Pharmaceutical Ingredients Research Articles

Photoprotective Effect of Taurine-Rich Protamex Extract From Salmon (Oncorhynchus keta) Byproduct Against Ultraviolet B-Induced Skin Damagein Human Dermal Fibroblasts and Zebrafish Model.

Exposure to ultraviolet (UV) light promotes reactive oxygen species (ROS) production and metalloproteinase (MMP) 1 expression, leading to skin damage. Several studies have reported that protein-rich fish byproducts from enzymatic hydrolysis exhibited a variety of health benefits such as antioxidant and anti-inflammation. In the current study, we investigated the protective effect of protein hydrolysate from salmon byproduct (SBPH) in ultraviolet B (UVB)-irradiated human dermal fibroblasts (HDFs) and zebrafish. Antioxidant activities of SBPH were evaluated by the oxidative radical scavenging assay. To determine the cytotoxicity of SBPH, the CCK-8 assay was performed. The protective effects of SBPH against photodamage was evaluated by DCF-DA, ELISA, and western blotting analysis in UVB-induced invitro and invivo model. SBPH significantly increased cell proliferation and suppressed UVB-induced intracellular ROS generation and MMP-1 expression by regulating activator protein 1 (AP-1) and mitogen-activated protein kinases (MAPKs) signaling pathways in HDF cells. In addition, SBPH reduced the expression of proinflammatory cytokines and alleviated the inflammatory response via suppressing nitric oxide synthase (NOS) and cyclooxygenase 2 (COX2). Moreover, UVB-induced abnormal homeostasis in HDF cells was remarkably improved via the downregulation of cell cycle regulatory proteins including p53 and p21. Furthermore, the invivo photoprotective effect was determined by reducing the level of ROS in the UVB-induced zebrafish model. These results demonstrate that SBPH possesses strong protective effects against UVB and may serve as a potential ingredient in pharmaceuticals and cosmeceuticals.

An extensive analysis of isoindigotin derivatives as effective corrosion inhibitors for mild steel in acidic corrosive environments: An electrochemical and theoretical investigation

Isoindigo and its derivatives are frequently employed as active ingredients in pharmaceuticals and in solar cells, largely due to their distinctive structural characteristics, which render them a green substance. The utilization of its polymers as efficacious corrosion inhibitors for the safeguarding of mild steel exhibits considerable promise. In order to achieve this, a green and highly efficient isoindigo polymer (E)-7-(9,9-bis(3-(dimethylamino) propyl)-9H-fluoren-2-yl)-1,1′-bis(3-(dimethylamino) propyl)-[3,3′-biindolinylidene]-2,2′-dione (PIIDN-FN) was synthesized using a simple one-step polymerization reaction and subsequently employed as a corrosion inhibitor for the first time. In this work, its ability to inhibit the corrosion of Q235 when added to 1 M HCl medium was the subject of corresponding electrochemical tests and surface analyses (including SEM, AFM and XPS etc.). The results implied that PIIDN-FN was able to achieve a maximum inhibition efficiency of 94.52 % at a concentration of 100 mg L−1, and the inhibition efficiency was still close to 90 % even at a high temperature of 328.15 K. Moreover, the PDP results indicated that PIIDN-FN is a hybrid corrosion inhibitor, and it was determined that the adsorption of the material onto the carbon steel surface conformed to the Langmuir isotherm model. Furthermore, quantum chemical calculations (QC) based on density functional theory (DFT) and molecular dynamics simulations (MD) facilitated the elucidation of the inhibition mechanism. The findings of the theoretical investigation suggest that PIIDN-FN adsorbs as a film on the surface of mild steel due to its conjugated structure, forming a complex with iron and thereby providing effective protection for carbon steel.

