Food-drug interaction between ferulic acid and nateglinide involving the fluorescein/H+ cotransport system

In clinical, patients usually take many kinds of drugs at the same time. Thus, drug-drug interactions involving transporters can often directly affect the therapeutic safety and efficacy of many drugs. However, there have been few studies on food-drug interactions involving transporters. Dietary polyphenols have been widely assumed to be beneficial to human health. Polyphenols are commercially prepared and used as functional foods. We report here for the first time that ferulic acid, which is widely used as a functional food, affects the transport of clinical agents. It is important to be aware of the potential of food-drug interactions and to act in order to prevent undesirable and harmful clinical consequences.     

Interaction of coenzyme Q10 with the intestinal drug transporter P-glycoprotein

In clinical trials, patients usually take many kinds of drugs at the same time. Thus, drug-drug interactions can often directly affect the therapeutic safety and efficacy of many drugs. Oral delivery is the most desirable means of drug administration. Changes in the activity of drug transporters may substantially influence the absorption of administered drugs from the intestine. However, there have been a few studies on food-drug interactions involving transporters. It is important to be aware of the potential of food-drug interactions and to act in order to prevent undesirable and harmful clinical consequences. Coenzyme Q10 (CoQ10) is very widely consumed by humans as a food supplement because of its recognition by the public as an important nutrient in supporting human health. Since intestinal efflux transporter P-glycoprotein (P-gp) is one of the major factors in drug-drug interactions, we focused on this transporter. We report here for the first time that CoQ10, which is widely used as a food supplement, affects the transport activity of P-gp.     

Interaction of different polyphenols with bovine serum albumin (BSA) and human salivary alpha-amylase (HSA) by fluorescence quenching

Phenolic compounds are responsible for major organoleptic characteristics of plant-derived food and beverages; these substances have received much attention, given that the major function of these compounds is their antioxidant ability. In the context of this study, our major aim was study the binding of several phenolic compounds such as (+)-catechin, (-)-epicatechin, (-)-epicatechin gallate, malvidin-3-glucoside, tannic acid, procyanidin B4, procyanidin B2 gallate, and procyanidin oligomers to different proteins (bovine serum albumin and human alpha-amylase) by fluorescence quenching of protein intrinsic fluorescence. From the spectra obtained, the Stern-Volmer, the apparent static, and the bimolecular quenching constants were calculated. The structure of polyphenols revealed to significantly affect the binding/quenching process; in general, the binding affinity increased with the molecular weight of polyphenol compounds and in the presence of galloyl groups. For catechin monomer and procyanidin dimer B4, the K(SV) was 14,100 and 13,800 M(-1), respectively, and for galloyl derivatives, the K(SV) was 19,500 and 21,900 M(-1), respectively. Tannic acid was shown to be the major quenching molecule for both proteins. However, comparing different proteins, the same polyphenol showed different quenching effects, which are suggested to be related to the three-dimensional structure of the proteins studied. For (+)-catechin and BSA, the K(SV) was 8700 M(-1), and with alpha-amylase, it was 14,100 M(-1); for tannic acid, the K(SV) was 10,0548 and 11,0674 M(-1), respectively. From the results obtained, besides the main binding analysis performed, we conclude that this technique is more sensitive than thought because we can detect several interactions that have not been proven by other methods, namely, nephelometry. Overall, fluorescence quenching has proven to be a very sensitive technique with many potentialities to analyze the interaction between polyphenols and proteins.     

Inhibitory effects of green tea polyphenols on the production of a virulence factor of the periodontal-disease-causing anaerobic bacterium Porphyromonas gingivalis

The effect of polyphenolic compounds isolated from green tea (Camellia sinensis) on the production of toxic end metabolites of Porphyromonas gingivalis was investigated. Green tea polyphenols completely inhibited the production of n-butyric acid and propionic acid at a concentration of 1.0-2.0 mg/mL in general anaerobic medium (GAM). (-)-Epigallocatechin gallate (EGCg), which is a major component of tea polyphenols also inhibited the production of phenylacetic acid at 0.5 mg/mL in GAM broth. In the experiment using resting cells of P. gingivalis, phenylacetic acid was produced from l-phenylalanine and phenylpyruvic acid, but this reaction was also inhibited by EGCg, (-)-epicatechin gallate, and (-)-gallocatechin gallate. However, (+)-catechin, (+)-gallocatechin, (-)-epicatechin, and (-)-epigallocatechin did not inhibit those reactions. These results indicate that the inhibitory effect on the production of toxic end metabolites of P. gingivalis can be attributed to the presence of the galloyl moiety, which is ester-linked with the 3-OH of the catechin moiety in the polyphenolic compounds. This study shows that continuous application of tea polyphenols on a daily basis can be considered as a useful and practical method for the prevention of periodontal diseases.     

