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1.
J Ethnopharmacol ; 252: 112565, 2020 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-31935495

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Vincetoxicum arnottianum (Wight) Wight (Family Apocynaceae) are used by local communities for inflammation, healing of wound and injuries and also for urticaria. AIM OF STUDY: Extract/fractions of V. arnottianum were evaluated for potential anti-inflammatory activity in rat. METHODS: Methanol extract of aerial parts of V. arnottianum (VAM) was partitioned on polarity for n-hexane (VAH), ethyl acetate (VAE), butanol (VAB) and aqueous (VAA) fractions. The extract/fractions were evaluated during in vitro assay for protection against heat induced protein denaturation and Carrageenan induced paw inflammation in rat. VAM and VAE were evaluated for anti-inflammatory potential against formalin and Freund's complete adjuvant (FCA) induced inflammation in paw of rat while croton oil induced inflammation in ear of rat, respectively. The level of inflammatory mediators; IL-17, IL-1ß, IL-6, TNF-α and nitric oxide (NO) was estimated in serum of rat. RESULTS: All the extract/fractions used in this study exhibited anti-inflammatory activity. However, VAE (300 mg/kg) exhibited potential anti-inflammatory activity in carrageenan (78.06 ± 4.6%), formalin (54.71 ± 0.34%) and croton oil (73.12 ± 1.9%) induced edema in rat. In FCA induced inflammation model VAM and VAE showed admiring proficiencies against alteration of body weight and organ weight indices, paw edema and histological studies. In serum increased level of pro-inflammatory cytokines (IL-1ß, TNF-α, IL-6, IL-17) and NO during adjuvant-induced inflammation were more efficiently restored with VAE treatment to rat. Presence of polyphenolics; rutin, gallic acid, caffeic acid, apigenin, myricetin and quercetin was indicated in VAE. CONCLUSION: The results suggest the presence of anti-inflammatory constituents in V. arnottianum.

2.
Pak J Pharm Sci ; 32(4(Supplementary)): 1797-1803, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31680075

RESUMO

Leukemia is a type of blood cancer where abnormal and immature leucocytes are produced in the bone marrow. Methadone hydrochloride is a man-made drug that is commonly used in the maintenance treatment for drug addiction. The objective of this research was to determine the cytotoxic activity and apoptotic effects of methadone hydrochloride treatment towards two leukemia cell lines which are CCRF-CEM and HL-60. CCRF-CEM and HL-60 cells were treated with methadone hydrochloride for 24 and 48 hours to determine the cytotoxic activity. IC50 at 24 hours obtained for CCRF-CEM was 121.6µmol/L while IC50 for HL-60 cells was 97.18µmol/L. Result obtained from DNA fragmentation assay showed no characteristic DNA ladder pattern in CCRF-CEM leukemia cells treated with methadone hydrochloride. Characteristics DNA ladder pattern was observed in methadone hydrochloride treated HL-60 cells. Formation of comets was seen in methadone hydrochloride treated CCRF-CEM and HL-60 cells with varying degree of DNA damage. The comets formed by methadone hydrochloride treated HL-60 cells were more prominent as compared to methadone-treated CCRF-CEM cells. The expression of apoptotic-related proteins in methadone-treated CCRF-CEM and HL-60 cells were checked by incubating the cell lysate with Raybio® Human Apoptosis Antibody Array. Significant alterations in expression level of apoptosis-related proteins in methadone hydrochloride treated CCRF-CEM cells were found involving upregulation of caspase-8 expression and downregulation of survivin expression. Methadone hydrochloride induced apoptosis in HL-60 cells involved upregulation of Bid and caspase-8 expression and downregulation of Bcl-2, p21 and survivin expression.

