The Potential of Vouacapanes from Pterodon emarginatus Vogel Against COVID-19 Cytokine Storm.

Purpose: The emergence of the COVID-19 pandemic has led to the search for potential therapeutic responses for various aspects of this disease. Fruits of Pterodon emarginatus Vogel (Fabaceae), sucupira, have been used in Brazilian traditional medicine because of their anti-inflammatory properties, which have been proven in vivo, in vitro, and in silico. Therefore, the aim of this work is to evaluate P. emarginatus oleoresin and isolated diterpenes by in vitro anti-inflammatory models. Methods: In this study, the mechanisms underlying the anti-inflammatory activity of P. emarginatus oleoresin and vouacapanes 6α,19ß-diacetoxy-7ß,14ß-dihydroxyvouacapan (V1), 6α-acetoxy-7ß,14ß-dihydroxyvouacapan (V2), and methyl 6α-acetoxy-7ß-hydroxyvouacapan-17ß-oate (V3) were investigated in HaCaT cells. Results: Oleoresin, V2, and V3 inhibited phospholipase A2 (30.78%, 24.96%, and 77.64%, respectively). Both vouacapanes also inhibited the expression of COX-2 (28.3% and 33.17%, respectively). The production of interleukin 6 (IL-6) was inhibited by oleoresin by 35.47%. However, oleoresin did not interfere with Nrf-2 expression or IL-8 production. Conclusion: The results support the ethnomedicinal use of P. emarginatus oleoresin as an anti-inflammatory herbal medicine, and also highlight P. emarginatus oleoresin and isolated vouacapanes as an attractive therapeutic approach for COVID-19 through the reduction or chronological control of the inflammatory mediators IL-6, cyclooxygenase-2 (COX-2), phospholipase A2, and INF-y (indirectly) during the SARS-CoV-2 infection process.

Enhanced Skin Permeation of Punicalagin after Topical Application of Pluronic Micelles or Vesicles Loaded with Lafoensia pacari Extract.

Punicalagin, the principal ellagitannin of Lafoensia pacari leaves, has proven antioxidant activity, and standardized extracts of L. pacari can be topically used for skin aging management. We hypothesized that Pluronic nanomicelles or vesicles could solubilize sufficiently large amounts of the standardized extracts of L. pacari and provide chemical stability to punicalagin. The standardized extracts of L. pacari were obtained with an optimized extraction procedure, and the antioxidant activity was characterized. Formulations containing Pluronic at 25% and 35% were obtained with or without Span 80. They were characterized by average diameter, polydispersity index, punicalagin content, physicochemical stability, and rheology. A release and skin permeation study was carried out in vertical diffusion cells. The extraction procedure allowed quantifying high punicalagin content (i.e., 141.61 ± 3.87 mg/g). The standardized extracts of L. pacari showed antioxidant activity for all evaluated methods. Pluronic at 25 and Pluronic at 35 with standardized extracts of L. pacari showed an average diameter of about 25 nm. The addition of Span 80 significantly increased the mean diameter by 15-fold (p < 0.05), indicating the spontaneous formation of vesicles. Pluronic formulations significantly protected punicalagin from chemical degradation (p < 0.05). Pluronic at 25 formulations presented as free-flowing liquid-like systems, while Pluronic at 35 resulted in an increase of about 44-fold in |ƞ*|. The addition of Span 80 significantly reduced the Pluronic sol-gel transition temperature (p < 0.05), indicating the formation of vesicles. Formulations with Span 80 significantly enhanced punicalagin skin permeation compared to formulations without Span 80 (p < 0.05). Formulations with Span 80 were demonstrated to be the most promising formulations, as they allowed significant permeation of punicalagin (about 80 to 315 µg/cm2), which has been shown to have antioxidant activity.

Treatment of cosmetic industry wastewater by flotation with Moringa oleifera Lam. and aluminum sulfate and toxicity assessment of the treated wastewater.

