Resumo em Inglês:

Ajisamat, an herb commonly used as an aphrodisiac in the Malaysian traditional medicine, corresponds to two different species from different families - Salacia macrophylla Blume, Celastraceae, and Prismatomeris glabra (Korth.) Valeton, Rubiaceae. Macromorphological inspection of the vegetative parts both plants reveals only a slight difference in the arrangement of the petioles. Microscopic investigation of the plants roots used as crude drugs revealed however distinctive anatomical features. Prismatic calcium oxalate crystals and banded paratracheal parenchyma are characteristics of S. macrophylla while P. glabradisplays an abundance as crystals. Other features such as vessels diameters and arrangements are also of diagnostic importance. Some of these characters were also identified in the powder of thes e plant materials and proposed for diagnostic purpose. The values for extraction of ethanol and water as well as total ash, acid-insoluble ash, water-soluble ash and sulfated ash were determined for both plants. Phytochemical studies were carried out on hexane and chloroform extracts of S. macrophylla and methanolic extract of P. glabra. S. macrophylla was shown to contain highly oxidized pentacyclic triterpenes while P. glabra contains anthraquinones. The pharmacognostical and hytochemical information can be utilised as the identification tools for Salacia macrophylla and Prismatomeris glabra

Resumo em Inglês:

The present study evaluated the chemical profile of polar extracts of Calendula officinalis L., Asteraceae, that were grown under different cultivation conditions: chemical fertilisation, organic fertilisation and mulching. Furthermore, we investigated metabolite variations during plant development by comparing the metabolites from harvested plants at 60 and 120 days after planting. We used HPLC-DAD-MS/MS to tentatively identify metabolites. In total, we identified seven known compounds: five flavonoid glycosides and two caffeoylquinic acids derivatives. There were no statistically significant differences in the expression of metabolites from plants grown under the examined soil treatments. However, five substances varied according to harvest time, suggesting that the biosynthesis of polar metabolites of Calendula officinalis is not affected by changes in soil composition. Therefore, this plant could represent a source for phytomedicines with a constant content of polar metabolites.

Resumo em Inglês:

Acanthospermum hispidum DC., Asteraceae, is widely used in folk medicine in Brazil to treat respiratory diseases; this biological property has been attributed to its phytosterol content. This study evaluated the spectrophotometric assay method to quantify the total phytosterol content in raw materials and extracts from roots of A. hispidum. The procedure was based on the quantification at 625 nm after the Liebermann-Burchard reaction. The method was evaluated for linearity, repeatability, intermediate precision, accuracy and robustness. The date indicated that the procedure is a valid analytical tool for materials and herbal derivatives from A. hispidum.

Resumo em Inglês:

Piper aduncum L., Piperaceae, stands out due to its biological activities, however, it is still found in the wild and little is known about its agronomic point of view. The aim of this study was to evaluate the growth and to analyze the chemical composition of essential oils from leaves of P. aduncum collected in two different sites of Cerrado as well as in cultivated plants. The cultivation was installed out in a greenhouse using cuttings of adult specimens. Essential oils were obtained from fresh leaves. Plants from the two studied locations showed erect growth habit and behavior of linear growth. The essential oils composition of P. aduncum from Bocaiuva did not differ between wild and cultivated plants, as the major substance identified as 1,8-cineole. The plants from Montes Claros site showed a distinct concentration for the two samples, being the major substance characterized as transocimene (13.4%) for wild and 1,8-cineole (31.3%) for cultivated plants. Samples from both locations showed a similar essential oil composition in cultivars. Our results showed that P. aduncum cultivation is feasible and the variation in chemical composition of the two sites may indicate an environmental influence, since chemical and isoenzyme analysis did not show great differences.

