Anti-acetylcholinesterase Activity Research Articles

Chemical Composition, In Vitro Antioxidant Activities, and Inhibitory Effects of the Acetylcholinesterase of Liparis nervosa (Thunb.) Lindl. Essential Oil.

The present study aimed to investigate the essential oil composition of Liparis nervosa (Thunb.) Lindl., grown in China, and to determine its antioxidant and inhibitory effects on acetylcholinesterase. The essential oil was obtained by hydrodistillation, and the chemical compounds were analyzed by GC-MS and GC-FID. We used 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing assay power (FRAP) to evaluate the antioxidant activity. The anti-acetylcholinesterase activity of the essential oil was also examined. Sixty-seven compounds were identified, representing 98.50 % of the total essential oil, which was shown to be rich in methyl (9E,11E)-octadeca-9,11-dienoate (31.69%), n-hexadecanoic acid (15.08%), isopropyl palmitate (12.44%), propyl tetradecanoate (7.20%), tetradecanoic acid (4.01%), 17-octadecynoic acid (3.71%), and pentacosane (2.24%). Its antioxidant ability was analyzed via ABTS (IC50 = 721.95 ± 9.93 μg/mL), DPPH scavenging capacity (IC50 > 10,000 μg/mL), and the FRAP method (Trolox equivalent antioxidant concentration 39.64 ± 3.38 μM/g). Acetylcholinesterase inhibition effects were evaluated and had an IC50 value of 51.96 ± 14.26 μg/mL. The results show that this essential oil has interesting biological potential, encouraging further investigations, especially regarding the mechanisms of action of its antioxidant and anti-acetylcholinesterase activity. This is the first time that the chemical composition, antioxidant activity, and acetylcholinesterase inhibition effects of essential oil from L. nervosa have been studied.

Phenolic profiles and acetylcholinesterase inhibitory activity in Australian adzuki bean

Adzuki bean is a minor pulse crop in Australia, but there is potential to expand its production if it can be established as a high-value crop. This study profiled the phenolics in the seed and seedcoat material of nine Australian adzuki bean genotypes using liquid chromatography with tandem mass spectrometry (LC-MS/MS). The most abundant phenolic compounds were catechin, rutin and quercetin-3-glucoside. The total phenolic content of the seedcoat (2714–3764 mg gallic acid equivalents [GAE]/100 g) was much higher than that of the seed material (60–286 mg GAE/100 g). The seedcoat material also showed moderate anti-acetylcholinesterase activity, which may provide potential anti-Alzheimer benefits. This may support the use of adzuki bean material – particularly the seedcoat – in the functional food market.

Determination of cytotoxic, anti-acetylcholinesterase and antioxidant activity of some medicinal Artemisia spp.

The study aims to investigated the antioxidant activities, phenolic compounds, acetylcholinesterase enzyme inhbition and cytotoxic effects of two different of Artemisia spp. (Artemisia dracunculus L. and Artemisia dracunculoides Pursh) cultivated in Turkey organically, for the first time. Total phenolic, total flavonoid contents of the plants determined spectrophotometrically while antioxidant activity DPPH, CUPRAC, and FRAP was determined using colorimetric method. And also acetylcholinesterase enzyme inhibition activity and anti-cancer activity in-vitro aganist human melanoma (VMM917, CRL-3232), lung carcinoma (A549, CCL-185) and, normal human fibroblast (hGF, PCS-201-018) cells were studied. Total phenolic (225-324 mgGAE/g sample) and total flavonoid contents (0.066-0.085 mgQAE/g sample), antioxidant activity (DPPH (1.371-1.655 mg/mL), CUPRAC (0.246-0.344 µM CTEAC) and FRAP (462.133-726.661 µM CTEAC)). A. dracunculus and A. dracunculoides extracts inhibited 40.09±0.65%, and 39.48±3.68% of acetylcholinesterase activity. It was determined that demonstrated the selective effect of A. dracunculus and A. dracunculoides on the cytotoxicity of A549 and hGF cells.

