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Lepidium peruvianum—an edible herbaceous biennial plant distributed in the Andes—has been used for centuries as food and as a natural medicine in treating hormonal disorders, as an antidepressant, and as an anti-osteoporotic agent. The presented study aims to prove its beneficial cosmetic and chemopreventive properties by testing the antiradical, whitening, cytotoxic, and anticancer properties of differently colored phenotypes that were extracted using three solvents: methanol, water, and chloroform, with the help of the chemometric approach to provide evidence on the impact of single glucosinolanes (seven identified compounds in the HPLC-ESI-QTOF-MS/MS analysis) on the biological activity of the total extracts. The tested extracts exhibited moderate antiradical activity, with the methanolic extract from yellow and grey maca phenotypes scavenging 49.9 ± 8.96% and 48.8% ± 0.44% of DPPH radical solution at a concentration of 1 mg/mL, respectively. Grey maca was the most active tyrosinase inhibitor, with 72.86 ± 3.42% of the enzyme activity calculated for the water extract and 75.66 ± 6.21% for the chloroform extract. The studies in cells showed no cytotoxicity towards the human keratinocyte line HaCaT in all studied extracts and a marked inhibition of cell viability towards the G361 melanoma cell line, which the presence of pent-4-enylglucosinolate, glucotropaeolin, and glucoalyssin in the samples could have caused. Given all biological activity tests combined, the three mentioned compounds were shown to be the most significant positive contributors to the results obtained, and the grey maca water extract was found to be the best source of the former compound among the tested samples. [ABSTRACT FROM AUTHOR]

The genus Vaccinium is represented by shrubs growing in a temperate climate that have been used for ages as traditional remedies in the treatment of digestive problems, in diabetes, renal stones or as antiseptics due to the presence of polyphenols (anthocyanins, flavonoids and tannins) in their fruits and leaves. Recent studies confirm their marked potential in the treatment of skin disorders and as skin care cosmetics. The aim of this review is to present the role of Vaccinium spp. as cosmetic products, highlight their potential and prove the biological properties exerted by the extracts from different species that can be useful for the preparation of innovative cosmetics. In the manuscript both skin care and therapeutic applications of the representatives of this gender will be discussed that include the antioxidant, skin lightening, UV-protective, antimicrobial, anti-inflammatory, and chemopreventive properties to shed new light on these underestimated plants. [ABSTRACT FROM AUTHOR]

Garlic (Allium sativum L.) has a reputation as a therapeutic agent for many different diseases such as microbial infections, hypertension, hypercholesterolaemia, diabetes, atherosclerosis and cancer. Health benefits of garlic depend on its content of biologically-active compounds, which differs between cultivars and geographical regions. The aim of this study was to evaluate and compare the biological activity of aqueous extracts from nine garlic varieties from different countries (Poland, Spain, China, Portugal, Burma, Thailand and Uzbekistan). Antioxidant properties were evaluated through free radical scavenging (DPPH•, ABTS•+) and ion chelation (Fe2+, Cu2+) activities. The cytotoxicity of garlic extracts was evaluated in vitro using Neutral Red Uptake assay in normal human skin fibroblasts. The obtained results revealed that garlic extracts contained the highest amount of syringic and p-hydroxybenzoic acids derivatives. The lowest IC50 values for DPPH•, ABTS•+ scavenging and Cu2+ chelating ability were determined in Chinese garlic extracts (4.63, 0.43 and 14.90 μg/mL, respectively). Extracts from Spanish cultivar Morado and Chinese garlic were highly cytotoxic to human skin fibroblasts as they reduced cellular proliferation by 70–90%. We showed diverse contents of proteins and phenolic components in garlic bulbs from different varieties. The obtained results could help to choose the cultivars of garlic which contain significant amounts of active compounds, have important antioxidant properties and display low antiproliferative effect and/or low cytotoxicity against normal human skin fibroblast BJ.

