ABSTRACT
A simple method to generate antibacterial peptides by alkaline hydrolysis of hen egg whites is reported. The method reproducibly generates short peptides with molecular weight of less than 14.4 kDa that exhibit low to no cytotoxicity on RAW 264.7 macrophage cells, but do inhibit the bacterial growth of Cutibacterium acnes (C. acnes), Staphylococcus aureus (S. aureus) and antibiotic-resistant S. aureus (MRSA), while also reducing nitric oxide production from heat-killed C. acnes-treated RAW 264.7 cells. Peptidomics revealed at least thirty peptides within the complex mixture, of which eight were evaluated individually. Three peptides (PK8, EE9 and RP8) were potent anti-inflammation and antibacterial agents, but notably the complex egg white hydrolysate (EWH) was more effective than the individual peptides. Electron microscopy suggests the antibacterial mechanism of both the hydrolysate and the selected peptides is through disruption of the cell membrane of C. acnes. These findings suggest that EWH and EWH-derived peptides are promising candidates for infection and inflammation treatment, particularly in managing acne and combating antibiotic-resistant bacteria like MRSA.
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OBJECTIVE: In the development of cosmetic products, sensory evaluation is an important step in determining consumer acceptance before it is released on a market but is often time-consuming and costly. However, correlating sensory characteristics with instrumental parameters using multivariate techniques is a potential way to facilitate the development of cosmetic products. METHODS: Sunscreen formulations varied in the content of grape seed extract (GSE) and ultraviolet (UV) filters, and benchmark products were characterized using sensory descriptive analysis and instrumental analysis. Principal Component Analysis (PCA) was applied to the panel's performance data to study how well the panelists performed compared to each other and to find an association between rheological and textural instrumental parameters of cream samples. Further, applying Partial Least Squares (PLS) regression analysis, the association between sensory attributes and instrumental parameters was analyzed. In addition, a preference for the sensory properties of the studied sunscreen products that are important for consumers living in Southeast Asia was assessed by PLS. RESULTS: In this study, both the sensory and instrumental properties of all tested formulations were described well by PCA. The practicality of PLS was confirmed by an established correlation between sensory attributes from the categories of appearance (glossiness), pick-up (integrity of shape, firmness, glossiness, stringiness), and after-feel (glossiness, spreadability, stickiness) with both rheological and textural parameters. Although the instrumental analysis could not completely replace sensory evaluation, a described method applying PLS can be used as an additional cost-effective and time-saving method during the development of cosmetic products. Moreover, PLS revealed that sunscreens with a light texture and glossy appearance providing smooth skin after-feel are likely to be preferred over the thicker formulations having a residual color appearance in Southeast Asia. CONCLUSION: Until a universal model is created, the cosmetics developers and companies can apply a described method of determining sensory properties from the instrumental parameters of their own products. Future studies will be worth exploiting the applicability of the PLS regression model on instrumental datasets predicting sensory characteristics of other sunscreen products.
OBJECTIF: Dans le développement de produits cosmétiques, l'évaluation sensorielle est une étape importante pour déterminer l'acceptation par le consommateur avant la mise sur le marché, mais elle est souvent longue et coûteuse. Cependant, la corrélation des caractéristiques sensorielles avec les paramètres instrumentaux à l'aide de techniques multivariées est un moyen potentiel afin de faciliter le développement des produits cosmétiques. MÉTHODES: Les formulations d'écrans solaires variants en termes de teneur en extrait de pépins de raisin (EPR) et en filtres ultraviolets (UV), et les produits de référence ont été caractérisés à l'aide d'une analyse sensorielle descriptive et d'une analyse instrumentale. L'analyse en composantes principales (ACP) a été appliquée aux données de performance du panel pour étudier la performance des panélistes les uns par rapport aux autres et pour trouver une association entre les paramètres instrumentaux rhéologiques et texturaux des échantillons de crème. En outre, l'association entre les attributs sensoriels et les paramètres instrumentaux a été analysée au moyen d'une analyse de régression PLS (Partial Least Squares). De plus, une préférence pour les propriétés sensorielles des produits de protection solaire étudiés importantes pour les consommateurs vivant en Asie du Sud-Est a été évaluée par PLS. RÉSULTATS: Dans cette étude, les propriétés sensorielles et instrumentales de toutes les formulations testées ont été bien décrites par l'ACP. L'aspect pratique de l'analyse PLS a été confirmé par une corrélation établie entre les attributs sensoriels des catégories de l'apparence (brillance), de la prise (intégrité de la forme, fermeté, brillance, filant) et de l'impression résiduelle (brillance, capacité d'étalement, adhésivité) avec les paramètres rhéologiques et texturaux. Bien que l'analyse instrumentale ne puisse pas remplacer complètement l'évaluation sensorielle, la méthode décrite appliquant la PLS peut être utilisée comme une méthode supplémentaire rentable et permettant de gagner du temps lors du développement de produits cosmétiques. En outre, l'analyse PLS a révélé que les écrans solaires à la texture légère et à l'aspect brillant, qui procurent une sensation de douceur sur la peau, sont susceptibles d'être préférés aux formulations plus épaisses ayant une couleur résiduelle en Asie du Sud-Est. CONCLUSION: En attendant la création d'un modèle universel, les développeurs et les entreprises de cosmétiques peuvent appliquer une méthode décrite pour déterminer les propriétés sensorielles à partir des paramètres instrumentaux de leurs propres produits. Les études futures devront exploiter l'applicabilité du modèle de régression PLS sur des ensembles de données instrumentales prédisant les caractéristiques sensorielles d'autres produits solaires.
