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Obtaining high-added value compounds from agricultural waste receives increasing attention, as it can both improve resource utilization efficiency and reduce waste generation. In this study, polysaccharides are extracted from the discarded roots of Abelmoschus manihot (L.) by the high-efficiency ultrasound-assisted extraction (UAE). The optimized condition was determined as solid–liquid ratio SL ratio = 1:20, temperature T = 30 °C and time T = 40 min, achieving an extraction yield of 13.41%. Composition analysis revealed that glucose (Glc, 44.65%), rhamnose (Rha, 26.30%), galacturonic acid (GalA, 12.50%) and galactose (Gal, 9.86%) are the major monosaccharides of the extract. The extract showed a low degree of esterification (DE) value of 40.95%, and its Fourier-transform infrared (FT−IR) spectrum exhibited several characteristic peaks of polysaccharides. Inspired by the wide cosmetic applications of polysaccharides, the skincare effect of the extract was evaluated via the moisture retention, total phenolic content (TPC) quantification, 2,2-Diphenyl-1-picrylhydrazyl (DPPH)-free radical scavenging activity, anti-hyaluronidase and anti-elastase activity experiments. The extract solutions demonstrated a 48 h moisture retention rate of 10.75%, which is superior to that of commercially available moisturizer hyaluronic acid (HA). Moreover, both the TPC value of 16.16 mg GAE/g (dw) and DPPH-free radical scavenging activity of 89.20% at the concentration of 2 mg/mL indicated the strong anti-oxidant properties of the extract. Furthermore, the anti-hyaluronidase activity and moderate anti-elastase activity were determined as 72.16% and 42.02%, respectively. In general, in vitro skincare effect experiments suggest moisturizing, anti-oxidant, anti-radical and anti-aging activities of the A. manihot root extract, indicating its potential applications in the cosmetic industry. [ABSTRACT FROM AUTHOR]

Objective: Larvae of Hermitia illucens, or black soldier fly larvae (BSFL), have been recognized for their high lipid yield with a remarkable fatty acid profile. BSFL oil (SFO) offers the added value of a low environmental footprint and a sustainable product. In this study, the characteristics and cosmetic-related activities of SFO were investigated and compared with rice bran oil, olive oil and krill oil which are commonly used in cosmetics and supplements. Methods: The physicochemical characteristics were determined including acid value, saponification value, unsaponifiable matter and water content of SFO. The fatty acid composition was determined using GC-MS equipped with TR-FAME. The in vitro antioxidant properties were determined using DPPH, FRAP and lipid peroxidation inhibition assays. Antihyaluronidase (anti-HAase) activity was measured by detecting enzyme activity and molecular docking of candidate compounds toward the HAase enzyme. The safety assessment towards normal human cells was determined using the MTT assay and the UVB protection upon UVB-irradiated fibroblasts was determined using the DCF-DA assay. The whitening effect of SFO was determined using melanin content inhibition. Results: SFO contains more than 60% polyunsaturated fatty acids followed by saturated fatty acids (up to 37%). The most abundant component found in SFO was linoleic acid (C18:2 n-6 cis). Multiple anti-oxidant mechanisms of SFO were discovered. In addition, SFO and krill oil prevented hyaluronic acid (HA) degradation via strong HAase inhibition comparable with the positive control, oleanolic acid. The molecular docking confirmed the binding interactions and molecular recognition of major free fatty acids toward HAase. Furthermore, SFO exhibited no cytotoxicity on primary human skin fibroblasts, HaCaT keratinocytes and PBMCs (IC50 values > 200 μg/mL). SFO possessed significant in-situ antioxidant activity in UVB-irradiated fibroblasts and the melanin inhibition activity as effective as well-known anti-pigmenting compounds (kojic acid and arbutin, p < 0.05). Conclusion: This study provides scientific support for various aspects of SFO. SFO can be considered an alternative oil ingredient in cosmetic products with potential implications for anti-skin aging, whitening and UVB protection properties, making it a potential candidate oil in the cosmetic industry. [ABSTRACT FROM AUTHOR]

