Profile Of Compounds Research Articles

Determining the impact of pre-pressing pretreatments applied to sugarcane on the aroma compounds and quality characteristics of sugarcane juice.

The study examined the effects of three pretreatments, blanching (5, 10, and 30min), ultrasound (15, 20, and 30min), and steam blanching (10, 20, and 30min) on sugarcane, assessing their impact on sugarcane juice quality parameters and aroma compounds. The control had the highest soluble solid content, while the ultrasound-15min (US-15min)-treated sample had the lowest, affecting pH, total acidity, and color values significantly. Color analysis showed lower L* values and less greenish tones in treated samples. The implemented pretreatments effectively reduce the browning index, with the US-20min treatment showing the most significant reduction compared to the control sample. All pretreatments deactivated polyphenol oxidase. Carbon isotope analysis yielded significant results. Principal component analysis and hierarchical clustering linked 1,1-diphenyl-2-picrylhydrazyl (DPPH) with 2,2'-azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and 5-hydroxymethyl furfural (HMF) with total phenolic content. The study also highlights significant variations in aroma compound profiles among pretreated sugarcane juice samples, with blanching for 10 min showing notable increases in specific compounds like 2-heptanone and nonanol. Hierarchical clustering showed similarities between blanching-30min and US-30min, contrasting with the control. Blanching-10min had a positive impact on sugarcane juice quality. In conclusion, the study emphasized how pretreatments affect physicochemical properties and aroma compounds in sugarcane juice. PRACTICAL APPLICATION: The research findings suggest that blanching and ultrasound pretreatments can be used by the food industry to improve sugarcane juice quality by reducing browning, enhancing color, and altering aroma profiles. These pretreatments could extend the shelf life and appeal of sugarcane juice, making it more attractive to consumers while maintaining its nutritional properties.

Evaluation of in vivo pharmacokinetic study of the anti-cancer drug imatinib using silkworms as an animal model.

Imatinib is an oral molecular targeted therapy that acts as a tyrosine kinase inhibitor. Silkworms present a promising experimental model for elucidating the pharmacokinetic and toxicity profiles of various compounds. This study aimed to establish an experimental paradigm for investigating the pharmacokinetics of imatinib in silkworms. A comparative analysis of imatinib pharmacokinetic parameters across silkworms, humans, mice, and rats revealed similarities in time to maximum concentration (Tmax) and apparent clearance values between silkworms and humans. However, differences in elimination half-life (t1/2) and apparent volume of distribution between silkworms and humans remained within 5- and 4-fold ranges, respectively. Importantly, mice demonstrated pharmacokinetic parameters closer to those of humans than rats during imatinib studies. Additionally, silkworms and mice exhibit similar Tmax and t1/2 values. This study highlights the potential of silkworms as valuable tools for investigating imatinib metabolism in pharmacokinetic studies. Furthermore, it underscores the applicability of silkworms in elucidating the pharmacokinetic parameters of various molecular-targeted drugs, thus facilitating advancements in drug development and evaluation.

Study of phenolic compounds of umbellate wintergreen herb and their influence on biochemical indicators of blood and urine in the rat model of chronic kidney disease

