Ascorbic Acid Treatments as Effective and Safe Anti-Aging Therapies for Sensitive Skin.

The most common signs of aging skin include a decrease in firmness and density, uneven skin tone, and a tendency to erythema. There is an ever-increasing interest in aesthetic treatments that maintain the skin's favorable appearance. However, such therapies are difficult in the case of sensitive skin, defined as a set of stimuli-triggered symptoms (stinging, erythema, burning, and itching) that would not appear in healthy skin. Sensitive skin is common and affects, to varying degrees, about half of the European population. This study was aimed at evaluating the effects of ascorbic acid-a known antioxidant-applied with sonophoresis and microneedling on the signs of photoaging in reactive and erythematous skin. A significant improvement in skin elasticity was observed after a series of tests. A significant reduction in erythema was observed after both therapies. The greatest reduction was observed on the cheeks after applying vitamin C combined with microneedling. At the same time, the results showed an excellent tolerance of both treatments, which proved them to be safe and effective.

An Overview of the Potential Medicinal and Pharmaceutical Properties of Ru(II)/(III) Complexes.

This review examines the existing knowledge about Ru(II)/(III) ion complexes with a potential application in medicine or pharmacy, which may offer greater potential in cancer chemotherapy than Pt(II) complexes, which are known to cause many side effects. Hence, much attention has been paid to research on cancer cell lines and clinical trials have been undertaken on ruthenium complexes. In addition to their antitumor activity, ruthenium complexes are under evaluation for other diseases, such as type 2 diabetes, Alzheimer's disease and HIV. Attempts are also being made to evaluate ruthenium complexes as potential photosensitizers with polypyridine ligands for use in cancer chemotherapy. The review also briefly examines theoretical approaches to studying the interactions of Ru(II)/Ru(III) complexes with biological receptors, which can facilitate the rational design of ruthenium-based drugs.

Mechanistic Studies of Arene-Ruthenium(II) Complexes with Carbothioamidopyrazoles as Alternative Cancer Drugs.

Arene-ruthenium(II) complexes with carbothioamidopyrazoles at the C-2 and C-5 positions have been recognized as chemotherapeutic agent alternatives to cisplatin and its oxaliplatin analogs. The aim of this study was to continue research on the biological aspect of arene-ruthenium(II) complexes and their anticancer activity. The present paper includes an additional 12 new tumor cells, analyzed by MTT, and employs a series of extended bioassays to better understand their potential mechanism of antitumor activity. The following tests were conducted: membrane permeability studies, intramolecular reactive oxygen and nitrogen species (ROS/RNS) assays, mitochondrial potential changes, DNA analysis by comet assay using the electrophoresis method, measurement of cleaved PARP protein levels, and determination of apoptotic and necrotic cell fractions by fluorescence microscopy. Additionally, the article presents lipophilicity studies based on RP-TLC and molecular docking studies. We hope that the presented data will prove useful in practical treatment, especially for patients with cancer.

A Subjective and Objective Assessment of Combined Methods of Applying Chemical Peels and Microneedling in Antiaging Treatments.

Combined methods of applying chemical peels and antioxidants could be an option for skin rejuvenation with no down-time. The penetration of active substances can be enhanced by microneedle mesotherapy. The study was conducted on a group of 20 female volunteers, aged 40-65 years. All volunteers received a series of eight treatments performed every seven days. The whole face was first treated with azelaic acid; following this, the right side received a 40% solution of vitamin C and the left side 10% vitamin C with microneedling. Hydration and skin elasticity were markedly improved, with better results observed on the microneedling side. Melanin and erythema index decreased. No significant side effects were seen. The combination of active ingredients and delivery techniques have great potential to enhance the effectiveness of cosmetic preparations, probably by multidirectional ways of action. In our study, we demonstrated that both 20% azelaic acid + 40% vitamin C treatment and 20% azelaic acid + 10% vitamin C + microneedle mesotherapy efficiently improved the assessed parameters of aging skin. However, the use of microneedling mesotherapy as a means of direct delivery of active compound to the dermis enhanced the effectiveness of the studied preparation.

