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  • About
  • The Global ETD Search service is a free service for researchers to find electronic theses and dissertations. This service is provided by the Networked Digital Library of Theses and Dissertations.
    Our metadata is collected from universities around the world. If you manage a university/consortium/country archive and want to be added, details can be found on the NDLTD website.
21

Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)

Recalde Gil, Maria Angélica January 2015 (has links)
The plant Garcinia gardneriana (Planch. & Triana) Zappi, popularly known in Brazil as "bacupari" has traditionally been used for various types of inflammatory diseases and the evaluation of their chemical composition, mainly of leaves, has resulted in biflavonoids as major compounds. These phenolic compounds have shown anti-inflammatory activity validating the popular use of the plant. In this work was isolated from dried branches of Garcinia gardneriana the biflavonoids: morelloflavone, that is an naringenin covalently linked to luteolin, Gb-2a which is an naringenin linked to eriodictyol and Gb-2a- 7-O-glucose. These compounds have been previously evaluated in various activities such as anti-inflammatory and anti-antioxidants but there is no report of its activity as enzymatic inhibitors. However, the monomers that form it, have been evaluated in the inhibition of aromatase and antidepressant activity with positive outcome, which commonly are used MAO-A inhibitors. In the isolation process were also founded terpenoid compounds as lupeol and friedelin The isolated and purified biflavonoids were used to evaluate enzyme inhibition "in vitro" in monoamine oxidases (MAO-A MAO-B) and aromatase. The compounds showed a positive response even of IC50 5,47 μM and 1,35 μM for MAO-A inhibition of and aromatase enzyme respectively; discovering a way for a new proposal to link both enzymes for treatment of hormone-dependent cancers and anxiety and depression disorders. / La planta Garcinia gardneriana (Planch. & Triana) Zappi, popularmente conocida en Brasil como "bacupari" ha sido tradicionalmente usada para varios tipos de enfermedades inflamatorias y la evaluación de su composición química, principalmente de las hojas, ha resultado en biflavonoides como compuestos mayoritarios. Estos compuestos fenólicos han demostrado actividad anti-inflamatória validando el uso popular de la planta. En este trabajo se asilaron a partir de tallos secos de la Garcinia gardneriana los biflavonoides: moreloflavona, que consiste en una naringenina unida covalentemente a luteolina, Gb-2a que es un compuesto que consiste en una naringenina unida a un eriodictyol y Gb-2a-7-O-glucose. Estos compuestos ya han sido previamente evaluados en diversas actividades como anti inflamatorios y anti antioxidantes pero no se tiene reporte de su actividad como inhibidores enzimáticos. Sin embargo, los monomeros que los conforman han sido evaluados en la inhibición de la aromatasa y con resultados positivos como en la actividad antidepresiva, para la cual comúnmente son usados los inibidores de MAO-A. En el proceso de aislamiento también fueron encontrados compuestos terpenoides como lupeol y friedelina. Los biflavonoides aislados y purificados se usaron para evaluar la inhibición enzimática “in vitro” en monoaminooxidasas (MAO-A, MAO-B) y aromatasa. Los compuestos presentaron una respuesta positiva calculada con IC50 de hasta 5,47 μM y 1,35 μM para la inhibición de las enzimas MAO-A y aromatasa respectivamente, abriendo el camino a una nueva propuesta de relacionar estas dos enzimas para tratamiento de cánceres hormonodependientes y transtornos de ansiedad y depresión.
22

Detecção in silico, isolamento e caracterização estrutural dos constitutintes micromoleculares antimaláricos e antioxidantes em galhosmdemGarcina gardneriana (Clusiaceae) /

