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1.
Molecules ; 28(7)2023 Mar 23.
Artigo em Inglês | MEDLINE | ID: mdl-37049664

RESUMO

Three new triterpenoids-spergulagenin B (1), spergulagenin C (2), and spergulagenin D (3)-were isolated from the aerial part of Glinus oppositifolius, along with 17 known compounds (4-20). The structures of these new compounds were identified by spectroscopic and MS analyses. Compounds 3, 5, 19, and 20 were evaluated for inhibition of nitric oxide production in LPS-stimulated RAW 264.7 cells with IC50 values of 17.03, 18.21, 16.30, and 12.64 µM, respectively. Compounds 3, 5, and 20 exhibited inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 cells with IC50 values of 18.35 ± 1.34, 17.56 ± 1.41, and 14.27 ± 1.29 µM, respectively.


Assuntos
Molluginaceae , Triterpenos , Animais , Camundongos , Molluginaceae/química , Triterpenos/farmacologia , Triterpenos/química , Óxido Nítrico , Lipopolissacarídeos/farmacologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Células RAW 264.7 , Estrutura Molecular
2.
Molecules ; 24(12)2019 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-31212847

RESUMO

Four new triterpenoids, 3ß,12ß,16ß,21ß,22-pentahydroxyhopane (1), 12ß,16ß,21ß,22-tetrahydroxyhopan-3-one (2), 3-oxo-olean-12-ene-28,30-dioic acid (3), and 3ß-hydroxyoleana-11,13(18)-diene-28,30-dioic acid 30-methyl ester (4); 21 new triterpenoid saponins, glinusopposides A-U (5-25); and 12 known compounds (26-37) were isolated from the whole plants of Glinus oppositifolius. The structures of the new compounds were elucidated based on the analysis of one-dimensional (1D) and two-dimensional (2D) nuclear magnetic resonance (NMR) and mass spectrometry (MS) data. All compounds from the plants were measured for antifungal activities against Microsporum gypseum and Trichophyton rubrum. Glinusopposide B (6), glinusopposide Q (21), glinusopposide T (24), and glinusopposide U (25) showed strong inhibitory activities against M. gypseum (MIC50 7.1, 6.7, 6.8, and 11.1 µM, respectively) and T. rubrum (MIC50 14.3, 13.4, 11.9, and 13.0 µM, respectively). For those active compounds with an oleanane skeleton, glycosylation (21-26) or oxidation (3) of 3-OH was helpful in increasing the activity; replacement of the 30-methyl group (29) by a carboxymethyl group (26) enhanced the activity; the presence of 11,13(18) double bonds (20) decreased the activity.


Assuntos
Antifúngicos/farmacologia , Glicosídeos/farmacologia , Microsporum/efeitos dos fármacos , Molluginaceae/química , Trichophyton/efeitos dos fármacos , Triterpenos/farmacologia , Antifúngicos/química , Glicosídeos/química , Espectroscopia de Ressonância Magnética , Modelos Moleculares , Conformação Molecular , Estrutura Molecular , Triterpenos/química
3.
Pharm Biol ; 57(1): 74-81, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30707846

RESUMO

CONTEXT: Mollugo pentaphylla L. (Molluginaceae) extract (MPE) has been reported to have anti-inflammatory effect on MSU-induced gouty arthritis in a mouse model. OBJECTIVE: This study examined the anti-inflammatory activities of an MPE in vitro and anti-osteoarthritis effects on monosodium iodoacetate (MIA)-induced osteoarthritis (OA) in vivo. MATERIALS AND METHODS: The dried whole plants of M. pentaphylla were extracted with 70% ethanol under reflux. The anti-inflammatory effect of MPE was evaluated in vitro in lipopolysaccharide (LPS)-treated RAW264.7 cells. The anti-osteoarthritic effect of MPE was investigated in a Sprague-Dawley rat model of MIA-induced OA. Each seven male rats were orally administered MPE (75, 150 or 300 mg/kg) or the positive control drug indomethacin (1 mg/kg) 3 days before MIA injection and once daily for 11 days thereafter. After the treatment with MPE, no evidence of systemic adverse effects was observed in any study group. RESULTS: MPE exhibited anti-inflammatory activity via inhibition of the production of NO (57.8%), PGE2 (97.1%) and IL-6 (93.2%) in LPS-treated RAW264.7 cells at 200 µg/mL. In addition, MPE suppressed IL-1ß (60.9%), TNF-α (37.9%) and IL- 6 (40.9%) production and suppressed the synthesis of MMP-2, MMP-9 and COX-2 in the MIA-induced OA rat model. CONCLUSIONS: These results demonstrate that MPE exerts potent anti-inflammatory activities and protects cartilage in an OA rat model. This might be a potential candidate for therapeutic OA treatment.


