Biological properties of Schinus terebinthifolia Raddi essential oil

Abstract Schinus terebinthifolia Raddi green fruits essential oil (EO) was evaluated regarding its phytochemical profile, antimicrobial and cytotoxic activities, and toxicity. Gas chromatography with mass spectrometry was applied to identify its constituents, thereafter the minimum inhibitory concentration, minimum bactericidal and fungicidal concentrations, and its antibiofilm activity were evaluated. The EO cytotoxicity was assessed in tumor and non-tumor human cells, and in vivo toxicity was evaluated in a Galleria mellonella model. The major constituents of S. terebinthifolia EO were alpha-phellandrene and beta-phellandrene. The EO had a weak activity against all strains of Candida albicans (MIC 1000µg/mL) and had no activity against non-albicans strains, bacteria, and C. albicans biofilm. Cytostatic activity against all tumor cell lines was shown. Additionally, cell viability remained at EO concentrations up to 62.5 µg/mL. At 16 mg/mL, 50% hemolysis was observed, and it had low toxicity in vivo. Overall, the S. terebinthifolia EO was characterized by low antimicrobial and antibiofilm activities, with no evidence of toxicity to human tumor and non-tumor cells

Match of Solubility Parameters Between Oil and Surfactants as a Rational Approach for the Formulation of Microemulsion with a High Dispersed Volume of Copaiba Oil and Low Surfactant Content.

PURPOSE: Aim was to formulate oil-in-water (O/W) microemulsion with a high volume ratio of complex natural oil, i.e. copaiba oil and low surfactant content. The strategy of formulation was based on (i) the selection of surfactants based on predictive calculations of chemical compatibility between their hydrophobic moiety and oil components and (ii) matching the HLB of the surfactants with the required HLB of the oil. METHOD: Solubility parameters of the hydrophobic moiety of the surfactants and of the main components found in the oil were calculated and compared. In turn, required HLB of oils were calculated. Selection of surfactants was achieved matching their solubility parameters with those of oil components. Blends of surfactants were prepared with HLB matching the required HLB of the oils. Oil:water mixtures (15:85 and 25:75) were the titrated with surfactant blends until a microemulsion was formed. RESULTS: Two surfactant blends were identified from the predictive calculation approach. Microemulsions containing up to 19.6% and 13.7% of selected surfactant blends were obtained. CONCLUSION: O/W microemulsions with a high volume fraction of complex natural oil and a reasonable surfactant concentration were formulated. These microemulsions can be proposed as delivery systems for the oral administration of poorly soluble drugs.

Anthelmintic activity in vitro and in vivo of Baccharis trimera (Less) DC against immature and adult worms of Schistosoma mansoni.

Although its efficiency against all Schistosoma species, praziquantel (PZQ) shows low efficacy against schistosomula and juvenile stages. The potential for development of resistance to PZQ has justified the search for new alternative chemotherapies. In this scenario, studies to new formulations, more comprehensive and without adverse effects, are being conducted. One viable and promising treatment is the study of medicinal plants as a new approach to the experimental treatment for Schistosomiasis. Amongst all the variety of the medicinal species studied, we can highlight Baccharis trimera (Less) DC, known as "Carqueja-amarga". This paper not only describes the effect of crude dichloromethane extract (DE) and aqueous fraction (AF) obtained from B. trimera, in vitro but also is the first one that investigates the in vivo efficacy of B. trimera against schistosomula, juvenile and adult worms of Schistosoma mansoni BH strain. In the experiment, mice were treated with DE, AF and PZQ (40 and 200mg/kg) over the period of larval development (3 and 30 post-infection; pi), and adult worms (60days post-infection; pi). The in vitro results show that the DE and AF effects are dose-dependents, being the 130µg/mL the most effective one in a shorter period of incubation. The exposure of the in vitro samples over adult parasites were able to inhibit 100% of the oviposition in females. Likewise caused the mortality of the parasites with morphological alterations on the tegument, on the suckers, oral and acetabulum, in both males and females after 6-72h of exposure. Additionally, the in vivo treatments against juvenile and adult infection were more effective compared to the control group untreated. Administrations of AF and DE in day 30pi (juvenile worms) show female worm total burden reductions of 75% and 68% respectively. At the same period of infection reductions of respectively 98% and 97% egg/g in the faeces were seen. In relation to the different egg developmental stages (oogram), the results showed significant reductions, due to the reduction in the number of worms, especially the females. In conclusion, B. trimera exhibits major schistosomicidal effects in vivo against immature and adult worms of S. mansoni, opening up perspectives for future researches on substance or compound isolation and the elucidation of its mechanisms of action.