Subject(s)
Cosmetics , Grape Seed Extract , Rheology , Skin , Sunscreening AgentsABSTRACT
BACKGROUND: Sunscreens and catechins from grape seed extract (GSE) are sensitive to various environmental factors and undergo certain changes over time that might affect the effectiveness of the final product. To this date, effects of thermal storage conditions have not been sufficiently addressed to guarantee the long-term stability of sunscreen formulations. AIMS: To study the chemical and mechanical accelerated and long-term stability of sunscreen formulation containing GSE at the Climatic Zone IVb conditions. METHODS: Stability studies were performed for 6 months for accelerated stability study at 30°C ± 2 and 50°C ± 2, 75 ± 5% relative humidity; and long-term stability study at 5°C ± 5. The quantification of constituents of three formulations: sunscreen with GSE, cream with UV filters only, and cream with GSE only was performed by high-performance liquid chromatography. In vitro spectrophotometry was used to determine changes in sun protection effectiveness through SPF and UVAPF values. Mechanical stability was evaluated by textural and rheological analyzes. RESULTS: All tested formulations were less stable at high-temperature conditions. The contents of catechin (С) and epicatechin (EC) in sunscreen with GSE were reduced to 37% and 50% at 50°C, respectively, whereas UV filters appeared to be stable. However, despite the significant reduction in catechins over time, polyphenols in GSE remained unchanged at different stored conditions. The SPF values and water resistance of sunscreen with GSE were maintained throughout the study. CONCLUSIONS: A current in vitro study has shown that sunscreen with GSE is a value-added anti-aging ingredient in sunscreen formulation because its polyphenolic composition as well as SPF values and water resistance were maintained under all temperature conditions over time.
Subject(s)
Grape Seed Extract , Sunscreening Agents , Humans , Sunscreening Agents/chemistry , Grape Seed Extract/chemistry , Spectrophotometry , Ultraviolet Rays , WaterABSTRACT
BACKGROUND: In our previous study, the semi-synthetic analog of andrographolide, 3,19-isopropylideneandrographolide (IPAD), acts more effectively against herpes simplex virus (HSV) infection in cell culture than does acyclovir. IPAD inhibits cytopathic effect and production of HSV wild types and drug-resistant strains. Its effect is associated with the reduction of immediate-early regulatory protein (ICP27) and early proteins (ICP8 and UL42), indicating a mode of action different from that of acyclovir. Therefore, studies of the anti-HSV activity of IPAD in animal models are required before further application. MATERIAL & METHOD: Prednisolone-treated BALB/c mice were cutaneously infected with HSV-1 wild-type KOS strain. Experimental groups included control groups (untreated or treated only with the cream base) and treatment groups (with acyclovir or IPAD creams). Creams were applied four times daily for 10 days after infection to the relevant groups. The skin lesion score was assessed twice a day for 10 days. In addition, the effect of IPAD on HSV copy number and HSV late gene (gD) expression was investigated in skin lesion cells by quantitative real-time polymerase chain reaction. RESULT: IPAD cream was significantly effective in delaying the development of skin lesions and regression of the skin lesion score by day 5 (P < 0.01) compared with untreated controls. In addition, this IPAD cream significantly reduced HSV DNA copy number and gD gene expression (P < 0.01). No signs of irritation were observed at the application site. CONCLUSION: Topical administration of IPAD cream reduced skin lesions in mice cutaneously infected with HSV-1 KOS.