Clinical evaluation of anti-aging effects of combined therapy-Azelaic acid, phytic acid, and vitamin C applied layer by layer in females with Fitzpatrick skin types II and III.

INTRODUCTION: Vitamins C, E, and A and substances of plant origin, including azelaic acid and phytic acid are frequently used in cosmetic preparations to counteract oxidative stress and negative effects of free radicals. The aim of the study was to evaluate a novel combined therapy consisting of azelaic acid, ascorbic acid, and phytic acid applied layer on layer. METHODS: Twenty study participants received a series of eight treatments performed every 7 days. Twenty percent azelaic acid and then 30% phytic acid were applied to the entire face, while 40% l-ascorbic acid only on the left side. The preparations were applied layer by layer. Skin parameters were measured before the series of treatments (T0), after the series of eight treatments (T1-8 weeks), and 1 month after the end of the treatment (T2-12 weeks). RESULTS: The application of two and three active compounds resulted in a significant improvement in erythema and hyperpigmentation both on the forehead and the cheeks, however, more pronounced effects were observed when all the three active compounds were used. Both applied types of treatment considerably increased skin moisture. All the participants (100%) were satisfied with the effects of the treatment. A majority of them reported an improvement in skin hydration, firmness, and elasticity, more uniform skin tone and a reduction of skin redness and wrinkles. CONCLUSIONS: Topical application of these active compounds resulted in improvement of skin elasticity and flexibility, reduction of wrinkles, hyperpigmentation, erythema, and telangiectasia as well as amelioration of skin tone.

Biochemical, Structural Analysis, and Docking Studies of Spiropyrazoline Derivatives.

In this study, we evaluated the antiproliferative potential, DNA damage, crystal structures, and docking calculation of two spiropyrazoline derivatives. The main focus of the research was to evaluate the antiproliferative potential of synthesized compounds towards eight cancer cell lines. Compound I demonstrated promising antiproliferative properties, especially toward the HL60 cell line, for which IC50 was equal to 9.4 µM/L. The analysis of DNA damage by the comet assay showed that compound II caused DNA damage to tumor lineage cells to a greater extent than compound I. The level of damage to tumor cells of the HEC-1-A lineage was 23%. The determination of apoptotic and necrotic cell fractions by fluorescence microscopy indicated that cells treated with spiropyrazoline-based analogues were entering the early phase of programmed cell death. Compounds I and II depolarized the mitochondrial membranes of cancer cells. Furthermore, we performed simple docking calculations, which indicated that the obtained compounds are able to bind to the PARP1 active site, at least theoretically (the free energy of binding values for compound I and II were -9.7 and 8.7 kcal mol-1, respectively). In silico studies of the influence of the studied compounds on PARP1 were confirmed in vitro with the use of eight cancer cell lines. The degradation of the PARP1 enzyme was observed, with compound I characterized by a higher protein degradation activity.

Arene-Ruthenium(II) Complexes with Carbothiamidopyrazoles as a Potential Alternative for Antibiotic Resistance in Human.

To meet the demand for alternatives to commonly used antibiotics, this paper evaluates the antimicrobial potential of arene-ruthenium(II) complexes and their salts, which may be of value in antibacterial treatment. Their antimicrobial activity (MIC, MBC/MFC) was examined in vitro against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Pseudomonas aeruginosa, Proteus vulgaris and Candida albicans and compared with classic antibiotics used as therapeutics. Selected arene-ruthenium(II) complexes were found to have synergistic effects with oxacillin and vancomycin against staphylococci. Their bactericidal effect was found to be associated with cell lysis and the ability to cut microbial DNA. To confirm the safety of the tested arene-ruthenium(II) complexes in vivo, their cytotoxicity was also investigated against normal human foreskin fibroblasts (HFF-1). In addition, the antioxidant and thus pro-health potential of the compounds, i.e., their nonenzymatic antioxidant capacity (NEAC), was determined by two different methods: ferric-TPTZ complex and DPPH assay.

Long-term effect of azelaic acid peel on sebum production in acne.