Enicostemma hyssopifolium is a perineal herb widely used as an antidiabetic agent in folklore medicine. The present work was focused on the assessment of its antiinflammatory and cytotoxic properties. Its methanolic extract was evaluated for antiinflammatory activity using murine monocytic macrophage RAW 264.7 cells, and screened for its cytotoxic property in different cancer cell lines. The methanolic extract was able to potentially inhibit the bacterial lipopolysaccharides-induced inflammatory response in RAW 264.7 cells. Results of the cytotoxicity studies revealed that the methanolic extract effectively induced the cytotoxicity at considerably lower concentration in MCF-7, A-549, and COLO-205 cell lines, while the viability of HeLa, CasKi, and HT-29 cells were inhibited at comparatively higher concentrations. Results thus indicated that E. hyssopifolium possessed potent anti-inflammatory and cytotoxic properties. This necessitates further exploration of bioactive phytochemical compounds responsible for these properties for therapeutic applications. [ABSTRACT FROM AUTHOR]

Objective: Larvae of Hermitia illucens, or black soldier fly larvae (BSFL), have been recognized for their high lipid yield with a remarkable fatty acid profile. BSFL oil (SFO) offers the added value of a low environmental footprint and a sustainable product. In this study, the characteristics and cosmetic-related activities of SFO were investigated and compared with rice bran oil, olive oil and krill oil which are commonly used in cosmetics and supplements.Methods: The physicochemical characteristics were determined including acid value, saponification value, unsaponifiable matter and water content of SFO. The fatty acid composition was determined using GC-MS equipped with TR-FAME. The in vitro antioxidant properties were determined using DPPH, FRAP and lipid peroxidation inhibition assays. Antihyaluronidase (anti-HAase) activity was measured by detecting enzyme activity and molecular docking of candidate compounds toward the HAase enzyme. The safety assessment towards normal human cells was determined using the MTT assay and the UVB protection upon UVB-irradiated fibroblasts was determined using the DCF-DA assay. The whitening effect of SFO was determined using melanin content inhibition.Results: SFO contains more than 60% polyunsaturated fatty acids followed by saturated fatty acids (up to 37%). The most abundant component found in SFO was linoleic acid (C18:2 n-6 cis). Multiple anti-oxidant mechanisms of SFO were discovered. In addition, SFO and krill oil prevented hyaluronic acid (HA) degradation via strong HAase inhibition comparable with the positive control, oleanolic acid. The molecular docking confirmed the binding interactions and molecular recognition of major free fatty acids toward HAase. Furthermore, SFO exhibited no cytotoxicity on primary human skin fibroblasts, HaCaT keratinocytes and PBMCs (IC50 values > 200 μg/mL). SFO possessed significant in-situ anti-oxidant activity in UVB-irradiated fibroblasts and the melanin inhibition activity as effective as well-known anti-pigmenting compounds (kojic acid and arbutin, p < 0.05).Conclusion: This study provides scientific support for various aspects of SFO. SFO can be considered an alternative oil ingredient in cosmetic products with potential implications for anti-skin aging, whitening and UVB protection properties, making it a potential candidate oil in the cosmetic industry.

Featured Application: Crude polysaccharide fraction from edible Armillaria mellea might be considered a functional food ingredient of natural origin.Armillaria mellea is a commonly harvested and consumed mushroom in Poland. Several activities of polysaccharides from this species have already been reported. However, polysaccharides from A. mellea growing in the wild in Poland have not yet been investigated. This study was conducted to obtain a crude polysaccharide fraction (AmPS) and investigate its chemical composition and biological properties. Our research suggests that A. mellea is a valuable source of polysaccharides, including β-glucans. 1H NMR and high-performance capillary electrophoresis analysis of AmPS revealed the occurrence of polysaccharides consisted of myo-inositol, mannitol, fucose, galactose, glucose, and mannose. Proteins, uronic acids, and phenolics were present only in trace amounts in the AmPS. The AmPS fraction was found to exhibit strong α-glucosidase inhibitory activity; however, no activity in relation to α-amylase was detected. The fraction was also able to inhibit pro-inflammatory enzymes, i.e., lipoxygenase, cyclooxygenase, and hyaluronidase. Moderate antioxidant and antiradical activity of AmPS was revealed by the ORAC and ABTS assay, respectively. The AmPS fraction was found to have antiproliferative potential against gastric and colorectal cancer cell lines (AGS, HT-29). These findings suggest that AmPS may be considered a health-beneficial food ingredient. Since A. mellea is a commonly known edible mushroom with a long tradition of use, its polysaccharides may be considered safe components for direct consumption or production of nutraceuticals. [ABSTRACT FROM AUTHOR]