Application of vegetable oils as pharmaceutical ingredient: the impact of liquid lipid type on the characteristics of nanostructured lipid carrier

Recently, drug encapsulation using a Nanostructured Lipid Carrier (NLC) has gained attention in formulation studies due to its high loading capacity and prevent drug expulsion during storage. Drug loading capacity is mainly affected by lipid type and composition, especially liquid lipids. Therefore, this research aims to evaluate the potential of avocado oil as a liquid lipid of NLC replacing pure oleic acid. All components including oil, glyceryl monostearate, Tween 20®, and Span 60® were processed to NLC by solvent injection method. The colloidal characteristics of NLC dispersion in water and 20 mM PBS pH 7 were determined, including transmittance, particle size, size distribution, zeta potential, loading capacity (LC), and loading efficiency (LE) of capsanthin in NLC. The results showed that NLC containing oleic acid (Fola) and avocado oil (Favo) dispersion in PBS exhibited a similar transmittance and zeta potential of 69-74% and -51 to -58 mV, respectively, whereas the particle size and size distribution of Favo were significantly higher than Fola. Moreover, the 1.3-fold higher LC and LE of Favo compared to Fola was insignificant (p>0.05). Additionally, the Tween 20® and Span 60® ratio of Favo should be improved to obtain an ideal particle size and size distribution as in Fola. In conclusion, avocado oil indicated the potential to be utilized as a liquid lipid of NLC formulation regarding zeta potential and drug loading. However, the surfactant composition should be adjusted to reduce the particle size of the NLC, leading to permeability enhancement in delivery, particularly oral administration.

Repurposing of drug candidates against Epstein-Barr virus: Virtual screening, docking computations, molecular dynamics, and quantum mechanical study.

Epstein-Barr virus (EBV) was the first tumor virus identified in humans, and it is mostly linked to lymphomas and cancers of epithelial cells. Nevertheless, there is no FDA-licensed drug feasible for this ubiquitous EBV viral contagion. EBNA1 (Epstein-Barr nuclear antigen 1) plays several roles in the replication and transcriptional of latent gene expression of the EBV, making it an attractive druggable target for the treatment of EBV-related malignancies. The present study targets EBV viral reactivation and upkeep by inhibiting EBNA1 utilizing a drug-repurposing strategy. To hunt novel EBNA1 inhibitors, a SuperDRUG2 database (> 4,600 pharmaceutical ingredients) was virtually screened utilizing docking computations. In accordance with the estimated docking scores, the most promising drug candidates then underwent MDS (molecular dynamics simulations). Besides, the MM-GBSA approach was applied to estimate the binding affinities between the identified drug candidates and EBNA1. On the basis of MM-GBSA//200 ns MDS, bezitramide (SD000308), glyburide (SD001170), glisentide (SD001159), and glimepiride (SD001156) unveiled greater binding affinities towards EBNA1 compared to KWG, a reference inhibitor, with ΔGbinding values of -44.3, -44.0, -41.7, -40.2, and -32.4 kcal/mol, respectively. Per-residue decomposition analysis demonstrated that LYS477, ASN519, and LYS586 significantly interacted with the identified drug candidates within the EBNA1 binding pocket. Post-dynamic analyses also demonstrated high constancy of the identified drug candidates in complex with EBNA1 throughout 200 ns MDS. Ultimately, electrostatic potential and frontier molecular orbitals analyses were performed to estimate the chemical reactivity of the identified EBNA1 inhibitors. Considering the current outcomes, this study would be an adequate linchpin for forthcoming research associated with the inhibition of EBNA1; however, experimental assays are required to inspect the efficiency of these candidates.

