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BACKGROUND/AIMS: The naturally occurring phenolic chemical curcumin (CUR), which was derived from the Curcuma longa plant, has a variety of biological actions, including anti-inflammatory, antimicrobial, antioxidant, and anticancer activities. Curcumin is known for its restricted bioavailability due to its hydrophobicity, poor intestinal absorption, and quick metabolism. To boost the biological effects of these bioactive molecules, it is necessary to raise both their bioavailability and their solubility in water. Aim: The aim of this study is to synthesize and characterize hybrid organic-inorganic complexes of copper and cobalt, and to evaluate their antimicrobial potential against a range of pathogenic microorganisms. METHODS: The synthesis of metal curcumin complexes (Cu-CUR and Co-CUR) was achieved by mixing curcumin with copper acetate monohydrate. The solid residue was isolated, filtered, and dried in an oven. X-ray diffraction analysis was used to identify the structure and phase of the prepared samples. FTIR spectra were recorded using a Shimadzu 2200 module. The antimicrobial activity of the prepared complexes was evaluated against four bacterial strains and two Candida species. The chemical materials were dissolved in DMSO to a final concentration of 20%, and the plates were incubated at 37°C for 24 hours. The results showed that the prepared complexes had antimicrobial activity against the tested microorganisms. RESULTS: The study compared the Powder X-ray diffraction (XRD) patterns of prepared copper and cobalt complexes to pure curcumin, revealing new, isostructural complexes. The FTIR analysis showed that the Cu-CUR and Co-CUR complexes varied in their inhibitory effect against microorganisms, with Co-CUR being more effective. The results are consistent with previous studies showing the cobalt-curcumin complex was effective against various bacterial genera, with inhibition activity varying depending on the species and strains of microorganisms. CONCLUSION: Copper and cobalt curcumin complexes, synthesized at room temperature, exhibit high crystallinity and antimicrobial activity. Co-CUR, with its superior antibacterial potential, outperforms pure curcumin in inhibiting microbes. Further investigation is needed to understand their interaction mechanisms with bacteria and fungi.

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The current study inspects the therapeutic effects of orally ingested insulin-loaded chitosan nanobeads (INS-CsNBs) with a pectin-dextrin (PD) coating on streptozotocin (STZ)-induced diabetes in Wistar rats. The study also assessed antioxidant effects in pancreatic tissue homogenate, insulin, C-peptide, and inflammatory markers interleukin-1 beta and interleukin-6 (IL-1ß and IL-6) in serum. Additionally, histopathological and immunohistochemical examination of insulin granules, oxidative stress, nuclear factor kappa B (NF-κB P65), and sirtuin-1 (SIRT-1) protein detection, as well as gene expression of nuclear factor erythroid 2-related factor 2 (Nrf2), heme oxygenase-1 (HO-1), B-cell lymphoma 2 (Bcl2), and Bcl-2-associated X protein (Bax) in pancreatic tissue were investigated. After induction of diabetes with STZ, rats were allocated into 6 groups: the normal control (C), the diabetic control (D), and the diabetic groups treated with INS-CsNBs coated with PD shell (50 IU/kg) (NF), free oral insulin (10 IU/kg) (FO), CsNBs-PD shell (50 IU/kg) (NB), and subcutaneous insulin (10 IU/kg) (Sc). The rats were treated daily for four weeks. Treatment of diabetic rats with INS-CsNBs coated with PD shell resulted in a significant improvement in blood glucose levels, elevated antioxidant activities, decreased NF-κB P65, IL-1ß, and IL-6 levels, upregulated Nrf-2 and HO-1, in addition to a marked improvement in the histological architecture and integrity compared to the diabetic group. The effects of oral INS-CsNBs administration were comparable to those of subcutaneous insulin. In conclusion, oral administration of INS-loaded Cs-NBs with a pectin-dextrin shell demonstrated an ameliorative effect on STZ-induced diabetes, avoiding the drawbacks of subcutaneous insulin.