Burgos, Rosilene Cristina Rossetto. January 2010 (has links)
Resumo: Este trabalho teve como principais objetivos a detecção, isolamento e elucidação estrutural dos constituintes micromoleculares presentes em folhas e galhos de Garcinia gardneriana, uma espécie da família Clusiaceae com poucos relatos na literatura sobre a sua composição fitoquímica. A detecção das moléculas foi realizada através de abordagens in silico com o estabelecimento de perfis cromatográficos e espectrométricos dos constituintes majoritários dos extratos brutos e frações. A comparação desses dados foi realizada através de dados existentes na literatura. A partir dessa metodologia foi possível detectar 11 triterpenos por GC-FID nos extratos e frações apolares: campesterol (1), estigmasterol (2), β-sitosterol (3), β- amirenona (4), α- amirina (5), β-amirina (6), lupenona (7), lupeol (8), acetato de β-amirina (9), acetato de α-amirina (10), friedelina (11) e mais 9 biflavonóides nos extratos e frações mais polares: xantochimusídeo (12), GB2 (13), fukugisídeo (14), GB 1a glicosilado (15), GB2a (16), morelloflavona (17), volkensiflavona (18), amentoflavona (19), podocarpusflavona (20) e uma benzofenona: 7-epiclusianona (21) através da técnica HPLC-DAD-ESI-MSHRMS. Quanto aos bioensaios in vitro realizados (inibição da polimerização do heme, redução do radical DPPH (antioxidante), inibidor da enzima acetilcolinesterase, tripanocida, citotóxico, antifúngico contra fitopatógenos e patógenos humanos) em todos os extratos e frações preparados, alguns resultados merecem destaque tais como a redução do radical DPPH com IC50 de 9,5, 7,4 e 7,5 μg/mL respectivamente para o extrato etanólico dos galhos, a fração acetato de etila dos galhos e folhas, a inibição da polimerização do heme com valores de 95,7, 98,6 e 68,0 %, de inibição para o extrato etanólico das folhas, e frações acetato de etila das folhas e galhos respectivamente / Abstract: This work had as main objective the detection, isolation and structural elucidation of the micromolecular constituents from leaves and twigs of Garcinia gardneriana, a Clusiaceae species with few literature reports regarding its phytochemical composition. The detection of molecules was performed by in silico detection with the establishment of chromatographic and spectroscopic profiles of the major constituents present in the crude extracts and fractions as well as comparison of data from database and literature reports. Based on this methodology we were able to detect 11 triterpenes by GC-FID in the extracts and nonpolar fractions: campesterol (1), stigmasterol (2), β-sitosterol (3), β-amirenone (4), α- amyrin (5), β-amyrin (6), lupenone (7), lupeol (8), β-amyrin acetate (9), α-amyrin acetate (10), friedelin (11) and more 9 biflavonoids from extracts and fractions polar: xanthochymuside (12) and GB2 (13), fukugiside (14), GB1 glycosylated (15), GB2a (16), morelloflavone (17), volkensiflavone (18), amentoflavone (19) , podocarpusflavone (20), 7-epiclusianone (21) by HPLC-DAD-ESI-MS-HRMS. As for the performed in vitro bioassays (inhibition of heme polymerization, reduction of the DPPH radical (antioxidant), inhibition of the enzyme acetylcholinesterase, trypanocidal, cytotoxic antifungal activity against plant pathogens and human pathogens) in all extracts and fractions prepared in this work, some results are worthy of mentioning such as the reduction of the DPPH radical with IC50 values of 9.5, 7.4 and 7.5 μg/mL respectively for the ethanol extract from twigs, the ethyl acetate fraction from the branches and leaves, as well as the inhibition of heme polymerization with values of 95.7, 98.6 and 68.0% from the ethanol extract from the leaves, and the ethyl acetate fractions leaves and branches / Orientador: Ian Castro Gamboa / Coorientador: Márcia Nasser Lopes / Banca: Mario Sergio Palma / Banca: Carlos Alexandre Carollo / Mestre
23

Potencial antimicrobiano de substâncias extraídas do fruto de Garcinia brasiliensis sobre isolados de Streptococcus spp. obtidos de mastite / Antimicrobial potential of substances extracts from Garcinia brasiliensis fruit on isolates of Streptococcus spp. obtained from mastitis