3.
IUBMB Life ; 71(10): 1418-1427, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31169978

RESUMO

Altered enzymatic machineries are a substantial biochemical characteristic of tumor cell metabolism that switch metabolic profile from oxidative phosphorylation to amplified glycolysis as well as increased lactate production under hypoxia conditions. Reprogrammed metabolic profile is an emerging hallmark of cancer. Overexpression of several glycolytic enzymes and glucose transporters has been reported in 24 different types of cancers that represent approximately 70% of all the cancer cases around the globe. Thus, targeting glycolytic enzymes could serve as tempting avenue for drug design against cancer. Phosphoglycerate mutase 1 (PGAM1) is an important glycolytic enzyme that catalyzes the conversion of 3-phosphoglycerate to 2-phosphoglycerate. Recent investigations have revealed the overexpression of PGAM1 in several human cancers that is linked with tumor growth, survival, and invasion. The aim of this review is to update scientific research network with cancer-specific role of PGAM1 to elucidate its capability as bonafide therapeutic target for cancer therapy. Moreover, we have also summarized the reported genetic and pharmacological inhibitors of PGAM1. This study suggests that further investigations on PGAM1 should focus on the exploration of molecular mechanisms of PGAM1 overexpression in development of cancer, assessment of biosafety profiles of known inhibitors of PGAM1, and utilization of PGAM1 inhibitors in combinatorial therapies. These future studies will surely support the unbiased strategies for the development of novel PGAM1 inhibitors for cancer therapies.

4.
Pak J Pharm Sci ; 31(4(Supplementary)): 1475-1484, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30058538

RESUMO

Roots, bark, stem/twigs, and leaves of Fraxinus xanthoxyloides are being used regionally for the cure of malaria, jaundice, internal injuries, pneumonia, pain, rheumatism and also in fracture of bones. Our objective was to assess the methanolic leaves extract of F. xanthoxyloides for its antioxidant capability against oxidative stress induced by carbon tetrachloride (CCl4) in the kidney of Sprague-Dawley rats. Duration of this experiment was 30 days and doses were given on alternative days. Urine of rats was assessed for kidney function and renal tissues for antioxidant enzymes activity, biochemical markers, comet assay and histopathology. Enhanced urinary creatinine, urobilinogen levels and decreased creatinine clearance, protein contents, and albumin levels were observed by CCl4 administration when matched to controls. CCl4 injection also decreased the level of reduced glutathione, catalase, super oxide dismutase, peroxidase, glutathione s-transferase, glutathione reductase, and tissue protein while elevated the levels of thiobarbituric acid reactive substances, DNA damages and H2O2 in renal tissues of experimental animals. Co-treatment of FXM and silymarin, lead to the restoration of all the above tested parameters of kidney. Through this study we affirmed the ameliorating role of F. xanthoxyloides in oxidative stress affiliated disorders of kidney.


Assuntos
Lesão Renal Aguda/induzido quimicamente , Lesão Renal Aguda/tratamento farmacológico , Tetracloreto de Carbono/toxicidade , Fraxinus , Extratos Vegetais/uso terapêutico , Folhas de Planta , Lesão Renal Aguda/patologia , Animais , Masculino , Metanol/uso terapêutico , Extratos Vegetais/isolamento & purificação , Ratos , Ratos Sprague-Dawley
5.
Adv Pharmacol Sci ; 2018: 9794625, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29853868