NADES-based essential oil extraction and isolation of new epoxysesquiterpene from Ageratina adenophora flowers

During the past decade, natural deep eutectic solvents (NADESs) have emerged as a green alternative to conventional organic solvents due to properties like low toxicity, diverse metabolite solubility, and biodegradability. In the present study, choline chloride (CC) and lactic acid (LA)-based NADES has been utilized as pre-extraction media prior to the hydrodistillation of Ageratina adenophora flowers. CC and LA were used in three different molar ratios (1:1, 1:2 and 1:3) along with water to extract essential oil from flowers. The essential oil yield was found to be increased from 2.84 mg/g to 13.52 mg/g using NADES-assisted hydrodistillation. Gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) were used to analyse the chemical diversity of the essential oils. In addition, a new epoxy containing sesquiterpene molecule named 5,11-epoxycadin-3,4-en-8-one, was also isolated from the essential oil without chromatography techniques. The molecular structure and absolute configuration have been deduced using NMR spectroscopy (1D & 2D NMR), and single-crystal X-ray diffraction (SC-XRD), respectively. Also, the morphology of the crystal surface was studied using scanning electron microscopy (SEM). Furthermore, the anti-acetylcholinesterase activity of the essential oils and isolated new molecule has also been investigated.

Neuroprotective and nephroprotective effects of Ircinia sponge in polycyclic aromatic hydrocarbons (PAHs) induced toxicity in animal model: a pharmacological and computational approach

The present study investigated the neuroprotective and nephroprotective effects of the sponge Ircinia sp. ethyl acetate extract (ISPE) against persistent aromatic pollutants in vitro and in vivo. Different exponential experimental assays were applied to this study. An in vitro study to investigate the potential therapeutic effect of ISPE using antioxidants (for example, ABTS and DPPH) and anti-Alzheimer assays (inhibition of acetylcholinesterase); the in-vivo study was designed to evaluate the protective effect of ISPE as neuroprotective and nephroprotective against the destructive effect of PAH. Several assays included oxidative assays (LPO), antioxidant biomarkers (GSH, GST), and inflammatory and neurodegenerative biomarkers (PTK,SAA). Additionally, the results were confirmed using histopathological examination. The in silico screening study improved the in vitro and in vivo findings through interaction between the aryl hydrocarbon receptor (AHR) and the polyphenolic content of ISPE extract, which was determined using LCMSM. The results and discussion showed that ISPE exhibited a promising antioxidant and anti-acetylcholinesterase activity as evidenced by IC50 values of 49.74, 28.25, and 0.18 µg/mL in DPPH, ABTS, and acetylcholinesterase inhibition assays, respectively. In vivo, the study showed that animals receiving ISPE before poly aromatic hydrocarbons administration PAHs (Prot, ISPE) showed significant amelioration in kidney functions manifested by the reduction of serum urea, uric acid, and creatinine by 40.6%, 66.4%, and 134.8%, respectively, concerning PAH-injected mice (HAA). Prot, ISPE revealed a decline in malondialdehyde (MDA) and total proteins (TP) in kidney and brain tissues by 73.63% and 50.21%, respectively, for MDA and 59.82% and 80.41%, respectively, for TP with respect to HAA. Prot, ISPE showed significant elevation in reduced glutathione (GSH) and glutathione transferase (GST) in kidney and brain tissues and reduction in the inflammatory and pre-cancerous biomarkers, namely, serum protein tyrosine kinases (PTKs) and serum amyloid A (SAA). These findings were further supported by histopathological examination of kidney and brain tissues, which revealed normal structure approaching normal control. Metabolic profiling of ISPE using LC–MS-MS showed the presence of fourteen polyphenolic compounds belonging mainly to phenolic acids and flavonoids. In silico study revealed that all the tested compounds exerted certain binding with the aryl hydrocarbon receptor, where rutin showed the best fitting (ΔG = − 7.6 kcal/mol−1) with considerable pharmacokinetic and pharmacodynamic properties revealed from in silico ADME (Absorption, Distribution, Metabolism, and Excretion) study. Hence, it can be concluded that the Ircinia sponge showed a promising protective effect versus kidney and brain toxicity triggered by PAHs.Graphical

Chemical Characterization, Antioxidant, Insecticidal and Anti-Cholinesterase Activity of Essential Oils Extracted from Cinnamomum verum L.

