4-Hydroxyderricin from Angelica keiskei: Analysis, Preparation, and Multiple Skin Care Effects
Introduction: The content of the bioactive component 4-hydroxyderricin (4-HD) in the roots, stems, and leaves of Angelica keiskei (Umbelliferae), a well-known medicinal and edible plant, was analyzed by HPLC. The dry root contained the highest level (2. 69 ± 0.09 mg/g) of 4-HD, which was then prepared and spectroscopically identified by column chromatography. Methods: The multiple skin care activities of 4-HD, including skin whitening, anti-allergy, and antiinflammation, were evaluated on enzymatic and cellular models. 4-HD showed a significant inhibitory effect on mushroom tyrosinase, and it could also strongly suppress the activity of tyrosinase in B16F10 cells. A molecular docking study revealed that 4-HD could closely bind to tyrosinase through hydrogen bonding and hydrophobic interactions. Results: In the anti-allergic assay, 4-HD could effectively reduce the degranulation rate in the neutral red staining test and largely down-regulate the release level of β-HEX in RBL-2H3 cells at the concentration of 5 μM. 4-HD decreased the production of NO in RAW264.7 cells induced by lipopolysaccharide (LPS), showing its anti-inflammatory effect. Conclusion: The skin whitening, anti-allergic, and anti-inflammatory effects of 4-HD have clearly demonstrated its potential usage in the pharmaceutical and cosmetic industries.
- Research Article
3
- 10.15188/kjopp.2020.04.34.2.67
- Apr 25, 2020
- Journal of Physiology & Pathology in Korean Medicine
The objective of this study is to investigate the skin whitening and antioxidant effects of the Anemarrhenae Rhizoma extract (ARE). Following the previously studied method, we examined the inhibitory effects of melanin synthesis and tyrosinase activity by using B16F10 cells. First, we measured the Diphenylpicrylhydrazyl (DPPH) assay, nitrite scavenging activity, and superoxide dismutase-like activity to verifying antioxidant efficacy according to skin whitening. In addition, we confirmed the skin whitening efficacy of ARE by measuring gene expression associated with a skin whitening by the Reverse transcription polymerase chain reaction (RT-PCR) method in B16F10 cells. In this study, we confirmed that ARE has skin whitening and antioxidant effects at high concentrations. In particular, ARE at a concentration of 500 ㎍/ml inhibited the expression of Tyrosinase, TRP-2 (tyrosinase-related protein), and MITF (microphthalmia transcription factor) genes better than Arbutin. In conclusion, our results confirmed that ARE has the potential for development as a skin whitening efficacy substance.
- Research Article
3
- 10.3390/nutraceuticals3010006
- Jan 12, 2023
- Nutraceuticals
The various clinical approaches for treating allergy-related diseases have shown modest progress in low side effects and improved clinical outcomes. Therefore, finding alternative anti-allergic agents is crucial. The present study explored the anti-allergic effects of amber extract (fossilized tree resin) in RBL-2H3 mast cells stimulated with different allergens. In order to support the information on the inflammatory effect of the amber extract, NO production analysis on RAW 264.7 cells was conducted. β-Hexosaminidase release, an indicator of the efficacy of the amber extract in preventing mast cell activation and degranulation, reactive oxygen species (ROS) generation, and the effect of the amber extract on key cytokines production on RBL-2H3 cells, was evaluated. The results demonstrated that amber extract at concentrations up to 50 μg/mL had no cytotoxic effect on RAW 264.7 and RBL-2H3 cells. Amber extract inhibited NO production in RAW 264.7 cells. Treatment with amber extract significantly suppressed the release of β-hexosaminidase, especially at 50 μg/mL. Furthermore, amber extract suppressed the significantly increased ROS levels induced by allergen stimulation and allergy-associated cytokines. The results also suggested that amber extract exerts anti-allergic inflammatory effects by inhibiting the MAPK and NF-κB signaling pathways, resulting in decreased cytokines production. Thus, the amber extract is a promising anti-allergic agent.