大孔树脂纯化黄精多酚及其抗氧化性与组成分析

考察4种树脂对黄精多酚粗提物的吸附-解吸特性,筛选出最佳的纯化树脂,并研究其纯化工艺,分析黄精多酚的体外抗氧化活性、红外光谱特性和单酚组成。结果表明,AB-8型大孔树脂最适合于对黄精多酚粗提液的纯化,静态吸附5 h达到饱和,静态解吸3 h达到平衡;在室温下,用质量浓度为0.80 mg/mL的黄精多酚粗提液以0.8 mL/min的流速上样;吸附平衡后以70%的乙醇为洗脱剂,在洗脱流速为1 mL/min时,大孔树脂纯化效果最好,经纯化后黄精多酚的纯度提高了3.37倍。黄精多酚具有较好的抗氧化能力,且具有良好的量效关系,纯化前后黄精多酚总还原能力的IC50值分别为(27.48±1.93)、(19.01±1.48)μg/mL,清除DPPH·的IC50值依次为(5.21±0.48)、(4.00±0.26)μg/mL,清除ABTS+·的IC50值依次为(4.89±0.82)、(4.21±0.53)μg/mL,经纯化后黄精多酚的抗氧化活性明显增强。红外光谱分析表明其具有多酚和黄酮的特征峰;HPLC-DAD分析表明,黄精多酚主要含绿源酸,阿魏酸,芦丁和熊果酸。     

Cytogenetic effects of grape extracts (Vitis vinifera) and polyphenols on mitomycin C-induced sister chromatid exchanges (SCEs) in human blood lymphocytes

In the present study, the effects of extracts and polyphenol-rich fractions as well as monomer polyphenols identified in them, from both red and white grapes, on mitomycin C (MMC) induced sister chromatid exchanges (SCEs) in human peripheral blood lymphocytes were investigated. The grape extracts and two of the three polyphenol-rich fractions promoted MMC-induced SCEs at concentrations from 75 to 300 microg/mL. However, none of the extracts or fractions alone induced SCEs. Thus, these results suggest caution especially with regard to the use of grape extracts as dietary supplements. On the other hand, the fact that these extracts were not genotoxic alone may indicate a selective activity against genetically damaged cells. This is the first study regarding the clastogenic effects of grape extracts in human cells. Moreover, from the tested polyphenols, caffeic acid, gallic acid, and rutin hydrate enhanced MMC-induced clastogenicity, whereas ferulic acid, protocatechuic acid, (+)-catechin, (-)-epicatechin, and trans-resveratrol had no effect at concentrations between 5 and 100 microM. The differences in the chemical structures of the tested polyphenols may account for their differential effects on MMC clastogenicity.     

A matured fruit extract of date palm tree (Phoenix dactylifera L.) stimulates the cellular immune system in mice

The immunomodulatory effects of a hot water extract from matured fruit of the date palm tree (Phoenix dactylifera L.) were investigated in comparison to those of prune and fig fruit in mice. The number of spleen IFN-γ(+)CD4(+), IFN-γ(+)CD49b(+) and IL-12(+)CD11b(+) cells was highest in mice given the date extract-added diet. Polyphenols identified in the date extract, such as chlorogenic acid, caffeic acid, pelargonin and ferulic acid, stimulated IFN-γ mRNA expression significantly in mouse Peyer's patch cell cultures. Chlorogenic acid and caffeic acid also increased the number of IFN-γ(+)CD4(+) cells significantly, while some polyphenols increased the number of IFN-γ(+)CD49b(+) and IL-12(+)CD11b(+) cells significantly. On the other hand, a 70% ethanol-insoluble date extract treated with trypsin increased the number of IFN-γ(+)CD49b(+) and IL-12(+)CD11b(+) cells significantly. These results indicate that some polyphenols and polysaccharides present in date fruit stimulate the cellular immune system in mice.     