Tobacco stalk nanofibrillated cellulose: An eco-friendly binder on fluidized bed granulation

The search for new excipients that provide formulation alternatives over existing ones and that are derived from natural resources has advanced over the years. Emerging from this scenario, an important alternative to traditional excipients is nanofibrillated cellulose (NFC), which is generally obtained from agricultural wastes and is a cellulose-rich material. Most of the time, the nanofibers are presented in aqueous dispersions that form a highly entangled network of fibrous particles that exhibit gel-like behavior. Therefore, the present work aimed to explore the gel-like behavior of NFC from tobacco stalks to evaluate it as a binder in a fluid bed granulation process for further application as a pharmaceutical ingredient. The granulation process was carried out using top spray mode with an inlet air temperature of 80 °C, airflow between 9 and 11 mm3 h−1, and atomizing air pressure of 0.7 bar. Povidone (PVP) was used as a standard binder for comparison purposes. The binder systems were sprayed on the powder blend of theophylline and maltodextrin at a feed rate of 3.05 mL⋅min−1. Granule properties, such as yield, moisture content, morphology, label-free Raman imaging, particle size distribution, drug content, and flow properties, were evaluated. The process using NFC provided granules with excellent drug uniformity, low moisture content (<2 %), high yield (>92 %), and passable flow properties. Their behavior was comparable to that of granules prepared with the classical PVP binder system. Therefore, this study opens a perspective for the reuse of NFC from tobacco stalk, an agricultural waste, as an alternative binder for the granulation process, contributing to environmental sustainability.

Efficacy and Safety of Fixed-Dose Combinations for Pain in Older Adults.

Pain is common in older adults and managing pain in this population can be challenging owing to altered pharmacokinetics, multimorbidity, polypharmacy, cognitive impairment, and physical frailty. A fixed-dose combination (FDC) analgesic contains two or more pharmaceutical ingredients in a single pill and may offer more benefits when compared with loose-dose formulations. The benefits include reduced pill burden and better adherence, a broader analgesic spectrum well-suited to multimechanistic pain conditions and more predictable pharmacokinetic and pharmacodynamic properties. These advantages may outweigh disadvantages such as reduced flexibility in dose adjustment. Most of the commonly used FDC analgesics are made up of a combination of paracetamol, muscle relaxant, nonsteroidal anti-inflammatory drug or opioid. They have been shown to have better efficacy and similar safety profiles compared with individual drugs. Adverse effects from the use of FDC analgesics in older patients were comparable with that observed in younger populations. With proper patient selection and continuous surveillance, FDC analgesics will likely benefit older adults by simplifying dosing regimen and improving compliance.

Deep Eutectic Solvents Enhancing Drug Solubility and Its Delivery.

Deep eutectic solvents (DES) are environmentally friendly solvents with the potential to dissolve bioactive compounds without affecting their characteristics. DES has special qualities that can be customized to meet the unique characteristics of a biomolecule/active pharmaceutical ingredient (API) in accordance with various therapeutic needs, providing a reliable approach in opening the door for the creation of cutting-edge drug formulations by resolving solubility issues in pharmaceutics. This study outlines newly developing approaches to solve the problem of inefficient API extraction due to poor solubility. These emerging strategies also have the capacity to alter the chemical and physical stability of API, which triggers drug's shelf life and their possible health benefits. It is anticipated that the highlighted methods and processes will be developed to capitalize on the DES potential to improve drug solubility and delivery in the pharmaceutical sector.

Spectrophotometric quantification of trace levels of cyanide in water-insoluble drug substances and confirmation of specificity through an orthogonal comparison approach

Some pharmaceutical ingredients use cyanide in their synthesis, and this impurity must be controlled as per ICH, FDA and EDQM regulatory compliance. Spectrophotometric approaches for measuring cyanide levels are confined to water or water-soluble compounds with poor solution stability and low sensitivity. No method is available for the cyanide in water-insoluble drug substances through spectrophotometry. To address this gap, our study proposed a spectrophotometric approach for measuring trace cyanide in water-insoluble drugs such as Primidone and Clobazam. This method utilizes chloramine-T, which reacts with cyanide to form cyanogen chloride (CNCl), consequently reacting with pyridine-barbituric acid to produce a coloured derivative (C13H10N4O6, MW: 318.06 g/mol). This protocol also involves the selection of a suitable solvent and optimizing the pH for sensitive/accurate quantification of cyanide impurity. Mass spectrometry confirms cyanide derivatization as part of the orthogonal procedure comparison of ICH Q2 (R2). Method validation follows ICH Q2 (R2) guidelines in determining specificity, LOD (0.396 ppm), LOQ (1.200 ppm), linearity (1.2-45 ppm), and recovery (91-99% with %RSD<10%) of the method. The stability of the pyridine-barbituric acid reagent and derivatized compound was also evaluated. This approach effectively measures cyanide in water-insoluble drugs, meeting essential regulatory standards.

