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[PMID]: 28841528 [Au] Autor: Lavtizar V; Kimura D; Asaoka S; Okamura H [Ad] Endereço: Laboratory of Maritime Environmental Management, Research Center for Inland Seas, Kobe University, 5-1-1 Fukaeminami, Higashinada-ku, Kobe, Hyogo 658-0022, Japan. [Ti] Título: The influence of seawater properties on toxicity of copper pyrithione and its degradation product to brine shrimp Artemia salina. [So] Source: Ecotoxicol Environ Saf;147:132-138, 2018 Jan. [Is] ISSN: 1090-2414 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Copper pyrithione (CuPT) is a biocide, used worldwide to prevent biofouling on submerged surfaces. In aquatic environments it rapidly degrades, however, one of the degradation products (HPT) is known to react with cupric ion back to its parent compound. Not much is known about the behavior and toxicity of CuPT and its degradation product HPT in different water systems. Hence, our aim was to investigate the ecotoxicity of CuPT, HPT as well as Cu to the brine shrimp Artemia salina in natural seawater and organic matter-free artificial seawater. Moreover, in order to elucidate the influence of ionic strength of water on CuPT toxicity, tests were performed in water media with modified salinity. The results showed that CuPT was the most toxic to the exposed crustaceans in a seawater media with the highest salinity and with no organic matter content. HPT in a presence of cupric ion converted to CuPT, but the measured CuPT concentrations and the mortality of A. salina in natural water were lower than in artificial water. The toxicity of CuPT to A. salina was significantly influenced by the organic matter content, salinity, and proportions of constituent salts in water. In a combination with cupric ion, non-hazardous degradation product HPT exhibits increased toxicity due to its rapid transformation to its parent compound. [Mh] Termos MeSH primário: Artemia/efeitos dos fármacos Desinfetantes/toxicidade Compostos Organometálicos/toxicidade Piridinas/toxicidade Água do Mar/química Tionas/toxicidade Poluentes Químicos da Água/toxicidade [Mh] Termos MeSH secundário: Animais Desinfetantes/análise Monitoramento Ambiental/métodos Substâncias Húmicas/análise Compostos Organometálicos/análise Piridinas/análise Salinidade Tionas/análise Poluentes Químicos da Água/análise [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Disinfectants); 0 (Humic Substances); 0 (Organometallic Compounds); 0 (Pyridines); 0 (Thiones); 0 (Water Pollutants, Chemical); 0 (copper pyrithione); 6GK82EC25D (pyrithione) [Em] Mês de entrada: 1803 [Cu] Atualização por classe: 180309 [Lr] Data última revisão: 180309 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170826 [St] Status: MEDLINE

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[PMID]: 29378554 [Au] Autor: Nesa ML; Karim SMS; Api K; Sarker MMR; Islam MM; Kabir A; Sarker MK; Nahar K; Asadujjaman M; Munir MS [Ad] Endereço: Department of Pharmacy, Atish Dipankar University of Science and Technology, Dhaka, Bangladesh. luthfunnesa_ph@yahoo.com. [Ti] Título: Screening of Baccaurea ramiflora (Lour.) extracts for cytotoxic, analgesic, anti-inflammatory, neuropharmacological and antidiarrheal activities. [So] Source: BMC Complement Altern Med;18(1):35, 2018 Jan 30. [Is] ISSN: 1472-6882 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: BACKGROUND: It has been observed that the various part of Baccaurea ramiflora plant is used in rheumatoid arthritis, cellulitis, abscesses, constipation and injuries. This plant also has anticholinergic, hypolipidemic, hypoglycemic, antiviral, antioxidant, diuretic and cytotoxic activities. The present studyaimed to assess the cytotoxic, analgesic, anti-inflammatory, CNS depressant and antidiarrheal activities of methanol extract of Baccaurea ramiflora pulp and seeds in mice model. METHODS: The cytotoxic activity was determined by brine shrimp lethality bioassay; anti-nociceptive activity was determined by acetic acid-induced writhing, formalin- induced licking