Maia, Natasha Lagos 01 August 2016 (has links)
Submitted by Marco Antônio de Ramos Chagas (mchagas@ufv.br) on 2017-03-16T11:36:37Z No. of bitstreams: 1 texto completo.pdf: 1129168 bytes, checksum: bd7fe00d19a030146a8ff280ce2feafd (MD5) / Made available in DSpace on 2017-03-16T11:36:37Z (GMT). No. of bitstreams: 1 texto completo.pdf: 1129168 bytes, checksum: bd7fe00d19a030146a8ff280ce2feafd (MD5) Previous issue date: 2016-08-01 / Coordenação de Aperfeiçoamento de Pessoal de Nível Superior / A mastite bovina é uma enfermidade de grande ocorrência em rebanhos leiteiros de todo o mundo, constituindo assim, um cenário preocupante, devido aos impactos na saúde pública e também na economia dos países, principalmente o Brasil, pois é um dos maiores produtores de leite. Concomitantemente à ocorrência da mastite, é crescente o número de isolados bacterianos causadores desta doença que têm apresentado resistência antimicrobiana às mais diversas substâncias farmacológicas, principalmente, devido à utilização indiscriminada destas drogas. A investigação de novas moléculas com potencial antimicrobiano, assim como o uso de associações com as drogas tradicionais, tornou-se de grande necessidade. Este trabalho teve como objetivo, investigar a ação antimicrobiana de duas substâncias bioativas, a gutiferona-A (M11) e 7- epiclusianona (M6), sobre isolados de campo, Streptococcus uberis (Su959) e Streptococcus agalactiae (Sa4605) obtidos de leite de animais com mastite. Realizaram-se testes para definição da Concentração Inibitória Mínima (CIM) dos antimicrobianos sintéticos e das substâncias bioativas, as quais variaram a de 0,6 a 125 μg/mL. Foi confirmado o potencial antimicrobiano destes últimos, além da ineficácia da ampicilina e gentamicina no controle da multiplicação de ambos os isolados. Após esta constatação, foi investigada a presença de interações sinérgicas, utilizando o método Checkerboard a partir de combinações de M11 e M6 com ampicilina e gentamicina. Dentre oito associações determinadas, seis apresentaram interação sinérgica positiva, evidenciando a recuperação e potencialização da ação dos antimicrobianos sintéticos frente aos isolados bacterianos estudados, antes resistentes à ação individual dos mesmos. Usando a metodologia do teste do MTT ((3-[-4,5- dimetil-tiazol-2-il]-2,5-difenil tetrazolium brometo), avaliou-se a viabilidade celular quando da exposição individual de cada antimicrobiano (sintético e bioativo), a fim de conhecer o caráter citotóxico destas sobre as células MAC-T (células epiteliais da glândula mamaria de bovinos). O resultado obtido mostrou que somente a M11 foi citotóxica nas concentrações 2xCIM e 1xCIM determinada previamente na presença de Su959 e 2xCIM determinada previamente na presença de Sa4605. Porém, as concentrações necessárias para potenciar ação dos antimicrobianos sintéticos são doses iguais ou abaixo de 0,5xCIM, não indicadas como tóxicas no teste in vitro. Assim, pode-se afirmar que a gutiferona- A e 7-epiclusianona apresentaram eficaz ação antimicrobiana individual sobre os isolados de campo de Streptococcus uberis e Streptococcus agalactiae, além de se mostrarem promissoras candidatas para serem utilizadas em associações com os antimicrobianos sintéticos ampicilina e gentamicina, a fim de recuperar e otimizar a ação antimicrobiana dos mesmos. / Bovine mastitis is a disease of high occurrence and widespread in herds around the world, making it a worrying scenario due to the impacts on public health and also on the countries’ economies, especially Brazil, due its large produce of milk. In meanwhile, the number of resistant bacterial isolates has been increased against a variety of pharmacological medicines, mostly because of drug-indiscriminate use. The investigation of new molecules with antimicrobial potential, as well as the association with traditional drugs, became a great necessity nowadays. The aim of this study was to investigate the antimicrobial action of two bioactive substances, gutiferone-A (M11) and 7-epiclusianone (M6), on wild isolates Streptococcus uberis (Su959) and Streptococcus agalactiae (Sa4605) obtained from animals infected with mastitis. Analysis were conducted to define the Minimum Inhibitory Concentration (MIC) of synthetic antimicrobials and bioactive molecules, ranging from 0.6 to 125 g/mL. The antimicrobial potential of the latter was confirmed, besides the inefficacy of ampicillin and gentamicin in control of the multiplication of both isolates. Later, the presence of synergistic interactions was investigated, using the Checkerboard method from combinations of M11 and M6 with ampicillin and gentamicin. Among the eight selected associations, six showed positive synergic interaction showing a recovery and powering the action of the synthetic antimicrobials against the bacterial isolates studied, previously resistant to their individual action. To assess the cell viability, we performed the method MTT (3 - [- 4,5-dimethyl-thiazol-2-yl]-2,5-diphenyl tetrazolium bromide), with individual exposure of each antimicrobial (synthetic and bioactive) targeting the MAC-T cells (bovine mammary gland epithelial cells). The results showed that only M11 was cytotoxic at 2xCIM and 1xCIM concentrations previously determined by Su959 presence. However, concentrations doses equal to or lower than 0.5x MIC are need to potentiate the action of synthetic antimicrobials, not indicated as toxic in the in vitro test. Thus, the gutiferone-A and 7- epiclusianone showed an effective antimicrobial action on the wild isolates of Streptococcus uberis and Streptococcus agalactiae, in addition to being promising candidates for use in combinations with the synthetic antimicrobials ampicillin and gentamicin, in order to recover and optimize their antimicrobial action.
24

Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)

Recalde Gil, Maria Angélica January 2015 (has links)
The plant Garcinia gardneriana (Planch. & Triana) Zappi, popularly known in Brazil as "bacupari" has traditionally been used for various types of inflammatory diseases and the evaluation of their chemical composition, mainly of leaves, has resulted in biflavonoids as major compounds. These phenolic compounds have shown anti-inflammatory activity validating the popular use of the plant. In this work was isolated from dried branches of Garcinia gardneriana the biflavonoids: morelloflavone, that is an naringenin covalently linked to luteolin, Gb-2a which is an naringenin linked to eriodictyol and Gb-2a- 7-O-glucose. These compounds have been previously evaluated in various activities such as anti-inflammatory and anti-antioxidants but there is no report of its activity as enzymatic inhibitors. However, the monomers that form it, have been evaluated in the inhibition of aromatase and antidepressant activity with positive outcome, which commonly are used MAO-A inhibitors. In the isolation process were also founded terpenoid compounds as lupeol and friedelin The isolated and purified biflavonoids were used to evaluate enzyme inhibition "in vitro" in monoamine oxidases (MAO-A MAO-B) and aromatase. The compounds showed a positive response even of IC50 5,47 μM and 1,35 μM for MAO-A inhibition of and aromatase enzyme respectively; discovering a way for a new proposal to link both enzymes for treatment of hormone-dependent cancers and anxiety and depression disorders. / La planta Garcinia gardneriana (Planch. & Triana) Zappi, popularmente conocida en Brasil como "bacupari" ha sido tradicionalmente usada para varios tipos de enfermedades inflamatorias y la evaluación de su composición química, principalmente de las hojas, ha resultado en biflavonoides como compuestos mayoritarios. Estos compuestos fenólicos han demostrado actividad anti-inflamatória validando el uso popular de la planta. En este trabajo se asilaron a partir de tallos secos de la Garcinia gardneriana los biflavonoides: moreloflavona, que consiste en una naringenina unida covalentemente a luteolina, Gb-2a que es un compuesto que consiste en una naringenina unida a un eriodictyol y Gb-2a-7-O-glucose. Estos compuestos ya han sido previamente evaluados en diversas actividades como anti inflamatorios y anti antioxidantes pero no se tiene reporte de su actividad como inhibidores enzimáticos. Sin embargo, los monomeros que los conforman han sido evaluados en la inhibición de la aromatasa y con resultados positivos como en la actividad antidepresiva, para la cual comúnmente son usados los inibidores de MAO-A. En el proceso de aislamiento también fueron encontrados compuestos terpenoides como lupeol y friedelina. Los biflavonoides aislados y purificados se usaron para evaluar la inhibición enzimática “in vitro” en monoaminooxidasas (MAO-A, MAO-B) y aromatasa. Los compuestos presentaron una respuesta positiva calculada con IC50 de hasta 5,47 μM y 1,35 μM para la inhibición de las enzimas MAO-A y aromatasa respectivamente, abriendo el camino a una nueva propuesta de relacionar estas dos enzimas para tratamiento de cánceres hormonodependientes y transtornos de ansiedad y depresión.
25