Seborrhea and the associated oily skin are undoubtedly the problem of women and men around the world. The pathogenesis of acne vulgaris involves excessive activity of sebaceous glands, as well as disturbances in the composition of sebum. The aim of the study was to assess the severity of seborrhea in a group of acne vulgaris patients and to determine the effect of a 20% azelaic acid solution on the activity of sebaceous glands. Twenty seven women, aged 19-25 years, underwent a series of six treatments with the application of a 20% solution of azelaic acid to the face. The mean values of sebum level showed a decreasing tendency. On the forehead, the results were as follows-195.5 before the treatment and 162.7 2 weeks after the last treatment. Measurements of the right cheek decreased from 175.3 to 141.3 The measurements taken 3 months after the study were 151.3 on the forehead and 138.9 on the cheek. Similarly, the values determining the total number of acne lesions and the severity of the disease according to the IGA scale also changed significantly. Chemical peel with 20% azelaic acid shows long-term sebostatic action, which inhibits the formation of new acne lesions.

The Anti-Acne Effect of Near-Infrared Low-Level Laser Therapy.

BACKGROUND: Acne vulgaris is a skin problem affecting many people of different ages. Phototherapy is one of the acne treatment options. The aim of the study was to assess the effect of near-infrared low-level laser therapy on acne lesions. MATERIALS AND METHODS: The prospective study involved a total number of 27 women, aged 18 to 45 years, with mild to severe acne. All the participants underwent a series of six treatments with the use of a 785 nm low-level laser with the power density 80mW/cm2, performed every two weeks. The analysis of the effectiveness of the performed procedures was based on sebumetric examination, photographic documentation and assessment of the change in the number of acne lesions. RESULTS: Significant improvements in acne lesions (assessed as non-inflammatory and inflammatory lesion counts) and a significant decrease in skin sebum excretion were observed after the treatment. No adverse effects were reported. CONCLUSION: A series of six treatments using a near-infrared low-level laser represents a safe and effective non-invasive therapy option for acne vulgaris.

Overview of the Antioxidant and Anti-Inflammatory Activities of Selected Plant Compounds and Their Metal Ions Complexes.

Numerous plant compounds and their metal-ion complexes exert antioxidative, anti-inflammatory, anticancer, and other beneficial effects. This review highlights the different bioactivities of flavonoids, chromones, and coumarins and their metal-ions complexes due to different structural characteristics. In addition to insight into the most studied antioxidative properties of these compounds, the first part of the review provides a comprehensive overview of exogenous and endogenous sources of reactive oxygen and nitrogen species, oxidative stress-mediated damages of lipids and proteins, and on protective roles of antioxidant defense systems, including plant-derived antioxidants. Additionally, the review covers the anti-inflammatory and antimicrobial activities of flavonoids, chromones, coumarins and their metal-ion complexes which support its application in medicine, pharmacy, and cosmetology.

Zinc(II) and nickel(II) complexes of 3,5-dimethyl-1-(pyridin-2-yl)-1H-pyrazole: relationship between fluorescence and crystal packing.

Two novel coordination complexes, namely, dichlorido[3,5-dimethyl-1-(pyridin-2-yl-κN)-1H-pyrazole-κN2]zinc(II), [ZnCl2(C10H11N3)], 1, and aquachloridobis[3,5-dimethyl-1-(pyridin-2-yl-κN)-1H-pyrazole-κN2]nickel(II) chloride monohydrate, [NiCl(C10H11N3)(H2O)]Cl·H2O, 2, have been synthesized. The crystal structure analyses revealed that complexes 1 and 2 are mononuclear and have ZnN2Cl2 distorted tetrahedral and NiN4OCl distorted octahedral structures, respectively. Complex 1 displays a dimer in the crystal structure, while complex 2 forms a chain along the [010] direction. The fluorescence properties of both complexes were also investigated. A search of the Cambridge Structural Database for other complexes of the ligand 3,5-dimethyl-1-(pyridin-2-yl)-1H-pyrazole (L) shows that there exist different coordination polyhedra with different arrangements as monomers, dimers and polycyclic structures. Here it has also been demonstrated that there is a relationship between the crystal packing and the fluorescence properties of ZnII and CdII complexes of L.

