Xanthan-carrageenan film containing sesame seed oil: A nanocomposite pharmaceutical platform for trichomoniasis treatment.

Trichomoniasis is a common sexually transmitted infection that poses significant complications for women. Challenges in treatment include adverse effects and resistance to standard antimicrobial agents. Given this context, a sesame seed oil nanoemulsion (SONE) was developed and showed anti-Trichomonas vaginalis activity. To facilitate the local application of SONE, a polysaccharide film was developed using xanthan gum (XG) and κ-carrageenan gum (CG). A blend of XG and CG (at 2 %, ratio 1:3) plasticized with glycerol produced a more promising film (XCF) than using the gums individually. The film containing SONE (SONE-XCF) was successfully obtained by replacing the aqueous solvent with SONE via solvent evaporation technique. The hydrophilic SONE-XCF exhibited homogeneity and suitable mechanical properties for vaginal application. Furthermore, SONE-XCF demonstrated mucoadhesive properties and high absorption capacity for excessive vaginal fluids produced in vaginitis. It also had a disintegration time of over 8 h, indicating long retention at the intended site of action. Hemolysis and chorioallantoic membrane tests confirmed the safety of the film. Therefore, SONE-XCF is a biocompatible film with a natural composition and inherent activity against T. vaginalis, possessing exceptional characteristics that make it appropriate for vaginal application, offering an interesting alternative for trichomoniasis treatment.

Development by design of experiment and validation of a HPLC-UV method for simultaneous quantification of 1-nitro-2-phenylethane and methyleugenol: Application to nail permeation/retention studies.

Aniba canelilla (Kunth) Mez is an aromatic tree from Amazon region whose essential oil presents 1-nitro-2-phenylethane (NP) and methyleugenol (ME) as major compounds. Several properties are attributed to Aniba canelilla essential oil (ACEO), such as antifungal. Onychomycoses are fungal nail infections that require novel therapeutic alternatives, especially topical ones. However, to ensure the success of topical therapy, the active compound should be able to penetrate/permeate the nail plate, which is challenging due to the highly keratinized composition of this structure. Thus, the aims of this article were to develop, validate and apply a high-performance liquid chromatography method (HPLC-UV) to quantify NP and ME in porcine hoof extract (PHE) and receptor fluid (RF) during in vitro permeation/retention studies in nail model, for which porcine hoof membranes were used. For method development, two Designs of Experiment (DoE) were adopted: 23 Full Factorial and Box-Behnken. Retention times of 5.65 and 7.49 min were achieved for NP and ME, respectively. The method was full validated for NP and ME quantification in receptor fluid, in accordance with the recommended parameters by ICH Q2(R1) Guideline. In addition, the method was full validated for NP and ME quantification in porcine hoof extract, considering the parameters and criteria of ICH M10 Guideline. In vitro permeation/retention studies were carried out in nail model, and promising results were obtained. NP reached the receptor fluid in the order of 441.1 ± 92.1 µg/cm2 at 72 h. The amount of NP and ME retained into porcine hoof membrane was 1272.6 ± 225.7 µg/cm2 and 84.7 ± 20.4 µg/cm2, respectively, at 72 h. Our findings open perspective to develop topical formulations containing ACEO as active compound aiming the management of onychomycosis.

Uncovering cloves: characterization of volatile compounds present in clove cigarettes.

Indonesian clove cigarettes-called "kretek" due to the crackling sound that can be heard when the product burns-are tobacco products containing clove and the "saus", a mixture of essential oils and plant extracts whose ingredients are mostly kept in secret. It is important to determine which ingredients those are to properly assess the effects that clove cigarettes can cause. An organoleptic, qualitative and quantitative analysis was made in 9 different brands of clove cigarettes obtained in Brazil. Nicotine, eugenol, menthol, and ß-caryophyllene were quantified through gas chromatography coupled to mass spectrometry. The samples presented 20 different compounds, and all samples had a different combination of the compounds. Nicotine concentrations were generally higher than eugenol, and lower than nicotine concentration in a conventional cigarette. One sample had menthol even though the cigarette pack did not inform that it was a menthol product. There were traces of 2 unusual substances. Clindamycin is an antibiotic that can be used to treat bacterial infections in respiratory airways, and octodrine is an amphetaminic stimulant used in nutritional supplements, considered as a substance of doping by the World Anti-Doping Association. The presence of both substances was not tested using certified reference materials, but its possible presence raises concern about the compounds in kretek cigarettes. There should be more studies about the contents of clove cigarettes, to improve antitobacco legislations and regulations. This way it would be possible to properly inform the risks of smoking clove cigarettes and to diminish the number of tobacco users throughout the world.