and biting, and tail immersion methods. The anti-inflammatory, CNS depressant and anti-diarrheal activities were assessed by carrageenan-induced hind paw edema, the open field and hole cross tests, and castor oil-induced diarrheal methods, respectively. The data were analyzed by one way ANOVA (analysis of variance) followed by Dunnett's test. RESULTS: In brine shrimp lethality bioassay, the LC values of the methanol extracts of Baccaurea ramiflora pulp and seed were 40 µg/mL and 10 µg/mL, respectively. Our investigation showed that Baccaurea ramiflora pulp and seed extracts (200 mg/kg) inhibited acetic acid induced pain 67.51 and 66.08%, respectively (p < 0.05) that was strongly comparable with that of Ibuprofen (72%) (p < 0.05). The Baccaurea ramiflora pulp and seed extracts (200 mg/kg) significantly (p < 0.05) reduced 58.5 and 53.4 in early and 80.8%, 76.61% in late phase of formalin-induced licking and biting. At 60 and 90 min pulp and seed extracts (200 mg/kg) inhibited nociception of thermal stimulus 50.16 and 62.4%, respectively (p < 0.05) which was comparable with the standard (morphine, 75.9% inhibition). The pulp and seed extracts (200 mg/kg) significantly (p < 0.05) reduced inflammation (42.00 and 55.22%, respectively) in carrageenan-induced hind paw edema and defecations (59.7 and 63.03%, respectively) in castor oil induced diarrhea. Both the extracts showed high sedative activity at 30, 60, 90, and 120 min. CONCLUSION: Our investigation demonstrated significant cytotoxic, analgesic, anti-inflammatory, CNS depressant and antidiarrheal activities of methanol extract of Baccaurea ramiflora pulp and seeds (200 mg/kg). [Mh] Termos MeSH primário: Analgésicos/farmacologia Anti-Inflamatórios/farmacologia Antidiarreicos/farmacologia Depressores do Sistema Nervoso Central/farmacologia Extratos Vegetais/farmacologia [Mh] Termos MeSH secundário: Analgésicos/química Animais Anti-Inflamatórios/química Antidiarreicos/química Artemia/efeitos dos fármacos Comportamento Animal/efeitos dos fármacos Depressores do Sistema Nervoso Central/química Diarreia Masculino Camundongos Manejo da Dor Extratos Vegetais/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Analgesics); 0 (Anti-Inflammatory Agents); 0 (Antidiarrheals); 0 (Central Nervous System Depressants); 0 (Plant Extracts) [Em] Mês de entrada: 1803 [Cu] Atualização por classe: 180305 [Lr] Data última revisão: 180305 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 180131 [St] Status: MEDLINE [do] DOI: 10.1186/s12906-018-2100-5

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[PMID]: 29361962 [Au] Autor: Fatima I; Kanwal S; Mahmood T [Ad] Endereço: Department of Plant Sciences, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan. [Ti] Título: Evaluation of biological potential of selected species of family Poaceae from Bahawalpur, Pakistan. [So] Source: BMC Complement Altern Med;18(1):27, 2018 Jan 24. [Is] ISSN: 1472-6882 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: BACKGROUND: Oxidative stress as well as bacterial and fungal infections are common source of diseases while plants are source of medication for curative or protective purposes. Hence, aim of study was to compare the pharmacological potential of seven grass species in two different solvents i.e. ethanol and acetone. METHODS: Preliminary phytochemical tests were done and antioxidant activities were evaluated using ELISA and their IC50 values and AAI (%) were recorded. ANOVA was used for statistical analyses. DNA damage protection assay was done using p1391Z plasmid DNA and DNA bands were analyzed. Antimicrobial activity was done via disc diffusion method and MIC and Activity Index were determined. Cytotoxic activity was carried out using the brine shrimps' assay and LC50 values were calculated using probit analysis program. RESULTS: Phytochemical studies confirmed the presence of secondary metabolites in most of the plant extracts. Maximum antioxidant potential was revealed in DiAEE, DiAAE (AAI- 54.54% and 43.24%) and DaAEE and DaAAE (AAI- 49.13% and 