Resumo em Inglês:

ABSTRACT Baccharis belongs to the Asteraceae family and comprises a number of medicinal species. Baccharis brevifolia DC., B. microdonta DC., B. pauciflosculosa DC., and B. trilobata A.S. Oliveira & Marchiori, which are popularly known in Brazil as “vassouras” (“broom”), are all found in Southern Brazil. The anatomical features of the leaf and stem were investigated by employing the usual light and scanning electron microtechniques, as a means of differentiating the taxa. The following anatomical characteristics can be considered to be diagnostic: the occurrence and type of stomata, midrib, stem and crystal shapes, and the presence of the petiole.

Resumo em Inglês:

ABSTRACT Chemical components act in plant defense and protection, but many of them are extracted and used medicinally. For Cerrado, active chemical components are used in the treatment of diseases, which strengthens the necessity for pharmacological studies of plants of that environment. The objective was to evaluate the histochemistry of the leaf blade of Byrsonima verbascifolia (L.) DC., Malpighiaceae, Campomanesia adamantium (Cambess.) O.Berg, Myrtaceae, Roupala montana Aubl., Proteaceae, and Solanum lycocarpum A. St.-Hil., Solanaceae, species that have been reported as producers of secondary metabolites for pharmacological use. The 3rd node leaves (median, intercostal and margin regions) were collected, fixed, included in Paraplast® or 2-hydroxyethyl methacrylate, sectioned in microtome, stained and photographed on microscope. This analysis aimed to find leaf regions which produced chemical compounds. For histochemical tests, intercostal areas were selected from median region leaf of the 3rd node. Samples fresh and newly collected and fixed and embedded in Paraplast® were used. Tests were conducted for lipids, terpenoids, phenolic compounds, alkaloids, sugars and proteins. Alkaloids were observed only in R. montana, as well as the results for phenolic compounds. Flavonoids are present in B. verbascifolia and R. montana. The lipid composition was showed for the chemical compounds of B. verbascifolia and C. adamantium, which proved to be part of the essential oils or resins oils in C. adamantium idioblasts. The chemical compounds of B. verbascifolia, C. adamantium and R. montana are present mainly in idioblasts among the parenchyma and epidermal cells. C. adamantium has secretory cavities, but only with lipid content. The identification of chemical compounds has not been possible in mature leaves of S. lycocarpum.

Resumo em Inglês:

ABSTRACT Ageratum conyzoides L., belonging to the family Asteraceae, is a tropical plant found in some regions of Africa, Asia and South America. This species is popularly known as billy goat weed, “mentrasto” and “catinga-de-bode” and has a large variety of secondary metabolites and biological activities mentioned in the literature. The objective of this work was to contribute the pharmacobotanical standardization of A. conyzoides. Cross-sections were obtained, by hand, for microscopic characterization of root, stem, petiole and leaf blade; to the leaf blade were still made paradermal and longitudinal sections, scanning electron microscopy analysis and maceration. The analysis showed that secretory structures ducts are evidenced only in the petiole and the leaf blade. The root has parenchymatous medullar region; stem, petiole and leaf blade exhibit striated cuticle. Non-glandular trichomes are present in stem, petiole and leaf blade, while capitate glandular trichomes are present only in the leaf blade and are restricted to the abaxial face. These anatomical features are useful for diagnosis of the species and provide support to their quality control.

Resumo em Inglês:

ABSTRACT Hyptis carpinifolia Benth., Lamiaceae, is a species known popularly as "rosmaninho" and "mata-pasto", and leaves are employed in Brazilian folk medicine to treat colds, flu, and rheumatism. The aim of this study was to perform a morphological description of H. carpinifolia and to evaluate the seasonal chemical variability of the leaf essential oils during 12 months. Macroscopic characterization of H. carpinifolia was carried out with the naked eye and with a stereoscopic microscope. Essential oils were isolated from leaves by hydrodistillation in Clevenger apparatus and analyzed by gas chromatography/mass spectrometry. Major compounds were found to be 1,8-cineole (39.6-61.8%), trans-cadina-1(6),4-diene (2.8-17.5%), β-caryophyllene (4.4-10.0%), prenopsan-8-ol (4.2-9.6%) and β-pinene (2.9-5.3%). Results of essential oils compositions were processed by cluster analysis and principal component analysis. Data showed high variability in the concentration of the components. Besides, there was a seasonal variability of chemical composition, probably related mainly to the rainfall regime.