Resumo em Inglês:

Pentacyclic triterpene Natural product Cytokine modulation Anti-inflammatory activity Dendritic cells Pentacyclic triterpenes are a large family of plant metabolites that exhibit a wide array of biological activities. The genus Cecropia,which encompasses many plant species, has been used as traditional medicine for the treatment of inflammatory diseases and is known to produce many active pentacyclic triterpenes. In this study we investigated the chemical composition of a pentacyclic triterpene fraction from the roots of Cecropia telenitida Cuatrec., Urticaceae. A novel compound, which we termed yarumic acid, and four known molecules (serjanic acid, spergulagenic acid A, 20-hydroxy-ursolic acid and goreishic acid I) were isolated and characterised. In a dendritic cell (DC)based assay, we demonstrated that non-toxic doses of these pentacyclic triterpenes inhibited the secretion of at least one of the proinflammatory cytokines tested (IL-1β, IL-12p40, IL-12p70, TNF-α). Spergulagenic acid A also inhibited nitric oxide production in lipopolysaccharide-stimulated dendritic cell. Serjanic acid and spergulagenic acid A, which were the most potent abundant compounds in the pentacyclic triterpene fraction, showed the most activity in the dendritic cell-based assay. These results show that all pentacyclic triterpenes might contribute to the anti-inflammatory activities of C. telenitida. Moreover, yarumic acid as well as the four known pentacyclic triterpenes, can be exploited as potential immunomodulatory/anti-inflammatory agents.

Resumo em Inglês:

We analyzed the effect of the combination of citral, eugenol and thymol, respectively the main constituents of essential oils of Cympobogon citratus (DC) Stapf, Poaceae (lemon grass), Syzygium aromaticum (L.) Merr. & L.M. Perry, Myrtaceae (clove) and Thymus vulgaris L., Lamiaceae (thyme), on the proliferation of the trypanosomatids Crithidia fasciculata and Trypanosoma cruzi. The constituents were initially added individually at different concentrations to C. fasciculata cultures to estimate the IC50/24h. Concentrations in a triple combination were about 2 times and 16.5 times lower against C. fasciculata and T. cruzi, respectively, as compared to isolated compounds. Incubation of C. fasciculata with the trypanocydal agent benznidazole did not affect parasite growth at concentrations up to 500 µg/ml, but the IC50 of this drug against T. cruziwas 15.8 µg/ml, a value about 2-5 times higher than that of constituents in the triple combination. Analysis of treated C. fasciculata by scanning electron microscopy showed rounding of the cell body. Our data show that combination of essential oil constituents resulted in increased inhibitory activity on growth of both non-pathogenic and pathogenic trypanosomatid species and indicate that the non-patogenic C. fasciculata may represent a resistant model for drug screening in trypanosomatids.

Resumo em Inglês:

Vasorelaxant activity Vasorelaxant effects of eight diterpenoids isolated from three Venezuelan plants [(+)-manool [(+)-labda-8(17),14-dien-13-ol], (+)-manoyl oxide, (+)-2-oxomanoyl oxide, sandaracopimara-8(14), 15-dien-3β, 19-diol, jhanidiol acetate (18-acetoxy-1βhydroxymanoyl oxide), jhanidiol (1β,18-dihydroxymanoyl oxide),ent-kaur-16-en-19ol and grandiflorenic acid (ent-kaur-9(11),16-dien-19-oic acid)] aortic rings were assessed in intact endothelium and endothelium-denuded isolated rat. Thw cumulative addition (10-6 to 10-4 M) of each product were carried out after contraction with phenylephrine (10-6 M). Jhanidiol acetate and ent-kaur-9,16-en-19-oic acid at 10-4 M dose concentration, exhibit the maximal vasorelaxant effect in endothelium-intact rings (51.61 ± 7.62% and 79.27 ± 7.41%, respectively). In endothelium-denuded aortic rings, the maximum vascular response exerted by both compounds was not abolished (64.14 ± 5.64% and 84.84 ± 3.62%, respectively). In denuded aortic rings, the half-maximal inhibitory concentration (IC50) Jhanidiol was obtained by the ethyl less than those obtained in rings endothelium (1.09 × 10-4 vs 7.29 × 10-5 M, respectively), although this difference was not significant. These results suggested that the mechanism behind the vasorelaxant effect of the two diterpene is mediated by endothelium-independent pathways.

