Iron-catalyzed regioselective synthesis of (E)-vinyl sulfones mediated by unprotected hydroxylamines.

An Fe-catalyzed unprotected hydroxylamine mediated Heck-type coupling between sulfinic acids and alkenes for the regioselective synthesis of (E)-vinyl sulfones has been developed. Mechanism studies indicated for the first time that a radical process may be involved and that hydroxylamines play multiple roles, including those of a mild oxidant and an in situ base. It was found for the first time that this transformation not only realizes C-S bond construction promoted by unprotected hydroxylamines, but also provides a practical and complementary method for the preparation of structurally important (E)-vinyl sulfones.

Impact of soy lecithin, zinc oxide, and methylsulfonylmethane, as excipient ingredients, on the bioaccessibility and intestinal transport of branched-chain amino acids from animal and plant protein mixtures.

To maximize the biological activity of branched-chain amino acids (BCAAs), it is necessary to find a new excipient agent to increase the bioavailability of BCAAs in protein mixtures. The aim of the current study was to investigate the effects of soy lecithin (SLC), zinc oxide (ZnO), and methylsulfonylmethane (MSM) on the bioaccessibility and intestinal transport of BCAAs from animal and plant protein mixtures (PMs) via an in vitro digestion model with human intestinal epithelial (Caco-2) cells. The bioaccessibility of total BCAAs in PMs considerably increased by 107.51 ± 1.50% with the addition of SLC, and the combined effects of SLC, ZnO, and MSM on enhancing the bioaccessibility of total BCAAs was observed (107.14 ± 0.18%). Interestingly, SLC showed a major role in binding bile acid, showing 65.78 ± 1.66% of binding capacity. Intestinal transport of BCAAs was measured to be at 100.48, 110.86, and 130.29 µg mL-1 for leucine, isoleucine, and valine, respectively, in PMs with SLC + ZnO + MSM, and it eventually amplified the amount of the total transported BCAAs (341.63 ± 6.34 µg mL-1), which was about 8.72 times higher than that of PM only. The cellular integrity of digesta-treated Caco-2 cells tended to decrease according to the incubation time, but it was recovered in the treatment of PM + SLC + ZnO + MSM, and nearly reached the control levels with 92.82 ± 0.53%. Results from the current study suggest that the co-consumption of proteins equally consisting of plant and animal sources with SLC, ZnO, and MSM could improve the bioavailability of total BCAAs, resulting in the improvement of health benefits.

Benzosuberene-sulfone analogues synthesis from Cedrus deodara oil and their therapeutic evaluation by computational analysis to treat type 2 diabetes.

Benzosuberene-sulfone (BSS) analogues have been semi-synthesized following green approaches from himachalenes, which has been extracted from essential oil of Cedrus deodara. In this process, benzosuberene in presence of different aryl or alkyl sodium sulfinates, I2 and potassium persulfate (K2S2O8) in acetonitrile-water solvent conditions gave BSS-analogues at room temperature. Under this reaction, a facile endocyclic ß-H elimination has been noticed for BSS-analogues synthesis instead of vinyl sulfones and the reason may be due to its specific structure and electronic environment. The BSS-compounds were obtained with moderate to excellent yields under mild conditions. All the compounds were computationally subjected to drug likeliness and toxicity prediction studies. Further, the synthesized molecules were evaluated under in-silico studies for their binding affinity towards the native Peroxisome Proliferator-Activated Receptor Gamma (PPARG), and two PPARG mutants (R357A and V290M). Both the mutant forms of PPARG are deficient in eliciting a response to treatment with full and partial agonists. Our computational studies suggested that the molecule 3q performed better than the standard drug (Rosiglitazone) in all three protein structures. This implies that our suggested molecule could act as a more potent antagonist to native PPARG and could also be developed to treat type-2 diabetes patients with R357A and V290M mutations, which didn't elicit any response to currently available drugs in the market.

Structural Determination, Biological Function, and Molecular Modelling Studies of Sulfoaildenafil Adulterated in Herbal Dietary Supplement.