Assuntos
Anti-Inflamatórios/farmacologia , Molluginaceae/química , Osteoartrite/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Condrócitos , Indometacina/farmacologia , Articulação do Joelho/patologia , Lipopolissacarídeos/farmacologia , Masculino , Camundongos , Osteoartrite/induzido quimicamente , Células RAW 264.7 , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Suporte de Carga
4.
BMC Complement Altern Med ; 17(1): 447, 2017 Sep 06.
Artigo em Inglês | MEDLINE | ID: mdl-28874151

RESUMO

BACKGROUND: Gout is an inflammatory condition induced by the deposition of monosodium urate (MSU) crystals in joints and soft tissues, and it can lead to acute or chronic arthritis. MSU are pro-inflammatory stimuli that can initiate, amplify and sustain an intense inflammatory response. In this study, we evaluated the anti-inflammatory effect of an extract of Mollugo pentaphylla (MPE) on MSU-induced gouty arthritis in a mouse model. METHOD: An MSU crystal suspension (4 mg/50 µL) was injected intradermally into the right paw. The mice were orally administered MPE (150 mg/kg or 300 mg/kg) or the positive control drug colchicine (1 mg/kg) 1 h before the MSU crystals were injected and then once daily for 3 days. The effects of MPE included inflammatory paw edema and pain upon weight-bearing activity, and we evaluated the inflammatory cytokine expression and paw tissue inflammation-related gene expression. RESULTS: MPE suppressed inflammatory paw edema and pain in the MSU-induced mice. MPE showed anti-inflammatory activity by inhibiting the production of TNF-α, interleukin (IL)-1ß, NLRP3 inflammasome and NF-κB. CONCLUSION: These results suggest that MPE has potent anti-inflammatory activities and may be useful as a therapeutic agent against gouty arthritis.


Assuntos
Artrite Experimental/tratamento farmacológico , Artrite Gotosa/tratamento farmacológico , Molluginaceae/química , Extratos Vegetais/uso terapêutico , Animais , Artrite Experimental/induzido quimicamente , Artrite Experimental/fisiopatologia , Artrite Gotosa/induzido quimicamente , Artrite Gotosa/fisiopatologia , Comportamento Animal/efeitos dos fármacos , Citocinas/sangue , Edema/fisiopatologia , Pé/fisiopatologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Medição da Dor , Extratos Vegetais/farmacologia , Ácido Úrico/efeitos adversos , Suporte de Carga
5.
Phytother Res ; 27(4): 507-14, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22648529

RESUMO

An extract of Glinus lotoides, a medicinal plant used in Africa and Asia for various therapeutic purposes, was recently shown to cause DNA damage in vitro. To further explore the potential genotoxicity of this plant, fractionation of the crude extract was performed using reverse phase solid-phase extraction and a stepwise gradient elution of methanol in water. Four fractions were collected and subsequently analysed for their DNA damaging effects in mouse lymphoma cells using an alkaline version of the comet assay. To identify potential genotoxic and non-genotoxic principles, each fraction was then subjected to liquid chromatography coupled to mass spectrometry, LC-MS/MS. 1D and 2D nuclear magnetic resonance analyses were used to confirm the identity of some saponins. Although fractions containing a mixture of flavonoids and oleanane-type saponins or oleanane-type saponins alone produced no DNA damage, those containing hopane-type saponins exhibited a pronounced DNA damaging effect without affecting the viability of the cells. To conclude, even if this study presents evidence that hopane-type of saponins are endowed with a DNA damaging ability, further studies are needed before individual saponins can be cited as a culprit for the previously reported genotoxicity of the crude extract of G. lotoides.


