Thesis (M. Phil.)--University of Hong Kong, 2006. / Title proper from title frame. Also available in printed format.

Diabetes mellitus is the most well-known endocrine dilemma suffered by hundreds of million people globally, with an annual mortality of more than one million people. This high mortality rate highlights the need for in-depth study of anti-diabetic agents. This review explores the phytochemical contents and anti-diabetic mechanisms of (cucurbitaceae). Studies show that contains several phytochemicals that have hypoglycemic effects, thus, the plant may be effective in the treatment/management of diabetes mellitus. Also, the biochemical and physiological basis of anti-diabetic actions is explained. exhibits its anti-diabetic effects via the suppression of MAPKs and NF-κβin pancreatic cells, promoting glucose and fatty acids catabolism, stimulating fatty acids absorption, inducing insulin production, ameliorating insulin resistance, activating AMPK pathway, and inhibiting glucose metabolism enzymes (fructose-1,6-bisphosphate and glucose-6-phosphatase). Reviewed literature was obtained from credible sources such as PubMed, Scopus, and Web of Science.

Thesis (MSc.(Biochemistry)) -- University of Limpopo, 2021 / Drug discovery from medicinal plants continues to play an important role in the development of anticancer agents, this is because medicinal plants are reservoirs of bioactive compounds that exert a plethora of pharmacological effects on human beings. This study aimed to analyse the phytochemical constituents of the Momordica cardiospermoides crude acetone and methanol leaf extracts as well as investigate their potential anti-metastatic effects on the MDA-MB-231 breast cancer cell line. Momordica cardiospermoides leaves were extracted with absolute methanol or acetone to produce crude methanol and acetone extracts, respectively. The extracts were then screened and analysed for phytochemicals using thin layer chromatography, qualitative and quantitative phytochemical tests, and their antioxidant activity was determined using the quantitative 2,2-diphenyl-1picrylhydrazyl (DPPH) free radical scavenging activity assay. The fingerprint profiles of the M. cardiospermoides leaf extracts revealed that compounds of the acetone extracts were optimally separated in the nonpolar mobile phase (TAE), whereas those of the methanol extract separated best in the polar mobile phase (EMW), thereby suggesting that the crude acetone and methanol extracts had more non-polar and polar compounds present, respectively. Furthermore, the qualitative phytochemical analysis indicated the presence of various phytochemicals such as flavonoids, steroids, coumarins, and tannins in both plant extracts, however, saponins were found present in the methanol extract and not in the acetone extract. Moreover, quantification of major phytochemicals revealed that the acetone extract had the highest total phenolic content (23.0683 mg GAE/g), total tannin content (22.0442 mg GAE/g) and total flavonoid (32.6933 mg QE/g) content as compared to the methanol extract (14.2349 mg GAE/g, 11.3164 mg GAE/g and 7.692 mg QE/g respectively). The DPPH free radical scavenging activity assay revealed that the extracts exhibited an increase in percentage inhibition/ DPPH scavenging effect, with an increase in extract concentration. The results also revealed that the acetone extract possessed a higher radical scavenging activity as compared to the methanol extract. These results are in correlation with the quantitative analysis of the extracts, as all the major phytochemicals found in higher amounts in the acetone extract have antioxidant properties. The extracts were then assessed in vitro for their cytotoxic effects on MDA MB-231 breast cancer cells and HEK 293 cells using the cell count and viability assay and the results obtained revealed a concentration-dependent decrease in the viability of MDA-MB-231 cells at 24 hours of treatment with either the acetone or methanol extract. Comparatively, treatment of HEK 293 cells with the acetone extract resulted in a significant decrease in the percentage of viable cells, whereas treatment with the methanol extract had no significant effect on the viability of HEK 293 cells, as the percentage of viable cells was maintained at 85–98% at 24 hours of treatment. These results also revealed that the methanol extract is more selective to cancer cells in comparison to the acetone extract, suggesting that the methanol extract is a better antineoplastic candidate. The mode of cell death induced by the methanol or acetone extracts was assessed using the acridine orange and ethidium bromide dual staining assay and the annexin V and dead cell kit. The results from the acridine orange/ethidium bromide dual staining assay showed that both extracts induced nuclei and cellular morphological changes in a concentration-depended