RESUMO
This study demonstrates in vivo analgesic and anti-inflammatory properties of hydroalcoholic extracts of leaves, bark and flowers from the Handroanthus impetiginosus (Bignoniaceae) plant, recognized as 'Ipê roxo' in Brazil. The extracts were evaluated in male Swiss albino mice via oral administration. Moreover, results of the in vivo paw oedema test induced by carrageenan revealed that extracts of leaves and bark displayed relevant anti-inflammatory activity potential at the dosage of 100 mg/kg, 300 mg/kg, and 500 mg/kg. Likewise, the results obtained for leaves and flowers extracts suggested potent analgesic action in the conventional hot plate test. UPLC/MS analysis of the hydroalcoholic extracts samples identified metabolites belonging to several classes, mainly naphthoquinones and iridoids derivatives as well as flavonoids. Thus, the obtained results indicate that the extracts of H. impetiginosus plant parts could be considered as a complementary herbal medicine for the treatment of pain and inflammation disorders.
RESUMO
Schistosomiasis mansoni is an infectious parasitic disease caused by worms of the genus Schistosoma, and praziquantel (PZQ) is the medication available for the treatment of schistosomiasis. However, the existence of resistant strains reinforces the need to develop new schistosomicidal drugs safely and effectively. Thus, the (±)-licarin A neolignan incorporated into poly-Æ-caprolactone (PCL) nanoparticles and not incorporated were evaluated for their in vivo schistosomicidal activity. The (±)-licarin A -loaded poly(ε-caprolactone) nanoparticles and the pure (±)-licarin A showed a reduction in the number of worm eggs present in spleens of mice infected with Schistosoma mansoni. In addition, the (±)-licarin A incorporated in the concentration of 20 mg/kg and 200 mg/kg reduced the number of worms, presenting percentages of 56.3% and 41.7%, respectively.
Assuntos
Nanopartículas , Esquistossomose mansoni , Esquistossomicidas , Animais , Caproatos , Lactonas , Lignanas , Camundongos , Poliésteres , Schistosoma mansoni , Esquistossomose mansoni/tratamento farmacológico , Esquistossomose mansoni/parasitologia , Esquistossomicidas/farmacologia , Esquistossomicidas/uso terapêuticoRESUMO
Origanum vulgare, known for its medicinal value, is officially accepted in many countries. The flowers and leaves are used globally in homeopathy. In Brazilian folk medicine, O. vulgare has been used to treat diabetes mellitus. This study evaluated the hypoglycemic activity of an infusion extract (RosCE) of commercially available O. vulgare leaves in alloxan-induced diabetic rats. Oral administration of RosCE resulted in the reduction of blood glucose levels after the first day of treatment, compared to the diabetic control group. These results showed that RosCE displays hypoglycemic activity, which may be due to the combined effect of rosmarinic acid, and other minor compounds. Reversed phase-high performance liquid chromatography-diode array detection was used to identify and quantify the major constituents of RosCE. This study presents evidence that supports the folkloric use of O. vulgare for the treatment of hyperglycemia, confirming the use of its infusion as an antidiabetic herbal medicine.
Assuntos
Diabetes Mellitus Experimental , Origanum , Aloxano , Animais , Glicemia , Cinamatos , Depsídeos , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ácido RosmarínicoRESUMO
Lignan dinitrohinokinin displays important biological activities, which led to the preparation of its poly-ε-caprolactone nanoparticles. Kinetics analysis revealed initially slow drug release followed by a prolonged, moderate release 6 h later due to DNHK diffusion through the polymeric matrix. Molecular dynamics simulations show that DNHK molecules that interact stronger with other DNHK molecules near the PCL/DNHK surface are more difficult to dissociate from the nanoparticle. The smaller diameter nanocapsules with negative surface charge conferred good colloidal stability. The formulations showed a size distribution with monodisperse systems formation. In vivo evaluation of schistosomicidal activity against Schistosoma mansoni showed that DNHK, when incorporated into nanoparticles, caused egg number reduction of 4.2% and 28.1% at 40 mg/kg and 94.2% and 84.4% at 400 mg/kg in the liver and the spleen, respectively. The PCL nanoparticles were stable in aqueous dispersion and could be optimized to be used as a promising lignan release agent.
