Biological effects and phytochemical study of the underground part of Iris scariosa Willd. ex Link extract: A new source of bioactive constituents.

The expected toxicity and resistance of chemotherapeutic agents necessitate and encourage for the use of natural chemotherapeutic sources of plant origin in the clinical stage of cancer therapy. Plants of the genus Iris (Iridaceae) used by local populations for the treatment of cancer, bacterial and viral infections. In this study, an ethanol extract of rhizomes of I. scariosa was prepared and tested for the cytotoxicity using the MTT assay. The extract exhibited the most potent cytotoxicity against the breast cancer cell line MCF7 (IC50 = 9.28 ± 0.49 µg/ml, selectively index ˃5), and induced apoptosis in MCF7 lines. Notably, the extract significantly inhibited the colony formation of MCF7 and HepG2 cancer cells at a concentration range from 10.6 to 85.0 µg/ml, including non-toxic concentrations for HepG2 cells. The ethanol extract was analyzed by HPLC, revealed the identification of 5 secondary metabolites (quercetin, rutin, myricetin, apigenin, artemisetin), the content of which was shown to reach around 15% of the extract. The petroleum ether (PE) part of the extract (yield 2.62%) was analyzed by GC-MS. The composition of tert-butyl methyl ether (TBME) part of the extract (yield 23.72%) was studied. Total of 15 individual compounds: two benzophenones, eight isoflavones, four flavones and a (2R)-flavanone were isolated. The pentamethoxyflavone artemisetin and flavanone pinocembrin were isolated for the first from Iris sp. The readily available isoflavones from the TBME part of extract (irilone, iriflogenin, irigenin and tectorigenin) may serve as new leads for the discovery of anticancer drugs.

Effect of soy isoflavone supplementation on blood pressure: a meta-analysis of randomized controlled trials.

BACKGROUND: Previous experimental studies have suggested that the consumption of soy isoflavones may have a potential impact on lowering blood pressure. Nevertheless, epidemiological studies have presented conflicting outcomes concerning the correlation between soy isoflavone consumption and blood pressure levels. Consequently, a comprehensive meta-analysis of all eligible randomized controlled trials (RCTs) was conducted to explore the influence of soy isoflavones on systolic blood pressure (SBP) and diastolic blood pressure (DBP) in adults. METHODS: A thorough search of PubMed, Embase, and the Cochrane Library for relevant literature up to April 30, 2023 was conducted. RCTs involving adults that compared soy isoflavone supplementation with a placebo (the same matrix devoid of soy isoflavone) were included. The combined effect size was presented as the weighted mean difference (WMD) along with 95% confidence interval (CI), employing a fixed-effects model. RESULTS: Our meta-analysis included a total of 24 studies involving 1945 participants. The results revealed a significant reduction in both SBP and DBP with soy isoflavone supplementation. Subgroup analyses suggested more pronounced reductions in SBP and DBP for interventions lasting ≥6 months, in individuals receiving mixed-type soy isoflavone, and among patients with metabolic syndrome or prehypertension. However, we did not detect significant nonlinear associations between supplementation dosage and intervention duration concerning both SBP and DBP. The overall quality of evidence was deemed moderate. CONCLUSIONS: The current meta-analysis revealed that supplementation with soy isoflavones alone effectively reduces blood pressure. Additional high-quality studies are required to investigate the efficacy of blood pressure reduction through supplementation with an optimal quantity and proportion of soy isoflavone.

Enrichment of milk antioxidant activity by dietary supplementation of red clover isoflavone in cows and its improvement on mice intestinal health.

