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Fulltext One Pot Selective Arylation of 2-Bromo-5-Chloro Thiophene; Molecular Structure Investigation via Density Functional Theory (DFT), X-ray Analysis, and Their Biological Activities

Rasool N, Kanwal A, Rasheed T, Ain Q, Mahmood T, Ayub K, et al.

Int J Mol Sci, 2016;17(7).
PMID: 27367666 DOI: 10.3390/ijms17070912

Synthesis of 2,5-bisarylthiophenes was accomplished by sequential Suzuki cross coupling reaction of 2-bromo-5-chloro thiophenes. Density functional theory (DFT) studies were carried out at the B3LYP/6-31G(d, p) level of theory to compare the geometric parameters of 2,5-bisarylthiophenes with those from X-ray diffraction results. The synthesized compounds are screened for in vitro bacteria scavenging abilities. At the concentration of 50 and 100 μg/mL, compounds 2b, 2c, 2d, 3c, and 3f with IC50-values of 51.4, 52.10, 58.0, 56.2, and 56.5 μg/mL respectively, were found most potent against E. coli. Among all the synthesized compounds 2a, 2d, 3c, and 3e with the least values of IC50 77, 76.26, 79.13 μg/mL respectively showed significant antioxidant activities. Almost all of the compounds showed good antibacterial activity against Escherichia coli, whereas 2-chloro-5-(4-methoxyphenyl) thiophene (2b) was found most active among all synthesized compound with an IC50 value of 51.4 μg/mL. All of the synthesized compounds were screened for nitric oxide scavenging activity as well. Frontier molecular orbitals (FMOs) and molecular electrostatic potentials of the target compounds were also studied theoretically to account for their relative reactivity.
Fulltext Compositional difference in antioxidant and antibacterial activity of all parts of the Carica papaya using different solvents

Asghar N, Naqvi SA, Hussain Z, Rasool N, Khan ZA, Shahzad SA, et al.

Chem Cent J, 2016;10:5.
PMID: 26848308 DOI: 10.1186/s13065-016-0149-0

Carica papaya is a well known medicinal plant used in the West and Asian countries to cope several diseases. Patients were advised to eat papaya fruit frequently during dengue fever epidemic in Pakistan by physicians. This study was conducted to establish Polyphenols, flavonoids and antioxidant potential profile of extracts of all major parts of the C. papaya with seven major solvents i.e. water, ethanol, methanol, n-butanol, dichloromethane, ethyl acetate, and n-hexane.
Fulltext Water Spinach, Ipomoea aquatic (Convolvulaceae), Ameliorates Lead Toxicity by Inhibiting Oxidative Stress and Apoptosis

Dewanjee S, Dua TK, Khanra R, Das S, Barma S, Joardar S, et al.

PLoS One, 2015;10(10):e0139831.
PMID: 26473485 DOI: 10.1371/journal.pone.0139831

BACKGROUND: Ipomoea aquatica (Convolvulaceae), an aquatic edible plant, is traditionally used against heavy metal toxicity in India. The current study intended to explore the protective role of edible (aqueous) extract of I. aquatica (AEIA) against experimentally induced Pb-intoxication.
METHODS: The cytoprotective role of AEIA was measured on mouse hepatocytes by cell viability assay followed by Hoechst staining and flow cytometric assay. The effect on ROS production, lipid peroxidation, protein carbonylation, intracellular redox status were measured after incubating the hepatocytes with Pb-acetate (6.8 μM) along with AEIA (400 μg/ml). The effects on the expressions of apoptotic signal proteins were estimated by western blotting. The protective role of AEIA was measured by in vivo assay in mice. Haematological, serum biochemical, tissue redox status, Pb bioaccumulation and histological parameters were evaluated to estimate the protective role of AEIA (100 mg/kg) against Pb-acetate (5 mg/kg) intoxication.
RESULTS: Pb-acetate treated hepatocytes showed a gradual reduction of cell viability dose-dependently with an IC50 value of 6.8 μM. Pb-acetate treated hepatocytes exhibited significantly enhanced levels (p < 0.01) of ROS production, lipid peroxidation, protein carbonylation with concomitant depletion (p < 0.01) of antioxidant enzymes and GSH. However, AEIA treatment could significantly restore the aforementioned parameters in murine hepatocytes near to normalcy. Besides, AEIA significantly reversed (p < 0.05-0.01) the alterations of transcription levels of apoptotic proteins viz. Bcl 2, Bad, Cyt C, Apaf-1, cleaved caspases [caspase 3, caspase 8 and caspase 9], Fas and Bid. In in vivo bioassay, Pb-acetate treatment caused significantly high intracellular Pb burden and oxidative pressure in the kidney, liver, heart, brain and testes in mice. In addition, the haematological and serum biochemical factors were changed significantly in Pb-acetate-treated animals. AEIA treatment restored significantly the evaluated-parameters to the near-normal position.
CONCLUSION: The extract may offer the protective effect via counteracting with Pb mediated oxidative stress and/or promoting the elimination of Pb by chelating. The presence of substantial quantities of flavonoids, phenolics and saponins would be responsible for the overall protective effect.
Ionic liquid as a potential solvent for preparation of collagen-alginate-hydroxyapatite beads as bone filler

Iqbal B, Sarfaraz Z, Muhammad N, Ahmad P, Iqbal J, Khan ZUH, et al.