manner, at 24 hours of treatment. Moreover, the annexin V and dead assay kit results revealed that the acetone extract induced necrotic cell death, while the methanol extract induced apoptotic cell death. Since the acetone extract was shown to be non-selective towards normal cells and induced necrotic cell death, it was discontinued for further assays. The effect of the methanol extract on MDA-MB-231 cell migration and attachment was determined using the wound healing assay and the adhesion assay. The results revealed that treatment with 150 or 300 µg/ml significantly suppressed MDA-MB-231 cell migration, associated with serpin E1 downregulation and TIMP-1 upregulation, at 24 hours of treatment. Moreover, treatment with the methanol extract also significant inhibited MDA-MB-231 cell adhesion in a concentration-dependent manner, as evident by the decrease in the number of crystal violet stained cells. The effect of the methanol extract on the expression of matrix metalloproteinase-2 and -9 was assessed using western blotting, and the results revealed that the extract significantly downregulated the expression of both MMP-2 and -9, suggesting that the methanol extract has inhibitory effects on MDA-MB-231 cell invasion. The human angiogenesis antibody array kit was then used to determine the effect of the extract on the expression of angiogenesis-related proteins. Treatment with 150 or 300 µg/ml of the extract significantly upregulated the expression levels of tissue inhibitor of metalloproteinases (TIMP) -1 and thrombospondin-1 in a concentration-dependent manner. The results also revealed a significant downregulation in the expression of serpin E1, in a concentration-dependent manner, in comparison to the untreated control. However, the expression of uPA, VEGF, and IGFBP-1, 2 and -3 was upregulated following treatment with 150 and 300 µg/ml of the extract. In conclusion, the current study demonstrated the potential of M. cardiospermoides crude methanol extract as an effective anti-metastatic agent or a source of compounds with anti-metastatic properties / South African Medical Research Council (SAMRC) Research Capacity Development Initiative and National Research Foundation (NRF)

L’arille de Momordica cochinchinensis (gac), un fruit de la famille des Cucurbitacées, est la source végétale la plus riche en lycopène et β-carotène. Ces deux composés ont, respectivement, un rôle de puissant antioxydant et de provitamine A, intéressant les compléments santé. Tout d'abord, un procédé d’extraction fractionnée douce a été développé pour extraire ces caroténoïdes naturels en gardant leur qualité originale. Puis, le lycopène et le β-carotène extraits ont été caractérisés et analysés. Au moins 95 % des extraits sont composés de l’isomère all-trans. Ils ne sont pas dégradés pendant le traitement thermique représentant les procédés de formulation. Leur stéréo-mutation thermique a été évaluée. Le lycopène est plus antioxydant et donc plus rapidement isomérisé que le β-carotène à haute température. L’isomérisation augmente leur activité antioxydante, qui a été évalué par test chimique TEAC et sur l’hémolyse des cellules sanguines (KRL) in vitro. Les deux caroténoïdes de l’arille de gac sont beaucoup plus antioxydants que le Trolox contre l’hémolyse. En comparant avec d’autres sources de β-carotène, les caroténoïdes extraits de gac dans ces conditions douces restent antioxydants même à des concentrations plus élevées contrairement à ceux extraits dans des conditions classiques qui deviennent prooxydants. Ces résultats permettent de discuter la bioactivité des caroténoïdes d'après leur qualité et de leur origine, c’est à dire leur source et leur procédé d’extraction. D’un point de vue applicatif, outre le procédé de fractionnement qui est industrialisable, le traitement thermique appliqué permet de contrôler la fonctionnalité des produits riches en caroténoïdes. / The aril of Momordica cochinchinensis (gac), plant from the Cucurbitaceae family, is the richest source of lycopene and β-carotene, which are a strong antioxidant and a pro-vitamin A, respectively, interesting for health-complements. First, a process of soft extraction-fractionation was developed for extracting effectively the natural carotenoids from gac without loss of their original quality. Then, the lycopene and β-carotene extracted from gac were analyzed and characterized. At least 95% of the extracts were composed of the all-trans isomer. They were not degraded during the heat-treatment mimicking formulation processing. Their thermal stereo-mutation was evaluated. Lycopene is more antioxidant, it is thus isomerized more rapidly than β-carotene at high temperature. The isomerization of carotenoids increases their antioxidant activity that was evaluated by the chemical test TEAC and through the hemolysis of red blood cells (KRL) in vitro. The lycopene and β-carotene from gac are notably more antioxidant than Trolox. By comparing with other sources of β-carotene, carotenoids extracted from gac in these soft conditions keep their antioxidant properties, even at high concentration, contrasting with extracts obtained in classical conditions that become prooxidant. From these results, the bioactivity of carotenoids is discussed from their quality and their origin that is their source and extraction process. For application, in addition to the fractionation process which is easily transferable to the industry scale, the heat-treatment used in this study is interesting for controlling products rich in functional carotenoids

