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Emerging Highlights on Natural Prodrug Molecules with Multifarious Therapeutic Perspectives
Published in Debarshi Kar Mahapatra, Cristóbal Noé Aguilar, A. K. Haghi, Applied Pharmaceutical Practice and Nutraceuticals, 2021
Mojabir Hussen Ansari, Vaibhav Shende, Debarshi Kar Mahapatra
Butyrin (tributyrin), the prodrug of butyric acid, is an essential triglyceride molecule that is naturally present in the butter and also in some butter products. It is a fatty liquid with acrid flavor and is specifically made up of ester of butyric acid and glycerol. Butyrate is also a product achieved by the fermentation process that took place mainly in the distal colon by the microorganism.9 Butyric acid and its derivatives possess notable antimicrobial activities at different concentrations against Salmonella typhimurium and Clostridium perfringens. Butyric acid, when administered alone as a therapeutic agent often shows compromised pharmacological activity (particularly, short half-life) as a result of rapid metabolism.10 In addition to it, the strong odor of butyrate hinders patient compliance; therefore, direct oral consumption of butyric acid is unacceptable. Although in a study, it was found that the best antimicrobial inhibition was reported by butyric acid and its derivative without the addition of lipase.11 Although focusing on veterinarian applications, recently, it has been discovered that the glycerides and individual administration of butyrin in broiler chickens feed concurrently extends the carcass weight and breast meat. Butyrate improves the epithelization process and brings about collagen lysis by reducing the matrix metalloproteinase release.12
Gastric Lipase
Published in Margit Hamosh, Lingual and Gastric Lipases: Their Role in Fat Digestion, 2020
A second study on species differences of the origin of preduodenal lipases confirmed and expanded20 our initial observation.19, 55 Thus, horse, pig, and macaque were shown to have predominantly gastric lipase, while, as in our studies, rat and mouse were found to have mainly (or only) lingual lipase. In this study, Moreau et al. have used tributyrin as substrate; therefore, a comparison to rates of hydrolysis of long-chain triglycerides was not presented. The lipase activities reported in this study are lower than in the study of DeNigris et al.,19 however, a direct comparison is difficult because of the differences in lipase quantitation techniques.
Production, purification and biochemical characterisation of a novel lipase from a newly identified lipolytic bacterium Staphylococcus caprae NCU S6
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Junxin Zhao, Maomao Ma, Zheling Zeng, Ping Yu, Deming Gong, Shuguang Deng
The SCNL can hydrolyse p-NP esters with different acyl chain length (Table 5), with the highest specific activity of 616.54 U/mg towards pNPS (18 carbons). The p-NP esters from C2 to C16 were hydrolysed moderately (45.46–54.54%) by SCNL apart from pNPB (4 carbons), indicating its preference for C4 with a higher specific activity of 479.91 U/mg. The lipase was similar to the lipases from M. cinnamomea36 and B. licheniformis DSM 1236924, possessed a strong hydrolysis efficiency for medium and long carbon chain length substrates, and had mild specificity towards short-chain p-NP esters. Among the triglycerides, SCNL showed a preference for short-chain and medium-chain fatty acids from C2 to C12, with the maximum activity (196.00 U/mg) in tributyrin (C4). The results indicated a lower hydrolytic activity of the enzyme for triglycerides with more than twelve carbons atoms (C14–C18), and that SCNL was a novel lipase different from esterases that only hydrolyse short-chain fatty acids.
Decrease in acetyl-CoA pathway utilizing butyrate-producing bacteria is a key pathogenic feature of alcohol-induced functional gut microbial dysbiosis and development of liver disease in mice
Published in Gut Microbes, 2021
Richa Singhal, Hridgandh Donde, Smita Ghare, Kendall Stocke, Jingwein Zhang, Manicka Vadhanam, Sreelatha Reddy, Leila Gobejishvili, Paula Chilton, Swati Joshi-Barve, Wenke Feng, Craig McClain, Kristi Hoffman, Joseph Petrosino, Marius Vital, Shirish Barve
An important function of the gut microbiome is the fermentation of indigestible dietary fibers leading to the production of short-chain fatty acids (SCFAs).7 Among the SCFAs produced by the gut microbiome, butyrate has been demonstrated to confer multiple health benefits to the host.7 Hence, depending on the type and extent of microbial dysbiosis, normal production of butyrate and consequent health benefits could be negatively impacted. With regard to the effects of alcohol on the gut microbiome and the development of liver disease, studies have demonstrated that i) chronic exposure to ethanol leads to a decrease in intestinal butyrate levels8,9 and ii) administration of tributyrin (Tb) – a butyrate prodrug significantly attenuates ethanol mediated intestinal barrier dysfunction and hepatic steatosis and injury.10–12 These findings clearly indicate that alcohol-induced gut dysbiosis likely affects the butyrate-producing microbial communities. Therefore, the major goal of the present study was to elucidate the effects of chronic ethanol consumption on butyrate synthesizing microbial communities and the associated butyrate synthesizing pathways.
The human gut microbiome – a new and exciting avenue in cardiovascular drug discovery
Published in Expert Opinion on Drug Discovery, 2019
Yu Du, Xingxing Li, Chunyan Su, Li Wang, Jiandong Jiang, Bin Hong
Butyrate, one of the SCFAs, is also known as a histone deacetylases inhibitor. Sodium butyrate has been administrated in animals with multiple metabolic benefits, including reduced HFD-induced obesity, greater insulin sensitivity and decreased hepatic steatosis [125]. Tributyrin, a triglyceride containing three butyrate moieties esterified to glycerol, has been designed to overcome the unpleasant taste and odor of butyrate. Tributyrin may be used as a prodrug of butyrate with similar metabolic effects and more favorable pharmacokinetic properties [126]. Tributyrin attenuated the obesity-associated inflammation and insulin-resistance in HFD-fed C57BL/6 male mice. Cresci et al. reported that pretreatment of mice with tributyrin ameliorated acute alcohol-induced liver damage by protecting against the loss of tight junction protein [127]. A recent study confirmed tributyrin administration significantly inhibited the development of atherosclerosis, lipid deposition and macrophage accumulation in the plaque of gnotobiotic ApoE−/- mice, indicating a promising strategy for CVD prevention [40].