Histone deacetylases (HDACs) are a group of epigenetic enzymes that control gene expression through their repressive influence on histone deacetylation transcription. HDACs are probable therapeutic targets for cancer treatment, spurring the progress of different types of HDAC inhibitors. Further, natural-source-based derived bioactive compounds possess HDAC inhibitor property. In this way, we hypothesized that plant isoquinoline alkaloid berberine (BBR) could be a HDAC inhibitor in the human lung cancer A549 cell line. BBR represses total HDAC and also class I, II, and IV HDAC activity through hyperacetylation of histones. Furthermore, BBR triggers positive regulation of the sub-G/G cell cycle progression phase in A549 cells. Moreover, BBR-induced A549 cell growth arrest and morphological changes were confirmed using different fluorescence-dye-based microscope techniques. Additionally, BBR downregulates oncogenes (TNF-α, COX-2, MMP-2, and MMP-9) and upregulates tumor suppressor genes (p21 and p53) mRNA and protein expressions. Besides, BBR actively regulates Bcl-2/Bax family proteins and also triggered the caspase cascade apoptotic pathway in A549 cells. Our finding suggests that BBR mediates epigenetic reprogramming by HDAC inhibition, which may be the key mechanism for its antineoplastic activity.

Green-synthesized CuO NPs inhibited HDAC and therefore shown apoptosis mediated anticancer activity in A549 lung cancer cell line.

Pomegranate peel (PP) was sequentially extracted with hexane, ethyl acetate, methanol, methanol/water and water (C1–C5, respectively) and the extracts were assessed for its antioxidant and antidiabetic potential. Extracts, C2 and C3, which exhibited maximum free radical scavenging and α‐glucosidase inhibitory activity, were further fractionated using hexane, ethyl acetate and methanol (C2–F1, F2, F3; C3–F4, F5, F6). Fractions, F1 and F5, of methanol extract showed highest 2,2‐diphenyl picrylhydrazyl scavenging activity (IC50 – 3.69 and 4.39 µg/mL, respectively); F5 exhibited significantly high 2,2′‐azinobis 3‐ethylbenzothiazoline 6‐sulfonic acid, superoxide and hydroxyl radical scavenging activity (IC50 – 3.6, 20.89 and 10.7 µg/mL) and α‐glucosidase inhibition (IC50 – 0.0453 µg/mL). F5 demonstrated promising inhibition against LDL oxidation (IC50 – 16.2 µg/mL) and ACE inhibition properties (IC50 – 0.77 µg/mL). These findings suggest the ability of PP extracts to manage type 2 diabetes and associated complications. Practical Applications Natural antioxidants have been recommended as an aid for prevention and management of diabetes and associated complications. Pomegranate peel (PP) is reported to be a rich source of dietary antioxidants. We evaluated the effect of activity guided fractionation of PP on antioxidant and antidiabetic potential of extracts prepared by sequential extraction followed by its fractionation. The results indicated that on fractionation of crude extracts, the antioxidant and antidiabetic activity of some of fractions were significantly improved. The antidiabetic effect of PP active fraction may be related to α‐glucosidase inhibition and enhanced glucose uptake. The active fraction was found to be effective in reducing cardiac problems associated with diabetes by inhibiting LDL oxidation and ACE. The study points out the potential of PP as nutraceuticals for the prevention and management of type 2 diabetes and associated complications.

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Single chain surfactant–cobalt(iii) complexes interact with minor grooves of CT-DNA, whereas double chin surfactant–cobalt(iii) complexes bind with CT-DNA through partial intercalation.