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1.
J Ethnopharmacol ; 309: 116338, 2023 Jun 12.
Article in English | MEDLINE | ID: mdl-36870462

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Fridericia chica (Bonpl.) L.G. Lohmann (Bignoniaceae), is a climber native to Brazil, found in all Brazilian biomes. It is mostly known in Brazil as "carajiru," and home medicines made from the leaves have been used to cure disorders including stomach ulcers and other gastrointestinal disorders. AIM OF THE STUDY: The objective of the study was to investigate the F. chica hydroethanolic extract of leaves (HEFc) preventative and curative antiulcer gastrointestinal efficacy as well as the mechanisms of action using in vivo rodent models. MATERIALS AND METHODS: F. chica was collected in the municipality of Juína, Mato Grosso, and its leaves were used to prepare the extract by maceration technique (70% hydroethanol in the 1:10 ratio, w/v) to obtain the HEFc. The chromatographic analysis of HEFc was carried out by High Performance Liquid Chromatography-Photo Diode Array-Electrospray Ionization-Mass Spectrometry (HPLC-PDA-ESI-MS)- LCQ Fleet™ system. To determine the potential antiulcer potential of HEFc (1, 5 and 20 mg/kg, p.o.), the gastroprotective activity was assessed in various animal models of stomach ulcers caused by acidified ethanol, water constraint stress, indomethacin, (acute), and acid acetic (chronic). Additionally, the prokinetic properties of the HEFC were assessed in mice. The gastroprotective underlying mechanisms were evaluated by the histopathological analysis and determination of gastric secretion (volume, free and total acidity), gastric barrier mucus, activation of PGs, NO, K +ATP channels, α2-adrenoceptor, antioxidant activity (GSH, MPO and MDA), NO and mucosal cytokines (TNF-α, IL-1ß, and IL-10) levels. RESULTS: The chemical composition of HEFc was analyzed and apigenin, scutellarin, and carajurone were identified. HEFc (1, 5 and 20 mg/kg) showed effect against acute ulcers induced by HCl/EtOH with a reduction in the ulcerated area of 64.41% (p < 0.001), 54.23% (p < 0.01), 38.71% (p < 0.01), respectively. In the indomethacin experiment, there was no change in the doses tested, whereas in the water immersion restraint stress ulcer there was a reduction of lesions at doses of 1, 5, and 20 mg/kg by 80.34% (p < 0.001), 68.46% (p < 0.01) and 52.04% (p < 0.01). HEFc increased the mucus production at doses of 1 and 20 mg/kg in 28.14% (p < 0.05) and 38.36% (p < 0.01), respectively. In the pyloric ligation-induced model of gastric ulceration, the HEFc decreased the total acidity in all doses by 54.23%, 65.08%, and 44.40% (p < 0.05) and gastric secretory volume in 38.47% at dose of 1 mg/kg (p < 0,05) and increased the free acidity at the dose of 5 mg/kg by 11.86% (p < 0.05). The administration of EHFc (1 mg/kg) showed a gastroprotective effect possibly by stimulating the release of prostaglandins and activating K+ATP channels and α2-adrenoreceptors. Also, the gastroprotective effect of HEFc involved an increase in CAT and GSH activities, and a reduction in MPO activity and MDA levels. In the chronic gastric ulcer model, the HEFc (1, 5 and 20 mg/kg) decreased the ulcerated area significantly (p < 0.001) at all doses by 71.37%, 91.00%, and 93.46%, respectively. In the histological analysis, HEFc promoted the healing of gastric lesions by stimulating the formation of granulation tissue and consequently epithelialization. On the other hand, regarding the effect of HEFc on gastric emptying and intestinal transit, it was observed that the extract did not alter gastric emptying, but there was an increase in intestinal transit at the dose of 1 mg/kg (p < 0.01). CONCLUSION: These outcomes confirmed the advantages of Fridericia chica leaves for the treatment of stomach ulcers, which are well-known. HEFc was discovered to have antiulcer characteristics through multitarget pathways, which might be related to an increase in stomach defense mechanisms and a decrease in defensive factor. HEFc can be regarded as a potential new antiulcer herbal remedy because of its antiulcer properties, which may be attributed to the mixture of flavonoids, apigenin, scutellarin and carajurone.


Subject(s)
Anti-Ulcer Agents , Bignoniaceae , Gastritis , Stomach Ulcer , Rats , Mice , Animals , Apigenin/analysis , Ulcer/drug therapy , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Extracts/chemistry , Stomach Ulcer/chemically induced , Stomach Ulcer/drug therapy , Stomach Ulcer/pathology , Phytotherapy , Rats, Wistar , Anti-Ulcer Agents/pharmacology , Anti-Ulcer Agents/therapeutic use , Anti-Ulcer Agents/chemistry , Indomethacin/pharmacology , Ethanol/chemistry , Gastritis/drug therapy , Water , Adenosine Triphosphate , Plant Leaves/chemistry
2.
J Ethnopharmacol ; 269: 113735, 2021 Apr 06.
Article in English | MEDLINE | ID: mdl-33359865