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 pg/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 of27.7:28.9:14.6:22.5:3.4:21.7. We modified the SPby 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. [ABSTRACT FROM AUTHOR]

Conifers have long been used as a source of compounds with therapeutic and health-promoting potential, as well as raw materials containing characteristic aromatic and flavour substances. The aim of this study was to characterise the mineral composition of the needles of selected conifers, i.e. Picea abies L., Larix decidua Mill., Pinus sylvestris L., Pseudotsuga menziesii and Juniperus communis L., Abies alba Mill., and to evaluate them as a source of bioactive compounds with antioxidant and inhibitory activity against hyaluronidase evaluated by an in vitro method. The highest total mineral content was found in Abies alba Mill., Pseudotsuga menziesii, while extracts obtained from Picea abies L. and Larix decidua Mill. were characterised by the highest content of phenolic compounds. Extracts from the needles of Larix decidua Mill. showed the highest antioxidant activity in DPPH and FRAP radical assays. The presence of tannins, terpenoids, saponins and coumarins was demonstrated in all the extracts tested by qualitative screening tests. Conifer needles, i.e. needles of Picea abies L., Larix decidua Mill, Abies alba, Pinus sylvestris L., Pseudotsuga menziesii and Juniperus communis L., can be a valuable and ecological source of polyphenols and minerals. [ABSTRACT FROM AUTHOR]

Featured Application: Crude polysaccharide fraction from Rosa rugosa Thunb. root may constitute a potential functional component, e.g., for the pharmaceutical or cosmetic industry.Rosa rugosa Thunb. (Rosaceae) plantations can provide industrial amounts of roots, which contain many biologically active metabolites. Here, we report the first studies of the chemical composition and pharmacological potential of a crude polysaccharide fraction obtained from R. rugosa roots (CPL-Rx). It was found that the roots contained water-soluble and -insoluble sugars, including a large amount of β-glucans (12.95 ± 0.30 g/100 g). The water-soluble fraction was found to be mostly composed of sugars (28.94 ± 0.01%), uronic acids (2.61 ± 0.41%), and polyphenols (4.55 ± 0.12%). High-performance capillary electrophoresis analysis showed that glucose was the prevalent monosaccharide (64.31%), followed by a smaller amount of galactose (11.77%), fructose (11.36%), and arabinose (4.27%). SDS-PAGE followed by liquid chromatography mass spectrometry revealed the presence of unbound protein identified as protein plastid transcriptionally active 14-Like. CPL-Rx was found to inhibit the activity of pro-inflammatory enzymes (cyclooxygenase and hyaluronidase) and to have antioxidant potential in the Trolox equivalent antioxidant capacity assay (0.302 ± 0.01 mmol Trolox/g), DPPH radical scavenging effect (EC50 3.92 ± 0.12 mg/mg DPPH•) and oxygen radical absorbance capacity assay (0.134 ± 0.10 mmol Trolox/g). It also exerted a slight antiproliferative effect on SW480 (colon) and A549 (lung) cancer cell lines. Our research provides the first insights into the composition and pharmacological application of crude polysaccharides from rugosa rose roots. It suggests that CPL-Rx may potentially be used for cosmetic and bio-medical purposes, especially as an antihyaluronidase or chemopreventive agent. [ABSTRACT FROM AUTHOR]