Assuntos
Lignanas , Nanopartículas , Esquistossomicidas , Portadores de Fármacos , Lignanas/farmacologia , PoliésteresRESUMO
The occurrence of sulfated steroids and phenolics in marine organisms is quite widespread, being typically reported from Echinoderms. In contrast, alkane and alkene aliphatic sulfates are considerably rarer with examples being reported from a diverse array of organisms including echinoderms, sponges and ascidians. While no ecological roles for these metabolites have been proposed, they do exhibit a diverse array of biological activities including thrombin inhibition; the ability to induce metamorphosis in larvae; antiproliferative, antibacterial and antifungal properties; and metalloproteinase inhibition. Of particular interest and an avenue for future development is the finding of antifouling properties with low or nontoxic effects to the environment. This review focuses on alkyl sulfates and related sulfamates, their structures and biological activities. Spectroscopic and spectrometric techniques that can be used to recognize the presence of sulfate groups are also discussed, data for which will enhance the ability of researchers to recognize this class of chemically- and biologically-interesting marine natural products.
Assuntos
Organismos Aquáticos/química , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Invertebrados/química , Sulfatos/química , Sulfatos/farmacologia , Animais , Antifúngicos/química , Antifúngicos/farmacologia , Equinodermos/química , Humanos , Larva/química , Urocordados/químicaRESUMO
Abstract The ethanol crude extract from cashew (Anacardium occidentale L. Anacardiaceae) displayed significant antiplasmodial activity (IC50 0.577 µg/ml). Liquid chromatography-high resolution Mass spectrometry analysis was performed to identify the main compounds existing in the ethanol extract. The occurrence of anacardic acids, cardols, and 2-methylcardols derivatives was confirmed in the extract. The IC50 obtained, when the main isolated compounds were evaluated in Plasmodium falciparum D6 strain, ranged from 5.39 µM to >100 µM. Tested here for the first time, the data showed that cardol triene 1 (IC50 = 5.69 µM) and 2-methylcardol triene 4 (IC50 = 5.39 µM) demonstrated good antimalarial activity. In conclusion, Anacardium occidentale nuts presented relevant biological potential, and further studies should be considered.
RESUMO
Six dibenzylbutyrolactonic lignans ((-)-hinokinin (1), (-)-cubebin (2), (-)-yatein (3), (-)-5-methoxyyatein (4), dihydrocubebin (5) and dihydroclusin (6)) were isolated from Piper cubeba seed extract and evaluated against Schistosoma mansoni. All lignans, except 5, were able to separate the adult worm pairs and reduce the egg numbers during 24 h of incubation. Lignans 1, 3 and 4 (containing a lactone ring) were the most efficient concerning antiparasitary activity. Comparing structures 3 and 4, the presence of the methoxy group at position 5 appears to be important for this activity. Considering 1 and 3, it is possible to see that the substitution pattern change (methylenedioxy or methoxy groups) in positions 3' and 4' alter the biological response, with 1 being the second most active compound. Computational calculations suggest that the activity of compound 4 can be correlated with the largest lipophilicity value.
