Single dose oral pharmacokinetic profile rubraxanthone in mice

Pharmacokinetic Profile of Tetraprenyltoluquinone After Single-Dose Oral Administration in Male Mice

“…TPTQ was shown to have rapidly absorption in the gastrointestinal tract with the absorption half-life parameter at 0.48±0.05 h and absorption rate constant (ka) of 1.448±0.17 h -1 . The value of ka describes the amount of drug that moves from the drug absorbed to the extravascular administration expressed per unit time [14] Viewed from its structure, TPTQ has a weak acid tructure characterized by the presence of a phenolic group, where absorption occurs through a passive diffusion mechanism in epithelial cells [9]. Drugs that are weakly acidic (pKa 3-7.5) in acidic stomach will be distributed in non-ionized form, so they are easily soluble in fat and easily penetrate the gastric membrane [16].…”

“…The elimination half-life of the TPTQ compound was at 12.131±0.55 h and it takes four to five half-lives for the drug to be eliminated by 94-97% [22]. It is suspected that this is related to its lipophilic structure which allows TPTQ to be distributed to tissues outside the plasma; this causes its elimination rate to be slow, namely 0.057±0.0 h -1 [9].…”

“…However, until now there has been no report regarding the pharmacokinetics of TPTQ in animals. Pharmacokinetic study plays a crucial role in the early stage of the development of new drugs in choosing the best dosing regimen and route of administration [9]. Despite of its promising in vitro studies, a lot of natural compounds have failed during preclinical trails due to poor pharmacokinetic properties, such as low bioavailability, low metabolic stability, and lack of pharmacodynamic reproducibility [10] In most cases, drug compounds have small amounts in the blood.…”

Innovation of 6-sulfonamide-2H-chromene derivatives as antidiabetic agents targeting α-amylase, α-glycosidase, and PPAR-γ inhibitors with in silico molecular docking simulation

“…24 Besides, umbelliferone (7-hydroxycoumarin) is used to reduce blood glucose levels. 25,26 H. Sun et al, synthesized new coumarin-avonoid hybrids, as compound I that displayed glucosidase inhibitory activity with IC 50 value of 1.47 ± 0.07 mM (Acarbose = 224.70 ± 14.14) and amylase with IC 50 value of 6.89 ± 1.17 mM (Acarbose = 2.72 ± 0.30 mM). 27 Furthermore, the scientic community's interest became more attractive to the sulfonamide (-SO 2 NH 2 ) core due to the wide variety of biological activity, such as anti-HIV, antimalarial, antithyroid, anticancer, high ceiling diuretic, insulinreleasing antidiabetic, carbonic anhydrase activity, and antimicrobial activity.…”

“…24 Besides, umbelliferone (7-hydroxycoumarin) is used to reduce blood glucose levels. 25,26 H. Sun et al , synthesized new coumarin–flavonoid hybrids, as compound I that displayed glucosidase inhibitory activity with IC 50 value of 1.47 ± 0.07 μM (Acarbose = 224.70 ± 14.14) and amylase with IC 50 value of 6.89 ± 1.17 μM (Acarbose = 2.72 ± 0.30 μM). 27 Asgari et al , developed a new bis-coumarin derivatives conjugated with 1,2,3-triazole nucleus to exhibit IC 50 values of compound II (IC 50 = 13.0 ± 1.5 μM) and compound III (IC 50 = 16.4 ± 1.7 μM) against α-glucosidase inhibitory activity.…”