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Homalium tomentosum (Vent.) Benth, is a valuable agroforestry species and has industrial importance high-quality wood is used for malas, the manufacture of matches, and is suitable for making a wide range of articles. Nevertheless, leaves and bark are relatively rich in phenols and flavonoids, used for medicinal purposes. In this study, phenols and flavonoids rich in bio-privileged antioxidants in ethyl-acetate extracted fractions of bark (HTEB), and leaves (HTEL) at 300, and 400 mg/kg were examined in carbon tetrachloride (CCl4)-induced hepatotoxicity in experimental rats. HTEB and HTEL (400) showed improvement in liver structural integrity, but, HTEB400 significantly improved serum (total protein, TP; alkaline phosphatase, ALP; total bilirubin, TB; serum glutamate oxaloacetate transaminase, SGOT, and serum glutamate pyruvate transaminase, SGPT), and hepatic oxidative (catalase, CAT; thiobarbituric acid reactive species, TBARS; reduced glutathione, GSH; superoxide dismutase, SOD), and inflammatory (transforming growth factor, TGF-ß; ineterleukin-6, IL-6) biomarkers accompanied by histopathological improvements of the liver. GC-MS analysis of HTEB and HTEL identified 14 and 18 compounds, but physicochemical properties of 3-major antioxidants of HTEB (levoglucosenone, (+)-borneol, α-N-normethadol), and HTEL (2-coumaranone, salicyl alcohol, D-allose) were satisfied for the parameters molecular weight, no. of H-acceptor and H-donor, partition co-efficient (clogP), and topological polar surface area (tPSA) of Lipinski's rule. ADME-Tox properties were directly related to the biological activities of HTEB and HTEL. Molecular docking investigation of α-N-normethadol showed the highest binding energy against TGF-ß and IL-6 than other antioxidants. HTEB and HTEL were powerful antioxidant potential, but levoglucosenone, (+)-borneol, and α-N-normethadol of HTEB demonstrated better activities in neutralizing reactive oxygen species (ROS) to preserve cellular membrane integrity in liver cirrhosis as found evidence in restoring the liver inflammatory cytokines. This study confirmed the economic interest of H. tomentosum bark as crude material for the preparation of biobased materials for the pharmaceutical and food industries.
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Antioxidantes , Fígado , Extratos Vegetais , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Animais , Fígado/efeitos dos fármacos , Fígado/patologia , Fígado/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Ratos , Masculino , Tetracloreto de Carbono , Ratos Wistar , Simulação de Acoplamento Molecular , Doença Hepática Induzida por Substâncias e Drogas/patologia , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Estresse Oxidativo/efeitos dos fármacos , Folhas de Planta/química , Necrose , Casca de Planta/químicaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Homalium zeylanicum (Gardner) Benth (Salicaceae) leaves are being used as folklore medicine to treat diabetes by the local folk of Andhra Pradesh, India. The medicinal claim of this plant with hypoglycaemic effects was initially studied by the authors. Results demonstrated the important antioxidant activities of the hydroalcohol fraction of leaves of H. zeylanicum leaves (HAHZL) were positively correlated with phenols and flavonoids contents. AIM OF THE STUDY: Based on the previous findings, additional research is needed to examine the efficacy of using HAHZL to treat hyperglycemia. We therefore investigated in vitro and in vivo glycemic response of HAHZL, and evaluation of possible mechanism of bioactive molecules in mitigating streptozotocin-induced cellular stress in experimental rats via attenuation of oxidative stress imparts inflammation. METHODS: GC-MS/MS analysis of HAHZL was carried out to identify bioactive constituents. In vitro antidiabetic (α-glucosidase, α-amylase) and anti-inflammatory activities were