The production of personal hygiene and body products generates wastewater with a high load of surfactants, a high chemical oxygen demand (COD), and abundant oils and greases. Aluminum sulfate (AS) and two solutions of natural coagulant from Moringa oleifera Lam. seeds prepared with a 1M NaCl solution and 1.5M NaCl solution were used. Aluminum sulfate, Moringa oleifera Lam. in 1M NaCl, and Moringa oleifera Lam. in 1.5M NaCl solutions reduced turbidity at rates 94.48%, 98.07%, and 97.87%; reduced COD at rates 46.36%, 49.15%, and 42.7%; and reduced oil and grease at rates 98.72%, 78.65%, and 97.41%, respectively. Mutagenicity tests with guppies showed a lower toxicity of Moringa oleifera Lam. extract compared with aluminum sulfate. This work shows that Moringa oleifera Lam. extract has high potential for use as an alternative to aluminum sulfate; therefore, this study will contribute to proposals for the sustainable treatment of effluents from the cosmetic industry.

Crude plant extract versus single compounds for vitiligo treatment: Ex vivo intestinal permeability assessment on Brosimum gaudichaudii Trécul.

Roots´ bark extract of Brosimum gaudichaudii Trécul (EBGT) is traditionally used for photochemotherapy of vitiligo due to the presence of furanocoumarins psoralen (PSO) and 5-methoxypsoralen (5-MOP) as major compounds. Though plant extracts may provide additional highly permeable psoralens-like substances which may act synergically on vitiligo's therapy. Thus, the aim of this work was to develop an LC-MS/MS method for screening new highly permeable furanocoumarins from B. gaudichaudii and to compare biomarkers permeability and solubility provided as single compounds or as crude extract, according to BCS. An optimized LC-MS/MS method showed twelve permeable and bioactive compounds, among which 9 furanocoumarins, 2 pyranocoumarins and 1 dihydrocinnamic acid derivative were detected in EBGT samples. Solubility of PSO and 5-MOP was found to be, respectively, six- and eleven-fold higher in crude extract than as pure compounds. Permeability (Papp) of PSO and 5-MOP in EBGT were higher than metoprolol, the low/high BCS permeability class boundary reference compound. Hence, both biomarkers were considered as highly permeable (BCS2) compounds. Their permeability were concentration-dependent displaying values from 30.26 ± 5.13-8.21 ± 2.16 × 10-6 cm/s and 10.72 ± 1.73-6.07 ± 1.27 × 10-6 cm/s, respectively, over a wide range (2.3-200.0 mg mL-1). Thus, a carrier-mediated absorption process is suggested as the main mechanism. Accordingly, all additional permeated coumarins, identified by LC-MS/MS, showed to be at comparable amount of biomarkers in the permeated samples inferring similar high permeability rate. Moreover, biomarkers and other highly absorbable and bioactive linear furanocoumarins from EBGT may be used for vitiligo´s photochemotherapy. Taken together, these findings bring additional evidences for using crude plant extract when aiming synergistic effects of bioactive compounds on melanogenic therapies.

Curcuma supplementation in high-fat-fed C57BL/6 mice: no beneficial effect on lipid and glucose profile or prevention of weight gain.

PURPOSE: This experimental study investigated the effects of curcuma supplementation on weight gain, Body Adiposity Index, glucose and lipid profile, and liver and pancreas histology in C57BL/6 mice fed with a high-fat diet. METHODS: 40 animals were separated into four groups: standard diet (SD), standard diet plus curcuma (SD + C), high-fat diet (HFD), and high-fat diet plus curcuma (HFD + C). Curcuma dose was 8 mg/animal/day. Histological and biochemical analyses were performed at the end of the experimental period. RESULTS: Curcuma prevented weight gain, despite a higher food intake, and increased brown adipose tissue weight only in mice receiving standard diet. However, these changes were not observed in HFD + C group. The groups that received curcuma (SD + C and HFD + C) showed a pancreas with diffuse macro- and microgoticular steatosis. CONCLUSIONS: Curcuma supplementation did not prevent weight gain or improved glucose and lipid profile in mice receiving high-fat diet. Furthermore, there was evidence of possible curcuma toxicity in the pancreas of C57BL/6 mice. The implications of these findings on humans still need to be investigated.

Anti-inflammatory activity of nanoemulsions of essential oil from Rosmarinus officinalis L.: in vitro and in zebrafish studies.

