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Molecules (Basel, Switzerland) Aug 2019Daidzein is a common isoflavone, having multiple biological effects such as anti-inflammation, anti-allergy, and anti-aging. α-Tocopherol is the tocopherol isoform with...
Daidzein is a common isoflavone, having multiple biological effects such as anti-inflammation, anti-allergy, and anti-aging. α-Tocopherol is the tocopherol isoform with the highest vitamin E activity including anti-allergic activity and anti-cancer activity. Hesperetin is a flavone, which shows potent anti-inflammatory effects. These compounds have shortcomings, i.e., water-insolubility and poor absorption after oral administration. The glycosylation of bioactive compounds can enhance their water-solubility, physicochemical stability, intestinal absorption, and biological half-life, and improve their bio- and pharmacological properties. They were transformed by cultured cells to 7-β-glucoside and 7-β-gentiobioside of daidzein, and 3'- and 7-β-glucosides, 3',7-β-diglucoside, and 7-β-gentiobioside of hesperetin. Daidzein and α-tocopherol were glycosylated by galactosylation with β-glucosidase to give 4'- and 7-β-galactosides of daidzein, which were new compounds, and α-tocopherol 6-β-galactoside. These nine glycosides showed higher anti-allergic activity, i.e., inhibitory activity toward histamine release from rat peritoneal mast cells, than their respective aglycones. In addition, these glycosides showed higher tyrosinase inhibitory activity than the corresponding aglycones. Glycosylation of daidzein, α-tocopherol, and hesperetin greatly improved their biological activities.
Topics: Animals; Anti-Allergic Agents; Biocatalysis; Cell Culture Techniques; Cosmetics; Functional Food; Glycosides; Glycosylation; Hesperidin; Humans; Isoflavones; Male; Mast Cells; Monophenol Monooxygenase; Plant Cells; Primary Cell Culture; Rats; Rats, Wistar; Solubility; Nicotiana; alpha-Tocopherol
PubMed: 31426346
DOI: 10.3390/molecules24162975 -
Journal of Medicine and Life Nov 2023Ifosfamide (IFO), an alkylating chemotherapy agent, is known for its association with neurotoxicity and encephalopathy. This trial was designed to evaluate the...
Ifosfamide (IFO), an alkylating chemotherapy agent, is known for its association with neurotoxicity and encephalopathy. This trial was designed to evaluate the protective action of daidzein (DZN) against IFO-induced neurotoxicity in male rats by determining the difference in certain inflammatory and apoptotic markers in the brain tissue of rats. Twenty-eight Wistar rats, weighing 120-150 g, were divided into four groups of seven rats: Group 1 (Control) received no treatment; Group 2 was orally administered DZN (100 mg/kg/day) for seven days; Group 3 received a single intraperitoneal (IP) dose of IFO (500 mg/kg); Group 4 received oral DZN (100 mg/kg/day) for one week prior to a single IP dose of IFO on the seventh day. Twenty-four hours post-treatment, serum and brain tissue samples were collected for analysis. The results indicated a significant increase in serum inflammatory markers (TNF-alpha, IL-6, and iNOS) and the anti-inflammatory marker (IL-10), along with elevated caspase-3 enzyme activity in the brain tissue of the IFO-treated group compared to the control group. Conversely, pre-treatment with DZN significantly reduced serum inflammatory markers and caspase-3 levels in tissue. The findings suggest that daidzein has anti-inflammatory and anti-apoptotic properties, potentially offering protection against IFO-induced neurotoxicity in rats.
Topics: Rats; Male; Animals; Ifosfamide; Rats, Wistar; Neuroprotective Agents; Caspase 3; Antineoplastic Agents, Alkylating; Fanconi Syndrome; Anti-Inflammatory Agents; Isoflavones
PubMed: 38406792
DOI: 10.25122/jml-2023-0082 -
Archives of Microbiology Oct 2019Equol improves menopausal symptoms and it is synthesized from daidzein, one of the isoflavonoids in soybeans, by the bacteria in the large intestines of some people. The...