Diseases of the kidneys and urinary tract are a common problem in people of all ages. Kidneys filter blood, removing water-soluble waste from the body, maintain water-salt balance, stabilize blood pressure and PH level. Intoxication, hypothermia, injuries and other causes lead to problems with the kidneys - inflammatory disease, urolithiasis, etc. Therefore, the development of effective herbal remedies that affect the etiopathogenic factors of diseases is urgent. The aim. Study of the profile of phenolic compounds of umbellate wintergreen, study of antioxidant and nephroprotective properties of umbellate wintergreen extract on the model of chromate-induced renal failure (chronic kidney disease) in rats. Materials and methods. Phenolic compounds were analyzed by high-performance liquid chromatography (HPLC) using a Waters e2695 Alliance HPLC system in combination with a 2998 PDA detector (Waters, Milford, MA, USA). Study of in vitro antioxidant activity by HPLC method for 50 % extract of umbellate wintergreen herb. A Waters 2695 chromatograph (Waters, USA) equipped with a Waters 996 diode-matrix detector was used. To determine the nephroprotective effect, 60 outbred sexually mature rats (males), divided into six groups, were studied. Based on the results of biochemical studies, creatinine clearance and urea clearance were calculated in experimental animals. Results. 8 phenolic compounds - apigenin, hyperoside, quercitrin, rutin, quercetin, gallic acid, guaiaverine and isoquercetin - were identified and quantified in umbellate wintergreen by HPLC. Based on the results of a preliminary assessment of the antioxidant contribution of individual phenolic compounds to the overall effectiveness of the umbellate wintergreen grass extract, a significant effect of caffeic acid derivatives and quercetin was determined. The use of Chimaphila umbellata extract in experimental animals was marked by the normalization of diuresis, a decrease in the total protein content of urine by 1.8 times. The effect of the use of umbellate wintergreen extract was expected to be dose dependent. Conclusions. The profile of umbellate wintergreen phenolic compounds was investigated by HPLC, and their antioxidant effect was determined. In the conditions of the development of renal failure in rats, the studied extract of Chimaphila umbellata improved the physical condition of the animals, reduced their mortality, improved the excretory function of the kidneys, normalized nitrogen and protein metabolism, contributed to the protection of the structure of the kidney tissue, and therefore had a positive effect on the course of nephropathy

Phenolic profile, antioxidant capacity and oxidoreductase enzyme activity in autochthonous grape varieties from Bosnia and Herzegovina

The variability of phenolic compounds among grape varieties has an important role in selecting winemaking techniques, but the use of phenolic profiles for quality control is still fragmented and incomplete. Given the recent climate change and global warming, biochemical characterisation of secondary metabolites in autochthonous grape varieties is a very important factor for their preservation and sustainable agriculture. Two autochthonous grape varieties from the western Herzegovina region in Bosnia and Herzegovina have been selected for the research targeting at the evaluation of their phenolic profiles, antioxidant activities, and the correlation with oxidoreductase enzymes polyphenol oxidase and Class III peroxidase, in different berry tissues. The obtained results indicate a similar qualitative profile of phenolic compounds in exocarp and mesocarp in both varieties, but their concentrations and antioxidant activity vary significantly. The correlation between phenolic compounds and oxidoreductase enzyme activities in different grape berry tissues is discussed in this article.

LC-MS/MS phenolic profileand remedial role ofUrtica dioica extract against Li2CO3-induced toxicity.

In this study, the protective role of Urtica dioica extract (Udex) against Li2CO3 toxicity in Allium cepa L. was investigated using various parameters such as germination rates, root growth, weight gain, mitotic index (MI), malondialdehyde (MDA), micronucleus (MN), antioxidant enzyme activity, chromosomal abnormalities (CAs) and anatomical changes. As the biological activity of Udex is related to its active content, the profile of phenolic compounds was determined by LC-MS/MS analysis. Li2CO3 caused abnormalities in the tested parameters and serious regressions in germination parameters. Application of 100mg/L Li2CO3 reduced the chlorophyll a and b contents by 73.04% and 65.7%, respectively. Li2CO3 application exhibited a cytotoxic effect by inducing significant decreases in MI and increases in the frequency of MN, and also showed a genotoxic effect by causing CAs. After 100mg/L Li2CO3 treatment, MDA, proline, superoxide dismutase, and catalase levels increased by 54.9%, 58.5%, 47.8%, and 52.3%, respectively. Li2CO3 and Udex co-administration resulted in a regression in increased biochemical parameters and genotoxicity parameters, and an improvement in germination parameters. Furthermore, Udex demonstrated efficacy in mitigating the detrimental effects of Li2CO3 on the root tip, particularly in the 200µg/mL Udex-treated group. The thickening of the cortex cell wall and conduction tissue, which is commonly induced by Li₂CO₃, was not observed in the Udex-treated group. The protective effect of Udex can be explained by the phenolic compounds it contains. Rutin was detected as the major component in Udex and other phenolics were listed according to their presence rate as protecatechuic acid > caffeic acid > p-coumaric acid > syringic acid > rosemarinic acid > epicatechin. Li ions, which increase in the environment after industrialization, are an important environmental pollutant and exhibit toxicity that affects many pathways in organisms. Scientific research should not only detect these toxic effects but also develop solutions to such problems. In this study, it was determined that the Udex application had a toxicity-reducing role against Li2CO3 toxicity. Also, it has been demonstrated that A. cepa is an important indicator in determining this toxicity and toxicity-reducing applications.