Assuntos
Dano ao DNA , Molluginaceae/química , Extratos Vegetais/toxicidade , Saponinas/toxicidade , Triterpenos/toxicidade , Animais , Linhagem Celular Tumoral , Cromatografia Líquida , Ensaio Cometa , Camundongos , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/toxicidade , Plantas Medicinais/química , Espectrometria de Massas em Tandem
6.
Comb Chem High Throughput Screen ; 25(10): 1661-1671, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33653239

RESUMO

BACKGROUND: The management of acute inflammation, which arises from complex biological responses to harmful stimuli, is an important determinant in the recovery from an otherwise detrimental outcome such as septicemia. However, the side effects and limitations of current therapeutics necessitate the development of newer and safer alternatives. Mollugo cerviana is a common medicinal herb of the Indian subcontinent and has been traditionally used for its fever mitigating anti-microbial and hepatoprotective action. We have already reported the rich presence of radical scavenging phytochemicals in the plant extracts and their strong antioxidant properties. OBJECTIVE: In the present study, we have evaluated the anti-inflammatory effects of methanolic extract (ME) of the areal parts of M. cerviana in a lipopolysaccharide (LPS)-induced acute inflammatory cell culture model. METHODS: RAW 264.7 mouse macrophage cells were stimulated by the bacterial endotoxin LPS at a concentration of 1 µg/mL. Cytotoxicity and anti-inflammatory potential of ME were carried out. RESULTS: The concentration of M. cerviana extract up to 150 µg/ml was found to be non-toxic to cells (MTT and NRU assay). LPS induces acute inflammation by binding to TLR-4 receptors, initiating a downstream signalling cascade that results in pro-inflammatory cytokine secretion. Extract treatment at 100 µg/ml suppressed LPS-induced gene expression (qPCR) and secretion (ELISA) of pro-inflammatory cytokines IL-1ß, IL-6 and TNF-α, and the chemokine CCL2, leading to dampening of the acute inflammatory cascade. LPS-induced elevation of ROS level (DCFDA method) was significantly reduced by extract treatment. Nitric oxide production, as indicated by nitrite level, was significantly reduced post extract treatment. CONCLUSION: This study demonstrated that M. cerviana methanolic extract has a potent antiinflammatory effect in the in vitro acute inflammation model of LPS-stimulated RAW 264.7 cells. There is no reported study so far on the anti-inflammatory properties of M. cerviana in an LPSinduced acute inflammatory model, which closely mimics a human bacteremia response. Hence, this study highlights the therapeutic potential of this extract as a source of anti-inflammatory lead molecules.


Assuntos
Anti-Inflamatórios , Inflamação , Molluginaceae , Extratos Vegetais , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Citocinas/metabolismo , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Lipopolissacarídeos , Macrófagos , Metanol , Camundongos , Molluginaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Células RAW 264.7
7.
Molecules ; 15(9): 6186-92, 2010 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-20877215

RESUMO

An amino acid derivative, L-(-)-(N-trans-cinnamoyl)-arginine, was isolated from the whole plant of Glinus oppositifolius (L.) Aug. DC. along with kaempferol 3-O-galactopyranoside, isorhamnetin 3-O-beta-D-xylopyranosyl-(1-->2)-beta-D-galactopyranoside, vitexin, vicenin-2, adenosine and L-phenylalanine. The structure determinations were based on analyses of chemical and spectroscopic methods.


Assuntos
Arginina/análogos & derivados , Molluginaceae/química , Aminoácidos , Arginina/isolamento & purificação , Estrutura Molecular , Extratos Vegetais/análise
8.
J Gen Appl Microbiol ; 54(2): 101-6, 2008 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-18497484

RESUMO

Propionibacterium acnes and Staphylococcus epidermidis are pus-forming bacteria that trigger inflammation in acne. The present study was conducted to evaluate the antimicrobial activities of Jeju medicinal plants against these etiologic agents of acne vulgaris. Ethanol extracts of Jeju plants were tested for antimicrobial activities by disc diffusion and broth dilution methods. The results from the disc diffusion assays revealed that four medicinal plants, Mollugo pentaphylla, Angelica anomala, Matteuccia orientalis, and Orixa japonica inhibited the growth of both pathogens. Among these, A. anomala had strong inhibitory effects. Its MIC values were 15.6 microg/ml and 125 microg/ml against P. acnes and S. epidermidis, respectively. The cytotoxic effects of the four extracts were determined by colorimetric MTT assays using two animal cell lines: human dermal fibroblasts and HaCaT cells. Although the M. orientalis root extract had moderate cytotoxicity in HaCaT cells at 200 microg/ml, most extracts exhibited low cytotoxicity at 200 microg/ml in both cell lines. In addition, the extracts reduced the P. acnes-induced secretion of interleukin-8 and tumor necrosis factor-alpha (TNF-alpha) in THP-1 cells, an indication of their anti-inflammatory effects. Based on these results, we suggest that M. pentaphylla, A. anomala, M. orientalis, and O. japonica are attractive acne-mitigating candidates for topical application.