This study is aimed at evaluating the potential of the essential oil of Cinnamomum verum (EOCV) as an antioxidant, as an insecticide against Callosobruchus maculatus and for its anti-acetylcholinesterase activity. To this end, EOCV was extracted via hydrodistillation from this plant, and the identification of the phytochemicals was performed using gas chromatography–mass spectrometry (GC–MS). The antioxidant power was determined via in vitro tests, the insecticidal ability was tested via exposing C. maculatus to EOCV, and molecular docking was used to evaluate the anti-cholinesterase ability. The results of these GC–MS analyses show that the main composition of EOCV comprises Cinnamaldehyde dimethyl acetal (64.50%), cinnamicaldehyde (35.04%) and α-Copaene (0.11%). The insecticidal potential of the studied OEs, determined by using the inhalation test, and expressed as the concentration of EOs required for the death of 50% of the insects (LC50) and that required the death of 95% of adults (LC95) after 96 h of exposure, was 3.99 ± 0.40 and 14.91 ± 0.10 μL/L of air, respectively. In the contact test, 96 h of exposure gave an LC50 and LC95 of 3.17 ± 0.28 and 8.09 ± 0.05 μL/L of air, respectively. A comparison of the antioxidant activity of EOCV to that of ascorbic acid via DPPH free radical scavenging ability and Ferric Reducing Antioxidant Power (FRAP) revealed the IC50 and EC50 values of EOCV to be much higher than that obtained for ascorbic acid, and the molecular docking simulation revealed Coumarin, Piperonal, Cinnamaldehyde dimethyl and alpha-Copaene as possessing potential inhibitory activities against human acetylcholinesterase. However, further experimental validation is needed to enhance the prospects of this study.

Neuroprotective effects of Cubebin and Hinokinin lignan fractions of Piper cubeba fruit in Alzheimer’s disease in vitro model

Abstract Objectives The current research examines the protective effects of the Piper cubeba ethanolic extract and its isolated lignans; Cubebin and Hinokinin fractions against Alzheimer’s Disease (AD) in vitro model. Methods Dried and powdered fruit of P. cubeba were extracted in ethanol and fractionated using silica gel column chromatography. Of the 15 eluted fractions, two fractions indicated presence of targeted Lignans; Hinokinin and Cubebin. They were monitored by thin layered chromatography and their structures were confirmed by LC-HRMS spectrometry and NMR analysis. Antioxidant activity of the crude extract and isolated lignan fractions were analyzed using FRAP, DPPH and ABTS assays. Anti-acetylcholinesterase activity was investigated in vitro and β-amyloid (Aβ) cytotoxicity on SHSY-5Y human neuroblastoma cell lines was studied using MTT assay. Results The crude extract showed similar if not significantly stronger antioxidant capacity compared to ascorbic acid in FRAP and DPPH assays. Both lignans exerted weaker yet potent activity. The crude extract yielded the strongest acetylcholinesterase inhibitory potential compared to the lignan fractions however, there was no significant difference (p<0.05) between IC50 values of lignan fractions. Significant neuroprotective effects against 50 μM Aβ at p<0.05 was observed for selected fractions compared to Aβ treated control. The crude extract was highly protective against Aβ at both 5 and 10 μg/mL. Cubebin and Hinokinin-containing fractions significantly improved the viability of the SH-SY5Y cells against Aβ cytotoxicity both only at the concentration of 100 μg/mL. Conclusions Results from our studies suggest that these phytoconstituents might be good candidates in prevention and treatment of AD.

