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1.
Phytochemistry ; 213: 113751, 2023 Sep.
Article in English | MEDLINE | ID: mdl-37307887

ABSTRACT

Boswellia dalzielii is a resin-producing tree endemic to West and Central Africa, used by local populations for various medicinal purposes. In this study, B. dalzielii gum resin was analyzed by GC-MS and UHPLC-MS to identify and quantify volatile and non-volatile compounds. Its main volatile constituents were α-pinene (54.9%), followed by α-thujene (4.4%) and α-phellandren-8-ol (4.0%). Pentacyclic triterpenoids such as ß-boswellic acids and their derivatives were quantified by UHPLC-MS and their content was shown to reach around 22% of the gum resin. Since some of the volatile and non-volatile compounds identified in this work are known to possess biological effects, the bioactivities of B. dalzielii ethanolic extract, essential oil, as well as fractions of the oil and extract were evaluated. Some of these samples exhibited interesting anti-inflammatory properties, and their antioxidant, anti-ageing and skin-bleaching activities were also tested.


Subject(s)
Boswellia , Phytochemicals , Resins, Plant , Aging/drug effects , Anti-Inflammatory Agents/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Boswellia/chemistry , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Phytochemicals/chemistry , Phytochemicals/pharmacology , Plant Extracts/chemistry , Plant Extracts/pharmacology , Resins, Plant/chemistry , Skin Lightening Preparations/chemistry , Skin Lightening Preparations/pharmacology , Triterpenes/chemistry , Triterpenes/pharmacology
2.
Int J Mol Sci ; 23(18)2022 Sep 08.
Article in English | MEDLINE | ID: mdl-36142265

ABSTRACT

The root of Pueraria lobata (Willd.) is used commercially in different products, including dietary supplements, cosmetics, and teas, but its stem part is rarely used and studied. Therefore, this study evaluated the antioxidant and anti-melanogenesis activities of the bioactive fraction of P. lobata stem and investigated whether the activated carbon decolorization technique would have an impact on its activity and chemical composition. We observed that the dichloromethane fraction of P. lobata stem (DCM-PLS) has excellent antioxidant and anti-melanin synthesis activity at a concentration of 50 µg/mL. For the investigation of the anti-melanogenesis mechanism, we evaluated the mRNA expression of tyrosinase, which was depressed by the DCM-PLS. Daidzin was identified as the main active ingredient in DCM-PLS by using a high-performance liquid chromatography-diode array detector-hyphenated with tandem mass spectrometry. In addition, the activated carbon decolorization technology has no negative impact on the main components and bioactivity of DCM-PLS. DCM-PLS also did not induce any skin response in the human skin safety test. Collectively, DCM-PLS could be used as a natural type of skin-whitening agent in skin care products.


Subject(s)
Bleaching Agents , Pueraria , Skin Lightening Preparations , Antioxidants/pharmacology , Charcoal , Humans , Methylene Chloride , Monophenol Monooxygenase , Plant Extracts/chemistry , Plant Extracts/pharmacology , Pueraria/chemistry , RNA, Messenger , Skin Lightening Preparations/pharmacology
3.
J Med Food ; 25(2): 192-204, 2022 Feb.
Article in English | MEDLINE | ID: mdl-35148197

ABSTRACT

In this study, we investigated the protective effects of low-molecular-weight fish collagen from tilapia against melanogenesis in melanocytes, ultraviolet B (UVB)-irradiated Hs27 skin fibroblasts, and hairless mice. We observed collagen production-related pathways in UVB-irradiated Hs27 skin fibroblasts and hairless mice, and the melanogenesis-related pathways in melanocyte and UVB-irradiated hairless mice. The collagen production-related pathways were activated in the UVB-irradiated Hs27 skin fibroblasts and hairless mice. In addition, UVB exposure stimulated the melanogenesis-related pathways in melanocytes and hairless mice. However, treatment with low-molecular-weight fish collagen significantly increased the messenger RNA expressions of collagen production-related factors and significantly decreased the production of cytokines. Furthermore, treatment with low-molecular-weight fish collagen suppressed melanogenesis by inhibiting glutathione synthesis and downregulating melanocyte-inducing transcription factor expression through the suppression of cyclic AMP/protein kinase A/cAMP-responsive binding protein signaling and nitric oxide production. Low-molecular-weight fish collagen exerts protective effects against UVB-induced photoaging, through anti-inflammatory, antioxidant, and anti-melanogenesis activities and could be used for developing effective natural anti-photoaging products.


Subject(s)
Collagen/pharmacology , Skin Aging , Skin Lightening Preparations , Tilapia , Animals , Mice , Mice, Hairless , Skin , Skin Aging/drug effects , Ultraviolet Rays
4.
BMC Complement Med Ther ; 22(1): 9, 2022 Jan 07.
Article in English | MEDLINE | ID: mdl-34996448