Equol improves menopausal symptoms and it is synthesized from daidzein, one of the isoflavonoids in soybeans, by the bacteria in the large intestines of some people. The purpose of this study was to isolate equol-producing bacteria using daidzein from the intestinal microflora and to produce equol-containing chungkookjang (short-term fermented soybean). Equol-producing bacteria from the feces of Sprague-Dawley female rats were isolated using media containing daidzein. The isolated bacteria were cultured in thioglycollate media and equol production was identified through thin-layer chromatography and ultraperformance liquid chromatography-mass spectrometry. The bacteria were identified by 16S rRNA sequencing. The rate of equol production in different concentrations of daidzein was assessed. The expression of genes that code for enzymes associated with the production of equol from daidzein was detected through reverse transcription quantitative PCR. The bacterium we isolated was Lactobacillus intestinalis (LC096206.1, 99%). L. intestinalis was found to express daidzein reductase, dihydrodaidzein reductase, and tetrahydrodaidzein reductase, the enzymes involved in producing equol from daidzein. The conversion rate of equol from daidzein was highest (29.5%) using 200 μM daidzein for 48 h of incubation. When chungkookjang fermented with Bacillus amyloquencies SRCM100001 was incubated with L. intestinalis, 0.32 ± 0.04 mg equol/g chungkookjang was produced. In conclusion, L. intestinalis efficiently produces equol from not only daidzein but also in chungkookjang.
Topics: Animals; Bacillus; Equol; Feces; Female; Fermentation; Fermented Foods; Gastrointestinal Microbiome; Humans; Isoflavones; Lactobacillus; Oxidoreductases; Phytoestrogens; RNA, Ribosomal, 16S; Rats; Rats, Sprague-Dawley; Soybean Proteins; Glycine max
PubMed: 31069407
DOI: 10.1007/s00203-019-01665-5 -
Phytomedicine : International Journal... May 2002Daidzein, coumestrol and zearalenone - compounds called phytoestrogens, considered as active biological factors affecting many important physiological and biochemical...
Daidzein, coumestrol and zearalenone - compounds called phytoestrogens, considered as active biological factors affecting many important physiological and biochemical processes appeared to be also significant regulators of adipocyte metabolism. In our experiments the influence of daidzein (0.01, 0.1 and 1 mM), coumestrol (0.001, 0.01 and 0.1 mM), zearalenone (0.01, 0.1 and 1 mM) and estradiol (0.01, 0.1 and 1 mM) on basal and insulin-stimulated (1 nM) lipogenesis from glucose and acetate was tested in adipocytes isolated from growing (160 +/- 5 g b.w) male Wistar rats. All tested compounds significantly attenuated glucose conversion to lipids. In the case of daidzein and coumestrol, this effect was probably due to inhibition of glycolysis. Daidzein (0.01, 0.1 and 1 mM), coumestrol (0.01 and 0.1 mM) and zearalenone (0.01, 0.1 and 1 mM) affected also basal and epinephrine-stimulated (1 microM) lipolysis. Daidzein (0.01 and 1 mM) augmented basal glycerides breakdown in adipocytes. The epinephrine-induced lipolysis was dependent on daidzein concentration and its stimulatory (0.1 mM) or inhibitory (1 mM) influence was observed. Zearalenone changed lipolysis only at the concentration of 1 mM and its effect was contradictory in the absence or presence of epinephrine (the stimulatory or inhibitory effect, respectively). Results obtained in experiments with inhibitors (insulin, 1 nM and H-89, 50 microM) and activators (dibutyryl-cAMP, 1 mM and forskolin, 1 microM) of lipolysis allowed us to assume that daidzein augmented basal lipolysis acting on PKA activity. The inhibitory effect of daidzein and zearalenone on epinephrine-induced lipolysis is probably due to restriction of HSL action. The influence of coumestrol on glycerides breakdown was less marked. Estradiol augmented only epinephrine-stimulated lipolysis.
Topics: Adipocytes; Animals; Coumestrol; Dose-Response Relationship, Drug; Epinephrine; Estradiol; Estrogens, Non-Steroidal; Isoflavones; Lipolysis; Male; Phytoestrogens; Phytotherapy; Plant Preparations; Rats; Rats, Wistar; Zearalenone
PubMed: 12120815
DOI: 10.1078/0944-7113-00148 -
Climacteric : the Journal of the... Feb 2013To determine whether daidzein improves insulin resistance by modifying weight gain, visceral fat accumulation, blood lipids and serum cytokines levels in ovariectomized...