Red clover (Trifolium pratense) isoflavone was supplemented to dairy cows, and antioxidant capacity of milk was assessed. Treated cows increased the activities of antioxidant enzymes, reduced production of oxidation products, and enhanced the concentrations of vitamin E and vitamin C. Moreover, milk fatty acid profile was positive influenced by 8 g/kg red clover isoflavone, with changes in the lower saturated and higher unsaturated fatty acids. We further demonstrated the efficacy of antioxidant capacity of milk in mice, found that milk from cows feeding red clover isoflavone increased the expressions of antioxidant enzymes, and alleviated lipopolysaccharide (LPS)-stimulated tissue damage of duodenum and jejunum, which was related to upregulated metabolism pathways of carbohydrate, lipid, and amino acid, as well as downregulated inflammatory related pathways. Together, dietary supplementation of red clover isoflavone is an effective way to improve milk antioxidant capacity, providing a natural strategy for developing functional foods.

Soybean Isoflavones Ameliorates Lactation Performance in Postpartum Mice by Alleviating Oxidative Stress and Regulating Gut Microflora.

Postpartum dysgalactiae syndrome (PPDS) is one of the key issues affecting breastfeeding, usually occurring as breast swelling, a low milk yield, and at length a stop of breast milk secretion. Therefore, there is a need to investigate the effectiveness of Traditional Chinese Medicine (TCM) diet therapy in treating or preventing PPDS. This study aims to analyze the effect of soybean isoflavone (SIF), a natural estrogen found in plants, on postpartum lactation performance in mice and to evaluate its potential as a treatment for PPDS. Adult female BALB/c mice at 8 weeks of age (25 ± 3 g) are randomly divided into four groups fed with different levels of SIF and a normal diet for 14 days. SIF (0, 50, 100, 200 mg kg-1 BW) is provided via intra-gastric route to the experimental mice. Using a high-throughput sequencing of microbial diversity and mammary gland metabolites, it is found that SIF-treated mice potentially show an improved milk performance via enhanced antioxidant capacity and altered gut microbiota. SIF from plant sources at a high dosage promotes the lactation in normal postpartum mice.

The effect of different LED wavelengths on the components and biosynthesis of isoflavonoid in sprout Astragalus membranaceus.

An artificial light source is the optimal element for studying the usability of the medicinal plant Astragalus membranaceus as a sprout vegetable. Based on artificial light source conditions, formononetin (FO) level was the highest (2.6 mg/L) in A. membranaceus exposed to white light emitting diode (LED) light, and calycosin (CA) level was the highest (3.09 mg/L) in the plant exposed to red LED light. According to the publicly available transcriptome data of LED-exposed sprout A. membranaceus LED, reference genes related to the content enhancement of FO, an isoflavone compound, and those related to the content enhancement of CA were selected. The expression patterns of these genes were assayed using qPCR. Among the genes related to FO enhancement, Gene-225190T showed the highest mRNA levels in cells of LED-white light-exposed sprout A. membranaceus; among the genes related to CA enhancement, Gene_042770T showed the highest expression under red LED light. Most genes related to the overall biosynthesis regulation of flavonoids of the upper concept of isoflavone were highly expressed in response to red LED light, and the transcriptional level of 4CL in response to red LED light was the highest. Based on these results, the artificial light sources that regulated the FO and CA contents in sprouts A. membranaceus were white and red LED lights, and the selected reference genes were capable of regulating isoflavone biosynthesis.

Bioactive compounds from Retama raetam (Forssk.) Webb & Berthel. and their insecticidal activity against cotton pests Aphis gosspyii and Amrasca biguttula.

