255 research outputs found
Supplemental Material, Supplementary_Data_Pheophytins_Ficus - Metabolomics-Coupled Functional Pharmacology of Chlorophyll Compounds Isolated From the Leaves of <i>Ficus Exasperata</i> Vahl (Moraceae) Provides Novel Pathways on Myometrial Activity
Supplemental Material, Supplementary_Data_Pheophytins_Ficus for Metabolomics-Coupled Functional Pharmacology of Chlorophyll Compounds Isolated From the Leaves of
Ficus Exasperata
Vahl (Moraceae) Provides Novel Pathways on Myometrial Activity by Enitome E. Bafor, Edward G. Rowan, and RuAngelie Edrada-Ebel in Reproductive Sciences
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Winners of the 2024 Tu Youyou Award
Professor Tu Youyou is a renowned Chinese scientist whose pioneering work led to the discovery in the 1970s of the antimalarial sesquiterpene lactone, artemisinin (qinghaosu), from the sweet wormwood tree, Artemisia annua L [...
The 9th European conference on marine natural products
The 9th European Conference on Marine Natural Products (ECMNP) in Glasgow follows its predecessors in La Toja (2013), Tjärnö (2011), Porto (2009), Ischia (2007), Paris (2005), Elmau (2002), Santiago de Compostela (1999), and Athens (1997). [...]
P43 The isolation and purification of bioactive metabolites from Ficus carica and their neuroprotective effects in Alzheimer's disease
Neurodegenerative disease including Alzheimer’s disease (AD) is a major cause of long-term disability. Incidence of Alzheimer’s disease increases with age. According to a recent report by WHO, there are approximately 47.5 million people suffering from dementia, with 7.7 million new cases each year. Acrolein is one of the key contributing factors to accelerate oxidative stress which then implicated AD. However, protection against neuronal damage remains a great challenge for researchers. Ficus carica (commonly known as fig) is a species of great antioxidant nutritional value comprising a protective mechanism against innumerable health disorders related to oxidative stress as well as AD. The purpose of this work was to characterise the bioactive metabolites in Ficus carica mesocarp against oxidative stress related AD. Crude extracts were prepared using several extraction methods to achieve non-polar layer. The isolated metabolites were tested on their effect on human neuroblastoma SHSY5Y cell line by a cell viability test. Molecular weights of the active metabolites were determined via LC-HRESIMS, GC-EIMS, and multivariate analysis via SIMCA was performed. Structural elucidation and identification of the interested active metabolites were studied by 1-D and 2-D NMR. NMR profiling demonstrated that aliphatic compounds such as γ-sitosterol were found to induce neuronal bioactivity
The metabolite products of chlorocholine chloride (CCC) in eggs and meat of laying hens fed 15N-CCC containing diets
An experiment was conducted to evaluate the metabolic products of chlorocholine chloride (CCC) in eggs and meat of laying hens fed a diet containing (15)N-CCC. Ten brown laying hens were randomly divided into two groups of five each. One group was offered (15)N-CCC free diet while the other group received a diet with 100 ppm (15)N-CCC for 11 days. Samples of eggs and meat from the laying hens were collected. Egg yolks and albumen were separated. Meat was collected from the breast and femur. The metabolic products of CCC were measured using ion trap electrospray ionisation mass spectrometry (ion trap-ESI-MS/MS). Determination of CCC or its metabolites in eggs and meat showed that CCC was metabolised to choline. Corresponding MS/MS spectra were obtained for m/z 104 (choline) or 105 ((15)N-choline), whereas nothing was detected at m/z 122 (CCC) or 123 ((15)N-CCC). The results from this study indicate that CCC will be metabolised in tissues of laying hens
Metabolomics identifies the building blocks of pharmacologically active metabolites in marine invertebrates and its microbial symbionts
Marine invertebrates harbour microorganisms that include bacteria, cyanobacteria and fungi within their tissues and in some cases these associated microorganisms may constitute up to 40% of their biomass. A number of pharmacologically active sponge natural products have been found to be structurally related to microbial metabolites. One example is ecteinascidin (ET-743) which was first isolated from the tunicate Ecteinascidia turbinata. The structure of ET-743 reveals striking similarities to safracin B, a metabolite of Pseudomonas fluorescens. ET-743 is commercially available as Yondelis® or under the generic name trabectedin and is used for the treatment of undifferentiated uterine sarcoma in women. To date, Yondelis® is made feasibly available through biotechnological methods and partial synthesis. Renieramycin is an analogue of ET-743 which was obtained from sponges Reniera and Xestospongia. Building blocks have also been isolated from these sponge genera. Sponges become fermenter vessels for the microorganism to produce these interesting metabolites. Through tools of metabolomics and genomics, the production of other novel drugs can be optimised to solve and come up with a sustainable solution to address the supply problem. Recently, we have applied metabolomics to screen for potential new antibiotics from sponge-derived microorganisms collected from under-investigated and under-exploited marine habitats of a geographic distance of more than 10,000 km coastline of Scotland