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Dilodendron bipinnatum (Sapindaceae) stem bark decoction and macerate were used to treat uterine inflammation, pain in general, dermatitis and bone fractures. These homemade preparations also have diuretic, stimulant, expectorants and sedative effects and are effective in treating worm infections in the Brazilian Pantanal population. Our previous research confirmed the anti-inflammatory activity of the hydroethanolic extract of inner stem bark of D. bipinnatum (HEDb). AIM: This work aimed to investigate the efficacy of HEDb in ameliorating experimental colitis in rats and to elucidate the possible mechanisms involved in the anti-ulcerative colitis properties of HEDb in rats and Caco-2 cell line. MATERIALS AND METHODS: The effects on cell viability, IL-8 and TNF-α in human colon adenocarcinoma (Caco-2) were determined by flow cytometer and ELISA. Wistar rats (n = 6-7) were orally gavaged with, vehicle (0.9% saline), HEDb at doses of 20, 100 or 500 mg/kg, or mesalazine at a dose of 500 mg/kg, at 48, 24 and 1 h prior to the administration of trinitrobenzene sulfonic acid via rectal administration to induce colitis. The anti-inflammatory effects of HEDb were assessed macroscopically, by myeloperoxidase (MPO) activity and for glutathione (GSH) concentration in the colon. Additionally, colonic histopathological analyses of UC severity were conducted by different staining methods (H&E, PAS and toluidine blue). Pro-inflammatory cytokines TNF-α and IL-1ß were quantified in colonic tissue by ELISA and colonic expressions of COX-2 and IL-17 were analyzed by western blotting. RESULTS: HEDb was shown to be non-cytotoxic with mean viability of 80% in Caco-2 cells. HEDb pre-treatments of 1, 5 or 20 µg/mL significantly reduced TNF-α production in Caco-2 cells by 21.8% (p < 0.05), 60.5 and 82.1% (p < 0.001) respectively following LPS treatment compared to LPS alone. However, no change in IL-8 production was observed. HEDb pre-treatment of rats subjected to TNBS significantly (p < 0.001) reduced colonic lesion score. Higher doses (100 and 500 mg/kg) caused a sharp downregulation of haemorrhagic damage, leukocyte infiltration, edema and restoration of mucus production. Moreover, mast cell degranulation was inhibited. Colonic MPO activity was reduced following all doses of HEDb, reaching 51.1% ± 1.51 (p < 0.05) with the highest dose. GSH concentration was restored by 58% and 70% following 100 and 500 mg/kg of HEDb, respectively. The oral treatment of HEDb at doses 20, 100 and 500 mg/kg decreased the concentrations of TNF-α and IL-1ß at all doses in comparison to vehicle treated control. In addition, HEDb inhibited the COX-2 and IL-17 expressions with maximal effect at 500 mg/kg (60.3% and 65% respectively; p < 0.001). In all trials, the effect of HEDb at all doses being 20, 100 and 500 mg/kg was statistically comparable to mesalazine (500 mg/kg). CONCLUSIONS: HEDb reduces colonic damage in the TNBS colitis model and relieves oxidative and inflammatory events, at least in part, by increasing mucus production, reducing leukocyte migration and reducing TNF-α (in vivo and in vitro), IL-1ß, IL-17 and COX-2 expression. Therefore, HEDb requires further investigation as a candidate for treating IBD.


Subject(s)
Antioxidants/pharmacology , Colitis, Ulcerative/prevention & control , Mucus/metabolism , Plant Bark/chemistry , Plant Extracts/pharmacology , Sapindaceae/chemistry , Animals , Antioxidants/chemistry , Antioxidants/therapeutic use , Brazil , Caco-2 Cells , Cell Survival/drug effects , Colitis, Ulcerative/chemically induced , Colitis, Ulcerative/pathology , Cyclooxygenase 2/metabolism , Disease Models, Animal , Edema/chemically induced , Edema/prevention & control , Glutathione/metabolism , Humans , Interleukin-17/metabolism , Interleukin-1beta/metabolism , Interleukin-8/metabolism , Lipopolysaccharides/toxicity , Mast Cells/drug effects , Peroxidase/metabolism , Plant Extracts/chemistry , Plant Extracts/therapeutic use , Rats, Wistar , Trinitrobenzenesulfonic Acid/toxicity , Tumor Necrosis Factor-alpha/metabolism
3.
J Ethnopharmacol ; 254: 112707, 2020 May 23.
Article in English | MEDLINE | ID: mdl-32112897

