Acceleration of Hydrolytic DNA Cleavage by Dicopper(II) Complexes with p-Cresol-Derived Dinucleating Ligands at Slightly Acidic pH and Mechanistic Insights

2019 ◽  
Vol 92 (4) ◽  
pp. 739-747 ◽  
Author(s):  
Masahito Kodera ◽  
Yuki Kadoya ◽  
Kenta Aso ◽  
Katsuki Fukui ◽  
Akiko Nomura ◽  
...  
2018 ◽  
Vol 69 (1) ◽  
pp. 191-195
Author(s):  
Elena Radu ◽  
Elena Emilia Oprescu ◽  
Cristina Emanuela Enascuta ◽  
Catalina Calin ◽  
Rusandica Stoica ◽  
...  

The dehydration of polysaccharides fraction in the presence of acid catalysts, is a chemical process in which results as secondary product humic matter. In our work, the humic acid mixture was for the first time based on our knowledge extracted from defatted microalgae biomass rich in polysaccharides by standard alkali treatment, followed by precipitation at acidic pH. The dried humic acid mixture has been characterized using infrared spectroscopic measurements (FT-IR). Exfoliated graphite nanoplatelets (xGnP) were used as new adsorbents for this type of humic acids mixture, their adsorption being investigated. The effect of several parameters such as: contact time, concentration of humic acid mixture, concentration of xGnP, temperature and pH of the solutions were studied. The process of adsorption took place with good results, in the following conditions: at a concentration of humic acid mixture of 18.6 mg L-1, an xGnP amount of 0.01 mg in 25 mL of solution, at a temperature of 25 �� and at acidic pH values, in aqueous solution.


2018 ◽  
Vol 69 (8) ◽  
pp. 2304-2305
Author(s):  
Oana Ruxandra Iana ◽  
Dragos Cristian Stefanescu ◽  
Viorel Zainea ◽  
Razvan Hainarosie

Variable pH values for skin have been reported in the literature, all within the acidic range, varying from 4.0 up to 7. 0. The origin of the acidic pH remains conjectural, and several factors have been incriminated with this role, such as eccrine and sebaceous secretions as well as proton pumps. Keeping low levels of pH prevents microbial dispersal as well as multiplication. The skin in the external auditory canal is also covered with this acidic mantle with antimicrobial value. Changes of pH in the external ear can lead to acute otitis externa. This condition is defined by the inflammation and infection of the cutaneous and subcutaneous tissues of the external auditory canal. 10% of the world�s population may suffer from acute otitis externa at least once in their lifetime. This paper aims to consolidate the relevance of an acidic pH in the healthy external ear and its relation to the pathogenesis and treatment of otitis externa through a prospective and interventional clinical study on 80 patients who presented to the outpatient department at Prof. Dr D. Hociota ENT Institute in Buch


2019 ◽  
Vol 15 (5) ◽  
pp. 445-455 ◽  
Author(s):  
Suraj N. Mali ◽  
Sudhir Sawant ◽  
Hemchandra K. Chaudhari ◽  
Mustapha C. Mandewale

Background: : Thiadiazole not only acts as “hydrogen binding domain” and “two-electron donor system” but also as constrained pharmacophore. Methods:: The maleate salt of 2-((2-hydroxy-3-((4-morpholino-1, 2,5-thiadiazol-3-yl) oxy) propyl) amino)- 2-methylpropan-1-ol (TML-Hydroxy)(4) has been synthesized. This methodology involves preparation of 4-morpholino-1, 2,5-thiadiazol-3-ol by hydroxylation of 4-(4-chloro-1, 2,5-thiadiazol-3-yl) morpholine followed by condensation with 2-(chloromethyl) oxirane to afford 4-(4-(oxiran-2-ylmethoxy)-1,2,5-thiadiazol- 3-yl) morpholine. Oxirane ring of this compound was opened by treating with 2-amino-2-methyl propan-1- ol to afford the target compound TML-Hydroxy. Structures of the synthesized compounds have been elucidated by NMR, MASS, FTIR spectroscopy. Results: : The DSC study clearly showed that the compound 4-maleate salt is crystalline in nature. In vitro antibacterial inhibition and little potential for DNA cleavage of the compound 4 were explored. We extended our study to explore the inhibition mechanism by conducting molecular docking, ADMET and molecular dynamics analysis by using Schrödinger. The molecular docking for compound 4 showed better interactions with target 3IVX with docking score of -8.508 kcal/mol with respect to standard ciprofloxacin (docking score= -3.879 kcal/mol). TML-Hydroxy was obtained in silico as non-carcinogenic and non-AMES toxic with good percent human oral absorption profile (69.639%). TML-Hydroxy showed the moderate inhibition against Mycobacteria tuberculosis with MIC 25.00 μg/mL as well as moderate inhibition against S. aureus, Bacillus sps, K. Pneumoniae and E. coli species. Conclusion: : In view of the importance of the 1,2,5-thiadiazole moiety involved, this study would pave the way for future development of more effective analogs for applications in medicinal field.


Author(s):  
Subbiah Latha ◽  
Palanisamy Selvamani ◽  
Thangavelu Prabha

: Natural products have a unique place in the healthcare industry. The genus Commiphora emerged as a potential medicinal with huge benefits as evidenced through its use in various traditional and modern systems of medicine. Therefore, we aimed to prepare a concise review on the pharmacological activities and the indigenous uses of various plant species belonging to the genus Commiphora along with the structural information of various active botanical ingredients present in these plants based on the published literatures and scientific reports. To collect the various published literatures on Commiphora in various journals; to study and classify the available information on the pharmacological uses and chemical constituents; and to present the gathered information as a precise review to serve as a potential reference for future research. Pharmacological and phytochemical data on Commiphora plant species were collected from various journals, books, reference materials, websites including scientific databases, etc for compilation. This review article describes the various pharmacological properties of plants of Commiphora species viz., Anti-arthritic and anti-inflammatory, Anti-atherogenic, Antibacterial, Anti-coagulant, Anti-dicrocoeliasis, Anti-epileptic, Anti-fascioliasis, Anti-fungal, Anti-heterophyidiasis, Anti-hyper cholesterolemic, Anti-hyperlipidemic, Anti-hypothyroidism, Anti-obesity, Anti-osteoarthritic, Anti-osteoclastogenesis, Anti-oxidant, Anti-parasitic, Anti-pyretic, Anti-schistosomiasis, Anti-septic, Anti-thrombotic, Anti-ulcer, Cardioprotective, COX enzyme inhibitory, Cytotoxic /Anti-carcinogenic/Anti-cancer, DNA cleavage, Hypotensive, Inhibits lipid peroxidation, Inhibits NO and NO synthase production, Insecticidal, Local anesthetic, Molluscicidal, Smooth muscle relaxant, Tick repellent activities along with toxicity studies. Furthermore, the review also included various secondary metabolites isolated from various species of Commiphora genus along with their chemical structures serve as a ready resource for researchers. We conclude that the plant species belonging to the genus Commiphora possesses abundant pharmacological properties with a huge treasure of diverse secondary metabolites within themselves. This review indicates the necessity of further in-depth research, pre-clinical and clinical studies with Commiphora genus which may help to detect the unidentified potential of the Commiphora plant species.


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