J Biomater Sci Polym Ed, 2018 07;29(10):1168-1184.
PMID: 29460709 DOI: 10.1080/09205063.2018.1443604

In this study, collagen/alginate/hydroxyapatite beads having different proportions were prepared as bone fillers for the restoration of osteological defects. Ionic liquid was used to dissolve the collagen and subsequently the solution was mixed with sodium alginate solution. Hydroxyapatite was added in different proportions, with the rationale to enhance mechanical as well as biological properties. The prepared solutions were given characteristic bead shapes by dropwise addition into calcium chloride solution. The prepared beads were characterized using FTIR, XRD, TGA and SEM analysis. Microhardness testing was used to evaluate the mechanical properties. The prepared beads were investigated for water adsorption behavior to ascertain its ability for body fluid uptake and adjusted accordingly to the bone cavity. Drug loading and subsequently the antibacterial activity was investigated for the prepared beads. The biocompatibility was assessed using the hemolysis testing and cell proliferation assay. The prepared collagen-alginate-HA beads, having biocompatibility and good mechanical properties, have showed an option of promising biologically active bone fillers for bone regeneration.
Fulltext Nigella sativa fixed and essential oil modulates glutathione redox enzymes in potassium bromate induced oxidative stress

Sultan MT, Butt MS, Karim R, Ahmed W, Kaka U, Ahmad S, et al.

BMC Complement Altern Med, 2015;15:330.
PMID: 26385559 DOI: 10.1186/s12906-015-0853-7

Nigella sativa is an important component of several traditional herbal preparations in various countries. It finds its applications in improving overall health and boosting immunity. The current study evaluated the role of fixed and essential oil of Nigella sativa against potassium bromate induced oxidative stress with special reference to modulation of glutathione redox enzymes and myeloperoxidase.
Fulltext A convenient method for the synthesis of (prop-2-ynyloxy)benzene derivatives via reaction with propargyl bromide, their optimization, scope and biological evaluation

Batool T, Rasool N, Gull Y, Noreen M, Nasim FU, Yaqoob A, et al.

PLoS One, 2014;9(12):e115457.
PMID: 25545159 DOI: 10.1371/journal.pone.0115457

A highly convenient method has been developed for the synthesis of (prop-2-ynyloxy) benzene and its derivatives. Differently substituted phenol and aniline derivatives were allowed to react with propargyl bromide in the presence of K2CO3 base and acetone as solvent. The compounds were synthesized in good yields (53-85%). Low cost, high yields and easy availability of compounds helped in the synthesis. Electron withdrawing groups favor the formation of stable phenoxide ion thus in turn favors the formation of product while electron donating groups do not favor the reaction. Phenol derivatives gave good yields as compared to that of aniline. As aprotic polar solvents favor SN2 type reactions so acetone provided best solvation for the reactions. K2CO3 was proved to be good for the synthesis. Antibacterial, Antiurease and NO scavenging activity of synthesized compounds were also examined. 4-bromo-2-chloro-1-(prop-2-ynyloxy)benzene 2a was found most active compound against urease enzyme with a percentage inhibition of 82.00±0.09 at 100 µg/mL with IC50 value of 60.2. 2-bromo-4-methyl-1-(prop-2-ynyloxy)benzene 2d was found potent antibacterial against Bacillus subtillus showing excellent inhibitory action with percentage inhibition of 55.67±0.26 at 100 µg/ml wih IC50 value of 79.9. Based on results, it can be concluded that some of the synthesized compounds may have potential antiurease and antibacterial effects against several harmful substances.
Fulltext Chemical composition, antioxidant and antimicrobial potential of essential oils from different parts of Daphne mucronata Royle

Ashraf I, Zubair M, Rizwan K, Rasool N, Jamil M, Khan SA, et al.

Chem Cent J, 2018 Dec 17;12(1):135.
PMID: 30556121 DOI: 10.1186/s13065-018-0495-1

This research work was executed to determine chemical composition, anti-oxidant and anti-microbial potential of the essential oils extracted from the leaves and stem of Daphne mucronata Royle. From leaves and stem oils fifty-one different constituents were identified through GC/MS examination. The antioxidant potential evaluated through DPPH free radical scavenging activity and %-inhibition of peroxidation in linoleic acid system. The stem's essential oil showed the good antioxidant activity as compared to leaves essential oil. Results of Antimicrobial activity revealed that both stem and leaves oils showed strong activity against Candida albicans with large inhibition zone (22.2 ± 0.01, 18.9 ± 0.20 mm) and lowest MIC values (0.98 ± 0.005, 2.44 ± 0.002 mg/mL) respectively. Leaves essential was also active against Escherichia coli with inhibition zone of 8.88 ± 0.01 mm and MIC values of 11.2 ± 0.40 mg/mL. These results suggested that the plant's essential oils would be a potential cradle for the natural product based antimicrobial as well as antioxidant agents.