The essential oil from Rosmarinus officinalis L. (OERO) has bioactive compounds with anti-inflammatory activity. The objective of this study was to evaluate the anti-inflammatory potency of nanoemulsions containing essential oil of Rosmarinus officinalis L. (NOERO, NECHA, NECULT, and NECOM) in vitro and in vivo. This study was accomplished in a quantitative format through tests with diphenyl picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cellular antioxidant activity (CCA), determination of nitric oxide production, cellular viability and anti-inflammatory activity in zebrafish. OERO's were submitted to the analysis-coupled gas chromatography-mass spectrometry (GC-MS), which highlighted 1,8-cineol and camphor as major compounds. NOEROs were obtained by a low-energy method and presenting the medium size smaller than 200 nm. The efficiency of encapsulation by spectrometry and gas chromatographic analysis was 67.61 and 75.38%, respectively. In the CCA assay, all of the samples presented percentage values of inhibition similar to the quercetin pattern, indicating antioxidant activity. In the test for determination of NO·, all of the samples inhibited the production of NO· when compared to LPS, and NOEROS were more effective than OEROS to 5 µg/mL. In the cell viability assay, the cells remained viable after contact with the samples, demonstrating an absence of cytotoxicity. This study showed that all nanoemulsions (NECHA, NECULT, and NECOM) showed no toxicity to macrophages, besides demonstrating antioxidant activity and potentiation of the essential oil effect in the proliferation of viable fibroblasts. Nanoemulsions has also shown the ability to potentiate the anti-inflammatory action of essential oils by exerting immunomodulatory activity by inhibiting the production of the pro-inflammatory mediator nitric oxide. The results obtained with NECHA in zebrafish confirm the hypothesis that prominent terpenic compounds, alpha-pinene, 1,8-cineole, and camphor, became more available at the target sites, inhibiting the inflammatory process in this animal species.

Development and Validation of a HPLC-UV Method for the Evaluation of Ellagic Acid in Liquid Extracts of Eugenia uniflora L. (Myrtaceae) Leaves and Its Ultrasound-Assisted Extraction Optimization.

A simple HPLC-UV method has been developed and validated for the quantification of ellagic acid (EA) in ethanol extracts of Eugenia uniflora L. (Myrtaceae) leaves. The ultrasound-assisted extraction (UAE) optimization was performed using a Box Behnken design (33) combined with response surface methodology to study the effects of the ethanol concentration (%, w/w), extraction time (minutes), and temperature (°C) on the EA concentration. The optimized results showed that the highest extraction yield of EA by UAE was 26.0 µg mL-1 when using 44% (w/w) ethanol as the solvent, 22 minutes as the extraction time, and 59°C as the extraction temperature. The concentration of EA in relation to the predicted value was 93.7% ± 0.4. UAE showed a strong potential for EA extraction.

Obtaining a Dry Extract from the Mikania laevigata Leaves with Potential for Antiulcer Activity.

BACKGROUND: Mikania laevigata leaves are commonly used in Brazil as a medicinal plant. OBJECTIVE: To obtain hydroalcoholic dried extract by nebulization and evaluate its antiulcerogenic potential. MATERIALS AND METHODS: Plant material and hydroalcoholic extract were processed and analyzed for their physicochemical characteristics. A method using HPLC was validated to quantify coumarin and o-coumaric acid. Hydroalcoholic extract was spray dried and the powder obtained was characterized in terms of its physicochemical parameters and potential for antiulcerogenic activity. RESULTS: The analytical method proved to be selective, linear, precise, accurate, sensitive, and robust. M. laevigata spray dried extract was obtained using colloidal silicon dioxide as adjuvant and was shown to possess 1.83 ± 0.004% coumarin and 0.80 ± 0.012% o-coumaric acid. It showed significant antiulcer activity in a model of an indomethacin-induced gastric lesion in mice and also produced a gastroprotective effect. CONCLUSION: This dried extract from M. laevigata could be a promising intermediate phytopharmaceutical product. SUMMARY: Research and development of standardized dried extract of Mikania laevigata leaves obtained through spray drying and the production process was monitored by the chemical profile, physicochemical properties and potential for anti-ulcerogenic activity. Abbreviations used: DE: M. laevigata spray dried extract, HE: hydroalcoholic extract.

