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Shigeto Uchiyama - One of the best experts on this subject based on the ideXlab platform.
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Effects of natural S-Equol supplements on overweight or obesity and metabolic syndrome in the Japanese, based on sex and equol status.
Clinical endocrinology, 2013Co-Authors: Takeshi Usui, Tomomi Ueno, Mayu Tochiya, Yousuke Sasaki, Kazuya Muranaka, Hajime Yamakage, Akihiro Himeno, Akira Shimatsu, Asami Inaguma, Shigeto UchiyamaAbstract:SummaryObjectives Epidemiologic studies indicate that soy intake has an important role in the prevention of age-related health problems. Daidzein, the principal isoflavone contained in soy, is converted to S-Equol by the intestinal bacteria. Not all individuals, however, can produce S-Equol, which is considered the most biologically active metabolite. We studied the effects of a natural S-Equol supplement on metabolic parameters associated with overweight or obesity and metabolic syndrome. Methods The study was a randomized, double-blinded, placebo-controlled, crossover design with no washout period. All subjects were considered overweight or obese if they had a body mass index ≧25 kg/m2. Placebo or natural S-Equol tablets containing 10 mg S-Equol were orally ingested each day for 12 weeks. A total of 54 Japanese overweight or obese outpatients were enrolled. The equol phenotype was determined, and various metabolic parameters, including cardio-ankle vascular index (CAVI), were measured. Results Equol non-producers comprised 67·9% of the overweight or obese subjects. The ratio of equol non-producers in this overweight or obese subject group was higher than the previously reported ratio of equol non-producers (approximately 50%) in the general population. Compared with the placebo group, intervention with natural S-Equol led to a significant decrease in HbA1c, serum low-density lipoprotein cholesterol (LDL-C) levels and CAVI score. Furthermore, the effect was more prominent in the subgroup of female equol non-producers. Conclusion The ratio of equol non-producers in overweight or obese populations might be higher than generally reported. Natural S-Equol might have a role in glycaemic control and in the prevention of cardiovascular disease by its effects to lower LDL-C levels and CAVI scores in overweight or obese individuals.
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discovery of an s equol rich food stinky tofu a traditional fermented soy product in taiwan
International Journal of Food Sciences and Nutrition, 2012Co-Authors: Yasuhiro Abiru, Shigeto Uchiyama, Tomomi Ueno, Megumi Kumemura, Kyosuke MasakiAbstract:A recent epidemiological study showed that daily intake of mg quantities of S-Equol is required for health-promoting effects in menopausal women. However, the maximum equol content in food was reported to be approximately 130 μg/100 g in egg yolk. The objective of this study was to find a high equol-containing food. We measured the equol content of 33 egg yolks and 21 fermented soybean foods. Equol was detected in 28 egg yolks at the maximum content of 43 μg/100 g. In the fermented soybean foods, equol was detected only in stinky tofu. We examined 16 stinky tofu samples purchased during different seasons and the average equol content was 1.39 mg/100 g, ranging from 0.34 to 2.68 mg/100 g. Equol was present in stinky tofu as the S-enantiomeric form and as an aglycon type. This is the first report demonstrating that stinky tofu contains high levels of S-Equol, which may exert beneficial effects in menopausal women.
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identification of a novel dihydrodaidzein racemase essential for biosynthesis of equol from daidzein in lactococcus sp strain 20 92
Applied and Environmental Microbiology, 2012Co-Authors: Yoshikazu Shimada, Masayuki Takahashi, Norihiro Miyazawa, Yasuhiro Abiru, Shigeto Uchiyama, Haretsugu HishigakiAbstract:Equol is metabolized from daidzein, a soy isoflavone, by the gut microflora. In this study, we identified a novel dihydrodaidzein racemase (l-DDRC) that is involved in equol biosynthesis in a lactic acid bacterium, Lactococcus sp. strain 20-92, and confirmed that histidine-tagged recombinant l-DDRC (l-DDRC-His) was able to convert both the (R)- and (S)-enantiomers of dihydrodaidzein to the racemate. Moreover, we showed that recombinant l-DDRC-His was essential for in vitro equol production from daidzein by a recombinant enzyme mixture and that efficient in vitro equol production from daidzein was possible using at least four enzymes, including l-DDRC. We also proposed a model of the metabolic pathway from daidzein to equol in Lactococcus strain 20-92.
