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Soy isoflavones are naturally occurring phytochemicals, which are biotransformed into functional derivatives through oxidative and reductive metabolic pathways of diverse microorganisms. Such representative derivatives, ortho-dihydroxyisoflavones (ODIs) and equols, have attracted great attention for their versatile health benefits since they were found from soybean fermented foods and human intestinal fluids. Recently, scientists in food technology, nutrition and microbiology began to understand their correct biosynthetic pathways and nutraceutical values, and have attempted to produce the valuable bioactive compounds using microbial fermentation and whole-cell/enzyme-based biotransformation. Furthermore, artificial design of microbial catalysts and/or protein engineering of oxidoreductases were also conducted to enhance production efficiency and regioselectivity of products. This minireview summarizes and introduces the past year's studies and recent advances in notable production of ODIs and equols, and provides information on available microbial species and their catalytic performance with perspectives on industrial application.

The phytochemical investigation of Placolobium vietnamense stems led to the isolation of a new isoflavone derivative (1) and three new benzil derivatives (2–4), together with four known pyranoisoflavones (5–8). The structures of all isolated compounds were determined on the basis of extensive spectroscopic analyses, including NMR and HRMS spectral data, as well as comparison of their spectroscopic data with those reported in the literature. The cytotoxicity of all isolated compounds was assessed against the human liver hepatocellular carcinoma (Hep G2) cell line, and compound 1 displayed the most significant cytotoxicity with an IC50 value of 8.0 μM. Furthermore, all isolated compounds were also tested for their inhibitory activity against NO production in RAW 264.7 macrophages. Of these, compound 1 exhibited the strongest inhibitory efficacy against the LPS-induced NO production with the IC50 value of 13.7 μM.

AChE and BuChE are druggable targets for the discovery of anti-Alzheimer’s disease drugs, while dual-inhibition of these two targets seems to be more effective. In this study, we synthesised a series of novel isoflavone derivatives based on our hit compound G from in silico high-throughput screening and then tested their activities by in vitro AChE and BuChE bioassays. Most of the isoflavone derivatives displayed moderate inhibition against both AChE and BuChE. Among them, compound 16 was identified as a potent AChE/BuChE dual-targeted inhibitor (IC50: 4.60 μM for AChE; 5.92 μM for BuChE). Molecular modelling study indicated compound 16 may possess better pharmacokinetic properties, e.g. absorption, blood–brain barrier penetration and CYP2D6 binding. Taken together, our study has identified compound 16 as an excellent lead compound for the treatment of Alzheimer’s disease.

The compound CNI1, identified as a novel antitumor agent based on the cytisine N-isoflavones scaffold, and its series of cytisine N-isoflavones derivatives (CNI2, CNI3, and CNI4), were first isolated from bitter bean seeds, a traditional Chinese medicinal source, by our research team. Cellular activity assays combined with virtual screening targeting P-gp revealed that CNI1, along with the three cytisine N-isoflavones derivatives, CNI2, CNI3, and CNI4, exhibited significant multidrug resistance (MDR) reversal activity in breast cancer. Despite this promising outcome, the precise molecular mechanisms and key targets involved in the MDR reversal of these compounds remain to be elucidated. To explore potential mechanisms, targets for CNI1, CNII2, CNI3, and CNI4 (CNI1-4) were predicted using SwissTargetPrediction and Pharmmapper databases, while MDR-related targets in breast cancer were retrieved from OMIM and GeneCards. The overlapping targets were utilized to construct a protein–protein interaction (PPI) network to identify core targets. Additionally, Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were conducted using the DAVID database to identify relevant signaling pathways. Molecular docking simulations were employed to evaluate the binding sites and energies of CNI1-4 with the identified key targets, with the highest binding energy complexes selected for subsequent molecular dynamics simulations. This study identified 81 intersecting multidrug resistance (MDR) targets and 19 core targets in breast cancer. GO and KEGG pathway enrichment analyses revealed that MDR was primarily mediated by genes involved in cellular processes, apoptosis, protein phosphorylation, as well as the MAPK and PI3K-Akt signaling pathways. Molecular docking studies demonstrated that the binding energies of P-gp, AKT1, and SRC to CNI1-4 were all lower than −10 kcal/mol, indicating strong binding affinities. Molecular dynamics simulations further confirmed the stable and favorable binding interactions of CNI1-4 with AKT1 and P-gp. This study provides preliminary insights into the potential targets and molecular mechanisms of cytisine N-isoflavones compounds in reversing MDR in breast cancer, offering crucial data for the pharmacological investigation of CNI1-4 and supporting the development of P-gp inhibitors.

