scholarly journals Synthesis, Antibacterial, Thrombolytic and Cytotoxic Evaluation of Substituted and Un-substituted Selenium-n-heterocyclic Carbene Adducts

Author(s):  
Amna Kamal ◽  
Muhammad Adnan Iqbal ◽  
Haq Nawaz Bhatti ◽  
Abdul Ghaffar

Abstract N-heterocyclic carbene salts bearing alkyl substituents (1-8) and their selenium N-heterocyclic carbene adducts (9-12) were synthesized and characterized by elemental analysis, FT-IR, NMR (1HNMR, 13CNMR) spectroscopic techniques. All the adducts were found to be stable in air and moisture at room temperature. Compounds (5-12) were evaluated against Bacillus subtilis Macrococcus brunensis and Bacillus cereus in vitro. The biological assay revealed that antibacterial activity of Selenium-N-heterocyclic carbene adducts are comparatively better than the salts. MIC and inhibition zone values showed that Bacillus subtilis is more active to selenium adducts (9-12) than Macrococcus brunensis and Bacillus cereus whereas opposite in the salts (5-8). In vitro studies of hemolysis and thrombolysis demonstrated that the synthesized compounds are innocuous for pre-clinical trials to mouse blood.

2017 ◽  
Vol 901 ◽  
pp. 124-132
Author(s):  
Artania Adnin Tri Suma ◽  
Tutik Dwi Wahyuningsih ◽  
Deni Pranowo

Some novel N-phenylpyrazolines were synthesized and investigated for their antibacterial activitiy. Chalcones 2-4 which were prepared from acetophenone and veratraldehyde derivatives were reacted with phenylhydrazine to give N-phenylpyrazolines 5-7. All of the synthesized compounds were characterized using FTIR, GC-MS, and NMR spectrometers. Further, antibacterial activity of N-phenylpyrazolines were evaluated by agar well-diffusion method against Staphylococcus aureus, Bacillus cereus, Bacillus subtilis, Escherichia coli, and Shigella flexneri. The highest activity (highest inhibition zone) of compound 5 was 2.6 mm (at 1000 ppm) against B. subtillis, compound 6 was 7.25 mm (at 1000 ppm) against S. aureus, and compound 7 was 6.75 mm (at 500 ppm) against S. aureus. The results indicated that compound 6 and 7 exhibited promising antibacterial activity.


Author(s):  
Yori Turu Toja ◽  
Eddy Suprayitno ◽  
Aulanni’am ◽  
Uun Yanuhar

Indonesia has many local plants with potential as herbal antibacterial properties, one of which is the local black fruit of Wandama. The objective of this study is to determine the antibacterial activity of the extract of black fruit seed against A. Hydrophila by in vitro and FTIR by Tilapia. The benefit of this research is to make black fruit seed extract as a natural remedy against tilapia attacked by Aeromonas Hydrophila. The antibacterial activity of black fruit seed extract against A. Hydrophila is investigated in vitro and using FTIR on tilapia in this research. The aim of this study is to establish black fruit seed extract as a natural treatment for tilapia infected with Aeromonas Hydrophila. The disc approach was used to conduct the in vitro research. Agar medium was poured into a sterile petri dish, and 2 drops of bacteria from the liquid medium were uniformly distributed and cooled. On the press, disc paper with black fruit seed extract was put and incubated for 18-24 hours at 35 C. An FTS 1000 version spectrophotometer system was used for the FTIR test. For the FT-IR study, a fraction of dried black fruit seeds was used. For clear preparation, 100 mg of dry extract is condensed in KBr pellets. A specimen of loaded black fruit seed samples was analyzed using FT-IR spectroscopy with a scanning range of 400-4000 cm-1 and a resolution of 4 cm-1. The results showed that the ethyl acetate fraction produced an inhibition zone (13.65 mm), the water fraction produced an inhibition zone (11.21 mm), and the n-hexane fraction produced the weakest inhibition zone (11.21 mm) (5.31mm). The concentration test results from 125 ppm, 250 ppm, 500 ppm and 1000 ppm obtained a large inhibition zone at a concentration of 1000 ppm with an inhibition zone area of 11.43 + 0.02. The absorbance value of black fruit seed extract in ethyl acetate solvent at 3430 cm-1 revealed the absorption band with the strongest vibration of the hydroxylate (-OH) functional group, according to FTIR research. Final thoughts with an average value of 13.65 + 0.06, black fruit seed extract using ethyl acetate can inhibit A. Hydrophila bacteria.