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Comparative Activities of the S-Enantiomer and Racemic Forms of Equol on Bone Fragility in Ovariectomized Mice
Bioscience biotechnology and biochemistry, 2012Co-Authors: Yoshifumi Kimira, Shigeto Uchiyama, Tomomi Ueno, Shin-ichi Katsumata, Kazuharu Suzuki, Yoshiko Ishimi, Herman Adlercreutz, Mariko UeharaAbstract:We compared the effects of the S-enantiomer and racemic forms of equol on bone using ovariectomized (OVX) mice. Femoral bone mineral density and bone strength decreased in the OVX mice, but not in OVX mice administered 0.5 mg/d S-Equol. This, however, did not hold for racemic equol. Serum and urine S-Equol concentrations were higher in the mice administered S-Equol than in those administered racemic equol. These results suggest that the inhibitory effects of S-Equol on bone fragility in OVX mice are greater than those of racemic equol.
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The effects of natural S-Equol supplementation on skin aging in postmenopausal women: a pilot randomized placebo-controlled trial.
Menopause (New York N.Y.), 2012Co-Authors: Ayuko Oyama, Shigeto Uchiyama, Tomomi Ueno, Tomohiko Aihara, Akira Miyake, Sumio Kondo, Kayoko MatsunagaAbstract:AbstractObjectiveThe aim of this study was to investigate the effects of the natural S-Equol supplement on skin aging in equol-nonproducing Japanese postmenopausal women.MethodsA randomized, double-blind, placebo-controlled trial examined the use of the natural S-Equol supplement for 12 weeks in 101
Kenneth D. R. Setchell - One of the best experts on this subject based on the ideXlab platform.
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S-Equol: a potential nonhormonal agent for menopause-related symptom relief.
Journal of women's health (2002), 2015Co-Authors: Wulf H. Utian, Michelle Jones, Kenneth D. R. SetchellAbstract:Abstract Many women suffering from vasomotor symptoms (VMS) are now seeking nonpharmaceutical treatments for symptom relief. Recently, S-Equol, an intestinal bacterial metabolite of the soybean isoflavone daidzein has received attention for its ability to alleviate VMS and provide other important health benefits to menopausal women. S-Equol is found in very few foods and only in traces. About 50% of Asians and 25% of non-Asians host the intestinal bacteria that convert daidzein into S-Equol. Clinical trials that evaluated the efficacy of an S-Equol-containing product found that VMS were alleviated but these trials were limited in scope and primarily involved Japanese women for whom hot flashes are a minor complaint. The only trial in the United States evaluating hot flashes found symptoms were significantly reduced by S-Equol, but the study lacked a placebo group, although it did include a positive control. The daily dose of S-Equol used in most trials was 10 mg, and because the half-life of S-Equol is 7–...
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S-(-)equol production is developmentally regulated and related to early diet composition.
Nutrition research (New York N.Y.), 2014Co-Authors: Nadine M Brown, Xueheng Zhao, James E Heubi, Stephanie L. Galandi, Suzanne S. Summer, Eileen C. King, Kenneth D. R. SetchellAbstract:S-(-)7-hydroxy-3-(4'-hydroxyphenyl)-chroman, or S-(-)equol, a biologically active intestinally derived bacterial metabolite of the soy isoflavones daidzin/daidzein, is not produced in neonatal life. Because its synthesis is dependent on equol-producing bacteria, we hypothesized that early nutrition may influence equol production. This prospective 2.5-year study determined the frequency of S-(-)equol production in healthy infants (n = 90) fed breast milk, soy infant formula, or cow's milk formula in their first year. Urinary S-(-)equol and daidzein were quantified by mass spectrometry after a standardized 3.5-day soy isoflavone challenge. Infants were tested at 6, 9, 12, 18, 24, and 36 months of age, and 3-day diet records were obtained at each visit to explore the effect of early and postweaning (>12 months) macronutrient and micronutrient dietary composition and S-(-)equol production. Use of antibiotics was also recorded. At age 6 months, none of the breast-fed infants produced S-(-)equol, whereas 3.8% and 6.0%, respectively, of soy and cow's milk formula-fed infants were equol producers. By age 3 years, 50% of the formula-fed infants were equol producers, compared with 25% of breast-fed infants. Use of antibiotics was prevalent among infants and may have impacted the stability of S-(-)equol production. No significant differences among the groups were observed in postweaning dietary intakes of total energy, carbohydrate, fiber, protein, fat, saturated fatty acids, or polyunsaturated fatty acids and the propensity to make S-(-)equol. In conclusion, S-(-)equol production is developmentally regulated and initially related to diet composition with the proportion of equol producers increasing over the first 3 years of life, with a trend for formula feeding favoring S-(-)equol production.
