Brazilian Folk Medicine Research Articles

Characterization of the volatile compounds and anatomical features in commercial samples of Echinodorus plant species

Echinodorus grandiflorus and Echinodorus macrophyllus are medicinal plants that are widely used in Brazilian folk medicine. The aims of this study were to evaluate the effect of oven drying with ventilation on the chromatographic profile of volatile compounds and to compare the leaf anatomy and volatile compounds of different commercial E. macrophyllus (Kunth) Micheli and E. grandiflorus Mich. Samples. The components found in fresh and dried samples were extracted by SPME and analysed by GC-MS, and the anatomical features of the leaves were observed microscopically. A total of 46 compounds were identified; five compounds were present in the dried and fresh samples of E. grandiflorus and all of the commercial samples. The anatomy analyses confirmed the authenticity of the species. Apparent differences in the volatile composition between the species were observed, allowing the identification of chemical marker. The results showed that commercial establishments do not conform to regulations, and the techniques used were effective for the characterization of volatile compounds and for quality control of medicinal plants.

Comparative analyses of metabolic fingerprint integrated with cytotoxic activity and in silico approaches of the leaves extract of Spondias mombin L. and Spondias tuberosa Arr. Cam. from Northeast, Brazil

Spondias species are a relevant source of natural-bioactive compounds in Brazilian folk medicine, and its biological potential has not been explored. Thus, this study aimed to determine the metabolomic fingerprint of Spondias mombin and Spondias tuberosa leaves based on the use of reversed-phase liquid chromatography coupled to a high-resolution mass spectrometer (UPLC-HRMS). The analysis by UPLC-HRMS allowed the annotation of 31 metabolites. The multivariate analysis allowed us to identify the biomarkers responsible for the distinction between species. Also, we correlate the biomarkers of S. mombin and S. tuberosa as supposed responsible for the difference in the degree of cytotoxicity between them. The in silico evaluation was performed to give more consistency to the correlation between biomarkers and cytotoxicity, which were compared to commercial drugs. Therefore, this study showed that S. mombin has the potential to become an input for the pharmaceutical industry as a source of raw material that can positively impact the sectors of agricultural production.

Contribution of spathulenol to the anti-nociceptive effects of Psidium guineense

ABSTRACT Objectives: Araçá-verdadeiro is the popular name of Psidium guineense (Myrtaceae), whose fruits and leaves are used in Brazilian folk medicine for treatment of inflammation and pain. The focus of the present research was an investigation of the anti-nociceptive, and anti-inflammatory effects of the essential oil from P. guineense (EOPG) leaves, and of spathulenol. The anxiolytic and antidepressive effects associated with chronic pain were also investigated in models of acute or persistent nociception or/and inflammatory pain. Methods and Results: Oral treatment with EOPG (10–100 mg/kg) or spathulenol (10 mg/kg) significantly inhibited formalin-induced nociceptive responses, both sensitivity to cold and edema. Oral treatment with EOPG (10 mg/kg) and spathulenol (10 mg/kg) did not reduce locomotor activity (open field test). Local administration of spathulenol (1000 µg/paw) significantly prevented formalin-induced nociceptive sensitivity to cold and paw edema, and carrageenan-induced mechanical hyperalgesia, paw edema and sensitivity to cold. In the Freund's complete adjuvant (CFA) model, oral treatment with EOPG (10 mg/kg) or spathulenol (10 mg/kg) for 21 days significantly inhibited all analyzed parameters. The percentage maximal inhibition by spathulenol was 76.00% (mechanical hyperalgesia), 71.90% (cold response), 85.00% (edema), 77.16% (myeloperoxidase activity), 97.72% (time in the closed arms in the elevated plus maze), and 49.00% (immobility time in the tail suspension test), in the CFA model. Models employed male Swiss mice, except for the CFA test, which employed C57bL6 male mice (n=6 /group). Conclusion: This study demonstrates that EOPG is an anti-nociceptive and anti-hyperalgesic agent, in acute and continuous treatment, and an anxiolytic and antidepressive agent when tested with the chronic pain experimental state.

