Honey and Aloe vera Solution Increases Survival and Modulates the Tumor Size In Vivo.

SCOPE: The combination of honey and Aloe vera is used as a popular complementary treatment for cancer due to their nutraceutical properties. This study aims to investigate the anticancer activity of honey and A. vera solution and its ethanolic extraction through in vitro and in vivo approaches. METHODS AND RESULTS: After comparisons of honey and A. vera (HA) solution and its ethanolic extraction solution (E) samples by UPLC-ESI-MS/MS, the study verifies HA-treatment affected only Walker tumor cells viability at the highest dose, and E-treatment has a more cytotoxic/antiproliferative effect in MCF-7 and Walker-256 cells. The in vivo results show a higher survival rate in Walker-256 tumor-bearing rats (WHA), with higher NK cell infiltration in tumor tissue and a tendency in the WE group. These results are possible due to decreased mannose-based immunomodulatory polysaccharides and aloin-A contents in the ethanolic extract solution compared to HA solution. CONCLUSION: The current study provides compelling evidence of selectively cytotoxic against tumor cells under honey and A. vera solution and ethanolic extraction solution treatment, due to the cytotoxic/antiproliferative compounds. Therefore, the use of honey and A. vera solution could be used as a basis for coadjuvant therapy in cancer treatment.

Tempol effect on oxidative and mitochondrial markers in preclinical models for prostate cancer.

Background: Tempol is a redox-cycling nitroxide considered a potent antioxidant. The present study investigated the tempol effects on oxidative stress and mitochondrial markers on prostate cancer (PCa). Methods: PC-3 and LnCaP cells were exposed to tempol. Cell viability test, western blot and Amplex Red analyses were performed. In vivo, five experimental groups evaluated tempol effects in the early (CT12 and TPL12 groups) and late stages (CT20, TPL20-I, and TLP20-II) of PCa development. The TPL groups were treated with 50 or 100 mg/kg tempol doses. Control groups received water as the vehicle. The ventral lobe of the prostate and the blood were collected and submitted to western blotting or enzymatic activity analyses. Results: In vitro, tempol decreased cell viability and differentially altered the H2O2 content for PC-3 and LNCaP. Tempol increased SOD2 levels in both cell lines and did not alter Catalase protein levels. In vivo, tempol increased SOD2 levels in the early stage and did not change Catalase levels in the different PCa stages. Systemically, tempol decreased SOD2 levels in the late-stage and improved redox status in the early and late stages, which was confirmed by reduced LDH in tempol groups. Alterations on energetic metabolism and oxidative phosphorylation were observed in TRAMP model. Conclusion: Tempol can be considered a beneficial therapy for PCa treatment considering its antioxidant and low toxicity properties, however the PCa progression must be evaluated to get successful therapy.

Two new naphthoquinone derivatives from Sinningia conspicua (Gesneriaceae).

Two new naphthoquinones, 7-hydroxy-2-O-methyldunniol (1) and 7-methoxy-2-O-methyldunniol (2) were isolated from the tubers of Sinningia conspicua (Seem.) G. Nicholson (Gesneriaceae). Nine known compounds were also obtained: 7-methoxydunniol (3), dunniol (4), 7-methoxy-α-dunnione (5), 7-hydroxydunnione (6), 2,4,4',6-tetramethoxychalcone (7), loureirin B (8), allo-calceolarioside A (9), ß-sitosterol (10) and stigmasterol (11). This is the first report of compounds 3 and 5 in Sinningia. n-Hexane, ethyl acetate and ethanol extracts, and compounds 1-5 were tested for cytotoxic activity against PC-3 (prostate) and SKMEL 103 (melanoma) human tumour cell lines and also against the 3T3 (fibroblast) non-cancer cell line. All samples were inactive.

Cymbopogon citratus Essential Oil Increases the Effect of Digluconate Chlorhexidine on Microcosm Biofilms.