Efficacy of 30% azelaic acid peel in the nonpharmacological treatment of facial acne.

BACKGROUND: Acne is a common, chronic, inflammatory disease of the pilosebaceous unit. It has a significant impact on patient quality of life, especially when lesions occur on cosmetically sensitive areas. Chemical peeling is a well-known option in the treatment of acne vulgaris, but little is known about azelaic acid (AZA) peels. OBJECTIVES: To determine the efficacy of 30% AZA peel, in decreasing the amount of secreted sebum, and reducing acne lesions. METHODS: The study involved 35 women, with acne lesions on face skin. All the subjects underwent a series of six treatments, performed every 2 weeks. RESULTS: A series of treatments contributed to a statistically significant reduction in the amount of secreted sebum. Similarly, highly significant values determining the overall number of acne lesions and the severity of the disease according to the IGA scale were also changed. The procedure was well tolerated by all participants. CONCLUSIONS: Peels with 30% AZA reduced acne lesions and normalized the activity of the sebaceous glands. The reduction of sebum allows us to believe that obtained good results in patients will be stable and long-lasting.

The relationship between Hirshfeld potential and cytotoxic activity: a study along a series of flavonoid and chromanone derivatives.

The present study examines a series of six biologically-active flavonoid and chromanone derivatives by X-ray crystal structure analysis: (E)-3-benzylidene-2-phenylchroman-4-one, C22H16O2, I, (E)-3-(4-methylbenzylidene)-2-phenylchroman-4-one, C23H18O2, II, (E)-3-(3-methylbenzylidene)-2-phenylchroman-4-one, C23H18O2, III, (E)-3-(4-methoxybenzylidene)-2-phenylchroman-4-one, C23H18O3, IV, (E)-3-benzylidenechroman-4-one, C16H12O2, V, and (E)-3-(4-methoxybenzylidene)chroman-4-one, C17H14O3, VI. The cytotoxic activities of the presented crystal structures have been determined, together with their intermolecular interaction preferences and Hirshfeld surface characteristics. An inverse relationship was found between the contribution of C...C close contacts to the Hirshfeld surface and cytotoxic activity against the WM-115 cancer line. Dependence was also observed between the logP value and the percentage contribution of C...H contacts to the Hirshfeld surface.

A Clinical Anti-Ageing Comparative Study of 0.3 and 0.5% Retinol Serums: A Clinically Controlled Trial.

BACKGROUND: Retinol influences the process of keratinization of the epidermis, which improves stratum corneum structure and reduces transepidermal water loss. It also significantly enhances mature skin by brightening hyperpigmentation and reducing the signs of photoageing. Cosmeceuticals are intended to both provide aesthetic effects for the skin and allow dermatological treatment. The aim of the study was to assess the rejuvenating effect of retinol serum on facial skin at concentrations of 0.3 and 0.5%, as well as any improvements in skin brightening and elasticity. MATERIALS AND METHODS: Thirty-seven volunteers were included in the study, after confirming tolerance. The novel formula was applied once daily to the face for a period of 12 weeks: one retinol concentration on the left side and the other on the right. The initial study with liquid crystal formula (study vehicle) was carried out for 8 weeks on 28 volunteers. Treatment efficiency was evaluated at baseline, and 56 and 84 days following treatment using the multi probe adapter and Fotomedicus imaging system. PRIMOS was used to measure skin surface roughness. The visual analogue scale method enabled the results to be determined by 3 independent specialists. RESULTS: Skin hyperpigmentation, unevenness, and wrinkles gradually decreased over the course of treatment, both on the left and right parts of the face. Adverse events were predominantly mild or moderate skin irritation. More frequent and more intense symptoms were observed on the left side (0.5%). CONCLUSION: Retinol in liquid crystal formulation is safe and provides significant clinical benefits associated with unification of skin colour, overall skin tone, skin elasticity, and moisture. Regular use of retinol typically results in brightening of the skin and reduced signs of ageing. The objective findings confirmed the effectiveness of the procedures.