Development of an analytical method for the quantification of pfaffic acid in Brazilian ginseng (Hebanthe eriantha).

Hebanthe eriantha (Poir.) Pedersen (Amaranthaceae), which is known as Brazilian ginseng is widely used in folk medicine as an aphrodisiac and antidiabetic tonic. The anti-tumor activity, attributed to the pfaffic acid present in roots of H. eriantha, is responsible for the great interest in the commercialization of this species. In Brazil, the species H. eriantha is mainly used in commercial preparations, although other plants of the genus Pfaffia and Hebanthe have been marketed as Pfaffia paniculata or Brazilian ginseng. The pfaffic acid present in the roots is mainly conjugated with sugars (pfaffosides) and can be used as an active marker of H. eriantha, which helps to differentiate this species from others marketed as Brazilian ginseng. The main objective of this study was to develop and validate a liquid chromatographic method to quantify pfaffic acid in the roots of H. eriantha. The extraction and hydrolysis conditions were optimized using an univariate and experimental design, respectively, and the quantification of pfaffic acid by high performance liquid chromatography with diode-array detection (HPLC-DAD) was validated. This method was used to evaluate the pfaffic acid content in 30 different genotypes of the species from a germplasm collection. The content of pfaffic acid ranged from 0.97 to 4.29% (w/w) on a dry weight basis.

Tegumentary changes in two diferent strains of schistosoma mansoni treated with artemisinin and artesunic acid

Different strains of Schistosoma mansoni can respond differently to conventional and experimental treatments. Therefore, the responses to potential schistosomicidal drugs must be checked with different parasite strains. This work aimed to analyze changes caused by different concentrations of artemisinin or artesunic acid administered on different days in the teguments of adult S. mansoni belonging to two Brazilian strains (BH and SJ), using scanning electron microscopy (SEM). Infected mice were treated with 300 or 500 mg/kg of artemisinin and artesunic acid, 30 or 45 days post infection. Fifteen days after treatment, worms were examined by SEM. Altered teguments were observed in males and females on both days of treatment with both compounds, but the injury with artesunic acid was more intense. The treatment utilizing 500 mg/kg of artesunic acid against the BH strain 30 days after the infection proved to be particularly effective, resulting in erosion, peeling, sensory structure damage, and vesicle formation on the tegument of males and females. It is concluded that artemisinin and artesunic acid showed qualitatively similar tegumentary changes in both genders of the BH and SJ parasite strains. However, changes induced by artesunic acid were more severe for the BH strain, which demonstrates greater susceptibility of this strain to this experimental treatment...

