DNA profiling, nutritional value and phytochemical investigation of Cissus rotundifolia Lam. growing in Yemen.

Cissus rotundifolia Lam. (Vitaceae) is a wild plant that is commonly used as food and medicine. There are limited studies on the phytochemical composition of this plant. So, this study aims to investigate C. rotundifolia growing in Yemen phytochemically. HPLC analysis of C. rotundifolia aerial parts led to the identification and quantification of four compounds (isoorientin, quercetrin, quercetin, and linarin), among which isoorientin and quercetrin were the major. Proximate analysis showed high fibre content and low moisture content, whereas the nutritional values showed a high carbohydrate content which gave rise to higher nutritional value (266.39 Kcal.). Potassium, calcium, iron, magnesium, and vitamin E were present in high concentrations. Investigation of the methylene chloride and n-butanol fractions lead to the isolation of seven compounds: ß-sitosterol, magnificol, ß-sitosterol-glucoside, quercetin, quercetrin, isoorientin, and linarin. This is the first report on isolating these compounds from the investigated plant.

Efficient Production of Some Bioactive Depsides and Simple Phenolic Acids by Microshoots of Aronia × Prunifolia (Purple Aronia) Agitated Cultures as the Result of Feeding Strategy with Four Different Biogenetic Precursors.

A precursor feeding strategy was used for the first time in agitated microshoot cultures of Aronia × prunifolia. This strategy involved the addition of biogenetic precursors of simple phenolic acids (phenylalanine, cinnamic acid, and benzoic acid) and depsides (caffeic acid) into the culture media, with an assessment of its effect on the production of these bioactive compounds. The in vitro cultures were maintained in Murashige-Skoog medium (1 mg/L BAP and 1 mg/L NAA). Precursors at five concentrations (0.1, 0.5, 1.0, 5.0, and 10.0 mmol/L) were fed into the medium at the time of culture initiation (point "0") and independently on the 10th day of growth cycles. The contents of 23 compounds were determined in methanolic extracts of biomass collected after 20 days of growth cycles using an HPLC method. All extracts contained the same four depsides (chlorogenic, neochlorogenic, rosmarinic, and cryptochlorogenic acids) and the same four simple phenolic acids (protocatechuic, vanillic, caffeic, and syringic acids). Chlorogenic and neochlorogenic acids were the predominant compounds in all extracts (max. 388.39 and 263.54 mg/100 g d.w.). The maximal total contents of all compounds were confirmed after feeding with cinnamic acid (5 mmol/L, point "0") and caffeic acid (10 mmol/L, point "0"), which caused a 2.68-fold and 2.49-fold increase in the contents of the estimated compounds vs. control cultures (603.03 and 558.48 mg/100 g d.w., respectively). The obtained results documented the efficacy of the precursor feeding strategy in enhancing the production of bioactive compounds in agitated cultures of A. × prunifolia and suggest a potential practical application value.

Fermentation of soybeans with Pleurotus cornucopiae and Pleurotus ostreatus increases isoflavone aglycones, total polyphenol content and antioxidant activity.

Edible basidiomycetes are highly active in the oxidative decomposition and polymerisation of polyphenols, and soybeans contain large amounts of isoflavones, which are polyphenol glycosides. Isoflavone aglycones exhibit weak estrogenic activities. In this study, we investigated the isoflavone content, polyphenol production, antioxidant activity and ergothioneine (EGT) content of soybeans fermented by Pleurotus cornucopiae and Pleurotus ostreatus. Isoflavone glycosides, which were abundant in unfermented soybeans, decreased, and aglycones increased on day 10 of culture in both edible basidiomycete-fermented soybeans. The total maximum polyphenol content in soybeans fermented by both mushrooms were approximately 4 times higher on day 30 to 40 of culture, than that of unfermented soybeans. P. cornucopiae-fermented soybeans showed maximum antioxidant activity on day 20 of culture, and this was approximately 6.1 times higher than that of unfermented soybeans. EGT was not detected in unfermented soybeans, whereas both fermented soybeans showed a maximum EGT content on day 20 of culture, which was especially high in P. cornucopiae-fermented soybeans. The antioxidant activity and EGT of P. cornucopiae-fermented soybeans were higher than those of P. ostreatus, suggesting that EGT was responsible for the increase in the antioxidant activity of P. cornucopiae-fermented soybeans.