Transthyretin amyloidosis (ATTR) is a disease caused by the deposition of transthyretin-derived fibrils in the body. Despite extensive research conducted over the years, there are currently only four drugs available in clinical use to treat this condition, two of which are repurposed drugs used off-label. However, these treatments present several limitations; therefore, there is an urgent need for new therapeutic options. In this context, dietary supplements containing natural compounds capable of stabilizing the transthyretin (TTR) protein could represent a promising approach to contrast the disease progression, potentially supporting the therapeutic effects of the aforementioned drugs. In light of this, the present review highlights and analyzes the natural compounds that have most recently been reported in the literature as TTR stabilizers. In particular, the studies elucidating the potential of these compounds in the treatment of ATTR, along with the available crystallographic data explaining their binding mode to TTR, are reported. Overall, although the use of natural compounds as supplements shows promise in managing ATTR, further research is still needed to explore its feasibility and confirm its effectiveness. Hopefully, this work will help shed light on these issues and serve as a useful starting point for the development of new strategies to treat this disease.

The functionality of soybeans is an important factor in the selection and utilization of excellent soybean cultivars, and isoflavones are representative functional substances in soybeans, which exhibit effects on antioxidants, estrogen activity, and cancer, and prevent cardiovascular diseases. This study analyzed ABTS, DPPH, estrogen, ER (ER) alpha, UCP-1, and NO inhibition activities in 48 types of soybean cultivars, as well as the relationship with 19 isolated types of individual isoflavone derivatives. Statistical analysis was conducted to find individual isoflavone derivatives affecting physiological activities, revealing the high correlation of three types of derivatives: genistein 7-O-(6″-O-acetyl)glucoside (6″-O-acetylgenistin), genistein 7-O-(2″-O-apiosyl)glucoside, and glycitein. Based on these results, 15 types of soybean cultivars were selected (one control type, seven yellow types, six black types, and one green type), which have both high physiological activities and a high content of individual isoflavone derivatives. In addition, these high correlations were further verified through a genome-wide association study (GWAS) to determine the association between activities, substances, and genetic characteristics. This study comprehensively describes the relationship between the specific physiological activities of soybean resources, individual isoflavone derivative substances, and SNPs, which will be utilized for in-depth research, such as selection of excellent soybean resources with specific physiological activities.

The aim of this study was to analyze the physiological activity of 48 soybean resources harvested in 2020 to identify the soybean resources’ relationships with individual isoflavone compounds and their genetic properties. These data will subsequently be compared with the research results on soybeans harvested in 2019. Initially, with respect to the physiological activity (6 types) and substances (19 types), this study evaluated the differences between the cultivation year (two years), seed coat color (three colors), and the interaction of the year and seed coat color of soybeans through ANOVA. Among the physiological activities, there were differences in the estrogen, estrogen receptor alpha, and UCP-1 (uncoupling protein-1) activities depending on the cultivation year. Moreover, there were differences in NO (nitric oxide), revealing differences in the ABTS (2, 2′-azino-bis-3ethylbenzo-thiazoline-6-sulfonic acid) and DPPH (2, 2-diphenyl-2-picrylhydrazyl) radical scavenging activities due to the seed coat color and the interaction of the year and seed coat color. Soybeans harvested in 2020 exhibited increased ABTS, DPPH, and NO inhibitory activities and reduced estrogen, estrogen receptor alpha, and UCP-1 activities compared to those harvested in 2019. According to the ANOVA results, eight of the nineteen individual derivatives illustrated yearly differences, while three derivatives displayed differences due to the seed coat color. Secondly, according to the relationship between the efficacy, derivative substances, and genetic properties, it was determined that genistein 7-O-(2″-O-apiosyl)glucoside (F5) is the individual isoflavone derivative that affected the six types of physiological activity, on which the genome-wide association study (GWAS) showed no significant differences for genetic properties. These results were inconsistent with the 2019 data, where three types of individual compounds, including F5, were proposed as substances that correlated with efficacy and there was a high correlation with genetic properties. Therefore, this study selected B17, B23, B15, B24, and Y7 as excellent varieties that are stable and highly functional in the cultivation environment, producing only small annual differences. The results of this study will be utilized as basic data for predicting soybean varieties and their cultivation, which have high environmental stability under climate variation and properly retain the functional substances and efficacy.