Cotton aphids, Aphis gosspyii and cotton jassids, Amrasca biguttula are destructive piercing sucking pests to many strategic crops, especially cotton, not only in Egypt but also all over the world. Using synthetic pesticides to control these pests led to several deleterious impacts. Natural pesticides can be used as a harmless alternative. Nine compounds were isolated from different fractions of Retama raetam using chromatographic techniques and identified by spectroscopic methods as eugenol (1), alpinumisoflavone (2), licoflavone C (3), ephedroidin (4), anagyrine (5), spartiene (6), genistein-8ß-C-glucoside (7), isoprunetin (8) and isoprunetin 7-O-ß-D-glucopyranoside (9). The methanol crude extract and its fractions (hexane, chloroform, ethyl acetate and butanol), as well as the isolated compounds were examined against A. gosspyii and A. biguttula as insecticides. The results showed that chloroform fraction was the most potent fraction against A. gosspyii and A. biguttula, with LC50 values of 65.66 and 64.43 ppm, respectively. As well, compounds 1, 5 and 6 were found to be more active, with LC50 values of 69.84, 25.49 and 27.22 ppm for A. gosspyii and 65.17, 24.07 and 24.78 ppm for A. biguttula, respectively. The most potent compounds (1, 5 and 6) exhibited AChE inhibition toward A. gosspyii compared with the control. So, it can be concluded that the isolated compounds eugenol 1, anagyrine 5 and spartiene 6 are the active principles due to their capability to inhibit AchE activity.

Cheminformatics identification of modulators of key carbohydrate-metabolizing enzymes from C. cujete for type-2 diabetes mellitus intervention.

Purpose: The therapeutic use of oral hypoglycaemic agents in the management of type-2 diabetes mellitus (T2DM) is without adverse effects; thus, calls for alternative and novel candidates from natural products in medicinal plants. Method: The study explored molecular docking and molecular dynamics (MD) simulation approaches to identify key antidiabetic metabolites from Crescentia cujete. Results: Molecular docking results identified four and/or five best compounds against each target enzyme (alpha-glucosidase, dipeptidyl peptidase-IV, aldose reductase, and protein tyrosine phosphatase-1B (PTP-1B)) implicated in diabetes. The resulting complexes (except against PTP-1B) had higher docking scores above respective standards (acarbose, Diprotin A, ranirestat). The MD simulation results revealed compounds such as benzoic acid (-48.414 kcal/mol) and phytol (-45.112 kcal/mol) as well as chlorogenic acid (-42.978 kcal/mol) and naringenin (-31.292 kcal/mol) had higher binding affinities than the standards [acarbose (-28.248 kcal/mol), ranirestat (-21.042 kcal/mol)] against alpha-glucosidase and aldose reductase, respectively while Diprotin A (-45.112 kcal/mol) and ursolic acid (-18.740 kcal/mol) presented superior binding affinities than the compounds [luteolin (-41.957 kcal/mol and naringenin (-16.518 kcal/mol)] against DPP-IV and PTP-1B respectively. Conclusion: While isoflavone (alpha-glucosidase), xylocaine (DPP-IV), luteolin (aldose reductase,) and chlorogenic acid (PTP-1B) were affirmed as the best inhibitors of respective enzyme targets, luteolin, and chlorogenic acid may be suggested and proposed as probable candidates against T2DM and related retinopathy complication based on their structural stability, compactness and affinity for three (DPP-IV, aldose reductase, and PTP-1B) of the four targets investigated. Further studies are warranted in vitro and in vivo on the antihyperglycaemic effects of these drug candidates. Supplementary Information: The online version contains supplementary material available at 10.1007/s40200-023-01249-7.

Long-Term Feeding Soy Protein Concentrates Protect Against Hepatic Steatosis Independent of Isoflavone Levels.

The health benefits of soy foods are attributed to the high-quality protein and the bioactive compounds such as isoflavones. We previously reported that feeding obese (fa/fa) Zucker rats soy protein concentrates (SPCs) with low isoflavone (LIF) and high isoflavone (HIF) for 9 weeks significantly reduced liver steatosis compared to a casein control (C) diet. The current study extended the dietary treatments to 18 weeks to investigate the long-term effect of LIF and HIF SPC diets. 6-week-old male lean (L, n = 21) and obese (O, n = 21) Zucker rats were fed a casein C diet, LIF and HIF SPC diets for 18 weeks and body weight (BW) was recorded twice weekly. Rats were killed after 18 weeks to measure liver steatosis and serum aspartate aminotransferase and alanine aminotransferase. Obese rats had significantly greater final BW, liver weight, liver weight as the percentage of BW, and steatosis score compared to lean rats in all three dietary groups. The obese high-isoflavones (OHIF) group had significantly higher BW compared to obese control (OC) group (P < .0001) and obese low-isoflavones (OLIF) group (P = .01). OC group had significantly greater liver weight, liver weight as the percentage of BW, and liver steatosis score compared to OLIF (P = .0077, P < .0001 and P < .0001, respectively) and OHIF (P = .0094, P < .0001, and P < .0001, respectively) groups. Taken together, long-term feeding of SPC diets protected against liver steatosis regardless of isoflavone levels.

