Base de dados : MEDLINE Pesquisa : B01.650.940.800.575.912.250.859.844.750 [Categoria DeCS] Referências encontradas : 31 [refinar] Mostrando: 1 .. 10   no formato [Detalhado]

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[PMID]: 28065566 [Au] Autor: Wang Q; Ma C; Ma Y; Li X; Chen Y; Chen J [Ad] Endereço: College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China. [Ti] Título: Structure-activity relationships of diverse xanthones against multidrug resistant human tumor cells. [So] Source: Bioorg Med Chem Lett;27(3):447-449, 2017 02 01. [Is] ISSN: 1464-3405 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Thirteen xanthones were isolated naturally from the stem of Securidaca inappendiculata Hassk, and structure-activity relationships (SARs) of these compounds were comparatively predicted for their cytotoxic activity against three human multidrug resistant (MDR) cell lines MCF-7/ADR, SMMC-7721/Taxol, and A549/Taxol cells. The results showed that the selected xanthones exhibited different potent cytotoxic activity against the growth of different human tumor cell lines, and most of the xanthones exhibited selective cytotoxicity against SMMC-7721/Taxol cells. Furthermore, some tested xanthones showed stronger cytotoxicity than Cisplatin, which has been used in clinical application extensively. The SARs analysis revealed that the cytotoxic activities of diverse xanthones were affected mostly by the number and position of methoxyl and hydroxyl groups. Xanthones with more free hydroxyl and methoxyl groups increased the cytotoxic activity significantly, especially for those with the presence of C-3 hydroxyl and C-4 methoxyl groups. [Mh] Termos MeSH primário: Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos Xantonas/química Xantonas/farmacologia [Mh] Termos MeSH secundário: Células A549 Linhagem Celular Tumoral Sobrevivência Celular/efeitos dos fármacos Seres Humanos Células MCF-7 Caules de Planta/química Caules de Planta/metabolismo Securidaca/química Securidaca/metabolismo Relação Estrutura-Atividade Xantonas/isolamento & purificação [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Xanthones) [Em] Mês de entrada: 1707 [Cu] Atualização por classe: 171124 [Lr] Data última revisão: 171124 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170110 [St] Status: MEDLINE

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[PMID]: 27927065 [Au] Autor: Saliu JA; Olabiyi AA [Ad] Endereço: a Department of Biochemistry , Adekunle Ajasin University , Akungba Akoko , Nigeria. [Ti] Título: Aqueous extract of Securidaca longipendunculata Oliv. and Olax subscropioidea inhibits key enzymes (acetylcholinesterase and butyrylcholinesterase) linked with Alzheimer's disease in vitro. [So] Source: Pharm Biol;55(1):252-257, 2017 Dec. [Is] ISSN: 1744-5116 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: CONTEXT: Plants have historically been used to treat neurodegerative diseases which include Alzheimer's disease. OBJECTIVE: This study investigated the antioxidant properties and inhibitory effect of aqueous extracts of Securidaca longipendunculata root and Olax subscropioidea leaf on the cholinergic system in rat brain in vitro. MATERIALS AND METHODS: Aqueous extracts (1:20 w/v) of S. longipendunculata root and O. subscropioidea leaf was prepared and the ability of the extract to inhibit the activities of acetylcholinesterase and butyrylcholinesterase was evaluated as well as antioxidants as typified by 2,2-azino-bis-(3-ethylbenthiazoline-6-sulphonic acid (ABTS ) radical scavenging ability and Fe chelation spectophotometrically. RESULTS: ABTS radical scavenging ability showed that S. longipendunculata (0.075 Mmol TEAC/100 g) had a higher scavenging ability than O. subscropioidea (0.07 Mmol TEAC/100 g). Also, the Fe chelating ability of both extracts revealed that S. longipendunculata (IC = 105.57 g/mL) had a significantly (p < 0.05) higher Fe chelating ability than O. subscropioidea (IC = 255.84 g/mL). Extracts of S. longipendunculata and O. subscropioidea inhibited acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities. However, S. longipendunculata (IC = 108.02 g/mL) has the higher AChE inhibitory activity than O. subscropioidea (IC = 110.35 g/mL). Also, both extracts inhibit BChE activity in vitro but S. longipendunculata (IC = 82.55 g/mL) had a higher BChE inhibitory activity than O. subscropioidea (IC = 108.44 g/mL). DISCUSSION AND CONCLUSIONS: The mechanism by which S. longipendunculata root and O. subscropioidea leaf perform their anti-Alzheimer's disease activity may be by their inhibition on the key enzymes linked to this disease. [Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo Doença de Alzheimer/tratamento farmacológico Butirilcolinesterase/metabolismo Inibidores da Colinesterase/farmacologia Olacaceae/química Extratos Vegetais/farmacologia Securidaca/química [Mh] Termos MeSH secundário: Doença de Alzheimer/enzimologia Animais Antioxidantes/isolamento & purificação Antioxidantes/farmacologia Benzotiazóis/química Inibidores da Colinesterase/isolamento & purificação Relação Dose-Resposta a Droga Compostos Ferrosos/química Quelantes de Ferro/isolamento & purificação Quelantes de Ferro/farmacologia Peroxidação de Lipídeos/efeitos dos fármacos Masculino Fitoterapia Extratos Vegetais/isolamento & purificação Folhas de Planta Raízes de Plantas Plantas Medicinais Ratos Wistar Ácidos Sulfônicos/química Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antioxidants); 0 (Benzothiazoles); 0 (Cholinesterase Inhibitors); 0 (Ferrous Compounds); 0 (Iron Chelating Agents); 0 (Plant Extracts); 0 (Sulfonic Acids); 0 (Thiobarbituric Acid Reactive Substances); 28752-68-3 (2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid); 39R4TAN1VT (ferrous sulfate); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161209 [St] Status: MEDLINE

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[PMID]: 27848204 [Au] Autor: Tofighi Z; Moradi-Afrapoli F; Ebrahimi SN; Goodarzi S; Hadjiakhoondi A; Neuburger M; Hamburger M; Abdollahi M; Yassa N [Ad] Endereço: Department of Pharmacognosy, Faculty of Pharmacy and Medicinal Plant Research Center, Tehran University of Medical Sciences, Tehran, 14174-14411, Iran. [Ti] Título: Securigenin glycosides as hypoglycemic principles of Securigera securidaca seeds. [So] Source: J Nat Med;71(1):272-280, 2017 Jan. [Is] ISSN: 1861-0293 [Cp] País de publicação: Japan [La] Idioma: eng [Ab] Resumo: Seeds of Securigera securidaca (Fabaceae) are used in Iranian folk medicine as an antidiabetic treatment. In this study, the antihyperglycemic activity of chloroform and methanol fractions (CF and MF) from S. securidaca seed extract was investigated and their bioactive constituents were identified. The antidiabetic effects of fractions were assessed by streptozocin-induced diabetic Naval Medical Research Institute mice. The hypoglycemic activity of MF at 100 mg/kg and CF at 400 mg/kg was comparable with glibenclamide (3 mg/kg). MF at 400 mg/kg and CF at 600 mg/kg showed equal hypoglycemic responses to 12.5 IU/kg insulin (P > 0.05). Three cardiac glycosides were isolated as active constituents responsible for the hypoglycemic activity. Securigenin-3- O -ß-glucopyranosyl-(1 â†’ 4)-ß-xylopyranoside (1) was a major compound in seeds. Securigenin-3- O -inositol-(1 â†’ 3)-ß-glucopyranosyl-(1 â†’ 4)-ß-xylopyranoside (2) and securigenin-3- O -α-rhamnopyranosyl-(1 â†’ 4)-α-glucopyranoside (3) were found as new natural products. When 1-3 were tested at 10 mg/kg there was a significant reduction of blood glucose levels in diabetic mice, comparable to that of 3 mg/kg glibenclamide (P > 0.05). The hypoglycemic effect was due to an increase in insulin secretion; the insulin levels in the diabetic mice significantly improved and were comparable with those in healthy animals (P > 0.05). Compounds responsible for the hypoglycemic properties of S. securidaca seeds were identified as cardiac glycosides and were found to act via an increase of insulin levels in a diabetic mouse model. [Mh] Termos MeSH primário: Glicemia/efeitos dos fármacos Diabetes Mellitus Experimental/tratamento farmacológico Fabaceae/química Hipoglicemiantes/farmacologia Extratos Vegetais/química Securidaca/química Sementes/química [Mh] Termos MeSH secundário: Animais Masculino Camundongos Extratos Vegetais/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Blood Glucose); 0 (Hypoglycemic Agents); 0 (Plant Extracts) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 171104 [Lr] Data última revisão: 171104 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161117 [St] Status: MEDLINE [do] DOI: 10.1007/s11418-016-1060-7