Subject(s)
Herpes Simplex , Herpesvirus 1, Human , Animals , Antiviral Agents/therapeutic use , Disease Models, Animal , Diterpenes , Herpes Simplex/drug therapy , MiceABSTRACT
BACKGROUND: Asian skin undergoing chronological aging, accumulates signs of photoaging mediated by prolonged exposure to ultraviolet (UV) radiation. Although sunscreens are effective in preventing signs of photoaging, polyphenol-rich extracts, for example, grape seed extract (GSE) can provide additional protection through the broad spectrum of biological activities. AIMS: To access the effectiveness of a sunscreen formulation containing GSE as an important cosmetic ingredient for the improvement of age-related changes in Asian skin using noninvasive evaluation techniques. METHODS: Noninvasive methods were used to assess changes in the biophysical properties corresponding to aging signs including melanin and erythema indices, color parameters of the CIE L*a*b* system, elasticity, and hydration of the forearm skin before and after applying the sunscreen with GSE. In addition, to confirm the effectiveness of the tested product, we compared it with benchmark sunscreen, and a cream base containing either GSE or UV filters. RESULTS: Twice-daily application of sunscreen containing 3% GSE significantly reduced the level of melanin and erythema and improved overall skin tone. The hydration was drastically increased after 3 h of wearing formulation and was maintained relatively high for 5 h. Skin elasticity parameters, including Young's modulus, retraction time, and viscoelasticity, improved in participants of all age categories (35-59 years). Moreover, sunscreen with GSE, as acclaimed by participants, improved overall skin appearance. CONCLUSIONS: The balancing potential of GSE on the skin, combined with the photoprotective properties of UV filters demonstrated an added value as an anti-aging agent and proved efficacy for both photo- and chronologically-aged Asian skin.
Subject(s)
Grape Seed Extract , Sunscreening Agents , Humans , Aged , Adult , Middle Aged , Sunscreening Agents/therapeutic use , Melanins , Skin , Ultraviolet Rays/adverse effects , Erythema/drug therapyABSTRACT
PURPOSE: A study of shear wave elastography (SWE) for evaluation of skin stiffness in systemic sclerosis (SSc) patients. The purpose of this study was to measure the skin stiffness and thickness in patients with scleroderma using shear wave elastography. METHODS: Prospective data collections of skin stiffness and thickness using SWE in SSc and control groups. RESULTS: Skin stiffness and thickness were done in 29 patients with SSc and a 29 control population using SWE on bilateral forearms. The SSc patients had thicker skin and higher stiffnesses than the control group. The mean of skin thickness and stiffness using SWE of SSc are 1.74 mm and 47.32 kPa while normal subjects were 1.5 mm and 19.5 kPa. Mean differences were 0.023 mm (95% CI 0.15-0.3, p < 0.001) and 27.82 kPa (95% CI 22.63-33.01, p < 0.001). The dorsal forearms tend to have a higher SWE than the volar forearms in SSc. No statistically significant differences between gender, age or dominancy of skin stiffness were found. SWE has a good correlation with clinical manual palpation of forearms (mRSS) with Spearman rho's of 0.550 (p = 0.002) and 0.508 (p = 0.005) of dominant and non-dominant forearms. CONCLUSION: The application of SWE can be used for evaluation of skin involvement in scleroderma patients with good correlations with the mRSS that was used in the current patients. Furthermore, SWE is a safe technique for either diagnosis or follow up.
Subject(s)
Elasticity Imaging Techniques , Scleroderma, Systemic , Elasticity Imaging Techniques/methods , Humans , Scleroderma, Systemic/diagnostic imaging , Skin/diagnostic imaging , UltrasonographyABSTRACT
This study aimed to investigate the potential of Mangifera indica L. seed kernel extract, which is highly discarded by the global food processing industry, as a multifunctional bioactive ingredient for nutraceutical and cosmeceutical applications. Different extracting solvents were utilized, the extracts were then tested for their antioxidant activities using DPPH, ABTS radical scavenging assays, and inhibition of lipid peroxidation. Additionally, total phenolic content (TPC), total flavonoid content (TFC), and gallic acid content were elucidated using Folin-Ciocalteu and aluminum chloride colorimetric assays, as well as high performance liquid chromatography. The hydroethanolic extract (KMHE) exhibited the highest percentage yield, with the highest antioxidant activity owing to its high phenolic content. KMHE consisted of 773.66 ± 9.42 mg GAE/g extract in TPC, 36.20 ± 4.20 mg RU/g extract in TFC. Additionally, gallic acid was shown to be a major constituent of KMHE. KMHE was investigated for anti-tyrosinase, anti-hyaluronidase, anti-MMP-2, and anti-MMP-9 activities. Moreover, the anti-inflammatory effects of KMHE were studied in RAW 264.7 cells induced by nitric oxide and KMHE was shown to prevent DNA damage, indicating an inhibitory effect on cellular aging. KMHE showed outstanding anti-tyrosinase activity and was as potent an anti-hyaluronidase as gallic acid. Additionally, our results reveal notable anti-MMP-2 and anti-MMP-9 effects that were not significantly different from those of gallic acid. Furthermore, KMHE demonstrated 61.54 ± 2.39% nitric oxide inhibition, with no cytotoxic effects, in RAW264.7 cells, and also prevented DNA damage in the human fibroblast BJ cell line with no cytotoxic effects. Therefore, KMHE could be a promising, natural multifunctional bioactive compound for nutraceutical and cosmeceutical applications.