Resumo em Inglês:

Mulberry leaves Flavones Pharmacokinetics Metabolites Rutin Quercetin Mulberry leaves, a traditional Chinese medicine, are effective in the treatment of diabetes mellitus. Rutin and quercetin are the main components of total flavones of mulberry leaf extract. To study the pharmacokinetics of rutin and quercetin in rat plasma and their metabolites in rat urine and feces after oral administration of total flavones of mulberry leaf extract. At different timepoints after oral administration of total flavones of mulberry leaf extract in rats, plasma concentrations of rutin and quercetin were determined by RP-HPLC. The main pharmacokinetic parameters were estimated using 3P97 software. The metabolites in rat urine and feces were determined by using UPLCESI-QTOF/MS and estimated MetaboLynxTM software. The plasma concentration-time curves of rutin and quercetin both were best fitted with a two-compartment model. Rutin and quercetin were absorbed rapidly and then slowly decreased. Two prototype compounds and seven metabolites were identified. The pharmacokinetic and metabolic results may be useful for further studies of the bioactive mechanism of mulberry leaf flavones and potential development of a new TCM.

Resumo em Inglês:

Anti-proliferative properties have been reported for certain species of the genus Artemisia. In this study, we investigated the cytotoxic and apoptotic effects of n-hexane, CH2Cl2, EtOAc, n-BuOH and H2O fractions obtained from a crude methanol extract of A. armeniaca on two myeloid cell lines, apoptosis-proficient HL60 cells and apoptosis-resistant K562 cells; in addition, J774 cells were used as a control. Among the solvent fractions of A. armeniaca, the CH2Cl2 fraction was found to have the largest anti-proliferative effect on cancer cells. The IC50 values obtained using an MTS assay for the CH2Cl2 fraction were 75 and 130 µg/ml for HL-60 cells and K562, respectively. The control cells were not significantly affected by this fraction. A flow cytometry histogram of cells treated with the CH2Cl2 fraction of A. armeniaca revealed a sub-G1 peak. DNA fragmentation, increased protein levels of Bax and cleavage of the poly (ADP-ribose) polymerase (PARP) protein confirmed the induction of apoptosis in cells after a 48-h exposure to the CH2Cl2 fraction. Our results corroborate the cytotoxic and apoptotic effects of the CH2Cl2 fraction of A. armeniaca on K562 and HL-60 cancer cell lines.

Resumo em Inglês:

Ischemic stroke is characterised by a lack of oxygen and glucose in the brain, leading to excessive glutamate release and neuronal cell death. Adenosine is produced in response to ATP depletion and acts as an endogenous neuromodulator that reduces excitotoxicity. Persea major (Meins.) L.E. Kopp (Lauraceae) is a medical plant that is indigenous to South Brazil, and the rural population has used it medicinally due to its anti-inflammatory properties. The aim of this study was to evaluate the neuroprotective effect of Persea major methanolic extract against oxygen and glucose deprivation and re-oxygenation as well as to determine its underlying mechanism of action in hippocampal brain slices. Persea major methanolic extract (0.5 mg/ml) has a neuroprotective effect on hippocampal slices when added before or during 15 min of oxygen and glucose deprivation or 2 h of re-oxygenation. Hippocampal slices subjected to oxygen and glucose deprivation and re-oxygenation showed significantly reduced glutamate uptake, and the addition of Persea major methanolic extract in the re-oxygenation period counteracted the reduction of glutamate uptake. The presence of A1 or A2A, but not A2B or A3 receptor antagonists, abolished the neuroprotective effect of Persea major methanolic extract. In conclusion, the neuroprotective effect of Persea major methanolic extract involves augmentation of glutamate uptake and modulation of A1 and A2B adenosine receptors.

Resumo em Inglês:

Gestational depression is detrimental to the health of the mother and the offspring and contributes to the appearance of depressive and anxiety symptoms during the postnatal period. Traditional antidepressants have undesirable side effects when utilised during gestation, but Hypericum perforatum has been characterised as an efficient and safe antidepressant that prevents the recurrence of symptoms. This study verified the effects of Hypericum perforatum on the behaviour of Wistar rats that were treated during gestation and evaluated 10 and 60 days post-treatment. Pregnant Wistar rats were divided into four groups of ten animals each: one control group that received distilled water and three treatment groups that were treated orally with 36, 72 or 144 mg/kg Hypericum perforatum extract. At 10 and 60 days after parturition and post-treatment, the rats were submitted to the holeboard, the tail suspension, and the forced swim tests. The animals treated with 144 mg/kg Hypericum perforatum exhibited greater head-dipping activity in the hole-board test and reduced immobility in the tail suspension and forced swim tests, suggesting less anxiety and depression 10 and 60 days post-treatment.The results indicated that treating rats with Hypericum perforatum during the gestational period decreased depressive behaviour and anxiety 10 and 60 days post-treatment.