Selected Soluble Dietary Fibres as Replacers of Octenyl Succinic Anhydride (OSA) Starch in Spray-Drying Production of Linseed Oil Powders Applied to Apple Juice

The aim of the study was to compare two kinds of soluble dietary fibres in a mixture with OSA-starch as wall components of linseed oil capsules. Comparison was made based on emulsion (droplet size, polydispersity index, and viscosity) and powder properties (outer structure, colour, surface oil content, and encapsulation efficiency). Additionally, linseed oil powders were applied to the food model (apple juice) and the colour, physical stability, and volatile compound profile of fortified juice were determined. Although the obtained linseed oil emulsions with different compositions of polysaccharide components showed some variation in droplet size, polydisperse index and viscosity, their encapsulation efficiency by spray-drying was very high (>98%). The powders produced had a similar structure and low surface oil content, and their 2% addition to apple juice did not change its stability and only slightly decreased its colour lightness and yellowness. However, greater differences in the volatile compounds of obtained juices were observed. Overall, the added powders reduced the volatility of aroma compounds typical of apple juice but introduced propanal and hexanal, especially the powders with the highest OSA-starch share.

O,S,Se-containing Biginelli products based on cyclic β-ketosulfone and their postfunctionalization.

A one-pot three-component Biginelli synthesis of dihydropyrimidinones/thiones/selenones via acetic acid or solvent-free Yb(OTf)3-catalyzed tandem reaction of β-ketosulfone (dihydro-2H-thiopyran-3(4H)-one-1,1-dioxide), an appropriate urea, and arylaldehyde has been developed. The reaction proceeds with high chemo- and regioselectivity to give diverse DHPMs in reasonable yields up to 95%. Moreover, an SO2-containing analogue of anticancer drug-candidate enastron (SO2 vs C=O) was obtained by using the here reported method in gram scale. We also demonstrate the reactivity of the Biginelli product in various directions - synthesis of condensed thiazoles and tetrazoles. In silico assessment of ADMET parameters shows that most compounds meet the lead-likeness requirements. The biological profiles of new compounds demonstrate high probability levels of activity against the following pathogens/diseases: Candida albicans, Alphis gossypii, Tripomastigote Chagas, Tcruzi amastigota, Tcruzi epimastigota, Leishmania amazonensis, and Dengue larvicida.

Investigation of the effects of psyllium powder addition on the quality of fresh and frozen gluten-free bread

The interest in gluten-free (GF) products has been growing since both the increase in prevalence of celiac disease and the preferences of GF diet. In this study, the contribution of psyllium powder (PP) to gluten-free (GF) bread quality, dough rheology and volatile compounds (VCs) profile was investigated throughout the frozen storage period of GF dough (-30 °C for 0, 7, 15, and 30 days). GF doughs containing 7.5% PP (PSY1) and 15% PP (PSY2) had lower tanδ value than GF control dough (p<0.05) according to the results obtained from fundamental rheological analysis. Frozen storage caused no effect on the tanδ value of PSY1 and PSY2 (p ≥ 0.05). PP addition increased the specific volume (SV) of GF breads (p<0.05). No significant effect of frozen storage on SV was shown for PSY2 while SV values of GF control bread (GFB) and PSY1 decreased (p<0.05). Lower crumb hardness was shown for PSY1 and PSY2 on day 0. Significant effect of frozen storage on crumb hardness was observed for PSY1 on day 30 while harder crumb structure was shown for GFB throughout the frozen storage (p<0.05). Psyllium addition led to a significant reduction in both L* value of crust and crumb color (p<0.05). In the VCs analysis performed by HS/GC-MS, ethanol and 1-butanol, 3-methyl from alcohol group, butanal, 3-methyl- and hexanal from aldehydes were common for GFB and GF breads containing psyllium. 1-butanol, 3-methyl-, butanal, 3-methyl- and hexanal were the VCs of PSY1 and they were also shown after frozen storage. This study suggested that quality deterioration due to frozen storage was less in gluten-free breads containing psyllium.

