizin-20-methanoate (2), 24-hydroxyglucoglycyrrhizin (3), rhaoglycyrrhizin (4), 11-deoxorhaoglycyrrhizin (5), rhaoglucoglycyrrhizin (6), rhaogalactoglycyrrhizin (7), 11-deoxo-20α-glycyrrhizin (8), 20α-galacturonoylglycyrrhizin (9), and 20α-rhaoglycyrrhizin (10).
The consumption of artificial sweeteners is very popular because they are low in calories. Although, Food and Drug Administration has approved aspartame, acesulfame-k, neotame, cyclamate and alitame for use as per acceptable daily intake value, but it is becoming increasingly evident that breakdown products of these sweeteners may produce harmful metabolic effects in the visceral tissues and brain. Thus, aspartame is hydrolyzed into phenylalanine, aspartic acid, and methanol. Phenylalanine regulates neurotransmitters, whereas aspartic acid plays an important role in inducing excitotoxicity in the brain. Lastly methanol is oxidized into formaldehyde and diketopiperazine, a carcinogen, which mediates a number of other highly toxic effects. In experimental rats saccharin is known to cause bladder cancer. Steviol, a natural extract from the Stevia plant is a mutagen, but the safety of steviol glycoside as well as steviol oxidatives has been proven. Sucralose (Splenda™) is chlorinated sucrose, which is 600 times sweeter than sucrose. Sucralose has been reported to cause dizziness, head and muscle aches, stomach cramps, diarrhea, chronic inflammation and bladder issues in rodents and humans. So far studies performed on the safety of artificial sweeteners have been a major concerned due to their neurological effects and cancer-related issues.
The human gustatory system is capable of identifying five major taste qualities: sweet. sour, bitter. salty and savory (umami). and perhaps several sub-qualities. This is a relatively small number of qualities given the vast number and structural diversity of chemical compounds that elicit taste. When we consume a food. our taste receptor cells are activated by numerous stimuli via several transduction pathways. An important food-related taste question which remains largely unanswered is: How do taste perceptions change when multiple taste stimuli are presented together in a food or beverage rather than when presented alone? The interactions among taste compounds is a large research area that has interested electrophysiologists, psychophysicists, biochemists, and food scientists alike. On a practical level, taste interactions are important in the development and modification of foods. beverages or oral care products. Is there enhancement or suppression of intensity when adding stimuli of the same or different qualities together? Relevant psychophysical literature on taste-taste interactions along with selected psychophysical theory is reviewed. We suggest that the position of the individual taste Stimuli on the concentration-intensity psychophysical curve (expansive, linear, or compressive phase of the curve) predicts important interactions when reporting enhancement or Suppression of taste mixtures.
The recent molecular identification and characterization of the T1R taste receptors have dramatically advanced understanding of the sweet taste. Genetic studies of sweetener preferences in mice have substantially contributed to this progress and they remain efficient tools for understanding how sweet taste perception is organized. Several lines of genetic evidence indicate that sweeteners belong to more than one group with potentially different receptor/transduction mechanisms. This is consistent with previous electrophysiological and pharmacological analyses of sweet taste responses and with very recent molecular studies. Analyzing taste responses in vivo, combined with in vitro molecular approaches, will continue to be a powerful tool for understanding sweet taste perception.
Consumption of sugar-sweetened beverages (SSBs) is considered to be a contributor to diabetes and the epidemic of obesity in many countries. The popularity of non-caloric carbonated soft drinks as an alternative to SSBs may be a factor in reducing the health risks associated with SSBs consumption. This study focuses on the perceptual discrimination of SSBs from artificially sweetened beverages (ASBs). Fifty-five college students rated 14 commercially available carbonated soft drinks in terms of sweetness and likeability. They were also asked to recognize, if the drinks contained sugar or a non-caloric artificial sweetener. Overall, participants showed poor accuracy in discriminating drinks’ sweeteners, with significantly lower accuracy for SSBs than ASBs. Interestingly, we found a dissociation between sweetener recognition and drink pleasantness. In fact, in spite of a chance-level discrimination accuracy of SSBs, their taste was systematically preferred to the taste of non-caloric beverages. Our findings support the idea that hedonic value of carbonated soft drinks is dissociable from its identification and that the activation of the pleasure system seems not to require explicit recognition of the sweetener contained in the soft drink. We hypothesize that preference for carbonated soft drinks containing sugar over non-caloric alternatives might be modulated by metabolic factors that are independent from conscious and rational consumers’ choices.