Assuntos
Anti-Helmínticos/farmacologia , Lignanas/farmacologia , Piper/química , Extratos Vegetais/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Animais , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Teoria da Densidade Funcional , Feminino , Lignanas/química , Lipídeos/química , Masculino , Camundongos Endogâmicos BALB C , Modelos Teóricos , Simulação de Acoplamento Molecular , Estrutura Molecular , Contagem de Ovos de Parasitas , Extratos Vegetais/química , Espectroscopia de Prótons por Ressonância Magnética , Schistosoma mansoni/química , Eletricidade Estática , Tubulina (Proteína)/químicaRESUMO
ABSTRACT Hyptis marrubioides Epling, Lamiaceae, a species from Brazilian Cerrado, has been used against gastrointestinal infections, skin infections, pain, and cramps. Herein, H. marrubioides seedlings were cultured in vitro under different wavelengths (white, blue, green, red, and yellow) with 50 µmol m-2 s-1 irradiance and a 16-h photoperiod. After 20 and 30 days of cultivation, shoot length, leaf number, fresh mass, and dry mass were evaluated. The flavonoid rutin content was determined by the HPLC-DAD method. The shoots were longer in plants cultivated under yellow (16.603 ± 0.790 cm, 1.8-fold), red (15.465 ± 0.461 cm, 1.7-fold), and green (14.677 ± 0.737 cm, 1.6-fold) lights than in control plants exposed to white light (9.203 ± 0.388 cm). The number of leaves increased in plants exposed to red (23.425 ± 1.138, 1.1-fold) and green (22.725 ± 1.814, 1.1-fold) lights, compared to control plants (20.133 ± 0.827). Fresh (0.665 ± 0.048 g, 1.2-fold) and dry (0.066 ± 0.005 g, 1.3-fold) mass of seedlings were the highest in seedlings grown under red light, compared to seedlings grown under white light (0.553 ± 0.048 and 0.028 ± 0.004, respectively). However, rutin production was higher under white (0.308 mg g-1 of dry weight) and blue lights (0.298 mg g-1 of dry weight). Thus, red light induces plant growth and increases leaf number and dry weight in in vitro-cultivated H. marrubioides, whereas blue and white lights promote the greatest rutin accumulation.
RESUMO
This article reports on the in vitro activity of the hydroalcoholic extract of Pfaffia glomerata roots, its hydrolyzed fractions, and pfaffic acid against Trypanosoma cruzi. The hydroalcoholic extract obtained from dried, milled P. glomerata roots was submitted to acid hydrolysis followed by partition with CHCl3 . The concentrated CHCl3 fraction was suspended in MeOH/H2 O and partitioned with hexane (F1), CHCl3 (F2), and AcOEt (F3), in this sequence. The trypanocidal activity of the hydrolyzed extract and its fractions was evaluated in vitro. The hydroalcoholic extract displayed low activity, but fraction F1 was active against trypomastigotes of the Y strain of T. cruzi, with IC50 = 47.89 µg/ml. The steroids campesterol (7.7%), stigmasterol (18.7%), ß-sitosterol (16.8%), Δ7 -stigmastenol (4.6%), and Δ7 -spinasterol (7.5%) were the major constituents of F1, along with fatty acid esters (7.6%) and eight aliphatic hydrocarbons (30.1%). Fractions F2 and F3 exhibited moderate activity, and pfaffic acid, one of the main chemical constituents of these fractions, displayed IC50 = 44.78 µm (21.06 µg/ml). On the other hand, the hydroalcoholic extract of P. glomerata roots, which is rich in pfaffosides, was inactive. Therefore, the main aglycone of pfaffosides, pfaffic acid, is much more active against trypomastigotes of the Y strain of T. cruzi than its corresponding glycosides and should be further investigated.
Assuntos
Amaranthaceae/química , Extratos Vegetais/farmacologia , Triterpenos/farmacologia , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Fracionamento Químico , Hidrólise , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/química , Triterpenos/isolamento & purificação , Tripanossomicidas/isolamento & purificaçãoRESUMO
(-)-Cubebin (CUB), isolated from seeds of Piper cubeba, was used as starting material to obtain the derivatives (-)-hinokinin (HK) and (-)-O-benzyl cubebin (OBZ). Using paw edema as the experimental model and different chemical mediators (prostaglandin and dextran), it was observed that both derivatives were active in comparison with both negative (5% Tween® 80 in saline) and positive (indomethacin) controls. The highest reduction in the prostaglandin-induced edema was achieved by OBZ (66.0%), while HK caused a 59.2% reduction. Nonetheless, the dextran-induced paw edema was not significantly reduced by either of the derivatives (HK or OBZ), which inhibited edema formation by 18.3% and 3.5%, respectively, in contrast with the positive control, cyproheptadine, which reduced the edema by 56.0%. The docking analysis showed that OBZ presented the most stable ligand-receptor (COX-2 - cyclooxygenase-2) interaction in comparison with CUB and HK.