Davilla elliptica (Dilleniaceae) a. St.-Hil. Ethnomedicinal, phytochemical, and pharmacological aspects: A review

Abstract Davilla elliptica (Dilleniaceae) is a shrub that occurs naturally in the Brazilian Savannah (Cerrado). This shrub has been widely used in Brazilian folk medicine in tea preparing; infusions; and decoctions from leaves and roots for gastritis, ulcers, and diarrhea treatment. Given the therapeutic potential of this species, the present study provides a comprehensive review on its ethnopharmacological uses, botanical aspects, phytochemistry characterization, and in vivo and in vitro pharmacological studies. The relevant studies on D. elliptica were retrieved from the following scientific databases: Web of Science, Google Scholar, Scopus, SciFinder, PubMed, Scielo, and ScienceDirect. Additional information derived from other literature sources, such as books and Ph.D. and MSc theses, was also considered after a critical review. Ethnopharmacological reports of D. elliptica revealed the use of infusions from roots with tonic and purgative effects, whereas leaves have been used as anti-inflammatory and anti-ulcerative treatments, as well as to treat diarrhea and gastric disorders. Furthermore, fresh leaves have been used in baths to treat swelling. Phytochemical studies have led to the isolation of several compounds, including flavonoids derived from quercetin and myricetin, and tannins, which are known to exhibit relevant pharmacological activities. In vitro assays using crude extracts and/or isolated fractions and chemical constituents from D. elliptica have evidenced antibacterial, cytotoxic activities, while in vivo studies have proven gastroprotective, anti-inflammatory, antihemorrhagic, and antibacterial activities, corroborating ethnomedicinal reports. No relevant side effects has been reported previously, and some studies found a low toxicity and genotoxicity. However, further studies are still needed to ensure the safety of its therapeutic use. Future studies should focused on molecular mechanisms involved in bioactive components’ effects based on both fractions and isolated compounds, creating great opportunities for new investigations.

Gastroprotective activity of punicalagin and Lafoensia pacari in mice

Lafoensia pacari A. St.-Hil., Lythraceae, is used in Brazilian folk medicine to treat ulcer and gastritis; thus, it is important to conduct research so as to better understand its medicinal properties. The aim of this study was to assess the antisecretory and antiulcerogenic activities of lyophilized aqueous fraction and punicalagin isolated from leaves of L. pacari. Antisecretory gastric acid activity and antiulcerogenic activity were investigated by pyloric ligation-induced and indomethacin-induced gastric lesion models, respectively. Results show that the lyophilized aqueous fraction of L. pacari and punicalagin reduced the volume of gastric secretion, free acidity, and total acidity in mice 4 h after pyloric ligation, as well as the rate of gastric damage following the indomethacin administration model. Reduction percentages varied according to the dose of each treatment and showed statistical difference. This finding indicates that the lyophilized aqueous fraction of L. pacari and punicalagin exert an antiulcerogenic effect due to their acid antisecretory activity.

A treatment with a boiled aqueous extract of Hancornia speciosa Gomes leaves improves the metabolic status of streptozotocin-induced diabetic rats

BackgroundHancornia speciosa is usually used in Brazilian folk medicine to treat diabetes. The hypothesis of the present study is that this medicinal plant exerts beneficial effects on hyperglycemia, preventing diabetic complications. Therefore, the aim of this study was to evaluate the treatment effect of the aqueous extract of H. speciosa leaves on metabolic parameters of diabetic rats.MethodsThe H. speciosa extract (400 mg/Kg) was administered to both nondiabetic and severely diabetic female Wistar rats by gavage. The Oral Glucose Tolerance Test was performed and the area under the curve (AUC) was estimated on day 17 of pregnancy. After 21 days of treatment, the animals were anesthetized and killed to obtain organ weights. Blood samples were collected for an analysis of serum biochemical parameters.ResultsAfter treatment with the H. speciosa extract, the parameters of nondiabetic rats remained unchanged. In treated diabetic rats, glycemia, AUC, dyslipidemia parameters, and relative organ weights were decreased compared with nontreated diabetic rats. Severely diabetic rats showed decompensated hyperglycemia, polydipsia, hyperphagia and dyslipidemia. However, the aqueous extract of H. speciosa leaves decreased diabetes complications (indicating a lack of toxicity), reduced blood glucose levels, and exerced lipid-lowering effects.ConclusionBased on or findings, the H. speciosa leaf extract may be a safe and promising candidate treatment for diabetes and other diseases.