44.52%). However, PoAEE and PoAAE showed minimum antioxidant potential (AAI- 41.04% and 34.11%). SaSEE, DiAEE and ElIEE showed very little DNA damage protection activity. In antimicrobial assay, DaAEE significantly inhibited the growth of most of the microbial pathogens (nine microbes out of eleven tested microbes) among ethanol extracts while DaAAE and ImCAE showed maximum inhibition (eight microbes out of eleven tested microbes) among acetone plant extracts. However, PoAEE and PoAAE showed least antimicrobial activity. F. oxysporum and A. niger were revealed as the most resistant micro-organisms. ImCEA and ImCAE showed maximum cytotoxic potential (LC50 11.004 ppm and 7.932 ppm) as compared to the other plant extracts. CONCLUSION: Fodder grasses also contains a substantial phenols and flavonoids contents along with other secondary metabolites and, hence, possess a significant medicinal value. Ethanol extracts showed more therapeutic potential as compared to the acetone extracts. This study provides experimental evidence that the selected species contains such valuable natural compounds which can be used as medicinal drugs in future. [Mh] Termos MeSH primário: Antioxidantes/farmacologia Extratos Vegetais/farmacologia Poaceae/química [Mh] Termos MeSH secundário: Animais Anti-Infecciosos/química Anti-Infecciosos/farmacologia Antioxidantes/química Artemia/efeitos dos fármacos Bactérias/efeitos dos fármacos Dano ao DNA/efeitos dos fármacos Flavonoides/química Flavonoides/farmacologia Fungos/efeitos dos fármacos Paquistão Fenóis/química Fenóis/farmacologia Extratos Vegetais/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Infective Agents); 0 (Antioxidants); 0 (Flavonoids); 0 (Phenols); 0 (Plant Extracts) [Em] Mês de entrada: 1803 [Cu] Atualização por classe: 180305 [Lr] Data última revisão: 180305 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 180125 [St] Status: MEDLINE [do] DOI: 10.1186/s12906-018-2092-1

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[PMID]: 29195214 [Au] Autor: Murugesan B; Sonamuthu J; Pandiyan N; Pandi B; Samayanan S; Mahalingam S [Ad] Endereço: Advanced Green Chemistry Lab, Department of Industrial Chemistry, School of Chemical Sciences, Alagappa University, Karaikudi 630 003, Tamil Nadu, India. [Ti] Título: Photoluminescent reduced graphene oxide quantum dots from latex of Calotropis gigantea for metal sensing, radical scavenging, cytotoxicity, and bioimaging in Artemia salina: A greener route. [So] Source: J Photochem Photobiol B;178:371-379, 2018 Jan. [Is] ISSN: 1873-2682 [Cp] País de publicação: Switzerland [La] Idioma: eng [Ab] Resumo: In this work, we report the fabrication of green fluorescent reduced graphene oxide quantum dots (rGOQDs) from the latex of Calotropis gigantea by simple one-step microwave assisted greener route. The latex of Calotropis gigantea calcined at 300°C and its ethanolic extract is used for the synthesis of QDs, The rGOQDs showed particle size ranging from 2 to 8nm and it exhibited green fluorescent in longer UV region at 360-520nm. The rGOQDs graphitic nature was confirmed by RAMAN and XRD analysis. The FTIR, XPS demonstrate that presence of functional groups such as CO, COC, -OH, hence it's addressing them as rGOQDs. It is used to design the greener and economically adopted fluorescent probe for the detection of Pb ions. It provides simple and appropriate for the selective and sensitive detection of Pb ions in water purification process. It also trapped the free radicals and neutralized that and act as an excellent radical scavenger in DPPH radical scavenging assessment. These rGOQDs showed excellent biocompatibility on brine shrimp nauplii (Artemia salina) up to 160µg/mL for 24h incubation. Furthermore, rGOQDS were demonstrated as fluorescent bioimaging probe selectively in the inner digestion part of Artemia salina. In summary, stable, economically viable, highly biocompatible, greener method based rGOQDs were prepared for heavy metal ion detecting, radical scavenging, bioimaging applications which can play a