Assuntos
Antibacterianos/farmacologia , Anti-Inflamatórios/farmacologia , Plantas Medicinais/química , Propionibacterium acnes/efeitos dos fármacos , Staphylococcus epidermidis/efeitos dos fármacos , Acne Vulgar/microbiologia , Angelica/química , Antibacterianos/toxicidade , Anti-Inflamatórios/toxicidade , Células Cultivadas , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Dryopteridaceae/química , Fibroblastos/efeitos dos fármacos , Humanos , Interleucina-8/biossíntese , Queratinócitos/efeitos dos fármacos , Molluginaceae/química , Monócitos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Raízes de Plantas/química , Rutaceae/química , Fator de Necrose Tumoral alfa/biossíntese
9.
AAPS PharmSciTech ; 9(1): 31-8, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-18446458

RESUMO

The purpose of this research was to improve the hygroscopicity and poor flow properties of the crude dry extract of the seeds of Glinus lotoides and improve the disintegration time of the core-tablets for enteric coated formulation thereof. The liquid crude extract of the plant was adsorbed on granulated colloidal silicon dioxide (Aeroperl 300 Pharma) at 30% w/w and the dry extract preparation (DEP) was dry-granulated with roller-compaction using Micro-Pactor. Hygroscopicity, flow property and disintegration time were improved significantly due to the adsorption and granulation processes. Moreover, the DEP does not become mucilaginous even at higher relative humidity levels (above 65%). Oblong tablets (20 x 8.25 mm) containing 947 mg of the granulated DEP (equivalent to the traditional dose), 363 mg of Avicel PH101 and 90 mg of Ac-di-Sol as disintegrant were formulated using an instrumented eccentric tablet machine at 20 kN. The tablets showed a crushing strength of 195 N, a friability of 0.4% and disintegrated within 9 min. The tablets were then enteric coated using polymethacrylate co-polymers (Eudragit L 100-55 and Kollicoat MAE 100P). The coated tablets resisted disintegration or softening in simulated gastric fluid for a minimum of 2 h and disintegrated within 15 min in intestine simulated fluid at pH 6.8. In addition to controlling the release of the active agents, the enteric coating improved the strength and decreased friability of the core-tablets.


Assuntos
Portadores de Fármacos/química , Composição de Medicamentos/métodos , Molluginaceae/química , Extratos Vegetais/química , Sementes/química , Dióxido de Silício/química , Extratos Vegetais/administração & dosagem , Estresse Mecânico , Comprimidos com Revestimento Entérico
10.
J Ethnopharmacol ; 111(3): 451-7, 2007 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-17210235

RESUMO

Seeds of Glinus lotoides L. (Molluginaceae) are used traditionally in the treatment of tapeworm infestation in Ethiopia. Previous studies on its anthelmintic activities confirmed its traditional claims, but data on safety profile were lacking. To this effect, single and repeated dose oral toxicities of the methanolic extracts of seeds of Glinus lotoides were conducted in rats. Doses of 0, 1000 and 5000 mg/kg of crude extract of Glinus lotoides were employed in single dose toxicity studies, while doses of 0, 250, 500, and 1000 mg/kg were used in repeated toxicity studies. In the single dose toxicity test, oral administration of 5000 mg/kg of Glinus lotoides produced mortality in two females and one male on day 4. No significant differences in body and organ weights were observed between controls and treated surviving animals. Moreover, both gross and microscopic examinations of organs did not show detectable differences between controls and treated animals of both sexes. In repeated dose toxicity studies, no mortality was observed when varying doses of the extracts were administered per day for a period of 28 days. There were no significant differences in body weight, absolute and relative organ weights between controls and treated animals of both sexes. Hematological analysis showed no differences in most parameters examined. In the biochemistry parameter analysis, no significant change occurred. Pathologically, neither gross abnormalities nor histopathological changes were observed. These finding suggest that none of the organs appeared to be target and the data could provide satisfactory preclinical evidence of safety to launch clinical trial on standardized formulation of plant extracts.