Unapproved ingredients included in herbal medicines and dietary supplements have been detected as adulterated synthetic drugs used for erectile dysfunction. Extraction from a dietary supplement was performed to isolate the compounds by HPLC analysis. The structural characterization was confirmed using mass spectrometry (ESI-TOF/MS and LC-MS/MS), 1H NMR, and 13C NMR spectroscopy techniques. Results identified the thus-obtained compound to be sulfoaildenafil, a thioketone analogue of sildenafil. The biological activities of this active compound have been focused for the first time by the experimental point of view performance in vitro. The results revealed that sulfoaildenafil can affect the therapeutic level of nitric oxide through the upregulation of nitric oxide synthase and phosphodiesterase type 5 (PDE5) gene expressions. This bulk material, which displays structural similarity to sildenafil, was analyzed for the presence of a PDE5 inhibitor using a theoretical calculation. These unique features of the potential activity of PDE5 protein and its inhibitors, sildenafil and sulfoaildenafil, may play a key consideration for understanding the mode of actions and predicting the biological activities of PDE5 inhibitors.

Chemoproteomics-Enabled De Novo Discovery of Photoswitchable Carboxylesterase Inhibitors for Optically Controlled Drug Metabolism.

Herein, we report arylazopyrazole ureas and sulfones as a novel class of photoswitchable serine hydrolase inhibitors and present a chemoproteomic platform for rapid discovery of optically controlled serine hydrolase targets in complex proteomes. Specifically, we identify highly potent and selective photoswitchable inhibitors of the drug-metabolizing enzymes carboxylesterases 1 and 2 and demonstrate their pharmacological application by optically controlling the metabolism of the immunosuppressant drug mycophenolate mofetil. Collectively, this proof-of-concept study provides a first example of photopharmacological tools to optically control drug metabolism by modulating the activity of a metabolizing enzyme. Our arylazopyrazole ureas and sulfones offer synthetically accessible scaffolds that can be expanded to identify specific photoswitchable inhibitors for other serine hydrolases, including lipases, peptidases, and proteases. Our chemoproteomic platform can be applied to other photoswitches and scaffolds to achieve optical control over diverse protein classes.

Methylsulfonylmethane sensitizes endometrial cancer cells to doxorubicin.

BACKGROUND: Methylsulfonylmethane (MSM) is a commonly used diet supplement believed to decrease the inflammation in joints and fastens recovery in osteoarthritis, gastric mucosal injury, or obesity-related disorders. It was also suggested that MSM might play a beneficial role in cancer treatment. PURPOSE: So far, the MSM might have a potentially beneficial effect in endometrial cancer (EC) treatment. STUDY DESIGN: This study evaluated the effect and usefulness of MSM in combinatory therapy with known drug doxorubicin (DOX). METHODS: The effect of combinational treatment of MSM and DOX on the induction of apoptosis was evaluated in EC cell lines (ISHIKAWA, MFE-296, MFE-280). RESULTS: We observed that MSM itself induces apoptosis in EC cell lines, and pre-treatment with MSM for 24 h increases the sensitivity of EC cells to DOX-induced apoptosis and DNA damage and that effect might be regulated by p42/44 (Erk1/2) MAPK and Akt (protein kinase B). CONCLUSION: These results for the first time show that MSM might act as a sensitizer of EC cells to known drugs, for which EC cells quickly acquire resistance. Graphical abstract.

Cystoisospora suis merozoite development assay for screening of drug efficacy in vitro.

Cystoisospora suis is a common diarrheal pathogen of piglets and typically controlled by metaphylactic toltrazuril application. Recently, toltrazuril resistance has been reported in the field; however, both evaluation of toltrazuril efficacy against field isolates and the anticoccidial drug development for pigs is hampered by costs and labor of animal experimentation. Therefore an in vitro merozoite development assay was developed to evaluate the efficacy of compounds against C. suis in vitro. Monolayers of IPEC-1 cells were infected with sporozoites derived from oocysts of defined C. suis laboratory strains and the optimal infection dose as well as concentration, time point and duration of treatment were evaluated by quantitative real-time PCR. Cell cultures were treated with bumped kinase inhibitor (BKI) 1369 at different time points to evaluate the possibility to delineate effects on different developmental stages in vitro during invasion and early infection, and to determine different inhibitory concentrations (IC50, IC95). BKI 1369 had an IC50 of 35 nM and an IC95 of 350 nM. Dose- and duration-dependent efficacy was seen when developing stages were treated with BKI 1369 after infection (days 0-1, 2-3 and 2-5) but not when sporozoites were pre-incubated with BKI 1369 before infection. Efficacies of further BKIs were also evaluated at 200 nM. BKI 1318, 1708, 1748 and 1862 had an efficacy comparable to that of BKI 1369 (which is also effective in vivo). BKI 1862 showed a more pronounced loss of efficacy in lower concentrations than BKI 1369, signifying pharmacokinetic differences of similar compounds detectable in vitro. In addition, the effects of toltrazuril and its metabolites, toltrazuril sulfoxide and toltrazuril sulfone, on a toltrazuril sensitive and a resistant strain of C. suis were evaluated. Inhibition of merozoite growth in vitro by toltrazuril and its metabolites was dose-dependent only for toltrazuril. Clear differences were noted for the effect on a toltrazuril-sensitive vs. a resistant strain, indicating that this in vitro assay has the capacity to delineate susceptible from resistant strains in vitro. It could also be used to evaluate and compare the efficacy of novel compounds against C. suis and support the determination of the optimal time point of treatment in vivo.