ABSTRACT

BACKGROUND: Bletilla striata is the main medicine of many skin whitening classic formulas in traditional Chinese medicine (TCM) and is widely used in cosmetic industry recently. However, its active ingredients are still unclear and its fibrous roots are not used effectively. The aim of the present study is to discover and identify its potential anti-melanogenic active constituents by zebrafish model and molecular docking. METHODS: The antioxidant activities were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, 2,2'-azino-bis-(3-ethylbenthiazoline-6-sulphonic acid) (ABTS) radical scavenging activity and ferric reducing antioxidant power (FRAP) assay. The anti-melanogenic activity was assessed by tyrosinase inhibitory activity in vitro and melanin inhibitory in zebrafish. The chemical profiles were performed by ultra-high-performance liquid chromatography combined with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF-MS/MS). Meanwhile, the potential anti-melanogenic active constituents were temporary identified by molecular docking. RESULTS: The 95% ethanol extract of B. striata fibrous roots (EFB) possessed the strongest DPPH, ABTS, FRAP and tyrosinase inhibitory activities, with IC50 5.94 mg/L, 11.69 mg/L, 6.92 mmol FeSO4/g, and 58.92 mg/L, respectively. In addition, EFB and 95% ethanol extract of B. striata tuber (ETB) significantly reduced the melanin synthesis of zebrafish embryos in a dose-dependent manner. 39 chemical compositions, including 24 stilbenoids were tentatively identified from EFB and ETB. Molecular docking indicated that there were 83 (including 60 stilbenoids) and 85 (including 70 stilbenoids) compounds exhibited stronger binding affinities toward tyrosinase and adenylate cyclase. CONCLUSION: The present findings supported the rationale for the use of EFB and ETB as natural skin-whitening agents in pharmaceutical and cosmetic industries.


Subject(s)
Antioxidants/pharmacology , Medicine, Chinese Traditional/methods , Melanins/antagonists & inhibitors , Molecular Docking Simulation , Plant Extracts/pharmacology , Polysaccharides/pharmacology , Skin Lightening Preparations/pharmacology , Animals , Antioxidants/chemistry , China , Models, Animal , Monophenol Monooxygenase/antagonists & inhibitors , Plant Extracts/chemistry , Plant Roots , Plant Tubers , Polysaccharides/chemistry , Skin Lightening Preparations/chemistry , Zebrafish
5.
J Ethnopharmacol ; 282: 114607, 2022 Jan 10.
Article in English | MEDLINE | ID: mdl-34506940

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: The root of Paeonia lactiflora is a traditionally-used whitening medicine in China for thousands of years. Although some tyrosinase inhibitors and/or antioxidants such as 1,2,3,4,6-pentagalloylglucose, gallic acid, have been isolated and identified, their tyrosinase inhibition pathway (monophenolase or diphenolase inhibition, or both two) have not been systematically studied and the underlying tyrosinase inhibition mechanism has not been revealed yet. Moreover, the exploring of new natural tyrosinase inhibitors and antioxidants is urgently needed. AIM OF THE STUDY: This review aimed to develop a new microplate-based high-resolution tyrosinase inhibition profiling assay and establish a furthermore triple high-resolution monophenolase/diphenolase/radical scavenging profiling for accelerating identification bioactive compounds from complicated plant extract. MATERIALS AND METHODS: The targeted isolation and structure elucidation were performed with high-performance liquid chromatography-high-resolution mass spectrometry and preparative high-performance liquid chromatography. It allows to be a proof of concept with the root of Paeonia lactiflora crude extract as a natural whitening herbal drug. RESULTS: The result showed that galloylpaeoniflorin specifically inhibited monophenolase activity. While 1,2,3,4,6-pentagalloylglucose, gallic acid and catechin demonstrated the inhibition towards both monophenolase and diphenolase. Among them, 1,2,3,4,6-pentagalloylglucose can inhibit monophenolase activity was reported for the first time. In addition, antioxidant properties were attributed to catechin, 1,2,3,4,6-pentagalloylglucose and gallic acid. Due to its low content and complicated configuration in the root of Paeonia lactiflora, a new potential tyrosinase inhibitor and radical scavenger which tentatively identified as hexagalloylglucose by high-resolution MS was still need further verification. What's more, the molecular docking unveiled that bioactive enzymatic inhibitors mainly interacted with amino acid catalytic residues of tyrosinase via H-bonds and van der wals, which may be helpful to understand their inhibition mechanisms with tyrosinase in the skin whitening. CONCLUSIONS: The platform provided a promising and efficient strategy for the rapid screening of whitening active components from natural sources.


Subject(s)
Chromatography, High Pressure Liquid/methods , Monophenol Monooxygenase/antagonists & inhibitors , Oxidoreductases/antagonists & inhibitors , Paeonia , Skin Lightening Preparations/pharmacology , Antioxidants/pharmacology , Enzyme Inhibitors/pharmacology , Humans , Hydrolyzable Tannins/pharmacology , Molecular Docking Simulation/methods , Phytochemicals/pharmacology , Plant Extracts/analysis , Plant Extracts/pharmacology
6.
Int J Cosmet Sci ; 43(6): 703-714, 2021 Dec.
Article in English | MEDLINE | ID: mdl-34674286