Assuntos
Anti-Helmínticos/toxicidade , Medicinas Tradicionais Africanas , Molluginaceae/toxicidade , Extratos Vegetais/toxicidade , Administração Oral , Análise de Variância , Animais , Anti-Helmínticos/administração & dosagem , Anti-Helmínticos/química , Peso Corporal/efeitos dos fármacos , Relação Dose-Resposta a Droga , Etiópia , Feminino , Testes Hematológicos , Masculino , Molluginaceae/química , Tamanho do Órgão/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Ratos , Sementes , Testes de Toxicidade
11.
Phytochemistry ; 66(6): 621-6, 2005 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-15771879

RESUMO

Seven hopane-type saponins were isolated from the methanol extract of Glinus lotoides. Six of them were identified as novel compounds and designated as lotoideside A [3-O-beta-D-xylopyranosyl (1-->2)-alpha-L-rhamnopyranosyl-6 alpha-O-beta-D-xylopyranosyl-22-beta-O-beta-D-glucopyranosyl-16 beta-hydroxy hopane (1)], lotoideside B [3-O-beta-D-xylopyranosyl (1-->2)-alpha-L-rhamnopyranosyl-22-beta-O-beta-D-glucopyranosyl-6 alpha,16 beta-dihydroxyhopane (2)], lotoideside C [3-OD-xylopyranosyl-6 alpha-O-beta-D-xylopyranosyl-16 beta-O-beta-D-xylopyranosyl-22 beta-hydroxyhopane (3)], lotoideside D [3-O-beta-D-xylopyranosyl-16 beta-O-alpha-L-arabinopyranosyl-6 alpha,22-beta-dihydroxyhopane (4)], lotoideside E [3-O-beta-D-xylopyranosyl-6 alpha-O-beta-D-xylopyranosyl-16 beta,22-beta-dihydroxyhopane (5)], and lotoideside F [3-O-beta-D-xylopyranosyl-22-beta-O-beta-D-glucopyranosyl-16 beta-hydroxyhopan-6-one (6)]. The known compound succulentoside B (7) was also encountered. Their structures were elucidated on the basis of one-and two-dimensional NMR spectroscopic techniques, ESIMS and chemical evidences.


Assuntos
Molluginaceae/química , Saponinas/isolamento & purificação , Estrutura Molecular , Saponinas/química
12.
J Chromatogr A ; 1083(1-2): 32-41, 2005 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-16078685

RESUMO

The total flavonoids and saponins of the seeds of Glinus lotoides in the crude extracts and tablet formulation thereof were quantified by reversed-phase high-performance liquid chromatographic (RP-HPLC) methods with UV detection. The saponins were analyzed after acid hydrolysis in 3 M HCI at 100 degrees C for 1 h. Vicenin-2 and mollugogenol B were isolated and used as reference substances for the quantification of total flavonoids and saponins, respectively. The identity and purity (> 97%) of the standards were confirmed by spectroscopic (UV, MS, and NMR) and chromatographic (HPLC) methods. The flavonoids and saponins of the crude extract of the seeds and tablet formulation were separated by RP-HPLC (Nucleosil RP-18 column, 250 mm x 4.6 mm) using linear gradient elution systems of acetonitrile-water-0.1 M H3PO4 for flavonoids and methanol-water for saponins. Satisfactory separation of the compounds was obtained in less than 30 and 25 min, for the flavonoids and saponins, respectively. The methods were validated for linearity, repeatability, limits of detection (LOD) and limits of quantification (LOQ). Repeatability (inter- and intra-day, n = 6 and 9, respectively) showed less than 2% relative standard deviation (RSD). The LOD and LOQ were found to be 0.075 and 0.225 mg/mL, respectively, for vicenin-2 and 0.027 and 0.082 mg/100 mL, respectively, for mollugogenol B. The content of flavonoids and saponins of six single tablets was between 95 and 103% for flavonoids and 94-98% for saponins. The validated HPLC methods were employed to standardize a fingerprint of a laboratory produced purified extract, which could be used as a secondary standard for the routine quality control. Accordingly, the purified extract was found to contain 21.3% flavonoids (vicenin-2, 10%) and 25.4% saponins (glinuside G, 14.2%).