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Piper umbellatum L. leaves, commonly found in the Amazon, Cerrado and Atlantic rain forest regions of Brazil, are widely used as a traditional medicine to treat gastrointestinal disorders and inflammation, among others diseases. Also, previous scientific studies demonstrated that P. umbellatum has gastroprotective and anti-inflammatory activity. AIM: To investigate the phytochemical profiles and the intestinal anti-inflammatory effect of the hydroethanolic extract of P. umbellatum (HEPu) leaf on ulcerative colitis in rats. MATERIALS AND METHODS: In this study, the chemical composition of HEPu was analyzed by gas chromatography-mass spectrometry (GC-MS) and liquid chromatography coupled to mass spectrometry (LC/MS). Also, this work studied the effects of HEPu on ulcerative colitis induced by 2,4,6-trinitrobenzene sulfonic acid (TNBS, 30 mg/mL in 20% ethanol) by intrarectal administration in rats. Simultaneously, animals were pre-treated orally with HEPu (30, 100 and 300 mg/kg), mesalazine (500 mg/kg), or vehicle. At the end of the experimental period, clinical signs of ulcerative colitis were evaluated by determination of weight loss, gross appearance, ulcer area and histological changes. Reduced glutathione (GSH), lipoperoxides (MDA) and nitric oxide (NO) levels, and superoxide dismutase (SOD), myeloperoxidase (MPO) and catalase (CAT) activities were determined in colon tissues. Also, pro-inflammatory mediators such as tumor necrosis factor alpha (TNF-α) and interleukin 1 beta (IL- 1ß) were quantified by immunoassay on the surface of fluorescent-coded magnetic beads (Luminex MagPix System). RESULTS: GC-MS analysis showed the presence of 17 different phytochemical compounds in the HEPu. LC/MS analyses revealed the presence of compounds in HEPu as protocatechuic acid, ferulic acid, kaempferol, rosmarinic acid, apigenin and ursolic acid. Treatment with HEPu significantly ameliorated weight loss, macroscopic damage, ulcerated area and histopathological changes such as sub-mucosal edema, cell infiltration, ulceration and necrosis (p < 0.001). Furthermore, HEPu (30, 100, and 300 mg/kg, p.o) inhibited the levels of oxidative parameters, such as MPO (49%, 53%, and 62%, p < 0.001), NO (20%, 19%, 22%, p < 0.01), and MDA (75%, 83%, 70%, p < 0.001), whereas increased the antioxidant activities such as SOD (208%, 192%, 64%, p < 0.001), GSH (94%, 75%, 49%, p < 0.01), and CAT (92%, 69%, 108%, p < 0.01). The extract also inhibited the pro-inflammatory cytokines TNF-α (81%, 85%, 85%, p < 0.001) and IL-1ß (95%, 79%, 89%, p < 0.001) levels. CONCLUSION: Together, these results revealed that P. umbellatum L. is a promising source of metabolites to be used in the treatment of inflammatory bowel disease.


Subject(s)
Anti-Inflammatory Agents/therapeutic use , Antioxidants/therapeutic use , Colitis, Ulcerative/drug therapy , Piper , Plant Extracts/therapeutic use , Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Catalase/metabolism , Colitis, Ulcerative/chemically induced , Colitis, Ulcerative/metabolism , Colitis, Ulcerative/pathology , Colon/drug effects , Colon/metabolism , Colon/pathology , Cytokines/metabolism , Female , Malondialdehyde/metabolism , Nitric Oxide/metabolism , Phytochemicals/analysis , Phytochemicals/pharmacology , Phytochemicals/therapeutic use , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Leaves , Rats, Wistar , Superoxide Dismutase/metabolism , Trinitrobenzenesulfonic Acid
4.
J Ethnopharmacol ; 225: 71-80, 2018 Oct 28.
Article in English | MEDLINE | ID: mdl-29960023

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Sphenodesme involucrata var. paniculata (C. B. Clarke) Munir is native as well as endemic to South India. Its leaves are used in folklore medicine to treat pain and rheumatism. OBJECTIVE: This study was aimed to investigate the chemical characterization, anti-nociceptive and mode of action underlying the anti-inflammatory effects of methanol extract of S. involucrata leaves (MESi). METHODS: Phytoconstituents of MESi was analyzed using colorimetric and liquid chromatography-mass spectrometry (LC-MS) methods, and the oral acute toxicity was evaluated in mice up to 2000 mg/kg. The anti-nociceptive effect was evaluated in hot plate and writhing tests; whereas the anti-inflammatory effect was investigated using carrageenan, cotton pellet and lipopolysaccharide (LPS)-induced peritonitis models at doses of 100, 200 and 400 mg/kg. Additionally nitric oxide (NO) and inflammatory cytokines levels were also evaluated. RESULTS: MESi exhibited the high content of phenolics and flavonoids as well as compounds like austricine, benzylglucosinolate, gossypin, justicidin B and cirsimarin were detected in LC-MS. In the acute toxicity study, oral administration of MESi did not cause any toxic effect and mortality up to 2000 mg/kg body weight in mice. In the anti-nociceptive tests, MESi augmented the latency period at higher dose (400 mg/kg), on the other hand attenuated writhings at the dose of 400 mg/kg by 87.87% (p < 0.001). In the carrageenan induced paw oedema MESi significantly inhibited the oedema formation at dose 400 mg/kg by 32.1%; besides, anti-inflammatory effect was registered in the cotton pellets-induced inflammation model at doses 200 and 400 mg/kg by 27.09% (p < 0.001) and 35.47% (p < 0.001) respectively. On the other hand, MESi appreciably reduced leukocyte, neutrophils infiltration, nitric oxide, TNF-α and IL-1ß levels and increased the IL-10 level in the (LPS)-induced peritonitis model. CONCLUSION: The results conclude that MESi has no acute toxic effect and it demonstrated potent anti-nociceptive and anti-inflammatory activities. Its anti-nociceptive activities are probably mediated through peripheral and central mechanisms. The anti-inflammatory effect of MESi involved the inhibition of neutrophils migration and the modulation of Th1 and Th2 cytokines, besides the attenuation of production of PGE2 and NO. LC-MS analysis revealed the predominant presence of the austricine, benzylglucosinolate, gossypin, justicidin B and cirsimarin compounds, which are possibly involved in the anti-nociceptive and anti-inflammatory effects of MESi. The current study provided supportive evidence for the folklore use of S. involucrata in the treatment of pain and inflammatory conditions.