Simple Summary: Drugs used to treat cancer are most often very toxic. Taking their high doses may adversely affect the patient's health, as a result of which the therapy, instead of helping, harms. An example of such a drug is 6-mercaptopurine, described in this paper. Due to these negative properties, it is necessary to create such systems that would release the drug in a controlled manner only in the vicinity of diseased tissues. In this work, a drug carrier was prepared that releases the drug only in the acidic environment of cancer, due to which healthy tissues will not be exposed to it. Systems that release the drug only in an acidic environment have not been described before and the application potential of such a carrier is very large. Hydroxy double salts are layered materials that are considered to be biocompatible. For this reason, research has been initiated on the possibility of their use in drug delivery. Despite their use for several types of drugs, their potential for controlled release of mercaptopurine (MERC) has not been studied. In this work, the synthesized hydroxy double salt (HDS) material was used as a carrier for this drug for the first time. The effectiveness of HDS synthesis has been proven by such techniques as X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). Based on the FT-IR and energy-dispersive X-ray spectroscopy (EDS) results, the effectiveness of drug sorption was proven. The exact amount of drug retained was determined by the UV-Vis technique. The obtained results indicate that the drug is evenly distributed on the surface of the carrier, which is important during the controlled delivery of drugs. In the most important stage of the research, the effectiveness of drug release in response to changes in the pH of the environment was proven. The drug is not released into an environment that mimics healthy human tissues. It is released only after contact with the acidic environment that usually surrounds cancer cells. The low cellular toxicity of HDS and significant cytotoxic effect of HDS-MERC were confirmed by in vitro studies on MCF-7 human breast and DU145 prostate cancer cell lines and non-cancerous keratinocytes HaCaT. Interestingly, coupling with the HDS carrier increased the cytotoxic effect of MERC towards DU145 cells. Such an "intelligent" drug carrier for mercaptopurine has not been previously described in the literature. The obtained results indicate its great potential. [ABSTRACT FROM AUTHOR]

The main aim of the study was to assess the acetylcholinesterase-inhibitory potential of triterpenoid saponins (astragalosides) found in the roots of Astragalus mongholicus. For this purpose, the TLC bioautography method was applied and then the IC50 values were calculated for astragalosides II, III and IV (5.9 μM; 4.2 μM, and 4.0 μM, respectively). Moreover, molecular dynamics simulations were carried outto assess the affinity of the tested compounds for POPC and POPG-containing lipid bilayers, which in this case are the models of the blood-brain barrier (BBB). All determined free energy profiles confirmed that astragalosides exhibit great affinity for the lipid bilayer. A good correlation was obtained when comparing the logarithm of n-octanol/water partition coefficient (logPow) lipophilicity descriptor values with the smallest values of free energy of the determined 1D profiles. The affinity for the lipid bilayers changes in the same order as the corresponding logPow values, i.e.,: I > II > III~IV. All compounds exhibit a high and also relatively similar magnitude of binding energies, varying from ca. −55 to −51 kJ/mol. Apositive correlation between the experimentally-determined IC50 values and the theoretically-predicted binding energies expressed by the correlation coefficient value equal 0.956 was observed. [ABSTRACT FROM AUTHOR]

Tyrosinase is a key enzyme in the melanogenesis pathway. Melanin, the product of this process, is the main pigment of the human skin and a major protection factor against harmful ultraviolet radiation (UVR). Increased melanin synthesis due to tyrosinase hyperactivity can cause hyperpigmentation disorders, which in consequence causes freckles, age spots, melasma, or postinflammatory hyperpigmentation. Tyrosinase overproduction and hyperactivity are triggered by the ageing processes and skin inflammation as a result of oxidative stress. Therefore, the control of tyrosinase activity is the main goal of the prevention and treatment of pigmentation disorders. Natural products, especially propolis, according to their phytochemical profile abundant in polyphenols, is a very rich resource of new potential tyrosinase inhibitors. Therefore, this study focused on the assessment of the tyrosinase inhibitory potential of six extracts obtained from the European propolis samples of various origins. The results showed the potent inhibitory activity of all tested propolis extracts towards commercially available mushroom tyrosinase. The four most active propolis extracts showed inhibitory activity in the range of 86.66–93.25%. Apart from the evaluation of the tyrosinase inhibition, the performed research included UHPLC–DAD–MS/MS (ultra high performance liquid chromatography coupled with diode array detection and tandem mass spectrometry) phytochemical profiling as well as antioxidant activity assessment using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the 2,2"-azino-bis(3-ethylbenzothiazoline-6-sulfuric acid (ABTS) radical scavenging tests. Moreover, statistical analysis was used to correlate the tyrosinase inhibitory and antioxidant activities of propolis extracts with their phytochemical composition. To summarise, the results of our research showed that tested propolis extracts could be used for skin cosmeceutical and medical applications. [ABSTRACT FROM AUTHOR]