ABSTRACT
BACKGROUND: Grape seed extract (GSE) is rich in polyphenolic compounds, particularly (+)-catechin (C) and (-)-epicatechin (EC). Strong antioxidant activity of these compounds makes GSE to be value-added to the cosmetics with anti-aging properties. However, a lack of stability in different environmental conditions makes GSE challenging for the development of photostable cosmetic sunscreen products. AIMS: To evaluate photoprotective effects of GSE on human dermal fibroblasts irradiated with UVA light and assess photostability of catechins in cream formulations containing GSE alone or in combination with octyl methoxycinnamate (OMC). METHODS: MTT assay was used to assess protective effects of GSE on fibroblasts irradiated with UVA light. A photostability of C and EC in GSE and in cream formulation containing GSE was investigated using high-performance liquid chromatography and confirmed by reflection and transmission spectrophotometry using Transpore™ tapes and polymethacrylate (PMMA) plates as substrates. RESULTS: High UVA doses damaged fibroblast structure and inhibited their growth. However, GSE increased cell viability and effectively protected them from UVA damage. Photostability of C and EC was achieved by combination of GSE and OMC that also improved absorption capacity of UV filter and increased overall efficacy of formulation. PMMA plates showed better applicability for in vitro photostability testing of sunscreen formulations. However, despite the instability of Transpore® tape under heat from UV exposure, it can still be economically a substrate of alternative choice for screening. CONCLUSIONS: GSE can be used as an effective and sustainable natural resource for prevention of UV-induced skin damage providing long-term protection against premature skin aging.
Subject(s)
Grape Seed Extract , Sunscreening Agents , Drug Stability , Fibroblasts , Grape Seed Extract/pharmacology , Humans , Sunscreening Agents/pharmacology , Ultraviolet Rays/adverse effectsABSTRACT
This study aimed to optimize nanoemulsions loading with Mangifera indica L. kernel extract using response surface methodology for enhancing the stability and skin permeation of the extract. Central composite design was employed for optimization and evaluation of three influencing factors including hydrophile-lipophile balance (HLB), % co-surfactant (PEG-7 glyceryl cocoate), and surfactant-to-oil ratio (SOR) on physical properties of the nanoemulsions. The desired nanoemulsions were then incorporated with the extract and characterized. Physicochemical properties of the extract-loaded nanoemulsions and their antibacterial effects against Propionibacterium acnes were also evaluated after storage at various conditions and compared to those of the initial. Ex vivo skin permeation was also investigated. The factors significantly (p < 0.05) influenced on droplet size, polydispersity index (PDI), and zeta potential, especially HLB of the surfactant and its combined effects with co-surfactant and SOR. The extract-loaded nanoemulsions revealed a very small spherical droplets (size of 26.14 ± 0.22 nm) with narrow size distribution (PDI of 0.16 ± 0.02). The formulation also presented an excellent stability profile and successfully enhanced antibacterial stability of the extract comparing with the extract solution. Ex vivo skin permeation study illustrated that the extract in nanoemulsions could be delivered through a primary skin barrier to reach viable epidermis dermis layers. In conclusion, the affinity of surfactant and hydrophilicity of the system play a crucial role in nanoemulsions' characteristics. Such results might provide promising anti-acne nanoemulsions with the notable capacities of extract stabilization and permeation enhancing which will be further clinically evaluated.
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Calcium alginate (CA) beads loaded with clotrimazole (CZ) were modified by adding poloxamer (PLX) in this study. Blends of PLX188 or PLX407 into sodium alginate (SA) dispersions caused a decrease in the SA zeta potential and led to viscosity synergism. SA with carboxyl and hydroxyl groups can interact with the hydroxyl groups of PLX via hydrogen bonding. A stronger interaction of SA with PLX407 was found when compared to the interaction between SA and PLX188. The PLX-CA beads gave a higher CZ entrapment efficiency than the CA beads. The highest PLX content used created an amorphous form of CZ in the beads because of the CZ solubilization by the PLX micelles. The addition of 0.5 or 1% w/v PLX can strengthen the CZ-loaded CA beads. Furthermore, the PLX-CA beads display a lower water uptake than the CA beads. PLX micellization can enhance CZ release and enhance the efficacy of CZ against Candida albicans. This study indicates that the molecular interaction of SA with PLX and the PLX micellization of CZ can improve the characteristics of CZ-loaded CA beads, which offer good potential for use as drug delivery systems or drug reservoirs in tablets for oral candidiasis.
