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Berberine and jatrorrhizine are major bioactive components that are emerging as potential anti-cancer drugs. However, no zinc(II) – berberine/jatrorrhizine – curcumin compounds have been reported in the literature to date. Therefore, the molecular mechanisms associated with their cytotoxicity remain unexplored. To investigate the potential mitochondria-targeting ability, anti-neoplastic activity, and utility in cell imaging of berberine and jatrorrhizine derivates, four novel zinc(II) complexes, [Zn(Ber)(H 2 O)Cl 2 ] (Zn(Ber)), [Zn(Ber)(Cur)Cl] (Zn(CurBer)), [Zn(Jat)(H 2 O)Cl 2 ] (Zn(Jat)), and [Zn(Jat)(Cur)Cl] (Zn(CurJat)) bearing the berberine-derived ligand 2,2,2-trifluoroacetate 10-methoxy-9-((9-((2-(pyridin-2-yl)ethyl)amino)nonyl)oxy) −5,6-dihydro- [1,3]dioxolo[4,5-g]isoquinolino [(Torre et al., 2015; de Ruijter et al., 2020) 3,23,2-a]isoquinolin-7-ium (Ber), the jatrorrhizine-derived ligand 2,2,2-trifluoroacetate 2,9,10-trimethoxy-3-((9- ((2-(pyridin-2-yl)ethyl)amino)nonyl)oxy)-5,6-dihydroisoquinolino [(Torre et al., 2015; de Ruijter et al., 2020) 3,23,2-a]isoquinolin-7-ium (Jat), and/or curcumin (H-Cur) were first synthesised in this study. Zn(Ber) , Zn(CurBer) , Zn(Jat) , and Zn(CurJat) showed higher cytotoxicity against human MCF-7 (breast adenocarcinoma) cells than did cisplatin, with IC 50 values ranging from 0.21 to 4.45 μM. The anti-neoplastic activities of the zinc(II) – berberine/jatrorrhizine – curcumin complexes were in the following order: Zn(CurBer) > Zn(CurJat) > Zn(Ber) > Zn(Jat) > cisplatin > H-Cur > Ber > Jat > ZnCl 2. Among these, Zn(CurBer) displayed the highest cytotoxicity (0.21 ± 0.06 μM). Furthermore, mechanistic investigations revealed that Zn(CurBer) and Zn(CurJat) could accumulate in the mitochondria, exhibit red fluorescence, and trigger mitophagy and apoptosis. In vivo anti-cancer evaluations also suggested that Zn(CurBer) inhibited MCF-7 xenograft tumour growth more effectively than cisplatin and Zn(CurJat). This is the first report describing the synthesis of zinc(II) – berberine/jatrorrhizine – curcumin complexes and their potential use as molecular probes and mitochondria-targeting anti-neoplastic drugs. The red-fluorescence zinc(II)-berberine/jatrorrhizine-curcumin complexes with mitochondrion-targeting antitumor drugs can be used for MCF-7 cancer treatment. [Display omitted] • Novel red Zn(II)-curcumin fluorescent probes bearing berberine and jatrorrhizine were prepared. • These Zn(II) probes exhibited selective cytotoxicity toward MCF-7 versus HL-7702. • These Zn(II) probes could synergistically promote mitochondrion-mediated apoptosis. • These Zn(II) probes could enhance tumour therapeutic effects in vitro and vivo. [ABSTRACT FROM AUTHOR]

Following the novel ‘vapor induced phase inversion’ (VIPI) method, we have prepared curcumin loaded chitosan/cellulose micro crystals composite films and characterized them by thermo gravimetric analysis (TGA), X-ray diffraction (XRD) and scanning electron microscopy (SEM). The equilibrium moisture absorption behavior of these films was investigated under different relative humidity (RH) environments and the data obtained was interpreted by the GAB isotherm model successfully. The films were also studied for their curcumin release behavior in the physiological fluid (PF) at 37 °C and the kinetic data obtained was best interpreted by Higuchi model. Finally, the films showed fair antimicrobial action against bacteria and fungi. [ABSTRACT FROM AUTHOR]

The synthesis, detailed structural and physicochemical characterization of a novel Ga(III)-curcumin complex with the ancillary aromatic chelator 1,10-phenanthroline is presented herein. The complex constitutes the only crystallographically characterized structure with Ga(III) as the metal core and a curcuminoid as the ligand. The photophysical properties of the complex revealed a significant red-shift in absorption, increased photostability and comparable free radical generation compared to plain curcumin. They all are highly desirable properties for a photosensitizer. Photodynamic therapy is a non-invasive method for the treatment of various cancers which requires a photosensitizing molecule able to generate reactive oxygen species upon light irradiation. Curcumin has been studied as a promising photosensitizer against cancer cells and metal complexation has been shown to increase its photodynamic effect. The novel curcumin-Ga complex exhibited no dark toxicity at low concentrations against MCF-7 breast cancer cells and upon irradiation a light-dose dependent decrease in cell survival was observed. This photodynamic effect was superior to the one caused by curcumin alone making the Ga(III)-curcumin complex a more promising photosensitizer than the parent ligand. [Display omitted] [ABSTRACT FROM AUTHOR]