Resumo em Inglês:

ABSTRACT In this study, a comprehensive phytochemical characterization of two morphologically related species from the genus Espeletia Mutis ex Bonpl., namely, Espeletia grandiflora Humb. & Bonpl. and Espeletia killipii Cuatrec., Asteraceae, has been performed by gas chromatography coupled to flame ionization detection, gas chromatography coupled to mass spectrometry and ultra-high performance liquid chromatography coupled to ultraviolet and high-resolution mass spectrometry. Analysis of ethanol extracts (70%, v/v) from leaves and concomitant compound dereplication allowed the identification of major peaks, most of them new reports for the genus Espeletia or the subtribe Espeletiinae. Chemical characterization of resins essential oils indicated several similarities and differences between both species and from other members of the subtribe. Chemometric analysis (hierarchical clustering analysis and orthogonal partial least-squares discriminant analysis) applied to the essential oil composition of 31 species from Espeletiinae furthermore allowed the identification of three primary clusters correlated with the taxonomy. Hence, this study underscored qualitative and semiquantitative differences between the chemical composition of leaves and resins of E. grandiflora and E. killipii, provided information on chemotaxonomy and described the presence of different trends in the essential oil composition from species of Espeletiinae.

Resumo em Inglês:

ABSTRACT Phytochemical investigation of the MeOH extract of Cucumis melo L. var. reticulates, Cucurbitaceae, seeds led to the isolation of a new triterpenoid: cucumol A (27-hydroxy taraxerol-3β-ol), along with three known compounds: α-spinasterol and D:B-friedoolean-5-ene-3-β-ol. Their structures were established by extensive 1D (1H, 13C, and DEPT) and 2D (1H–1H COSY, HMQC, and HMBC) NMR, as well as IR and HRESIMS spectral analyses. Compound 3 displayed cytotoxic activity against L5178Y and Hela cancer cell lines with ED50 of 1.30 and 5.40 µg/ml, respectively compared to paclitaxel (0.07 and 0.92 µg/ml, respectively).

Resumo em Inglês:

ABSTRACT Different solvent extracts of Dichotomaria obtusata (J. Ellis & Solander) Lamark, Galaxauraceae, a red algae collected from the coast of Bushehr in the Persain Gulf, was investigated for its cytotoxic properties and chemical constituents. The fresh alga, after extraction with methanol and dichloromethane were combined and partitioned between water, dichloromethane and ethyl acetate. The above fractions were then tested against MOLT-4 (human lymphoblastic leukemia) cancer cell line. The IC50 values of the dichloromethane and ethyl acetate layers of the crude extract were 29.8 ± 3.1 and 30.6 ± 7.9 µg/ml against MOLT-4 cells, respectively, while the water layer showed a week activity with IC50 > 50 µg/ml. After fractionation of the active extracts using open column chromatography over silica gel and preparative thin layer chromatography purification, two terpenoid derived compounds, trans-phytol palmitate and γ-tocopherol were isolated from the dichloromethane and ethyl acetate extracts. The structures of the compounds were elucidated using different spectral data including 1H NMR, 13C NMR, HSQC, HMBC and EI-MS. The IC50 values of compounds trans-phytol palmitate, γ-tocopherol and an undetermined mixture of compounds (F-13-14) were determined as 43.4 ± 1.6, – and 20.3 ± 6.2 µg/ml against LS180 (human colon adenocarcinoma); 53.2 ± 9.3, >100 and 27.6 ± 6.9 µg/ml against MCF-7 (human breast adenocarcinoma) and 40.0 ± 4.1, 48.8 ± 1.8 and 15.9 ± 0.3 µg/ml against MOLT-4 cell lines, respectively, which were comparable to the IC50 values of standard anticancer agent, cisplatin against the same cell lines. The red algae collected from the Persian Gulf contained substances that could inhibit the growth of human cancer cell lines and may represent a natural source for the discovery of novel anticancer agents.

Resumo em Inglês:

ABSTRACT Two new flavonoids (1 and 2), named 4',7-dihydroxy-5-hydroxymethyl-8-prenylflavonoid and 4',7-dihydroxy-5-hydroxymethyl-6,8-diprenylflavonoid, together with seven known flavonoids (3–9) were isolated from the aerial parts of Capsella bursa-pastoris (L.) Medik., Brassicaceae, for the first time. The chemical structures of the purified compounds (1–9) were identified by their spectroscopic data and references. Moreover, compounds (1–9) were evaluated for their hepatoprotective activities against D-galactosamine induced toxicity in WB-F344 cells by using a MTT colorimetric method. As a result, compounds 2, 3, 6, and 9 (10 µM) exhibited moderate hepatoprotective activities.