The Impact of the Inoculation of Different Pied de Cuve on the Chemical and Organoleptic Profiles of Wines.

Controlling the microorganisms involved in alcoholic fermentation during wine production can be achieved by adding a small quantity of spontaneously fermenting must to freshly crushed grapes, a technique known as pied de cuve (PdC). This method not only serves as an inoculation starter but also enhances the microbial footprint unique to each wine region. Recent studies have confirmed that wines inoculated with PdC exhibit efficient fermentation kinetics comparable to those inoculated with commercial strains of Saccharomyces cerevisiae. However, further research is required to draw robust conclusions about the chemical and sensory impacts of PdC-inoculated wines. In this study, we examined the chemical and sensory effects of the PdC technique across three different harvests: Muscat of Alexandria (Spain, harvests 2022 and 2023) and Sauvignon Blanc (Chile, harvest 2023). Each PdC was prepared using various stressors (sulfur dioxide, ethanol, and temperature). Our findings revealed that wines produced with PdC exhibited similar fermentation kinetics and sensory profiles to those inoculated with commercial strains. Notably, PdC fermentations resulted in lower concentrations of acetic acid compared to both the commercial strain and spontaneous fermentations. The sensory analysis indicated that PdC wines significantly differed from those made with commercial strains, with PdC wines displaying more pronounced tropical notes. These results suggest that the PdC technique, particularly when using specific stressors, can maintain desirable fermentation characteristics while enhancing certain sensory attributes, offering a viable alternative to traditional inoculation methods.

Application of a Novel Dissolution Medium with Lipids for In Vitro Simulation of the Postprandial Gastric Content.

Food can change various physiological parameters along the gastrointestinal tract, potentially impacting postprandial drug absorption. It is thus important to consider different in vivo conditions during in vitro studies. Therefore, a novel dissolution medium simulating variable postprandial pH values and lipid concentrations was developed and used in this study. Additionally, by establishing and validating a suitable analytical method, the effects of these parameters on the dissolution of a model drug, cinnarizine, and on its distribution between the lipid and aqueous phases of the medium were studied. Both parameters, pH value and lipid concentration, were shown to influence cinnarizine behavior in the in vitro dissolution studies. The amount of dissolved drug decreased with increasing pH due to cinnarizine's decreasing solubility. At pH values 5 and 7, the higher concentration of lipids in the medium increased drug dissolution, and most of the dissolved drug was distributed in the lipid phase. In all media with a lower pH of 3, dissolution was fast and complete, with a significant amount of drug distributed in the lipid phase. These results are in accordance with the in vivo observed positive food effect on cinnarizine bioavailability described in the literature. The developed medium, with its ability to easily adjust the pH level and lipid concentration, thus offers a promising tool for assessing the effect of co-ingested food on the dissolution kinetics of poorly soluble drugs.

The optimised method of HPLC analysis of glutathione allows to determine the degree of oxidative stress in plant cell culture.

Redox regulations and antioxidant defence play a central role in the acclimation of plants to their environment. Glutathione represents an essential component of the cellular antioxidant defence system, which keeps levels of reactive oxygen species (ROS) under control. High-performance liquid chromatography (HPLC) separation with fluorescence detection is a sensitive method that enables analysis of reduced and oxidised glutathione levels in small samples of plant tissues or plant cell culture. We aimed to optimise the method to obtain more accurate information about the total level of glutathione and the proportion of the reduced form (GSH) by choosing the most suitable reduction reagent and the conditions under which the reduction occurs. The applicability of the developed method was verified by analysing tobacco cells treated with hydrogen peroxide, which caused a decrease in the GSH/total glutathione ratio. Significant changes in the level of glutathione as well as in the GSH/total glutathione ratio were also observed during tobacco cell culture development.