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Diabetes is an emerging health condition globally and is suggested to have a direct connection with the gut microbiota that determine our metabolic outcomes. Sensitivity to insulin and glucose metabolism is normal in healthy people as compared to those people who cannot maintain their glucose metabolism. One of the reasons of the differences is that healthy people have different microbiome that leads to achieve more short chain fatty acids and make up more branched amino acids, while the gut microbiota of the other group of people are more likely to produce compounds that affects glucose metabolism. Herein, this review will present the research related to the impact of gut microbes on diabetes carried out in the past decade. The review focus on the relation between gut microbiota and Type-1 Diabetes (T1D), Type-2 Diabetes (T2D), and how gut microbiota could be an alternative therapy for treatment of diabetes.

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The current study offers an efficient design of novel nanoparticle microspheres (MCs) using a hydrothermal approach. The Co0.5Ni0.5GaxFe2-xO4 (0.0 ≤ x ≤ 1.0) MCs were prepared by engineering the elements, such as cobalt (Co), nickel (Ni), iron (Fe), and gallium (Ga). There was a significant variation in MCs' physical structure and surface morphology, which was evaluated using energy dispersive X-ray analysis (EDX), X-ray diffractometer (XRD), high-resolution transmission electron microscopy (HR-TEM), and scanning electron microscope (SEM). The anti-proliferative activity of MCs was examined by MTT assay and DAPI staining using human colorectal carcinoma cells (HCT-116), human cervical cancer cells (HeLa), and a non-cancerous cell line-human embryonic kidney cells (HEK-293). Post 72 h treatment, MCs caused a dose dependent inhibition of growth and proliferation of HCT-116 and HeLa cells. Conversely, no cytotoxic effect was observed on HEK-293 cells. The anti-fungal action was assessed by the colony forming units (CFU) technique and SEM, resulting in the survival rate of Candida albicans as 20%, with severe morphogenesis, on treatment with MCs x = 1.0. These findings suggest that newly engineered microspheres have the potential for pharmaceutical importance, in terms of infectious diseases and anti-cancer therapy.

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In the present study, biocompatible manganese nanoparticles have been linked with zinc and iron molecules to prepare different derivatives of Mn0.5Zn0.5ErxYxFe2-2xO4 NPs (x = 0.02, 0.04, 0.06, 0.08, 0.10), using an ultrasonication approach. The structure, surface morphology, and chemical compositions of Mn0.5Zn0.5ErxYxFe2-2xO4 NPs were elucidated by X-ray diffractometer (XRD), High-resolution transmission electron microscopy (HR-TEM), scanning electron microscope (SEM), and Energy Dispersive X-Ray Analysis (EDX) techniques. The bioactivity of Mn0.5Zn0.5ErxYxFe2-2xO4 NPs on normal (HEK-293) and (HCT-116) colon cancer cell line was evaluated. The Mn0.5Zn0.5ErxYxFe2-2xO4 NPs treatment post 48 h resulted in a significant reduction in cells (via MTT assay, having an IC50 value between 0.88 µg/mL and 2.40 µg/mL). The specificity of Mn0.5Zn0.5ErxYxFe2-2xO4 NPs were studied by treating them on normal cells line (HEK-293). The results showed that Mn0.5Zn0.5ErxYxFe2-2xO4 NPs did not incur any effect on HEK-293, which suggests that Mn0.5Zn0.5ErxYxFe2-2xO4 NPs selectively targeted the colon cancerous cells. Using Candida albicans, antifungal activity was also studied by evaluating minimum inhibitory/fungicidal concentration (MIC/MFC) and the effect of nanomaterial on the germ tube formation, which exhibited that NPs significantly inhibited the growth and germ tube formation. The obtained results hold the potential to design nanoparticles that lead to efficient bioactivity.