Introduction: Halophytes are a group of relict plants found in areas with a high amount of easily soluble salts. They constitute a fascinating group of plants in terms of the high content and unique profile of active compounds, synthesized as defense mechanisms against stressful environmental conditions. Among produced compounds, antioxidants are the most common, as they reduce oxidative stress resulting from soil salinity or excessive solar exposure. Extracts and substances obtained from halophyte species may be a valuable source of active ingredients for multifunctional cosmetic products. Aim: The aim of the presented research was to analyze the cosmetic potential of aqueous (W) and hydroethanolic (70%, v/v, WE) extracts from the leaves and flowers of sea lavender (Limonium vulgare Mill.) and sea fennel (Crithmum maritimum L.). Material and methods: The extracts were compared for their antioxidant capacity by DPPH free radical scavenging assay, the content of active compounds and the depigmentation potential assessed by the tyrosinase inhibitory activity. Safety of the extracts was analyzed by the determination of cytotoxicity against human keratinocytes HaCaT in vitro. Results: The comparative studies have shown that sea lavender extracts have a higher cosmetic potential than sea fennel extracts. WE extracts from sea lavender flowers and leaves shown the greatest antioxidant capacity as they neutralize ca. 50% of the radical at the concentration of 0,008 mg/mL. The same extracts contain the highest levels of flavonoids (209,65 and 210,77 µg QE/mL respectively). The highest content of polyphenols (886,15 µg GAE/mL) and tyrosinase inhibitory potential were found in WE flower extract from sea lavender. At the concentration of 0.5 mg/mL the extract reduced the activity of tyrosinase by 83.7%. All analyzed extracts were not cytotoxic for cells in vitro. The highest cytotoxicity was observed for flower extracts of sea lavender (W) and sea fennel (WE) as at the concentration of 100 µg/mL they reduced the viability by ca. 22%. Conclusions: To sum up, extracts from sea lavender have a great application potential on the skin and can be used as active ingredients in skin care products with protecting and skin-lightening properties. [ABSTRACT FROM AUTHOR]

Introduction: "Zero Waste" is a philosophy of life and an economic approach to minimize the amount of waste produced by an individual or community. Aim: The aim of the research was to evaluate selected cosmetic properties (antioxidant, skin-lightening and cytotoxic) of aqueous (W) and hydroethanolic (70% v:v, WE) extracts obtained from flowers of H. arenarium and herbs of H. italicum. Materials and methods: In the cosmetics industry, this trend might be applicable in the production of natural cosmetics by the utilization of plant by-products of waste material (eg. leaves, stems, peels or foots) for the extraction of bioactive compounds. An example of a natural resource that could potentially be better utilized are immortelle species (Helichrysum arearium, Helichrysum italicum), rich in bioactive compounds with medicinal and cosmetic properties. The cosmetic industry uses mostly the extracts obtained from the flowers of Helichrysum species and the herbs (stems + leaves) are usually considered as waste. Results: The results showed that the WE herb extract of H. italicum has the highest antioxidant properties as at the concentration of 1 mg/mL it neutralized ca. 95% of DPPH and ca. 100% of ABTS free radicals. The skin-lightening potential of Helichrysum extracts was analyzed using the lysate of B16F10 murine melanoma cells, containing murine tyrosinase. W and WE flower extracts of H. arenarium and WE extract of H. italicum showed dose-dependent inhibitory effect on tyrosinase, reducing the activity of the enzyme by ca. 41-45% at the highest tested concentration (1 mg/mL). In vitro cytotoxicity studies showed that Helichrysum sp. extracts are not toxic for human keratinocytes HaCaT - the highest reduction of cellular viability (30%) was noted for WE herb extract of H. italicum at 250 μg/mL. Conclusions: To summarize, presented research showed that leaf extracts form Helichrysum sp. are valuable raw materials for the extraction of antioxidant, skin-lightening and safe active ingredients of cosmetics. [ABSTRACT FROM AUTHOR]