Structure and properties of lipase activated by cellulose-silica polyethersulfone membrane for production of pentyl valerate.

Herein, this study extracted nanocrystalline cellulose (NC) and silica (SiO2) from raw oil palm leaves (OPL), and employed as nanofillers in polyethersulfone (PES) to produce NC-SiO2-PES as support to immobilize Candida rugosa lipase (CRL) (NC-SiO2-PES/CRL). XRD, TGA-DTG and FTIR-ATR data affirmed that NC and SiO2 were isolated from OPL with corresponding crystallinity indices of 68 % and 70 %. A 0.02 cm membrane size with 5% (w/v) of NC-SiO2 without PVP K30 was optimal for membrane fabrication. CRL immobilized on the Glut-AP-NC-SiO2-PES membrane gave a higher conversion of pentyl valerate (PeVa) (91.3 %, p < 0.05) compared to Glut-NC-SiO2-PES (73.9 %) (p < 0.05). Characterization of the NC-SiO2-PES/CRL biocatalyst verified the presence of CRL. Hence, raw OPL is a proven good source of NC and SiO2, as reinforcement nanofillers in PES. The overall findings envisage the promising use of NC-SiO2-PES/CRL to catalyze an expedient and high yield of PeVa, alongside the suitability of NC-SiO2-PES for activating other enzymes.

Biologically Active Compounds from Goji (Lycium Barbarum L.) Leaves Aqueous Extracts: Purification and Concentration by Membrane Processes.

Goji (Lycium barbarum L.) leaves and fruits have been described as a valuable source of bioactive compounds with a great potential for the development of health-promoting formulations. The present study aimed to evaluate the potential of a sustainable process for the recovery of phenolic compounds from Goji leaves through a combination of aqueous extraction and membrane-based operations. Water was used as a safe, cheap, and non-hazardous extraction solvent, and parameters of extraction of dried Goji leaves were optimized in order to maximize the yield of polyphenols, total soluble solids (TSS), and total antioxidants simultaneously. The aqueous extract was clarified by ultrafiltration and then processed with three flat-sheet polyethersulphone (PES) membranes with molecular weight cut-off (MWCO) values in the range of 0.3-4.0 kDa, in order to remove sugar compounds from polyphenols and improve the antioxidant activity of the produced fractions. Among the selected membranes, a 1 kDa membrane exhibited the best performance in terms of purification of polyphenols from the clarified aqueous extract. The rejection by this membrane of TSS and total carbohydrates was in the range of 15.8-25.3%, and was decreased by increasing the volume reduction factor (VRF). On the other hand, the retention values for total polyphenols and total antioxidant activity (TAA) were in the range of 73-80%, and were increased by increasing the VRF.

A Simple Zinc-Mediated Method for Selenium Addition to Michael Acceptors.

In this work, we focused our attention on seleno-Michael type reactions. These were performed using zinc-selenolates generated in situ from diphenyl diselenide 1, 1,2-bis(3-phenylpropyl)diselenide 30, and protected selenocystine 31 via an efficient biphasic Zn/HCl-based reducing system. Alkenes with a variety of electron-withdrawing groups were investigated in order to gauge the scope and limitations of the process. Results demonstrated that the addition to acyclic α,ß-unsaturated ketones, aldehydes, esters amides, and acids was effectively achieved and that alkyl substituents at the reactive ß-centre can be accommodated. Similarly, cyclic enones undergo efficient Se-addition and the corresponding adducts were isolated in moderate to good yield. Vinyl sulfones, α,ß-unsaturated nitriles, and chalcones are not compatible with these reaction conditions. A recycling experiment demonstrated that the unreacted Zn/HCl reducing system can be effectively reused for seven reaction cycles (91% conversion yield at the 7° recycling rounds).