Probing the interaction of polyphenols with lipid bilayers by solid-state NMR spectroscopy

Polyphenols are bioactive natural products that appear to act against a wide range of pathologies. Mechanisms of activity have not been established, but recent studies have suggested that some polyphenols bind to membranes. This study examined the interaction between lipid bilayers and three structurally diverse polyphenols. It was hypothesized that features of the polyphenols such as polarity, molecular size, molecular geometry, and number and arrangement of phenol hydroxyl groups would determine the tendency to interact with the bilayer. The examined compounds included a mixed polyphenol, (-)-epigallocatechin gallate (EGCg); a proanthocyanidin trimer comprising catechin-(4→8)-catechin-(4→8)-catechin (cat?; and a hydrolyzable tannin, 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose (PGG). These polyphenols were incorporated at different levels into 2H-labeled 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) multilamellar vesicles (MLVs). 31P and 2H solid-state NMR experiments were performed to determine the dynamics of the headgroup region and the hydrophobic acyl chain region of the lipid bilayer upon addition of polyphenols. The chemical shift anisotropy (CSA) width of the 31P NMR spectra decreased upon addition of polyphenols. Addition of PGG induces a dramatic reduction on the CSA width compared with the control lipid bilayer sample, whereas addition of cat? barely reduces the CSA width. The 2H quadupolar splitting of the lipids also decreased upon addition of polyphenols. At the same concentration, PGG substantially reduced the quadrupolar splitting, whereas cat? barely reduced it when compared with the control sample. From a calculation of the order parameters of the acyl chain region of the lipid bilayer, it was concluded that the hydrophobic part of the lipid bilayer was perturbed by PGG, whereas cat? did not cause large perturbations. The data suggest that the polarity of the polyphenols affects the interaction between tannins and membranes. The interactions may relate to the biological activities of polyphenols.     

低植酸作物遗传改良途径与磷资源高效利用

  【目的】  磷是作物生长发育所必需的营养元素。在植物体内,磷多以植酸形式储存在成熟籽粒中。非反刍动物,包括人类,无法消化植酸来获取磷及植酸螯合的有益元素,籽粒中收获的大量磷素进入人及动物排泄物,不仅造成磷资源浪费,也加大了环境风险。因此,培育籽粒低植酸品种是改善作物营养品质、降低磷素环境风险的重要途径。本文综述作物籽粒磷的来源,控制籽粒植酸磷含量的主要生理过程及遗传改良策略等研究进展,为相关领域研究奠定基础。  主要进展  籽粒植酸磷的积累主要由3步组成,木质部或韧皮部向籽粒转运无机磷酸盐,籽粒利用无机磷酸盐合成植酸,植酸被运输至液泡中储存。目前已分离鉴定到负责相关过程的转运蛋白和关键酶及其编码基因,如SULTR3;4、SULTR3;3、PHT1;4蛋白介导无机磷酸盐向籽粒的转运,MIPS、ITPK、IPK1酶参与植酸的合成,以及MRP蛋白介导植酸合成后的转运储藏。对籽粒低植酸突变体的产量、农艺性状表型及改良策略的优缺点进行比较,籽粒低植酸品种可能存在产量下降、种子萌发率低等不足。  展望  未来可以从特异性修饰籽粒中关键基因的时空表达、发掘关键基因的优良等位变异及针对品种的磷营养管理3个方向,深入研发籽粒低植酸含量的高产品种,实现磷资源高效利用。     

Tea polyphenols inhibit the transport of dietary phenolic acids mediated by the monocarboxylic acid transporter (MCT) in intestinal Caco-2 cell monolayers

It was previously reported that a fluorescent marker dye, fluorescein, is transported via the monocarboxylic acid transporter (MCT). Fluorescein transport was competitively inhibited by MCT substrates such as ferulic and salicylic acids. Tea polyphenols, in particular, epigallocatechin gallate (EGCg) and epicatechin gallate (ECg), inhibited the transport of fluorescein. Tea polyphenols also inhibited the transport of salicylic and ferulic acids, suggesting tea polyphenols might be substrates of MCT. However, the transepithelial flux of tea polyphenols was much lower than that of the MCT substrates and was inversely correlated with the paracellular permeability of Caco-2 cell monolayers. These findings suggest that tea polyphenols are not substrates but inhibitors of MCT. Furthermore, the transepithelial transport of these polyphenols is mainly via paracellular diffusion. However, directional transport of ECg and EGCg from the basolateral to the apical side was observed, indicating that the behavior of tea polyphenols in the intestinal epithelium is complex.     