Subject(s)
Alginates/chemistry , Antifungal Agents/chemistry , Clotrimazole/chemistry , Drug Carriers/chemistry , Poloxamer/chemistry , Surface-Active Agents/chemistry , Candida albicans/drug effects , Drug Compounding , Drug Liberation , Hydrophobic and Hydrophilic Interactions , Micelles , Microspheres , Solubility , Surface Properties , ViscosityABSTRACT
Propionibacterium acnes has been recognized as a main target for medical treatment of acne since this bacterium promotes acne inflammation by inducing upregulation of pro-inflammatory cytokines production, resulting in an accumulation of neutrophils and oxygen-free radicals produced by neutrophils within acne lesion. The aims of this study were to evaluate the biological activities of Mangifera indica kernel extracts grown in Northern Thailand (Kaew-Moragot cultivar), related to anti-acne properties including antimicrobial effect against acne-inducing bacteria together with the first elucidation of the mechanism of action against Propionibacterium acnes, anti-oxidation, and anti-inflammation. The kernels of M. indica, obtained from raw and ripe fruits, were macerated using various solvents. Agar diffusion and broth microdilution methods were performed to investigate the antibacterial activities of the extracts against P. acnes, Staphylococcus aureus, and Staphylococcus epidermidis. The ethanolic fractions exhibited the strongest antimicrobial effect against P. acnes with minimum inhibitory concentration and minimum bactericidal concentration of 1.56â¯mg/mL and 12.50â¯mg/mL, respectively. Bactericidal effect against P. acnes of these extracts could be observed after 3â¯h of incubation from time-kill curve. The chromatograms of high-performance liquid chromatography showed that the extracts existed gallic acid with high total phenolic content. These extracts additionally showed strong free radical scavenging properties on 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) as well as a notable inhibitory effect on linoleic acid peroxidation, which highly correlated to their antimicrobial effect, total phenolic, and gallic acid contents. The images, studied through using transmission electron microscopy, revealed that the extract certainly disrupted P. acnes cell membrane after exposure for 1â¯h as well as induced the consequent leakage of cytoplasmic materials. The inhibitory effects of the extracts on IL-8 secretion from LPS-inducing RAW 264.7â¯cells were also presented. In conclusion, the kernel extracts of raw M. indica fruit were effective against aerobic and anaerobic acne-inducing bacteria particularly P. acnes and exerted antioxidant along with anti-inflammatory activities. Therefore, the extracts might be potential agents for inflammatory acne treatment. However, clinical study is needed for further investigation.
Subject(s)
Acne Vulgaris/microbiology , Anti-Bacterial Agents/pharmacology , Mangifera/chemistry , Plant Extracts/pharmacology , Propionibacterium acnes/drug effects , Chromatography, High Pressure Liquid , Humans , Microbial Sensitivity Tests , Propionibacterium acnes/physiology , Staphylococcus aureus/drug effects , Staphylococcus aureus/physiology , Staphylococcus epidermidis/drug effects , Staphylococcus epidermidis/physiologyABSTRACT
Polysaccharide-protein composites offer potential utility for the delivery of drugs. The objectives of this work were to investigate the molecular interactions between sodium alginate (SA) and sodium caseinate (SC) in dispersions and films and to characterize calcium alginate (CA) beads mixed with SC for the delivery of fluconazole (FZ) and clotrimazole (CZ). The results demonstrated that SA could interact with SC, which caused a viscosity synergism in the dispersions. Hydrogen bonding between the carboxyl or hydroxyl groups of SA and the amide groups of SC led to the formation of soluble complexes that could reinforce the CA beads prepared by calcium cross-linking. The SC-CA beads provided higher drug entrapment efficiency, lower water uptake and erosion, and slower drug release than for the CA beads. The loaded FZ was an amorphous form, but CZ crystals were embedded in the bead matrix due to the low water solubility of this drug. However, SC micellization could enhance the water solubility and efficacy of CZ against Candida albicans. This finding indicates that SA can interact with SC via hydrogen bonding to form complexes and that the anticandidal-loaded SC-CA beads can be used as drug delivery systems and drug reservoirs in tablets for oral candidiasis.