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[PMID]: 26125283 [Au] Autor: Ahmadi A; Khalili M; Margedari Sh; Nahri-Niknafs B [Ad] Endereço: Department of Medicinal Chemistry, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran. [Ti] Título: The Effects of Solvent Polarity on Hypoglycemic and Hypolipidemic Activities of Securigera Securidaca (L.) Seeds. [So] Source: Drug Res (Stuttg);66(3):130-5, 2016 Mar. [Is] ISSN: 2194-9387 [Cp] País de publicação: Germany [La] Idioma: eng [Ab] Resumo: The search for indigenous natural antidiabetic and antilipidemec agents is still ongoing. Medicinal plants are widely used for this purpose. These herbs are very rich sources of bioactive compounds as flavonoids, polyphenols, tannins, alkaloids which have been reported as effective role to reduce blood glucose and lipid levels. Securigera securidaca seed is reputed in folk medicine for their value as antidiabetic and antilipidemec drugs. In this research, the effect of solvent polarity in bioactive extraction contents of this plant was evaluated by GC-MS analysis. Then antidiabetic and antilipidemic activies of different extracts were investigated in streptozotocine-induced diabetic rats and compared to glibenclamide as known chemical drug for diabetes.The results indicated that, carbon tetrachloride extract of Securigera securidaca seeds showed the best and significant hypoglycemic and hypolipidemic activities compared to other extracts because of its more sterols and fatty acids content with beta cells protecting effect from high glucose-induced apoptosis and also increasing in insulin level and sensitivity. [Mh] Termos MeSH primário: Hipoglicemiantes/química Hipoglicemiantes/farmacologia Hipolipemiantes/química Hipolipemiantes/farmacologia Securidaca/química Sementes/química Solventes/química [Mh] Termos MeSH secundário: Alcaloides/química Alcaloides/farmacologia Animais Antioxidantes/metabolismo Glicemia/efeitos dos fármacos Diabetes Mellitus Experimental/induzido quimicamente Diabetes Mellitus Experimental/tratamento farmacológico Flavonoides/química Flavonoides/farmacologia Glibureto/farmacologia Hipolipemiantes/metabolismo Masculino Extratos Vegetais/química Extratos Vegetais/farmacologia Polifenóis/química Polifenóis/farmacologia Ratos Ratos Wistar Estreptozocina/farmacologia Taninos/química Taninos/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Alkaloids); 0 (Antioxidants); 0 (Blood Glucose); 0 (Flavonoids); 0 (Hypoglycemic Agents); 0 (Hypolipidemic Agents); 0 (Plant Extracts); 0 (Polyphenols); 0 (Solvents); 0 (Tannins); 5W494URQ81 (Streptozocin); SX6K58TVWC (Glyburide) [Em] Mês de entrada: 1612 [Cu] Atualização por classe: 161230 [Lr] Data última revisão: 161230 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 150701 [St] Status: MEDLINE [do] DOI: 10.1055/s-0035-1555773

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[PMID]: 26666038 [Au] Autor: Zha HY; Yang XD; Zhang LJ; Jin DQ; Wang Z; Xu LZ; Yang SL [Ti] Título: [Saponins from roots of Securidaca inappendiculata with cytotoxic activities]. [So] Source: Zhongguo Zhong Yao Za Zhi;40(14):2849-53, 2015 Jul. [Is] ISSN: 1001-5302 [Cp] País de publicação: China [La] Idioma: chi [Ab] Resumo: Seven acylated triterpene saponins were isolated from the roots of Securidaca inappendiculata by means of various chromatographic techniques such as silica gel, MPLC, preparative HPLC, and semi-preparative HPLC. Their chemical structures were identified as securioside A(1), securioside B(2), 3-O-ß-D-glucopyranosyl presenegenin 28-O-ß-D-xylopyranosyl-(1-->4)-α-L-rhamnopyranosyl-(1-->2)-[ß-D-glucopyranosyl-(1-->3)]-4-O-[(E)-3,4-dimethoxycinnamoyl]-ß-D-fucopyranosyl