Inflammation is a vital response provided by the immune system that ensures survival during infection and tissue injury. The aim of the present study was to study the in-vitro anti-inflammatory activity of combined extracts of Opuntia Dillenii, Berberis Aristata and Tinospora Cordifolia Plants. Non-Steroidal Anti-Inflammatory drugs (NSAIDs) are the most common medication used to treat inflammation. But these drugs may cause moderate to severe adverse effects upon long term use. Here, an attempt was made to use the herbal drug combinations to treat inflammation and to evaluate best combination to treat inflammation. HRBC method was used to study the anti-inflammatory activity. The in-vitro results suggest that, the combination of Opuntia dillenii and Berberis aristata inhibits the haemolysis of erythrocytes; so the combination can be used to treat inflammation.
A new series of thiazolidine-4-one derivatives were synthesized in order to determine their anti-inflammatory activity. The compounds were combined in acceptable yield and the structures of all recently blended compounds were set up based on their IR, 1HNMR, and elemental analysis. The synthesized compounds were tested for anti-inflammatory activity, and the compound 4(a) and 4(b) shows significant anti-inflammatory activity and compound 4(c), 4(d), 4(e) also shows appreciable anti-inflammatory activity.
The present investigation of efficient and cost-effective method for the synthesis of 7, 7-dimethyl-4-phenyl tetrahydroquinazaloine-(1H, 3H)-2, 5-dionesderivatives employing dimedone, urea and substituted aromatic aldehydes using methane sulfonic acid as a catalyst under solvent free condition. The newly synthesized compounds were analysed by 1H-NMR and 13CNMR, Mass spectral and Elemental analysis. Antimicrobial activities of the titled compounds were also examined by various strains and exhibited mild to moderate anti-bacterial and anti-fungal activities.
S. Chinnayya Setty, N. Krishnarao*, B.V. Durgarao, V. Narasingrao, P. Ramalakshmi, Shaik Lakshman.
Krohnke 2, 4, 6-Triarylpyridines (TAPs) are efficiently synthesized by using various reactants with ammonium carbonate in water under sealed conditions. Using this protocol, Krohnke pyridines (4a-4q) are prepared in higher yields and purities than with other methodologies without the use of a catalyst or an organic solvent.
K. Balaji*, V. Tejeswara Rao, Anjali Jha, Abdul Razzak, T. V. S. P. V. Satya Guru.
Asthma is a chronic inflammatory disease of airways characterized by sudden attacks of laboured breathing, chest constriction, coughing and excess mucous production. Adenosine receptor was selected as a target as it displays multiple actions i.e. leukotriene antagonist, decrease inflammation, mast cell stabilizer and inhibit release of histamine. Xanthine was selected as a lead molecule as 1, 3, 8-substituted derivative have good selectivity but low to moderate affinity on A2B and 1, 3, 7, 8-substituited derivative have good affinity on A2A and A2B receptor. Selective activation of A2A AR has possible therapeutic approach for treatment of Asthma but have cardiovascular side effect specially diminishing B.P. Selective antagonism of A2B may result adverse effect related to Cystic fibrosis. The purpose of this research was to propose a compound which acts on both A2A and A2B adenosine receptor. SAR, predictions using lipinski’s rule of five, PASS and OSIRIS proposed 1-Allyl-3-ethyl-7-methyl-8-(3, 4, 5-trimethoxyphenyl) xanthine (1). Docking Simulation study of 1 done on A2A and then, A2A receptor was used to prepare model of A2B receptor using Swiss pdb viewer and VMD software. Compound 1 showed all interactions on both [A2A binding energy -6.29kcal/mol, binding affinity 14.11µM, on modified A2A (A2B receptor) binding energy -5.16 kcal/mol and binding affinity 64.54 µM]. So, it is concluded that compound 1 is potential antiasthmatic acting on both A2A and A2B and thus is expected to show minimal cardiovascular and cystic fibrosis side effects.
As a part of our research, in present report an improved process for the synthesis of some novel derivatives of2-phenyl-1H-benzimidazole employing organo acid catalyst which possesses thebasic skeleton in various bioactive compounds. The newly synthesized compounds was obtained from the condensation of reaction between O-Phenylenediamine and various substituted arylaldehydein the presence of camphor sulfonic acid in aqueous medium. The yield of all newly derivatives synthesized compounds was found to be in the range of 90 - 95%. The synthesized compounds were characterized by using 1HNMR, 13CNMR and MASS spectral data together with elemental analysis. In addition to evaluate the biological properties.