The sense of taste allows organisms to evaluate the quality of the food they consume with each of the five basic taste qualities fulfilling a specie subtask. The recent years have seen the molecular identification and characterization of sweet, umami, bitter and sour taste receptors. Their discovery allowed tremendous progress to be made in the understanding of peripheral taste transduction and quality coding. The present review summarizes the recent advances in taste transduction and gives an outlook over the next steps to go.
Effective dispersion of the active species over the support almost always guarantees high catalytic efficiency. To achieve this high dispersion, a favourable interaction of the active species with the support is crucial. We show here that the crystal structure of the titania support determines the interaction and consequently the nature of ruthenium particles deposited on the support. Similar crystal structures of RuO2 and rutile titania result in a good lattice matching and ensure a better interaction during the heating steps of catalyst synthesis. This helps maintain the initial good dispersion of the active species on the support also in the subsequent reduction step, leading to better activity and selectivity. This highlights the importance of understanding the physico-chemical processes during various catalyst preparation steps, because the final catalyst performance often depends on the type of intermediate structures formed during the preparation.
Facing a mounting obesity crisis, food and beverage companies are under pressure to increase the nutritional value of their products. However, reducing the amount of sugar and calories in consumer products without compromising on taste is a momentous challenge. This chapter focuses on the recent discovery of positive allosteric modulators of the sweet taste receptor. These modulators, capable of enhancing sweet taste without some of the off-notes typically associated with zero-calorie sweeteners, could likely revolutionise the flavour industry.
Two new flavonoids, 8-formyl-3′,4′-dihydroxy-6,7-dimethoxyflavone (1) and 8-formyl-4′-hydroxy-3′,6,7- trimethoxyflavone (2), were isolated from the fruits of Ziziphus jujuba Mill. Their structures were elucidated on the basis of extensive NMR and MS means. The anti-tobacco mosaic virus (anti-TMV) and antioxidant activity of 1 and 2 were evaluated. They both showed anti-TMV activity with inhibition rates of 92.8% and 88.6%, and antioxidant activity with an IC50 value of 3.16 μg/mL and 3.87 μg/mL, respectively.
FINAL REPORT 2.8 Report from Joint Industry Programme to summarize the current technical/policy obstacles on use of dispersants for each Arctic nation
Non-nutritive sweeteners (NNSs) provide sweetness to foods and beverages without adding calories. They have thus been found useful in minimizing the dietary sugar content of diabetics and the dietary energy content of individuals attempting to lose or maintain body weight. Their usefulness in weight reduction has recently been questioned, however, based on the notion that they can actually increase hunger and food intake and thereby promote weight gain. The evidence offered in support of this idea comes principally from the fields of taste physiology, metabolic endocrinology, human behavior, and epidemiology. This review evaluates this evidence and does not find it compelling. Indeed, the most straightforward findings to the contrary derive from several intervention studies in both children and adults showing that the chronic, covert replacement of dietary sugar with NNSs does not increase, and can in fact reduce, energy intake and body weight.
Reliable and sensitive chromatographic methods have been developed and applied to determine derivatized di- and tripeptides: aspartame, carnosine, glutathione, alanyl-glutamine, and γ-glutamyl-cysteine. Photodiode-array detection was used for dansyl-chloride derivatives, while fluorescent detection was carried out for orthophthaldialdehyde derivatized peptides to obtain higher sensitivity. The sensitivity and detection limits were determined and compared in order to select the most efficient analytical method. Transition metal complexes [zinc(II), cadmium(II), silver(I), and copper(II)] with cysteine containing peptides were also determined with ultraviolet-visible detection. The structural identification was carried out by the analysis of the mass-spectra recorded with an atmospheric pressure chemical ionization method in separate chromatographic experiments.