Where should I start? A scoping review about the publications on clove cigarettes.

INTRODUCTION: The general lack of knowledge about the composition of clove cigarettes and the large number of terms that can be used to define different types of cigarettes that contain cloves makes it difficult to find scientific articles focused on the subject. We reviewed the publications that cited clove cigarettes to assess their relevance. METHODS: We searched publications on Scopus, ScienceDirect, PubMed, and Portal CAPES during the first semester of 2021, without date restrictions. Through a quality assessment, the studies found were assorted in ten different categories. RESULTS: Indonesian clove cigarettes-also known as kretek-are a mixture of tobacco and cloves rolled in a cigarette and sprayed with oils, plant extract, and food flavorings, in an unknown quantity and composition, different from each brand, which is usually kept in secret. Due to the relatively low prevalence of use in the general population, most publications on tobacco products tend to ignore clove cigarettes or place them in an existing category. Clove cigarettes can be hand-rolled, machine-made, filtered, unfiltered, and each form can be named differently. The interchangeable use of each term, sometimes grouping conventional cigarettes in the mix, can lead the researcher to consider a publication that should be excluded. CONCLUSION: The existing regulations on flavored cigarettes, although well-intentioned, are still somewhat vague and broad, leaving possible loopholes that can be exploited by the tobacco industries. Fully understanding the precise effects caused by clove cigarettes can be an important tool in future discussions about tobacco control.

Two morphotypes versus two chemotypes of Psidium cattleyanum: Chemical and pharmacological comparison and a rational approach for marker selection.

Psidium cattleyanum has two morphotypes: one with yellow fruits and other with red fruits. The leaves are popularly used as anti-inflammatory. However, no distinction is made between the types. Therefore, this study compared chemical and pharmacological data of both morphotypes to select proper biomarkers to ensure P. cattleyanum leaves quality. After extraction optimization by experimental design, 28 samples were analyzed by HPLC. Using Principal Component Analysis, it was possible to detect two chemotypes, unrelated to the color of the fruits. However, the extracts obtained from both chemotypes seemed to play similar anti-inflammatory effect, demonstrated by anti-chemotactic activity. The compounds common to both chemotypes were isolated and identified as hyperoside, miquelianin and quercitrin; these compounds also demonstrated anti-inflammatory potential. Since both chemotypes played similar activity, along with the isolated flavonoids, these flavonoids were selected as biomarkers for quality control of P. cattleyanum leaves. Following ICH guidelines, a HPLC method was validated. In summary, this study demonstrated that hyperoside, miquelianin and quercitrin can be used as biomarkers for quality control of P. cattleyanum leaves and a method was developed and validated to be used interchangeably for both morpho- and chemotypes.

Leishmanicidal and antichemotactic activities of icetexanes from Salvia uliginosa Benth.

BACKGROUND: Several species of Salvia are used as medicinal plants around the world. Biological activities of isolated compounds have been described, being diterpenes frequently responsible for the effects. PURPOSE: Isolation of diterpenes from Salvia uliginosa Benth. and evaluation of the antichemotactic and leishmanicidal activities of the isolated compounds. STUDY DESIGN: To isolate diterpenes from S. uliginosa and evaluate their antichemotactic and leishmanicidal activities in vitro. METHODS: The exudate of S. uliginosa was obtained by rapidly dipping the aerial parts in dichloromethane. The compounds were isolated by repeated column chromatography over silica gel. The effects on L. amazonensis growth, survival, DNA degradation, ROS generation, as well as the antichemotactic activity and cytotoxicity of the compounds towards human erythrocytes and macrophages were evaluated. RESULTS: A novel icetexane diterpene, isoicetexone (IsoICT) along with the known diterpenes icetexone (ICT), and 7-acetoxy-6,7-dihydroicetexone were isolated from the dichloromethane surface exudate of S. uliginosa. The structures were elucidated using NMR and MS experiments, and by comparison with previously reported data. IsoICT and ICT at low concentrations caused completely inhibition of neutrophils migration in vitro. In addition, IsoICT and ICT showed high leishmanicidal activity against L. amazonensis, induced ROS production in parasites and presented low cytotoxicity against macrophages and human erythrocytes, and moderate to high selectivity index. CONCLUSION: These data indicated that IsoICT and ICT exhibit potent antichemotactic and leishmanicidal effects. Further studies are needed in order to evaluate the in vivo activities as well as the toxicity of the compounds.