Evaluation of fruta-do-lobo (Solanum lycocarpum St. Hill) starch on the growth of probiotic strains

Fruta-do-lobo (Solanum lycocarpum St. Hill) is a native fruit commonly used in Brazilian folk medicine as a hypoglycemic agent. These properties are attributed to their starch, mainly its resistant fraction. Resistant starch has shown to increases the growth of Bifidobacterium and Lactobacillus in the gut, even though not being selective for these strains. In this scenario, this study aimed to investigate the potential prebiotic activity of fruta-do-lobo starch (FLS). FLS showed around 30% of resistant starch and their prebiotic potential was evaluated with five probiotic strains L. acidophilus (LA3 and LA5), L. casei (LC01) and B. animalis (BB12) and B. lactis (BLC1) in a concentration range of 1.0–2.0% of starch. In a preliminary screening, we evaluated, during 48 h, the viability of the starch with promoting growth agent. An increase in the growth of the probiotic strains tested was observed. We also evaluated the microorganism’s metabolic activity by assessing the short-chain fatty acid (SCFA) production, using the best starch growth promotion conditions (2% of FLS and strains BLC1, LA5, and LC01). As expected, MRS and lactose were preferentially metabolized by BLC1, with the highest growth rates: 0.231 and 0.224 h−1, respectively. However, for this strain, the FLS growth rate (0.222 h−1) was 65% higher than FOS (0.144 h−1). Also, for LA5 FLS promoted higher growth (0.150 h−1) than FOS (0.135 h−1). Additionally, FLS promoted acetate production. These data are promising and indicate that FLS may have prebiotic potential and more studies need to be done with pathogenic microorganisms.

In vitro antileishmanial and antioxidant activities of essential oils from different parts of Murraya paniculata (L.) Jack: a species of Rutaceae that occur in the Cerrado biome in Brazil

In Brazilian folk medicine, Murraya paniculata has been used for treating intestine disorders, rheumatism and cough. This paper aims to investigate the in vitro antileishmanial and antioxidant activities of essential oils (EO) from M. paniculata leaves and fruits (ripe and unripe ones). Natural antioxidants may be very beneficial to improve quality of life, since they are capable of protecting the body against damage caused by free radicals and, consequently, either preventing or postponing many diseases from starting their cycles. One of the techniques which has been widely used for detecting antioxidant compounds is the method based on the elimination of the stable free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH•). It has been considered easy, precise, fast, simple, economical and appropriate to determine antioxidant activity of pure substances and complex mixtures, such as EO. Thus, antioxidant potential of EO was evaluated by using the method of the free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH•). EO from M. paniculata leaves and fruits exhibited weak potential, since EC50 values were above 700 µg/mL. Several reports have stated that volatile oils from plants show promising leishmanicidal activity against promastigote forms of Leishmania amazonensis; in relation to this activity, leaf oil was highly active (IC50 = 7.33±2.07 µg/mL) while ripe and unripe fruit oils were active, with values of IC50 = 30.77±2.07 µg/mL and 13.04±1.64 µg/mL, respectively. Both GC-FID and GC-MS analyses revealed that the major components determined in EO from M. paniculata were sesquithujene (25.0%), trans-β-caryophyllene (23.8%), α-zingiberene (21.0%), α-ylangene (13.3%), germacrene D (13.1%), α-copaene (12.7%), and β-cubebene (10.2%). In vitro antileishmanial and antioxidant activities of EO from M. paniculata have also been described for the first time.

In vitro antimicrobial activity of Spiranthera odoratissima A. St. Hil. essential oils against foodborne pathogens and food spoilage bacteria

In Brazilian folk medicine, Spiranthera odoratissima has been used to treat rheumatism, infection and abdominal pain. Essential oils (EOs) are technological options that may be employed in natural foods due to their antimicrobial activities. This paper aimed to investigate the chemical composition and in vitro antibacterial effects of EOs from S. odoratissima leaves and flowers against foodborne and spoilage bacteria Listeria monocytogenes, Salmonella enteritidis, Salmonella typhimurium, Yersinia enterocolitica, Staphylococcus aureus, Escherichia coli, Clostridium botulinum, Bacillus cereus and Pseudomonas aeruginosa. Minimum inhibitory concentration (MIC) values of EOs were calculated by the broth microdilution method on 96-well microplates. Both GC-FID and GC-MS analyses revealed that the major components determined in EOs from S. odoratissima leaves were β-caryophyllene (23.8%), bicyclogermacrene (10.8%) and δ-cadinene (7.1%). Major constituents found in EOs from its flowers were β-caryophyllene (14.1%), spathulenol (8.1%) and γ-cadinene (7.2%). EOs from S. odoratissima leaves and flowers showed strong antibacterial activity against Yersinia enterocolitica (MIC = 0.30 mg/mL), Staphylococcus aureus (MIC = 0.12 mg/mL), Clostridium botulinum (MIC = 0.30 mg/mL), Bacillus cereus (MIC = 0.20 mg/mL) and Listeria monocytogenes (MIC = 0.25 mg/mL). These EOs could be important natural alternatives to prevent bacterial growth in food products.