Comparative Study of Phytochemistry, Antioxidant and Biological Activities of Berberis libanotica Fruit and Leaf Extracts.

Berberis libanotica Ehrenb. ex C.K. Schneider of the Berberidaceae family is an endemic Lebanese plant and is widely used in folk medicine. This study highlights the phytochemical composition and biological activities (in vitro) of fruit and leaf extracts. The two organs were extracted by cold maceration with four solvents of increasing polarity: cyclohexane, dichloromethane, ethyl acetate and methanol. The extracts were screened for their chemical composition by HPLC-DAD to identify and quantify the phenolic compounds. Volatile compounds were detected by GC-MS. The antioxidant capacity through DPPH inhibition was tested. The anti-acetylcholinesterase, antibacterial and anti-proliferative activities were evaluated. Thirteen compounds, including 12 phenolics, were detected in the fruits, whereas 8 phenolic compounds were identified in the leaves. A total of 137 volatile compounds were identified in both organs. At 50 μg/mL, the methanolic leaf extract presented the highest antioxidant capacity, with an inhibition percentage of 54.9%. The dichloromethane fruit extract reduced the acetylcholinesterase activity by 65.3%. The cyclohexane leaf extract reduced the proliferation of the HCT-116 cells by 54.8%, while the dichloromethane fruit extract exhibited the best inhibition against the Caco-2 cells (54%). Interestingly, the minimum inhibitory concentration (MIC) value of the cyclohexane fruit extract against Salmonella enterica serovar Kentucky was 2.4 μg/mL, and the MIC value of the cyclohexane leaf extract against E. coli was 9.7 μg/mL.

Multi-Targeting Neuroprotective Effects of Syzygium aromaticum Bud Extracts and Their Key Phytocompounds against Neurodegenerative Diseases.

Alzheimer's disease (AD) is a neurodegenerative disease that causes a gradual loss of normal motor and cognitive function. The complex AD pathophysiology involves various factors such as oxidative stress, neuroinflammation, amyloid-beta (Aβ) aggregation, disturbed neurotransmission, and apoptosis. The available drugs suffer from a range of side effects and are not able to cover different aspects of the disease. Therefore, finding a safer therapeutic approach that can affect multiple targets at a time is highly desirable. In the present study, the underlying neuroprotective mechanism of an important culinary spice, Syzygium aromaticum (Clove) extract, and major bioactive compounds were studied in hydrogen peroxide-induced oxidative stress in human neuroblastoma SH-SY5Y cell lines as a model. The extracts were subjected to GC-MS to identify important bioactive components. The extracts and key bio-actives reduced reactive oxygen species (ROS), restored mitochondrial membrane potential (MMP), and provided neuroprotection from H2O2-induced oxidative stress in cell-based assays due to the antioxidant action. They also reduced lipid peroxidation significantly and restored GSH content. Clove extracts have also displayed anti-acetylcholinesterase (AChE) activity, anti-glycation potential, and Aβ aggregation/fibrilization inhibition. The multitarget neuroprotective approach displayed by Clove makes it a potential candidate for AD drug development.

Plants of the genus Mahonia as a Potential Traditional Chinese Medicine for the Prevention and Treatment of Alzheimer's Disease.

Alzheimer's disease (AD), a prevalent multiple neurodegenerative disease, has gained attention, particularly in the aging population. However, presently available therapies merely focus on alleviating the symptoms of AD and fail to slow disease progression significantly. Traditional Chinese medicine (TCM) has been used to ameliorate symptoms or interfere with the pathogenesis of aging-associated diseases for many years based on disease-modifying in multiple pathological roles with multi-targets, multi-systems and multi-aspects. Mahonia species as a TCM present potential for anti-inflammatory activity, antioxidant activity, anti-acetylcholinesterase activity, and anti-amyloid-beta activity that was briefly discussed in this review. They are regarded as promising drug candidates for AD therapy. The findings in this review support the use of Mahonia species as an alternative therapy source for treating AD.