Characterization of Forced Degradation Products of Netarsudil: Optimization and Validation of a Stability-Indicating RP-HPLC Method for Simultaneous Quantification of Process-Related Impurities.

Objectives: The aim of this study is to examine resolution, identification, and characterization of forced degradation products of netarsudil by liquid chromatography-tandem mass spectrometry by validating a simple and sensitive high-performance liquid chromatography method for the resolution, identification, and quantification of two process-related impurities in netarsudil. Materials and Methods: Chromatographic separation was accomplished on a ZORBAX Eclipse XDB C18 (250 x 4.6 mm; 5 µ id) column at room temperature as the stationary phase and 257 nm as the detector wavelength with the mobile phase consisting of acetonitrile, methanol, and pH 4.6 phosphate buffer in 45:35:20 (v/v) at 1.0 mL/min flow rate in isocratic elution. Results: The method reported very sensitive detection limits of 0.008 µg/mL for impurity 1 and 0.003 µg/mL for impurity 1. The method produces a calibration curve linear in the concentration level of 25-200 for netarsudil and 0.025-0.2 µg/mL for impurities. The proposed method gives acceptable results for other validation parameters such as accuracy, precision, ruggedness, and robustness. The drug was subjected to various stress conditions such as acid, base, peroxide, and thermal and ultraviolet light to investigate the stability-indicating ability of the method. Considerable degradation was observed in stress studies, and the degradation products were well resolved from process-related impurities. The characterization of degradation products was performed on the basis of collision-induced dissociation mass spectral data, and the possible structures of the six degradation compounds of netarsudil were proposed. Conclusion: The outcomes of other validation studies were likewise satisfactory and proven adequate for the regular analysis of netarsudil and its process-related impurities in bulk drug and pharmaceutical dosage forms and can also be applied for the evaluation of the stress degradation mechanism of netarsudil.

Spectral and HPLC Analyses of Synthesized Butin and Butein.

Butin and butein are significant bioactive flavanones derived from plants, existing as tautomers of each other. However, their physicochemical attributes, such as their spectral profiles under varying experimental conditions in aqueous solutions and established chromatographic methods for distinguishing between them, remain undetermined. In this study, we determined the basic properties of butin and butein using conventional spectroscopic, reversed-phase, and chiral HPLC analyses. The spectra of the synthesized butin and butein were analyzed using a UV-Vis spectrophotometer in several solvents with different polarities as well as in aqueous solutions at various pH values. Furthermore, the behavior of the measured spectra was reproduced by calculations to reveal the effects of the solvent and pH on the spectra of butin and butein in organic and aqueous solutions. Subsequently, we assessed the structural stability of butin and butein using reversed-phase HPLC, which revealed that butein is unstable compared with butin in a general culture medium. The synthesized butin was effectively separated into R- and S-isomers with positive and negative Cotton effects, respectively, via HPLC using a chiral column. These findings will aid in uncovering the individual properties of both butin and butein that may have been concealed by their tautomerism and enable the synthesis of S-butin, which is typically challenging and time-consuming to isolate.

Hydroxytyrosol permeability comparisons and strategies to improve hydroxytyrosol stability in formulations.

There has been a growing interest in hydroxytyrosol (HT) due to its powerful antioxidant and free-radical scavenging properties when added to formulations such as pharmaceuticals and cosmetics. To study the stability and transdermal properties of hydrogels and creams (HT-based formulations), a high-performance liquid chromatography method was developed for determining HT. In the Franz diffusion cell system, both hydrogel and cream show a rapid and similar penetration profile through the Bama miniature pig skin. However, the Strat-M® membrane exhibits slightly lower permeability and is selective to different formulations; that is, the cream has a permeability value of 10.69%, while the hydrogel has a value of 5.27%. The dynamics parameters from the permeation assays indicate that the model using the Strat-M® membrane can be used as a screening tool to evaluate the skin uptake and permeation efficacy of different formulations. Adding 3-O-ethyl-L-ascorbic acid to HT-based formulations can effectively prevent discoloration under prolonged high-temperature storage, while combining multiple antioxidants delays degradation most effectively. This study provides novel ideas for functional formulation optimization to enhance the realism and reproducibility of cosmetic products containing HT and provides scientific evidence for the production, packaging, shelf life, storage, and transportation of products.