Tunable Heteroaromatic Sulfones Enhance in-Cell Cysteine Profiling.

Heteroaromatic sulfones react with cysteine via nucleophilic aromatic substitution, providing a mechanistically selective and irreversible scaffold for cysteine conjugation. Here we evaluate a library of heteroaromatic sulfides with different oxidation states, heteroatom substitutions, and a series of electron-donating and electron-withdrawing substituents. Select substitutions profoundly influence reactivity and stability compared to conventional cysteine conjugation reagents, increasing the reaction rate by >3 orders of magnitude. The findings establish a series of synthetically accessible electrophilic scaffolds tunable across multiple centers. New electrophiles and their corresponding alkyne conjugates were profiled directly in cultured cells, achieving thiol saturation in a few minutes at submillimolar concentrations. Direct addition of desthiobiotin-functionalized probes to cultured cells simplified enrichment and elution to enable the mass spectrometry discovery of >3000 reactive and/or accessible thiols labeled in their native cellular environments in a fraction of the standard analysis time. Surprisingly, only half of the annotated cysteines were identified by both iodoacetamide-desthiobiotin and methylsulfonylbenzothiazole-desthiobiotin in replicate experiments, demonstrating complementary detection by mass spectrometry analysis. These probes offer advantages over existing cysteine alkylation reagents, including accelerated reaction rates, improved stability, and robust ionization for mass spectrometry applications. Overall, heteroaromatic sulfones provide modular tunability, shifted chromatographic elution times, and superior in-cell cysteine profiling for in-depth proteome-wide analysis and covalent ligand discovery.

Effects of Hydrogen Peroxide and Sodium Hypochlorite Aging on Properties and Performance of Polyethersulfone Ultrafiltration Membrane.

Chemical reaction of main polymer and additive with oxidative cleaning agents plays an important role in aging of polymeric membrane for water and wastewater treatment. As a green and powerful oxidant, hydrogen peroxide (H2O2) can achieve good cleaning efficacy under alkaline condition, but its influence on membrane aging was poorly understood. In this study, degradation of polyethersulfone (PES) membrane due to H2O2 exposure under alkaline condition (pH 9 and 11) was holistically investigated by humic acid (HA) filtration experiments and multiple membrane characterization techniques, with sodium hypochlorite (NaClO) aging examined as a comparison. Membrane permeability and HA retention rate was hardly changed by H2O2 aging at an exposure dose of 500 g·h/L, whereas NaClO aging led to substantial increase of membrane permeability and significant decrease of retention ability. Meanwhile, H2O2 aging slightly increased fouling propensity with HA filtration, while NaClO aging resulted in more serious fouling. ATR-FTIR and XPS analysis revealed much less degradation of PES and hydrophilic additive by H2O2 than that by NaClO, and membrane morphology and surface properties were characterized to explain the variation of filtration performance. Overall, compared with cleaning with NaClO, membrane degradation can be minimized by cleaning with H2O2.

In silico Design, Virtual Screening and Synthesis of Novel Electrolytic Solvents.

We report the building, validation and release of QSPR (Quantitative Structure Property Relationship) models aiming to guide the design of new solvents for the next generation of Li-ion batteries. The dataset compiled from the literature included oxidation potentials (Eox ), specific ionic conductivities (κ), melting points (Tm ) and boiling points (Tb ) for 103 electrolytes. Each of the resulting consensus models assembled 9-19 individual Support Vector Machine models built on different sets of ISIDA fragment descriptors.(1) They were implemented in the ISIDA/Predictor software. Developed models were used to screen a virtual library of 9965 esters and sulfones. The most promising compounds prioritized according to theoretically estimated properties were synthesized and experimentally tested.

Determination of perillaldehyde in perilla herbs using relative molar sensitivity to single-reference diphenyl sulfone.