Role of different oils and cooking materials on chemical compounds and antioxidant properties of garlic

This study determined the effects of cooking Taşköprü garlic, which is grown with a geographical indication in Turkiye, in three cooking materials (unbleached parchment paper (UP), bleached parchment paper (BP), and oven bag (OB)) and four vegetable oils (sunflower oil (SO), hazelnut oil (HO), corn oil (CO), and olive oil (OO)) on total phenolic content, antioxidant activity, phenolic compound profile, and chemical compound profile. The effects of cooking material (CM) and oil type (OT) on garlic samples’ TPC were found to be insignificant (p > 0.05). However, cooking material (CM) and oil type (OT) impacted antioxidant activity. According to cooking material, statistically, the highest antioxidant activity with the DPPH method was identified in garlic cooked using UP and BP, while the highest antioxidant activity with the ABTS method was found in garlic cooked with BP and OB. The garlic samples roasted with the mentioned oils and cooking materials were analyzed by LC-MS/MS in terms of thirty-five phenolic compounds. However, only five of these compounds (quinic acid, fumaric acid, hesperidin, ferulic acid, and rosmarinic acid) were detected in the samples. The chemical components of the cooked garlic samples primarily consist of terpenoids (β–sitosterol and squalene). The use of cooking material affected the amount of squalene compound in all garlic samples cooked with olive oil. Among these samples, the lowest squalene rate (52.11%) was found in only roasted garlic. In addition, according to GC-MS results, we can say that the use of hazelnut oil and unbleached parchment paper in the roasting process has a protective effect on the cis-vaccenic acid compound, which is known to show anticancer properties.Graphical

Exploring the Bioactive Potential of Moroccan Lemon Grass (Cymbopogon citratus L.): Investigations on Molecular Weight Distribution and Antioxidant and Antimicrobial Potentials.

Research on lemon grass (Cymbopogon citratus L.) revealed a variety of active molecules and examined their biological characteristics. However, most of these studies were conducted on wild varieties, while cultivated plants were addressed less. This study aimed to characterize the biomolecules and biological activities of lemon grass growing under North African conditions in Morocco. Phenolic compound profiles of aqueous (AE), ethanol (EE), and methanol (ME) extracts and their fractions were obtained with steric exclusion chromatography on Sephadex G50 gel and identified by LC-MS/MS. Then, total polyphenols (TPC), flavonoids (TFC), and antioxidant activities (FRAP: scavenging value and TAC: Total Antioxidant Capacity) of the fraction were evaluated, as well as the antimicrobial activity. The obtained results showed that the ME contained eight major compounds (i.e., apigenine-7-O-rutinoside and myricitine-3-O-rutinoside). The AE showed the presence of five molecules (i.e., kaempferol-3-O-glucuronide), while EE showed the presence of three molecules (i.e., quercetine-3-O-rutinoside). Regarding the chemical characterization, the highest value of total phenolic content (TPC) was obtained in AE (25) (4.60 ± 0.29 mg/g), and the highest value of total flavonoid content (TFC) was obtained in ME (29) (0.7 ± 0.08 mg/g). Concerning the antioxidant activity, the highest FRAP was obtained in ME (29) (97.89%), and the highest total antioxidant capacity (TAC) was obtained in ME (29) (89.89%). Correlation between FRAP, TPC, and TFC was noted only in fractions of AE and ME. All tested extracts of C. citratus and their fractions showed a significant antimicrobial effect. The lowest minimum inhibitory concentration (MIC) was recorded for ME against E. coli. Extracts' biological activities and their fractions were governed by their active molecules. These data are new and clarify a novel aspect of bioactive molecules in the extracts of cultivated C. citratus. Equally, throughout this research, we clarified the relationship between identified molecules and their biological properties, including antioxidant and anti-microbial activities, which is new for the study area. This study is suggested as a reference for comparative studies and other assays of other biological activities for the study plant.