2021 ◽  
Vol 34 (1) ◽  
pp. 209-215
Author(s):  
Pravin S. Kulkarni ◽  
Swapnil R. Sarda ◽  
Amol U. Khandebharad ◽  
Mazahar Farooqui ◽  
Brijmohan R. Agrawal

A new series of 5-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-3-aryl-1,2,4-oxadiazole (6a-o) have been synthesized by a cyclocondensation reaction of ethyl 5-(4-chlorophenyl)-1-phenyl-1H-pyrazole-3- carboxylate (3a-c) with aryl imidoxime (5a-e). The newly synthesized pyrazolyl-1,2,4-oxadiazole (6a-o) derivatives were characterized by spectroscopic techniques and screened for in vitro antibacterial activity against Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178), Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388) and in vitro antifungal activity against Aspergillus niger (ATCC 504) Candida albicans (NCIM 3100).


2020 ◽  
Vol 9 (4) ◽  
pp. 1725-1736

Infectious diseases are emerging at an alarming rate, which is posing a great threat to the population because of the continuous battle with pathogens. .Green plants are rich in bioactive molecules providing valuable sources of antimicrobial compounds. Antibacterial activity of various solvent extracts of E.cotinifolia leaves was screened against some human pathogenic bacteria like Bacillus subtilis, Bacillus cereus, Staphylococcus aureus, Klebsiella pneumonia, Salmonella typhi, Escherichia coli, and Enterobacter aerogenes by agar cup diffusion and minimum inhibitory concentrations (MIC) determined by micro broth dilution Methanol extract of Euphorbia cotinifolia was separated by silica gel column, leading to the isolation of new compounds and structure was elucidated by spectroscopic techniques. The solvent extracts and newly isolated compounds were tested for their antibacterial activity. Methanol and ethyl acetate recorded significant activity against Enterobacter aerogenes and Bacillus subtilis, which showed a maximum inhibition zone of 17.25 mm. MIC ranged from 0.3- 1.25 mg/mL for methanol and ethyl acetate extracts. The inhibition zone measured against test bacteria was 15.25-19.50 mm, 13.50-19.25 mm, 12- 18.50 mm, 15- 20 mm, and 13- 19 mm in ECMF1, ECMF2, ECMF3, compound 1, respectively, and MIC of the compounds 1 and 2 was 78- 833 µg/ ml and 139- 625 µg/ ml, respectively. The identification of active compounds of methanol extract, which would lead to the discovery of new antimicrobial drugs from the test plant.


2021 ◽  
Vol 17 ◽  
Author(s):  
Bambang Susilo ◽  
Abd. Rohim ◽  
Midia Lestari W. H.

Background: S. cristaefolium is the brown seaweed extracted using the serial technique with different solvents. Methods: S. cristaefolium powder (50 mesh) was extracted with hexane, ethyl acetate, and methanol respectively. The S. cristaefolium powder residue had been dried before being re-extracted with the next different solvents. Three serial extracts were obtained and named as the 1-stage extract, 2-stage extract, and 3-stage extract. Besides, a single-step extract (extraction using only methanol) was also produced to compare with three serial extracts in antibacterial activity tests (against E. coli and S. aureus). The three serial extracts were detected their antibacterial compounds using GC-MS, LC-HRMS, and FT-IR. Results: The 3-stage extract had the highest extraction yield. On S. aureus, the inhibition zone in all extracts was not significantly different. On E.coli, the highest inhibition zone (5.42±0.14 mm) was the 3-stage extract, indeed it is higher than both antibiotic and a single-step extract. Phenol, 9-Tricosene(Z)-, palmitic acid, and oleamide were contained in all extracts. Other antibacterial compound types, both the 1-stage and 2-stage extracts contained 8 types whilst the 3-stage extract contained the most types (12 types). Particularly, hexyl cinnamic aldehyde and betaine were detected only in the 3-stage extract with the dominant area. The carboxylic acid groups were detected in all extracts to confirm the fatty acid structure. Several cinnamic aldehyde groups were detected only in the 3-stage extract. Conclusions: Thus, the extraction technique serially could produce the 3-stage extract which has the strongest antibacterial activity and the richest antibacterial compounds.