Detecção in silico, isolamento e caracterização estrutural dos constitutintes micromoleculares antimaláricos e antioxidantes em galhosmdemGarcina gardneriana (Clusiaceae)

Burgos, Rosilene Cristina Rossetto [UNESP] 06 August 2010 (has links) (PDF)
Made available in DSpace on 2014-06-11T19:28:32Z (GMT). No. of bitstreams: 0 Previous issue date: 2010-08-06Bitstream added on 2014-06-13T18:34:46Z : No. of bitstreams: 1 burgos_rcr_me_araiq.pdf: 5329390 bytes, checksum: 925b0dcf4d0c43239e31000b7272f966 (MD5) / Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) / Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) / Este trabalho teve como principais objetivos a detecção, isolamento e elucidação estrutural dos constituintes micromoleculares presentes em folhas e galhos de Garcinia gardneriana, uma espécie da família Clusiaceae com poucos relatos na literatura sobre a sua composição fitoquímica. A detecção das moléculas foi realizada através de abordagens in silico com o estabelecimento de perfis cromatográficos e espectrométricos dos constituintes majoritários dos extratos brutos e frações. A comparação desses dados foi realizada através de dados existentes na literatura. A partir dessa metodologia foi possível detectar 11 triterpenos por GC-FID nos extratos e frações apolares: campesterol (1), estigmasterol (2), β-sitosterol (3), β- amirenona (4), α- amirina (5), β-amirina (6), lupenona (7), lupeol (8), acetato de β-amirina (9), acetato de α-amirina (10), friedelina (11) e mais 9 biflavonóides nos extratos e frações mais polares: xantochimusídeo (12), GB2 (13), fukugisídeo (14), GB 1a glicosilado (15), GB2a (16), morelloflavona (17), volkensiflavona (18), amentoflavona (19), podocarpusflavona (20) e uma benzofenona: 7-epiclusianona (21) através da técnica HPLC-DAD-ESI-MSHRMS. Quanto aos bioensaios in vitro realizados (inibição da polimerização do heme, redução do radical DPPH (antioxidante), inibidor da enzima acetilcolinesterase, tripanocida, citotóxico, antifúngico contra fitopatógenos e patógenos humanos) em todos os extratos e frações preparados, alguns resultados merecem destaque tais como a redução do radical DPPH com IC50 de 9,5, 7,4 e 7,5 μg/mL respectivamente para o extrato etanólico dos galhos, a fração acetato de etila dos galhos e folhas, a inibição da polimerização do heme com valores de 95,7, 98,6 e 68,0 %, de inibição para o extrato etanólico das folhas, e frações acetato de etila das folhas e galhos respectivamente / This work had as main objective the detection, isolation and structural elucidation of the micromolecular constituents from leaves and twigs of Garcinia gardneriana, a Clusiaceae species with few literature reports regarding its phytochemical composition. The detection of molecules was performed by in silico detection with the establishment of chromatographic and spectroscopic profiles of the major constituents present in the crude extracts and fractions as well as comparison of data from database and literature reports. Based on this methodology we were able to detect 11 triterpenes by GC-FID in the extracts and nonpolar fractions: campesterol (1), stigmasterol (2), β-sitosterol (3), β-amirenone (4), α- amyrin (5), β-amyrin (6), lupenone (7), lupeol (8), β-amyrin acetate (9), α-amyrin acetate (10), friedelin (11) and more 9 biflavonoids from extracts and fractions polar: xanthochymuside (12) and GB2 (13), fukugiside (14), GB1 glycosylated (15), GB2a (16), morelloflavone (17), volkensiflavone (18), amentoflavone (19) , podocarpusflavone (20), 7-epiclusianone (21) by HPLC-DAD-ESI-MS-HRMS. As for the performed in vitro bioassays (inhibition of heme polymerization, reduction of the DPPH radical (antioxidant), inhibition of the enzyme acetylcholinesterase, trypanocidal, cytotoxic antifungal activity against plant pathogens and human pathogens) in all extracts and fractions prepared in this work, some results are worthy of mentioning such as the reduction of the DPPH radical with IC50 values of 9.5, 7.4 and 7.5 μg/mL respectively for the ethanol extract from twigs, the ethyl acetate fraction from the branches and leaves, as well as the inhibition of heme polymerization with values of 95.7, 98.6 and 68.0% from the ethanol extract from the leaves, and the ethyl acetate fractions leaves and branches
26