The aim of this study was to evaluate the effect of the Cymbopogon citratus essential oil and its association with chlorhexidine on cariogenic microcosm biofilm composition and acidogenicity. Minimum inhibitory and bactericide concentrations from the essential oil and chlorhexidine were determined by broth microdilution assay. Microcosms (polymicrobial) biofilms were produced on glass coverslips, using inoculum from human saliva in McBain culture medium (0.5% sucrose exposure for 6 h/day) for 3 days in 24-well plates. The biofilms were treated twice a day and their composition was evaluated by microorganism quantification. The acidogenicity was evaluated by measuring the pH of the spent culture medium in contact with the biofilm. Overall, the association of C. citratus and chlorhexidine reduced total bacterial counts and aciduric bacteria (maximum reduction of 3.55 log UFC/mL) in microcosm biofilms. This group also presented the lowest acidogenicity even when exposed to sucrose-containing medium. C. citratus essential oil increases the effect of digluconate chlorhexidine on microcosm biofilms. Based on these findings, this study can contribute to the development of new formulations that might allow for the use of mouthwashes for a shorter period, which may reduce undesirable effects and increase patient compliance to the treatment.

Multiple LEDT wavelengths modulate the Akt signaling pathways and attenuate pathological events in mdx dystrophic muscle cells.

This study is aimed at investigating the effects of LEDT, at multiple wavelengths, on intracellular calcium concentration; on transient receptor potential canonical channels; on calcium-binding protein; on myogenic factors; on myosin heavy chains; on Akt signaling pathway; on inflammatory markers; and on the angiogenic-inducing factor in dystrophic muscle cell culture experimental model. Dystrophic primary muscle cells were submitted to LEDT, at multiple wavelengths (420 nm, 470 nm, 660 nm, and 850 nm), and evaluated after 48 h for cytotoxic effects and intracellular calcium content. TRPC-1, TRPC-6, Calsequestrin, MyoD, Myogenin, MHC-slow, MHC-fast, p-AKT, p-mTOR, p-FoxO1, Myostatin, NF-κB, TNF-α, and VEGF levels were evaluated in dystrophic primary muscle cells by western blotting. The LEDT, at multiple wavelengths, treated-mdx muscle cells showed no cytotoxic effect and significant lower levels in [Ca2 +]i. The mdx muscle cells treated with LEDT showed a significant reduction of TRPC-1, NF-κB, TNF-α and MyoD levels and a significant increase of Myogenin, MHC-slow, p-AKT, p-mTOR, p-FoxO1 levels, and VEGF levels. Our findings suggest that different LEDT wavelengths modulate the Akt-signaling pathways and attenuate pathological events in dystrophic muscle cells, and a combined multiwavelength irradiation protocol may even provide a potentially therapeutic strategy for muscular dystrophies.

Aloe vera and Honey Solution and Their Ethanolic Extraction Solution Could Act on Metastasis-Regulating Processes in Walker 256 Tumor Tissues In Vivo?

Research has shown that both Aloe vera and honey have anticancer and nutrition properties, including the inhibition of metastasis. In order to evaluate the effect of a solution of Aloe vera and honey (A) and their ethanolic fraction (F) on metastasis-regulating processes in primary tumors, Wistar rats were subcutaneously implanted with Walker 256 tumors and treated with A and F (670 µl/kg by gavage, daily for 21 days). An analysis of the primary tumor tissues of these animals showed a decrease in N-cadherin expression in groups WA and WF, with a concomitant increase in E-cadherin expression in group WA compared to the control group. Cathepsin D activity was also decreased in the tumor tissues from groups WA and WF. In addition, the number of blood vessels and their diameter significantly reduced in tumor tissues from groups WA and WF compared to those from control group. UHPLC-ESI-MS/MS analysis of the samples A and F, suggested presence of molecules with verified antitumor activity, including caffeic acid, ferulic acid, mannose, aloin A, aloin B, pinocembrin, chrysin, and kaempferol. These data showed that treatment with A and F could reduce the metastatic propensity of tumors by modulating neoangiogenesis and the process of epithelial-to-mesenchymal transition.