How to standardize the multiplicity of methods to evaluate natural antioxidants

A great multiplicity of methods has been used to evaluate the activity of natural antioxidants by using different techniques of inducing and catalyzing oxidation and measuring the end point of oxidation for foods and biological systems. Antioxidant in vitro protocols for foods should be based on analyses at relatively low levels of oxidation under mild conditions and on the formation and decomposition of hydroperoxides. For antioxidant in vivo protocols, widely different methods have been used to test the biological protective activity of phenolic compounds. Unfortunately, many of these protocols have been based on questionable methodology to accurately measure oxidative damage and to assess relevant changes in biological targets. Many studies testing the ex vivo activity of phenolic compounds to inhibit human low-density lilpoprotein (LDL) oxidation have been difficult to evaluate because of the structural complexity of LDL particles and because a multitude of markers of oxidative damage have been used. Although studies with animal models of atherosclerosis have demonstrated the antioxidant effect of phenolic compounds in delaying the progress of this disease, human clinical trials of antioxidants have reported inconsistent and mixed results. Complex mixtures of plant polyphenols have been shown to be absorbed to varying degrees as metabolites in the intestine, but little is known about their interactions, bioavailability, and their in vivo antioxidant activity. Several metabolites identified in human plasma after consuming flavonoids need to be tested for possible nonantioxidant activities. More research and better-designed human studies are required to clarify the complex questions of bioavailability of polyphenols and the factors affecting their in vivo activities. Until we know what relevant in vivo activities to measure, any claims on the biological and health protective effects of natural polyphenolic compounds in our diet are premature.     

Absorption of anthocyanins from blueberry extracts by caco-2 human intestinal cell monolayers

Recent studies have shown that dietary polyphenols may contribute to the prevention of cardiovascular disease and cancer. Anthocyanins from different plant sources including blueberries have been shown to possess potential anticancer activities. One of the key factors needed to correctly relate the in vitro study results to human disease outcomes is information about bioavailability. The objectives of the current study were to evaluate the absorption of blueberry anthocyanin extracts using Caco-2 human intestinal cell monolayers and investigate the effects of different aglycones, sugar moieties, and chemical structure on bioavailability of different types of anthocyanins. The results of this study showed that anthocyanins from blueberries could be transported through the Caco-2 cell monolayers although the transport/absorption efficiency was relatively low compared to other aglycone polyphenols. The transport efficiency of anthocyanins averaged approximately 3-4% [less than 1% in delphinidin glucoside (Dp-glc)]. No significant difference in transport/absorption efficiency was observed among three blueberry cultivars. The observed trends among different anthocyanins generally agreed well with some published in vivo results. Dp-glc showed the lowest transport/absorption efficiency, and malvidin glucoside (Mv-glc) showed the highest transport/absorption efficiency. Our result indicates that more free hydroxyl groups and less OCH(3) groups can decrease the bioavailability of anthocyanins. In addition, cyanindin glucoside (Cy-glc) showed significantly higher transport efficiency than cyanidin galactoside (Cy-gal), and peonidin glucoside (Pn-glc) showed significantly higher transport efficiency than peonidin galactoside (Pn-gal), indicating that glucose-based anthocyanins have higher bioavailability than galactose-based anthocyanins.     

水稻磷素吸收与转运分子机制研究进展

磷素是植物体内重要的大量元素之一,其含量约占植物干重的 0.2%。由于磷元素作为许多重要生物大分子的关键组分,且参与植物体内许多的生理生化反应,因此植物的生长和发育都离不开磷元素。植物在长期的进化过程中,形成了一套高效地吸收和利用磷素的分子调控机制。本文将重点阐述水稻中无机磷从土壤吸收进根系再转运到地上部并进行分配的分子机制,并对今后的水稻磷素吸收和转运的研究重点进行展望。水稻根系主要通过定位在细胞膜上的磷酸盐转运体 (Phosphate Transporter1,PHT1) 吸收土壤中无机磷。当无机磷被吸收进入根系细胞内部后,通过质外体和共质体两种养分的运输途径,将其运输到根中维管束,并通过PHO1 将无机磷由根系加载到地上部。然后水稻根据其地上部不同组织器官对无机磷的需求进行分配,而多余的无机磷将储存在液泡内,维持细胞内无机磷的平衡。目前对磷酸盐转运体吸收磷素的分子机制研究较为清楚,但对于磷素在植物体内的储存、分配和再利用过程的机制还研究较少。液泡作为水稻无机磷储存的主要部位,对于维持细胞内无机磷的平衡尤其重要;节是水稻营养元素 (包括磷素) 在地上部进行分配的重要部位。但目前对于定位于液泡膜上和节上的磷酸盐转运体的机制研究较少。因此,未来挖掘与解析水稻体内负责磷素储存、分配和再利用的磷酸盐转运体及其作用机制,能为培育磷高效利用的水稻提供新的依据。     