Potencial inibitório in vitro de biflavonoides de Garcinia gardneriana : um estudo sobre monoamina oxidades e CYP19 (aromatase)

Recalde Gil, Maria Angélica January 2015 (has links)
The plant Garcinia gardneriana (Planch. & Triana) Zappi, popularly known in Brazil as "bacupari" has traditionally been used for various types of inflammatory diseases and the evaluation of their chemical composition, mainly of leaves, has resulted in biflavonoids as major compounds. These phenolic compounds have shown anti-inflammatory activity validating the popular use of the plant. In this work was isolated from dried branches of Garcinia gardneriana the biflavonoids: morelloflavone, that is an naringenin covalently linked to luteolin, Gb-2a which is an naringenin linked to eriodictyol and Gb-2a- 7-O-glucose. These compounds have been previously evaluated in various activities such as anti-inflammatory and anti-antioxidants but there is no report of its activity as enzymatic inhibitors. However, the monomers that form it, have been evaluated in the inhibition of aromatase and antidepressant activity with positive outcome, which commonly are used MAO-A inhibitors. In the isolation process were also founded terpenoid compounds as lupeol and friedelin The isolated and purified biflavonoids were used to evaluate enzyme inhibition "in vitro" in monoamine oxidases (MAO-A MAO-B) and aromatase. The compounds showed a positive response even of IC50 5,47 μM and 1,35 μM for MAO-A inhibition of and aromatase enzyme respectively; discovering a way for a new proposal to link both enzymes for treatment of hormone-dependent cancers and anxiety and depression disorders. / La planta Garcinia gardneriana (Planch. & Triana) Zappi, popularmente conocida en Brasil como "bacupari" ha sido tradicionalmente usada para varios tipos de enfermedades inflamatorias y la evaluación de su composición química, principalmente de las hojas, ha resultado en biflavonoides como compuestos mayoritarios. Estos compuestos fenólicos han demostrado actividad anti-inflamatória validando el uso popular de la planta. En este trabajo se asilaron a partir de tallos secos de la Garcinia gardneriana los biflavonoides: moreloflavona, que consiste en una naringenina unida covalentemente a luteolina, Gb-2a que es un compuesto que consiste en una naringenina unida a un eriodictyol y Gb-2a-7-O-glucose. Estos compuestos ya han sido previamente evaluados en diversas actividades como anti inflamatorios y anti antioxidantes pero no se tiene reporte de su actividad como inhibidores enzimáticos. Sin embargo, los monomeros que los conforman han sido evaluados en la inhibición de la aromatasa y con resultados positivos como en la actividad antidepresiva, para la cual comúnmente son usados los inibidores de MAO-A. En el proceso de aislamiento también fueron encontrados compuestos terpenoides como lupeol y friedelina. Los biflavonoides aislados y purificados se usaron para evaluar la inhibición enzimática “in vitro” en monoaminooxidasas (MAO-A, MAO-B) y aromatasa. Los compuestos presentaron una respuesta positiva calculada con IC50 de hasta 5,47 μM y 1,35 μM para la inhibición de las enzimas MAO-A y aromatasa respectivamente, abriendo el camino a una nueva propuesta de relacionar estas dos enzimas para tratamiento de cánceres hormonodependientes y transtornos de ansiedad y depresión.
27

Informovanost studentů vybraných školo v oblasti vybraných druhů nutraceutik / Selected schools' students' awareness of selected types of nutraceuticals

Homolková, Zuzana January 2017 (has links)
The main topic of this work is food supplements, their legislation and other theory connected with them, the main focus is on plant nutraceuticals, of which are chosen food supplements marketed to support immunity system - echinacea, sea buckthorn and oyster mushroom, food supplements to support psyche - St. John's wort, ginkgo and valerian and dietary supplements to support body fitness - tribulus, garcinia and psyllium. Subsequently, the topic focuses on the marketing of nutraceuticals, its modern ways and the possibilities of increasing the students' awareness in this field through the principles of media education. In the practical part, 112 students aged 15-19 are presented with a lecture presenting the topic and inviting students to raise their interest in the subject. The feedback of the lecture is provided by a questionnaire whose questions correspond to the hypotheses set by the author. KEYWORDS nutraceuticals, media education, marketing, Echinacea, Garcinia, Pleurotus, Hippophae, Gingko, Plantago, Hypericum, Valeriana, Tribulus
28

Studies of the active constituents of Angelica sinensis and Garcinia hanburyi on colon cancer. / 當歸及藤黃的活性成分對大腸癌的抗癌作用研究 / CUHK electronic theses & dissertations collection / Dang gui ji teng huang de huo xing cheng fen dui da chang ai de kang ai zuo yong yan jiu

