Hyaluronidase Inhibitory Activity Research Articles

Elderberry Leaves with Antioxidant and Anti-Inflammatory Properties as a Valuable Plant Material for Wound Healing.

Sambuci folium (elderberry leaves) have been used in traditional medicine, mainly externally, to treat skin diseases and wounds. Therefore, the aim of this study was to screen the biological activity of elderberry leaves (antioxidant potential and possibility of inhibition of tyrosinase and hyaluronidase enzymes) combined with phytochemical analysis. For this purpose, a phytochemical analysis was carried out. Elderberry leaves of 12 varieties ("Sampo", "Obelisk", "Dwubarwny", "Haschberg", "Haschberg 1", "Koralowy", "Sambo", "Black Beauty", "Black Tower", "Golden hybrid", "Samyl", "Samyl 1") in two growth stages. The compounds from the selected groups, phenolic acids (chlorogenic acid) and flavonols (quercetin), were chromatographically determined in hydroalcoholic leaf extracts. All tested elderberry leaf extracts showed antioxidant effects, but the most promising potential: very high compounds content (TPC = 61.85 mg GAE/g), antioxidant (e.g., DPPH IC50 = 1.88 mg/mL; CUPRAC IC0.5 = 0.63 mg/mL) and optimal anti-inflammatory (inhibition of hyaluronidase activity 41.28%) activities were indicated for older leaves of the "Sampo" variety. Additionally, the extract obtained from "Sampo" and "Golden hybrid" variety facilitated the treatment of wounds in the scratch test. In summary, the best multidirectional pro-health effect in treating skin inflammation was specified for "Sampo" leaves II extract (leaves during the flowering period); however, wound treatment was noted as rich in chlorogenic acid younger leaf extracts of the "Golden hybrid" variety.

Isolation, Characterization, Genome Annotation, and Evaluation of Hyaluronidase Inhibitory Activity in Secondary Metabolites of Brevibacillus sp. JNUCC 41: A Comprehensive Analysis through Molecular Docking and Molecular Dynamics Simulation.

Brevibacillus sp. JNUCC 41, characterized as a plant-growth-promoting rhizobacterium (PGPR), actively participates in lipid metabolism and biocontrol based on gene analysis. This study aimed to investigate the crucial secondary metabolites in biological metabolism; fermentation, extraction, and isolation were performed, revealing that methyl indole-3-acetate showed the best hyaluronidase (HAase) inhibitory activity (IC50: 343.9 μM). Molecular docking results further revealed that the compound forms hydrogen bonds with the residues Tyr-75 and Tyr-247 of HAase (binding energy: -6.4 kcal/mol). Molecular dynamics (MD) simulations demonstrated that the compound predominantly binds to HAase via hydrogen bonding (MM-PBSA binding energy: -24.9 kcal/mol) and exhibits good stability. The residues Tyr-247 and Tyr-202, pivotal for binding in docking, were also confirmed via MD simulations. This study suggests that methyl indole-3-acetate holds potential applications in anti-inflammatory and anti-aging treatments.

Chitosan/Pomegranate Seed Oil Emulgel Composition as a New Strategy for Dermal Delivery of Hydrocortisone.

Multifunctional delivery systems capable of modulating drug release and exerting adjunctive pharmacological activity have attracted particular attention. Chitosan (CS) and pomegranate seed oil (PO) appear to be attractive bioactive components framing the strategy of complex therapy and multifunctional drug carriers. This research is aimed at evaluating the potential of CS in combination with PO in studies on topical emulgels containing hydrocortisone as a model anti-inflammatory agent. Its particular goal was to distinguish alterations in anti-inflammatory action followed with drug dissolution or penetrative behavior between the designed formulations that differ in CS/PO weight ratio. All formulations favored hydrocortisone release with up to a two-fold increase in the drug dissolution rate within first 5 h as compared to conventional topical preparations. The clear effect of CS/PO on the emulgel biological performance was observed, and CS was found to be prerequisite for the modulation of hydrocortisone absorption and accumulation. In turn, a greater amount of PO played the predominant role in the inhibition of hyaluronidase activity and enhanced the anti-inflammatory effect of preparation E-3. Emulgels showed a negligible reduction in mouse fibroblasts' L929 cell viability, confirming their non-irritancy with skin cells. Overall, the designed formulation with a CS/PO ratio of 6:4 appeared to be the most promising topical carrier for the effective treatment of inflammatory skin diseases among the tested subjects.