Perillaldehyde (PRL) is one of the essential oil components derived from perilla plants (Perilla frutescens Britton) and is a characteristic compound of the traditional medicine "perilla herb ()" listed in the The Japanese Pharmacopoeia, 17th edition (JP17). HPLC using an analytical standard of PRL has been used to quantitatively determine the PRL content in perilla herb. However, PRL reagents have been reported to decompose easily. In this study, we utilized an alternative quantitative method using on a single reference with relative molar sensitivity (RMS) based on the results of experiments performed in two laboratories. It was possible to calculate the exact RMS using an offline combination of 1H-quantitative NMR spectroscopy (1H-qNMR) and an HPLC/photodiode array (PDA) detector (or an HPLC/variable-wavelength detector [VWD]). Using the RMS of PRL to the single-reference compound diphenyl sulfone (DFS), which is an inexpensive and stable compound, the PRL content in the perilla herb could be determined using HPLC/PDA or HPLC/VWD without the need for the analytical standard of PRL. There was no significant difference between the PRL contents of perilla herb determined using the method employing the single-reference DFS with RMS and using the JP17 assay, the calibration curve of which was generated using the analytical standard of PRL with adjusted purity measured by 1H-qNMR. These results demonstrate that our proposed method using a single reference with RMS is suitable for quantitative assays of perilla herb and can be an alternative method for the current assay method defined in the JP17.

Supplementing multi-functional groups to polysulfone membranes using Azadirachta indica leaves powder for effective and highly selective acid recovery.

Moderate and eco-pleasing ion-exchange trade membranes are in need to recover acid from industrial waste. Present study is focused on incorporation of plant waste (Azadirachta indica, neem leaves powder (NP)) of different composition as filler to polysulfone (PSf) membrane matrix to achieve acid recovery. Membranes were characterized, their chemical, mechanical and thermal stabilities and effectiveness in acid recovery via diffusion has been inspected. Multi-functional groups (-COOH, -NH2, -OH, -OAc, -C = O) present in different components of NP contributes in their own means in H+ ion transportation through membrane in acid recovery. They assisted formation of hydrogen bond and provided channels for ion permeation, and facilitated selective transportation of H+ ion over Fe2+ ions and explained mechanism is in accordance with Grotthuss-type and vehicle mechanism. Membrane with 15% of NP showed better performance in terms of ion exchange capacity (IEC) and acid recovery, at optimum concentration of NP, composite the membrane showed highest IEC values of 3.9771 mmol/g, UH+ value of ≈46.499 × 10-3 m/h and greater separation factor ≈154, which is higher than commercially available DF-120 membrane. An original thought of utilizing NP in membrane matrix opens up promising opportunities for extremely straightforward, easy, cost-effective and greener methods of recovery acid.

Nano-curcumin incorporated polyethersulfone membranes for enhanced anti-biofouling in treatment of sewage plant effluent.

Biofouling is a severe problem in membrane systems which hampers their broad applications because it requires regular chemical cleaning, reduces membrane life, and also decreases product quality. In this study, nanocurcumin (CCM) was prepared by sonication-assisted wet-milling technique and then incorporated in polyethersulfone (PES) membrane to enhance the anti-biofouling property. TEM analysis of the curcumin showed that nanomaterials are spherical. FTIR studies confirmed that the presence of CCM nanomaterial in PES membrane. Zone inhibition studies revealed that PES/CCM nanocomposite membranes exhibited the better anti-biofouling propensity against Escherichia coli and Pseudomonas aeruginosa. Static adhesion studies also showed that PES/CCM nanocomposite membranes prevented the attachment and proliferation of E. coli cells. Also, PES/2 wt% CCM nanocomposite membrane had a high thermal degradation temperature of 575.62 °C and tensile strength of 1.87 MPa. Moreover, addition of CCM nanomaterial in casting solution altered the membrane morphology and hydrophilicity. Further, pure water flux was increased up to 64.48 L·m-2·h-1 for PES/2 wt% CCM nanocomposite membrane. Filtration of raw sewage treatment plant effluent was also carried out. The incorporation of curcumin in membranes was effectively improved the antifouling tendency without compromised affecting the chemical oxygen demand reduction. This study highlights the anti-biofouling potential of CCM incorporated PES nanocomposite membranes, which could be utilized for various filtration applications.

Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.

Pulmonary edema is a common ailment of heart failure patients and has remained an unmet medical need due to dose-limiting side effects associated with current treatments. Preclinical studies in rodents have suggested that inhibition of transient receptor potential vanilloid-4 (TRPV4) cation channels may offer an alternative-and potentially superior-therapy. Efforts directed toward small-molecule antagonists of the TRPV4 receptor have led to the discovery of a novel sulfone pyrrolidine sulfonamide chemotype exemplified by lead compound 6. Design elements toward the optimization of TRPV4 activity, selectivity, and pharmacokinetic properties are described. Activity of leading exemplars 19 and 27 in an in vivo model suggestive of therapeutic potential is highlighted herein.