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Dietary Factors Influence Production of the Soy Isoflavone Metabolite S-(-)Equol in Healthy Adults
The Journal of nutrition, 2013Co-Authors: Kenneth D. R. Setchell, James E Heubi, Nadine M Brown, Suzanne S. Summer, Eileen C. King, Sidney John Cole, Trish Guy, Bevan HokinAbstract:S-(-)equol, an intestinally derived metabolite of the soy isoflavone daidzein, is proposed to enhance the efficacy of soy diets. Adults differ in their ability to produce equol when consuming soy foods for reasons that remain unclear. Therefore, we performed a comprehensive dietary analysis of 143 macro- and micronutrients in 159 healthy adults in the United States (n = 89) and Australia (n = 70) to determine whether the intake of specific nutrients favors equol production. Three-d diet records were collected and analyzed using Nutrition Data System for Research software and S-(-)equol was measured in urine by mass spectrometry. Additionally, in a subset of equol producers and nonproducers (n = 10/group), we examined the long-term stability of equol producer status by retesting 12, 18, and 24 mo later. Finally, the effect of oral administration of the antibiotic metronidazole (500 mg/d for 7 d) on equol production was examined in 5 adults monitored during a 4-mo follow-up period. Equol producers accounted for 30.3% and 28.6% of the United States and Australian participants, respectively (overall frequency, 29.6%). No significant differences were observed for total protein, carbohydrate, fat, saturated fat, or fiber intakes between equol producers and nonproducers. However, principal component analysis revealed differences in several nutrients, including higher intakes of polyunsaturated fatty acids (P = 0.039), maltose (P = 0.02), and vitamins A (P = 0.01) and E (P = 0.035) and a lower intake of total cholesterol (P = 0.010) in equol producers. During a 2-y period, equol producer status remained unchanged in all nonproducers and in 80% of equol producers, whereas metronidazole abolished equol production in only 20% of participants. In conclusion, these findings suggest that major differences in the macronutrient content of the diet appear not to influence equol production, but subtle differences in some nutrients may influence the ability to produce equol, which was a relatively stable phenomenon.
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Impact of perinatal exposure to equol enantiomers on reproductive development in rodents.
Reproductive toxicology (Elmsford N.Y.), 2011Co-Authors: Nadine M Brown, Stephanie L. Lindley, David P. Witte, Kenneth D. R. SetchellAbstract:There is now considerable interest in the intestinally derived soy isoflavone metabolite, equol, which occurs in the enantiomeric forms, S-(−)equol and R-(+)equol, both differing in biological actions. Little is known about effects of either enantiomer on reproductive development, yet such knowledge is fundamental because of the recent commercialization of S-(−)equol as a dietary supplement. S-(−)equol and R-(+)equol were therefore investigated to determine their effects on reproductive development and fertility in the Sprague–Dawley rat. Neither enantiomer affected fertility, number of litters produced, number of pups per litter, number of male and female pups born, birth weight, anogenital distance, testicular descent or vaginal opening. Histological analysis showed no major abnormalities in ovary, testis, prostate or seminal vesicle tissue with dietary exposure to S-(−)equol or R-(+)equol, but both enantiomers triggered hyperplasia of uterine tissue. With R-(+)equol this stimulatory effect subsided after exposure was discontinued, but the effect of S-(−)equol was prolonged.
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Mammary gland differentiation by early life exposure to enantiomers of the soy isoflavone metabolite equol.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 2010Co-Authors: Nadine M Brown, Stephanie L. Lindley, David P. Witte, C.a. Belles, Linda Zimmer-nechemias, Mi-ok Kim, Kenneth D. R. SetchellAbstract:The role of soy in reducing breast cancer risk has been suggested to be associated with early exposure to isoflavones, which alter mammary gland morphology. The objective of the study was to determine the effect of dietary exposure to the enantiomers of a key soy isoflavone metabolite, equol, on mammary gland development and later chemoprotection using the DMBA-induced animal model of breast cancer. Animals were exposed to S-(-)equol or R-(+)equol (250 mg/kg diet) during the neonatal (0-21 days) or prepubertal (21-35 days) periods only. Histological evaluation of the mammary glands showed that both enantiomers fed neonatally via the dam led to significant precocial mammary gland differentiation. By day 50, early S-(-)equol or R-(+)equol exposure resulted in a decrease in immature terminal end structures and an increase in mature lobules, suggesting an early 'imprinting' effect. Despite these morphological changes to the mammary gland, neonatal and prepubertal exposure to equol had no long-term chemoprevention against mammary tumors induced by DMBA, although for R-(+)equol there was a trend to delaying tumor formation. In summary, early exposure to equol was not chemopreventive, but neither did it increase tumor formation in response to DMBA, suggesting exposure in early life does not influence breast cancer risk.