Ethnomedicinal, Phytochemical, and Pharmacological Properties of Diospyros mollis Griff.: A Review

Objective/Background The genus Diospyros L. (Ebenaceae) includes about 778 species worldwide, with over 500 of them known for their significant health benefits. Among them, Diospyros mollis Griff. has been used as a tonic and treatment for many diseases related to digestive disorders and intestinal parasites. Furthermore, the fruit has also been used for dyeing silk fabrics. The purpose of this comprehensive review is to provide researchers with important information about D. mollis, particularly regarding its chemical composition and biological effects. This information can support current understanding and future studies to develop novel herbal formulations based on this species. Additionally, this review aims to compile and summarize the available literature on this species, covering its botanical, ethnomedicinal, phytochemical, and pharmacological properties reported to date. Methods The relevant information on D. mollis was collected via online electronic and databases, including Scopus, Pubmed, Web of Science, Google Scholar, ScienceDirect, Springer Link, SciFinder, and other scientific databases. Results A comprehensive review of the literature reveals that D. mollis contains various chemical constituents such as naphthalene and naphthoquinone derivatives, triterpenoids, alkaloids, sterols, glycosides, and fatty acid esters isolated from the berry, root, bark, and leaf of this species, with several pharmacological effects and other applications. Many pharmacological effects, such as hyaluronidase inhibitory, anthelmintic, and antiparasitic activities of various extracts and isolated compounds of D. mollis, are reported in this review. The review demonstrates the importance of D. mollis in the treatment of diseases, its application in fabric dyeing techniques, and its traditional use. Conclusion In conclusion, D. mollis emerges as a promising botanical resource with its rich history in traditional medicine and diverse chemical constituents, paving the way for potential future applications and innovations in the field of herbal medicine and drug development.

The Eleutherococcus senticosus fruits' intractum affects changes in the transepithelial electric potential in the distal section of the rabbit's large intestine and inhibits hyaluronidase

Ethnopharmacological relevanceEleutherococcus senticosus (Rupr. et Maxim.) Maxim. has been used in traditional Russian medicine due to its recognized immunostimulant and anti-inflammatory activities. Compounds present in the fruits have demonstrated the capability to modulate the activity of enzymes such as hyaluronidase, suggesting their potential value in the development of effective therapies for various conditions where anti-inflammatory properties are beneficial, such as gastrointestinal diseases and tumor growth. Aim of the studyIn order to support the use of the fruits in folk medicine, this study is aimed to evaluate, post-mortem, the impact of E. senticosus fruits intractum (40 % extract made from fresh fruits) on the transepithelial electrogenic transport of sodium ions in the colon. The objective of this study was also to examine the impact of the intractum on proinflammatory serum hyaluronidase in children diagnosed with acute leukemia. MethodsThe study employed the Ussing technique to examine electrophysiological characteristics of isolated epithelial tissue, using the distal colon wall isolated from 10 New Zealand white male rabbits. The effect of the intractum on the inhibition of human serum hyaluronidase was examined with turbidimetric screening methods, using the blood samples collected from patients diagnosed with acute leukemia. ResultsFor the first time, we discovered that the intractum used in the stimulation fluid, caused hyperpolarization reactions in colon tissue. Statistical analysis showed that these reactions were significantly different in relation to the control. The intractum significantly inhibited hyaluronidase activity with the mean value by group of 60 %, and 40 % for aescin used as a control. ConclusionThe results support the traditional use of the fruits in inflammatory-related diseases. The use of intractum of E. senticosus on the distal colon wall demonstrates its protective effect on the wall integrity and in a relation to hyaluronidase inhibition may additionally indicate its anti-inflammatory property. Thus, the results mean that the intractum may be used in colon-related diseases.

Screening of probiotic Lactobacillus to reduce peanut allergy and with potential anti-allergic activity.