Subject(s)
Analgesics , Anti-Inflammatory Agents , Lamiaceae , Plant Extracts , Analgesics/analysis , Analgesics/therapeutic use , Analgesics/toxicity , Animals , Anti-Inflammatory Agents/analysis , Anti-Inflammatory Agents/therapeutic use , Anti-Inflammatory Agents/toxicity , Carrageenan , Cytokines/immunology , Edema/drug therapy , Female , Granuloma/drug therapy , Lipopolysaccharides , Male , Methanol/chemistry , Mice , Pain/drug therapy , Peritonitis/drug therapy , Peritonitis/immunology , Phytochemicals/analysis , Phytochemicals/therapeutic use , Phytochemicals/toxicity , Phytotherapy , Plant Extracts/analysis , Plant Extracts/therapeutic use , Plant Extracts/toxicity , Plant Leaves , Rats, Wistar , Solvents/chemistry , Toxicity Tests, Acute
5.
Mem. Inst. Oswaldo Cruz ; 108(8): 974-982, 6/dez. 2013. tab, graf
Article in English | LILACS | ID: lil-697147

ABSTRACT

Infusions of Aspidosperma nitidum (Apocynaceae) wood bark are used to treat fever and malaria in the Amazon Region. Several species of this family are known to possess indole alkaloids and other classes of secondary metabolites, whereas terpenoids, an inositol and the indole alkaloids harmane-3 acid and braznitidumine have been described in A. nitidum . In the present study, extracts from the wood bark, leaves and branches of this species were prepared for assays against malaria parasites and cytotoxicity testing using human hepatoma and normal monkey kidney cells. The wood bark extracts were active against Plasmodium falciparum and showed a low cytotoxicity in vitro, whereas the leaf and branch extracts and the pure alkaloid braznitidumine were inactive. A crude methanol extract was subjected to acid-base fractionation aimed at obtaining alkaloid-rich fractions, which were active at low concentrations against P. falciparum and in mice infected with and sensitive Plasmodium berghei parasites. Our data validate the antimalarial usefulness of A. nitidum wood bark, a remedy that can most likely help to control malaria. However, the molecules responsible for this antimalarial activity have not yet been identified. Considering their high selectivity index, the alkaloid-rich fractions from the plant bark might be useful in the development of new antimalarials.


Subject(s)
Animals , Humans , Mice , Antimalarials/pharmacology , Aspidosperma/chemistry , Plant Bark/chemistry , Plant Extracts/pharmacology , Plasmodium berghei/drug effects , Plasmodium falciparum/drug effects , Antimalarials/isolation & purification , Malaria/drug therapy , Malaria/parasitology , Parasitic Sensitivity Tests , Plant Extracts/isolation & purification
6.
Mem Inst Oswaldo Cruz ; 108(8): 974-82, 2013 Dec.
Article in English | MEDLINE | ID: mdl-24402150

ABSTRACT

Infusions of Aspidosperma nitidum (Apocynaceae) wood bark are used to treat fever and malaria in the Amazon Region. Several species of this family are known to possess indole alkaloids and other classes of secondary metabolites, whereas terpenoids, an inositol and the indole alkaloids harmane-3 acid and braznitidumine have been described in A. nitidum . In the present study, extracts from the wood bark, leaves and branches of this species were prepared for assays against malaria parasites and cytotoxicity testing using human hepatoma and normal monkey kidney cells. The wood bark extracts were active against Plasmodium falciparum and showed a low cytotoxicity in vitro, whereas the leaf and branch extracts and the pure alkaloid braznitidumine were inactive. A crude methanol extract was subjected to acid-base fractionation aimed at obtaining alkaloid-rich fractions, which were active at low concentrations against P. falciparum and in mice infected with and sensitive Plasmodium berghei parasites. Our data validate the antimalarial usefulness of A. nitidum wood bark, a remedy that can most likely help to control malaria. However, the molecules responsible for this antimalarial activity have not yet been identified. Considering their high selectivity index, the alkaloid-rich fractions from the plant bark might be useful in the development of new antimalarials.