ester(3), 3-O-ß-D-glucopyranosyl presenegenin 28-O-ß-D-xylopyranosyl-(1-->4)-α-L-rhamnopyranosyl-(1-->2)-[ß-D-glucopyranosyl-(1-->3) ] -4-O-[(E/Z)-3, 4-dimethoxycinnamoyl]-ß-D-fucopyranosyl ester(3/4), 3-O-ß-D-glucopyranosyl presenegenin 28-O-α-L-arabinopyranosyl-(1-->3)-ß-D-xylopyranosyl-(1-->4)-α-L-rhamnopyranosyl-(1-->2)-4-O-[(E)-3,4-dimethoxycinnamoyl]-ß-D-fucopyranosyl ester(5), polygalasa- ponin XLV(6), and polygalasaponin XLVI (7) on the basis of spectroscopic data analysis and physicochemical properties. Among them, compounds 5-7 were isolated from the plants in genus Securidaca for the first time and compounds 3, 3/4 were isolated from the species for the first time. The cytotoxicity assay showed that compounds 2, 3/4, 5 have moderate cytotoxic activities against Lewis lung carcinoma LLC cells with IC50 values of 41.10, 38.17, and 48.92 µmol · L(-1), respectively; compound 2 exhibited moderate cytotoxic activities against human breast cancer MCF-7 cells with an IC50 value of 47.93 µmol · L(-1). [Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/isolamento & purificação Saponinas/isolamento & purificação Securidaca/química [Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/farmacologia Seres Humanos Células MCF-7 Raízes de Plantas/química Saponinas/química Saponinas/farmacologia [Pt] Tipo de publicação: ENGLISH ABSTRACT; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Antineoplastic Agents, Phytogenic); 0 (Saponins) [Em] Mês de entrada: 1601 [Cu] Atualização por classe: 151215 [Lr] Data última revisão: 151215 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 151216 [St] Status: MEDLINE

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[PMID]: 25724970 [Au] Autor: Mongalo NI; McGaw LJ; Finnie JF; Staden JV [Ad] Endereço: University of South Africa, College of Agriculture and Environmental Sciences, Private Bag X6, Florida 1710, South Africa; Research Centre for Plant Growth and Development, School of Life Sciences, University of KwaZulu-Natal, Pietermaritzburg, Private Bag X01, Scottsville 3209, South Africa. [Ti] Título: Securidaca longipedunculata Fresen (Polygalaceae): a review of its ethnomedicinal uses, phytochemistry, pharmacological properties and toxicology. [So] Source: J Ethnopharmacol;165:215-26, 2015 May 13. [Is] ISSN: 1872-7573 [Cp] País de publicação: Ireland [La] Idioma: eng [Ab] Resumo: ETHNOPHARMACOLOGICAL RELEVANCE: Securidaca longipedunculata Fresen (Polygalaceae) is a multi-purpose plant with a long history of use in African traditional medicine to treat various sexually transmitted infections, hernias, coughs, fever, ascariasis, constipation, headaches, rheumatism, stomach ache, malaria, tuberculosis, pain, epilepsy, pneumonia, skin infections, and it is also used as an aphrodisiac for men. The current paper provides an overview of the present phytochemistry, toxicology, ethnomedicinal uses and pharmacological properties of S. longipedunculata. MATERIALS AND METHODS: The information reported in this paper was collected from a literature search using various computerised databases including ScienceDirect, Scopus, Scielo, PubMed and Google Scholar. The extra information was sourced from various academic dissertations, theses and botanical books. RESULTS: Phytochemically, extracts from various parts of S. longipedunculata, especially the root bark, contain numerous valuable compounds including xanthones, some benzyl benzoates and triterpene saponins amongst others. Toxicity studies, both in vivo and in vitro, revealed that extracts are only toxic at relatively high concentrations. Furthermore, extracts have antimicrobial, antioxidant, antiparasitic, anti-diabetic, anti-inflammatory, antimalarial, insecticidal, pesticidal, and anticonvulsant properties. CONCLUSIONS: S. longipedunculata is an important plant species with potential benefits in the treatment of transmissible and infectious diseases, including malaria, tuberculosis, and those caused by community acquired microorganisms. Although extracts from this species generally have little toxicity