Characterization of 3-aminospirostane alkaloids from roots of Solanum paniculatum L. with hepatoprotective activity.

Solanum paniculatum L., popularly known as jurubeba, has traditionally been used in Brazilian folk medicine for liver diseases. However, there is a lack of knowledge about the chemical characterization of 3-aminospirostane alkaloids, an important class related to pharmacological activities. This work aimed to characterize the alkaloids using liquid chromatography with tandem mass spectrometry (LC/MS/MS) supported by molecular networking and theoretical calculations as well as to evaluate the contribution to hepatoprotective activity. S. paniculatum roots were collected and macerated with MeOH/H2 O (8:2) obtaining the crude extract (SP-CE). From this, partition using EtOAc with pH variation yielded the alkaloidic fraction (SP-AF). Both were evaluated in an acute liver injury model (100 and 200 mg/kg), after intraperitoneal administration of carbon tetrachloride (CCl4 ) in mice. AST (aspartate transaminase) and ALT (alanine transaminase) serum levels were investigated, as well as the histopathological characteristics. The SP-CE and SP-AF were analyzed by LC/MS/MS, using quadrupole/time-of-flight and ion-trap systems. The alkaloids annotated by the GNPS molecular network had their structures defined using gas-phase ionization and fragmentation reaction supported by theoretical calculations. The SP-CE and SP-AF decreased the ALT serum levels compared with the negative control. The group treated with the SP-CE (at the highest dose) demonstrated a significant decrease of ALT. Hepatic cell degeneration decrease was observed mainly at the highest dose of the treatment. Detailed electrospray ionization MS/MS data allowed us to identify alkaloids not previously reported, to propose their gas-phase reactions and to redefine the initial open ring fragmentation mechanism of the steroidal alkaloids with the jurubidine moiety. The results allowed us to identify seven steroidal alkaloids from jurubeba and redefine the initial mechanism of fragmentation. A significant hepatoprotective effect was also demonstrated, corroborating its traditional use.

Investigation of the antioxidant and hypoglycemiant properties of Alibertia edulis (L.C. Rich.) A.C. Rich. leaves

Ethnopharmacological relevanceAlibertia edulis (L.C. Rich.) A.C. Rich is a vegetable species used in Brazilian folk medicine due to it is putative hypoglycemiant effect but has never been pharmacologically investigated. It is popularly used for the control of diabetes, especially in the state of Mato Grosso, Brazil. Following confirmation of the antioxidant activity of A. edulis by Aquino et al. (2017), the aim of this study was to evaluate the effects of leaves of A. edulis aqueous extract (AEAE) on some biochemical parameters in mice fed a high-fat fed. Material and methodsLeaves of A. edulis were air-dried in an oven at 40 °C for 10 days and ground into a fine powder by mechanical milling. The AEAE was prepared by decoction (1:10 w/v) at 97 °C for 15 min, and later filtered and lyophilized. Preliminary phytochemical analysis of the AEAE has been already indetified the presence of caffeic acid, quercetin 3-rhamnosyl-(1 → 6)-galactoside and iridois ioxide, ferulic acid and rutin in decocted leaves (Aquino et al., 2017). In one experiment, the acute oral toxicity AEAE was evaluated at 2,000 mg/kg of body weight. The animals were observed periodically for 14 days. In second experiment, the animals were divided into four groups (n = 5): Control, AEAE 200, AEAE 400 mg/kg and positive control (Metformin 100 mg/kg). In a third experiment, animals were divided into: Control RC (standard diet) (n = 24) and Control HFF (high-fat fed) (n = 24) groups for induction of glucose intolerance. After eight weeks, they were further subdivided into six groups (n = 8 each) RC or HFF with or without AEAE at doses of 200 and 400 mg/kg (2-wk) treatments to assess glucose tolerance. Plasma indicators of glucose tolerance and liver damage, skeletal muscle expression of antioxidant enzymes, and expression of the antioxidant proteins of superoxide dismutase (SOD), catalase, glutathione peroxidase (GPx) and phosphorylated IKK were determined. ResultsThe HF-fed animals developed glucose intolerance which the AEAE failed to revert. Meanwhile, the AEAE treatment did lower the glucose levels in the normolipidic cohorts by virtue of its antioxidant property. It was also observed that the treatment with the AEAE reduced food intake negatively interfering weight accretion. Beyond that, the treatment with AEAE interfered in the SOD and catalase expression and inhibited phosphorylation of IKK thus suggesting that the observed hypoglycemiant power may be related to its known antioxidant potential. No sings of toxicity or hemolysis were detectaed at indicating that, at the concentrations evaluated, the extract was not toxic to normal cells. ConclusionThe AEAE showed a hypoglycemiant effect in the normolipidic mice that received the control diet, but not in those that were made glucose-intolerant by consuming a high-fat fed. The extract also exhibited substantial protection against hemolysis and oxidative stress. Moreover, no signs of toxicity were evident at 2000 mg/kg of body weight.

