SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL STUDY OF MANNICH BASES AND THEIR COPPER (II) COMPLEXES

Objective: The present study is focused on the synthesis of novel Mannich bases and their metal complexes, and to characterize them by physical, chemical and biological methods. Mannich bases, 2-(piperazin-1-yl(thiophen-2-yl)methyl)hydrazinecarboxamide (PTMHC), 2-(piperazin-1-yl(thiophen-2-yl)methyl)hydrazinecarbothioamide (PTMHCT), and 2-((4-methylpiperazin-1-yl)(thiophen-2-yl)methyl)hydrazinecarboxamide (MPTMHC) and 2-((4-methylpiperazin-1-yl)(thiophen-2-yl)methyl)hydrazinecarbothioamide (MPTMHCT), were prepared by Mannich condensation method.Methods: The compounds and complexes were prepared by known literature methods. Characterizations were carried out through physical methods such as elemental analyses, melting point and TLC. IR, 1H NMR, [13]C NMR and Mass spectral studies were carried out to characterize the ligands. The methods like EPR, magnetic susceptibility measurements, conductance measurements and thermal analysis were carried out for complexes besides the UV-Vis and IR spectral studies. Anti-cancer activity of synthesized ligands was performed using human lung and colon cancer cell lines.Results: Eight compounds have been prepared and characterized. Four among the eight compounds were used as ligands for the preparation of metal complexes. The results of physical and chemical methods show all the complexes act as bidentate ligands. The coordination with the metal ion takes place through N, S and O atoms. The results of molar conductivity and magnetic susceptibility measurements reveal the electrolytic and non-electrolytic nature of the metal complexes. EPR and TG-DTA studies also support the other spectral data.Conclusions: Copper (II) complexes of PTMHC, PTMHCT, MPTMHC, and MPTMHCT were prepared and their structures were determined. The anti-cancer activity of the synthesized ligands and their complexes was evaluated. The synthesized novel ligands of Mannich bases can serve as a potential anti-cancer agent.Â

The Biochemical evaluation of Indus viva I pulse natural ayurvedic syrup and It's In silico-interaction analysis: Biochemical evaluation of Indus viva I pulse natural ayurvedic syrup and It's In silico-interaction analysis

Indusviva I pulse health drink is a natural and ayurvedic syrup that is rich in antioxidants, essential carbohydrates, health-promoting vitamins, lipids, and proteins and is used to treat aches, pains, ulcers, inflammatory, heart, and respiratory diseases and for regulating fat, cholesterol levels, blood circulation and for boosting immunity. Indusviva ipulse health drink is a unique combination of herbs and an antioxidant fruit blend that is used in folk medicine owing to its medicinal properties of phytoconstituents by all age groups in South Asia. The study aimed to evaluate GC-MS, HPLC, anticancer, antidiabetic, and spectral studies that are used to disclose phytochemicals and their medicinal properties. GC-MS and HPLC chromatogram of methanol extracts exhibited 12 and 6 peaks respectively confirming the presence of 12 phytoconstituents in Indusviva ipulse health drink (1I – 12I). The total phenol and flavonoid content found in the extracted sample of Indusviva ipulse health drink were 0.16 and 0.36 mg/ml respectively. It is a polyherbal formulation of brown-coloured liquid whose UV spectrum in methanol is characteristic of an aromatic compound with λmax of 319 and 412 nm. IR spectrum gave peaks at 3457, 2922, 2857, 2121, 1641, 1055, 1033, and 621cm-1 indicating the presence of an alcoholic, alkyl, aldehyde or ketone, alkyne, carbonyl, anhydride, and methyl group respectively. LC-HRMS study gave these molecular weights (m/z): 1134. 7017, 1150.6475, and 1168.6797. Aromatic characteristics were confirmed through UV, IR, 1H-NMR, 13C-NMR, and LC-HRMS spectral studies. 1H-NMR study indicates the presence of aromatic protons and methyl protons. Aqueous extract of Indusviva ipulse health drink was tested for Cytotoxicity Assay of human bone cancer (MG-63) cell lines and ptyalin prevent characters that exhibited a valid inhibitory value of 90.87% in 10 µg/ml for MG-63 and value of 74.41% in 500 μg/ml for alpha-amylase which is comparatively more efficient than the available standard drug. Cytotoxicity Assay for human bone cancer (MG-63) cell lines and alpha-amylase both showed the inhibitory activity of IC50 68.95 and IC50 36.18 μg/ml respectively. Based on the result of this research, it can be proposed that Indusviva I pulse health drink may serve as a potential remedy for human bone cancer (MG-63) cell line and that alpha-amylase inhibitory activity is proportional to the dose

Synthesis, characterization, anticancer activity, optical spectroscopic and docking studies of novel thiophene-2-carboxaldehyde derivatives

2-((4-Methylpiperazin-1-yl)(thiophen-2-yl)methyl)hydrazinecarboxamide (L1) and (2-(piperazin-1-yl(thiophen-2-yl)methyl)hydrazinecarboxamide (L2) from the family of thiophene-2-carboxaldehyde derivatives have been synthesized. These new compounds have good antibacterial as well as antifungal activity and also less toxic in nature. Exemplary binding characteristics of these novel compounds and pharmacokinetic mechanism were confirmed by optical spectroscopic, anticancer and docking studies. The binding of thiophene-2-carboxaldehyde derivatives to carrier protein, Human Serum Albumin (HSA) has been investigated by studying its quenching mechanism, binding kinetics and the molecular distance (r) between donor (HSA) and acceptor (thiophene-2-carboxaldehyde derivatives) according to Forster’s theory of non-radiative energy transfer (FRET). The micro environment of HSA has also been studied by using synchronous fluorescence spectroscopy technique and the molecular docking technique has been used to explore the hydrogen bonding, hydrophobic interaction between the human serum albumin with L1 and L2 compound

Sublethal Effects of Arsenic on Oxygen Consumption, Hematological and Gill Histopathological Indices in Chanos chanos

Background: The current study was performed aiming to evaluate possible changes in the effect on oxygen consumption, hematology and gill histopathological parameters in fish (Chanos chanos) upon exposure to sublethal concentration of the metalloid arsenic. Methods: Bioassay tests were conducted for determining the LC50 values of arsenic for 96 h. Oxygen consumption in control and arsenic-exposed fish was estimated using Winkler’s method. Red blood corpuscular (RBC) count was examined with a Neubauer counting chamber under a phase contrast microscope. Hemoglobin (Hb) was estimated following the acid hematin method. Histopathological studies were carried by processing and staining the gill tissues with hematoxylin and eosin in accordance with standard histological techniques. They were then subjected to examination under a scanning electron microscope. Results: Chanos chanos exposed to 1/10th of LC50 (24.61%) for a period of 30 days exhibited a maximum decline in the rate of respiration, followed by a decline in RBC and Hb above 45.59% and 51.60%, respectively. Significant toxic lesions encompassing fused gill lamellae, detached gill epithelium, hyperplasia and hypertrophy of respiratory epithelium became heavy handed on the 30th day. Conclusion: Information synthesized from our study serves to be useful in monitoring and managing (As) contamination in the aquatic environment