Subject(s)
Alginates/chemistry , Antifungal Agents/chemistry , Candida albicans/drug effects , Caseins/chemistry , Drug Carriers/chemistry , Microspheres , Antifungal Agents/pharmacology , Drug Liberation , Glucuronic Acid/chemistry , Hexuronic Acids/chemistry , Solubility , Water/chemistryABSTRACT
Novel antioxidant and anti-inflammatory peptides were isolated from hydrolysates of Siamese crocodile (Crocodylus siamensis) hemoglobin. C. siamensis hemoglobin hydrolysates (CHHs) were obtained by pepsin digestion at different incubation times (2, 4, 6, and 8 H) at 37 °C and subjected to antioxidant and anti-inflammatory activity assessment. CHH obtained by 2-H hydrolysis (2H-CHH) showed the highest anti-inflammatory activity with respect to decreasing nitric oxide (NO) production, whereas the strongest antioxidant activity was found for 6-H hydrolysis (6H-CHH) against nitric oxide radicals. To evaluate the anti-inflammatory and antioxidant activity of individual peptide components, 2H-CHH and 6H-CHH were purified by semipreparative HPLC. Peptide fraction P57 isolated from 6H-CHH was found to exhibit the highest nitric oxide radical inhibition activity (32.0%). Moreover, purification of 2H-CHH yielded peptide fraction P16, which displayed a high efficacy in decreasing NO production of macrophage RAW 264.7 cells (83.2%) and significantly reduced proinflammatory cytokines and inflammatory mediators interleukin-6 (IL-6), interleukin-1 beta (IL-1ß), and prostaglandin-E2 (PGE2 ) production to about 2.0, 0.3, and 1.9 ng/mL, respectively. Using LTQ orbitrap XL mass spectrometry, active peptide sequences were identified as antioxidant KIYFPHF (KF7), anti-inflammatory SAFNPHEKQ (SQ9), and IIHNEKVQAHGKKVL (IL15). Additionally, CHHs simulated gastric and intestinal in vitro digestion positively contributed to antioxidant and anti-inflammatory activity. Taken collectively, the results of this work demonstrate that CHHs contain several peptides with anti-inflammatory and antioxidant properties, which may prove valuable as treatment or supplement against diseases associated with inflammation and oxidative stress.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Antioxidants/pharmacology , Cytokines/biosynthesis , Hemoglobins/chemistry , Nitric Oxide/biosynthesis , Oligopeptides/pharmacology , Alligators and Crocodiles , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Antioxidants/chemistry , Antioxidants/isolation & purification , Cells, Cultured , Free Radicals/antagonists & inhibitors , Free Radicals/metabolism , Hydrolysis , Macrophages/drug effects , Macrophages/metabolism , Mice , Oligopeptides/chemistry , Oligopeptides/isolation & purification , RAW 264.7 CellsABSTRACT
Lactoferrin chimera (LFchimera), a heterodimeric peptide containing lactoferrampin (LFampin265-284) and a part of lactoferricin (LFcin17-30), possesses a broad spectrum of antimicrobial activity. However, there is no report on the inhibitory effects of LFchimera against multispecies oral biofilms. This study aimed to determine the effects of LFchimera in comparison to chlorhexidine digluconate (CHX) and minocycline hydrochloride (MH), on in vitro multispecies biofilms derived from subgingival plaque of periodontitis patients harboring Aggregatibacter actinomycetemcomitans. First the effects of LFchimera against planktonic and an 1-day old biofilm of the periodontopathic bacteria, A. actinomycetemcomitans ATCC 43718 were established. Then, the effects on biofilm formation and bacterial viability in the multispecies biofilm were determined by crystal violet staining and LIVE/DEAD BacLight Bacterial Viability kit, respectively. The results revealed that a significant reduction (P < 0.05) in biofilm formation occurred after 15 min exposure to 20 µM of LFchimera or CHX compared to control. In contrast, MH at concentration up to 100 µM did not inhibit biofilm formation. The ratio of live/dead bacteria in biofilm was also significantly lower after 15 min exposure to 20 µM of LFchimera compared to control and 20-50 µM of CHX and MH. Altogether, the results obtained indicate that LFchimera is able to inhibit in vitro subgingival biofilm formation and reduce viability of multispecies bacteria in biofilm better than CHX and MH.