Evaluation of potential inhibitory effects on acetylcholinesterase, pancreatic lipase, and cancer cell lines using raw leaves extracts of three fabaceae species

The present study examined the biological potential and phytochemicals of Sophora mollis, Mucuna pruriens, and Indigofera atropurpurea methanolic leaf extracts. In vitro anti-acetylcholinesterase and anti-lipase assays were performed using different concentrations of plant extracts, and the IC50 values were determined. The cytotoxic potential of the selected plant extracts was assessed against HeLa, PC3, and 3T3 cell lines using an MTT assay. S. mollis leaf extract displayed the highest inhibition percentage (114.60% ± 19.95 at 1000 μg/mL) for the anti-acetylcholinesterase activity with a prominent IC50 value of 75.9 μg/mL. The anti-lipase potential was highest with the M. pruriens leaf extract (355.5 μg/mL IC50), followed by the S. mollis extract (862.7 μg/mL IC50). Among the cell lines tested, the cytotoxic potential of the I. atropurpurea extract (91.1 ppm IC50) against the PC3 cell line was promising. High-performance liquid chromatography revealed gallic acid, chlorogenic acid, caffeic acid, vanillic acid, rutin trihydrate, and quercetin dihydrate in varying concentrations in all plant species. The concentration of chlorogenic acid (69.09 ppm) was highest in M. pruriens, and the caffeic acid concentration (45.20 ppm) was higher in S. mollis. This paper reports the presence of bioactive therapeutic compounds in selected species of the Fabaceae family that could be micro-propagated, isolated, and utilized in pharmaceutical industries.

Chemical compositions and anti-acetylcholinesterase, nitric oxide suppressing activities of Piper longum fruits oil

Piper longum fruits oil in Binh Dinh, Vietnam was obtained via steam distillation with oil collection efficiency reaching 1.01%. The chemical compositions of the essential oil from Piper longum fruits in Binh Dinh, Vietnam is determined via the GC-MS method that includes 35 components (99.68%), among which the main components are caryophyllene (10.78%), 3-heptadecene (9.95%), zingiberene (9.54%), germacrene D (8.96%), pentadecane (8.76%), heptadecane (8.73%), β-bisabolene (5.98%), humulene (5.80%), (E)-5-tetradecene (2.73%), α-bisabolene (2.47%), tridecane (2.35%). The essential oil of Piper longum in Binh Dinh, Vietnam also showed weak anti-acetylcholinesterase activity with IC50 (µg/mL) = 164.55±13.79 compared to galantamine as a positive control and potent nitric oxide suppressing activity with IC50 (µg/mL) = 13.02±0.29 compared to dexamethasone as a positive control.

PHYTOCHEMICAL SCREENING, TLC PROFILE AND 1H NMR ANALYSIS OF Passiflora foetida EXTRACTS

Passiflora foetida also known as red fruits passionflower is widely found in Malaysia. Previous studies on this plant reported its therapeutic properties such as anticancer, antidiabetic, anti-hyperpigmentation, antioxidant, analgesic, anti-inflammatory, anti-acetylcholinesterase, and antimicrobial activities. In this study, different parts of the plant (aerial, stem, leaf and fruit) were used for the phytochemical screening such as alkaloid, flavonoid, terpenoid and saponin tests. The aerial, leaf and stem parts show positive results in all tests, however, there are slightly different in color intensity of each test. The fruit, except for terpenoid, shows positive results in alkaloid, flavonoid and saponin tests. Then, thin layer chromatography (TLC) profile was carried out in various solvent systems including chloroform/methanol (9:1) solvent system and ethylacetate/hexane (1:9). The TLC profile shows that chloroform/methanol (9:1) solvent system give better separation of compounds as compared to ethylacetate/hexane (1:9) solvent system. There are characteristic spots found on the TLC plate that possibly attributed to the presence of flavonoids, steroids, and terpenoids. Moreover, the fresh aerial part extract of P. foetida was analyzed using 1H-NMR and found some signals that indicated the presence of phenolic and flavonoid compounds in the extract. This study can act as a preliminary study that provides the information on the metabolite profile of different parts of P. foetida and might be useful for the future study.