Alterações tegumentares em duas diferentes linhagens de Schistosoma mansoni submetidas a tratamento com artemisinina e ácido artesúnicoDiferentes linhagens de Schistosoma mansoni podem responder de formas distintas a tratamentos experimentais. Portanto, ensaios com potenciais fármacos esquistossomicidas necessitam ser realizados com várias linhagens. Este trabalho visou analisar as alterações causadas por diferentes concentrações de artemisinina e ácido artesúnico, administradas em diferentes dias, sobre o tegumento de adultos de S. mansoni de duas linhagens brasileiras (BH e SJ), utilizando-se microscopia eletrônica de varredura (MEV). Os camundongos infectados foram tratados com 300 e 500 mg/kg de artemisinina ou ácido artesúnico, 30 ou 45 dias após a infecção. Após 15 dias do tratamento, os vermes foram analisados pela MEV. A destruição do tegumento foi observada em machos e fêmeas nos dois dias de tratamento com ambos os compostos, mas observou-se que o ácido artesúnico provocou uma destruição mais intensa. O tratamento realizado com 500 mg/g de ácido artesúnico contra parasitos da linhagem BH, 30 dias após a infecção, mostrou ser o mais efetivo, resultando em erosão, descamação, destruição das estruturas sensoriais e formação de vesículas nos machos e nas fêmeas. Ficou evidenciado que as linhagens BH e SJ apresentaram alterações tegumentares diferentes quanto à intensidade, com ambos os compostos. No entanto, a destruição do tegumento foi mais intensa na linhagem BH, especialmente com o ácido artesúnico, o que demonstrou maior suscetibilidade desta linhagem a esse tratamento experimental...

Schistosoma mansoni: in vitro schistosomicidal activity of essential oil of Baccharis trimera (less) DC.

Schistosomiasis is a chronic parasitic disease caused by the trematode species Schistosoma mansoni. Chemotherapy is the only immediate recourse to minimize the prevalence and incidence of this disease worldwide. At present, praziquantel (PZQ) is the drug of choice for the treatment of all forms of schistosomiasis. However, dependence on a single drug is concern because some strains can become resistant. In this context, medicinal plants become potential candidates as sources of new drug prototypes. This study provides findings on the schistosomicidal activity of the essential oil of Baccharis trimera in in vitro assays. During the assays parameters such as motility of adult worms, oviposition, morphological changes on the tegument and especially the mortality rate of adult worms of the BH strain were evaluated. The assays, which were carried out with four concentrations - 24, 48, 91 and 130 µg/mL - of the essential oil, have shown a promising activity regarding the parameters under study. It was possible to notice a significant decline in the motility of the worms and a mortality rate of 100% 30 h after they had been exposed to the essential oil in the concentration of 130 µg/mL. Male worms were more susceptible, producing a dose-response effect within a smaller exposition period than female worms. In what refers to morphological changes, the essential oil of B. trimera induced a peeling on the tegument surface, as well as the destruction of tubercles and spines, which resulted in smooth areas on the body surface. The essential oil also caused tegument destruction in female worms, in addition to destruction of the oral and acetabular suckers. It is the first time that the schistosomicidal activity has been reported for essential oil of B. trimera (less) DC.

Antimicrobial Activity of Essential Oils against Streptococcus mutans and their Antiproliferative Effects.

This study aimed to evaluate the activity of essential oils (EOs) against Streptococcus mutans biofilm by chemically characterizing their fractions responsible for biological and antiproliferative activity. Twenty EO were obtained by hydrodistillation and submitted to the antimicrobial assay (minimum inhibitory (MIC) and bactericidal (MBC) concentrations) against S. mutans UA159. Thin-layer chromatography and gas chromatography/mass spectrometry were used for phytochemical analyses. EOs were selected according to predetermined criteria and fractionated using dry column; the resulting fractions were assessed by MIC and MBC, selected as active fractions, and evaluated against S. mutans biofilm. Biofilms formed were examined using scanning electron microscopy. Selected EOs and their selected active fractions were evaluated for their antiproliferative activity against keratinocytes and seven human tumor cell lines. MIC and MBC values obtained for EO and their active fractions showed strong antimicrobial activity. Chemical analyses mainly showed the presence of terpenes. The selected active fractions inhibited S. mutans biofilm formation (P < 0.05) did not affect glycolytic pH drop and were inactive against keratinocytes, normal cell line. In conclusion, EO showed activity at low concentrations, and their selected active fractions were also effective against biofilm formed by S. mutans and human tumor cell lines.

Bioassay guided purification of the antimicrobial fraction of a Brazilian propolis from Bahia state.