- Research Article
21
- 10.1016/j.phytochem.2020.112630
- Dec 27, 2020
- Phytochemistry
Sesquiterpene derivatives from the agarwood of Aquilaria malaccensis and their anti-inflammatory effects on NO production of macrophage RAW 264.7 cells
- Research Article
75
- 10.1016/j.bmcl.2011.09.128
- Oct 7, 2011
- Bioorganic & Medicinal Chemistry Letters
Alkaloids from Chelidonium majus and their inhibitory effects on LPS-induced NO production in RAW264.7 cells
- Research Article
2
- 10.3390/ijms25179353
- Aug 29, 2024
- International journal of molecular sciences
Milk boasts an array of potent bioactive compounds, such as lactoferrin (Lf), immunoglobulins, and functional proteins, all delivering substantial therapeutic benefits. In this study, Immune Powder (a functional dairy formulation) and its primary component called Fractionated Milk Protein (FMP) containing Lf, zinc, and immunoglobulins and formulated by Ausnutria Pty Ltd. were evaluated for their potential broad-spectrum pharmacological activity. In particular, this study investigated the antibacterial (against pathogenic Escherichia coli), prebiotic (promoting Lactobacillus delbrueckii growth), anti-inflammatory (inhibition of NO production in RAW264.7 macrophages), and antiviral (against human coronavirus 229E) effects of the samples. In addition, the impact of simulated gastric digestion on the efficacy of the samples was explored. LCMS-based proteomics was implemented to unveil cellular and molecular mechanisms underlying antiviral activity. The Immune Powder demonstrated antibacterial activity against E. coli (up to 99.74 ± 11.47% inhibition), coupled with prebiotic action (10.84 ± 2.2 viability fold-change), albeit these activities diminished post-digestion (p < 0.01). The Immune Powder effectively mitigated NO production in lipopolysaccharide-stimulated RAW264.7 macrophages, with declining efficacy post-digestion (p < 0.0001). The Immune Powder showed similar antiviral activity before and after digestion (p > 0.05) with up to 3-fold improvement. Likewise, FMP exhibited antibacterial potency pre-digestion at high concentrations (95.56 ± 1.23% inhibition at 125 mg/mL) and post-digestion at lower doses (61.82 ± 5.58% inhibition at 3906.25 µg/mL). FMP also showed enhanced prebiotic activity post-digestion (p < 0.0001), NO inhibition pre-digestion, and significant antiviral activity. The proteomics study suggested that the formulation and its primary component shared similar antiviral mechanisms by inhibiting scavenger receptor binding and extracellular matrix interaction.
- Research Article
1
- 10.20402/ajbc.2021.0229
- Dec 29, 2021
- Asian Journal of Beauty and Cosmetology
Purpose: This research verified the skin whitening and moisturizing effects of hydrolyzed swiftlet nest extracts (HSNE) in vitro using human keratinocytes and melanoma.Methods: To confirm the antioxidant effect of HSNE, DPPH radical-scavenging activity was measured. To find out the whitening effect of HSNE, the genes related to melanogenesis, mRNA expression of tyrosinase (TYR), tyrosinase related protein (TRP) 1, 2 and microphthalmia associated transcription factor (MITF) were measured. We also measured the melanin contents after treatment of HSNE to confirm the anti-melanogenesis effect. Using reverse transcription polymerase chain reaction (RT-PCR), the genes related to moisturizing such as aquaporin (AQP) 3, hyaluronan synthase (HAS) 1, 2, and 3 were determined. The results of the tests were analyzed with student’s t-test and expressed as mean±standard deviation.Results: DPPH radical scavenging effects of HSNE increased in a concentration dependent manner. The expression of melanogenesis-related genes were inhibited by the treatment of HSNE in a concentration-dependent manner (MITF, TYR, TRP1, and 2). Melanin contents also decreased with the treatment of HSNE. The expression of moisturizing-related genes (HAS1, 2, 3, and AQP3) increased in a concentration-dependent manner.Conclusion: It is confirmed that the hydrolyzed swiftlet nest extracts have skin whitening and moisturizing effects and can be used as a functional cosmetic raw material.