Resumo em Inglês:

Adiantum capillus-veneris L., Pteridaceae, is a fern reputed to have numerous applications in traditional medicine in the treatment of leprosy, animal bites, thyroid dysfunction and musculoskeletal disorder.The proposed study was aimed to investigate the potency of the fern Adiantum capillus-veneris on the thyroid dysfunction - hypothyroidism in terms of determining thyroid gland weight, thyroid peroxidase activity, estimation of iodine in urine, concentrations of total thyroxine (T4), triiodothyronine (T3) and thyroid stimulating hormone (TSH) in serum. The weight of thyroid gland was decreased, while thyroid peroxidase activity, serum T4 (p < 0.01) and serum T3 levels (p < 0.01) were increased in animals treated with the ethanol plant extract (500 mg/kg); but serum TSH level decreased significantly (p < 0.01) when compared with hypothyroid control animals. The SOD, Catalase and glutathione antioxidant enzyme levels and lipid peroxidation were measured.The results of lipid peroxidation and antioxidant enzyme assay indicated that the level of malondialdehyde was significantly lowered and the levels of antioxidant enzymes were significantly increased when treated with ethanol extract of Adiantum capillus(500 mg/kg). Polyphenolic compounds viz., quercetin and gallic acid were determined by HPTLC analysis. With the outlined results, Adiantum capillus could be used for the regulation of hypothyroidism.

Resumo em Inglês:

The present study reports the anti-allergic activity of ethanolic extract of Zizyphus jujuba Mill., Rhamnaceae, and its possible mode of action. The effect of extract of Z. jujuba at different doses (250, 500 and 1000 mg/kg, orally) was simulated on studied animal models of asthma and allergy: a) milk induced eosinophilia and leukocytosis; b) compound 48/80 induced mast cell degranulation; and, c) active and passive cutaneous anaphylaxis. In addition, extract of Z. jujuba's effect on sensitized guinea pig ileum (ex vivo) and tracheal chain preparations (in vitro) were investigated.Treatment with extract of Z. jujuba at all doses significantly: prevented the milk-induced eosinophilia and compound 48/80 induced degranulation of mesenteric mast cells; decreased passive cutaneous and active anaphylactic reactions. In addition, extract of Z. jujuba inhibited acetylcholine as well as histamine induced tracheal chain contraction, and also antigen induced contraction of sensitized guinea pig ileum (Shultz-Dale inhibition test). Furthermore, it exhibited also free radicals scavenging activity (in vitro). The observed anti-allergic and anti-anaphylactic activity of extract of Z. jujuba may be largely through the stabilization of mast cells by the membrane presence of phytoconstituents (steroidal saponins and flavonoids).

Resumo em Inglês:

The aim of the present study was to investigate the pancreatic regeneration potential of of diferent fractions of the ethanol extract Clitoria ternateaL., Fabaceae. The antidiabetic and antihyperlipidemic potential was evaluated in streptozotocin-induced diabetic rats and correlated with its in vivoand in vitro antioxidant activity. The extract and its fractions were initially screened for acute and sub-chronic antidiabetic activity in the dose range of 100200 mg/kg. The most potent extract and fractions were further evaluated for pancreatic β-cells regeneration activity along with antioxidant and antihyperlipidemic activity. The polyphenolic, flavonoid and flavanone contents were assessed and correlated with its antidiabetic activity. The most significant pancreatic regeneration activity, antidiabetic and antihyperlipidemic activity and was shown by ethanol extract and butanol soluble fraction at a dose level of 200 mg/kg, while rutin was found to be least potent. In conclusion, pancreatic regeneration studies of ethanol extract treated rats show nesidioblastosis. It is also suggested that the factors causing regeneration are present within the pancreas. The newly generated islets may have formed from the ductal precursor cells and reduced oxidative stress helps in restoration of β-cell function.