Armillaria mellea is a commonly harvested and consumed mushroom in Poland. Several activities of polysaccharides from this species have already been reported. However, polysaccharides from A. mellea growing in the wild in Poland have not yet been investigated. This study was conducted to obtain a crude polysaccharide fraction (AmPS) and investigate its chemical composition and biological properties. Our research suggests that A. mellea is a valuable source of polysaccharides, including β-glucans. 1H NMR and high-performance capillary electrophoresis analysis of AmPS revealed the occurrence of polysaccharides consisted of myo-inositol, mannitol, fucose, galactose, glucose, and mannose. Proteins, uronic acids, and phenolics were present only in trace amounts in the AmPS. The AmPS fraction was found to exhibit strong α-glucosidase inhibitory activity; however, no activity in relation to α-amylase was detected. The fraction was also able to inhibit pro-inflammatory enzymes, i.e., lipoxygenase, cyclooxygenase, and hyaluronidase. Moderate antioxidant and antiradical activity of AmPS was revealed by the ORAC and ABTS assay, respectively. The AmPS fraction was found to have antiproliferative potential against gastric and colorectal cancer cell lines (AGS, HT-29). These findings suggest that AmPS may be considered a health-beneficial food ingredient. Since A. mellea is a commonly known edible mushroom with a long tradition of use, its polysaccharides may be considered safe components for direct consumption or production of nutraceuticals.

Rosa rugosa Thunb. (Rosaceae) plantations can provide industrial amounts of roots, which contain many biologically active metabolites. Here, we report the first studies of the chemical composition and pharmacological potential of a crude polysaccharide fraction obtained from R. rugosa roots (CPL-Rx). It was found that the roots contained water-soluble and -insoluble sugars, including a large amount of β-glucans (12.95 ± 0.30 g/100 g). The water-soluble fraction was found to be mostly composed of sugars (28.94 ± 0.01%), uronic acids (2.61 ± 0.41%), and polyphenols (4.55 ± 0.12%). High-performance capillary electrophoresis analysis showed that glucose was the prevalent monosaccharide (64.31%), followed by a smaller amount of galactose (11.77%), fructose (11.36%), and arabinose (4.27%). SDS-PAGE followed by liquid chromatography mass spectrometry revealed the presence of unbound protein identified as protein plastid transcriptionally active 14-Like. CPL-Rx was found to inhibit the activity of pro-inflammatory enzymes (cyclooxygenase and hyaluronidase) and to have antioxidant potential in the Trolox equivalent antioxidant capacity assay (0.302 ± 0.01 mmol Trolox/g), DPPH radical scavenging effect (EC50 3.92 ± 0.12 mg/mg DPPH•) and oxygen radical absorbance capacity assay (0.134 ± 0.10 mmol Trolox/g). It also exerted a slight antiproliferative effect on SW480 (colon) and A549 (lung) cancer cell lines. Our research provides the first insights into the composition and pharmacological application of crude polysaccharides from rugosa rose roots. It suggests that CPL-Rx may potentially be used for cosmetic and bio-medical purposes, especially as an antihyaluronidase or chemopreventive agent.

Two triterpene saponins (IPS-1, IPS-2) for the first time were isolated from the roots of Impatiens parviflora DC. (Balsaminaceae). Their anti-inflammatory activity was evaluated by means of two in vitro models: anti-hyaluronidase and anti-denaturation assays. Both saponins were shown to be potent hyaluronidase inhibitors that affect the enzyme in a dose-dependent manner. The anti-hyaluronidase effect of IPS-2 (IC50 = 286.7 µg/mL) was higher than that of the reference drug: escin (IC50 = 303.93 µg/mL). Both saponins protected bovine serum albumin from heat-induced denaturation in a dose-dependent manner. IPS-1 demonstrated higher anti-denaturation effect (IC50 = 86.7 µg/ml) than IPS-2 (IC50 = 109.76 µg/mL) or the standard drug: acetylsalicylic acid (IC50 = 262.22 µg/mL). In conclusion, potent activity of IPS-1, IPS-2 in both in vitro assays shows that saponins from I. parviflora have anti-inflammatory activity. The obtained results allow to suggest that such compounds may be beneficial in inflammatory conditions, especially associated with excessive degradation of hyaluronic acid. [ABSTRACT FROM AUTHOR]