One-pot enantioselective synthesis of chiral phenyllactic acids by combining stereocomplementary d- and l-lactate dehydrogenases with multi-enzyme expression fine-tuning

Chiral phenyllactic acid (PLA) is a new type of antiseptic agent and a valuable precursor for active ingredients in pharmaceuticals and agrochemicals. In this study, we designed a multi-enzyme cascade that combined stereocomplementary d- and l-lactate dehydrogenases with threonine aldolase, phenylserine dehydratase, and formate dehydrogenase for the one-pot conversion of achiral glycine and benzaldehyde to synthesize d-PLA and l-PLA. To overcome the imbalance of multi-enzymes in a single cell, two enzyme modules, overexpressing four enzymes, were assembled in Escherichia coli cells to construct whole-cell catalysis systems (WCCSs). Furthermore, by optimizing reaction conditions and components, recombinant E. coli (WCCS 26) was able to produce 100 mM d-PLA with >99 % ee using a fed-batch strategy, while E. coli (WCCS 60) produced 47.2 mM l-PLA with >99 % ee. This study presents a sustainable and efficient method for synthesizing chiral PLAs from food-grade achiral starting materials.

Flaxseed (Linum usitatissimum) mucilage: A versatile stimuli–responsive functional biomaterial for pharmaceuticals and healthcare

The present review is novel as it discusses the main findings of researchers on the topic and their implications, as well as highlights the emerging research in this particular area and its future prospective. The seeds of Flax (Linum usitatissimum) extrude mucilage (FSM) that has a diverse and wide range of applications, especially in the food industry and as a pharmaceutical ingredient. FSM has been blended with several food and dairy products to improve gelling ability, optical properties, taste, and user compliance. The FSM is recognized as a foaming, encapsulating, emulsifying, suspending, film–forming, and gelling agent for several pharmaceutical preparations and healthcare materials. Owing to stimuli (pH) –responsive swelling–deswelling characteristics, high swelling indices at different physiological pHs of the human body, and biocompatibility, FSM is considered a smart material for intelligent, targeted, and controlled drug delivery applications through conventional and advanced drug delivery systems. FSM has been modified through carboxymethylation, acetylation, copolymerization, and electrostatic complexation to get the desired properties for pharma, food, and healthcare products. The present review is therefore devoted to the isolation techniques, structural characterization, highly valuable properties for food and pharmaceutical industries, preclinical and clinical trials, pharmacological aspects, biomedical attributes, and patents of FSM.

Investigation of the Effects of Energy-Efficient Drying Techniques and Extraction Methods on the Bioactive and Functional Activity of Banana Inflorescence

