Wantida Chaiyana

Inhibition of cholinesterase by essential oil from food plant

Inhibition of cholinesterase has attracted much attention recently because of its potential for the treatment of Alzheimers disease. In this work, the anticholinesterase activities of plant oils were investigated using Ellmans colorimetric method. The results indicate that essential oils obtained from Melissa officinalis leaf and Citrus aurantifolia leaf showed high acetylcholinesterase and butyrylcholinesterase co-inhibitory activities. C. aurantifolia leaf oil revealed in this study has an IC(50) value on acetylcholinesterase and butyrylcholinesterase of 139 ± 35 and 42 ± 5 μg/ml, respectively. GC/MS analysis revealed that the major constituents of C. aurantifolia leaf oil are monoterpenoids including limonene, l-camphor, citronellol, o-cymene and 1,8-cineole.

Characterization of potent anticholinesterase plant oil based microemulsion

In the present study, essential oils of three edible Thai plants, Cymbopogon citratus (Gramineae), Citrus hystrix (Rutaceae) and Zingiber cassumunar (Zingiberaceae) were comparatively tested for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities using Ellmans colorimetric method. C. citratus oil exhibited the highest activity with IC(50) values of 0.34±0.07μl/ml and 2.14±0.18μl/ml against BChE and AChE activity, respectively. It was further investigated whether microemulsions of this oil could be obtained. The effects of type of surfactant and co-surfactant as well as pH and ionic strength on the phase behavior of the oil/water system were investigated. Brij 97, Triton X-114, Tween 20 and Tween 85 were employed as surfactant whereas ethanol and hexanol were used as cosurfactants. The size analysis, electrical conductivity measurements and cholinesterase inhibition assays were done in selected microemulsion. The results revealed that the type and concentration of surfactant and co-surfactant exhibited a distinct influence on the C. citratus oil microemulsions. Moreover, the inhibitory activities of the microemulsion formulation were remarkable.

Characterization and in vitro permeation study of microemulsions and liquid crystalline systems containing the anticholinesterase alkaloidal extract from Tabernaemontana divaricata.

The aims of the present study were to characterize the microstructure and study the skin permeation enhancement of formulations containing the alkaloidal extract from Tabernaemontana divaricata. The extract was loaded in the formulations composed of Zingiber cassumunar oil, Triton X-114, ethanol and water with the oil:surfactant ratios of 1:5 and 2:5. The formulations were characterized by photon correlation spectroscopy, polarizing light microscopy, differential scanning calorimetry, and viscosity measurement. A reverse micellar phase, w/o microemulsions, liquid crystalline systems, liquid crystal in microemulsion systems and coarse emulsions were formed along the aqueous dilution line of both oil:surfactant ratios. Formulations with the ratio of 1:5 containing 0.1 μg/ml extract showed a significantly higher acetylcholinesterase inhibition than those with the ratio of 2:5. The skin of stillborn piglet was used in the permeation study. The liquid crystalline and microemulsion systems significantly increased the transdermal delivery of the extract within 24h. It was concluded that the alkaloidal extract from T. divaricata stem loaded in liquid crystalline or microemulsion systems comprising Z. cassumunar oil/Triton X-114/ethanol/water may act as an alternative percutanous formulations for enhancing the acetylcholine level in Alzheimers patients.

Inhibition of 5α-Reductase, IL-6 Secretion, and Oxidation Process of Equisetum debile Roxb. ex Vaucher Extract as Functional Food and Nutraceuticals Ingredients

This study aims to investigate the biological activities related to hair loss of Equisetum debile extracts, including 5α-reductase inhibition, interleukin-6 (IL-6) secretion reduction, and anti-oxidation. E. debile extracts were obtained by maceration in various solvents. Crude extract (CE) was obtained by maceration in 95% ethanol. Chlorophyll-free extract (CF) was the CE which of the chlorophyll has been removed by electrocoagulation. Hexane extract (HE), ethyl acetate extract (EA), and ethanolic extract (ET) were fraction extracts obtained from maceration in hexane, ethyl acetate, and 95% ethanol, respectively. The extracts were investigated for inhibitory activity against 5α-reductase and IL-6 secretion. Total phenolic contents (TPC) were investigated and antioxidant activities were determined by means of 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), 2,2′-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP) assays. The inhibition of lipid peroxidation was determined by the ferric thiocyanate method. The cytotoxicity of the extracts on dermal papilla cells and irritation test by hens egg test chorioallantoic membrane assay were also investigated. All extracts could inhibit 5α-reductase and decrease IL-6 secretion in lipopolysaccharide-stimulated macrophage. The antioxidant activity of E. debile extracts was directly related to their TPC. ET which contained the highest TPC (68.8 ± 6.7 mg GA/g) showed the highest equivalent concentration (EC1) of 289.1 ± 26.4 mM FeSO4/g, TEAC of 156.6 ± 34.6 mM Trolox/g, and 20.0 ± 6.0% DPPH inhibition. However, EA exhibited the highest inhibition against lipid peroxidation (57.2 ± 0.4%). In addition, EA showed no cytotoxicity on dermal papilla cell line and no irritation on chorioallantoic membrane of hen’s eggs. In conclusion, EA was suggested as the most attractive ingredients for functional food and nutraceuticals because of the high inhibitory activity against 5α-reductase, IL-6 secretion, and lipid peroxidation inhibition.