RESUMO

Natural products, an infinite treasure of bioactive chemical entities, persist as an inexhaustible resource for discovery of drugs. This review article intends to emphasize on one of the naturally occurring flavonoids, astragalin (kaempferol 3-glucoside), which is a bioactive constituent of various traditional medicinal plants such as Cuscuta chinensis. This multifaceted compound is well known for its diversified pharmacological applications such as anti-inflammatory, antioxidant, neuroprotective, cardioprotective, antiobesity, antiosteoporotic, anticancer, antiulcer, and antidiabetic properties. It carries out the aforementioned activities by the regulation and modulation of various molecular targets such as transcription factors (NF-κB, TNF-α, and TGF-ß1), enzymes (iNOS, COX-2, PGE2, MMP-1, MMP-3, MIP-1α, COX-2, PGE-2, HK2, AChe, SOD, DRP-1, DDH, PLCγ1, and GPX), kinases (JNK, MAPK, Akt, ERK, SAPK, IκBα, PI3K, and PKCß2), cell adhesion proteins (E-cadherin, vimentin PAR-2, and NCam), apoptotic and antiapoptotic proteins (Beclin-1, Bcl-2, Bax, Bcl-xL, cytochrome c, LC3A/B, caspase-3, caspase-9, procaspase-3, procaspase-8, and IgE), and inflammatory cytokines (SOCS-3, SOCS-5, IL-1ß, IL-4, IL-6, IL-8, IL-13, MCP-1, CXCL-1, CXCL-2, and IFN-γ). Although researchers have reported multiple pharmacological applications of astragalin in various diseased conditions, further experimental investigations are still mandatory to fully understand its mechanism of action. It is contemplated that astragalin could be subjected to structural optimization to ameliorate its chemical accessibility, to optimize its absorption profiles, and to synthesize its more effective analogues which will ultimately lead towards potent drug candidates.

6.
Mol Carcinog ; 57(10): 1267-1277, 2018 10.
Artigo em Inglês | MEDLINE | ID: mdl-29802724

RESUMO

We recently identified and characterized nummularic acid (NA) as a major chemical constituent of Fraxinus xanthoxyloides, a medicinal plant used for over hundred years in traditional medicine. In this study, we describe its potential anti-cancer activity using prostate cancer (PCa) cells as a model. We found that NA treatment (5-60 µM) significantly reduced the proliferation and colony formation capabilities of PCa DU145 and C4-2 cells in a time and dose dependent manner, reduced the migratory and invasive properties and increased apoptotic cell population. Mechanistically, we found that NA treatment to PCa cells resulted in a sustained activation of adenosine monophosphate-activated protein kinase (AMPK). NA simultaneously increased acetyl CoA carboxylase phosphorylation and decreased pS6 phosphorylation, the two major substrates of AMPK. Further, NA treatment significantly elevated the cellular ADP/ATP ratio and altered glycolytic rate. We further observed a reversible decrease in oxygen consumption rate in NA treated cells when compared to the control. Finally, we performed global untargeted metabolomics which showed that NA treatment alters PCa cell metabolism at multiple sites including glycolysis, tricarboxylic acid, and glutamine metabolism which supported our observation of a possible AMPK activation. In summary, we report NA as a novel small molecule activator of AMPK that alters cellular metabolism to induce energy crisis and ultimately cancer cell death. Because of its unique mechanism NA could be potentially applicable against other cancer types.


Assuntos
Proliferação de Células/efeitos dos fármacos , Metabolismo Energético/efeitos dos fármacos , Fraxinus/química , Plantas Medicinais/química , Triterpenos/farmacologia , Acetil-CoA Carboxilase/metabolismo , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Humanos , Masculino , Metabolômica/métodos , Estrutura Molecular , Peptídeos Cíclicos , Fosforilação/efeitos dos fármacos , Neoplasias da Próstata/metabolismo , Neoplasias da Próstata/patologia , Triterpenos/química
7.
Artigo em Inglês | MEDLINE | ID: mdl-29279716

RESUMO

Fraxinus, a member of the Oleaceae family, commonly known as ash tree is found in northeast Asia, north America, east and western France, China, northern areas of Pakistan, India, and Afghanistan. Chemical constituents of Fraxinus plant include various secoiridoids, phenylethanoids, flavonoids, coumarins, and lignans; therefore, it is considered as a plant with versatile biological and pharmacological activities. Its tremendous range of pharmacotherapeutic properties has been well documented including anticancer, anti-inflammatory, antioxidant, antimicrobial, and neuroprotective. In addition, its bioactive phytochemicals and secondary metabolites can be effectively used in cosmetic industry and as a competent antiaging agent. Fraxinus presents pharmacological effectiveness by targeting the novel targets in several pathological conditions, which provide a spacious therapeutic time window. Our aim is to update the scientific research community with recent endeavors with specifically highlighting the mechanism of action in different diseases. This potentially efficacious pharmacological drug candidate should be used for new drug discovery in future. This review suggests that this plant has extremely important medicinal utilization but further supporting studies and scientific experimentations are mandatory to determine its specific intracellular targets and site of action to completely figure out its pharmacological applications.