Peanut is a significant source of nutrition and a valuable oilseed crop. It is also a serious allergy source, which poses a threat to 1.1% of the population. This study aimed to screen lactic acid bacteria (LAB) with the capacity to alleviate peanut allergenicity and exhibit anti-allergic properties. The results show that LAB can make use of substances in peanuts to reduce the pH of peanut milk from 6.603 to 3.593-4.500 by acid production and that it can utilize the protein in peanuts to reduce the allergenic content (especially Ara h 1) and improve biological activity in peanut pulp. The content of Ara h 1 peanut-sensitizing protein was reduced by 74.65% after fermentation. The protein extracted from fermented peanut pulp is more readily digestible by gastrointestinal juices. The inhibitory activity assay of hyaluronidase (an enzyme with strong correlation to allergy) increased from 46.65% to a maximum of 90.57% to reveal that LAB fermentation of peanut pulp exhibited a robust anti-allergic response. The strains identified in this study exhibited the ability to mitigate peanut allergenicity partially and to possess potential anti-allergic properties. Lactobacillus plantarum P1 and Lactobacillus salivarius C24 were identified as the most promising strains and were selected for further research. © 2023 Society of Chemical Industry.

Pre-Clinical Evaluation for Anti-Inflammatory, Antioxidant and Antibacterial Potential of Boswellia seratta

Objective: The present study was undertaken to evaluate the anti-inflammatory, anti-oxidant and antibacterial potential of Boswellia serrata extract. Methods: Antioxidant activity was determined using DPPH, Hydroxyl, and Total antioxidant capacity and nitric oxide radical scavenging activities. Anti-inflammatory activity was determined using hyaluronidase enzyme inhibitory assay in which Indomethacin was taken as a reference drug. Agar diffusion was used as a test for antibacterial activity. Grampositive (Staphylococcus aureus) and gram-negative (Escherichia coli) bacteria were chosen for the experiment. As a standard medication, ciprofloxacin was used. Results: Test sample free radical scavenging activity was assessed at 10μg, 50μg, and 100μg concentrations. Results demonstrated dose-dependent inhibition (75.90% at 100μl concentration). Results for hydroxyl radical scavenging activity were compared to Ascorbic acid at concentrations of 10μl, 50μl, and 100μl. Hydoxyl radical scavenging activity was dosedependent like free radical scavenging activity. Inhibition was highest at 100μl concentration (89%), while standard medication Ascorbic acid demonstrated 94.84%.Sample concentrations (10μg, 50μg, and 100μg) were tested for nitric oxide scavenging activity, with maximal scavenging reported. Obtained 87.64% at 100μl concentration, compared to 89.73% for reference medication BHA. Hyaluronidase enzyme inhibition testing results show 84.84 % inhibition at 100μl concentration (Maximum inhibition). Conclusions: Boswellia serrata standard extract shows dose-dependent free radical scavenging and hyaluronidase inhibitory activities.

Improving Solubility and Permeability of Hesperidin through Electrospun Orange-Peel-Extract-Loaded Nanofibers.

Orange peel, which is a rich source of polyphenolic compounds, including hesperidin, is produced as waste in production. Therefore, optimization of the extraction of hesperidin was performed to obtain its highest content. The influence of process parameters such as the kind of extraction mixture, its temperature and the number of repetitions of the cycles on hesperidin content, the total content of phenolic compounds and antioxidant (DPPH scavenging assay) as well as anti-inflammation activities (inhibition of hyaluronidase activity) was checked. Methanol and temperature were key parameters determining the efficiency of extraction in terms of the possibility of extracting compounds with the highest biological activity. The optimal parameters of the orange peel extraction process were 70% of methanol in the extraction mixture, a temperature of 70 °C and 4 cycles per 20 min. The second part of the work focuses on developing electrospinning technology to synthesize nanofibers of polyvinylpyrrolidone (PVP) and hydroxypropyl-β-cyclodextrin (HPβCD) loaded with hesperidin-rich orange peel extract. This is a response to the circumvention of restrictions in the use of hesperidin due to its poor bioavailability resulting from low solubility and permeability. Dissolution studies showed improved hesperidin solubility (over eight-fold), while the PAMPA-GIT assay confirmed significantly better transmucosal penetration (over nine-fold). A DPPH scavenging assay of antioxidant activity as well as inhibition of hyaluronidase to express anti-inflammation activity was established for hesperidin in prepared electrospun nanofibers, especially those based on HPβCD and PVP. Thus, hesperidin-rich orange peel nanofibers may have potential buccal applications to induce improved systemic effects with pro-health biological activity.

Hyaluronidase-inhibiting Polysaccharide from Caulerpa lentillifera.