ABSTRACT

OBJECTIVE: In this study, we examined the effect of C. japonicum flower extract (CFE) on melanogenesis and its mechanism in vitro and ex vivo. METHODS: The effect of CFE on melanogenesis was investigated with lightly (HEMn-LP) and moderately (HEMn-MP) pigmented normal human melanocytes, reconstituted three-dimensional skin (3D skin) model and ex vivo human hair follicles. The melanogenesis-inducing effect of CFE was evaluated using melanin content and intracellular tyrosinase activity assay. The amount and type of eumelanin and pheomelanin were analysed by using HPLC method. The mechanism involved in the effect of CFE on hyperpigmentation was explored by cyclic adenosine monophosphate (cAMP) immunoassay and western blot analysis for tyrosinase, microphthalmia-associated transcription factor (MITF) and phosphorylated CRE-binding protein (pCREB) expression. The degree of pigmentation in 3D skin and L-values were measured using a CR-300 chroma meter. The amount of dissolved melanin was measured using a spectrophotometer. The content of melanin in the hair follicles was evaluated by Fontana Masson staining. RESULTS: C. japonicum flower extract significantly increased the melanin content and cellular tyrosinase activity in both HEMn-LP and HEMn-MP cells. The markers of pheomelanin and eumelanin in HEMn-LP and HEMn-MP were also increased by CFE. We observed that CFE treatment on melanocytes increased intracellular cAMP with inducing pCREB and up-regulating the protein levels of TYR and MITF. Furthermore, CFE considerably increased the melanin content in a 3D skin model and ex vivo human hair follicles. CONCLUSIONS: These results suggest that CFE exerts hyperpigmentation activity through cAMP signalling in human melanocytes that it can improve follicular depigmentation and vitiligo by stimulating the melanin synthesis.


OBJECTIF: Dans cette étude, nous avons examiné l'effet de l'extrait de fleur de C. japonicum (EFC) sur la mélanogenèse et son mécanisme in vitro et ex vivo. MÉTHODES: L'effet du EFC sur la mélanogenèse a été étudié avec des mélanocytes humains normaux légèrement (HEMn-LP) et modérément (HEMn-MP) pigmentés, un modèle de peau reconstituée en 3 dimensions (peau 3D) et des follicules pileux ex vivo. L'effet inducteur de la mélanogénèse de la EFC a été évalué en utilisant la teneur en mélanine et le dosage de l'activité de la tyrosinase intracellulaire. La quantité et le type d'eumélanine et de phéomélanine ont été analysés en utilisant la méthode HPLC. Le mécanisme impliqué dans l'effet de la EFC sur l'hyperpigmentation a été exploré par immunoessai à l'adénosine monophosphate cyclique (AMPc) et Western blot pour l'expression de la tyrosinase, du facteur de transcription associé à la microphtalmie (MITF) et l'expression de la protéine CREB phosphorylée. Le degré de pigmentation de la peau 3D, les valeurs L ont été mesurées à l'aide d'un chromamètre CR-300. La quantité de mélanine dissoute a été mesurée à l'aide d'un spectrophotomètre. La teneur en mélanine des follicules pileux a été évaluée par coloration Fontana Masson. RÉSULTATS: EFC a augmenté de manière significative la teneur en mélanine et l'activité de la tyrosinase cellulaire dans les cellules HEMn-LP et HEMn-MP. Les marqueurs de phéomélanine et d'eumélanine dans HEMn-LP et HEMn-MP ont également été augmentés par EFC. Nous avons observé que le traitement EFC sur les mélanocytes augmentait l'AMPc intracellulaire en induisant pCREB et en régulant à la hausse les niveaux de protéines de TYR et MITF. De plus, le EFC a considérablement augmenté la teneur en mélanine dans un modèle de peau 3D et dans les follicules pileux humains ex vivo. CONCLUSIONS: Ces résultats suggèrent que la EFC exerce une activité d'hyperpigmentation via la signalisation de l'AMPc dans les mélanocytes humains qu'elle peut améliorer la dépigmentation folliculaire et le vitiligo en stimulant la synthèse de mélanine.


Subject(s)
Hair Follicle/drug effects , Melanins/metabolism , Plant Extracts/pharmacology , Skin Lightening Preparations/pharmacology , Skin/drug effects , Vitiligo/drug therapy , Aged , Cirsium , Female , Flowers , Humans , Melanocytes/drug effects
7.
Int J Mol Sci ; 22(15)2021 Jul 28.
Article in English | MEDLINE | ID: mdl-34360871

ABSTRACT

The root of Pueraria lobata (Willd.) is a widely used herbal medicine worldwide, whereas the stem of the plant is discarded or used as feed for livestock. To reuse and exploit the stem of P. lobata as a resource, we investigated its potential as a skin-whitening agent. We found that the developed, enriched P. lobata stem (PLS) extract significantly inhibited melanin production in the 3-isobutyl-1-methylxanthine-induced B16/F10 cells at a concentration of 50 µg/mL. To further confirm the mechanism of the antimelanogenic effect of the enriched PLS extracts, we examined the mRNA expression of tyrosinase, which was suppressed by the extracts. To standardize and implement effective quality control of the enriched PLS extracts, its major chemical constituents were identified by high-performance liquid chromatography-photodiode array-electrospray ionization-mass spectrometry. In total, 12 constituents were identified. In silico analysis showed that the main constituents, puerarin and daidzin, had excellent binding affinities for human tyrosinase. Collectively, our results suggest that the PLS extracts could be used as anti-pigmentation agents.