Investigation of the Skin Anti-photoaging Potential of Swertia chirayita Secoiridoids Through the AP-1/Matrix Metalloproteinase Pathway by Molecular Modeling

Secoiridoids are bioactive compounds, which are present in plants and exhibit anti-inflammatory activity. In this work, to understand the structural basis of five secoiridoids; amarogentin, amaroswerin, gentiopicrin, sweroside, and swertiamarin for potent inhibitors of the target proteins associated with the collagen degradation pathway, namely MMP-1, MMP-3, MMP-9 and transcription factor AP-1, molecular docking, binding mode modeling, and MD simulations were carried out. The binding inhibitory effects of the secoiridoids were screened on these proteins. The obtained results in terms of binding conformation, binding free energy, protein–ligand interaction profile, structural flexibility, and binding energy decomposition of the secoiridoid inhibitors were elucidated. The molecular modeling clarified inhibitory effect on account of the five secoiridoids towards all three Matrix metalloproteinases (MMPs). Moreover, amarogentin and gentiopicrin may interfere with gene expression via binding to AP-1. Among all screened secoiridoids, amarogentin and gentiopicrin exhibited an interesting binding affinity to the MMPs and AP-1. The results suggest that amarogentin has the highest potential for application as an anti-aging agent with the MMP inhibitory and anti-transcriptional activities, even though further studies are needed to determine the anti-aging effect in vitro, in vivo and by clinical evaluation.

Enhancement of antioxidant and skin moisturizing effects of olive oil by incorporation into microemulsions

The aims of the present study were to develop olive oil microemulsions and characterize their antioxidant and skin moisturizing properties. The acid, iodine, and saponification values of olive oil were 0.38 ± 0.01 mg potassium hydroxide/g, 88.2 ± 5.9 mg iodine/g, and 192.2 ± 1.4 mg potassium hydroxide/g, respectively. Pseudoternary phase diagrams, constructed using the water titration method, produced suitable microemulsions: microemulsion 1 (10% olive oil, 64% Tween 85, 16% propylene glycol, and 10% water) and microemulsion 2 (10% olive oil, 64% Tween 85, 16% ethanol, and 10% water). Microemulsions 1 and 2 exhibited Newtonian flow behavior with internal droplet sizes of 443.60 ± 27.66 nm and 139.37 ± 12.15 nm, respectively. Their in vitro antioxidant and skin moisturizing properties were investigated in comparison with native olive oil. Microemulsion 2 possessed the highest significant antioxidant effect (p < 0.05) giving half maximal inhibitory concentration values in radical-scavenging activity against 1,1-diphenyl-2-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) of 4.78 ± 1.25 mg/mL and 14.85 ± 11.18 mg/mL, respectively. The lipid peroxidation inhibition of microemulsion 2 was comparable to native olive oil, whereas the skin moisturizing effect of microemulsion 1 was comparable to the well-known skin moisturizer, hyaluronic acid. In conclusion, microemulsions enhanced both antioxidant and skin moisturizing effects and were attractive formulations for using as a cosmetic or drug delivery system.