Algal sulfated polysaccharides are known to be effective hyaluronidase inhibitors. We evaluated hyaluronidase inhibitory activity of sulfated polysaccharide (SP) from Caulerpa lentillifera. Results showed that SP with IC50 of 163 µg/mL appears to allosterically inhibit the hyaluronidase activity. Main sugar composition and sulfate content of SP was estimated to be Gal, Glc, Xyl, Man, uronic acids, and sulfate in the weight percent of 27.7: 28.9: 14.6: 22.5: 3.4: 21.7. We modified the SP by desulfation and partial hydrolysis with trifluoroacetic acid (TFA) to investigate the effect of sulfate content and molecular weight on inhibition. Hyaluronidase inhibitory activity of desulfated SP, 0.1 M TFA-hydrolyzed SP and 0.5 M TFA-hydrolyzed SP were significantly lower than that of native SP, revealing that sulfate content or molecular weight is important for hyaluronidase inhibition.

A Comprehensive Study on the Anti-cancer Effects of Quercetin and Its Epigenetic Modifications in Arresting Progression of Colon Cancer Cell Proliferation

Colon cancer etiology involves a wide spectrum of genetic and epigenetic alterations, finding it challenging to find effective therapeutic strategies. Quercetin exhibits potent anti-proliferative/apoptotic properties. In the present study, we aimed to elucidate the anti-cancer and anti-aging effect of quercetin in colon cancer cell lines. The anti-proliferative effect of quercetin was assessed in vitro by CCK-8 in normal and colon cancer cell lines. To check the anti-aging potential of quercetin, collagenase, elastase, and hyaluronidase inhibitory activity assays were performed. The epigenetic and DNA damage assays were performed using the human NAD-dependent deacetylase Sirtuin-6, proteasome 20S, Klotho, Cytochrome-C, and telomerase ELISA kits. Furthermore, the aging-associated miRNA expression profiling was performed on colon cancer cells. The treatment with quercetin inhibited cell proliferation of colon cancer cells in a dose-dependent manner. Quercetin arrested colon cancer cell growth by modulating expression of aging proteins including Sirtuin-6 and Klotho and also by inhibiting telomerase activity to restrict the telomere length which is evident from qPCR analysis. Quercetin also exhibited DNA damage protection by reducing proteasome 20S levels. The miRNA expression profiling results displayed differential expression of miRNA in colon cancer cell, and in addition, the highly upregulated miRNA was involved in the regulation of cell cycle, proliferation, and transcription. Our data suggest that quercetin treatment inhibited cell proliferation in colon cancer cells through regulating the anti-aging protein expression and provides better understanding for quercetin’s potential use in colon cancer treatment.

Fast and efficient identification of hyaluronidase specific inhibitors from Chrysanthemum morifolium Ramat. using UF-LC-MS technique and their anti-inflammation effect in macrophages

The purpose of the study was to establish a rapid analytical strategy to screen potential anti-inflammatory compounds from Flos Chrysanthemum flower. The enzyme assay was conducted to prescreen botanical extracts, in which Chrysanthemum morifolium aqueous extract (CME) displayed hyaluronidase (HAase) inhibitory activity in a dose-dependent manner with the values of 8.31, 24.25, and 66.51% at concentrations of 1.00, 2.00, and 4 0.00 mg/mL, respectively. Eight potential compounds targeting HAase (compounds 9, 10, 11, 13, 15, 17, 20 and 21) from CME were screened using ultrafiltration affinity liquid chromatography coupled with mass spectrometry (UF-LC-MS) technology. The well-known inhibitor, dipotassium glycyrrhizinate (DG), was used as a positive control and competitive ligand to eliminate false positives. Then, four of these potential components (compounds 9, 10, 17, and 21), namely eriodictyol-7-O-glucoside, luteoloside, apigenin-7-O-glucoside and diosmetin-7-O-glucoside, were distinguished as potent HAase specific inhibitor candidates with high BD and CBD values. The enzyme inhibitory activities of candidate compounds were verified using enzyme inhibition assay. At a concentration of 1000 μM, compounds 9, 10, 17, and 21 showed 40.15, 44.85, 18.04, and 24.15% inhibition of HAase, respectively. Furthermore, all the four compounds significantly decreased the production of nitric oxide (NO) and IL-6, and significantly suppressed the mRNA expression of inducible NO synthase (iNOS) and IL-1β in both murine and human macrophages.