Resumo em Inglês:

Blepharis maderaspatensis (L.) B. Heyne ex Roth, Acanthaceae, is a procumbent or scrambling perennial herb used traditionally for treatment of snakebites, wounds, edema and gout. The anti-inflammatory and anti-nociceptive properties of the ethanol extract of the whole plant of B. maderaspatensis was investigated using carrageenan-induced paw edema in rats, xyleneinduced edema in mice, mouse writhing and tail clip tests respectively. The effect of the extract on inflammatory mediators, serotonin and histamine, using the most active dose (75 mg/kg) was also carried out. The results showed that the extract of B. maderaspatensis in carrageenan-induced test caused a significant inhibition (84.5%, 90 min) of paw edema at a dose of 75 mg/kg while the xylene-induced test caused a significant inhibition (62.65%) at 50 mg/kg. The histamine-induced test showed significant inhibition (90.9%, 90 min) while serotonin-induced test showed moderate inhibition (54.10%, 180 min). In the mouse writhing and tail clip tests, the extract produced a significant inhibition of 66.21% and 15.81% at 75 mg/kg, respectively. These results collectively demonstrate that the ethanol extract of B. maderaspatensis possesses anti-inflammatory and anti-nociceptive properties, and this supports the ethnopharmacological use of the plant in the treatment of inflammation.

Resumo em Inglês:

Sidastrum micranthum (A. St.-Hil.) Fryxell, Malvaceae, grows in the northeastern region of Brazil, where the leaves of this species are traditionally used to treat coughs, bronchitis or asthma. Male Swiss mice (20-22 g) were tested in models of acute pain (acetic acid-induced abdominal writhing, tail flick and formalin test), oedema assessment test (paw oedema test) and model for evaluation of spontaneous motor performance (open field test). The hydroethanolic extract of S. micranthum was administered orally at doses of 50-500 mg/kg. In addition were administered water, vehicle, morphine 5.01 mg/kg (evaluation of pain and motor performance) and dexamethasone 2.25 mg/kg (evaluation of oedema formation). The extract showed a significant effect at all doses in the acetic acid-induced abdominal writhing test and at the second phase of the formalin test, while in the first phase of this test and in the paw oedema test only at the highest dose (500 mg/kg). In the formalin and paw oedema tests, the extract had a potentiation of the anti-nociceptive and anti-inflammatory effects by pretreatment with L-NAME and reduction of the effect by pretreatment with L-arginine. The extract was not toxic after oral administration (LD50 > 2000 mg/kg).

Resumo em Inglês:

Natural products are regarded as major and important sources of molecules used in chemotherapy. Hypericum brasiliense Choisy, Hypericaceae, is an annual bush, native in the southern and southeastern Brazil. This species has been used in Brazilian folk medicine the anti-spasmodic and for the treatment of infectious diseases. H. brasiliense is chemically composed by flavonoids and xanthones. In addition, this species contain phloroglucinols, a class of substances with citotoxity effects against tumor cells lines. On the present study, hexanic extract and derivatives phloroglucinols obtained from H. brasiliense were tested against some human tumor cell lines. Hexanic extract presented a potent antiproliferative activity, with selective action on OVCAR-03 (ovarian), NCIADR/ RES (ovarian resistant) and UACC-62 (melanoma) tumor cell lines. Uliginosin B was the most active derivative phloroglucinol, presenting selectivity against NCI-ADR/ RES ( resistant ovarian) and OVCAR-03 (ovarian) tumor cell lines. Analysis of the results suggests that phloroglucinol derivatives with isoprenyl unit closed in the 9' position increases antiproliferative activity. Furthermore, this study contributes to identification of anti-tumor molecules and valorization of Hypericum brasiliense.

Resumo em Inglês:

The ground seed of Moringa oleifera Lam., Moringaceae, has been evaluated for its molluscicidal activity against the snails Biomphalaria glabrata, Physa marmorata and Melanoides tuberculatus. The results show that M. oleifera is active against B. glabrata (LC50 0.419 g/l; LC90 1.021 g/l and P. marmorata (LC50 0.339 g/l; LC90 0.789 g/l) but has no effect against M. tuberculatus. The great innovation of the use of M. oleifera, in addition to being innocuous to humans, is the present nutritional potential for humans and animals as well as providing an ecosystemic service as water purifier.