Subject(s)
Anti-Bacterial Agents/pharmacology , Antimicrobial Cationic Peptides/pharmacology , Biofilms/drug effects , Periodontitis/microbiology , Aggregatibacter actinomycetemcomitans/drug effects , Aggregatibacter actinomycetemcomitans/physiology , Humans , In Vitro Techniques , Microbial Sensitivity Tests , Microbial Viability/drug effects , Plankton/drug effectsABSTRACT
Formulation of sunscreen products to obtain high values of sun protection factor (SPF) and protection from ultraviolet A (PA) is challenging work for cosmetic chemists. This study aimed to study factors affecting SPF and PA values using ultraviolet transmission spectroscopy as well as texture profiles of sunscreen formulations using 23 factorial designs. Results demonstrate that the correlation coefficient between the labeled SPF values of counter-brand sunscreen products and the in vitro SPF values was 0.901. In vitro SPF determination showed that the combination effect of phase volume ratio (PVR) and xanthan gum caused a significant increase to the SPF values of the formulations, whereas the interaction effect between PVR and stearic acid significantly decreased the SPF value. In addition, there was the interaction effect between xanthan gum and stearic acid leading to significant reduction of hardness, compressibility, and pH, but significantly increasing the adhesiveness. All tested factors did not significantly affect the cohesiveness of tested formulations. In conclusion, apart from sunscreen agents, the other ingredients also affected the SPF and PA values. The calculated SPF values range from 21 to 60. However, a selected formulation needs to be confirmed by the standard method of testing. In addition, the physical, chemical, and biological stability; shelf life; and sensory evaluation of all formulations need to be evaluated.
Subject(s)
Cosmetics/chemistry , Sun Protection Factor , Sunscreening Agents/chemistry , Ultraviolet Rays , Drug Stability , Spectrophotometry, UltravioletABSTRACT
Thunbergia laurifolia Linn (Rang Chuet) possesses antioxidant and anti-inflammatory properties as well as anticancer activities. The aim of the present study was to evaluate the efficacy of T. laurifolia in reducing inflammation from pathological changes in Syrian hamsters infected with the human liver fluke Opisthorchis viverrini. Hamster groups were also administered N-nitrosodimethylamine (NDMA) and treated with T. laurifolia. Light microscopic observation of histopathological changes, liver function tests for alanine transaminase (ALT) and alkaline phosphatase (ALP) and kidney function tests for blood urea nitrogen (BUN) and creatinine were performed. Antioxidant effects of both fresh and dried Rang Chuet solutions were observed. Analysis of the histopathological changes showed anti-inflammatory properties, both in the case of O. viverrini infection or with NDMA administration, by reducing the aggregation of inflammatory cells surrounding the hepatic bile ducts as indicated by normal serum ALT, ALP, BUN and creatinine levels in treated Syrian hamsters. The present study found that fresh and dried Rang Chuet solutions clearly reduced the inflammatory cells in both O. viverrini-infected and NDMA-administered groups and was correlated with the total antioxidant capacity. These findings suggest that T. laurifolia possesses antioxidant and anti-inflammatory properties and that its application may be useful for prevention of the inflammatory process, one of the risk factors of O. viverrini-associated cholangiocarcinoma (CCA).
Subject(s)
Acanthaceae/chemistry , Anthelmintics/administration & dosage , Anti-Inflammatory Agents/administration & dosage , Antioxidants/administration & dosage , Opisthorchiasis/drug therapy , Plant Extracts/administration & dosage , Alanine Transaminase/blood , Alkaline Phosphatase/blood , Animals , Anthelmintics/isolation & purification , Anti-Inflammatory Agents/isolation & purification , Antioxidants/isolation & purification , Creatinine/blood , Cricetinae , Disease Models, Animal , Histocytochemistry , Liver/pathology , Mesocricetus , Microscopy , Opisthorchiasis/parasitology , Opisthorchiasis/pathology , Plant Extracts/isolation & purification , Treatment Outcome , Urea/bloodABSTRACT
Andrographis paniculata has been reported to have antiviral, antipyretic and anticancer activities. Andrographolide, an ent-labdane diterpene, is an active constituent in this plant. In this study, andrographolide (1) and its natural derivative 14-deoxy-11,12-didehydroandrographolide (2) and 5 other semisynthetic derivatives were tested for their activity against Gram-positive and Gram-negative bacteria and Candida albicans. Only derivatives bearing a 14-acetyl group showed activity, and this activity was only against Gram-positive bacteria. 14-Acetylandrographolide showed the highest potency against Bacillus subtilis; the other 14-acetylandrographolides with additional substitution at the 3- and 19-hydroxyl groups showed lower activity against Gram-positive bacteria. The morphology of B. subtilis after being treated with 14-acetylandrographolide was investigated with TEM. This is the first report on 14-acetylandrographolide's quantified antibacterial activity, and the crucial functional group of this ent-labdane that plays an important role in perturbing the morphogenesis of B. subtilis leading to cell death.