- Research Article
206
- 10.1111/ics.12728
- Aug 28, 2021
- International Journal of Cosmetic Science
Skin, our first interface to the external environment, is subjected to oxidative stress caused by a variety of factors such as solar ultraviolet, infrared and visible light, environmental pollution, including ozone and particulate matters, and psychological stress. Excessive reactive species, including reactive oxygen species and reactive nitrogen species, exacerbate skin pigmentation and aging, which further lead to skin tone unevenness, pigmentary disorder, skin roughness and wrinkles. Besides these, skin microbiota are also a very important factor ensuring the proper functions of skin. While environmental factors such as UV and pollutants impact skin microbiota compositions, skin dysbiosis results in various skin conditions. In this review, we summarize the generation of oxidative stress from exogenous and endogenous sources. We further introduce current knowledge on the possible roles of oxidative stress in skin pigmentation and aging, specifically with emphasis on oxidative stress and skin pigmentation. Meanwhile, we summarize the science and rationale of using three well-known antioxidants, namely vitamin C, resveratrol and ferulic acid, in the treatment of hyperpigmentation. Finally, we discuss the strategy for preventing oxidative stress-induced skin pigmentation and aging.
- Research Article
2
- 10.1016/j.jep.2025.119359
- Feb 1, 2025
- Journal of ethnopharmacology
5β-hydroxycostic acid from Laggera alata ameliorates sepsis-associated acute kidney injury through its anti-inflammatory and anti-ferroptosis effects via NF-κB and MAPK pathways.
- Research Article
3
- 10.1016/j.phytol.2021.08.010
- Oct 1, 2021
- Phytochemistry Letters
Anti-inflammatory quinolizidine alkaloids from the aerial parts of Sophora tonkinensis
- Research Article
23
- 10.1186/s41240-019-0126-3
- May 31, 2019
- Fisheries and Aquatic Sciences
BackgroundIn the present study, the skin-whitening effects of a marine-sourced mixture that includes a fucoidan-rich extract of Undaria pinnatifida (UPEF), a phlorotannin-rich extract of Ecklonia cava (ECE), and glycosaminoglycans (GAGs) from sea squirt skin were investigated.MethodsThe whitening effects of the mixture and its components were evaluated by measuring the inhibition of mushroom tyrosinase and melanin synthesis in alpha-melanocyte-stimulating hormone (α-MSH)-stimulated B16F10 melanoma cells.ResultsEach component alone markedly inhibited mushroom tyrosinase in a dose-dependent manner, and in α-MSH-stimulated B16F10 cells, they inhibited melanin synthesis and were cytotoxic. However, the whitening effects of UPEF, ECE, and GAGs in combination were greater than those of each component alone. A mixture in the ratio of 4:5:1 (UEG-451) showed the strongest activity without cytotoxicity. Further study suggested that UEG-451 inhibits α-MSH-stimulated melanogenesis in B16F10 cells by downregulating tyrosinase and tyrosinase-related proteins, such as TRP-1 and TRP-2, via the inhibition of MITF expression.ConclusionsThese results suggest that mixing the different components at optimum ratios might be an effective way to improve their bioactivities and reduce toxicity and that UEG-451 possesses strong whitening effects that could be used in the cosmetic industry.
- Research Article
3
- 10.1080/14786419.2023.2220063
- May 31, 2023
- Natural Product Research
In this study, analysis of the chemical constituents and bioactivities of the unpolar fractions [petroleum ether (PE) and chloroform (C)] of fruits and leaves of Alpinia oxyphylla Miq. were carried out, as well as the bioactivities of the main compounds nootkatone and valencene. From PE and C fractions of the fruits, and PE fraction of the leaves, 95.80%, 59.30%, and 82.11% of the chemical constituents respectively were identified by GC-MS. Among these identified compounds, nootkatone was the main compound in all of three fractions, while valencene was the second main compound in the PE fractions of the fruits and leaves. The bioactivities results showed that all of the fractions and the major compound nootkatone showed tyrosinase inhibitory, as well as inhibitory effect on NO production in LPS-stimulated RAW264.7 cells. While valencene only presented inhibitory activity on NO production in RAW264.7 cells. The critical genes involved in nootkatone biosynthesis in A. oxyphylla were identified from the public transcriptome datasets, and protein sequences were preliminarily analyzed. Our studies develop the usage of the unpolar fractions of A. oxyphylla, especially its leaves as the waste during its production, and meanwhile provide the gene resources for nootkatone biosynthesis.