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/análise , Molluginaceae/química , Saponinas/análise , Sementes/química , Apigenina/análise , Flavonoides/isolamento & purificação , Glucosídeos/análise , Padrões de Referência , Saponinas/isolamento & purificação , Comprimidos/química
13.
J Ethnopharmacol ; 101(1-3): 204-14, 2005 Oct 03.
Artigo em Inglês | MEDLINE | ID: mdl-15996844

RESUMO

Glinus oppositifolius (L.) Aug. DC. (Aizoaceae) is a Malian medicinal plant used against various types of illnesses related to the immune response, like joint pains, inflammations, fever, malaria and wounds. Two pectin type polysaccharides, GOA1 and GOA2, being isolated from a 50 degrees C water extract from the aerial parts of Glinus oppositifolius were investigated for their activity towards the complement system and different leukocyte subsets because of the assumed effects on conditions related to the immune system. The polysaccharide polymer in GOA1 was shown to contain considerable amounts of the neutral sugars arabinose (26.4 mol%) and galactose (42.9 mol%), and methylation analysis indicated the presence of arabinogalactans type I (AG-I) and type II (AG-II). GOA2 was rich in galacturonic acid (68.3 mol%), along with rhamnose, arabinose and galactose. Structural studies indicated that rhamnose and galacturonic acid might constitute a rhamnogalacturonan backbone, often found in pectic substances, with side chains consisting of arabinose and galactose. Both GOA1 and GOA2 were shown to exhibit potent dose-dependent complement fixating activities, and induced chemotaxis of macrophages, T cells and NK cells.


Assuntos
Molluginaceae/química , Pectinas/isolamento & purificação , Aminoácidos/análise , Carboidratos/análise , Quimiotaxia/efeitos dos fármacos , Testes de Fixação de Complemento , Humanos , Peso Molecular , Óxido Nítrico/análise , Pectinas/análise , Pectinas/química , Pectinas/farmacologia , Proteínas/análise
14.
Pharmazie ; 59(1): 34-8, 2004 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-14964419

RESUMO

Extraction methods were standardised for saponin-containing extracts from the seeds of Glinus lotoides and the effects of some extraction process variables, such as the extracting solvent (various concentrations of methanol in water) and method of extract drying (freeze-drying and vacuum oven-drying), on the physical properties of the extracts were investigated. Physicochemical properties, namely particle size and size distribution, morphology, water uptake profiles and sorption isotherms, densities, flow properties and compaction profiles, of the crude dry extracts of 60% methanol (extract A), 70% methanol (extract B) and 80% methanol (extract C) were investigated. The average particle sizes (X50) of extracts A, B and C were found to be 68.4, 92.1 and 68.5 microm, respectively. Scanning electron micrographs of freeze-dried and vacuum oven-dried extract A showed that the particles are irregular in shape and are compact masses with sharp edges. The percent water uptake by the crude extracts was found to increase with an increase in relative humidities, while the hygroscopicity increased with decreasing methanol ratio of the extracting solvent. The bulk and the true densities of the three extracts (A, B and C) ranged from 0.66 to 0.67 and 1.49 to 1.50 g/ml, respectively. The tapped density (0.94 g/ml) and hence the porosity (56.0%), Carr's index (29.8%) and Hausner ratio (1.42) of extract A were greater than those of extracts B and C. Measurements of angle of repose indicated that all of the extracts exhibit poor flow properties. Compaction studies revealed that extract C has higher compactibility than extracts A and B.


Assuntos
Molluginaceae/química , Absorção , Fenômenos Químicos , Físico-Química , Liofilização , Lipídeos/análise , Microscopia Eletrônica de Varredura , Tamanho da Partícula , Extratos Vegetais/química , Padrões de Referência , Saponinas/química , Sementes/química , Solventes , Água/química
15.
BMC Res Notes ; 7: 220, 2014 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-24713133