Sucralose is a synthetic organochlorine sweetener (OC) that is a common ingredient in the world's food supply. Sucralose interacts with chemosensors in the alimentary tract that play a role in sweet taste sensation and hormone secretion. In rats, sucralose ingestion was shown to increase the expression of the efflux transporter P-glycoprotein (P-gp) and two cytochrome P-450 (CYP) isozymes in the intestine. P-gp and CYP are key components of the presystemic detoxification system involved in first-pass drug metabolism. The effect of sucralose on first-pass drug metabolism in humans, however, has not yet been determined. In rats, sucralose alters the microbial composition in the gastrointestinal tract (GIT), with relatively greater reduction in beneficial bacteria. Although early studies asserted that sucralose passes through the GIT unchanged, subsequent analysis suggested that some of the ingested sweetener is metabolized in the GIT, as indicated by multiple peaks found in thin-layer radiochromatographic profiles of methanolic fecal extracts after oral sucralose administration. The identity and safety profile of these putative sucralose metabolites are not known at this time. Sucralose and one of its hydrolysis products were found to be mutagenic at elevated concentrations in several testing methods. Cooking with sucralose at high temperatures was reported to generate chloropropanols, a potentially toxic class of compounds. Both human and rodent studies demonstrated that sucralose may alter glucose, insulin, and glucagon-like peptide 1 (GLP-1) levels. Taken together, these findings indicate that sucralose is not a biologically inert compound.
Taste receptors function as one of the interfaces between internal and external milieus. Taste receptors for sweet and umami (T1R [taste receptor, type 1]), bitter (T2R [taste receptor, type 2]), and salty (ENaC [epithelial sodium channel]) have been discovered in the recent years, but transduction mechanisms of sour taste and ENaC-independent salt taste are still poorly understood. In addition to these five main taste qualities, the taste system detects such noncanonical "tastes" as water, fat, and complex carbohydrates, but their reception mechanisms require further research. Variations in taste receptor genes between and within vertebrate species contribute to individual and species differences in taste-related behaviors. These variations are shaped by evolutionary forces and reflect species adaptations to their chemical environments and feeding ecology. Principles of drug discovery can be applied to taste receptors as targets in order to develop novel taste compounds to satisfy demand in better artificial sweeteners, enhancers of sugar and sodium taste, and blockers of bitterness of food ingredients and oral medications.
J. Inst. Brew. 110(4), 352–359, 2004 Lagers are generally brewed to minimise the final sugar content. Residual saccharides, derived from starch, contribute little to sweetness. Despite this, certain lagers exhibit sweet characters. These have not been explored in lagers, but are thought to origi-nate from: maltol; 4-hydroxy-2,5-dimethyl-3(2H)-furanone (HDMF); 4-hydroxy-2(or 5)-ethyl-5(or 2)-methyl-3(2H)-fura-none (HEMF); hydroxymethylfurfural (HMF); diacetyl; and certain esters (ethyl acetate, ethyl caproate, ethyl caprylate, and iso amyl acetate). This study used time-intensity (TI) profiling, employing 13 assessors, to study sweetness in 10 lagers, scored similarly for sweetness in rank rating. Single intensity maxima were obtained with all products and all assessors. Data were analysed using ANOVA of curve parameters and non-centred and centred principal component analyses (PCA). In ANOVA only the area under curve (A tot) values differed significantly. However, shape of TI profile, or signature, differed between as-sessors who could on this basis be divided into two groups. In the multivariate data analyses, non-centred PCA showed sig-nificant differences between lagers, parametric modelling and conventional PCA did not. However TI profile data suggested sweetness intensity perceived over the 120 seconds following ingestion could differ, although differences in scoring in rank rating were not significant.
The role of habituation of mouthing activity in the control of ingestion was investigated in 6-, 12-, and 18-day-old rat pups. In pups at all ages, oral habituation to a flavored diet inhibited ingestion of a continuous oral infusion of that same diet. Twelve-day-old pups that had orally habituated to a diet continued to consume less of a continuous oral infusion of that diet both 30 min and 3 hr later, and the duration of suppressed ingestion was shown to be dependent on the rate of stimulus presentation during habituation experience. These data suggest that oral habituation may be a diet-specific influence on both intra- and intermeal patterning.
Two groups of three subjects participated in a residential study that assessed the effects of varying the macronutrient and caloric content of a required lunch meal on subsequent food choice and intake. Lunches contained 431 or 844 kcal, with the caloric differential created by manipulating the calories derived from either fat or carbohydrate (CHO). Each lunch condition (high-fat, high-CHO, low-fat, and low-CHO) was examined for 3 consecutive days. Subjects controlled their own patterns of food intake and could consume any item or number of items at any time during the day or night. There were no significant differences in total daily caloric intake across conditions, indicating that subjects compensated for the caloric content of the lunch regardless of the macronutrient content. Total daily caloric intake under the high-fat and high-CHO conditions was 2824 +/- 151 (mean +/- SEM) and 2988 +/- 187 kcal, respectively, whereas intake under the low-fat and low-CHO conditions was 2700 +/- 131 and 2890 +/- 247 kcal, respectively.