Nadine M Brown - One of the best experts on this subject based on the ideXlab platform.
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S-(-)equol production is developmentally regulated and related to early diet composition.
Nutrition research (New York N.Y.), 2014Co-Authors: Nadine M Brown, Xueheng Zhao, James E Heubi, Stephanie L. Galandi, Suzanne S. Summer, Eileen C. King, Kenneth D. R. SetchellAbstract:S-(-)7-hydroxy-3-(4'-hydroxyphenyl)-chroman, or S-(-)equol, a biologically active intestinally derived bacterial metabolite of the soy isoflavones daidzin/daidzein, is not produced in neonatal life. Because its synthesis is dependent on equol-producing bacteria, we hypothesized that early nutrition may influence equol production. This prospective 2.5-year study determined the frequency of S-(-)equol production in healthy infants (n = 90) fed breast milk, soy infant formula, or cow's milk formula in their first year. Urinary S-(-)equol and daidzein were quantified by mass spectrometry after a standardized 3.5-day soy isoflavone challenge. Infants were tested at 6, 9, 12, 18, 24, and 36 months of age, and 3-day diet records were obtained at each visit to explore the effect of early and postweaning (>12 months) macronutrient and micronutrient dietary composition and S-(-)equol production. Use of antibiotics was also recorded. At age 6 months, none of the breast-fed infants produced S-(-)equol, whereas 3.8% and 6.0%, respectively, of soy and cow's milk formula-fed infants were equol producers. By age 3 years, 50% of the formula-fed infants were equol producers, compared with 25% of breast-fed infants. Use of antibiotics was prevalent among infants and may have impacted the stability of S-(-)equol production. No significant differences among the groups were observed in postweaning dietary intakes of total energy, carbohydrate, fiber, protein, fat, saturated fatty acids, or polyunsaturated fatty acids and the propensity to make S-(-)equol. In conclusion, S-(-)equol production is developmentally regulated and initially related to diet composition with the proportion of equol producers increasing over the first 3 years of life, with a trend for formula feeding favoring S-(-)equol production.
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Dietary Factors Influence Production of the Soy Isoflavone Metabolite S-(-)Equol in Healthy Adults
The Journal of nutrition, 2013Co-Authors: Kenneth D. R. Setchell, James E Heubi, Nadine M Brown, Suzanne S. Summer, Eileen C. King, Sidney John Cole, Trish Guy, Bevan HokinAbstract:S-(-)equol, an intestinally derived metabolite of the soy isoflavone daidzein, is proposed to enhance the efficacy of soy diets. Adults differ in their ability to produce equol when consuming soy foods for reasons that remain unclear. Therefore, we performed a comprehensive dietary analysis of 143 macro- and micronutrients in 159 healthy adults in the United States (n = 89) and Australia (n = 70) to determine whether the intake of specific nutrients favors equol production. Three-d diet records were collected and analyzed using Nutrition Data System for Research software and S-(-)equol was measured in urine by mass spectrometry. Additionally, in a subset of equol producers and nonproducers (n = 10/group), we examined the long-term stability of equol producer status by retesting 12, 18, and 24 mo later. Finally, the effect of oral administration of the antibiotic metronidazole (500 mg/d for 7 d) on equol production was examined in 5 adults monitored during a 4-mo follow-up period. Equol producers accounted for 30.3% and 28.6% of the United States and Australian participants, respectively (overall frequency, 29.6%). No significant differences were observed for total protein, carbohydrate, fat, saturated fat, or fiber intakes between equol producers and nonproducers. However, principal component analysis revealed differences in several nutrients, including higher intakes of polyunsaturated fatty acids (P = 0.039), maltose (P = 0.02), and vitamins A (P = 0.01) and E (P = 0.035) and a lower intake of total cholesterol (P = 0.010) in equol producers. During a 2-y period, equol producer status remained unchanged in all nonproducers and in 80% of equol producers, whereas metronidazole abolished equol production in only 20% of participants. In conclusion, these findings suggest that major differences in the macronutrient content of the diet appear not to influence equol production, but subtle differences in some nutrients may influence the ability to produce equol, which was a relatively stable phenomenon.