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Combining two or more nanoparticles is a promising approach. Previously we have reported synthesis of nanoparticles Dysprosium (Dy) substituted with manganese (Mn) zinc (Zn) by using ultrasonication method. The five different nanoparticles (NPs) Mn0.5Zn0.5DyxFe2-xO4 (x ≤ 0.1) have been structurally and morphologically characterized but there is no report on the biological application of these NPs. In the present study, we have examined the anti-cancer, anti-bacterial, and anti-fungal activities of Mn0.5Zn0.5DyxFe2-xO4 (x ≤ 0.1) NPs. Human colorectal carcinoma cells (HCT-116) were tested with different concentrations of NPs by using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. In addition, the impact of NPs was also examined on normal cells such as human embryonic kidney cells, HEK-293. After 48 h of treatment, Mn0.5Zn0.5DyxFe2-xO4 NPs (x = 0.02, 0.04 and 0.06) showed no inhibitory action on cancer cell's growth and proliferation, whereas Mn0.5Zn0.5DyxFe2-xO4 NPs (x = 0.08 and 0.1) showed profound inhibitory action on cancer cell's growth and proliferation. However, the treatment of Mn0.5Zn0.5DyxFe2-xO4 NPs on the normal cells (HEK-293) did not show cytotoxic or inhibitory action on HEK-293 cells. The treatment of Mn0.5Zn0.5DyxFe2-xO4 NPs (x ≤ 0.1) also inhibited both the bacteria (Escherichia coli ATCC35218 and Staphylococcus aureus) with lowest MIC and MBC values of 4 and 8 mg/mL and fungus (Candida albicans) with MIC and MFC values of 4 and 8 mg/mL on treatment with x = 0.08 and 0. 1.

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There is enormous interest in combining two or more nanoparticles for various biomedical applications, especially in anti-cancer agent delivery. In this study, the microsphere nanoparticles were prepared (MSNPs) and their impact on cancer cells was examined. The MSNPs were prepared by using the hydrothermal method where strontium (Sr), barium (Ba), dysprosium (Dy), samarium (Sm), and iron oxide (Fe8-2xO19) were combined, and dysprosium (Dy) and samarium (Sm) was substituted with strontium (Sr) and barium (Ba), preparing Sr0.5Ba0.5DyxSmxFe8-2xO19 (0.00 ≤ x ≤ 1.0) MSNPs. The microspheres were characterized by X-ray powder diffraction (XRD), high-resolution transmission electron microscopy (HR-TEM), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and energy-dispersive X-ray spectroscopy (EDX) techniques. The diffraction pattern of nanohexaferrites (NHFs) reflected the signature peaks of the hexagonal structure. The XRD revealed a pure hexagonal structure without any undesired phase, which indicated the homogeneity of the products. The crystal size of the nanoparticles were in the range of 22 to 36 nm by Scherrer's equation. The SEM of MSNPs showed a semi-spherical shape with a high degree of aggregation. TEM and HR-TEM images of MSNPs verified the spherical shape morphology and structure that approved an M-type hexaferrite formation. The anti-cancer activity was examined on HCT-116 (human colorectal carcinoma) and HeLa (cervical cancer cells) using MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay and post-48 h treatment of MSNPs caused a dose-dependent inhibition of HCT-116 and HeLa cell proliferation and growth. Conversely, no significant cytotoxic effect was observed on HEK-293 cells. The treatments of MSNPs also induced cancer cells DNA disintegration, as revealed by 4',6-diamidino-2-phenylindole (DAPI) staining. Finally, these findings suggest that synthesized MSNPs possess potential inhibitory actions on cancerous cells without harming normal cells.