Chemical profiling and probiotic viability assessment in Gueuze-style beer: Fermentation dynamics, metabolite and sensory characterization, and in vitro digestion resistance

Probiotic viability, metabolite concentrations, physicochemical parameters, and volatile compounds were characterized in Gueuze beers formulated with probiotic lactic acid bacteria (LAB) and yeast. Additionally, the sensory profile of the beers and the resistance of the probiotics to digestion were determined. The use of 2 International Bitterness Units resulted in high concentrations of probiotic LAB but a decline in probiotic yeast as pH decreased. Secondary fermentation led to the consumption of maltose, citric acid, and malic acid, and the production of lactic and propionic acids. Carbonation and storage at 4 °C had minimal impact on probiotic viability. The addition of probiotic LAB resulted in a distinct aroma profile with improved sensory characteristics. Our results demonstrate that sour beers produced with probiotic LAB and a probiotic yeast, and fermented using a two-step fermentation process, exhibited optimal physicochemical parameters, discriminant volatile compound profiles, promising sensory characteristics, and high probiotic concentrations after digestion.

The Effect of Phytogenic Additive in Broiler's Diet on Production Results, Physicochemical Parameters, and the Composition of Volatile Organic Compounds of Broiler Meat Assessed by an Electronic Nose System.

The primary objective of this study was to investigate the impact of a phytogenic additive (PA) in broiler chickens' diet on production, physiochemical parameters, and the profile of volatile organic compounds present in broiler chickens' meat. The experiment was conducted in a commercial chicken house, where Ross 308 broiler chickens were divided into two groups, each consisting of 65,000 broilers. One group was fed a diet supplemented with 100 ppm of PA throughout the rearing period. The primary chemical composition of the meat and its physicochemical parameters were determined. A visual assessment of breast muscles for defects and volatile organic compounds were evaluated using an electronic nose system. No statistically significant differences were shown in the production performance of the chickens; while summarizing all production parameters, a higher EPEF index of 31 points in the experimental group was highlighted. Breast muscle quality showed differences in drip loss and WHC (p ≤ 0.01) in favor of the experimental group, and a lower cutting force value (p ≤ 0.05) was found for breast muscles from the experimental group. The group also had a lower proportion of muscles with a white striping defect, and the results of volatile organic compound profiling showed the most aroma units.

Lacticaseibacillus casei as Anti-blowing Agents: Impact on the Evolution of Ripening and Sensory Profile of Montasio Cheese

AbstractRecently, the Lacticaseibacillus casei group strains have been gaining growing interest due to their potential to be used as secondary adjunct cultures in cheese. This work aimed to test autochthonous Lb. casei strains as anti-blowing agents and to evaluate their impact on the evolution of the ripening and the sensory profile of Montasio cheese. The cheesemaking trial included a control production without lysozyme (C1), a control with lysozyme (C2), and four experimental productions, each containing a different pool of autochthonous Lb. casei strains (EX1-4). Samples were taken during ripening, and physicochemical, microbiological, and sensory analyses were carried out. Lb. casei counts indicate that the selected strains survived the cheesemaking and maintained their viability of about 9 log cfu g−1 at the end of the ripening. Only EX3 showed a significant slowdown of the proteolytic index compared to controls over time. Furthermore, from the principal component analysis, it emerged that at the end of the 120-day-long ripening, C2 and the experimental samples were characterized by similar profiles of volatile compounds. The late-blowing defect (LBD) was observed exclusively in C1, whereas it was not detected in the control sample with lysozyme or in any experimental samples. These findings not only confirmed the efficacy of lysozyme in preventing LBD but also supported the effectiveness of the selected Lb. casei strains as anti-blowing agents with the ability to contribute to the final volatile profile without compromising the typicality of the product.