Polyether sulfone flat-sheet membrane impregnated with Mn-Al layered double hydroxide nanoparticles for green microfiltration of acrylamide in cocoa products.

A new polyether sulfone (PES) membrane modified with manganese-aluminum layered double hydroxide (Mn-Al LDH) was prepared and utilized in the membrane micro-solid phase extraction (M-µSPE) of acrylamide for the first time. The analyses were conducted using HPLC-UV. The extraction efficiency of the PES membrane was enhanced two-fold with the addition of LDH. The fabricated LDH@PES was characterized using ATR-FTIR, SEM, XRD, and nitrogen adsorption/desorption isotherms. The specific surface area, average pore diameter, thickness, cross-sectional channels, and LDH particle size of the LDH@PES membrane were determined. The extraction key factors including membrane composition, desorption conditions, sample pH, and salt concentration were studied. The method was validated by determining the limit of detection, the limit of quantification, linear range, r2, matrix effect, enrichment factor, and precision. Extraction recoveries ranged from 87.4 to 103.5% with RSD < 5.9%. Finally, the method's green features were assessed with the AGREE protocol. This is the first report on the application of LDH@PES for microfiltration/extraction of acrylamide in various chocolate and cocoa products.

Valorization of Olive Pomace Using Ultrasound-Assisted Extraction for Application in Active Packaging Films.

Bioactive compounds that can be recovered by the solid wastes of the olive oil sector, such as polyphenols, are known for their significant antioxidant and antimicrobial activities with potential application in nutraceutical, cosmetic, and food industries. Given that industrial demands are growing, and the polyphenol market value is ever increasing, a systematic study on the recovery of natural antioxidant compounds from olive pomace using ultrasound-assisted extraction (UAE) was conducted. Single-factor parameters, i.e., the extraction solvent, time, and solid-to-liquid ratio, were investigated evaluating the total phenolic content (TPC) recovery and the antioxidant activity of the final extract. The acetone-water system (50% v/v, 20 min, 1:20 g mL-1) exhibited the highest total phenolic content recovery (168.8 ± 5.5 mg GAE per g of dry extract). The olive pomace extract (OPE) was further assessed for its antioxidant and antibacterial activities. In DPPH, ABTS, and CUPRAC, OPE exhibited an antioxidant capacity of 413.6 ± 1.9, 162.72 ± 3.36 and 384.9 ± 7.86 mg TE per g of dry extract, respectively. The antibacterial study showed that OPE attained a minimum inhibitory activity (MIC) of 2.5 mg mL-1 against E. coli and 10 mg mL-1 against B. subtilis. Hydroxytyrosol and tyrosol were identified as the major phenolic compounds of OPE. Furthermore, active chitosan-polyvinyl alcohol (CHT/PVA) films were prepared using different OPE loadings (0.01-0.1%, w/v). OPE-enriched films showed a dose-dependent antiradical scavenging activity reaching 85.7 ± 4.6% (ABTS) and inhibition growth up to 81% against B. subtilis compared to the control film. Increased UV light barrier ability was also observed for the films containing OPE. These results indicate that OPE is a valuable source of phenolic compounds with promising biological activities that can be exploited for developing multifunctional food packaging materials.

Biochemical Profiling and Physicochemical and Biological Valorization of Iraqi Honey: A Comprehensive Analysis.