Copaifera multijuga, Copaifera pubiflora and Copaifera trapezifolia Oleoresins: Chemical Characterization and in vitro Cytotoxic Potential against Tumoral Cell Lines

Copaifera species (Fabaceae) comprises approximately 70 species of large trees, from which 16 can be found in Brazil. The oleoresins obtained from their trunk are widely used in Brazilian folk medicine, which display important antitumoral potential. Chemically, these oleoresins are mainly composed of a mixture of sesquiterpenes and diterpenes. In this paper we are describing the isolation and identification of 12 already known terpenes from oleoresins obtained from three different Copaifera species (C. multijuga, C. pubiflora and C. trapezifolia) and 2 novel diterpenes (ent-16-hidroxy-3,13 clerodadien-15,18-dioic acid and ent-labda-5,13-dien-15-oic acid) from C. trapezifolia. Both new compounds were identified by nuclear magnetic resonance (NMR) spectroscopic (1H and 13C NMR, correlation 1H-1H (COSY), heteronuclear multiple quantum coherence (HMQC) and heteronuclear multiple bond correlation (HMBC)) and by high-resolution electrospray ionization mass spectrometry (HR-ESIMS) analyses. The cytotoxic potential of these oleoresins, their main non-volatile compounds and their volatile compound fractions were evaluated against a panel of tumoral (MCF-7, ACP01, A549, HeLa) and normal cell lines (MCF-10A, GM07492-A) through XTT (tetrazolium salt) and SRB (sulforhodamine B) assays. The novel diterpene ent-labda-5,13-dien-15-oic acid displayed relevant cytotoxic effect against most of the cancer cell lines with mean inhibitory concentration (IC50) values ranging from 3.57 ± 1.12 to 22.56 ± 1.03 µg mL-1, and a high selectivity level in both assays.

Anti-HIV-1 and antibacterial potential of Hyptis radicans (Pohl) Harley & J.F.B. Pastore and Hyptis multibracteata Benth. (Lamiaceae)

There is an urgency to develop more effective treatments to overcome the problem of drug resistance in patients with HIV and bacterial infections that leads from the increased risk of disease progression, to increased medical costs, prolonged hospital stays and increased mortality. Flavonoids and other phenolics are groups of natural bioactive compounds widely distributed in edible plants and are well documented to possess antiviral and antimicrobial activities. Hyptis (Lamiaceae) is known to be used in Brazilian folk medicine to treat various diseases. The aim of this study was to evaluate antibacterial and anti-HIV-1 activities of Hyptis radicans and Hyptis multibracteata and correlate these data with their phenolic compound content. Antibacterial activity was evaluated against two Gram-negative bacteria, Pseudomonas aeruginosa and Escherichia coli, and a Gram-positive Bacillus subtilis, in vitro. H. multibracteata fractions were more effective on inhibiting B. subtillis with MIC50 23.6 μg mL−1 and 12.13 μg mL−1 for hexane and ethyl acetate phases, respectively. Hexane phase also presented activity against P. aeruginosa with MIC50 of 37.55 μg mL−1. Crude extract and hydromethanol phase from H. radicans showed moderate anti-HIV-1 activity (MIC50 159 μg mL−1; MIC50 180 μg mL−1), contents of total phenolic compounds are not the main sample feature to define anti-HIV activity but there is correlation between rosmarinic acid and anti-HIV1 activity of H. radicans. There was no correlation between phenolic content and antibacterial activity of H. multibracteata, This study provides the first evidence of the anti-HIV-1 and antibacterial activity for these two species of Hyptis.

Sorocea guilleminiana Gaudich.: Wound healing activity, action mechanisms, and chemical characterization of the leaf infusion.

