Mangiferin: A promising natural xanthone from Mangifera indica for the control of acyclovir - resistant herpes simplex virus 1 infection.

Mangiferin is found in many plant species as the mango tree (Mangifera indica) with ethnopharmacological applications and scientific evidence. The emergence of resistant herpes simplex virus (HSV) strains to Acyclovir (ACV) has encouraged the search for new drugs. We investigated the in vitro and in vivo activity of mangiferin obtained from M. indica against ACV-resistant HSV-1 (AR-29) and sensitive (KOS) strains. The in vitro activity was performed under varying treatment protocols. The substance showed a CC50 > 500 µg/mL and IC50 of 2.9 µg/mL and 3.5 µg/mL, respectively, for the AR-29 and KOS strains. The in vivo activity was performed in Balb/c mice treated with 0.7% topical mangiferin formulation. This formulation inhibited most effectively the AR-29 strain, attenuated the lesions, postponed their appearance or enhanced healing, in comparison to control group. We demonstrated the potentiality of mangiferin from M. indica to control HSV replication with emphasis to ACV-resistant infection.

Antiherpetic Effect of Topical Formulations Containing Sulfated Polysaccharide from Adenanthera pavonina.

Adenanthera pavonina is a native tree of Africa and Asia, introduced in Brazil for reforestation and wood industry. Several pharmacological activities have described scientifically, including antiviral activity. This study evaluated the antiviral effect of sulfated polysaccharide of Adenanthera pavonina (SPAp) against acyclovir (ACV)-resistant (AR-29) and sensitive (KOS) herpes simplex virus strains. The 50% cytotoxic concentration (CC50) was determined by MTT method and the 50% inhibitory concentration (IC50) was evaluated by plaque reduction assay. The in vivo SPAp antiviral activity was performed in Balb/c mice infected by skin scarification and treated with topical 0.5% (w/w) SPAp formulations. SPAp showed a CC50 of 47.81 µg/mL and the IC50 were 0.49 µg/mL (SI = 97.5) and 0.54 µg/mL (SI = 88.5) for the strains KOS and AR-29, respectively. Our results demonstrated that mice treated with SPAp presented a delay in the development and progression of skin lesions compared with the control group.

Development and characterization of multiple emulsions for controlled release of Trichilia catigua (Catuaba) extract.

Considering the antioxidant activity of the Trichilia catigua extract (TCE), the aim of the current study was to develop and characterize W/O/W multiple emulsions containing different vegetable oils as a platform to deliver a TCE. The extract displayed antioxidant activity (IC50) of 4.59 µg/mL and total phenol content (TPC) of 50.84%. Formulations were prepared by the phase-inversion emulsification method and analyzed for morphological appearance, pH, conductivity, droplet size and distribution, content of active, rheological properties, in vitro release, skin permeation, and stability. Formulations prepared with canola oil were selected and displayed regular morphology, mean diameter 2.77 µm (without TCE), 3.07 µm with 0.5% and 3.23 µm with 1.0% TCE. Rheometry (flow) showed pseudoplastic behavior with minimal thixotropy for both systems. TCE could be released from emulsions containing 1.0% and 0.5% TCE in a controlled manner for 16 and 23 h, respectively. The emulsions allowed good retention of TCE in the skin (stratum corneum, epidermis, and dermis). In a 180-d assessment of accelerated chemical stability, TPC was more reduced for the emulsions at 40 °C; other parameters remained stable. Multiple emulsions containing TCE were developed, exhibited good characteristics, and may be considered for future investigations as anti-aging formulations for the skin.

Nail Lacquer Containing Origanum vulgare and Rosmarinus officinalis Essential Oils and Biogenic Silver Nanoparticles for Onychomycosis: Development, Characterization, and Evaluation of Antifungal Efficacy.

Onychomycosis is a common fungal nail infection for which new antifungals are needed to overcome antimicrobial resistance and the limitations of conventional treatments. This study reports the development of antifungal nail lacquers containing oregano essential oil (OEO), rosemary essential oil (REO), and biogenic silver nanoparticles (bioAgNPs). The formulations (F) were tested against dermatophytes using agar diffusion, ex vivo nail infection, and scanning electron microscopy techniques. They were evaluated for their pharmacotechnical characteristics and by FTIR-PAS to assess permeation across the nail. F-OEO and F-OEO/bioAgNPs were promising candidates for the final nail lacquer formulation, as they permeated through the nail and showed antifungal efficacy against dermatophytes-contaminated nails after 5 days of treatment. Treated nails exhibited decreased hyphae and spores compared to the untreated control; the hyphae were atypically flattened, indicating loss of cytoplasmic content due to damage to the cytoplasmic membrane. The formulations were stable after centrifugation and thermal stress, maintaining organoleptic and physicochemical characteristics. Both F-OEO and F-OEO/bioAgNPs had pH compatible with the nail and drying times (59-90 s) within the reference for nail lacquer. For the first time, OEO and bioAgNPs were incorporated into nail lacquer, resulting in a natural and nanotechnological product for onychomycosis that could combat microbial resistance.