- Research Article
46
- 10.1016/j.ejmech.2014.12.036
- Dec 26, 2014
- European Journal of Medicinal Chemistry
Structural exploration, synthesis and pharmacological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives as iNOS inhibitors against inflammatory diseases.
- Research Article
24
- 10.1016/j.bmcl.2010.10.013
- Oct 16, 2010
- Bioorganic & Medicinal Chemistry Letters
28-Nor-oleanane-type triterpene saponins from Camellia japonica and their inhibitory activity on LPS-induced NO production in macrophage RAW264.7 cells
- Research Article
10
- 10.5012/bkcs.2014.35.8.2481
- Aug 20, 2014
- Bulletin of the Korean Chemical Society
Department of Pharmacy, Hanyang University, Ansan 426-791, KoreaReceived May 15, 2014, Accepted May 29, 2014Twelve thienyl/furanyl-hydroxyphenylpropenones were systematically designed and synthesized, andevaluated for their inhibitory effect on LPS-induced ROS and NO production in RAW 264.7 macrophages.Compound 11 displayed the most significant inhibitory activity of LPS-induced ROS and NO production inRAW 264.7 macrophages. Structure-activity relationship study indicated that para-hydroxyphenyl moietyplays an important role for inhibitory activities on both LPS-induced ROS and NO production as well as 3-thienyl moiety on molecule.Key Words : Thieny/Furanyl-hydroxyphenylpropenones, LPS-induced ROS and NO, Inhibition, Structure-activity relationship studyIntroductionReactive oxygen species (ROS), the molecules containinghighly reactive oxygen, actively interact with variousintracellular molecules. Excessive ROS production results inalterations of diverse intracellular signaling pathways andcauses significant damages to the target cells, collectivelyknown as oxidative stress. Abnormally high production ofROS contributes to the development of diverse pathologicalevents, such as DNA mutation, carcinogenesis, aging, celldeath and inflammation,
- Research Article
47
- 10.4062/biomolther.2012.098
- Mar 31, 2013
- Biomolecules and Therapeutics
This study examined the total polyphenol content of eight wild edible plants from Ethiopia and their effect on NO production in Raw264.7 cells. Owing to its relatively high polyphenol concentration and inhibition of NO production, the methanol extract of Adansonia digitata L. leaf (MEAD) was subjected to detailed evaluation of its antioxidant and anti-inflammatory effects. Antioxidant effects were assessed by measuring free-radical-scavenging activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and oxygen-radical-absorbance capacity (ORAC) assays, while anti-inflammatory effects were assessed by measuring inducible nitric oxide synthase (iNOS) expression in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. In the ORAC assay, MEAD was 10.2 times more potent than vitamin C at eliminating peroxyl radicals. In DPPH assay, MEAD also showed a strong ROS scavenging effect. MEAD significantly inhibited iNOS activity (IC50=28.6 μg/ml) of LPS-stimulated Raw264.7 cells. We also investigated the relationship between iNOS expression and nuclear factor kappa B (NF-κB) activation. MEAD inhibited IκBα degradation and NF-κB translocation from the cytosol to the nucleus in LPS-induced RAW264.7 cells without significant cytotoxic effects, as confirmed by MTT assay. These results suggest that MEAD inhibits anti-inflammatory iNOS expression, which might be related to the elimination of peroxyl radicals and thus the inhibition of IκBα-mediated NF-κB signal transduction.
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