Our study aimed to analyze five monovarietal honeys from the Salah Eddine region in Iraq, focusing on physicochemical, antioxidant, and antimicrobial properties and polyphenolic compounds. Our objective was to evaluate the strengths and qualities of Iraqi honeys, ensuring compliance with the Codex Alimentarius standard for honey. The spectrophotometric analysis included assessments of reduced sugar (75.8-77.7%), fructose-to-glucose ratio (0.7-0.9%), sucrose (2.2-2.9%), HMF (17.23-18.87 mg/kg), and melanoidin content (0.25-0.44), which were all determined. The electrical conductivity (0.39-0.46 mS/cm) using a conductivity meter, pH (4.02-4.31), and mineral composition were determined in all samples using atomic absorption spectrometry. Antioxidant activities were spectrophotometrically determined, through DPPH free radical scavenging (7.87-95.62 mg/mL), as was the total antioxidant activity (14.26-22.15 mg AAE/g), with correlations established with biochemical constituents such as the total phenol content, highlighting the significant presence of Coumaric acid (0.38-2.34 µg/mL), Catechin (1.80-2.68 µg/mL), and Quercetin (0.30 µg/mL) using HPLC. The study also observed notable antimicrobial activities using Escherichia coli, Staphylococcus aureus, and Candida albicans on Mueller-Hinton agar as well as through diffusion technique. In conclusion, our findings, including the antioxidant and antimicrobial strengths, underscore the substantial potential of Iraqi honeys in mitigating damage and preventing the onset of various diseases, affirming their good quality and adherence to international honey standards.

Regional Variations in Peucedanum japonicum Antioxidants and Phytochemicals.

Peucedanum japonicum has long been a staple in East Asian cuisine. In the context of traditional medicine, various members of the Peucedanum genus have been investigated for potential medicinal properties. In laboratory settings, some compounds derived from this plant have shown antioxidant and anti-inflammatory properties-characteristics often associated with potential medicinal applications. This study aimed to determine which part of the P. japonicum plants cultivated on two Korean islands contains the most antioxidant compounds. This determination was made through assessments of total polyphenol content and total flavonoid content, coupled with evaluation of antioxidant activity via DPPH and ABTS assays. The results showed that the aerial parts contain a richer array of bioactive compounds and demonstrate superior antioxidant activity compared to their root counterparts in the plants from both islands. To characterize the phytochemicals underpinning this bioactivity, LC-MS/MS and HPLC analyses were carried out. These methods detected varying amounts of chlorogenic acid, peucedanol 7-O-glucoside, rutin, and peucedanol, with good separation and retention times. This study addresses the lack of research on the antioxidant activity of different parts of P. japonicum. The findings hold significance for traditional medicine, dietary supplements, and the development of functional foods. Understanding antioxidant distribution aids in the development of medicinal and nutritional applications, influences agricultural practices, and contributes to regional biodiversity-conservation efforts. The study's geographical scope provides insights into how location impacts the concentration of bioactive compounds in plants. Overall, the results contribute valuable data for future research in plant biology, biochemistry, and related fields.

Pro-fluorescent probe with morpholine moiety and its reactivity towards selected biological oxidants.

Biological oxidants participate in many processes in the human body. Their excessive production causes organelle damage, which may result in the accumulation of cytotoxic mediators and cell degradation and may manifest itself in various diseases. Peroxynitrite (ONOO- ), hypochlorous acid (HOCl), hydrogen peroxide (H2 O2 ), and peroxymonocarbonate (HOOCO2 - ) are important oxidants in biology, toxicology, and various pathologies. Derivatives of coumarin, containing an oxidant-sensitive boronate group, have been recently developed for the fluorescent detection of inflammatory oxidants. Here, we report the synthesis and characterization of 4-[2-(morpholin-4-yl)-2-oxoethyl]-2-oxo-2H-chromen-7-yl boronic acid (MpC-BA) as a fluorescent probe for the detection of oxidants, with better solubility in water, high stability and fast response time toward peroxynitrite and hypochlorous acid. The effectiveness of the MpC-BA probe for the detection of peroxynitrite was measured by adding bolus ONOO- or using the co-generating superoxide and nitrogen oxide system. MpC-BA is oxidized by ONOO- to 7-hydroxy-4-[2-(morpholin-4-yl)-2-oxoethyl]-2H-chromen-2-one (MpC-OH). However, peroxynitrite-specific product (MpC-H) is formed in the minor reaction pathway. MpC-OH is also yielded in the reaction of MpC-BA with HOCl, and the subsequent formation of a chlorinated MpC-OH gives a specific product for HOCl (MpC-OHCl). H2 O2 slowly oxidizes MpC-BA. However, the addition of NaHCO3 increased the MpC-OH formation rate. We conclude that MpC-BA is potentially an improved fluorescent probe detecting peroxynitrite and hypochlorite in biological settings. Complementation of the fluorescence measurements by HPLC-based identification of chlorinated and reduced coumarin(s) will help identify the oxidants detected.

