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Shilajit, a blackish-brown exudation obtained from steep rocks of different mountains, has been longly used as a therapeutic agent in traditional medicine. The present study was designed to evaluate the antioxidant, cytotoxic and hyperalgesia-suppressing activity of the aqueous and DMSO extracts of a native Shilajit. The antioxidant and cytotoxic effects of Shilajit extracts was determined using DPPH scavenging activity and MTT assay methods, respectively. In order to examine the hyperalgesia-suppressing activity of the Shilajit aqueous extract the STZ-induced diabetic animals were subjected to oral administration of the extract (50, 100 and 200 mg/kg daily) for six weeks followed by evaluating the behavioral examination (hot plate and tail flick tests) compared to those of diabetic control (Sham) and vehicle groups. The obtained results of antioxidant evaluation of Shilajit represented scavenging activity of 50% at concentration of 2500 μg/mL and 6000 μg/mL in the case of aqueous and DMSO extracts, respectively. Cytotoxic study of water extract of Shilajit revealed IC50 of 727.5±1.9 μg/mL and 1103±3.2 μg/mL on cell lines of MCF-7 (breast cancer) and A549 (lung cancer), respectively. Thermal pain response examination of diabetic rats treated with aqueous extract of Shilajit (100 mg/kg and 200 mg/kg) for six weeks reduced hyperalgesia compared to vehicle and Sham groups. To sum up, considering the moderate antioxidant and hyperalgesia-suppressing activity of this native Shilajit make it as a suitable candidate for further investigation after isolation and characterization of the active compounds. [ABSTRACT FROM AUTHOR]

A novel series of coumarin-lipoic acid conjugates were synthesized via cycloaddition click reaction to find out new multi-target-directed ligands (MTDLs) for treatment of Alzheimer's disease (AD). All of synthesized compounds were screened for neuroprotective and anti-cholinesterase activities. Based on primary screening, two compounds ( 5 and 11 ) were subjected to further biological evaluations. In particular, compound 11 which was the most potent AChE inhibitor showed good inhibitory effect on Aβ-aggregation and intracellular ROS (reactive oxygen species) formation, as well as the ability of selective bio-metal chelation and neuroprotection against H 2 O 2 - and Aβ 1-42 -induced cytotoxicity. In the light of these results, the applied hybridization approach introduced new promising lead compound with desired multifunctional properties, being useful in the treatment of Alzheimer's disease. [ABSTRACT FROM AUTHOR]

The present study was designed to isolate a highly selenium-tolerant lactobacillus strain from an Iranian traditional dairy product named as Spar. Different criteria such as tolerance to the low pH, simulated gastric juice (SGJ), simulated intestinal juice (SIJ) and bile salts tolerance as well as Caco-2 cell adhesion assay were examined to evaluate the probiotic potentials of the selected isolate. Furthermore, the antioxidant properties of the isolate cultivated in medium containing and free of SeO 3 2− ions were evaluated using DPPH scavenging and reducing power assays. The isolate was identified using conventional identification and 16S rDNA gene sequencing methods as Lactobacillus brevis LSe. The obtained results showed that the isolate was able to tolerate high concentration of sodium selenite (3.16 mM). By decreasing the pH of the SGJ from 6 to 3, the survival percent of L. brevis LSe was not significantly changed over the time ( p > 0.05). In addition, the survival percent of the isolate in the SIJ (pH 6 and pH 8) was not statistically altered after 3 h, 6 h and 24 h of incubation ( p > 0.05). In the presence of bile salts (0.3% and 0.6%) the survival rate of L. brevis LSe was not significantly decreased ( p > 0.05). L. brevis LSe also demonstrated the satisfactory ability to adhere to Caco-2 cells which were similar to that of the reference strain L. plantarum . The obtained results of antioxidant evaluation showed that L. brevis LSe containing elemental Se exhibited significantly higher radical scavenging ability (36.5 ± 1.31%) and reducing power (OD 700 , 0.14) than L. brevis LSe cultured in selenite-free medium ( p < 0.05). To sum up, further investigations should be conducted to merit the probable potential health benefit of Se-enriched L. brevis LSe and its application as Se-containing supplements or fermented foods. [ABSTRACT FROM AUTHOR]