2022 ◽  
Vol 8 (1) ◽  
pp. 80
Author(s):  
Yongmei Li ◽  
Mengyuan Xia ◽  
Pengbo He ◽  
Qiaoming Yang ◽  
Yixin Wu ◽  
...  

Citrus is among the most important plants in the fruit industry severely infected with pathogens. Citrus green mold caused by Penicillium digitatum is one of the most devastating diseases during post-harvest stages of citrus fruit. In this study, a potential endophyte Bacillus subtilis L1-21, isolated from healthy citrus plants, was assessed for its biocontrol activity against the pathogen P. digitatum. Based on an in vitro crosstalk assay, we suggested that B. subtilis L1-21 inhibits the pathogen with an inhibition zone of 3.51 ± 0.08 cm. Biocontrol efficacy was highest for the fermented culture filtrate of B. subtilis L1-21. Additionally, using GC-MS analysis, 13 compounds were detected in the extract of this endophyte. The culture filtrate in Landy medium could enlarge and deform pathogen spores and prevent them from developing into normal mycelium. Accordingly, the Landy culture filtrate of B. subtilis L1-21 was stable in the temperature range of 4–90 °C and pH of 3–11. Further, MALDI-TOF-MS for B. subtilis L1-21 detected surfactin, fengycin, bacillaene and bacilysin as potential antifungal compounds. GFP-tagged B. subtilis L1-21 easily colonized in citrus fruit peel and pulp, suggesting its role in eliminating the fungal pathogen. Altogether, it is highly expected that the production of antifungal compounds, and the colonization potential of B. subtilis L1-21 are required against the post-harvest P. digitatum pathogen on citrus fruit.


Author(s):  
K Sunand ◽  
K Vinay Kumar ◽  
K Ashwini ◽  
P Suresh Kumar ◽  
S Vishnu ◽  
...  

Aim: To synthesize and evaluate 4-aminoantipyrine related schiff’s bases as antibacterial agents. Objective: To synthesize, purify, characterize and evaluate 4-aminoantipyrine. Method: Schiff bases derived from 4-aminoantipyrine play a vital role in biological and pharmacological activities. Knowing the importance of 4-aminoatipyrine schiff bases and their analogues wide varieties of bioactivities like analgesic, antiviral, antipyretic, anti-rheumatic, antimicrobial and anti-inflammatory activities have been widely studied. 4-aminoantipyrine compounds C1 (anisaldehyde), C2 (p-hydroxybenzaldehyde) and C3(vanillin) were prepared by condensation between 4-amino antipyrine and substituted aromatic benzaldehydes. The products were purified by recrystallization by using ethanol, characterized by IR spectroscopy. The N-H stretching in 4-aminoantipyrine is shown at 3430 cm-1 and -3325 cm-1. The -HC=N- stretching is observed in the range of 1508-1504 cm-1 The –OCH3 stretching is found at 1888 cm-1. 4-amino antipyrine related schiff’s bases evaluated their activity as antimicrobials in-vitro by spread plate method against E.coli. Schiff bases have potent antibacterial activity with gram negative bacteria E.coli. Results: Synthesis and characterization of a schiff bases derived from substituted benzaldehydes and 4-aminoantipyrine was evaluated and characterized with the IR spectroscopic techniques and schiff bases have shown potent antibacterial activity against E.Coli.