Radical Scavenger Capacity of Jabuticaba Fruit (Myrciaria cauliflora) and Its Biological Effects in Hypertensive Rats.

Jabuticaba is an exotic fruit native to Brazil that has been arousing medicinal interest. Using chemical (HPLC-PDA, resonance mass spectra, and NMR), electroanalytical (differential pulse voltammetry, radical scavenging assay), and pharmacological (in vivo and in vitro) approaches, we have identified its bioactive compounds and hypotensive effects on hypertensive rats. The hydroalcoholic extract of jabuticaba (HEJ) presents a great quantity of phenolic compounds, and several molecules with hydroxyl groups present high efficiency as an antioxidant. The treatment with HEJ (100 and 300 mg/kg/day, for four weeks) presented hypotensive effects on L-NAME-induced hypertensive rats, possibly improving the nitric oxide bioavailability because of its high antioxidant potential. Furthermore, renal and cardiac hypertrophies were also attenuated after the HEJ treatment. Moreover, the vascular responses to contractile and dilating agonists were improved with the HEJ treatment, which is also able to induce nitric oxide production in endothelial cells.

Essential Oil Composition, Antimicrobial and Pharmacological Activities of Lippia sidoides Cham. (Verbenaceae) From São Gonçalo do Abaeté, Minas Gerais, Brazil.

BACKGROUND: Lippia sidoides (Verbenaceae) is used in Brazilian folk medicine as an antiseptic, and it is usually applied topically on skin, mucous membranes, mouth, and throat, or used for vaginal washings. OBJECTIVES: To analyze the chemical composition of the essential oil from L. sidoides collected in São Gonçalo do Abaeté, Minas Gerais and grown in Hidrolândia, Goiás; to evaluate the antimicrobial activity of the essential oil, crude ethanol extract, and hexane, dichloromethane, ethyl-acetate, and aqueous fractions (AFs); to study the antinociceptive, anti-inflammatory, and central nervous system activities of the crude ethanol extract. MATERIALS AND METHODS: The essential oils were obtained by hydro-distillation using a Clevenger-type apparatus and analyzed by GC/MS. The antimicrobial activity in vitro was performed by broth microdilution method. The pharmacological tests were performed using female Swiss albino mice. RESULTS: The major components of the essential oil were isoborneol (14.66%), bornyl acetate (11.86%), α-humulene (11.23%), α-fenchene (9.32%), and 1.8-cineole (7.05%), supporting the existence of two chemotypes of this species. The hexane fraction (HF) had good antifungal activity against Cryptococcus sp. ATCC D (MIC = 31.25 µg/mL) and Cryptococcus gatti L48 (MIC = 62.5 µg/mL). In the pharmacological tests, the crude ethanol extract presented antinociceptive and anti-inflammatory activities. CONCLUSION: Given that the ethanol extract of L. sidoides is included in the Formulary of Phytotherapeutic Agents of the Brazilian Pharmacopeia as an anti-inflammatory for oral cavities, the present work provides scientific evidence to back this use and highlight the importance of selecting the appropriate chemotype on the basis of the expected biological response. SUMMARY: The major components of the essential oil of L. sidoides were isoborneol bornyl acetate, α-humulene, α-fenchene, and 1.8-cineole. The HF had good antifungal activity against Cryptococcus sp. ATCC D and C. gatti L4.The crude ethanol extract of L. sidoides presented antinociceptive and anti-inflammatory activities.The present work provides scientific evidence of the importance of selecting the appropriate chemotype on the basis of the expected biological response. Abbreviations used: UFG: Universidade Federal de Goiás; HF: hexane fraction; DF: dichloromethane fraction; EAF: ethyl acetate fraction; AF: aqueous fraction; MeOH: methanol; MIC: minimum inhibitory concentration; ATCC: American Type Culture Collection; MH: Müller Hinton; DMSO: dimethyl sulfoxide; RPMI: Roswell Park Memorial Institute; NaCl: sodium chloride; µL: microliters; mL: milliliters; µg: microgram; kg: kilogram; h: hour; min: minute; cm: centimeter; COBEA: Brazilian College of Animal Experiments; p.o.:, oral; i.p.: intraperitoneal; s.c.: subcutaneous; SEM: standard error of the mean; RI: retention indices.

