Cosmeceutical Potentials of Grammatophyllum speciosum Extracts: Anti-Inflammations and Anti-Collagenase Activities with Phytochemical Profile Analysis Using an Untargeted Metabolomics Approach

Grammatophyllum speciosum is the largest orchid species and a well-known traditional medicinal plant. Due to skin aging, natural products that inhibit this process can attract the attention of consumers and scientists because radical-scavenging activity, collagenase inhibition, and inflammatory suppression are valuable in dermatological applications. This study investigated the phytochemicals in G. speciosum leaves extracts that have cosmeceutical potentials, including radical-scavenging, anticollagenase, and anti-inflammatory abilities. G. speciosum leaves were extracted using water-based extraction methods. High-resolution mass spectrometry was used to identify the phytochemicals in the extracts. Fibroblast and keratinocyte cell cytotoxicity was determined. Antioxidant abilities were measured using DPPH and ABTS assays. The effect of the extracts on nitric oxide (NO) in macrophage cells was investigated. ELISA of the collagenase enzyme was determined. A total of 721 annotated metabolites were identified in the extracts. Vitexin and orientin were the most abundant metabolites. Cell viability was >80% in both cell lines when the extract concentration was <1 mg/mL. The IC50 values for DPPH and ABTS were 56 and 117 μg/mL, respectively. Furthermore, the extracts revealed that NO and collagenase activity were suppressed by 42% and 23%, respectively. The extracts can suppress ROS, inflammatory, and collagenase activities without causing fibroblast and keratinocyte cell death. Thus, this study provides information on metabolites in G. speciosum leaves, which is promising as cosmeceuticals or pharmaceuticals with anti-inflammatory and anti-collagenase activities.

Anti-Aging Potential of Extracts from Washingtonia filifera Seeds

The aim of this study was to test the inhibitory effect of fruit extracts from Washingtonia filifera on skin aging-related enzymes. The pulp extracts did not exert a significant enzyme inhibition while seed extracts from W. filifera exhibit anti-elastase, anti-collagenase, and anti-tyrosinase activities. Tyrosinase was mildly inhibited while a stronger effect was observed with respect to elastase and collagenase inhibition. Alcoholic extracts provided better results than aqueous extracts. Among them, methanol extracts showed the prominent enzyme inhibitory activities being IC50 value for elastase and collagenase comparable and even better than the reference compound. The inhibition mode of the most active extracts was investigated by Lineweaver-Burk plot analysis. Seed extracts from W. filifera were also investigated for their photo-protective effect by Mansur equation and the antioxidant activity of W. filifera extract was evaluated in oxidative-stressed cells. To evaluate the safety of the extract, the effect on cell viability of human keratinocytes cells was analyzed. Methanol extract presented the best photo-protective effect and exerted an antioxidant activity in a cellular system with no cytotoxic effect. The overall results demonstrate that W. filifera extracts are promising sources of bioactive compounds that could be used in cosmetic and pharmaceutical preparation.

Secondary metabolites changes in germinated barley and its relationship to anti-wrinkle activity

The purpose of this research was to identify metabolite change during barley (Hordeum vulgare) germination and reveal active principles for the anti-wrinkle activity. Barley was germinated with deionized water (DW) and mineral-rich water (MRW) for the comparison of the effect of mineral contents on the metabolites changes during germination. The effects of germinated barley extracts (GBEs) on collagen production and collagenase inhibition were evaluated in vitro using human dermal fibroblasts (HDFs). A pronounced anti-wrinkle activity was observed in the test group treated with the MRW-GBEs. In order to find out the active components related to the anti-wrinkle activity, an orthogonal projection to latent structure-discriminant analysis (OPLS-DA) was performed, using the data from secondary metabolites profiling conducted by UPLC–PDA–ESI–MS. The anti-wrinkle activity of MRW-GBEs was revealed to be associated with the increase of oligomeric compounds of procyanidin and prodelphinidin, indicating that it can be used as an active ingredient for anti-wrinkle agents.