Subject(s)
Antimalarials/pharmacology , Aspidosperma/chemistry , Plant Bark/chemistry , Plant Extracts/pharmacology , Plasmodium berghei/drug effects , Plasmodium falciparum/drug effects , Animals , Antimalarials/isolation & purification , Humans , Inhibitory Concentration 50 , Malaria/drug therapy , Malaria/parasitology , Mice , Parasitic Sensitivity Tests , Plant Extracts/isolation & purification
7.
J Ethnopharmacol ; 144(3): 497-505, 2012 Dec 18.
Article in English | MEDLINE | ID: mdl-23069941

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Lafoensia pacari St.-Hil. is a tree native to the Brazilian Cerrado. Its bark macerate is popularly used in Brazilian folk medicine for the treatment of peptic ulcer, wound healing and inflammation. AIM OF THE STUDY: To evaluate the antiulcer activities of the methanol extract of Lafoensia pacari (MELP) and possible mechanisms of actions involved. MATERIALS AND METHODS: The stem bark of Lafoensia pacari was macerated in methanol to obtain the crude methanol extract of Lafoensia pacari (MELP). The gastroprotective and ulcer healing of MELP were evaluated using ethanol, indomethacin, cold-restraint stress-induced (acute) and acetic acid (chronic) ulcer models. The probable mode of action of MELP was also evaluated by determining intestinal transit, involvement of non-protein sulfhyhydryls (NP-SH), gastric mucus secretion, gastric secretory parameters and pro-inflammatory cytokines, tumor necrosis factor-α (TNF-α) and interleukin-17 (IL-17). Phytochemical analysis was carried out using classical methods and ellagic acid, one of the most important pharmacological active compounds was confirmed by HPLC. RESULTS: The results of the pharmacological studies on MELP demonstrated potent and effective gastroprotection against ethanol, indomethacin and cold stress-induced acute ulcers and ulcer healing in acetic acid induced chronic ulcer. MELP had no significant effect on the intestinal motility and it is also independent of mucus production but rather have a mucolytic effect. In pylorus-ligated rats the extract showed anti-secretory activity by decreasing total gastric juice volume and gastric acidity while increasing the gastric pH. The gastroprotection against ethanol is partially attributed to effective attenuation in the decrease in NP-SH levels, inhibition of the increases in the pro-inflammatory cytokines, TNF-α and IL-17. Phytochemical analysis of MELP revealed the presence of pyrrogalic tannins, saponins, steroids, triterpenoids and simple phenols, with ellagic acid being the major components. CONCLUSION: The results of this study showed that MELP possesses preventive and curative effects against gastric ulcer in experimental animals. These effects are partly dependent on its anti-oxidant, anti-secretory properties and inhibition of pro-inflammatory cytokines and independent of gastric/intestinal motility and mucus secretion. Ellagic acid, a compound of proven antiulcer activity, was found in MELP as the major component. These results confirmed the traditional use of MELP in Brazilian popular medicine for the treatment of gastric ulcers and shed some light on some of its mechanisms of action.


Subject(s)
Anti-Ulcer Agents/therapeutic use , Lythraceae , Phytotherapy , Plant Extracts/therapeutic use , Stomach Ulcer/drug therapy , Acetic Acid , Animals , Anti-Ulcer Agents/pharmacology , Brazil , Ethanol , Gastrointestinal Transit/drug effects , Indomethacin , Interleukin-17/blood , Male , Medicine, Traditional , Methanol/chemistry , Mice , Plant Bark , Plant Extracts/pharmacology , Rats , Rats, Wistar , Solvents/chemistry , Stomach Ulcer/blood , Stomach Ulcer/chemically induced , Stomach Ulcer/physiopathology , Stress, Psychological , Tumor Necrosis Factor-alpha/blood
8.
J Agric Food Chem ; 59(13): 6957-65, 2011 Jul 13.
Article in English | MEDLINE | ID: mdl-21644797

ABSTRACT

Ellagic acid (EA), a plant-derived polyphenol, exhibits antioxidant, anti-inflammatory, and gastroprotective effects. Its gastroprotective mechanisms have not been fully elucidated nor have its effects on chronic ulcer previously been described. Toward these ends, the antiulcer activities of EA were evaluated in acute (ethanol and indomethacin) and chronic (acetic acid) ulcer models in Wistar rats. In this study, oral administration of EA significantly prevented the gastric ulceration caused by ethanol, indomethacin, and acetic acid treatments. Its gastroprotective mechanism in ethanol-induced ulcer were partly due to intensification in the endogenous production of nitric oxide, an antioxidant effect by replenishing depletion of endogenous nonprotein sulfhydryls and attenuation of tumor necrosis factor-α increase, whereas in indomethacin ulcer, it is partly due to a reduction in the plasma level of leukotriene B(4). In acetic acid ulcer, promotion of ulcer-healing effects was partly due to attenuation of the elevated levels of the inflammatory cytokines TNF-α, interferon-γ, and interleukins-4 and -6. These findings suggest that ellagic acid exerts its antiulcer activity by strengthening the defensive factors and attenuating the offensive factors.