Introduction: Hyperpigmentation is one of the most common aesthetic problems and a target of many cosmetic products. Unfortunately, many of recently used skinlightening active ingredients are unstable in cosmetic formulations and lack expected effectiveness. Moreover, prolonged application of such ingredients often results in side effects, including skin irritation, contact dermatitis, leukoderma, or impaired wound healing. For this reason, modern cosmetology is constantly searching for new, effective and safe substances that reduce hyperpigmentation. The source of such substances are plant extracts. Aim: The presented research assessed the possibility of using pear (Pyrus communis L.) and bilberry (Vaccinium vitis-idaea L.). leaf extracts in skinlightening cosmetics. Leaves of this plant species are currently used mostly as waste material, therefore their utilization in the cosmetic industry might help in more sustainable usage of natural resources. Material and methods: The leaves were extracts in water (W extracts) or water:propylene glycol mixture (1:1,v:v, WG extracts) and compared for their phytochemical content (polyphenols and flavonoids) antioxidant activity (using DPPH and ABTS radical scavenging assays) and skin-lightening potential (using tyrosinase inhibitory assay). Results: Bilberry WG extract showed the highest content of polyphenols and flavonoids among all tested extract (2751,5 µg GAE/mL and 199,3 µg QE/mL, respectively). Bilberry W extracts was the most effective antioxidant in DPPH assay and the WG bilberry extracts was the most active in ABTS assay. The highest tyrosinase inhibitory properties were observed for 1% (v/v) bilberry WG and pear W extracts - both inhibited the tyrosinase activity by 25%. BoThextracts then incorporated in the formulation of cosmetic emulsion. To enhance the skin-lightening potential of the product kojic acid was also implemented in the formulation. Prepared cosmetic was analyzed for its physicochemical properties (colour, smell, viscosity, pH), microbiological safety and stability. Conclusions: Presented results showed in practice that pear and bilberry leaf extracts might be applied in formulations of skin lightening cosmetics. [ABSTRACT FROM AUTHOR]

Introduction: natural cosmetics are consistently gaining popularity in today's cosmetic market. To meet the systematically growing demand for unique natural cosmetics, the manufacturers are searching for innovative ingredients. Such an ingredient is dragon's blood, a latex from Croton lechleri tree. This resin is widely known in South American countries as it has played a significant role in traditional medicine thanks to its anti-microbial, anti-inflammatory, and wound-healing properties. Dragon's blood extracts are also used in cosmetic formulations. Aim: The aim of this study was to experimentally investigate the polyphenolic content, antioxidant activity of ethanolic, hydroethanolic (50%, v/v) and aqueous extract from dragon's blood as well as to evaluate the influence of dragon's blood extract on the stability of a prototypic cosmetic emulsion. Material and methods: The extracts were prepared using ultrasound-assisted extraction and filtered. The total polyphenolic content was compared using spectrophotometric method with Folin-Ciocalteu reagent and sodium carbonate. The antioxidant potential was determined using DPPH scavenging assay. The stability test of the prototypic cosmetic emulsion was carried out by storing it at various temperatures (4°C, 25°C, 40°C, -10°C) for 28 days. The study included organoleptic evaluation of color, consistency and odor as well as measurements of viscosity, density, and pH of the cosmetic. Results: Among the prepared extracts the ethanolic extract displayed the highest antioxidant activity (DPPH radical scavenging at 0.39% was above 90%) and polyphenolic content (1330.55 µg gallic acid equivalents, GAE/mL). Almost no antioxidant activity and significantly lowest content of polyphenols (23.15 µg GAE/mL) was determined for the aqueous extract. The addition of 1% (m/m) dragon's blood extract to the prototypic cosmetic emulsion did not affect its stability during the storage at various temperature conditions. Conclusions: To summarize, the results showed that dragon's blood extracts are auspicious active ingredients of cosmetic formulations. The addition of dragon's blood extract to the emulsion did not affect its stability and physiochemical properties. [ABSTRACT FROM AUTHOR]