Bioactive Metabolite from Endophytic Aspergillus versicolor SB5 with Anti-Acetylcholinesterase, Anti-Inflammatory and Antioxidant Activities: In Vitro and In Silico Studies.

Endophytic fungi are a highly unpredictable group of microorganisms that can create a diverse range of secondary metabolites with biological activity. These metabolites enhance the host's ability to tolerate stress caused by various factors, such as disease, insects, pathogens, and herbivores. The secondary metabolites produced by endophytic fungi may have potential applications in agriculture, pharmacy, and medicine. The purpose of this study was to examine the anti-acetylcholinesterase activity of secondary metabolites extracted from endophytic fungi. Aspergillus versicolor SB5 was one of the many endophytic fungi isolated from Juncus rigidus and identified genetically with accession number ON872302. Our study utilized fermentation and microbial cultivation techniques to obtain secondary metabolites. During the course of our investigation, we isolated a compound called Physcion (C1) from the endophytic fungus Aspergillus versicolor SB5. We subsequently identified that C1 possesses inhibitory activity against COX-2 and LOX-1, with IC50 values of 43.10 and 17.54 µg/mL, respectively, making it an effective anti-inflammatory agent. Moreover, we found that C1 also exhibited potent anticholinesterase activity (86.9 ± 1.21%). In addition to these promising therapeutic properties, our experiments demonstrated that C1 possesses strong antioxidant capacity, as evidenced by its ability to scavenge DPPH, ABTS, O2 radicals, and NO and inhibit lipid peroxidation. To further investigate the molecular mechanisms underlying C1 pharmacological properties, we employed SwissADME web tools to predict the compound's ADME-related physicochemical properties and used Molecular Operating Environment and PyMOL for molecular docking studies.

Antioxidant, Anti-Skin-Aging, Anti-Inflammatory, and Anti-Acetylcholinesterase Activities of Rourea oligophlebia Extracts.

The objective of this study was to evaluate the antioxidant, anti-skin-aging, anti-inflammatory, and anti-acetylcholinesterase activities of the hexane (n-hex), AcOEt, BuOH, MeOH, and aqueous extracts from R. oligophlebia roots. The total phenolic and flavonoid contents (TPC and TFC) were determined using Folin-Ciocalteu and AlCl3 colorimetric assays. The antioxidant capacity was examined by reducing power (RP), ferric reducing antioxidant power (FRAP), ABTS⋅+ , and DPPH⋅+ radical cation assays. All extracts potentially exhibited antioxidant activity with IC50 values ranging from 2.93 to 5.73 μg/mL for ABTS⋅+ and from 5.69 to 7.65 μg/mL for DPPH⋅+ except the n-hex extract. The BuOH, MeOH, and aqueous extract possess promising anti-skin-aging activities, as observed by an attenuation of UV-A toxicity on human keratinocytes. We proposed that these anti-skin-aging properties are possibly due to direct scavenging activity against reactive oxygen species and upregulate cellular antioxidant machinery. Moreover, we found that the antioxidant capacity was well correlated with anti-inflammatory capacity against nitric oxide (NO) production in terms of the n-hex, AcOEt, and BuOH extracts with IC50 values from 23.21 to 47.1 μg/mL. In contrast, these activities were found to be poorly correlated with AchE activity. To the best of our knowledge, this is the first report of the antioxidant, anti-skin-aging, anti-inflammatory, and anti-acetylcholinesterase activities of the extracts of R. oligophlebia roots. These findings indicated that this species could be a potential source of natural antioxidant, anti-aging, and anti-inflammatory agents. Consequently, it may be suggested as a medicinal plant that prevents diseases related to oxidative stress and inflammatory responses.