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The aim of this study was to synthesize a series of nickel(II)phthalocyanines (NiPcs) bearing four 4(3H)-quinazolinone ring system units, (qz)4NiPcs 4a-d. The electronic factors in the 4(3H)-quinazolinone moiety that attached to the NiPc skeleton had a magnificent effect on the antibacterial activity of the newly synthesized (qz)4NiPcs 4a-d against Escherichia coli. The minimum MICs and MBCs value were recorded for compounds 4a, 4b, 4c, and 4d, respectively. The results indicated that the studied (qz)4NiPcs 4a-d units possessed a broad spectrum of activity against Escherichia coli. Their antibacterial activities were found in the order of 4d > 4c > 4b > 4a against Escherichia coli, and the strongest antibacterial activity was achieved with compound 4d.

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BACKGROUND: The aim of the present study was to modify the structural activity of zinc(II)phthalocyanine by combining it with thiophenyl groups then loaded in lipid nano-carriers and evaluate its parameters required for the structure-activity relationship (SAR) for photodynamic therapy (PDT) of cancer. METHODS: Tetra (4-Thiophenyl) sulfonated phthalocyaninatozinc(II) (PhS·SO3Na)4ZnPc 5 was synthesized and characterized by various spectroscopic methods as a test compound. Liver hepatocellular carcinoma (HepG2) cells were treated with the synthesized (PhS·SO3Na)4ZnPc 5 derivative loaded in lipid nano carriers to understand the effect of combined compound on liver cancer cells. Furthermore, HepG2 cells were irradiated by visible red light at 60 mW/cm2 for 20 min. The phototoxicity of (PhS·SO3Na)4ZnPc 5 after being formulated in both (L) and transfersomes (T) was investigated. RESULTS: Overall, the results indicate that combination of thiophenyl groups substitution, in particular in the structure of sulfonated zinc phthalocyanine is able to improve the photodynamic properties of ZnPc, and (PhS·SO3Na)4ZnPc 5 loaded in lipid nano-carriers can be a promising combined PDT treatment strategy for Liver hepatocellular carcinoma (HepG2) cells. CONCLUSIONS: The new formulation ZnPc-lipid nano-carriers will be beneficial in the upcoming clinical trials and would enhance the inhibition of tumor growth.

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Potential biologically active derivatives of the curcumin were prepared by the cyclocondensation reaction cyclohexanone 2, imino pyrimidine 3, pyrmidinones 4, thiopyrimidine 6 and pyranone 5, 7 when treated with acetylacetone, guanidine, ureaethylcyanoacetate, thiourea and ethylacetoacetate, respectively. The structures of compounds (2-7) were elucidated by means of microanalysis as well as spectral measurements such as IR, 1H-NMR, MS. The anti-diabetic potential of curcumin derivatives were evaluated by assessing amylase inhibition assay, also inhibition of histamine release activity of curcumin derivatives were assessed by U937 human monocytes. The results for amylase inhibition activity revels that the curcumin inhibits α-amylase in a concentration dependent manner. Compounds 4 and 5 exhibited significant inhibitory activity against amylase enzyme and was comparable with that of acrabose. Also, compounds 5, 6 and 7 exhibited significant inhibitory activity against histamine. Our results concluded that curcumin pyrmidinones and pyranone derivatives have highly effects as anti-diabetic and anti-histamine activities.

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Hay synthesis of a novel series of symmetrically tetra-substituted thiophenyl zinc(II)phthalocyanines (RS)4ZnPcs 4a-c was reported. Their novel 4-thiophenyl-phthalonitriles precursors 3(a-c) were synthesized from their substituted thiophenols 2(a-c). They were screened for their in-vitro antitumor activity on Human lung adenocarcinoma (A549), human breast adenocarcinoma (MCF-7) and hepatocellular carcinoma in comparison with healthy normal cells (human fibroblast cells). Preliminary study of the structure-activity relationship showed that electronic factors in the trifluoromethyl moiety that attached to the ZnPc skeleton had a magnificent effect on the antitumor activity of the newly synthesized (RS)4ZnPcs 4a-c. More interestingly, the ZnPc 4c showed promising anticancer activity against the tested human cancer cell lines. The detailed synthesis, characterization and biological screening data were reported.

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