investigated. HFD/low-STZ-prompted diabetic Wistar rats were administered with HAHZL (300 and 400 mg/kg; oral) for 28 days. Blood serum, oxidative stress, inflammation, DNA damage, and antidiabetic markers of pancreas and liver were determined. Histopathological studies of liver and pancreas were performed to assess the protective role of HAHZL. RESULTS: GC-MS/MS study revealed 7 bioactive compounds e.g., Phenol, 4-ethenyl-, acetate (28.68%), hydroquinone (9.10%), n-hexadecanoic acid (0.55%), phytol (0.57%), arbutin (17.65%), Vitamin E (1.04%), ß-Sitosterol (1.54%) which possess antioxidant, anti-inflammatory and anti-diabetic activities. HAHZL showed significant in vitro glycemic response as evidenced by the inhibition of α-amylase, and α-glucosidase activities. Lineweaver-Burk plot revealed that HAHZL exhibited competitive and mixed competitive inhibition towards α-amylase and α-glucosidase, respectively. HAHZL at 400 mg/kg modulated the pathophysiology associated with HFD/STZ-induced type2 diabetes mellitus and significantly (p < 0.001) improved antihyperglycemic (SG, SI, HOMA-IR, and HbA1C), antidyslipidemic (TC, HDL-C, LDL-C, and TG), antioxidative (MDA, SOD, CAT, GSH, and 8-OHdG) and anti-inflammatory (TNF-α, and CRP) markers in serum, pancreas and liver. In vitro and in vivo test results were corroborated by the improvement of pancreatic and hepatic tissue architecture in diabetic rats. CONCLUSION: HAHZL bearing bioactive components phenol, 4-ethenyl-,acetate, hydroquinone, n-hexadecanoic acid, arbutin, phytol, vitamin E and ß-sitosterol balanced glycemic level by normalising the levels of glycaemic indices, lipid profile, pancreas and liver functional markers in STZ-induced T2DM rats.
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Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Salicaceae/química , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Relação Dose-Resposta a Droga , Feminino , Hipoglicemiantes/isolamento & purificação , Inflamação/tratamento farmacológico , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Ratos , Ratos Wistar , EstreptozocinaRESUMO
Phytochemical investigation of the aerial parts of Homalium cochinchinensis led to the isolation of secondary metabolites belonging to the spermidine alkaloid, glycoside, depsidone and phenol classes. Of the eleven secondary metabolites isolated in this study, two spermidine alkaloids, dovyalicins H (1) and I (2), which belong to a rare group among this class, and six glycosides (3-8) are previously undescribed. The structures of all new isolates were determined by interpretation of spectroscopic and spectrometric data. In this report, the structural elucidation of these unprecedented secondary metabolites (1-8) is described.
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The phytochemical investigation of the stems of Homalium stenophyllum afforded seven new phenolic glycosides (1-5 and 8-9) and two known compounds (6 and 7). Their structures were elucidated by comprehensive analyses of NMR spectroscopic, mass spectrometric data and chemical hydrolysis. Additionally, their anti-inflammatory activities against the NO production in LPS-induced macrophages were evaluated.
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Glicosídeos , Fenóis , Salicaceae/química , Anti-Inflamatórios/farmacologia , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Macrófagos/efeitos dos fármacos , Estrutura Molecular , Fenóis/isolamento & purificação , Fenóis/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Caules de Planta/químicaRESUMO
The phytochemical investigation of the stems of Homalium stenophyllum afforded seven new phenolic glycosides (1-5 and 8-9) and two known compounds (6 and 7). Their structures were elucidated by comprehensive analyses of NMR spectroscopic, mass spectrometric data and chemical hydrolysis. Additionally, their anti-inflammatory activities against the NO production in LPS-induced macrophages were evaluated.