Subject(s)
Ellagic Acid/therapeutic use , Stomach Ulcer/drug therapy , Stomach Ulcer/prevention & control , Acetic Acid , Animals , Anti-Ulcer Agents/therapeutic use , Cytokines/blood , Dinoprostone/analysis , Ethanol , Female , Gastric Mucosa/chemistry , Indomethacin , Leukotriene B4/blood , Male , Mucus/drug effects , Rats , Rats, Wistar , Stomach Ulcer/chemically induced
9.
Braz. j. pharm. sci ; 46(3): 515-523, July-Sept. 2010. ilus
Article in English | LILACS | ID: lil-564918

ABSTRACT

Macrosiphonia velame (Apocynaceae), popularly known as "velame-branco", is mainly used for treating inflammatory conditions. The antiinflammatory, antinociceptive and antipyretic effects of the hydroethanolic extract of the xylopodium from M. velame (HEMv) were evaluated using several animal models. HEMv showed low acute oral toxicity with LD50 of 4.176 ± 218.5 mg/kg in mice. In tests of carrageenan and dextran-induced paw edema and carrageenan-induced pleurisy in rats, and croton oil-induced cutaneous dermatitis in mice, HEMv presented systemic and topical antiinflammatory activities. In experiments of nociception induced by acetic acid, formalin and capsaicin in mice, the HEMv evidenced an antinociceptive effect, being active against both inflammatory and neurogenic pain. Additionally, the HEMv prevented brewer's yeast-induced pyrexia in rats. It is likely that the pharmacologic mechanism of HEMv may involve the inhibition of different mediators of the inflammatory response, such as histamine, serotonin, prostaglandins and leukotrienes. A preliminary phytochemical study was also undertaken on HEMv, which revealed the presence of flavonoids, phenolic compounds, pentacyclic triterpenoids, saponins, coumarins, catechins, tannins, and alkaloids. Taken together, these results suggest that M. velame extract has antiinflammatory, antinociceptive and antipyretic properties and further validate the traditional use of this plant in inflammatory conditions.


Macrosiphonia velame (Apocynaceae), conhecida popularmente como velame-branco, é utilizada no tratamento de inflamações. Avaliou-se nesse estudo, os efeitos antiinflamatório, antinociceptivo e antipirético do extrato hidroetanólico do xilopódio de M. velame (HEMv) em modelos animais. O HEMv apresentou baixa toxicidade aguda oral, com DL50= 4.176 ± 218,5 mg/kg nos camundongos. Nos testes de edema de pata por carragenina e dextrana e pleurisia por carragenina em ratos e dermatite cutânea por óleo de croton em camundongos, o HEMv apresentou atividade antiinflamatória sistêmica e tópica. Nos experimentos de nocicepção induzida por ácido acético, formalina e capsaicina em camundongos, o HEMv inibiu a resposta nociceptiva nos três modelos, mostrando-se ativo tanto na dor de origem inflamatória como neurogênica. Adicionalmente, o HEMv bloqueou a hipertermia induzida por levedura de cerveja nos ratos. É provável que os efeitos farmacológicos observados para o HEMv decorram da inibição de mediadores da resposta inflamatória produzidos pelas vias da COX e/ou LOX bem como da inibição da liberação de histamina e serotonina. A análise fitoquímica do HEMv revelou a presença de flavonóides, compostos fenólicos, triterpenóides pentacíclicos, saponinas, cumarinas, catequinas, taninos catéquicos e alcalóides. Estes resultados validam sob o ponto de vista pré-clínico, o uso popular de M. velame em processos inflamatórios.


Subject(s)
Animals , Male , Adult , Rats , Anti-Inflammatory Agents , Analgesics, Non-Narcotic/analysis , Analgesics/analysis , Apocynaceae/chemistry , Plant Extracts/pharmacology , Analysis of Variance , Pharmacognosy/statistics & numerical data , Skin Tests , Data Interpretation, Statistical
10.
Rev. bras. farmacogn ; 20(4): 549-562, ago.-set. 2010. ilus, tab
Article in Portuguese | LILACS | ID: lil-557944

ABSTRACT

O presente trabalho verificou a utilização de plantas medicinais encontradas no Cerrado mato-grossense para o tratamento de hiperlipidemias e obesidade. Entrevistas com 180 pessoas acima de 50 anos foram realizadas em Nova Xavantina-MT. O questionário abordou nome popular, parte utilizada, forma de preparo e uso das espécies citadas, além de informações gerais sobre o uso de plantas. As dez plantas mais citadas foram coletadas, identificadas e estudadas por meio de uma revisão bibliográfica. A maioria dos entrevistados (95,6 por cento) declarou utilizar plantas medicinais regularmente, sendo que 71,5 por cento deles herdaram o conhecimento sobre plantas dos pais e avós e 94,20 por cento relataram aconselhar o uso aos mais jovens. Além disso, 93,6 por cento atestaram que as plantas são mais eficazes que os medicamentos de farmácia e 57 por cento consideraram forte o efeito das mesmas, ou seja, sempre resolvem o problema de saúde. Quanto aos efeitos adversos, 95,9 por cento disseram nunca ter sentido após o uso de plantas. Dos entrevistados, 56,7 por cento conheciam ou já haviam utilizado plantas medicinais no tratamento de hiperlipidemias e obesidade, sendo citadas 54 espécies medicinais diferentes pertencentes a 53 gêneros e 38 famílias, com destaque para Fabaceae (13 por cento). As dez plantas mais citadas foram: guatambu (Aspidosperma tomentosum Mart.), quina-do-cerrado (Strychnos pseudoquina St. Hil.), ipê-roxo [Tabebuia impetiginosa (Mart. Ex DC.) Standl], embaúba (Cecropia pachystachya Trec.), calunga (Simaba sp.), pata-de-vaca [Bauhinia rufa (Bong.) Steud.], mangaba (Hancornia speciosa Gomez), batata-de-tiú [Jatropha elliptica (Pohl.) Muell. Arg.], folha-de-carne (Casearia sylvestris Sw.) e manacá (Spiranthera odoratissima A. St.-Hil.). A folha foi a parte mais utilizada (46 por cento) e o preparo das plantas ocorre principalmente por meio de infusão citado por 36,5 por cento dos entrevistados. Apesar do uso popular destas plantas no combate as hiperlipidemias e obesidade, há necessidade de estudos fitoquímicos e farmacológicos que comprovem estas atividades, com vistas ao desenvolvimento de um fitoterápico.