Isolation and Characterization of Collagen and Collagen Peptides with Hyaluronidase Inhibition Activity Derived from the Skin of Marlin (Istiophoridae).

Type I and V collagens are the major components of fibrillogenic proteins in fish skin, and their hydrolysis products possess hyaluronidase inhibitory activity. In this study, for the first time, type I and V collagens were isolated from the skin of shortbill spearfish and striped marlin. Type I (2α1[I]α2[I]) and type V (α1[V]α3[V]α2[V]) collagens composed of distinct α-peptide chains with comparable structures were investigated using sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) and UV spectrophotometric chromatography. After enzymatic digestion, the collagen peptides were purified by using ultrafiltration (30 KDa) and high-performance liquid chromatography (RP-HPLC) to yield CPI-F3 and CPV-F4 fractions with strong hyaluronidase inhibition rates (42.17% and 30.09%, respectively). Based on the results of simulated gastrointestinal fluid, temperature, and pH stability assays, CPI-F3 and CPV-F4 exhibited stability in gastric fluid and showed no significant changes under the temperature range from 50 to 70 °C (p > 0.05). The results of this first research on the bioactivity of type V collagen peptides provide valuable information for the biomedical industry and show the potential for future bioactivity investigations of type V collagen and its peptides.

Salicornia ramosissima: A New Green Cosmetic Ingredient with Promising Skin Effects.

This study aims to validate a new cosmetic ingredient from Salicornia ramosissima S J. Woods through in vitro and ex vivo assays. The halophyte extracts were obtained by subcritical water extraction (SWE) at different temperatures (110, 120, 140, 160 and 180 °C). The antioxidant/radical scavenging activities and the phenolic profile were screened for all extracts. The optimal extract was assessed in keratinocytes and fibroblasts, while permeation assays were performed in Franz cells. The inhibitory activity of hyaluronidase and elastase was also evaluated. The sample extracted at 180 °C presented the highest phenolic content (1739.28 mg/100 g of dry weight (dw)). Despite not being efficient in the sequestration of ABTS•+, this extract scavenged the DPPH• (IC50 = 824.57 µg/mL). The scavenging capacity of superoxide (O2•-) and hypochlorous acid (HOCl) was also considerable (respectively, IC50 = 158.87 µg/mL and IC50 = 5.80 µg/mL). The cell viability assays confirmed the absence of negative effects on keratinocytes, while the fibroblasts' viability slightly decreased. The ex vivo permeation of rutin, quercetin and syringic acid after 24 h was, respectively, 11, 20 and 11%. Additionally, the extract showed a good elastase and hyaluronidase inhibitory activity. The results obtained support the S. ramosissima bioactivity as a cosmetic ingredient.

까치버섯(Polyozellus multiplex) 추출물의 생리활성과 이를 첨가한 양갱의 이화학적 및 관능적 품질 특성

Total phenol content (TPC) of Polyozellus multiplex was the highest at 97.22±0.91 mg/g when extracted with 70% ethanol. ABTS radical cation decolorization of both water and 70% ethanol extract samples was greater than 95.00%. The TBARS inhibition activity of P. multiplex extracted with 70% ethanol was higher than that of water extract samples and anti-oxidation activity was identified as 80% or more at 50-200 μg/mL TPC concentration. The α-glucosidase inhibitory activity of P. multiplex showed above 85.0% in both water and 70% ethanol extracts at 150 μg/mL phenolics. Hyaluronidase inhibitory activity was 46.28% and 27.52% in the water and 70% ethanol extracts at 200 μg/mL TPC concentration, respectively. The white and red yanggaeng color values of L, a, and b were all changed with the added extracted powder. Rheological analysis of hardness, springiness, and chewiness, demonstrated decreases as the extracted powder content increased. However, as the added extracted powder increased, cohesiveness was not affected. As a result of the sensory test, it was determined that for white and red yanggaeng, the addition of 0.5% (white) and 1.0% or less (red) of the extracted powder is appropriate, respectively. Considering the intrinsic color of P. multiplex powder extracts, it is thought that it may be desirable to manufacture it based on red yanggaeng. Therefore, it was thought that can be expected biological activities of yanggaeng prepared with P. multiplex extracted powder.