Hydrogel-Containing Biogenic Silver Nanoparticles: Antibacterial Action, Evaluation of Wound Healing, and Bioaccumulation in Wistar Rats.

Wound infections are feared complications due to their potential to increase healthcare costs and cause mortality since multidrug-resistant bacteria reduce treatment options. This study reports the development of a carbomer hydrogel containing biogenic silver nanoparticles (bioAgNPs) and its effectiveness in wound treatment. This hydrogel showed in vitro bactericidal activity after 2 h, according to the time-kill assay. It also reduced bacterial contamination in rat wounds without impairing their healing since the hydrogel hydrophilic groups provided hydration for the injured skin. The high number of inflammatory cells in the first days of the skin lesion and the greater degree of neovascularization one week after wound onset showed that the healing process occurred normally. Furthermore, the hydrogel-containing bioAgNPs did not cause toxic silver accumulation in the organs and blood of the rats. This study developed a bioAgNP hydrogel for the treatment of wounds; it has a potent antimicrobial action without interfering with cicatrization or causing silver bioaccumulation. This formulation is effective against bacteria that commonly cause wound infections, such as Pseudomonas aeruginosa and Staphylococcus aureus, and for which new antimicrobials are urgently needed, according to the World Health Organization's warning.

Hydrogel Containing Oleoresin From Copaifera officinalis Presents Antibacterial Activity Against Streptococcus agalactiae.

Streptococcus agalactiae or Group B Streptococcus (GBS) remains a leading cause of neonatal infections worldwide; and the maternal vaginal-rectal colonization increases the risk of vertical transmission of GBS to neonates and development of infections. This study reports the in vitro antibacterial effect of the oleoresin from Copaifera officinalis Jacq. L. in natura (copaiba oil) and loaded into carbomer-hydrogel against planktonic and sessile cells of GBS. First, the naturally extracted copaiba oil was tested for the ability to inhibit the growth and metabolic activity of planktonic and sessile GBS cells. The time-kill kinetics showed that copaiba oil exhibited a dose-dependent bactericidal activity against planktonic GBS strains, including those resistant to erythromycin and/or clindamycin [minimal bactericidal concentration (MBC) ranged from 0.06 mg/mL to 0.12 mg/mL]. Copaiba oil did not inhibit the growth of different Lactobacillus species, the indigenous members of the human microbiota. The mass spectral analyses of copaiba oil showed the presence of diterpenes, and the kaurenoic acid appears to be one of the active components of oleoresin from C. officinalis related to antibacterial activity against GBS. Microscopy analyses of planktonic GBS cells treated with copaiba oil revealed morphological and ultrastructural alterations, displaying disruption of the cell wall, damaged cell membrane, decreased electron density of the cytoplasm, presence of intracellular condensed material, and asymmetric septa. Copaiba oil also exhibited antibacterial activity against established biofilms of GBS strains, inhibiting the viability of sessile cells. Low-cost and eco-friendly carbomer-based hydrogels containing copaiba oil (0.5% - CARB-CO 0.5; 1.0% - CARB-CO 1.0) were then developed. However, only CARB-CO 1.0 preserved the antibacterial activity of copaiba oil against GBS strains. This formulation was homogeneous, soft, exhibited a viscoelastic behavior, and showed good biocompatibility with murine vaginal mucosa. Moreover, CARB-CO 1.0 showed a slow and sustained release of the copaiba oil, killing the planktonic and sessile (established biofilm) cells and inhibiting the biofilm formation of GBS on pre-coated abiotic surface. These results indicate that carbomer-based hydrogels may be useful as topical systems for delivery of copaiba oil directly into de vaginal mucosa and controlling S. agalactiae colonization and infection.

Statistical mixture design selective extraction of compounds with antioxidant activity and total polyphenol content from Trichilia catigua.

Statistical design mixtures of water, methanol, acetone and ethanol were used to extract material from Trichilia catigua (Meliaceae) barks to study the effects of different solvents and their mixtures on its yield, total polyphenol content and antioxidant activity. The experimental results and their response surface models showed that quaternary mixtures with approximately equal proportions of all four solvents provided the highest yields, total polyphenol contents and antioxidant activities of the crude extracts followed by ternary design mixtures. Principal component and hierarchical clustering analysis of the HPLC-DAD spectra of the chromatographic peaks of 1:1:1:1 water-methanol-acetone-ethanol mixture extracts indicate the presence of cinchonains, gallic acid derivatives, natural polyphenols, flavanoids, catechins, and epicatechins.