at low concentrations, further efforts are required to investigate the potential toxicity of S. longipedunculata. The antimicrobial properties of extracts and purified compounds against microorganisms causing sexually transmitted infections are also deserving of further research. Moreover, the pharmacokinetic properties of extracts and compounds of the species need to be explored as there is insufficient data available on these aspects. [Mh] Termos MeSH primário: Medicina Tradicional Africana/métodos Fitoterapia/métodos Securidaca [Mh] Termos MeSH secundário: Etnobotânica/métodos Seres Humanos Extratos Vegetais/uso terapêutico Securidaca/química [Pt] Tipo de publicação: JOURNAL ARTICLE; REVIEW [Nm] Nome de substância: 0 (Plant Extracts) [Em] Mês de entrada: 1601 [Cu] Atualização por classe: 150414 [Lr] Data última revisão: 150414 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 150301 [St] Status: MEDLINE

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[PMID]: 25026334 [Au] Autor: Zuo J; Xia Y; Mao KJ; Li X; Chen JW [Ad] Endereço: College of Pharmacy, Nanjing University of Chinese Medicine , Nanjing , China. [Ti] Título: Xanthone-rich dichloromethane fraction of Securidaca inappendiculata, the possible antirheumatic material base with anti-inflammatory, analgesic, and immunodepressive effects. [So] Source: Pharm Biol;52(11):1367-73, 2014 Nov. [Is] ISSN: 1744-5116 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: CONTEXT: Securidaca inappendiculata Hassk. is an traditional Chinese medicine curing rheumatoid arthritis, but there is a lack of reports on material base research. OBJECTIVE: To find the active fraction of S. inappendiculata contributing the most to antirheumatic activity. MATERIALS AND METHODS: Prior to assays in vivo, mice were treated with different fractions from S. inappendiculata for 5 d at doses relative to 10, 5, and 2.5 g/kg of crude drug. Hot plate test and carrageenan-induced paw edema test were used to investigate analgesic and anti-inflammatory activities. PGE2 levels in inflammatory paws were determined by a colorimetric method. Carbon clearance test in vivo and lymphocyte transformation test in vitro were employed to assess the immune regulation activity. HPLC was used to explore the main compounds in the active fraction. RESULTS: All the fractions, especially the dichloromethane fraction (SID), alleviated inflammation. High dose of SID (112 mg/kg) inhibited paw swelling by 63.1%, and decreased PGE2 level to 38 ng/mL. The ethyl acetate fraction (SIE) and SID suppressed the carbon clearance rate (K = 0.044, 0.038 for high dose) efficiently. All fractions hindered the transformation and proliferation of lymphocyte, and prolonged the reaction time of rats in the hot plate test. The concentrations of two typical xanthones: 2-hydroxyl-1,7-dimethoxyl-xanthone and 1,7-dihydroxyl-xanthone in SID were 0.93% and 1.19%, respectively, by HPLC analysis. CONCLUSION: SID exhibited significant anti-inflammatory, analgesic, and immunodepressive effects in vivo and vitro, and deemed as the main material base for the antirheumatic activity. [Mh] Termos MeSH primário: Analgésicos/uso terapêutico Anti-Inflamatórios/uso terapêutico Antirreumáticos/uso terapêutico Imunossupressores/uso terapêutico Extratos Vegetais/uso terapêutico Securidaca [Mh] Termos MeSH secundário: Analgésicos/isolamento & purificação Analgésicos/farmacologia Animais Anti-Inflamatórios/isolamento & purificação Anti-Inflamatórios/farmacologia Antirreumáticos/isolamento & purificação Antirreumáticos/farmacologia Relação Dose-Resposta a Droga Edema/tratamento farmacológico Edema/imunologia Edema/patologia Feminino Imunossupressores/isolamento & purificação Imunossupressores/farmacologia Masculino Cloreto de Metileno/isolamento & purificação Cloreto de Metileno/farmacologia Cloreto de Metileno/uso terapêutico Camundongos Camundongos Endogâmicos ICR Medição da Dor/efeitos dos fármacos Medição da Dor/métodos Extratos Vegetais/isolamento & purificação Extratos Vegetais/farmacologia Caules de Planta Distribuição Aleatória Ratos Xantonas/isolamento & purificação Xantonas/farmacologia Xantonas/uso terapêutico [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Analgesics); 0 (Anti-Inflammatory Agents); 0 (Antirheumatic Agents); 0 (Immunosuppressive Agents); 0 (Plant Extracts); 0 (Xanthones); 588X2YUY0A (Methylene Chloride); 9749WEV0CA (xanthone) [Em] Mês de entrada: 1506 [Cu] Atualização por classe: 141014 [Lr] Data última revisão: 141014 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 140716 [St] Status: MEDLINE [do] DOI: 10.3109/13880209.2014.892143