Anti-Menopausal Effect of Soybean Germ Extract and Lactobacillus gasseri in the Ovariectomized Rat Model.

Menopause is a significant phase in a woman's life. Menopausal symptoms can affect overall well-being and quality of life. Conventionally, hormone replacement therapy (HRT) is used to alleviate menopausal symptoms; however, depending on the conditions, HRT may lead to side effects, necessitating the exploration of alternative therapies with fewer side effects. In this study, we investigated the effects of a combination of soybean germ extract (S30) containing 30% (w/w) isoflavone and a probiotic, Lactobacillus gasseri (LGA1), on menopausal conditions in an ovariectomized (OVX) rat model. We evaluated the impact of S30+LGA on body weight, estrogen markers, uterine and bone health, vascular markers, and neurotransmitter levels. The results revealed that treatment with S30+LGA1 significantly improved body weight and uterine and bone health. Moreover, S30+LGA1 demonstrated promising effects on lipid profile, liver function, and vascular markers and positively impacted serotonin and norepinephrine levels, indicating potential mood-enhancing effects. In conclusion, S30+LGA1, possessing anti-menopausal effects in vitro and in vivo, can be recommended as a soy-based diet, which offers various health benefits, especially for menopausal women.

Changes in Nutrient Components and Digestive Enzymatic Inhibition Activities in Soy Leaves by Ethephon Treatment.

In this study, the high isoflavone-enriched soy leaves (IESLs) were manufactured by treating with the chemical inducer ethephon, a plant growth regulator, to confirm changes in the properties of soy leaves (SLs), which are underutilized. Ethephon treatment concentrations consisted of 0 (SL1), 150 (SL2), and 300 (SL3) µg/mL. The composition analysis and physiological activity were conducted according to the ethephon treatment concentration of SLs. There was no significant difference in the proximate composition and fatty acids, except for an increase with increasing ethephon treatment concentrations. Depending on the ethephon treatment concentration, free amino acids increased to 1413.0, 1569.8, and 2100.4 mg/100 g, and water-soluble vitamins increased to 246.7, 244.7, and 501.6 mg/100 g. In particular, the functional substance isoflavone increased significantly to 1430.11, 7806.42, and 14,968.00 µg/g. Through this study, it was confirmed that the nutritional components and isoflavones of SLs increased according to the ethephon treatment concentration, a chemical inducer treatment agent. This can be used as a high-value-added biosubstance for raw materials for functional foods, cosmetics, and for natural drugs.

A Combination of Soy Isoflavone and L-Carnitine Improves Running Endurance in Mice.

The present study aimed to investigate the effect of APIC, a mixture containing soy isoflavone and L-carnitine on running endurance. Male C57BL/6 mice were orally administered APIC for 8 weeks. The APIC group exhibited a significant increase in treadmill running time until exhaustion compared to the control group. The respiratory exchange ratio in the APIC group was lower, indicating an enhancement in fatty acid oxidative metabolism. Furthermore, APIC supplementation increased the proportion of oxidative myofibers. Biochemical parameters associated with endurance capacity were also affected by APIC, as evidenced by increased muscle ATP levels and decreased levels of muscle triglycerides and blood lactate. qPCR and immunoblot analysis of C2C12 myotubes and gastrocnemius muscles indicated that APIC treatment stimulated AMPK signaling, mitochondrial biogenesis, and fatty acid metabolism. Additionally, treatment with APIC led to an increased oxygen consumption rate in C2C12 myotubes. Collectively, these findings suggest that APIC supplementation enhances mitochondrial biogenesis, promotes a switch from glycolytic to oxidative fiber types, and improves fatty acid metabolism through the activation of the AMPK signaling pathway in murine skeletal muscle. Ultimately, these effects contribute to the enhancement of running endurance.