January 2010 (has links)
Colorectal cancer is the second leading cause of cancer-related mortality in Hong Kong and lack of selectivity has limited the success of conventional chemotherapy. Given the recent interest in the anti-cancer effects of traditional Chinese medicine (TCM), there are two approaches to studying its bioactivity: as a mixture of ingredients or as single compounds. The objective of the present study is to examine the anti-tumor effects of Angelicae Sinensis Radix (DG) and Garcinia hanburyi resin (TH) using both approaches, respectively, as they are traditionally used to treat inflammation. In the present study, their anti-cancer effects and the mechanisms of actions were examined for the development of potential novel chemotherapeutic drugs for colon cancer since inflammation is a predisposing factor for colon cancer. / DG extract and its three main bioactive phtbalides: n-butylidenephthalide, senkyunolide A and z-ligustilide (LGT), were found to be cytotoxic to HT-29 cells with IC50 values (24 h) of 20.70 +/- 0.85, 72.51 +/- 8.65, 18.74 +/- 1.14 and 41.98 +/- 3.64 mug/ml, respectively. The results evidenced that LGT induced G0/G 1 arrest and apoptosis, triggering cleavage of PARP, pro-caspases-3, -8 and -9 and nuclear fragmentation. LGT and cisplatin synergistically reduced the viability of HT-29 cells. More interestingly, DG extract was more potent than individual phthalides, suggesting that there are other bioactive components and/or synergistic interactions. / Individual compounds purified from TH were investigated because gambogic acid isolated from this herb has been used clinically to treat cancer, 30-Epicambogin (EPC) and guttiferone K (GUTK) showed the highest cytotoxic selectivity and potency on HT-29 cells among 15 isolated compounds. IC50 values (24 h) for EPC and GUTK in HT-29 cells were 5.36+/-0.25 and 5.39+/-0.22 muM, respectively, and both induced G0/G1 arrest by down-regulation of cyclins D1, D3, CDK4 and CDK6, while up-regulation of p21Waf1/CiP1 and p27KiP1. Both compounds triggered the activation of caspases-3, -8 and -9 in apoptosis. The in vivo anti-tumor effects of GUTK were further investigated by using a subcutaneous Colon-26 mouse tumor model. GUTK (10 mg/kg i.p.) reduced tumor volume by 33.6% and potentiated the anti-tumor effects of 5-fluorouracil when administered concurrently. / Our findings revealed that DG rather than individual phthalides, is worthy for further study as a potential anti-cancer drug, due to the synergistic interactions among multi-components in the herb. On the other hand, EPC and GUTK, isolated from TH have potential to be developed as novel anti-tumor candidates for combination use with 5-fluorouracil. The results strongly support the use of different approaches to study TCM for chemotherapy, according to its traditional and empirical use. / Subsequently, the anti-proliferative effects of DG and Chuanxiong Rhizoma (CX) extracts and mixtures containing three phthalides in the proportions similar to their presence in both extracts were examined, since CX also contains the same phthalides, but in different proportions. DG extract was significantly more potent than its corresponding phthalide mixture to inhibit cancer cell proliferation and synergistic interaction was observed among the phthalides and other bioactive components, while the phthalides in CX extract interacted antagonistically with other components. / Kan, Lai Ting Winnie. / Adviser: Ge Lin. / Source: Dissertation Abstracts International, Volume: 73-02, Section: B, page: . / Thesis (Ph.D.)--Chinese University of Hong Kong, 2010. / Includes bibliographical references (leaves 267-311). / Electronic reproduction. Hong Kong : Chinese University of Hong Kong, [2012] System requirements: Adobe Acrobat Reader. Available via World Wide Web. / Electronic reproduction. [Ann Arbor, MI] : ProQuest Information and Learning, [201-] System requirements: Adobe Acrobat Reader. Available via World Wide Web. / Abstract also in Chinese.
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Effects of kolaviron–a Garcinia kola biflavonoid on biochemical and histological parameters in streptozotocin - induced diabetes and diabetic complications (nephrotoxicity and hepatotoxicity) in male Wistar rats