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Impact of perinatal exposure to equol enantiomers on reproductive development in rodents.
Reproductive toxicology (Elmsford N.Y.), 2011Co-Authors: Nadine M Brown, Stephanie L. Lindley, David P. Witte, Kenneth D. R. SetchellAbstract:There is now considerable interest in the intestinally derived soy isoflavone metabolite, equol, which occurs in the enantiomeric forms, S-(−)equol and R-(+)equol, both differing in biological actions. Little is known about effects of either enantiomer on reproductive development, yet such knowledge is fundamental because of the recent commercialization of S-(−)equol as a dietary supplement. S-(−)equol and R-(+)equol were therefore investigated to determine their effects on reproductive development and fertility in the Sprague–Dawley rat. Neither enantiomer affected fertility, number of litters produced, number of pups per litter, number of male and female pups born, birth weight, anogenital distance, testicular descent or vaginal opening. Histological analysis showed no major abnormalities in ovary, testis, prostate or seminal vesicle tissue with dietary exposure to S-(−)equol or R-(+)equol, but both enantiomers triggered hyperplasia of uterine tissue. With R-(+)equol this stimulatory effect subsided after exposure was discontinued, but the effect of S-(−)equol was prolonged.
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Mammary gland differentiation by early life exposure to enantiomers of the soy isoflavone metabolite equol.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 2010Co-Authors: Nadine M Brown, Stephanie L. Lindley, David P. Witte, C.a. Belles, Linda Zimmer-nechemias, Mi-ok Kim, Kenneth D. R. SetchellAbstract:The role of soy in reducing breast cancer risk has been suggested to be associated with early exposure to isoflavones, which alter mammary gland morphology. The objective of the study was to determine the effect of dietary exposure to the enantiomers of a key soy isoflavone metabolite, equol, on mammary gland development and later chemoprotection using the DMBA-induced animal model of breast cancer. Animals were exposed to S-(-)equol or R-(+)equol (250 mg/kg diet) during the neonatal (0-21 days) or prepubertal (21-35 days) periods only. Histological evaluation of the mammary glands showed that both enantiomers fed neonatally via the dam led to significant precocial mammary gland differentiation. By day 50, early S-(-)equol or R-(+)equol exposure resulted in a decrease in immature terminal end structures and an increase in mature lobules, suggesting an early 'imprinting' effect. Despite these morphological changes to the mammary gland, neonatal and prepubertal exposure to equol had no long-term chemoprevention against mammary tumors induced by DMBA, although for R-(+)equol there was a trend to delaying tumor formation. In summary, early exposure to equol was not chemopreventive, but neither did it increase tumor formation in response to DMBA, suggesting exposure in early life does not influence breast cancer risk.
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The chemopreventive action of equol enantiomers in a chemically induced animal model of breast cancer
Carcinogenesis, 2010Co-Authors: Nadine M Brown, Xueheng Zhao, Stephanie L. Lindley, David P. Witte, Linda Zimmer-nechemias, Mi-ok Kim, Carrie A. Belles, Kenneth D. R. SetchellAbstract:We describe for the first time the chemopreventive effects of S-(-)equol and R-(+)equol, diastereoisomers with contrasting affinities for estrogen receptors (ERs). S-(-)equol, a ligand for ERbeta, is an intestinally derived metabolite formed by many humans and by rodents consuming diets containing soy isoflavones. Whether the well-documented chemopreventive effect of a soy diet could be explained by equol's action was unclear because neither diastereoisomers had been tested in animal models of chemoprevention. Sprague-Dawley rats (n = 40-41 per group) were fed a soy-free AIN-93G diet or an AIN-93G diet supplemented with 250 mg/kg of S-(-)equol or R-(+)equol beginning day 35. On day 50, mammary tumors were induced by dimethylbenz[a]anthracene and thereafter, animals were palpated for number and location of tumors. On day 190, animals were killed and mammary tumors were removed and verified by histology, and the degree of invasiveness and differentiation was determined. S-(-)equol and R-(+)equol plasma concentrations measured on days 35, 100 and 190 by tandem mass spectrometry confirmed diet compliance and no biotransformation of either diastereoisomer. In this model, S-(-)equol had no chemopreventive action, nor was it stimulatory. In contrast, R-(+)equol compared with Controls reduced palpable tumors (P = 0.002), resulted in 43% fewer tumors (P = 0.004), increased tumor latency (88.5 versus 66 days, P = 0.003), and tumors were less invasive but showed no difference in pattern grade or mitosis. Both enantiomers had no effect on absolute uterine weight but caused a significant reduction in body weight gain. In conclusion, the novel finding that the unnatural enantiomer, R-(+)equol, was potently chemopreventive warrants investigation of its potential for breast cancer prevention and treatment.