OBJECTIVE
To determine whether daidzein improves insulin resistance by modifying weight gain, visceral fat accumulation, blood lipids and serum cytokines levels in ovariectomized Sprague-Dawley rats.
MATERIALS AND METHODS
Twenty-eight 12-week-old female rats were divided into three groups: the sham-operated group (SHAM) (n =10), the ovariectomized group receiving daidzein therapy (DAID) (n =10), and the ovariectomized control group (Control) (n =8). The rats in the DAID group received 50 mg/kg daidzein via gavage daily. Weight and food intake were recorded every 2 weeks. All of the animals were euthanized 12 weeks after ovariectomy, after which their fasting insulin, glucose, blood lipids, estradiol, interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), adiponectin and leptin levels were measured.
RESULTS
After 12 weeks, the ovariectomized rats demonstrated an increase in their body weight and visceral fat; compared to the SHAM rats, the ovariectomized rats also experienced a significant increase in their serum IL-6 levels and insulin resistance, which was calculated using the homeostatic model assessment of insulin resistance (HOMA-IR) (p <0.05). Daidzein therapy decreased weight gain, visceral fat, the HOMA-IR index and IL-6 levels that were induced by ovariectomy. Rats which had received daidzein therapy had lower levels of TNF-α, leptin and blood lipids (except for high density lipoprotein cholesterol) than the other two groups. IL-6 levels positively correlated with the HOMA-IR index in all of the rats after adjustment for body weight (r =0.495; p =0.016).
CONCLUSION
We conclude that daidzein can improve insulin resistance induced by ovariectomy by decreasing weight gain, visceral fat accumulation, blood lipids, TNF-α, leptin and IL-6 levels.
Topics: Analysis of Variance; Animals; Blood Glucose; Cholesterol, HDL; Cholesterol, LDL; Female; Insulin Resistance; Interleukin-6; Intra-Abdominal Fat; Isoflavones; Leptin; Ovariectomy; Phytoestrogens; Rats; Rats, Sprague-Dawley; Triglycerides; Tumor Necrosis Factor-alpha; Weight Gain
PubMed: 22607577
DOI: 10.3109/13697137.2012.664831 -
Life Sciences Mar 2020The aim of this study was to investigate the inhibition of daidzein or/and regular exercise on breast cancer and to reveal the potential biological mechanisms. BALB/c...
The aim of this study was to investigate the inhibition of daidzein or/and regular exercise on breast cancer and to reveal the potential biological mechanisms. BALB/c mice pretreated with regular exercise training for 20 days (15 m/min, 60 min/d) were orthotopically transplanted with mouse breast cancer cells (4T1), and then treated with daidzein (145 mg/kg) by gavage for another 22 days. Results showed that exercise or daidzein inhibited tumor growth in mice to a different degree. Particularly, co-treatment with exercise and daidzein showed an obviously synergistic inhibition on the tumor growth (P < 0.01), compared with the tumor control. Further researches indicated that the combination of exercise and daidzein synergistically mobilized and redistributed natural killer cells through upregulating the level of epinephrine and interleukin-6. Moreover, exercise combined with daidzein induces apoptosis in cancer cells via Fas/FasL-initiated mitochondrial apoptosis signaling pathway. These results suggested that regular exercise combined with daidzein may explore a candidate way to prevent and treat the breast cancer.
Topics: Animals; Antineoplastic Agents, Phytogenic; Apoptosis; Blotting, Western; Breast Neoplasms; Cell Line, Tumor; Combined Modality Therapy; Exercise Therapy; Female; Flow Cytometry; Isoflavones; Killer Cells, Natural; Mice; Mice, Inbred BALB C; Neoplasm Transplantation
PubMed: 32007575
DOI: 10.1016/j.lfs.2020.117387 -
Osteoporosis International : a Journal... Sep 2010Thyroid C cells hormone, calcitonine, inhibits bone resorption. We have demonstrated that daidzein treatment of orchidectomized rats (model for osteoporosis) stimulated...
SUMMARY
Thyroid C cells hormone, calcitonine, inhibits bone resorption. We have demonstrated that daidzein treatment of orchidectomized rats (model for osteoporosis) stimulated C cells and increased trabecular bone mass. These results suggest that, besides direct action, daidzein may also affect bone structure indirectly through enhancement of thyroid C cell activity.