We recently identified a β-agarase, Gaa16B, in the marine bacterium Gilvimarinus agarilyticus JEA5. Gaa16B, belonging to the glycoside hydrolase 16 family of β-agarases, shows less than 70.9% amino acid similarity with previously characterized agarases. Recombinant Gaa16B lacking the carbohydrate-binding region (rGaa16Bc) was overexpressed in Escherichia coli and purified. Activity assays revealed the optimal temperature and pH of rGaa16Bc to be 55 ∘C and pH 6–7, respectively, and the protein was highly stable at 55 ∘C for 90 min. Additionally, rGaa16Bc activity was strongly enhanced (2.3-fold) in the presence of 2.5 mM MnCl2. The Km and Vmax of rGaa16Bc for agarose were 6.4 mg/mL and 953 U/mg, respectively. Thin-layer chromatography analysis revealed that rGaa16Bc can hydrolyze agarose into neoagarotetraose and neoagarobiose. Partial hydrolysis products (PHPs) of rGaa16Bc had an average molecular weight of 88–102 kDa and exhibited > 60% hyaluronidase inhibition activity at a concentration of 1 mg/mL, whereas the completely hydrolyzed product (CHP) showed no hyaluronidase at the same concentration. The biochemical properties of Gaa16B suggest that it could be useful for producing functional neoagaro-oligosaccharides. Additionally, the PHP of rGaa16Bc may be useful in promoting its utilization, which is limited due to the gel strength of agar.

Hyaluronidases (HYALs) are enzymes ubiquitously found in venoms from diverse animals and seem to be related to venom spreading. HYAL activity might be important to Tityus spp. envenoming, since anti- Tityus serrulatus HYAL (TsHYAL) rabbit antibodies neutralize T. serrulatus venom (TsV) lethality. The present work aimed to verify and compare HYAL activity of venoms from other Brazilian Tityus spp. (Tityus bahiensis, Tityus stigmurus and Tityus obscurus) and to test whether anti-TsHYAL antibodies and Brazilian horse therapeutic scorpion antivenom (produced by Fundação Ezequiel Dias (FUNED), Butantan and Vital Brazil Institutes) can recognize and inhibit HYAL activity from these venoms. In ELISA assays, anti-TsHYAL and scorpion antivenoms recognized T. serrulatus, T. bahiensis and T. stigmurus venoms, however, they demonstrated weaker reaction with T. obscurus , which was also observed in Western blotting assay. Epitope mapping by SPOT assay revealed different binding patterns for each antivenom. The assay showed a weaker binding of scorpion antivenom produced by FUNED to peptides recognized by anti-TsHYAL antibodies. Anti-TsHYAL antibodies and antivenoms produced by Butantan and Vital Brazil institutes inhibited HYAL activity of all tested venoms in vitro , whereas FUNED antivenom did not show the same property. These results call attention to the importance of hyaluronidase inhibition, that can aid the improvement of antivenom production. • Tityus scorpion venoms of medical relevance in Brazil show hyaluronidase activity. • Antibodies against T. serrulatus hyaluronidase recognize and neutralize hyaluronidase activity of other Tityus venoms. • Brazilian scorpion antivenoms show different binding patterns towards T. serrulatus hyaluronidase in SPOT assay. • Brazilian scorpion antivenoms also show different hyaluronidase neutralization potential against the tested venoms. [ABSTRACT FROM AUTHOR]

Abstract: BACKGROUND: Guayusa (Ilex guayusa Loes.) leaves, native of the Ecuadorian Amazon, are popularly used for preparing teas. This study aimed to assess the influence of leaf age on the phenolic compounds and carotenoids and the bioactivity and digestibility (in vitro) of aqueous and hydroalcoholic leaf extracts. RESULTS: In total, 14 phenolic compounds were identified and quantified. Chlorogenic acid and quercetin‐3‐O‐hexose were the main representatives of the hydroxycinnamic acids and flavonols respectively. Seven carotenoids were quantified, lutein being the main compound. Ripening affected phenolic content significantly, but there was no significant difference in carotenoid content. Antioxidant capacity, measured by the DPPH• method, was also significantly affected by leaf age. The measurement of in vitro digestibility showed a decrease in phenolic content (59%) as well as antioxidant capacity, measured by the ABTS•+ method, in comparison with initial conditions of the guayusa infusion. Antibacterial and anti‐inflammatory activities were assayed with young leaves owing to their higher phenolic contents. Guayusa did not show any antibacterial activity against Escherichia coli ATCC 25922 or Staphylococcus aureus ATCC 25923. Finally, the hydroalcoholic and aqueous extracts exhibited high in vitro anti‐inflammatory activity (>65%). CONCLUSION: Young guayusa leaves have potential applications as a functional ingredient in food and pharmaceutical industries. © 2017 Society of Chemical Industry [ABSTRACT FROM AUTHOR]