8.
Pak J Pharm Sci ; 30(5): 1709-1713, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29084693

RESUMO

Excessive hemorrhage through any reasons is a life threatening process. Artemisia scoparia of family Asteraceae has been used in local system of medicine to stop bleeding from wounds and in injuries, antiseptic, in healing urticarial and for removal of worms from the body. Aerial parts of A. scoparia was extracted with 95% methanol (ASM) and fractionated through liquid-liquid partition in ascending order of n-hexane (ASH), chloroform (ASC), ethyl acetate (ASE), and the remaining as the aqueous fraction (ASA). Phytochemical classes of the extract/fractions were determined by qualitative assays. Prothrombin time (PT) was estimated on the plasma of human blood by Owren method. Capillary tube method was applied to determine the hemostasis activity in Sprague-Dawley rat. Tannins, saponins, terpenoids, quinones, betacyanins and flavonoids were present whereas phlobatannins, anthraquinones and alkaloids were established absent in ASM, ASC, ASE and ASA. Prothrombin time was significantly decreased by mixing (10 µg) of ASM (16.67±1.15 sec), ASH (12.33±0.57 sec), ASC (15.33±0.57 sec) and ASA (9.0±1.0 sec) to that of vehicle (20.0±1.0 sec). Administration (200 mg/kg) of all the extract/fractions showed significantly less (26.00±11.79 sec - 41.00±7.21 sec) hemostasis time as compared to the (242.67±39.67 sec) control rats. The results suggested the therapeutics importance of A. scoparia use in bleeding pathologies.


Assuntos
Artemisia/química , Hemostasia/efeitos dos fármacos , Hemostáticos/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Hemostáticos/isolamento & purificação , Humanos , Masculino , Compostos Fitoquímicos/isolamento & purificação , Componentes Aéreos da Planta/química , Extratos Vegetais/isolamento & purificação , Tempo de Protrombina , Ratos Sprague-Dawley , Solventes/química
9.
J Ethnopharmacol ; 198: 407-416, 2017 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-28119101

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Stem bark of Alnus nitida (Spach) Endl. (family Betulaceae) is used by local communities in northern areas of Pakistan as a remedy for swelling, injuries and pain. However no pharmacological study of this plant has been reported to confirm these activities. In this study anti-inflammatory and analgesic effect of A. nitida stem bark have been evaluated. METHODS: Powder of the stem bark of A. nitida was extracted with methanol (ANBM) and partitioned in escalating polarity to get the n-hexane (ANBH), chloroform (ANBC), ethyl acetate (ANBE) and the residual soluble aqueous (ANBA) fractions. The methanol extract and derived fractions were evaluated for anti-inflammatory activity by using in vitro heat induced albumin denaturation assay and various in vivo assays; carrageenan-induced hind paw edema method, Freunds' complete adjuvant induced arthritis, histamine induced paw edema and xylene induced ear edema in Sprague Dawley rat. The extracts/fractions were also evaluated for analgesic effects by using hot plate analgesic test and acetic acid induced writhing test in rat. The ANBM composition was analyzed by HPLC-DAD and GC-MS analysis. RESULTS: Results of heat induced albumin denaturation activity indicated that among the extract/fractions ANBC at concentration range of 100-500µg/ml remarkably protected the heat induced albumin denaturation. The pretreatment with ANBC significantly reduced the carrageenan induced edema with 90.81±1.6% after 4h, comparing with 86.63±3.42% reduction produced by the reference drug diclofenac potassium. Histopathological alterations of the gastric and hind paw were decreased with the extract/fractions. Furthermore, anti-inflammatory effects of ANBC were evident in Freunds' complete adjuvant induced arthritis, histamine induced paw edema and xylene induced ear edema. The latency time in hot plate analgesic assay with ANBC (61.59±0.38%) after 90min was comparable to standard drug morphine (69.31±2.67%) and aspirin (67.24±2.08%). Similarly ANBC significantly (p<0.01) inhibited the pain sensation in acetic acid induced writhing test in rat. HPLC-DAD analysis of ANBM indicated the presence of gallic acid, catechin and rutin while the GC-MS analysis of ANBM indicated the presence of 30 compounds predominantly of neophytadiene, 3,7,11,15 tetramethyl-2-hexadecen-1-ol, phytol, vitamin E and linalool. CONCLUSION: The results of this study suggested that the presence of polyphenols, sterols, terpenoids and other constituents might contributed towards the anti-inflammatory and analgesic activities of the crude methanol extract of A. nitida bark and its derived fractions. This study endorsed the folklore use of A. nitida bark for inflammation related disorders.