Sorocea guilleminina Gaudich. is a tree or shrub endemic to Brazil. Its leaves are used in Brazilian folk medicine for the healing of wounds, stomach problems, inflammation and as diuretic. The present study evaluates the activity and action mechanisms of the healing properties of the aqueous extract of S. guilleminiana leaves (AESg), in experimental models in vivo and in vitro, as well as performs a phytochemical analysis of the extract. The AESg was prepared by infusion: Ten g of dry leaves powder in 1 L hot water, soaked for 15 min, filtered, lyophilized, and stored at -30 °C. Phytochemical analyses were realized by colorimetry and HPLC/ESI/MS. Its' in vitro cytotoxicity was evaluated on fibroblastic N3T3 cells. The potential of the wound healing activity in vivo was evaluated using excision and incision wound rat models, by histopathology of the injured skin along with the determination of nitric oxide, cytokines (IL-1β, IL-10, and TNF-α), and antioxidant parameters (GSH, MPO and CAT). In vitro wound healing activity was also demonstrated in scratched N3T3 cells, by measuring the proliferation/migration rate. The phytochemical analysis of the AESg revealed a strong presence of polar compounds, especially flavonoids (4 majoritarian), as well as terpenes and/or sterols (2 majoritarian). The AESg showed no toxicity in the N3T3 cell line (IC50 > 800 μg/mL). Topical treatment with the AESg showed an increase (p < 0.05) in wound contraction with 2 mg/g cream on days 5 and 9 (43.56% and 6.70% increase, respectively), and with 50 mg/g on days 7 and 9 (10.88% and 7.91%, respectively), compared to the vehicle (non-ionic neutral cream). Topical application of AESg (2 or 50 mg/g non-ionic cream) in incised wounds caused an increase in the force necessary for the rupture of the wound when compared to the vehicle group. No changes in cytokines (IL-1β, IL-10, or TNF-α) or NO accumulation was found with up to 50 mg/g AESg treatment. For antioxidant activity on the incision wound, an increase in GSH levels was denoted with the AESg use, at the lowest and highest dose (2 and 50 mg/g) by 75.86% and 61.20% respectively, when compared to the vehicle. Also, the CAT activity was accentuated by AESg at the highest dose (50 mg/g) by 85.87%. Finally, the AESg at all doses attenuated MPO activity significantly in the incision wound by 71.35%, 73.21%, 78.08%, respectively. In the scratch test on N3T3 cells, the treatment with AESg resulted also in an increase in fibroblast proliferation/migration rate, compared to the vehicle. AESg is not cytotoxic. The results confirm the popular use of the leaf infusion of S. guilleminiana for the treatment of cutaneous wounds, possibly by stimulating the proliferation of fibroblasts with a consequent deposition of collagen, fastening rearrangement of collagen fibers, and greater transformation into myofibroblasts, essential in the healing process. Preliminary chemical analyzes of AESg revealed the presence mainly of phenolic compounds, being salicylic acid, gallic acid, pinocembrin and isoquercitrin the majoritarian ones.

Genotoxic Assessment of the Dry Decoction of Myracrodruon urundeuva Allemão (Anacardiaceae) Leaves in Somatic Cells of Drosophila melanogaster by the Comet and SMART Assays.

Medicinal plants are worldwide used as an efficient treatment of many diseases. Myracrodruon urundeuva Allemão (Anacardiaceae) is widely used Brazilian folk medicine to treat inflammations and infections of the female genital tract, conditions of the stomach and throat, and to heal wounds on the skin and mucous membranes. Several pharmacological properties of extracts and compounds isolated from M. urundeuva are found in the literature, corroborating its uses as antiulcer and gastroprotective, anti-inflammatory and analgesic, as well as antimicrobial. Despite these many uses in traditional herbal medicine, there are few reports of its toxic-genetic effect. This work aimed to investigate the genotoxic and mutagenic potential in vivo of the dry decoction of M. urundeuva leaves on somatic cells of Drosophila melanogaster, through the Comet assay and somatic mutation and recombination test (SMART). Six concentrations (0.5, 1.0, 2.0, 4.0, 8.0, and 16.0 mg/mL) were studied after feeding individuals for 24 hr in culture medium hydrated with extracts of M. urundeuva. In the Comet assay, all concentrations showed a genotoxic effect significantly higher than the negative control group, treated with distilled water. The two highest concentrations were also superior to the positive control group, treated with cyclophosphamide (1 mg/mL). In the SMART, there was a mutagenic effect at all concentrations tested, with a clear dose-dependent relationship. Both recombination and mutation account for these mutagenic effects. The set of results indicate that the dry decoction of M. urundeuva leaves is genotoxic and mutagenic for D. melanogaster under the experimental conditions of this study. Environ. Mol. Mutagen. 61:329-337, 2020. © 2019 Wiley Periodicals, Inc.