Subject(s)
Melanins/biosynthesis , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Plant Stems/chemistry , Pueraria/chemistry , Skin Lightening Preparations/pharmacology , Cell Line, Tumor , Humans , Isoflavones/pharmacology , Melanoma, Experimental , Monophenol Monooxygenase/metabolism
8.
Pak J Pharm Sci ; 34(1): 77-84, 2021 Jan.
Article in English | MEDLINE | ID: mdl-34248006

ABSTRACT

Skin-whitening effect is closely linked with the melanogenesis inhibitory activity and free radical scavenging capacity. The purpose of the present study was to evaluate the skin-whitening effect of cumin (Cuminum cyminum L.) extract. The whitening activity was evaluated by cell-free mushroom tyrosinase assay, free radical scavenging assay, cell viability assay, cellular tyrosinase assay and melanin content assay using B16F10 murine melanoma cells. The results showed that cumin extract exhibited concentration-dependent inhibitory effect on both monophenolase and diphenolase activities of mushroom tyrosinase (IC50 values of 1.027mg/mL and 0.977mg/mL, respectively). Kinetic study on diphenolase showed that the cumin extract was a reversible mixed-type inhibitor, and the inhibition constant (KI) was determined to be 0.62mg/mL. In addition, cumin extract significantly suppressed melanin production and cellular tyrosinase activity of B16F10 melanoma cells in a concentration and time dependent manner without cytotoxicity. Moreover, cumin extract exerted strong scavenging capacity on DPPH, hydroxyl and superoxide anion radicals. Taken together, these results strongly suggest that cumin is a potential skin-whitening agent for the cosmetic industry.


Subject(s)
Cell Survival/drug effects , Cuminum , Free Radical Scavengers/pharmacology , Plant Extracts/pharmacology , Skin Lightening Preparations/pharmacology , Skin/drug effects , Animals , Cell Line, Tumor , Cell Survival/physiology , Dose-Response Relationship, Drug , Free Radical Scavengers/isolation & purification , Melanoma, Experimental , Mice , Plant Extracts/isolation & purification , Skin/metabolism , Skin Lightening Preparations/isolation & purification
9.
Molecules ; 26(5)2021 Feb 25.
Article in English | MEDLINE | ID: mdl-33669031

ABSTRACT

Response surface methodology was employed to optimize the ultrasound-assisted extraction (UAE) conditions for simultaneous optimization of dependent variables, including DPPH radical scavenging activity (RSA), tyrosinase activity inhibition (TAI), and collagenase activity inhibition (CAI) of peanut shell extracts. The effects of the main variables including extraction time (5.0~55.0 min, X1), extraction temperature (26.0~94.0 °C, X2), and ethanol concentration (0.0%~99.5%, X3) were optimized. Based on experimental values from each condition, quadratic regression models were derived for the prediction of optimum conditions. The coefficient of determination (R2) of the independent variable was in the range of 0.89~0.96, which demonstrates that the regression model is suitable for the prediction. In predicting optimal UAE conditions based on the superimposing method, extraction time of 31.2 min, extraction temperature of 36.6 °C, and ethanol concentration of 93.2% were identified. Under these conditions, RSA of 74.9%, TAI of 50.6%, and CAI of 86.8% were predicted, showing good agreement with the experimental values. A reverse transcription polymerase chain reaction showed that peanut shell extract decreased mRNA levels of tyrosinase-related protein-1 and matrix metalloproteinase-3 genes in B16-F0 cell. Therefore, we identified the skin-whitening and anti-wrinkle effects of peanut shell extracts at protein as well as gene expression levels, and the results show that peanut shell is an effective cosmetic material for skin-whitening and anti-wrinkle effects. Based on this study, peanut shell, which was considered a byproduct, can be used for the development of healthy foods, medicines, and cosmetics.


Subject(s)
Antioxidants/pharmacology , Arachis/chemistry , Plant Extracts/pharmacology , Skin Lightening Preparations/pharmacology , Ultrasonic Waves , Animals , Antioxidants/chemistry , Antioxidants/isolation & purification , Biphenyl Compounds/antagonists & inhibitors , Matrix Metalloproteinase 3/genetics , Matrix Metalloproteinase 3/metabolism , Membrane Glycoproteins/antagonists & inhibitors , Membrane Glycoproteins/genetics , Membrane Glycoproteins/metabolism , Mice , Oxidoreductases/antagonists & inhibitors , Oxidoreductases/genetics , Oxidoreductases/metabolism , Picrates/antagonists & inhibitors , Plant Extracts/chemistry , Plant Extracts/isolation & purification , RNA, Messenger/antagonists & inhibitors , RNA, Messenger/genetics , RNA, Messenger/metabolism , Skin Aging/drug effects , Skin Lightening Preparations/chemistry , Skin Lightening Preparations/isolation & purification , Tumor Cells, Cultured
10.
J Ethnopharmacol ; 264: 113272, 2021 Jan 10.
Article in English | MEDLINE | ID: mdl-32810622