Resumo em Inglês:

ABSTRACT Seaweeds are related to anti-inflammatory, anti-bacterial and anti-noceptive effects. This work aimed to verify the potential of seaweed Padina gymnospora (Kützing) Sonder 1871 to improve wound healing in vitro. P. gymnospora was collected at a bethonic area in Espirito Santo. Methanolic extract of P. gymnospora was obtained by percolation. To determine cytotoxicity, colorimetric MTT tests were performed against normal fibroblasts (L929), macrophages (RAW 264.7) and human ovarian carcinoma (OVCAR-3) cell lines using concentration range of 12–110 µg ml-1. To evaluate in vitro wound healing, monolayer of fibroblasts L929 was seeded and artificial wounded. Cell proliferation was blocked by 5 µg ml-1 Mytomycin C. Nitric oxide inhibition was quantified with Raw 264.7 by Griess reaction. Minimal inhibitory concentration (MIC) against Staphylococcus aureus was determined. Eletrospray ionization with Fourier transform ion cyclotron resonance mass spectrometry (ESI-FT-ICR MS) was applied to detail composition of P. gymnospora methanolic extract. No cytotoxic effect in all cell lines was detected until the maximum concentration of 110 µg ml-1. P. gymnospora promoted significantly migration at the concentration of 25 µg ml-1 (p < 0.05). A prominent inhibition of nitric oxide formation was achieved in a concentration of 20 µg ml-1 of methanolic extract of P. gymnospora (62.06 ± 1.20%). Antibacterial activity against S. aureus could be demonstrated with MIC of 500 µg ml-1. ESI-FT-ICR MS analysis indicated eleven molecules between then, linolenic, oleic and linoleic acid. P. gymnospora favored wound repair in vitro what could be related to its fatty acid composition. In addition, its antimicrobial effect, and NO inhibition activity contribute for a new approach of P. gymnospora as a promise natural product for treatment of cutaneous wound.

Resumo em Inglês:

ABSTRACT Gout is a destructive arthritis with a high prevalence worldwide. However, the available therapy is not able to increase life quality in many patients. Campomanesia velutina (Cambess) O. Berg, Myrtaceae, is used in Brazilian folk medicine to treat pain, inflammation and rheumatism. The aim of this study was to evaluate the potential of ethanolic and aqueous extracts from C. velutina leaves to treat hyperuricemia and inflammation in gout arthritis model. Ethanolic extract of leaves and aqueous extract of leaves were in vitro assayed on xanthine oxidase inhibitory effect and in vivo on an experimental model of oxonate-induced hyperuricemia in mice, liver xanthine oxidase inhibition and monosodium urate crystal-induced paw edema model. The extracts at both tested doses (100 and 300 mg/kg) reduced serum urate levels. They were also able to inhibit xanthine oxidase in vitro and in vivo, demonstrating that this might be the mechanism of action underlying the urate-lowering effects. In addition, the extracts showed significant anti-inflammatory activity on monosodium urate crystal-induced paw edema, especially aqueous extract (100 and 300 mg/kg) that reduced edema at all evaluated times. Rutin and myricitrin were identified in ethanolic and in aqueous extracts. In this study, myricitrin was able to reduce serum uric acid levels and inhibit liver xanthine oxidase at the dose of 15 mg/kg. The anti-hyperuricemic activity of rutin has been previously reported. Thus, rutin and myricitrin seem to contribute to the observed effects of ethanolic and aqueous extracts. The results demonstrated the ability of aqueous and ethanolic extracts to lower serum urate levels and to reduce edema induced by monosodium urate crystals. Therefore, they may contribute to the management of gout in the future.