Calycosin inhibits triple-negative breast cancer progression through down-regulation of the novel estrogen receptor-α splice variant ER-α30-mediated PI3K/AKT signaling pathway.

BACKGROUND: Triple-negative breast cancer (TNBC) is a heterogeneous carcinoma characterized by the most aggressive phenotype among all breast cancer subtypes. However, therapeutic options for TNBC patients have limited clinical efficacy due to lack of specific target and efficient targeted therapeutics. AIM: To investigate the biological characteristics of a novel estrogen receptor (ER)-α splice variant ER-α30 in breast cancer cells, and its possible role in the anticancer effects of calycosin, a typical phytoestrogen derived from the herbal plant Astragalus membranaceus, against TNBC. This may also provide a better understanding of the inhibitory activity of calycosin on TNBC progression. METHODS: Breast cancer tissues and para-cancer tissues were collected and analyzed for the expression levels of ER-α30 using immunohistochemistry (IHC), and its expression in two TNBC cell lines (MDA-MB-231 and BT-549) was detected by western blot and qRT-PCR assays. Then the alteration of cell viability, apoptosis, migration, invasion and epithelial-mesenchymal transition (EMT) in response to overexpression or knockdown of ER-α30 was separately determined by CCK-8, Hoechst 33258, wound healing, transwell and western blot assays in two TNBC cell lines. Next, the anticancer effects of calycosin on MDA-MB-231 cells were evaluated through CCK-8, colony formation, flow cytometry, Hoechst 33258 and western blot assays, along with the role of ER-α30 in these effects and the possible downstream targets of ER-α30. In addition, the in vivo experiments were carried out using MDA-MB-231 xenograft model intraperitoneally treated with calycosin. The volume and weight of xenograft tumor were measured to evaluate the in vivo anticancer activities of calycosin, while the corresponding changes of ER-α30 expression in tumor tissues were detected by IHC. RESULTS: It was demonstrated that the novel ER-α splice variant ER-α30 was primarily distributed in the nucleus of TNBC cells. Compared with normal breast tissues, ER-α30 expression was found in significantly higher levels in breast cancer tissues of ER- and progesterone receptor (PR)-negative subtype, so did in TNBC cell lines (MDA-MB-231 and BT-549) when compared to normal breast cell line MCF10A. Moreover, ER-α30 overexpression strikingly enhanced cell viability, migration, invasion and EMT progression and reduced apoptosis in TNBC cells, whereas shRNA-mediated knockdown of ER-α30 revealed the opposite results. Notably, calycosin suppressed the expression of ER-α30 in a dose-dependent manner, accompanied with the inhibition of TNBC growth and metastasis. A similar finding was observed for the xenografts generated from MDA-MB-231 cells. The treatment with calycosin suppressed the tumor growth and decreased ER-α30 expression in tumor tissues. Furthermore, this inhibition by calycosin was more pronounced in ER-α30 knockdown cells. Meanwhile, we found a positive relationship between ER-α30 and the activity of PI3K and AKT, which could also be inactivated by calycosin treatment. CONCLUSION: For the first time, it is demonstrated that the novel estrogen receptor-α splice variant ER-α30 could function as pro-tumorigenic factor in the context of TNBC by participating in cell proliferation, apoptosis, invasion and metastasis, thus it may serve as a potential therapeutic target for TNBC therapy. Calycosin could reduce the activation of ER-α30-mediated PI3K/AKT pathway, thereby inhibited TNBC development and progression, suggesting that calycosin may be a potential therapeutic option for TNBC.

