Assessment of antidiabetic, anti-inflammatory, antioxidant and anticancer activity competence of methonolic extracts of Trianthema ortulacastrum and Andrographis paniculata.

An in-vitro investigation was performed to evaluate and compare the phytochemical, antioxidant, antidiabetic, anti-inflammatory, and anti-lung cancer activities of methanol extracts of aerial parts of Andrographis paniculata and Trianthema portulacastrum. Furthermore studied major functional groups of phytochemicals present in the methanol extracts of these plants through Fourier transform infrared (FTIR) analysis. The results showed that the methanol extract of A. paniculata contain more number of pharmaceutically valuable phytochemicals such as alkaloids, flavonoids, terpenoids, saponin, glycoside, phytosterol, and tannin than T. portulacastrum. Similar way the methanol extract of A. paniculata showed considerable dose dependent antioxidant (DPPH: 63%), antidiabetic (α-amylase: 82.31% and α-glucosidase inhibitions: 72.34%), and anti-inflammatory (albumin-denaturation inhibition: 76.3% and anti-lipoxygenase: 61.2%) activities (at 900 µg mL-1 concentration) than T. portulacastrum. However, the anti-lung cancer activities of these test plants against A549 cells were not considerable. According to FTIR analysis, the A. paniculata methanol extract has a larger number of characteristic peaks attributed to the active functional groups of pharmaceutically valuable bioactive components that belong to different types of phytochemicals. These findings imply that A. paniculata methanol extracts can be used for additional research, such as bioactive compound screening and purification, as well as assessing their potential biomedical uses in various in-vitro and in-research settings.

Nano-composite rGO-Ag-Cu-Ni mediated photocatalytic degradation of anthracene and benzene.

Polycyclic aromatic hydrocarbons (PAHs) are omnipresent, persistent, and carcinogenic pollutants continuously released in the atmosphere due to the rapid increase in population and industrialization worldwide. Hence, there is an ultimate rise in concern about eliminating the toxic PAHs and their related aromatic hydrocarbons from the air, water, and soil environment by employing efficient removal technologies using nanoparticles as a catalyst. Here, the degradation of selective PAHs viz., anthracene and benzene using laboratory synthesized rGO-Ag-Cu-Ni nanocomposite (catalyst) was studied. Characterization studies revealed the nanocomposites exhibited surface plasma resonance at 350 - 450 nm, confirming the presence of Ag, Cu, and Ni metal ions embedded on the reduced graphene substrate. It was found that the nanocomposites synthesized were spherical, amorphous in nature, and aggregated together with measurements ranging from 423 to 477 nm. An SEM-EDX analysis of the nanocomposite demonstrated that it contained 25.13% O, 14.24% Ni, 27.79% Cu, and 32.84% Ag, which confirms the synthesis of the nanocomposite. Crystalline, sharp nanocomposites of average size 17-41 nm with an average diameter of 118.5 nm (X-ray diffraction and DLS) were observed. FTIR spectra showed that the nanocomposites had the functional groups alkanes, alkenes, alkynes, carboxylic acids, and halogen derivatives. Batch adsorption studies revealed that the maximum degradation achieved at optimum nano-composite concentration of 10 µg/mL, pH value of 5, PAHs concentration of 2 µg/mL and effective irradiation source being UV radiations in the case of both benzene and anthracene pollutants. The degradation of benzene and anthracene followed Freundlich & Langmuir isotherm with the highest R2 value of 0.9894 & 0.9885, respectively. Adsorption kinetic studies under optimum conditions revealed that the adsorption of both benzene and anthracene followed Pseudo-second order kinetics. Antimicrobial studies revealed that the synthesized nano-composite exhibited potential antimicrobial activity against Gram positive bacterium (Bacillus subtilis, Staphylococcus aureus), Gram negative bacterium (Klebsiella pneumonia, Escherichia coli) and fungal strain (Aspergillus niger) respectively. Thus, the synthesized rGO-Ag-Cu-Ni nano-composite acts as an effective antimicrobial agent as well as a PAHs degrading agent, helping to overcome antibiotics resistance and to mitigate the overgrowing PAHs pollution in the environment.

Deacetylated nimbin analog N2 fortifies alloxan-induced pancreatic ß-cell damage in insulin-resistant zebrafish larvae by upregulating phosphoenolpyruvate carboxykinase (PEPCK) and insulin levels.