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[PMID]: 24779644 [Au] Autor: Dibwe DF; Awale S; Kadota S; Morita H; Tezuka Y [Ad] Endereço: Institute of Natural Medicine, University of Toyama , 2630-Sugitani, Toyama 930-0194, Japan. [Ti] Título: Muchimangins G-J, fully substituted xanthones with a diphenylmethyl substituent, from Securidaca longepedunculata. [So] Source: J Nat Prod;77(5):1241-4, 2014 May 23. [Is] ISSN: 1520-6025 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Four highly oxygenated xanthones, muchimangins G-J (1-4), have been isolated from the roots of Securidaca longepedunculata collected in Democratic Republic of Congo. Their structures were elucidated by analyses of spectroscopic data to be fully substituted xanthones with a diphenylmethyl substituent at C-2. [Mh] Termos MeSH primário: Securidaca/química Xantonas/isolamento & purificação [Mh] Termos MeSH secundário: República Democrática do Congo Estrutura Molecular Extratos Vegetais/química Raízes de Plantas/química Xantonas/química [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Plant Extracts); 0 (Xanthones) [Em] Mês de entrada: 1409 [Cu] Atualização por classe: 140911 [Lr] Data última revisão: 140911 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 140501 [St] Status: MEDLINE [do] DOI: 10.1021/np5000445

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[PMID]: 24621306 [Au] Autor: Zuo J; Ji CL; Xia Y; Li X; Chen JW [Ad] Endereço: College of Pharmacy, Nanjing University of Chinese Medicine , China and. [Ti] Título: Xanthones as α-glucosidase inhibitors from the antihyperglycemic extract of Securidaca inappendiculata. [So] Source: Pharm Biol;52(7):898-903, 2014 Jul. [Is] ISSN: 1744-5116 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: CONTEXT: Securidaca inappendiculata Hassk. (SI) is used to cure fractures and rheumatoid arthritis in China. Also, it is a potential antidiabetes drug; however, there are no reports on this. OBJECTIVE: The study was designed to evaluate the antihyperglycemic activities of fractions and compounds from SI, and attempt to explore the mechanism. MATERIALS AND METHODS: Antihyperglycemic activities were evaluated by the suppression on serum glucose levels in vivo and α-glucosidase inhibition assays in vitro. Fractions were given to mice by gastric intubation for 8 d. The high, medium, and low doses of fractions were equal to 10, 5, and 2.5 g/kg of the herb [SID (dichloromethane fraction) and SIE (ethyl acetate fraction) were doubled]. The serum glucose was monitored at 1 and 12 h after feeding. The silica gel and LH-20 chromatography were used to isolate active compounds. Structure-activity relationship analysis was based on IC50s and structures. RESULTS: The IC50s of SID, SIE, SIA (acetone fraction), SIM (methanol fraction), and acarbose were 712, 446, 1123, 1418, and 735 µg/mL. The postprandial and fasting serum glucose levels of SID, SIE, SIA, and SIM (high dose) were 5.5, 5.9, 6.2, 6.3 and 3.7, 3.5, 4.0, 5.0 mmol/L, while those of vehicle control were 7.5 and 5.6 mmol/L. Eleven xanthones isolated all exhibited inhibitory activities, mainly in a non-competitive reversible manner. The IC50s varied from 3.2 to 77.3 µg/mL. Structure-activity relationship analysis exhibited free hydroxyls contributed the most importance to the activity. CONCLUSION: The results indicated that xanthones from SI were powerful agents for antidiabetes. [Mh] Termos MeSH primário: Glicemia/efeitos dos fármacos Inibidores de Glicosídeo Hidrolases/farmacologia Hipoglicemiantes/farmacologia Securidaca/química