vital role in the future nanotechnology-based biomedical field. [Mh] Termos MeSH primário: Artemia/metabolismo Calotropis/química Depuradores de Radicais Livres/química Grafite/química Pontos Quânticos/química [Mh] Termos MeSH secundário: Animais Artemia/química Artemia/efeitos dos fármacos Materiais Biocompatíveis/química Materiais Biocompatíveis/toxicidade Calotropis/metabolismo Técnicas Eletroquímicas Corantes Fluorescentes/química Íons/química Látex/química Chumbo/análise Microscopia Eletrônica de Transmissão Microscopia de Fluorescência Micro-Ondas Óxidos/química Tamanho da Partícula Pontos Quânticos/toxicidade Espectroscopia de Infravermelho com Transformada de Fourier [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Biocompatible Materials); 0 (Fluorescent Dyes); 0 (Free Radical Scavengers); 0 (Ions); 0 (Latex); 0 (Oxides); 2P299V784P (Lead); 7782-42-5 (Graphite) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180212 [Lr] Data última revisão: 180212 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171202 [St] Status: MEDLINE

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[PMID]: 29175602 [Au] Autor: Thangaraj M; Gengan RM; Ranjan B; Muthusamy R [Ad] Endereço: Department of Chemistry, Faculty of Applied Sciences, Durban University of Technology, Durban 4001, South Africa. [Ti] Título: Synthesis, molecular docking, antimicrobial, antioxidant and toxicity assessment of quinoline peptides. [So] Source: J Photochem Photobiol B;178:287-295, 2018 Jan. [Is] ISSN: 1873-2682 [Cp] País de publicação: Switzerland [La] Idioma: eng [Ab] Resumo: A series of quinoline based peptides were synthesized by a one-pot reaction through Ugi-four component condensation of lipoic acid, cyclohexyl isocyanide, aniline derivatives and 2-methoxy quinoline-3-carbaldehyde derivatives under microwave irradiation. The products were obtained in excellent yields and high purity. Solvent optimization and the effect of microwave irradiation with various powers were also observed. All the synthesized compounds were characterized by FTIR, NMR spectral data and elemental analysis. A total of eight peptides were subjected to antimicrobial, antioxidant and toxicity evaluation. Among them, four peptides showed potential towards antibacterial screening with Bacillus cereus, Staphylococcus aureus, Escherichia coli, Enterococcus faecalis and Candida albicans, Candida utilis and three peptides showed antioxidant test positive (DPPH). Besides, toxicity of all the peptides were evaluated by using brine shrimp and it was observed that four peptides showed mortality rate less than 50% up to 48h. Molecular docking studies revealed that the higher binding affinity of the two peptides toward DNA gyrase than ciprofloxacin based on Libdock score. The described chemistry represents a facile tool to synthesize complex heterocycles of pharmaceutical relevance in a highly efficient and one-pot fashion. The advantages of this method are its green approach, inexpensive solvent, shorter reaction times and excellent yields. [Mh] Termos MeSH primário: Anti-Infecciosos/síntese química Antioxidantes/química Simulação de Acoplamento Molecular Peptídeos/química Quinolinas/química [Mh] Termos MeSH secundário: Animais Anti-Infecciosos/química Anti-Infecciosos/farmacologia Artemia/efeitos dos fármacos Artemia/crescimento & desenvolvimento Bacillus cereus/efeitos dos fármacos Sítios de Ligação Candida/efeitos dos fármacos DNA Girase/química DNA Girase/metabolismo Enterococcus faecalis/efeitos dos fármacos Escherichia coli/efeitos dos fármacos Testes de Sensibilidade Microbiana Peptídeos/síntese química Estrutura Terciária de Proteína Staphylococcus aureus/efeitos dos fármacos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Infective Agents); 0 (Antioxidants); 0 (Peptides); 0 (Quinolines); E66400VT9R (quinoline); EC 5.99.1.3 (DNA Gyrase) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180212 [Lr] Data última revisão: 180212 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171128 [St] Status: MEDLINE