Ayepola, Omolola Rebecca January 2014 (has links)
Thesis submitted in fulfillment of the requirements for the Doctor of Technology: Biomedical Technology In the Faculty of Health and Wellness At the CAPE PENINSULA UNIVERSITY OF TECHNOLOGY 2014 / Diabetes mellitus (DM) results in severe metabolic imbalances and pathological changes in many tissues. Chronic inflammation and oxidative stress have been implicated in the pathophysiology of diabetes mellitus. Garcinia kola (Family: Guttiferae) is a plant well known for its ample medicinal values. The seed of the plant also known as ‘bitter kola’ due to its bitter taste is used as a masticatory agent in traditional hospitality, cultural and social ceremonies in Africa. Kolaviron (KV) is a defatted ethanol extract from the seeds of Garcinia kola (GK). Kolaviron has been shown in experimental models of diseases to have numerous beneficial effects due to the presence of flavonoids (mainly Garcinia biflavonoid (GB)-1, GB-2 and kolaflavanone). However, there is paucity of information regarding the possible effect of kolaviron on inflammatory mediators and oxidative stress in diabetes mellitus. Therefore, this study was carried out to investigate the potential beneficial effects of kolaviron on antioxidant status, inflammatory mediators and apoptosis. Other biochemical and histological alterations in the blood, liver and kidney of streptozotocin-induced diabetic rats were also evaluated. A single intraperitoneal injection of freshly prepared solution of streptozotocin (50 mg/kg.b.wt.) in citrate buffer (0.1M, pH 4.5) was administered to overnight fasted rats for diabetes induction. Diabetes was confirmed by stable hyperglycemia (>18 mmol/l) in the tail blood glucose after 5 days of streptozotocin injection. Kolaviron (100 mg/kg b.wt.) was administered to diabetic rats (by gastric gavage) on the 6th day after the induction of diabetes and treatment continued for 6 weeks (5 times weekly). The effects on blood glucose, body weight, organ (liver and kidney) weight, serum biochemical parameters, oxidative status, inflammatory mediators and histology of the liver, kidney and pancreas were assessed. Kolaviron (KV) treatment lowered blood glucose in diabetic and normoglycemic rats and reduced glycated haemoglobin [HbA1C (%)]. Plasma insulin level was raised in diabetic rats treated with KV. Histomorphometric analysis of the pancreas revealed increased β-cell area of pancreatic islets of kolaviron-treated diabetic group. The indices of organ (liver and kidney) damage were increased in diabetic rats. However, KV treatment protected against liver and kidney damage. The characteristic features of diabetic dyslipidemia such as elevated serum triglyceride and cholesterol concentration which are major risk factors for cardiovascular disease were also significantly reduced in KV-treated diabetic rats. Alteration in antioxidant enzymes status was observed in the liver, kidney and blood (erythrocyte, plasma and serum) of diabetic rats. Lowered catalase (CAT) activity was observed in the liver and kidney of diabetic rats while KV treatment significantly (p < 0.05) elevated catalase activity in the liver and kidney. There was no significant change (p > 0.05) in erythrocyte catalase activity among all treatment groups. Erythrocyte of diabetic rats showed a marked reduction in the activity of superoxide dismutase (SOD) with no significant changes in liver and kidney SOD activity of diabetic rats compared to control whereas KV administration to rats markedly increased SOD activity. Glutathione peroxidase (GPX) activity was elevated in the erythrocyte and kidney of STZ-induced diabetic rats with no significant effect on liver GPX activity. KV treatment reversed the alteration in GPX activity in the kidney and erythrocyte. Level of reduced glutathione (GSH), a non-enzymatic antioxidant was decreased in the both liver and kidney of diabetic rats and treatment of diabetic rats with KV elevated GSH concentration in both tissues. Also, malondialdehyde (MDA), a marker of lipid peroxidation was elevated in the liver, kidney and plasma of diabetic rats and significantly (p < 0.05) lowered following KV treatment. Diabetes induction reduced the capacity of liver and kidney to absorb oxygen radicals as demonstrated by lowered oxygen radical absorbance capacity (ORAC) values. KV administration to normal and diabetic rats significantly increased ORAC values. Increased rate of apoptosis, a major cellular response to high glucose induced stress was observed in the renal and hepatic tissues of diabetic control rats. Kolaviron treatment of diabetic rats protected the liver and kidney against hyperglycemia-induced apoptosis and decreased the number of TUNEL positive cells A significant (p < 0.05) elevation of pro-inflammatory cytokines; monocyte chemoattractant protein (MCP-1), Interleukin-1β (IL-1β), IL-6 and tumor necrosis factor (TNF)-𝛂 was observed in the liver of diabetes rats. KV treatment lowered these inflammatory biomarkers. On the other hand, the kidney of diabetic rats showed elevated concentration of pro-inflammatory IL-1β with no significant effect on kidney TNF-𝛂. An increase in the serum concentration of MCP-1 and IL-1β was observed in the untreated diabetic rats while kolaviron treatment normalized the alteration in serum concentration of MCP-1, IL-1β and vascular endothelial growth factor (VEGF). In conclusion, persistent and chronic hyperglycemia promotes the generation of free radicals and inflammatory molecules which contributes to progressive development of micro- and macro vascular complications and multi-organ damage. Kolaviron demonstrated beneficial effects on markers of oxidative stress and inflammation in the diabetic rats and also promoted the survival and functional integrity of the liver and kidney.
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Síntese de derivados do ácido quínico, genisteína e cluvenona, potenciais agentes antimicrobianos, antitumorais e contra a esclerose múltipla