Hubertus Jarry - One of the best experts on this subject based on the ideXlab platform.
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The influence of equol on the hypothalamic–pituitary–thyroid axis and hepatic lipid metabolic parameters in adult male rats
Life Sciences, 2015Co-Authors: Panida Loutchanwoot, Prayook Srivilai, Hubertus JarryAbstract:Abstract Aims Equol, the principal active metabolite of soy-derived phytoestrogen daidzein, has well-known estrogenic actions. Results of several studies indicate that equol may also have anti-androgenic activities. However, mechanisms of action of equol on hypothalamic–pituitary–thyroid axis (HPTA) and hepatic lipid metabolism in adult male rats have not been determined yet. Main methods Equol at two doses of 100 and 250 mg/kg body weight (BW)/day was orally gavaged for 5 days to groups of 4-month-old male rats. As a positive anti-androgenic control group, animals received 100 mg of pure anti-androgenic drug flutamide/kg BW/day. Circulating concentrations of thyroid hormones and lipids, and expression levels of genes underlying HPTA function were determined by radioimmunoassay and TaqMan® real-time reverse transcription polymerase chain reaction, respectively. Key findings Flutamide significantly decreased relative prostate weight, whereas equol did not. Both equol and flutamide caused a significant increase in relative liver weights, and decreases in plasma levels of total tetraiodothyronine (T4) and triiodothyronine (T3), whereas free T4 and T3 concentrations were not reduced. Equol caused the marked down-regulation of hypothalamic thyrotropin-releasing hormone mRNA expression, whereas flutamide did not. Equol as well as flutamide significantly down-regulated the expression levels of pituitary thyrotropin beta-subunit mRNA, without altering thyrotropin secretion. Equol caused reductions in plasma levels of total cholesterol, high- and low-density lipoproteins and triglycerides, whereas flutamide exerted opposite effects. Significance This is the first study to reveal that in male rats equol did not affect HPTA function and liver lipid metabolism through the anti-androgenic pathway, however, the intrinsic estrogenic actions of equol were observed.
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The influence of equol on the hypothalamic-pituitary-thyroid axis and hepatic lipid metabolic parameters in adult male rats.
Life Sciences, 2015Co-Authors: Panida Loutchanwoot, Prayook Srivilai, Hubertus JarryAbstract:Abstract Aims Equol, the principal active metabolite of soy-derived phytoestrogen daidzein, has well-known estrogenic actions. Results of several studies indicate that equol may also have anti-androgenic activities. However, mechanisms of action of equol on hypothalamic–pituitary–thyroid axis (HPTA) and hepatic lipid metabolism in adult male rats have not been determined yet. Main methods Equol at two doses of 100 and 250 mg/kg body weight (BW)/day was orally gavaged for 5 days to groups of 4-month-old male rats. As a positive anti-androgenic control group, animals received 100 mg of pure anti-androgenic drug flutamide/kg BW/day. Circulating concentrations of thyroid hormones and lipids, and expression levels of genes underlying HPTA function were determined by radioimmunoassay and TaqMan® real-time reverse transcription polymerase chain reaction, respectively. Key findings Flutamide significantly decreased relative prostate weight, whereas equol did not. Both equol and flutamide caused a significant increase in relative liver weights, and decreases in plasma levels of total tetraiodothyronine (T4) and triiodothyronine (T3), whereas free T4 and T3 concentrations were not reduced. Equol caused the marked down-regulation of hypothalamic thyrotropin-releasing hormone mRNA expression, whereas flutamide did not. Equol as well as flutamide significantly down-regulated the expression levels of pituitary thyrotropin beta-subunit mRNA, without altering thyrotropin secretion. Equol caused reductions in plasma levels of total cholesterol, high- and low-density lipoproteins and triglycerides, whereas flutamide exerted opposite effects. Significance This is the first study to reveal that in male rats equol did not affect HPTA function and liver lipid metabolism through the anti-androgenic pathway, however, the intrinsic estrogenic actions of equol were observed.