Chemical composition of essential oil from Varronia curassavica Jacq. accessions in different seasons of the year

Varronia curassavica Jacq. is a native shrub species of the Atlantic Forest and is used as a phytomedicine in Brazilian folk medicine against inflammations, ulcers and arthritis and in commercial products as an anti-inflammatory drug. In this study, for the first time, the chemical profiles of the essential oils from three accessions of V. curassavica from different geographic origins in Brazil, namely, Bahia (BA), São Paulo (SP) and Rio de Janeiro (RJ), were evaluated according to their origin and season of the year. The yield of essential oil between accessions ranged from 0.44 to 2.74% (v/w) which the highest amount was found to BA and the lowest to SP. The substances with the highest relative proportions were α-pinene (RJ – 49.2% and SP – 32.6%) and (E)-caryophyllene (SP – 16.1% and RJ – 11.1%). For BA, the substance with the highest content was amorpha-4,7(11)-diene (14.5%), followed by eudesm-7 (11)-en-4-ol (7.00%). Principal component analysis (PCA) revealed that the accession from Rio de Janeiro showed the most similarity to composition of its essential oil, whereas the accession from Bahia presented the most dissimilarity. Regardless of the differences within each population, the grouping of the samples occurred according to their origins, and no mixing occurred between the samples from the accessions. The difference in the chemical profiles found by the PCA analysis was corroborated by the hierarchical cluster analysis (HCA), which the samples from São Paulo were similar to those from Bahia, and those from Rio de Janeiro were the ones that differed most from the other accessions. Among the evaluated accessions, those from Rio de Janeiro (RJ) showed the highest content of α-humulene, with a higher production during the spring (2.89%), while SP had the highest (E)-caryophyllene content (16,12%) in all evaluated seasons, showing the potential of these accessions for cultivation of V. curassavica and consequently production of its essential oil for a phytomedicine application.

Bioguided extraction of phenolic compounds and UHPLC-ESI-Q-TOF-MS/MS characterization of extracts of Moringa oleifera leaves collected in Brazil.

Moringa oleifera leaves are used in Brazilian folk medicine for their hypoglycemic and nutritional properties. In this context, the chemical and biological characteristics were determined. Conventional successive solid-liquid extraction with simultaneous bioguided purification using solvents with different polarities was performed with M. oleifera leaves, yielding six fractions and extracts. The fractions showed better results for antioxidant activity than the extracts. All of them were evaluated by scavenging of synthetic free radicals and reactive oxygen species, and Fr-Ace and Fr-EtOAc showed >100 mg GAE g-1 of phenolic content, while for FRAP and ORAC assays the values were higher than 1600 μmol Fe2+ g-1 and 3500 mmol TEAC g-1 respectively. The UPLC-ESI-QTOF-MS analysis of hydroalcoholic extract (HE) allowed identifying 24 compounds, with flavonoid derivatives being the most abundant group. Furthermore, the alkaloid trigonelline and sesquiterpenoid abscisic acid were identified for the first time in M. oleifera leaves. Finally, gallic acid, caffeic acid, rutin and quercetin were found in concentrations of 16.5, 2129, 477.4 and 127.5 μg g-1 respectively in HE, all of which were higher in fractions and extracts. These results suggest that bioguided extraction is an important technique, due to its ability to concentrate active compounds in a logical and rational way. In addition, M. oleifera leaves grown in Brazil are an important source of phenolic compounds with antioxidant activity that can be used in food, nutraceutical and pharmaceutical products.