The huge health-beneficial potential of polysaccharides encourages the search for novel sources and applications of these compounds. One poorly explored source of polysaccharides is the rose. The content and biological activity of polysaccharides in rose organs is an almost completely unaddressed topic, therefore, polysaccharide-rich extracts (crude polysaccharides, CPLs) from petals, leaves, hips, and achenes of Rosa rugosa Thunb. were studied for their composition and the influence on various cellular processes involved in the development of cancer and other civilization diseases. The study revealed the presence of water-soluble and -insoluble polysaccharides (including β-glucans) and protein-polysaccharide conjugates in rose organs. Rose hips were found to be the most abundant source of polysaccharides. Different polysaccharide-rich extracts showed the ability to inhibit pro-inflammatory enzymes (COX-1, COX-2, hyaluronidase), a radical scavenging effect (against DPPH• and ABTS•+), and antiproliferative activity (in the A549 lung and SW480 colon cancer cell lines) in in vitro assays. Therefore, rose crude polysaccharides are very promising and can potentially be used as natural chemopreventive agents.

This study evaluated methanol extracts from the leaves and branches of the Thai medicinal plant Diospyros mollis (Ebenaceae). Seven triterpenes and 22 aromatic compounds, including five new compounds, were isolated, and their structures were determined. The new compounds had the following structures: diospyrol glycoside (makluoside A, 1), 8,8′-di- O-6-β- d-apiofuranosyl-β- d-glucopyranosyl-6,6′-dimethyl-2,3′-binaphthalene-1-ol-1′,4′- dione (makluoside B, 2), and 3-methyl-1,8- naphthalenediol glycosides (makluosides C-E, 3- 5). Makluoside B is the first example of a naphthoquinone glycoside that has both a 3-methyl-1,8-naphthalenediol unit and a 5-hydroxy-7-methyl-1,4-naphthoquinone unit. The hyaluronidase inhibitory activity of the isolates was evaluated, revealing that one of the triterpene derivatives possessed moderate inhibitory activity. [ABSTRACT FROM AUTHOR]

The current work presents the development of a nanostructured lipid carrier (NLC) as a colloidal encapsulation and controlled release system for bioactive γ-oryzanol (GO) from rice bran oil. GO-loaded NLC (GO-NLC) were prepared using rice bran oil GO via a hot homogenisation method with sunflower oil (liquid lipid) and stearic acid (solid lipid) as the encapsulating lipid matrix, and rice bran phospholipids and Tween 80 as stabilisers. Fabricated GO-NLC had a 95% encapsulation efficiency with a spherical 'yolk–shell' morphology and a 143 nm mean particle diameter. A 60-day storage stability study showed that GO-NLC had high GO retention (>90%) at ambient temperature in light and dark conditions. In vitro release studies demonstrated that GO can be released from GO-NLC via different modes: slow controlled release into simulated intestinal fluid, following the Korsmeyer-Peppas model, and rapidly into a surfactant solution (Tween 80), following first-order release kinetics. Lastly, in vitro studies showed encapsulation of GO in NLCs afforded an 18-fold increase in free radical-scavenging activity, a two-fold increase in hyaluronidase-inhibitory, and a 200-fold improvement in anti-inflammatory activity. These suggest that GO-NLC is a suitable GO delivery system, which can either perform as an oral extended-release formulation or a rapid-release, surfactant triggered system, with improved health-promoting bioactivities. • GO (payload) and phospholipids (stabiliser) can be extracted from rice bran. • Nanostructured lipid carriers (GO-NLC) can be fabricated for the delivery of GO. • GO-NLCs are spherical "yolk-shell" nanostructures. • GO-NLCs have different release profiles depending on the release media. • GO-NLC enhances the health-promoting bioactivities of γ-oryzanol. [ABSTRACT FROM AUTHOR]

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 IC 50 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., Competing Interests: The authors declare no conflicts of interest, (2023 by The Japanese Society of Applied Glycoscience.)