Antioxidant activity and irritation property of venoms from Apis species

ABSTRACT Pharmacological effects of bee venom has been reported, however, it has been restricted to the bee venom collected from European honey bee (Apis mellifera). The aim of the present study was to compare the antioxidant activities and irritation properties of venoms collected from four different Apis species in Thailand, which includes Apis cerena (Asian cavity nesting honeybee), Apis florea (dwarf honeybee), Apis dorsata (giant honeybee), and A. mellifera. Melittin content of each bee venom extracts was investigated by using high‐performance liquid chromatography. Ferric reducing antioxidant power, 2, 2′‐azinobis (3‐ethylbenzothiazoline‐6‐sulfonic acid), and 1, 1‐diphenyl‐2‐picrylhydrazyl assay were used to determine the antioxidant activity, whereas, hens egg test chorioallantoic membrane assay was used to determine the irritation property of each bee venom extracts. Melittin was the major constituent in all bee venom extracts. The melittin content in A. dorsata, A. mellifera, A. florea, and A. cerena were 95.8 ± 3.2%, 76.5 ± 1.9%, 66.3 ± 8.6%, and 56.8 ± 1.8%, respectively. Bee venom extract from A. dorsata possessed the highest antioxidant activity with the inhibition of 41.1 ± 2.2% against DPPH•, Trolox equivalent antioxidant capacity of 10.21 ± 0.74 mM Trolox/mg and equivalent concentration (EC1) of 0.35 ± 0.02 mM FeSO4/mg. Bee venom extract from A. mellifera exhibited the highest irritation, followed by A. cerena, A. dorsata, and A. florea, respectively. Melittin was the compound responsible for the irritation property of bee venom extracts since it could induce severe irritation (irritation score was 13.7 ± 0.5, at the concentration of 2 mg/ml). The extract from A. dorsata which possessed the highest antioxidant activity showed no irritation up to the concentration of 0.1 mg/ml. Therefore, bee venom extract from A. dorsata at the concentration not more than 0.1 mg/ml would be suggested for using as cosmetic ingredients since it possessed the highest antioxidant activity with no irritation. This study is the first report to compare the bee venom extracts from different Apis species and display their potential application of bee venom extracts in cosmetic products. Graphical abstract Figure. No Caption available. HighlightsBee venom from A. dorsata possessed the highest antioxidant activity comparing to A. mellifera, A. cerena, and A. florea.Melittin, a major constituent of bee venom, was responsible for the irritation property since it induced severe irritation.Bee venom from A. dorsata possessed high antioxidant activity and showed no irritation at the concentration of 0.1 mg/ml.Bee venom from A. dorsata was suggested for using as cosmetic ingredient at the concentration not more than 0.1 mg/ml.

Improvement of Stability and Transdermal Delivery of Bioactive Compounds in Green Robusta Coffee Beans Extract Loaded Nanostructured Lipid Carriers

The aim of this study was to develop green robusta coffee beans extract loaded nanostructured lipid carriers (NLCs) for enhancing dermal application and its efficiency. The green robusta coffee beans extract cultivated in Chumphon (CP) exhibited the highest antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay with IC50 of 34.1 ± 0.9 µg/ml, lipid peroxidation inhibition with percentage inhibition of 38.8 ± 1.7, and ferric reducing antioxidant power (FRAP) assay with a FRAP value of 234.5 ± 12.3 mM FeSO4/g. The extract contained caffeine, chlorogenic acid, and caffeic acid as major compounds. The anti-inflammatory test indicated that CP could decrease the secretion of IL-6 in macrophage cells and caused no irritation to blood vessels on the irritation test by hen’s egg test chorioallantoic membrane (HET-CAM) assay. The particle size of CP-loaded NLCs was 158.1 ± 0.2 nm with a narrow polydispersity index and showed no noticeable difference after the stability test. Entrapment efficacy of CP-loaded NLCs was found to be over 60%. Caffeine and chlorogenic acid in CP-loaded NLCs were released sustainably and penetrated deeper into the skin than the extract in a conventional emulsion. In conclusion, the CP-loaded NLCs can be further used in cosmetics for dermal applications due to good efficacy and safety.

Molecular modeling of non-covalent binding of Ligustrum lucidum secoiridoid glucosides to AP-1/matrix metalloproteinase pathway components

Ligustrum lucidum secoiridoid glucosides have been demonstrated to treat various types of diseases such as inflammation, pain, hepatotoxicity and hyperlipidermic as well as tonic for liver and kidney. Matrix metalloproteinases (MMPs) play a key role upon the pathology of photoaging. The present computational study showed that among the six secoiridoid glucosides (ligustroside, lucidumoside A, lucidumoside C, neonuezhenide, oleoside dimethylester, and oleuropein), ligustroside and lucidumoside A competitively inhibit all MMP-1, MMP-3, and MMP-9 activities in the docking models. The molecular docking analysis revealed a network of interactions between MMP-1, MMP-3, and MMP-9 and the ligands; ligustroside and lucidumoside A, and oxygen-containing and hydrophobic functional groups appear to be responsible for these enhanced interactions. The effect of ligustroside and lucidumoside A on the transcription factor AP-1 action was also investigated using molecular docking and dynamics simulations. The experiments suggested that inhibition of an AP-1–DNA complex formation could be on account of the direct interference of AP-1 binding onto the DNA binding sequence by ligustroside and lucidumoside A. The results suggest that both compounds have the highest potential for application as an anti-aging agent with the MMP inhibitory and anti-transcriptional activities.

Stability and solubility improvement of Sompoi (Acacia concinna Linn.) pod extract by topical microemulsion

Graphical AbstractUnlabelled image