Xantonas/farmacologia [Mh] Termos MeSH secundário: Acarbose/farmacologia Acetatos/química Acetona/química Animais Relação Dose-Resposta a Droga Medicamentos de Ervas Chinesas/química Medicamentos de Ervas Chinesas/farmacologia Inibidores de Glicosídeo Hidrolases/química Hipoglicemiantes/química Masculino Cloreto de Metileno/química Camundongos Extratos Vegetais/farmacologia Caules de Planta/química Relação Estrutura-Atividade Xantonas/isolamento & purificação [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Acetates); 0 (Blood Glucose); 0 (Drugs, Chinese Herbal); 0 (Glycoside Hydrolase Inhibitors); 0 (Hypoglycemic Agents); 0 (Plant Extracts); 0 (Xanthones); 1364PS73AF (Acetone); 588X2YUY0A (Methylene Chloride); 76845O8NMZ (ethyl acetate); T58MSI464G (Acarbose) [Em] Mês de entrada: 1504 [Cu] Atualização por classe: 140612 [Lr] Data última revisão: 140612 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 140314 [St] Status: MEDLINE [do] DOI: 10.3109/13880209.2013.872673

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[PMID]: 24583103 [Au] Autor: Zuo J; Xia Y; Li X; Chen JW [Ad] Endereço: College of Pharmacy, Nanjing University of Chinese Medicine, 138 Xian Lin Road, Nanjing, China. [Ti] Título: Therapeutic effects of dichloromethane fraction of Securidaca inappendiculata on adjuvant-induced arthritis in rat. [So] Source: J Ethnopharmacol;153(2):352-8, 2014 Apr 28. [Is] ISSN: 1872-7573 [Cp] País de publicação: Ireland [La] Idioma: eng [Ab] Resumo: ETHNOPHARMACOLOGICAL RELEVANCE: Securidaca inappendiculata (SI) is a traditional antirheumatic medicine used in China. The present study was designed to investigate the therapeutic efficacy of dichloromethane fraction of SI (SID) at three different doses on adjuvant induced arthritis (AA) rats. METHODS: Arthritis severity was evaluated by arthritic score, body weight loss, paw circumference, histological changes and hyperplasia of lymphatic tissues. Serum samples were collected for estimation of superoxide dismutase (SOD), glutathione (GSH), hydroxy radical (OH·), nitric oxide (NO), malondialdehyde (MDA), N-acetyl glucosaminidase (NAG), sialic acid (SA), alkaline phosphatase (ALP), aspartate transaminase (AST) and alanine transaminase (ALT). The levels of GSH, MDA, NAG and SA in liver were also assessed. The levels of interleukin-1 (IL-1), tumor necrosis factor alpha (TNF-α), monocyte chemotactic protein 1 (MCP-1) and vascular endothelial growth factor (VEGF) were determined using ELISA method. Another portion of blood was used for total and differential leucocyte counts. RESULTS: Administration with SID (at high dose with 100 mg/kg) significantly ameliorated the AA severity, suggested by the modulatory effects on body weight loss, paw swelling, hyperplasia of lymphatic tissues and synovial membrane, neutrocytosis and lymphocytosis. It also decreased levels of NO, MDA and OH·, restored SOD and GSH levels in serum. The abnormal increased levels of AST, ALT, ALP, NAG and SA significantly were reverted (compared with AA rats, P<0.01). A similar result was observed in livers. Levels of IL-1, TNF-α, MCP-1 and VEGF were reduced dramatically by SID too. CONCLUSION: The results suggest SID possesses substantial anti-arthritic activity. The therapeutic efficacy may be due to immumodepressive effects, cytokines regulation, increasing membrane stability and antioxidantive activity. [Mh] Termos MeSH primário: Artrite Experimental/tratamento farmacológico Cloreto de Metileno/uso terapêutico Extratos Vegetais/uso terapêutico Securidaca [Mh] Termos MeSH secundário: Animais Artrite Experimental/patologia Masculino Cloreto de Metileno/isolamento & purificação Extratos Vegetais/isolamento & purificação Caules de Planta Ratos Ratos Sprague-Dawley Resultado do Tratamento [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Plant Extracts); 588X2YUY0A (Methylene Chloride) [Em] Mês de entrada: 1412 [Cu] Atualização por classe: 140414 [Lr] Data última revisão: 140414 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 140304 [St] Status: MEDLINE

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