Improving natto quality through Co-fermentation of functionally complementary Bacillus and Lactiplantibacillus species

Natto, a nutritious fermented soybean product, is known for its health benefits. Modern production methods use Bacillus subtilis as the starter culture to ensure consistent quality. However, this method overlooks the potential positive effects of other microbial species present in traditionally, naturally fermented natto. This study explored the effects of ARTP-induced mutants of B. subtilis var. natto and several strains of lactic acid bacteria (LAB) on natto quality. The results showed that these two types of bacteria have complementary roles in fermentation. B. subtilis var. natto, with enhanced extracellular protease activity, promotes the hydrolysis of soy protein and enhances the product's ACE inhibitory and fibrinolytic activities. Meanwhile, two strains of Lactiplantibacillus plantarum reduced the content of total volatile basic nitrogen (TVB-N) while increasing the content of folic acid in the final product. In addition, B. subtilis var. natto and LAB produce different profiles of volatile compounds (VOCs). Subsequently, B. subtilis var. natto and Lpb. plantarum were used to co-ferment natto in different ratios. The results showed that the two types of bacteria could co-colonize and enhance fermentation quality through their respective strengths. Specifically, Lpb. plantarum strains co-metabolized with B. subtilis var. natto to elevate the content of pyrazines, characteristic VOCs in natto. The optimal quality of natto was achieved when Lpb. plantarum HIS6, Lpb. plantarum LP3 and B. subtilis var. natto Y15-11 were combined in a 2:1:2 ratio. This study not only identified effective combinations of starter cultures with complementary benefits but also elucidated the metabolic pathways of key volatile compounds. Our findings also provide technical insights for improving natto quality, enhancing consumer acceptance, and supporting industrial production.

Effects of unconventional non-Saccharomyces yeast fermentation on the chemical profile and bioaccessibility of watermelon wine

This study evaluated effects of watermelon fermentation using different non-Saccharomyces yeast strains (Brettanomyces lambicus, Brettanomyces bruxellensis, and Lachancea thermotolerans) on the chemical profile of the derived wines. A control product was produced using Saccharomyces cerevisiae. Analytical techniques, namely HPLC-DAD-RID and LLE-GC/MS, were used to evaluate sugars, organic acids, alcohols, phenolic compounds, amino acids, and volatile compounds profiles. Fermentation reduced the sugar (glucose and fructose) and amino acid contents and increased alcohol (ethanol and glycerol), organic acids (lactic and acetic acids), phenolics, and volatile compounds. The use of the B. bruxellensis strain resulted in an alcoholic beverage with quality parameters similar to that from S. cerevisiae but with higher concentrations of phenolics (rutin, gallic acid, caftaric acid, and caffeic acid) and important volatile compounds (isoamyl acetate). The watermelon wine had a higher content of bioaccessible phenolic compounds than the must, especially catechin, procyanidin B1, procyanidin B2 and gallic acid, due to their high bioaccessibility (>70%). The yeast type influenced the chemical profile of the beverages. B. bruxellensis is a promising tool to obtain watermelon alcoholic beverage in an industrial scale.

Influence of Ultrasonication and UV-C Processing on the Functional Characteristics and Anticarcinogenic Activity of Blackthorn Vinegar.

In recent years, consumer trends have been changing toward fresh food products such as fruit juice, vinegar, etc. that are a good source of bioactive components, high nutritional characteristics, and beneficial microorganisms. Blackthorn (Prunus spinosa L.) vinegar (BV) is one of these nutritious foods. The study aims to examine the efficacy of ultraviolet-C (UV-C) light applied by a modified reactor and ultrasonication on bioactive compounds (total phenolic, total flavonoid, ascorbic acid content, and antioxidant activity) of traditionally produced BV. Furthermore, the volatile organic compound (VOC) profile, hydroxymethylfurfural (HMF) content, cytotoxicity properties, and color were assessed. UV-C light and ultrasonication processes enriched most bioactive components, but these methods did not significantly improve ascorbic acid (p > 0.05) compared to pasteurization. Twenty-seven volatile compounds were analyzed in order to determine the VOC profile. As a result, thermal and nonthermal methods were found to affect the profile significantly (p < 0.05). No significant differences were detected in total soluble solids (4.70-4.77), titratable acidity (3.81-3.87), and pH (3.39-3.41) values. The anticarcinogenic activities of UV-C-treated BVs were more significant than others. Nonthermal treatments were generally better than pasteurization in maintaining and enriching the quality of BV. In this study, UV-C light and ultrasonication technology can be used as an alternative to traditional thermal techniques to improve the quality of BV.

Effects of Berberis vulgaris, and its active constituent berberine on cytochrome P450: a review.

