Hay synthesis of a novel series of symmetrically tetra-substituted thiophenyl zinc(II)phthalocyanines (RS)ZnPcs 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)ZnPcs 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.
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.
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, H-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.
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.
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.
Several species of thymus have therapeutic properties, so they are used in traditional medicine. In this work was carried out to synthesize Thymus vulgalis silver nanoparticles (TSNPS) and evaluate antioxidant and antimicrobial activities of TSNPS and T. vulgalis essential oil extract (TEOE). The essential oils analyzed by GC-MS and were characterized. Major compounds of phenol, 2 methyl 5 (1 methylethyle) (CAS), thymol and 1,2 Benzene dicarboxylic acid, 3 nitro (CAS) (48.75%, 32.42% and 8.12%, respectively) were detected. Results demonstrated that the TSNPS gave a highest DPPH radical scavenging activity, it was obtained 97.2 at 1000 ug/ml. TSNPS, Thymus + Hexane (T+H), Thymus + Ethanol (T+E) gave the greatest antimicrobial activity than amoxicillin (AM) and ciprofloxacin (CIP). In conclusion: The essential oil of thymus (Vulgaris) and thymus (Vulgaris) silver nanoparticles can be a good source of natural preservatives as an antioxidant and antimicrobial agents for increasing the shelf life of foodstuffs.
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