INTRODUCTION
Thyroid C cells produce calcitonin (CT) which acts as an inhibitor of bone resorption. In this study, the influence of daidzein treatment on thyroid C cells, bone structure, and bone function in orchidectomized (Orx) middle-aged rats was investigated.
METHODS
Sixteen-month-old Wistar rats were divided into Orx and sham-operated (SO) groups. Half the Orx rats were given subcutaneous injections of daidzein (30 mg/kg b.w./day) for 3 weeks. CT-immunopositive thyroid C cells were morphometrically analyzed. The metaphyseal region of the proximal tibia was measured histomorphometrically, and cancellous bone area (B.Ar), trabecular thickness (Tb.Th), trabecular number (Tb.N), and trabecular separation (Tb.Sp) were calculated. Serum samples were analyzed for CT and osteocalcin (OC), calcium (Ca) and phosphorus concentrations, and urine samples for Ca levels.
RESULTS
Treatment of Orx animals with daidzein significantly increased volume of C cells compared to the Orx rats. Daidzein also enhanced B.Ar, Tb.Th, and Tb.N and reduced Tb.Sp. The serum OC and urinary Ca concentrations decreased significantly in comparison with the Orx group.
CONCLUSIONS
These findings indicate that daidzein treatment stimulates thyroid C cells, increase trabecular bone mass, and decrease bone turnover in Orx middle-aged rats, which is the model of male osteoporosis.
Topics: Animals; Biomarkers; Bone Density Conservation Agents; Calcitonin; Disease Models, Animal; Drug Evaluation, Preclinical; Isoflavones; Male; Orchiectomy; Osteoporosis; Rats; Rats, Wistar; Thyroid Gland; Tibia
PubMed: 19859640
DOI: 10.1007/s00198-009-1092-x -
European Journal of Pharmacology Mar 2010Daidzein, a phytoestrogen, has been reported to produce vasodilation via inhibition of Ca(2+) inflow. However, the involvement of large-conductance Ca(2+)-activated K(+)...
Daidzein, a phytoestrogen, has been reported to produce vasodilation via inhibition of Ca(2+) inflow. However, the involvement of large-conductance Ca(2+)-activated K(+) (BK(Ca)) channels in the effect of daidzein is debated. Therefore, the present study was designed to investigate the effect of daidzein on the rat cerebral basilar artery and the underlying molecular mechanisms. Isolated cerebral basilar artery rings and single vascular smooth muscle cells (VSMCs) were used for vascular reactivity and electrophysiology measurements, to investigate the effect of daidzein on BK(Ca) channels in cerebral basilar artery smooth muscle. In addition, the human BK(Ca) channel alpha-subunit gene (hslo) was transfected into HEK293 cells, to directly assess whether daidzein activates BK(Ca) channels. The results showed that daidzein produced a concentration-dependent but endothelium-independent relaxation in rat cerebral basilar arteries. Paxilline, a selective BK(Ca) channel blocker, significantly inhibited the daidzein-induced vasodilation, whereas NS1619, a selective BK(Ca) channel opener, enhanced the vasodilation. In the whole-cell configuration, daidzein increased noisy oscillation currents in cerebral basilar artery VSMCs in a concentration-dependent manner, and washout of daidzein or blockade of BK(Ca) channels with paxilline fully reversed the increase. However, daidzein did not substantially affect hSlo currents in HEK293 cells when applied to the outside of the cell membrane. In conclusion, these results indicate that the activation of BK(Ca) channels in VSMCs at least partly contributes to the daidzein-induced vasodilation of the rat cerebral basilar artery. The beta1-subunit of BK(Ca) channels plays a critical role in the activation of BK(Ca) currents by daidzein.
Topics: Animals; Basilar Artery; Cerebral Arteries; Dose-Response Relationship, Drug; Electrophysiology; Isoflavones; Male; Muscle, Smooth, Vascular; Patch-Clamp Techniques; Phytoestrogens; Potassium Channels, Calcium-Activated; Rats; Rats, Sprague-Dawley; Vasodilation
PubMed: 20044987
DOI: 10.1016/j.ejphar.2009.12.032 -
Molecular Medicine Reports Dec 2016Isoflavone is a type of phytoestrogen that exists in soy‑based products. Previous studies have reported that certain foods containing isoflavones, particularly infant...