Optimization of Ultrasound-assisted Extraction of Phenolic Compounds from Myrcia amazonica DC. (Myrtaceae) Leaves.

BACKGROUND: Myrcia amazonica. DC is a species predominantly found in northern Brazil, and belongs to the Myrtaceae family, which possess various species used in folk medicine to treat gastrointestinal disorders, infectious diseases, and hemorrhagic conditions and are known for their essential oil contents. MATERIALS AND METHODS: This study aimed applied the Box-Behnken design combined with response surface methodology to optimize ultrasound-assisted extraction of total polyphenols, total tannins (TT), and total flavonoids (TF) from M. amazonica DC. RESULTS: The results indicated that the best conditions to obtain highest yields of TT were in lower levels of alcohol degree (65%), time (15 min), and also solid: Liquid ratio (solid to liquid ratio; 20 mg: 5 mL). The TF could be extracted with high amounts with higher extraction times (45 min), lower values of solid: Liquid ratio (20 mg: mL), and intermediate alcohol degree level. CONCLUSION: The exploitation of the natural plant resources present very important impact for the economic development, and also the valorization of great Brazilian biodiversity. The knowledge obtained from this work should be useful to further exploit and apply this raw material. SUMMARY: Myrcia amazonica leaves possess phenolic compounds with biological applications;Lower levels of ethanolic strength are more suitable to obtain a igher levels of phenolic compouds such as tannins;Box-Behnken design indicates to be useful to explore the best conditions of ultrasound assisted extraction. Abbreviation used: Nomenclature ES: Ethanolic strength, ET: Extraction time, SLR: Solid to liquid ratio, TFc: Total flavonoid contents, TPc: Total polyphenol contents, TTc: Total tannin contents.

Ultrasound-assisted extraction of azadirachtin from dried entire fruits of Azadirachta indica A. Juss. (Meliaceae) and its determination by a validated HPLC-PDA method.

Azadirachta indica A. Juss., also known as neem, is a Meliaceae family tree from India. It is globally known for the insecticidal properties of its limonoid tetranortriterpenoid derivatives, such as azadirachtin. This work aimed to optimize the azadirachtin ultrasound-assisted extraction (UAE) and validate the HPLC-PDA analytical method for the measurement of this marker in neem dried fruit extracts. Box-Behnken design and response surface methodology (RSM) were used to investigate the effect of process variables on the UAE. Three independent variables, including ethanol concentration (%, w/w), temperature (°C), and material-to-solvent ratio (gmL(-1)), were studied. The azadirachtin content (µgmL(-1)), i.e., dependent variable, was quantified by the HPLC-PDA analytical method. Isocratic reversed-phase chromatography was performed using acetonitrile/water (40:60), a flow of 1.0mLmin(-1), detection at 214nm, and C18 column (250×4.6mm(2), 5µm). The primary validation parameters were determined according to ICH guidelines and Brazilian legislation. The results demonstrated that the optimal UAE condition was obtained with ethanol concentration range of 75-80% (w/w), temperature of 30°C, and material-to-solvent ratio of 0.55gmL(-1). The HPLC-PDA analytical method proved to be simple, selective, linear, precise, accurate and robust. The experimental values of azadirachtin content under optimal UAE conditions were in good agreement with the RSM predicted values and were superior to the azadirachtin content of percolated extract. Such findings suggest that UAE is a more efficient extractive process in addition to being simple, fast, and inexpensive.

Bioactive Compounds Found in Brazilian Cerrado Fruits.

Functional foods include any natural product that presents health-promoting effects, thereby reducing the risk of chronic diseases. Cerrado fruits are considered a source of bioactive substances, mainly phenolic compounds, making them important functional foods. Despite this, the losses of natural vegetation in the Cerrado are progressive. Hence, the knowledge propagation about the importance of the species found in Cerrado could contribute to the preservation of this biome. This review provides information about Cerrado fruits and highlights the structures and pharmacologic potential of functional compounds found in these fruits. Compounds detected in Caryocar brasiliense Camb. (pequi), Dipteryx alata Vog. (baru), Eugenia dysenterica DC. (cagaita), Eugenia uniflora L. (pitanga), Genipa americana L. (jenipapo), Hancornia speciosa Gomes (mangaba), Mauritia flexuosa L.f. (buriti), Myrciaria cauliflora (DC) Berg (jabuticaba), Psidium guajava L. (goiaba), Psidium spp. (araçá), Solanum lycocarpum St. Hill (lobeira), Spondias mombin L. (cajá), Annona crassiflora Mart. (araticum), among others are reported here.