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: The Zulu and Xhosa people of South Africa use the stem bark of Cassipourea flanaganii as a skin-lightning cosmetic. AIM OF THE STUDY: To isolate and identify compounds responsible for the skin lightning properties from the stem bark of Cassipourea flanaganii and to evaluate their cytotoxicity towards skin cells. MATERIALS AND METHODS: Extracts from the stem bark of Cassipourea flanaganii were isolated using chromatographic methods and structures were determined using NMR, IR and MS analysis. The tyrosinase inhibitory activity and the ability to inhibit the production of melanin were determined using human primary epidermal melanocyte cells. Cytoxicity was established using the same melanocytes and a neutral red assay. RESULTS: One previously undescribed compound, ent-atis-16-en-19-al (1) along with the known ent-atis-16-en-19-oic acid (2), ent-atis-16-en-19-ol (3), ent-kaur-16-en-19-oic acid (4), ent-kaur-16-en-19-al (5), ent-manoyl oxide (6), guinesine A (7), guinesine B (8), guinesine C (9), lichenxanthone (10), 2,4-dihydroxy-3,6-dimethyl benzoic acid methyl ester (11), lynoside (12), lupeol (13), ß-amyrin (14), docosyl ferulate (15), stigmasterol, sitosterol and sitosterol-O-glucoside were isolated in this investigation. An impure fraction containing compound 3 was acetylated to obtain 19-acetoxy-ent-atis-16-ene (3a). Compounds 10 and 11 are usually isolated from lichen, hence they are possible contaminants of lichen harvested with the bark. Compounds 1, 3a, 5-14 were not significantly cytotoxic to the primary epidermal melanocyte cells (P > 0.05) when compared to the negative and positive controls (DMSO, 0.1% and hydrogen peroxide, 30 wt% in water). Inhibition of tyrosinase was significantly greater with respect to the negative control (P < 0.001) for compounds 3a, 5-8 and 9-10 at 10 µM and for compounds 5-8 and 9-10 at 100 µM. Compared to hydroquinone (the positive control) at 10 µM, the level of inhibition was comparable or to that of compounds 3a, 5, 6, and 8-10 at 10 µM, with 9 and 10 showing a greater level of inhibition. Inhibition of melanin was both concentration and time dependent for all compounds tested with higher melanin content at 24 h compared to 48 h s and at 10 mM compared to100 mM at both time points; melanin content was significantly lower for hydroquinone at both time points and concentrations. CONCLUSIONS: Compounds 1, 5-14, isolated from Cassipourea flanaganii and the derivative 3a showed low cytotoxicity. All compounds had a clear time and concentration dependent effect on melanin content which did not appear to be dependent on their inhibition of tyrosinase.


Subject(s)
Melanins/antagonists & inhibitors , Melanocytes/drug effects , Monophenol Monooxygenase/antagonists & inhibitors , Plant Extracts/pharmacology , Rhizophoraceae , Skin Lightening Preparations/pharmacology , Cell Survival/drug effects , Cell Survival/physiology , Cells, Cultured , Dose-Response Relationship, Drug , Humans , Melanins/metabolism , Melanocytes/metabolism , Monophenol Monooxygenase/metabolism , Plant Bark , Plant Extracts/isolation & purification , Plant Stems , Skin Lightening Preparations/isolation & purification
11.
Lipids ; 55(6): 649-659, 2020 11.
Article in English | MEDLINE | ID: mdl-33128473

ABSTRACT

In the present study, we demonstrated that borage (Borago officinalis L.) seed oil subjected to immobilized lipase pretreatment are enriched with linoleic acid (LNA, 18:2n-6), γ-linolenic acid (GLA, 18:3n-6), and oleic acid (OLA, 18:1n-9). We further showed that lipase-treated borage oil (LT-BOL) regulates the activity and degradation of tyrosinase, an important enzyme implicated in the synthesis of melanin in murine melanocytes, B16F10. LT-BOL and its free fatty acid components reduced the levels of melanin and tyrosinase in melanocytes with GLA exerting similar or stronger effects compared with LNA and OLA. The brightening efficacy of LT-BOL on melanin metabolism in humans was tested by an 8-week, double-blind, randomized clinical trial, which enrolled 21 Korean female adults (mean age 48.57 ± 3.28). Visual evaluation showed that cream containing 1% LT-BOL significantly decreased (p < 0.05) melasma on the treated skin area after 6 and 8 weeks. The analysis of the skin brightness using Chromameter CR-400 confirmed that the brightness of the treated area was significantly increased (p < 0.01) after 4, 6, and 8 weeks. Together, our results suggest that LT-BOL may be suitable as a natural skin whitening cosmeceutical product.


Subject(s)
Lipase/chemistry , Melanocytes/drug effects , Plant Oils/chemistry , Plant Oils/pharmacology , Skin Lightening Preparations/pharmacology , gamma-Linolenic Acid/chemistry , gamma-Linolenic Acid/pharmacology , Camellia/chemistry , Double-Blind Method , Enzymes, Immobilized/chemistry , Fatty Acids, Nonesterified/chemistry , Fatty Acids, Nonesterified/pharmacology , Female , Humans , Melanins/analysis , Melanins/metabolism , Melanocytes/physiology , Melanoma, Experimental/drug therapy , Melanoma, Experimental/pathology , Middle Aged , Monophenol Monooxygenase/antagonists & inhibitors , Monophenol Monooxygenase/metabolism , Skin Lightening Preparations/chemistry
12.
Clin Exp Dermatol ; 45(8): 974-979, 2020 Dec.
Article in English | MEDLINE | ID: mdl-32852805

ABSTRACT

This review is part of a series of annual updates that summarize the evidence base for atopic eczema (AE). The aim is to provide a succinct guide for clinicians on the key findings from 14 systematic reviews on the prevention and topical treatment of AE published or indexed in 2018. Various supplements, including long-chain polyunsaturated fatty acids, vitamin D and the probiotic Lactobacillus rhamnosus GG, given prenatally and postnatally, have not been shown to prevent AE in infants, although mixed strains of probiotics may decrease the risk of AE if given to the mother during pregnancy and to the infant for the first 6 months of life. In the postnatal period, there is no evidence that hydrolysed formula, compared with cow's milk formula (CMF), reduces the risk of AE in partially breastfed infants. However, weak evidence suggests that a specific partially hydrolysed whey formula decreases the risk of AE compared with CMF. No specific skin practices can be recommended to reduce the eczema risk in healthy term babies. There is weak evidence of a low risk of reversible hypothalamic-pituitary-adrenal axis suppression following 2-4 weeks of treatment with low-potency topical steroids, and conflicting evidence as to whether bleach bathing affects skin flora or AE severity. A single study demonstrated that the topical Janus kinase inhibitor tofacitinib at 2% significantly reduces the Eczema Area and Severity Index compared with vehicle. Topical naltrexone cream 1% improves pruritus (measured using a visual analogue scale) by 30% more than placebo. There is weak evidence that topical alternative therapies, including antioxidants, micronutrients and some herbal medicines, may improve AE.