Rezende Júnior, Celso de Oliveira 18 July 2014 (has links)
Submitted by Renata Lopes (renatasil82@gmail.com) on 2016-02-25T13:51:08Z No. of bitstreams: 1 celsodeoliveirarezendejunior.pdf: 4187877 bytes, checksum: e397d45f85368ea5d9904f085b86462e (MD5) / Approved for entry into archive by Adriana Oliveira (adriana.oliveira@ufjf.edu.br) on 2016-03-03T13:29:51Z (GMT) No. of bitstreams: 1 celsodeoliveirarezendejunior.pdf: 4187877 bytes, checksum: e397d45f85368ea5d9904f085b86462e (MD5) / Made available in DSpace on 2016-03-03T13:29:51Z (GMT). No. of bitstreams: 1 celsodeoliveirarezendejunior.pdf: 4187877 bytes, checksum: e397d45f85368ea5d9904f085b86462e (MD5) Previous issue date: 2014-07-18 / CAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior / Neste trabalho são descritas as sínteses e avaliações biológicas de diferentes classes de compostos orgânicos e está dividido em três capítulos. O primeiro deles descreve a síntese de derivados da genisteína com distintas propriedades físico-químicas, a fim de avaliar a influência dessas propriedades na atividade biológica contra a esclerose múltipla. Foram sintetizados compostos condensados a carboidratos derivados da D-glicose e D-galactose e derivados lipofílicos com cadeias alquila ou acila lineares de doze ou quatorze carbonos. Esses compostos foram submetidos a ensaios de citotoxicidade e anti-inflamatórios in vitro e os compostos mais ativos foram avaliados quanto a sua atividade na modulação da resposta imune in vivo no modelo de encefalomielite auto-imune experimental (EAE). Na síntese dos drivados éteres verificaram-se diferentes reatividades: os compostos com cadeias alquila lineares foram obtidos em rendimentos melhores, seguido dos derivados da D-glicose e D-galactose, respectivamente. A regiosseletividade obtida na síntese dos derivados éteres foi sugerida por nOe, enquanto que nos derivados ésteres foi sugerida por RMN de 1H. Os ensaios biológicos revelaram que todos os compostos apresentaram atividade in vitro e os derivados de carboidrato foram mais citotoxicicos que os derivados com cadeias lipofílicas lineares. Após os ensaios in vivo, o composto 13 foi considerado um protótipo para o tratamento da esclerose múltipla. O segundo capítulo descreve a síntese e avaliação das propriedades antimicrobianas de surfactantes derivados do ácido quínico condensados a diaminas N-alquiladas, variando-se o tamanho da cadeia alquila (parte apolar) e a estrutura do ácido quínico (parte polar), estabelecendo-se uma relação estrutura e atividade. Foram sintetizados 32 compostos através de reações de amidação entre uma lactona derivada do ácido quínico com diaminas Nalquiladas em rendimentos satisfatórios. 17 compostos apresentaram atividades semelhantes ou melhores do que a droga de referência. Também estão sendo realizados alguns ensaios antiparasitários e anti-inflamatórios com esses compostos. O terceiro capítulo descreve a síntese e avaliação das propriedades antitumorais de derivados de xantonas Garcinia, especificamente de cluvenona. Foram sintetizados diversos compostos com grupos retiradores e doadores de eletróns, hidrofílicos e contendo a unidade sal de trifenilfosfônio no anel A de hidroxicluvenonas, que auxiliarão no entendimento da relação estrutura e atividade para essa classe de compostos. Sintetizou-se também um composto derivado da 6- hidroxicluvenona condensada com o BODIPY com potencial atividade antitumoral e propriedades fluorescentes com o objetivo de realizar estudos de localização celular e mecanismo de ação. A etapa chave para a síntese desses compostos foi uma reação em cascata de Claisen/Diels-Alder. / In this work the synthesis and biological evaluation of different classes of organic compounds are described and it is divided into three chapters. The first chapter describes the synthesis of genistein derivatives with different physicochemical properties in order to assess the influence of these properties in biological activity against multiple sclerosis. Carbohydrate derivatives from D-glucose and D-galactose and compounds condensed with lipophilic alkyl or acyl linear chains of twelve or fourteen carbons were synthesized. Cytotoxicity and anti-inflammatory activities in vitro were performed and the most active compounds were evaluated in modulating the immune response in vivo model of experimental autoimmune encephalomyelitis. Reactivity of ethers derivatives was different: compounds with linear alkyl chains were obtained in higher yields, followed by the derivatives of D-glucose and D-galactose, respectively. The regioselectivity obtained in the synthesis of ether derivatives were suggested by nOe, while the ester derivatives were suggested by 1H NMR. All compounds showed in vitro activity and carbohydrate derivatives were more cytotoxic than lipophilic derivatives. After in vivo tests, compound 13 was considered a prototype for the treatment of multiple sclerosis. The second chapter describes the synthesis and evaluation of the antimicrobial properties of surfactants derived from quinic acid (popar part) condensates with N-alkylated diamines (nonpolar part). The size of the alkyl chain and the structure of quinic acid were altered, settling a relationship structure and activity. 32 compounds were synthesized by amidation reactions between a lactone derivative of quinic acid with N-alkylated diamines in satisfactory yields. 17 of these compounds showed equal or better equal activities than the drug reference. Some antiparasitic and anti-inflammatory tests are also being conducted for these compounds. The third chapter describes the synthesis and evaluation of antitumoral properties of derivatives of Garcinia xanthones, specifically cluvenone. Several compounds were synthesized with electron withdrawing and donors groups, containing hydrophilic and the triphenylphosphonium salt unit in the A ring of hidroxicluvenonas. These compounds will help in understanding the structure and activity relationship for this class of compounds. A BODIPY Hydroxicluvenone conjugate compound with potential antitumor activity and fluorescent properties was synthesized with the aim of studying the cellular location and mechanism of action. The key step for the synthesis of these compounds was a reaction cascade Claisen / Diels-Alder reaction.

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