Submitted by Mario BC (mario@bc.ufrpe.br) on 2016-09-19T12:32:08Z No. of bitstreams: 1 Fabian Santana Silva.pdf: 2324497 bytes, checksum: 5c4e600acdaff03ee633bf78d5a2a9d2 (MD5) / Made available in DSpace on 2016-09-19T12:32:08Z (GMT). No. of bitstreams: 1 Fabian Santana Silva.pdf: 2324497 bytes, checksum: 5c4e600acdaff03ee633bf78d5a2a9d2 (MD5) Previous issue date: 2016-02-19 / In Brazil, the snapmelons of momordica botanical group are known in different regions of the country such as melon caxi, meloite, melon papoco and snow melon. There are few reports in the literature with snapmelons, requiring studies aimed at understanding the genetic variability. This study aimed to evaluate the melon caxi access reactions the Meloidogyne enterolobii and M. javanica, and then select the promising genotypes for the crop breeding program for resistance to root knot nematode UFRPE. The isolated M. enterolobii e M. javania they was kept in pure wing vegetation and multiplied in susceptible tomato plants. The extraction of the eggs was performed according to the technique proposed by Hussey &Barker (1973) and modified by Bonetti & Ferraz (1981). The experiments carried out in a randomized block design were conducted in the period February to April 2015, and from October to December of the same year. These experiments were conducted in a protected environment with the sowing of accesses made in PVC tubes containing commercial substrate Basaplant®. Infestation was performed of each species separately in egg suspension ratio of 3000 eggs.tubete-1. 45 days after the infestation of the seedlings, we proceeded to the evaluation of the hits, where the roots were washed for counting the number of galls per root system. After counting galls, the eggs were extracted from the roots of melon plants by technical Hussey and Barker (1973), modified by Boneti and Ferraz (1981). The thus obtained eggs were counted using a stereomicroscope, obtaining the number of eggs per root system. The reproduction factor: FR ≥ 1 indicate good host, FR <1.0 poor host and FR = 0 host not based on the classification proposed by Oostenbrink (1966). All tested accessions showed FR> 1 proved to be good hosts for M. enterolobii and M. javania. / No Brasil, os snapmelons do grupo botânico momordica são conhecidos em diferentes regiões do país como melão caxi, meloite, melão papoco e melão de neve. Existem poucos relatos na literatura com os snapmelons, necessitando de estudos que visem o conhecimento da variabilidade genética. O presente trabalho teve como objetivo avaliar as reações de acessos de melão caxi à Meloidogyne enterolobii e M. javania e, posteriormente, selecionar os genótipos promissores com resistência aos nematoides das galhas para o programa de melhoramento da cultura para da UFRPE. Os isolados de M. enterolobii e M. javania foram mantidos puros em casa de vegetação e multiplicados separadamente em plantas de tomate suscetíveis. A extração dos ovos foi realizada conforme técnica proposta por Hussey e Barker (1973) e modificada por Bonetti e Ferraz (1981). Os experimentos foram em blocos casualizados, sendo conduzidos no período de fevereiro a abril de 2015, e de outubro a dezembro do mesmo ano. Esses experimentos foram realizados em ambiente protegido com a semeadura dos acessos realizada em tubetes de PVC contendo substrato comercial Basaplant®. Foi realizada a infestação do substrato com uma suspensão de ovos de cada espécie separadamente na proporção de 3000 ovos.tubete-1. Aos 45 dias após a infestação das plântulas, procedeu-se a avaliação dos acessos, onde as raízes foram lavadas para a contagem do número de galhas por sistema radicular. Após a contagem das galhas, os ovos foram extraídos das raízes das plantas de melão pela técnica de Hussey & Barker (1973), modificada por Boneti & Ferraz (1981). Os ovos assim obtidos foram contados com auxílio de estereomicroscópio, obtendo-se o número de ovos por sistema radicular. O fator de reprodução: FR ≥ 1 indicará boa hospedeira, FR < 1,0 má hospedeira e FR = 0 não hospedeira com base na classificação proposta por Oostenbrink (1966). Todos os acessos testados apresentaram FR >1 mostraram-se bons hospedeiros para o M. enterolobii e M. javania.