Subject(s)
Andrographis/chemistry , Anti-Bacterial Agents/pharmacology , Diterpenes/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Antifungal Agents/chemistry , Antifungal Agents/isolation & purification , Antifungal Agents/pharmacology , Candida albicans/drug effects , Diterpenes/chemistry , Diterpenes/isolation & purification , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effectsABSTRACT
The aims of this study were to investigate the antibacterial activity of lemongrass oil (LG) and its major components which were citral, geraniol and myrcene, against four strains of clinically isolated bovine mastitis pathogens, including Staphylococcus aureus, Streptococcus agalactiae, Bacillus cereus and Escherichia coli by the broth microdilution method, as well as their activity on S. aureus biofilm formation. Attempts to clarify their mechanisms of action by investigation of the effects on intracellular material leakage and morphological changes of S. aureus DMST 4745 were also made. The results demonstrate that S. agalactiae and B. cereus are more susceptible to LG, citral and geraniol than S. aureus and E. coli. Moreover, they also inhibit S. aureus biofilm formation and exhibit effective killing activities on preformed biofilms. The LG appears to have multiple targets in the bacterial cell, depending on concentration used as well as the amount of its components.
Subject(s)
Bacillus cereus/drug effects , Mastitis, Bovine/microbiology , Plant Oils/chemistry , Plant Oils/pharmacology , Staphylococcus aureus/drug effects , Streptococcus agalactiae/drug effects , Terpenes/chemistry , Terpenes/pharmacology , Acyclic Monoterpenes , Animals , Biofilms , Cattle , Dose-Response Relationship, Drug , Escherichia coli/drug effects , Female , Monoterpenes/chemistry , Monoterpenes/pharmacologyABSTRACT
Increasing awareness of hazards associated with the use of antibiotic and chemical agents has accelerated investigations into plants and their extracts as new sources of antimicrobial agents. Therefore, this study aimed at determining the effects of oil and 95% ethanol extracts of Boesenbergia pandurata rhizomes and Piper sarmentosum leaf against four oral pathogens which were Streptococcus mutans, Lactobacillus sp., Aggregatibacter actinomycetemcomitans and Candida albicans. Employing the disc diffusion and broth microdilution methods, the results showed that B. pandurata oil (BPO) was the most effective extract against C. albicans. Time-kill assay with the BPO demonstrated killing of C. albicans at concentrations equal to 2 and 2.5 times the MIC. The times required to reach the fungicidal endpoint at 2 and 2.5 times the MIC were 60 and 44 min, respectively. In addition, our results also demonstrated that the BPO possesses potent anti-Candida biofilm activity in vitro. Therefore, the BPO could be considered as a natural antifungal agent against Candida infections and has significant potential for further investigation.
Subject(s)
Biofilms/drug effects , Piper , Plant Extracts/pharmacology , Zingiberaceae , Anti-Infective Agents/pharmacology , Candida albicans/physiology , Humans , Medicine, Traditional , Microbial Sensitivity Tests/methods , Mouth/microbiology , Plant Extracts/chemistry , Plant Leaves/chemistry , Plant Oils/chemistry , Plant Oils/pharmacology , Rhizome/chemistryABSTRACT
Pods of Acacia concinna (Leguminosae) contain several saponins. In this study, four saponin fractions which were acetone fraction (AAC), aqueous fraction (WAC), hydromethanolic fraction (HAC) and methanolic fraction (MAC) were generated and their haemolytic activities and surface activities were determined in comparison with quillaja saponin (QS). There were no significant differences between the haemolytic activities of MAC and QS. However, the surface tensions of MAC was significantly lower than QS (p < 0.001). Furthermore, the immunomodulatory effect and the adjuvant potential of MAC on the cellular and humoral immune response of BALB/c mice against ovalbumin were investigated. The splenocyte proliferations induced by MAC were significantly higher than QS at the concentrations of 200, 400, 800 and 1000 microg/ml (p < 0.05). BALB/c mice were immunized subcutaneously either with OVA 20 microg alone or with OVA 20 microg combining with QS (10 microg) or MAC (10 and 40 microg). Ten days after the second immunization, concanavalin A (Con A)-, pokeweed mitogen (PWM)-, and OVA-stimulated splenocyte proliferation and OVA-specific antibodies in serum were measured. The results suggested that MAC (40 microg) could activate T and B cells. In addition, OVA-specific IgG, IgG1 IgG2a and IgG2b antibody levels in serum were significantly enhanced by MAC (40 microg) as compared with OVA control group (p < 0.001). This finding suggested that MAC might be effect on Th1 and Th2 helper T cells. In conclusion, the results indicated that MAC at a dose of 40 microg could be used as vaccine adjuvant to increase immune responses.