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I1 Sponging off nature for new drug leads
Biochemical Pharmacology 139 (2017) 105–110
Contents lists available at ScienceDirect
Biochemical Pharmacology journal homepage: www.elsevier.com/locate/biochempharm
ICMAN-IUPHAR Abstracts - Invited Speakers
Theme 1: Novel sources of nutraceuticals and natural products I1 Sponging off nature for new drug leads Raymond Andersen University of British Columbia, Vancouver, Canada The secondary metabolites found in marine organisms represent an extremely rich source of novel chemical diversity for academic drug discovery and chemical biology programs. Among the marine invertebrates, marine sponges have historically been one of the most prolific sources of new natural products. Our group at UBC has amassed a sizable library of crude extracts from marine sponges, other marine invertebrates, and cultured marine microorganisms collected in many of the world’s oceans. In collaboration with biologists, this crude extract library has been screened for activity in cell-based and pure enzyme assays designed to identify promising marine natural product lead compounds for the development of drugs. Bioassay-guided fractionation of crude extracts and extensive spectroscopic analysis has been used to identify the structures of pure natural products active in the assays. Biology-oriented chemical synthesis has been undertaken to probe the SAR for new natural product pharmacophores that we have discovered and to provide material for in vivo testing in animal models. Several new drug candidates for the treatment of cancer, inflammation, cystic fibrosis, and infectious diseases have emerged from this research program. Three of them have progressed to phase II/III clinical trials in humans and others are in preclinical evaluation/development. The lecture will present some highlights from our academic ‘Drugs from the Sea’ and chemical biology research.
available applications inspired the scientific community to intensify its efforts for the valorization of all kind of food by-products for recovery purposes. Nowadays, many relevant projects progress around the world and across different disciplines, whereas the existence of numerous scientific articles, patents, congresses and commercialization efforts have emerged a wealth of literature in the field. However, despite this plethora of information and the developed technologies that promise the recovery, recycling and sustainability of valuable compounds inside the food chain, the respective shelf products remain rather limited. This is happening because the industrial implementation of recovery processes meets several implementation problems that require careful consideration of different aspects. For instance, a commercially feasible product can be manufactured only if a certain degree of flexibility and alternative choices can be adapted in the developing methodology. The current presentation highlights the most important assets that cause stifling of innovation in the field. Finally, solutions are provided in order to help progress and reveal relevant innovations with an ultimate goal to fulfil market and consumers’ needs. doi:10.1016/j.bcp.2017.06.050
Theme 2: Bioavailability/pharmacokinetics of nutraceuticals and natural product pharmaceuticals I4 Factors affecting bioavailability of plant polyphenols Junji Terao Faculty of Nursing and Rehabilitation, Konan Women’s University, Kobe City, Japan
doi:10.1016/j.bcp.2017.06.049
I2 Nutraceuticals retrieved from food processing waste Charis M. Galanakis Food Waste Recovery Group, ISEKI Food Association, Vienna, Austria The prospect of recovering high added-value compounds from the non-consumed materials of food processing is a story started a few decades ago. The first successful efforts dealt with the recovery of oil from olive kernel, the production of essential oils, flavonoids, sugars and pectin from citrus peel, as well as the recapture of protein concentrates and lactose from cheese whey. These commercially
Nowadays plant polyphenols attract much attention in the prevention of chronic diseases. Epidemiological and intervention studies strongly suggest that polyphenol intake has beneficial effects on vascular health. It is unlikely that polyphenols act as direct antioxidants, although oxidative stress profoundly contributes to vascular impairment leading to cardiovascular diseases. Polyphenols, in particular, low-molecular weight flavonoids may exert their function by tuning the cellular redox state to an adaptive response or tolerable stress. However, the optimum intake of flavonoids from supplements or diet has not been clarified yet, because a number of exogenous and endogenous factors modulating their bioavailability affect their vascular function. This lecture will focus on the current knowledge of the bioavailability and its consequence on vascular function of an antioxidative flavonoid quercetin. Current