Biological Evaluation of 3-Benzylidenechromanones and Their Spiropyrazolines-Based Analogues.

A series of 3-benzylidenechrmanones 1, 3, 5, 7, 9 and their spiropyrazoline analogues 2, 4, 6, 8, 10 were synthesized. X-ray analysis confirms that compounds 2 and 8 crystallize in a monoclinic system in P21/n space groups with one and three molecules in each asymmetric unit. The crystal lattice of the analyzed compounds is enhanced by hydrogen bonds. The primary aim of the study was to evaluate the anti-proliferative potential of 3-benzylidenechromanones and their spiropyrazoline analogues towards four cancer cell lines. Our results indicate that parent compounds 1 and 9 with a phenyl ring at C2 have lower cytotoxic activity against cancer cell lines than their spiropyrazolines analogues. Analysis of IC50 values showed that the compounds 3 and 7 exhibited higher cytotoxic activity against cancer cells, being more active than the reference compound (4-chromanone or quercetin). The results of this study indicate that the incorporation of a pyrazoline ring into the 3-arylideneflavanone results in an improvement of the compounds' activity and therefore it may be of use in the search of new anticancer agents. Further analysis allowed us to demonstrate the compounds to have a strong inhibitory effect on the cell cycle. For instance, compounds 2, 10 induced 60% of HL-60 cells to be arrested in G2/M phase. Using a DNA-cleavage protection assay we also demonstrated that tested compounds interact with DNA. All compounds at the concentrations corresponding to cytotoxic properties are not toxic towards red blood cells, and do not contribute to hemolysis of RBCs.

Antagonists of Vitamin K-Popular Coumarin Drugs and New Synthetic and Natural Coumarin Derivatives.

Many natural coumarins and their chemically synthesized analogs and derivatives exert diverse properties, such as anticancer, antioxidant, anti-inflammatory, or anticoagulant, with the latter being of the utmost importance. The widely used warfarin, acenocoumarol, and phenprocoumon exert anticoagulant properties by inhibiting the vitamin K epoxide reductase complex. In this interdisciplinary review, we present biochemical principles of the coagulation processes and possible methods for their tuning based on the use of coumarins. We also summarize chemical methods of synthesis of coumarins and discuss structures and properties of those that have been used for a long time, as well as newly synthesized compounds. Brief information on the clinical use of coumarins and other anticoagulant drugs is given, including the severe effects of overdosing and methods for reversing their action.

An evaluation of the physicochemical parameters and the content of the active ingredients in original formulas containing retinol.

INTRODUCTION: Three original cosmetic formulations containing retinol as an active component with liquid crystal, lamellar, and lipid bases were prepared. The formulas contain different concentrations of retinol, that is, 0.5%, 0.3%, and 0.15%. OBJECTIVES: The aim of the study was to evaluate a spectrophotometric method for assessing the quantity of retinol in the nine cosmetic products and to determine the viscosity of each formula. MATERIALS AND METHODS: The formulations were tested for stability; final product testing was preceded by sample weighing and pH measurement as well as exposure to the light source from xenon lamp that maps solar radiation in the range of 310-800 nm. Microbiological purity test was performed according to the PN-EN ISO 29621:2011 method and viscosity carried out using a cone-plate digital rheometer (DV-III Brookfield, version 3.0) on 0.5 cm3 emulsion samples at 32°C. The retinol content in preparations was assayed by UV spectrophotometry. RESULTS: Each of prepared cosmetic products with retinol storing in a room temperature occurred to be stable. The liquid crystal emulsion has the higher viscosity than lamellar and lipid emulsions. Although the retinol concentration in lipid serum was determined with high accuracy, the method has some limitations associated with differences between the lipid cosmetic base and the lamellar and liquid crystal sera. Nevertheless, the UV spectrophotometric method described herein is a simple and highly accurate approach for determining the retinol content in lipid cosmetics: Its coefficient of correlation was R2  = 0.9982 with a relative standard deviation (n = 3) in the range of 0.5%-1.5%. CONCLUSION: The presented UV spectrophotometric method represents an effective tool for fast and accurate determination of retinol content in lipid formulations. Probably, the method could be used in studies of other retinol-based preparations, for example, medications, and for determining the effective life of retinol-containing products in storage.