N. Krishnarao*, K. Apparao, B. V. Durgarao, V. Narasingrao.
Cancer is major health problem worldwide. The epidermal growth factor receptor (EGFR) play a considerable role in carcinogenesis through their involvement in proliferation, apoptosis, enhanced cell motility etc. Two anilinoquinazoline EGFR tyrosine kinase inhibitors: Gefitinib and Erlotinib have gained approval for patients with Non Small Cell Lung Cancer. Use of these drugs associated with resistance due to secondary point mutation T790M, which substitutes methionine for threonine at amino acid position 790 of EGFR gene domainis major drawback. These findings will certainly affect the development of the next generation of EGFR inhibitors with the ability to overcome T790M. This article include molecular docking simulation of Erlotinib with EGFR receptor so that we can use the same dimension for docking of various molecules with corrected Lipinski’s parameters. Docking of other EGFR inhibitor AEE788 with wild type EGFR and T790M mutant EGFR support the preparation of new EGFR inhibitors which will act also in resistant conditions of first generation EGFR inhibitors. In this docking study binding energy for Erlotinib docking was found to be -6.44Kcal/mol, for AEE788 in wild type EGFR found to be -10.79Kcal/mol and for AEE788 in T790M mutant EGFR found to be -11.05Kcal/mol.
Schiff bases played a special role as chelating ligands in main group and transition metal chemistry because of their stability under a variety of redox condition. In addition they have different biological activity for example; antimicrobial activity and insecticides and further their metal complexes show more enhancements in all these activities. The present work represents the synthesis, spectral characterization, Thermal properties and antimicrobial activity of Novel series of Schiff base derived from 2, 4-bis (hydrazino)-6-substituted triazine and their Schiff base derivatives. A series of metal complexes of Ni (II), Mn (II) and Cu (II) have been synthesized with newly derived biologically active ligands. The probable structure of the complexes has been proposed on the basis of elemental analyses and spectral data. All the complexes of Ni (II), Mn (II) and Cu (II) were screened for their antimicrobial properties.
Background: The intake of anabolic -androgenic steroids (AASs) and nutritional supplements as ergogenic aids has been increasing among young men in Benghazi, Libya. Objectives: To assess the use of AASs and nutritional supplements by undergraduate male students in the faculty of Pharmacy and faculty of Medicine at the University of Benghazi. Moreover, is to investigate the awareness and knowledge of students regarding the health consequences ASSs and nutritional supplements intake. Subjects and Methods: A cross sectional study involved 350 undergraduate male students from both Pharmacy and Medicine the faculty. Self-administered questionnaires were distributed randomly during the period of the study which was conducted from January to May 2019. Results: 31% of the students used AASs and/or nutritional supplements. Out of the 31 %, 53% used protein supplements, 24% used AASs, 9% used both protein and AASs and 14% used other nutritional supplements. Only 8% of the students who used AASs and/or nutritional supplements had experienced some adverse effects. Increased blood pressure was the most prevalent adverse effects among those students (36%). However, 65% of students reported no awareness about health risks of the ergogenic substances presented at the marketing points. Conclusions: Theuse of AASs and nutritional supplements by undergraduate students was without any awareness about the possible health consequences. Hence, an awareness and guidance should be provided by health care professionals providing ergogenic substances.
M. Y. G. Younis*, Narges M. Kablan, Enas A. Mansor, Mohamoud F. Rasheed, Abdelsalam Ali, Isam Denna.
Stannous chloride (SnCl2), an inorganic salt. The known toxicity potential of stannous chloride has given rise to increasing concern about the human. Ginseng is a plant of medical importance and it has been used by elderly Asian to boost physical and mental vitality. Rabbits were orally given sub lethal dose of stannous chloride (20mg/kg BW), while ginseng (100mg/kg BW) was given alone or in combination with stannous chlorid. The tested doses were given to rabbits every day for 12 weeks. Results showed thatSnCl2 caused a significant (PB/0.05) increase in the levels of plasma cholesterol, triglyceride (TG), low density lipoprotein (LDL) and very low density lipoprotein (VLDL), while the level of high density lipoprotein (HDL) decreased. Ginseng alone significantly (PB/0.05) decreased the levels of cholesterol, TG, LDL and VLDL and increased HDL and alleviated the harmful effects of SnCl2on lipid profiles.
Fayrouz A. Khaled*, Nesreen A. Abd- Alhady, Sara M Elgazwi.