Subject(s)
Dermatitis, Atopic/drug therapy , Dermatitis, Atopic/prevention & control , Eczema/drug therapy , Eczema/prevention & control , Administration, Topical , Animals , Breast Feeding/statistics & numerical data , Complementary Therapies/adverse effects , Complementary Therapies/statistics & numerical data , Dermatitis, Atopic/diagnosis , Eczema/pathology , Fatty Acids/administration & dosage , Fatty Acids/therapeutic use , Female , Humans , Hypothalamo-Hypophyseal System/drug effects , Infant Formula/adverse effects , Infant, Newborn , Janus Kinase Inhibitors/administration & dosage , Janus Kinase Inhibitors/therapeutic use , Lacticaseibacillus rhamnosus/immunology , Milk/adverse effects , Naltrexone/administration & dosage , Naltrexone/therapeutic use , Narcotic Antagonists/administration & dosage , Narcotic Antagonists/therapeutic use , Pituitary-Adrenal System/drug effects , Pregnancy , Probiotics/therapeutic use , Skin Lightening Preparations/adverse effects , Steroids/administration & dosage , Steroids/pharmacology , Vitamin D/therapeutic use , Whey Proteins/administration & dosage , Whey Proteins/adverse effects , Whey Proteins/chemistry
13.
J Drugs Dermatol ; 19(8): 763-768, 2020 Aug 01.
Article in English | MEDLINE | ID: mdl-32845587

ABSTRACT

Post-inflammatory hyperpigmentation (PIH) is a reactive process resulting from increased melanin or abnormal distribution of melanin secondary to inflammatory skin conditions, dermatologic therapies, and external stimuli. Because PIH is a common condition that has a substantial effect on the quality of life, an understanding of its treatment modalities is essential. Though there are many therapeutic strategies for hyperpigmentary conditions such as melasma that are described in the literature, fewer studies focus on PIH. This article aims to provide a comprehensive literature review of therapies specifically used to treat PIH, such as topical combinations, chemical peels, and lasers. J Drugs Dermatol. 2020;19(8): doi:10.36849/JDD.2020.4887.


Subject(s)
Dermatitis/complications , Keratolytic Agents/administration & dosage , Low-Level Light Therapy/methods , Melanosis/therapy , Skin Lightening Preparations/administration & dosage , Administration, Cutaneous , Clinical Trials as Topic , Dermatitis/immunology , Drug Therapy, Combination/methods , Humans , Melanosis/immunology , Melanosis/pathology , Melanosis/psychology , Observational Studies as Topic , Quality of Life , Skin/drug effects , Skin/immunology , Skin/pathology , Skin/radiation effects , Skin Pigmentation/drug effects , Skin Pigmentation/immunology , Skin Pigmentation/radiation effects , Treatment Outcome
14.
J Med Food ; 23(8): 870-878, 2020 Aug.
Article in English | MEDLINE | ID: mdl-32609563

ABSTRACT

We sought to investigate the effect of extracts from Rosa gallica petals (RPE) on skin whitening and anti-wrinkle activity. Tyrosinase activity was attenuated by RPE treatment, concomitant with the reduction of melanin accumulation in human B16F10 melanoma. Treatment of the facial skin of volunteers in a clinical trial with an RPE-containing formulation enhanced skin brightness (L* value) significantly. The underlying mechanism responsible was determined to be associated with mitogen-activated protein kinase (MAPK) activation. In addition, RPE exhibited anti-wrinkle formation activity of human dermal fibroblasts by suppressing matrix metalloproteinase (MMP)-1 level. In vivo study, RPE also inhibited solar ultraviolet-stimulated MMP-1 level by c-Jun regulation. Overall, our findings indicate that RPE evokes skin whitening and anti-wrinkle formation activity by regulating intracellular signaling, supporting its utility as an ingredient for skin whitening and anti-wrinkle cosmetic products.


Subject(s)
Plant Extracts/pharmacology , Rosa/chemistry , Skin Aging/drug effects , Skin Lightening Preparations/pharmacology , Skin/drug effects , Cells, Cultured , Fibroblasts , Humans , JNK Mitogen-Activated Protein Kinases/metabolism , MAP Kinase Signaling System/drug effects , Matrix Metalloproteinase 1/metabolism , Melanins/metabolism , Melanoma, Experimental , Ultraviolet Rays
15.
Recent Pat Drug Deliv Formul ; 14(3): 223-232, 2020.
Article in English | MEDLINE | ID: mdl-32479252