Assuntos
Alnus/química , Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Extratos Vegetais/farmacologia , Analgésicos/administração & dosagem , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Aspirina/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Cromatografia Gasosa-Espectrometria de Massas , Inflamação/tratamento farmacológico , Inflamação/patologia , Masculino , Medicina Tradicional/métodos , Morfina/farmacologia , Dor/tratamento farmacológico , Dor/patologia , Paquistão , Casca de Planta , Extratos Vegetais/administração & dosagem , Caules de Planta , Ratos , Ratos Sprague-Dawley
10.
BMC Complement Altern Med ; 16(1): 407, 2016 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-27776508

RESUMO

BACKGROUND: Leaves and root bark of Fraxinus xanthoxyloides Wall. (Oleaceae) are used locally for the treatment of jaundice, malaria and pneumonia. Decoction of stem, twigs and bark is used in pain, internal injuries, rheumatism and in bone fracture. In this investigation we have evaluated the methanol extract of leaves for its hepatoprotective potential against CCl4 induced hepatic injuries in rat. METHODS: Powder of F. xanthoxyloides leaves was extracted with methanol (FXM) and subjected for the determination of polyphenolics through HPLC-DAD analysis. Sprague-Dawley (Rattus novergicus) male rats were divided into eight groups (six rats in each). Group I: non-treated control; Group II: vehicle treated (DMSO plus olive oil) while Group III- VI treated with 1 ml/kg body weight (bw) of CCl4 (30 % in olive oil) for 30 days (15 dosages) to induce the hepatic injuries. Group IV: treated with silymarin (100 mg/kg bw); Group V and VI with FXM (200, 400 mg/kg bw) on alternate days with CCl4 treatment. Group VII and VIII was administered with FXM (200, 400 mg/kg bw) alone (15 dosages). After 30 days the serum was evaluated for liver function enzymes and biochemical markers, liver samples for antioxidant enzymes, biochemical markers, comet assay and for histopathology. RESULTS: HPLC-DAD analysis of FXM revealed the existence of rutin and caffeic acid. In CCl4 treated rats the level of alanine transaminase (ALT), aspartate transaminase (AST), total bilirubin was significantly increased while the albumin concentration in serum was decreased as compared to control group. The level of hepatic antioxidant enzymes, catalase (CAT), peroxidase (POD), superoxide dismutase (SOD), glutathione-S-transferase (GST) and glutathione reductase (GSR) was significantly decreased against the control group. Further, significant decrease in GSH while increase in lipid peroxides (TBARS), H2O2, DNA damages and comet length was induced with CCl4 in hepatic tissues of rat. In contrast, co-administration of FXM and silymarin restored the biochemical and histopathological status of the liver. CONCLUSION: Results of present investigation revealed that F. xanthoxyloides leaves possibly protect the liver against CCl4 induced injuries like silymarin by its antioxidant constituents.