The chemical compositions of essential oils of Lavandula angustifolia, Lavandula latifolia, Lavandula hybrida cultivar Grosso and cultivar Super, Thymus zygis with high proportions of thymol and linalool and Thymus hyemalis, fromMurcia country (Spain), were studied in relative (%), absolute (mM) and chiral concentrations by GC/MS. Hyaluronidase inhibition and antioxidant activities of the essential oils were evaluated using ABTS.+, DPPH., ORAC, chelating power, hydroxyl radical, nitric oxide, TBARS and reducing power assays. Linalool and linalyl acetate were the most abundant components in the Lavandula genus whereas thymol, linalool and 1,8-cineole were the most abundant molecules in the respective Thymus species. Chiral determination of the main components showed (+)-enantiomers like terpinen-4-ol, β-pinene, borneol and α-terpineol and (-)-enantiomers like linalool, linalyl acetate and camphene in Lavandula sp. In the case of Thymus sp. (+)-enantiomers like α-pinene, limonene, terpinen-4-ol and α-terpineol and (-)-enantiomers like borneol were found. Essential oils containing thymol were found especially powerful in all assays but chelating power, ORAC and hydroxyl radical scavenging assays. The capacity for inhibiting hyaluronidase showed that T. zygis with a high proportion of thymol was the most effective inhibitor. Essential oils containing thymol and linalool/linalyl acetate have a potential use as antioxidant agents. Thymol shows strong inhibition of hyaluronidase. [ABSTRACT FROM AUTHOR]

Inhibition of the necrotizing hyaluronidase, phospholipase A 2 and protease enzymes in four snake venoms by crude water and ethanol extracts of 88 plant species used against snakebites in traditional Chinese medicine was measured. High-resolution hyaluronidase inhibition profiles were constructed for the 22 plants showing highest hyaluronidase inhibition, and the results were used to guide subsequent structural analysis towards specific hyaluronidase inhibitors. Structural analysis was performed by high-performance liquid chromatography, high-resolution mass spectrometry, solid-phase extraction and nuclear magnetic resonance spectroscopy, i.e. , HPLC–HRMS–SPE–NMR. This allowed identification of four non-tannin inhibitors, i.e. , lansiumamide B ( 6 ) from Clausena excavata Burm.f., myricetin 3- O -β- d -glucopyranoside ( 7 ) from Androsace umbellata (Lour.) Merr., and vitexin ( 8 ) and 4′,7-dihydroxy-5-methoxyflavone-8- C -β- d -glucopyranoside ( 9 ) from Oxalis corniculata L. Absolute configuration of 2,3-dihydroxy- N -methyl-3-phenyl- N -[( Z )-styryl]propanamide ( 1 ) was determined using the Mosher method, which revealed two enantiomers, i.e. , ( 2S,3R )-2,3-dihydroxy- N -methyl-3-phenyl- N -[( Z )-styryl]propanamide and ( 2R,3S )-2,3-dihydroxy- N -methyl-3-phenyl- N -[( Z )-styryl]propanamide with a ratio of 7:3. [ABSTRACT FROM AUTHOR]

We recently identified a β-agarase, Gaa16B, in the marine bacterium Gilvimarinus agarilyticus JEA5. Gaa16B, belonging to the glycoside hydrolase 16 family of β-agarases, shows less than 70.9% amino acid similarity with previously characterized agarases. Recombinant Gaa16B lacking the carbohydrate-binding region (rGaa16Bc) was overexpressed in Escherichia coli and purified. Activity assays revealed the optimal temperature and pH of rGaa16Bc to be 55 °C and pH 6–7, respectively, and the protein was highly stable at 55 °C for 90 min. Additionally, rGaa16Bc activity was strongly enhanced (2.3-fold) in the presence of 2.5 mM MnCl2. The Km and Vmax of rGaa16Bc for agarose were 6.4 mg/mL and 953 U/mg, respectively. Thin-layer chromatography analysis revealed that rGaa16Bc can hydrolyze agarose into neoagarotetraose and neoagarobiose. Partial hydrolysis products (PHPs) of rGaa16Bc had an average molecular weight of 88–102 kDa and exhibited > 60% hyaluronidase inhibition activity at a concentration of 1 mg/mL, whereas the completely hydrolyzed product (CHP) showed no hyaluronidase at the same concentration. The biochemical properties of Gaa16B suggest that it could be useful for producing functional neoagaro-oligosaccharides. Additionally, the PHP of rGaa16Bc may be useful in promoting its utilization, which is limited due to the gel strength of agar. [ABSTRACT FROM AUTHOR]