ABSTRACT

BACKGROUND: Many topical agents are available in the market, which interfere with the pigmentation process at different levels. They are often known to cause side effects ranging from irritation to tumor over chronic use. OBJECTIVE: The present study was designed to develop and characterize an anti blemish cream containing herbal oils. METHODS: A herbal cream was formulated using dill, nagarmotha and black cumin oil and subjected to evaluation of its anti blemish potential against stress augmented UV-B rays-induced hyperpigmentation. Topical oil in water type of creams containing 2%, 4% and 6% of each oil was formulated using herbal oils. The formulated cream was characterized for solubility, pH, particle size, grittiness, viscosity, stability, phase separation, shelf life and spreadability, and found to be stable. Acute dermal toxicity was carried out individually for dill, nagarmotha and black cumin oil according to the OECD guidelines 402. Hyperpigmentation was induced in all the experimental animals by stress-augmented UV-B irradiation method. The animals were treated for 30 days (twice daily) with standard and test formulations by topical administration, whereas the disease group was left untreated. The skin of the animals was subjected to photographical study as well as grading for pigmentation and irritation before and after treatment. After the treatment period, the serum antioxidant levels were estimated and histopathology, histochemical studies of skin were performed. RESULTS: The animals treated with test formulations containing 2%, 4%, and 6% of herbal oil showed significant improvement in pigmentation compared to disease control as it is evident in photographic biochemical, histopathological and histochemical studies. CONCLUSION: Thus, it was concluded that the developed anti-blemish cream containing herbal oils possesses significant anti-blemish potential. This study necessitates further evaluations in human subjects as it could have a high positive therapeutic value in the treatment of hyperpigmentation.


Subject(s)
Hyperpigmentation/drug therapy , Plant Oils/administration & dosage , Skin Lightening Preparations/administration & dosage , Administration, Cutaneous , Anethum graveolens , Animals , Cyperus , Disease Models, Animal , Drug Compounding , Female , Hyperpigmentation/etiology , Hyperpigmentation/pathology , Nigella sativa , Plant Oils/chemistry , Rats, Wistar , Skin Cream , Skin Lightening Preparations/chemistry , Skin Pigmentation/radiation effects , Stress, Psychological/complications , Ultraviolet Rays
16.
Molecules ; 25(11)2020 May 29.
Article in English | MEDLINE | ID: mdl-32486036

ABSTRACT

The cosmetic industry is among the fastest growing industries in the last decade. As the beauty concepts have been revolutionized, many terms have been coined to accompany the innovation of this industry, since the beauty products are not just confined to those that are applied to protect and enhance the appearance of the human body. Consequently, the terms such as cosmeceuticals and nutricosmetics have emerged to give a notion of the health benefits of the products that create the beauty from inside to outside. In the past years, natural products-based cosmeceuticals have gained a huge amount of attention not only from researchers but also from the public due to the general belief that they are harmless. Notably, in recent years, the demand for cosmeceuticals from the marine resources has been exponentially on the rise due to their unique chemical and biological properties that are not found in terrestrial resources. Therefore, the present review addresses the importance of marine-derived compounds, stressing new chemical entities with cosmeceutical potential from the marine natural resources and their mechanisms of action by which these compounds exert on the body functions as well as their related health benefits. Marine environments are the most important reservoir of biodiversity that provide biologically active substances whose potential is still to be discovered for application as pharmaceuticals, nutraceuticals, and cosmeceuticals. Marine organisms are not only an important renewable source of valuable bulk compounds used in cosmetic industry such as agar and carrageenan, which are used as gelling and thickening agents to increase the viscosity of cosmetic formulations, but also of small molecules such as ectoine (to promote skin hydration), trichodin A (to prevent product alteration caused by microbial contamination), and mytiloxanthin (as a coloring agent). Marine-derived molecules can also function as active ingredients, being the main compounds that determine the function of cosmeceuticals such as anti-tyrosinase (kojic acid), antiacne (sargafuran), whitening (chrysophanol), UV protection (scytonemin, mycosporine-like amino acids (MAAs)), antioxidants, and anti-wrinkle (astaxanthin and PUFAs).


Subject(s)
Aquatic Organisms/chemistry , Biological Products/chemistry , Cosmeceuticals/chemistry , Cosmetics/chemistry , Dietary Supplements , Skin Aging/drug effects , Acne Vulgaris/drug therapy , Animals , Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Humans , Indoles/metabolism , Monophenol Monooxygenase/antagonists & inhibitors , Phenols/metabolism , Skin/drug effects , Skin Lightening Preparations , Wound Healing
17.
Bioorg Med Chem Lett ; 30(13): 127201, 2020 07 01.
Article in English | MEDLINE | ID: mdl-32386982

ABSTRACT

A series of aryl sulfide derivatives was synthesized and evaluated for their anti-melanogenic activities. Several compounds, including 3e, 3i and 3q exhibited good anti-melanogenic activities. Among the derivatives, compound 3i showed good inhibitory effects against melanin synthesis and showed no toxicity in reconstituted human eye and skin tissues.


Subject(s)
Melanins/antagonists & inhibitors , Skin Lightening Preparations/pharmacology , Sulfides/pharmacology , Animals , Cell Line, Tumor , Drug Evaluation, Preclinical , Humans , Skin Lightening Preparations/chemical synthesis , Skin Lightening Preparations/toxicity , Sulfides/chemical synthesis , Sulfides/toxicity , Zebrafish
18.
Biosci Biotechnol Biochem ; 84(7): 1436-1443, 2020 Jul.
Article in English | MEDLINE | ID: mdl-32299303

ABSTRACT

Melanin metabolism disorders may cause severe impacts on the psychological and social activities of patients. Different from the other two steps of melanin metabolism, namely synthesis and transport, little has been known about the mechanism of melanin degradation. Isoimperatorin (ISO) suppressed the activity of tyrosinase, an essential enzyme in melanin biosynthesis, hence, we investigated the effects and mechanism of ISO in melanin reduction. ISO stimulation significantly reduces the melanin contents and PMEL 17 protein levels; meanwhile, the activity and the protein levels of two critical lysosomal enzymes, Cathepsin B and Cathepsin D, can be significantly increased by ISO treatment. MiR-3619 inhibited the expression of CSTB and CSTD, therefore affecting ISO-induced degradation of melanin. In summary, ISO reduces the melanin content via miR-3619/CSTB and miR-3619/CSTD axes. ISO could be a potent skin-whitening agent, which needs further in vivo and clinical investigation.


