Resumo em Inglês:

Abstract Marantodes pumilum (Blume) Kuntze (synonym: Labisia pumila (Blume) Fern.-Vill), Primulaceae, is well known for its traditional use as a post-partum medication among women in Malaysia. Three varieties of M. pumilum, var. alata Scheff., var. pumila and var. lanceolata (Scheff.) Mez. are commonly used. Nowadays, M. pumilum powder or extracts are commercially available as herbal supplements and beverages. Authentication of the variety is an important component of product quality control. Thus, the present work was aimed to compare the three varieties using microscopic, spectroscopic and chromatographic techniques. Microscopic anatomical examination and powder microscopy were performed on fresh and dried plant materials, respectively. Fingerprint profiles of the varieties were obtained using attenuated total reflectance-Fourier transform infrared spectrophotometer, high performance thin layer chromatography and high performance liquid chromatography. The microscopic examination showed presence of anisocytic stomata, scale and capitate glandular trichome in all varieties. The type of stomata and trichomes, outline structure of stem and leaf margin, petiole and midrib, organization of vascular system, areolar venation, pattern of anticlinal walls, the distribution of secretory canals and cell inclusion as well as the measurement of selected structures could be used to distinguish and identify each variety of M. pumilum. In addition, spectroscopic and chromatographic fingerprint analyses of the three varieties exhibited distinguishable profiles based on the intensity of certain peaks or bands. The findings from this study will provide systematic identification for these varieties.

Resumo em Inglês:

Abstract Amphilophium crucigerum (L.) L.G. Lohmann, known as “pente-de-macaco” is a species of Bignoniaceae native to Brazil, and whose seeds are used in folk medicine. This study aimed to describe morphoanatomical features of this species of fruit to aid in its correct identification and pharmacognostic analysis. Samples of ovary, pericarp and seed were fixed with 3% glutaraldehyde, sectioned on a rotary microtome and analyzed by stereomicroscope. The results are shown in three parts: (1) The ovary presents peltate trichomes, long non-glandular trichomes and emergences in the epidermis; it is 2-carpellate and unilocular with two intruding parietal placenta; ovules are numerous on the placenta; it presents a large quantity of crystals. (2) The pericarp is woody, densely echinate and elliptic shape; it presents a 2-valved capsule and is septicidal; it presents emergences, stomata, lenticels, crystals and a large quantity of clustered stones cells. (3) Seeds are alate, exalbuminate and exotestal; there is a large amount of crystals in the exotestal region; it presents an endothelium and remnant endosperm. Histochemical tests showed the presence of lipophilic substances, polysaccharides, phenolic substances, alkaloids and a small quantity of starch. These pharmacobotanical features described for A. crucigerum are essential for the pharmacognostic analysis of the drug plant.

Resumo em Inglês:

Abstract Hortia oreadica Groppo, Kallunki & Pirani, Rutaceae, known as “para-tudo”, “quina”, and “quina-do-campo”, is used in traditional medicine locally to treat stomach pain and fevers. The aims of this study were: analyze the chemical composition of essential oils from leaves, flowers and fruits of H. oreadica and verify the seasonal variation of the chemical components of essential oils from leaves. The essential oils were obtained by hydrodistillation using a Clevenger type apparatus and analyzed by GC/MS. The major components found in the samples of the essential oils were the amorpha-4,7(11)-diene (29.27% – flowers, 20.26% – fruits, 27.66–37.89% – leaves), bicyclogermacrene (23.28% – flowers, 20.64% – fruits, 14.71% to 31.37% – leaves). This work represents the first study of the chemical composition of essential oils from leaves, flowers and fruits and seasonal variation in the essential oils from leaves of H. oreadica.

Resumo em Inglês:

Abstract In the course of our ongoing effort to identify bioactive compounds from marine-derived fungi, the marine fungus, Penicillium species was isolated from the Red Sea tunicate, Didemnum species. Two new cerebrosides, penicillosides A and B were isolated from the marine-derived fungus, Penicillium species using different chromatographic methods. Their structures were established by different spectroscopic data including 1D (1H NMR and 13C NMR) and 2D NMR (COSY, HSQC, and HMBC) studies as well as high-resolution mass spectral data. Penicilloside A displayed antifungal activity against Candida albicans while penicilloside B illustrated antibacterial activities against Staphylococcus aureus and Escherichia coli in the agar diffusion assay. Additionally, both compounds showed weak activity against HeLa cells.