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[PMID]: 27775125 [Au] Autor: Cásedas G; Les F; Gómez-Serranillos MP; Smith C; López V [Ad] Endereço: Department of Pharmacy, Faculty of Health Sciences, Universidad San Jorge, 50.830 Villanueva de Gállego, Zaragoza, Spain. ilopez@usj.es. [Ti] Título: Bioactive and functional properties of sour cherry juice (Prunus cerasus). [So] Source: Food Funct;7(11):4675-4682, 2016 Nov 09. [Is] ISSN: 2042-650X [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Sour cherry juice (Prunus cerasus) is consumed as a nutritional supplement claiming health effects. The aim of the study was to evaluate the different properties of sour cherry juice in terms of antioxidant activity and inhibition of target enzymes in the central nervous system and diabetes. The content of polyphenols and anthocyanins was quantified. Different experiments were carried out to determine the radical scavenging properties of the juice. The activity of sour cherry juice was also tested in physiological relevant enzymes of the central nervous system (acetylcholinesterase, monoamine oxidase A, tyrosinase) and others involved in type 2 diabetes (α-glucosidase, dipeptidyl peptidase-4). Sour cherry juice showed significant antioxidant effects but the activity of the lyophilized juice was not superior to compounds such as ascorbic, gallic or chlorogenic acid. Furthermore, sour cherry juice and one of its main polyphenols known as chlorogenic acid were also able to inhibit monoamine oxidase A and tyrosinase as well as enzymes involved in diabetes. This is the first time that sour cherry juice is reported to inhibit monoamine oxidase A, α-glucosidase and dipeptidyl peptidase-4 in a dose dependent manner, which may be of interest for human health and the prevention of certain diseases. [Mh] Termos MeSH primário: Artemia/efeitos dos fármacos Sucos de Frutas e Vegetais/análise Prunus avium/química [Mh] Termos MeSH secundário: Animais Antioxidantes Bioensaio Sobrevivência Celular Alimento Funcional Células HeLa Seres Humanos Compostos Fitoquímicos/química Compostos Fitoquímicos/metabolismo Superóxidos/química alfa-Glucosidases/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antioxidants); 0 (Phytochemicals); 11062-77-4 (Superoxides); EC 3.2.1.20 (alpha-Glucosidases) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180201 [Lr] Data última revisão: 180201 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161025 [St] Status: MEDLINE

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[PMID]: 29199218 [Au] Autor: Mohareb RM; Abbas NS; Ibrahim RA [Ad] Endereço: Department of Chemistry, Faculty of Science, Cairo University. [Ti] Título: Uses of Cyclohexan-1,4-dione for the Synthesis of 2-Amino-4,5-dihydrobenzo[b]thiophen-6(7H)-one Derivatives with Anti-proliferative and Pim-1 Kinase Activities. [So] Source: Chem Pharm Bull (Tokyo);65(12):1117-1131, 2017. [Is] ISSN: 1347-5223 [Cp] País de publicação: Japan [La] Idioma: eng [Ab] Resumo: The reaction of cyclohexan-1,4-dione with elemental sulfur and any of the 2-cyano-N-arylacetamide derivatives 2a-c gave the 2-amino-4,5-dihydrobenzo[b]thiophen-6(7H)-one derivatives 3a-c to be used in some heterocyclization reactions. The multicomponent reactions of any of compounds 3a-c with aromatic aldehydes 6a-c and either of malononitrile or ethylcyanoacetate gave the 5,9-dihydro-4H-thieno[2,3-f]chromene derivatives 9a-r, respectively. The anti-proliferative evaluation of the newly synthesized compounds against the six cancer cell lines A549, HT-29, MKN-45, U87MG, SMMC-7721 and H460 showed that the nine compounds 3c, 5c, 9e, 9h, 9i, 9j, 9l, 9q, 11e and 13e with highest cytotoxcity. Toxicity of these compounds against shrimp larvae revealed that compounds 3c, 9j, 9q, and 13e showed no toxicity against the tested organisms. The c-Met kinase inhibition of the most potent compounds showed that compounds 9j, 9q, 10e, 12e and 13e have the highest activities. Compounds 9j, 9l, 9q and 11e showed high activity towards tyrosine kinases. Moreover, compounds 9j, 9q and 