The cytochrome P450 (CYP450) family is crucial for metabolizing drugs and natural substances. Numerous compounds, such as pharmaceuticals and dietary items, can influence CYP activity by either enhancing or inhibiting these enzymes, potentially leading to interactions between drugs or between drugs and food. This research explores the impact of barberry and its primary component "berberine" on key human CYP450 enzymes.The text discusses the effects of this plant on the 12 primary human CYP450 enzymes, with summarized data presented in tables. Berberine exerts an influence on the function of various CYP450 isoforms, including CYP3A4/5, CYP2D6, CYP2C9, CYP2E1, CYP1A1/2, and most isoforms within the CYP2B subfamily. Given the significant role of these CYP450 isoforms in metabolizing commonly used drugs and endogenous substances, as well as activating procarcinogens into carcinogenic metabolites, the influence of barberry and its active constituent on these enzymes may impact the pharmacokinetics and toxicity profiles of various compounds. More specifically, regarding the crucial role of CYP2D6 and CYP3A4 in metabolizing clinically used drugs, and the inhibitory effects of berberine on these two CYP450 isoforms, it seems that the most important drug interaction of berberine that should be considered is related to its inhibitory effect on CYP2D6 and CYP3A4.In conclusion, due to the impact of barberry on multiple CYP450 isoforms, healthcare providers should conduct thorough consultations and investigations to ensure patient safety and prevent any potential adverse interactions before recommending the consumption of these herbs. Additional research, particularly clinical trials is crucial for preventing any potentially adverse interactions in patients who consume this herb.

Effect of ultrasound assisted extraction and simulated in vitro gastrointestinal digestion on phenolic compound profile, bio-accessibility, and LC-ESI-QTOF-MS analysis of black beans (Phaseolus vulgaris L.) extract

Effect of ultrasound assisted extraction and simulated in vitro gastrointestinal digestion on phenolic compound profile, bio-accessibility, and LC-ESI-QTOF-MS analysis of black beans (Phaseolus vulgaris L.) extract

Discovery of Indolo[3,2-c]isoquinoline Derivatives as Novel Top1/2 Dual Inhibitors with Orally Efficacious Antitumor Activity and Low Toxicity.

Topoisomerase (Top) inhibitors used in clinical cancer treatments are limited because of their toxicity and severe side effects. Noteworthily, Top1/2 dual inhibitors overcome the compensatory effect between Top1 and 2 inhibitors to exhibit stronger antitumor efficacies. In this study, a series of indolo[3,2-c]isoquinoline derivatives were designed as Top1/2 dual inhibitors possessing apparent antiproliferative activities. Mechanistic studies indicated that the optimal compounds 23 and 31 with increasing reactive oxygen species levels damage DNA, inducing both cancer cell apoptosis and cycle arrest. Importantly, the results of the toxicity studies showed that compounds 23 and 31 possessed good oral safety profiles. In xenograft models, compound 23 exhibited remarkable antitumor potency, which was superior to the clinical Top inhibitors irinotecan and etoposide. Overall, this work highlights the therapeutic potential and safety profile of compound 23 as a Top1/2 dual inhibitor in tumor therapy and provides valuable lead compounds for further development of Top inhibitors.

Synthesis and Optimization of Small Molecule Inhibitors of Prostate Specific Antigen.

Semen liquefaction is a postejaculation process that transforms semen from a gel-like (coagulated) form to a water-like consistency (liquefied). This process is primarily regulated by serine proteases from the prostate gland, most prominently, prostate-specific antigen (PSA; KLK3). Inhibiting PSA activity has the potential to impede liquefaction of human semen, presenting a promising target for nonhormonal contraception in the female reproductive tract. This study employed triazole B1 as a starting compound. Through systematic design, synthesis, and optimization, we identified compound 20 (CDD-3290) as a 216 nM inhibitor of PSA with better stability in media than triazole B1. Further, we also evaluated the selectivity profile of compound 20 (CDD-3290) by testing against closely related proteases and demonstrated excellent inhibition of PSA versus α-chymotrypsin and elastase and similar potency versus thrombin. Thus, compound 20 is an improved PSA inhibitor that can be tested for efficacy in vitro or in the female reproductive tract.