Avaliação da atividade antisséptica de sabonete líquido contendo extrato glicólico de flores de Tagetes patula L / Sessment of antiseptic activit y of liquid soap with glycolic extract of Tagetes patula l. flowers

Tagetes patula L. (Asteraceae), popularmente conhecida como cravo de defunto ou cravo francês, é utilizada na medicina popular como antisséptica, depurativa do sangue e repelente de insetos. O presente estudo avaliou a atividade antisséptica de sabonete líquido contendo extrato glicólico de T. patula 7,5% (p/v). O extrato glicólico foi obtido por turbo-extração utilizando propilenoglicol e etanol (7:3; v/v) a 10 % (p/v). A avaliação fitoquímica preliminar da droga vegetal indicou a presença de compostos fenólicos e teor de flavonoides de 5,73% ± 0,19 (CV = 3,33%). No teste para avaliação da atividade antimicrobiana houve a inibição do crescimento de Staphylococcus aureus na concentração de avaliada.

Tagetes patula L. (Asteraceae), or French marigold, known in Brazil as cravo-de-defunto, is used in folk medicine as antiseptic, blood thinner and insect repellent. Current study analyzes the antiseptic activity of the liquid soap with the glycolic extract of T.patula 7.5% (p/v). Glycolic extract was obtained by turbo-extraction with propylenoglycol and ethanol (7:3; v/v) 10 % (p/v). Preliminary photochemical evaluation of the vegetal drug showed phenolic compounds and flavonoid rates at 5.73% ± 0.19 (CV = 3.33%). When the pharmaceutical formulation was evaluated for antimicrobial activity, growth inhibition of Staphylococcus aureus occurred at the assessed concentration.

Avaliação do fator de proteção solar em fotoprotetores acrescidos com extratos da flora brasileira ricos em substâncias fenólicas / Evaluation of the Sun Protection Factor in sunscreens added to with vegetable extracts rich in phenolic substances

Sabe-se que o número de casos de câncer de pele tem crescido muito nos últimos anos. Com isso, novos produtos são constantemente desenvolvidos no intuito de aumentar a gama de substâncias para proteção solar. O principal objetivo desse trabalho foi a análise in vitro da propriedade fotoprotetora de uma formulação contendo filtros solares químicos, adicionada de extratos brutos de Guazuma ulmifolia, Maytenus ilicifolia, Stryphnodendron adstringens e Trichilia catigua, respectivamente, e a avaliação quanto ao acréscimo do Fator de Proteção Solar (FPS). O ensaio foi conduzido pelo método espectrofotométrico in vitro do Fator de Proteção Solar (FPS). O teor de Polifenóis Totais (PT) e sua correlação com a Capacidade Antioxidante (CA) dos extratos avaliados foram realizados. Os resultados demonstram que as formulações foram estáveis após a adição dos extratos, quanto a características físico-químicas (características macroscópicas, ensaio de centrifugação e pH) quando comparadas ao controle. O ensaio de FPS in vitro demonstrou decaimento do FPS das formulações acrescidas de extratos vegetais ricas em compostos fenólicos, exceto para o extrato de S. adstringens. Os FPS obtidos para os extratos foram ≤2. O teor em PT foram (%): G. ulmifolia, 24,26±0,34; M. ilicifolia, 14,66±0,18; S. adstringens, 34,38±0,62 e T. catigua, 41,60±0,13. Os valores da CA (IC50) frente ao radical DPPH foram (miug/mL): vitamina C (7,52±0,12), G. ulmifolia (8,94±0,13), M. ilicifolia (38,41±0,93), S. adstringens (7,31±0,15) e T. catigua (5,48±0,04). A CA foi diretamente proporcional ao teor de PT.

It is known that the number of cases of skin cancer has increased greatly in recent years. Therefore, new products are constantly developed in order to increase the range of substances for sun protection. The aim of this study was evaluate in vitro the property the sunscreen containing chemical sunscreens, with added to extracts of Guazuma ulmifolia, Maytenus ilicifolia, Stryphnodendron adstringens and Trichilia catigua, Sun Protection Factor (SPF). The test was conducted by the spectrophotometric method of in vitro Sun Protection Factor (SPF). The percentage of the Total Polyphenol (TP) and its correlation with Antioxidant Capacity (CA) of the extracts evaluated were performed. The results show that the formulations were stable after the addition of extracts, in relation as the physico-chemical characteristics (macroscopic characteristics, test centrifugation and pH) when compared to control (time 0). The FPS test in vitro showed decrease SPF of the formulations added of plant extracts rich in phenolic compounds, except for the extract of S. adstringens. The FPS for the extracts obtained were ≤2. The percentage of the PT were (%): G. ulmifolia, 24,26±0,34; M. ilicifolia, 14,66±0,18; S. adstringens, 34,38±0,62 e T. catigua, 41,60±0,13. The values of CA (IC50) against the DPPH radical were (miug/mL): vitamin C (7,52±0,12), G. ulmifolia (8,94±0,13), M. ilicifolia (38,41±0,93), S. adstringens (7,31±0,15) e T. catigua (5,48±0,04). CA was directly proportional to the content of PT.