Chemical composition and antiproliferative, antioxidant and trypanocidal activities of the fruits from Campomanesia xanthocarpa (Mart.) O. Berg (Myrtaceae).

Chemical investigation of the extracts of the fruits from Campomanesia xanthocarpa resulted in the isolation of six known compounds identified by NMR and comparison with literature data (2',4'-dihydroxy-5'-methyl-6'-methoxychalcone (1), 2',4'-dihydroxy-3',5'-dimethyl-6'-methoxychalcone (2), 2'-hydroxy-3'-methyl-4',6'-dimethoxychalcone (3), 2',6'-dihydroxy-3'-methyl-4'-methoxychalcone (4), 5-hydroxy-7-methoxy-8-methylflavanone (5) and 7-hydroxy-5-methoxy-6-methylflavanone (6)). The considerable antioxidant capacity of the extracts was demonstrated by ORAC-FL and DPPH tests. The antiproliferative assay of the extracts and 5 was done in vitro, against many different cancer cell lines besides a healthy one. The extracts presented low cytotoxicity and the substance demonstrated promising results against all the cancer cell lines tested, with IC50 values ranging from 4.75 to 45.81 µmol L-1. The in vitro trypanocidal activity was evaluated against the epimastigote form of the Y strain of Trypanosoma cruzi and an improvement in the activity of the substances 2 (221.81 µmol L-1) and 5 (61.87 µmol L-1) was observed regarding the values obtained for the extracts.

Bioguided identification of antimicrobial compounds from Chrysopogon zizaniodes (L.) Roberty root essential oil.

Aim: To determine the group of compounds from Chrysopogon zizaniodes root essential oil that have antimicrobial activity. Materials & methods: Thin-layer chromatography coupled to direct bioautography was used to determinate the fraction(s) having antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VREF). Through GC-MS identification, the fractions with the greatest similarity to the active thin-layer chromatography fraction were used to determinate the MIC. Results: The subfraction 8 from column chromatography was responsible for the best MIC for MRSA (62.5 µg/ml) and VREF (125 µg/ml). Five compounds possibly responsible for antimicrobial activity were preliminary identified. Conclusion: We suggest that Cedr-8-en-13-ol, could be the more relevant compound involved in the antimicrobial activity in this study.

Anticonvulsant, sedative, anxiolytic and antidepressant activities of the essential oil of Annona vepretorum in mice: Involvement of GABAergic and serotonergic systems.

Annona vepretorum is an endemic species of the Caatinga biome, known in Northeastern Brazil as "araticum" and/or "pinha da Caatinga". In the present study it was evaluated the neuropharmacological potential of the essential oil obtained from the leaves of Annona vepretorum, as well as of the inclusion complexes of oil obtained with cyclodextrin. Thus, were used neuropharmacological tests already consolidated in the literature like open-field, elevated plus maze, rota-rod, tail suspension test, thiopental-induced sleep test, among others. The acute treatment of essential oil (EO) has anxiolytic, sedative, antiepileptic and antidepressant effects. The anxiolytic and anticonvulsant effects seems to be related to the GABAergic system, probably in the receptor subtypes that mediate the effects of the benzodiazepines, to generate anxiolytic activity. The sedative effect seems to be involved with other signaling pathways. The antidepressant effect of EO seems to be related to its action on serotonergic receptors. It was verified that some behavioral parameters were improved with the oil complexed with ß-cyclodextrin, but this effect was not uniform for all the doses and tests used. Further studies are needed in order to use other options for drug delivery systems. Thus, the essential oil of Annona vepretorum is a promising agent with neurobiological activity and a potential target for drug discovery, since the natural products such as medicinal plants have been a source of new therapeutic proposals.

