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1.
Chirality ; 36(4): e23660, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38511944

ABSTRACT

A green and efficient process for the synthesis of cenobamate has been accomplished in 70% yield and >99% ee through the bio-reduction of ß-ketotetrazole using Daucus carota whole plant cells. The corresponding ß-hydroxytetrazole was isolated in 60% yield and >98% ee. This is the first report on the biocatalytic reduction of ß-ketotetrazole using plant enzymes derived from D. carota root cells with excellent enantioselectivity.


Subject(s)
Anticonvulsants , Carbamates , Chlorophenols , Ketones , Tetrazoles , Stereoisomerism , Biocatalysis
2.
Drug Des Devel Ther ; 9: 3579-88, 2015.
Article in English | MEDLINE | ID: mdl-26203224

ABSTRACT

Wound healing represents a dynamic set of coordinated physiological processes observed in response to tissue injury. Several natural products are known to accelerate the process of wound healing. Tetrahydrocurcumin (THC), an in vivo biotransformed product/metabolite of curcumin, is known to exhibit a wide spectrum of biological activities similar to those of native curcuminoids. The poor bioavailability of these curcuminoids limits their clinical applications. The present study highlights the percutaneous absorption and wound healing activity of glucosyl-conjugated THC (glucosyl-THC) in male Wistar rats. A high plasma concentration of glucosyl-THC (4.35 µg/mL) was found in rats 3 hours after application. A significant enhanced wound healing activity and reduced epithelialization time were observed in rats that received glucosyl-THC. This may have been due to the improved bioavailability of the glucosyl compound. The nonstaining and lack of skin-sensitive side effects render the bioconjugated glucosyl-THC a promising therapeutic compound in the management of excision wounds and in cosmetic applications, in the near future.


Subject(s)
Curcumin/analogs & derivatives , Skin Absorption , Wound Healing/drug effects , Animals , Biological Availability , Curcumin/chemistry , Curcumin/pharmacokinetics , Curcumin/pharmacology , Glycosylation , Male , Rats , Rats, Wistar
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