Vitamin D fortification of selected edible insect species through UVB-treatment.

Edible insects are attracting increased interest worldwide, because they are arguably more sustainable than more established animal foods. Apart from being rich in protein and minerals, they can also form vitamin D3 after treatment with UVB light (290-315 nm). However, only limited research, which has almost exclusively been conducted on living insects, reared under UVB lamps, has been done in this regard. As research on mushrooms has shown, that vitamin D formation is much more effective and less time consuming, when a previously sliced or ground product is treated with UVB light, it would likely be more practical to treat powdered insects with UVB light, rather than rearing them under UVB lamps. Therefore, the aim of this work was to confirm the presence of vitamin D3 in powdered UVB-treated yellow mealworms (Tenebrio molitor), migratory locusts (Locusta migratoria) and two-spotted crickets (Gryllus bimaculatus) as well as to subsequently quantify potential vitamin D content. Samples were analyzed via HPLC, and presence of vitamin D3 was verified via standard addition and spectrum analysis. UVB-treated migratory locusts and two-spotted crickets did not contain quantifiable amounts of vitamin D3. However, UVB-treated mealworms showed substantial amounts of vitamin D3 (8.95-18.24 µg/g dry matter). Thus, the UVB-treatment of powdered mealworm is an effective approach via which to enhance their vitamin D3 content and even modest serving sizes can supply the recommended daily intake of vitamin D.

In vivo toxicity, anti-hyperlipidaemic, antioxidant and anti-atherogenic activities of 'LIPO A' A traditional herbal product in rodents.

Hyperlipidemia accounts for about 17 million deaths worldwide each year. High cost and side effects have limited the use of conventional anti-lipidaemic agents in some cases, majority of whom resort to traditional medicine. The current research focused on validating the safety and efficacy of a herbal product, 'LIPO A' used in the management of hyperlipidaemia. Induction of hyperlipidaemia was achieved by oral administration of 3 mL of cholesterol in coconut oil for 4 weeks in male Sprague Dawley rats with water available as 40 % sucrose. Subsequently, the animals were treated with 100, 200 and 400 mg/kg of the product 'LIPO A' for 4 additional weeks with atorvastatin as reference drug (at 2 mg/kg body weight). Blood samples were taken for serum biochemistry and atherogenic ratios were then calculated. 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) scavenging assay, total antioxidant capacity, physicochemical and phytochemical analysis were also carried out using standard methods. Treatment resulted in a dose-dependent reduction in total cholesterol with maximum reduction of 46.01 % at 400 mg/kg compared to atorvastatin with 49.30 %. There were significant changes in the low-density lipoprotein cholesterol and high-density lipoprotein cholesterol (LDL-c/HDL-c) and Total Cholesterol (TC/HDL-c) ratios which measures the atherogenic and coronary risk indices respectively. Acute and subacute toxicity studies did not reveal any signs of toxicity. High Performance Liquid Chromatography (HPLC) fingerprint revealed six well resolved peaks with two prominent compounds with retention times 24.88 and 23.95 min, which could serve as quality control markers for the product. The herbal product showed considerable antihyperlipidemic and antioxidant actions in rodent models and lend credence to its use in traditional medicine for hyperlipidaemia.