Plant-derived foods with therapeutic potential have strong connection with both the pharmaceutical and nutraceutical industries. The effectiveness of these therapeutic properties is heavily influenced by the thermal treatment during drying and extraction methods. Traditional convective drying is a very energy incentive and lengthy process. Although some advanced and hybrid drying methods have been developed, these have not been applied in drying of banana inflorescence. In this study, we investigated the effects of freeze-drying (FD) and intermittent microwave convective drying (IMCD), as well as traditional convective oven drying (CD), on the polyphenol profile of banana inflorescence when extracted using the energy-efficient Accelerated Solvent Extraction method (ASE). Our findings revealed that the freeze-dried banana inflorescence powder exhibited the highest extraction of bioactive compounds when using 75% methanol at 100 °C as a solvent. It recovered 2906.3 ± 20.83 mg/100 g of the phenolic compounds and 63.12 ± 0.25% antioxidant activity under the optimal extraction conditions. While IMCD was found to be the second-best drying method in terms of preserving bioactive compounds, its operational time and cost were significantly lower compared to freeze-drying. Furthermore, our study confirmed the presence of medicinal compounds such as gallic acid, protocatechuic acid, caffeic acid, coumaric acid, catechin, ferulic acid, kaempferol, and quercetin in banana inflorescence. The development of innovative functional foods and pharmaceutical ingredients through green extraction methods and optimal drying conditions holds significant potential to save energy in the process, enhance human health, and promote environmental sustainability and circular economy processes. These efforts align with supporting Sustainable Development Goals (SDGs) 3 and 12.

Adsorption of diclofenac by a novel H2SO4-CTAB co-modified granular spent bleaching earth carbon: Preparation, performance and mechanism

Diclofenac (DCF), a widely used pharmaceutical ingredient, exhibits long-lasting properties and significant ecotoxicity in aquatic ecosystems. In this study, a new granular adsorbent, GSBE@CH-CTAB, was synthesized to remove DCF by initially granulating powder spent bleaching earth carbon (SBE@C) with polytetrafluoroethylene (PTFE) emulsion as a binding agent, followed by a co-modification process involving H2SO4 and cetyltrimethyl ammonium bromide (CTAB). The adsorption capacity of the prepared adsorbent for DCF under the best conditions was 4.26 mg/g. In a wide pH range, GSBE@CH-CTAB could maintain a high adsorption capacity and show a good reusability. The presence of the three cations inhibited the adsorption of DCF (inhibition effect: Mg2+>Al3+>Na+). The adsorption process conformed to the pseudo-second-order kinetic model and Langmuir isotherm model. From the theoretical evaluation results, it could be inferred that DCF molecules were adsorbed on GSBE@CH-CTAB surface in both horizontal and non-horizontal directions at all operating temperatures. The main mechanisms of adsorption included electrostatic interaction, pore filling interaction, π-π interaction and H bond interaction. The granular adsorbent GSBE@CH-CTAB prepared in this study could effectively remove DCF, treat waste with waste, and solve the problem that powder adsorbent was easy to lose and difficult to recover, which was of great significance for the remediation of polluted water.

A comprehensive study of pharmaceutics solubility in supercritical solvent through diverse thermodynamic and hybrid Machine learning approaches

The pharmaceutical industry is increasingly drawn to the research of innovative drug delivery systems through the use of supercritical CO2 (scCO2)-based techniques. Measuring the solubility of drugs in scCO2 at varying conditions is a crucial parameter in this context. In this research, the supercritical solubility of two pharmaceutical ingredients, namely Febuxostat and Chlorpromazine, has been assessed theoretically using various thermodynamic approaches, including PR, SRK, UNIQUAC, and Wilson models. Additionally, hybrid machine learning models of PO-GPR, and PO-KNN were applied to anticipate the supercritical solubility of these medicines. Verification of the accuracy of each model for each pharmaceutical substance is conducted against previously reported experimental solubility data. In the comparison between the SRK and PR models, it is observed that the SRK model displays greater precision in correlating the solubility of both drugs. It consistently achieves a mean Radj value of 0.995 across all cases and mean AARD% values of 14.47 and 9.30 for Febuxostat and Chlorpromazine, respectively. Furthermore, the findings indicate that the UNIQUAC model surpasses the Wilson model in precisely representing the solubility of both medicines. It consistently achieves a mean Radj value higher than 0.985 across both cases and mean AARD% values of 11.39 and 7.08 for Febuxostat and Chlorpromazine, respectively. Additionally, the performance of both hybrid machine learning models proved to be excellent in anticipating the supercritical solubility of both compounds.