Anti-Arthritic Activity of Sanguisorba Minor Subsp. Balearica Against “Freund’s Complete Adjuvant-Induced” Arthritis in Rats

Therapeutic properties of Sanguisorba L. genus plants are supported by numerous in vivo and in vitro studies showing the anti-viral, anti-ulcerogenic, anti-cancer, anti-acetylcholinesterase, radioprotective, anti-allergic, and anti-inflammatory activities. The present study was designed to investigate anti-arthritic activity of the “Sanguisorba minor subsp. balearica (Bourg. ex Nyman) Muñoz Garm. & C.Navarro” (Smb), a subspecies of Sanguisorba L. genus, on CFA-induced arthritic rat model. The extract of aerial parts of the Smb was obtained by the consecutive steps of maceration process. The phytochemical content of the extract was analyzed by the High Performance Liquid Chromatography (HPLC) method. Complete Freund’s Adjuvant-induced arthritic rats were used to examine the anti-arthritic activity of the plant extract. HPLC analysis revealed high amount of phenolic compounds in the Smb extract. The identified phenolics are ellagic acid, gallic acid, quercetin dehydrate and p-coumaric acid with the concentrations of 4,1288; 2,6342; 0,0871 and 0,0633 ppm, respectively. Injection of Smb extract to rats caused a decrease in paw thickness in the CFA-induced arthritic animals. The decrease in paw thicknesses of animals treated by quercetin and Smb 70 mg/kg groups was higher than diclofenac sodium group. Smb 34 mg/kg group also showed a decrease in paw thickness but it was lower compared to quercetin and Smb 70 mg/kg groups and higher than the diclofenac sodium group. According to the histopathological evaluations of the joint tissues, both 34 mg/kg and 70 mg/kg Smb extract treatment of animals were improved inflammatory deformations related to arthritis.

How Closely Does Induced Agarwood’s Biological Activity Resemble That of Wild Agarwood?

Continuous innovation in artificially-induced agarwood technology is increasing the amount of agarwood and substantially alleviating shortages. Agarwood is widely utilized in perfumes and fragrances; however, it is unclear whether the overall pharmacological activity of induced agarwood can replace wild agarwood for medicinal use. In this study, the volatile components, total chromone content, and the differences in the overall activities of wild agarwood and induced agarwood, including the antioxidant, anti-acetylcholinesterase, and anti-glucosidase activity were all determined. The results indicated that both induced and wild agarwood's chemical makeup contains sesquiterpenes and 2-(2-phenylethyl)chromones. The total chromone content in generated agarwood can reach 82.96% of that in wild agarwood. Induced agarwood scavenged 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) radicals and inhibited acetylcholinesterase activity and α-glucosidase activity with IC50 values of 0.1873 mg/mL, 0.0602 mg/mL, 0.0493 mg/mL, and 0.2119 mg/mL, respectively, reaching 80.89%, 93.52%, 93.52%, and 69.47% of that of wild agarwood, respectively. Accordingly, the results distinguished that induced agarwood has the potential to replace wild agarwood in future for use in medicine because it has a similar chemical makeup to wild agarwood and has comparable antioxidant, anti-acetylcholinesterase, and anti-glucosidase capabilities.

Chemical Composition and In Vitro Antioxidant Activity and Anti-Acetylcholinesterase Activity of Essential Oils from Tadehagi triquetrum (L.) Ohashi.