Mouthwash containing Croton doctoris essential oil: in vitro study using a validated model of caries induction.

AIM: To validate an in vitro caries model and to evaluate an experimental mouthwash containing Croton doctoris essential oil.  Materials & methods: To validate the experimental model, we used McBain medium and polymicrobial biofilms. The EOM (essential oil mouthwash) was tested using the validated model. Microbial composition (colony-forming unit/ml), acidogenicity, enamel demineralization (percentage of surface enamel hardness loss), cytotoxicity and essential oil composition were evaluated. RESULTS: The model was validated with 0.5% sucrose, duration of 4 days and treatments twice per day. There were statistically significant differences between the EOM, the negative control and chlorhexidine mouthwash in colony-forming unit/ml and percentage of surface enamel hardness loss. Cytotoxicity was similar to that of chlorhexidine mouthwash.  A total of 66.11% of the essential oil consists of sesquiterpenes. CONCLUSION: The experimental mouthwash showed antimicrobial activity against polymicrobial biofilms and reduced enamel demineralization.

Diuretic herb Gomphrena celosioides Mart. (Amaranthaceae) promotes sustained arterial pressure reduction and protection from cardiac remodeling on rats with renovascular hypertension.

ETHNOPHARMACOLOGICAL RELEVANCE: Gomphrena celosioides Mart., belonging to the Amaranthaceae family, is a weed known as "perpétua," and its ethnopharmacological use is to treat of urinary tract disorders and kidney stones. Urinary tract disorders and kidney stones could include several pathological conditions such hypertension, diuretic and lithiasic problems. In the present work a model of renovascular hypertension was developed in vivo to investigate its usefulness as an antihypertensive drug. AIM OF THE STUDY: Evaluate the effect of acute and 28 day oral administration of G. celosioides extract on systemic arterial pressure and diuresis of renovascular-hypertensive rats, as well as its effect on cardiac remodeling and vascular reactivity. MATERIALS AND METHODS: Ethanolic extract of G. celosioides (EEGC) was used. To induce renovascular hypertension, adult male Wistar rats were submitted to Goldblatt 1K1C or 2K1C surgery. The mean arterial pressure (MAP) of 1K1C animals was directly assessed by cannulation of the carotid artery before and after intraduodenal acute administration of 30, 100 or 300 mg/kg of EEGC. For the 4-week assay, 2K1C animals received daily treatments with water (control group), 100 mg/kg EEGC or 15 mg/kg enalapril for 28 days. Diuresis and caudal blood pressure were assessed weekly, and at the 28th day of treatment, the MAP was directly quantified shortly before euthanasia. Internal organs were removed, weighed and routinely processed for histology and the left ventricle wall was measured. Blood was collected for biochemical analysis and mechanism investigation by quantification of angiotensin converting enzyme (ACE) activity and aldosterone, nitrite and thiobarbituric acid reactive substances (TBARS) concentration. The rats' mesenteric beds were isolated and cannulated to have their pressure variation assessed after crescent doses of phenylephrine (Phe), acetylcholine (ACh) and sodium nitroprusside (SNP). RESULTS: EEGC acutely reduced MAP the dose of 100 mg/kg. In the 4-week assay, EEGC acted as diuretic after acute administration after 1, 2, 3 and 4 weeks of treatment. EEGC also acted as an antihypertensive and it showed significant difference already after 1 week (and after 3 and 4 weeks) compared to control, with its MAP close to pre-surgery values at the end of the experiment. It promoted ACE inhibition, which led to lower aldosterone levels. The lower TBARS and higher nitrite concentration found in the EEGC group suggest antioxidant activity and NO maintenance. Moreover, EEGC counteracted the impairment of vascular reactivity induced by renovascular hypertension. The extract group presented thinner left ventricle wall compared to the control, meaning reduced hypertension-induced cardiac remodeling. CONCLUSIONS: The G. celosioides diuretic effect is maintained on renovascular hypertensive rats and can reduce the blood pressure after the first week of treatment by inhibiting ACE and these effects are longstanding and strong enough to promote protection against cardiac remodeling. Therefore, it shows potential as an antihypertensive drug.