Screening for novel anti-trypanosomal drugs through metabolomic tools
There is a drastic need for new and improved anti-trypanosomal drugs to be developed due to the alarming rate of resurgence of trypanosomiasis, development of drug resistance, lack of efficacy of chemotherapy, drug-related adverse effects and drawbacks of the existing useful drugs. A novel, affordable, safe, and efficacious anti-trypanosomal drug should be to able combat the almost neglected yet life-threatening trypanosomiasis. We have established metabolomic methods to screen diverse biological sources of potentially novel and sustainable sources of antitrypanosomal drugs. Metabolomic profiling was done on organic extracts of diverse natural sources by using high resolution LCFTMS and NMR. The secondary metabolite profiles of anti-trypanosomal acitve extracts were then compared to those of the inactive samples with the aid of SIEVE and MZmine, both are automated label-free differential expression softwares. Together with high resolution NMR, principal component analysis and off-line databases were utilised to identify resonances that quantifies and confirms the presence of the secondary metabolite of interest. Preliminary highthroughput chromatographic separation of the active secondary metabolites was achieved on the active extracts exhibiting an interesting chemical profile. From African propolis we have identified active extracts to contain new highly oxygenated phloroglucinol derivatives. Tools of metabolomics were also applied to biotechnologically optimize the production of bioactive secondary metabolites in marine-derived fungi and endophytes. At small scales, efficient cultivation processes are developed to later scale-up to a fermenter system. Through tools of metabolomics and genomics, the production of other potential novel drugs can be optimised to solve and come up with a sustainable solution to address the supply problem. A novel anti-trypanosomal active macrolide lactone from a Streptomyces spp. was derived from the sponge Haliclona collected from the Irish Sea. Metabolomic studies through SIEVE showed that amino acid catabolism is an important source of building blocks for macrolide formation. Amino acid utilization is regulated through the process, which indirectly regulates macrolide biosynthesis
Analgesics
Analgesic drugs act in various ways on the peripheral and central nervous systems; they include paracetamol (para-acetylaminophenol, also known in the US as acetaminophen), the non-steroidal anti-inflammatory drugs (NSAIDs) such as the salicylates, and opioid drugs such as morphine and opium. They are distinct from anesthetics, which reversibly eliminate sensation
Metabolomics of plant endophytes and marine microbial symbionts
Metabolomic methods can also be utilised to screen diverse biological sources of potentially novel and sustainable sources of antibiotics and pharmacological-active drugs. Dereplication studies by LC-HRFTMS and NMR can establish the chemical profile of endophytic and/or endozoic microbial extracts and their plant or animal sources. Identifying the compounds of interest at an early stage will aid in the isolation of the bioactive components. Therefore metabolite profiling is important for functional genomics and in the search for new pharmacologically active compounds. Using the tools of metabolomics through the employment of LC-HRFTMS as well as high resolution NMR will be a very efficient approach. Metabolomic profiling has found its application in screening extracts of macroorganisms as well as in the isolation and cultivation of suspected microbial producers of bioactive natural products. Metabolomics is being applied to identify and biotechnologically optimize the production of pharmacologically active secondary metabolites. The links between metabolome evolution during optimisation and processing factors can be identified through metabolomics. Information obtained from a metabolomics data can efficiently establish cultivation and production processes at a small scale which will be finally scaled up to a fermenter system, whilst maintaining or enhancing synthesis of the desired compounds. MZmine and SIEVE softwares are utilized to perform differential analysis of sample populations to find significant expressed features of complex biomarkers between parameter variables. Metabolomes are identified with the aid of existing high resolution MS and NMR records from online or inhouse databases like AntiMarin, a database of microbial secondary metabolites and marine natural products. This is further validated through available reference standards and NMR experiments. Metabolomics has become a powerful tool in systems biology which allows us to gain insights into the potential of natural marine isolates for synthesis of significant quantities of promising new agents, and allows us to manipulate the environment within fermentation systems in a rational manner to select a desired metabolome
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