This study checked the use of medicinal plants found in the Cerrado mato-grossense for the treatment of hyperlipidemia and obesity. Interviews with 180 people over 50 years were held in Nova Xavantina-MT. The questionnaire addressed popular name, part used, type of preparation and use of the species mentioned, beyond general information about the use of plants. The ten plants most cited were collected, identified and studied through a literature review. Most respondents (95.6 percent) said using medicinal plants regularly, while 71.5 percent of them inherited the knowledge of plants of parents and grandparents and 94.20 percent reported the use to advise youngsters. Furthermore, 93.6 percent attested that the plants are more effective than the drugs from pharmacy and 57 percent considered the strong effect of the same, i.e., they always solved health problems. Regarding adverse effects, 95.9 percent said they have never felt them after the use of plants. Of the respondents, 56.7 percent knew or had used medicinal plants in the treatment of hyperlipidemias and obesity, being cited 54 medicinal species belonging to 53 different genera and 38 families, with emphasis on Fabaceae (13 percent). The ten most cited were: guatambu (Aspidosperma tomentosum Mart.), quina-do-cerrado (Strychnos pseudoquina St. Hil.), ipê-roxo [Tabebuia impetiginosa (Mart. Ex DC.) Standl], embaúba (Cecropia pachystachya Trec.), calunga (Simaba sp.), pata-de-vaca [Bauhinia rufa (Bong.) Steud.], mangaba (Hancornia speciosa Gomez), batata-de-tiú [Jatropha elliptica (Pohl.) Muell. Arg.], folha-de-carne (Casearia sylvestris Sw.) and manacá (Spiranthera odoratissima A. St.-Hil.). The leaf was the most used (46 percent) and the preparation of the plants occurs mainly through the infusion cited by 36,5 percent of respondents. Despite the popular use of these plants for treatment of obesity and hyperlipidemia, further chemical and pharmacological studies are required to demonstrate these activities, in order to develop a phytotherapic product.

11.
Rev. bras. farmacogn ; 19(1a): 130-139, Jan.-Mar. 2009. mapas, tab
Article in Portuguese | LILACS | ID: lil-522432

ABSTRACT

O trabalho teve por objetivo proceder o levantamento etnobotânico das espécies vegetais utilizadas popularmente no Distrito de Pirizal - MT, no pantanal mato-grossense, como antiúlceras e antiinflamatórias. A entrevista aberta foi realizada através da aplicação de um roteiro base a 38 informantes adultos, na faixa etária de 25 a 75 anos. Indagou-se o nome popular das plantas, partes utilizadas, preparados e vias de administração, e realizou-se a revisão bibliográfica das plantas mais citadas no estudo, utilizando-se as bases de dados convencionais. Foram citadas 49 espécies pertencentes a 47 gêneros e 32 famílias, destacando-se a família Fabaceae. As plantas mais citadas simultaneamente como antiúlceras e antiinflamatórias foram Lafoensia pacari St. Hil. (9,2 por cento), Hyptis crenata Pohl (8,8 por cento), Hyptis suaveolens (L.) Poit (6,7 por cento), Stachytarpheta cayenensis (L.C.Rich) Vahl (5,8 por cento), Waltheria indica L. (5 por cento), Strychnos pseudoquina St. Hil. (4,2 por cento) e Vatairea macrocarpa (Benth.) Ducke (3,3 por cento). A parte da planta mais citada foi a folha (57,1 por cento), a via de administração mais utilizada no tratamento das úlceras gástricas foi a oral (100 por cento), com preferência para os chás (75 por cento), enquanto nas inflamações foram os banhos tópicos (60 por cento.). A revisão bibliográfica apontou a necessidade de aprofundar os estudos químico-farmacológicos para Vatairea macrocarpa (Benth.) Ducke e Hyptis crenata Pohl.