Six subjects participated in a residential study assessing the effects of covert macronutrient and energy manipulations during three required-eating occasions (breakfast, lunch, and afternoon snack) on total macronutrient and energy intakes. Overall, energy content of the occasions varied between ≈3000 and ≈7000 kJ (≈700 and ≈ 1700 kcal) with the majority of the differential derived from either fat or carbohydrate (CHO). Each condition (high, medium, and low fat; high, medium, and low CHO; and no required eating) was examined for 2 d. Subjects compensated for the energy content of the required occasions such that only under the low-CHO condition (11 297 ± 3314 kJ) was total daily energy intake lower than that observed in the absence of required occasions (13 297 ± 1356 kJ). Only total energy intake under the high-fat condition (12 326 ± 2548 kJ) was significantly different from its matched CHO condition (high-CHO condition: 14 665 ± 2686 kJ). In contrast to the clear evidence for caloric compensation, there were no differential effects of condition on macronutrient intake, ie, there was no macronutrient compensation.
This chapter provides an overview of the present knowledge of the receptors that mediate sweet taste. It emphasizes that no sweet receptor has ever been isolated nor are the physicochemical properties of molecules necessary to initiate a sweet sensation well understood. The most prominent theory to date is that a pair of simultaneous hydrogen bonds separated by approximately 3 Å is a necessary condition for sweetness. The investigations that shed light on the nature of sweet receptors derive from a range of disciplines including organic chemistry, biochemistry, neurophysiology, psychology, biophysics, and medicinal chemistry. The chapter discusses the following topics—(1) the chemical structure of sweeteners; (2) biochemical approaches to understanding sweet receptors; (3) the electrophysiological and behavioral approaches in animals; (4) the psychophysical studies in humans including data implicating sodium transport and adenosine receptors in sweet taste; and (5) computer-assisted molecular design—a new approach to design sweeteners.
Intense sweeteners represent one of the most fascinating areas of food science. Chemically these products are extremely diverse, from amino acids (e.g. aspartame) to halogenated sugars (e.g. sucralose). Several of these products were discovered accidentally (e.g. saccharin), while others are the result of concerted efforts to develop a commercially viable high intensity sweetener (e.g. alitame).
It is almost certain that since early in time the sense of sweet taste has directed both man and animals to nutritive substances. Thus taste perception probably played an essential role for survival. From an evolutionary view point, it is also likely that plants took advantage of this aspect of sweet taste to propagate their species by producing sweet fruits and other edible parts. Thus, on a volume basis, most natural sweet substances are carbohydrates from plants. However, it is also apparent that some non-carbohydrate compounds have accidentally acquired a sweet taste with no nutritive intention. Most natural sweeteners belong to this category. In modern times, at least for most people of the Western world, the attainment of adequate nourishment has not been an issue, and sweet taste perception has been sought after for the alternative purpose of giving pleasure and enjoyment. In fact, twentieth-century man is more likely than not to consume excess calories. This overnourished population has increasingly succumbed to obesity and to illnesses which are favored by excess calorie consumption (e.g. cardiovascular disease, diabetes, cancer, etc.). Therefore non-nutritive sweeteners have assumed increasing importance in modern days. This chapter covers natural high-potency sweeteners, their synthetic modificants and high-potency sweeteners constituted of natural sub-units. Specifically excluded are carbohydrate sweeteners, which, though ubiquitous in nature, are of trivial sweetness potency. Among many reviews on sweeteners, a recent one (van der Wel et al., 1987) gives extensive coverage to carbohydrate sweeteners as well as many non-natural sweeteners. This chapter covers protein sweeteners (by S.-H. Kim) and non-protein sweeteners such as peptide sweeteners, terpenoid sweeteners, and polyketide sweeteners (by G.E. DuBois). Since interest in sweeteners is proportional to their viability for use in food products, the sweeteners discussed in this review will generally be described relative to the properties requisite for commercial viability. A detailed dissertation on these properties is provided in Section 6.6 and the reader is referred to it for clarification of any points not apparent in earlier sections. In the sweetener literature, various methods have been employed for reporting sweetness potencies. This complication is discussed in detail in Section 6.6. We have recalculated sweetness potencies in some cases, for the purpose of placing all data on the same scale. The recalculation methodology employed is described in Section 6.6.