BACKGROUND: Brazilian propolis type 6 (Atlantic forest, Bahia) is distinct from the other types of propolis especially due to absence of flavonoids and presence of other non-polar, long chain compounds, but presenting good in vitro and in vivo antimicrobial activity. Several authors have suggested that fatty acids found in this propolis might be responsible for its antimicrobial activity; however, so far no evidence concerning this finding has been reported in the literature. The goals of this study were to evaluate the antibacterial activity of the main pure fatty acids in the ethanolic extract and fractions and elucidate the chemical nature of the bioactive compounds isolated from Brazilian propolis type 6. METHODS: Brazilian propolis type 6 ethanolic extract (EEP), hexane fraction (H-Fr), major fatty acids, and isolated sub-fractions were analyzed using high performance liquid chromatography (HPLC), high resolution gas chromatography with flame ionization detection (HRGC-FID), and gas chromatography-mass spectrometry (GC-MS). Three sub-fractions of H-Fr were obtained through preparative HPLC. Antimicrobial activity of EEP, H-Fr, sub-fractions, and fatty acids were tested against Staphyloccus aureus ATCC 25923 and Streptococcus mutans Ingbritt 1600 using minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). RESULTS: EEP and H-Fr inhibited the growth of the microorganisms tested; nevertheless, no antimicrobial activity was found for the major fatty acids. The three sub-fractions (1, 2, and 3) were isolated from H-Fr by preparative HPLC and only sub-fraction 1 showed antimicrobial activity. CONCLUSION: a) The major fatty acids tested were not responsible for the antimicrobial activity of propolis type 6; b) Sub-fraction 1, belonging to the benzophenone class, was responsible for the antimicrobial activity observed in the present study. The identification of the bioactive compound will improve the development of more efficient uses of this natural product.

Anti-Candida activity of Brazilian medicinal plants.

Essential oils and ethanolic extracts from the leaves and/or roots of 35 medicinal plants commonly used in Brazil were screened for anti-Candida albicans activity. The oils were obtained by water-distillation using a Clevenger-type system. Essential oils from 13 plants showed anti-Candida activity, including Aloysia triphylla, Anthemis nobilis, Cymbopogon martini, Cymbopogon winterianus, Cyperus articulatus, Cyperus rotundus, Lippia alba, Mentha arvensis, Mikania glomerata, Mentha piperita, Mentha sp., Stachys byzantina, and Solidago chilensis. The ethanol extract was not effective at any of the concentrations tested. Chemical analyses showed the presence of compounds with known antimicrobial activity, including 1,8-cineole, geranial, germacrene-D, limonene, linalool, and menthol.

Antiulcerogenic activity of some sesquiterpene lactones isolated from Artemisia annua.

Artemisinin 1, dihydro-epideoxyarteannuin B 2 and deoxyartemisinin 3 were isolated from the sequiterpene lactone-enriched fraction obtained from the crude ethanolic extract of Artemisia annua L. These compounds were tested on ethanol and indomethacin-induced ulcer models. Compound 1 did not afford cytoprotection under the experimental models tested. Only compounds 2 and 3 decreased the ulcerative lesion index produced by ethanol and indomethacin in rats. These compounds did not demonstrate antiulcerogenic activity when tested on the ethanol-induced ulcer model, with previous administration of indomethacin, suggesting that the antiulcerogenic activity is a consequence of prostaglandin synthesis increase.

Dosagem de artemisinina em Artemisia annua L. por cromatografia líquida de alta eficiência com detecção por índice de refração

Artemisinin is a sesquiterpene lactone used in treatment of chloroquine-resistant malaria. This paper presents high-performance liquid chromatographic assay for artemisinin in leaves of A. annua using differential refractometer detector and a single step of clean-up in a silica cartridge. The average of recoveries were 95 percent and the limit of quantification was 0,21 percent p/p using 200 mg of the leaves. This method was found to be simple, robust and relatively rapid.