Resumo em Inglês:

ABSTRACT Among 23 extracts of medicinal and edible plants tested, Mauritia flexuosa L.f., Arecaceae, showed significant antioxidant ability (DPPH and ORAC = 1062.9 and 645.9 ± 51.4 µg TE/mg extract, respectively), while Annona montana Macfad., Annonaceae, demonstrated the most promising anti-proliferative effect (IC50 for Hep-G2 and HT-29 = 2.7 and 9.0 µg/ml, respectively). However, combinatory antioxidant/anti-proliferative effect was only detected in Oenocarpus bataua Mart., Arecaceae (DPPH = 903.8 and ORAC = 1024 µg TE/mg extract; IC50 for Hep-G2 and HT-29 at 102.6 and 38.8 µg/ml, respectively) and Inga edulis Mart., Fabaceae (DPPH = 337.0 and ORAC = 795.7 µg TE/mg extract; IC50 for Hep-G2 and HT-29 at 36.3 and 57.9 µg/ml, respectively). Phenolic content was positively correlated with antioxidant potential, however not with anti-proliferative effect. None of these extracts possessed toxicity towards normal foetal lung cells, suggesting their possible use in development of novel plant-based agents with preventive and/or therapeutic action against oxidative stress-related diseases.

Resumo em Inglês:

ABSTRACT The aim of this study was to provide scientific knowledge to support the use of Vernonia condensata Baker, Asteraceae, beverages for their alleged hypocholesterolemic properties by testing their action as HMG-CoA reductase inhibitors and their capacity to lower dietary cholesterol permeation. Chlorogenic acid, and other caffeoylquinic acids derivatives were identified as the main components of these beverages by LC–MS/MS. No changes in the composition were notice after the in vitro gastrointestinal digestion and no toxicity against Caco-2 and HepG2 cell lines was detected. Cholesterol permeation through Caco-2 monolayers was reduced in 37% in the presence of these herbal teas, and the caffeoylquinic acids permeated the monolayers in 30–40% of their initial amount in 6 h. HMG-CoA reductase activity was reduced with these beverages, showing an IC50 of 217 µg ml−1. It was concluded that caffeoylquinic acids, the major components, justified 98% of the enzyme inhibition measured.

Resumo em Inglês:

ABSTRACT The aim of this study was to investigate the effect of capsaicin and ethanolic Capsicum extracts on B104 neuroblastoma cells as a potential anticancer agent. Additionally, this study also aims to examine the influence of co-extracted bioactive compounds (vitamin E, vitamin C and quercetin) in Capsicum fruit extracts on the cytotoxic effects of capsaicin in neuroblastoma cells. MTT and LDH assays were used to determine viability and cell death in B104 neuroblastoma cells. Antioxidative properties of capsaicin, vitamin E, vitamin C and quercetin were estimated by means of cyclic and square wave voltammetry. There was a significant cytotoxicity of capsaicin (100 µmol/l) after 24 h incubation and for capsaicin (250 µmol/l), even when cells are treated for 1 h. On the other hand, ethanolic Capsicum extracts which contained capsaicin (0.5–2.1 mmol/l) did not show any cytotoxic effect. We suggest therefore, that other co-extracted compounds within the ethanolic extracts interact antagonistic with the cytotoxic effect of capsaicin and their interactions should be further investigated. Our results indicate that capsaicin in high concentration induces cytotoxic effects in a dose dependent manner, but other bioactive compounds present in Capsicum fruits prevent the cytotoxic effects of the extracts on neuroblastoma cells.

Resumo em Inglês:

ABSTRACT The essential oil from Croton polyandrus Spreng., Euphorbiaceae, leaves was tested for the toxicity and antitumor activity. The concentration producing 50% hemolysis was 141 µg/ml on mice erythrocytes. In the acute toxicological study, the estimated LD50 was 447.18 mg/kg. The essential oil did not induce increase in number of micronucleated erythrocytes, suggesting low genotoxicity. Essential oil (100 or 150 mg/kg) showed significant antitumor activity in Ehrlich ascitic carcinoma model. We observed that essential oil induces cell-cycle arrest at the G0/G1 phase, and increases the sub-G1 peak, which represents a marker of cell death by apoptosis. Survival also increased for the treated animals. The toxicological analyses revealed reduction in body weight, increased aspartate aminotransferase and alanine aminotransferase activity, hematological changes, and a thymus index reduction. These data suggest gastrointestinal and liver toxicity, anemia, leukopenia/lymphocytopenia, and immunosuppressive effects. Histopathological analysis revealed the weak hepatotoxicity of essential oil. In summary, essential oil of C. polyandrus displays in vivo antitumor activity and moderate toxicity.