Evaluation of extraction method on the chemical composition in Apeiba tibourbou Aubl's extracts.

BACKGROUND: The extraction method of bioactive compounds is an important step in the manufacturing of herbal medicines, because secondary metabolites with therapeutic potential are usually found in small quantities in plant materials. OBJECTIVE: Due the potential of Apeiba tibourbou Aubl, this study aimed to evaluate the impact of the extraction method on the quality of herbal extract and optimize the extraction of fatty acid, rosmarinic (Ra) and caffeic (Ca) acid from A. tibourbou. MATERIALS AND METHODS: Determinations of residual moisture (Rm), proteins (Pt), lipids (Lp), total fiber (Tf), and carbohydrate (Cy) were performed in triplicate samples according assessment of antioxidant capacity. Extraction of fatty acids was carried out by two different methods: (i) By shoxlet and (ii) bligh and dyer. The optimized conditions were determined by surface response methodology (RSM), and the criterion of desirability was the maximum extraction of Ra and Ca. RESULTS: The method of bligh and dyer was able to extraction more total Lp than the shoxlet. However, the extraction of fatty acid was different for the two methods. The optimized conditions to extract RA and Ca was calculated by RSM, 42°C, 30% (alcohol degree) and 24 min, this conditions maximize simultaneously the extraction of Ca (0, 04%) and Ry (1.89). CONCLUSION: It was observed that the extraction method alters the chemical composition of extract, and it is possible to extract Ca and Ra from A. tibourbou's leaves using ultrasound-assisted extraction.

Technical aspects on production of fluid extract from Brosimum gaudichaudii Trécul roots.

INSTRUCTION: Despite the increased use of Brosimum gaudichaudii roots as raw material on medicine to treatment of vitiligo, there are not studies that showing the impact of unit operations on the quality and standardized of the extract of B. gaudichaudii. The quality of the herbal extract is essential to ensure the safety and efficacy of pharmaceutical product. Due the medical and commercial importance, this study aimed to evaluate the impact of the extraction method (ultrasound or percolation) on the quality of herbal extract and optimize the extraction of psoralen and 8-methoxypsoralen (8-MOP) from B. gaudichaudii. MATERIALS AND METHODS: The extraction recovery was evaluate by high-performance liquid chromatography (C8 reverse phase column and acetonitrile: Water 45:55 and flow rate 0.6 mL/min). The extraction was performed by ultrasound-assisted extraction (UEA) or percolation using a Box-Behnken design. RESULTS: From both chemical markers (psoralen and bergapten), the optimal conditions for the UEA were an extraction time of 25 min, the mean particle size of 100 µm, and an ethanol: Water ratio of 55:45 (v/v). CONCLUSION: The extraction by percolation revealed that ethanol 55% was more efficient than ethanol 80% to extract psoralen and bergapten.

Obtainment of pellets using the standardized liquid extract of Brosimum gaudichaudii Trécul (Moraceae).

BACKGROUND: The standardized liquid extract of Brosimum gaudichaudii Trécul is an alternative for the treatment of vitiligo. There is a shortage of solid oral dosage forms developed from standardized extracts of this plant specie. OBJECTIVE: This study is aimed to obtain pellets with a standardized liquid extract of B. gaudichaudii. RESULTS: The standardized liquid extract of B. gaudichaudii was obtained through maceration and percolation with a 55% ethanol-water solution (v/v). Pellets were obtained through a mixture of extract of 500 g of B. gaudichaudii standardized extract, 500 g of microcrystalline cellulose PH101 and 10 g of hydroxypropyl methylcellulose K100. The pellets obtained presented a homogeneity yield of 92%, aspect ratio of 1.16 ± 0.65, shape fator e R of 0.35 ± 0.09 and Feret diammeter of 0.87 ± 0.27. These pellets were coated with a suspension composed of titanium dioxide, aluminum red lacquer, ethyl cellulose, talc and magnesium stearate. Before the photostability test, the uncoated pellets showed psoralen content equal to 0.13 ± 0.01% and to the 5-MOP was 1.40 ± 0.27%. After exposure to one level (3 J.cm(-2)) of UVB irradiation the uncoated pellets presented a degradation of 2.16% of psoralen and 8.1% of 5-MOP. After exposure to three levels (10, 20 and 30 J.cm(-2)) of UVA irradiation the uncoated pellets exhibited photodegradation of 9.78, 17.64, 24.21% of psoralen and 18.95, 23.68, 28.48% for 5-MOP. The coated pellets where unaffected after photostability test. CONCLUSION: Pellets were obtained with the standardized liquid extract of B. gaudichaudii and coating is a technological alternative to ensure the stability of the formula.