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ETHNOPHARMACOLOGICAL RELEVANCE: Homalium zeylanicum (Gardner) Benth. is a medicinal plant traditionally used in controlling diabetes which thus far has been assessed by the authors only to a very limited extent. PURPOSE: To fill the research gap in the literature review, we investigated the antihyperglycemic effects of hydro alcohol fraction of bark of H. zeylanicum (HAHZB) by modulating oxidative stress and inflammation in high-fat diet fed-streptozotocin (HFD/STZ)-induced type-2 diabetic rats. MATERIALS AND METHODS: To understand the antioxidant capacity of HAHZB, oxygen radical absorbance capacity (ORAC) and cell-based antioxidant protection in erythrocytes (CAP-e) were performed. GC-MS/MS analysis was performed to assess the bioactive components in HAHZB. HFD/STZ-induced diabetic rats were treated orally with HAHZB (300 and 400 mg/kg) for 28 days. After the end of the experiment, marker profiling and histopathological observation of blood and pancreas were examined. The study also highlights interaction between diabetes, oxidative stress and inflammation by examining the increased pro-inflammatory cytokines e.g. TNF-α and C-reactive protein (CRP) promotes DNA damage e.g. oxidation of 8-hydroxy-2-deoxyguanosine (8-OHdG) in chronic hyperglycaemia. RESULTS: In ex vivo cellular antioxidant capacity of -CAP-e and ORAC assays, HAHZB showed remarkable free radical scavenging ability in a dose dependent manner. GC-MS/MS analysis identified 28 no. of compounds and out of which, oleic acid (1.03%), ethyl tridecanoate (11.77%), phytol (1.29), 9,12-octadecadienoic acid, methyl ester, (E,E)-(5.97%), stigmasterol (1.30%) and ß-sitosterol (2.86%) have antioxidant, anti-inflammatory and anti-diabetic activities. HAHZB 400 mg/kg significantly (p < 0.001) improved the lipid profile (TC: 74.66 ± 0.59, HDL-C: 22.08 ± 0.46, LDL-C: 38.06 ± 0.69, and TG: 171.92 ± 1.01 mg/dL) as well as restoring antidiabetic markers (SG: 209.62 ± 1.05 mg/dL, SI: 15.07 ± 0.11 µIU/mL, HOMA-IR: 7.79 ± 0.04 %, and HbA1C: 8.93 ± 0.03 %) and renal functional markers (Tg: 291.26 ± 0.57 pg/mL, BUN: 23.79 ± 0.14 mg/dL, and Cr: 1.34 ± 0.04 mg/dL) in diabetic rats. Oxidative stress markers of pancreas (MDA: 3.65 ± 0.17 nM TBARS /mg protein, SOD: 3.14 ± 0.28 U/mg protein, CAT: 7.88 ± 0.23 U/mg protein, GSH: 12.63 ± 0.28 µM/g of tissue) were restored to normal as evidenced by histological architecture of pancreatic islet cells. The increased level of pro-inflammatory cytokines and oxidative DNA damage were significantly restored (TNF-α: 54.48 ± 3.19 pg/mL, CRP: 440.22 ± 7.86 ng/mL, and 8-OHdG: 63.65 ± 1.84 ng/mL) by HAHZB in diabetic rats. CONCLUSION: The present findings confirm that the presence of bioactive compounds in HAHZB exert therapeutic protective effect by decreasing oxidative, inflammation and pancreatic ß-cell damage in oxidative stress induced diabetic rats.
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Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/farmacologia , Células Secretoras de Insulina/efeitos dos fármacos , Extratos Vegetais/farmacologia , Salicaceae , 8-Hidroxi-2'-Desoxiguanosina/sangue , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Biomarcadores/sangue , Glicemia/metabolismo , Citocinas/sangue , Dano ao DNA , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/patologia , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/induzido quimicamente , Diabetes Mellitus Tipo 2/patologia , Dieta Hiperlipídica , Feminino , Hipoglicemiantes/isolamento & purificação , Mediadores da Inflamação/sangue , Células Secretoras de Insulina/metabolismo , Células Secretoras de Insulina/patologia , Masculino , Estresse Oxidativo/efeitos dos fármacos , Casca de Planta , Extratos Vegetais/isolamento & purificação , Ratos Wistar , Salicaceae/química , EstreptozocinaRESUMO
Commonly used to treat skin injuries in Asia, several Homalium spp. have been found to promote skin regeneration and wound healing. While ethnobotanical surveys report the use of H. bhamoense trunk bark as a wound salve, there are no studies covering bioactive properties. As impaired cutaneous healing is characterized by excessive inflammation, a series of inflammatory mediators involved in wound healing were targeted with a methanol extract obtained from H. bhamoense trunk bark. Results showed concentration-dependent inhibition of hyaluronidase and 5-lipoxygenase upon exposure to the extract, with IC50 values of 396.9 ± 25.7 and 29.0 ± 2.3 µg mL-1, respectively. H. bhamoense trunk bark extract also exerted anti-inflammatory activity by significantly suppressing the overproduction of interleukin 6 (IL-6) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages at concentrations ranging from 125 to 1000 µg mL-1, while leading to a biphasic effect on nitric oxide (NO) and tumor necrosis factor alpha (TNF-α) levels. The phenolic profile was elucidated by HPLC-DAD, being characterized by the occurrence of ellagic acid as the main constituent, in addition to a series of methylated derivatives, which might underlie the observed anti-inflammatory effects. Our findings provide in vitro data on anti-inflammatory ability of H. bhamoense trunk bark, disclosing also potential cutaneous toxicity as assessed in HaCaT keratinocytes.