Resumo em Inglês:

Abstract This study investigated the effects of the flavonoids 5-hydroxy-7,4′-dimethoxyflavone, casticin, and penduletin, isolated from Croton betulaster Müll Arg., Euphorbiaceae, a plant utilized in popular medicine in Brazil, on the growth and viability of the human glioblastoma cell line GL-15. We observed that 5-hydroxy-7,4′-dimethoxyflavone and casticin were not toxic to GL-15 cells after 24 h of exposure. However, casticin and penduletin inhibited the metabolic activity of glioblastoma cells significantly at a concentration of 10 µM (p ≤ 0.05). Flavonoids casticin and penduletin also induced a significant and dose-dependent growth inhibition beginning at 24 h of exposure, and the most potent flavonoid was penduletin. It was also observed that penduletin and casticin induced an enlargement of the cell body and a reduction of cellular processes, accompanied by changes in the pattern of expression of the cytoskeletal protein vimentin. Signs of apoptosis, such as the externalization of membrane phosphatidyl serine residues, nuclear condensation, and fragmentation, were also detected in cells treated with 50–100 µM flavonoids. Our results indicate that flavonoids extracted from C. betulaster present antitumoral activity to glioblastoma cells, with penduletin proving to be the most potent of the tested flavonoids. Our results also suggest that these molecules may be promising supplementary drugs for glioblastoma treatment.

Resumo em Inglês:

Abstract Some species of the Clusia genus have been shown to have important biomedical properties, including the ability to inhibit tumor growth in vitro and the usefulness for skin care. In this study, we examined the cytotoxic effect of hexane, ethyl acetate and methanol extracts from Clusia latipes Planch. & Triana, Clusiaceae, leaves on survival of human prostate cancer cells (PC-3), colon cancer cells (RKO), astrocytoma cells (D-384), and breast cancer cells (MCF-7). The ethyl acetate extract displayed the most substantial cytotoxic effect. However, using a Comet assay, we observed that the hexane extract induced a genotoxic effect (DNA damage) on human lymphocytes in an in vitro model. Chromatographic purification of the C. latipes hexane extract led to the isolation and identification of friedelin, friedolan-3-ol, and hesperidin as active cytotoxic compounds in hexane extract, while β-amyrine was identified as an active cytotoxic compound in the ethyl acetate extract of C. latipes, thereby supporting further studies of the molecular mechanisms underlying the effect of these secondary metabolites on cancer cell survival.

Resumo em Inglês:

Abstract The ferulic and gallic acid related compounds from natural origin were studied against xanthine oxidase and cyclooxygenase-2 along with their anti-inflammatory activity. The compounds gallic acid, ferulic acid, caffeic acid and p-coumaric acid revealed promising anti-inflammatory activity (30–40% TNF-α and 60–75% IL-6 inhibitory activity at 10 µM). Bioavailability of compounds were checked by in vitro cytotoxicity using CCK-8 cell lines and confirmed to be nontoxic, but found toxic at higher concentration (50 µM). Gallic, ferulic, caffeic acid was demonstrated potential dual inhibition toward xanthine oxidase and cyclooxygenase-2 as calculated by IC50: 68, 70.2, and 65 µg/ml (xanthine oxidase) and 68.5, 65.2, and 62.5 µg/ml (cyclooxygenase-2), respectively. The structure activity relationship and in silico drug relevant properties (HBD, HBA, PSA, c Log P, ionization potential, molecular weight, EHOMO and ELUMO) further confirmed that the compounds were potential candidates for future drug discovery study, which was expected for further rational drug design against xanthine oxidase and cyclooxygenase.

Resumo em Inglês:

Abstract The essential oil of Chenopodium ambrosioides L., Amaranthaceae, was obtained by steam distillation in a Clevenger apparatus and characterization was performed using chromatographic and spectroscopic assays (GC-FID, GC/MS, 1H NMR). Two major compounds were identified: p-cymene (42.32%) and ascaridole (49.77%). The ethanolic extract and hydrolate were fractionated by liquid–liquid partitioning and the compounds were characterized by GC/MS. The essential oil, ethanol extract and fractions by partitioning with dicloromethane, ethyl acetate and butanol were tested in tumor cell lines (K562, NALM6, B15, and RAJI). Significant cytotoxic activity was found for essential oil (IC50 = 1.0 µg/ml) for RAJI cells and fraction dicloromethane (IC50 = 34.0 µg/ml) and ethanol extract (IC50 = 47.0 µg/ml) for K562 cells. The activity of the essential oil of C. ambrosioides is probably related to the large amount of ascaridol, since the other major compound, p-cymene, is recognized as a potent anti-inflammatory and has low cytotoxic activity.