The effects of extraction method on recovery rutin from Calendula officinalis L. (Asteraceae).

BACKGROUND: Calendula officinalis L. (Asteraceae) is a Mediterranean specie, but in Europe and America it is cultivated for ornamental or medicinal purposes. This species is widely used for presenting activities, antiinflammatory antibacterial and antioxidant. However the therapeutic action is linked to the amount of assets of the extracted raw material. The extraction method of bioactive compounds is an important step in the manufacturing of herbal medicines, because secondary metabolites with therapeutic potential are usually found in small quantities in plant materials. OBJECTIVE: Due the medical and commercial importance of C. officinalis, this study aimed to evaluate the impact of the extraction method on the quality of herbal extract and optimize the extraction of rutin from C. officinalis. MATERIALS AND METHODS: The extraction of rutin was performed by ultrasound and shaker and the optimized conditions were determined by response surface methodology. RESULTS: The results of ultrasound extraction assisted (UEA) and maceration dynamic (MD) showed that rutin yield ranged from 0.218 to 2.28% (w/w) when extract by ultrasound and 0.1-1.44% by MD. The optimal extraction condition for rutin (2.48% to UEA or 1.46% to MD) from C. officinalis by UEA or MD were a 19-22 min extraction, ethanol: water ratio of 35-40% and 0.05-0.056 mg/mL to raw material: solvent ratio. CONCLUSION: The UEA is more efficient to extraction rutin.

Chemical Constituents of Essential Oil from Lippia sidoides Cham. (Verbenaceae) Leaves Cultivated in Hidrolândia, Goiás, Brazil.

Several studies involving the family Verbenaceae, occurring in the Brazilian Cerrado, have emphasized the popular use of many aromatic species. We highlight the use of Lippia sidoides Cham., known as "alecrim pimenta," native to northeastern Brazil and northern Minas Gerais. Leaves of this species were collected in antropized Brazilian Cerrado area, in Hidrolândia, Goiás, and their essential oils were extracted by hydrodistillation in a Clevenger-type apparatus and thereafter analyzed GC/MS. Among the compounds identified in this study were the most abundant oxygenated monoterpenes, followed by sesquiterpenes hydrocarbons. The oxygenated monoterpene 1,8-cineole was the major constituent followed by isoborneol and bornyl acetate. The chemical composition of essential oil described in this paper differs from that described in the literature for L. sidoides found in its native environment, where the major constituents are thymol and carvacrol.

Psoralen and bergapten: in silico metabolism and toxicophoric analysis of drugs used to treat vitiligo.

PURPOSE: To discuss the contribution of psoralen and bergapten metabolites on psoralens toxicity. METHODS: Computational chemistry prediction of metabolic reactions and toxicophoric groups based on the expert systems Derek and Meteor. RESULTS: a total of 15 metabolites were suggested for both psoralen and bergapten based on phase 1 and 2 biotransformations until the 3rd generation. Five toxicophoric substructures were shared among psoralen, bergapten and their corresponding metabolites; one toxicophoric marker (resorcinol) was only identified in bergapten and its biotransformation products. CONCLUSION: Although the toxic effects of psoralens are well known and documented, there is little information concerning the role of their metabolites in this process. We believe this work add to the knowledge of which molecular substructures are relevant to the process of metabolism and toxicity induction, thus guiding the search and development of more effective and less toxic drugs to treat vitiligo.