RESUMO

BACKGROUND: The negative impact of synthetic molluscicides on the environment and their high cost necessitated search for an alternative approach of using plant extracts for the control of schistosomiasis. The objective of this study was, therefore, to evaluate aqueous and ethyl acetate crude extracts of Glinus lotoides fruits for their cercariacidal activity and molluscicidal effect against schistosome snail intermediate hosts. METHODS: Assessment of the molluscicidal activity against Biomphalaria pfeifferi was made by immersion method in accordance with WHO guideline. The results of mortality were statistically analyzed using probit analysis. The attenuating effect of the plant on Schistosoma mansoni cercariae was determined using establishment of adult worms as a parasitological parameter post exposure. RESULTS: The 24 and 48 hour-LC50 values for the aqueous extract of G. lotoides fruits were 47.1 and 44.1 mg/L, respectively, whereas that of ethyl acetate were 66.1 and 59.6 mg/L, respectively. The 24 and 48 hour LC90 values for the aqueous extract of G. lotoides fruits were 56.96 and 51.0 mg/L, respectively, while that of ethyl acetate were 77.2 and 70.0 mg/L, respectively. The in vitro cercariacidal activity was determined after 2 hrs of exposure to the aqueous plant extract. It was found out that the LC50 and LC90 values were 18.7 and 41.7 mg/L, respectively. Besides, infectivity of Schistosoma mansoni cercariae to mice was determined by exposing mice to cercariae pre-treated with the sub-lethal concentrations (3.7, 11.6 and 18.7 mg/L) of the aqueous extract. A significant reduction in worm burden in mice was obtained at 11.6 mg/L (p < 0.05). Moreover, the reduction in number of worms recovered was highly significant at 18.7 mg/L (p < 0.001). CONCLUSIONS: The results showed that G. lotoides has molluscicidal activity against B. pfeifferi snails and cercariacidal activity against S. mansoni. Yet, further comprehensive evaluation is recommended for the possible use of G. lotoides against B. pfeifferi and the schistosome parasite.


Assuntos
Anti-Helmínticos/farmacologia , Molluginaceae/química , Moluscocidas/farmacologia , Extratos Vegetais/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Acetatos , Animais , Biomphalaria/efeitos dos fármacos , Biomphalaria/fisiologia , Feminino , Frutas/química , Dose Letal Mediana , Masculino , Camundongos , Schistosoma mansoni/crescimento & desenvolvimento , Esquistossomose mansoni/tratamento farmacológico , Esquistossomose mansoni/parasitologia , Solventes , Água
16.
Nat Prod Res ; 27(7): 624-9, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22594571

RESUMO

Evaluation of α-glucosidase inhibitory activity led to the isolation of six triterpene saponins from the aerial parts of Glinus oppositifolius including one new and five known constituents. The structure of the new saponin, glinoside C (1), was established as 16-O-(ß-D-glucopyranosyl)-3ß,12ß,16ß,21α,22-pentahydroxy hopane by extensive use of 1-D, 2-D NMR and mass spectral techniques. The other constituents identified were 3-O-(ß-D-xylopyranosyl)-spergulagenin A (2), spergulacin (3), spergulin A (4), spergulacin A (5) and spergulin B (6). Compound 1 exhibited the greatest inhibition of the enzyme with IC50 of 127 ± 30 µM. Kinetics study for the compound 1 demonstrated mixed type of inhibition (Ki = 157.9 µM).


Assuntos
Inibidores de Glicosídeo Hidrolases , Molluginaceae/química , Saponinas/química , Triterpenos/química , Triterpenos/farmacologia , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Saponinas/farmacologia
17.
Asian Pac J Trop Med ; 5(11): 862-7, 2012 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23146799

RESUMO

OBJECTIVE: To evaluate the protective effect of ethanol extract of Mollugo nudicaulis (M. nudicaulis) against perchloroethylene-induced hepatotoxicity. METHODS: The hepatoprotective activity of the ethanol extract of M. nudicaulis (200 mg/kg body wt) was studied in percholoroethylene (1 000 mg/kg body wt) induced hepatotoxicity in Wistar albino rats. The serum levels of AST, ALT, ALP, bilirubin and the liver content of SOD, CAT, GPx, GST, GSH, vitamin C were assessed to evaluate the hepatoprotective and antioxidant activities of the extract. The activity of the extract was compared with silymarin, a standard reference drug. In addition, serum urea, uric acid and creatinine levels were measured to evaluate the kidney function. The histopathological examination of the liver tissues was observed to support the biochemical parameters. RESULTS: The results revealed that the extract significantly (P<0.05) restored the serum levels of AST, ALT, ALP, bilirubin and significantly (P<0.05) increased the antioxidant enzymes SOD, CAT, GPx, GST, GSH, vitamin C in perchloroethylene-induced rats to its normalcy. The biochemical observations were supported by the histopathological studies of the liver tissues. CONCLUSIONS: The results led to the conclusion that M. nudicaulis possess hepatoprotective and antioxidant activities against perchloroethylene-induced hepatotoxicity in rats.


