Posted by admin on Dec 31, 2020 in |
Cancer is the second leading cause of death globally. Among the group of cancer diseases, breast cancer is the most common type of cancer to affect women. The treatment options that are currently available for this include surgery, radiation therapy and therapy through medication or drugs. But, since all these are harmful and have severe side effects, drugs from natural plant compounds are being developed to act against cancer and its metastatic activity. The aim of this article is to perform qualitative and quantitative analysis of alkaloids in leaf extract of Carica papaya (CP) and also study the anticancer and anti-metastatic activity of it in MCF-7 breast cancer cell lines. CP, commonly known as papaya or papaw, belonging to the family of Caricaceae has many medicinal uses including dengue treatment, anti-inflammatory and anticancer properties. The leaf extract of CP was prepared by ethyl acetate extraction method. Various tests such as MTT assay, Wound healing assay, DNA fragmentation assay, Caspase 7/9 induction detection assay and Annexin V assay were performed...
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Posted by admin on Dec 31, 2020 in |
Cobalt(II), nickel(II), copper(II) and zinc(II) complexes having the general formula ML2 (where, L= cuminaldehyde benzoyl-hydrazone, CABH) have been synthesized and characterized based on mass spectra, molar conductivity, FT-IR and UV-Vis spectral data. The complexes are found to be non-electrolytes. FT-IR data suggest that the CABH acts as a uni-negative bidentate ligand. The copper complex is investigated using ESR spectroscopy at room temperature and liquid nitrogen temperature (LNT). The spin Hamiltonian, orbital reduction, and bonding parameters are calculated for the complex. The interactions of these complexes with calf thymus DNA have been investigated using absorption spectrophotometry. The zinc complex binds DNA more strongly than cobalt, nickel or copper complexes. The metal complexes are screened for their antibacterial activity against pathogenic bacterial strains. Complexes showed higher activity than the ligand. Copper complex shows more activity than any other complexes under...
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Posted by admin on Dec 31, 2020 in |
The main objective of the present research work to synthesize, characterization, and in-vivo evaluation of Pyridazine derivatives. To study the different synthesized derivatives by using different analytical parameters like IR, Mass, and NMR analysis. And also find out the antihypertensive activity. The studies on the hydralazine group drugs led to the synthesis of many Pyridazine derivatives with a wide activity spectrum on the cardiovascular system. Pyridazine derivatives, a class of compounds containing the N-N bond, exhibit a wide range of pharmacological activities such as antidepressant, antihypertensive, and cardiotonic, etc. Some 6-(substituted phenyl)-2-(substituted methyl)-4,5-dihydropyridazin-3(2H)-one derivative was synthesized by reacting 6-Phenyl substituted 2,3,4,5-Tetrahydro pyridazin-3-one with cyclic secondary amine under Mannich reaction conditions. A total of twenty compounds (vj1-vj20) were synthesized under Mannich reaction conditions. Out of twenty compounds, around six derivatives were selected for evaluation of antihypertensive activities by a non-invasive method using the Tail Cuff method. Most of the compounds showed good antihypertensive activity. Few compounds like vj3, vj6, vj9, vj14, vj19, and vj20 were found to show a highly...
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Posted by admin on Dec 31, 2020 in |
Benzthiazole, Chalcones, and their analogs have a wide variety of biological activities like antihelminthic, antifungal, antibacterial, anti-diabetic, anti-tubercular, anti-inflammatory, anticonvulsant, diuretic etc., In the present research work, an effort has been made to synthesize some new series of novel benzothiazole linked chalcones from 3-amino-acetophenone and potassium thiocyanate which were dissolved in glacial acetic acid at room temperature. Liquid bromine in glacial acetic acid was then added drop-wise, and finally, the reaction mass is quenched and basified with ammonia to obtain the desired Benzthiazole linked chalcone. The progress of the reaction is monitored through TLC. The purity of the compounds was identified by TLC and purified by recrystallization and column chromatography. The structures were determined by IR, 1H NMR, and Mass spectral data. The synthesized benthiazole linked chalcone analogues were screened for anti-tubercular activity by the use of MABA (Microplate Alamar Blue assay) analytical method on H37Rv strain of Mycobacterium tuberculosis. Based on the results of anti-tubercular activity, it can be seen that the compounds containing electron-withdrawing groups like chlorine,...
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Posted by admin on Dec 31, 2020 in |
Nicotinic acetylcholine receptor α3β4 is considered as a potential target for anti-smoking drug discovery. In this study, in-silico approaches, including molecular docking and molecular dynamics simulation were applied to investigate binding affinities of 300 alkaloids into the α3β4 (Pdb id: 6PV8). The docking results showed that most of the alkaloids fitted well into the binding pocket of α3β4. The top hit compounds were A122 (indole alkaloid) and A128 (tropane alkaloid) with their binding affinities of less than -8.0 kcal.mol-1 and the interactions with key residue, Trp149. Structures and binding affinities relationships between the indole and tropane compounds with the α3β4 emphasized the important roles of indole backbone and the benzyl substituent at C3 of tropane scaffold in forming the hydrophobic interactions making good binding affinities. Molecular dynamics simulations revealed the potential of A128 to binding stably with the α3β4 during 20 ns. Binding free energy of the complex A128 – α3β4 was calculated based on Molecular Mechanics – Poisson Boltzmann Surface Area (MM-PBSA) method, which also emphasized the importance...
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