Transport of cadmium from soil to grain in cereal crops: A review

Due to rapid urbanization and industrialization, many soils for crop production are contaminated by cadmium(Cd), a heavy metal highly toxic to many organisms. Cereal crops such as rice, wheat, maize, and barley are the primary dietary source of Cd for humans, and reducing Cd transfer from soil to their grains is therefore an important issue for food safety. During the last decade, great progress has been made in elucidating the molecular mechanisms of Cd transport, particularly in rice. Inter-and intraspecific variations in Cd accumulation have been observed in cereal crops. Transporters for Cd have been identified in rice and other cereal crops using genotypic differences in Cd accumulation and mutant approaches. These transporters belong to different transporter families and are involved in the uptake, vacuolar sequestration, root-to-shoot translocation, and distribution of Cd. Attempts have been made to reduce Cd accumulation in grains by manipulating these transporters through overexpression or knockout of the transporter genes, as well as through marker-assisted selection breeding based on genotypic differences in Cd accumulation in the grains. In this review, we describe recent progress on molecular mechanisms of Cd accumulation in cereal crops and compare different molecular strategies for minimizing Cd accumulation in grains.     

酸法提取青稞麸皮结合酚工艺优化

为了提高青稞的附加利用价值,该文以青稞麸皮为研究对象,考察了提取试剂、酸质量分数、萃取pH值、料液比和提取温度对多酚质量分数和 DPPH·自由基清除能力的影响。采用中心组合设计优化其结合酚提取工艺。结果表明,青稞结合酚提取最优工艺条件为：提取试剂为硫酸,酸质量分数为11.10%,水料比为1：17 g/mL,提取温度为75℃,pH值不作处理,此条件下提取得到的结合酚质量分数达224.33 mg/(100 g),DPPH·自由基清除能力达9919.28μmol/(100 g),与预测值多酚质量分数243.80 mg/(100 g),其DPPH·自由基清除能力9087.02μmol/(100 g)基本一致。高效液相色谱法检测到最优工艺下所得青稞结合酚中含有8种酚酸及8种黄酮类物质,总量达325.104 mg/(100 g)。研究结果为全面评价青稞结合酚含量及青稞麸皮的高效利用提供科学依据。     

Effect of 3-O-octanoyl-(+)-catechin on the responses of GABA(A) receptors and Na+/glucose cotransporters expressed in xenopus oocytes and on the oocyte membrane potential

Recently, 3-O-octanoyl-(+)-catechin (OC) was synthesized from (+)-catechin (C) by incorporation of an octanoyl chain into C in the light of (-)-epicatechin gallate (ECg) and (-)-epigallocatechin gallate (EGCg), which are the major polyphenols found in green tea and have strong physiological activities. OC was found to inhibit the response of ionotropic gamma-aminobutyric acid (GABA) receptors (GABA(A) receptors) and Na+/glucose cotransporters expressed in Xenopus oocytes in a noncompetitive manner more strongly than does C. OC also induced a nonspecific membrane current and decreased the membrane potential of the oocyte, and thus death of the oocyte occurred even at lower concentrations than that induced by C or EGCg. Although EGCg produced H2O2 in aqueous solution, OC did not. This newly synthesized catechin derivative OC possibly binds to the lipid membrane more strongly than does C, Ecg, or EGCg and as a result perturbs the membrane structure.     