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Anti-Inflamatórios/farmacologia , Interleucina-6/efeitos adversos , Lipopolissacarídeos/efeitos adversos , Macrófagos/efeitos dos fármacos , Medicina Tradicional/métodos , Nephropidae/química , Extratos Vegetais/farmacologia , Animais , Araquidonato 5-Lipoxigenase/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citocinas/metabolismo , Medicina Herbária , Hialuronoglucosaminidase/efeitos dos fármacos , Hidroxibenzoatos , Mediadores da Inflamação/farmacologia , Concentração Inibidora 50 , Interleucina-6/metabolismo , Queratinócitos , Lipopolissacarídeos/metabolismo , Camundongos , Óxido Nítrico/metabolismo , Células RAW 264.7 , Fator de Necrose Tumoral alfaRESUMO
Phenyl myristate was isolated from Homalium nepalense, which is known for its therapeutic virtues in traditional medicine. However, the study of radical scavenging-capacity of phenyl myristate is limited by its relatively low abundance in medicinal plants. We have studied the isolation, structure-elucidation, and bioactivities of high-performance thin-layer chromatography validated phenyl myristate from hydroalcohol-extract of bark of H. nepalense. The chemical structure of phenyl myristate was elucidated by spectroscopic methods. The chromatography was performed on high-performance thin-layer chromatography aluminum plates coated with silica-gel 60 F254 . Determination and quantitation of phenyl myristate were performed by densitometric-scanning at 254 nm (chloroform-methanol, 9:1, v/v; Rf 0.49). The method was validated according to International Council for Harmonisation guidelines in terms of linearity, specificity, sensitivity, accuracy, precision, robustness, and stability. Linearity-range of phenyl myristate was 100-500 ng/5 µL with correlation-coefficient r2 = 0.9997. Limits of detection and quantitation were 3.35 and 10.17 ng, respectively. Phenyl myristate showed significant free-radical-scavenging activities in 2,2-diphenyl-1-picrylhydrazyl, oxygen-radical-absorbance-capacity, and ex vivo cell-based-antioxidant-protection-in-erythrocytes assays. Molecular-docking approach of phenyl myristate showed effective binding at active sites of human serum albumin (HSA) with the lowest binding energy (-8.4 kcal/mol) that was comparable with ascorbic acid (-5.0 kcal/mol). These studies provide mechanistic insight into the potential free radical scavenging activities of phenyl myristate.