Randomized parallel control trial checking the efficacy and impact of two concentrations of retinol in the original formula on the aging skin condition: Pilot study.

BACKGROUND: The aging process is defined as natural, biological, progressive, and physiologically irreversible phenomena occurring in the body. OBJECTIVE: We attempted to evaluate the efficacy and tolerability of treating signs of the aging skin using retinol 0.15% and 0.3%. Retinol was added to the original, developed liquid crystal formula. METHODS: Patients at two sites (n = 20, n = 20) presenting signs of aging applied a novel formulation of retinol at 0.15% (on the left) and 0.3% (on the right) concentrations daily to their faces for 2 months. An expert blinded evaluation of images was carried out after 8 weeks. Tolerability was assessed throughout the whole study. Positive results of the observational pilot study guaranteed a follow-up trial with the use of the higher concentration and another parallel study. RESULTS: In the observational pilot study, most of the participants showed an improvement in the overall skin condition. These improvements were assessed after 4 and 8 weeks. Those observed after 56 days were more remarkable than those identified 28 days, however, without any statistical significance. Application of retinol formula 0.3% and serum 0.15% gives similar results after 8 weeks of daily care. Both products improve the overall skin condition considerably, even the skin color, hydration, and radiance. In a VAS assessment, the number of wrinkles decreased and skin discoloration was reduced. Side effects such as burning, dryness, pruritus, and erythema during the 8-week study period were minimal. CONCLUSIONS: The topical formulation of liquid crystal serum with retinol 0.15% and 0.3% improves the overall skin condition after 8 weeks. Burning, pruritus, dryness, and erythema caused by the application of retinol 0.15% and 0.3% concentrations were minimal. Nevertheless, there were no significance changes found between the left and right side of the face. These encouraging results justify a longer-term study to determine whether topically applied retinol 0.3% can provide more benefits as compared to those observed after topical application of retinol 0.15%.

A blinded study assessment of the efficacy of an original formula with retinol in combination with sonophoresis.

An appropriately designed cosmetic product and regimen of treatment can improve facial skin appearance and provide good tolerability. The aim of the study was to evaluate the effect of 0.3 and 0.5% retinol in liquid crystal formula, applied with sonophoresis, on mature skin. Serum with various concentrations of retinol was applied to the left and right sides of the face and treated with ultrasound. The treatments were performed once a week for a period of 7 weeks. The skin condition before and after treatment was compared using the Fotomedicus system. The Visual Analogue Scale method enabled the results to be assessed by three independent specialists. The Multi Probe Adapter system was used to evaluate the efficacy of a series of treatments. Subjective assessment of volunteers identified perceived improvement of skin conditions. In addition, treatment was associated with greater skin moisture level, reduced wrinkling and decreased skin discoloration. Mild side effects appeared mainly after the first treatment and on the left side of the face with 0.5% retinol. More significant results may be obtained by extending the treatment duration in longer-term studies. Nonetheless, the findings confirmed the effectiveness of the procedures.

Crystal structures of (E)-3-(4-hy-droxy-benzyl-idene)chroman-4-one and (E)-3-(3-hy-droxy-benzyl-idene)-2-phenyl-chroman-4-one.

The synthesis and crystal structures of (E)-3-(4-hy-droxy-benzyl-idene)chroman-4-one, C16H12O3, I, and (E)-3-(3-hy-droxy-benzyl-idene)-2-phenyl-chroman-4-one, C22H16O3, II, are reported. These compounds are of inter-est with respect to biological activity. Both structures display inter-molecular C-H⋯O and O-H⋯O hydrogen bonding, forming layers in the crystal lattice. The crystal structure of compound I is consolidated by π-π inter-actions. The lipophilicity (logP) was determined as it is one of the parameters qualifying compounds as potential drugs. The logP value for compound I is associated with a larger contribution of C⋯H inter-action in the Hirshfeld surface.