13e showed the highest inhibitor activity towards Pim-1 kinase. [Mh] Termos MeSH primário: Cicloexanonas/química Inibidores de Proteínas Quinases/síntese química Proteínas Proto-Oncogênicas c-pim-1/antagonistas & inibidores Tiofenos/química [Mh] Termos MeSH secundário: Células A549 Animais Antineoplásicos/síntese química Antineoplásicos/química Antineoplásicos/farmacologia Artemia/efeitos dos fármacos Linhagem Celular Tumoral Proliferação Celular/efeitos dos fármacos Ensaios de Seleção de Medicamentos Antitumorais Células HT29 Seres Humanos Inibidores de Proteínas Quinases/química Inibidores de Proteínas Quinases/farmacologia Proteínas Proto-Oncogênicas c-met/antagonistas & inibidores Proteínas Proto-Oncogênicas c-met/metabolismo Proteínas Proto-Oncogênicas c-pim-1/metabolismo Relação Estrutura-Atividade Tiofenos/síntese química Tiofenos/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antineoplastic Agents); 0 (Cyclohexanones); 0 (Protein Kinase Inhibitors); 0 (Thiophenes); 073790YQ2G (benzothiophene); EC 2.7.10.1 (Proto-Oncogene Proteins c-met); EC 2.7.11.1 (Proto-Oncogene Proteins c-pim-1) [Em] Mês de entrada: 1801 [Cu] Atualização por classe: 180110 [Lr] Data última revisão: 180110 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171205 [St] Status: MEDLINE [do] DOI: 10.1248/cpb.c17-00582

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[PMID]: 29101486 [Au] Autor: Sunil Kumar D; Janakiram P; Murali Krishna Kumar M; Krishna Geetha G [Ad] Endereço: Department of Marine Living Resources, Andhra University, Visakhapatnam, Andhra Pradesh, 530003, India. [Ti] Título: Inhibitory activity of bio-active compounds isolated from Anadara granosa in shrimp health management. [So] Source: World J Microbiol Biotechnol;33(11):207, 2017 Nov 03. [Is] ISSN: 1573-0972 [Cp] País de publicação: Germany [La] Idioma: eng [Ab] Resumo: The crude extract isolated from the visceral mass of Anadara granosa, an intertidal bivalve mollusc was tested for inhibitory activity against pathogenic bacteria of the shrimp and fish viz. Vibrio harveyi and Staphylococcus aureus respectively by agar well diffusion and contact bioautography methods. Maximum inhibitory activity was shown against V. harveyi by methanol and chloroform (9:1) extract. Twelve fractions (1-12) could be separated from the crude extract through column chromatography. Five out of twelve fractions (7, 8, 9, 10, and 11) showed antibacterial activity and they were further run on column chromatography for purity. The fraction no. 9 showed highest antibacterial activity among the five and was subjected to NMR for the proton, C and H -H correlation, IR and mass spectral analysis for structural elucidation. Structure of the compound isolated from fraction no: 9 was determined as 1-(((2Z, 4Z)-dodeca-2,4-dienoyl)oxy)-3-hydroxypropan-2-yl tetradecanoate. [Mh] Termos MeSH primário: Antibacterianos/química Antibacterianos/farmacologia Arcidae/química Artemia/microbiologia Fatores Biológicos/química Fatores Biológicos/farmacologia [Mh] Termos MeSH secundário: Animais Metanol/química Testes de Sensibilidade Microbiana Staphylococcus aureus/efeitos dos fármacos Vibrio/efeitos dos fármacos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Bacterial Agents); 0 (Biological Factors); Y4S76JWI15 (Methanol) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171114 [Lr] Data última revisão: 171114 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171105 [St] Status: MEDLINE [do] DOI: 10.1007/s11274-017-2340-4