[Use of strongly acting sustained-release opioids in pediatrics : Pitfalls and solutions for morphine and hydromorphone]. / Anwendung stark wirksamer retardierter Opioide in der Pädiatrie : Fallstricke und Lösungen für Morphin und Hydromorphon.

BACKGROUND: In pediatrics, adequate treatment with potent opioids requires the administration of sustained-release preparations for many patients; however, the dosing and administration of sustained-release morphine and hydromorphone preparations via gastrointestinal tubes confronts providers with a major hurdle, especially as the company Mundipharma GmbH has discontinued the production and distribution of the preparation MST retard granules in 2019, which has been proven for these purposes in pediatrics. The aim of this study was to establish a production technique for available sustained-release opioid preparations, which are particularly suitable for use in the low-dose range required in pediatrics and which can also be administered via gastrointestinal tubes. METHOD: Low-dose preparations were produced by opening of morphine and hydromorphone capsules and weighing of the sustained-release pellets. To evaluate the partition, an analysis of the drug content via high performance liquid chromatography (HPLC) was conducted. Moreover, the administration via gastrointestinal tubes (charrière, Ch 8-Ch 10) was examined by an ex vivo experiment. RESULTS: The examination showed a practicable method to produce low dosages of sustained-release morphine and hydromorphone. The preparations are in accordance with the test for content uniformity of the European Pharmacopoeia (Ph. Eur.). Furthermore, the pellets were administered to gastrointestinal tubes Ch 8 (morphine) and Ch 10 (hydromorphone) by a syringe application technique and passed the tubes completely. CONCLUSION: The production technique can be considered as safe and enables the off-label oral application or application via gastrointestinal tubes of sustained-release opioids in pediatrics.

Antiproliferative polyketides from fungus Xylaria cf. Longipes SWUF08-81 in different culture media.

Bioactive compounds from the wood-decay fungus Xylaria cf. longipes SWUF08-81, cultivated in three different culture media (GM, YM and PDB), were isolated. Their structures and stereochemistry were deduced from spectroscopic and MS data analysis, together with quantum chemical calculations of 13C NMR chemical shifts and electronic circular dichroism (ECD) spectra. Five undescribed polyketides including dibenzofuran (1), mellein (2), dihydroisocoumarin (15), and two pyrans (16, 17), together with twenty-three compounds were determined. Compounds 18 and 20 were significantly toxic against cancer cell lines (HCT116, HT29, MCF-7 and HeLa) based on the MTT assay. Quantification by HPLC showed that 18 was produced three-fold higher in the broth of PDB than YM. These studies showed that the production of different compounds were primarily dependent on nutrition sources and it has given a starting point for the growth optimization conditions for the scaling up of bioactive compounds production.

Phytochemical, bactericidal, antioxidant and anti-inflammatory properties of various extracts from Pongamia pinnata and functional groups characterization by FTIR and HPLC analyses.

The present research looked into possible biomedical applications of Pongamia pinnata leaf extract. The first screening of the phytochemical profile showed that the acetone extract had more phytochemicals than the other solvent extracts. These included more saponins, proteins, phenolic compounds, tannins, glycosides, flavonoids, steroids, and sugar. The P. pinnata acetone extract exhibited highest antibacterial activity against C. diphtheriae. The bactericidal activity was found in the following order: C. diphtheria (14 mm) > P. aeruginosa (10 mm) > S. flexneri (9 mm) > S. marcescens (7 mm) > S. typhi (7 mm) > S. epidermidis (7 mm) > S. boydii (6 mm) > S. aureus (3 mm) at 10 mg mL-1 concentration. MIC value of 240 mg mL-1 and MBC is 300 mg mL-1 of concentration with 7 colonies against C. diphtheriae was noticed in acetone extract. Acetone extract of P. pinnata was showed highest percentage of inhibition (87.5 %) at 625 mg mL-1 concentrations by DPPH method. Furthermore, the anti-inflammatory activity showed the fine albumin denaturation as 76% as well as anti-lipoxygenase was found as 61% at 900 mg mL-1 concentrations correspondingly. FT-IR analysis was used to determine the functional groups of compounds with bioactive properties. The qualitative examination of selected plants through HPLC yielded significant peak values determined by intervals through the peak value. In an acetone extract of P. pinnata, 9 functional groups were identified. These findings concluded that the acetone extract has high pharmaceutical value, but more in-vivo research is needed to assess its potential.

