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Enzyme Kinetics and Drugs as Enzyme Inhibitors
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
These drugs comprise statins, fibrates, niacin, Ezetimibe, and bile acid sequestrants as well as phytosterols and (n − 3) long-chain polyunsaturated fatty acids that can reduce circulating triglycerides and raise HDL-cholesterol (Micallef and Garg, 2008), and Orlistat (Tetrahydrolipstatin) that is derived from Lipstatin (its biosynthesis has been reported by Bai et al., 2014), isolated from Streptomyces toxytricini and acting as a potent and selective inhibitor of human pancreatic lipase. Orlistat is used as drug to treat obesity; as a consequence of inhibiting lipase activity, triglycerides from the diet are not hydrolyzed and therefore excreted unchanged. Phytosterols, omega-3 fatty acids, and Orlistat are not treated here in more detail.
Diabetes and Antidiabetic Therapy: Control of Glucose
Published in Richard J. Sundberg, The Chemical Century, 2017
Orlistat is an inhibitor of pancreatic lipase. It is produced by hydrogenation of lipstatin, which is produced by the bacterium, Streptomyces toxytricini.10 It has been shown to promote weight loss, delay the progression to type-2 diabetes and reduce cardiovascular events in obese patients.
Genotoxic effects of caffeine in female mice exposed during pregnancy and lactation period and their offspring
Published in Journal of Environmental Science and Health, Part C, 2023
Marina Lummertz Magenis, Pamela Souza de Marcos, Adriani Paganini Damiani, Anderson Ricardo Cantareli da Silva, Luiza Martins Longaretti, Ive Bahia Franca, Juliana Da Silva, Carina Rodrigues Boeck, Vanessa Moraes de Andrade
The genotoxic effects of caffeine on DNA, both in vitro and in vivo, are conflicting, and there is evidence suggesting that its effects on DNA might be dose-dependent.5–8 Long-term administration of caffeine in mice had adverse effects on the functions of their dopaminergic and serotonergic neurons.5 Noschang et al.8 observed an increase in DNA damage after caffeine treatment in mice. Alternatively, another study showed a reduction in DNA damage in the neural tissue and peripheral blood of aged mice treated with caffeine.6 Similarly, in an in vitro study, caffeine reduced the genotoxicity induced by orlistat (drug indicated for the treatment of obesity).7 Despite several studies on caffeine, only a few have attempted to assess its effects on offspring.