Thesis (M. Sc. (Biochemistry)) -- University of Limpopo, 2021 / Plant-derived products have been used for years in the treatment of various ailments with low or no side effects. Thus, screening of medicinal plants for potential anticancer activity, in vitro, could help identify plant extracts or compounds that can be developed for use as anticancer agents with less or no side effects. The aim of this study was to investigate the probable anticancer effects and induced mechanism of action of Momordica balsamina crude leaf acetone extract in lung A549 cancer cells. The effect of the extract on cell viability, proliferation and cell division cycle were determined using Muse count & viability, Ki67 proliferation and cell cycle assay kits, respectively. The presence of biochemical and morphological features associated with apoptosis were analysed by Muse annexin-V & dead cell assay kit and Acridine orange/Ethidium bromide dual staining. The effect of the extract on the mRNA expression levels of cell cycle regulatory genes was determined using RT PCR. Proteome profiler antibody array was used to determine the effect of the extract on the protein expression levels of apoptosis regulatory genes. The findings revealed that the crude leaf acetone extract of M. balsamina decreased the percentage viability of lung A549 cells with less effect on the percentage viability of normal cells (KMST-6). Furthermore, a significant anti-proliferative effect in extract treated A549 cells was observed. Characteristic nuclear and morphological features of apoptosis such as chromatin and nuclear condensation, externalisation of phosphatidylserine and loss of cell membrane function were observed in A549 cells treated with the extract. Although there was no relative upregulation of Bax and Bad protein expression, a downregulation of the Bcl-xl and Bcl-2 protein expression was observed in extract-treated cells. This led to the release of Cytochrome c and HTRA2/Omi leading to pro-caspase-3 cleavage. Furthermore, presence of HTRA2/Omi in the cytosol inhibited the functions of IAPs such as XIAP and cIAP1/2. Phosphorylation of p53 at different serine residues led to upregulated protein expression levels of p27/Kip1 protein which resulted in the cell division cycle arrest at G0/G1-phase. Reverse transcriptase polymerase chain reaction results showed that the extract modulated mRNA expression levels of p53, p21, cyclin B and cdc2 genes. In summary, M. balsamina extract induced cell division cycle arrest and apoptosis in A549 cells through intrinsic apoptosis pathway via p53-mediated mechanism. / South African Medical Research Council (SAMRC)

Submitted by Automa??o e Estat?stica (sst@bczm.ufrn.br) on 2017-12-12T19:38:30Z No. of bitstreams: 1 ReginaCarmenEsposito_TESE.pdf: 1609404 bytes, checksum: bbff08f10f8b71c6162cfba459bc5243 (MD5) / Approved for entry into archive by Arlan Eloi Leite Silva (eloihistoriador@yahoo.com.br) on 2017-12-14T19:40:52Z (GMT) No. of bitstreams: 1 ReginaCarmenEsposito_TESE.pdf: 1609404 bytes, checksum: bbff08f10f8b71c6162cfba459bc5243 (MD5) / Made available in DSpace on 2017-12-14T19:40:52Z (GMT). No. of bitstreams: 1 ReginaCarmenEsposito_TESE.pdf: 1609404 bytes, checksum: bbff08f10f8b71c6162cfba459bc5243 (MD5) Previous issue date: 2017-09-29 / O aumento benigno da pr?stata, mais conhecido como hiperplasia benigna da pr?stata (HBP), leva a sintomas do trato urin?rio inferior (STUI), que contribuem para diminuir a qualidade de vida dos homens acima da quarta d?cada. O mesmo vem sendo tratado, na sua maioria, por medicamentos alop?ticos do grupo dos inibidores da 5-alfa-redutase e/ou alfa-bloqueadores e/ou fitoter?picos. A literatura cient?fica apresenta uma escassez de ensaios cl?nicos randomizados, controlados com cegamento sobre a efic?cia de medicamentos homeop?ticos que j? tenham mat?ria m?dica para esta doen?a, bem como de novos rem?dios homeop?ticos. O presente estudo visou a avaliar a efic?cia do produto homeop?tico, contendo Momordica charantia 12CH, no controle dos STUI, devido ? HBP em ensaio cl?nico, randomizado, duplo cego e placebo controlado. Foram aleatorizados 81 pacientes em grupo A - Placebo e grupo B - Momordica charantia 12CH e avaliados a cada