Assuntos
Antioxidantes/administração & dosagem , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Molluginaceae/química , Extratos Vegetais/administração & dosagem , Tetracloroetileno/toxicidade , Animais , Antioxidantes/isolamento & purificação , Doença Hepática Induzida por Substâncias e Drogas/patologia , Creatinina/sangue , Enzimas/sangue , Feminino , Histocitoquímica , Fígado/enzimologia , Extratos Vegetais/isolamento & purificação , Ratos , Ratos Wistar , Resultado do Tratamento , Ureia/sangue , Ácido Úrico/sangue
18.
J Nutr Sci Vitaminol (Tokyo) ; 56(5): 311-8, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-21228502

RESUMO

The purpose of this study is to determine the anticancer activity and the nutritional values of the seeds of Glinus lotoides, a plant used as a dietary vegetable and medicinal plant in Asia and Africa. To achieve this goal, the seeds were extracted in soxhlet using solvents, namely n-hexane, dichloromethane, methanol and water. The methanol and n-hexane extracts showed differential growth inhibitory responses in carcinoma cell lines (Calu-3 IC(50)=29.7 and 79.8 µg/mL and Caco-2 IC(50)=69.7 and 74.6 µg/mL, respectively) as compared to normal cell lines (MDCK IC(50)=106.1 and 131.1 µg/mL and IEC-6 IC(50)=134.0 and 128.5 µg/mL, respectively). In addition, these extracts induced significant apoptosis in the cancer cells (p<0.05) at 100 µg/mL. The seeds of G. lotoides were found to contain nutritional compounds of well-established chemopreventive activity, including vitamin E, folic acid, selenium and calcium. The hydrophilic oxygen radical absorption capacity (ORAC) value was found to be 123 µM Trolox Equiv./g, indicating the antioxidant activity of the plant. These data suggest that the seeds of G. lotoides could potentially be used in the diet in chemoprevention of cancer and warrant further confirmatory preclinical and clinical studies. The amount of protein, carbohydrate, fat, ash, moisture, sugar profile and fatty acids further support the nutritional value of the seeds.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Molluginaceae/química , Extratos Vegetais/farmacologia , Sementes/química , África , Animais , Antioxidantes/farmacologia , Apoptose , Ásia , Linhagem Celular Tumoral , Quimioprevenção , Cães , Humanos , Medicinas Tradicionais Africanas , Valor Nutritivo , Ratos , Solventes/metabolismo , Verduras/química
19.
J Nat Prod ; 68(3): 443-6, 2005 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-15787456

RESUMO

Four new hopane-type saponins, glinusides F, G, H, and I (1-4), and the known succulentoside B (5), as well as the two known flavones 5,7,4'-trihydroxyflavone-6,8-di-C-glucoside (vicenin-2) and 5,7,4'-trihydroxyflavone-8-C-sophoroside (vitexin-2' '-O-glucoside), were isolated from the seeds of Glinus lotoides growing in Ethiopia. On the basis of the spectroscopic data analysis, including 2D NMR and HRESIMS, the new structures were characterized as 3beta-O-beta-D-xylopyranosyl-6alpha-O-beta-D-xylopyranosyl-16beta-O-beta-D-xylopyranosyl-22-hydroxyhopane (1), 3beta-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-xylopyranosyl-6alpha,16beta-dihydroxy-22-O-alpha-L-rhamnopyranosylhopane (2), 3beta-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-xylopyranosyl-6alpha-O-beta-D-xylopyranosyl-16beta-hydroxy-22-O-alpha-L-rhamnopyranosylhopane (3), and 3beta-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-d-xylopyranosyl-6alpha-O-beta-D-xylopyranosyl-16beta-O-beta-D-xylopyranosyl-22-hopane (4).


Assuntos
Molluginaceae/química , Plantas Medicinais/química , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , Etiópia , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Saponinas/química , Sementes/química , Triterpenos/química
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