In vitro gastrointestinal digestion of a bisdemethoxycurcumin-rich Curcuma longa extract and its oral bioavailability in rats

Abstract

Background Nonetheless curcumin has potential health benefits, its low bioavailability limits the application of conventional turmeric extract with curcumin as major curcuminoid. This is a comparative study to assess the stability, bioaccessibility and biological activity of BDMC in standardized C. longa extract (REVERC3) relative to curcumin in regular turmeric extract (RTE). Here we report the preparation of a standardized Curcuma longa extract (REVERC3™) standardized to contain 75 ± 5 w/w % bisdemethoxycurcumin (BDMC), 1.2 ± 0.8 w/w % curcumin and 10 ± 5 w/w % demethoxycurcumin (DMC). The turmeric extracts were subjected to in vitro gastrointestinal digestion and the curcuminoids in undigested and digested samples were analyzed using HPLC to determine the bioaccessibility. Further, the undigested and digested samples were evaluated for lipase inhibition and antioxidant activities. Male Wistar rats were administered with single dose (1000 mg/kg) of standardized C. longa extract and RTE to determine the plasma concentration of BDMC and curcumin respectively at different time points using LCMS/MS. Results The bioaccessibility of BDMC was significantly higher than curcumin (p < 0.05). BDMC was found superior to curcumin having significant lipase inhibitory effect (p < 0.01), ABTS radical scavenging (p < 0.05), and nitric oxide scavenging activities (p < 0.01). Interestingly, the relative bioavailability of BDMC in standardized C. longa extract was 18.76 compared to curcumin. The Cmax of BDMC was 4.4-fold higher than curcumin. Conclusion BDMC is reported to have higher bioaccessibility and bioavailability than curcumin. Our findings rationalize use of BDMC-enriched standardized C. longa extract for improved physiological benefits counteracting the regular turmeric extract with less bioavailable curcumin as major curcuminoid.

Bisdemethoxycurcumin-mediated Attenuation of Apoptosis Prevents Gentamicin-induced Ototoxicity in Mouse Cochlear UB/OC-2 Cells

“…These disadvantages are overcome by BDMC, which differs from DMC and curcumin by lack of o-methoxy groups on its phenolic rings. Sudeep et al examined the gastrointestinal digestion of BDMC and curcumin in male rats and reported significantly higher bioavailability of BDMC, with a 4.4-fold higher plasma concentration than that of curcumin (18). Moreover, the antioxidant capacity of BDMC was superior to that of curcumin at the same concentration (18).…”

“…Generally, lipid-soluble, small, and non-polar molecules tend to pass through the round window membrane more readily (25). BDMC is the most stable in non-polar solvents of the curcuminoids (18).…”

“…To the best of our knowledge, there are no reports on BDMC, one of the rarest compounds in nature, in relation to AG-induced ototoxicity. As BDMC is safe with a highly stable structure and good bioavailability among curcuminoids, it might be a potential candidate worth of in-depth research (18).…”

Phenolic Derivatives with Anti‐Acetylcholinesterase Inhibitory Activities from Galeola nudifolia in Vietnam

“…[11] However, these medications do not possess disease-modifying properties. [8,9] Furthermore, undesirable side effects have also been observed in treatments using these medications. [8,9] Therefore, searches for new natural AChE inhibitors from natural resources as potent drug seeds are still conducted, and several natural compounds with AChE inhibitory activity have been reported, including huperzine, [12] a possible treatment agent for AD, as well as tomatine, [13] berberine, [14] palmatine, and jatrorrhizine.…”

Design of Hybrid Polymeric-Lipid Nanoparticles Using Curcumin as a Model: Preparation, Characterization, and In Vitro Evaluation of Demethoxycurcumin and Bisdemethoxycurcumin-Loaded Nanoparticles

“…Indeed, there are reports studying the anti-inflammatory and anticancer properties of DMC and BDM [ 31 , 32 ]. In turn, evidence indicates DMC and BDM possess the same drawbacks compromising CUR’s bioavailability [ 33 , 34 ]. Hence, these two curcuminoids are promising molecules for the improvement of their limited bioavailability through PLHNs.…”