Resumo em Inglês:

Abstract Echinochloa crus-galli (L.) P. Beauv., Poaceae, grains are used as a feed for birds and millet for humans. The sulforhodamine B assay was used to assess its cytotoxicity against four human cancer cell lines. The ethanolic extract (70%) proved to be most active against HCT-116 and HELA cell lines (IC50 = 11.2 ± 0.11 and 12.0 ± 0.11 µg/ml, respectively). On the other hand, the chloroform and ethyl acetate fractions exhibited their highest activities against HCT-116 cell lines. The chloroform and ethyl acetate fractions were subjected to several chromatographic separations to render pure phenolic compounds (1-8). Compounds 1-8 were identified as: 5,7-dihydroxy-3′,4′,5′-trimethoxy flavone, 5,7,4′-trihydroxy-3′,5′-dimethoxy flavone (tricin), quercetin, flavone, apigenin-8-C-sophoroside, 2-methoxy-4-hydroxy cinnamic acid, p-coumaric acid and quercetin-3-O-glucoside. All the isolated phenolic compounds exhibited various significant activities against the four human carcinoma where the methoxylated flavones (1 and 2) were the most active, in a way comparable to the anticancer drug Doxorubicin®. Thus, these methoxylated flavonoids may be considered as lead compounds for the treatment of cancer, which supports previous claims of E. crus-galli traditional use. This is the first report of the occurrence of these phenolic compounds in E. crus-galli.

Resumo em Inglês:

Abstract Aleurites moluccanus L. (Willd.), Euphorbiaceae, is a tree that is native to Indonesia and India. Various parts of this tree are commonly used in traditional medicine to treat pain, fever, inflammation, hepatitis, gastric ulcer and other ailments. An oral suspension containing dried extract of A. moluccanus was developed and in vivo anti-inflammatory activity was evaluated. Extract 100 and 50 mg/ml loaded oral suspensions were prepared using different suspending agents. The formulations were analysed by their appearance, pH, density, redispersion time, rate of settling, rheological behaviour, distribution of particle size and zeta potential. The dose uniformity was determined by measuring the content of total phenolic compounds expressed in swertisin by a validated HPLC method, as well as the dissolution profile. The stability of oral suspensions was analysed in accelerated studies (40 °C for 6 months). The anti-inflammatory activity was analysed using an in vivo paw oedema model. The taste and odour of the suspensions were shown to be characteristic of the extract. Carmellose sodium (CS; 0.5%) and microcrystalline cellulose and carmellose sodium mixture (MCCS; 1%) showed better physical behaviour. The content of total phenolic compounds was 1.6 mg/ml and approximately 100% of the total phenolic compounds dissolved within 10 min. During the stability study, the formulations were approved by their physical–chemical properties and were shown to lose 12–14% of total phenolic compounds at 40 °C after 6 months. Suspensions containing 50 mg/ml of standardised dried extract inhibited around 35 ± 7.6% of paw oedema. Formulations containing CS showed more anti-inflammatory activity. Suspensions containing dry extract of A. moluccanus were successfully obtained and showed physical and physical–chemistry properties that were appropriate and characteristic of this dosage form, suitable for administration in paediatric and elderly populations, making this an alternative to tablets.

Resumo em Inglês:

Abstract The “bacuri” (Platonia insignis Mart., Clusiaceae) is a native tropical fruit from the Brazilian Amazon and Northeast Regions. Its seeds are used to treat inflammatory diseases, diarrhea and skin problems in traditional medical practices. Regarding its widespread medicinal uses, it is important to evaluate the biological and toxicological potential of this species. This way, the aim of this study was to investigate the in vitro cytotoxic and immunomodulatory effects of the hexanic extract of P. insignis seeds, as well as its in vivo acute oral toxicity. The biological evaluation was performed by the determination of cytotoxic (MTT and hemolysis assay) and immunomodulatory (phagocytic capacity, lysosomal volume and nitrite production) activities of EHSB in murine peritoneal macrophages. In addition, the oral acute toxicity was evaluated using female Wistar rats treated with EHSB (2.0 g/kg), in accordance with the OECD 423 Guideline. The EHSB showed low toxicity for macrophages in the MTT test (CC50 value: 90.03 µg/ml), as well as for erythrocytes, which caused only 2.5% hemolysis at the highest concentration. A strong immunomodulatory activity was observed by a markedly increase of the NO production, phagocytic ability and lysosomal volume. On the other hand, it was not observed deaths or changes in the clinical and behavioral parameters in the toxicological evaluation. This manner, the present study contributes to the knowledge about the immunomodulatory and toxicological properties of the P. insignis. This may provide perspectives for the evaluation and development of effective and safe phytomedicines created from the Brazilian local biodiversity.

Resumo em Inglês:

Abstract The aim of the present study was to assess the activity of the hazelnut oil in the treatment of polycystic ovary syndrome in rats. Serum follicle-stimulating hormone, luteinizing hormone, estradiol, progesterone, testosterone, serum lipid parameters, leptin and glucose levels were evaluated. Moreover, antioxidant activity was tested using superoxide dismutase, malondialdehyde, catalase, glutathione peroxidase levels. The phytosterol content of the oil was determined by HPLC. The plasma high density lipoprotein-cholesterol level was found to be significantly high and leptin and glucose concentrations were found to be significantly low in the treatment group. According to the phytochemical analysis, the main components of the oil were detected as α-tocopherol, γ-tocopherol, squalene, β-sitosterol, campesterol and stigmasterol. Corylus avellana oil was found to be effective in the treatment of polycystic ovary syndrome via regulating gonadotropins, steroids and serum lipid parameters and possesses antioxidant activity.

Resumo em Inglês:

Abstract The hypolipidemic activity of friedelin isolated from Azima tetracantha Lam., Salvadoraceae, was studied in Triton WR-1339 and high-fat diet-induced hyperlipidemic rats. In Triton WR-1339 induced hyperlipidemic rats, treatment with friedelin (50 and 70 mg/kg) showed a significant (p < 0.01) lipid-lowering effect as assessed by reversal of plasma levels of total cholesterol (TC), triacylglycerides (TG), high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C). In high-fat diet fed hyperlipidemic rats, treatment with friedelin (50 and 70 mg/kg) caused lowering of lipid levels in plasma and liver. The hypolipidemic activity of friedelin was compared with fenofibrate, a known lipid-lowering drug, in both models.

Resumo em Inglês:

Abstract Prior studies demonstrate that a proteinase fraction from Vasconcellea cundinamarcensis V.M. Badillo, Caricaceae, exhibits wound healing activity in gastric and cutaneous models and antitumoral/antimetastatic effects. Here, we present the toxicity, pharmacokinetics and biodistribution data for this proteinase fraction following a single dose into Swiss mice by i.v., s.c. or p.o. routes. The i.v. and s.c. toxicity assays demonstrate that proteinase fraction at ≤20 mg/kg is non-lethal after single injection, while parental administration (p.o.) of ≤300 mg/kg does not cause death. Based on p.o. acute toxicity dose using Organisation for Economic Cooperation and Development protocols, proteinase fraction ranks as Class IV “harmful” substance. Proteinase fraction shows high uptake determined as Kp (distribution tissue/blood) in organs linked to metabolism and excretion. Also, high bioavailability (≈100%) was observed by s.c. administration. The blood contents following i.v. dose fits into a pharmacokinetic bi-compartmental model, consisting of high removal constants – kel 0.22 h−1 and kd 2.32 h−1and a half-life – t½ = 3.13 h. The Ames test of proteinase fraction (0.01–1%) demonstrates absence of mutagenic activity. Likewise, genotoxic evaluation of proteinase fraction (5 or 10 mg/kg, i.p.) shows no influence in micronuclei frequency. In conclusion, the acute doses for proteinase fraction lack mutagenic and genotoxic activity, clearing the way for clinical assays.