Protective effects of patchouli alcohol against DSS-induced ulcerative colitis

Patchouli alcohol (PA) is a widely used pharmaceutical ingredient in various Chinese traditional herbal medicine (THM) formulations, known for its modulatory effects on the gut microbiota. The present study investigated PA's anti-inflammatory and regulatory effects on gut microbiota and its mode of action (MOA). Based on the assessments of ulcerative colitis (UC) symptoms, PA exhibited promising preventions against inflammatory response. In accordance, the expressions of pro-inflammatory factors, including interleukin (IL)-1β, IL-6, tumor necrosis factor-α, and chemokine ligand 5 were significantly attenuated under PA treatment. Furthermore, PA enhanced the intestinal barrier damage caused by dextran sodium sulfate (DSS). Interestingly, PA exhibited negligible inventions on DSS-induced gut microbiota dysbiosis. PA did not affect the diversity of the DSS gut microbiota, it did alter the composition, as evidenced by a significant increase in the Firmicutes-Bacteroidetes (F/B) ratio. Finally, the MOA of PA against inflammation in DSS-treated mice was addressed by suppressing the expressions of heme oxygenase-1 (HO-1) and inducible nitric oxide synthase (iNOS). In conclusion, PA prevented inflammatory response in the DSS-induced UC mice model via directly suppressing HO-1 and iNOS-associated antioxidant signal pathways, independent of its effects on gut microbiota composition.

Risks of dairy derived excipients in medications for lactose intolerant and cow milk protein allergic patients

The use of lactose and cow milk protein (CMP) as potential allergens in pharmaceuticals and their ability to cause allergic reactions remains a significant concern in medicine. Lactose, a common pharmaceutical excipient due to its inert, inexpensive, and stable properties, is found in many prescription-only and over-the-counter medications. However, despite their widespread use, individuals with lactose intolerance (LI) or cow milk protein allergy (CMPA) may experience adverse reactions to these excipients. This study investigated the prevalence of lactose and other dairy-derived ingredients in pharmaceuticals marketed in Portugal. Using the Summary of Product Characteristics (SmPC) from the INFOMED database, various medications, including analgesics, antipyretics, non-steroidal anti-inflammatory drugs (NSAIDs), and antiasthmatics, were analyzed. Results showed a high prevalence of dairy-derived excipients, particularly in antiasthmatic drugs (62.6%) and NSAIDs (39%). Although CMP are not explicitly mentioned in SmPCs, the presence of lactose as an ingredient poses a risk of cross-contamination. The findings emphasize the need for healthcare professionals to be aware of potential allergens in medications and the importance of developing lactose-free alternatives to ensure the safety of patients with LI and CMPA. Further research is required to assess the safety and implications of lactose in medicines for these populations.

Simultaneously Enhanced Catalytic Activity and Thermostability of a Baeyer-Villiger Monooxygenase from Oceanicola granulosus by Reshaping the Binding Pocket.

Enzymatic oxygenation of various cyclic ketones into lactones via Baeyer-Villiger monooxygenases (BVMOs) could provide a promising route for synthesizing fragrances and pharmaceutical ingredients. However, unsatisfactory catalytic activity and thermostability restricted their applications in the pharmaceutical and food industries. In this study, we successfully improved the catalytic activity and thermostability of a Baeyer-Villiger monooxygenase (OgBVMO) from Oceanicola granulosus by reshaping the binding pocket. As a result, mutant OgBVMO-Re displayed a 1.0- to 6.4-fold increase in the activity toward branched cyclic ketones tested, accompanied by a 3 °C higher melting point, and a 2-fold longer half-life time (t1/2 (45 °C)). Molecular dynamics simulations revealed that reshaping the binding pocket achieved strengthened motion correlation between amino acid residues, appropriate size of the substrate-binding pocket, beneficial surface characteristics, lower energy barriers, and shorter nucleophilic distance. This study well demonstrated the trade-off between the enzyme activity and thermostability by reshaping the substrate-binding pocket, paving the way for further engineering other enzymes.