Application of instantaneous nebulization dispersive liquid-phase microextraction combined with HPLC for the determination of chalcone and isoflavone in traditional Chinese medicines.

A simple and rapid instantaneous nebulization dispersive liquid-phase microextraction method was developed, and combined with high-performance liquid chromatography for determination of the contents of seven analytes in traditional Chinese medicines. In this study, using the sprinkler device to achieve instantaneous synchronous dispersion and extraction, only one spray can rapidly achieve the concentration and enrichment of seven kinds of chalcone and isoflavones. The key factors affecting the extraction efficiency were optimized including the type and volume of extractant, the pH and salt concentration of the sample phase, and the number of dispersion. Under the optimal conditions, the enrichment factor of the target analytes ranged from 103.1 to 180.9, with good linearity and correlation coefficients above 0.9970. The limits of detection ranged from 0.02 to 0.15 ng/mL, with good accuracy (recoveries 91.1 to 108.9%) and precision (relative standard deviations 1.5-7.1%). This method has short extraction time (2 s), low organic solvent consumption and high enrichment effect, so it has a wide application prospects.

1-Aminocyclopropane-1-carboxylic Acid Enhances Phytoestrogen Accumulation in Soy Plants (Glycine max L.) by Its Acceleration of the Isoflavone Biosynthetic Pathway.

The low levels of bioactive metabolites in target plants present a bottleneck for the functional food industry. The major disadvantage of soy leaves is their low phytoestrogen content despite the fact that these leaves are an enriched source of flavonols. Our study demonstrated that simple foliar spraying with 1-aminocyclopropane-1-carboxylic acid (ACC) significantly enhanced the phytoestrogen contents of the whole soy plant, including its leaves (27-fold), stalks (3-fold), and roots (4-fold). In particular, ACC continued to accelerate the biosynthesis pathway of isoflavones in the leaves for up to 3 days after treatment, from 580 to 15,439 µg/g. The detailed changes in the levels of this metabolite in soy leaves are disclosed by quantitative and metabolomic analyses based on HPLC and UPLC-ESI-TOF/MS. The PLS-DA score plot, S-plot, and heatmap provide comprehensive evidence to clearly distinguish the effect of ACC treatment. ACC was also proved to activate a series of structural genes (CHS, CHR, CHI, IFS, HID, IF7GT, and IF7MaT) along the isoflavone biosynthesis pathway time-dependently. In particular, ACC oxidase genes were turned on 12 h after ACC treatment, which was rationalized to start activating the synthetic pathway of isoflavones.

Microbial Metabolism of the Soy Isoflavones Daidzein and Genistein in Postmenopausal Women: Human Intervention Study Reveals New Metabotypes.

BACKGROUND: Soy isoflavones belong to the group of phytoestrogens and are associated with beneficial health effects but are also discussed to have adverse effects. Isoflavones are intensively metabolized by the gut microbiota leading to metabolites with altered estrogenic potency. The population is classified into different isoflavone metabotypes based on individual metabolite profiles. So far, this classification was based on the capacity to metabolize daidzein and did not reflect genistein metabolism. We investigated the microbial metabolite profile of isoflavones considering daidzein and genistein. METHODS: Isoflavones and metabolites were quantified in the urine of postmenopausal women receiving a soy isoflavone extract for 12 weeks. Based on these data, women were clustered in different isoflavone metabotypes. Further, the estrogenic potency of these metabotypes was estimated. RESULTS: Based on the excreted urinary amounts of isoflavones and metabolites, the metabolite profiles could be calculated, resulting in 5 metabotypes applying a hierarchical cluster analysis. The metabotypes differed in part strongly regarding their metabolite profile and their estimated estrogenic potency.

In silico molecular docking analysis of three molecules isolated from Litsea guatemalensis Mez on anti-inflammatory receptors.