Quantitative examination of oxidized polyphenol-protein complexes

We quantitatively examined interactions between polyphenols and proteins under oxidizing conditions, using radiolabeled 1,2,3,4,6-penta-O-galloyl-d-glucopyranose (PGG) and bovine serum albumin (BSA) as model compounds. We tested NaIO(4), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation (ABTS.+), and 2,2'-azobis(isobutyramidine) dihydrochloride (AAPH) as model oxidants and used sodium dodecyl sulfate to disrupt noncovalent PGG-BSA interactions after the oxidation. We used trichloroacetic acid to isolate the PGG-BSA products after oxidation for radiochemical quantitation. NaIO(4) and ABTS.+ oxidized PGG-BSA complexes more rapidly than AAPH. Using NaIO(4) as the oxidant, we found that soluble oxidized PGG-BSA complexes formed rapidly and were converted to insoluble complexes if PGG was present in excess over BSA.     

Proanthocyanidin composition in the seed coat of lentils (Lens culinaris L.)

Lentils (Lens culinaris L.) are a popular food in many countries. However, little is known about their phenolic composition. Because polyphenols in lentils are located essentially in their seed coat, the objective of this work was to study the composition of proanthocyanidins, the major group of polyphenols, in this part of the tissue. The use of C(18) Sep-Pak cartridges permitted the fractionation of lentil seed coat extract into monomer, oligomer, and polymer proanthocyanidin fractions. Subsequent thiolysis of oligomer and polymer fractions followed by HPLC analysis allowed the mean degree of polymerization (mDP) and the structural composition of proanthocyanidins to be determined. A fractionation of lentil seed coat extracts on a polyamide column followed by HPLC and HPLC-DAD-MS analyses was used to identify the individual proanthocyanidins. The results showed that the major monomeric flavan-3-ol was (+) catechin-3-glucose, with lesser amounts of (+)-catechin and (-)-epicatechin. In the oligomer fraction, various dimer, trimer, and tetramer proanthocyanidins constituted of catechin, gallocatechin, and catechin gallate units were identified, and several procyanidins and prodelphinidins from pentamers to nonamers constitute the polymer fraction. The most abundant proanthocyanidins in the seed coat of lentils are the polymers (65-75%), with a mDP of 7-9, followed by the oligomers (20-30%), with a mDP of 4-5.     

Isolation and quantitative analysis of phenolic antioxidants, free sugars, and polyols from mango (Mangifera indica L.) stem bark aqueous decoction used in Cuba as a nutritional supplement

An aqueous decoction of mango (Mangifera indica L.) stem bark has been developed in Cuba on an industrial scale to be used as a nutritional supplement, cosmetic, and phytomedicine. Previously we reported its antioxidant activity, and we concluded that the product could be useful to prevent the production of reactive oxygen species and oxidative tissue damage in vivo. A phytochemical investigation of mango stem bark extract has led to the isolation of seven phenolic constituents: gallic acid, 3,4-dihydroxy benzoic acid, gallic acid methyl ester, gallic acid propyl ester, mangiferin, (+)-catechin, (-)-epicatechin, and benzoic acid and benzoic acid propyl ester. All structures were elucidated by ES-MS and NMR spectroscopic methods. Quantitative analysis of the compounds has been performed by HPLC, and mangiferin was found to be the predominant component. Total polyphenols were assayed also by the Folin-Ciocalteu method. The free sugars and polyols content was also determined by GC-MS.     

Polyphenol-induced inhibition of the response of na(+)/glucose cotransporter expressed in Xenopus oocytes

To study the effects of polyphenols on the Na(+)/glucose cotransporter (SGLT1) response, SGLT1 was expressed in Xenopus oocytes by injecting cRNA synthesized from the cloned cDNA of the small intestine cotransporter of rats, and the electrical response elicited by glucose or galactose was measured by a voltage clamping method. Most phenol derivatives had no effect on the response. However, the polyphenols (+)-catechin, (-)-epicatechin gallate (ECg), and (-)-epigallocatechin gallate (EGCg), which are components of green tea, caused an inhibition of the response, which was almost independent of glucose concentration. The inhibition constants were estimated to be 2.3 mM for (+)-catechin and 0.45 mM for both ECg and EGCg, assuming the noncompetitive inhibition mechanism. Saponin prepared from tea seeds also inhibited the response significantly. Tannic acid and aqueous extracts of teas induced nonspecific electrical responses in both cRNA-injected and noninjected oocytes at lower concentrations than those that caused an inhibition of the SGLT1 response when their dose-dependent effects were examined. These results are possibly helpful in the development of a dietary supplement for diabetic patients.