Numerous species of Allium genus have been used in the traditional medicine based on their vast biological effects, e.g., antimicrobial, digestion stimulant, anti-sclerotic, soothing, antiradical or wound healing properties. In this work, unpolar and polar extracts from two lesser-investigated species of Allium growing in Kazakhstan, Alliumgalanthum Kar. & Kir. (AG) and A. turkestanicum Regel. (AT), were studied for their composition and biological effects. In the HPLC-ESI-QTOF-MS/MS analyses of water and alcoholic extracts simple organic acids, flavonoids and their glycosides were found to be the best represented group of secondary metabolites. On the other hand, in the GC-MS analysis diethyl ether, extracts were found to be rich sources of straight-chain hydrocarbons and their alcohols, fatty acids and sterols. The antimicrobial activity assessment showed a lower activity of polar extracts, however, the diethyl ether extract from AT bulbs and AG chives showed the strongest activity against Bacillus subtilis ATCC 6633, B. cereus ATCC 10876, some species of Staphylococcus (S. aureus ATCC 25923 and S. epidermidis ATCC 12228) and all tested Candida species (Candida albicans ATCC 2091, Candida albicans ATCC 10231, Candida glabrata ATCC 90030, Candida krusei ATCC 14243 and Candida parapsilosis ATCC 22019) with a minimum inhibitory concentration of 0.125–0.5 mg/mL. The highest antiradical capacity exhibited diethyl ether extracts from AG bulbs (IC50 = 19274.78 ± 92.11 mg Trolox eq/g of dried extract) in DPPH assay. In ABTS scavenging assay, the highest value of mg Trolox equivalents, 50.85 ± 2.90 was calculated for diethyl ether extract from AT bulbs. The same extract showed the highest inhibition of mushroom tyrosinase (82.65 ± 1.28% of enzyme activity), whereas AG bulb ether extract was the most efficient murine tyrosinase inhibitor (54% of the enzyme activity). The performed tests confirm possible cosmeceutical applications of these plants. [ABSTRACT FROM AUTHOR]

TMEFF2 is a type I transmembrane protein with two follistatin (FS) and one EGF-like domain over-expressed in prostate cancer; however its biological role in prostate cancer development and progression remains unclear, which may, at least in part, be explained by its proteolytic processing. The extracellular part of TMEFF2 (TMEFF2-ECD) is cleaved by ADAM17 and the membrane-retained fragment is further processed by the gamma-secretase complex. TMEFF2 shedding is increased with cell crowding, a condition associated with the tumour microenvironment, which was mediated by oxidative stress signalling, requiring jun-kinase (JNK) activation. Moreover, we have identified that TMEFF2 is also a novel substrate for other proteases implicated in prostate cancer, including two ADAMs (ADAM9 and ADAM12) and the type II transmembrane serine proteinases (TTSPs) matriptase-1 and hepsin. Whereas cleavage by ADAM9 and ADAM12 generates previously identified TMEFF2-ECD, proteolytic processing by matriptase-1 and hepsin produced TMEFF2 fragments, composed of TMEFF2-ECD or FS and/or EGF-like domains as well as novel membrane retained fragments. Differential TMEFF2 processing from a single transmembrane protein may be a general mechanism to modulate transmembrane protein levels and domains, dependent on the repertoire of ADAMs or TTSPs expressed by the target cell., (© 2017 The Authors. Cell Biology International published by John Wiley & Sons Ltd on behalf of International Federation of Cell Biology.)