Impact of protein deficient diet on the pharmacokinetics of glibenclamide in a model of malnutrition in rats.

Purpose: The present investigation deals with the impact of protein energy malnourished condition on the pharmacokinetic profile of glibenclamide. Protein energy malnourished condition leads to malnutrition related diabetes mellitus (MRDM), Fibrocalculus pancreatic diabetes mellitus (FCPD) or Lean body mass diabetes mellitus (LBMDM). Method: In the present study, malnutrition was developed in female wistar rats using a modified protein deficient diet (0.5%). The experiment was performed on 12 animals, each group containing 6 female wistar rats. The control group animals were fed with standard pellet diet (AIN 93 G diet) while group 2 received the low protein diet (0.5%) for 75 days. Glibenclamide (Gli) suspension (30 mg/kg) was administered orally to these rats on 75 days and kinetic parameters were evaluated by HPLC analysis.The pharmacokinetic interpretation done by pksolver software version 2.0, statistical comparison done by applying student T test. Results: The results of body weight and hematological parameters indicated a significant decreased in the body weight in protein deficit rats to 124.1 ± 6.2 g compared to 235.5 ± 8.4 g (p < 0.01) control rats; whereas a decrease in the hemoglobin to 5.8 ± 0.6 g/dL, total blood protein level to 6.9 ± 0.6 g/dL and blood albumin levels to 2.7 ± 0.4 g/dL in protein deficit rats compared to 15 ± 0.7 g/dL(p < 0.05), 8.1 ± 0.4 g/dL(p < 0.05), and 4.5 ± 0.2 g/dL(p < 0.05), respectively in control rats. All these findings reflect the malnourished condition and weight loss due to a protein deficit diet in experimental animals. There was an increase in the fasting blood glucose levels up to 150 ± 17.4 mg/dL in the protein deficit diet group as compared to 98.7 ± 14.1 mg/dL(p < 0.05) in control rats reflect the prediabetes state in malnourished animals. The results of the pharmacokinetic study reflect a significant lowering of half-life (T½) of glibenclamide to 96.8 ± 0.8 min. in malnourished rats compared to 166.7 ± 0.74 min. (p < 0.001) in control rats. The maximum concentration (Cmax) of glibenclamide in the malnourished rats was significantly higher 20.74 ± 0.65 µg/mL and also took double time i.e. about 180 min. to reach maximum concentration (Tmax) compared to the control rats values 7.9 ± 0.84 µg/mL (p < 0.001) and 90.0 ± 0.24 min. (p < 0.001) respectively. The area under the plasma concentration-time curve [AUC(0-∞)] in malnourished rats increased 4439.1 ± 40.6 µg/ml*min as compared to 1235.9 ± 55.8 µg/ml*min (p < 0.001) in control rats. There was a lowering in the total body clearance (CL) to 0.4 ± 0.02 L/hr and volume of distribution (Vd) to 1.75 ± 0.07 L of glibenclamide in the protein deficit group compared to 1.4 ± 0.3 L/hr (p < 0.001) and 3.14 ± 0.8 L (p < 0.01), respectively in the control rats. Conclusion: From this study it concludes that there is an increase in the T½, Cmax, Tmax and AUC(0-∞) of glibenclamide in malnourished rats while the total body clearance and volume of distribution is lowered. Therefore this study proposes to conduct an adequate pharmacokinetic study in malnourished patients to decide whether the standard glibenclamide dose should be adapted according to the nutritional status of the individual.