Contents lists available at ScienceDirect
Biochemical Pharmacology journal homepage: www.elsevier.com/locate/biochempharm
ICMAN-IUPHAR Abstracts - Invited Speakers
Theme 1: Novel sources of nutraceuticals and natural products I1 Sponging off nature for new drug leads Raymond Andersen University of British Columbia, Vancouver, Canada The secondary metabolites found in marine organisms represent an extremely rich source of novel chemical diversity for academic drug discovery and chemical biology programs. Among the marine invertebrates, marine sponges have historically been one of the most prolific sources of new natural products. Our group at UBC has amassed a sizable library of crude extracts from marine sponges, other marine invertebrates, and cultured marine microorganisms collected in many of the world’s oceans. In collaboration with biologists, this crude extract library has been screened for activity in cell-based and pure enzyme assays designed to identify promising marine natural product lead compounds for the development of drugs. Bioassay-guided fractionation of crude extracts and extensive spectroscopic analysis has been used to identify the structures of pure natural products active in the assays. Biology-oriented chemical synthesis has been undertaken to probe the SAR for new natural product pharmacophores that we have discovered and to provide material for in vivo testing in animal models. Several new drug candidates for the treatment of cancer, inflammation, cystic fibrosis, and infectious diseases have emerged from this research program. Three of them have progressed to phase II/III clinical trials in humans and others are in preclinical evaluation/development. The lecture will present some highlights from our academic ‘Drugs from the Sea’ and chemical biology research.
available applications inspired the scientific community to intensify its efforts for the valorization of all kind of food by-products for recovery purposes. Nowadays, many relevant projects progress around the world and across different disciplines, whereas the existence of numerous scientific articles, patents, congresses and commercialization efforts have emerged a wealth of literature in the field. However, despite this plethora of information and the developed technologies that promise the recovery, recycling and sustainability of valuable compounds inside the food chain, the respective shelf products remain rather limited. This is happening because the industrial implementation of recovery processes meets several implementation problems that require careful consideration of different aspects. For instance, a commercially feasible product can be manufactured only if a certain degree of flexibility and alternative choices can be adapted in the developing methodology. The current presentation highlights the most important assets that cause stifling of innovation in the field. Finally, solutions are provided in order to help progress and reveal relevant innovations with an ultimate goal to fulfil market and consumers’ needs. doi:10.1016/j.bcp.2017.06.050
Theme 2: Bioavailability/pharmacokinetics of nutraceuticals and natural product pharmaceuticals I4 Factors affecting bioavailability of plant polyphenols Junji Terao Faculty of Nursing and Rehabilitation, Konan Women’s University, Kobe City, Japan
doi:10.1016/j.bcp.2017.06.049
I2 Nutraceuticals retrieved from food processing waste Charis M. Galanakis Food Waste Recovery Group, ISEKI Food Association, Vienna, Austria The prospect of recovering high added-value compounds from the non-consumed materials of food processing is a story started a few decades ago. The first successful efforts dealt with the recovery of oil from olive kernel, the production of essential oils, flavonoids, sugars and pectin from citrus peel, as well as the recapture of protein concentrates and lactose from cheese whey. These commercially
Nowadays plant polyphenols attract much attention in the prevention of chronic diseases. Epidemiological and intervention studies strongly suggest that polyphenol intake has beneficial effects on vascular health. It is unlikely that polyphenols act as direct antioxidants, although oxidative stress profoundly contributes to vascular impairment leading to cardiovascular diseases. Polyphenols, in particular, low-molecular weight flavonoids may exert their function by tuning the cellular redox state to an adaptive response or tolerable stress. However, the optimum intake of flavonoids from supplements or diet has not been clarified yet, because a number of exogenous and endogenous factors modulating their bioavailability affect their vascular function. This lecture will focus on the current knowledge of the bioavailability and its consequence on vascular function of an antioxidative flavonoid quercetin. Current