Edwin D. Lephart - One of the best experts on this subject based on the ideXlab platform.
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Resveratrol, 4' Acetoxy Resveratrol, R-equol, Racemic Equol or S-Equol as Cosmeceuticals to Improve Dermal Health.
International journal of molecular sciences, 2017Co-Authors: Edwin D. LephartAbstract:Phytochemicals are botanical compounds used in dermatology applications as cosmeceuticals to improve skin health. Resveratrol and equol are two of the best-known polyphenolic or phytoestrogens having similar chemical structures and some overlapping biological functions to 17β-estradiol. Human skin gene expression was reviewed for 28 different biomarkers when resveratrol, 4′ acetoxy resveratrol (4AR), R-equol, racemic equol or S-Equol were tested. Sirtuin 1 activator (SIRT 1) was stimulated by resveratrol and 4AR only. Resveratrol, R-equol and racemic equol were effective on the aging biomarkers proliferating cell nuclear factor (PCNA), nerve growth factor (NGF), 5α-reductase and the calcium binding proteins S100 A8 and A9. Racemic equol and 4AR displayed among the highest levels for the collagens, elastin and tissue inhibitor of the matrix metalloproteinase 1 (TIMP 1). S-Equol displayed the lowest level of effectiveness compared to the other compounds. The 4AR analog was more effective compared to resveratrol by 1.6-fold. R-equol and racemic equol were almost equal in potency displaying greater inhibition vs. resveratrol or its 4′ analog for the matrix metalloproteinases (MMPs), but among the inflammatory biomarkers, resveratrol, 4AR, R-equol and racemic equol displayed high inhibition. Thus, these cosmeceuticals display promise to improve dermal health; however, further study is warranted to understand how phytochemicals protect/enhance the skin.
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skin aging and oxidative stress equol s anti aging effects via biochemical and molecular mechanisms
Ageing Research Reviews, 2016Co-Authors: Edwin D. LephartAbstract:Oxygen in biology is essential for life. It comes at a cost during normal cellular function, where reactive oxygen species (ROS) are generated by oxidative metabolism. Human skin exposed to solar ultra-violet radiation (UVR) dramatically increases ROS production/oxidative stress. It is important to understand the characteristics of human skin and how chronological (intrinsic) aging and photo-aging (extrinsic aging) occur via the impact of ROS production by cascade signaling pathways. The goal is to oppose or neutralize ROS insults to maintain good dermal health. Botanicals, as active ingredients, represent one of the largest categories used in dermatology and cosmeceuticals to combat skin aging. An emerging botanical is equol, a polyphenolic/isoflavonoid molecule found in plants and food products and via gastrointestinal metabolism from precursor compounds. Introductory sections cover oxygen, free radicals (ROS), oxidative stress, antioxidants, human skin aging, cellular/molecular ROS events in skin, steroid enzymes/receptors/hormonal actions and genetic factors in aging skin. The main focus of this review covers the characteristics of equol (phytoestrogenic, antioxidant and enhancement of extracellular matrix properties) to reduce skin aging along with its anti-aging skin influences via reducing oxidative stress cascade events by a variety of biochemical/molecular actions and mechanisms to enhance human dermal health.
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Protective effects of equol and their polyphenolic isomers against dermal aging: microarray/protein evidence with clinical implications and unique delivery into human skin.
Pharmaceutical biology, 2013Co-Authors: Edwin D. LephartAbstract:AbstractContext: Equol is a polyphenolic/isoflavonoid molecule that can be expressed as isomers. However, the characteristics of the equol isomers on dermal gene/protein expression and human skin percutaneous absorption remain unknown.Objective: Perform a comprehensive investigation on equol as: R-equol, racemic equol or S-Equol to determine their differential expression of skin-related genes, quantify collagen expression and determine percutaneous absorption in human skin.Methods: Quantified: (i) gene expression/mRNA levels via gene array technology using human skin equivalents with equol exposure at 1.2% in qPCR experiments, (ii) in vitro collagen expression in human fibroblasts, and (iii) percutaneous absorption by Franz cell techniques.Results: In the qPCR studies, only three genes displayed the greatest significant expression by S-Equol, whereas 16 genes displayed the greatest significant levels (either stimulation or inhibition) by R-equol and/or racemic equol, such as extracellular matrix proteins ...