Subject(s)
Cathepsin B/metabolism , Cathepsin D/metabolism , Drugs, Chinese Herbal/pharmacology , Furocoumarins/pharmacology , Keratinocytes/metabolism , Melanins/metabolism , MicroRNAs/metabolism , Signal Transduction/drug effects , Skin Lightening Preparations/pharmacology , Cathepsin B/genetics , Cathepsin D/genetics , Gene Knockdown Techniques , HaCaT Cells , Humans , MicroRNAs/genetics , Monophenol Monooxygenase/antagonists & inhibitors , Signal Transduction/genetics , Transfection , gp100 Melanoma Antigen/metabolism
19.
J Cosmet Dermatol ; 19(5): 1093-1098, 2020 May.
Article in English | MEDLINE | ID: mdl-32196865

ABSTRACT

BACKGROUND: Melasma is a difficult to treat pigmentation disorder. However, some successes have been attained by microneedling. The aim of the present study was to evaluate the efficacy of microneedling using meso-depigmentation solution (mesoneedling) in comparison with standard microneedling, over a 4-month treatment period. METHODS: As a part of this pilot study, 20 patients received microneedling on one side and mesoneedling on another side of their face. Treatment was repeated on a monthly basis for 4 months. Treatment efficacy was defined through Dermacatch® colorimetry, modified Melasma Area and Severity (mMASI) score determination, Investigator's Global Assessment (IGA), and patient questionnaires, whereby all assessments were conducted at the baseline, as well after 2 and 4 months of treatment. RESULTS: Before treatments, mean difference between pigmented and normal skin calculated by Dermacatch® was 43.7 ± 20.12 and 44.6 ± 20.72 in microneedling sides and mesoneedling sides, respectively. After two and four sessions, these values declined to 34.5 ± 16.26 and 28.05 ± 13.79 on the side subjected to microneedling, while 29.75 ± 15.07 and 20.45 ± 10.58 were measured on the mesoneedling side. Statistically significant differences have been observed between microneedling and mesoneedling treatments at both time points (P = .0001, P = .0001). The mMASI scores obtained upon treatment completion were significantly lower on both the microneedling and the mesoneedling side. The IGA and patients' self-assessment scores further confirmed that both treatments were effective in treating melasma, without producing any notable side-effects or complications. CONCLUSION: In sum, both microneedling and mesoneedling are effective in decreasing melanin content in the epidermal melasma lesions.


Subject(s)
Cosmetic Techniques/adverse effects , Dry Needling/methods , Melanosis/therapy , Skin Lightening Preparations/administration & dosage , Adolescent , Adult , Combined Modality Therapy/adverse effects , Combined Modality Therapy/instrumentation , Combined Modality Therapy/methods , Cosmetic Techniques/instrumentation , Dry Needling/adverse effects , Dry Needling/instrumentation , Face , Female , Humans , Injections, Intradermal/adverse effects , Injections, Intradermal/instrumentation , Injections, Intradermal/methods , Male , Melanosis/diagnosis , Middle Aged , Needles/adverse effects , Pilot Projects , Severity of Illness Index , Treatment Outcome , Young Adult
20.
Ann Pharm Fr ; 78(2): 142-149, 2020 Mar.
Article in English | MEDLINE | ID: mdl-32089252

ABSTRACT

INTRODUCTION: The standardized litchi extract had been revealed on phytochemical actives, in vitro and cellular activities against aging and darkening of skin. However, a formulation containing the extract has never been developed as per clinical evaluated. MATERIALS AND METHODS: The litchi serum was developed, safety and efficacy were clinically evaluated in human volunteers. The stable and none irritated 0.05 and 0.1% litchi serums were randomized-single blind placebo control clinical applied on the inner forearm of 29 volunteers for a consecutive 112 days and monitored by Mexameter® MX18, Cutometer® MPA 580 and Visioscan® VC 98. RESULTS: Skin lightening efficacy of the 0.1% and 0.05% litchi serum was significantly (P<0.001 and P<0.05) higher than the placebo. Skin elasticity and wrinkle reduction was significantly (P<0.05 and P<0.005) achieved by the 0.1% litchi serum. The efficacy of litchi serums was confirmed by a split-face, randomized, single-blind controlled that the 0.1% litchi serum was significantly (P<0.05) better than the 0.05% one of all examined parameters. CONCLUSION: Safety and efficacy of litchi extract are clinically confirmed for hyperpigmentation and aging of skin treatments.


Subject(s)
Hyperpigmentation/drug therapy , Litchi/chemistry , Plant Extracts/therapeutic use , Skin Aging/drug effects , Skin Lightening Preparations/therapeutic use , Adult , Drug Compounding , Elasticity , Female , Healthy Volunteers , Humans , Irritants , Male , Middle Aged , Plant Extracts/adverse effects , Pruritus/chemically induced , Single-Blind Method , Skin/drug effects , Skin Lightening Preparations/adverse effects , Young Adult
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