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.
β‐caryophyllene (BCP), a natural sesquiterpene present in plants, is a selective agonist of cannabinoid receptor type‐2 (CB2) of the endocannabinoid system. In this study, we have prepared an extract from Piper nigrum (black pepper) seeds using supercritical fluid extraction, standardized to contain 30% BCP (ViphyllinTM). The beneficial effects of prophylactic treatment with Viphyllin on cognitive functions were demonstrated in Scopolamine‐induced dementia model mice. Male Swiss albino mice (25–30 g) were administered with Viphyllin (50 mg and 100 mg/kg body weight p.o.) or donepezil (1.60 mg/kg) for 14 days. Subsequently, cognitive deficits were induced by treating the animals intraperitoneally with Scopolamine (0.75 mg/kg). The cognitive behavior of mice was evaluated using a novel object recognition test (NORT) and Morris water maze (MWM) test. The brain homogenates were studied for biochemical parameters including cholinesterase activities and antioxidant status. Western blot analysis was performed to investigate the mechanism of action. Viphyllin dose dependently improved the recognition and spatial memory and cholinergic functions in Scop‐treated mice. The extract was found protective against Scop‐induced oxidative damage and histopathologic changes in the brain. At 100 mg/kg Viphyllin markedly reduced the proBDNF/mBDNF ratio (p < .05) and augmented the TrkB expression (p < .01). Viphyllin (100 mg/kg) was found to be neuroprotective by reducing the Scop‐induced upregulation of p‐JNK and p‐p38 MAPK proteins, Bax/Bcl‐2 ratio, and caspase activation in the brain. Viphyllin also exerted anti‐inflammatory effects by downregulating Cox‐2, TNF‐α, and NOS‐2 in Scop‐induced mice (p < .05). To summarize, our data encourage Viphyllin as a functional ingredient/dietary supplement for brain health and cognition.
Practical applications
Black pepper is a culinary spice having several medicinal attributes. Essential oils in the seeds of the plant give aroma and flavor to it. Here we have prepared an extract from the seeds of black pepper using supercritical fluid extraction, characterized for the presence of β‐caryophyllene (not <30%). This research work further validates the neuroprotective mechanism of the extract in Scopolamine‐induced cognitive impairment model mice. The findings from this study strongly suggest the beneficial neuroactive properties of black pepper seed extract having the presence of BCP, a CB2 receptor agonist. It can thus be used potentially as a functional food ingredient for cognition and brain function.
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