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biochemical investigation and gene analysis of equol a plant and soy derived isoflavonoid with antiaging and antioxidant properties with potential human skin applications
Biofactors, 2012Co-Authors: Remona Gopaul, Helen Knaggs, Edwin D. LephartAbstract:The purpose of this study was to investigate the effects of equol, a plant and intestinal flora derived isoflavonoid molecule on the expression of skin genes and proteins using human dermal models. As equol has been shown to mimic 17β-estradiol and bind specifically to 5α-dihydrotestostone (5α-DHT), these agents were used (in addition to equol) to determine whether equol may play important and beneficial roles in the extracellular matrix (ECM). Equol at 0.3 or 1.2% in qPCR experiments using a human skin barrier model examined ECM gene expression. Equol, 5α-DHT, and 17β-estradiol at 10 nM were studied in human monolayer fibroblasts cultures (hMFC) for ECM protein expression. Human fibroblast three-dimensional organotypic cultures revealed equol's influence (@ 10 nM) on ECM proteins via fluorescent-activated cell sorting (FACS) analysis. In qPCR experiments, equol significantly increased collagen, elastin (ELN), and tissue inhibitor of metalloprotease and decreased metalloproteinases (MMPs) gene expression and caused significant positive changes in skin antioxidant and antiaging genes. In hMFC, equol significantly increased collagen type I (COL1A1), whereas, 5α-DHT significantly decreased cell viability that was blocked by equol. FACS analysis showed equol and 17β-estradiol significantly stimulated COL1A1, collagen type III (COL3A1), and ELN while MMPs were significantly decreased compared with control values. Finally, tamoxifen blocked the positive influences of equol on ECM proteins via FACS analysis. These findings suggest that equol has the potential to be used topically for the treatment and prevention of skin aging, by enhancing ECM components in human skin.
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equol an isoflavonoid potential for improved prostate health in vitro and in vivo evidence
Reproductive Biology and Endocrinology, 2011Co-Authors: Trent D Lund, Crystal Blake, Amy Hamaker, Edwin D. LephartAbstract:Background: To determine: in vitro binding affinity of equol for 5alpha-dihydrotestosterone (5alpha-DHT), in vitro effects of equol treatment in human prostate cancer (LNCap) cells, and in vivo effects of equol on rat prostate weight and circulating levels of sex steroid hormones. Methods: First, in vitro equol binding affinity for 5alpha-DHT was determined using 14C5alpha-DHT combined with cold 5alpha-DHT (3.0 nM in all samples). These steroids were incubated with increasing concentrations of equol (02,000 nM) and analyzed by Sephadex LH-20 column chromatography. 14C5alpha-DHT peak/profiles were determined by scintillation counting of column fractions. Using the 14C5alpha-DHT peak (0 nM equol) as a reference standard, a binding curve was generated by quantifying shifts in the 14C5alpha-DHT peaks as equol concentrations increased. Second, equol’s in vitro effects on LNCap cells were determined by culturing cells (48 hours) in the presence of increasing concentrations of dimethyl sulfoxide (DMSO) (vehicle-control), 5alpha-DHT, equol or 5alpha-DHT+equol. Following culture, prostate specific antigen (PSA) levels were quantified via ELISA. Finally, the in vivo effects of equol were tested in sixteen male Long-Evans rats fed a low isoflavone diet. From 190215 days, animals received 0.1cc s.c. injections of either DMSO-control vehicle (n = 8) or 1.0 mg/kg (body weight) of equol (in DMSO) (n = 8). At 215 days, body and prostate weights were recorded, trunk blood was collected and serum assayed for luteinizing hormone (LH), 5alpha-DHT, testosterone and 17beta-estradiol levels. Results: Maximum and half maximal equol binding to 5alpha-DHT occurred at approximately 100 nM and 4.8 nM respectively. LNCap cells cultured in the presence of 5alpha-DHT significantly increased PSA levels. However, in the presence of 5alpha-DHT+equol, equol blocked the significant increases in PSA levels from LNCap cells. In vivo equol treatment significantly decreased rat prostate weights and serum 5alpha-DHT levels but did not alter LH, testosterone, and estradiol levels. Conclusions: Equol administration appears to have potential beneficial effects for prostate health and other 5alpha-DHT mediated disorders. Equol administration: reduces PSA levels from LNCap cells under 5alpha-DHT stimulation, decreases rat prostate size, decreases serum 5alpha-DHT levels and androgen hormone action, while not altering other circulating sex steroids or LH levels.