Assuntos
Sequestradores de Radicais Livres/análise , Simulação de Acoplamento Molecular , Ácido Mirístico/análise , Extratos Vegetais/análise , Salicaceae/química , Compostos de Bifenilo/antagonistas & inibidores , Cromatografia em Camada Fina , Eritrócitos/efeitos dos fármacos , Sequestradores de Radicais Livres/farmacologia , Humanos , Estrutura Molecular , Ácido Mirístico/farmacologia , Picratos/antagonistas & inibidores , Extratos Vegetais/farmacologiaRESUMO
Homalium hainanense is a large evergreen tree species belonging to Salicaceae family, and its wood is tough, fine-grained, which makes it a good source of commercial use for building construction and furniture manufacturing. In this study, we sequenced the complete chloroplast genome of H. hainanense based on next generation sequencing and used these data to assess genomic resources. The size of the H. hainanense chloroplast genome was 157,852 bp, including a large single-copy region (85,888 bp), a small single-copy region (16,592 bp), and a pair of inverted repeats regions (27,686 bp). The overall GC content of the H. hainanense chloroplast genome was 36.6%. The plastome of H. hainanense was predicted to contain 112 unique genes, including 78 protein coding genes, 30 tRNA genes and 4 rRNA genes. The reconstructed phylogeny revealed that Homalium was monophyletic and H. hainanense was sister to H. stenophyllum, H. paniculiflorum and H. racemosum.
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Objective is to evaluate the ameliorative effects of Homalium zeylanicum in carbon tetrachloride-induced oxidative stress and liver injury in rats. To establish the nature of antioxidant principles in the bioactive ethyl acetate fractions of bark (HZEB) and leaf (HZEL); oxygen radical absorbance capacity (ORAC) and cell-based antioxidant protection in erythrocytes (CAP-e) assays were performed. From acute toxicity study, HZEB and HZEL at 200 and 300 mg/kg b.w., were relatively safe at their effective doses. The degree of protection was measured by using biochemical parameters such as serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), alkaline phosphatase (ALP), total bilirubin (TB) and total protein (TP) contents. Hepatic markers e.g. thiobarbituric acid reactive species (TBARS), superoxide dismutase (SOD), catalase (CAT) and reduced glutathione (GSH) were evaluated along with histopathological observations of liver tissues. Both fractions showed significant improvement in restoring SGOT, SGPT, ALP, TB and TP level. TBARS, SOD, CAT and GSH levels were significantly altered towards normal values. Both fractions at 300 mg/kg showed remarkable improvement in liver markers as compared to silymarin. Histopathological examinations showed reduction in hepatic necrosis and appeared normal hepatocellular architecture in HZEB and HZEL treated groups. In CAP-e assay, IC50 of HZEB (54.66 mg/mL) was higher than HZEL (60.88 mg/mL) and in ORAC assay, AUC of HZEB and HZEL were 33.46, 21.29 respectively and results were comparable with trolox. GC-MS and LC-MS analysis identified a total no. of 44 compounds. Few compounds were identified as bioactive compounds e.g. catechol (7.23%), tetraacetyl-d-xylonic nitrile (3%), oleic acid (0.49%), 2,6-bis(1,1-dimethylethyl)-phenol (3.71%), 3,4,5-trimethoxy-phenol (0.31%), and conifer alcohol (7.41%). The presence of antioxidant principles in both fractions were responsible for hepatoprotective activities, however, the presence of catechol (7.23%) in the bark part imparted better activities in protecting liver than leaf of H. zeylanicum.
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Tetracloreto de Carbono/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Animais , Doença Hepática Induzida por Substâncias e Drogas/patologia , Relação Dose-Resposta a Droga , Feminino , Masculino , Estresse Oxidativo/fisiologia , Casca de Planta , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta , Ratos , Resultado do TratamentoRESUMO
The purpose of this study was to evaluate ameliorative effects of Homalium nepalense Benth. (Flacourtiaceae) on CCl4-induced hepatocellular injury in rats. Oxygen-radical absorbance-capacity (ORAC) and cell-based-antioxidant-protection-in-erythrocytes (CAP-e) were performed and found that the ethyl acetate fractions of bark (HNEB) and leaf (HNEL) showed a remarkable degree of antioxidant activities in a dose dependent manner. Antioxidant potential HNEB was higher than HNEL and was comparable with trolox. HNEB and HNEL at 300 and 400â¯mg/kg showed significant hepatoprotective activities against CCl4-induced hepatotoxicity as evidenced by restoration of SGOT, SGPT, ALP, TB and TP level. The level of TBARS, SOD, CAT and GSH were significantly improved and restored towards normal value. Both fractions at 400â¯mg/kg showed remarkable improvements in marker levels as comparable to silymarin. Histopathological observations of liver tissues revealed the reduction of necrosis with appearance of sinusoidal space, central vein, and bile duct both in case of HNEB and HNEL. GC-MS and LC-MS confirmed occurrence of a total 53 no. of phytocompounds in HNEB and HNEL. Based on their retention times-(RT) and mass-to-charge-ratios-(m/z), some of the major bioactive compounds were catechol (5.89%), 5-hydroxymethylfurfural (5.87%), salicylic acid (4.89%), eugenol (1.60%), doconexent (0.31%), ß-sitosterol (1.59%), 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one (1.15%), coniferyl alcohol (2.99%), hexadecanoic acid methyl ester (1.05%), and betulin (1.20%). H. nepalense possesses significant hepatoprotection effect because of its antioxidant constituents.