Assuntos
Antioxidantes/farmacologia , Fraxinus/química , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Animais , Antioxidantes/química , Biomarcadores/análise , Tetracloreto de Carbono/toxicidade , Doença Hepática Induzida por Substâncias e Drogas , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
11.
BMC Complement Altern Med ; 16: 268, 2016 Aug 03.
Artigo em Inglês | MEDLINE | ID: mdl-27488054

RESUMO

BACKGROUND: Alnus nitida (Spach) Endl. is traditionally used for inflammatory disorders. Diarylheptanoids constituents having diverse therapeutically importance including hepato-protective was reported in A. nitida. The aim of this study was to explore the antioxidant and hepato-protective profile of A. nitida stem bark's crude methanol extract (ANM). METHODS: Crude methanol extract of A. nitida stem bark and its derived fractions were assessed for phytochemical classes and in vitro antioxidant profiling by multidimensional assays. Hepato-protective assessment of ANM was investigated on rats, which were made hepatotoxic using carbon tetrachloride (CCl4). Additionally HPLC-DAD analysis of ANM, and its derived ethyl acetate and aqueous fraction was carried out to determine the presence of active constituents. RESULTS: Qualitative analysis of crude extract-and its fractions depicted the presence of terpenoids, saponins, coumarins, phenols and flavonoids. Maximum quantity of total phenolic content (TPC) and total flavonoid content (TFC) was recorded in ANM and its derived fractions; n-hexane (ANH), chloroform (ANC), ethyl acetate (ANE) and the residual aqueous (ANA). ANM exhibited the best total antioxidant capacity, total reducing power, and scavenging of DPPH and OH radicals. ANE and ANA exhibited strong scavenging potential for iron chelation, nitric oxide and ß-carotene bleaching assay. ANM treatment converse the activities of serum-marker enzymes and lipid profile, altered by CCl4 treatment in rat. CCl4 induced hepatic-cirrhosis in rat resulted in decrease of antioxidant enzyme activities such as catalase, peroxidase, superoxide dismutase, glutathione peroxidase, glutathione-S-transferase and glutathione reductase-which were restored towards the normal level with ANM. Similarly diminished level of reduced glutathione while enhanced level of lipid peroxides, hydrogen peroxide and nitrite in liver of cirrhotic rats was normalized by treatment of ANM. The histopathological studies of liver tissues also represented that ANM possessed the hepato-protective activity. HPLC-DAD analysis against eight known standards confirmed the presence of gallic acid, catechin and rutin in ANM and in ANA while in ANE gallic acid was only detected. CONCLUSION: Based on the results of antioxidants, restoration of various antioxidant enzymes and histopathological studies, the recent study concludes that antioxidant potential of A. nitida bark might protect the liver damages.


Assuntos
Alnus/química , Antioxidantes/farmacologia , Casca de Planta/química , Extratos Vegetais/farmacologia , Animais , Antioxidantes/química , Tetracloreto de Carbono/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/patologia , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Flavonoides/química , Flavonoides/farmacologia , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Oxirredução/efeitos dos fármacos , Fenóis/análise , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
12.
BMC Complement Altern Med ; 16: 230, 2016 Jul 19.
Artigo em Inglês | MEDLINE | ID: mdl-27430329