Neuropharmacological effects of essential oil from the leaves of Croton conduplicatus Kunth and possible mechanisms of action involved.

ETHNOPHARMACOLOGICAL RELEVANCE: Croton conduplicatus Kunth (Euphorbiaceae) is a Brazilian aromatic medicinal plant, widely known as "quebra-faca". In folk medicine, its leaves and stem-barks are used as a natural analgesic for the treatment of headaches. AIM OF THE STUDY: In this study, we describe for the first time the neuropharmacological potential of the essential oil obtained from the leaves of Croton conduplicatus (EO) in experimental models of pain, anxiety and insomnia. The mechanisms of action involved in these activities were also investigated. MATERIAL AND METHODS: Different experimental models were used to evaluate the antinociceptive (acetic acid, formalin-induced nociception and hot plate tests), anxiolytic (elevated plus maze and hole board tests) and sedative (thiopental-induced sleeping time) effects of EO in mice. EO was evaluated in three different doses (25, 50 and 100 mg/kg, i.p.) and compared with positive and negative controls in all experimental protocols. When appropriate, animals were pretreated with pharmacological antagonists (naloxone, atropine and flumazenil) in order to evaluate the mechanisms of action involved. A docking study also was performed to identify possible targets involved. RESULTS: EO (25, 50 and 100 mg/kg, i.p.) demonstrated a significant antinociceptive activity in all experimental models. Pretreatment with naloxone or atropine reversed the antinociceptive response (p < 0.05), suggesting the involvement of opioid and muscarinic receptors, respectively. A docking study was performed with the major components identified in EO (1,8 cineole - 21.42%, spathulenol - 15.47%, p-cymene - 12.41% and caryophyllene oxide - 12.15%), demonstrating favorable interaction profile with different subtypes of muscarinic (M2, M3 and M4) and opioids (delta and mu) receptors. EO also showed anxiolytic (mainly at doses of 25 and 50 mg/kg, i.p.) and sedative (only at the dose of 100 mg/kg, i.p.) effects in mice. These pharmacological responses were reversed by flumazenil (p < 0.05), indicating possible involvement of GABAA receptors. CONCLUSION: Our findings support the traditional use of this plant as a natural analgesic and suggest that EO is a multi-target natural product, presenting not only antinociceptive effect but also anxiolytic and sedative activities depending on the dose used.

Cymbopogon citratus essential oil: effect on polymicrobial caries-related biofilm with low cytotoxicity.

The objective of this study was to evaluate the effects of Cymbopogon citratus essential oil and its main compound (citral) against primary dental colonizers and caries-related species. Chemical characterization of the essential oil was performed by gas chromatography/mass spectroscopy (GC/MS), and the main compound was determined. Antimicrobial activity was tested against Actinomyces naeslundii, Lactobacillus acidophilus, S. gordonii, S. mitis, S. mutans, S. sanguinis and S. sobrinus. Minimum inhibitory and bactericide concentrations were determined by broth microdilution assay for streptococci and lactobacilli reference, and for clinical strains. The effect of the essential oil on bacterial adhesion and biofilm formation/disruption was investigated. Negative (without treatment) and positive controls (chlorhexidine) were used. The effect of citral on preformed biofilm was also tested using the same methodology. Monospecies and microcosm biofilms were tested. ANOVA or Kruskal-Wallis tests were used (α=0.05). Cytotoxicity of the essential oil to human keratinocytes was performed by MTT assay. GC/MS demonstrated one major component (citral). The essential oil showed an inhibitory effect on all tested bacterial species, including S. mutans and L. acidophilus. Essential oil of C. citratus (10X MIC) reduced the number of viable cells of lactobacilli and streptococci biofilms (p < 0.05). The essential oil inhibited adhesion of caries-related polymicrobial biofilm to dental enamel (p < 0.01). Citral significantly reduced the number of viable cells of streptococci biofilm (p < 0.001). The essential oil showed low cytotoxicity to human keratinocytes. Based on these findings, this study can contribute to the development of new formulations for products like mouthwash, against dental biofilms.

