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Nanostructures for Improving the Oral Bioavailability of Herbal Medicines
Published in Bhaskar Mazumder, Subhabrata Ray, Paulami Pal, Yashwant Pathak, Nanotechnology, 2019
Polymeric micelles have often been applied to enhance the solubility and, hence, the bioavailability of orally administered drugs, including phytochemicals. The polymeric micelles composed of pluronic P123 and solutol HS15 were prepared by the thin film dispersion method and loaded with naringenin, a poorly soluble drug (Zhai et al., 2013). Sustained release of naringenin for 36 hours was achieved and the cytotoxicity of the drug-loaded polymeric micelle against cancer cell lines was also significantly enhanced when compared to the free naringenin. The bioavailability of paclitaxel entrapped in glycyrrhizic acid micelles following oral administration was also reported to be six times higher than that of taxol (Yang et al., 2015). There was also a report of 6-fold increments in the antiproliferative activity of curcumin against colorectal cancer cells when compared to those cells treated with a solution containing an equivalent concentration of free curcumin (Wang et al., 2012).
Indoor Air Pollution
Published in William J. Rea, Kalpana D. Patel, Reversibility of Chronic Disease and Hypersensitivity, Volume 4, 2017
William J. Rea, Kalpana D. Patel
Since it is clear from this study and interpretation of earlier studies of Aldridge with rat liver slices78 that the P450 system is required for the conversion of TAPs into toxic metabolites, Baker et al. investigated whether naturally occurring inhibitors would block the conversion of TAPs to toxic metabolites. Naringenin, a compound found in grapefruit, inhibited the conversion of D125 into BChE inhibitor(s) in a concentration-dependent manner. The inhibition was observed at concentrations that fall well below the reported ∼6 μM concentration of naringenin observed in plasma following ingestion of grapefruit juice.182 Lu et al.164 recently described the naringenin enantiomer-dependent inhibition of cytochromes CYP19, CYP2C9, CYP2C19, and CYP3A by the (R)- and (S)-enantiomers of naringenin. Additional research will be required to determine which of the P450 isomers are involved in the bioactivation of each of the TAPs and which naringenin enantiomer is the most potent inhibitor of the bioactivation of a specific TAP by a relevant P450 isozyme. While consumption of grapefruit juice following an exposure may block the conversion of TAP to toxic inhibitor, an important caveat comes from the observation that the microsomal/NADPH system is also involved in the inactivation of active metabolite(s) (data not shown). Aldridge78 had observed in his earlier studies that incubation of ToCP with liver slices for extended periods of time decreased toxicity following bioactivation.
Compounds of Plant Origin as AMP-Activated Protein Kinase Activators
Published in Alexander V. Kutchin, Lyudmila N. Shishkina, Larissa I. Weisfeld, Gennady E. Zaikov, Ilya N. Kurochkin, Alexander N. Goloshchapov, Chemistry and Technology of Plant Substances, 2017
Daria S. Novikova, Gleb S. Ivanov, Alexander V. Garabadzhiu, Viacheslav G. Tribulovich
Naringenin (Fig. 9.13) is a flavonoid found in citrus fruit, especially in grapefruit, and also tomatoes. It has been reported to possess antioxidant, anticancer, and antiatherogenic properties, as well as effects on lipid metabolism and plasma glucose levels. It showed an insulin-like effect in studies in vitro. Naringenin does not have a significant effect on glucose transport in myoblasts suggesting that naringenin affects GLUT4 translocation or activity. It was shown that the mechanism of naringenin action involves the activation of AMPK and is similar to that of resveratrol [83]. It was hypothesized that antidiabetic and antiobesity effects of naringenin in vivo reported recently may be mediated by AMPK [84].
Anti-glycation effect and the α-amylase, lipase, and α-glycosidase inhibition properties of a polyphenolic fraction derived from citrus wastes
Published in Preparative Biochemistry & Biotechnology, 2020
Annayara C. F. Fernandes, Ádina L. Santana, Isabela M. Martins, Debora K. T. Moreira, Juliana A. Macedo, Gabriela A. Macedo
The agroindustrial wastes of citrus have been considered a low cost and feasible source of flavonoids, a class of polyphenols associated with strong antioxidant activity. The flavonoids detected in the extracts of citrus wastes are composed of naringin, hesperidin, naringenin, and hesperitin.[14,15]