Isoflavonoids possess a 3-phenylchroman skeleton and are the biologically active secondary metabolites of various plants that are used for different health promoting and restoring effects through a variety of mechanisms. Chromatographic separation of the n-hexane extract from the stems of Placolobium vietnamense led to the isolation of a new isoflavone derivative, placovinane (1), together with four known compounds (2–5). The structures of isolated compounds were identified from their spectroscopic data and by comparison with the literature. All isolated compounds were evaluated for their α-glucosidase inhibition. They all exhibited potent α-glucosidase inhibition with IC50 values ranging from 11.0 to 87.3 µM, which was significantly less than the positive control acarbose (IC50 179 µM). The cytotoxicity of 1 was evaluated against KB, Hep G2, and MCF7 cell lines, and displayed weak cytotoxicity toward KB and Hep G2 cell lines, with the IC50 values of 89.6 and 93.8 μM, respectively.

Malnutrition is sharply decreased, and over or imbalanced nutrition and lifestyle related disorders are dramatically increased during past two decades globally. Food and medicine arise from the similar origins. In the early era, people experienced sickness, diarrhea, unconsciousness, even death due to ingestion of poisonous plants, while some ailments were alleviated or relieved after eating certain plants. Over time, we have learnt to identify and classify plants based on their characteristic features, as well as developed knowledge about herbal medicines. During the past century, scientists have isolated and identified thousands of compounds from natural sources, and exploited their usage and the relationships between these compounds and their molecular mechanisms. Numerous preparations of natural products are commercially available on the market worldwide. Substantial functional foods and nutraceuticals have been developed such as omega-3 fatty acid, flavonoids and isoflavones, isothiocyanates, carotenoids, dietary fiber, probiotics, prebiotics, phytosterols, polyphenols, alkaloids, terpenoids, saponinoids, polysaccharides, peptides, curcumin, parthenolide, cucurbitacins, 1,8-cineole, pseudopterosins, catechins, capsaicin, conjugated linoleic acid, fucoxanthin, soy isoflavone, glabridin, astaxanthin and cyaniding-3-glucoside, lyprinol, bromelain, marine sponge natural products and Boswellia serrata gum resin etc. They are widely used to adjunctive prevent and treat lifestyle-related continually increasing non-communicable diseases such as diabetes, cardiovascular diseases, cancers, mental disorders, senile dementias, body weight control etc.. However, some functions are need to be confirmed by randomised controlled clinical trial, and detailed mechanism need to be explored.

Daidzein and genistein are two major components of soy isoflavones. They exist abundantly in plants and possess multiple bioactivities. In contrast, ortho-hydroxydaidzein (OHD) and ortho-hydroxygenistein (OHG), including 6-hydroxydaidzein (6-OHD), 8-hydroxydaidzein (8-OHD), 3'-hydroxydaidzein (3'-OHD), 6-hydroxygenistein (6-OHG), 8-hydroxygenistein (8-OHG), and 3'-hydroxygenistein (3'-OHG), are rarely found in plants. Instead, they are usually isolated from fermented soybean foods or microbial fermentation broth feeding with soybean meal. Accordingly, the bioactivity of OHD and OHG has been investigated less compared to that of soy isoflavones. Recently, OHD and OHG were produced by genetically engineering microorganisms through gene cloning of cytochrome P450 (CYP) enzyme systems. This success opens up bioactivity investigation and industrial applications of OHD and OHG in the future. This article reviews isolation of OHD and OHG from non-synthetic sources and production of the compounds by genetically modified microorganisms. Several bioactivities, such as anticancer and antimelanogenesis-related activities, of OHD and OHG, are also discussed.