High performance lamellar structured graphene oxide nanocomposite membranes via Fe3O4-coordinated phytic acid control of interlayer spacing for organic solvent nanofiltration (OSN)

Graphene oxide (GO), a 2D nanomaterial known for its precise molecular sieving, holds potential for Organic Solvent Nanofiltration (OSN) and wastewater treatment. However, challenges such as thin interlayer spacing, extended diffusion pathways, and susceptibility to dehydration and negative charge-induced swelling limit its separation performance. To overcome these limitations, Herein, we have fabricated novel Fe3O4 coordinated PhA intercalated GO nanocomposite membranes. Impressively, these nanocomposite membranes exhibited remarkable separation efficiency for dyes, pesticides, and pharmaceutical ingredients, addressing the drawbacks associated with pristine GO membranes and enhancing their overall performance. The optimum G10(1)/P1.5-F100µL nanocomposite membrane displayed impressive solvent permeance of 40.43, 33.45, 20.70, 16.24, and 5.6 L/m2 h bar for acetone, methanol, water, ethanol, and IPA, respectively, while maintaining a rejection rate of ≥98.97 % for the MO dye (MW = 327.33 g/mol). Furthermore, the membrane exhibited outstanding efficiency in separating tetracycline (TC) in ethanol (≥97.97 %) and Pendimethalin (PM) in water (≥99.88 %). Additionally, it demonstrated high rejection capabilities for MB (≥98 %) and CR (≥98.78 %) in harsh DMF solvent. Importantly, the nanocomposite membrane displayed outstanding durability throughout continuous separation of Pendimethalin (PM) in a water solution over a period of 168 h. The PM separation remained nearly unchanged for the entire 168-h duration, demonstrating high mechanical strength and chemical stability. Additionally, the single nanocomposite membrane showcased high efficiency in feed change separation, successfully separating CR in ethanol and PM in water. These results, compared to the other GO-based nanocomposite membranes, demonstrate the exceptional stability and immense potential for real OSN applications.

Comprehensive Identification of Costus pictus Rhizome Extract as a Potent Plant Food: Unveiling Anti-Diabetic, Antimicrobial, Anticancer, and Anti-Inflammatory Properties.

Plant-derived foods are esteemed as natural preventives due to the constraints of contemporary pharmaceuticals, intensifying scrutiny of traditional medicinal flora. This study marked the first extensive evaluation of the anti-diabetic, anticancer, and anti-inflammatory effects of Costus pictus rhizomes, expanding beyond its well-known anti-diabetic properties in leaves. Hot air-dried C. pictus rhizomes underwent ultrasound-assisted extraction to produce the rhizome extract. Anti-diabetic effects were determined through enzymatic inhibition studies targeting "α-amylase and α-glucosidase," crucial enzymes in glucose regulation, revealing potent inhibitory effects with IC50 values of 266.591 and 324.938µg/ml, respectively. The ubiquity of breast cancer and constrained therapeutic alternatives for triple negative breast cancer led to the utilization of the "MDA-MB 231 cell line" for the study. The rhizome extracts demonstrated cytotoxicity at an IC50 concentration of 770µg/ml, with a pronounced decline in the "reactive oxygen species (ROS)" and "mitochondrial membrane potential (MMP)." They also regulated the cell cycle arrest at the G2/M phase and positively induced apoptosis, thus making it a potent anticancer candidate. Anti-inflammatory effects were assessed using "RAW 264.7 macrophage cell line" and exhibited dose-dependent reduction with IC50 of 495.074µg/ml, declining nitric oxide (NO) levels. Antimicrobial studies provided insights into its effectiveness against pathogens. This pivotal understanding laid groundwork for advancing C. pictus rhizome extract as a potential ingredient in pharmaceuticals or functional foods, leading to favorable health outcomes.