Isoflavone is a type of phytoestrogen that exists in soy‑based products. Previous studies have reported that certain foods containing isoflavones, particularly infant formula, may have potential adverse effects on male reproductive function. However, few studies have focused on the effects of isoflavones on testosterone biosynthesis and Sertoli cell function during the neonatal period. The aim of the present study was to investigate the influence of daidzein, a common isoflavone, on testosterone secretion and Sertoli cell function during the neonatal period. The organ culture method was used to assess the effects of daidzein on neonatal mouse testes. Cultured testes were treated with daidzein (0, 0.03, 0.3, 3 or 30 µmol/l) for 72 h. To verify the mechanism of action of daidzein on androgen production, Leydig cells were also treated with daidzein for 24 h. As anticipated, testosterone secretions were suppressed by daidzein (30 µmol/l) in cultured testes and Leydig cells. Further analysis demonstrated that the expression levels of steroidogenic acute regulatory protein (StAR), cholesterol side‑chain cleavage enzyme (P450scc) and 3β‑hydroxysteroid dehydrogenase (3β‑HSD), which are transport proteins and key enzymes in androgen biosynthesis, were suppressed in cultured neonatal mouse testes. In addition, the expression levels of StAR, P450scc, 3β‑HSD and 17α‑hydroxylase/20‑lyase were decreased in Leydig cells. Notably, proliferation of Sertoli cells was also inhibited by daidzein (30 µmol/l). Furthermore, the expression levels of vimentin were significantly suppressed in the testes following treatment with daidzein, whereas inhibin B expression exhibited no change. In conclusion, daidzein may suppress steroidogenic capability and impair Sertoli cell function in the neonatal period in vitro.
Topics: Animals; Animals, Newborn; Cell Survival; Cells, Cultured; Gene Expression Regulation; Gene Expression Regulation, Enzymologic; Isoflavones; Leydig Cells; Male; Mice; Sertoli Cells; Testis; Testosterone
PubMed: 27840926
DOI: 10.3892/mmr.2016.5896 -
Biochimie Aug 2014Pulmonary fibrosis (PF) is a progressive lethal disorder. In this study, the effect of daidzein, a soyisoflavone against Bleomycin (BLM) induced PF in rats was...
Daidzein exhibits anti-fibrotic effect by reducing the expressions of Proteinase activated receptor 2 and TGFβ1/smad mediated inflammation and apoptosis in Bleomycin-induced experimental pulmonary fibrosis.
Pulmonary fibrosis (PF) is a progressive lethal disorder. In this study, the effect of daidzein, a soyisoflavone against Bleomycin (BLM) induced PF in rats was elucidated. A single intratracheal instillation of BLM (3 U/kg.bw) was administered in rats to induce PF. Daidzein (0.2 mg/kg) was administered subcutaneously, twice a week for a period of 28 days. Daidzein restored the histological alteration and aberrant collagen deposition, suppressed the mast cells, and reduced the expressions of Cyclooxygenase 2 (COX2) and Nuclear factor kappa B (Nf-kB) in lung tissue of BLM-induced rats. Treatment with daidzein reduced the expression of Matrix metalloproteinase 2 (MMP-2) and increased the expression of Tissue inhibitor of matrixmetalloproteinases 1 (TIMP 1). Recently, Proteinase activated receptor 2 (PAR2) has been reported to play a major role in the progression of PF. Confocal microscopic and immunoblot analysis revealed that BLM injured rat lungs exhibited increased expression of PAR2 that was reduced upon treatment with daidzein. During BLM induction, Transforming growth factor beta (TGFβ1) was found to be up-regulated along with p-smad2/3, a mediator of TGFβ signaling. Further, daidzein regulated the apoptosis by modulating the expressions of Bcl-2, Bax and caspase 3. This study provides evidence on the anti-fibrotic role of daidzein in BLM-induced experimental fibrosis.
Topics: Animals; Apoptosis; Bleomycin; Collagen; Gene Expression Regulation; Inflammation; Isoflavones; Male; Matrix Metalloproteinase 2; Pulmonary Fibrosis; Rats; Receptor, PAR-2; Smad Proteins; Tissue Inhibitor of Metalloproteinase-1; Transforming Growth Factor beta1
PubMed: 24769130
DOI: 10.1016/j.biochi.2014.04.005