Oral treatment with essential oil of Hyptis spicigera Lam. (Lamiaceae) reduces acute pain and inflammation in mice: Potential interactions with transient receptor potential (TRP) ion channels.

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Hyptis comprehends almost 400 species widespread in tropical and temperate regions of America. The use of Hyptis spicigera Lam. (Lamiaceae) is reported in traditional medicine due to its gastroprotective, anti-inflammatory and analgesic properties. AIM OF THE STUDY: The rationale of this study was to investigate the potential use of the essential oil of H. spicigera (EOHs) as analgesic. MATERIAL AND METHODS: The antinociceptive effect of EOHs was verified analyzing acute nocifensive behavior of mice induced by chemical noxious stimuli [i.e., formalin and transient receptor potential (TRP) channels agonists]. We also verified the effects of EOHs on locomotor activity and motor performance in mice. Finally, we investigate the involvement of central afferent C-fibers with EOHs analgesic effect. RESULTS: EOHs presented antinociceptive effect at 300 and 1000mg/kg on formalin-induced pain behavior model, presenting 50% and 72% of inhibition during the first phase (ED50 =292mg/kg), and 85% and 100% during de second phase (ED50 =205mg/kg), respectively. Temperature of the hind paw was reduced by EOHs treatment in a dose-dependent manner; oedema was diminished only by EOHs 1000mg/kg. EOHs does not impaired locomotor activity or motor performance. For mice injected with capsaicin, a TRPV1 activator, EOHs (1000mg/kg, ED50 =660mg/kg) showed decreased (63%) nociceptive behavior. When injected with cinnamaldehyde (TRPA1 activator), mice treated with EOHs showed 23%, 43% and 66% inhibition on nociceptive behavior (100, 300 and 1000mg/kg, respectively; ED50 402mg/kg). When mice were injected with menthol (TRPM8 activator), EOHs showed 29%, 59% and 98% inhibition of nociceptive behavior (100, 300 and 1000mg/kg, respectively; with ED50 =198mg/kg. Finally, when desensitized mice were injected with menthol, EOHs (300mg/kg) does not show antinociceptive effect. CONCLUSIONS: This study demonstrated the efficacy of EOHs on experimental models of nociception. We have found the involvement of TRP channels V1, A1 and M8 with EOHs activity, which was remarkably potent and efficient in inhibiting pain evoked by menthol, a TRPM8 channel activator. TRPM8 channels from TRPV1+ C-fibers, but not TRPM8+ C-fibers nor TRPM8+ Aδ mechanosensory fibers, mediate EOHs analgesic effects.

Cymbopogon citratus essential oil: effect on polymicrobial caries-related biofilm with low cytotoxicity

Abstract The objective of this study was to evaluate the effects of Cymbopogon citratus essential oil and its main compound (citral) against primary dental colonizers and caries-related species. Chemical characterization of the essential oil was performed by gas chromatography/mass spectroscopy (GC/MS), and the main compound was determined. Antimicrobial activity was tested against Actinomyces naeslundii, Lactobacillus acidophilus, S. gordonii, S. mitis, S. mutans, S. sanguinis and S. sobrinus. Minimum inhibitory and bactericide concentrations were determined by broth microdilution assay for streptococci and lactobacilli reference, and for clinical strains. The effect of the essential oil on bacterial adhesion and biofilm formation/disruption was investigated. Negative (without treatment) and positive controls (chlorhexidine) were used. The effect of citral on preformed biofilm was also tested using the same methodology. Monospecies and microcosm biofilms were tested. ANOVA or Kruskal-Wallis tests were used (α=0.05). Cytotoxicity of the essential oil to human keratinocytes was performed by MTT assay. GC/MS demonstrated one major component (citral). The essential oil showed an inhibitory effect on all tested bacterial species, including S. mutans and L. acidophilus. Essential oil of C. citratus (10X MIC) reduced the number of viable cells of lactobacilli and streptococci biofilms (p < 0.05). The essential oil inhibited adhesion of caries-related polymicrobial biofilm to dental enamel (p < 0.01). Citral significantly reduced the number of viable cells of streptococci biofilm (p < 0.001). The essential oil showed low cytotoxicity to human keratinocytes. Based on these findings, this study can contribute to the development of new formulations for products like mouthwash, against dental biofilms.