BACKGROUND: The Litsea genus has four native species from Mesoamerica. Litsea guatemalensis Mez. is a native tree, traditionally used as a condiment and herbal medicine in the region. It has demonstrated antimicrobial, aromatic, anti-inflammatory and antioxidant activity. Bioactive fractionation attributed the anti-inflammatory and anti-hyperalgesic activities to pinocembrin, scopoletin, and 5,7,3´4´-tetrahydroxy-isoflavone. In silico analysis, these molecules were analyzed on receptors involved in the anti-inflammatory process to determine which pathways they interact. OBJECTIVE: To analyze and evaluate 5,7,3',4'-tetrahydroxyisoflavone, pinocembrin, and scopoletin using the in silico analysis against selected receptors involved in the inflammatory pathway. METHOD: Known receptors involved in the anti-inflammatory process found as protein-ligand complex in the Protein Data Bank (PDB) were used as references for each receptor and compared with the molecules of interest. The GOLD-ChemScore function, provided by the software, was used to rank the complexes and visually inspect the overlap between the reference ligand and the poses of the studied metabolites. RESULTS: 53 proteins were evaluated, each one in five conformations minimized by molecular dynamics. The scores obtained for dihydroorotate dehydrogenase were greater than 80 for the three molecules of interest, scores for cyclooxygenase 1 and glucocorticoid receptor were greater than 50, and identified residues with interaction in binding sites overlap with the reference ligands in these receptors. CONCLUSION: The three molecules involved in the anti-inflammatory process of L. guatemalensis show in silico high affinity to the enzyme dihydroorotate dehydrogenase, glucocorticoid receptors and cyclooxygenase-1.

Antidiabetic Effects of Genistein: Mechanism of Action.

Diabetes mellitus is a metabolic disease recognized by abnormal glucose level due to defects in insulin action, insulin secretion, or both. Administration of soybean and isoflavones are accompanied by a lower risk of diabetes. The present review analyzed the previous published papers related to genistein. This isoflavone, which has been used for the prevention of some chronic diseases can inhibit hepatic glucose production, increase ß-cell proliferation, reduce ß-cell apoptosis, and show potential antioxidant and anti-diabetic effects. Therefore, genistein may be useful in the management of diabetes. The beneficial effects of this isoflavone on metabolic syndrome, diabetes, cardiovascular disease, osteoporosis, and cancer have been reported in animal and human studies. Moreover, genistein reduces hepatic glucose production, normalizes hyperglycemia, and gut microbiota and exhibits potential anti-oxidative, anti-apoptotic, and hypolipidemic effects. However, studies on the underlying mechanisms of the action of genistein are very limited. Therefore, the present study reviews multifaceted aspects of genistein to reveal a possible anti-diabetic mechanism of this agent. Genistein by regulating several signaling pathways can be used for the prevention and management of diabetes.

A Study of the Mechanisms and Characteristics of Fluorescence Enhancement for the Detection of Formononetin and Ononin.

In this work, the origins for the spectral difference between two isoflavones, formononetin (F) and ononin (FG), are revealed via a comparison study of the fluorescence molecular structure. The fluorescence enhancement of FG in hot alkaline conditions is reported for the first time. For F, there is almost no fluorescence under acidic conditions, but when the pH is >4.8, its fluorescence begins to increase due to the deprotonation of 7-OH. Under a pH between 9.3 and 12.0, the anionic form of F produces a strong and stable fluorescence. The fluorescence quantum yield (Yf) of F is measured to be 0.042. FG shows only weak fluorescence in aqueous solutions under a wide range of pH until it is placed in hot alkaline solutions, which is attributed to the cleavage reaction of the γ-pyrone ring in FG. The Yf of FG is determined to be 0.020. Based on the fluorescence sensitization methods of F and FG, the quantitative analysis and detection of two substances can be realized. The limit of the detections for F and FG are 2.60 ng·mL-1 and 9.30 ng·mL-1, respectively. The linear detection ranges of F and FG are 11.7~1860 ng·mL-1 and 14.6~2920 ng·mL-1, respectively. Although the structural relationship between F and FG is glycoside and aglycone, under hot alkaline conditions, the final products after the cleavage and hydrolysis reactions are essentially different. The different fluorescence characteristics between F and FG pave a way for further identification and a quantitative analysis of the corresponding components in Chinese herbal medicine.