RESUMO

BACKGROUND: Different parts of Fraxinus xanthoxyloides Wall. (Oleaceae) are used traditionally in the treatment of internal wounds, bone fracture, pain, jaundice, malaria and in pneumonia. These ailments involve protective and essential mechanisms of the organism in response to infection, injury and trauma. However, prolonged inflammation may lead to inflammatory disorders. The present investigation was carried to evaluate the crude methanol extract of F. xanthoxyloides leaves and its fractions for their anti-inflammatory and analgesic effects. METHODS: Methanol extract of F. xanthoxyloides leaves was fractionated through liquid-liquid partition on escalating polarity of solvents. Acetic acid and thermal responses were used to evaluate the analgesic effects of extract/fractions in rat. Anti-inflammatory effects were monitored through in vitro; TNF-α activated NFkB in 293/NFkB-Luc HEK cells and LPS-activated nitric oxide (NO) assay in RAW 264.7 cells. For in vivo studies carrageenan induced paw edema model was used in rat. Both in vitro and in vivo studies have indicated that chloroform fraction exhibited superior anti-inflammatory effects to other extract/fractions and therefore, was used in air pouch model in rat to estimate the inhibition in leukocyte migration and synthesis of inflammatory mediators. In addition, phytochemical investigation of crude extract was carried out by GC-MS analysis. RESULTS: GC-MS studies of crude extract revealed the presence of various classes of which terpenoids (26.61 %), lactam (16.47 %), esters (15.81 %), phenols (8.37 %), and steroid (6.91 %) constituted the major categories. Among the extracts chloroform fraction (200 mg/kg bw) significantly (P <0.001) increased the percent latency time (76.13 ± 4.49 %) in hot plate test after 120 min and decreased (P <0.001) the count of writhes (77.23 ± 5.64 %) as compared to other extracts. The in vitro studies indicated that chloroform fraction at 15 µg/ml more effectively inhibited the TNF-α induced synthesis of NFkB (85.0 ± 8.12 %, IC50 = 5.98 µg/ml) and LPS-instigated nitric oxide (78.23 ± 2.39 %, IC50 = 6.59 µg/ml) synthesis. Although all the extract/fractions showed a dose dependent increase in inhibition of edema formation however, chloroform fraction (4(th) h = 77.64 ± 3.04 %) at 200 mg/kg bw exhibited relatively higher (P <0.001) anti-inflammatory activity in carrageenan-induced paw edema in rat. Moreover, chloroform fraction had the ability to decrease (P <0.001) the influx of leukocytes and the concentration of inflammatory mediators; TNF-α, NO, IL-6 and PGE2 in air pouch exudate. CONCLUSION: The study demonstrates the therapeutic potential of F. xanthoxyloides leaves against the inflammatory disorders suggesting the presence of active constituents in chloroform fraction.


Assuntos
Anti-Inflamatórios/farmacologia , Citocinas/sangue , Fraxinus/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Animais , Anti-Inflamatórios/química , Carragenina/toxicidade , Edema/induzido quimicamente , Edema/metabolismo , Feminino , Células HEK293 , Humanos , Inflamação , Masculino , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
13.
BMC Complement Altern Med ; 16: 149, 2016 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-27233360

RESUMO

BACKGROUND: Artemisia scoparia is traditionally used in the local system of medicine in kidney disorders. This study aimed at scrutinizing the nephroprotective prospective of A. scoparia methanol extract against carbon tetrachloride (CCl4) provoked DNA damages and oxidative stress in kidneys of rat. METHODS: Dried aerial parts of A. scoparia were powdered and extracted with methanol to obtain the viscous material (ASM). Sprague Dawley male rats (42) were grouped (7) having 6 rats in each. Group I remained untreated and Group II treated intraperitoneally (i.p) with DMSO + olive oil (1 ml/kg body weight (bw). Rats of Group III - VI were treated with CCl4 (1 ml/kg bw; i.p 30 % v/v in olive oil). Animals of Group IV were co-administered with 100 mg/kg bw of silymarin whereas rats of Group V and VI with 150 mg/kg bw and 300 mg/kg bw of ASM at an interval of 48 h for four weeks. Animals of Group VII were administered with ASM (300 mg/kg bw) alone. DNA damages were investigated with comet assay in renal tissues while the oxidative injuries were estimated in serum and renal tissues. RESULTS: Co-administration of ASM to rats significantly reduced the DNA damages at 300 mg/kg dose as indicated in comet length (40.80 ± 2.60 µm), head length (34.70 ± 2.21 µm), tail length (7.43 ± 1.24 µm) and DNA content in head (88.03 ± 2.27 %) to that of CCl4 for comet length (63.16 ± 2.11 µm), head length (23.29 ± 1.50 µm), tail length (39.21 ± 2.81 µm) and DNA content of head (74.81 ± 2.18 %) in renal cell's nuclei. Increased level of urea, creatinine, bilirubin, blood urea nitrogen whereas decreased concentration of proteins in serum of CCl4 treated animals were restored towards the normal level with co-administration of ASM. CCl4 injection in rats decreased the activity level of CAT, POD, SOD, GST and γ-GT and GSH contents while elevated levels of TBARS, H2O2 and nitrite contents were observed in renal tissues. A noteworthy retrieval of all these parameters and the altered histopathological observations was notified near to the normal values after treatment with both the doses of ASM. CONCLUSION: Results obtained suggested the therapeutic role of ASM in oxidative stress related disorder of kidneys.