Antimicrobial photodynamic effect of extracts and oxoaporphine alkaloid isomoschatoline from Guatteria blepharophylla.

Photodynamic Therapy, a tumor therapy idealized at the beginning of the last century, emerges nowadays as a promising treatment alternative against infectious diseases. In this study we report a bioguided study of Guatteria blepharophylla phytoderivatives for antimicrobial PDT. Crude extracts and fraction from the species bark were obtained and further fractionated for substances isolation. All samples were evaluated in relation to their photophysical (absorbance and fluorescence) and photochemical properties (1,3-DPBF bleaching method). Then, bioassays were conducted using as biological models bacteria and yeast strains and a diode laser as a light source. Phytochemical analyses lead to the isolation of 5 isoquinoline alkaloids from oxoaporphine subclass, denominated GB1 to GB5. Photophysical and photochemical analysis showed that extracts, fraction and GB1 (isomoschatoline) presented absorption profile with bands at 600-700nm and were positive for singlet oxygen production. Photobiological assays indicate that these samples presented photodynamic antimicrobial activity against both gram-positive and gram-negative bacterial and some Candida ssp. yeast strains at sub-inhibitory concentrations. The susceptibility of gram-negative bacteria was significantly enhanced when CaCl2 or MgCl2 were employed. Greater energy doses and double sample's dosage also decreased microbial survival. It is suggested that GB1 photodynamic activity happens through both types I and II photochemical mechanisms, but with a predominance of the latter. Phytoderivatives of G. blepharophylla promoted antimicrobial effect, however more detailed study concerning chemical composition of the crude extracts and fractions as also photophysical and photochemical characteristics of GB1 are necessary to ensure their potential as photosensitizers at antimicrobial photodynamic inactivation.

Chemical composition of the essential oil from the leaves of Anaxagorea brevipes (Annonaceae) and evaluation of its bioactivity.

The essential oil obtained by hydrodistillation from leaves of Anaxagorea brevipes was analysed by gas chromatography fitted with a flame ionisation detector (GC-FID) and coupled to mass spectrometry (GC-MS). Thirty one components were identified, representing around 75.7% of total oil. The major components were ß-eudesmol (13.16%), α-eudesmol (13.05%), γ-eudesmol (7.54%), guaiol (5.12%), caryophyllene oxide (4.18%) and ß-bisabolene (4.10%). The essential oil showed antimicrobial activity against Gram-positive bacteria and yeast with the MIC values between 25.0 and 100 µg/mL. The highest antiproliferative activity was observed for the oil against MCF-7 (breast, TGI = 12.8 µg/mL), NCI-H460 (lung, TGI = 13.0 µg/mL) and PC-3 (prostate, TGI = 9.6 µg/mL) cell lines, while against no cancer cell line HaCat (keratinocyte) the TGI was 38.8 µg/mL. The oil exhibited a small antioxidant activity assessed through ORAC-FL assay (517 µmol TE/g). This is the first report regarding the chemical composition and bioactivity of A. brevipes essential oil.