Bauhinia forficata link, a Brazilian medicinal plant traditionally used to treat cardiovascular disorders, exerts endothelium-dependent and independent vasorelaxation in thoracic aorta of normotensive and hypertensive rats

Ethnopharmacological relevanceBauhinia forficata Link, commonly known as “cow's paw”, is a native plant from South America. Its leaves are widely used in Brazilian folk medicine to treat diabetes and cardiovascular disorders. Although this species' biological potential has been extensively proven as an antidiabetic, anti-inflammatory and antioxidant agent, there is a lack of studies to evidence its action on the cardiovascular system.Aim of the study: This study was designed to investigate the vascular effects of B. forficata leaves preparations and its majority compound kaempferitrin, as well as its aglycone form kaempferol, in rat aortic rings of normotensive (NTR) and hypertensive (SHR) rats. Materials and methodsAorta rings from NTR and SHR precontracted with phenylephrine were exposed to cumulative concentrations of B. forficata extract, fractions (1–50 μg/mL) and compounds (0.001–0.3 μg/mL). The mechanisms involved in the vasorelaxant effect of ethyl-acetate plus butanol fraction (EAButF) were also evaluated. ResultsAlthough kaempferitrin is the most abundant compound found in both methanolic extract and EAButF, 24 minor phenolic compounds were identified in B. forficata leaves, including kaempferol. EAButF was the only with endothelium-dependent and independent vasorelaxant properties in both NTR and SHR. The incubation with L-NAME or ODQ completely blocked EAButF-induced vasorelaxation. On the other hand, the incubation with propranolol, atropine, indomethacin, glibenclamide or barium chloride did not change the vasorelaxant activity of EAButF (50 μg/mL). Nevertheless, the incubation with tetraethylammonium and 4-aminopyridine significantly influenced the EAButF activity. It was also shown that Ca2+ influx or efflux is not related to EAButF vasorelaxation potential. Kaempferitrin and kaempferol were also able to relax the rat aortic rings in 34.70% and 40.54%, respectively. ConclusionsThis study shows, for the first time, the vasorelaxant effect of EAButF from B. forficata leaves, an effect that may be attributed to the modulation of vascular tone through nitric oxide/soluble guanylate cyclase pathway, and potassium channels. The bioactive kaempferitrin and kaempferol seem to be important for the effects observed with the fraction. Finally, preparations obtained from the leaves of B. forficata may be interesting candidates for new or complementary strategies regarding cardiovascular diseases.

Evaluation of prolyl oligopeptidase and acetylcholinesterase inhibition by Phyllanthus tenellus Roxb. from Brazil

Phyllanthus tenellus Roxb. (Phyllanthaceae) is a plant used in Brazilian folk medicine for the treatment of intestinal infections and diabetes. Despite its use in traditional medicine, it was reported that P. tenellus extract may cause several effects in the central nervous system (CNS) of animals, such as agitation and signs of depression. The aim of this study was to determine the main constituents of P. tenellus methanol extract and to investigate whether the extract is able to inhibit the enzymes prolyl oligopeptidase (POP), acetylcholinesterase (AChE) and dipeptidyl peptidase-IV (DPP-IV). Corilagin (1) was isolated as the main constituent of the P. tenellus extract, along with rutin (2) and vitexin-2″-O-rhamnoside (3). The extract presented the ability to inhibit mainly POP. Dichloromethane and ethyl acetate fractions showed the highest inhibitory potency against POP (IC50 values of 1.7 ± 0.4 and 11.7 ± 2 µg/mL, respectively). All fractions were inactive against AChE. Corilagin displayed selective POP inhibition in a dose-dependent manner, with IC50= 19.7 ± 2.6 µg/mL. Corilagin exhibited moderate capacity to pass through the phospholipid membrane by passive diffusion, presenting effective permeability (Pe) of 1.26 × 10–7 cm/s.

Evaluation of genotoxicity and coumarin production in conventional and organic cultivation systems of Mikania glomerata Spreng

Mikania glomerata Sprengel, popularly known as “guaco,” is used in Brazilian folk medicine for several inflammatory and allergic conditions. Besides, the popular use “guaco” is indicated by the Brazilian Ministry of Health as a safe and effective herbal medicine. The biological activity of M. glomerata extracts is due to the presence of the coumarins, a large family of phenolic substances found in plants and is made of fused benzene and α-pyrone rings. Considering that there are few data on the biological effects of the extracts of M. glomerata, mainly in genetic level, this work aims to evaluate, in vitro, the genotoxicity and coumarin production in M. glomerata in conventional and organic growing. The data showed that the organic culture system showed double the concentration of coumarin being significantly more productive than the conventional system. Besides, the results of comet assay suggest that extracts of M. glomerata cultivated in a conventional system was genotoxic, increased DNA damage levels while the organic extracts seem to have antigenotoxic effect possibly due to the concentration of coumarins. Additional biochemical investigations are necessary to elucidate the mechanisms of action of M. glomerata extracts, which were found to have a role in protection against DNA damage.