consulta pela anamnese, com o Escore Internacional de Sintomas Prost?ticos (IPSS), pelos exames de imagem com mensura??o do Volume Prost?tico (PV) e do Volume de Urina Residual P?s-esvaziamento (PVR) e laboratoriais pelo Ant?geno Prost?tico Espec?fico (PSA), Prote?na C Reativa quantitativa (PCR) e Interleucina-6 (IL-6). Em 72 amostras, foram realizados imunofenotipagem de linf?citos e subpopula??es por citometria de fluxo. Tanto a vari?vel principal (IPSS) quanto as vari?veis secund?rias (PSA, PV, PVR e PCR) e acess?rias (IL-6, linf?citos totais, linf?citos B, linf?citos T, linf?citos T helper, linf?citos T citot?xico e rela??o CD4/CD8 e c?lulas Natural Killer) n?o apresentaram signific?ncia estat?stica nas m?dias entre os grupos tratado e Placebo. Quanto ?s vari?veis de seguran?a, o uso da medica??o homeop?tica, pelos pacientes, n?o trouxe interfer?ncia durante os seis meses do experimento, seja na taxa de glicemia de jejum, seja nas dosagens de alanina aminotransferase, aspartato aminotransferase, fosfatase alcalina, bilirrubinas totais e fra??es e creatinina, usadas para avalia??o hep?tica e da fun??o renal respectivamente. A aus?ncia de infec??o urin?ria, confirmada pelo sum?rio de urina dos pacientes, predominou em ambos os grupos A e B durante todo o per?odo do ensaio cl?nico. Pode-se concluir que o tratamento com a Momordica charantia 12CH n?o apresentou diferen?a significativa para o placebo, quanto ? efic?cia no controle dos STUI, por HBP, por?m mostrou-se seguro. Pesquisas de alta qualidade, que permitam a prescri??o, a partir da individualiza??o dos sintomas e com diferentes dinamiza??es, devem ser realizadas, para possibilitar uma interpreta??o mais decisiva. / The benign enlargement of the prostate, better known as benign prostatic hyperplasia (BPH) results in symptoms of the lower urinary tract (LUTS) that contributes to lower quality of life of men over the fourth decade, and is mostly treated by allopathic drugs of the group of 5-alpha-reductase inhibitors and / or alpha-blockers, and / or phytotherapics. The scientific literature shows lack research from randomised and doubleblind clinical trials on the efficacy of homeopathic medicinal products that already have homeopathic medical materia and new homeopathic medicinal for BPH.The present study aimed to evaluate the effectiveness of the homeopathic product containing Momordica charantia 12CH in the LUTS control caused by BPH in a clinical, randomized, double-blind and placebo-controlled trial.A total of 81 patients were randomized to group A - Placebo and group B - Momordica charantia 12CH and evaluated at each visit by anamnesis with the International Prostate Symptom Score (IPSS), by imaging tests measured prostate volume (PV) and post-void residual (PVR) and laboratory tests for prostate specific antigen (PSA), quantitative C-reactive protein (CRP) and interleukin-6 (IL-6), and in 72 samples, lymphocyte and subpopulation immunophenotyping were performed by flow cytometry.Both the main variable (IPSS) and the secondary variables (PSA, PV, PVR and CRP) and accessory variables (IL-6, total lymphocytes, B lymphocytes, T lymphocytes, T helper cells, cytotoxic T lymphocytes and CD4 / CD8 ratio and Natural Killer cells) did not present statistical significance in the means between the groups treated and Placebo.About the safety variables, the use of homeopathic medication by the patients did not interfere during the six months of research, either in the fasting glucose level, as well as in the dosages of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, total bilirubins and fractions and creatinine levels used for hepatic evaluation and renal function respectively.The absence of urinary infection confirmed by urinalysis of patients predominated in both groups A and B throughout the clinical trial period. It can be concluded that treatment with Momordica charantia 12CH did not show a significant difference for placebo in the efficacy in the control of STUI by BPH, but it demostrated to be safe. High quality researchs, which allows prescription, from the individualization of symptoms and with different dynamizations, must be performed, to enable more decisiveinterpretation of its effectiveness.