P-Coumaric acid pronounced protective effect against potassium bromate-induced hepatic damage in Swiss albino mice.

Potassium bromate (KBrO3) is a common dietary additive, pharmaceutical ingredient, and significant by-product of water disinfection. p-coumaric acid (PCA) is a naturally occurring nutritional polyphenolic molecule with anti-inflammatory and antioxidant activities. The goal of the current investigation was to examine the protective effects of p-coumaric acid against the liver damage caused by KBrO3. The five groups of animals-control, KBrO3 (100 mg/kg bw), treatment with KBrO3 along with Silymarin (100 mg/kg bw), KBrO3, followed by PCA (100 mg/bw, and 200 mg/kg bw) were randomly assigned to the animals. Mice were slaughtered, and blood and liver tissues were taken for assessment of the serum biochemical analysis for markers of liver function (alanine transaminase, aspartate transaminase, alkaline phosphatase, albumin, and protein), lipid markers and antioxidant markers (TBARS), glutathione peroxidase [GSH-Px], glutathione (GSH), and markers of hepatic oxidative stress (CAT), (SOD), as well as histological H&E stain, immunohistochemical stain iNOS, and COX-2 as markers of inflammatory cytokines. PCA protects against acute liver failure by preventing the augmentation of blood biochemical markers and lipid profiles. In mice liver tissues, KBrO3 increases lipid indicators and depletes antioxidants, leading to an increase in JNK, ERK, and p38 phosphorylation. Additionally, PCA inhibited the production of pro-inflammatory cytokines and reduced the histological alterations in KBrO3-induced hepatotoxicity. Notably, PCA effectively mitigated KBrO3-induced hepatic damage by obstructing the TNF-α/NF-kB-mediated inflammatory process signaling system. Additionally, in KBrO3-induced mice, PCA increased the intensities of hepatic glutathione (GSH), SOD, GSH-Px, catalase, and GSH activities. Collectively, we demonstrate the molecular evidence that PCA eliminated cellular inflammatory conditions, mitochondrial oxidative stress, and the TNF-α/NF-κB signaling process, thereby preventing KBrO3-induced hepatocyte damage.

NADES-based extraction optimization and enrichment of Cyanidin-3-O-galactoside from Rhododendron arboreum Sm.: Kinetics and thermodynamics insights

Cyanidin-3-O-galactoside (Cy3-gal) is the most widespread anthocyanin that has been found to be applicable to nutraceutical and pharmaceutical ingredients. Nevertheless, the process of separation and purification, susceptibilities to heat, and pH inactivation present some limitations. In the present study, natural deep eutectic solvents (NADES) with an ultrasonic-assisted extraction method were briefly studied, and the recovery of Cy3-gal from Rhododendron arboreum was highlighted. The NADES, consisting of choline chloride and oxalic acid (1:1), was screened out as an extractant, and single-factor experiments combined with a two-site kinetic model were employed to describe the extraction process. Further, the work investigated ultrasound-assisted adsorption/desorption to efficiently purify Cy3-gal using macroporous resins. The optimal extraction conditions to attain maximum Cy3-gal yield was 30% water in a 50:1 (mL/g) solvent-to-sample ratio, 11.25 W/cm3 acoustic density, and 50% duty cycle for 16 min of extraction time. Under these conditions, the results revealed 23.07 ± 0.14 mg/g of Cy3-gal, two-fold higher than the traditional solvents. Furthermore, of the different resins used, Amberlite XAD-7HP showed significantly (p < 0.05) higher adsorption/desorption capacities (12.82 ± 0.18 mg/g and 10.97 ± 0.173 mg/g) and recovery (48.41 ± 0.76%) percent over other adsorbents. Experiments on the degrading behavior (40–80 °C) of the recovered Cy3-gal were performed over time, and the first-order kinetic model better explained the obtained data. In conclusion, the study asserts the use of ultrasonication with NADES and XAD-7HP resin for the improved purification of Cy3-gal from the crude extract.