An ethnobotanical survey was conduced to study the vegetal species from Pantanal, in the district of Pirizal-MT, popularly used as anti-inflammatory and anti-ulcer. Ethnobotanical data were collected through open interviews and ethnopharmacology questionnaire with 38 local informers, in the age group of 25 to 75 years old. The local name, the part normally used, the mode of preparation and the administration route were asked to them. A bibliographic review of the plants most cited in the study was carried out using the conventional databases. A total of 49 species were cited belonging to 47 genera and 32 families, with emphasizing the Fabaceae family. The plants most cited were Lafoensia pacari St. Hil (9.2 percent), Hyptis crenata Pohl (8.8 percent), Hyptis suaveolens (L.) Poit (6.7 percent), Stachytarpheta cayenensis (L.C.Rich) Vahl (5.8 percent), Waltheria indica L. (5 percent), Strychnos pseudoquina St.Hil (4.2 percent) and Vatairea macrocarpa (Benth.) Ducke (3.3 percent). The part of the plant most cited was the leaf (57.1 percent), the most used administration route in the treatment of ulcers was oral (100 percent), in the form of teas (75 percent), while in the inflammations, topical baths were preferentially used (60 percent). The literature review indicated the need for further chemical-pharmacological studies on Vatairea macrocarpa (Benth.) Ducke and Hyptis crenata Pohl.

12.
Rev. bras. farmacogn ; 19(1b): 242-248, Jan.-Mar. 2009. tab, mapas
Article in English | LILACS | ID: lil-523090

ABSTRACT

Os extratos em hexano, diclorometano, acetato de etila e etanol das entrecascas de Bowdichia virgilioides, Calophyllum brasiliense, Cariniana rubra, Lafoensia pacari e Stryphnodendron obovatum, do rizoma de Simaba ferruginea e do látex de Croton urucurana foram triados contra um painel de bactérias e fungos usando o método de microdiluição em caldo. O látex de Croton urucurana foi o material derivado de planta com maior atividade antimicrobiana. Os extratos em acetato de etila e hexano da entrecasca de Calophyllum brasiliense destacaram-se por suas seletivas atividades antibacterianas. Os extratos polares da entrecasca de Lafoensia pacari notabilizaram-se por suas potentes e seletivas atividades contra leveduras e os extratos polares e não-polares de Bowdichia virgilioides por suas atividades antifúngicas contra hialo-hifomicetos e dermatófitos. Este é o primeiro relato mostrando atividades antifúngicas para os extratos de Cariniana rubra e Simaba ferruginea. Esse trabalho demonstrou a atividade antimicrobiana de plantas medicinais do Cerrado de Mato Grosso em ensaios in vitro e indica que elas podem ser potenciais candidatas para o desenvolvimento de novas estratégias no tratamento de infecções bacterianas e fúngicas.


Hexane, dichloromethane, ethyl acetate and ethanol extracts from stem barks of Bowdichia virgilioides, Calophyllum brasiliense, Cariniana rubra, Lafoensia pacari, and Stryphnodendron obovatum and rhizome of Simaba ferruginea and Dragon's blood red sap from Croton urucurana were screened against a panel of bacteria and fungi using the micro-broth dilution method. Dragon's blood from Croton urucurana was the most effective antimicrobial plant material. Ethyl acetate and hexane extracts of Calophyllum brasiliense stem bark deserved distinction by their selective antibacterial activity. Lafoensia pacari stem bark polar extracts distinguished by their potent and selective anti-yeast activity and Bowdichia virgilioides polar and non-polar extracts by their antifungal activity towards hyalohypho-mycetes and dermatophytes. This is the first report showing antifungal activity for polar extracts of Cariniana rubra and Simaba ferruginea. This study has demonstrated antimicrobial activity of Mato Grosso Cerrado ethnomedicinal plants in in vitro assays and has indicated that they can be effective potential candidates for the development of new strategies to treat fungal and bacterial infections.

13.
Z Naturforsch C J Biosci ; 60(9-10): 701-6, 2005.
Article in English | MEDLINE | ID: mdl-16320611

ABSTRACT

Simaba ferruginea (Simaroubaceae) is a Brazilian medicinal plant used in traditional medicine to treat several ailments, including gastric ulcers, fever, diarrhea, and dolorous and inflammatory processes. This study examines the chemical composition and antiulcerogenic effects of rhizomes from this plant. Bioassay-guided fractionation led to the isolation of two bioactive indole alkaloids called canthin-6-one (1) and 4-methoxycanthin-6-one (2). The alkaloid fraction and both alkaloids demonstrated potent antiulcerogenic effects when evaluated in gastric lesion-induced animals, as well as significant antinociceptive activity in mice. These results confirm and justify the popular use of S. ferruginea against gastric ulcers and dolorous processes.


Subject(s)
Anti-Ulcer Agents/chemistry , Anti-Ulcer Agents/therapeutic use , Rhizome/chemistry , Simaroubaceae/chemistry , Stomach Ulcer/chemically induced , Stomach Ulcer/drug therapy , Acetic Acid , Alkaloids/chemistry , Alkaloids/isolation & purification , Alkaloids/therapeutic use , Animals , Brazil , Indomethacin , Male , Medicine, Traditional , Methanol , Phytotherapy , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plants, Medicinal , Rats , Rats, Wistar
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