Feeding Soy Protein Concentrates with Low and High Isoflavones Alters 9 and 18 Weeks Serum Isoflavones and Inflammatory Protein Levels in Lean and Obese Zucker Rats.

Soy's anti-inflammatory properties contribute to the health benefits of soy foods. This study was designed to investigate the bioavailability of soy isoflavones and whether the isoflavone content of soy protein concentrate diet would affect serum inflammatory proteins in an obese (fa/fa) Zucker rat model. Six-week-old male lean (L) and obese (O) Zucker rats were fed a casein control diet (C), soy protein concentrate with low isoflavones (SPC-LIF), or soy protein concentrate with high isoflavones (SPC-HIF) (7 rats/dietary group) before being killed at 9 and 18 weeks. Serum samples were analyzed for isoflavones and inflammatory proteins. At both time points, serum total (aglycone + conjugates) genistein, daidzein, and equol concentrations were significantly higher in L-SPC-HIF and O-SPC-HIF groups compared with L-SPC-LIF and O-SPC-LIF groups, respectively, and were not detectable in either L-C or O-C groups. At week 9, serum C-reactive protein (CRP) concentration was significantly lower in O-SPC-HIF group compared with O-C and O-SPC-LIF group, whereas proteins tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) levels did not differ between any groups. At week 18, serum CRP levels in both O-SPC-HIF and O-SPC-LIF groups were significantly lower compared with the O-C group. TNF-α level was higher in the O-SPC-LIF group compared with both O-C and O-SPC-HIF groups, whereas IL-6 levels were not different between any groups. Taken together, feeding Zucker rats SPC-LIF and SPC-HIF diets led to different serum isoflavone concentrations in both L and O Zucker rats and altered CRP and TNF-α levels in obese Zucker rats compared with controls.

Sophora alopecuroides Alleviates Neuroinflammation and Oxidative Damage of Parkinson's Disease In Vitro and In Vivo.

For centuries, Sophora alopecuroides L. has been used both as a food and an herbal medicine in northern China. A new cytisine-type alkaloid, N-methylene-(5,7,4[Formula: see text]-trihydroxy)-isoflavone (LY01), was found in the fruits of Sophora alopecuroides L. and shows neuroprotective effects against Parkinson's disease (PD). PD is a frequently occurring, irreversible neurodegenerative disease that seriously threatens the health of the elderly population. There is no cure for PD. The available treatments help manage the symptoms, but their use is limited by multiple side effects. Therefore, more pharmacological treatments addressing this pathology are urgently required. This study aimed to evaluate the neuroprotective effects of LY01 against PD, as well as their underlying mechanisms, using both in vitro and in vivo experimental models. A 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine hydrochloride (MPTP)-induced mouse model of PD was used to assess the effects of LY01 on the motor coordination deficit, progression of the pathology, and molecular characteristics. 1-Methyl-4-phenylpyridinium (MPP[Formula: see text])-activated SH-SY5Y cells and lipopolysaccharide (LPS)-activated BV-2 cells were used to evaluate LY01 effects on oxidative damage and neuroinflammation. In the rotarod test, LY01 alleviated the impaired motor coordination in PD mice. Furthermore, LY01 treatment prevented the loss of dopaminergic neurons in the substantia nigra and striatum of the PD mice, reduced neuroinflammation in the mice with MPTP-induced PD and the LPS-activated BV-2 cells, and diminished oxidative stress in the PD mice and the MPP[Formula: see text]-induced SH-SY5Y cells. In conclusion, these results suggest the potential of LY01 as a therapeutic agent for treating PD.