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[PMID]: 28893216 [Au] Autor: Satish PVV; Sunita K [Ad] Endereço: Department of Zoology and Aquaculture, Acharya Nagarjuna University, Nagarjuna Nagar 522510, Guntur district, Andhra Pradesh, India. [Ti] Título: Antimalarial efficacy of Pongamia pinnata (L) Pierre against Plasmodium falciparum (3D7 strain) and Plasmodium berghei (ANKA). [So] Source: BMC Complement Altern Med;17(1):458, 2017 Sep 11. [Is] ISSN: 1472-6882 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: BACKGROUND: The objective of the current study was to assess the in vitro antiplasmodial activities of leaf, bark, flower, and the root of Pongamia pinnata against chloroquine-sensitive Plasmodium falciparum (3D7 strain), cytotoxicity against Brine shrimp larvae and THP-1 cell line. For in vivo study, the plant extract which has shown potent in vitro antimalarial activity was tested against Plasmodium berghei (ANKA strain). METHODS: The plant Pongamia pinnata was collected from the herbal garden of Acharya Nagarjuna University of Guntur district, Andhra Pradesh, India. Sequentially crude extracts of methanol (polar), chloroform (non-polar), hexane (non-polar), ethyl acetate (non-polar) and aqueous (polar) of dried leaves, bark, flowers and roots of Pongamia pinnata were prepared using Soxhlet apparatus. The extracts were screened for in vitro antimalarial activity against P. falciparum 3D7 strain. The cytotoxicity studies of crude extracts were conducted against Brine shrimp larvae and THP-1 cell line. Phytochemical analysis of the plant extracts was carried out by following the standard methods. The chemical injury to erythrocytes due to the plant extracts was checked. The in vivo study was conducted on P. berghei (ANKA) infected BALB/c albino mice by following 4-Day Suppressive, Repository, and Curative tests. RESULTS: Out of all the tested extracts, the methanol extract of the bark of Pongamia pinnata had shown an IC value of 11.67 µg/mL with potent in vitro antimalarial activity and cytotoxicity evaluation revealed that this extract was not toxic against Brine shrimp and THP-1 cells. The injury to erythrocytes analysis had not shown any morphological alterations and damage to the erythrocytes after 48 h of incubation. Because methanolic bark extract of Pongamia pinnata has shown good antimalarial activity in vitro, it was also tested in vivo. So the extract had exhibited an excellent activity against P. berghei malaria parasite while decrement of parasite counts was moderately low and dose-dependent (P < 0.05) when compared to the control groups, which shown a daily increase of parasitemia, unlike the CQ-treated groups. The highest concentration of the extract (1000 mg/kg b.wt./day) had shown 83.90, 87.47 and 94.67% of chemo-suppression during Suppressive, Repository, and Curative tests respectively which is almost nearer to the standard drug Chloroquine (5 mg/kg b.wt./day). Thus, the study has revealed that the methanolic bark extract had shown promisingly high ((P < 0.05) and dose-dependent chemo-suppression. The phytochemical screening of the crude extracts had shown the presence of alkaloids, flavonoids, triterpenes, tannins, carbohydrates, phenols, coumarins, saponins, phlobatannins and steroids. CONCLUSIONS: The present study is useful to develop new antimalarial drugs in the scenario of the growing resistance to the existing antimalarials. Thus, additional research is needed to characterize the bioactive molecules of the extracts of Pongamia pinnata that are responsible for inhibition of malaria parasite. [Mh] Termos MeSH primário: Antimaláricos/farmacologia Millettia/química Extratos Vegetais/farmacologia Plasmodium berghei/efeitos dos fármacos Plasmodium falciparum/efeitos dos fármacos [Mh] Termos MeSH secundário: Animais Antimaláricos/química Antimaláricos/toxicidade Artemia/efeitos dos fármacos Linhagem Celular Sobrevivência Celular/efeitos dos fármacos Células Cultivadas Eritrócitos/efeitos dos fármacos Seres Humanos Malária/parasitologia Camundongos Camundongos Endogâmicos BALB C Parasitemia/parasitologia Casca de Planta/química Extratos Vegetais/química Extratos Vegetais/toxicidade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antimalarials); 0 (Plant Extracts) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170918 [Lr] Data última revisão: 170918 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170913 [St] Status: MEDLINE [do] DOI: 10.1186/s12906-017-1958-y

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MEDLINE