This study aims to evaluate the protective behaviour of N2, a semi-natural analog of nimbin, for its anti-diabetic efficacy against alloxan-induced oxidative damage and ß-cell dysfunction in in-vivo zebrafish larvae. A 500 µM of alloxan was exposed to zebrafish larvae for 24 h to induce oxidative stress in the pancreatic ß-cells and co-exposed with N2 to study the protection of N2 by inhibiting ROS by DCFH-DA, DHE and NDA staining along with Cellular damage, apoptosis and lipid peroxidation. The zebrafish was further exposed to 500 µM alloxan for 72 h to induce ß-cell destruction along with depleted glucose uptake and co-exposed to N2 to study the protective mechanism. Glucose levels were estimated, and PCR was used to verify the mRNA expression of phosphoenolpyruvate carboxykinase (PEPCK) and insulin. Alloxan induced (24 h) oxidative stress in the pancreatic ß-cells in which N2's co-exposure inhibited ROS by eliminating O-2 radicals and restoring the glutathione levels, thus preventing cellular damage and lipid peroxidation. The zebrafish exposed to 500 µM alloxan for 72 h was observed with ß-cell destruction along with depleted glucose uptake when stained with 2NBDG, wherein N2 was able to protect the pancreatic ß-cells from oxidative damage, promoted high glucose uptake and reduced glucose levels. N2 stimulated insulin production and downregulated PEPCK by inhibiting gluconeogenesis, attenuating post-prandial hyperglycemia. N2 may contribute to anti-oxidant protection against alloxan-induced ß-cell damage and anti-hyperglycemic activity, restoring insulin function and suppressing PEPCK expression.

Design and In Vitro Evaluation of Novel Cationic Lipids for siRNA Delivery in Breast Cancer Cell Lines.

Breast cancer is the most common cause of cancer mortality in Western nations, with a terrible prognosis. Many studies show that siRNA plays a role in the development of tumors by acting as a tumor suppressor and apoptosis inhibitor or both. siRNAs may be used as diagnostic and prognostic biomarkers in breast cancer. Antisurvivin siRNA was chosen as a therapeutic target in breast cancer treatment because it directly targets survivin, an inhibitor of apoptosis protein, that causes cell death. However, siRNA-based treatment has significant limitations, including a lack of tissue selectivity, a lack of effective delivery mechanisms, low cellular absorption, and the possibility of systemic toxicity. To address some of these issues, we provide a siRNA delivery method based on cationic lipids. In the recent past, cationic liposomes have displayed that they offer a remarkable perspective in proficient siRNA delivery. The presence of a positive charge plays a vital role in firm extracellular siRNA binding along with active intracellular siRNA separation and low biological adversities. Consequently, the methods for developing innovative cationic lipids through rendering and utilization of appropriate positive charges would certainly be helpful for benign and effective siRNA delivery. In the current study, an effort was made to synthesize a 3,4-dimethoxyaniline lipid (DMA) to improve the effectiveness and protection of successful siRNA delivery. DMA cationic lipid successfully delivered survivin siRNA that reduced the survivin mRNA expression, indicating the possibility of utilizing siRNA therapeutics for breast cancer. It is expected that this innovative quaternary amine-based liposome can open up new avenues in the process of developing an easy and extensively used platform for siRNA delivery. Cationic lipoplexes, a potential carrier system for siRNA-based therapies in the treatment of breast cancer, were proven by our data.

Synthesis and biological activity of Schiff base series of valproyl, N-valproyl glycinyl, and N-valproyl-4-aminobenzoyl hydrazide derivatives.

Series of Schiff bases of valproic acid hydrazide, N-valproylglycine hydrazide and N-valproyl-4-aminobenzoyl hydrazide derivatives were synthesized and characterized by IR, NMR ((1)H- and (13)C-NMR) and elemental analysis. The prepared compounds were evaluated in transgenic zebrafish embryos (Tg: flil-1: enhanced green fluorescent protein (EGFP)) for antiangiogenic activity and in HepG2 liver carcinoma cell line for anti cancer activity. The Schiff bases of N-valproylglycine hydrazide derivatives were most potent in term of suppressing angiogenic blood vessels formation and anticancer activity at very low concentration, followed by the Schiff bases of valproic acid hydrazide derivatives which exhibited moderate activity, while the Schiff bases of N-valproyl-4-aminobenzoyl hydrazide derivatives, ethyl 4-(2-propylpentanamido)benzoate (VABE) and N-(4-(hydrazinecarbonyl)phenyl)-2-propylpentanamide (VABH) in contrast exhibited pro-angiogenic activity and weaker anticancer activity which mean that these derivatives targeted a common signaling pathway in term of affecting the blood vessels formation.