IN VITRO ANTI-WRINKLE AND TYROSINASE INHIBITORY ACTIVITIES OF GRAPEFRUIT PEEL and STRAWBERRY EXTRACTS

The research aims to analyse the antioxidant, anti-tyrosinase and anti-wrinkle activities from grapefruit (Citrus Maxima L) and strawberry extracts. Samples were extracted by maceration using 96% ethanol and ethyl acetate, subsequently. The Ferric Reducing Antioxidant Power (FRAP) and β-carotene bleaching (BCB) were used to measure the antioxidant activity. The effect of anti-wrinkle was determined by testing the inhibition of elastase and collagenase enzyme, while anti-tyrosinase activity was analysed using mushroom tyrosinase enzyme. The results showed that strawberry extracts in ethanolic (SE) and ethyl acetate (SEA) have antioxidant activity in FRAP (EC50 = 404.39 ± 3.27 µg / mL and 1978.65 ± 37.25 µg/mL) and BCB (IC50 = 292.30 ± 4.69 µg/mL and 671.11 ± 6.74 µg/mL). Whereas the grapefruit peel extracts both in ethanolic (GPE) and ethyl acetate (GPEA) have antioxidant activity in FRAP (EC50 219.47 ± 71.96 µg / ml and 309.44 ± 95.76 µg/ml) and BCB (EC50 245.19 ± 162.47 µg/ml and 567.54 ± 95.31 µg/ml). As positive standards for FRAP antioxidant analysis were quercetin and vitamin C which has IC50 respectively 18.97 ± 4.50 µg/mL and 24.47 ± 1.44 µg/mL. While in BCB analysis, Butylated Hydroxy Toluene (BHT) used as positive standard (IC50 38.68 ± 5.70 µg/mL). The samples of SE, SEA, GPE and GPEA showed tyrosinase inhibitory activity which the IC50 values were respectively 492.68 ± 1.43; 2658 ± 48.08; 3312.5 ± 222.74; 2985.17 ± 122.80 µg/ml. Kojic acid (IC50 111.52 ± 0.42 µg/ml) is used as positive standard in this study. In addition, SE, SEA, GPE and GPEA were able to inhibit elastase and collagenase enzymes, although their activities were still lower than the positive standard used in this study. Elastastinal in concentration 50 µg/mL giving elastase inhibition about 71.71 ± 0.81 µg/mL, while vitamin C in the same concentration showed collagenase inhibition about 66.79 ± 1.23 µg/mL. It can be concluded that the extract of strawberry and grapefruit peel has antioxidant, anti-tyrosinase and anti-wrinkle activity through inhibition of elastase and collagenase enzymes; thus, they can be used as antiaging cosmetic ingredients.

Evaluation of antioxidant and anti-collagenase activity of Rosa damascena L. flower petal and receptacle extract

Background: Rosa damascena L. is the most notable species of the Rosaceae family in the world, and has been used in food, cosmetics, and the pharmaceutical industry. Bioactive compounds in this flower are known to have several activities, such as antioxidant, antimicrobial, and anti-inflammatory. In this study, the antioxidant and collagenase inhibitory activities of R. damascena L. petal and receptacle extracts were evaluated. Methods: Ethanolic extraction of R. damascena L. petals (EERP) and R. damascena L. receptacles (EERR) were obtained, and bioactive compounds (flavonoids, phenolics, alkaloids, steroids, tannins, terpenoids, and triterpenoids) were classified by phytochemical screening. Antioxidant activities were analyzed by Ferric Reducing Antioxidant Power (FRAP) assay, while anti-collagenase analysis was examined through the inhibition of collagenase. Results: Phytochemical test revealed the presence of flavonoids, phenolics, alkaloids, steroids, triterpenoids, triterpenes, and tannin. EERP showed higher FRAP activity (164.23 ± 1.34 μM Fe(II)) than EERR (12.85 ± 6.19 μM Fe(II)). EERP also had higher inhibitory activity of collagenase (IC50 = 115.48±1.78 µM/mL) compared to EERR (IC50 = 141.96±6.13 µM/mL). Conclusions: R. damascena L. petal and receptacle ethanol extracts contain several components, such as phenolics, flavonoids, alkaloids, tannins, terpenes, triterpenoids, and steroids. These extracts exhibit antioxidant activity and collagenase inhibition. R. damascena L. petal extract showed higher antioxidant activity through FRAP assay and inhibitory activity of collagenase than R. damascena L. receptacle extract.

Elastase/Collagenase Inhibition Compositions of Citrus unshiu and Its Association with Phenolic Content and Anti-Oxidant Activity