Antiproliferative activity, antioxidant capacity and chemical composition of extracts from the leaves and stem of Chresta sphaerocephala

AbstractIn this study, antiproliferative and antioxidant activities of crude extracts (hexane, ethyl acetate and methanol) from leaves and stem of Chresta sphaerocephala DC., Asteraceae, were investigated. Antiproliferative activity was tested in vitro against ten human cancer cells and against VERO (no cancer cell). Antioxidant activities were determined using DPPH and ORAC-FL assays and the total phenolic content was estimated by Folin–Ciocalteu method. Hexane and ethyl acetate extracts (leaves and stem) exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 50.40 and 250 µg/ml. For VERO cell, TGI values were >250 µg/ml for all extracts, except to hexane extract of the stem (TGI 80.92 µg/ml). In an initial evaluation, ethyl acetate and methanol extracts (leaves and stem) have shown levels of phenolic compounds between 6.94 and 30.96 mg GAE/kg in Folin–Ciocalteu assay, DPPH free-radical scavenging activity with SC50 in the range of 75.22 and 400 µg/ml and antioxidant capacity between 290.08 and 1088 µmol TE/g of extract in ORAC-FL assay. HPLC-DAD and ESI-MS analysis allowed the identification of flavonoids in the methanol extract from the leaves of C. sphaerocephala. Three steroids and nine triterpenoids were identified in the bioactive hexane extracts using HRGC.

Anti-hyperalgesic and Anti-inflammatory Activity of Alternanthera Maritima Extract and 2″-O-α-L-rhamnopyranosylvitexin in Mice.

Alternanthera maritima are used in Brazilian popular medicine for the treatment of inflammatory and infectious diseases. Species of Alternanthera have demonstrated biological activities in previous scientific studies. The aim of this study was to determine whether the ethanol extract of the aerial parts of A. maritima (EEAM) and the isolated compound 2″-O-α-L-rhamnopyranosyl-vitexin inhibit mechanical hyperalgesia and parameters of inflammation in mice. The oral administration of EEAM significantly inhibited carrageenan (Cg)-induced paw edema and reduced leukocyte migration into the pleural cavity. 2″-O-α-L-rhamnopyranosylvitexin significantly inhibited paw edema and reduced both leukocyte migration and the leakage of protein into the pleural cavity. Both EEAM and 2″-O-α-L-rhamnopyranosylvitexin significantly prevented the Cg-induced hyperalgesia. Local administration of 2″-O-α-L-rhamnopyranosylvitexin significantly prevented the Cg- and tumor necrosis factor (TNF)-induced hyperalgesia. In conclusion, this study demonstrated that EEAM is an anti-inflammatory and anti-hyperalgesic agent, and the results suggested that 2″-O-α-L-rhamnopyranosylvitexin is responsible for the effects of EEAM and the mechanism involves the TNF pathway.

Two new hydronaphthoquinones from Sinningia aggregata (Gesneriaceae) and cytotoxic activity of aggregatin D.

Two new hydronaphthoquinones, aggregatins E and F (1 and 2, resp.) were isolated from the tubers of Sinningia aggregata (Ker-Gawl.) Wiehler (Gesneriaceae), along with twelve known compounds aggregatin D (3), tectoquinone (4), 1-hydroxy-2-methylanthraquinone (5), icosyl ferulate (6), pustuline (7), 1,6-dihydroxy-2-methylanthranquinone (8), 6-hydroxy-2-methylanthraquinone (9), 7-hydroxy-2-methylanthraquinone (10), tyrosol (11), halleridone (12), calceolarioside B (13), and cornoside (14). All compounds were identified by analysis of spectroscopic and spectrometric data. Compounds 3, 4, and 10 had already been reported in this species. Compounds 2 and 3 were evaluated against several tumor cell lines, but only 3 exhibited activities against UACC-62, 786-0 and OVCAR-3 cell lines, with IC50 values of 12.3, 12.8 and 0.3 µg/ml, respectively, without toxic effects on non-cancer cell line HaCat (human keratinocyte).