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[PMID]: 28870197 [Au] Autor: Zahra SS; Ahmed M; Qasim M; Gul B; Zia M; Mirza B; Haq IU [Ad] Endereço: Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan. [Ti] Título: Polarity based characterization of biologically active extracts of Ajuga bracteosa Wall. ex Benth. and RP-HPLC analysis. [So] Source: BMC Complement Altern Med;17(1):443, 2017 Sep 05. [Is] ISSN: 1472-6882 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: BACKGROUND: The concept of botanical therapeutics has revitalized due to wide importance of plant derived pharmaceuticals. Therefore, the ameliorative characteristics of Ajuga bracteosa were studied. METHODS: Total phenolic content, flavonoid content, antioxidant capacity, reducing power and free-radical scavenging activity were determined colorimetrically. Specific polyphenols were quantified by RP-HPLC analysis. Preliminary cytotoxicity was tested using brine shrimp lethality assay while antiproliferative activity against THP-1 and Hep-G2 cell lines was determined by MTT and SRB protocols respectively. Antileishmanial potential was assessed via MTT colorimetric method. To investigate antidiabetic prospect, α-amylase inhibition assay was adopted whereas disc diffusion method was used to detect likely protein kinase inhibitory, antibacterial and antifungal activities. RESULTS: Among fifteen different extracts, maximum total phenolic content (10.75 ± 0.70 µg GAE/mg DW), total reducing power (23.90 ± 0.70 µg AAE/mg DW) and total antioxidant capacity (11.30 ± 0.80 µg AAE/mg DW) were exhibited by methanol extract with superlative percent extract recovery (17.50 ± 0.80% w/w). Chloroform-methanol extract demonstrated maximum flavonoid content (4.10 ± 0.40 µg QE/mg DW) and ethanol extract exhibited greatest radical scavenging activity (IC 14.40 ± 0.20 µg/ml). RP-HPLC based quantification confirmed polyphenols such as pyrocatechol, gallic acid, resorcinol, catechin, chlorogenic acid, caffeic acid, syringic acid, p-coumaric acid, ferulic acid, vanillic acid, coumarin, sinapinic acid, trans-cinnamic acid, rutin, quercetin and kaempferol. The brine shrimp lethality assay ranked 78.60% extracts as cytotoxic (LC ≤ 250 µg/ml) whereas significant THP-1 inhibition was shown by methanol-acetone extract (IC 4.70 ± 0.43 µg/ml). The antiproliferative activity against Hep-G2 hepatoma cancer cell line was demonstrated by n-hexane, ethylacetate and methanol-distilled water (IC 8.65-8.95 µg/ml) extracts. Methanol extract displayed prominent protein kinase inhibitory activity (MIC 12.5 µg/disc) while n-hexane extract revealed remarkable antileishmanial activity (IC 4.69 ± 0.01 µg/ml). The antidiabetic potential was confirmed by n-hexane extract (44.70 ± 0.30% α-amylase inhibition at 200 µg/ml concentration) while a moderate antibacterial and antifungal activities were unveiled. CONCLUSION: The variation in biological spectrum resulted due to use of multiple solvent systems for extraction. We also deduce that the valuable information gathered can be utilized for discovery of anticancer, antileishmanial, antioxidant and antidiabetic bioactive lead candidates. [Mh] Termos MeSH primário: Ajuga/química Extratos Vegetais/análise Extratos Vegetais/farmacologia [Mh] Termos MeSH secundário: Animais Antioxidantes/análise Antioxidantes/farmacologia Artemia Linhagem Celular Sobrevivência Celular/efeitos dos fármacos Cromatografia Líquida de Alta Pressão Inibidores Enzimáticos/análise Inibidores Enzimáticos/farmacologia Flavonoides/análise Flavonoides/farmacologia Seres Humanos Fenóis/análise Fenóis/farmacologia alfa-Amilases/antagonistas & inibidores alfa-Amilases/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antioxidants); 0 (Enzyme Inhibitors); 0 (Flavonoids); 0 (Phenols); 0 (Plant Extracts); EC 3.2.1.1 (alpha-Amylases) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170908 [Lr] Data última revisão: 170908 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170906 [St] Status: MEDLINE [do] DOI: 10.1186/s12906-017-1951-5

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