Reactive oxygen species (ROS)-induced oxidative stress is reportedly associated with progressive neuronal cell damage. Glechoma hederacea L. (Lamiaceae), belonging to the Labiatae family, has demonstrated several biologic activities including depigmentation, antimelanogenic, antitumor, antioxidative, hepatoprotective, and antiinflammatory activities. Previously, we reported that rosmarinic acid, chlorogenic acid, caffeic acid, rutin, genistin, and ferulic acids were the most abundant phytochemicals detected in hot water extracts of G. hederacea L. (HWG). This study aimed to study the neuroprotective effects of phenolic acids and flavonoid-rich HWG against hydrogen peroxide (H 2 O 2 )-induced oxidative damage in PC12 cells and its inhibitory effect on acetylcholinesterase (AChE). The experiment analyzed cytotoxicity, ROS production, mitochondrial transmembrane potential (MMP) level, and caspase-3 activity and used comet assay and antioxidant enzyme activity to determine the redox status of PC12 cells. Results showed that the inhibitory effect of HWG on AChE was in a competitive pattern (IC 50 , 23.23 mg/ml). HWG antagonized H 2 O 2 -mediated cytotoxicity and DNA damage, reduced ROS production, stabilized MMP, and inhibited caspase-3 activity and apoptosis. Furthermore, HWG inhibited the release of cytochrome C and apoptosis-inducing factors (AIF) and decreased the malondialdehyde levels in PC12 cells. Collectively, HWG rich in antioxidant phenolic acids and flavonoids may have neuroprotective effects. Practical applicationsPolyphenolic compounds are one of the most important natural products, known to possess a range of health-promoting effects. In this study, it was found that HWG, which is rich in antioxidant phenolic acids and flavonoids, can protect PC12 cells from oxidative stress induced by H 2 O 2 and may have neuroprotective effects.
Background: Glechoma hederacea (Lamiaceae) is a traditional Chinese herb belonging to the Labiatae family and has many biological activities. This study aimed to investigate the in vitro effects of different polar parts of the water extracts of G. hederacea (Lamiaceae) on HepG2 cells and the possible underlying mechanism.Methods: The cytotoxic effects were determined using the MTT assay. Apoptosis was quantified using annexin V-FITC/PI staining. Caspase-3 and caspase-9 activities were measured using PhiphiLux-G1D2 kit. Apoptosis-related protein expression was determined using western blot analysis. Reactive oxygen species (ROS) generation, mitochondrial transmembrane potential (MMP), and calcium ion levels were measured using specific fluorescence probes and flow cytometry. The HepG2 cell antioxidant state was determined using DAPI and comet assay, and antioxidant enzyme activities. The polyphenol contents of different polar parts of fractional extracts were determined using HPLC. Results: Our results showed that rosmarinic acid, caffeic acid, and ferulic acid were the major polyphenolic components in the ethyl acetate fraction extract (EAFE) of G. hederacea L.. EAFE could significantly inhibit HepG2 cell proliferation, induce apoptosis, and cause S phase arrest. The apoptogenic activity of EAFE involved ROS induction, Ca2+ accumulation, glutathione depletion, MMP disruption, caspases 3, 9 activation, and Bax/Bcl-2 ratio increment.Conclusion: Our findings suggest that the polyphenols in the EAFE can inhibit HepG2 cell growth and induce apoptosis through the mitochondria-mediated pathway and ROS-mediated endoplasmic reticulum stress. EAFE could be developed as a functional food or nutraceutical ingredient for chemotherapy.
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