In vitro biological activities and preliminary phytochemical screening of different extracts from Achillea sintenisii Hub- Mor

This study was designed to investigate in vitro biological activities and phytochemical composition of aqueous and ethanolic extracts from Achillea sintenisii Hub- Mor. (AS). To determine the chemical composition of AS extracts, phytochemical analyses were performed by using HPLC–ESI-Q-TOF-MS-MS. Afterwards, both extracts were investigated in terms of their effect on fibroblast proliferation, collagen synthesis, and hydrogen peroxide-induced damage. In addition to cell culture analysis, antibacterial, antioxidant, hyaluronidase inhibitory activities and total phenolic contents of the extracts were analyzed in cell-free systems. Our results demonstrated that the aqueous and ethanolic extracts did not show cytotoxic activity on fibroblasts, on the contrary, promoted fibroblast proliferation. Both AS extracts potently inhibited hyaluronidase activity and the inhibitory effect of ethanolic extract was comparable with the positive control, especially at high concentrations. The aqueous extract was the potent stimulator of collagen synthesis at 200 µg/mL concentration. Although the ethanolic extract showed antibacterial activity against all gram-positive bacteria, the aqueous extract was only effective against K. pneumoniae and B. subtilis. The ability of AS extracts, which have a rich phenolic compound content (≥50 mg GAE/g), to scavenge free radicals and protect fibroblasts against hydrogen peroxide-induced damage can be considered as a result of their antioxidant potential. Our findings scientifically support the widespread use of this plant, by demonstrating the pharmacological properties of the extracts.

Hyaluronidase Inhibitory Activity and In Silico Docking Study of New Eugenol 1,2,3‐triazole Derivatives

AbstractChemical transformation study is considered as an important tool for new drugs discovery. It was conducted on the natural compound eugenol for semi‐synthesizing new structural scaffolds. Three new eugenol 1,2,3‐triazole derivatives as well as a known one were synthesizedviaclick chemistry using the Cu(I)‐catalyzed azide–alkyne 1,3‐dipolar cycloaddition method. All derivatives were characterized by NMR analysis in combination with ESIMS. Molecular docking andin vitroinhibition potency of eugenol and its derivatives towards hyaluronidase enzyme were examined. The synthesized derivative 4‐((4‐allyl‐2‐methoxyphenoxy)methyl)‐1‐benzyl‐1H‐1,2,3‐triazole showed an enhanced hyaluronidase inhibitory effect, 1.5 times, higher than its parent compound eugenol.

Polyphenolic Characterization, Antioxidant, Antihyaluronidase and Antimicrobial Activity of Young Leaves and Stem Extracts from Rubus caesius L.

Fruits are the main food part of the European dewberry (Rubus caesius L.), known as a source of polyphenols and antioxidants, while very little attention is paid to leaves and stems, especially young first-year stems. The purpose of this work was to analyze for the first time water and ethanol extracts obtained from young, freshly developed, leaves and stems of the European dewberry to determine their antioxidant and biological activity, whereas most of the papers describe biological properties of leaves collected during summer or autumn. As the phytochemical profile changes during the growing season, the quantitative and qualitative content of flavonoid glycosides and flavonoid aglycones was analyzed using reversed phase liquid chromatography/electrospray ionization triple quadrupole mass spectrometry (LC-ESI-MS/MS) with multiple reaction monitoring (MRM). The ability to inhibit hyaluronidase as well as antioxidant activity (2,2 diphenyl-1-picrylhydrazyl: DPPH and ferric antioxidant power: FRAP) were estimated. Extracts were also analyzed against Gram-positive and Gram-negative bacteria. The results of the qualitative phytochemical analysis indicated the presence of flavonoid aglycones and flavonoid glycosides, with the highest amount of tiliroside, hyperoside, isoquercetin, astragalin, rutin and catechin in ethanol extracts. DPPH and FRAP tests proved the high antioxidant activity of the extracts from leaves or stems and the antihyaluronidase assay revealed for the first time that water and ethanol extracts obtained from the stems exhibited the ability to inhibit hyaluronidase activity resulting in an IC50 of 55.24 ± 3.21 and 68.7 ± 1.61 μg/mL, respectively. The antimicrobial activity has never been analyzed for European dewberry and was the highest for Clostridium bifermentans and Clostridium sporogenes—anaerobic sporulation rods as well as Enterococcus faecalis for both water and ethanol extracts.