Citrus fruits are rich sources of different phytochemicals for human health due to their high anti-oxidant capacity. However, the anti-aging effect of citrus fruits has not been well understood. In this study, methanol extracts taken at various developmental stages from tissues of Citrus unshiu was used to investigate its anti-aging effect by an elastase/collagenase inhibition assay, and a gas chromatography-mass spectrometry (GC-MS) analysis was carried out to identify the potential anti-aging compositions. The elastase/collagenase inhibitory activity was greatest in the flesh of immature green fruit (i.e., early July flesh (EJF)), and four candidate compounds were selected by GC-MS and evaluated by a collagenase inhibition assay. Three of the four candidate compounds (heptadecanoic acid, D-allose, and 5-hydroxymethyl-2-furaldehyde (HMF)) showed anti-aging activity, and the activity was highest in heptadecanoic acid, followed by D-allose and HMF. The total phenolic content (TPC), total flavonoid content (TFC), and anti-oxidant activity (DPPH and ferric reducing anti-oxidant power (FRAP) assay) were also investigated. Interestingly, the patterns of the total phenolic/flavonoid content and the anti-oxidant activity were different from that of the elastase/collagenase inhibitory activity. Flowers had the most anti-oxidant activity followed by immature fruit, and the fruit peels had more anti-oxidant activity than its flesh at all stages of development. This study demonstrated that the flesh of immature fruit and flowers of C. unshiu could be sources of anti-aging and anti-oxidant agents for human health, respectively.

Comparison of Antiaging and Antioxidant Activities of Protocatechuic and Ferulic Acids

Background: Skin-aging is a progressive changes in the skin combine with cumulative extrinsic factors which are mostly caused by free radicals caused by exposure to lots of free radicals molecules from pollutant, wrongly food intake, or too much sun bathing. These free radicals can be tackled by a treatment using antioxidants. Prevention of aging can be done by escalating antioxidant intake. Protocatechuic acid (PCA) and Ferulic acid (FA) have been known for their scavenging properties on free radicals and antiaging activity. Antioxidant and antiaging activity of both compounds have not been compared comprehensively before. Hence, current study was conducted to compare the potential of PCA and FA for their antioxidant and antiaging activities using various methods.Materials and Methods: Antioxidant analysis of PCA and FA was conducted using H2O2 scavenging assay, 2,2’-azinobis-3-ethylbenzo-thiazoline-6-sulfonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazil (DPPH), and ferric reducing antioxidant power (FRAP). Meanwhile, antiaging activities of PCA and FA were examined using inhibitory activities of tyrosinase, collagenase, elastase, hyaluronidase and tyrosinase.Results: IC50 of scavenging activity of ABTS were 125.18 µg/mL (PCA) and 35.55 µg/mL (FA), inhibition activity of collagenase were 126.16 µg/mL (PCA) and 52.85 µg/mL (FA) and inhibition activity of tyrosinase were 246.42 µg/mL (PCA), 253.58 µg/mL (FA).Conclusion: In conclusion, FA has better ABTS scavenging and collagenase inhibition activities compared to PCA. Meanwhile, PCA has better activity of tyrosinase inhibition than FA.Keywords: antioxidant, antiaging, ferulic acid, protocatechuic acid

Endogenous Collagenases Regulate Osteoclast Fusion

The precise regulation of osteoclast differentiation and function is crucial for the maintenance of healthy bone. Despite several reports of collagenase expression in bone tissues, the precise isoform expression as well as the role in osteoclasts are still unclear. In the present report, the expression of matrix metalloprotease (MMP)8 and MMP13 was confirmed in mouse bone marrow macrophage osteoclast precursors. The mRNA and protein expressions of both collagenases were significantly reduced by receptor activator of nuclear factor κB ligand (RANKL) stimulation. Notably, either inhibition of MMP expression by siRNA or treatment of cells with collagenase inhibitor Ro 32-3555 significantly augmented osteoclast fusion and resorption activity without affecting the osteoclast number. The inhibition of collagenase by Ro 32-3555 increased the expression of osteoclast fusion genes, Atp6v0d2 and Dcstamp, without affecting nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1) protein expression. The enhanced osteoclast fusion by collagenase inhibition appears to be mediated through an extracellular signal regulated kinase (ERK)-dependent pathway. Collectively, these data provide novel information on the regulation of osteoclast fusion process.

Absolute Configuration of Mycosporine-Like Amino Acids, Their Wound Healing Properties and In Vitro Anti-Aging Effects

Mycosporine-like amino acids (MAAs) are water-soluble metabolites, reported to exhibit strong UV-absorbing properties. They have been found in a wide range of marine organisms, especially those that are exposed to extreme levels of sunlight, to protect them against solar radiation. In the present study, the absolute configuration of 14 mycosporine-like-amino acids was determined by combining the results of electronic circular dichroism (ECD) experiments and that of advanced Marfey’s method using LC-MS. The crystal structure of a shinorine hydrate was determined from single crystal X-ray diffraction data and its absolute configuration was established from anomalous-dispersion effects. Furthermore, the anti-aging and wound-healing properties of these metabolites were evaluated in three different assays namely the inhibition of collagenase, inhibition of advanced glycation end products (AGEs) and wound healing assay (scratch assay).