The present study was designed for microwave assisted synthesis of zinc nanoparticles (Zn NPs) using Lavandula vera leaf extract in the presence of ZnSO 4 (1 mM). The biogenic Zn NPs were then characterized using scanning electron microscopy (SEM), energy dispersive X-ray (EDX), X-ray diffraction spectroscopy (XRD), UV–visible spectroscopy, and Fourier transform infrared spectroscopy (FTIR) techniques. Thereafter, the cytotoxic effect of ZnSO 4 and Zn NPs on different cell lines was investigated by MTT-based cytotoxicity assay and their antioxidant properties were assessed using DPPH scavenging activity and reducing power assay. The SEM micrograph showed that the Zn NPs had spherical shape with the size range of 30–80 nm. For A549, MCF-7, HT-29, and Caco-2 cell lines treated with Zn NPs, the concentration necessary causing 50% cell death (IC 50 ) was found to be 22.3 ± 1.1 μg mL −1 , 86 ± 3.7 μg mL −1 , 10.9 ± 0.5 μg mL −1 , and 56.2 ± 2.8 μg mL −1 , respectively. In the case of ZnSO 4 , the same results (IC 50 ) were observed at concentration of 81.6 ± 1.3 μg mL −1 (A549), 121.0 ± 2.4 μg mL −1 (MCF-7), 43.0 ± 1.4 μg mL −1 (HT-29), and 85.7 ± 2.3 μg mL −1 (Caco-2). The obtained results of antioxidant activity showed that the IC 50 values of butylated hydroxyanisole (BHA) and Zn NPs were 44 μg mL −1 and 65.3 μg mL −1 , respectively, while ZnSO 4 at concentration of 200 μg mL −1 exhibited only 10.9% DPPH radical scavenging effect. Moreover, the reducing power of Zn NPs and BHA were significantly higher than ZnSO 4 ( p < 0.05). To sum up, application of L. vera leaf extract combined with microwave heating energy led to simple and fast formation of Zn nanostructures exhibited higher antioxidant and cytotoxic activity compared to soluble Zn +2 ions. However, identification of the related mechanisms merit further studies. [ABSTRACT FROM AUTHOR]

The present study was designed to evaluate antioxidant and cytotoxic effect of selenium nanoparticles (Se NPs) biosynthesized by a newly isolated marine bacterial strain Bacillus sp. MSh-1. An organic–aqueous partitioning system was applied for purification of the biogenic Se NPs and the purified Se NPs were then investigated for antioxidant activity using DPPH scavenging activity and reducing power assay. Cytotoxic effect of the biogenic Se NPs and selenium dioxide (SeO2) on MCF-7 cell line was assesed by MTT assay. Tranmission electron micrograph (TEM) of the purified Se NPs showed individual and spherical nanostructure in size range of about 80–220nm. The obtained results showed that, at the same concentration of 200μg/mL, Se NPs and SeO2 represented scavenging activity of 23.1±3.4% and 13.2±3.1%, respectively. However, the data obtained from reducing power assay revealed higher electron-donating activity of SeO2 compared to Se NPs. Higher IC50 of the Se NPs (41.5±0.9μg/mL) compared to SeO2 (6.7±0.8μg/mL) confirmed lower cytotoxicity of the biogenic Se NPs on MCF-7 cell line. [ABSTRACT FROM AUTHOR]

New series of triazole-containing 3-phenylcoumarin–lipoic acid conjugates were designed as multi-functional agents for treatment of Alzheimer's disease. The target compounds 4a-o were synthesized via the azide-alkyne cycloaddition reaction and their biological activities were primarily evaluated in terms of neuroprotection against H 2 O 2 -induced cell death in PC12 cells and AChE/BuChE inhibition. The promising compounds 4j and 4i containing four carbons spacer were selected for further biological evaluations. Based on the obtained results, the benzocoumarin derivative 4j with IC 50 value of 7.3 µM was the most potent AChE inhibitor and displayed good inhibition toward intracellular reactive oxygen species (ROS). This compound with antioxidant and metal chelating ability showed also protective effect on cell injury induced by Aβ 1-42 in SH-SY5Y cells. Although the 8-methoxycoumarin analog 4i was slightly less active than 4j against AChE, but displayed higher protection ability against H 2 O 2 -induced cell death in PC12 and could significantly block Aβ-aggregation. The results suggested that the prototype compounds 4i and 4j might be promising multi-functional agents for the further development of the disease-modifying treatments of Alzheimer's disease. [ABSTRACT FROM AUTHOR]

In the present investigation a bismuth nanoparticles (Bi NPs) producing bacterial strain (designated as Delftia sp. SFG) was isolated from salt marsh and the biogenic Bi NPs was purified, characterized, and their cytotoxic and antioxidant activities were determined. The spherical shaped Bi NPs was inspected by transmission electron microscopy (TEM), scanning electron microscopy (SEM) equipped with energy dispersive X-ray (EDX) microanalyzer, and X-ray diffraction spectroscopy (XRD) method. Furthermore, the related size distribution pattern (20–120 nm), UV–vis and Fourier transform infrared (FTIR) spectrums of the produced Bi NPs were determined. The attained results of cytotoxic effect (determined by MTT-based colorimetric assay) of the purified Bi NPs revealed IC 50 of 10.9 ± 0.9 μg mL −1 , 35.4 ± 0.5 μg mL −1 , and 42.8 ± 1.7 μg mL −1 against A549, MCF-7, and 3T3 cell lines. Determination of antioxidant activity showed IC 50 values of 123.1 μg mL −1 and 307.2 μg mL −1 for butylated hydroxyanisole (BHA) and Bi NPs, respectively. [ABSTRACT FROM AUTHOR]