Evaluation of biosafety and skin-care efficacy for “Four white” medicinal materials used in cosmetics

ObjectiveTo verify the antioxidant, whitening and anti-inflammatory effects of “Four white” extracts in cosmetic applications. MethodsThe extracts of the Chinese herbal medicines “Four white” (Silkworm Larva, Japanese Ampelopsis root, Largehead Atractylodes rhizome. White peony root) were prepared by an alcoholic extraction method. The safety and irritation of the extracts were assessed by the erythrocyte hemolysis test and MTT. The antioxidant ability of the extracts was determined by measuring their capabilities to scavenge hydroxyl and DPPH radicals, reduce iron ions and cellular antioxidant assays. The whitening capability was determined by the ability of tyrosinase inhibition. Its anti-inflammatory capacity was determined by measuring the inhibiting rates against hyaluronidase and lipopolysaccharide (LPS)-induced NO production in RAW264.7 cells. ResultsThe results of the irritation test showed that the “Four white” extract has low irritation and high biosafety. It can scavenge different free radicals and has protective effect against oxidative damage. The tyrosinase inhibition test showed that the extracts had whitening ability. In terms of anti-inflammatory activity, it can inhibit hyaluronidase activity to a certain extent and reduce the production of NO by LPS-stimulated cells. Conclusion“Four white” extract has high biosafety and skin-care efficiency such as antioxidant, whitening and anti-inflammatory properties.

Antiallergic Properties of Biflavonoids Isolated from the Flowers of Mesua ferrea Linn.

The methanolic extract from the flowers of Mesua ferrea Linn. (Calophyllaceae) showed significant hyaluronidase inhibitory activity. Following a bioassay-guided separation of the extract, two biflavonoids, viz., mesuaferrone-A (1) and mesuaferrone-B (2), were isolated, along with ten flavonoids (3–12), two xanthones (13 and 14), three triterpenes (15–17), a phenylpropanoid (18), and five aromatics (19–24). Among the isolates, 1 and 2 (IC50 = 51.1 µM and 54.7 µM, respectively) exhibited hyaluronidase inhibitory activity equivalent to that of the commercially available antiallergic agents disodium cromoglycate (64.8 μM) and ketotifen fumarate (76.5 μM). These biflavonoids (1 and 2) are 8-8″ linked dimers that are composed of naringenin (1a) or apigenin (3), with their corresponding monomers lacking inhibitory activity (IC50 > 300 μM). In addition, 1 and 2 (IC50 = 49.4 µM and 49.2 µM, respectively) inhibited the release of β-hexosaminidase, which is a marker of antigen-IgE-mediated degranulation, in rat basophilic leukemia (RBL-2H3) cells. These inhibitory activities were more potent than those of the antiallergic agents tranilast and ketotifen fumarate (IC50 = 282 μM and 158 μM, respectively), as well as one of the corresponding monomers (1a; IC50 > 100 μM). Nonetheless, these effects were weaker than those of the other monomer (3; IC50 = 6.1 μM).

Synthesis and Biological Evaluations of Betulinic Acid Derivatives With Inhibitory Activity on Hyaluronidase and Anti-Inflammatory Effects Against Hyaluronic Acid Fragment Induced Inflammation.

We previously reported that the structural modifications of pentacyclic triterpenoids including oleanolic acid resulted in enhanced hyaluronidase inhibitory activity but whether this applies to other pentacyclic triterpenoids such as betulinic acid (BA) is unknown. Herein, we synthesized BA derivatives with an α,β-unsaturated ketene moiety and evaluated for their: 1) hyaluronidase inhibitory activity and, 2) anti-inflammatory effects against lipopolysaccharides (LPS) induced inflammation. Compared to BA, the BA derivatives exerted improved anti-hyaluronidase activity (26.3%–72.8% vs. 22.6%) and anti-inflammatory effects by reducing nitrite production in BV2 cells (3.9%–46.8% vs. 3.4%) and RAW264.7 cells (22.7%–49.2% vs. 20.4%). BA derivatives inhibited LPS-induced production of pro-inflammatory cytokines in THP-1 cells (15.2%–22.4%). BA derivatives also exerted promising anti-inflammatory effects against hyaluronic acid fragment induced nitrite production (8.6%–35.6%) in THP-1 cells. BA derivatives showed augmented anti-hyaluronidase and anti-inflammatory effects but further biological evaluations using in vivo models are warranted to confirm their efficacy.