Resumo em Inglês:

Abstract Lavandula officinalis Chaix, Lamiaceae, extracts can inhibit inflammation and also pain induced by formalin in mice. This study evaluated the effects of L. officinalis hydro-alcoholic extract on pain induced by formalin and also cyclooxygenase (COX) type 1 and 2 activity in mice. To evaluate probable analgesic and anti-inflammatory effects of the extract, flowers were prepared by maceration and extraction in alcohol and their analgesic effects were studied in male mice, using formalin and hot plate tests. The effect of intraperitoneal hydro-alcoholic extracts of L. officinalis (100, 200, 250, 300, 400 and 800 mg/kg), subcutaneous morphine (10 mg/kg), dexamethasone (10 mg/kg; i.p.) and indomethacin (10 mg/kg; i.p.) on formalin induced pain were studied. Our results indicated that administration of the extract (100, 200, 250, 300, 400 and 800 mg/kg; i.p.) has inhibitory effects on inflammation induced by formalin injection into the animals hind paw. Moreover, this inhibitory effect was equal to the effects of morphine, dexamethasone and indomethacin. The extract in100, 200 and 300 mg/kg; significantly reduced heat-induced pain. The extract also reduced COX activity in dose dependent manner, where the inhibitory effect on COX1 activity was 33% and on COX2 activity was 45%. Here for the first time we show that L. officinialis extract can modulate pain and inflammation induced by formalin by inhibition of COX enzymes.

Resumo em Inglês:

Abstract Medicinal plants are treating and preventing various diseases. There is urgency in recording such data. This is first ethno botanical study in which statistical calculations about plants are done by Informant Consensus Factor method in the study area. The aim of the present study is to identify plants collected for medicinal purposes by the traditional healers of Kudavasal taluk located in Thiruvarur district of Tamil Nadu, India and to document prepare and use the traditional names of these plants. Field study was carried out for a period of one year in (tk), located in Thiruvarur district of Tamil Nadu. The ethnoveterinary information's were collected through interviews among traditional healers. The collected data were analyzed through RFC, UV, CI, FI, RI and ICF. A total of 54 species of plants distributed in 51 genera belonging to 33 families were identified as commonly used ethno medicinal plants by traditional healers in Kudavasal (tk) for the treatment of 12 ailment categories based on the animal body systems treated. Leaves are the most frequently used plant parts and most of the medicines are prepared in the form of paste, administrated orally and inhalation. The most important species according to their use value are Oryza sativa (0.977). In these studies some of the plant species are first position in relative importance Datura metel (2.00) followed by Azadirachta indica (1.80). ICF values of the present study indicate that a urological ailment is the highest use report. In this study, documenting the medicinal plants and associated indigenous knowledge can be used for conservation and sustainable use of medicinal plants in the area and for validation of these plant preparations for veterinary treatment. The study has various socioeconomic dimensions associated with the local communities.

Resumo em Inglês:

Abstract Chitosan is largely known for its activity against a wide range of microorganisms, in which the most acceptable antimicrobial mechanism is found to include the presence of charged groups in the polymer backbone and their ionic interactions with bacteria wall constituents. This interaction suggests the occurrence of a hydrolysis of the peptidoglycans in the microorganism wall, provoking the leakage of intracellular electrolytes, leading the microorganism to death. The charges present in chitosan chains are generated by protonation of amino groups when in acid medium or they may be introduced via structural modification. This latter can be achieved by a methylation reaction resulting in a quaternized derivative with a higher polymeric charge density. Since the charges in this derivative are permanents, it is expected a most efficient antimicrobial activity. Hence, in the present study, commercial chitosan underwent quaternization processes and both (mother polymer and derivative) were evaluated, in gel form, against Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative), as model bacteria. The results, as acquired from turbidity measurements, differ between materials with an expressive reduction on the Gram-positive microorganism (S. aureus) growth, while E. coli (Gram-negative) strain was less sensitive to both polymers. Additionally, the antibacterial effectiveness of chitosan was strongly dependent on the concentration, what is discussed in terms of spatial polymer conformation.

Resumo em Inglês:

Abstract Spilanthol (C14H23NO, 221.339 g/mol) is a bioactive compound that is found in many different plants that are used as traditional remedies throughout the world. It is present in Heliopsis longipes and several species in the genus Acmella, including A. oleracea L., also known as paracress and jambu. Its leaves and flowers have sensory properties (pungency, tingling, numbing, mouth-watering) that make it a popular spice and ingredient in several Brazilian dishes. Spilanthol can exert a variety of biological and pharmacological effects including analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial, antilarvicidal and insecticidal activities. So, the aim of this review is to present a literature review on the spilanthol that describes its occurrence, chemistry, extraction and biological activities.