Assuntos
Artemisia/química , Dano ao DNA/efeitos dos fármacos , Rim/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Animais , Antioxidantes/metabolismo , Biomarcadores/sangue , Tetracloreto de Carbono , Ensaio Cometa , Rim/enzimologia , Masculino , Estresse Oxidativo/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley
14.
BMC Complement Altern Med ; 15: 349, 2015 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-26445953

RESUMO

BACKGROUND: Plants provide an alternative source to manage various human disorders due to diverse metabolites. Euphorbia dracunculoides of family Euphorbiaceae is used by local practitioners in rheumatism, epilepsy, edema, snake bite, warts and also possesses diuretic and purgative effects. The present study evaluated the antioxidant, anti-inflammatory and analgesic activities of various extracts of E. dracunculoides. Further, phytochemical constituents of the leading extracts were also investigated. METHODS: Dry powder of E. dracunculoides was extracted with n-hexane (EDH), acetone (EDA), ethanol (EDE), ethanol + water (1:1) (EDEW) and methanol (EDM) and screened for phytochemical classes, total phenolic (TPC) and flavonoid content (TFC). Antioxidant effects of the extracts were manifested by in vitro multidimensional assays. The anti-inflammatory and analgesic activities of the extracts were evaluated through carrageenan induced paw edema and hot plate test in rat. In addition, GC-MS analysis of EDH and HPLC-DAD analysis of EDEW was carried out to determine the presence of active constituents. RESULTS: Qualitative analysis of various extracts of E. dracunculoides assured the existence of tannins and coumarins while presence of anthraquinones and anthocyanins was not traced in these extracts. Maximum quantity of TPC and TFC was recorded in EDEW followed by EDE. EDEW and EDE showed significant antioxidant activities with therapeutic potential against hydroxyl and phosphomolybdate radicals, ß-carotene bleaching assay and in reducing of iron while moderate to low scavenging abilities were recorded for DPPH, nitric oxide and for iron chelation. During anti-inflammatory activity after 4 h of drug administration the 300 mg/kg body weight dose of EDH (68.660 ± 10.502%) and EDE (51.384 ± 8.623%) exhibited strong anti-inflammatory activity and reduced the carrageenan-induced paw edema in rat as compared to standard drug diclofenac sodium (78.823 ± 6.395%). Treatment of rats with EDH (70.206 ± 5.445%) and EDE (56.508 ± 6.363%) after 90 min showed significant increase in percent latency time in hot plate test as compared to morphine (63.632 ± 5.449%) treatment in rat. GC-MS analysis of EDH indicated the presence of 30 compounds predominantly of steroids and terpenoids. HPLC-DAD analysis against known standards established the presence of rutin, catechin, caffeic acid and myricetin in EDEW. CONCLUSION: Our results suggest that presence of various polyphenolics, terpenoids and steroids render E. dracunculoides with therapeutic potential for oxidative stress and inflammation related disorders.


Assuntos
Analgésicos/administração & dosagem , Anti-Inflamatórios/administração & dosagem , Antioxidantes/administração & dosagem , Edema/tratamento farmacológico , Euphorbia/química , Extratos Vegetais/administração & dosagem , Analgésicos/química , Animais , Anti-Inflamatórios/química , Antioxidantes/química , Edema/imunologia , Humanos , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
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