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Antioxidantes/uso terapêutico , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Fígado/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Salicaceae/química , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/toxicidade , Biomarcadores/sangue , Tetracloreto de Carbono , Doença Hepática Induzida por Substâncias e Drogas/patologia , Relação Dose-Resposta a Droga , Feminino , Dose Letal Mediana , Fígado/patologia , Testes de Função Hepática , Masculino , Casca de Planta/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Folhas de Planta/química , RatosRESUMO
Two new phenolic glycosides (1 and 2) and two new isocoumarin glycosides (3 and 4), along with 14 known compounds (5-18), were isolated from the stems of Homalium paniculiflorum. Their structures were established on the basis of extensive spectroscopic analyses and chemical methods. All new compounds were evaluated for their anti-inflammatory activities via examining the inhibitory activity on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in mouse macrophage RAW 264.7 cells in vitro. Compounds 1 and 4 exhibited inhibitory activities with IC50 values of 30.23 ± 1.23 µM and 19.36 ± 0.19 µM, respectively.
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Glicosídeos/química , Inflamação/tratamento farmacológico , Isocumarinas/química , Salicaceae/química , Animais , Humanos , Inflamação/induzido quimicamente , Lipopolissacarídeos/toxicidade , Camundongos , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Fenol/química , Caules de Planta/química , Células RAW 264.7/efeitos dos fármacosRESUMO
A new dihydrochalcone glycoside, phloretin-4-O-ß-D-glucopyranoside (1), together with seven known flavonoids (2-8), were isolated from the stems of Homalium stenophyllum. The structure of 1 was elucidated by extensive spectroscopic methods and the known compounds were identified by comparisons with data reported in the literature. The known compounds (2-8) were isolated from the genus Homalium for the first time. All compounds were evaluated for their antibacterial activities against six pathogenic bacteria in vitro.
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Antibacterianos/química , Antibacterianos/farmacologia , Chalconas/química , Glicosídeos/química , Salicaceae/química , Antibacterianos/isolamento & purificação , Flavonoides/química , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Caules de Planta/químicaRESUMO
Homalium zeylanicum (Gardner) Benth. (Flacourtiaceae) is a medicinal plant useful in controlling rheumatism, inflammation and diabetes. The objective of this work evaluates in vitro antioxidant, antidiabetic, and antiinflammatory properties of hydroalcohol extract of bark of H. zeylanicum (HAHZ). It also describes isolation and structure determination of lucidenic acid A, which is the first report in this plant. In order to explain the role of antioxidant principles, DPPH, nitric oxide, hydroxyl, superoxide and metal chelating assays were performed. Antidiabetic and anti-inflammatory activities were investigated by quantifying α-amylase, α-glucosidase and protein denaturation inhibitory activities of HAHZ. Biochemical estimations were performed. The chemical structure of the triterpenoid was elucidated using 1H, 13C NMR and high resolution-MS. IC50 of DPPH, nitric oxide, hydroxyl, superoxide and metal chelating activities were of 36.23 ± 0.27, 40.11 ± 0.32, 35.23 ± 0.57, 43.34 ± 0.22 and 11.54 ± 0.08 µg/mL, respectively. IC50 of α-amylase and α-glucosidase activities were 29.12 ± 0.54, and 18.55 ± 0.15 µg/mL. Total phenolic and total flavonoid contents were recorded at 233.65 mg/g GAE and 172.7 mg/g QE. Regarding kinetic behaviour, HAHZ showed competitive inhibition on α-glucosidase and mixed competitive inhibition on α-amylase. Lucidenic acid A was confirmed by spectroscopic studies. Anti-inflammatory activity of lucidenic acid A was determined by using protein denaturation assay with IC50 13 µg/mL but HAHZ showed 30.34 ± 0.13 µg/mL. Phenols and flavonoids could be attributed to inhibition of intestinal carbohydrases for anti-diabetic activities whereas triterpenoids could be responsible for anti-inflammatory activity of H. zeylanicum.