Adsorptive removal of harmful algal species Microcystis aeruginosa directly from aqueous solution using polyethylenimine coated polysulfone-biomass composite fiber.

In recent times, the treatment of harmful algal blooms (HABs) became an important environmental issue to preserve and remediate water resources globally. In the present study, the adsorptive removal of harmful algal species Microcystis aeruginosa directly from an aqueous medium was attempted. Waste biomass (Escherichia coli) was immobilized using polysulfone and coated using the cationic polymer polyethylenimine (PEI) to generate PEI-coated polysulfone-biomass composite fiber (PEI-PSBF). The density of M. aeruginosa in an aqueous medium (BG11) was significantly decreased by treatment with PEI-PSBF. additionally, analysis using FE-SEM, confirmed that the removal of M. aeruginosa algal cells by PEI-PSBF was caused by the adsorption mechanism. According to the profiles of phosphorus for the algal cell growth in M. aeruginosa cultivating samples, we found that the adsorbed M. aeruginosa onto the PEI-PSBF lost their biological activity compared to the non-treated M. aeruginosa cells.

Discovery of N-{2-Methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}-N'-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazine-2,4-diamine (ASP3026), a Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor.

Anaplastic lymphoma kinase (ALK) is a validated therapeutic target for treating echinoderm microtubule-associated protein-like 4 (EML4)-ALK positive non-small cell lung cancer (NSCLC). We synthesized a series of 1,3,5-triazine derivatives and identified ASP3026 (14a) as a potent and selective ALK inhibitor. In mice xenografted with NCI-H2228 cells expressing EML4-ALK, once-daily oral administration of 14a demonstrated dose-dependent antitumor activity. Here, syntheses and structure-activity relationship (SAR) studies of 1,3,5-triazine derivatives are described.

The Inhibitory Effect of Panax Ginseng Extract on Amyloid-like Fibril Formation of Trypsin in Aqueous Ethanol.

BACKGROUND: In case of several chronic diseases, prevention is could be more effective than treatment. Functional foods that contain significant amounts of bioactive components gained considerable attention not only in traditional but in modern medicine as well. We have investigated how P. ginseng extract inhibits the in vitro formation of amyloid-like fibrils of phenylmethylsulfonyl- trypsin (PMS-trypsin) in 60% ethanol at pH 7.0. The model system used is non-physiological, but it is capable of detecting the anti-amyloidogenic effect of the various agents. OBJECTIVE: The main objective of this study was to examine the possible inhibitory effect of ginseng extract on amyloid-like fibril formation of trypsin in aqueous ethanol. METHODS: The amyloid formation and aggregation kinetics of PMS-trypsin was studied by turbidity measurements, Congo Red (CR) binding assays, size exclusion chromatography and Electronic Circular Dichroism (ECD) measurements and the shapes of amyloid fibrils became visible by Transmission Electron Microscopy (TEM). RESULTS: In the presence of 500-fold diluted P. ginseng extract in the incubation mixture, the absorption at 350 nm decreased to 47.1% after incubation for 24 h, compared relative to the sample which contained no additives. CR binding experiments suggested that the aggregates in our samples have amyloid-like properties, and P. ginseng extract inhibits the amyloid-like fibril formation of PMS-trypsin depending on concentration. Our results show that the ginseng extract does not bind to the fibrils. In the absence of P. ginseng extracts large sized colloid aggregates were abundant. Adding P. ginseng extracts to our samples decreased the light dispersion of the solution. This is due to the decrease of the rate of the aggregation or to the smaller size of the aggregates evolved. Our results show that the presence of ginseng extract helps to maintain the native structure of the protein. In the presence of 500-fold diluted P. ginseng extract, TEM images demonstrated, that P. ginseng extract has inhibitory effect on the formation of amyloid-like fibrils of PMS-trypsin. CONCLUSION: The results indicated that P. ginseng extract significantly inhibits the formation of amyloid-like fibrils of PMS-trypsin in aqueous ethanol, and helps to maintain the native structure of the protein. The rate of inhibition depends on concentration. P. ginseng extract is an efficient antiamyloidogenic agent.