2018 ◽  
Vol 68 (2) ◽  
pp. 129-144 ◽  
Author(s):  
Maria-Viorica Ciocilteu ◽  
Andreea Gabriela Mocanu ◽  
Adriana Mocanu ◽  
Catalin Ducu ◽  
Oana Elena Nicolaescu ◽  
...  

Abstract The main objective of this study was to synthesize hydroxyapatite-ciprofloxacin composites using a chemical precipitation method and to evaluate the properties and in vitro release profile of the drug from the hydroxyapatite-ciprofloxacin composites. Composite characterization was achieved by FT-IR, XRD and DLS. Ciprofloxacin determination was accomplished by HPLC, resulting in good incorporation efficiency of the drug (18.13 %). The in vitro release study (Higuchi model C = K t1/2 and Ritger-Peppas model, C = K t0.6) showed a diffusion-controlled mechanism. The antibacterial activity showed that the bacterial growth inhibition zones were approximately equal for the synthesis composites and for the mechanical mixture on the Staphylococcus aureus germ. The use of hydroxyapatite, which is a biocompatible, bioactive and osteoconductive material, with ciprofloxacin, which has good antibacterial activity in this composite, makes it suitable for the development of bone grafts. Furthermore, the synthesis process allows a slow local release of the drug.


2019 ◽  
Vol 41 (6) ◽  
pp. 1090-1090
Author(s):  
Mehmet Poyraz Mehmet Poyraz ◽  
Musa Sari Musa Sari ◽  
Halil Berber Halil Berber ◽  
Nursenem Karaca and Fatih Demirci Nursenem Karaca and Fatih Demirci

A new Schiff base, namely 2-methoxy-6-((2-(4 nitrophenyl) hydrazineylidene) methyl)phenol was synthesized and characterized by melting points, elemental analysis, thermogravimetric analysis and spectroscopic techniques (FT-IR, 1H-NMR and UV-VIS spectra). The chemical structure of compound was further confirmed by single crystal structural X-ray diffraction. The Schiff base is crystallized in the triclinic space group P-1. In the crystal, molecules are linked by O-H…O hydrogen bonds between the hydroxy “-O-” atom and the methoxy “-O-” atom. Furthermore, the synthesized Schiff base was tested for the in vitro anticandidal activities using CLSI broth microdilution method against human pathogenic Candida albicans, C. parapsilosis and C. krusei standard strains. In the anticandidal activity test results, the new Schiff base was found to be effective at 1 mg/mL - 0.25 mg/mL concentrations. (The last line omitted) (The sentence marked in red will be deleted)


Author(s):  
Rini Hamsidi ◽  
Wahyuni Wahyuni ◽  
Adryan Fristiohady ◽  
Muhammad Hajrul Malaka ◽  
Idin Sahidin ◽  
...  

Carthamus tinctorius Linn, also known as safflower, is a plant with the potential of being used in the production of antimalarial drugs. The purpose of this study was to isolate and identify the steroid compounds in the safflower and determine its antimalarial activity in vitro. The isolation process was conducted through extraction and chromatography methods. Then, the characterization of the isolated compounds was conducted through spectroscopic techniques which include Fourier Transform Infrared Spectroscopy (FT-IR), NMR 1-D (1H and 13C-NMR), and NMR 2-D (HMQC, HMBC, and H-H COZY) as well as comparing data with the existing literatures. In addition, the tests conducted were with variations of isolate concentrations (10, 1, 0.1, 0.01, and 0.001 μg/mL) against 3D7 strain of Plasmodium falciparum. Based on the FT-IR spectroscopic data, the steroid compounds isolated from safflowers might be stigmasterols. In addition, the isolates had -OH functional group in the region of 3431 cm-1, C-O in the region of 1053 cm-1, and Csp3-H in regions of 2960, 2934, and 2865 cm-1. The NMR 1-D data showed presence of 29 carbon atoms, while the protons were 48 in number. Furthermore, the IC50 value of the compound was 34.03 μg/mL with a percentage inhibition of 43.92% against the growth of P. falciparum. Therefore, it was classified as inactive agent in inhibiting the growth of malaria parasites, however, it could be used as a marker compound in C. tinctorius Linn extract.


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