Otostegia fruticosa is traditionally used to treat tonsillitis, stomach ache, asthma, arthritis, and febrile illness in different parts of Ethiopia and other countries. In this experiment 70% ethanolic crude extract and fractions of the leaf of Otostegia fruticosa (Forssk.) Schweinf. ex Penzig were evaluated for their in-vivo anti-inflammatory and analgesic activities and in-vitro hyaluronidase inhibition properties at different concentrations. Tail immersion, acetic acid induced writhing and carrageenan-induced paw edema model were used to assess the in-vivo analgesic and anti-inflammatory activities, respectively. Swiss albino mice of either sex were randomly divided into five groups of six mice per group and for evaluation of the fractions randomly divided into six groups of six mice per group. The test groups were treated with hydroalcoholic extract of Otostegia fruticosa (O. fruticosa) at doses of 100, 200, and 400 mg/kg. The positive control groups received either pethidine 5 mg/kg or aspirin at 100 mg/kg or 150 mg/kg. The negative control groups were orally given sunflower oil. All the fractions were administered at the dose of 400 mg/kg. In all models, the higher dose (400 mg/kg) of the crude extract and chloroform fraction showed a significant central and peripheral analgesic and anti-inflammatory activities with comparable effects to standards used. The hyaluronidase inhibition assay result showed that the test samples displayed concentration-dependent inhibitory activities. These findings indicate that 70% ethanol extract and organic solvent fractions of O. fruticosa leaves have potential analgesic, anti-inflammatory, and enzyme inhibitory activities.

The huge health-beneficial potential of polysaccharides encourages the search for novel sources and applications of these compounds. One poorly explored source of polysaccharides is the rose. The content and biological activity of polysaccharides in rose organs is an almost completely unaddressed topic, therefore, polysaccharide-rich extracts (crude polysaccharides, CPLs) from petals, leaves, hips, and achenes of Rosa rugosa Thunb. were studied for their composition and the influence on various cellular processes involved in the development of cancer and other civilization diseases. The study revealed the presence of water-soluble and -insoluble polysaccharides (including β-glucans) and protein-polysaccharide conjugates in rose organs. Rose hips were found to be the most abundant source of polysaccharides. Different polysaccharide-rich extracts showed the ability to inhibit pro-inflammatory enzymes (COX-1, COX-2, hyaluronidase), a radical scavenging effect (against DPPH• and ABTS•+), and antiproliferative activity (in the A549 lung and SW480 colon cancer cell lines) in in vitro assays. Therefore, rose crude polysaccharides are very promising and can potentially be used as natural chemopreventive agents. [ABSTRACT FROM AUTHOR]

This study aimed to compare the biological activities of 35 herbal hydroethanolic extracts and select high potential extract, which showed antioxidative activity and inhibitory activities of α-glucosidase, lipase, and hyaluronidase, and to investigate the isolation, structural elucidation, and biological activities of five phenolic compounds from the selected extracts of Rosa gallica. On the basis of one-dimensional nuclear magnetic resonance together with the comparison with the literature values, the phenolic compounds were identified as methyl gallate (1), kaempferol-3-O-arabinofuranoside (2), multinoside A acetate (3), kaempferol (4), and quercetin (5), respectively. The results suggest that the extracts from R. gallica show the strongest biological activities in 35 herbal extracts and that 1, 4, and 5 among the five isolated compounds from rose extracts are effective in promoting antioxidative and enzymatic inhibitory activities.