The present study aimed to determine the chemical compositions of essential oils (EOs) from Tadehagi triquetrum (L.) Ohashi and evaluate their antioxidant and anti-cholinesterase activity under the comprehensive influence of chemical components. The essential oils were extracted from T. triquetrum (L.) Ohashi by hydrodistillation. A total of 58 organic compounds were identified by GC-FID and GC-MS analysis. The major components of T. triquetrum (L.) Ohashi EOs were identified as palmitic acid (22.46%), 1-Octen-3-ol (14.07%), Caryophyllene (7.20%), (Z)-18-Octadec-9-enolide (6.04%), and 3-Hexen-1-ol (4.55%). The antioxidant activity of the essential oils was determined by using ABTS assay, DPPH assay, and FRAP assay, with IC50 values of 2.12 ± 0.05 mg/mL, 4.73 ± 0.91 mg/mL against the ABTS, DPPH, and FRAP value 117.42 ± 8.10 mM/g. The result showed that it had moderate antioxidant activities in the experiment, which why it is likely that it will be used as an antioxidant. At the same time, the EOs also showed moderate anti-acetylcholinesterase activity. This study expands the chemical and biological knowledge of the EOs of T. triquetrum.

Evaluation of Biological Activities of Twenty Flavones and In Silico Docking Study

This work aimed to evaluate the biological activities of 20 flavones (M1 to M20) and discuss their structure-activity relationships. In vitro assays were established to assess their numerous biological activities (anti-α-amylase, anti-acetylcholinesterase, anti-xanthine oxidase, anti-superoxide dismutase, and anticancer cell lines (HCT-116, MCF7, OVCAR-3, IGROV-1, and SKOV-3 cells lines)). An in silico docking study was also established in order to find the relationship between the chemical structure and the biological activities. In vitro tests revealed that M5 and M13 were the most active in terms of anti-α-amylase activity (IC50 = 1.2 and 1.4 µM, respectively). M17 was an inhibitor of xanthine oxidase (XOD) and performed better than the reference (allopurinol), at IC50 = 0.9 µM. M7 presented interesting anti-inflammatory (IC50 = 38.5 µM), anti-supriode dismutase (anti-SOD) (IC50 = 31.5 µM), and anti-acetylcholinesterase (IC50 = 10.2 µM) activities. Those abilities were in concordance with its high scavenging activity in antioxidant ABTS and DPPH assays, at IC50 = 6.3 and 5.2 µM, respectively. Selectivity was detected regarding cytotoxic activity for those flavones. M1 (IC50 = 35.9 µM) was a specific inhibitor to the MCF7 cancer cell lines. M3 (IC50 = 44.7 µM) and M15 (IC50 = 45.6 µM) were particularly potent for the OVCAR-3 cell line. M14 (IC50 = 4.6 µM) contributed more clearly to inhibiting the colon cancer cell line (HCT116). M7 (IC50 = 15.6 µM) was especially active against the ovarian SKOV human cancer cell line. The results of the biological activities were supported by means of in silico molecular docking calculations. This investigation analyzed the contribution of the structure-activity of natural flavones in terms of their biological properties, which is important for their future application against diseases.

Acetylcholinesterase inhibitors: structure-activity relationship and kinetic studies on selected flavonoids

Flavonoids are secondary plant metabolites that have long been included in the human diet. These natural products are well known for their beneficial effects on health. Thus, in this study, the in vitro inhibitory activity of 28 different flavonoids (1-28) against acetylcholinesterase was evaluated, and the type of inhibition for the most active compound (12) was studied. Acetylcholinesterase (AChE) inhibitors are considered the main class of medication used for the treatment of the primary dementia phase in Alzheimer's disease (AD). Our study used galantamine as a positive control and showed that 7,8-dihydroxyflavone (12) has the highest anti-acetylcholinesterase activity. The inhibitory type of 7,8-dihydroxyflavone, which is non-competitive inhibition, was determined for the first time. Furthermore, the obtained data allowed us to identify the characteristic flavonoid structure that facilitates AChE inhibition: the presence of a hydroxyl group at C7 in the benzo-γ-pyrane ring of the molecule.