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ETHNOPHARMACOLOGICAL RELEVANCE: The tropical ulcer is a debilitating bacterial infection that is common in Papua New Guinea. Deploying healthcare infrastructure to remote and inaccessible rainforest locations is not practical, therefore local plants may be the best treatment option. Here we present an ethnobotanical survey of the tropical ulcer plant medicines used by the semi-nomadic Apsokok who roam the remote central mountains of Papua New Guinea's West New Britain Province. In vitro biological activity in assays relevant to tropical ulcer wound healing is also presented. MATERIALS AND METHODS: Focus groups and semi-structured interviews were used to acquire information on the uses of plants, vouchers of which were identified by comparison with authentic herbarium specimens. Antibacterial disc diffusion assays with Staphylococcus aureus and Fusobacterium ulcerans, MMP-9 enzyme inhibition and dermal fibroblast stimulation assays were carried out on plant saps and aqueous extracts of plant material. LC-MS was used to identify known plant metabolites. RESULTS: The ethnobotanical survey identified sixteen species that were used to treat tropical ulcers, all of which were applied topically. A subset of twelve species were investigated further in vitro. Four species produced zones of inhibition with S. aureus, all 12 species provided low level inhibition of MMP-9 and 8 species stimulated dermal fibroblast proliferation, although cytotoxicity occurred at higher concentrations. The extract of Homalium foetidum Benth. inhibited S. aureus and MMP-9 while at lower sub-cytotoxic concentrations stimulated fibroblast proliferation. Trans-3-O-p-coumaroylquinic acid cis-3-O-p-coumaroylquinic acid were detected in the aqueous extract of H. foetidum. CONCLUSIONS: Topical application of plant saps to wounds results in very high localised concentrations of plant metabolites which is likely to result in inhibition of MMP proteases. H. foetidum is a candidate plant for tropical ulcer treatment in remote areas.
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Etnofarmacologia , Maconha Medicinal/uso terapêutico , Úlcera Cutânea/tratamento farmacológico , Etnicidade , Etnobotânica , Humanos , Metaloproteinase 9 da Matriz/genética , Metaloproteinase 9 da Matriz/metabolismo , Papua Nova Guiné/epidemiologia , Papua Nova Guiné/etnologia , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Úlcera Cutânea/epidemiologiaRESUMO
OBJECTIVE: Homalium letestui Pellegr (Flacourtiaceae) has been traditionally used by the Ibibios of Southern Nigeria to treat stomach ulcer, malaria and other inflammatory diseases and Yorubas of western Nigeria as an antidote. This study evaluates the hepatoprotective properties of the ethanol extract of the plant stem. MATERIALS AND METHODS: The hepatoprotective effect of the extract of the stem of the plant (200-600 mg/kg) was evaluated by the assay of liver function parameters, namely total and direct bilirubin, serum protein and albumin, total cholesterol, alanine aminotransaminase (ALT), aspartate aminotransaminase (AST), and alkaline phosphatase activities (ALP), antioxidant enzymes like superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx), reduced glutathione (GSH) and histopathological study of the liver. Also, GCMS analysis of n-butanol fraction of the extract was carried out. RESULTS: Administration of the extract of the stem of the plant caused a significant (p<0.05 - 0.001) dose-dependent reduction of high levels of liver enzymes (ALT, AST and ALP), total cholesterol, direct and total bilirubin as well as elevation of serum levels of total protein, albumin and antioxidant enzymes (SOD, CAT, GPx and GSH). Histology of the liver sections from extract and silymarin-treated animals showed reductions in the pathological features compared to the paracetamol-treated animals. The chemical pathological changes were consistent with histopathological observations suggesting marked hepatoprotective effect of the extract of H. letestui stem. GCMS analysis of n-butanol fraction revealed the presence of 16 bioactive compounds. CONCLUSION: The results show that the extract of H. letestui has hepatoprotective potential which may be due to the antioxidant activity of its phytoconstituents.