Development of analytical method for the quality control of the fruit bark of Punica granatum L. (pomegranate) and antichemotatic activity of extract and rich fraction in punicalagins.

Pomegranate is of current interest owing to the existing potential for industrial uses of fruit peels. This includes its availability as a raw vegetable material, a byproduct that constitutes residue in the use of the species and is recognized as a functional product, and beneficial health properties, as will be demonstrated in the studies cited. Therefore, it is necessary to ensure its effectiveness and safety. Toward this end, the aim of this study was to develop and validate an analytical method for the separation and quantification of total punicalagin present in the bark of the fruit of Punica granatum by HPLC. Purity tests such as water determination and total ashes were also performed. The ability of the extract and enriched fraction of punicalagin to inhibit leukocyte migration in vitro was determined by the Boyden's chamber method. The developed HPLC method demonstrated good separation and quantification of the punicalagin α and ß anomers. The method is efficient and reliable, and can ultimately be used for the analysis of the extract of pomegranate. The crude extract and the fraction of punicalagins significantly inhibited leukocyte migration at concentrations of 1 and 10 µg/mL in relation to the negative control, indicating potential antichemotactic action.

Alkaloid profiling and anticholinesterase activity of South American Lycopodiaceae species.

The alkaloid extracts of four Huperzia and one Lycopodiella species, from Brazilian habitats, were tested for their in vitro anticholinesterase activities. IC(50) values showed a potent acetylcholinesterase inhibition for H. reflexa (0.11 ± 0.05 µg/mL), followed by H. quadrifariata (2.0 ± 0.3 µg/mL), H. acerosa (5.5 ± 0.9 µg/mL), H. heterocarpon (25.6 ± 2.7 µg/mL) and L. cernua (42.6 ± 1.5 µg/mL). A lower inhibition of butyrylcholinesterase was observed for all species with the exception of H. heterocarpon (8.3 ± 0.9 µg/mL), whose alkaloid extract presented a selectivity for pseudocholinesterase. Moreover, the chemical study of the bioactive extracts performed by GC-MS, revealed the presence of a number of Lycopodium alkaloids belonging to the lycopodane, flabellidane and cernuane groups. Surprisingly, the potent acetylcholinesterase inhibitors huperzines A and B were not detected in the extracts, suggesting that other alkaloids may be responsible for such an effect.

Assay of caffeoylquinic acids in Baccharis trimera by reversed-phase liquid chromatography.

Baccharis trimera commonly named 'carqueja', is wide-spread in South America and are used as raw material for herbal medicines. A reversed-phase liquid chromatography (RP-LC) method coupled to diode array detector was developed for the analysis of caffeoylquinic acids (CQAs), the main compounds responsible for its digestive activity. The identity of the quinic acids was established by mass spectrometry and were them: 5-O-[E]-caffeoylquinic acid, 3,4-O-[E]-dicaffeoylquinic acid, 3,5-O-[E]-dicaffeoylquinic acid, 4,5-O-[E]-dicaffeoylquinic acid and a tricaffeoylquinic acid. The RP-LC method for the quantitation of the caffeoylquinic acids was validated according to ICH guidelines, based on the following parameters: linearity, selectivity, robustness, limits of detection and quantification, precision and recovery. Hydroalcoholic extracts were prepared by the maceration of the plant material with ethanol:water 1:1 (v/v) in a 0.1:25 g mL(-1) plant:solvent ratio in a water bath at 40°C. Validation data indicated that the HPLC method proposed is suitable for the analysis of caffeoylquinic acids in B. trimera raw material. The results of the LOD and LOQ analyses for the 5-CQA were 4.1 µg mL(-1) and 12.5 µg mL(-1), respectively, 1.3 µg mL(-1), 3.9 µg mL(-1) for 4,5-diCQA and 1.7 µg mL(-1), 5.1 µg mL(-1) for triCQA. The levels of total CQAs ranged from 2.1 to 4.0 g% (w/w). The influence of season harvest and site collection was also evaluated and variations were observed in the results and can be related to phonologic phase, different locations, seasons and soil. Long term and photostability of plant material were carried out and was observed a stable behavior during the time of the experiments.

Pharmacological evaluation of Copaifera multijuga oil in rats.