Resumo em Inglês:

ABSTRACT Banara parviflora (A. Gray) Benth. is a species that belongs to Salicaceae family and is native to Southern Brazil. Fractionation of the ethanolic extract from Banara parviflora leaves afforded, a new compound identified as N 1,N 8-dibenzoylspermidinyl-N 4-acetamide, a spermidine alkaloid. The structure was elucidated by spectroscopic methods (IR, MS, 1H, 13C and 2-D NMR).

Resumo em Inglês:

ABSTRACT The standardized 80% ethanolic extract of the leaves of Ocimum basilicum var. thyrsiflorum (L.) Benth., Lamiaceae, growing in KSA, exhibited a significant antioxidant activity compared to the ethyl acetate and butanol extracts, which was correlated to its higher phenolic and flavonoid contents. Chromatographic separation of the 80% ethanol extract resulted in the isolation of ten known compounds; cinnamic acid, gallic acid, methylgallate, ellagic acid, methyl ellagic acid, apigenin, luteolin, vitexin, isovitexin, and 3"-O-acetylvitexin. Compound 3"-O-acetylvitexin, a C-glycosylated derivative of apigenin, was isolated for the first time from genus Ocimum. The 80% ethanolic extract and 3"-O-acetylvitexin showed significant cytotoxic activities against the HCT116 human colon cancer cell line [IC50 values 22.3 ± 1.1 and 16.8 ± 2.0 µg/ml (35.4 µM), respectively].

Resumo em Inglês:

ABSTRACT Piper marginatum Jacq., Piperaceae, is a widely distributed Neotropical species abundant in the Caribbean, exhibiting a characteristic winged petiole and a heart-shaped leaf, its two vegetative landmarks for rapid identification. The species has been employed by traditional indigenous cultures for its reputed medicinal properties. The plant is most frequently employed by local healers in Central America, the Antilles and South America, for alleviating gastrointestinal ailments, administered as a decoction or infusion for its tonic, diuretic and carminative effects. These beneficial properties may be attributed to the presence of various phytochemicals within P. marginatum, with most of the studies focusing on the essential oil of the plant. Monoterpenoids, sesquiterpenoids and phenylpropanoids of a varied chemical structure have been identified in the essential oil, while phenylalkanoids, aristolactams, amides and flavonoids have been purified by chromatographic techniques from the extracts. The biological and pharmacological examination of P. marginatum showed that the plant may be a valuable source of mosquitocidal, antifungal, antitumoral and hemostatic agents. Future bioguided research may yield biologically relevant molecules useful in medicine or agriculture.

Resumo em Inglês:

ABSTRACT Infectious diseases associated with antimicrobial resistance are considered to represent an important public health problem. In this regard, the mushroom Agaricus blazei Murrill contains several bioactive substances that promote significant functional properties, among them, antimicrobial activity, which has attracted the interest of the scientific community. Thus, the aim of this study was to determine whether evidence of the antimicrobial action of A. blazei has been reported in the literature. In this integrative review, manuscripts held in research databases available online were examined with a view to answering the question “Does the mushroom A. blazei exert antimicrobial activity against Gram-negative and/or Gram-positive bacteria?” Only eight scientific articles that have addressed the antimicrobial properties of A. blazei, in vitro and in vivo, were found, all characterized as pre-clinical, i.e., with level VII evidence. Most authors have found that the A. blazei extract promotes an antimicrobial effect against peritonitis, as well as deadly oral infections, especially those caused by Gram-positive bacteria. However, the scientific data currently available are not sufficient to verify the antimicrobial aspect of the mushroom A. blazei and thus further investigation is required.

Resumo em Inglês:

ABSTRACT Celosia argentea L., Amaranthaceae, is widely used as traditional medicine with a long history in China. It is a unique source of Semen Celosiae whose contributions include purging the hepatic pathogenic fire, improving eyesight, and treating other eye diseases. Over 79 compounds from this plant were isolated and identified, mainly including saponins, peptides, phenols, fatty acids, and amino acids, of which saponins have been considered as the characteristic and active constituents of Celosia argentea. Experimental evidences manifested that Celosia argentea, with its active compounds, possesses wide-reaching biological activities such as hepatoprotection, tumor treatment, anti-diarrhea, anti-diabetes, anti-oxidant, anti-hypertension, and for treatment of a number of eye diseases. The objective of the study was to provide an overview of the ethno-pharmacology, chemical constituents, pharmacology, and related clinical applications of Celosia argentea, and to reveal their therapeutic potentials, and secure an evidence base for further research works on Celosia argentea.