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Homalium glandulosum Tagane & V. H. Nguyen, from Vu Quang National Park in northern Vietnam, is newly described. This species is characterized by distinct glands, often stalked, at the base of the lamina and along the margin of the stipules and bracteoles. Illustrations, DNA barcodes of the two regions of rbcL and matK, and a key to the species of Homalium in Vietnam are also provided.
RESUMO
Three species of the genus Homalium - e.g. Homalium nepalense, Homalium tomentosum and Homalium zeylanicum (Flacourtiaceae) - are recorded in India which are confined to the Eastern Ghat hill ranges. While H. zeylanicum is the IUCN red-listed medium-sized tree, the other two are endangered species of medicinal significance. The antioxidant potential of leaf and bark of the plants was evaluated through successive extraction methods by using hexane, chloroform, ethyl acetate and methanol. The extracts were subjected to in vitro assays as DPPH, hydroxyl, nitric oxide and superoxide along with its biochemical estimation. Amongst all, the ethyl acetate extracts of bark is found to be most potent compared with that of the leaves. H. nepalense has the highest amount of total phenolic and flavonoid contents followed by H. tomentosum and H. zeylanicum, respectively, and significant antioxidant behaviour.
Assuntos
Sequestradores de Radicais Livres/química , Extratos Vegetais/química , Plantas Medicinais/química , Salicaceae/química , Espécies em Perigo de Extinção , Flavonoides/química , Flavonoides/isolamento & purificação , Sequestradores de Radicais Livres/isolamento & purificação , Índia , Fenóis/química , Fenóis/isolamento & purificação , Casca de Planta/química , Folhas de Planta/químicaRESUMO
OBJECTIVE: Homalium letestui Pellegr (Flacourtiaceae) is used in traditional medicine in parts of Nigeria for the treatment of malaria, ulcer, and inflammatory diseases and as an aphrodisiac. This investigation was aimed to evaluate the cytotoxic, immunomodulatory, and antileishmanial properties of stem extract and fractions of Homalium letestui (H. letestui). MATERIALS AND METHODS: Cytotoxic activity against HeLa cells was done using sulphorhodamine (SRB) method and DNA interaction activity using gel electrophoresis. Immunomodulatory activity of the extract in whole blood, neutrophils, and macrophages was also investigated using luminol/lucigenin-based chemiluminescence assay. The extract and fractions were similarly screened for antileishmanial activity against promastigotes of Leishmania major in vitro. The GCMS analysis of the most active fraction against HeLa cells was carried out. RESULTS: The stem extract exerted prominent cytotoxic activity with the dichloromethane fraction exhibiting the most pronounced effect (GI50 -5.12±1.45 µg/ml, LC50- 57.3±2.33 µg/ml, TGI -12.6±0.87 µg/ml). The crude extract and the fractions did not interact with DNA when investigated using electrophoresis. The extract significantly ((p<0.05 - 0.001) inhibited oxidative burst activity in whole blood (-27.90-66.90%), isolated polymorphonuclear cells (PMNs) (16.50-67.0%), and mononuclear cells (MNCs) (4.31-98.50%) when two different phagocytosis activators (serum opsonizing zymosan-A and PMA) were used. The extract also exhibited moderate antileishmanial activity against promastigotes of Leishmania major in vitro. GCMS analysis of active fraction revealed pharmacologically active compounds. CONCLUSION: These results suggest that the stem extract/fractions of H. letestui possess cytotoxic, immunomodulatory, and antileishmanial activities.