CONTEXT: Copaiba oil is an oleoresin made up of resin acids and volatile compounds, and it is obtained by tapping the trunks of trees that are members of the Copaifera L. (Leguminoseae) genus and are found in tropical parts of Latin America. OBJECTIVE: This study analyzed the chemical composition of Copaifera multijuga Hayne oil and conducted preclinical trials to investigate anti-inflammatory effects and any action it may have on the central nervous system (CNS) of rats. MATERIALS AND METHODS: The chemical analysis was carried out using gas chromatography with mass spectroscopy. Anti-inflammatory activity was measured by leucocytes mobilization, by chemotaxis assay in Boyden's chamber, and by pleurisy model in rats. CNS effect was determined by plus maze and open-field assays. The statistical test applied was analysis of variance (ANOVA) followed by Tukey's test or ANOVA followed by Duncan's test. RESULTS: The oil was composed of sesquiterpenes with the predominance of ß-caryophyllene (36.0%), followed by α-copaene (18.8%), ß-bisabolene (8.5%), and α-trans-bergamotene (7.0%). Data demonstrated that at 100 and 200 mg/kg doses and at a concentration of 200 µl/ml copaiba essential oil presented anti-inflammatory effects both in vivo and in vitro based on reduced leukocyte migration to the rats' pleural cavity and to the chemotactic agent lipopolysaccharide solution, respectively. During the experiments investigating CNS effects, locomotive and exploratory activities were reduced and the animals' anxiety increased at 100 and 200 mg/kg. CONCLUSION: The results obtained suggest that copaiba oil has an interesting anti-inflammatory effect and important effect on the CNS.

Comparative analysis of the chemical composition and antioxidant activity of red (Psidium cattleianum) and yellow (Psidium cattleianum var. lucidum) strawberry guava fruit.

UNLABELLED: Strawberry guava (Psidium cattleianum Sabine) is a native fruit of Brazil widely consumed fresh and used in the food industry. In this context, the present study deals with the chemical characterization and the antioxidant activity of the red (Psidium cattleianum) and yellow (P. cattleianum var. lucidum Hort.) strawberry guava fruits, cultivars Irapuã and Ya-Cy, respectively. Knowledge of chemical composition is fundamental to human nutrition, contributing to the quality of foods. Phenolic compounds in both fruits were analyzed by HPLC-DAD and the total flavonoid content was determined by the Folin-Ciocalteu assay. The antioxidant activity was evaluated by the total reactive antioxidant (TRAP) method. Psidium cattleianum presented a higher content of polyphenolic compounds than P. cattleianum var. lucidum (501.33 and 292.03 mg/100 g, respectively), with hyperoside being one of the major flavonoids identified for both cultivars. In addition to flavonoids, P. cattleianum presented an anthocyanin, identified as cyanidin. The antioxidant activity varied in a concentration-dependent manner for both strawberry guava species. The volatile oils in fruits and fatty acids in seeds were quantified by GC-EM. The analysis of the essential oil of yellow strawberry guava was compared with a previous study on the red cultivar, revealing ß-caryophyllene as the main component in both oils. The fatty acid composition was also quite similar and was especially characterized by the presence of unsaturated fatty acids (86.25% and 76%, respectively), among which linoleic acid as the most abundant. PRACTICAL APPLICATION: In this study, the chemical characterization and the antioxidant activity of the red (Psidium cattleianum) and yellow (P. cattleianum var. lucidum Hort.) strawberry guava fruits were investigated. This is important for potential application of strawberry guava as functional food. Moreover, it may be the experimental basis for further development and use in food industry.

Appraisal of the antichemotactic activity of flavonoids on polymorphonuclear neutrophils.

Flavonoids are polyphenols that are ubiquitous in plants and frequently consumed in the diet. They are suggested to have many beneficial actions on human health, including anti-inflammatory activity. Their properties have been studied in a number of cell types, but little is known about their effects on neutrophil biology. Consequently, we selected 25 flavonoids with different structural features to evaluate their in vitro inhibition of rat polymorphonuclear neutrophil (PMN) chemotaxis, employing a modified Boyden chamber. Migratory activity was measured towards a chemotactic stimulant, formyl-Met-Leu-Phe or lipopolysaccharide. Furthermore, the cytotoxic effect of flavonoids on PMNs was determined by the release of cytosolic lactate dehydrogenase (LDH). Ten flavonoids significantly retarded the migration of PMNs with at least one of the concentrations tested in a range between 0.625 and 100 µM; the best antichemotactic agents were flavone, flavonol, quercetin and rutin. None of the flavanones evaluated presented any significant inhibition of migration in this assay. Our findings indicated that non-hydroxylated flavones possess a better antichemotactic activity when compared to flavones with hydroxy groups. The presence of a sugar moiety in rutin did not produce any increase in this effect, when compared to the respective aglycone analogue. Finally, none of the flavonoids exhibited cell toxicity and for many of these flavonoids this is the first report of the inhibition of PMN chemotaxis.